Preparation of 131I-thyroid stimulating hormone (TSH) and application thereof

A technology of thyroid stimulating hormone and 131I-TSH, which is applied in the field of medical use of 131I-TSH, can solve the problems of reduced iodine intake, decreased protein expression, waste of social resources and medical resources, etc., and achieves stable markers and simple preparation process. Effect

Inactive Publication Date: 2010-07-28
JIANGSU INST OF NUCLEAR MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, some poorly differentiated and dedifferentiated thyroid cancer cells lose their unique functions and characteristics, such as the decreased expression of sodium / iodide symporter (NIS) protein and decreased iodine uptake. Diffuse lesions, first use 131 I blind treatment, the second is to take tumor differentiation inducers, such as all-trans retinoic acid, etc.
However, based on domestic and foreign researches, the current method for these poor / poorly differentiated thyroid cancer patients, through 131 The means of I cannot achieve the purpose of inhibiting the growth of thyroid cancer cells, controlling and treating thyroid cancer, which brings great difficulties to the clinical treatment of thyroid cancer and causes a waste of social and medical resources.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1: 131 Preparation of I-TSH (chloramine-T method)

[0021] 5 μg thyrotropin was dissolved in 20 μL 0.2mol / L pH 7.4 PBS, and 20 μL Na 131 I (0.5-2mCi), 20μL 1mg / mL chloramine-T, shake at room temperature for 30-60 seconds, add 100μL 2mg / mL sodium metabisulfite to stop the reaction. The reaction solution was loaded onto a fully equilibrated and saturated PD-10 column with 50mmol / L pH 7.4 PBS (containing 0.5% BSA), collected step by step at 1mL / tube, and the protein peak was obtained.

Embodiment 2

[0022] Example 2: 131 Preparation of I-TSH (peroxide oxidation method)

[0023] 5 μg thyrotropin was dissolved in 20 μL 0.2mol / L pH 7.4 PBS, and 20 μL Na 131 I (0.5-2mCi), 20 μL 3% hydrogen peroxide, shake at room temperature for 30-60 seconds, let stand for 15 minutes, add 100 μL 2mg / mL sodium metabisulfite to terminate the reaction. The reaction solution was loaded onto a fully equilibrated and saturated PD-10 column with 50mmol / L pH 7.4 PBS (containing 0.5% BSA), collected step by step at 1mL / tube, and the protein peak was obtained.

Embodiment 3

[0024] Example 3: 131 Preparation of I-TSH (Iodogen method)

[0025] 5 μg thyrotropin was dissolved in 20 μL 0.2mol / L pH 7.4 PBS, added to the Eppendorf tube coated with 2 μg Iodogen, and 20 μL Na 131 I (0.5-2mCi), shake the reaction at room temperature for 30-60 seconds, let it stand for 20 minutes, suck out the reaction solution to terminate the reaction, and apply the reaction solution to a well-balanced and saturated 50mmol / L pH7.4PBS (containing 0.5%BSA) PD-10 column, collect in steps at 1mL / tube, and take the protein peak.

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PUM

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Abstract

The invention relates to the preparation of 131I-thyroid stimulating hormone (TSH) and an application thereof, belonging to the field of radionuclide therapeutic drugs. The compound 131I-thyroid stimulating hormone is a radioiodine marker for thyroid stimulating hormone with pathoclisis in vivo acting on thyrocyte. A preparation method of the 131I-thyroid stimulating hormone comprises the following steps of: carrying out iodine 131 marking on the thyroid stimulating hormone by utilizing a chloramine-T method, a peroxide oxidation method or an iodogen method, and introducing radionuclide iodine 131 for treatment into tyrosine residues in thyroid stimulating hormone molecules. The marking rate of the prepared 131I-TSH is 85.9 percent, the radiochemical purity after purification achieves more than 90 percent, and the prepared 131I-TSH can be stored stably for more than one week at room temperature; the 131I-TSH is mainly metabolized through the liver and excreted through the kidneys; the percentage of ID/g of the 131I-TSH in the thyroid gland is not obviously reduced in four hours; and the 131I-TSH can be concentrated in thyroid gland issues sealed by an iodine solution. Concerning low/undifferentiated thyroid tumours incapable of iodine uptake, the 131I-TSH can increase the radioiodine uptake of thyroid gland cancer cells, and the radioiodine 131 can be chosen for treatment.

Description

technical field [0001] 131 I-thyroid-stimulating hormone ( 131 I-TSH) preparation and its application in the treatment of low / dedifferentiated thyroid cancer, the present invention relates to the field of medicine, in particular to 131 Medicinal uses of I-TSH. Background technique [0002] Thyroid cancer is currently the most common malignant tumor of the endocrine system. Clinically, there are mainly surgical resection, radioactive iodine, and thyroid-stimulating hormone suppression, among which the application of radioactive iodine has attracted more and more attention. However, some poorly differentiated and dedifferentiated thyroid cancer cells lose their unique functions and characteristics, such as the decreased expression of sodium / iodide symporter (NIS) protein and decreased iodine uptake. Diffuse lesions, first use 131 I blind treatment, the second is to take tumor differentiation inducers, such as all-trans retinoic acid and so on. However, based on domestic a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/59C07K1/13A61K51/08A61P35/00A61K101/02
Inventor 俞惠新包建东谭成林秀峰张莉赵新灿
Owner JIANGSU INST OF NUCLEAR MEDICINE
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