Effect of roxatidine bismuth citrate (MX1) against acetylsalicylic acid- and indomethacin-induced gastric mucosal damage in rats.

We have studied the effect of the newly synthesized agent, roxatidine bismuth citrate (N-[3-(3-(1-piperidinyl-methyl)phenoxy)propyl]-hydroxyacetamide-2-hydroxypropane-1,2,3-tricarboxylate-bismuth(3+) complex), code name MX 1 , against acetylsalicylic acid (ASA)- and indomethacin-induced gastric mucosal damage in rats. Effects of MX (12.5, 50, 125, 184, 250 mg/kg) were compared to the effects of equimolar doses of roxatidine and bismuth subcitrate. Effect of MX 1 (10 -6 M) on mucin biosynthesis measured by [ 3 H] glucosamine incorporation in rat gastri corpus has been determined. MX 1 -pretreatment dose-dependently decreased the mean ulcer number and length in all doses used in an extent similar to that of roxatidine and more pronounced in comparison with bismuth subcitrate. The morphometrical results have been confirmed histomorphologically The biosynthesis of mucin was found to be significantly enhanced after MX 1 addition. The results of the present study suggest that MX has a gastroprotective effect against ASA- and indomethacin-induced ulcers which might be due both to its H 2 -blocking and mucus-stimulating activity.