DISSOLUTION ENHANCEMENT OF ATOVAQUONE USING CYCLODEXTRINS AND FORMULATING TO ORODISPERSIBLE TABLETS

The aim of the study was to enhance the dissolution rate of atovaquone by preparing inclusion complexes with cyclodextrins (β-CD/ HP β-CD) and formulating their orodispersible tablets. Phase solubility studies were conducted by adding 0.5, 1, 2 and 4% of cyclodextrins in water. The values of Gibb's free energy were found increased. Inclusion complexes of atovaquone were prepared using β -CD/ HP β -CD by kneading method. Tablets were formulated using superdisintegrants i.e., sodium starch glycolate, crospovidone and Ac-Di sol at concentrations of 4, 8 and 12% of tablet weight by direct compression technique. The interaction studies were made by Fourier transform infrared spectroscopy and differential scanning calorimetry, and no significant interaction was observed. Inclusion complexes showed better dissolution than pure atovaquone and HP-β-CD established better than β-CD. Inclusion complexes of atovaquone at 1:0.25 w/w (drug: HP β -CD) in the tablets with 12% of crospovidone showed satisfactory results.