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抗锥虫药苄硝唑在人体中的单剂量药代动力学

Single-dose pharmacokinetics of the trypanosomicide benznidazole in man.

作者信息

Raaflaub J, Ziegler W H

出版信息

Arzneimittelforschung. 1979;29(10):1611-4.

PMID:583230
Abstract

The single-dose pharmacokinetics of N-benzyl-2-nitro-1-imidazole acetamide (benznidazole, Radanil) following administration of 1 tablet Radanil (100 mg) was investigated in six healthy volunteers. The absorption of the drug was fairly rapid. Peak plasma levels of 2.2--2.8 microgram/ml were reached after 3--4 h. The log c versus time curves showed little interindividual variation. The shape of the curves indicates that the drug follows the kinetics of a one-compartment model. The elimination half-lives ranged from 10.5 to 13.6 h, with a mean value of 12 h. The relative bioavailability of the compound (oral tablet versus oral solution) was checked in three of the subjects and found to be 91.7% on an average.

摘要

在6名健康志愿者中研究了服用1片硝呋替莫(100毫克)后N-苄基-2-硝基-1-咪唑乙酰胺(硝呋替莫,拉达尼尔)的单剂量药代动力学。药物吸收相当迅速。3-4小时后血浆峰值水平达到2.2-2.8微克/毫升。对数浓度与时间曲线显示个体间差异很小。曲线形状表明该药物符合一室模型动力学。消除半衰期为10.5至13.6小时,平均值为12小时。在3名受试者中检查了该化合物(口服片剂与口服溶液)的相对生物利用度,平均为91.7%。

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