两种规格阿莫西林分散片生物等效性研究

Bioavailability Study of Two Kinds of Amoxycillin Dispersible Tablets

目的研究两种规格阿莫西林分散片与参比制剂的人体相对生物利用度,评价其人体生物等效性。方法采用3制剂3周期2重3*3拉丁方试验设计方案,24例男性健康受试者空腹条件下口服单剂量3种阿莫西林分散片,剂量均为1g,服药后于8h内抽取静脉血,高效液相色谱法测定血浆阿莫西林浓度。采用DAS药动学程序进行数据处理,计算参数并评价试验制剂与参比制剂的生物等效性。结果阿莫西林分散片试验制剂A(每片0.25g)、试验制剂B(每片0.125g)与参比制剂(每片0.25g)的tmax分别为(1.68±0.56)h,(1.65±0.54)h,(1.79±0.61)h;t1/2ke分别为(1.19±0.34)h,(1.16±0.31)h,(1.10±0.15)h;Cmax分别为(12.42±3.01)μg·mL-1,(11.85±3.40)μg·mL-1,(11.16±3.07)μg·mL-1;AUC0-8h分别为(33.83±7.81),(32.38±7.62),(31.37±7.25)μg·mL-1·h;AUC0-∞分别为(35.10±7.72),(33.63±7.87),(32.50±7.32)μg·mL-1·h。试验制剂A、B的相对生物利用度分别为(110.2±21.9)%和(106.0±25.3)%。结果表明,试验制剂与参比制剂主要药动学参数tmax、Cmax、AUC0-8h及AUC0-∞差异无显著性(P>0.05)。结论阿莫西林分散片试验制剂与参比制剂具有生物等效性。

Objective To study the relative boiavailability of two specifications of amoxycillin dispersible tablets with the reference one and to evaluate the bioequivalence in healthy volunteers. Methods The 3 formulations in 3 periods with double 3 ＊ 3 Latin square test were adopted. 24 healthy volunteers were orally given with 1 g of either amoxycillin dispersible tablets in an open randomized cross-over test. The plasma amoxycillin concentration was determined within 8 h administration by HPLC. The data were processed by DAS pharmacokinetic program, which were calculated to evaluate the bioequivalence between tested formulations and reference formulation. Results The pharmacokinetics markers of amoxyciUin dispersible tablets were as follows： tmax were （1.68±0.56）h,（1.65±0.54）h,（1.79±0.61）h;t1/2ke were（1.19±0.34）h,（1.16±0.31）h,（1.10±0.15）h;Cmax were（12.42±3.01）μg·mL^-1,（11.85±3.40）μg·mL^-1,（11.16±3.07）μg·mL^-1,AUC0-8h were（33.83±7.81）μg·mL^-1·h,（32.38±7.62）μg·mL^-1·h,（31.37±7.25）μg·mL^-1·h;AUC0-∞ were（35.10±7.72）μg·mL^-1·h,（33.63±7.87）μg·mL^-1·h,（32.50±7.32）μg·mL^-1·h.respectively. The relative bioavailability of two tested formulations were （ 110.2 ± 21.9 ） %, （ 106.0 ± 25.3 ） % , respectively. The results show that there were no significant differences in parameters tmax, Cmax, AUC0-8h and AUC0-∞ between tested formulations and reference formulation （P 〉0.05 ）. Conclusion Three formulations of amoxycillin dispersible tablets are bioequivalent.