氨基比林咖啡因片人体生物等效性研究

Bioequivalence of 2 aminopyrine-caffeine tablets in healthy volunteer

目的：比较两种氨基比林咖啡因片的人体相对生物利用度,并进行生物等效性评价。方法：按照两制剂两周期随机交叉设计,选择18例健康志愿者单剂量口服受试制剂或参比制剂各1片（氨基比林150 mg,咖啡因40 mg）,采用HPLC-UV法测定其血药浓度。以DAS软件计算药动学参数,并进行统计学分析,评价两种制剂生物等效性。结果：氨基比林受试和参比制剂AUC0-∞分别为（8.057±2.082）和（8.041±2.101）mg.h.L^-1;Cmax分别为（2.054±0.264）和（2.034±0.270）mg.L^-1;Tmax分别为（0.76±0.18）和（0.82±0.25）h,两者无明显差异;咖啡因受试和参比制剂AUC0-∞分别为（8.156±2.035）和（8.140±2.005）mg.h.L^-1;Cmax分别为（1.131±0.231）和（1.119±0.194）mg.L^-1;Tmax分别为（0.81±0.34）和（0.97±0.78）h,上述药动学参数差异无统计学意义。氨基比林受试制剂的相对生物利用度为（101.4±11.5）%;咖啡因的相对生物利用度为（99.1±9.0）%。结论：两种制剂具有生物等效性。

Objective： To study the pharmacokinetics of 2 aminopyrine-caffeine tablets in health volunteers. Methods： Eighteen volunteers were orally administered by either aminopyrine-eaffeine tablet with 2-way crossover design. The concentrations of aminopyrine and caffeine in plasma were determined by HPLC-UV; the pharmacokinetic parameters were calculated by DAS software. Results： The pharmacokinetic parameters of aminopyrine of two tablets were as follows ： AUC0-∞ were （8. 057 ± 2. 082） and （8. 041 ± 2. 101 ） mg.h.L^-1 ; Cmax were （2. 054 ± 0. 264 ） and （2. 034 ± 0. 270） mg. L^-1 ; Tmax were （0.76 ± 0.18 ） and （0.82 ± 0.25 ） h, respectively. The pharmacokinetic parameters of caffeine of two tablets were as follows： AUC0-∞ were （8. 156 ± 2. 035 ） and （8. 140±2.005） mg.h.L^-1; Cmax were （1. 131 ±0.231） and （1. 119 ±0. 194） mg.L^-1; Tmax were （0.81 ± 0.34） and （0.97 ±0.78） h, respectively. The relative bioavailability of aminopyrine and caffeine were （101.4 ± 11. 5） % and （99.1 ± 9.0） % , respectively. Conclusion ： The 2 aminopyrine-caffeine tablets are bioequivalent.