FORMULATION, CHARACTERIZATION AND EVALUATION OF DOCETAXEL COCRYSTALS FAST RELEASE TABLETS FOR TREATMENT OF CANCER

Abstract

The current study aims to improve the dissolution and oral bioavailability of a BCS IV drug Docetaxel (DXT) by co-crystallization with a co-former, syringic acid (SYA). A co-crystal of DXT with SYA in different molar ratios were prepared by liquid assisted grinding method. Prepared co-crystals were evaluated for melting point and solubility. Solubility study showed that maximum solubility was achieved with 1:2 molar ratio which was further characterized by FTIR, differential scanning calorimetry (DSC) and powder X-ray diffraction. FT-IR revealed evidence of significant intermolecular interactions based on two characteristic shifts toward lower frequencies pertaining to the complex formation between drug and co-former. The results of DSC and PXRD in were also in full compliance with the reported study. The Docetaxel co-crystals exhibited greater dissolution than the pure drug. The Docetaxel co-crystals were further converted into fast release tablets with superdisintegrant and subliming agent. The formulation parameters were optimized by 3² full factorial CCD design. Disintegration time and in-vitro dissolution were taken as dependant variables and effect of superdistigrant and subliming agent was studied. A checkpoint batch comprising of maximum quantity of Crospovidone and Camphor was selected on the basis of desirability, as it has shown minimum disintegration time and maximum drug release. The optimized formulation was kept under stressed condition to check the stability of product and results indicated that it was found stable.