Emulsion in water containing abamectin and fosthiazate and preparation method thereof

By optimizing the combination of emulsifier and dispersant, the stability of avermectin and thiazolytein water emulsions is improved, and the stability problems caused by environmental changes during transportation are solved, thereby achieving higher emulsification dispersion and stability of active ingredients.

CN119498287AActive Publication Date: 2025-02-25QINGDAO RAINBOW CHEM CO LTD
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Patent Information

Application Number
CN202311069801.9
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2023-08-23
Publication Date
2025-02-25
Estimated Expiration
2043-08-23

AI Technical Summary

Technical Problem

The existing aqueous emulsions of avermectin and thiazolyte are susceptible to environmental changes during sea transportation, and have problems such as stratification, demulsification, and water dissipation. The active ingredients are easy to degrade, affecting the efficacy of the drug.

Method used

By screening and combining emulsifiers and dispersants, the auxiliary system is optimized, the stability and emulsification dispersion of water emulsifiers are improved, and the risk of decomposition of active ingredients is reduced.

Benefits of technology

It significantly improves the stability of the water emulsion, avoids the influence of environmental changes during transportation, reduces the risks of stratification, demulsification, water evolution and crystallization, and extends the stability of the active ingredients.

✦ Generated by Eureka AI based on patent content.

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Abstract

The invention provides an aqueous emulsion containing abamectin and fosthiazate, which comprises the following components in percentage by mass: 10-50% of active pharmaceutical ingredients, 2-10% of an emulsifier, 0.5-8% of a dispersant, 10-40% of a solvent, 1-6% of a cosolvent, 3-8% of an antifreezing agent, 0.1-2% of a stabilizer and the balance of deionized water, the active pharmaceutical ingredients comprise abamectin and fosthiazate. By optimizing the mass ratio, the pesticide effect of the product is improved, and meanwhile, the pesticide application frequency is reduced. According to the invention, by preferably selecting the auxiliary agent, the stability of the product is improved, the influence of environmental change in the transportation process is effectively solved, and the risks of layering, demulsification, water separation and crystallization are avoided. And the problem of decomposition of effective components is solved, the use in different countries and regions is met, and large-scale popularization and application are facilitated.
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Description

Technical Field

[0001] The invention relates to the technical field of pesticide preparations, in particular to an aqueous emulsion containing avermectin and thiabendazole and a preparation method thereof. Background Art

[0002] Abamectin has stomach poison and contact killing effects on mites and insects, but cannot kill eggs. Its mechanism of action is to interfere with neurophysiological activities and stimulate the release of γ-aminobutyric acid, which has an inhibitory effect on the nerve conduction of arthropods. It is mainly used to control resistant pests such as diamondback moth, leaf miner, and red spider.

[0003] Fosthiazate is an organophosphorus nematicide that inhibits the synthesis of acetylcholinesterase in root-knot nematodes. It has strong contact activity and is highly active against some pests that have developed resistance to traditional insecticides. It can prevent and control nematodes, aphids, etc.

[0004] The combination of avermectin and thiazole has been proven to have a significant synergistic effect and can reduce the dosage of active ingredients, which can not only reduce costs, but more importantly, reduce harm to plants. However, the quality of related products is currently unstable, and they are easily affected by environmental changes during maritime transportation, and are prone to stratification, demulsification, water precipitation, etc., and there is a risk of crystallization; at the same time, the flash point is low, and the active ingredients are easily degraded, which seriously affects the efficacy and is not conducive to the use and promotion of the product. Summary of the invention

[0005] In view of this, the technical problem to be solved by the present invention is to provide an aqueous emulsion containing avermectin and thiazolyl and a preparation method thereof, which has high stability.

[0006] The present invention provides an aqueous emulsion containing avermectin and thiazolyl, which comprises, by mass percentage:

[0007] Active pharmaceutical ingredient 10%-50%, emulsifier 2%-10%, dispersant 0.5%-8%, solvent 10%-40%, cosolvent 1%-6%, antifreeze 3%-8%, stabilizer 0.1%-2%, deionized water to make up 100%;

[0008] The active ingredients of the medicine include avermectin and thiazolyl.

[0009] The mass content of the active pharmaceutical ingredient is preferably 10% to 30%.

[0010] The present invention uses avermectin and thiathiocarbazate as active pharmaceutical ingredients, and the mass ratio of the avermectin to thiathiocarbazate is preferably 1:(1-50), more preferably 1:(5-20). In some specific embodiments of the present invention, the mass ratio of the avermectin to thiathiocarbazate includes but is not limited to 1:5, 1:9, 1:10, 1:15, and 1:19.

[0011] Avermectin: Appearance is light yellow to white crystalline powder, odorless. Melting point 155~157℃, vapor pressure 2×10 - 7 Pa, relative density 1.16 (21°C). Solubility at 21°C: toluene 350g / L, acetone 100g / L, isopropanol 70g / L, chloroform 25g / L, ethanol 20g / L, methanol 19.5g / L, cyclohexane 6g / L, kerosene 0.5g / L, water 10μg / L. LogP value is 4.4±0.3. Stable under normal conditions, will not hydrolyze at pH 5-9.

[0012] Thiazole phosphine: The pure product is a light yellow liquid. Melting point <25°C, relative density 1.26 (20°C), boiling point 198°C, vapor pressure 5.6×10 -4 Pa (25°C), solubility in water is 9.85 g / L (0.87%), and the distribution coefficient is 1.75.

[0013] From the perspective of both properties, avermectin has requirements for the type and amount of solvents, and the combination of emulsifiers and dispersants determines the spontaneous dispersibility of the preparation in water and the stability of the emulsion. Avermectin has the risk of degradation. The present invention performs a large amount of screening work on the auxiliary agent system, and finally obtains a system with the best matching degree between the components, especially the screening and combination of emulsifiers and dispersants, which improves the stability of the dosage form, has the advantages of good emulsification and dispersibility, and is resistant to transportation, and effectively solves the problems of sample precipitation, poor dispersion, unstable emulsion, easy decomposition, etc.

[0014] The aqueous emulsion provided by the present invention contains an emulsifier, and the mass content of the emulsifier is preferably 2%-10%, more preferably 2%-8%. In some specific embodiments of the present invention, the mass content of the emulsifier is specifically 2%, 4%, 6% or 8%.

[0015] The present invention preferably uses a composite emulsifier, which includes a first emulsifier and a second emulsifier.

[0016] Preferably, the first emulsifier is selected from one or more of octylphenol polyoxyethylene polyoxypropylene ether, cyclohexene polyoxyethylene polyoxypropylene, benzyl biphenol polyoxyethylene polyoxypropylene, benzylphenol polyoxyethylene polyoxypropylene, phenethylphenol polyoxyethylene ether polyoxypropylene ether, isopropylphenyl phenethylphenol polyoxyethylene ether, styrene phenol polyoxyethylene ether, octylphenol polyoxyethylene ether, secondary octylphenol polyoxyethylene ether, nonylphenol polyoxyethylene ether, bis-nonylphenol polyoxyethylene ether, benzylphenol polyoxyethylene ether, fatty lauryl alcohol polyoxyethylene ether, oleyl alcohol polyoxyethylene ether, isotridecanol polyoxyethylene ether, fatty acid polyoxyethylene ether, fatty amine polyoxyethylene ether, and methyl alcohol polyoxyethylene ether; more preferably, one or more of methyl alcohol polyoxyethylene ether and nonylphenol polyoxyethylene ether; further preferably, methyl alcohol polyoxyethylene ether.

[0017] Preferably, the second emulsifier is selected from one or more of glycerol esters, polyglycerol esters, sugar esters, EO-PO block polyethers, calcium dodecylbenzene sulfonate, distyrylphenol polyformaldehyde condensates, triglycerol monostearate, aromatic phenol polyoxyethylene ether formaldehyde condensates, stearates, polyoxyethylene oleates, castor oil polyoxyethylene ether phosphates, sorbitan ester ethers, polyglycerol fatty acid esters, succinate sulfonates, α-sulfo fatty acid ester salts, and polyarylphenol ether sulfates; more preferably, one or more of EO-PO block polyethers and calcium dodecylbenzene sulfonate; and further preferably, EO-PO block polyethers.

[0018] The aqueous emulsion contains a dispersant, and the mass content of the dispersant is preferably 0.5%-8%, more preferably 1%-2%. In some specific embodiments of the present invention, the mass content of the dispersant is 1%, 1.5% or 2%.

[0019] Preferably, the dispersant is selected from one or more of high molecular polymer, polystyrene acrylic acid sodium salt, maleic rosin block polyether sulfonate ammonium salt, diisopropylnaphthalene sulfonate sodium salt, benzylnaphthalene sulfonic acid formaldehyde condensate sodium salt, styrene acrylic acid copolymer sodium salt, tristyrylphenol polyoxyethylene ether phosphate triethanolamine salt, maleic rosin block polyether sulfonate ammonium salt, styrene maleic anhydride copolymer sodium salt, maleic anhydride acrylic acid copolymer, fatty alcohol polyoxyethylene polyoxypropylene ether, styrene maleic anhydride copolymer sodium salt, alkanolamide polyoxyethylene ether phosphate, sodium lignin sulfonate, calcium lignin sulfonate, sodium diethyl succinate sulfate, and acrylic acid maleic styrene sodium sulfonate; more preferably, one or more of tristyrylphenol polyoxyethylene ether phosphate triethanolamine salt and benzylnaphthalene sulfonic acid formaldehyde condensate sodium salt; further preferably, tristyrylphenol polyoxyethylene ether phosphate triethanolamine salt or benzylnaphthalene sulfonic acid formaldehyde condensate sodium salt.

[0020] The mass ratio of the first emulsifier, the second emulsifier and the dispersant is preferably 1-4:1-4:1-4, more preferably 1-2:1-2:1-2, and further preferably 1.5:1.5:1.

[0021] In some specific embodiments of the present invention, the first emulsifier, the second emulsifier and the dispersant are methyl alcohol polyoxyethylene ether, EO-PO block polyether and tristyrylphenol polyoxyethylene ether phosphate triethanolamine salt, and their mass contents are 3%, 3% and 2%, respectively.

[0022] In some specific embodiments of the present invention, the first emulsifier, the second emulsifier and the dispersant are methyl alcohol polyoxyethylene ether, EO-PO block polyether and benzylnaphthalenesulfonic acid formaldehyde condensate sodium salt, and their mass contents are 3%, 3% and 2%, respectively.

[0023] In some specific embodiments of the present invention, the first emulsifier, the second emulsifier and the dispersant are methyl alcohol polyoxyethylene ether, calcium dodecylbenzenesulfonate and sodium salt of benzylnaphthalenesulfonic acid formaldehyde condensate, respectively, and their mass contents are 3%, 3% and 1%, respectively.

[0024] In some specific embodiments of the present invention, the first emulsifier, the second emulsifier and the dispersant are nonylphenol polyoxyethylene ether, calcium dodecylbenzenesulfonate and sodium salt of benzylnaphthalenesulfonic acid formaldehyde condensate, respectively, and their mass contents are 3%, 3% and 1%, respectively.

[0025] In some specific embodiments of the present invention, the first emulsifier, the second emulsifier and the dispersant are nonylphenol polyoxyethylene ether, calcium dodecylbenzene sulfonate and sodium salt of benzylnaphthalenesulfonic acid formaldehyde condensate, respectively, and their mass contents are 1%, 1% and 1%, respectively.

[0026] In some specific embodiments of the present invention, the first emulsifier, the second emulsifier and the dispersant are nonylphenol polyoxyethylene ether, calcium dodecylbenzenesulfonate and sodium salt of benzylnaphthalenesulfonic acid formaldehyde condensate, respectively, and their mass contents are 1%, 1% and 1.5%, respectively.

[0027] In some specific embodiments of the present invention, the first emulsifier, the second emulsifier and the dispersant are respectively nonylphenol polyoxyethylene ether, calcium dodecylbenzenesulfonate and sodium salt of benzylnaphthalenesulfonic acid formaldehyde condensate, and their mass contents are respectively 4%, 4% and 1%.

[0028] The present invention has been proved through experimental research that the stability of the avermectin·thiazole phosphine aqueous emulsion can be greatly affected by screening the first emulsifier, the second emulsifier and the dispersant, including spontaneous dispersibility in water, high and low temperature storage stability and crystallization. The present invention performs a large amount of screening work on the auxiliary agent system, and finally obtains a system with the best matching degree between the above components, especially the combination of emulsifier and dispersant, which solves the problem of obvious decomposition of avermectin in the product, greatly improves the stability of the product, has the advantage of good emulsification and dispersibility, effectively solves the influence of environmental changes during transportation, avoids the risks of stratification, demulsification, water separation and crystallization, and also solves the problem of decomposition of effective ingredients.

[0029] The specific combination of the first emulsifier, the second emulsifier and the dispersant can achieve the best effect.

[0030] The aqueous emulsion contains a solvent, and the mass content of the solvent is preferably 10%-40%, more preferably 15%-40%. In some specific embodiments of the present invention, the mass content of the solvent is 15%, 32% or 40%.

[0031] Preferably, the solvent is selected from one or more of solvent oil S-200, solvent oil S-150, solvent oil S-100, N,N-dimethyldecylamide, and cyclohexanone; more preferably, one or more of solvent oil S-200 and solvent oil S-150.

[0032] The aqueous emulsion contains a co-solvent, and the mass content of the co-solvent is preferably 1%-6%, more preferably 2%-4%. In some specific embodiments of the present invention, the mass content of the co-solvent is 2%, 3% or 4%.

[0033] Preferably, the co-solvent is selected from one or more of N-methylpyrrolidone, isophorone, dimethyl sulfoxide, and methyl oleate; more preferably, it is one or more of N-methylpyrrolidone and isophorone.

[0034] The aqueous emulsion contains antifreeze, and the mass content of the antifreeze is preferably 3%-8%, more preferably 5%-8%. In some specific embodiments of the present invention, the mass content of the antifreeze is 5%, 6%, 7% or 8%.

[0035] Preferably, the antifreeze agent is selected from one or more of urea, potassium chloride, ethylene glycol, propylene glycol, polyethylene glycol and sodium chloride; more preferably one or more of ethylene glycol and polyethylene glycol.

[0036] The water solvent contains a stabilizer, and the mass content of the stabilizer is preferably 0.1%-2%, more preferably 1%-2%. In some specific embodiments of the present invention, the mass content of the stabilizer is 1% or 2%.

[0037] Preferably, the stabilizer is selected from one or more of dibutyl hydroxytoluene, butyl hydroxyanisole, propyl gallate, sodium carbonate, and o-hydroxydimethyl ketone; more preferably, it is one or more of dibutyl hydroxytoluene and butyl hydroxyanisole.

[0038] In some specific embodiments of the present invention, the solvent, co-solvent, antifreeze agent and stabilizer are solvent oil S-200, N-methylpyrrolidone, ethylene glycol and butylated hydroxytoluene, and their mass contents are 32%, 2%, 5% and 1% respectively.

[0039] In some specific embodiments of the present invention, the solvent, co-solvent, antifreeze agent and stabilizer are solvent oil S-150, isophorone, ethylene glycol and butylated hydroxytoluene, and their mass contents are 32%, 2%, 5% and 1% respectively.

[0040] In some specific embodiments of the present invention, the solvent, co-solvent, antifreeze agent and stabilizer are solvent oil S-150, isophorone, ethylene glycol and butylated hydroxyanisole, and their mass contents are 40%, 2%, 5% and 1% respectively.

[0041] In some specific embodiments of the present invention, the solvent, co-solvent, antifreeze agent and stabilizer are solvent oil S-150, isophorone, polyethylene glycol and butylated hydroxyanisole, and their mass contents are 15%, 2%, 8% and 2% respectively.

[0042] The aqueous emulsion provided by the present invention further contains a balance of water.

[0043] The present invention provides a method for preparing the aqueous emulsion containing avermectin and thiazolyl, comprising the following steps:

[0044] S1) mixing antifreeze agent and water uniformly to obtain an aqueous phase;

[0045] The active pharmaceutical ingredient, emulsifier, dispersant, solvent, cosolvent and stabilizer are mixed to obtain an oil phase;

[0046] S2) mixing the aqueous phase and the oil phase to obtain an aqueous emulsion containing avermectin and thiazolyl.

[0047] Preferably, in the above mixing process, each material is subjected to high-speed shearing at a shearing speed of 1000-10000 r / min.

[0048] The present invention has no special limitation on the feeding method of the above materials, and any feeding method disclosed in the prior art can be used. Preferably, after homogenization, the particles are tested with a laser particle size distribution analyzer until the particle size D90 is less than 1.2 μm.

[0049] Compared with the prior art, the present invention provides an aqueous emulsion containing avermectin and thiazole, which comprises, by mass percentage, 10%-50% of active pharmaceutical ingredients, 2%-10% of emulsifier, 0.5%-8% of dispersant, 10%-40% of solvent, 1%-6% of cosolvent, 3%-8% of antifreeze, 0.1%-2% of stabilizer, and 100% of deionized water; the active pharmaceutical ingredients include avermectin and thiazole. The present invention optimizes the above-mentioned mass ratio, improves the efficacy of the product, and reduces the amount of insecticide and the frequency of application, thereby reducing the cost of the drug. The present invention improves the stability of the product by optimizing the auxiliary agent, effectively solves the influence of environmental changes during transportation, and avoids the risks of stratification, demulsification, water precipitation and crystallization. It also solves the problem of decomposition of active ingredients, meets the use of different countries and regions, and is conducive to large-scale promotion and application. DETAILED DESCRIPTION

[0050] In order to further illustrate the present invention, the aqueous emulsion containing avermectin and thiazolyl and the preparation method thereof provided by the present invention are described in detail below with reference to the examples.

[0051] Examples 1-8

[0052] According to the ratio in Table 1, antifreeze and water are added into the kettle, and they are fully mixed and dispersed evenly; the original drug, emulsifier, dispersant, solvent, co-solvent and stabilizer are put into the oil phase kettle, and after they are completely dissolved, the oil phase is mixed with the water phase to obtain an aqueous emulsion containing avermectin and thiazolyl.

[0053] Comparative Example 1-2

[0054] The preparation method is the same as that of Examples 1-8, and the distribution ratio of each group is shown in Table 1.

[0055] Table 1 Ratio of raw materials in Examples 1-8 and Comparative Examples 1-2 (mass percentage)

[0056]

[0057]

[0058]

[0059] The properties of the aqueous emulsions prepared in Examples 1-8 and Comparative Examples 1-2 were tested, and the results are shown in Table 2 below.

[0060] Table 2 Performance of the avermectin·thiazolyl aqueous emulsion prepared in Examples 1-8 and Comparative Examples 1-2

[0061]

[0062]

[0063] Example 9 Single Factor Control Experiment

[0064] On the basis of Example 1, the first emulsifier methyl alcohol polyoxyethylene ether was replaced by polyurethane, and the other materials and their contents remained unchanged to prepare an aqueous emulsion, which was recorded as 1#.

[0065] On the basis of Example 1, the second emulsifier EO-PO block polyether was replaced with Nongru 700#, and the other materials and contents remained unchanged to prepare an aqueous emulsion, which was recorded as 2#.

[0066] On the basis of Example 1, the dispersant tristyrylphenol polyoxyethylene ether phosphate triethanolamine salt was replaced with alkylbenzene sulfonate, and the other materials and contents remained unchanged to prepare an aqueous emulsion, which was recorded as 3#.

[0067] On the basis of Example 1, the solvent oil S-200 was replaced by toluene, and the other materials and their contents remained unchanged to prepare an aqueous emulsion, which was recorded as 4#.

[0068] On the basis of Example 1, the stabilizer butylated hydroxytoluene was replaced by triisopropanolamine, and the other materials and their contents remained unchanged to prepare an aqueous emulsion, which was recorded as 5#.

[0069] The properties of the prepared aqueous emulsion were tested and the results are shown in Table 3 below.

[0070] Table 3 Performance of avermectin·thiazolyl emulsion in water 1#-5#

[0071]

[0072]

[0073] Test Example 3 Indoor toxicity test of thiazolyl and avermectin:

[0074] Pepper root knot nematode blocks were collected from pepper fields in Hualong Town, Shouguang City, Shandong Province, and indoor toxicity tests were conducted in the laboratory of Weifang Runfeng Chemical Co., Ltd., and 2nd instar larvae were used for the test. The root of the diseased plant was separated from the root of the root knot nematode. After the single egg mass was inoculated on the root of the pepper for purification and culture, the diseased roots were collected, cut into small sections of about 2 cm, rinsed in 1% sodium hypochlorite solution for about 4 minutes, and washed and collected nematode eggs using 200 mesh and 500 mesh nematode sieves. The eggs were diluted with distilled water to 200 eggs / mL, and the egg liquid was dripped onto a shallow plate covered with 2 layers of towel paper and placed for 3 days. Then the hatched 2nd instar larvae were collected to make a suspension for biological testing. Test method: Use a pipette to draw 2mL of the drug solution from low concentration to high concentration and add it to the test tube respectively, then draw 2mL of the prepared nematode suspension and add it to the culture tube, so that the drug solution and the nematode suspension are mixed evenly in equal amounts (100 / mL). The treated samples were placed in a (25±1)°C culture box for culture, and 1 mL was taken out 24 hours after treatment to examine the death of nematodes using a counting dish, and each sample was repeated 3 times. The results are shown in Table 4.

[0075] The embodiment of the present invention adopts the method of indoor toxicity determination. According to the Sun Yunpei method, the indoor toxicity determination is carried out to clarify the co-toxicity coefficient (CTC) of two drugs after compounding in a certain ratio. CTC < 80 is antagonistic effect, 80 ≤ CTC ≤ 120 is additive effect, and CTC > 120 is synergistic effect.

[0076] All experimental reagents were provided by Shandong Weifang Runfeng Chemical Co., Ltd.

[0077] Table 4 Indoor toxicity data

[0078] Test drug Ratio <![CDATA[LC 50 (mg / L)]]> CTC Thiazofosfate -- 42.6 -- Avermectin -- 8.4 -- Thiazofosfamide: Avermectin 50:1 35.1 112.4 Thiazofosfamide: Avermectin 19:1 24.7 143.3 Thiazofosfamide: Avermectin 9:1 21.3 142.1 Thiazofosfamide: Avermectin 4:1 17.6 133.4 Thiazofosfamide: Avermectin 1:1 13.1 107.1

[0079] The results of the indoor toxicity test showed that the combination of thiamethoxam and avermectin had a significant synergistic effect, and the effect on pepper root-knot nematodes was significantly better than that of a single agent. In addition, a good synergistic effect was obtained when the mass ratio of avermectin to thiamethoxam was 1:19.

[0080] Test Example 4: Field efficacy test of thiazolyl and avermectin:

[0081] This experiment was conducted in the pepper shed of Shouguang Vegetable Base. The control agents were 20% thiazolyl emulsion (commercially available) and 1.8% avermectin emulsifiable concentrate (commercially available). There were 5 treatments in total, namely: Treatment 1: clean water spray, blank control; Treatment 2: Example 1; Treatment 3: Example 5; Treatment 4: 20% thiazolyl emulsion; Treatment 5: 1.8% avermectin emulsifiable concentrate, 20m per plot. 2 , the cells are randomly arranged.

[0082] Table 5: Application amount of each experimental group

[0083]

[0084] According to the dosage of the preparation per mu, 400L of water was added to prepare the solution for root irrigation of the plants, and the amount of solution was converted into the volume of the plot for uniform root irrigation. The weather was good when the pesticide was applied, and there were no adverse weather factors on the day of application.

[0085] Field efficacy test investigation, calculation and statistical methods for root-knot nematode: Specifically, 5 random sampling points were selected in each plot, and soil samples were collected from the root area of ​​the crop (0-20 cm deep) at each point, with a total of 500 mL of samples. After soil collection, the soil was brought back to the laboratory for separation using the shallow plate method, and the number of separated nematodes was recorded. The samples were checked once at 30 days and 60 days after application. The results are shown in Table 6.

[0086]

[0087]

[0088] Table 6 Field efficacy test results of each treatment agent for controlling pepper root-knot nematodes

[0089]

[0090] The results of the field efficacy test showed that the synergistic effect of thiazolyl and avermectin was obvious. Under normal use, the control effect on pepper root-knot nematodes was significantly better than that of a single agent. In addition, Example 1 obtained more stable physical indicators and lower formulation dosage by optimizing the auxiliary agent.

[0091] The above embodiments are only used to help understand the method and core idea of ​​the present invention. It should be noted that, for those skilled in the art, several improvements and modifications can be made to the present invention without departing from the principles of the present invention, and these improvements and modifications also fall within the scope of protection of the claims of the present invention.

Claims

1. An aqueous emulsion containing avermectin and thiazolyl, characterized in that: In terms of mass percentage, it includes: Active pharmaceutical ingredient 10%-50%, emulsifier 2%-10%, dispersant 0.5%-8%, solvent 10%-40%, cosolvent 1%-6%, antifreeze 3%-8%, stabilizer 0.1%-2%, deionized water to make up 100%; The active ingredients of the medicine include avermectin and thiazolyl.

2. The aqueous emulsion containing avermectin and thiazolyl as claimed in claim 1, characterized in that: The emulsifier includes a first emulsifier and a second emulsifier; The first emulsifier is selected from one or more of octylphenol polyoxyethylene polyoxypropylene ether, cyclohexene polyoxyethylene polyoxypropylene, benzyl biphenol polyoxyethylene polyoxypropylene, benzylphenol polyoxyethylene polyoxypropylene, phenethylphenol polyoxyethylene ether polyoxypropylene ether, isopropylphenyl phenethylphenol polyoxyethylene ether, styrenephenol polyoxyethylene ether, octylphenol polyoxyethylene ether, secondary octylphenol polyoxyethylene ether, nonylphenol polyoxyethylene ether, bis-nonylphenol polyoxyethylene ether, benzylphenol polyoxyethylene ether, fatty lauryl alcohol polyoxyethylene ether, oleyl alcohol polyoxyethylene ether, isotridecanol polyoxyethylene ether, fatty acid polyoxyethylene ether, fatty amine polyoxyethylene ether, and methyl alcohol polyoxyethylene ether; The second emulsifier is selected from one or more of glycerol esters, polyglycerol esters, sugar esters, EO-PO block polyethers, calcium dodecylbenzene sulfonate, distyrylphenol polyformaldehyde condensates, triglycerol monostearate, arylphenol polyoxyethylene ether formaldehyde condensates, stearates, polyoxyethylene oleates, castor oil polyoxyethylene ether phosphates, sorbitan ester ethers, polyglycerol fatty acid esters, succinate sulfonates, α-sulfo fatty acid ester salts, and polyarylphenol ether sulfates; The dispersant is selected from one or more of high molecular polymer, polystyrene acrylic acid sodium salt, maleic rosin block polyether sulfonate ammonium salt, diisopropylnaphthalene sulfonate sodium salt, benzylnaphthalene sulfonic acid formaldehyde condensate sodium salt, styrene acrylic acid copolymer sodium salt, tristyrylphenol polyoxyethylene ether phosphate triethanolamine salt, maleic rosin block polyether sulfonate ammonium salt, styrene maleic anhydride copolymer sodium salt, maleic anhydride copolymer sodium salt, maleic anhydride acrylic acid copolymer, fatty alcohol polyoxyethylene polyoxypropylene ether, styrene maleic anhydride copolymer sodium salt, alkanolamide polyoxyethylene ether phosphate, sodium lignin sulfonate, calcium lignin sulfonate, sodium diethyl succinate sulfate, and sodium butadiene styrene sulfonate.

3. The aqueous emulsion containing avermectin and thiazolyl as claimed in claim 2, characterized in that: The first emulsifier is selected from one or more of methyl alcohol polyoxyethylene ether and nonylphenol polyoxyethylene ether; The second emulsifier is selected from one or more of EO-PO block polyether and calcium dodecylbenzene sulfonate; The dispersant is selected from one or more of tristyrylphenol polyoxyethylene ether phosphate triethanolamine salt and benzylnaphthalenesulfonic acid formaldehyde condensate sodium salt.

4. The aqueous emulsion containing avermectin and thiazolyl as claimed in claim 3, characterized in that: The first emulsifier is methyl alcohol polyoxyethylene ether; The second emulsifier is EO-PO block polyether; The dispersant is tristyrylphenol polyoxyethylene ether phosphate triethanolamine salt or benzylnaphthalenesulfonic acid formaldehyde condensate sodium salt.

5. The aqueous emulsion containing avermectin and thiazolyl as claimed in any one of claims 2 to 4, characterized in that: The mass ratio of the first emulsifier, the second emulsifier and the dispersant is 1-4:1-4:1-4.

6. The aqueous emulsion containing avermectin and thiazolyl as claimed in claim 5, characterized in that: The mass ratio of the first emulsifier, the second emulsifier and the dispersant is 1-2:1-2:1-2.

7. The aqueous emulsion containing avermectin and thiazolyl as claimed in claim 6, characterized in that: The mass ratio of the first emulsifier, the second emulsifier and the dispersant is 1.5:1.5:

1.

8. The aqueous emulsion containing avermectin and thiazolyl as claimed in claim 1, characterized in that: The solvent is selected from one or more of solvent oil S-200, solvent oil S-150, solvent oil S-100, N,N-dimethyldecylamide, and cyclohexanone; The cosolvent is selected from one or more of N-methylpyrrolidone, isophorone, dimethyl sulfoxide, and methyl oleate; The antifreeze agent is selected from one or more of urea, potassium chloride, ethylene glycol, propylene glycol, polyethylene glycol and sodium chloride; The stabilizer is selected from one or more of butylated hydroxytoluene, butylated hydroxyanisole, propyl gallate, sodium carbonate, and o-hydroxydimethyl ketone.

9. The aqueous emulsion containing avermectin and thiazolyl as claimed in claim 8, characterized in that: The solvent is selected from one or more of solvent oil S-200 and solvent oil S-150; The cosolvent is selected from one or more of N-methylpyrrolidone and isophorone; The stabilizer is selected from one or more of butylated hydroxytoluene and butylated hydroxyanisole; The antifreeze agent is selected from one or more of ethylene glycol and polyethylene glycol.

10. The method for preparing the aqueous emulsion containing avermectin and thiazolyl as claimed in any one of claims 1 to 9, comprising the following steps: S1) mixing antifreeze agent and water uniformly to obtain an aqueous phase; The active pharmaceutical ingredient, emulsifier, dispersant, solvent, cosolvent and stabilizer are mixed to obtain an oil phase; S2) mixing the aqueous phase and the oil phase to obtain an aqueous emulsion containing avermectin and thiazolyl.

Citation Information

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