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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 authors studied the pharmacokinetics of 131I-labeled anti-human hepatocellular carcinoma monoclonal antibodies HAb18 and F(ab’)2, Fab fragments in mice. The results showed that: (1) The pharmacokinetics patterns of the three markers were quite different. The clearance process of intact antibody HAb18 was in accordance with the open-to-empty model. The clearance rate was related to the injected dose. According to the dose from high to low, the T1/2 (whole excretion) were 48.08h, 42.65h, 40.54h; T1/2 (blood clearance) was 61.42h, 48.07h, 41.03h in order. (2) The removal rate of antibody fragments was significantly faster than that of intact antibodies, and the biphasic decrease in the clearance process was consistent with the two-compartment model. F(ab’). The overall excretion of T1/2a was 5.29 h, T1/2β was 39.37 h; the T1/2a for blood clearance was 4.20 h, T1/2β was 34.61 h. The total excretion of Fab fragments was 3.51 h, T1/2β was 20.22 h, T1/2a for blood clearance was 1.39 h, T1/2β was 24.39 h. Tip: Intact antibodies are suitable for tumor-directed therapy. Imaging diagnostics are better for antibody fragments.