COMPARISON OF GRAPHICAL AND COMPUTERIZED METHODS FOR CALCULATING BINDING PARAMETERS FOR 2 STRONGLY BOUND DRUGS TO HUMAN-SERUM ALBUMIN

被引:32
作者
VALLNER, JJ
PERRIN, JH
WOLD, S
机构
[1] UNIV WISCONSIN, SCH PHARM, MADISON, WI 53706 USA
[2] UNIV WISCONSIN, DEPT STATISTICS, MADISON, WI 53706 USA
关键词
D O I
10.1002/jps.2600650813
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The determination of drug-protein binding parameters (n''s and K''s) can lead to important information on the required therapeutic dosage regimen and possible clinical complications associated with competitive displacement of one drug by a concurrently administered agent. Graphical and computer estimates of the data are often incorrectly formulated, and seldom are adequate data obtained at low binding ratios. Commonly used graphical procedures, inadequately formulated computer methods, and a statistically correct computer method were used to compare results obtained from a circular dichroic examination of dicumarol-human serum albumin and fenoprofen-human serum albumin interactions. Literature binding constants for dicumarol-albumin range from 1 .times. 105 to 30 times that figure, and a wide range in parameter estimates may be obtained depending on the method of data analysis. The parameter estimates in the case of fenoprofen-albumin are even more variable.
引用
收藏
页码:1182 / 1187
页数:6
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