Bioequivalence Study of Fixed-Dose Combination of Remogliflozin Etabonate 100 mg/Vildagliptin 50 mg with Individual Components in Healthy Indian Male Subjects under Fed Conditions

Abstract

Background and Objective. Combination of sodium glucose co-transporter-2 (SGLT2) and dipeptidyl peptidase-4 (DPP4) inhibitors has shown promising results in the treatment of type 2 diabetes mellitus. A Fixed Dose Combination (FDC) of remogliflozin and vildagliptin will reduce the pill burden and help improve treatment compliance. This study was conducted to establish the bioequivalence of an oral FDC of remogliflozin etabonate (100mg) and vildagliptin (50mg) with single tablets of Remo ® (remogliflozin etabonate; 100 mg) and Galvus ® (vildagliptin; 50 mg) Methods. Pharmacokinetic parameters i.e. maximum concentration (C max ) and area under concentration-time curve (AUC 0-t , and AUC 0-∞ ) were calculated to determine bioequivalence. Safety was assessed and adverse events were monitored throughout the trial. Results.For both remogliflozin and vildagliptin, 90% confidence interval (CI) of the geometric least-squares mean ratios of C max , AUC 0-t , and AUC 0-∞ values between FDC and reference products fell within the standard regulatory bioequivalence range of 85.0-125.0%. Remogliflozin etabonate and its metabolite, GSK279782, also demonstrated geometric least-squares mean ratio of ~ 100%. No clinical abnormalities or adverse events were reported during the study. Conclusion.The FDC of remogliflozin etabonate and vildagliptin was bioequivalent to the reference products (Remo ® and Galvus ® ) under fed state without any safety concerns.