摘要
本文研究了12名男性健康志愿者单剂口服国产和进口盐酸索他洛尔片剂160mg的药代动力学和相对生物利用度。按照随机、交叉试验设计,采集服药后0.5,1.0,1.5,2,3,4,6,8,12,24,36,48h的血样本。HPLC方法测定索他洛尔的血药浓度。两种制剂的药-时曲线符合口服吸收有滞后时间的二房室模型及一级动力学吸收、消除过程。国产索他洛尔的主要药代动力学参数:Cmax1.45±0.36mg/l,Tpeak2.5±0.98h,T1/2β9.67±1.67h,AUC0-t14.92±2.85mg·h·L-1。国产索他洛尔相对于进口制剂的生物利用度为99.7±17.8%,国产索他洛尔与进口制剂生物等效。
The pharmacokinetics and relative bioavailability of domestic sotalol tablets were studied in 12 healthy male volunteers. A single oral dose of 160 mg of domestic or imported sotalol (test and reference preparation) was given according to a randomized 2-way cross-over design, blood samples were withdrawn up to 48 hours post administration, and plasma concentrations of sotalol were assayed by a high performance liquid chromatography ( HPLC ) method. The concentration-time curves of two preparations fitted to a two-compartment model with first order absorption and elimination. The main pharmacokinetic parameters of the test preparation were as follows: Cmax 1.45 ±0.36 mg·L-1 , Tpeak 2.50±0.98 h, T1/2β 9.67±1.67 h, AUC0-t 14.92 ±2.85 mg·h·L-1. The pharmacokinetics and relative bioavailability data obtained in the study furnished definite proof of bioequivalence of both domestic and imported sotalol tablets.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
1998年第1期40-43,共4页
The Chinese Journal of Clinical Pharmacology