埃索美拉唑给药时间与食物摄入的关系对其药代动力学的影响。
Effect of timing of dosing in relation to food intake on the pharmacokinetics of esomeprazole.
作者信息
Sostek Mark B, Chen Yusong, Andersson Tommy
机构信息
AstraZeneca LP, Wilmington, DE, USA.
出版信息
Br J Clin Pharmacol. 2007 Sep;64(3):386-90. doi: 10.1111/j.1365-2125.2007.02889.x. Epub 2007 Apr 10.
Abstract
AIM
To investigate the pharmacokinetics of esomeprazole before a high-fat meal vs. fasting.
METHODS
This open-label, randomized, crossover study consisted of two 5-day dosing periods of esomeprazole 40 mg per day. On days 1 and 5, subjects received esomeprazole 15 min before a high-fat meal (fed) or 4 h before a non-high-fat meal (fasting).
RESULTS
On days 1 and 5, ratio of fed to fasting area under the plasma concentration-time curve [0.56, 90% confidence interval (CI) 0.50, 0.64, and 0.78, 90% CI 0.74, 0.82, respectively] and peak plasma concentration (0.34, 90% CI 0.28, 0.41, and 0.47, 90% CI 0.41, 0.52, respectively) were outside of the limits of bioequivalence.
CONCLUSIONS
Esomeprazole bioavailability was reduced when taken within 15 min before eating a high-fat meal vs. that while fasting.
摘要
目的
研究高脂餐前与空腹时埃索美拉唑的药代动力学。
方法
本开放标签、随机、交叉研究包括两个为期5天的给药期，每天服用40毫克埃索美拉唑。在第1天和第5天，受试者在高脂餐前15分钟（进食状态）或非高脂餐前4小时（空腹状态）服用埃索美拉唑。
结果
在第1天和第5天，血浆浓度-时间曲线下进食状态与空腹状态的面积比[分别为0.56，90%置信区间（CI）0.50，0.64；以及0.78，90%CI 0.74，0.82]和血浆峰浓度[分别为0.34，90%CI 0.28，0.41；以及0.47，90%CI 0.41，0.52]均超出生物等效性限度。
结论
与空腹时相比，在高脂餐前15分钟内服用埃索美拉唑时，其生物利用度降低。
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