Brazilian Journal of Chemical Engineering | |
Enhancement of solubility of albendazole by complexation with β-cyclodextrin | |
C. Moriwaki2  G. L. Costa2  C. N. Ferracini2  F. F. De Moraes1  G. M. Zanin1  E. A. G. Pineda1  G. Matioli2  | |
[1] ,Universidade Estadual de Maringá Departamento de Farmácia e Farmacologia Maringá PR ,Brasil | |
关键词: Albendazole; Cyclodextrins; β-cyclodextrin; Complexation; Solubility; | |
DOI : 10.1590/S0104-66322008000200005 | |
来源: SciELO | |
【 摘 要 】
A high dosage of albendazole (ABZ) is required for treating systemic helminthe infections because of its low solubility. Aiming at increasing ABZ solubility, complexation with beta-cyclodextrin (β-CD) using aqueous and acetic acid solutions as ABZ solubilizer was studied. In aqueous β-CD, complexation increased solubility 53.4 times, giving a complex equilibrium constant of 1266 L mol-1 with a maximum ABZ concentration of 276 µmol L-1 for 16.3 mmol L-1 β-CD. For complexation in 1.05 mol L-1 acetic acid, UV absorbance spectra and ¹H-NMR analysis confirmed complex formation. The UV absorbance of ABZ/acid acetic/β-CD solutions was modeled by the formation of two complexes with molar ratios 1:1 and 1:2 ABZ:β-CD. When neutralized with NaOH these solutions did not form precipitates only for the ABZ:β-CD molar ratios of 1:8 and 1:10, showing that ABZ solubility could be increased 306 times. Results show that high β-CD molar ratios hold ABZ in solution by complexation enhanced by the acetate anion.
【 授权许可】
CC BY
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