The effects of food and dose on the oral systemic availability of itraconazole in healthy subjects

We have studied the influence of food and dose (50, 100, 200 mg) on the oral systemic availability of the broad spectrum antifungal itraconazole and the pharmacokinetics after repeated dosing of 100 mg in six healthy volunteers. The relative systemic availability of itraconazole capsules compared wi...

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Bibliographic Details
Published inEuropean journal of clinical pharmacology Vol. 36; no. 4; p. 423
Main Authors Van Peer, A, Woestenborghs, R, Heykants, J, Gasparini, R, Gauwenbergh, G
Format Journal Article
LanguageEnglish
Published Germany 01.07.1989
Subjects
Administration, Oral
Adult
Antifungal Agents - administration & dosage
Antifungal Agents - adverse effects
Antifungal Agents - pharmacokinetics
Dose-Response Relationship, Drug
Food
Humans
Itraconazole
Ketoconazole - administration & dosage
Ketoconazole - adverse effects
Ketoconazole - analogs & derivatives
Ketoconazole - pharmacokinetics
Male
Random Allocation
Reference Values
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Summary:We have studied the influence of food and dose (50, 100, 200 mg) on the oral systemic availability of the broad spectrum antifungal itraconazole and the pharmacokinetics after repeated dosing of 100 mg in six healthy volunteers. The relative systemic availability of itraconazole capsules compared with solution averaged 39.8% in the fasting state but 102% in the post-prandial state. Food did not significantly affect the tmax of the capsules. Itraconazole AUC at single doses of 50, 100, and 200 mg had a ratio of 0.3:1:2.7, and the steady-state AUC (0-24) after 15 days of 100 mg was five times the single-dose AUC. These findings suggest non-linear itraconazole pharmacokinetics in the range of therapeutically used doses. Furthermore, capsules should be given shortly after a meal to ensure optimal oral systemic availability.
ISSN:0031-6970
DOI:10.1007/bf00558308