Gastroprotective effect of MX1 (a novel salt of the active metabolite of roxatidine with a complex of bismuth and citric acid) against stress ulcers in rats

J Pharm Pharmacol. 1997 Aug;49(8):791-5. doi: 10.1111/j.2042-7158.1997.tb06114.x.

Abstract

We have studied the effect of the newly synthesized agent MX1, a salt of the active metabolite of the H2-blocker roxatidine with a complex of bismuth and citric acid (N-[3-(3-(1-piperidinylmethyl)phenoxy)propyl]-hydroxyacetamide+ ++ -2-hydroxypropane-1,2,3-tricarboxilate-bismuth(3+) complex), against restraint stress ulcers in rats (24 h immobilization). The effects of MX1 (12.5, 50, 125, 184 and 250 mg kg-1) were compared with the effects of equimolar doses of roxatidine (6.5, 25, 70, 100 and 140 mg kg-1) and bismuth subcitrate (6.5, 25, 70, 100 and 140 mg kg-1). The results show that MX1-pre-treatment, at all the doses used, significantly reduces the mean number and size of ulcers. Even at the lowest dose the number of ulcers was reduced by 64.3% and the size of the ulcer by 55.9%. Roxatidine (25, 70, 100 and 140 mg kg-1) dose-dependently reduces ulcer size and number by 24.6, 55.6, 85.3 and 89.0% and by (+7.2), 14.3, 57.1 and 67.9%, respectively. Bismuth subcitrate significantly reduces ulcer size and number only at the highest dose employed (-28.5 and -44.8%, respectively). The morphometric results have been confirmed histomorphologically. The results suggest that MX1 has a gastroprotective effect against stress-induced ulcers which is similar to that of the parent compound and more pronounced than that of bismuth subcitrate.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antacids / therapeutic use*
  • Anti-Ulcer Agents / therapeutic use*
  • Drug Combinations
  • Gastric Mucosa / drug effects
  • Gastric Mucosa / metabolism
  • Histamine H2 Antagonists / therapeutic use*
  • Male
  • Organometallic Compounds / therapeutic use*
  • Peptic Ulcer / etiology
  • Peptic Ulcer / prevention & control*
  • Piperidines / therapeutic use*
  • Rats
  • Rats, Wistar
  • Restraint, Physical

Substances

  • Antacids
  • Anti-Ulcer Agents
  • Drug Combinations
  • Histamine H2 Antagonists
  • MX(1) complex
  • Organometallic Compounds
  • Piperidines
  • bismuth tripotassium dicitrate
  • roxatidine acetate