CN108057020A - A kind of pyridaben antiparasitic preparation for animals and preparation method thereof - Google Patents
A kind of pyridaben antiparasitic preparation for animals and preparation method thereof Download PDFInfo
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Abstract
The invention discloses a kind of pyridaben antiparasitic preparations for animals and preparation method thereof, belong to field of veterinary.The pyridaben antiparasitic preparation for animals includes pyridaben 1~30%, double solvents 5~60%, emulsifier 5~30%, infiltration synergist 1~25%, and surplus is diluent；The double solvents is made of glycerol formal, propylene glycol, dimethyl acetamide and purified water.Pharmaceutical grade and food grade solvent used in pyridaben antiparasitic preparation for animals provided by the present invention are the substance of hypotoxicity, solves the solubility problem of pyridaben by compounding perfection, the defects of solvent toxicity used in existing pyridaben preparation can be overcome larger, animal health may be endangered.Product of the present invention is directly can to pour into a mould or embrocate in the pyridaben preparation on livestock and poultry fur, its active ingredient is made to achieve the effect that kill vermin by fur diffusion, is had no toxic side effect and drug residues, safe to use, economical environment-protective.
Description
Technical field
The invention belongs to field of veterinary, and in particular to a kind of pyridaben antiparasitic preparation for animals and preparation method thereof.
Background technology
Pyridaben chemical name is the chloro- 2H- pyridazin-3-ones of 2- tertiary butyls -5- (4- tertiary butyls benzylthio) -4-, is colourless
Crystal belongs to pyridazinone Insecticidal and acaricidal agent, without interior absorption.Pyridaben is less toxic contact acaricide, to tetranychid, Panonychus citri,
Unguiculus mite closes the food vegetalitas evil mite such as goitre mite and is respectively provided with apparent control effect, and to ovum, deutonymph, effective into mite, into mite
The mobile phase it is also effective.According to Wang Jianguo et al.《Metrifonate, pyridaben observe the effect of pig's sarcoptidosis》(Wang Jianguo, Zhang Xianhui
The effect of metrifonate, pyridaben is to pig's sarcoptidosis observation [J] Henan animal and veterinary:General news column, 2000 (11):25-25.) report
Pyridaben is heterocyclic compound insecticides, cures mainly red spider, and itch mite and red spider are insect of the same race, therefore pyridaben is to itch mite
Worm also shows good killing effect.Experiments have shown that pyridaben has apparent effect for the scabies mite prevention of poultry, there is height
The advantages that effect is less toxic, cheap, easy to use.
Since pyridaben itself is not soluble in water, the dissolubility in each solvent is poor, "《Newly organized pesticide commodity handbook》
In the pyridaben physics and chemistry that (Zhang Minheng is edited, Chemical Industry Press, 2006.6) includes, and pyridaben dissolubility (20 DEG C, g/
L)：Ketone 0.46, benzene 110, dimethylbenzene 390, ethyl alcohol 57, thiacyclohexane 320, n-octyl alcohol 63, normal hexane 10.“《Chinese pharmaceutic adjuvant》”
It is mentioned in (Luo Mingsheng, Gao Tianhui, Beijing, Chemical Industry Press, 2006)：Solvent is by toxicity magnitude classification one kind, two classes, three
Class, four class solvents.A kind of toxicity is big, such as benzene, carbon tetrachloride etc., generally forbids to use, and two classes use for limitation, three classes hypotoxicity
Solvent, four classes are without enough toxicity data solvents.
Traditional pyridaben product goes to make usually using substantial amounts of organic solvent.As contained in pyridaben missible oil product
The organic solvents such as a large amount of dimethylbenzene, toluene.This kind of organic solvent smell and toxicity are all very big.At present, rattled away due to commercially available
Related product such as emulsion of mite spirit etc. is not the veterinary drug developed for animal, has been used in preparation substantial amounts of organic molten
Agent, these organic solvent toxicities are deeper, larger to the side effect of poultry, may cause the inadaptable of animal, can additionally pollute
Environment and water source." a kind of active ingredient is the aqueous emulsion of pyridaben to the Chinese patent that number of patent application is 200810101134.7
And preparation method thereof " and number of patent application be a kind of 200810101922.6 Chinese patents " preparation side of pyridaben micro-emulsion
Method ", they are primarily directed to crops and plant uses, solvent (dimethylbenzene, toluene, dimethylformamide etc.) and emulsification
Agent (33#, 34# etc.) is mostly the big preparation of toxicity, is not suitable for animal use.In addition, with regard to pyridaben dissolubility wherein and
Speech, only dimethylbenzene or thiacyclohexane dissolubility is larger, and suitable for the solvent of pyridaben, and dimethylbenzene and thiacyclohexane are all toxicity
Greatly, the big solvent of smell is not suitable for livestock and poultry use.
Therefore, a kind of pyridaben antiparasitic preparation for animals efficiently, less toxic is developed to be of great significance.
The content of the invention
It is an object of the invention to overcome the deficiencies of the prior art and provide a kind of pyridabens for animals efficiently, less toxic, environmentally friendly
Antiparasitic preparation and preparation method thereof.
The technical solution used in the present invention is：
A kind of pyridaben antiparasitic preparation for animals includes the component of following masses percentage：Pyridaben 1~30% is answered
Bonding solvent 5~60%, emulsifier 5~30%, infiltration synergist 1~25%, surplus is diluent；The double solvents is by sweet
Oily formal, propylene glycol, dimethyl acetamide and purified water composition.
Preferably, the double solvents includes the component of following masses percentage：Glycerol formal 1-45%, propylene glycol 2-
30%th, dimethyl acetamide 5-75%, surplus are purified water.
Preferably, the double solvents includes the component of following masses percentage：Glycerol formal 15-30%, propylene glycol
2-10%, dimethyl acetamide 45-65%, surplus are purified water.
Preferably, the double solvents includes the component of following masses percentage：Glycerol formal 25%, propylene glycol 5%,
Dimethyl acetamide 55%, surplus purified water.
The present invention is compounded to obtain double solvents using glycerol formal, propylene glycol, dimethyl acetamide, purified water,
It can be very good to solve the problems, such as that pyridaben dissolubility is bad.Solubility of the pyridaben in double solvents is about 332g/L.This
Outside, it is nonirritant since each component in double solvents has small toxicity, the features such as the stink of no discomfort, (dissolved with dimethylbenzene
Spend for 390g/L), thiacyclohexane (solubility is about 320g/L) compare, be more suitable for solvent.
Preferably, it is (8- that infiltration synergist, which is long chain glyceride or medium chain triglycerides and water-based azone according to mass ratio,
12)：(4-7) is mixed to get.
Preferably, medium chain triglycerides are MCT Oil.
Long chain glyceride and medium chain triglycerides viscosity are low, and solidification point is low, can make the moisturizing factor and antifreezing agent of transdermal solution.
Long chain glyceride and medium chain triglycerides liquid condition are very intact, have good antioxygenic property, prevent oxidation of drug, improve
The quality of transdermal solution and storage period.While long chain glyceride and medium chain triglycerides are absorbed by the skin, drug is also corresponding
Ground absorbs therewith.
The present invention is combined using long chain glyceride and medium chain triglycerides with high-effective penetrating promoter azone, increases skin keratin
The flowing of layer lipoid, so as to increase penetrability of the drug to skin, gets through skin barrier, plays the role of playing drug effect.
Preferably, emulsifier is Tween 80, polysorbate60, polysorbas20, sorbester p18, sorbester p17, sorbester p37, hydrogenation polyoxyethylene
One kind or any number of combination in castor oil, Emulsifier EL-60.
Preferably, diluent is purified water.
A kind of preparation method of pyridaben antiparasitic preparation for animals, according to each component is weighed described in any of the above-described, first
Double solvents is heated to 40-50 DEG C, adds in pyridaben, stirring and dissolving；Emulsifier is added, 1800-2200r/ minutes at a high speed
It is mixed into O/W states；It adds infiltration synergist to stir evenly, adds diluent to full dose, pyridaben for animals is prepared kills and post
Infested preparation.
The beneficial effects of the invention are as follows：
The present invention provides a kind of pyridaben antiparasitic preparation for animals, which is colourless to yellow clarified solution body, color and luster
Uniformly, property is stablized.
Pharmaceutical grade and food grade solvent used in pyridaben antiparasitic preparation for animals provided by the present invention are hypotoxicity
Substance, solve the solubility problem of pyridaben by compounding perfection, can overcome molten used in existing pyridaben preparation
Agent toxicity is larger, the defects of may endangering animal health.
The characteristics of present invention easily multiplies for livestock and poultry fur and carries parasite, providing one kind directly can pour into a mould or embrocate
In the pyridaben preparation on livestock and poultry fur, its active ingredient is made to achieve the effect that kill vermin by fur diffusion, this
Product have no toxic side effect and drug residues.
The homogeneous stability system that the present invention is formed using water as matrix, by dissolving the processes such as active compound, microemulsified, surface are lived
Property agent content it is high, emulsified particles is small, and drug effect is high using effect.The present invention reduces cost by matrix of water, mitigates pollution pressure.
Present invention pyridaben preparation for animals is efficient, it is less toxic, safe to use, energy saving, do not pollute substantially.
Preparation method provided by the present invention is simple to operation, is easy to implement industrialization.
Specific embodiment
In order to further deepen explanation of the invention and realize present invention convenient for masses, below in conjunction with specific reality
Applying example and comparative example, the present invention will be further described.
Embodiment 1
10% pyridaben antiparasitic preparation includes the component of following masses percentage：
Wherein double solvents is by glycerol formal 25%, propylene glycol 5%, dimethyl acetamide 55%, surplus purified water group
Into by mass percentage.
Permeating synergist is：MCT Oil and water-based azone are according to mass ratio 10：5 are mixed to get.
Preparation method：Accurate to weigh pyridaben original powder, pyridaben is dissolved as liquid by the double solvents for adding in warm (45 DEG C)
After body shape object, add Tween 80 and be sufficiently stirred emulsification, then mixed at high speed (2000r/ minutes) adds in infiltration into O/W states
Synergist stirs evenly, and last surplus adds in purified water, and stirs evenly to get 10% pyridaben antiparasitic preparation.
By detection, pyridaben is about 332g/L in double solvents solubility in the present embodiment.
Embodiment 2
15% pyridaben microemulsion formulation, including following masses percent composition：
Wherein double solvents is by glycerol formal 25%, propylene glycol 5%, dimethyl acetamide 55%, surplus purified water group
Into by mass percentage.
Permeating synergist is：MCT Oil and water-based azone are according to mass ratio 10：5 are mixed to get.
Preparation method：Accurate to weigh pyridaben original powder, pyridaben is dissolved as liquid by the double solvents for adding in warm (45 DEG C)
After body shape object, add Tween 80 and be sufficiently stirred emulsification, then mixed at high speed (2000r/ minutes) adds in infiltration into O/W states
Synergist stirs evenly, and last surplus adds in purified water, and stirs evenly to get 15% pyridaben antiparasitic preparation.
By detection, pyridaben is about 333g/L in double solvents solubility in the present embodiment.
Embodiment 3
10% pyridaben antiparasitic preparation, including following masses percent composition：
Wherein double solvents is by glycerol formal 25%, propylene glycol 5%, dimethyl acetamide 55%, surplus purified water group
Into；By mass percentage.
Permeating synergist is：MCT Oil and water-based azone are according to mass ratio 10：5 are mixed to get.
Preparation method：Accurate to weigh pyridaben original powder, pyridaben is dissolved as liquid by the double solvents for adding in warm (45 DEG C)
After body shape object, add Tween 80 and be sufficiently stirred emulsification, then mixed at high speed (2000r/ minutes) adds in infiltration into O/W states
Synergist stirs evenly, and last surplus adds in purified water, and stirs evenly to get 10% pyridaben antiparasitic preparation.
By detection, pyridaben is about 331g/L in double solvents solubility in the present embodiment.
Embodiment 4
15% pyridaben microemulsion formulation, including following masses percent composition：
Wherein double solvents is by glycerol formal 25%, propylene glycol 5%, dimethyl acetamide 55%, surplus purified water group
Into；By mass percentage.
Permeating synergist is：MCT Oil and water-based azone are according to mass ratio 10：5 are mixed to get.
Preparation method：Accurate to weigh pyridaben original powder, pyridaben is dissolved as liquid by the double solvents for adding in warm (45 DEG C)
After body shape object, add Tween 80 and be sufficiently stirred emulsification, then mixed at high speed (2000r/ minutes) adds in infiltration into O/W states
Synergist stirs evenly, and last surplus adds in purified water, and stirs evenly to get 15% pyridaben microemulsion formulation.
By detection, pyridaben is about 332g/L in double solvents solubility in the present embodiment.
Related assays are carried out to the product of embodiment.
Detection project and requirement are as follows：
(1) transparency temperature scope：-5℃-65℃.
(2) through when stablize：It is stored under room temperature 60 days and stablizes qualification.
(3) low-temperature stabilization：- 5 DEG C storage 14 days it is not stratified, not muddy, do not crystallize.
(4) heat storage stability：It is stored 2 weeks under conditions of 55 ± 2 DEG C, detects the content of active ingredient, calculate content point
Solution rate, no more than 5%；Observation occurs without oil reservoir and precipitation.
(5) stability of emulsion (20 times)：200 times are diluted with standard hard water, 1h is stood in 30 DEG C of waters bath with thermostatic control and is taken out, is seen
Examine lotion separation situation or on without under oil slick without precipitation.
By measuring, the product indices of embodiment 1-4 are qualified.
In order to absolutely prove beneficial effects of the present invention, beneficial effects of the present invention are done further below by way of test example
Explanation.
Test example one：Pyridaben antiparasitic preparation stability tests (accelerated test)
1st, test objective：Prove that pyridaben antiparasitic preparation nature provided by the present invention is stablized, content is maintained at mark
It is more than quasi- value.
2nd, trial drug：10% pyridaben antiparasitic preparation, prepares, lot number 16102101 according to embodiment 1.15%
Pyridaben antiparasitic preparation, prepares according to embodiment 2, lot number 16102102.More than sample is by the positive allusion quotation biology in Foshan City
Technology Co., Ltd. provides.
3rd, test method：Reference《Republic of China Veterinary Pharmacopoeia》Accelerated test in one stability of version in 2015 is surveyed
The method of determining is detected.By commercially available back, in 40 DEG C ± 2 DEG C of temperature, placed 6 months under conditions of relative temperature 70% ± 5%, it is real
When monitor humiture, 1st month during experiment, 2 months, 3 months, 6 the end of month it is separately sampled once, detection wherein pyridaben
Content.
4th, result of the test is shown in Table 1.
1 pyridaben stability test result of table
1 result of table the result shows that, a kind of pyridaben antiparasitic preparation for animals of the invention pass through accelerated test, content
Change less, property stabilization.
Test example two, the experiment of pyridaben antiparasitic preparation mite killing safe effect
1st, test objective：It is low toxicity, the mite-killing preparation of safety to prove pyridaben antiparasitic preparation provided by the present invention.
2nd, trial drug：10% pyridaben antiparasitic preparation, prepares, lot number 16102101 according to embodiment 1.15%
Pyridaben antiparasitic preparation, prepares according to embodiment 2, lot number 16102102.More than sample is by the positive allusion quotation biology in Foshan City
Technology Co., Ltd. provides.
3rd, test method：30 chickens are selected, are randomly divided into 3 groups, every group 10.Respectively 10% pyridaben group, 15%
Pyridaben group and blank control group.10% and 15% pyridaben antiparasitic preparation is taken to embrocate under each group chicken wing respectively
On square soft textive, observe whether its mental condition and skin have red and swollen appearance.And it is compared with not applying any acaricidal blank.
4th, result of the test is shown in Table 2.
2 pyridaben miticidal effect of table is tested
Table 2 the result shows that, a kind of pyridaben antiparasitic preparation for animals of the invention is directly embrocated on chicken, spirit it is good
Good, chicken is a kind of safe and efficient mite-killing preparation without red swelling of the skin, damage and inflammation phenomenon.
Test example three, the experiment of pyridaben antiparasitic preparation miticidal effect
1st, test objective：It is efficient mite-killing preparation to prove pyridaben antiparasitic preparation provided by the present invention.
2nd, trial drug：
10% pyridaben antiparasitic preparation, prepares, lot number 16102101 according to embodiment 1.
Control group 1：Preparation method is same as Example 1, does not add infiltration synergist in formula.
Control group 2：Purified water blank group compares.
More than sample is provided by Zhengdian Biological Tech. Co., Ltd., Foshan City.
3rd, test method：The affected pig of farm natural infection itch mite 30 is randomly divided into 3 groups, every group 10.Take each group sample
Product are according to 1：300 dosage spray is shone in the pig of corresponding group, and 3 days are once, are used in conjunction 2 times, observe its mental condition and in 7 days,
Its except mite effect is visually observed after 14 days.And it is compared with purified water blank group.
4th, result of the test is shown in Table 3.
3 pyridaben miticidal effect of table is tested
Table 3 the result shows that, a kind of apparent, the of the invention pyridaben antiparasitic for animals of addition infiltration synergist synergistic effect
Preparation has display effect to pig's sarcoptidosis, is a kind of less toxic, efficient mite-killing preparation.
Comparative example 1
It is formulated with embodiment 1, the difference is that, double solvents is pure by glycerol formal 40%, propylene glycol 30%, surplus
Change water composition.
By detection, pyridaben is about 25g/L in double solvents solubility in this comparative example.Due to the solubility of pyridaben
It is bad, obtain that product is unstable in room temperature storage and when low-temp storage, and easily muddy, crystallization is undesirable.
Comparative example 2
It is formulated with embodiment 1, the difference is that, double solvents is by propylene glycol 20%, dimethyl acetamide 55%, surplus
Purified water forms.
By detection, pyridaben is about 88g/L in double solvents solubility in this comparative example.Due to the solubility of pyridaben
It is bad, obtain that product is unstable in room temperature storage and when low-temp storage, and easily muddy, crystallization is undesirable.
Comparative example 3
Formula with embodiment 1, the difference is that, double solvents by glycerol formal 25%, dimethyl acetamide 55%,
Surplus purified water forms.
By detection, pyridaben is about 106g/L in double solvents solubility in this comparative example.Due to the dissolving of pyridaben
It spends bad, obtains that product is unstable in room temperature storage and when low-temp storage, and easily muddy, crystallization is undesirable.
Comparative example 4
It is formulated with embodiment 1, the difference is that, double solvents is by glycerol formal 20%, propylene glycol 35%, dimethyl
Acetamide 20%, surplus purified water composition.
The usage amount of propylene glycol is excessive in this comparative example, overruns, and the dosage of corresponding dimethyl acetamide is reduced,
Obtained double solvents is not good enough for the solute effect of pyridaben.By detection, pyridaben is dissolved in double solvents in this comparative example
Degree is about 78g/L.Since the solubility of pyridaben is bad, product unstable, appearance in room temperature storage and low-temp storage is obtained
Easily muddy, crystallization, it is undesirable.
Above-described embodiment is the preferable embodiment of the present invention, but embodiments of the present invention and from above-described embodiment
Limitation, other any Spirit Essences without departing from the present invention with made under principle change, modification, replacement, combine, simplification,
Equivalent substitute mode is should be, is included within protection scope of the present invention.
Claims (7)
1. a kind of pyridaben antiparasitic preparation for animals, which is characterized in that include the component of following masses percentage：Pyridaben 1
~30%, double solvents 5~60%, emulsifier 5~30%, infiltration synergist 1~25%, surplus is diluent；It is described compound
Solvent is made of glycerol formal, propylene glycol, dimethyl acetamide and purified water.
2. pyridaben antiparasitic preparation for animals according to claim 1, which is characterized in that under the double solvents includes
The component of row mass percent：Glycerol formal 1-45%, propylene glycol 2-30%, dimethyl acetamide 5-75%, surplus are pure
Change water.
3. pyridaben antiparasitic preparation for animals according to claim 2, which is characterized in that under the double solvents includes
The component of row mass percent：Glycerol formal 15-30%, propylene glycol 2-10%, dimethyl acetamide 45-65%, surplus are
Purified water.
4. pyridaben antiparasitic preparation for animals according to claim 1, it is characterised in that：It is sweet for long-chain to permeate synergist
Grease or medium chain triglycerides and water-based azone are (8-12) according to mass ratio：(4-7) is mixed to get.
5. pyridaben antiparasitic preparation for animals according to claim 1, it is characterised in that：Emulsifier is Tween 80, spits
Temperature 60, polysorbas20, sorbester p18, sorbester p17, sorbester p37, hydrogenation Emulsifier EL-60, one kind in Emulsifier EL-60 or
Any number of combination.
6. pyridaben antiparasitic preparation for animals according to claim 1, it is characterised in that：Diluent is purified water.
7. a kind of preparation method of pyridaben antiparasitic preparation for animals, it is characterised in that：According to any one of claim 1-6 institutes
It states and weighs each component, double solvents is first heated to 40-50 DEG C, add in pyridaben, stirring and dissolving；Add emulsifier, 1800-
2200r/ minutes mixed at high speed are into O/W states；It adds infiltration synergist to stir evenly, diluent is added to be prepared to full dose
Pyridaben antiparasitic preparation for animals.
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| Application Number | Title | Priority Date | Filing Date |
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| CN201711129833.8A Pending CN108057020A (en) | 2017-11-15 | 2017-11-15 | A kind of pyridaben antiparasitic preparation for animals and preparation method thereof |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114306231A (en) * | 2021-12-29 | 2022-04-12 | 天津市中升挑战生物科技有限公司 | Flurara pesticide and preparation method and application thereof |
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| CN101530074A (en) * | 2008-03-14 | 2009-09-16 | 北京绿色农华植保科技有限责任公司 | Preparation method of pyridaben micro-emulsion |
| CN102603669A (en) * | 2012-04-05 | 2012-07-25 | 南开大学 | Derivatives of alpha-methoxyl imino-5-methyl-1,2,3-thiadiazole-4- carboxylic acid methyl ester and preparation methods and uses thereof |
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| CN101530074A (en) * | 2008-03-14 | 2009-09-16 | 北京绿色农华植保科技有限责任公司 | Preparation method of pyridaben micro-emulsion |
| CN102603669A (en) * | 2012-04-05 | 2012-07-25 | 南开大学 | Derivatives of alpha-methoxyl imino-5-methyl-1,2,3-thiadiazole-4- carboxylic acid methyl ester and preparation methods and uses thereof |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114306231A (en) * | 2021-12-29 | 2022-04-12 | 天津市中升挑战生物科技有限公司 | Flurara pesticide and preparation method and application thereof |
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Application publication date: 20180522 |