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1. 发明申请

US20020103181A1 Pharmaceutical composition for controlled release of an active ingredient 审中-公开
标题翻译：用于控制释放活性成分的药物组合物
公开(公告)号：US20020103181A1
公开(公告)日：2002-08-01
申请号：US09726636
申请日：2000-11-30
申请人： LUPIN LABORATORIES LIMITED
发明人： Himadri Sen , Rajesh Suresh Kshirsagar , Chandrashekhar Shriram Kandi , Shailesh Suresh Bhamare
IPC分类号： A61K031/545
CPC分类号： A61K31/545 , A61K9/205 , A61K9/209
摘要： A pharmaceutical composition in the form of a tablet for controlled release of an active ingredient comprises a betalactam antibiotic such as cephalexin, cefaclor or their pharmaceutically acceptable hydrates, salts or esters as active ingredient, and a mixture of hydrophilic polymers selected from the group consisting of at least one sodium alginate and at least one xanthan gum as controlled release matrix; and optionally probenecid as an antibiotic adjuvant as either immediate release or controlled release part. The composition may also contain one or more of a water soluble and/or water dispersible diluent, wherein the quantities of the hydrophilic polymers and water soluble and/or water dispersible diluents are such that the therapeutically effective active ingredient is released at a rate suitable for once or twice daily administration of the pharmaceutical composition. Inclusion of probenecid allows reduction in the amount of active incorporated in the hydrophilic polymer matrix but still provides the desired once a day profile. The resulting modified release matrix formulation not containing probenecid may be administered once or twice daily. The resulting modified release matrix formulation containing probenecid may be administered once daily.
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β-内酰胺抗生素如头孢氨苄，头孢克洛或其药学上可接受的水合物，盐或酯作为活性成分，以及选自以下的亲水性聚合物的混合物：至少一种藻酸钠和至少一种黄原胶作为受控释放基质; 和可选地作为抗生素佐剂的丙磺舒作为立即释放或控制释放部分。组合物还可以含有一种或多种水溶性和/或水分散性稀释剂，其中亲水性聚合物和水溶性和/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一次或两次给药药物组合物。包含丙磺舒可以减少亲水性聚合物基质中掺入的活性物质，但仍能提供所需的一天一次。不含丙磺舒的所得改性释放基质制剂可以每天施用一次或两次。含有丙磺舒的所得改性释放基质制剂可以每天施用一次。

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