Document Detail

Determination of protein binding by in vitro charcoal adsorption.
MedLine Citation:
PMID:  8576843     Owner:  NLM     Status:  MEDLINE    
Certain compounds such as SC-52151 have extensive nonspecific adsorption to the ultrafiltration devices or to dialysis membranes and therefore can not be measured by the conventional ultrafiltration or equilibrium dialysis methods. A new method based on charcoal adsorption was developed to overcome this difficulty. Unlike many conventional methods, which are based on the separation of free drug from bound drug under equilibrium conditions, the new method is operated under nonequilibrium conditions and involves measuring the time course of decline of the percentage of bound drug remaining in plasma while the free drug is being removed by charcoal adsorption. Theoretical aspects of the method and the data processing procedure are presented. SC-98A, a compound with minimal nonspecific adsorption to the ultrafiltration membrane, was used to demonstrate the applicability of this method against the ultrafiltration method. Using this method, the protein binding of SC-52151 in human plasma at 1.0 microgram/ml was determined to be in the range of 91.4-97.7% at room temperature.
J Yuan; D C Yang; J Birkmeier; J Stolzenbach
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Journal of pharmacokinetics and biopharmaceutics     Volume:  23     ISSN:  0090-466X     ISO Abbreviation:  J Pharmacokinet Biopharm     Publication Date:  1995 Feb 
Date Detail:
Created Date:  1996-03-11     Completed Date:  1996-03-11     Revised Date:  2004-11-17    
Medline Journal Info:
Nlm Unique ID:  0357115     Medline TA:  J Pharmacokinet Biopharm     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  41-55     Citation Subset:  IM    
Pharmacokinetics, Bioanalytical and Radiochemistry Function, G. D. Searle Research and Development, Skokie, Illinois 60077, USA.
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MeSH Terms
Blood Proteins / metabolism
Protein Binding*
Urea / analogs & derivatives,  metabolism
Reg. No./Substance:
0/Blood Proteins; 0/SC 52151; 16291-96-6/Charcoal; 57-13-6/Urea

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