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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 poor physical properties, interference with imaging quality, and high bone uptake

Inactive Publication Date: 2011-03-30
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

Experimental program
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Effect test

example 1

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

[0078] 1. Prepare 200ml 1mol / L hydrochloric acid / ROH solution

[0079] The principle of using acetyl chloride to react violently with alcohol to produce HCl:

[0080] CH 3 COCl+ROH→CH 3 COOR+HCl

[0081] Prepare a hydrochloric acid / ROH solution with a concentration of about 1mol / L equivalent. Practice has proved that the ester impurities produced by this treatment do not participate in the reaction and are removed during the filtration treatment of the reactants, which does not affect the experiment.

[0082] 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, while stirring vigorously while dripping, mix evenly, use a wide range of pH test paper to measure the pH value between 2 and 3 between.

[0083] 2. Ligand dimercaptosuccinate (DMSR / DMSR 2 )Synthes...

example 2

[0092] This example is the preparation of a lyophilized dimercaptosuccinate kit (take the preparation of 100 as an example)

[0093] Weigh 200mg of dimercaptosuccinate DMSR / DMSR2 and dissolve in 40ml pH10.0 borax-sodium hydroxide buffer solution, add Vc10mg (5mg / ml, 2ml), and then add 20mg SnCl 2 .2H 2 In O hydrochloric acid solution (10mg / ml, 2ml), adjust the pH to 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 freeze drying for 24 hours, stoppered and sealed to obtain a freeze-dried kit. When the dimercaptosuccinate is different, the corresponding freeze-dried kit can be obtained. SnCl can be adjusted according to the output of the kit and the content requirements of the components in each kit 2 .2H 2 O. The dosage of dimercaptosuccinic acid is such that their weight ratio falls within the range of (0.1-10): (1-20).

example 3

[0095] This example is 99m Preparation of Tc-DMSMe

[0096] 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), use pH 10.0 borax-sodium hydroxide to adjust the pH between 8.4 to 8.5 in a vial, and mix about 18.5 to 185 megabeques (MBq) 99m TcO 4 - Eluent (from medical 99 Mo- 99m Tc generator) add the bottle to react at room temperature for 15 minutes, then the required 99m Tc-DMSMe

[0097] 2) Freeze-drying method: about 18.5~185 MBq (MBq) 99m TcO 4 - Eluent (from medical 99 Mo- 99m Tc generator) was added to the DMSMe kit, mixed and reacted at room temperature for 15 minutes to obtain the desired 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 <99m>Tc(V), <99m>TcN(22) and <99m>Tc(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 invention relates to a 99m Tc-labeled radioactive complex and its preparation method and application, especially its application as a 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 complex with Tc(V) core as the central core ( 99m The research of Tc(V)-DMSA) is very active. Its structure is shown in (Figure a). It is mainly used for tumor imaging. It is used in soft tissue tumors, medullary thyroid carcinoma, head and neck tumors, bone metastases and other malignant tumors. The imaging diagnosis showed high sensitivity and specificity, and it has been widely used in clinical practice. [0003] In recent years, malignant tumors, commonly referred to as cancers, have become the most serious type of diseases that endanger human health and seriously affect human health. Therefore, the research on tumor imaging drugs is one of the hotspots ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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