Поиск патентов

05-01-2012 дата публикации

Dpp iv inhibitor formulations

Номер: US20120003313A1

Автор: Anja Kohlrausch, Gerd Seiffert, Patrick Romer

Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention relates to pharmaceutical compositions of DPP IV inhibitors with an amino group, their preparation and their use to treat diabetes mellitus.

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Номер записи: 1

19-01-2012 дата публикации

Tablet formulation

Номер: US20120012499A1

Автор: Hikaru Fujita, Koichi Wada, Manabu Nakatani, Thomas Friedl

Принадлежит: Novo Nordisk AS

The present invention relates to a pharmaceutical fixed dose combination tablet comprising repaglinide and metformin. The present invention also provides a method of producing said tablet.

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Номер записи: 2

19-01-2012 дата публикации

Modified release formulations containing drug-ion exchange resin complexes

Номер: US20120015030A1

Автор: Ketan Mehta, Yu-Hsing Tu

Принадлежит: Tris Pharma Inc

A solid dose composition containing a mixture of a cured, modified release-barrier coated methylphenidate-ion exchange resin complex-matrix and an uncoated methylphenidate-ion exchange resin complex is described. The barrier coated methylphenidate-ion exchange resin complex-matrix comprises methylphenidate complexed with a pharmaceutically acceptable ion-exchange resin to form the complex which is admixed with a polymer to form a methylphenidate-ion exchange resin complex-matrix, which is subsequently coated with a modified release coating. The modified coating contains polyvinyl acetate polymer and a plasticizer and is cured.

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Номер записи: 3

23-02-2012 дата публикации

Tablet sleeve for improved performance

Номер: US20120045510A1

Автор: Joel Waldman

Принадлежит: Individual

A capsule-like dosage form, method for producing such dosage form and apparatus are disclosed. Such dosage form is achieved by applying a sleeve over the caplet to provide a coating which is smoother and easier to swallow than an uncoated caplet. The production of the capsule-like dosage form is readily facilitated by simple and inexpensive modifications to existing empty gelatin capsule making equipment.

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Номер записи: 4

08-03-2012 дата публикации

Therapeutic or prophylactic agent for dyskinesia

Номер: US20120058186A1

Автор: Kotoe Ohta, Suguru Takaki, Yasuhide Horiuch

Принадлежит: TORAY INDUSTRIES INC

The present invention relates to a stable orally disintegrating coated tablet containing a drug, wherein the tablet is coated with a coating layer containing a water-soluble substance and a polyvinyl alcohol resin of not less than 5% by weight based on the weight of the coating layer, the water-soluble substance dissolving in an amount of 1 g or more in less than 10 mL of water at 20° C., having a hydroxyl group(s) in its molecule, and having a molecular weight of not more than 200 per a unit hydroxyl group. There is provided a stable orally disintegrating coated tablet which does not cause a crack in the coating layer even when the orally disintegrating tablet has been swollen by moisture absorption under high humidity, while ensuring rapid disintegration properties in an oral cavity. In the case of an orally disintegrating tablet containing a light-unstable drug, degradation of the drug can be suppressed by blending a light shading agent in the coating layer.

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Номер записи: 5

05-04-2012 дата публикации

Easily administrable solid preparation

Номер: US20120082723A1

Автор: Kuniomi Warabino, Yumio Kudou

Принадлежит: Mochida Pharmaceutical Co Ltd

It is an object to provide a coating composition, which is used for an orally-administered preparation, the administering property of which has been improved, and/or an easily administrable preparation that does not affect dissolution property. The aforementioned object can be achieved using a coating composition comprising a first thickener selected from the group consisting of a carboxyvinyl polymer and sodium alginate, a polyvalent metal compound, and at least one type of a second thickener selected from the group consisting of xanthan gum, guar gum and sodium alginate, with the proviso that when the first thickener is sodium alginate the second thickener is not sodium alginate, or using a coating composition comprising, as thickeners, hydroxypropylmethylcellulose and sugar or sugar alcohol having a solubility at 20° C. of 30 or more.

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Номер записи: 6

12-07-2012 дата публикации

Use of a copolymer in the form of a solubiliser for a poorly water-soluble compound

Номер: US20120178728A1

Автор: Kathrin Meyer-Böhm, Marianna Pierobon, Nathalie Bouillo, Rainer Dobrawa, Ralf Widmaier, Ronald Frans Maria Lange

Принадлежит: BASF SE

The use of copolymers obtained by free-radical polymerization of a mixture of i) 30 to 80% by weight of N-vinyllactam, ii) 10 to 50% by weight of vinyl acetate, and iii) 10 to 50% by weight of a polyether, with the proviso that the total of components i), ii) and iii) equals 100% by weight, as solubilizers for slightly water-soluble substances.

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Номер записи: 7

26-07-2012 дата публикации

Oral dosage forms

Номер: US20120189693A1

Автор: Charanjit R. Behl, Christopher C. Dick, David F. Erkoboni, Gary Bubb

Принадлежит: Elite Laboratories Inc

Aspects of the present invention are directed to oral dosage forms comprising a compressed microtablet, wherein said microtablet has a major dimension that is between about 0.25 mm and about 1.0 mm and comprises at least about 0.01 weight percent of at least one pharmaceutically active agent that is distributed substantially throughout said microtablet. Additional aspects of the present invention are directed to methods for producing compressed microtablets having a major dimension that is between about 0.25 mm and about 1.0 mm.

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Номер записи: 8

02-08-2012 дата публикации

Deferacirox dispersible tablets

Номер: US20120196909A1

Автор: Jean-Pierre Cassiere, Karine Deffez

Принадлежит: NOVARTIS AG

The invention pertains to dispersible tablets comprising as active ingredient 4-[3,5-bis(2-hydroxyphenyl)-[1,2,4]triazol-1-yl]benzoic acid or pharmaceutically acceptable salt thereof in an amount of from 5 to 40% in weight by weight of the total tablet.

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Номер записи: 9

06-09-2012 дата публикации

Product for the management of inflammations, pressure sores and/or oral sores (aphthas) as well as the use of such product

Номер: US20120225111A1

Автор: Gert Hartmut Scholz

Принадлежит: Lohmann and Rauscher GmbH and Co KG

The invention relates to a product for the management of inflammations, pressure sores and/or oral sores (aphthas) which is made predominantly, and preferably completely, from a bioresorbable material, with the bioresorbable material exhibiting a flexible and/or compressible pad element which adheres to the mucosa, and in particular being designed completely as a pad element.

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Номер записи: 10

04-10-2012 дата публикации

Devices and methods for weight control and weight loss

Номер: US20120251589A1

Автор: Paolo Costa

Принадлежит: TERATEKNE Inc

The present invention provides, compositions, devices; and methods for affecting, among other things, weight loss and/or weight control, by sequestering nutrients or other compounds such as toxins from absorption in the digestive tract. The compositions, devices, and methods employ one or more members made of a compressible, absorbent matrix material. In various embodiments, the matrix material is suitable for routine use. The compressible absorbent matrix material has a size, shape and/or geometry configured for efficient packing into a small space, and/or configured to absorb and substantially retain digested material in the stomach. The devices and compositions may further comprise one or more hydrogel(s), soluble or insoluble fibers, waxes and/or gums to provide the desired mechanical properties and/or absorptive or shielding properties.

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Номер записи: 11

20-12-2012 дата публикации

SOLID DISPERSIONS CONTAINING 20-O-beta-D-GLUCOPYRANOSYL-20(S)-PROTOPANAXADIOL

Номер: US20120322752A1

Автор: Bong Hang Hur, Jae Won Jang, Sang Cheol Chi, Sung Kyun Lee, Yong-Duck Park

Принадлежит: Il Hwa Co Ltd

The present invention provides solid dispersion, comprising: 20-O-β-D-glucopyranosyl-20(S)-protopanaxadiol which is a pharmacologically active ingredient; and a saturated polyglycolized glyceride which is a lipid matrix. The solid dispersion of the present invention has effects of increasing dissolution rate of 20-O-β-D-glucopyranosyl-20(S)-protopanaxadiol.

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Номер записи: 12

03-01-2013 дата публикации

Utilization of Dialkylfumarates

Номер: US20130004526A1

Автор: Hans-Peter Strebel, Rajendra Kumar Joshi

Принадлежит: Biogen Idec International GmbH

The present invention relates to the use of certain dialkyl fumarates for the preparation of pharmaceutical preparations for use in transplantation medicine or for the therapy of autoimmune diseases and said compositions in the form of micro-tablets or pellets. For this purpose, the dialkyl fumarates may also he used in combination with conventional preparations used in transplantation medicine and immunosuppressive agents, especially cyclosporines.

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Номер записи: 13

10-01-2013 дата публикации

Modified release formulations of memantine oral dosage forms

Номер: US20130012593A1

Автор: Antonia Periclou, Mahendra G. Dedhiya, Niranjan Rao, Shashank Mahashabde, Suneel K. Rastogi, Wattanaporn Abramowitz

Принадлежит: Forest Laboratories Holdings Ltd

The present invention provides pharmaceutical compositions given once daily containing at least one therapeutically active ingredient selected from the group consisting of memantine and a pharmaceutically acceptable salt of memantine, and a pharmaceutically acceptable polymeric matrix carrier. The dosage forms of the invention sustain the release of the therapeutically active agent from about 4 to about 24 hours when said dosage form is exposed to aqueous solutions, following entry of said form into a use environment, wherein said dosage form has a dissolution rate of more than about 80% after passage of about 6 hours to about 12 hours following said entry into said use environment.

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Номер записи: 14

24-01-2013 дата публикации

Controlled Release Formulations of Opioids

Номер: US20130022646A1

Автор: Edward M. Rudnic, Gary W. Pace, Michael Vachon

Принадлежит: Individual

Pharmaceutical formulations containing opioid components that each has a release profile. The components may provide immediate or controlled release of the opioid. The invention is also directed to methods of controlling release of one or more opioid compounds and methods of treating pain.

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Номер записи: 15

14-02-2013 дата публикации

Quick Dissolving, Long Acting Zinc Therapeutic Formulations

Номер: US20130039981A1

Автор: Subraman Rao Cherurkuri

Принадлежит: Individual

The present invention comprises a quick dissolving, long acting zinc therapeutic cold formulation containing high levels of an active compound encapsulated within bioadhesive/muco-adhesive polymers as a controlled release oral drug delivery system. The composition allows for increased residence time for enhanced prophylactic and therapeutic efficacy within the mouth and oral cavity. This allows for a reduction in the number of doses necessary to achieve therapeutic relief which will result in increased patience compliance.

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Номер записи: 16

07-03-2013 дата публикации

Oral drug delivery system

Номер: US20130059004A1

Автор: Amarjit Singh, Nitin Bhalachandra Dharmadhikari, Yashoraj Rupsinh Zala

Принадлежит: Sun Pharma Advanced Research Co Ltd

An oral drug delivery system comprising a coated tablet having one or more surfaces. The coated tablet further comprises a core and a coating surrounding the core. The core comprises an active ingredient composition comprising at least one active ingredient and a pharmaceutically acceptable excipient and a reactive composition located in an immediate vicinity of one or more preselected surfaces. The coating is operable to be reliably removed fully from the one or more of the preselected surfaces of the tablet upon contact with an aqueous environment, but not removed from at least one of the surfaces.

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Номер записи: 17

07-03-2013 дата публикации

Device For The Manufacture Of A Dosage Form With A Hole And Method Of Manufacture

Номер: US20130059062A1

Автор: Girish Kumar Jain, Rahul Sudhakar Dabre, Ramakant Kashinath Gundu

Принадлежит: Individual

This invention is related to a device for the manufacture of a dosage form with a hole and method of manufacture. The dosage form may be a modified release dosage form comprising a core coated with a polymeric coat comprising one or more rate controlling polymers, said dosage form having a hole extending through the dosage form resulting in an inner radial surface and an outer radial surface, said core comprising at least one therapeutically active ingredient, characterized in that the inner radial surface is partially coated with said polymeric coat.

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Номер записи: 18

21-03-2013 дата публикации

Solid dispersion comprising an anti-hiv agent

Номер: US20130072531A1

Автор: Ellen Verhoeven, Jody Voorspoels, Yves Gonnissen, Yves Ruysschaert

Принадлежит: Aicuris GmbH and Co KG

The present invention relates to solid dispersions comprising a compound of formula or a salt, a solvate or a solvate of a salt thereof, dispersed in a polymeric, inert, non-toxic, pharmaceutically acceptable excipient.

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Номер записи: 19

04-04-2013 дата публикации

Taste masked pharmaceutical composition

Номер: US20130084332A1

Автор: Annette Grave, Martin Folger, Norbert Poellinger, Randolph Seidler, Stefan Lehner

Принадлежит: BOEHRINGER INGELHEIM VETMEDICA GMBH

This application relates to taste masked multi-layered particles an inert core, one or more coating layer(s) comprising a pharmaceutically active ingredient and a binder, an intermediate coating layer (seal coating) free from a low molecular weight water-soluble ionic compound and comprising a water-soluble pharmaceutical film-forming compound selected from (i) HPMC and PEG or (ii) PVP, and an outer coating layer (final or taste masking coating) free from a low molecular weight water-soluble ionic compound and comprising (i) a poly(meth)acrylate or (ii) a mixture comprising 60-90% (w/w) EC and 10-40% (w/w) HPMC, wherein the pharmaceutically active ingredient is water-soluble and comprises either at least one basic group and/or a bitter taste. Further disclosed are methods for the production of such particles and pharmaceutical compositions comprising them.

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Номер записи: 20

11-04-2013 дата публикации

Sustained Release Pharmaceutical Compositions for Highly Water Soluble Drugs

Номер: US20130089608A1

Автор: Bledsoe David L., CHEN Andrew Xian

Принадлежит: Farnam Companies, Inc.

The present invention provides pharmaceutical compositions for controlled release of pharmaceutically active agents, especially those with a high water solubility, high dose, and/or short half-life. In addition, the present application provides methods for preparing and using such pharmaceutical compositions. 1. A sustained release pharmaceutical tablet , said tablet comprising:tramadol micronized at a dose selected from the group consisting of 90 mg, 180 mg, 300 mg and 600 mg;a matrix comprising hydroxypropylmethyl cellulose (HMPC) and the micronized tramadol dispersed in the matrix;microcrystalline cellulose; anda tablet lubricant.2. The pharmaceutical tablet of claim 1 , wherein the pharmaceutically active agent contributes greater than 15% of the total weight of the pharmaceutical composition.3. The pharmaceutical tablet of claim 1 , wherein the pharmaceutically active agent contributes greater than 50% of the total weight of the pharmaceutical composition.4. The pharmaceutical tablet of claim 1 , wherein the pharmaceutically active agent is present in an amount of about 50% to about 80% by weight.5. The pharmaceutical tablet of claim 1 , wherein the hydrophilic polymer is present in an amount of about 15% to about 50% by weight.6. The pharmaceutical tablet of claim 1 , wherein the HPMC is a high molecular weight HPMC in an amount of about 20% to about 30% by weight of the tablet.7. The pharmaceutical tablet of claim 1 , wherein the tableting lubricant is present in an amount of about 1% to about 3% by weight of the tablet.8. The pharmaceutical tablet of claim 7 , wherein the tablet lubricant is magnesium stearate.9. The pharmaceutical tablet of claim 1 , further comprising a coating on the tablet.10. The pharmaceutical tablet of claim 9 , wherein said coating is a release-controlling layer.11. The pharmaceutical tablet of claim 9 , wherein said coating constitutes about 1% to about 5% by weight of the tablet.12. The pharmaceutical tablet of claim 9 , wherein ...

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Номер записи: 21

18-04-2013 дата публикации

Pharmaceutical compositions of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyriodin-2-yl)benzoic acid and administration thereof

Номер: US20130095181A1

Автор: Christopher Ryan Young, Irina Nikolaevna Kadiyala, Marinus Jacobus Verwijs, Ritu Rohit Kaushik, Rossitza Gueorguieva Alargova

Принадлежит: Vertex Pharmaceuticals Inc

A pharmaceutical composition comprising Compound 1, (3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid), and at least one excipient selected from: a filler, a diluent, a disintegrant, a surfactant, a binder, a glidant and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Methods for treating a patient in need thereof include administering an oral pharmaceutical formulation of Compound 1 to the patient.

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Номер записи: 22

25-04-2013 дата публикации

Method and agent for detecting drugs in beverages

Номер: US20130098286A1

Автор: Catherine Herry, Emmanuel Dupau, Pauline Contamin

Принадлежит: Ethypharm SAS

The present invention relates to a method for combating chemical submission, which comprises: putting into solution, in a beverage, a pharmaceutical form comprising an active ingredient and at least 0.05 mg, preferably from 0.2 to 5 mg, even more preferentially from 0.3 to 2 mg of at least one water-soluble colouring agent chosen from: indigocarmine or E 132, erythrosine or E 127, brilliant blue FCF, alphazurine FG, fast green FCF, quinzarine green SS, orange II, tartrazine and Sunset yellow FCF, detecting the pharmaceutical form, said detection being characterized by the immediate change in colour of the beverage; it also relates to the use of said colorant for combating chemical submission, and also to a non-film-coated solid pharmaceutical form comprising said colorant.

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Номер записи: 23

02-05-2013 дата публикации

Dual Controlled Release Dosage Form

Номер: US20130108693A1

Автор: Juan A. Vergez, Marcelo A. Ricci

Принадлежит: OSMOTICA KERESKEDELMI ES SZOLGALTATO KFT

A dosage form that provides a controlled release of at least two different active agents is provided. Particular embodiments include a dosage form that provides therapeutically effective levels of a first active agent and a second active agent in a mammal for an extended period of time following oral administration. An osmotic device containing a bi-layered core is provided. The osmotic device provides a dual controlled release of both drugs from the core. The layers of the core are in stacked, substantially concentric or substantially eccentric arrangement.

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Номер записи: 24

23-05-2013 дата публикации

Solid Drug Tablets for Implantable Drug Delivery Devices

Номер: US20130129824A1

Автор: Daniel Karen Danielle, Hutchins Burleigh M., Larrivee-Elkins Cheryl, Lee Heejin

Принадлежит: TARIS BIOMEDICAL, INC.

A drug dosage form is provided in the form of a solid tablet which is greater than 50% by weight the local anesthetic agent. The local anesthetic agent may be selected from the group consisting of an aminoamide, an aminoester, and a combination thereof. The drug tablet may be in the form of a mini-tablet which is greater than 70 wt % drug, with the balance being excipient. For example, the anesethetic agent may include lidocaine, in a salt or base form, combined with binder and lubricant excipients. Implantable drug delivery devices including the tablets are also provided, e.g., one or more of the drug tablets may be contained in a biocompatible housing. The drug tablets may be substantially cylindrical with flat end faces, and the device may have from 10 to 100 drug tablets aligned in the housing with the flat end faces of adjacent tablets abutting one another. 1. A solid drug unit comprising:a drug in the form of a mini-tablet which is greater than 70% by weight the drug, with the balance being at least one excipient,wherein the mini-tablet is cylindrical with flat end faces, the length of the tablet exceeding its diameter so that the mini-tablet has an aspect ratio of greater than 1:1, andwherein the mini-tablet has a diameter from 1.0 mm to 3.2 mm and a length from 1.7 mm to 4.8 mm, such that the mini-tablet is sized and shaped for insertion through the urethra of a patient.2. The solid drug unit of claim 1 , wherein the mini-tablet has a diameter from 1.5 mm to 3.1 mm and a length from 2.0 mm to 4.5 mm.3. The solid drug unit of claim 1 , wherein the drug is between 70 wt % and 99 wt % of the mini-tablet.4. The solid drug unit of claim 1 , wherein the drug is an anesthetic agent claim 1 , and antimicrobial agent claim 1 , or a chemotherapeutic agent.5. The solid drug unit of claim 4 , wherein the excipient comprises a binder and a lubricant.6. The solid drug unit of claim 1 , wherein the drug comprises lidocaine.7. The solid drug unit of claim 1 , wherein the ...

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Номер записи: 25

23-05-2013 дата публикации

Pharmaceutical composition for treatment of respiratory tract infections

Номер: US20130131033A1

Автор: Mayank Jasvantbhai Shah

Принадлежит: TOYOCHEM LABORATORIES

The present invention relates to a pharmaceutical composition comprising ciprofloxacin or salts of thereof and amoxycillin or salts of thereof and other pharmaceutical excipients. The present invention provides more reliable effect against all bacteria, including the most commonly causative streptococci , responsible for especially respiratory tract infections. The invention makes up for the weakness of ciprofloxacin against streptococci.

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Номер записи: 26

27-06-2013 дата публикации

Small-volume oral transmucosal dosage forms

Номер: US20130165481A1

Автор: Andrew I. Poutiatine, Larry Hamel, Pamela Palmer, Stelios Tzannis, Thomas Schreck

Принадлежит: AcelRx Pharmaceuticals Inc

Small-volume oral transmucosal dosage forms or NanoTabs® comprising a predetermined amount of a pharmaceutically active drug are provided. Exemplary applications include use of the NanoTabs® to administer a drug for the treatment of acute, post-operative or breakthrough pain.

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Номер записи: 27

01-08-2013 дата публикации

Low Concentration Meloxicam Tablets

Номер: US20130195977A1

Автор: Folger Martin A., Lehner Stefan, Schmitt Horst

Принадлежит: BOEHRINGER INGELHEIM VETMEDICA GMBH

A solid tablet formed through direct compression of powder, the powder comprising meloxicam as an active ingredient and one or more excipients which are homogenously dispersed within the tablet that can be broken into two, three or four units with each unit containing equal amounts of the meloxicam. 1. A method of forming a chewable , solid tablet for administration to companion animals , the method comprising:(a) mixing meloxicam or a pharmaceutically acceptable salt thereof with a first portion of a primary filler to form a first mixture,(b) screening the first mixture through a mesh having a mesh size of 0.6 mm to 1.5 mm to form a first screened mixture;(c) mixing a second portion of the first filler with a second filler to form a second mixture;(d) screening the second mixture through a mesh having a mesh size of 0.6 mm to 1.5 mm to form a second screened mixture;(e) combining the first screened mixture with the second screened mixture to form a final mixture;(f) compressing the final mixture into a tablet having a diameter of 10 mm-20 mm; and(g) scoring the tablet to enable the division of the tablet into individually administered doses,wherein the meloxicam or pharmaceutically is homogenously distributed within the tablet.2. The method of further comprising screening the final mixture through a mesh having a mesh size of 0.6 mm to 1.5 mm to form a final screened mixture before compression.3. The method according to wherein:the first and second fillers are selected from the group consisting of calcium phosphate, lactose, maltodextrin, mannitol, sorbitol, cross-linked polyvinyl pyrrolidone, sodium carboxymethyl cellulose, starch and microcrystalline cellulose; andthe first filler is different from the second mixture.4. The method according to claim 1 , further comprising:mixing a first excipient with a second excipient to form an excipient mixture;screening the excipient mixture through a mesh having a mesh size of 0.6 mm to 1.5 mm to form a screened excipient ...

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Номер записи: 28

01-08-2013 дата публикации

Darunavir Compositions

Номер: US20130195978A1

Автор: KAMALAKAR REDDY Goli, KHADGAPATHI Podili, Parthasarashi Reddy Bandi

Принадлежит: HETERO RESEARCH FOUNDATION

The present invention relates to an oral pharmaceutical composition of amorphous darunavir. 1. An oral pharmaceutical composition comprises amorphous darunavir having a dparticle size in the range of about 150 μm to 250 μm.2. The oral pharmaceutical composition according to claim 1 , wherein the dparticle size is in the range of 175 to 225 μm.3. The oral pharmaceutical composition according to claim 1 , wherein dparticle size is in the range of 190 to 200 μm.4. The oral pharmaceutical composition according to claim 1 , wherein the composition is in the form of tablets.5. The oral pharmaceutical composition according to claim 4 , wherein the tablet is film coated.6. The oral pharmaceutical composition according to claim 1 , wherein the composition may contain one or more additional excipients.7. The oral pharmaceutical composition according to claim 6 , the excipients are selected from diluents claim 6 , binders claim 6 , disintegrants and lubricants.8. The oral pharmaceutical composition according to claim 7 , wherein the diluent is selected from lactose claim 7 , sucrose claim 7 , glucose claim 7 , mannitol claim 7 , sorbitol claim 7 , calcium carbonate claim 7 , microcrystalline cellulose claim 7 , Prosolv claim 7 , magnesium stearate and mixtures thereof.9. The oral pharmaceutical composition according to claim 7 , wherein the diluent is Prosolv.10. The oral pharmaceutical composition according to claim 7 , wherein the binder is selected from L-Hydroxy propyl cellulose claim 7 , polyvinyl pyrrolidine claim 7 , hydroxyl propyl methyl cellulose claim 7 , hydroxyl ethyl cellulose and pre-gelatinized starch.11. The oral pharmaceutical composition according to claim 7 , wherein the disintegrant is selected from croscarmellose sodium claim 7 , crospovidone claim 7 , sodium starch glycolate and low substituted hydroxyl propyl cellulose.12. The oral pharmaceutical composition according to claim 7 , wherein the disintegrant is selected from low substituted hydroxyl propyl ...

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Номер записи: 29

01-08-2013 дата публикации

Parenteral Formulations Of Dopamine Agonists

Номер: US20130197005A1

Автор: Anthony H. Cincotta

Принадлежит: VEROSCIENCE LLC

This invention relates to stable pharmaceutical compositions for parenteral administration comprising dopamine agonists and peripheral acting agents useful for treatment of metabolic disorders or key elements thereof. The parenteral dosage forms exhibit long stable shelf life and distinct pharmacokinetics.

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Номер записи: 30

08-08-2013 дата публикации

RAPIDLY DISINTEGRATING COATED TABLETS

Номер: US20130202700A1

Автор: Bean Anthony S., Franzoi Fernanda, Waldman Joel H.

Принадлежит: McNeil-PPC, Inc.

Coated dosage forms comprising a tablet core, preferably in compressed form, that has a coating over its exterior surface and one or more patterns debossed in the tablet surface are disclosed. Methods for manufacturing such dosage forms are also disclosed. 1. A dosage form comprising:a) a core having an exterior surface and first and second ends;b) at least one debossed pattern in said core;wherein said at least one debossed pattern contains at least one wall;wherein the at least one wall contains a wall angle from vertical of about 25 degrees or less; andc) a coating over portions of the exterior surface of the core.2. The dosage form of claim 1 , wherein the at least one debossed pattern contains a depth of more than about 0.25 mm.3. The dosage form of claim 1 , wherein the coating is a film-based coating.4. The dosage form of claim 3 , wherein the film-based coating comprises hydroxypropylmethylcellulose.5. The dosage form of claim 1 , comprising at least two patterns debossed in said core.6. The dosage form of claim 1 , wherein the core is a compressed tablet.7. The dosage form of claim 6 , wherein the compressed tablet has an elongated shape.8. The dosage form of claim 1 , wherein the core comprises at least one active ingredient and wherein the dosage form allows for dissolution of the at least one active ingredient following an immediate release profile.9. The dosage form of claim 8 , wherein the at least one active ingredient is selected from the group consisting of acetaminophen claim 8 , acetyl salicylic acid claim 8 , ibuprofen claim 8 , naproxen claim 8 , ketoprofen claim 8 , flurbiprofen claim 8 , diclofenac claim 8 , cyclobenzaprine claim 8 , pseudoephedrine claim 8 , phenylephrine claim 8 , phenylpropanolamine claim 8 , chlorpheniramine claim 8 , dextromethorphan claim 8 , diphenhydramine claim 8 , astemizole claim 8 , terfenadine claim 8 , fexofenadine claim 8 , loratadine claim 8 , desloratadine claim 8 , cetirizine claim 8 , and pharmaceutically ...

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Номер записи: 31

08-08-2013 дата публикации

Pharmaceutical composition for the prolonged release of trimetazidine

Номер: US20130202710A1

Автор: Christophe Hermelin, Jean-Manuel Pean, Patrick Genty

Принадлежит: Laboratoires Servier SAS

Composition for the prolonged release of trimetazidine wherein the inner phase comprises trimetazidine and the outer layer comprises a retardant and an anti-agglomerant.

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Номер записи: 32

12-09-2013 дата публикации

PHARMACEUTICAL COMPOSITION COMPRISING CITRATE AND BICARBONATE SALTS, AND USE THEREOF FOR TREATING CYSTINURIA

Номер: US20130236545A1

Автор: Granier Luc-Andre, Guittet Catherine, Roussel-Maupetit Caroline

Принадлежит: ADVICENNE

A solid oral pharmaceutical composition in the form of tablets including:—a first solid oral pharmaceutical formulation in the form of at least one micro-tablet, the micro-tablet consisting of a core including at least one Krebs cycle precursor salt as active ingredient, and of a coating including at least one coating agent, and—a second oral pharmaceutical formulation in the form of at least one mini-tablet, the mini-tablet consisting of a core including at least one bicarbonate salt as active ingredient and at least one prolonged-release matrix, and of a coating including at least one coating agent. The use thereof as a medicament, in particular in the treatment and/or prevention of cystinuria. 1. Solid pharmaceutical composition for oral use in the form of tablets comprising: 'and', 'a first solid pharmaceutical formulation for oral use in the form of at least one microtablet, said microtablet being constituted by a core comprising at least one Krebs cycle precursor salt as active ingredient, and a coating comprising at least one coating agent,'}a second pharmaceutical formulation for oral use in the form of at least one mini-tablet, the mini-tablet being constituted by a core comprising at least one bicarbonate salt as active ingredient and at least one sustained-release matrix, and a coating comprising at least one coating agent.2. Composition according to claim 1 , such that it comprises from 30 to 70% of the first formulation and from 70 to 30% of the second formulation claim 1 , by weight relative to the total weight of the composition.3. Composition according to claim 1 , such that the first formulation comprises from 40% to 80% claim 1 , preferably from 50 to 70% claim 1 , by weight Krebs cycle precursor salt based on the total weight of the first formulation and such that the second formulation comprises from 40% to 80% claim 1 , preferably from 50 to 80% claim 1 , by weight bicarbonate salt based on the total weight of the second formulation.4. ...

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Номер записи: 33

26-09-2013 дата публикации

Pharmaceutical dosage form

Номер: US20130251759A1

Автор: Andrea Schüessele, Anne Faure, Elisabeth Arkenau-Maric, Eric Galia, Eugeen Marie Jozef Jans, Filip René Irena Kiekens, Iris Ziegler, Jody Firmin Marceline Voorspoels, Johannes Bartholomuäs, Lutz Barnscheid, Marc FREVEL

Принадлежит: GRUENENTHAL GmbH

The invention relates to a pharmaceutical dosage form, preferably with controlled release of a pharmacologically active compound (A) contained therein, the pharmaceutical dosage form very preferably being tamper-resistant and most preferably having a breaking strength B 1 of at least 500 N in direction of extension E 1 and having a breaking strength B 2 of less than 500 N in direction of extension E 2 .

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Номер записи: 34

26-09-2013 дата публикации

Tamper resistant dosage forms

Номер: US20130251801A1

Автор: Edward P. O'Donnell, Haiyong H. Huang, Richard O. Mannion, William H. McKenna

Принадлежит: Purdue Pharma LP

The present invention relates to pharmaceutical dosage forms, for example to a tamper resistant dosage form including an opioid analgesic, and processes of manufacture, uses, and methods of treatment thereof.

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Номер записи: 35

26-09-2013 дата публикации

Method to improve the safety of handling of high potency drugs in solid dosage forms without changing their efficacy

Номер: US20130251804A1

Автор: Rebanta Bandyopadhyay, Susen Werle

Принадлежит: Emphascience Inc

A method to improve the safety of handling of drug substances that are dispensed as solid oral dosage forms is described that does not alter the drug-release profile and the therapeutic efficacy of the pharmaceutical product.

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Номер записи: 36

03-10-2013 дата публикации

Tamper resistant dosage forms

Номер: US20130259938A1

Автор: Edward P. O'Donnell, Haiyong H. Huang, Richard O. Mannion, William H. McKenna

Принадлежит: Purdue Pharma LP

The present invention relates to pharmaceutical dosage forms, for example to a tamper resistant dosage form including an opioid analgesic, and processes of manufacture, uses, and methods of treatment thereof.

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Номер записи: 37

03-10-2013 дата публикации

Controlled release dosage forms

Номер: US20130259941A1

Автор: Edward O'Donnell

Принадлежит: Purdue Pharma LP

Dosage forms having a core having a surface having means for controlling release(s) on an active agent(s); methods of manufacturing, tools used in manufacturing; and uses of the dosage forms are described.

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Номер записи: 38

10-10-2013 дата публикации

Tableted compositions containing atazanavir

Номер: US20130266648A1

Автор: Faranak Nikfar, Otilia May Koo, Steven Diaz

Принадлежит: Bristol Myers Squibb Co

Disclosed are compressed tablets containing atazanavir sulfate, optionally with another active agents, e.g., anti-HIV agents, granules that contain atazanavir sulfate and an intragranular lubricant that can be used to make the tablets, compositions comprising a plurality of the granules, processes for making the granules and tablets, and methods of treating HIV.

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Номер записи: 39

17-10-2013 дата публикации

Pharmaceutical compositions of linezolid

Номер: US20130274262A1

Автор: BANDI Parthasaradhi Reddy, Goli Kamalakar Reddy, Lekkala Vamshi Krishna, Podili Khadgapathi

Принадлежит: HETERO RESEARCH FOUNDATION

The present invention relates to stable pharmaceutical compositions comprising linezolid crystalline Form III with one or more pharmaceutically acceptable excipients, wherein the composition retains linezolid in its original crystalline form.

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Номер записи: 40

31-10-2013 дата публикации

Bromocriptine Formulations

Номер: US20130287848A1

Автор: Anthony H. Cincotta, Craig Michael Bowe, Laura Jean Weston, Paul Clark Steams

Принадлежит: VEROSCIENCE LLC

The present application describes pharmaceutical formulations of bromocriptine mesylate and methods of manufacturing and using such formulations. The formulations are useful for improving glycemic control in the treatment of type 2 diabetes.

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Номер записи: 41

31-10-2013 дата публикации

Liquid ganaxolone formulations and methods for the making and use thereof

Номер: US20130287851A1

Автор: Kenneth Shaw, Mingbao Zhang

Принадлежит: Marinus Pharmaceuticals Inc

In certain embodiments, the invention is directed to composition comprising stable particles comprising ganaxolone, wherein the volume weighted median diameter (D50) of the particles is from about 50 nm to about 500 nm.

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Номер записи: 42

31-10-2013 дата публикации

Drug eluting ocular implant

Номер: US20130289467A1

Автор: David Applegate, David Haffner, Harold Heitzmann, Ken CURRY

Принадлежит: Dose Medical Corp

Disclosed herein are drug delivery devices and methods for the treatment of ocular disorders requiring targeted and controlled administration of a drug to an interior portion of the eye for reduction or prevention of symptoms of the disorder. The devices are capable of controlled release of one or more drugs and may also include structures which allow for treatment of increased intraocular pressure by permitting aqueous humor to flow out of the anterior chamber of the eye through the device.

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Номер записи: 43

07-11-2013 дата публикации

Pharmaceutical Compositions Containing Dimethyl Fumarate

Номер: US20130295169A1

Автор: Dawson Katherine, Goldman David, Nirula Ajay

Принадлежит:

Provided herein are compositions containing compounds, or pharmaceutically acceptable salts, that metabolize to monomethyl fumarate with certain pharmacokinetic parameters and methods for treating, prophylaxis, or amelioration of neurodegenerative diseases including multiple sclerosis using such compositions in a subject, wherein if the compositions contain dimethyl fumarate, the total amount of dimethyl fumarate in the compositions ranges from about 43% w/w to about 95% w/w. 1. A composition comprising dimethyl fumarate and one or more excipients , wherein the total amount of dimethyl fumarate in the composition ranges from about 43% w/w to about 95% w/w.2. (canceled)3. The composition of claim 1 , wherein the total amount of dimethyl fumarate in the composition is about 65% w/w.4. The composition of claim 1 , wherein the total amount of dimethyl fumarate in the composition is about 95% w/w.5. (canceled)6. (canceled)7. The composition of claim 1 , wherein the composition is in the form of a compact.8. The composition of claim 7 , wherein the compact has a tensile strength that is equal to or greater than about 1.5 MPa at an applied pressure of about 100 MPa.9. (canceled)10. The composition of claim 7 , wherein the compact is in the form of a microtablet.11. The composition of claim 10 , wherein dimethyl fumarate is the only active ingredient in the composition.12. The composition of claim 10 , wherein the microtablet is uncoated and has a mean diameter ranging from about 1 mm to about 3 mm.13. (canceled)14. A composition comprising claim 10 , about 43% w/w to about 95% w/w dimethyl fumarate claim 10 , a total amount of about 3.5% w/w to about 55% w/w of one or more fillers claim 10 , a total amount of about 0.2% w/w to about 20% w/w of one or more disintegrants claim 10 , a total amount of about 0.1% w/w to about 9.0% w/w of one or more glidants claim 10 , and a total amount of about 0.1% w/w to about 3.0% w/w of one or more lubricants.15. (canceled)16. (canceled) ...

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Номер записи: 44

07-11-2013 дата публикации

COMPOSITIONS FOR CONTROL OF DRUG ABUSE

Номер: US20130295170A1

Автор: Dordunoo Stephen

Принадлежит: KYDES Pharmaceuticals LLC

Opiates, amphetamines, barbiturates and other drugs such as benzodiazepines are extensively abused or misused and are frequently the cause of death by overdosing. These drugs are also prone to oxidation and the final degradation products depend on the reactants and the reaction conditions. This invention describes the use of inactivating agents such as permanganates, peroxides, persulfates, bismuthates, periodates or other oxidants in a dosage form as an approach to minimize abuse and overdose. The product is designed such that the inactivating agent is released if there is an attempt to extract the drug from the formulation or in cases of overdose. Once released, the inactivating agent quickly degrades the drug and converts it into inactive compounds. Since the reactants (drug and inactivating agent) are incompatible in situations of normal drug usage, they are kept separated within the vehicle of the invention, but released for interaction in case of misuse. A catalyst may be included in the formulation to facilitate the reaction. 1. A drug formulation , comprising:an active component,a degrading component capable of degrading the active component,and a membrane separating the active component from the degrading component,wherein the membrane prevents degradation of the active component by the degrading component.2. The drug formulation of claim 1 , wherein the membrane is resistant to gastric fluids.3. The drug formulation of claim 1 , wherein the active component is selected from the group consisting of an opiate claim 1 , an amphetamine claim 1 , a barbiturate claim 1 , or a digoxin.4. The drug formulation of claim 3 , wherein the opiate is selected from the group consisting of morphine claim 3 , codeine claim 3 , thebaine claim 3 , papaverine claim 3 , and derivatives thereof.5. The drug formulation of claim 3 , wherein the amphetramine is selected from the group consisting of methamphetamine [(2S)-N-methyl-1-phenylpropan-2-amine]) claim 3 , MDA (3 claim 3 ,4- ...

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Номер записи: 45

07-11-2013 дата публикации

Tablet comprising a first and second region

Номер: US20130295174A1

Автор: Christopher E. Szymczak, Gerard P. Mcnally, Harry S. Sowden, Jen-Chi Chen, Kenneth Day, Oliver Anderson, William J. Stuhl

Принадлежит: McNeil PPC Inc

In one aspect, the present invention features a tablet including a first region and a second region, wherein: (i) the first region and the second region each include at least 10%, by volume, of the tablet; (ii) the first region includes a pharmaceutically active agent and the composition of the first region is different from the composition of the second region; (iii) the first region has a density less than about 0.8 g/cc; and (iv) the first region disintegrates in the mouth when placed on the tongue in less than about 30 seconds; wherein the shape of the tablet includes two opposing major faces separated by a side wall, and the interface between the first region and the second region is along at least one major face of the tablet.

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Номер записи: 46

07-11-2013 дата публикации

DIVIDABLE GALENICAL FORM ALLOWING MODIFIED RELEASE OF THE ACTIVE INGREDIENT

Номер: US20130295176A1

Автор: FONKNECHTEN Gilles, GENTY Patrick, Pean Jean-Manuel, Wuthrich Patrick

Принадлежит:

Dividable galenical form for the modified release of active ingredient, wherein the non-subdivided galenical form and a portion of said form obtained by subdivision have identical dissolution profiles. 1. A dividable prolonged-release tablet comprising gliclazide , a cellulose derivative , wherein the cellulose derivative comprises from 50 to 60% of the total weight of the tablet , and a binder , wherein the tablet which has not been subdivided and a half tablet which is obtained by subdividing the tablet have similar dissolution profiles , which dissolution profiles are both largely linear over the time of dissolution.2. The tablet of claim 1 , wherein the cellulose derivative is selected from hydroxymethylcellulose claim 1 , hydroxyethylcellulose claim 1 , hydroxypropylcellulose and hydroxypropyl methylcellulose.3. The tablet of claim 1 , wherein the cellulose derivative is hydroxypropyl methylcellulose of low viscosity.4. The tablet of claim 1 , wherein the binder is maltodextrin claim 1 , polyvidone or a hydroxypropyl methylcellulose of very low viscosity.5. The tablet of claim 1 , wherein the tablet comprises a hydrophilizing agent.6. The tablet of claim 6 , wherein the hydrophilizing agent is colloidal silica.7. The tablet of claim 1 , which comprises maltodextrin and anhydrous colloidal silica.8. The tablet of claim 1 , wherein the gliclazide comprises from 12% to 40% of the total weight of the tablet.9. The tablet of claim 1 , wherein the binder comprises from 2% to 15% of the total weight of the tablet.10. The tablet of claim 1 , which comprises 60 mg gliclazide.11. The tablet of claim 1 , comprising 18.7% gliclazide claim 1 , 22.3% lactose monohydrate claim 1 , 6.9% maltodextrin claim 1 , 50% low-substituted hydroxypropyl methylcellulose claim 1 , 0.5% magnesium stearate and 1.6% anhydrous colloidal silica.12. The tablet of claim 1 , which bears one or more breaking grooves perpendicular to the height and length of the tablet.13. The tablet of claim 1 , ...

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Номер записи: 47

14-11-2013 дата публикации

CONTROLLED RELEASE HYDROCODONE FORMULATIONS

Номер: US20130302418A1

Автор: HUANG Hua-Pin, Masselink John K., OSHLACK Benjamin, Tonelli Alfred P.

Принадлежит:

A solid oral controlled-release dosage form of hydrocodone is disclosed, the dosage form comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and controlled release material. 138-. (canceled)39. A solid oral controlled-release dosage form comprising a matrix comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof and an amount of a controlled release material sufficient to render the dosage form suitable for once-a-day administration , wherein the dosage form is a tablet which providesan in-vitro release rate of hydrocodone or a pharmaceutically acceptable salt thereof, when measured by the USP Basket Method at 100 rpm in 900 ml aqueous buffer at a pH of between 1.6 and 7.2 at 37° C., of from 0% to about 35% at 1 hour, from about 10% to about 70% at 4 hours, from about 20% to about 75% at 8 hours, from about 30% to about 80% at 12 hours, from about 40% to about 90% at 18 hours, and greater than about 60% at 24 hours,{'sub': 24', 'max, 'the dosage form further providing a C/Cratio of about 0.55 to about 1 and a therapeutic effect for at least 24 hours when administered to an individual patient or a patient population at steady-state.'}40. The dosage form of claim 39 , which provides a C/C. ratio of 0.55 to 0.85 after said administration.41. The dosage form of claim 39 , which provides a C/Cratio of 0.55 to 0.75 after said administration.42. The dosage form of claim 39 , which provides a C/C. ratio of 0.6 to 0.7 after said administration.43. The dosage form of claim 39 , which provides a C/Cratio of 0.7 to 0.85 after said administration.44. The dosage form of claim 39 , wherein the controlled release material comprises a material selected from the group consisting of gums claim 39 , cellulose ethers claim 39 , acrylic resins claim 39 , waxes claim 39 , shellac and oils.45. The dosage form of claim 44 , wherein the cellulose ether is an alkylcellulose claim 44 , a ...

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Номер записи: 48

21-11-2013 дата публикации

SUSTAINED RELEASE AMINOPYRIDINE COMPOSITION

Номер: US20130310426A1

Автор: Blight Andrew R., Cohen Ron

Принадлежит: Acorda Therapeutics, Inc.

A pharmaceutical composition which comprises a therapeutically effective amount of a aminopyridine dispersed in a release matrix, including, for example, a composition that can be formulated into a stable, sustained-release oral dosage formulation, such as a tablet which provides, upon administration to a patient, a therapeutically effective plasma level of the aminopyridine for a period of at least 12 hours, preferably 24 hours or more and the use of the composition to treat various neurological diseases. 18-. (canceled)9. A method of treating a disease associated with a neurological disorder , said method comprising:{'sub': max', 'τ', 'avSS, 'administering an aminopyridine on a dosing regimen to obtain an in vivo C:C ratio of 1.0 to 3.5 and a Cof about 15 ng/ml to about 35 ng/ml.'}10. The method of wherein said C:Cratio is about 1.5 to about 3.0.11. The method of wherein said C:C ratio is about 2.0 to about 3.0.12. The method of wherein said neurological disorder comprises a spinal cord injury claim 9 , Alzheimer's disease claim 9 , multiple sclerosis claim 9 , or amyotrophic lateral sclerosis.13. The method of wherein said neurological disorder comprises a spinal cord injury.14. The method of wherein said neurological disorder comprises multiple sclerosis.15. The method of wherein said dosing regimen is comprised of administering a tablet twice daily.16. The method of wherein said twice daily administration comprises every twelve hours.17. The method of wherein said aminopyridine comprises 4-aminopyridine.1823-. (canceled) This application relates to U.S. Provisional Application Ser. No. 60/528,760, filed Dec. 11, 2003, U.S. Provisional Application No. 60/560,894 filed Apr. 9, 2004, U.S. Provisional Application No. 60/528,592 filed Dec. 11, 2003, 60/528,593 filed Dec. 11, 2003, and PCT/US2004/008101 filed on Mar. 17, 2004, all of which are incorporated herein by reference in their entirety.This invention relates to a sustained release oral dosage form of an ...

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Номер записи: 49

21-11-2013 дата публикации

MODIFIED RELEASE FORMULATIONS OF MEMANTINE ORAL DOSAGE FORMS

Номер: US20130310460A1

Автор: ABRAMOWITZ Wattanaporn, Dedhiya Mahendra G., MAHASHABDE Shashank, PERICLOU Antonia, RAO Niranjan, RASTOGI Suneel K.

Принадлежит: FOREST LABORATORIES HOLDINGS LTD.

The present invention provides pharmaceutical compositions given once daily containing at least one therapeutically active ingredient selected from the group consisting of memantine and a pharmaceutically acceptable salt of memantine, and a pharmaceutically acceptable polymeric matrix carrier. The dosage forms of the invention sustain the release of the therapeutically active agent from about 4 to about 24 hours when said dosage form is exposed to aqueous solutions. following entry of said form into a use environment, wherein said dosage form has a dissolution rate of more than about 80% after passage of about 6 hours to about 12 hours following said entry into said use environment. 2. The modified release solid oral dosage form according to claim 1 , wherein said active ingredient is memantine hydrochloride.3. The modified release solid oral dosage form according to claim 1 , wherein the dissolution rate of more than about 80% is achieved after about 12 hours.4. The modified release solid oral dosage form of claim 3 , comprising the active ingredient in an amount within the range of from about 1.0% w/w to about 20% w/w.5. The modified release solid oral dosage form according to claim 1 , wherein the dissolution rate of more than about 80% is achieved after about 6 hours.6. The modified release solid oral dosage form of claim 5 , wherein the active ingredient is present in amounts ranging from about 1.0% w/w to about 35% w/w.7. The modified release solid oral dosage form of claim 1 , wherein the polymeric carrier is a polymeric matrix.8. The modified release solid oral dosage form of claim 7 , wherein the polymeric matrix is a swellable matrix and comprises hydroxypropyl methylcellulose.9. The modified release solid oral dosage form of claim 8 , wherein the dissolution rate of more than about 80% is achieved after about 12 hours claim 8 , and wherein the hydroxypropyl methylcellulose is present in amounts from about 50% w/w to about 80% w/w.10. The modified release ...

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Номер записи: 50

12-12-2013 дата публикации

Oral formulations and lipophilic salts of methylnaltrexone

Номер: US20130330407A1

Автор: Christopher Richard Diorio, Eric C. Ehrnsperger, Jonathan Marc Cohen, Kadum A. Al Shareffi, Syed M. Shah, Xu Meng

Принадлежит: WYETH LLC

The present invention provides compositions comprising methylnaltrexone or a salt thereof, and compositions and formulations thereof, for oral administration.

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Номер записи: 51

19-12-2013 дата публикации

Medical Devices and Implements with Liquid-Impregnated Surfaces

Номер: US20130337027A1

Автор: Adam T. Paxson, Brian R. Solomon, Christopher J. Love, J. David Smith, Kripa K. Varanasi, Rajeev Dhiman

Принадлежит: Massachusetts Institute of Technology

Described herein are medical devices and medical implements with high lubricity to flesh (or biological fluid) and/or inhibited nucleation on its surface. The device has a surface comprising an impregnating liquid and a plurality of micro-scale and/or nano-scale solid features spaced sufficiently close to stably contain the impregnating liquid therebetween. The impregnating liquid fills spaces between said solid features, the surface stably contains the impregnating liquid between the solid features, and the impregnating liquid is substantially held in place between the plurality of solid features regardless of orientation of the surface.

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Номер записи: 52

26-12-2013 дата публикации

Oral Composition

Номер: US20130344148A1

Автор: Lee James Aiping, Wong David, Yang Peter Pingfan

Принадлежит: Magnifica Inc.

The present invention relates to a tablet composition comprising a particle and a pharmaceutically acceptable carrier, wherein the particle comprises an amorphous structure and a submicron domain, and wherein the amorphous structure is a molecular solid dispersion of a drug in a polymeric matrix and the submicron domain is a submicron drug particle. The tablet may further comprise a micronized drug particle. The pharmaceutically acceptable carrier comprises a binder, a filler, a lubricant, and optionally a gelling agent, a glidant and an anti-sticking agent. 1. An oral tablet composition comprising: (1) a drug particle essentially consisting of an amorphous structure and a submicron domain and (2) a carrier , wherein the ratio of the amorphous structure to the submicron domain is 1:50 to 1:4 , and wherein the average diameter of the oral particle is from mesh 20 to mesh 100.2. The oral tablet composition as claimed in claim 1 , wherein the amorphous structure comprises a drug and an amphiphilic polymer claim 1 , wherein the submicron domain essentially consists of a drug.3. The oral tablet composition as claimed in claim 2 , wherein the amphiphilic polymer is polyvinylpyrrolidone.4. The oral tablet composition as claimed in claim 3 , wherein more than 100 parts water is needed to dissolve 1 part drug.5. The oral tablet composition as claimed in claim 3 , wherein more than 1000 parts water is needed to dissolve 1 part drug.6. The oral tablet composition as claimed in claim 3 , wherein more than 10 claim 3 ,000 parts water is needed to dissolve 1 part drug.7. An oral tablet composition comprising: (1) a drug particle essentially consisting of an amorphous structure and a submicron domain and (2) a carrier claim 3 , wherein the ratio of the amorphous structure to the submicron domain is 1:50 to 1:4 claim 3 , wherein the average diameter of the oral particle is from mesh 20 to mesh 100 claim 3 , wherein more than 100 parts water is needed to dissolve 1 part drug; ...

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Номер записи: 53

02-01-2014 дата публикации

Coated tablet formulations and uses thereof

Номер: US20140004184A1

Автор: Arwinder Singh Nagi, Chimanlall Goolcharran, Krishnendu Ghosh, Mainuddin Mahmud, Muhammad Ashraf

Принадлежит: WYETH LLC

The present invention provides coated tablet formulations comprising neratinib maleate, and improved methods for making such coated tablets.

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Номер записи: 54

09-01-2014 дата публикации

Encased Tamper Resistant Controlled Release Dosage Forms

Номер: US20140010875A1

Автор: Huang Haiyong Hugh

Принадлежит: Purdue Pharma L.P.

In certain embodiments, the present invention is directed to a solid controlled release dosage form comprising: a core comprising a first portion of an opioid analgesic dispersed in a first matrix material; and a shell encasing the core and comprising a second portion of the opioid analgesic dispersed in a second matrix material; wherein the amount of opioid analgesic released from the dosage form is proportional within 20% to elapsed time from 8 to 24 hours, as measured by an in-vitro dissolution in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) at 37 C. 1129-. (canceled)130. A method of preparing a solid controlled release dosage form comprising:preparing a core comprising a first portion of an opioid analgesic dispersed in a first matrix material; andencasing the core with a shell comprising a second portion of the opioid analgesic dispersed in a second matrix material;wherein the amount of opioid analgesic released from the dosage form is proportional within 20% to elapsed time from 8 to 24 hours, as measured by an in-vitro dissolution in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) at 37° C.131. A method of preparing a solid controlled release dosage form comprising:preparing a core comprising a first portion of an opioid analgesic dispersed in a first matrix material comprising polyethylene oxide; andencasing the core in a shell comprising a second portion of the opioid analgesic dispersed in a second matrix material comprising polyethylene oxide.132. A method of preparing a solid controlled release dosage form comprising:preparing a compressed core comprising a first portion of an opioid analgesic dispersed in a first matrix material comprising polyethylene oxide; andencasing the core by compression coating a second portion of the opioid analgesic dispersed in a second matrix material comprising polyethylene oxide over the core.133. A method of preparing a solid ...

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Номер записи: 55

09-01-2014 дата публикации

Encased Tamper Resistant Controlled Release Dosage Forms

Номер: US20140011832A1

Автор: Huang Haiyong Hugh

Принадлежит: Purdue Pharma L.P.

In certain embodiments, the present invention is directed to a solid controlled release dosage form comprising: a core comprising a first portion of an opioid analgesic dispersed in a first matrix material; and a shell encasing the core and comprising a second portion of the opioid analgesic dispersed in a second matrix material; wherein the amount of opioid analgesic released from the dosage form is proportional within 20% to elapsed time from 8 to 24 hours, as measured by an in-vitro dissolution in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) at 37 C. 1133-. (canceled)134. A method of preparing a solid controlled release dosage form comprising:combining a therapeutically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and a controlled release excipient;wherein the amount of hydrocodone or salt thereof released from the dosage form is proportional within 20% to elapsed time, at any two time points from 8 to 24 hours, as measured by an in-vitro dissolution in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) at 37° C.; andthe dosage form can be flattened without breaking, wherein the thickness of the dosage form after flattening corresponds to no more than about 20% of the thickness of the dosage form before flattening; andthe amount of hydrocodone or salt thereof released at 0.5 hour from a flattened dosage form deviates no more than about 20% points from a non-flattened dosage form as measured by an in-vitro dissolution in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) at 37° C.135. A method of preparing a solid controlled release dosage form comprising:combining a therapeutically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and a controlled release excipient;wherein the amount of hydrocodone or salt thereof released from the dosage form at 2 hours is less than ...

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Номер записи: 56

16-01-2014 дата публикации

Sustained Release Aminopyridine Composition

Номер: US20140018397A1

Автор: Michael Myers, Seamus Mulligan, Sean Cunningham

Принадлежит: Alkermes Pharma Ireland Ltd

A pharmaceutical composition which comprises a therapeutically effective amount of a aminopyridine dispersed in a release matrix, including, for example, a composition that can be formulated into a stable, sustained-release oral dosage formulation, such as a tablet which provides, upon administration to a patient, a therapeutically effective plasma level of the aminopyridine for a period of at least 12 hours, preferably 24 hours or more and the use of the composition to treat various neurological diseases.

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Номер записи: 57

23-01-2014 дата публикации

NEW ABUSE-RESISTANT PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF OPIOID DEPENDENCE

Номер: US20140023704A1

Автор: Fischer Andreas

Принадлежит: OREXO AB

There is provided pharmaceutical compositions for the treatment of e.g. opioid dependency comprising microparticles of a pharmacologically-effective amount of buprenorphine, or a pharmaceutically-acceptable salt thereof, in associative admixture with particles comprising a weak acid, or particles comprising weakly-acidic buffer forming materials. The composition may further comprise a disintegrant and/or particles of a pharmacologically-effective amount of naloxone, or a pharmaceutically-acceptable salt thereof. The compositions are useful in the treatment of opioid dependency/addiction and/or pain. 123-. (canceled)24. A method of treatment of opioid dependency and/or addiction , which method comprises administration of a tablet composition suitable for sublingual administration comprising:(a) microparticles of a pharmacologically-effective amount of buprenorphine, or a pharmaceutically-acceptable salt thereof in intimate contact with particles comprising citric acid;(b) a pharmacologically-effective amount of naloxone, or a pharmaceutically-acceptable salt thereof; and(c) a disintegrant selected from the group croscarmellose sodium, sodium starch glycolate, crosslinked polyvinylpyrrolidone and mixtures thereof.to a person suffering from, or susceptible to, opioid dependency and/or addiction.25. A method as claimed in claim 24 , wherein the microparticles of buprenorphine or salt thereof have a weight based mean diameter of less than about 15 μm.26. A method as claimed in or wherein the tablet composition comprises an interactive mixture comprising microparticles of buprenorphine or salt thereof presented upon the surfaces of carrier particles.27. A method as claimed in claim 26 , wherein the carrier particles are of a size that is between about 100 and about 800 μm.28. A method as claimed in or claim 26 , wherein the carrier particles are water-soluble.29. A method as claimed in any one of to claim 26 , wherein the carrier particles comprise mannitol.30. A method ...

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Номер записи: 58

30-01-2014 дата публикации

TAMPER RESISTANT DOSAGE FORMS

Номер: US20140031381A1

Автор: "ODonnell Edward P.", Huang Haiyong H., Mannion Richard O., McKenna William H.

Принадлежит: Purdue Pharma L.P.

The present invention relates to pharmaceutical dosage forms, for example to a tamper resistant dosage form including an opioid analgesic, and processes of manufacture, uses, and methods of treatment thereof. 1199-. (canceled)200. A method of treating pain comprising administering , to a patient in need thereof , a solid oral extended release pharmaceutical dosage form comprising an extended release matrix formulation , the extended release matrix formulation comprising a composition comprising at least:(1) at least one polyethylene oxide having, based on rheological measurements, an approximate molecular weight of at least 1,000,000; and(2) at least one active agent comprising an opioid analgesic; andwherein the extended release matrix formulation is cured at a temperature of at least about 60° C. for a time period of at least about 1 minute.201. A method of treating pain comprising administering , to a patient in need thereof , a solid oral extended release pharmaceutical dosage form comprising an extended release matrix formulation , the extended release matrix formulation comprising a composition comprising at least:(1) at least one polyethylene oxide having, based on rheological measurements, an approximate molecular weight of at least 1,000,000; and(2) at least one active agent comprising an opioid analgesic; andwherein the composition comprises at least about 80% (by wt) polyethylene oxide having, based on rheological measurements, an approximate molecular weight of at least 1,000,000 and the extended release matrix formulation is cured at a temperature of at least about 60° C. for a time period of at least about 1 minute.202. A method of treating pain comprising administering , to a patient in need thereof , a solid oral extended release pharmaceutical dosage form comprising an extended release matrix formulation , the extended release matrix formulation comprising a composition comprising at least an extended release matrix formulation which is cured at a ...

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Номер записи: 59

20-02-2014 дата публикации

PHARMACEUTICAL COMPOSITIONS OF MEMANTINE

Номер: US20140050784A1

Автор: DEROSA Gregg R., HARONSKY Elina, Kagan Elena, SHAHAR Nitzan

Принадлежит:

The present invention relates to oral dosage forms comprising Memantine or a pharmaceutically acceptable salt thereof, pharmaceutical formulations comprising the oral dosage forms, and methods for treating mild, moderate or severe Alzheimer's dementia, or neuropathic pain comprising the oral dosage forms and formulations. 1. A modified release solid oral dosage form comprising a therapeutically effective amount of memantine or a pharmaceutically acceptable salt thereof , and at least one pharmaceutically acceptable rate controlling excipient , wherein the solid oral dosage form is adapted for administering with an interval between doses of 5 days or above 5 days to a patient in a need thereof , and wherein the solid oral dosage form:{'sub': max', 'min', 'tau, '(c) provides an in vivo plasma profile at steady state comprising a Cof about 160 ng/ml or less, a Cof more than about 30 ng/ml, and an AUCof more than about 14,000 ng h/ml, and/or'}(d) has a dissolution profile of: not more than 45% at 24 hours, not more than 70% at 48 hours, and not more than 80% at 55 hours.2. A modified release solid oral dosage form according to adapted for administering once weekly to a patient in need thereof.3. The modified release solid oral dosage form according to or claim 1 , wherein the dosage form comprises memantine or a pharmaceutically acceptable salt thereof in an amount of at least about 112 mg claim 1 , at least about 140 mg claim 1 , at least about 160 mg claim 1 , at least about 170 mg claim 1 , or at least about 190 mg.4. The modified release solid oral dosage form according to or claim 1 , wherein the dosage form comprises memantine or a pharmaceutically acceptable salt thereof in an amount of about 140 to about 190 mg claim 1 , about 160 to about 190 mg claim 1 , about 170 mg to about 190 mg claim 1 , or about 140 to about 200 mg claim 1 , about 160 to about 200 mg claim 1 , about 170 to about 200 mg or about 190 to about 200 mg.5. A modified release solid oral dosage ...

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Номер записи: 60

20-02-2014 дата публикации

PHARMACEUTICAL COMPOSITIONS RESISTANT TO ABUSE

Номер: US20140050787A1

Автор: Haahr Anne-Mette, Hoeilund-Jensen Jocob Aas, Hoeyrup Hemmingsen Pernille Kristine, Lindhardt Karsten, Lyhne-Iversen Louise Inoka, Oevergaard Jan Martin, Olsen Martin Rex, Tygesen Peter Holm

Принадлежит: EGALET LTD.

The present invention provides immediate release pharmaceutical compositions for oral administration that are resistant to abuse. 144.-. (canceled)45. An abuse resistant pharmaceutical composition , the pharmaceutical composition comprising a shell resistant to physical tampering and a matrix composition ,wherein the matrix composition is at least partly contained within the shell and comprises an active drug substance,wherein the shell comprises an outer shell wall having an inner surface and an outer surface, the outer surface being a double curved surface,wherein the shell extends from a first end to a second end, the shell having a length in a range of from 4 mm to 20 mm,{'sup': 2', '2, 'wherein the outer shell wall has a first opening at the first end and a second opening at the second end, the first opening and the second opening having an area in a range of from about 1 mmto about 100 mm, and'}wherein the outer shell wall is of varying thickness and has a maximum thickness in a range of from 1.0 mm to about 10 mm, the outer shell wall being impermeable to water.46. The pharmaceutical composition according to claim 45 , wherein the shell comprises one or more reinforcement elements extending from the inner surface of the outer shell wall.47. The pharmaceutical composition according to claim 46 , wherein the one or more reinforcement elements comprises a first reinforcement wall.48. The pharmaceutical composition according to claim 47 , wherein the first reinforcement wall is a plane wall.49. The pharmaceutical composition according to claim 47 , wherein the first reinforcement wall is perpendicular to a first axis from the first end to the second end.50. The pharmaceutical composition according to claim 47 , wherein the first reinforcement wall is parallel to a first axis extending from the first end to the second end.51. The pharmaceutical composition according to claim 47 , wherein the first reinforcement wall has a thickness in a range of from 0.2 mm to 2 ...

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Номер записи: 61

27-02-2014 дата публикации

Modified Release Formulations Containing Drug-Ion Exchange Resin Complexes

Номер: US20140056984A1

Автор: Ketan Mehta, Yu-Hsing Tu

Принадлежит: Tris Pharma Inc

An aqueous liquid suspension containing a coated drug-ion exchange resin complex comprising a core composed of an amphetamine complexed with a pharmaceutically acceptable ion-exchange resin and an uncoated amphetamine-ion exchange resin complex is provided. The coated amphetamine-ion exchange resin complex is in admixture with a polymer to form a matrix. Methods of making the coated complex and the liquid suspension are described.

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Номер записи: 62

06-03-2014 дата публикации

Modified release compositions comprising tacrolimus

Номер: US20140065225A1

Автор: Per Holm, Tomas Norling

Принадлежит: Veloxis Pharmaceuticals AS

A modified release composition comprising tacrolimus releases less than 20% w/w of the active ingredient within 0.5 hours when subjected to an in vitro dissolution test using USP Paddle method and using 0.1 N HCl as dissolution medium and has increased bioavailability by effectively reducing or even avoiding the effects of CYP3A4 metabolism. The modified composition may be coated with an enteric coating; and/or may comprise a solid dispersion or a solid solution of tacrolimus in a hydrophilic or water-miscible vehicle and one or more modifying release agents; and/or may comprise a solid dispersion or a solid solution of tacrolimus in an amphiphilic or hydrophobic vehicle and optionally one or more modifying release agents.

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Номер записи: 63

06-03-2014 дата публикации

Novel Method

Номер: US20140066516A1

Автор: Geoffrey Douglas Clarke, Ian Burnett, Timothy James Grattan

Принадлежит: GlaxoSmithKline LLC

The present invention is directed to a novel method for reducing intrapatient variability in pharmaceutically active agent which is suitably not absorbed in the stomach, such as paracetamol, containing formulations in patients having gastric dysmotility, or a method of improving analgesia in a diabetic patient, or improving absorption of an active agent is a patient with gastric dysmotility, which methods comprises administering orally to said patient in need thereof a pharmaceutical dosage form comprising a first active agent, calcium carbonate, at least one first binding agent, and at least one disintegrating agent as intragranular components in the form of a granulate, and as an extragranular component at least one hydrophilic colloid, an optionally a second binding agent, calcium carbonate, a super disintegrant, and a second active agent.

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Номер записи: 64

20-03-2014 дата публикации

Compressed Chewing Gum Tablet

Номер: US20140079756A1

Автор: Andersen Carsten, Arent Nicolai, Lorenzen Gitte, Thorengaard Bitten, Wittorff Helle

Принадлежит:

A compressed chewing gum tablet includes at least a first and a second chewing gum module, the first chewing gum module including a first chewing gum composition including at least a first active ingredient and chewing gum granules containing gum base, the second chewing gum module including a second chewing gum composition including at least a second active ingredient and chewing gum granules containing gum base, wherein the first active ingredient is a pharmaceutically active ingredient, and the second active ingredient is selected from the group consisting of pharmaceutically active ingredients and enhancers, wherein the gum base content of the first and second chewing gum modules is different. 1. A compressed chewing gum tablet comprising at least a first and a second chewing gum module ,said first chewing gum module comprising a first chewing gum composition comprising at least a first active ingredient and chewing gum granules containing gum base,said second chewing gum module comprising a second chewing gum composition comprising at least a second active ingredient and chewing gum granules containing gum base,wherein the first chewing gum composition is different in composition than the second chewing gum composition,wherein said first active ingredient is nicotine and said second active ingredient is an enhancer; andwherein at least part of the enhancer is contained within the second chewing gum module outside the chewing gum granules of the second chewing gum module, and wherein nicotine is contained within said chewing gum granules of the first chewing gum module.2. The compressed chewing gum tablet of wherein substantially all of the nicotine is contained within said chewing gum granules of the first chewing gum module.3. The compressed chewing gum tablet of wherein substantially all of the enhancer is contained within the second chewing gum module outside the chewing gum granules of the second chewing gum module.4. The compressed chewing gum tablet of ...

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Номер записи: 65

20-03-2014 дата публикации

Modified Release Tranexamic Acid Formulation

Номер: US20140079779A1

Автор: Fersharaki Shahin, Joshi Mayank R.

Принадлежит: Watson Laboratories, Inc. - Florida

A modified release dosage form for the oral administration of tranexamic acid. 124-. (canceled)25. A modified release dosage form comprising: (i) tranexamic acid;', '(ii) a release controlling material;', '(iii) a binder;', '(iv) a filler;', '(v) a glidant;', '(vi) a disintegrant; and', '(vii) optionally, one or more lubricants; and, '(A) a compressed matrix core which comprises (i) a coating agent which is insoluble in water but soluble in aqueous media with a pH below 4;', '(ii) a film former;', '(iii) a plasticizer; and', '(iv) an anti-sticking agent, '(B) a functional coating on said compressed matrix core which comprises'}wherein the dosage form, exhibits the following dissolution profile when tested in a USP Type 2 (paddle) apparatus at 50 RPM in 900 ml of 0.1 N HCl at 37° C.: after 15 minutes 10-50% of the tranexamic acid is released; after 30 minutes 40-95% of the tranexamic acid is released; after 45 minutes 50-99% of the tranexamic acid is released; and after 60 minutes, not less than 70% of the tranexamic acid is released.26. The modified release dosage form as defined in where the filler is selected from the group consisting of sugars claim 25 , lactose monohydrate claim 25 , calcium phosphate claim 25 , dextrin claim 25 , dextrose claim 25 , maltitol claim 25 , maltose claim 25 , starch claim 25 , sucrose claim 25 , or microcrystalline cellulose.27. The modified release dosage form as defined in wherein said filler comprises lactose monohydrate and microcrystalline cellulose.28. The modified release dosage form as defined in wherein the binder in the core is water soluble.29. The modified release dosage form as defined in where the binder in the core is selected from the group consisting of methyl cellulose claim 25 , hydroxymethyl cellulose claim 25 , polyvinyl pyrrolidone claim 25 , hydroxyethyl cellulose claim 25 , hydroxypropyl cellulose claim 25 , hydroxypropyl methylcellulose claim 25 , polyethylene oxides claim 25 , gums claim 25 , acrylate ...

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Номер записи: 66

20-03-2014 дата публикации

Methods for prophylatic appetite suppression

Номер: US20140080857A1

Автор: Anthony A. McKinney, Gary Tollefson, Rick Soltero, Ronald S. Vladyka, Simon Kwok-Pan Yau

Принадлежит: Orexigen Therapeutics Inc

Pharmaceutical formulations comprise sustained-release zonisamide. Methods of preparing such pharmaceutical formulations involve intermixing zonisamide with a suitable excipient configured to control the dissolution profile of the zonisamide. Methods of treatment involve administering the pharmaceutical formulations to patients in need of such treatment.

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Номер записи: 67

07-01-2021 дата публикации

TAMPER RESISTANT DOSAGE FORMS

Номер: US20210000747A1

Автор: "ODonnell Edward P.", Huang Haiyong H., Mannion Richard O., McKenna William H.

Принадлежит:

The present invention relates to pharmaceutical dosage forms, for example to a tamper resistant dosage form including an opioid analgesic, and processes of manufacture, uses, and methods of treatment thereof. 1169-. (canceled)170. A process of preparing a solid oral extended release pharmaceutical dosage form , comprising the steps of:(a) combining (1) at least one polyethylene oxide (PEO) having, based on rheological measurements, an approximate molecular weight of at least 800,000, and (2) at least one opioid analgesic, to form a composition;(b) shaping the composition to form an extended release matrix formulation;(c) subsequently heating said extended release matrix formulation by subjecting the extended release matrix formulation to an elevated temperature that is at least the softening temperature of said PEO for a time period of at least about 1 minute; and(d) cooling the heated extended release matrix formulation.171. The process of claim 170 , wherein said time period is at least about 15 minutes.172. The process of claim 170 , wherein said elevated temperature is at least about 55° C.173. The process of claim 170 , wherein said elevated temperature is at least about 62° C.174. The process of claim 170 , wherein the total PEO content of the shaped composition is at least about 15% (by weight) of the shaped composition.175. The process of claim 170 , wherein the total PEO content of the shaped composition is at least about 30% (by weight) of the shaped composition.176. The process of claim 170 , wherein the total PEO content of the shaped composition is at least about 50% (by weight) of the shaped composition.177. The process of claim 170 , wherein the extended release matrix is shaped by direct compression to form a tablet.178. The process of claim 170 , wherein said cooling is at a temperature below 50° C.179. The process of claim 170 , wherein the extended release matrix is shaped to form a tablet; the heating step takes place in a coating pan; said time ...

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Номер записи: 68

07-01-2021 дата публикации

TAMPER RESISTANT DOSAGE FORMS

Номер: US20210000748A1

Автор: "ODonnell Edward P.", Huang Haiyong H., Mannion Richard O., McKenna William H.

Принадлежит:

The present invention relates to pharmaceutical dosage forms, for example to a tamper resistant dosage form including an opioid analgesic, and processes of manufacture, uses, and methods of treatment thereof. 1169-. (canceled)170. A solid oral extended release pharmaceutical dosage form , comprising a shaped , heated , and cooled extended release matrix , said matrix comprising at least one polyethylene oxide (PEO) having , based on rheological measurements , an approximate molecular weight of at least 800 ,000 , and at least one opioid analgesic , wherein the shaped matrix is heated to an elevated temperature that is at least the softening temperature of said PEO for a time period of at least about 1 minute and thereafter cooled.171. The dosage form of claim 170 , wherein said time period is at least about 15 minutes.172. The dosage form of claim 170 , wherein said elevated temperature is at least about 55° C.173. The dosage form of claim 170 , wherein said elevated temperature is at least about 62° C.174. The dosage form of claim 170 , wherein the total PEO content of the shaped matrix is at least about 15% (by weight) of said matrix.175. The dosage form of claim 170 , wherein the total PEO content of the shaped matrix is at least about 30% (by weight) of said matrix.176. The dosage form of claim 170 , wherein the total PEO content of the shaped matrix is at least about 50% (by weight) of said matrix.177. The dosage form of claim 170 , wherein the extended release matrix is shaped by direct compression to form a tablet.178. The dosage form of claim 170 , wherein said cooling is at a temperature of below 50° C.179. The dosage form of claim 170 , wherein the extended release matrix is shaped to form a tablet and heated in a coating pan; said time period is at least about 5 minutes; and said elevated temperature is at least about 60° C.180. The dosage form of claim 179 , wherein the opioid analgesic is oxycodone or a pharmaceutically acceptable salt thereof.181. The ...

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Номер записи: 69

07-01-2021 дата публикации

TAMPER RESISTANT DOSAGE FORMS

Номер: US20210000749A1

Автор: "ODonnell Edward P.", Huang Haiyong H., Mannion Richard O., McKenna William H.

Принадлежит:

The present invention relates to pharmaceutical dosage forms, for example to a tamper resistant dosage form including an opioid analgesic, and processes of manufacture, uses, and methods of treatment thereof. 1169-. (canceled)170. A method of treating pain comprising administering to a patient in need thereof a solid oral extended release pharmaceutical dosage form , comprising a shaped , heated , and cooled extended release matrix , said matrix comprising at least one polyethylene oxide (PEO) having , based on rheological measurements , an approximate molecular weight of at least 800 ,000 , and at least one opioid analgesic , wherein the shaped matrix is heated to an elevated temperature which is at least the softening temperature of said PEO for a time period of at least about 1 minute and thereafter cooled.171. The method of claim 170 , wherein said time period is at least about 15 minutes.172. The method of claim 170 , wherein said elevated temperature is at least about 55° C.173. The method of claim 170 , wherein said elevated temperature is at least about 62° C.174. The method of claim 170 , wherein the total PEO content of the shaped matrix is at least about 15% (by weight) of said matrix.175. The method of claim 170 , wherein the total PEO content of the shaped matrix is at least about 30% (by weight) of said matrix.176. The method of claim 170 , wherein the total PEO content of the shaped matrix is at least about 50% (by weight) of said matrix.177. The method of claim 170 , wherein the extended release matrix is shaped by direct compression to form a tablet.178. The method of claim 170 , wherein said cooling is at a temperature below 50° C.179. The method of claim 170 , wherein the extended release matrix is shaped to form a tablet and heated in a coating pan; said time period is at least about 5 minutes; and said elevated temperature is at least about 60° C.180. The method of claim 179 , wherein the opioid analgesic is oxycodone or a pharmaceutically ...

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Номер записи: 70

03-01-2019 дата публикации

ANIMAL FEED BOLUS AND METHODS FOR MANUFACTURING THE SAME

Номер: US20190000758A1

Автор: BEGUIN Jean Marie, DAGORNE Rene-Pol

Принадлежит: CAN TECHNOLOGIES, INC.

The present invention relates to an animal feed bolus having two or more sections, wherein each section has a different composition. The different sections of the bolus are formulated to have different release times and/or to provide compositions with different nutritional purposes. Also described herein are methods for manufacturing such boluses, and methods for feeding an animal using such boluses. 1. An animal feed bolus , comprising:a first section, anda second section connected to the first section,wherein the first section has a different composition and release rate than the second section.2. (canceled)3. The bolus of claim 1 , wherein the release rate of the first section is less than one day.4. The bolus of claim 1 , wherein the release rate of the first section is less than 12 hours.5. The bolus of claim 1 , wherein the release rate of the first section is less than 6 hours.6. The bolus of claim 1 , wherein the release rate of the first section is less than 1 hour.7. The bolus of claim 2 , wherein the release rate of the second section is greater than 2 days.8. The bolus of claim 2 , wherein the release rate of the second section is greater than 1 week.9. The bolus of claim 2 , wherein the release rate of the second section is greater than 15 days.10. (canceled)11. The bolus of claim 1 , wherein the first section comprises about 50 wt % of the bolus.12. The bolus of claim 1 , wherein the first section comprises about 40 wt % of the bolus.13. The bolus of claim 1 , wherein the first section comprises less than about 30 wt % of the bolus.14. The bolus of claim 1 , wherein the first section comprises less than about 20 wt % of the bolus.15. The bolus of claim 1 , wherein the first section comprises less than about 10 wt % of the bolus.16. The bolus of claim 1 , wherein the first section comprises vitamin E.17. (canceled)18. The bolus of claim 1 , wherein the second section comprises a nutrient selected from the group consisting of zinc claim 1 , selenium ...

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Номер записи: 71

03-01-2019 дата публикации

TAMPER RESISTANT DOSAGE FORMS

Номер: US20190000767A1

Автор: "ODonnell Edward P.", Huang Haiyong H., Mannion Richard O., McKenna William H.

Принадлежит:

The present invention relates to pharmaceutical dosage forms, for example to a tamper resistant dosage form including an opioid analgesic, and processes of manufacture, uses, and methods of treatment thereof. 1. A process of preparing a solid oral extended release pharmaceutical dosage form , [ (1) at least one polyethylene oxide having, based on rheological measurements, an approximate molecular weight of at least 1,000,000, and', '(2) at least one active agent,', 'to form a composition;, '(a) combining at least'}, '(b) shaping the composition to form an extended release matrix formulation; and', '(c) curing said extended release matrix formulation comprising at least a curing step of subjecting the extended release matrix formulation to a temperature which is at least the softening temperature of said polyethylene oxide for a time period of at least about 1 minute., 'comprising at least the steps of2. The process of claim 1 , wherein in step c) the extended release matrix formulation is subjected to a temperature which is at least the softening temperature of said polyethylene oxide for a time period of at least about 5 minutes.3. The process of claim 1 , wherein in step c) the extended release matrix formulation is subjected to a temperature which is at least the softening temperature of said polyethylene oxide for a time period of at least about 15 minutes.4. The process of claim 1 , or claim 1 , wherein in step b) the composition is shaped to form an extended release matrix formulation in the form of tablet.5. The process of claim 4 , wherein in step b) the composition is shaped by direct compression of said composition.6. The process of any one of to claim 4 , wherein in step c) the extended release matrix formulation is subjected to a temperature of at least about 60° C. or at least about 62° C. preferably at least about 68° C. claim 4 , at least about 70° C. claim 4 , at least about 72° C. or at least about 75° C.7. The process of claim 6 , wherein the ...

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Номер записи: 72

04-01-2018 дата публикации

Novel pharmaceutical composition

Номер: US20180000741A1

Автор: Hee Chul Chang, Ji Hoon Jung, Sanghee Kim

Принадлежит: BIO-SYNECTICS Inc, Daewoong Pharmaceutical Co Ltd

Disclosed herein a pharmaceutical composition comprising aprepitant a pharmaceutically acceptable salt thereof; at least one hydrocarbon derivative selected from among a fatty acid of 14 to 18 carbon atoms, and a fatty alcohol of 14 to 18 carbon atoms; and at least one selected from among polyoxyethyelene-type nonionic surfactant, sucrose fatty acid ester, and Macrogol 15 hydroxystearate. The pharmaceutical composition of the present disclosure can release aprepitant or a pharmaceutically acceptable salt thereof to effectively exert the pharmaceutical efficacy, and can be dissolved in a fasted state simulated gastrointestinal fluid so that it can be useful for study on the in vivo pharmacokinetic behavior of aprepitant.

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Номер записи: 73

04-01-2018 дата публикации

MODIFIED RELEASE COMPOSITIONS OF EPALRESTAT OR A DERIVATIVE THEREOF AND METHODS FOR USING THE SAME

Номер: US20180000792A1

Автор: CARON Judy, Kalofonos Isabel, Martin-Doyle William

Принадлежит: Bionevia Pharmaceuticals Inc.

Modified release pharmaceutical compositions of epalrestat are provided. Methods of manufacturing the tablets and treating various diseases and conditions, including diabetes and diabetic complications, by administering the modified release compositions to patients in need thereof are also provided. 132.-. (canceled)33. A modified release pharmaceutical composition , comprising epalrestat or a pharmaceutically acceptable derivative thereof; and one or more water-swellable polymers; wherein the sustained release pharmaceutical composition is administered to a patient once or twice a day to provide a continuous therapeutic effect throughout the day.34. The modified release pharmaceutical composition of claim 33 , which(i) when administered to a patient on a regular dosing schedule, provides a relatively flat plasma concentration profile of epalrestat at steady state, wherein there are no substantial peaks or troughs in the relatively flat plasma concentration profile, and the minimum plasma concentration of epalrestat in the relatively flat plasma concentration profile is sufficient to provide a therapeutic effect to the patient; or(ii) when administered to a patient on a regular dosing schedule, provides a relatively flat plasma concentration profile of epalrestat at steady state such that a mean Cmin/Cmax epalrestat ratio during dosing interval is about 0.55 to about 1.0, and the Cmin is sufficient to provide a therapeutic effect; or(iii) provides to a patient a therapeutic effect for about 12 to about 24 hours and a relatively flat plasma concentration profile of epalrestat at steady state such that the minimum plasma concentration of epalrestat during the dosing interval is about 55% of the maximum plasma concentration during the dosing interval.35. The modified release pharmaceutical composition of claim 33 , wherein the water-swellable polymer is a cellulose ether polymer.36. The modified release pharmaceutical composition of claim 35 , wherein the cellulose ...

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Номер записи: 74

02-01-2020 дата публикации

PARENTERAL SUSTAINED-RELEASE DELIVERY OF CARVEDILOL DISPERSE SYSTEMS

Номер: US20200000706A1

Автор: GUO Dongwei, Huang Jingjun, IVANOVA Vera, MAEDA Kaoru, Wang Wan

Принадлежит: ASCENDIA PHARMACEUTICALS, LLC

Carvedilol parenteral sustained release systems by IV infusion, injection, or subcutaneous routes are disclosed. Preparation of carvedilol disperse systems such as liposomes, biodegradable microparticles or nanoparticles, and polymeric microparticles or nanoparticles have been presented in the present invention. Compositions containing carvedilol encapsulated in liposomes showed higher bioavailability and lower clearance rate than that of the free solution after intravenous administration. In vitro release of those liposomes in buffer solutions shows drug extended release over 48 hours, and correspondingly the in vivo animal data shows that parenteral administration of carvedilol encapsulated in liposomal materials has sustained release PK profile. 1. A parenteral drug delivery composition for sustained release , comprising a non-selective β-adrenergic receptor blocker , an α-adrenergic receptor blocker , or an α-β adrenergic receptor blocker , wherein the adrenergic receptor blocker is encapsulated inside microparticles or nanoparticles.2. The composition of claim 1 , wherein the non-selective β- claim 1 , α- claim 1 , or α-β adrenergic receptor blocker is carvedilol or its metabolites.3. The composition of claim 1 , wherein the composition is a liposome formulation.4. The composition of claim 1 , wherein the microparticles or nanoparticles are biodegradable.5. The composition of claim 1 , wherein the microparticles or nanoparticles are polymeric.6. The composition of claim 3 , wherein (i) the liposome formulation contains 0.001 to 10% percent (m/m) carvedilol or a pharmacologically acceptable salt thereof claim 3 , (ii) the liposome formulation is in a size range of 0.02 microns to 0.9 microns in diameter claim 3 , and (iii) the liposome formulation provides a longer residence time of the carvedilol in vivo claim 3 , as compared to a free-carvedilol solution administered parenterally.7. The composition of claim 6 , wherein the liposome formulation before dosing ...

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Номер записи: 75

02-01-2020 дата публикации

MULTICOMPONENT GUMMY COMPOSITIONS WITH HARD CORE

Номер: US20200000716A1

Автор: Bagley Lindsey, Godfrey Graham, Huatan Hiep, JONES Huw, Kanji Nazim, Muniz Luis C., Oryniak Caryn, Romanoschi Ovidiu

Принадлежит: CHURCH & DWIGHT CO., INC.

The present disclosure provides oral, chewable dosage forms that are suitable for delivery of one or more active ingredients to a consumer, particularly a human individual. The dosage forms can be configured as multicomponent compositions formed of: a first component including a gummy composition; a second component that is a particulate material or is a pre-formed solid unit or plurality of pre-formed solid units; and an active ingredient. The second component can be, for example, in the form of a pharmaceutically acceptable oral dosage unit, such as a tablet, a caplet, a soft shell capsule, a hard shell capsule, a microcapsule, or a pastille. 1. A chewable , multicomponent composition for oral administration , the multicomponent composition comprising:a first component that is a hydrocolloid system comprising about 70% to about 94% w/w of one or more hydrophilic bulking agents, about 1% to about 20% w/w of one or more hydrophilic, long chain polymers, and about 5% to about 35% w/w of a water source, the first component being in the form of a gel;a second component that is in the form of a particulate material or is a pre-formed solid unit or plurality of pre-formed solid units; andan active ingredient;wherein the first component substantially surrounds the second component.2. (canceled)3. The multicomponent composition of claim 1 , further comprising a third component configured as a layer between the first component and the second component.4. The multicomponent composition of claim 3 , wherein the third component is configured as a barrier layer that substantially prevents passage of water between the first component and the second component.5. The multicomponent composition of claim 1 , wherein one or more of the following conditions is met:the active ingredient is included in the second component;the active ingredient is included in the first component;the active ingredient is in an encapsulated form;the gummy composition is elastic or viscoelastic;the ...

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Номер записи: 76

02-01-2020 дата публикации

ERYTHRITOL GRANULES AND METHOD FOR PRODUCING SAME, METHOD FOR PRODUCING TABLETS USING SAME, AND TABLETS

Номер: US20200000729A1

Автор: KIMURA Yuki, MINODA Kanako, TOCHIO Takumi, YAMAMOTO Hiromitsu

Принадлежит:

[Problem] 1. Erythritol granules comprising hydroxypropyl cellulose or hydroxypropyl methylcellulose , the granules having a property that when a sample obtained by adding 1.6 mg of magnesium stearate to 160 mg of the erythritol granules is filled in a mortar having a diameter of 8 mm and compressed at a compression rate of 10 mm/min and a pressure of 0 to 100 MPa , an average yield pressure in the range of 30 to 100 MPa is less than 2941 MPa.2. Erythritol granules comprising more than 1.48% by mass and less than 15.25% by mass of hydroxypropyl cellulose or more than 1.48% by mass and less than 10.71% by mass of hydroxypropyl methylcellulose.3. The erythritol granules according to claim 1 , for producing tablets by a dry direct tableting method.4. The erythritol granules according to claim 1 , having a property that when tablets each having a diameter of 8 mm and weighing 200 mg per tablet are formed by adding 1 part by weight of magnesium stearate to 100 parts by weight of the erythritol granules and then tableting the mixture by a dry direct tableting method at a tableting pressure of 5.0 to 6.0 kN claim 1 , a hardness of each of the tablets is not less than 3.5 kgf.5. A method for producing erythritol granules claim 1 , comprising a granulation step of spraying a spray liquid comprising hydroxypropyl cellulose and/or hydroxypropyl methylcellulose to erythritol powder while fluidizing or stirring the erythritol powder claim 1 , and then drying.6. The method for producing erythritol granules according to claim 5 , wherein the granulation step is carried out by a fluidized bed granulation method.7. The method for producing erythritol granules according to claim 5 , wherein in the spray liquid claim 5 , a concentration of the hydroxypropyl cellulose is more than 2.5% by mass and less than 30% by mass claim 5 , or a concentration of the hydroxypropyl methylcellulose is more than 2.5% by mass and less than 20% by mass.8. The method for producing erythritol granules ...

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Номер записи: 77

07-01-2021 дата публикации

Pharmaceutical Composition and Preparation Method Therefor and Uses Thereof

Номер: US20210000828A1

Автор: Jiaquan WU

Принадлежит: Wuxi Shuangliang Biotechnology Co Ltd

The present disclosure belongs to the field of pharmaceutical preparations, and discloses a pharmaceutical composition and a preparation method therefor and uses thereof. The pharmaceutical composition comprising EGFR inhibitor (C-005) and the pharmaceutical tablets prepared therefrom of the present disclosure are suitable for the treatment of cancer, preferably lung cancer, particularly non-small cell lung cancer.

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Номер записи: 78

03-01-2019 дата публикации

Solid dosage forms of (s)-ethyl 2-amino-3-(4-(2-amino-6-((r)-1-(4-chloro-2-(3-methyl-1h-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate

Номер: US20190000843A1

Автор: Jinling Chen, Kalyan Nuguru, Matthew S. DEAVER, Richard J. Holl

Принадлежит: LEXICON PHARMACEUTICALS, INC.

Solid pharmaceutical dosage forms comprising (S)-ethyl 2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate (telotristat) are disclosed, as well as methods of making them and compositions useful in their manufacture.

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Номер записи: 79

04-01-2018 дата публикации

MODIFIED RELEASE FORMULATIONS CONTAINING DRUG-ION EXCHANGE RESIN COMPLEXES

Номер: US20180000954A1

Автор: Mehta Ketan, Tu Yu-Hsing

Принадлежит:

A particulate, modified release barrier coated drug-cation exchange resin complex comprising a core composed of a drug complexed with a pharmaceutically acceptable ion-exchange resin is provided. Methods of making and products containing this coated complex are described. 1. An orally ingestible aqueous liquid suspension comprising: (i) a particulate drug-cation exchange resin complex comprising at least one drug bound to a pharmaceutically acceptable water insoluble cation exchange resin, and further comprising a water insoluble polymer or copolymer, or hydrophilic polymer which forms a matrix with the drug-cation exchange resin complex, which particulate drug-cation exchange resin complex-(water insoluble polymer or copolymer or a hydrophilic polymer) matrix is capable of passing through a number 40 mesh screen, and', '(ii) about 25% w/w to about 50% w/w of a water permeable, water insoluble, non-ionic, modified release polymeric diffusion barrier coating which provides a modified release profile to the drug in said drug-cation exchange resin complex-(water insoluble polymer or copolymer or hydrophilic polymer) matrix, wherein said at least one drug is methylphenidate, said barrier coating having an elongation factor of about 125% to about 400% and comprising a water insoluble polymer and about 2.5% w/w to about 20% w/w plasticizer based on the weight of the barrier coating; and, '(A) barrier coated particulates which provide a modified release profile which comprise (iiia) an uncoated particulate methylphenidate-cation exchange resin complex of a size capable of passing through a number 40 mesh screen, wherein said uncoated methylphenidate-cation exchange resin complex is methylphenidate bound to a pharmaceutically acceptable water insoluble cation exchange resin and/or', '(iiib) methylphenidate or a pharmaceutically acceptable salt thereof which is not complexed with an ion exchange resin; and, '(B) at least one of (iiia) and/or (iiib)(C) a pharmaceutically ...

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Номер записи: 80

02-01-2020 дата публикации

Crystalline Form of Ribociclib Succinate

Номер: US20200002343A1

Автор: Bahareh Khalili, Fabio E. S. Souza

Принадлежит: Apotex Inc

The present invention provides a novel crystalline form of Ribociclib succinate, Ribociclib succinate Form APO-I, including Ribociclib succinate, benzyl alcohol and water, compositions thereof, processes for the preparation thereof, and the use of this crystalline form in the treatment of conditions associated with increased CDK4/6 kinase activity, and in particular, cancers, including certain forms of breast cancer.

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Номер записи: 81

07-01-2021 дата публикации

INKJET INK AND TABLET

Номер: US20210002503A1

Автор: HOSHINO Yuichi, Saito Masatoshi

Принадлежит: TOPPAN PRINTING CO.,LTD.

An inkjet ink in which a food color containing at least sodium copper chlorophyllin and a pigment other than sodium copper chlorophyllin is dispersed in a dispersion medium containing propylene glycol, and which prevents the occurrence of precipitation of the pigment components or other components even when the inkjet ink is stored for a long period of time, and there is also provided a tablet having a print pattern printed by the inkjet ink. The inkjet ink of the present embodiment, which is edible, comprises a food color containing at least sodium copper chlorophyllin and a pigment other than sodium copper chlorophyllin, and a dispersion medium containing propylene glycol, and has a propylene glycol content in the range of 0.001 mass % or more and 19 mass % or less relative to the total mass of the inkjet ink. 1. An inkjet ink that is edible , comprising:a food color containing at least sodium copper chlorophyllin and a pigment other than the sodium copper chlorophyllin; and,a dispersion medium containing propylene glycol,wherein a content of the propylene glycol is in a range of 0.001 mass % or more and 19 mass % or less relative to a total mass of the inkjet ink.2. The inkjet ink of claim 1 , wherein a content of the propylene glycol is in a range of 0.01 mass % or more and 2.5 mass % or less relative to a total mass of the inkjet ink.3. The inkjet ink of claim 1 , wherein a content of the food color is in a range of 1 mass % or more and 10 mass % or less relative to a total mass of the inkjet ink.4. The inkjet ink of claim 1 , wherein the inkjet ink comprises at least one of New Coccine claim 1 , erythrosine and Brilliant Blue FCF claim 1 , as a pigment other than the sodium copper chlorophyllin.5. The inkjet ink of claim 1 , wherein a content of a pigment other than the sodium copper chlorophyllin in the food color is in a range of 0.1 parts by mass or more and 1.5 parts by mass or less relative to 1 part by mass of the sodium copper chlorophyllin.6. The ...

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Номер записи: 82

01-01-2015 дата публикации

Regimen for suppressing organ rejection

Номер: US20150004154A1

Автор: William J. Polvino

Принадлежит: Veloxis Pharmaceuticals AS

The present invention relates to a method of suppressing organ rejection in a patient receiving an organ transplant by initiating oral treatment with a once-daily extended release tacrolimus dosage form, for example, at an initial dose of from about 0.15 to about 0.20 mg/kg/day within 24 or 48 hours following transplantation. The once-daily extended release tacrolimus dosage form (i) provides low fluctuation and/or swing of tacrolimus, (ii) provides a significantly lower C max than an immediate release formulation of tacrolimus while providing the same or greater area under the curve (AUC), (iii) releases the tacrolimus substantially in the colon and/or the lower ileum, (iv) releases at most 63.5% of the tacrolimus in the dosage form at the 12 hour time point, or (v) any combination of any of the foregoing.

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Номер записи: 83

13-01-2022 дата публикации

DISPERSIBLE COMPOSITIONS

Номер: US20220008333A1

Автор: Goyvaerts Nicolaas Martha Felix, Patankar Harshad, Ranga Rajan Gopal Rajan

Принадлежит:

The present invention is concerned with dispersible compositions comprising rilpivirine or a pharmaceutically acceptable acid addition salt thereof as an active ingredient. Such compositions are useful in the treatment of HIV infection and their dispersibility properties lend themselves to be useful in particular amongst the pediatric or geriatric population. 1. A dispersible composition comprising E-4-[[4-[[4-(2-cyanoethenyl)-2 ,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]-benzonitrile (rilpivirine) or a pharmaceutically acceptable acid addition salt thereof , as the active ingredient , wherein said active ingredient is present in the dispersible composition in the form of granules , said granules further comprising a pharmaceutically acceptable excipient; wherein the dispersible composition comprises 2.5 mg base equivalent of E-4-[[4-[[4-(2-cyanoethenyl)-2 ,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]-benzonitrile; and wherein the dispersible composition further comprises next to the granules , in the extragranular fraction , a non-soluble diluent.2. The dispersible composition according to wherein the pharmaceutically acceptable excipient of the granules comprises a wetting agent.3. The dispersible composition according to wherein the pharmaceutically acceptable excipient of the granules comprises a disintegrant.4. The dispersible composition according to wherein the pharmaceutically acceptable excipient of the granules comprises a diluent.56.-. (canceled)7. The dispersible composition according to comprising in the extragranular fraction a wetting agent.8. The dispersible composition according to comprising in the extragranular fraction a disintegrant.9. The dispersible composition according to wherein the composition is a tablet.10. The dispersible composition according to wherein the active ingredient is rilpivirine HCl.1113.-. (canceled)14. A combination comprising a dispersible composition according to and one or more other therapeutic agents useful in the ...

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Номер записи: 84

13-01-2022 дата публикации

Combination Therapy for Male Sexual Dysfunction

Номер: US20220008415A1

Автор: FOSTER Howell

Принадлежит:

Pharmaceutical formulations containing a serotonin reuptake inhibitor and a phosphodiesterase 5 inhibitor are provided for the treatment of premature ejaculation and the increase in intravaginal ejaculatory latency time. Specific formulations contain tadalafil (1-30 mg per dose) and escitalopram (1-30 mg) in daily dose and on-demand formulations. 1. A method for delaying the onset of ejaculation in a male subject comprising administering to the subject 18 milligrams (mg) of escitalopram or a salt thereof and 9 mg of tadalafil or a salt thereof on-demand prior to sexual activity , wherein the onset of ejaculation by the subject is delayed during sexual activity by greater than 10 minutes.2. The method of claim 1 , wherein the escitalopram and tadalafil are administered at the same time.3. The method of claim 1 , wherein the escitalopram and tadalafil are administered orally in a single pharmaceutical formulation.4. The method of claim 1 , wherein the on-demand administering is within 36 hours prior to sexual activity.5. The method of claim 4 , wherein the on-demand administering is from 30 minutes to 5 hours prior to sexual activity.6. The method of claim 4 , wherein the on-demand administering is from 2 hours to 24 hours prior to sexual activity.7. The method of claim 4 , wherein said escitalopram and said tadalafil are co-administered to said male subject within about 36 hours claim 4 , within about 24 hours claim 4 , within about 12 hours claim 4 , within about 6 hours prior to sexual activity claim 4 , or within about 2 hours prior to sexual activity.8. The method of claim 1 , wherein the escitalopram and tadalafil are administered as a rapid dissolve tablet comprising 2.75% (w/w) escitalopram oxalate USP 39 powder claim 1 , 1.37% (w/w) tadalafil powder claim 1 , 81.22% (w/w) rapid dissolve tablet base powder claim 1 , 3.82% (w/w) micronized silica gel claim 1 , 9.16% (w/w) polyethylene glycol 3350 claim 1 , 0.61% (w/w) acesulfame potassium powder claim 1 , 0.46% ...

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Номер записи: 85

20-01-2022 дата публикации

UNIT ORAL DOSE COMPOSITIONS COMPOSED OF IBUPROFEN AND FAMOTIDINE FOR THE TREATMENT OF ACUTE PAIN AND THE REDUCTION OF THE SEVERITY AND/OR RISK OF HEARTBURN

Номер: US20220016088A1

Автор: Schachtel Bernard

Принадлежит:

Described herein are unit oral dose compositions that reduce the severity of heartburn and/or the risk of the occurrence of heartburn in a human in need of taking ibuprofen for the OTC treatment of acute pain wherein the human is not experiencing heartburn prior to the oral administration of the unit oral dose composition comprising orally administering to the human of a unit oral dose composition comprising (i) ibuprofen at a dosage from about 50 mg to about 400 mg per unit oral dose composition and (ii) famotidine at a dosage from about 3 mg to about 20 mg per unit oral dose composition, wherein the dissolution rate of famotidine in the unit oral dose composition in said human at a specified time within 45 minutes of administration of said unit oral dose composition to said human is greater than the dissolution rate of ibuprofen in the unit oral dose composition in said human at the same specified time. 1. A method for reducing the severity of heartburn and/or the risk of the occurrence of heartburn in a human in need of taking ibuprofen for the treatment of acute pain wherein the human is not experiencing heartburn prior to the oral administration of the unit oral dose composition comprising orally administering to the human of a unit oral dose composition comprising (i) ibuprofen at a dosage from about 50 mg to about 400 mg per unit oral dose composition and (ii) famotidine at a dosage from about 3 mg to about 20 mg per unit oral dose composition ,wherein the dissolution rate of famotidine in the unit oral dose composition in said human at a specified time within 45 minutes of administration of said unit oral dose composition to said human is greater than the dissolution rate of ibuprofen in the unit oral dose composition in said human at the same specified time.2. The method of claim 1 , wherein the famotidine in the unit oral dose composition has a dissolution rate that is about 10% to about 30% greater than the dissolution rate of ibuprofen at about 5 minutes ...

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Номер записи: 86

12-01-2017 дата публикации

Process for the preparation of a solid, orally administrable pharmaceutical composition

Номер: US20170007612A1

Автор: Klaus Benke

Принадлежит: Bayer Intellectual Property GmbH

The present invention relates to a process for the preparation of a solid, orally administrable pharmaceutical composition, comprising 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophenecarboxamide in hydrophilized form, and its use for the prophylaxis and/or treatment of diseases.

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Номер записи: 87

11-01-2018 дата публикации

FORMULATIONS OF 3-(6-(1-(2,2-DIFLUOROBENZO[D][1,3]DIOXOL-5-YL) CYCLOPROPANECARBOXAMIDO)-3-METHYLPYRIDIN-2-YL)BENZOIC ACID

Номер: US20180008546A1

Автор: Verwijs Marinus Jacobus

Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

A pharmaceutical composition comprising Compound 1, (3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid), and at least one excipient selected from: a filler, a disintegrant, a surfactant, a binder, and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Processes of preparing pharmaceutical compositions comprising Compound 1 are also disclosed. 152-. (canceled)53. A continuous process for preparing a tablet comprising 3-(6-(1-(2 ,2-Difluorobenzo[d][1 ,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid , comprising the steps of:a) mixing 3-(6-(1-(2,2-Difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid, a filler, and a disintegrant in a blender to form a blend;b) preparing a granulation solution with water, a binder, and a surfactant;c) feeding the blend from step a) into a continuous twin screw granulator while adding the granulation solution from step b) to produce granules;d) drying the granules from step c) and milling them;e) blending the milled granules from step d) with a filler, disintegrant, and lubricant to form a blend;f) compressing the blend from step e) into a tablet; andg) optionally coating the tablet from step f).54. The process of claim 53 , wherein 3-(6-(1-(2 claim 53 ,2-Difluorobenzo[d][1 claim 53 ,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid is in Form I claim 53 , wherein the Form I is characterized by one or more peaks at 15.2 to 15.6 degrees claim 53 , 16.1 to 16.5 degreees claim 53 , and 14.3 to 14.7 degrees in an X-ray powder diffraction obtained using Cu K alpha radiation.5512. The process of claims and claim 53 , wherein the tablet further comprises N-(5-hydroxy-2 claim 53 ,4-ditert-butyl-phenyl)-4-oxo-1H-quinoline-3-carboxamide.56. A tablet prepared by the process of any one of -.57. A method of ...

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Номер записи: 88

11-01-2018 дата публикации

EXTENDED RELEASE COMPOSITIONS OF AN AMINOALKYL NITRATE

Номер: US20180008558A1

Автор: Sartor Dirk, Scherhag Armin, STUCKLER Hubert, VANKAN Pierre

Принадлежит: CARDIOLYNX AG

The present invention relates to extended release compositions of an amino-C2-C6-alkyl nitrate and of pharmaceutically acceptable salt thereof, in particular 2-aminoethyl nitrate, and to fixed dose combinations with further pharmaceutically active drug substances. 2-Aminoethyl nitrate does not provoke nitrate tolerance, but has a very short half life in physiological systems. 1. An extended release composition of an amino-C-C-alkyl nitrate and of pharmaceutically acceptable salts thereof , wherein release is over 4-24 hours.2. An extended release composition according to claim 1 , wherein the amino-C-C-alkyl nitrate is selected from 4-aminobutyl nitrate claim 1 , 3-aminopropyl nitrate claim 1 , 2-amino-1-methylethyl nitrate claim 1 , and 2-aminoethyl nitrate.3. An extended release composition according to claim 1 , wherein the amino-C-C-alkyl nitrate is 2-aminoethyl nitrate.4. An extended release composition according to claim 1 , wherein the pharmaceutically acceptable salt is the tosylate.5. An extended release composition according to further comprising another pharmaceutically active compound in a fixed-dose combination.6. An extended release composition according to wherein the other pharmaceutically active compound is selected from the group of angiotensin receptor blockers claim 5 , angiotensin enzyme inhibitors claim 5 , renin antagonists claim 5 , beta blockers claim 5 , calcium channel blockers claim 5 , endothelin antagonists claim 5 , statins claim 5 , biguanides claim 5 , glitazones claim 5 , sulfonureas claim 5 , SGLT2 antagonists claim 5 , DPP-4 inhibitors claim 5 , antithrombotics claim 5 , antiplatelets claim 5 , anticoagulants claim 5 , antianginal drugs claim 5 , vasodilators claim 5 , and aldosterone antagonists.7. An extended release composition according to wherein the other pharmaceutically active compound is selected from valsartan claim 5 , azilsartan claim 5 , mazisentan claim 5 , cilostazol claim 5 , pioglitazone claim 5 , sitagliptin and ...

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Номер записи: 89

11-01-2018 дата публикации

PHARMACEUTICAL COMPOSITION CONTAINING CRYSTALLINE MACITENTAN

Номер: US20180008603A1

Автор: Englmeier Ludwig, Raneburger Johannes, Stefinovic Marijan

Принадлежит:

The present invention relates to an oral solid dosage form, in particular a tablet, comprising macitentan free base polymorphic form I. 1. A pharmaceutical composition comprising:crystalline macitentan free base having X-ray powder diffraction pattern showing peak maxima at 2 theta/° values of 11.4±0.2, 13.0±0.2, 16.1±0.2, and 25.4±0.2 when a radiation wavelength of 1.5419 Å is used; andat least one excipient.2. The pharmaceutical composition according to claim 1 , which is an oral solid dosage form.313- (canceled).14. The pharmaceutical composition according to claim 1 , comprising at most 5% by weight of amorphous Macitentan free base.15. The pharmaceutical composition according to claim 1 , comprising at most 1% by weight of amorphous Macitentan free base.16. The oral solid dosage form according to claim 2 , being a compressed dosage form.17. The oral solid dosage form according to being a tablet.18. The oral solid dosage form according to being an immediate release tablet.19. The oral solid dosage form according to claim 2 , comprising at least one filler claim 2 , at least one desintegrant claim 2 , at least one binder claim 2 , at least one lubricant claim 2 , and at least one surfactant.20. The oral solid dosage form according to claim 2 , wherein the crystalline Macitentan free base has a particle size distribution having a D98% of at most 680 μm and a D5% of at least 0.5 μm.21. The oral solid dosage form according to claim 2 , wherein the crystalline Macitentan free base has a particle size distribution having a D50% of from 3 μm to 250 μm.22. The oral solid dosage form according to claim 2 , wherein the crystalline Macitentan free base has a particle size distribution having a D50% of from 15 μm to 150 μm.23. The oral solid dosage form according to claim 2 , wherein the oral solid dosage form is to be administered to patients in a country having an area with an Af or an Am climate according to the Köppen-Geiger climate classification.24. The oral solid ...

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Номер записи: 90

14-01-2021 дата публикации

ABUSE-RESISTANT PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF OPIOID DEPENDENCE

Номер: US20210008061A1

Автор: Fischer Andreas

Принадлежит:

There is provided pharmaceutical compositions for the treatment of e.g. opioid dependency comprising microparticles of a pharmacologically-effective amount of buprenorphine, or a pharmaceutically-acceptable salt thereof, in associative admixture with particles comprising a weak acid, or particles comprising weakly-acidic buffer forming materials. The composition may further comprise a disintegrant and/or particles of a pharmacologically-effective amount of naloxone, or a pharmaceutically-acceptable salt thereof. The compositions are useful in the treatment of opioid dependency/addiction and/or pain. 1. (canceled)2. A method of treatment of opioid dependence in a subject , which method comprises the sublingual administration of a tablet comprising:(i) a dosage amount of buprenorphine or a pharmaceutically-acceptable salt thereof (calculated as the free base) that is 11.4 mg (±2%), 8.6 mg (±2%), 5.7 mg (±2%), 2.9 mg (±2%), or 1.4 mg (±2%);(ii) a dosage amount of naloxone or a pharmaceutically-acceptable salt thereof (calculated as the free base) that is about ¼ of the above doses of buprenorphine or salt thereof; and(iii) a weak acid,which tablet is made by compressing either:(a) a simple mixture comprising components (i), (ii) and (iii); and/or(b) granules comprising one or more of components (i), (ii) and (iii).3. The method as claimed in claim 2 , wherein the tablet further comprises a disintegrant.4. The method as claimed in claim 3 , wherein the disintegrant is selected from the group croscarmellose sodium claim 3 , sodium starch glycolate claim 3 , crosslinked polyvinylpyrrolidone claim 3 , and mixtures thereof.5. The method as claimed in claim 2 , wherein the weak acid is selected from the group consisting of citric acid claim 2 , malic acid claim 2 , tartaric acid claim 2 , fumaric acid claim 2 , adipic acid claim 2 , succinic acid claim 2 , lactic acid claim 2 , acetic acid claim 2 , oxalic acid claim 2 , maleic acid claim 2 , ammonium chloride claim 2 , and ...

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Номер записи: 91

14-01-2021 дата публикации

ABUSE-RESISTANT PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF OPIOID DEPENDENCE

Номер: US20210008062A1

Автор: Fischer Andreas

Принадлежит:

There is provided pharmaceutical compositions for the treatment of e.g. opioid dependency comprising microparticles of a pharmacologically-effective amount of buprenorphine, or a pharmaceutically-acceptable salt thereof, in associative admixture with particles comprising a weak acid, or particles comprising weakly-acidic buffer forming materials. The composition may further comprise a disintegrant and/or particles of a pharmacologically-effective amount of naloxone, or a pharmaceutically-acceptable salt thereof. The compositions are useful in the treatment of opioid dependency/addiction and/or pain. 1. (canceled)2. A pharmaceutical composition in the form of a compressed tablet suitable for sublingual administration , which comprises:(i) a dosage amount of buprenorphine or a pharmaceutically-acceptable salt thereof (calculated as the free base) that is 11.4 mg (±2%), 8.6 mg (±2%), or 5.7 mg (±2%);(ii) a dosage amount of naloxone or a pharmaceutically-acceptable salt thereof (calculated as the free base) that is about ¼ of the above doses of buprenorphine or salt thereof in the tablet; and(iii) a weak acid,wherein the tablet weighs no more than about 250 mg and has a hardness that is in the range of about 10N to about 100N, as measured by the US Pharmacopoeia method <1217>.3. The composition as claimed in claim 2 , wherein the tablet further comprises a disintegrant.4. The composition as claimed in claim 3 , wherein the disintegrant is selected from the group croscarmellose sodium claim 3 , sodium starch glycolate claim 3 , crosslinked polyvinylpyrrolidone claim 3 , and mixtures thereof.5. The composition as claimed in claim 2 , wherein the weak acid is citric acid.6. The composition as claimed in claim 5 , wherein the tablet further comprises a binder claim 5 , carrier particles claim 5 , sodium citrate or any combination of these.7. The composition as claimed in claim 2 , wherein the tablet has a hardness that is in the range of about 15N to about 50N.8. A method ...

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Номер записи: 92

10-01-2019 дата публикации

CELECOXIB AND AMLODIPINE FORMULATION AND METHOD OF MAKING THE SAME

Номер: US20190008777A1

Автор: EFRATI Yitshak Itsik

Принадлежит:

Provided herein is a celecoxib and amlodipine composition and method of making the same. The composition contains granules containing celecoxib. The amlodipine is incorporated into the composition as an extragranulate. 1. A method of preparing a pharmaceutical composition comprising celecoxib and amlodipine or pharmaceutically acceptable salts thereof , the method comprising the steps of:(i) wet granulating celecoxib or a pharmaceutically acceptable salt thereof and one or more excipients to obtain a wet granulate;(ii) drying the wet granulate of step (i) to obtain a dry granulate having a loss on drying (LOD) % of about 2.5% or less; and(iii) admixing the dry granulate of step (ii) with an extragranulate comprising amlodipine or a pharmaceutically acceptable salt thereof and optionally one or more excipients.2. The method of claim 1 , wherein the dry granulate has LOD % in the range of from about 0.5% to about 2%.3. The method of claim 2 , wherein the dry granulate has LOD % in the range of from about 0.5% to about 1.5%.4. The method of claim 1 , wherein step (i) comprises dry mixing celecoxib or a pharmaceutically acceptable salt thereof and one or more excipients to obtain a dry mixture claim 1 , and spraying the dry mixture with a granulation solution or suspension to obtain a wet granulate.5. The method of claim 4 , wherein the granulation solution or suspension comprises an aqueous medium.6. The method of claim 4 , wherein the granulation solution or suspension comprises an organic medium.7. The method of claim 1 , wherein the extragranulate in step (iii) comprises one or more excipients claim 1 , and wherein the one or more excipients in the wet granulate of step (i) and the one or more excipients in the extragranulate of step (iii) are the same or different selected from the group consisting of a diluent claim 1 , a disintegrant claim 1 , a surfactant claim 1 , a binder claim 1 , a glidant claim 1 , a lubricant claim 1 , and combinations thereof.8. The ...

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Номер записи: 93

08-01-2015 дата публикации

PHARMACEUTICAL COMPOSITION AND ADMINISTRATIONS THEREOF

Номер: US20150010628A1

Автор: DAS LAURA, Dokou Eleni, ISRANI MEGHNA JAI, JAMZAD SHAHLA, KNEZIC Dragutin, KUZMISSION ANDREW G.

Принадлежит:

The present invention relates to pharmaceutical compositions containing a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide including formulations of the solid dispersions into powders, granules and mini-tablets, methods for manufacturing and processing the powders and mini-tablets and methods for treating cystic fibrosis employing the pharmaceutical composition. 1. A pharmaceutical composition comprising a solid dispersion of amorphous or substantially amorphous Compound 1 , a filler , a sweetener , a disintegrant , a glidant and a lubricant , and optionally a wetting agent.220-. (canceled)21. A pharmaceutical composition comprising:a solid dispersion of amorphous or substantially amorphous Compound 1 in an amount of about 35 to about 47 percent by weight of the pharmaceutical composition;sucralose in an amount of about 2 percent by weight of the pharmaceutical composition;croscarmellose sodium in an amount from about 3 to about 6 percent of by weight of the pharmaceutical composition;SLS in an amount of about 0 to about 0.5 percent by weight of the pharmaceutical composition;colloidal silicon dioxide in an amount of about 1 percent by weight of the pharmaceutical composition;magnesium stearate in an amount of about 1.5 percent by weight of the pharmaceutical composition; andmannitol in an amount of about 42 to about 57.5 percent of by weight of the pharmaceutical composition.22. The pharmaceutical composition of claim 21 , wherein the croscarmellose sodium is present in an amount of about 5 percent of by weight of the pharmaceutical composition.23. The pharmaceutical composition of claim 22 , wherein the SLS is present in an amount of about 0.5 percent by weight of the pharmaceutical composition.24. The pharmaceutical composition of claim 21 , wherein the solid dispersion is present in an amount of about 35 percent by weight of the pharmaceutical composition.25. The pharmaceutical composition of claim 21 , ...

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Номер записи: 94

10-01-2019 дата публикации

ABUSE-PROOFED DOSAGE FORM

Номер: US20190008849A1

Автор: ARKENAU MARIC Elisabeth, Bartholomaeus Johannes, KUGELMANN Heinrich

Принадлежит: Grünenthal GmbH

The invention relates to a dosage form that is thermoformed without discoloration and is safeguarded from abuse, comprising at least one synthetic or natural polymer having a breaking strength of at least 500 N in addition to one or more active substances that could be subject to abuse. The invention also relates to a corresponding method for producing said dosage form. 1. An abuse-proofed dosage form thermoformed by extrusion without discoloration comprising one or more active ingredients with abuse potential (A) , optionally physiologically acceptable auxiliary substances (B) , at least one synthetic or natural polymer (C) and optionally at least one wax (D) ,wherein the dosage form exhibits a breaking strength of at least 500 N.2. The dosage form according to claim 1 , which is in the form of a tablet.3. The dosage form according to claim 1 , which contains as polymer (C) at least one polymer selected from the group consisting of polyalkylene oxide claim 1 , polyethylene claim 1 , polypropylene claim 1 , polyvinyl chloride claim 1 , polycarbonate claim 1 , polystyrene claim 1 , polyacrylate claim 1 , copolymers thereof and mixtures thereof.4. The dosage form according to claim 3 , wherein the polyalkylene oxide is selected from the group consisting of polymethylene oxide claim 3 , polyethylene oxide claim 3 , polypropylene oxide claim 3 , copolymers thereof and mixtures thereof.5. The dosage form according to claim 1 , wherein the polymer (C) comprises polyethylene oxide having a molecular weight of at least 0.5 million.6. The dosage form according to claim 5 , wherein the molecular weight of the polyethylene oxide (C) is at least 1 million.7. The dosage form according to claim 6 , wherein the molecular weight of the polyethylene oxide is in the range of from about 1 to about 15 million.8. The dosage form according to claim 1 , which contains the wax (D) claim 1 , and the wax (D) is at least one natural claim 1 , semi-synthetic or synthetic wax with a softening ...

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Номер записи: 95

10-01-2019 дата публикации

PHARMACEUTICAL COMPOSITIONS AND METHODS FOR FABRICATION OF SOLID MASSES COMPRISING ANTI-INTERLEUKIN ANTIBODIES

Номер: US20190008925A1

Автор: Hashim Mir, Imran Mir, Korupolu Radhika, Morales Mercedes

Принадлежит: InCube Labs, LLC

Embodiments of the invention provide shaped masses comprising one or more drugs such as proteins or polypeptides and methods for forming such shaped masses. One embodiment provides a shaped mass comprising a drug such as a protein or polypeptide having a biological activity in the body of a mammal. The shaped mass is formed by compression of a precursor material comprising the drug wherein an amount of biologically active drug in the mass is a preserved above a minimum level. Drugs which may be incorporated into the shaped mass may include one or more glucose regulating proteins such as insulin, incretins; and immunoglobulins such as TNF-inhibiting antibodies or interleukin neutralizing antibodies. Embodiments of the shaped mass may be incorporated into a tissue penetrating member which is inserted into the intestinal wall allowing for the oral delivery of proteins and peptides which would otherwise be degraded in the intestinal tract. 1. (canceled)2. A shaped mass comprising an immunoglobulin G (IgG) , the shaped mass comprising the IgG , wherein at least about 67% of the IgG in the shaped mass has affinity for an antigen , the shaped mass having a density in a range of about 0.80 to about 1.10 mg/mm.3. The shaped mass of claim 2 , wherein the density is in a range of about 1.00 to about 1.01 mg/mm.4. The shaped mass of claim 2 , wherein the precursor material has a particle size in a range of about 50 to about 450 μm.5. The shaped mass of claim 2 , wherein the compression is performed in a mold or fixture.6. The shaped mass of claim 2 , wherein the shaped mass is formed by compression of a powder comprising the IgG.7. The shaped mass of claim 2 , wherein the shaped mass has a pellet or cylindrical shape.8. The shaped mass of claim 2 , wherein the shaped mass has a tablet shape.9. The shaped mass of claim 2 , wherein the shaped mass has a tissue penetrating shape.10. The shaped mass of claim 2 , wherein the shaped mass comprises a biodegradable material said ...

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Номер записи: 96

10-01-2019 дата публикации

PHARMACEUTICAL COMPOSITIONS AND METHODS FOR FABRICATION OF SOLID MASSES COMPRISING POLYPEPTIDES AND/OR PROTEINS

Номер: US20190008926A1

Автор: Hashim Mir, Imran Mir, Korupolu Radhika, Morales Mercedes

Принадлежит: InCube Labs, LLC

Embodiments of the invention provide shaped masses comprising one or more drugs such as proteins or polypeptides and methods for forming such shaped masses. One embodiment provides a shaped mass comprising a drug such as a protein or polypeptide having a biological activity in the body of a mammal. The shaped mass is formed by compression of a precursor material comprising the drug wherein an amount of biologically active drug in the mass is a preserved above a minimum level. Drugs which may be incorporated into the shaped mass may include one or more glucose regulating proteins such as insulin, incretins; and immunoglobulins such as TNF-inhibiting antibodies or interleukin neutralizing antibodies. Embodiments of the shaped mass may be incorporated into a tissue penetrating member which is inserted into the intestinal wall allowing for the oral delivery of proteins and peptides which would otherwise be degraded in the intestinal tract. 1. A shaped mass comprising an immunoglobulin G (IgG) , wherein:at least about 67% of the IgG in the shaped mass has affinity for an antigen; andthe shaped mass has a density in a range of about 0.80 to about 1.10 mg/mm3.2. The shaped mass of claim 1 , wherein the density is in a range of about 1.00 to about 1.01 mg/mm3.3. The shaped mass of claim 1 , wherein IgG is an antibody.4. The shaped mass of claim 1 , wherein the shaped mass has a pellet shape.5. The shaped mass of claim 1 , wherein the shaped mass has a cylindrical shape.6. The shaped mass of claim 1 , wherein the shaped mass has a tablet shape.7. The shaped mass of claim 1 , wherein the shaped mass has a tissue penetrating shape.8. The shaped mass of claim 1 , wherein the shaped mass comprises a pharmaceutical excipient.9. The shaped mass of claim 8 , wherein the pharmaceutical excipient comprises at least one of a lubricant claim 8 , a binding agent or a bulking agent.10. The shaped mass of claim 1 , the shaped mass degrades in tissue to release the IgG into a patient's ...

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Номер записи: 97

09-01-2020 дата публикации

ABUSE-PROOFED ORAL DOSAGE FORM

Номер: US20200009082A1

Автор: ARKENAU-MARIC Elisabeth, BARTHOLOMÄUS Johannes, KUGELMANN Heinrich

Принадлежит: Grünenthal GmbH

The present invention relates to an abuse-proofed oral dosage form with controlled release of (1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol for once daily administration, which comprises the active ingredient and/or one or more of the pharmaceutically acceptable salts thereof (A), at least one synthetic or natural polymer (C), delayed-release auxiliary substances, optionally physiologically acceptable auxiliary substances (B) and optionally a wax (D), component (C) or (D) in each case exhibiting a breaking strength of at least 500 N, preferably of at least 1000 N. 1. An abuse-proofed , oral dosage form with controlled release of (1R ,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol for once daily administration , comprising (1R ,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol and/or at least one of the pharmaceutically acceptable salts or derivatives thereof (A) , at least one synthetic or natural polymer (C) , optionally delayed-release matrix auxiliary substances , optionally physiologically acceptable auxiliary substances (B) , optionally a wax (D) and optionally at least one delayed-release coating , component (C) or (D) in each case exhibiting a breaking strength of at least 500 N.2. A dosage form according to claim 1 , which is in the form of a tablet.3. A dosage form according to claim 1 , which is in multiparticulate form claim 1 , optionally press-molded into tablets or packaged in capsules.4. A dosage form according to claim 1 , wherein the polymer (C) is at least one polymer selected from among the group consisting of polyethylene oxides claim 1 , polyethylenes claim 1 , polypropylenes claim 1 , polyvinyl chlorides claim 1 , polycarbonates claim 1 , polystyrenes claim 1 , polyacrylates and the copolymers thereof.5. A dosage form according to claim 4 , wherein the polyethylene oxide is of high molecular weight.6. A dosage form according to claim 4 , wherein the polymer (C) is a water-soluble or water-swellable polymer.7. A dosage ...

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Номер записи: 98

09-01-2020 дата публикации

Ceritinib formulation

Номер: US20200009141A1

Автор: Sebastien Breulles, Simon Ensslin

Принадлежит: NOVARTIS AG

The present disclosure relates to a new pharmaceutical composition comprising Ceritinib. Particularly it is directed to the tablet that is prepared by wet granulation, wherein povidone is used as a binder. Further feature of the composition is that the drug and the binder form the inner phase, whereas all other excipients are added in a powder form as an outer phase. This way, the sticking of the composition is prevented and sufficient tablet hardness can be reached.

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Номер записи: 99

12-01-2017 дата публикации

VERIFICATION METHOD

Номер: US20170010091A1

Автор: Stuck Alexander, Walter Harald

Принадлежит:

The present invention relates to a verification method of tablets, in particular pharmaceutical tablets. It further relates to an invisible secure marking or information which is a part of such tablet. The invention further relates to tablets suitable for such verification method, to processes for manufacturing such tablets and methods for reading the information. 1. A verification method for a pharmaceutical tablet , comprising:compressing a powder mixture in a die between two punch tools to produce a core of the tablet, the compressing including embossing one or more three-dimensional structures on the surface of the core;applying a coating over the surface of the core to produce the tablet in finalized form with the one or more three-dimensional structures at an interface between the core and the coating, the coating rendering each of the one or more three-dimensional structures invisible to the unaided eye by appropriate color, thickness, reflection or scattering properties thereof; andverifying authenticity of the tablet after production of the tablet by scanning the tablet with an optical interferometry microscope to detect the one or more three-dimensional structures.2. The verification method of claim 1 , wherein verifying authenticity of the tablet further comprises:recording a data set with the detection device, the data set describing characteristics of the one or more three-dimensional structures; andcomparing the recorded data set with at least one predefined data set associated with the punch tools.3. The verification method of claim 2 , wherein the die and punch tools define one of a plurality of embossing tools used to make pharmaceutical tablets claim 2 , each of which is associated with one of a plurality of predefined data sets defining characteristics of the corresponding embossing tool claim 2 , and comparing the recorded data set further comprises:confirming whether the recorded data set matches at least one of the plurality of predefined data ...

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Номер записи: 100

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