单剂量和多剂量口服布洛伪麻那敏干混悬剂在健康人体的药代动力学  

Pharmacokinetics of ibuprefen and pseudo ephedrine with chlorpheniramine suspension after single and multiple doses in healthy volunteers

作　　者：宋敏[1,2] 谭鸿毅[2] 谭志荣[3] 刘畅[2] 阳丽[2] 向红[2] 黄志军[2] 张桂香[1,2] 阳国平[2] 

机构地区：[1]中南大学药学院,长沙410013 [2]中南大学湘雅三医院,长沙410013 [3]中南大学临床药理研究所,长沙410013

出　　处：《中国临床药理学杂志》2010年第1期28-32,36,共6页The Chinese Journal of Clinical Pharmacology

摘　　要：目的研究布洛伪麻那敏干混悬剂(抗感冒药)在健康成年志愿者体内的药代动力学。方法3个单剂量组及1个多剂量组口服给药,用高效液相色谱-紫外检测法测定给药后不同时间布洛芬血药浓度,高效液相色谱-串联质谱法测定给药后不同时间伪麻黄碱和氯苯那敏血药浓度。用DAS Ver 2.0计算药代动力学参数并进行统计分析。结果3组单剂量及连续口服布洛芬(单剂:200,400,600 mg;连续:200 mg)、伪麻黄碱(单剂:30,60,90 mg;连续:30 mg)及氯苯那敏(单剂:2,4,6 mg;连续2 mg)7天后的主要药代动力学参数(tmax,Cmax,AUC0-t,AUC0-∞,t1/2等)结果显示,布洛芬、伪麻黄碱和氯苯那敏血药浓度-时间曲线拟合结果均符合一室模型,体内过程均呈线性动力学特征。结论连续多次给药,3组分都不存在药酶诱导或抑制现象。Objective To study the pharmacokinetics profiles of ibuprofen and pseudo ephedrine with chlorpheniramine suspension after single and multiple dosing in healthy volunteers. Methods Three single and one multiple oral doses of ibuprofen and pseudo ephedrine with chlorpheniramine suspension were given to healthy volunteers respectively. Ibuprofen concentrations in plasma were determined by HPLC - UV method. Pseudo ephedrine and chlorpheniramine concentrations in plasma were determined by HPLC-MS-MS method. The pharmacokinetic parameters were obtained with statistical analysis by DAS Vet 2.0. Results The main pharmacokinetic parameters of 3 single doses （ibuprofen： 200, 400, 600 mg pseudo ephedrine： 30, 60, 90 mg; chlorpheniramine： 2, 4, 6 mg） and multiple dose （ibuprofe, pseudo ephedrine and chlorpheniramine 200, 30, 2 mg, respectively） shown that the concentration- time curves of ibuprofen, pseudo ephedrine and chlorpheniramine were described by one - compartment open model and physiological dispositions were assumed by linear kinetics characteristics. Conclusion In multiple dosing study, physiological dispositions of ibuprofen, pseudo ephedrine and chlorpheniramine all existed no induction and inhibition of drug enzyme phenomenon.

关 键 词：布洛芬 伪麻黄碱 氯苯那敏 药代动力学 高效液相色谱 高效液相色谱-串联质谱 

分 类 号：R969.1[医药卫生—药理学] R971.1[医药卫生—药学]