双黄连口服液中有效成分的大鼠在体肠吸收研究  

Study on in situ intestinal absorption of active ingredients in Shuanghuanglian oral liquid in rats

作　　者：周伟[1] 狄留庆[1] 毕肖林[1] 陈乐天[1] 杜秋[1] 

机构地区：[1]南京中医药大学药学院南京市中药微丸产业化工程技术研究中心,江苏南京210046

出　　处：《中国中药杂志》2011年第13期1733-1738,共6页China Journal of Chinese Materia Medica

基　　金：江苏省中医药局项目(HZ07051);江苏省"青蓝工程"科技创新团队支持计划[苏教师(2008)30号]

摘　　要：目的:研究双黄连口服液中黄芩苷、绿原酸、连翘苷、连翘酯苷A 4种主要有效成分在大鼠肠吸收动力学特征,了解双黄连口服液中药物配伍对其主要有效成分吸收的影响。方法:运用在体肠循环模型,研究比较双黄连口服液与其4种有效成分在体肠循环过程中的浓度变化的差异。结果:黄芩苷、绿原酸、连翘苷、连翘酯苷A分别在40～160,6～24,3～12,2.6～10.4 mg.L-1吸收量与浓度呈线性关系,无高浓度饱和现象,吸收转化速率常数Ka,单位时间百分吸收转化率A基本保持不变;除黄芩苷、绿原酸、连翘酯苷A外,在pH 5.0～7.43,连翘苷的吸收不受pH影响;4种成分在各肠段的Ka,A均无明显差异。黄芩提取液中的黄芩苷、金银花提取液中的绿原酸、连翘提取液中的连翘苷的Ka,A与双黄连口服液中相应成分的Ka,A相比,无显著性差异;但连翘提取液中的连翘酯苷A的Ka,A显著大于双黄连口服液中相应成分的Ka,A。结论:双黄连口服液中黄芩苷、绿原酸、连翘苷、连翘酯苷A在大鼠小肠主要以被动扩散方式吸收,且无特殊的吸收窗;双黄连口服液组方配伍显著改变了连翘酯苷A的吸收。Objective： To study the intestinal absorption kinetics characteristic of the main four active ingredients in Shuanghuanglian oral liquid（SHL） and to investigate the influence of herbal compatibility in SHL on absorption of main effective ingredients.Method： The in situ rat circulation model was used to investigate the concentration change differences of the four active components in SHL during perfusion.Result： The absorption quantity of different concentrations of baicalin,chlorogenic acid,phillyrin and forsythoside A ranging from 40-160,6-24,3-12,2.6-10.4 mg·L-1 respectively was linear with concentration and showed no saturation at high concentration.The absorption rate constant Ka and the hourly absorption percentages A were essentially unchanged.The pH changing from 5.0-7.43 had little influence on the absorption of phillyrin except baicalin,chlorogenic acid and forsythoside A.The calculated Ka and A of the four active ingredients had no significant differences from that obtained after perfusing via duodenum,jejunum,ileum and colon;The calculated Ka and A of baicalin in Scutellariae Radix（SR）,chlorogenic acid in Lonicerae Japonicae Flos（LJF） and phillyrin in Forsythiae Fructus（FF） had no significant differences compared with that in SHL,but the calculated Ka and A of forsythoside A in FF were obviously superior to that in SHL.Conclusion： The intestinal absorption of the four active ingredients in SHL was mainly passive diffusion and had no difference in different segments of rat intestine;the compatibility of SHL compounds changed the absorption of forsythoside A in FF obviously.

关 键 词：双黄连口服液 黄芩苷 绿原酸 连翘苷 连翘酯苷A 肠吸收 

分 类 号：R286.0[医药卫生—中药学]