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

Synthesis method of gatifloxacin-chalcone conjugate slow release agent

A technology of gatifloxacin and its synthesis method, which is applied in the directions of pharmaceutical formulation, drug combination, drug delivery, etc., can solve problems such as failure and short retention time, and achieve the effect of promoting inhibition, improving water solubility and bioavailability

Active Publication Date: 2020-06-09
大连永达苏利药业有限公司
View PDF3 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The object of the present invention is to overcome the problem of short retention time of gatifloxacin and chalcone drugs in the body and easy to be metabolized and lose efficacy in the prior art, and provides a slow-moving compound of gatifloxacin and chalcone. Synthetic method of release agent

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
  • Synthesis method of gatifloxacin-chalcone conjugate slow release agent
  • Synthesis method of gatifloxacin-chalcone conjugate slow release agent
  • Synthesis method of gatifloxacin-chalcone conjugate slow release agent

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] A synthetic method of gatifloxacin and chalcone conjugate slow-release agent, comprising the following steps:

[0028] S1. Preparation of gatifloxacin and chalcone conjugates;

[0029] S2. Ginkgo biloba polyprenol and chitosan were mixed and dissolved in 0.2mol / L acetic acid solution at a molar ratio of 2:1, using Cu as a catalyst, and reacted at 180°C for 2 hours to obtain composite chitosan;

[0030] S3. Dissolve the gatifloxacin and chalcone conjugate obtained in step S1 and the complex chitosan obtained in step S2 in a hydrochloric acid solution with a mass fraction of 0.5% according to a mass ratio of 1:30, and Ultrasound 20min;

[0031] S4. Adjust the mixed solution obtained in step S3 to be neutral, and spray dry it.

[0032] The structure of the chalcone is:

[0033]

[0034] R1 is Br and R2 is H.

Embodiment 2

[0036] A synthetic method of gatifloxacin and chalcone conjugate slow-release agent, comprising the following steps:

[0037] S1. Preparation of gatifloxacin and chalcone conjugates;

[0038] S2. Ginkgo biloba polyprenol and chitosan were mixed and dissolved in 0.5mol / L acetic acid solution at a molar ratio of 5:1, using Cu as a catalyst, and reacted at 160°C for 1 hour to obtain composite chitosan;

[0039] S3. Dissolve the gatifloxacin and chalcone conjugate obtained in step S1 and the complex chitosan obtained in step S2 in a hydrochloric acid solution with a mass fraction of 0.1% according to a mass ratio of 1:50, and Ultrasound for 30min;

[0040] S4. Adjust the mixed solution obtained in step S3 to be neutral, and spray dry it.

[0041] The structure of the chalcone is:

[0042]

[0043] R1 is Br, and X is S.

Embodiment 3

[0045] A synthetic method of gatifloxacin and chalcone conjugate slow-release agent, comprising the following steps:

[0046] S1. Preparation of gatifloxacin and chalcone conjugates;

[0047] S2. Ginkgo polyprenol and chitosan were mixed and dissolved in 0.3mol / L acetic acid solution at a molar ratio of 4:1, and Cu was used as a catalyst to react at 170°C for 1 hour to obtain composite chitosan;

[0048] S3. Dissolve the gatifloxacin and chalcone conjugate obtained in step S1 and the complex chitosan obtained in step S2 in a hydrochloric acid solution with a mass fraction of 0.2% according to a mass ratio of 1:45, and Ultrasound for 25 minutes;

[0049] S4. Adjust the mixed solution obtained in step S3 to be neutral, and spray dry it.

[0050] The structure of the chalcone is:

[0051]

[0052] R1 is Br, and X is N.

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

No PUM Login to View More

Abstract

The invention relates to the field of medicine preparation, and in particular to a synthesis method of a gatifloxacin-chalcone conjugate slow release agent. The synthesis method comprises the following steps: S1, preparing a gatifloxacin-chalcone conjugate; S2, mixing ginkgo polyprenol and chitosan according to a molar ratio of (2-5):1, dissolving the mixture in an acetic acid solution with a concentration of 0.2-0.5mol / L, and performing reacting for 1-2h by using Cu as a catalyst to obtain composite chitosan; S3, dissolving the gatifloxacin-chalcone conjugate obtained in the step S1 and thecomposite chitosan obtained in the step S2 in a hydrochloric acid solution with a mass fraction of 0.1-0.5% according to a mass ratio of 1:(30-50), and performing ultrasound at 50-100 Hz for 20-30 minutes; and S4, adjusting the mixed solution obtained in the step S3 to neutral and performing spray drying. The drug sustained-release agent obtained by the method has a good drug sustained-release effect and has a good inhibiting effect on cancer cells.

Description

technical field [0001] The invention relates to the field of medicine preparation, in particular to a synthesis method of a gatifloxacin-chalcone conjugate slow-release preparation. [0002] technical background [0003] Gatifloxacin (Gatifloxacin, 1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo- 3-quinoline carboxylic acid) is a new 6-fluoro-8-methoxyquinolone compound created by Kyorin Pharmaceutical Co., Ltd., and quinolones have become highly effective, low-toxicity, broad-spectrum first-line antibiotics widely used clinically. Infectious medicines. Among the pharmacophore with diverse structures, chalcones with α, β-unsaturated ketone structure characteristics are natural effective ingredients with various pharmacological activities. Natural chalcones are mostly α, β-unsaturated ketones substituted by polyhydroxybenzene rings, and their poor water solubility leads to low bioavailability, which limits their clinical application. The bioava...

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
IPC IPC(8): A61K9/52A61K47/36A61K47/54A61K47/32A61K31/496A61P35/00
CPCA61K9/5036A61K9/5026A61K47/54A61K31/496A61P35/00
Inventor 曹庆华
Owner 大连永达苏利药业有限公司
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