OBJECTIVE: To examine the effect of grapefruit juice on the disposition of oral administered itraconazole in healthy subjects. METHODS:Twenty-two healthy male subjects received a single 100 mg dose of itraconazole with either 350 ml grapefruit juice, orange juice or mineral water. Plasma concentrations of itraconazole were measured by HPLC, and pharmacokinetic parameters; Cmax, Tmax, T1/2, AUC, and AUC corrected by human body surface area: AUC/S, were calculated. RESULTS:Grapefruit juice had no effect on any pharmacokinetic parameter of itraconazole. However, T1/2, AUC, or AUC/S were significantly decreased in orange juice treatment group compared to those in mineral water group (average decrease 56%, p < 0.01, 41%, p < 0.05, and 43%, p < 0.05, respectively). CONCLUSION: Coadministration of grapefruit juice did not affect any pharmacokinetic parameter of itraconazole while that of orange juice decreased the parameters of T1/2, AUC, and AUC/S of the drug.
RCT Entities:
OBJECTIVE: To examine the effect of grapefruit juice on the disposition of oral administered itraconazole in healthy subjects. METHODS: Twenty-two healthy male subjects received a single 100 mg dose of itraconazole with either 350 ml grapefruit juice, orange juice or mineral water. Plasma concentrations of itraconazole were measured by HPLC, and pharmacokinetic parameters; Cmax, Tmax, T1/2, AUC, and AUC corrected by human body surface area: AUC/S, were calculated. RESULTS:Grapefruit juice had no effect on any pharmacokinetic parameter of itraconazole. However, T1/2, AUC, or AUC/S were significantly decreased in orange juice treatment group compared to those in mineral water group (average decrease 56%, p < 0.01, 41%, p < 0.05, and 43%, p < 0.05, respectively). CONCLUSION: Coadministration of grapefruit juice did not affect any pharmacokinetic parameter of itraconazole while that of orange juice decreased the parameters of T1/2, AUC, and AUC/S of the drug.
Authors: Michael J Hanley; Paul Cancalon; Wilbur W Widmer; David J Greenblatt Journal: Expert Opin Drug Metab Toxicol Date: 2011-01-22 Impact factor: 4.481