Preparation method of 131I-labeled metaiodobenzylguanidine

A technology of m-iodobenzylguanidine and benzylguanidine, which is applied in the field of preparation of m-iodobenzylguanidine, can solve the problems of high transport requirements of radioactive substances, impossibility of clinical application, harsh reaction, etc., and achieve good clinical diagnosis and treatment effect and high radiochemical purity , the effect of mild and simple conditions

Inactive Publication Date: 2016-12-07
JIANGSU INST OF NUCLEAR MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Hunter reported the use of solid-phase synthesis to prepare carrier-free 131 I-m-iodobenzylguanidine, this method is simple to separate, and the obtained product has high purity and few impurities, but the resin is required to reach the grade for injection, and the reaction is almost harsh. It is only found in laboratory preparation and literature reports, and cannot be put into actual production.
Some are prepared by substituting tin precursor compounds 131 I-m-iodobenzylguanidine brings tin and other toxic impurities, which are difficult to remove and cannot be used clinically
[0004] All current technologies 131 I-m-iodobenzylguanidine is prepared in factories or laboratories and then transported to hospitals for clinical use. On the one hand, the transportation requirements of radioactive substances are high and the cost is high; In loss, the longer the time, the greater the loss

Method used

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  • Preparation method of 131I-labeled metaiodobenzylguanidine
  • Preparation method of 131I-labeled metaiodobenzylguanidine
  • Preparation method of 131I-labeled metaiodobenzylguanidine

Examples

Experimental program
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Effect test

Embodiment 1

[0038] Embodiment 1: Add N,N'-di(tert-butoxycarbonyl)-3-(tributyltin base)-benzylguanidine 70 μ g successively in 10 ml control vial, 500 μ l of acetic acid, 16.5 μ l of 30% hydrogen peroxide solution, Na 131 I solution 13.5mCi (0.1ml), physiological saline 1ml, react at room temperature for 20 minutes. Add 100 μl of trifluoroacetic acid and heat to 100° C. for 20 minutes. After the reaction was completed, let it stand still, cooled to room temperature, added 1 g of 717 anion exchange resin, and stirred gently for 2 minutes. Aspirate the supernatant and filter it through a 0.22 μm microporous membrane to obtain the marker 131 I-m-iodobenzylguanidine.

Embodiment 2

[0039] Embodiment 2: Add N,N'-di(tert-butoxycarbonyl)-3-(tributyltin base)-benzylguanidine 70 μ g successively in 10 ml control vial, 500 μ l of acetic acid, 16.5 μ l of 30% hydrogen peroxide solution, Na 131 I solution 13.5mCi (0.1ml), physiological saline 1ml, react at room temperature for 20 minutes. Add 100 μl of trifluoroacetic acid and heat to 100° C. for 20 minutes. After the reaction, let it stand still, cool to room temperature, draw out the reaction solution with a syringe, inject it into a self-made small disposable 717 anion exchange resin packed column, and then elute with 1ml of normal saline. Combine the solutions and filter them with a needle filter with a 0.22 μm filter membrane to obtain the marker 131 I-m-iodobenzylguanidine.

Embodiment 3

[0040] Example 3: 70 μg of N,N'-bis(tert-butoxycarbonyl)-3-(tributyltin-yl)-benzylguanidine, 25 μg of N-chlorosuccinimide, and dihydrogen phosphate were sequentially added to a 10ml control vial Potassium 3.4mg, Sodium Hydroxide 0.3mg, Na 131 I solution 13.5mCi (0.1ml), physiological saline 1.5ml, react at room temperature for 20 minutes. Add 40 μg of sodium metabisulfite, and heat to 100° C. for 20 minutes to react. After the reaction was completed, let it stand still, cooled to room temperature, added 1 g of 717 anion exchange resin, and stirred gently for 2 minutes. Aspirate the supernatant and filter it through a 0.22 μm microporous membrane to obtain the marker 131 I-m-iodobenzylguanidine.

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Abstract

The invention relates to a method for preparing 131I-metaiodobenzylguanidine with high radioactive specific activity and without a carrier. The method comprises the following steps: performing normal-temperature reaction on a labeled precursor N,N'-di(t-butyloxycarboryl)-3-(tributyltin)-bethanidine, a buffer solution, an oxidizing agent and Na131I for 20 minutes, and adding a reducing agent and heating to 100 DEG C to react for 20 minutes; standing after the reaction is finished, cooling to room temperature, adding anion exchange resin and lightly stirring for 2 minutes; absorbing supernate and passing through a microfiltration membrane to obtain the product. The 131I-metaiodobenzylguanidine, prepared by using hydrogen peroxide--trifluoroacetic acid or N-chlorosuccinimide--sodium pyrosulfite as the oxidizing agent and the reducing agent, has high radiochemical purity and high radioactive specific activity. Reaction byproducts are removed from the 131I-metaiodobenzylguanidine solution after anion exchange resin treatment and microfiltration membrane filtration, and the tin amount is reduced to trace amount, so the 131I-labeled metaiodobenzylguanidine is suitable for clinical diagnosis and treatment. The condition of the labeling reaction is mild and simple, so preparation can be finished in a hospital, and high cost and decay loss of medicines caused by transportation are avoided.

Description

technical field [0001] The invention relates to the field of radiopharmaceuticals, in particular to a 131 Preparation method of I-labeled m-iodobenzylguanidine. Background technique [0002] 131 I is an ideal radionuclide used in diagnosis and treatment. It can release γ-rays and β-rays at the same time, and its physical half-life is 8.04d. m-iodobenzylguanidine is a guanidinium derivative, similar in structure to norepinephrine, and they are all benzene rings with substituents in the meta position. m-iodobenzylguanidine has a more polar guanidinium group, mainly Iodine substitution produces different pharmacological effects. Since adrenal cells need to ingest guanidine ethyl guanidine to biosynthesize catecholamines, m-iodobenzylguanidine has adrenal-targeting properties. When there are highly selective lesions (pheochromocytoma) or hyperplasia (abnormal proliferation of tumor cells) in the adrenal medulla, radioisotope 131 I-labeled m-iodobenzylguanidine is easy to en...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C277/08C07C279/06
CPCC07C277/08C07B2200/05
Inventor 陈志明王刚谢敏浩杨红
Owner JIANGSU INST OF NUCLEAR MEDICINE
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