The change of pharmacokinetics of fexofenadine enantiomers through the single and simultaneous grapefruit juice ingestion
作者: Yumiko AkamineMasatomo MiuraHisakazu KomoriIkumi TamaiIchiro IeiriNorio Yasui-FurukoriTsukasa Uno
作者单位: 1Department of Pharmacy, Akita University Hospital, Akita, Japan
2Faculty of Pharmacy, Institute of Medical, Pharmaceutical and Health Sciences, Kanazawa University, Kanazawa, Japan
3Department of Clinical Pharmacokinetics, Graduate School of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan
4Department of Neuropsychiatry, Hirosaki University School of Medicine, Hirosaki, Japan
5Department of Pharmacy, Zikeikai-Aoimori Hospital, Aomori, Japan
刊名: Drug Metabolism and Pharmacokinetics, 2015, Vol.30 (5), pp.352-357
来源数据库: Elsevier Journal
DOI: 10.1016/j.dmpk.2015.06.005
关键词: EnantiomerFexofenadineGrapefruit juiceOATP2B1Pharmacokinetics
英文摘要: Abstract(#br)The stereoselective pharmacokinetics of fexofenadine are associated with OATP2B1-mediated transport, and grapefruit juice (GFJ) is an inhibitor of OATP2B1. Therefore, in this study, we aimed to investigate whether and to what extent GFJ ingestion affected the pharmacokinetics of fexofenadine enantiomers in healthy subjects. In a randomized, two-phase, open-label, crossover study, 14 subjects received 60 mg of racemic fexofenadine simultaneously with water or GFJ. Ingestion of GFJ significantly decreased the areas under the plasma concentration-time curve (AUC 0–24 ) for ( R )- and ( S )-fexofenadine by 39% and 52%, respectively. Subsequently, GFJ increased the mean R/S ratio of the AUC 0–24 from 1.58 to 1.96 ( P < 0.05). Although GFJ greatly reduced the amounts of ( R )- and...
全文获取路径: Elsevier  (合作)
影响因子:2.071 (2012)

  • grapefruit 葡萄柚黄
  • juice 
  • simultaneous 同时的
  • change 变化
  • ingestion 摄食
  • single 单独的
  • through 经过