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Relationship between plasma or serum drug concentration and amount of drug in the body at steady state upon multiple dosing

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Abstract

The average amount of drug in the body at steady state (\(\bar X\))upon repetitive dosing in a two-compartment open system is related to the average steady-state plasma level (\(\bar C\))by the apparent volume of distribution at steady state Vssrather than by Vβ,the apparent volume of distribution at pseudodistribution equilibrium, despite the fact that\(\bar C\)is directly proportional to 1/Vβ.Multiplication of\(\bar C\) by \(\ddot V_\beta \)results in an overestimate of\(\bar X\)the magnitude of which depends on the distribution and elimination parameters of the drug. The significance and utility of the volume parameters, Vβand Vss,employed in multicompartment systems are considered.

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Perrier, D., Gibaldi, M. Relationship between plasma or serum drug concentration and amount of drug in the body at steady state upon multiple dosing. Journal of Pharmacokinetics and Biopharmaceutics 1, 17–22 (1973). https://doi.org/10.1007/BF01060025

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  • DOI: https://doi.org/10.1007/BF01060025

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