Open AccessEnhanced Bioavailability of Itraconazole in Hydroxypropylβ-Cyclodextrin Solution versus Capsules in Healthy Volunteers
Author(s) -
Joseph A. Barone,
Bruce L. Moskovitz,
Joseph A. Guarnieri,
Alan E. Hassell,
John L. Colaizzi,
Robert Bierman,
Lois Jessen
Publication year - 1998
Publication title -
antimicrobial agents and chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.07
H-Index - 259
eISSN - 1070-6283
pISSN - 0066-4804
DOI - 10.1128/aac.42.7.1862
Subject(s) - bioavailability , itraconazole , capsule , bioequivalence , crossover study , pharmacology , pharmacokinetics , chemistry , oral administration , dosage form , plasma concentration , medicine , biology , antifungal , dermatology , placebo , botany , alternative medicine , pathology
The bioavailabilities and bioequivalences of single 200-mg doses of itraconazole solution and two capsule formulations were evaluated in a crossover study of 30 male volunteers. The two capsule formulations were bioequivalent. The bioavailabilities of the solutions itraconazole and hydroxyitraconazole were 30 to 33% and 35 to 37% greater, respectively, than those of either capsule. However, the maximum concentrations of the drug in plasma (C max ), the times toC max , and the terminal half-lives were comparable for all three formulations. These data indicate that the bioavailabilities of itraconazole and hydroxyitraconazole are enhanced when administered as an oral solution instead of capsules.
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