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[大鼠体内硝西泮及其代谢产物的胆汁排泄]

[Biliary excretion of nitrazepam and its metabolites in rats].

作者信息

Golovenko N Ia, Karaseva T L

出版信息

Farmakol Toksikol. 1978 Jan-Feb;41(1):17-9.

PMID:624385
Abstract

A single intravenous administration of nitrasepam (10 mg/kg) resulted in its excretion as free and conjugated metabolites in the bile of albino rats. The initial compounds, amino- and acetamido derivatives were deteced among free metabolits. Conjugated forms were recovered as N-glucoronides (5-nitro-2-aminobenzophenon and amine) and as O-glucoronides (C3-hydroxylated derivatives of nitrasepam and of acetamide). The presence of a considerable amount of nitrasepam and of its metabolites in the rats' bile is suggestive of their enterohepatic circulation.

摘要

对白化病大鼠单次静脉注射硝西泮(10毫克/千克)后,其以游离和结合代谢物的形式经胆汁排出。在游离代谢物中检测到了初始化合物、氨基和乙酰氨基衍生物。结合形式以N-葡萄糖醛酸苷(5-硝基-2-氨基二苯甲酮和胺)和O-葡萄糖醛酸苷(硝西泮和乙酰胺的C3-羟基化衍生物)的形式回收。大鼠胆汁中存在大量硝西泮及其代谢物,提示其存在肠肝循环。

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