公开(公告)号：US20090041835A1

公开(公告)日：2009-02-12

申请号：US12139702

申请日：2008-06-16

申请人： Yusuki Kato ,  Masahiro Yamauchi ,  Hiroko Kusano ,  Atsushi Ishihara

发明人： Yusuki Kato ,  Masahiro Yamauchi ,  Hiroko Kusano ,  Atsushi Ishihara

IPC分类号： A61K9/127 ,  A61K31/407

CPC分类号： A61K31/55 ,  A61K9/127

摘要： The present invention provides a method of inhibiting the leakage of a drug encapsulated in liposomes, which comprises satisfying at least two requirements selected from the group consisting of the following three requirements: using at least two lipid bilayers of the liposomes, controlling the average particle size of the liposomes to 120 nm or more, and using lipid having a phase transition temperature higher than in vivo temperature as lipid constituting the liposomes. Also, the present invention provides a liposome preparation which is stable in vivo and satisfies at least two requirements selected from the group consisting of the following three requirements: the number of lipid bilayers of the liposomes is at least two, the liposomes have an average particle size of 120 nm or more, and lipid constituting the liposomes has a phase transition temperature higher than in vivo temperature.

摘要翻译： 本发明提供一种抑制包封在脂质体中的药物的泄漏的方法，其包括满足选自以下三个要求的至少两个要求：使用脂质体的至少两个脂质双层，控制平均粒径 的脂质体达到120nm以上，并且使用具有比体内温度高的相变温度的脂质作为构成脂质体的脂质。 另外，本发明提供脂质体制剂，其在体内稳定且满足选自以下三个要求的至少两个要求：脂质体的脂质双层数至少为2个，脂质体具有平均粒子 大小为120nm以上，构成脂质体的脂质的相转变温度高于体内温度。