FORMULATION AND EVALUATION OF FAST DISSOLVING TABLETS OF ROSUVASTATIN: RESEARCH ARTICLE

Abstract

The objective of the present study was to formulate and evaluate fast dissolving tablets of Rosuvastatin (BCS Class II drug) to enhance solubility, improve bioavailability and patient compliance especially for the paediatric and geriatric patients with sufficient therapeutic benefits. Rosuvastatin exhibits poor solubility in water and low bioavailability of approximately 20%. Four solid dispersions (1:1, 1:2, 1:4 and 1:6 w/w) were prepared by melting method using PEG 4000 as a polymer. Solid dispersions were characterized for drug content uniformity, XRD, DSC and in vitro dissolution studies.  It was then further compressed into tablets by direct compression method using different superdisintegrants like sodium starch glycolate, crospovidone and croscarmellose sodium. All the fast dissolving tablets were evaluated for pre compression parameters such as angle of repose (θ), bulk and tapped density, percentage compressibility (%) and Hausner ratio. Post compression parameters like general appearance, uniformity of weight, tablet hardness, thickness, friability, estimation of drug content, in vitro disintegration time, wetting time, in vitro dispersion time and water absorption ratio were evaluated. Among the solid dispersions prepared and based on the dissolution studies performed, SD4 formulation having 1:6 ratio was selected for the preparation of fast dissolving tablets.  Crospovidone as superdisintegrant was found to be ideal for rapid dispersion and for improving dissolution rate, which in turn increased the bioavailability. The drug release of tablet formulations in the presence of various superdisintegrants was in the order of crospovidone > croscarmellose sodium > sodium starch glycolate. This study indicated the possibility of utilizing the selected best formulation F6 in the preparation of Rosuvastatin fast dissolving tablet as a new dosage form for oral administration having increased solubility, improved bioavailability, rapid dissolution and more patient compliance.

Keywords: Rosuvastatin, solid dispersion, PEG 4000, Fast dissolving tablets, crospovidone, superdisintegrants