SOLID COMPOSITION FOR CONTROLLED RELEASE OF IONIZABLE ACTIVE AGENTS WITH POOR AQUEOUS SOLUBILITY AT LOW PH AND METHODS OF USE THEREOF
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 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.
申请公布号
WO2010057036(A3)
申请公布日期
2011.06.09
申请号
WO2009US64455
申请日期
2009.11.13
申请人
PORTOLA PHARMACEUTICALS, INC.;PATHEON INC.;RAMANI, CHANDIR;WANG, JUAN;KANE, ANIL;CHOW, KWOK;LAMBING, JOE
发明人
RAMANI, CHANDIR;WANG, JUAN;KANE, ANIL;CHOW, KWOK;LAMBING, JOE