Empagliflozin and metformin are oral antidiabetic drugs commonly used to treat type 2 diabetes mellitus as a combination therapy. This study aimed to compare the pharmacokinetics and safety of a newly developed fixed-dose combination of 5-mg empagliflozin L-proline and 1000-mg metformin with the reference drug. A randomized, open-label, single-dose, 2-period, 2-treatment, crossover study was conducted in healthy Korean subjects. The subjects received a single oral dose of reference drug or test drug at each period. The pharmacokinetic (PK) parameters were calculated using a noncompartmental method. The geometric mean ratios and 90% confidence intervals of the plasma maximum concentration (C ) and area under the concentration-time curve from time zero to the last quantifiable concentration (AUC ) were calculated. A total of 27 healthy subjects were included in the PK analysis. For empagliflozin, the geometric mean ratios (90% confidence intervals) of the test to reference drug for C and AUC were 1.03 (0.99-1.08) and 1.03 (1.00-1.06), respectively. For metformin, the corresponding values for C and AUC were 0.99 (0.92-1.06) and 1.00 (0.94-1.06), respectively. In conclusion, a fixed-dose combination of empagliflozin L-proline and metformin showed similar PK characteristics to the reference drug, and both drugs were safe in healthy subjects.© 2023, The American College of Clinical Pharmacology.
