诃子制草乌模拟炮制品在人工胃液与肠液中的水解行为研究  

Hydrolysis of Simulation Processing Products of Aconitum kusnezoffii Processed with Terminalia chebula in Simulated Gastric Fluid and Intestinal Fluid

作　　者：刘帅[1] 刘晓艳[1] 林森[1] 杨畅[1] 李飞[1] 杜红[1] 

机构地区：[1]北京中医药大学中药学院,北京100029

出　　处：《中国药房》2015年第13期1752-1754,共3页China Pharmacy

基　　金：国家自然基金资助项目(No.81102815;81102807);高等学校博士学科点专项科研基金(No.20110013120017)

摘　　要：目的：研究诃子制草乌模拟炮制品在人工胃液与肠液中的水解行为,明确二者相互作用机制,为诃子制草乌的炮制减毒提供依据。方法：采用高相液相色谱（HPLC）法测定诃子制草乌在人工胃肠液中孵育不同时间（胃液中孵育2 h,肠液中孵育5、6、7、8 h）后其降解产物乌头碱、苯甲酰乌头原碱和苯甲酸的含量。结果：诃子制草乌中乌头碱含量在人工胃液中减少,在人工肠液中明显回升,在人工肠液孵育6~8 h时含量稳定;诃子制草乌中苯甲酰乌头原碱在人工胃液中未测得,在人工肠液中测得;诃子制草乌中苯甲酸在人工胃肠液中含量变化呈先递增再递减的趋势,且在人工肠液中孵育6 h时达最大值,7~8 h时维持稳定。结论：诃子制草乌炮制过程中鞣质与乌头碱可能结合生成难溶性物质,胃肠液p H对游离乌头碱的释放和水解有一定影响,人工胃液酸性环境对其水解有抑制作用,而人工肠液碱性环境对其水解有促进作用。OBJECTIVE： To study the hydrolysis of simulation processing products ofAconitum kusnezoffii processed with Ter- minalia chebula in simulated gastric fluid and intestinal fluid, identify the mechanism of interactions of both and provide a basis for preparing A. kusnezoffii processed with T. chebula and reducing its toxicity. METHODS： After A. kusnezoffii processed with T. cheb- ula was incubated in simulated gastric fluid and intestinal fluid for different periods of time （2 h in gastric fluid and 5, 6, 7 and 8 h in intestinal fluid）, HPLC was adopted to determine the content of aconitine, benzoylaconine and benzoic acid. RESULTS, The content of aconitine in A. kusnezoffii processed with T. chebula was decreased in the simulated gastric fluid, but obviously increased in the simulated intestinal fluid and had stable content after incubation in the simulated intestinal fluid for 6-8 h. No benzoylaconine was detected in the simulated gastric fluid, but it was found in the simulated intestinal fluid. The content of benzoic acid in the sim- ulated gastric fluid tended to increase followed by decrease, got largest value after incubation in the simulated intestinal fluid for 6 h and maintained stable at 7-8 h. CONCLUSIONS： During the preparation ofA. kusnezoJfii processed with T. chebula, tannins may combine with aconitine to form insoluble substances. The pH of gastric and intestinal fluid has certain effect on the release and hy- drolysis of free aconitine, the acidic environment of simulated gastric fluid has inhibition effect on the hydrolysis and the alkaline has promoting effect.

关 键 词：诃子制草乌 鞣质 乌头碱 模拟炮制 人工胃液 人工肠液 体外代谢 

分 类 号：R283.2[医药卫生—中药学]