HPLC-MS法测定人血浆中雷贝拉唑的浓度及其药动学

HPLC-MS assay of rabeprazole tablets in human plasma and study on its pharmacokinetics

目的建立人血浆中雷贝拉唑的HPLC-MS测定方法,用其测定了志愿者口服雷贝拉唑钠肠溶片(20 mg)后的血药浓度,并评价两种制剂的生物等效性。方法18名健康男性志愿者分别单剂量口服受试制剂和参比制剂20 mg,采用HPLC-MS法测定血浆中雷贝拉唑的浓度。计算主要药动学参数及相对生物利用度,以判断生物等效性。结果受试制剂和参比制剂在受试者体内的药动学参数:tmax分别为(2.6±0.4)和(2.6±0.3)h,ρmax分别为(684.8±114.1)和(692.4±89.0)μg.L-1,t1/2分别为(1.7±0.5)和(1.8±0.5)h;用梯形法计算,AUC0→t分别为(2 036±358.6)和(2 194±340.3)μg.h.L-1,AUC0→∞分别为(2 169±430.2)和(2 287±348.5)μg.h.L-1;以AUC0→t计算,雷贝拉唑的相对生物利用度平均为(93.1±14.6)%。结论两种雷贝拉唑片具有生物等效性。

A/M To develop an HPLC-MS assay for determination of rabeprazole in human plasma and to investigate the pharmacokinefics and bioequivalenee of two rabeprazole tablets in human. METHODS A single oral dose of 20 mg rabeprazole tablets was given according to a randomized crossover design. The plasma concentrations of rabeprazole were determined by a HPLC-MS method. RESULTS The main pharmacokinetie parameters of the test and the reference tablets were as follows： tmax were （2.6 ± 0.4） and （2.6 ± 0.3） h; pmax were （684.8 ± 114.1 ） and （692.4 ± 89.0 ） μg. L^-1;t1/2 were （1.7 ±0.5） and （1.8±0.5）h;AUC0→1 were （2036±358.6） and （2194±340.3）μg.h.L^-1; AUC0→1 were （2 169 ± 430.2） and （ 2 287 ± 348.5） μg. h. L^- 1, respectively. The relative bioavailability of the test formulation was（93.1 ± 14.6）%. CONCLUSION The two tablets show bioequivalenee.