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Related Experiment Videos

Availability of phenindione-beta-cyclodextrin inclusion complex.

S S Tous1, A M el-Sayed, S A el-Harras

  • 1Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Egypt.

Die Pharmazie
|May 1, 1992
PubMed
Summary
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This study shows that beta-cyclodextrin forms an inclusion complex with phenindione, enhancing its dissolution and permeability. The complexation also increased the prothrombin time effect in rabbits.

Area of Science:

  • Pharmaceutical Sciences
  • Physical Chemistry
  • Drug Delivery

Background:

  • Phenindione is an anticoagulant drug with limited aqueous solubility.
  • Beta-cyclodextrin (beta-CD) is a cyclic oligosaccharide known for its ability to form inclusion complexes with poorly soluble drugs.
  • Improving phenindione's solubility and dissolution characteristics is crucial for its effective therapeutic application.

Purpose of the Study:

  • To investigate the inclusion complexation between phenindione and beta-cyclodextrin in aqueous solution.
  • To evaluate the impact of complexation on phenindione's solubility, dissolution rate, and permeability.
  • To assess the in vivo anticoagulant activity of the phenindione-beta-CD complex.

Main Methods:

  • Solubility, dissolution, and permeation studies were conducted to confirm complex formation.

Related Experiment Videos

  • The phenindione-beta-CD inclusion complex was prepared in a 1:1 molar ratio.
  • Physicochemical properties of the complex were analyzed.
  • Permeability studies were performed in the presence of human albumin.
  • Prothrombin time was measured in rabbits after administration of phenindione and its complex.

    • Main Results:

    • Complex formation between phenindione and beta-CD was confirmed by solubility, dissolution, and permeation studies.
    • The apparent stability constant of the phenindione/beta-CD complex was determined to be 492.7.
    • Dissolution rate of phenindione significantly increased in the presence of beta-CD.
    • Permeability coefficients showed an increase for the inclusion complex compared to the pure drug.
    • The prothrombin time-increasing effect was more pronounced for the phenindione-beta-CD complex than for pure phenindione in rabbits.

    Conclusions:

    • Beta-cyclodextrin effectively forms an inclusion complex with phenindione in aqueous solution.
    • The phenindione-beta-CD inclusion complex exhibits enhanced solubility, dissolution, and permeability.
    • The complexation potentially improves the anticoagulant efficacy of phenindione, as indicated by increased prothrombin times in vivo.