Preparation of celecoxib-dimethyl-beta-cyclodextrin inclusion complex: characterization and in vitro permeation study.

作者: Cinzia Anna Ventura , Ignazio Giannone , Donatella Paolino , Venerando Pistarà , Antonino Corsaro

DOI: 10.1016/J.EJMECH.2005.03.001

关键词: Stability constants of complexesDissolutionAqueous solutionSolubilityDrug carrierInclusion compoundChemistryPermeationNuclear chemistryChromatographyCyclodextrin

摘要: The ability of 2,6-di-O-methyl-beta-cyclodextrin (DM-beta-Cyd) to include the anti-inflammatory drug celecoxib (CCB) was evaluated. complex prepared by kneading and freeze-drying methods characterized in solid state aqueous solution. Water solubility dissolution rate CCB, a medium simulating gastric fluid, significantly increased after complexation, with complete obtained 30 180 min for freeze-dried kneaded complexes respectively. Phase studies showed Ap-type diagrams. Stability constants 1:1 1:2 CCB-DM-beta-Cyd (1)H-NMR suggested probable inclusion only an external interaction second Cyd molecule. Thermodynamic parameters binding process existence van der Waals forces between CCB DM-beta-Cyd. DM-beta-Cyd influenced permeation through CaCo-2 cells monolayer. increase observed due fast included destabilizing action exerted macrocycle on biomembrane.

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