Novel Sublimation-Based Approach For The Development Of Rapidly Disintegrating Bosentan Tablets: Enhancing Bioavailability And Patient Compliance Through Optimized Porous Design

Abstract

This study aimed to develop and evaluate Bosentan mouth dissolving tablets (MDTs) prepared by the sublimation method to enhance patient compliance and bioavailability. Nine formulations (F1–F9) were designed using varying levels of Crospovidone as a superdisintegrant and Camphor as a sublimating agent. Pre-compression assessments demonstrated excellent flowability with Carr’s Index values below 15% and consistent Hausner’s Ratios around 1.15–1.16. Post-compression evaluations confirmed compliance with pharmacopeial standards for weight variation, hardness, friability, disintegration time, and drug content uniformity. Notably, disintegration times decreased from 26 seconds (F1) to 18 seconds (F9), correlating with increased porosity observed via microscopy. In vitro dissolution studies revealed enhanced drug release profiles, with optimized formulations achieving nearly 90% release within 5 minutes. Accelerated stability testing over 3 months showed minimal changes in critical quality attributes, confirming formulation robustness. In vivo pharmacokinetic evaluation in animal models demonstrated significantly higher Cmax, reduced Tmax, and improved AUC values for the MDT formulation compared to the conventional tablet, indicating faster absorption and enhanced bioavailability. Overall, the sublimation method proved effective in producing stable, rapidly disintegrating Bosentan MDTs with superior pharmacokinetic performance, offering a promising strategy for improving therapeutic outcomes and patient convenience.