Department of Materia Medica, University of Glasgow, Stobhill General Hospital, Glasgow.
Br J Clin Pharmacol. 1974 Aug;1(4):325-8. doi: 10.1111/j.1365-2125.1974.tb00261.x.
1 The binding of [(3)H]-digoxin to human plasma proteins was studied using both ultrafiltration and frontal analysis, to establish a suitable method for the measurement of digoxin-protein interaction, and to assess the effect of variations in digoxin protein binding on its distribution. 2 Using ultrafiltration, [(3)H]-digoxin was found to bind to plasma proteins to the extent of 30-40% over a concentration range of 0.001-1 ng/ml. Frontal analysis was unsuccessful in the measurement of digoxin protein binding. 3 Dilution experiments using plasma and human serum albumin suggested that variations in digoxin protein binding would be unlikely to cause significant alterations in the levels of free drug in the body. 4 The possible clinical implications of these results are discussed.
本研究采用超滤法和前沿分析法研究了[(3)H]地高辛与人血浆蛋白的结合情况,旨在建立一种合适的方法来测量地高辛与蛋白的相互作用,并评估地高辛蛋白结合的变化对其分布的影响。
超滤法结果显示,[(3)H]地高辛在 0.001-1ng/ml 的浓度范围内与血浆蛋白的结合率为 30-40%。但前沿分析法未能成功测量地高辛的蛋白结合。
使用血浆和人血清白蛋白进行的稀释实验表明,地高辛蛋白结合的变化不太可能导致体内游离药物水平发生显著变化。
讨论了这些结果的可能临床意义。