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A kind of doxorubicin embolization microsphere and preparation method thereof

A technology of microspheres and slow-release microspheres, applied in the field of medicine, can solve the problems of inability to obtain lipiodol emulsion, increase adverse reactions, reduce local efficacy, etc., to reduce the possibility of contamination, reduce adverse reactions, and reduce operation steps. Effect

Active Publication Date: 2020-10-09
AFFILIATED YONGCHUAN HOSPITAL OF CHONGQING MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this method has two major defects: ① local deposition of lipiodol emulsion sometimes cannot achieve satisfactory results, and as time goes on, the cytotoxic effect of chemotherapy drugs on tumor tissue also decreases; ② traditional Drug carriers are lipids, and chemotherapy drugs are water-soluble, such traditional emulsions cause rapid release of chemotherapy drugs into the bloodstream, thereby rapidly entering the systemic circulation, increasing systemic adverse reactions and reducing local efficacy
The usage of doxorubicin embolic microspheres is to take out the embolic microspheres stored in normal saline, load doxorubicin drug, and inject them into the catheter. When the drug is loaded, the microspheres are most likely to contaminate the microspheres, leading to aggravation of the patient’s condition
Therefore, the current problems that doxorubicin embolic particles need to solve are, on the one hand, the embolization problem of the microspheres. The better the embolization effect, the better the therapeutic effect; Pollution caused by multiple operation steps; on the other hand, there is a problem of convenient storage of doxorubicin embolic particles. The currently used doxorubicin particles need to be stored in normal saline, which is extremely inconvenient and not easy to carry

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Embodiment 1: Preparation of doxorubicin embolization microspheres 1:

[0024] Step 1: Dissolve 10g of polysuccinimide in 100ml of N,N-dimethylformamide, then add 3g of ethyl cellulose, stir in a water bath at 50°C for 6 hours, then cool to 5°C and add 10ml of ethanolamine , after adjusting the pH=6.9, heat the water bath to 20°C and stir for 10 hours, add a crosslinking agent, stir and react for 3 hours, then raise the temperature to 25°C and add 8g of polyvinyl alcohol, stir for 5 minutes, then continue to heat up to 60°C, continue to stir for 2 hours, then drop in 20 wt% sodium hydroxide solution, hydrolyzed at 35°C for 2 hours, and then washed with deionized water until neutral to obtain a polyaspartic acid composite hydrogel;

[0025] Step 2: Add 2g of slow-release microspheres into the polyaspartic acid composite hydrogel, stir at 2000rpm for 3h, then vacuum freeze-dry at -10°C and vacuum at 15Pa for 20min to obtain a gel layer wrapped slow-release microspheres; ...

Embodiment 2

[0029] Embodiment 2: Preparation of doxorubicin embolization microspheres two:

[0030] Step 1: Dissolve 8g of polysuccinimide in 100ml of N,N-dimethylformamide, then add 3g of ethyl cellulose, stir in a water bath at 50°C for 6 hours, cool to 5°C, and then add 10ml Ethanolamine, after adjusting the pH to 7, heat the water bath to 20°C and stir for 10 hours, add a cross-linking agent, stir and react for 3 hours, then raise the temperature to 25°C and add 10g of polyvinyl alcohol, stir for 6 minutes, continue to heat up to 55°C, continue to stir for 2 hours, and then drop Add 20wt% sodium hydroxide solution, hydrolyze at 35°C for 2h, then wash with deionized water until neutral to obtain polyaspartic acid composite hydrogel;

[0031] Step 2: Add 1.5 g of sustained-release microspheres into the polyaspartic acid composite hydrogel, stir at 2500 rpm for 2 h, and then vacuum freeze-dry at -10 °C and vacuum at 15 Pa for 20 min to obtain a gel coated with layer of slow-release micr...

Embodiment 3

[0035] Embodiment 3: Preparation of doxorubicin embolization microspheres three:

[0036] Step 1: Dissolve 15g of polysuccinimide in 150ml of N,N-dimethylformamide, then add 5g of ethyl cellulose, stir in a water bath at 50°C for 6 hours, cool to 5°C, and then add 10ml of ethanolamine , after adjusting the pH=7.1, heat the water bath to 20°C and stir for 10 hours, add a cross-linking agent, stir for 3 hours, then add 12g of polyvinyl alcohol to 35°C, stir for 8 minutes, continue to heat up to 50°C, continue to stir for 3 hours, then drop in 20 wt% sodium hydroxide solution, hydrolyzed at 35°C for 2 hours, and then washed with deionized water until neutral to obtain a polyaspartic acid composite hydrogel;

[0037] Step 2: Add 2g of slow-release microspheres into the polyaspartic acid composite hydrogel, stir at 3000rpm for 3h, then vacuum freeze-dry at -10°C and vacuum at 15Pa for 20min to obtain a gel layer wrapped Sustained-release microspheres;

[0038] Step 3: Dissolve 14...

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Abstract

The invention discloses a doxorubicin embolism microsphere, and a preparation method thereof, and belongs to the technical field of medicine. According to the preparation method, the doxorubicin embolism microsphere is of a three-layer structure, wherein a slow release microsphere is taken as an internal layer, a gel layer is taken as a middle layer, a composite film is taken as an external layer;the slow release microsphere is loaded with doxorubicin; the space between the gel layer and the composite film is filled with a sodium chloride solution. According to the preparation method, polyaspartic acid is added to prepare the doxorubicin embolism microsphere, the doxorubicin embolism microsphere possesses excellent embolism effect; the doxorubicin embolism microsphere is provided with thethree-layer structure, so that it is not necessary to store the doxorubicin embolism microsphere in liquid, the doxorubicin embolism microsphere is convenient to store, carry, and use.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a doxorubicin embolization microsphere and a preparation method thereof. Background technique [0002] Liver cancer is one of the most common malignant tumors in the world, and its case fatality rate ranks third among malignant tumors. In my country, about 383,000 people die of liver cancer every year, accounting for 51% of the global liver cancer deaths, which has brought a heavy burden to our society and medical care. Most patients with liver cancer are in the middle and advanced stages when they are diagnosed, and portal vein tumor thrombus (PVTT) is a typical clinical manifestation of patients at this stage. Portal vein tumor thrombus, that is, cancer tissue in the portal vein of the liver, has an incidence rate as high as 44.0-62.2%. If no treatment is given, the median survival period of such patients is only 2.7-4.0 months, which is an important factor affect...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/52A61K47/34A61K47/02A61K47/36A61K47/42A61K31/704A61P35/00A61L24/00A61L24/08A61L24/10A61L24/04
CPCA61K9/0019A61K9/501A61K9/5031A61K9/5036A61K9/5052A61K31/704A61L24/001A61L24/0015A61L24/046A61L24/08A61L24/102A61L2300/216A61L2300/416A61L2400/06A61P35/00C08L5/04C08L77/00
Inventor 邓怡曾丽陈青松
Owner AFFILIATED YONGCHUAN HOSPITAL OF CHONGQING MEDICAL UNIV