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尼莫地平在中国急性蛛网膜下腔出血患者中的药代动力学研究。

Investigation of nimodipine pharmacokinetics in Chinese patients with acute subarachnoid haemorrhage.

作者信息

Kumana C R, Kou M, Yu Y L, Fong K Y, Fung C F, Chang C M, Mück W, Lauder I J

机构信息

Department of Medicine, University of Hong Kong.

出版信息

Eur J Clin Pharmacol. 1993;45(4):363-6. doi: 10.1007/BF00265956.

Abstract

Nimodipine pharmacokinetics was investigated in 12 Chinese patients with acute subarachnoid haemorrhage receiving an IV infusion of 1.6 or 2 mg/h (based on estimated body weight) for 10 days. Peripheral venous blood samples were collected for up to 4 days and plasma nimodipine was assayed by GC/ECD. The mean value was taken as the steady state concentration (Css) and Clearance (CL) (hourly dose/Css) was calculated. Eight survivors were given oral nimodipine (60 or 90 mg) every 6h (based on body weight), blood was sampled over 6 h and the plasma nimodipine level determined. The values for Css, CL and CL.kg-1 were 33.5 micrograms.l-1, 58 l.h-1 and 1.0 l.h-1 x kg-1 respectively; in survivors receiving the drug orally, bioavailability of the 30 mg tablet was 9%. In one very sick patient given crushed tablets by naso-gastric tube, the AUC was very low; in vitro studies indicated that adsorption of nimodipine by the tubing was unlikely to have been the cause. The pharmacokinetic findings in Chinese patients are comparable to previously reported values in Caucasians.

摘要

对12例急性蛛网膜下腔出血的中国患者进行了尼莫地平的药代动力学研究,这些患者接受静脉输注1.6或2mg/h(根据估计体重),持续10天。采集外周静脉血样长达4天,采用气相色谱/电子捕获检测法测定血浆尼莫地平。取平均值作为稳态浓度(Css),并计算清除率(CL)(每小时剂量/Css)。8名幸存者每6小时口服尼莫地平(60或90mg)(根据体重),在6小时内采集血样并测定血浆尼莫地平水平。Css、CL和CL.kg-1的值分别为33.5μg.l-1、58 l.h-1和1.0 l.h-1 x kg-1;在口服该药的幸存者中,30mg片剂的生物利用度为9%。在一名通过鼻胃管给予碾碎片剂的重病患者中,曲线下面积(AUC)非常低;体外研究表明,尼莫地平不太可能被管道吸附。中国患者的药代动力学研究结果与先前报道的高加索人的值相当。

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