Pharmacokinetic enhancement of poorly aqueous soluble rosuvastatin using natural gum as carriers: pharmaceutical modeling of release kinetics and bio-stastistical evaluation

Abstract

The major focus of the present investigation is to enhance the solubility and dissolution rate of Rosuvastatin Calcium. Preaparation of Solid dispersions of Rosuvastatin Calcium by using Vitamin E TPGS, A.Marmelos, and Gum Karaya as carriers in different ratios through solvent evaporation method. As Solid dispersions have been traditionally used effective techniques to improve the dissolution properties and bioavailability of poorly-soluble drugs. The model drug selected Rosuvastatin Calcium, which is BCS class-II drug with anti-hyperlipidemic potential. The reported bioavailability from oral route of drug is only 20%. So aim of current study is to improve the solubility and dissolution rate of a poorly water-soluble drug Rosuvastatin Calcium, by solid dispersion technique. Physical mixtures and solid dispersions were prepared using Vitamin E TPGS, MGK & natural polymers A.Marmelos in different to drug to carrier ratios, dispersions were prepared by solvent evaporation technique. Prepared formulations were characterized in solid state by FTIR analysis, powder X-ray diffraction, Scanning electron microscopy and in-vitro dissolution study. The aqueous solubility of Rosuvastatin Calcium was favored by presence of both the polymers. Solid state characterizations indicated the Rosuvastatin Calcium was present in amorphous form and entrapped in polymer matrix. In contrast to the very slow dissolution rate of pure Rosuvastatin Calcium, the dispersion of the drug in the polymers considerably enhanced the dissolution rate. Solid dispersion prepared with TPGS showed maximum 91.19% Drug release. The best formulation of solid dispersion selected and subjected to fast dissolving tablets. The mixtures of solid dispersion and excipients were evaluated for pre-compression parameters. After then fast dissolving tablets were prepared by direct compression technique. The formulated tablets were evaluated by post compression parameters. In-vitro drug release performance of the develope