国产克拉霉素胶囊人体生物利用度

Bioavailability of domestic clarithromycin capsules in normal volunteers

目的:比较国产克拉霉素胶囊与进口克拉霉素片的人体生物利用度.方法:10名健康男性志愿者交叉单剂量po国产克拉霉素胶囊(A)和进口克拉霉素片(B).采用微生物法测定其血药浓度.计算药物动力学参数.结果:A、B两种剂型体内过程经药物动力学程序拟合,符合一空模型,C_(max)分别为(2.45±0.33)和(2.67±0.53)mg/L,t_(max)分别为(1.71±0.44)和(1.77±0.38)h,T(1/2)(ke)分别为(3.47±0.67)和(3.28±0.46)h,AUC分别为(16.84±3.19)和(17.68±2.25)[(mg/L)·h].经统计分析.两种制剂的药物动力学参数均无显著性差异(P>0.05).国产克拉霉素胶囊的相对生物利用度为95.16%.结论:两种制剂体内生物作用等效.

AIM: To compare pharmacokinetics and bioavailability of clarithromycin in 10 healthy male volunteers. METHODS:The clarithromycin concentrations in serum were mea-sured by bioassay after a single crossover oral dose of 500 mg. RESULTS:It was found that the serum concentration time curve of the 2 preparations were fitted to a one-compartment model. The c_(max) were (2.45 ± 0. 33)and (2. 67 ± 0. 53)mg/L,the t_(max) were (1. 71 ± 0. 44)and (1. 77 ± 0. 38)h,the T1/2(ke)were(3. 47 ± 0. 67)and(3. 28 ± 0. 46)h,the AUC were(16. 84 ± 3.19)and(17. 68 ± 2. 25)[(mg/L) · h], CONCLUSION:The pharmacokinetic parameters ob-tained from our statistic studies show no significant difference between 2 products ,P>0. 05. The relative bioavailability of domestic capsules to imported tablets is 95. 16%, so it demon-strates that both preparations are bioequivalent.