CN1813760A - Ceftiofur-containing powder injection for beast - Google Patents
Ceftiofur-containing powder injection for beast Download PDFInfo
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- CN1813760A CN1813760A CN 200510061948 CN200510061948A CN1813760A CN 1813760 A CN1813760 A CN 1813760A CN 200510061948 CN200510061948 CN 200510061948 CN 200510061948 A CN200510061948 A CN 200510061948A CN 1813760 A CN1813760 A CN 1813760A
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Abstract
The present invention relates to a veterinary powder injection preparation containing ceftiofur for preventing and curing animal microbial infective diseases. It is characterized by that it contains 20-100% of ceftiofur free acid or ceftiofur hydrochloride aseptic powder, and the rest is medicinal auxiliary material. Besides, said invention also provides its application method.
Description
Technical field
The invention belongs to the technical field of pharmaceuticals of control animal microorganism infectious disease, be specially a kind of powder needle injection for animals that contains ceftiofur.
Background technology
Ceftiofur (ceftofur) is semisynthetic third generation animal specific cephalosporin, has broad-spectrum antibacterial action, to gram-positive bacterium and gram negative bacteria, comprises that the beta-lactamase-producing strain is all effective.The at present existing very good ceftiofur sodium injection of water solublity dissolves with sterilized water during use, intramuscular injection, and once amount is administered once every 12-24 hour for 1-5mg/kg b.w., also has Ceftiofur Hydrochloride is prepared into oil suspension subcutaneous or intramuscular injection.But, in the ceftiofur building-up process, reduce 15-30% to the hydrochlorate synthesis yield from free acid, reduce 5-10% from hydrochlorate to the sodium salt synthesis yield, and need more expensive freeze drying equipment etc., prepare the production cost height of injectable powder, limit it and apply with sodium salt.
Free acid of ceftiofur or ceftiofur hydrochloride are lyophobic dust, with the polarity solvent with it dissolving, after being expelled in the body, diffusion with the polarity solvent, " taken away " the part active ingredient, this part active ingredient has played quick-acting effects, and remaining active ingredient is separated out with microcrystalline state, and this part active ingredient has played slow releasing function.Use hydrophobic vehicle, as glyceryl triacetate or plant wet goods, with the hydrophilic solvent, as dimethyl acetylamide or N-methyl-ketopyrrolidine, for cosolvent dissolves or disperses free acid of ceftiofur or ceftiofur hydrochloride, after preparation is expelled in the body, the very fast expansion of hydrophilic solvent and partially hydrophobic solvent and part active ingredient, reach site of action, this part active ingredient has played quick-acting effects, and remaining hydrophobic vehicle " is rolled in " with active ingredient, forms the hydrophobicity agglomerate, thereby limited the diffusion velocity of active ingredient, the active ingredient in the agglomerate has played slow releasing function.When containing ethyl cellulose about 1%, castor oil hydrogenated, Acetic acid, hydroxy-, bimol. cyclic ester or lactide in the system, the slow releasing function of preparation is better, by the ratio of adjusting hydrophilic solvent and hydrophobic vehicle or the content of adjusting slow-released carrier, or by adjusting dosage, all can change the slow release effect of preparation, the adjustable extent of duration of efficacy is at 0.5-10 days, the longest reaching more than 20 days.Therefore, consider, prepare powder needle injection with free acid of ceftiofur or ceftiofur hydrochloride and prepare injectable powder than with ceftiofur sodium and significantly reduced production cost, help applying from production cost.
Summary of the invention
The object of the invention is to solve the above-mentioned problems in the prior art, and design provides a kind of technical scheme that contains the powder needle injection for animals of ceftiofur, and its production cost is low, and quick-acting, had good sustained release effect.
Described a kind of powder needle injection for animals that contains ceftiofur is characterized in that containing the free acid of ceftiofur or the ceftiofur hydrochloride aseptic powder of 20-100% weight percentage, and surplus is medical auxiliary agent.
Described a kind of powder needle injection for animals that contains ceftiofur is characterized in that containing free acid of ceftiofur or the ceftiofur hydrochloride aseptic powder of weight percentage 50-98%, is preferably: 60-95%, more preferably: 70-90%.
Described a kind of powder needle injection for animals that contains ceftiofur, it is characterized in that described medical auxiliary agent is medical diluent or slow releasing carrier material, be specially polyvinylpyrrolidone, molecular weight greater than one or more the compositions in 1000 Polyethylene Glycol, Acetic acid, hydroxy-, bimol. cyclic ester, lactide, Acetic acid, hydroxy-, bimol. cyclic ester/lactide copolymer, ethyl cellulose, the castor oil hydrogenated.
Described a kind of powder needle injection for animals that contains ceftiofur, it is characterized in that adding weight percentage in the described aseptic powder is the local analgesia agent of 2-40%, be preferably 5-30%, 10-25% more preferably, described local analgesia agent is a kind of in chlorobutanol, lignocaine and salt thereof, tetracaine and salt thereof, procaine and the hydrochlorate thereof.
Described a kind of powder needle injection for animals that contains ceftiofur, it is characterized in that adding weight percentage in the described aseptic powder is the 30-50% nonsteroidal anti-inflammatory drug, be preferably 35-45%, 40-45% more preferably, described nonsteroidal anti-inflammatory drug is: diclofenac or its sodium salt, ibuprofen, naproxen, tiaprofenic acid, nabumetone, etodolac, ketoprofen, flurbiprofen, the loxoprofen, piroxicam, benzydamine, for promise happiness health, Phenylbutazone, indomethacin, meclofenamic acid or its sodium salt, dipyrone, Aspirin-arginin, a kind of in the flunixin meglumine.
Described a kind of powder needle injection for animals that contains ceftiofur is characterized in that containing the free acid of ceftiofur or the ceftiofur hydrochloride aseptic powder of 20-100% weight percentage, and surplus is medical auxiliary agent; During use, will contain free acid of ceftiofur or ceftiofur hydrochloride aseptic powder and mix, and be prepared into and contain the liquid that the active ingredient weight/volume percent is 5-30%, under the animal skins or intramuscular injection with liquid dispersion medium; The liquid dispersant that is used with this aseptic powder is 1,2-propylene glycol, formal glycerine, contain volume ratio 2-40%N-methyl-pyrrolidone solution, contain volume ratio 2-40% dimethylacetamide solution, one or more the compositions in the water for injection of the solution that contains volume ratio 0.2-35% non-ionic surface active agent, glyceryl triacetate, suffering-capric acid triglyceride, benzyl benzoate, vegetable oil, ethyl oleate, dimethicone, medical injection water, hydrochloric procaine.
Described a kind of powder needle injection for animals that contains ceftiofur, it is characterized in that adding by weight/volume in the described liquid dispersant is local analgesia agent and/or the 0-20% nonsteroidal anti-inflammatory drug of 0-3%, be preferably: 1-2.5%, 3-15%, more preferably: 2-2.5%, 5-15%;
Described local analgesia agent is a kind of in chlorobutanol, lignocaine and salt thereof, tetracaine and salt thereof, procaine and the hydrochlorate thereof;
Described nonsteroidal anti-inflammatory drug is: diclofenac or its sodium salt, ibuprofen, naproxen, tiaprofenic acid, nabumetone, etodolac, ketoprofen, flurbiprofen, loxoprofen, piroxicam, benzydamine, a kind of in promise happiness health, Phenylbutazone, indomethacin, meclofenamic acid or its sodium salt, dipyrone, Aspirin-arginin, the flunixin meglumine.
Described a kind of powder needle injection for animals that contains ceftiofur, it is characterized in that the surplus in the solution of dimethylacetamide solution, 0.2-35% non-ionic surface active agent of the described N-methyl-pyrrolidone solution that contains volume ratio 2-40%, 2-40% is 1, one or more compositionss in 2-propylene glycol or formal glycerine or glyceryl triacetate or the benzyl benzoate.
Described a kind of powder needle injection for animals that contains ceftiofur; it is characterized in that adding in the liquid dispersant polyvinylpyrrolidone, ethyl cellulose, Acetic acid, hydroxy-, bimol. cyclic ester or lactide or Acetic acid, hydroxy-, bimol. cyclic ester/lactide copolymer, one or more of castor oil hydrogenated, acetylated monoglyceride.
Described a kind of powder needle injection for animals that contains ceftiofur is characterized in that:
Aseptic powder: free acid of ceftiofur or ceftiofur hydrochloride 80%, surplus are cetomacrogol 1000 0;
Liquid dispersant: volume ratio is dimethyl acetylamide or the N-methyl-ketopyrrolidine of 15-30%, and volume ratio is 1% benzyl alcohol, and glyceryl triacetate or formal glycerine add to volume ratio 100%;
When using with liquid dispersant and aseptic powder by volume/weight ratio is 3-9: 1 ratio mixing, under the animal skins or intramuscular injection, pig, cattle, sheep per kilogram of body weight dosage are the 1-10mg ceftiofur.
Above-mentioned a kind of powder needle injection for animals that contains ceftiofur, quick-acting, had good sustained release effect, adopt free acid of ceftiofur or ceftiofur hydrochloride to prepare aseptic powder, reduced the production cost more than 20%, help it and apply than prepare injectable powder with ceftiofur sodium.This injection is applicable to the control of animal microorganism infectious disease, during use aseptic powder is mixed with liquid dispersant, is prepared into solution, molten suspension, suspension or emulsion, subcutaneous or intramuscular injection.
The proportioning that relates in the patent application document of the present invention unless otherwise indicated, is weight proportion.
The specific embodiment
Below, the present invention is elaborated by the preferred preparation scheme and the specific embodiment.Below represent weight-volume proportion, volume proportion respectively with w/v, v/v.
Preferred formulation: 1) aseptic powder: polyvinylpyrrolidone 0-10%, local analgesia agent 0-20%, free acid of ceftiofur or ceftiofur hydrochloride add to 100%.
2) liquid dispersant is a kind of in following:
One or more mixture 20-40% (v/v) in a, N-methyl-ketopyrrolidine, dimethyl acetylamide, the formal glycerine, 1, the 2-propylene glycol adds to 100% (v/v), also can add the local analgesia agent of 0.5-2% (w/v) and/or the polyvinylpyrrolidone of 2-10% (w/v).
One or more mixture 20-40% (v/v) in b, N-methyl-ketopyrrolidine, dimethyl acetylamide, the formal glycerine, glyceryl triacetate adds to 100% (v/v), also can add local analgesia agent, 0.2-3% (w/v) ethyl cellulose or 2-10% (w/v) Acetic acid, hydroxy-, bimol. cyclic ester/lactide of 0.5-2% (w/v).
C, N-methyl-ketopyrrolidine or dimethyl acetylamide 5-40% (v/v), formal glycerine adds to 100% (v/v), also can add the local analgesia agent of 0.5-2% (w/v), polyvinylpyrrolidone or the ethyl cellulose 0.5-2% (w/v) of 2-10% (w/v).
D, glyceryl triacetate or ethyl oleate or dimethyl acetylamide/benzyl benzoate/vegetable oil (1: 2-3: 4-7), also can add the castor oil hydrogenated of 2% (w/v), the acetylated monoglyceride of 30% (w/v).
When 3) using, aseptic powder is mixed with liquid dispersant, be prepared into the solution that contains active component 3-30%, molten suspension, suspension or emulsion, press 1-30mg active ingredient amount/kg b.w., suitable injected dose is 4-10mg active ingredient amount/kg b.w., subcutaneous or intramuscular injection, a drug, duration of efficacy is 0.5-10 days, is applicable to the control of animal microorganism infectious disease.
Further optimize preparation, as described in preparation 1-5:
Preparation 1:1) aseptic powder: free acid of ceftiofur or ceftiofur hydrochloride 98-100%, surplus is a cetomacrogol 1000 0.2) liquid dispersant: dimethyl acetylamide or N-methyl-ketopyrrolidine 10-30% (v/v), local analgesia agent 0.5-2% (w/v), ethyl cellulose 0-2% (w/v), glyceryl triacetate add to 100% (v/v).
Preparation 2:1) aseptic powder: free acid of ceftiofur or ceftiofur hydrochloride 100%.2) liquid dispersant: formal glycerine 30% (v/v), dimethyl acetylamide 20% (v/v), ethyl cellulose 0-2% (w/v), local analgesia agent 0.5-2% (w/v), glyceryl triacetate add to 100% (v/v).
Preparation 3:1) aseptic powder: free acid of ceftiofur or ceftiofur hydrochloride 100%.2) liquid dispersant: 1,2-propylene glycol 0-50% (v/v), local analgesia agent 0.5-2% (w/v), polyvinylpyrrolidone 3-6% (w/v), formal glycerine to 100% (v/v).
Preparation 4:1) aseptic powder: free acid of ceftiofur or ceftiofur hydrochloride 100%.2) liquid dispersant: dimethyl acetylamide 20-40% (v/v), local analgesia agent 0.5-2% (w/v), polyvinylpyrrolidone 3-6% (w/v), 1, the 2-propylene glycol adds to 100% (v/v).
Preparation 5:1) aseptic powder: free acid of ceftiofur or ceftiofur hydrochloride 100%.2) liquid dispersant: dimethyl acetylamide 10-15% (v/v), benzyl benzoate 20-30% (v/v), vegetable oil add to 100% (v/v), also can add aluminium stearate 0.5-1.5% (w/v).
Specific embodiment is as follows.
Embodiment 1: with ceftiofur hydrochloride 0.5g, be sub-packed in the 5ml cillin bottle, dimethyl acetylamide/glyceryl triacetate (3: 7) liquid dispersant is sub-packed in the 2ml peace bottle, during use liquid dispersant is injected in the 5ml cillin bottle, shake and be prepared into solution.This solution is used for animals such as pig, cattle, sheep, control bacterial infection disease, subcutaneous injection, using dosage is: cattle, sheep 2-6mg ceftiofur hydrochloride/kg b.w., every injection in 24-72 hour once, pig 3-10mg ceftiofur hydrochloride/kg b.w., every injection in 24-72 hour once.
Embodiment 2: with ceftiofur hydrochloride 1g, be sub-packed in the 5ml cillin bottle, formal glycerine/1 that 4ml is contained 2% lignocaine and 5% polyvinylpyrrolidone, 2-propylene glycol (1: 1) solution is loaded on respectively in the 5ml peace bottle, to pacify during use the bottle in solution be injected in the cillin bottle that ceftiofur hydrochloride is housed, shake and make it dissolving, be prepared into and contain 20% ceftiofur hydrochloride solution, using method is as described in the embodiment 1.
Embodiment 3: with ceftiofur hydrochloride 1g, be sub-packed in the 5ml cillin bottle, dimethyl acetylamide/glyceryl triacetate (3: the 7) solution that 4ml is contained 0.5% chlorobutanol and 1.5% ethyl cellulose (RT-20) is loaded on respectively in the 5ml peace bottle, during use, dimethyl acetylamide/glyceryl triacetate (3: 7) solution in the peace bottle is taken out, be injected in the cillin bottle that ceftiofur hydrochloride is housed, shake, make it dissolving, be prepared into and contain 20% ceftiofur hydrochloride solution.Using dosage is: cattle, sheep 3-10mg ceftiofur hydrochloride/kg b.w., every injection in 48-96 hour once; Pig 5-10mg ceftiofur hydrochloride/kg b.w., every injection in 48-96 hour once.
Embodiment 4: with ceftiofur hydrochloride 1g, be sub-packed in the 5ml cillin bottle, N-Methyl pyrrolidone/glyceryl triacetate (3: the 7) solution that 4ml is contained 0.5% chlorobutanol and 2% ethyl cellulose (RT-20) is loaded on respectively in the 5ml peace bottle, during use, N-Methyl pyrrolidone/glyceryl triacetate (3: 7) solution in the 5ml peace bottle is taken out, be injected in the cillin bottle that ceftiofur hydrochloride is housed, shake, make it dissolving, be prepared into and contain 20% ceftiofur hydrochloride solution.Using dosage is: cattle, sheep 3-20mg ceftiofur hydrochloride/kg b.w., every injection in 48-120 hour once, pig 5-20mg ceftiofur hydrochloride/kg b.w., every injection in 48-120 hour once.
Embodiment 5: with ceftiofur hydrochloride 0.5g, be sub-packed in the 5ml cillin bottle, N-Methyl pyrrolidone/glyceryl triacetate (3: 7) cosolvent that will contain 2% lignocaine is loaded on respectively in the 2ml peace bottle, during use, N-Methyl pyrrolidone/glyceryl triacetate (3: 7) cosolvent is injected in the cillin bottle, shake, be prepared into solution.Using dosage is: cattle, sheep 2-6mg ceftiofur hydrochloride/kg b.w., every injection in 24-72 hour once; Pig 3-10mg ceftiofur hydrochloride/kg b.w., every injection in 24-72 hour once.
Embodiment 6: with the free sour 0.5g of micronized ceftiofur, be sub-packed in the 5ml cillin bottle, the ethyl oleate solution 4ml that will contain 0.5% chlorobutanol is sub-packed in the 5ml peace bottle, during use, ethyl oleate solution is injected in the cillin bottle, shakes, be prepared into oil suspension.Using dosage is: cattle, sheep 2-6mg ceftiofur hydrochloride/kg b.w., every injection in 24-120 hour once; Pig 3-10mg ceftiofur hydrochloride/kg b.w., every injection in 24-120 hour once.
Embodiment 7: with the free sour 15g of ceftiofur; be sub-packed in 100ml cillin bottle or the plastic bottle; the glycerol triacetate solution 90ml that will contain 0.5% chlorobutanol, 2% castor oil hydrogenated and 35% acetylated monoglyceride is sub-packed in the 100ml container; during use; glycerol triacetate solution is injected in the cillin bottle; shake mixing.Using dosage is: cattle, sheep 2-6mg ceftiofur/kg b.w., every injection in 24-120 hour once; Pig 3-10mg ceftiofur/kg b.w., every injection in 24-120 hour once.
Embodiment 8: with the free sour 1g of micronized ceftiofur, be sub-packed in the 5ml cillin bottle, dimethyl acetylamide/benzyl benzoate/Semen Maydis oil (1: 2: 7) solution 4ml that will contain 0.5% chlorobutanol is sub-packed in the 5ml peace bottle, during use, dimethyl acetylamide/benzyl benzoate/Semen Maydis oil (1: 2: 7) solution is injected in the cillin bottle, shake mixing.Using dosage is: cattle, sheep 2-6mg ceftiofur/kg b.w., every injection in 24-120 hour once; Pig 3-10mg ceftiofur/kg b.w., every injection in 24-120 hour once.
Embodiment 9: ceftiofur hydrochloride and ketoprofen are pressed 2: 1 (w/w) mix homogeneously, packing, every bottle of 1.5g.Inject 4ml solution during use in bottle: contain polyvinylpyrrolidone 5%, formal glycerine 50%, 1,2-propylene glycol 45% makes it dissolving.Subcutaneous or intramuscular injection, pig, cattle, sheep per kilogram of body weight injection ceftiofur 2-4mg, ketoprofen 1-2mg every injection in 24 hours once, injects this agent 3-5 time a course of treatment.
Embodiment 10: the free sour micropowder of ceftiofur is sub-packed in the cillin bottle, every bottle of 1.5g, in bottle, inject the 8.5ml dispersant when using: contain ketoprofen 12%, castor oil hydrogenated 2%, all the other are dimethicone, after making it to be uniformly dispersed, subcutaneous injection, cattle, sheep per kilogram of body weight injection ceftiofur 5mg, ketoprofen 3.3mg, every injection in 72 hours once, inject this agent 1-2 time a course of treatment.
Embodiment 11; Free sour micropowder of ceftiofur or ceftiofur hydrochloride are sub-packed in the cillin bottle, every bottle of 1.5g, in bottle, inject the 8.5ml dispersant when using: contain benzyl alcohol 1%, castor oil hydrogenated 2%, Tween803%, all the other are dimethicone, after making it to be uniformly dispersed, subcutaneous injection, cattle, sheep per kilogram of body weight injection ceftiofur 7mg every injection in 96 hours once, inject this agent 1-2 time a course of treatment.
Embodiment 12: free sour micropowder of ceftiofur or ceftiofur hydrochloride are sub-packed in the cillin bottle; every bottle of 1.5g; in bottle, inject the 8.5ml dispersant when using: contain benzyl alcohol 1%, castor oil hydrogenated 2%, acetylated monoglyceride 35%, all the other are glyceryl triacetate; after making it to be uniformly dispersed; subcutaneous injection; cattle, sheep per kilogram of body weight injection ceftiofur 7mg every injection in 96 hours once, inject this agent 1-2 time a course of treatment.
Embodiment 13: ceftiofur hydrochloride/polyvinylpyrrolidone is pressed 1: 0.2 mix homogeneously, the cillin bottle packing 1.2g of every bottle of 5ml, inject the 3.8ml dispersant during use: benzyl alcohol 1% (v/v), N-methyl-ketopyrrolidine 20% (v/v), 1,2-propylene glycol 79% (v/v), shake up the back and give cattle, Corii Caprae seu Ovis injection down, dosage is 3-5mg, every injection in 48 hours once, injects this agent 2-3 time a course of treatment.
Embodiment 14: with the solid dispersion aseptic powder of ceftiofur hydrochloride/cetomacrogol 1000 0 by proportioning combination in 1: 1, particle diameter is 70-150 μ m, is sub-packed in the 25ml cillin bottle every bottle of 2.6g; Disperse with water for injection during use, pig, cattle, sheep intramuscular injection, injected dose is 3-5mg/kg b.w, injects once in 48 hours, be 2-3 a course of treatment.
Embodiment 15: with the solid dispersion aseptic powder of ceftiofur hydrochloride/Macrogol 4000 by proportioning combination in 1: 2, the particle diameter of aseptic powder is 100-200 μ m, be sub-packed in the 25ml cillin bottle, every bottle of 3g, the water for injection that adds hydrochloric procaine during use disperses, press 4-5mg/kg b.w dosage and give pig, cattle, sheep muscle or subcutaneous injection, every injection in 48 hours once, be 2-3 a course of treatment.
Embodiment 16:, with the solid dispersion aseptic powder of the free acid/polyvinylpyrrolidone of ceftiofur by the combination of 6: 4 proportionings, be sub-packed in the 25ml cillin bottle, every bottle of 2g, dissolve with the formal glycerine solution that contains benzyl alcohol during use, press 6-7mg/kg b.w dosage and give pig, cattle, sheep muscle or subcutaneous injection, every injection in 60 hours once, be 2-3 a course of treatment.
The test example, give the blood drug level analysis behind the beef injection with embodiment 2, embodiment 9, embodiment 15 preparations:
9 female cattlees of body weight 210-250 kilogram are divided into three groups.The 1st group, injection embodiment 2 preparations, injected dose is 4mg ceftiofur/kg b.w.; The 2nd group, injection embodiment 9 preparations, injected dose is 4mg ceftiofur/kg b.w.; The 3rd group, injection example 15 preparations, injected dose is 4mg ceftiofur/kg b.w.; The 4th group, inject commercially available ceftiofur sodium injection, injected dose is 4mg ceftiofur/kg b.w..Injected preceding 20 minutes and injected back 1h, 1.5h, 2h, 3h, 4h, 8h, 12h, 16h, 24h, 36h, 48h, 60h, 72h, 96h blood sampling, adopt HPLC to detect (detection is limited to 0.2 μ g/ml), the result is as shown in table 1 below:
Table 1
| Time | 1 | 1.5 | 2 | 3 | 4 | 8 | 12 | 16 | 24 | 36 | 48 | 72 | 96 |
| The 1st group the 2nd group the 3rd group the 4th group | 1.2 0.9 1.4 4.3 | 3.1 3.4 4.1 12.6 | 4.5 4.8 5.3 11.7 | 9.9 8.2 10.6 9.6 | 9.3 11.4 13.9 8.3 | 8.1 9.6 11.0 5.6 | 7.2 8.1 9.7 4.1 | 5.1 - 8.1 1.2 | 3.7 4.3 6.4 0.4 | 2.8 - 4.3 0.27 | 2.4 2.7 3.6 0.21 | 1.3 1.5 2.2 - | 0.3 0.4 1.4 - |
Annotate: the MIC of ceftiofur is 0.25-8 μ g/ml, and to the MIC difference of different bacterium, data are meansigma methods in the table.
Conclusion (of pressure testing): as seen from Table 1, the preparation described in the patent of the present invention has good slow release effect, is better than commercially available ceftiofur sodium injection.
Claims (10)
1. powder needle injection for animals that contains ceftiofur is characterized in that containing the free acid of ceftiofur or the ceftiofur hydrochloride aseptic powder of 20-100% weight percentage, and surplus is medical auxiliary agent.
2. a kind of powder needle injection for animals that contains ceftiofur as claimed in claim 1 is characterized in that containing free acid of ceftiofur or the ceftiofur hydrochloride aseptic powder of weight percentage 50-98%.
3. a kind of powder needle injection for animals that contains ceftiofur as claimed in claim 1, it is characterized in that described medical auxiliary agent is medical diluent or slow releasing carrier material, be specially polyvinylpyrrolidone, molecular weight greater than one or more the compositions in 1000 Polyethylene Glycol, Acetic acid, hydroxy-, bimol. cyclic ester, lactide, Acetic acid, hydroxy-, bimol. cyclic ester/lactide copolymer, ethyl cellulose, the castor oil hydrogenated.
4. a kind of powder needle injection for animals that contains ceftiofur as claimed in claim 1, it is characterized in that in the described aseptic powder that adding weight percentage is the local analgesia agent of 2-40%, described local analgesia agent is a kind of in chlorobutanol, lignocaine and salt thereof, tetracaine and salt thereof, procaine and the hydrochlorate thereof.
5. a kind of powder needle injection for animals that contains ceftiofur as claimed in claim 1, it is characterized in that in the described aseptic powder that adding weight percentage is the 30-50% nonsteroidal anti-inflammatory drug, described nonsteroidal anti-inflammatory drug is: diclofenac or its sodium salt, ibuprofen, naproxen, tiaprofenic acid, nabumetone, etodolac, ketoprofen, flurbiprofen, loxoprofen, piroxicam, benzydamine, a kind of in promise happiness health, Phenylbutazone, indomethacin, meclofenamic acid or its sodium salt, dipyrone, Aspirin-arginin, the flunixin meglumine.
6. a kind of powder needle injection for animals that contains ceftiofur as claimed in claim 1 is characterized in that containing the free acid of ceftiofur or the ceftiofur hydrochloride aseptic powder of 20-100% weight percentage, and surplus is medical auxiliary agent; During use, will contain free acid of ceftiofur or ceftiofur hydrochloride aseptic powder and mix, and be prepared into and contain the liquid that the active ingredient weight/volume percent is 5-30%, under the animal skins or intramuscular injection with liquid dispersion medium; The liquid dispersant that is used with this aseptic powder is 1,2-propylene glycol, formal glycerine, contain volume ratio 2-40%N-methyl-pyrrolidone solution, contain volume ratio 2-40% dimethylacetamide solution, one or more the compositions in the water for injection of the solution that contains volume ratio 0.2-35% non-ionic surface active agent, glyceryl triacetate, suffering-capric acid triglyceride, benzyl benzoate, vegetable oil, ethyl oleate, dimethicone, medical injection water, hydrochloric procaine.
7. a kind of powder needle injection for animals that contains ceftiofur as claimed in claim 6 is characterized in that adding by weight/volume in the described liquid dispersant is local analgesia agent and/or the 0-20% nonsteroidal anti-inflammatory drug of 0-3%;
Described local analgesia agent is a kind of in chlorobutanol, lignocaine and salt thereof, tetracaine and salt thereof, procaine and the hydrochlorate thereof;
Described nonsteroidal anti-inflammatory drug is: diclofenac or its sodium salt, ibuprofen, naproxen, tiaprofenic acid, nabumetone, etodolac, ketoprofen, flurbiprofen, loxoprofen, piroxicam, benzydamine, a kind of in promise happiness health, Phenylbutazone, indomethacin, meclofenamic acid or its sodium salt, dipyrone, Aspirin-arginin, the flunixin meglumine.
8. a kind of powder needle injection for animals that contains ceftiofur as claimed in claim 6, it is characterized in that the surplus in the solution of dimethylacetamide solution, 0.2-35% non-ionic surface active agent of the described N-methyl-pyrrolidone solution that contains volume ratio 2-40%, 2-40% is 1, one or more compositionss in 2-propylene glycol or formal glycerine or glyceryl triacetate or the benzyl benzoate.
9. a kind of powder needle injection for animals that contains ceftiofur as claimed in claim 6; it is characterized in that adding in the liquid dispersant polyvinylpyrrolidone, ethyl cellulose, Acetic acid, hydroxy-, bimol. cyclic ester or lactide or Acetic acid, hydroxy-, bimol. cyclic ester/lactide copolymer, one or more of castor oil hydrogenated, acetylated monoglyceride.
10. a kind of powder needle injection for animals that contains ceftiofur as claimed in claim 6 is characterized in that:
1) aseptic powder: free acid of ceftiofur or ceftiofur hydrochloride 80%, surplus are cetomacrogol 1000 0;
2) liquid dispersant: volume ratio is dimethyl acetylamide or the N-methyl-ketopyrrolidine of 15-30%, and volume ratio is 1% benzyl alcohol, and glyceryl triacetate or formal glycerine add to volume ratio 100%;
When 3) using with liquid dispersant and aseptic powder by volume/weight ratio is 3-9: 1 ratio mixing, under the animal skins or intramuscular injection, pig, cattle, sheep per kilogram of body weight dosage are the 1-10mg ceftiofur.
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Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN101773477A (en) * | 2010-03-18 | 2010-07-14 | 青岛康地恩药业有限公司 | Ceftiofur lung targeting microsphere used for beasts and birds and preparation method thereof |
| CN101829063A (en) * | 2010-03-18 | 2010-09-15 | 青岛康地恩药业有限公司 | Lung targeting microsphere of veterinary ceftiofur hydrochloride and preparation method |
| CN102341125A (en) * | 2008-11-19 | 2012-02-01 | 梅里亚有限公司 | Formulations comprising ceftiofur and ketoprofen or ceftiofur and benzyl alcohol |
| CN101874773B (en) * | 2009-04-28 | 2012-05-30 | 上海市动物疫病预防控制中心 | Long-acting ceftiofur hydrochloride injection and preparation method thereof |
| CN103721263A (en) * | 2014-01-08 | 2014-04-16 | 王玉万 | Oil injection containing antibacterial agents/polyethylene glycol drug-loading particles |
| CN104352501A (en) * | 2014-11-10 | 2015-02-18 | 重庆泰通动物药业有限公司 | Compound ceftiofur sodium injection |
| CN104586777A (en) * | 2014-12-22 | 2015-05-06 | 广东省天宝生物制药有限公司 | Ceftiofur hydrochloride powder injection as well as preparation method and application thereof |
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| CN1569000A (en) * | 2003-07-16 | 2005-01-26 | 王玉万 | Quick-acting and long-acting aliporina contained injection |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN102341125A (en) * | 2008-11-19 | 2012-02-01 | 梅里亚有限公司 | Formulations comprising ceftiofur and ketoprofen or ceftiofur and benzyl alcohol |
| CN101874773B (en) * | 2009-04-28 | 2012-05-30 | 上海市动物疫病预防控制中心 | Long-acting ceftiofur hydrochloride injection and preparation method thereof |
| CN101773477A (en) * | 2010-03-18 | 2010-07-14 | 青岛康地恩药业有限公司 | Ceftiofur lung targeting microsphere used for beasts and birds and preparation method thereof |
| CN101829063A (en) * | 2010-03-18 | 2010-09-15 | 青岛康地恩药业有限公司 | Lung targeting microsphere of veterinary ceftiofur hydrochloride and preparation method |
| CN101773477B (en) * | 2010-03-18 | 2012-06-13 | 青岛康地恩药业有限公司 | Ceftiofur lung targeting microsphere used for beasts and birds and preparation method thereof |
| CN103721263A (en) * | 2014-01-08 | 2014-04-16 | 王玉万 | Oil injection containing antibacterial agents/polyethylene glycol drug-loading particles |
| CN104352501A (en) * | 2014-11-10 | 2015-02-18 | 重庆泰通动物药业有限公司 | Compound ceftiofur sodium injection |
| CN104586777A (en) * | 2014-12-22 | 2015-05-06 | 广东省天宝生物制药有限公司 | Ceftiofur hydrochloride powder injection as well as preparation method and application thereof |
| CN104586777B (en) * | 2014-12-22 | 2017-07-21 | 广东省天宝生物制药有限公司 | Ceftiofur Hydrochloride powder-injection and preparation method and application |
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