Abstract:
Cefuroxime axetil is a broad-spectrum, β-lactamase stable, second generation cephalosporin antibiotic. Cefuroxime axetil, an orally absorbed pro-drug of cefuroxime is used to treat elderly group of patient with sympathomimetic urinary tract infections. The drug is practically insoluble in water and exhibits slow intrinsic dissolution rate and poor bioavailability. The objective of this work was to enhance the dissolution rate of cefuroxime axetil by converting it into liquisolid compacts. Liquisolid compacts consisted of microcrystalline cellulose (Avicel pH 102) as carrier material, Aerosil 200 as coating material, and propylene glycol as nonvolatile solvent. Solubility studies of cefuroxime axetil in propylene glycol, Tween 80, polyethylene glycol 400 and glycerin were carried out and propylene glycol (11.12±1.06 mg/ml) was selected as a non volatile solvent in which drug is having the highest solubility. The drug concentration was kept constant in all formulations. Optimization was carried out using Box-Behnken design by selecting liquid load factor, amount of nonvolatile solvent, and carrier coating ratio as independent variables; cumulative percentage drug release, hardness, and angle of repose were considered as dependent variable. Any interaction between cefuroxime axetil and the other components were evaluated by FTIR. Dissolution test was carried out at pH 1.2. The results showed that liquisolid compacts demonstrated significantly higher drug release rates than those of directly compressed tablet.

Keywords: Cefuroxime Axetil, Liquisolid Tablet, Avicel 102, Box-Behnken Design, Aerosil 200, Carrier Material, Coating Material.