摘要
作者对１３１Ｉ标记的抗人肝细胞癌单克隆抗体ＨＡｂ１８及Ｆ（ａｂ′）２、Ｆａｂ片段在小鼠体内的药代动力学进行研究。结果表明：（１）３种标记物的药代动力学模式有很大差异，完整抗体ＨＡｂ１８的清除过程符合开放一空模型，清除速率与注射剂量有关。按照剂量从高至低，其Ｔ１／２（整体排泄）分别为４８．０８ｈ、４２．６５ｈ、４０．５４ｈ；Ｔ１／２（血液清除）依次为６１．４２ｈ、４８．０７ｈ、４１．０３ｈ。（２）抗体片段的清除速率明显快于完整抗体，清除过程呈双相下降，符合二室模型。Ｆ（ａｂ′）。整体排泄的Ｔ１／２ａ为５．２９ｈ，Ｔ１／２β为３９．３７ｈ；血液清除的Ｔ１／２ａ为４．２０ｈ，Ｔ１／２β为３４．６１ｈ。Ｆａｂ片段整体排泄的Ｔ１／２ａ为３．５１ｈ，Ｔ１／２β为２０．２２ｈ；血液清除的Ｔ１／２ａ为１．３９ｈ，Ｔ１／２β为２４．３９ｈ。提示：完整抗体适用于肿瘤导向治疗，显像诊断则以抗体片段为佳。
The pharmacokinetics of 131I-labelled HAb18 McAb against primary hepatocellular carcinoma(PHC) and its F(ab' )2 and Fab fragments following i. v. administration in BALB/c mice was investigated. Dynamic observations showed that the pharmacokinetics of 131 I-labelled HAb18 was significantly different from that of the fragments. (1 ) The pharmacokinetics of HAb18 conformed to a onecompart-mendal open pharmacokinetic model. The clearance rate was relevant to injection doses, andthe higher doses produced lower clearance values. (2)The pharmacokinetics of the F(ab' )2 was similarto that of the Fab and fitted to a two-compartmental pharmacokinetic model. The clearance process ofthe fragments was significantly fast than intact HAb18 McAb. These results suggest that the fragmentshave an adventage to targeted imaging for PHC, wherase the radio-labelled indict anibody is more suitable for cancer therapy.
出处
《细胞与分子免疫学杂志》
CSCD
1996年第1期16-21,共6页
Chinese Journal of Cellular and Molecular Immunology
关键词
单克隆抗体
药代动力学
肝肿瘤
antibody
monoclonal
F(ab')_2
Fab
pharmacokinetics
