大鼠血浆中雌二醇的柱前衍生化LC-MSMS法测定及其药动学应用.pdfVIP

• 750 • 中国医药工业杂志 Chinese Journal of Phannaceuticals 2014，崎(8) 〈药理与临床3 大鼠血浆中雌二醇的柱前衍生化LC-MS瓜1S 法测定及其药动学应用 台软，周臻，罗华菲，李周，葛庆华* (中国医药工业研究总院上海医药工业研究院，药物制剂国家工程研究中心，上海 201203) 摘要:建立了柱前衍生化液相色谱·串联质谱法测定血浆中的雌二醇。以雌二醇 -d 为内标，采用 C8 色谱柱，血浆样品 3 经液-液萃取、柱前衍生化处理后，采用 ESI 离子源，多反应离子监测 (MRM) ，正离子扫描，进行测定。结果表明，雌 二醇在 50 ~ 10 000 pglml 浓度范围内线性关系良好，方法回收率为 94.0%~ 107.2% , RSDlO.O% 。同时测定了雌性大 鼠体内雌二醇基础值和给予雌二醇透皮贴剂后的血药浓度。结果显示本法灵敏度高、重现性好，适用于药动学研究。 关键词z 雌二醇:柱前衍生化:液相色谱·串联质谱:测定 中图分类号: 0657.7+2; R969 文献标志码:A 文章编号; 1001-8255 (2014) 08-0750-04 Determination ofEstradiol in Rat Plasma by LC-MS岛1S Following Derivatization and Its Pharmacokinetic Application TAI Yi , ZHOU Zhen, LUO Huafei , 11 Zhou , GE Qinghua* (National Pharmaceutical Engineering and Research Center, Shanghai lnstitute 01Pharmaceutical lndus町， China State Institute 01Pharmaceutical Industry, Shanghai 201203) ABSTRACT: A LC-MS/MS method was established for the determination of estradiol in rat plasma by derivatization. Plasma samples were extracted and derivatized before injection. An ESI ion source was used and operated in the positive ion mode with multiple reaction monitoring (MRM) mode. Estradiol-d3 was chosen as the intemal standard and a Cl8 column was used. The calibration curve was linear in the concentration range of50 - 10 000 pg/ml. The method recoveries were 94.0% - 107.2% , with RSDs less than 10%. The method was applied in the detennination of estradiol in blank female rat plasma and the pharmacokinetic study of the estradiol patch in rats. The results showed that this method was selective, accurate and sensitive, and was successfully applied in pha口nacokinetic study for estrad