Background/Aim. Glimepiride, as an antidiabetic from the group of sulfonylurea, is administered perorally in the treatment of diabetes mellitus. The aim of this study was to compare pharmacokinetic profiles and relative bioavailabilities of the two oral formulations of glimepiride, generic and innovator tablets, after a single dose of the active drug. Methods. An oral dose of 6 mg glimepiride was given under fasting conditions to 24 healthy volunteers. A one-week washout period was applied between the two consecutive periods. The serum samples obtained before dosing, and at various time points up to 48 hours, were analyzed for glimepiride concentration using the validated highperformance liquid chromatographic method with ultraviolet detection. Pharmacokinetic parameters representing early (maximal concentration, time to reach maximal concentration) and total exposure (area under the curve from the time 0 to the infinite time) to glimepiride were obtained and further analyzed using the multifactorial analysis of variance and the non-parametric Wilcoxon signed ranks test. Comparison of the secondary kinetic variables was only descriptive. Results. The point estimates of the ratios of geometric means (test/reference) of maximal concentrations and areas under the curve were 1.046 (90% confidence interval: 0.906−1.208) and 1.022 (90% confidence interval: 0.856−1.220), respectively, while the median values of times to reach maximal concentration, at 5% level of significance, did not differ significantly. Both formulations were well tolerated. Transient mild hypoglycaemia, which had been noted in 6 participants, resolved spontaneously within 30−60 minutes. Conclusion. Since all the parametric 90% confidence intervals for the log-transformed main variables of glimepiride were within the 0.80 and 1.25 interval, accepted as the definition of bioequivalence, and the differences in times to reach maximal concentration also did not reach statistical significance, studied tablets were considered bioequivalent.