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99m锝标记肝素:在药代动力学和生物分布研究中作为肝素活性示踪剂的潜在价值。

99m Technetium labelled heparin: potential value as a tracer of heparin activity in pharmacokinetic and biodistribution studies.

作者信息

Perdrisot R, Barbu M, Bok B, Berthelot J L, Mazoyer B, Colas-Linhart N

出版信息

Biomed Pharmacother. 1984;38(8):414-6.

PMID:6543145
Abstract

Pharmacokinetics and biodistribution of 99m Technetium (99mTc) labelled heparin were studies to assess its value as a tracer of heparin kinetics in comparison with unlabelled heparin. In vitro, the stability and labelling efficiency (98%) of the labelled drug were excellent and elution was minimal. In vivo, after I.V. infusion of the drug, there was no difference in the same animal between anticoagulant activity measurements and radioactive countings, both displaying a plasmatic biexponential pattern (T1 = 2.9 minutes, T2 = 76 minutes). Biodistribution studies showed primarily liver, spleen and kidney accumulation, with no thyroid uptake. The advantages of this technetium labelling may therefore be used for the heparin drug in various experimental and pathological situations even in humans.

摘要

研究了99m锝(99mTc)标记肝素的药代动力学和生物分布,以评估其作为肝素动力学示踪剂与未标记肝素相比的价值。在体外,标记药物的稳定性和标记效率(98%)极佳,洗脱极少。在体内,静脉注射该药物后,同一动物的抗凝活性测量值与放射性计数之间无差异,两者均呈现血浆双指数模式(T1 = 2.9分钟,T2 = 76分钟)。生物分布研究显示主要在肝脏、脾脏和肾脏蓄积,无甲状腺摄取。因此,这种锝标记的优点可用于肝素药物,甚至在各种实验和病理情况下用于人类。

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