Niwa T, Tokuma Y, Noguchi H
Res Commun Chem Pathol Pharmacol. 1987 Jan;55(1):75-88.
The in vitro protein binding of nilvadipine, a new dihydropyridine calcium antagonist, was studied by equilibrium dialysis, ultracentrifugation, and equilibrium gel filtration. In the experiment with equilibrium dialysis, nilvadipine was highly bound to the plasma of man (97.5-98.7%) and dog (99.1-99.2%) with no plasma concentration dependency in a range of 10-100 ng/ml. Ultracentrifugation gave lower protein binding than that by equilibrium dialysis. From the experiments with equilibrium dialysis and equilibrium gel filtration, we found that lipoproteins and albumin are the main nilvadipine binding proteins in the plasma. The protein binding of nilvadipine in human plasma was unaffected or slightly decreased in the presence of therapeutic concentration of phenytoin, diazepam, salicylic acid, propranolol, quinidine and trichloromethiazide.
采用平衡透析法、超速离心法和平衡凝胶过滤法研究了新型二氢吡啶类钙拮抗剂尼伐地平的体外蛋白结合情况。在平衡透析实验中，尼伐地平与人血浆（97.5 - 98.7%）和犬血浆（99.1 - 99.2%）高度结合，在10 - 100 ng/ml范围内无血浆浓度依赖性。超速离心法测得的蛋白结合率低于平衡透析法。通过平衡透析和平衡凝胶过滤实验，我们发现脂蛋白和白蛋白是血浆中尼伐地平的主要结合蛋白。在苯妥英、地西泮、水杨酸、普萘洛尔、奎尼丁和三氯甲噻嗪治疗浓度存在的情况下，尼伐地平在人血浆中的蛋白结合不受影响或略有下降。
