CN101467986A - Long acting florfenicol oleo-injection and preparation method thereof - Google Patents

Long acting florfenicol oleo-injection and preparation method thereof Download PDF

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Publication number
CN101467986A
CN101467986A CNA200710300061XA CN200710300061A CN101467986A CN 101467986 A CN101467986 A CN 101467986A CN A200710300061X A CNA200710300061X A CN A200710300061XA CN 200710300061 A CN200710300061 A CN 200710300061A CN 101467986 A CN101467986 A CN 101467986A
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CN
China
Prior art keywords
injection
florfenicol
oleo
long acting
oil
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Pending
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CNA200710300061XA
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Chinese (zh)
Inventor
吴红云
李建正
喻伟
陈伟斌
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Zhengzhou Houyi Pharmaceutical Co Ltd
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Zhengzhou Houyi Pharmaceutical Co Ltd
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Priority to CNA200710300061XA priority Critical patent/CN101467986A/en
Publication of CN101467986A publication Critical patent/CN101467986A/en
Pending legal-status Critical Current

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Abstract

The invention relates to long-acting oleo-injection of florfenicol and a preparation method thereof. The injection is made from the following raw and auxiliary materials in terms of weight percentage: 1-35% of florfenicol, 0.1-5% of suspending agent, 0.1-4% of emulsifying agent, 0.005-1% of antioxidant and oil for injection which is added till the total percentage is 100%. Advantages of the inventive long-acting oleo-injection of florfenicol are as follows: the oil solution, suspensions after being injected into muscles will locally form a storage house; then dissolved or suspended medicinal molecules are distributed into aqueous gaps in vivo from the oil solution, and gradually enter blood circulation to exert curative effect thereof. The inventive long-acting oleo-injection has advantages of few administration times and durable and effective medicament concentration. Curative effect of the injection is not affected even dosage thereof is reduced.

Description

Long acting florfenicol oleo-injection and preparation method thereof
Technical field
The present invention relates to a kind of long acting florfenicol oleo-injection that is used for the treatment of poultry sensitivity bacterial disease, simultaneously, also relate to the preparation method of this long acting florfenicol oleo-injection, belong to the veterinary and use medicine.
Background technology
Go into effect with the market economic system Economy Growth since Reform to the mid-90 from early 1980s, the period of a high speed development has been experienced in China's animal husbandry, and the harm of livestock and poultry pestilence also becomes increasingly conspicuous, and has seriously influenced the sound development of animal husbandry.New disease is on the increase, and harm is also strengthening, and has caused serious economy loss not only for breed enterprise, has caused threat also for the physical and mental health of consumer.Two more than ten years of past, China's animal drug industry has been advanced the people all-round developing period, and veterinary drug research has obtained tremendous development, but compares with some developed countries, still exists very big gap.The new veterinary drug kind of listing and quality can't adapt to the needs of present China livestock and poultry breeding industry development.
Florfenicol is a chloromycetin veterinary special broad-spectrum antibiotic of new generation, have the characteristics such as wide, safe and efficient that distribute in the has a broad antifungal spectrum, good absorbing, body, remarkable for the poultry bacterial disease therapeutic effect due to the sensitive organism, gram positive bacteria and negative bacterium are all had effect, are the drug of first choices of the various infection that cause of Bacillus typhi, Salmonella paratyphi, Salmonella.This medicine is at present more than 20 country's listings, because chloromycetin has the untoward reaction of serious induced aplastic anemia, and to forbid being used for food animal, therefore, and on animal diseases control, food animal especially, florfenicol has broad application prospects.In recent years because a large amount of uses of medicine, the continuous appearance of drug-resistance of bacteria problem and residue of veterinary drug problem, therefore the developing focus of antibacterials for animals and preparation thereof must meet the requirement of animal specific and food safety.The exploitation of veterinary drug novel form will develop towards scientific and practicality direction, and the long-acting sustained-release dosage form that can reduce dosage and raising curative effect will obtain development and application energetically.
Summary of the invention
The object of the present invention is to provide that a kind of good effect, short treating period, medication number of times are few, with high content of technology, the treatment fowl bacterial disease of instant effect and the broad-spectrum long-acting florfenicol oleo-injection of viral secondary infection.
To achieve these goals, technical scheme of the present invention has adopted a kind of long acting florfenicol oleo-injection, is made by the supplementary material of following weight proportioning: florfenicol 1-35% (W/V), suspending agent 0.1%~5% (W/V), emulsifying agent 0.1~4% (W/V), antioxidant 0.005~1% (W/V), oil for injection add to 100% (W/V).
But described oil for injection is any one or its combination in any in soybean oil, Oleum sesami, Oleum Ricini, Oleum Cocois and the Semen Maydis oil of injection.
Described suspending agent is any or its combination in any in aluminium stearate, tragakanta, gelatin and the various cellulose.
Described emulsifying agent is any or its combination in any in lecithin, Polysorbate, fatty glyceride and the polyoxyethylene fatty acid ester.
Described antioxidant is the tert-butyl group to any or its combination in any in hydroxyl Fructus Foeniculi, dibutyl phenol, PG and the tocopherol.
Simultaneously, technical scheme of the present invention has also adopted a kind of preparation method of long acting florfenicol oleo-injection, may further comprise the steps: (1) takes by weighing florfenicol 1-35% (W/V), suspending agent 0.1%~5% (W/V), emulsifying agent 0.1~4% (W/V), antioxidant 0.005~1% (W/V), oil for injection by weight and adds to 100% (W/V); (2) earlier above-mentioned supplementary material is done filtration and sterilization treatment respectively; (3) with suspending agent, antioxidant and emulsifying agent add in the oil for injection, and mixing, add florfenicol again and pass through colloid mill or high pressure homogenization machine repeated treatments, and the qualified after-filtration of particle diameter, fill are promptly.
The present invention is to be principal agent with the florfenicol, and the employing oil for injection is a solvent, and adds the long-acting mixed suspension preparation of Gong the beasts drug administration by injection that adjuvants such as suitable antioxidant, suspending agent and emulsifying agent are prepared from.Florfenicol in the preparation of the present invention is a chloromycetin veterinary special broad-spectrum antibiotic of new generation, have the characteristics such as wide, safe and efficient that distribute in the has a broad antifungal spectrum, good absorbing, body, remarkable for the fowl bacterial disease therapeuticing effect due to the sensitive organism, gram positive bacteria and negative bacterium all there is effect, be the drug of first choice of the various infection that cause of Bacillus typhi, Salmonella paratyphi, Salmonella, be widely used clinically at veterinary drug.
The outstanding advantage of long acting florfenicol oleo-injection of the present invention is: can form " bank " in the part after the intramuscular injection of oily solution suspensoid, the dissolving or the drug molecule of suspendible distribute from oily solution subsequently and enter aqueous gap in the body, progress into blood circulation again, bring into play its curative effect.Long-acting oily injection agent of the present invention has that the medication number of times is few, the sustainable effective advantage of drug level, reduces accumulated dose and does not influence its curative effect, so consider it is a kind of dosage form of practicality from the pharmacoeconomics angle.Preparation of the present invention has stronger antibacterial activity to multiple gram positive bacteria, mycoplasma and gram negative bacteria etc.Actinobacillus pleuropneumoniae, streptococcus, haemophilus, salmonella typhi, pasteurella haemolytica, pasteurella multocida, shigella dysenteriae, klebsiella, escherichia coli etc. are extremely sensitive to this product.The pharmacokinetics intramuscular injection absorbs rapidly, and the blood drug level height is widely distributed, long half time, and the valid density length of holding time, cattle 28 hours, pig mainly through liver, kidney metabolism, are discharged with feces more than 32 hours on a small quantity.
Injection of the present invention can be used for the treatment of the infection due to pig, the chicken sensitive organism, as actinobacillus suis pleuropneumonia, Bacillus pasteurii disease, typhoid fever, paratyphoid fever, colibacillosis etc. and respiratory system seven big obstinate diseases: breeding and respiratory disorder, porcine contagious pleuropneumonia, the disease of breathing, haemophilus parasuis disease, pig lung plague, popular pneumonia, atrophic rhinitis.Can also be used for the treatment of other diseases as enteritis, HUANGBAI(sic) dysentery, typhoid fever, streptococcicosis, serious symptom mixed infection.
Intramuscular injection: once measure every 1kg body weight, pig, chicken 20mg.Every 48 hours once, logotype is 2 times.
The specific embodiment
Embodiment 1
The long acting florfenicol oleo-injection of present embodiment, (W/V) that makes by the supplementary material of following weight proportioning: florfenicol 10%, aluminium stearate 0.5%, lecithin 0.1%, the tert-butyl group to hydroxyl Fructus Foeniculi 0.005%, all the other are soybean oil.
Preparation method is: (1) take by weighing by weight florfenicol 10%, florfenicol 10%, aluminium stearate 0.5%, lecithin 0.1%, the tert-butyl group to hydroxyl Fructus Foeniculi 0.005%, all the other are soybean oil; (2) earlier above-mentioned supplementary material is done filtration and sterilization treatment respectively; (3) suspending agent aluminium stearate and emulsifier lecithin are added in the soybean oil, and mixing, adding florfenicol again and pass through colloid mill or high pressure homogenization machine repeated treatments, the qualified after-filtration of particle diameter, fill are promptly.
Embodiment 2
The long acting florfenicol oleo-injection of present embodiment, (W/V) that is made by the supplementary material of following weight proportioning: florfenicol 15%, tragakanta 1%, Polysorbate 1.5%, dibutyl phenol 0.01%, all the other are Oleum sesami.
Preparation method is with embodiment 1.
Embodiment 3
The long acting florfenicol oleo-injection of present embodiment, (W/V) that is made by the supplementary material of following weight proportioning: florfenicol 20%, gelatin 2%, fatty glyceride 2.5%, PG 0.5%, all the other are Oleum Ricini.
Preparation method is with embodiment 1.
Embodiment 4
The long acting florfenicol oleo-injection of present embodiment, (W/V) that is made by the supplementary material of following weight proportioning: florfenicol 30%, cellulose 5%, polyoxyethylene fat 1.5%, PG 1%, all the other are Oleum Cocois.
Preparation method is with embodiment 1.
Embodiment 5
The long acting florfenicol oleo-injection of present embodiment, (W/V) that is made by the supplementary material of following weight proportioning: florfenicol 25%, gelatin 4%, fat acid esters 4%, tocopherol 0.8%, all the other are Semen Maydis oil.
Preparation method is with embodiment 1.
It should be noted last that: above embodiment is only in order to explanation, and unrestricted technical scheme of the present invention, although the present invention is had been described in detail with reference to the foregoing description, those of ordinary skill in the art is to be understood that: still can make amendment or be equal to replacement the present invention, and not breaking away from any modification or partial replacement of the spirit and scope of the present invention, it all should be encompassed in the middle of the claim scope of the present invention.

Claims (10)

1, a kind of long acting florfenicol oleo-injection is characterized in that: made by the supplementary material of following weight proportion: florfenicol 1-35%, suspending agent 0.1%-5%, emulsifying agent 0.1-4%, antioxidant 0.005-1%, oil for injection add to 100%.
2, long acting florfenicol oleo-injection according to claim 1 is characterized in that: but described oil for injection is any one or its combination in any in soybean oil, Oleum sesami, Oleum Ricini, Oleum Cocois and the Semen Maydis oil of injection.
3, long acting florfenicol oleo-injection according to claim 1 is characterized in that: described suspending agent is any or its combination in any in aluminium stearate, tragakanta, gelatin and the various cellulose.
4, long acting florfenicol oleo-injection according to claim 1 is characterized in that: described emulsifying agent is any or its combination in any in lecithin, Polysorbate, fatty glyceride and the polyoxyethylene fatty acid ester.
5, long acting florfenicol oleo-injection according to claim 1 is characterized in that: described antioxidant is the tert-butyl group to any or its combination in any in hydroxyl Fructus Foeniculi, dibutyl phenol, PG and the tocopherol.
6, a kind of preparation method as arbitrary described long acting florfenicol oleo-injection in the claim 1-5 is characterized in that: may further comprise the steps: (1) takes by weighing florfenicol 1-35% (W/V), suspending agent 0.1%~5% (W/V), emulsifying agent 0.1~4% (W/V), antioxidant 0.005~1% (W/V), oil for injection by weight and adds to 100% (W/V); (2) earlier above-mentioned supplementary material is done filtration and sterilization treatment respectively; (3) with suspending agent, antioxidant and emulsifying agent add in the oil for injection, and mixing, add florfenicol again and pass through colloid mill or high pressure homogenization machine repeated treatments, and the qualified after-filtration of particle diameter, fill are promptly.
7, long acting florfenicol oleo-injection according to claim 6 is characterized in that: but described oil for injection is any one or its combination in any in soybean oil, Oleum sesami, Oleum Ricini, Oleum Cocois and the Semen Maydis oil of injection.
8, long acting florfenicol oleo-injection according to claim 6 is characterized in that: described suspending agent is any or its combination in any in aluminium stearate, tragakanta, gelatin and the various cellulose.
9, long acting florfenicol oleo-injection according to claim 6 is characterized in that: described emulsifying agent is any or its combination in any in lecithin, Polysorbate, fatty glyceride and the polyoxyethylene fatty acid ester.
10, long acting florfenicol oleo-injection according to claim 6 is characterized in that: described antioxidant is the tert-butyl group to any or its combination in any in hydroxyl Fructus Foeniculi, dibutyl phenol, PG and the tocopherol.
CNA200710300061XA 2007-12-25 2007-12-25 Long acting florfenicol oleo-injection and preparation method thereof Pending CN101467986A (en)

Priority Applications (1)

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Application Number Priority Date Filing Date Title
CNA200710300061XA CN101467986A (en) 2007-12-25 2007-12-25 Long acting florfenicol oleo-injection and preparation method thereof

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CN101467986A true CN101467986A (en) 2009-07-01

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103520211A (en) * 2013-10-23 2014-01-22 挑战(天津)动物药业有限公司 Compound florfenicol injection as well as preparation method and application thereof
CN113827561A (en) * 2021-07-21 2021-12-24 杭州艾贝德生命科技研究院有限公司 Sustained-release florfenicol suspension injection and preparation process thereof

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103520211A (en) * 2013-10-23 2014-01-22 挑战(天津)动物药业有限公司 Compound florfenicol injection as well as preparation method and application thereof
CN103520211B (en) * 2013-10-23 2015-10-07 天津市中升挑战生物科技有限公司 A kind of compound florfenicol injection and preparation method thereof and application
CN113827561A (en) * 2021-07-21 2021-12-24 杭州艾贝德生命科技研究院有限公司 Sustained-release florfenicol suspension injection and preparation process thereof

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Open date: 20090701