CN102988286A - Enrofloxacin injection - Google Patents
Enrofloxacin injection Download PDFInfo
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- CN102988286A CN102988286A CN2012105405838A CN201210540583A CN102988286A CN 102988286 A CN102988286 A CN 102988286A CN 2012105405838 A CN2012105405838 A CN 2012105405838A CN 201210540583 A CN201210540583 A CN 201210540583A CN 102988286 A CN102988286 A CN 102988286A
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Abstract
The invention aims at disclosing enrofloxacin injection. The injection comprises the following components according to weight percentage: 1%-10% of enrofloxacin, acid which is 0.1mol to 5mol more than the enrofloxacin or 0.1mol to 5mol of other mixed acid, preparation auxiliaries accounting for 0.1%-30% of a solution, and the balance of injection water. Compared with the prior art, the enrofloxacin injection functions rapidly as active substances achieve high blood concentration within a short time after being applied, and the active substances are also eliminated rapidly, so that the enrofloxacin injection is particularly suitable for treatment of animals serving as food products, and the purpose of the enrofloxacin injection is achieved.
Description
Technical field
The present invention relates to a kind of injection and preparation method thereof, particularly a kind of enrofloxacin injection that is applicable to brutish high-efficiency antimicrobial.
Background technology
Enrofloxacin (Enrofloxacin) has another name called grace fluorine quinoline carboxylic acid, belongs to the chemosynthesis antibacterial of Fluoroquinolones (Fluoroquinolones), be little yellow or light yellow crystalline powder, bitter in the mouth, water insoluble, be soluble in the organic solvents such as sodium hydroxide solution, methanol and cyanogen methane.The absorption of for oral administration and intramuscular injection rapidly and more complete, blood medicine degree reached the peak in 0.5-2 hour.Except the central nervous system, the drug level of nearly all tissue all is higher than blood plasma, and this is conducive to the treatment of systemic infection and deep tissue infection.This product is eliminated by kidney and non-kidney mode, and approximately the medicine original shape of 15%-50% passes through homaluria.Metabolism in animal body mainly is to slough ethyl and become ciprofloxacin.This product is the broad-spectrum sterilization medicine, and mycoplasma is had specially good effect.Escherichia coli, klebsiella bacillus, Salmonella, Bacillus proteus, bacillus pyocyaneus, haemophilus, pasteurella multocida, pasteurella haemolytica, golden Portugal bacterium and streptococcus etc. there is sterilization effectiveness.
Enrofloxacin is as the animal-use drug product, long half time in animal body has good tissue distribution, belongs to the broad-spectrum antibacterial, have bacteriostasis for gram positive bacteria, negative bacterium and mould slurry, once be used in the vibrio disease of cultured fishes and the control of escherichia coli disease.
But, present known enrofloxacin injection, onset is slower, and active substance is eliminated slower.
Therefore, need especially a kind of enrofloxacin injection, solved the problem of above-mentioned existing existence.
Summary of the invention
The object of the present invention is to provide a kind of enrofloxacin injection, for the deficiencies in the prior art, after the administration at short notice active substance can reach high blood drug level, rapid-action, active substance is eliminated also fast, is particularly suitable for being used for the treatment of animals (waiting time is short) of food product.
Technical problem solved by the invention can realize by the following technical solutions:
A kind of enrofloxacin injection is characterized in that, it comprises the following component of percentage by weight: enrofloxacin 1%-10%, and be in excess in acid or its mixed acid 0.1-5mol of enrofloxacin 0.1-5mol and account for the formulation auxiliary agents of solution 0.1-30%, surplus is water for injection.
In one embodiment of the invention, described enrofloxacin is preferably 2.5%-10%.
In one embodiment of the invention, described acid or its mixed acid are in excess in enrofloxacin and are preferably 0.1-1mol.
In one embodiment of the invention, described acid is the form of open chain or the form of lactone.
In one embodiment of the invention, described acid comprises one or several the combination in multi-hydroxy carboxy acid, aminoacid, hydrochloric acid, methanesulfonic acid, ethyl sulfonic acid, propanoic acid, succinic acid, 1,3-propanedicarboxylic acid, citric acid, ascorbic acid, phosphoric acid or the lactic acid.
Further, described multi-hydroxy carboxy acid is one or several the combination in gluconic acid, galacturonic acid, glucuronic acid or the lactobionic acid.
Further, described aminoacid is one or more the combination in glutamic acid or the aspartic acid.
In one embodiment of the invention, described enrofloxacin injection comprises that also percentage by weight is the liquid carrier of 1-30%.
Further, described liquid carrier comprises ethanol, glycerol, propylene glycol, the combination of one or several in Polyethylene Glycol or the 2,2'-ethylenedioxybis(ethanol)..
In one embodiment of the invention, the pH value of described enrofloxacin injection is 3-5.5, and Osmolality is 200-900 mM of osmotic pressure concentration/kilogram.
Further, preferably, the pH value of described enrofloxacin injection is 3.5-5, and Osmolality is 260-390 mM of osmotic pressure concentration/kilogram.
In one embodiment of the invention, described formulation auxiliary agents comprises one or several the combination in thickening agent, absorbent, light stabilizer, crystallization blocker, chelating agent, antioxidant, antiseptic or the local anesthetic.
Further, described thickening agent comprises one or several the combination in methylcellulose, hydroxyethyl-cellulose, hydroxypropyl cellulose, sodium carboxymethyl cellulose, polyvinylpyrrolidone or the gelatin.
Further, described chelating agent comprises one or several the combination in NaEDTA, phosphate, nitrate, acetate or the citrate.
Further, described antioxidant comprises one or several the combination in ascorbic acid, sulfite compound, Cys, thio-2 acid, thiolactic acid or the monothioglycerol.
Further, described antiseptic comprises PHB ester, phenol and derivant, methaform, benzylalcohol, ethanol, butanols, l, the combination of one or several in 3 one butanediols, chlorhexidine salt, benzoic acid and salt or the sorbic acid.
Further, described local anesthetic comprises one or several the combination in procaine hydrochloride or the lidocaine hydrochloride.
Enrofloxacin injection of the present invention, compared with prior art, after the administration at short notice active substance can reach high blood drug level, rapid-action, it is also fast that active substance is eliminated, and is particularly suitable for being used for the treatment of animals of food product, realizes purpose of the present invention.
Characteristics of the present invention can be consulted the detailed description of the better embodiment of this case and be obtained to be well understood to.
The specific embodiment
For technological means, creation characteristic that the present invention is realized, reach purpose and effect is easy to understand, further set forth the present invention below in conjunction with concrete.
Enrofloxacin injection of the present invention, it comprises the following component of percentage by weight: enrofloxacin 1%-10%, be in excess in acid or its mixed acid 0.1-5mol of enrofloxacin 0.1-5mol and account for the formulation auxiliary agents of solution 0.1-30%, surplus is water for injection.
In the present invention, described enrofloxacin is preferably 2.5%-10%.
In the present invention, described acid or its mixed acid are in excess in enrofloxacin and are preferably 0.1-1mol.
In the present invention, described acid is the form of open chain or the form of lactone.If the acid of using be its lactone form, then it its lactonic ring is at least part of before is hydrolyzed with enrofloxacin formation salt or complex.
In the present invention, described acid comprises one or several the combination in multi-hydroxy carboxy acid, aminoacid, hydrochloric acid, methanesulfonic acid, ethyl sulfonic acid, propanoic acid, succinic acid, 1,3-propanedicarboxylic acid, citric acid, ascorbic acid, phosphoric acid or the lactic acid.Described multi-hydroxy carboxy acid is one or several the combination in gluconic acid, galacturonic acid, glucuronic acid or the lactobionic acid.Described aminoacid is one or more the combination in glutamic acid or the aspartic acid.
In the present invention, described enrofloxacin injection comprises that also percentage by weight is the liquid carrier of 1-30%.Described liquid carrier comprises ethanol, glycerol, propylene glycol, the combination of one or several in Polyethylene Glycol or the 2,2'-ethylenedioxybis(ethanol)..
In the enrofloxacin injection of the present invention, use as far as possible various materials that pH is transferred to 3-6.5, phosphoric acid for example, citric acid, three (methylol) aminomethane, ascorbic acid, acetic acid, succinic acid, tartaric acid, gluconic acid and lactic acid, and their salt.
The pH value of described enrofloxacin injection is 3-5.5, and Osmolality is 200-900 mM of osmotic pressure concentration/kilogram.Preferably, the pH value of described enrofloxacin injection is 3.5-5, and Osmolality is 260-390 mM of osmotic pressure concentration/kilogram.
Described enrofloxacin injection can be by adding NaCI, glucose, fructose, glycerol, sorbitol, mannitol, sucrose or xylose, or the mixture of these materials such as adapts at the condition of oozing.
In the present invention, described formulation auxiliary agents comprises one or several the combination in thickening agent, absorbent, light stabilizer, crystallization blocker, chelating agent, antioxidant, antiseptic or the local anesthetic.
Described thickening agent comprises one or several the combination in methylcellulose, hydroxyethyl-cellulose, hydroxypropyl cellulose, sodium carboxymethyl cellulose, polyvinylpyrrolidone or the gelatin.Described chelating agent comprises one or several the combination in NaEDTA, phosphate, nitrate, acetate or the citrate.Described antioxidant comprises one or several the combination in ascorbic acid, sulfite compound, Cys, thio-2 acid, thiolactic acid or the monothioglycerol.Described antiseptic comprises PHB ester, phenol and derivant, methaform, benzylalcohol, ethanol, butanols, l, the combination of one or several in 3 one butanediols, chlorhexidine salt, benzoic acid and salt or the sorbic acid.Described local anesthetic comprises one or several the combination in procaine hydrochloride or the lidocaine hydrochloride.
The preparation method of enrofloxacin injection of the present invention adds formulation auxiliary agents again for enrofloxacin is added in the solution of entry in stirring, if need to be diluted with water to the concentration that needs.
The pH of water soluble preparation of the present invention is 3-5.5, is preferably 3.5-5.The Osmolality of water base suspension is 200-900 mM of osmotic pressure concentration/kilogram, is preferably 260-390 mM of osmotic pressure concentration/kilogram, and
The salt that enrofloxacin injection of the present invention can become with respective acids from enrofloxacin or begin preparation from its hydrate.
Yet, also can directly prepare salt in the solution with being added to for the acid that forms the required some of salt.But under 30-69 ℃ of temperature, carry out accelerate dissolution.Can be at obtain solution under the blanket of nitrogen.Can be made into the solution of active substance ready for using with this method, and the solution of making is packed in the suitable vessel, for example, the ampoule bottle of packing into; In injection bottle or the infusion bottle, or make the precursor that is fit to this solution of preparation, for example, concentrated solution or lyophilization thing.The container of dress preparation can be made or is made of plastics by glass, can contain some plays special protection function to content material in the material of preparation container, for example, and protection light and oxygen.The preparation of solution can be carried out in being with or without the batch container of heat transfer jacket among the following embodiment.When using the container that can not heat, if necessary available preheating water.
Although solvent can be added in the solid,, generally be after first most of solvent being put into container, again each composition to be dissolved wherein in succession.
When using sour lactone form, before adding, active component first with its dissolving, normally uses heating or the method for placement a period of time, so that lactone is hydrolyzed into free acid.Temperature used herein is 40-70 ℃, is preferably 50-60 ℃.Before the cooling or after the cooling, under agitation other composition in turn is dissolved into or is mixed in the preparation liquid, supply remaining solvent after, can come sterilising filtration by suitable bacteria filter and/or heat sterilization.
Above demonstration and described ultimate principle of the present invention and principal character and advantage of the present invention.The technical staff of the industry should understand; the present invention is not restricted to the described embodiments; that describes in above-described embodiment and the description just illustrates principle of the present invention; without departing from the spirit and scope of the present invention; the present invention also has various changes and modifications; these changes and improvements all fall in the claimed scope of the invention, and the claimed scope of the present invention is defined by appending claims and equivalent thereof.
Claims (17)
1. enrofloxacin injection, it is characterized in that, it comprises the following component of percentage by weight: enrofloxacin 1%-10%, and be in excess in acid or its mixed acid 0.1-5mol of enrofloxacin 0.1-5mol and account for the formulation auxiliary agents of solution 0.1-30%, surplus is water for injection.
2. enrofloxacin injection as claimed in claim 1 is characterized in that, described enrofloxacin is preferably 2.5%-10%.
3. enrofloxacin injection as claimed in claim 1 is characterized in that, described acid or its mixed acid are in excess in enrofloxacin and are preferably 0.1-1mol.
4. enrofloxacin injection as claimed in claim 1 is characterized in that, described acid is the form of open chain or the form of lactone.
5. enrofloxacin injection as claimed in claim 1, it is characterized in that, described acid comprises one or several the combination in multi-hydroxy carboxy acid, aminoacid, hydrochloric acid, methanesulfonic acid, ethyl sulfonic acid, propanoic acid, succinic acid, 1,3-propanedicarboxylic acid, citric acid, ascorbic acid, phosphoric acid or the lactic acid.
6. enrofloxacin injection as claimed in claim 5 is characterized in that, described multi-hydroxy carboxy acid is one or several the combination in gluconic acid, galacturonic acid, glucuronic acid or the lactobionic acid.
7. enrofloxacin injection as claimed in claim 5 is characterized in that, described aminoacid is one or more the combination in glutamic acid or the aspartic acid.
8. enrofloxacin injection as claimed in claim 1 is characterized in that, described enrofloxacin injection comprises that also percentage by weight is the liquid carrier of 1-30%.
9. enrofloxacin injection as claimed in claim 8 is characterized in that, described liquid carrier comprises ethanol, glycerol, propylene glycol, the combination of one or several in Polyethylene Glycol or the 2,2'-ethylenedioxybis(ethanol)..
10. enrofloxacin injection as claimed in claim 1 is characterized in that, the pH value of described enrofloxacin injection is 3-5.5, and Osmolality is 200-900 mM of osmotic pressure concentration/kilogram.
11. enrofloxacin injection as claimed in claim 10 is characterized in that, preferably, the pH value of described enrofloxacin injection is 3.5-5, and Osmolality is 260-390 mM of osmotic pressure concentration/kilogram.
12. enrofloxacin injection as claimed in claim 1 is characterized in that, described formulation auxiliary agents comprises one or several the combination in thickening agent, absorbent, light stabilizer, crystallization blocker, chelating agent, antioxidant, antiseptic or the local anesthetic.
13. enrofloxacin injection as claimed in claim 12, it is characterized in that, described thickening agent comprises one or several the combination in methylcellulose, hydroxyethyl-cellulose, hydroxypropyl cellulose, sodium carboxymethyl cellulose, polyvinylpyrrolidone or the gelatin.
14. enrofloxacin injection as claimed in claim 12 is characterized in that, described chelating agent comprises one or several the combination in NaEDTA, phosphate, nitrate, acetate or the citrate.
15. enrofloxacin injection as claimed in claim 12 is characterized in that, described antioxidant comprises one or several the combination in ascorbic acid, sulfite compound, Cys, thio-2 acid, thiolactic acid or the monothioglycerol.
16. enrofloxacin injection as claimed in claim 12, it is characterized in that, described antiseptic comprises PHB ester, phenol and derivant, methaform, benzylalcohol, ethanol, butanols, l, the combination of one or several in 3 one butanediols, chlorhexidine salt, benzoic acid and salt or the sorbic acid.
17. enrofloxacin injection as claimed in claim 12 is characterized in that, described local anesthetic comprises one or several the combination in procaine hydrochloride or the lidocaine hydrochloride.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012105405838A CN102988286A (en) | 2012-12-13 | 2012-12-13 | Enrofloxacin injection |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012105405838A CN102988286A (en) | 2012-12-13 | 2012-12-13 | Enrofloxacin injection |
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| Publication Number | Publication Date |
|---|---|
| CN102988286A true CN102988286A (en) | 2013-03-27 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2012105405838A Pending CN102988286A (en) | 2012-12-13 | 2012-12-13 | Enrofloxacin injection |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103191055A (en) * | 2013-04-24 | 2013-07-10 | 重庆市畜牧科学院 | Preparation method of orbifloxacin injection |
| CN105412019A (en) * | 2016-01-11 | 2016-03-23 | 郭敏 | Soluble enrofloxacin powder and preparation method thereof |
| CN105434359A (en) * | 2016-01-11 | 2016-03-30 | 郭敏 | Enrofloxacin preparation and preparation method thereof |
| CN110248643A (en) * | 2017-02-13 | 2019-09-17 | 拜耳动物保健有限责任公司 | Liquid composition containing Pradofloxacin |
| CN110680801A (en) * | 2019-10-21 | 2020-01-14 | 庞燕 | Anhydrous calcium chloride enrofloxacin injection for livestock as well as preparation method and application thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1706386A (en) * | 2005-04-29 | 2005-12-14 | 史同瑞 | Enrofloxacin suspension and its prepn process |
| CN102415991A (en) * | 2011-11-24 | 2012-04-18 | 陈鹏举 | Enrofloxacin long-acting injection and preparation method thereof |
-
2012
- 2012-12-13 CN CN2012105405838A patent/CN102988286A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1706386A (en) * | 2005-04-29 | 2005-12-14 | 史同瑞 | Enrofloxacin suspension and its prepn process |
| CN102415991A (en) * | 2011-11-24 | 2012-04-18 | 陈鹏举 | Enrofloxacin long-acting injection and preparation method thereof |
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103191055A (en) * | 2013-04-24 | 2013-07-10 | 重庆市畜牧科学院 | Preparation method of orbifloxacin injection |
| CN105412019A (en) * | 2016-01-11 | 2016-03-23 | 郭敏 | Soluble enrofloxacin powder and preparation method thereof |
| CN105434359A (en) * | 2016-01-11 | 2016-03-30 | 郭敏 | Enrofloxacin preparation and preparation method thereof |
| CN110248643A (en) * | 2017-02-13 | 2019-09-17 | 拜耳动物保健有限责任公司 | Liquid composition containing Pradofloxacin |
| CN110248643B (en) * | 2017-02-13 | 2023-11-24 | 拜耳动物保健有限责任公司 | Liquid composition containing prafloxacin |
| CN110680801A (en) * | 2019-10-21 | 2020-01-14 | 庞燕 | Anhydrous calcium chloride enrofloxacin injection for livestock as well as preparation method and application thereof |
| CN110680801B (en) * | 2019-10-21 | 2022-10-18 | 庞燕 | Anhydrous calcium chloride enrofloxacin injection for livestock as well as preparation method and application thereof |
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Application publication date: 20130327 |