阿莫西林/克拉维酸国产分散片与进口糖浆人体生物等效性研究

Bioequivalence of domestic amoxycillin and clauvlanate dispersible tablets and imported augmentin syrup

20名健康受试者采用随机交叉给药方案 ,分别单剂量口服国产阿莫西林 /克拉维酸 (4∶ 1)分散片和进口制剂 (含阿莫西林 5 0 0 m g,克拉维酸 12 5 mg) ,进行人体药代动力学和生物等效性研究。采用高效液相色谱法测定血清中阿莫西林及克拉维酸的浓度 ,经 3P97程序拟合 ,阿莫西林采用梯形法计算的两者 AUC0 - t均值分别为 (2 2 .94± 5 .0 4)和 (2 3.0 6± 5 .87) mg· h/L ,实测 Cmax均值分别为 (10 .71± 3.2 7)和 (9.99± 2 .96 )mg/L ,实测 Tmax均值分别为 (1.0 3± 0 .2 7)和 (0 .95± 0 .2 6 ) h。克拉维酸采用梯形法计算的两者 AUC0 - t均值分别为 (5 .2 3± 1.5 0 )和 (5 .42± 1.49) mg·h/L,实测 Cmax均值分别为 (2 .5 0± 0 .6 1)和 (2 .44± 0 .6 9) mg/L,实测Tmax均值分别为 (1.0 0± 0 .32 )和 (1.0 5± 0 .33) h。经统计学分析 ,国产制剂和进口制剂具有生物等效性。阿莫西林的相对生物利用度为 (10 1.2± 15 .8) % ,克拉维酸的相对生物利用度为 (97.3± 13.7) %。

A single oral administration of 625mg domestic amoxycillin and clavulanate dispersible tablets and augmentin syrup were given to 20 healthy volunteers in an open randomized crossover study. Serum concentrations of amoxycillin and clavulanic acid were determined with RP-HPLC. The pharmacokinetic parameters for amoxycillin and clavulanate dispersible tablets and augmentin syrup were calculated as follows: AUC 0-t: (22.94±5.04)mg·h/L, (23.06±5.87)mg·h/L (amoxycillin), C max: (10.71±3.27)mg/L, (9.99±2.96)mg/L (amoxycillin), T max: (1.03±0.27)h, (0.95±0.26)h (amoxycillin), AUC 0-t: (5.23±1.50)mg·h/L, (5.42±1.49)mg·h/L (clavulanic acid), C max: (2.50±0.61)mg/L, (2.44± 0.69)mg/L (clavulanic acid), T max: (1.00±0.32)h, (1.05±0.33)h (clavulanic acid). The pharmacokinetic parameters showed that there were no significant difference between two products. The relative bioavailability of amoxycillin and clavulanate dispersible tablets were (101.2±15.8)% for amoxycillin and (97.3±13.7)% for clavulanic acid.