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目的建立测定血浆中兰索拉唑对映体浓度的高效毛细管电泳分析方法,并用于兰索拉唑在人体内立体选择性药代动力学研究。方法用乙醚作提取溶剂提取血浆中兰索拉唑。采用高效毛细管电泳法测定6名健康男性受试者经口给予兰索拉唑片后不同时刻血浆中药物对映体浓度,绘制血药浓度-时间曲线,并计算主要药动学参数。结果 S—与R—兰索拉唑对映体的主要药动学参数如下:ρmax分别为(0.538±0.039)mg.L-1和(1.050±0.250)mg.L-1,tmax为(1.8±0.7)h和(1.8±0.7)h,t1/2分别为(1.6±0.7)h和(2.7±1.0)h,用梯形法计算,AUC0-t分别为(1.49±0.36)mg.h.L-1和(4.35±1.52)mg.h.L-1。结论兰索拉唑两对映体在人体内的代谢过程具有立体选择性。
Objective To establish a high performance capillary electrophoresis method for the determination of enantiomeric concentrations of lansoprazole in plasma and to study the stereoselective pharmacokinetics of lansoprazole in human. Methods Lansoprazole in plasma was extracted with diethyl ether as extraction solvent. The plasma concentrations of enantiomers in plasma of 6 healthy male volunteers after oral administration of lansoprazole tablets were determined by high performance capillary electrophoresis. The plasma concentration-time curves were plotted and the main pharmacokinetic parameters were calculated. Results The main pharmacokinetic parameters of S- and R-lansoprazole enantiomers were as follows: ρmax were (0.538 ± 0.039) mg.L-1 and (1.050 ± 0.250) mg.L-1, respectively, and tmax was ± 0.7) h and (1.8 ± 0.7) h, respectively, and the values of t1 / 2 were (1.6 ± 0.7) h and (2.7 ± 1.0) h, respectively. The AUC0-t was (1.49 ± 0.36) mg.hL- 1 and (4.35 ± 1.52) mg.hL-1. Conclusion The two enantiomers of lansoprazole have stereoselectivity in human metabolism.