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Double phospho acid compound of 99mT.C. mark and preparation method

A technology of bisphosphonic acid and complex, which is applied in the fields of radiopharmaceuticals and nuclear medicine to achieve good effects

Inactive Publication Date: 2007-10-03
JIANGSU INST OF NUCLEAR MEDICINE
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Now we label 2-(1-methylimidazol-2-yl)-1-hydroxyethane-1,1-bisphosphonic acid with technetium-99m, given that its structure is similar to MIDP, but completely different (bisphosphonic acid It is connected to the 2-position of the imidazole ring), it is expected to be a promising bone imaging agent, and there are no reports at home and abroad

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  • Double phospho acid compound of 99mT.C. mark and preparation method
  • Double phospho acid compound of 99mT.C. mark and preparation method
  • Double phospho acid compound of 99mT.C. mark and preparation method

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Embodiment Construction

[0026] Technetium-99m-labeled 2-(1-methylimidazol-2-yl)-1-hydroxyethane-1,1-bisphosphonic acid complex ( 99m Tc-HMIBP) Preparation and Performance Determination

[0027] 1) 99m Preparation of Tc-HMIBP

[0028] In a 10ml vial, add 3-5 mg of 2-(1-methylimidazol-2-yl)-1-hydroxyethane-1,1-bisphosphonic acid, SnCl 2 2H 2 O hydrochloric acid solution 0.05 ~ 0.25mL (the concentration of hydrochloric acid is 0.1mol L -1 , containing 1.0g·L -1 SnCl 2 2H 2 O), after shaking well, use phosphate buffer solution (pH4.3) to adjust the pH to 4~6, add freshly rinsed pertechnetium-99m acid ( 99m TCO 4 - ) solution of 18.5 to 185 megabeq (MBq), fully mixed, placed at room temperature for 8 to 15 minutes, and the labeling is completed, and the technetium-99m labeled 2-(1-methylimidazol-2-yl )-1-hydroxyethane-1,1-bisphosphonic acid complex ( 99m Tc-HMIBP).

[0029] 2) 99m Determination of Tc-HMIBP labeling rate

[0030] The labeling rate of technetium-99m-labeled imidazole bisphosph...

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Abstract

This invention relates to a preparation method of technetium - 99m noted 2 - ( 1 - methyl glyoxaline - 2 - group) - 1 - hydroxy ethane - 1, 1 - double phosphonic acid complex, belongs to radiopharmaceuticals and nuclear medicine region. It uses ligand double phosphonic acid ( HMIBP), reducer, pH buffering agent and so on to compose drug box, then add high technetium acid ( 99mTcO4 -) solution to drug box for reaction, obtain technetium - 99m labeled 2 - ( 1 - methyl glyoxaline - 2 - group) - 1 - hydroxy ethane - 1, 1 - double phosphonic acid complex ( 99mTc - HMIBP). This technetium - 99m labeled double phosphonic acid complex used for nuclear medicine diagnose discovery or Rheumatoid and tumour treatment, and so on. The osseous tissue intake dose ( Am, bone) (%ID / g) and ( Am, bone / Am, blood) ratio of this invention is higer than literature value, illustrate that this invention has better effect as bone developer.

Description

technical field [0001] Technetium-99m labeled 2-(1-methylimidazol-2-yl)-1-hydroxyethane-1,1-bisphosphonic acid complex and its preparation method relate to the fields of radiopharmaceuticals and nuclear medicine. Background technique [0002] Bone is composed of three parts: osteocytes, glial fibers and bone matrix. Bone matrix is ​​composed of inorganic salts and organic matter. Inorganic salt accounts for about 2 / 3 of adult bone, and its main component is hydroxyapatite crystal [Ca 10 (PO 4 ) 6 (OH) 2 ], with a large surface area, similar to an ion exchange resin, which can exchange or adsorb with the corresponding ions in blood by means of ion exchange or surface adsorption. When the bone is damaged, the bone in the lesion area can undergo two changes of osteogenesis or osteolysis depending on the amount of blood supply, strong or low osteogenesis. More crystals can be deposited at the same time in the new bone formation of osteogenic injury. Imaging agents such as...

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F13/00C07F9/28A61K51/04A61K103/10
Inventor 罗世能郭雪花王洪勇谢敏浩何拥军邹霈刘娅灵
Owner JIANGSU INST OF NUCLEAR MEDICINE