Lin S Y, Yang J C
Pharm Weekbl Sci. 1986 Aug 22;8(4):223-8. doi: 10.1007/BF01957782.
Inclusion complexation of warfarin and alpha- or beta-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 alpha- and beta-cyclodextrin complexes are 10.29 M-1 and 148.88 M-1, respectively. The greater the stability constant of the inclusion complex the lesser the permeability of warfarin. Solid complexes of warfarin and alpha- or beta-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 alpha- and beta-cyclodextrins, respectively. The dissolution rate of warfarin was significantly improved by complex formation.
通过溶解度法、膜渗透研究、薄层色谱法、溶出度研究、红外光谱法和差示扫描量热法，研究了华法林与α-或β-环糊精在水相和固相中形成包合物的情况。加入环糊精后，华法林的溶解度增加。α-和β-环糊精配合物的表观稳定常数分别为10.29 M-1和148.88 M-1。包合物的稳定常数越大，华法林的渗透性越小。通过冷冻干燥得到了华法林与α-或β-环糊精的固体配合物。在包合物和物理混合物之间观察到红外吸收光谱和DSC热谱图存在明显差异。对于α-和β-环糊精，冷冻干燥的华法林-环糊精配合物的溶出速率分别提高了约1200倍和550倍。通过形成配合物，华法林的溶出速率得到显著提高。
