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    • 10. 发明申请
    • Controlled Release Compositions Comprising Heterocyclic Amide Derivative Nanoparticles
    • 包含杂环酰胺衍生物纳米颗粒的控制释放组合物
    • US20080254114A1
    • 2008-10-16
    • US11571377
    • 2006-03-02
    • Scott A. JenkinsGary Liversidge
    • Scott A. JenkinsGary Liversidge
    • A61K9/16A61K31/404A61K9/54A61K9/26A61P11/06
    • 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。