The effects of pummelo juice on pharmacokinetics of sildenafil in healthy adult male Jordanian volunteers
The effects of pummelo juice on pharmacokinetics of sildenafil in healthy adult male Jordanian volunteers
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DOI：
10.1007/s00228-009-0738-0
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发表时间：
2010-02-01
影响因子：
2.9
通讯作者：
AbuRuz, Salah M.
中科院分区：
文献类型：
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作者：
Al-Ghazawi, Mutasim A.;Tutunji, Maha S.;AbuRuz, Salah M.
目的研究柚汁对口服西地那非药动学的影响。方法：本研究是一项比较、随机、两期、两处理、两顺序、单剂量、交叉研究，研究在空腹条件下，柚汁对枸橼酸西地那非片（相当于50 mg西地那非）在健康男性受试者体内的药代动力学的影响，并与水作对照。在一项交叉研究中，6名健康的正常成年男性在两个不同的时期给药50毫克西地那非和柚子汁或水。结果研究结果表明，柚汁可使西地那非生物利用度降低60%左右[最大血药浓度（C(max)）]；从212.44 ng/ml到134.07 ng/ml， 90%置信区间（90% CI） 44.70 ~ 89.11，血药浓度时间曲线下面积（AUC(∞)）从0到∞；从564.51 ng。Hr /ml降至336.87 ng。hr/ml, 90% CI 39.17-90.92]。这种相互作用与预期相反，推测是由于对转运蛋白的影响或西地那非与果汁中的某些成分之间的物理化学相互作用。结论患者在服用西地那非之前或服用后立即不宜饮用柚汁。
Purpose The main purpose of this work was to investigate the effect of pummelo juice on the pharmacokinetics of sildenafil after oral administration.Methods This was a comparative, randomized, two-period, two-treatment, two-sequence, single dose, crossover study investigating the effect of pummelo juice on the pharmacokinetics of sildenafil citrate tablets (equivalent to 50 mg sildenafil) in healthy male participants under fasting conditions compared with water as a control. Six healthy normal adult males were administered 50 mg sildenafil with pummelo juice or water at two different periods in a crossover study.Results Study results showed that pummelo juice reduced the rate and extent of sildenafil bioavailability to around 60% [maximum plasma concentration (C(max)); from 212.44 ng/ml to 134.07 ng/ml, 90% confidence interval (90% CI) 44.70-89.11, and area under the plasma concentration time curve from zero to infinity (AUC(infinity)); from 564.51 ng.hr/ml to 336.87 ng.hr/ml, 90% CI 39.17-90.92]. This interaction was opposite to that expected and is speculated to be due to either an effect on transporters or a physicochemical interaction between sildenafil and some components of the juice.Conclusion Patients should be advised not to drink pummelo juice before or immediately after taking sildenafil.