Cardot J M, Lefèvre G Y, Godbillon J A
Centre de Recherche Biopharmaceutique, Laboratories Ciba-Geigy, Rueil-Malmaison, France.
J Pharmacokinet Biopharm. 1994 Apr;22(2):147-56. doi: 10.1007/BF02353540.
The pharmacokinetics of recombinant hirudin (rec-hirudin, Ciba-Geigy, CGP 39,393) in healthy volunteers after iv administration was investigated on the basis of the data from five different studies. A total of 77 plasma profiles following a single iv bolus dose of either 0.1, 0.3, 0.5, or 1 mg/kg of rec-hirudin was used for the evaluation. Plasma concentrations and especially AUC were proportional to the dose. Kinetics of rec-hirudin after a bolus iv injection were best described by a three-compartment open model. Mean apparent terminal half-life was 2.8 hr and the total clearance 0.138 L/hr per kg.
基于五项不同研究的数据，对健康志愿者静脉注射重组水蛭素（rec-水蛭素，汽巴-嘉基公司，CGP 39393）后的药代动力学进行了研究。单次静脉推注剂量为0.1、0.3、0.5或1mg/kg重组水蛭素后，共77份血浆浓度曲线用于评估。血浆浓度尤其是药时曲线下面积（AUC）与剂量成正比。静脉推注后重组水蛭素的动力学最好用三室开放模型来描述。平均表观终末半衰期为2.8小时，总清除率为每千克0.138升/小时。
