新型抗炎药托美汀在大鼠和小鼠体内的处置与代谢研究。II. 尿代谢产物
Studies on disposition and metabolism of tolmetin, a new anti-inflammatory agent, in rats and mice. II. Urinary metabolites.
作者信息
Hashimoto M, Miyazaki H, Nambu K, Fujii T, Arakawa S, Yoshida K, Utsui Y
出版信息
Drug Metab Dispos. 1979 Jan-Feb;7(1):20-3.
A new urinary metabolite of tolmetin was found in rat urine and identified as the hydroxymethyl metabolite (tolmetin-OH), an intermediate in the formation of the known carboxy metabolite (tolmetin-COOH). In rats of two strains, the following percentages of the urinary reactivity of [14Ia1tolmetin were found in 24 hr: unchanged tolmetin-COOH (58--60%), tolmetin-OH (18--24 %), and its conjugate 6--14%. Mouse urine contained the unchanged drug (about 20%), its conjugate and tolmetin-COOH (60%). Similarly to mouse urine, human urine contained negligible amounts of tolmetin-OH.
在大鼠尿液中发现了托美丁的一种新的尿液代谢物，鉴定为羟甲基代谢物（托美丁 - OH），它是已知羧基代谢物（托美丁 - COOH）形成过程中的一种中间体。在两种品系的大鼠中，24小时内[14C]托美丁的尿液反应性百分比如下：未变化的托美丁 - COOH（58 - 60%）、托美丁 - OH（18 - 24%）及其结合物（6 - 14%）。小鼠尿液中含有未变化的药物（约20%）、其结合物和托美丁 - COOH（60%）。与小鼠尿液类似，人类尿液中托美丁 - OH的含量可忽略不计。
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