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Method and equipment for on-line prepn. of dopamine transport protein developer [IIC]-beta-CFT

A transport protein and imaging agent technology, applied in the field of nuclear medicine, can solve the problems of high technical difficulty, expensive oxygen-18 gas, and low labeling rate, and achieve the effects of reducing the dose received, simplifying equipment, and saving time

Inactive Publication Date: 2006-07-19
GENERAL HOSPITAL OF PLA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

but 18 F-FP-β-CIT has the following disadvantages as a DAT imaging agent: (1) the amount of expensive precursor is large, generally greater than 5 mg (4000 yuan / mg); (2) the labeling rate is low, at 10% (3) The specific activity prepared by one-step method is on the low side
but currently 18 F-β-CFT is prepared by electrophilic substitution, which has obvious shortcomings: (1) F-18 electrophilic substitution preparation 18 The technology of F-β-CFT is very difficult; (2) the raw material oxygen-18 gas for producing F-18 gas is very expensive; (3) the electrophilic substitution product has a carrier
The conventional method has the following deficiencies: (1) the preparation procedure is complicated, and the heating of the reaction bottle and the pipetting of the radioactive solution need to be completed by a manipulator, which is difficult to realize automatic preparation; (2) the preparative HPLC separation is difficult to complete in an ordinary laboratory; 3) The preparation time is long, and the synthesis efficiency without correction is low, only about 30-40%

Method used

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  • Method and equipment for on-line prepn. of dopamine transport protein developer [IIC]-beta-CFT
  • Method and equipment for on-line prepn. of dopamine transport protein developer [IIC]-beta-CFT

Examples

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Effect test

Embodiment 1

[0022] A dopamine transporter imaging agent prepared online[ 11 The method of C]-β-CFT, its used equipment such as figure 1 As shown, the steps are as follows:

[0023] (1) Weigh 0.05-0.1 mg of the precursor nor-β-CFT and add it to the reaction bottle 3 containing the acetone solution. The volume of the acetone solution in the reaction bottle 3 is 50-100 μL, of which 50 μL, 70 μL, and 100 μL can be selected , the amount of precursor nor-β-CFT can be 0.05 mg or 0.075 mg or 0.1 mg, the reaction bottle 3 is placed in the activity meter 4, and the activity meter 4 is equipped with an ice bath to maintain the temperature of the reaction bottle at 4-10 ℃.

[0024] (2) Will 11 On-line conversion of C-iodomethane with trifluoromethylsulfonyl-Ag 11 C-trifluoromethylsulfonyl-methane, and 11 C-trifluoromethylsulfonyl-methane is passed into the reaction bottle 3, the radioactive material often opens the solenoid valve K3 to enter the reaction bottle 3, and reacts with the nor-β-CFT i...

Embodiment 2

[0028] A dopamine transporter imaging agent prepared online[ 11 The method of C]-β-CFT, its used equipment such as figure 2 As shown, the steps are as follows:

[0029] (1) Weigh 0.05-0.1 mg of the precursor nor-β-CFT, and dissolve it with DMSO solution. The volume of the DMSO solution is 50-100 μL, of which 50 μL, 70 μL, and 100 μL can be selected. The precursor nor-β-CFT The dosage can be 0.05mg or 0.075mg or 0.1mg, put the DMSO solution dissolved in nor-β-CFT into a 1×200mm stainless steel spiral tube 3 for injection, and dry the excess liquid with nitrogen, and the stainless steel spiral tube 3 Placed in the activity meter 4, an ice bath is provided in the activity meter 4 to maintain the temperature of the stainless steel spiral tube 3 at 4-10°C.

[0030] (2) Will 11 On-line conversion of C-iodomethane with trifluoromethylsulfonyl-Ag 11 C-trifluoromethylsulfonyl-methane, and 11 C-trifluoromethylsulfonyl-methane passes into the stainless steel spiral tube 3, the radi...

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Abstract

A process for equipment for preparing the radioactive medicine [11C]-beta-CFT used to diagnose the early Parkinson's disease by PET method is disclosed. Said process includes reaction between 11C-iodomethane and triflate-Ag to obtain 11C-triflate-methane, reacting no the actone solution containing nor-beta-CFT to obtain coarse product, separating-purifying by C-18 column, and eluting it in bottle.

Description

technical field [0001] The invention relates to the preparation of positron radiopharmaceuticals in the field of nuclear medicine, in particular to radiodiagnostic drugs for early diagnosis of Parkinson's disease (PD) used in positron tomography (PET) diagnosis[ 11 C]-β-CFT preparation method and equipment. Background technique [0002] PD is a degenerative disease of substantia nigra-striatum DA neurons and pathways, which changes the DA receptors of the anterior and posterior membranes. Changes in DAT are more sensitive and direct than changes in receptors. The more successful DAT tracers are CIT and CFT series, among which β-CIT has the highest affinity with DAT (Ki=1.4nM), but it has the same high affinity with other receptors, and the striatum and the surrounding Tissue count ratio is not high. use 18 F-labeled FP-β-CIT and FE-β-CIT can prolong the time from injection to imaging to increase the uptake ratio of striatum to cerebellum, generally 18 Imaging of F-FP-β-...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K51/00A61P25/28
Inventor 张锦明田嘉禾
Owner GENERAL HOSPITAL OF PLA