Development of kit formulations for (99m) TcN-MPO: a cationic radiotracer for myocardial perfusion imaging.
Development of kit formulations for (99m) TcN-MPO: a cationic radiotracer for myocardial perfusion imaging.
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DOI：
10.1002/jlcr.3221
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发表时间：
2014-07
影响因子：
1.8
通讯作者：
Liu, Shuang
中科院分区：
文献类型：
--
作者：
Zheng, Yumin;Ji, Shundong;Tomaselli, Elena;Liu, Shuang
本研究的目的是开发99 mTcN-MPO的试剂盒配方，以支持其作为SPECT放射性示踪剂的临床评价。使用三种不同的制剂（含/不含SnCl 2的两瓶制剂和单瓶制剂）进行放射性标记研究，以探索影响99 mTcN-MPO放射化学纯度（RCP）的因素。我们发现影响99 mTcN-MPO RCP的最重要因素是PNP 5的纯度。使用两瓶制剂制备> 98%RCP（n = 20）的99 mTcN-MPO。对于含/不含SnCl 2的单瓶制剂，β-环糊精（β-CD）作为PNP 5的稳定剂特别有用。99 mTcN-MPO对β-CD的RCP为95 - 98%，而对γ-CD的RCP仅为90 - 93%。PNP 5与β-CD的内腔结合更好，在单瓶制剂中形成比γ-CD更稳定的包合物。在Sprague-Dawley（SD）大鼠中进行的生物分布和成像研究的结果清楚地证明了三种不同制剂的生物等效性。SPECT数据表明，在注射后0 - 30分钟可以获得高质量的图像，而不会受到肝脏放射性的显著干扰。考虑到99 mTc标记的容易性和99 mTcN-MPO的高RCP，非SnCl 2单瓶制剂是未来临床研究的有吸引力的选择。
The objective of this study was to develop a kit formulation for 99mTcN-MPO to support its clinical evaluations as a SPECT radiotracer. Radiolabeling studies were performed using three different formulations (two-vial formulation and single-vial formulations with/without SnCl2) to explore the factors influencing radiochemical purity (RCP) of 99mTcN-MPO. We found that the most important factor affecting the RCP of 99mTcN-MPO was the purity of PNP5. 99mTcN-MPO was prepared >98% RCP (n = 20) using the two-vial formulation. For single-vial formulations with/without SnCl2, β-cyclodextrin (β-CD) is particularly useful as a stabilizer for PNP5. The RCP of 99mTcN-MPO was 95 – 98% using β-CD, but its RCP was only 90 – 93% with γ-CD. It seems that PNP5 fits better into the inner cavity of β-CD, which forms more stable inclusion complex than γ-CD in the single-vial formulations. The results from biodistribution and imaging studies in Sprague-Dawley (SD) rats clearly demonstrated biological equivalence of three different formulations. SPECT data suggested that high quality images could be obtained at 0 – 30 min post-injection without significant interference from the liver radioactivity. Considering the ease for 99mTc-labeling and high RCP of 99mTcN-MPO, the non-SnCl2 single-vial formulation is an attractive choice for future clinical studies.
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DOI：
10.1007/s00259-011-1877-y
发表时间：
2011-11-01
影响因子：
9.1
作者：
Fiechter, Michael;Ghadri, Jelena R.;Kaufmann, Philipp A.
通讯作者：
Kaufmann, Philipp A.
影响因子：
2.4
作者：
Hatada, Kengo;Ruiz, Mirta;Glover, David K.
通讯作者：
Glover, David K.
影响因子：
4
作者：
Liu, Shuang
通讯作者：
Liu, Shuang
影响因子：
9.3
作者：
Maddahi, Jamshid;Czernin, Johannes;Phelps, Michael
通讯作者：
Phelps, Michael
DOI：
10.1039/dt9900003729
发表时间：
1990-12-01
期刊：
JOURNAL OF THE CHEMICAL SOCIETY-DALTON TRANSACTIONS
影响因子：
--
作者：
DUATTI, A;MARCHI, A;PASQUALINI, R
通讯作者：
PASQUALINI, R