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[光活化在放射性药物制备中的应用。I. 用锝(99mTc)标记的人免疫球蛋白]

[Use of photoactivation in the preparation of radiopharmaceuticals. I. Human immunoglobulin labelled with technetium (99mTc)].

作者信息

Komárek P, Kleisner I, Konopková M, Komárko I

机构信息

Katedra farmaceutické technologie IPVZ, Praha.

出版信息

Ceska Slov Farm. 1997 Jun;46(3):122-7.

PMID:9440949
Abstract

The aim of the study was to evaluate the photochemical effects of ultraviolet (UV) light on biologically active substances usable in radionuclide diagnosis. Human immunoglobulin (IgG) was irradiated with UV light at 254 nm and labelled with technetium(99mTc) by reducing pertechnetate(99mTc) with stannous chloride, or by use of redox polymer (RP SP-C25). Radiochemical purity was evaluated using paper chromatography. The biodistribution of labelled IgG in rats with experimentally induced inflammation was determined by counting the 99mTc activity of isolated organs or by planar gamma camera imaging 4 and 26 hours after administration. Irradiated IgG shows a higher efficacy of 99mTc labelling (98%) compared with non-irradiated IgG (95%) and photoactivation raises the number of free SH groups. UV light has a beneficial effect on 99mTc-IgG stability. The stability of a kit prepared using redox polymer is significantly higher (by 20%) compared with that of a kit prepared using stannous chloride (by 10%). Human IgG irradiation more than triples 99mTc deposition into inflammatory lesions. Photoactivation can be used in formulating protein-based radiopharmaceuticals in an effort to improve their biodistribution in nuclear medicine diagnostic imaging.

摘要

本研究的目的是评估紫外线(UV)对可用于放射性核素诊断的生物活性物质的光化学效应。用254nm的紫外线照射人免疫球蛋白(IgG),并通过用氯化亚锡还原高锝酸盐(99mTc)或使用氧化还原聚合物(RP SP-C25)将其用锝(99mTc)标记。使用纸色谱法评估放射化学纯度。通过在给药后4小时和26小时计数分离器官的99mTc活性或通过平面γ相机成像来确定标记的IgG在实验性诱导炎症的大鼠中的生物分布。与未照射的IgG(95%)相比,照射的IgG显示出更高的99mTc标记效率(98%),并且光活化增加了游离SH基团的数量。紫外线对99mTc-IgG的稳定性有有益影响。与使用氯化亚锡制备的试剂盒(10%)相比,使用氧化还原聚合物制备的试剂盒的稳定性显著更高(20%)。人IgG照射使99mTc在炎症病变中的沉积增加了两倍多。光活化可用于配制基于蛋白质的放射性药物,以改善其在核医学诊断成像中的生物分布。

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