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    • 12. 发明申请
    • CONTROLLED RELEASE COMPOSITIONS COMPRISING AN ACYLANILIDE
    • 控制释放包含ACYLANILIDE的组合物
    • WO2006076533A1
    • 2006-07-20
    • PCT/US2006/001163
    • 2006-01-12
    • ELAN PHARMA INTERNATIONAL LIMITEDLIVERSIDGE, GaryJENKINS, Scott
    • LIVERSIDGE, GaryJENKINS, Scott
    • A61K9/14A61K9/20A61K9/26
    • A61K9/5084
    • The invention relates to a controlled release composition comprising acylanilide, and preferably bicalutamide, for use, in particular, in combination therapy with a luteinizing hormone-releasing hormone (LHRH) analogue for the treatment of stage D2 metastatic carcinoma of the prostate. The controlled release composition comprises an immediate release component and a modified release component or formulation. The immediate release component comprises a first population of bicalutamide. The modified release formulation preferably comprises a second population of acylanilide bicalutamide, and a controlled release constituent. The controlled release formulation is preferably in the form of an erodable formulation, a diffusion controlled formulation or an osmotic controlled formulation. The combination of the immediate release and modified release components in operation deliver the active ingredient in a pulsed or bi-modal manner.
    • 本发明涉及包含酰基苯胺,优选比卡鲁胺的控释组合物,特别是用于与促黄体生成激素释放激素(LHRH)类似物联合治疗以治疗前列腺D2期转移性癌。 控释组合物包含立即释放组分和改性释放组分或制剂。 立即释放组分包含比卡鲁胺的第一群体。 改性释放制剂优选包含第二种酰基苯胺比卡鲁酰胺和控释组分。 控制释放制剂优选为可侵蚀制剂,扩散控制制剂或渗透控制制剂的形式。 在操作中即时释放和释放组分的组合以脉冲或双向方式递送活性成分。