Plasma protein binding—lipophilicity relationships: interspecies comparison of some organic acids
- 1 February 1987
- journal article
- research article
- Published by Oxford University Press (OUP) in Journal of Pharmacy and Pharmacology
- Vol. 39 (2) , 79-83
- https://doi.org/10.1111/j.2042-7158.1987.tb06949.x
Abstract
Relationships between plasma protein binding of 11 organic acids (benzoic and phenylacetic acid derivatives) and their lipophilicity were studied in man, rabbits, rats and mice. For description, the relationship fu = 1/(1 + aDb) was developed, where fu is the fraction of the unbound drug in plasma, D is the partition coefficient octanol/water and a and b are parameters. While the value of the parameter a is widely different in interspecies comparison, the value of the parameter b is very close in all species studied and is approximately equal to 1. The model used allows the simple calculation of the extent of plasma binding of structurally similar drugs from their lipophilicity, or conversion of the extent of plasma binding from one species to another.This publication has 15 references indexed in Scilit:
- o- and m-Iodohippurate binding to plasma proteins as a model drug transport mechanismJournal of Pharmacy and Pharmacology, 1984
- Quantitative structure-pharmacokinetic relationships and drug designPharmacology & Therapeutics, 1981
- Disease-induced Changes in the Plasma Binding of Basic DrugsClinical Pharmacokinetics, 1980
- Effect of plasma protein and tissue binding on the biologic half‐life of drugsClinical Pharmacology & Therapeutics, 1978
- Plasma and Tissue Protein Binding of Drugs in PharmacokineticsDrug Metabolism Reviews, 1976
- Linear Relationships between Plasma Binding and Lipophilicity of Disopyramide DerivativesJournal of Pharmaceutical Sciences, 1975
- Two techniques for evaluating small molecule-macromolecule binding in complex systemAnalytical Biochemistry, 1975
- Pentazocine binding to blood cells and plasma proteinsClinical Pharmacology & Therapeutics, 1974
- OVERVIEW OF DRUG‐PROTEIN BINDINGAnnals of the New York Academy of Sciences, 1973
- THE ATTRACTIONS OF PROTEINS FOR SMALL MOLECULES AND IONSAnnals of the New York Academy of Sciences, 1949