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18F-boron trifluoride tyrosine kit and application thereof

A technology of boron trifluoride and tyrosine, which is applied in the field of radiopharmaceuticals and nuclear medicine, can solve the problems of small labeling volume, health hazards of radiation dose, inapplicability to clinical large-scale, modular labeling conditions, etc., and achieve simple operation steps , the effect of reducing radioactivity

Active Publication Date: 2020-12-04
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, the existing boron trifluoride tyrosine labeling process has the disadvantages of small labeling volume (no more than 100uL), low yield (<3.7E9Bq), and is not suitable for clinical large-scale and modular labeling conditions; and its labeling process It is very dependent on the experience of the operator, and manual marking poses a health hazard to the radiation dose brought by the operator

Method used

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  • 18F-boron trifluoride tyrosine kit and application thereof
  • 18F-boron trifluoride tyrosine kit and application thereof
  • 18F-boron trifluoride tyrosine kit and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0068] According to the precursor content shown in Table 1, experiment according to the following experimental steps:

[0069] a) Dissolving a specific mass of precursor (i.e. FBY) in 1 ml of saline;

[0070] b) Use 1ml of normal saline to rinse and retain the QMA column with 1000mCi F-18 fluoride ions, and 18 F-wash into the reaction tube;

[0071] c) using concentrated brine to adjust the pH to 2;

[0072] d) The reaction tube is sealed and heated at 85°C for 20 minutes;

[0073] e) Analysis of radioactivity yield using paper chromatography (ITLC-SG paper, 95% acetonitrile / water development)

[0074] Table 1

[0075] serial number precursor radioactivity yield 1-1 0.1mg FBY 5.3％ 1-2 0.2mg FBY 7.6％ 1-3 0.5mg FBY 29.3％ 1-4 1.0mg FBY 46.8％ 1-5 1.5mg FBY 48.8％ 1-6 2.0mg FBY 49.2％

Embodiment 2

[0077] According to the hydrochloric acid content shown in table 2, experiment according to the following experimental steps:

[0078] a) Dissolving 1 mg of FBY precursor in 1 ml of hydrochloric acid of a specific concentration;

[0079] b) Use 1ml of normal saline to rinse and retain the QMA column with 500mCi F-18 fluoride ions, and 18 F-wash into the reaction tube;

[0080] c) The reaction tube is sealed and heated at 85°C for 20 minutes;

[0081] d) Analysis of radioactivity yield using paper chromatography (ITLC-SG paper, 95% acetonitrile / water development)

[0082] Table 2

[0083] serial number Hydrochloric acid concentration radioactivity yield 2-1 0.02M 0％ 2-2 0.04M 0％ 2-3 0.06M 5.1％ 2-4 0.08M 45.1％ 2-5 0.10M 46.0％ 2-6 0.15M 45.8％ 2-7 0.20M 43.6％

Embodiment 3

[0085] According to the reaction time shown in table 3, experiment according to the following experimental steps:

[0086] a) Dissolving 1 mg of FBY precursor in 1 ml of 0.08M hydrochloric acid;

[0087] b) Use 1ml of normal saline to rinse and retain the QMA column with 500mCi F-18 fluoride ions, and 18 F-wash into the reaction tube;

[0088] c) The reaction tube is sealed and heated at 85°C for a specific time;

[0089] d) Add 1ml of normal saline to quench the reaction after the reaction;

[0090] e) Analysis of radioactivity yield using paper chromatography (ITLC-SG paper, 95% acetonitrile / water development)

[0091] table 3

[0092] serial number Reaction time radioactivity yield 3-1 2min 10.3％ 3-2 4min 21.1％ 3-3 6min 28.7％ 3-4 8min 36.9％ 3-5 10min 44.6％ 3-6 15min 45.4％ 3-7 20min 45.1％

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Abstract

The invention relates to a 18F boron trifluoride tyrosine kit and application thereof. The kit comprises a precursor bottle A, a hydrochloric acid solution bottle B, a sodium salt solution bottle C, adeionized water bottle D, a sodium salt solution bottle E, a normal saline bottle F, a normal saline bottle G, a product bottle H, a QMA column, a SepPak Aluma column and a sterile filter membrane. The kit provided by the invention overcomes the problems in 18F boron trifluoride tyrosine labeling in the prior art, constructs and perfects a new 18F boron trifluoride tyrosine labeling preparation process flow, can be directly mounted on a radiopharmaceutical multifunctional synthesis module for use, is suitable for automatic operation and clinical use in hospitals, and has a wide application prospect. And large-volume and large-dose marking reaction requirement under automatic module marking can be met.

Description

technical field [0001] The invention relates to the technical field of radiopharmaceuticals and nuclear medicine, in particular to a 18 F-boron trifluoride tyrosine kit and its application. Background technique [0002] Tumor is still a common and frequently-occurring disease that seriously threatens human health, and is one of the main causes of death. In the diagnosis of tumors and related diseases, molecular imaging technology combines molecular probes and medical imaging technology to conduct qualitative and quantitative research on pathological and physiological processes in vivo at the cellular and molecular levels. [0003] Positron Emission Tomography (PET) is a molecular imaging technique based on radioactive molecular probes. PET technology is based on the detection of paired photons emitted by the annihilation of positrons. From 11 C, 18 The positrons emitted from positron-decaying isotopes such as F quickly collide with the negative electrons widely distribu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F5/02C07B59/00A61K31/69A61K51/04A61K41/00A61P35/00A61K101/02
CPCA61K41/0095A61K51/0406A61P35/00C07B59/001C07B2200/05C07F5/02
Inventor 刘志博陈俊艺
Owner PEKING UNIV