RESUMO
INTRODUCTION: Levocetirizine dihydrochloride is an orally active, third-generation non-sedative antihistamine used in the symptomatic relief of seasonal and perennial allergic rhinitis. The present work aimed at preparing quick release films of levocetirizine with the purpose of developing a dosage form for a very quick onset of action, which is beneficial in managing severe conditions of allergies, aiding in the enhancement of bioavailability, and is very convenient for administration, without the problem of swallowing and using water. MATERIALS AND METHODS: The films of levocetirizine dihydrochloride were prepared by using polymers such as hydroxypropyl methylcellulose (HPMC) and polyvinyl alcohol (PVA), as either single polymer or in combination of two, by a solvent casting method. They were evaluated for physical characteristics such as uniformity of weight, thickness, folding endurance, drug content uniformity, surface pH, percentage elongation, and tensile strength, and gave satisfactory results. The formulations were subjected to disintegration, in vitro drug release tests, and in vivo studies on rats. RESULTS: A marked increase in the dissolution rate was exhibited by fast-dissolving films of levocetirizine dihydrochloride containing HPMC as a polymer, when compared to conventional tablets. The haloperidol-induced catalepsy, milk-induced leukocytosis, and nasal provocation in vivo studies in rats proved that the fast-dissolving films of levocetirizine dihydrochloride produced a faster onset of action compared to the conventional tablets. CONCLUSIONS: Fast dissolving films of levocetirizine dihydrochloride can be considered suitable for clinical use in the treatment of allergic rhinitis and other conditions of allergies, where a quicker onset of action for a dosage form is desirable along with the convenience of administration.
