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British Journal of Anaesthesia, Vol 81, Issue 3 422-424, Copyright © 1998 by The Board of Management and Trustees of the British Journal of Anaesthesia

LABORATORY INVESTIGATIONS

Steady-state propofol brain:plasma and brain:blood partition coefficients and the effect-site equilibration paradox

S. Dutta, Y. Matsumoto, A. Muramatsu, M. Matsumoto, M. Fukuoka and W. F. Ebling
Department of Pharmaceutics, State University of New York at Buffalo, Amherst, NY 14260, USA; Department of Pharmaceutics and Department of Clinical Pharmacology and Toxicology, Showa College of Pharmaceutical Sciences, Machida, Tokyo, 194 Japan; Department of Pharmaceutics, Showa College of Pharmaceutical Sciences, Machida, Tokyo, 194 Japan; Department of Clinical Pharmacology and Toxicology, Showa College of Pharmaceutical Sciences, Machida, Tokyo, 194 Japan

Based on volume-flow relationships, CNS agents that are highly lipid soluble (log octanol-water partition coefficient > 2) are expected to have equilibration half-times (T1/2 kE0) that are proportional to brain solubility. Propofol, the most lipophilic anaesthetic in clinical use, has T1/2 kE0 values of 1.7 and 2.9 min in rats and humans, respectively, compared with an expected value of at least 8 min. As a first step in exploring this discrepancy between observed and predicted values, we determined the steady state brain:plasma and brain:blood partition coefficients in rats after a 4-h infusion of propofol. Brain:plasma and brain:blood partition coefficients were 8.2 (SD 1.6) and 3.0 (0.5), respectively. T1/2 kE0 predictions based on brain: blood partitioning in rats are more in agreement with the observed equilibration half-time, suggesting that drug bound to the formed elements of blood participates in the uptake and transfer of propofol to its effect site.
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