液相色谱-串联质谱法测定健康人体血浆中米格列醇浓度及其药代动力学研究

Determination the concentration of miglitol in healthy human plasma and study on its pharmacokinetics by LC/MS/MS

目的建立测定血浆中米格列醇片(降血糖药)的液相色谱-串联质谱法,考察米格列醇在中国健康志愿者体内的药代动力学。方法血浆样品经液-液提取后,进行色谱分离,在三重四极杆串联质谱仪上,以多反应离子监测(MRM)方式进行定量分析,用于监测的离子为m/z 208．3→m／z 146．1 (米格列醇)和m/z 268．5→m/z 250．4(内标,伏格列波糖)。结果米格列醇的最低定量浓度为5．0 μg·L-1,线性范围为5～2 000 μg·L-1,精密度与准确度符合生物样品分析要求。结论该法操作简便、快速、灵敏度高,适于临床药代动力学研究。

Objective To establish a rapid and sensitive LC/M5/MS method for the analysis of miglitol in plasma and study the pharmacokinetics of miglitol in China healthy volunteers. Methods Plasma samples containing miglitol and voglibose （internal standard, IS ） were extracted with liquid- liquid extraction, followed by liquid chromatographic separation and on - line MS/MS using turboionspray ionization as an interface detection. Muhy reaction monitoring with mass transitions m/z 208.3 146.1 and m/z 268.5→250.4 were used for miglitol and IS, respectively. Results The limits of quantitation of method for miglitol was 5.0 μg·L^-1, the calibration curves in plasma was linear in the range of 5 to 2000μg·L^-1 and intra - and inter - day precision over this range were less than 3.0%. Conclusion The method is shown to be accurate and convenient, and suitable for clinical pharnacokinetics.