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用Iodogen法制备125I-rhIL-2。产品用SephadexG-50凝胶过滤纯化。流出的组分用SDS-PAGE测定纯度,选取放化纯度高于95%的进行药代动力学研究。在iv剂量为500,1000及2500ng/mouse的125I-rhIL-2后,浓度-时间曲线按三房室模型拟合,其快分布相T1/2π约为3min,慢分布相T1/2α约为82min,终末消除相T1/2β为7.5h左右。AUC与剂量呈较好的线性关系(r=0.9998)。im125I-rhIL-21000ng/mouse后浓度-时间曲线符合一室一级吸收,绝对生物利用度为0.52,达峰浓度、时间分别为23.05ng/ml和1.94h。iv15min后,在肝脏中的浓度最高。24h内排出约77%的标记药物。
125I-rhIL-2 was prepared by the Iodogen method. The product was purified by gel filtration on Sephadex G-50. The eluted fractions were assayed for purity by SDS-PAGE. Pharmacokinetic studies were performed with radiochemical purity greater than 95%. After iv doses of 500, 1000 and 2500 ng / mouse of 125I-rhIL-2, the concentration-time curves were fitted in a three-compartment model with a fast distribution phase T1 / 2π of approximately 3 min and a slow distribution phase T1 / 2α of approximately 82min, terminal elimination phase T1 / 2β is about 7.5h. AUC showed a good linear relationship with the dose (r = 0.9998). After im125I-rhIL-21000ng / mouse, the concentration-time curve was in accordance with the first-order absorption, the absolute bioavailability was 0.52 and the peak concentration was 23.05ng / ml and 1.94h respectively. After iv15min, the highest concentration in the liver. Approximately 77% of the labeled drug is discharged within 24 hours.