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Bile acid containing prodrugs with enhanced bioavailability

机译：含胆汁酸的前药具有更高的生物利用度

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摘要

Many compounds have poor bioavailability or variable bioavailability because of poor absorption of the compound in the small intestine. Conjugation of the compound with bile acid to form a prodrug will increase the bioavailibility of the compound and/or reduce the bioavailability variability of the compound because of the active transport of the prodrug by the intestinal bile acid transporter and because of increased lipophilic nature of the prodrug. A linker group can be used between the bile acid and the compound. One example of a bile acid containing prodrug is acyclovir valylchenodeoxycholate, where valine is the linker group. Another example of this prodrug is atenolol cholic acid amide.

机译：由于化合物在小肠中吸收不良，因此许多化合物的生物利用度较差或生物利用度不均。化合物与胆汁酸结合形成前药会增加化合物的生物利用度和/或降低化合物的生物利用度变异性，这是由于前药通过肠胆汁酸转运蛋白的主动转运以及由于其亲脂性的增加所致。前药。可以在胆汁酸和化合物之间使用连接基团。含有胆汁酸的前药的一个例子是阿昔洛韦缬氨酰去氧胆酸，其中缬氨酸是连接基团。该前药的另一个实例是阿替洛尔胆酸酰胺。

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公开/公告号AU2001253226B2

专利类型
公开/公告日2006-06-08

原文格式PDF
申请/专利权人 UNIVERSITY OF MARYLAND BALTIMORE;
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申请/专利号AU20010253226
发明设计人 KIMBERLEY A. LENTZ;ANDREW COOP;JAMES E. POLLI;DEAN Y. MAEDA;
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申请日2001-04-06
分类号A61K35/50;A61K47/48;A61K;A61K31/165;A61K31/522;A61K31/575;A61K31/58;A61K39/395;A61K39/40;A61K39/42;A61K39/44;A61P9/04;A61P31/12;A61P43;C07J9;C07J41;C07J43;
国家 AU
入库时间 2022-08-21 21:34:42

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