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[35S]-噻唑烷羧酸在大鼠体内的药代动力学与代谢。I. 消除与分布。

Pharmacokinetics and metabolism of [35S]-Thiazolidine carboxylic acid in the rat. I. Elimination and distribution.

作者信息

Harmand M F, Blanquet P

出版信息

Eur J Drug Metab Pharmacokinet. 1982 Oct-Dec;7(4):323-7. doi: 10.1007/BF03189636.

Abstract

The localization and elimination of 35S-Thiazolidine carboxylic acid has been studied in rats following a single oral dose (100 mg/kg) and multiple oral doses (100 mg/kg/day) over 15 days. The compound was rapidly and completely absorbed as evaluated by the time of the maximum plasma 35S-concentration (140 micrograms eq/ml at 30 min) and the amount of radioactivity in the feces (less than 1% of the dose over 48 h). Urinary excretion seems to be the unique route of elimination. There was specific tissue accumulation of drug or metabolite, particularly in liver (29% of the dose at 3 h), pancreas (7% of the dose at 3 h), adrenals (320 micrograms eq/g at 3 h), pituitary and thyroid (230 micrograms eq/g at 3h). Fixation of radioactivity appears significantly higher after chronic treatment than after acute treatment.

摘要

在大鼠单次口服剂量(100毫克/千克)以及连续15天多次口服剂量(100毫克/千克/天)后,对35S - 噻唑烷羧酸的定位与消除情况进行了研究。通过血浆中35S浓度最大值出现的时间(30分钟时为140微克当量/毫升)以及粪便中的放射性量(48小时内少于给药剂量的1%)评估,该化合物吸收迅速且完全。尿液排泄似乎是唯一的消除途径。药物或代谢物存在特定的组织蓄积,特别是在肝脏(给药后3小时为给药剂量的29%)、胰腺(给药后3小时为给药剂量的7%)、肾上腺(给药后3小时为320微克当量/克)、垂体和甲状腺(给药后3小时为230微克当量/克)。慢性治疗后放射性的固定明显高于急性治疗后。

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