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SOLID COMPOSITION FOR CONTROLLED RELEASE OF IONIZABLE ACTIVE AGENTS WITH POOR AQUEOUS SOLUBILITY AT LOW PH AND METHODS OF USE THEREOF
专利权人:
Portola Pharmaceuticals; Inc.
发明人:
Chandir Ramani,Juan Wang,Anil Kane,Kwok Chow,Joe Lambing
申请号:
US13633055
公开号:
US20130172374A1
申请日:
2012.10.01
申请国别(地区):
US
年份:
2013
代理人:
摘要:
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 37° C. and (b) a hydrophilic polymer matrix composition comprising: i) a hydrophilic polymer selected from the group consisting of METHOCEL™, POLYOX™ 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.
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