基于UPLC-MS法研究5种柴胡皂苷在大鼠体内的药代动力学及组织分布  

Study on Pharmacokinetics and Tissue Distribution of Five Saikosaponin in Chaihu(Radix Bupleuri)in Rats by UPLC-MS

作　　者：曾德浩[1] 闫雪[1] ZENG Dehao;YAN Xue(The First Affiliated Hospital of Guangzhou University of Chinese Medicine,Guangzhou 510405,Guangdong,China)

机构地区：[1]广州中医药大学第一附属医院,广东广州510405

出　　处：《辽宁中医杂志》2024年第12期141-146,共6页Liaoning Journal of Traditional Chinese Medicine

基　　金：广东省中医药局课题项目(20161017)。

摘　　要：目的应用超高效液相色谱(ultra performance liquid chromatography,UPLC)-高分辨率质谱联用仪(mass spectrometry,MS)探究5种柴胡皂苷在大鼠体内的药代动力学及组织分布,在找出有效部位中的化学成分及其共性的同时研究其主要有效成分的药代动力学。方法应用UPLC法对指标成分柴胡皂苷a(saikosaponin a,SSa)、柴胡皂苷c(saikosaponin c,SSc)、柴胡皂苷b1(saikosaponin b1,SSb1)、柴胡皂苷d(saikosaponin d,SSd)、柴胡皂苷b2(saikosaponin b2,SSb2)进行含量测定,应用于组织分布研究。选择柴胡醇提物灌胃SD大鼠,给药后0.25、0.5、0.75、3、5 h处死,取心、肝、脾、肺、肾组织,样品经预处理后,采用上述方法测定组织中各皂苷类成分的含量,进行组织分布研究。结果UPLC-MS法提示血清中的内源性物质对内标和待测物质均无干扰,柴胡皂苷类成分的线性良好,高、中、低浓度的日内和日间精密度SD值均低于10%,经冻融循环及长短期稳定性的考察,柴胡皂苷类无明显降解,稳定性良好,符合生物样本分析方法的指导原则。待测成分无明显的基质效应。该研究测定的5种柴胡皂苷类成分组织分布存在一定相似性。在肝、肺组织中的含量高于其他组织,其特点为肝、肺>心、肾>脾,并且在肝脏组织中0.5 h最高,在肺组织中0.75 h较高;SSa与SSd具有相似结构,在组织分布中提现出了相似的特点:肺>肝、肾>心、脾,肺组织中的含量高于其他组织,在0.75 h有最大值,而相对含量较高的肝组织中也是在0.5 h有最大值。结论该研究通过UPLC-MS分析柴胡中SSa、SSc、SSb1、SSd、SSb2等5种皂苷类成分,对其予以定量分析。提示UPLC-MS方法灵敏、快速、可靠,并成功地用于柴胡药代动力学及组织分布研究,获得了柴胡皂昔类成分的药动学参数,提示各成分在不同组织中分布特点。体外柴胡醇提物成分容易吸收,在临床应用时可依据药理作用选择。Objective To explore the pharmacokinetics of five saikosaponin in Chaihu(Radix Bupleuri)under ultra performance liquid chromatography(UPLC)-mass spectrometry(MS),and to study the pharmacokinetics of the main active components while finding out the chemical constituents and their commonalities in the active parts.Methods The contents of saikosaponin a(SSa),saikosaponin c(SSc),saikosaponin b1(SSb1),saikosaponin d(SSd)and saikosaponin b2(SSb2)were determined by UPLC.SD rats were administrated with Chaihu(Radix Bupleuri)extract in the stomach.After 0.25,0.5,0.75,3 and 5 h,the heart,liver,spleen,lung and kidney tissues were taken out.After the samples were pretreated,the contents of saponins in the tissues were determined by the above methods,and the tissue distribution was studied.Results The UPLC-MS method indicated that the endogenous substances in serum had no interference with the internal standard and the substance to be measured.The linearity of saikosaponins was good,and the precision SD values of high,medium and low concentrations were all lower than 10%.Through freeze-thaw cycle and long-term and short-term stability investigation,saikosaponins did not degrade significantly,and the stability was good,complying with the guidelines of biological sample analysis methods.There was no obvious matrix effect of the components under test.There were some similarities in the tissue distribution of the five saposide components determined in this study.The content in liver and lung tissues was higher than that in other tissues,which was characterized as liver and lung>heart and kidney>spleen,and the highest content was found in liver tissue at 0.5 h and lung tissue at 0.75 h.SSa and SSd had similar structure,showing similar characteristics in tissue distribution:lung>liver,kidney>heart and spleen.The content of SSA in lung tissue was higher than that in other tissues,and had a maximum value at 0.75 h,while that in liver tissue with relatively high content also had a maximum value at 0.5 h.Conclusion:In this study,five s

关 键 词：UPLC-MS 柴胡 皂苷类 药代动力学 

分 类 号：R285[医药卫生—中药学]