Species Differences in the Binding of Phenylbutazone to Plasma Albumin

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Abstract
The binding of phenylbutazone to plasma albumins from man, rat, rabbit and dog has been measured at 37°C by equilibrium dialysis. Species differences were found both in the number of phenylbutazone binding sites per albumin molecule and the affinity of such sites for the drug. Using the binding parameters from this study we have shown how it is possible to estimate the effect of plasma albumin binding on the distribution of a drug in the body. These calculations suggest that although phenylbutazone has a stronger affinity for human plasma albumin than for plasma albumins from the other 3 species it is unlikely that the longer biologic half life of the drug in man can be attributed solely to a difference in plasma binding. Using the binding parameters for human plasma albumin the effect of complete displacement of phenylbutazone from plasma and tissue binding sites on the concentration of free drug in plasma has also been estimated.

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