国产头孢布烯胶囊与其进口制剂人体生物等效性比较

目的:比较国产头孢布烯胶囊与进口头孢布烯胶囊的人体生物等效性.方法:20名健康志愿者随机交叉单剂量口服200 mg国产和进口头孢布烯2种胶囊,采用高效液相色谱法测定血浆中药物含量,对药动学参数进行统计分析,确定是否生物等效.结果:头孢布烯胶囊体内过程符合口服给药二室模型,国产及进口制剂中头孢布烯的主要药代动力学参数分别为达峰时间(2.66±0.37)和(2.72±0.34)h,最大血药浓度(20.42±3.41)和(19.93±3.29)mg/L; 浓度-时间曲线下面积(AUC0～∞)(104.86±17.26)和(101.68±17.44)mg·-1·h-1·L-1.用梯形法计算所得的AUC0～t分别为(103.33±20.82)和(101.68±17.44)mg·h-1·L-1,由AUC0～t计算国产头孢布烯胶囊的相对生物利用度为(103.4±21.0)%.结论:国产头孢布烯胶囊与进口头孢布烯胶囊具有生物等效性.

Comparison of domestic and imported ceftibuten capsules in healthy volunteers

Objective:To compare the bioequivalence of domestic and imported ceftibuten capsules.Methods:A dose of 200 mg domestic or imported ceftibuten capsules was randomly given to 20 healthy volunteers in two-way cross-over design.Plasma concentrations of ceftibuten was determined by high performance liquid chromatography(HPLC) method.The pharmacokinetic parameters were calculated with the aid of DAS 2.0 pharmacokinetics software.The bioequivalence of the domestic and imported capsules were calculated by analysis of variance and two one side t-test.Results:The concentration-time curves of the two preparations were fitted to a two-compartment model.The main pharmacokinetic parameters of domestic or imported ceftibuten capsules were as follows:Tmax/h(2.66±0.37 vs 2.72±0.34);Cmax/mg/L(20.42±3.41 vs 19.93±3.29);AUC0-∞(104.86±17.26)and(101.68±17.44)mg·h-1·L-1;AUC0-t(103.33±20.82)and(101.68±17.44)mg·h-1·L-1,respectively.The relative bioavailability of domestic drug was(103.4±21.0)%.Conclusions:The domestic and imported capsules are bioequivalent.