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, 2-sequnce, 2-treatment, 2-period, crossover study.
Pharmacotherapy. 2020 Jun 04;:
Authors: Chen G, Zhang D, Du A, Zhang Y, Zhang Y, Zhang L, Zang S, Liu X, Wang Z, Zhen H, Liu Y, Yang S, Wang J
OBJECTIVES: To evaluate the pharmacokinetic properties and safety of empagliflozin, and 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, 2-sequence, 2-treatment, 2-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 received a single oral dose of the other formulation after a 7-day washout period.
RESULTS: 29 subjects under each condition completed the study. The maximum plasma concentration (Cmax ), the area under the plasma concentration-time curve (AUC) from 0 to t (AUC0-t ), and the AUC from 0 to infinity (AUC0-∞ ) 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·h/mL, and 1328.08 ± 243.84 and 1293.22 ± 224.82 ng·h/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·h/mL, and 1241.76 ± 202.47 and 1225.54 ± 192.10 ng·h/mL under fed condition, respectively.
CONCLUSIONS: The two formulations of empagliflozin were bioequivalent, and both were generally well tolerated under fasting and fed conditions.
PMID: 32498113 [PubMed – as supplied by publisher]