【摘要】 目的:建立非那西丁及其代谢产物的液质联用检测法,研究莪术油对大鼠肝微粒体CYP1A2酶活性的影响,为临床合理用药提供参考。方法:色谱柱为XDB-C18(150mm×2.1mm,5μm),流动相为乙腈-0.1%甲酸,流速:0.4mL.min-1,柱温:30℃,以多反应监测方式采集数据。以非那西丁为探针药物,采用体外实验,实验组给予莪术油,对照组给予生理盐水,评价药物代谢酶CYP1A2酶活性的变化。结果:非那西丁和对乙酰氨基酚的检测浓度线性范围分别为4～1600ng.mL-1(r=0.9973)、3-2000ng.mL-1(r=0.9973)。实验组测得的扑热息痛/非那西丁的比值:11.30±0.71,对照组:9.60±1.04,t检验显示P<0.05,有统计学意义。结论:本法可用于检测大鼠肝微粒体孵育液中非那西丁及其代谢物浓度。莪术油对大鼠肝CYP1A2酶的活性,有体外诱导作用。更多还原

【Abstract】 Objective: To develop an HPLC-MS determination method of phenacetin and paracetamol and to investigate the effect of Zedoary Turmeric oil on the activity of rat CYP1A2 for providing reference to rational drug use in clinic.Methods:Samples were separated on XDB-C18(150mm×2.1mm,5μm) column,acetonitrile-0.1 % formic acid was used as mobile phrase,and the flow rate was 0.4 mL·min–1,the column temperature was 30℃.The multiple reaction monitor was adopted to detect the concentration of phenacetin and paracetamol.Phenacetin was used as a probe of CYP1A2.The activity of rat CYP1A2 was evaluated by an in-vitro experiment which two group involved,experiment group was given Zedoary Turmeric oil and the control group was given saline.Results: The calibration curves were linear in the ranges of 4~1600ng·mL-1(r=0.9973) phenacetin and 3~2000ng·mL-1(r=0.9973) paracetamol.The ratio of paracetamol /phenacetin in experiment group was 11.30±0.71,the ratio of control group was 9.60±1.04,pair T test was P<0.05.Conclusion: The method is suitable for determination of phenacetin and paracetamol in rat liver microsomal incubation system.The activity of rat liver CYP1A2 can be enhanced by Zedoary Turmeric oil.更多还原