SOLUBILITY AND DISSOLUTION ENHANCEMENT OF WATER INSOLUBLE DRUG BY USING DIFFERENT HYDROPHILLIC CARRIERS AND FORMULATED INTO TABLET DOSAGE FORM
Authors: Prachi Sharma, Taranjit Kaur, Ajeet Pal Singh
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Rosuvastatin calcium is a BCS class II drug (low solubility and high permeability), used as a lipid lowering agent by acting as HMG CoA reductase inhibitor and it is used for the management of hyperlipidemia. Increase in the solubility of the poorly water soluble drug is the most challenging aspect for various new chemical entities which leads to the unsatisfactory dissolution profile, consequently, the bioavailability. There are various techniques to enhance the solubility of the drug, such as particle size reduction, nanosuspension, use of surfactants, salt formation, pH modifier, solid dispersion etc. Solid dispersions in water-soluble carriers have attracted considerable interest as a means of improving the dissolution rate and hence possibly bioavailability, of a range of hydrophobic drugs. Carriers are the major players in these formulations, e.g., hydroxypropylmethylcellulose, ethyl cellulose, methyl cellulose, polyvinyl pyrrolidone, polyvinyl alcohol etc. HPMC and EC is one of the most efficient polymers among all of these to work as a carrier for these drugs to enhance solubility. Four ratios of drug: carrier were prepared (1:1, 1:3, 1:5, 1:7) and 1:7 was the optimized ratio which shows a maximum release of the drug via dissolution profile. In the present work, Solid Dispersions were prepared by Kneading technique to enhance the solubility of Rosuvastatin Calcium. Solid dispersions were evaluated for Fourier transform infrared spectroscopy (FTIR), thermal analysis, dissolution studies, powder X-ray diffraction (PXRD), scanning electron microscopy (SEM), and stability studies to confirm enhancement in solubility. The prepared solid dispersions are formulated into tablet dosage form and characterized by various parameters i.e. weight variation, hardness, friability, disintegration, and dissolution rate. The evaluated parameters of tablet dosage form show increase in solubility and dissolution rate of the pure drug.