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

Antimicrob Agents Chemother. 1998 Jul;42(7):1862-5. doi: 10.1128/AAC.42.7.1862.


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.

Publication types

  • Clinical Trial
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adolescent
  • Adult
  • Aged
  • Antifungal Agents / administration & dosage
  • Antifungal Agents / adverse effects
  • Antifungal Agents / pharmacokinetics*
  • Biological Availability
  • Capsules
  • Chemistry, Pharmaceutical
  • Cross-Over Studies
  • Humans
  • Itraconazole / administration & dosage
  • Itraconazole / adverse effects
  • Itraconazole / analogs & derivatives
  • Itraconazole / pharmacokinetics*
  • Male
  • Middle Aged
  • Solutions


  • Antifungal Agents
  • Capsules
  • Solutions
  • hydroxyitraconazole
  • Itraconazole