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首页> 外文期刊>Clinical Pharmacology and Therapeutics >Pomegranate juice and pomegranate extract do not impair oral clearance of flurbiprofen in human volunteers: Divergence from in vitro results
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Pomegranate juice and pomegranate extract do not impair oral clearance of flurbiprofen in human volunteers: Divergence from in vitro results

机译：石榴果汁和石榴提取物不会损害人类志愿者的佛索口服清关：来自体外结果的分歧

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摘要

Nutrient interactions with prescription drugs are a topic of ongoing basic and clinical research. Pomegranate juice and a 1-g capsule containing pomegranate extract were evaluated in vitro and in vivo as inhibitors of cytochrome P450 2C9 (CYP2C9), with flurbiprofen serving as the index substrate. Fluconazole was the positive control inhibitor. The in vitro 50% inhibitory concentration (IC 50) values for pomegranate juice and extract were below 1% (vol/vol), with no evidence of mechanism-based (irreversible) inhibition. In clinical studies, flurbiprofen pharmacokinetics were unchanged by pomegranate juice or extract as compared to a low-polyphenol placebo control beverage. However, fluconazole significantly reduced the oral clearance of flurbiprofen. Despite inhibition of CYP2C9 in vitro, pomegranate juice and extract had no effect on CYP2C9 activity in human subjects, and can be consumed by patients taking CYP2C9 substrate drugs with negligible risk of a pharmacokinetic interaction.
机译：与处方药的营养相互作用是正在进行的基本和临床研究的主题。 在体外和体内评估石榴汁和含有石榴提取物的1g胶囊作为细胞色素P450 2C9（CYP2C9）的抑制剂，用Flbiprofen用作指数底物。 氟康唑是阳性对照抑制剂。 石榴汁和提取物的体外50％抑制浓度（IC 50）值低于1％（Vol /体积），没有基于机制（不可逆的）抑制的证据。 在临床研究中，与低多酚安慰剂对照饮料相比，石绿醇汁或提取物不变。 然而，氟康唑显着降低了流泡的口腔间隙。 尽管在体外抑制CYP2C9，石榴汁和提取物对人类受试者的CYP2C9活性没有影响，并且可以通过服用CYP2C9底物药物的患者消耗可忽略的药代动力学相互作用。

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    HanleyM.J.; MasseG.; HarmatzJ.S.; CourtM.H.; GreenblattD.J.;

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    Program in Pharmacology and Experimental Therapeutics Sackler School of Graduate Biomedical;

    Program in Pharmacology and Experimental Therapeutics Sackler School of Graduate Biomedical;

    Program in Pharmacology and Experimental Therapeutics Sackler School of Graduate Biomedical;

    Program in Pharmacology and Experimental Therapeutics Sackler School of Graduate Biomedical;

    Program in Pharmacology and Experimental Therapeutics Sackler School of Graduate Biomedical;

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  • 正文语种 eng
  • 中图分类 药理学;
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