| Autor: |
Mais, R.F., Keresztes-Nagy, S., Zaroslinski, J.F., Oester, Y.T. |
| Zdroj: |
Journal of Pharmaceutical Sciences; September 1974, Vol. 63 Issue: 9 p1423-1427, 5p |
| Abstrakt: |
Three mathematical procedures were devised which allowed for the interconversion and interpretation of protein—drug binding data in the literature. A minicomputer program enabled the calculation of the fraction of drug bound for a specified total drug and protein concentration, given the protein binding constants and the number of sites. The corollary problem of finding the total drug concentration for a particular fraction drug bound was included. In addition, the concept of partial fraction bound for binding systems with multiple classes of sites was introduced and a formula was derived which made possible the calculation of this value from the usual binding constants. Finally, an equation was derived which allowed the total drug concentration and the fraction bound to be obtained from the binding information for selected rvalues. These were obtained from the Scatchard plot and the associated binding constants. Examples of the utility of these procedures are supplied based on data for human serum albumin binding of four drugs of clinical interest. Evidence is given to show the prominence of the contribution by the secondary sites to the total binding at therapeutic levels of the drugs. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
|
Plný text