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Preparation capable of bone imaging and bone metastases tumor curing and preparation and application thereof

A technology of bone metastasis and bone imaging, which can be used in radioactive preparations in vivo, preparations for in vivo experiments, and medical preparations containing active ingredients, etc. good therapeutic effect

Active Publication Date: 2018-09-11
THE AFFILIATED HOSPITAL OF SOUTHWEST MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

At present, the commonly used nuclides in China include phosphorus-32 ( 32 P), strontium-89( 89 Sr) and samarium-153 ( 153 Sm), the toxicity of phosphorus-32 is relatively large, and it has dose-limiting bone marrow suppression, so it is rarely used now
Compared to 32P, 89 Sr can relieve bone pain to a certain extent, and its application can significantly reduce the usage rate of analgesic drugs. Combined with chemotherapy drugs, the curative effect is better, but its response cross section is very low, the production volume is small, the price is relatively expensive, and it cannot be used for imaging.
Members of the Sm lanthanides, 153 Sm can be used to label phosphate drugs, which can be used for both imaging and treatment, and the safety is better than the first two drugs, but 153 The short half-life of Sm (1.95 days) is not suitable for long-distance transportation, and the need for large doses in batch processing also limits its use

Method used

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  • Preparation capable of bone imaging and bone metastases tumor curing and preparation and application thereof
  • Preparation capable of bone imaging and bone metastases tumor curing and preparation and application thereof
  • Preparation capable of bone imaging and bone metastases tumor curing and preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

example 177

[0034] this example 177 The specific preparation method of Lu-ibandronic acid is as follows:

[0035] Add 1.5 mg of ibandronic acid to 177 Lu activity of 0.25mCi (10mCi / ml) 177 LuCl 3 In the solution, adjust the pH of the solution to 5 with hydrochloric acid, react at a temperature of 90° C. for 1 hour, sterilize and filter with a 0.22 μm sterile filter. The labeling rate was determined by thin layer paper chromatography (TLC).

[0036] Prepared in this example 177 The Lu-ibandronic acid product was 97% radiochemically pure.

example 2

[0038] this example 177 The specific preparation method of Lu-ibandronic acid is as follows:

[0039] Add 5 mg of ibandronic acid to 177 Lu activity of 2.5mCi (50mCi / ml) 177 LuCl 3 In the solution, adjust the pH of the solution to 5 with hydrochloric acid, react at a temperature of 60° C. for 2 hours, and use a 0.22 μm sterile filter to sterilize and filter. The labeling rate was determined by thin layer paper chromatography (TLC).

[0040] Prepared in this example 177 The radiochemical purity of the Lu-ibandronic acid product was 96.5%.

example 3

[0042] Add 5 mg of ibandronic acid to 177 Lu activity of 2.5mCi (50mCi / ml) 177 LuCl 3 In the solution, adjust the pH of the solution to 5 with hydrochloric acid, react at a temperature of 60° C. for 6 hours, and use a 0.22 μm sterile filter to sterilize and filter. The labeling rate was determined by thin layer paper chromatography (TLC).

[0043] Prepared in this example 177 The radiochemical purity of the Lu-ibandronic acid product was 95.4%.

[0044] Though the proportioning several reaction conditions of example 2 and example 3 can reach the radiochemical purity more than 95%, the required reactant consumption is big compared with optimal conditions (example 1), and the reaction time is longer, along with reaction Prolonging the time will not further improve the radiochemical purity, and a higher radiochemical purity has been reached during the reaction for 2 hours.

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Abstract

The invention provides a preparation capable of bone imaging and bone metastases tumor curing, and belongs to the technical field of bone metastases tumor curing. The preparation is <177>Lu-ibandronicacid. The invention further provides a preparation method of the preparation. According to the preparation method, ibandronic acid is added into a <177>LuCl3 solution, the solution pH is adjusted bymeans of hydrochloric acid, after reaction is carried out at a certain temperature for a certain time, sterilization is conducted, and filtering is conducted to obtain the preparation. According to the preparation capable of bone imaging and bone metastases tumor curing and the preparation method, by combining a radionuclide <177> Lu and the ibandronic acid, the preparation <177>Lu-ibandronic acidcapable of bone imaging and achieving bone metastases tumor curing is provided; the <177> Lu is a bone-seeking imaging agent, a large dose of the <177> Lu has curing action on bone metastases, and the ibandronic acid also has higher action on curing bone metastases, so that the <177>Lu-ibandronic acid preparation can bring the curing action of the radionuclide <177> Lu and the ibandronic acid onthe bone metastases tumor into play better.

Description

technical field [0001] The invention belongs to the technical field of bone metastases treatment, and specifically relates to a preparation for both bone imaging and bone metastases treatment, as well as its preparation and application. Background technique [0002] The incidence of malignant tumors is increasing year by year, and bone is a common site for advanced metastasis of malignant tumors. The clinical treatment of bone metastases is very difficult, and an effective and targeted treatment is urgently needed. [0003] With the development of nuclear medicine, new radiopharmaceuticals and radiopharmaceutical-labeled targeted drugs are constantly being used in the treatment of tumors. Radionuclide therapy can not only relieve pain, but also kill tumor cells and even Some patients achieved remission. At present, the commonly used nuclides in China include phosphorus-32 ( 32 P), strontium-89( 89 Sr) and samarium-153 ( 153 Sm), phosphorus-32 has relatively large toxic ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/00A61K31/663A61P35/04A61K103/30
CPCA61K31/663A61K51/00A61P35/04A61K2300/00
Inventor 陈跃张蜀茂胥芹黄占文蔡亮张伟刘楠张莉
Owner THE AFFILIATED HOSPITAL OF SOUTHWEST MEDICAL UNIV
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