Wosilait W D, Nagy P
Res Commun Chem Pathol Pharmacol. 1976 May;14(1):75-81.
The distribution of Halofenate between the free and albumin bound forms was calculated by the use of two computer programs using both Scatchard association constants for a 3,3,7 model, and six stepwise equilbrium constants over a range of drug concentrations reported in man. The calculations, using either set of constants, showed that only 0.3 to 0.5% of the drug would be free. Using Scatchard association constants, it was estimated that 92 to 95% of the drug would be bound by the high affinity set of sites, and lesser amounts by sites of lesser affinity. A more complex pattern of distribution was obtained with the stepwise equilibrium constants. At low concentrations of Halofenate the complex with one mole of drug/mole of protein was most abundant and at the highest concentration studied the complex with two moles of drug/mole of protein was most abundant.
通过使用两个计算机程序来计算卤芬酯在游离形式和与白蛋白结合形式之间的分布，这两个程序分别使用了针对3,3,7模型的Scatchard结合常数，以及在人体报告的一系列药物浓度范围内的六个逐步平衡常数。使用任何一组常数进行的计算均表明，只有0.3%至0.5%的药物处于游离状态。使用Scatchard结合常数估计，92%至95%的药物将与高亲和力位点结合，较少的量与低亲和力位点结合。使用逐步平衡常数获得了更复杂的分布模式。在低浓度的卤芬酯下，一摩尔药物/摩尔蛋白质的复合物最为丰富，而在研究的最高浓度下，两摩尔药物/摩尔蛋白质的复合物最为丰富。
