A container closure system that allows for greater recovery of radiolabeled peptide compared to the standard borosilicate glass system
A container closure system that allows for greater recovery of radiolabeled peptide compared to the standard borosilicate glass system
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DOI：
10.1016/j.apradiso.2013.06.019
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发表时间：
2013-10-01
影响因子：
1.6
通讯作者：
Mahmood, Umar
中科院分区：
文献类型：
--
作者：
Leece, Alicia K.;Heidari, Pedram;Mahmood, Umar
目的：通常用于合成放射性药物PET示踪剂的肽是亲脂性的，并且粘附在容器封闭系统（CCS）的壁上，因此在合成发生后，昂贵的肽和产物不能完全回收。本研究比较了标准的美国药典（USP） I型硼硅酸盐玻璃CCS和环聚烯烃共聚物晶体顶顶（CZ） CCS，标记后反应瓶中Ga-68-氯和Ga-68- dotatoc （[Ga-68] Ga-DOTA-D-Phe1-Tyr3-octreotide）的保留率。方法：采用ga -68-氯、2 M HEPES（4-（2-羟乙基）哌嗪-l-乙磺酸）或0.75 M乙酸钠、1-30 μ g DOTATOC加入CZ或玻璃CCS中进行DOTATOC的镓标记。将反应混合物加热15分钟后冷却至室温。然后通过注射器取出粗反应混合物，进行最后的处理。然后使用剂量校准器对CCS进行检测，以确定Ga-68-DOTATOC的残留量。采用非配对学生t检验评估统计学显著性。结果：在不同多肽用量和不同缓冲体系的所有实验中（n=72）， CZ CCS保持的活性低于玻璃CCS。使用2 M HEPES和15 μ g或30 μ g的DOTATOC， CZ CCS与玻璃CCS相比保留了约10%的标记DOTATOC （p < 0.05）。使用醋酸钠或HEPES缓冲系统和15 μ g或30 μ g的DOTATOC， CZ CCS比玻璃CCS保留了大约2.5%的总反应活性（p < 0.05）。在相同的反应条件下，玻璃和CZ CCS的产率相当。CZ和玻璃小瓶均未显示ga -68-氯的残留。结论：对于涉及肽标记的应用，如Ga-68-DOTATOC，与玻璃CCS相比，CZ CCS可以提高产品的回收率。(C) 2013 Elsevier Ltd.版权所有。
Objectives: Often peptides used in synthesis of radiopharmaceutical PET tracers are lipophilic and adhere to the walls of container closure systems (CCS) such that costly peptide and product are not fully recoverable after synthesis occurs. This investigation compares a standard United States Pharmacopeia (USP) Type I borosilicate glass CCS to a cyclic polyolefin copolymer Crystal Zenith (CZ) CCS, for Ga-68-chloride and Ga-68-DOTATOC ([Ga-68] Ga-DOTA-D-Phe1-Tyr3-octreotide) retention in the reaction vial after labeling.Methods: (68)Gallium labeling of DOTATOC was conducted by adding Ga-68-chloride, 2 M HEPES (4-(2-hydroxyethyl)piperazine-l-ethanesulfonic acid) or 0.75 M sodium acetate, and 1-30 mu g of DOTATOC into the CZ or glass CCS. The reaction mixture was heated for 15 min and cooled to room temperature. The crude reaction mixture was then withdrawn via syringe, for final processing. The CCS was then assayed using a dose calibrator to determine the amount of retained Ga-68-DOTATOC. Statistical significance was assessed using an unpaired Students t-test.Results: In all experiments (n=72) with various amounts of peptide and different buffering systems, the CZ CCS retained less activity than the glass CCS. Using 2 M HEPES and 15 mu g or 30 mu g of DOTATOC, the CZ CCS retained approximately 10% less of the labeled DOTATOC compared to the glass CCS (p < 0.05). Utilizing either a sodium acetate or a HEPES buffering system with 15 mu g or 30 mu g of DOTATOC, the CZ CCS retained approximately 2.5% less of the total reaction activity compared to the glass CCS (p < 0.05). Product yield was equivalent in glass and CZ CCS under the same reaction conditions. Both the CZ and glass vials showed no retention of Ga-68-chloride.Conclusion: For applications involving the labeling of peptides such as Ga-68-DOTATOC, the CZ CCS compared to the glass CCS, results in an improved recovery of product. (C) 2013 Elsevier Ltd. All rights reserved.