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Related Experiment Videos

Dose-dependent bioavailability of amoxycillin.

A Arancibia1, A Icarte, C González

  • 1Department of Pharmaceutical Sciences and Technology, University of Chile, Santiago.

International Journal of Clinical Pharmacology, Therapy, and Toxicology
|June 1, 1988
PubMed
Summary

This study investigated amoxycillin bioavailability in healthy adults across various doses. Higher amoxycillin doses showed a trend toward decreased bioavailability, with the 1g dose exhibiting the lowest recovery.

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Area of Science:

  • Pharmacokinetics and Drug Metabolism
  • Clinical Pharmacology

Background:

  • Amoxycillin is a widely used antibiotic.
  • Understanding amoxycillin bioavailability is crucial for optimizing therapeutic efficacy.
  • Dose-dependent pharmacokinetic profiles require thorough investigation.

Purpose of the Study:

  • To evaluate the bioavailability of amoxycillin at different single oral doses.
  • To determine the impact of dose escalation on amoxycillin's pharmacokinetic profile.
  • To assess amoxycillin's urinary recovery across a range of administered doses.

Main Methods:

  • Healthy volunteers received single oral doses of amoxycillin (250 mg, 500 mg, 750 mg, 1 g).
  • Urine samples were collected over 24 hours post-administration.
  • Amoxycillin concentrations in urine were quantified using a microbiological assay.

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  • Relative bioavailability was calculated by comparing 24-hour urinary recovery to a 250 mg reference dose.

    • Main Results:

    • Mean 24-hour urinary recovery of amoxycillin was 59.6% (250 mg), 55.9% (500 mg), 58.5% (750 mg), and 45.8% (1 g).
    • A notable decrease in mean urinary recovery was observed at the 1 g dose.
    • Relative bioavailability indicated a potential dose-dependent reduction in absorption or increase in non-urinary clearance at higher doses.

    Conclusions:

    • Amoxycillin bioavailability may be dose-dependent, with reduced recovery at higher doses.
    • The 1g dose of amoxycillin showed a diminished pharmacokinetic profile compared to lower doses.
    • Further research into the mechanisms underlying this dose-dependent effect is warranted.