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Effects of liquid and freeze-dried grapefruit juice on the pharmacokinetics of praziquantel and its metabolite 4′-hydroxy praziquantel in beagle dogs
Grapefruit juice changes the pharmacokinetic parameters of a variety of drugs metabolized primarily by cytochrome P450 3A. In a three-phase crossover study, six male beagle dogs were administered 100 ml of water (control), 100 ml of commercial liquid grapefruit juice, or 10 g of freeze-dried grapefr...
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Published in: | Pharmacological research 2003, Vol.47 (1), p.87-92 |
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Main Authors: | , , , , , |
Format: | Article |
Language: | English |
Subjects: | |
Citations: | Items that this one cites Items that cite this one |
Online Access: | Get full text |
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Summary: | Grapefruit juice changes the pharmacokinetic parameters of a variety of drugs metabolized primarily by cytochrome P450 3A. In a three-phase crossover study, six male beagle dogs were administered 100
ml of water (control), 100
ml of commercial liquid grapefruit juice, or 10
g of freeze-dried grapefruit juice (equivalent to 100
ml of liquid grapefruit juice) with 100
ml of water, followed after 2
h by single oral dose of praziquantel (30
mg
kg
−1). After treatment, the dogs were sampled at different times. Determination of praziquantel and its metabolite 4′-hydroxy praziquantel (identified by GC/MS) was performed by HPLC. Liquid and freeze-dried grapefruit juice preadministration increased the
C
max of praziquantel about three-fold and the AUC 2.5- and 2.3-fold, respectively. The
T
max (0.75
h) was unaffected by liquid or freeze-dried grapefruit juice, while
T
1/2 was 2.3- and 1.7-fold higher compared with controls. The amount of 4′-hydroxy praziquantel was also affected by both liquid and freeze-dried grapefruit juice administration: the AUC and
C
max increased four- and three-fold, respectively and the
T
max was significantly enhanced.
These findings demonstrate that both freeze-dried grapefruit juice and commercial liquid grapefruit juice significantly increase plasma concentrations and
T
1/2 of praziquantel in dogs. |
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ISSN: | 1043-6618 1096-1186 |
DOI: | 10.1016/S1043-6618(02)00251-7 |