LC-MS/MS法测定人血浆中伊伐布雷定浓度及药动学

目的：建立人血浆中伊伐布雷定的液相色谱-质谱-质谱联用测定方法,研究健康人体药代动力学。方法：以地西泮为内标物,采用液相色谱-质谱-质谱联用法,电喷雾电离源选择性正离子峰检测。测30名健康志愿者单剂量口服盐酸伊伐布雷定片的体内血药浓度,获得药动学参数。结果：伊伐布雷定在0.101-101 ng·mL-1浓度范围内呈良好的线性关系（r=0.998）,最低检测浓度为0.101 ng·mL-1。高、中、低浓度的方法提取回收率分别为93.2%、86.6%、87.5%,日内、日间精密度RSD均小于15%。结论：LC-MS/MS方法灵敏度高,专属性强,准确,简便,适用于盐酸伊伐布雷定片的人体药代动力学研究。

Determination of Ivabradine in Human Plasma by LC-MS/MS and Study of Pharmacokinetics

Objective： To determine ivabradine in human plasma by a LC/MS/MS method,and to investigate its pharmacokinetics.Methods： Ivabradine concentrations in plasma were determined by LC-MS/MS.The test and reference formulations of ivabradine were given to 30 healthy male volunteers.Results： The linear range for rosuvastatin was 0.101-101 ng·mL-1（r = 0.998）.The quantitation limit for rosuvastatin was 0.101 ng·mL-1.The draw recovery rates were 93.2 %,86.6 % and 87.5 %,and RSD for intra-day and inter-day was both less than 15 %.Conclusion： LC-MS/MS method is sensitive,accurate and simple,and suitable for the study on pharmacokinetic of ivabradine in human.