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1. 发明授权

US5948440A Modified release matrix formulation of cefaclor and cephalexin 失效
标题翻译：头孢克洛和头孢氨苄的改性释放基质配方
公开(公告)号：US5948440A
公开(公告)日：1999-09-07
申请号：US992151
申请日：1997-12-17
申请人： Jagdish Arora , Girish Jain , Himadri Sen
发明人： Jagdish Arora , Girish Jain , Himadri Sen
IPC分类号： A61K9/20 , A61K9/22 , A61K9/28 , A61K9/30 , A61K31/545 , A61K47/38
CPC分类号： A61K31/545 , A61K9/2054 , A61K9/2866 , Y10S514/964
摘要： A pharmaceutical composition in the form of a tablet for controlled release of an active ingredient comprises cefaclor, cephalexin, or their pharmaceutically acceptable hydrates, salts, or esters as active ingredient, and a mixture of hydrophilic polymers of different viscosity grades selected from the group consisting of at least one hydroxypropyl methylcellulose and at least one hydroxypropylcellulose. The composition optionally also contains one or more of a water soluble or water dispersible diluent. The quantities of the hydrophilic polymers and water soluble or water dispersible diluent are such that the therapeutically effective active ingredient is released at a rate suitable for twice daily administration of the pharmaceutical composition to human subjects. The tablets may also be coated with a rapidly dissolving water soluble polymeric film coat. In a preferred embodiment, the composition comprises about 50% to about 90% by weight of cefaclor, cephalexin, or their pharmaceutically acceptable hydrates, salts, or esters, and about 5% to about 35% of a mixture of hydrophilic polymers of different grades, wherein the hydrophilic polymers comprise about 0.1% to about 20% by weight of hydroxypropyl methylcellulose and about 0.1% to about 20% by weight of hydroxypropyl cellulose.
摘要翻译：用于控制释放活性成分的片剂形式的药物组合物包括头孢克洛，头孢氨苄或其药学上可接受的水合物，盐或酯作为活性成分，以及不同粘度等级的亲水聚合物的混合物，其选自的至少一种羟丙基甲基纤维素和至少一种羟丙基纤维素。组合物任选地还含有一种或多种水溶性或水分散性稀释剂。亲水性聚合物和水溶性或水分散性稀释剂的量使得治疗有效的活性成分以适合于每天两次向药物组合物施用给人类受试者的速率释放。片剂也可以用快速溶解的水溶性聚合物膜包衣包衣。在优选的实施方案中，组合物包含约50％至约90％重量的头孢克洛，头孢氨苄或其药学上可接受的水合物，盐或酯，以及约5％至约35％的不同等级的亲水性聚合物的混合物，其中所述亲水性聚合物包含约0.1重量％至约20重量％的羟丙基甲基纤维素和约0.1重量％至约20重量％的羟丙基纤维素。

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