葛根芩连复方环境中黄芩素的中药生物药剂学分类系统属性研究  

Research on attributes of biopharmaceutics classification system for Chinese materia medica of baicalein in Gegen Qinlian Decoction environment

作　　者：刘洋[1] 杨丽[1] 张鑫[1] 程亚茹 龚燚婷 董玲[1] LIU Yang;YANG Li;ZHANG Xin;CHENG Ya-ru;GONG Yi-ting;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3653-3661,共9页China Journal of Chinese Materia Medica

基　　金：国家自然科学基金项目(81473362)

摘　　要：针对复方多成分环境对单一成分溶解度、渗透性影响及单成分在复方环境下的中药生物药剂学属性分类问题,该文以黄芩素为研究对象,考察单成分生物药剂学属性及其在葛根芩连汤多成分环境下的中药生物药剂学属性。通过经典摇瓶法、特性溶出速率试验和高效液相色谱法研究黄芩素单成分及其在复方中的溶解度,通过美国食品药品监督管理局(FDA)规定的渗透性边界的标准物质对在体单向肠灌流进行模型验证,并对黄芩素的渗透性做定量研究。最终得出黄芩素单成分为低溶解性高渗透性的BCS-Ⅱ类,其在葛根芩连复方环境中可能归属于自身溶解性差但在复方环境下提升较好和渗透性好在复方环境下提升良好的CMMBCS-Ⅰ类。该研究可为临床确定黄芩素的最佳人体口服剂量提供验证思路,同时为中药生物药剂学分类系统的研究提供数据基础。For the effects of multi-component environment on the solubility and permeability of single components,and the problems of biopharmaceutical attribute classification of single components in the compound prescriptions environment,baicalein was used as the research object in this study to investigate the biopharmaceutic attributes of single-component and their traditional Chinese medicine( TCM) biopharmaceutic attributes in the multi-component environment of Gegen Qilian Decoction. Shaking flask method,intrinsic dissolution rate test and HPLC were used to determine solubility of baicalein. Markers specified by FDA were utilized as permeable boundary reference materials to verify the applicability of the single-pass intestinal perfusion method( SPIP),and the quantitative research on the permeability of baicalein was also conducted. It is concluded that baicalein could be categorized as BCS-Ⅱ drug based on its low solubility and high intestinal permeability values,and it may be categorized into CMMBCS-I in the multi-component environment of Gegen Qilian Decoction due to its poor solubility but enhanced solubility and permeability in compound environment. This study could provide verification ideas for clinical determination of the best human oral dose of baicalein,and provide the data basis for the study of biopharmaceutics classification system of Chinese materia medica( CMMBCS).

关 键 词：黄芩素 溶解性 渗透性 单向肠灌流 中药生物药剂学分类系统 

分 类 号：R28[医药卫生—中药学]