Cheruvallath V K, Riley C M, Narayanan S R, Lindenbaum S, Perrin J H
Department of Pharmaceutical Chemistry, University of Kansas, Lawrence 66046, USA.
Pharm Res. 1996 Jan;13(1):173-8. doi: 10.1023/a:1016066325476.
The heats of reaction between the enantiomers and racemates of ibuprofen and naproxen and human serum albumin (HSA) are to be measured with and without the addition of octanoic acid. The effects of octanoic acid on the free energies of interaction between the drugs and HSA is to be determined and compared to that estimated from theoretical equations.
The heats of reaction have been measured directly by flow microcalorimetry.
The data showed that octanoic acid lowered the 1:1 binding constants for all the drug-HSA interactions investigated. The effect of octanoic acid was greater on the R than on the S forms of the drugs as shown by the differences in free energies of interaction in the presence and absence of octanoic acid.
The increased free energy differences for the binding of the enantiomers of both drugs to HSA in the presence of octanoic acid is closer to the value deemed to be necessary for the separation of enantiomers by Davenkov, and shows the importance of the addition of octanoic acid to the mobile phase in the separation of these enantiomers on immobilized albumin columns.
测量布洛芬和萘普生的对映体、外消旋体与人类血清白蛋白（HSA）之间在添加和不添加辛酸情况下的反应热。确定辛酸对药物与HSA之间相互作用自由能的影响，并与理论方程估算值进行比较。
通过流动微量热法直接测量反应热。
数据表明，辛酸降低了所有所研究药物与HSA相互作用的1:1结合常数。如存在和不存在辛酸时相互作用自由能的差异所示，辛酸对药物R型的影响大于S型。
在辛酸存在下，两种药物对映体与HSA结合的自由能差异增加，更接近达文科夫认为对映体分离所需的值，这表明在固定化白蛋白柱上分离这些对映体时，向流动相中添加辛酸的重要性。
