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Preparation method and application of radioiodinated biodegradable chitosan-collagen composite microsphere medicine

A composite microsphere, radioactive technology, applied in the directions of radioactive physical shape, radioactive carrier, drug combination, etc., can solve the problems of radiation damage, low probability of tumor resection, low sensitivity, etc., to achieve strong self-repair ability and prevent thyroid damage. , the effect of good biocompatibility

Inactive Publication Date: 2017-01-25
WEST CHINA HOSPITAL SICHUAN UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] At present, the treatment methods for malignant tumors mainly include surgical resection, radiotherapy, chemotherapy and various comprehensive treatment methods, among which surgical resection is the preferred treatment method, but most patients with malignant tumors are already in the middle and late stage of the tumor when they are diagnosed, and surgical resection is complete. The chance of tumor is very small, for example, the surgical resection rate of primary liver cancer is less than 10%, and that of pancreatic cancer is less than 15%.
Moreover, the prognosis of surgical resection is not ideal. At present, the 5-year survival rate of patients with liver cancer after surgery is 20-45%, while the 5-year survival rate of pancreatic cancer is less than 15%.
At present, most patients can only be treated by non-surgical methods clinically, and malignant tumors of the hepatobiliary and pancreatic system are less sensitive to most chemotherapy drugs, and the clinical effective rate of common chemotherapy drugs is less than 20%. Due to the shielding of the ribs, the effect is poor, and the liver and digestive tract are more sensitive to radiation and are prone to radiation damage, making the hepatobiliary and pancreatic system a relatively restricted area for external radiation therapy. Therefore, it is urgent to find a new method of non-surgical treatment with significant curative effect
However, the labeling rate of radioactive iodine in separate chitosan microspheres is not high, and the actual curative effect is not good.

Method used

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  • Preparation method and application of radioiodinated biodegradable chitosan-collagen composite microsphere medicine
  • Preparation method and application of radioiodinated biodegradable chitosan-collagen composite microsphere medicine

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Embodiment 1

[0051] Embodiment 1 The preparation of iodine 131 labeled chitosan-collagen composite microspheres of the present invention

[0052] 1. Preparation method

[0053] Raw materials: Na 131 I, Na 125 I (Sodium Iodide); Chitosan; Type I Collagen;

[0054] (1) The microspheres are prepared by the improved emulsification condensation method, the specific method is as follows:

[0055] Take chitosan and collagen in a molar ratio of 2:1, specifically, dissolve the collagen in 2% acetic acid solution to obtain a collagen solution with a collagen concentration of 3.62 mg / ml, then add 10 mg of chitosan 1.66ml of collagen solution; 2% acetic acid solution was stirred for 1h and dissolved to obtain a colorless transparent viscous solution; the solution was slowly added to liquid paraffin containing sorbitan oleate (wherein, 10ml of liquid paraffin, sorbitol glycerin 0.8ml of acid ester), stirred at room temperature for 1h to obtain milky liquid; slowly dropwise added 210ul concentration...

Embodiment 2

[0071] Example 2 Preparation of Iodine 131 Labeled Chitosan-Collagen Composite Microspheres of the Present Invention

[0072] 1. Preparation method

[0073] Raw materials: Na 131 I, Na 125 I (Sodium Iodide); Chitosan; Type I Collagen;

[0074] (1) The microspheres are prepared by the improved emulsification condensation method, the specific method is as follows:

[0075] Take chitosan and collagen in a ratio of 1:1, specifically, dissolve collagen in 2% acetic acid solution to obtain a collagen solution with a collagen concentration of 3.62mg / ml, then add 5mg of chitosan to 3.3ml In the collagen solution; slowly add the solution to liquid paraffin containing sorbitan oleate (wherein, liquid paraffin 10ml, sorbitan glyceride 0.8ml), after stirring at room temperature for 1h, milky liquid is obtained; Slowly add 150 ul of 25% glutaraldehyde solution to the emulsion under the condition of cross-linking for 1 hour to solidify and form the microspheres; add a sufficient amount of...

Embodiment 3

[0082] Example 3 Preparation of Iodine 131 Labeled Chitosan-Collagen Composite Microspheres of the Present Invention

[0083] 1. Preparation method

[0084] Raw materials: Na 131 I, Na 125 I (Sodium Iodide); Chitosan; Type I Collagen;

[0085] (1) The microspheres are prepared by the improved emulsification condensation method, the specific method is as follows:

[0086] Take chitosan and collagen in a molar ratio of 1:2, specifically, dissolve the collagen in 2% acetic acid solution to obtain a collagen solution with a collagen concentration of 3.62 mg / ml, then add 5 mg of chitosan 3.3ml of collagen solution; slowly add this solution to liquid paraffin containing sorbitan oleate (wherein, 20ml of liquid paraffin, 1.6ml of sorbitan glyceride), and stir at room temperature for 1h to obtain a milky liquid; Slowly add 220 ul of 25% glutaraldehyde solution to the emulsion under stirring for crosslinking for 1 hour to solidify and form the microspheres; add sufficient isopropan...

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Abstract

The invention discloses a composite microsphere. The composite microsphere is formed in a way that chitosan and collagen are combined. The invention further discloses a radioactive microsphere for radioactive therapy, and radionuclides are marked on the microsphere. The invention further discloses a preparation method and application of the microsphere. According to the composite microsphere, the preparation method and the application, a biodegradable chitosan-collagen composite microsphere is used as nuclide and a drug carrier, both the chitosan and the collagen have good biocompatibility, are biodegradable and can be stably combined with a plurality of radionuclides and drugs (such as chemotherapy drugs, bioactive macromolecules and the like), and clinical application prospects are good.

Description

technical field [0001] The invention relates to a preparation method and application of radioactive iodine-labeled biodegradable chitosan-collagen composite microsphere medicine. Background technique [0002] According to the World Health Organization (WHO), the annual death toll caused by malignant tumors exceeds 6.2 million, and there are about 11 million new cancer patients in the world every year, and the incidence of malignant tumors is still increasing at an annual rate of 1.8-4%. , Malignant tumors have become the second leading cause of death in the world after cardiovascular and cerebrovascular diseases. In Asia including my country, the incidence of primary liver cancer, which is directly pathologically related to hepatitis B, is extremely high; and in recent years, with the improvement of the living standards of the Chinese people, pancreatic cancer, biliary tract cancer and other systemic malignancies The incidence of tumors is also on the rise. Under the existin...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/12A61K51/06A61K51/08A61P35/00A61K101/02
CPCA61K51/1251A61K51/06A61K51/08
Inventor 李林蔡华伟庞富文张文杰
Owner WEST CHINA HOSPITAL SICHUAN UNIV
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