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用于表征99mTc标记生物共轭物的放射性液相色谱-质谱联用技术

Radio-LC-MS for the characterization of 99mTc-labeled bioconjugates.

作者信息

Liu S, Ziegler M C, Edwards D S

机构信息

DuPont Pharmaceuticals Company, Medical Imaging Division, North Billerica, Massachusetts 01862, USA.

出版信息

Bioconjug Chem. 2000 Jan-Feb;11(1):113-7. doi: 10.1021/bc990111r.

DOI:10.1021/bc990111r
PMID:10639093
Abstract

This report describes the first example of using radio-LC-MS for determining the composition of (99m)Tc radiopharmaceuticals at the tracer level. The in-line radiometric detector is a useful addition to a standard LC-MS and provides direct correlation between the MS data and the radioactive species in a radiopharmaceutical kit. Complexes [(99m)Tc(HYNICtide)(tricine)(L)] (RP444, L = TPPTS; RP445, L = TPPDS; and RP446, L = TPPMS) were prepared using a decayed generator eluant. All the ternary ligand (99m)Tc complexes show the expected monoprotonated molecular ions, (M + 1)(+), and diprotonated molecular ions, (M + 2)(2+). The LC-MS spectral data support the proposed structure and are consistent with those obtained for their corresponding (99)Tc analogues. Ternary ligand complexes [(99m)Tc(HYNICtide)(tricine)(L)] (L = ISONIC-HE and ISONIC-Sorb) are neutral, and the molecular weights are also lower than that of RP444. Using a fresh generator eluant (24 h prior elution), only 1-2 mCi of (99m)Tc [(7 x 10(-)(12))-(1.5 x 10(-)(11)) mol of technetium complex] are required to obtain a reasonably clean mass spectrum. Radio-LC-MS is a quick and accurate analytical tool for characterization of (99m)Tc radiopharmaceuticals at the tracer level.

摘要

本报告描述了使用放射性液相色谱 - 质谱法在示踪剂水平测定(99m)Tc放射性药物组成的首个实例。在线放射性检测器是标准液相色谱 - 质谱仪的一个有用补充,它能在质谱数据与放射性药物试剂盒中的放射性物质之间建立直接关联。使用衰变发生器洗脱液制备了配合物[(99m)Tc(HYNICtide)(tricine)(L)](RP444,L = TPPTS;RP445,L = TPPDS;以及RP446,L = TPPMS)。所有三元配体(99m)Tc配合物均显示出预期的单质子化分子离子(M + 1)(+)和双质子化分子离子(M + 2)(2+)。液相色谱 - 质谱光谱数据支持所提出的结构,并且与相应的(99)Tc类似物所获得的数据一致。三元配体配合物[(99m)Tc(HYNICtide)(tricine)(L)](L = ISONIC - HE和ISONIC - Sorb)呈中性,且分子量也低于RP444。使用新鲜的发生器洗脱液(洗脱前24小时),仅需1 - 2毫居里的(99m)Tc[(7×10^( - 12)) - (1.5×10^( - 11))摩尔的锝配合物]就能获得相当纯净的质谱图。放射性液相色谱 - 质谱法是一种在示踪剂水平表征(99m)Tc放射性药物的快速且准确的分析工具。

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