A compound sanitary insecticide composition and its application

By compounding oxadone and compound I-72, a compounded sanitary insecticide composition with various dosage forms is formed, which solves the problems of pyrethroid insecticide resistance and oxadone stability, and achieves high-efficiency, low-toxicity, long-lasting insecticidal effects and environmentally friendly insecticide applications.

CN119111547BActive Publication Date: 2025-09-12JIANGSU YANGNONG CHEM CO LTD +1
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Patent Information

Application Number
CN202310695406.5
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2023-06-13
Publication Date
2025-09-12
Estimated Expiration
2043-06-13

AI Technical Summary

Technical Problem

Existing pyrethroid insecticides can cause pests to develop resistance after long-term use. In addition, pyrethroids are unstable under high temperatures and light and easily degrade in water, affecting their efficacy.

Method used

The oxadiazine is compounded with the piperic acid derivative compound I-72 to form a compounded sanitary insecticide composition in various dosage forms, including emulsifiable concentrates, water emulsions, microemulsions, etc., supplemented with stabilizers and other adjuvants to improve stability and insecticidal effects.

Benefits of technology

It achieves high efficiency, low toxicity, and long-lasting insecticidal effects, delays pest resistance, reduces the number of spraying times, reduces costs, and is environmentally friendly.

✦ Generated by Eureka AI based on patent content.

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Abstract

The present invention discloses a compound sanitary insecticide composition and its application. The active ingredients are active ingredient A and active ingredient B, wherein active ingredient A is pyrethroid and active ingredient B is a piperic acid derivative compound, with the remainder being an adjuvant. The weight ratio of active ingredient A to active ingredient B is 1:20 to 20:1, preferably 1:5 to 5:1, and the total weight percentage of active ingredient A and active ingredient B in the composition is 2 to 80%. The binary composition solves the problem of pest resistance to pyrethroids and has the characteristics of high efficiency, low toxicity, and environmental friendliness. The binary composition is suitable for indoor and outdoor control of pests including mosquitoes, flies, cockroaches, fleas, bedbugs, millipedes, and other sanitary pests, and is suitable for homes, restaurants, hotels, train compartments, and animal husbandry.
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Description

Technical Field

[0001] The present invention relates to a binary sanitary insecticide composition and application thereof, in particular to an insecticide composition containing methoprene and a piperic acid derivative compound and application thereof, belonging to the technical field of sanitary insecticide. Background Art

[0002] For a long time, the types of preparations used to control public health pests have been relatively single, and most of the residual spraying and space spraying insecticides used for public health pests are single or compound pyrethroids. The long-term use of pyrethroid insecticides has caused health pests such as mosquitoes, flies, and cockroaches to develop varying degrees of resistance to some pyrethroids.

[0003] Methicillin has both contact and stomach toxic effects on insect pests, with good knockdown activity. It possesses the dual properties of inhibiting acetylcholinesterase and acting on synapses, making it primarily used as a sanitary insecticide for controlling houseflies, cockroaches, and other pests. However, the technical form of methicillin is relatively unstable, being unstable above 50°C and gradually degrading under light. Furthermore, its solubility in water is only 1 g / L, making it susceptible to degradation in aqueous liquid formulations. Therefore, ensuring the stability of methicillin in pesticide formulations is a key approach to improving its efficacy.

[0004] Chinese invention patent CN112457288 discloses a piperic acid derivative and its application. Compound I-72 has a novel mechanism of action, exhibits no cross-resistance with existing commonly used insecticides, exhibits a broad insecticide spectrum, and exhibits long-lasting efficacy. The compound's structural formula is as follows:

[0005]

[0006] At present, the only registered formulation of oxadone is aerosol for use against sanitary pests. The present invention has found through experiments that the combination of oxadone and piperic acid derivatives has a synergistic effect. On the one hand, it has good environmental compatibility and reduces the amount of pesticide used. On the other hand, from the perspective of the mechanism of action, oxadone and piperic acid derivatives have different mechanisms of action and no cross-resistance exists, which improves the control effect. The combination of insecticides with different mechanisms of action can also delay pest resistance, which is beneficial to pest resistance management. Summary of the Invention

[0007] The technical problem to be solved by the present invention is to address the deficiencies in the prior art and to provide a compound sanitary insecticide composition and its application. The composition is a compound sanitary insecticide composition of oxadone and compound I-72. After compounding, the two have the characteristics of high efficiency, low toxicity, and good lasting effect, can reduce the number of applications, reduce costs, and be more environmentally friendly; on the other hand, the compound of oxadone and compound I-72 can delay the development of drug resistance in sanitary pests.

[0008] In order to achieve the above object, the present invention adopts the following technical solutions:

[0009] The present invention first provides a compound sanitary insecticide composition, wherein the active ingredients are composed of active ingredient A and active ingredient B, the total weight of active ingredient A and active ingredient B accounts for 2-80% of the weight of the entire insecticide composition, and the balance is adjuvant;

[0010] The active ingredient A is oxadiazine;

[0011] The active ingredient B is a piperic acid derivative compound represented by formula I (referred to as compound I-72):

[0012]

[0013] In the above technical solution, the weight ratio of the compound of oxadone and the piperic acid derivative compound is 1:20 to 20:1, preferably 1:5 to 5:1.

[0014] In the above technical solution, the auxiliary agent is any one of a dispersant, an emulsifier, a stabilizer, an antifreeze agent, a thickener, a preservative, a defoaming agent, a solvent, a wetting agent, a disintegrant, water and a filler, or a mixture of two or more in any proportion.

[0015] In the above technical solution, the compound sanitary insecticide composition is in the form of one of emulsifiable concentrate, aqueous emulsion, microemulsion, soluble liquid, suspension, wettable powder and water-dispersible granules; it can be prepared into a preparation according to the needs in accordance with the technical methods known in the art.

[0016] In the above technical solution, the compound sanitary insecticide composition, when in the form of emulsifiable concentrate, comprises the following raw materials in weight percentage: 1% to 10% of oxadone, 1% to 20% of compound I-72, 7% to 20% of emulsifier, and the solvent is supplemented to 100%.

[0017] In the above technical solution, the compound sanitary insecticide composition, when in the form of an aqueous emulsion, comprises the following raw materials in weight percentage: 1% to 20% of oxadone, 1% to 20% of compound I-72, 2% to 6% of a stabilizer, 5% to 30% of an emulsifier, 10% to 30% of a solvent, 1% to 5% of an antifreeze agent, 0.1% to 0.5% of a defoaming agent, and water is added to 100%.

[0018] In the above technical solution, the compound sanitary insecticide composition, when in the form of a microemulsion, comprises the following raw materials in weight percentage: 1% to 10% of oxadone, 1% to 10% of compound I-72, 2% to 6% of a stabilizer, 10% to 40% of an emulsifier, 30% to 50% of a solvent, and water to 100%.

[0019] In the above technical solution, the compound sanitary insecticide composition, when in the form of a soluble liquid, comprises the following raw materials in weight percentage: 1% to 10% of oxadone, 1% to 20% of compound I-72, 2% to 6% of stabilizer, 5% to 20% of emulsifier, and the solvent is supplemented to 100%.

[0020] In the above technical solution, the compound sanitary insecticide composition, when in the form of a suspension, comprises the following raw materials in weight percentage: 1% to 20% of oxadone, 1% to 20% of compound I-72, 0.5% to 5% of a wetting agent, 1% to 20% of a dispersant, 2% to 6% of a stabilizer, 0.2% to 2% of a thickener, 1% to 10% of an antifreeze agent, 0.1% to 0.5% of a preservative, 0.1% to 0.5% of a defoaming agent, and water is added to 100%.

[0021] In the above technical solution, the compound sanitary insecticide composition, when in the form of a wettable powder, comprises the following raw materials in weight percentage: 1% to 20% of oxadone, 1% to 40% of compound I-72, 2% to 6% of a stabilizer, 0.5% to 5% of a wetting agent, 1% to 15% of a dispersant, and the filler is supplemented to 100%.

[0022] In the above technical solution, the compound sanitary insecticide composition, when in the form of water-dispersible granules, comprises the following raw materials in weight percentage: 1% to 40% of oxadone, 1% to 40% of compound I-72, 2% to 6% of stabilizer, 1% to 4% of wetting agent, 1% to 10% of dispersant, 1% to 10% of disintegrant, and the filler is supplemented to 100%.

[0023] In the above technical solution, the stabilizer is selected from: any one of benzotriazole and sodium hexametaphosphate or a mixture of the two in any proportion, the purpose of which is to prevent the degradation of oxadone and prevent the weakening of the drug efficacy.

[0024] In the above technical solution, the dispersant is selected from: any one of polycarboxylates, alkylphenol polyoxyethylene ether formaldehyde condensates, naphthalenesulfonic acid formaldehyde condensates sodium salts, fatty acid polyoxyethylene ethers, fatty amine polyoxyethylene ethers, lignin sulfonates, and block polyethers, or a mixture of two or more in any proportion.

[0025] In the above technical solution, the wetting agent is selected from: any one of naphthalene sulfonate, alkyl sulfate, phenylethylphenol polyoxyethylene ether phosphate, alkyl sulfonate, opening powder BX, sodium dodecylbenzene sulfonate, or a mixture of two or more in any proportion.

[0026] In the above technical solution, the emulsifier is selected from: any one of calcium dodecylbenzenesulfonate, dodecylphenol polyoxyethylene ether, phenethylphenol polyoxyethylene ether, nonionic hydroxy polyethylene oxide block copolymer, castor oil polyoxyethylene ether, polyoxyethylene ether formaldehyde condensate sulfate, and fatty alcohol polyoxyethylene ether, or a mixture of two or more in any proportion.

[0027] In the above technical solution, the thickener is selected from: any one of xanthan gum, methyl cellulose, and magnesium aluminum silicate, or a mixture of two or more of the above in any proportion.

[0028] In the above technical solution, the preservative is selected from: any one of potassium sorbate, sodium benzoate, and kasonon, or a mixture of two or more of them in any proportion.

[0029] In the above technical solution, the defoaming agent is selected from: any one of silicone compounds, silicone oil, lauric acid, and stearic acid, or a mixture of two or more of them in any proportion.

[0030] In the above technical solution, the solvent is selected from: any one of isopropyl myristate, tributyl citrate, acetyl tributyl citrate, diisopropyl adipate, N,N-dimethyl decanoyl amide, aromatic solvent oil, dodecylbenzene, N-methyl pyrrolidone, or a mixture of two or more in any proportion.

[0031] The disintegrant is selected from the group consisting of ammonium sulfate, sodium bicarbonate, and sodium sulfate.

[0032] The antifreeze agent is selected from one or more of ethylene glycol, propylene glycol, glycerol, glycerin and urea.

[0033] The filler is selected from one or more of kaolin, diatomaceous earth, bentonite, white carbon black and corn starch.

[0034] The present invention also provides an application of the compound sanitary insecticide composition in preventing and controlling sanitary pests in application fields.

[0035] In the above technical solution, the application fields include homes, restaurants, hotels, carriages, animal breeding and other places.

[0036] In the above technical solution, the sanitary pests include Culex pipiens pallens, Culex pipiens quinquefasciatus, Aedes albopictus, Aedes aegypti, Anopheles sinensis, housefly, city fly, big-headed golden fly, Lucilia sericata, Lucilia cuprina, bright green fly, German cockroach, American cockroach, human flea, bed bug, striped millipede, pink millipede, etc.

[0037] In the above technical solution, when the compound sanitary insecticide composition is used to control sanitary pests, the insecticide composition is diluted 50-300 times with water and sprayed on surfaces such as walls, doors, windows, ceilings and home furnishings, so that the binary sanitary insecticide remains on the surface of the above objects, knocking down and killing the sanitary pests. Its applicable dosage forms are suspension concentrate, wettable powder and water-dispersible granules.

[0038] In the above technical solution, when the compound sanitary insecticide composition is used to control sanitary pests, the insecticide composition is diluted 50-300 times with water and then evenly sprayed into the space using spray equipment such as ultra-low volume, fog machine, and constant volume spray, so that the sanitary pests are exposed to the agent when they are active in the spraying space, thereby knocking down and killing the sanitary pests, thereby controlling the sanitary pests. Its applicable dosage forms are emulsifiable concentrates, water emulsions, microemulsions and soluble liquids.

[0039] Compared with the existing technology, it has the following characteristics:

[0040] The present invention's insecticide composition boasts high efficacy, low toxicity, and environmental friendliness, primarily addressing pyrethroid resistance in sanitary pests. Experiments have shown that a combination of pyrethroid-containing fentamidine and compound I-72 not only addresses this resistance issue but also significantly improves both knockdown and lethality against sanitary pests compared to existing insecticides. DETAILED DESCRIPTION

[0041] The following describes in detail the specific implementation of the technical solution of the present invention, but the present invention is not limited to the following description:

[0042] The preparation methods of the dosage forms in each embodiment of the present invention are as follows:

[0043] The preparation method of the emulsifiable concentrate is as follows: weigh oxadone, compound I-72, an emulsifier and a solvent according to a formula, heat and mix them evenly, and then the emulsifiable concentrate can be prepared.

[0044] The preparation method of the water emulsion is as follows: weigh oxadone, compound I-72, emulsifier, and solvent according to the ratio, heat and dissolve them to form the oil phase, weigh water, stabilizer and antifreeze according to the ratio to form the aqueous phase, slowly add the aqueous phase to the oil phase under shear conditions, and finally add the defoaming agent, continue shearing for 5 minutes, and the water emulsion can be obtained.

[0045] The preparation method of the microemulsion is as follows: weigh methadone, compound I-72, stabilizer, emulsifier, solvent, and water according to the formula, heat to dissolve, and mix evenly to obtain the microemulsion.

[0046] The preparation method of the soluble liquid is as follows: weigh oxadone, compound I-72, stabilizer, emulsifier, and solvent according to the formula, heat to fully dissolve and mix evenly to obtain the soluble liquid.

[0047] The preparation method of the suspension concentrate is as follows: a wetting agent, a dispersant, a stabilizer, an antifreeze agent, a preservative, a defoamer and water are weighed in proportion and mixed evenly, and then oxadiazine and compound I-72 are added, and the mixture is transferred to a sand mill, and an appropriate amount of zirconium oxide beads are added to the sand mill, and the mixture is ground for 2-3 hours. A thickener is added and the grinding is continued for half an hour, and the zirconium oxide beads are removed by filtering to obtain the suspension concentrate.

[0048] The preparation method of the wettable powder is as follows: the oxadone, compound I-72, stabilizer, wetting agent, dispersant and filler in the proportions are uniformly mixed, and the mixture is crushed by an ultrafine air flow mill to obtain the wettable powder.

[0049] The preparation method of water-dispersible granules is as follows: the oxadone, compound I-72, stabilizer, wetting agent, dispersant, disintegrant and filler in the said proportion are mixed evenly, crushed with an ultrafine air flow mill, kneaded with an appropriate amount of water, and then put into a granulator for extrusion granulation. After drying, water-dispersible granules can be obtained.

[0050] The present invention will be described below in conjunction with specific embodiments:

[0051] Formulation Example 1: 20% oxadiazine·Compound I-72 Suspension

[0052] 4g of oxadipone, 6g of compound I-721, 1.5g of benzotriazole, 1.5g of sodium hexametaphosphate, 5g of sodium polycarboxylate, 3g of sodium ligninsulfonate, 1g of block polyether, 2g of sodium naphthalenesulfonate, 5g of ethylene glycol, 1.5g of magnesium aluminum silicate, 0.3g of xanthan gum, 0.5g of potassium sorbate, 0.2g of silicone oil, and water to 100g. A suspension concentrate was prepared according to the above preparation method.

[0053] Formulation Example 2: 10% oxadiazine·Compound I-72 Suspension

[0054] 2g of oxadipone, 8g of compound I-72, 1g of benzotriazole, 1g of sodium hexametaphosphate, 5g of sodium polycarboxylate, 1g of phenylethylphenol polyoxyethylene ether phosphate, 5g of glycerol, 1.5g of magnesium aluminum silicate, 0.3g of xanthan gum, 0.5g of kasone, 0.2g of lauric acid, and water to 100g. A suspension concentrate was prepared according to the above preparation method.

[0055] Formulation Example 3: 40% Methadone·Compound I-72 Suspension

[0056] 20g of oxadipone, 20g of compound I-72, 2.5g of benzotriazole, 2.5g of sodium hexametaphosphate, 8g of sodium polycarboxylate, 2g of fatty acid polyoxyethylene ether, 2g of sodium lauryl sulfonate, 2g of urea, 3g of propylene glycol, 1.5g of methylcellulose, 0.3g of xanthan gum, 0.5g of sodium benzoate, 0.2g of silicone oil, and water to 100g. A suspension concentrate was prepared according to the above preparation method.

[0057] Formulation Example 4: 18% Methadone·Compound I-72 Water Dispersible Granules

[0058] Water-dispersible granules were prepared by the above method: 15 g of oxadipone, 3 g of compound I-72, 2 g of benzotriazole, 2 g of sodium hexametaphosphate, 8 g of sodium salt of naphthalenesulfonic acid formaldehyde condensate, 2 g of sodium ligninsulfonate, 2 g of flavonoid powder BX, 5 g of ammonium sulfate, and corn starch to make up to 100 g.

[0059] Formulation Example 5: 40% Methadone·Compound I-72 Water Dispersible Granules

[0060] Water-dispersible granules were prepared using the above method: 10g of methoprene, 30g of compound I-72, 1.5g of benzotriazole, 1.5g of sodium hexametaphosphate, 6g of naphthalenesulfonic acid formaldehyde condensate sodium salt, 2g of sodium ligninsulfonate, 3g of sodium lauryl sulfate, 1g of flavonoid powder BX, 5g of sodium sulfate, 20g of corn starch, and bentonite to make up to 100g.

[0061] Formulation Example 6: 80% Methadone·Compound I-72 Water Dispersible Granules

[0062] Water-dispersible granules were prepared using the above method: 40 g of oxadipone, 40 g of compound I-72, 3 g of benzotriazole, 3 g of sodium hexametaphosphate, 6 g of naphthalenesulfonic acid formaldehyde condensate sodium salt, 4 g of sodium ligninsulfonate, 1 g of sodium lauryl sulfate, 2 g of flavonoid powder BX, 5 g of sodium bicarbonate, and corn starch to make up to 100 g.

[0063] Formulation Example 7: 24% Mefenamicone·Compound I-72 Wettable Powder

[0064] A wettable powder was prepared by the above method: 16 g of mefenamic acid, 28 g of compound I-7, 2 g of benzotriazole, 2 g of sodium hexametaphosphate, 4 g of sodium dodecylbenzenesulfonate, 3 g of naphthalenesulfonic acid formaldehyde condensate sodium salt, 3 g of white carbon black, and kaolin to make up to 100 g.

[0065] Formulation Example 8: 30% Methadone·Compound I-72 Wettable Powder

[0066] A wettable powder was prepared by the above method: 20 g of methoprene, 10 g of compound I-72, 2 g of benzotriazole, 2 g of sodium hexametaphosphate, 2 g of sodium lauryl sulfate, 10 g of fatty amine polyoxyethylene ether, 3 g of naphthalenesulfonic acid formaldehyde condensate sodium salt, 3 g of white carbon black, and diatomaceous earth to make up to 100 g.

[0067] Formulation Example 9: 40% Methadone·Compound I-72 Wettable Powder

[0068] A wettable powder was prepared by the above method: 5g of methoprene, 5g of compound I-723, 1g of benzotriazole, 1g of sodium hexametaphosphate, 4g of sodium naphthalenesulfonate, 5g of sodium ligninsulfonate, 5g of sodium naphthalenesulfonic acid formaldehyde condensate, 5g of white carbon black, and corn starch to make up to 100g.

[0069] Formulation Example 10: 8% Methadone·Compound I-72 emulsifiable concentrate

[0070] 6g of oxadipone, 22g of compound I-7, 4g of polyoxyethylene dodecylphenol ether, 3g of calcium dodecylbenzenesulfonate, 10g of tributyl citrate, and aromatic solvent oil S-150# are added to make up to 100g. An emulsifiable concentrate is prepared according to the above preparation method.

[0071] Formulation Example 11: 15% Methadone·Compound I-72 emulsifiable concentrate

[0072] 9g of oxadipone, 6g of compound I-72, 8g of castor oil polyoxyethylene ether, 4g of calcium dodecylbenzenesulfonate, 10g of tributyl citrate, and dodecylbenzene are added to make up to 100g. An emulsifiable concentrate is prepared according to the above preparation method.

[0073] Formulation Example 12: 30% Methadone·Compound I-72 emulsifiable concentrate

[0074] An emulsifiable concentrate was prepared by the above method: 10 g of oxadipone, 20 g of compound I-72, 8 g of fatty alcohol polyoxyethylene ether, 8 g of phenethylphenol polyoxyethylene ether, 4 g of calcium dodecylbenzenesulfonate, 10 g of isopropyl myristate, and dodecylbenzene to a total of 100 g.

[0075] Formulation Example 13: 6% Methadone·Compound I-72 Emulsion in Water

[0076] An aqueous emulsion was prepared by the above method: 1g of oxadipone, 5g of compound I-72, 1g of benzotriazole, 1g of sodium hexametaphosphate, 8g of fatty alcohol polyoxyethylene ether, 2g of phenethylphenol polyoxyethylene ether, 4g of calcium dodecylbenzenesulfonate, 20g of dodecylbenzene, 5g of glycerol, 0.2g of silicone oil, and water to 100g.

[0077] Formulation Example 14: 15% Methadone·Compound I-72 Emulsion in Water

[0078] 3g of oxadipone, 12g of compound I-72, 1g of benzotriazole, 1g of sodium hexametaphosphate, 8g of fatty alcohol polyoxyethylene ether, 2g of phenethylphenol polyoxyethylene ether, 2g of polyoxyethylene ether formaldehyde condensate sodium sulfate, 8g of calcium dodecylbenzenesulfonate, 20g of dodecylbenzene, 5g of propylene glycol, 0.2g of silicone oil, and water to 100g. Prepare an aqueous emulsion according to the above preparation method.

[0079] Formulation Example 15: 31% Mefenamicone·Compound I-72 Emulsion in Water

[0080] An aqueous emulsion was prepared using 20g of methoprene, 1g of compound I-72, 2g of benzotriazole, 2g of sodium hexametaphosphate, 8g of fatty alcohol polyoxyethylene ether, 2g of phenethylphenol polyoxyethylene ether, 2g of calcium dodecylbenzenesulfonate, 15g of tributyl citrate, 5g of dodecylbenzene, 5g of ethylene glycol, 0.2g of stearic acid, and water to 100g.

[0081] Formulation Example 16: 8% Mefenamicone·Compound I-72 Microemulsion

[0082] 1g of oxadiazine, compound I-727g, 1g of benzotriazole, 1g of sodium hexametaphosphate, 20g of fatty alcohol polyoxyethylene ether, 5g of calcium dodecylbenzenesulfonate, 50g of N,N-dimethylhexylamine, and water to make up to 100g. A microemulsion was prepared according to the above preparation method.

[0083] Formulation Example 17: 13% Methadone·Compound I-72 Microemulsion

[0084] 3g of oxadiazine, 10g of compound I-72, 1g of benzotriazole, 1g of sodium hexametaphosphate, 20g of castor oil polyoxyethylene ether, 5g of calcium dodecylbenzenesulfonate, 30g of N,N-dimethyltaurate, 15g of acetyl tributyl citrate, and water to make up to 100g. A microemulsion was prepared according to the above preparation method.

[0085] Formulation Example 18: 20% Methadone·Compound I-72 Microemulsion

[0086] A microemulsion was prepared by the above method: 10g of oxadiazine, 10g of compound I-72, 1g of benzotriazole, 1g of sodium hexametaphosphate, 20g of polyoxyethylene dodecylphenol ether, 5g of calcium dodecylbenzenesulfonate, 30g of N,N-dimethyldecanoamide, 15g of dodecylbenzene, and water to make up to 100g.

[0087] Formulation Example 19: 2% oxazolidinone·Compound I-72 soluble solution

[0088] 1g of oxadipone, 1g of compound I-72, 1g of benzotriazole, 1g of sodium hexametaphosphate, 10g of nonionic hydroxypolyethylene oxide block copolymer, 2g of calcium dodecylbenzenesulfonate, and N-methylpyrrolidone to make up to 100g. A soluble liquid was prepared according to the above preparation method.

[0089] Formulation Example 20: 20% oxadiazine·Compound I-72 soluble solution

[0090] 5g of methicillin, 15g of compound I-72, 1g of benzotriazole, 1g of sodium hexametaphosphate, 10g of dodecylphenol polyoxyethylene ether, 5g of calcium dodecylbenzenesulfonate, 25g of diisopropyl adipate, and N-methylpyrrolidone to make up to 100g. A soluble liquid was prepared according to the above preparation method.

[0091] Formulation Example 21: 21% oxadiazine·Compound I-72 soluble solution

[0092] 1g of oxadipone, 20g of compound I-72, 1g of benzotriazole, 1g of sodium hexametaphosphate, 8g of dodecylphenol polyoxyethylene ether, 2g of calcium dodecylbenzenesulfonate, 10g of nonionic hydroxypolyethylene oxide block copolymer, 10g of N,N-dimethyldecanoamide, and N-methylpyrrolidone to a total of 100g. A soluble liquid was prepared according to the above preparation method.

[0093] The products obtained from the various formulation examples of the present invention were subjected to verification tests below.

[0094] Control agent 1: 20% oxadiazine suspension

[0095] 20g of oxadipone, 1.5g of benzotriazole, 1.5g of sodium hexametaphosphate, 5g of sodium polycarboxylate, 2g of sodium naphthalenesulfonate, 3g of sodium ligninsulfonate, 1g of block polyether, 5g of ethylene glycol, 1.5g of magnesium aluminum silicate, 0.5g of potassium sorbate, 0.3g of xanthan gum, 0.2g of silicone oil, and water to 100g. A suspension concentrate was prepared according to the preparation method of Preparation Example 1 of the present invention.

[0096] Control agent 2: 18% compound I-72 water dispersible granules

[0097] Compound I-7218g, benzotriazole 2g, sodium hexametaphosphate 2g, naphthalenesulfonic acid formaldehyde condensate sodium salt 8g, sodium lignin sulfonate 2g, flaking powder BX2g, ammonium sulfate 5g, and corn starch to 100g. Water-dispersible granules were prepared according to the preparation method of Formulation Example 4 of the present invention.

[0098] Control agent 3: 20% oxadiazine·Compound I-72 suspension (without stabilizer)

[0099] 4g of oxadipone, 6g of compound I-721, 5g of sodium polycarboxylate, 2g of sodium naphthalenesulfonate, 3g of sodium ligninsulfonate, 1g of block polyether, 5g of ethylene glycol, 1.5g of magnesium aluminum silicate, 0.5g of potassium sorbate, 0.3g of xanthan gum, 0.2g of silicone oil, and water to 100g were used to prepare a suspension concentrate according to the above preparation method.

[0100] Control agent 4: 8% chlorpyrifos emulsifiable concentrate

[0101] 8g of oxadipone, 4g of dodecylphenol polyoxyethylene ether, 3g of calcium dodecylbenzenesulfonate, 10g of tributyl citrate, and dodecylbenzene are added to make up to 100g. An emulsifiable concentrate is prepared by referring to the preparation method of Preparation Example 10 of the present invention.

[0102] Control agent 5: 6% compound I-72 aqueous emulsion

[0103] Compound I-726g, 1g benzotriazole, 1g sodium hexametaphosphate, 8g fatty alcohol polyoxyethylene ether, 2g phenethylphenol polyoxyethylene ether, 4g calcium dodecylbenzenesulfonate, 20g dodecylbenzene, 5g glycerol, 0.2g silicone oil, and water to 100g. Prepare an aqueous emulsion according to the preparation method of Preparation Example 13 of the present invention.

[0104] Control agent 6: 6% oxazolidinone·Compound I-72 aqueous emulsion (without stabilizer)

[0105] An aqueous emulsion was prepared by the above method: 1 g of oxadipone, 5 g of compound I-72, 8 g of fatty alcohol polyoxyethylene ether, 2 g of dodecylphenol polyoxyethylene ether, 4 g of calcium dodecylbenzenesulfonate, 20 g of dodecylbenzene, 5 g of glycerol, 0.2 g of silicone oil, and water to make up to 100 g.

[0106] Control agent 7: 8% highly effective cypermethrin wettable powder (commercially available)

[0107] Control agent 8: 10% highly effective chlorfenapyr wettable powder (commercially available)

[0108] Control agent 9: 4.5% highly effective cypermethrin emulsion in water (commercially available)

[0109] Control agent 10: 10% highly effective chlorfenapyr emulsion in water (commercially available)

[0110] Verification test 1: Co-toxicity coefficient of oxadone and compound I-72 against Culex pipiens pallens

[0111] Test subjects: Culex pipiens pallens, female adults that did not feed on blood on the 3rd to 5th day after emergence (laboratory-reared);

[0112] Test method: Refer to the Indoor Bioassay Test Guidelines for Pesticides Part 1: Contact Activity Test, and use the spot method NY / T1154.1-2006 to conduct activity determination experiments on Culex pipiens pallens.

[0113] Data Statistics: The co-toxicity coefficient method was used to evaluate the activity of the two compounds against Culex pipiens pallens. DPS statistical software was then used to calculate the toxicity regression equation to obtain the LD50 value for each drug. The toxicity index and co-toxicity coefficient were then calculated using the Sun Yunpei method. A co-toxicity coefficient greater than 120 indicates a synergistic effect, a co-toxicity coefficient between 80-120 indicates an additive effect, and a co-toxicity coefficient less than 80 indicates an antagonistic effect. The results are shown in the table below:

[0114] Table 1 Determination of co-toxicity coefficient (for Culex pipiens pallens)

[0115]

[0116]

[0117] As can be seen from Table 1, the co-toxicity coefficient of oxadone:compound I-72 at a ratio of 1:5 to 5:1 is greater than 120, showing a significant synergistic effect.

[0118] Verification test 2: efficacy test for preventing and controlling mosquitoes and flies

[0119] Test subjects: Culex pipiens and houseflies (laboratory reared)

[0120] Test method: Refer to GB / T13919.1-2009 Indoor efficacy test and evaluation of public health insecticides for pesticide registration, residual spraying test.

[0121] Test agents: Preparation Examples 1, 2, 3, 4, 5, 6, 7, 8, and 9 were diluted with water to 1000 ppm, and control agents 1, 2, 3, 7, and 8 were diluted with water to 1000 ppm.

[0122] Statistics:

[0123] Table 2: Efficacy test of formulation examples 1-9 against mosquitoes and flies

[0124]

[0125]

[0126] As can be seen from Table 2, the KT50 values ​​of the above-mentioned examples of the compounding of oxadipone and compound I-72 for Culex pipiens pallens and houseflies are all less than 5 minutes, and the 24-hour mortality rate exceeds 90%, while the KT50 values ​​of the control agents 1, 2, 7, and 8 for Culex pipiens pallens and houseflies are all greater than 5 minutes, and the 24-hour mortality rate is not greater than 90%. The above-mentioned examples of the compounding of oxadipone and compound I-72 have a significant synergistic effect on the knockdown and lethality of mosquitoes and flies, and compared with commercially available products, the knockdown and lethality of the present invention for mosquitoes and flies are higher. The knockdown and lethality of control agent 3 are reduced compared to Example 1, which illustrates the improvement of the efficacy of the stabilizer. It can be seen that oxadipone and compound I-72 have a good control effect on Culex pipiens pallens and houseflies using a residual spraying method.

[0127] Verification test 3: mosquito and fly control spray efficacy test

[0128] Test subjects: Culex pipiens and houseflies (laboratory reared)

[0129] Test method: Refer to GB / T13919.1-2009 Indoor efficacy test and evaluation of public health insecticides for pesticide registration, spray test.

[0130] Test agents: Preparation Examples 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, and 21 were diluted with water to 800 ppm, and control agents 4, 5, 6, 9, and 10 were diluted with water to 800 ppm.

[0131] Statistics:

[0132] Table 3: Efficacy test of formulation examples 10-21 against mosquitoes and flies

[0133]

[0134]

[0135] As can be seen from Table 3, the KT50 values ​​of the above-mentioned examples of the compounding of oxadipone and compound I-72 for Culex pipiens pallens and houseflies are all less than 5 minutes, and the 24-hour mortality rate exceeds 90%, while the KT50 values ​​of the control agents 4, 5, 9, and 10 for Culex pipiens pallens and houseflies are all greater than 5 minutes, and the 24-hour mortality rate is not greater than 90%. The above-mentioned examples of the compounding of oxadipone and compound I-72 have a significant synergistic effect on the knockdown and lethality of mosquitoes and flies, and compared with commercially available products, the knockdown and lethality of the present invention for mosquitoes and flies are higher. The knockdown and lethality of control agent 6 are reduced compared to Example 13, which illustrates the improvement of the efficacy of the stabilizer. It can be seen that oxadipone and compound I-72 have a good control effect on Culex pipiens pallens and houseflies using a space spray method.

[0136] Verification test 4: efficacy test for preventing and controlling millipede retention

[0137] Test subject: Millipede

[0138] Test Method: 20 millipedes of the same age and in good condition were selected and placed in a transparent tank. The tank was then placed in a 10 m² (2 m x 5 m) area. The applicator sprayed the test agent evenly within the designated area using a small spray bottle at a rate of 15 mL / m². After application, all test insects were collected and transferred to a clean, transparent plastic box. Standard feeding was resumed, and the number of test insects that died after 2 and 24 hours was recorded. Three replicates were set for each treatment, and the 2- and 24-hour mortality rates were calculated.

[0139] Test agents: Preparation Examples 1, 2, 3, 4, 5, 6, 7, 8, and 9 were diluted with water to 1000 ppm, and control agents 1, 2, 3, 7, and 8 were diluted with water to 1000 ppm.

[0140] Statistics:

[0141] Table 4: Efficacy test of formulation examples 1-9 against millipedes

[0142]

[0143]

[0144] The results in Table 4 show that the above examples of the combination of oxadipone and compound I-72 had a better lethal effect on millipedes 2 hours and 24 hours after application than the control agent. This shows that the combination of oxadipone and compound I-72 has a good control effect on millipedes when applied using a residual spraying method.

[0145] All percentages in the formulations of the present invention are by weight. The processing methods and techniques of the various formulations of the compositions are based on existing technologies and may be adjusted and modified according to different circumstances. Any modifications, equivalent substitutions, and improvements made within the spirit and principles of the present invention shall be included within the scope of protection of the present invention.

Claims

1. A compound sanitary insecticide composition, characterized in that: The active ingredients are composed of active ingredient A and active ingredient B, the total weight of active ingredient A and active ingredient B accounts for 2 to 80% of the weight of the entire insecticide composition, and the balance is adjuvants, which include stabilizers; The active ingredient A is oxadiazine; The active ingredient B is a piperic acid derivative compound shown in formula I The stabilizer is selected from: any one of benzotriazole and sodium hexametaphosphate or a mixture of the two in any proportion.

2. The compound sanitary insecticide composition according to claim 1, characterized in that: The weight ratio of the compounding of oxadone and the piperic acid derivative compound is 1:20 to 20:

1.

3. The compound sanitary insecticide composition according to claim 1, characterized in that: The auxiliary agent is any one of a dispersant, an emulsifier, a stabilizer, an antifreeze agent, a thickener, a preservative, a defoaming agent, a solvent, a wetting agent, a disintegrant, water and a filler, or a mixture of two or more in any proportion; the compound sanitary insecticide composition has a dosage form of one of an emulsifiable concentrate, an aqueous emulsion, a microemulsion, a soluble liquid, a suspension, a wettable powder and a water-dispersible granule.

4. The compound sanitary insecticide composition according to claim 3, characterized in that: The compound sanitary insecticide composition, when in the form of an emulsifiable concentrate, comprises the following raw materials in weight percentage: 1% to 10% of oxadone, 1% to 20% of compound I-72, 7% to 20% of an emulsifier, and the solvent is supplemented to 100%; the compound sanitary insecticide composition, when in the form of an aqueous emulsion, comprises the following raw materials in weight percentage: 1% to 20% of oxadone, 1% to 20% of compound I-72, 2% to 6% of a stabilizer, 5% to 30% of an emulsifier, 10% to 30% of a solvent, 1% to 5% of an antifreeze agent, 0.1% to 0.5% of a defoaming agent, and the water is supplemented to 100%.

5. The compound sanitary insecticide composition according to claim 3, characterized in that: The compound sanitary insecticide composition, when in the form of a microemulsion, comprises the following raw materials in weight percentage: 1% to 10% of oxadone, 1% to 10% of compound I-72, 2% to 6% of a stabilizer, 10% to 40% of an emulsifier, 30% to 50% of a solvent, and water makes up to 100%; the compound sanitary insecticide composition, when in the form of a soluble liquid, comprises the following raw materials in weight percentage: 1% to 10% of oxadone, 1% to 20% of compound I-72, 2% to 6% of a stabilizer, 5% to 20% of an emulsifier, and solvent makes up to 100%.

6. The compound sanitary insecticide composition according to claim 3, characterized in that: The compound sanitary insecticide composition, when in the form of a suspension, comprises the following raw materials in weight percentage: 1% to 20% of oxadipone, 1% to 20% of compound I-72, 0.5% to 5% of a wetting agent, 1% to 20% of a dispersant, 2% to 6% of a stabilizer, 0.2% to 2% of a thickener, 1% to 10% of an antifreeze agent, 0.1% to 0.5% of a preservative, 0.1% to 0.5% of a defoaming agent, and the amount is made up to 100% with water; the compound sanitary insecticide composition, when in the form of a wettable powder, comprises the following raw materials in weight percentage: 1% to 20% of oxadipone, 1% to 40% of compound I-72, 2% to 6% of a stabilizer, 0.5% to 5% of a wetting agent, 1% to 15% of a dispersant, and the amount is made up to 100% with a filler.

7. The compound sanitary insecticide composition according to claim 3, characterized in that: The compound sanitary insecticide composition, when in the form of water-dispersible granules, comprises the following raw materials in weight percentage: 1% to 40% of oxadone, 1% to 40% of compound I-72, 2% to 6% of stabilizer, 1% to 4% of wetting agent, 1% to 10% of dispersant, 1% to 10% of disintegrant, and filler is added to 100%.

8. Use of the compound sanitary insecticide composition according to claim 1 in controlling sanitary pests in application fields.

9. The use according to claim 8, characterized in that The application fields include homes, restaurants, hotels, carriages and animal breeding sites; the sanitary pests include Culex pipiens pallens, Culex pipiens quinquefasciatus, Aedes albopictus, Aedes aegypti, Anopheles sinensis, housefly, city fly, Chrysopa bigheaded, Lucilia sericata, Lucilia cuprina, Lucilia luminifera, German cockroach, American cockroach, human flea, bed bug, striped millipede and pink millipede.

Citation Information

Patent Citations

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