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Clinical Trial
. 1998 Jul;42(7):1862-5.
doi: 10.1128/AAC.42.7.1862.

Enhanced bioavailability of itraconazole in hydroxypropyl-beta-cyclodextrin solution versus capsules in healthy volunteers

J A Barone  1 , B L Moskovitz, J Guarnieri, A E Hassell, J L Colaizzi, R H Bierman, L Jessen
Affiliations
Clinical Trial

Enhanced bioavailability of itraconazole in hydroxypropyl-beta-cyclodextrin solution versus capsules in healthy volunteers

J A Barone et al. Antimicrob Agents Chemother. 1998 Jul.

Abstract

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 (Cmax), the times to Cmax, 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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Figures

FIG. 1
FIG. 1
Mean plasma ITR concentrations versus time.
FIG. 2
FIG. 2
Mean plasma OH-ITR concentrations versus time.
See this image and copyright information in PMC

References

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