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PHARMACOKINETICS

Effect of Simulated Microgravity on the Disposition and Tissue Penetration of Ciprofloxacin in Healthy Volunteers

Edgar L. Schuck, PhD, Maria Grant, MD and Hartmut Derendorf, PhD, FCP

From the Department of Pharmaceutics, College of Pharmacy, (Dr Schuck, Dr Derendorf), and the Department of Pharmacology and Therapeutics (Dr Grant), University of Florida, Gainesville.

This study evaluated the effects of simulated microgravity (sµG) on the pharmacokinetics of ciprofloxacin. Six healthy volunteers participated in a crossover study to compare the pharmacokinetics of ciprofloxacin after a single 250-mg oral dose in normal gravity (1G) and sµG. Plasma and urine samples were collected, and in vivo microdialysis was employed to obtain the free interstitial concentrations in the thigh muscle. Tissue penetration (f) was determined as the ratio of the free tissue area under the concentration versus time curve (AUCtiss,free)/AUCplasma,free. Plasma and free interstitial ciprofloxacin concentrations were simultaneously fit to a 1-compartment body model after correction for protein binding and tissue penetration. Total and free plasma concentrations were very similar in sµG and 1G. Tissue penetration in sµG (f =0.61 ± 0.36) was slightly lower than in 1G (f =0.92 ± 0.63); however, the difference was not significant. The authors conclude that the disposition of ciprofloxacin was not affected by simulated microgravity.

Key Words: Pharmacokinetics • microgravity • ciprofloxacin • tissue penetration • microdialysis

Address for reprints: Hartmut Derendorf, PhD, Department of Pharmaceutics, PO Box 100494, College of Pharmacy, University of Florida, Gainesville, FL 32610.


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