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Synthesis method of <18>F-labeled amino acid polypeptide drugs and kit

A drug synthesis and amino acid technology, applied in the preparation method of peptides, chemical instruments and methods, peptides, etc., can solve the problems of radiation safety protection risks, difficult automatic industrial production, etc., and achieve the promotion of development, huge social benefits and social benefits. Benefit, the effect of high-dose industrialization

Active Publication Date: 2017-12-22
北京派特生物技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, existing 18 F-AlF labeled amino acid peptide drugs, such as 18 F-AlF-NOTA-Glu, 18 F-AlF-NOTA-NOC, 18 F-AlF-NOTA-PEG3-Glu-RGD2 and 18 F-AlF-NOTA-PEG3-β-Glu-RGD2, etc., can only be prepared in low doses by kit method 18 F-AlF-NOTA-Biomolecules, not accelerator-produced at all 18 f - Ions are used directly for 18 F-AlF labels amino acids and peptides, which is difficult to realize fully automatic industrial production, and brings certain risks to radiation safety protection

Method used

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  • Synthesis method of &lt;18&gt;F-labeled amino acid polypeptide drugs and kit
  • Synthesis method of &lt;18&gt;F-labeled amino acid polypeptide drugs and kit
  • Synthesis method of &lt;18&gt;F-labeled amino acid polypeptide drugs and kit

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 118

[0048] Example 1 18 Fully automatic industrial synthesis of F-AlF-NOTA-Glu injection

[0049] Kit composition: 0.4-0.5mL physiological saline (bottle 1), 200-300μg precursor NOTA-Glu+2mM 24μL AlCl 3 (bottle 2), 0.8-1.2mL pH4-5 acidic acetonitrile solution (bottle 2') (bottle 2' is in the kit, but in figure 1 Not shown in , the solution from vial 2' was added to vial 2 before synthesis), 15 mL of water for injection (bottle 3), 10 mL of water for injection (bottle 4), 1.5 mL of ethanol (bottle 5) and 18 mL of 0.57 mM ascorbic acid containing Normal saline (bottle 6). Auxiliary materials include: SEP-PAK C18 separation column, SEP-PAK QMA column, column pretreatment solvent or solution (ethanol, water for injection, 8.4% sodium bicarbonate solution), syringe and needle, receiving bottle, import and export without Bacterial membrane. SEP-PAK QMA cartridges can also be replaced by other anion cartridges; physiological saline can be replaced by other inorganic salt solutions; a...

Embodiment 218

[0052] Example 2 18 Fully automatic industrial synthesis of F-AlF-NOTA-NOC injection

[0053] Kit composition: 0.4-0.5mL physiological saline (bottle 1), 200-300μg precursor NOTA-NOC+2mM 24μL AlCl 3 (bottle 2), 0.8-1.2mL pH4-5 acidic acetonitrile solution (bottle 2'), 15mL normal saline (bottle 3), 10mL normal saline (bottle 4), 1.5mL ethanol (bottle 5) and 18mL containing 0.57mM ascorbic acid Normal saline (bottle 6). Auxiliary materials include: HLB small column, SEP-PAK QMA small column, small column pretreatment solvent or solution (ethanol, normal saline, water for injection, 8.4% sodium bicarbonate solution), syringe and needle, receiving bottle, sterile import and export filter membrane. SEP-PAK QMA cartridges can also be replaced by other anion cartridges; physiological saline can be replaced by other inorganic salt solutions; acetonitrile can be replaced by dimethyl sulfoxide, ethanol, and methanol; HLB cartridges can also be separated by SEP-PAK C18 small column ...

Embodiment 318

[0056] Example 3 18 Fully automatic industrial synthesis of F-AlF-NOTA-PEG3-β-Glu-RGD2 injection

[0057] Kit composition: 0.4-0.5mL normal saline (bottle 1), 200-300μg precursor NOTA-PEG3-β-Glu-RGD2+2mM 24μL AlCl 3 (bottle 2), 0.8-1.2mL pH4-5 acidic acetonitrile solution (bottle 2'), 15mL water for injection (bottle 3), 10mL water for injection (bottle 4), 1.5mL ethanol (bottle 5) and 18mL containing 0.57mM ascorbic acid Normal saline (bottle 6). Auxiliary materials include: SEP-PAK C18 separation column, SEP-PAK QMA column, column pretreatment solvent or solution (ethanol, water for injection, 8.4% sodium bicarbonate solution), syringe and needle, receiving bottle, import and export without Bacterial membrane. SEP-PAK QMA cartridges can also be replaced by other anion cartridges; physiological saline can be replaced by other inorganic salt solutions; acetonitrile can be replaced by dimethyl sulfoxide, ethanol, and methanol; SEP-PAK C18 cartridges can also be replaced by H...

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Abstract

The embodiment of the invention relates to a synthesis method of <18>F-labeled amino acid polypeptide drugs and a kit. The method comprises the following steps: capturing <18>F<-> ions produced by a cyclotron through an anion small column; introducing 0.4-0.5ml of normal saline into the anion small column, then eluting the <18>F<-> ions to obtain first reaction liquid, and introducing the first reaction liquid into a reaction bottle; adding precursor-AlCl3 acid solution-organic solvent mixed liquid with a pH value of 4-5 into the reaction bottle, wherein the precursor is NOTA derivative, and NOTA is triazacyclononane triacetoxyl or triazacyclononane diacetoxyl; heating the reaction bottle to 100-110 DEG C and carrying out labeled synthesis; cooling, then adding water into liquid in a solid-phase extraction reaction bottle and diluting; separating the diluted liquid in the solid-phase extraction reaction bottle through a solid-phase extraction small column and enabling products to be obtained to be adsorbed to the solid-phase extraction small column; washing the solid-phase extraction small column with water and removing organic solvents and impurities; washing the solid-phase extraction small column with alcohol, putting the products to be obtained in a product bottle, and adding preparation liquid to obtain the synthesized products.

Description

technical field [0001] The present invention relates to the field of drug synthesis, in particular to a 18 F-labeled amino acid polypeptide drug synthesis method and kit. Background technique [0002] 18 F-fluorodeoxyglucose ( 18 F-FDG) has been widely used in early tumor diagnosis and guiding treatment, but it is a non-specific positron emission tomography (PET drug), prone to false positive and false negative results. 18 F-labeled amino acids and targeting receptor specificity 18 F-labeled polypeptide PET drugs can make up 18 The serious shortage of F-FDG is an important development direction for the development of PET drugs. However, existing general 18 The method for labeling biomolecules involves the use of N-succinimide-4- 18 F-fluorobenzoate ( 18 F-SFB) and 18 F-4-nitrophenyl-2-fluoropropionate ( 18 F-NFP) marks the amino acid polypeptide-NH2 group, and the reaction steps are many, the operation is more complicated, the synthesis time is long, and it is diff...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06C07K1/13C07D255/02
CPCC07D255/02C07K7/06
Inventor 唐刚华胡晓平胡生焰
Owner 北京派特生物技术有限公司
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