目的:建立测定血浆中穿心莲内酯和脱水穿心莲内酯的LC/MS/MS法,研究单体穿心莲内酯和脱水穿心莲内酯的药代动力学.方法:测定大鼠血浆中的穿心莲内酯和脱水穿心莲内酯时,血浆样品经沉淀蛋白处理后,以甲醇-水(85∶15)为流动相,采用Lichrospher C18柱分离.选用电喷雾离子源,选择反应监测方式扫描,负离子方式检测.结果:穿心莲内酯和脱水穿心莲内酯在该条件下分离良好,保留时间分别为3.57min和4.51min.穿心莲内酯和脱水穿心莲内酯的线性范围均为0.02～10μg·m-1.定量下限均为0.02μg·mL-1,最低检出量为0.003ng.结论:该方法简便、灵敏、专属性强,适合于穿心莲内酯和脱水穿心莲内酯在大鼠体内的药代动力学研究.

This study aimed to establish a LC/MS/MS method for the simultaneous determination of andrographolide and dehydroandrographolide in rat plasma and to reveal their pharmacokinetics. After a simple protein precipitation using methanol, andrographolide and dehydroandrographolide were chromatographed on a Lichrospher C18 column using methanol-water (85:15) as the mobile phase. The detection was performed by the selected reaction monitoring (SRM) mode via the electrospray ionization source (ESI) operating in the negative ionization mode. The experimental results showed that andrographolide and dehydroandrographolide were completely separated in the chromatographic condition. Both of them had a linear range of 0.02-10ug·mL-1 and LLOQ of 0.02ug·mL-1. This method is simple, sensitive and rapid, and is suitable to the pharmacokinetics study of andrographolide and dehydroandrographolide.

国家自然科学基金面上项目(30600823):中药穿心莲二萜内酯类活性成分的跨膜转运机理及药物代谢动力学研究，负责人：廖琼峰；国家自然科学基金面上项目(30600818):黄连配伍吴莱萸复方活性成分的药代动力学及其配伍机制研究，负责人：谢智勇。