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Comparison of the Effects of Single and Repeated Oral Doses of Lansoprazole and Rabeprazole on Ambulatory 24-Hour Intragastric pH in Healthy Volunteers

机译:兰索拉唑和雷贝拉唑单次和重复口服剂量对健康志愿者动态24小时胃内pH值影响的比较

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Background: As the comparative pharmacokinetics and pharmacodynamics of lansoprazole and rabeprazole have not previously been studied, we set out in this study to compare the pharmacokinetics and pharmacodynamics of single and repeated daily doses of lansoprazole 15mg and 30mg with those of rabeprazole 10mg and 20mg. Methods: This was an open-label, randomised, crossover, two-centre study in 72 healthy volunteers. Each subject received each of the four treatments for 5 days, with 2-week washout periods. Continuous 24-hour intragastric pH and pharmacokinetics were studied on days 1 and 5. Results: Mean 24-hour pH and percentage time for pH >4 were not significantly different between lansoprazole 30mg and rabeprazole 20mg. Mean 24-hour pH and percentage time for pH >4 were significantly greater after lansoprazole 30mg and rabeprazole 20mg than after lansoprazole 15mg and rabeprazole 10mg, respectively. Lansoprazole resulted in greater acid suppression during hours 0-5 on days 1 and 5, whereas rabeprazole had greater suppression during hours 11-24 on day 5. Time to maximum plasma concentration was significantly shorter for lansoprazole on both days. Conclusion: Lansoprazole had a consistently faster onset of action, whereas rabeprazole had a greater effect during the evening hours after 5 days of administration.
机译:背景:由于以前尚未研究过兰索拉唑和雷贝拉唑的比较药代动力学和药效学,因此我们在本研究中着手比较每日一次和反复服用兰索拉唑15mg和30mg与雷贝拉唑10mg和20mg的药代动力学和药效学。方法:这是一项对72位健康志愿者进行的开放标签,随机,交叉,两中心研究。每个受试者接受四种治疗中的每种治疗,持续5天,并有2周的洗脱期。在第1天和第5天研究了连续24小时胃内pH和药代动力学。结果:兰索拉唑30mg和雷贝拉唑20mg的平均24小时pH和pH> 4的百分比时间无显着差异。兰索拉唑30mg和雷贝拉唑20mg后,平均24小时pH和pH> 4的百分比时间分别显着大于兰索拉唑15mg和雷贝拉唑10mg后。兰索拉唑在第1天和第5天的0-5小时导致更大的酸抑制作用,而雷贝拉唑在第5天的第11-24小时具有更大的抑制酸作用。结论:兰索拉唑起效持续较快,而雷贝拉唑在给药5天后的晚上具有更大的作用。

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