Abstract

Varenicline tartrate is a smoking cessation aid that works by blocking nicotine receptors in the brain. It helps reduce cravings and withdrawal symptoms and helps you quit smoking. The study aimed to formulate and characterize varenicline tartrate orodispersible tablets using the synthetic disintegrants crospovidone and croscarmellose sodium in different ratios and directly compressible microcrystalline cellulose as diluent, and mannitol to improve mouthfeel using the direct compression method. A total of 13 varenicline orodispersible tablets are formulated and subsequently evaluated for pre-compression and post-compression physicochemical parameters such as angle of repose, Carr index, Hausner ratio, hardness, thickness, mass variation, drug content, friability, wetting time, disintegration time, dispersion time and water absorption ratio. Optimization was performed with percentage of crospovidone (X₁ or A) and croscarmellose sodium (X₂ or B) as independent variables, while disintegration time (Y₁) and wetting time (Y₂) were selected as dependent variables using the central composite design of Design-Expert^® DX 12. Optimized formulations showed 99.68 % drug release in 60 min while the cumulative percentage drug release of pure drug was only 56.84 %. Finally, it was concluded that dissolution rate and bioavailability are improved with varenicline tartrate orodispersible tablets.