盐酸阿扎司琼氯化钠注射液在健康人群中药物动力学和代谢转化研究  

Clinical Pharmacokinetics and Metabolites Investigation of Azasetron Hydrochloride in Healthy Volunteers

作　　者：袁赛红 戴冰 

机构地区：[1]湖南省中医药大学第一附属医院药剂科,湖南省长沙市410007

出　　处：《临床合理用药杂志》2011年第06X期23-25,共3页Chinese Journal of Clinical Rational Drug Use

摘　　要：目的研究健康受试者静脉注射盐酸阿扎司琼后的药物动力学及体内代谢转化特征。方法 15名健康志愿者静脉滴注盐酸阿扎司琼10mg后,用高效液相色谱法测定血浆和尿液中盐酸阿扎司琼浓度,计算主要药动学参数。结果盐酸阿扎司琼主要动力学参数为AUC0-t为(63.37±13.02)(mg/L)h,AUC0-∞为(51.89±11.84)(mg/L)h,Cmax为(7.125±0.591)mg/L,Tmax为(0.667±0.249)h。12%的原型药经尿液排出。结论盐酸阿扎司琼在生物体内能迅速被吸收,分布快,药效明显。Objective To investigate the clinical pharmacokinetics and metabolites of Azasetron Hydrochloride after intravenous infusion in healthy volunteers. Methods Azasetron Hydrochloride for injection were given to 15 healthy volunteers of a dose of 10 mg, the concentrations of Azasetron Hydrochloride in human plasma and fine were determined by HPLC, the main pharmacokinetic parameters ere calculated. Results The ain pharmacokinetic parameters of Azasetron Hydrochloride ere as the followings ： AUC0 - t （63.37 ＋ 13.02） （mg/L） h, AUC0 - ~ （51.89 ＋ 11.84） （rag/L） h, Cm, （7- 125 ~ 0. 591 ） mg/ L, Tin,, （0. 667 ~ 0. 249） h. 12 percent of Azasetron Hydrochloride were discharged by urine. Conclusion Azasetron Hydro- chloride was speedy absorbed and distributed in vivo, The efficacy was obvious.

关 键 词：盐酸阿扎司琼 药物动力学 代谢 高效液相 

分 类 号：R96[医药卫生—药理学]