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    • 9. 发明授权
    • Drug complex
    • 药物复合体
    • US06458347B1
    • 2002-10-01
    • US09172085
    • 1998-10-14
    • Shuichi SugawaraMasahiro KajikiHiroshi KuriyamaNobuya Kitaguchi
    • Shuichi SugawaraMasahiro KajikiHiroshi KuriyamaNobuya Kitaguchi
    • A61K3177
    • A61K47/61A61K47/60
    • Disclosed is a drug complex of a drug having a hydroxyl group, which is capable of controlling the rate of the release of the drug therefrom in blood, the drug complex being represented by the following formula (1): A—B—C  (1) wherein A represents at least one carrier selected from the group consisting of saccharides each having a carboxyl group, polyethylene glycols each having a carboxyl group, aliphatic carboxylic acids each having a carboxyl group, and derivatives thereof each having a carboxyl group; B represents at least one spacer comprised of a compound having a amino group and a carboxyl group; C represents at least one drug having a hydroxyl group, wherein the carrier A is bonded to the spacer B through an amide bond formed between the carboxyl group of the carrier A and the amino group of the spacer B; and the spacer B is bonded to the drug C through an ester bond formed between the carboxyl group of the spacer B and the hydroxyl group of the drug C.
    • 公开了具有羟基的药物的药物复合物,其能够控制药物在血液中的释放速率,药物复合物由下式(1)表示:其中A表示至少一种载体 选自具有羧基的糖类,各自具有羧基的聚乙二醇,各自具有羧基的脂肪族羧酸,以及各自具有羧基的衍生物; B表示至少一个由具有氨基和羧基的化合物组成的间隔物; C表示至少一种具有羟基的药物,其中载体A通过形成在载体A的羧基和间隔基B的氨基之间的酰胺键与间隔基B结合; 并且间隔物B通过在间隔物B的羧基和药物C的羟基之间形成的酯键与药物C结合。