Dosmalfate, a heptakis(hydrogensulfate) aluminium complex of diosmin, was launched
in Spain for the prevention and treatment of gastroduodenal lesions induced by NSAID
therapy. Dosmalfate can be prepared from diosmin by initial treatment with a pyridine
sulfur trioxide complex followed by sodium hydroxide and finally aluminium
hydroxychloride. In several pharmacological models of acute and chronic ulcers, this new
cytoprotective agent has demonstrated significant protection against damage to the gastric
mucosa or esophagus erosion, hemorrhage or perforation. Several mechanisms of action
could be involved, partly mediated by the endogenous prostaglandins. In several clinical
studies with patients receiving long-term NSAID therapy for chronic inflammatory disease,
the efficacy of dosmalfate in preventing gastric ulcer was high and comparable to that of
misoprostol, but with significantly less adverse events. In rats and humans, dosmalfate,
administered orally at very high doses, displayed a very poor absorption and consequently,
a very low incidence of side effects, particularly on CNS, cardiovascular or respiratory
systems.
