Evaluation Parameters and In-Vitro Studies of Floating Beads of Analgesic Drug

Abstract

The objective of this present investigation was to develop gastro-retentive floating sustained release alginate beads of Diclofenac sodium by the ionotropic gelation method. The floating beads were prepared by dispersing Diclofenac sodium together with CaCO3 (as gas forming agent) into a solution of sodium alginate and HPMC. The resulting solution was then extruded through a 22 gauge syringe needle into 100 ml cross-linking solution containing calcium chloride (1% w/v) plus acetic acid (10% v/v). Prepared beads were evaluated for their micromeritic characteristics, particle size, in-vitro dissolution studies, encapsulation efficiency, buoyancy test and FT-IR spectroscopy. The drug
entrapment efficiency was increased with the increment of polymer ratio. All of the formulations (F1 to F5) floated immediately or with a very short lag time and remained floating upto 12 hours. Rough and porous surface was observed in microscopic studies and many large hollow pores or multiple small hollow pockets were observed in case of cross-sectional microscopic studies of beads. In vitro dissolution studies were performed for twelve hours into 900 ml 0.1N HCl (pH 1.2) using USP Apparatus II (paddle type) maintained at a temperature of 37ºC and stirred at a speed of 50 rpm. The dissolution study revealed that, after eleven hours the percent of drug release for five formulations were 76.7% (F1), 73.5%% (F2),72.2% (F3), 70.56% (F4), and 69.1 %(F5) and all of the formulations followed zero order and Higuchi model.