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Radioactive rhenium-N-accessory ingredient of alkyl dinitrogen disulfide for curing liver cancer and preparation method

An alkyl disulfide diazepine, radioactive technology, applied in the field of preparations containing radioactive substances, can solve the problems of poor retention characteristics, poor retention performance, radiation damage to lung tissue, etc., and achieves high labeling rate and good stability. Effect

Inactive Publication Date: 2005-01-12
INST OF NUCLEAR PHYSICS & CHEM CHINA ACADEMY OF
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In 2001, Jeong J M et al. (Nucl Med Biol, 2001; 28(1): 197~204) reported the synthesis of TDD (2,2,9,9-tetramethyl-4,7-diaza-1,10-di sulfur decane), with 188 Re mark, then put 188 Re-TDD was extracted with iodized oil, and the 188 Re-TDD lipiodol solution, after perfusion through the hepatic artery of tumor-bearing mice, observed a higher concentration of hepatoma, but 188 Relatively poor retention properties of Re-TDD in liver tumors
In 2002, Lee Y S et al. (Nucl Med Comm, 2002; 23:237~242) synthesized a series of derivatives with long-chain alkanes on the nitrogen atom of TDD (especially HDD (n-hexadecyl-TDD) with relatively good biochemical properties), and 188 The iodized oil solution in which Re forms the complex improves its uptake performance and retention characteristics in liver tumors, but the presence of long-chain alkane substituents greatly improves the uptake performance of the complex in lung tissue due to the blocking effect of capillaries and retention characteristics, may cause certain radiation damage to normal lung tissue
The disadvantage is that rhenium nuclide-labeled iodized oil sol preparation has poor stability in vivo, and the uptake and retention performance of the sol preparation in the liver tumor area is relatively poor

Method used

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  • Radioactive rhenium-N-accessory ingredient of alkyl dinitrogen disulfide for curing liver cancer and preparation method
  • Radioactive rhenium-N-accessory ingredient of alkyl dinitrogen disulfide for curing liver cancer and preparation method
  • Radioactive rhenium-N-accessory ingredient of alkyl dinitrogen disulfide for curing liver cancer and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Prepare high-labeled 188 Re-NEPTDD

[0053] Add ligand NEPTDD 10.0mg, sodium gluconate 200.0mg into a 10ml reaction tube, fill with nitrogen gas protection, add SnCl 2 15.0 mg of nitrogen-saturated reducing agent solution, carrier rhenium 1.0 mg and 1 mCi 188 Re (in ReO 4 - form, the same below). Adjust the pH of the reaction system to 3.5-4.0, and react the reaction tube in a water bath at 50°C for 15 minutes. The labeling rate of the prepared marker was 81% when analyzed by radioactive paper chromatography. Its development system is two, namely acetone and saline, in the acetone system, ReO 4 - R f 0.7~0.9, the R of colloidal rhenium f 0.0~0.1, the R of the marker f is 0.0~0.1; in normal saline system, ReO 4 - R f 0.7~0.9, the R of colloidal rhenium f 0.0~0.1, the R of the marker f 0.7 to 0.9, the same below.

Embodiment 2

[0055] Prepare high-labeled 188 Re-NEPTDD

[0056] Add 20.0mg of ligand NEPTDD and 400.0mg of sodium gluconate into a 10ml reaction tube, fill with argon for protection, add SnCl-containing 2 40.0 mg of nitrogen-saturated reducing agent solution, 2.0 mg of rhenium carrier and 100 mCi 188 Re. Adjust the pH of the reaction system to 3.5-4.0, and react the reaction tube in a water bath at 70°C for 30 minutes. The labeling rate of the prepared marker was 79% when analyzed by radioactive paper chromatography.

[0057] figure 1 Prepared for Example 2 188 Whole-body SPECT imaging of Re-NEPTDD lipiodol solution in rabbits after hepatic artery perfusion for 1 hour. Depend on figure 1 It can be seen that the liver imaging of the white rabbit is relatively clear, indicating that the complex has ideal uptake and retention in the liver; the kidney and bladder of the white rabbit are slightly imaging, indicating that the complex is mainly metabolized by the kidney; other organs of th...

Embodiment 3

[0059] Prepare high-labeled 188 Re-NEPTDD

[0060] Add ligand NEPTDD 15.0mg, sodium tartrate 400.0mg in a 10ml reaction tube, fill with helium gas protection, add SnCl 2 15.0 mg of nitrogen-saturated reducing agent solution, carrier rhenium 2.0 mg and 10 mCi 188 Re. Adjust the pH of the reaction system to 3.5-4.0, and react the reaction tube in a water bath at 70°C for 45 minutes. The labeling rate of the prepared marker was 83% when analyzed by radioactive paper chromatography.

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Abstract

In this invention process, reaction ligand, protector, radiorhenium, and reducing agent are added into reactor, regulating pH value in the reaction system, under suitable reaction temp. Finally, the reaction product is extracted by iodized oil to obtain radiorhenium-N-alkyldithiodiaza type coordination compound for treating hepatoma by perfusion of iodized oil and said compound solution into hepatic artery, with higher marking rate and high stability.

Description

1. Technical field [0001] The invention belongs to the field of preparations containing radioactive substances used for treatment or in vivo tests, and specifically relates to medical radioactive rhenium-N-alkyl disulfide complexes and a preparation method thereof which can be used for liver cancer treatment. 2. Background technology [0002] The treatment methods for liver cancer include surgery, chemotherapy and radiotherapy. Surgery is only effective for early stage patients; systemic chemotherapy is not suitable for most liver cancer patients due to its unsatisfactory effect and relatively large side effects. [0003] Normal liver cells are mainly supplied by the portal vein, while the blood supply of liver cancer cells is mainly completed by the hepatic artery. Therefore, many embolic agents concentrate in HCC cells through hepatic artery infusion. [0004] Iodized oil is highly fat-soluble and viscous, and is easy to concentrate at the site of liver cancer. Many rese...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/00A61P35/00C07D211/26C07F13/00
Inventor 王文进罗顺忠刘国平何佳恒杨玉青王关全邴文增魏洪源蒋树斌蒲满飞
Owner INST OF NUCLEAR PHYSICS & CHEM CHINA ACADEMY OF
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