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8,2’-二异戊烯基槲皮素-3-甲醚是藏药小叶莲中的主要成分,具有较好的抗乳腺癌活性.本文首次建立了快速、灵敏的测定大鼠血浆中8,2’-二异戊烯基槲皮素-3-甲醚浓度的UPLC-MS/MS方法.以8-异戊烯基山柰酚为内标,采用watersACQUITY UPLC BEH C18色谱柱(2.1 mm×100 mm,1.7μmrn),以0.1％甲酸水-乙腈为流动相梯度洗脱,流速为0.4 mL·min-1,柱温为30℃C.通过电喷雾离子化四极杆串联质谱,负离子多反应监测(MRM)模式,用于定量分析的离子反应分别为m/z451.30→177.25(8,2’-二异戊烯基槲皮素-3-甲醚)、m/z 353.25→298.15 (8-异戊烯基山柰酚).8,2’-二异戊烯基槲皮素-3-甲醚浓度为0.1-2000 ng/mL时线性关系良好(r=0.9954),高、中、低三个浓度的提取回收率在103％-115％范围内,日内、日间精密度均小于15％,准确度在-6％～15％之间.该方法简单快速灵敏,适用于检测8,2’-二异戊烯基槲皮素-3-甲醚的血药浓度并进行大鼠体内的药物动力学研究.药物动力学试验结果表明,雌性大鼠口服灌胃给药100 mg/kg的8,2’-二异戊烯基槲皮素-3-甲醚,2小时达到血浆峰浓度,生物半衰期为6.79小时,20小时内能维持一定量的血药浓度,有利于药物在生物体内产生作用.“,”8,2’-Diprenylquercetin 3-methyl ether with significant anti-breast cancer activity is the main constituent of Tibetan medicine Sinopodophylli Fructus.In the present study,we developed and validated a rapid and sensitive ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method for the determination of 8,2’-diprenylquercetin 3-methyl ether in rat plasma.8-Prenylkaempferol was used as the internal standard.The separation was carried out using Waters ACQUITY UPLC BEH C18 column (2.1 mm×100 mm,1.7 μm) with a mobile phase consisting of acetonitrile and 0.1％ formic acid in water on a gradient program at a flow rate of 0.4 mL·min-1 and temperature of 30 ℃C.Triple quadrupole mass spectrometric detection in negative ion mode was used for multiple-reaction monitoring of the transitions at m/z 451.30→177.25 and m/z 353.25→298.15 for 8,2’-diprenylquercetin 3-methyl ether and 8-prenylkaempferol,respectively.The calibration curves were linear within the concentration range 0.1-2000 ng/mL (r =0.9954).The recoveries were 103％-115％,and the results were consistent across low,middle and high concentration levels.The intra-and inter-day precisions were within 15％,and the bias was between-6％ ～15％.This method was simple,rapid and sensitive,which could be applied to the determination of 8,2’-diprenylquercetin 3-methyl ether in plasma and pharmacokinetic study in rats.Pharmacokinetic test indicated that the peak plasma concentration occurred in 2 h after the female rats were intragastrically administered with 8,2’-diprenylquercetin 3-methyl ether at the dose of 100 mg/kg,and the biological half-life was 6.79 h.The blood drug concentration maintained equal amount for 20 h,which was conducive to the in vivo effects of drugs.