国产阿莫西林/克拉维酸片人体生物等效性研究

Bioequivalence of amoxicillin and clavulanic acid tablets in healthy volunteers

目的 :以进口阿莫西林 /克拉维酸片为对照 ,考察国产制剂的人体生物等效性。方法 :10名健康受试者随机交叉单剂量口服 2种制剂 (阿莫西林 2 5 0mg ,克拉维酸钾 12 5mg)后 ,采用微生物法测定血浆中药物浓度。结果 :血药浓度数据经 3P97拟合 ,两者的体内过程皆符合血管外口服给药一室模型 ,采用梯形法计算的阿莫西林AUC0～t分别为 (12 .89± 1.0 3)和 (13.5 4± 0 .5 9) (mg·h) /L ,实测Cmax分别为 (5 .17± 0 .45 )和 (5 .2 5± 0 .46 )mg/L ;Tmax分别为 (1.0 5± 0 .16 )和 (1.0 8± 0 .2 3)h ,t1/ 2 分别为 (1.16± 0 .17)和 (1.37± 0 .2 3)h。克拉维酸钾的AUC0～t分别为 (8.2 5± 0 .92 )和 (8.18± 0 .5 1) (mg·h) /L ,实测Cmax分别为 (3 .94± 0 .5 2 )和 (4 .10± 0 .35 )mg/L ;Tmax分别为(1.10± 0 .2 1)和 (1.0 3± 0 .10 )h ,t1/ 2 分别为 (0 .98± 0 .11)和 (1.0 1± 0 .14)h。阿莫西林的相对生物利用度为 (95 .3±7.3) % ;克拉维酸钾的相对生物利用度为 (10 0 .6± 6 .0 ) %。结论 :经统计学分析 。

Objective:To study the relative bioequivalence of domestic and imported amoxicillin and clavulanic acid tablets.Methods:The randomized and crossover study was conducted in 10 healthy male volunteers.After a single dose of the drugs their plasma drug concentration was determined by microbiological assay.Results:Both the domestic and imported tablets of amoxicillin and clavulanic acid fitted to one compartment model.The pharmacokinetics parameters obtained were:C max =(5.17± 0.45 )mg/L,T max =(1.05±0.16)h,t 1/2 =(1.16±0.17)h,AUC 0～t =(12.89±1.03)(mg·h)/L for domestic amoxicillin;C max =(5.25±0.46)mg/L,T max =(1.08±0.23)h,t 1/2 =(1.37±0.23)h,AUC 0～t =(13.54±0.59)(mg·h)/L for imported amoxicillin;C max =(3.94±0.52)mg/L,T max = (1.10± 0.21)h,t 1/2 =(0.98±0.11)h,AUC 0～t =(8.25±0.92)(mg·h)/L for domestic clavulanic acid;C max =(4.10±0.35)mg/L,T max =(1.03±0.10)h,t 1/2 =(1.01±0.14)h,AUC 0～t =(8.18± 0.51) (mg·h)/L for imported clavulanic acid.The relative bioequivalence was:(95.3±7.3)% for amoxicillin;(100.6±6.0)% for clavulanic acid.Conclusion:The domestic and imported amoxicillin and clavulanic acid tablets are bioequivalence.