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首页> 外文期刊>Journal of pharmaceutical sciences. >Pharmacokinetics of amitriptyline and one of its metabolites, nortriptyline, in rats: little contribution of considerable hepatic first-pass effect to low bioavailability of amitriptyline due to great intestinal first-pass effect.
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Pharmacokinetics of amitriptyline and one of its metabolites, nortriptyline, in rats: little contribution of considerable hepatic first-pass effect to low bioavailability of amitriptyline due to great intestinal first-pass effect.

机译：阿米替林及其代谢物之一去甲替林的药代动力学在大鼠中：由于大肠的首过效应，肝首过效应对阿米替林的低生物利用度的贡献很小。

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摘要

Pharmacokinetics of amitriptyline and nortriptyline were evaluated after intravenous (2.5-10 mg/kg) and oral (10-100 mg/kg) administration of amitriptyline to rats. The hepatic, gastric, and intestinal first-pass effects of amitriptyline were also measured at a dose of 10 mg/kg. The areas under the plasma concentration-time curve (AUCs) of amitriptyline were dose-proportional following both intravenous and oral administration. After oral administration of amitriptyline, approximately 1.50% of the dose was not absorbed, the extent of absolute oral bioavalability (F) was approximately 6.30%, and the hepatic and intestinal first-pass effects of amitriptyline were approximately 9% and 87% of the oral dose, respectively. Although the hepatic first-pass effect was 78.9% after absorption into the portal vein, the value was only 9% of the oral dose due to considerable intestinal first-pass effect in rats. The low F of amitriptyline in rats was primarily attributable to considerable intestinal first-pass effect. This study proves the little contribution of considerable hepatic first-pass effect to low F of amitriptyline due to great intestinal first-pass effect in rats. The lower F value of amitriptyline in rats than that in humans (46 +/- 48%) was due to grater metabolism of amitriptyline in rats' liver and/or small intestine.
机译：在对大鼠静脉内（2.5-10 mg / kg）和口服（10-100 mg / kg）施用阿米替林后，评估了阿米替林和去甲替林的药代动力学。阿米替林的肝，胃和肠道首过效应也以10 mg / kg的剂量进行了测量。静脉和口服给药后，阿米替林的血浆浓度-时间曲线下面积均与剂量成正比。口服阿米替林后，约1.50％的剂量未被吸收，绝对口服生物利用度（F）约为6.30％，阿米替林对肝脏和肠道的首过效应分别约为阿米替林的9％和87％。口服剂量分别。尽管吸收到门静脉后肝的首过效应为78.9％，但由于大鼠的肠首过效应相当大，该值仅为口服剂量的9％。大鼠阿米替林的低F主要归因于可观的肠道首过效应。这项研究证明，由于大鼠的大肠首过效应，肝首过效应对阿米替林低F的贡献很小。大鼠中阿米替林的F值低于人的F值（46 +/- 48％），这是由于阿米替林在大鼠肝脏和/或小肠中的碎屑代谢。

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