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目的研究SD大鼠单次及多次皮下注射聚乙二醇干扰素α2b(PEG-IFNα2b)的药代动力学特征。方法单次皮下注射按18、180、900μg/kg给药;多次皮下注射按180μg/kg,1、4、7d给药;在不同时间点采集血样,ELISA法检测血药浓度,并计算药代动力学参数。结果SD大鼠单次给药的血药浓度-时间曲线呈剂量依赖关系,体内呈一级动力学过程,具有线性动力学特征;多次给药后,未见PEG-IFNα2b的达峰值时间延长及峰浓度升高的现象,曲线下面积(AUC)亦未见增加,末次给药后大鼠的血药浓度曲线呈一室开发模型,半衰期与单次给药半衰期无明显差异,多次皮下给药无蓄积倾向。结论PEG-IFNα2b半衰期比IFNα2b显著延长,使用PEG-IFNα2b可以减少用药频次,并可能提高疗效。
Objective To study the pharmacokinetics of peginterferon α2b (PEG-IFNα2b) single and multiple subcutaneous in SD rats. Methods A single subcutaneous injection of 18,180,900μg / kg administration; multiple subcutaneous injection of 180μg / kg, 1,4,7 d administration; blood samples were collected at different time points, ELISA assay blood concentration and calculate the drug Generational dynamics parameters. Results The plasma concentration-time curve of single-dose administration of SD rats showed a dose-dependent relationship with a first-order kinetic process in vivo with linear kinetic characteristics. After repeated administration, the peak time of PEG-IFNα2b was not prolonged And the peak concentration increased, the area under the curve (AUC) also did not increase, the last dose of rat plasma concentration curve showed a one-compartment development model, half-life and single administration half-life no significant difference in multiple subcutaneous No tendency to accumulate. Conclusion The half-life of PEG-IFNα2b is significantly longer than that of IFNα2b. The use of PEG-IFNα2b can reduce the frequency of medication and may improve the curative effect.