Evidence for the interaction between antacid and gastric mucosa using an "artificial stomach" model including gastric mucosa.
In light of evidence that certain aluminum-based antacids adhere to the gastric mucosa, we modified our previously described "artificial stomach" (AS) model by including a piece of hog stomach and compared the antacid activity of six aluminum-containing antacid products in the model with and without gastric mucosa. The activity of three of these, Maalox, Riopan and Supralox, was not significantly different in the two systems. In contrast, the activity of the other three, Aludrox, Phosphalugel and Simeco, was significantly greater with mucosa. Antacid activity of one product from each set (Supralox, Phosphalugel) was evaluated in two in vivo methods in human volunteers. For both antacids, results in vivo were similar to those obtained with the AS-containing mucosa. Without mucosa, in vivo and in vitro results were dissimilar for Phosphalugel, thus validating the modified AS. The difference between the two sets of antacids can be explained by 1) the fact that the Al:Mg ratio in the set affected by mucosa is greater than that of unaffected antacids, and 2) a weaker antacid load than in unaffected Supralox. We suggest that in an acid milieu, aluminum ions in antacids like Aludrox, Phosphalugel and Simeco are bound to sialic acid residues in mucus glycoproteins, thus retarding the transit of these antacids through both the AS and the real stomach and prolonging their activity in both situations. When the Al:Mg ratio is low or when the amount of antacid salts is large, aluminum ions tend to be buried in complexes, giving them less chance to interact with gastric mucus, so they transit the stomach more quickly.
Vatier
J L
JL
INSERM U 10 and Biochemistry B, CHU X. Bichat, Paris, France.
Gao
Z
Z
Fu-Cheng
X M
XM
Vitre
M T
MT
Levy
D A
DA
Cohen
G
G
Mignon
M
M
D000328:Adult; D000535:Aluminum / Q000494:pharmacology*; D000863:Antacids / Q000494:pharmacology*; D005744:Gastric Acid / Q000378:metabolism; D005745:Gastric Acidity Determination; D005746:Gastric Emptying; D005753:Gastric Mucosa / Q000187:drug effects* / Q000378:metabolism; D006801:Humans; D066298:In Vitro Techniques; D008274:Magnesium / Q000494:pharmacology; D008297:Male; D008954:Models, Biological
D000863:Antacids; D000535:Aluminum; D008274:Magnesium