ENHANCEMENT OF SOLUBILITY AND DISSOLUTION PROPERTIES OF BOSENTAN BY INCLUSION COMPLEXATION
Bharathi A.*, G. Bhargavi, Ch. Sri Sailaja and D. Chandra Sekhar Naik
Abstract
The cyclodextrins have a wide range of applications in different areas
of drug delivery and pharmaceutical industry due to their complexation
ability and other versatile characteristics. The most common
pharmaceutical application of cyclodextrin is to enhance the solubility,
stability, safety and bio availability of drug molecules. The major aim
of the study was to enhance the solubility and dissolution rate of
Bosentan by complexation with Cyclodextrins (β-CD). The solid
complexes of bosentan and β-CD were prepared in 1:1 and 1:2 molar
ratios by two methods like kneading and co-solvent evaporation. The
binary complexes 1:1 molar ratio of kneading method heighted of drug release compared to
reaming method of ratios. Further the selected cyclodextrin complexes are designed to
formulate dispersible tablet using selected for different concentration of super disintegrate
like sodium starch glycol late, dicalcium phosphate by direct compression method. The
optimized formulation showed more than 80% drug release with in 1hr.
Keywords: Bosentan, Cyclodextrins, inclusion complexation, solubility enhancement, dissolution rate.
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