基于UPLC/TOF-MS的双龙方大鼠体内药代动力学研究  

Pharmacokinetics research of Shuanglong Formula in rats based on UPLC/TOF-MS

作　　者：王佩瑶[1,2] 陈曦[2,3] 孟宪生[1] 王勇[2] 梁琼麟[2] 王义明[2] 罗国安[2] 

机构地区：[1]辽宁中医药大学,辽宁大连116600 [2]清华大学化学系,北京100084 [3]中国医学科学院药用植物研究所,北京100193

出　　处：《中成药》2011年第11期1889-1895,共7页Chinese Traditional Patent Medicine

基　　金：国家"新药创制"重大专项基金(2008ZX09202);国家"十一五"科技支撑计划项目(2006BAI08B0401)

摘　　要：目的研究双龙方(人参、丹参)在大鼠体内的药代动力学规律。方法利用UPLC/TOF-MS进行血清样品分析,考察了双龙方中人参皂苷、丹参酚酸两大类物质在大鼠体内的药代动力学参数,主要包括房室模型,小分布容积、曲线下面积、达峰时间和峰浓度。结果除Rb2和M-Rb1符合二室模型外,双龙方中其它人参皂苷和丹参酚酸类化合物均满足一室模型;测定了双龙方中丹参素、丹参酚酸G、丹参酚酸K、丹参酚酸M、人参皂苷Rb1、Rb2、Rc、Rd、M-Rb1、M-Rd的小分布容积、曲线下面积、达峰时间、峰浓度等药代动力学参数,并绘制了药时曲线。结论明确了双龙方中人参皂苷、丹参酚酸两大类物质在大鼠体内的生物转化规律;丹参酚酸与人参皂苷协同作用,有助于维持药物的有效浓度,延长其有效作用时间;临床上使用双龙方时,每隔8 h服用一次即可维持所需药效浓度。AIM To study pharmacokinetic behavior of Shuanglong Formula（Ginseng radix et rhizoma,Salviae miltiorrhizae radix et rhizoma） in rats.METHODS UPLC/TOF-MS was applied in sample analysis.The pharmacokinetics parameters of ginsenosides and salvianolic acids in Shuanglong Formula were studied,mainly including compartmental model,volume of distribution（Vd/F）,area under the curve（AUC0-∞）,time to peak（Tmax） and peak concentration（Cmax）.RESULTS Most of ginsenosides and salvianolic acids compounds of Shuanglong Formula fitted to one compartment model except M-Rb1 and Rb2.The Vd/F,AUC0-∞,Tmax,Cmax of tanshinol,salvianolic acid G,salvianolic acids K,salvianolic acids M,Rb1,Rb2,Rc,Rd,M-Rb1,M-Rd were assayed and the concentration-time curve was obtained.CONCLUSION The biotransformation rule of ginsenosides and salvianolic acids in Shuanglong Formula in rats is identified： The synergistic reaction between ginsenosides and salvianolic acids is good for keeping the effective concentration and extending the effective duration of action.Additionally,it is effective in dose of Shuanglong Formula administered at 8 hour intervals.

关 键 词：双龙方 人参皂苷 丹参酚酸 药代动力学 UPLC/TOF-MS 大鼠 

分 类 号：R944.27[医药卫生—药剂学]