Abstract
Binding of drugs in plasma, tissues, microsomes, hepatocytes, and red blood cells (RBCs) are all of potential interest in drug discovery. Computational predictors for plasma protein binding (PPB) have been published. Several commercial in silico calculators of PPB are available. Drug binding is measured using in vitro assays, including equilibrium dialysis, ultrafiltration, ultracentrifugation, microdialysis, and plasmon resonance. Equilibrium dialysis is the most commonly used method for plasma, tissue, microsome, and hepatocyte binding. Fraction unbound can be measured with precision and accuracy to below 1% using equilibrium dialysis with longer incubation, plasma dilution, and presaturation techniques. RBC binding is significant for some compounds.
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