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[对甲状腺素处理大鼠中对乙酰氨基酚的首过代谢]

[First-pass metabolism of acetaminophen in thyroxine treated rats].

作者信息

Zhu C Y, Hirate J, Kanamoto I, Nakagawa T, Adachi I, Horikoshi I, Bhargava V O

机构信息

Department of Hospital Pharmacy, Toyama Medical and Pharmaceutical University, Japan.

出版信息

Yakugaku Zasshi. 1991 Jan;111(1):40-4. doi: 10.1248/yakushi1947.111.1_40.

Abstract

The study on the first-pass metabolism of acetaminophen was carried out in normal and thyroxine-treated rats, administered 30 mg/kg by three routes of intravenous, intraperitoneal, and oral one. Unconjugated acetaminophen and two major metabolites, glucuronide and sulfate in the plasma and urine were then measured 5 and 24 h after the administration, respectively. It was found that there was no difference in total percentage of excreted amount, independent of the routes for administration, between normal and thyroxine-treated rats. This fact shows that acetaminophen is absorbed completely from the gastrointestinal tract. However, it was also found that the extraction ratio of gastrointestinal tract in thyroxine-treated rats became smaller, and that the volume of distribution and total body clearance became larger than those in normal rats. The first-pass metabolism of acetaminophen was found to be influenced by the continuous administration of thyroxine.

摘要

对正常大鼠和甲状腺素处理的大鼠进行了对乙酰氨基酚首过代谢的研究,通过静脉内、腹腔内和口服三种途径给予30mg/kg的剂量。然后分别在给药后5小时和24小时测量血浆和尿液中未结合的对乙酰氨基酚以及两种主要代谢物葡萄糖醛酸苷和硫酸盐。结果发现,正常大鼠和甲状腺素处理的大鼠之间,排泄总量的百分比没有差异,与给药途径无关。这一事实表明对乙酰氨基酚从胃肠道完全吸收。然而,还发现甲状腺素处理的大鼠胃肠道的提取率变小,分布容积和全身清除率比正常大鼠大。发现甲状腺素的持续给药会影响对乙酰氨基酚的首过代谢。

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