CN109464419A - A kind of composition and its preparation method and application containing diclazuril - Google Patents
A kind of composition and its preparation method and application containing diclazuril Download PDFInfo
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- CN109464419A CN109464419A CN201811471669.3A CN201811471669A CN109464419A CN 109464419 A CN109464419 A CN 109464419A CN 201811471669 A CN201811471669 A CN 201811471669A CN 109464419 A CN109464419 A CN 109464419A
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/5015—Organic compounds, e.g. fats, sugars
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
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- Pharmacology & Pharmacy (AREA)
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- Animal Behavior & Ethology (AREA)
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- Tropical Medicine & Parasitology (AREA)
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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Abstract
The invention discloses a kind of composition and its preparation method and application containing diclazuril.The composition contains the diclazuril particle of urea cladding.When preparing the composition, urea liquid is first made, is then added thereto diclazuril, stirs and evenly mixs rear solidification mixture and obtain the diclazuril solia particle of urea cladding.Diclazuril is covered by interparticle, can be greatly improved with air exclusion, stability；And composition mobility is very good, is easy to mix, and it is easy to use；Composition is soluble easily in water, and bioavilability is high；Preparation method is simple, is easy to industrialization and industrialized production.
Description
Technical field
The invention belongs to field of veterinary medicine preparation, and in particular to a kind of composition containing diclazuril and preparation method thereof and use
On the way.
Background technique
Diclazuril belongs to blue prolixity class treating animal coccidiosis medicine, have the characteristics that wide spectrum, efficiently, low toxicity, be current dosage maximum,
Best one of the anticoccidial drug of effect.Although current diclazuril Anti-human globulin test mechanism is also not clear that it is to the soft of chicken
The Eimerias such as tender, heap-type, murder by poisoning, Bu Shi, huge, el pato worm and rabbit coccidia etc. have good effect.It is to coccidia master
Peak of action is wanted, it is different with the different genera of coccidia, such as to Eimeria tenella main function point in 2nd generation schizont coccidia
Sexual cycle, but to huge, E.brunetti schizont is invalid；To Eimeria maxima position coccidia conjunction
Sub-stage；Have efficiently to the E.brunetti microgametophyte stage；Ground gram ball benefit also has inhibition to make in laing eggs of formation egg capsule
Be mainly used for preventing and treating coccidiosis of domestic fowls with, clinic, anticoccidial drug that the control efficiency of coccidia is routinely applied better than other and
Coban plasma carrier anticoccidial drug.
Additive capacity of the diclazuril in feed is extremely low, is lmg/kg, causes directly to add diclazuril into feed
When carrying out globidiosis prevention, often can not effectively it be uniformly mixed because concentration is too low.Current existing diclazuril product is main
It is prepared after the diclazuril pre-mixing agent and addition organic solvent, solubilizer that have the different size being prepared after addition diluent
0.5% solution of diclazuril agent.The diclazuril pre-mixing agent listed is mostly powder, although preparation process is simple, transporter
Just, but its mobility and uniformity are poor, it is difficult to mix with feed, and easily be layered in use process, use is more inconvenient；At present
It is used after granule though having for it to be prepared into proper auxiliary materials, solves mobility and mixing uniformity to a certain extent,
But for the uniformity for ensuring diclazuril content in granule, diclazuril need to be carried out to ultra micro together with surfactant and mixed
It closes after crushing, then continues to mix granulation with common diluent, the high requirements on the equipment, production efficiency is lower, and is difficult to realize produce
Industry.Solution of diclazuril, which is predominantly added in animal diet followed, to carry out using being easily uniformly mixed with water with easy to use
The advantages that, but it is main liquid preparation is made in diclazuril by adding the methods of solubilizer, cosolvent and organic solvent so
Stability is poor, and the diclazuril aqueous solution validity period of preparation is only 4 hours, and biology is sharp greatly, after medication for toxicity and irritation
Expenditure is lower and has injury to body.
For these reasons, it is necessary to a kind of composition and preparation method thereof containing diclazuril is developed, to overcome
The problem of existing diclazuril pre-mixing agent makes and uses process.
Summary of the invention
In view of the problems of the existing technology, the purpose of the present invention is to provide a kind of compositions containing diclazuril.It should
Composition mobility and uniformity are good, and stability is high, easy to use.
The present invention also provides the method for preparation the composition and the purposes of the composition.
The technical solution adopted by the invention is as follows:
A kind of composition containing diclazuril, the composition contain the diclazuril particle of urea cladding.
Further, the weight ratio of the composition above-mentioned containing diclazuril, the urea and diclazuril be 10~
2000:1, preferably 50~1000:1, more preferably 100~500:1, most preferably 150~250:1.In the present invention, into one
The weight ratio for walking preferred urea and diclazuril is 2000:1,1800:1,1500:1,1200:1,80:1,50:1,20:1；More into
One step is preferably 1000:1,800:1,100:1；Most preferably 500:1,400:1,350:1,200:1.
Further, the composition above-mentioned containing diclazuril, the composition also contain diluent and/or phagostimulant and/
Or corrigent.
Further, the composition above-mentioned containing diclazuril, the diluent include but is not limited to calcium carbonate, carbonic acid
Sodium, starch, pregelatinized starch, dextrin, microcrystalline cellulose, powdered glucose, cane sugar powder, lactose, polyethylene glycol, sorbierite, sweet dew
One of alcohol, maize cob meal, corn flour, corn bran powder, soyabean protein powder, bean cake powder or more than one.
Further, the composition above-mentioned containing diclazuril, the phagostimulant include but is not limited to monosodium glutamate, saccharin, fennel
Perfume, amino acid, molasses.
Further, the composition above-mentioned containing diclazuril, the corrigent include but is not limited to all kinds of essence, sweet taste
Agent and/or odor mask.
A method of preparing the aforementioned composition containing diclazuril, comprising: urea liquid is prepared, then by diclazuril
It is added thereto, stirs and evenly mixs rear solidification mixture.
The preparation method of composition as one preferred containing diclazuril, comprising: first weigh urea by weight, heat
To being completely melt, then diclazuril is added thereto, solidification is allowed to cool after stirring and evenly mixing rapidly, is crushed to obtain the final product.
Preparation method as another preferably composition containing diclazuril, comprising: first weigh urea by weight, add
Enter into suitable quantity of water, be stirred to dissolve, be then added thereto diclazuril, stir homogeneous into suspension, be spray-dried to obtain the final product.
Further, the mass volume ratio of the preparation method of the above-mentioned composition containing diclazuril, urea and water be 0.1~
10g/mL, preferably 0.5~5g/mL, more preferably 0.8~1.2g/mL.
The present invention also provides the aforementioned compositions containing diclazuril to prepare the purposes in veterinary medicine.
Further, the veterinary medicine is birds drug.
Further, the birds are chicken.
The beneficial effects of the present invention are:
1. composition of the invention is soluble easily in water, it can promote diclazuril and quickly absorb in vivo, improve bioavilability.
2. the urea in the composition in addition to the carrier that can be used as diclazuril, can also be absorbed by animal and be used as non-protein
State nitrogen source.
3. good with diclazuril formulation flows prepared by composition, content is uniform；Diclazuril is embedded in urea,
It can be greatly improved with air exclusion, stability.
4. the composition preparation method is simple, it is easy to industrialization and industrialized production.
Specific embodiment
Summary of the invention of the invention is described further below in conjunction with specific embodiment.
In composition provided by the invention containing diclazuril, the diclazuril particle containing urea cladding.
The weight ratio of the urea and diclazuril is 20~2000:1, preferably 100~1000:1, more preferably 200
~500:1, most preferably 200~350:1.
Then composition of the invention is cooled and solidified or spraying dry by the way that diclazuril to be added in the urea after fusing
It is dry to obtain.Wherein, diclazuril is evenly dispersed into the urea of liquid, and resolidification forms particle, and mixing uniformity ratio is used
Solid filler agent and the direct mixed effect of diclazuril are good.And with side that solution of diclazuril is adsorbed on to solid-state carrier surface
Method, if patent CN106822034A is compared, diclazuril of the invention is covered by inside, can obtain with air exclusion, stability
To being greatly improved.In addition, composition of the invention has the physical property similar with solid urea, mobility is very good, with this
Composition further makes preparation or directly mixes feeding with feed, is all very easy to mix, easy to use.
Other combination with medication can also be added composition of the invention as needed and be coated on urea together with diclazuril
In.Other combination with medication include but is not limited to antimicrobial drug, the drug for treating diarrhea etc..
Suitable dilution is added in the diclazuril particle that composition of the invention can also be coated to urea as needed
The ingredients such as agent and/or corrigent, use after mixing.
It is non-limiting embodiment of the invention below, all raw materials are commercially available.
Embodiment 1~17
Prepare raw material according to the formula of each embodiment of table 1.Urea is weighed, 133~135 DEG C is heated to, it is made to be fused into liquid
Diclazuril is added in body, and cooling makes to solidify after stirring and evenly mixing rapidly, adjusts mesh size, is grinding to obtain the urine containing diclazuril
Plain solid, partial size are 10~80 mesh.
Table 1
Embodiment 18~25
Prepare raw material according to the formula of each embodiment of table 2.Urea is weighed, is added in suitable quantity of water, the ratio of urea and water
It for 0.1~10g/mL, is stirred to dissolve, diclazuril is added, stirring homogeneous is spray-dried that gram pearl containing ground is made at suspension
The urea granules or pellet of benefit adjust atomisation pressure and spray velocity, control the grain of urea granules or pellet containing diclazuril
Diameter is in 10~80 mesh.
Table 2
| Embodiment number | Urea (g) | Diclazuril (g) | Graininess |
| 18 | 100 | 1 | Pellet |
| 19 | 200 | 1 | Particle |
| 20 | 220 | 1 | Particle |
| 21 | 300 | 1 | Pellet |
| 22 | 350 | 1 | Pellet |
| 23 | 400 | 1 | Particle |
| 24 | 500 | 1 | Pellet |
| 25 | 600 | 1 | Pellet |
Embodiment 26
Use of the composition as diclazuril pre-mixing agent: the preparation of any one embodiment of Example 1~25 contains ground gram
The urea granules or appropriate pellet (being about 1g containing diclazuril) of pearl benefit, with 1000kg corn flour, corn bran powder, soybean protein
The feed of the daily feeding of the poultry such as powder, bean cake powder is uniformly mixed, feeding.
Embodiment 27
Use of the composition as feed medicated premix: the preparation of any one embodiment of Example 1~25 contains ground gram
The urea granules or appropriate pellet (being about 1g containing diclazuril) of pearl benefit are added in 1000kg feed raw material, are uniformly mixed system
For at feed, feeding.
Embodiment 28
Stability test: diclazuril composition, diclazuril raw material and commercially available diclazuril prepared by Example 7 is pre-
Each 5g of mixture, is laid in surface plate, and thickness is about 1cm, by the requirement of medicine stability test, respectively at (60 DEG C ± 2 of high temperature
DEG C), place 10 days under the conditions of high humidity (25 DEG C, RH92.5%) and illumination (4500Lx ± 500Lx), respectively at 0 day, 5 days and 10
Its sampling measures the content of wherein diclazuril, and with the content of diclazuril in 0 day sample for 100%, calculates 5 days and 10
Diclazuril evaluates its stability relative to 0 day relative amount in its sample, as a result such as the following table 3:
3 stability test of table
Results of stability shows that diclazuril composition stability prepared by the present invention is substantially better than diclazuril original
Material medicine and commercially available diclazuril pre-mixing agent, the composition of the invention can improve the stability of diclazuril well.
Claims (10)
1. a kind of composition containing diclazuril, which is characterized in that the composition contains the diclazuril of urea cladding.
2. the composition according to claim 1 containing diclazuril, which is characterized in that the weight of the urea and diclazuril
Amount is than being 10~2000:1, preferably 50~1000:1, more preferably 100~500:1, most preferably 150~250:1.
3. the composition according to claim 1 containing diclazuril, which is characterized in that the composition also contains diluent
And/or phagostimulant and/or corrigent.
4. the composition according to claim 3 containing diclazuril, which is characterized in that the diluent be selected from calcium carbonate,
Sodium carbonate, starch, pregelatinized starch, dextrin, microcrystalline cellulose, powdered glucose, cane sugar powder, lactose, polyethylene glycol, sorbierite,
One of mannitol, maize cob meal, corn flour, corn bran powder, soyabean protein powder, bean cake powder or more than one.
5. the composition according to claim 3 containing diclazuril, which is characterized in that the phagostimulant is selected from monosodium glutamate, sugar
One of essence, fennel, amino acid, molasses are a variety of.
6. the composition according to claim 3 containing diclazuril, which is characterized in that the corrigent is selected from essence, sweet tea
One of taste agent, odor mask are a variety of.
7. a kind of method for preparing the composition described in claim 1~6 any one containing diclazuril, which is characterized in that
Include: to prepare urea liquid, be then added thereto diclazuril, stirs and evenly mixs rear solidification mixture.
8. the method for composition of the preparation containing diclazuril according to claim 7 characterized by comprising first by weight
Amount weighs urea, is heated to being completely melt, is then added thereto diclazuril, solidification is allowed to cool after stirring and evenly mixing rapidly,
It crushes to obtain the final product.
9. the method for composition of the preparation containing diclazuril according to claim 7 characterized by comprising first by weight
Amount weighs urea, is added in suitable quantity of water, is stirred to dissolve, is then added thereto diclazuril, stirring homogeneous at suspension,
It is spray-dried to obtain the final product.
10. the composition described in claim 1~6 any one containing diclazuril is preparing the purposes in veterinary medicine, excellent
Selecting the veterinary medicine is birds drug, more preferably chicken drug.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201811471669.3A CN109464419A (en) | 2018-12-04 | 2018-12-04 | A kind of composition and its preparation method and application containing diclazuril |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201811471669.3A CN109464419A (en) | 2018-12-04 | 2018-12-04 | A kind of composition and its preparation method and application containing diclazuril |
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| CN109464419A true CN109464419A (en) | 2019-03-15 |
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Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001026660A1 (en) * | 1999-10-08 | 2001-04-19 | New Ace Research Company | Novel compositions and methods for prevention and treatment of protozoal disease |
| CN102274189A (en) * | 2011-07-21 | 2011-12-14 | 瑞普（天津）生物药业有限公司 | Decoquinate-containing suspension formula and preparation method thereof |
| CN104922586A (en) * | 2015-01-19 | 2015-09-23 | 山东宝来利来生物工程股份有限公司 | Preparing and application of probiotics-fermented traditional Chinese medicinal preparation for preventing and treating coccidiosis in chicken |
| CN107441200A (en) * | 2017-08-16 | 2017-12-08 | 洛阳市兽药厂 | A kind of compound diclazuril sol particle and preparation technology |
| CN107929289A (en) * | 2016-10-11 | 2018-04-20 | 朱隆娅 | A kind of diclazuril pre-mixing agent and preparation method thereof |
-
2018
- 2018-12-04 CN CN201811471669.3A patent/CN109464419A/en active Pending
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001026660A1 (en) * | 1999-10-08 | 2001-04-19 | New Ace Research Company | Novel compositions and methods for prevention and treatment of protozoal disease |
| CN102274189A (en) * | 2011-07-21 | 2011-12-14 | 瑞普（天津）生物药业有限公司 | Decoquinate-containing suspension formula and preparation method thereof |
| CN104922586A (en) * | 2015-01-19 | 2015-09-23 | 山东宝来利来生物工程股份有限公司 | Preparing and application of probiotics-fermented traditional Chinese medicinal preparation for preventing and treating coccidiosis in chicken |
| CN107929289A (en) * | 2016-10-11 | 2018-04-20 | 朱隆娅 | A kind of diclazuril pre-mixing agent and preparation method thereof |
| CN107441200A (en) * | 2017-08-16 | 2017-12-08 | 洛阳市兽药厂 | A kind of compound diclazuril sol particle and preparation technology |
Non-Patent Citations (2)
| Title |
|---|
| 张炳盛等编著: "《中药药剂学》", 28 February 2013, 中国医药科技出版社 * |
| 马素英等: "地克珠利固体分散体的制备与质量研究", 《黑龙江畜牧兽医》 * |
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Effective date of registration: 20210420 Address after: 610041 No. 302, No. 3, Building 333, North Yizhou Avenue, Chengdu High-tech Zone, Sichuan Province Applicant after: WIDT BIOTECHNOLOGY Co.,Ltd. Applicant after: CHONGQING WEIDIT PHARMACEUTICAL Co.,Ltd. Address before: 610041 No. 302, No. 3, Building 333, North Yizhou Avenue, Chengdu High-tech Zone, Sichuan Province Applicant before: WIDT BIOTECHNOLOGY Co.,Ltd. |
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