Dissolution Enhancement and Physicochemical Characterization of Bosentan Mouth-Dissolving Tablets Incorporating Croscarmellose Sodium and Crospovidone as Superdisintegrants

Abstract

Bosentan is a dual endothelin receptor antagonist widely used in the treatment of pulmonary arterial hypertension. However, its poor aqueous solubility can limit dissolution and delay drug release, potentially affecting therapeutic performance. The present study aimed to develop mouth-dissolving tablets (MDTs) of Bosentan and evaluate the influence of croscarmellose sodium (CCS) and crospovidone (CP) as superdisintegrants on tablet disintegration and dissolution enhancement. Bosentan MDTs were prepared by direct compression using varying concentrations (2–8%) of CCS and CP. Preformulation studies including solubility analysis, melting point determination, UV spectroscopy, and FTIR compatibility assessment were performed. The prepared formulations were evaluated for pre-compression and post-compression parameters, wetting time, water absorption ratio, dispersion time, disintegration time, and in vitro dissolution behaviour. The optimized formulation was further characterized using FTIR, DSC, SEM, drug release kinetic modelling, and accelerated stability studies. All formulations complied with pharmacopeial quality requirements. Increasing superdisintegrant concentration significantly improved wetting, disintegration, and dissolution characteristics. Formulation F8 containing 8% crospovidone exhibited the shortest disintegration time (25 ± 1 s), highest water absorption ratio (130 ± 6%), and maximum drug release (99.8 ± 0.4%) within 30 min. FTIR and DSC studies confirmed drug–excipient compatibility, while SEM revealed a porous structure conducive to rapid hydration. Stability studies demonstrated satisfactory formulation stability over three months. Crospovidone was more effective than croscarmellose sodium in enhancing the performance of Bosentan MDTs. The optimized formulation showed rapid disintegration, improved dissolution, and excellent stability, indicating its potential as a patient-friendly oral dosage form.