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Application of radioisotope-labeled monoanthranuclear anthraquinone compounds in the preparation of drugs for detecting myocardial activity

A radioactive isotope, monoanthranuclear anthraquinone technology, applied in the field of medicine, can solve problems such as wrong use of treatment methods, inability to accurately judge the state of heart cells, and delays in disease progression

Active Publication Date: 2017-05-24
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 monoanthranuclear anthraquinone compounds in the preparation of drugs for detecting myocardial activity
  • Application of radioisotope-labeled monoanthranuclear anthraquinone compounds in the preparation of drugs for detecting myocardial activity
  • Application of radioisotope-labeled monoanthranuclear anthraquinone compounds in the preparation of drugs for detecting myocardial activity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Example 1 Preparation of Myocardial Infarction Rat Model

[0020] 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the negative pressure in the chest cavity was restored, the chest cavity was quickly sutured, the endotracheal tube was withdrawn, and 160,000 U of pen...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

[0021] Example 2 Preparation of iodine-131 labeled rhein

[0022] Weigh 0.4 mg rhein, dissolve it in 182.8 μl DMSO, and shake it well to obtain a 2.2 mg / ml rhein DMSO solution. Add 182.8 μl of rhein DMSO solution with a concentration of 2.2 mg / ml into a coated tube with an Iodogen content of 40 μg, add 45.7 μl of 17500 μCi Na iodine-131 solution, and then add 15 μl of PBS, shake well, and place in a water bath at 45°C The reaction was heated for about 90 minutes. After the reaction was terminated, the labeling rate was measured by TLC method. The labeling rate was greater than 95%, indicating that the labeling was successful. Labeling rate measurement method: the reaction solution was determined by paper chromatography, Whatman filter paper was used as the carrier, and 0.1mol / L HCl was used as the mobile phase for development. Labeling rate was measured by paper chromatography. Free 131I was distributed at the front of the solvent, while 131I-labeled rhein remained at the ori...

Embodiment 3

[0023] Example 3 Distribution of iodine-131-labeled rhein on rat model of myocardial infarction

[0024] The iodine-131 labeled rhein solution prepared in Example 2 was diluted with PEG 400-propylene glycol (1:1). Six myocardial infarction model rats were taken, and each rat was intravenously injected with 100 μCi of iodine-131-labeled rhein solution (radiochemical purity: 90%). After 12 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 separately, 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).

[0025] After iodine-131 labeled rhein for 12 hours, the distribution value in necrotic myocardium was 0.78%ID / g, and that in normal myocardium was 0.15%ID / g, and the d...

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Abstract

The present invention relates to the field of medicine, in particular to the application field of monoanthranuclear anthraquinone compounds, and more specifically to the application of radioisotope-labeled monoanthranuclear anthraquinone compounds in the preparation of drugs for myocardial activity detection. The radioactive isotope-labeled monoanthranuclear anthraquinone compound has a specific binding force for myocardial necrosis cells, and the radiation source generated by the radioisotope, and the purpose of effectively detecting myocardial necrosis cells is achieved through the combined use of detectors.

Description

technical field [0001] The present invention relates to the field of medicine, in particular to the application field of monoanthranuclear anthraquinone compounds, and more specifically to the application of radioisotope-labeled monoanthranuclear anthraquinone compounds in the preparation of drugs for myocardial activity detection. 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 infarc...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K51/04A61K101/02A61K103/10A61K103/36
Inventor 张健高萌蒋翠花王小宁张东建刘雪娇黄德健王琴
Owner JIANGSU PROVINCE INST OF TRADITIONAL CHINESE MEDICINE
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