单克隆抗体及F(ab′)_2片段在小鼠体内的药物动力学研究

The study of pharmacokinetics of intact monoclonal antibody and its Fregment F(ab')_2 in mice

用^(125)I标记单克隆抗体(IgG2a)和相应片段F(ab′)_2,比较它们经静脉或腹腔不同途径注射后在小鼠体内的药物动力学变化。结果显示,同一种抗体形式(完整抗体或F(ab′)_2经iv或ip不同途径给药时,整体排泄率、血液清除率和生物半衰期等无明显差异(P>0.05);而相同途径给药时,完整抗体与F(ab′)_2比较,二者的Ke、T1/2、TBCL显著差异(P<0.05-0.01),完整抗体腹腔注射的生物利用度94％。提示:F(ab′)_2片段有利于改善肿瘤体内定位显象,腹腔注射是有效的给药途径。

Pharmacoki netics of intact MAb 2F7 (IgG2a) and its fragment F (ab')_2 are studied in mice. Different iniection routes (iv or i p) didn't affect clearance of intact Ab or F (ab' )_2 (P>0.05). When compared intact Ab with F (ab')_2 in same iniection route, their Ke, T 1/2 and TBCL are very distinct (P<0.05-0.01).EBA % of Ab ip is 94%. F (ab')_2 with faster clearance can improve tumor imaging in vivo.Intraperitoneal iniection of MAb is a effective way.