Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Eutectic of 5-fluorouracil and sarcosine as well as preparation method and application thereof

A technology of fluorouracil and sarcosine, which is applied in the field of chemical medicine and drug co-crystal, can solve the problems of low solubility, poor permeability and multi-solvent of 5-fluorouracil, and achieves simple and easy experimental operation, improved permeability and improved permeability. Effect

Active Publication Date: 2021-08-10
SHANGHAI UNIV +1
View PDF9 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] CN108373451A discloses a co-crystal of 5-fluorouracil and proline and its preparation method, and CN110790712A discloses a co-crystal of 5-fluorouracil and L-phenylalanine and its preparation method. These two patents both provide A co-crystal preparation method, as well as the characterization of the co-crystal structure and the test of the solubility performance, does not involve the change of permeability
However, the solubility of 5-fluorouracil itself is not low, and it is of little significance to increase its solubility, mainly because of its poor permeability
In addition, the preparation methods of the two patents are all solution methods, requiring more solvents

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Eutectic of 5-fluorouracil and sarcosine as well as preparation method and application thereof
  • Eutectic of 5-fluorouracil and sarcosine as well as preparation method and application thereof
  • Eutectic of 5-fluorouracil and sarcosine as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0029] Another aspect of the embodiments of the present invention also provides a method for preparing the co-crystal of 5-fluorouracil and sarcosine, which includes: under crystallization conditions, the molar ratio of 5-fluorouracil and sarcosine is 2:1 Mixing, at least mechanochemical and solution methods are used to obtain said co-crystal of 5-fluorouracil and sarcosine.

[0030]In some embodiments, the preparation method of the co-crystal of 5-fluorouracil and sarcosine specifically includes the following steps: under crystallization conditions, mixing 5-fluorouracil and sarcosine according to a molar ratio of 2:1 to obtain a mixture , and add solvent to grind, and react to obtain the co-crystal of 5-fluorouracil and sarcosine.

[0031] Further, the solvent includes any one or a combination of at least two of water, methanol, ethanol, isopropanol, acetone, acetonitrile, ethyl acetate, methylene chloride, toluene, cyclohexane and n-hexane, etc., But not limited to this. ...

Embodiment 1

[0050] The preparation method of the co-crystal of 5-fluorouracil-sarcosine provided in this example comprises the following steps:

[0051] Put 130.0 mg of 5-fluorouracil and 44.5 mg of sarcosine with a molar ratio of 2:1 in a Pulverisette 23 micro ball mill, then add 52 μL of ethanol, and grind for 20 minutes at 40 Hz and 25 ° C to obtain 5-fluorouracil-sarcosine of eutectics.

Embodiment 2

[0053] The preparation method of the co-crystal of 5-fluorouracil-sarcosine provided in this example comprises the following steps:

[0054] Put 520mg of 5-fluorouracil and 178mg of sarcosine with a molar ratio of 2:1 in a 20mL glass bottle, add 5mL of ethanol, stir and react at room temperature for 72h, centrifuge the mixture, and dry the solid in a vacuum oven for 24h. A co-crystal of 5-fluorouracil-sarcosine was obtained.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
diameteraaaaaaaaaa
thicknessaaaaaaaaaa
Login to View More

Abstract

The invention discloses a co-crystal of 5-fluorouracil and sarcosine as well as a preparation method and application of the co-crystal. The molecular formula of the eutectic is [2C4H3FN2O2.C3H7NO2], the eutectic has a basic structural unit composed of two 5-fluorouracil molecules and a sarcosine molecule, the eutectic is crystallized in a triclinic system, the space group is P-1, and the cell parameters are alpha = 67.862 (8) degrees, beta = 78.308 (8) degrees and gamma = 77.131 (7) degrees. According to the pharmaceutical co-crystal of 5-fluorouracil and sarcosine, the skin membrane permeability of 5-fluorouracil can be greatly improved, and the bioavailability of 5-fluorouracil can be improved; and the preparation method is simple, easy to implement, green, efficient, high in yield, low in cost, free of solvent residues and suitable for large-scale production.

Description

technical field [0001] The present invention specifically relates to a co-crystal of 5-fluorouracil and sarcosine and a preparation method thereof, and the use of the drug co-crystal of 5-fluorouracil and sarcosine in the preparation of anticancer drugs, belonging to chemical medicine and drug co-crystal technology field. Background technique [0002] The physical and chemical properties of drugs determine the value and efficacy of drugs, which will further affect the production, storage, transportation and clinical effects of drugs, and are also one of the important reasons why drugs can be marketed. To improve the physicochemical properties of drugs, drug co-crystallization offers a promising way. Drug co-crystals can improve the bioavailability of drugs by improving the solubility, dissolution rate, permeability, and stability of drug active ingredients. Along with the research on drug co-crystals, a variety of co-crystal drugs have been listed one after another. [00...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): C07D239/553C07C229/12C07C227/42A61P35/00A61K31/513
CPCC07D239/553C07C229/12A61P35/00C07B2200/13
Inventor 谢起煌张海禄万文王晓娟叶馨
Owner SHANGHAI UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com