Gastrointestinal transit of amoxicillin modified-release tablets and a placebo tablet including pharmacokinetic assessments of amoxicillin.
BACKGROUND
We have investigated the gastrointestinal transit time of, the influence of food intake on, the disintegration of, and the pharmacokinetics of amoxicillin in a modified-release form.


METHODS
Radiolabelled modified-release tablets of amoxicillin and placebo tablets were administered, in an open three-way, randomized, crossover design, as single doses during omeprazole treatment, to six male healthy subjects during fasting and non-fasting conditions. Radioscintigraphic images and plasma samples were obtained.


RESULTS
The estimated mean (and range) gastric emptying time of the modified-release tablet after drug administration was 0.3 h (0.1-1.0 h) during fasting conditions, 4.3 h (1.7-5.0 h) after a light breakfast, and 4.9 h (1.9-18.0 h) after a heavy breakfast. The small-intestinal transit time during fasting conditions was 4.7 h (2.9-6.9 h) and was not significantly changed after light or heavy breakfast intake. The relative bioavailability of the modified-release tablet was 55%, compared with a commercially available amoxicillin immediate-release tablet.


CONCLUSIONS
The modified-release tablet of amoxicillin administered postprandially apparently increases the amoxicillin release time in the stomach. The relevance of its use for anti-H. pylori treatment can be questioned.
Gottfries
J
J
Astra Hässle AB, Mölndal, Sweden.
Svenheden
A
A
Alpsten
M
M
Bake
B
B
Larsson
A
A
Idström
J P
JP
D000328:Adult; D000658:Amoxicillin / Q000493:pharmacokinetics* / Q000600:supply & distribution; D001682:Biological Availability; D018592:Cross-Over Studies; D003692:Delayed-Action Preparations; D016903:Drug Monitoring; D004435:Eating; D005215:Fasting; D005746:Gastric Emptying; D005772:Gastrointestinal Transit; D006801:Humans; D008297:Male; D010406:Penicillins / Q000493:pharmacokinetics* / Q000600:supply & distribution; D010919:Placebos
D003692:Delayed-Action Preparations; D010406:Penicillins; D010919:Placebos; D000658:Amoxicillin