Selective binding of sucralfate to ulcer lesion. II. Experiments in rats with gastric ulcer receiving 14C-sucralfate or potassium 14C-sucrose sulfate.
Selective binding of sucralfate to ulcer lesion. II. Experiments in rats with gastric ulcer receiving 14C-sucralfate or potassium 14C-sucrose sulfate.
复制标题
硫糖铝与溃疡病灶选择性结合。
DOI：
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发表时间：
1980
期刊：
影响因子：
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通讯作者：
H. Kamiyama
中科院分区：
文献类型：
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作者：
R. Nagashima;Y. Hinohara;T. Hirano;Y. Tohira;H. Kamiyama
用14C-蔗糖硫酸盐或14C-蔗糖硫酸钾的碱性铝盐14C-硫糖铝酸盐或14C-蔗糖硫酸钾对醋酸诱导的胃溃疡大鼠进行灌胃。在14C-硫糖铝给药后1、3、6和24小时，胃溃疡组织中代表蔗糖硫酸盐部分特异性结合的放射性活度显著升高，动物体内溃疡/非溃疡的平均比值分别达到6、7、12和2.5。显微放射自显影提供了直接的体内证据，证明14C-蔗糖硫酸盐部分与渗出的蛋白质结合，导致溃疡凹陷表面形成胃蛋白酶抗性屏障。在正常粘膜区域未见类似结果。与单纯服用可溶性钾盐相比，服用14C-硫糖铝对溃疡病变的结合作用更强、持续时间更长，并可在胃和十二指肠内滞留。这些发现不仅证明了碱性铝复合体在治疗上的显著作用，而且还证实了在粘附性的存在或不存在、局部屏障效应和作用持续时间方面与胃酶抑制剂(如硫酸支链淀粉)的可能差异。
14C-Sucralfate, a basic aluminum salt of 14C-sucrose sulfate, or potassium 14C-sucrose sulfate was administered orally to rats with acetic acid-induced gastric ulcer. The radioactivities representing specific binding of the sucrose sulfate moiety were found significantly higher in ulcer sections of the stomach, with the mean within-animal ulcer/non-ulcer ratio attaining 6, 7, 12 and 2.5, respectively, at 1, 3, 6 and 24 h after 14C-sucralfate administration. Microautoradiography provided direct in vivo evidence for binding of the 14C-sucrose sulfate moiety to exuded proteins resulting in effect in formation of a pepsin-resistant barrier over the surface of an ulcer crater. No comparable findings were obtained in the area of normal mucosa. The administration of 14C-sucralfate was associated with much greater and longer-sustained binding to the ulcer lesion and retention in the stomach and duodenum than simple administration of the soluble potassium salt. These findings not only demonstrate therapeutically significant effects of basic aluminum compoundation but also substantiate likely differences from pepsin inhibitors such as amylopectin sulfate in terms of presence or absence of adhesiveness, local barrier effects, and long duration of actions.