| 郝 攀,张春丽,马 超.131I-BDI-1在荷人膀胱癌裸鼠体内的药代动力学研究[J].肿瘤学杂志,2015,21(4):275-278. |
| 131I-BDI-1在荷人膀胱癌裸鼠体内的药代动力学研究 |
| Study on Biodistribution and Pharmacokinetic of 131I-BDI-1 in Nude Mice Bearing Human Bladder Carcinoma |
| 投稿时间：2014-10-15 |
| DOI：10.11735/j.issn.1671-170X.2015.04.B004 |
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| 中文关键词: 药代动力学 膀胱肿瘤 组织分布 裸鼠 BDI |
| 英文关键词:pharmacokinetic bladder neoplasms biodistribution nude mice BDI |
| 基金项目:北京市自然科学基金（7112129）；卫生部重点实验室、江苏省分子核医学重点实验室开放课题基金（KF201101） |
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| 中文摘要: |
| 摘 要：［目的］ 用131I标记人膀胱癌特异性单克隆抗体BDI-1，探讨其在荷瘤裸鼠体内的生物分布及药代动力学参数，为其作为膀胱癌诊断和治疗的新型靶向药物提供基础数据。［方法］ 用Ch-T法进行BDI-1的131I标记，标记完成后，采用Sephadex G-25分离纯化，用纸层析法测定标记产物的放化纯度，经尾静脉注入到荷人膀胱癌裸鼠体内，在不同时间处死裸鼠，测定裸鼠体内生物分布，采用 DAS 2.0 软件计算药代动力学参数。［结果］静注后，131I-BDI-1主要分布于荷瘤裸鼠肝脏、脾脏、肾脏和肿瘤等组织。血液药—时曲线符合开放性二房室分布模型，其中分布相半衰期［t1/2(α)］为0.1693h，消除相半衰期［t1/2(β)］为69.315h，峰值时间tmax为0.033h，平均血浆清除率为67.154L/（h·kg），曲线下面积AUC(0-t)为904.006mg/L·h-1；药物在肿瘤中摄取的峰时为72h。［结论］ 131I-BDI-1在荷人膀胱癌裸鼠中具有特异的肿瘤摄取，其在血液中清除较快，而在肿瘤中具有较快的吸收半衰期及较长的清除半衰期，适合作为一种肿瘤的靶向诊断与治疗药物。 |
| 英文摘要: |
| Abstract：［Purpose］ To investigate the biodistribution and pharmacokinetics of 131I-BDI-1 in nude mice model bearing human bladder cancer，for the basic date used as a new targeted drug. ［Methods］ Anti human bladder carcinoma monoclonal antibodies BDI-1 was labeled with 131I by chloramine-T method to prepare 131I-BDI-1 at room temperature. The radio-chemical purity was tested with paper chromatography. Nude mice bearing human bladder cancer were injected of 131I-BDI-1 via tail vein. Then the mice were sacrificed at different time.Its biodistribution was analyzed. DAS 2.0 was used to calculate pharmacokinetics. ［Results］ The biodistribution data showed that 131I-BDI-1 accumulated mainly in liver，spleen，kidney and tumor. It was indicative of a two-compartment model with the main pharmacokinetic parameters as follows：t1/2(α)，t1/2(β) and tmax were 0.1693h，69.315h，0.033h respectively. CL，k10，k12 and k21 were 67.154L/（h·kg），6.021h-1，1.103h-1，0.88h-1 respectively. The AUC(0-t)was 904.006mg/L·h-1.The highest time tumor uptake of 131I-BDI-1 was 72h. ［Conclusion］ 131I-BDI-1 in nude mice model bearing human bladder cancer has a specific tumor intake，and in the blood it clears up faster.The t1/2(β) and CL suggest that it could be applied in guiding diagnosis and treatment for bladder cancer. |
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