摘要
目的研究胃炎灵颗粒对大鼠体内细胞色素P450酶活性的影响。方法分别以右美沙芬(CYP2D6)、咪达唑仑(CYP3A4)、奥美拉唑(CYP2C19)、茶碱(CYP1A2)、氯唑沙宗(CYP2E1)和甲苯磺丁脲(CYP2C9)作为探针底物,大鼠6只,每日灌胃胃炎灵颗粒4 g/kg,采用LC-MS/MS测定给药前后大鼠体内6种探针药物的血药浓度。结果胃炎灵颗粒连续给药10 d后,与给药前相比,大鼠体内的右美沙芬(P <0. 01)、甲苯磺丁脲(P <0. 01)代谢减慢,氯唑沙宗(P <0. 01)代谢加快,奥美拉唑、咪达唑仑、茶碱的代谢无显著差异。结论胃炎灵颗粒在大鼠体内对CYP2D6酶产生中强抑制作用,对CYP2C9酶产生弱抑制作用,对CYP2E1酶产生轻微诱导作用,对CYP3A4、CYP2C19和CYP1A2基本没有影响。
Objective To study the effect of Weiyanling granule on the activities of six CYP450 isoforms in rats.Methods Dextromethorphan,midazolam,o meprazole,theophylline,chlorzoxazone and tolbutamide were used as the probe drugs for CYP2D6,CYP3A4,CYP2C19,CYP1A2,CYP2E1 and CYP2C9,respectively.The six probe drugs were simultaneously given to six rats(4 g/kg).Six rats were given Weiyanling granule(4 g/kg).The concentration of six probe drugs in rats'plasma was measured by LC-MS/MS before and after giving drugs.Results After 10 d of treatment,the metabolism of dextromethorphan and tolbutamide decreased(P<0.01),while the metabolism of chlorzoxazone increased(P<0.01),but no significant difference in metabolism of omeprazole,midazolam or theophylline was observed.Conclusion Weiyanling granule has a moderate&high inhibitory effect on CYP2D6,a weak inhibitory effect on CYP2C9,and a weak induction effect on CYP2E1 in rats,while it has no effect on CYP3A4,CYP2C19 or CYP1A2.
作者
冯星月
余辉
蒋志涛
张咏梅
FENG Xing-yue;YU Hui;JIANG Zhi-tao;ZHANG Yong-mei(College of Pharmacy,Nanjing University of Traditional Chinese Medicine,Nanjing 210023,China;Zhangjiagang Hospital of Traditional Chinese Medicine,Affiliated Hospital of Nanjing University of Traditional Chinese Medicine,GraduateWorkstation of Enterprises in Jiangsu Province,Zhangjiagang 215600,China)
出处
《实用药物与临床》
CAS
2019年第1期5-11,共7页
Practical Pharmacy and Clinical Remedies
基金
苏州市科技计划发展项目(SYSD2016161)
