FORMULATION AND EVALUATION OF ORODISPERSIBLE TABLETS OF BOSENTAN USING 2³ FACTORIAL DESIGN

Abstract Background: Bosentan is an endothelin receptor antagonist belonging to BCS Class I, used in the treatment of pulmonary arterial hypertension (PAH). Conventional oral formulations may not provide sufficiently rapid onset of action required for effective management of PAH symptoms. Orodispersible tablets (ODTs) offer advantages including rapid disintegration in the oral cavity, ease of administration without water, and improved patient compliance. Objective: The present study aimed to formulate and optimize orodispersible tablets of Bosentan using 2³ factorial design to achieve rapid disintegration and enhanced drug release for improved therapeutic outcomes in PAH management. Methods: Orodispersible tablets were prepared by wet granulation method using croscarmellose sodium as superdisintegrant, PVP K30 as binder, and magnesium stearate as lubricant. A 2³ full factorial design was employed to study the effect of three independent variables (PVP K30, croscarmellose sodium, and magnesium stearate concentrations) on dependent variables including disintegration time, wetting time, and drug release. Formulations were evaluated for physical characteristics, in-vitro disintegration, and dissolution studies. Results: FTIR studies confirmed the absence of drug-excipient incompatibility. Among the eight factorial batches, formulation G8 containing PVP K30 (5%), croscarmellose sodium (5%), and magnesium stearate (10 mg) demonstrated optimal characteristics with disintegration time of 12±1 seconds, wetting time of 10±1 seconds, and drug release of 98.96±1.66% within 15 minutes. Stability studies at 40°C/75% RH for 30 days confirmed formulation stability with no significant changes in critical quality attributes.