Formulation and Evaluation of Floating Alginate Beads of Diclofenac Sodium

Abstract

ABSTRACT:The objective of this present investigation is to develop gastroretentive sustained release alginate beads of Diclofenac sodium by the ionotropic gelation method. The floating beads were prepared by dispersing Diclofenac sodium together with CaCO 3 (as gas forming agent) into a solution of sodium alginate. 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 encapsulation efficiency, buoyancy test, FT-IR spectroscopy, scanning electron microscopy (SEM) and release behaviour. In vivo floating behaviour was studied by sonography. 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 24 hours. Rough and porous surface was observed in case of surface SEM and many large hollow pores or multiple small hollow pockets were observed in case of cross-sectional SEM of beads. In vivo floating behaviour of the beads was confirmed by ultrasonographic examination of a healthy male volunteer after ingestion of capsule containing floating beads. In vitro dissolution studies were performed for eleven 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.

Formulation and Evaluation of Diazepam-Loaded Intravaginal Alginate Beads: An Investigation Study for the Treatment of Pelvic Floor Dysfunction

“…1). This was in a good correlation with Rasel and Hasan, who found that the release of diclofenac sodium significantly decreased from 76.7% to 69.1%, as the amount of SA increased from 2 g to 4 g [15]. This could be ascribed to the formation of a tight junction between the glucuronic acid residues as a result of cross-linking.…”

“…2). An increase in the cross-linking agent concentration, led to the formation of more rigid gel structure with smaller pore size, which retained the drug and retarded the penetration of the dissolution medium into the beads which in turn decreased the total amount of the drug released [15]. This was in a good correlation with Mandal et al who reported a significant decrease in the amount of trimetazidine dihydrochloride release from 38% to 30% with an increase in Cacl2 concentration from 1% to 3% [41].…”

“…Accurately weighed quantity of the formed beads equivalent to 10 mg of the drug was crushed, suspended in 100 ml phosphate buffer pH 6.5 and stirred at 100 RPM at 25°C in a thermostatic shaker water bath (Julabo SW-20 C, Germany) till equilibrium [15]. The solution was filtered, suitably diluted and the drug entrapped was determined by RP-C18 HPLC method using a mobile phase consisting of acetonitrile, methanol, and 1% phosphate buffer (pH 3) in a ratio of 18:58:24 (v/v/v) at a flow rate of 1 ml/min and the effluent was monitored using UV detection at 232 nm [17] against drug free beads as a blank.…”

“…Ionotropic gelation method was used for the preparation of DZ-loaded beads [14,15]. Accurately weighed amount of SA was dissolved in phosphate buffer pH 6.5 by stirring under gentle heating.…”

Evaluation of the Effect of Psyllium on the Viability of Lactobacillus Acidophilus in Alginate-Polyl Lysine Beads

“…The rough and approximately porous surface characteristics of alginate beads shown in SEM pictures is in good agreement with the other studies which can be explained by the egg-box structure of calcium alginate beads. [21][22][23][24] Alginate is able to form gel by reaction with divalent cations such as Ca 2+ . Gelation of alginate is mainly achieved by the exchange of Na + from the guluronic acids with Ca 2+ , and stacking of these guluronic groups to form the characteristic egg-box structure.…”