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Polymeric micelle freeze-dried preparation of taxane anti-tumor drugs as well as preparation method and application of polymeric micelle freeze-dried preparation

A technology of anti-tumor drugs and taxanes, which is applied in the direction of anti-tumor drugs, drug combinations, freeze-dried delivery, etc., can solve the problems of safety concerns and poor stability of micelles, and achieve improved safety and high encapsulation efficiency , the effect of large drug loading

Active Publication Date: 2017-02-15
GUANGDONG ZHONGSHENG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] One of the objects of the present invention is to provide a polymer micelle lyophilized preparation of taxane antineoplastic drugs, aiming at solving the problem of poor stability of micelles of existing block copolymer-loaded taxane drugs, security concerns

Method used

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  • Polymeric micelle freeze-dried preparation of taxane anti-tumor drugs as well as preparation method and application of polymeric micelle freeze-dried preparation
  • Polymeric micelle freeze-dried preparation of taxane anti-tumor drugs as well as preparation method and application of polymeric micelle freeze-dried preparation
  • Polymeric micelle freeze-dried preparation of taxane anti-tumor drugs as well as preparation method and application of polymeric micelle freeze-dried preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Synthesis of polycaprolactone-polyethylene glycol-polycaprolactone block copolymer:

[0037]A polycaprolactone-polyethylene glycol-polycaprolactone block copolymer with a weight ratio of 10:20:10 was prepared by ring-opening polymerization. Under the protection of nitrogen, 40g of polyethylene glycol monomethyl ether (molecular weight: 2000), 40g of caprolactone, and 0.1g of stannous octoate were successively added to the reactor that was fully dried at a high temperature of 60°C for 12 hours, and the reactor was vacuumed. Temperature <1mmHg, seal the reactor, heat up to 130°C for 12h, cool, add 160ml of dichloromethane to dissolve and dilute, add 160ml of purified water and stir at room temperature for 24h, let stand to separate layers, and dry the dichloromethane layer with anhydrous magnesium sulfate After suction filtration, the filtrate was precipitated with 3200 ml of anhydrous ether and then vacuum-dried to obtain a white solid product.

[0038] The white solid ...

Embodiment 2

[0040] Synthesis of polyethylene glycol monomethyl ether-polycaprolactone block copolymer:

[0041] A polyethylene glycol monomethyl ether-polycaprolactone block copolymer with a weight ratio of 50:50 was prepared by ring-opening polymerization. Under the protection of nitrogen, 50g of polyethylene glycol monomethyl ether (molecular weight: 2000), 50g of caprolactone, and 1g of stannous octoate were successively added to the reactor that was fully dried at a high temperature of 100°C for 4 hours, and the reactor was sealed and filled with dry nitrogen. Pressurize to >4kg, heat up to 180°C to react for 1h, cool, add 50ml of dichloromethane to dissolve and dilute, add 10ml of deionized water and stir at room temperature for 12h, stand to separate layers, dry the dichloromethane layer with anhydrous magnesium sulfate, and pump filtered, the filtrate was concentrated to dryness, added water to dissolve, and obtained a blank polymer micelle solution, which was concentrated by ultra...

Embodiment 3

[0043] Synthesis of polyethylene glycol monomethyl ether-poly(D,L) lactide block copolymer:

[0044] A polyethylene glycol monomethyl ether-poly(D,L) lactide block copolymer with a weight ratio of 50:50 was prepared by ring-opening polymerization. Under nitrogen protection, add 50g of polyethylene glycol monomethyl ether (molecular weight: 2000), 50g of D, L-lactide, and 0.5g of stannous octoate into the reactor that has been fully dried at a high temperature of 120°C for 1 hour, and seal the reactor. , filled with dry nitrogen and pressurized to >2kg, heated to 150°C to react for 4 hours, cooled, added 100ml of dichloromethane to dissolve and dilute, then added 100ml of water for injection and stirred at room temperature for 24h, stood to separate layers, and dichloromethane layer was washed with anhydrous sulfuric acid Magnesium is dried and filtered with suction, the filtrate is concentrated to dryness, and dissolved in water for injection to obtain a blank polymer micelle ...

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Abstract

The invention discloses a polymeric micelle freeze-dried preparation of taxane anti-tumor drugs as well as a preparation method and an application of the polymeric micelle freeze-dried preparation. The polymeric micelle freeze-dried preparation consists of a polyether / polyester segmented copolymer and taxane drugs, wherein the weight ratio of the polyether / polyester segmented copolymer to the taxane drugs is at (1-99) to 1; and in the polyether / polyester segmented copolymer, the molecular weight ratio of polyether to polyester is at 1 to (0.5-2). According to the taxane anti-tumor drug polymeric micelle freeze-dried preparation prepared by the invention, the physical stability of a redissolved solution is significantly increased; and meanwhile, the occurrence rate of a guinea pig allergic reaction in the taxane anti-tumor drug polymeric micelle freeze-dried preparation prepared from the polyether / polyester segmented copolymer which is subjected to ultrafiltration and freeze-drying treatment is obviously reduced, so that the safety of the taxane anti-tumor drug polymeric micelle freeze-dried preparation is further enhanced.

Description

technical field [0001] The invention belongs to the technical field of nanomedicine, and relates to a polymer micelle freeze-dried preparation of taxane antitumor drugs, in particular to a polymer micelle freeze-dry preparation of taxane antitumor drugs and a preparation method thereof and apply. Background technique [0002] Tumor has become the number one killer threatening human health, and the current treatment methods for malignant tumors are mainly surgical treatment, drug treatment and radiotherapy. Currently used antitumor drugs mainly kill tumor cells by inhibiting cell differentiation, but chemotherapy drugs lack selectivity for tumor cells and normal cells, so they show strong toxic and side effects on normal cells. For example, paclitaxel and docetaxel of the taxane class, although the above-mentioned drugs have been marketed with corresponding injections and are widely used, there are still many problems with the taxane class of drugs, such as Sanofi-Aventis’ ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K9/107A61K31/337A61K47/34A61P35/00
CPCA61K9/0019A61K9/1075A61K9/19A61K31/337A61K47/34A61K2300/00
Inventor 张兰陈小新龙超峰谢称石廖小英白少伟孙金鑫钱志勇
Owner GUANGDONG ZHONGSHENG PHARMA
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