UPLC-MS法研究辛芍提取物的药动学及其绝对生物利用度  

Simultaneous determination of two components of Xin Shao extract in rat plasma by UPLC-MS and their pharmacokinetics and absolute bioavailability

作　　者：郑林[1] 牟景丽[1] 唐丽[1] 刘跃[1] 王爱民[2] 兰燕宇[2] 

机构地区：[1]贵阳医学院药学院,贵州省药物制剂重点实验室,贵阳550004 [2]民族药与中药开发应用教育部工程研究中心,贵阳550004

出　　处：《中国新药杂志》2014年第7期819-823,共5页Chinese Journal of New Drugs

基　　金：国家自然科学基金(81060335;81260636);贵州省社会发展攻关计划(黔科合SY字[2011]3033号);贵州省科学技术基金(黔科合J字[2012]2029号)

摘　　要：目的:建立UPLC-MS同时测定大鼠静脉注射和口服给予辛芍提取物后血浆中野黄芩苷和芍药苷的分析方法,研究2种指标成分在大鼠体内的药动学特征及其绝对生物利用度。方法:采用Waters BEH C18(50 mm×2.1 mm,1.7μm)色谱柱;流速为0.35 mL·min-1;流动相为0.1%甲酸乙腈溶液-0.1%甲酸水溶液,梯度洗脱;质谱采用电喷雾电离源(ESI);扫描方式为选择性离子监测(SIM)。结果:野黄芩苷和芍药苷2种成分呈良好线性关系(r>0.999),提取回收率,精密度、准确度、基质效应和稳定性均良好。静注和口服给药后的野黄芩苷和芍药苷在大鼠体内消除半衰期分别为(0.93±0.85),(9.51±5.43)和(1.16±0.41),(4.59±0.61)h;口服后的达峰时间分别为(9.67±1.51)和(10±1.79)h,峰浓度分别为(1.67±0.81)和(5.59±3.23)mg·L-1。绝对生物利用度分别为26.48%和5.38%。结论:该方法可特异、快速、准确、灵敏地同时测定生物样品中芍药苷、野黄芩苷2种成分的血药浓度,不同给药途径下所检测成分的药动学参数存在一定差异且绝对生物利用度较低。Objective：To develop a sensitive and reliable ultra performance liquid chromatography tandem mass sepctrometry（UPLC-MS）method for simultaneous determination of paeoniflorin and scutellarin in rat plasma，and there by to study their pharmacokinetics in rats. Methods：The two compounds were simultaneously determined by UPLC on C18 column. The mobile phase，consisting of acetonitrile and 0.1% aqueous formic acid，was programmed in a linear gradient mode. The flow rate was 0.35 mL？min－1. The compounds were ionized in the electrospray ionization ion source of the mass spectrometer and detected in SIM mode. Results：The relationships between the concentrations and the peak areas of the two compounds were both linear（r＞0.99）. The precisions，accuracy，extraction recoveries，matrix effects and stability of the analytes all met the requirements. The t1/2z of scutellarin and paeoniflorin after intravenous injection and oral administration were （0.93±0.85），（9.51±5.43） and （1.16±0.41），（4.59±0.61） h, respectively. The Tmax were （9.67±1.51） and （10±1.79） h，Cmax were （1.67±0.81） and （5.59±3.23） mg？L－1, and the absolute bioavailability were 27.94% and 5.38%, respectively. Conclusion：The developed method is simple，rapid，sensitive enough and has been successfully applied to the pharmacokinetic study. The absolute bioavailability of the compounds of interest was low. There exist some differences in the pharmacokinetic parameters after oral administration and intravenous injection. Key words：UPLC-MS；rats；pharmacokinetics；Xin Shao extract；absolute bioavailability

关 键 词：UPLC—MS 大鼠 药动学 辛芍提取物 绝对生物利用度 

分 类 号：R969.1[医药卫生—药理学]