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Iodogen method for preparation of hypericin radioactive iodine marker

A technology of radioactive iodine and hypericin, which is applied in the preparation of organic compounds, quinone preparation, chemical instruments and methods, etc., can solve the problems of unsatisfactory labeling rate, cumbersome preparation process, long cycle, etc., and achieve low cost , The preparation process is simple, the effect of short time

Active Publication Date: 2009-07-08
南京成至诚医药科技有限公司
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Problems solved by technology

As a result, the preparation process is very cumbersome, and the cycle is long, the cost is high, and the marking rate is not satisfactory.

Method used

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  • Iodogen method for preparation of hypericin radioactive iodine marker

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preparation example Construction

[0033] 所述Iodogen涂管的制备:配制浓度为1mg / ml Iodogen / 二氯甲烷溶液,将溶液定量地加入玻璃或塑料试管中,用氮气将二氯甲烷吹干,即制得Iodogen涂管,涂管于4摄氏度冰箱保存。

[0034] 所述加入的新鲜配制的Iodogen DMSO溶液浓度为2mg / ml。

Embodiment 1

[0036] 本专利提出的标记路线,使用的氧化剂是1,3,4,6-Tetrachloro-3α,6α-Diphenylglycouril(商品名:Iodogen),标记率可达99%以上,反应液可直接使用。

[0037] 具体的标记路径如下:

[0038] A:

[0039] 1.在碘-131溶液(50μl,12mCi,溶于0.1N NaOH水溶液中)中加入酸性溶液(0.1N HCl,50μl),再加入金丝桃素DMSO溶液(2mg / ml,400μl)。

[0040] 2.混合液中加入新鲜配制的Iodogen DMSO(2mg / ml,200μl)溶液。

[0041] 3.室温下反应10分钟。

[0042] 4.取样进行纸层析(新华1号滤纸,0.1N HCl为展开剂,展开后,标记金丝桃素位于原点,游离放射性碘位于前沿)。

[0043] 5.用伽玛计数器测定的标记率为99.4%。

[0044] B:

[0045] 1.在碘-131溶液(10μl,1mCi,水溶液)中加入金丝桃素DMSO溶液(1mg / ml,60μl)。

[0046] 2.将混合液移入Iodogen涂管(含Iodogen 20ug)

[0047] 3.室温下反应10分钟。

[0048] 4.取样进行纸层析(新华1号滤纸,0.1N HCl为展开剂,展开后,标记金丝桃素位于原点,游离放射性碘位于前沿)。

[0049] 5.用伽玛计数器测定的标记率为99.3%。

[0050] 本标记过程已进行了几十次,平均标记率为99.4±0.4%,n=29。

[0051] Iodogen涂管的制备:配制1mg / ml Iodogen / 二氯甲烷溶液,将溶液定量地加入玻璃或塑料试管中,用氮气将二氯甲烷吹干,即制得Iodogen涂管。涂管于4度冰箱保存,可长期备用(至少一年)。

[0052] Since each nuclide of the isotope has the same chemical properties, the labeling process and obtained labeling rate of iodine-131 can be applied to iodine-123, iodine-124, and ...

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Abstract

The invention discloses an Iodogen method in the process of preparing a hypericin radioiodinated labelled substance, which can effectively improve the labeling rate, and has the advantages of simple preparation method and low cost. The method comprises the following steps: 1) mixing DMSO (Dimethyl sulfoxide) solution of the hypericin with a radioiodinated aqueous solution with pH value of between 6.5 and 7.5, and taking no hypericin precipitation as the condition of meeting requirement after being mixed; and adding the radioiodinated aqueous solution according to the required radioactivity amount during mixing; 2) adding an oxidant 1,3,4,6-Tetrachloro-3alpha,6alpha-Diphenylglycouril(trade-name: Iodogen) into the mixed solution, wherein the dosage of the oxidant meets the requirement of an excessive reaction according to the radioactive iodine; 3) reacting the prepared mixed solution at room temperature for 2 to 10 minutes; and 4) sampling and subjecting the reacted solution to measurement of the labeling rate.

Description

technical field [0001] 本发明涉及一种金丝桃素放射性碘标记物制备过程中的Iodogen法。 Background technique [0002] 金丝桃素(hypericin)是一种植物提取物,现在已有人工合成方法,目前在治疗抑郁症及抗病毒等方面有所应用。金丝桃素放射性碘标记物是以放射性碘取代金丝桃素上的氢而形成的放射性碘标记物,有可能用于肿瘤,心肌梗塞等疾病的诊断和治疗(国外已有相关专利)。金丝桃素放射性碘标记物制备过程中,涉及到氧化剂的使用。在已有的使用过氧乙酸作为氧化剂的报告中,标记率只有60%左右(见参考文献:Sang Wook Kim,Jeong Hoon Park,Seung DaeYang,Min Goo Hur,Chang Woon Choi,and Kook Hyun Yu,Bull.Korean Chem.Soc.2008,Vol.29,No.102023),标记物使用前必须经过纯化。由此造成制备过程非常繁琐,而且周期长,费用高,标记率也无法让人满意。 Contents of the invention [0003] 本发明的目的就是为了解决上述问题,提供一种可有效提高标记率,且制备方法简便,费用较低的金丝桃素放射性碘标记物制备过程中的Iodogen法。 [0004] To achieve the above object, the present invention adopts the following technical solutions: [0005] 一种金丝桃素放射性碘标记物制备过程中的Iodogen法, [0006] 1)将金丝桃素DMSO(Dimethyl sulfoxide)溶液与pH值为6.5-7.5的放射性碘水溶液混合,混合后以无金丝桃素析出为满足要求;金丝桃素DMSO溶液与放射性碘水溶液的量均按制备标记物所需的量加入。(由于该标记物的最大比活度为2.5*10 10 mCi / mg,而实际应用中不可能使用这么大的比活度,所以在标记过程中金丝桃素总是过量的。 ) [0007] 2)在混合液中加入商品名为Iodogen的氧化剂1,3,4,6-Tetrachloro-3α,6α-Diphenylglycouril,其用量根据放射性碘确定并满足过量...

Claims

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Application Information

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IPC IPC(8): C07C50/36C07C46/00
Inventor 孙自平倪以成
Owner 南京成至诚医药科技有限公司
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