Unlock instant, AI-driven research and patent intelligence for your innovation.

Method for preparing azithromycin monohydrate

A technology of azithromycin and monohydrate, which is applied in the field of preparation of azithromycin monohydrate, can solve the problems of complicated operation method, poor preparation adaptability, poor fluidity and the like, and achieves the effects of good fluidity, good preparation adaptability and good quality

Active Publication Date: 2014-06-11
ZHEJIANG GUOBANG PHARMA
View PDF11 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The operation method of this patent is relatively cumbersome, and the refining rate is about 95%.
Due to the use of reverse dropwise crystallization in this method, the crystal form obtained is very fine, has poor fluidity, and poor preparation adaptability

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
  • Method for preparing azithromycin monohydrate
  • Method for preparing azithromycin monohydrate
  • Method for preparing azithromycin monohydrate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Put 20g of azithromycin dihydrate into a mixed solvent of 30mL of methanol and 20mL of acetone, raise the temperature to 50-55°C, slowly add 200mL of purified water dropwise, cool to 15-20°C for suction filtration, and vacuum bake at 50-60°C5 Hours, 19.44 g of azithromycin monohydrate was obtained, with a yield of 97.2% and a HPLC (high performance liquid chromatography) purity of 99.2%.

Embodiment 2

[0028] Put 20g of azithromycin dihydrate into a mixed solvent of 10mL of methanol and 50mL of acetone, heat up to 40-45°C, slowly add 200mL of purified water dropwise, cool to 15-20°C for suction filtration, and vacuum bake at 50-60°C for 5 Hours, 19.21 g of azithromycin monohydrate was obtained, yield: 96.1%, HPLC purity 98.5%.

Embodiment 3

[0030] Put 20 grams of azithromycin dihydrate into a mixed solvent of 50 mL of methanol and 10 mL of acetone, raise the temperature to 65-70 °C, slowly add 200 mL of purified water dropwise, cool to 15-20 °C for suction filtration, and vacuum bake at 50-60 °C for 5 Hours, 19.03 g of azithromycin monohydrate was obtained, yield: 95.15%, HPLC purity 98.6%.

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 mainly discloses a method for preparing an azithromycin monohydrate. The azithromycin monohydrate is prepared by crystallizing an azithromycin dihydrate or 9-deoxo-9a-aza-9a-homoerythromycin A which are taken as raw materials. The method comprises the following steps of: slowly adding the raw materials and water which is taken as an anti-solvent-out agent into an acetone-methanol mixed solvent at proper temperature, crystallizing, filtering, and baking under baking conditions to obtain the stable azithromycin monohydrate in which the residual quantity of the solvent is qualified. The method is easy to operate and high in yield (more than or equal to 95 percent), the quality is high (more than or equal to 98.5 percent), and the obtained product has a good crystal form, is high in fluidity and preparation adaptability, and can be industrially controlled easily.

Description

technical field [0001] The invention relates to a preparation method of azithromycin monohydrate, belonging to the technical field of preparation of macrolide drugs. Background technique [0002] Azithromycin is as the second generation erythromycin product, and its structural formula is: [0003] [0004] Azithromycin is the first semi-synthetic aza-15-membered ring macrolide antibiotic. Compared with erythromycin, azithromycin retains the advantages of erythromycin and further expands its antibacterial spectrum. Azithromycin is effective against some difficult bacteria. Bactericidal effect, especially for Gram-negative bacteria. It is widely used in respiratory system, urinary system, skin and soft tissue infections, etc. It is approved by the US FDA to replace penicillins as the first-line anti-infective drug, and it can also treat mycobacterial infection in AIDS patients. Another outstanding advantage of azithromycin is that it has unique pharmacokinetic properties....

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 Patents(China)
IPC IPC(8): C07H17/00C07H1/00
Inventor 金勇乔伟侯仲轲王兆刚邱家军
Owner ZHEJIANG GUOBANG PHARMA