Mucosal protective activity of activated aluminum complex.
The antacid ES Riopan was acidified ex vivo to pH 2.5 to completely eliminate its buffering capacity and was then tested as a mucosal protective agent. The pH 2.5 acidified antacid solution was named activated aluminum complex. Activated aluminum complex was 8.2 times more potent than its parent antacid in protecting against acidified aspirin-induced gastric lesions in the rat. Activated aluminum complex had a duration of action greater than 10 h in the ethanol-induced gastric lesion model, while ES Riopan was active for 6 h. Activated aluminum complex was able to inhibit both acid- and nonacid-mediated ulcers in the stomach and intestine. Its mucosal protective activity was not blocked by pretreatment with indomethacin. These results demonstrate that the nonbuffering antacid activated aluminum complex exerted a more potent and longer-lasting mucosal protective activity than its parent antacid. The activity was probably due to the presence of a hexaaquoaluminum cation and supports the argument that antacids possess mucosal protective effects independent of their acid-neutralizing capacity.
DiJoseph
J F
JF
Division of Immunopharmacology, Wyeth-Ayerst Research, Princeton, N.J.
Borella
L E
LE
Wells
C L
CL
Mir
G N
GN
D000536:Aluminum Hydroxide / Q000627:therapeutic use*; D000818:Animals; D000863:Antacids / Q000627:therapeutic use*; D001241:Aspirin; D003543:Cysteamine; D004381:Duodenal Ulcer / Q000139:chemically induced / Q000188:drug therapy / Q000473:pathology; D000431:Ethanol; D005753:Gastric Mucosa / Q000187:drug effects* / Q000473:pathology; D006863:Hydrogen-Ion Concentration; D007213:Indomethacin / Q000494:pharmacology; D007413:Intestinal Mucosa / Q000187:drug effects* / Q000473:pathology; D008026:Ligation; D008276:Magnesium Hydroxide / Q000627:therapeutic use; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D013276:Stomach Ulcer / Q000139:chemically induced / Q000188:drug therapy / Q000209:etiology / Q000473:pathology
D000863:Antacids; D000431:Ethanol; D000536:Aluminum Hydroxide; D003543:Cysteamine; C016545:magaldrate; D008276:Magnesium Hydroxide; D001241:Aspirin; D007213:Indomethacin