Radioactive composition, method for its single radiosynthesis and use thereof

A technology of radioactive composition and radiosynthesis, applied in radioactive carriers, in vivo radioactive preparations, pharmaceutical formulations, etc., can solve the problems of increasing patient costs, time-consuming and inability to solve

Active Publication Date: 2019-11-12
GUANGDONG HUIXUAN PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, multiple molecular probes are administered in divided doses and multiple imaging is not only cumbersome, time-consuming and increases the cost of patient visits, but also patients and staff will receive more radiation exposure
However, although the simultaneous imaging of multiple molecular probes in a single administration can avoid some defects of multiple imaging in divided administration, it needs to provide multiple PET molecular probes at the same time, and it cannot solve the problem of producing multiple PET molecular probes at a time. Difficulties with molecular probes, and the potential for radiation chemist workers to be exposed to less radioactivity

Method used

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  • Radioactive composition, method for its single radiosynthesis and use thereof
  • Radioactive composition, method for its single radiosynthesis and use thereof
  • Radioactive composition, method for its single radiosynthesis and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Embodiment 1 double tracer 18 F-FDG+ 18 Automatic Synthesis of F-FPA Compound Molecular Probe

[0032] use 18 F-FDG automatic synthesizer ( figure 1 ) and two-step on-column hydrolysis to prepare two PET drugs 18 F-FDG+ 18 F-FPA compound molecular probe, completed under computer control 18 F-FDG+ 18 The F-FPA compound molecular probe is automatically produced, and its synthesis process is shown in figure 2 . Mainly include: (1) 18 F-F - catch. passed by cyclotron 18 O(p,n) 18 Produced by F nuclear reaction 18 F-F - , at N 2 Under the airborne band, after the pretreatment Sep-Pak light QMA anion column placed in the radioactivity meter, 18 F-F - trapped in the column, 18 O-water is collected in a recovery bottle. (2) The solvent evaporates. in N 2 Under the action, the No. 1 bottle contains K 2 CO 3 and acetonitrile aqueous solution (1.0-1.5mL) of catalyst K222, the 18 F-F - Eluted into a closed reaction bottle, heated the mixed solution to 95°C...

Embodiment 2

[0034] Embodiment 2 double tracer 18 F-FDG+ 18 Automated synthesis of F-NFPGlu compound molecular probe

[0035] use 18 F-FDG automatic synthesizer ( figure 1 ) and two-step on-column hydrolysis to prepare two PET drugs 18 F-FDG+ 18 F-NFPGlu compound molecular probe, completed under computer control 18 F-FDG+ 18 The F-NFPGlu compound molecular probe is automatically produced, and its synthesis process is shown in figure 2 . Mainly include: (1) 18 F-F -catch. passed by cyclotron 18 O(p,n) 18 Produced by F nuclear reaction 18 F-F - , at N 2 Under the airborne band, after the pretreatment Sep-Pak light QMA anion column placed in the radioactivity meter, 18 F-F - trapped in the column, 18 O-water is collected in a recovery bottle. (2) The solvent evaporates. in N 2 Under the action, the No. 1 bottle contains K 2 CO 3 and acetonitrile aqueous solution (1.0-1.5mL) of catalyst K222, the 18 F-F - Eluted into a closed reaction bottle, heated the mixed solution...

Embodiment 3 3

[0037] Example 3 Three Tracers 18 F-FDG+ 18 F-FPA+ 18 Automated synthesis of F-NFPGlu compound molecular probe

[0038] use 18 F-FDG automatic synthesizer ( figure 1 ) and two-step on-column hydrolysis to prepare three PET drugs 18 F-FDG+ 18 F-FPA+ 18 The F-NFPGlu compound molecular probe completes its automated production under computer control, and its synthesis process is shown in figure 2 . Mainly include: (1) 18 F-F - catch. passed by cyclotron 18 O(p,n) 18 Produced by F nuclear reaction 18 F-F - , at N 2 Under the airborne band, after the pretreatment Sep-Pak light QMA anion column placed in the radioactivity meter, 18 F-F - trapped in the column, 18 O-water is collected in a recovery bottle. (2) The solvent evaporates. in N 2 Under the action, the No. 1 bottle contains K 2 CO 3 and acetonitrile aqueous solution (1.0-1.5mL) of catalyst K222, the 18 F-F - Eluted into a closed reaction bottle, heated the mixed solution to 95°C, and evaporated to d...

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Abstract

The invention relates to composition (a compound molecular probe preparation) containing various radioactive compounds such as <18>F-FDG (<18>F-fludeoxyglucose), <18>F-FPA (2-<18>F-fluoropropionic acid) and / or <18>F-NFPGlu ((N-2-<18>F-fluoropropionyl)-L-alpha-glutamic acid), a one-time radioactive synthesis method of the composition and an application of the composition in preparation of positron emission computed tomography drugs. The composition comprising <18>F-FDG+<18>F-FPA and <18>F-FDG+<18>F-NFPGlu or <18>F-FDG+<18>F-FPA+<18>F-NFPGlu as PET drugs can be obtained from precursors through nucleophilic fluorination reaction and a hydrolysis reaction, wherein the precursors comprise a mannose triflate and ethyl 2-bromopropionate mixture and a mannose triflate and (N-2-bromopropionyl)-L-alpha-diethyl glutamate mixture or a mixture of mannose triflate, ethyl 2-bromopropionate and (N-2-bromopropionyl)-L-alpha-diethyl glutamate. The composition can be used for differential diagnosis and therapeutic effect evaluation of tumor, cardiovascular and cerebrovascular diseases and nervous and mental diseases and can overcome limitation of <18>F-FDG.

Description

【Technical field】 [0001] The present invention relates to the composition of radioactive compounds, its single radiation synthesis method and its application in the preparation of positron emission tomography medicine. In particular, the present invention relates to a drug comprising two PET 18 F-FDG+ 18 F-FPA and 18 F-FDG+ 18 F-NFPGlu radioactive composition and containing three PET drugs 18 F-FDG+ 18 F-FPA+ 18 F-NFPGlu radioactive composition, its single radiation synthesis method and its application in the preparation of PET imaging agent. 【Background technique】 [0002] 18 F-fluorodeoxyglucose ( 18 F-FDG) is the most widely used positron emission tomography (PET) imaging agent (drug) for differential diagnosis and curative effect monitoring of tumors, cardiovascular and cerebrovascular diseases, and neuropsychiatric diseases, but some false positives and false negatives may also occur result. Imaging with multiple molecular probes can compensate for 18 The lac...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K51/04A61K101/02
CPCA61K51/0402A61K51/0406A61K51/0491
Inventor 唐刚华
Owner GUANGDONG HUIXUAN PHARMA TECH
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