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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 correlation between the pharmacokinetics and plasma concentration of gliclazide (GL) after oral administration in healthy Chinese and the hypoglycemic effect. Methods: The plasma concentrations of 10 healthy volunteers after oral administration of GL were determined by high performance liquid chromatography (HPLC). The pharmacokinetic parameters were fitted by the SCIENTIST program. The blood glucose level was also determined by time course. RESULTS: The GL curve was in agreement with the single-compartment open model with Tmax of (4.272 ± 0.63 1) h, Tlag of (0.047 ± 0.223) h and Cmax of (7.497 ± 0 .93 5) μg / ml, t1 / 2 was (9.873 ± 2 .678) h, AUC was (104.4986 ± 2 7.52 3) (μg · h) / ml. 5h after administration of blood glucose levels dropped to the lowest point, the blood glucose level and plasma concentration of the correlation coefficient was 0.82 3 (P <0.01). CONCLUSION: GL absorbs slowly and there is a certain individual difference in the degree of absorption in the human body. There was a significant correlation between the decrease in blood glucose level and plasma concentration.