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

Azithromycin new crystal-form compound and preparation method thereof

A technology of azithromycin and compounds, applied in the field of medicine, can solve the problems of low stability of azithromycin crystalline products, difficulty in solvent recovery, poor fluidity, etc., and achieve good quality stability, good fluidity, and suitable for long-term storage.

Active Publication Date: 2015-09-16
CSPC OUYI PHARM CO LTD
View PDF13 Cites 7 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] By analyzing and studying the above-mentioned azithromycin crystals, it is found that the azithromycin crystalline products obtained by the existing methods all have disadvantages such as low stability, low purity, strong hygroscopicity, poor fluidity, expensive reagents used in the method, difficult solvent recovery, etc., and Does not well meet the pharmaceutical industry's demand for azithromycin polymorphs

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
  • Azithromycin new crystal-form compound and preparation method thereof
  • Azithromycin new crystal-form compound and preparation method thereof
  • Azithromycin new crystal-form compound and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1 Preparation of Azithromycin New Crystal Form Compound

[0029] Add 375ml of methyl acetate and 625ml of isopropyl ether to 100g of crude azithromycin, heat to 50°C to dissolve, cool to room temperature, then add 500mL of water to the solution, stir and mix evenly, then cool down to 5-10°C, and stand for crystallization After 3 hours, it was filtered and dried to obtain 97.7 g of the new crystal form of azithromycin, with a yield of 97.7% and an HPLC purity of 99.82%.

Embodiment 2

[0030] Example 2 Preparation of Azithromycin New Crystal Form Compound

[0031] Add 570ml of methyl acetate and 1430ml of isopropyl ether to 100g of crude azithromycin, heat to 40°C to dissolve, cool to room temperature, then add 200mL of water to the solution, stir and mix evenly, then cool down to 5-10°C, and stand for crystallization After 5 hours, it was filtered and dried to obtain 95.1 g of the new crystal form of azithromycin, with a yield of 95.1% and an HPLC purity of 99.52%.

Embodiment 3

[0032] Example 3 Preparation of Azithromycin New Crystal Form Compound

[0033] Add 35ml of methyl acetate and 165ml of isopropyl ether to 100g of crude azithromycin, heat to 45°C to dissolve, cool to room temperature, then add 200mL of water to the solution, stir and mix evenly, stand for crystallization for 1h, filter, and dry to obtain azithromycin The new crystalline compound was 98.4g, the yield was 98.4%, and the HPLC purity was 99.43%.

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 an azithromycin new crystal-form compound and a preparation method thereof, belonging to the technical field of medicine. According to the azithromycin new crystal-form compound provided by the invention, an X-ray powder diffraction diagram has characteristic peaks at the positions that the reflection angle 2theta is 3.8+ / -0.2 degrees, 15.4+ / -0.2 degrees, 17.2+ / -0.2 degrees, 18.7+ / -0.2 degrees, 20.1+ / -0.2 degrees and 23.2+ / -0.2 degrees. The azithromycin new crystal-form compound provided by the invention is subjected to a stability test under the conditions that the temperature is 40+ / -2 DEG C and the relative humidity is 75+ / -5 percent. The test result shows that the content of each related substance of the azithromycin new crystal-form compound provided by the invention is not changed obviously, and excellent quality stability is achieved. The repose angle measuring result shows that the azithromycin new crystal-form compound has excellent fluidity and is more suitable for medicine preparation and long-time storage.

Description

technical field [0001] The invention relates to a compound and a preparation method thereof, in particular to a new crystal form compound of azithromycin and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Azithromycin is the first 15-membered azamacrolide antibiotic listed on the market. It was first listed in the United States by Pfizer in 1991. It is known as the "blockbuster" of antibiotic drugs in the 20th century. Azithromycin has a wide antibacterial spectrum and strong antibacterial effect. It is widely used clinically for acute pharyngitis and acute tonsillitis caused by Streptococcus pyogenes; sinusitis, otitis media, acute bronchitis and acute exacerbation of chronic bronchitis caused by sensitive bacteria; Streptococcus pneumoniae, influenza Pneumonia caused by Haemophilus and Mycoplasma pneumoniae; urethritis and cervicitis caused by Chlamydia trachomatis and non-multidrug-resistant Neisseria gonorrhoeae; ...

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): C07H17/00C07H1/06
CPCC07H1/06C07H17/00
Inventor 郑雪清齐新英张文静韩彩霞刘光苹
Owner CSPC OUYI PHARM CO LTD
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