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99m Tc marked polyamine complex as tumor diagnosing developing agent and its preparation

A complex and labeling technology, applied in the field of radiopharmaceuticals and nuclear medicine, can solve the problems of high cost and difficulty in promotion, and achieve the effects of low price, low price and popular use.

Inactive Publication Date: 2007-04-04
潘尚仁
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the nuclides used in positron emission tomography agents must be produced by accelerators, which is expensive and difficult to promote

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1、99

[0018] Embodiment 1, 99m Labeling of technetium-triethylenetetramine:

[0019] Triethylenetetramine (the chemical name is N, N`-bis(2-aminoethyl)-1,2-ethanediamine, the common name of the drug is Trientine), which has been approved as a therapeutic drug for the treatment of hepatolenticular degeneration in foreign countries . We use it with [ 99m Tc] technetium complex preparation [ 99m Tc] triethylenetetramine technetium injection.

[0020] Sodium stannous glucoheptonate for injection (containing sodium glucoheptonate 8 mg, stannous chloride 0.8 mg, produced by Jiangyuan Pharmaceutical Factory) freeze-dried product bottle, add [ 99m Tc] Sodium pertechnetate injection 1ml (370mBq), then add 2ml of triethylenetetramine physiological saline solution (containing 10mg of triethylenetetramine, adjust the pH to 6.5 with dilute hydrochloric acid), shake well, let it stand for 15min, and it is ready.

[0021] Radiochemical purity was determined by paper chromatography. Use Xi...

Embodiment 2、99

[0022] Embodiment 2, 99m Technetium-diethylenetriamine labeling:

[0023] Sodium stannous glucoheptonate for injection (containing sodium glucoheptonate 8 mg, stannous chloride 0.8 mg, produced by Jiangyuan Pharmaceutical Factory) freeze-dried product bottle, add [ 99m Tc] Sodium pertechnetate injection 1ml (370mBq), then add 2ml of diethylenetriamine physiological saline solution (containing 5mg of diethylenetriamine, adjust the pH to 3.5 with dilute hydrochloric acid), shake well, and let stand for 15min to obtain.

[0024] Radiochemical purity was determined by paper chromatography. Use Xinhua No. 1 paper as the carrier, and the developer uses methanol: chloroform: water (85:15:5) mixed solvent, [ 99mTc] Rf of pertechnetate is at 0.1-0.2, 99m The Rf of technetium-glucoheptonate is below 0.6, [ 99m Rf of Tc]-diethylenetriamine technetium marker is at 0.7-1.0.

Embodiment 3

[0025] Embodiment 3, the preparation of kit:

[0026] Take 5-10g of tetraethylenepentamine, dissolve it with an appropriate amount of water for injection, adjust the pH to 3.5-8 with hydrochloric acid, add 0.5-1g of tin chloride, 5-10g of sodium glucoheptonate, adjust the pH to 3.5-8, and use Dilute with water for injection to a final volume of 1000ml, filter through a 4-micron microporous membrane until clarified, dispense into vials, 1ml per bottle, and freeze-dry to obtain the product. Before use, add [ 99m Tc] sodium pertechnetate injection 370 ~ 740MBq, ready to stand for 15 minutes.

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PUM

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Abstract

The 99mTc marked polyamine complex as tumor diagnosing developer and its preparation relates to the field of radioactive medicine and nuclear medicine technology. The 99mTc marked polyamine complex has the chemical expression of 99mTcvO(III)-[NH2.(CH2)2-4...NH...(CH2)2-4NH2], and the polyamine as ligand may be diethylenetriamine, triethylenetetramine, tetraethylenepentamine, spermidine or spermine. The preparation process includes adding reductant stannous ion and stabilizer hydroxy acid salt into polyamine solution to prepare freeze dried medicine kit, and adding sodium pertechnetate for 99mTc marking to prepare 99mTc marked polyamine complex injection. One other preparation process is also provided. The product is used as tumor diagnosing developer, and has simple preparation process and high target / ground contrast and high use effect after being injected into tumor.

Description

technical field [0001] 99m Technetium-labeled polyamine complex tumor diagnostic imaging agent and its preparation, the invention relates to the technical field of radiopharmaceuticals and nuclear medicine. Background technique [0002] Polyamines are important substances for regulating cell growth in organisms, and they are ubiquitous in various tissues in the body. Polyamine molecule is a straight-chain aliphatic amine with multiple nitrogen atoms and more positive charges. It can combine with negatively charged DNA and RNA molecules to stabilize its structure and promote certain links in the synthesis of nucleic acids and proteins. . Polyamines in organisms mainly refer to putrescine, spermidine and spermine, which have a special pathway to maintain the balance of polyamine pools in cells through synthesis, uptake, degradation and excretion. Polyamines are particularly abundant in vigorously growing tissues such as embryos and tumors. Since the discovery of the relati...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F13/00A61K51/00A61K103/10
Inventor 潘尚仁
Owner 潘尚仁
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