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Oridonin polymer micelle administration preparation and preparation method thereof

A technology of oridonin and polymer glue, which is applied in the field of drug delivery preparation and preparation of oridonin polymer micelles, and can solve the problem of unsatisfactory solubilization effect and high toxicity of low-molecular surfactants. problems, to achieve the effects of easy enrichment, reduced toxicity, and extended circulation time

Inactive Publication Date: 2009-05-06
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The low-molecular-weight surfactants used in pharmacy to solubilize insoluble drugs are either unsatisfactory in solubilization effect or relatively toxic

Method used

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  • Oridonin polymer micelle administration preparation and preparation method thereof
  • Oridonin polymer micelle administration preparation and preparation method thereof
  • Oridonin polymer micelle administration preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Embodiment 1: Preparation of amphiphilic block copolymer mPEG-PDLLA

[0036] (1) Add 2.5g D, L-lactide and 4g polyethylene glycol monomethyl ether (molecular weight 5000) into a three-necked bottle equipped with a magnetic stirrer, and heat the oil bath to 140°C for melting (decompression vacuum ), add a mass percentage of 0.05% stannous octoate catalyst, react for 8h, stop the reaction, cool to room temperature, and dissolve the product with 10ml of dichloromethane or chloroform, precipitate with 200ml of cold ether, filter, and vacuum dry at 30°C for 24-48 hour, the product mPEG-PDLLA was obtained, and the molecular weight of the PDLLA block was calculated to be 3000 by NMR. The mPEG-PDLLA with a molecular weight of 8000 was obtained 8000

[0037] (2) Add 4.5g D, L-lactide and 4g polyethylene glycol monomethyl ether (molecular weight 5000) into a three-necked bottle equipped with a magnetic stirrer, and heat the oil bath to 140°C for melting (decompression vacuum )...

Embodiment 2

[0039] Embodiment 2: Preparation of amphiphilic block copolymer mPEG-PLLA

[0040] Add 4.5g of L-lactide and 4g of polyethylene glycol monomethyl ether (molecular weight: 5000) into a three-necked bottle equipped with a magnetic stirrer, heat the oil bath to 140°C for melting (decompression and vacuum), then add mass The percentage is 0.05% stannous octoate catalyst, react for 10h, stop the reaction, cool to room temperature, dissolve the product with 10ml of dichloromethane or chloroform, precipitate with 200ml of cold ether, filter, and vacuum dry at 30°C for 24-48 hours to obtain the product mPEG - PLLA, the molecular weight of the PLLA block is calculated to be 5000 by nuclear magnetic spectrum. The mPEG-PLLA with a molecular weight of 10000 was obtained 10000

Embodiment 3

[0041] Embodiment 3: Preparation of amphiphilic block copolymer mPEG-PLGA

[0042] (1) Add 4.5g of D, L-lactide and glycolide mixture (LA / GA=50 / 50) and 4g of polyethylene glycol monomethyl ether (molecular weight 5000) to a three-necked magnetic stirrer In the bottle, after the oil bath is heated to 140°C for melting (decompression and vacuum), add the stannous octoate catalyst that is 0.05% by mass percentage, react for 10h, stop the reaction, cool to room temperature, and the product is dissolved with 10ml of dichloromethane or chloroform. Precipitate with 200ml of cold ether, filter, and vacuum dry at 30°C for 24-48 hours to obtain the product mPEG-PLGA. The molecular weight of the PLGA block is calculated to be 5000 by NMR. The mPEG-PLGA with a molecular weight of 10000 was obtained 10000(50 / 50)

[0043] (2) Add 4.5g of D, L-lactide and glycolide mixture (LA / GA=75 / 25) and 4g of polyethylene glycol monomethyl ether (molecular weight 5000) to a three-necked three-necked st...

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Abstract

The invention belongs to the medicine technology field, which provides an oridonin A polymer micelle drug delivery preparation and a preparation method thereof. The polymer is diblock copolymer, and the hydrophilic section is polyethylene glycol monomethyl ether while the hydrophobic section can be chosen from biodegradable poly (D, L-lactic acid), poly (L-lactic acid), poly (lactide-glycolide), caprolactone, PHDCA or the mixture thereof. The polymer medicament micelle traditional Chinese medicine is enveloped in one or two polymers by a physics form or prepared to be the micelle after being covalent bonded with the polymer by a chemical reaction. The prepared micelle exists in the state of aqueous dispersion or freeze-dried powder. The particle size distribution range of the oridonin A polymer micelle is 5 to 500nm while the drug loading is 0.01 to 40 percent. The oridonin A polymer micelle prolongs the circulation time of the medicament in bodies, and AUC0-infinite value is 2.19 times of that of common injections, thus leading the medicament to enrich in tumor parts easier, improving the efficacy and reducing the toxicity.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a polymer micelle drug delivery preparation of oridonin and a preparation method thereof, specifically, directly physically encapsulating oridonin into a synthesized amphiphilic block copolymer Oridonin A and the synthesized amphiphilic block copolymer are further covalently bonded to form an amphiphilic block copolymer-oridonin A bonded drug, and then prepared into micelles. Background technique [0002] Oridonin is a natural organic compound of ent-kau-rene-diterpenoid isolated from Labtea plants of the genus Rabdosia. The ingredients have strong anti-tumor activity and are effective against a variety of transplanted tumors. They are mainly used clinically for the treatment of liver cancer, esophageal cancer, and pancreatic cancer. Oridonin has poor water solubility and cannot meet the needs of directly making an aqueous solution for injection. In order to make an aqueous solut...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K9/00A61K31/352A61P35/00C08G63/91C08G63/66A61K47/59A61K47/60
Inventor 王东凯张文涛
Owner SHENYANG PHARMA UNIVERSITY
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