Availability of phenindione-beta-cyclodextrin inclusion complex.
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.
Tous
S S
SS
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Egypt.
el-Sayed
A M
AM
el-Harras
S A
SA
Jun
H W
HW
D000818:Animals; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D003505:Cyclodextrins / Q000493:pharmacokinetics*; D006801:Humans; D008297:Male; D010539:Permeability; D010630:Phenindione / Q000493:pharmacokinetics* / Q000494:pharmacology; D011517:Prothrombin Time; D011817:Rabbits; D012709:Serum Albumin; D012995:Solubility; D013055:Spectrophotometry, Infrared; D014961:X-Ray Diffraction; D047392:beta-Cyclodextrins
D003505:Cyclodextrins; D012709:Serum Albumin; D047392:beta-Cyclodextrins; D010630:Phenindione; C031215:betadex