UPLC-MS/MS法测定大鼠血浆中妇科断红饮胶囊3种有效成分的含量及其药代动力学研究  

Pharmacokinetics and content of three active ingredients from Fuke Duanhongyin Capsule in rat plasma by UPLC-MS/MS

作　　者：牟晴蕊 白璐 赵洪庆[1] 谭喜平 王宇红[1] 吴梦瑶 MOU Qingrui;BAI Lu;ZHAO Hongqing;TAN Xiping;WANG Yuhong;WU Mengyao(Technology Innovation Center,Hunan University of Chinese Medicine,Changsha,Hunan 410208,China;Zhuzhou Qianjin Pharmaceutical Co.,Ltd,Zhuzhou,Hunan 412000,China)

机构地区：[1]湖南中医药大学科技创新中心,湖南长沙410208 [2]株洲千金药业股份有限公司,湖南株洲412000

出　　处：《湖南中医药大学学报》2023年第6期1035-1041,共7页Journal of Hunan University of Chinese Medicine

基　　金：国家自然科学基金项目(81874464);湖南省研究生创新项目(CX20210714);湖南中医药大学产学研合作项目(2020430102003702)。

摘　　要：目的建立UPLC-MS/MS法测定大鼠血浆中妇科断红饮胶囊主要有效成分在大鼠血浆中的浓度,并初步研究其在大鼠体内的药代动力学行为。方法雌性SD大鼠单次或重复灌胃给药妇科断红饮胶囊内容物后,收集72 h内的血液样本,通过UPLC-MS/MS同时测定3种指标性成分的浓度,由Phoenix WinNonlin 8.1计算药代动力学参数。结果以苯海拉明为内标,芍药苷、益母草碱、三七皂苷R1的检测范围分别为2~2000、0.1~300、0.1~800 ng·mL^(-1)。准确度分别在85%~115%之间,日内精密度与日间精密度RSD≤15%。与单次给药组比较,重复给药组大鼠3种成分的药时曲线下面积显著增大,平均滞留时间MRT(0-∞)显著延长(P<0.01),消除半衰期t1/2无明显变化。结论该方法线性关系良好,线性范围宽,定量限低,精密度、回收率等均符合生物样品定量要求,提示该方法快速、灵敏、重复性好,可用于妇科断红饮胶囊3种有效成分在大鼠体内的相关药代动力学研究。以其主要成分芍药苷、益母草碱和三七皂苷R1为代表,妇科断红饮胶囊具有吸收快、分布广的优点。Objective To establish an UPLC-MS/MS method to determine the concentration of the main active ingredients of Fuke Duanhongyin Capsule(FKDHYC)in rat plasma and to preliminarily study their pharmacokinetic behaviors in rats.Methods After single or repeated gavage administration of FKDHYC in female Sprague-Dawley(SD)rats,blood samples were collected within 72 h.The concentration of the three indicator ingredients were determined simultaneously by UPLC-MS/MS and pharmacokinetic parameters calculated by Phoenix WinNonlin 8.1.Results With diphenhydramine hydrochloride as the internal standard,the detection ranges of paeoniflorin,leonurine and notoginsenoside R1 were 2~2000,0.1~300,0.1~800 ng·mL^(-1)respectively.The accuracy was in the range of 85%~115%,and the intra-day and inter-day precisions were≤15%.Compared with the single administration group,the area under the concentration-time curve of the three ingredients in the repeated administration group was significantly increased and the mean retention time(MRT(0-∞))was significantly extended(P<0.01),while the elimination half-life(t1/2)showed no significant change.Conclusion The method of UPLC-MS/MS has good linearity,wide linear range,and low limit of quantification.The precision and recovery meet the requirements for the quantification of biological samples,suggesting that the method is rapid,sensitive and reproducible,and can be used for the pharmacokinetic study of the three active ingredients of FKDHYC in rats.Represented by paeoniflorin,leonurine,and notoginsenoside R1,FKDHYC has the advantages of fast absorption and wide distribution.

关 键 词：妇科断红饮 芍药苷 益母草碱 三七皂苷R1 药时曲线 药代动力学 UPLC-MS/MS 

分 类 号：R284[医药卫生—中药学]