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首页> 美国卫生研究院文献>other >Grapefruit juice lyophilized grapefruit juice and powdered whole grapefruit inhibit cytochrome P450 mediated triazolam hydroxylation by beagle dog liver microsomes
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Grapefruit juice lyophilized grapefruit juice and powdered whole grapefruit inhibit cytochrome P450 mediated triazolam hydroxylation by beagle dog liver microsomes

机译：葡萄柚汁冻干葡萄柚汁糖粉整体葡萄柚抑制细胞色素p450介导的特唑胺羟基化由比格犬肝微粒体

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Coadministration of grapefruit juice has been proposed to enhance the systemic availability and decrease the required dose of drugs such as cyclosporine that are extensively metabolized in the intestine and liver. Although grapefruit juice inhibits human cytochrome P450 (CYP) 3A, effects on dog CYP have not yet been reported. Consequently, we determined whether grapefruit juice (GFJ) inhibits triazolam hydroxylation by Beagle dog liver microsomes (DLM) using human liver microsomes (HLM) as positive control. Results were compared to effects of lyophilized GFJ and commercially-available powdered grapefruit capsules, which may be more convenient dosage forms. GFJ inhibited α-hydroxytriazolam formation in both DLM and HLM with similar IC50 values of 0.56 and 0.52% (v/v), respectively. Lyophilized GFJ and powdered grapefruit also inhibited DLM α-hydroxytriazolam formation with IC50 values of 0.76 and 1.2 mg / mL, respectively. Consistent with mechanism-based enzyme inhibition, preincubation of DLM with any of the grapefruit products for 20 minutes resulted in significant enhancement of inhibition of triazolam α-hydroxylation by 8 to 20%. The results indicate that 16 grams of lyophilized GFJ or 23 grams of powdered grapefruit would be equivalent to dosing 100 mL of GFJ. In vivo pharmacokinetic interaction studies are needed to confirm these in vitro findings.

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