五加皮Age蛋白的药动学研究

Pharmacokinetics of Age protein in Cortex Acanthopanax

目的研究五加皮Age蛋白的药动学特征。方法采用氯胺T法用125I标记Age蛋白,形成125I-Age复合物。S180荷瘤小鼠iv给药后,采用同位素示踪法结合SDS-PAGE电泳测定血浆中Age蛋白质量浓度。用3P87药动学软件分析血浆中Age蛋白的药动学参数。结果小鼠iv125I-Age后,Age蛋白在体内的代谢符合二房室分布模型。按剂量50、100、200μg/kgiv后,测得Age蛋白分布相半衰期(t1/2α)分别为0.34、0.45、0.26h,消除相半衰期(t1/2β)为14.13、16.49、17.42h,全身清除率(CLs)为0.0454、0.0491、0.0533mL/(h·kg)。结论Age蛋白在荷瘤小鼠体内药动学行为符合线性二室模型,在体内的分布和消除均较慢。

Objective To study the pharmacokinetic characteristics of Age protein in Cortex Acanthopanax. Methods Age protein was labeled using ^125I with chloramine-T method, the concentration of Age protein in mouse plasma was determined by radioisotope tracer labeling method combined with SDS-PAGE. The pharmacokinetic parameters of Age protein in plasma were evaluated by a pharma- cokinetic 3P87 software. Results The results showed that concentration-time curves after iv ^125I-Age to mice were fitted to a two-compartment model. Following iv ^125I-Age to mice in three doses of 50, 100, and 200 μg/kg, the t1/2α were 0.34, 0.45, and 0.26 h, and t1/2β were 14.13, 16.49, and 17.42 h. The systemic clearances （CLs） were 0. 045 4, 0. 049 1, and 0. 053 3 mL/（h· kg）. Conclusion Pharmacokinetics of Age protein conforms to linear two-compartment model and it＇s distribution and elimination are both slow in tumor-bearing mice in vivo.