目的 对中国男性健康志愿者口服氨苄西林丙磺舒胶囊后进行生物等效性评价.方法 选取20名海南医学院男性健康志愿者,采用单剂量双周期、随机和交叉试验设计,口服氨苄西林丙磺舒胶囊0.75g后,以HPLC法分别测定不同时间点的氨苄西林和丙磺舒血药浓度.并利用DAS 2.0软件计算其药动学参数和进行统计学分析.结果 参比制剂与受试制剂的氨苄西林主要药动学参数Tmax、Cmax、AUC0→12和AUC0→∞分别为(2.05±0.56)h和(2.13±0.46)h;(10.47±4.40)mg/mL和(10.65±4.22)mg/mL;(59.77±27.24)(mg·h)/mL和(62.68±24.56)(mg·h)/mL;(68.18±30.34)(mg·h)/mL和(71.78±28.76)(mg·h)/mL.丙磺舒主要药动学参数Tmax、Cmax、AUC0→24和AUC0→∞分别为(1.98±0.82)h和(1.75±0.73)h;(18.41±5.67)mg/mL和(19.78±5.45)mg/mL;(109.41±41.34)(mg· h)/mL和(113.07±38.78)(mg·h)/mL;(114.47±41.24)(mg·h)/mL和(118.88±38.21)(mg·h)/mL.参比制剂与受试制的氨苄西林、丙磺舒主要药动学参数经统计学分析均无显著性差异.结论 两制剂具有生物等效性.%Objective To investigate the bioequivalence of the ampicillin and probenecid capsules in Chinese healthy males.Methods A total of 20 Chinese healthy male participants were recruited in a randomized crossover study.A single oral dose of 0.75g ampicillin and probenecid was given to the participants to evaluate the serum concentrations at different points by High performance liquid phase (HPLC) and pharmacokinetic parameters by DAS 2.0 software.Results The results did not show significant differences in main pharmacokinetic parameters of ampicillin between the measured and the reference preparations.The Tmax,Cmax,AUC0→12 and AUC0→∞ values of the measured preparation were (2.13±0.46)h,(10.65±4.22)mg/mL,(62.68±24.56)(mg·h)/mL and (71.78±28.76)(mg·h)/mL,respectively;of reference preparation,those were (2.05±0.56)h,(10.47±4.40)mg/mL,(59.77±27.24)(mg·h)/mL and (68.18±30.34)(mg·h)/mL respectively.Meanwhile,it exhibited similar profiles in the pharmaeokinetics parameters of probenecid between the measured and the reference preparations without statistical differences,and the Tmax,Cmax,AUC0→12 and AUC0→∞ values of the measured preparation were (1.75±0.73)h,(19.78±5.45)mg/mL,(113.07±38.78)(mg.h)/mL and (118.88±38.21)(mg·h)/mL,and of the reference preparation were (1.98±0.82)h,(18.41±5.67)mg/mL,(109.41±41.34)(mg·h)/mL and (114.47±41.24)(mg·h)/mL,respectively.Conclusion The results showed that the measured formulations of ampicillin and probenecid capsules are bioequivalent to the reference preparations.
展开▼
