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[长春西汀在大鼠体内的药代动力学及处置情况]

[Pharmacokinetics and disposition of vinpocetine in rats].

作者信息

Yao J H, Su C Y, Chu X Y

机构信息

Department of Pharmacology, Dalian Medical College.

出版信息

Yao Xue Xue Bao. 1994;29(2):81-5.

PMID:8042515
Abstract

A reverse-phase HPLC method for determination of vinpocetine in biological samples was developed. The method was simple, highly specific and accurate. After i.v. administration of vinpocetine in rats, the plasma concentration-time curves of vinpocetine was found to be fitted to a two-compartment open model. Dosing 5 and 10 mg.kg-1 vinpocetine in rats, the elimination of the drug from plasma accorded with linear kinetics and the elimination half-lives were shown to be 1.76 +/- 0.27 h. The volumes of distribution were 7.30 +/- 0.49 L.kg-1 (5 mg.kg-1) and 6.07 +/- 0.67 L.kg-1 (10 mg.kg-1) respectively. The drug levels were high in the lung, spleen, liver and kidney, moderate in brain, fat and testis and low in heart, muscle and blood. Our results demonstrate that vinpocetine was eliminated in a rapid rate and distributed widely in the body. The bioavailability of vinpocetine after ig administration was 54.54% in rats. A small amount of unchanged vinpocetine was detected in urine, feces and bile after i.v. and ig administration.

摘要

建立了一种反相高效液相色谱法用于测定生物样品中的长春西汀。该方法简便、特异性高且准确。大鼠静脉注射长春西汀后,发现长春西汀的血浆浓度-时间曲线符合二室开放模型。给大鼠分别静脉注射5和10 mg·kg-1长春西汀后,药物从血浆中的消除符合线性动力学,消除半衰期分别为1.76±0.27小时。分布容积分别为7.30±0.49 L·kg-1(5 mg·kg-1)和6.07±0.67 L·kg-1(10 mg·kg-1)。药物在肺、脾、肝和肾中的含量较高,在脑、脂肪和睾丸中的含量中等,在心脏、肌肉和血液中的含量较低。我们的结果表明长春西汀消除速度快且在体内分布广泛。大鼠灌胃给药后长春西汀的生物利用度为54.54%。静脉注射和灌胃给药后,在尿液、粪便和胆汁中检测到少量未变化的长春西汀。

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