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目的 :建立35S MAbSZ3 9药代动力学模型 ,求取药代动力学参数 ,设计合理用药方案。方法 :以药代动力学程序包处理35S MAbSZ3 9给药后荷瘤鼠各时间点的血药浓度 ,进行药代动力学研究 ;以35S nIgG及35S为对照组 ,了解35S MAbSZ3 9的荷瘤鼠体内分布特点。结果 :35S MAbSZ3 9在荷人脑胶质瘤裸小鼠体内药代动力学符合三室线性模型 ,总药时方程为ct=1 764e-3 49t+1 10 6e-0 5t+0 0 2 5e-0 0 17t,t1/ 2α为 0 2 3h ,t1/ 2 β为 1 4 6h ,t1/ 2 γ为 4 2 9h。体内分布研究表明 ,35S MAbSZ3 9可特异性浓聚于胶质瘤 ,在正常组织中无明显蓄积 ,发挥了单抗导向的高选择性作用 ,在给药后第 5天 ,与35S nIgG及35S相比 ,特异指数分别为 4 1和 4 87,具有显著优越性 (P <0 0 5 )。结论 :35S MAbSZ3 9有望作为一种高效低毒的导向放疗制剂应用于胶质瘤治疗 ,以一周间隔多疗程治疗方案为佳
OBJECTIVE: To establish a 35S MAbSZ3 9 pharmacokinetic model to determine pharmacokinetic parameters and design a rational drug regimen. Methods: Pharmacokinetics of 35S MAbSZ3 9 drug-treated mice at various time points after treatment of plasma concentration, pharmacokinetic study; 35S nIgG and 35S as a control group to understand 35S MAbSZ3 9 tumor Rat body distribution characteristics. Results: The pharmacokinetics of 35S MAbSZ3 9 in nude mice bearing human glioma were in accordance with the three-compartment linear model. The total time-course equation was ct = 1 764e-3 49t + 1 10 6e-0 5t + 0 0 2 5e- 0 0 17t, t1 / 2α is 0 2 3h, t1 / 2 β is 1 4 6h, t1 / 2 γ is 4 2 9h. In vivo distribution studies showed that 35S MAbSZ3 9 could specifically accumulate in gliomas without obvious accumulation in normal tissues, which showed the high selective effect of mAb-directed. On the fifth day after administration, 35S MAbSZ3 9 was associated with 35S nIgG and 35S Compared with the specific index of 4 1 and 4 87, respectively, with significant advantages (P <0 05). Conclusion: 35S MAbSZ3 9 is expected to be used as a highly effective and low toxicity targeted radiotherapy in glioma treatment.