【摘要】 目的研究99Tcm-ASON-EGF药物的制备及其在健康兔体内的药代动力学特征。方法制备99Tcm-ASON-EGF,用放射性计数法测定兔血药浓度变化;采用3p97软件处理数据,根据AIC值、R2值、1/c与F检验,判断药物客观符合的房室模型;随后,求出其分布半衰期、消除半衰期、中央室分布容积、总表观分布容积、总清除率;最后用三氯醋酸法测定其血浆蛋白结合率。结果99Tcm-ASON-EGF的最佳房室模型是二室模型,其分布半衰期是5.28min;消除半衰期是89.23min;中央室分布容积是67.8ml;总表观分布容积是915.6ml;总清除率是7.1ml/min。与人血浆孵育1.5h后,血浆蛋白结合率为10.69%。结论99Tcm-ASON-EGF在健康兔体内的转运过程符合二室模型,具有良好的药代动力学特征。更多还原

【Abstract】 Objective To prepare and explore the pharmacokinetic parameters for ~ 99 Tc~ m -ASON-EGF in healthy rabbits. Methods ~ 99 Tc~ m -ASON-EGF was prepared according to previous methods and its changes of concentration in blood were measured by radioactivity counts per minute. The experimental data were dealt with by 3p97 software and its true compartment model was estimated by AIC value, R~ 2 value, the 1/c and F test. Subsequently, its half-life of distribution (T_ 1/2 α), half-life of elimination (T_ 1/2 β), central compartment volume of distribution (Vc), total apparent volume of distribution (Vd) and total rate of clearance (CL) were calculated by the software. Finally, the binding rate of plasma protein was determined by trichloroacetic acid precipitation. Results The best model of ~ 99 Tc~ m -ASON-EGF in vivo was two-compartment model and its T_ 1/2 α, T_ 1/2 β, Vc, Vd and CL were 5.28 min, 89.23 min, 67.8 ml, 915.6 ml and 7.1 ml/min respectively. After being incubated with fresh plasma for 1.5 h, its binding rate was 10.69%. Conclusion Its process of transportation in healthy rabbits is fitted to two-compartment model and the pharmacokinetic properties are desirable.更多还原