The Use of Heat Treatment to Eliminate Drug Interactions Due to Grapefruit Juice(Biopharmacy)

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概要

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• Grapefruit juice (GJ) contains components that may increase the bioavailability of drugs; however, approaches to the removal of these components have been little investigated. It is known that furanocoumarin derivatives (FCs), such as bergamottin (BG) and 6',7'-dihydroxybergamottin (DHB) in GJ, induce such drug interactions. In the present study, it was found that the heat treatment of grapefruit juice decreases concentrations of BG and DHB as well as their interactions both in vitro and in vivo. We incubated GJ for 10, 20, 30, 40, 50, and 60 min at 37, 62, 72, and 95℃; FCs in each sample were then measured, using high-performance liquid chromatography (HPLC). The concentrations of BG and DHB were decreased in a time- and temperature-dependent manner, by 82.5 and 97.9% respectively, after incubation for 1h at 95℃. In contrast, the concentration of bergaptrol (BT) increased in a time- and temperature-dependent manner (27.7% after 60 min at 95℃). In addition, the effect of each GJ sample on testosterone 6β-oxidation in human liver microsomes was observed. The inhibitory effects of GJ heated to 95℃ were decreased in a time-dependent manner, as in the case of BG and DHB concentrations. Furthermore, 2ml of GJ treated for 60 min at 95℃ was administered into the rat duodenum. After 30 min, nifedipine (NFP) was administered intraduodenally at a dose of 3mg/kg body weight. The concentrations of NFP in the plasma samples were determined by HPLC. No significant increase in the AUC of NFP was observed in the rats given heat-treated GJ. These results suggest that the heat treatment of GJ reduces the concentrations of FCs, thus eliminating the potential for drug interactions.

• 公益社団法人日本薬学会の論文
• 2006-11-01

著者

• Uesawa Yoshihiro

  明治薬科大学 臨床薬剤学

• Uesawa Yoshihiro

  Clinical Pharmaceutics Laboratory Department Of Pharmaceutics Meiji Pharmaceutical University

• Mohri Kiminori

  Clinical Pharmaceutics Laboratory Department Of Pharmaceutics Meiji Pharmaceutical University

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• The Use of Heat Treatment to Eliminate Drug Interactions Due to Grapefruit Juice(Biopharmacy)
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• UV-Irradiated Grapefruit Juice Loses Pharmacokinetic Interaction with Nifedipine in Rats(Biopharmacy)

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