高效毛细管电泳法测定血浆中兰索拉唑对映体浓度

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。

Application of HPCE on the determination of two enantiomers of lansoprazole in human plasma

Objective To establish a method of capillary electrophoresis for the determination of lansoprazole in human plasma,and study the enantioselectivity of lansoprazole.Methods Human plasma was extracted using ether.The concentration of lansoprazole enantiomers in plasma was determined by HPCE after oral administrated of rac-lansoprazole by six healthy volunteers,then the concentration-time curves were plotted and the main pharmacokinetic parameters were calculated,respectively.Results The main pharmacokinetic parameters of S-lansoprazole and R-lansoprazole were as follows:ρmax were(0.538±0.039)mg · L-1 and(1.050±0.250)mg · L-1,tmax were(1.8±0.7)h and(1.8±0.7)h,t1/2 were(1.6±0.7)h and(2.7±1.0)h,AUC0-t were(1.49±0.36)mg · h · L-1 and(4.35±1.52)mg · h · L-1,AUC0-∞ were(1.67±0.44)mg · h · L-1 and(5.02±1.90)mg · h · L-1,respectively.Conclusions The metabolic process of the two enantiomers of lansoprazole is enantioselective.