基于抗炎活性的葛根芩连片整体的中药生物药剂学分类系统研究  

Study on biopharmaceutics classification system of Chinese materia medica for Gegen Qinlians Tablets based on anti-inflammatory activity

作　　者：王子禹 刘洋[1] 张鑫[1] 李彦萍 程亚茹 董玲[1] WANG Zi-yu;LIU Yang;ZHANG Xin;LI Yan-ping;CHENG Ya-ru;DONG Ling(Beijing University of Chinese Medicine,Beijing 102488,China)

机构地区：[1]北京中医药大学

出　　处：《中国中药杂志》2019年第17期3662-3671,共10页China Journal of Chinese Materia Medica

基　　金：国家自然科学基金项目(81473362)

摘　　要：中药生物药剂学分类系统(CMMBCS)研究最终应落实到中药复方整体研究层面,而中药复方整体的溶解度和渗透性等重要参数不止是各成分溶解度和渗透性的简单加和。该研究以葛根芩连片为研究对象,采用HPLC同时测定葛根芩连片中12个代表性成分葛根素、大豆苷、黄芩苷、大豆苷元、汉黄芩苷、黄芩素、汉黄芩素、甘草酸、盐酸黄连碱、表小檗碱、盐酸小檗碱、盐酸巴马汀的含量,得到各成分的质量权重;利用脂多糖(LPS)诱导RAW264. 7细胞构建体外炎症模型,考察葛根芩连片中12个代表性成分的抗炎作用,得到各成分的药效权重。通过经典摇瓶法和在体单向肠灌流法分别测定葛根芩连片中各有效成分的溶解度和有效渗透系数,并采用质量权重和药效权重相结合的方式进行整合,得到能够代表葛根芩连片整体性质的剂量数和有效渗透系数,结果表明葛根芩连片属于低溶解度、低渗透性药物,应归为CMMBCSⅣ类。The research on biopharmaceutics classification system of Chinese materia medica( CMMBCS) should be finally implemented to the holistic research level of traditional Chinese medicine compounds,while the overall biopharmaceutical properties of traditional Chinese medicine compounds are not only the sum of solubility and permeability of each component. In this study,Gegen Qinlian Tablets was used as the research object,and the contents of 12 representative components,i.e. puerarin,daidzin,baicalin,daidzein,wogonoside,baicalein,wogonin,glycyrrhizic acid,coptisine hydrochloride,epiberberine,berberine hydrochloride and palmatine hydrochloride,were simultaneously determined by HPLC to obtain the mass weight of each component. The in vitro lipopolysaccharide( LPS)-induced RAW264. 7 cells inflammation model was established to investigate the anti-inflammatory effects of 12 representative components and obtain the efficacy weight of each component. In order to obtain the number of doses and effective permeability coefficient which can represent the overall biopharmaceutical properties of Gegen Qinlian Tablets,mass weight was combined with efficacy weight to integrate the solubility and permeability data of each component determined by typical shake flask method and in situ single pass intestinal perfusion model respectively. The results indicated that Gegen Qinlian Tablets should be categorized Ⅳ drug of the CMMBCS with low solubility and low permeability.

关 键 词：葛根芩连片 溶解度 肠渗透性 中药生物药剂学分类系统 

分 类 号：R28[医药卫生—中药学]