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

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: 4

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: 5

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: 6

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: 7

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: 8

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: 9

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: 10

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: 11

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: 12

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: 13

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: 14

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: 15

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: 16

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: 17

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: 18

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: 19

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: 20

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: 21

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: 22

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: 23

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: 24

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: 25

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: 26

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: 27

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: 28

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: 29

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: 30

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: 31

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: 32

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: 33

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: 34

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: 35

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: 36

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: 37

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: 38

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: 39

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: 40

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: 41

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: 42

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: 43

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: 44

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: 45

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: 46

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: 47

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: 48

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: 49

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: 50

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: 51

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: 52

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: 53

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: 54

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: 55

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: 56

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: 57

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: 58

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: 59

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: 60

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: 61

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: 62

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: 63

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: 64

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: 65

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: 66

03-02-2022 дата публикации

Niclosamide Formulations and Methods of Use

Номер: US20220031642A1

Автор: Akash BAKSHI, Andrew Bartynski, Nadja Mannowetz

Принадлежит: Neurobo Pharmaceuticals Inc

Disclosed are niclosamide formulations for use in the treatment and prevention of viral infection. In some embodiments, the infection is transduced by a coronavirus, including a SARS-Cov-2 virus.

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Номер записи: 67

03-02-2022 дата публикации

Amorphous kinase inhibitor formulations and methods of use thereof

Номер: US20220031677A1

Автор: Corey Bloom, Fred Jordan, Michael D. Kaufman, Scott Bone

Принадлежит: Deciphera Pharmaceuticals LLC

Provided herein is an amorphous compound represented by Formula (I): and compositions thereof, which are useful in the treatment of disorders related to the activity of the c-KIT and PDGFRα kinases, and oncogenic forms thereof.

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Номер записи: 68

03-02-2022 дата публикации

PHARMACEUTICAL COMPOSITIONS OF 3-(6-(1-(2,2-DIFLUOROBENZO[D][1,3]DIOXOL-5-YL) CYCLOPROPANECARBOXAMIDO)-3-METHYLPYRIDIN-2-YL) BENZOIC ACID AND ADMINISTRATION THEREOF

Номер: US20220031679A1

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

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 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. 155-. (canceled)56. A tablet for oral administration comprising:a. 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Compound 1) Form I, wherein the Compound 1 Form I is present in an amount ranging from 25 mg to 250 mg;b. a filler;c. a disintegrant which is croscarmellose sodium and is present in an amount of about 6 wt % to about 10 wt % by weight of the tablet;d. a surfactant;e. a lubricant; andf. a binder.57. The tablet of claim 56 , wherein the filler is selected from cellulose claim 56 , modified cellulose claim 56 , sodium carboxymethyl cellulose claim 56 , ethyl cellulose hydroxymethyl cellulose claim 56 , hydroxypropylcellulose claim 56 , cellulose acetate claim 56 , microcrystalline cellulose claim 56 , dibasic calcium phosphate claim 56 , sucrose claim 56 , lactose claim 56 , corn starch claim 56 , potato starch claim 56 , and any combination thereof.58. The tablet of claim 56 , wherein the filler is microcrystalline cellulose (MCC) and is present in the tablet in an amount ranging from 20 wt % to 55 wt % by weight of the tablet.59. The tablet of claim 56 , wherein the surfactant is selected from sodium lauryl sulfate claim 56 , sodium stearyl fumarate claim 56 , polyoxyethylene 20 sorbitan mono-oleate claim 56 , and any combination thereof.60. The tablet of claim 56 , wherein the surfactant is sodium lauryl sulfate and is present in an amount ...

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Номер записи: 69

03-02-2022 дата публикации

Tamper Resistant Immediate Release Formulations

Номер: US20220031693A1

Автор: Adjei Akwete L., Chen Sibao, KUPPER Robert J., Mancinelli Vincent

Принадлежит:

Disclosed in certain embodiments is an immediate release solid oral dosage form comprising a plurality of particles, each particle comprising: (i) a core comprising a first active agent; (ii) a coating comprising a second active agent layered over the core; and (iii) a material that is sensitive to acidic pH layered over the coated core; wherein the dosage form releases at least about 70% of the second active agent within 45 minutes as measured by in-vitro dissolution in a USP Apparatus 2 (paddle) at 50 rpm in 500 ml 0.1 N HCl at 37° C. 1. A method of treating pain comprising administering to a patient in need thereof , an immediate release solid oral dosage form comprising a plurality of particles , each particle comprising:(i) an active agent; and(ii) a material that is sensitive to acidic pH;wherein the dosage form releases at least about 70% of the active agent within 45 minutes as measured by in-vitro dissolution in a USP Apparatus 2 (paddle) at 50 rpm in 500 ml 0.1 N HCl at 37° C.2. The method of claim 1 , wherein the plurality of particles are dispersed in a matrix.3. The method of claim 2 , wherein the matrix comprises a gelling agent.4. The method of claim 2 , wherein the matrix comprises a disintegrant.5. The method of claim 2 , wherein the matrix comprises a filler.6. The method of claim 1 , wherein each particle comprises either (I) a core comprising the active agent and the material sensitive to acidic pH layered on the core; or (II) a core comprising a first active agent claim 1 , a coating comprising a second active agent layered over the core and a material that is sensitive to acidic pH layered over the coated core.7. The method of claim 6 , wherein the core comprises an inert excipient layered with the active agent.8. The method of claim 6 , wherein the core comprises the active agent dispersed in a pharmaceutically acceptable excipient.9. The method of claim 1 , wherein each particle comprises:(i) a core comprising an inert excipient; and(ii) a ...

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Номер записи: 70

15-01-2015 дата публикации

Dosage form comprising lopinavir and ritonavir

Номер: US20150017237A1

Автор: Dominique Meergans, Konstantin Holfinger

Принадлежит: ratiopharm GmbH

The present invention relates to an oral dosage form comprising crystalline lopinavir and crystalline ritonavir. The invention further relates to methods of preparing said oral dosage forms containing the above pharmaceutical active agents.

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Номер записи: 71

15-01-2015 дата публикации

Method for treating intestinal diseases presenting at least one inflammatory component

Номер: US20150017239A1

Автор: Gerald Thomas PROEHL, Ii Emerson David Ballard, Luigi Moro, Michael Fangching HUANG, Wendell Wierenga

Принадлежит: COSMO TECHNOLOGIES LTD, Santarus Inc

The present disclosure relates to methods for treating intestinal diseases presenting at least one inflammatory component such as inflammatory bowel disease or diverticular disease and/or maintaining remission of intestinal diseases presenting at least one inflammatory component such as inflammatory bowel disease (IBD) or diverticular disease using budesonide MMX compositions.

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Номер записи: 72

17-01-2019 дата публикации

CONTROLLED RELEASE AND TASTE MASKING ORAL PHARMACEUTICAL COMPOSITION

Номер: US20190015342A1

Автор: AJANI Mauro, FOSSATI Lorenzo, PEDRANI Massimo, VILLA Roberto

Принадлежит: COSMO TECHNOLOGIES LIMITED

Controlled release and taste masking compositions containing one or more active principles inglobated in a three-component matrix structure, i.e. a structure formed by successive amphiphilic, lipophilic or inert matrices and finally inglobated or dispersed in hydrophilic matrices. The use of a plurality of systems for the control of the dissolution of the active ingredient modulates the dissolution rate of the active ingredient in aqueous and/or biological fluids, thereby controlling the release kinetics in the gastrointestinal tract. 1. (canceled)2. (canceled)3. A tablet for the treatment of ulcerative colitis consisting essentially of (1) a tableted core , and (2) a coating on said tableted core , wherein said tableted core consists of a compressed blend of ingredients , said ingredients comprising:(a) 9 mg of budesonide;(b) hydroxypropyl methylcellulose; and(c) magnesium stearate;wherein said coating on said tableted core comprises methacrylic acid copolymer type A, methacrylic acid copolymer type B, or a mixture of methacrylic acid copolymer type A and methacrylic acid copolymer type B;wherein following oral administration of the tablet to a human, the tablet provides an AUC of said budesonide in said human of about 16.43±10.52 (ng)×(h)/mL;and wherein said tablet provides extended release of budesonide in the colon of said human effective to treat ulcerative colitis in said human.4. The tablet of claim 3 , wherein said ingredients further comprise hydroxypropyl cellulose claim 3 , silicon dioxide claim 3 , lactose claim 3 , microcrystalline cellulose claim 3 , and lecithin.5. The tablet of claim 3 , wherein said ingredients further comprise starch or a starch derivative.6. The tablet of claim 4 , wherein said ingredients further comprise starch or a starch derivative.7. The tablet of claim 3 , wherein said ingredients do not comprise stearic acid.8. The tablet of claim 4 , wherein said ingredients do not comprise stearic acid.9. The tablet of claim 5 , wherein ...

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Номер записи: 73

17-01-2019 дата публикации

CONTROLLED RELEASE AND TASTE MASKING ORAL PHARMACEUTICAL COMPOSITIONS

Номер: US20190015428A1

Автор: AJANI Mauro, FOSSATI Lorenzo, PEDRANI Massimo, VILLA Roberto

Принадлежит: COSMO TECHNOLOGIES LIMITED

The invention relates to tablet comprising granules dispersed in at least one hydrophilic compound or matrix. The granules contain an active agent, at least one amphiphilic compound and at least one lipophilic compound. The tablet may include a gastro-resistant film coating. 1. (canceled)2. (canceled)3. A controlled release oral pharmaceutical composition consisting essentially of: a) budesonide in an amount to treat intestinal inflammation;', 'b) magnesium stearate, stearic acid, or a mixture thereof;', 'c) hydroxyalkyl cellulose; and', 'd) optionally starch or a starch derivative; and, '(1) a tableted core consisting of a compressed blend of ingredients, said ingredients comprising(2) a coating on said tableted core, said coating consisting essentially of a gastro-resistant film.4. The controlled release oral pharmaceutical composition according to claim 3 , wherein said ingredients further comprise lactose.5. The controlled release oral pharmaceutical composition according to claim 3 , wherein said ingredients comprise magnesium stearate.6. The controlled release oral pharmaceutical composition according to claim 3 , wherein said hydroxyalkyl cellulose is hydroxypropyl methylcellulose.7. The controlled release oral pharmaceutical composition according to claim 3 , wherein said ingredients comprise starch.8. The controlled release oral pharmaceutical composition according to claim 7 , wherein said ingredients comprise magnesium stearate.9. The controlled release oral pharmaceutical composition according to claim 8 , wherein said ingredients further comprise lactose.10. The controlled release oral pharmaceutical composition according to claim 7 , wherein said hydroxyalkyl cellulose is hydroxypropyl methylcellulose.11. The controlled release oral pharmaceutical composition according to claim 3 , wherein said ingredients comprise a starch derivative and magnesium stearate.12. The controlled release oral pharmaceutical composition according to claim 11 , wherein said ...

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Номер записи: 74

17-01-2019 дата публикации

PHARMACEUTICAL COMPOSITIONS AND METHODS FOR FABRICATION OF SOLID MASSES COMPRISING TNF-INHIBITING ANTIBODIES

Номер: US20190015482A1

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 a TNF inhibiting antibody , the shaped mass comprising the TNF inhibiting antibody , wherein at least about 75% of the TNF inhibiting antibody in the shaped mass has affinity for an epitope on a TNF molecule , the shaped mass having a density in a range of about 0.80 to about 1.10 mg/mm3.3. The shaped mass of claim 2 , wherein the density is in a range of about 0.85 to about 1.05 mg/mm3.4. The shaped mass of claim 2 , wherein the density is in a range of about 1.00 to about 1.01 mg/mm3.5. The shaped mass of claim 2 , wherein the precursor material has a particle size in a range of about 100 to 400 μm.6. The shaped mass of claim 2 , wherein at least about 80% of TNF inhibiting antibody in the shaped mass has affinity for an epitope on a TNF molecule.7. The shaped mass of claim 2 , wherein the TNF inhibiting antibody comprises adalimumab.8. The shaped mass of claim 7 , wherein the shaped mass comprises a therapeutically effective dose of adalimumab for treatment of an autoimmune disorder.9. The ...

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Номер записи: 75

19-01-2017 дата публикации

PHARMACEUTICAL FORM FOR COMBATING CHEMICAL SUBMISSION OF A MEDICAMENT

Номер: US20170016925A1

Автор: Contamin Pauline, Dupau Emmanuel, Herry Catherine

Принадлежит: ETHYPHARM

A pharmaceutical form for combating chemical submission includes an active ingredient and at least one compound which enables immediate modification of the organoleptic characteristics of a beverage into which the pharmaceutical form is introduced. The compound is selected from the group consisting of an opacifier, a fluorescent agent, floating particles, particles that are perceptible in the mouth, effervescent microgranules, and mixtures thereof. 1. A method of enabling the immediate detection of a pharmaceutical form illicitly introduced into a drink , said pharmaceutical form comprising an active principle which modifies the state of consciousness of a person , said method comprising: an active principle which modifies the state of consciousness of a person,', 'particles having a total diameter greater than 500 μm and a density less than one and that float in the drink and are perceptible in the mouth, said particles being microgranules comprising an insoluble blank support or a blank support coated with an insoluble polymer selected from the group consisting of non-water-soluble cellulose derivatives, (meth)acrylic (co)-polymer derivatives, polyvinyl acetate and mixtures thereof, or coated with a lipid material selected from the group consisting of glyceryl palmitostearate, waxes, polyoxyl-glycerides and glyceryl behenate,', 'a disintegration agent or disintegrant selected from the group consisting of crosslinked sodium carboxymethylcellulose known in the trade by the term croscarmellose, crospovidone and mixtures thereof,', 'a soluble diluent with binding properties selected from the group consisting of mannitol, xylitol, sorbitol, maltitol and mixtures thereof, provided that sorbitol is not the sole soluble diluent, and', 'a lubricant selected from the group consisting of magnesium stearate, sodium stearylfumarate, stearic acid, micronized polyoxyethylene glycol (micronized macrogol 6000) and mixtures thereof,', 'said pharmaceutical form being an ...

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Номер записи: 76

28-01-2016 дата публикации

Abuse-proofed oral dosage form

Номер: US20160022588A1

Автор: Elisabeth Arkenau-Maric, Heinrich Kugelmann, Johannes Bartholomäus

Принадлежит: GRUENENTHAL 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.

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Номер записи: 77

10-02-2022 дата публикации

SUSTAINED RELEASE AMINOPYRIDINE COMPOSITION

Номер: US20220040161A1

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:Cratio 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:Cratio 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: 78

24-01-2019 дата публикации

APIXABAN SOLID COMPOSITION AND PREPARATION METHOD THEREOF

Номер: US20190022008A1

Автор: HUANG Fangfang, HUANG Qibiao, HUANG Xin, You Jinsong, Zhao Feng

Принадлежит: SUNSHINE LAKE PHARMA CO., LTD.

The present invention provided an apixaban solid composition and a preparation method thereof. The method comprises granulating apixaban by wet granulation, wherein the apixaban has a particle size Dmore than 89 μm. 1. An apixaban solid composition comprising apixaban having a particle size Dmore than 89 μm , wherein the apixaban is dissolved in a wetting agent.23-. (canceled)4. The apixaban solid composition of claim 1 , wherein the apixaban has a particle size Dbetween 100 μm and 550 μm.5. (canceled)6. The apixaban solid composition of claim 46 , wherein the binder is povidone; or wherein the binder has a content of 2.00% to 8.00% by weight claim 46 , based on the total weight of the apixaban solid composition.7. The apixaban solid composition of claim 46 , wherein the binder is provided in dissolved form in an acidic substance or an organic solvent.89-. (canceled)10. The apixaban solid composition of further comprising a filler claim 46 , a disintegrant claim 46 , a surfactant and a lubricant.11. The apixaban solid composition of claim 10 , wherein the filler is corn starch claim 10 , pregelatinized starch claim 10 , complex starch claim 10 , lactose anhydrous claim 10 , lactose monohydrate claim 10 , microcrystalline cellulose claim 10 , methylcellulose claim 10 , hydroxy propyl cellulose claim 10 , hydroxy propyl methyl cellulose claim 10 , mannitol claim 10 , maltitol claim 10 , inositol claim 10 , xylitol claim 10 , lactitol or a combination thereof.12. The apixaban solid composition of claim 10 , wherein the filler is a mixture of lactose anhydrous and microcrystalline cellulose claim 10 , and wherein the content of the lactose anhydrous is from 33.50% to 63.50% and the content of the microcrystalline cellulose is from 24.00% to 54.00% by weight claim 10 , based on the total weight of the apixaban solid composition.13. (canceled)14. The apixaban solid composition of claim 10 , wherein the disintegrant is croscarmellose sodium; or wherein the disintegrant is ...

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Номер записи: 79

24-01-2019 дата публикации

SUSTAINED RELEASE AMINOPYRIDINE COMPOSITION

Номер: US20190022076A1

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:Cratio 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:Cratio 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: 80

24-01-2019 дата публикации

CONTROLLED RELEASE HYDROCODONE FORMULATIONS

Номер: US20190022086A1

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

Принадлежит:

A solid oral controlled-release oral dosage form of hydrocodone is disclosed. The dosage form comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and a sufficient amount of a controlled release material to render the dosage form suitable for twice-a-day administration to a human patient, the dosage form providing a C/Cratio of 0.55 to 0.85, said dosage form providing a therapeutic effect for at least about 12 hours. 141-. (canceled)42. A solid oral dosage form of hydrocodone comprising:a tablet core and a controlled release coating over the tablet core,wherein from about 0.5 mg to about 1250 mg hydrocodone or an equivalent amount of a pharmaceutically acceptable salt thereof is present in the dosage form,the dosage form releases hydrocodone for about 12 hours or longer and{'sub': 12', 'max, 'provides a plasma concentration profile of hydrocodone with a C/Chydrocodone ratio of 0.55 to 0.85.'}43. The dosage form of claim 42 , which releases hydrocodone for about 12 hours.44. The dosage form of claim 42 , which releases hydrocodone for about 24 hours.45. The dosage form of claim 42 , which provides a hydrocodone plasma concentration of at least about 8 ng/ml at about 2 hours after administration.46. The dosage form of claim 45 , which comprises a pharmaceutically acceptable polymer.47. The dosage form of claim 46 , wherein the pharmaceutically acceptable polymer comprises between 1% and 80% of the dosage form by weight.48. The dosage form of claim 42 , which comprises a material having a melting point of from 30 to about 200° C.49. The dosage form of claim 46 , wherein the pharmaceutically acceptable polymer is a hydroxyalkylcellulose.50. The dosage form of claim 49 , wherein the hydroxyalkylcellulose is a hydroxypropyl cellulose or a hydroxypropylmethylcellulose.51. The dosage form of claim 50 , wherein the hydroxyalkylcellulose is the hydroxypropylmethyl cellulose.52. The dosage form of claim 48 , wherein the ...

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Номер записи: 81

24-01-2019 дата публикации

CERITINIB FORMULATION

Номер: US20190022095A1

Автор: BREULLES Sebastien, ENSSLIN Simon

Принадлежит:

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. 1. A pharmaceutical composition comprising at least 150 mg and up to 750 mg Ceritinib and more than 40 and up to 70 weight percent of Ceritinib based on the total weight of the pharmaceutical composition , wherein the composition comprises granules consisting of or substantially consisting of Ceritinib and a binder and the granules are obtainable by wet granulation.2. The pharmaceutical composition according to claim 1 , wherein the binder is selected from the group consisting of starch claim 1 , Hypromellose (Hydroxypropylmethyl cellulose) claim 1 , Hydroxypropyl cellulose claim 1 , Hydroxy ethyl cellulose claim 1 , Povidone (Polyvinylpyrrolidone) claim 1 , Copovidone (copolyvidone) claim 1 , Gelatine and Polymethacrylate.3. The pharmaceutical composition according to claim 1 , wherein the binder is povidone (polyvinylpyrrolidone).4. The pharmaceutical composition according to claim 1 , further comprising another pharmaceutical excipient.5. The pharmaceutical composition according to claim 1 , further comprising a lubricant.6. The pharmaceutical composition according to claim 5 , wherein the lubricant is magnesium stearate.7. The pharmaceutical composition according to comprising at least 0.5 and up to 3 weight percent of magnesium stearate claim 6 , preferably at least 1 and up to 2 weight percent of magnesium stearate claim 6 , at least 1.3 and up to 1.7 weight percent of magnesium stearate claim 6 , particularly 1.5 weight percent of magnesium stearate based on the total weight of the pharmaceutical ...

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Номер записи: 82

24-01-2019 дата публикации

CONTROLLED RELEASE AND TASTE MASKING ORAL PHARMACEUTICAL COMPOSITIONS

Номер: US20190022112A1

Автор: AJANI Mauro, FOSSATI Lorenzo, PEDRANI Massimo, VILLA Roberto

Принадлежит: COSMO TECHNOLOGIES LIMITED

The invention relates to tablet comprising granules dispersed in at least one hydrophilic compound or matrix. The granules contain an active agent, at least one amphiphilic compound and at least one lipophilic compound. The tablet may include a gastro-resistant film coating. 1. (canceled)2. (canceled)3. A controlled release oral pharmaceutical composition consisting essentially of: a) budesonide in an amount to treat intestinal inflammation;', 'b) magnesium stearate, stearic acid, or a mixture thereof;', 'c) hydroxyalkyl cellulose; and', 'd) optionally starch or a starch derivative; and, '(1) a tableted core consisting of a dispersion of ingredients, said ingredients comprising(2) a coating on said tableted core, said coating consisting essentially of a gastro-resistant film.4. The controlled release oral pharmaceutical composition according to claim 3 , wherein said ingredients further comprise lactose.5. The controlled release oral pharmaceutical composition according to claim 3 , wherein said ingredients comprise magnesium stearate.6. The controlled release oral pharmaceutical composition according to claim 3 , wherein said hydroxyalkyl cellulose is hydroxypropyl methylcellulose.7. The controlled release oral pharmaceutical composition according to claim 3 , wherein said ingredients comprise starch.8. The controlled release oral pharmaceutical composition according to claim 7 , wherein said ingredients comprise magnesium stearate.9. The controlled release oral pharmaceutical composition according to claim 8 , wherein said ingredients further comprise lactose.10. The controlled release oral pharmaceutical composition according to claim 7 , wherein said hydroxyalkyl cellulose is hydroxypropyl methylcellulose.11. The controlled release oral pharmaceutical composition according to claim 3 , wherein said ingredients comprise a starch derivative and magnesium stearate.12. The controlled release oral pharmaceutical composition according to claim 11 , wherein said ...

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Номер записи: 83

24-01-2019 дата публикации

PHARMACEUTICAL FORMULATIONS CONTAINING MICROPARTICLES OR NANOPARTICLES OF A DELIVERY AGENT

Номер: US20190022228A1

Автор: Arbit Ehud, Dhoot Nikhil, Dinh Steven, Harris Jamila, Klein George, Lee Jongbin, Levchik Halina, Liao Jun, Liu Puchun, Majuru Shingai, Wang Nai Fang

Принадлежит:

This invention relates to microparticles and/or nanoparticles containing a delivery agent and/or an active agent. This invention also relates to pharmaceutical formulations and solid dosage forms, including controlled release solid dosage forms of active agent and a delivery agent. 111-. (canceled)12. A pharmaceutical formulation comprising particles having a median particle size of less than about 999 micrometers , the particles comprising a delivery agent and an active agent.1316-. (canceled)17. The pharmaceutical formulation of claim 12 , wherein the particles have a median particle size of about 45 to about 150 micrometers.18. The pharmaceutical formulation of claim 12 , wherein the particles have a median particle size of about 150 to about 250 micrometers.19. The pharmaceutical formulation of claim 12 , wherein the particles have a median particle size of about 250 to about 425 micrometers.20. The pharmaceutical formulation of claim 12 , wherein the particles have a median particle size of about 425 to about 850 micrometers.21. The pharmaceutical formulation of claim 12 , wherein the particles have a median particle size of about 100 to about 1000 nanometers.22. The pharmaceutical formulation of claim 21 , wherein the particles have a median particle size of about 500 to about 1000 nanometers.2338-. (canceled)39. The pharmaceutical formulation of claim 12 , wherein the delivery agent compound is selected from N-(8-[2-hydroxybenzoyl]amino)caprylic acid claim 12 , N-(10-[2-hydroxybenzoyl]-amino)decanoic acid claim 12 , 8-(2-hydroxy-4-methoxybenzoylamino)octanoic acid claim 12 , 8-(2-hydroxy-5-chlorobenzoylamino)-octanoic acid claim 12 , 4-[(2-hydroxy-4-chlorobenzoyl)-amino]butanoic acid claim 12 , and pharmaceutically acceptable salts thereof.40. The pharmaceutical formulation of claim 12 , wherein the delivery agent compound is N-(8-[2-hydroxybenzoyl]-amino)caprylic acid or a pharmaceutically acceptable salt thereof.41. The pharmaceutical formulation of claim ...

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Номер записи: 84

02-02-2017 дата публикации

SUSTAINED RELEASE AMINOPYRIDINE COMPOSITION

Номер: US20170027874A1

Автор: Cunningham Sean, Muligan Seamus, Myers Michael

Принадлежит:

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. 1. A sustained release tablet comprising:{'sub': max', 'τ', 'avSS, 'a sustained release matrix and an aminopyridine, said tablet exhibiting a release profile to obtain a C:C ratio in vivo of about 1.0 to about 3.5 and a predetermined C.'}2. The sustained release tablet of wherein said C:C ratio is about 1.5 to about 3.0.3. The sustained release tablet of wherein said predetermined Cis about 21 ng/ml.4. The sustained release tablet of wherein said predetermined Cis about 31 ng/ml.5. The sustained release tablet of wherein said predetermined Cis about 40 ng/ml.6. The sustained release tablet of wherein said C:C ratio is about 2.0 to about 3.0.7. The sustained release tablet of wherein said aminopyridine is 4-aminopyridine.8. The sustained release table of wherein said sustained release matrix is hydroxypropylmethylcellulose.9. A method of treating a disease associated with a neurological disorder claim 1 , said method comprising:{'sub': max', 'τ', 'avSS, 'administering an aminopyridine on a dosing regimen to obtain an in vivo C:Cratio 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:Cratio 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 ...

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Номер записи: 85

04-02-2016 дата публикации

DUAL DRUG DOSAGE FORMS WITH IMPROVED SEPARATION OF DRUGS

Номер: US20160030352A1

Автор: LIM JONG, Louie-Helm Jenny, Shell John N.

Принадлежит:

Drug tablets that include a prolonged-release core and an immediate-release layer or shell are prepared with a thin barrier layer of drug-free polymer between the prolonged-release and immediate-release portions of the tablet. The barrier layer is penetrable by gastrointestinal fluid, thereby providing full access of the gastrointestinal fluid to the prolonged-release core, but remains intact during the application of the immediate-release layer, substantially reducing or eliminating any penetration of the immediate-release drug into the prolonged-release portion. 118.-. (canceled)19. A dosage form for delivering a first drug that is immediately releasable upon ingestion and a second drug that is releasable by prolonged release defined as a release rate that is slow enough to leave at least about 40% of said second drug unreleased one hour after ingestion , said dosage form comprising:a prolonged-release section comprising said second drug dispersed in a solid matrix that releases said second drug by prolonged release upon immersion of said dosage form in gastrointestinal fluid;a polymeric film adhering to a surface of said prolonged-release section, said polymeric film being penetrable by gastrointestinal fluid and devoid of both said first drug and said second drug; andan immediate-release section comprising a solid layer adhering to said polymeric film, said solid layer comprising said first drug dispersed in a matrix that promotes immediate release of said first drug upon immersion of said dosage form in gastrointestinal fluidwherein said first and second drugs are selected from the group consisting of a diuretic, an angiotensin converting enzyme inhibitor, an angiotensin II antagonist, pyridoxine hydrochloride and a statin.20. The dosage form of claim 19 , wherein said solid matrix is selected from the group consisting of celluloses claim 19 , substituted celluloses claim 19 , microcrystalline cellulose claim 19 , polysaccharides claim 19 , substituted ...

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Номер записи: 86

29-01-2015 дата публикации

Tamper Resistant Immediate Release Formulations

Номер: US20150030677A1

Автор: Akwete L. Adjei, Robert J. Kupper, Sibao CHEN, Vincent Mancinelli

Принадлежит: Rhodes Pharmaeuticals LP

Disclosed is an immediate release solid oral dosage form comprising (i) an active agent; and (ii) a material that is sensitive to acidic pH;

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Номер записи: 87

01-02-2018 дата публикации

Encased Tamper Resistant Controlled Release Dosage Forms

Номер: US20180028450A1

Автор: Huang Haiyong Hugh

Принадлежит:

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. 1136-. (canceled)137. A solid controlled release dosage form comprising:a core comprising a first portion of hydrocodone or a pharmaceutically acceptable salt thereof dispersed in a first matrix material; anda shell encasing the core and comprising a second portion of the hydrocodone or pharmaceutically acceptable salt thereof dispersed in a second matrix material;wherein the first matrix material, the second matrix material, or both the first and the second matrix materials comprise polyethylene oxide having an average molecular weight from about 300,000 to about 10,000,000.138. The solid controlled release dosage form of claim 137 , wherein both the first and second matrix materials comprise polyethylene oxide having an average molecular weight from about 300 claim 137 ,000 to about 10 claim 137 ,000 claim 137 ,000.139. The solid controlled release dosage form of claim 138 , wherein both the first and second matrix materials comprise polyethylene oxide having average molecular weight from about 1 claim 138 ,000 claim 138 ,000 to about 10 claim 138 ,000 claim 138 ,000.140. The solid controlled release dosage form of claim 138 , wherein the first matrix material comprises polyethylene oxide having an average molecular weight from about 500 claim 138 ,000 to about 1 claim 138 ,000 claim 138 ,000.141. The solid controlled release dosage form of claim 138 , wherein the ...

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Номер записи: 88

01-02-2018 дата публикации

CONTROLLED RELEASE PHARMACEUTICAL COMPOSITIONS COMPRISING A FUMARIC ACID ESTER

Номер: US20180028483A1

Автор: MUELLER Bernd W., Nilsson Henrik

Принадлежит:

The present invention relates to controlled release pharmaceutical compositions comprising fumaric acid ester(s) as active substance(s). The compositions are suitable for use in the treatment of e.g. psoriasis or other hyperproliferative, inflammatory or autoimmune disorders and are designated to release the fumaric acid ester in a controlled manner so that local high concentrations of the active substance within the gastrointestinal tract upon oral administration can be avoided and, thereby, enabling a reduction in gastro-intestinal related side-effects. 1. A pharmaceutical composition comprising as an active substance one or more fumaric acid esters selected from di-(C-C)alkylesters of fumaric acid and mono-(C-C)alkylesters of fumaric acid , or a pharmaceutically acceptable salt thereof , which—upon oral administration and in comparison to that obtained after oral administration of Fumaderm® tablets in an equivalent dosage—gives a reduction in GI related side effects.2. The pharmaceutical composition according to in the form of a controlled release composition.3. A controlled release pharmaceutical composition for oral use comprising as an active substance one or more fumaric acid esters selected from di-(C-C)alkylesters of fumaric acid and mono-(C-C)alkylesters of fumaric acid claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein the release of the fumaric acid ester—when subjected to an in vitro dissolution test employing 0.1 N hydrochloric acid as dissolution medium during the first 2 hours of the test and then 0.05 M phosphate buffer pH 6.5 as dissolution medium—is as follows:within the first 3 hours after start of the test at the most about 70% w/w of the total amount of the fumaric acid ester contained in the composition is released.4. A controlled release pharmaceutical composition for oral use comprising as an active substance one or more fumaric acid esters selected from di-(C-C)alkylesters of fumaric acid and mono-(C-C)alkylesters of ...

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Номер записи: 89

01-02-2018 дата публикации

Novel Formulations of a Bruton's Tyrosine Kinase Inhibitor

Номер: US20180028537A1

Автор: Atluri Harisha, Chong Ching Wah, Hulvat James Francis, Kuehl Robert, McVey Alexander Jacob, Minikis Ryan Mitchell, Shu Cassandra, Tay Pearl Shwe-Cho

Принадлежит:

Described herein is the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, including novel pharmaceutical formulations thereof. Also disclosed are pharmaceutical compositions that include the Btk inhibitor, as well as methods of using the Btk inhibitor, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. 2. The pharmaceutical composition of claim 1 , wherein the solid dispersed ibrutinib is a spray-dried ibrutinib composition.3. The pharmaceutical composition of claim 2 , wherein the spray-dried ibrutinib composition comprises ibrutinib dispersed into one or more solubility enhancers.4. The pharmaceutical composition of claim 3 , wherein the solubility enhancer is a polymer matrix; and the polymer matrix comprises one or more polymers.5. The pharmaceutical composition of claim 4 , wherein the spray-dried ibrutinib composition comprises 1-90% w/w ibrutinib dispersed into the polymer matrix.6. The pharmaceutical composition claim 4 , wherein the polymer in the polymer matrix is a linear polymer claim 4 , a cross-linked polymer claim 4 , a co-polymer claim 4 , a graft polymer; or any combination thereof7. The pharmaceutical composition of claim 4 , wherein the polymer has a molecular weight in a range of about 2 claim 4 ,000 to about 500 claim 4 ,000 daltons claim 4 , about 100 claim 4 ,000 to about 200 claim 4 ,000 daltons claim 4 , about 200 claim 4 ,000 to about 300 claim 4 ,000 daltons claim 4 , or about 400 claim 4 ,000 to about 500 claim 4 ,000 daltons.8. A solid dispersion formulation comprising a solid dispersion pharmaceutical composition according to claim 1 , and a pharmaceutically acceptable carrier.9. The solid dispersion formulation of claim 8 , wherein the solid dispersion formulation is in a form of ...

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Номер записи: 90

31-01-2019 дата публикации

MODIFIED RELEASE FORMULATION OF LACOSAMIDE

Номер: US20190029968A1

Автор: Dalal Satish Kumar, Jahagirdar Harshal, Konda Kishore Kumar, Kulkarni Shirishkumar

Принадлежит: Lupin Limited

The present invention provides a modified release formulation of lacosamide. The modified release formulation of the present invention comprising lacosamide and modified release polymer provides modified release of lacosamide with minimal Cto Cpeak to trough variation over a period of at least 12 hrs. 114.-. (canceled)15. A modified release formulation comprising lacosamide and modified release polymer.16. The modified release formulation of claim 15 , wherein the modified release polymer is selected from the group consisting of hydrophilic polymer claim 15 , hydrophobic polymer claim 15 , wax; and mixtures thereof.17. The modified release formulation of claim 16 , wherein the hydrophilic polymer is selected from the group consisting of cellulose derivatives such as methyl cellulose claim 16 , hydroxypropyl methylcellulose claim 16 , hydroxyethyl cellulose claim 16 , hydroxypropyl cellulose claim 16 , hydroxyethyl methylcellulose claim 16 , carboxymethylcellulose and sodium carboxymethylcellulose; vinyl pyrrolidone polymers such as polyvinylpyrrolidone and copolymers of vinyl pyrrolidone and vinyl acetate; polysaccharides; gums of plant claim 16 , animal claim 16 , mineral or synthetic origin; polysaccharide such as alginic acid derivatives; chitosan claim 16 , gellan and xanthan gum; alkylene oxide such as polyethylene oxide; and mixtures thereof.18. The modified release formulation of claim 16 , wherein the hydrophobic polymer is selected from the group consisting of ethyl cellulose; methacrylic acid derivatives; cellulose acetate and its derivatives; poly vinyl alcohols and its derivatives; polyacrylamide derivatives; and mixtures thereof.19. The modified release formulation of claim 16 , wherein the wax is selected from the group consisting of glycerol palmitostearate; beeswax; glycowax; castor wax; carnauba wax; glycerol monostearate; stearyl alcohol; glycerol behenic acid ester; cetyl alcohol; natural and synthetic glycerides; waxes; fatty acids; hydrogenated ...

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Номер записи: 91

31-01-2019 дата публикации

Methylphenidate Extended Release Chewable Tablet

Номер: US20190030014A1

Автор: KATHALA Kalyan, Perumal Ashok, Tu Yu-Hsing

Принадлежит:

An oral methylphenidate extended release tablet is described, which can be scored and still retain its extended release profile. The tablet contains a combination of an uncoated methylphenidate-ion exchange resin complex, a barrier coated methylphenidate-ion exchange resin complex-matrix, and an uncomplexed methylphenidate active component. Following administration of a single dose of the extended release methylphenidate chewable tablet, a therapeutically effective amount of methylphenidate is reached in less than about 20 minutes and the composition provides a twelve-hour extended release profile. 1(a) a sustained release methylphenidate component comprising a water-insoluble, water-permeable, pH-independent barrier coated, methylphenidate-ion exchange resin complex in a polymeric matrix, wherein said barrier coating is over the methylphenidate-ion exchange resin complex-matrix;(b) a first immediate release component which comprises an immediate release uncoated methylphenidate-ion exchange resin complex;(c) a second immediate release methylphenidate component which comprises an uncomplexed methylphenidate;wherein said first immediate release component (b) has a slower onset of release than (c);wherein about 50% w/w to about 90% w/w of the methylphenidate active component is provided by the sustained release component based on the total amount of methylphenidate in the tablet, andwherein said chewable tablet is capable of being divided and providing tablet portions which retain a therapeutically effective immediate release and 12 hour extended release profile.. A methylphenidate extended release chewable tablet having a therapeutically effective immediate release and a 12-hour extended release profile, wherein said chewable tablet is a uniform solid dispersion comprising: Methylphenidate hydrochloride (HCl) and dexmethylphenidate hydrochloride both have the empirical formula CHNO.HCl. Methylphenidate HCl is a racemic mixture of d,1-threo-methyl α-phenyl-2- ...

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Номер записи: 92

30-01-2020 дата публикации

TAMPER-RESISTANT DOSAGE FORM WITH IMMEDIATE RELEASE AND RESISTANCE AGAINST SOLVENT EXTRACTION

Номер: US20200030317A1

Автор: Barnscheid Lutz, DENKER JANA, GEIßLER- FICHTNER ANJA, WENING Klaus

Принадлежит: Grünenthal GmbH

A tamper-resistant pharmaceutical dosage form comprising a multitude of particles which comprise a pharmacologically active compound, a polyalkylene oxide, and a disintegrant; wherein the pharmacologically active compound is dispersed in a matrix comprising the polyalkylene oxide and the disintegrant; wherein the dosage form provides under in vitro conditions immediate release of the pharmacologically active compound in accordance with Ph. Eur. The tamper-resistant pharmaceutical dosage form is useful in methods of treat diseases or disorders susceptible to the pharmacologically active compound; and in some embodiments discourages abuse in that when reduced to a powder the powdered dosage form exhibits a lower score for drug-liking than the pharmacologically active compound itself as assessed on a visual analog scale. 1. A tamper-resistant pharmaceutical dosage form comprising:a multitude of particles, each of which particles comprises an extruded mixture of a pharmacologically active compound, a polyalkylene oxide, and a disintegrant;wherein the pharmacologically active compound is selected from the group consisting of amphetamine and the physiologically acceptable salts thereof;wherein the tamper-resistant pharmaceutical dosage form provides under in vitro conditions immediate release of the pharmacologically active compound in accordance with Ph. Eur.; andwherein the tamper-resistant pharmaceutical dosage form exhibits a lower score for drug-liking than the pharmacologically active compound by itself as assessed on a visual analog scale, wherein said lower score for drug-liking is assessed on said visual analog scale by manipulating the tamper-resistant pharmaceutical dosage form to a first powder, insufflating the first powder intranasally, and assessing the drug-likability score of the first powder insufflated intranasally, and comparing said drug-likability score to that of a second powder of the pharmacologically active compound by itself insufflated ...

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Номер записи: 93

30-01-2020 дата публикации

COMPOSITIONS COMPRISING FUSIDIC ACID AND PACKAGES THEREFOR

Номер: US20200030448A1

Автор: PEREIRA David Eugene

Принадлежит:

Described are solid pharmaceutical compositions of fusidic acid, and pharmaceutically acceptable salts thereof, dosage units of the pharmaceutical compositions, and packages for pharmaceutical compositions of fusidic acid, and pharmaceutically acceptable salts thereof, which increase stability against the degradation of the fusidic acid, and pharmaceutically acceptable salts thereof. Also described are uses of the pharmaceutical compositions and dosage units in treating diseases. 1. A solid pharmaceutical composition comprising fusidic acid , or a pharmaceutically acceptable salt thereof , and mannitol.261.-. (canceled) This application claims priority under 35 U.S.C. § 119(e) to U.S. Provisional Application Ser. No. 61/489,017 filed May 23, 2011. The entire disclosure of which is incorporated herein by reference.The invention described herein pertains to solid pharmaceutical compositions of fusidic acid, and pharmaceutically acceptable salts thereof, dosage units of the pharmaceutical compositions, and packages for pharmaceutical compositions of fusidic acid, and pharmaceutically acceptable salts thereof. The invention described herein also pertains to solid pharmaceutical compositions and packages that may enhance stability to the degradation of the fusidic acid, or pharmaceutically acceptable salt thereof. The invention described herein also pertains to uses of the pharmaceutical compositions and dosage units in treating diseases.Fusidic acid is a tetracyclic triterpenoid or fusidane antibiotic derived from the fungus that inhibits bacterial protein synthesis. Fusidic Acid has the following structure.The term fusidic acid is also often used to denote not only fusidic acid, but also its pharmaceutically acceptable salts, such as the sodium salt, sodium fusidate, as well as hydrates, solvates or mixtures thereof, any of which may be considered the fusidic acid component. Accordingly, as used herein, the term fusidic acid generally refers individually and ...

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Номер записи: 94

04-02-2021 дата публикации

Multiparticulate solid dosage form having an elastic texture

Номер: US20210030681A1

Автор: Jean-Claude Tritsch

Принадлежит: DSM IP ASSETS BV

The present invention relates to a multiparticulate solid dosage form ( 1 ) which has an elastic texture and which contains a plurality of microcapsules ( 2 ) having a core ( 2 a ) and a shell ( 2 b ) that are embedded in an edible matrix ( 3 ). Microcapsules ( 2 ) contain an active ingredient which may be a pharmaceutical drug and/or a micronutrient. The multiparticulate solid dosage form of the invention is obtainable by a method wherein a mixture comprising water, microcapsules and starch particles is casted. The starch particles swell or dissolve only after casting.

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Номер записи: 95

04-02-2021 дата публикации

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

Номер: US20210030748A1

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 to 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;(ii) naloxone or a pharmaceutically-acceptable salt thereof provided in an amount (calculated as the free base) that is about ¼ of the dosage amount of buprenorphine or salt thereof;(iii) a weak acid; and(iv) a disintegrant;wherein, when an aqueous USP/NF potassium phosphate buffer with a pH of 6.8 is dripped at a rate of about 2 mL per minute through a tube with an inner diameter of about 3 mm onto said tablet placed on top of a Porosity 1 20 mm diameter silica filter in a glass funnel with an upper inner diameter of 55 mm, in which the distance between the end of the tube and the silica filter in the funnel is about 7.5 cm, the cumulative release of buprenorphine from said tablet is more than 40% of the dosage amount after 2.5 minutes.3. The pharmaceutical composition as claimed in claim 2 , wherein the disintegrant is selected from the group croscarmellose sodium claim 2 , sodium starch glycolate claim 2 , crosslinked polyvinylpyrrolidone claim 2 , and mixtures thereof.4. The pharmaceutical composition as claimed in claim 2 , wherein the weak acid is provided in the form of particles comprising the weak acid.5. The pharmaceutical composition as ...

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Номер записи: 96

04-02-2021 дата публикации

Pharmaceutical composition including sodium alkyl sulfate

Номер: US20210030755A1

Автор: Kenji Kusumoto, Sadahiro Miyamura

Принадлежит: Taiho Pharmaceutical Co Ltd

The object of the present invention is to improve the dissolution and the absorption of (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl-1-pyrrolidinyl)-2-propen-1-one effective as an antitumor agent from a pharmaceutical formulation comprising the same. Provided is a pharmaceutical composition comprising (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl-1-pyrrolidinyl)-2-propen-1-one in combination with sodium alkyl sulfate having an alkyl group containing 10 to 18 carbon atoms, in particular, with sodium lauryl sulfate.

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Номер записи: 97

05-02-2015 дата публикации

Delayed Release Pharmaceutical Compositions of Salsalate

Номер: US20150037408A1

Автор: Brij Khera, Kothari Jay Shantilal, MISTRY Gaurav Navinbhai, Muthaiyyan Esakkimuthu KANNAN

Принадлежит: Individual

The present invention relates to modified release pharmaceutical compositions comprising salsalate. The invention also relates to processes for the preparation of such compositions.

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Номер записи: 98

05-02-2015 дата публикации

CONTROLLED RELEASE HYDROCODONE FORMULATIONS

Номер: US20150037409A1

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

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 of hydrocodone , the dosage form comprising an amount of a hydrocodone bitartrate salt equivalent to from about 5 mg to about 60 mg of hydrocodone ,the dosage form providinga ratio of a plasma concentration of hydrocodone at the end of a dosing interval to a maximum plasma concentration of hydrocodone during the dosing interval of about 0.55 to about 1, and an effective pain relief over a period of time of about 12 hours or longer after administration to a human patient or a population of patients,an in-vitro release of hydrocodone when measured by the USP Basket method at 100 rpm in 700 ml aqueous buffer at a pH of 1.2 at 37° C. of from 10% to about 45% by weight hydrocodone released at 1 hour,the dosage form is a capsule comprisinga first portion of said amount of the hydrocodone bitartrate salt in an immediate release form andthe remaining portion of said amount of the hydrocodone bitartrate salt and a controlled release material in an extended release form, whereinsaid hydrocodone bitartrate salt is the only active agent in the dosage form.40: The dosage form of claim 39 , wherein the effective pain relief is provided for about 12 hours.41: The dosage form of claim 40 , wherein said administration is first administration.42: The dosage form of claim 41 , wherein the controlled release material comprises a material selected from the group consisting of gums claim 41 , cellulose ethers claim 41 , acrylic resins claim 41 , waxes claim 41 , shellac and oils.43: A solid oral controlled-release dosage form of hydrocodone claim 41 , the dosage form comprising an amount of a hydrocodone bitartrate salt equivalent to from about 5 mg to about 60 mg of hydrocodone and a controlled ...

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Номер записи: 99

05-02-2015 дата публикации

Tamper resistant dosage forms

Номер: US20150037412A1

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: 100

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