The effects of orange juice and lemon juice on the pharmacokinetics of itraconazole and hydroxyitraconazole in healthy subjects

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Objective : To assess effects of acidic beverages, orange juice and lemon juice, on pharmacokinetics of itraconazole and its active metabolite, hydroxyitraconazole, when co-administration of weak base drug (pKa 3.7), itraconazole with these beverages. Methods : This was a randomized, three-way crossover study. Nine healthy male subjects took a single oral dose of itraconazole 100 mg with lemon juice (pH 2.9), _ orange juice (pH 4.0) and water (pH 7.2). Plasma samples were assayed using a high-pressure liquid chromatography. Results : For co-administration of lemon juice, C_<max> (maximal plasma drug concentration) and AUC_<0-48> (area under the plasma concentration-time curve from time zero to 48 h) of itraconazole were increased 1.8-fold and 1.6-fold compared to water. C_<max> and AUC_<0-48> of hydroxyitraconazole were also increased 1.7-fold and 1.7-fold compared to water. For co-administration of orange juice, C_<max> and AUC_<0-48> of itraconazole and hydroxyitraconazole were from 1.1-fold to 1.3-fold higher than that with water. Conclusion : Lemon juice which is pH 2.9 was increased bioavailability of itraconazole and hydroxyitraconazole. On the other hand, orange juice which is pH 4.0 is slightly increased bioavailability of them.
2007-03-31