2种埃索美拉唑制剂的人体生物等效性研究

目的:研究埃索美拉唑胶囊剂与片剂的人体药动学特性,并评价其生物等效性。方法:将24名男性健康志愿者随机分为2组,按双周期单剂量交叉口服2种埃索美拉唑制剂各40mg,以高效液相色谱法测定血浆中埃索美拉唑的浓度,用DAS2.0程序进行数据处理,计算药动学参数,并评价其生物等效性。结果:埃索美拉唑胶囊剂和片剂的Cmax分别为(884.71±265.97)、(919.53±218.44)ng.mL-1,tmax分别为(1.45±0.39)、(1.65±0.45)h,t1/2分别为(2.30±0.51)、(2.23±0.47)h,AUC0～12分别为(3897.50±1033.58)、(4059.57±1715.07)ng.h.mL-1,AUC0～∞分别为(4222.70±1066.73)、(4320.22±1426.73)ng.h.mL-1。埃索美拉唑胶囊剂相对于片剂的生物利用度为(96.01±10.5)%。结论:埃索美拉唑胶囊剂和片剂具有生物等效性。

Bioequivalence of Esomeprazole Capsules vs. Esomeprazole Tablets in Healthy Volunteers

OBJECTIVE： To study the pharmacokinetic characteristics of esomeprazole capsules versus esomeprazole tablets in healthy volunteers and to evaluate their bioequivalence. METHODS： A single oral dose of 40 mg esomeprazole capsules or esomeprazole tablets was given to 24 healthy male volunteers who were randomly assigned to two groups in an open randomized crossover test. The plasma concentration was determined by HPLC. The pharmacokinetic parameters of esomeprazole were analyzed by DAS 2.0 program. The bioequivalence of the two preparations was evaluated. RESULTS： The pharmacokinetic parameters of esomeprazole capsules and esomeprazole tablets were as follows： Cmax were （884.71 ± 265.97） ng · mL^-1 and（919.53± 218.44）ng· mL^-1; tmax were（1.45±0.39）h and（1.65±0.45）h; tl/2 were （2.30±0.51）h and （2.23± 0.47） h;AUC0-12 were（3 897.50± 1 033.58）ng· h · mL^-1 and（4 059.57± 1 715.07）ng · h · mL ^-1; AUC0-∞ were （4 222.70±1 066.73） ng · h · mL^-1 and （4 320.22± 1 426.73） ng · h · mL ^-1. The relative bioavailability of esomeprazole capsules was （96.01± 10.5）%. CONCLUSION： Esomeprazole capsules and esomeprazole tablets are bioequivalent.