CN104127382A - Emulsion cefquinome sulfate injection and preparation method thereof - Google Patents

Emulsion cefquinome sulfate injection and preparation method thereof Download PDF

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Publication number
CN104127382A
CN104127382A CN201410359402.0A CN201410359402A CN104127382A CN 104127382 A CN104127382 A CN 104127382A CN 201410359402 A CN201410359402 A CN 201410359402A CN 104127382 A CN104127382 A CN 104127382A
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injection
cefquinome sulfate
emulsion
cefquinome
preparation
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Chinese (zh)
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陈诚
王建华
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Chongqing Academy of Animal Sciences
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Chongqing Academy of Animal Sciences
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Abstract

The invention specifically relates to an emulsion cefquinome sulfate injection and a preparation method thereof, belonging to the technical field of veterinary antibiotic preparations. The invention provides the emulsion cefquinome sulfate injection to overcome technical problems. According to a technical scheme in the invention, the emulsion cefquinome sulfate injection comprises the following raw materials: cefquinome sulfate, 2.5% g/mL; an emulsifier, 0.1 to 2% w/w; a suspending aid, 0.1 to 10% w/w; deflocculant, 0.1 to 10% w/w; and balancing injection water. The invention further provides a preparation method for the injection. The injection is uniformly dispersed, has a small particle size, does not settle in a long period of time and has wide application prospects.

Description

A kind of emulsion-type Cefquinome sulfate injection and preparation method thereof
Technical field
The invention belongs to veterinary drug antibiotic formulations technical field, be specifically related to a kind of emulsion-type Cefquinome sulfate injection and preparation method thereof.
Background technology
Cefquinome sulfate, chemistry is by name: (6R, 7R)-7-[(Z)-(thiazolamine-4-yl)-2-methoxyimino acetylamino]-3-(5,6,7,8-tetrahydric quinoline group-1-methyl)-8-oxo-5-thia-1-azabicyclo [4,2,0] oct-2-ene-carboxylate, white, off-white color are to pale yellow powder.Cefquinome sulfate be the 4th generation cephalosporins animal specific medicine, there are extremely strong antibacterial activity in Dui Jin Portugal bacterium, streptococcus, Aerugo false single armful of bacterium, enterobacteria section (escherichia coli, Salmonella, klebsiella, citric acid fungus, serratia marcesens), are widely used in pig, cattle respiratory disease and milch cow, sow mastitis, endometritis; Birds is caused by intractable large intestine antiperspirant bacterium, Salmonella, bacillus pyocyaneus and staphylococcus etc. has loose bowels, the treatment of diarrhoea, pericarditis perihepatitis, there is has a broad antifungal spectrum, antibacterial action is strong, consumption is few, plasma half-life is long, without plurality of advantages such as nephrotoxicity.
Kinetics data shows, Cefquinome sulfate oral absorption is poor, and clinical conventional its sulfate is made suspension injection or ointment, through intramuscular injection or breast perfusion.Application number is the preparation method that the Chinese patent of CN101987100A discloses a kind of Cefquinome sulfate suspension injection, take Cefquinome sulfate micropowder, vitamin E is raw material, ethyl oleate is that oil for injection is made suspension injection, improves safety, reduces intramuscular injection zest.Application number is that the Chinese patent of CN102319210A discloses a kind of Veterinary long-acting cefquinome sulfate injection and preparation method thereof, this injection is that castor oil hydrogenated and soybean lecithin proportioning mixture, antibacterial chlorobutanol, emulsifying dispersant Arlacel-60 and solvent Macrogol 200 form by Cefquinome sulfate, suspending agent, can prolong drug effective acting time in vivo, reduce medication number of times.Application number is that the Chinese patent of CN102614184A discloses sulfated compound cefquinome suspensoid and preparation method thereof for a kind of domestic animal, this invention be take Cefquinome sulfate, florfenicol, aluminium stearate, the light base toluene of dibutyl, benzyl alcohol, tween 80, ethyl oleate and is made suspension injection as component, to compare antimicrobial spectrum wider with single preparations of ephedrine, and antibacterial action is stronger.At present on the market be all suspensoid, product produces precipitation, particle diameter is larger.
Summary of the invention
The technical problem to be solved in the present invention is to provide a kind of emulsion-type Cefquinome sulfate injection.
Technical scheme of the present invention is a kind of emulsion-type Cefquinome sulfate injection, consists of: Cefquinome sulfate 2.5%g/mL, emulsifying agent 0.1~2%w/w, suspending agent 0.1~10%w/w, deflocculant 0.1~10%w/w, surplus are water for injection the raw material of following percentage by weight.
Concrete, described emulsifying agent is at least one in Tween-60, Tween-65, tween 80, tween 85, poloxamer-188, lecithin.
Concrete, described suspending agent is at least one in methylcellulose, hydroxypropyl emthylcellulose, carbomer, arabic gum, xanthan gum, aluminium stearate.
Concrete, described deflocculant is at least one in sodium citrate, sodium tartrate, aluminum chloride, sodium sulfate.
The present invention also provides the preparation method of described injection, comprise the steps: to take Cefquinome sulfate, emulsifying agent, suspending agent, deflocculant according to the ratio of Cefquinome sulfate 2.5%g/mL, emulsifying agent 0.1~2%w/w, suspending agent 0.1~10%w/w, deflocculant 0.1~10%w/w, in the waters for injection of 60 ℃, dissolve, standardize solution, by mulser high speed shear emulsifying 5min, finally by 3KGY, (KGY is the unit of irradiation dose, the Chinese meaning is kilogray) the sterilizing of 60Co-Y x ray irradiation x, make emulsion-type Cefquinome sulfate injection.
Beneficial effect of the present invention: add emulsifying agent to pass through the emulsifying of mulser high speed shear in the present invention and can effectively disperse Cefquinome sulfate solid particle, reduce particle size, realize Cefquinome sulfate micronize, keep injection stable.The present invention is used in conjunction suspending agent and deflocculant, can improve injection viscosity and further improve stablizing effect, and by adding deflocculant to prevent that microgranule flocculation is poly-, control diameter of particle, injection is uniformly dispersed, granularity is little, precipitated and separated not for a long time, has good stability, an advantage such as mobility is high, absorption is fast, bioavailability is high, good effect, intramuscular injection zest are little, high-low temperature resistant, animal tolerance.
Accompanying drawing explanation
Resulting cefquinome sulfate injection granularmetric analysis in Fig. 1 embodiment 1
Resulting cefquinome sulfate injection granularmetric analysis in Fig. 2 embodiment 2
The specific embodiment
The preparation of embodiment 1 injection of the present invention
Take Cefquinome sulfate 1.25g, Tween-60 0.5g, methylcellulose 1.0g, sodium citrate 1.0g is in beaker, then add the water for injection of 60 ℃ to be settled to 50mL, by mulser high speed shear emulsifying 5min, finally by the 60Co-Y x ray irradiation x sterilizing of 3KGY, make emulsion-type Cefquinome sulfate injection.
Get Cefquinome sulfate emulsion, add in laser particle size analyzer, measure its particle diameter, the results are shown in Figure 1, measuring its mean diameter is 0.941 μ m.
The preparation of embodiment 2 injections of the present invention
Take Cefquinome sulfate 1.25g, Tween-65 0.6g, hydroxypropyl emthylcellulose 1.2g, sodium tartrate 1.1g is in beaker, then add the water for injection of 60 ℃ to be settled to 50mL, by mulser high speed shear emulsifying 5min, finally by the 60Co-Y x ray irradiation x sterilizing of 3KGY, make emulsion-type Cefquinome sulfate injection.
Get Cefquinome sulfate emulsion, add in laser particle size analyzer, measure its particle diameter and see Fig. 2, measuring its mean diameter is 0.805 μ m.
The preparation of embodiment 3 injections of the present invention
Take Cefquinome sulfate 1.25g, tween 80 0.7g, Acritamer 940 0.4g, aluminum chloride 1.5g is in beaker, then add the water for injection of 60 ℃ to be settled to 50mL, by mulser high speed shear emulsifying 5min, finally by the 60Co-Y x ray irradiation x sterilizing of 3KGY, make emulsion-type Cefquinome sulfate injection.
Get Cefquinome sulfate emulsion, add in laser particle size analyzer, measuring its mean diameter is 1.085 μ m.
The preparation of embodiment 4 injections of the present invention
Take Cefquinome sulfate 1.25g, tween 85 1.4g, arabic gum 1.8g, sodium sulfate 1.5g is in beaker, then add the water for injection of 60 ℃ to be settled to 50mL, by mulser high speed shear emulsifying 5min, finally by the 60Co-Y x ray irradiation x sterilizing of 3KGY, make emulsion-type Cefquinome sulfate injection.
Get Cefquinome sulfate emulsion, add in laser particle size analyzer, measuring its mean diameter is 1.214 μ m.
The preparation of embodiment 5 injections of the present invention
Take Cefquinome sulfate 1.25g, poloxamer-188 0.4g, xanthan gum 0.4g, sodium sulfate 1.5g is in beaker, then add the water for injection of 60 ℃ to be settled to 50mL, by mulser high speed shear emulsifying 5min, finally by the 60Co-Y x ray irradiation x sterilizing of 3KGY, make emulsion-type Cefquinome sulfate injection.
Get Cefquinome sulfate emulsion, add in laser particle size analyzer, measuring its mean diameter is 1.174 μ m.
The preparation of embodiment 6 injections of the present invention
Take Cefquinome sulfate 1.25g, lecithin 0.8g, aluminium stearate 1.0g, aluminum chloride 1.0g is in beaker, then add the water for injection of 60 ℃ to be settled to 50mL, by mulser high speed shear emulsifying 5min, finally by the 60Co-Y x ray irradiation x sterilizing of 3KGY, make emulsion-type Cefquinome sulfate injection.
Get Cefquinome sulfate emulsion, add in laser particle size analyzer, measuring its mean diameter is 0.962 μ m.
Embodiment 1~6 is obtained to injection and carry out stability test.Accelerated test refers to places injection 6 months at 40 ℃ of temperature; Long term test refers to places injection 18 months at 25 ℃.
Table 1 cefquinome sulfate injection stability test

Claims (5)

1. an emulsion-type Cefquinome sulfate injection, is characterized in that: following raw materials according, consist of: Cefquinome sulfate 2.5%g/mL, emulsifying agent 0.1~2%w/w, suspending agent 0.1~10%w/w, deflocculant 0.1~10%w/w, surplus are water for injection.
2. injection as claimed in claim 1, is characterized in that: described emulsifying agent is at least one in Tween-60, Tween-65, tween 80, tween 85, poloxamer-188, lecithin.
3. injection as claimed in claim 1 or 2, is characterized in that: described suspending agent is at least one in methylcellulose, hydroxypropyl emthylcellulose, carbomer, arabic gum, xanthan gum, aluminium stearate.
4. the injection as described in claim 1~3 any one, is characterized in that: described deflocculant is at least one in sodium citrate, sodium tartrate, aluminum chloride, sodium sulfate.
5. the preparation method of emulsion-type Cefquinome sulfate injection, it is characterized in that: comprise the steps: to take Cefquinome sulfate, emulsifying agent, suspending agent, deflocculant according to the ratio of Cefquinome sulfate 2.5%g/mL, emulsifying agent 0.1~2%w/w, suspending agent 0.1~10%w/w, deflocculant 0.1~10%w/w, in the waters for injection of 60 ℃, dissolve, standardize solution, by mulser high speed shear emulsifying 5min, finally by the 60Co-Y x ray irradiation x sterilizing of 3KGY, make emulsion-type Cefquinome sulfate injection.
CN201410359402.0A 2014-07-25 2014-07-25 Emulsion cefquinome sulfate injection and preparation method thereof Pending CN104127382A (en)

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Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105287374A (en) * 2015-12-07 2016-02-03 中牧南京动物药业有限公司 Preparation method of cefquinome sulfate breast injectant and obtained preparation
CN107049943A (en) * 2017-05-10 2017-08-18 郑州百瑞动物药业有限公司 Milk cow Ceftiofur Hydrochloride injecta and preparation method thereof
CN111450057A (en) * 2020-06-03 2020-07-28 江苏中牧倍康药业有限公司 Cefquinome sulfate self-microemulsion and preparation method thereof
CN111450114A (en) * 2020-05-21 2020-07-28 苏州汇涵医用科技发展有限公司 Compound disinfectant liquid containing hydrogen peroxide and silver ions and preparation method thereof

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Publication number Priority date Publication date Assignee Title
CN102319210A (en) * 2011-09-29 2012-01-18 武汉回盛生物科技有限公司 A kind of long-acting veterinary cefquinome sulfate injection and preparation method thereof
CN103169654A (en) * 2011-12-20 2013-06-26 普莱柯生物工程股份有限公司 Aqueous suspension injection contain Cefquinome sulfate and preparation method
CN103751103A (en) * 2014-02-21 2014-04-30 山东鲁抗立科药业有限公司 Long-acting cefquinome sulfate injection and preparation method thereof

Patent Citations (3)

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Publication number Priority date Publication date Assignee Title
CN102319210A (en) * 2011-09-29 2012-01-18 武汉回盛生物科技有限公司 A kind of long-acting veterinary cefquinome sulfate injection and preparation method thereof
CN103169654A (en) * 2011-12-20 2013-06-26 普莱柯生物工程股份有限公司 Aqueous suspension injection contain Cefquinome sulfate and preparation method
CN103751103A (en) * 2014-02-21 2014-04-30 山东鲁抗立科药业有限公司 Long-acting cefquinome sulfate injection and preparation method thereof

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Title
杨明: "《中药药剂学》", 31 August 2008 *

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105287374A (en) * 2015-12-07 2016-02-03 中牧南京动物药业有限公司 Preparation method of cefquinome sulfate breast injectant and obtained preparation
CN107049943A (en) * 2017-05-10 2017-08-18 郑州百瑞动物药业有限公司 Milk cow Ceftiofur Hydrochloride injecta and preparation method thereof
CN107049943B (en) * 2017-05-10 2020-02-14 郑州百瑞动物药业有限公司 Ceftiofur hydrochloride injection for dairy cattle and preparation method thereof
CN111450114A (en) * 2020-05-21 2020-07-28 苏州汇涵医用科技发展有限公司 Compound disinfectant liquid containing hydrogen peroxide and silver ions and preparation method thereof
CN111450057A (en) * 2020-06-03 2020-07-28 江苏中牧倍康药业有限公司 Cefquinome sulfate self-microemulsion and preparation method thereof

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Application publication date: 20141105