Enhancement of Solubility and Dissolution Rate of Simvastatin Tablets by Liquisolid Compact Approach

Abstract

The aim of the current work was to improve the solubility and dissolution rate of poorly water-soluble drug, simvastatin (SM) by using the liquisolid compact technique (LS; SM-LS). Liquid load factors, and excipient ratios were used to calculate the required amounts of excipients necessary to prepare the SM-LS and compressed to tablets according to mathematical models. Avicel PH102, Aerosil 200 and Crosspovidone (CP) was used as carrier, coating material and disintegrant, respectively. Drug-excipient mixtures were evaluated compatibility by Attenuated total reflectance (ATR) and differential scanning calorimetry (DSC). Prepared SM-LS formulations were evaluated for various pre-compression and post-compressional parameters, in-vitro dissolution, and stability studies (40 ± 2°C / 75 ± 5% RH) for 3 months. Among the different formulations, LS10 formulation which contains 30% drug, 5% CP, Avicel pH 102: Aerosil 200 (1:10) showed 14-folds increase in dissolution rate when compared with pure SM powder. FTIR-ATR and DSC studies confirmed that there was no interaction between the drug and excipients. Further, the LS10 formulation had shown comparable dissolution profile with commercially available tablet formulation. The LS10 formulation showed no significant changes in the physicochemical properties over 3 months during stability studies. Therefore, the SM loaded LS formulation could be considered as an alternative approach to enhance the solubility and dissolution for commercial formulations. Keywords: Liquisolids compacts, solubility, dissolution, carrier, coating material, stability.