Pharmacokinetics of empagliflozin, a sodium glucose cotransporter 2 (SGLT2) inhibitor, and metformin following co-administration in healthy volunteers

摘要

Objective: This open-label study investigated potential drug-drug interactions between empagliflozin and metformin. Methods: 16 healthy men received treatment A (empagliflozin 50 mg q.d. for 5 days), treatment B (empagliflozin 50 mg q.d. for 4 days with metformin 1,000 mg b.i.d. for 3 days and 1,000 mg q.d. on Day 4) and treatment C (metformin 1,000 mg b.i.d. for 3 days and 1,000 mg q.d .on Day 4) in the sequence AB then C, or C then AB. Results: Metformin had no clinically relevant effect on the area under the steady state plasma concentration-time curve (AUC??,ss geometric mean ratio (GMR): 96.9; 90% CI: 92.3 - 101.7) or the maximum plasma concentration at steady state (Cmax,ss GMR: 100.5; 90% CI: 88.8 - 113.7) of empagliflozin. Similarly, empagliflozin had no clinically relevant effect on AUC??,ss (GMR: 100.7; 90% CI: 95.9 - 105.6) or C max,ss (GMR: 103.6; 90% CI: 96.5 - 111.2) of metformin. The renal clearance of empagliflozin and metformin were unaffected by co-administration. Both drugs were well tolerated alone and in combination and did not cause hypoglycemia. Conclusions: These data support co-administration of empagliflozin and metformin without dose adjustment. ? 2013 Dustri-Verlag Dr. K. Feistle.