CAJ | 학술논문

目的：建立测定大鼠血浆中野黄芩素及其代谢产物葡萄糖醛酸结合物浓度的UPLC-MS/MS法，并讨论两者在大鼠体内的药代动力学过程。方法色谱采用 Waters BEH C18色谱柱，流动相为0．1%甲酸乙腈-0．1%甲酸水溶液，梯度洗脱，质谱采用多反应监测( MRM)进行正离子检测野黄芩素。大鼠静脉给予野黄芩素，测定给药后不同时间的野黄芩素的血药浓度；采用酶解方式间接测定野黄芩素葡萄糖醛酸结合物的血药浓度，以DAS 2．0软件获得药动学参数。结果野黄芩素在0．116~28．2 mg · L-1呈良好线性相关，提取回收率为80．5%~90．0%，精密度、准确度、稳定性良好。药代动力学研究结果表明静脉给予野黄芩素后其原型及其葡萄糖醛酸结合物药代动力学过程均符合二室模型。结论本研究所建立的方法具有灵敏度高，重现性好，操作简便等特点，可用于同时测定野黄芩素及其葡萄糖醛酸结合物在体内的浓度，便于原型药物及其代谢物产物的药动学研究。
목적：건립측정대서혈장중야황금소급기대사산물포도당철산결합물농도적UPLC-MS/MS법，병토론량자재대서체내적약대동역학과정。방법색보채용 Waters BEH C18색보주，류동상위0．1%갑산을정-0．1%갑산수용액，제도세탈，질보채용다반응감측( MRM)진행정리자검측야황금소。대서정맥급여야황금소，측정급약후불동시간적야황금소적혈약농도；채용매해방식간접측정야황금소포도당철산결합물적혈약농도，이DAS 2．0연건획득약동학삼수。결과야황금소재0．116~28．2 mg · L-1정량호선성상관，제취회수솔위80．5%~90．0%，정밀도、준학도、은정성량호。약대동역학연구결과표명정맥급여야황금소후기원형급기포도당철산결합물약대동역학과정균부합이실모형。결론본연구소건립적방법구유령민도고，중현성호，조작간편등특점，가용우동시측정야황금소급기포도당철산결합물재체내적농도，편우원형약물급기대사물산물적약동학연구。
Aims To establish a UPLC-MS/MS meth-od for the determination of plasma concentration of scutellarein and its metabolite and to study their phar-macokinetics in rat plasma. Methods The analysis was achieved by BEH C18 column with a mobile phase composed of 0 . 1 % formic acid in acetonitrile and 0 . 1% aqueous formic acid using step gradient elution. A TQD tandem mass spectrometry equipped with electros-pray ionization source was used as detector and opera-ted by multiple reaction monitoring( MRM) positive ion mode. After intravenous injection of scutellarein, the concentrations of scutellarein and its major metabolite glucuronide scutellarin in rat plasma were determined at different time points. The pharmacokinetic parame-ters were calculated by DAS 2. 0 software. Results Good linearity was achieved for scutellarein, the ex-traction recovery was between 80 . 5 % to 90 . 5 %, the precisions and accuracy were good. The result showed the pharmacokinetic profiles of scutellarein and glucu-ronide scutellarin both fit to the two-compartment mod-el. Conclusion The above mentioned method is spe-cific, rapid, sensitive and suitable for the pharmacoki-netic studies of scutellarein and its metabolite.