Effect of protein binding on penetration of beta-lactams into rabbit peripheral lymph

Author:

Woodnutt G1,Berry V1,Mizen L1

Affiliation:

1. SmithKline Beecham Pharmaceuticals, Betchworth, Surrey, England.

Abstract

The relevance of protein binding to penetration of beta-lactams into body fluids was investigated by examining the distribution of amoxicillin, ceftriaxone, clavulanic acid, temocillin, and ticarcillin into rabbit peripheral lymph after intravenous administration. The elimination half-lives in rabbit plasma varied between 0.34 h (temocillin) and 1.80 h (ceftriaxone), and the half-lives measured in lymph were similar to those in plasma (0.37 to 1.76 h). The percent penetration (area under the concentration-time curve in lymph/area under the concentration-time curve in plasma x 100) was high for amoxicillin (97.6%), temocillin (89.4%), and clavulanic acid (90.8%) but was lower for ticarcillin (76.0%) and for ceftriaxone (67.3%). There was a direct correlation between plasma protein binding and percent penetration. Correction for plasma and tissue binding increased the percent penetration for all compounds, and figures approached 100%. The results presented demonstrate the use of this model to examine the relationships between plasma pharmacokinetics, protein binding, and distribution of antibiotics.

Publisher

American Society for Microbiology

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology

Reference25 articles.

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4. Bergeron M. G. and L. Brousseau. 1986. Tissue fluid pharmacokinetic models in humans and animals p. 71-107. In O. Zak and M. Sande (ed.) Experimental models in antimicrobial chemotherapy vol. 1. Academic Press New York.

5. Pharmacokinetics of antibiotics in tissues and tissue fluids: a review;Cars O.;Scand. J. Infect. Dis. Suppl.,1991

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