Improvement of Solubility and Dissolution Rate of Poorly Water-Soluble Anti-Cholestermic Drug Atorvastatin by Solid Dispersion Technique

Abstract

Atorvastatin calcium belongs to class II drug, which is characterized by low solubility and high permeability, which makes the drug to have low bioavailability. Enhancement of its solubility makes the drug more bioavailable and has fewer side effects. This was achieved by forming solid dispersion of the drug and formulating the tablets. Atorvastatin was mixed with various proportions of excipients which showed no color change at the end of two months, proving no drug-excipient interaction as confirmed by FTIR studies. The pre-compression blend of atorvastatin solid dispersions which were prepared by solvent evaporation technique were characterized with respect to angle of repose, bulk density, tapped density, Carr’s index and Hausner’s ratio. The pre-compression blends of all the batches were showed good to fair flowability and compressibility especially with F2 formulation having excellent results. The prepared formulations were evaluated for various quality control parameters. The tablets formulations passed all the tests of post formulation studies such as weight variation, friability, drug content, etc. From the in vitro studies, among all the formulations F2 formulation containing drug and mannitol in the ratio of 1:2 showed good dissolution rate of 97.43% in 25 minutes. While the formulations containing PVP k30 and PEG 4000 showed less release. Therefore, F2 formulation was found to be the better formulation as per dissolution profile. By conducting further studies like preclinical and clinical, the formulation can be adopted for manufacturing in bulk. &nbsp