Pharmacokinetics, Safety, and Bioequivalence of Two Empagliflozin Formulations after Single Oral Administration under Fasting and Fed Conditions in Healthy Chinese Subjects: An Open‐label Randomized Single‐dose Two‐sequence, Two‐treatment, Two‐period Crossover Study

Objectives To evaluate the pharmacokinetic properties and safety of empagliflozin, and the bioequivalence of test formulation empagliflozin tablet compared with the brand‐name drug Jardiance (reference formulation) after single oral administration under fasting and fed conditions in healthy Chinese subjects. Methods An open‐label randomized single‐dose two‐sequence, two‐treatment, two‐period crossover study was conducted in healthy Chinese subjects, with 30 subjects under fasting condition and another 30 subjects under fed condition. Under each condition, subjects received a single oral administration of either the test or reference empagliflozin formulation, and then they received a single oral dose of the other formulation after a 7‐day washout period. Results A total of 29 subjects under each condition completed the study. The maximum plasma drug concentration, the area under the plasma concentration‐time curve (AUC) from 0 to t (AUC 0–t ), and the AUC from 0 to infinity (AUC 0–∞ ) of test formulation and reference formulation was 186.90 ± 47.21 and 190.60 ± 40.94 ng/ml, 1303.04 ± 234.28 and 1267.78 ± 217.07 ng·hour/ml, and 1328.08 ± 243.84 and 1293.22 ± 224.82 ng·hour/ml under fasting condition, and 151.55 ± 23.86 and 154.08 ± 30.40 ng/ml, 1215.65 ± 197.62 and 1199.26 ± 186.23 ng·hour/ml, and 1241.76 ± 202.47 and 1225.54 ± 192.10 ng·hour/ml under fed condition, respectively. Conclusions The two formulations of empagliflozin were bioequivalent, and both were generally well tolerated under fasting and fed conditions.