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    • 10. 发明申请
    • Modified-release compositions of at least one form of venlafaxine
    • 至少一种文拉法辛的改性释放组合物
    • US20050244498A1
    • 2005-11-03
    • US11003028
    • 2004-12-03
    • Pawan SethPaul Maes
    • Pawan SethPaul Maes
    • A61K9/00A61K9/24A61K9/28A61K31/277
    • A61K9/2866A61K9/282A61K9/284A61K31/277
    • The present invention relates to a modified release composition of at least one form of venlafaxine, which is an enhanced absorption delayed controlled release composition for oral administration suitable for once daily dosing. The composition comprises a core comprising at least one form of venlafaxine selected from the group consisting of venlafaxine, an active metabolite of venlafaxine, a pharmaceutically acceptable salt of venlafaxine, a pharmaceutically acceptable salt of an active metabolite of venlafaxine, and combinations thereof, and a pharmaceutically acceptable excipient. The composition further comprises a modified release coating which substantially surrounds the core. The compositions of the invention provide enhanced absorption delayed controlled release of the at least one form of venlafaxine such that the combined geometric mean ratio of the composition of the invention to the reference product for the AUC0-t or the Cmax for venlafaxine and its active metabolite O-desmethylvenlafaxine is greater than 2 after first administration of the composition under fed or fasting conditions.
    • 本发明涉及文拉法辛的至少一种形式的改性释放组合物,其是适用于每日一次给药的口服给药的增强的吸收延迟控释组合物。 所述组合物包含核心,其包含选自文拉法辛,文拉法辛的活性代谢物,文拉法辛的药学上可接受的盐,文拉法辛的活性代谢物的药学上可接受的盐及其组合中的至少一种形式的文拉法辛和 药学上可接受的赋形剂。 组合物还包含基本上围绕芯的改性释放涂层。 本发明的组合物提供增强的吸收延迟控制释放至少一种形式的文拉法辛,使得本发明的组合物与参考产品的组合几何平均比例用于AUC 0-t或 对于文拉法辛及其活性代谢物O-去甲基文拉法辛的C max max大于2,在给予或禁食条件下首次施用组合物后。