左旋泮托拉唑钠对应激性大鼠胃溃疡的影响
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摘要
目的:探讨泮托拉唑钠中的主要活性成份和作用强度,为左旋泮托拉唑钠的临床开发提供依据。方法:采用随机数字表法,将70只SD大鼠分为7组,各组均单次尾静脉注射相应药物溶液,模型组、正常组给予等容量生理盐水,束水应激造成大鼠应激性胃溃疡,通过检测溃疡指数、溃疡抑制率、胃液pH值、H~+-K~+-ATP酶活性,评价左旋泮托拉唑钠的抗溃疡效果,并与右旋泮托拉唑钠和泮托拉唑钠进行比较。结果:左旋泮托拉唑钠中、高剂量组可以显著抑制束水应激性胃溃疡大鼠溃疡指数,升高胃液pH值,降低H~+-K~+-ATP酶活性(P <0. 05,P <0. 01);右旋泮托拉唑钠影响不显著,泮托拉唑钠与中剂量左旋泮托拉唑钠作用相当。结论:左旋泮托拉唑钠为泮托拉唑钠的主要活性成分。
Objective: To determine effect of pantolazole sodium on irritable stomach ulcer in rats,and evaluate its main active component,providing an experimental basis for the clinical development. Methods: A total of 70 SD rats were randomly divided into 7 groups. The corresponding drug solution was injected into each group from the tail vein,the model group and the normal group were given the same amount of normal saline. Irritable gastric ulcer was induced by water immersing. The ulcer index,ulcer inhibition rate,gastric juice PH value,and H+-K+-ATPase activity were detected. The effects of S(-)-pantoprazole sodium were compared with that of pantoprazole. Results: S(-)-pantoprazole sodium at 1. 8 and 3. 6 mg·kg-1 significantly inhibited the ulcer index,increased the p H value in gastric juice,and decreased the activity of H+-K+-ATPase activity( P < 0. 05,< 0. 01). The effects of S(-)-pantoprazole sodium were similar to that of pantoprazole. Conclusion: The main active component of pazoprazole sodium may be S(-)-pantoprazole.
Objective: To determine effect of pantolazole sodium on irritable stomach ulcer in rats,and evaluate its main active component,providing an experimental basis for the clinical development. Methods: A total of 70 SD rats were randomly divided into 7 groups. The corresponding drug solution was injected into each group from the tail vein,the model group and the normal group were given the same amount of normal saline. Irritable gastric ulcer was induced by water immersing. The ulcer index,ulcer inhibition rate,gastric juice PH value,and H+-K+-ATPase activity were detected. The effects of S(-)-pantoprazole sodium were compared with that of pantoprazole. Results: S(-)-pantoprazole sodium at 1. 8 and 3. 6 mg·kg-1 significantly inhibited the ulcer index,increased the p H value in gastric juice,and decreased the activity of H+-K+-ATPase activity( P < 0. 05,< 0. 01). The effects of S(-)-pantoprazole sodium were similar to that of pantoprazole. Conclusion: The main active component of pazoprazole sodium may be S(-)-pantoprazole.
引文
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[9]邱珲,杨庆云,童元峰,等.泮托拉唑钠单水合物和倍半水合物的晶型与稳定性差异研究[J].中国新药杂志,2015,24(8):869-875.
[2]陈坚.质子泵抑制剂的分类及药理学特性[J].上海医药,2013,34(21):3-7.
[3]曹春芽,肖聪颖,郑钦芳,等.紫苏对实验性胃溃疡的保护作用及机制研究[J].中药药理与临床,2016,32(4):56-61.
[4] JI HY,LEE HW,KIM HH,et al. Characterization of human liver cytochrome P450 enzymes involved in the metabolism of a new H+/K+-ATPase inhibitor KR-60436[J]. Toxicol Lett,2005,155(1):103-114.
[5] ZHANG W,ZHENG SB,ZHUANG Y,et al. H+/K+ATPase expression in human parietal cells and gastric acid secretion in elderly individuals[J]. J Dig Dis,2013,14(7):366-372.
[6]高小玲,靖慧军,郭文峰,等.奥美拉唑体内外给药对壁细胞H+-K+-ATP酶活的影响[J].世界中西医结合杂志,2014,9(4):365-368.
[7]郭锋,陆华龙,陈根,等.左旋泮托拉唑钠临床前毒理学研究[J].中南医学科学杂志,2012,40(1):51-54.
[8]叶玲梅,蔡咏梅.质子泵抑制剂的不良反应及防治对策[J].中国药房,2011,22(8):760-761.
[9]邱珲,杨庆云,童元峰,等.泮托拉唑钠单水合物和倍半水合物的晶型与稳定性差异研究[J].中国新药杂志,2015,24(8):869-875.