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Diphospho-acid complex of radiative technetium-99m marked oxazole phosphinic acid

A technology of complexes and bisphosphonates, applied in the fields of radiopharmaceuticals and nuclear medicine, can solve problems such as no reports, and achieve good results

Inactive Publication Date: 2005-10-12
JIANGSU INST OF NUCLEAR MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But with technetium-99m ( 99m Tc) labeled zoled

Method used

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  • Diphospho-acid complex of radiative technetium-99m marked oxazole phosphinic acid
  • Diphospho-acid complex of radiative technetium-99m marked oxazole phosphinic acid
  • Diphospho-acid complex of radiative technetium-99m marked oxazole phosphinic acid

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Experimental program
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Effect test

Embodiment 1

[0028] Technetium-99m zoledronic acid complex ( 99m Tc-ZL) Preparation and Performance Determination

[0029] 1) Preparation of technetium-99m zoledronic acid complex

[0030] In a 10ml vial, add 3-5mg of zoledronic acid, SnCl 2 2H 2 O hydrochloric acid solution 0,05 ~ 0.2mL (the concentration of hydrochloric acid is 1mol L -1 , containing 2.5g·L -1 SnCl 2 2H 2 O), after shaking well, use phosphate buffer solution (pH8.0) to adjust the pH to 5-7, add freshly rinsed pertechnetium-99m acid ( 99m TCO4 - ) solution of 18.5 to 185 megabeq (MBq), fully mixed, placed at room temperature for 5 to 10 minutes, and the labeling is completed, the technetium-99m labeled zoledronic acid complex of the present invention ( 99m Tc-ZL).

[0031] 2) Determination of labeling rate of technetium-99m zoledronic acid complex

[0032] The labeling rate of the technetium-99m zoledronic acid complex refers to the percentage of the radioactivity of the technetium-99m zoledronic acid complex in...

Embodiment 2

[0038] Technetium-99m-labeled 2-(2-methylimidazol-1-yl)-1-hydroxyethane-1,1-diphosphonic acid complex ( 99m Tc-MZL) Preparation and Performance Determination

[0039] 1) 99m Preparation of Tc-MZL

[0040] In a 10ml vial, add 3-5 mg of 2-(2-methylimidazol-1-yl)-1-hydroxyethane-1,1-diphosphonic acid, SnCl 2 2H 2 O hydrochloric acid solution 0.05 ~ 0.2mL (the concentration of hydrochloric acid is 1mol L -1 , containing 2.5g·L -1 SnCl 2 2H 2 O), after shaking well, use phosphate buffer solution (pH8.0) to adjust the pH to 5-7, add freshly rinsed pertechnetium-99m acid ( 99m TCO 4 - ) solution of 18.5 to 185 megabeq (MBq), fully mixed, and placed at room temperature for 5 to 10 minutes to obtain the technetium-99m labeled 2-(2-methylimidazol-1-yl)-1 -Hydroxyethane-1,1-diphosphonic acid complex (99mTc-MZL).

[0041] 2) 99m Determination of Tc-MZL labeling rate

[0042] Adopt HPLC method to measure: adopt U.S. Varian 5000 type HPLC instrument, chromatographic column is C...

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Abstract

Diphosphate complex of ZL phosphonic acid with radioactive technetium-99m mark and its production are disclosed. Diphosphate of ZL phosphonic acid is 2-(imidazole-1-radical)-1-hydroxyl ethane-1, 1-di-(2-ethylhexyl)phosphoric acid ZL phosphonic acid , ZL), 2-(2-methyl imidazole-1-radical)-1-hydroxyl ethane-1, and 1-diphosphate(MZL). It is carried out by combining diphosphate(ZL or MZL) of ligand ZL phosphonic acid and reducer with pH buffering agent to be medicine pack, adding pertechnetate(99mTcO4-) solution into medicine pack, reacting, and obtaining diphosphate complex 99mTc-ZL or 99mTc-MZL of ZL phosphonic acid with radioactive technetium-99m mark. It can be used for nuclear medical diagnostic image or treat rheumatoid disease and tumor.

Description

technical field [0001] The bisphosphonic acid complex of radioactive technetium-99m labeled zoledronic acid and its preparation method relate to the fields of radiopharmaceuticals and nuclear medicine. Background technique [0002] The main inorganic salt component of bone is hydroxyapatite crystal, which has a structure similar to ion exchange column and has a large surface area. It obtains phosphate and other elements from blood through chemical adsorption and ion exchange to complete metabolic renewal. Radiopharmaceuticals such as technetium-99m[ 99m Tc]-phosphonate is quickly adsorbed and deposited on the surface of hydroxyapatite crystals in bones after intravenous injection, which specifically shows the metabolism of bones. When there are local bone lesions, such as inflammation, tumor, fracture, etc. causing changes in local blood flow and / or bone inorganic salt metabolism, abnormally increased radioactivity will be displayed in the corresponding parts. These abnorma...

Claims

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Application Information

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IPC IPC(8): A61K51/00A61P19/02A61P29/00A61P35/00C07F9/6503C07F13/00
Inventor 罗世能王洪勇谢敏浩何拥军邹霈刘娅灵刘晓亚
Owner JIANGSU INST OF NUCLEAR MEDICINE
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