Brijesh Kantilal Vaniya ,Shrenik K Shah, Dhaval J Patel and Hiren N Khatri
Abstract:
Inclusion complex has been used as effective metllhod to improve the dissolution properties and bioavailability of poorly water soluble drugs. The aim of present study was to improve the dissolution rate of poorly soluble drug, bicalutamide (BIC), by cyclodextrin inclusion complexation. The phase solubility profile of bicalutamide with hydroxypropyl-β-Cyclodextrin (HP- β-CD) was classified as An-type. Stability constant with 1:2 molar ratio was calculated from the phase solubility diagram. Gibbs free energy (ΔGtr) values were negative, indicating the spontaneous nature of BIC solubilization. Solid inclusion complexes were prepared at 1:1.5, 1:2 drug/carrier ratio by physical mixing, kneading method and solvent evaporation techniques. Optimized complex was characterized by using FTIR and differential scanning calorimetry. It could conclude that stability of BIC and the absence of well define drugpolymer interaction. Inclusion complex prepared by kneading method showed the most improvement in wettability and dissolution rate as compare with pure BIC and physical mixture. Tablets prepared using optimized ratio with HP-β-CD showed significant improvement in the release profile of BIC as compared with marketed tablets (CALUT).
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