The Effect of Food on the Pharmacokinetics of the Potassium-Competitive Acid Blocker Vonoprazan.
The Effect of Food on the Pharmacokinetics of the Potassium-Competitive Acid Blocker Vonoprazan.
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DOI：
10.1002/cpdd.1009
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发表时间：
2022-03
影响因子：
2
通讯作者：
中科院分区：
文献类型：
--
作者：
在这里，我们报告了一项关于口服竞争钾酸阻滞剂vonoprazan的食品效应研究。在第一阶段随机开放标签交叉研究中，健康受试者在隔夜禁食后或高脂早餐后30分钟接受一次20毫克的vonoprazan。在给药后0小时和随后的17个评估点测定血浆vonoprazan浓度，直至48小时。经过5天的洗涤后，受试者在交替进食/禁食状态下接受第二次20毫克的vonoprazan剂量(重复相同的过程)。24名受试者完成了这项研究。Vonoprazan的暴露并没有受到食物的显著影响。在进食和禁食条件下，最大血药浓度、0-24小时血药浓度-时间曲线下面积和外推至无穷大的血药浓度-时间曲线下面积的几何平均值分别为1.05(90%可信区间0.98-1.12)、1.13(1.09-1.18)和1.15(1.11-1.19)。四名受试者经历了6次不良反应，这些不良反应都很轻微，被认为与研究药物无关。Vonoprazan可以在不考虑食物摄入的情况下使用。
Herein, we report a food‐effect study of vonoprazan, an oral potassium‐competitive acid blocker. In a phase 1, randomized, open‐label, crossover study, healthy subjects received a single 20‐mg dose of vonoprazan either following an overnight fast or 30 minutes after a high‐fat breakfast. Plasma vonoprazan levels were determined at 0 hour and at 17 subsequent assessment points up to 48 hours after dosing. After a 5‐day washout, subjects received a second 20‐mg vonoprazan dose in the alternative fed/fasted state (identical process repeated). Twenty‐four subjects completed the study. Vonoprazan exposure was not meaningfully affected by food. Geometric mean ratios for maximum concentration, area under the concentration‐time curve from time 0 to 24 hours, and area under the plasma concentration–time curve extrapolated to infinity obtained under fed and fasting conditions were 1.05 (90% confidence interval, 0.98‐1.12), 1.13 (1.09‐1.18), and 1.15 (1.11‐1.19), respectively. Four subjects experienced 6 adverse events that were all mild and considered unrelated to the study drug. Vonoprazan can be administered without regard to food intake.
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Vonoprazan Fumarate是一种新型的钾肥酸阻滞剂，用于胃食管反流疾病的管理：迄今为止的安全性和临床证据。
影响因子：
4.2
作者：
Sugano K
通讯作者：
Sugano K
影响因子：
3.9
作者：
Astruc, B.;Jenkins, H.;Jenkins, R.
通讯作者：
Jenkins, R.
影响因子：
2.1
作者：
Furuta, Takahisa;Shirai, Naohito;Ishizaki, Takashi
通讯作者：
Ishizaki, Takashi
影响因子：
3.5
作者：
Nishida, Haruyuki;Hasuoka, Atsushi;Kajino, Masahiro
通讯作者：
Kajino, Masahiro
影响因子：
7.6
作者：
Fennerty, MB;Johanson, JF;Sostek, M
通讯作者：
Sostek, M