[关键词]
[摘要]
目的 以"体外-体内"多维化学物质组关联网络为基础,结合体内药动学研究,明确茯苓药效质量标志物,并建立质量标志物的高效液相色谱-串联质谱定量方法,进行茯苓药材质量评价。方法 以薯蓣皂苷为内标,建立茯苓三萜类成分的超高效液相色谱-三重四级杆串联质谱(UHPLC-MS/MS)定量分析方法,绘制体内药效成分的药动学曲线,以此为依据明确茯苓药效质量标志物主要包括去氢土莫酸、土莫酸、茯苓新酸B等7种成分。检测10批茯苓药材中含量较高的成分和质量标志物的质量分数,并分别以质量分数较高成分、质量分数较高或药效质量标志物为变量进行10批茯苓药材的聚类分析。结果 以不同指标为变量进行聚类分析评价茯苓药材质量时,结果存在差异。结论 仅以质量分数较高的成分进行茯苓质量控制的方法在一定程度上存在片面性。为了全面精准的控制茯苓质量,需要充分考虑茯苓体内外成分变化和体内动力学过程,选取真正与药效相关的药效质量标志物用于其质量控制。
[Key word]
[Abstract]
Objective The quality markers of Poria cocos were identified based on the "in vitro-in vivo" multidimensional chemical group associated network and in vivo pharmacokinetics, and the mass spectrometry method for quantitative detection of quality markers was established to evaluate the quality of P. cocos. Methods A quantitative analysis method of triterpenoids in P. cocos was established by ultra-high performance liquid chromatography-triple quadruple tandem mass spectrometry (UHPLC-MS/MS) while dioscin was chosen as internal reference substance. The pharmacokinetic curves of active ingredients in vivo were drawn. Seven quality markers of P. cocos including dehydrotumulosic acid, tumulosic acid, and poricoic acid B were identified based on the results of pharmacokinetics. The content of high content components and quality markers in 10 batches of P. cocos were detected and used as variables for cluster analysis of 10 batches of P. cocos. Results There were differences in the results of clustering analysis with different indexes as variables in evaluating the quality of P. cocos. Conclusion To a certain extent, the method of quality control of P. cocos with high content components is one-sided. In order to comprehensively and accurately control the quality of P. cocos, it is necessary to take into full account the in vivo and in vitro changes and the in vivo dynamic process of P. cocos composition, and select the effective quality markers related to its pharmacodynamics for its quality control.
[中图分类号]
[基金项目]
国家自然科学基金重点基金资助项目(81530094)