Benzovindiflupyr-containing bactericidal composition for flight control of unmanned aerial vehicle as well as preparation method and application of benzovindiflupyr-containing bactericidal composition

Abstract

The invention relates to a benzovindiflupyr-containing bactericidal composition for unmanned aerial vehicle flight control and a preparation method and application thereof, and relates to the field of pesticides, the benzovindiflupyr-containing bactericidal composition comprises the following raw materials by weight: 1-20% of benzovindiflupyr, 1-20% of a triazole bactericide, 8-12% of a composite permeation synergist, 3-6% of a dispersant, 2-5% of a wetting agent, and 50-75% of a plant oil-based solvent and polar solvent compounded solvent; optionally, the composite permeation synergist is selected from polyether modified polysiloxane, a wax dissolving agent and the like; optionally, the plant oil-based solvent is selected from rosin-based plant oil, an SHP-240 tree source solvent and the like; through dosage form suitability optimization, synergistic interaction mechanism innovation and environmental protection improvement, the problems of pesticide effect loss, resistance risk and environmental pollution of a compound preparation in unmanned aerial vehicle application in the prior art are solved.

Description

Technical Field

[0001] This invention relates to the field of pesticides, and in particular to a fungicide composition containing benzo[a]fluoroquinolones for use in drone-based aerial spraying, its preparation method, and its application. Background Technology

[0002] The information disclosed in this background section is intended only to enhance the understanding of the overall background of the invention and should not be construed as an admission or in any way implying that the information constitutes prior art known to those skilled in the art.

[0003] Benzvindiflupyr, chemically named N-[9-(dichloromethyl)-1,2,3,4-tetrahydro-1,4-methylenenaphthyl-5-yl]-3-(difluoromethyl)-1-methyl-1H-pyrazole-4-carboxamide, is a pyrazoleamide fungicide developed by Syngenta and launched in 2012. It belongs to the succinate dehydrogenase inhibitor (SDHI) class and works by interfering with protein complex II (succinate dehydrogenase or succinate-ubiquinone reductase) in the mitochondrial respiratory electron transport chain of pathogens, leading to tricarboxylic acid cycle disorders and ultimately death. This fungicide has no interaction with triazole fungicides and methoxyacrylate fungicides and is effective in controlling various diseases such as wheat leaf blight, peanut black spot, rust, wheat powdery mildew, and gray mold. Its structural formula is as follows: .

[0004] Fluticasone (chemical name: (2RS,3SR)-1-[3-(2-chlorophenyl)-2,3-oxo-bridged-2-(4-fluorophenyl)propyl]-1H-1,2,4-triazole) is a systemic triazole fungicide developed by BASF. Fluticasone inhibits the synthesis of ergosterol in pathogens, hinders the formation of pathogen cell walls, and has a strong affinity for fungal enzymes (14-demethylases). It is rapidly absorbed by the plant and translocated to the infected parts, immediately stopping disease infection and exhibiting excellent residual efficacy. It has good control effects on leaf spot, powdery mildew, and rust diseases in crops such as bananas, onions, garlic, and peanuts, and can increase the chitinase activity of crops, enhancing their own disease resistance.

[0005] Plant diseases pose a serious threat to agricultural production. Although traditional fungicides can effectively control diseases, long-term use of a single fungicide can easily lead to pathogens developing resistance, reducing the effectiveness of control.

[0006] However, existing fungicide compositions containing benzo[a]flufenicol are mostly designed for traditional ground spraying, which has the following problems: Insufficient formulation compatibility: Traditional benzo[a]fluconazole compound formulations are mostly designed for ground spraying, which has problems such as uneven droplet size, rapid evaporation, and droplet drift, resulting in a pesticide efficacy loss rate of more than 40%.

[0007] Duration of efficacy and risk of drug resistance: The use of benzo[a]fluconazole alone is prone to inducing resistance (such as succinate dehydrogenase subunit mutation), while the existing compound combinations have limited synergistic effects, requiring frequent application, which increases costs and the risk of drug resistance.

[0008] Environmental limitations: Traditional solvents, such as aromatic hydrocarbons (e.g., xylene, which are highly toxic), can easily pollute non-target environments during aerial spraying and leave high residue levels.

[0009] Application limitations: Existing technologies mostly focus on common diseases (such as wheat powdery mildew), lack rapid control solutions for explosive diseases (such as wheat scab and corn leaf blight), and are not adapted to the stability requirements of high temperature and high humidity environments.

[0010] Therefore, developing novel compound fungicides, delaying the development of pathogen resistance, improving the adaptability of drone-based aerial spraying technology, and innovating application scenarios have become current hot topics in pesticide research. Summary of the Invention

[0011] Purpose of the invention The purpose of this invention is to provide a fungicide composition containing benzylfluopyrazosulfuron for aerial spraying by drones, its preparation method, and its application. This invention solves the problems of efficacy loss, resistance risk, and environmental pollution associated with existing compound formulations used in drone applications by optimizing dosage form compatibility, innovating synergistic mechanisms, and improving environmental friendliness.

[0012] Solution In a first aspect, to achieve the objective of this invention, embodiments of this invention provide a fungicide composition containing benzylflufenicol for use in drone aerial spraying, comprising the following raw materials by weight percentage: 1%-20% benzylflufenicol, 1%-20% triazole fungicide, 8-12% composite penetration enhancer, 3-6% dispersant, 2-5% wetting agent, and 50-75% compound solvent of vegetable oil-based solvent and polar solvent; Optionally, the composite penetration enhancer is selected from at least two of the following: polyether-modified polysiloxane, solvent, oleic acid, siloxane polyoxyethylene ether, glycerol, and isosorbide dimethyl ether. Optionally, the vegetable oil-based solvent is selected from at least one of the following: rosin-based vegetable oil, SHP-240 tree-derived solvent, methylated sunflower seed oil, sodium cottonseed oil sulfate, turpentine, coconut oil, palm oil, and jatropha oil; Optionally, the polar solvent is selected from at least one of xylene, dimethyl sulfoxide, N,N-dimethylformamide, dipropylene glycol methyl ether, sec-butyl acetate, and N-methylpyrrolidone.

[0013] Furthermore, the composite penetration enhancer includes polyether-modified polysiloxane and a wax solvent, wherein the weight ratio of polyether-modified polysiloxane (HLB value 8.1, optionally DY-ET113) to wax solvent is 1:(5~15), optionally 1:9; Optionally, in the compound solvent of vegetable oil-based solvent and polar solvent, the weight ratio of vegetable oil-based solvent to polar solvent is 45:(10~30), optionally 45:(12~28), optionally 45:22; Optionally, the dispersant is selected from one or more of alkylphenol polyoxyethylene ether phosphate, sulfosuccinate, polycarboxylate-polyether block copolymer, benzyl dimethylphenol polyoxyethylene ether, alkyl naphthalene sulfonate, castor oil polyoxyethylene ether, acrylic acid-maleic anhydride copolymer, and isomeric decayl alcohol polyoxyethylene ether. Optionally, the dispersant includes polycarboxylate-polyether block copolymer and / or castor oil polyoxyethylene ether. Optionally, the dispersant includes polycarboxylate-polyether block copolymer and castor oil polyoxyethylene ether in a weight ratio of 2:(0~1). Optionally, the wetting agent is selected from one or more of fatty alcohol polyoxyethylene ether, alkylphenol polyoxyethylene ether, triphenylethylphenol polyoxypropylene polyoxyethylene block polymer, sorbitan fatty acid ester polyoxyethylene ether, and fatty alcohol polyoxyethylene ether, and optionally, the wetting agent is an alkyl glycoside.

[0014] Furthermore, the weight ratio of benzoxystrobin to triazole fungicide is 1:8 to 2:1, optionally 1:4 to 1:1, optionally 1:3 to 1:1, optionally 1:5, 1:4, 1:3, 1:2, 1:1 or 2:1; And / or, the triazole fungicide is flutriafol.

[0015] Further, the raw materials include the following weight fractions: 1%-5% benzylfluopyram, 2%-20% triazole fungicide, 8-12% compound penetration enhancer, 3-6% dispersant, 2-5% wetting agent, and 50-75% compound solvent of vegetable oil-based solvent and polar solvent; Optionally, the raw materials include the following weight fractions: 1%-10% benzylflufenicol, 5%-20% triazole fungicide, 8-12% compound penetration enhancer, 3-6% dispersant, 2-5% wetting agent, and 50-75% compound solvent of vegetable oil-based solvent and polar solvent.

[0016] Further, the raw materials include the following weight fractions: 1%-5% benzylfluopyram, 8%-20% triazole fungicide, 10-12% compound penetration enhancer, 4.5-6% dispersant, 3.5-5% wetting agent, and 57-73% compound solvent of vegetable oil-based solvent and polar solvent; Optionally, the raw materials include the following weight fractions: 3%-5% benzyl sulfadiazine, 10%-12% triazole fungicide, 10-12% compound penetration enhancer, 4.5-6% dispersant, 3.5-5% wetting agent, and 65-69% compound solvent of vegetable oil-based solvent and polar solvent; Optionally, the raw materials include the following weight fractions: 3%-5% benzo[a]fluconazole, 10%-12% flutriafol, 1-2% polyether-modified polysiloxane, 9-10% wax solvent, 3-4.5% polycarboxylate-polyether block copolymer, 0-4.5% castor oil polyoxyethylene ether, 3.5-5% alkyl glycoside, 45-47% SHP-240 resin solvent, and 20-25% N-methylpyrrolidone; Optionally, the raw materials include the following weight fractions: 3%-5% benzo[a]fluconazole, 10%-12% flutriafol, 1% polyether-modified polysiloxane, 9% wax solvent, 3-4.5% polycarboxylate-polyether block copolymer, 0-4.5% castor oil polyoxyethylene ether, 3.5% alkyl glycoside, 45-47% SHP-240 resin solvent, and 22-25% N-methylpyrrolidone; Optionally, the raw materials include the following weight fractions: 4%-5% benzo[a]fluconazole, 10%-11% flutriafol, 1% polyether-modified polysiloxane, 9% wax solvent, 3-4.5% polycarboxylate-polyether block copolymer, 0-4.5% castor oil polyoxyethylene ether, 3.5% alkyl glycoside, 45-46% SHP-240 resin solvent, and 22-24% N-methylpyrrolidone; Optionally, the raw materials include the following weight fractions: 4%-5% benzo[a]fluconazole, 10%-11% flutriafol, 1% polyether-modified polysiloxane, 9% wax solvent, 4.5% polycarboxylate-polyether block copolymer, 3.5% alkyl glycoside, 45-46% SHP-240 resin solvent, and 22-23% N-methylpyrrolidone; Optionally, the raw materials include the following weight fractions: 4% benzo[a]fluconazole, 11% flutriafol, 1% polyether-modified polysiloxane, 9% solvent, 4.5% polycarboxylate-polyether block copolymer, 3.5% alkyl glycoside, 45% SHP-240 resin solvent, and N-methylpyrrolidone to make up to 100%.

[0017] Furthermore, the bactericidal composition is in the form of an ultra-low volume liquid.

[0018] Furthermore, it also includes the following dosage form excipients by weight fraction: antifreeze 0-10%, thickener 0-1.5%, and defoamer 0-0.15%.

[0019] In a second aspect, a method for preparing the bactericidal composition described in the first aspect is provided, comprising the following steps: dissolving benzo[i]fluconazole and triazole fungicides in a portion of a compound solvent, and mixing them with a compound penetration enhancer, dispersant, wetting agent, and the remaining compound solvent to obtain an ultra-low volume liquid. Specifically: in a mixing container equipped with a stirring device, a portion of the compound solvent is first mixed with the active ingredients (benzo[i]fluconazole and triazole fungicides), and stirred until fully dissolved; then, the compound penetration enhancer, dispersant, wetting agent, and the remaining compound solvent are added, and the mixture is continuously stirred under normal temperature and pressure conditions until the system is homogeneous, ultimately obtaining an ultra-low volume liquid containing a composition of benzo[i]fluconazole and triazole fungicides; optionally, the stirring rate is maintained at 60–150 rpm, and the stirring time is 20–60 minutes.

[0020] Thirdly, the application of the bactericidal composition described in the first aspect or the bactericidal composition prepared by the preparation method described in the second aspect in the prevention and control of plant diseases is provided. Optionally, the plant disease is a plant disease caused by fungi or bacteria, and optionally the plant disease is wheat powdery mildew fungus or corn leaf blight fungus.

[0021] Fourthly, a method of using the bactericidal composition as described in the first aspect or the bactericidal composition prepared by the preparation method described in the second aspect is provided. The formulation generally does not require high-multiple dilution with water as conventional pesticides, and can be used directly or after dilution with only a very small amount of solvent. A key feature is that the amount of stock solution applied per unit area is extremely small.

[0022] Beneficial effects: (1) The present invention uses a compound synergistic bactericidal composition of benzyl benzoate specifically designed for drone aerial spraying scenarios. Through optimization of dosage form compatibility, innovation of synergistic mechanism and improvement of environmental protection, it solves the problems of efficacy loss, resistance risk and environmental pollution of compound preparations in drone applications in the prior art.

[0023] (2) This invention solves the problems of efficacy loss, resistance risk, and environmental pollution in drone spraying of existing benzylfloxacin compound formulations by innovating formulation adaptability (ULV liquid), environmentally friendly solvent system (plant oil-based compound), and breakthrough in synergistic mechanism (dual target inhibition). The ULV liquid has a droplet settling rate of ≥85%, and almost settles immediately after spraying, reducing the drift and waiting time of the liquid in the air, ensuring "coverage wherever the medicine is applied", and achieving high efficiency within 3 days after application, filling the technical gap in rapid control of explosive diseases. The composition of this invention can be used for drone ultra-low volume spraying, with an operating efficiency of 50-80 mu / hour. Compared with traditional manual ground spraying (operating efficiency of only 5-10 mu / hour), the efficiency is increased by more than 10 times. That is, this invention can quickly contain the disease in the early stage and prevent its further spread, while existing technologies require a longer time to achieve a similar level of control. Detailed Implementation

[0024] To make the objectives, technical solutions, and advantages of the embodiments of the present invention clearer, the technical solutions in the embodiments of the present invention will be clearly and completely described below. Obviously, the described embodiments are only some embodiments of the present invention, not all embodiments. Based on the embodiments of the present invention, all other embodiments obtained by those skilled in the art without creative effort are within the scope of protection of the present invention. Unless otherwise expressly stated, throughout the specification and claims, the term "comprising" or its variations such as "including" or "comprising of," etc., will be understood to include the stated elements or components, and does not exclude other elements or other components.

[0025] Furthermore, to better illustrate the present invention, numerous specific details are provided in the following detailed embodiments. Those skilled in the art should understand that the present invention can be practiced without certain specific details. In some embodiments, materials, elements, methods, and means well known to those skilled in the art are not described in detail in order to highlight the spirit of the invention.

[0026] The technical grade benzo[i]floxacin and flutriafol in the following examples can be obtained commercially. Other raw materials are conventional commercial products. For example, polyether-modified polysiloxane was purchased from Shandong Dayi DY-ET113, which has an HLB value of 8.1 and is an excellent nonionic special surfactant.

[0027] Application Example 1: Bioassay Test materials: test pathogens (such as Rhizoctonia solani), petri dishes, PDA medium, pipettes, aseptic workbench, etc.

[0028] Test reagents: benzovindiflubenzuron (A), flutriafol (B).

[0029] Test Method: The stock solutions of each agent were diluted into five series of concentrations and placed in petri dishes for later use. The mycelial growth rate method was used to inoculate the pathogens onto the prepared drug-treated culture media, ensuring a consistent inoculation amount. Each concentration treatment was replicated in triplicate, and a blank control group was set up, whose culture medium did not come into contact with any agent. The pathogens were cultured under suitable temperature and humidity conditions, and the mycelial growth was observed and recorded regularly to calculate the inhibition rate. Through in-depth analysis of the experimental data, a virulence regression equation was derived to determine the lethal median concentration of the toxin and calculate the correlation coefficient. Simultaneously, the co-toxicity coefficient (CTC value) was calculated using the Sun Yunpei method, thus providing a more comprehensive assessment of the toxin's toxic effects.

[0030] LC50 calculation: Single-dose LC 50 The mycelial growth inhibition method was used to determine the compound LC. 50 Estimation based on the equivalent line graph method.

[0031] Single-dose A is used as the standard drug.

[0032] Measured toxicity index ATI = (LC50 of single dose A) 50 / Compound LC 50 ) × 100%.

[0033] Theoretical Toxicity Index (TTI) = (ATI of single dose A × proportion of the active ingredient in the mixture + ATI of single dose B × proportion of the active ingredient in the mixture) / total proportion.

[0034] Cotoxicity coefficient CTC = (Measured toxicity index ATI / Theoretical toxicity index ATI) × 100%.

[0035] The co-toxicity coefficient (CTC) of the compound combination is greater than 120, indicating a significant synergistic effect; 120 ≥ CTC ≥ 80 indicates an additive or partial synergistic effect; and CTC < 80 indicates an antagonistic effect.

[0036] The results for benzo[a]fluconazole (A) and flutriafol (B) are shown in Table 1.

[0037] Table 1. Virulence test results of benzo[a]fluconazole and flutriafol mixture against Rhizoctonia solani.

[0038] The results are shown in Table 1. The co-toxicity coefficient (CTC) of benzimidazole and flutriafol in the weight ratio range of 1:8 to 2:1 was greater than 120, and both showed a synergistic effect on the tested pathogens. In particular, the CTC was 149 to 153 in the range of 1:4 to 1:1, which was significantly higher than other ratio ranges.

[0039] Formulation Examples Example 1: 15% Benzobacterium fluopyram·Flutrithazole Ultra-Low Volume Liquid This embodiment includes the following raw materials in the following weight fractions: 4% benzo[a]fluconazole, 11% flutriafol, 1% polyether-modified polysiloxane (purchased from Shandong Dayi Chemical), 9% wax solvent, 4.5% polycarboxylate-polyether block copolymer, 3.5% alkyl glycoside, 45% SHP-240 resin solvent, and N-methylpyrrolidone to make up the difference.

[0040] Example 2: 15% Benzobacterium fluopyram·Flutrithazole Ultra-Low Volume Liquid This embodiment includes the following raw materials in the following weight fractions: 4% benzo[a]fluconazole, 11% flutriafol, 1% polyether-modified polysiloxane, 9% wax solvent, 4.5% castor oil polyoxyethylene ether, 3.5% alkyl glycoside, 45% SHP-240 resin solvent, and N-methylpyrrolidone to make up the difference.

[0041] Example 3: 15% Benzobacterium fluopyram·Flutrithazole Ultra-Low Volume Liquid This embodiment includes the following raw materials in the following weight fractions: 4% benzo[a]fluconazole, 11% flutriafol, 1% polyether-modified polysiloxane, 9% wax solvent, 1.5% castor oil polyoxyethylene ether, 3% polycarboxylate-polyether block copolymer, 3.5% alkyl glycoside, 45% SHP-240 resin solvent, and N-methylpyrrolidone to make up the difference.

[0042] Example 4: 15% Benzobacterium fluopyram·Flutrithazole Ultra-Low Volume Liquid This embodiment includes the following raw materials in the following weight fractions: 3% benzo[a]fluconazole, 12% flutriafol, 1% polyether-modified polysiloxane, 9% wax solvent, 4.5% polycarboxylate-polyether block copolymer, 3.5% alkyl glycoside, 45% SHP-240 resin solvent, and N-methylpyrrolidone to make up the difference.

[0043] Example 5: 15% Benzophenoxynil·Flutrithazole Ultra-Low Volume Liquid This embodiment includes the following raw materials in the following weight fractions: 2% benzo[a]fluconazole, 13% flutriafol, 1% polyether-modified polysiloxane, 9% wax solvent, 4.5% polycarboxylate-polyether block copolymer, 3.5% alkyl glycoside, 45% SHP-240 resin solvent, and N-methylpyrrolidone to make up the difference.

[0044] Example 6: 5% Benzophenoxynil·Flutrithazole Ultra-Low Volume Liquid This embodiment includes the following raw materials in the following weight fractions: 1% benzo[a]fluconazole, 14% flutriafol, 1% polyether-modified polysiloxane, 9% wax solvent, 4.5% polycarboxylate-polyether block copolymer, 3.5% alkyl glycoside, 45% SHP-240 resin solvent, and N-methylpyrrolidone to make up the difference.

[0045] Example 7: 15% Benzophenoxynil·Flutrithazole Ultra-Low Volume Liquid This embodiment includes the following raw materials in the following weight fractions: 5% benzo[a]fluconazole, 10% flutriafol, 1% polyether-modified polysiloxane, 9% wax solvent, 4.5% polycarboxylate-polyether block copolymer, 3.5% alkyl glycoside, 45% SHP-240 resin solvent, and N-methylpyrrolidone to make up the difference.

[0046] Example 8: 9% Benzophenoxynil·Flutrithazole Ultra-Low Volume Liquid This embodiment includes the following raw materials in the following weight fractions: 1% benzo[a]fluconazole, 8% flutriafol, 1% polyether-modified polysiloxane, 9% wax solvent, 4.5% polycarboxylate-polyether block copolymer, 3.5% alkyl glycoside, 45% SHP-240 resin solvent, and N-methylpyrrolidone to make up the difference.

[0047] Example 9: 25% Benzophenoxynil·Flutrithazole Ultra-Low Volume Liquid This embodiment includes the following raw materials in the following weight fractions: 5% benzo[a]fluconazole, 20% flutriafol, 1% polyether-modified polysiloxane, 9% wax solvent, 4.5% polycarboxylate-polyether block copolymer, 3.5% alkyl glycoside, 45% SHP-240 resin solvent, and N-methylpyrrolidone to make up the difference.

[0048] Comparative Example 1: 15% Benzophenoxynil·Flutrithazole Ultra-Low Volume Liquid This embodiment includes the following raw materials in the following weight fractions: 4% benzo[a]fluconazole, 11% flutriafol, 1% polyether-modified polysiloxane, 9% azone, 4.5% polycarboxylate-polyether block copolymer, 3.5% alkyl glycoside, 45% SHP-240 resin solvent, and N-methylpyrrolidone to make up the difference.

[0049] Comparative Example 2: 15% Benzophenoxynil·Flutrithazole Ultra-Low Volume Liquid This embodiment includes the following raw materials in the following weight fractions: 4% benzo[a]fluconazole, 11% flutriafol, 10% wax solvent, 4.5% polycarboxylate-polyether block copolymer, 3.5% alkyl glycoside, 46% SHP-240 resin solvent, and N-methylpyrrolidone to make up the difference.

[0050] Comparative Example 3: 15% Benzophenoxynil·Flutrithazole Ultra-Low Volume Liquid This embodiment includes the following raw materials in the following weight fractions: 4% benzo[a]fluconazole, 11% flutriafol, 1% ordinary silicone oil, 9% JFC penetrant, 4.5% polycarboxylate-polyether block copolymer, 3.5% alkyl glycoside, 45% SHP-240 resin solvent, and N-methylpyrrolidone to make up the difference.

[0051] Comparative Example 4: 15% Benzophenoxynil·Flutrithazole Ultra-Low Volume Liquid This embodiment includes the following raw materials in the following weight fractions: 4% benzo[a]fluconazole, 11% flutriafol, 1% polyether-modified polysiloxane, 9% wax solvent, 8% polycarboxylate-polyether block copolymer, 45% SHP-240 resin solvent, and N-methylpyrrolidone to make up the difference.

[0052] Comparative Example 5: 15% Benzophenoxynil·Flutrithazole Ultra-Low Volume Liquid This embodiment includes the following raw materials in the following weight fractions: 4% benzo[a]fluconazole, 11% flutriafol, 1% polyether-modified polysiloxane, 9% wax solvent, 8% alkyl glycoside, 45% SHP-240 resin solvent, and N-methylpyrrolidone to make up the difference.

[0053] Comparative Example 6: 15% Benzophenoxynil·Flutrithazole Ultra-Low Volume Liquid This embodiment includes the following raw materials in the following weight fractions: 4% benzo[a]fluconazole, 11% flutriafol, 1% polyether-modified polysiloxane, 9% wax solvent, 4.5% polycarboxylate-polyether block copolymer, 3.5% alkyl glycoside, 45% mineral oil, and N-methylpyrrolidone to make up the difference.

[0054] Comparative Example 7: 15% Benzophenoxynil·Flutrithazole EC This embodiment includes the following raw materials in the following weight fractions: 4% benzo[a]fluconazole, 11% flutriafol, 1% polyether-modified polysiloxane, 9% wax solvent, 4.5% polycarboxylate-polyether block copolymer, 3.5% alkyl glycoside, 45% SHP-240 resin solvent, and propylene glycol to make up the difference.

[0055] Comparative Example 8: 15% Benzophenoxynil·Flutrithazole Ultra-Low Volume Liquid This embodiment includes the following raw materials in the following weight fractions: 15% benzo[a]fluoroazole, 1% polyether-modified polysiloxane, 9% solvent, 4.5% polycarboxylate-polyether block copolymer, 3.5% alkyl glycoside, 45% SHP-240 resin solvent, and N-methylpyrrolidone to make up the difference.

[0056] Comparative Example 9: 15% Benzophenoxynil·Flutrithazole Ultra-Low Volume Liquid This embodiment includes the following raw materials in the following weight fractions: 15% flutriafol, 1% polyether-modified polysiloxane, 9% wax solvent, 4.5% polycarboxylate-polyether block copolymer, 3.5% alkyl glycoside, 45% SHP-240 resin solvent, and N-methylpyrrolidone to make up the difference.

[0057] Comparative Example 10:15% Benzophenoxynil·Flutrithazole Ultra-Low Volume Liquid This embodiment includes the following raw materials in the following weight fractions: 4% benzo[a]fluoroazole, 11% flutriafol, 1% polyether-modified polysiloxane, 9% wax solvent, 7% alkylphenol polyoxyethylene ether, 3.5% calcium dodecylbenzenesulfonate, 20% cyclohexanone, and xylene to make up the difference.

[0058] Comparative Example 11:15% Benzobacterium fluopyram·Flutrithazole Ultra-Low Volume Liquid This embodiment includes the following raw materials in the following weight fractions: 4% benzo[a]fluoroazole, 11% flutriafol, 1% polyether-modified polysiloxane, 9% wax solvent, 6% polycarboxylate-polyether block copolymer, 2% calcium dodecylbenzenesulfonate, 5% ethylene glycol, 25% acetone, and water to make up the difference.

[0059] Test Example 2: Droplet Performance Test Droplet size distribution test Equipment calibration: Use standard particles (10-300μm) to calibrate the laser particle size analyzer (Malvern Spraytec) to ensure an error of <±2%.

[0060] Pharmaceuticals: Examples 1-9 and Comparative Example 1.

[0061] Reference standard: ISO 25358:2018 "Measurement of droplet spectra in agricultural aerial spray".

[0062] Nozzle model: XR110015 (centrifugal type, compatible with drones); Injection pressure: 0.3 MPa, flow rate: 1.0 L / min, spray width: 5 m; Spraying height: 1.5 m (simulating drone flight altitude).

[0063] Data acquisition: Spraying was performed in a sealed experimental chamber, and the droplet size distribution was recorded in real time by a laser particle size analyzer. This process was repeated 3 times.

[0064] Data processing: Calculate the volume median diameter (VMD) and span (Span= The results are shown in Table 2.

[0065] Table 2. Droplet size distribution of each embodiment and comparative example.

[0066] As shown in Table 2, the droplet size of Example 1 (Dv50=112μm) is the smallest and the span is the narrowest, indicating that 1% polyether siloxane + 9% wax solvent + 4.5% polycarboxylic acid ester + 3.5% alkyl glycoside can synergistically reduce surface tension.

[0067] Evaporation resistance test Experimental conditions: Room temperature group: 25℃±1℃, RH 60%±5%.

[0068] Sample preparation: Spray the drug solution evenly onto the glass slide (initial weight W0 = 1.000 g), and repeat 5 times for each group.

[0069] Weighing monitoring: Using a precision balance (accuracy 0.001 g), the residual amount W was recorded every 30 minutes. t It lasted for 4 hours.

[0070] Evaporation residue rate calculation: Evaporation residue rate (%) = 1 - ( ×100%).

[0071] Relative evaporation rate R (%) = .

[0072] If R > 1: the sample evaporates faster than the reference; if R = 1: the sample and reference evaporate at roughly the same rate. If R < 1: the sample evaporates slower than the reference, with n-dodecane used as the reference.

[0073] The results are shown in Table 3.

[0074] Table 3. Evaporation resistance results for each embodiment and comparative example.

[0075] As shown in Table 3, Example 1 exhibits the best resistance to evaporation, with an evaporation residue rate of 92.5% (relative evaporation rate = 1.0). This demonstrates that the SHP-240 (high-boiling-point resin solvent) + NMP (strong film-forming agent) + 1% polyether siloxane (surface spreading agent) of the present invention can form a dense liquid film.

[0076] The SHP-240 / NMP solvent system (average boiling point 215°C) of the present invention, combined with polyether siloxane and amphiphilic surfactant, achieves a liquid film formation index of 0.95 (out of 1.0), which is 137% higher than that of traditional solvents (comparative examples 10-11) and 111% higher than that of single solvent replacement schemes (comparative examples 6-7).

[0077] Coverage uniformity test Standard: Based on ASABE S572.1 standard (spray uniformity assessment) Fluorescent labeling: Add 0.1% rhodamine B fluorescent dye (Sigma-Aldrich) to the drug solution to ensure no activity interference.

[0078] Spraying simulation: A rotating spray tower (Spraying Systems Co.) was used to simulate the flight trajectory of a drone, spraying onto wheat leaves (plant height 50 cm) at a rate of 20-35 ml / m².2 .

[0079] Image acquisition: The leaves were illuminated by a UV lamp (365 nm), and the distribution of fluorescence dots was captured by a high-definition camera (resolution 1200 dpi).

[0080] Data Analysis: Coverage (%): The percentage of the total area covered by fluorescent dots; Droplet density: The number of droplets per unit area (usually cm²). Automatically identified and counted by software, reflecting the density of droplet distribution.

[0081] Coefficient of variation: the standard deviation of coverage of all sampling points divided by its mean. The results are shown in Table 4.

[0082] Table 4. Coverage uniformity test results for each embodiment and comparative example.

[0083] As shown in Table 4, the breakthrough spreading mechanism of Example 1 can achieve a leaf coverage rate of 95.2%. This invention employs a dual synergistic effect: polyether siloxane is used to reduce the static surface tension to 28.1 mN / m, and the wax solvent dynamically exfoliates the wax layer, reducing the contact angle to 15.3°, forming an ultra-thin continuous liquid film (thickness ≤8μm), achieving a coverage rate exceeding 95%, which is significantly superior to other penetrants (such as azone in Comparative Example 1).

[0084] Rainwater erosion resistance test Standard: Based on OECD Guideline 501 (pesticide residues washed away by rain).

[0085] Drug film deposition: Spray the drug solution onto wheat leaves and let it stand for 1 hour to form a stable drug film.

[0086] Simulated rainfall: Using an artificial rainmaking device (Veejet 8001 nozzle), the rainfall intensity was 50 mm / h, lasting for 30 minutes.

[0087] Efficacy testing: Pathogen: Fusarium graminearum (Wheat scab) Fusarium graminearum (The wheat scab fungus that is routinely obtained can be obtained by screening diseased wheat or by purchasing it commercially.)

[0088] Methods: Testing was conducted using an artificial rainfall simulation device. The formulation of this invention and a comparative sample were sprayed onto wheat leaves (during a susceptible growth stage) and allowed to stand for 2 hours to form a stable film. The efficacy before washout was measured (as a baseline). Subsequently, simulated rainfall at intensities of 5 mm / h and 20 mm / h was applied for 15 minutes, and after natural evaporation of moisture from the leaf surface, the efficacy after washout was measured again. The efficacy retention rate was calculated to evaluate the formulation's resistance to rain washout.

[0089] Retention rate of active ingredients (%) = (Amount of active ingredients retained after rinsing / Amount of active ingredients retained before rinsing) × 100.

[0090] The formulation of this invention exhibits significant resistance to rainwater runoff, with an active ingredient retention rate exceeding 90% (p<0.001) 2 hours after application, making it suitable for use in rainy areas.

[0091] The results are shown in Table 5.

[0092] Table 5. Test results of rainwater erosion resistance of each embodiment and comparative example.

[0093] As shown in Table 5, the formulation of this invention, through its optimized solvent and adjuvant system, significantly improves the adhesion of the pesticide solution to the leaf surface and its resistance to rain washout. Its "active ingredient retention rate" is significantly better than that of traditional formulations (e.g., the residue rate in Example 1 is as high as 94.2%), ensuring long-lasting and stable disease protection for crops under variable climatic conditions, especially during the rainy summer season. This effectively solves the industry problems of short-lasting pesticide effect and high cost of re-spraying after rain in existing technologies.

[0094] Test Example 3: Field Aerial Spraying Test Experimental location: This experiment was conducted in an experimental field in the suburbs of Zhaoxian County, Shijiazhuang City, Hebei Province. The soil in the experimental field was brown soil with a pH value of 6.5-7.0. The relative humidity of the soil was maintained at 60%-80% before sowing. The weather was sunny on the day of application, with an average temperature of 25°C, a relative humidity of 65%, and a wind speed of less than level 3 (i.e., <3.4 m / s).

[0095] Test agents: Examples 1-9 and Comparative Examples 1-11 are ultra-low volume liquid agents. No additional adjuvants are required when using them. It is recommended to use drones for aerial spraying. The water consumption is 0.8-1.0 liters per acre. Dilute 50-80 times before application.

[0096] Experimental Methods: The experiment employed unmanned aerial vehicle (UAV) spraying. Before application, the wheat powdery mildew disease index was investigated (Reference: Zhao Jianting; Shi Yinlu; Disease Index and its Representation Method [J]; Shanxi Agricultural Sciences; 1990, Issue 03). Application was performed at the initial stage of disease. The disease index was investigated and the control efficacy was calculated at 3, 7, and 14 days after application. The effective period (i.e., the number of days with an efficacy of 70% or higher) was also calculated. The calculation formula is as follows: Calculation formula: Disease index = 100 × ∑(number of diseased leaves at each level × representative value at each level) / (total number of leaves surveyed × highest level representative value).

[0097] Prevention efficacy (%) = (Disease index of control group) (Disease index in treatment group) / (Disease index in control group) × 100% The results are shown in Table 6.

[0098] Table 6. Prevention efficacy of each embodiment and comparative example

[0099] According to Table 6, Example 1 of this invention achieves a significant breakthrough by maintaining efficacy for 21 days at a dosage of 20g / mu, reducing the dosage by 42.8% while increasing efficacy by 23.5% compared to traditional methods. In contrast, Comparative Examples 1-11 show a 10-15% drop in efficacy 14 days after application compared to 7 days after application. This invention effectively extends the protection period through a triple innovation of "interface activation - three-dimensional deposition - micro-domain sustained release". The present invention provides a benzo[i]floxacin compound synergistic bactericidal composition specifically for drone-based aerial spraying. Through optimization of dosage form compatibility, innovation of synergistic mechanism, and improvement of environmental friendliness, it solves the problems of efficacy loss, resistance risk, and environmental pollution that exist in traditional formulations used in drone applications.

[0100] The advantages of this invention are: The composition of this invention uses ultra-low volume liquid (ULV) as the core formulation, achieving precise control of droplet size (50-150 μm) and viscosity (50-100 mPa·s). It is compatible with drone centrifugal nozzles, reducing evaporation rate by 60% and increasing sedimentation rate to ≥85%, significantly superior to traditional emulsifiable concentrates. Field trials show that a single application achieves 96.7% control efficacy against wheat scab, with a residual effect of ≥14 days, reducing the dosage per acre by 30%, and exhibiting extremely low toxicity to non-target organisms (LD50 for bees >100 μg / bee), aligning with the trend of green agriculture.

[0101] This invention is the first ULV liquid agent adapted for UAV ultra-low volume aerial spraying. By controlling the droplet size (VMD=80.5μm) and using an anti-drift agent (polyether modified polyoxysilane), it solves the technical bottlenecks of traditional formulations such as droplet drift (settling rate <60%) and rapid evaporation (residual amount <30%), thereby improving the operation efficiency by 5 times.

[0102] This invention uses SHP-240 tree-derived solvent and polar solvent (N-methylpyrrolidone) in combination with wax solvent and polyether-modified polyoxysilane to significantly enhance the adhesion of the pesticide solution to the crop surface. After rinsing, the efficacy reduction rate is less than 10%, the droplet evaporation rate is reduced to 15.2% (4 hours), the leaf adhesion is increased by 3 times, and the pesticide solution retention time is extended.

[0103] This invention employs a dual-target synergistic mechanism—benzo[a]fluconazole (SDHI class) and flutriafol (triazole class) work through a dual mechanism of inhibition of mitochondrial respiratory chain complex II and blockade of ergosterol synthesis, achieving a synergistic co-toxicity coefficient (CTC) of 170-220, which is significantly higher than conventional compound formulations (CTC<120).

[0104] This invention employs dual-target inhibition to reduce the risk of single-point mutations in pathogens. Field trials showed a 30% increase in control efficacy against benzo[a]fluoroquinolones-resistant strains. This further reduces the risk of pathogen resistance to a single agent.

[0105] The environmental friendliness and innovative application scenarios of this invention: The formulation employs a fully biodegradable solvent system, replacing traditional aromatic solvents (such as xylene, acetone, and other volatile solvents) with vegetable oils to avoid stratification or precipitation, ensuring that the formulation remains stable at room temperature for over 24 months.

[0106] Enables rapid control of explosive diseases: Adapted to the high-efficiency coverage characteristics of drones, it achieves over 92% efficacy with a single application against explosive diseases such as wheat scab and corn leaf blight. Its rain-resistant properties make it suitable for rainy areas. The compound formulation can simultaneously control multiple fungal diseases, such as rice sheath blight, wheat scab, and apple black spot, reducing the need for multiple applications and lowering overall costs.

[0107] It should also be noted that the various specific technical features described in the above specific embodiments can be combined in any suitable manner without contradiction. In order to avoid unnecessary repetition, the present invention will not describe the various possible combinations separately.

[0108] Furthermore, various different embodiments of the present invention can be combined in any way, as long as they do not violate the spirit of the present invention, they should also be regarded as the content of the present invention.

Claims

1. A fungicide composition containing benzylflufenicol for aerial spraying by drones, characterized in that, The raw materials include the following weight percentages: 1%-20% benzylfluopyram, 1%-20% triazole fungicide, 8-12% compound penetration enhancer, 3-6% dispersant, 2-5% wetting agent, and 50-75% compound solvent of vegetable oil-based solvent and polar solvent; Optionally, the composite penetration enhancer is selected from at least two of the following: polyether-modified polysiloxane, solvent, oleic acid, siloxane polyoxyethylene ether, glycerol, and isosorbide dimethyl ether. Optionally, the vegetable oil-based solvent is selected from at least one of the following: rosin-based vegetable oil, SHP-240 tree-derived solvent, methylated sunflower seed oil, sodium cottonseed oil sulfate, turpentine, coconut oil, palm oil, and jatropha oil; Optionally, the polar solvent is selected from at least one of xylene, dimethyl sulfoxide, N,N-dimethylformamide, dipropylene glycol methyl ether, sec-butyl acetate, and N-methylpyrrolidone.

2. The bactericidal composition according to claim 1, characterized in that, The composite penetration enhancer includes polyether-modified polysiloxane and a wax solvent, wherein the weight ratio of polyether-modified polysiloxane to wax solvent is 1:(5~15), or optionally 1:9; Optionally, in the compound solvent of vegetable oil-based solvent and polar solvent, the weight ratio of vegetable oil-based solvent to polar solvent is 45:(10~30), optionally 45:(12~28), optionally 45:22; Optionally, the dispersant is selected from one or more of alkylphenol polyoxyethylene ether phosphate, sulfosuccinate, polycarboxylate-polyether block copolymer, benzyl dimethylphenol polyoxyethylene ether, alkyl naphthalene sulfonate, castor oil polyoxyethylene ether, acrylic acid-maleic anhydride copolymer, and isomeric decayl alcohol polyoxyethylene ether. Optionally, the dispersant includes polycarboxylate-polyether block copolymer and / or castor oil polyoxyethylene ether. Optionally, the dispersant includes polycarboxylate-polyether block copolymer and castor oil polyoxyethylene ether in a weight ratio of 2:(0~1). Optionally, the wetting agent is selected from one or more of fatty alcohol polyoxyethylene ether, alkylphenol polyoxyethylene ether, triphenylethylphenol polyoxypropylene polyoxyethylene block polymer, sorbitan fatty acid ester polyoxyethylene ether, and fatty alcohol polyoxyethylene ether, and optionally, the wetting agent is an alkyl glycoside.

3. The bactericidal composition according to claim 1 or 2, characterized in that, The weight ratio of benzoxystrobin to triazole fungicide is 1:8 to 2:1, optionally 1:4 to 1:1, optionally 1:3 to 1:1, optionally 1:5, 1:4, 1:3, 1:2, 1:1 or 2:1; And / or, the triazole fungicide is flutriafol.

4. The bactericidal composition according to any one of claims 1 to 3, characterized in that, The raw materials include the following weight fractions: 1%-5% benzyl fluoride, 2%-20% triazole fungicide, 8-12% compound penetration enhancer, 3-6% dispersant, 2-5% wetting agent, and 50-75% compound solvent of vegetable oil-based solvent and polar solvent; Optionally, the raw materials include the following weight fractions: 1%-10% benzylflufenicol, 5%-20% triazole fungicide, 8-12% compound penetration enhancer, 3-6% dispersant, 2-5% wetting agent, and 50-75% compound solvent of vegetable oil-based solvent and polar solvent.

5. The bactericidal composition according to any one of claims 1 to 4, characterized in that, The raw materials include the following weight fractions: 1%-5% benzylflufenicol, 8%-20% triazole fungicide, 10-12% compound penetration enhancer, 4.5-6% dispersant, 3.5-5% wetting agent, and 57-73% compound solvent of vegetable oil-based solvent and polar solvent; Optionally, the raw materials include the following weight fractions: 3%-5% benzyl sulfadiazine, 10%-12% triazole fungicide, 10-12% compound penetration enhancer, 4.5-6% dispersant, 3.5-5% wetting agent, and 65-69% compound solvent of vegetable oil-based solvent and polar solvent; Optionally, the raw materials include the following weight fractions: 3%-5% benzo[a]fluconazole, 10%-12% flutriafol, 1-2% polyether-modified polysiloxane, 9-10% wax solvent, 3-4.5% polycarboxylate-polyether block copolymer, 0-4.5% castor oil polyoxyethylene ether, 3.5-5% alkyl glycoside, 45-47% SHP-240 resin solvent, and 20-25% N-methylpyrrolidone; Optionally, the raw materials include the following weight fractions: 3%-5% benzo[a]fluconazole, 10%-12% flutriafol, 1% polyether-modified polysiloxane, 9% wax solvent, 3-4.5% polycarboxylate-polyether block copolymer, 0-4.5% castor oil polyoxyethylene ether, 3.5% alkyl glycoside, 45-47% SHP-240 resin solvent, and 22-25% N-methylpyrrolidone; Optionally, the raw materials include the following weight fractions: 4%-5% benzo[a]fluconazole, 10%-11% flutriafol, 1% polyether-modified polysiloxane, 9% wax solvent, 3-4.5% polycarboxylate-polyether block copolymer, 0-4.5% castor oil polyoxyethylene ether, 3.5% alkyl glycoside, 45-46% SHP-240 resin solvent, and 22-24% N-methylpyrrolidone; Optionally, the raw materials include the following weight fractions: 4%-5% benzo[a]fluconazole, 10%-11% flutriafol, 1% polyether-modified polysiloxane, 9% wax solvent, 4.5% polycarboxylate-polyether block copolymer, 3.5% alkyl glycoside, 45-46% SHP-240 resin solvent, and 22-23% N-methylpyrrolidone; Optionally, the raw materials include the following weight fractions: 4% benzo[a]fluconazole, 11% flutriafol, 1% polyether-modified polysiloxane, 9% solvent, 4.5% polycarboxylate-polyether block copolymer, 3.5% alkyl glycoside, 45% SHP-240 resin solvent, and N-methylpyrrolidone to make up to 100%.

6. The bactericidal composition according to any one of claims 1 to 5, characterized in that, The bactericidal composition is in the form of an ultra-low volume liquid.

7. The bactericidal composition according to any one of claims 1 to 6, characterized in that, It also includes the following dosage form excipients by weight fraction: antifreeze 0-10%, thickener 0-1.5%, and defoamer 0-0.15%.

8. A method for preparing the bactericidal composition according to any one of claims 1 to 7, characterized in that, Includes the following steps: Benzoflufenicol and triazole fungicides are dissolved in a portion of a compound solvent, and then mixed with a compound penetration enhancer, dispersant, wetting agent, and the remaining compound solvent to obtain an ultra-low volume liquid.

9. The application of a bactericidal composition according to any one of claims 1 to 7 or a bactericidal composition prepared by the preparation method according to claim 8 in the prevention and control of plant diseases; Optionally, the plant disease is a plant disease caused by fungi or bacteria, and optionally the plant disease is wheat powdery mildew fungus or corn leaf blight fungus.

10. A method of using a bactericidal composition according to any one of claims 1 to 7 or a bactericidal composition prepared by the preparation method according to claim 8, characterized in that, The formulation typically does not require high-level dilution with water like conventional pesticides; it can be used directly or after dilution with only a very small amount of solvent.

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