Dawes J, Prowse C V, Pepper D S
Thromb Haemost. 1985 Oct 30;54(3):630-4.
The competitive binding assay described will specifically and accurately measure concentrations of administered heparin in biological fluids with a sensitivity of 60 ng ml-1. Neither endogenous glycosaminoglycans, nor plasma proteins such as ATIII and PF4 interfere in the assay. Semi-synthetic highly sulphated heparinoids and LMW heparin can also be measured. Using this assay heparin clearance followed simple first-order kinetics over the dose range 100-5,000 units, but the half-life was strongly dose-dependent. There was good correlation with heparin activity measurements by APTT and anti-Xa clotting assays. Plasma concentrations were measurable for at least 5 h following subcutaneous injection of 10,000 units of heparin. Excretion in the urine could be followed after all but the lowest intravenous dose. This assay, used in conjunction with measurements of heparin anticoagulant activity, will be valuable in the elucidation of mechanisms of action of heparin and the heparinoids, and in the assessment and management of problems related to heparin therapy.
所述竞争性结合测定法可特异性且准确地测量生物体液中所给予肝素的浓度,灵敏度为60 ng/ml。内源性糖胺聚糖以及诸如抗凝血酶III(ATIII)和血小板第4因子(PF4)等血浆蛋白均不干扰该测定。半合成的高硫酸化类肝素和低分子量肝素也可进行测量。使用该测定法,在100 - 5000单位的剂量范围内,肝素清除遵循简单的一级动力学,但半衰期强烈依赖于剂量。与通过活化部分凝血活酶时间(APTT)和抗Xa凝血测定法进行的肝素活性测量具有良好的相关性。皮下注射10000单位肝素后,血浆浓度至少可测量5小时。除最低静脉注射剂量外,其他剂量下均可追踪尿液中的排泄情况。该测定法与肝素抗凝活性测量相结合,对于阐明肝素和类肝素的作用机制以及评估和处理与肝素治疗相关的问题将具有重要价值。