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目的 :建立测定兰索拉唑及其代谢产物 5’ 羟基兰索拉唑和兰索拉唑砜的血药浓度的方法 ,用于测定其血药浓度并进行临床药代动力学研究。方法 :采用高效液相 二极管阵列色谱法测定兰索拉唑及其代谢产物 5’ 羟基兰索拉唑和兰索拉唑砜的血药浓度。结果 :兰索拉唑的校正标准曲线为Y =0 .0 135 8+0 .0 0 12 2 7X (r =0 .9994 ) ,其 2 5 ,2 0 0 ,2 0 0 0μg·L-1三浓度的血样回收率分别为 87.99% ,94 .38% ,77.2 1% ;精密度分别 7.79% ,1.2 1% ,5 .4 9% ;5’ 羟基兰索拉唑的校正标准曲线分别为Y=0 .0 0 2 5 36+0 .0 0 0 912 6X (r=0 .9990 ) ,其 2 0 ,10 0 ,5 0 0 μg·L-1三浓度的血样回收率分别为 85 .85 % ,87.64% ,10 7.70 % ;精密度分别为 10 .73% ,6.98% ,5 .62 % ;兰索拉唑砜的校正标准曲线分别为Y =0 .0 1486+0 .0 0 1462X (r =0 .9995 ) ,其 2 0 ,10 0 ,10 0 0μg·L-1三浓度的血样回收率分别为 79.84 % ,85 .18% ,10 0 .68% ;精密度分别为 9.2 2 % ,2 .36% ,4 .81%。志愿受试者禁食口服 30mg兰索拉唑胶囊后 ,兰索拉唑及其代谢产物 5’ 羟基兰索拉唑和兰索拉唑砜的Cmax 分别为 113.2 1,15 61.5 4 ,131.14μg·L-1。结论 :此方法可满足测定要求 ,可用于兰索拉唑的药代动力学研究。
OBJECTIVE: To establish a method for the determination of plasma concentration of lansoprazole and its metabolites 5 ’- hydroxy - lansoprazole and lansoprazole sulfone for the determination of its plasma concentration and its clinical pharmacokinetic study. Methods: The plasma concentrations of lansoprazole and its metabolites 5 ’-hydroxyl-lansoprazole and lansoprazole-sulfone were determined by high performance liquid chromatography with diode array. Results: The calibration curve of lansoprazole was Y = 0.13535 +0.012 2 7X (r = 0.9994), and the calibration curves of lansoprazole were 25, 200, 200μg · L-1 The recoveries of three concentrations of blood samples were 87.99%, 94.38% and 77.2%, respectively; the precision were 7.79%, 1.2 1% and 5.94% respectively. The calibration curves of 5 ’-hydroxysalaprazole were Y = 0. 0 2 5 36 +0. 0 0 912 6X (r = 0 .9990). The recovery rates of blood samples at three concentrations of 20, 100 and 500 μg · L-1 were 85.85 %, 87.64% and 10 7.70% respectively. The calibration curves were 10.73%, 6.98% and 5.62% respectively. The calibration curves of lansoprazole sulfone were Y = 0.01486 + 0.01462X ( r = 0.9995). The recovery rates of blood samples at three concentrations of 20, 100 and 100 μg · L-1 were 79.84%, 85.18% and 100.68%, respectively, with the precision of 9.2% , 2.36%, 4.81%. After oral administration of 30 mg of lansoprazole capsules, the Cmax of lansoprazole and its metabolites 5 ’-hydroxyl-lansoprazole and lansoprazole-sulfone were 113.2 1,15 61.5 4 and 131.14 μg · L-1. Conclusion: This method can meet the determination requirements and can be used for the pharmacokinetics of lansoprazole.