发明名称 IMPROVED ORAL DOSAGE FORMULATIONS
摘要 A formulation comprising, and process for preparing, improved oral dosage forms of 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-urea, a chemical entity with anti-inflammatory properties. Granulation of 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-urea within specified ranges provides improved dissolution of 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-urea and oral bioavailability, as well as content uniformity. Incorporation into the formulation of an aqueous soluble inclusion compound capable of forming a complex with 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-urea, such as beta-cyclodextrin provides enhanced stability of 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-urea, in particular in highly ionic environments. Chipping and disintegration of tablets containing more than about 10 % betacyclodextin can be prevented by applying a polymeric coat to the surface of the tablet at a temperature below 40 DEG C.
申请公布号 WO0207772(A3) 申请公布日期 2002.10.17
申请号 WO2001US21860 申请日期 2001.07.11
申请人 BOEHRINGER INGELHEIM PHARMACEUTICALS, INC. 发明人 CAPPOLA, MICHAEL, L.;GEREG, GEORGE, W.;WAY, SUSAN
分类号 A61K9/14;A61K9/16;A61K9/20;A61K9/48;A61K31/5355;A61K31/5377;A61K47/30;A61K47/36;A61K47/40;A61K47/48;A61P1/04;A61P17/06;A61P19/02;A61P29/00 主分类号 A61K9/14
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