Compound bug killing composition and application thereof

Abstract

The invention relates to a sanitary insecticide, in particular to a compound bug killing composition (a perfluthrin and bisamide insecticide) and application thereof. The composition comprises an active component A and an active component B in a weight ratio of (1: 20)-(20: 1), the active ingredient A is afluthrin; and the active ingredient B is any one selected from the group consisting of cyprosulfuron, flubendiamide and polyflubendiamide. The binary composition provided by the invention not only solves the problem of resistance of bed bugs to pyrethroid, but also improves the pesticide effect and pesticide effect stability of the composition through the synergistic interaction among the active components, and has the characteristics of high efficiency, low toxicity, environmental friendliness and the like. The binary composition is suitable for preventing and treating bugs in indoor activity places such as families, carriages, hotels, factory dormitories and the like.

Description

Technical Field

[0001] This invention relates to a sanitary insecticide, specifically to a compound bed bug control composition (pyrethroid and diamide insecticide) and its application. Background Technology

[0002] In the field of integrated pest management, the control of indoor sanitary pests has always faced severe challenges. Bed bugs, due to their strong environmental adaptability and reproductive capacity, have become a global problem. For a long time, the control model relying on single chemical agents has led to increasingly prominent problems of pesticide resistance, especially the widespread development of resistance to pyrethroid insecticides (such as permethrin and lambda-cyhalothrin), which has significantly reduced the effectiveness of conventional spraying treatments in practice.

[0003] In recent years, diamide insecticides (such as cyprodinil and brofenoxuron-methyl) have attracted attention due to their novelty and unique mechanism of action. These compounds target γ-aminobutyric acid (GABA) receptors in the insect nervous system, interfering with the normal function of chloride ion channels, causing disordered nerve signal transmission in pests, ultimately leading to paralysis and death. This mechanism is completely different from that of traditional pyrethroid insecticides, offering new possibilities for delaying or overcoming resistance. However, the use of diamide insecticides alone faces problems such as slow efficacy, high cost, and potential resistance risks.

[0004] Scientific formulation has become an industry consensus to improve control efficacy and extend pesticide lifespan. Procymidone, a pyrethroid containing polyfluorobenzyl groups, not only possesses excellent knockdown activity but also has a long history of safe application in textile protection and other fields, making its application in indoor bed bug control products highly promising and valuable. This study is the first to explore the combination of propofol with diamide insecticides and verify its synergistic effect in actual bed bug control. To further enhance the contact and absorption efficiency of the pesticide on the target surface, this formulation specifically introduces a high-efficiency penetration adjuvant to enhance the deposition and penetration ability of the active ingredient on the bed bug's body wall, thereby achieving a more stable and reliable control effect in complex and concealed environments. Summary of the Invention

[0005] The primary objective of this invention is to provide a compound bed bug-killing composition (a combination of permethrin and a diamide insecticide) that has a synergistic effect against bed bugs, especially highly resistant bed bugs, and its application.

[0006] To achieve the above objectives, the technical solution adopted by the present invention is as follows: A compound bed bug killing composition, comprising active ingredient A and active ingredient B, wherein the weight ratio of active ingredient A to active ingredient B is 1:20 to 20:1; The active ingredient A is propofol; The active ingredient B is selected from any one of cyclopropionamide, brofenoxam, and polyflufenoxam.

[0007] The weight ratio of active ingredient A to active ingredient B in the composition is 1:5 to 5:1.

[0008] The application of the compound bedbug-killing composition, specifically its application in the control of sanitary pests.

[0009] The sanitary pest mentioned is the bedbug, and the application is limited to indoor locations.

[0010] An agent for controlling sanitary pests, comprising the composition described above.

[0011] The formulation comprises an active ingredient and excipients, wherein the active ingredient is the composition of claim 1, accounting for 1 to 60% of the formulation mass.

[0012] The auxiliary agent is one or more of the following: emulsifier, antifreeze, defoamer, solvent, penetrant, and water.

[0013] The auxiliary agent is a penetrant, or a penetrant combined with one or more emulsifiers, antifreeze agents, defoamers, solvents, and water.

[0014] The penetrant accounts for 1% to 5% of the formulation mass; the penetrant is ethoxylated trisiloxane.

[0015] The sanitary pest in question is the bedbug.

[0016] The dosage form is one of emulsifiable concentrate, water emulsion, microemulsion, and soluble liquid; it can be formulated into a preparation according to the requirements and in accordance with the technical methods known in the art.

[0017] In the above technical solution, when the formulation is an emulsifiable concentrate, it includes the following raw materials by weight percentage: 1%~60% propofol, 1%~60% active ingredient B, 7%~20% emulsifier, 1%~5% penetrant, and solvent to make up to 100%.

[0018] In the above technical solution, when the formulation is an emulsion, it includes the following raw materials by weight percentage: 1%~20% propofol, 1%~20% active ingredient B, 5%~30% emulsifier, 1%~5% penetrant, 10%~30% solvent, 1%~5% antifreeze, 0.1%~0.5% defoamer, and water to 100%.

[0019] In the above technical solution, when the formulation is a microemulsion, it includes the following raw materials by weight percentage: 1%~20% propofol, 1%~20% active ingredient B, 10%~40% emulsifier, 1%~5% penetrant, 30%~50% solvent, and water to make up to 100%.

[0020] In the above technical solution, when the formulation is a soluble liquid, it includes the following raw materials in weight percentage: 0.1%~40% propofol, 0.1%~40% active ingredient B, 5%~20% emulsifier, 1%~5% penetrant, and solvent to 100%.

[0021] The penetrant is selected as ethoxylated trisiloxane.

[0022] The emulsifier is selected from any one, two or more of the following: calcium propylene glycol phenyl ether sulfonate, dodecylphenol polyoxyethylene ether, sodium dodecylbenzene sulfonate, phenethylphenol polyoxyethylene ether, nonionic hydroxyl polyoxyethylene block copolymer, castor oil polyoxyethylene ether, polyoxyethylene ether formaldehyde condensate sulfate, and fatty alcohol polyoxyethylene ether, mixed in any proportion.

[0023] The defoamer is selected from any one, two or more of silicone oil, lauric acid, and stearic acid in any proportion.

[0024] The solvent is selected from any one, two or more of the following: tributyl citrate, diisopropyl adipate, ethylene glycol phenyl ether, propylene glycol phenyl ether, dipropylene glycol methyl ether, dipropylene glycol dimethyl ether, N,N-dimethylacetamide, N,N-dimethyldecylamide, and N-methylpyrrolidone, mixed in any proportion.

[0025] The antifreeze is selected from one or more of ethylene glycol, propylene glycol, and glycerol.

[0026] When using the compound insecticidal composition or formulation containing the composition to control bed bugs, dilute the insecticidal composition with water 50-300 times and spray it in places where bed bugs may appear indoors, including the bottom of mattresses, corners, backs of cabinets, crevices in car seats, and other hidden and dark areas. This forms a film on the surface of the areas where bed bugs are active, and the bed bugs can be killed in a short time after crawling and coming into contact with it. Suitable formulations include emulsifiable concentrates, water-in-oil emulsions, microemulsions, and soluble liquids.

[0027] Compared with existing technologies, it has the following characteristics: The bedbug-killing composition of this invention is characterized by high efficiency, low toxicity, and environmental friendliness, and is mainly used to solve the problem of bedbug resistance to traditional insecticides. Experiments have shown that the insecticide composition formulated with propofol not only solves this resistance problem, but also significantly improves its lethality against bedbugs compared to existing bedbug insecticides.

[0028] Meanwhile, the formulation containing the composition of the present invention enhances the penetration of the drug into the body surface of bedbugs by adding a specific penetrant, thereby improving the permeability and lethality of the drug. Detailed Implementation

[0029] The following describes in detail the specific embodiments of the technical solution of the present invention, but the present invention is not limited to the following description: The preparation methods of the dosage forms in the various embodiments of the present invention are as follows: The preparation method of emulsifiable concentrate is as follows: weigh propofol, active ingredient B, emulsifier, penetrant and solvent according to the formula, heat and mix evenly to obtain emulsifiable concentrate.

[0030] The preparation method of water-in-oil emulsion is as follows: Weigh out propofol, active ingredient B, emulsifier, penetrant and solvent according to the ratio, heat and dissolve them to form the oil phase, weigh out water and antifreeze according to the ratio to form the water phase, slowly add the water phase to the oil phase under shear conditions, and finally add the defoamer. Continue shearing for 5 minutes to obtain the water-in-oil emulsion.

[0031] The preparation method of microemulsion is as follows: Weigh out propofol, active ingredient B, emulsifier, solvent, penetrant and water according to the formula, heat to dissolve and mix evenly to obtain microemulsion.

[0032] The preparation method of soluble liquid is as follows: Weigh out propofol, active ingredient B, emulsifier, penetrant and solvent according to the formula, heat to fully dissolve and mix evenly to obtain soluble liquid.

[0033] The present invention will now be described in conjunction with specific embodiments: Formulation Example 1: 12% Profenofibrate·Pofluorfenoxam EC 4g of propargyl fluoride, 8g of polyfluorinated biamide, 4g of dodecylphenol polyoxyethylene ether, 3g of propylene glycol phenyl ether sulfonate calcium, 10g of tributyl citrate, 2g of ethoxylated modified trisiloxane, and ethylene glycol phenyl ether to be made up to 100g. An emulsifiable concentrate was prepared according to the above method.

[0034] Formulation Example 2: 30% Profenofibrate·Cyprodinil EC 12g of propargyl, 18g of cyprodinil, 5g of castor oil polyoxyethylene ether, 10g of sodium dodecylbenzenesulfonate, 10g of tributyl citrate, 3g of ethoxylated trisiloxane, and propylene glycol phenyl ether to be made up to 100g. An emulsifiable concentrate was prepared according to the above method.

[0035] Formulation Example 3: 60% Profenofibrate·Bromoxynil Dimethoate Emulsifiable Concentrate 8g of propargyl fluoride, 52g of bromoxynil dimethoate, 2g of fatty alcohol polyoxyethylene ether, 6g of phenethylphenol polyoxyethylene ether, 8g of sodium dodecylbenzenesulfonate, 5g of ethoxylated trisiloxane, and propylene glycol phenyl ether to be made up to 100g. An emulsifiable concentrate was prepared according to the above method.

[0036] Formulation Example 4: 8% Profenofibrate·Pofluorfenoxam Water Emulsion 2g of propofol, 6g of polyfluorinated biamide, 8g of polyoxyethylene ether formaldehyde condensate sulfate, 2g of phenethylphenol polyoxyethylene ether, 4g of propylene glycol phenyl ether sulfonate calcium, 20g of ethylene glycol phenyl ether, 5g of glycerol, 0.2g of silicone oil, 2g of ethoxylated modified trisiloxane, and water to a final volume of 100g. An aqueous emulsion was prepared according to the above method.

[0037] Formulation Example 5: 18% Profenofibrate·Cyprodinil Water-Emulsion 5g of propargyl, 13g of cyprodinil, 8g of fatty alcohol polyoxyethylene ether, 2g of phenethylphenol polyoxyethylene ether, 2g of sodium sulfate of polyoxyethylene ether formaldehyde condensate, 8g of calcium propylene glycol phenyl ether sulfonate, 20g of ethylene glycol phenyl ether, 5g of propylene glycol, 0.2g of lauric acid, 2g of ethoxylated trisiloxane, and water to a final volume of 100g. An aqueous emulsion was prepared according to the above method.

[0038] Formulation Example 6: 21% Profenofibrate·Bromoxynil Dimethoate Water Emulsion A water-based emulsion was prepared by adding 1g of propargite, 20g of bromoxynil dimethyl ether, 8g of fatty alcohol polyoxyethylene ether, 2g of phenethylphenol polyoxyethylene ether, 2g of propylene glycol phenyl ether sulfonate calcium, 15g of tributyl citrate, 5g of propylene glycol phenyl ether, 5g of ethylene glycol, 0.2g of stearic acid, 8g of ethoxylated trisiloxane, and water to a final volume of 100g.

[0039] Formulation Example 7: 10% Profenofibrate·Pofluorfenoxam Microemulsion 3g of propofol, 7g of polyfluorinated biamide, 20g of fatty acid polyoxyethylene ether, 5g of propylene glycol phenyl ether sulfonate calcium, 20g of N,N-dimethyldecylamide, 10g of dipropylene glycol methyl ether, 2g of ethoxylated trisiloxane, and water to a final volume of 100g were prepared according to the above method.

[0040] Formulation Example 8: 13% Profenofibrate·Cyprodinil Microemulsion 3g of propargyl, 10g of cyprodinil, 20g of castor oil polyoxyethylene ether, 5g of propylene glycol phenyl ether sulfonate calcium, 30g of N,N-dimethyldecylamide, 15g of dipropylene glycol dimethyl ether, 3g of ethoxylated trisiloxane, and water to a final volume of 100g were added. A microemulsion was prepared according to the above method.

[0041] Formulation Example 9: 25% Profenofibrate·Bromoxynil Dimethoate Microemulsion 10g of propargyl fluoride, 15g of bromoxynil dimethicone, 20g of dodecylphenol polyoxyethylene ether, 5g of propylene glycol phenyl ether sulfonate calcium, 30g of N,N-dimethylacetamide, 15g of propylene glycol phenyl ether, 5g of ethoxylated modified trisiloxane, and water to a final volume of 100g were added. A microemulsion was prepared according to the above method.

[0042] Formulation Example 10: 1% Profenofibrate·Pofluorfenoxam Soluble Liquid 0.2g of propofol, 0.8g of polyfluorinated biamide, 10g of nonionic hydroxyl polyethylene oxide block copolymer, 2g of propylene glycol phenyl ether sulfonate calcium, 1g of ethoxylated modified trisiloxane, and N-methylpyrrolidone to a final volume of 100g were prepared according to the above method.

[0043] Formulation Example 11: 20% Profenofibrate·Cyprofloxacin Soluble Liquid 5g of propargyl sulfadiazine, 15g of cyclopropargyl flufenoxuron, 10g of dodecylphenol polyoxyethylene ether, 5g of propylene glycol phenyl ether sulfonate calcium, 25g of diisopropyl adipate, 5g of ethoxylated trisiloxane, and N-methylpyrrolidone to a final volume of 100g were prepared according to the above method.

[0044] Formulation Example 12: 40% Profenofibrate·Bromoxynil Dimethoate Soluble Liquid 2g of propargyl fluoride, 38g of bromoxynil dimethyl benzoate, 8g of dodecylphenol polyoxyethylene ether, 2g of propylene glycol phenyl ether sulfonate calcium, 10g of nonionic hydroxyl polyethylene oxide block copolymer, 10g of N,N-dimethyldecylamide, 5g of ethoxylated modified trisiloxane, and N-methylpyrrolidone to a final volume of 100g were prepared according to the above method.

[0045] Control agent 1: 12% propargite emulsifiable concentrate 12g of propofol, 8g of fatty alcohol polyoxyethylene ether, 8g of phenylethylphenol polyoxyethylene ether, 4g of propylene glycol phenyl ether sulfonate calcium, 2g of ethoxylated modified trisiloxane, and propylene glycol phenyl ether to be made up to 100g. An emulsifiable concentrate was prepared according to the above method.

[0046] Control agent 2: 8% polyflufenicol emulsion The following ingredients were prepared: 8g of polyfluorinated diamide, 8g of polyoxyethylene ether formaldehyde condensate sulfate, 2g of phenethylphenol polyoxyethylene ether, 4g of propylene glycol phenyl ether sulfonate calcium, 20g of ethylene glycol phenyl ether, 5g of glycerol, 0.2g of silicone oil, 2g of ethoxylated modified trisiloxane, and water to a final volume of 100g. A water-in-oil emulsion was prepared according to the above method.

[0047] Control agent 3: 13% cyprodinil microemulsion 13g of cyclopropaneflunomide, 20g of castor oil polyoxyethylene ether, 5g of propylene glycol phenyl ether sulfonate calcium, 30g of N,N-dimethyldecylamide, 15g of dipropylene glycol dimethyl ether, 3g of ethoxylated trisiloxane, and water to a final volume of 100g were added. A microemulsion was prepared according to the above method.

[0048] Control agent 4: 40% bromofenopram soluble liquid A soluble liquid was prepared by the following methods: 40g of bromoxynil dimethyl benzoyl diamide, 8g of dodecylphenol polyoxyethylene ether, 2g of propylene glycol phenyl ether sulfonate calcium, 10g of nonionic hydroxyl polyethylene oxide block copolymer, 10g of N,N-dimethyldecylamide, 5g of ethoxylated modified trisiloxane, and N-methylpyrrolidone to a final volume of 100g.

[0049] Control agent 5: 25% propiconazole·cyprodinil microemulsion (without penetrant) 5g of propargyl, 20g of cyprodinil, 0.8g of BHT, 10g of tricaprylic acid glyceride, 30g of N,N-dimethylacetamide, and water to a final volume of 100g were added. A microemulsion was prepared according to the above method.

[0050] Control agent 6: 1% propiconazole·polyfluorfenazate soluble liquid (without penetrant) 0.2g of propofol, 0.8g of polyfluorinated biamide, 10g of nonionic hydroxyl polyethylene oxide block copolymer, 2g of propylene glycol phenyl ether sulfonate calcium, and N-methylpyrrolidone to a final volume of 100g were prepared according to the above method.

[0051] Control agent 7: 0.5% dinotefuran soluble solution (commercially available) Control agent 8: 31% imidacloprid·high-efficiency cypermethrin suspension (commercially available) Verification Experiment 1: Co-toxicity coefficient of propofol and active ingredient B to bed bugs Test subject: Bed bugs (reared in the laboratory); Test method: In accordance with the guidelines for indoor bioassay of pesticides, Part 1: Contact activity test, the filter paper film method (NY / T 1154.8-2007) was used to test the activity of bed bugs.

[0052] Data statistics: The co-toxicity coefficient method was used to evaluate the activity of the combined drug and its counterpart against bedbugs. Then, the toxicity regression equation was calculated to obtain the LC50 value of each drug. Finally, the toxicity index and co-toxicity coefficient of the agents were calculated according to the Sun Yunpei method. A co-toxicity coefficient greater than 120 indicates a synergistic effect, a co-toxicity coefficient between 80 and 120 indicates an additive effect, and a co-toxicity coefficient less than 80 indicates an antagonistic effect. The test results are shown in the table below: Table 1. Determination of co-toxicity coefficients of propofol and cyprodinil (for bed bugs)

[0053] As shown in Table 1, when the ratio of propofol to cyprodinil is 1:20 to 20:1, the co-toxicity coefficient against bed bugs is greater than 120. In particular, when the ratio is 1:5 to 5:1, the co-toxicity coefficient exceeds 140, showing a significant synergistic effect.

[0054] Table 2. Determination of co-toxicity coefficients of propofol and bromfenoxam (for bed bugs)

[0055] As shown in Table 2, when the ratio of propiconazole to bromuconazole is 1:20 to 20:1, the co-toxicity coefficient against bed bugs is greater than 120. In particular, when the ratio is 1:5 to 5:1, the co-toxicity coefficient exceeds 140, showing a significant synergistic effect.

[0056] Table 3. Determination of co-toxicity coefficients of propofol and polyfluorinated diamide (for bed bugs)

[0057] As shown in Table 3, when the ratio of propofol to polyfluorinated diamide is 1:20 to 20:1, the co-toxicity coefficient against bed bugs is greater than 120. In particular, when the ratio is 1:5 to 5:1, the co-toxicity coefficient exceeds 140, showing a significant synergistic effect.

[0058] Verification Experiment 2: Bedbug Control Film Method Experiment Experimental subject: Bed bugs (laboratory-bred) Test method: Refer to the pesticide film method in GB / T26352-2010, "Test Method for Drug Resistance in Cockroaches - German Cockroach Bioassay". Test reagents: The active ingredients in formulations 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, and 12 were diluted with water to 300 ppm. Control reagents 1, 2, 3, 4, 7, and 8 were diluted with water to 300 ppm.

[0059] Data statistics: Table 4. Efficacy tests of formulation examples 1-12 against bed bugs.

[0060] As can be seen from Table 4, the KT of formulations 1-12 of the present invention against bedbugs 50 The values ​​were all less than 10 minutes, and the mortality rate exceeded 90% within 24 hours, while the control agents 1, 2, 3, 4, 7, and 8 showed lower KT values ​​against bedbugs. 50 The values ​​are all greater than 10 minutes, and the mortality rate is not greater than 90% within 24 hours. The formulation of this invention has a significant synergistic effect on the knockdown and lethality of bed bugs.

[0061] Verification Experiment 3: Effect of Penetrant on Drug Efficacy Experimental subject: Bed bugs (laboratory-bred) Test method: Refer to the pesticide film method in GB / T26352-2010, "Test Method for Drug Resistance in Cockroaches - German Cockroach Bioassay". Test reagents: In formulations 9 and 10, the active ingredients were diluted with water to 300 ppm, and in control reagents 5 and 6, the active ingredients were diluted with water to 300 ppm.

[0062] Data statistics: Table 5. Results of efficacy experiments of several treatments against bed bugs.

[0063] The experimental results show that the knockdown time and lethality of the drug with added penetrant are better than those of the drug without added penetrant.

[0064] All percentages in the formulations of this invention are by weight. The processing methods and techniques for each formulation are 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 this invention should be included within the scope of protection of this invention.

Claims

1. A complex composition for killing bed bugs, characterized by: The composition comprises active ingredient A and active ingredient B, wherein the weight ratio of active ingredient A to active ingredient B is 1:20 to 20:1; The active ingredient A is propofol; The active ingredient B is selected from any one of cyclopropionamide, brofenoxam, and polyflufenoxam.

2. The complexed chinch bug composition of claim 1, wherein: The weight ratio of active ingredient A to active ingredient B in the composition is 1:5 to 5:

1.

3. The application of the compound bedbug-killing composition according to claim 1, characterized in that: Application of the composition in the control of sanitary pests.

4. The application according to claim 3, characterized in that: The sanitary pest mentioned is the bedbug, and the application is limited to indoor locations.

5. A preparation for controlling sanitary pests, characterized in that: Contains the composition of claim 1.

6. The pest control preparation according to claim 5, characterized in that: The formulation comprises an active ingredient and excipients, wherein the active ingredient is the composition of claim 1, accounting for 1 to 60% of the formulation mass.

7. The pest control preparation according to claim 6, characterized in that: The auxiliary agent is one or more of the following: emulsifier, antifreeze, defoamer, solvent, penetrant, and water.

8. The pest control preparation according to claim 6, characterized in that: The auxiliary agent is a penetrant, or a penetrant combined with one or more emulsifiers, antifreeze agents, defoamers, solvents, and water.

9. The pest control preparation according to claim 6, characterized in that: The penetrant accounts for 1% to 5% of the formulation mass; the penetrant is ethoxylated trisiloxane.

10. The pest control preparation according to any one of claims 5-9, characterized in that: The sanitary pest in question is the bedbug.

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