Dissolution rate enhancement of febuxostat by liquisolid technique

Abstract

Development of liquisolid compacts is one of the pharmaceutical formulation technologies to improve the dissolution rate of poorly soluble drugs. The intent of present investigation was to enhance the dissolution rate of poorly soluble drug Febuxostat by delivering the drug as a liquisolid compact. Febuxostat is amorphous substance, widely used in the treatment of chronic gout and hyperuricemia. It is a BCS class II drug, practically insoluble in water exhibiting poor dissolution pattern and low oral bioavailability (49%). Liquisolid Technique is used for enhance the solubility of poorly water soluble drugs. Febuxostat tablet was prepared by Liquisolid compacts technique and it is optimized by using different concentration of drug in non-volatile solvent (PEG400) and different ratio of Carrier (Avicel 102) to adsorbent material (Aerosil 200). The solid state property of liquisolid compact powder was characterized by Fourier Transform Infra-Red Spectroscopy (FT-IR). FTIR studies of Febuxostat and Liquisolid compact powder confirmed that the drug was pure and there is no chemical interaction between drug with excipients. The prepared Liquisolid Tablets were evaluated for hardness, Friability, drug content and in vitro dissolution study. The solubility and dissolution rate were found significantly increased in these Liquisolid compact systems compared with pure drug alone. The highest improvement of solubility and dissolution rate was found with 45% w/w Conc. of drug in PEG 400 and 10:1 ratio of carrier to adsorbent material. Dissolution rate of drug is increased; this is attributed to improve solubility of Febuxostat. The dissolution studies for liquisolid compacts and conventional formulations were performed and it was found that liquisolid compacts of Febuxostat showed significant higher drug release than conventional. Total of nine formulations were prepared and F2 was optimized formulation with drug release of 97.11%.The preparation of Liquisolid compact is a promising strategy to improve the solubility and dissolution of drug having low solubility.