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Небесная энциклопедия

Космические корабли и станции, автоматические КА и методы их проектирования, бортовые комплексы управления, системы и средства жизнеобеспечения, особенности технологии производства ракетно-космических систем

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Мониторинг СМИ

Мониторинг СМИ и социальных сетей. Сканирование интернета, новостных сайтов, специализированных контентных площадок на базе мессенджеров. Гибкие настройки фильтров и первоначальных источников.

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Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 6248. Отображено 100.
05-01-2012 дата публикации

Method of Inhibition of Respiratory Depression Using Positive Allosteric AMPA Receptor Modulators

Номер: US20120004219A1
Автор: John Greer
Принадлежит: University of Alberta

The invention is directed to a method for alleviating respiratory depression in a subject as a result of disease of pharmacological agents such as opiates, opioids or barbiturates. The invention also discloses pharmaceutical compositions for use with the method, the composition containing in combination, an analgesic, anaesthetic, or a sedative and a positive allosteric AMPA receptor modulator in an amount sufficient to reduce or inhibit respiratory depression caused by the analgesic, anaesthetic, or sedative.

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Номер записи: 1
09-02-2012 дата публикации

Prolonged duration local anesthesia with minimal toxicity

Номер: US20120034296A1
Автор: Daniel S. Kohane, Hila Epstein-Barash
Принадлежит: Childrens Medical Center Corp, Massachusetts Institute of Technology

Compositions containing site 1 sodium channel blockers for use as local anesthetics with rapid nerve block, improved potency and efficacy, and no local toxicity have been developed. Liposomes were employed for increased loading of the site 1 sodium channel blocker, producing prolonged duration of block without systemic toxicity. In one embodiment, the compositions contain a site 1 sodium channel blocker alone. In another embodiment, the compositions contain a site 1 sodium channel blocker in combination with a corticosteroid. As demonstrated by the examples, encapsulating site 1 sodium channel blockers in liposomes results in rapid and prolonged nerve block without systemic toxicity, which is enhanced by the addition of a corticosteroid. Fluid liposomes showed more rapid release of STX than did solid ones, and dexamethasone accelerated STX release.

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Номер записи: 2
08-03-2012 дата публикации

Anesthesia reversal methods and systems

Номер: US20120055481A1
Автор: Derek Jo Sakata, Dwayne R. Westenskow, Joseph A. Orr
Принадлежит: ANECARE LLC

An apparatus for reversing inhaled anesthesia, which may be configured to be positioned along a breathing circuit or anesthesia delivery circuit, includes an anesthesia removal component and a blood flow acceleration component. The blood flow acceleration component facilitates an increase in the ventilation of the individual without resulting in a significant decrease in the individual's P a CO 2 level and, thus, a decrease in the rate at which blood flows through the individual's brain. A method of reversing the effects of inhaled anesthesia includes increasing the rate of ventilation of an anesthetized individual while causing the individual to inhale gases with at least atmospheric amounts of CO 2 .

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Номер записи: 3
15-03-2012 дата публикации

Preparation for external application

Номер: US20120064011A1
Автор: Dirk Schumann
Принадлежит: Bubbles and Beyond GmBH

Preparations for external application to human and animal skin, comprising: a) a composition in the form of a fluid nanophase system, comprising the components of a1) at least one water-insoluble substance with a water solubility of less than 4 gram per liter, a2) at least one amphiphilic substance (NP-MCA), which has no surfactant structure, does not build structures alone, the solubility of which is between 4 g and 1000 g per liter in water or oil and which does not enrich preferably at the oil-water interface, a3) at least one anionic, cationic, amphoteric and/or non-ionic surfactant, a4) at least one polar protic solvent, in particular having hydroxy functionality, a5) if necessary one or more adjuvants, wherein the percentage relate to the total weight of the composition each; and b) a therapeutic, cosmetic or diagnostically effective agent in a therapeutic, cosmetic or diagnostically effective amount.

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Номер записи: 4
05-04-2012 дата публикации

Photochrome- or near ir dye-coupled polymeric matrices for medical articles

Номер: US20120082713A1
Автор: Aron B. Anderson, Emily R. Rolfes Meyering
Принадлежит: Surmodics Inc

The invention provides polymers comprising pendent photochrome or near IR dye groups, as well as polymeric matrices made from these polymers, which can be used as or in association with a medical article. The polymers can be synthesized using methods that facilitate the preparation of medical articles having good biocompatibility. Exemplary polymeric matrices are in the form of lubricious coatings on medical devices, such as catheters. Visualization by irradiation of the photochrome or near IR dye can improve detection of the polymeric matrix on a device or in the body. This, in turn can improve aspects of a medical procedure, such as device insertion or matrix formation, as well as being useful for assessing the quality of the matrix.

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Номер записи: 5
05-04-2012 дата публикации

Topical Anesthetic Uses of Szeto-Schiller Peptides

Номер: US20120083452A1
Автор: Nicholas V. Perricone
Принадлежит: Individual

Topical anesthetic compositions include Szeto-Schiller peptides and a dermatologically acceptable carrier, and optionally a vasoconstrictor and tyrosine. A method of providing local analgesia to the skin involves applying to skin the topical anesthetic compositions.

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Номер записи: 6
05-04-2012 дата публикации

Nasal sinus spray for treatment of sinus headache and method of using same

Номер: US20120083516A1
Автор: Lyndon Mansfield
Принадлежит: Individual

Disclosed is a nasal spray containing the combination of a vasoconstrictor and a topical local anesthetic.

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Номер записи: 7
12-04-2012 дата публикации

Mu-Conotoxin Peptides and Use Thereof as a Local Anesthetic

Номер: US20120087969A1
Автор: Evelyne Benoit, Jordi Molgo, Philippe Favreau, Reto Stocklin
Принадлежит: Atheris Laboratories, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE CNRS

In one embodiment, the present invention relates to novel mu-conotoxin peptides, biologically active fragments thereof, combinations thereof and/or variants thereof. An embodiment of the invention also relates to their use in pharmaceutical composition for the treatment or prevention of pain, and their use in the preparation of an anesthetic.

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Номер записи: 8
19-04-2012 дата публикации

Oral medicinal composition and oral medicinal capsule having the composition encapsulated therein

Номер: US20120093925A1
Автор: Tsuyoshi Shimoo
Принадлежит: Morishita Jintan Co Ltd

The present invention relates to an oral medicinal composition comprising (a) a medical agent that is low in solubility in both water and oils but is soluble in a polyethylene glycol, (b) a polyethylene glycol that is solid at temperatures of 40° C. or lower, and (c) an oily or aqueous auxiliary agent. The oral medicinal composition cannot provide any stimulus or unpleasant feeling during being dissolved in the mouth, and is improved in the solubility of the medicinal agent in the mouth, and is also improved in the absorbability of the medicinal agent in the mouth.

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Номер записи: 9
03-05-2012 дата публикации

Injectable composition containing hydroxychloroquine for local administration for treating hemorrhoids

Номер: US20120108633A1
Автор: Oh-Young Yeo
Принадлежит: Individual

The present invention relates to an injectable composition for local administration for treating hemorrhoids, which contains hydroxychloroquine. Specifically, the composition contains a solution of hydroxychloroquine in physiological saline for injection, together with a local anesthetic and an antioxidant.

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Номер записи: 10
14-06-2012 дата публикации

Trp inhibitors and uses thereof

Номер: US20120148604A1
Автор: Eric M. Ostertag, John Stuart Crawford
Принадлежит: Transposagen Biopharmaceuticals Inc

The present invention, relates to methods including compounds, derivatives, antibodies, interfering RNA, biologies, polypeptides, dominant negative effectors, and their use in the treatment of neuropathic pain by inhibition of transient receptor potential (TRP) channels. In another embodiment, this invention relates to inhibitors, antagonists, and agonists of TRPC4. TRPC4 therapeutic agents and modulators include but are not limited to small molecule inhibitors, compounds, amino acid derivatives, polypeptides, RNA interference agents, natural chemicals, ligand derivatives, and ions. TRPC4 therapeutic agents and modulators are developed for the treatment of neuropathic pain, including but not limited to pain sensations such as nociception, hyperalgesia, allodynia, and loss of sensory function.

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Номер записи: 11
28-06-2012 дата публикации

Transdermal drug delivery device including an occlusive backing

Номер: US20120165762A1
Автор: David Kanios, Juan A. Mantelle, Viet Nguyen
Принадлежит: Noven Pharmaceuticals Inc

A transdermal drug delivery system for the topical application of one or more active agents contained in one or more polymeric and/or adhesive carrier layers, proximate to a non-drug containing polymeric backing layer which can control the delivery rate and profile of the transdermal drug delivery system by adjusting the moisture vapor transmission rate of the polymeric backing layer.

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Номер записи: 12
26-07-2012 дата публикации

Androgen composition for treating an opthalmic condition

Номер: US20120190661A1
Автор: Adnan K.. Salameh, Anuradha V. Gore, Chetan P. Pujara, Jaya Giyanani, John T. Trogden
Принадлежит: Allergan Inc

The disclosure provides compositions for treating an ocular condition. The composition comprises a physiologically effective amount of an androgen, wherein the composition is suitable for topical administration to an eye. The disclosure further provides methods for treating an ocular condition with the disclosed compositions.

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Номер записи: 13
06-09-2012 дата публикации

Systems and methods for gas treatment

Номер: US20120222556A1
Автор: Biljna Milin, Dusanka Filipovic, Frederick Cashin, Laurence Whitby
Принадлежит: Blue Zone Tech Ltd

A system and process for the recovery of at least one halogenated hydrocarbon from a gas stream. The recovery includes adsorption by exposing the gas stream to an adsorbent with a lattice structure having pore diameters with an average pore opening of between about 5 and about 50 angstroms. The adsorbent is then regenerated by exposing the adsorbent to a purge gas under conditions which efficiently desorb the at least one adsorbed halogenated hydrocarbon from the adsorbent. The at least one halogenated hydrocarbon (and impurities or reaction products) can be condensed from the purge gas and subjected to fractional distillation to provide a recovered halogenated hydrocarbon.

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Номер записи: 14
27-12-2012 дата публикации

Mucosal bioadhesive slow release carrier for delivering active principles

Номер: US20120326350A1
Автор: Caroline Lemarchand, Dominique Costantini
Принадлежит: Bioalliance Pharma SA

A mucosal bioadhesive slow release carrier comprising an active principle and devoid of starch, lactose, which can release the active principal for a duration of longer than 20 hours. This bioadhesive carrier contains a diluent, an alkali metal alkylsulfate, a binding agent, at least one bioadhesive polymer and at least one sustained release polymer, as well as a method for its preparation.

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Номер записи: 15
31-01-2013 дата публикации

Transdermal Delivery Systems for Sufentanil

Номер: US20130028953A1
Автор: Felix Theeuwes, Su Ii Yum
Принадлежит: Durect Corp

Transdermal delivery systems for administering sufentanil through the skin are provided. The systems contain a sufficient amount of sufentanil to induce and maintain a constant state of analgesia when applied to a subject. The systems are characterized as having one or more features including a high degree of dosage form rate control over flux of sufentanil from the system, a high net flux of sufentanil from the system through the skin, lack of a permeation enhancer, an adhesive member demonstrating superior shear time, a low coefficient of variation in the net flux of sufentanil from the system, a high delivery efficiency, and a substantially constant steady state net flux of sufentanil from the system. Methods of using the transdermal delivery systems to administer a sufficient amount of sufentanil to induce and maintain analgesia for extended periods when applied to a subject are also provided.

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Номер записи: 16
21-02-2013 дата публикации

Analgesic and anti-inflammatory composition

Номер: US20130045279A1
Автор: Jeffrey D. Edwards, John Palermo
Принадлежит: CAMBRIDGE SCIENTIFIC PTY LTD

The present invention discloses a composition that contains (1) an effective amount of an analgesically and/or anti-inflammatory active fraction separated from a mixture of plasma and/or serum, and (2) at least one metal, metal ion or metal salt, in which the mixture has been denatured. Also disclosed are methods of producing the composition for treating a subject afflicted with inflammation and/or pain.

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Номер записи: 17
18-04-2013 дата публикации

Use of inhaled nitrous oxide or xenon for preventing neuropathic pain caused by cancer chemotherapy

Номер: US20130095194A1
Автор: Baptiste Bessiere, Guy Simonnet, Jan Pype
Принадлежит: LAir Liquide SA pour lEtude et lExploitation des Procedes Georges Claude

The invention relates to a gaseous inhalable medicament containing xenon or N 2 O as active ingredient for use by inhalation for preventing and/or for treating neuropathic pain or pains caused by at least one cancer chemotherapy substance administered to a patient suffering from cancer, in particular a patient suffering from breast cancer, lung cancer, ovarian cancer, prostate cancer, colon cancer, rectal cancer or a gastric cancer or cancer of the upper aerodigestive tracts. The cancer chemotherapy substance contains one or more compounds chosen from platinum salts, taxanes, alkaloids, thalidomide and bortezomib, in particular paclitaxel, docetaxel or oxaliplatin. The effective volume proportion of nitrous oxide or of xenon is between 5 and 70%.

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Номер записи: 18
06-06-2013 дата публикации

Topical pharmaceutical composition comprising flurbiprofen

Номер: US20130143831A1
Автор: Koral Embil, Ray Figueroa
Принадлежит: Edko Pazarlama Tanitim Ticaret Ltd Sirketi

The invention provides topical pharmaceutical compositions comprising flurbiprofen, or a pharmaceutically acceptable derivative thereof, in combination with a solubilising system which comprises at least one glycol ether and at least one glycol ester. These are suitable for treating any condition associated with pain, inflammation and/or stiffness, for example sub-dermal pain in the joints or soft tissue.

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Номер записи: 19
27-06-2013 дата публикации

Composition and method for compounded therapy

Номер: US20130165430A1
Автор: Charles D. Hodge, II Jay Richard Ray
Принадлежит: JCDS Holdings LLC

The present embodiments relate to topically delivered compounded medications. A transdermal cream may provide the effective topical administration of multiple medications simultaneously. The transdermal cream may include low concentrations of local anesthetics, a NSAID, an anticonvulsant, and/or other active ingredients. For instance, the transdermal cream may include lidocaine, prilocaine, meloxicam, and lamotrigine and/or topiramate. Alternatively, the transdermal cream may include a lidocaine/prilocaine base cream to which is added a fine powder of one or more ground up medications to form a compounded medication. The compounded medication in powder form may be generated from grinding up tablets of NSAIDs, anticonvulsants, nerve depressants, antidepressants, muscle relaxants, NMDA receptor antagonists, opiate or opioid agonists, and/or other agents. The compounded medication in powder form may include meloxicam, lamotrigine, topiramate, and/or other active ingredients. In another aspect, the present embodiments relate to methods of compounding medications and transdermal creams or gels.

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Номер записи: 20
04-07-2013 дата публикации

Method and composition for prolonging analgesic effect of local anesthetic

Номер: US20130172387A1
Автор: Yu-Chun Hung
Принадлежит: MACKAY MEMORIAL HOSPITAL

Disclosed herein is a method for prolonging analgesic effect of a membrane permeable local anesthetic in a subject in need thereof. The method uses cinnamaldehyde as an adjuvant which, when administered prior to or simultaneously with the administration of a local anesthetic, prolongs the analgesic effect of the local anesthetic. Also disclosed herein is a method for providing analgesic effect in a subject in need thereof. The method uses cinnamaldehyde as an analgesic compound which, when administered alone to the subject in an analgesically effective amount, provides the analgesic effect.

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Номер записи: 21
11-07-2013 дата публикации

Method for formulating large diameter synthetic membrane vesicles

Номер: US20130177637A1
Автор: Ernest George Schutt, Kathleen D.A. Los, Peter Andrew Walters, Ronald Warren Mcguire
Принадлежит: Pacira Pharmaceuticals Inc

The present invention generally relates to the field of pharmaceutical sciences. More specifically, the present invention includes apparatus and devices for the preparation of pharmaceutical formulations containing large diameter synthetic membrane vesicles, such as multivesicular liposomes, methods for preparing such formulations, and the use of specific formulations for therapeutic treatment of subjects in need thereof. Formation and use of the pharmaceutical formulations containing large diameter synthetic membrane vesicles produced by using the apparatus and devices for therapeutic treatment of subjects in need thereof is also contemplated.

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Номер записи: 22
11-07-2013 дата публикации

Xenon-based anesthetic gas composition usable during an endarterectomy involving the clamping of the carotid artery

Номер: US20130177654A1
Автор: Catherine Billoet, Yannick Le Manach
Принадлежит: Air Liquide Sante International SA

The invention relates to a xenon-based anesthetic gas composition to be used, via inhalation, to maintain or preserve cerebral perfusion during an endarterectomy involving the clamping of the carotid artery in a mammal under general anesthesia. The xenon is preferably used in combination with at least one injectable anesthetic morphine agent such as remifentanil, sulfentanil, fentanyl, and alfentanil. Advantageously, the xenon is mixed with an oxygen-containing gas and administered to the patient after the patient has been anesthetized, put to sleep, and intubated. The use of xenon makes it possible to achieve a reduction in the pressure gradient during the clamping of the internal carotid artery relative to the usual anesthetic agents, and to achieve stable hemodynamics.

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Номер записи: 23
18-07-2013 дата публикации

Method for formulating large diameter synthetic membrane vesicles

Номер: US20130183372A1
Автор: Ernest George Schutt, Kathleen D.A. Los, Peter Andrew Walters, Ronald Warren Mcguire
Принадлежит: Pacira Pharmaceuticals Inc

The present invention generally relates to the field of pharmaceutical sciences. More specifically, the present invention includes apparatus and devices for the preparation of pharmaceutical formulations containing large diameter synthetic membrane vesicles, such as multivesicular liposomes, methods for preparing such formulations, and the use of specific formulations for therapeutic treatment of subjects in need thereof. Formation and use of the pharmaceutical formulations containing large diameter synthetic membrane vesicles produced by using the apparatus and devices for therapeutic treatment of subjects in need thereof is also contemplated.

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Номер записи: 24
01-08-2013 дата публикации

Gantrez Hydrogel With Dry Tack

Номер: US20130195771A1
Автор: Michael J. Borja
Принадлежит: Individual

A Gantrez hydrogel comprising sodium, calcium, zinc, strontium, and ferric cations, and a polyvinylpyrrolidone based tack agent is disclosed. A method for preparation of the Gantrez hydrogel is also disclosed.

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Номер записи: 25
17-10-2013 дата публикации

Chemical Compounds

Номер: US20130274243A1
Автор: Alan Daniel Brown, Brian Edward Marron, Christopher William West, Duncan Charles Miller, Laia MALET SANZ, Mark Ian Kemp, Mark J. Suto, Sarah Elizabeth Skerratt, Sharanjeet Kaur Bagal, Wolfgang Klute
Принадлежит: Pfizer Ltd

The invention relates to benzimidazole and imidazopyridine derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new Na v 1.8 modulators of formula (I) or pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , X and Y are as defined in the description. Na v 1.8 modulators are potentially useful in the treatment of a wide range of disorders, particularly pain.

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Номер записи: 26
31-10-2013 дата публикации

Drug Delivery System And Method For Conscious Sedation/Analgesia

Номер: US20130284168A1
Автор: C. Curtiss Mancuso, Gianluca PULITI, John C. McNeirney, Ross C. Terrell, Thelissa Isaac, William H. Burns, Jr.
Принадлежит: Piramal Critical Care Inc

Inhalant anesthetics are developed with a number of properties including rapid onset and recovery, controllability, and, ideally, a broad safety profile. The efficacy of these agents is measured by their ability to create anesthesia within the framework of the other desirable properties. The instant invention focuses on the dosage level where analgesia occurs but amnesia or lack of consciousness does not. In addition to identifying the dosage level where pain is sharply reduced or eliminated but awareness remains, a delivery system for safe and effective delivery of the agent is described.

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Номер записи: 27
16-01-2014 дата публикации

Solid dosage formulations of narcotic drugs having improved buccal adsorption

Номер: US20140018392A1
Автор: Federico Stroppolo, Shahbaz Ardalan
Принадлежит: ALPEX PHARMA SA

Disclosed is a pharmaceutical composition in the form of a tablet suitable for dissolution in the buccal cavity, said composition comprising i) an effective amount of a narcotic active ingredient, and ii) a pharmaceutically acceptable amine having a pK of about 8 or greater, wherein the molar ratio of amine:active ingredient is at least about 5:1.

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Номер записи: 28
06-02-2014 дата публикации

Analgesic method

Номер: US20140039040A1
Автор: Ping-Heng TAN
Принадлежит: I-SHOU UNIVERSITY

An analgesic medication includes an oligonucleotide being a double strand RNA comprising 18 to 70 base pairs, and a pharmaceutical acceptable vehicle for delivering the said oligonucleotide into cells, wherein a dosage of the oligonucleotide in the analgesic is 50 μg to 200 μg/kg per time, and the pharmaceutical acceptable vehicle is selected from a group of polyethyleneimine, lipofectamine and iFect.

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Номер записи: 29
06-03-2014 дата публикации

Aerosol Forming Device For Use In Inhalation Therapy

Номер: US20140060532A1
Автор: Craig C. Hodges, Daniel D. Rogers, Daniel Mufson, Martin J. Wensley, Peter M. Lloyd
Принадлежит: Alexza Pharmaceuticals Inc

The present invention relates to the inhalation delivery of aerosols containing small particles. Specifically, it relates to a device that forms drug containing aerosols for use in inhalation therapy. In a device aspect of the present invention, a device for delivering drug containing aerosols for inhalation therapy is provided. The device includes a housing and an airway that has a gas/vapor mixing airway. The airway further includes a subassembly, which has a metallic substrate coated on its surface with a composition comprising a drug.

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Номер записи: 30
14-01-2021 дата публикации

ANTISEPTIC COMPOSITION COMPRISING UNITHIOL AND DIMETHYLSULFOXIDE, USE OF THE COMPOSITION AND METHOD OF WOUND TREATMENT WITH ITS USE

Номер: US20210008006A1
Автор: AFINOGENOV Gennady Evgenievich, AFINOGENOVA Anna Gennadievna, MANASHEROV Tamaz Omarovich, MATELO Svetlana Konstantinovna
Принадлежит:

Colloidal antiseptic compositions for treating wounds and/or for use in surgical operations are provided. The compositions form an elastic air- and water-permeable biodegradable film on the wound surface and have antiseptic, hemostatic, anti-inflammatory, wound-healing, and especially anesthetic and antitoxic effects. The compositions include a collagen hydrolysate, one or more salts of alginic acid and one or more antiseptics, and additionally include unithiol and dimethylsulfoxide. The compositions may also optionally include one or more anesthetics. 1. An antiseptic composition comprising a collagen hydrolysate , one or more pharmaceutically acceptable salts of alginic acid , one or more antiseptics , unithiol , dimethylsulfoxide , and a pharmaceutically acceptable aqueous carrier.2. The composition according to claim 1 , wherein the amount of unithiol is about 0.1 to about 10 wt % based on the total weight of the composition.3. The composition according to claim 1 , wherein the amount of dimethylsulfoxide is about 0.05 to about 5 wt % based on the total weight of the composition.4. The composition according to claims 1 , further comprising one or more anesthetics.5. The composition according to claim 4 , wherein one or more of the anesthetics is selected from the group consisting of lidocaine claim 4 , trimecaine claim 4 , tetracaine claim 4 , novocaine and a combination thereof.6. The composition according to claim 4 , wherein the amount of one or more anesthetics is about 0.01 to about 10 wt % based on the total weight of the composition.7. (canceled)8. The composition according to claim 1 , wherein the pharmaceutically acceptable carrier includes an aqueous solution of sodium hypochlorite.9. The composition according to claim 1 , wherein said one or more antiseptics are selected from the group consisting of oxyquinoline derivatives claim 1 , quaternary ammonium compounds claim 1 , silver-based antiseptics claim 1 , biguanides claim 1 , bisphenols claim 1 , ...

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Номер записи: 31
14-01-2021 дата публикации

CANNABIS COMPOSITIONS AND METHODS

Номер: US20210008139A1
Автор: Gignac Marcel, Morgan David, Price Evan, Walser Lennie
Принадлежит:

A composition comprises an extract from a first plant tissue and an extract from a second plant tissue.

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Номер записи: 32
10-01-2019 дата публикации

DELIVERY SYSTEMS FOR PROPOFOL

Номер: US20190008770A1
Автор: ASERIN Abraham, GARTI LEVI Sharon, GARTI Nissim, PERLSTEIN My
Принадлежит: YISSUM Research Development Company of the Hebrew University of Jerusalem LTD.

Provided is a novel dilutable delivery systems and propofol microemulsions suitable for intravenous delivery of propofol. 178.-. (canceled)79. A propofol-microemulsion comprising an oil phase in the form of oil droplets dispersed in an aqueous diluent continuous phase , wherein the oil phase comprises propofol , at least one surfactant comprising polyethylene glycol 15-hydroxystearate (Solutol HS 15) , at least one solvent comprising medium-chain triglycerides (MCT) , at least one co-surfactant , and at least one co-solvent , the oil droplets having a size of at most 20 nm in the continuous phase , the propofol and the surfactant having diffusion coefficients having the same order of magnitude when in the microemulsion (as measured by SD-NMR) , and the microemulsion being suitable for parenteral administration.80. The propofol-microemulsion of claim 79 , wherein the diffusion coefficients of propofol and the surfactant (when in the microemulsion) are at least of one order of magnitude smaller than the other components of the microemulsion.81. The propofol-microemulsion of claim 79 , wherein the diffusion coefficients of propofol and the surfactant (when in the microemulsion) are of an order of magnitude of 1×10m/sec claim 79 , when in the microemulsion claim 79 , as measured by SD-NMR.82. The propofol-microemulsion of claim 79 , wherein the polydispersity index (PDI) of the distribution of oil droplets is between about 0.03 and 0.08.83. The propofol-microemulsion of claim 79 , wherein the oil droplets size is between about 10 and 20 nm.84. The propofol-microemulsion of claim 79 , wherein said diluent is selected from water claim 79 , water for injection claim 79 , saline claim 79 , dextrose solution claim 79 , or a buffer having a pH between 3 and 9.85. The propofol-microemulsion of claim 79 , wherein the co-surfactant is different from said surfactant and is selected from polyols claim 79 , diglycerides claim 79 , polyoxyethylenes claim 79 , lecithins and ...

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Номер записи: 33
27-01-2022 дата публикации

Ion channel modulators

Номер: US20220024930A1
Автор: Andrew Mark Griffin, Brian Edward Marron, Gabriel Martinez Botella
Принадлежит: Praxis Precision Medicines Inc

The present invention is directed to, in part, fused heteroaryl compounds and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel including neurological disorders (e.g., Dravet syndrome, epilepsy), pain, and neuromuscular disorders are also provided herein.

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Номер записи: 34
17-01-2019 дата публикации

Pharmaceutical formulation

Номер: US20190015329A1
Автор: Mahmoud El-Tamimy
Принадлежит: Phosphagenics Ltd

The present invention relates to a formulation comprising a primary surfactant, a tocol phosphate, water, an active agent, and optionally an oil, wherein the active agent and/or the optional oil comprises a hydrophobic phase.

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Номер записи: 35
28-01-2016 дата публикации

Devices and methods for delivering particles

Номер: US20160022910A1
Автор: Victor K. TSUI
Принадлежит: Powder Pharmaceuticals Inc

Systems, devices, and methods for delivering therapeutic particles are disclosed. In one variation, a device for delivering particles includes a gas supply configured for supplying gas under pressure, a particle cassette comprising the particles, a cassette housing, and a cassette membrane. The cassette housing can comprise an Ethylene Vinyl Acetate (EVA) copolymer of 18% to 28% by weight of Vinyl Acetate (VA). The device can also include a safety interlock to prevent or minimize the risk that the device will be unintentionally activated. The device can also have a silencer.

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Номер записи: 36
28-01-2021 дата публикации

HEXADECAHYDRO-1H-CYCLOPENTA[A]PHENANTHRENE DERIVATIVES USEFUL IN TREATING PAIN AND INFLAMMATION

Номер: US20210024571A1
Автор: CROSS Jennifer, Harwig Curtis, IYANAR Karthikeyan, Keregadde Mahesh Narayan, KHER Samir Satish, Pettigrew Jeremy D., SEENISAMY Jeyaprakashnarayanan
Принадлежит: AQUINOX PHARMACEUTICALS (CANADA) INC.

wherein, R, R, R, R, Rand Rare described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable salt or solvate thereof, are described herein, as well as other compounds. These compounds are useful in treating inflammation and/or pain. Compositions comprising a compound of the invention are also disclosed, as are methods of using the compounds to treat inflammation and/or pain. 6. The compound of selected from:(1R,3aS,3bS,4R,5R,5aS,10aR,10bS,12aR)-8-amino-10a,12a-dimethyl-1-((R)-6-methylheptan-2-yl)-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-d]thiazole-4,5-diol(1S,3aS,3bR,4R,5R,5aS,10aR,10bS,12aS)-1,10a,12a-trimethyl-1,2,3,3a,3b,4,5,5a,6,7,10,10a,10b,11,12,12a-hexadecahydrocyclopenta[5,6]naphtho[1,2-f]indazole-1,4,5-triol;(3aS,3bR,4R,5R,5aS,10aR,10bS,12aR)-10a,12a-dimethyl-3,3a,3b,4,5,5a,6,7,10,10a,10b,11,12,12a-tetradecahydrocyclopenta[5,6]naphtho[1,2-f]indazole-4,5-diol;(2R,3bR,4R,5R,5aS,10aR,10bS)-1,1,10a-trimethyl-1,2,3,3b,4,5,5a,6,7,10,10a,10b,11,12-tetradecahydrocyclopenta[5,6]naphtho[1,2-]indazole-2,4,5-triol;(1R,3aS,3bS,4R,5R,5aS,10aR,10bS,12aR)-1-((2S,5R)-5-ethyl-3-hydroxy-6-methylheptan-2-yl)-10a,12a-dimethyl-1,2,3,3a,3b,4,5,5a,6,7,10,10a,10b,11,12,12a-hexadecahydrocyclopenta[5,6]naphtho[1,2-f]indazole-4,5-diol;(1R,3aS,3bS,4R,5R,5aS,10aR,12aR)-10a,12a-dimethyl-1-((R)-6-methylheptan-2-yl)-1,2,3,3a,3b,4,5,5a,6,7,10,10a,10b,11,12,12a-hexadecahydrocyclopenta[5,6]naphtho[1,2-f]indazole-4,5-diol;(1R,3aS,3bS,4R,5R,5aS,10aR,10bS,12aR)-10a,12a-dimethyl-1-((R)-6-methylheptan-2-yl)-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[2,3-d][1,2,3]thiadiazole-4,5-diol;(1R,3aS,3bS,4R,5R,5aS,10aR,10bS,12aR)-10a,12a-dimethyl-1-((R)-6-methylheptan-2-yl)-2,3,3a,3b,4,5,5a,6,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[3,2-d]isoxazole-4,5-diol; or(1R,3aS,3bS,4R,5R,5aS,10aR,10bS,12aS)-10a,12a-dimethyl-1-(prop-1-en-2-yl)-1,2,3 ...

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Номер записи: 37
17-02-2022 дата публикации

LONG ACTING IN-SITU FORMING/GELLING COMPOSITIONS

Номер: US20220047566A1
Автор: HE Chang, Li Yunhua, Nekkanti Vijay Kumar, Tang Zhiwen, YANG Jun, Yue Baohua
Принадлежит:

The present invention provides sustained release formulations comprising one or more active pharmaceutical ingredient(s); at least one biocompatible polymer excipient; and at least one biocompatible solvent; methods for preparing the sustained release formulations, and methods for treating localized pain in a subject in need thereof. 1. A sustained release formulation , the sustained release formulation comprises:a. one or more active pharmaceutical ingredient(s);b. at least one biocompatible polymer excipient; andc. at least one biocompatible solvent;wherein one of the active pharmaceutical ingredients has a particle size distribution ranging from about 0.5 μm to about 100.0 μm.2. The sustained release formulation of claim 1 , wherein the one or more pharmaceutical ingredient(s) is an anesthetic drug claim 1 , an anti-inflammatory drug claim 1 , an antiemetic drug claim 1 , or a combination thereof.3. The sustained release formulation of claim 2 , wherein the one or more active pharmaceutical ingredient(s) comprise bupivacaine claim 2 , ropivacaine claim 2 , levobupivacaine claim 2 , lidocaine claim 2 , buprenorphine claim 2 , celecoxib claim 2 , meloxicam claim 2 , dexamethasone claim 2 , betamethasone claim 2 , betamethasone-21-acetate claim 2 , triamcinolone acetonide claim 2 , nepafenac claim 2 , aprepitant claim 2 , cox 1 inhibitors claim 2 , cox 2 inhibitors claim 2 , rolapitant claim 2 , fosaprepitant claim 2 , granisetron claim 2 , ondansetron claim 2 , palonosetron claim 2 , prochlorperazine claim 2 , hyaluronic acid claim 2 , sodium hyaluronate claim 2 , cross-linked derivatives of hyaluronic acid claim 2 , or a combination thereof.4. The sustained release formulation of claim 1 , wherein the at least one biocompatible polymer excipient comprises hyaluronic acid claim 1 , sodium hyaluronate claim 1 , cross-linked derivatives of hyaluronic acid claim 1 , PEG 3350 claim 1 , PEG 4000 claim 1 , polyethylene oxide (PolyOX) claim 1 , methylcellulose claim 1 , ...

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Номер записи: 38
31-01-2019 дата публикации

Adsorption of fluorinated anesthetics within the pores of molecular crystals

Номер: US20190030167A1
Автор: Ognjen MILJANIC, Teng-Hao CHEN, Watchareeya KAVEEVIVITCHAI
Принадлежит: UNIVERSITY OF HOUSTON SYSTEM

A method of delivering or sequestering anesthetic agents by adsorption of such agents by porous partially fluorinated compounds which display high weight adsorption capacities.

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Номер записи: 39
17-02-2022 дата публикации

OXYSTEROLS AND METHODS OF USE THEREOF

Номер: US20220048943A1
Автор: Harrison Boyd L., Martinez Botella Gabriel, Robichaud Albert Jean, Salituro Francesco G.
Принадлежит:

Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R, R, and Rare as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions. 2. (canceled)3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris substituted Calkyl.4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris unsubstituted Calkyl.5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —CH claim 1 , —CF claim 1 , —CHOCH claim 1 , —CH(CH)(CF) claim 1 , —CHCH claim 1 , or —CH(CH).6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —CHor —CHCH.7. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris unsubstituted Calkyl.8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris substituted or unsubstituted ethyl claim 1 , substituted or unsubstituted isopropyl claim 1 , or substituted or unsubstituted tert-butyl.911-. (canceled)12. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein represents a single bond.1617-. (canceled)2021-. (canceled)23. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.24. A method of inducing sedation or anesthesia comprising administering to a subject an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or a pharmaceutical composition thereof.25. A method for treating a disorder claim 1 , comprising administering to a subject in need thereof an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or a pharmaceutical composition thereof; wherein the disorder is a gastrointestinal (GI) disorder ...

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Номер записи: 40
30-01-2020 дата публикации

LOCAL ANESTHETIC-CONTAINING ACIDIC EMULSION COMPOSITION

Номер: US20200030305A1
Автор: Chida Yuichiro, Masui Kuniharu, Nomura Mai, Okamoto Kazuki
Принадлежит:

An object of the present invention is to provide a local anesthetic-containing composition characterized by (1) exerting immediate and long-lasting medicinal effect without sustained release after administration, and/or (2) having storage stability. 1. An O/W type acidic emulsion composition comprising a local anesthetic and a fatty acid ester containing an ester-bonded fatty acid having 6 to 12 carbon atoms.216-. (canceled)17. The acidic emulsion composition according to claim 1 , wherein the fatty acid ester is a glyceride.18. The acidic emulsion composition according to claim 1 , wherein the local anesthetic is an amide-type local anesthetic.19. The acidic emulsion composition according to claim 1 , wherein the local anesthetic is selected from the group consisting of levobupivacaine claim 1 , bupivacaine claim 1 , ropivacaine claim 1 , salts thereof claim 1 , and any combination thereof.20. The acidic emulsion composition according to claim 17 , wherein the glyceride is one or more fatty acid glycerides comprising one or more fatty acids having 6 to 12 carbon atoms as a constituent fatty acid claim 17 , and is selected from the group consisting of a fatty acid monoglyceride claim 17 , a fatty acid diglyceride and a fatty acid triglyceride.21. The acidic emulsion composition according to claim 1 , wherein the emulsion composition has a pH of 3 or higher but lower than 7.0.22. The acidic emulsion composition according to claim 1 , wherein the emulsion composition has a pH of 3 to 6.5.23. The acidic emulsion composition according to claim 1 , wherein the emulsion composition has a pH of 3 to 6.0.24. The acidic emulsion composition according to claim 1 , further comprising EDTA.25. The acidic emulsion composition according to claim 1 , further comprising a long-chain fatty acid glyceride.26. The acidic emulsion composition according to claim 1 , wherein the proportion of the local anesthetic in an aqueous phase is 15% or more of the total amount of the local ...

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Номер записи: 41
25-02-2021 дата публикации

Cooling Composition and Method of Use

Номер: US20210052495A1
Автор: Olsson Charles Robert
Принадлежит:

A sprayable cooling composition comprising at least one refrigerant (DME) as well as at least one non-volatile antiseptic agent (cetrimide), wherein the cooling composition is capable of eliciting both a local refrigerant effect to a body surface area to which it is applied and providing antisepsis due to the non-volatile antiseptic agent remaining on the body surface area. The composition is useful for surgical and animal husbandry procedures, such as piglet castration. 120.-. (canceled)21. A sprayable cooling composition comprising at least one refrigerant as well as at least one non-volatile antiseptic agent , wherein the cooling composition is capable of eliciting both a local refrigerant effect to a body surface area to which it is applied and providing antisepsis due to the non-volatile antiseptic agent remaining on the body surface area.22. The composition of claim 21 , wherein the cooling composition comprises anywhere between approximately 20% (w/w) and approximately 80% (w/w) of said at least one refrigerant.23. The composition of claim 21 , wherein the cooling composition comprises anywhere between approximately 1% and approximately 5% weight/weight of said at least one non-volatile antiseptic agent.24. The composition of claim 21 , wherein the at least one refrigerant comprises one or more refrigerants selected from the group consisting of:a compressed gas;a liquefied hydrocarbon;a fluorinated hydrocarbon;an ether; anda hydrofluoroalkane.25. The composition of claim 21 , wherein the at least one refrigerant is dimethyl ether (DME).26. The composition of claim 21 , wherein the at least one non-volatile antiseptic agent is one or more antiseptic agents selected from the group consisting of: cetrimide; povidone-iodine; chlorhexidine; iodine; benzalkonium chloride; benzoic acid; nitrofurazone; benzoyl peroxide; hydrogen peroxide; hexachlorophene; phenol; resorcinol; cetylpyridinium chloride; chlorhexidine gluconate; and parachoroxylenol.27. The composition ...

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Номер записи: 42
25-02-2021 дата публикации

COMPOSITIONS AND METHODS FOR PAIN MANAGEMENT

Номер: US20210052602A1
Автор: Bonner Dennis J.
Принадлежит:

Disclosed herein, in part, are pharmaceutical compositions comprising an opioid agonist such as codeine or a pharmaceutically acceptable salt thereof, hydroxyzine or a pharmaceutically acceptable salt thereof, a gabapentinoid, optionally a 5-HT3 antagonist and a pharmaceutically acceptable excipient. Methods of treating neuropathic and nociceptive pain comprising administering a disclosed pharmaceutical composition to a subject in need thereof is also provided herein 1. A pharmaceutical composition comprising:codeine or a pharmaceutically acceptable salt thereof;hydroxyzine or a pharmaceutically acceptable salt thereof;a gabapentinoid;optionally a 5-HT3 antagonist; anda pharmaceutically acceptable excipient.2. The pharmaceutical composition of claim 1 , wherein the 5-HT3 antagonist is present and is selected from the group consisting of ondansetron or a pharmaceutically acceptable salt thereof claim 1 , tropisetron claim 1 , granisetron claim 1 , dolasetron claim 1 , palonosetron claim 1 , ramosetron claim 1 , galanolactone claim 1 , mirtazapine claim 1 , olanzapine claim 1 , cisapride claim 1 , renzapride and metoclopramide.3. (canceled)4. The pharmaceutical composition of claim 2 , wherein the 5-HT3 antagonist is ondansetron or a pharmaceutically acceptable salt thereof.5. The pharmaceutical composition of claim 1 , wherein the gabapentinoid is selected from the group consisting of gabapentin or a pharmaceutically acceptable salt thereof claim 1 , gabapentin encarbil claim 1 , and atagabalin.6. (canceled)7. The pharmaceutical composition of claim 1 , comprising gabapentin and ondansetron HCl.8. The pharmaceutical composition of claim 1 , further comprising a stool softener and/or a constipation agent claim 1 , wherein the stool softener or constipation agent is docusate or a pharmaceutically acceptable salt thereof claim 1 , or naloxegol.9. (canceled)10. (canceled)11. (canceled)12. (canceled)13. (canceled)14. (canceled)15. The pharmaceutical composition of claim 1 ...

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Номер записи: 43
10-03-2022 дата публикации

Pharmaceutical compositions for use in treating pain

Номер: US20220071934A1
Автор: Carl Oscar BROWN, Hao-Wen Kao, Hui-ting WANG, Keelung Hong, Min-Wen Kuo, Pei-Hsien HU, Sheue-Fang Shih, Tien-Tzu TAI, Wan-ni YU, Weenee Yeun Ng JAO, Yi-Yu Lin, Yun-Long TSENG
Принадлежит: Taiwan Liposome Co Ltd, TLC Biopharmaceuticals Inc

Provided is a pharmaceutical composition for use in treating postsurgical pain. The pharmaceutical composition comprises a lipid-based complex. The lipid-based complex comprises an amide-type anesthetic and at least one lipid, wherein a molar ratio of the amide-type anesthetic to the at least one lipid of the lipid-based complex is at least 0.5:1. The total amount of the amide-type anesthetic is at least 1.5 to 5 times of a standard therapeutic dose for treating postsurgical pain with the amide-type anesthetic to achieve an improved pain control with desired prolonged analgesic effect.

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Номер записи: 44
10-03-2022 дата публикации

GEL COMPOSITION WITH AN ANAESTHETIC EFFECT OF SHORT AND LONG TERM DURATION

Номер: US20220071973A1
Автор: PACHECO DOS SANTOS DIAS José António
Принадлежит:

The present invention is enclosed in the medical area, specifically within the area of lubricant gels for trans-urethral procedures, referring to a gel pharmaceutical composition with an anaesthetic effect of short and long duration, for being administered through the urethra. It is an object of the present invention a gel composition with an anaesthetic effect of short and long term duration for administration through the urethra which comprises a lubricant gel, at least one local short duration anaesthetic composition and at least one local long duration anaesthetic composition which comprises ropivacaine or bupivacaine. The presence of between a long-acting anaesthetic composition in the lubricant gel of the present invention, combined with a short-term acting anaesthetic composition, provides an enormous asset to existing products, because of the immediate and substantially superior and longer-lasting well-being of patients. Advantageously, it is for use as a local anaesthetic with short and long term duration. 1. A gel composition with an anaesthetic effect of short and long term duration for administration through the urethra characterised in that it comprises a lubricant gel , at least one local short duration anaesthetic composition and at least one local long duration anaesthetic composition , the local long duration anaesthetic composition comprising ropivacaine and/or bupivacaine , the ratio between the w/w percentage of the local long duration and short anaesthetic compositions being such that the effect of the local long duration anaesthetic composition overlaps with the effect of the local short duration anaesthetic composition.2. A gel composition according to the previous claim wherein the local long duration anaesthetic composition specifically comprises ropivacaine hydrochloride and/or bupivacaine hydrochloride.3. A gel composition according to the previous claim wherein the local long duration anaesthetic composition specifically consists of ...

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Номер записи: 45
04-03-2021 дата публикации

DEVICES AND SYSTEMS FOR TREATING PAIN BASED ON LIGHT THERAPY

Номер: US20210060355A1
Автор: Ibrahim Mohab M., Khanna Rajesh
Принадлежит:

Devices and systems for treating based on light therapy are disclosed. One example device includes an eyewear configured for placement in front of an eye to allow light to reach the eye, and one or more filters having transmission spectra within a range that approximately spans 450 to 570 nm associated with blue or green light. The one or more filters is configured to block light spectra outside of said range and to allow the blue or green light to reach the eye for administering light therapy to a subject exhibiting pain. 120-. (canceled)21. A device for facilitating pain treatment through light therapy , comprising:an eyewear configured for placement in front of an eye to allow light to reach the eye; andone or more filters having transmission spectra within a range that approximately spans 450 to 570 nm associated with blue or green light, whereinthe one or more filters is configured to block light spectra outside of said range and to allow the blue or green light to reach the eye for administering light therapy to a subject exhibiting pain.22. The device of claim 21 , wherein the eyewear is a pair of goggles.23. The device of claim 22 , wherein the eyewear is a pair of ski goggles.24. The device of claim 21 , wherein the eyewear is a pair of eyeglasses.25. The device of claim 21 , wherein the eyewear is a contact lens.26. The device of claim 21 , wherein the transmission spectra of the one or more filters is within a range that allows only the green light to pass therethrough.27. The device of claim 21 , wherein the one or more filters enable administering light therapy using light having broader spectra than the range 450 to 570 nm while allowing the blue or green light to be administered to the eye due to blockage of unwanted light spectra.28. The device of claim 21 , wherein the light having the broader spectra includes one or more of: a white fluorescent light claim 21 , sunlight after passing through a glass window claim 21 , or a white light emitting diode ...

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Номер записи: 46
20-02-2020 дата публикации

ENHANCED SOLUBILITY DRUG-CONTAINING FORMULATIONS

Номер: US20200054754A1
Автор: HURREY Michael Laird, Noymer Peter, OSTOVIC Drazen
Принадлежит:

This invention describes compositions comprising at least 75 mg/mL of solubilized otherwise poorly soluble drug in an aqueous environment, wherein the composition further comprises a combination of 3 or more acids. Methods of providing analgesia, anti-pyretic effects or reducing pain in a subject presenting with a pain condition, and methods of reducing administration site irritation, inflammation or a combination thereof in a subject presenting with a pain condition, comprising the steps of administering such compositions and infusion pumps containing such compositions are also described. 1. A composition comprising at least 75 mg/mL of solubilized otherwise poorly soluble drug in an aqueous environment further comprising a combination of 3 or more acids.2. The composition of claim 1 , wherein said combination of 3 or more acids is selected from the group consisting of acetic claim 1 , phosphoric claim 1 , hydrochloric and sulfuric acids.3. The composition of claim 1 , wherein said combination of 3 or more acids is selected from the group consisting of acetic claim 1 , phosphoric claim 1 , hydrochloric claim 1 , sulfuric claim 1 , and citric acids.4. The composition of claim 1 , wherein said composition comprises a combination of four or more acids.5. The composition of claim 4 , wherein said composition comprises a combination of four acids.6. The composition of claim 1 , wherein said otherwise poorly soluble drug is in free-base form.7. The composition of claim 1 , wherein said otherwise poorly soluble drug is an anesthetic.8. The composition of claim 1 , wherein said otherwise poorly soluble drug is bupivacaine claim 1 , ropivacaine claim 1 , mepivacaine claim 1 , levobupivacaine claim 1 , procaine claim 1 , chloroprocaine claim 1 , etidocaine claim 1 , prilocaine or tetracaine.9. The composition of claim 1 , wherein said otherwise poorly soluble drug is bupivacaine or ropivacaine.10. The composition of claim 9 , wherein said drug is bupivacaine and said ...

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Номер записи: 47
04-03-2021 дата публикации

7-MEMBERED AZA-HETEROCYCLIC CONTAINING DELTA-OPIOID RECEPTOR MODULATING COMPOUNDS, METHODS OF USING AND MAKING THE SAME

Номер: US20210061812A1
Автор: DAUBERT Tamara Ann MISKOWSKI, HAWKINS Michael John, Herr Robert Jason, Kargbo Robert Borbo, Liu Guodong, PITIS Philip Michael, Romero Donna, SPEERSCHNEIDER Aimee CROMBIE, YAMASHITA Dennis SHINJI, Yuan Catherine C.K.
Принадлежит:

The present embodiments are directed, in part, to compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof for modulating the activity of delta opioid receptor, biased and/or unbiased, and/or methods for treating pain, migraines, headaches, depression, Parkinsons Disease, anxiety, and/or overactive bladder, and other disorders and conditions described herein or any combination thereof. 3. The compound of claim 1 , wherein Y is O.4. The compound of claim 3 , wherein Ris a bond claim 3 , a —C(═O) claim 3 , optionally substituted C-Cbranched or unbranched alkyl.510-. (canceled)11. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Zis ethyl.12. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein when Xis N claim 1 , Xis C claim 1 , and when Xis C claim 1 , Xis N.13. (canceled)14. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris H claim 1 , optionally substituted C-Cbranched or unbranched alkyl claim 1 , —CHRor —CHCHR claim 1 , wherein Ris optionally substituted aryl claim 1 , optionally substituted haloalkyl claim 1 , optionally substituted ketone claim 1 , optionally substituted cycloalkyl claim 1 , optionally substituted C-Calkenyl claim 1 , optionally substituted C-Chaloalkenyl claim 1 , or optionally substituted heteroaryl.15. (canceled)16. The compound of claim 14 , or a pharmaceutically acceptable salt thereof claim 14 , wherein Ris cyclopropyl claim 14 , diflourocyclopropyl claim 14 , —CH═CF claim 14 , or 2 claim 14 ,2-diflourocyclopropyl.1719-. (canceled)20. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris H claim 1 , optionally substituted C-Cbranched or unbranched alkyl claim 1 , —CHRor —CHCHR claim 1 , and wherein Ris optionally substituted aryl claim 1 , optionally substituted haloalkyl claim 1 , optionally substituted ketone claim 1 , optionally ...

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Номер записи: 48
28-02-2019 дата публикации

AQUEOUS PHARMACEUTICAL FORMULATION COMPRISING PROPOFOL

Номер: US20190060232A1
Автор: MENGLER Christopher
Принадлежит: Cuda Anesthetics, LLC

Disclosed herein is an aqueous pharmaceutical formulation comprising about 10 mg/mL of propofol, 175 mg/mL of sulfobutylether β-cyclodextrin, a citric buffer, wherein the composition has a pH of about 5.5. Also disclosed is a method of inducing and maintaining anesthesia or sedation in a patient by administering the aqueous pharmaceutical formulation. 1. An aqueous pharmaceutical composition comprising about 10 mg/mL of propofol and 175 mg/mL of sulfobutylether β-cyclodextrin.2. The aqueous pharmaceutical composition of claim 1 , wherein the composition comprises citric acid.3. The aqueous pharmaceutical composition of claim 1 , wherein the sulfobutylether β-cyclodextrin is sulfobutylether 7β-cyclodextrin.4. The aqueous pharmaceutical composition of claim 3 , wherein the sulfobutylether β-cyclodextrin is Captisol®.5. An aqueous pharmaceutical composition according to claim 1 , wherein the composition further comprises a preservative claim 1 , an antioxidant claim 1 , a tonicity modifier claim 1 , a buffer claim 1 , an additional solubilizing agent claim 1 , or a combination thereof.6. The aqueous pharmaceutical composition of claim 1 , wherein the composition comprises less than 0.5% 4 claim 1 ,4′-dihydroxy-3 claim 1 ,3′ claim 1 ,5 claim 1 ,5′-tetraisopropyl-biphenyl.7. The aqueous pharmaceutical composition of claim 1 , wherein the composition comprises no more than 0.3% total degradation impurities upon storage at 25° C. for 6 months.8. An aqueous pharmaceutical composition comprising about 10 mg/mL of propofol claim 1 , 175 mg/mL of sulfobutylether β-cyclodextrin claim 1 , and wherein upon administration claim 1 , the composition provides to a patient a dose-normalized propofol plasma Cof about 5 to about 8 (ng/mL)/(mg/kg).9. The aqueous pharmaceutical composition of claim 8 , wherein the sulfobutylether β-cyclodextrin is sulfobutylether 7β-cyclodextrin.10. A pharmaceutical composition consisting essentially of about 10 mg/mL of propofol claim 8 , 175 mg/mL of ...

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Номер записи: 49
11-03-2021 дата публикации

IMPLANTABLE POLYMER DEPOTS FOR THE CONTROLLED RELEASE OF THERAPEUTIC AGENTS

Номер: US20210069101A1
Автор: Boyd Stephen W., Feldstein Michael, GIFFORD, HANCOCK Jackie Joe, III Hanson S., Lee Wei Li, Luo Jingnan, Mokarram-Dorri Nassireddin, Naga Karun D., Ruane Patrick H., Seet Daniel Boon Lim, Teu Koon Kiat, WANG HONGLEI
Принадлежит:

The present technology relates to depot assemblies for the controlled, sustained release of a therapeutic agent. The assembly can include a depot having a therapeutic region comprising a therapeutic agent, and a control region comprising a bioresorbable polymer and a releasing agent mixed with the polymer. The releasing agent may be configured to dissolve when the depot is placed in vivo to form diffusion openings in the control region. The depot may be configured to be implanted at a treatment site in vivo and, while implanted, release the therapeutic agent at the treatment site for no less than 3 days. 1. A depot for the treatment of postoperative pain via sustained , controlled release of an analgesic , comprising:a therapeutic region comprising the analgesic;a control region comprising a bioresorbable polymer and a releasing agent mixed with the polymer, wherein the releasing agent is configured to dissolve when the depot is placed in vivo to form diffusion openings in the control region; andwherein the depot is configured to be implanted at a treatment site in vivo and, while implanted, release the analgesic at the treatment site for no less than 7 days.2. The depot of claim 1 , wherein the analgesic in the therapeutic region comprises at least 50% of the total weight of the depot.3. The depot of claim 1 , wherein the depot is configured to release the analgesic at the treatment site for no less than 14 days.4. The depot of claim 3 , wherein about 20% to about 50% of the analgesic is released in the first about 3 to about 5 days of the 14 days claim 3 , and wherein at least 80% of the remaining analgesic is released in the last 11 days of the 14 days.5. The depot of claim 3 , wherein about 20% to about 40% of the analgesic is released in the first 3 days of the 14 days claim 3 , and wherein at least 80% of the remaining analgesic is released in the last 11 days of the 14 days.6. The depot of claim 3 , wherein at least 90% of the remaining analgesic is released ...

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Номер записи: 50
11-03-2021 дата публикации

PREPARATION OF (-)-COCAINE HYDROCHLORIDE

Номер: US20210069173A1
Автор: KIM Se-Ho, Yao Qingwei
Принадлежит:

Efficient methods are provided for large scale production of ethyl cocaine-free cocaine hydrochloride. Compositions and methods comprising administration of cocaine hydrochloride are provided. 1. A method of preparing (−)-cocaine hydrochloride , the method comprising:obtaining (+)-2-carbomethoxy-3-tropinone (2-CMT) bitartrate that had been produced by a method that does not employ ethanol;exposing the (+)-2-carbomethoxy-3-tropinone (2-CMT) bitartrate continuously supplied sodium mercury amalgam (Na—Hg) and sulfuric acid in an aqueous solution whereby the (+)-2-CMT bitartrate is converted to a mixture of compounds comprising (−)-ecognine methyl ester ((−)-EME) or a pharmaceutically acceptable salt thereof and pseudoecgonine methyl ester (PEM) or a pharmaceutically acceptable salt thereof, wherein a sodium salt of the sulfuric acid formed as a by-product is allowed to precipitate; andbenzoylating the (−)-EME or a pharmaceutically acceptable salt thereof to form (−)-cocaine or a pharmaceutically acceptable salt thereof; andadding hydrochloric acid to the (−)-cocaine base to form the (−)-cocaine hydrochloride.2. The method of claim 1 , further comprisingseparating the (−)-EME or pharmaceutically acceptable salt thereof from the PEM or a pharmaceutically acceptable salt thereof.3. The method of claim 2 , wherein the separating comprises dissolving the mixture of compounds comprising the (−)-EME and the PEM in isopropyl alcohol; adding methanolic HCl to form a solution mixture; and adding acetone to the solution mixture to form a heterogenous mixture claim 2 , wherein (−)-EME HCl precipitates from the mixture.4. The method of claim 2 , wherein the separating comprises stirring the mixture of compounds comprising the (−)-EME and the PEM in cyclohexane claim 2 , allowing the PEM to precipitate claim 2 , and filtering off the precipitated PEM.5. The method of claim 3 , wherein the solution mixture is at least partially evaporated and fresh isopropyl alcohol is added prior to ...

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Номер записи: 51
29-05-2014 дата публикации

Hyaluronic acid based formulations

Номер: US20140148406A1
Автор: Pierre F. Lebreton
Принадлежит: ALLERGAN INDUSTRIE SAS

Disclosed herein are soft tissue fillers, for example, dermal and subdermal fillers, based on low molecular weight hyaluronic acids and pharmaceutically acceptable salts thereof, and methods of manufacturing same.

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Номер записи: 52
24-03-2022 дата публикации

Linear polysaccharide based film products

Номер: US20220088201A1
Автор: Beuford Arlie Bogue, Eric Dadey, Garry L. Myers, Michael Li
Принадлежит: Aquestive Therapeutics Inc

Film products, especially suitable for oral delivery, which can be formed during manufacture in the form of large and/or heavy film strips or sheets and subsequently cut into uniform dosage units, each dosage unit being uniform in content and having distributed therein a linear polysaccharide, such as pullulan, a plasticizer, and an active component.

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Номер записи: 53
07-03-2019 дата публикации

Compositions and Methods for On-Demand High-Efficiency Triggerable Anesthesia

Номер: US20190070115A1
Автор: Cullion Kathleen J., Kohane Daniel S., Rwei Alina Y., ZHAN Changyou
Принадлежит:

Compositions and methods for administration of local anesthetics that are delivered by a single injection and enable repeated on-demand or high influx analgesia over extended periods have been developed. Pharmaceutical compositions including an effective amount of one or more sodium channel blockers including site 1 sodium channel blockers, optionally one or more alpha-2-adrenergic agonists, which are optionally encapsulated in liposomes, particles or microbubbles, and one or more triggerable elements are provided. The triggerable elements allow delivery of the encapsulated anesthetic drugs when an appropriate triggering stimuli are applied. Exemplary triggering agents or stimuli include near-infrared irradiation, UV- and visible light, ultrasound and magnetic field. In one embodiment, ultrasound is used to trigger a burst of microbubbles to enhance penetration of local anesthetic. 1. A pharmaceutical composition comprisingtriggerable liposomes, particles or microbubbles encapsulating at least one site I sodium channel blocker,wherein the site I sodium channel blocker is releasedupon exposing to a triggering agent in an amount effective to produce anesthesia.2. The pharmaceutical composition of claim 1 , wherein the triggering agent is selected from the group consisting of near-infrared irradiation claim 1 , ultraviolet and visible light claim 1 , ultrasound and magnetic field.3. The pharmaceutical composition of claim 1 , wherein the liposomes or particles contain one or more triggerable elements.4. The pharmaceutical composition of claim 3 , comprising liposomes claim 3 , wherein the triggerable elements are any material that disrupts membrane bilayer to release the encapsulated content in response to any of the triggering agents.5. The pharmaceutical composition of claim 1 , further comprising one or more alpha-2-adrenergic agonist claim 1 , local anesthetic or vasoconstrictor encapsulated in liposomes or particles.6. The pharmaceutical composition of claim 4 , ...

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Номер записи: 54
05-06-2014 дата публикации

Proteolytic extract from bromelain for the treatment of connective tissue disorders

Номер: US20140154229A1
Автор: Eilon Asculai, Guy RUBIN, Lior Rosenberg
Принадлежит: MediWound Ltd

The present invention relates to a proteolytic extract obtained from bromelain for the treatment of connective tissue diseases. In particular, the present invention relates to a pharmaceutical composition that includes proteolytic extract obtained from bromelain for the treatment of diseases such as Dupuytren's disease and Peyronie's disease.

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Номер записи: 55
18-03-2021 дата публикации

ANALGESIC FORMULATION FOR CONTROL OF PAIN IN DOGS

Номер: US20210077426A1
Автор: KuKanich Katherine, KuKanich Stanley, Locuson Charles W., Rankin David
Принадлежит:

Provided herein are treatments for reducing pain in dogs. The treatments generally comprise a combination of an opioid compound, such as methadone, and an azole compound, such as fluconazole. The treatments may further comprise an opioid abuse deterrent that advantageously inhibits opioid effects in humans while maintaining desirable analgesic effects in dogs. Additionally, the treatments provided herein avoid the undesirable side effects of prior art opioid treatments for dogs. The treatments may be administered as separate doses or in a single formulation product for improved compliance. The treatments have wide use potential in dogs from perioperative patients to inpatients and outpatients and may be used, for example, for sedation in minor procedures, analgesia, and decreasing temperature in canine patients. 1. A method of providing an analgesic effect in a dog comprising administering to the dog an opioid compound and an azole compound.2. The method of claim 1 , wherein the opioid compound is selected from the group consisting of methadone claim 1 , methadone enantiomers claim 1 , codeine claim 1 , morphine claim 1 , hydrocodone claim 1 , oxycodone claim 1 , meperidine claim 1 , nalbuphine claim 1 , buprenorphine claim 1 , butorphanol claim 1 , fentanyl claim 1 , and combinations thereof.3. The method of claim 2 , wherein the opioid compound is methadone.4. The method of claim 1 , wherein the azole compound is a triazole antifungal compound.5. The method of claim 4 , wherein the azole compound is a triazole antifungal compound selected from the group consisting of albaconazole claim 4 , efinaconazole claim 4 , epoxiconazole claim 4 , fluconazole claim 4 , isavuconazole claim 4 , itraconazole claim 4 , posaconazole claim 4 , propiconazole claim 4 , ravuconazole claim 4 , terconazole claim 4 , voriconazole claim 4 , and combinations thereof6. The method of claim 5 , wherein the azole compound is fluconazole.7. The method of claim 1 , wherein the opioid compound ...

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Номер записи: 56
18-03-2021 дата публикации

METHOD OF COUNTERING RESPIRATORY DEPRESSION VIA ACTIVATION OF NEURONAL HETEROMERIC NICOTINIC ACETYLCHOLINE RECEPTORS

Номер: US20210077478A1
Автор: GREER JOHN J., REN Jun
Принадлежит:

Compounds capable of activating a neuronal heteromeric nicotinic acetylcholine receptor are provided and can be administered in the form of pharmaceutical compositions of the like. Methods for using the compounds for treating, preventing, or ameliorating respiratory depression and overdose induced by an opioid, or other cause of respiratory depression are also provided. Methods of inducing analgesia, anesthesia, or sedation in a subject, while simultaneously treating, preventing, or ameliorating respiratory depression and overdose induced by an opioid, or other cause of respiratory depression are also provided. 1. A method of treating , preventing , or ameliorating respiratory depression and overdose induced by an opioid , or other cause of respiratory depression in a subject , comprising administering to the subject an effective amount of a compound capable of activating a neuronal heteromeric nicotinic acetylcholine receptor or a composition comprising same.2. The method of claim 1 , wherein the other cause of respiratory depression is selected from a non-opioid drug claim 1 , obstructive sleep apnea claim 1 , central sleep apnea claim 1 , apnea of prematurity claim 1 , hypoxia claim 1 , Prader-Willi Syndrome claim 1 , Rett Syndrome claim 1 , Pompe Disease claim 1 , Cheyne-Stokes breathing claim 1 , neuronal degeneration claim 1 , stroke claim 1 , heart failure claim 1 , brain trauma claim 1 , Parkinson's Disease claim 1 , or spinal cord injury.3. The method of claim 1 , wherein the compound is selected from a positive allosteric modulator of the neuronal heteromeric nicotinic acetylcholine receptor or a nicotinic acetylcholine agonist selected from a full agonist or a partial agonist.4. The method of claim 3 , wherein the neuronal heteromeric nicotinic acetylcholine receptor is an α4β2 nicotinic acetylcholine receptor.5. The method of claim 3 , wherein the neuronal heteromeric nicotinic acetylcholine receptor is an α4β4 nicotinic acetylcholine receptor.6. The ...

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Номер записи: 57
25-03-2021 дата публикации

PHARMACEUTICAL COMPOSITIONS AND METHODS FOR ANESTHESIOLOGICAL APPLICATIONS

Номер: US20210085691A1
Автор: Saadeh Dennis Elias
Принадлежит:

Pharmaceutical compositions and methods of use including a benzodiazepine-based compound, an NMDA antagonist, and optionally a β-blocker, antiemetic, an NSAID, and/or an antihistamine medication. 1. A pharmaceutical composition , comprising a therapeutically effective quantity of a pharmaceutical formulation , wherein the pharmaceutical composition comprises:a therapeutically effective quantity of a first pharmaceutically active compound selected from the group consisting of midazolam, diazepam, lorazepam, flunitrazepam, alprazolam, chlordiazepoxide, clonazepam and clorazepate, and pharmaceutically acceptable salts, hydrates, solvates or N-oxides thereof, optionally in combination with a non-benzodiazepine compound selected from the group consisting of eszopiclone, ramelteon, zolpidem, and zaleplon; anda therapeutically effective quantity of a second pharmaceutically active compound selected from the group consisting of ketamine, dextrorphan, etomidate, methadone, memantine, amantadine, dextromethorphan, and pharmaceutically acceptable salts, hydrates, solvates or N-oxides thereof;wherein the first and second pharmaceutically active compounds are molded or compressed with a binder to form the pharmaceutical composition.2. The pharmaceutical composition of claim 1 , wherein the pharmaceutical formulation further comprises a therapeutically effective quantity of a third pharmaceutically active compound selected from the group consisting of β-blockers claim 1 , antiemetic medicaments claim 1 , NSAIDs claim 1 , antihistamines claim 1 , α-2-adrenergic agonists claim 1 , pain relievers and combinations thereof claim 1 , or pharmaceutically acceptable salts claim 1 , hydrates claim 1 , solvates or N-oxides thereof.3. The pharmaceutical composition of claim 2 , wherein the β-blocker claim 2 , the α-2-adrenergic agonist or the pain reliever is selected from the group consisting of metoprolol claim 2 , propranolol claim 2 , acebutolol claim 2 , nadolol claim 2 , atenolol ...

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Номер записи: 58
25-03-2021 дата публикации

INSOLUBLE COMPLEX OR SOLVATE THEREOF, PHARMACEUTICAL COMPOSTION AND USE THEREOF

Номер: US20210087144A1
Автор: Cheng Kaisheng, Gao Shu, Lu Xiaorong, Peng Jiashi, Sun Hongzhang, Wang Xiao, Wang Yihua, Zhang Shanchun
Принадлежит:

The present invention provides a complex of formula (I) or a solvate thereof (wherein n is 1 to 4), a pharmaceutical composition, and use of the pharmaceutical composition in the prevention or treatment of surgical pain, intraoperative pain and postsurgical pain. The technical solution according to the present invention provides a medicament which can be produced by a simple production process and can stably release a local anesthetic in body for a long period. The medicament can be released for at least three days or more, which can prolong the analgesic effect on the postsurgical pain, can be used conveniently by the physician and the patient, and has a good treatment compliance. 2. The complex or the solvate thereof according to claim 1 , wherein n is 2.3. The complex or the solvate thereof according to claim 2 , wherein the solvate is a methanol solvate claim 2 , an ethanol solvate claim 2 , or a hydrate.4. The complex or the solvate thereof according to claim 2 , wherein the complex or the solvate is an ethanol solvate having a polymorph A claim 2 , wherein an X-ray powder diffraction pattern thereof claim 2 , measured with Cu—Kα radiation claim 2 , has diffraction peaks at about 4.9±0.2 claim 2 , 9.8±0.2 claim 2 , and 12.0±0.2 represented by 2θ.5. The complex or the solvate thereof according to claim 4 , wherein the X-ray powder diffraction pattern of the polymorph A is substantially as shown in .6. The complex or the solvate thereof according to claim 2 , wherein the complex or the solvate thereof is a methanol solvate having a polymorph B claim 2 , wherein an X-ray powder diffraction pattern thereof claim 2 , measured with Cu—Kα radiation claim 2 , has diffraction peaks at about 10.9±0.2 claim 2 , 12.6±0.2 claim 2 , and 13.7±0.2 represented by 2θ.7. The complex or the solvate thereof according to claim 6 , wherein the X-ray powder diffraction pattern of the polymorph B is substantially as shown in .8. The complex or the solvate thereof according to claim 2 , ...

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Номер записи: 59
29-03-2018 дата публикации

DISPERSION ANAESTHETIC DEVICE

Номер: US20180085325A1
Автор: HALL Judith, Paul Alison, Wilkes Antony
Принадлежит:

The invention concerns a cartridge for an inhalation device for delivering anaesthetic to a human or animal wherein anaesthetic in said cartridge is dispersed in an anaesthetic control release medium; an inhalation device for use with said cartridge and a formulation comprising at least one selected anaesthetic and anaesthetic control release medium. 1. A formulation comprising an anaesthetic control release medium and at least one selected inhalation anaesthetic.2. The formulation according to claim 1 , wherein said anaesthetic is dispersed or distributed in said medium in a stable and chemically unaltered state.3. The formulation according to claim 1 , wherein said anaesthetic control release medium is an emulsion.4. The formulation according to claim 1 , wherein said non-anaesthetic component of the emulsion is non-volatile.5. The formulation according to claim 3 , wherein said emulsion is provided by a non-ionic surfactant selected from the group consisting of: halogenated non-ionic surfactants claim 3 , ethylene oxide based fluorocarbon surfactants claim 3 , propylene oxide or ethylene oxide based hydrocarbon surfactants claim 3 , partially fluorinated sulfosuccinate surfactants and branched hydrocarbon sulfosuccinate surfactants claim 3 , and any combination thereof.6. The formulation according to claim 3 , wherein said emulsion is a non-ionic or an anionic surfactant selected from the group consisting of: Zonyl FSN-100 claim 3 , Capstone FS-3100 claim 3 , Chemguard S-550 L-100 claim 3 , Polyfox 159 claim 3 , Brij O20 claim 3 , Tween claim 3 , Capstone FS-63 claim 3 , and any combination thereof.7. The formulation according to claim 3 , wherein said emulsion has a droplet size between 10-1000 nm.8. The formulation according to claim 1 , wherein the anaesthetic content is between 0.25-44% by volume.9. The formulation according to claim 1 , wherein said formulation comprises a gelling agent.10. The formulation according to claim 9 , wherein the gelling agent is ...

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Номер записи: 60
21-03-2019 дата публикации

Topical formulations of chloroprocaine and methods of using same

Номер: US20190083446A1
Автор: Augusto Mitidieri, Clara BIANCHI, Elisabetta Donati
Принадлежит: Sintetica SA

Topical dosages and formulations of chloroprocaine and pharmaceutically acceptable salts thereof are provided that are efficacious, chemically stable and physiologically balanced for safety and efficacy, particularly during ophthalmic procedures or in response to ophthalmic abrasions or trauma.

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Номер записи: 61
31-03-2016 дата публикации

Drug loaded microspheres for post-operative chronic pain

Номер: US20160089335A1
Автор: Gary R. Strichartz, Phillip Blaskovich, Rachit Ohri
Принадлежит: COVIDIEN LP

A microsphere is disclosed. The microsphere includes at least one biodegradable polymer and at least one local anesthetic, wherein about 75% of the at least one local anesthetic is released by about 72 hours and from about 80% to about 90% of the at least one local anesthetic is released by about 120 hours, thereby relieving chronic pain for at least 28 days.

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Номер записи: 62
21-03-2019 дата публикации

PHARMACOLOGICALLY ACTIVE COMPOUNDS

Номер: US20190084993A1
Автор: "ONeill Paul M.", BERRY Neil, Leuwer Martin, Pidathala Chandrakala
Принадлежит: THE UNIVERSITY OF LIVERPOOL

The present invention relates to compounds of formula I shown below: 2. A compound according to claim 1 , wherein R claim 1 , R claim 1 , Rand Rare each independently selected from hydrogen claim 1 , fluoro or methyl; or Rand Rare linked such that together they form a 4 or 5 membered carbocyclic or heterocyclic ring.3. A compound according to claim 1 , wherein R claim 1 , R claim 1 , Rand Rare all hydrogen; or Rand Rare linked such that together they form a 4 or 5 membered heterocyclic ring.4. A compound according to claim 1 , wherein one or two of R claim 1 , R claim 1 , Rand Ris a substituent other than hydrogen.5. A compound according to claim 1 , wherein Rand Rare hydrogen and one of Rand Ris fluoro.618-. (canceled)19. A compound according to claim 1 , which is selected from any one of the following:(3-fluoroazetidin-1-yl)(4-hydroxy-3,5-diisopropylphenyl) methanone; and(4-Hydroxy-3,5-diisopropylphenyl)(2-oxa-6-azaspiro[3.3]heptan-6-yl)methanone;or a pharmaceutically acceptable salt or solvate thereof.20. A pharmaceutical composition comprising a compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , in admixture with a pharmaceutically acceptable diluent or carrier.2123-. (canceled)24. A method of treating chronic pain or inducing anaesthesia in a patient in need of such treatment claim 1 , said method comprising administering to said patient a therapeutically effective amount of a compound according to .26. A pharmaceutical composition comprising a compound according to claim 19 , or a pharmaceutically acceptable salt thereof claim 19 , in admixture with a pharmaceutically acceptable diluent or carrier.27. A method of treating chronic pain or inducing anaesthesia in a patient in need of such treatment claim 19 , said method comprising administering to said patient a therapeutically effective amount of a compound according to . This application is a continuation of U.S. application Ser. No. 15/587,068, filed May 4, 2017, which is ...

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Номер записи: 63
05-05-2022 дата публикации

TOPICAL ANALGESIC COMPOSITIONS AND METHODS OF USE

Номер: US20220133658A1
Автор: Goskonda Venkat R., Nallakrishnan Ravi
Принадлежит:

The present invention is directed to topical skin composition comprising one or more active ingredients and one or more permeation enhancers. The present invention is further directed to a method of reducing or eliminating pain.

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Номер записи: 64
05-05-2022 дата публикации

Quaternary ammonium salt compound, preparation method therefor and use thereof

Номер: US20220135526A1
Автор: Bowen KE, Jin Liu, Jun Yang, Lei Tang, Wensheng Zhang
Принадлежит: West China Hospital of Sichuan University

A quaternary ammonium salt compound of formula I is fast-acting and has a long-term local anaesthetic effect after a single administration, the sensory nerve block time being longer than the motor nerve block time, has both a long-acting local anaesthetic effect and a selective local anaesthetic effect, and also significantly reduces the side effects of quaternary ammonium salt compounds with the structural features of surfactants and is highly safe; thus, the compound of formula I and the pharmaceutically acceptable salt thereof can be used for the preparation of saft drugs having a long-term local anaesthetic effect and a selective local anaesthetic effect

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Номер записи: 65
07-04-2016 дата публикации

Topical composition for pain relief

Номер: US20160095832A1
Автор: Patrick Musitano
Принадлежит: Patrick Musitano

The composition comprises 0.5% to 10% by weight of a neuropathic analgesic; 0.5% to 10% by weight of a muscle relaxant; 0.5% to 20% by weight of an anti-inflammatory analgesic; and 0.5% to 10% by weight of an anesthetic.

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Номер записи: 66
12-05-2022 дата публикации

Patch

Номер: US20220142951A1
Автор: IGAUE Tsuyoshi, Nagaike Daisaku
Принадлежит: KOBAYASHI PHARMACEUTICAL CO., LTD.

A patch () comprising: a nonwoven fabric (); and an adhesive layer () on the nonwoven fabric (), wherein the adhesive layer () comprises a cool feeling agent, a local anesthetic and/or an anti-inflammatory analgesic, and water, and the adhesive layer () has a maximum thickness of 0.50 mm or more. 1. A patch comprising:a nonwoven fabric; andan adhesive layer on the nonwoven fabric,wherein the adhesive layer comprises (i) a cool feeling agent, (ii) a local anesthetic and/or an anti-inflammatory analgesic, and (iii) water, andthe adhesive layer has a maximum thickness of 0.50 mm or more.2. The patch according to claim 1 ,wherein the local anesthetic comprises lidocaine.3. The patch according to claim 1 ,wherein the cool feeling agent comprises menthol.4. The patch according to claim 1 ,wherein an area to which the adhesive layer is applied is smaller than an area of the nonwoven fabric,the adhesive layer has an outer edge portion whose thickness is gradually reduced toward an edge, andan angle formed by a side surface of gel and the nonwoven fabric in the outer edge portion is 5° or more and less than 90°.5. The patch according to claim 1 ,{'sup': '2', 'wherein the adhesive layer has an adhesive force of 10 to 100 gf/cm.'}6. The patch according to claim 1 ,wherein the adhesive layer has a maximum thickness of 1.00 mm or more.7. The patch according to claim 1 , further comprising an infiltration layer in which part of the adhesive layer infiltrates into the nonwoven fabric claim 1 ,wherein the infiltration layer has a maximum thickness of 0.001 to 0.500 mm.8. The patch according to claim 1 ,wherein a content of the cool feeling agent is 0.01 to 10% by weight based on a total amount of the adhesive layer.9. The patch according to claim 1 ,wherein a total content of the local anesthetic and the anti-inflammatory analgesic is 1 to 7.5% by weight based on a total amount of the adhesive layer.10. The patch according to claim 1 ,wherein a content of the cool feeling agent is ...

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Номер записи: 67
01-04-2021 дата публикации

BICYCLIC HETEROARYL DERIVATIVES AND PREPARATION AND USES THEREOF

Номер: US20210094925A1
Автор: Xiang Jia-Ning, Xu Xuesong, Zhou Wei
Принадлежит:

The present invention relates compounds of Formula (A), as well as their preparation and uses, and further relates pharmaceutical compositions comprising these compounds and their uses as modulators of dysfunctional glutamate transmission. The present invention also relates to uses of the compounds or pharmaceutical compositions in treating or preventing certain neurological and psychiatric disorders and diseases as well as cancer in humans. 3. The method of claim 1 , wherein administering comprises orally administering.4. The method of claim 1 , wherein administering comprises transdermally administering.5. The method of claim 1 , wherein administering comprises administering a therapeutically effective amount of a pharmaceutical composition comprising the compound or a pharmaceutically acceptable salt thereof.6. The method of claim 5 , wherein claim 5 ,the pharmaceutical composition is an oral pharmaceutical formulation; andadministering comprises orally administering.7. The method of claim 5 , wherein claim 5 ,the pharmaceutical composition is a transdermal pharmaceutical formulation; andadministering comprises transdermally administering.8. The method of claim 1 , wherein the disease or disorder is anxiety.9. The method of claim 1 , wherein the disease or disorder is ataxia.10. The method of claim 1 , wherein the disease or disorder is attention deficit disorder.11. The method of claim 1 , wherein the disease or disorder is cancer.12. The method of claim 1 , wherein the disease or disorder is bipolar disorder.13. The method of claim 1 , wherein the disease or disorder is dementia.14. The method of claim 1 , wherein the disease or disorder is depression.15. The method of claim 1 , wherein the disease or disorder is drug addiction.16. The method of claim 1 , wherein the disease or disorder is eating disorder.17. The method of claim 1 , wherein the disease or disorder is Huntington's disease.18. The method of claim 1 , wherein the disease or disorder is obsessive- ...

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Номер записи: 68
08-04-2021 дата публикации

Substituted 3-Dialkylaminomethyl-Piperidin-4-yl-Benzamides and Methods of Making and Using Same

Номер: US20210101868A1
Автор: Bayoumy Shariff, Dax Scott L., Kuo Lawrence C., Tounge Brett A.
Принадлежит:

The invention relates to certain substituted 3-dialkylaminomethyl-piperidin-4-yl-benzamides, and compositions comprising the same, which in certain embodiments are useful for treating and/or preventing pain in a subject in need thereof. 2. (canceled)3. The compound of claim 1 , wherein Rand Rare methyl.4. The compound of claim 1 , wherein Ris selected from the group consisting of H and methyl.5. The compound of claim 1 , wherein L is selected from the group consisting of methylene (—CH—) claim 1 , 1 claim 1 ,2-ethylene (—CH—CH—) claim 1 , and 1 claim 1 ,3-propylene (—CH—CH—CH—).6. The compound of claim 1 , wherein Ris selected from the group consisting of phenyl claim 1 , thienyl substituted phenyl claim 1 , and substituted thienyl.7. The compound of claim 1 , wherein Rand Rare H claim 1 , wherein Rand Rare methyl claim 1 , wherein Ris selected from the group consisting of H and methyl claim 1 , wherein L is selected from the group consisting of methylene (—CH—) claim 1 , 1 claim 1 ,2-ethylene (—CH—CH—) claim 1 , and 1 claim 1 ,3-propylene (—CH—CH—CH—) claim 1 , and wherein Ris selected from the group consisting of phenyl claim 1 , thienyl substituted phenyl claim 1 , and substituted thienyl.8. The compound of claim 1 , wherein the —Rand —CHNRRgroups have syn relative stereochemistry.10. A compound selected from the group consisting of:3-(-(2-Chloro-4-fluoro-benzyl)-3-dimethylaminomethyl-4-hydroxy-piperidin-4-yl)-benzamide (6);(+)-Ent-A-syn-3-(1-(2-chloro-4-fluorobenzyl)-3-((dimethylamino)methyl)-4-hydroxy piperidin-4-yl)benzamide [(+)-Ent-A-syn-(6)];(−)-Ent-B-syn-3-(1-(2-chloro-4-fluorobenzyl)-3-((dimethylamino)methyl)-4-hydroxy piperidin-4-yl)benzamide [(−)-Ent-B-syn-(6)];(+)-Ent-A-anti-3-[1-(2-chloro-4-fluorobenzyl)-3-[(dimethylamino)methyl]-4-hydroxypiperidin-4-yl]benzamide [(+)-Ent-A-anti-(6)];(−)-Ent-B-anti-3-[1-(2-chloro-4-fluorobenzyl)-3-[(dimethylamino)methyl]-4-hydroxypiperidin-4-yl]benzamide [(−)-Ent-B-anti-(6)];3-(3-Dimethylaminomethyl-4-hydroxy-1- ...

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Номер записи: 69
23-04-2015 дата публикации

Sheet and liquid combination systems for dermal delivery of lidocaine, diclofenac, and other drugs

Номер: US20150110852A1
Автор: Jie Zhang
Принадлежит: Individual

A system for dermal delivery of lidocaine, bupivacaine, diclofenac, or ketoprofen is provided which comprises at least two components, for example, a sheet of a solid and flexible material, and a vehicle liquid comprising a solvent and optionally other ingredients. A drug, selected from group consisting of lidocaine, bupivacaine, diclofenac, and ketoprofen, can be impregnated in the sheet or contained in the vehicle liquid. These two components can be stored separately and joined either shortly before or at the time of application. To use the system, the vehicle liquid may be applied either on the target skin area or on the sheet, and the sheet may then be applied on the target skin area so that the vehicle liquid is positioned between the sheet and the skin and brought into contact with the ingredients impregnated in the sheet.

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Номер записи: 70
19-04-2018 дата публикации

TREATMENT OF PAIN

Номер: US20180104223A1
Автор: GONZALEZ Isabel, Pritchard Martyn, Richardson Peter
Принадлежит: PROXIMAGEN LIMITED

(3S)-Tetrahydrofuran-3-yl(4S)-4-isopropyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]-pyridine-5-carboxylate, and salts thereof for use in the treatment of pain. 1. (3S)-Tetrahydrofuran-3-yl (4S)-4-isopropyl-1 ,4 ,6 ,7-tetrahydro-5H-imidazo[4 ,5-c]pyridine-5-carboxylate and hydrates and pharmaceutically acceptable salts thereof , for use in , or in the manufacture of a medicament for , the treatment of pain.2. A method for the treatment of pain claim 1 , which comprises administering to a subject suffering from pain an effective amount of a compound according to .3. A pharmaceutical composition comprising a compound according to claim 1 , and one or more suitable excipients.4. A compound claim 1 , use or method according to wherein the pain is inflammatory pain.5. A compound according to wherein the pharmaceutically acceptable salt is the mesylate.6. A compound according to wherein the pharmaceutically acceptable salt is the sulphate claim 1 , or a hydrate thereof. The present invention relates to the use of the SSAO inhibitor (3S)-Tetrahydrofuran-3-yl (4S)-4-isopropyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridine-5-carboxylate, and salts thereof in the treatment of pain.Semicarbazide-sensitive amine oxidase (SSAO) activity is an enzyme activity expressed by Vascular Adhesion Protein-1 (VAP-1) or Amine Oxidase, Copper Containing 3 (AOC3), belongs to the copper-containing amine oxidase family of enzymes (EC.1.4.3.6). Therefore inhibitors of the SSAO enzyme may also modulate the biological functions of the VAP-1 protein.SSAO activity has been found in a variety of tissues including vascular and non-vascular smooth muscle tissue, endothelium, and adipose tissue [Lewinsohn, 1984, 17, 223-256; Nakos & Gossrau, 1994, 32, 3-10; Yu et al., 1994, 47, 1055-1059; Castillo et al., 1998, 33, 415-423; Lyles & Pino, 1998, 52, 239-250; Jaakkola et al., 1999, 155, 1953-1965; Morin et al., 2001, 297, 563-572; Salmi & Jalkanen, 2001, 22, 211-216]. In addition, SSAO protein is found in blood ...

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Номер записи: 71
23-04-2015 дата публикации

Depot Formulations of a Local Anesthetic and Methods for Preparation Thereof

Номер: US20150111923A1
Автор: Michael Naveh, Shimon Amselem
Принадлежит: PAINREFORM Ltd

The invention provides extended release pro-liposomal, non-aqueous, pharmaceutical formulations of a local anesthetic in the form of a clear oily solution and methods for making same. The formulations can be administered by infiltration into an incision, or by injection.

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Номер записи: 72
29-04-2021 дата публикации

OPIOID RECEPTOR ANTAGONIST CONJUGATE AND USE THEREOF

Номер: US20210121455A1
Автор: HE Mei
Принадлежит: SHANGHAI HANMAI BIO-PHARMA CO., LTD.

The present invention relates to an opioid receptor antagonist conjugate and a use thereof. In particular, the present invention relates to a covalent coupling conjugate of a hydrophilic polymer and an opioid receptor antagonist and the use thereof. 1. A conjugate as represented by formula (I) or a pharmaceutically acceptable salt thereof:{'br': None, 'i': 'm', 'P—(W)\u2003\u2003 (I)'} W is a non-naloxone opioid receptor antagonist; and', 'm is a natural number between 1 and 10., 'wherein, P is a hydrophilic polymer;'}2. The conjugate according to claim 1 , wherein the hydrophilic polymer is polyethylene glycol.3. The conjugate according to claim 1 , wherein the hydrophilic polymer is a polyethylene glycol having 2 to 45 —CHCHO— structural unit claim 1 , preferably the polyethylene glycol having 2 to 40 —CHCHO— structural unit claim 1 , preferably the polyethylene glycol having 2 to 30 —CHCHO— structural unit claim 1 , preferably the polyethylene glycol having 2 to 20 —CHCHO— structural unit claim 1 , preferably the polyethylene glycol having 2 to 10 —CHCHO— structural unit claim 1 , and more preferably the polyethylene glycol having 2 to 8 —CHCHO— structural unit.4. The conjugate according to claim 3 , wherein the polyethylene glycol is a monodisperse polyethylene glycol.5. The conjugate according to claim 1 , wherein the non-naloxone opioid receptor antagonist is derived from a compound selected from the group consisting of 6-amino-14-hydroxy-17-allyl norfloxacin morphine claim 1 , naltrel claim 1 , naltrexone claim 1 , N-methylnaltrexone claim 1 , nalmefene claim 1 , nalbuphine claim 1 , butorphanol claim 1 , cyclozocine claim 1 , pentazocine claim 1 , nalorphine claim 1 , naltrindole claim 1 , nobelnatofimin claim 1 , oxilorphan claim 1 , levallorphan claim 1 , methylnaltrexone claim 1 , buprenorphine claim 1 , seklowan claim 1 , oxymorphone claim 1 , codeine claim 1 , oxycontin claim 1 , morphine claim 1 , ethylmorphine hydrochloride claim 1 , diacetylmorphine ...

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Номер записи: 73
29-04-2021 дата публикации

GPR183 ANTAGONISTS FOR THE TREATMENT OF PAIN

Номер: US20210122750A1
Автор: Arnatt Christopher K., Salvemini Daniela
Принадлежит:

Disclosed herein are compositions and methods for treating neuropathic pain in a subject in need thereof. Compositions disclosed herein are GPR183 antagonists. The methods include administering to a subject in need thereof a therapeutically effective amount of a GPR183 antagonist. 2. The compound of claim 1 , wherein L is a substituted or unsubstituted nitrogen containing ring system comprising one or two optionally aromatic rings and one or more carbonyl groups.5. The compound of claim 4 , wherein p is 1 and ring B is aryl or heteroaryl.6. The compound of claim 4 , wherein Rand Rtogether with the atoms they are attached to form a carbonyl group.8. The compound of claim 1 , wherein L is a substituted or unsubstituted nitrogen containing ring system comprising one or two optionally aromatic rings and one or more alkoxy substituents.10. The compound of claim 9 , wherein p is 1 such that ring C is a 6 membered ring.11. The compound of claim 9 , wherein at least one of R claim 9 , R claim 9 , R claim 9 , and Ris alkoxy or —OH.13. The compound of claim 12 , wherein at least one of R claim 12 , R claim 12 , R claim 12 , R claim 12 , and Ris halo.15. A method for treating pain in a subject in need thereof claim 12 , the method comprising: administering to the subject in need thereof a therapeutically effective amount of a GPR183 antagonist.16. The method of claim 15 , wherein the GPR183 antagonist comprises a compound Formula (XVII) and pharmaceutically acceptable salts thereof.18. The method of claim 15 , wherein the pain is at least one of chemotherapy-induced neuropathy claim 15 , diabetic neuropathy claim 15 , cancer pain claim 15 , autoimmune neuropathy claim 15 , and traumatic neuropathy.19. The method of claim 17 , wherein the GPR183 antagonist is administered orally claim 17 , intravenously claim 17 , intrathecalyl claim 17 , sublingually claim 17 , transdermally claim 17 , subcutaneously claim 17 , topically claim 17 , intranasally claim 17 , intraarterially claim ...

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Номер записи: 74
09-06-2022 дата публикации

Compositions and Methods of Achieving Pain Relief

Номер: US20220175703A1
Автор: Brown Dale G., Hill Ira D.
Принадлежит:

In one aspect, this invention relates to a method for treating pain and subsequent resulting conditions. In yet another aspect, this invention relates to formulating agents to rapidly reverse painful conditions. 1. A method of treating a subject in need of pain relief by administering to a subject an effective pain-relieving amount of a composition comprising a mixture of spilanthol , pellitorine , beta-caryophyllene and pro-vitamin B5.2. The method of claim 1 , where the composition further contains menthol.3. The method of claim 1 , wherein the painful condition is caused by or related to a body condition selected from the group consisting of: Chronic and Acute Pain of the muscles claim 1 , joints and ligaments claim 1 , Migraine Headaches claim 1 , Diabetes claim 1 , Arteriosclerosis claim 1 , Radiation Dermatitis claim 1 , Pruritus claim 1 , Insect bites claim 1 , Anaphylactic Shock from serious allergic responses to allergens from Insect Bites claim 1 , Food Allergies claim 1 , Pollens and other Environmentally induced allergies claim 1 , Carbuncles claim 1 , Acne claim 1 , Dermal burns due to exposure to sun claim 1 , x-rays and/or excessive heat claim 1 , Cancer claim 1 , Mucositis claim 1 , Aphthous ulcers claim 1 , Periodontal and Gingivitis disease claim 1 , Herpes simplex claim 1 , Herpes zoster claim 1 , Coronavirus-19 claim 1 , Yeast and/or Microbial infections claim 1 , Psoriasis claim 1 , Crohn's disease claim 1 , Lupus claim 1 , painful scarring claim 1 , Irritable Bowel disease claim 1 , other Autoimmune Diseases and Diseases causally related to autoimmune diseases like fibromyalgia claim 1 , Rheumatoid and Osteoarthritis claim 1 , and Xerostomia.4. The method of claim 1 , wherein said composition is administered to the subject by a route selected from the group consisting of mucosal claim 1 , dermal claim 1 , oral claim 1 , inhalation claim 1 , injection claim 1 , nasal claim 1 , and other common routes known in the medical arts.5. The method of ...

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Номер записи: 75
09-06-2022 дата публикации

Oral Formulation of Clonidine and Midazolam for Sedation in Dental Procedures

Номер: US20220175794A1
Автор: McCarley James Liddell, Wilson Pamala Lea
Принадлежит:

A drug composition in solid drug matrix formulation comprising clonidine, midazolam, and fentanyl. The amounts of the drug contained in the solid drug matrix are sufficient to induce sedation in preparation for a clinical procedure. When administered in the mouth, the drug ingredients are absorbed by transmucosal passage. This solid drug matrix formulation may be particularly useful in pediatric dentistry practice. Also disclosed is a method of inducing sedation in a patient by administering the solid drug matrix formulation to the patient prior to performing a clinical procedure. 1. A solid drug matrix formulation comprising:clonidine in an amount ranging from 10-300 μg;midazolam in an amount ranging from 1-40 mg;fentanyl in an amount ranging from 10-300 μg.2. The drug formulation of claim 1 , wherein the amount of fentanyl is less than 190 μg.3. The drug formulation of claim 2 , wherein the amount of fentanyl is less than 175 μg.4. The drug formulation of claim 3 , wherein the amount of fentanyl is less than 150 μg.5. The drug formulation of claim 1 , being in the form of a lozenge or lollipop.6. The drug formulation of claim 1 , having a size of at least 1.0 cm along its widest dimension.7. The drug formulation of claim 6 , having a size of at least 1.5 cm along its widest dimension.8. The drug formulation of claim 6 , having a size of less than 3.5 cm along its widest dimension.9. The drug formulation of claim 1 , having a total weight in the range of 2.0-25 grams.10. The drug formulation of claim 9 , having a total weight of less than 15 grams.11. The drug formulation of claim 10 , having a total weight of less than 10 grams.12. The drug formulation of claim 1 , further comprising a sweetener or flavor enhancer.13. A method of inducing sedation in a patient claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'having a solid drug matrix formulation of ;'}administering the solid drug matrix formulation to the patient orally and letting dwell in ...

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Номер записи: 76
27-04-2017 дата публикации

Volatile anesthetic compositions and methods of use

Номер: US20170112783A1
Автор: Allen Burton, Christopher C. Capelli, Hatice Ozsoy, Phillip C. Phan
Принадлежит: University of Texas System

The present invention provides methods for reducing pain in a subject in need thereof by delivering a volatile anesthetic in a solution or an emulsion that can additionally include an extractive solvent in an amount effective to reduce pain without substantially interfering with motor function. Chronic or acute pain may be treated, or the volatile anesthetic may be delivered as a regional anesthetic to a subject to anesthetize a portion of the subject prior to surgery. Dosing regimes including a one-time administration, continuous and/or periodic administration are contemplated.

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Номер записи: 77
13-05-2021 дата публикации

Dental topical anesthetic gel

Номер: US20210137833A1
Автор: Daniel Wang, Heng SUN, XIAO YANG
Принадлежит: Pac-Dent Inc

The present invention relates to a dental topical anesthetic gel containing a full spectrum blend of active cannabinoids and at least one component including tetracaine, benzocaine, lidocaine, and butamben. Further, the dental topical gel may also contain a chemical penetration enhancer, at least one drug to enhance the effects of cannabinoids, at least one antibacterial agent and at least one antifungal agent. The forms and use of the dental topical anesthetic gel are also disclosed.

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Номер записи: 78
13-05-2021 дата публикации

Ketamine and Propofol Admixture

Номер: US20210137851A1
Автор: Nicholson Wayne T., Panyam Jayanth, Smischney Nathan J.
Принадлежит:

Pharmaceutical formulations comprising ketamine, propofol, and a lipid are provided. Methods of making the formulations and methods of using the formulations to provide sedation, amnesia, analgesia, anxiolysis, and/or stable hemodynamics are also provided. 1. A pharmaceutical formulation , comprising:ketamine;propofol; anda lipid, wherein the ketamine is substantially dissolved in the lipid.2. The pharmaceutical formulation of claim 1 , wherein the formulation is an oil-in-water emulsion.3. The pharmaceutical formulation of claim 1 , wherein the formulation is essentially free of chloride ions.4. The pharmaceutical formulation of claim 1 , wherein the formulation comprises from about 2.5% (w/v) to about 20% (w/v) lipid.5. The pharmaceutical formulation of claim 1 , wherein the ketamine is present in a concentration of from about 1 mg/ml to about 10 mg/ml.6. The pharmaceutical formulation of claim 1 , wherein the propofol is present in a concentration of from about 1 mg/ml to about 10 mg/ml.7. The pharmaceutical formulation of claim 1 , wherein the ketamine is present in a concentration of from about 2 mg/ml to about 5 mg/ml.8. The pharmaceutical formulation of claim 1 , wherein the propofol is present in a concentration of from about 5 mg/ml to about 8 mg/ml.9. The pharmaceutical formulation of claim 1 , wherein the ratio of ketamine to propofol is from about 1:4 to about 2:1.10. The pharmaceutical formulation of claim 1 , wherein the ketamine is present in a concentration of about 5 mg/ml and the propofol is present in a concentration of about 5 mg/ml.11. The pharmaceutical formulation of claim 1 , wherein the lipid is selected from soybean oil claim 1 , purified egg phospholipid claim 1 , oleic acid claim 1 , glyceryl ester and mixtures thereof.12. The pharmaceutical formulation of claim 1 , wherein the formulation is an emulsion and maintains phase stability for at least two years.13. A method of manufacturing a pharmaceutical formulation comprising ketamine and ...

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Номер записи: 79
09-04-2020 дата публикации

POLYAMIDE COMPOUND AND USE THEREOF

Номер: US20200109166A1
Автор: CAI Jiaqiang, Deng Hua, HUANG Haitao, SONG Hongmei, SU Donghai, TAN Yuting, Tian Qiang, Wang Jingyi, WANG Lichun, Wu Lei, Wu Yongyong, Yang Long, Yu Nan, ZENG Hong, ZHAO Mingliang, Zhong Wei, ZHOU Xin
Принадлежит: SICHUAN KELUN-BIOTECH BIOPHARMACEUTICAL CO., LTD.

The invention relates to a polyamide compound and a use thereof. Specifically, the invention relates to a type of polyamide compound (which preferably comprise one or more amide bonds formed by condensation of same or different L-amino acids or D-amino acids), or stereoisomers, crystalline polymorphs, solvates, metabolites, prodrugs or pharmaceutically acceptable salts or esters thereof, or pharmaceutical compositions thereof, as well as a method for preparing the polyamide compound and a use thereof in the prevention or treatment of diseases associated with κ-opioid receptor. The polyamide compound of the invention has excellent κ-opioid receptor agonistic activity and hydrophilicity, thus having a lesser ability of penetrating the blood-brain barrier and a lower capacity for entering the brain. The compound of the invention has higher selectivity for a κ-opioid receptor, lower addictiveness, improved pharmacokinetic properties, and improved safety (lower toxicity and/or fewer side effects), good patient compliance, and/or lesser propensity for developing tolerance, among other excellent medicinal properties. 25-. (canceled)7: The compound claim 1 , or the stereoisomer claim 1 , the crystalline polymorph claim 1 , the solvate claim 1 , the metabolite claim 1 , the prodrug or the pharmaceutically acceptable salt or ester thereof claim 1 , according to claim 1 , wherein Ris H or Calkyl claim 1 , wherein Calkyl is optionally substituted with one or more groups independently selected from the group consisting of hydroxyl claim 1 , amino and carboxyl.8. (canceled)9: The compound claim 1 , or the stereoisomer claim 1 , the crystalline polymorph claim 1 , the solvate claim 1 , the metabolite claim 1 , the prodrug or the pharmaceutically acceptable salt or ester thereof according to claim 1 , wherein the W group is selected from the group consisting of —(CH)OH claim 1 , HOCH(CH(OH))CH— claim 1 , (HOCH)CH— claim 1 , (HOCH)C— claim 1 , —(CH)NH claim 1 , —(C(R))CON(R) claim 1 ...

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Номер записи: 80
25-04-2019 дата публикации

Ready-to-administer solution of fentanyl citrate

Номер: US20190117560A1
Автор: Kandarp Maheshkumar Dave, Milan Natvarbhai Thakkar, PRASHANT Kane, SAMARTH Kumar, Subhas Balaram Bhowmick
Принадлежит: SUN PHARMACEUTICAL INDUSTRIES LTD

A method of treating a patient in need of therapy with fentanyl or a salt thereof, the method comprising providing a ready-to-administer solution consisting essentially of fentanyl or a salt thereof as the sole active ingredient, a sugar or sugar alcohol and water for injection, the solution having a pH in the range of 3.5 to 7.5, and parenterally administering the solution to the patient.

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Номер записи: 81
25-04-2019 дата публикации

PERMEANT DELIVERY SYSTEM AND METHODS FOR USE THEREOF

Номер: US20190117947A1
Автор: Baudys Mirek, Enscore David, SMITH Alan, TAGLIAFERRI Frank, Tolia Gaurav
Принадлежит: NITTO DENKO CORPORATION

Disclosed are a patch, system, and method for delivery of a permeant composition into a subject via at least one formed pathway through a biological membrane of the subject. The patch comprises a matrix, at least one hydrophilic permeant disposed within the matrix, wherein at least a portion of the permeant can dissolve in biological moisture received from the subject, and at least one permeability enhancer disposed within the matrix. Also disclosed are systems and methods for delivery of a permeant composition into a subject via at least one formed pathway through a skin layer of the subject. 163-. (canceled)64. A method for delivering a permeant through a biological membrane of a subject comprising:a) forming one or micropores in the biological membrane; and i) a matrix;', 'ii) at least one hydrophilic permeant disposed within the matrix, wherein at least a portion of the hydrophilic permeant can dissolve in biological moisture received from the subject through said one or more micropores; and', 'iii) at least one permeability enhancer disposed within the matrix., 'b) placing a patch in physical contact with said one or more micropores, wherein said patch comprises65. The method of claim 64 , wherein the one or more micropores are formed using at least one device from the group consisting of: thermal porators claim 64 , mechanical porators claim 64 , laser porators claim 64 , and hydraulic porators.66. The method of claim 64 , wherein the one or more micropores are formed using a heat conducting element placed in substantial physical contact with the biological membrane to deliver sufficient energy to the biological membrane to thermally ablate said biological membrane.67. The method of claim 64 , wherein the one or more micropores are formed using a thin film tissue interface device.68. The method of claim 64 , wherein the hydrophilic permeant is a bioactive agent.69. The method of claim 68 , wherein the bioactive agent is a protein drug.70. The method of claim ...

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Номер записи: 82
12-05-2016 дата публикации

Transdermal drug delivery device including an occlusive backing

Номер: US20160128949A1
Автор: David Kanios, Juan A. Mantelle, Viet Nguyen
Принадлежит: Noven Pharmaceuticals Inc

A transdermal drug delivery system for the topical application of one or more active agents contained in one or more polymeric and/or adhesive carrier layers, proximate to a non-drug containing polymeric backing layer which can control the delivery rate and profile of the transdermal drug delivery system by adjusting the moisture vapor transmission rate of the polymeric backing layer.

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Номер записи: 83
01-09-2022 дата публикации

SUSTAINED RELEASE DRUG DELIVERY SYSTEMS AND RELATED METHODS

Номер: US20220273633A1
Автор: AUTIO Susan, DAVIS MARK P., HALLADAY STEVEN, JOICE JUDY, Langecker Peter, LISSIN DMITRI, Miksztal Andrew R., MILLER VAELING, VERITY ADRIAN NEIL
Принадлежит:

The present disclosure provides for methods of producing analgesia in a subject. In some cases, methods produce analgesia in a subject undergoing arthroscopic subacromial decompression surgery. The present disclosure also relates to improved sustained release drug delivery systems. In some cases, a composition comprises an active pharmaceutical agent; at least one of sucrose acetate isobutyrate and a polyorthoester; an organic solvent; and 2,6-dimethylaniline, wherein the 2,6-dimethylaniline is present at a level less than 500 ppm. In some cases, a composition comprises bupivacaine N-oxide at a level less than 1 wt %, based on weight of the composition. In some cases, a composition comprises metal present at a level less than 5 ppm. Dosage forms and methods are also provided. 1. A method of producing analgesia in a subject having arthroscopic subacromial decompression surgery , comprising:drawing up 5 mL of a bupivacaine composition into a 5 mL syringe using a 16-gauge or larger bore needle to fill the syringe, the bupivacaine composition comprising bupivacaine free base or salt thereof;discarding the 16-gauge or larger bore needle; andadministering the 5 mL of the bupivacaine composition into the subacromial space of the subject using an 18-gauge or larger bore needle to produce post-surgical analgesia.2. A method of reducing or eliminating opioid consumption in a subject having arthroscopic subacromial decompression surgery , comprising:drawing up 5 mL of a bupivacaine composition into a 5 mL syringe using a 16-gauge or larger bore needle to fill the syringe, the bupivacaine composition comprising bupivacaine free base or salt thereof;discarding the 16-gauge or larger bore needle; andadministering the 5 mL of the bupivacaine composition into the subacromial space of the subject using an 18-gauge or larger bore needle to produce post-surgical analgesia.3. The method of claim 1 , further comprising storing the bupivacaine composition at a temperature ranging from 15 ...

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Номер записи: 84
01-09-2022 дата публикации

Orally inhaled and nasal benzodiazepines

Номер: US20220273672A1
Автор: Brett Cooper, Christopher Reilly, Derek Jo Sakata, John Graham, Karl-Uwe Petersen, Tatjana Bevans, Thomas Stöhr
Принадлежит: Paion UK Ltd, University of Utah Research Foundation UURF

The present invention relates to Orally Inhaled and Nasal Drug Product (OINDP) comprising a benzodiazepine, in particular remimazolam.

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Номер записи: 85
23-04-2020 дата публикации

Pramipexole for Use in the Treatment of Pain

Номер: US20200121651A1
Автор: Escalona Patricio Rodrigo, Milligan Erin Damita
Принадлежит:

The present invention is directed to the discovery that pramipexole is useful as an agent for the treatment of pathological pain, especially including chronic pain, including chronic nociceptive pain (principally from inflammation) and neuropathic pain, including peripheral neuropathy and central neuropathy. The action of pramipexole in treating pain is non-addictive. In addition, it has been discovered that pramipexole may be co-administered with an opioid agent in the treatment of pain in order to treat pain and reduce the development of tolerance of a patient or subject to the opioid agent such that the opioid agent may have a lasting effect without the requirement of escalating doses, compared to its administration in the absence of pramipexole. Additional embodiments of the present invention are described. 1. A method of treating pain in a subject comprising administering to said subject a composition consisting essentially of an effective amount of pramipexole optionally in combination with a pharmaceutically acceptable carrier , additive or excipient , wherein said pramipexole is non-addictive.2. The method according to wherein said pramipexole is coadministered with an effective amount of at least one opioid analgesic agent.3. The method according to wherein pramipexole is the sole analgesic agent in the composition.4. The method according to wherein said opioid analgesic agent is selected from the group consisting of codeine claim 2 , fentanyl claim 2 , hydrocodone claim 2 , hydromorphone claim 2 , morphine claim 2 , meperidine claim 2 , oxycodone (atone or in combination with naloxone) claim 2 , buprenorphine claim 2 , opium claim 2 , tramadol claim 2 , levorphanol claim 2 , nalbuphine claim 2 , tapentadol claim 2 , butorphanol claim 2 , propoxyphene claim 2 , pentazocine claim 2 , alfentanil claim 2 , sufentanil claim 2 , remifentanil and mixtures thereof.5. The method according to wherein said opioid analgesic agent is selected from the group consisting ...

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Номер записи: 86
03-06-2021 дата публикации

OPIOID RECEPTOR MODULATORS AND PRODUCTS AND METHODS RELATED THERETO

Номер: US20210163402A1
Автор: Bhatt Ulhas, Ding Pingyu, Duquette Jason, LI Yihong, McGee Lawrence R, Medina Julio Cesar, Nerurkar Alok, Nguyen Thomas, Sadlowski Corinne, Seidl Frederick, Sperandio David, Wang Xiaodong, Wei Zhi-Liang
Принадлежит:

Compounds are provided having the structure of Formula (I): 1100-. (canceled)102. The compound of claim 101 , or a pharmaceutically acceptable isomer claim 101 , racemate claim 101 , hydrate claim 101 , solvate claim 101 , isotope claim 101 , or salt thereof claim 101 , wherein:ring A is phenyl, pyridinyl, or pyrazinyl;{'sub': 3', '7, 'sup': '7', 'ring C is a C-Ccycloalkyl or 3-7 membered heterocycloalkyl, substituted with 0-5 R;'}{'sup': 1', '2, 'Rand Rare each, independently, H, methyl, ethyl, isopropyl or cyclopropyl, substituted with 0-3 halo;'}{'sup': 3', '4, 'sub': 1', '6', '1', '6, 'Rand Rare each, independently, H, (C-C)alkyl, (C-C)haloalkyl, or cyclopropylmethyl;'}{'sup': 5', '1', '2', '3', '5, 'sub': 1', '6', '1', '6', '1', '6, 'each Ris independently —C(O)NRR, —OH, halo, (C-C)alkyl, (C-C)haloalkyl, (C-C)alkoxy, or carbocycle; or Rand one R, together with the atoms to which they are connected, form a 5-7 membered heterocycle;'}{'sup': '6', 'sub': 1', '6', '1', '6', '1', '6, 'each Ris independently halo, (C-C)alkyl, (C-C)haloalkyl, (C-C)alkoxy, or carbocycle;'}{'sup': '7', 'sub': 1', '6', '1', '6', '1', '6, 'each Ris independently halo, (C-C)alkyl, (C-C)haloalkyl, (C-C)alkoxy, or carbocycle;'}{'sup': '8', 'Ris H;'}m is 1-3; andn is 0-3.103. The compound of claim 102 , or a pharmaceutically acceptable isomer claim 102 , racemate claim 102 , hydrate claim 102 , solvate claim 102 , isotope claim 102 , or salt thereof claim 102 , wherein ring A is phenyl.104. The compound of claim 103 , or a pharmaceutically acceptable isomer claim 103 , racemate claim 103 , hydrate claim 103 , solvate claim 103 , isotope claim 103 , or salt thereof claim 103 , wherein ring B is phenyl claim 103 , indazolyl claim 103 , 2 claim 103 ,3-dihydrobenzoxazolyl claim 103 , benzoxazolonyl claim 103 , or pyrazolopyridinyl.105. The compound of claim 104 , or a pharmaceutically acceptable isomer claim 104 , racemate claim 104 , hydrate claim 104 , solvate claim 104 , isotope claim 104 , or ...

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Номер записи: 87
03-06-2021 дата публикации

ION CHANNEL MODULATORS

Номер: US20210163488A1
Автор: Griffin Andrew Mark, Marron Brian Edward, Martinez Botella Gabriel, REDDY Kiran, WITTMANN Marion
Принадлежит:

The present invention is directed to, in part, fused heteroaryl compounds and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel including neurological disorders (e.g., Dravet syndrome, epilepsy), pain, and neuromuscular disorders are also provided herein. 13. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein Ris cyclobutyl optionally substituted with one or more R.14. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein Ris Chaloalkyl.15. The compound of any one of - and , or a pharmaceutically acceptable salt thereof , wherein Ris CF.16. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein Ris phenyl.17. The compound of any one of - and - , or a pharmaceutically acceptable salt thereof , wherein Ris Calkyl and Ris hydrogen or Calkyl.18. The compound of any one of - and - , or a pharmaceutically acceptable salt thereof , wherein Rand Rare each Calkyl.19. The compound of any one of - and - , or a pharmaceutically acceptable salt thereof , wherein Rand Rare each methyl.20. The compound of any one of - and - , or a pharmaceutically acceptable salt thereof , wherein Ris methyl and Ris hydrogen.21. The compound of any one of - and - , or a pharmaceutically acceptable salt thereof , wherein Rand Rare each hydrogen.22. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein Ris —CF—OR.23. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein Ris Calkyl optionally substituted with cyclopropyl.24. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein Ris cyclopropyl.25. The compound of any one of - , or a pharmaceutically acceptable ...

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Номер записи: 88
30-04-2020 дата публикации

NOVEL 5-HYDROXY PYRIDINE-BASED COMPOUND FOR USE AS P2X1 AND P2X3 RECEPTOR ANTAGONIST AND PHARMACEUTICAL COMPOSITION COMPRISING SAME

Номер: US20200131131A1
Автор: JUNG Young Hwan, Kim Yong Chul
Принадлежит:

The present invention relates to novel 5-hydroxy pyridine-based compounds useful as P2X1 and P2X3 receptor antagonists and compositions comprising the same. The compounds according to the present invention have an activity of strongly antagonizing P2X1 and P2X3 receptors, and thus can be effectively used as a drug for treating or preventing chronic inflammatory diseases or neuropathic pain diseases caused by P2X1 and P2X3 receptor activity. 7. The compound claim 1 , an isomer thereof or a pharmaceutically acceptable salt thereof of claim 1 , wherein the compound represented by General Formula 1 is any one selected from the group consisting of: 5-Hydroxy-2-(4-methoxyphenethyl)pyridine-3 claim 1 ,4-dicarboxylic acid (13a); 5-Hydroxy-2-(4-methoxyphenethyl)-6-methylpyridine-3 claim 1 ,4-dicarboxylic acid (13b); 6-Ethyl-5-hydroxy-2-(4-methoxyphenethyl)pyridine-3 claim 1 ,4-dicarboxylic acid (13c); 5-Hydroxy-2-(4-methoxyphenethyl)-6-propylpyridine-3 claim 1 ,4-dicarboxylic acid (13d); 6-Butyl-5-hydroxy-2-(4-methoxyphenethyl)pyridine-3 claim 1 ,4-dicarboxylic acid (13e); 5-Hydroxy-6-isopropyl-2-(4-methoxyphenethyl)pyridine-3 claim 1 ,4-dicarboxylic acid (13f); 5-Hydroxy-6-isobutyl-2-(4-methoxyphenethyl)pyridine-3 claim 1 ,4-dicarboxylic acid (13g); 6-Benzyl-5-hydroxy-2-(4-methoxyphenethyl)pyridine-3 claim 1 ,4-dicarboxylic acid (13h); 5-Hydroxy-2-(4-methoxyphenethyl)-6-phenethylpyridine-3 claim 1 ,4-dicarboxylic acid (13i) claim 1 , 3-Hydroxy-6-(4-methoxyphenethyl)pyridine-2 claim 1 ,4 claim 1 ,5-tricarboxylic acid (13j); 5-Hydroxy-2-(4-methoxyphenethyl)-6-(2-(methylthio)ethyl)pyridine-3 claim 1 ,4-dicarboxylic acid (13k); 5-Hydroxy-2-(4-methoxyphenethyl)-6-(2-(methylsulfonyl)ethyl)pyridine-3 claim 1 ,4-dicarboxylic acid (13l); Ethyl 4-cyano-5-hydroxy-2-(4-methoxyphenethyl)-6-methylnicotinate (14); Ethyl 5-hydroxy-2-(4-methoxyphenethyl)-6-methyl-4-(1H-tetrazol-5-yl)nicotinate (15); 4-Cyano-5-hydroxy-2-(4-methoxyphenethyl)-6-methylnicotinic acid (16); 5-Hydroxy-2-(4- ...

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Номер записи: 89
10-06-2021 дата публикации

THE USE OF 7-BROMO-5-(O-CHLOROPHENYL)-3-PROPOXY-1,2-DIHYDRO-3H-1,4-BENZODIAZEPIN-2-ONE FOR INHIBITION OF NEUROPATHIC PAIN AND SEIZURES OF DIFFERENT ETIOLOGY

Номер: US20210169895A1
Автор: ADRONATI Sergey Andreevich, GOLOVENKO Mykola Yakovich, KABANOVA Tatiyana Anatolyevna, KHALIMOVA Olena Igorivna, LARIONOV Vitaly Borysovich, PAVLOVSKIY Viktor Ivanovich, REDER Anatoly Semenovich, VOLOSHCHUK Natalia Ivanivna
Принадлежит:

The invention relates to medical chemistry, in particular to the use of 7-bromo-5-(o-chlorophenyl)-3-propoxy-1,2-di-hydro-3H-1,4-benzodiazepin-2-one as a drug which inhibits neuropathic pain without the formation of defects in the gastric mucosa (ulcerogenic effect), and possesses an anticonvulsant property. 1. (canceled)5. The method of claim 2 , wherein the neuropathic pain is caused by diabetes mellitus claim 2 , herpetic infection claim 2 , stroke claim 2 , multiple sclerosis claim 2 , malignant diseases claim 2 , HIV infection claim 2 , or post-traumatic or postoperative damage to the peripheral nervous system.6. The method of claim 2 , wherein the therapeutically effective amount of the compound of formula (I) is administered orally or intraperitoneally.7. The method of claim 3 , wherein pain is inhibited in the subject.8. The method of claim 3 , wherein inflammation is reduced in the subject.9. The method of claim 3 , wherein convulsions are prevented in the subject. The invention relates to medical chemistry, in particular to the use of 7-bromo-5-(o-chlorophenyl)-3-propoxy-1,2-dihydro-3H-1,4-benzodiazepin-2-one (1) for the inhibition of neuropathic pain without damage of the gastric mucosa (ulcerogenic effect) and some convulsions caused by chemical agents and electrostimulation.The International Association for the Study of Pain (IASP) defines neuropathic pain (NP) as pain “caused by primary damage or dysfunction of the nervous system” (see Lau F H, Chung K C. Silas Weir Mitchell, M D: the physician who discovered causalgia. J Hand Surg. 2004; 29, pp. 181-187). According to estimates, millions of people are afflicted with NP, although exact figures are currently unavailable. Most of common diseases, injuries or interventions cause NP by damaging somatosensory pathways in the peripheral or central nervous system. NP refers to chronic pain unlike acute-nociceptive. The main factors leading to the emergence of NP include diabetes mellitus, herpetic infection, ...

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Номер записи: 90
25-05-2017 дата публикации

Non-diffusive botulinum toxin causing local muscle paralysis, and purification method thereof

Номер: US20170143849A1
Автор: Hyun Sub Lee, Yong Hoon Chung
Принадлежит: Medexgen Inc

The present invention relates to a method for purifying a non-spreading botulinum toxin that causes local muscle paralysis and a non-spreading botulinum toxin obtained thereby. The method comprises the steps of: subjecting a purified botulinum toxin type A product to ion-exchange chromatography using a controlled pH of buffer, concentration of sodium chloride (NaCl), thereby separating the botulinum toxin type A product into subfractions; and collecting a subfraction having an A260/A280 value in a specific range from the separated subfractions.

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Номер записи: 91
07-05-2020 дата публикации

Compounded compositions and methods for treating pain

Номер: US20200138757A1
Автор: II Jay Richard Ray
Принадлежит: CMPD LICENSING LLC

A method of compounding a topical cream includes combining ingredients including lidocaine and prilocaine, 2.5%/2.5%, cream, diclofenac sodium, 1.5%, topical solution, comprising DMSO 45.5% (w/w) and propylene glycol, lidocaine hydrochloride, 4%, topical solution; and mixing the ingredients to generate a cream.

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Номер записи: 92
07-05-2020 дата публикации

METHODS OF TREATING PAIN AND/OR INFLAMMATORY DISORDERS USING LAPATINIB

Номер: US20200138818A1
Автор: Zhan Chang-Guo, Zheng Fang, Zhou Shuo, Zhou Ziyuan
Принадлежит:

A method of treating pain is disclosed, which involves administering an effective amount of lapatinib or a pharmaceutically-acceptable salt thereof to a subject in need of treatment for pain. 1. A method of treating pain , comprising: administering an effective amount of lapatinib or a pharmaceutically-acceptable salt thereof to a subject in need of treatment for pain.2. The method of and further comprising identifying the subject has having a need for analgesia.3. The method of claim 1 , wherein the pain is chronic.4. The method of claim 1 , wherein the pain is acute.5. The method of claim 1 , wherein the pain is selected from the group consisting of arthralgia (pain in joint) claim 1 , bone pain claim 1 , pain in an extremity (limb) claim 1 , musculoskeletal pain claim 1 , and headache.6. The method of claim 1 , wherein the subject does not have cancer.7. The method of claim 1 , wherein opioids are contraindicated for the subject.8. The method of claim 7 , wherein the subject has or is associated with one or more of the following conditions: history of or a current substance use disorder claim 7 , history of or a current alcohol addiction claim 7 , history of or a current opioid addiction or opioid use disorder (OUD) claim 7 , suspected opioid misuse (e.g. claim 7 , overdose claim 7 , early refills claim 7 , diversion claim 7 , taking more than prescribed).9. The method of claim 7 , wherein the subject has or is associated with one or more of the following conditions: prior diversion of controlled substances (providing the medication to someone for whom it was not intended) claim 7 , a family history of substance abuse claim 7 , a history of legal problems claim 7 , a history of incarceration claim 7 , frequent contact with high-risk individuals or environments claim 7 , social instability claim 7 , multiple psychosocial stressors claim 7 , history of previous problems with employers claim 7 , family claim 7 , and friends claim 7 , history of risk-taking and ...

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Номер записи: 93
17-06-2021 дата публикации

High concentration local anesthetic formulations

Номер: US20210177782A1
Автор: Arthur F. Michaelis, James N. Campbell
Принадлежит: Centrexion Therapeutics Corp, Vallinex Inc

A transdermal topical anesthetic formulation, which can be used to ameliorate or inhibit pain, has been developed. In the preferred embodiment, the topical anesthetic is a local anesthetic such as lidocaine, most preferably lidocaine free-base in a gel, and the dosage of the local anesthetic is effective in the painful area or immediately adjacent areas, to ameliorate or eliminate the pain. High concentration of local anesthetic in solution in the carrier is used to drive rapid release and uptake of the drug. Relief is typically obtained for a period of several hours.

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Номер записи: 94
31-05-2018 дата публикации

NOVEL ANTI-HUMAN NGF ANTIBODY FAB FRAGMENT

Номер: US20180147281A1
Автор: Aoki Toshiaki, FUJITA Hirotada, Tanaka Hirotsugu
Принадлежит: Astellas Pharma Inc.

To provide a superior anti-human NGF antibody Fab fragment that maintains a high neutralizing activity, and that reduces systemic side-effects arising from systemic exposure while expressing a local drug effect, and means for treating postoperative pain by using such antibody fragment. 1. An anti-human NGF antibody Fab fragment selected from the group consisting of (a) and (b):(a) an anti-human NGF antibody Fab fragment comprising a heavy-chain fragment consisting of the amino acid sequence of SEQ ID NO: 5 and a light-chain consisting of the amino acid sequence of SEQ ID NO: 8; and(b) an anti-human NGF antibody Fab fragment derived from at least one posttranslational modification of the anti-human NGF antibody Fab fragment of (a).2. The anti-human NGF antibody Fab fragment according to claim 1 , comprising a heavy-chain fragment consisting of the amino acid sequence of SEQ ID NO: 5 and a light-chain fragment consisting of the amino acid sequence of SEQ ID NO: 8.3. The anti-human NGF antibody Fab fragment according to claim 1 , wherein said at least one posttranslational modification is pyroglutamylation at the N-terminus of a heavy-chain variable region.4. The anti-human NGF antibody Fab fragment according to claim 1 , comprising a heavy-chain fragment consisting of the amino acid sequence of SEQ ID NO: 5 claim 1 , where a glutamine at amino acid position 1 of SEQ ID NO: 5 is modified to a pyroglutamic acid claim 1 , and a light-chain fragment consisting of the amino acid sequence of SEQ ID NO: 8.5. A polynucleotide comprising a base sequence encoding a heavy-chain fragment consisting of the amino acid sequence of SEQ ID NO: 5.6. An expression vector selected from the group consisting of (a) and (b):(a) an expression vector comprising a polynucleotide comprising a base sequence encoding a heavy-chain fragment consisting of the amino acid sequence of SEQ ID NO: 5, and a polynucleotide comprising a base sequence encoding a light-chain consisting of the amino acid ...

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Номер записи: 95
22-09-2022 дата публикации

Pain management methodology

Номер: US20220296536A1
Автор: David Flint
Принадлежит: Individual

A pain management system and methodology for preventing or alleviating chronic pain, and/or pain associated with a medical procedure prior to the medical procedure being performed, includes (a) aurally isolating a patient for a chosen period shortly prior to the patient receiving propofol in accordance with step (c), (b) exposing the patient to a repetitive, positive message during the chosen period, and (c) subsequently administering an effective quantity of propofol to the patient. For step (b), the repetitive, positive message may be delivered from a pre-recorded memory card inserted in headphones.

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Номер записи: 96
22-09-2022 дата публикации

Membrane Active Molecules

Номер: US20220296584A1
Автор: James M. SONNER, John L. Krstenansky
Принадлежит: Branequest Inc

A method of inducing anesthesia, sedation, and a method for treating disorders including central nervous system disorder, peripheral nervous system disorder, depression ischemia, and treatment with an anticonvulsant by administering an effective amount of a compound to a subject in need thereof.

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Номер записи: 97
22-09-2022 дата публикации

ORGANIC COMPOUNDS

Номер: US20220296591A1
Автор: Davis Robert, Li Peng, MATES Sharon, SNYDER Gretchen, VANOVER Kimberly, Yao Wei
Принадлежит:

The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving the 5-HTreceptor, the serotonin transporter (SERT), pathways involving the dopamine Dand Dreceptor signaling system, and/or the μ-opioid receptor. 2. The method according to claim 1 , wherein L is O.3. The method according to claim 1 , wherein Z is —CH(O—R)—.4. The method according to claim 1 , wherein Z is —C(═O)—.5. The method according to claim 1 , wherein Z is —O—.6. The method according to claim 1 , wherein X is —NH—.7. The method according to claim 1 , wherein X is —N(CH)—.10. The method according to wherein the compound is in the form of a salt.11. The method according to claim 1 , wherein the compound is administered to the patient in the form of a pharmaceutically acceptable composition comprising the compound in free or pharmaceutically acceptable salt form claim 1 , in admixture with a pharmaceutically acceptable diluent or carrier.12. The method of claim 11 , wherein the pharmaceutically acceptable diluent or carrier comprises a polymeric matrix.13. The method according to claim 12 , wherein the polymeric matrix is a biodegradable poly(d claim 12 ,l-lactide-co-glycolide) microsphere.14. The method according to wherein the central nervous system disorder is selected from idiopathic pain claim 1 , neuropathic pain claim 1 , chronic pain claim 1 , fibromyalgia claim 1 , dental pain claim 1 , and traumatic pain claim 1 , obsessive-compulsive disorder (OCD) claim 1 , obsessive-compulsive personality disorder (OCPD) claim 1 , general anxiety disorder claim 1 , social anxiety disorder claim 1 , panic disorder claim 1 , agoraphobia claim 1 , compulsive gambling disorder claim 1 , compulsive eating disorder claim 1 , body dysmorphic disorder claim 1 , hypochondriasis claim ...

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Номер записи: 98
22-09-2022 дата публикации

TREATMENT OF NEUROPATHIC PAIN ASSOCIATED WITH CHEMOTHERAPY-INDUCED PERIPHERAL NEUROPATHY

Номер: US20220296679A1
Автор: Lee JungHun, LEE Nayeon
Принадлежит:

The present invention relates to methods of treating chemotherapy-induced peripheral neuropathy. In particular, the methods provide a new way of reducing neuropathic pain associated with chemotherapy-induced peripheral neuropathy by administering a nucleic acid construct encoding human HGF proteins. This application further provides nucleic acid constructs, pharmacological compositions, and methods of administration of the nucleic acid constructs that are effective in treating the neuropathic pain. 1. A method of treating neuropathic pain associated with exposure to a chemotherapy drug , comprising the steps of: a first sequence comprising exons 1-4 of a human HGF gene or a degenerate sequence of the first sequence,', 'a second sequence comprising intron 4 of the human HGF gene or a fragment of the second sequence, and', 'a third sequence comprising exons 5-18 of the human HGF gene or a degenerate sequence of the third sequence., 'wherein the nucleic acid construct comprises, 'administering to a subject that has previously been exposed to the chemotherapy drug a first therapeutically effective amount of a nucleic acid construct capable of expressing two isoforms of a human hepatocyte growth factor (HGF) protein,'}2. The method of claim 1 , wherein the chemotherapy drug is selected from the group consisting of a plant alkaloid claim 1 , a taxane claim 1 , an epothilone claim 1 , a proteasome inhibitor claim 1 , an immunomodulator claim 1 , and an antineoplastic biologic.3. The method of claim 2 , wherein the chemotherapy drug is vincristine claim 2 , bortezomib claim 2 , paclitaxel claim 2 , or cisplatin.4. The method of claim 3 , wherein the chemotherapy drug is paclitaxel.5. The method of claim 3 , wherein the chemotherapy drug is vincristine.6. The method of claim 3 , wherein the chemotherapy drug is bortezomib.7. The method of claim 3 , wherein the chemotherapy drug is cisplatin.8. The method of claim 1 , wherein the subject is a human cancer patient.9. The ...

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Номер записи: 99
08-06-2017 дата публикации

Intravesical drug delivery methods and devices

Номер: US20170157360A1
Автор: Heejin Lee, Michael J. Cima
Принадлежит: Massachusetts Institute of Technology

An implantable medical device is provided for controlled drug delivery within the bladder, or other body vesicle. The device may include at least one drug reservoir component comprising a drug; and a vesicle retention frame which comprises an elastic wire having a first end, an opposing second end, and an intermediate region therebetween, wherein the drug reservoir component is attached to the intermediate region of the vesicle retention frame. The retention frame prevents accidental voiding of the device from the bladder, and it preferably has a spring constant selected for the device to effectively stay in the bladder during urination while minimizing the irritation of the bladder.

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Номер записи: 100