Briggs C J, Hubbard J W, Savage C, Smith D
J Pharm Sci. 1983 Aug;72(8):918-21. doi: 10.1002/jps.2600720819.
The binding of drugs to plasma proteins has been studied extensively using a variety of methods, including equilibrium dialysis. Published information on controls used in these studies is frequently inadequate; in other cases, there are deficiencies in the experimental design for the controls. A method is described that eliminates many of the problems associated with artifactual errors in dialysis studies. Multiple replicated controls are performed at the same time as the test, under identical conditions. The controls are used to correct for concentration-dependent binding of drug to the membrane or other equipment. The method was used to determine the binding of sulfadimethoxine to CF-IV-1 alpha-globulin at therapeutic concentrations. The level of binding was low (9-13%), but the stringent control technique permitted statistical analysis which showed each mean test value to be significantly different from its corresponding control. Furthermore, there was a linear relationship between the control-corrected percentage binding values and total drug concentration, whereas there was no correlation between total drug concentration and the uncorrected percentage binding values.
使用包括平衡透析在内的多种方法，对药物与血浆蛋白的结合进行了广泛研究。关于这些研究中所用对照的已发表信息常常不充分；在其他情况下，对照的实验设计存在缺陷。本文描述了一种方法，该方法消除了透析研究中与人为误差相关的许多问题。在与测试相同的条件下，同时进行多个重复对照。这些对照用于校正药物与膜或其他设备的浓度依赖性结合。该方法用于测定治疗浓度下磺胺二甲氧嘧啶与CF-IV-1α球蛋白的结合。结合水平较低（9-13%），但严格的对照技术允许进行统计分析，结果表明每个测试平均值与其相应对照有显著差异。此外，对照校正后的结合百分比值与总药物浓度之间存在线性关系，而总药物浓度与未校正的结合百分比值之间没有相关性。
