Comprehensive in Vitro, in Vivo, and Stability Evaluation of Optimized Modified-Release Bilayer Tablets of Empagliflozin and Metformin
Abstract
The present study aimed to comprehensively evaluate the in vitro–in vivo performance, release kinetics, and stability
of an optimized modified-release bilayer tablet containing empagliflozin and metformin hydrochloride for improved
diabetes management. The bilayer system was designed to provide an immediate release of empagliflozin for rapid
onset of action and a sustained release of metformin hydrochloride for prolonged glycemic control. In vitro dissolution
studies demonstrated that the empagliflozin layer released more than 85% of the drug within 15 minutes, confirming
its immediate-release behavior, while the metformin layer exhibited a controlled release profile with approximately
54-56% drug release at 2 hours, 83–87% at 6 hours, and more than 85% at 10 hours. Release kinetic modeling indicated
that the optimized formulation best fitted the Korsmeyer–Peppas model (R² = 0.9935), suggesting a non-Fickian
diffusion-controlled release mechanism. In vivo pharmacokinetic studies in male Wistar rats revealed rapid absorption
of empagliflozin (T_max = 1.2 ± 0.3 h) and sustained plasma concentrations of metformin, with the test formulation
showing slightly higher systemic exposure compared to the marketed reference product. Pharmacodynamic evaluation
demonstrated a rapid reduction in blood glucose levels within 30 minutes, followed by prolonged glycemic control
over 24 hours, with statistically significant improvement compared to both control and reference groups (p < 0.05).…
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