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Related Experiment Videos

Interstitial tissue concentrations of cefpodoxime.

Ping Liu1, Markus Müller, Maria Grant

  • 1Department of Pharmaceutics, College of Pharmacy, University of Florida, Gainesville, FL 32610, USA.

The Journal of Antimicrobial Chemotherapy
|June 22, 2002
PubMed
Summary

Microdialysis measured free cefpodoxime tissue concentrations, revealing greater penetration than cefixime. This suggests cefpodoxime may offer superior efficacy due to enhanced tissue drug levels.

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Area of Science:

  • Pharmacology
  • Infectious Diseases
  • Clinical Pharmacy

Background:

  • Microdialysis enables measurement of free antibiotic concentrations at target sites, crucial for antibacterial effect.
  • Understanding tissue penetration of antibiotics is vital for optimizing antimicrobial therapy.
  • Cefpodoxime and cefixime are cephalosporin antibiotics used to treat various infections.

Purpose of the Study:

  • To investigate the tissue penetration of cefpodoxime using microdialysis in animal and human studies.
  • To compare the tissue penetration of cefpodoxime with cefixime in healthy volunteers.
  • To assess the pharmacokinetic/pharmacodynamic implications of differing tissue penetration.

Main Methods:

  • Microdialysis was employed in Wistar rats to measure plasma, muscle, and lung concentrations of cefpodoxime after intravenous administration.

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  • A randomized crossover study in healthy volunteers measured plasma and muscle concentrations of cefpodoxime and cefixime after oral dosing.
  • Free antibiotic concentrations in plasma and tissue were quantified to determine penetration and exposure.

    • Main Results:

    • In rats, free muscle and lung concentrations of cefpodoxime served as surrogate markers for pulmonary target site concentrations.
    • In humans, cefpodoxime demonstrated significantly greater tissue penetration than cefixime, with peak free muscle concentrations and AUC(t) more than double.
    • While total plasma concentrations were similar, free muscle concentrations highlighted superior cefpodoxime tissue exposure.

    Conclusions:

    • Cefpodoxime exhibits superior tissue penetration compared to cefixime in humans.
    • Enhanced tissue penetration of cefpodoxime suggests a potentially greater clinical efficacy.
    • Microdialysis is a valuable tool for evaluating antibiotic tissue distribution and informing therapeutic strategies.