Enhancement of Solubility of Albendazole by Complexation with -cyclodextrin

نویسندگان

  • C. Moriwaki
  • G. L. Costa
  • C. N. Ferracini
  • F. F. de Moraes
  • G. M. Zanin
  • E. A. G. Pineda
  • G. Matioli
چکیده

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 ( -CD) using aqueous and acetic acid solutions as ABZ solubilizer was studied. In aqueous -CD, complexation increased solubility 53.4 times, giving a complex equilibrium constant of 1266 L mol with a maximum ABZ concentration of 276 μmol L for 16.3 mmol L -CD. For complexation in 1.05 mol L acetic acid, UV absorbance spectra and H-NMR analysis confirmed complex formation. The UV absorbance of ABZ/acid acetic/ -CD solutions was modeled by the formation of two complexes with molar ratios 1:1 and 1:2 ABZ: CD. When neutralized with NaOH these solutions did not form precipitates only for the ABZ: -CD molar ratios of 1:8 and 1:10, showing that ABZ solubility could be increased 306 times. Results show that high CD molar ratios hold ABZ in solution by complexation enhanced by the acetate anion.

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تاریخ انتشار 2008