СОСТАВ АЭРОЗОЛЯ, НАХОДЯЩИЙСЯ ПОД ДАВЛЕНИЕМ

Изобретение относится к химико-фармацевтической промышленности и касается состава аэрозоля, в частности к медикаментам для инъекций. Изобретение заключается в том, что состав азрозоля содержит сжиженный гидрофтороалкан, диспергируемый в нем порошкообразный медикамент и растворимый в указанном гидрофтороалкане полимер, причем полимер включает в себя повторяющиеся структурные единицы, представляющие собой амидосодержащие единицы и единицы, содержащие сложный эфир карбоновой кислоты. Изобретение обеспечивает создание экологически чистого состава аэрозоля, в котором поддерживается необходимое для надежной работы давление и в котором обеспечивается хорошая растворимость и стабилизация лекарственных препаратов. 18 з.п. ф-лы, 3 табл.

СРЕДСТВО И СПОСОБ ДЛЯ ЛЕЧЕНИЯ НЕЙРОСЕНСОРНОЙ ТУГОУХОСТИ

Изобретение относится к области медицины, а именно к оториноларингологии, и касается лечения нейросенсорной тугоухости. Способ включает назначение этиотропной и симптоматической терапии в соответствии с международными и национальными рекомендациями, в сочетании с лекарственным препаратом Семакс в форме носовых капель, который вводят в каждую половину полости носа пациента в дозировке 1-1,5 мг 3 раза в день в течение трех суток, далее по 0,5-1 мг в течение двух недель и затем по 150-300 мкг в продолжении двух недель. Изобретение обеспечивает уменьшение порога слухового восприятия пациента, улучшение разборчивости речи и уменьшение вероятности нежелательных реакций. 3 ил., 1 пр.

СПОСОБ ЛЕЧЕНИЯ СПАСТИЧЕСКОЙ ДИПЛЕГИИ

Способ лечения спастической диплегии, включающий медикаментозную терапию, отличающийся тем, что в качестве медикаментозной терапии используют введение аминалона 0,25-0, 5 г 2-3 раза в день в течение 6-8 мес, церебролизина 1,0-1,2 мл в/м курс 15-20 инъекций через день, префизона 1 мл в/м ежедневно курс 15-20 инъекций, пирогенала 100-200 МПД 15-20 инъекций в течение 1-1,5 мес, мидокалма 50-75 мг 2 раза в день в течение 1-1,5 мес, витамина B12 150-300 мкг 15-20 инъекций (через день), причем инъекции витамина B12 и церебролизина чередуют через день, через 1,5 мес после начала медикаментозной терапии проводят лечебную физкультуру с тепловыми процедурами, а после окончания медикаментозной терапии проводят гипнотерапию в течение 3-5 мес через день.

Применение пептида АКТГ(6-9)-ПГП для анальгетического эффекта при боли, вызванной температурным раздражением

Изобретение относится к области биотехнологии, конкретно к биологически активным пептидным фрагментам АКТГ, и может быть использовано в медицине для анальгетического эффекта при боли, вызванной температурным раздражением. Для этой цели применяют пептид АКТГ-ПГП структуры His-Phe-Arg-Trp-Pro-Gly-Pro. Изобретение позволяет достичь анальгетического эффекта при использовании малых доз пептида. 1 табл., 1 пр.

КОМПОЗИЦИЯ, СОДЕРЖАЩАЯ СОЛИ ПЕПТИДОВ С ПОЛИЭФИРАМИ, ИМЕЮЩИМИ КОНЦЕВЫЕ КАРБОКСИГРУППЫ И СПОСОБ ЕЕ ПОЛУЧЕНИЯ

Данное изобретение касается новых солей, состоящих из катиона, произведенного из пептида, содержащего одну основную группу, и аниона, произведенного из полиэфира с концевыми карбоксигруппами, способов приготовления таких солей и применения этих солей в производстве фармацевтических композиций с пролонгированным действием. Соли данного изобретения обладают множеством свойств, используемых для приготовления фармацевтических препаратов пролонгированного действия, независимо от того, находятся ли эти соли в чистой форме или в смеси либо с избытком свободной, несвязанной формы пептида, либо с избытком свободного полиэфира.

Способ обработки адреналина для придания ему устойчивости

ACTH-Fragmente enthaltende pharmazeutische Zusammensetzungen zur Behandlung von Schockzuständen sowie von respiratorischen und Herz-Kreislauf-Insuffizienzen.

Im Dickdarm zerfallende, Polypeptide enthaltende orale Formulierungen.

Manufacture of biologically active fission products of the adrenocorticotropic hormone

Biologically active fission products of the adrenocorticotropic hormone are obtained by hydrolysing the hormone and simultaneously dialysing the reaction solution, the fission products being isolated from the dialysate. The hydrolysis vessel is preferably a tube of flexible semipermeable material e.g. "Cellophane" (Registered Trade Mark) closed at one end, capable of being rotated, and arranged within a somewhat larger glass tube which is immersed in a water bath at a predetermined temperature. The external liquid used for dialysis has approximately the same pH as the internal liquid, and the external liquid is continuously renewed. Preferred hydrolytic agents are proteolytic agents such as pepsin or trypsin, but other agents such as dilute hydrochloric acid may be used. In examples (a) the adrenocorticotropic hormone from pig pituitaries is hydrolysed with 0.05 N hydrochloric acid containing pepsin at 37 DEG C. and the external liquid is 0.05 N hydrochloric acid continuously stirred. Every ...

New adrenocorticotrophic hormone preparations and processes for making same

An ACTH preparation of enhanced and prolonged action is formed by mixing an injectable aqueous solution of ACTH with one or more salts, hydroxides, or oxides, of the metals zinc, nickel, cobalt, copper and iron, which form a sparingly soluble complex with ACTH at a pH approximately that of the tissue fluid. The insoluble complex may be formed prior to injection, being maintained at pH 6 to 8 by tertiary sodium phosphate, or deposited after injection of an acidic solution. The metal compound e.g. zinc phosphate, hydroxide oxide, may be present from 5 to 15 mg. per 100 U.S.P. Units of ACTH and the aqueous solvent may contain 0,5 per cent phenol and 2,5 per cent glycerol.

PHARMACEUTICAL PREPARATIONS OF CORTICOTROPIN-ACTIVE POLYPEPTIDES AND THE PRODUCTION THEREOF

Improvements in or relating to a therapeutically active composition comprising acth

Phosphorylated hesperidin containing at least three phosphorus atoms per molecule is prepared by dissolving hesperidin in a heterocyclic nitrogeneous organic solvent (pyridine, quinoline) and adding an inorganic oxygenated phosphohalogen esterifying agent, e.g. phosphorus oxychloride. The mixture is quenched with water at a temperature below 40 DEG C., filtered, the filtrate neutralized and the ester precipitated by addition of a C1 to C4 aliphatic alcohol. The product may be purified by dissolving in water and reprecipitated with alcohol. Other precipitating agents are acetone, aliphatic ethers and ethyl acetate. The ester may be used in therapeutic compositions containing ACTH (see Group VI).ALSO:A therapeutically active composition comprises ACTH and biochemically active phosphorylated hesperidin (i.e. active as a hyaluronidase inhibitor in vitro tests and in in vitro intradermal dye spreading and capillary permeability tests) containing at least three phosphorus atoms per molecule.

DERMATOLOGICAL COMPOSITION

... 1487543 Dermatological compositions DSO PHARMACHIM 7 May 1976 [11 May 1975] 18963/76 Heading A5B A dermatological composition comprises from 5 to 10 parts by weight of ichthyol, from 0.05 to 0.1 part by weight of dexamethasone, from 0.5 to 1 part by weight of salicylic acid, from 0.1 to 0.3 part by weight of Vit. A, palmitate and, in an amount to make the composition up to 100 parts by weight, an ointment base.

Corticotropin reaction complexes

A substantially water-insoluble reaction complex comprises corticotropin and alginic acid, carboxyethyl cellulose, carboxymethyl-cellulose, carboxymethylhydroxyethylcellulose, cellulose sulphate or cellulose acetate phthalate. The complex may be dispersed in an injectable pharmaceutical extending medium, e.g. isotonic saline solution, water and vegetable oils.

Use of antagonists of morphine in the preparation of drugs for purpose immunomodulator and antiviral, in particular intended to treat the acquired immuno-overdrawn states.

Treatment of HIV

Treatment of HIV

Treatment of HIV

Treatment of HIV

SALZE VON PEPTIDEN MIT CARBOXY-TERMINIERTEN POLYESTERN

SALTS OF PEPTIDEN WITH CARBOXY SCHEDULING POLYESTERS

USE FROM MORPHINE ANTAGONISTS TO THE PRODUCTION OF MEDICINES WITH IMMUNMODULATORI AND ANTIVIRAL EFFECT, IN PARTICULAR INTENDS FOR THE TREATMENT OF ACQUIRED CONDITIONS OF LACK OF IMMUNE.

Procedure for the production of new 5-Aroylpyrrolderivaten and their salts

Procedure for the production of new 5-Aroylpyrrolderivaten and their salts

Procedure for the production of new 5-Aroylpyrrolderivaten

A PHYSIOLOGICALLY EFFECTIVE POLYPEPTID ABSTENTION PHARMACEUTICAL COMPOSITION

Beta-endorphin/crf gene therapy for locally combating pain

Improved chimeric toxins

PYRROLIDINE DERIVATIVES

UTILIZATION OF MORPHINE ANTAGONISTS IN THE PREPARATION OF DRUGS HAVING AN IMMUNOMODULATOR AND ANTIVIRAL EFFECT, PARTICULARLY FOR TREATING ACQUIRED IMMUNODEFICIENCY STATES

MEDICATION HAVING PENETRATION THROUGH CUTANEOUS SURFACES INTO ARTICULAR AND MUSCULAR AREAS

MEDICATION HAVING PENETRATION THROUGH CUTANEOUS SURFACES INTO ARTICULAR AND MUSCULAR AREAS A medication that penetrates the surface of the skin is provided. The articular and muscular areas subject to discomfort may be relieved by the topical application of the medication. The medication has a penetrant of dimethyl sulfoxide, an anti-inflammatory agent, made from glucocorticoids, and a topical anesthetic compound. The medication greatly relieves pain and reduces swelling.

TREATMENT OF OPTIC NEURITIS

The present invention provides a method for treating a patient having demyelinating optic neuritis (DON) comprising the sequential or simultaneous administration of a steroid compound and an interferon-beta protein. It is found that early, aggressive treatment of IFN-b is beneficial in such a treatment regimen, for example where the interferon-beta protein is administered at a cumulative weekly dose of more than 12 MIL). The method according to the invention is particularly suitable and beneficial for treatment of patients having early stage DON. In particular, the DON that will benefit from being treated according to the present invention may be in subclinical stage.

OVULATION-PREVENTING AGENT FOR HORMONAL CONTRACEPTION

COMPOSITIONS FOR INHALATION

Pharmaceutical compositions containing a mixture of a pharmaceutically activ e polypeptide and an enhancer compound which enhances the systemic absorption of the polypeptide in the lung of a patient, the mixture being in the form of a dry powder, in which at least 50 % of the total mass of polypeptide and enhancer consists of primary particles having a diameter less than or equal to about 10 microns, the primary particles optionally being formed into agglomerates; and methods of delivering such compositions by inhalation.

OVULATION-PREVENTING AGENT FOR HORMONAL CONTRACEPTION

Ovulation-inhibiting means for hormonal contraception, comprising two hormone constituents packed spatially separate in a packing unit intended for chronologically sequential, oral administration, each thereof being composed of a plurality of daily hormone units accommodated spatially separate and individually removable in the packaging unit, whereby a first of said hormone constituents contains essentially only an estrogen preparation effecting a disturbance of the follicle stimulation as hormonal agent but the second hormone constituent contains an estrogen preparation and a gestagen preparation at least in a dose adequate for inhibiting ovulation, characterized in that the total number of daily hormone units is equal to the total number of days in the desired cycle; in that the first hormone constituent covers 5 through 14 daily units and the second hormone constituent covers 23 through 14 daily units; and in that the number of daily units of the first hormone constituent is lower than ...

SALTS OF PEPTIDES WITH CARBOXY-TERMINATED POLYESTERS

... 2136751 9324150 PCTABS00028 This invention relates to novel salts composed of a cation derived from a peptide containing at least one basic group and an anion derived from a carboxy-terminated polyester, processes for the manufacture of such salts, and the use of such salts in the manufacture of extended release pharmaceutical compositions. The salts of the invention possess a variety of properties which are useful in the formulation of extended release pharmaceutical compositions, whether the salts are in pure form or are in admixture with either an excess of the peptide in its free, unbound form or an excess of the free polyester.

Furniture

Verfahren zur Darstellung des corticotropen Hormons.

Furniture

Verfahren zur Herstellung eines adrenocorticotropen Präparates

Verfahren zur Gewinnung eines Gemisches von biologisch wirksamen Produkten.

Verfahren zur Herstellung von langwirkenden Suspensionen einer Komplexverbindung von adrenokortikotropen Hormon (ACTH)

Verfahren zur Reinigung des adreno-corticotropen Hormons

VERFAHREN ZUR HERSTELLUNG VON 5-AROYLPYRROL-DERIVATEN UND DEREN VERWENDUNG.

Oily, injectable peptide/aluminium alkanoate compsns - - with prolonged duration of activity

Oily, injectable compsns. of peptides in which (A) the peptide or its salt is adsorbed on an Al salt of a fatty acid, the absorbate being suspended in the oil or (b) the peptide or its salt is suspended in a gel formed from an Al salt of a fatty acid and an oil. The compsns. are for i.m. or s.c. injection or may be given intranasally. They have greatly prolonged duration of activity compared with known compsns. which may be of 7-8 days. Pref. peptide/Al salt ratio is 1:5-1:10. The gels pref. contain 0.5-2% w/v of Al salt in the oil. The pref. Al salt is aluminium stearate and the pref. oil is arachis oil.

Procédé de fabrication d'une préparation corticotropique à action prolongée

Verfahren zur Herstellung von wässrigen Suspensionen von Partikeln eines schwerlöslichen Komplexes mit prolongierter ACTH-Aktivität

Verfahren zur Herstellung protrahiert wirkender ACTH-Präparate

USE FROM PEPTIDEN TO THE PRODUCTION OF RESOLVENTS.

Salts of Peptiden with polyesters with finalconstant Carboxygruppen.

Micro particle for injection and their manufacturing processes.

ЛЕЧЕНИЕ ВИЧ

Предлагаются способы лечения ВИЧ с помощью пептидов проопиомеланокортина (РОМС) и кортикотропинвысвобождающего фактора (CRF) и их продуктов, а также применение таких пептидов для получения лекарственных средств.

ЛЕКАРСТВЕННОЕ СРЕДСТВО

Описан анализ продукта козьей сыворотки, обладающий множеством терапевтических эффектов. Продукт идентифицирован как содержащий пептиды проопиомеланокортин (РОМС) и кортикотропин-релизинг-фактор (CRF), а также продукты разложения указанных пептидов. Заявители описывают способы лечения заболеваний, включая злокачественные новообразования, рассеянный склероз и нервные заболевания, с использованием указанных пептидов и их продуктов, а также лекарственных средств, содержащих указанные пептиды, и способы получения пептидов.

ЛЕЧЕНИЕ НЕВРИТА ЗРИТЕЛЬНОГО НЕРВА

Настоящие изобретение относится к способу лечения больного демиелинизирующим невритом зрительного нерва (ДНЗН), предусматривающему последовательное или одновременное введение стероидного соединения и белка интерферона-бета. Обнаружено, что раннее активное лечение IFN-β полезно при таком режиме лечения, где, например, белок интерферона-бета вводят в совокупной недельной дозе более 12 ММЕ. Способ по изобретению особенно подходит для лечения пациентов на ранних стадиях ДНЗН и оказывает положительное влияние на этих больных. В частности, ДНЗН, при котором проявится положительное влияние лечения по настоящему изобретению, может находиться на субклинической стадии.

СПОСОБ ЛЕЧЕНИЯ ЗАБОЛЕВАНИЯ

Описаны способы лечения заболеваний, включая злокачественные новообразования, рассеянный склероз и нервные заболевания, с использованием пептидов кортикотропин-релизинг-фактора (CRF) и проопиомеланокортина (РОМС) и их продуктов, а также лекарственных средств, содержащих указанные пептиды.

TREATMENT OF NEURITIS OF THE OPTICAL NERVE

MICRO-CAPSULES WITH THE RETARDED LIBERATION, BASED BEYOND THE COPOLYMER OF LACTIDE AND GLYCOLIDE, THAT INCLUDE POLYPEPTIDE AND SUGAR

СПОСОБ ДИАГНОСТИКИ, ПСИХОФИЗИОЛОГИЧЕСКОЙ КОРРЕКЦИИ И ЛЕЧЕНИЯ НЕВРОТИЧЕСКИХ РАССТРОЙСТВ И ПАТОЛОГИЧЕСКИХ ЗАВИСИМОСТЕЙ ОРГАНИЗМА

Изобретение относится к области медицины. Цель - обеспечение достоверности результатов, снижение ошибок при диагностике и эффективной коррекции сложной сочетанной патологии. Способ включает диагностику, по результатам которой определяют объем лечебно-профилактических мероприятий. Диагностику осуществляют с учетом фактора бессознательных установок по тестовым и компьютерным программам. Лечебно-профилактические мероприятия проводят тремя функциональными блоками - фармакологической коррекции, аппаратных методик и психофизиологической коррекции. Фармакологическая коррекция включает комплексный прием препаратов: мебикар (мебикс), гипоксен (олифен), димефосфан, дельторан, семакс 0,1%, винибис. Блок аппаратных методик включает транскраниальную мездиэнцифальную стимуляцию, магнито-, лазерную терапию и цветотерапию. Психофизиологическая коррекция включает создание тест-карты "Линия жизни", выделение причин стрессовых факторов, определение позитивной коммуникации и социально-психологической совместимости ...

СПОСОБ ЛЕЧЕНИЯ ОБОСТРЕНИЙ БРОНХИАЛЬНОЙ АСТМЫ

Способ лечения обострений бронхиальной астмы заключается в ингаляционном применении кортикостероида. Определяют величину пиковой объемной скорости выдоха и при ее значении 80-50 % относительно надлежащих величин назначают индивидуальную оптимальную дозу препарата на протяжении 7-10 дней с последующим снижением дозы до поддерживающей.

ЛЕКАРСТВЕННОЕ СРЕДСТВО

Описан анализ продукта козьей сыворотки, обладающий множеством терапевтических эффектов. Продукт идентифицирован как содержащий пептиды проопиомеланокортин (РОМС) и кортикотропин-релизинг-фактор (CRF) , а также продукты разложения указанных пептидов. Заявители описывают способы лечения заболеваний, включая ревматоидный артрит, неврит зрительного нерва, аутоиммунные заболевания, воспалительные состояния, ожирение и сексуальная дисфункция, с использованием указанных пептидов и их продуктов, а также лекарственных средств, содержащих указанные пептиды.

THE MEDICINE

СПОСОБ ДИАГНОСТИКИ, ПСИХОФИЗИОЛОГИЧЕСКОЙ КОРРЕКЦИИ И ЛЕЧЕНИЯ НЕВРОТИЧЕСКИХ РАССТРОЙСТВ И ПАТОЛОГИЧЕСКИХ ЗАВИСИМОСТЕЙ ОРГАНИЗМА

Способ диагностики, психофизиологической коррекции и лечения невротических расстройств и патологических зависимостей организма, заключающийся в исследованиях организма, основанных на диагностике с выделением групп риска, по полученным результатам которой определяют объем лечебно-профилактических мероприятий, отличающийся тем, что в нем диагностику осуществляют на основе соотношения бессознательных и сознательных установок по тестовым и компьютерным программам, построенным на сочетании психологических и психофизиологических характеристик, при этом обработку тестового материала проводят с определением эмоционального отношения к событиям прошлого и актуальности проблем настоящего, затем выделяют наиболее значимые проблемы личности после чего определяют на достижение каких жизненных целей ориентирован человек, а лечебно-профилактические мероприятия проводят тремя функциональными блоками - блок фармакологической коррекции, блок аппаратных методик и блок психофизиологической коррекции, при этом ...

СПОСІБ ЛІКУВАННЯ ГОСТРОГО ІНФЕКЦІЙНОГО ТОКСИКОЗУ У ДІТЕЙ ГРУДНОГО ВІКУ З ВИКОРИСТАННЯМ ДЕКСАЗОНУ

Спосіб лікування гострого інфекційного токсикозу у дітей грудного віку з використанням дексазону. При цьому на початку розвитку токсикозу призначають одноразове внутрішньовенне введення дексазону в комплексі посиндромної і підтримуючої терапії, що дозволяє зменшити ризик збереження тяжкості стану цих хворих впродовж першого тижня лікування.

Adrenocorticotropic hormone analogs and related methods

ACTH analog compounds of the present invention include compounds comprising an ACTH peptide sequence with one or more structural modifications that can have one or more of the following preferred ACTH analog biological functions: (1) reduction of corticosteroid secretion by adrenal membrane in the presence of the ACTH analog compared to unmodified ACTH, (2) reduction of corticosteroid secretion by adrenal membrane in the presence of endogenous ACTH and (3) increased MC-2R binding affinity with reduced activation of the MC-2R receptor compared to unmodified ACTH binding to the MC-2R melanocortin. The ACTH analog compounds of the present invention are therefore useful for treatment or prevention of diseases and disorders related to ACTH, ACTH receptors or corticosteroid secretion, such as premature labor and Cushing's Disease.

Method of preparation of adrenocorticotrophic hormone

COMPOSITIONS CONTAINING PEPTIDE SALTS FORMS WITH CARBOXY-TERMINATED POLYESTERS AND METHODS FOR THEIR PRODUCTION.

Original process of extraction and purification of a.c.t.h.

Preparations having a protracted acth-effect and method for producing them

PHARMACEUTICAL COMPOSITION CONTAINING CORTICOSTEROID AND OF ASSIMILABLE PHOSPHORUS

USE OF A PEPTIDE AS A THERAPEUTIC AGENT

The present invention is directed to the use of the peptide compound Pyr-Pro-Leu-Pro-Asp-Cys-Cys-Arg-Gln-Lys-Thr-Cys-Ser-Cys-Arg-Leu-Tyr-Glu-Leu-Leu-His-Gly-Ala-Gly- Asn-His-Ala-Ala-Gly-lle-Leu-Thr-Leu-NH2 as a therapeutic agent for the prophylaxis and/or treatment of cancer, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, lung diseases, heart and vascular diseases and metabolic diseases. Moreover the present invention relates to pharmaceutical compositions preferably in form of a lyophilisate or liquide buffer solution or artificial mother milk formulation or mother milk substitute containing the peptide Pyr-Pro-Leu-Pro-Asp-Cys-Cys-Arg-Gln-Lys-Thr-Cys-Ser-Cys-Arg-Leu-Tyr-Glu-Leu-Leu-His-Gly-Ala-Gly-Asn-His-Ala-Ala-Gly-Ile-Leu-Thr-Leu-NH2 optionally together with at least one pharmaceutically acceptable carrier, cryoprotectant, lyoprotectant, excipient and/or diluent.

ACTH FOR TREATMENT OF ACUTE RESPIRATORY DISTRESS SYNDROME

Provided herein are methods of treatment of acute respiratory distress syndrome comprising administration of adrenocorticotropic hormone (ACTH), or fragment, analog, complex or aggregate thereof, or any combination thereof, to an individual in need thereof ...

ADSORPTION COMPLEXES OF PEPTIDES HAVING ADRENOCORTICOTROPIC HORMONE ACTIVITY

An injectable preparation suitable for hormone therapy is provided by a suspension in an aqueous injectable vehicle of an adsorption complex of a salt, hydroxide or oxide of zinc, nickel, cobalt, copper or iron and a peptide having ACTH activity with an amino acid sequence of at least that of the first 19 and not more than that of the first 31 amino acid residues of the ACTH molecule, the amount of metal being between about 1 and 20 mg. per 100 U.S.P. units of peptide.

Methods of treating overproduction of cortisol using ACTH antagonist peptides

The present invention provides methods of treating overproduction of cortisol in a subject by administering to the subject a peptide that antagonizes adrenocorticotropin hormone (ACTH) to block the activation of melanocortin 2 receptors.

Methods and reagents for treating neurodegenerative diseases and motor deficit disorders

The invention relates to a novel method for treating a variety of diseases and disorders, including polyglutamine expansion diseases such as Huntington's disease, neurological degeneration, psychiatric disorders, and protein aggregation disorders and diseases, comprising administering to patients in need thereof a therapeutically effective amount of one or more deacetylase inhibitors. The invention is also directed to a transgenic fly useful as a model of polyglutamine expansion diseases, which may be used to test potential therapeutic agents.

Combination of a MC1R receptor agonist and UVB for the treatment and/or prevention of pigmentation disorders

A system comprising a combination of at least one MCI R receptor agonist and a source of NB-UVB, wherein said system is adapted for simultaneous or sequential use of said MC1R receptor agonist and said NB-UVB in amounts effective for the treatment and/or prevention of dermatological conditions linked to a hypopigmentation.

CRF ANALOGS

Analogs of CRF, which are based upon rCRF, oCRF, sauvagine and alpha-helical CRF, are disclosed that can be administered to achieve a substantial elevation of ACTH, beta-endorphin, beta-lipotropin, other products of the pro-opiomelanocortin gene and corticosterone levels and/or an increase in blood pressure over an extended period of time. One analog which has been found to be particularly potent is: H-D-Pro-Pro-Ile-Ser-Leu-Asp-Leu-Thr-D-Phe-His-Leu-Leu-Arg-Glu-Val-Leu-Glu-Nle-Ala-Arg-Ala-Glu-Gln-Leu-Ala-Gln-Gln-Ala-His-Ser-Asn-Arg-Lys-CML-Nle-Glu-Ile-Ile-NH2. In the analogs of the native 41-residue polypeptides, one or more of the first six N-terminal residues may be deleted and/or the N-terminal alpha-amino group may be acylated by an acylating agent containing up to 7 carbon atoms. A number of other substitutions may also be made throughout the chain. These analogs or pharmaceutically or veterinarily acceptable salts thereof, dispersed in a pharmaceutically or veterinarily acceptable ...

Pulverformulierungen, die Melezitose als Verdünnungsmittel enthalten

Preparations of the adrenocorticotropic hormone having a protracted effect, and method for producing the same

An adrenocorticotropic hormone preparation having a protracted effect contains the reaction product of the hormone and a water-soluble ether of cellulose, suitably one containing a free carboxylic group, e.g. methyl cellulose, sodium carboxymethyl cellulose, hydroxy ethyl cellulose. Ethers of alcohols having in addition to the alcohol group involved in the ether formation an acid group such as glycollic acid, are preferred. The preparation is suitably in the form of an aqueous solution containing 0.5 to 5 per cent of the cellulose ether, suitably in the form of a salt, e.g. the sodium salt, and for instance 20 i.u. of the hormone per mol.

Method for producing preparations with protracted acth-effect and such preparations

Preparations with protracted ACTH effect are produced by combining ACTH or ACTH peptides in an aqueous medium with a high molecular weight organic compound containing acid groups derived from sulphuric, phosphoric or thiophosporic acid. The molecular weight should be at least 2000 but not so high that the compound is insoluble in water or weakly alkaline solutions. The acid groups may be introduced by esterification. Specified naturally occurring materials include heparin (which contains acid sulphuric acid ester groups) and compounds such as agar, carageen, alginic acid, dextran and hyaluronic acid which contain esterifiable carbohydrate or carbohydrate-like residues in the molecule. An exhaustive list of synthetic substances which may be sulphated or phosporylated is given. Specifications 700,761 [Group IV(b)], 753,319 and 757,800 [both in Group IV(a)] are referred to.

Orally administrable hormonal and anti-coagulant medicines comprising chelating agents

Therapeutic compositions for oral administration and comprising a protein hormone, a polypeptide hormone, a steroidal hormone or a synthetic or naturally occurring sulphated polysaccharide whose therapeutic effect depends on its absorption into the bloodstream and which per se is not efficaciously administrable per os, comprise an alkali metal or ammonium salt of an amino acid capable of binding calcium and/or magnesium as an adjuvant. Specified amino acids include ethylene-diamine tetraacetic acid (preferred); o-diamine-cyclo-hexane tetra acetic acid; nitrilo-triacetic acid; alkylene polyamine polyacetic acids of general formula wherein n is a whole number from 2 to 6, m is 0, 1 or 2, D is -CH2.COOH or -CH2.CH2 COOH and A is the same as D or is a lower (C1-6) alkyl or hydroxy lower alkyl group (specific examples being given). Further suitable amino acids are di-(2-aminoethyl)-ether-N,N,N1,N1-tetraacetic acid; di-(2-aminoethyl)ethylene - glycol - N,N,N1,N1 - tetraacetic ...

OVULATIONSHEMMENDES MEANS TO HORMONALEN KONTRAZEPTION

IN THE LARGE INTESTINE DISINTEGRATING, POLYPEPTIDE ABSTENTION ORAL FORMULATIONS.

ACTH CONTAINING MICROSPHERES WITH STEERED DELIVERY

SALZE VON PEPTIDEN MIT CARBOXY-TERMINIERTEN POLYESTERN

PREPARATION FOR PREVENTING OR FIGHT AGAINST COMPLICATIONS WITH DIABETES.

PROCEDURES FOR THE PRODUCTION OF INJECT-CASH OLIGEN PEPTIDPRAPARATEN

Frequency assisted transdermal agent delivery method and system

Physiologically active polypeptide-containing pharmaceutical composition

Modulated release from biocompatible polymers

Ovulation-inhibiting means for hormonal contraception

Adrenocorticotropic hormone analogs and related methods

ACTH analog compounds of the present invention include compounds comprising an ACTH peptide sequence with one or more structural modifications that can have one or more of the following preferred ACTH analog biological functions: (1) reduction of corticosteroid secretion by adrenal membrane in the presence of the ACTH analog compared to unmodified ACTH, (2) reduction of corticosteroid secretion by adrenal membrane in the presence of endogenous ACTH and (3) increased MC-2R binding affinity with reduced activation of the MC-2R receptor compared to unmodified ACTH binding to the MC-2R melanocortin. The ACTH analog compounds of the present invention are therefore useful for treatment or prevention of diseases and disorders related to ACTH, ACTH receptors or corticosteroid secretion, such as premature labor and Cushing's Disease.

ADRENOCORTICOTROPIC HORMONE ANALOGS AND RELATED METHODS

SMALL PEPTIDES AND METHODS FOR TREATMENT OF ASTHMA AND INFLAMMATION

... ▓▓▓Methods for treating allergies, cutaneous inflammation, arthritis, chronic ▓obstruction pulmonary disease and treating chronic inflammatory bowel disease ▓are described. Also described is a method for inhibiting the infiltration of ▓eosinophils into airways of a patient, a method for inhibiting the mucous ▓release into airways of a patient, a method for blocking IgE activation of a ▓lymphocyte, a method for stabilizing the cell membrane of a lymphocyte, ▓thereby preventing their further involvement in the increased inflammatory ▓response to an IgE antigen challenge, and a method for inhibiting the ▓migration of T-cells. Such methods involve administering to said patient a ▓therapeutically effective amount of a peptide having the formula f-Met-Leu-X, ▓wherein X is selected from the group consisting of Tyr, Tyr-Phe, Phe-Phe and ▓Phe-Tyr.▓ ...

POLY (LACTIDE-CO-GLYCOLIDE)-BASED SUSTAINED RELEASE MICROCAPSULES COMPRISING A POLYPEPTIDE AND A SUGAR

This invention relates to compositions for the sustained release of biologically active polypeptides, and methods of forming and using said compositions, for the sustained release of biologically active polypeptides. The sustained release compositions of this invention comprise a biocompatible polymer having dispersed therein, a biologically active polypeptide and a sugar.

ADRENOCORTICOTROPIC HORMONE RECEPTOR AND USES

The present invention relates to a mammalian adrenocorticotropic hormone receptor. The invention is directed toward the isolation, characterization and phar- macological use of mammalian adrenocorticotropic hor- mone receptor, the gene corresponding to this receptor, a recombinant eukaryotic expression construct capable of expressing a mammalian-adrenocorticotropic hormone receptor in cultures of transformed eukaryotic cells and such cultures of transformed eukaryotic cells that syn- thesize mammalian adrenocorticotropic hormone recep- tor. The invention also provides methods for screening ACTH R agonists and antagonists in vitro using prepar- ations of receptor from-such cultures of eukaryotic cells transformed with a recombinant eukaryotic expression construct comprising the ACTH R receptor gene. The in- vention specifically provides human and bovine ACTH R genes.

5USE OF A PEPTIDE AS A THERAPEUTIC AGENT

The present invention is directed to the use of the peptide compound Pyr-Gln-Asp-Tyr(SO3H)-Thr-Gly-Trp-Met-Asp-Phe-NH2 as a therapeutic agent for the prophylaxis and/or treatment of cancer, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, lung diseases, heart and vascular diseases and metabolic diseases. Moreover the present invention relates to pharmaceutical compositions preferably in form of a lyophilisate or liquide buffer solution or artificial mother milk formulation or mother milk substitute containing the peptide Pyr-Gln-Asp-Tyr(SO3H)-Thr-Gly-Trp-Met-Asp-Phe-NH2 optionally together with at least one pharmaceutically acceptable carrier, cryoprotectant, lyoprotectant, excipient and/or diluent.

ANTI-HEMORRHAGE MEDICATION PACK

An anti-hemorrhage medication pack for administering an anti-hemorrhage drug for the treatment of a hemorrhage caused by trauma comprising: a drug with an active ingredient selected from the group consisting of a 1-24 amino acid sequence of adrenocorticotropic hormone (ACTH 1-24) and all its fragments and analogues, and analogues of fragments, with agonist activity on MC4 melanocortin receptors, and synthetic agonists of the MC4 melanocortin receptors; and an auto-injector including the drug for automatically injecting said drug into a patient, said auto-injector including a first container suitable for containing a lyophilized pharmacological part of the anti-hemorrhage drug and a second container for containing a liquid part of the anti-hemorrhage drug; actuating means configured for connecting the first and second containers by interrupting a dividing wall, thereby mixing the lyophilized pharmacological part with the liquid part of the anti-hemorrhage drug only at the moment of administering ...

A SUSTAINED-RELEASE COMPOSITION CONTAINING PEPTIDES AS ACTIVE INGREDIENT

The present invention relates to a sustained-release drug composition consisting essentially of microparticies of a peptide as the active substance and a biocompatible water-soluble polymer, in particular peptide as meianocortin receptor ligand. The present invention relates also to an injection formulation comprising the sustained-release drug composition suspended in an injection medium.

Immunoglobulin Formulation and Method of Preparation Thereof

A stable aqueous pharmaceutical formulation comprising a therapeutically effective amount of an antibody, polysorbate 80, a buffer which inhibits polysorbate oxidation is described along with methods of making the preparation. Also described are formulations with high antibody concentrations which maintain fixed volumes and which may be used on patients of variable weight. 1. A stable , aqueous pharmaceutical formulation comprising an immunoglobulin , a phosphate buffer , a polysorbate , and sodium chloride.2. The formulation of claim 1 , wherein the polysorbate is polysorbate 80.3. The formulation of claim 2 , wherein the polysorbate 80 is present in an amount of about 0.001% to about 2.0% (w/v).4. The formulation of claim 3 , wherein the polysorbate 80 is present in the amount of about 0.02% (w/v).5. The formulation of claim 1 , wherein the immunoglobulin is present in the amount of about 0.1 mg/mL to about 200 mg/mL.6. The formulation of claim 5 , wherein the immunoglobulin is present in the amount of about 1.7 mg/mL.7. The formulation of claim 5 , wherein the immunoglobulin is present in the amount of about 5 mg/mL.8. The formulation of claim 5 , wherein the immunoglobulin is present in the amount of about 20 mg/mL.9. The formulation of claims 1 , wherein the formulation has a pH of about 3.0 to about 7.0.10. The formulation of claim 9 , wherein the pH is about 5.5 to about 6.5.11. The formulation of claim 10 , wherein the pH is about 6.0∀0.5.12. The formulation of claim 1 , wherein the formulation is in a fixed volume and the immunoglobulin is present in the amount of about 50 mg/mL.13. The formulation of claim 12 , wherein the immunoglobulin binds alpha-4 integrin.14. The formulation of claim 13 , wherein the immunoglobulin is natalizumab.15. The formulation of claim 1 , wherein the phosphate buffer is at pH 6.0∀0.5 claim 1 , the polysorbate is polysorbate 80 and is present in an amount of about 0.02% (w/v) claim 1 , the immunoglobulin is natalizumab claim 1 , ...

ORODISPERSIBLE TABLETS OF ERYTHRITOL AND ISOMALT

Erythritol is granulated together with at least 10% w/w isomalt. Prior and/or after granulation a disintegrant is added and orodispersible tablets are prepared. The tablet has a disintegration time of less than 100 seconds, less than 90 seconds, preferably less than 80 seconds, more preferably less than 60 seconds and said disintegration time was determined according to the European Pharmacopoeia VI, Test method 2.9.1 by using a pharmaceutical disintegration tester model ZT 73 whereby 6 tablets having a surface of 1 square centimeter and a weight of 350 mg, at a compression force of 20 kN, were analyzed and mean values were calculated. The process for preparing the orodispersible tablet, its use, and the intermediate granulate are described as well. 111.-. (canceled)12. An orodispersible tablet comprising:a disintegrant;erythritol; andat least 10% w/w isomalt,wherein the orodispersible tablet, when prepared with a compression force of 20 kN and having a surface of one square centimeter and a weight of 350 mg, has a disintegration time of less than 100 seconds, the disintegration time determined according to the European Pharmacopoeia VI, Test method 2.9.1 using a pharmaceutical disintegration tester model ZT 73.13. The tablet of claim 12 , wherein isomalt is present in an amount of less than 50% w/w.14. The tablet of claim 12 , wherein the disintegrant is present in an amount of 0.5 to 20% w/w.16. A method for preparing the orodispersible tablet of claim 12 , the method comprising:granulating erythritol, isomalt, and optionally the disintegrant to prepare a granulate;optionally adding disintegrant to the granulate; andtabletting the granulate.17. The method of claim 16 , wherein an active ingredient is added prior to and/or after the granulating.18. A granulate comprising:disintegrant;erythritol; andfrom 10% w/w to 50% w/w isomalt.19. The granulate of claim 18 , wherein the disintegrant is present in an amount of 0.5 to 5% w/w.20. The granulate of claim 18 , wherein ...

LIPASE INHIBITING COMPOSITION

Pharmaceutical compositions that contain a lipase inhibitor having a melting point ≧37° C., a sucrose fatty acid ester wherein the sucrose fatty acid ester is a mono-, di-, tri- or tetra-ester, and optionally one or more pharmaceutically acceptable excipients, are useful for treatment of obesity. 1. A pharmaceutical composition comprising(i) orlistat;(ii) a sucrose fatty acid ester or a mixture of sucrose fatty acid esters, wherein the sucrose fatty acid ester comprises a sucrose moiety and at least one to four fatty acid moieties, and wherein the fatty acid moiety in the sucrose fatty acid ester or mixture of sucrose fatty acid esters is selected from the group consisting of a C12-C18 saturated fatty acid; andwherein the sucrose fatty acid ester or a mixture of sucrose fatty acid esters have an HLB value of about 16;(iii) one or more pharmaceutically acceptable excipients.2. The composition according to claim 1 , wherein the composition comprises 20 to 60 mg orlistat.3. The composition according to claim 1 , wherein the sucrose fatty acid ester or mixture of sucrose fatty acid esters is selected from sucrose palmitate claim 1 , sucrose stearate claim 1 , sucrose myristate or sucrose laurate.4. The composition according to claim 1 , wherein 0.05 mg to 20 mg sucrose fatty acid ester or mixture of sucrose fatty acid esters is used per 1 mg orlistat.5. The composition according to claim 1 , wherein the sucrose fatty acid ester contains at least two fatty acid moieties.6. The composition according to wherein the two fatty acid moieties are the same or different.7. The composition according to wherein the two fatty acid moieties are the same.8. The composition according to claim 1 , wherein the sucrose moiety in the sucrose fatty acid ester or mixture of sucrose fatty acid esters is about 80% mono esterified.9. The composition according to wherein in the mixture of sucrose fatty acid esters the most prevalent sucrose fatty acid ester in said mixture is a mono ester.10. ...

VISCOUS BUDESONIDE FOR THE TREATMENT OF INFLAMMATORY DISEASES OF THE GASTROINTESTINAL TRACT

Provided herein are methods for preventing or alleviating the symptoms of and inflammation associated with inflammatory diseases and conditions of the gastrointestinal tract, for example, those involving the esophagus. Also provided herein are pharmaceutical compositions useful for the methods of the present invention. 1. A method of preventing or alleviating esophageal inflammation in an individual comprising orally administering to said individual a corticosteroid in association with at least one excipient to increase the viscosity of the composition.2. The method of claim 1 , wherein the viscosity of the composition is about that of a suspension prepared by adding about 5 to about 15 grams of sucralose to 4 ml of water claim 1 , wherein the viscosity is measured at 25 degrees Celsius.3. The method of claim 1 , wherein the viscosity of the composition is about that of a suspension prepared by adding about 10 to about 12 grams of sucralose to 4 ml of water claim 1 , wherein the viscosity is measured at 25 degrees Celsius.4. The method of claim 1 , wherein said corticosteroid is topical.5. The method of claim 1 , wherein said corticosteroid is Budesonide.6. The method of claim 1 , wherein said individual has eosinophilic esophagitis.7. The method of claim 1 , wherein said individual has been diagnosed with a disease or condition selected from the group consisting of eosinophilic esophagitis claim 1 , inflammatory bowel diseases involving the esophagus claim 1 , Crohn's disease claim 1 , esophageal inflammation secondary to caustic/irritant ingestion claim 1 , persistent/recurrent esophageal strictures of any cause and including caustic/irritant ingestion claim 1 , pill-induced esophagitis claim 1 , systemic diseases claim 1 , congenital diseases claim 1 , and post-surgery inflammation.8. The method of claim 1 , wherein said individual is a child.9. The method of claim 1 , wherein said individual is a child less than 16 years old.10. The method of claim 1 , wherein ...

Method for Bowel Preparation

The present invention provides methods for facilitating cleansing of the gastrointestinal tract of a patient prior to a diagnostic, surgical or therapeutic procedure. The methods can improve patient compliance, and thus, efficacy of the preparation. Specifically, the present methods make the gastrointestinal tract preparation composition palatable for the patient to consume. For example, for a patient preparing to undergo colonoscopy, the present methods make the bowel preparation solution taste significantly less salty. 1. A method for cleansing the gastrointestinal tract of a patient comprising the steps of:determining the pH of a gastrointestinal tract preparation composition which has a salty taste, and adjusting the pH to range from about 3 to about 6.4 if necessary;providing a taste-modifying substance to the patient; andadministering orally the gastrointestinal tract preparation composition to the patient, wherein the salty taste of the gastrointestinal tract preparation composition is reduced by at least about 20% compared to the salty taste of the gastrointestinal tract preparation composition had the taste-modifying substance not been provided.2. The method of claim 1 , wherein the gastrointestinal tract is the intestine and the gastrointestinal tract preparation composition is a bowel preparation solution.3. The method of claim 2 , wherein the intestine is the colon.4. The method of claim 1 , wherein the gastrointestinal tract is cleansed prior to carrying out a diagnostic claim 1 , therapeutic and/or surgical procedure on the patient.5. The method of claim 1 , wherein the gastrointestinal tract is cleansed prior to an endoscopy.6. The method of claim 5 , wherein the endoscopy is a colonoscopy or sigmoidoscopy.7. The method of claim 1 , wherein the gastrointestinal tract is cleansed prior to a barium enema examination claim 1 , capsule endoscopy claim 1 , colon surgery or gastrointestinal tract surgery.8. The method of claim 1 , wherein the taste- ...

CROSSLINKED POLYSACCHARIDE BEADS AND THEIR BIOMEDICAL USES

The present inventions relates to beads as biocompatible material adapted for use within the human or animal body. Said beads are highly useful for tissue engineering, in situ tissue regeneration, as well as for drug and/or cells delivery. In addition, said beads may support biotechnological applications such as cell carriers. 2. The method according to claim 1 , wherein said method further comprises the following steps:d) submerging said beads into an aqueous solution; ande) washing said beads.3. The method of claim 1 , wherein said polysaccharide is a mixture of pullulan/dextran in a ratio of 75:25 w/w.4. The method according to claim 1 , wherein said cross-linking agent is selected from the group consisting of trisodium trimetaphosphate (STMP) claim 1 , phosphorus oxychloride (POCl) claim 1 , epichlorohydrin claim 1 , formaldehydes claim 1 , carbodiimides claim 1 , and glutaraldehydes.5. The method according to claim 1 , wherein said hydrophobic phase is a vegetal oil.6. The method according claim 1 , wherein the alkaline aqueous solution further comprises a porogen agent.7. The method according to claim 6 , wherein the porogen agent is selected from the group consisting of sodium chloride claim 6 , calcium chloride claim 6 , ammonium carbonate claim 6 , ammonium bicarbonate claim 6 , calcium carbonate claim 6 , sodium carbonate claim 6 , sodium bicarbonate and mixtures thereof.8. The method according to claim 1 , wherein the alkaline aqueous solution further comprises hydroxyapatite.9. The method according to claim 1 , wherein the alkaline aqueous solution further comprises a drug.11. The bead according to claim 10 , wherein said bead has a size of from 5 nm to 5 mm.1217-. (canceled)18. The method of claim 1 , wherein step b) is performed in the absence of a surfactant.19. The method of claim 5 , wherein said vegetal oil is selected from the group consisting of canola oil claim 5 , corn oil claim 5 , cottonseed oil claim 5 , safflower oil claim 5 , soybean oil ...

Stabilized Formulations Containing Anti-PCSK9 Antibodies

The present invention provides pharmaceutical formulations comprising a human antibody that specifically binds to human proprotein convertase subtilisin/kexin type 9 (PCSK9). The formulations may contain, in addition to an anti-PCSK9 antibody, at least one amino acid, at least one sugar, or at least one non-ionic surfactant. The pharmaceutical formulations of the present invention exhibit a substantial degree of antibody stability after storage for several months. 1. A liquid pharmaceutical formulation comprising:(a) an antibody, which comprises a heavy chain complementarity determining region (HCDR) 1 of SEQ ID NO:2, an HCDR2 of SEQ ID NO:3, an HCDR3 of SEQ ID NO:4, a light chain complementarity determining region (LCDR) 1 of SEQ ID NO: 6, an LCDR2 of SEQ ID NO:7, and an LCDR3 of SEQ ID NO:8, and which binds specifically to human proprotein convertase subtilisin/kexin type 9 (human PCSK9);(b) histidine;(c) polysorbate 20; and(d) sucrose, at pH of 6.0±0.32. The pharmaceutical formulation of claim 1 , wherein the antibody comprises a heavy chain variable domain (HCVD) of SEQ ID NO:1 and a light chain variable domain (LCVD) of SEQ ID NO:5.3. The pharmaceutical formulation of claim 1 , wherein(a) over 90% of the antibodies have a molecular weight of 155 kDa±1 kDa;(b) over 50% of the antibodies have an isoelectric point of about 8.5; and(c) from 75% to 90% of the antibodies are fucosylated.4. The pharmaceutical formulation of claim 1 , wherein the antibody concentration is from 50 mg/mL±7.5 mg/mL to 175 mg/mL±26.25 mg/mL.5. The pharmaceutical formulation of claim 1 , wherein the histidine concentration is 10 mM±1.5 mM.6. The pharmaceutical formulation of claim 1 , wherein the polysorbate 20 concentration is from 0.01% w/v±0.0015% to 0.2% w/v±0.03%.7. The pharmaceutical formulation of claim 1 , wherein the sucrose concentration is from 5%±0.75% to 12%±1.8%.8. The pharmaceutical formulation of claim 2 , wherein the antibody concentration is 175 mg/mL±26.25 mg/mL claim 2 , ...

WATER-SOLUBLE PHARMACEUTICAL COMPOSITION COMPRISING AT LEAST ONE THERAPEUTICALLY ACTIVE SUBSTANCE HAVING HYDROPHOBIC PROPERTIES AND AT LEAST ONE COMPOUND SELECTED FROM AMONG SIALOGLYCOSPHINGOLIPIDS, GLYCOSPHINGOLIPIDS OR A MIXTURE OF SIALOGLYCOSPHINGOLIPIDS AND GLYCOSPHINGOLIPIDS

This invention discloses water soluble pharmaceutical compositions including at least one therapeutically active substance and at least one compound selected from the sialoglycosphingolipids, the glycosphingolipids or a mixture of sialoglicosphingolipids and glycosphingolipids, in which at least one of the therapeutically active substances is a drug with hydrophobic characteristics. In particular, sterile compositions for i.v. administration, composed of nano-glycosphingolipids micelles or modified glycosphingolipids, which can be coated with albumin in a noncovalent form and which allow transport and controlled release of highly hydrophobic molecules are disclosed. 149-. (canceled)50. A water soluble pharmaceutical composition , comprising at least one therapeutically active hydrophobic substance and at least one compound selected from sialoglycosphingolipids and a mixture of sialoglycosphingolipids and glycosphingolipids , wherein at least one of said therapeutically active substances is a drug with hydrophobic characteristics , and said compound which is at least one in number is presented in the form of micelles , wherein said micelles form a complex with a plasma protein.51. The water soluble pharmaceutical composition according to claim 50 , wherein said compound which is at least one in number is selected from sialoglycosphingolipids.52. The water soluble pharmaceutical composition according to claim 50 , wherein said plasma protein is albumin.53. The water soluble pharmaceutical composition according to claim 50 , wherein said drug with hydrophobic characteristics is a drug selected from antitumor drugs and antimycotic drugs.54. The water soluble pharmaceutical composition according to claim 53 , wherein the glycosphingolipid(s) is/are selected from gangliosides.55. The water soluble pharmaceutical composition according to claim 54 , wherein the gangliosides are selected from monosialogangliosides claim 54 , disialogangliosides claim 54 , ...

POLYSACCHARIDE GEL FORMULATION HAVING INCREASED LONGEVITY

Described herein are polysaccharide gel formulations including at least one inhibitor of polysaccharide degradation and methods of making the same. The methods described herein involve the steps of providing at least one polysaccharide and incorporating at least one inhibitor of degradation into the polysaccharide. In some embodiments, the incorporating step comprises 1) mixing the at least one inhibitor with the at least one polysaccharide at a highly hydrated state thereby encapsulating the at least one inhibitor in a polysaccharide network, and 2) dehydrating the polysaccharide network thereby controlling release kinetics or final swell ratio. In another embodiment, the incorporating step comprises 1) encapsulating at least one inhibitor into a biocompatible or biodegradable vessel and 2) combining the polysaccharide and the vessel into a gel formulation. The polysaccharide gel formulations described herein can be used for a variety of cosmetic applications. 1. A polysaccharide gel formulation with an increased degradation time comprising cross-linked hyaluronic acid and tannic acid , wherein the formulation is made by a process including the step of encapsulating tannic acid in a polysaccharide network.2. The formulation of wherein the step of encapsulating tannic acid in a polysaccharide network comprises mixing the tannic acid with the polysaccharide at a highly hydrated state.3. The formulation of wherein the process further comprises the step of dehydrating the polysaccharide network.4. The formulation of wherein the tannic acid is present at a concentration of about 0.0001% to about 1%. This application is a continuation of U.S. patent application Ser. No. 12/558,270, filed Sep. 11, 2009, which is a continuation of U.S. patent application Ser. No. 12/276,167, filed Nov. 21, 2008, now U.S. Pat. No. 8,394,782, which claims the benefit of U.S. Provisional Patent Application No. 60/991,473, filed Nov. 30, 2007, the entire disclosures of which applications are ...

TREATMENT OF HIV

We describe methods of treatment of HIV using proopiomelanocortin (POMC) and corticotropin releasing factor (CRF) peptides and their products, as well as uses of such peptides in the preparation of medicaments. 113-. (canceled)14. A method of treatment of HIV comprising administering a corticotropin releasing factor (CRF) peptide to a patient.15. The method of claim 14 , wherein one or more of the following effects is achieved: a reduction in viral load; an increase in CD4 cells; or an increase in CD8 cells.16. The method of wherein the CRF is non-human CRF.17. The method of wherein the CRF is goat CRF.18. The method of claim 14 , and further comprising administering a POMC peptide or a POMC product.19. The method of claim 18 , and further comprising administering two or more of alpha claim 18 , beta claim 18 , and gamma melanocyte stimulating hormone (MSH); adrenocorticotrophin (ACTH); beta and gamma lipotropin (LPH); and beta endorphin. The present invention relates to methods of treatment of HIV, and to use of POMC and/or CRF peptides in the preparation of medicaments for the treatment of HIV.The human immunodeficiency virus/acquired immunodeficiency syndrome (HIV/AIDS) epidemic has caused over 20 million deaths worldwide and currently affects about 40 million people. This has a serious socio-economic impact particularly on developing countries. To date, the only effective weapon against HIV and AIDS is therapy, notably highly active anti-retroviral therapy (HAART). However, this is not available worldwide, can have toxic side effects and often those most in need are deprived of treatment. Therefore the requirement for an effective therapeutic HIV vaccine or prophylactic treatment has become increasingly extremely urgent.International Patent Application PCT/GB2005/050108 describes the use of corticotropin releasing factor (CRF) and/or proopiomelanocortin (POMC) peptides in the treatment of a range of disorders in patients. The reader is referred to PCT/GB2005/ ...

STABILIZED HUMAN IMMUNOGLOBULIN COMPOSITION

The invention relates to a liquid pharmaceutical composition comprising human immunoglobulins G (IgGs), comprising at least 200 mM, preferably 250 mM±50 mM, of glycine and between 20 and 100 mg/l of a non-ionic detergent, and having a pH of less than or equal to 4.8. 1. Liquid pharmaceutical composition comprising human immunoglobulins G (IgGs) , comprising at least 200 mM of glycine , and between 20 and 100 mg/l of a non-ionic detergent , wherein the said composition has a pH of less than or equal to 4.8.2. The composition according to claim 1 , said composition having a pH of between 4.4 and 4.8 claim 1 , preferably 4.6.3. The composition according to claim 1 , which composition containing no mannitol.4. The composition according to claim 1 , wherein concentration of immunoglobulins G is 100 g/l±20 g/l.5. The composition according to claim 1 , comprising 35 mg/l±15 mg/l claim 1 , of non-ionic detergent.6. The composition according to claim 1 , wherein the only excipients are glycine and the non-ionic detergent.7. The composition according to claim 1 , wherein the non-ionic detergent is chosen from polysorbate 20 claim 1 , polysorbate 80 and/or polyethylene-polypropylene glycol such as Pluronic® F68.8. The composition according to claim 7 , comprising:100 g/l of IgG250 mM of glycine50 mg/l of polysorbate 80.9. The composition according to claim 7 , comprising:100 g/l of IgG250 mM of glycine20 mg/l of polysorbate 20.10. The composition according to claim 1 , wherein the immunoglobulins G are obtained by fractionation of human blood plasma.11. The composition according to claim 1 , which is obtained by reconstitution with water claim 1 , from a freeze-dried product.12. A solid composition obtained by desiccation claim 1 , of a liquid composition according to .13. A solid composition according to claim 12 , wherein dessication is freeze-drying.14. The composition of claim 1 , comprising at least 250 mM ±50 mM of glycine.15. The composition according to claim 2 , which ...

STABLE PHARMACEUTICAL COMPOSITIONS OF FESOTERODINE

The present invention relates to stable pharmaceutical compositions comprising fesoterodine or a pharmaceutically acceptable salt thereof. In particular, the invention relates to pharmaceutical compositions of fesoterodine or a pharmaceutically acceptable salt thereof and a stabilizer. The invention also relates to processes for making such compositions and the methods of using such compositions. 1. A pharmaceutical composition comprising fesoterodine or a pharmaceutically acceptable salt thereof , a stabilizer and one or more pharmaceutically acceptable excipients.2. The pharmaceutical composition according to claim 1 , wherein said stabilizer is sugar or its derivative.3. The pharmaceutical composition according to claim 2 , wherein said stabilizer is selected one or more from mannitol claim 2 , maltitol claim 2 , sucrose claim 2 , fructose claim 2 , galactose claim 2 , lactitol claim 2 , inositol claim 2 , and erythritol.4. The pharmaceutical composition according to claim 1 , wherein the stabilizer is sugar.5. The pharmaceutical composition according to claim 4 , wherein the sugar is selected one or more form glucose claim 4 , mannose claim 4 , galactose claim 4 , fructose claim 4 , lactose claim 4 , sucrose and maltose.6. The pharmaceutical composition according to claim 1 , wherein the amount of stabilizer is about 1% w/w to about 50% w/w of the composition.7. The pharmaceutical composition according to claim 1 , wherein fesoterodine or a pharmaceutically acceptable salt thereof is fesoterodine hydrogen fumarate.8. The pharmaceutical composition according to claim 1 , wherein fesoterodine or a pharmaceutically acceptable salt thereof is present in amount of about 1 mg to about 50 mg.9. The pharmaceutical composition according to claim 1 , wherein one or more pharmaceutically acceptable excipients selected from diluents claim 1 , binders claim 1 , rate controlling polymers claim 1 , lubricants claim 1 , disintegranting agents claim 1 , glidants claim 1 , film ...

METHOD FOR IN VIVO TARGETING OF NANOPARTICLES VIA BIOORTHOGONAL COPPER-FREE CLICK CHEMISTRY

The present disclosure relates to a method for in vivo targeting of a nanoparticle via bioorthogonal copper-free click chemistry, more particularly to a method for in vivo targeting of a nanoparticle, including: injecting a precursor capable of being metabolically engineered in vivo when injected into a living system and having a first bioorthogonal functional group into the living system; and injecting a nanoparticle having a second bioorthogonal functional group which can perform a bioorthogonal copper-free click reaction with the first bioorthogonal functional group attached thereto into the living system. 1. A method for in vivo targeting of a nanoparticle , comprising:injecting a precursor capable of being metabolically engineered in vivo when injected into a living system and having a first bioorthogonal functional group into the living system; andinjecting a nanoparticle having a second bioorthogonal functional group which can perform a bioorthogonal copper-free click reaction with the first bioorthogonal functional group attached thereto into the living system.2. The method for in vivo targeting of a nanoparticle according to claim 1 , wherein the metabolic engineering is metabolic glycoengineering.4. The method for in vivo targeting of a nanoparticle according to claim 1 , wherein the first bioorthogonal functional group is an azide group.5. The method for in vivo targeting of a nanoparticle according to claim 1 , wherein the second bioorthogonal functional group is a functional group capable of reacting with the first bioorthogonal functional group in vivo in the absence of a catalyst.7. The method for in vivo targeting of a nanoparticle according to claim 1 , wherein the nanoparticle has a surface to which the second bioorthogonal functional group can be attached and has a size of 10-1000 nm such that in vivo circulation is possible.8. The method for in vivo targeting of a nanoparticle according to claim 1 , wherein the nanoparticle is an organic ...

Compositions for Drug Administration

The present invention provides compositions and methods and for increasing the bioavailability of therapeutic agents in a subject, as well as compositions and methods for providing migraine pain relief. The compositions include at least one alkyl glycoside and at least one therapeutic agent, such as a 5-HT receptor agonist, wherein the alkylglycoside has an alkyl chain length from about 10 to about 16 carbon atoms. 1. A composition comprising:a) a therapeutically effective amount of a 5-HT receptor agonist; andb) an alkylsaccharide.2. The composition of claim 1 , wherein the 5-HT agonist is sumatriptan claim 1 , naratriptan claim 1 , rizatriptan claim 1 , eletriptan claim 1 , frovatriptan claim 1 , almotriptan claim 1 , zolmitriptan claim 1 , salt thereof claim 1 , or combination thereof.3. The composition of claim 1 , wherein the alkylsaccharide concentration is about 0.05% to 2%.4. The composition of claim 1 , wherein the alkylsaccharide has an alkyl chain including between 10 to 16 carbons.5. The composition of claim 4 , wherein the alkylsaccharide is undecyl-beta-D-maltoside claim 4 , dodecyl-beta-D-maltoside claim 4 , tridecyl-beta-D-maltoside claim 4 , tetradecyl-beta-D-maltoside claim 4 , sucrose mono-dodecanoate claim 4 , or combination thereof.6. The composition of claim 1 , wherein the composition is formulated for administration into the circulatory system of a subject via the oral claim 1 , ocular claim 1 , intranasal claim 1 , nasolacrimal claim 1 , inhalation claim 1 , pulmonary claim 1 , sublingual claim 1 , buccal claim 1 , or CSF delivery route.7. The composition of claim 1 , wherein the composition provides a Tmax for the 5-HT agonist of about 30 minutes or less in a human.8. The composition of claim 1 , wherein the composition provides an AUC 0-1 hr for the 5-HT agonist of about 1.3 fold claim 1 , 1.5 fold claim 1 , or greater as compared to a corresponding AUC 0-1 hr provided in the absence of the alkylsaccharide.9. The composition of claim 1 , ...

Controlled Release Formulations

The present invention provides stable, self-assembling, biocompatible and biodegradable hydrogel formulations, into which one or more compounds may be incorporated allowing for delayed release or controlled release of the incorporated compounds as the hydrogel is degraded in the body. 1. A controlled release formulation comprising a therapeutic agent entrapped in an alkyglycoside biodegradable hydrogel.2. The controlled release formulation of claim 1 , wherein the therapeutic agent is methotrexate.3. The controlled release formulation of claim 1 , wherein the therapeutic agent is folic acid.4. The controlled release formulation of claim 1 , wherein the therapeutic agent is curcumin.5. The controlled release formulation of claim 4 , further comprising sodium bicarbonate.6. The controlled release formulation of claim 1 , wherein alkylglycoside is tetradecylmaltoside.7. A controlled release formulation comprising a therapeutic agent entrapped in a sucrose ester biodegradable hydrogel.8. The controlled release formulation of claim 7 , wherein the therapeutic agent is methotrexate.9. The controlled release formulation of claim 7 , wherein the therapeutic agent is folic acid.10. The controlled release formulation of claim 9 , further comprising sodium bicarbonate.11. The controlled release formulation of claim 7 , wherein the therapeutic agent is curcumin.12. The controlled release formulation of claim 7 , wherein the sucrose stearate is a sucrose stearate.13. A controlled release bilayer formulation comprising a first layer and a second layer claim 7 , wherein the first layer comprises a first therapeutic agent entrapped in a alkylglycoside biodegradable hydrogel claim 7 , and the second layer comprises a second therapeutic agent entrapped in a sucrose ester biodegradable hydrogel.14. The controlled release bilayer formulation of claim 13 , wherein the first layer comprises a first therapeutic agent entrapped in a tetradecylmaltoside biodegradable hydrogel claim 13 , and ...

SUSTAINED RELEASE PHARMACEUTICAL COMPOSITIONS COMPRISING PREGABALIN

The present invention relates to stable once daily sustained release pharmaceutical compositions comprising pregabalin or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable excipient wherein pharmaceutical composition is bioequivalent to conventional immediate release formulation of pregabalin administered twice daily. The present invention further relates to a composition comprising pregabalin and sugar esters as release retarding agent for maintaining uniform release rate of the drug and process for the preparation of such oral sustained release formulations. 1. A sustained release pharmaceutical composition adapted for once daily dosing , comprising pregabalin or a pharmaceutically acceptable salt , complex , solvate or hydrate thereof , release retarding agent(s) and optionally other pharmaceutically acceptable excipients thereof , wherein said pharmaceutical composition is bioequivalent to immediate release formulations of pregabalin administered twice daily.2. A sustained release pharmaceutical composition according to claim 1 , wherein the release retarding agent is selected from the group consisting of cellulose ethers claim 1 , cellulose esters claim 1 , acrylic acid copolymers claim 1 , waxes claim 1 , gums claim 1 , glyceryl fatty acid esters and sucrose fatty acid esters.3. A sustained release pharmaceutical composition according to claim 2 , wherein the sucrose fatty acid ester is selected from the group comprising claim 2 , sucrose stearate claim 2 , sucrose distearate claim 2 , sucrose palmitate claim 2 , sucrose oleate claim 2 , sucrose laurate claim 2 , sucrose behenate claim 2 , sucrose erucate and combinations thereof.4. A sustained release pharmaceutical composition according to claim 1 , wherein the composition comprises pregabalin in an amount from about 25% to about 75% by weight of the dosage form and release retarding agent in an amount from about 20% to about 80% by weight of the dosage form.5. A sustained release ...

Oral Drug Delivery System

Dosage forms and drug delivery devices suitable for administration of pharmaceutical compounds and compositions, including the oral drug administration of compounds. 179.-. (canceled)80. A composition comprising:a drug;sucrose acetate isobutyrate (SAIB);a cellulose acetate butyrate (CAB) having a number average molecular weight ranging from 66,000 Daltons to 83,000 Daltons; anda solvent.81. The composition of claim 80 , wherein the drug is present in an amount ranging from about 2 mg to about 250 mg.82. The composition of claim 80 , wherein the drug comprises an opioid claim 80 , a central nervous system (CNS) depressant claim 80 , or a stimulant.83. The composition of claim 80 , wherein the drug comprises hydrocodone claim 80 , hydromorphone claim 80 , levorphanol claim 80 , morphine claim 80 , oxymorphone claim 80 , or oxycodone.84. The composition of claim 80 , wherein the drug comprises a stimulant selected from dextroamphetamine and methylphenidate.85. The composition of claim 80 , wherein the drug comprises methylphenidate.86. The composition of claim 80 , wherein the composition comprises from about 20 weight percent to about 90 weight percent of the SAIB.87. The composition of claim 80 , wherein the CAB has a butyryl content ranging from about 17% to about 38%.88. The composition of claim 80 , wherein the CAB has an acetyl content ranging from about 13% to about 30%.89. The composition of claim 80 , wherein the CAB has a butyryl content ranging from about 17% to about 38% and an acetyl content ranging from about 13% to about 30%.90. The composition of claim 80 , wherein the CAB has at least one feature selected from a butyryl content ranging from about 17% to about 38% claim 80 , an acetyl content ranging from about 13% to about 30% claim 80 , and a hydroxyl content ranging from about 0.8% to about 1.7%.91. The composition of claim 80 , wherein the composition comprises from about 1 weight percent to about 8.6 weight percent of the CAB.92. The composition of ...

LIQUID FORMULATIONS OF LONG ACTING INTERFERON ALPHA CONJUGATE

Disclosed is a liquid formulation in which a long-acting INFα conjugate that has improved in vivo duration and stability can be stored stably for a long period of time. It comprises a stabilizer comprising a buffer, a sugar alcohol, a non-ionic surfactant and an isotonic agent. Being free of human serum albumin and other potential factors harmful to the body, the liquid formulation is free of concerns about viral infections and guarantees excellent storage stability to long-acting INFα conjugates. 1. A liquid formulation , comprising a pharmaceutically effective amount of a long-acting interferon alpha conjugate in which interferon alpha and an immunoglobulin Fc region are covalently linked together , and an albumin-free stabilizer containing a buffer , a sugar alcohol , a non-ionic surfactant and an isotonic agent.2. The liquid formulation of claim 1 , wherein the interferon alpha is native IFNα claim 1 , a derivative of native IFNα or a polypeptide having an activity similar to that of native IFNα.3. The liquid formulation of claim 1 , wherein the immunoglobulin Fc region is derived from an immunoglobulin selected from the group consisting of IgG claim 1 , IgA claim 1 , IgD claim 1 , IgE and IgM.4. The liquid formulation of claim 3 , wherein the immunoglobulin Fc region is a hybrid of two or more domains selected from the group consisting of IgG claim 3 , IgA claim 3 , IgD claim 3 , IgE claim 3 , and IgM claim 3 , said domains having different origins.5. The liquid formulation of claim 3 , wherein the immunoglobulin Fc region is a dimer or multimer of a single chain immunoglobulin composed of domains of same origin.6. The liquid formulation of claim 3 , wherein the immunoglobulin Fc region is an IgG4 Fc region.7. The Liquid formulation of claim 6 , wherein the immunoglobulin Fc region is an aglycosylated human IgG4 Fc region.8. The liquid formulation of claim 1 , wherein the interferon alpha is covalently linked to the immunoglobulin Fc region via a non-peptide ...

THERAPY-ENHANCING GLUCAN

A therapeutic composition for treatment of cancer in a mammal is disclosed. The composition comprises an effective amount of a glucan composition which is suitable for oral administration and for absorption through the gastrointestinal tract of the mammal, and at least one antibody for the cancer. A method of treating cancer in a mammal is also disclosed. The method comprises administering a suitable orally administered glucan and at least one antibody for the treatment of cancer to the mammal. In addition a composition for delivery of peptide, protein, RNA, DNA or plasmid comprising effective amount of a beta-glucan is disclosed. 123-. (canceled)24. A method for facilitating absorption of a DNA , RNA or plasmid in a subject , comprising orally administering an effective amount of a β-glucan and said DNA , RNA or plasmid , wherein expression of said DNA , RNA or plasmid after absorption is increased compared to oral administration in the absence of said β-glucan.25. The method of claim 24 , wherein expression of said DNA claim 24 , RNA or plasmid is increased by up to about 6-fold in the presence of said β-glucan than in its absence.26. The method of claim 24 , wherein expression of said DNA claim 24 , RNA or plasmid occurs in the monocytes of said subject.27. The method of claim 24 , wherein said glucan is derived from yeast.28. The method of claim 24 , wherein said β-glucan comprises β-1 claim 24 ,3 bonds in the backbone and branches of β-1 claim 24 ,3-linked glucose units claim 24 , attached to the backbone via β-1 claim 24 ,6 glycosidic bonds.29. The method of claim 24 , wherein said glucan has an average molecular weight of about 15 to about 350 kD.30. The method of claim 24 , wherein the subject is a human or animal.31. A method for increasing the expression of a DNA claim 24 , RNA or plasmid in a subject claim 24 , comprising orally administering said DNA claim 24 , RNA or plasmid claim 24 , and an amount of a β-glucan effective in increasing said expression. ...

Stable Formulations for Lyophilizing Therapeutic Particles

The present disclosure generally relates to lyophilized pharmaceutical compositions comprising polymeric nanoparticles which, upon reconstitution, have low levels of greater than 10 micron size particles. Other aspects of the invention include methods of making such nanoparticles. 1. A lyophilized pharmaceutical composition comprising:polymeric nanoparticles comprising: a poly(lactic) acid-block-poly(ethylene)glycol copolymer or poly(lactic)-co-poly(glycolic) acid-block-poly(ethylene)glycol copolymer, and a therapeutic agent;sucrose or trehalose; andhydroxypropyl β-cyclodextrin; wherein upon reconstitution of the lyophilized pharmaceutical composition in an aqueous medium, the composition comprises 4 to 6 weight percent of the sucrose or trehalose; and 7 to 12 weight percent of the hydroxypropyl β-cyclodextrin.2. The lyophilized pharmaceutical composition of claim 1 , wherein the poly(lactic) acid portion of the copolymer has a weight average molecular weight of about 10 kDa to about 25 kDa and the poly(ethylene)glycol portion of the copolymer has a weight average molecular weight of about 4 to about 6 kDa.3. The lyophilized pharmaceutical composition of claim 1 , wherein the poly(lactic) acid portion of the copolymer has a weight average molecular weight of about 16 kDa and the poly(ethylene)glycol portion of the copolymer has a weight average molecular weight of about 5 kDa.4. The lyophilized pharmaceutical composition of claim 1 , comprising about 4 to 6 weight percent sucrose.5. The lyophilized pharmaceutical composition of claim 1 , wherein the polymeric nanoparticles have a diameter of about 60 nm to about 140 nm.6. The lyophilized pharmaceutical composition of claim 2 , wherein the polymeric nanoparticles comprise about 3 to about 40 weight percent therapeutic agent.7. The lyophilized pharmaceutical composition of claim 1 , wherein the polymeric nanoparticles further comprise a ligand conjugated polymer.8. A 100 mL aqueous sample of a reconstituted ...

DRUG DELIVERY COMPOSITIONS

The present invention relates material that is useful in drug delivery compositions. The material comprises cellulose nanofibers and/or derivatives thereof, wherein the cellulose nanofibers are in a form of a hydrogel or membrane. The invention also provides methods for producing these materials and compositions and uses thereof. 1. A drug delivery composition , characterized in that the composition comprises cellulose nanofibers and/or derivatives thereof , wherein the cellulose nanofibers and/or derivatives thereof are in the form of a hydrogel and said cellulose nanofibers are obtained by mechanical disintegration , and drug or medicament.2. The composition according to claim 1 , characterized in that the diameter of cellulose nanofibers and/or derivatives thereof or nanofiber bundles in the cellulose nanofibers is less than 1 preferably less than 200 nm claim 1 , more preferably less than 100 nm.3. The composition according to claim 1 , characterized in that the cellulose nanofiber derivatives comprise chemically or physically modified derivatives of cellulose nanofibers or nanofiber bundles.4. The composition according to claim 1 , characterized in that the cellulose nanofibers and/or derivatives thereof are obtained from raw material comprising plant material or microbial cellulose or derived from bacterial fermentation processes.5. The composition according to claim 1 , characterized in that the composition is a topical claim 1 , subcutaneous claim 1 , intramuscular or intraocular composition.6. A method for producing a drug delivery composition according to claim 1 , characterized In that the method comprises the steps ofobtaining cellulose nanofibers by mechanical disintegration of cellulose raw material, cellulose pulp, or refined pulp,mixing together said cellulose nanofibers with water, combining the mixture with a medicament or drug to obtain the composition.7. The method according to claim 6 , characterized in that the mechanical disintegration is ...

LIQUID MEDICINAL COMPOSITION CONTAINING ECHINOCANDIN ANTIFUNGAL AGENT MICAFUNGIN

The present invention provides a liquid medicinal composition containing micafungin or a pharmaceutically acceptable salt thereof and a stabilizing agent. 2. The pharmaceutical composition according to claim 1 , wherein preferably claim 1 , the pharmaceutically acceptable salt of compound of Formula I is sodium salt.3. The pharmaceutical composition according to claim 1 , wherein said stabilizing agent is selected from: monosaccharide claim 1 , disaccharide or polysaccharide claim 1 , or the combinations thereof; preferably claim 1 , lactose claim 1 , sucrose claim 1 , maltose claim 1 , trehalose claim 1 , or the combinations thereof.4. The pharmaceutical composition according to claim 1 , wherein said composition is a liquid formulation.5. The pharmaceutical composition according to claim 1 , wherein the composition contains 1-150 mg/ml of compound of Formula I or a pharmaceutically acceptable salt thereof.6. The pharmaceutical composition according to claim 5 , wherein the composition contains 5-100 mg/ml of compound of Formula I or a pharmaceutically acceptable salt thereof.7. The pharmaceutical composition according to claim 1 , wherein the composition contains 10-500 mg/ml of stabilizing agent.8. The pharmaceutical composition according to claim 7 , wherein the composition contains 20-400 mg/ml of stabilizing agent.9. Use of the pharmaceutical composition according to claim 1 , wherein the composition is used for preparing medicaments for preventing and/or treating fungal infections in mammalian. The present invention relates to a liquid pharmaceutical composition for treating and/or preventing fungal infections. Particularly, the present invention relates to the compound of Formula I or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable amount of stabilizing agent, such as monosaccharide, disaccharide or polysaccharide, or the combinations thereof, preferably, lactose, sucrose, maltose, trehalose, or the combinations thereof. Said ...

Delivery of Therapeutic Agents Using Oligonucleotide-Modified Nanoparticles as Carriers

Disclosed are drug delivery compositions comprising an oligonucleotide-modified nanoparticle and a therapeutic agent. Specifically, disclosed are compositions comprising a number of oligonucleotide molecules in a ratio to therapeutic agent molecules to allow a sufficient transportation of the therapeutic agent molecules into a cell. The therapeutic agents include both hydrophobic and hydrophilic. Different attachments of therapeutic agents in a composition are also described. 1. A drug delivery composition comprising an oligonucleotide-modified nanoparticle and a therapeutic agent , said therapeutic agent being deliverable at a significantly lower level in the absence of attachment to the oligonucleotide-modified nanoparticle compared to the delivery of the therapeutic agent when attached to the oligonucleotide-modified nanoparticle , wherein the composition has a number of oligonucleotide molecules compared to therapeutic agent molecules in a ratio that is sufficient to allow transport of the therapeutic agent into a cell.2. The composition of wherein the therapeutic agent is a low molecular weight therapeutic agent.3. The composition of or wherein the therapeutic agent is hydrophobic.43. The composition of any of through wherein the therapeutic agent is hydrophilic.54. The composition of any one of through claims 1 , further comprising a detectable marker.65. The composition of any of through wherein the therapeutic agent is an agent selected from Table 2.76. The composition of any one of through wherein the oligonucleotide and the therapeutic agent are independently directly attached to the nanoparticle.86. The composition of any of through wherein the therapeutic agent is attached to the oligonucleotide attached to the nanoparticle.9. The composition of wherein the therapeutic agent is covalently attached to the oligonucleotide attached to the nanoparticle.10. The composition of wherein the therapeutic agent is non-covalently attached to the oligonucleotide ...

NANOPARTICLE DELIVERY SYSTEM AND COMPONENTS THEREOF

The present disclosure relates generally to a nanoparticle delivery system. The nanoparticles are formed from amphiphilic block copolymers comprising polylactide and dextran. The dextran may be conjugated to a targeting moiety in such a manner that the surface of the nanoparticle is coated with the targeting moiety. The size and targeting of the nanoparticles can be tuned by controlling surface density of the targeting moiety. The present disclosure also relates to polymers and macromolecules useful in the preparation of the mucoadhesive nanoparticles, as well as compositions, methods, commercial packages, kits and uses related thereto. 1. A block copolymer useful in the formation of a nanoparticle delivery system for encapsulating a hydrophobic therapeutic agent , the block copolymer having a hydrophobic portion consisting of polylactide and a hydrophilic portion consisting of dextran , the dextran having a plurality of functional groups capable of conjugation to a targeting moiety.2. The block copolymer of claim 1 , which is poly(D claim 1 ,L-lactide)-b-dextran.3. The block copolymer of claim 2 , wherein at least a portion of the functional groups are conjugated to the targeting moiety.4. The block copolymer of claim 3 , wherein the targeting moiety is phenylboronic acid.5. A nanoparticle useful for encapsulating a hydrophobic therapeutic agent claim 3 , the nanoparticle comprising a plurality of amphiphilic block copolymers claim 3 , each copolymer having a hydrophobic portion consisting of polylactide and a hydrophilic portion consisting of dextran claim 3 , the dextran having a plurality of functional groups capable of conjugation to a targeting moiety.6. The nanoparticle of claim 5 , wherein the block copolymer is poly(D claim 5 ,L-lactide)-b-dextran.7. The nanoparticle of claim 6 , wherein at least a portion of the functional groups are conjugated to the targeting moiety claim 6 , thereby providing a surface-functionalized nanoparticle.8. The nanoparticle of ...

PHARMACEUTICAL FORMULATION

A pharmaceutical formulation for a PKC modulatory peptide and a transport moiety comprising the aforementioned components and an anti-aggregant. 2. The solution of claim 1 , wherein the anti-aggregant sugar is selected from the group consisting of mannitol claim 1 , fructose claim 1 , sucrose and glycerol.3. The solution of claim 1 , wherein the conjugate is KAI-9803.4. The solution of claim 3 , wherein the anti-aggregant sugar is mannitol.5. An aqueous solution comprising claim 3 ,0.1 mg/mL to 10 mg/mL of a conjugate comprising a PKC modulatory peptide linked to a transport peptide via a disulfide bond, wherein the PKC modulatory peptide comprises the amino acid sequence SFNSYELGSL (SEQ ID NO:34),5.0 mg/mL to 40 mg/mL of an anti-aggregant sugar, andwater for injection.6. The solution of claim 5 , wherein the anti-aggregant sugar is selected from the group consisting of mannitol claim 5 , fructose claim 5 , sucrose and glycerol.7. The solution of claim 5 , wherein the conjugate is KAI-9803.8. The solution of claim 7 , wherein the anti-aggregant sugar is mannitol.9. An aqueous solution comprising claim 7 ,2.0 mg/mL to 3.0 mg/mL of a conjugate comprising a PKC modulatory peptide linked to a transport peptide via a disulfide bond, wherein the PKC modulatory peptide comprises the amino acid sequence SFNSYELGSL (SEQ ID NO:34),15 mg/mL to 25 mg/mL of an anti-aggregant sugar, andwater for injection.10. The solution of claim 9 , wherein the anti-aggregant sugar is selected from the group consisting of mannitol claim 9 , fructose claim 9 , sucrose and glycerol.11. The solution of claim 9 , wherein the conjugate is KAI-9803.12. The solution of claim 11 , wherein the anti-aggregant sugar is mannitol.13. An aqueous solution comprising claim 11 ,0.5 mg/mL to 5.0 mg/mL of a conjugate comprising a PKC modulatory peptide linked to a transport peptide via a disulfide bond, wherein the PKC modulatory peptide comprises the amino acid sequence SFNSYELGSL (SEQ ID NO:34),10.0 mg/mL to 30 ...

ORAL TABLET COMPOSITIONS OF DEXLANSOPRAZOLE

Oral tablet compositions of dexlansoprazole or pharmaceutically acceptable salts or hydrated forms thereof having a gradual release and processes for the manufacture of the tablet composition and its use in the treatment of gastrointestinal disorders. 1. An oral tablet of dexlansoprazole or pharmaceutically acceptable salts or hydrated forms thereof having a gradual release wherein said tablet comprises:a) 5.0 to 40.0% of dexlansoprazole in powder form;b) 60.0 to 95.0% of dexlansoprazole granule comprising lactose, microcrystalline cellulose, a hydrophobic and/or hydrophilic agent, an alkali compound, binders or their mixtures; andc) a single enteric coating that dissolves at between pH 5.5 and 6.4.2. The oral tablet according to claim 1 , wherein the compression force to form the tablet is between 2 to 30 kN.3. The oral tablet according to claim 1 , wherein the compression force to form the tablet is between 3 to 12 kN.4. The oral tablet according to claim 1 , wherein the weight ratio of lactose to microcrystalline cellulose in dexlansoprazole granule is between 1:20 and 1:5 by weight.5. The oral tablet according to claim 1 , wherein the weight ratio of lactose to microcrystalline cellulose in dexlansoprazole granule is about 1:9 by weight.6. The oral tablet according to claim 1 , wherein the hydrophobic and/or hydrophilic agents are selected from the group comprising hydrogenated vegetable oils such as hydrogenated castor oil; glyceryl behenate claim 1 , wax claim 1 , wax-like substance claim 1 , fats claim 1 , oils claim 1 , fatty acid claim 1 , fatty alcohol claim 1 , shellac claim 1 , pullulan claim 1 , agar claim 1 , gellan gum claim 1 , guar gum claim 1 , carageenan claim 1 , acacia gum claim 1 , gum arabic claim 1 , dextran claim 1 , pectin and their mixtures.7. The oral tablet according to claim 1 , wherein the single enteric coating that dissolves at between pH 5.5 and 6.4 is selected from the group comprising of cellulose acetate phthalate claim 1 , ...

COMBINED PHARMACEUTICAL PREPARATION

The invention relates to a combined pharmaceutical composition or pharmaceutical preparation, comprising a first component containing a first ligand for a polyspecific lectin in a reticuloendothelial cell and a second component containing a carrier, a labeling agent, or a medicament for treating a disease associated with a target cell, each of which is targeted by a second ligand for a polyspecific lectin in a reticuloendothelial cell different from the first ligand, and also relates to a method for labeling a target cell and a method for treating a disease associated with a target cell, each using the same. 1. A combined pharmaceutical preparation comprising a first component containing mannose or a compound having terminal mannose and a second component containing a substance selected from the group consisting of a drug that controls the activity or growth of a fucosylated molecule-producing cell , a medicament for treating a disease related to a fucosylated molecule-producing cell , a carrier and a labeling agent , wherein the substance is targeted by a fucose or a molecule having terminal fucose.2. The pharmaceutical preparation according to claim 1 , wherein the first component and the second component are administered simultaneously and/or sequentially.3. (canceled)4. The pharmaceutical preparation according to claim 1 , wherein the medicament comprises a drug selected from the group consisting of an anti-inflammatory agent and an antitumor agent.57.-. (canceled)8. The pharmaceutical preparation according to claim 1 , wherein the labeling agent contains a label selected from the group consisting of a gas or a substance that generates a gas under physiological conditions claim 1 , a radioisotope claim 1 , a magnetic substance claim 1 , a nuclear magnetic resonance element claim 1 , a substance that affects the relaxation time of a nuclear magnetic resonance element claim 1 , a substance that binds to a labeling substance claim 1 , a fluorescent substance claim ...

LIQUID FORMULATION OF G-CSF

Provided are pharmaceutical liquid formulations of G-CSF, which are stable over a long time period and substantially free of excipients, as well as ready-to-use syringes containing such formulations and corresponding kits. 120-. (canceled)21. A method for the treatment of cancer , severe chronic neutropenia (SCN) , HIV infection , a damage of the central nervous system , adverse side effects owing to cytotoxic chemotherapy , or for the accompanying therapy of diseases , wherein a mobilization of peripheral blood precursor cells is required , the method comprising administering a medicament to a patient in need thereof , wherein the medicament comprises an aqueous liquid formulation of G-CSF , the aqueous liquid formulation of G-CSF comprising G-CSF , sorbitol at a concentration of 5% w/v , polysorbate at a concentration of 0.05 to 0.06 mg/ml and acetate at a concentration of 10 mM as a buffer substance at a pH value of 4.15 to 4.3.22. The method of claim 21 , wherein the medicament is administered by subcutaneous or intravenous administration.23. The method of claim 21 , wherein the administration of G-CSF is provided at a dosage of 5 to 30 μg/kg body weight. 1. Field of the InventionObjects of the present invention are stable, aqueous liquid formulations of G-CSF, substantially consisting of G-CSF and a sugar alcohol, a surfactant, a buffer substance at a pH value of about 4.1 to 4.4, and optionally also amino acids and/or glycerol and/or carbohydrates and/or preservatives.2. Description of Related ArtMany of the hitherto known dosage forms for protein agents have disadvantages. For instance, certain preparations contain pharmaceutical additives or excipients that cannot readily be categorized as harmless from a medical point of view. Due to their origin and physico-chemical properties, polymers and proteins bear a certain risk potential with respect to their suitability as pharmaceutical additives. Proteins of human or animal origin as well as proteins obtained ...

Compositions For Achieving A Therapeutic Effect In An Anatomical Structure

Compositions and methods of using the compositions are provided for forming an embolus within a region of an anatomical lumen for a transitory period in order to achieve a therapeutic effect. 1. A particle to form an embolus within a region of an anatomical lumen , comprising a biodegradable inorganic substance selected from the group consisting of hydroxyapatite , dahlite , brushite , calcium sulphate , octacalcium phosphate , amorphous calcium phosphate and beta-tricalcium phosphate and a combination thereof , wherein the biodegradable inorganic substance allows the particle to form the embolus within the region for a transitory period , and where the transitory period is less than one week.2. The particle of claim 1 , wherein the biodegradable inorganic substance allows a diameter of the particle to be reduced or to disintegrate into fragments.3. The particle of claim 1 , further comprising a therapeutic substance.4. The particle of claim 1 , further comprising a polymeric material.5. The particle of claim 3 , wherein the therapeutic substance is selected from the group consisting of antineoplastic claim 3 , antiplatelet claim 3 , anticoagulant claim 3 , fibrinolytic claim 3 , antimitotic claim 3 , thrombin inhibitor claim 3 , antiinflammatory claim 3 , antiproliferative claim 3 , antioxidant claim 3 , antiangio genic claim 3 , angiogenic claim 3 , arterio genic and antiallergic substances claim 3 , and combinations thereof.617-. (canceled)18. A composition for a therapeutic treatment claim 3 , comprising a particle including a surfactant and a therapeutic substance claim 3 , the particle configured to form an embolus within a region of an anatomical lumen.19. The composition of claim 18 , wherein the surfactant is selected from the group consisting of sorbitan monooleate claim 18 , polyoxyethylene trioleate claim 18 , and poly(ethylene oxide)-b-poly(propylene oxide)-b-poly(ethylene oxide) triblock copolymers.20. The composition of claim 18 , wherein the ...

TREATMENT OF HIV

We describe methods of treatment of HIV using proopiomelanocortin (POMC) and corticotropin releasing factor (CRF) peptides and their products, as well as uses of such peptides in the preparation and medicaments. 119.-. (canceled)20. A method of treatment of HIV comprising administering a corticotropin releasing factor (CRF) peptide to a patient.21. The method of claim 20 , wherein one or more of the following effects is achieved: a reduction in viral load; an increase in CD4 cells; or an increase in CD8 cells.22. The method of wherein the CRF is non-human CRF.23. The method of wherein the CRF is goat CRF.24. The method of further comprising administering one or more peptide regulatory or releasing factors.25. The method of wherein the factors are selected from the group comprising α-HLA claim 24 , TGF-β claim 24 , and IL-10.26. The method of further comprising administering one or more of vasopressin claim 20 , β-endorphin claim 20 , and an enkephalin.27. The method of further comprising administering CRF binding protein (CRF-BP).28. The method of further comprising administering a POMC peptide or a POMC product.29. A method of treatment of HIV comprising administering a POMC peptide and/or a POMC product to a patient.30. A method of treatment of HIV comprising administering two or more of alpha claim 20 , beta claim 20 , and gamma melanocyte stimulating hormone (MSH); adrenocorticotrophin (ACTH); beta and gamma lipotropin (LPH); and beta endorphin.31. A method for the treatment of HIV in a patient claim 20 , said method comprising administering to said patient a composition selected from the group consisting of (i) a corticotropin releasing factor (CRF) peptide and a POMC peptide and (ii) a CRF peptide and a POMC product.32. The method of wherein said CRF peptide is a non-human CRF peptide.33. The method of wherein said non-human CRF peptide is a goat CRF peptide.34. The method of wherein said administering achieves an effect selected from the group consisting of: ...

Highly concentrated aqueous protein solution with reduced viscosity

In an aqueous solution, a composition includes at least one protein, including at least one antibody fragment, and at least one water-soluble viscosity-reducing agent chosen from the group consisting of cytidine, 2′-deoxycytidine, uridine, 2′-deoxyuridine, thymidine and ribothymidine, alone or as a mixture. The protein includes at least one antibody fragment being at a concentration greater than or equal to 50 mg/ml. 1. A composition comprising , in an aqueous solution , at least one protein comprising at least one antibody fragment , and at least one water-soluble viscosity-reducing agent chosen from the group consisting of cytidine , 2′-deoxycytidine , uridine , 2′-deoxyuridine , thymidine and ribothymidine , alone or as a mixture.2. The composition as claimed in claim 1 , wherein the viscosity-reducing agent is chosen from cytidine claim 1 , 2′-deoxycytidine and uridine claim 1 , alone or as a mixture.3. The composition as claimed in claim 1 , wherein the concentration of protein comprising at least one antibody fragment in the final formulation is greater than or equal to 50 mg/ml.4. The composition as claimed in claim 1 , wherein the concentration of protein comprising at least one antibody fragment in the final formulation is between 50 and 350 mg/ml.5. The composition as claimed in claim 1 , wherein the concentration of protein comprising at least one antibody fragment in the final formulation is between 100 and 350 mg/ml.6. The composition as claimed in claim 1 , wherein its pH is between 5 and 8.7. The composition as claimed in claim 1 , wherein the concentration of viscosity-reducing agent is greater than or equal to 10 mM.8. The composition as claimed in claim 1 , wherein the final concentration of viscosity-reducing compound is between 10 and 350 mM.9. The composition as claimed in claim 1 , wherein the final concentration of viscosity-reducing compound is between 50 and 350 mM.10. The composition as claimed in claim 1 , wherein the protein comprising at ...

SELF-GELATINIZABLE NUCLEIC ACID

The purpose of the invention of the present application is to a method for preparing a hydrogel composed substantially only of nucleic acids. The invention of the present application provides: a nucleic acid sol-like composition for producing a nucleic acid gel without requiring the use of any nucleic acid ligase, wherein the composition comprises at least two nucleic acid monomers which are partly complementary to each other and are independently selected from the group consisting of a nucleic acid, a nucleic acid derivative, a modified nucleic acid, a compound capable of binding to a nucleic acid in complementary manner and a mixture thereof, one of the nucleic acid monomers has a moiety that constitutes a cohesive protruding end and a complementary nucleotide sequence moiety that can bind to at least one of the other nucleic acid monomers to form a double strand, and the composition contains no nucleic acid ligase; and a nucleic acid gel produced using the composition. 116-. (canceled)17. A sol-like composition for producing a nucleic acid gel which does not contain a nucleic acid linking enzyme in a living body , the composition containing a mixture of two or more oligonucleotides composed of a cohesive protruding end moiety and a complementary base sequence moiety in the composition at a nucleic acid concentration of 0.3 mM+1.6/x (the number of bases in the protruding end moiety) mM or less , not containing a nucleic acid linking enzyme , and having a salt concentration of 80 mM/x (the number of bases in the protruding end moiety) or less in terms of a NaCl concentration:whereinthe cohesive protruding end moiety is a single strand nucleic acid moiety having 4 or more nucleotide length and being complementary to a cohesive protruding end moiety in at least another oligonucleotide to such a degree as to form a double strand sequence showing a melting temperature that is equal to or higher than the body temperature in a physiological condition, andthe ...

Treatment of Prior Disease With Oral Interferon Alpha

The present disclosure is directed to compositions and methods for treating prion diseases through oral administration of low doses of interferon-alpha. In one embodiment a composition is administered comprising interferon-alpha and trehalose. 1. A method of treating bovine spongiform encephalopathy , said method comprisingidentifying animals at risk of bovine spongiform encephalopathyadministering to said animals a composition comprising an effective amount of interferon-alpha.2. The method of wherein the interferon is administered orally.3. The method of wherein the interferon is admixed with the animals' water or feed.4. The method of wherein the amount of interferon-alpha is administered in a dosage of about 0.1 IU/lb to about 100 IU/lb of patient body weight.5. The method of wherein said composition further comprises trehalose.6. The method of wherein the composition further comprises a disaccharide selected from the group consisting of maltose claim 5 , lactose and fructose.7. The method of wherein the disaccharide is anhydrous crystalline maltose.8. A supplemented animal feed claim 6 , comprising:a feed supplement, wherein said feed supplement comprisesa type I interferon;trehalose; anda disaccharide selected from the group consisting of maltose, lactose and fructose;anda standard animal feed formulation, wherein said feed supplement is admixed with said standard animal feed formulation.9. The supplemented animal feed of wherein the type I interferon is interferon-alpha.10. The supplemented animal feed of wherein the disaccharide is anhydrous crystalline maltose.11. The supplemented animal feed of wherein the animal feed formulation isfor a ruminant species, said feed supplement being prepared in an encapsulated form, whereinthe encapsulated feed supplement bypasses the rumen before releasing its contents to thedigestive tract of the ruminant species.12. A method of stablizing PrPc in a vertebrate species claim 8 , said method comprising administering a ...

SUSTAINED RELEASE SOLID DOSAGE PREPARATIONS

A sustained release solid dosage preparation is provided comprising an active ingredient admixed with an excipient. At least part of the excipient consists of glucomannan microparticles having an average particle size less than 50 μm. The glucomannan microparticles forms, when absorbing water, a hydrogel matrix for the active ingredient capable releasing the active ingredient almost entirely up about 6 hours. 1. A sustained release solid dosage preparation comprising an active ingredient admixed with an excipient , wherein at least part of said excipient consists of glucomannan microparticles having an average particle size of from about 25 μm to less than 50 μm which forms , when absorbing water in the digestive tract , a hydrogel matrix for the active ingredient capable of releasing the active ingredient almost entirely up to about 6 hours.2. (canceled)3. The sustained release solid dosage preparation according to claim 1 , wherein said glucomannan microparticles pass through 200 mesh screen entirely.4. The sustained release solid dosage preparation according to claim 1 , wherein said glucomannan microparticles are produced from crude or refined konjac glucomannan flour by subjecting the flour to the wet grinding process after decreasing the moisture content by suspending in an aqueous ethanol having an ethanol concentration greater than 70% to allow diffusion of water into the aqueous ethanol.5. The sustained release solid dosage preparation according to further comprising an auxiliary excipient selected from the group consisting of a sugar alcohol claim 1 , a saccharide claim 1 , a polysaccharide claim 1 , and gum.6. The sustained release solid dosage preparation according to claim 1 , wherein the mixture of said active ingredient and said excipient is encapsulated in a hard capsule.7. The sustained release solid dosage preparation according to claim 1 , wherein the mixture of said active ingredient and said excipient is directly compressed into tablets with ...

ANTI-CONNEXIN ANTIBODY FORMULATIONS

The present disclosure relates to pharmaceutical compositions and methods for treating a disease or condition associated with opening of Cx43 hemichannels in astrocytes or osteocytes, preferably for treating an inflammatory disease or condition or a neurodegenerative disease such as spinal cord injury. 1. A pharmaceutical formulation comprising:an anti-Cx43 antibody or antigen binding fragment thereof;a buffer;a surfactant; anda stabilizer;wherein the pharmaceutical formulation has a pH of between about 5 and about 6; a first, second and third heavy chain complementarity determining region (CDR) sequence having the amino acid sequence of SEQ ID NOs: 1, 2, and 3, respectively; and', 'a first, second and third light chain CDR sequence having the amino acid sequence of SEQ ID NOs: 4, 5, and 6, respectively., 'wherein the anti-Cx43 antibody or antigen binding fragment thereof comprises2. The pharmaceutical formulation of claim 1 , wherein the anti-Cx43 antibody or antigen binding fragment thereof comprises a heavy chain variable domain having the amino acid sequence of SEQ ID NO: 7 claim 1 , and a light chain variable domain having the amino acid sequence of SEQ ID NO: 8.3. The pharmaceutical formulation of claim 2 , wherein the anti-Cx43 antibody or antigen binding fragment thereof comprises a heavy chain having an amino acid sequence selected from the group consisting of SEQ ID NOs: 9-17 claim 2 , and a light chain having the amino acid sequence of SEQ ID NO: 18.4. The pharmaceutical formulation of claim 1 , wherein the anti-Cx43 antibody or antigen binding fragment thereof binds to an epitope located within the amino acid sequence of FLSRPTEKTI (SEQ ID NO: 19).5. The pharmaceutical formulation of claim 4 , wherein the epitope comprises one or more amino acids selected from the group consisting of R4 claim 4 , P5 claim 4 , E7 claim 4 , K8 and I10 of SEQ ID NO: 19.6. The pharmaceutical formulation of claim 4 , wherein the epitope consists of R4 claim 4 , P5 claim 4 , ...

LIQUID PHARMACEUTICAL COMPOSITION

The present invention relates to novel liquid pharmaceutical compositions of adalimumab, which include adalimumab or a biosimilar thereof, EDTA, and a small polyol stabiliser such as glycerol. Such a combination of components furnishes formulations having a stability (e.g. on storage and when exposed to stress) which is comparable to or an improvement upon those known in the art, and with fewer ingredients. Such advances will help adalimumab treatments to become more widely available at lower cost, and prolong the viability of pre-loaded delivery devices (e.g. pre-filled syringes) to reduce unnecessary waste of the drug. 1. A liquid pharmaceutical composition comprising:(a) adalimumab;(b) EDTA; and(c) a C2-C5 polyol.2. The liquid pharmaceutical composition according to claim 1 , wherein the polyol is a C2-C4 polyol claim 1 , suitably glycerol.3. The liquid pharmaceutical composition according to any one of to claim 1 , wherein the composition further comprises a buffer system claim 1 , suitably an acetate buffer system claim 1 , suitably an acetate buffer system formed without generating sodium chloride claim 1 , suitably an acetate buffer system formed by basification of a quantity of acetic acid.4. The liquid pharmaceutical composition according to any one of to claim 1 , comprising 25 to 125 mg/ml adalimumab.5. The liquid pharmaceutical composition according to any one of to claim 1 , wherein the composition is free of claim 1 , substantially free of claim 1 , or comprises at most 40 mM of a tonicifier claim 1 , suitably where the tonicifier is sodium chloride; and/orwherein the liquid pharmaceutical composition comprises arginine, suitably L-arginine.6. The liquid pharmaceutical composition according to claim 1 , comprising:(a) adalimumab;(b) EDTA;(c) a C2-C5 polyol;(d) a buffer system; and(e) a surfactant;wherein the composition has a pH between 4.0 and 6.0.7. The liquid pharmaceutical composition according to claim 6 , comprising:(a) adalimumab;(b) EDTA;(c) a ...

IMMUNOPROTEASOME INHIBITOR FORMULATIONS

Provided herein are pharmaceutical formulations comprising KZR-616 or a salt thereof, and a sugar, wherein the formulations are lyophilized, methods of preparing said formulations, methods of treating immune-related diseases, and methods of treating inflammation. 2. The formulation of claim 1 , wherein KZR-616 is as a maleate salt.3. The formulation of or claim 1 , having a pH of 3.0 to 4.5 claim 1 , as measured prior to lyophilization.4. The formulation of claim 3 , having a pH of 3.8 to 4.3.5. The formulation of claim 4 , having a pH of 4.2.6. The formulation of any one of to claim 4 , is absent an additional buffer.7. The formulation of any one of to claim 4 , further comprising a succinate buffer.8. The formulation of any one of to claim 4 , wherein the KZR-616 or a salt thereof is present at an amount of 50 to 300 mg/mL claim 4 , as measured prior to lyophilization.9. The formulation of claim 8 , wherein the KZR-616 or a salt thereof is present in an amount of 100 mg/mL to 200 mg/mL.10. The formulation of claim 9 , wherein the KZR-616 or a salt thereof is present in an amount of 125 mg/mL based on the weight of the KZR-616 free base.11. The formulation of any one of to claim 9 , wherein the sugar is present at an amount of 0.1 wt % to 5 wt % claim 9 , based upon total weight of the formulation.12. The formulation of claim 11 , wherein the sugar is present in an amount of 1.5 wt % to 3 wt %.13. The formulation of claim 12 , wherein the sugar is present in an amount of 2 wt %.14. The formulation of any one of - claim 12 , wherein the sugar comprises mannitol claim 12 , trehalose claim 12 , or a combination thereof.15. The formulation of claim 14 , wherein the sugar comprises trehalose.16. The formulation of any one of - claim 14 , wherein the lyophilized formulation has a moisture content of less than 1%.17. The formulation of any one of to claim 14 , having a pH of 4.1 to 4.3 (as measured when reconstituted) after storage at 5° C. claim 14 , 25° C. claim 14 , or ...

"Medical Articles Coated With Organopolysiloxane Containing a Protein Solution"

This invention relates to methods for evaluating or inhibiting the aggregation of a protein in an aqueous suspension including organopolysiloxane and medical articles coated with organopolysiloxane containing a protein solution including sugar and non-ionic surfactant. 1. A medical article , comprising:(a) a container comprising a chamber for receiving a solution, wherein the inner surface of the chamber has a coating thereon prepared from a composition comprising an organopolysiloxane; and (i) at least one proteinaceous material;', '(ii) at least one non-ionic surfactant; and', '(iii) at least one sugar., '(b) a solution comprising2. The medical article according to claim 1 , wherein the chamber is selected from the group consisting of a syringe barrel claim 1 , drug cartridge container claim 1 , needleless injector container claim 1 , liquid dispensing device container claim 1 , and liquid metering device container.3. The medical article according to claim 2 , wherein the chamber is a syringe barrel.4. The medical article according to claim 1 , wherein the chamber is formed from glass claim 1 , metal claim 1 , ceramic claim 1 , plastic claim 1 , rubber claim 1 , or combinations thereof.5. The medical article according to claim 1 , wherein the chamber is prepared from an olefinic polymer selected from the group consisting of polyethylene claim 1 , polypropylene claim 1 , poly(1-butene) claim 1 , poly(2-methyl-1-pentene) claim 1 , and cyclic polyolefins.6. The medical article according to claim 1 , wherein the organopolysiloxane is polydimethylsiloxane.7. The medical article according to claim 1 , further comprising a sealing member having an exterior surface in sliding engagement with at least a portion of the interior surface of the chamber.8. The medical article according to claim 1 , wherein the sugar is selected from the group consisting of monosaccharides claim 1 , disaccharides claim 1 , trisaccharides claim 1 , oligosaccharides and mixtures thereof.9. A ...

IMMUNOCONJUGATES TARGETING CD46 AND METHODS OF USE THEREOF

Disclosed herein are immunoconjugates comprising a CD46 binding domain and effector agent. Further provided herein are methods of treating cancer comprising administering to a subject having cancer a pharmaceutical composition comprising immunoconjugates comprising a CD46 binding domain and effector agent. 1. A pharmaceutical composition comprising an immunoconjugate , a pharmaceutically acceptable buffer , and a pharmaceutically acceptable stabilizing agent , [ a first heavy chain comprising SEQ ID NO: 9,', 'a first light chain comprising SEQ ID NO: 10,', 'a second heavy chain comprising SEQ ID NO: 9, and', 'a second light chain comprising SEQ ID NO: 10; and, 'a recombinant antibody comprising, 'one, two, three or four pairs of adducts;', 'wherein each adduct of said one, two, three or four pairs of adducts comprises a monomethylauristatin E (MMAE) that is conjugated to said recombinant antibody via a maleimidocaproyl-valine-citrulline-para-amino benzyloxycarbonyl (mc-vc-PAB) linker;', 'wherein each of said one, two, three or four pairs of adducts is conjugated to a pair of cysteine residues of said recombinant antibody,', C219 of the first heavy chain and C214 of the first light chain;', 'C219 of the second heavy chain and C214 of the second light chain;', 'C225 of the first heavy chain and C225 of the second light chain; and', 'C228 of the first heavy chain and C228 of the second light chain., 'wherein said pairs of cysteine residues are selected from], 'wherein the immunoconjugate comprises2. The pharmaceutical composition of claim 1 , wherein the buffer comprises citrate claim 1 , phosphate claim 1 , acetate claim 1 , tromethamine claim 1 , histidine claim 1 , succinate claim 1 , malate claim 1 , or α-ketoglutaric acid.3. The pharmaceutical composition of claim 1 , wherein the buffer comprises from about 10 mM to about 30 mM histidine and the pH is from about 5 to about 7.4. The pharmaceutical composition of claim 1 , wherein the buffer comprises about 20 mM ...

PREPARATION OF SOLID DOSAGE FORMS COMPRISING ANTIBODIES BY SOLUTIONS/SUSPENSION LAYERING

The present invention relates to a method for preparing immediate and sustained release solid dosage forms, comprising antibodies and functional fragments thereof, by solution/suspension layering,optionally coated with a delayed release coating; the solid dosage forms prepared by the method; and the use of the solid dosage forms in the topical treatment in the gastrointestinal tract of a patient. 1. A method for preparing a solid dosage form comprising i) an inert core unit; and ii) a drug coating , comprising at least one antibody or functional fragment thereof as active agent , a buffer and at least one polymeric binder deposited on the inert core unit by drug layering; said comprising the steps of;a) preparing an active agent coating liquid, comprising the at least one antibody or functional fragment thereof, the buffer and the at least one polymeric binder, as an aqueous solution or suspension;b) layering the inert core unit with the active agent coating liquid of step (a) using spray coating;c) drying the wet drug layered inert core unit, simultaneously with step b), or after step b) has been completed, to give rise to a dried solid dosage form.2. The method according to claim 1 , wherein the active agent coating liquid comprises 1-50 mg/ml of the at least one antibody or functional fragment thereof.3. The method according to claim 1 , wherein the active agent coating liquid comprises:i) 0.5-5 wt.-% antibody or functional fragment thereof;ii) 1-20 wt.-% polymeric binder; andiii) 0-2 wt.-% anti-tacking agent.4. The method according to claim 1 , wherein during the fluidized-bed spray coating the atomizing air pressure at the spray nozzle is lower than 200 kPa.5. The method according to claim 1 , wherein at any time during steps a) and c) the temperature of the at least one antibody or functional fragment thereof is lower than the melting temperature (Tm) of the at least one antibody or functional fragment thereof.6. The method according to claim 1 , wherein the ...

PHARMACEUTICAL COMPOSITION IN SOLID EXTRUDED FORM

A pharmaceutical composition including an extruded solid and one or more pharmaceuticals or nutraceuticals is provided. The extruded solid includes hydroxypropylmethylcellulose acetate succinate and isomalt. 1. A pharmaceutical composition comprising an extrudable solid and one or more pharmaceuticals wherein the extrudable solid comprises hydroxypropylmethyl cellulose acetate succinate and isomalt2. The pharmaceutical composition of claim 1 , in the form of a tablet claim 1 , pellet or granule.3. The pharmaceutical composition according to claim 1 , further comprising a control release agent.4. The pharmaceutical composition according to wherein the control release agent is selected from the group consisting of hypromellose claim 3 , hydroxypropyl cellulose claim 3 , ethylcellulose claim 3 , hydroxypropylmethylcellulose phthalate claim 3 , cellulose acetate phthalate claim 3 , carboxymethylethylcellulose claim 3 , methyl methacrylate-methacrylate copolymer claim 3 , methacrylate-ethyl acrylate copolymer claim 3 , methacrylate-methyl acrylate-methyl methacrylate copolymer claim 3 , polyvinyl acetate phthalate and shellac.5. The pharmaceutical composition according to claim 1 , further comprising a disintegrant.6. The pharmaceutical composition according to wherein the disintegrant is selected from the group consisting of hydroxypropylcellulose claim 5 , low-substituted hydroxypropylcellulose claim 5 , carboxymethylcellulose claim 5 , sodium carboxymethylcellulose claim 5 , calcium carboxymethylcellulose claim 5 , crospovidone claim 5 , croscarmellose sodium claim 5 , starches; crystalline cellulose claim 5 , sodium starch glycolate claim 5 , and alginic acid or a salt thereof.7. The pharmaceutical composition according to claim 1 , further comprising a filler.8. The pharmaceutical composition according to wherein the filler comprises lactose claim 7 , lactose monohydrate claim 7 , lactitol claim 7 , saccharose claim 7 , sorbitol claim 7 , mannitol claim 7 , ...

IMMUNOGLOBULIN FORMULATION AND METHOD OF PREPARATION THEREOF

A stable aqueous pharmaceutical formulation comprising a therapeutically effective amount of an antibody, polysorbate 80, a buffer which inhibits polysorbate oxidation is described along with methods of making the preparation. Also described are formulations with high antibody concentrations which maintain fixed volumes and which may be used on patients of variable weight. 1. A stable , aqueous pharmaceutical formulation comprising from about 20 mg/ml to about 150 mg/ml of natalizumab , polysorbate 80 present in an amount of about 0.0001% to 2% (w/v) , about 10 mM phosphate buffer , and about 140 mM NaCl.2. The formulation of claim 1 , comprising about 150 mg/ml natalizumab.3. The formulation of claim 1 , wherein the formulation is isotonic.4. The formulation of claim 1 , wherein the formulation is stable at a temperature of 2° C. to 8° C. for at least 6 months.5. The formulation of claim 1 , wherein the formulation has a pH of 3.0 to 7.0.6. The formulation of claim 4 , wherein the pH is 5.5 to 6.5.7. An article of manufacture comprising a container holding the stable claim 1 , aqueous pharmaceutical formulation of .8. An article of manufacture comprising a container holding the stable claim 2 , aqueous pharmaceutical formulation of .9. An article of manufacture comprising a container holding the stable claim 3 , aqueous pharmaceutical formulation of .10. An article of manufacture comprising a container holding the stable claim 4 , aqueous pharmaceutical formulation of .11. An article of manufacture comprising a container holding the stable claim 5 , aqueous pharmaceutical formulation of .12. An article of manufacture comprising a container holding the stable claim 6 , aqueous pharmaceutical formulation of . This application is a continuation of U.S. application Ser. No. 12/572,978, filed Oct. 2, 2009, which is a continuation of U.S. application Ser. No. 10/773,406, filed Feb. 9, 2004, which claims priority under 35 U.S.C. §119 to U.S. Provisional Application No. 60 ...

COMPOSITION COMPRISING HIGHLY-CONCENTRATED ALPHA1 PROTEINASE INHIBITOR AND METHOD FOR OBTAINING THEREOF

Compositions include highly-concentrated Alpha-1 Proteinase Inhibitor (A1PI) in a concentration greater than or equal to 100 mg/ml. Pharmaceutical compositions can be prepared from these compositions. The pharmaceutical compositions can be suitable for subcutaneous administration. The highly-concentrated A1PI solutions can be obtained by single-pass tangential flow filtration (SPTFF). 1. A composition comprising Alpha1-Proteinase Inhibitor (A1PI) in an aqueous solution , wherein the concentration of A1PI is greater than or equal to 100 mg/ml.2. The composition of claim 1 , wherein the concentration of A1PI is greater than or equal to 150 mg/ml.3. The composition of claim 1 , wherein the concentration of A1PI is greater than or equal to 200 mg/ml.4. The composition of claim 1 , wherein further comprises one or more uncharged excipient.5. The composition of claim 4 , wherein said one or more uncharged excipient is at a concentration to achieve an osmolality between 220 and 410 mOsm/kg HO.6. The composition of claim 5 , wherein said one or more uncharged excipient is at a concentration to achieve an osmolality of about 300 mOsm/kg HO.7. The composition of claim 1 , wherein the one or more uncharged excipient is selected from the group consisting of sorbitol claim 1 , serine claim 1 , trehalose claim 1 , alanine claim 1 , sucrose claim 1 , and mannitol claim 1 , and combinations thereof8. The composition of claim 7 , wherein the one or more uncharged excipient is selected from the group consisting of sorbitol claim 7 , trehalose claim 7 , alanine claim 7 , and combinations thereof.9. A pharmaceutical composition comprising the composition according to and a pharmaceutically acceptable carrier.10. The pharmaceutical composition of claim 9 , wherein the pharmaceutical composition is formulated for intravenous claim 9 , subcutaneous claim 9 , aerosol claim 9 , or intradermal administration.11. The pharmaceutical composition of claim 10 , wherein the pharmaceutical ...

STABLE ANTIBODY FORMULATION

The present invention provides stable pharmaceutical formulations comprising a human antibody that specifically binds to human programmed death-1 protein (PD-1). In certain embodiments, the formulations contain, in addition to an anti-PD-1 antibody, a buffer, an amino acid, a non-ionic surfactant, and a sugar. The pharmaceutical formulations of the present invention exhibit a substantial degree of antibody stability upon stress and storage. 172-. (canceled)73. A liquid pharmaceutical formulation comprising:(a) an antibody which binds specifically to human programmed death-1 (PD-1), wherein the antibody comprises three heavy chain complementarity determining regions (CDRs) (HCDR1, HCDR2 and HCDR3) contained in a heavy chain variable region (HCVR) of SEQ ID NO: 1 and three light chain CDRs (LCDR1, LCDR2 and LCDR3) contained in a light chain variable region (LCVR) of SEQ ID NO: 2;(b) a buffer comprising histidine;(c) an organic solvent comprising polysorbate;(d) a stabilizer comprising a sugar; and(e) a viscosity modifier comprising an amino acid;wherein the formulation has a pH of 6.0±0.3.74. The pharmaceutical formulation of claim 73 , wherein the antibody concentration is from 5 mg/mL±0.75 mg/mL to 250 mg/mL±37.5 mg/mL.75. The pharmaceutical formulation of claim 74 , wherein the antibody concentration is 25 mg/mL±3.75 mg/mL.76. The pharmaceutical formulation of claim 74 , wherein the antibody concentration is 50 mg/mL±7.5 mg/mL.77. The pharmaceutical formulation of claim 74 , wherein the antibody concentration is 150 mg/mL±22.5 mg/mL.78. The pharmaceutical formulation of claim 74 , wherein the antibody concentration is 175 mg/mL±26.25 mg/mL.79. The pharmaceutical formulation of claim 73 , wherein the histidine buffer concentration is from 5 mM±1 mM to 20 mM±4 mM.80. The pharmaceutical formulation of claim 79 , wherein the histidine buffer concentration is 10 mM±2 mM.81. The pharmaceutical formulation of claim 80 , wherein the histidine buffer comprises L-histidine ...

ROMIDEPSIN FORMULATIONS AND USES THEREOF

Provided herein are formulations of romidepsin. Also provided are methods for producing these formulations and uses thereof. In one embodiment, the formulation is a combination of romidepsin and mannitol. 1. A formulation comprising romidepsin and mannitol.2. The formulation of claim 1 , wherein substantially all of the romidepsin is amorphous.3. The formulation of claim 1 , wherein the ratio of romidepsin to mannitol is about 1:3.4. The formulation of claim 1 , wherein the ratio of romidepsin to mannitol is about 1:2.5. The formulation of claim 1 , wherein the ratio of romidepsin to mannitol is about 2:1.6. The formulation of claim 1 , wherein the formulation is a unit dosage form.7. The formulation of claim 6 , wherein the amount of romidepsin is about 10 mg per vial.8. The formulation of claim 6 , wherein the amount of mannitol is about 20 mg per vial.9. The formulation of claim 1 , wherein said composition is soluble in a solvent system consisting of propylene glycol (PG) claim 1 , ethanol (EtOH) and water.10. The formulation of claim 9 , wherein the amount of PG is between about 10% and about 70%.11. The formulation of claim 9 , wherein the amount of EtOH is between about 15% and about 65%.12. The formulation of claim 9 , wherein the amount of water is between about 20% and about 60%.13. The formulation of claim 9 , wherein the ratio of solvents is 45% PG claim 9 , 30% EtOH claim 9 , and 25% water.14. The formulation of claim 9 , wherein the ratio of solvents is 30% PG claim 9 , 40% EtOH claim 9 , and 30% water.15. The formulation of claim 9 , wherein the ratio of solvents is 53.3% PG claim 9 , 13.4% EtOH claim 9 , and 33.3% water.16. The formulation of claim 9 , wherein said composition is soluble in the solvent system within 30 seconds claim 9 , wherein the volume of the solvent system is 2 mL claim 9 , and wherein the amount of formulation is up to 30 mg.17. The formulation of claim 16 , wherein the amount of romidepsin is about 10 mg and the amount of ...

USE OF URODILATIN FOR PREPARING A MEDICAMENT FOR THE TREATMENT OF CARDIOVASCULAR, RENAL, PULMONARY AND NEURONAL SYNDROME WHILE AVOIDING A REBOUND

Use of urodilatin for preparing a medicament for the treatment of cardiovascular, renal, pulmonary and neuronal syndromes while avoiding a rebound, wherein said medicament for the delivery of urodilatin is suitable in a first quantity for a first period of at least 48 hours, followed by delivery over a second period of at least 12 hours with successive reduction of said first quantity continuously or gradually to 0 ng/kg/min. 1. Use of urodilatin for preparing a medicament for the treatment of cardiovascular , renal , pulmonary and neuronal syndromes while avoiding a rebound , wherein said medicament for the delivery of urodilatin is suitable in a first quantity for a first period of 48 hours or more , followed by delivery over a second period of 12 hours or more , in particular 24 hours or more with successive reduction of said first quantity continuously or gradually to 0 ng/kg/min.2. The use according to claim 1 , wherein said first period is from 48 hours to 120 hours claim 1 , from 48 hours to 96 hours claim 1 , from 48 hours to 72 hours claim 1 , from 48 hours to 60 hours claim 1 , from 72 hours to 96 hours claim 1 , from hours to 120 hours claim 1 , or from 96 hours to 120 hours.3. The use according to claim 1 , wherein said second period is from 12 hours to 72 hours claim 1 , from 12 hours to 48 hours claim 1 , from 12 hours to 36 hours claim 1 , from 12 hours to 24 hours claim 1 , from 24 hours to 72 hours claim 1 , from 24 hours to 48 hours claim 1 , from 24 hours to 36 hours claim 1 , from 36 hours to 48 hours claim 1 , from 36 hours to 72 hours claim 1 , or from 48 hours to 72 hours.4. The use according to claim 3 , wherein said successive reduction of the first quantity of urodilatin is effected from 15 ng/kg/min to 12.5 ng/kg/min after 4 hours claim 3 , to 10.0 ng/kg/min after 8 hours claim 3 , to 7.5 ng/kg/min after 12 hours claim 3 , to 5.0 ng/kg/min after 16 hours claim 3 , to 2.5 ng/kg/min after 20 hours claim 3 , and to 0 ng/kg/min after 24 hours. ...

FORMULATIONS OF HUMAN ANTI-PD-LI ANTIBODIES

This disclosure relates to formulations and compositions of an antibody directed against human anti-PD-L1, such as durvalumab. 2. The antibody formulation of claim 1 , wherein the anti-PD-L1 antibody comprises:(a) a light chain variable domain comprising the amino acid sequence of SEQ ID NO: 1, and a heavy chain variable domain comprising the amino acid sequence of SEQ ID NO: 2; or a VH CDR2 having the amino acid sequence of SEQ ID NO: 4; and', 'a VH CDR3 having the amino acid sequence of SEQ ID NO: 5; and', 'a VL CDR1 having the amino acid sequence of SEQ ID NO: 6; and', 'a VL CDR2 having the amino acid sequence of SEQ ID NO: 7; and', 'a VL CDR3 having the amino acid sequence of SEQ ID NO: 8., '(b) a VH CDR1 having the amino acid sequence of SEQ ID NO: 3; and'}3. The antibody formulation of claim 1 , wherein the buffer is histidine/histidine-HCl buffer.4. The antibody formulation of claim 1 , wherein the disaccharide is trehalose dihydrate.5. The antibody formulation of claim 1 , wherein the disaccharide is sucrose.6. The antibody formulation of claim 1 , wherein the surfactant is polysorbate 80.7. The antibody formulation of claim 1 , wherein the formulation is a liquid formulation claim 1 , a frozen formulation claim 1 , a lyophilized formulation claim 1 , or a reconstituted formulation.8. The antibody formulation of claim 1 , wherein less than about 1% of the anti-PD-L1 antibody forms an aggregate upon storage at 40° Celsius for about 1 month as measured by high-pressure size exclusion chromatography (HP-SPEC).9. The antibody formulation of claim 1 , wherein at least 97% of the anti-PD-L1 antibody is present as a monomer following storage at about 40° Celsius for about 1 month as measured by high-pressure size exclusion chromatography (HP-SEC).10. The antibody formulation of claim 1 , wherein at least 99% of the anti-PD-L1 antibody is present as a monomer following storage at about 40° Celsius for about 1 month as measured by high-pressure size exclusion ...

Absorption Enhancers for Drug Administration

A composition including a surfactant and at least one alkyl glycoside and/or saccharide alkyl ester and a drug. The surfactant composition(s) when admixed with a drug is non-toxic and non-irritating, while stabilizing and increasing the bioavailability of the drug. The invention also provides compositions that enhance absorption of drugs via the oral, ocular, nasal, nasolacrimal, inhalation or pulmonary, oral cavity (sublingual or Buccal cell) or CSF delivery route of a patient, including but not limited to insulin, glucagon and exendin-4. 1. An intranasal pharmaceutical composition comprising a suitable nontoxic , nonionic alkyl glycoside in combination with a compound that affects the central nervous system.2. The pharmaceutical composition of claim 1 , wherein the compound is a therapeutically effective amount of an anti-seizure agent.3. The pharmaceutical composition of claim 1 , wherein the alkyl glycoside has a hydrophobic alkyl group joined by a linkage to a hydrophilic saccharide.4. The pharmaceutical composition of claim 1 , wherein the alkyl glycoside is selected from the group consisting of octyl- claim 1 , nonyl- claim 1 , decyl- claim 1 , undecyl- claim 1 , dodecyl- claim 1 , tridecyl- claim 1 , tetradecyl- claim 1 , pentadecyl- claim 1 , hexadecyl- claim 1 , heptadecyl- claim 1 , and octadecyl-α- or β-D-maltoside claim 1 , -glucoside or -sucroside.5. The pharmaceutical composition of claim 1 , wherein the alkyl glycoside is dodecyl-α-D maltoside or dodecyl-β-D maltoside claim 1 , or a combination thereof.6. The pharmaceutical composition of claim 1 , wherein the alkyl glycoside is dodecyl β-D-maltoside.7. The pharmaceutical composition of claim 1 , wherein the alkyl glycoside has a concentration in the range of about 0.01% to 1.0%.8. The pharmaceutical composition of claim 6 , wherein the alkyl glycoside has a concentration in the range of about 0.01% to 1.0%.9. The pharmaceutical composition of claim 1 , wherein the alkyl glycoside has a hydrophile- ...

MICROBUBBLE ULTRASOUND CONTRAST AGENT FOR EXTERNAL USE

A microbubble ultrasound contrast agent for external use is provided. The microbubble ultrasound contrast agent applied externally can safely and efficiently enhance the permeation and absorption of the drug or small molecules in the local region of the body surface. A method of preparing the microbubble ultrasound contrast agent and a method of enhancing percutaneous absorption of a chemical or small molecules through a topical region of a biological body surface are provided. 1. An external use microbubble ultrasound contrast agent , comprising:a medium, wherein the medium is in a form of an aqueous solution or a gel form; and{'sup': 8', '10, 'a plurality of microbubbles dispersed in the medium, wherein a concentration of the microbubbles ranges from 4×10to 2×10particles/ml.'}2. The microbubble ultrasound contrast agent as claimed in claim 1 , wherein a material of the microbubbles is selected from albumin claim 1 , polymers claim 1 , liposomes claim 1 , copolymers or mixtures thereof or a combination of thereof claim 1 , and the medium is selected from an isotonic saline solution claim 1 , an agar gel claim 1 , an aloe gel claim 1 , a topical gel or a combination of thereof.3. The microbubble ultrasound contrast agent as claimed in claim 2 , wherein the material of the microbubbles further comprises hexose and/or pentose.4. The microbubble ultrasound contrast agent as claimed in claim 3 , wherein the hexose is dextrose.5. The microbubble ultrasound contrast agent as claimed in claim 1 , wherein the medium is a gel form medium and a content of the gel form medium is less than or equivalent to 0.2 percentages by weight of a total weight of the microbubble ultrasound contrast agent.6. The microbubble ultrasound contrast agent as claimed in claim 1 , wherein a particle size of the microbubbles ranges from 0.5 micrometers to 3.7 micrometers.7. The microbubble ultrasound contrast agent as claimed in claim 1 , further comprising a chemical or small molecules claim 1 , ...

METHOD OF EXTENDING HALF-LIFE OF CRYSTALINE ANTIBODIES

A composition for extending the half-life of a crystalline antibody, including synergistically effective amounts of a half-life-extending compound and a crystalline antibody. A composition for extending the half-life of a crystalline antibody including synergistically effective amounts of lactulose and a crystalline anti-PCSK9 antibody. A method of extending the half-life of a crystalline antibody, by administering a synergistically effective amount of a half-life-extending compound and a crystalline antibody to an individual, and extending the half-life of the crystalline antibody. A method of promoting antibody recycling by affecting a receptor for an antibody to recycle the antibody. 1. A composition for extending the half-life of a crystalline antibody , comprising synergistically effective amounts of a half-life-extending compound and a crystalline antibody.2. The composition of claim 1 , wherein said half-life-extending compound is chosen from the group consisting of a non-absorbable sugar claim 1 , a compound that converts NH3 to NH4+ claim 1 , a prebiotic claim 1 , a hydrogen-generating compound claim 1 , and combinations thereof.3. The composition of claim 2 , wherein said half-life-extending compound is lactulose or homologues thereof and is in an amount lower than indicated for treating constipation claim 2 , said amount being less than 10 g/day.4. The composition of claim 2 , wherein said non-absorbable sugar is chosen from the group consisting of lactulose claim 2 , glucose claim 2 , galactose claim 2 , fructose claim 2 , mannitol claim 2 , inulin claim 2 , sucralose claim 2 , aspartame claim 2 , dextrose claim 2 , maltodextrin claim 2 , homologues claim 2 , and combinations thereof.5. The composition of claim 2 , wherein said prebiotic is chosen from the group consisting of lactulose claim 2 , disaccharides claim 2 , inulin claim 2 , fructooligosaccharides (FOS) claim 2 , xylooligosaccharides (XOS) claim 2 , polydextrose claim 2 , oligofructose- ...

FORMULATIONS

The present invention relates to a pharmaceutical formulation comprising (i) a therapeutically effective amount of a bispecific protein comprising a soluble T cell receptor (TCR) and an scFV; and (ii) a surfactant. The w/w ratio of surfactant to protein is in the range of 0.75:1 to 1.5:1. The formulation may further comprise a bulking agent and/or a stabiliser. A further pharmaceutical formulation comprises (i) a therapeutically effective amount of a bispecific protein comprising a soluble T cell receptor (TCR) and an scFV; (ii) a bulking agent; and (iii) a stabiliser. The w/w ratio of stabiliser to bulking agent may be greater than 1:1. 2. The formulation of claim 1 , wherein the w/w ratio of surfactant to protein is 1:1.3. The formulation of claim 1 , further comprising a bulking agent.4. The formulation of claim 1 , further comprising a stabiliser.5. The formulation of claim 4 , wherein the ratio of stabiliser to bulking agent is greater than 1:1.7. The formulation of claim 6 , wherein the ratio of stabiliser to bulking agent is greater than 1.5:1.8. The formulation of claim 7 , wherein the ratio of stabiliser to bulking agent is in the range of from 3:1 to 7:1.9. The formulation of claim 6 , further comprising a surfactant.10. The formulation of claim 9 , wherein the surfactant is a polysorbate.11. The formulation of claim 10 , wherein the polysorbate is polysorbate 20.12. The formulation of claim 11 , wherein the bulking agent is a polyol.13. The formulation of claim 12 , wherein the polyol is mannitol.14. The formulation of claim 13 , wherein the stabiliser is a disaccharide.15. The formulation of claim 1 , further comprising a buffer.16. The formulation of claim 15 , wherein the buffer is phosphate/citrate.17. The formulation of claim 1 , having a pH in the range of from 6-7.18. The formulation of claim 1 , wherein the formulation is aqueous.19. The formulation of claim 1 , wherein the formulation is lyophilised.20. A method of making an aqueous ...

THERAPEUTIC PROTEIN FORMULATIONS

The present invention generally concerns formulations having a pH that inhibits aspartyl isomerization at an Asp-Asp motif in a therapeutic protein contained in such a formulation. 1. A formulation comprising a therapeutic protein having an Asp-Asp motif , wherein the formulation has a pH that inhibits aspartyl isomerization of an Asp residue in the Asp-Asp motif.2. A formulation comprising a therapeutic protein having an Asp-Asp motif , wherein the pH of the formulation is greater than 6.0 and less than 9.0.3. The formulation of claim 2 , wherein the pH is from 6.25 to 7.0.4. The formulation of claim 3 , wherein the pH is about 6.5.5. The formulation of claim 2 , wherein the therapeutic protein is an antibody.6. The formulation of claim 5 , wherein the antibody comprises a hypervariable region (HVR) that comprises an Asp-Asp motif.7. The formulation of claim 6 , wherein the Asp-Asp motif occurs in HVR-H3.8. The formulation of claim 7 , wherein the antibody is an anti-STEAP-1 antibody that comprises an HVR-H3 comprising the amino acid sequence of SEQ ID NO:16.9. The formulation of claim 8 , wherein the anti-STEAP-1 antibody further comprises one or more HVRs selected from (a) an HVR-H1 comprising the amino acid sequence of SEQ ID NO:14; (b) an HVR-H2 comprising the amino acid sequence of SEQ ID NO:15; (c) an HVR-L1 comprising the amino acid sequence of SEQ ID NO:11; (d) an HVR-L2 comprising the amino acid sequence of SEQ ID NO:12; and (e) an HVR-L3 comprising the amino acid sequence of SEQ ID NO:13.10. The formulation of claim 9 , wherein the antibody comprises (a) an HVR-H1 comprising the amino acid sequence of SEQ ID NO:14; (b) an HVR-H2 comprising the amino acid sequence of SEQ ID NO:15; (c) an HVR-H3 comprising the amino acid sequence of SEQ ID NO:16; (d) an HVR-L1 comprising the amino acid sequence of SEQ ID NO:11; (e) an HVR-L2 comprising the amino acid sequence of SEQ ID NO:12; and (f) an HVR-L3 comprising the amino acid sequence of SEQ ID NO:13.11. The ...

METHOD OF STEM CELL DELIVERY INTO THE BRAIN DURING CHRONIC DISEASE USING BLOOD BRAIN BARRIER PERMEABILIZERS

Blood brain barrier (BBB) permeabilizers, such as mannitol, can facilitate the entry of stem cells from the periphery to the stroke brain. It is unknown whether BBB permeation in the chronic stage of the disease still facilitates the entry of stem cells from the periphery to the injured brain. Evidence herein shows BBB permeation in the chronic stage of stroke assisted in the entry of stem cells from the periphery to the stroke brain. Stroke models treated with human umbilical cord stem cells (hUCBC) only (2 million viable cells), mannitol or a combination. Results revealed that hUCBC alone or combined with mannitol displayed significant behavioral and histological deficits compared to control animals, with the HUCBC-mannitol combined treatment showing improvements over hUCBC only treatments in brain cell survival in the peri-infarct area. BBB permeation in chronic stroke also lowers the effective stem cell dose necessary to improve functional outcomes. 1. A method of treating a chronic neurodegenerative disease , comprising the steps:identifying a patient suffering from a chronic neurodegenerative disease;obtaining at least one umbilical cord blood stem cell; andadministering the least one umbilical cord blood stem cell and a blood brain barrier permeabilizer to the patient after the acute phase of the neurodegenerative disease.2. The method of claim 1 , wherein the chronic neurodegenerative disease is chronic stroke.3. The method of claim 2 , wherein the least one umbilical cord blood stem cell and a blood brain barrier permeabilizer are administered 1 month after stroke. This application claims priority to U.S. Provisional Patent Application Ser. No. 62/214,027, entitled “Method of Stem Cell Delivery into the Brain During Chronic Disease using Blood Brain Barrier Permeabilizers”, filed Sep. 3, 2015, the contents of which are hereby incorporated by reference into this disclosure.This invention relates to treating chromic neuronal diseases. Specifically, the ...

STABLE ANTIBODY COMPOSITIONS AND METHODS OF STABILIZING SAME

The invention provides compositions and methods for inhibiting fractionation of immunoglobulins comprising a lambda light chain based on the observation that iron, in the presence of histidine, results in increased fragmentation of a recombinant fully human IgG molecule containing a lambda light chain due to cleavage in the hinge region. The invention further provides an aqueous pharmaceutical formulation comprising an antibody, or antigen-binding portion thereof, that binds the p40 subunit of IL-12/IL-23 and a buffer system comprising histidine, wherein the formulation has enhanced stability, including enhanced resistance to fragmentation. 1144.-. (canceled)145. A pharmaceutical formulation comprising:(a) 45 mg of antibody C340,(b) 1-10% sucrose,(c) 0.001-0.1% polysorbate 80, and(d) a buffer system comprising 1-50 mM histidine and having a pH of 5.7 to 6.3.146. A pharmaceutical formulation comprising:(a) 90 mg/mL of antibody C340,(b) 1-10% sucrose,(c) 0.001-0.1% polysorbate 80, and(d) a buffer system comprising 1-50 mM histidine and having a pH of 5.7 to 6.3.147. The formulation of claim 145 , wherein the formulation has a pH of about 6.148. The formulation of claim 145 , wherein the histidine comprises L-histidine.149. The formulation of claim 145 , wherein the formulation has a shelf life of at least 18 months.150. The formulation of claim 146 , wherein the formulation has a pH of about 6.151. The formulation of claim 146 , wherein the histidine comprises L-histidine.152. The formulation of claim 146 , wherein the formulation has a shelf life of at least 18 months.153. A method of treating a subject having a disorder in which the activity of the p40 subunit of IL-12 and/or IL-23 is detrimental claim 145 , the method comprising administering the formulation of to the subject claim 145 , thereby treating the subject.154. The method of claim 153 , wherein the disorder is psoriasis.155. The method of claim 153 , wherein the disorder is psoriatic arthritis.156. The ...

NICOTINE-CONTAINING PHARMACEUTICAL COMPOSITION

A composition intended to be employed for therapeutic purposes incorporates a nicotinic compound, a sugar substitute, and a sugar alcohol syrup. Representative forms of nicotine include free base (e.g., as a mixture of nicotine and microcrystalline cellulose), a nicotine salt (e.g., as nicotine bitartrate) or nicotine polacrilex. The composition is useful for treatment of central nervous system conditions, diseases, and disorders, and as a nicotine replacement therapy. 127-. (canceled)28. A method of preparing a nicotine-containing pharmaceutical composition , comprising:(i) mixing a non-hygroscopic sugar substitute capable of forming a glassy matrix in an amount of at least about 80% by weight and a sugar alcohol syrup in a melted state to form a mixture;(ii) cooling the mixture and incorporating a nicotinic compound into the cooled mixture; and(iii) further cooling the mixture to room temperature to form a solid nicotine-containing pharmaceutical composition.29. The method of claim 28 , wherein at least a portion of the nicotinic compound is in the form of a free base claim 28 , a salt claim 28 , a complex claim 28 , or a solvate.30. The method of claim 28 , wherein the nicotinic compound is nicotine polacrilex.31. The method of claim 28 , wherein the nicotinic compound is sorbed onto a porous particulate carrier.32. The method of claim 31 , wherein the porous particulate carrier comprises microcrystalline cellulose.33. The method of claim 28 , wherein the sugar substitute is isomalt.34. The method of claim 28 , wherein the sugar alcohol syrup is in an amount sufficient to slow recrystallization of the sugar substitute in melted form.35. The method of claim 28 , wherein the sugar alcohol syrup is maltitol syrup or xylitol syrup.36. The method of claim 28 , wherein the pharmaceutical composition comprises at least about 85% by weight of the sugar substitute.37. The method of claim 28 , wherein the pharmaceutical composition comprises at least about 4.0% by weight ...

Method of Treating Patients with a Mucinous Glycoprotein (MUC-1) Vaccine

The present invention provides a method for treating an individual who is afflicted with a cancer, such as non-small cell lung cancer or prostate cancer, by administering to that individual a MUC-1-based formulation. The formulation may be a MUC-1 based liposomal vaccine formulation. 1. (canceled)2. A method for treating a subject with prostate cancer comprising:(a) selecting for treatment a subject having prostate cancer wherein the subject has been HLA-typed and does not have an HLA haplotype selected from DQB1-02 and CWO7, and (i) a liposome; and', '(ii) at least one polypeptide comprising the amino acid sequence selected from the group consisting of the amino acid sequence of SEQ ID NO. 1 and the amino acid sequence of SEQ ID NO. 2., '(a) administering to that subject, for a period of time, a MUC-1-based formulation, wherein the formulation comprises3. The method of claim 1 , wherein the formulation further comprises at least one adjuvant.4. The method of claim 3 , wherein the adjuvant is selected from the group consisting of lipid A claim 3 , muramyl dipeptide claim 3 , alum claim 3 , a cytokine claim 3 , and a combination thereof.5. The method of claim 4 , wherein the lipid A is monophosphoryl lipid A or a synthetic lipid A.6. The method of claim 4 , wherein the cytokine is interleukin-2.7. The method of claim 2 , further comprising a step (c) evaluating the treated subject.8. The method of claim 7 , wherein evaluating the treated subject is performed: (i) before the period of time of step (b); (ii) during the period of time of step (b); (iii) after the period of time of step (b); or (iv) a combination thereof.9. The method of claim 7 , wherein evaluating the treated subject comprises measuring an immune reaction in the treated subject.10. The method of claim 9 , wherein measuring the immune reaction in the treated subject comprises measuring a T-cell proliferation.11. The method of claim 7 , wherein evaluating the treated subject comprises determining at ...

PROGRAMMABLE SELF-ASSEMBLED NANOSTRUCTURES BASED ON SIDECHAIN-MODIFIED PNA FOR THE MULTIVALENT DISPLAY OF LIGANDS

The invention concerns compositions comprising strands of polynucleotide and strands of PNA, each PNA strand comprising: (i) from 2 to 50 nucleobase subunits and (ii) one or more gamma substituents. The PNA strands are complementary to at least a portion of at least some of the polynucleotide strands, and the molar ratio of PNA strands to polynucleotide strands being at least 1:1. Certain gamma substituents are capable of effecting attachment of a PNA strand to a cell. The invention also concerns construction of nanostructure platforms and vaccines and use of the inventive compositions in inhibiting disease states in mammals. 1. A composition comprising:strands of polynucleotide and (i) from 2 to 50 nucleobase subunits; and', '(ii) one or more gamma substituents;, 'strands of PNA, each PNA strand comprisingthe PNA strands being complementary to at least a portion of at least some of the polynucleotide strands, andthe molar ratio of PNA strands to polynucleotide strands being at least 1:1.2. The composition of claim 1 , wherein said polynucleotide strands are DNA.3. The composition of claim 2 , wherein the DNA is single-stranded.4. The composition of claim 1 , wherein said polynucleotide strands are RNA.5. The composition of claim 4 , wherein the RNA is single-stranded.6. The composition of claim 1 , wherein the PNA strand comprises 2 claim 1 , 3 claim 1 , 4 claim 1 , 5 claim 1 , 6 claim 1 , 7 claim 1 , 8 claim 1 , 9 claim 1 , 10 claim 1 , 11 claim 1 , 12 claim 1 , 13 claim 1 , 14 claim 1 , 15 claim 1 , 16 claim 1 , 17 claim 1 , 18 claim 1 , 19 claim 1 , or 20 nucleobase subunits.7. The composition of claim 1 , wherein each nucleobase subunit comprises 1 claim 1 , 2 claim 1 , or 3 gamma substituents.8. The composition of claim 1 , wherein said PNA comprises a backbone having at least one cyclopentyl residue.9. The composition of claim 1 , wherein said gamma substituent is capable of binding to a protein on the surface of a cell.10. The composition of claim 9 , ...

FORMULATIONS OF MONOCLONAL ANTIBODIES

The present invention provides a formulation comprising: (i) a monoclonal antibody; and (ii) an ionic excipient; wherein the monoclonal antibody is present at a concentration of about 50 mg/ml or greater (e.g. about 50 mg/ml to about 200 mg/ml) and the ionic excipient is present at a concentration of about 50 to about 150 mM and the formulation has a pH of 5.5 to 6.5. 146-. (canceled)47. A formulation comprising:i. an anti-GM-CSFRα antibody; andii. an ionic excipient;wherein the anti-GM-CSFRα antibody has a pI in the range of pH 6.0 to pH 7.5 and the VH and VL sequences of CAM-3001, andwherein the anti-GM-CSFRα antibody is present at a concentration of about 50 mg/ml or greater and the ionic excipient is present at a concentration of about 50 to about 150 mM and the formulation has a pH of 5.5 to 7.5.48. The formulation of claim 47 , wherein the aggregation rate of the monoclonal antibody in the formulation is reduced compared to the aggregation rate of the same antibody in the same formulation but without an ionic excipient.49. The formulation of claim 47 , wherein the anti-GM-CSFRα antibody has a pI in the range of pH 6.4 to pH 7.5.50. The formulation of claim 47 , wherein the anti-GM-CSFRα antibody is an IgG4 monoclonal antibody.51. The formulation of claim 47 , wherein the anti-GM-CSFRα antibody is present in the formulation at a concentration of about 100 mg/ml to about 200 mg/ml.52. The formulation of claim 51 , wherein the monoclonal antibody is present in the formulation at a concentration of about 100 mg/ml or of about 150 mg/ml.53. The formulation of claim 47 , wherein the formulation has a pH in the range of about pH 5.5 to about pH 6.5.54. The formulation of claim 53 , wherein the formulation has a pH of about pH 5.8.55. The formulation of claim 47 , wherein the ionic excipient is a salt claim 47 , optionally claim 47 , wherein the salt is NaCl claim 47 , arginine hydrochloride claim 47 , or lysine hydrochloride.56. The formulation of claim 47 , wherein ...

PD-L1 ANTIBODY PHARMACEUTICAL COMPOSITION AND USE THEREOF

The present invention provides a PD-L1 antibody pharmaceutical composition and use thereof. In particular, the present invention provides a pharmaceutical composition comprising the PD-L1 antibody or an antigen-binding fragment thereof in a succinate buffer. In addition, the pharmaceutical composition may also contain a sugar and a nonionic surfactant. 1. A pharmaceutical composition , comprising an anti-PD-L1 antibody or antigen-binding fragment thereof , and a buffer; wherein the buffer is preferably a succinate buffer or an acetate buffer , more preferably a succinate buffer.2. The pharmaceutical composition according to claim 1 , the pH of the pharmaceutical composition is about 4.5 to 6.0 claim 1 , preferably about 5.0 to 6.0 claim 1 , more preferably about 5.0 to 5.5 claim 1 , most preferably 5.2.3. The pharmaceutical composition according to or claim 1 , wherein the concentration of the buffer is about 5 mM to 50 mM claim 1 , preferably about 10 mM to 30 mM claim 1 , more preferably 10 mM to 20 mM claim 1 , most preferably 20 mM.4. The pharmaceutical composition according to any one of to claim 1 , wherein the concentration of the antibody is about 30 mg/mL to about 80 mg/mL claim 1 , preferably about 40 mg/mL to 60 mg/mL claim 1 , more preferably about 45 mg/mL to 55 mg/mL claim 1 , most preferably 50 mg/mL.5. The pharmaceutical composition according to any one of to claim 1 , further comprising a saccharide; the saccharide is preferably disaccharide claim 1 , more preferably trehalose or sucrose claim 1 , most preferably sucrose.6. The pharmaceutical composition according to claim 5 , wherein the concentration of the saccharide is about 30 mg/mL to 90 mg/mL claim 5 , preferably about 40 mg/mL to 80 mg/mL claim 5 , more preferably 55 mg/mL to 65 mg/mL claim 5 , most preferably 60 mg/mL.7. The pharmaceutical composition according to any one of to claim 5 , further comprising a surfactant; the surfactant is preferably polysorbate claim 5 , more preferably ...

WIREFRAME NANOSTRUCTURES

The present invention generally relates to nanotechnology and, in particular, to wireframe nanostructures which may be formed from nucleic acids. In various aspects, the invention relates to molecular structures having a plurality of vertices and pathways connecting the vertices, which may be formed from nucleic acids, including bundles or tubes of nucleic acids. Such molecular structures may form shapes such as icosahedrons, octahedrons, tetrahedrons, or other polyhedra, which may define an interior space. The interior space may be used, for example, to contain a molecule for further study, or to contain a molecule for drug delivery purposes. In some cases, the molecular structure may be stabilized using relatively short nucleic acid strands that interact with two or more nucleic acid portions within the structure, thereby substantially immobilizing the portions relative to each other. Other aspects of the invention relate to techniques for forming such molecular structures, techniques for using such molecular structures, techniques of promoting such molecular structures, kits involving such molecular structures, and the like. 1118-. (canceled)119. A composition , comprising:a solution, comprising a plurality of substantially identical molecular structures, each molecular structure defining a plurality of vertices and pathways forming a polyhedral structure defining a hollow three-dimensional interior space, the vertices each having at least three pathways emanating therefrom, each pathway connecting two vertices, wherein each pathway connecting two vertices comprises a nanotube comprising a plurality of nucleic acids, wherein the molecular structure has a smallest dimension in any direction that is at least about 100 nm.120. The composition of claim 119 , wherein the molecular structure is substantially rigid.121. The composition of claim 119 , wherein at least one of the nucleic acids has a length of at least about 500 nucleotides.122. The composition of claim ...

METHODS FOR FORMING POLYPLEXES

The present disclosure relates method for forming polyplexes, which find use in gene therapy applications as safe and non-toxic nucleic acid transfection agents. 1. A method for making one or more polyplexes , the method comprising: i. a polymer in a first liquid stream;', 'ii. a nucleic acid component in a second liquid stream;, '(a) providing(b) contacting the polymer in the first liquid stream with the nucleic acid component in the second liquid stream to form a polyplex having a size and charge that is suitable for therapeutic administration; and(c) isolating the polyplex to provide a stabilized polyplex.2. The method of claim 1 , wherein the isolating comprises conveying the polyplex in a liquid channel for a residence time sufficient to stabilize the polyplex.3. The method of any one of the preceding claims claim 1 , further comprising assessing and harvesting one or more polyplexes.4. The method of any one of the preceding claims claim 1 , wherein the first liquid stream and first liquid streams are solutions.5. The method of any one of the preceding claims claim 1 , further comprising flowing the first liquid stream and the second liquid stream through a flow-regulating device at a rate that provides a polyplex having a size and charge that is suitable for transdermal administration.6. The method of claim 5 , wherein flow-regulating device is selected from the group consisting of a positive displacement pump claim 5 , a syringe driven pump claim 5 , a pressure driven pump claim 5 , and a gravity feed pump.7. The method of any one of the preceding claims claim 5 , wherein the contacting step uses a nozzle claim 5 , a micro fluidics mixing device claim 5 , a touch tube claim 5 , a liquid bridge claim 5 , a vertical mixer claim 5 , a rotating double tube claim 5 , or an atomizer.8. The method any one of the preceding claims claim 5 , wherein the contacting step occurs in an air gap or in carrier fluid within the liquid channel.9. The method of any one of the ...

POLYMERIC ARTIFICIAL TEAR SYSTEM

The present invention relates to artificial tear formulations and ophthalmic formulations suitable for drug delivery. The formulations comprise galactomannans such as guar or hydroxypropyl guar and a borate source such as boric acid. The formulations further comprise a cis-diol such as sorbitol that interferes with the cross-linking of galactomannan and borate. Optionally, the formulations are substantially free of divalent cations. 1. An ophthalmic formulation comprising a galactomannan , borate , and a cis-diol , wherein said formulation is substantially free of divalent cations.2. A formulation according to wherein said galactomannan is present at a concentration of about 0.1 w/v % to about 2.0 w/v % and said borate is present at a concentration of about 0.2 w/v % to about 2.0 w/v %.3. A formulation according to wherein said galactomannan is present at a concentration of about 0.16 w/v % to about 0.19 w/v % and said borate is present at a concentration of about 0.7 w/v %.4. A formulation according to wherein said galactomannan is selected from the group consisting of:guar, hydroxylpropyl guar, and combinations thereof.5. A formulation according to wherein said cis-diol is selected from the group consisting of sorbitol claim 1 , mannitol claim 1 , polyethylene glycols claim 1 , polypropylene glycols claim 1 , polyethyleneoxide-polybutyleneoxide block copolymers claim 1 , and combinations thereof.6. A formulation according to wherein said cis-diol is sorbitol or mannitol.7. A formulation according to wherein said cis-diol is present at a concentration of about 1.4 w/v %.8. A formulation according to wherein said borate is boric acid.9. A formulation according to further comprising a demulcent selected from the group consisting of:glycerin, polyvinyl pyrrolidone, polyethylene oxide, polyethylene glycol, propylene glycol, polyacrylic acid, and combinations thereof.10. A formulation according to wherein said demulcent is polypropylene glycol or polyethylene glycol.11. ...

Stannous Fluoride Sugar Alcohol Solid Solutions

Stannous fluoride polyol solid solutions combine three complimentary, biochemical mechanisms attributed to Sn, F and Polyol, respectively to reduce growth and metabolism of while effecting superior Bioactivity Quotients. The stannous fluoride polyol solid solution particulate compositions of the present invention comprise: 1. Stannous fluoride polyol solid solution particulate compositions comprising:(a) stannous fluoride at between about 0.01 and about 0.8% by weight;(b) a polyol at between about 0.1 and about 30% by weight, wherein the polyol is selected from the group consisting of erythritol, xylitol, isomalt, maltitol, sorbitol, and combinations thereof;(c) an astringency neutralizer at between about 0.01 and about 0.4% by weight, where the ratio of astringency neutralizer to stannous fluoride is from between about 0.01 and about 0.2;(d) a mucoadhesive at between about 1.5 and about 70% by weight, wherein the ratio of mucoadhesive to stannous fluoride polyol is from between about 7 to 1 and about 25 to 1;(e) a pH stabilizer, selected from the group consisting of malic, fumaric, citric acid and combinations thereof, wherein the ratio of pH stabilizer to stannous fluoride polyol is from between about 0.03 and 5 and preferably from between about 0.1 and about 3; and(f) optional flavorants, stabilizers, preservatives, conditioners, and oral care adjuncts.2Streptococcus mutans. The stannous fluoride polyol solid solution particulates of claim 1 , further suspended in an oral care composition selected from the group consisting of toothpastes claim 1 , brushing gels claim 1 , prophy pastes claim 1 , varnishes claim 1 , muco-adherent films claim 1 , and combinations thereof claim 1 , which reduce growth and metabolism of claim 1 , growth and metabolism of organisms claim 1 , resulting in the curing or mitigation of microbial or viral infections producing thrush claim 1 , periodontitis claim 1 , canker sores claim 1 , and other oral diseases.3. The stannous fluoride ...

HIGHLY SOLUBLE STEVIA SWEETENER

A method for making highly soluble sweetener compositions is described. The resulting sweetener compositions readily provide high concentration solutions, and also possess superior taste qualities. The compositions can be used as sweeteners, sweetness enhancers, and flavor enhancers in foods, beverages, cosmetics and pharmaceuticals. 1Stevia. A method for producing a high solubility sweetener comprising the steps of:{'i': 'Stevia', 'A) providing a first sweetener;'}{'i': Stevia', 'Stevia, 'B) providing a second sweetener that is different from the first sweetener;'}C) providing water;{'i': 'Stevia', 'D) mixing the water and first and second sweeteners to make a mixture;'}E) increasing the temperature of the mixture by a gradient method to make a solution;F) holding the solution at an elevated temperature;{'i': 'Stevia', 'G) decreasing the temperature of the solution by a gradient method to obtain a high stability and high concentration sweetener solution; and'}{'i': Stevia', 'Stevia, 'H) spray drying the high stability and high concentration sweetener solution, to provide the high solubility sweetener.'}2Stevia. The method of wherein the first sweetener is selected from the group consisting of Stevioside claim 1 , Rebaudioside A claim 1 , Rebaudioside B claim 1 , Rebaudioside C claim 1 , Rebaudioside D claim 1 , Rebaudioside E claim 1 , Rebaudioside F claim 1 , Steviolbioside claim 1 , Dulcoside A claim 1 , Rubusoside claim 1 , or other glycoside of steviol claim 1 , and a mixture thereof.3Stevia. The method of wherein the second sweetener is selected from the group consisting of: Stevioside claim 1 , Rebaudioside A claim 1 , Rebaudioside B claim 1 , Rebaudioside C claim 1 , Rebaudioside D claim 1 , Rebaudioside E claim 1 , Rebaudioside F claim 1 , Steviolbioside claim 1 , Dulcoside A claim 1 , Rubusoside claim 1 , or other glycoside of steviol claim 1 , and a mixture thereof.4Stevia. The method of wherein a ratio of the first and second sweeteners is about 99:1 to ...

STABLE FORMULATION OF AZACITIDINE OR SALTS THEREOF AND THEIR PROCESS FOR PREPARATION

The present invention relates to a stable pharmaceutical composition comprising azacitidine or its pharmaceutically acceptable salts, one or more sugar alcohols and one or more pharmaceutically acceptable excipients, wherein said composition is suitable for parenteral administration. The invention also relates to processes for preparing the preparation of such reconstitutable formulations. The invention also relates to therapeutic methods of use of such formulations and to use of such formulations in the manufacture of medicaments. 1. A stable pharmaceutical composition comprising azacitidine or its pharmaceutically acceptable salts , one or more sugar alcohols and one or more pharmaceutically acceptable excipients , wherein said composition is suitable for parenteral administration.2. The stable pharmaceutical composition of claim 1 , wherein said composition is not lyophilized.3. The stable pharmaceutical composition of claim 1 , wherein said composition is a reconstitutable formulation.4. The stable pharmaceutical composition of claim 1 , wherein the sugar alcohol comprises one or more of sorbitol claim 1 , mannitol claim 1 , glycerol claim 1 , allitol claim 1 , talitol claim 1 , glucitol claim 1 , iditol claim 1 , dulcitol claim 1 , xylitol claim 1 , adonitol claim 1 , ribitol claim 1 , arabitol claim 1 , erythritol claim 1 , threitol claim 1 , glycerol claim 1 , and inositol.5. The stable pharmaceutical composition of claim 4 , wherein the sugar alcohol is mannitol.6. The stable pharmaceutical composition of claim 5 , wherein the mannitol is present in an amount of about 0.1% weight to about 60% weight of the composition.7. A kit comprising a stable reconstitutable pharmaceutical composition suitable for parenteral administration comprising azacitidine or its pharmaceutically acceptable salts claim 5 , one or more sugar alcohols and one or more pharmaceutically acceptable excipients claim 5 , and a reconstitution vehicle.8. The kit of claim 7 , wherein the kit ...

FORMULATIONS OF (S)-3-(4-((4-(MORPHOLINOMETHYL)BENZYL)OXY)-1-OXOISOINDOLIN-2-YL)PIPERIDINE-2,6-DIONE

Pharmaceutical compositions and single unit dosage forms of (S)-3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, or a pharmaceutically acceptable stereoisomer, prodrug, salt, solvate, hydrate, or clathrate, are provided herein. Also provided are methods of treating, managing, or preventing various disorders, such as cancer, an inflammatory disease and/or an immune-related disorder. 1. An oral dosage form in the form of a capsule which comprises: 1) Compound A , or a pharmaceutically acceptable prodrug , salt , solvate , hydrate , clathrate , stereoisomer , tautomer , or racemic mixtures thereof , at an amount of about 0.1 to about 3 weight percent of the total weight of the dosage form; 2) a carrier or excipient at an amount of about 90 to 99.9 weight percent of total weight of the oral dosage form , wherein the carrier or excipient is starch , lactose or a mixture thereof.2. The oral dosage form of claim 1 , wherein Compound A is present at an amount of about 0.1 to about 1 weight percent of total weight of the dosage form.3. The oral dosage form of claim 1 , wherein the carrier or excipient is present at an amount of about 95 to about 99.9 weight percent of total weight of the dosage form.4. The oral dosage form of claim 1 , wherein the carrier or excipient is a mixture of starch and lactose.5. The oral dosage form of claim 4 , wherein the starch is pregelatinized starch.6. The oral dosage form of claim 4 , wherein the lactose is anhydrous lactose.7. The oral dosage form of further comprising a lubricant at an amount of 0.01 to 1 weight percent of total weight of the oral dosage form8. The oral dosage form of claim 7 , wherein the lubricant is present at an amount of 0.1 to 0.5 weight percent of total weight of the dosage form.9. The oral dosage form of claim 7 , wherein the lubricant is stearic acid.10. An oral dosage form which weighs about 75 mg and comprises: 1) Compound A claim 7 , or a pharmaceutically acceptable prodrug ...

PHARMACEUTICAL FORMS OF DIAZABICYCLOOCTANE DERIVATIVES AND PROCESS FOR PRODUCING THE SAME

The present invention relates to a pharmaceutical composition and a lyophilisate of a diazabicyclooctane derivative represented by Compound I, a process for producing the same and methods for using the same. 2. The pharmaceutical composition of claim 1 , wherein the ratio of Compound (I) and the bulking agent is 3:1 (mg/mL).3. The pharmaceutical composition of claim 1 , wherein the ratio of Compound (I) and the bulking agent is 2:1 (mg/mL).4. The pharmaceutical composition of claim 1 , wherein the ratio of Compound (I) and the bulking agent is 1:1 (mg/mL).5. The pharmaceutical composition of claim 1 , wherein the bulking agent is sucrose claim 1 , trehalose claim 1 , dehydrate or mannitol.7. The process of claim 6 , wherein the ratio of Compound (I) and the bulking agent is 3:1 (mg/mL).8. The process of claim 6 , wherein the ratio of Compound (I) and the bulking agent is 2:1 (mg/mL).9. The process of claim 6 , wherein the ratio of Compound (I) and the bulking agent is 1:1 (mg/mL).10. The process according to claim 6 , wherein the freezing step is at a temperature of at least −30° C.±5° C. or colder.11. The process according to claim 7 , wherein the freezing step is at a temperature of −40° C.±5° C.12. The process according to claim 6 , wherein the pressure is reduced to 30 mTorr after the freezing step.13. The process according to claim 6 , wherein the first drying step is increased to a temperature of at least −25° C.±5° C. or warmer.14. The process according to claim 6 , wherein the second drying step is increased to a temperature of at least 10° C.±5° C. or warmer.15. The process according to claim 6 , wherein the bulking agent is sucrose claim 6 , trehalose dehydrate or mannitol.17. The method according to claim 17 , wherein the ratio of Compound (I) and the bulking agent is between 1:1 to 3:1 (mg/mL).18. The method according to claim 17 , wherein the ratio of Compound (I) and the bulking agent is 2:1 (mg/mL).19. The method according to for treating a bacterial ...

PHARMACEUTICAL COMPOSITIONS CONTAINING ANTI-LINGO-1 ANTIBODIES

Pharmaceutical compositions containing anti-LINGO-1 antibodies or LINGO-1-binding fragments thereof are provided. These pharmaceutical compositions find use in the treatment of CNS demyelinating diseases, such as multiple sclerosis and optic neuritis (e.g., acute optic neuritis). 1. A pharmaceutical composition comprising an anti-LINGO-1 antibody or LINGO-1-binding fragment thereof , histidine , and at least one excipient selected from the group consisting of proline and methionine , wherein the anti-LINGO-1 antibody or LINGO-1-binding fragment comprises an immunoglobulin heavy chain variable domain (VH) and an immunoglobulin light chain variable domain (VL) , the VH and VL , respectively , comprising: VH-CDR1 comprises the amino acid sequence set forth in SEQ ID NO:6;', 'VH-CDR2 comprises the amino acid sequence set forth in SEQ ID NO:7; and', 'VH-CDR3 comprises the amino acid sequence set forth in SEQ ID NO:8; and, '(a) VH complementarity determining regions (CDRs), wherein'} VL-CDR1 comprises the amino acid sequence set forth in SEQ ID NO:14;', 'VL-CDR2 comprises the amino acid sequence set forth in SEQ ID NO:15; and', 'VL-CDR3 comprises the amino acid sequence set forth in SEQ ID NO:16, and, '(b) VL CDRs, wherein'}wherein the composition has a pH of about 6.0 to about 7.0.2. The pharmaceutical composition of claim 1 , wherein the composition further comprises arginine hydrochloride.3. The pharmaceutical composition of claim 2 , wherein the composition comprises arginine hydrochloride at a concentration of about 70 mM to about 170 mM.4. The pharmaceutical composition of any one of to claim 2 , wherein the composition comprises the anti-LINGO-1 antibody or LINGO-1-binding fragment at a concentration of 50 mg/ml to 300 mg/ml.5. The pharmaceutical composition of any one of to claim 2 , wherein the composition comprises the anti-LINGO-1 antibody or LINGO-1-binding fragment at a concentration of 100 mg/ml to 250 mg/ml.6. The pharmaceutical composition of any one of to ...

STABLE FORMULATIONS OF POLYPEPTIDES AND USES THEREOF

Formulations are provided that contain single variable domains with a good solubility and good stability under different storage, transportation and stress conditions. The formulations are useful as pharmaceutical formulation. The formulation comprises an aqueous carrier with a pH of 5.5 to 8.0, a buffer selected from the group consisting of histidine pH 6.0-6.5, hepes pH 7.0-8.0, MES pH 6.0, succinate pH 6.0-6.5 and acetate pH 5.5-6.0; an excipient; and/or a surfactant selected from Tween 80, Tween 20 and poloxamers. The formulation is further characterized that it has an inorganic salt concentration of 150 mM or lower. 1. A formulation comprising an aqueous carrier having a pH of 5.5 to 8.0 and a polypeptide comprising one or more single variable domains at a concentration of 1 mg/mL to 200 mg/mL , said formulation being formulated for administration to a human subject and said formulation further comprising one or more components selected from:a) A buffer at a concentration of 10 mM to 100 mM selected from the group consisting of histidine pH 6.0-6.5, hepes pH 7.0-8.0, MES pH 6.0, succinate pH 6.0-6.5 and acetate pH 5.5-6.0;b) An excipient at a concentration of 1% to 20%;c) A surfactant at a concentration of 0.001% to 1% selected from Tween 80, Tween 20 or a poloxamer;wherein said formulation has an inorganic salt concentration of 150 mM or lower.2. The formulation of claim 1 , that does not contain any inorganic salt.3. The formulation of claim 1 , wherein the concentration of polypeptide is about 1 to 200 mg/ml or more claim 1 , preferably about 5 to 100 mg/mL or more claim 1 , more preferably about 5 to 50 mg/mL or more claim 1 , most preferably about 5 to 30 mg/mL or more claim 1 , such as around 5 mg/mL claim 1 , around 10 mg/mL claim 1 , around 20 mg/mL claim 1 , around 30 mg/mL claim 1 , around 40 mg/mL claim 1 , around 50 mg/mL claim 1 , around 60 mg/mL claim 1 , around 70 mg/mL claim 1 , around 80 mg/mL claim 1 , around 90 mg/mL claim 1 , around 100 mg/ ...

Formulation Including a Combination of beta-Endorphin and Adrenocorticotropic Hormone

The present specification provides compositions of β-endorphin and adrenocorticotropic hormone (ACTH). These compositions are useful in methods of treating disease. 1. A method of treating an inflammatory , autoimmune , allergic , infectious or neurologic disease or disorder comprising administering a clinically effective amount of adrenocorticotropic hormone (ACTH) and β-endorphin , or analogues thereof of either or both , to a person in need thereof.2. The method of claim 1 , wherein treating comprises resolving an acute exacerbation of the disease.3. The method of claim 1 , wherein treating comprises maintenance therapy claim 1 , whereby incidences or severity of exacerbations of the disease is reduced.4. The method of claim 3 , wherein the disease in relapsing-remitting multiple sclerosis and the incidence or severity of relapses is reduced.5. The method of claim 1 , wherein the person in need thereof has a family history of multiple sclerosis claim 1 , and the treatment is prophylactic.6. The method of comprising administering 40-120 units of ACTH.7. The method of claim 6 , wherein the mass ratio of ACTH:β-endorphin is 2:1.8. The method of comprising administering 0.8-1.2 mg of ACTH.9. The method of claim 8 , wherein the mass ratio of ACTH:β-endorphin is 2:1. This application is a continuation-in-part of PCT/US2020/022473, filed Mar. 12, 2020, which claims the benefit of U.S. Provisional Patent Application Nos. 62/818,034, filed Mar. 13, 2019 and 62/981,379, filed Feb. 25, 2020, each of which is incorporated herein by reference in their entirety.The present disclosure is directed to co-formulations of β-endorphin and adrenocorticotropic hormone (ACTH) as well as their use in methods of treating mammalian disease.Extracts from animal pituitary glands have been used since the 1950s to treat numerous disease indications including multiple sclerosis, systemic lupus erythematosus, proteinuria in nephrotic syndrome, polymyositis, symptomatic sarcoidosis, psoriatic ...

Use of Anti-MCAM Antibodies for Treatment or Prophylaxis of Giant Cell Arteritis, Polymyalgia Rheumatica or Takayasus Arteritis

The invention provides anti-MCAM antibodies that inhibit the ability of human MCAM to bind a laminin alpha-4 chain and pharmaceutical compositions and pharmaceutical formulations incorporating the same for use in treatment or prophylaxis of giant cell arteritis, polymyalgia rheumatica (PMR) or Takayasu's arteritis, methods of generating such antibodies, and their use in the manufacture of medicaments for treatment of neuroinflammatory disease, autoimmune disease, or cancer. 14-. (canceled)5. The method of claim 77 , wherein the mature heavy chain variable region is at least 90% identical to SEQ ID NO:161 claim 77 , and the mature light chain variable region is at least 90% identical to SEQ ID NO:123.6. The method of claim 77 , wherein the mature heavy chain variable region is at least 95% identical to SEQ ID NO:161 and the mature light chain variable region is at least 95% identical to SEQ ID NO:123.7. The method of claim 77 , wherein the mature heavy chain variable region is at least 98% identical to SEQ ID NO:161 and the mature light chain variable region is at least 95% identical to SEQ ID NO:123.8. The method of claim 77 , wherein the mature heavy chain variable region is at least 99% identical to SEQ ID NO:161 and the mature light chain variable region is at least 95% identical to SEQ ID NO:123.9. The method of claim 77 , wherein the mature heavy chain variable region has the amino acid sequence of SEQ ID NO:157 claim 77 , SEQ ID NO:158 claim 77 , SEQ ID NO:159 claim 77 , SEQ ID NO:160 claim 77 , or SEQ ID NO:161 claim 77 , and wherein the mature light chain variable region is at least 95% identical to SEQ ID NO:123.10. The method of claim 77 , wherein the mature heavy chain variable region is at least 95% identical to SEQ ID NO:161 and the mature light chain variable region is at least 98% identical to SEQ ID NO:123.11. The method of claim 77 , wherein the mature heavy chain variable region is at least 95% identical to SEQ ID NO:161 and the mature light chain ...

BOLAAMPHIPHILIC COMPOUNDS, COMPOSITIONS AND USES THEREOF

Bolaamphiphilic compounds are provided according to formula I: 1. A pharmaceutical composition comprising a bolaamphiphile complex; wherein the bolaamphiphile complex comprises one or more bolaamphiphilic compounds according to formula I:{'br': None, 'sup': 2', '1', '1, 'HG-L-HG\u2003\u2003I'}or a pharmaceutically acceptable salt, solvate, hydrate, prodrug, stereoisomer, tautomer, isotopic variant, or N-oxide thereof, or a combination thereof;{'sup': 1', '2', '1, 'sub': 1', '20, 'wherein: each HGand HGis independently a hydrophilic head group, and wherein Lis alkylene, alkenyl, heteroalkylene, or heteroalkenyl linker; unsubstituted or substituted with C-Calkyl, hydroxyl, or oxo; and'}a pharmaceutically acceptable carrier.2. (canceled)3. (canceled)4. (canceled)5. The pharmaceutical composition according to claim 1 , wherein{'sup': '1', 'sub': 1', '20, 'Lis heteroalkylene, or heteroalkenyl linker comprising C, N, and O atoms; unsubstituted or substituted with C-Calkyl, hydroxyl, or oxo.'}6. The method or the pharmaceutical composition according to claim 1 , wherein{'sup': '1', 'sub': 2', 'n1', '2', 'n2', '2', 'n3, 'Lis —O—(CH)—O—C(O)—(CH)—C(O)—O—(CH)—O—.'}7. The pharmaceutical composition according to claim 1 , wherein{'sup': '1', 'claim-text': [{'br': None, 'sup': 2', '3, 'sub': 2', 'n4, '—O-L-C(O)—O—(CH)—O—C(O)-L-O—,'}, {'br': None, 'or'}, {'br': None, 'sup': '2', 'sub': 2', 'n5', '2', 'n6, '—O-L-C(O)—O—(CH)—O—(O)—(CH)—,'}], 'Lis'}{'sup': 2', '3, 'sub': 4', '20', '1', '8, 'and wherein each Land Lis C-Calkylene or alkenyl linker; unsubstituted or substituted with C-Calkyl or hydroxy;'}and n4, n5, and n6 is independently an integer from 4-20.8. The pharmaceutical composition according to claim 7 , wherein each Land Lis independently —C(R)—C(OH)—CH—(CH═CH)—(CH)—; Ris C-Calkyl claim 7 , and n7 is independently an integer from 4-20.11. (canceled)12. (canceled)13. (canceled)14. The pharmaceutical composition according to claim 10 , wherein the bolaamphiphilic compound is ...

SUBSTITUTED ANIONIC COMPOUNDS CONSISTING OF A BACKBONE MADE UP OF A DISCRETE NUMBER OF SACCHARIDE UNITS

The invention relates to substituted anionic compounds consisting of a backbone made up of a discrete number u of between 1 and 8 (1≦u≦8) of identical or different saccharide units, linked via identical or different glycosidic bonds, said saccharide units being chosen from the group consisting of pentoses, hexoses, uronic acids, N-acetylhexosamines in cyclic form or in open reduced form, which are randomly substituted. It also relates to the process for the preparation thereof and to the pharmaceutical compositions comprising same. 1. Substituted anionic compounds , in isolated form or as a mixture , consisting of a backbone made up of a discrete number u of between 1 and 8 (1≦u≦8) of identical or different saccharide units , linked via identical or different glycosidic bonds , said saccharide units being chosen from the group consisting of pentoses , hexoses , uronic acids , N-acetylhexosamines in cyclic form or in open reduced form , wherein they are substituted with: {'br': None, 'sub': 1', 'a', '2', 'n', 'm, '—[R]—[[Q]-[R]]\u2003\u2003Formula I'}, 'a) at least one substituent of general formula Ithe substituents being identical or different when there are at least two substituents, in which:{'sub': 3', '15', '1, 'if n is equal to 0, then the radical -[Q]- is derived from a Cto Ccarbon-based chain which is optionally branched or substituted, optionally unsaturated and/or optionally comprising one or more ring(s) and/or comprising at least one heteroatom chosen from O, N and S and at least one function L chosen from amine and alcohol functions, said radicals -[Q]- being attached to the backbone of the compound by means of a linker arm Rto which it is bonded via a function T, or directly bonded to the backbone via a function G,'}{'sub': 2', '15', '2', '1, 'if n is equal to 1 or 2, then the radical -[Q]- is derived from a Cto Ccarbon-based chain which is optionally branched or substituted, optionally unsaturated and/or optionally comprising one or more ring(s) and/ ...

Stable, Aqueous Antibody Formulations

The present invention relates to stable, aqueous antibody formulations. In some embodiments, the stable, aqueous formulations comprise about 2 mg/mL to about 100 mg/mL of an anti-IL5R antibody, and about 0.002% to about 0.01% polysorbate-20. Also provided are methods of making and methods of using such antibody formulations. 1. A stable , aqueous antibody formulation comprising:a. about 2 mg/mL to about 100 mg/mL of an antibody, wherein the antibody comprises a heavy chain variable region and a light chain variable region, wherein the heavy chain variable region comprises the Kabat-defined CDR1, CDR2, and CDR3 sequences of SEQ ID NOs: 5-7, and wherein the light chain variable region comprises the Kabat-defined CDR1, CDR2, and CDR3 sequences of SEQ ID NOs: 8-10, andb. about 0.002% to about 0.01% polysorbate-20.2. The antibody formulation of claim 1 , further comprising an uncharged excipient.3. The antibody formulation of claim 2 , wherein the uncharged excipient is trehalose.4. (canceled)5. The antibody formulation of claim 1 , comprising about 20 to about 100 mg/ml of the antibody.6. (canceled)7. The antibody formulation of claim 5 , wherein the uncharged excipient concentration is about 200 mM to about 400 mM.8. (canceled)9. (canceled)10. (canceled)11. (canceled)12. The antibody formulation of claim 1 , further comprising histidine.13. The antibody formulation of claim 12 , wherein the histidine concentration is about 15 mM to about 30 mM.14. (canceled)15. (canceled)16. (canceled)17. (canceled)18. (canceled)19. (canceled)20. (canceled)21. The antibody formulation of claim 1 , wherein the formulation is stable upon storage at about 25° C. for at least 3 months.22. (canceled)23. (canceled)24. (canceled)25. (canceled)26. (canceled)27. (canceled)28. (canceled)29. The antibody formulation of claim 1 , wherein the formulation is substantially free from particles upon storage at about 40° C. for at least 1 month as determined by visual inspection.30. (canceled)31. The ...

MANUFACTURE OF RECOMBINANT CLOSTRIDIUM BOTULINUM NEUROTOXINS

The invention provides methods for producing soluble di-chain BoNT/A protein. 1. A method for producing soluble di-chain BoNT/A protein , said method comprising:a) providing a soluble single-chain BoNT/A protein;b) contacting said BoNT/A protein with endoproteinase Lys-C(Lys-C) in solution; andc) separating the soluble BoNT/A protein from the Lys-C by contacting the solution containing soluble BoNT/A protein and Lys-C with a hydrophobic surface, wherein the soluble BoNT/A protein binds with preference to the hydrophobic surface.2. The method according to claim 1 , wherein the soluble single-chain BoNT/A protein is produced (i) in a host cell claim 1 , by expressing a nucleic acid encoding said single-chain BoNT/A protein in an expression system; or (ii) in an in vitro expression system.3. The method according to claim 2 , wherein the host cell is a bacterial host cell and the expression system is a bacterial expression system.4E. coliE. coli. The method according to claim 3 , wherein the bacterial expression system is an expression system and the host cell is an cell.5. The method according to claim 2 , wherein said soluble single-chain BoNT/A protein is expressed in the cytoplasm of said host cell.6. The method according to claim 2 , wherein said soluble single-chain BoNT/A protein is expressed at a level of at least 5 mg/L.7E. coliE. coli. The method according to claim 2 , comprising lysis of the bacterial or host cell to provide a bacterial or host cell homogenate containing said soluble single-chain BoNT/A protein.8. The method according to claim 1 , wherein the hydrophobic surface is an inert matrix to which a ligand consisting of aryl or alkyl groups is attached.9. The method according to claim 8 , wherein the ligand is selected from the group consisting of: butyl claim 8 , phenyl and octyl ligands.10. The method according to claim 9 , wherein a high performance hydrophobic surface is used.11. A composition comprising an active di-chain BoNT/A protein made by ...

METHODS OF ADMINISTERING BONE MORPHOGENETIC PROTEIN COMPOSITIONS

The present invention relates to compositions of bone morphogenetic proteins, particularly solid and liquid formulations of such proteins comprising one or more stabilizing excipients. The invention further provides methods of producing the compositions, kits comprising the compositions and methods of using the compositions in the treatment of diseases of skeletal and non-skeletal tissues. 1. A preparation of bone morphogenetic protein comprising: an aqueous carrier; and , bone morphogenetic protein solubilized in said carrier at a concentration of at least about 10 mg/ml.2. The protein preparation of claim 1 , further comprising a stabilizing excipient.3. The protein preparation of claim 2 , wherein the stabilizing excipient is selected from the group consisting of: sugars claim 2 , polyols claim 2 , surfactants claim 2 , and any combination thereof.4. The protein preparation of claim 3 , wherein the stabilizing excipient is selected from the group consisting of glucose claim 3 , sucrose claim 3 , raffinose claim 3 , trehalose claim 3 , lactose claim 3 , mannitol claim 3 , sorbitol claim 3 , Tween 80 claim 3 , Tween 20 and Pluronic F-68 and combinations thereof5. The protein preparation of claim 4 , wherein the stabilizing excipient is trehalose.6. The protein preparation of claim 5 , having a pH of from about 2.5 to about 3.5.7. The protein preparation of claim 5 , wherein the aqueous carrier comprises a buffer of the single acidic group type selected from the group consisting of: potassium phosphate claim 5 , proprionic acid claim 5 , lactic acid claim 5 , trifluoroacetic acid and acetic acid; or the two acidic group type selected from the group consisting of: sodium glutamate and sodium succinate.8. The protein preparation of claim 5 , wherein the protein is selected from the group consisting of BMP-2 claim 5 , BMP-4 claim 5 , BMP-5 claim 5 , BMP-6 claim 5 , BMP-7 claim 5 , GDF-5 claim 5 , GDF-6 claim 5 , GDF-7 claim 5 , and sequence variants of any one of the ...

Rapid Setting High Strength Calcium Phosphate Cements Comprising Cyclodextrins

Rapid setting high strength calcium phosphate cements and methods of using the same are provided. Aspects of the cements include fine and coarse calcium phosphate particulate reactants and a cyclodextrin which, upon combination with a setting fluid, produce a flowable composition that rapidly sets into a high strength product. The flowable compositions find use in a variety of different applications, including the repair of hard tissue defects, e.g., bone defects such as fractures. 1. A method of producing a flowable composition that sets into a calcium phosphate containing product , the method comprising:combining: (i) a first particulate calcium phosphate reactant having a mean particle size of 8 μm or less; and', '(ii) a second calcium phosphate reactant having a mean particle size of 10 μm or greater;, '(a) a dry reactant component comprising(b) a cyclodextrin; and(c) a setting fluid;in a ratio sufficient to produce the flowable composition that sets into a calcium phosphate containing product.2. The method according to claim 1 , wherein the ratio of the first to second particulate calcium phosphate reactants in the dry reactant component ranges from 1 to 10.3. The method according to claim 2 , wherein the first and second particulate calcium phosphate reactants are tricalcium phosphate.4. The method according to claim 1 , wherein the first particulate calcium phosphate reactant has a mean particle size of 4 μm.5. The method according to claim 1 , wherein the cyclodextrin is present in the setting fluid.6. The method according to claim 1 , wherein the cyclodextrin is present in the dry reactant component.7. The method according to claim 6 , wherein the cyclodextrin is present in the dry reactant component in an amount ranging from 0.01 to 10 wt %.8. The method according to claim 1 , wherein the cyclodextrin is α-cyclodextrin.9. The method according to claim 1 , wherein the flowable composition has a 4-minute setting strength of 1000 N or greater.10. The method ...

PHARMACEUTICAL FORMULATIONS OF HER2 ANTIBODY-DRUG CONJUGATE

The invention relates to a pharmaceutical formulation comprising a mixture of a non-reducing sugar, a recombinant humanized anti-Her2 monoclonal antibody-MMAE conjugate, and a surfactant. The pharmaceutical formulation has characteristics of reduced particulate matter, reduced aggregates, improved stability of the conjugate, improved appearance of the lyophilized powders and the like. 1. An aqueous liquid pharmaceutical formulation of an antibody-drug conjugate , whereinthe formulation comprises the antibody-drug conjugate, a non-reducing sugar, an amino acid, and a solubilizer,the non-reducing sugar is selected from mannitol, sucrose, trehalose, and a combination thereof,the amino acid is selected from histidine, alanine, arginine, glycine, glutamic acid, a hydrochloride of the above amino acids, and a combination thereof, andthe solubilizer is selected from glycerol, Tween 80, and a combination thereof.2. The aqueous liquid pharmaceutical formulation according to claim 1 , wherein the concentration of the mannitol is 100-300 mmol/L and the concentration of the sucrose is 0-100 mmol/L.3. The aqueous liquid pharmaceutical formulation according to claim 1 , wherein the histidine is histidine hydrochloride at a concentration of 0-100 mmol/L and the arginine is arginine hydrochloride at a concentration of 0-160 mmol/L.4. The aqueous liquid pharmaceutical formulation according to claim 3 , wherein the content of the glycerol is 0-1 and the mass percentage of Tween 80 is 0-0.02% (w/v).5. The aqueous liquid pharmaceutical formulation according to claim 4 , wherein the antibody of the antibody-drug conjugate is an anti-HER2 monoclonal antibody; and the drug is MMAE claim 4 , MMAF claim 4 , DM1 claim 4 , DM4 claim 4 , or a derivative thereof.7. The aqueous liquid pharmaceutical formulation according to claim 5 , wherein the anti-HER2 monoclonal antibody comprises a heavy chain and a light chain claim 5 ,(i) the heavy chain comprises CDRs 1-3 having amino acid sequences as ...

USES OF CD20-BINDING MOLECULES AND ADDITIONAL THERAPEUTIC AGENTS

Provided herein are uses of CD20-binding molecules and one or more additional therapeutic agents. Certain CD20-binding molecules useful in the methods disclosed herein comprise 1) two or more CD20 binding regions and 2) one or more Shiga toxin effector polypeptides derived from an A Subunit of a member of the Shiga toxin family. Also disclosed herein are uses of CD20-binding molecules, and compositions thereof, (such as in conjunction with one or more additional therapeutic agents) for selective killing of specific cell types (such as a CD20-expressing tumor cell) and/or treating a variety of conditions, including cancers and tumors involving a CD20-expressing cell. 1. A method for treating or slowing the progression of a non-Hodgkin's lymphoma;wherein the method comprises administering to a subject in need thereof:(i) an effective amount of a CD20-binding molecule; and(ii) an effective amount of lenalidomide;wherein the CD20-binding molecule comprises a polypeptide having the sequence of SEQ ID NO: 54.2. The method of claim 1 , wherein the CD20-binding molecule is administered at a dose of about 10 μg/kg claim 1 , about 20 μg/kg claim 1 , about 25 μg/kg claim 1 , about 50 μg/kg claim 1 , or about 75 μg/kg of the subject's body weight3. The method of claim 2 , wherein the CD20-binding molecule is administered on each of days 1 claim 2 , 3 claim 2 , 5 claim 2 , 8 claim 2 , 10 claim 2 , and 12 of a first 28-day cycle.4. The method of claim 3 , wherein lenalidomide is administered daily on days 1 to 21 of the first 28-day cycle.5. The method of claim 3 , further comprising administering the CD20-binding molecule weekly during a second 28-day cycle following the first 28-day cycle claim 3 , wherein the CD20-binding molecule is administered on days 1 claim 3 , 8 claim 3 , 15 claim 3 , and 22 of the second 28-day cycle.6. The method of claim 5 , wherein each dose administered during the second 28-day cycle is in an amount of about 10 μg/kg claim 5 , about 25 μg/kg claim 5 ...

Omega-3 Fatty Acid Ester Compositions

Described herein are compositions including at least one Omega-3 fatty acid ester and at least one surface active agent; wherein the compositions form micelles when in contact with an aqueous medium. Also provided is a method of administering to a subject a composition comprising at least one Omega-3 fatty acid ester and at least one surface active agent, wherein the at least one Omega-3 fatty acid ester forms micelles when in contact with an aqueous medium, and the bioavailability of the at least one Omega-3 fatty acid ester is substantially independent of a food effect. Said compositions are useful for treating cardiovascular conditions or disorders in a subject and for reducing side effects associated with the ingestion of Omega-3 fatty acid esters. Described are also various dosage forms for administering said compositions and use of said compositions in functional foods. Provided herein are also kits with instructions on how to administer said compositions. 1. A pharmaceutical mixed-fatty-acids composition in which , a) at least 80% by weight of the composition is comprised of a combination of (all-Z omega-3)-5 ,8 ,11 ,14 ,17-eicosapentaenoic acids (EPA) and (all-Z omega-3)-4 ,7 ,10 ,13 ,16 ,19-docosahexaenoic acids (DHA) in a weight ratio of EPA:DHA of from about 1:2 to about 2:1; b) (all-Z omega-3)-6 ,9 ,12 ,15 ,18-heneicosapentaenoic acid is present in an amount of at least 1% by weight; and c) at least one surface active agent is provided; wherein said at least one surface active agent comprises from about 15% (wt/wt) to about 31% (wt/wt) polysorbate 80 and from about 0.5% (wt/wt) to about 5% (wt/wt) of a block copolymer of polyethylene glycol and polypropylene glycol polyoxamer having a chemical formula HO(CHO)(CHO)(CHO)(CHO)H (Pluronic F87); and wherein said composition , when administered to a human at equal dosage strengths , provides for substantially the same bioavailability when administered with or without food to said human in need of such ...

NANOSTRUCTURE COATED WITH A TWIST-STRAINED DOUBLE-STRANDED CIRCULAR DEOXYRIBONUCLEIC|ACID (DNA), METHOD FOR MAKING AND USE

A SWCNT coated with a twist-strained double-stranded circular deoxyribonucleic acid (DNA) is provided, together with methods for preparing the coated SWCNT, for removing the DNA coating from the SWCNT, and for sorting SWCNTs using the DNA coating. 123-. (canceled)24. A nanostructure coated with a twist-strained double-stranded circular deoxyribonucleic acid (DNA).25. The nanostructure of claim 24 , wherein the nanostructure is a carbon nanostructure.26. The nanostructure according to claim 25 , which is a single wall carbon nanotube.27. The nanostructure according to claim 26 , which is 100-700 nanometers in length.28. A method for(I) coating a nanostructure with a twist-strained double-stranded circular DNA, comprising incubating a nanostructure with a relaxed double-stranded circular DNA under conditions promoting a change in topology of said DNA to twist-strained double-stranded circular DNA, to thereby coat the nanostructure;(II) removing a twist-strained double-stranded circular DNA from a nanostructure coated with twist-strained double-stranded circular DNA, comprising incubating said nanostructure under conditions to relax the twist-strained double-stranded circular DNA; or(III) sorting nanostructures by size, comprising separating nanostructures that are coated with twist-strained double-stranded circular DNA.29. The method according to claim 28 , wherein in (I) said conditions comprise the presence of divalent cations.30. The method according to claim 29 , wherein said conditions comprise the presence of Mg.31. The method according to claim 30 , wherein said conditions comprise a Mgconcentration of about 60 to about 80 mM.32. The method according to claim 28 , wherein in (I) said conditions comprise a temperature of about 0 degrees centigrade to about 10 degrees centigrade.33. The method according to which further comprises in (I) separating a nanostructure that is coated with twist-strained double-stranded circular DNA from free DNA.34. The method ...

Compositions for Transfecting Resistant Cell Types

A reagent composition for delivery nucleic acid therapeutics to cells is provided. The reagent includes ionizable lipid, structural lipid, and a stabilizing agent which improves the transfection efficiency of nucleic acids, and leaves transfected cells viable. The 5 transfection reagent is effective in plasmid and mRNA delivery, and in neurons and progenitor-like cells. It may be used for ex vivo cell therapy. 1. A transfection reagent composition comprising:35-50 Mol % of an ionizable lipid, or a pharmaceutically acceptable salt thereof;15 to 25 Mol % structural lipid;35 to 41 Mol % sterol; and0.5 to about 10 Mol % of a stabilizing agent, wherein the stabilizing agent comprises more than one surfactant.2. The composition of claim 1 , wherein the ionizable lipid is an amino lipid or a pharmaceutically acceptable salt thereof.3. (canceled)4. The composition of claim 1 , wherein the stabilizing agent is a polysorbate.5. The composition of claim 4 , wherein the stabilizing agent is polysorbate (80).6. The composition of claim 1 , wherein the stabilizing agent is a maltoside.7. The composition of claim 1 , wherein the stabilizing agent is a mixture of polysorbates.8. A transfection reagent composition comprising:35-50 Mol % of an ionizable lipid, or a pharmaceutically acceptable salt thereof;15 to 25 Mol % structural lipid:35 to 41 Mol % sterol; and0.5 to about 10 Mol % of a stabilizing agent comprising a mixture of polysorbate and maltoside.9. The composition of claim 8 , wherein the stabilizing agent is a mixture of polysorbate 80 claim 8 , polysorbate 20 claim 8 , and Tridecyl-D-maltoside.10. The composition of wherein the mixture is an equal ratio of polysorbate 80 claim 9 , polysorbate 20 claim 9 , and Tridecyl-D-maltoside.11. The composition of claim 1 , wherein the ionizable lipid comprises about 40 Mol % of the composition.12. The composition of claim 1 , wherein the stabilizing agent comprises about 0.5 to 5 Mol % of the composition.13. The composition of claim ...

Nucleic Acid and Other Compositions and Methods for the Modulation of Cell Membranes

The present invention provides compositions and methods for transferring phospholipids and other molecules between the leaflets of a cell membrane. The compositions comprise at least one nucleic acid or compound having a hydrophilic region, where the composition is able to form a nanostructure that forms a toroidal pore in a lipid membrane. The nucleic acid or hydrophilic region-containing compound further contains an attached molecule capable of inserting the nanostructure into the lipid membrane. The invention also provides methods for scrambling lipids and other molecules in a cell membrane, which can be used to alter the function of a selected cell or to facilitate the death of the cell. The scrambling activity of synthetic scramblases described herein outperforms previously known enzymatically active DNA nanostructures and naturally occurring scramblases, in some cases by several orders of magnitude. 1. A composition comprising one or more hydrophilic regions forming a nanostructure and one or more hydrophobic or amphiphilic molecules attached to the one or more hydrophilic regions , wherein the one or more hydrophobic or amphiphilic molecules are able to insert the composition into a lipid membrane where the nanostructure forms a toroidal pore in the lipid membrane.2. The composition of claim 1 , wherein the composition comprises one or more nucleic acids which form the nanostructure comprising at least one interconnected nucleic acid duplex.3. The composition of claim 2 , wherein at least one of the nucleic acids comprises a polynucleotide sequence having at least 90% sequence identity to any of SEQ ID NO:1-8.4. The composition of claim 1 , wherein the composition comprises a plurality of nucleic acids which form a nanostructure comprising four interconnected nucleic acid duplexes claim 1 , wherein the one or more hydrophobic or amphiphilic molecules are attached to the 5′ or 3′ ends of at least two of the nucleic acids.5. The composition of claim 1 , wherein ...

PHARMACEUTICAL COMPOSITIONS HAVING IMPROVED STORAGE STABILITY

The present invention relates to a pharmaceutical composition that provides long-term stability of a hydrolytically labile antipsychotic agent 1. A method for minimizing degradation of a hydrolytically labile antipsychotic agent comprising adding to a composition comprising the antipsychotic agent and an aqueous vehicle (a) a non-ionic water insoluble or immiscible ester co-surfactant and (b) a water miscible or soluble non-ionic surfactant.2. The method of claim 1 , wherein the non-ionic water insoluble or immiscible ester co-surfactant is provided in an amount sufficient to minimize degradation of the antipsychotic agent.3. The method of claim 2 , wherein the amount of the non-ionic water insoluble or immiscible ester co-surfactant sufficient to minimize degradation is 0.25-0.45 weight percent of the total composition.4. The method of claim 2 , wherein the amount of the non-ionic water insoluble or immiscible ester co-surfactant sufficient to minimize degradation is 0.3-0.4 weight percent of the total composition.5. The method of claim 2 , wherein the amount of the non-ionic water insoluble or immiscible ester co-surfactant sufficient to minimize degradation does not exceed 0.5 weight percent of the total composition.6. The method of claim 2 , wherein the non-ionic water insoluble or immiscible ester co-surfactant is provided in an amount providing less than 50 parts per million of the hydrolyzed antipsychotic agent degradation product after the total composition stands for at least 24 months.7. The method of claim 2 , wherein the degradation of the hydrolytically labile antipsychotic agent is minimized at temperatures selected from any of 25° C.-40° C. claim 2 , over a time period selected from any of 1 month-24 months.8. (canceled)9. The method of claim 1 , wherein the composition is in a ready to use form.10. The method of claim 1 , wherein the non-ionic water insoluble or immiscible ester co-surfactant is a sorbitan ester of a carboxylic acid claim 1 , wherein ...

COMPOSITIONS COMPRISING SHORT-ACTING BENZODIAZEPINES

A composition is provided with a benzodiazepine and at least one hygroscopic excipient, in particular lactose and/or dextran. 139-. (canceled)41. A composition according to claim 40 , wherein the benzodiazepine according to formula (I) is methyl 3-[(4S)-8-bromo-1-methyl-6-(pyridine-2-yl)-4H-imidazo[1 claim 40 ,2-a][1 claim 40 ,4]benzodiazepin-4-yl]propanoate (remimazolam).42. A composition according to claim 41 , wherein in the pharmaceutically acceptable salt of the benzodiazepine is formulated in cationic form and the counter ion is benzene sulfonate (besylate).43. A composition as in claim 40 , wherein the dextran possesses a molecular weight of less than 150 kD.44. A composition according to claim 40 , wherein the disaccharide is selected from the group consisting of lactose claim 40 , maltose claim 40 , sucrose and trehalose.45. A composition according to claim 40 , wherein the composition comprises a mixture of a first hygroscopic excipient and a second hygroscopic excipient.46. A composition according to claim 40 , wherein the composition comprises a mixture of a disaccharide and dextran.47. A composition according to claim 46 , wherein the disaccharide is lactose claim 46 , and wherein the lactose and dextran have a wt % ratio between 1:1.0 to 1:10.48. A composition according to claim 40 , wherein the total amount of hygroscopic excipients and the total amount of benzodiazepines or salts thereof claim 40 , calculated for the base claim 40 , in the composition have a wt % ratio between 20:1 to 1:1.49. A composition according to claim 40 , which is a pharmaceutical formulation.52. The composition according to claim 50 , wherein less than 1% of the carboxylic ester moiety of the benzodiazepine is hydrolysed during storage.53. The composition according to claim 50 , wherein the hygroscopic excipient is a substance which at 25° C. and 1013.25 hPa reversibly binds water molecules.54. A Method of preparing a pharmaceutical composition comprising the steps of{'claim ...

METHODS FOR TREATING DIABETES AND REDUCING BODY WEIGHT

Methods for reducing body weight, altering body composition, treating diabetes, reducing HbAand reducing average daily blood glucose by the use of exendins, exendin agonists or exendin analog agonists are provided. 1133-. (canceled)134. A method for treating diabetes in a human in need thereof , the method comprising administering once monthly to the human an effective amount of a pharmaceutical composition comprising exendin-4 or an exendin analog to achieve a mean steady state plasma concentration of the exendin-4 or the exendin-4 analog at least 170 pg/ml for at least one month in the human to treat diabetes.135. The method of claim 134 , wherein the pharmaceutical composition comprises exendin-4.136. The method of claim 134 , wherein the pharmaceutical composition comprises the exendin analog.137. The method of claim 136 , wherein the exendin analog comprises the amino acid sequence of any one of SEQ ID NOs: 2 and 9-142.138. The method of claim 134 , wherein the pharmaceutical composition further comprises a sugar.139. The method of claim 134 , wherein the pharmaceutical composition further comprises a poly(lactide-co-glycolide) copolymer.140. The method of claim 139 , wherein the poly(lactide-co-glycolide) copolymer is purified 50:50 (lactide:glycolide) poly(D claim 139 ,L-lactide-co-glycolide).141. The method of claim 134 , wherein the pharmaceutical composition comprises 5% (w/w) exendin-4 claim 134 , 2% (w/w) sucrose claim 134 , and 93% (w/w) poly(lactide-co-glycolide)copolymer.142. The method of claim 134 , wherein the mean steady state plasma concentration of exendin-4 or the exendin analog is 170 pg/ml to 600 pg/ml.143. The method of claim 134 , wherein the mean steady state plasma concentration of exendin-4 or the exendin analog is 170 pg/ml to 350 pg/ml.144. The method of claim 134 , wherein the mean steady state plasma concentration of exendin-4 or the exendin analog is 170 pg/ml to 290 pg/ml.145. The method of claim 134 , wherein the diabetes is type ...

ORGANIC-INORGANIC HYBRID SOLID HAVING A MODIFIED OUTER SURFACE

The present invention concerns metal-organic hybrid solids having a modified outer surface. These solids can be used, for example, for the storage and vectoring of molecules of interest such as pharmaceutically active ingredients, compounds of interest in cosmetics and markers, for example contrast agents. These solids have good results in terms of active drug loading capacities, biocompatibility, stability and controlling the release of the active ingredients encapsulated. 3. A solid according to claim 1 , wherein the ligand L is a di- claim 1 , tri- or tetracarboxylate ligand selected from the group comprising: CH(CO)(fumarate) claim 1 , CH(CO)(succinate) claim 1 , CH(CO)(glutarate) claim 1 , CH(CO)(muconate) claim 1 , CH(CO)(adipate) claim 1 , CH(CO)(azelate) claim 1 , CHS(CO)(2 claim 1 ,5-thiophenedicarboxylate) claim 1 , CH(CO)(terephthalate) claim 1 , CHN(CO)(2 claim 1 ,5-pyrazine dicarboxylate) claim 1 , CH(CO)(naphthalene-2 claim 1 ,6-dicarboxylate) claim 1 , CH(CO)(biphenyl-4 claim 1 ,4′-dicarboxylate) claim 1 , CHN(CO)(azobenzenedicarboxylate) claim 1 , CH(CO)(benzene-1 claim 1 ,2 claim 1 ,4-tricarboxylate) claim 1 , CH(CO)(benzene-1 claim 1 ,3 claim 1 ,5-tricarboxylate) claim 1 , CH(CO)(benzene-1 claim 1 ,3 claim 1 ,5-tribenzoate) claim 1 , CH(CO)(benzene-1 claim 1 ,2 claim 1 ,4 claim 1 ,5-tetracarboxylate claim 1 , CH(CO)(naphthalene-2 claim 1 ,3 claim 1 ,6 claim 1 ,7-tetracarboxylate) claim 1 , CH(CO)(naphthalene-1 claim 1 ,4 claim 1 ,5 claim 1 ,8-tetracarboxylate) claim 1 , CH(CO)(biphenyl-3 claim 1 ,5 claim 1 ,3′ claim 1 ,5′-tetracarboxylate) claim 1 , and the modified analogs selected from the group comprising 2-aminoterephthalate claim 1 , 2-nitroterephthalate claim 1 , 2-methylterephthalate claim 1 , 2-chloroterephthalate claim 1 , 2-bromoterephthalate claim 1 , 2 claim 1 ,5-dihydroxoterephthalate claim 1 , tetrafluoroterephthalate claim 1 , tetramethylterephthalate claim 1 , dimethyl-4 claim 1 ,4′-biphenyldicarboxylate claim 1 , tetramethyl-4 ...

SUBSTITUTED ANIONIC COMPOUNDS CONSISTING OF A BACKBONE MADE UP OF A DISCRETE NUMBER OF SACCHARIDE UNITS

The invention relates to substituted anionic compounds consisting of a backbone made up of a discrete number u of between 1 and 8 (1≦u≦8) of identical or different saccharide units, linked via identical or different glycosidic bonds, said saccharide units being chosen from the group consisting of hexoses in cyclic form or in open reduced form, which are randomly substituted. It also relates to the process for the preparation thereof and to the pharmaceutical compositions comprising same. 1. Substituted anionic compounds , in isolated form or as a mixture , consisting of a backbone made up of a discrete number u of between 1 and 8 (1≦u≦8) of identical or different saccharide units , linked via identical or different glycosidic bonds , said saccharide units being chosen from the group consisting of hexoses in cyclic form or in open reduced form , characterized in that they are substituted with: {'br': None, 'sub': 1', 'a', 'm, '—[R]-[AA]\u2003\u2003formula V'}, 'c) at least one substituent of general formula Vthe substituents being identical or different when there are at least two substituents, in which:the radical -[AA]- denotes an amino acid residue,{'sub': '1', 'claim-text': [{'sub': 'a', 'either a bond and then a=0, and the amino acid residue -[AA] is directly bonded to the backbone via a function G,'}, {'sub': 2', '15', 'a', '1, 'or a Cor Ccarbon-based chain, and then a=1, which is optionally substituted and/or comprising at least one heteroatom chosen from O, N and S and at least one acid function before the reaction with the amino acid, said chain forming, with the amino acid residue -[AA], an amide function, and is attached to the backbone by means of a function Fresulting from a reaction between a hydroxyl function borne by the backbone and a function or a substituent borne by the precursor of the radical —R—,'}], 'the radical —R— being{'sub': 'a', 'Fis a function chosen from ether, ester or carbamate functions,'}{'sub': 'a', 'Gis a carbamate function,'}m is ...

POLYMER-CARBOHYDRATE CONJUGATES FOR DRUG DELIVERY TECHNOLOGY

The invention comprises compounds, methods of making, and methods of using. The compounds may have a linear or cylic backbone and three or four appended functional groups: one or two lipohilic compounds including sterols or “fat soluble” vitamins, one or two hydrophilic polymer, and one or two carbohydrate. A group of polymer-carbohydrate conjugates having a central backbone and three appended functional groups are disclosed wherein one lipophilic compound is void of both steroid acids. The conjugate may have fatty acids as the primary lipophilic carrier, one hydrophilic polymer, and one carbohydrate. Specific functional groups may be selected for specific applications in formulating pharmaceuticals, cosmetics, nutriceuticals, and the like. Typical coupling reaction of the conjugates may involve one or more or combinations or in series of alkylation including N-alkylation or O-alkylation, etherification, esterification and amidation chemical processes. A variety of linkers between the backbone and functional groups may also be selected to modify the carriers or center backbones for the coupling reactions and optimize performance of the conjugates. 2. The chemical compound of wherein:said Backbone comprises at least three available binding positions or sites for the conjugation of a first carrier, a second carrier, and a third carrier, each said available binding position or site comprising an expendable amino, hydroxyl, or carboxylic group;said first carrier comprising said lipophilic molecule and an expendable amino, hydroxyl, or carboxylic group;said second carrier comprising said polymer and an expendable amino, hydroxyl, or carboxylic group; andsaid third carrier comprising said carbohydrate and an expendable amino, hydroxyl, or carboxylic group.3. The chemical compound of wherein:said Backbone comprises at least four available binding positions or sites for the conjugation of a first carrier, a second carrier, a third carrier, and a fourth carrier, each said ...

CTLA4-IG FUSION PROTEIN FORMULATION

The present invention discloses a stable pharmaceutical formulation of a fusion protein, wherein the formulation contains buffer, sugar alcohol/polyol, amino acid and surfactant, and wherein the formulation is devoid of sucrose. Additionally, the formulation may also be devoid of a salt. The disclosed fusion protein formulations are liquid formulations that are also suitable for lyophilization. 1. A stable aqueous pharmaceutical formulation of a CTLA4-Ig fusion protein comprising , CTLA4-Iq fusion protein , a buffer , polyol , amino acid and surfactant , and wherein the formulation is devoid of sucrose.2. The formulation according to claim 1 , wherein the ratio of CTLA4-Ig fusion protein to polyol is 1:0.7 or lower and the ratio of CTLA4-Ig fusion protein to amino acid is 1:0.1 or lower.3. The formulation according to claim 1 , wherein the concentration of CTLA4-Ig fusion protein formulation is from about 20 mg/ml to about 200 mg/ml.4. The formulation according to claim 1 , wherein the pH of the formulation is from 6.0 to 8.0.5. The formulation according to claim 1 , wherein the formulation has a viscosity of less than 15 cp.6. The formulation according to claim 1 , whereinthe fusion protein in formulation is stable at 30° C. for at least two weeks and contains less than about 10% of fusion protein molecule in aggregate form.7. A stable formulation of CTLA4-Ig fusion protein comprising phosphate buffer claim 1 , mannitol claim 1 , histidine and surfactant claim 1 , and wherein the formulation is devoid of sucrose.8. The formulation according to claim 7 , wherein the concentration of mannitol is about 80 mg/ml and the concentration of histidine is between 10 mg/ml-15 mg/ml.9. A method of obtaining a stable formulation of CTLA4-Ig fusion protein comprising addition of buffer claim 7 , polyol claim 7 , histidine and surfactant to the CTLA4-Ig fusion protein claim 7 , and wherein histidine and polyol are also added to the pre-formulation process steps of ultrafiltration ...

FORMULATION OF HUMAN ANTIBODIES FOR TREATING TNF-ALPHA ASSOCIATED DISORDERS

A liquid aqueous pharmaceutical formulation is described which has a high protein concentration, a pH of between about 4 and about 8, and enhanced stability. 1. A stable liquid aqueous pharmaceutical formulation comprising: a human anti-human Tumor Necrosis Factor alpha (TNFα) IgG1 antibody at a concentration of 45 to 105 mg/ml , wherein the antibody is D2E7 , and a buffer system;wherein the formulation is isotonic, suitable for single-use subcutaneous injection, and has a pH of 4 to 8.2. The formulation of claim 1 , wherein the buffer system comprises an organic acid.3. The formulation of claim 2 , wherein the organic acid is selected from the group consisting of succinate claim 2 , acetate claim 2 , and histidine.4. The formulation of claim 2 , wherein the pH is 4.5 to 6.0.5. The formulation of claim 2 , wherein the formulation comprises a surfactant.6. The formulation of claim 5 , wherein the surfactant is a polysorbate.7. The formulation of claim 6 , wherein the polysorbate is polysorbate-80.8. The formulation of claim 2 , wherein the formulation comprises a tonicity agent.9. The formulation of claim 8 , wherein the tonicity agent is a polyol.10. The formulation of claim 9 , wherein the polyol is a sugar claim 9 , a sugar alcohol or a sugar acid.11. The formulation of claim 10 , wherein the sugar is trehalose.12. The formulation of claim 10 , wherein the sugar is sucrose.13. The formulation of claim 10 , wherein the sugar alcohol is sorbitol.14. The formulation of claim 10 , wherein the sugar alcohol is mannitol.15. The formulation of claim 10 , wherein the formulation comprises a surfactant.16. The formulation of claim 15 , wherein the surfactant is a polysorbate.17. The formulation of claim 16 , wherein the polysorbate is polysorbate-80.18. The formulation of claim 17 , wherein the sugar is trehalose.19. The formulation of claim 17 , wherein the sugar is sucrose.20. The formulation of claim 17 , wherein the sugar alcohol is sorbitol.21. The formulation of ...

Camptothecin Conjugates of Anti-CD22 Antibodies for Treatment of B Cell Diseases

Disclosed herein are compositions and methods of use comprising combinations of anti-CD22 antibodies with a therapeutic agent. The therapeutic agent may be attached to the anti-CD22 antibody or may be separately administered, either before, simultaneously with or after the anti-CD22 antibody. In preferred embodiments, the therapeutic agent is an antibody or fragment thereof that binds to an antigen different from CD22, such as CD19, CD20, CD21, CD22, CD23, CD37, CD40, CD40L, CD52, CD80 and HLA-DR. However, the therapeutic agent may an immunomodulator, a cytokine, a toxin or other therapeutic agent known in the art. More preferably, the anti-CD22 antibody is part of a DNL complex, such as a hexavalent DNL complex. Most preferably, combination therapy with the anti-CD22 antibody or fragment and the therapeutic agent is more effective than the antibody alone, the therapeutic agent alone, or the combination of anti-CD22 antibody and therapeutic agent that are not conjugated to each other. Administration of the anti-CD22 antibody and therapeutic agent induces apoptosis and cell death of target cells in diseases such as B-cell lymphomas or leukemias, autoimmune disease or immune dysfunction disease. 124-. (canceled)25. A method of treating a B cell lymphoma or B cell leukemia comprising administering to a human with a B cell lymphoma or B cell leukemia , an immunoconjugate consisting of (i) an anti-CD22 antibody or antigen binding fragment thereof; and (ii) at least one therapeutic agent attached by a chelating agent to the anti-CD22 antibody or fragment thereof , wherein the therapeutic agent is an alpha-emitting radionuclide , wherein the anti-CD22 antibody or fragment thereof comprises the light chain complementarity determining region (CDR) sequences CDR1 (KSSQSVLYSANHKYLA , SEQ ID NO:1) , CDR2 (WASTRES , SEQ ID NO:12) , and CDR3 (HQYLSSWTF , SEQ ID NO:3) and the heavy chain CDR sequences CDR1 (SYWLH , SEQ ID NO:4) , CDR2 (YINPRNDYTEYNQNFKD , SEQ ID NO:5) , and CDR3 ( ...

FORMULATIONS COMPRISING TRIPTAN COMPOUNDS

The invention provides a pharmaceutical composition for intranasal administration comprising a salt of sumatriptan or a physiologically acceptable solvate thereof, an alkyl glycoside or saccharide alkyl ester and optionally at least one pharmaceutically acceptable excipient, wherein the said composition provides Tvalue of less than 30 minutes upon said administration. Other aspects and embodiments are contemplated and described. 152-. (canceled)53. A method of treating a human suffering from or susceptible to cephalic pain comprising intranasal administration of a composition comprising sumatriptan , or a physiologically acceptable solvate thereof , an alkyl glycoside or saccharide ester and optionally a pharmaceutically acceptable excipient , wherein , said composition provides a Tsubstantially equivalent to subcutaneous administration of said sumatriptan.54. The method as claimed in claim 53 , wherein said composition provides Tvalue of less than 30 minutes.55. (canceled)56. (canceled)57. The method as claimed in claim 53 , wherein said composition provides Tvalue ranging from about 4 minutes to about 15 minutes.58. The method as claimed in claim 53 , wherein said alkyl glycoside or saccharide alkyl ester is selected from dodecyl maltoside (1-O-n Dodecyl-β-D-Maltopyranoside) claim 53 , tridecyl maltoside claim 53 , sucrose monododecanoate claim 53 , sucrose monotridecanoate and sucrose monotetradecanoate.59. The method as claimed in claim 58 , wherein said alkyl glycoside or saccharide alkyl ester is dodecyl maltoside (1-O-n-Dodecyl-β-D-Maltopyranoside).60. (canceled)61. (canceled)62. The method as claimed in claim 53 , wherein said composition upon nasal administration provides a ratio of Cto AUCof at least about 0.3.6371.-. (canceled)72. The method as claimed in claim 53 , wherein said alkyl glycoside or saccharide alkyl ester is present in a concentration of from about 0.05 to about 3.0%.73. The method as claimed in claim 72 , wherein said alkyl glycoside or ...

COMPOSITIONS AND METHODS FOR FECAL MICROBIOTA TRANSPLANTATION

The present disclosure provides human fecal microbiota compositions, including fresh, frozen, and lyophilized compositions, for the treatment of disorders associated with dysfunctional microbiota, such as recurrent infection. In particular, the fecal microbiota composition comprises a cryoprotectant sugar, such as mannitol. 1. A composition comprising (a) an extract of human feces comprising viable fecal microbiota and (b) at least one sugar.2. The composition of claim 1 , wherein the sugar is mannitol or sucrose.3. The composition of claim 1 , wherein the at least one sugar is present at a concentration of 0.5% to 5% (vol/vol).4. The composition of claim 1 , wherein the at least one sugar is present at a concentration of 1% to 3% (vol/vol).5. The composition of claim 1 , wherein the at least one sugar is present at a concentration of at least 1% claim 1 , 2% claim 1 , 3% claim 1 , 4% claim 1 , 5% claim 1 , 6% claim 1 , 7% claim 1 , 8% claim 1 , 9% claim 1 , or 10% (vol/vol).6. The composition of claim 1 , wherein the composition comprises at least 4 different phyla of bacteria selected from the group consisting of Bacteroidetes claim 1 , Firmicutes claim 1 , Proteobacteria claim 1 , Verrucomicrobiae claim 1 , and Actinobacteria.7. The composition of claim 1 , wherein the composition comprises at least 5 claim 1 , 6 claim 1 , 7 claim 1 , 8 claim 1 , 9 claim 1 , or 10 different classes of bacteria selected from the group consisting of Actinobacteria claim 1 , Bacteroidia claim 1 , Bacilli claim 1 , Clostridia claim 1 , Erysipelotrichi claim 1 , Alphaproteobacteria claim 1 , Betaproteobacteria claim 1 , Gammaproteobacteria claim 1 , Mollicutes claim 1 , and Verrucomicrobiae.8. The composition of claim 1 , wherein the composition comprises at least 4 claim 1 , 5 claim 1 , 6 claim 1 , 7 claim 1 , 8 claim 1 , 9 claim 1 , or 10 different families of bacteria selected from the group consisting of Lachnospiraceae claim 1 , Enterobacteriaceae claim 1 , Bacteroidaceae claim 1 ...

ANTISEPTIC AGENT COMPRISING MEGLUMINE OR SALT THEREOF

The present invention addresses the problem of providing a novel application of meglumine or a salt thereof. The present invention is an antiseptic agent consisting of meglumine or a salt thereof, and a pharmaceutical composition comprising the antiseptic agent according to the present invention, and pertaining to: a pharmaceutical composition which does not comprise benzalkonium chloride and which is placed in a reusable container; a product that comprises the pharmaceutical composition comprising the antiseptic agent according to the present invention and a reusable container; and a method of improving the antiseptic effect of the pharmaceutical composition by comprising meglumine or a salt thereof in the pharmaceutical composition that has been placed in the reusable container. 1. An antiseptic agent consisting of meglumine or a salt thereof.2. The antiseptic agent according to claim 1 , which is for use in a pharmaceutical composition to be placed in a repeatedly operable container.3. The antiseptic agent according to claim 1 , which is for use in a pharmaceutical composition not comprising benzalkonium chloride.4. The antiseptic agent according to claim 1 , which is for use in a pharmaceutical composition not comprising polyhexamethylene biguanide.5. The antiseptic agent according to claim 1 , which is for use in a pharmaceutical composition not comprising boric acid or a salt thereof.6. The antiseptic agent according to claim 1 , which is for use in a pharmaceutical composition not comprising N-hexadecanyl-DABCO.7. The antiseptic agent according to claim 1 , which is for use in a pharmaceutical composition comprising 0.0001 to 0.1% (w/v) of edetic acid or a salt thereof.8. An antiseptic composition comprising the antiseptic agent according to claim 1 , but not comprising an antiseptic agent other than the antiseptic agent according to .9. A pharmaceutical composition comprising the antiseptic agent according to claim 1 ,the pharmaceutical composition not ...

LOW ACIDIC SPECIES COMPOSITIONS AND METHODS FOR PRODUCING AND USING THE SAME

The instant invention relates to low acidic species (AR) compositions comprising a protein, e.g., an antibody, or antigen-binding portion thereof, and methods, e.g., cell culture and/or protein purification methods, for producing such low AR compositions. Methods for using such compositions to treat a disorder, e.g., a disorder in which TNFα is detrimental, are also provided. 1. A low acidic species adalimumab pharmaceutical composition suitable for administration to a human subject comprising 40 mg of adalimumab wherein the low acidic species adalimumab pharmaceutical composition comprises less than 10% total acidic species of adalimumab , wherein the acidic species of adalimumab have a net negative charge relative to the adalimumab main species and the acidic species comprise species selected from the group consisting of charge variants , structure variants , fragmentation variants and any combinations thereof; wherein the acidic species of adalimumab do not include process-related impurities selected from the group consisting of host cell proteins , host cell nucleic acids , chromatographic materials and media components; and wherein said low acidic species adalimumab pharmaceutical composition demonstrates reduced cell infiltration , reduced synovial proliferation , reduced proteoglycan loss , reduced cartilage destruction , and/or reduced bone erosion compared to a non-low acidic species composition of adalimumab; and a pharmaceutically acceptable carrier.2. The pharmaceutical composition of claim 1 , wherein the charge variants comprise one or more of deamidation variants claim 1 , glycation variants claim 1 , afucosylation variants claim 1 , MGO variants or citric acid variants claim 1 , the structure variants comprise one or more of glycosylation variants or acetonation variants claim 1 , and the fragmentation variants comprise one or more of Fab fragment variants claim 1 , C-terminal truncation variants or variants missing a heavy chain variable domain.3. ...

PHARMACEUTICAL COMPOSITION

Provided is a pharmaceutical composition containing pemafibrate, a salt thereof or a solvate thereof and having excellent homogeneity. The pharmaceutical composition is provided containing the following components (A) and (B): (A) pemafibrate, a salt thereof or a solvate thereof; and (B) a disaccharide species. 1. A pharmaceutical composition comprising the following components (A) and (B):(A) pemafibrate, a salt thereof or a solvate thereof, and(B) a disaccharide species.2. The pharmaceutical composition of claim 1 , wherein the component (B) is one or more selected from the group consisting of sucrose claim 1 , lactulose claim 1 , lactose claim 1 , maltose claim 1 , trehalose claim 1 , cellobiose claim 1 , kojibiose claim 1 , nigerose claim 1 , isomaltose claim 1 , isotrehalose claim 1 , neotrehalose claim 1 , sophorose claim 1 , laminaribiose claim 1 , gentiobiose claim 1 , turanose claim 1 , maltulose claim 1 , palatinose claim 1 , gentiobiulose claim 1 , mannobiose claim 1 , melibiose claim 1 , melibiulose claim 1 , neolactose claim 1 , galactosucrose claim 1 , scillabiose claim 1 , rutinose claim 1 , rutinulose claim 1 , vicianose claim 1 , xylobiose claim 1 , primevelose claim 1 , sucralose and a solvate thereof.3. The pharmaceutical composition of claim 1 , wherein (B) is one or more selected from the group consisting of sucrose claim 1 , lactose claim 1 , maltose claim 1 , trehalose claim 1 , palatinose claim 1 , sucralose and a solvate thereof.4. The pharmaceutical composition of claim 1 , further comprising a component (C):(C) cellulose.5. The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition is a solid preparation.6. The pharmaceutical composition of claim 1 , wherein a dosage form thereof is a tablet claim 1 , a capsule claim 1 , a granule claim 1 , a powder or a pill.7. A method for improving content uniformity of pemafibrate claim 1 , a salt thereof or a solvate thereof in a pharmaceutical composition claim 1 , the method ...

Oral Administration of Tocilizumab Treatment of Autoimmune Disease

The present invention provides a method for treating or delaying the onset of an autoimmune condition in a human subject comprising orally administering to the subject at an effective dose of tocilizumab. 1. A method for treating or delaying the onset of an autoimmune condition in a human subject comprising orally administering to the subject an effective dose of tocilizumab.2. The method of claim 1 , wherein the tocilizumab is administered in a liquid form.3. The method of claim 1 , wherein the tocilizumab is administered in a solid form.4. The method of claim 1 , wherein the condition is rheumatoid arthritis claim 1 , psoriasis claim 1 , type 1 diabetes claim 1 , systemic lupus erythematosus claim 1 , transplant rejection claim 1 , autoimmune thyroid disease (Hashimoto's disease) claim 1 , sarcoidosis claim 1 , scleroderma claim 1 , granulomatous vasculitis claim 1 , Crohn's disease claim 1 , ulcerative colitis claim 1 , Sjogren's disease claim 1 , ankylosing spondylitis claim 1 , polymyositis dermatomyositis claim 1 , polyarteritis nodosa claim 1 , immunologically mediated blistering skin diseases claim 1 , Behcet's syndrome claim 1 , multiple sclerosis claim 1 , systemic sclerosis claim 1 , Goodpasture's disease or immune mediated glomerulonephritis.5. The method of claim 1 , wherein neuropeptide Y is administered in a dose from about 1.0 mg to about 50 mg.6. The method of claim 5 , wherein tocilizumab is administered in a dose from about 10 mg.7. The method of claim 1 , wherein said tocilizumab administration decreases levels of IL-6 claim 1 , Th1-like cytokines IL-2 claim 1 , IL-12 claim 1 , TNF-a and IFN-g.8. The method of claim 1 , wherein said tocilizumab administration increases levels of IL-4 claim 1 , IL-10 and IL-13.9. The method of claim 1 , further comprising administering a compound selected from the group consisting of a SIRS peptide claim 1 , a-MSH claim 1 , ACTH and SST.10. A method of decreasing innate inflammatory cytokines IL-1b and TNF-a claim ...

Organic Compounds

A solid pharmaceutical composition suitable for oral administration, comprising: (a) S 1 P receptor agonist; and (b) a sugar alcohol.

ADRENOCORTICOTROPIC HORMONE-BASED PHARMACEUTICAL FORMULATIONS AND METHODS FOR FABRICATING AND USING THEREOF

Pharmaceutical compositions for treating, mitigating or preventing multiple sclerosis, autoimmune diseases and associated conditions are described herein. Methods for fabricating the compositions and using them are also described. 1. A pharmaceutical composition , comprising a quantity corticotropin of a non-animal derivation , wherein the composition is free of gelatin and free of preservatives.2. The pharmaceutical composition of claim 1 , wherein the corticotropin comprises a quantity of a recombinant polypeptide and optionally a quantity of a naturally occurring polypeptide.3. The pharmaceutical composition of claim 2 , wherein the corticotropin is free of the naturally occurring polypeptide.4. The pharmaceutical composition of claim 3 , wherein the recombinant polypeptide is the amino acid sequence selected from the group of SEQ ID NO: 1 claim 3 , SEQ ID NO: 2 claim 3 , SEQ ID NO: 3 claim 3 , SEQ ID NO: 4 claim 3 , SEQ ID NO: 5 claim 3 , and combinations thereof.5. The pharmaceutical composition of claim 4 , wherein the recombinant polypeptide is the amino acid sequence as set forth in SEQ ID NO: 1.6. The pharmaceutical composition of claim 1 , further comprising an amino acid selected from the group consisting of cysteine claim 1 , methionine claim 1 , and combinations thereof.7. The pharmaceutical composition of claim 6 , further comprising a water-soluble thickening agent selected from the group consisting of carboxymethyl cellulose claim 6 , dextrose claim 6 , mannitol claim 6 , methyl cellulose claim 6 , hydroxyethyl cellulose claim 6 , hydroxypropyl cellulose claim 6 , non-cross-linked or partially cross-linked polyacrylates claim 6 , polyoxyethylene sorbitan monolaurates claim 6 , polyoxyethylene sorbitan monopalmitates claim 6 , polyoxyethylene sorbitan monostearates claim 6 , polyoxyethylene sorbitan monooleates claim 6 , and combinations thereof.8. The pharmaceutical composition of claim 7 , further comprising at least one non-ionic poly(oxyethlene-co ...