Formulation and characterization of ternary complex of sublingual film of buspirone hydrochloride

Abstract

Taste masked sublingual film of buspirone hydrochloride (BH) was developed with the objectives of taste masking, fast disintegration, increased dissolution and better patient compliance. The film was formulated using Polyox WSR N-10, polyvinyl pyrolidone (PVP) K-30 and propylene glycol as a plasticizer. Taste masking was obtained by ternary complexation between BH, β-cyclodextrin and PVP K-30. Optimized batch contained 3 % w/v of Polyox WSR N-10, 2 % w/v PVP K-30 and propylene glycol (20 % weight of Polyox WSR N-10). The optimized formulation also contained BH: β-CD (1:1.5 molar ratio), BH: sucralose (1:0.5 ratio) and 0.15 ml orange flavour. This batch was evaluated for % elongation, tensile strength, in vitro disintegration time and in vitro dissolution studies. In-vitro permeation studies employing rabbit sublingual mucosa, indicated higher drug permeability at the ventral surface than at the bottom surface of the mouth. In-vivo absorption studies in rabbits revealed that 50.27 ± 5.24 % of BH was absorbed sublingually from film within 5 min. The kinetics of in vivo drug absorbed from sublingual film in human volunteers indicated that there is no significant difference between ex vivo and in vivo data obtained for the drug absorption. The formulation, subjected to stability studies at 25 °C/60 % RH for 2 months, showed good stability indicating suitable packaging and storage conditions.