Enhanced bioavailability of itraconazole in hydroxypropyl-beta-cyclodextrin solution versus capsules in healthy volunteers.
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.
Barone
J A
JA
College of Pharmacy, Rutgers-State University of New Jersey, Piscataway 08855-0789, USA. jbarone@rci.rutgers.edu
Moskovitz
B L
BL
Guarnieri
J
J
Hassell
A E
AE
Colaizzi
J L
JL
Bierman
R H
RH
Jessen
L
L
D000293:Adolescent; D000328:Adult; D000368:Aged; D000935:Antifungal Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D001682:Biological Availability; D002214:Capsules; D002626:Chemistry, Pharmaceutical; D018592:Cross-Over Studies; D006801:Humans; D017964:Itraconazole / Q000008:administration & dosage / Q000009:adverse effects / Q000031:analogs & derivatives / Q000493:pharmacokinetics*; D008297:Male; D008875:Middle Aged; D012996:Solutions
D000935:Antifungal Agents; D002214:Capsules; D012996:Solutions; C084794:hydroxyitraconazole; D017964:Itraconazole