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1. 发明申请

WO2004052405A1 ORAL FORMULATIONS FOR POORLY ABSORPTIVE HYDROPHILIC DRUGS 审中-公开
标题翻译：不良吸收性水解药物的口服制剂
公开(公告)号：WO2004052405A1
公开(公告)日：2004-06-24
申请号：PCT/KR2003/002700
申请日：2003-12-10
申请人： CHONG KUN DANG PHARMACEUTICAL CORP. , MC TECHNOLOGIES, INC. , HONG, CHUNG-IL , SHIN, Hee-Jong , KI, Min-Hyo , CHOI, Mee-Hwa
发明人： HONG, CHUNG-IL , SHIN, Hee-Jong , KI, Min-Hyo , CHOI, Mee-Hwa
IPC分类号： A61K47/48
CPC分类号： B82Y5/00 , A61K47/6929
摘要： Disclosed herein is a pharmaceutical composition for oral absorption of polar drugs. The composition consists essentially of (a) at least one polar active substance having a bioavailability of less than 30% which is poorly absorptive through lipid membranes because of its high hydrophilicity and charged ion; (b) at least one organic alkalizing agent having an amino acid or polyol structure which shows alkalinity in aqueous solution and is ionically bonded to the polar active substance; and (c) at least one surfactant having a C 6-18 fatty acid structure which has an HLB of 4 to 18. Alternatively, the composition consists essentially of (d) at least one organic alkalizing agent having the characteristics of both the organic alkalizing agent and the surfactant instead of the organic alkalizing agent and the surfactant. The composition enables polar active drugs to penetrate the gastro- intestinal membrane and oral dosage forms to be substituted for injections.
摘要翻译：本文公开了用于口服吸收极性药物的药物组合物。所述组合物基本上由（a）至少一种具有小于30％的生物利用度的极性活性物质组成，其通过脂质膜难以吸收，因为它具有高亲水性和带电离子; （b）至少一种具有在水溶液中显示碱度并与极性活性物质离子键合的氨基酸或多元醇结构的有机碱化剂; 和（c）至少一种具有HLB为4至18的C 6-18脂肪酸结构的表面活性剂。或者，组合物基本上由（d）至少一种具有两种有机碱化剂的有机碱化剂和表面活性剂代替有机碱化剂和表面活性剂。该组合物可使极性活性药物穿透胃肠膜和口服剂型以代替注射。

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