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    • 32. 发明申请
    • Pharmaceutical compositions for controlled release delivery of biologically active compounds
    • 用于控释释放生物活性化合物的药物组合物
    • US20060034923A1
    • 2006-02-16
    • US11201932
    • 2005-08-11
    • Yuhua LiBenjamin Chien
    • Yuhua LiBenjamin Chien
    • A61K31/663A61K9/22
    • A61K31/663A61K9/0024A61K9/1647A61K9/7007A61K31/704A61K38/22A61K38/26A61K38/31A61K47/34A61K47/541A61K47/548
    • The present invention provides compositions and methods for the controlled release delivery of one or more biologically active compounds to a subject. Specifically, the invention provides for a pharmaceutical composition for the controlled release delivery of biologically active compounds to a subject comprising: a) a complex of a biologically active compound having at least one basic functional group and a polyanion derived from hexahydroxycyclohexane having at least two negatively charged functional groups; and b) a pharmaceutically acceptable carrier comprising a biodegradable, water-insoluble polymer. By complexing a biologically active compound with a polyanion, the tight, stable complex may be incorporated into a long-acting dosage system having a more desired drug release curve over time than that is found in the prior art. The invention also provides the methods of making such compositions and the methods of use thereof.
    • 本发明提供了一种或多种生物活性化合物向受试者的控制释放递送的组合物和方法。 具体地说,本发明提供了用于向受试者控释生物活性化合物的药物组合物,包括:a)具有至少一个碱性官能团的生物活性化合物和衍生自六羟基环己烷的聚阴离子的复合物,其具有至少两个负面 带电功能组; 和b)包含可生物降解的水不溶性聚合物的药学上可接受的载体。 通过使生物活性化合物与聚阴离子络合,紧密,稳定的复合物可以掺入长效剂量系统中,其具有比现有技术中发现的更长时间的药物释放曲线。 本发明还提供了制备这种组合物的方法及其使用方法。