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    • 10. 发明授权
    • Multiparticulate modified release composition
    • 多微粒改性组合物
    • US06902742B2
    • 2005-06-07
    • US10331754
    • 2002-12-30
    • John G. DevanePaul StarkNiall M. M. FanningGurvinder Singh Rekhi
    • John G. DevanePaul StarkNiall M. M. FanningGurvinder Singh Rekhi
    • A61K9/26A61K9/20A61K9/40A61K9/48A61K9/50A61K9/54A61K9/56A61K9/58A61K31/4458A61K47/32A61P11/00A61P25/00A61P43/00A61K9/14
    • A61K9/5084
    • The invention relates to a multiparticulate modified release composition that in operation delivers an active ingredient in a pulsed or bimodal manner. The multiparticulate modified release composition comprises an immediate release component and a modified release component; the immediate release component comprising a first population of active ingredient containing particles and the modified release component comprising a second population of active ingredient containing particles coated with a controlled release coating; wherein the combination of the immediate release and modified release components in operation deliver the active ingredient in a pulsed or a bimodal manner. The invention also relates to a solid oral dosage form containing such a multiparticulate modified release composition. The plasma profile achieved by the multiparticulate modified release composition is advantageous in reducing patient tolerance to the active ingredient and in increasing patient compliance by reducing dosage frequency.
    • 本发明涉及一种多微粒改性释放组合物,其在操作中以脉冲或双峰方式递送活性成分。 多微粒改性释放组合物包含立即释放组分和改性释放组分; 所述立即释放组分包含含有颗粒的第一组活性成分,所述改性释放组分包含第二组活性成分,所述活性成分含有涂覆有控释涂层的颗粒; 其中操作中的速释组分和改进释放组分的组合以脉冲或双峰方式递送活性成分。 本发明还涉及含有这种多微粒改性释放组合物的固体口服剂型。 通过多微粒改性释放组合物实现的血浆曲线有利于减少患者对活性成分的耐受性,并通过降低剂量频率提高患者依从性。