<sup>125</sup>I示踪法检测西夫韦肽在生物体内的代谢过程

¹²⁵I示踪法检测西夫韦肽在生物体内的代谢过程

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。125I-sifuvirtide放化纯度＞99.0%，比活为3.9 GBq•g-1；标记后的蛋白仍具有一定生物活性。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286.5-26125.5 Bq•mL-1时，线性为0.9998±0.0005，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%。

Abstract: 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 (t1/2) 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.125I-sifuvirtide is prepared by Iodogen method, the radiochemical purity of