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    • 57. 发明申请
    • NANOPARTICULATE COMPOSITIONS OF HETEROCYCLIC AMIDE DERIVATIVES
    • 杂环化合物衍生物的纳米颗粒组合物
    • WO2006096462A1
    • 2006-09-14
    • PCT/US2006/007465
    • 2006-03-02
    • ELAN PHARMA INTERNATIONAL LIMITEDLIVERSIDGE, GaryJENKINS, Scott
    • LIVERSIDGE, GaryJENKINS, Scott
    • A61K9/14
    • A61K9/145A61K9/146A61K9/2018A61K9/2027A61K9/205A61K9/2054A61K9/2077
    • The present invention is directed to compositions comprising nanoparticulate heterocyclic amide derivative and preferably zafirlukast nanoparticles, also collectively referred to as "active ingredient," having improved solubility in water. The nanoparticles of the composition have an effective average particle size of less than about 2,000 nm, and are useful in the treatment of asthma. The invention also relates to a multiparticulate modified release composition comprising the active ingredient that in operation delivers the drug in a pulsed or bimodal manner for the treatment of asthma. The controlled release composition comprises an immediate release component and a modified release component. The immediate release component comprises a first population of heterocyclic amide derivative, and preferably zafirlukast particles, and the modified release component comprises a second population of heterocyclic amide derivative, and preferably zafirlukast nanoparticles, and a controlled release component, wherein the combination of the immediate release and modified release components in operation delivers the active ingredient in a pulsed or bimodal manner. The heterocyclic amide derivative can be released from the multiparticulate particles in an erosable, diffusion or osmotic controlled release system.
    • 本发明涉及包含纳米颗粒杂环酰胺衍生物和优选扎非司酮纳米颗粒的组合物,其也统称为“活性成分”,其具有改善的在水中的溶解度。 组合物的纳米颗粒具有小于约2,000nm的有效平均粒度,并且可用于治疗哮喘。 本发明还涉及一种多微粒改性释放组合物,其包含在操作中以脉冲或双峰方式递送药物以治疗哮喘的活性成分。 控释组合物包含立即释放组分和改性释放组分。 立即释放组分包含第一批杂环酰胺衍生物,优选扎法司他颗粒,并且改性释放组分包含第二组杂环酰胺衍生物,优选扎非司酮纳米颗粒和控释组分,其中立即释放组合 并且操作中的改性释放组分以脉冲或双峰方式递送活性成分。 杂环酰胺衍生物可以在可侵蚀,扩散或渗透控制释放系统中从多颗粒颗粒中释放。
    • 59. 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。