Abstract
Inclusion complexation of warfarin and α- or β-cyclodextrins in water and in the solid phase were studied by a solubility method, a membrane permeation study, thin-layer chromatography, a dissolution study, IR spectroscopy and differential scanning calorimetry. The solubility of warfarin increased with the addition of cyclodextrins. The apparent stability constants of the α- and β-cyclodextrin complexes are 10.29M −1 and 148.88M −1 respectively. The greater the stability constant of the inclusion complex the lesser the permeability of warfarin. Solid complexes of warfarin and α- or β-cyclodextrins were obtained by freeze-drying. Clear differences in IR absorption spectra and DSC thermograms were observed between the inclusion complexes and physical mixtures. The dissolution rate of the freeze-dried warfarin-cyclodextrin complexes was increased about 1200-fold and 550-fold for α- and β-cyclodextrins, respectively. The dissolution rate of warfarin was significantly improved by complex formation.
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This paper is Part IV of ‘Drug Interaction in Pharmaceutical Formulation’.
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Lin, SY., Yang, JC. Inclusion complexation of warfarin with cyclodextrins to improve some pharmaceutical characteristics. Pharmaceutisch Weekblad Scientific Edition 8, 223–228 (1986). https://doi.org/10.1007/BF01957782
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DOI: https://doi.org/10.1007/BF01957782