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[中离子型二脱氢-4-甲基-5-苯基-1,3,4-噻二唑烷-2-硫酮(LU 2443)的生物转化与药代动力学。大鼠药代动力学研究]

[Biotransformation and pharmacokinetics of mesionic didehydro-4-methyl-5-phenyl-1,3,4-thiadiazolidine-2-thione (LU 2443). Studies on the pharmacokinetics in rats].

作者信息

Neidlein R, Eder T

出版信息

Arzneimittelforschung. 1982;32(11):1447-52.

PMID:6891252
Abstract

After p.o. application in rats the pharmacokinetic properties of the mesionic dihydro-4-methyl-5-phenyl-1,3,4-thiadiazolidine-2-thione (LU 2443) were examined. The compound is extensively absorbed, in the maximum 18% are eliminated unabsorbed. The half-time of the activity in plasma is 13.17 h, the highest concentration in plasma after p.o. application as a solution of polyethyleneglycol is reached after 5.09 h. The elimination is mainly renal--namely 61.9%, 28.7% are eliminated with the faeces. After 96 h 90.6% of the applicated activity was eliminated. The distribution of LU 2443 was in the whole organism; entrance of the compound into liquor was proven. By radiography of the total animal a transient accumulation of LU 2443 and its metabolites in liver and kidney was determined; besides, a considerable concentration of activity in the suprarenal medulla was found.

摘要

在大鼠口服给药后,对离子型二氢-4-甲基-5-苯基-1,3,4-噻二唑烷-2-硫酮(LU 2443)的药代动力学特性进行了研究。该化合物吸收广泛,最大有18%未被吸收而消除。血浆中活性的半衰期为13.17小时,口服聚乙二醇溶液后,5.09小时达到血浆中最高浓度。消除主要通过肾脏,即61.9%,28.7%随粪便排出。96小时后,90.6%的给药活性被消除。LU 2443在整个机体中分布,已证实该化合物进入脑脊液。通过对整个动物的放射成像,确定了LU 2443及其代谢产物在肝脏和肾脏中的短暂蓄积;此外,还发现肾上腺髓质中有相当浓度的活性。

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