摘要
目的：了解健康志愿者口服阿克他利（Ａｃｔａｒｉｔ，Ａｃｔａ）的药代动力学；以进口阿克他利为对照求出相对生物利用度。方法：在２０例健康志愿者中选择１２名健康志愿者（男８例，女４例）采用分层随机方法分为二组，每组６人，分别口服国产阿克他利片剂２００ｍｇ，３００ｍｇ，进行人体药代动力学试验。选择８名男性健康志愿者，随机分为二组，采用双交叉试验设计，分别口服４００ｍｇ进口或国产阿克他利片，进行人体药代动力学试验并求出相对生物利用度。结果：口服 ２００ ｍｇ、３００ｍｇ国产阿克他利的主要药代动力学参数分别为：ｔ＿（１／２ｋｅ）１．０３±０．２２，０．９１±０．０５ｈ；ｔ＿（ｍａｘ）１．０８±０．２０，１．０８±０．２０ｈ；Ｃ＿（ｍａｘ）３．８７±１．００，５．３９±１．０３ｍｇ·Ｌ～（－１）；ＡＣＵ＿（０－６）５．９１±０．７６，８．０２± ０．８９ｍｇ上·Ｌ～（－１）。口服４００ｍｇ国产和进口阿克他利的主要药代动力学参数为别为ｔ＿（１／２ｋｅ）０·９４±０．０３，０．９４±０．０４ｈ；ｔ＿（ｍａｘ）１．１３ ± ０．２３，１．１３±０．２３ｈ；Ｃ＿（ｍａｘ）７·６７ ±１．６０，７·８０ ±１·７ｌｍｇ·Ｌ～（－１）；
OBJECTIVE: To study pharmacokinetics and relative bioavailability following oral administration of actarit in healthy volunteers. METHODS: In 20 healthy volunteers, 12 healthy volunteers (male 8, female 4) who were stratifed randomly into two groups, took domestic actarit 200mg, 300 mg, respectively. In two-crossed test design, 8 male healthy volunteers, who were randomly divided into two groups, took domestic and imported actarit(400mg) respectively. The imported actarit was selected as a standard control. The relative bioavailability of domestic actarit was analyzed in healthy volunteers. RESULTS: The main pharmacokinetic parameters following oral administration of domestic actarit (200mg, 300mg) were t_(1/2ke) 1.03± 0.22,0.9 1 ±0.05h;t_(max) 1.08 ±0.20,1.08 ±0.20h; C_(max) 3.87 ±1.00,5.39 ±1.03mg.L_(-1)ACU_(0-6) 5.91 ±0.76,8.02 ±0.89mg.h.L^(-1) The main pharmacokinetic parameters after oral administration of domestic and imported actarit (400mg) were t_(1.2ke),± 0.94 ±0.03,0.94 ±0.04h;t_(max) 1.13 ±0.23,1.13±0.23h;C_(max) 7.67 ±1.60,7.80±1.7lmg.L^(-1)AUC_(0-6) 11.84±1 .89,11.92±2.0lmg.h.L^(-1) CONCLUSION: The concentration-time curves of domestic actarit conformed to one-compartmental model of the first-order absorption in healthy volunteers. The relative bioavailability of domestic actarit was 99.5±1.59%, and its 90% confident limit was 100.4~101.4%.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
2002年第1期49-52,共4页
The Chinese Journal of Clinical Pharmacology
