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Mucosal protective activity of activated aluminum complex
J F DiJoseph1, L E Borella, C L Wells
1Division of Immunopharmacology, Wyeth-Ayerst Research, Princeton, N.J.
Digestion
|January 1, 1990
Summary
A new activated aluminum complex, derived from the antacid ES Riopan, shows superior gastric protection. This non-buffering agent offers enhanced and prolonged mucosal defense against ulcers compared to the original antacid.
Area of Science:
- Gastroenterology
- Pharmacology
- Materials Science
Background:
- Antacids are commonly used to treat acid-related gastrointestinal disorders.
- The acid-neutralizing capacity of antacids is their primary mechanism of action.
- Emerging evidence suggests antacids may possess additional mucosal protective properties.
Purpose of the Study:
- To evaluate the mucosal protective potential of an acidified antacid preparation, termed activated aluminum complex.
- To compare the efficacy and duration of action of activated aluminum complex against its parent antacid, ES Riopan.
- To investigate the mechanism underlying the mucosal protective activity of activated aluminum complex.
Main Methods:
- ES Riopan antacid was acidified ex vivo to pH 2.5 to create activated aluminum complex, eliminating buffering capacity.
- Gastric lesions were induced in rats using acidified aspirin and ethanol.
- The protective effects and duration of action of activated aluminum complex and ES Riopan were assessed by lesion quantification.
Main Results:
- Activated aluminum complex demonstrated 8.2 times greater potency than ES Riopan in preventing acidified aspirin-induced gastric lesions.
- The duration of action for activated aluminum complex exceeded 10 hours, significantly longer than ES Riopan's 6-hour activity.
- Activated aluminum complex inhibited both acid- and non-acid-mediated ulcers and its activity was unaffected by indomethacin pretreatment.
Conclusions:
- The non-buffering activated aluminum complex exhibits significantly enhanced and prolonged mucosal protective activity compared to its parent antacid.
- The protective effect is likely attributed to the hexaaquoaluminum cation, suggesting a mechanism independent of acid neutralization.
- These findings support the hypothesis that antacids possess intrinsic mucosal protective effects beyond their acid-suppressing capabilities.