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.
