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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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Bibliographic Details
Published in:Pharmacological research 2003, Vol.47 (1), p.87-92
Main Authors: Giorgi, M., Meucci, V., Vaccaro, E., Mengozzi, G., Giusiani, M., Soldani, G.
Format: Article
Language:English
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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.
ISSN:1043-6618
1096-1186
DOI:10.1016/S1043-6618(02)00251-7