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活性铝复合物的黏膜保护活性

Mucosal protective activity of activated aluminum complex.

作者信息

DiJoseph J F, Borella L E, Wells C L, Mir G N

机构信息

Division of Immunopharmacology, Wyeth-Ayerst Research, Princeton, N.J.

出版信息

Digestion. 1990;45(1):19-25. doi: 10.1159/000200220.

Abstract

The antacid ES Riopan was acidified ex vivo to pH 2.5 to completely eliminate its buffering capacity and was then tested as a mucosal protective agent. The pH 2.5 acidified antacid solution was named activated aluminum complex. Activated aluminum complex was 8.2 times more potent than its parent antacid in protecting against acidified aspirin-induced gastric lesions in the rat. Activated aluminum complex had a duration of action greater than 10 h in the ethanol-induced gastric lesion model, while ES Riopan was active for 6 h. Activated aluminum complex was able to inhibit both acid- and nonacid-mediated ulcers in the stomach and intestine. Its mucosal protective activity was not blocked by pretreatment with indomethacin. These results demonstrate that the nonbuffering antacid activated aluminum complex exerted a more potent and longer-lasting mucosal protective activity than its parent antacid. The activity was probably due to the presence of a hexaaquoaluminum cation and supports the argument that antacids possess mucosal protective effects independent of their acid-neutralizing capacity.

摘要

抗酸剂ES Riopan在体外被酸化至pH 2.5以完全消除其缓冲能力,然后作为黏膜保护剂进行测试。pH 2.5酸化的抗酸剂溶液被命名为活性铝络合物。在保护大鼠免受酸化阿司匹林诱导的胃损伤方面,活性铝络合物的效力是其母体抗酸剂的8.2倍。在乙醇诱导的胃损伤模型中,活性铝络合物的作用持续时间超过10小时,而ES Riopan的活性持续6小时。活性铝络合物能够抑制胃和肠道中酸介导和非酸介导的溃疡。吲哚美辛预处理不会阻断其黏膜保护活性。这些结果表明,非缓冲抗酸剂活性铝络合物比其母体抗酸剂具有更强、更持久的黏膜保护活性。这种活性可能归因于六水合铝阳离子的存在,并支持抗酸剂具有独立于其酸中和能力的黏膜保护作用这一观点。

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