Abstract: Objective: To study the effect of Glimepiride on the blood glucose concentrations in healthy volunteers. Methods: Forty healthy volunteers were divided into eight groups to receive a single dose of 1, 2, 4, 6, 8, 10 mg Glimepiride or placebo and blood glucose concentrations were determined on the pre administration day, the administration day and the post administration day. Moreover, a full physical examination and a series of laboratory examinations were taken before the trial conducted and the results were assessed by SAS software. Results: Blood glucose concentrations of healthy volunteers after administration of 2, 4, 6, 8 or 10 mg Glimepiride decreased significantly during 2 h after breakfast on the administration day compared with the pre administration day （P＜0 05）. The blood glucose concentrations at 2 h after lunch, supper and 9∶00 PM on the administration day in 10 mg Glimepiride group were significantly lower than those of other groups （P＜0 05）. Conclusion: A single dose of 2~10 mg Glimepiride in healthy volunteers decreased the blood glucose concentrations （P＜0 05）, which indicated a dose-response relationship.