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Prostatic cancer diagnosis developer and preparation method thereof

A technology for diagnosing imaging and prostate cancer, applied in the field of nuclear medicine, can solve the problems of false positives, low specificity, low sensitivity, etc., and achieve the effects of high uptake, simple labeling method, high sensitivity and specificity

Inactive Publication Date: 2018-06-22
XIANGYA HOSPITAL CENT SOUTH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Currently, radioactive diagnostic imaging agents for prostate cancer are 18 F-FDG, but this diagnostic imaging agent has the defects of low sensitivity, low specificity and easy to cause false positive

Method used

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  • Prostatic cancer diagnosis developer and preparation method thereof
  • Prostatic cancer diagnosis developer and preparation method thereof
  • Prostatic cancer diagnosis developer and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Using a proton cyclotron 18 O(p,n) 18 The F reaction produces an activity of 100mCi 18 f - ; the resulting 18 f - Transfer to the anion exchange column QMA through pipeline (QMA is READI-CLING TM type column, the column body is hollowed out, and about 1 / 5Plus C18 column filler is refilled) to capture, after the capture is completed, use N 2 Blow dry the QMA, then rinse with 0.3ml PH=4.2 acetic acid-sodium acetate buffer solution, elute to get 18 f - The buffer solution, its activity is 90mCi;

[0022] to 0.3ml 18 f - Add 300ug NOTA-modified neurotensin, 0.5ml acetonitrile and 0.03ml 0.4M AlCl to the buffer solution 3 solution and reacted at 80°C for 10min, then added 5ml of deionized water to quench the reaction, and then passed the reaction solution over Al 2 o 3 Column, obtain filtrate;

[0023] Pass the filtrate through C 18 Plus column was enriched, and then rinsed with 2mL ethanol and 10mL normal saline in sequence, and the rinse solution was passed t...

Embodiment 2

[0039] Using a proton cyclotron 18 O(p,n) 18 The F reaction produces an activity of 100mCi 18 f - ,; then the generated 18 f - Transfer to the anion exchange column QMA through pipeline (QMA is READI-CLING TM type column, the column body is hollowed out, and about 1 / 5Plus C18 column filler is refilled) to capture, after the capture is completed, use N 2 Blow dry the QMA, then rinse with 0.3ml PH=4.2 acetic acid-sodium acetate buffer solution, elute to get 18 f - The buffer solution, its activity is 80mCi;

[0040] to 0.3ml 18 f - Add 300ug NOTA-modified neurotensin, 0.5ml acetonitrile and 0.03ml 0.4M AlCl to the buffer solution 3 solution and reacted at 80°C for 10min, then added 5ml of deionized water to quench the reaction, and then passed the reaction solution over Al 2 o 3 Column, obtain filtrate;

[0041] Pass the filtrate through C 18 Plus column was enriched, and then rinsed with 2mL ethanol and 10mL normal saline in sequence, and the rinse solution was pa...

Embodiment 3

[0043] Using a proton cyclotron 18 O(p,n) 18 The activity of F reaction is 110mCi 18 f - ,; then the generated 18 f - Transfer to the anion exchange column QMA through pipeline (QMA is READI-CLING TM type column, the column body is hollowed out, and about 1 / 5Plus C18 column filler is refilled) to capture, after the capture is completed, use N 2 Blow dry the QMA, then rinse with 0.3ml PH=4.2 acetic acid-sodium acetate buffer solution, elute to get 18 f - The buffer solution, its activity is 84mCi;

[0044] to 0.3ml 18 f - Add 300ug NOTA-modified neurotensin, 0.5ml acetonitrile and 0.03ml 0.4M AlCl to the sodium acetate solution 3 solution and reacted at 80°C for 10min, then added 5ml of deionized water to quench the reaction, and then passed the reaction solution over Al 2 o 3 Column, obtain filtrate;

[0045] Pass the filtrate through C 18 Plus column was enriched, and then rinsed with 2mL ethanol and 10mL normal saline in sequence, and the rinse solution was pas...

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Abstract

The invention discloses a prostatic cancer diagnosis developer, which has a structural formula shown in the description. The close relevancy of neurotensin and prostatic cancer is utilized; the neurotensin is marked by A1-18F; the prostatic cancer diagnosis developer is obtained. The diagnosis developer has excellent pharmacokinetic properties; the intake quantity on the prostate tumor is high; high sensitivity and specificity are realized on the prostatic cancer diagnosis; false positive cannot easily occur. In addition, a marking method is simple; after 6h from the marking, the radiochemicalpurity is still as high as 99 percent.

Description

technical field [0001] The invention belongs to the technical field of nuclear medicine, and in particular relates to a diagnostic imaging agent for prostate cancer and a preparation method thereof. Background technique [0002] Prostate cancer is currently the most common tumor among European and American men, and more than 200,000 people die of prostate cancer every year. The incidence of prostate cancer in my country shows a clear upward trend. Since the PSA screening mechanism has not been established, when the diagnosis is confirmed, it is often already in the middle and late stages. The 5-year survival rate of early low-risk prostate cancer after treatment can reach 82%, and early diagnosis is crucial for the prognosis of prostate cancer. [0003] The methods currently used for cancer diagnosis mainly include X-ray (CT), ultrasound (US), magnetic resonance imaging (MRI) and nuclear medicine PET. Among them, US and MRI are based on the analysis of the anatomical struc...

Claims

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Application Information

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IPC IPC(8): A61K51/08
CPCA61K51/085
Inventor 胡硕周明李子博
Owner XIANGYA HOSPITAL CENT SOUTH UNIV
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