G. Cardaci et al., REDUCED AMOXICILLIN UPTAKE INTO HUMAN GASTRIC-MUCOSA WHEN GASTRIC-JUICE PH IS HIGH, Antimicrobial agents and chemotherapy, 39(9), 1995, pp. 2084-2087
Amoxicillin when administered with gastric acid suppressors has been s
hown to be effective in eradication of Helicobacter pylori in 50 to 80
% of subjects, The aim of this investigator-blind crossover study was
to determine if gastric mucosal amoxicillin uptake was affected by inc
reasing gastric juice pH, Fifteen male subjects (7 H. pylori positive
and 8 H. pylori negative) were randomized to receive 150 mg of ranitid
ine twice a day, 300 mg of ranitidine twice a day, or no drug for 2 da
ys prior to upper endoscopy, The last dose of ranitidine was given 60
min prior to upper endoscopy, and amoxicillin (500 mg) was given 30 mi
n prior to upper endoscopy. The amoxicillin concentrations in mucosal
biopsy samples, gastric juice, and serum were determined by a standard
microbiological bioassay technique. Mean amoxicillin levels were grea
ter in samples of antrum, fundus, and duodenum for volunteers who rece
ived no ranitidine than in those receiving 300 mg of ranitidine (P < 0
.05) and those receiving 150 mg of ranitidine (P < 0.05 except for fun
dus), Amoxicillin levels in the antrum, fundus, and duodenum were nega
tively correlated with gastric juice pH (P < 0.005 for antrum; P < 0.0
01 for fundus and duodenum), There was no correlation between gastric
juice pH and amoxicillin levels in either gastric juice or serum, The
amoxicillin concentration in gastric juice was significantly higher wi
th 300 mg of ranitidine than with no ranitidine (P < 0.05), Thus, lowe
r gastric juice pH is associated with a higher rate of mucosal uptake
of amoxicillin.