Liquisolid Technique for Enhancement of Dissolution Properties of Fenofibrate

The in vitro dissolution property of slightly water soluble Fenofibrate (FN) was improved by exploring the potential of Liquisolid system (LS). The in vitro release pattern of LS compacts and directly compressed tablets were studied using USP-II apparatus. Different LS compacts were prepared using a mathematical model to calculate the required quantities of powder and liquid ingredients to produce acceptably flowable and compressible admixture. Avicel PH 102, Aerosil 200 and Explotab were employed as carrier, coating material and disintegrants respectively for preparing LS compacts. The prepared LS compacts were evaluated for their flow properties such as bulk density, tapped density, angle of repose, Carr’s compressibility index and Hausner’s ratio. The interaction between drug and excipients in prepared LS compacts were studied by differential scanning calorimetry (DSC) and Xray powder diffraction (XRPD). The drug release rates of LS compacts were distinctly higher as compared to directly compressed tablets, which show significant benefit of LS in increasing wetting properties and surface area of drug available for dissolution. The LS1 of LS powder system showed acceptable flowability, Carr’s compressibility index and Hausner’s ratio. The DSC and XRD studies conforms the no significant interaction between the drug and excipients used in LS compacts. From this study it concludes that the LS technique is a promising alternative for improvement of dissolution property of water-insoluble drugs. INTRODUCTION: In aqueous systems, Fenofibrate (FN) has a poor solubility and displays no amphiphilic character. Therefore the drug is molecularly dispersed in water until the solubility product of FN is exceeded. Schubert et al reported that, the solubilization of FN was linearly increased on addition of lecithin . The poor dissolution rate of such water-insoluble drugs confronts a major obstacle in development of pharmaceutical dosage forms. The oral absorption of these drugs is often controlled by dissolution in GI tract. Thus dissolution of drug is of prime importance in absorption. The different techniques used to enhance the dissolution of water insoluble drugs, some of them are particle size reduction, surfactant as solublizing agent, drug complex with hydrophilic carrier, pro-drug approach, formulation of drug as solid solution to improve the dissolution rate by decreasing the crystallinity . Among these the most promising method for promoting dissolution is the use of LS compacts .