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佐美酸的血浆蛋白结合率。

Plasma protein binding of zomepirac sodium.

作者信息

O'Neill P J

出版信息

J Pharm Sci. 1981 Jul;70(7):818-9. doi: 10.1002/jps.2600700733.

Abstract

The plasma protein binding of zomepirac, a new nonnarcotic analgesic, was studied using equilibrium dialysis. Experiments were performed using human plasma and plasma from mice, rats, and rhesus monkeys, all species of pharmacological or toxicological interest. At concentrations approximating those achieved in vivo, the binding was fairly constant at 98-99% in all species except the rhesus monkey, where binding was decreased from 98 to approximately 96% at higher concentrations (greater then 50 microgram/ml). Zomepirac (10 microgram/ml) did not appear to displace or to be displaced by warfarin (10 microgram/ml) caused a concentration-dependent decrease in zomepirac (10 microgram/ml) binding. Zomepirac did not affect salicylate binding.

摘要

采用平衡透析法研究了新型非麻醉性镇痛药佐美酸的血浆蛋白结合情况。实验使用了人血浆以及小鼠、大鼠和恒河猴的血浆,这些都是具有药理学或毒理学研究价值的物种。在接近体内所能达到的浓度下,除恒河猴外,所有物种的结合率相当恒定,为98% - 99%,在恒河猴中,较高浓度(大于50微克/毫升)时结合率从98%降至约96%。佐美酸(10微克/毫升)似乎不会被华法林(10微克/毫升)置换,也不会置换华法林,华法林会导致佐美酸(10微克/毫升)的结合呈浓度依赖性降低。佐美酸不影响水杨酸盐的结合。

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