Comparison of plasma and free tissue levels of ceftriaxone in rats by microdialysis

Journal of Pharmaceutical Sciences
A KovarH Derendorf

Abstract

Ceftriaxone has a very high plasma protein binding (up to 98%) that is saturable and decreases with higher concentrations. This high protein binding results in high concentrations in plasma that are frequently related to the anti-infective activity. However, because only the free fraction of the drug is pharmacologically active and most of the infections are located in the tissues, it is more relevant to evaluate unbound concentrations in the interstitial space. Plasma and tissue pharmacokinetics of ceftriaxone in rats after single intravenous administration were investigated at two different concentrations (50 and 100 mg/kg). Both plasma and tissue samples were taken simultaneously from the same animal and analyzed by reversed-phase high-performance liquid chromatography. Free tissue levels in the thigh muscle were measured by microdialysis. The concentration in plasma is much higher than the free concentration in tissue. After determination of nonlinear protein binding by microdialysis and including these parameters in the pharmacokinetic model, it is possible to predict free concentrations in the interstitial space from plasma levels for any given dose.

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Citations

May 21, 2005·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Ping LiuHartmut Derendorf
Mar 3, 2004·Journal of Pharmacological and Toxicological Methods·Samia EzzineFrance Varin
Dec 8, 2000·Advanced Drug Delivery Reviews·A de la PeñaH Derendorf
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Apr 21, 2011·The Journal of Antibiotics·Bibiana Verlindo de AraujoTeresa Dalla Costa
Sep 10, 2008·Antimicrobial Agents and Chemotherapy·Stephan SchmidtHartmut Derendorf
Apr 24, 2004·Antimicrobial Agents and Chemotherapy·Markus MüllerHartmut Derendorf
Nov 24, 2005·Antimicrobial Agents and Chemotherapy·Sandrine MarchandWilliam Couet
May 27, 2005·Antimicrobial Agents and Chemotherapy·Sandrine MarchandWilliam Couet
Aug 30, 2005·Antimicrobial Agents and Chemotherapy·Sandrine MarchandWilliam Couet
Feb 24, 2001·Journal of Clinical Pharmacology·A KovarH Derendorf
Dec 18, 2001·Journal of Pharmaceutical Sciences·F X MathyR K Verbeeck
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Jan 15, 2022·Analytical and Bioanalytical Chemistry·Mark Thomas O'Connell, Jan Krejci

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