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Application of radioisotope-labeled meso-position dianthrone compound in preparation of drug for detecting myocardial activity

A radioisotope, myocardial activity technology, applied in the field of medicine, can solve the problems of wrong use of treatment methods, inability to accurately judge the state of heart cells, delay of disease and other problems

Inactive Publication Date: 2013-10-09
JIANGSU PROVINCE INST OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the limitations of each method, it is impossible to accurately judge the state of heart cells, resulting in the wrong use of treatment methods and delaying the treatment.

Method used

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  • Application of radioisotope-labeled meso-position dianthrone compound in preparation of drug for detecting myocardial activity
  • Application of radioisotope-labeled meso-position dianthrone compound in preparation of drug for detecting myocardial activity
  • Application of radioisotope-labeled meso-position dianthrone compound in preparation of drug for detecting myocardial activity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Example 1 Preparation of Myocardial Infarction Rat Model

[0019] SD rats with a body weight of 200-300 g were intraperitoneally injected with 10% chloral hydrate (0.3 mL / 100 g). After anesthesia, the rats were fixed on their backs on the mouse table, connected to a small animal ventilator through orotracheal intubation, the respiratory rate was 60-80 times / min, the respiratory ratio was 1 / 1, and the tidal volume was 4mL / 100g. After disinfecting the skin with povidone iodine, the chest was opened along the 3rd and 4th intercostal spaces along the left sternum to expose the heart, the pericardium was peeled off, a thread was threaded parallel to the left atrial appendage at the interventricular groove, and the left anterior descending coronary artery was ligated. After ligation, the air in the chest cavity was pumped out, the negative pressure in the chest cavity was restored, the chest cavity was quickly sutured, the endotracheal tube was withdrawn, and 160,000 U of pen...

Embodiment 2

[0020] Example 2 Preparation of Iodine-131 Labeled Rhubarb Dicanthrone A

[0021] Weigh 13mg of Rhubarb palmatum dianthrone A (powder), dissolve in 1.0ml DMSO, oscillate to obtain 1.3mg / ml Rheum palmatum dianthrone ADMSO solution. Take 200 μl of 1.3 mg / ml rhubarb palmatum dianthrone A solution, add 800 μl of DMSO solution, shake well, and obtain 0.26 mg / ml rhubarb palmatum dianthrone A solution. Add 400 μl of rhubarb palmatum dianthrone ADMSO solution with a concentration of 0.26 mg / ml into the prepared coated tube with a content of 400 μg of lodogen, add 100 μl of 200 μCi Na iodine-131 solution, shake well and heat in a water bath at 45°C. After reacting for about 90 minutes, after the reaction was terminated, the labeling rate was measured by TLC method, Whatman filter paper was used as the carrier, and 0.1mol / L HCl was used as the mobile phase for development.

Embodiment 3

[0022] Example 3 Distribution of Iodine-131 Labeled Rhubarb Danthrone A on Myocardial Infarction Rat Model

[0023] The iodine-131-labeled Rheum palmatum dianthrone A solution prepared in Example 2 was added to PEG400 and diluted with propylene glycol (1:1). Six myocardial infarction model rats were taken, and 100 μCi of iodine-131-labeled rhubarb palmate dianthrone A solution (radiochemical purity: 90%) was intravenously injected into each rat. After 24 hours, the model rats were euthanized, and various organs (thyroid, kidney, liver, spleen, lung, normal myocardium, infarcted myocardium, small intestine, stomach, muscle and fur, etc.) were taken, weighed and radioactivity was measured with a gamma counter. , after decay correction, the results were expressed as the radioactive uptake per gram of organ or tissue as a percentage of the total injected dose (%ID / g).

[0024] After iodine-131 labeled rhubarb palmatum dianthrone A24h, the distribution value in necrotic myocardium...

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Abstract

The invention relates to the drug field, in particular relates to the application field of a meso-position dianthrone compound, and more specifically relates to application of a radioisotope-labeled meso-position dianthrone compound in preparation of a drug for detecting myocardial activity. The specific bonding force of the radioisotope-labeled meso-position dianthrone compound is utilized to the myocardial necrotic cells, and a radiation source generated by radioisotope is utilized, and a detector is used in a combined manner for achieving the purpose of effectively detecting the myocardial necrotic cells.

Description

technical field [0001] The present invention relates to the field of medicines, in particular to the application field of median dianthrone compounds, more specifically to the application of radioactive isotope-labeled median dianthrone compounds in the preparation of drugs for detecting myocardial activity . Background technique [0002] Myocardial infarction is a disease with high morbidity and mortality among cardiovascular diseases. After myocardial infarction, the cells in the infarcted area will degenerate and die, forming necrotic tissue, which cannot be regenerated. The area of ​​necrotic tissue is the most important diagnostic index of acute myocardial infarction. There is about 40% viable myocardium in the infarct area of ​​acute myocardial infarction, which may recover or spontaneously restore myocardial vitality after revascularization. Accurately identifying whether the ischemic myocardium is reversible in patients with myocardial infarction plays a decisive ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/04A61K101/02A61K103/10A61K103/36
Inventor 张健倪以成孙自平蒋翠花李玥江骁高萌姚楠汪俊虎吉云
Owner JIANGSU PROVINCE INST OF TRADITIONAL CHINESE MEDICINE
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