Pharmacokinetics of Moclobemide Sustained Release Tablets after Multiple Oral Dose Administration in Healthy Volunteers  

吗氯贝胺缓释片多剂量口服后在人体的药代动力学研究(英文)

作　　者：胡道德[1] 毛丹卓[2] 裴元英[2] 

机构地区：[1]上海交通大学附属第一人民医院药剂科,上海200080 [2]复旦大学药学院药剂学教研室,上海200032

出　　处：《Journal of Chinese Pharmaceutical Sciences》2004年第4期249-253,共5页中国药学（英文版）

摘　　要：To investigate the pharmacokinetic characteristics of moclobemide sustainedrelease tablets after multiple oral dose administration in healthy Chinese volunteers. MethodsMoclobemide sustained release tablets were given as a multiple oral dose regimen of 300 mg oncedaily for five consecutive days to 12 healthy volunteers. The concentrations of moclobemide inplasma were determined by reversed-phase high performance liquid chromatography. The partialpharmacokinetic parameters were calculated using 3p97 pharmacokinetic program. Results Theconcentration-time profile fitted an one-compartment model best. The steady-state pharmacokineticparameters of moclobemide sustained release tablets after multiple oral doses were as follows:C_(max) was (1 950 +- 156) μg· L^(-1), T_(max) was (6.00 +-1.55) h, T_(1/2(kel)) was (3.14 +-0.12)h, AUC_(ss 0-24) was (22 836 +- 1 842) μg·h· L^(-1), MRT was (7.68+-0.36) h, CL/F_((s)) was(20.2+-2.1) L·h^(-1), and V/F_((c)) was (91.4+-9.4) L, respectively. No marked adverse events werenoted during this study. Conclusion The formulation has a sustained-release effect and goodtolerance in the healthy volunteers, which provides useful information for clinical practice.目的　研究中国健康男性志愿者多剂量口服吗氯贝胺缓释片的药代动力学特征。方法　十二名健康志愿者口服吗氯贝胺缓释片 ,每日一次 ,每次一片 ,连续服五天。采用反相高效液相色谱法测定人血浆中吗氯贝胺含量。应用 3p97程序拟合药动学参数。结果　吗氯贝胺血药浓度 -时间曲线符合一室模型 ,主要稳态药动学参数Cmax为 (1 95 0± 1 5 6 ) μg·L- 1 ,Tmax为 (6 0 0± 1 5 5 )h ,T1 2 (kel) 为 (3 1 4± 0 1 2 )h ,AUCss0 - 2 4 为 (2 2 836± 1 84 2 ) μg·h·L- 1 ,MRT为 (7 6 8± 0 36 )h ,CL F(s)为 (2 0 2± 2 1 )L·h- 1 ,V F(c) 为 (91 4± 9 4)L。试验期间 ,受试者未出现明显的不良反应。结论　吗氯贝胺缓释片具有缓释作用和良好的耐受性 ,其结果可为临床应用提供参考。

关 键 词：moclobemide sustained release tablets high performance liquidchromatography phar- macokinetics multiple dose 

分 类 号：R96[医药卫生—药理学]