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1. 发明申请

US20080193509A1 Liposome Preparation Containing Slightly Water-Soluble Camptothecin 审中-公开
标题翻译：含有轻微水溶性喜树碱的脂质体制备
公开(公告)号：US20080193509A1
公开(公告)日：2008-08-14
申请号：US11629869
申请日：2005-06-17
申请人： Keisuke Yoshino , Shigenori Nozawa , Yoshitaka Ogata , Yasuo Kurosaki , Seigo Sawda , Ikuo Kato , Takeshi Matsuzaki
发明人： Keisuke Yoshino , Shigenori Nozawa , Yoshitaka Ogata , Yasuo Kurosaki , Seigo Sawda , Ikuo Kato , Takeshi Matsuzaki
IPC分类号： A61K9/127 , A61K31/4375
CPC分类号： A61K9/1272 , A61K31/4745
摘要： The present invention aims at providing a slightly water-soluble camptothecin liposome preparation with an excellent retention in blood for a drug, which can stably hold a slightly water-soluble camptothecin compound for a long period of time, whereby hydrolysis of an α-hydroxylactone ring in blood is suppressed and the slightly water-soluble camptothecin compound is kept in a structure in which the ring is not opened and which makes the compound effective as an antitumor-active drug, and, moreover, the liability of the drug to leave a liposome is advantageously reduced, so that it is possible to maintain the drug concentration in plasma for a long period of time after administration. This object is achieved by the liposome preparation as described in the specification. The liposome preparation according to the present invention includes a liposome preparation including as lipid components for forming a membrane a phospholipid and a fatty acid, and containing as a drug a lightly water-soluble camptothecin compound.
摘要翻译：本发明的目的在于提供一种在血液中具有优异的药物保留性的轻微水溶性喜树碱脂质体制剂，其能够长时间稳定地保持轻微的水溶性喜树碱化合物，从而水解α-羟基内酯环在血液中被抑制，轻微的水溶性喜树碱化合物保持在不打开环的结构中，并且使得化合物作为抗肿瘤活性药物有效，此外，药物离开脂质体的责任有利地减少，使得可以在施用后长时间维持血浆中的药物浓度。该目的通过如说明书中所述的脂质体制备来实现。根据本发明的脂质体制剂包括脂质体制剂，其包含作为形成磷脂和脂肪酸的膜的脂质成分，并且作为药物含有轻度水溶性的喜树碱化合物。

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