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    • 33. 发明申请
    • Extended release formulation of beta-lactam antibiotics
    • β-内酰胺抗生素的延长释放制剂
    • US20060233878A1
    • 2006-10-19
    • US10568325
    • 2003-09-30
    • Shailesh BhamareIndu BhushanHimadri Sen
    • Shailesh BhamareIndu BhushanHimadri Sen
    • A61K31/545A61K9/22
    • A61K9/2018A61K9/2027A61K31/545
    • A pharmaceutical composition for controlled drug delivery comprising a β-lactam antibiotic or its pharmaceutically acceptable hydrates, salts or esters, and one or more carbomers. The above β-lactam antibiotics formulation avoids the limitations of known β-lactam controlled release form which are found to be either complex and/or cost-extensive to obtain requiring multiphase and/or selective coatings or fail to achieve the desired controlled release for once daily dosage form. Importantly, in the β-lactam antibiotic form of the above the rate-controlling polymer wherein the Cmax of the formulation is substantially the same as that of a single dose of the immediate release formulation. Also advantageously the formulation achieves a rate controlling polymer wherein the T>MIC for the formulation is more than 17 hours when the MIC is 0.25 mcg/ml and more than 10 hours when the MIC is 2 mcg/ml. The above β-lactam antibiotic form is thus directed to serve as the much desired simple and cost-effective controlled release form suitable for once daily administration.
    • 用于受控药物递送的药物组合物,其包含β-内酰胺抗生素或其药学上可接受的水合物,盐或酯,以及一种或多种卡波姆。 上述β-内酰胺抗生素制剂避免了已知的β-内酰胺控制释放形式的限制,其被认为是复杂的和/或成本广泛的以获得需要多相和/或选择性涂层或不能达到期望的一次控制释放 日剂量。 重要的是,在上述β-内酰胺抗生素形式中,速率控制聚合物,其中制剂的最大值与单剂量的立即释放制剂基本上相同。 还有利地,制剂实现速率控制聚合物,其中当MIC为0.25mcg / ml时,制剂的T> MIC大于17小时,当MIC为2mcg / ml时超过10小时。 因此,上述β-内酰胺抗生素形式被用作适合于每日一次给药的理想的简单和成本有效的控制释放形式。
    • 36. 发明授权
    • Modified release matrix formulation of cefaclor and cephalexin
    • 头孢克洛和头孢氨苄的改性释放基质配方
    • US5948440A
    • 1999-09-07
    • US992151
    • 1997-12-17
    • Jagdish AroraGirish JainHimadri Sen
    • Jagdish AroraGirish JainHimadri Sen
    • A61K9/20A61K9/22A61K9/28A61K9/30A61K31/545A61K47/38
    • A61K31/545A61K9/2054A61K9/2866Y10S514/964
    • 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.
    • 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。