A pesticide composition and its preparation method and application

By combining flufenac and acephate, the problems of enhanced pest resistance and antagonism of pesticide compounds are solved, and the preparation and application of highly effective insecticides are realized, which are suitable for pest control of a variety of crops.

CN116473063BActive Publication Date: 2025-10-03CHINA AGRI UNIV
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Patent Information

Application Number
CN202310262557.1
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2023-03-17
Publication Date
2025-10-03
Estimated Expiration
2043-03-17

AI Technical Summary

Technical Problem

Long-term, large-scale, and repeated application of a single active compound to control pests can easily lead to increased pest resistance, especially for pests with overlapping generations such as Lepidoptera and Hemiptera. In addition, the combined use of different pesticide compounds poses risks of antagonism and environmental stability.

Method used

Flufenac and acephate are compounded in a specific ratio to form an insecticide composition, and adjuvants such as sodium lignin sulfonate, magnesium aluminum silicate, ethylene glycol, bentonite and xanthan gum are added to prepare it into microemulsions, water emulsions and other dosage forms, which significantly improve the insecticidal effect.

Benefits of technology

It significantly enhances the killing effect on pests, improves the prevention efficiency, reduces the amount of medicine used, and delays the development of pest resistance. It is suitable for a variety of crops such as corn, tea, tobacco, cotton, rice, wheat, etc., and can prevent and control leaf-feeding, piercing-sucking and underground pests.

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Abstract

The present invention relates to the field of crop planting technology, and in particular to a pesticide composition, a preparation method thereof, and an application thereof. The composition comprises: flubendiamide and acephate; the mass ratio of flubendiamide to acephate is (0.8-10):1. The present invention has found that under a specific ratio, the compounding of flubendiamide and acephate with different mechanisms of action and modes of action can significantly improve the prevention and control effect, effectively reduce the amount of pesticide used, reduce costs, and reduce harm to the environment. The compounded pesticide provided by the present invention has good fast-acting property and a long lasting effect. The prevention effect can reach more than 80% after 1 day of treatment with the agent, and the prevention effect is about 90% after 15 days of treatment. It can effectively delay the generation of pest resistance and is particularly suitable for the control of resistant pests.
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Description

Technical Field

[0001] The present invention relates to the technical field of crop planting, and in particular to an insecticide composition, a preparation method thereof and an application thereof. Background Art

[0002] Flufenac is a benzamide insecticide independently developed and manufactured by Hailier Pharmaceutical Group. It effectively activates insect nicotinic acid receptors, leading to the excessive release of calcium ions from cellular calcium stores, causing paralysis and death. Flufenac has a unique mechanism of action, high insecticidal activity, is environmentally friendly, and has low toxicity to mammals. It is highly effective against a variety of Lepidoptera pests, particularly the fall armyworm, rice stem borer, armyworm, bean pod borer, apple leaf roller, borer, cabbage worm, and diamondback moth, all at low doses. Flufenac also has high activity against Thysanoptera thrips (such as thrips, orchid thrips, tobacco thrips, and palm thrips).

[0003] Acephate is an organophosphorus pesticide, a systemic insecticide developed during the process of reducing the toxicity of methamidophos. It has stomach and contact effects, can kill eggs, and has a certain fumigant effect. It is a slow-acting insecticide. It acts on acetylcholinesterase, hindering the normal conduction of insect nerves, leading to death. It can be used on a variety of crops, including corn, tea, tobacco, cotton, rice, wheat, and rapeseed, to control a variety of chewing and piercing-sucking pests, mites, and sanitary pests.

[0004] Repeated, long-term, and high-volume application of the same active compound for pest control can easily lead to the development of resistance, especially in Lepidoptera and Hemiptera pests with overlapping generations. Furthermore, the simultaneous use of multiple pesticides for pest control presents the potential for antagonism between the different pesticide compounds, potentially damaging environmental stability. Summary of the Invention

[0005] In order to solve the technical problems existing in the prior art, the present invention provides an insecticide composition, a preparation method thereof, and an application thereof. By compounding flufenacet and acephate, the insecticide composition significantly improves the insecticide killing effect at a certain ratio.

[0006] In a first aspect, the present invention provides a composition comprising:

[0007] Flufenac and acephate;

[0008] The mass ratio of flubendiamide to acephate is (0.8-10):1.

[0009] The molecular formula of flubendiamide is C 17 H 10 BrCl3FN5O2, structural formula:

[0010]

[0011] The molecular formula of acephate: C4H 10 NO3PS.

[0012] Furthermore, the mass ratio of flubendiamide to acephate is (1-5):1.

[0013] Long-term and large-scale repeated application of the same active compound pest control is likely to lead to enhanced pest resistance, especially some Lepidoptera and Hemiptera generations of overlapping pests are very likely to produce resistance. The present invention has found that flubendiamide and acephate are compounded as insecticides with good synergistic effects under a certain compounding ratio, and the two are significantly improved with different insecticidal mechanisms to kill pests. In addition, the present invention finds that when flubendiamide and acephate are in a compounding ratio of 1:2-5 or more, there will be antagonism between the two, and this antagonism is irregular, and when the ratio is 1:2, the antagonism is significantly higher than 1:5.

[0014] Furthermore, the mass ratio of flubendiamide to acephate is (1.5-3):1.

[0015] In a second aspect, the present invention provides an insecticide comprising the composition.

[0016] Furthermore, the mass percentage of the composition in the insecticide is 15 to 40%.

[0017] Furthermore, in parts by weight, it comprises:

[0018] The composition comprises 20 to 35 parts, 5 to 10 parts of sodium lignin sulfonate, 0.5 to 3 parts of magnesium aluminum silicate, 2 to 10 parts of ethylene glycol, 2 to 5 parts of bentonite and 0.5 to 5 parts of xanthan gum.

[0019] Furthermore, the formulation of the insecticide is one or more of a microemulsion, an emulsion in water, a wettable powder, a water-dispersible granule, an emulsifiable concentrate or a suspension concentrate.

[0020] In a third aspect, the present invention provides a method for preparing the insecticide, comprising:

[0021] The components are mixed in proportion to prepare a suspension.

[0022] The present invention further provides the use of the insecticide in expanding the scope of killing pests, improving the control effect on pests or delaying the resistance of pests to pesticides.

[0023] Furthermore, the pests include one or more of leaf-feeding pests, piercing-sucking pests, underground pests or borer pests.

[0024] Furthermore, the pests are lepidopteran pests, preferably including one or more of fall armyworm, corn borer, rice stem borer, diamondback moth, armyworm, aphid, cotton bollworm, thrips, leafhopper or tobacco budworm.

[0025] The present invention has the following beneficial effects:

[0026] The present invention provides a composite insecticide by compounding flufenacet and acephate. The combination of these two ingredients exhibits a good synergistic effect, significantly improving the killing effect on various pests. The control effect can reach over 80% one day after treatment, and the control effect is still around 90% after 15 days of treatment. The composite insecticide provided by the present invention reduces the dosage and improves the control effect, which is of great significance for the comprehensive management of pests. DETAILED DESCRIPTION

[0027] To make the objectives, technical solutions, and advantages of the present invention more clear, the technical solutions of the present invention are described clearly and completely below. Obviously, the embodiments described are only some of the embodiments of the present invention, not all of them. All other embodiments derived by persons of ordinary skill in the art based on the embodiments of the present invention without inventive effort are within the scope of protection of the present invention.

[0028] Example 1

[0029] This example provides the toxicity effects of insecticides prepared from flufenacet and acephate in different ratios on fall armyworm. Specifically, the droplet method was used, with fall armyworm as the test object. The specific test steps are as follows:

[0030] The bioassay was conducted in accordance with the Agricultural Industry Standard of the People's Republic of China NY / T 1154.1-2006 "Guidelines for Indoor Bioassay Tests of Pesticides - Insecticides Part 1: Contact Activity Test - Spot Method", with slight adjustments made according to the actual test conditions. The specific steps are as follows:

[0031] The original drug was prepared into a mother liquor with acetone according to the proportion (the mass ratios of flufenacet:acephate were 1:0, 5:1, 2:1, 1:1, 1:2, 1:5, and 0:1, respectively), the volume of the mother liquor was 10 mL, and the concentration of the mother liquor was 5000 mg / L.

[0032] Dilute the stock solution with acetone to 5 to 7 working concentrations (10 mg / L, 5 mg / L, 2.5 mg / L, 1.25 mg / L, and 0.625 mg / L, respectively) as needed. Use a micropipette (Hamilton PB600-1) to drip 0.5 μL onto the pronotum of third-instar larvae (average weight approximately 0.005 g). Transfer the test larvae after dripping to a 24-well culture plate and feed them normally with sufficient artificial diet. Repeat the treatment three times for each group, with 10 larvae treated in each replicate. Larvae treated with acetone dripping served as a control. Check the results 48 hours after treatment. If the larvae do not respond when lightly touched with a brush, they are considered dead.

[0033] The data were statistically analyzed using POLO software (LeOra Software Inc., California, USA). A control mortality rate of less than 10% was considered valid and was corrected using the control mortality rate. The slope value of the toxicity regression line and its standard error SE and LD were calculated. 50 Values ​​and P values, etc.

[0034] The co-toxicity coefficient (CTC value) of the mixture was calculated using the Sun Yunpei method.

[0035] The percentage of agent A in the mixture = agent A content / (agent A content + agent B content) × 100%

[0036] Actual toxicity index (ATI) of mixture = LD of agent A 50 / LD of mixture 50 ×100

[0037] Theoretical Toxicity Index (TFI) of mixture = ATI(A) × percentage of agent A in the mixture + ATI(B) × percentage of agent B in the mixture

[0038] Co-toxicity coefficient (CTC) = actual toxicity index (ATI) of the mixture / theoretical toxicity index (TFI) of the mixture × 100

[0039] A co-toxicity coefficient ≥120 indicates a synergistic effect; a co-toxicity coefficient ≤80 indicates an antagonistic effect; and a co-toxicity coefficient between 80 and 120 indicates an additive effect.

[0040] Toxicity test results:

[0041] Table 1 Results of indoor toxicity tests of flufenacet and acephate against Spodoptera frugiperda larvae

[0042]

[0043] As shown in Table 1, compared with a single agent, when the weight ratio of flufenacet to acephate in the insecticidal composition was 1:1, 2:1 and 5:1, the co-toxicity coefficient was greater than 120, showing an obvious synergistic effect, which indicates that the composition has excellent insecticidal activity against fall armyworm.

[0044] Example 2

[0045] This experiment further tested the field efficacy of the compound pesticide formulation of the present invention against fall armyworm. The specific test object was fall armyworm. The test method was as follows:

[0046] The pesticide was applied during the corn bell stage. The fall armyworm was moderately infested, with a moderate insect population density and mostly young insects, which could meet the requirements of the field efficacy test. The experiment was arranged in random blocks with protected rows around. Each treatment was repeated 4 times and a water control was set. Each plot was 60m 2 Before spraying, the insect population was investigated by five-point sampling method. Ten plants were investigated at each point. A total of 50 corn plants were investigated in each plot and marked. A 3WBD-20 backpack electric sprayer was used for uniform spraying. Each treatment was carried out at a rate of 1000 plants per 667 m2. 2 Each plot was sprayed evenly with 40 kg of water per area. No other pesticides were used during the trial. The insect population was counted 1, 3, 7, and 14 days after application, and the insect population reduction rate and corrected control efficacy were calculated.

[0047]

[0048]

[0049] Preparation of experimental agent: A suspension concentrate (1:1) containing 22% of flubendiamide and acephate as the active ingredient of the composition was prepared. The suspension concentrate comprised 11% flubendiamide, 11% acephate, 6% sodium lignin sulfonate, 1% magnesium aluminum silicate, 4% ethylene glycol, 1% bentonite, 0.8% xanthan gum, and the weight was made up to 100% with deionized water.

[0050] The preparation method comprises a suspension concentrate (2:1) containing 30% of flubendiamide and acephate as the active ingredient of the composition, and the suspension concentrate comprises, based on the total weight of the suspension concentrate, 20% of flubendiamide, 10% of acephate, 7% of sodium lignin sulfonate, 1% of magnesium aluminum silicate, 4% of ethylene glycol, 4% of bentonite, 1% of xanthan gum, and deionized water to make up to 100%.

[0051] The preparation method comprises a suspension concentrate (5:1) containing 30% of flubendiamide and acephate as the active ingredient of the composition, and the suspension concentrate comprises, based on the total weight of the suspension concentrate, 25% of flubendiamide, 5% of acephate, 8% of sodium lignin sulfonate, 2% of magnesium aluminum silicate, 4% of ethylene glycol, 3% of bentonite, 0.8% of xanthan gum, and deionized water to make up the total weight to 100%.

[0052] Table 2 Field control efficacy of the compound pesticide formulation of the present invention against fall armyworm

[0053]

[0054] Table 2 shows that the field efficacy of a mixture of flufenacet and acephate against fall armyworm increases with increasing dosage. Furthermore, at the tested dose, the mixture was significantly more effective against fall armyworm than either flufenacet or acephate alone, demonstrating excellent rapidity and long-lasting efficacy. Because flufenacet and acephate have different mechanisms of action, their combined use can enhance control effectiveness, reduce pesticide dosage, and delay the development of pest resistance.

[0055] Example 3

[0056] This experiment further tested the field efficacy of the compound pesticide formulation of the present invention against the rice stem borer. The specific test object was the rice stem borer, and the test method was as follows:

[0057] This experiment selected the first generation of early rice stem borer. The experimental plots were flat and the water and fertilizer management was consistent. No other pesticides were applied before and during the experiment. The pesticides were applied in the evening. The experiment was arranged in random blocks with protected rows around the perimeter. Each treatment was replicated 4 times and a water control was set. Each plot was 30m 2 Before spraying, the insect population was investigated by using a five-point sampling method. Ten rice clumps were surveyed at each sampling point. A fixed-point and fixed-plant survey was conducted. A 3WBD-20 backpack electric sprayer was used for uniform spraying. Each treatment was carried out at a rate of 10000 tonnes per 667 m2. 2 Each plot was sprayed evenly with 30 kg of water per area. No other pesticides were used during the trial. The insect population was counted 1, 3, 7, and 14 days after application, and the insect population reduction rate and corrected control efficacy were calculated.

[0058]

[0059]

[0060] Preparation of experimental agent: A suspension concentrate (1:1) containing 22% of flubendiamide and acephate as the active ingredient of the composition was prepared. The suspension concentrate comprised 11% flubendiamide, 11% acephate, 6% sodium lignin sulfonate, 1% magnesium aluminum silicate, 4% ethylene glycol, 1% bentonite, 0.8% xanthan gum, and the weight was made up to 100% with deionized water.

[0061] The preparation method comprises a suspension concentrate (2:1) containing 30% of flubendiamide and acephate as the active ingredient of the composition, and the suspension concentrate comprises, based on the total weight of the suspension concentrate, 20% of flubendiamide, 10% of acephate, 7% of sodium lignin sulfonate, 1% of magnesium aluminum silicate, 4% of ethylene glycol, 4% of bentonite, 1% of xanthan gum, and deionized water to make up to 100%.

[0062] The preparation method comprises a suspension concentrate (5:1) containing 30% of flubendiamide and acephate as the active ingredient of the composition, and the suspension concentrate comprises, based on the total weight of the suspension concentrate, 25% of flubendiamide, 5% of acephate, 8% of sodium lignin sulfonate, 2% of magnesium aluminum silicate, 4% of ethylene glycol, 3% of bentonite, 0.8% of xanthan gum, and deionized water to make up the total weight to 100%.

[0063] Table 3 Field control efficacy of the compound pesticide formulation of the present invention against rice stem borer

[0064]

[0065] Table 3 shows that the field efficacy of a mixture of flufenacet and acephate against the rice stem borer increases with increasing dosage. Furthermore, at the tested dosage, the mixture was significantly more effective than either flufenacet or acephate alone, demonstrating excellent rapidity and long-lasting efficacy. Because flufenacet and acephate have different mechanisms of action, their combined use can enhance control effectiveness, reduce pesticide dosage, and delay the development of pest resistance.

[0066] In summary, the present invention utilizes effective amounts of the two active ingredients, flufenacet and acephate, to form a pesticide composition that exhibits significant synergistic effects. Compared to single agents, the resulting pesticide composition significantly improves the control of lepidopteran pests, particularly fall armyworm and rice stem borer. The insecticidal composition of the present invention has the advantages of a low dosage per unit dose, good rapidity of action, and a long-lasting effect. Furthermore, it is safe for the environment and crops, and has great potential for widespread use in agricultural production.

[0067] Finally, it should be noted that the above embodiments are only used to illustrate the technical solutions of the present invention, rather than to limit it. Although the present invention has been described in detail with reference to the aforementioned embodiments, those skilled in the art should understand that they can still modify the technical solutions described in the aforementioned embodiments, or make equivalent replacements for some of the technical features therein. However, these modifications or replacements do not deviate the essence of the corresponding technical solutions from the spirit and scope of the technical solutions of the various embodiments of the present invention.

Claims

1. A composition, characterized in that include: Flufenac and acephate; The mass ratio of flubendiamide to acephate is (1-5):

1.

2. An insecticide, characterized in that The insecticide comprises the composition of claim 1.

3. The insecticide according to claim 2, characterized in that The mass percentage of the composition in the insecticide is 15-40%.

4. The insecticide according to claim 3, characterized in that The mass percentage of the composition in the insecticide is 20-35%.

5. The insecticide according to claim 4, characterized in that In parts by weight, it comprises: 20-35 parts of the composition, 5-10 parts of sodium lignin sulfonate, 0.5-3 parts of magnesium aluminum silicate, 2-10 parts of ethylene glycol, 2-5 parts of bentonite and 0.5-5 parts of xanthan gum.

6. The method for preparing the insecticide according to claim 5, characterized in that: include: The components are mixed in proportion to prepare a suspension.

7. Use of the composition according to claim 1 or the insecticide according to any one of claims 2 to 5 in expanding the scope of killing pests, improving the control effect on pests or delaying the resistance of pests.

8. The use according to claim 7, characterized in that The pests include one or more of leaf-feeding pests, piercing-sucking pests, underground pests or boring pests.

9. The use according to claim 7, characterized in that The pests are lepidopteran pests selected from fall armyworm, corn borer, rice stem borer, diamondback moth, armyworm, aphid, cotton bollworm, thrips, leafhopper or tobacco budworm.

Citation Information

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