Development and characteristics of sucralfate.

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.