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    Method for producing liposomal formulations of active ingredients
    9.
    发明申请
    Method for producing liposomal formulations of active ingredients 审中-公开
    生产活性成分脂质体制剂的方法

    公开(公告)号：US20050031679A1

    公开(公告)日：2005-02-10

    申请号：US10937556

    申请日：2004-09-09

    申请人： Clemens Unger ,  Ulrich Massing ,  Regina Moog

    发明人： Clemens Unger ,  Ulrich Massing ,  Regina Moog

    IPC分类号： A61K9/127 ,  A61K31/475 ,  A61K33/24

    CPC分类号： A61K31/704 ,  A61K9/1278 ,  A61K31/475 ,  A61K31/7048 ,  A61K31/7068 ,  A61K33/24

    摘要： The invention relates to a method for producing liposomes which comprise as active ingredient at least one physiologically active or/and diagnostic compound, by production of a mixture of membrane-forming amphiphiles, dispersion of the mixture in water and high pressure homogenization of the dispersion until the liposomes are formed, wherein (a) the mixture is adjusted to result in a liposome preparation containing at least 20% by weight lipids, (b) the active ingredient is added to this liposome preparation and (c) the active ingredient-containing mixture is incubated with mechanical agitation until at least 10% of the liposomes have a content of the active ingredient, the temperature being controlled so that negligible phospholipid hydrolysis occurs, but diffusion is increased. The invention also relates to the liposome preparation produced by this method and to the use of this liposome preparation as diagnostic or therapeutic composition, which, where appropriate, contains further excipients, carriers or/and stabilizers.

    摘要翻译： 本发明涉及一种生产脂质体的方法，其包括作为活性成分的至少一种生理活性或/和诊断化合物，通过生产成膜两亲物的混合物，混合物在水中的分散和高分散分散体直到 形成脂质体，其中（a）调节混合物以产生含有至少20重量％脂质的脂质体制剂，（b）将活性成分加入到该脂质体制剂中，和（c）含活性成分的混合物 与机械搅拌一起孵育直到至少10％的脂质体具有活性成分的含量，控制温度使得发生可忽略不计的磷脂水解，但扩散增加。 本发明还涉及通过该方法制备的脂质体制剂以及该脂质体制剂作为诊断或治疗组合物的用途，其在适当时含有其它赋形剂，载体或/和稳定剂。