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法莫替丁在10名中国健康志愿者体内的药代动力学和生物利用度

Pharmacokinetics and bioavailability of famotidine in 10 Chinese healthy volunteers.

作者信息

Gao S, Liu G L, Wang S X, Gao X H

机构信息

Department of Clinical Pharmacology, Changhai Hospital, China.

出版信息

Zhongguo Yao Li Xue Bao. 1991 May;12(3):195-8.

PMID:1781278
Abstract

The pharmacokinetics and bioavailability of famotidine were investigated by HPLC method in 10 Chinese healthy volunteers. Data obtained from HPLC were analysed automatically using a MCPKP program on microcomputer. Linear pharmacokinetics were observed following either iv or po administration. After 20 mg iv, plasma levels declined biexponentially with an initial T1/2 of 0.3 +/- 0.2 h and terminal T1/2 of 3.5 +/- 0.8 h. The plasma elimination T1/2 following po administration were 3.4 +/- 0.7 h and 3.5 +/- 0.5 h for capsules and tablets respectively. Oral absorption was incomplete. The absolute bioavailabilities were 38 +/- 10% for capsules and 43 +/- 11% for tablets. Renal excretion was the major route of elimination. About 72% of the dose were recovered as unchanged famotidine in urine. Mean renal and plasma clearance were 416 and 541 ml.min-1 respectively.

摘要

采用高效液相色谱法对10名中国健康志愿者进行了法莫替丁的药代动力学和生物利用度研究。用微机上的MCPKP程序自动分析高效液相色谱法获得的数据。静脉注射或口服给药后均观察到线性药代动力学。静脉注射20mg后,血浆浓度呈双指数下降,初始半衰期为0.3±0.2小时,终末半衰期为3.5±0.8小时。口服给药后,胶囊和片剂的血浆消除半衰期分别为3.4±0.7小时和3.5±0.5小时。口服吸收不完全。胶囊和片剂的绝对生物利用度分别为38±10%和43±11%。肾排泄是主要的消除途径。约72%的剂量以原形法莫替丁的形式在尿液中回收。平均肾清除率和血浆清除率分别为416和541ml·min-1。

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