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

Autor: Barone JA; College of Pharmacy, Rutgers-State University of New Jersey, Piscataway 08855-0789, USA. jbarone@rci.rutgers.edu, Moskovitz BL, Guarnieri J, Hassell AE, Colaizzi JL, Bierman RH, Jessen L
Jazyk: angličtina
Zdroj: Antimicrobial agents and chemotherapy [Antimicrob Agents Chemother] 1998 Jul; Vol. 42 (7), pp. 1862-5.
DOI: 10.1128/AAC.42.7.1862
Abstrakt: 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.
Databáze: MEDLINE