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    • 7. 发明公开
    • LIPOSOME WITH INCREASED RETENTION VOLUME
    • LIPOSOM MITERHÖHTEMRETENTIONSVOLUMEN
    • EP0804925A1
    • 1997-11-05
    • EP95913349.7
    • 1995-03-27
    • DAIICHI PHARMACEUTICAL CO., LTD.
    • KIKUCHI, Hiroshi, Daiichi Pharmaceutical Co., Ltd.YACHI, Kiyoto, Daiichi Pharmaceutical Co., Ltd.
    • A61K9/127A61K47/24B01J13/02
    • A61K9/127
    • The present invention provides liposome preparations capable of efficiently holding water soluble substance particularly non-electrolytic water soluble substances.
      Liposomes and suspensions thereof comprising multilamellar liposomes characterized in that the liposome membrane is formed from a neutral phospholipid comprising a substantially saturated fatty acid residue a charged phospholipid comprising a substantially saturated fatty acid residue, ratio of said neutral phospholipid and charged phospholipid is 200:1 to 3:1, weighted average particle size of the liposome is 50 nm to 3,000 nm, and an encapsulation capacity of the liposome (internal aqueous phase (volume)/lipids (weight)) is at least 5 mℓ/g.
      The present liposome preparation can encapsulate an aqueous solution of a non-electrolytic water soluble substances with an encapsulation capacity (internal aqueous phase/lipids) of at least 5 mℓ/g.
    • 本发明提供能够有效保持水溶性物质,特别是非电解水溶性物质的脂质体制剂。 包含多层脂质体的脂质体和悬浮液的特征在于脂质体膜由包含基本上饱和的脂肪酸残基的中性磷脂形成,包含基本上饱和的脂肪酸残基的带电磷脂,所述中性磷脂和带电磷脂的比例为200:1至 如图3:1所示,脂质体的加权平均粒径为50nm〜3000nm,脂质体(内部水相(体积)/脂质(重量))的包封容量为5ml / g以上。 本脂质体制剂可以包封具有至少5m l / g的包封能力(内部水相/脂质)的非电解水溶性物质的水溶液。