Insecticide and acaricide composition and its application
By rationally compounding pesticides with different mechanisms of action, the problem of pest resistance is solved, the efficiency of pesticide use is improved, the cost is reduced, and the service life of the pesticide is extended.
Patent Information
- Application Number
- CN202411411679.3
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- Filing Date
- 2024-10-11
- Publication Date
- 2025-09-23
- Estimated Expiration
- 2044-10-11
AI Technical Summary
The existing technology has serious problems of pest resistance, low efficiency of pesticide use, and long-term use leads to increased risks to the environment and food safety.
An insecticidal and acaricidal composition is used, comprising active ingredient A and active ingredient B, wherein active ingredient A is a compound of formula I, and active ingredient B is bifenazate, chlorfenapyr, flonicamid or Flumetnicam. By rationally compounding pesticides with different mechanisms of action, the control effect on Acarina, Lepidoptera and Hemiptera pests is improved.
It significantly improves the efficiency of pesticide use, reduces the amount of pesticide used, reduces the cost of pesticide use, delays the development of pest resistance, and extends the service life of the pesticide.
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Figure CN119278949B_ABST
Abstract
Description
Technical Field
[0001] The invention belongs to the technical field of pesticide killing insects and acarids, and discloses an insect killing and acarid killing composition and application thereof. Background Art
[0002] Bifenazate, chemically known as isopropyl 3-(4-methoxybiphenyl-3-yl)hydrazinecarboxylate, is a carbazate acaricide. Developed by Chemtura Corporation in the United States, it entered the US market in 1999 for the control of mite pests on ornamental plants. Bifenazate has a broad spectrum of activity and a long-lasting effect, effective against pest mites such as spider mites (Tetranychus urticae), spider mites (Tetranychus viridis), and Panonychus urticae (Panonychus citri). As an inhibitor of complex III of the electron transport chain, it kills mites by blocking electron transfer. It exhibits no cross-resistance with existing commercial acaricides and is effective against phytophagous mites, making it suitable for the integrated control of pest mites.
[0003] Chlorfenapyr, a pyrrole insecticide and acaricide developed by the American Cyanamid Corporation, boasts a broad spectrum of insecticides, high efficacy, safety, and a long-lasting effect. It acts on the mitochondria within insect cells, disrupting the physiological process of oxidative phosphorylation, which converts adenosine diphosphate (ADP) to adenosine triphosphate (ATP). It effectively controls a variety of insect pests and mites, including the diamondback moth, beet armyworm, armyworm, thrips, and cabbage aphids. It is particularly effective against resistant pests and exhibits no cross-resistance with other insecticides.
[0004] Developed by Ishihara Sangyo Co., Ltd. of Japan, flonicamid is a pyridineamide insect growth regulator with a unique mechanism of action, particularly effective against piercing-sucking pests, demonstrating remarkable neurological effects and rapid antifeedant properties. Flunicamid has contact, stomach, systemic, and rapid antifeedant properties. Piercing-sucking pests that ingest plant sap containing flonicamid quickly cease feeding and eventually die of starvation, effectively preventing the spread of viral diseases.
[0005] Flumetnicam, CAS number: 158062-71-6, Chinese chemical name: 4-(trifluoromethyl)pyridine-3-carboxamide, is a nicotinamide insecticide. This compound is a metabolite of flonicamid and has insecticidal activity.
[0006] The compound of formula I belongs to the isoxazoline class of insecticides, with the CAS number 2892524-05-7. It is an allosteric modulator of γ-aminobutyric acid (GABA)-gated chloride channels, exhibiting a unique mechanism of action and lacking cross-resistance with other insecticides. This compound possesses stomach toxicity, contact toxicity, and some systemic activity, is highly fast-acting, and has an ovicidal effect. Its insecticidal spectrum covers a wide range of pests, including Lepidoptera, Coleoptera, Acarina (eggs, larvae, nymphs, and adults), Hemiptera (aphids), and Thysanoptera (thrips).
[0007] To address pest resistance, extend the effective use period of pesticides, and ensure agricultural product safety, pesticide combination strategies are crucial. Scientifically and rationally combining two or more pesticides with different mechanisms of action reduces the concentration of each individual pesticide while enhancing overall control effectiveness and interfering with the mechanisms that drive pest resistance. This approach has been proven to significantly improve control efficiency and reduce pesticide usage, making it a key component of current integrated pest management strategies. Summary of the Invention
[0008] To address the aforementioned problems in the prior art, the present invention provides an insecticide and acaricide composition. This insecticide and acaricide composition exhibits significant synergistic effects against Acarina, Lepidoptera, and Hemiptera pests, improving pesticide efficiency and reducing pesticide usage, thereby lowering pesticide costs for farmers. It is also environmentally friendly and food-safe.
[0009] In order to achieve the above object, the present invention adopts the following technical solution: an insecticide and acaricide composition, wherein the insecticide and acaricide composition comprises active ingredient A and active ingredient B, wherein the active ingredient A is a compound represented by formula I: (Formula I), the active ingredient B is any one of bifenazate, chlorfenapyr, flonicamid, and flumetnicam, and the mass ratio of the active ingredient A to the active ingredient B is 1:42 to 48:1, or any value within the above numerical range.
[0010] Furthermore, the active ingredient B is bifenazate, and the mass ratio of the compound of formula I to bifenazate is 1:24 to 48:1, or any value within the above numerical range;
[0011] The active ingredient B is chlorfenapyr, and the mass ratio of the compound of formula I to chlorfenapyr is 1:25 to 32:1, or any value within the above numerical range;
[0012] The active ingredient B is flonicamid, and the mass ratio of the compound of formula I to flonicamid is 1:20 to 25:1, or any value within the above numerical range;
[0013] The active ingredient B is flumetnicam, and the mass ratio of the compound of formula I to flumetnicam is 1:42 to 28:1, or any value within the above numerical range.
[0014] Furthermore, the active ingredient B is bifenazate, and the mass ratio of the compound of formula I to bifenazate is 1:24 to 32:1, or any value within the above numerical range;
[0015] The active ingredient B is chlorfenapyr, and the mass ratio of the compound of formula I to chlorfenapyr is 1:15 to 26:1, or any value within the above numerical range;
[0016] The active ingredient B is flonicamid, and the mass ratio of the compound of formula I to flonicamid is 1:15 to 20:1, or any value within the above numerical range;
[0017] The active ingredient B is flumetnicam, and the mass ratio of the compound of formula I to flumetnicam is 1:30 to 14:1, or any value within the above numerical range.
[0018] Furthermore, the active ingredient B is bifenazate, and the mass ratio of the compound of formula I to bifenazate is 1:12 to 32:1, or any value within the above numerical range;
[0019] The active ingredient B is chlorfenapyr, and the mass ratio of the compound of formula I to chlorfenapyr is 1:6 to 26:1, or any value within the above numerical range;
[0020] The active ingredient B is flonicamid, and the mass ratio of the compound of formula I to flonicamid is 1:15 to 10:1, or any value within the above numerical range;
[0021] The active ingredient B is flumetnicam, and the mass ratio of the compound of formula I to flumetnicam is 1:24 to 7:1, or any value within the above numerical range.
[0022] Furthermore, based on 100 wt% of the total weight of the composition, the total weight of the active ingredient A and the active ingredient B accounts for 0.01% to 80% of the total weight of the pesticide composition.
[0023] Furthermore, the insecticide and acaricide composition contains, in addition to the active ingredients, auxiliary ingredients permitted in pesticides, and the auxiliary ingredients are selected from one or more of wetting agents, dispersants, emulsifiers, thickeners, disintegrants, antifreeze agents, defoaming agents, solvents, preservatives, stabilizers, synergists or carriers.
[0024] Furthermore, the insecticide and acaricide composition is prepared into a formulation form permitted by pesticides, and the formulation form is a solid preparation or a liquid preparation.
[0025] Furthermore, the solid preparation includes powders, granules, pellets, tablets, strips, wettable powders, oil-dispersible powders, emulsion powders, water-dispersible granules, emulsion granules, water-dispersible tablets, soluble powders, soluble tablets or soluble granules;
[0026] The liquid preparations include soluble solutions, soluble gels, oils, film-spreading oils, emulsifiable concentrates, latexes, dispersible solutions, ointments, aqueous emulsions, oil emulsions, microemulsions, lipid suspensions, microcapsule suspensions, oil suspensions, dispersible oil suspensions, suspoemulsions, microcapsule suspension-suspension concentrates, microcapsule suspension-water emulsions, or microcapsule suspension-suspoemulsions;
[0027] Furthermore, the solid preparation is a wettable powder or a water-dispersible granule, and the liquid preparation is a suspension, an emulsifiable concentrate, a microemulsion, an aqueous emulsion, or a dispersible oil suspension.
[0028] The present invention also discloses the use of the insecticide and acaricide composition for preventing and controlling agricultural, forestry or gardening pests or mites.
[0029] Furthermore, the harmful mites are of the order Acarina, and the harmful insects are of the order Lepidoptera or Hemiptera.
[0030] The harmful mites are tea yellow mite, two-spotted spider mite, panonychus mite and cinnabarinus spider mite; the lepidopteran pests are Spodoptera litura, Spodoptera exigua and Plutella xylostella; and the hemiptera pests are aphids.
[0031] In order to obtain the desired insecticide effect, the dosage of the insecticide and acaricide composition varies depending on various factors, such as the crop to be protected, the type of pest, the degree of infection, climatic conditions, application site, application method, dosage form used, etc.
[0032] The beneficial effects of the present invention are as follows:
[0033] 1. The insecticide and acaricide composition of the present invention rationally combines compounds with different mechanisms of action, and has significant synergistic effects on different target pests and mites under appropriate ratios;
[0034] 2. The insecticide and acaricide composition of the present invention improves the efficiency of pesticide use, reduces the amount of pesticide used, and reduces the cost of pesticide use;
[0035] 3. The insecticide and acaricide composition of the present invention interferes with the development mechanism of pest resistance, delays the development of pest resistance to a certain extent, and prolongs the service life of the agent.
[0036] In order to make the technical solutions, objectives and advantages of the present invention more clearly understood, the present invention is described with reference to the following specific embodiments. However, the present invention can be implemented in various forms and should not be limited to the embodiments described herein.
[0037] Preparation Example
[0038] Preparation Example 1: 20% Formula I compound·bifenazate suspension (3:1)
[0039] Formula composition: 15% compound of formula I, 5% bifenazate, 3% fatty alcohol polyoxyethylene ether phosphate, 1% naphthalenesulfonate formaldehyde condensate, 3% alkyl aryl polyoxyethylene ether polyoxypropylene ether, 0.25% xanthan gum, 1% magnesium aluminum silicate, 5% ethylene glycol, 0.1% sodium benzoate, 0.5% silicone oil, and deionized water to make up the balance;
[0040] Preparation method: According to the formula ratio, the active ingredients, surfactants and other functional additives are placed in a reactor in sequence, water is added and mixed evenly, and the suspension product is obtained by high-speed shearing, wet sand grinding, and finally homogenization filtration.
[0041] Preparation Example 2: 21% Formula I compound·bifenazate water dispersible granules (6:1)
[0042] Formula composition: 18% compound of formula I, 3% bifenazate, 10% sodium salt of polycarboxylate, 5% polystyrene phenol polyoxyethylene ether sulfate, 3% BX powder, 6% sodium salt of lignin sulfonate, 10% ammonium sulfate, and kaolin makes up the balance;
[0043] Preparation method: According to the formula ratio, the active ingredient is added to the carrier, and surfactants and other functional additives are added thereto, mixed, and after air flow grinding, 10-25% water is added, and then kneading, granulation, drying, and screening are carried out to obtain a water-dispersible granule product; or the crushed powder is sprayed with water in a boiling granulator, granulated, dried, and then sieved to obtain the product.
[0044] Preparation Example 3: 35% Formula I compound·bifenazate wettable powder (1:6)
[0045] Formula composition: 5% compound of formula I, 30% bifenazate, 10% sodium salt of polycarboxylate, 6% sodium octylphenol polyoxyethylene ether sulfonate, 3% lakai powder BX, and kaolin to make up the balance;
[0046] Preparation method: According to the formula ratio, the active ingredients, dispersants, wetting agents and fillers are mixed, uniformly stirred in a stirring kettle, and pulverized and mixed uniformly multiple times in a jet mill to prepare the wettable powder of the composition of the present invention.
[0047] Preparation Example 4: 2.6% Formula I compound·Bifenazate emulsifiable concentrate (1:12)
[0048] Formula composition: 0.2% compound of formula I, 2.4% bifenazate, 10% EO / PO block copolymer, 10% acetophenone, 12% dimethyl sulfoxide, 10% cyclohexanone, 1% calcium dodecylbenzenesulfonate, and xylene makes up the balance;
[0049] Preparation method: according to the formula ratio, the active ingredient, solvent and cosolvent are added to the mixing kettle and stirred to dissolve, then the emulsifier is added and the balance is supplemented with the remaining solvent, and the mixture is stirred evenly in the stirring kettle. After filtering, the desired emulsifiable concentrate of the present invention is obtained.
[0050] Preparation Example 5: 30% Formula I compound·chlorfenapyr suspension (5:1)
[0051] Formula composition: 25% compound of formula I, 5% fenpyroximate, 3% styrylphenol polyoxyethylene ether phosphate, 5% polyoxyethylene sorbitan monooleate, 2% sodium lignin sulfonate, 0.25% xanthan gum, 1% magnesium aluminum silicate, 5% ethylene glycol, 0.1% sodium benzoate, 0.5% silicone oil, and deionized water to make up the balance;
[0052] Preparation method: Same as Preparation Example 1.
[0053] Preparation Example 6: 45% Formula I compound·chlorfenapyr water dispersible granules (1:2)
[0054] Formula composition: 15% compound of formula I, 30% chlorfenapyr, 6% sodium salt of polycarboxylate, 5% alkylnaphthalene formaldehyde condensate sulfonate, 10% sodium alkyl polyoxyethylene ether sulfonate, 2% sodium lauryl sulfate, 5% white carbon black, 25% starch, and kaolin makes up the balance;
[0055] Preparation method: Same as Preparation Example 2.
[0056] Preparation Example 7: 11% Formula I compound·chlorfenapyr wettable powder (10:1)
[0057] Formula composition: 10% compound of formula I, 1% chlorfenapyr, 3% tea saponin, 5% succinate sulfonate, 4% lakai powder BX, and kaolin to make up the balance;
[0058] Preparation method: Same as Preparation Example 3.
[0059] Preparation Example 8: 16% Formula I compound·chlorfenapyr emulsifiable concentrate (1:15)
[0060] Formula composition: 1% compound of formula I, 15% chlorfenapyr, 10% EO / PO block copolymer, 15% acetophenone, 10% N-methylpyrrolidone, 8% sorbitan polyoxyethylene ether, 3% calcium dodecylbenzenesulfonate, and xylene to make up the balance;
[0061] Preparation method: same as Preparation Example 4.
[0062] Preparation Example 9: 0.7% Formula I compound·chlorfenapyr aqueous emulsion (1:6)
[0063] Formula composition: 0.1% compound of formula I, 0.6% chlorfenapyr, 5% tristyrylphenol polyoxyethylene ether polyoxypropylene ether, 3% sodium octylphenol polyoxyethylene ether sulfonate, 20% cyclohexanone, 4% xylene, 0.2% xanthan gum, 5% glycerol, 0.1% sodium sorbate, and deionized water to make up the balance;
[0064] Preparation method: According to the formula ratio, the active ingredient is added together with the solvent, emulsifier, and cosolvent to dissolve into a uniform oil phase; water, antifreeze agent and other pesticide adjuvants are mixed together to form a uniform aqueous phase; while stirring at high speed in a reactor, the oil phase is added to the aqueous phase, and a shearing machine is turned on for high-speed shearing for about half an hour to form an oil-in-water emulsion.
[0065] Preparation Example 10: 1.9% Formula I Compound·Chlorfenapyr Microemulsion (18:1)
[0066] The formula comprises: 1.8% of a compound of formula I, 0.1% of chlorfenapyr, 12% of trimethylbenzene, 15% of cyclohexanone, 12% of Guerbet alcohol polyoxyethylene ether, 5% of EO-PO block copolymer, 1% of alkylphenol formaldehyde resin polyoxyethylene ether sulfate, 5% of glycerol, 0.05% of an organosilicon defoaming agent, and deionized water to make up the balance.
[0067] Preparation method: According to the formula ratio, the active ingredient solvent, emulsifier, etc. are mixed to prepare the oil phase, the antifreeze solution and water are mixed to prepare the aqueous phase, the oil phase is added to the aqueous phase under stirring and stirred evenly, and shearing is continued for 10 minutes. Then, a silicone oil defoamer is added and stirred evenly to obtain small droplets of oil phase particles with a diameter of 0.01 to 0.1 microns, thereby preparing the microemulsion described in the present invention.
[0068] Preparation Example 11: 22% Formula I compound·Flunic acid amide suspension (1:10)
[0069] Formula composition: 2% compound of formula I, 20% flonicamid, 2% phenylethylphenol polyoxyethylene polyoxypropylene ether, 3% sodium alkyl polyoxyethylene ether sulfonate, 5% styrenated phenol polyoxyethylene ether phosphate, 3% ethylene glycol oxyethylene polyoxypropylene ether, 0.25% xanthan gum, 1% magnesium aluminum silicate, 5% ethylene glycol, 0.1% sodium sorbate, 0.5% silicone oil, and deionized water to make up the balance;
[0070] Preparation method: Same as Preparation Example 1.
[0071] Preparation Example 12: 55% Formula I compound·Flunic acid amide water dispersible granules (10:1)
[0072] Formula composition: 50% compound of formula I, 5% flonicamid, 12% dispersant NNO, 4% succinate sulfonate, 3% sodium polycarboxylate, 2% sodium lignin sulfonate, 20% starch, and light calcium carbonate makes up the balance.
[0073] Preparation method: Same as Preparation Example 2.
[0074] Preparation Example 13: 48% Formula I compound·Flunic acid amide wettable powder (1:5)
[0075] Formula composition: 8% compound of formula I, 40% flonicamid, 3% naphthalenesulfonate formaldehyde condensate, 5% dispersant NNO, 7% sodium ligninsulfonate, 5% white sugar, 5% kaolin powder BX, and kaolin makes up the balance;
[0076] Preparation method: Same as Preparation Example 3.
[0077] Preparation Example 14: 21% Formula I compound·Flunic acid amide dispersible oil suspension (5:2)
[0078] Formula composition: 15% compound of formula I, 6% flonicamid, 2% sodium lauryl sulfate, 10% sorbitan oleate polyoxyethylene ether, 3% fatty alcohol polyoxyethylene ether, 2% calcium dodecylbenzenesulfonate, 1% silicon dioxide, 1% organic bentonite, 20% 200# solvent oil, and methyl oleate to make up the balance;
[0079] Preparation method: According to the formula ratio, the active ingredients, surfactants and other functional additives are placed in the reactor in sequence, oil is added and mixed evenly, and the dispersible oil suspension product is obtained by high-speed shearing, wet sand grinding, and finally homogenization filtration.
[0080] Preparation Example 15: 21% Formula I compound·flumetnicam suspension (1:6)
[0081] Formula composition: 3% compound of formula I, 18% flumetnicam, 1% sodium lauryl sulfate, 1% naphthalenesulfonate formaldehyde condensate, 4% tristyrylphenol ethoxylate phosphate, 0.25% xanthan gum, 1% magnesium aluminum silicate, 5% propylene glycol, 0.01% potassium benzisothiazolinone, 0.5% silicone oil, and deionized water to make up the balance;
[0082] Preparation method: Same as Preparation Example 1.
[0083] Preparation Example 16: 40% Formula I compound·flumetnicam water dispersible granules (7:1)
[0084] Formula composition: 35% compound of formula I, 5% flumetnicam, 12% lignin sulfonate, 5% succinate sulfonate, 3% sodium lauryl sulfate, 5% white carbon black, 25% starch, and kaolin makes up the balance;
[0085] Preparation method: same as Preparation Example 2.
[0086] Preparation Example 17: 33% Formula I compound·flumetnicam wettable powder (1:2)
[0087] Formula composition: 11% compound of formula I, 22% flonicamid, 4% sodium salt of polycarboxylate, 6% fatty alcohol polyoxyethylene ether sulfate, 7% sodium lignin sulfonate, 8% white sugar, 5% pulverized powder BX, and kaolin makes up the balance;
[0088] Preparation method: Same as Preparation Example 3.
[0089] Preparation Example 18: 13% Formula I compound·flumetnicam dispersible oil suspension (1:12)
[0090] Formula composition: 1% compound of formula I, 12% flumetnicam, 2% lignin sulfonate, 12% sorbitan oleate polyoxyethylene ether, 5% alkylphenol polyoxyethylene ether, 3% calcium dodecylbenzenesulfonate, 2% silicon dioxide, 1% organic bentonite, 18% 200# solvent oil, and methyl oleate to make up the balance;
[0091] Preparation method: According to the formula ratio, the active ingredients, surfactants and other functional additives are placed in the reactor in sequence, oil is added and mixed evenly, and the dispersible oil suspension product is obtained by high-speed shearing, wet sand grinding, and finally homogenization filtration.
[0092] Indoor biological activity test
[0093] Example 1: Indoor biological activity test of spider mite
[0094] Test reference: The test refers to NY / T 1154.12-2008 "Guidelines for Indoor Bioassay Tests of Pesticides - Insecticides Part 12: Spider Mite Slide Dipping Method".
[0095] Test target: adult two-spotted spider mites;
[0096] Test agents: technical drug of the compound of formula I, technical drug of bifenazate;
[0097] Preparation of pharmaceutical preparation: Dissolve the above raw drugs in a suitable solvent, and then dilute with 0.1% Tween-80 aqueous solution to prepare 5 series of mass concentration gradients.
[0098] Test method: Attach double-sided tape to one end of a glass slide, and stick the back of the test mite to the double-sided tape, 30 mites per glass slide, and place in an environment with a temperature of (26±1)℃ and a relative humidity of 60% to 80% for 4 hours. Examine with a dissecting microscope, remove dead and inactive individuals, and record the number of live mites. Then, immerse one end of the glass slide with mites in a drug solution of the corresponding concentration, immerse for 5 seconds, remove, and use filter paper to absorb excess drug solution on the mite and its surroundings. Place under the same breeding conditions for 3 days before examination. Touch the mite body lightly with a brush 5 times. Mites whose legs do not move are considered dead. Use clean water with an appropriate amount of Tween-80 aqueous solution as a control. When conducting toxicity determinations, repeat each concentration 4 times and calculate the median lethal concentration.
[0099] Calculation method:
[0100] Based on the survey data, calculate the mortality rate of each treatment. Calculate as follows:
[0101]
[0102] Where:
[0103] P——mortality rate, in percentage (%);
[0104] K——indicates the number of dead insects, the unit is head;
[0105] N——represents the total number of insects processed, in heads.
[0106]
[0107] Where:
[0108] P1——adjusted mortality rate, in percentage (%);
[0109] P t ——Treatment mortality rate, expressed in percentage (%);
[0110] P0 - blank control mortality rate, in percentage (%).
[0111] If the control mortality rate is less than 5%, no correction is required; if the control mortality rate is between 5% and 20%, correction should be made according to the correction mortality formula; if the control mortality rate is greater than 20%, the test needs to be repeated.
[0112] Analyze with statistical analysis system to obtain toxicity regression equation, correlation coefficient and LC 50 The activity of the test agent on the biological test material is evaluated by the value.
[0113] The co-toxicity coefficient (CTC value) of the mixture is calculated as follows:
[0114]
[0115] Where:
[0116] ATI - measured toxicity index of mixture;
[0117] S——LC of standard acaricide 50 , the unit is milligrams per liter (mg / L);
[0118] M——LC of the mixture 50 , the unit is milligrams per liter (mg / L).
[0119] TTI=TI A ×P A +TI B ×P B
[0120] Where:
[0121] TTI – Theoretical Toxicity Index of Mixtures;
[0122] TI A ——Agent toxicity index;
[0123] P A ——The percentage of agent A in the mixture, in percentage (%);
[0124] TI B ——Toxicity index of agent B;
[0125] P B ——The percentage of agent B in the mixture, in percentage (%).
[0126]
[0127] Where:
[0128] CTC – Co-toxicity coefficient;
[0129] ATI - measured toxicity index of mixture;
[0130] TTI - Theoretical Toxicity Index of Mixture.
[0131] A co-toxicity coefficient (CTC) of 120 or higher indicates a synergistic effect; a co-toxicity coefficient (CTC) of 80 or lower indicates an antagonistic effect; and a co-toxicity coefficient (CTC) of 80 or lower indicates an additive effect.
[0132] The indoor test results are shown in the table below:
[0133] Table 1 Results of indoor biological activity test on Tetranychus urticae by combining compound of formula I and bifenazate
[0134]
[0135]
[0136] Indoor test results showed that the compound of Formula I and bifenazate, when combined at an appropriate mass ratio, exhibited high activity against two-spotted spider mites. The co-toxicity coefficient against two-spotted spider mites was greater than 120 at a mass ratio of 1:24 to 48:1, indicating a synergistic effect. The co-toxicity coefficient against two-spotted spider mites was greater than 130 at a mass ratio of 1:24 to 32:1, demonstrating a significant synergistic effect. The co-toxicity coefficient against two-spotted spider mites was greater than 140 at a mass ratio of 1:12 to 32:1, demonstrating a significant synergistic effect.
[0137] Example 2: Indoor biological activity test on Spodoptera litura
[0138] Test basis: The test is based on NY / T 1154.14-2008 "Guidelines for Indoor Bioassay Tests of Pesticides - Insecticides Part 14: Leaf Dipping Method"
[0139] Test agents: technical drug of the compound of formula I and chlorfenapyr technical drug;
[0140] Test target: 3rd instar larvae of Spodoptera litura;
[0141] Preparation of pharmaceutical preparation: The above raw materials are prepared into mother liquor with organic solvent, and then 5 series of mass concentrations are prepared with 0.1% Tween-80 aqueous solution according to the method of equal proportion.
[0142] Chemical treatments: Select fresh, uniformly grown, untreated cabbage leaves and use a hole punch to create appropriate leaf discs. The discs are immersed in the test solution. After 10 seconds, they are removed, air-dried, and placed in a Petri dish containing 1% water agar. Test insects are then inoculated. Each treatment is replicated four times, with a treatment containing no chemical (including all organic solvents and emulsifiers) serving as a blank control. Each replicate contains 20 test insects.
[0143] Rearing and Observation: Treated insects were housed and observed at a temperature of (25 ± 1)°C, a humidity of 60% to 80%, and a photoperiod of L:D = (16:8) h. Mortality was checked 48 h after treatment, and the total number of insects and the number of dead insects were recorded.
[0144] Calculation method:
[0145] Based on the survey data, calculate the mortality rate of each treatment. Calculate as follows:
[0146]
[0147] Where:
[0148] P——mortality rate, in percentage (%);
[0149] K——indicates the number of dead insects, the unit is head;
[0150] N——represents the total number of insects processed, in heads.
[0151]
[0152] Where:
[0153] P1——adjusted mortality rate, in percentage (%);
[0154] P t ——Treatment mortality rate, expressed in percentage (%);
[0155] P0 - blank control mortality rate, in percentage (%).
[0156] If the control mortality rate is less than 5%, no correction is required; if the control mortality rate is between 5% and 20%, correction should be made according to the correction mortality formula; if the control mortality rate is greater than 20%, the test needs to be repeated.
[0157] Analyze with statistical analysis system to obtain toxicity regression equation, correlation coefficient and LC 50 The activity of the test agent on the biological test material is evaluated by the value.
[0158] The co-toxicity coefficient (CTC value) of the mixture is calculated as follows:
[0159]
[0160] Where:
[0161] ATI - measured toxicity index of mixture;
[0162] S——LC of standard pesticide 50 , the unit is milligrams per liter (mg / L);
[0163] M——LC of the mixture 50 , the unit is milligrams per liter (mg / L).
[0164] TTI=TI A ×P A +TI B ×P B
[0165] Where:
[0166] TTI – Theoretical Toxicity Index of Mixtures;
[0167] TI A ——Agent toxicity index;
[0168] P A ——The percentage of agent A in the mixture, in percentage (%);
[0169] TIB ——Toxicity index of agent B;
[0170] P B ——The percentage of agent B in the mixture, in percentage (%).
[0171]
[0172] Where:
[0173] CTC – Co-toxicity coefficient;
[0174] ATI - measured toxicity index of mixture;
[0175] TTI - Theoretical Toxicity Index of Mixture.
[0176] A co-toxicity coefficient (CTC) of 120 or higher indicates a synergistic effect; a co-toxicity coefficient (CTC) of 80 or lower indicates an antagonistic effect; and a co-toxicity coefficient (CTC) of 80 or lower indicates an additive effect.
[0177] The indoor test results are shown in the table below:
[0178] Table 2 Results of indoor biological activity test on Spodoptera litura with compound of formula I and chlorfenapyr
[0179]
[0180]
[0181] Indoor test results showed that the compound of Formula I and chlorfenapyr in an appropriate mass ratio exhibited good activity against Spodoptera litura. When the compound of Formula I and chlorfenapyr were mixed at a ratio of 1:25 to 32:1, the co-toxicity coefficient against Spodoptera litura was greater than 120, indicating a synergistic effect. When the mass ratio of the compound of Formula I to chlorfenapyr was 1:15 to 26:1, the co-toxicity coefficient against Spodoptera litura was greater than 140, indicating a significant synergistic effect. When the mass ratio of the compound of Formula I to chlorfenapyr was 1:6 to 26:1, the co-toxicity coefficient was greater than 150, indicating a significant synergistic effect.
[0182] Example 3: Indoor bioactivity test on melon aphid
[0183] Test basis: The test refers to the spray method recommended by the Agricultural Industry Standard of the People's Republic of China "Guidelines for Indoor Bioassay Tests of Pesticides" to evaluate the joint action mode.
[0184] Test target: 2nd instar nymphs of melon aphid.
[0185] Test method: Accurately weigh a certain amount of the compound of formula I, flonicamid, and flumetnicam technical into a volumetric flask, dissolve them in a suitable solvent, and then prepare five concentration gradients using a 0.1% Tween-80 aqueous solution in equal proportions.
[0186] Thirty aphids of uniform size were placed in a 9-cm-diameter Petri dish and sprayed with a 1-mL spray volume under a Potter spray tower. After the solution settled for 1 minute, the test insects were removed and reared normally in an incubator at a temperature of (26 ± 1)°C, a relative humidity of 60% to 80%, and a photoperiod of 16 h:8 h (light:dark). Four replicates were performed for each concentration. Twenty-four hours after treatment, the number of dead and live insects in each treatment was examined, and the corrected mortality rate for each treatment was calculated.
[0187] Calculation method:
[0188] Based on the survey data, calculate the mortality rate of each treatment. Calculate as follows:
[0189]
[0190] Where:
[0191] P——mortality rate, in percentage (%);
[0192] K——indicates the number of dead insects, the unit is head;
[0193] N——represents the total number of insects processed, in heads.
[0194]
[0195] Where:
[0196] P1——adjusted mortality rate, in percentage (%);
[0197] P t ——Treatment mortality rate, expressed in percentage (%);
[0198] P0 - blank control mortality rate, in percentage (%).
[0199] If the control mortality rate is less than 5%, no correction is required; if the control mortality rate is between 5% and 20%, correction should be made according to the correction mortality formula; if the control mortality rate is greater than 20%, the test needs to be repeated.
[0200] Analyze with statistical analysis system to obtain toxicity regression equation, correlation coefficient and LC 50 The activity of the test agent on the biological test material is evaluated by the value.
[0201] The co-toxicity coefficient (CTC value) of the mixture is calculated as follows:
[0202]
[0203] Where:
[0204] ATI - measured toxicity index of mixture;
[0205] S——LC of standard pesticide 50 , the unit is milligrams per liter (mg / L);
[0206] M——LC of the mixture 50 , the unit is milligrams per liter (mg / L).
[0207] TTI=TI A ×P A +TI B ×P B
[0208] Where:
[0209] TTI – Theoretical Toxicity Index of Mixtures;
[0210] TI A ——Agent toxicity index;
[0211] P A ——The percentage of agent A in the mixture, in percentage (%);
[0212] TI B ——Toxicity index of agent B;
[0213] P B ——The percentage of agent B in the mixture, in percentage (%).
[0214]
[0215] Where:
[0216] CTC – Co-toxicity coefficient;
[0217] ATI - measured toxicity index of mixture;
[0218] TTI - Theoretical Toxicity Index of Mixture.
[0219] A co-toxicity coefficient (CTC) of 120 or higher indicates a synergistic effect; a co-toxicity coefficient (CTC) of 80 or lower indicates an antagonistic effect; and a co-toxicity coefficient (CTC) of 80 or lower indicates an additive effect.
[0220] The indoor test results are shown in the table below:
[0221] Table 3 Results of indoor bioassay on melon aphids with the compound of formula I and flonicamid
[0222]
[0223] Laboratory test results showed that the compound of Formula I combined with flonicamid exhibited high activity against melon aphids at appropriate mass ratios. When the mass ratio of the compound of Formula I to flonicamid was 1:20-25:1, the co-toxicity coefficient was greater than 120, indicating a synergistic effect. When the mass ratio of the compound of Formula I to flonicamid was 1:15-20:1, the co-toxicity coefficient was greater than 130, demonstrating a significant synergistic effect. When the mass ratio of the compound of Formula I to flonicamid was 1:15-10:1, the co-toxicity coefficient was greater than 140, demonstrating a significant synergistic effect.
[0224] Table 4 Results of indoor bioassay on melon aphids using the compound of formula I and flumetnicam
[0225]
[0226] Laboratory test results showed that the compound of Formula I combined with flumetnicam in appropriate mass ratios exhibited high bioactivity against melon aphids. The mass ratios of Formula I to flumetnicam ranged from 1:42 to 28:1, resulting in a co-toxicity coefficient exceeding 120, demonstrating a synergistic effect. The mass ratios of Formula I to flumetnicam ranged from 1:30 to 14:1, resulting in a co-toxicity coefficient exceeding 130, demonstrating a significant synergistic effect. The mass ratios of Formula I to flumetnicam ranged from 1:24 to 7:1, resulting in a co-toxicity coefficient exceeding 140, demonstrating a significant synergistic effect.
[0227] Field efficacy trials
[0228] Example 4: Field efficacy test for controlling strawberry two-spotted spider mite
[0229] The experimental site is the strawberry greenhouse in Xinggongshan Village, Dongpu Town, Shaoxing City, Zhejiang Province. The soil in the experimental plot is loess with a pH value of 6-7 and an organic matter content of more than 3%, which is suitable for the growth of strawberries.
[0230] Experimental crop: Strawberry (Akihime).
[0231] Test subject: Tetranychus urticae.
[0232] Experimental design: The plots were arranged in random blocks, and each plot was determined to be 24m2. 2 , set up 4 repeated statistics. In order to prevent the drugs from interfering with each other, set up protection rows between the plots.
[0233] Test method: The test was carried out at the early stage of the strawberry two-spotted spider mite. The application method was strictly determined by one staff member using a 3WBD-16B backpack electric sprayer to spray evenly, with a spray volume of 50kg / 667m 2 .
[0234] Survey method: Random sampling was performed at five locations, with five leaves fixed at each location, for a total of 25 leaves. The mite population was checked before application, and the number of live mites was checked 3 and 10 days after application.
[0235] Calculation method of drug efficacy:
[0236]
[0237] The results of the field efficacy test are shown in the table below:
[0238] Table 5 Results of field trials on the efficacy of pesticides against two-spotted spider mites in strawberries
[0239]
[0240] 21% Formula I compound + bifenazate water-dispersible granules (6:1) and 20% Formula I compound + bifenazate suspension concentrate (3:1) demonstrated excellent control against strawberry spider mites. Three days after application, the combined formulations achieved control efficacies of 86.54% and 88.69%, significantly higher than those achieved with 43% bifenazate suspension concentrate and 30% Formula I compound water-dispersible granules. Ten days after application, the control efficacies of 21% Formula I compound + bifenazate water-dispersible granules (6:1) and 20% Formula I compound + bifenazate suspension concentrate (3:1) continued to increase, reaching 89.07% and 91.81%, respectively. No phytotoxicity was observed on strawberry leaves or fruit at the test doses during the trial.
[0241] Example 5: Field efficacy test for controlling cabbage armyworm and beet armyworm
[0242] The test site is the cabbage field in Lingbei Village, Gujing Town, Xinhui District, Jiangmen City, Guangdong Province. The land in the test plot is flat and easy to irrigate, so the water and fertilizer management in each plot is uniform.
[0243] Experimental crop: Cabbage (Jingfeng No. 1).
[0244] Test insects: Spodoptera litura, Spodoptera exigua.
[0245] Experimental design: The experiment set up 5 treatments, including 4 chemical treatments and 1 water control. The experimental plots were arranged in random blocks, with 4 replicates for each treatment and an area of 25m 2 .
[0246] Test method: During the test, cabbage was in the rosette stage, and the young larvae of beet armyworm and Spodoptera litura were in full bloom. The Changjiang-10A backpack sprayer was used for spraying at a rate of 750 kg / hm2. 2 Before application and 3 and 7 days after application, a 5-point sampling method was used, with 2 plants at each point. The number of live larvae on the leaves of the entire plant was observed, and the control effect of each treatment area was calculated based on the insect population reduction rate.
[0247] Calculation method of drug efficacy:
[0248]
[0249] The results of the field efficacy test are shown in the following table:
[0250] Table 6 Results of field efficacy tests on cabbage armyworm and beet armyworm
[0251]
[0252] As shown in Table 6, 3 days after spraying, the 30% formula I compound·chlorfenapyr suspension concentrate (5:1) and the 11% formula I compound·chlorfenapyr wettable powder (10:1) at 45 g / hm2 2 The control effects of the two doses were 91.49% and 89.98% respectively, while the control agents 30% chlorfenapyr suspension concentrate and 30% water dispersible granules of the compound of formula I were 91.49% and 89.98% respectively at 67.5 and 90 g / hm2. 2 The control effect under the dosage was 71.31% and 69.72% respectively; 7 days after spraying, 30% formula I compound·chlorfenapyr suspension concentrate (5:1) and 11% formula I compound·chlorfenapyr wettable powder (10:1) at 45g / hm 2 The control effects of the two doses were 94.78% and 92.94% respectively, while the control agents 30% chlorfenapyr suspension concentrate and 30% water dispersible granules of the compound of formula I at 67.5 and 90 g / hm 2 The control effect under the dose was 75.58% and 73.67%
[0253] During the test, the various treatment agents showed no phytotoxicity to cabbage at the test doses, had little impact on the natural enemies of pests, and had a concurrent preventive effect on Spodoptera litura, Spodoptera exigua, Pieris rapae, and Plutella xylostella in the test plots.
[0254] Example 6: Field efficacy test for controlling cucumber aphids
[0255] The experimental site was a cucumber greenhouse in Xiaohongqiao Village, Shatou Town, Guangling District, Yangzhou City. The soil in the experimental site was clay soil with medium soil fertility.
[0256] Experimental crop: cucumber (Jinyou 401).
[0257] Experimental design: The experiment has 8 treatments, each with 4 replicates, a total of 32 plots, and a plot area of 20m 2 , randomized block arrangement.
[0258] Test method: Spray the cucumbers when they are in the fruiting period and melon aphids are at their peak. Use a Singapore Linong manual sprayer to spray at normal pressure, spraying evenly on the front and back of the upper and lower leaves of the cucumbers.
[0259] Survey Method: Aphid counts were conducted once before spraying, and live aphid counts were conducted 1, 3, and 7 days after spraying. Five random sampling points were selected from each plot, with two plants and five leaves per plant surveyed at each point. A total of 50 leaves were surveyed per plot.
[0260] The formula for calculating the prevention effect is as follows:
[0261]
[0262] The results of the field efficacy test are shown in the following table:
[0263] Table 7 Results of field efficacy test on cucumber aphids
[0264]
[0265] As shown in Table 7, the compound of Formula I combined with flonicamid and flumetnicam exhibited significant control efficacy against cucumber aphids. The control efficacy of the combined formulations ranged from 84.22% to 88.38% one day after application and from 87.51% to 91.44% three days after application. Both combined formulations demonstrated superior control efficacy compared to the control.
[0266] In summary, through indoor toxicity assays and field efficacy tests, it can be seen that the composition of the present invention has a good control effect on pests or mites, is safe for target crops, has significant control effects, and is superior to a single agent in delaying the development of resistance and prolonging the effect.
[0267] Although the present application describes specific embodiments in detail by way of example, the disclosure of the present application may adopt various modifications and alternative forms. However, it should be understood that the disclosure of the present application is not limited to the specific forms disclosed. On the contrary, the disclosure of the present application covers all modifications, equivalents and alternative forms within the scope of the disclosure of the present application, and the scope of the present application is limited by the appended claims and their legal equivalents.
Claims
1. An insecticide and acaricide composition, characterized in that: The insecticide and acaricide composition comprises active ingredient A and active ingredient B, wherein the active ingredient A is a compound represented by formula I: (Formula I), The active ingredient B is any one of bifenazate, chlorfenapyr, flonicamid, and flumetnicam; The mass ratio of the compound of formula I to bifenazate is 1:24 to 48:1; The mass ratio of the compound of formula I to chlorfenapyr is 1:25 to 32:1; The mass ratio of the compound of formula I to flonicamid is 1:20 to 25:1; The mass ratio of the compound of formula I to flumetnicam is 1:42~28:
1.
2. The insecticide and acaricide composition according to claim 1, characterized in that: The mass ratio of the compound of formula I to bifenazate is 1:24 to 32:1; The mass ratio of the compound of formula I to chlorfenapyr is 1:15 to 26:1; The mass ratio of the compound of formula I to flonicamid is 1:15 to 20:1; The mass ratio of the compound of formula I to flumetnicam is 1:30 to 14:
1.
3. The insecticide and acaricide composition according to claim 1, characterized in that: The mass ratio of the compound of formula I to bifenazate is 1:12 to 32:1; The mass ratio of the compound of formula I to chlorfenapyr is 1:6 to 26:1; The mass ratio of the compound of formula I to flonicamid is 1:15 to 10:1; The mass ratio of the compound of formula I to flumetnicam is 1:24 to 7:
1.
4. The insecticide and acaricide composition according to claim 1, characterized in that: The total weight of the insecticide and acaricide composition is 100 wt %, and the total weight of the active ingredient A and the active ingredient B accounts for 0.01% to 80% of the total weight of the insecticide and acaricide composition.
5. The insecticide and acaricide composition according to claim 1, characterized in that: The insecticide and acaricide composition contains, in addition to the active ingredients, auxiliary ingredients permitted in pesticides, wherein the auxiliary ingredients are selected from one or more of wetting agents, dispersants, emulsifiers, thickeners, disintegrants, antifreeze agents, defoaming agents, solvents, preservatives, stabilizers, synergists or carriers.
6. The insecticide and acaricide composition according to claim 1, characterized in that: The insecticide and acaricide composition is prepared into a formulation form permitted by pesticides, and the formulation form is a solid preparation or a liquid preparation.
7. The insecticide and acaricide composition according to claim 6, characterized in that: The solid preparations are wettable powders and water-dispersible granules, and the liquid preparations are suspensions, emulsifiable concentrates, microemulsions, aqueous emulsions, and dispersible oil suspensions.
8. Use of the insecticide and acaricide composition according to any one of claims 1 to 7 for controlling agricultural, forestry or gardening pests or mites.
9. The use according to claim 8, characterized in that The harmful mites are of the order Acarina, and the harmful insects are of the order Lepidoptera or Hemiptera. The harmful mites are tea yellow mite, two-spotted spider mite, panonychus mite and cinnabarinus spider mite; the lepidopteran pests are Spodoptera litura, Spodoptera exigua and Plutella xylostella; and the hemiptera pests are aphids.
Citation Information
Patent Citations
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