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A preparation method of memantine bi-sulfur bi-nitrogen derivates medicinal box marking by technetium

A technology of dimethyladamantaneaminoacetamide and kits, applied in the field of radiopharmaceutical labeling, to achieve good stability

Inactive Publication Date: 2008-04-09
JIANGSU INST OF NUCLEAR MEDICINE
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] At present, foreign literature reports are all using 18 F. 123 I or 11 C-labeled NMDA receptor antagonists are used to study changes in psychiatric disease receptors. 99m Report of Tc-labeled NMDA receptor

Method used

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  • A preparation method of memantine bi-sulfur bi-nitrogen derivates medicinal box marking by technetium
  • A preparation method of memantine bi-sulfur bi-nitrogen derivates medicinal box marking by technetium
  • A preparation method of memantine bi-sulfur bi-nitrogen derivates medicinal box marking by technetium

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Effect of pH change on labeling rate. Remove the buffer (Na 2 HPO 4 and KH 2 PO 4 ) to the newly prepared buffer solutions with different pH values ​​(1-12), and then added Na 99m TCO 4 After the labeling was completed, the labeling rate was determined by TLC and HPLC. When the pH is between 4.0-7.0, the labeling rate is stable and >95%. see picture 1.

Embodiment 2

[0030] The effect of the content of each component in the kit on the labeling rate. Keep the content of other components unchanged, and change the NCAM and SnF in the kit respectively 2 ,, the content of EDTA and GH, and the labeling rate was measured after labeling. The labeling rate of GH is greater than 95% between 2-20mg; the labeling rate of EDTA is greater than 95% between 0.2-4.0mg; the labeling rate of stannous is greater than 95% between 5-200μg; the labeling rate of NCAM is between 20-200μg Greater than 95%. See Figure 2-5.

Embodiment 3

[0032] Stability test

[0033] The labeled reaction solution was placed at room temperature for 1, 2, 3, 4, 5, and 6 hours to measure the labeling rate respectively, and the labeling rate was still greater than 90% after 6 hours.

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Abstract

The invention relates to a preparation method of a technetium-labeled memantine amine disulfide dinitrogen derivative medicine box, and belongs to the radio pharmaceutical-labeled technical field. In particular, the invention relates to a<99M> Tc-N-[2-(N-(2-ethyl sulfhydryl)) amino acetyl-(2-ethyl sulfhydryl)-3, 5-dimethyl memantine alkane amino acetamide medicine box, and the preparation method of a<99M> Tc-NCAM medicine box for short. The N-[2-(N-(2-ethyl sulfhydryl)) amino acetyl-(2-ethyl sulfhydryl)-3 and the 5-dimethyl memantine alkane amino acetamide (NCAM) are taken as the raw materials, auxiliary materials of sodium glucoheptonate, ethylene diamine tetraacetic acid, SnF2, etc. are utilized to prepare the NCAM medicine box, 50 to 1000MBq Na<99M> TcO4 solution which is newly leached is added to operate a <99M> Tc lable, so as to prepare the <99M> Tc- NCAM medicine box. The content of each component in the medicine box is in the following range: NCAM is of 20 to 200 microgram, SnF2 is of 5 to 200 microgram, the ethylene diamine tetraacetic acid is of 0.2 to 4.0 mg, the sodium glucoheptonate is of 2 to 20 mg, and the pH value is of 4.0 to 7.0. The labeling rate of the prepared medicine box is more than 90 percent, and the stability is good.

Description

technical field [0001] The present invention relates to 99m The preparation method of Tc-N-[2-(N-(2-mercaptoethyl))aminoacetyl]-N-(2-mercaptoethyl)-3,5-dimethyladamantyl aminoacetamide kit , belongs to the technical field of radiopharmaceutical labeling. Background technique [0002] 99m Tc-N-acetyl-Amantadine ( 99m Tc-NCAM) is designed to connect disulfide diazepam ligand at the amino position of memantine, and use it to form a stable complex with technetium ( 99m Tc-NCAM), the complex has no registration number on CA, and there is no relevant report at home and abroad. [0003] 99m Tc-NCAM is electrically neutral, logP1.8, (the size of the lipid-water partition coefficient P determines whether it can penetrate the blood-brain barrier BBB, when logP<0.5, it is difficult for drugs to pass through the BBB, logP should be between 0.5 and 2 Only when the drug penetrates the BBB better), the molecular weight is 413 (the relative molecular weight of the drug determines w...

Claims

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Application Information

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IPC IPC(8): A61K51/04A61K103/10
Inventor 周杏琴张建康徐希杰邹美芬钦晓峰张荣军曹国宪罗世能
Owner JIANGSU INST OF NUCLEAR MEDICINE
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