瑞格列奈在健康人体的药代动力学和药效动力学研究  

Pharmacokinetic and pharmacodynamic studies on repaglinide in healthy Chinese volunteers

作　　者：谭鸿毅[1] 宋敏[2] 阳国平[1] 黄志军[1] 刘畅[1] 阳丽[1] 向红[1] 付志敏[2] 黄原原[2] 

机构地区：[1]中南大学湘雅三医院 [2]中南大学药学院

出　　处：《中国临床药理学与治疗学》2009年第9期979-983,共5页Chinese Journal of Clinical Pharmacology and Therapeutics

摘　　要：目的:研究瑞格列奈的药代动力学和药效动力学。方法:19名健康男性受试者单剂量口服4 mg瑞格列奈片,采用HPLC-MS-MS法测定给药后不同时间瑞格列奈的血药浓度,用快速血糖仪测定不同时间指尖血的血糖。利用DAS 2.0计算药动学参数和进行统计分析。结果:瑞格列奈体内过程符合一室开放模型,达峰浓度Cmax为(83.1±23.6)μg/L;达峰时间tmax为(0.71±0.21)h;AUC0-8为(97.1±37.8)μg.L-1.h;t1/2为(1.6±0.7)h。给药后血药浓度水平升高,血糖随之下降,于给药后1 h最低,达(3.0±0.65)mmol/L。结论:瑞格列奈起效迅速、作用持续时间短,适合餐后血糖调节,用于通过运动和控制饮食治疗无效的2型糖尿病患者。AIM： To study the pharmacokinetics and pharmacodynamics of repaginide in healthy volunteers.METHODS：19 healthy male volunteers in single oral dose of repaglinide tablets 4 mg.The plasma concentrations of repaglinide were determined by HPLC-MS-MS.The glucose levels of fingertip blood were measured by blood glucose monitoring system.The pharmacokinetic parameters were obtained by statistical analysis of DAS Ver 2.0.RESULTS： Plasma concentration-time curve conformed to one-compartment open model.The main pharmacokinetic parameters： Cmax,tmax,AUC0-88 and t1/2 were（83.1±23.6） μg/L,（0.71±0.21） h,（97.1±37.8） μg·L^-1·h,（1.6±0.7） h.The level of blood concentration was increased and blood glucose was decreased and reached its lowest value（3.0±0.65） mmol/L 1 h after administration of repaglinide.CONCLUSION： Repaglinide is characterised by fast-acting and short effects on insulin secretion.It is a prandial glucose regulator for treatment of type 2 diabetes mellitus that is not controlled by exercise and diet.

关 键 词：瑞格列奈 药代动力学 药效动力学 血糖 

分 类 号：R977.15[医药卫生—药品]