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锝-99m(V)二巯基丁二酸在动物肿瘤模型中的药代动力学和生物分布

The pharmacokinetics and biodistribution of technetium-99m(V)dimercaptosuccinic acid in an animal tumor model.

作者信息

Watkinson J C, Allen S J, Laws D E, Lazarus C R, Maisey M N, Clarke S E

机构信息

Department of Otolaryngology, Guy's Hospital, London, England.

出版信息

J Nucl Med. 1991 Jun;32(6):1235-8.

PMID:1646304
Abstract

This study used an established rabbit tumor model with squamous carcinoma to evaluate the pharmacokinetics and biodistribution of technetium-99m-(V)dimercaptosuccinic acid. A total of 54 rabbits were studied (25 with no tumor; 29 with tumor). Technetium-99m(V)dimercaptosuccinic acid had a bi-exponential blood clearance in rabbits with no tumors (28 and 325 min) and in rabbits with tumors (27 and 352 min). There was no significant difference (p greater than 0.05) in mean clearance times between the two groups and clearance appeared unaffected by tumor mass. Technetium-99m(V)dimercaptosuccinic acid had a bi-exponential cumulative urine excretion with no apparent difference in half-times between non-tumor and tumor rabbit groups (200 and 240 min, respectively). Technetium-99m(V)dimercaptosuccinic acid had a major organ biodistribution in rabbits which included bone, kidneys, bladder and the blood pool. The major route of excretion was via the urine. There was no significant difference (p greater than 0.05) in organ biodistribution between rabbits with no tumors and rabbits with tumors and there was no evidence of active uptake of technetium-99m(V)dimercaptosuccinic acid by either squamous carcinoma or inflammatory tissue.

摘要

本研究使用已建立的兔鳞状细胞癌肿瘤模型来评估锝-99m-(V)二巯基丁二酸的药代动力学和生物分布。总共研究了54只兔子(25只无肿瘤;29只患有肿瘤)。锝-99m(V)二巯基丁二酸在无肿瘤兔子(28和325分钟)和患有肿瘤的兔子(27和352分钟)体内呈现双指数血液清除。两组之间的平均清除时间无显著差异(p大于0.05),且清除似乎不受肿瘤大小的影响。锝-99m(V)二巯基丁二酸呈现双指数累积尿排泄,非肿瘤和肿瘤兔组之间的半衰期无明显差异(分别为200和240分钟)。锝-99m(V)二巯基丁二酸在兔子体内的主要器官生物分布包括骨骼、肾脏、膀胱和血池。主要排泄途径是通过尿液。无肿瘤兔子和患有肿瘤的兔子之间的器官生物分布无显著差异(p大于0.05),且没有证据表明鳞状细胞癌或炎症组织对锝-99m(V)二巯基丁二酸有主动摄取。

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The pharmacokinetics and biodistribution of technetium-99m(V)dimercaptosuccinic acid in an animal tumor model.锝-99m(V)二巯基丁二酸在动物肿瘤模型中的药代动力学和生物分布
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In vitro and in vivo evaluation of the influence of type III NaPi co-transporter activity during apoptosis on 99mTc-(V)DMSA uptake in the human leukaemic cell line U937.体外和体内评估凋亡过程中III型钠磷共转运体活性对人白血病细胞系U937摄取99mTc-(V)DMSA的影响。
Eur J Nucl Med Mol Imaging. 2004 Oct;31(10):1421-7. doi: 10.1007/s00259-004-1605-y. Epub 2004 Jun 16.
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Evaluation of Tc-99m(V) DMSA for imaging inflammatory lesions: an experimental study.
锝-99m(V)二巯基丁二酸用于炎性病变成像的评估:一项实验研究。
Ann Nucl Med. 1996 Nov;10(4):419-23. doi: 10.1007/BF03164803.