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Medicine box for preparing 99mTc complex and preparation method and use thereof

A technology of 99mtc and complexes, which is applied in the field of new 99mTc mixed complexes, can solve the problems of tumor imaging interference, myocardial imaging interference, and high bone uptake, and achieve slow myocardial absorption and clearance, high myocardial absorption, and low blood background Effect

Inactive Publication Date: 2009-01-07
BEIJING NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The disadvantage is that the bone uptake is relatively high, which interferes with the imaging of some tumors
However, the drug has high uptake in the liver, which interferes with imaging of the myocardium

Method used

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  • Medicine box for preparing 99mTc complex and preparation method and use thereof
  • Medicine box for preparing 99mTc complex and preparation method and use thereof
  • Medicine box for preparing 99mTc complex and preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1: the preparation of A kit

[0029] The kit is used to prepare [ 99m Tc(CO)3 (OH 2 ) 3 ] + intermediate. The composition of the kit is: 5 mg of sodium carbonate, 5 mg of vitamin C, 10 mg of sodium borohydride, 15 mg of potassium sodium tartrate, 20 mg of lactose and 10 ml of 1 standard atmosphere of CO gas. Dissolve the above-mentioned substances in 2 milliliters of sterile water for injection, filter and sterilize with a 0.22 μm microporous membrane, put the filtrate in a sterile penicillin vial, then place the penicillin vial in a lyophilizer, and control the temperature to Pre-freeze at -45~-40°C for 2 hours, then carry out vacuum drying, naturally generate temperature and finally control the temperature at 25-28°C, keep it for 4 hours, the vacuum degree is 0.7Pa, and then fill the above-mentioned freeze-drying system with CO for 1 minute , and then the penicillin vial containing the white freeze-dried powder was sealed with a rubber stopper, further...

Embodiment 2

[0030] Embodiment 2: the preparation of B kit

[0031] The kit is used to prepare 99m Tc(CO) 3 DMSA intermediate. The composition of the kit is: 5 mg DMSA and 5 mg vitamin C. Dissolve the above-mentioned substances in 2 milliliters of sterile water for injection, filter and sterilize with a 0.22 μm microporous membrane, put the filtrate in a sterile penicillin vial, then place the penicillin vial in a lyophilizer, and control the temperature to -45~-40°C, pre-freeze for 2 hours, then carry out vacuum drying, naturally increase the temperature and finally control the temperature at 25-28°C, keep it for 4 hours, the vacuum degree is 0.7Pa, and then fill the above-mentioned freeze-drying system with nitrogen for 1 minute , and then the penicillin vial containing the white freeze-dried powder was sealed with a rubber stopper, further sealed with an aluminum cap, labeled, and stored in a refrigerator at 5-8°C.

Embodiment 3

[0032] Embodiment 3: the preparation of C kit

[0033] The kit is used to prepare 99m Tc(CO) 3 - DMSA-MIBI complex. The composition of the kit is: 1 mg MIBI, 5 mg tartaric acid and 5 mg vitamin C. Dissolve the above-mentioned substances in 2 milliliters of sterile water for injection, filter and sterilize with a 0.22 μm microporous membrane, put the filtrate in a sterile penicillin vial, then place the penicillin vial in a lyophilizer, and control the temperature to -45~-40°C, pre-freeze for 2 hours, then carry out vacuum drying, naturally increase the temperature and finally control the temperature at 25-28°C, keep it for 4 hours, the vacuum degree is 0.7Pa, and then fill the above-mentioned freeze-drying system with nitrogen for 1 minute , and then seal the penicillin vial containing the white freeze-dried powder with a rubber stopper, and then further seal it with an aluminum cap. After passing the quality inspection, label it and store it in a refrigerator at 5-8°C.

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Abstract

The invention relates to a medicine box used for preparing <99m>Tc complex, and a method for preparing novel <99m>Tc mixed ligand complex containing carbon monoxide (CO), 2, 3-dimercaptosuccinic acid (DMSA) and tetra (2-methoxy isobutyronitrile) cuprous (I) tetrafluoroborate complex salt (MIBI) by utilizing the medicine box. The medicine box comprises the following three medicine boxes: firstly, medicine box A which is composed of sodium carbonate, vitamin C, sodium borohydride, seignette salt, lactose and CO gas, and the weight ratio is (5-100):(5-100):(10-200):(15-300):(20-400):(10-200); secondly, medicine box B which is composed of DMSA and the vitamin C, and the weight ratio is (5-100):(5-100); and thirdly, medicine box C which is composed of tartaric acid, MIBI, and the vitamin C, and the weight ratio is (5-100):(1-20):(5-100). The preliminary biological experiments show that the mixed ligand complex <99mTc(CO)3(DMSA)(MIBI)> prepared by utilizing the medicine box has good myocardial uptake and detention, the uptake in the liver is greatly reduced, the fault that the liver uptake of the prior myocardial imaging agent <99m>Tc-MIBI is high can be overcome, and a higher heart / liver ratio can be achieved in 30 minutes after the administration, and thereby the medicine box is favorable for the myocardial imaging in the early stage.

Description

technical field [0001] The present invention relates to a method for preparing 99m The kit of Tc complex, and utilize this kit to prepare carbon monoxide (CO), 2,3-dimercaptosuccinic acid (DMSA) and tetrakis (2-methoxyisobutyronitrile) cuprous (I) tetrafluoroboric acid A new type of complex salt (MIBI) ligand 99m Tc mixed complex method. Background technique [0002] The diagnosis and treatment of tumors and myocardial perfusion imaging have always been the focus of radiopharmaceutical research, and 99m The development of Tc-labeled tumor imaging agents and myocardial perfusion imaging agents has also been a subject of general interest in nuclear medicine. [0003] 99m As a relatively mature pro-tumor imaging agent, Tc(V)-DMSA is effective for head and neck tumors, myeloma, thyroid cancer, malignant soft tissue tumors, expanded fibrous tumors, low-grade sarcoma, osteosarcoma, early lung cancer and its metastatic cancer. , medullary thyroid cancer, etc. have a relatively...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/04A61K103/10
Inventor 王学斌杨树业张现忠唐志刚张俊波陆洁
Owner BEIJING NORMAL UNIVERSITY
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