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Application of copolymer in antitumor drugs

A technology of anti-tumor drugs and copolymers, applied in the field of medicine, can solve the problems of many adverse reactions, low bioavailability, poor quality stability of preparations, etc.

Inactive Publication Date: 2015-09-09
海南路易丹尼生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Antineoplastic drugs include antimetabolites, tecans, tinib, vinblastine, camptothecin, paclitaxel, platinum, mycins, hormones, etc., which are poor in water solubility, especially when prepared into preparations. It is an injection, which needs to add a large amount of organic solvents to help dissolve it. When it is used, it has a strong pain and many adverse reactions, such as redness, erythema, allergy, itching, etc., or it is made into a suspoemulsion. low degree

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Embodiment 1 Preparation of polylactic acid-polyoxyethylene copolymer

[0042](1) Polymerization reaction: under the protection of dry high-purity nitrogen, weigh 2 kg of polyoxyethylene and 2 kg of polylactic acid in a fully dry polymerization reactor, add 8.33 g of stannous octoate, and heat to 70 ° C to dissolve polyoxyethylene. Under vacuum conditions, the polymerization reaction was carried out in an oil bath at 150°C for about 10 hours.

[0043] (2) Dissolving: After the polymerization reaction was finished, 1.8 kg of dichloromethane was added to the solid obtained in the reactor to dissolve.

[0044] (3) Mixed precipitation: the above solution was added to a container containing 18 kg of isopropyl ether (pre-cooled at -20° C.), and the target product precipitated.

[0045] (4) Filtration (discard the solution phase): open the valve on the isopropyl ether container to pump the above mixed precipitate into the filter through an evacuation pump, and collect the pre...

Embodiment 2

[0047] Example 2 Preparation of paclitaxel micelles for injection

[0048] (1) Dissolution: According to the formulation ratio of the preparation, accurately weigh 0.3kg of paclitaxel raw material drug and 1.5kg of polylactic acid-polyoxyethylene copolymer into the liquid preparation tank, add about 15kg of ethanol, control the temperature at 60-80°C, and start stirring , Paclitaxel and copolymer excipients were fully dissolved in ethanol, and a clear solution was obtained in about 30 minutes.

[0049] (2) Evaporating the solvent: heating to boiling, and evaporating ethanol to obtain a transparent gel-like drug film mixed with paclitaxel and copolymer auxiliary materials.

[0050] (3) Dissolving: Add 30 L of 5 mM phosphate buffer solution prepared with water for injection into the liquid preparation tank to fully dissolve the gel-like drug film to obtain a paclitaxel micelle solution.

[0051] (4) Charcoal adsorption: Add 9g of activated carbon, stir and adsorb for 15min, and...

Embodiment 3

[0059] Example 3 Preparation of docetaxel micelles for injection

[0060] (1) Dissolution: According to the formulation ratio of the preparation, accurately weigh 0.2kg of docetaxel raw material drug and 1.0kg of polylactic acid-polyoxyethylene copolymer into the liquid preparation tank, add about 10kg of ethanol, and control the temperature at 60-80°C , start stirring to fully dissolve the docetaxel and copolymer excipients in ethanol, and obtain a clear solution in about 30 minutes.

[0061] (2) Evaporating the solvent: heating to boiling, and evaporating ethanol to obtain a transparent gel-like mixed drug film of docetaxel and copolymer excipients.

[0062] (3) Dissolving: Add 30 L of 5 mM phosphate buffer solution prepared with water for injection into the liquid preparation tank to fully dissolve the gel-like drug film to obtain a docetaxel micelle solution.

[0063] (4) Charcoal adsorption: Add 9g of activated carbon, stir and adsorb for 15min, and remove carbon by filt...

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Abstract

The invention provides a copolymer which can be used as a carrier of anti-metabolism drugs and tecans, tinibs, vinblastine, camptothecin, paclitaxel, platinum, mycin and hormone antitumor drugs, and segmented copolymer micelles are formed. The solubility of the antitumor drugs is greatly increased, the curative effect is improved, moreover, the in-vivo cycling time of the drugs is extended, the pharmaceutical activity is improved, the burst release effect is reduced, and the bioavailability is increased.

Description

technical field [0001] The invention relates to a copolymer and its application, in particular to the application of a copolymer in antitumor drugs, and belongs to the technical field of medicine. Background technique [0002] With the rapid development of life sciences and polymer materials science, the research and application of environment-sensitive polymer materials in intelligent drug controlled release systems plays an important role, and the research on pH- and temperature-sensitive biodegradable polymer materials has attracted much attention. Such polymer materials are divided into block copolymers, graft copolymers, cationic polymers and anionic polymers according to their structure and properties. For block copolymers, according to the arrangement of the chain segments, they can be divided into A-B type diblocks, A-B-A and B-A-B type triblock copolymers, mainly including polyoxyethylene, polylactic acid, polyglycolic acid, polylactic acid hydroxyl Acetic acid and...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/34A61K47/32A61K31/337A61P35/00C08G81/00
Inventor 王平
Owner 海南路易丹尼生物科技有限公司
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