富马酸比索洛尔片剂人体药代动力学及相对生物利用度

Pharmacokinetics and Relative Bioavailability of Bisoprolol Hemifumarate

目的 比较国产与进口富马酸比索洛尔片剂的人体药代动力学及两药的相对生物利用度。方法 受试者自身交叉口服同等剂量的国产与进口富马酸比索洛尔片剂 ,HPLC内标定量方法测定血药浓度 ,3P87计算机程序处理药代数据。结果 两种片剂的体内过程均符合一级吸收二室模型 ,国产片剂的主要药代动力学参数 T1/ 2α、T1/ 2 β、Cmax、Tmax和AUC0 -36分别为 1.32h、7.42h、49.6 0ng·ml-1、2 .5 4h和 489.49ng·ml-1·h-1;进口片剂的主要药代动力学参数T1/ 2α、T1/ 2 β、Cmax、Tmax和AUC0 -36分别为 1.31h、7.94h、48.5 3ng·ml-1、2 .5 7h和 5 2 0 .82ng·ml-1·h-1。结论 相对生物利用度为 95 .31%。

Aim To study the pharmacokinetics and relative bioavailability of Bisoprolol hemifumarate tablet (BSP) in comparision with Bisoprolol hemifumarate tablet (Concor 5).Methods Crossover self-controlled study was conducted in 8 healthy male volunteers.After a single dose of 15mg (5mg×3) drug was given,the plasma drug concentrations were determined by HPLC.Results The pharmacokinetic parameters of BSP and Concor 5 were C max 49.60 and 48.53ng·ml -1 ;T max 2.54 and 2.57h;AUC 0-36 489.49 and 520.82ng·ml -1 ·h -1 . Two-compartment model with first-order absorption was fitted to the concentration-time profiles of both tablets.Conclusions The relative bioavailability of BSP was 95.31%±9.65%.Both tablets are bioequivalent.