Research & Development, Takeda Global Research & Development Center, Inc., Deerfield, IL 60015, USA.
Aliment Pharmacol Ther. 2010 May;31(9):1001-11. doi: 10.1111/j.1365-2036.2010.04272.x. Epub 2010 Feb 20.
Dexlansoprazole MR is a Dual Delayed Release proton pump inhibitor formulated to extend the duration of acid suppression.
To evaluate the pharmacokinetics and pharmacodynamics of dexlansoprazole MR dosed before 4 different meal times.
In this randomized, open-label, four-way crossover study, 48 healthy subjects received dexlansoprazole MR 60 mg once daily 30 min before breakfast, lunch, dinner or an evening snack. Pharmacokinetics of dexlansoprazole MR and intragastric pH were assessed over a 24-h postdose interval on day 5 for each regimen.
Absorption was delayed when dexlansoprazole MR was administered before each regimen relative to breakfast; however, systemic exposures of dexlansoprazole at all regimens were bioequivalent. There were no statistically significant differences in mean 24-h intragastric pH between dosing before dinner or an evening snack vs. breakfast; however, there was a small (0.2), but statistically significant difference between lunch and breakfast. There was a statistically significant difference of 7 percentage points in the percentage of time intragastric pH was >4 for the snack regimen relative to the breakfast regimen, but there were no statistically significant differences between lunch or dinner compared with breakfast.
Dexlansoprazole MR provides comparable acid control when administered at different times of the day.
多库兰索拉唑 MR 是一种双重延迟释放质子泵抑制剂，旨在延长酸抑制的持续时间。
评估多库兰索拉唑 MR 在 4 种不同用餐时间前给药的药代动力学和药效学。
在这项随机、开放标签、四向交叉研究中，48 名健康受试者每天一次接受多库兰索拉唑 MR 60mg，在早餐、午餐、晚餐或晚餐小吃前 30 分钟服用。在每种方案的第 5 天，在给药后 24 小时内评估多库兰索拉唑 MR 的药代动力学和胃内 pH 值。
与早餐相比，在每种方案前给药时，多库兰索拉唑 MR 的吸收被延迟；然而，所有方案的多库兰索拉唑的全身暴露均具有生物等效性。在晚餐或小吃与早餐相比，24 小时内平均胃内 pH 值没有统计学显著差异；然而，与早餐相比，午餐和早餐之间存在较小的（0.2）但统计学显著差异。与早餐相比，小吃方案胃内 pH 值>4 的时间百分比有统计学显著差异增加了 7 个百分点，但与午餐或晚餐相比，无统计学显著差异。
多库兰索拉唑 MR 在一天中的不同时间给药时提供相当的酸控制。
