Min D I, Ku Y M, Perry P J, Ukah F O, Ashton K, Martin M F, Hunsicker L G
College of Pharmacy, University of Iowa, Iowa City, 52242, USA.
Transplantation. 1996 Jul 15;62(1):123-5. doi: 10.1097/00007890-199607150-00023.
This study investigated the effect of grapefruit juice on cyclosporine A (CsA) bioavailability in 10 renal transplant patients. Under CsA steady state conditions, patients were randomly administered their usual dose of CsA with either 8 ounces of grapefruit juice or 8 ounces of water. Using a crossover design, a 12-hr pharmacokinetic study was then conducted. Grapefruit juice increased the area under the concentration versus time curve (4218+/-1497 ng x hr/ml [grapefruit juice] vs. 3415+/-1288 ng x hr/ml [water], P=0.029) and 12-hr trough (244+/-214 ng x ml [grapefruit juice] vs. 132+/-56 ng x ml [water], P=0.09), but it did not change peak concentration (734+/-290 ng x ml [grapefruit juice] vs. 708+/-305 ng x ml [water], P=0.76). In addition, grapefruit juice delayed the time to peak concentration compared with water (5.4+/-3.0 hr [grapefruit juice] vs. 2.8+/-0.8 hr [water], P=0.025). These data suggest that concurrent administration of grapefruit juice with CsA will delay the absorption of CsA and increase the drug exposure of CsA without changing peak concentration.
本研究调查了葡萄柚汁对10例肾移植患者中环孢素A（CsA）生物利用度的影响。在CsA稳态条件下，患者被随机给予其常规剂量的CsA，同时饮用8盎司葡萄柚汁或8盎司水。采用交叉设计，随后进行了一项12小时的药代动力学研究。葡萄柚汁增加了浓度-时间曲线下面积（[葡萄柚汁组]4218±1497 ng·hr/ml vs. [水组]3415±1288 ng·hr/ml，P = 0.029）以及12小时谷浓度（[葡萄柚汁组]244±214 ng/ml vs. [水组]132±56 ng/ml，P = 0.09），但未改变峰浓度（[葡萄柚汁组]734±290 ng/ml vs. [水组]708±305 ng/ml，P = 0.76）。此外，与水相比，葡萄柚汁延迟了达到峰浓度的时间（[葡萄柚汁组]5.4±3.0小时 vs. [水组]2.8±0.8小时，P = 0.025）。这些数据表明，葡萄柚汁与CsA同时给药会延迟CsA的吸收，并增加CsA的药物暴露量，而不改变峰浓度。
