Experiment 69060
Worktypes
Details
| Property | Value |
|---|---|
| Pharmacology | |
| Administration route | ORAL |
| Organism | Citrus paradisi (RUTACEAE) |
| Citation | OHANI,M: KAWABATTA,S: KARIYA,S: UCHINO,K: ITOU,K: KOTAKI,H: KASUYAMA,K: MORIKAWA,A: SEO,I: NISHIDA,N:. (2002). EFFECT OF GRAPEFRUIT PULP ON THE PHARMACOKINETICS OF THE DIHYDROPYRIDINE CALCIUM ANTAGONISTS NIFEDIPINE AND NISOLDIPINE.. 122(5) |
| Amount utilized | |
| Compound isolated | |
| Disease | THE EFFECT OF THE INTAKE OF 200 G OF GRAPEFRUIT PULP (CORRESPONDING TO ONE GRAPEFRUIT) ON THE PHARMACOKINETICS OF THE CALCIUM ANTAGONISTS NIFEDIPINE (NF) AND NISOLDIPINE (NS) WERE INVESTIGATED IN 8 HEALTHYL JAPANESE MALE VOLUNTEERS. A CROSSOVER DESIGN WAS USED FOR THE STUDY: GROUP I DID NOT INGEST ANY GRAPEFRUIT (CONTROL GROUP); GROUP II INGESTED GRAPEFRUIT 1 H AFTER DRUG ADMINISTRATION; AND GROUP III INGESTED GRAPEFRUIT 1 H BEFORE DRUG ADMINISTRATION. THE INTAKE OF GRAPEFRUIT PULP INCREASED THE PLASMA CONCENTRATIONS OF BOTH NF AN NS, AN EFFECT THAT HAS PREVIOUSLY BEEN REPORTED WITH GRAPEFRUIT JUICE. THE INCREASE WAS MOST MARKED WHEN GRAPEFRUIT WAS EATEN BEFORE DRUG ADMINISTRATION. THE INCREASE IN THE AUC0-24 WAS SIGNIFICANT FOR BOTH DRUGS (P>0.05). THE FINDING THAT THE RATIOS OF CMAX AND AUC0-24 FOR UNCHANGED DRUG AND METABOLITES DID NOT VARY AMONG THE THREE GROUPS FOR EITHER DRUG SUGGESTS THAT THE INCREASE IN SERUM CONCENTRATION PRODUCED BY GRAPEFRUIT INTAKE MAY BE DUE TO OTHER FACTORS THAN AN INHIBITORY EFFECT ON DRUG METABOLISM. ALSO, THE INCREASES IN CMAX AND AUC0-24 OF NS PRODUCED BY GRAPEFRUIT INTAKE WERE SMALLER THAN THOSE PRODUCED BY GRAPEFRUIT JUICE INTAKE, INDICATING THAT GRAPEFRUIT PULP AND JUICE HAVE DIFFERENT EFFECTS ON THE PHARMACOKINETICS. |
| Dose amount | 200.0 GM |
| Number | 1 |
| Qualitative result | ACTIVE |
| Animal | HUMAN ADULT |
| Per unit | DAY |
| Dose expression | DOSE |
| Extract | FRUIT |
| Gender | MALE |