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新型低分子量肝素克利肝素在健康志愿者体内的药代动力学

Pharmacokinetics of Clivarin a new low molecular weight heparin in healthy volunteers.

作者信息

Andrassy K, Eschenfelder V, Koderisch J, Weber E

机构信息

Department of Medicine, University Hospital, Heidelberg, Germany.

出版信息

Thromb Res. 1994 Jan 15;73(2):95-108. doi: 10.1016/0049-3848(94)90084-1.

Abstract

The antithrombotic activity and pharmacokinetics of Clivarin, a low molecular weight heparin was randomly studied in 10 healthy male volunteers. Doses of 20, 40, 60 and 80 anti F Xa U/kg BW were injected intravenously and subcutaneously in crossover fashion. The heparin concentrations were measured by inhibition of clotting assays (anti IIa and anti Xa activities using amidolytic assays and [dilute] thrombin time). The pharmacokinetic profile of Clivarin is characterized by a linear relationship between dose and absorption, relatively low clearance and a long elimination half-life, and a high anti Xa/anti IIa ratio of 5.3.

摘要

对一种低分子量肝素——克利肝素的抗血栓活性和药代动力学进行了随机研究,研究对象为10名健康男性志愿者。以交叉方式静脉注射和皮下注射20、40、60和80抗FXa U/kg体重的剂量。通过抑制凝血试验(使用酰胺分解试验和[稀释]凝血酶时间测定抗IIa和抗Xa活性)来测量肝素浓度。克利肝素的药代动力学特征为剂量与吸收之间呈线性关系、清除率相对较低、消除半衰期较长,且抗Xa/抗IIa比率高达5.3。

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