瑞格列奈分散片在健康人体中的相对生物利用度研究

目的研究瑞格列奈分散片与瑞格列奈片在中国男性健康志愿者体内的相对生物利用度。方法采用随机双周期自身交叉对照试验设计，20名健康男性受试者分别口服受试制剂瑞格列奈分散片和参比制剂瑞格列奈片4mg，采用LC-MS／MS法测定给药后不同时间瑞格列奈的血药浓度。利用DAS2．0计算药动学参数和进行统计分析，通过方差分析和双单侧t检验及90％置信区间法进行生物等效性评价。结果受试制剂与参比制剂中瑞格列奈的Cmax分别为（110．8±59．9）、（101．5±48．8）μg·L^-1；tmax分别为（0．54±0．20）和（0．65±0．34）h；AUC0～8分别为（112．5±38．4）和（110．8±42．O）μg·h·L^-1；AUC0-∞分别为（114．1±38．8）和（112．7±41.8）μg·h·L^-1。受试制剂对参比制剂的相对生物利用度F（以AUC0-8作为评价依据）为（105．0±25．0）％。结论受试制剂与参比制剂具有生物等效性。

Bioequivalence of repaglinide in healthy volunteers

Objective To evaluate the bioequivalence of repaglinide dispersible tablets and repaglinide tablets. Methods A randomized crossed-over study was conducted in 20 healthy volunteers. After a single dose of test and reference preparations （containing 4 mg repaglinide）, the plasma drug levels were determined by LC-MS/MS. The related pharmacokinetic parameters were calculated by DAS 2.0 and the bioequiavailability of the two preparations was evaluated by variance analysis and two one sided t tests by 90% confidence interval method. Results The main pharmacokinetics parameters of the test and reference preparations were as follows ： Cmax was （110. 8±59. 9） and （101.5±48.8）μg·L^-1 ; tmax was （0. 54±0.20） and （0.65±0.34） h; AUG0-8 was （112.5±38.4） and （110.8±42.0）μg·h·L^-1 ; AUG0-∞ was （ 114.1 ± 38.8） and （ 112.7± 41.8） μg·h·L^-1. The relative bioavailability of repaglinide dispersible tablets was （105.0±25.0） % as against the reference preparation. Conclusion The two formulations are bioequivalent.