Equilibrium gel filtration to measure plasma protein binding of very highly bound drugs

Weiss, Markus
Gatlik, Ewa

Publication date

December 2013

Abstract

For very highly bound drugs (fu<2%) the determination of the unbound fraction in plasma (fu) and a reliable estimation of protein binding differences across species, populations, or concentrations is challenging. The difficulty is not mostly assay sensitivity but rather experimental bias. In equilibrium gel filtration (EGF) - opposite to the commonly used methods - the amount bound at a set free concentration is determined. Therefore, signals and differences are bigger for more highly protein bound drugs. We describe here a new experimental set-up developed to investigate binding in plasma and compare results with those obtained with standard methods for 9 Novartis compounds. The method was then applied for two drugs for which it was challe...

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Equilibrium gel filtration to measure plasma protein binding of very highly bound drugs

Abstract

Extracted data

Equilibrium gel filtration to measure plasma protein binding of very highly bound drugs

Abstract

Extracted data

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