Atorvastatin ascorbic acid cocrystal strategy to improve the safety and efficacy of atorvastatin

Abstract

The study was aimed to investigate the effect of dissolution enhancement on the hypolipidemic effect and hepatotoxicity of the drug in hyperlipidemic rats. Atorvastatin ascorbic acid cocrystals were prepared by phase solution methods and characterized by Fourier transformation infrared spectroscopy, differential scanning calorimetry, scanning electron microscopy, X-Ray powder diffraction. Results of characterization confirmed that atorvastatin ascorbic acid cocrystals exhibited particle size was 221 nm. In in vitro study, results of dissolution test showed that the release of atorvastatin was increased to 1.6 folds. From In vivo study results, it was observed that in atorvastatin ascorbic acid cocrystals treated rats, serum total cholesterol, triglycerides, liver transaminase levels were significantly decreased, and liver glutathione activity was increased. In conclusion, atorvastatin ascorbic acid cocrystals therapy exhibited less hepatotoxicity in presence of ascorbic acid when compared to atorvastatin alone therapy and also the efficacy of therapy was improved.