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18F-E[c(RGDyk)2], medicine box used for automatic production thereof, and preparation method and use of medicine box

A technology of 18F-E and 1.18F-E, applied in the direction of peptides, can solve the problems such as the limitation of popularization and application of imaging agents, and achieve the effects of good pharmacokinetic characteristics, good retention and convenient operation.

Active Publication Date: 2013-09-11
JIANGSU INST OF NUCLEAR MEDICINE
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, due to the constraints of traditional preparation techniques, the clinical application of these imaging agents is limited.

Method used

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  • 18F-E[c(RGDyk)2], medicine box used for automatic production thereof, and preparation method and use of medicine box
  • 18F-E[c(RGDyk)2], medicine box used for automatic production thereof, and preparation method and use of medicine box
  • 18F-E[c(RGDyk)2], medicine box used for automatic production thereof, and preparation method and use of medicine box

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Embodiment Construction

[0031] The preferred embodiments of the present invention will be described below in conjunction with the accompanying drawings. It should be understood that the preferred embodiments described here are only used to illustrate and explain the present invention, and are not intended to limit the present invention.

[0032] 1. Preparation of 100 automated production 18 Kit for F-E[c(RGDyk)2]

[0033] method 1:

[0034] 1) Dissolve 100mg E[c(RGDyk)2]-NO2 in 100mL ethanol and mix well;

[0035] 2) After aseptically filtering the solution prepared in step 1, divide it into 100 tubes of controlled antibiotic bottles, pass the divided antibiotic bottles into the cold room shelf of the freeze dryer through the transfer window, close the door, and freeze dry for 24 hours. hours, the gland is sealed;

[0036] 3) Dissolve 1.5g crown ether K222 in 90mL acetonitrile, add 10mL 30mg / mL K 2 CO 3 Aqueous solution, mixed evenly, sterile filtered, and divided into 1mL / bottle crown ether K22...

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Abstract

The invention discloses 18F-E[c(RGDyk)2], a medicine box used for automatic production thereof, and a preparation method and use of the medicine box, relates to a polyethylene terephthalate (PET) developer and a preparation method and use thereof and relates to the technical field of radiative medicines and nuclear medicines. The medicine box contains a raw material reagent A and a raw material reagent B. A bottle A contains E[c(RGDyk)2]-NO2; and A bottle B contains acetonitrile solution of crown ether K222 / K2CO3. The 18F-E[c(RGDyk)2] prepared by the medicine box has high absorbing performance and excellent retaining performance in model mouse tumor, and has a very high target / non target ratio, excellent pharmacokinetic characteristic and high biological performance, and can completely meet the requirements of PET developer of tumour integrin alphavbeta3 receptor.

Description

technical field [0001] The invention relates to a PET imaging agent and its preparation method and application, and belongs to the technical field of radiopharmaceuticals and nuclear medicine. Background technique [0002] Positron emission tomography (PET) is a cutting-edge technology for biomedical research and clinical diagnosis in the 21st century. Gain insight into the activity of labeled drugs in normal or sick people. Compared with SPECT, PET has high resolution and can be quantitatively analyzed, which has obvious advantages. [0003] 18 F has the characteristics of close to 100% positron efficiency, low positron energy (0.64 MeV) and relatively short physical half-life (t1 / 2=109.7 minutes), and is an ideal PET imaging nuclide. The polypeptide has the advantages of rapid tissue penetration, rapid clearance in the blood, low immunogenicity, etc., and is a suitable carrier for the preparation of PET imaging agents. Currently, peptides 18 The F-labeled process incl...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K7/52
Inventor 杨敏陈小元徐宇平潘栋辉罗世能王立振
Owner JIANGSU INST OF NUCLEAR MEDICINE
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