Pharmacokinetic and pharmacodynamic studies on repaglinide in 20 healthy Chinese volunteers / 第二军医大学学报

ABSTRACT

Objective: To evaluate pharmacokinetic and pharmacodynamic of repaglinide tablets in Chinese subjects.Methods: Twenty healthy male volunteers were enrolled in the study. A single dose (4 mg) of repaglinide tablets was givenorally. Plasma concentrations of repaglinide were determined by HPLC method. Blood glucose and serum insulin leve1s weremeasured by biochemistry and radioimmunoassay methods respectively. Results: Plasma concentration-time curve conformedto one-compartment open model. The pharmacokinetic parameters were as follows tmax (0. 75?0.43 ) h,cmax (54.44?24.97)ng/ml, t1/2 (0. 80?0. 31) h, MRT (1. 55?0. 41) h, C1/F (61. 43?20. 10) L/h and AUC (73. 34?29.95) h? ng/ml. Thelevel of serum insulin was raised and the level of blood glucose decreased after administration of repaglinide. The highest levelof serum insulin was (l26. 24?95.93) mU/L at 0.75h and blood glucose level reached its lowerest vaIue (2. 34I0.44) mmol/L 1 h after oral administration. Conclusion: Repaglinide is characterised by fast-acting and short effects on in-sulin secretion. It decreases serum glucose level by stimulating insulin secretion from the pancreatic ?-cells. It is a novel oralprandial glucose regulator for the treatment of type 2 diabetes mellitus.