基于化学表征和生物效价检测的大黄配方颗粒质量评价研究

Quality evaluation of rhubarb dispensing granules based on multicomponent simultaneous quantitative analysis and bioassay

该文尝试将多指标成分同时定量分析和生物效价分析方法联合使用的模式应用于中药配方颗粒的质量评价,并以大黄配方颗粒为模式药进行了示范性研究。采用超高效液相色谱法同时测定大黄配方颗粒中芦荟大黄素-8-O-β-D-葡萄糖苷等10个蒽醌类化学成分的含量;在复方地芬诺酯片致小鼠便秘模型上,测定不同批次大黄配方颗粒致泻生物效价;在体外抗大鼠血小板聚集模型基础上,测定不同批次大黄配方颗粒的活血生物效价;采用SPSS统计软件对测定的10个蒽醌类化学成分与致泻、活血生物效价之间的相关性进行统计学分析。多指标化学含量测定结果显示10个批次间大黄配方颗粒的化学表征差异较大,与此同时,致泻、活血生物效价均存在一定的差异性;相关性分析结果显示大黄配方颗粒的致泻生物效价强弱和其含有的结合型蒽醌糖苷类成分的含量有显著相关性(P<0.01),活血生物效价的强弱和其含有的游离型蒽醌成分的含量有显著相关性(P<0.01)。综上,采用多组分化学表征和生物效价检测联用的模式可以客观量化、更全面的反映不同批次大黄配方颗粒的整体质量差异。

This study attempts to evaluate the quality of Chinese formula granules by combined use of multi-component simultaneous quantitative analysis and bioassay. The rhubarb dispensing granules were used as the model drug for demonstrative study. The ultra- high performance liquid chromatography （UPLC） method was adopted for simultaneously quantitative determination of the 10 anthraqui- none derivatives （such as aloe emodin-8-O-β-D-glucoside） in rhubarb dispensing granules; purgative biopotency of different batches of rhubarb dispensing granules was determined based on compound diphenoxylate tablets-induced mouse constipation model; blood activa- ting biopotency of different batches of rhubarb dispensing granules was determined based on in vitro rat antiplatelet aggregation model; SPSS 22. 0 statistical software was used for correlation analysis between 10 anthraquinone derivatives and purgative biopotency, blood activating biopotency. The results of multi-components simultaneous quantitative analysisshowed that there was a great difference in chemical characterizationand certain differences inpurgative biopotency and blood activating biopotency among 10 batches of rhubarbdispensing granules. The correlation analysis showed that the intensity of purgative biopotency was significantly correlated with the con- tent of conjugated anthraquinone glycosides （ P 〈 0. 01 ） , and the intensity of blood activating biopotency was significantly correlated with the content of free anthraquinone （ P 〈 0. 01）. In summary, the combined use of multi-component simultaneous quantitative analy- sis and bioassay can achieve objective quantification and more comprehensive reflection on overall quality difference among different batches of rhubarb dispensing granules.