Unlock instant, AI-driven research and patent intelligence for your innovation.

A carrier-free [ * Preparation method and application of i]mibg

A clinical application, carrier-free technology, applied in the field of radiopharmaceuticals and nuclear medicine, can solve the problems that it is not suitable for clinical application, MIBG cannot be directly injected into the human body, etc., and achieve the effect of high yield, easy operation and high yield

Inactive Publication Date: 2017-08-15
JIANGSU INST OF NUCLEAR MEDICINE
View PDF2 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] For this reason, the technical problem to be solved by this invention is [ * I] MIBG can not be directly injected into the human body, is not suitable for clinical application, and then provides a carrier-free suitable for clinical application[ * I] preparation method and application of MIBG

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • A carrier-free [ <sup>*</sup> Preparation method and application of i]mibg
  • A carrier-free [ <sup>*</sup> Preparation method and application of i]mibg
  • A carrier-free [ <sup>*</sup> Preparation method and application of i]mibg

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0041] The preparation routes of the following examples of the present invention are as follows:

[0042]

[0043] The instrument models involved in the following embodiments include:

[0044] HPLC, the model is waters sunfire, produced in the United States;

[0045] Radioactive activity meter, model is CALIRAD ISOTOPE CALIBRATOR CRC-250, produced by VICTOREEN company, the United States;

[0046] γ-counter, the model is γ-counter 2480, manufactured by PE Company, USA;

[0047] Ultraviolet detector 2487 is produced by waters company;

[0048] Infrared spectrometer, the model is IR Bruker TENSOR-27, produced in Germany;

[0049] NMR instrument, model Bruker AvanceⅢ400, produced in Germany;

[0050] Mass spectrometer, the model is SQ Detector2, produced in the United States;

[0051] The isotope detector, the model is Radiomatic 610TR, produced by PE Company.

Embodiment 1

[0053] This example prepares carrier-free [ 123 I] The method of MIBG is as follows:

[0054] Take 100 μg (0.228 μmol) of 3-(tributyltin-based)-benzylguanidine represented by the formula A-I and add it to 150 μL of methanol solvent, and add the above mixed solution to 130 μL of sodium dihydrogen phosphate buffer solution with a pH value of 3.5 , and then freeze-dry the above mixture to obtain a freeze-dried powder. The freeze-drying procedure is as follows: the above-mentioned mixture is pre-frozen at minus 40°C for 6 hours, and then kept in vacuum for 2 hours, and the temperature is raised to minus 20°C. Keep it for 2 hours, then raise the temperature to minus 10°C and keep it for 12 hours, then raise the temperature to 10°C and keep it for 2 hours, finally raise the temperature to 25°C and keep it for 5 hours, take it out of the pot, and you can get frozen dry powder; 0.7 mL of 1.0 mCi of Na 123 I, and add 200 μL of a mixed solution containing 80mmoL / L acetic acid solution...

Embodiment 2

[0057] This example prepares carrier-free [ 124 I] The method of MIBG is as follows:

[0058] Take 40 μg (0.091 μmol) of 3-(tributyltin-based)-benzylguanidine represented by the formula A-I and add it to 100 μL of ethanol solvent, and add the above mixed solution to 100 μL of potassium dihydrogen phosphate buffer solution with a pH value of 8.0 , and then freeze-dry the above mixture to obtain a freeze-dried powder. The freeze-drying procedure is as follows: the above-mentioned mixture is pre-frozen at minus 40°C for 6 hours, and then kept in vacuum for 2 hours, and the temperature is raised to minus 20°C. Keep it for 2 hours, then raise the temperature to minus 10°C and keep it for 12 hours, then raise the temperature to 10°C and keep it for 2 hours, finally raise the temperature to 25°C and keep it for 5 hours, take it out of the pot, and you can get frozen dry powder; 3 mL of 0.1 mCi of Na 124 I, and add 100 μL of a mixed solution containing 120mmoL / L acetic acid solution...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention provides a carrier-free [ * I] the preparation method of MIBG, by dissolving tributyltin benzylguanidine in alcoholic solvent and adding in an appropriate amount of phosphate buffer solution to freeze-dry to obtain freeze-dried powder, then the powder after the freeze-drying is added to containing * In the aqueous solution of I ion, then add oxidizing agent and acid buffer solution to react, because the lyophilized powder of tributyltin benzylguanidine is insoluble in water, so after the reaction is completed, unreacted tributyltin benzylguanidine can be easily removed in the reaction solution, owned[ * I] MIBG not only yield is high, and labeling rate is high, and unreacted tin precursor and the by-product of tin after reaction can be removed completely easily, do not contain impurity, make the carrier-free [ * I] MIBG can be directly injected into the human body, which is more suitable for clinical application.

Description

technical field [0001] The invention belongs to the technical field of radiopharmaceuticals and nuclear medicine, in particular to a carrier-free [ * I] preparation method and application of MIBG. Background technique [0002] Meta-iodobenzylguanidine (MIBG) belongs to the analogue of guanethidine, which can be concentrated in the adrenal medulla and is a homologue of the norepinephrine neurotransmitter (NE), with the help of NE, it can be enriched for sympathetic Absorbed by nerve cells, it is a very valuable carrier in the diagnosis and treatment of myocardial abnormalities and neuroendocrine tumors. widely used in the prior art to 131 I-labeled MIBG for imaging and diagnosis and treatment of neuroendocrine tumors. [0003] Now clinically used abroad 131 I] MIBG is mostly passed 131 I and MIBG are prepared by the method of isotope exchange. The medicine prepared by this method contains a large amount of unlabeled MIBG carrier, not only the labeling rate is low, but al...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): A61K51/04A61K101/02
Inventor 王刚陈志明吴二明汪洋黄荷云
Owner JIANGSU INST OF NUCLEAR MEDICINE