DEVELOPMENT OF SUSTAINED RELEASE GASTRO-RETENTIVE TABLET FORMULATION OF BEPOTASTINE BESILATE USING QUALITY BY DESIGN (QBD) APPROACH

The objective of the present study was to develop sustained release gastro-retentive (SRGR) tablet formulation of bepotastine besilate for once-a-day dosing using quality by design (QbD) approach. Quality target product profile (QTPP) of bepotastine besilate SRGR tablet formulation was defined and critical quality attributes (CQAs) were identified. Potential risk factors were identified using fish bone diagram and failure mode effect analysis (FMEA) tool and screened by Plackett–Burman design and finally bepotastine besilate SRGR tablet formulation was optimized using Box–Behnken design. It was observed that formulation variables X1: hydrophobic release controlling agent (mg/tab) and X2: hydrophilic release controlling agent (mg/tab) have strikingly influenced drug release (%) (Y1), while floating lag time (min) (Y2) was significantly impacted by formulation variable X4: gas generating agent (mg/tab). A design space plot within which the CQAs remained unchanged was established at lab scale. In conclusion, this study demonstrated the suitability of a hydrophobic-hydrophilic polymer combination along with gas generating agent to achieve SRGR tablet formulation for once-a-day dosing of bepotastine besilate using systematic QbD approach.