FORMULATION, DEVELOPMENT AND EVALUATION OF ROSUVASTATIN CALCIUM IMMEDIATE RELEASE TABLETS

Swapna Velivela*, Vinyas Mayasa, V. Rama Mohan Guptha, Nikunja B. Pati, CH. Ramadevi

ABSTRACT

Rosuvastatin calcium is a synthetic lipid lowering agent which inhibits the enzyme 3-hydroxy-3-methylglutarylcoenzymeA to mevalonate, a precursor of sterols, including cholesterol. It comes under class II of Biopharmaceutical Classification System. The purpose of this study was to develop and evaluate Rosuvastatin calcium immediate release tablets by wet granulation method using different proportions of superdisintegrants and binder. Pre-formulation studies were done initially and the results were found to be within the limits. All the mentioned batches were prepared and granules were evaluated for pre-compression parameters such as loss on drying, bulk density, tapped density and compressibility index. Tablets were evaluated for weight variation, thickness, hardness, friability; disintegration time and assay were found to be within the limits. In vitro dissolutions were performed in 0.05M 6.8 PH phosphate buffer and effect of various superdisintegrants was explored. Final selection of formulation was based on dissolution profile, from dissolution studies formulation 11 showed 80% drug release within 15 minutes. Similarity and difference factors which revealed that formulation (F11) containing 1.5% polyplasdone XL 10 and polyplasdone XL 100 each and 20% binder are most successful as it exhibited in vitro drug release. In vitro drug release profile reveals that with increased concentration of polyplasdone XL 10 and polyplasdone XL 100 (1.5%) and decreased binder concentration (20%) there was increased in drug release. Accelerated stability studies were performed for the optimized batch which indicated that there were no changes in drug content and in vitro dissolution.

Keywords: Biopharmaceutical Classification System, pre-compression parameters, Polyplasdone XL 10, Rosuvastatin calcium, superdisintegrants,