Development of novel bepotastine salicylate salt bioequivalent to the commercial bepotastine besilate in beagle dogs.

To develop a novel salt form of bepotastine with bioequivalent to the commericial bepostastine besilate, bepostastine salicylate was prepared and its physicochemical properties were investigated. Furthermore, the bepotastine salicylate-loaded tablet was prepared by the wet granulation method, and the dissolution and bioavailability in beagle dogs were evaluated compared to the bepotastine besilate-loaded commercial product. Bepotastine salicylate improved the solubility of bepotastine, and the extent of solubility improvement by salicylate form was similar to that by besilate form. However, this novel salt exhibited negligible hygroscopicity similar to besilate form, and showed slightly higher melting point than besilate form. It was stable in various pH solutions. Furthermore, the bepotastine salicylate-loaded tablet composed of bepotastine salicylate, microcrystalline cellulose, D-mannitol, povidone, sodium starch glycolate and sodium stearyl fumarate at the weight ratio of 9.63/60.97/38/3.6/6/1.8 showed similar dissolution to the bepotastine besilate-loaded commercial product in water, pH 1.2, pH 4.0 and pH 6.8 and was bioequivalent to the commercial product in beagle dogs. Thus, this bepotastine salicylate-loaded tablet would be a promising candidate with bioequivalence to the bepotastine besilate-loaded commercial product.