【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。更多还原

【Abstract】 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.更多还原