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: C_max, t_max, AUC_0-88 and t_1/2 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.

Key words: repaglinide, pharmacokinetics, pharmacodynamics, blood glucose