单向在体肠灌流在中药研究中的应用

化合物的溶解性和渗透性在评价候选药物的口服吸收及生物药剂学分类系统占有重要地位,基于中药多成分特点,所提出的中药生物药剂学分类系统更适用于中药成分的研究。谱效相关技术的普及为寻找中药药效物质成分提供了新方法,而以肠吸收谱为切入点,避免了血清谱复杂的体内分布、代谢过程带来的难题,且不易遗漏不吸收的有效组分,更加简便,更适用于复方药效物质基础的研究。单向在体肠灌流模型是公认的研究药物在体吸收的模型,在一定程度上准确模拟了口服药物的在体吸收,联用运用肠系膜取血等技术,可较为真实反映成分吸收入血情况,更加适用于中药生物药剂学分类系统及谱效相关的研究,值得注意的是,单向在体肠灌流实际上反映的是各组分表观吸收,欲进一步了解其吸收机制,还需结合单个药物、成分的单向肠灌流研究及在体吸收研究。在单一成分研究的基础上,再对其多成分环境下的特征和规律进行研究,回归到以中药或复方为整体的研究中去。近年来,单向在体肠灌流在中药研究中应用越来越多。查阅近20年文献,对筛选出用于中药研究的200多篇文献进行分析,结合课题组经验,总结其在中药有效成分、单味药、药对、复方研究中的应用及使用时的注意事项,为其在中药研究中的进一步应用提供参考。

Application of Single-pass Intestinal Perfusion Technique in Traditional Chinese Medicine

Compound solubility and permeability play an important role in evaluating oral absorption of drug candidates as well as their Biopharmaceutics Classification System(BCS). Based on the characteristics of multicomponent of traditional Chinese medicine(TCM), the BCS of Chinese materia medica(CMMBCS) is more suitable for TCM research. The popularization of the spectral correlation technique provides a new method for finding the active ingredients of TCM. Taking intestinal absorption spectrum as the breakthrough point, it avoids the problems of the complex distribution of serum spectrum, as well as the metabolic process, and is not easy to omit the non-absorbent effective components, which is more convenient and more suitable for the study. The single-pass intestinal perfusion(SPIP) model is generally recognized as the model for in situ drug absorption study, which is able to correctly simulate the in situ absorption conditions of oral drugs. Combined with mesenteric blood taking method, it can reflect the actual composition absorption into the blood, more suitable for the study of CMMBCS and spectrum efficiency. However, SPIP actually reflects the apparent absorption of each component in compound, and a single composition of SPIP and in vivo absorption research should be combined for further absorption mechanism. It is necessary to study the absorption characteristics in multicomponent environment on the basics of single component research, and then return to TCM or compound for the whole research. In recent years, SPIP has been widely used in TCM research. In the literatures of recent 20 years, more than 200 articles were analyzed to summarize its applications in TCM, and combined with the experience of research team, it could be used to summarize the effective components, single herb, pair-herb compatibility, application in Chinese medicine compound, and the notice items in use, in order to provide reference for further application in TCM research.