伊曲康唑血浆浓度的增加但葡萄柚汁大大减少塞。
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Lilja JJ,后方JT Laitila J, Luurila H, Neuvonen PJ
伊曲康唑血浆浓度的增加但葡萄柚汁大大减少塞。
中国新药杂志。2003年3月,73 (3):192 - 8。
- PubMed ID
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12621384 (在PubMed]
- 文摘
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目的:我们的目的是评价伊曲康唑的影响和葡萄柚汁的药物动力学该项receptor-blocking剂塞在健康志愿者。方法:在随机三相交叉研究中,12名健康志愿者口服伊曲康唑200毫克或安慰剂,一天两次或200毫升葡萄柚汁每天3次,2天。第三天上午,1小时后摄入的伊曲康唑,安慰剂或葡萄柚汁,每个主题用200毫升水摄入100毫克塞(安慰剂和伊曲康唑阶段)或葡萄柚汁。此外,200毫升的水或葡萄柚汁摄取4和10小时后塞摄入量。伊曲康唑血浆浓度的塞,hydroxyitraconazole和尿液的排泄塞进测量剂量后33小时。收缩期和舒张期血压和心率与科目记录坐姿前塞和2,4,6,10个小时后。结果:在伊曲康唑阶段,平均面积血浆浓度时间曲线从0到33小时塞(AUC(0-33))为80% (P < . 05)大于安慰剂的阶段。在葡萄柚汁阶段,平均AUC值(0-33)和血浆浓度峰值塞被减少到约13% (P <措施)和5% (P <措施)各自的安慰剂相值。累计排泄的尿液塞被伊曲康唑增加了59% (P < . 05)下降了85%,葡萄柚汁(P <措施)。血流动力学变量阶段之间没有差别。 CONCLUSIONS: Itraconazole almost doubles but grapefruit juice greatly reduces plasma concentrations of celiprolol. The itraconazole-celiprolol interaction most likely resulted from increased absorption of celiprolol possibly as a result of P-glycoprotein inhibition in the intestine. The reduced celiprolol concentrations during the grapefruit juice phase were probably caused by physicochemical factors that interfered with celiprolol absorption, although other mechanisms cannot be excluded. The grapefruit juice-celiprolol interaction is probably of clinical relevance.