【摘要】 采用Iodogen法标记了西夫韦肽(Sifuvirtide),并用S-100 HR凝胶柱分离纯化标记物1。25I-sifuvirtide放化纯度>99.0%,比活度为3.9 GBq.g-1;标记后的蛋白仍具有一定的生物活性。三氯醋酸(TCA)沉淀法测定125I-sifuvirtide在生物样品中含量:血浆中125I-sifuvirtide的放射性活度为286.5~26 125.5 Bq.mL-1时,125I-sifuvirtide的放射性计数和沉淀放射性计数的线性相关系数为0.999 8±0.000 5,回收率为72.3%±6.9%。猕猴静脉和皮下推注125I-sifuvirtide后,血浆TCA酸沉放射性浓度时间曲线符合二房室模型;皮下给药后平均消除半衰期为95.83 h,达峰时间平均为3.35 h,平均绝对生物利用度为85.2%。更多还原

【Abstract】 ¹²⁵I-sifuvirtide is prepared by Iodogen method,the radiochemical purity of ¹²⁵I-sifuvirtide is over 99.0%,and the specific activity of ¹²⁵I-sifuvirtide is 3.9 GBq·g^-1.The labeled product still maintain some biological activity.The radioactivity in plasma is determined by trichloroacetic acid precipitation method.The pharmacokinetics of ¹²⁵I-sifuvirtide is successfully modeled using two-compartmental after subcutaneous（SC） or intravenous（IV） administration in rhesus monkeys according to the curve of radioactivity of TCA precipitable vs time.The mean half-life(t_1/2) value is 95.83 h,the mean time to maximum concentration is 3.35 h,and the mean bioavailability is 85.2% after SC administration.更多还原