title: Gastrointestinal transit of amoxicillin modified-release tablets and a placebo tablet including pharmacokinetic assessments of amoxicillin.
abstract: 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.
authors.affiliation: Astra Hässle AB, Mölndal, Sweden.
authors.forename: J
authors.initials: J
authors.lastname: Gottfries
authors.forename: A
authors.initials: A
authors.lastname: Svenheden
authors.forename: M
authors.initials: M
authors.lastname: Alpsten
authors.forename: B
authors.initials: B
authors.lastname: Bake
authors.forename: A
authors.initials: A
authors.lastname: Larsson
authors.forename: J P
authors.initials: JP
authors.lastname: Idström
mesh_terms: 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
chemical_list: D003692:Delayed-Action Preparations; D010406:Penicillins; D010919:Placebos; D000658:Amoxicillin