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Effect of β-cyclodextrin complexation on physicochemical properties of zaleplon
The physicochemical properties and dissolution profile of zaleplon (ZPN) $\beta$-cyclodextrin ($\beta$CD) inclusion complex were investigated. The phase solubility profile of ZPN with $\beta$-cyclodextrin was classified as A L-type. Stability constant with 1:1 molar ratio was calculated from the phase solubility diagram and the aqueous solubility of ZPN was found to be enhanced by 714% (p < 0.001) for $\beta$-cyclodextrin. Binary systems of ZPN with $\beta$CD were prepared by kneading method. The solid-state properties of complex were characterized by differential scanning calorimetry, Fourier transformation-infrared spectroscopy and powder X-ray diffractometry. It could be concluded that ZPN could form inclusion complex with $\beta$-cyclodextrin. The dissolution profile of inclusion complex was determined and compared with those of ZPN alone and its physical mixture. The dissolution rate of ZPN was significantly increased by complexation with $\beta$CD, as compared with pure drug and physical mixture.
Journal | Journal of Inclusion Phenomena and Macrocyclic Chemistry |
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ISSN | 09230750 |