Experiment 647122

Details

PropertyValue
Pharmacology
Administration routeORAL
OrganismCitrus paradisi (RUTACEAE)
CitationPENZAK,SR: GUBBINS,PO: GURLEY,BJ: WANG,PL: SACCENTE,M:. (1999). GRAPEFRUIT JUICE DECREASES THE SYSTEMIC AVAILABILITY OF INTRACONAZOLE CAPSULES IN HEALTHY VOLUNTEERS.. 21(3)
Amount utilized
Compound isolated
DiseaseTO DETERMINE THE EFFECT OF GRAPEFRUIT JUICE ON THE SYSTEMIC AVAILABILITY OF ITRACONAZOLE CAPSULES, SERUM ITRACONAZOLE AND HYDROXY-ITRACONAZOLE CONCENTRATIONS WERE DETERMINED IN 11 HEALTHY VOLUNTEERS STUDIED IN A RANDOMIZED, TWO-WAY CROSSOVER DESIGN. CONCURENT GRAPEFRUIT JUICE RESULTED IN A 43% DECREASE IN THE MEAN ITRACONAZOLE AUC0-48 (2507 NG.HR/ML, 1434 NG.HR/ML. P=0.046) AND A 47% DECREASE IN THE MEAN HYDROXY-ITRACONAZOLE AUC0-72 (7264 NG.HR/ML VERSUS 3880 NG.HR/ML, P=0.025). GRAPEFRUIT JUICE ALSO SINGIFICANTLY INCREASED THE MEAN ITRACONAZOLE TMAX (5.5 VERSUS 4 HOURS). WE CONCLUDE THAT CONCOMITANT GRAPEFRUIT JUICE DOES NOT ENHANCE THE SYSTEMIC AVAILABILITY OF ITRACONAZOLE CAPSULES, BUT RATHER APPEARS TO IMPAIR ITRACONAZOLE ABSORPTION. THEREFORE, CONCOMITANT GRAPEFRUIT JUICE WILL NOT LIKELY BE USEFUL IN IMPROVING THE ORAL AVAILABILITY OF ITRACONAZOLE CAPSULES.
Dose amount240.0 ML
Number1
Qualitative resultACTIVE
AnimalHUMAN ADULT
Per unitDAY
Dose expressionDOSE
ExtractFRUIT JUICE
GenderGIVEN TO BOTH SEXES