泮托拉唑钠肠溶微丸胶囊剂的人体生物等效性

Bioequivalence of pantoprazole sodium enteric-coated capsules in human

目的评价单剂量口服2种泮托拉唑钠制剂后的人体生物等效性。方法20名男性健康受试者随机分成2组,采用自身对照交叉给药的方式,单剂量口服试验制剂和参比制剂各40mg,在设定时间点抽取静脉血,采用HPLC-UV检测方法测定血药浓度。结果试验制剂和参比制剂的t_(max)分别为(2.68±0.54)、(3.43±0.67)h,ρ_(max)为(1 966±781)、(2 265±772)μg·L^(-1),MRT为(4.55±0.98)、(5.22±1.03)h,t_(1/2)为(1.94±0.50)、(1.68±0.37)h,AUC_(0→15h)为(7 787±5 391)、(7 989±4 492)μg·h·L^(-1),AUC_(0→∞)为(7 955±5 634)、(8 143±4 715)μg·h·L^(-1)。结论试验制剂平均相对生物利用度为(94.4±14.1)%,试验制剂与参比制剂生物等效。

AIM To study the pharmacokinetics, relative bioavailability and bioequivalence of pantoprazole sodium enteric-coated capsule and pantoprazole sodium enteric-coated tablet in healthy volunteers. METHODS A single oral dose of 40 mg pantoprazole enteric-coated capsules and pantoprazole enteric-coated tablets were given to 20 healthy volunteers in a randomized crossover study. Pantoprazole concentrations in plasma were determined by HPLC with ultraviolet detector. RESULTS The main pharmacokinetic parameters of pantoprazole enteric-coated capsules（as test formulation） and enteric-coated tablets （ as reference） were as follows： t max were （2.68 ± 0.54）, （ 3.43 ± 0.67） h ; ρ max were （ 1 955 ± 781）, （2 265 ± 772）μg· L^-1; MRT were（4.55± 0.98）, （5.22 ± 1.03）h; t1/2 were（1.94 ± 0.50 ）, （1.68 ± 0.37）h; AUC0→15 h were（7 787 ± 5 391 ）, （7 989 ± 4 492）μg· h· L^- 1 ; AUC0→∞ were（7 955 ± 5 634）, （8 143 ± 4 715）μg· h· L^- 1. CONCLUSION The relative bioavailability of pantoprazole enteric-coated capsules and pantoprazole enteric-coated tablets was （94.4± 14. 1）% and the results of statistical analysis demonstrates that the two formulations are of bioequivalence.