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Azitromycin double salts and their preparing method and use

A technology for azithromycin and uses, applied in the field of medicine and preparation thereof, can solve the problems that azithromycin is difficult to reach the inflammatory site, difficult to reach the therapeutic concentration, self-structure damage, etc., and achieves the effects of improving water solubility, increasing concentration and reducing trouble

Inactive Publication Date: 2006-05-24
西安新安医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These two patents disclose that azithromycin has antibacterial properties and is therefore used as an antibiotic. It has good clinical anti-inflammatory effects. However, when treating phlegm-proliferating inflammation, azithromycin itself is difficult to reach the inflammatory site due to the hindrance of sticky phlegm. reach effective therapeutic concentrations
French patent (FR8503679) invented a salt composed of erythromycin and erdosteine ​​to treat phlegm-proliferating inflammation, but erythromycin itself is unstable to acid, and salt formation with acid will destroy its own structure
At present, there is no public report on the combination of azithromycin and fudosteine ​​to form a double salt

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Dissolve 749g of azithromycin in 2 liters of dichloromethane, add 358g of fudosteine ​​solution in dichloromethane dropwise at 5-10°C, stir at room temperature for half an hour after the addition, distill off the dichloromethane under reduced pressure to obtain azithromycin The crude compound salt of fudosteine ​​was recrystallized from dichloromethane / n-hexane to obtain the refined product, and dried under vacuum at 40°C to obtain a white crystalline powder.

Embodiment 2

[0027] Add 749 g of azithromycin and 358 g of fudosteine ​​to 10 liters of water, stir at room temperature until the raw materials are completely dissolved, the pH is 7.3, and spray-dried to obtain a white powder, namely azithromycin-fudosteine ​​double salt.

Embodiment 3

[0029] Add 749g of azithromycin and 358g of fudosteine ​​into 10 liters of water, stir at room temperature until the raw materials are completely dissolved, the pH is 7.4, sterilize and filter to obtain the clear liquid, and freeze-dry the clear liquid under aseptic conditions (-30°C) to obtain quantitative salt Crystal, that is, azithromycin-fodosteine ​​double salt.

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PUM

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Abstract

The invention relates to an azithromycin fudosteine compound salt. Its feature is that it combines azithromycin and fudosteine, which is double to azithromycin. And its molecular formula is that C38H72N2O12.2C6H13NO3S.nH2O, n=0,1,2,3,4,5. Its advantages are that it has good water solubility and is uneasy to absorption of moisture; the aqueous solution pH value acidity is close to human-body. Using the azithromycin fudosteine compound salt as the main medicine can make various pre oral and injection preparation. The preparations are mainly used to treat abundant expectoration type infection of the respiratory.

Description

technical field [0001] The invention relates to a medicine and a preparation method thereof, in particular to a double salt of azithromycin and a preparation method and application thereof. Background technique [0002] (-)-(R)-amino-3-(3-hydroxypropyl mercapto) propionic acid is called "fudosteine" (English name: fudosteine ​​CAS: 13189-98-5) for the first time in October 2001 Listed in Japan, bronchitis is a common and frequently-occurring disease. Its morbidity and mortality are relatively high in the world and tend to increase. It is often manifested as cough, expectoration, or accompanied by shortness of breath and wheezing. , Severe cases may be complicated by emphysema, pulmonary heart disease and so on. Fudosteine ​​is a new type of expectorant, a new generation of mucolytic drugs, belonging to cysteine ​​derivatives. The indications of fudosteine ​​almost cover the symptoms of excessive phlegm and difficult cough of all respiratory diseases including bronchitis. ...

Claims

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Application Information

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IPC IPC(8): C07H17/08A61K9/20A61K9/48A61K31/7048A61P11/10C07D413/14
Inventor 苏红军
Owner 西安新安医药科技有限公司
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