Fabrication and Evaluation of Rosuvastatin Calcium Fast- Disintegrating Tablets Using β-Cyclodextrin and Superdisintegrants
Purpose: To formulate fast-disintegrating tablets (FDT) of rosuvastatin calcium (RST) using β- cyclodextrin (CD) and different superdisintegrants to enhance their solubility.
Methods: A total of 15 FDT formulations of RST were prepared using three different techniques. The FDTs were evaluated for micromeritic properties, as well as by Fourier transform infrared spectroscopy (FTIR), thermal analysis, disintegration time (DT), dissolution rate, powder x-ray diffraction (XRDP), scanning electron microscopy (SEM) and stability studies.
Results: XRDP showed that RST was changed from crystalline to amorphous form. SEM images revealed the presence of small microscopic pores that enhanced water penetration and provided rapid dissolution rate compared with the pure drug. There was maximum release of drug (99 %) from F4 formulation containing solid dispersion of RST, CD and superdisintegrants. DT and wetting time were 25 s (p = 0.032) and 33 s (p = 0.023), respectively, for F4 formulation. In vitro dispersion time was also lowest for F4 at 23 s (p = 0.023). FTIR and DSC studies also confirmed complex formation of drug with CD and superdisintegrants.
Conclusion: FDT is a suitable strategy to enhance the dissolution rate of RST and thus is an effective tool to improve bioavailability of poorly water soluble drugs.
Keywords: Solubility, β-cyclodextrin, Kyron, Polymer, Rosuvastatin, Fast-disintegrating tablets