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[硫糖铝:抗溃疡治疗新概念的发展。其药效学特性综述]

[Sucralfate: development of a new concept of anti-ulcer treatment. Review of its pharmacodynamic properties].

作者信息

Gorget C

出版信息

Rev Med Interne. 1985 Jun;6(3):313-9. doi: 10.1016/s0248-8663(85)80124-7.

Abstract

Sucralfate, a new drug for peptic ulcer disease, is a sulfated disaccharide, basic aluminium sucrose sulfate complex. Its development is the result of a lot studies on sulfated polysaccharides, well-known for their antipeptic activities and also, for their anticoagulant activities. Sucralfate is free from toxicity, including anticoagulant activity like all the disaccharides and is an antiulcer agent better than other drugs of its chemical family. Sucralfate is characterized by the following properties: When exposed to gastric acid, it turns into a viscous and adhesive substance which binds selectively and durably to the lesions of gastric and duodenal mucosa. The affinity of sucralfate for defective mucosa is explained by the formation of electrostatic bindings between the negatively charged sucralfate polyanions and the positively charged proteins exuding from lesions. Barrier effect to the penetration of acid, pepsin and bile salts. Interference with binding of the pepsin with the lesions. Adsorption of pepsin and bile salts. Protection of normal mucosa weakness of the reaction with acid. Possibility of stimulation of synthesis of local prostaglandins. Sucralfate is slightly absorbed by the digestive mucosa. That explains the absence of systemic effects and of toxicity. The pharmacodynamic effects corroborated by good therapeutical results make sucralfate an original antiulcer drug which leads a new way in the treatment of peptic disease.

摘要

硫糖铝是一种治疗消化性溃疡病的新药,它是一种硫酸化二糖,即碱性铝蔗糖硫酸盐复合物。它的研发是对硫酸化多糖进行大量研究的成果,硫酸化多糖以其抗溃疡活性以及抗凝活性而闻名。硫糖铝没有毒性,包括不像所有二糖那样具有抗凝活性,并且是一种比其化学家族中的其他药物更好的抗溃疡剂。硫糖铝具有以下特性:当暴露于胃酸时,它会变成一种粘性和粘附性物质,该物质会选择性且持久地与胃和十二指肠粘膜的损伤部位结合。硫糖铝对受损粘膜的亲和力可通过带负电荷的硫糖铝聚阴离子与从损伤部位渗出的带正电荷的蛋白质之间形成静电结合来解释。对酸、胃蛋白酶和胆盐渗透的屏障作用。干扰胃蛋白酶与损伤部位的结合。吸附胃蛋白酶和胆盐。保护正常粘膜对酸反应的减弱。刺激局部前列腺素合成的可能性。硫糖铝仅被消化粘膜少量吸收。这就解释了其不存在全身作用和毒性的原因。良好治疗效果所证实的药效学作用使硫糖铝成为一种原创性抗溃疡药物,为消化性疾病的治疗开辟了一条新途径。

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