Colas Linhart N, Laforest M D, Guiraud-Vitaux F, Gardin I, Petiet A, Berthelot J L, Bok B
Laboratoire de Biophysique, Faculté Xavier Bichat, Paris, France.
Biomed Pharmacother. 1990;44(6):317-23. doi: 10.1016/0753-3322(90)90135-v.
A low molecular weight heparin, enoxaparin, was labelled with 99mTc and the characteristics of the labelled compound determined. In vitro the stability, and labelling efficiency (98%) of the labelled drug were excellent. Rats were injected with 99mTc-enoxaparin to study pharmacokinetics and distribution. The results were used to calculate dosimetric estimates which are a prerequisite for pharmacokinetic studies on labelled LMWH (low molecular weight heparin) in human subjects. Biodistribution studies showed preferential liver and spleen accumulation. But the doses absorbed by these target organs remained below the upper limits of the dose received by a patient undergoing hepatic scintigraphy.
一种低分子量肝素——依诺肝素,用99mTc进行标记,并对标记化合物的特性进行了测定。在体外,标记药物的稳定性和标记效率(98%)极佳。给大鼠注射99mTc-依诺肝素以研究其药代动力学和分布情况。这些结果被用于计算剂量测定估计值,这是对人类受试者进行标记低分子量肝素药代动力学研究的一个前提条件。生物分布研究显示,药物在肝脏和脾脏有优先蓄积。但这些靶器官摄取的剂量仍低于接受肝脏闪烁扫描检查的患者所接受剂量的上限。