通脉丸有效组分配伍浓缩液在大鼠体内的毒代动力学研究  

Toxicokinetics of Tongmai Pills and the Effectiveness of Its Combination Components Concentrate in Rats

作　　者：陈天朝[1] 刘瑞霞[2] 于兰兰[2] 

机构地区：[1]河南中医学院第一附属医院,郑州450000 [2]河南中医学院药学院,郑州450008

出　　处：《世界科学技术-中医药现代化》2016年第5期868-874,共7页Modernization of Traditional Chinese Medicine and Materia Medica-World Science and Technology

基　　金：河南省教育厅科技攻关项目(2011A360003):基于系统论通脉丸减毒机制的研究;负责人:陈天朝;河南省教育厅重点项目(13A350597):基于药辅统一的中药丸剂释药机制研究;负责人:陈天朝

摘　　要：目的:本研究通过通脉丸方中各味中药有效组分提取液的不同配伍,研究其内部的减毒机制,为其安全性评价提供依据。方法:分别灌胃给予大鼠8组通脉丸有效组分不同配伍浓缩液,采用UPLC检测给药后不同时间点大鼠体内士的宁的血药浓度,应用SPSS软件拟合毒代动力学参数。结果:士的宁在大鼠体内符合非房室模型,第1-8组毒代动力学参数AUC(0-t)分别为10.271 9±3.224 7、8.806 1±1.245 8、13.496 6±4.582 5、11.031 5±2.873 2、9.929 1±1.499 7、5.042 0±2.171 2、15.136 2±6.353 3、5.751 5±1.492 8μg·h·m L-1。通脉丸原方与其余配伍方在大鼠体内产生的毒性不同,AUC减少率大小顺序为第6组>第8组>第2组>第5组>第1组>第4组>第3组>第7组,"丹参、赤芍、琥珀、蜂蜜"减毒作用最强。结论:UPLC分析方法适用于大鼠血浆士的宁的测定。This study aimed to investigate the mechanism of internal attenuation and provide references for safety evaluation by extracting effective components from the Chinese herbs of Tongmai pills. Rats were dividedinto eight groups and intragastrically administered with the concentrated decoction of the Tongmai prescription. Serum strychnine levels of all groups were detected by UPLC at various time points after administration. At last, its fitting parameters in toxicokinetic were calculated using SPSS software. It was found that the parameters of serum strychnine in rats fitted with the non-compartmental model with the AUC（0-t） outputs as follows： 10.271 9±3.224 7,8.806 1±1.245 8,13.496 6±4.582 5,11.031 5±2.873 2,9.929 1±1.499 7,5.042 0±2.171 2,15.136 2±6.353 3,5.751 5±1.492 8 μg·h·m L-1. Different toxicities between the concentrated decoction from Tongmai pills（group 1） and other decoctions consisting of the some herbs in Tongmai pills（group 2-group 8） were showed in this study with the AUC outputs ranging from the most to the least as follows： group 6, group 8, group 2, group 5, group 1, group 4, group 3 and group 7. So the decoction with salvia, red peony, amber and honey presented the strongest toxicity attenuated effect. In conclusion, it was demonstrated that UPLC worked well in determining serum strychnine of rats.

关 键 词：配伍减毒 士的宁 毒代动力学 药动学参数 

分 类 号：R285[医药卫生—中药学]