发明名称 PHARMACEUTICAL COMPOSITION COMPRISING A PROTEINASE INHIBITOR AND A MONOGLYCERIDE
摘要 1. A pharmaceutical composition, comprising (a) a therapeutically effective amount of proteinase inhibitor, pharmaceutically acceptable salts thereof or or esters (including salts thereof) (b) a pharmaceutically acceptable carrier comprising monoglycerides of (C8-C10) medium chain fatty acids, the monoglyceride is present in the amount enough for dissolving proteinase inhibitor. 2. The composition of claim 1, wherein the weight ratio of monoglyceride in (b) to the compound in (a) is at least about 1.5. 3. The composition of claim2, wherein the weight ratio of monoglyceride in (b) to the compound in (a) is at least about 3.0. 4. The composition of any claims 1 to 3, wherein the acid number of the compound (b) is less or equal to about 0,04. 5. The composition of any claims 1 to 4, wherein further comprising polyvinylpyrrolidone. 6. The composition of any claims 1 to 4, wherein the compound (a) is formula N-tert-butyl-decahydro-2-[2(R)-hydroxy-4-phenyl-3-(S)-[[N-(2-quinolylcarbonyl)-L-asparginyl]amino]butyl]-(4aS,8aS)-isoquinline-3-carboxamide. 7. The composition of claim 6, further comprising about 0.01 to about 0.5% dl .alpha.-tocopherol by weight of the composition. 8. The pharmaceutical composition of any claim 1 to 7 in the form of a unit dose of said pharmaceutical composition.
申请公布号 EA001413(B1) 申请公布日期 2001.02.26
申请号 EA19980000023 申请日期 1996.06.04
申请人 F.HOFFMAN-LA ROCHE 发明人 BAILY, CAROLE, ANNE
分类号 C07D295/08;A61K9/48;A61K31/00;A61K31/18;A61K31/195;A61K31/34;A61K31/341;A61K31/35;A61K31/351;A61K31/38;A61K31/381;A61K31/40;A61K31/403;A61K31/425;A61K31/426;A61K31/44;A61K31/4402;A61K31/4418;A61K31/4427;A61K31/445;A61K31/47;A61K31/472;A61K31/4725;A61K31/495;A61K31/535;A61K31/5375;A61K45/00;A61K45/08;A61K47/14;A61K47/22;A61K47/34;A61P31/12;A61P31/18;A61P37/04;A61P43/00;C07D207/16;C07D209/52;C07D211/60;C07D213/30;C07D213/38;C07D215/48;C07D217/26;C07D277/24;C07D277/28;C07D307/20;C07D309/38;C07D333/32;C07D333/78;C07D401/12;C07D401/14;C07D495/04 主分类号 C07D295/08
代理机构 代理人
主权项
地址