Enhancement and evaluation of vardenafil hydrochloride trihydrate absorption in orodispersible tablet formulations: Establishment of in vitro, in vivo correlation and bioequivalence study

Abstract

The study's objectives were to create, produce, and test vardenafil hydrochloride trihydrate orodispersible tablets in vitro and to see how well they worked in rabbits. The absolute bioavailability of vardenafil hydrochloride trihydrate, a very strong and specific phosphodiesterase 5 (PDE5) inhibitor, is 15 %. Three different techniques were used to manufacture the orodispersible tablets: sublimation, effervescence, and superdisintegrant. Thickness, hardness, weight variation, friability, wetting time, in vitro disintegration time, and in vitro drug release were among the parameters that were evaluated for these formulations. Twelve New Zealand white rabbits participated in a randomized, single-dose, balanced, two-period crossover study to examine the pharmacokinetics. The modified formulation showed no signs of drug-excipient incompatibility, a reasonable tablet hardness (2.6 ± 0.15 kg/cm²), and a considerably improved disintegration time of 7.3 ± 1.1 s (p < 0.05). The area under the curve (AUC₀-∞) for the test and reference formulations was 174.38 ± 95.91 and 176.45 ± 76.88, respectively, according to in vivo pharmacokinetic study. In comparison to the reference, the optimized formulation also showed better maximum concentration (Cmax) and a shorter time to achieve maximum concentration (Tmax). Overall, the optimized vardenafil orodispersible tablet showed improved peak concentration, quicker absorption, and comparable bioavailability to the reference formulation.