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Medicine box for preparing technetium-99m labeled DTPA-LSA, preparation method and application thereof

A -99m, labeling technology, applied in the field of DTPA-LSA kits and preparation, can solve the problems of complex preparation process of kits, destroy protein structure, complex synthesis steps, etc., and achieve fast preparation of kits, simple synthesis steps, labeling high rate effect

Active Publication Date: 2010-06-16
BEIJING NORMAL UNIVERSITY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, GSA is obtained by reacting 2-imino-2-methoxyethyl-1-thio-β-D-galactopyranoside with human serum albumin, and its synthesis steps are relatively complicated
In 2004, Jeong et al. reported that a novel ligand LSA (neolactosyl human serum albumin) was obtained by linking lactose and human serum albumin in the form of a Schiff base by reductive ammoniation. The reaction was simple and mild, and LSA was reduced with β-mercaptoethanol. To obtain ligands containing sulfhydryl groups, use 99m After Tc labeling, it shows better stability and excellent biological properties, but LSA is marked by opening disulfide bonds, which will destroy the structure of the protein, affect its protein activity, and then affect its biological properties
There are many steps in the synthesis of GSA ligand, and the preparation process of the kit is complicated

Method used

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  • Medicine box for preparing technetium-99m labeled DTPA-LSA, preparation method and application thereof
  • Medicine box for preparing technetium-99m labeled DTPA-LSA, preparation method and application thereof
  • Medicine box for preparing technetium-99m labeled DTPA-LSA, preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0034] Preparation of DTPA-LSA

[0035] Take 67.5 mg of human serum albumin and dissolve it in 5 mL of phosphate buffer at pH 8.0, add 200 mg of lactose, and stir at room temperature for 2 h. Add 200 mg of sodium cyanoborohydride, mix well, filter through a 0.22 μm sterile filter, and react at 37° C. for 7 days. After the reaction, filter through a 0.22 μm sterile membrane and dialyze in sterile secondary water for 3 days. Freeze dried. Get LSAs.

[0036] Take 60 mg of the obtained LSA, dissolve it in 4 mL of newly prepared HEPES buffer solution with pH 7.0, add 10 mg of DTPA cyclic anhydride, stir gently at room temperature, and react for 20 min. After the reaction, filter through a 0.22 μm sterile membrane and dialyze in sterile secondary water for 3 days. Get DTPA-LSA.

[0037] Preparation of 75 DTPA-LSA freeze-dried kits

[0038] a. Dissolve 225mg of DTPA-LSA ligand in 37.5mL pH 3.5 tartrate-potassium sodium tartrate buffer, then add 0.4mL 3.8mg / mL SnCl 2 2H 2 O hy...

Embodiment 2

[0042] Prepare DTPA-LSA step with embodiment 1

[0043] Prepare 100 DTPA-LSA freeze-dried kits

[0044] a. Dissolve 200mg of DTPA-LSA ligand in 50mL pH 3.5 tartaric acid-potassium sodium tartrate buffer, then add 1mL of 10mg / mL SnCl 2 2H 2 O hydrochloric acid solution (1mol / L); the solution is mixed evenly, and its pH is controlled between 2.5 and 3.0;

[0045] b. Add nitrogen-filled secondary water to the solution obtained in step a. to make the volume to 100mL;

[0046] c. After the solution prepared in step b. is aseptically filtered, it is subpackaged in 100 control antibiotic bottles, then placed in a lyophilizer for 24 hours, and then sealed with a stopper, to obtain the preparation method according to the present invention. 99m Freeze-dried kit of Tc-DTPA-LSA.

Embodiment 3

[0048] Prepare DTPA-LSA step with embodiment 1

[0049] Prepare 150 DTPA-LSA freeze-dried kits

[0050] a. Dissolve 750mg DTPA-LSA ligand in 75mL pH 3.5 tartaric acid-potassium sodium tartrate buffer, then add 0.4mL 3.8mg / mL SnCl 2 2H 2 O hydrochloric acid solution (1mol / L); the solution is mixed evenly, and its pH is controlled between 3.0 and 3.5;

[0051] b. Add nitrogen-filled secondary water to the solution obtained in step a. to make the volume to 150mL;

[0052] c. After the solution prepared in step b. is aseptically filtered, it is subpackaged in 150 control antibiotic bottles, then placed in a freeze dryer for 24 hours, and then sealed with a stopper, to obtain the method for preparing antibiotics according to the present invention. 99m Freeze-dried kit of Tc-DTPA-LSA.

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Abstract

The invention discloses a medicine box for preparing technetium-99m (99mTc) labeled DTPA-LSA (99mTc-DTPA-LSA), a preparation method and application thereof. The medicine box is prepared by the method as follows: dissolving DTPA-LSA ligand in nitrogen-filled secondary water; adding buffer solution; mixing well; adding a reducing agent in a weight ratio of the reducing agent to the ligand of 1:10-800; performing sterile filtration on solution after dissolution is completely over; and putting the obtained product into containers separately. In the aspect of preparing 99mTc-DTPA-LSA, the medicine box has the advantages of use convenience, high labeling rate, good biological properties of prepared 99mTc-DTPA-LSA, low use cost and the like, and is beneficial to extensive clinical application. 99mTc-DTPA-LSA complex prepared by utilizing the medicine box can be sued as a novel liver imaging agent applied in the technical fields of radiopharmaceutical chemistry and clinical nuclear medicine.

Description

Technical field [0001] The present invention relates to 99m The field of Tc-labeled radiopharmaceutical chemistry and clinical nuclear medicine technology, especially relates to a method for preparing technetium-99m( 99m Tc) labeled DTPA-LSA ( 99m Tc-DTPA-LSA) kit, preparation method and application. Background technique [0002] ASGP receptor (Asialoglycoprotein receptor, ASGP-R) is the abbreviation of asialoglycoalbumin receptor. a bit. Almost all plasma proteins except albumin are glycoproteins whose sugar chain ends with sialic acid when synthesized by the liver and released into the blood. Sialic acid forms weak linkages with other sugar groups, is unstable in the blood and is easily cleared. The sialic acid moiety is removed, marking the end of the glycoprotein's life. The galactose structure in most plasma proteins is located at the second position of the terminal, so when the terminal sugar is enzymatically hydrolyzed, the glycoprotein ending with galactose can...

Claims

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Application Information

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IPC IPC(8): A61K51/08A61K103/10
Inventor 张现忠杨文江王学斌唐志刚张俊波陆洁
Owner BEIJING NORMAL UNIVERSITY
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