基于“双态”在体肠循环灌流模型研究隔山消提取物肠吸收特性差异  

Differences in intestinal absorption characteristics of Cynanchum auriculatum extract based on in situ intestinal circulation perfusion model in two states

作　　者：孙佳[1] 刘利琴 勾健 陈思颖[1] 巩仔鹏[1] 刘亭[2] 李勇军[2] 陆苑[1] SUN Jia;LIU Li-qin;GOU Jian;CHEN Si-ying;GONG Zi-peng;LIU Ting;LI Yong-jun;LU Yuan(Provincial Key Laboratory of Pharmaceutics in Guizhou Province,State Key Laboratory of Functions and Applications of Medicinal Plants,Guizhou Medical University,Guiyang 550004,China;Engineering Research Center for the Development and Application of Ethnic Medicine and Traditional Chinese Medicine(Ministry of Education),Guizhou Medical University,Guiyang 550004,China;School of Pharmaceutical Sciences,Guizhou Medical University,Guiyang 550004,China)

机构地区：[1]贵州医科大学、贵州省药物制剂重点实验室、省部共建药用植物功效与利用国家重点实验室,贵州贵阳550004 [2]贵州医科大学民族药与中药开发应用教育部工程研究中心,贵州贵阳550004 [3]贵州医科大学药学院,贵州贵阳550004

出　　处：《中国中药杂志》2022年第23期6340-6347,共8页China Journal of Chinese Materia Medica

基　　金：国家自然科学基金项目(81760700);贵州省中医药管理局中医药、民族医药科学技术研究课题(QZYY-2021-087);贵州医科大学博士启动基金项目(校博合J字[2020]013号)。

摘　　要：该文旨在考察隔山消提取物中6个成分(丁香酸、东莨菪内酯、白首乌二苯酮、告达亭、青阳参苷元和去酰基萝藦苷元)的肠吸收特性。采用在体肠循环灌流模型,研究“双态”即正常与功能性消化不良(FD)模型状态下,隔山消提取物中丁香酸等成分在不同肠段、不同药物浓度及胆汁影响下的肠吸收差异。结果表明,随着浓度的增加,白首乌二苯酮的吸收显著降低(P<0.01),丁香酸等成分的吸收不呈剂量依赖性增加,提示白首乌二苯酮可能为主动吸收过程,其他成分可能并非单纯的一种吸收方式;正常与FD模型状态下各成分的主要吸收部位不同,FD模型状态下的累积吸收转化率总体上低于正常状态下的累积吸收转化率;除东莨菪内酯外,胆汁对“双态”下的青阳参苷元等成分的吸收均具有显著抑制作用(P<0.05)。可见小肠对药物的吸收具有选择性,FD病理状态和胆汁对主要成分的吸收均有影响,这为隔山消创新药物研制及药材资源深度开发提供了理论依据。The present study aimed to investigate the intestinal absorption characteristics of six components(syringic acid,scopoletin,baishouwu benzophenone,caudatin,qingyangshengenin,and deacylmetaplexigenin)in Cynanchum auriculatum extract.In situ intestinal circulation perfusion model was employed to investigate the differences in intestinal absorption characteristics of C.auriculatum extract under the influence of different intestinal segments,different drug concentrations,and bile in the normal and functional dyspepsia(FD)states.The results showed that the absorption of baishouwu benzophenone decreased with the increase in the concentration of C.auriculatum extract(P<0.01),while the absorption of syringic acid and other components increased in a dose-independent manner,suggesting that baishouwu benzophenone might follow active absorption,while other components might not be on a single absorption pattern.The main absorption sites of each component in the normal state were different from those in the FD state.The cumulative absorption conversion rates in the FD state were generally lower than those in the normal state,and bile inhibited the absorption of other components except for scopoletin in both states(P<0.05).As revealed,the small intestine showed selectivity to the absorption of drugs,and the pathological state(such as FD)and bile both affected the absorption of the main components,which provides a theoretical basis for the development of new drugs and further development of C.auriculatum.

关 键 词：隔山消 “双态” 在体肠循环灌流模型 肠吸收 差异 

分 类 号：R285.5[医药卫生—中药学]