CN1069647C - Compound with broad-spectrum antibacterial action - Google Patents
Compound with broad-spectrum antibacterial action Download PDFInfo
- Publication number
- CN1069647C CN1069647C CN98110427A CN98110427A CN1069647C CN 1069647 C CN1069647 C CN 1069647C CN 98110427 A CN98110427 A CN 98110427A CN 98110427 A CN98110427 A CN 98110427A CN 1069647 C CN1069647 C CN 1069647C
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- CN
- China
- Prior art keywords
- compound
- erdosteine
- broad
- azithromycin
- trachitis
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
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Abstract
The present invention relates to a compound with a broad-spectrum antibacterial function. Macrolide antibiotic azithromycin and expectorant erdosteine are combined into double salt, and the molar ratio of a molecule is 1:2. The main clinical application of the present invention is to cure excessive phlegm type trachitis and upper respiratory tract infection. The compound can be prepared into capsules, tablets, injections, oral medicinal liquid and granules. In the compound of the present invention, erdosteine and azithromycin have coordinating antibacterial functions to cause the concentration of azithromycin in the position of trachitis to be increased. The curative effect of azithromycin to excessive phlegm type trachitis can be increased, and the administration trouble of two kinds of medicine can be reduced.
Description
The present invention relates to a kind of compound and uses thereof, belong to chemical pharmacy field with broad-spectrum antibacterial action.
Broad spectrum antibiotic commonly used is in the recent period treated various inflammation, and clinical have anti-inflammatory curative effect preferably, but when treatment abundant expectoration type trachitis, because the obstruction of sticking phlegm, antimicrobial drug itself is difficult for reaching inflammation part, thereby is difficult for reaching effective treatment concentration.French Patent (FR8503679) is illustrated, a kind of salt of forming by erythromycin and Erdosteine [(±)-N-(Carboxymethylthioacetyl)-homocysteine thiolactone], curative effect to erythromycin is improved, but still have deficiency, the one, erythromycin itself is unstable to acid, with sour salify self structure is destroyed, two is that two kinds of salifiable ratios of composition do not conform to clinical medicine dose.
The objective of the invention is at the problems referred to above, invent a kind of double salt of forming by broad spectrum antibiotic Azythromycin and Erdosteine.
The present invention is achieved in that by macrolide antibiotics Azythromycin (Azithromycin) and combines generation double salt with expectorant Erdosteine [(±)-N-(Carboxymethylthioacetyl)-homocysteine thiolactone].Its structural formula is as follows:
In the The compounds of this invention, the mole ratio of having divided of Azythromycin and Erdosteine is 1: 2.Its clinical main application is treatment abundant expectoration type trachitis and upper respiratory tract infection.Compound of the present invention can be made capsule, tablet, injection, oral liquid, electuary.
The present invention has in the compound of broad-spectrum antibacterial action, two bases are arranged in the Azythromycin molecule, and becoming the molecules of salt mol ratio with Erdosteine is 1: 2, and molecular weight ratio is to be equivalent to 500: 332 at 749: 498, dosage during just with clinical being used is suitable, and Azythromycin is more stable to acid.The phlegm-dispelling functions that Erdosteine is stronger in the The compounds of this invention can be coordinated with the anti-microbial effect of Azythromycin, Azythromycin is improved in the concentration at bronchitis position, both promoted and improved the curative effect of Azythromycin, can reduce the trouble of taking two kinds of medicines again abundant expectoration type trachitis.
The present invention prepares embodiment:
Embodiment 1
The 500g Azythromycin is dissolved in 2 liters the methylene dichloride, drip 332g Erdosteine and 1 liter of solution that methylene dichloride forms in 5-10 ℃, after adding, in stirring at room 30 minutes, remove methylene dichloride under reduced pressure, get the crude product of quantitative salt, get elaboration, be white crystal with 1: 1 methylene dichloride/normal hexane recrystallization.Yield 85%.
Embodiment 2
Azythromycin and the Erdosteine molecule mol ratio with 1: 2 is added in 1 liter of distilled water, is stirred to CL, Sterile Filtration gets clear liquid, with lyophilize under the clear liquid aseptic condition (20 ℃), quantitative salt crystal.Yield 100%.
Claims (2)
1, a kind of compound with broad-spectrum antibacterial action is characterized in that combining generation double salt with the expectorant Erdosteine by the macrolide antibiotics Azythromycin, and its structural formula is as follows:
The molecule mole ratio of Azythromycin and Erdosteine is 1: 2.
2, the described purposes of compound in the medicine of preparation treatment abundant expectoration type trachitis and upper respiratory tract infection of a kind of claim 1 with broad-spectrum antibacterial action.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN98110427A CN1069647C (en) | 1998-08-31 | 1998-08-31 | Compound with broad-spectrum antibacterial action |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN98110427A CN1069647C (en) | 1998-08-31 | 1998-08-31 | Compound with broad-spectrum antibacterial action |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1246482A CN1246482A (en) | 2000-03-08 |
| CN1069647C true CN1069647C (en) | 2001-08-15 |
Family
ID=5220475
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN98110427A Expired - Fee Related CN1069647C (en) | 1998-08-31 | 1998-08-31 | Compound with broad-spectrum antibacterial action |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1069647C (en) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR057882A1 (en) | 2005-11-09 | 2007-12-26 | Novartis Ag | DOUBLE ACTION COMPOUNDS OF ANGIOTENSIN RECEPTOR BLOCKERS AND NEUTRAL ENDOPEPTIDASE INHIBITORS |
| CN101810633B (en) * | 2010-03-31 | 2011-12-14 | 湖北丝宝药业有限公司 | Applications of dirithromycin to preparation of medicines for treating chronic noninfective respiratory diseases |
| CN105395538B (en) * | 2015-12-15 | 2016-07-20 | 刘月平 | A kind of pharmaceutical composition treating acute upper respiratory tract infection |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1054535A (en) * | 1990-03-05 | 1991-09-18 | 吉林省农业科学院长白山生物资源研究所 | Nutrient-extracting technology from fresh ginseng stem and leaf |
-
1998
- 1998-08-31 CN CN98110427A patent/CN1069647C/en not_active Expired - Fee Related
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1054535A (en) * | 1990-03-05 | 1991-09-18 | 吉林省农业科学院长白山生物资源研究所 | Nutrient-extracting technology from fresh ginseng stem and leaf |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1246482A (en) | 2000-03-08 |
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| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C06 | Publication | ||
| PB01 | Publication | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20010815 Termination date: 20150831 |
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| EXPY | Termination of patent right or utility model |