Effect of pKb on Lipophilic Binding of Disopyramide Derivatives to Human Plasma

• Published in: Journal of pharmaceutical sciences 1975-10, Vol.64 (10), p.1632-1635
• Main Authors: Chien, Yie W., Akers, Michael J., Yonan, Peter K.
• Format: Article
• Language: English
• Subjects: 13 disopyramide derivatives-determination; Blood Proteins - metabolism; Disopyramide - analogs & derivatives; Disopyramide - blood; Disopyramide derivatives-determination of plasma binding; Disopyramide derivatives—determination of plasma binding, partition coefficient and pKb, relationship between pKb and binding; Humans; Hydrogen-Ion Concentration; Kinetics; Lipophilic binding of 13 disopyramide derivatives to human plasma-relationship to pKb; partition coefficient and pKb; Partition coefficients; Partition coefficients, 13 disopyramide derivatives—determination; Plasma binding; Plasma binding, 13 disopyramide derivatives—determination, relationship to pKb; Protein Binding; Pyridines - analogs & derivatives; relationship between pKb and binding; relationship to pKb; Structure-Activity Relationship
• ISSN: 0022-3549; 1520-6017
• DOI: 10.1002/jps.2600641008

The extent of plasma binding, the partition coefficient, and the pKb of 13 disopyramide derivatives were determined. The structural variation on the diisopropylaminoethyl group of disopyramide molecules influenced these physical parameters to varying degrees. Results demonstrated that the extent of interaction between drugs and human plasma was a linear function of their lipophilicity and inversely proportional to the magnitude of the pKb value.