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.