Development and characteristics of sucralfate.
Development and characteristics of sucralfate.
复制标题
硫糖铝的发展及特点。
DOI：
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发表时间：
1981
影响因子：
2.9
通讯作者：
R. Nagashima
中科院分区：
文献类型：
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作者：
R. Nagashima
硫糖铝是蔗糖辛硫酸盐的一种碱性铝盐，用于中和酸和胃蛋白酶的活性。它在化学上不同于其他硫酸盐化的胃酶阴离子抑制剂，因为它是纯二糖蔗糖的碱基和衍生物。硫糖铝的开发是由于观察到硫酸双糖不具有硫酸盐多糖的抗凝血活性，并且抑制胃蛋白酶活性和防止实验性溃疡只依赖于硫酸盐化的程度。硫糖铝被发现比蔗糖八硫酸盐和氢氧化铝的混合物更有效地保护幽门结扎的动物免受消化性溃疡的侵袭。硫糖铝有几种不同寻常的性质。一遇到胃酸，它就变成一种高度浓缩、粘稠的物质，具有缓冲胃酸的能力。这些特性被保留在十二指肠中。硫糖铝与蛋白质形成稳定的络合物，并通过阻止胃酶与底物的相互作用来抑制蛋白质的水解。硫糖铝还通过直接吸附胃蛋白酶来抑制胃蛋白酶的活性。此外，硫糖铝还能吸附胆汁盐。这些性质的总和意味着硫糖铝提供了对已确定的侵略性因素、酸、胃酶和胆盐的全面防御。
Sucralfate, a basic aluminum salt of sucrose octasulfate, was developed to counteract the activities of both acid and pepsin. It differs chemically from other sulfated anionic inhibitors of pepsin in being a base and a derivative of pure disaccharide sucrose. The development of sucralfate was guided by the observations that sulfated disaccharides do not exhibit the anticoagulant activity of sulfated polysaccharides, and that the inhibition of peptic activity and the protection against experimental ulceration depend only on the degree of sulfation. Sucralfate has been found to protect pylorusligated animals from peptic ulceration more effectively than a mixture of sucrose octasulfate and aluminum hydroxide. Sucralfate has several unusual properties. On encountering gastric acid, it becomes a highly condensed, viscous substance with the capacity to buffer acid. These properties are retained in the duodenum. Sucralfate forms stable complexes with proteins and inhibits their hydrolysis by preventing pepsin-substrate interaction. Sucralfate also inhibits peptic activities by direct adsorption of pepsin. In addition, sucralfate adsorbs bile salts. The sum of these properties implies that sucralfate provides a comprehensive defense against identified aggressive factors, acid, pepsin, and bile salts.