Mombelli G, Schaedelin J, Beck E A
Schweiz Med Wochenschr. 1977 Jun 11;107(23):810-5.
In 2 groups of 4 probands the pharmacokinetics of heparin were investigated by a physiologic method (factor Xa inhibition) and an isotope method (35S-heparin) following a single intravenous injection of 5000 IU heparin and a single subcutaneous injection of 10000 IU heparin respectively. Following intravenous administration the anticoagulant effect and radioactivity fall exponentially. The half-life is about 50 min and the distribution volume 3000 ml (factor Xa inhibition) and 3800 ml (radioactivity). With subcutaneous injection peak concentrations above 0.2 IR heparin/ml were measured by both methods 2-4 h after administration; 9 h after administration, no further factor Xa inhibition was detectable in 2 probands. In the light of these and previously published results, some practical aspects of the conduct of therapy and prophylaxis of thromboembolism with heparin are discussed.
在两组各4名先证者中，分别单次静脉注射5000 IU肝素和单次皮下注射10000 IU肝素后，采用生理学方法（因子Xa抑制）和同位素方法（35S-肝素）研究了肝素的药代动力学。静脉给药后，抗凝作用和放射性呈指数下降。半衰期约为50分钟，分布容积为3000 ml（因子Xa抑制法）和3800 ml（放射性法）。皮下注射后，两种方法均在给药后2 - 4小时测得峰值浓度高于0.2 IR肝素/ml；给药后9小时，2名先证者中未检测到进一步的因子Xa抑制作用。根据这些结果以及先前发表的结果，讨论了肝素在血栓栓塞治疗和预防中的一些实际应用方面。
