目的：建立同时测定生物样品中半枝莲碱 A 和半枝莲碱 B 的 LC-MS/MS 分析方法,并对其药代动力学进行研究。方法血浆样品采用乙酸乙酯萃取,BDS Hypersil C18(50 mm×2.1 mm,2.4μm)色谱柱进行梯度洗脱,柱温40℃,流动相为乙腈：0.05%甲酸水溶液,流速为0.25 mL/min。电喷雾离子源,MRM 模式。大鼠单剂量灌胃500 mg/kg 半枝莲提取物后,检测半枝莲碱 A 和半枝莲碱 B 的血药浓度,DAS 软件对其血药浓度-时间曲线进行拟合,统计矩模型计算药动学参数。结果半枝莲碱 A 和半枝莲碱 B 在0.512~258.0 ng/mL 和0.482~241.0 ng/mL 间线性关系良好(r 2>0.994)；精密度、准确度、提取回收率和基质效应、稳定性均符合生物样品分析要求。半枝莲碱 A 和半枝莲碱 B 的 AUC(0-t)分别为(88.69±12.4)μg/L·h 和(57.09±9.84)μg/L·h,达峰浓度分别为(10.22±1.31)ng/mL 和(6.27±0.80)ng/mL。结论该方法简便、准确、灵敏,可用于半枝莲提取物中半枝莲碱 A 和半枝莲碱 B 体内药代动力学研究。%OBJECTIVE The aim of this study was to develop and validate a LC-MS∕MS method to simultaneously determi-nation of Scutebarbatine A and Scutebarbatine B in rat plasma and applicated this method to pharmacokinetic study of Scutebar-batine A and Scutebarbatine B after oral administration of Scutellaria barbata extract.METHODS Plasma samples were pre-pared with ethyl acetate using liquid-liquid extraction.Then samples were separated by using BDS Hypersil C1 8(50 mm×2.1 mm,2.4 μm)with gradient elution program and oven temperature was set at 40 ℃.And the mobile phase was consisted with acetonitrile∕water(0.05% formic acid) at a flow rate of 0.25 mL∕min.Determination was carried out on a tandem mass spec-trometer in positive ion mode using a multiple reaction monitoring(MRM)via a electrospray ionization(ESI)interface.After oral administration of 500 mg∕kg Scutellaria barbata extract,plasma samples were collected and analyzed by using a DAS soft-ware to analyze to the pharmacokinetic parameters.RESULTS Scutebarbatine A and Scutebarbatine B were liner at the range of 0.5 12~258.0 ng∕mL,0.482~241.0 ng∕mL,respectively with a r 2 larger than 0.994.Accuracy,precious,extraction effi-ciency,matrix effects and stability study were all meet the requirement of the bioanalytical method.The AUC(0-t) for Scutebar-batine A and Scutebarbatine B were(88.69±12.4)μg∕L.h,(57.09±9.84)μg∕L.h,respectively.And the Cmax for Scutebar-batine A and Scutebarbatine B were(10.22±1.31)ng∕mL and (6.27 ±0.80)ng∕mL.CONCLUSION The method was sim-ple,accurate,and sensitive,which could be used for the pharmacokinetic study of Scutebarbatine A and Scutebarbatine B after oral administration of Scutellaria barbata extract.
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