摘要
目的 研究99m 锝标记肝癌单克隆抗体HAb18及其片段F(ab′) 2 在正常小鼠体内的药代动力学。方法 4组小鼠经尾静脉分别注入 7.5MBq99mTc HAb18;0 .9MBq ,7.5MBq ,37MBq99mTc F(ab′) 2 ,在不同时间点测尾血的放射性计数。另取 18只小鼠尾静脉注入 7.5MBq99mTc F(ab′) 2 在不同点处死 ,测量各脏器放射性计数。结果 99mTc F(ab′) 2 ,99mTc HAb18的药代动力学均符合二室开放模型 ,二者在 7.5MBq剂量时有关的参数分别为t1 2 β(5 .3± 0 .4)h ,(15 .5± 1.4)h (P <0 .0 5 ) ;Vc(12 9.2± 2 3.7)μl·g- 1 ,(10 3 .5± 6 .8) μl·g- 1 (P >0 .0 5 ) ;CL(6 3.4± 12 .5 ) ,(10 .6± 1.3) μl·g·h- 1 (P <0 .0 1) ;AUC(0 .0 0 7± 0 .0 0 1) ,(0 .0 4± 0 .0 0 7)MBq·h·μl- 1 (P <0 .0 1)。结论 不同剂量的99mTc F(ab′) 2
OBJECTIVE To study the phamacokinetics of anti hepatoma monoclonal antibody HAb18 and its F(ab′) 2 fragment labeled with 99m Tc in mice.METHODS The different doses of radio immunoconjugates were intravenously administered to normal BALB/c mice.The blood radioactivity was measured at different time.Biodistribution was investigated by killing the mice at different time.The organs radioactivity measured.RESULTS The pharmacokinetic characteristics of both 99m Tc F(ab′) 2 and 99m Tc IgG conformed to a two compartment open model.The parameters of F(ab′) 2 and IgG were t 1/2β (5.3±0.4),(15.5±1.4) h ( P <0.05); V c(129.2±23.7),(103.5±6.8) μl·g -1 ( P > 0.05 ); CL (63.4±12.5),(10.6±1.3) μl·g·h -1 ( P <0.01); AUC (0.007±0.001),(0.04±0.007) MBq·h·μl -1 ( P < 0.01 ).CONCLUSION The elimination of 99m Tc F(ab′) 2 in different doses followed first order,respectively.
出处
《中国药学杂志》
CSCD
北大核心
2000年第7期465-467,共3页
Chinese Pharmaceutical Journal