UPLC-MS/MS同时测定银丹心脑通软胶囊中7种活性成分及药代动力学研究  

Simultaneous determination of seven bioactive compounds and pharmacokinetics in rat plasma after oral administration of Yindan Xinnaotong Ruanjiaonang by UPLC-MS/MS

作　　者：贡磊磊 原会俊 王岚[1] 殷小杰[1] 许海玉[1] 梁日欣[1] 杨洪军[1] 

机构地区：[1]中国中医科学院中药研究所,北京100700

出　　处：《中国中药杂志》2017年第23期4665-4673,共9页China Journal of Chinese Materia Medica

基　　金：国家"重大新药创制"科技重大专项(2012ZX09201201)

摘　　要：该文采用超高效液相色谱串联质谱(UPLC-MS/MS),建立大鼠血浆中槲皮素(QCT)、山柰酚(KMF)、异鼠李素(ISR)、银杏内酯A(GA)、银杏内酯B(GB)、银杏内酯C(GC)、白果内酯(BB)7种成分的分析方法。同时,探讨单次灌胃给药银丹心脑通软胶囊后上述7种成分在大鼠体内的药代动力学特征。方法学考察结果表明,7种化合物线性关系良好(r≥0.997 1),日内、日间精密度和准确度的RSD均小于11%,基质效应和回收率分别为93.28%~103.6%和72.43%~95.77%,样品室温放置6,12 h,-20℃反复冻存和-20℃长期冻存后基本稳定,其RSD均在11%以下,方法学考察符合生物样品分析要求。大鼠灌胃银丹心脑通软胶囊后,上述7种成分的血浆药代动力学参数如下:Cmax(45.02±11.28),(49.90±13.82),(27.85±8.38),(76.31±18.19),(76.54±15.43),(35.35±10.28),(48.70±12.34)μg·L^(-1);tmax(0.33±0.11),(0.50±0.23),(0.33±0.14),(0.75±0.29),(1.0±0.35),(1.5±0.23),(0.75±0.50)h;该研究建立的UPLC-MS/MS方法适于对大鼠口服银丹心脑通软胶囊后的槲皮素、山柰酚、异鼠李素、银杏内酯A、银杏内酯B、银杏内酯C和白果内酯的药代动力学研究。To estabish ultra-performance liquid chromatography-tandem mass spectrometry （UPLC-MS/MS） method for simultane- ous determination of quercetin （ QCT）, isorhamnetin （ ISR）, kaempferol （ KMF）, ginkgolide A （ GA）, ginkgolide B （ GB ）, ginkgolide C （GC） and bilobalide（BB） in rat plasma and investigate the pharmacokinetic process of seven compounds after oral administration of Yindan Xinnaotong Ruanjiaonang, The results indicated that all calibrations curves showed good linearity （r〉0. 997 1 ）. RSD of intra- day and inter-day precisions were all within 11%. The matrix effects and extraction recovery were in the range of 93.28%-103.6% and72.43%-95.77% respectively. The peak concentration （Cma） of QCT, ISR, KMF, GA, GB, GC and BB were Cmax（45.02±11.28）,（49.90±13.82）,（27.85±8.38）,（76.31±18.19）,（76.54±15.43）,（35.35±10.28）,（48.70±12.34）μg·L^（-1）;tmax（0.33±0.11）,（0.50±0.23）,（0.33±0.14）,（0.75±0.29）,（1.0±0.35）,（1.5±0.23）,（0.75±0.50）h, re- spectively. The peak time （ t ） of seven constituents were （0.33±0.11）,（0.50±0.23）,（0.33±0.14）,（0.75±0.29）,（1.0±0.35）,（1.5±0.23）,（0.75±0.50）h, resoectivelv. UPLC-MS/MS method established in this research was proved to be so rapid andsensitive that it can be applied to the pharmacokinetic study of seven bioactive constituents in Yindan Xinnaotong Ruanjiaonang.

关 键 词：银丹心脑通软胶囊 活性成分 血浆 药代动力学 

分 类 号：R285.5[医药卫生—中药学]