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CN102406597A - Diclazuril solution and preparation method thereof - Google Patents

Diclazuril solution and preparation method thereof Download PDF

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Publication number
CN102406597A
CN102406597A CN2011102978617A CN201110297861A CN102406597A CN 102406597 A CN102406597 A CN 102406597A CN 2011102978617 A CN2011102978617 A CN 2011102978617A CN 201110297861 A CN201110297861 A CN 201110297861A CN 102406597 A CN102406597 A CN 102406597A
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CN
China
Prior art keywords
diclazuril
solution
povidone
usp
polyethylene glycol
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CN2011102978617A
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Chinese (zh)
Inventor
高建辉
廖洪
宋莉
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SHANGHAI HENGFENGQIANG ANIMAL PHARMACEUTICAL CO Ltd
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SHANGHAI HENGFENGQIANG ANIMAL PHARMACEUTICAL CO Ltd
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Priority to CN2011102978617A priority Critical patent/CN102406597A/en
Publication of CN102406597A publication Critical patent/CN102406597A/en
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Abstract

The invention discloses a diclazuril solution which is prepared from the following raw materials in percentage by weight: diclazuril 2%, high-molecular polymer 4%, and polyethylene glycol to 100 ml. The invention also discloses a preparation method of the diclazuril solution. Tests show that the diclazuril solution has the characteristics of stable property, convenient administration and the like.

Description

Solution of diclazuril and preparation method thereof
Technical field
The present invention relates to solution of diclazuril and preparation method thereof.
Background technology
Diclazuril belongs to triazine benzene acetonitrile chemical compound, for novel, efficient, low toxicity anticoccidial drug, is widely used in chicken coccidiosis.The diclazuril anticoccidial mechanism of action is also not clear.Coccidiosis is mainly acted on the peak phase, different with the different genera of coccidiosis, as to the main application point of Eimeria tenella the 2nd generation the schizont coccidiosis sexual cycle arranged.But to huge, Bu Shi Eimeria schizont is invalid.To the zygote stage of Eimeria maxima application point coccidiosis; The Bu Shi Eimeria microgametophyte stage is had efficiently.Ground gram ball profit also has inhibitory action to forming the spore egg capsule.
Diclazuril is tender to chicken, heap type, murder by poisoning, Bu Shi, Eimeria maxima effect are splendid, and decapacitation is controlled outside the generation and death of caecum coccidiosis effectively after the medication, even the disease chicken coccidial oocyst is all disappeared, and real is the ideal worm medicine of killing.Diclazuril also has efficiently gentle Eimeria.Show that according to clinical trial diclazuril is superior to other conventional anticoccidial drug and monensin plasma carrier anticoccidial drugs of using to the prevention effect of coccidiosis.
Diclazuril 1mg/kg feedstuff concentration can be controlled el pato's parasitosis effectively, its effect even surpass polyether antibiotics.The sharp 1mg/kg feedstuff of ground gram ball concentration can be prevented and treated turkey gland Eimeria, turkey Eimeria, peafowl Eimeria effectively and disperseed Eimeria to infect.Also have evidence, to fluoropurine (Arprinocid), clopidol, halofuginone hydrobromide, oxygen benzene guanidine, the drug-fast Eimeria tenella of monensin, it is still effective to use diclazuril.
Diclazuril 1mg/kg spice is fed rabbit, and is efficient to tame rabbit liver coccidiosis and intestinal coccidiosis tool.
There is following defective in existing diclazuril preparation:
(1) because these article are prone to cause the drug resistance of coccidiosis, even cross resistance (Toltrazuril), therefore, logotype must not be above 6 months.Also should not use similar medicine such as Toltrazuril when rotating medication.
(2) these article are of short duration action time, and drug withdrawal is after one day, and effect disappears basically, and therefore, the necessary continuous use of broiler is in case outburst once again.
(3) because extremely low with concentration, spice allows that the change value is 0.8~1.2mg/kg, otherwise affects the treatment.Therefore spice must fully be mixed thoroughly.
(4) the drinking-water liquid of solution of diclazuril, the stable phase of China regulation is merely 4h, therefore, must show with joining at present, otherwise affect the treatment.Cause commercial production and storing and clinical use inconvenient like this.
Summary of the invention
One object of the present invention is to provide solution of diclazuril, with overcome existing solution of diclazuril must be at present with defective such as join, affect the treatment easily at present.
The technical problem that will solve required for the present invention, can realize through following technical scheme:
Solution of diclazuril of the present invention, form by following raw materials by weight percent:
Diclazuril 2%
High molecular polymer 4%
Polyethylene Glycol adds to 100ml.
Said high molecular polymer is one or more in 30 POVIDONE K 30 BP/USP 30, the 30 POVIDONE K 30 BP/USP 17.
Said high molecular polymer is a 30 POVIDONE K 30 BP/USP 30.
Preferably, described solution of diclazuril, by weight percentage, wherein said diclazuril account for gross weight 2%, 30 POVIDONE K 30 BP/USP 30 (PVPk30) is 4%, Polyethylene Glycol is for adding to 100ml.
Another object of the present invention is to provide the method for preparing of said solution of diclazuril, and its preparation technology is: be dissolved in PVPk30 (30 POVIDONE K 30 BP/USP 30) in the Polyethylene Glycol, after the stirring and dissolving; Add diclazuril; Be heated to 60 degree, stir and to make dissolving, both described solution of diclazuril.
The application of said solution of diclazuril in the medicine of the disease that preparation control turkey gland Eimeria, turkey Eimeria, peafowl Eimeria and dispersion Eimeria infect.
The invention has the beneficial effects as follows:
Solution of diclazuril of the present invention is dissolved in diclazuril in the macromolecular material, makes macromolecular material wrap diclazuril, and after the administration, diclazuril slowly discharges from macromolecular material again, reaches long lasting effect; Has stable in properties, characteristics such as convenient drug administration through test solution of diclazuril of the present invention.
The specific embodiment
In order to make technological means of the present invention, creation characteristic, to reach purpose and effect and be easy to understand and understand,, further set forth the present invention below in conjunction with specific embodiment.
Embodiment 1
Solution of diclazuril, by weight percentage, form by following raw materials by weight percent:
Diclazuril 2%
30 POVIDONE K 30 BP/USP 30 4%
Polyethylene Glycol adds to 100ml.
Be dissolved in PVPk30 (30 POVIDONE K 30 BP/USP 30) in the Polyethylene Glycol, after the stirring and dissolving, add diclazuril, be heated to 60 degree, stir and make dissolving, both.
Through being dissolved in diclazuril in the macromolecular material, make macromolecular material wrap diclazuril, after the administration, diclazuril slowly discharges from macromolecular material again, reaches long lasting effect.
Embodiment 2
The described solution of diclazuril of present embodiment, by weight percentage, said diclazuril account for gross weight 2%, 30 POVIDONE K 30 BP/USP 17 is 4%, Polyethylene Glycol adds to 100ml.Method for preparing is with embodiment 1.
Embodiment 3
The application of the solution of diclazuril of embodiment 1
Mix and raise: every 1000kg feedstuff 1g fowl;
Solution of diclazuril: mix the every 1L drinking-water of drink fowl 0.5~1mg (effective ingredient).
Embodiment 4
The assay experiment and the result thereof of the solution of diclazuril that embodiment 1-2 prepares.
Accelerated test
These article of getting; Simulation listing packing; Place in the exsiccator that fills saturated nacl aqueous solution (RH 75%45%); Be positioned over temperature again and be in 40 ℃ ± 2 ℃ the calorstat, respectively at 1,2,3, the sampling in June, investigate appearance luster, content, clarity, related substance, particulate matter, the aseptic and bacterial endotoxin of sample.
The result sees table 1.
Table 1. accelerated test result (40 ± 2 ℃ of temperature, relative humidity 75% ± 5%)
Figure BDA0000095947770000041
Figure BDA0000095947770000051
Figure BDA0000095947770000052
Figure BDA0000095947770000061
Result of the test
Show according to table 1, solution of diclazuril accelerated test 6 months, each item index does not have significant change.
Brief summary
The result shows through accelerated test, and specification is the 100mL:2g solution of diclazuril, is packaged as simulation listing packing, and solution of diclazuril is 40 ± 2 ℃ in temperature, relative humidity be 75% ± 5% condition place 6 months stable.
Long term test
Test material
Sample title: solution of diclazuril
Sample specification: 100mL:2g
Sample lot number: be respectively 20070302,20070304,20070306
Test method
To supply test agent is 25 ± 2 ℃ in temperature; Relative humidity is 60% ± 5% condition held 12 months; In the time of 3,6,9,12 months, take a sample respectively; According to " quality standard " down pertinent regulations measure character, content and pH value, record result's (result sees the following form 2), and with batch 0 month record relatively.
Table 2. long-term test results (25 ± 2 ℃ of temperature, relative humidity 60% ± 5%)
Figure BDA0000095947770000071
Figure BDA0000095947770000081
Figure BDA0000095947770000082
Figure BDA0000095947770000091
Result of the test
Show according to table 3, solution of diclazuril long term test 36 months, each item index does not have significant change.
Brief summary
Show through long-term test results: specification is the 100mL:2g solution of diclazuril, is packaged as simulation listing packing, and solution of diclazuril is 25 ± 2 ℃ in temperature, and relative humidity is 60% ± 5% condition held 36 months, and is stable.
Through test, the solution of diclazuril of embodiment 1-3 has water breakthrough white and characteristics such as separates out, and diclazuril is dissolved in the macromolecular material; Make macromolecular material wrap diclazuril; After the administration, diclazuril slowly discharges from macromolecular material again, reaches long lasting effect.
The raw material that relates among the embodiment 1-5 is commercially available product.
More than show and described ultimate principle of the present invention, principal character and advantage of the present invention.The technical staff of the industry should understand; The present invention is not restricted to the described embodiments; That describes in the foregoing description and the description just explains principle of the present invention; The present invention also has various changes and modifications under the prerequisite that does not break away from spirit and scope of the invention, and these variations and improvement all fall in the scope of the invention that requires protection.The present invention requires protection domain to be defined by appending claims and equivalent thereof.

Claims (5)

1. solution of diclazuril is characterized in that, is made up of following raw materials by weight percent:
Diclazuril 2%
High molecular polymer 4%
Polyethylene Glycol adds to 100ml.
2. solution of diclazuril according to claim 1 is characterized in that, said high molecular polymer is one or more in 30 POVIDONE K 30 BP/USP 30, the 30 POVIDONE K 30 BP/USP 17.
3. solution of diclazuril according to claim 2 is characterized in that, said high molecular polymer is a 30 POVIDONE K 30 BP/USP 30.
4. solution of diclazuril according to claim 2 is characterized in that, by weight percentage, said diclazuril account for gross weight 2%, 30 POVIDONE K 30 BP/USP 30 is 4%, Polyethylene Glycol is for adding to 100ml.
5. preparation is characterized in that according to the method for the described solution of diclazuril of claim 1-4, is dissolved in 30 POVIDONE K 30 BP/USP 30 in the Polyethylene Glycol, after the stirring and dissolving, adds diclazuril, is heated to 60 degree, stir and make dissolving, both described solution of diclazuril.
CN2011102978617A 2011-09-30 2011-09-30 Diclazuril solution and preparation method thereof Pending CN102406597A (en)

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Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102670616A (en) * 2012-05-25 2012-09-19 鼎正动物药业(天津)有限公司 Novel diclazuril preparation and preparation method thereof
CN105726598A (en) * 2016-02-29 2016-07-06 王腊俊 Compound solution for preventing and treating chicken coccidiosis and preparation method thereof
CN106474055A (en) * 2015-09-01 2017-03-08 瑞普(天津)生物药业有限公司 A kind of novel composing prescription of solution of diclazuril and preparation method thereof
CN107929289A (en) * 2016-10-11 2018-04-20 朱隆娅 A kind of diclazuril pre-mixing agent and preparation method thereof
CN108186561A (en) * 2018-03-12 2018-06-22 石家庄市金元康牧药业有限公司 A kind of solution of diclazuril and preparation method thereof
CN115611880A (en) * 2022-11-09 2023-01-17 浙江国邦药业有限公司 A kind of diclazuril related substance and its preparation method

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1490009A (en) * 2002-10-17 2004-04-21 王玉万 Sustained release injection containing medicine against coccindian

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1490009A (en) * 2002-10-17 2004-04-21 王玉万 Sustained release injection containing medicine against coccindian

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102670616A (en) * 2012-05-25 2012-09-19 鼎正动物药业(天津)有限公司 Novel diclazuril preparation and preparation method thereof
CN102670616B (en) * 2012-05-25 2013-07-03 鼎正动物药业(天津)有限公司 Novel diclazuril preparation and preparation method thereof
CN106474055A (en) * 2015-09-01 2017-03-08 瑞普(天津)生物药业有限公司 A kind of novel composing prescription of solution of diclazuril and preparation method thereof
CN106474055B (en) * 2015-09-01 2020-01-07 瑞普(天津)生物药业有限公司 New formula of diclazuril solution and preparation method thereof
CN105726598A (en) * 2016-02-29 2016-07-06 王腊俊 Compound solution for preventing and treating chicken coccidiosis and preparation method thereof
CN107929289A (en) * 2016-10-11 2018-04-20 朱隆娅 A kind of diclazuril pre-mixing agent and preparation method thereof
CN108186561A (en) * 2018-03-12 2018-06-22 石家庄市金元康牧药业有限公司 A kind of solution of diclazuril and preparation method thereof
CN115611880A (en) * 2022-11-09 2023-01-17 浙江国邦药业有限公司 A kind of diclazuril related substance and its preparation method

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Application publication date: 20120411