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  • Title: Availability of phenindione-beta-cyclodextrin inclusion complex.
    Author: Tous SS, el-Sayed AM, el-Harras SA, Jun HW.
    Journal: Pharmazie; 1992 May; 47(5):365-8. PubMed ID: 1409827.
    Abstract:
    The inclusion complexation was occurred between beta-cyclodextrin (beta-CD) and phenindione (1) in aqueous solution. The complex formation was proved by solubility, dissolution and permeation study. The inclusion complex was prepared and its physicochemical properties was studied. 1 was combined with beta-CD in 1:1 molar ratio. Using the solubility data, the value of apparent stability constant obtained of 1/beta-CD complex was 492.7. The dissolution rate of 1 was increased in presence of beta-CD. The permeability coefficients of 1 were 7.86 x 10(-3), 4.76 x 10(-3) and 5.0 x 10(-3), corresponding to pure drug, its physical mixture with beta-CD and the inclusion complex, respectively. The presence of human albumin generally decreased the permeability coefficient of the drug. The reduction (79.5%) was found to be nearly equal in case of either pure 1 or its complex with beta-CD. Administration of 1 or its inclusion complex with beta-CD to rabbits increase prothrombin times, the effect was more pronounced in the complex form of drug than free one.
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