Lundahl J, Regårdh C G, Edgar B, Johnsson G
Department Clinical Research, Malmö, Sweden.
Eur J Clin Pharmacol. 1995;49(1-2):61-7. doi: 10.1007/BF00192360.
In this randomised, cross-over study, in nine healthy males given felodipine ER 10 mg PO 200 ml grapefruit juice was found to increase the plasma levels of felodipine even when the juice was taken 24 hours before the drug. Grapefruit juice drunk simultaneously with and 1, 4, 10 or 24 hours before the drug administration resulted in a 32-99% increase in mean Cmax values of felodipine, relative to concomitant water and felodipine intake. The effect on AUC was also significant when juice was taken up to 10 h before the drug. The effect of the interaction decreased with increasing time between juice and drug intake. All treatments produced a significant decrease in diastolic blood pressure and an increase in heart rate in comparison with morning basal values. The change in haemodynamic variables was approximately the same after all treatment combinations. Headache was reported more frequently after treatments including grapefruit juice.
在这项随机交叉研究中，对9名健康男性口服10毫克非洛地平缓释片后发现，即使在服药前24小时饮用200毫升葡萄柚汁，也会使非洛地平的血浆水平升高。与药物同时服用以及在给药前1、4、10或24小时饮用葡萄柚汁，相对于同时摄入水和非洛地平，非洛地平的平均Cmax值增加了32%-99%。当在给药前长达10小时饮用果汁时，对AUC的影响也很显著。果汁与药物摄入之间的时间间隔越长，相互作用的影响越小。与早晨基础值相比，所有治疗均使舒张压显著降低，心率增加。所有治疗组合后血流动力学变量的变化大致相同。在包括葡萄柚汁的治疗后，头痛的报告更为频繁。
