Clinical Applications Lab., Inc. San Diego California.
Merck & Co. Kenilworth New Jersey.
Pharmacol Res Perspect. 2016 May 19;4(3):e00238. doi: 10.1002/prp2.238. eCollection 2016 Jun.
Proton pump inhibitors (PPIs) effectively block gastric acid secretion and are the treatment of choice for heartburn. PPIs differ, however, in onset of action and bioavailability. In this single-center, open-label, three-way crossover study, onset of action of immediate-release omeprazole 20 mg/sodium bicarbonate 1100 mg (IR-OME) and delayed-release (DR) lansoprazole 15 mg was evaluated in 63 healthy fasting adults. Subjects were randomized to once daily IR-OME, or DR-lansoprazole, or no treatment for 7 days. The primary efficacy endpoint was the earliest time where a statistically significant difference was observed between IR-OME and DR-lansoprazole in median intragastric pH scores for three consecutive 5-min intervals on day 7. Secondary endpoints compared effects of active treatments on days 1 and 7 (e.g., time to sustained inhibition, percentage of time with pH >4). A significant difference in median intragastric pH favoring IR-OME was observed on day 7 starting at the 10- to 15-min interval postdosing (P = 0.024) and sustaining through the 115- to 120-min interval (P = 0.017). On day 1, IR-OME achieved sustained inhibition of intragastric acidity significantly faster than DR-lansoprazole. IR-OME maintained pH >4 significantly longer than DR-lansoprazole over a 24-h period (P = 0.007) on day 7. Overall, results of this study demonstrate IR-OME is safe and well tolerated and that treatment with IR-OME results in significantly faster onset of action and better gastric acid suppression at steady state than DR-lansoprazole.
质子泵抑制剂（PPIs）能有效抑制胃酸分泌，是治疗烧心的首选药物。然而，不同的 PPI 在起效时间和生物利用度方面存在差异。在这项单中心、开放标签、三交叉研究中，评估了口服 20mg 奥美拉唑和 1100mg 碳酸氢钠（IR-OME）及口服 15mg 兰索拉唑（DR）在 63 名健康空腹成年人中的起效时间。受试者随机分为每日一次 IR-OME、DR-兰索拉唑或不治疗 7 天。主要疗效终点是第 7 天三个连续 5 分钟间隔内最早观察到 IR-OME 和 DR-兰索拉唑之间中位胃内 pH 评分存在统计学差异的时间。次要终点比较了两种活性药物在第 1 天和第 7 天的作用（例如，持续抑制时间、pH 值>4 的时间百分比）。第 7 天，IR-OME 组在给药后 10-15 分钟（P=0.024）和 115-120 分钟（P=0.017）开始，中位胃内 pH 值出现有利于 IR-OME 的显著差异。第 1 天，IR-OME 实现胃内酸度持续抑制的速度明显快于 DR-兰索拉唑。第 7 天，IR-OME 在 24 小时内保持 pH 值>4 的时间明显长于 DR-兰索拉唑（P=0.007）。总的来说，这项研究的结果表明，IR-OME 是安全且耐受良好的，与 DR-兰索拉唑相比，IR-OME 治疗可显著更快地起效，在稳态时可更好地抑制胃酸。
