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 bismu th citrate (N-[3-(3-(l-piperidinylmethyl)phenoxy)propyl]-hydroxyacetamide-2 -hydroxypropane-1,2,3-tricarboxylate-bismuth(3+) complex), code name MXl, a gainst acetylsalicylic acid (ASA)- and indomethacin-induced gastric mucosal damage in rats. Effects of MXl (12.5, 50, 125, 184, 250 mg/kg) were compar ed to the effects of equimolar doses of roxatidine and bismuth subcitrate. Effect of MXl (10(-6) M) on mucin biosynthesis measured by [H-3] glucosamin e incorporation in rat gastric corpus has been determined. MXl-pretreatment dose-dependently decreased the mean ulcer number and length in all doses u sed in an extent similar to that of roxatidine and more pronounced in compa rison with bismuth subcitrate. The morphometrical results have been confirm ed histomorphologically. The biosynthesis of mucin was found to be signific antly enhanced after MXl addition. The results of the present study suggest that MXl has a gastroprotective effect against ASA- and indomethacin-induc ed ulcers which might be due both to its H-2-blocking and mucus-stimulating activity. (C) 1998 Prous Science. All rights reserved.