Fundam Clin Pharmacol. 1990;4:141s-150s. doi: 10.1111/j.1472-8206.1990.tb00072.x.

Measurement of free drug in phase I: is it useful?.

Fundamental & clinical pharmacology

J Barré, P Riant, J P Tillement

PMID: 2093625 DOI: 10.1111/j.1472-8206.1990.tb00072.x

Abstract

Early investigation of protein binding of a new drug is mandatory. The following questions have to be answered: is unbound fraction constant over tested concentrations? Which proteins are involved? What are the binding parameters? Can the drug compete with other therapeutic agents for the binding sites or in other words can drug displacements be predicted? What is the interindividual variability in protein binding? Is the binding stereoselective? All this information is necessary in predicting the pharmacokinetic behaviour of the drug and in assisting in the design of future pharmacokinetic protocols in phases II and III. The use of free drug concentration should also be considered when comparing the bioavailability of regular vs sustained release dosage forms of drugs exhibiting concentration-dependent binding and when studying concentration-effect relationships.

Substances

• Pharmaceutical Preparations

MeSH terms

• Drug Evaluation / methods
• Humans
• Pharmaceutical Preparations / metabolism
• Pharmacokinetics

Publication Types

• Journal Article
• Review

LinkOut - more resources

• Full Text Sources
  • Wiley
• Medical
  • MedlinePlus Health Information