鹿茸断续膏中柚皮苷的小鼠体内药代动力学研究和血中代谢产物鉴定  

Pharmacokinetics Study and the Identification of Metabolites in Mice Plasma of Naringin from Lurong Duanxu Gao

作　　者：李婷 王佳[1] 杨苗[1] 王云华[1] 刘继华[1] LI Ting;WANG Jia;YANG Miao;WANG Yun-hua;LIU Ji-hua(Pharmacy of School,Jilin University,Changchun 130021,China)

机构地区：[1]吉林大学药学院,吉林长春130021

出　　处：《中药材》2018年第4期966-969,共4页Journal of Chinese Medicinal Materials

基　　金：吉林省重点科技攻关项目(20150204037YY)

摘　　要：目的:建立超高效液相色谱-串联质谱法测定给予小鼠鹿茸断续膏后,血清中柚皮苷的药代动力学及代谢产物。方法:以UPLC-QTOF-MS检测小鼠血清中柚皮苷的浓度,流动相为乙腈-水梯度洗脱,经BEH-C_(18)色谱柱(2.1 mm×50 mm,1.7μm),流速0.4 mL/min,柱温40℃。质谱条件:电喷雾离子源(ESI);正离子扫描模式。代谢产物检测以MSE检测模式,UNIFI软件处理数据,鉴定柚皮苷的血中代谢物,分析代谢过程。结果:本法专属性好,柚皮苷在0.06～2.68μg/mL的范围内线性关系良好,准确度与精密度符合要求。检测得到给予鹿茸断续膏后血中柚皮苷的血药浓度-时间曲线,以及药代动力学参数,UNIFI软件分析鉴定出血中柚皮苷代谢物8个。结论:本法经方法学验证,适用于血样中柚皮苷的定量检测。研究结果显示,贴膏剂中的柚皮苷成分进入血中达峰时间为4 h,半衰期为19 h,血药浓度上升及降低都较缓慢,药效维持时间较长,在血中代谢过程以脱糖、加水和加氢为主要代谢过程。Objective:To determine the pharmacokinetics and metabolism of naringin from Lurong Duanxu gao induced mice in serum after plaster administrationby ultra performance liquid chromatography tandem mass spectrometry(UPLC-QTOF-MS).Methods:The concentration of naringin in mouse serum was determined by UPLC/MS-QT OF,and the mobile phase was eluted by acetonitrile-water gradient.The column was BEH-C18(50 mm×2.1 mm,1.7 μm),the flow rate was 0.4 mL/min,and column temperature was 40 ℃.Mass spectrometry conditions was electrospray ion source(ESI)with positive ion scanning mode.Metabolites were detected by MSE detection mode,and UNIFI software was used to identify the metabolites of naringin in plasma.Results:The specificity of this method was good.The calibration cruve was linear over the concentration range of 0.06~2.68 μg/mL.Accuracy and precision conformed the requirement.The plasma concentration-time curve and pharmacokinetic parameters of naringin were detected,and eight metabolites of naringin in plasma were identified by UNIFI software.Conclusion:The results show that this method is suitable for the quantitative detection of naringin in a blood sample.This study indicates that the concentration of naringin in blood comes to a peak after plaster administration at 4 h,and the IC50 is 19 h,the concentration of naringin in plasma increases and decreases lowly in this period,the efficacy maintaines for a long time relatively,the desugar,hydration,and hydrogenation are the main metabolic processes in blood.

关 键 词：鹿茸断续膏 柚皮苷 药代动力学 代谢产物 

分 类 号：R285.5[医药卫生—中药学]