Single-Dose Pharmacokinetics of Amprenavir Coadministered with Grapefruit Juice

Abstract
In this crossover study in 12 healthy volunteers, coadministration of amprenavir (1,200 mg; single dose) with grapefruit juice slightly reduced the maximum concentration of drug in serum ( C max ) compared to administration with water (7.11 versus 9.10 μg/ml), slightly increased the time to C max (1.13 versus 0.75 h), and did not affect the area under the concentration-time curve from 0 to 12 h (AUC 0-12 ), the AUC 0-∞ , or the concentration at 12 h. Therefore, grapefruit juice does not clinically significantly affect amprenavir pharmacokinetics.