Abstract

CHARACTERIZATION AND SOLUBILITY ENHANCEMENT OF NITAZOXANIDE THROUGH β-CYCLO DEXTRIN INCLUSION COMPLEX

*Gupta Shikhar k, Soni Girish C. Jain S.K.

Institute of Pharmacy, Bundelkhand University, Jhansi – 284128. U.P. India.

ABSTRACT

The improvement of nitazoxanide bioavailability by complexation with chemically modified cyclodextrins (CyDs) has been exploited to analyse the drug/macrocycle binding affinity by a conventional method with new useful measures. Formulation were investigated in aqueous medium and in presence an amount of β-cyclodextrin at different host/guest molar ratios. The increase in solubility could be attributed to the possible masking of hydrophobic groups of Nitazoxanide, by increasing the wetting of the drug, and/or by decreasing the crystallinity of the drug. The percent drug release data from various formulations of inclusion complexes was found in the range of 50.48±0.98% to 94.47±0.46% within 120 minutes. The pure drug exhibited only 33.85 ± 0.19% to 35.4 ± 0.72% of release. The drug release profile of the formulations DSP1, DSK1, DSE1, and DSC1, in S.G.F.was found to be 64.41±0.43%,93.64±0.34%,92.76±0.64% and 85.88±0.72% respectively,whereas in 7.4 pH buffer it was found to be 67.41±0.29%, 94.47±0.46%, 87.85±0.66% and 82.80±0.65% respectively which are much better than other formulations prepared by their respective methods. The complexes prepared by different methods help to improve aqueous solubility, in-vitro and in-vivo release profiles. Overall, kneading system (DSK1) showed superior dissolution properties when compared to other methods used. These findings are extremely important from a commercial point of view as the prepared complexes remove the drawback of poor dissolution profile of Nitazoxanide.

Keywords: Cyclodextrin, Bioavailability, Crystallinity, Kneading system.