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

• Published in: Pharmacotherapy Vol. 40; no. 7; p. 623
• Main Authors: Chen, Gang, Zhang, Dan, Du, Aihua, Zhang, Yanan, Zhang, Ying, Zhang, Lina, Zang, Siqi, Liu, Xiaona, Wang, Zejuan, Zhen, Haiqing, Liu, Yujing, Yang, Shuya, Wang, Jin
• Format: Journal Article
• Language: English
• Published: United States 01.07.2020
• Subjects: Administration, Oral; Adult; Area Under Curve; Benzhydryl Compounds - administration & dosage; Benzhydryl Compounds - chemistry; Benzhydryl Compounds - pharmacokinetics; Biological Availability; Cross-Over Studies; Drug Compounding; Fasting; Female; Glucosides - administration & dosage; Glucosides - chemistry; Glucosides - pharmacokinetics; Humans; Male; Reference Values; Sodium-Glucose Transporter 2 Inhibitors - administration & dosage; Sodium-Glucose Transporter 2 Inhibitors - chemistry; Sodium-Glucose Transporter 2 Inhibitors - pharmacokinetics; Therapeutic Equivalency; Young Adult; empagliflozin; pharmacokinetics; high-performance liquid chromatography; Jardiance; safety; bioequivalence
• ISSN: 1875-9114
• DOI: 10.1002/phar.2432

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. 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. 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 ), and the AUC from 0 to infinity (AUC ) 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. The two formulations of empagliflozin were bioequivalent, and both were generally well tolerated under fasting and fed conditions.