Pharmacokinetic Comparison Between a Fixed‐Dose Combination of Empagliflozin L‐Proline/Metformin and Empagliflozin/Metformin in Healthy Korean Subjects

• Published in: Clinical pharmacology in drug development Vol. 12; no. 12; pp. 1156 - 1163
• Main Authors: Lee, HyunJoon, Chung, Jae‐Yong, Yu, Kyung‐Sang, Park, Shin‐Jung, Lee, Soyoung
• Format: Journal Article
• Language: English
• Published: United States Wiley Subscription Services, Inc 01.12.2023
• Subjects: Antidiabetics; Area Under Curve; Cross-Over Studies; diabetes mellitus; Diabetes Mellitus, Type 2 - drug therapy; Drug Combinations; Drug dosages; empagliflozin L‐proline; fixed‐dose combination; Healthy Volunteers; Humans; metformin; Metformin - pharmacokinetics; Pharmacokinetics; Republic of Korea; Republic of Korea; pharmacokinetics; metformin; diabetes mellitus; empagliflozin L-proline; fixed-dose combination
• DOI: 10.1002/cpdd.1310
• ISSN: 2160-763X; 2160-7648

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 (Cmax) and area under the concentration–time curve from time zero to the last quantifiable concentration (AUClast) 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 Cmax and AUClast were 1.03 (0.99–1.08) and 1.03 (1.00–1.06), respectively. For metformin, the corresponding values for Cmax and AUClast 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.