格列齐特在健康中国人体内的药代动力学研究

THE PHARMACOKINETICS OF GLICLAZIDE IN CHINESE MALE HEALTHY VOLUNTEERS

目的 :研究格列齐特 (GL)口服给药后在健康中国人体内的药代动力学及血药浓度与降糖效应的相关性。方法 :采用高效液相色谱法测定 10名健康受试者单剂量口服GL后的血药浓度 ,SCIENTIST程序拟合药代动力学参数 ;同时测定经时过程的血糖水平。结果 :GL药时曲线符合单室开放模型 ,Tmax为 ( 4 .2 72± 0 .63 1)h ,Tlag为( 0 .4 87± 0 .2 2 3 )h ,Cmax为 ( 7.4 97± 0 .93 5 ) μg/ml,t1/ 2 为 ( 9.873± 2 .678)h ,AUC为 ( 10 4 .986± 2 7.5 2 3 ) ( μg·h) /ml。给药后 5h血糖水平降至最低点 ,血糖水平与血药浓度的相关系数为 0 .82 3 (P <0 .0 1)。结论 :GL吸收较慢 ,人体内吸收程度存在一定的个体差异。血糖水平的降低与血药浓度具有显著的相关性。

OBJECTIVE:To study the pharmacokinetics of gliclazide(GL) and the relationship between its antidiabetic effect and serum GL concentration.METHODS:The study was conducted in 10 male healthy volunteers. After receiving a single oral dose of GL, their serum GL and glucose concentrations were determined and the pharmacokinetic parameters were obtained by SCIENTIST program.RESULTS:Its concentration time curve fitted to one compartment model and the pharmacokinetic parameters obtained are listed below:T max =(4.272±0.631)h, T 1ag =(0.487±0.223)h,C max =(7.497±0.935)μg/ml, T 1/2 =(9.873±2.687) h, AUC =(104.986±27.523)(μg·h)/ml. The serum glucose level reached lowest point after 5h of administration.CONCLUSION:The GL is slowly absorbed and great difference in absorb ability exists between individuals. The reduction in serum glucose is correlated to serum GL level.