CN101416968A - Preparation method of ceftiofur long-acting injector - Google Patents
Preparation method of ceftiofur long-acting injector Download PDFInfo
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- CN101416968A CN101416968A CNA2007101898074A CN200710189807A CN101416968A CN 101416968 A CN101416968 A CN 101416968A CN A2007101898074 A CNA2007101898074 A CN A2007101898074A CN 200710189807 A CN200710189807 A CN 200710189807A CN 101416968 A CN101416968 A CN 101416968A
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- ceftiofur
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- vitamin
- soybean oil
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Abstract
A ceftiofur long acting injection consists of the following substances: 2.5g to 5.0g of ceftiofur crude drugs, 0.5g to 3.0g of span 80, 0.1g to 0.3g of Vitamin E, 0.2g to 0.5g of aluminium stearate, 0.25g to 0.5g of chlorobutanol and soybean oil. The preparation method of the ceftiofur long acting injection comprises the following steps: (1) smashing the ceftiofur crude drugs till the particle size of the ceftiofur crude drugs is 5 Mum; (2) adding the span 80 into a mortar for grinding till the span 80 becomes even; (3) then, adding the aluminium stearate, the Vitamin E and the chlorobutanol into the mortar together; and (4) moving the mixture into a measuring vessel and adding the soybean oil into the measuring vessel till the total volume of the substances in the measuring vessel reaches 100ml. The ceftiofur long acting injection has the advantages of obvious therapeutic effect, long half-life period, less adverse reaction, reducing medication times, saving manual labor and time and the like.
Description
Technical field:
The present invention relates to a kind of preparation method of veterinary drug, relate to a kind of preparation method of ceftiofur long-acting injection specifically.
Background technology:
Ceftiofur is off-white powder, and is water insoluble, and heat decomposition temperature is 212 ℃, and pH is that 7.0 o'clock dissolubility is 8mg/ml.The molecular formula of ceftiofur is C
19H
17N
5O
7S
3Molecular weight is 523.55, chemistry [6R-[6A, 7B (z)] by name] 7-[[(A-amino-4-thiophene furan base) (methoxyimino) acetyl] amino]-3-[[(2-furan carbonyl) sulfo-] methyl]-8-oxo-5-thia-1-azabicyclo [4,2,0] oct-2-ene-2-carboxylic acid.Because of amino is arranged on thiazolyl, carboxyl is arranged on azabicyclo, so be the soda acid amphoteric compound, can generate acid soluble-salt or alkali soluble salt with hydrochloric acid and sodium hydroxide reaction.Ceftiofur is easily destroyed in highly acid or strong basicity environment, easily decomposes under hot conditions.The dried powder of its sodium salt or hydrochlorate is comparatively stable, effect duration can reach more than 2 years, but its aqueous solution only can be preserved 12h at 15-30 ℃, can preserve 7 days at 2-8 ℃, the freezing preservation for 8 weeks, it has excellent treatment effectiveness to diarrhoea, pneumonia, transmissible gastroenteritis or the mastitis of domestic animal.Because its dissolubility in water is relatively poor, suit to be mixed with suspensoid, give animal through subcutaneous or intramuscular injection then.The pharmacological efficacy of at present commercially available ceftiofur injection is shorter, thereby needs be administered once every day, logotype three days.This causes very big trouble clinically, and as labor intensive and time, animal is produced stress be waited.For reduce animal stress, reduce the medication number of times, our developmental research goes out a kind of long-acting ceftiofur injection, the purpose that the long-acting ceftiofur injection is reached is that the half-life is reached about 96h, treatment concentration is kept the long period.
Summary of the invention:
In order to overcome above-mentioned defective, the invention provides a kind of preparation method of ceftiofur long-acting injection, its half-life will reach about 96h.The half-life that mainly solves existing common ceftiofur injection is short, medication technical problem often.
For achieving the above object, the present invention adopts following technical scheme:
The preparation method of described ceftiofur long-acting injection, its injection is made up of following material:
Ceftiofur crude drug 2.5-5.0g
Sorbester p17 0.5g--3.0g
Vitamin E 0.1-0.3g
Aluminium stearate 0.2-0.5g
Chlorobutanol 0.25-0.5g
Soybean oil is to 100mL
The preparation method of described ceftiofur long-acting injection, its preparation method is:
1. to pulverize its granularity be 5 μ m to the ceftiofur crude drug;
2. adding sorbester p17 is ground in mortar evenly;
3. then with aluminium stearate, vitamin E, chlorobutanol, add in the mortar together; ,
4. move to after in the measuring device, add to 100mL with soybean oil at last.
The preparation method of described ceftiofur long-acting injection, sorbester p17 can also be by the Tween 80 of equivalent in its injection, phospholipid, poloxamer, the K value substitutes between the PVP of K12～K15.
The preparation method of described ceftiofur long-acting injection, soybean oil can also be substituted by Oleum Arachidis hypogaeae semen, the Oleum Brassicae campestris of equivalent in its injection.
The preparation method of described ceftiofur long-acting injection, vitamin E can also be substituted by dibutyl phenol, the butylated hydroxyarisol of equivalent in its injection.
Ceftiofur acts on to be pass on peptidase and blocks the synthetic of mucopeptide, and mucopeptide is the important composition composition of bacteria cell wall, the death so can make the bacteria cell wall disappearance, thus reach the effect of quick sterilization.The ceftiofur antibacterial activity is extremely strong, and gram positive bacteria, negative bacterium and anaerobe are all had higher efficacy, and also effective to the various antibacterials that can produce beta-lactamase.Ceftiofur has stable beta-lactam nucleus, is difficult for producing drug resistance.
The present invention has mainly solved the physical stability problem of ceftiofur, and the drug microparticles dispersion in this suspensoid is big, and has added stabilizing agent therein, has improved the physical stability of suspensoid.Macromolecule suspending agents such as sorbester p17, aluminium stearate, vitamin E, chlorobutanol, sodium carboxymethyl cellulose can increase the viscosity of disperse medium with sedimentation velocity that reduces microgranule and the hydrophilic that increases microgranule.Suspensoid can produce good slow releasing function to medicine, reaches long lasting purpose.
The long-acting ceftiofur injection is in the intravital pharmacokinetics research of pig
Because the highest in the various tissues behind the pig multiple dose intramuscular injection ceftiofur, for 4.47ug/ml, secondly be lung, be respectively 2.93ug/ml, be liver, fat and muscle once more, so the blood drug level of this medicine is with the assay in kidney with kidney Chinese medicine concentration.
1. test material
1.1 the injection ceftiofur contains ceftiofur 1 gram
The long-acting ceftiofur injection, 10 milliliters include ceftiofur 1 gram
1.2 test pig: 60 of 4～5 months Yorkshires
2. experimental technique:
2.1 60 pigs are divided into test and matched group, 30 of test group, 30 of matched groups at random.
2.2 the pig of test group is pressed 3mg/kg intramuscular injection long-acting ceftiofur injection, once-a-day, measures blood drug level after 3 days.
2.3 the pig of matched group is pressed 3mg/kg intramuscular injection injection ceftiofur, once-a-day, measures blood drug level after 3 days.
3. result of the test: the blood drug level of the pig of test group is 7.0mg/kg
The blood drug level of the pig of matched group is 0.5mg/kg
4. conclusion: can draw the effect that the long-acting ceftiofur injection has significant prolongation curative effect by above data.
Owing to adopted technique scheme, the present invention to have following beneficial effect:
The present invention has the effect of significant prolongation curative effect, long half time and untoward reaction are few, can reduce administration number of times again, save manpower and time, alleviate the advantages such as stress that frequent injection brings to ill domestic animal, therefore will have more wide application prospect at veterinary clinic.
The specific embodiment:
The ceftiofur long-acting injection of the present invention's preparation, its injection is made up of following material:
Ceftiofur crude drug 2.5-5.0g
Sorbester p17 0.5g--3.0g
Vitamin E 0.1-0.3g
Aluminium stearate 0.2-0.5g
Chlorobutanol 0.25-0.5g
Soybean oil is to 100mL
Embodiment 1: get ceftiofur crude drug 2.5g
Sorbester p17 0.5g
Vitamin E 0.1g
Aluminium stearate 0.2g
Chlorobutanol 0.25g
Soybean oil is to 100mL
Its preparation method is:
1. the ceftiofur crude drug being pulverized its granularity is 5 μ m,
2. add sorbester p17 and in mortar, be ground to evenly,
3. then aluminium stearate, vitamin E, chlorobutanol are added in the mortar together,
4. move at last in the measuring device, add to 100mL with soybean oil at last.
Embodiment 2: get ceftiofur crude drug 3.0g
Sorbester p17 1.0g
Vitamin E 0.1g
Aluminium stearate 0.2g
Chlorobutanol 0.25g
Soybean oil is to 100mL
Its preparation method is with embodiment 1.
Embodiment 3: get ceftiofur crude drug 4.0g
Sorbester p17 1.5g
Vitamin E 0.1g
Aluminium stearate 0.2g
Chlorobutanol 0.25g
Soybean oil is to 100mL
Its preparation method is with embodiment 1
Embodiment 4: get ceftiofur crude drug 5.0g
Sorbester p17 2.0g
Vitamin E 0.2g
Aluminium stearate 0.4g
Chlorobutanol 0.35g
Soybean oil adds to 100mL
Its preparation method is with embodiment 1
Embodiment 5: get ceftiofur crude drug 2.5g
Sorbester p17 3.0g
Vitamin E 0.3g
Aluminium stearate 0.5g
Chlorobutanol 0.5g
Soybean oil is to 100mL
Its preparation method is with embodiment 1
In the foregoing description 1,2,3,4,5, employed sorbester p17 can also be by the Tween 80 of equivalent in its ceftiofur long-acting injection, phospholipid, and poloxamer, the K value substitutes between the PVP of K12～K15.Employed soybean oil can also be substituted by Oleum Arachidis hypogaeae semen, the Oleum Brassicae campestris of equivalent in its ceftiofur long-acting injection.Employed vitamin E can also be substituted by dibutyl phenol, the butylated hydroxyarisol of equivalent in its ceftiofur long-acting injection.
Claims (5)
1, a kind of ceftiofur long-acting injection, its injection is made up of following material:
Ceftiofur crude drug 2.5-5.0g
Sorbester p17 0.5g--3.0g
Vitamin E 0.1-0.3g
Aluminium stearate 0.2-0.5g
Chlorobutanol 0.25-0.5g
Soybean oil is to 100mL
2, a kind of preparation method of ceftiofur long-acting injection, its preparation method is:
1. to pulverize its granularity be 5 μ m to the ceftiofur crude drug;
2. adding sorbester p17 is ground in mortar evenly;
3. then with aluminium stearate, vitamin E, chlorobutanol, add in the mortar together;
4. move to after in the measuring device, add to 100mL with soybean oil at last.
3, a kind of ceftiofur long-acting injection according to claim 1 is characterized in that: described sorbester p17 can also be by the Tween 80 of equivalent, phospholipid, and poloxamer, the K value substitutes between the PVP of K12～K15.
4, a kind of ceftiofur long-acting injection according to claim 1 is characterized in that: described soybean oil can also be substituted by Oleum Arachidis hypogaeae semen, the Oleum Brassicae campestris of equivalent.
5, a kind of ceftiofur long-acting injection according to claim 1 is characterized in that: described vitamin E can also be substituted by dibutyl phenol, the butylated hydroxyarisol of equivalent.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2007101898074A CN101416968A (en) | 2007-10-22 | 2007-10-22 | Preparation method of ceftiofur long-acting injector |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2007101898074A CN101416968A (en) | 2007-10-22 | 2007-10-22 | Preparation method of ceftiofur long-acting injector |
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|---|---|
| CN101416968A true CN101416968A (en) | 2009-04-29 |
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| CNA2007101898074A Pending CN101416968A (en) | 2007-10-22 | 2007-10-22 | Preparation method of ceftiofur long-acting injector |
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Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101780088A (en) * | 2010-02-26 | 2010-07-21 | 商丘爱己爱牧动物药业有限公司 | Compound Ceftiofur Hydrochloride injecta |
| CN101978947A (en) * | 2010-10-20 | 2011-02-23 | 南京日升昌生物技术有限公司 | Long-acting Cefquinome sulfate injection and preparation method thereof |
| CN102885820A (en) * | 2011-07-20 | 2013-01-23 | 洛阳惠中兽药有限公司 | Medicinal composition containing ceftiofur bisbenzylethylenediamine |
| CN103705447A (en) * | 2013-12-24 | 2014-04-09 | 山东鲁抗立科药业有限公司 | Long-acting ceftiofur hydrochloride injection and preparation method thereof |
| CN104958313A (en) * | 2015-06-17 | 2015-10-07 | 侯强红 | Tilmicosin and ceftiofur injection and preparing equipment and process |
| CN105726461A (en) * | 2014-12-10 | 2016-07-06 | 瑞普（天津）生物药业有限公司 | Ceftiofur hydrochloride breast injectant during dry period |
| 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 |
| CN109568255A (en) * | 2018-12-19 | 2019-04-05 | 南京农业大学 | Compound long-acting injection and preparation method thereof containing Ceftiofur and Meloxicam |
-
2007
- 2007-10-22 CN CNA2007101898074A patent/CN101416968A/en active Pending
Cited By (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101780088A (en) * | 2010-02-26 | 2010-07-21 | 商丘爱己爱牧动物药业有限公司 | Compound Ceftiofur Hydrochloride injecta |
| CN101978947A (en) * | 2010-10-20 | 2011-02-23 | 南京日升昌生物技术有限公司 | Long-acting Cefquinome sulfate injection and preparation method thereof |
| CN101978947B (en) * | 2010-10-20 | 2012-04-18 | 南京日升昌生物技术有限公司 | Long-acting Cefquinome sulfate injection and preparation method thereof |
| CN102885820A (en) * | 2011-07-20 | 2013-01-23 | 洛阳惠中兽药有限公司 | Medicinal composition containing ceftiofur bisbenzylethylenediamine |
| CN103705447B (en) * | 2013-12-24 | 2015-10-28 | 山东鲁抗立科药业有限公司 | A kind of long-acting ceftiofur hydrochloride injection and preparation method thereof |
| CN103705447A (en) * | 2013-12-24 | 2014-04-09 | 山东鲁抗立科药业有限公司 | Long-acting ceftiofur hydrochloride injection and preparation method thereof |
| CN105726461A (en) * | 2014-12-10 | 2016-07-06 | 瑞普（天津）生物药业有限公司 | Ceftiofur hydrochloride breast injectant during dry period |
| CN105726461B (en) * | 2014-12-10 | 2021-02-09 | 瑞普（天津）生物药业有限公司 | Ceftiofur hydrochloride breast injection in dry period |
| CN104958313A (en) * | 2015-06-17 | 2015-10-07 | 侯强红 | Tilmicosin and ceftiofur injection and preparing equipment and process |
| CN104958313B (en) * | 2015-06-17 | 2018-02-02 | 侯强红 | A kind of Tilmicosin and Cefliofur injection and process equipment and technique |
| 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 |
| CN109568255A (en) * | 2018-12-19 | 2019-04-05 | 南京农业大学 | Compound long-acting injection and preparation method thereof containing Ceftiofur and Meloxicam |
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Open date: 20090429 |