European Journal of Biomedical and Pharmaceutical Sciences

FORMULATION AND EVALUATION OF REGIOSELECTIVE CONTROLLED RELEASE DRUG DELIVERY OF QUETIAPINE FUMARATE

*R. Sunitha, M. Lakshmi Surekha, R. Padma and M. Murali Krishna

ABSTRACT

The present study deals with the formulation and evaluation of Hydrodynamically Balanced Gastroretentive Systems which can retard the release of Quetiapine Fumarate for a prolonged period of time specifically in the upper part of the GIT i.e, stomach. Quetiapine Fumarate is an antipsychotic drug and it shows pH dependent solubility, since it is having high solubility at stomach pH, and as the pH increases its solubility decreases rapidly. Therefore gastro retentive floating drug delivery system has been selected with a view to improve its bioavailability. The purpose of this research is to increase the gastric residence time by preparing gastroretentive floating tablets whereby making it available at its site of absorption and to achieve an extended action for a time period of 24 hrs. Quetiapine Fumarate floating tablets were prepared by wet granulation method using various grades of METHOCEL, and POLYOX with three different concentrations. Preformulation studies were carried out and the compatibility of the drug with the excipients was confirmed through differential scanning calorimetry studies. The prepared gastroretentive floating tablets were evaluated for uniformity of weight, hardness, friability, density, drug content, floating lag time, floating time, swelling index and in vitro dissolution studies. The optimized formulations F5, F7, F14, F6 and F18 showed a floating time more than 20 hrs with matrix integrity in pH 1.2. The in vitro release studies revealed that the drug release was controlled upto 24hrs. Optimized formulations showed no significant change in physical appearance, pre and post compression parameters and drug dissolution studies after storage at 40° C ± 2° C and 75% ± 5% relative humidity in a humidity chamber for 3 months. Using Higuchi’s Model and the Korsmeyer equation, the drug release mechanism from the floating controlled release tablets was found to be Anomalous (non-Fickian) diffusion.

Keywords: Quetiapine Fumarate, Gastroretentive floating tablets, Floating lag time, Floating time, Swelling index.