文冠木及复方古日古木-7不同给药方式下主要成分的药代动力学性质  

Pharmacokinetic Properties of Major Bioactive Constituents of Wood of Xanthoceras sorbifolia and A Compound Mongolian Medicine Gurigumu-7 in Different Administration Forms

作　　者：马超美 高杰 许海燕 武丹丹 叶日贵 OlusegunS.Ajala MA Chao-mei;GAO Jie;XU Hai-yan;WU Dan-dan;YE Ri-gui;Olusegun S.Ajala(Key Laboratory of Herbage and Endemic Crop Biotechnology,School of Life Sciences, Inner Mongolia University,Hohhot 010070,China;School of pharmacy,Inner Mongolia Medical University,Hohhot 010110,China;Department of Pharmaceutical Chemistry,The University of Lagos,Lagos,Nigeria)

机构地区：[1]内蒙古大学生命科学学院/牧草与特色作物生物技术教育部重点实验室,内蒙古呼和浩特010070 [2]内蒙古医科大学药学院,内蒙古呼和浩特010110 [3]拉各斯大学药学院,尼日利亚拉各斯

出　　处：《中国现代中药》2020年第2期305-310,共6页Modern Chinese Medicine

基　　金：国家自然科学基金项目(81660711)。

摘　　要：本文综述分析文献报道的文冠木及蒙药复方古日古木-7(G-7)主要成分的药代动力学性质等数据,探讨水煎剂和散剂(或甲醇提取物)可吸收成分的差异及原理。G-7含红花、石膏、麻黄、紫花地丁、诃子、蓝盆花、木通。其中诃子含有大量多酚成分,有抗丙肝病毒蛋白酶等活性。给药G-7后诃子主要成分的血药浓度-时间曲线下面积(AUC0~10 h)比单独给药诃子时明显增加。没食子酸、诃子裂酸、诃黎勒酸的AUC0~10 h分别增加了2.6、10.3、3.0倍,说明G-7中其他药材可增加诃子主要活性成分的吸收。给大鼠灌胃G-7甲醇提取物后,极性较小的鞣花酸的AUC0~10 h>没食子酸,而灌胃水煎剂时极性大的没食子酸的AUC0~10 h>鞣花酸。文冠木不能被溶剂提取出的大分子鞣质可被胃液降解成其组成单元——表儿茶素;灌胃文冠木全粉时表儿茶素的AUC0~10 h和最大血药浓度(Cmax)明显增加,分别达到灌胃其提取物时的1.1和1.2倍。甲醇提取物(或中药全粉的散剂)给药后,亲脂性及不可提取成分的体内吸收较多,因此,民族药散剂的体内药效物质与水煎剂有所不同,这可能是有些药材在民族医药与中医药中用途不同的科学原理;这些结果也提示,民族药散剂的主要质量控制指标成分也会与汤剂有所不同。This paper reviews and analyzes,the pharmacokinetic properties of the major constituents of a Mongolian compound medicine Gurigumu-7(G-7)and a medicinal material Xanthoceras sorbifolia wood,and discusses the differences between the absorbable constituents of water decoction and powder(or methanol extract).Terminalia chebula fruit which is one of the 7 medicinal materials in G-7 contains polyphenol constituents that inhibit hepatitis C protease.After administration of G-7 to rats,the major bioactive constituents displayed area under the concentration-time curve(AUC0-10 h)values larger than those administrated of T.chebula fruit alone.The AUC0-10 h values of gallic acid,chebulic acid,and chebulagic acid increased 2.6,10.3,and 3.0 times,respectively,indicating that the other medicinal materials in G-7 improved the absorption of T.chebula constituents.After gavaging to rats of G-7 methanol extract,the AUC0-10 h value of ellagic acid which was more lipophilic than gallic acid was larger than that of gallic acid,while gallic acid showed larger AUC0-10 h value than ellagic acid when G-7 decoction was gavaged to rats.The macromolecular tannins which could not be extracted by solvent in X.sorbifolia degraded into epicatechin by gastric juice.The AUC0-10 h value and Cmax of epicatechin after administration of X.sorbifolia wood powder were significantly higher(1.1 and 1.2 times)than those after administration of X.sorbifolia wood extract.Lipophilic and insoluble components were absorbed in larger amounts after administration of the plant powder than administration of the plant extract.Therefore,the pharmacodynamic substances of ethnic medicinal plant powder are different from those of decoction.This might be part of the scientific reasons that ethnic medicinal systems in which plant powders are often administrated directly use some medicinal plants for diseases different from TCM uses for.The study also suggested that the main quality control indicators of ethnic medicinal plant powder were different from those of decoction

关 键 词：民族药散剂 药代动力学 药效物质基础 脂溶性成分 难提取成分 

分 类 号：R284[医药卫生—中药学] R285[医药卫生—中医学]