Insecticidal and acaricidal composition
By mixing sodium channel modulators and voltage-dependent sodium channel blockers in a specific proportion to form an insecticide and acaricide composition, the problems of pest resistance and insufficient effectiveness of existing mixtures are solved, efficient and low-dose pest control is achieved, and environmental pollution and costs are reduced.
Patent Information
- Application Number
- CN202510386010.1
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Priority Date
- 2024-04-01
- Filing Date
- 2025-03-30
- Publication Date
- 2025-10-14
AI Technical Summary
Existing insecticides and acaricides with a single active ingredient are prone to causing pest resistance during long-term use, and it is difficult to predict synergistic effects when selecting components for existing mixtures.
Active component A and active component B are mixed in a specific ratio, wherein component A is selected from sodium channel modulator compounds and component B is selected from voltage-dependent sodium channel blocker compounds, to prepare an insecticidal and acaricidal composition, which is then mixed with a carrier and an adjuvant to form a variety of dosage forms for controlling agricultural and urban pests.
Delay the development of pest resistance, improve control effects, reduce dosage, reduce environmental pollution, achieve synergistic effects, and reduce costs.
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Figure CN120770401A_ABST
Abstract
Description
Technical Field
[0001] The invention belongs to the field of insecticides and acaricides, and relates to an insecticide and acaricide composition. Background Art
[0002] In crop production, such as agriculture and horticulture, damage caused by pests and diseases remains significant. Due to biodiversity and the simultaneous occurrence of multiple pests and diseases, the field of plant protection has long demanded the development of new insecticides and acaricides with improved activity, lower dosages, and improved environmental friendliness. Insecticides and acaricides containing a single active ingredient, when used continuously for pest control, can easily lead to the development of resistance in pests. Mixing insecticides and acaricides containing two or more active ingredients into a blend plays an important role in expanding the insecticide spectrum, combating both pests and diseases, controlling vector insects to manage viral diseases, and reducing farmers' application costs. It can also delay the development of pest resistance. Although mixtures can delay resistance, the use of two substances alone is not always predictable. Summary of the Invention
[0003] In view of the shortcomings of the existing technology, the present invention aims to provide an insecticide and pest control composition to meet the demand for increasingly improved and updated insecticides and pest control agents in the fields of agriculture, forestry and urban sanitation.
[0004] To achieve the above object, the technical solution adopted by the present invention is:
[0005] An insecticide and acaricide composition, comprising an active component A and an active component B, wherein the weight ratio of active component A to active component B is 1:99 to 99:1; active component B is selected from sodium channel modulators or voltage-dependent sodium channel blockers; and active component A is selected from compound I or a stereoisomer thereof, wherein compound I has the following structure:
[0006]
[0007] In some embodiments, the sodium channel modulator is selected from cypermethrin, lambda-cyhalothrin, fenpropathrin, fenvalerate, flucythrinate, flumethrin, beta-cyfluthrin, cyfluthrin, bifenthrin, deltamethrin, acrinathrin, cis-cypermethrin, alpha-cypermethrin), bifenthrin, cyhalothrin, permethrin, fluvalinate, allethrin, bioallethrin, cycloprothrin, gamma-cyhalothrin, theta-cypermethrin, zeta-cypermethrin, cyphe nothrin), empenthrin, esfenvalerate, imiprothrin, meperfluthrin, metofluthrin, dimefluthrin, prallethrin, phenothrin, resmethrin, bioresmethrin, cismethrin, tefluthrin, tetramethrin amethrin), tetramethylfluthrin, tralomethrin, beta-cypermethrin, ethofenprox, transfluthrin, esdépalléthrine, barthrin, bioethanomethrin, brofenvalerate, brofluthrinate, bromethrin, butethrin,Chlorempenthrin, cyclethrin, cyhalothrin, lambda-cyhalothrin, dimethrin, d-fanshiluquebingjuzhi, fenfluthrin, fenpirithrin, esfenvalerate, furamethrin, imiprothrin, japothrins, kadethrin, methotrexate, pentmethrin, biopermethrin, methyl proparthrin, resmethrin, terallethrin, tralocythrin, valerate, flufenprox, halfenprox, sulfoxime, thiofluoximate, flumethrin, furethrin, heptafluthrin, momfluorothrin, transpermethrin, profluthrin, pyresmethrin, protrifenbute, silafluofen, DDT or methoxychlor;
[0008] In some exemplary embodiments, the sodium channel modulators are selected from cypermethrin.
[0009] In some embodiments, the voltage-dependent sodium channel blocker is selected from indoxacarb or metaflumizone.
[0010] In some typical embodiments, the voltage-dependent sodium channel blockers are selected from indoxacarb.
[0011] In some embodiments, the active component A is compound I, and the active component B is selected from cypermethrin; the weight ratio of the two active components is 30:1-1:30.
[0012] In some embodiments, the active component A is compound I, and the active component B is selected from indoxacarb; the weight ratio of the two active components is 30:1-1:30.
[0013] Furthermore, the composition is mixed with a carrier and any auxiliary agent to prepare a preparation containing the composition. The cumulative content of the active ingredient of the composition in the preparation is between 0.5wt% and 95wt%. Preferably, the cumulative content of the active ingredient in the preparation is between 1% and 85%.
[0014] The carrier of the present invention may be solid or liquid, and any carrier commonly used in formulating pesticide compositions can be used.
[0015] Suitable solid carriers include: minerals, plants, synthetic fillers and inorganic salts. Minerals include silicates, carbonates, sulfates and oxides. Silicates include kaolin, sepiolite, pearl clay, montmorillonite, mica, vermiculite, pyrophyllite and talc. Carbonates include calcium carbonate and dolomite. Sulfates include ammonium sulfate, sodium sulfate and calcium sulfate. Oxides include quicklime, magnesium lime and diatomaceous earth. Plants include citrus pulp, corn cob cobs, husk powder, rice husk, soybean straw powder, tobacco powder, walnut shells and sawdust. Synthetic fillers include precipitated calcium carbonate hydrate, precipitated calcium carbonate and white carbon black. Inorganic salts include potassium chloride and sodium chloride.
[0016] Liquid carriers include water and organic solvents. When the active ingredient is in the form of a suspensoid, the organic solvent serves as a solubilizer and antifreeze agent. Suitable organic solvents include aromatic hydrocarbons such as benzene, xylene, toluene, alkylbenzenes, alkylnaphthalenes, and chlorinated aromatic hydrocarbons; chlorinated aliphatic hydrocarbons such as vinyl chloride, chloroform, dichloromethane, chloroform, carbon tetrachloride, and polychlorinated ethanes; aliphatic hydrocarbons such as petroleum fractions, cyclohexane, light mineral oil, and paraffin; alcohols such as methanol, ethanol, isopropanol, butanol, isobutanol, ethylene glycol, propylene glycol, glycerol, and fatty alcohols; ethers such as methyl glycol ether, ethyl glycol ether, and petroleum ether; ketones such as acetone, methyl ethyl ketone, methyl isobutyl ketone, cyclohexanone, isophorone, and N-methyl-pyrrolidone; specialty solvents such as dimethylformamide, dimethyl sulfoxide, polyethylene glycol, and capronitrile; and vegetable oils and methylated vegetable oils. The above organic solvents can be used alone, as a mixture, or mixed with water.
[0017] The auxiliary agent of the present invention may include one or more of a surfactant, a defoaming agent, a thickener, a suspending agent and an antifreeze agent as needed, and may also include other auxiliary agents commonly used in the industry as needed.
[0018] Surfactants can be emulsifiers, dispersants, stabilizers or wetting agents; they can be ionic or nonionic. Suitable surfactants include: sodium and calcium salts of polyacrylic acid and lignin sulfonic acid; condensation products of fatty acids or fatty amines containing at least 12 carbon atoms with ethylene oxide and / or propylene oxide; fatty acid esters of glycerol, lauryl alcohol-1, tetradecanol-1, sorbitol, sucrose or pentaerythritol; and condensation products thereof with ethylene oxide and / or propylene oxide; sulfates or sulfonates of their condensation products; alkali metal or alkaline earth metal salts of sulfuric acid or sulfonic acid containing at least 10 carbon atoms in the molecule, preferably sodium salts, such as sodium lauryl sulfate, sodium secondary alkyl sulfate, sodium salt of sulfonated castor oil, sodium alkylaryl sulfonate and sodium dodecylbenzene sulfonate; polymers of ethylene oxide, and copolymers of ethylene oxide and propylene oxide.
[0019] Emulsifiers include nonionic emulsifiers and anionic emulsifiers. Nonionic emulsifiers are preferably nonylphenol polyoxyethylene ether, fatty alcohol polyoxyethylene ether, styrylphenyl polyoxyethylene ether, alkylphenol formaldehyde resin polyoxyethylene ether, terminal hydroxy polyoxyethylene polyoxypropylene ether, styrylphenol formaldehyde resin polyoxyethylene polyoxypropylene ether, and castor oil polyoxyethylene ether. Anionic emulsifiers mainly include calcium dodecylbenzene sulfonate, triphenyl ethyl phenol polyoxyethylene ether phosphate amine salt, nonylphenol polyoxyethylene ether phosphate amine salt, and castor oil polyoxyethylene ether phosphate amine salt.
[0020] The dispersant of the present invention comprises one or more of: sodium salt of acrylic acid homopolymer, disodium salt of maleic acid, sodium salt of naphthalenesulfonic acid formaldehyde condensate, rosin block polyoxyethylene ether polyoxypropylene ether sulfonate, hydroxyl-terminated polyoxyethylene polyoxypropylene ether block copolymer, triphenyl phenol polyoxyethylene ether phosphate, fatty alcohol polyoxyethylene ether phosphate, and sodium salt of p-hydroxyphenyl lignin sulfonate.
[0021] The wetting agent of the present invention comprises one or a combination of two or more of fatty alcohol polyoxyethylene ether, naphthalene sulfonate, sodium lauryl sulfate and alkylphenol resin polyoxyethylene ether sulfate.
[0022] The thickener of the present invention comprises one or more of xanthan gum, magnesium aluminum silicate, sodium alginate, sodium carboxymethyl cellulose, gum arabic, gelatin and polyvinyl alcohol.
[0023] The defoaming agent of the present invention includes foaming agents, silicones, C8-10 fatty alcohols, C10-20 saturated fatty acids and amides.
[0024] The fungicide and insecticide of the present invention can be formulated into any dosage form permitted in agriculture as needed, such as powdery preparations, granular preparations, dispersible powdery preparations, dispersible granular preparations, dispersible sheet preparations, soluble solid preparations, soluble liquid preparations, oil preparations, ultra-low volume preparations, dispersible liquid preparations, emulsion preparations, suspension preparations, suspoemulsions or seed coating preparations.
[0025] The invention discloses an application of an insecticide and acaricide composition, and an application of the composition in preparing an insecticide and acaricide for controlling agricultural pests or urban health pests.
[0026] The agricultural pests include armyworms, beet armyworms, cotton bollworms, cutworms, cabbage armyworms, apple leafrollers, rice leafrollers, corn borers, striped stem borers, diamondback moths, cabbage worms, gypsy moths, East Asian migratory locusts, underground pests, leafminers, leafminers, aphids, leafhoppers, flower scale insects, potato beetles, flea beetles, thrips, blind bugs, cinnabar spider mites, hawthorn spider mites, citrus rust mites, apple spider mites, two-spotted spider mites, gall mites, flour mites, etc., and urban pests include termites, cockroaches, ants, flies, mosquitoes, etc. When used to control agricultural pests, it can be applied to fruit trees, cereals, beans, vegetables, and flowers. It can be used on fruit trees such as apples, pears, citrus, and lychees; cereals such as wheat and rice; beans such as soybeans and kidney beans; cotton; and vegetables such as cabbage, cauliflower, Chinese cabbage, rapeseed, tomatoes, and peppers. When used to control urban pests, it can be used in homes, public places, offices, and on trees and dams infested with termites.
[0027] Furthermore, the present invention provides a method for using the insecticide and acaricide composition, wherein the prepared insecticide and acaricide is applied to the pests to be controlled or the medium in which they grow, in an effective dose. A generally suitable effective dose is 10 to 500 grams per hectare, and a preferred effective dose is 15 to 100 grams per hectare.
[0028] The beneficial effects of the present invention are as follows: 1. The present invention adopts compounds with different mechanisms of action in insecticide and acaricide, which are mixed in a specific proportion and work in coordination with each other. The pest control can delay the occurrence of pest resistance and improve the control effect on resistant populations. It shows obvious synergistic effect in insecticide and acaricide, and improves the control effect of single active ingredient compounds in the composition on pests. At the same time, the synergistic effect of the combination of the present invention is not linearly related to that of a single agent.
[0029] 2. The dosage of the composition of the present invention in killing insects and acarids is significantly lower than the dosage of a single compound in the composition, thereby reducing the cost of use and reducing environmental pollution. DETAILED DESCRIPTION
[0030] The following examples may enable those skilled in the art to more fully understand the present invention, but the present invention is not limited to the scope of the examples.
[0031] Indoor biological activity assay
[0032] Example 1 Determination of the synergistic effect of a composition containing Compound I on second-instar larvae of Plutella xylostella
[0033] Test subjects: Second-instar larvae of the diamondback moth, a sensitive strain reared indoors.
[0034] Test conditions: temperature: 24-26°C, relative humidity: 60%, light intensity: L:D = 14:10.
[0035] Preparation of drug solution: According to different experimental requirements, the test samples (compositions of different ratios of the present invention and the original drug) were accurately weighed using an electronic analytical balance. The original drug was dissolved in acetone and then diluted with 0.1% Tween 80 water to a drug solution of a certain concentration according to the experimental design dosage.
[0036] Experimental method: Select fresh cabbage leaves grown in the greenhouse, use a hole punch to cut the cabbage leaves into round leaflets with a diameter of 3 cm, put them into the prepared solution and immerse them for 10 seconds. After natural drying in the shade, place them in a culture dish with a diameter of 9 cm with filter paper, and inoculate neatly with healthy test insects. Each treatment has 20-25 heads, and each treatment is repeated 4 times. A blank control is also set up.
[0037] Based on the concept of toxicity combination proposed by Bliss, the theoretical mortality rate P when insecticides and acaricides are mixed can be calculated using the following formula:
[0038] P=P m +P n (1-P m )
[0039] P m is the target mortality rate (%) when the concentration of the first active component is m; P n The target mortality rate (%) when the second active ingredient is used at a concentration of n.
[0040] If the actual mortality rate of the target after the two active components are mixed at a certain concentration is greater than the theoretical mortality rate P, then it is determined that the two active components have a synergistic effect when mixed at the set concentration, otherwise it is an antagonistic effect.
[0041] The results are shown in Table 1.
[0042] Table 1 Synergistic effect of compound I mixed with cypermethrin and other two pesticides on diamondback moth larvae
[0043]
[0044]
[0045] Example 2 Determination of the synergistic effect of the composition containing compound I on Tetranychus cinnabarinus
[0046] Test subjects: Tetranychus cinnabarinus, adult mites, sensitive strain raised indoors.
[0047] Test conditions: temperature: 24-26°C, relative humidity: 60%, light intensity: L:D = 14:10.
[0048] Preparation of drug solution: According to different experimental requirements, the test samples (compositions of different ratios of the present invention and the original drug) were accurately weighed using an electronic analytical balance. The original drug was dissolved in acetone and then diluted with 0.1% Tween 80 water to a drug solution of a certain concentration according to the experimental design dosage.
[0049] Test Method: Activity against adult Tetranychus cinnabarinus mites was determined using a potted seedling spray method. First, 40-60 uniformly sized adult Tetranychus cinnabarinus mites were placed on bean seedlings at the stage of first pair of true leaves (leaving one true leaf intact). After the adult mites stabilized, the population was counted. The test materials were then treated with the solution using the airbrush method, applying 1.5 mL per plant. A blank control was established.
[0050] After natural air drying, the treated specimens were placed in an observation room where the temperature, humidity, and lighting were adjusted as needed. After 72 hours, the number of live mites was counted and the mortality rate was calculated. The evaluation was conducted using the Bliss method, a classic method for evaluating the effects of mixed agents. Based on his concept of toxicity, Bliss proposed that the theoretical mortality rate (P) of mixed insecticides and acaricides can be calculated using the following formula:
[0051] P=P m +P n (1-P m )
[0052] P m is the target mortality rate (%) when the concentration of the first active component is m; P n The target mortality rate (%) when the second active ingredient is used at a concentration of n.
[0053] If the actual mortality rate of the target after the two active components are mixed at a certain concentration is greater than the theoretical mortality rate P, then it is determined that the two active components have a synergistic effect when mixed at the set concentration, otherwise it is an antagonistic effect.
[0054] The results are shown in Table 1.
[0055] Table 2 Synergistic effect of compound I mixed with cypermethrin and other two agents on adult Tetranychus cinnabarinus
[0056]
[0057]
Claims
1. An insecticide and acaricide composition comprising an active component A and an active component B, wherein the weight ratio of active component A to active component B is 1:99 to 99:1; active component B is selected from a sodium channel modulator or a voltage-dependent sodium channel blocker; and active component A is selected from compound I or a stereoisomer thereof, wherein compound I has the following structure:
2. The insecticide and acaricide composition according to claim 1, characterized in that: The sodium channel modulator in the active component B is selected from cypermethrin, lambda-cyhalothrin, fenpropathrin, fenvalerate, flucythrinate, flumethrin, beta-cyfluthrin, cyfluthrin, bifenthrin, deltamethrin, acrinathrin, alp-cypermeth ... ha-cypermethrin), bifenthrin, cyhalothrin, permethrin, fluvalinate, allethrin, bioallethrin, cycloprothrin, gamma-cyhalothrin, theta-cypermethrin, zeta-cypermethrin, cyphenothrin thrin), empenthrin, esfenvalerate, imiprothrin, meperfluthrin, metofluthrin, dimefluthrin, prallethrin, phenothrin, resmethrin, bioresmethrin, cismethrin, tefluthrin, tetramethrin methrin), tetramethylfluthrin, tralomethrin, beta-cypermethrin, ethofenprox, transfluthrin, esdépalléthrine, barthrin, bioethanomethrin, brofenvalerate, brofluthrinate, bromethrin, butethrin,Chlorempenthrin, cyclethrin, cyhalothrin, lambda-cyhalothrin, dimethrin, d-fanshiluquebingjuzhi, fenfluthrin, fenpirithrin, esfenvalerate, furamethrin, imiprothrin, japothrins, kadethrin, methotrexate, pentmethrin, biopermethrin, methyl proparthrin, resmethrin, terallethrin, tralocythrin, valerate, flufenprox, halfenprox, sulfoxime, thiofluoximate, flumethrin, furethrin, heptafluthrin, momfluorothrin, transpermethrin, profluthrin, pyresmethrin, protrifenbute, silafluofen, DDT or methoxychlor; The voltage-dependent sodium channel blockers are selected from indoxacarb or metaflumizone.
3. The insecticide and acaricide composition according to claim 1 or 2, characterized in that: The active component A is selected from compound I or its stereoisomers, and the active component B is selected from cypermethrin. The weight ratio of the two active components is 30:1-1:
30.
4. The insecticide and acaricide composition according to claim 1 or 2, characterized in that: The active component A is selected from compound I or its stereoisomers, and the active component B is selected from cypermethrin. The weight ratio of the two active components is 4:45 to 1:
16.
5. The insecticide and acaricide composition according to claim 1 or 2, characterized in that: The active component A is selected from compound I or its stereoisomers, and the active component B is selected from indoxacarb; the weight ratio of the two active components is 30:1-1:
30.
6. The insecticide and acaricide composition according to claim 1 or 2, characterized in that: The active component A is selected from compound I or its stereoisomers, and the active component B is selected from indoxacarb; the weight ratio of the two active components is 1:
8.
7. The insecticide and acaricide composition according to claim 1, characterized in that: The composition is mixed with a carrier and any auxiliary agent to prepare a preparation containing the composition, wherein the cumulative content of the active component of the composition in the preparation is between 0.5wt% and 95wt%; preferably, the cumulative content of the active component in the preparation is between 1% and 85%.
8. Use of the insecticide and acaricide composition according to claim 1, characterized in that: The composition is used in preparing insecticides and acaricides for controlling agricultural pests or urban health pests.
9. The use of the insecticide and acaricide composition according to claim 8, characterized in that: The prepared insecticide and acaricide is applied to the pests to be controlled or the medium where they grow in an effective dose.
