Bioequivalence Study of Two Empagliflozin Tablets in Healthy Chinese Subjects Under Fasting and Fed Conditions

• Published in: Clinical pharmacology in drug development Vol. 14; no. 7; p. 542
• Main Authors: Lei, Yuyan, Liu, Yuan, Gao, Lichen, Peng, Xueqiong, Chen, Lulu, Li, Chao, Chen, Weiming, Xu, Junmei, Ouyang, Dongsheng, Li, Xiaohui
• Format: Journal Article
• Language: English
• Published: United States 01.07.2025
• Subjects: Administration, Oral; Adult; Area Under Curve; Benzhydryl Compounds - administration & dosage; Benzhydryl Compounds - adverse effects; Benzhydryl Compounds - blood; Benzhydryl Compounds - pharmacokinetics; Cross-Over Studies; East Asian People; Fasting - blood; Female; Food-Drug Interactions; Glucosides - administration & dosage; Glucosides - adverse effects; Glucosides - blood; Glucosides - pharmacokinetics; Healthy Volunteers; Humans; Male; Middle Aged; Sodium-Glucose Transporter 2 Inhibitors - administration & dosage; Sodium-Glucose Transporter 2 Inhibitors - adverse effects; Sodium-Glucose Transporter 2 Inhibitors - pharmacokinetics; Tablets; Tandem Mass Spectrometry; Therapeutic Equivalency; Young Adult; empagliflozin; pharmacokinetics; LC‐MS/MS; healthy subject; bioequivalence
• ISSN: 2160-7648
• DOI: 10.1002/cpdd.1530

Empagliflozin is a highly selective sodium-glucose cotransporter 2 inhibitor and an effective medication for treating diabetes. This study aimed to assess the pharmacokinetics and bioequivalence of two 10-mg empagliflozin tablets in healthy Chinese subjects and examine food's effect on absorption. The research was conducted as a single-center, randomized, open-label, single-dose, 2-way crossover study involving 47 subjects (fasting: n = 23, fed: n = 24). Subjects received either the test or reference drug and switched to the alternative after a 7-day washout period. Blood samples were collected before administration and up to 48 hours after dosing, analyzed using validated liquid chromatography-tandem mass spectrometry techniques to determine empagliflozin levels. In both studies, all 23 subjects completed the study phases under fasting and fed conditions. In both scenarios, when comparing the test and reference formulations, the 90% confidence intervals for the geometric mean ratios of maximum plasma concentration, area under the concentration-time curve from time 0 to the last measurable concentration, and area under the concentration-time curve from time 0 to infinity fell within the bioequivalence threshold of 80%-125%, confirming their acceptability. The study found that a high-fat meal slightly reduced drug exposure and slightly accelerated absorption. No serious adverse events were observed. This research confirmed the pharmacokinetic similarity of the 2 empagliflozin formulations and demonstrated their good tolerance under fasting and fed conditions.