三种不同剂量埃索美拉唑对健康志愿者胃内pH值的影响

Effect of esomeprazole with different dosage and usage on intragastric pH of healthy volunteers

目的观察不同剂量埃索美拉唑对健康志愿者胃内pH值的影响。方法研究为随机、开放、三交叉设计试验，入选的15名健康志愿者分别按3种剂量口服埃索美拉唑[每日1次每次20mg（A剂量）、每日1次每次40mg（B剂量）、每日2次每次20mg（C剂量）]，每种剂量连续口服5d，第5天时进行24h胃内pH值监测。结果按A、B、C三种剂量口服埃索美拉唑5d后，24h胃内pH值〉4的时间分别为（18．70±4．19）、（19．27±2．68）、（21．16±2．45）h，其中C剂量与其余2种用法比较，差异均有统计学意义（P值均〈0．05），其余2种用法间比较差异无统计学意义（P〉0．05）。C剂量埃索美拉唑用药后胃内全天和夜间的中位pH值及胃内pH值〉3、4、5的时间百分比（全天：6．73±0．64、95．0％±7．5％、92．0％±10．6％、86．7％±14．5％；夜间：6．22±1．30、93．2％±13．1％、87．8％±20．3％、78．6％±28．9％）与A剂量（全天：5．99±1．83、85．1％±16．3％、81．1％±18．1％、71．5％±20．3％；夜间：4．90±2．14、72．9％±30．5％、67．2％±31．9％、55．7％±31．8％）和B剂量（全天：6．33±0．62、87．9％±9．5％、83．5％±11．7％、75．6％±15．5％；夜间：4．93±1.60、75．7％±20．8％、66．9％±23．8％、53．3％±30．3％）这2种用法比较，差异均有统计学意义（P值均〈0．05），后2种用法间比较差异均无统计学意义（P值均〉0．05）。结论埃索美拉唑具有较强的抑酸作用，每日2次每次20mg的剂量抑酸效果优于每日1次每次20mg和每日1次每次40mg，后2种方法抑酸效果相似。

Objective To evaluate the effect of esomeprazole with different dosage and usage regimes on intragastric pH of healthy volunteers. Methods It was a randomized, open-label, three- way crossover study. Fifteen healthy volunteers received esomeprazole with 3 different dosages （20 mg or 40 mg once daily or 20 mg twice daily） with 5 days each. Twenty-four continuous ambulatory intragastric pH was recorded at day 5 of each regime. Results The mean time of intragastric pH above 4 was higher in regime of 20 mg twice daily [（21.16 ±2.45） hours ] than that in regimes of 20 mg once daily [（18.70±4.19） hours] and 40 mg once daily [-（19.27±2.68 ） hours] （P〈0.05）. The percentages of the sleeping and active period that pH remained above 3,4,5 were significantly higher in regime of 20 mg twice daily（day time： 95. 0%±7.5% ,92.0%±10.6% ,86.7%± 14.5% ;night time：93.2%±13.1 % ,87.8%± 20.3% ,78.6%±28. 9%） compared with regimes of 40 mg once daily（day time：87.9%±9.5% ,83.5%± 11.7%,75.6%±15.5%,night time： 75.7%±20.8%,66.9%±23.8%,53.3%±30.3%） and 20 mg once daily（day time： 85.1%±16.3%, 81.1%±18. 1%, 71.5%±20.3% ; night time： 72.9 %±30.5%, 67.2%±31.9% ,55.7%±31.8%）（P〈0.05）. Esomeprazole maintained intragastric pH above these pH thresholds for a similar propotion of sleeping and active periods with 40 mg once daily and 20 mg once daily. Conclusions Esomeprazole has strong inhibitory effect on intragastric acid. The regime of 20 mg twice daily is superior to 40 mg once daily and 20 mg once daily in both day and night time acid inhibition. There is no difference between esomeprazole 40 mg once daily and 20 mg once daily.