摘要
目的研究聚乙二醇化重组人白细胞介素-6(PEG-rhIL-6)单次皮下注射后在大鼠体内的药代动力学过程和组织分布。方法用同位素示踪法,碘标记PEG-rhIL-6,采用三氯乙酸(TCA)沉淀法检测放射性浓度,3P87软件判断房室模型和计算各种参数,并检测125I-PEG-rhIL-6皮下注射大鼠后不同时间的血药浓度,组织分布以及排泄。结果3、20和40μg/kg3个剂量的125I-PEG-rhIL-6皮下注射大鼠后,吸收半衰期(t1/2Ka)分别为10.44、11.25和11.37h;消除半衰期(t1/2Ke)分别为20.47、21.53和19.77h,达峰时间(Tpeak)分别为20.51、21.96和21.30h;PEG-rhIL-6在大鼠体内的组织分布主要在血液;PEG-rhIL-6主要通过尿液排出体外。结论PEG-rhIL-6在大鼠体内的药代动学过程基本符合线性药动学特征,血药浓度-时间曲线符合一房室模型。经PEG修饰的rhIL-6在大鼠体内的半衰期明显延长。
Objective To study the pharmaeokinetics and tissue distribution of PEG-rhIL-6 in rats after a single dose administration. Methods Pharmacokinetics and distribution of PEG-rhIL-6 in rats were studied by ^125I isotope tracing method. Pharmacokinetie analysis was performed using 3P97 computer software. Results PEG-rhIL- 6 declined in one-compartment model with half-lives of 10.44-11.37 h for t1/2 Ka, 19.77-21. 53 h for t1/2 Ke and 20.51-21.96 h for Tpeak, respectively. PECr-rhIL-6 was mainly distributed in blood and excreted via urine. Conclusion The half-lives of PEG-rhIL-6 are prolonged after being modified by PEG.
出处
《四川大学学报（医学版）》
CAS
CSCD
北大核心
2009年第1期149-152,共4页
Journal of Sichuan University(Medical Sciences)
