RELATIONSHIP BETWEEN GASTROPROTECTIVE EFFECT OF LOCALLY ACTING ANTIULCER AGENT ECABET SODIUM AND ITS BINDING TO GASTRIC-MUCOSA IN RATS - COMPARISON WITH SUCRALFATE

The present study was designed to examine the relationship between the gastroprotective efficacy of the locally acting antiulcer drug ecabet sodium (ecabet) against ethanol-induced gastric lesions and the amoun t of the drug bound to the mucosa in comparison with sucralfate in rat s. Oral administration of ecabet (25-100 mg/kg) and sucralfate (25-400 mg/kg) dose dependently prevented the formation of ethanol-induced ga stric lesions, and dose dependently increased the amount of each drug bound to the gastric mucosa. Pretreatment with the antisecretory agent cimetidine (200 mg/kg, per os) significantly reduced the gastroprotec tive effect of sucralfate in proportion to a decrease in its binding t o the mucosa. The same pretreatment tended to reduce both gastroprotec tion by ecabet and its binding to the mucosa. In an in vitro study usi ng an everted Stomach sac, the binding of sucralfate to the mucosa was more markedly decreased than that of ecabet on increasing the pH. The se findings indicate that ecabet and sucralfate protect the gastric mu cosa against ethanol in proportion to the amount of each drug bound to the gastric mucosa and that the binding of these drugs to the mucosa is under the influence of intraluminal pH. However, the gastroprotecti ve effect of ecabet seems to be less dependent on intraluminal acidity than that of sucralfate.