Haughey D B, Lima J J
Eur J Clin Pharmacol. 1982;22(2):185-9. doi: 10.1007/BF00542466.
Serum and plasma disopyramide (D) protein binding was compared after blood was collected from four normal subjects in various Vacutainer tubes. The fraction of disopyramide bound to proteins in control serum and plasma was drug concentration dependent and correlated well with the capacity factor (N) associated with a high affinity protein binding site. D free fraction increased 60% at a postequilibrium concentration of 2 micrograms/ml in plasma following exposure of blood to green-top Vacutainer stoppers due to a 60% reduction in the affinity constant associated with the high affinity protein binding site. Heparin and EDTA had no effect on the plasma protein binding of D. These results suggest a competitive inhibition of disopyramide binding to alpha 1-acid-glycoprotein following contact of blood with rubber Vacutainer stoppers.
在使用不同的真空管从四名正常受试者采集血液后,比较了血清和血浆中丙吡胺(D)的蛋白结合情况。对照血清和血浆中与蛋白结合的丙吡胺比例取决于药物浓度,并且与高亲和力蛋白结合位点的容量因子(N)密切相关。在血液接触绿色顶盖真空管塞后,血浆中丙吡胺的游离分数在平衡后浓度为2微克/毫升时增加了60%,这是由于与高亲和力蛋白结合位点相关的亲和常数降低了60%。肝素和乙二胺四乙酸(EDTA)对丙吡胺的血浆蛋白结合没有影响。这些结果表明,血液与橡胶真空管塞接触后,丙吡胺与α1-酸性糖蛋白的结合受到竞争性抑制。