DISSOLUTION ENHANCEMENT OF DIACEREIN USING WATER SOLUBLE CARRIER BY SOLID DISPERSION TECHNOLOGY

Abstract

Diacerein is generally used in the treatment of Osteoarthritis , this drug comes under the class anthraquinone. The drug is practically insoluble in water and exhibits exceptionally slow and intrinsic dissolution rate with poor bioavailability. In the present study, diacerein and I²-cyclodextrin (I²-CD) solid dispersions were prepared with a view to study the effect and influence of I²-CD on the solubility and dissolution rate of this poorly aqueous soluble drug. Phase solubility profile revealed that the solubility of diacerein was significantly increased in the presence of I²-CD and indicating the possible 1:1 stoichiometric inclusion complex with a stability constant of 339.66 M-1. Effect of variable such as drug: Carrier ratios were studied. Physical characterization of the solid dispersion was characterized by Fourier transform infrared spectroscopy (FT-IR), Differential scanning calorimetry (DSC) and X-ray diffraction studies (XRD). These studies revealed that a distinct loss of drug crystallinity in the solid dispersion is ostensibly accounting for enhancement of dissolution rate in distilled water containing 0.1% Tween 80. The scanning electron microscopy (SEM) study revealed that all the binary systems appeared as agglomerates and exhibiting the presence of a homogenous solid phase which could also be responsible for the enhanced dissolution rate in comparison with the pure drug. The drug release from the prepared solid dispersion exhibited a first order kinetics. Solid dispersion of diacerein showed a 7.66 times fold increase in dissolution rate over the pure drug.