【作者】 冯年平； 狄斌； 刘文英；

【Author】 Nian-Ping Feng1, Bin Di2 and Wen-Ying Liu2 1 Shanghai University of Traditional Chinese Medicine, Shanghai 201203, P. R. China 2 China Pharmaceutical University, Nanjing 210009, P. R. China

【机构】 上海中医药大学； 中国药科大学；

【摘要】 中药配伍与其体内代谢特征之间存在着一定的对应关系,即中药配伍-代谢关系。本文以双黄连复方为实例,用LC-DAD和LC/MSn等测试手段,通过对双黄连复方和黄芩单方中主要药效成分黄芩苷在大鼠体内的代谢产物,以及灌胃给予不同组合方后黄芩苷的药代动力学的研究,初步揭示了中药配伍-代谢关系。中药配伍-代谢关系的研究对阐明中药配伍原理和作用机制、改革中药剂型、开发现代新中药以及制订中药制剂科学的质量标准等方面都有重要意义。更多还原

【Abstract】 The hypothesis of compatibility-metabolism correlation is proposed. There exists a correlation between compatibility of TCM compound prescriptions and the metabolic characteristics of their active ingredients. In order to verify the hypothesis, the Shuang-Huang-Lian (SHL) compound recipe, a traditional Chinese formula containing Flos lonicerae(FL),Radix scutellariae(RS) and Fructus forsythiae(FF), and is commonly used for treating acute upper respiratory tract infection, acute bronchitis and light pneumonia, was taken for an example. Modern instrumental techniques, LC-MSn and HPLC-DAD, were mainly used to analyze the metabolites of baicalin in the SHL and one-herb Radix scutellariae(RS) in rat bile, urine and faces, and the pharmacokinetics of SHL and the different combinations of its constitutional herbs (RS+FF, RS+FL and RS) were also investigated after orally administered. Male Sprague-Dawley rats were randomly assigned to four groups and orally administered with SHL, RS, RS+FF and RS+FL, respectively. At different time points after administration, the concentrations of baicalein in rat serum were determined and main pharmacokinetic parameters were estimated. The results indicated that the change of compatibility leaded directly to the change of the in vivo metabolites of baicalin, and there were significant differences (p<0.05) in the parameters, t1/2(β) and Cmax among different combinations of herbs. Results indicated that SHL delayed the elimination and reduce the bioavailability of baicalein in rat serum. The hypothesis of compatibility-metabolism correlation is of great significance to explain the principles of the compatibility and the acting mechanisms of TCM compound prescriptions, to develop new dosage forms and modern TCM new drugs, and to establish scientific quality standards for TCM preparations. The differences of compatibility of traditional Chinese medicines can result in the differences of metabolism characteristics.更多还原