~(125)I-神经生长因子的制备及其药代动力学研究

    PREPARATION OF ~(125)I LABELLED NERVE GROWTH FACTOR AND STUDY OF ITS PHARMACOKINETICS

    • 摘要: 用氯胺T法制备了12 5I 神经生长因子 (12 5I NGF) ,放化纯度大于 95 %。经静注和肌注两种途径并采用十二烷基磺酸钠 聚丙烯酰胺凝胶 (SDS PAGE)电泳法测定了小鼠血浆中NGF的浓度。研究结果表明 ,静注12 5I NGF后的小鼠体内代谢符合二房室分布模型 ;肌注12 5I NGF后的小鼠体内代谢符合一房室分布模型。按剂量2 5 μg/kg静注12 5I NGF后 ,测得消除相半衰期 (t1/ 2 ( β) )为 3 6 5h。按剂量 75 ,2 5 ,10 ,3 3μg/kg肌注12 5I NGF ,测得消除相半衰期 (t1/g( β) )分别为 1 79,2 2 5 ,2 30 ,3 2 4h ,平均达峰时间 (tmax)为 0 5 8h ,平均血浆清除率 (CLs)为0 37L/ (h·kg) ,表观分布容积 (Vd)为 1 18L/kg ,体内平均滞留时间 ( tr)为 2 78h。

       

      Abstract: I Nerve growth factor ( 125 I NGF) with more than 95% of radiochemical purity is prepared by chloramine T method.After iv and im injection of 125 I NGF,pharmacokinetics of NGF in mice is determined by SDS PAGE method. The results show that concentration time curves after iv injection are fitted to a 2 compartment model and those after im injection are fitted to a 1 compartment model. After iv injection of 25 μg/kg,the elimination half life ( t 1/2 (β) ) is 3.65 h. After im injection of 75,25,10,3.3 μg/kg, t 1/2(β) is 1.79,2.25,2.30,3.24 h,respectively. The mean plasma clearance (CLs) is 0.37 L/(h·kg), the appearance volume of distribution ( V d) is 1.18 L/kg and the mean residence time ( r) in mice is 2.78 h. The pharmacokinetics of 125 I NGF in mice is useful for clinical trial.

       

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