银杏叶提取物对大鼠美托洛尔药动学的影响

发布时间：2018-08-31 07:36

【摘要】：目的:探讨银杏叶提取物对大鼠美托洛尔药动学的影响。方法:将大鼠随机分为美托洛尔组和美托洛尔联合银杏叶提取物组,美托洛尔组口服给予美托洛尔40 mg·kg~(-1),美托洛尔联合银杏叶提取物组口服给予银杏叶片28.8 mg·kg~(-1)(按黄酮醇苷量)和美托洛尔40 mg·kg~(-1)。给药后2,5,10,20,40,60,90,120,240,360,480,720 min股动脉采血,液相色谱串联质谱(LC-MS/MS)测定美托洛尔及代谢物血药浓度。结果:美托洛尔组联合灌胃给予银杏叶提取物与美托洛尔后,美托洛尔Ka和AUC0-t显著降低(P0.05),tmax显著增加(P0.05),美托洛尔代谢产物O-去甲基美托洛尔和α-羟基化美托洛尔AUC0-t显著增加(P0.05),而CL显著减小(P0.05)。结论:银杏叶提取物能够显著降低美托洛尔的血药浓度,抑制其代谢物O-去甲基美托洛尔和α-羟基化美托洛尔的清除。
[Abstract]:Objective: to study the effect of ginkgo biloba extract on pharmacokinetics of metoprolol in rats. Methods: rats were randomly divided into metoprolol group and metoprolol combined with ginkgo biloba extract group. The metoprolol group was given metoprolol 40 mg kg~ (-1) orally, and the metoprolol combined with ginkgo biloba extract group was given orally 28.8 mg kg~ (-1) (according to the amount of flavonol glucoside) and 40 mg kg~ (-1) metoprolol. The blood samples were collected from femoral artery of 2 minutes and 5 pieces of 10 ~ (10) ~ 10 ~ (10) C ~ (20) C ~ (40) C ~ (40) C ~ (60) C ~ (-) ~ (90) 1202403 604 ~ 80720 min. The concentrations of metoprolol and metabolites were determined by liquid chromatography tandem Results: in metoprolol group, ginkgo biloba extract and metoprolol were given by gavage. The Ka and AUC0-t of metoprolol decreased significantly (P0.05), the metabolites of metoprolol increased significantly (P0.05), the AUC0-t of O-demethylmetoprolol and 伪 -hydroxylmetoprolol increased significantly (P0.05), while the CL decreased significantly (P0.05). Conclusion: ginkgo biloba extract can significantly reduce the serum concentration of metoprolol and inhibit the scavenging of its metabolites Odemethylmetoprolol and 伪 -hydroxylmetoprolol.
【作者单位】：青海省人民医院药剂科;兰州大学第一医院药剂科;
【基金】：国家自然科学基金面上项目(编号:81373494)
【分类号】：R965

【相似文献】