Technetium-99m signed dimercaptosuccinate complexes, preparing method and application thereof

A technology of dimercaptosuccinate and dimercaptosuccinic acid is applied in the application field as a tumor imaging agent, and can solve the problems of lack of specificity, poor physical properties and high bone uptake

Inactive Publication Date: 2007-12-12
BEIJING NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Its shortcomings are: ① lack of specificity (the inflammatory lesion is also positive); ② poor physical properties, the energy range of the emitted gamma rays (93-394 kiloelectron volts) is too wide; ③ 67 Ga-gallium citrate is excreted by the intestinal tract, which interferes with the imaging quality; ④ It takes a long time to wait for imaging after intravenous injection (48-72 hours)
[0011] It can be seen that the existing relatively successful soft tissue tumor imaging agents 99m Tc(V)-DMSA still has the disadvantage of interference caused by high bone uptake. If we can provide a tumor imaging agent that can be better taken up by soft tissue tumors, has higher sensitivity, lower bone uptake, and clearer contrast , will have broad application prospects

Method used

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  • Technetium-99m signed dimercaptosuccinate complexes, preparing method and application thereof
  • Technetium-99m signed dimercaptosuccinate complexes, preparing method and application thereof
  • Technetium-99m signed dimercaptosuccinate complexes, preparing method and application thereof

Examples

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example 1

[0077] This example is ligand dimercaptosuccinate (DMSR / DMSR 2 ) preparation

[0078] 1. The principle of preparing 200ml 1mol / L hydrochloric acid / ROH solution and using the violent reaction of acetyl chloride and alcohol to produce HCl:

[0079] CH 3 COCl+ROH→CH 3 COOR+HCl

[0080] Prepare a hydrochloric acid / ROH solution with a concentration of about 1 mol / L equivalent. Practice has proved that the ester impurities produced by this treatment do not participate in the reaction and are removed when the reactant is filtered, which does not affect the experiment.

[0081] with hydrochloric acid / methanol (CH 3 OH) solution as an example, after calculation: absorb about 16ml of redistilled acetyl chloride and slowly add it dropwise to 200ml of chromatographic grade methanol. between.

[0082] 2. Ligand dimercaptosuccinate (DMSR / DMSR 2 )Synthesis

[0083] Add 8.017gmeso-DMSA to the newly prepared 200ml 1mol / L equivalent hydrochloric acid / ROH solution, stir vigorously and h...

example 2

[0090] This example is the preparation of dimercaptosuccinate freeze-dried kit (take the preparation of 100 as an example)

[0091] Weigh dimercaptosuccinate DMSR / DMSR2 200mg and dissolve in 40ml pH10.0 borax-sodium hydroxide buffer solution, add Vc10mg (5mg / ml, 2ml), then add 20mg SnCl 2 .2H 2 In the hydrochloric acid solution of O (10 mg / ml, 2 ml), adjust the pH between 8.4 and 8.5 with pH 10.0 borax-sodium hydroxide. After aseptic filtration, it is divided into 100 penicillin vials, then placed in a freeze dryer for 24 hours, and then sealed with a stopper to obtain a freeze-dried medicine box. When the dimercaptosuccinates are different, corresponding lyophilized kits can be obtained. SnCl can be adjusted according to the output of the kit and the requirements for the content of the components in each kit 2 .2H 2 O, the consumption of dimercaptosuccinic acid, make their weight ratio fall in (0.1~10): (1~20) scope.

example 3

[0093] This example is 90m Preparation of Tc-DMSMe

[0094] 1) Wet method: add 0.2mg SnCl to 0.5ml DMSMe solution (4.0g / L) 2 .2H 2 O hydrochloric acid solution (10mg / ml, 0.1ml), with pH 10.0 borax-sodium hydroxide to adjust the pH in the vial between 8.4 to 8.5, about 18.5 to 185 megabecquerel (MBq) 99m TCO 4 - Wash solution (from medical 99 Mo- 99m Tc generator obtains) adds this bottle room temperature reaction 15 minutes, promptly obtains required 99m Tc-DMSMe

[0095] 2) Freeze-drying method: about 18.5-185 megabecco (MBq) 99m TCO 4 - Wash solution (from medical 99 Mo- 99m Tc generator (obtained) was added in the DMSMe kit, after mixing, it was reacted at room temperature for 15 minutes to obtain the required 99m Tc-DMSMe complex.

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Abstract

The invention relates to a kind of dimercaptosuccinate complex marked by technetium- 99m, the preparation method and its application. It is characterized in that it takes 99mTc(V), 99mTcN(22) and 99mTc(I)(CO)3 as central nuclear, the dimercaptosuccinate ligand is represented by DMSR / DMSR2, the R is alkyl or cyclohexyl with carbon number from 1 to 5. Said complex is prepared with wet or freeze- dried method, and is used as imaging agent for tumor. The advantages includes simple preparation, low price and high target / non target ratio.

Description

technical field [0001] The present invention relates to a 99m Tc-labeled radioactive complex and its preparation method and application, especially its application as tumor imaging agent. Background technique [0002] Now I am at 99m In the field of Tc-labeled radiopharmaceutical chemistry, in recent years 99m Dimercaptosuccinic acid complexes with Tc(V) core as the central core ( 99m The research of Tc(V)-DMSA) is very active. Its structural formula is shown in (Figure a). It is mainly used for tumor imaging. It has shown high sensitivity and specificity in imaging diagnosis and has been widely used in clinic. [0003] In recent years, malignant tumors, usually called cancer, have become the most serious disease that endangers human health and seriously affects human health. Therefore, the research on tumor imaging drugs is one of the hot spots in radiopharmaceutical research today. In terms of imaging, due to 99m Tc has excellent nuclear properties such as short half...

Claims

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Application Information

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IPC IPC(8): C07F13/00A61K51/00A61K103/10C07C323/52
Inventor 王学斌易鹏张现忠张俊波陆洁唐志刚杨树业
Owner BEIJING NORMAL UNIVERSITY
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