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Mebendazole complexes with various cyclodextrins: preparation and physicochemical characterization
Authors:Malika Lahiani-Skiba  Aude Coquard  Fréderic Bounoure  Philippe Vérité  Philippe Arnaud  Mohamed Skiba
Institution:(1) Laboratoire de Pharmacie Galénique, ADEN 3234, UFR Médecine & Pharmacy, Rouen University, 22, Bd Gambetta, 76000 Rouen, France;(2) Laboratoire de Chimie Analytique, ADEN 3234, UFR Médecine & Pharmacy, Rouen University, 22, Bd Gambetta, 76000 Rouen, France;(3) In-Cyclo, ADEN 3234, UFR Médecine & Pharmacy, Rouen University, 22, Bd Gambetta, 76000 Rouen, France
Abstract:Mebendazole is an antihelmintic drug, active against many intestinal parasites. Its systemic efficacy is limited by its poor water solubility. The use of natural or derivatized cyclodextrins permeated to multiply notably its apparent solubility, especially with permethyl β-cyclodextrine (PM β-CD) (multiplied by 4700). The inclusion complex formation between mebendazole and this methylated β-cyclodextrin, was characterized by mass spectrometry, powder X-ray diffractometry and Fourier transform infrared spectroscopy: mebendazole seemed to be included in permethyl β-cyclodextrin by its aromatic rings. To prepare inclusion complex of mebendazole and PMβ-CD by solvent evaporation, acetone may be used and the ratio using lower amount of cyclodextrin (MBZ:CD, 1:2) should be used.
Keywords:Mebendazole  Cyclodextrins  Inclusion complex  Physicochemical characterization
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