Title:
SOLID COMPOSITION FOR CONTROLLED RELEASE OF IONIZABLE ACTIVE AGENTS WITH POOR AQUEOUS SOLUBILITY AT LOW PH AND METHODS OF USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2010/057036
Kind Code:
A3
Abstract:
A novel solid composition and methods for making and using the solid composition are provided. The solid composition comprises: (a) at least one active agent with a solubility of less than about 0.3 mg/ml in an aqueous solution with a pH of at most about 6.8 at a temperature of about 37oC; and (b) a hydrophilic polymer matrix composition comprising: i) a hydrophilic polymer selected from the group consisting of METHOCELTM, POLYOXTM WSR 1105 and combinations thereof; and optionally ii) a hydrophobic polymer selected from the group consisting of Ethocel 20 premium; and (c) an alkalizer selected from the group consisting of calcium carbonate, magnesium oxide heavy and sodium bicarbonate; wherein the composition provides at least about 70% release of the active between about 7 to about 12 hours following oral administration.
Inventors:
RAMANI CHANDIR (CA)
WANG JUAN (US)
KANE ANIL (CA)
CHOW KWOK (CA)
LAMBING JOE (US)
WANG JUAN (US)
KANE ANIL (CA)
CHOW KWOK (CA)
LAMBING JOE (US)
Application Number:
PCT/US2009/064455
Publication Date:
June 09, 2011
Filing Date:
November 13, 2009
Export Citation:
Assignee:
PORTOLA PHARM INC (US)
PATHEON INC (CA)
RAMANI CHANDIR (CA)
WANG JUAN (US)
KANE ANIL (CA)
CHOW KWOK (CA)
LAMBING JOE (US)
PATHEON INC (CA)
RAMANI CHANDIR (CA)
WANG JUAN (US)
KANE ANIL (CA)
CHOW KWOK (CA)
LAMBING JOE (US)
International Classes:
A61K9/20; A61K31/19; A61K31/192; A61K31/405; A61K31/517; A61P7/02; A61P9/00
Foreign References:
| US20060228411A1 | 2006-10-12 | |||
| US20080279845A1 | 2008-11-13 | |||
| US20070123547A1 | 2007-05-31 |
Other References:
RIIS ET AL: "pH-independent drug release of an extremely poorly soluble weakly acidic drug from multiparticulate extended release formulations", EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, ELSEVIER SCIENCE PUBLISHERS B.V., AMSTERDAM, NL, vol. 65, no. 1, 1 December 2006 (2006-12-01), pages 78 - 84, XP005788727, ISSN: 0939-6411, DOI: DOI:10.1016/J.EJPB.2006.07.001
MEKA L. ET AL.: "Design and evaluation of polymeric coated minitablets as multiple unit gastroretentive floating drug delivery systems for furosemide.", JOURNAL OF PHARMACEUTICAL SCIENCES, vol. 98, no. 6, 13 November 2008 (2008-11-13), pages 2122 - 2132, XP002629134, DOI: 10.1002/jps.21562
MEKA L. ET AL.: "Design and evaluation of polymeric coated minitablets as multiple unit gastroretentive floating drug delivery systems for furosemide.", JOURNAL OF PHARMACEUTICAL SCIENCES, vol. 98, no. 6, 13 November 2008 (2008-11-13), pages 2122 - 2132, XP002629134, DOI: 10.1002/jps.21562
Attorney, Agent or Firm:
HOPKINS, Mark H. et al. (Two Embarcadero Center Eighth Floo, San Francisco California, US)
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