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Antimicrobial Agents and Chemotherapy, October 2004, p. 3850-3857, Vol. 48, No. 10
0066-4804/04/$08.00+0     DOI: 10.1128/AAC.48.10.3850-3857.2004
Copyright © 2004, American Society for Microbiology. All Rights Reserved.

[¹⁸F]Ciprofloxacin, a New Positron Emission Tomography Tracer for Noninvasive Assessment of the Tissue Distribution and Pharmacokinetics of Ciprofloxacin in Humans

Martin Brunner,^1* Oliver Langer,¹ Georg Dobrozemsky,^2,3 Ulrich Müller,¹ Markus Zeitlinger,¹ Markus Mitterhauser,^2,4 Wolfgang Wadsak,² Robert Dudczak,² Kurt Kletter,² and Markus Müller¹

Department of Clinical Pharmacology, Division of Clinical Pharmacokinetics,¹ Department of Nuclear Medicine,² Department of Biomedical Engineering and Physics, Medical University of Vienna,³ Institute of Pharmaceutical Technology and Biopharmaceutics, University of Vienna, Vienna, Austria⁴

Received 10 February 2004/ Returned for modification 10 May 2004/ Accepted 5 July 2004

The biodistribution and pharmacokinetics of the fluorine-18-labeled fluoroquinolone antibiotic [¹⁸F]ciprofloxacin in tissue were studied noninvasively in humans by means of positron emission tomography (PET). Special attention was paid to characterizing the distribution of [¹⁸F]ciprofloxacin to select target tissues. Healthy volunteers (n = 12) were orally pretreated for 5 days with therapeutic doses of unlabeled ciprofloxacin. On day 6, subjects received a tracer dose (mean injected amount, 700 ± 55 MBq, which contained about 0.6 mg of unlabeled ciprofloxacin) of [¹⁸F]ciprofloxacin as an intravenous bolus. Thereafter, PET imaging and venous blood sampling were initiated. Time-radioactivity curves were measured for liver, kidney, lung, heart, spleen, skeletal muscle, and brain tissues for up to 6 h after radiotracer administration. The first application of [¹⁸F]ciprofloxacin in humans has demonstrated the safety and utility of the newly developed radiotracer for pharmacokinetic PET imaging of the tissue ciprofloxacin distribution. Two different tissue compartments of radiotracer distribution could be identified. The first compartment including the kidney, heart, and spleen, from which the radiotracer was washed out relatively quickly (half-lives [t_1/2s], 68, 57, and 106 min, respectively). The second compartment comprised liver, muscle, and lung tissue, which displayed prolonged radiotracer retention (t_1/2, >130 min). The highest concentrations of radioactivity were measured in the liver and kidney, the main organs of excretion (standardized uptake values [SUVs], 4.9 ± 1.0 and 9.9 ± 4.4, respectively). The brain radioactivity concentrations were very low (<1 kBq · g^–1) and could therefore not be quantified. Transformation of SUVs into absolute concentrations (in micrograms per milliliter) allowed us to relate the concentrations at the target site to the susceptibilities of bacterial pathogens. In this way, the frequent use of ciprofloxacin for the treatment of a variety of infections could be corroborated.

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* Corresponding author. Mailing address: Department of Clinical Pharmacology, Division of Clinical Pharmacokinetics, Medical University of Vienna, Allgemeines Krankenhaus, Währinger Gürtel 18-20, A-1090 Vienna, Austria. Phone: 43-1-40400-2981. Fax: 43-1-40400-2998. E-mail: martin.brunner{at}meduniwien.ac.at.

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Antimicrobial Agents and Chemotherapy, October 2004, p. 3850-3857, Vol. 48, No. 10
0066-4804/04/$08.00+0     DOI: 10.1128/AAC.48.10.3850-3857.2004
Copyright © 2004, American Society for Microbiology. All Rights Reserved.

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