Technetium-99m-marked poly N-vinyl benzyl-D-lactose amide composition and preparation method

A technology of vinylbenzyl and lactamide, which is applied in the fields of radiopharmaceutical chemistry and clinical nuclear medicine, can solve the problems of human serum albumin being easily deteriorated and difficult to store.

Inactive Publication Date: 2010-10-06
BEIJING NORMAL UNIVERSITY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, human serum albumin is ea...

Method used

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  • Technetium-99m-marked poly N-vinyl benzyl-D-lactose amide composition and preparation method
  • Technetium-99m-marked poly N-vinyl benzyl-D-lactose amide composition and preparation method
  • Technetium-99m-marked poly N-vinyl benzyl-D-lactose amide composition and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0077] With Tricine as co-ligand, 99m Tc(PVLA)(tricine) 2 Preparation of:

[0078] Dissolve 0.2mg of p(VLA-co-VNI) in 0.5mL phosphate buffer (0.05mol / L pH6.0, containing 30mg co-ligand tricine), and add 2mg / mL SnCl 2 2H 2 O solution 10μL, shake well. Add fresh at the end 99m TCO 4 - Eluent 0.5mL (37MBq), fully shake, seal and react in boiling water bath for 20min. get 99m Tc(PVLA)(tricine) 2 .

[0079] The HiTrap desalting gel column (Sephadex G25) was equilibrated with 25 mL eluent (0.05 mol / L phosphate buffer at pH 7.5), and the flow rate was controlled between 1 and 10 mL / min. Mark 0.25mL 99m Tc(PVLA)(tricine) 2 Use a 1mL syringe to load the sample, first rinse with 1.25mL eluent, and collect 1mL eluent to obtain a sample that removes impurities and has a recovery rate of >95%. 99m Tc(PVLA)(tricine) 2 solution.

[0080] Identified by chromatography and RP-HPLC, the retention time is 11.9 min, and the radiochemical purity is greater than 99%. HPLC conditions ...

Embodiment 2

[0082] With Bicine as co-ligand, 99m Preparation of Tc(PVLA)(bicine):

[0083] Dissolve 1mg of p(VLA-co-VNI) in 0.5mL phosphate buffer (0.05mol / L pH6.0, containing 20mg co-ligand bicine), and add 2mg / mL SnCl 2 2H 2 O solution 5 μL, shake well. Add fresh at the end 99m TCO 4 - Eluent 0.5mL (37MBq), fully shake, seal and react in boiling water bath for 20min. get 99m Tc(PVLA)(bicine).

[0084] The HiTrap desalting gel column (Sephadex G25) was equilibrated with 25 mL eluent (0.05 mol / L phosphate buffer at pH 7.5), and the flow rate was controlled between 1 and 10 mL / min. Mark 0.25mL 99m Tc(PVLA) (bicine) was loaded with a 1mL syringe, first rinsed with 1.25mL of eluent, and collected 1mL of eluent to obtain a product with the removal of impurities and a recovery rate of >95%. 99m Tc(PVLA) (bicine) solution.

Embodiment 3

[0086] With HEDTA as co-ligand, 99m Preparation of Tc(PVLA)(HEDTA):

[0087] Dissolve 3mg of p(VLA-co-VNI) in 0.5mL phosphate buffer (0.05mol / L pH6.0, containing 50mg co-ligand HEDTA), and add 2mg / mL SnCl 2 2H 2 O solution 20μL, shake well. Add fresh at the end 99m TCO 4 - Eluent 0.5mL (37MBq), fully shake, seal and react in boiling water bath for 20min. get 99m Tc(PVLA)(HEDTA).

[0088] The HiTrap desalting gel column (Sephadex G25) was equilibrated with 25 mL eluent (0.05 mol / L phosphate buffer at pH 7.5), and the flow rate was controlled between 1 and 10 mL / min. Mark 0.25mL 99m Tc(PVLA) (HEDTA) was loaded with a 1mL syringe, first rinsed with 1.25mL of eluent, and collected 1mL of eluent to obtain a product with the removal of impurities and a recovery rate of >95%. 99m Tc(PVLA)(HEDTA) solution.

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Abstract

The invention discloses a technetium-99m-marked poly N-vinyl benzyl-D-lactose amide composition. By using 99mTc as a central core, using polymer-poly N-vinyl benzyl-D-lactose amide-N-vinyl benzyl-6-hydrazino pyridine-3-formamide containing 6-hydrazino pyridine-3-formamide groups and galactose groups as a ligand, adopting one of N-tris hydroxymethyl-methylglycine, N,N-2-hydroxyethyl glycine and N-2-hydroxyethyl ethylene diaminetriacetic acid as a common ligand and adopting one of tris(3-sulfonatophenyl) phosphine hydrate or tris(3-sulfonatophenyl) phosphine sodium salt as a synergetic ligand, the technetium-99m-marked poly N-vinyl benzyl-D-lactose amide composition is prepared through the steps of mixing, reduction, reaction, purification and the like. The composition has the advantages of good chemical stability and biological performance, high specific activity, high liver uptake value and target to non-target ratio, simple preparation and low operating cost and can be used for preparing novel liver receptor developers applied in the technical fields of radiopharmaceutical chemistry and clinical nuclear medicine.

Description

Technical field [0001] The invention relates to the technical fields of technetium-99m-labeled radiopharmaceutical chemistry and clinical nuclear medicine, in particular to a technetium-99m-labeled poly(N-vinylbenzyl-D-lactosamide) complex and a preparation method thereof and apply. 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 serve as the substr...

Claims

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Application Information

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IPC IPC(8): C08F212/14C08F8/42C08F8/32C08F8/40A61K51/06A61K103/10
Inventor 张现忠杨文江王学斌陆洁张俊波唐志刚
Owner BEIJING NORMAL UNIVERSITY
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