PROCESS
    2.
    发明公开
    PROCESS 审中-公开
    处理

    公开(公告)号:EP1915131A1

    公开(公告)日:2008-04-30

    申请号:EP06769601.3

    申请日:2006-08-09

    申请人: AstraZeneca AB

    IPC分类号: A61K9/10

    摘要: The present invention relates to a process for the preparation of a stable dispersion of particles, particularly sub-micron particles in an aqueous medium and to a stable dispersion of particles in a liquid medium. The process provided comprises the following steps: 1) combining a) an emulsion comprising a continuous aqueous phase; an inhibitor; a stabiliser; with b) the substantially water-insoluble substance; and 2) increasing the temperature to vicinity of the melting temperature of the substantially water-insoluble substance. The sub-micron dispersion provided exhibit reduced or substantially no particle growth during storage and reduced crystallisation rate of the substantially water insoluble active compound.

    摘要翻译: 本发明涉及一种制备稳定的颗粒分散体,特别是亚微米颗粒在含水介质中的稳定分散体和颗粒在液体介质中稳定分散体的方法。 所提供的方法包括以下步骤:1)合并a)包含连续水相的乳液; 一种抑制剂; 一个稳定器; 与b)基本上不溶于水的物质; 和2)将温度升高到基本上不溶于水的物质的熔化温度附近。 所提供的亚微米分散体在储存过程中表现出减少的或基本上没有颗粒生长并且降低了基本上不溶于水的活性化合物的结晶速率。

    MODIFIED RELEASE FORMULATION
    3.
    发明授权
    MODIFIED RELEASE FORMULATION 有权
    药物缓释

    公开(公告)号:EP1322293B1

    公开(公告)日:2006-09-27

    申请号:EP01963156.3

    申请日:2001-08-30

    申请人: AstraZeneca AB

    IPC分类号: A61K9/20

    CPC分类号: A61K9/2054 A61K9/205

    摘要: A pharmaceutical modified release formulation comprising a pharmacologically active substance and a modified water-soluble polysaccharide, which modified water-soluble polysaccharide is obtainable by: a) forming a precipitate of a water-soluble polysaccharide by contacting a solution of the water-soluble polysaccharide with a solvent in which the polysaccharide is poorly soluble or insoluble; or b) milling a water-soluble polysaccharide. The modified water-soluble polysaccharides provide modified release formulations with high tablet hardness. Also claimed are a process for preparing the modified release formulation, and the use of the modified water-soluble polysaccharides as an excipient in a pharmaceutical formulation.

    MODIFIED RELEASE FORMULATION
    5.
    发明公开
    MODIFIED RELEASE FORMULATION 有权
    修改释放制剂

    公开(公告)号:EP1322293A1

    公开(公告)日:2003-07-02

    申请号:EP01963156.3

    申请日:2001-08-30

    申请人: AstraZeneca AB

    IPC分类号: A61K9/20

    CPC分类号: A61K9/2054 A61K9/205

    摘要: A pharmaceutical modified release formulation comprising a pharmacologically active substance and a modified water-soluble polysaccharide, which modified water-soluble polysaccharide is obtainable by: a) forming a precipitate of a water-soluble polysaccharide by contacting a solution of the water-soluble polysaccharide with a solvent in which the polysaccharide is poorly soluble or insoluble; or b) milling a water-soluble polysaccharide. The modified water-soluble polysaccharides provide modified release formulations with high tablet hardness. Also claimed are a process for preparing the modified release formulation, and the use of the modified water-soluble polysaccharides as an excipient in a pharmaceutical formulation.

    摘要翻译: 包含药理学活性物质和改性水溶性多糖的药物改性释放制剂,所述改性水溶性多糖可通过以下获得:a)通过使水溶性多糖的溶液与 其中多糖难溶或不溶的溶剂; 或b)研磨水溶性多糖。 改性的水溶性多糖提供具有高片剂硬度的改良释放制剂。 还要求保护一种制备改性释放制剂的方法,以及改性的水溶性多糖作为药物制剂中的赋形剂的用途。