Effect of cyclodextrin on the pharmacology of antifungal oral azoles.
Concentrations of oral azoles in serum were compared in a single-dose pharmacologic study in mice. When hydroxypropyl-beta-cyclodextrin was used as a carrier and compared with a standard carrier, polyethylene glycol, drug concentrations determined by bioassay showed that the peak concentration and area under the concentration-time curve were greatly enhanced for itraconazole and saperconazole; moderately enhanced for ketoconazole; but negligibly affected for fluconazole, miconazole, and SCH 42427.
Hostetler
J S
JS
Department of Medicine, Santa Clara Valley Medical Center, San Jose, California.
Hanson
L H
LH
Stevens
D A
DA
D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000818:Animals; D000935:Antifungal Agents / Q000493:pharmacokinetics*; D001393:Azoles / Q000493:pharmacokinetics*; D001682:Biological Availability; D003505:Cyclodextrins / Q000494:pharmacology*; D004337:Drug Carriers; D005260:Female; D051379:Mice; D011092:Polyethylene Glycols; D047392:beta-Cyclodextrins
D000935:Antifungal Agents; D001393:Azoles; D003505:Cyclodextrins; D004337:Drug Carriers; D047392:beta-Cyclodextrins; D000073738:2-Hydroxypropyl-beta-cyclodextrin; D011092:Polyethylene Glycols