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5-fluorouracil drug-loading microspheres and preparation method thereof

A technology of fluorouracil and drug-loaded microspheres is applied in the field of coating 5-fluorouracil drug-loaded microspheres with biodegradable polymer materials and the preparation field thereof, which can solve the problem of the lack of sustained-release preparations, the disadvantage of the body, and the drug-loading capacity of the microspheres. Low problems, to achieve the effect of good compatibility and dispersion

Active Publication Date: 2013-01-02
海宁经开产业园区开发建设有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] 5-fluorouracil (5-fluorouracil, referred to as 5-Fu) is one of the most commonly used anti-tumor drugs in clinical practice. It has a wide anti-cancer spectrum and has been widely used in the treatment of various solid tumors. It is positively correlated, but its plasma half-life is extremely short, and the plasma half-life t1 / 2 is about 10-20 minutes
At present, there are many studies on fluorouracil microspheres coated with degradable polymer materials, all of which adopt O / O type and O / W type emulsification volatilization method and spray drying method to prepare fluorouracil polylactic acid microspheres, or use chitosan as the The disadvantage of the microspheres of the carrier is that the microspheres prepared by the O / O type and O / W type emulsification and volatilization method have low drug loading, while the spray drying method has higher requirements for the preparation conditions, and the preparation process uses If organic solvents, surfactants and molding agents are removed, some of them will remain in the pharmaceutical preparations, which is harmful to the body.
Each of the above-mentioned applications is a fluorouracil sustained-release product developed for a specific application field. There is no sustained-release preparation suitable for surgical wounds and epidermal administration. Bioglue α- A cyanoacrylate with a degradation rate consistent with bioglue alpha-cyanoacrylate in an extended-release formulation

Method used

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Examples

Experimental program
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Effect test

preparation example Construction

[0019] The preparation of 5-fluorouracil drug-loaded microspheres is prepared according to the following steps:

[0020] a preparation of complex solution

[0021] Dissolve 5-fluorouracil in an alcohol solvent, and magnetically stir for 1 hour to 2 hours under sealed conditions to obtain a solution with a mass percentage of 5-fluorouracil of 0.05wt% to 1wt%, and then in the solution, press 5-fluorouracil and α - The mass ratio of cyanoacrylate is 1 / 100-50 / 100, add α-cyanoacrylate, and stir for 2 hours to 3 hours under sealed conditions to obtain the compound of 5-fluorouracil and α-cyanoacrylate solution.

[0022] b Electrostatic spray into a ball

[0023] Inhale the composite solution obtained in step a into the spinning solution tube for electrospinning, place the flat-bottomed circular glass container on the magnetic stirrer platform, and put a conductive ring electrode in the flat-bottomed circular glass container, and the flat-bottomed circular glass container The rati...

Embodiment 1

[0028] a preparation of complex solution

[0029] Dissolve 5-fluorouracil in an alcohol solvent, and stir magnetically for 1 hour under sealed conditions to obtain a solution with a mass percentage of 5-fluorouracil of 0.05 wt%. Add α-methyl cyanoacrylate in a mass ratio of 1 / 100, and stir for 2 hours under sealed conditions to obtain a composite solution of 5-fluorouracil and α-methyl cyanoacrylate;

[0030] b Electrostatic spray into a ball

[0031] Inhale the composite solution obtained in step a into the spinning solution tube for electrospinning, place the flat-bottomed circular glass container on the magnetic stirrer platform, and put a conductive ring electrode in the flat-bottomed circular glass container, and the flat-bottomed circular glass container The ratio of the diameter of the bottom surface of the container to the diameter of the conductive ring electrode is 5 / 4, and the conductive ring electrode is grounded. Pour distilled water into a flat-bottomed circular...

Embodiment 2

[0034] a preparation of complex solution

[0035] Dissolve 5-fluorouracil in an alcohol solvent, and stir magnetically for 1 hour under sealed conditions to obtain a solution with a mass percentage of 5-fluorouracil of 0.1 wt%. adding ethyl α-cyanoacrylate in a mass ratio of 10 / 100, and stirring for 2 hours under sealed conditions to obtain a composite solution of 5-fluorouracil and ethyl α-cyanoacrylate;

[0036] b Electrostatic spray into a ball

[0037] Inhale the composite solution obtained in step a into the spinning solution tube for electrospinning, place the flat-bottomed circular glass container on the magnetic stirrer platform, and put a conductive ring electrode in the flat-bottomed circular glass container, and the flat-bottomed circular glass container The ratio of the diameter of the bottom surface of the container to the diameter of the conductive ring electrode is 5 / 4, and the conductive ring electrode is grounded. Pour distilled water into a flat-bottomed cir...

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Abstract

The invention relates to 5-fluorouracil drug-loading microspheres and a preparation method thereof. The invention especially relates to bio-degradable high-molecular-material-coated 5-fluorouracil drug-loading microspheres and a preparation method thereof. According to the preparation method, alpha-cyanoacrylate is adopted as a carrier, and 5-fluorouracil is embedded during an alpha-cyanoacrylate monomer polymerization process, such that drug-loading microspheres with an average particle size of 200nm-5mum are obtained, wherein the mass ratio of 5-fluorouracil to alpha-cyanoacrylate is 1 / 100-50 / 100. The invention aims at overcoming defects of existing 5-fluorouracil drug-loading microspheres and preparation methods thereof, and at providing a sustained-release preparation which can be used on surgical wounds and in epidermal administrations. With the cooperation of biological glue in surgical sutures in body cavity or on body surface, degradation speed consistency can be provided. The operation is simple. According to the invention, various other additives such as organic solvents, surfactants, and excipients are not needed.

Description

technical field [0001] The invention relates to 5-fluorouracil drug-loaded microspheres and a preparation method thereof, in particular to a biodegradable polymer material-coated 5-fluorouracil drug-loaded microsphere and a preparation method thereof. Background technique [0002] 5-fluorouracil (5-fluorouracil, referred to as 5-Fu) is one of the most commonly used anti-tumor drugs in clinical practice. It has a wide anti-cancer spectrum and has been widely used in the treatment of various solid tumors. There is a positive correlation, but its plasma half-life is extremely short, and the plasma half-life t1 / 2 is about 10-20 minutes. Frequent administration is required, and the toxic and side effects are relatively large, which is not easily accepted by patients. In order to reduce the toxic and side effects of 5-fluorouracil and improve the utilization rate of the drug, it can be mixed with biodegradable polymer materials to make drug-loaded microspheres with sustained rele...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/513A61K47/14A61P35/00
Inventor 柏自奎陈立波
Owner 海宁经开产业园区开发建设有限公司
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