Borella L E, Seethaler K, Lippmann W
Arzneimittelforschung. 1979;29(5):793-8.
The antiulcerogenic and antipeptic activities of sucralfate (Ulcerlmin), a basic aluminum sucrose sulfate complex, were investigated. In rats, sucralfate inhibited the formation of ulcers induced by pyloric ligation, indometacin and cysteamine. In doses antagonizing forestomach ulcer formation, sucralfate increased the pH of the gastric juice in a dose-related manner. In vitro, at pH 1.9, sucralfate inhibited rat, dog and hog pepsin in a concentration-related manner and also the peptic activity in human gastric juice. Sucralfate may act as an inhibitor of pepsin by precipitating the enzyme or by binding with it reversibly. The antipeptic activity appears to be directly related to the amount of sucralfate in suspension rather than that in solution. In the gastrointestinal tract, the basic nature of sucralfate may enhance the antipeptic activity of the sucralfate molecule. In rats, sucralfate decreases the rate of gastric emptying.
对一种碱性硫酸铝蔗糖复合物——硫糖铝(胃溃宁)的抗溃疡和抗胃蛋白酶活性进行了研究。在大鼠中,硫糖铝可抑制幽门结扎、吲哚美辛和半胱胺诱导的溃疡形成。在拮抗前胃溃疡形成的剂量下,硫糖铝可使胃液pH值呈剂量相关升高。在体外,pH值为1.9时,硫糖铝可呈浓度相关地抑制大鼠、犬和猪的胃蛋白酶以及人胃液中的胃蛋白酶活性。硫糖铝可能通过使胃蛋白酶沉淀或与其可逆性结合而起到胃蛋白酶抑制剂的作用。抗胃蛋白酶活性似乎与悬浮液中硫糖铝的量直接相关,而非与溶液中的量相关。在胃肠道中,硫糖铝的碱性性质可能会增强硫糖铝分子的抗胃蛋白酶活性。在大鼠中,硫糖铝可降低胃排空速率。