中药渗透性规律及其评价研究进展  

Research progress on permeability characteristics of Chinese materia medica and evaluation approaches

作　　者：许敏[1,2] 姜壮壮 陶丽 刘延庆[1,2] XU Min;JIANG Zhuang-zhuang;TAO Li;LIU Yan-qing(College of Medicine, Yangzhou University, Yangzhou 225000, China;Key Laboratory of Toxic Pathogens-Based Therapeutic Approaches of Gastric Cancer, State Administration of TraditionalChinese Medicine, Yangzhou 225000, China)

机构地区：[1]扬州大学医学院,江苏扬州225000 [2]国家中医药管理局胃癌毒邪论治重点研究室,江苏扬州225000

出　　处：《中草药》2019年第14期3477-3483,共7页Chinese Traditional and Herbal Drugs

基　　金：国家自然科学基金面上项目(81773944);国家自然科学基金青年基金(81803782);江苏省自然科学基金青年基金(BK20170516);中国博士后科学基金资助项目(2017M611936);江苏省博士后科研资助计划(1701185B);扬州大学科技创新培育基金资助项目(2017CXJ102);扬州大学研究生实践创新计划(XSJCX18_080)

摘　　要：中药血清药理学通过从正常与疾病模型动物血清中分离、鉴定血清移行成分从而寻找药效物质基础,此方法存在一定局限性。大部分中药药效成分在生物药剂学分类系统中属于低溶解-低渗透性药物,生物利用度低但生物效应高,血清药理学不能评价非血清移行成分的功效关联规律。基于中药化学成分的复杂性,中药成分的渗透性相互作用可能影响各自的渗透性行为,形成不同的口服吸收处方。因此中药成分的渗透性尤其是多组分共存条件下的中药渗透性规律研究是解决中药功效物质基础问题值得探索的方向之一。首先概述了中药肠渗透与跨生物屏障渗透性评价的体内外实验模型及其各自的应用价值;然后探讨了常见中药活性成分的结构与渗透动力学的关系,特别是中药渗透性研究的定量构动关系研究;最后基于渗透性实验模型与构动关系研究,评述近年来关于中药多组分渗透动力学规律及其渗透机制研究进展,发现中药化学成分之间可以通过促进药物转运或者形成离子配伍而影响成分间的渗透吸收,以期为寻找和预测复杂化学成分的中药渗透性规律研究及成分间相互作用机制研究提供一定的参考与借鉴。The research methods of serum pharmacology and serum biochemistry of traditional Chinese medicine isolate and identify serum transitional components from the serum of normal and disease model animals in order to find the material basis of pharmacodynamics. There are some limitations in this method for identifying the components of traditional Chinese medicine to play its pharmacological activities. Most active ingredients of traditional Chinese medicine belong to low-solubility and low-permeability drugs in the classification system of biopharmaceutics. Their bioavailability is low, but their overall biological effects are high. The classical pharmacokinetic-pharmacodynamic theory of serum pharmacology can not explain and evaluate the pharmacological effects of their non-serum transitional components. Based on the complexity of the chemical components of traditional Chinese medicine, the osmotic interaction of traditional Chinese medicine components may affect their osmotic behavior and form different oral absorption prescriptions. Therefore, the study on the permeability of traditional Chinese medicine components, especially under the condition of multi-component coexistence, is one of the topics worth to solve the problem of the functional substance basis of traditional Chinese medicine. This paper first outlines the in vitro and in vivo screening experimental models and their respective application value for the evaluation of intestinal permeability and trans-biological barrier permeability of traditional Chinese medicines. Then, the advantages and disadvantages of each model are compared, and the relationship between the structure and osmotic kinetics of common active components of traditional Chinese medicines based on osmotic model is discussed, especially the research progress of quantitative structure-kinetics relationship in permeability study of traditional Chinese medicines. Finally, based on the relationship between permeability experimental model and structure-kinetics, the recent progress in the stu

关 键 词：中药渗透性 渗透模型 定量构动关系 肠渗透模型 渗透相互作用 

分 类 号：R285.61[医药卫生—中药学]