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健康受试者口服酚麻美敏片后氢溴酸右美沙芬及其代谢物的人体药动学研究
引用本文:卢俊钢,吴春艳,孙慧婧,宋敏,杭太俊.健康受试者口服酚麻美敏片后氢溴酸右美沙芬及其代谢物的人体药动学研究[J].药物分析杂志,2011(9).
作者姓名:卢俊钢  吴春艳  孙慧婧  宋敏  杭太俊
作者单位:中国药科大学药物分析室;江苏恩华药业股份有限公司;
摘    要:目的:研究20名健康受试者单剂量口服2片酚麻美敏片(每片含对乙酰氨基酚325 mg,盐酸伪麻黄碱30 mg,氢溴酸右美沙芬15 mg,马来酸氯苯那敏2 mg)后氢溴酸右美沙芬及其代谢物O-去甲右美沙芬的人体药代动力学。方法:以盐酸克仑特罗为内标,采用LC-MS/MS法ESI正离子化,选择性反应监测,同时测定人血浆中的氢溴酸右美沙芬及其代谢物O-去甲右美沙芬浓度;并采用β-葡萄糖醛酸酶酶解后测定O-去甲右美沙芬总量浓度,采用DAS 2.0计算药动学参数。结果:测得血浆中游离氢溴酸右美沙芬和O-去甲右美沙芬的主要药代动力学参数分别为Cmax(4.4±4.6),(9.7±5.4)μg.L-1;Tmax(4.2±3.3),(1.8±0.8)h;AUC0-τ(61.0±84.2),(59.4±25.4)h.μg.L-1;t1/2(9.5±2.9),(6.0±2.8)h;MRT0-τ(13.8±5.5),(7.6±2.8)h。酶解后测得O-去甲右美沙芬的主要药代动力学参数为Cmax(536±165)μg.L-1;Tmax(2.1±0.6)h;AUC0-τ(3504±710)h.μg.L-1;t1/2(6.4±2.7)h;...

关 键 词:氢溴酸右美沙芬  O-去甲右美沙芬  代谢物  酶解  液相色谱-串联质谱法  药动学  

Pharmacokinetics of dextromethorphan and its metabolite in Chinese healthy volunteers after a single oral dose of compound anti-cough agent
LU Jun-gang,WU Chun-yan,SUN Hui-jing,SONG Min,HANG Tai-jun.Pharmacokinetics of dextromethorphan and its metabolite in Chinese healthy volunteers after a single oral dose of compound anti-cough agent[J].Chinese Journal of Pharmaceutical Analysis,2011(9).
Authors:LU Jun-gang  WU Chun-yan  SUN Hui-jing  SONG Min  HANG Tai-jun
Institution:LU Jun-gang1,WU Chun-yan2,SUN Hui-jing1,SONG Min1,HANG Tai-jun1(1.Department of Pharmaceutical Analysis,China Pharmaceutical University,Nanjing 210009,China,Jiangsu Nhwa Pharmaceutical Co.LTD,Xuzhou 221007,China)
Abstract:Objective:To evaluate the pharmacokinetics of dextromethorphan hydrobromide and its metabolite dextrorphan in Chinese healthy volunteers after a single oral dose of 2 tablets of compound paracetamol,pseudoephedrine,dextromethorphan and chlorphenamine.Methods:The plasma concentrations of dextromethorphan hydrobromide and dextrorphan were determined by an LC-MS/MS method with positive ion ESI MRM detection using clenbuterol hydrochloride as internal standard.The dextrorphan was determined both before and afte...
Keywords:dextromethorphan hydrobromide  dextrorphan  metabolite  enzymatic hydrolysis  LC-MS/MS  pharmacokinetics  
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