Awni W M, Cavanaugh J H, Witt G, Granneman G R, Dubé L M
Pharmacokinetics and Biopharmaceutics Department, Abbott Laboratories, Abbott Park, Illinois, USA.
Clin Pharmacokinet. 1995;29 Suppl 2:62-6. doi: 10.2165/00003088-199500292-00009.
The present study was undertaken to assess the effect of food on the pharmacokinetic parameters of zileuton. In a nonblinded crossover study, 18 healthy male volunteers who had fasted overnight were randomised to receive a single oral dose of zileuton 600mg in the presence or absence of food consisting of a standardised breakfast on the following morning. The mean zileuton peak plasma concentration (Cmax) increased significantly by 27% after food intake, while the mean area under the plasma concentration versus time curve increased by only 1.4%, a difference that was not statistically significant. The mean time to Cmax was unaffected by the presence of food, as were the other pharmacokinetic parameters assessed. Overall, the results suggest that food has a relatively small effect on the rate of zileuton absorption compared with the fasting state, while the bioavailability of the drug appears to be unaffected. Thus, it is concluded that it is appropriate to administer zileuton with or without food.
本研究旨在评估食物对齐留通药代动力学参数的影响。在一项非盲交叉研究中，18名过夜禁食的健康男性志愿者被随机分组，在次日早晨有无包含标准化早餐的食物的情况下接受单次口服600mg齐留通。进食后，齐留通的平均血浆峰浓度（Cmax）显著升高27%，而血浆浓度-时间曲线下的平均面积仅增加1.4%，差异无统计学意义。达到Cmax的平均时间不受食物存在的影响，其他评估的药代动力学参数也是如此。总体而言，结果表明与禁食状态相比，食物对齐留通吸收速率的影响相对较小，而药物的生物利用度似乎未受影响。因此，得出结论，无论有无食物，服用齐留通都是合适的。
