Bridging in vitro buoyancy to clinical performance: A PBPK-driven analysis of once-daily Bepotastine gastro-retentive tablet in beagles and humans.

In 30 seconds

This randomized controlled trial evaluated a low-density gastro-retentive tablet of Bepotastine in beagles and humans. The study found that the tablet achieved 95.7% systemic exposure compared to a twice-daily reference, indicating effective gastric retention and bioequivalence in humans. The formulation demonstrated sustained buoyancy for over 4 hours.

Key findings

• The gastro-retentive tablet achieved 95.7% systemic exposure relative to a twice-daily reference in beagles.
• Non-floating sustained-release formulations reached only 64.5-88.6% systemic exposure.
• The clinical study confirmed bioequivalence of the gastro-retentive formulation to the reference product in 28 healthy subjects.
• The formulation showed no clinically significant food effect.

Why it matters

The development of a gastro-retentive drug delivery system for Bepotastine addresses the challenges of short half-life and narrow absorption window, potentially improving therapeutic outcomes for patients requiring once-daily dosing.