Experiment 68200

Details

PropertyValue
Pharmacology
Administration routeORAL
OrganismCitrus paradisi (RUTACEAE)
CitationUNO,T: OHKUBO,T: SUGAWARA,K: HIGASHIYAMA,A: MOTOMURA,S: ISHIZAKI,T:. (2000). EFFECTS OF GRAPEFRUIT JUICE ON THE STEREOSELECTIVE DISPOSITION OF NICARDIPINE IN HUMANS: EVIDENCE OF DOMINANT PRESYSTEMIC ELEMINATION AT THE GUT SITE.. 56(9/10)
Amount utilized
Compound isolated
DiseaseTHE KINETIC PROFILES OF (+)- AND (-)-NICARDIPINE WERE STUDIED IN THE SIX NORMAL HEALTHY MALE VOUNTEERS WHO RECEIVED ORAL (40 MG) AND INTRAVENOUS (2 MG) RACEMIC NICARDIPINE, FIRST WITH WATER AND SECOND WITH GRAPEFRUIT JUICE. BOTH THE ENANTIOMERS WERE DETERMINED BY THE STEREOSELECTIVE HIGH-PERFORMANCE LIQUID CHROMATOGRAPHIC METHOD, AND HEMODYNAMIC PARAMETES (ARTERIAL BLOOD PRESSURE, HEART RAT, AND ELECTROCARDIOGRAM) WERE ASSESSED WHEN EACH BLOOD SAMPLE WAS TAKEN. GRAPEFRUIT JUICE COMPARED WITH WATER INTAKE CAUSED A SIGNIFICANT (P<0.05) INCREASE IN MEAN ORAL (+)- AND (-)-NICARDIPINE BIOAVAILABILITY(FOBS) (48.6+5.0% AND 105.6+7.8%) AND DOSE-ABSORBED (FABS) 5.6% AND 110.9+8.8%, RESPECTIVELY) WITH NO SIGNIFICANT CHANGE IN THE HEPATIC FIRST-PASS EFFECT.
Dose amount300.0 ML
Number1
Qualitative resultACTIVE
AnimalHUMAN ADULT
Per unitDAY
Dose expressionDOSE
ExtractJUICE