Clinical single-tube fluorine-18 multifunctional module equipment and radiopharmaceutical synthesis process

A multifunctional, clinical technology, applied in chemical/physical processes, chemical/physical/physical chemical processes, chemical/physical/physical chemical stationary reactors, etc. problems, to reduce the additional radiation dose, eliminate the interference of impurities, and avoid solvent conversion.

Active Publication Date: 2021-02-23
派特(北京)科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] 1. Based on 18 F-FDG synthesis, the module that assists the HPLC separation system, adopts a separate nucleophilic synthesis and purification system, which cannot effectively integrate the whole process of synthesis, separate operations in the operation, and there is a disconnection phenomenon, and new drugs cannot be developed independently in the later stage
[0005] 2. The powerful All-In-One module synthesizes different nuclides on the same module, and there is a problem of mutual contamination of nuclides, which does not meet the GCP requirements for drug synthesis; at the same time, there is a phenomenon of valve waste due to multiple valve combinations
[0007] 4. All the above modules measure the radioactivity of the product outlet pipeline during HPLC separation, and there is no display for the distribution and residue of radioactivity on the HPLC column, and it is impossible to warn the radioactive peak of the product
Especially when there are multiple side reactions, when a large radioactivity peak is dete...

Method used

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  • Clinical single-tube fluorine-18 multifunctional module equipment and radiopharmaceutical synthesis process
  • Clinical single-tube fluorine-18 multifunctional module equipment and radiopharmaceutical synthesis process
  • Clinical single-tube fluorine-18 multifunctional module equipment and radiopharmaceutical synthesis process

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 118

[0048] Example 1. 18 Synthesis of F-DCFPyL

[0049] like image 3 Reagents were individually installed in the following vials and mounted on the module prior to synthesis as shown:

[0050] B1: 1 mL of TBA-containing acetonitrile solution; B2: 2 mL of acetonitrile; B3: 5 mg of precursor dissolved in 0.5 mL of acetonitrile; B4: 0.5 mL of 50% phosphoric acid (V / V); B5: 7 mL of HPLC mobile phase; B6: 10 mL of 0.5 mol / L NaHCO 3 .

[0051] The 2200mCi 18 The F ions are transferred from the accelerator to the QMA column, start the automatic program, and run automatically under the control of the computer: rinse the QMA column with the acetonitrile solution containing TBA in the B1 bottle into the reaction tube, heat, aerate and azeotropically remove water with acetonitrile, and then Add acetonitrile in bottle B2 to remove water repeatedly, cool to 45℃, add the precursor in bottle B3, nucleophilic reaction at 50℃ for 5min, then add phosphoric acid in bottle B4, hydrolyze at 50℃...

Embodiment 218F-7

[0054] Example 2. 18 Synthesis of F-7Q-PSMA

[0055] like image 3 As shown, the reagents were separately installed in the following vials prior to synthesis:

[0056] B1: 1 mL of acetonitrile solution containing TBA; B2: 2 mL of acetonitrile; B3: 0.5 mg of precursor dissolved in 0.5 mL of DMF; B4: empty; B5: 7 mL of HPLC mobile phase; B6: 10 mL of 0.5 mol / L NaHCO 3 .

[0057] The 800mCi 18 The F ions are transferred from the accelerator to the QMA column, start the automatic program, and run automatically under the control of the computer: rinse the QMA column with the acetonitrile solution containing TBA in the B1 bottle into the reaction tube, heat, aerate and azeotropically remove water with acetonitrile, and then Add the acetonitrile solution in bottle B2 to repeat water removal, cool to 45 °C, add the precursor in bottle B3, and conduct nucleophilic reaction at 50 °C for 5 min. After adding the HPLC mobile phase in bottle B5, separate the upper half of the mixture by...

Embodiment 318

[0060] Example 3. 18 Synthesis of F-FMSIO

[0061] like image 3 As shown, the reagents were separately installed in the following vials prior to synthesis:

[0062] B1: 1mL acetonitrile solution containing K2.2.2; B2: 2mL acetonitrile; B3: 5mg precursor dissolved in 1mL acetonitrile; B4: 2ml 1mol / L hydrochloric acid; B5: 1mL 2mol / L NaOH and 5mL HPLC mobile phase mixture; B6: empty .

[0063] The 1940mCi 18 The F ions are transferred from the accelerator to the QMA column, start the automatic program, and run automatically under computer control: rinse the QMA column with the acetonitrile solution containing K2.2.2 in the B1 bottle and put it into the reaction tube, heat, aerate and azeotropically remove water with acetonitrile, Then add the acetonitrile solution in the B2 bottle to repeat the water removal, cooling, add the precursor in the B3 bottle, nucleophilic reaction at 115 ℃ for 5 minutes, then add the hydrochloric acid solution in the B4 bottle, hydrolyze at 110 ℃...

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PUM

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Abstract

The invention relates to clinical single-tube fluorine 18 multifunctional module equipment and a radiopharmaceutical synthesis process. The clinical single-tube fluorine 18 multifunctional module equipment comprises a fluorine-18 ioncapturing and releasingmodule, a high performance liquid chromatography column purification module and a product collection module, wherein the high performance liquidchromatography column purification module adopts liquid for intravenous injection as an HPLC mobile phase; a QMA column of the fluorine-18 ion capturing and releasing module captures fluorine-18 ionsgenerated from an accelerator, and the leacheate of the QMA column and a prodrug respectively enter a reaction tube for mixing with the HPLC mobile phase; the reaction tube is connected with an HPLCseparation column of the high performance liquid chromatography column purification module; the HPLC separation column is connected with the product collection module; and a product having been subjected to online dilution and sterile filtration membrane treatment can be used for intravenous injection. By adopting the equipment and the process provided by the invention, solvent conversion used bya common module can be avoided, a target compound can be correctly collected, the pH value and the radioactive concentration of the product can be adjusted on line, and the process is suitable for full-automatic preparation of clinically common positron emission drugs under a GMP condition.

Description

technical field [0001] The invention belongs to the synthesis technology of fluorine-18-labeled radiopharmaceuticals, in particular to a clinical single-tube fluorine-18 multifunctional modular equipment and a radiopharmaceutical synthesis process. Background technique [0002] 18 F-FDG is currently the most widely used radiopharmaceutical, and is widely used in the diagnosis of various common diseases. but 18 F-FDG is glucose metabolism, which only reflects the uptake and retention of glucose in organs and tumors. There are many deficiencies in practical clinical applications, such as deficiencies in tumor receptors, tumor proliferation, and cellular hypoxia imaging. There is an urgent need for other positron radiopharmaceuticals to make up for 18 Inadequacy of F-FDG. Several specific positron radiopharmaceuticals, such as those for prostate cancer, have been reported in the literature: 18 Imaging drugs for F-DCFPyL and Aβ deposition in the brain 18 F-AV1, cellular hy...

Claims

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Application Information

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IPC IPC(8): B01D15/10B01J4/00B01J19/24C07D213/73
CPCB01D15/10B01J4/001B01J19/2415C07D213/73
Inventor 周彤
Owner 派特(北京)科技有限公司
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