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    • 9. 发明申请
    • POLYMERIC IMPLANTS, PREFERABLY CONTAINING A MIXTURE OF PEG AND PLG, FOR CONTROLLED RELEASE OF A GNRH
    • 聚合物植入物,含有PEG和PLG的混合物,用于控制释放的GNRH
    • WO2006071208A1
    • 2006-07-06
    • PCT/US2004/043079
    • 2004-12-23
    • DURECT CORPORATIONBROWN, James, E.GIBSON, John, W.
    • BROWN, James, E.GIBSON, John, W.
    • A61K9/00A61K38/00A61K9/16
    • A61K9/1647A61K9/0024A61K9/1635
    • Controlled release compositions for controlling release of a GnRH molecule or a GnRH analog are provided. The compositions include a GnRH molecule or GnRH analog as an active agent, and a controlled release component for controlling release of the GnRH molecule or GnRH analog from the composition. The compositions provide a sustained mean steady state plasma concentration (Css) of the active agent of at least about 1.5 ng/mL for a period of at least about 48 hours when the composition is administered to a subject. In addition, the use of a controlled release component in the manufacture of a composition for the controlled release of a GnRH molecule or GnRH analog is provided. The controlled release component'is capable of providing a sustained mean steady state plasma concentration (C 38 ) of the active agent of at. least about 1.5 ng/mL for a period of at least about 48 hours when the manufactured composition is administered to a subject. The controlled release component can include a polymeric material and/or a non-polymeric material. When the compositions are administered to a subject, for example when implanted, the compositions release the active agent in a controlled fashion. Methods for producing the compositions are also provided, as are methods of using the compositions to provide for controlled release of the GnRH molecule or GnRH analog in a subject. Preferred polymeric material is PLG or a copolymer of PLG and a PEG derivative such as methoxy PEG. Preferred non-polymeric material can be SAIB.
    • 提供了用于控制GnRH分子或GnRH类似物释放的控制释放组合物。 组合物包括GnRH分子或GnRH类似物作为活性剂,以及用于控制组合物中GnRH分子或GnRH类似物释放的控释组分。 当组合物施用于受试者时,组合物提供至少约1.5ng / mL的持续的平均稳态血浆浓度(Css)至少约48小时的时间。 此外,提供了控制释放组分在制备用于控制释放GnRH分子或GnRH类似物的组合物中的用途。 控制释放组分“能够提供at的活性剂的持续平均稳态血浆浓度(C 38 S 38)。 至少约1.5ng / mL至少约48小时的时间。 控制释放组分可以包括聚合物材料和/或非聚合材料。 当将组合物施用于受试者时,例如当植入时,组合物以受控的方式释放活性剂。 还提供了用于制备组合物的方法,以及使用该组合物提供受试者中GnRH分子或GnRH类似物的受控释放的方法。 优选的聚合物材料是PLG或PLG和PEG衍生物如甲氧基PEG的共聚物。 优选的非聚合物材料可以是SAIB。