FORMULATION AND IN-VITRO EVALUATION OF TRIMETAZIDINE DIHYDROCHLORIDE FLOATING BEADS

This study's objective is to develop gastro-retentive floating beads that control the release of trimetazidine dihydrochloride, an effective antianginal agent; which is freely soluble in water and suffers from rapid absorption and relatively short plasma half-life (6.0 ± 1.4 h). By emulsion gelation method, trimetazidine calcium alginate floating beads were prepared using sodium alginate solution, hydroxypropyl methyl cellulose and peppermint oil. The effect of sodium alginate concentrations (2, 3, and 4%w/v), peppermint oil percentage (15, 20, and 25% v/v), and hydroxypropyl methyl cellulose type on floating properties besides in vitro drug release from the beads were studied. The results indicated that at (2% w/v) sodium alginate solution, bead formulas achieved best floating ability. On the other hand, floating time was longer at intermediate oil percentage (20%v/v), at the same time increased hydroxypropyl methyl cellulose viscosity produced longer floating time and prolonged drug release. The density of the formulated beads was found to be within the range (0.26-0.5g/ml). According to similarity factor, formulas (F9 and F12) which contain (2% w/v sodium alginate, 20% v/v oil and hydroxypropyl methyl cellulose (15 000 centipoises) were the best formulas that showed higher similarity factor (66.19 and 59.08 respectively) of Trimetazidine release in comparison to the reference product, with good floating ability and prolonged duration of more than 8 hours. In conclusion, oil entrapped floating beads give promising results for sustaining the release of highly water soluble drugs.