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Docetaxel nano polymer micelle freeze-drying preparation and preparation method thereof

A nanopolymer, docetaxel technology, applied in the field of medicine, can solve the problems of drug leakage, unsuitable for large-scale production, unable to be further promoted and truly applied, and achieve the effect of improving stability

Active Publication Date: 2015-07-08
NANJING ZAIMING PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, the micelles prepared from the existing polyethylene glycol monomethyl ether-polylactic acid block polymer and docetaxel have poor stability after dispersion in water, and the drug will leak in a short time, making the Due to its low physical stability in clinical application, it cannot be further promoted and truly applied
In order to solve this problem, CN201010114289 discloses a technology to improve the stability of micelles after reconstitution by adding amino acids in polymer micelles, but the added substances have higher requirements for industrial production, and the added stabilizers increase The complexity of the preparation process is reduced, and the amino acids added at the same time have a degradative effect on the main drug, which is not suitable for large-scale production

Method used

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  • Docetaxel nano polymer micelle freeze-drying preparation and preparation method thereof
  • Docetaxel nano polymer micelle freeze-drying preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0032] Example 1 Preparation of polyethylene glycol monomethyl ether-polylactic acid block polymer.

[0033] (1) Weigh 51.07g of D,L-lactide and 50.57g of polyethylene glycol monomethyl ether 2000 for later use, dry polyethylene glycol monomethyl ether 2000 in vacuum at 100°C for 7 hours, replace with nitrogen, add D, For L-lactide, put in 0.2g of catalyst stannous octoate, vacuumize to a vacuum degree of 0.096Mpa, seal it, and keep the reaction temperature at 100°C. After the D and L-lactide are all melted, replace with nitrogen three times, and then pump Vacuum to ensure the negative pressure in the reactor, airtight, heat up to 140 ° C, react for 12 hours, the reaction is complete, and a light yellow clear viscous liquid is obtained.

[0034](2) Add dichloromethane to the light yellow clear viscous liquid obtained in step (1), add 25ml of dichloromethane, stir for 30min; then add 510ml of anhydrous glacial ether, stir for 30min; then statically Set aside for 12 hours, vacu...

Embodiment 2

[0035] Example 2 Preparation of polyethylene glycol monomethyl ether-polylactic acid block polymer.

[0036] (1) Weigh 48.77g of D,L-lactide and 51.27g of polyethylene glycol monomethyl ether 2000 for later use, dry polyethylene glycol monomethyl ether 2000 at 120°C for 5 hours in vacuum, replace with nitrogen, and put into D,L -Lactide, then put in 0.048g catalyst stannous octoate, vacuumize to a vacuum degree of 0.095Mpa, maintain the reaction temperature at 120°C, after the D,L-lactide is completely melted, replace with nitrogen for 3 times, and then pump Vacuum to ensure the negative pressure in the reactor, nitrogen protection, then raise the temperature to 140 ° C, react for 14 hours, the reaction is complete, and a light yellow clear liquid is obtained.

[0037] (2) Add 29ml of dichloromethane to the above light yellow clear liquid to dissolve, stir to dissolve; then add 586ml of ice anhydrous ether, stir for 30min; stand at 5°C for 12h, then vacuum dry by suction filtr...

Embodiment 3

[0038] Example 3 Preparation of polyethylene glycol monomethyl ether-polylactic acid block polymer.

[0039] (1) Weigh 47.53g of D,L-lactide and 52.17g of polyethylene glycol monomethyl ether 2000 for later use, dry polyethylene glycol monomethyl ether 2000 at 130°C for 7 hours in vacuum, replace with nitrogen, and put in 0.3g of catalyst Stannous octoate, then put in D, L-lactide, evacuate to a vacuum degree of 0.093Mpa, maintain the reaction temperature at 130°C, after the D, L-lactide is completely melted, replace with nitrogen for 3 times, and then evacuate , ensure negative pressure in the reactor, airtight, then raise the temperature to 150° C., react for 6 hours, and the reaction is completed to obtain a light yellow clear liquid.

[0040] (2) Add 45ml of dichloromethane to the light yellow clear liquid in step (1), stir to dissolve; then add 550ml of ice anhydrous diethyl ether, stir for 30min; stand at 0°C for 12h, then vacuum dry by suction filtration. Purification ...

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Abstract

The invention discloses a docetaxel nano polymer micelle freeze-drying preparation, including a methoxypolyethylene glycol-poly lactic acid segmented copolymer carrier material and docetaxel. Docetaxel is encapsulated in the carrier material, and the docetaxel and the carrier material are in the ratio of 0.01-0.15. The methoxypolyethylene glycol-poly lactic acid segmented copolymer is formed by ring open polymerization of D,L-lactide and methoxypolyethylene glycol, wherein the weight ratio of methoxypolyethylene glycol and D,L-lactide) is 1: 0.55-0.65 or 1: 0.73-0.89 or 1:0.91-0.99. Through optimization of the weight ratio of polyester and polyether in the methoxypolyethylene glycol polylactide segmented copolymer, and further optimization of the weight ratio of docetaxel and the carrier, the time of the prepared docetaxel micelle with entrapment rate more than 90% after water redissolution can reach more than 12 h, which is meets the actual situation of clinical drug application, so as to meet the clinical requirements.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a freeze-dried preparation of docetaxel nanometer polymer micelles and a preparation method thereof. Background technique [0002] Docetaxel (DTX), also known as docetaxel, molecular formula C 43 h 53 NO 14 , with a molecular weight of 807.88, is a paclitaxel antineoplastic drug, which can bind to free tubulin, promote the assembly of tubulin into stable microtubules, and inhibit its depolymerization, resulting in the loss of normal function. Fixation of microtubules, thereby inhibiting cell mitosis and exerting anti-tumor effects. It is clinically used in breast cancer, non-small cell lung cancer, pancreatic cancer, soft tissue sarcoma, head and neck cancer, gastric cancer, ovarian cancer and prostate cancer, etc., both alone and in combination. [0003] However, docetaxel also has disadvantages such as poor water solubility, short half-life and high toxicity, w...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/337A61K47/34A61P35/00
CPCA61K47/34A61K9/19A61K31/337C08G63/664A61K9/1075A61P35/00A61P43/00A61K9/10C08L67/04A61K9/5153A61K9/141A61K9/14C08G63/08C08G63/81C08G63/85
Inventor 不公告发明人
Owner NANJING ZAIMING PHARM CO LTD
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