TASTE MASKED RAPID ORO-DISINTEGRATING TABLETS OF CETIRIZINE HYDROCHLORIDE

摘要

Cetirizine is an orally active, selective H_1-receptor antagonist and useful as a non-sedating antihistamine. It is used for the symptomatic relief of allergic rhinitis and chronic urticaria. The concept of formulating orally disintegrating tablets containing cetirizine hydrochloride offers a suitable approach in serving desired objective of rapid dissolution with increased bioavailability to provide quick relief in episodes of allergic conditions. The development of such fast dissolving dosage forms will assist in solving the problems encountered in administration of drugs to the pediatric and elderly patients having difficulty in swallowing and also offering additional benefits of convenience of administration while travelling and dosing anywhere, anytime without the need of water. Based on preformulation studies prototype tablet formulations containing superdisintegrants like kyron T 314, indion 414, tulsion 339 and croscarmellose sodium and their combinations were formulated by direct compression technique. Taste masking was achieved by adding flavours and using citric acid along with aspartame and mannitol. Tablets were evaluated for hardness, friability, weight variation, in vitro disintegration, in vivo disintegration and mouthfeel, wetting time, drug content uniformity and in vitro dissolution studies. The optimized formulation was subjected to stability study for one month at 40deg/75% RH. The tablets disintegrated in vitro and in vivo within 18 to 118 sec and 22 to 120 sec respectively. Almost 90% of drug was released from all formulations within 6 min. The drug release from the formulations followed first order kinetics. Stability study of the tablets showed non-significant drug loss. The formulation containing indion 414 alone was found to give the best results. Apart from meeting all quality parameters, the tablets exhibited faster rate of drug release.