奥美拉唑肠溶胶囊的人体相对生物利用度与生物等效性研究

Relative Bioavailability and Bioequivalence of Omeprazole Enteric-coated Capsules in Healthy Volunteers

目的建立测定血浆奥美拉唑浓度的高效液相色谱(HPLC)法,研究奥美拉唑肠溶胶囊的相对生物利用度及其生物等效性。方法按两制剂双周期自身对照交叉试验设计,男性健康志愿者20例,分别单剂量口服2种国产奥美拉唑肠溶胶囊,用HPLC法测定血药浓度,计算药动学参数,并评价两种制剂的生物等效性。结果口服奥美拉唑肠溶胶囊参比制剂及受试制剂40 mg后的主要药动学参数:峰浓度(Cmax)分别为(906.01±589.55)和(875.87±662.95)ng.mL-1;达峰时间(tmax)分别为(2.21±0.88)和(2.07±0.87)h;血药浓度-时间曲线下面积(AUC0-12)分别为(1 778.70±1 164.11)和(1 834.25±1 342.25)ng.h.mL-1;半衰期(t1/2Ke)分别为(0.96±0.25)和(0.85±0.18)h。受试制剂对参比制剂平均相对生物利用度F为(104.02±13.60)%。结论该两种奥美拉唑胶囊生物等效。

Objective To set up a method of content determination for omeprazole in human plasma by HPLC and study the pharmacokinetics and relative bioavailability of omeprazole enteric-coated capsules. Methods A single dose of reference and test omeprazole enteric-coated capsules was given to 20 healthy volunteers,respectively,in a randomized 2-way cross-over study.The plasma concentration of omeprazole was determined by HPLC and their pharmacokinetics as well as relative bioavailability was measured. Results The main pharmacokinetic parameters of two formulations,reference and test ones were as follows： Cmax were（906.01±589.55）and（875.87±662.95） ng·mL-1,tmax were（2.21±0.88）and（2.07±0.87）h,AUC0-12 were（1 778.70±1 164.11）and（1 834.25±1 342.25）ng·h·mL-1;t1/2 Ke were（0.96±0.25）and（0.85±0.18）h.The relative bioavailability of F0→12 was（104.02 ±13.60）%. Conclusion The two kinds of omeprazole enteric-coated capsules are bioequivalent.