UV-Irradiated Grapefruit Juice Loses Pharmacokinetic Interaction with Nifedipine in Rats(Biopharmacy)

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In the present study, UV-irradiated grapefruit juice was used to investigate the effects of UV light on nifedipine pharmacokinetics. Grapefruit juice in quartz vessels was UV irradiated (302nm) with a transillumi-nator for 0 to 6h at 4℃, and furanocoumarins, potent contributors to the pharmacokinetic interaction, in each juice sample were measured using HPLC. The concentrations of all three types of furanocoumarins, bergamottin, 6',7'-dihydroxybergamottin, and bergaptol, decreased in a time-dependent manner. Concentrations of bergamottin, 6',7'-dihydroxybergamottin, and bergaptol were decreased to 1.66, 1.98, and 5.58%, respectively, after UV irradiation for 6h. Two milliliters of untreated and UV-irradiated grapefruit juice were preadministered into the duodenum in rats to assess the effects of UV irradiation on nifedipine pharmacokinetics in vivo. After 30 min, nifedipine was intraduodenally administered at a dose of 3mg/kg body weight. The nifedipine concentrations in the plasma samples were determined using HPLC. A significant increase in the area under the concentration-time curve of nifedipine was observed in untreated grapefruit juice to 1.6-fold that in the control group, but not in the UV-irradiated grapefruit juice. These findings suggest that UV irradiation is useful to eliminate pharma-cokinetic interactions with grapefruit juice.
公益社団法人日本薬学会の論文
2006-06-01