99mTc(III) complex containing arylboronic acid as well as kit formula thereof and application thereof

An arylboronic acid, 99mtc technology, applied in the field of 99mTc complexes, can solve the problems of limiting the clinical use of Tc-Teboroxime, lack of linear relationship of local myocardial blood flow, unfavorable evaluation of myocardial vitality, etc., achieving high labeling rate and radiochemical purity, Inexpensive, easy-to-get results

Inactive Publication Date: 2017-05-31
FUWAI HOSPITAL CHINESE ACAD OF MEDICAL SCI & PEKING UNION MEDICAL COLLEGE
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Problems solved by technology

99m Tc-Sestamibi is currently a radioactive tracer commonly used in the diagnosis of CAD in nuclear medicine, but a major disadvantage is that the first extraction rate is low. When the myocardial blood flow > 2.5mL / min / g Flow lacks a linear relationship
Currently, in all 99m Tc-labeled radioactive tracer for myocardial perfusion, 99m The first pass rate of Tc-Teboroxime is the highest, but the myocardial retention is poor. About 60% of the radioactivity is cleared from the myocardium after 5 minutes after injection. When the myocardial blood flow reaches 2.5mL / min / g, the myocardial uptake value and local blood flow are in There is a linear relationship within 5 minutes after injection, which is not conducive to the evaluation of myocardial viability
These factors limit 99m Clinical application of Tc-Teboroxime

Method used

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  • 99mTc(III) complex containing arylboronic acid as well as kit formula thereof and application thereof
  • 99mTc(III) complex containing arylboronic acid as well as kit formula thereof and application thereof
  • 99mTc(III) complex containing arylboronic acid as well as kit formula thereof and application thereof

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Embodiment Construction

[0030] Below to 99m TcCl(CDO)(CDOH) 2 B(F-5F) is taken as an example, and the present invention is described in detail through examples.

[0031] 1. 99m TcCl(CDO)(CDOH) 2 Preparation of B(F-5F)

[0032] Contains 2mg CDOH 2 , 4-5mg 5-formaldehyde furan-2-boronic acid, 60mg SnCl 2 2H 2 Add 1.o mL 99m TCO 4 - solution (370-1110 MBq). Heat the above vial to 100°C and react for 10-15min. Then the reaction solution was diluted to 3.7 MBq / mL with physiological saline containing about 20% propylene glycol.

[0033] The radiochemical purity of the diluted solution was determined by high performance liquid chromatography (HPLC) or rapid thin layer chromatography (ITLC). The specific apparatus and conditions are as follows: HPLC assay uses Agilent HP-1100 HPLC system (Agilent Technologies), -ram IN / US probe (Tampa, FL) and Zorbax C 8 Chromatographic column (4.6mm×250mm, Agilent Technologies). HPLC condition is A phase is 10mM NH 4 OAc buffer, pH=6.8; phase B is methanol, t...

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Abstract

The invention provides a 99mTc(III) complex containing arylboronic acid. A molecular formula of the 99mTc(III) complex is 99mTcC1(CDO)(CDOH)2B(F-R), wherein F is furyl and R is methoxyl, formaldehyde or hydroxymethyl. The compound has the characteristics of simple preparation, low price, high labeling rate, high radiochemical purity, high target to non-target ratio, high heart uptake value, long residence time and the like, and can be used as a novel technetium-99m labeled myocardial perfusion imaging agent which is applied to the technical fields of radiopharmaceutical chemistry and clinical nuclear medicines.

Description

technical field [0001] The present invention relates to 99m Tc complexes, specifically relate to a kind of aryl boronic acid-containing 99m Tc(III) complexes and kit formulations and applications for preparing said complexes. Background technique [0002] Cardiovascular disease (CAD) is one of the most serious diseases threatening human health. In my country, the morbidity and mortality of CAD are on the rise. At present, it is estimated that there are 290 million people with cardiovascular disease in the country. In 2012, the data released by "China Cardiovascular Disease Report 2013" showed that the mortality rate of cardiovascular disease in 2012 was 255 / 100,000. An estimated 3.5 million people die from cardiovascular disease each year. In 2012, cardiovascular disease accounted for 41.1% of urban residents' disease deaths, and 38.7% in rural areas, ranking first among various diseases and higher than tumors and other diseases. [0003] Cardiovascular disease (CAD) is...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F13/00C07B59/00A61K51/04A61K103/10
CPCA61K51/0482C07B59/004C07B2200/05C07F13/005
Inventor 赵祚全汪蕾方纬
Owner FUWAI HOSPITAL CHINESE ACAD OF MEDICAL SCI & PEKING UNION MEDICAL COLLEGE
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