Small modular multifunctional automatic 18F labelling PET (positron emission tomography) drug synthesizer

A modular technology for drug synthesis, applied in chemical instruments and methods, isotope introduction of organic compounds, organic chemistry, etc., can solve the problems of unsuitable PET drug production, high maintenance and warranty costs, and large synthesizer volume, so as to ensure that the instrument Safety, easy installation, powerful effect

Active Publication Date: 2015-01-07
BEIJING SHANWEIZHENGZI MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the synthesizer has a large volume and is inconvenient to maintain; the maintenance and warranty cost is relatively high if a connecting valve is used
In addition, both domestically produced and imported multifunctional automatic synth

Method used

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  • Small modular multifunctional automatic 18F labelling PET (positron emission tomography) drug synthesizer
  • Small modular multifunctional automatic 18F labelling PET (positron emission tomography) drug synthesizer
  • Small modular multifunctional automatic 18F labelling PET (positron emission tomography) drug synthesizer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Embodiment 1 FDG automatic synthesis

[0046] self-test. Adjust the pressure of the cylinder pressure valve to be greater than 0.5MPa, add N 2 The pressure is 0.2MPa, blowing air to evaporate N 2 The flow rate is 80-100ml / min; add water, acetonitrile, acetonitrile and water 2-3ml to No. 1, No. 2, No. 3 and No. 5 bottles respectively. After connecting the pipelines, installing the waste bottle and receiving bottle, start the self-test procedure. Check heating and gas delivery for proper operation.

[0047] Preparation before production.

[0048] 1. Prepare the QMA cartridge. Take 0.3M NaHCO 3 (or Na 2 CO 3 ) 10ml, passed through a Sep Pak light QMA cartridge to remove excess liquid. Take 10ml of water for injection, pass through the QMA column, and get rid of excess liquid. Or take another 10ml of chromatographically pure acetonitrile, pass through the QMA column, and remove the excess liquid.

[0049] 2. C-18 cartridge processing. Take 10ml of absolute ethan...

Embodiment 2

[0063] Example 2 18F-FLT automatic synthesis

[0064] Preparation before production. Edit 3'-deoxy-3'- in the package 18 F-fluorothymidine (18F-FLT) automated synthesis procedure ( figure 2 FDG1-fluorinated part and HPLC part). Install Sep Pak Light QMA Cartridges and Sep Pak Al in place 2 o 3 Neutral separation cartridge. Add K222 solution to No. 1 bottle, that is, add 1.5ml of acetonitrile water (volume ratio 10 / 1) solution, containing 15mg of phase transfer catalyst amino polyether 4,7,13,16,21,24-hexaoxa-1 , 10-diazabicyclo[8,8,8]hexacane (Kryptofix2.2.2, K222) and 3mg K 2 CO 3 ; Add 15 mg of the precursor 3-N-t-tert-butoxycarbonyl-1-[5'-O-(4,4'-dimethoxytrityl)-2'-deoxy-3 to bottle No. 3 '-O-(4-nitrobenzenesulfonyl)-β-D-threo-furanosyl]thymine in acetonitrile solution (1mL); add 1mol / L hydrochloric acid (1mL) to bottle No. 4; add 1mol / L sodium hydroxide solution (1mL); add ethanol-water eluent (1mL) with a volume ratio of less than 10:90 into No. 6 bottle. Clos...

Embodiment 3

[0071] Example 3 18 F-FCH automatic synthesis

[0072] Preparation before production. Edit (N-18F-fluoromethyl)choline in the package ( 18 F-FCH) automated synthesis program ( figure 2 FDG1-fluorinated part and FDG2-converted part). Install 1 Sep Pak Light QMA cartridge, 3 Sep Pak plus SiO2 cartridges, 1 Sep Pak plus tC18 cartridge and Sep Pak CM cartridge at a suitable location. FDG1-fluorinated part: add 1.5mL K222 solution to bottle No. 1; add dibromomethane (300 μL) in acetonitrile (2 mL) solution to bottle No. 3. FDG2-conversion part: Load N,N-dimethylethanolamine 0.4mL in Sep Pak plus tC18 cartridge; add 10mL ethanol to No. 1 bottle; add 10mL water to No. 2 bottle; add 3mL saline to No. 3 bottle. Close the thermal cell door.

[0073] Automated manufacturing. Select the 18F-FCH synthesis program in the menu of the software, press the "start operation" button, and complete it under the control of the computer 18 F-FCH automated synthesis.

[0074] (1)[K / K222]+ 1...

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PUM

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Abstract

The invention provides a small modular multifunctional automatic 18F labelling PET (positron emission tomography) drug synthesizer and relates to an automatic PET drug synthesizer. The small modular multifunctional automatic 18F labelling PET drug synthesizer comprises a single FDG (fluorodeoxyglucose) synthesis module or two FDG synthesis modules which are connected in series, namely a module FDG1 and a module FDG2, a PET drug product separating system and a control system, wherein the single FDG synthesis module or the two FDG synthesis modules which are connected in series are used for independently completing FDG synthesis or continuously completing double-batch FDG synthesis in a combined manner; the PET drug product separating system is connected with the single FDG synthesis module or a second module, namely the module FDG2, in the two FDG synthesis modules which are connected in series; and the control system is used for connecting and controlling the FDG synthesis module and the PET drug product separating system. The small modular multifunctional automatic PET drug synthesizer has the characteristics of ingenious structure, small size, simple mounting, friendly interface, simple operation, safety, stability, reliability, convenience in maintenance, powerful function and flexibility, is simple to mount and operate, and convenient to maintain, and the production requirement of 18F labelling PET drugs for the current market and scientific research can be met.

Description

technical field [0001] The invention relates to a medicine preparation device, in particular to a PET (Positron Emission Tomography) medicine automatic synthesizer. Background technique [0002] 2- 18 F-2-deoxy-D-glucose (FDG) is the most commonly used positron emission tomography (PET) radiopharmaceutical (also known as imaging agent), and has been widely used in PET clinical diagnosis of tumors, cardiovascular diseases and neuropsychiatric diseases and efficacy evaluation. However, false positive and false negative results may also occur during clinical examination of FDG, so it is necessary to imitate or develop a variety of PET drugs to improve the sensitivity, accuracy and specificity of PET diagnosis. FDG is usually produced with a dedicated automated synthesizer to meet the needs of clinical PET. However, with the continuous introduction and development of PET technology, it is necessary to produce a variety of PET drugs clinically, and the specific automatic synth...

Claims

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Application Information

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IPC IPC(8): C07B59/00G21G1/04
Inventor 唐刚华张勇
Owner BEIJING SHANWEIZHENGZI MEDICAL TECH
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