Abstract

FORMULATION AND CHARACTERIZATION OF TRIMETAZIDINE HYDROCHLORIDE MICROSPHERES USING DOUBLE EMULSION SOLVENT EVAPORATION TECHNIQUE

Saraswathi S.* and Senthamarai R.

ABSTRACT

The present research work was intended to formulate and characterize Trimetazidine hydrochloride microspheres by a novel W/O/O double emulsion solvent evaporation technique which was designed to release the drug in the colon. Polymers such as Eudragit L 100 and S 100 were employed as encapsulation materials for preparing microspheres. Twelve trial formulations (FT1-FT12) were developed by varying the ratio of polymer combination and drug - polymer. Preformulation studies have been carried out for the drug and excipients. Morphological studies were performed for all prepared microsphere by Scanning Electron Microscopy. Percentage yield, particle size, percent drug content, encapsulation efficiency, in vitro drug release and kinetics were analyzed for all the trial batches (FT1-FT12). From the results, it was observed that, Formulation FT7 with 1:1.5 ratio of Eudragit L & S 100 combination and drug- polymer ratio of 1:2 showed spherical shaped microspheres with a maximum encapsulation efficiency of 80.12% when compared with other batches. The in vitro drug release study inferred that the formulation FT7 showed a maximum release of 97.65% up to 24 hours in pH 6.8 which followed non-fickian zero order release kinetics. From the outcome of results, it was concluded that the Trimetazidine hydrochloride loaded Eudragit microspheres showed a maximum encapsulation efficiency with a colonic drug release of 24 h and can be used as an effective antianginal drug without any haemodynamic effects.

Keywords: Stable Angina Pectoris, Trimetazidine Hydrochloride, Microspheres.