雷贝拉唑钠拆分体对大鼠实验性胃溃疡作用的比较研究  

Comparison of the effects of rabeprazole sodium and its racemes on experimental gastric ulcer in rats

作　　者：许庆华[1] 李宗河[1] 黄菲菲[1] 王昉彤[1] 

机构地区：[1]四川抗菌素工业研究所药理学教研室,成都610052

出　　处：《中国新药杂志》2015年第8期917-923,共7页Chinese Journal of New Drugs

摘　　要：目的:比较雷贝拉唑钠右旋体、左旋体和消旋体对H+,K+-ATP酶活性抑制作用的强弱,以及体内抗实验性大鼠胃溃疡作用的强弱。方法:取正常SD大鼠胃黏膜,体外测定雷贝拉唑钠右旋体、左旋体以及消旋体对H+,K+-ATP酶的抑制作用。建立水应激型、消炎痛刺激、幽门结扎法3种大鼠胃溃疡模型,观察三者对实验性胃溃疡形成的影响。并在水应激模型中取SD大鼠胃黏膜测定体内对H+,K+-ATP酶活性的影响。结果:右旋体、左旋体以及消旋体体外抑制H+,K+-ATP酶的活性未见明显差异;但在水应激模型中体内对H+,K+-ATP酶活性有抑制作用,且雷贝拉唑钠右旋体>左旋体和消旋体。与模型组比较,雷贝拉唑钠右旋体对3种SD大鼠实验性胃溃疡具有明显的抑制作用(P<0.01或P<0.05),效果优于消旋体和左旋体,能显著抑制胃溃疡的发生。结论:体外H+,K+-ATP酶活性抑制测定结果,三者之间抑制效果没有明显差异;但体内酶活性抑制作用雷贝拉唑钠右旋体强于消旋体和左旋体。等剂量雷贝拉唑钠右旋体对3种大鼠胃溃疡的抗溃疡作用强于消旋体和左旋体。Objective： To compare the inhibiting effects of rabeprazole sodium and its isomers on H ^＋ , K ^＋ ATPase activity, and experimental gastric ulcer in rats. Methods： The anti-ulcer effects of rabeprazole and its isomers were evaluated in three different rat models of gastric ulcer, namely pyloric ligation, indomethacin stimulation, and water stress. H^＋ , K ^＋ -ATPase activity of gastric mucosa was determined in normal or water stress rats. Results： Compared with ulcer control, dexrabeprazole significantly inhibited the development of gastric ulcer in three models （P 〈0.01 or P 〈 0.05）, and its effect was more potent than the S （ - ）-isomer and rabeprazole. Dexrabeprazole, rabeprazole and S（ - ）-isomer had similar inhibiting effects on H ^＋ , K ^＋ -ATPase activity in vitro. However, dexrabeprazole had an inhibiting effect on H ^＋ , K ^＋ -ATPase activity more potent than rabeprazole and the S（ -）-isomer in vivo. Conclusion： Three drugs have similar effects on H^＋, K^＋-ATPase activity in vitro; but dexrabeprazole is more potent than rabeprazole and the S（ - ）-isomer in vivo. Dexrabeprazole is superior to rabeprazole and S（ - ）-isomer at the same doses for inhibiting gastric ulcer in three rat models.

关 键 词：雷贝拉唑钠右旋体 胃溃疡 H+ K+-ATP酶活性 抑制作用 

分 类 号：R975[医药卫生—药品]