Formulation development and Characterization of Olanzapine Controlled Release Gastroretentive Tablets

Abstract

Olanzapine (OLZ), an atypical antipsychotic drug belonging to BCS class II. OLZ being weak acid has an absorption window in stomach only. OLZ has a tendency to accumulate in the body and thus leads to increase the side effects. Conventional OLZ tablets have a drawback of short dosing frequency. Thus in the present study, floatable mucoadhesive tablets of OLZ using direct compression technology was formulated. Mucoadhesion was achieved by using various mucoadhesive polymers i.e. HPMC K100M, PEO 303, Carbopol 940P. Effervescent agent i.e. citric and, sodium carbonate were incorporated to impart floating. Gastroretentive Formulations were subjected to various evaluation parameters like floating lag time, total floating time, mucoadhesive force, initial drug release as well as controlled drug release for 12 hours. All different polymers were checked individually as a matrix forming agents. The combination of HPMC K100M, PEO 303, and Carbopol 940P was optimized using simplex centroid design to get the desired results. The simplex centroid design was used to get the optimized ratio of polymers. The effect of these variables were seen for the response variablesY30, Y60, Y120, Y180, Y240, Y300, Y360, Y420, Y480, Y540, Y600, Y660, Y720, floating lag time, mucoadhesion force. Checkpoint batch was prepared in order to validate the model obtained. The ratio of 10.8: 26.3: 42.9 for PEO 303: Carbopol 940: HPMC K100M was the considered as optimized in terms of drug release profile, mucoadhesion and floating lag time. Release of the optimized batch was best fitted to Weibull equation showing least SSR and highest R square value upon model fitting. The present study proves the potential of gastroenteritis approach for sustained release of OLZ