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

An alkyl disulfide type, 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 achieve high labeling rate and good stability Effect

Inactive Publication Date: 2007-08-08
INST OF NUCLEAR PHYSICS & CHEM CHINA ACADEMY OF
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] In 2001, Jeong JM et al. (Nucl Med Biol, 2001; 28(1): 197-204) reported the synthesis of TDD (2,2,9,9-tetramethyl-4,7-diazo-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 YS et al. (Nucl Med Comm, 2002; 23:237~242) synthesized a series of derivatives with long-chain alkanes on the TDD nitrogen atom (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

[0049] Prepare high-labeled 188 Re-NEPTDD

[0050] In a 10ml reaction tube, add ligand NEPTDD10.0mg, sodium gluconate 200.0mg, fill with nitrogen, 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 - The Rf of rhenium is 0.7-0.9, the Rf of colloidal rhenium is 0.0-0.1, and the Rf of the marker is 0.0-0.1; in the normal saline system, ReO 4 - R f is 0.7-0.9, the Rf of colloidal rhenium is 0.0-0.1, and the Rf of the marker f 0.7 to 0.9, the same below.

Embodiment 2

[0052] Prepare high-labeled 188 Re-NEPTDD

[0053] In a 10ml reaction tube, add ligand NEPTDD 20.0mg, sodium gluconate 400.0mg, fill with argon for protection, add SnCl 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.

[0054] Fig. 1 is that embodiment 2 prepares 188 Whole-body SPECT imaging of Re-NEPTDD lipiodol solution in rabbits after hepatic artery perfusion for 1 hour. It can be seen from Figure 1 that the liver image 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 imaged, indicating that the complex is mainly metabolized by the kidney; Visualization of organs is almost negligibl...

Embodiment 3

[0056] Prepare high-labeled 188 Re-NEPTDD

[0057] In a 10ml reaction tube, add ligand NEPTDD15.0mg, sodium tartrate 400.0mg, fill with helium for 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

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. Background technique [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 researchers...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D211/26C07F13/00A61K51/00A61K103/10A61P35/00
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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