奥美拉唑肠溶胶囊人体药代动力学及生物等效性研究

Study on Pharmacokinetics and Bioequivalence of Omeprazole Enteric - coated Capsules in Healthy Volunteers

目的:研究两厂家产奥美拉唑肠溶胶囊在正常人体的药代动力学与生物等效性。方法:将18名健康男性志愿受试者随机交叉口服 40mg奥美拉唑肠溶胶囊受试制剂和参比制剂后,采用高效液相色谱法,以卡马西平为内标,测定奥美拉唑的血浆药物浓度。结果:受试和参比制剂均符合一级吸收开放性一室模型,主要药代动力学参数0-12 h药-时曲线下面积(AUC0→12)分别为(2 719．9±1 551．7),(2 820．8± 1 668．1)ng·h/mL,峰浓度(Cmax)分别为(820．1±420．1),(760．0±415．4)ng/mL,达峰时间(Tmax)分别为(2．4±0．6),(2．5±0．6)h,血浆半衰期(t1/2)分别为(2．2±0．8),(2．4±0．9)h。相对生物利用度为(99．69±13．51)％。结论:两种奥美拉唑肠溶胶囊为生物等效制剂。

Objective： To study the pharmacokinetics and bioequivalenee between test and reference products of omeprazole enteric-coated capsules in 18 male healthy volunteers. Methods： A dose of 40 mg omeprazole enteric-coated capsules （test and reference products） was given according to a randomized cross - over design. Plasma concentrations of omeprazole were determined by HPLC. Results： The concentration - time curves of both preparations fitted to a one- compartment model. The main pharmacokinetic parameters AUC0→12, Cmax, Tmax, T1/2 were （2 719. 9 ＋ 1 551.7）ng · h/mL and （2 820. 8 ＋ 1 668. 1 ）ng · h/mL, （820. 1 ＋420. 1 ）ng/mL and （760. 0 ＋415.4）ng/mL, （2. 4 ＋0. 6）h and （2.5 ＋0. 6）h, （2.2 ＋0. 8）h and （2.4 ＋0. 9）h, respectively. Relative bioavailability was （99.69 ＋ 13.51）%. Conclusion： The test and refer ence omeprazole enteric- coated capsules were bioequivalent.