Bactericidal composition containing bixafen and application thereof

By screening the emulsifier formula, microemulsions of biphenopyramidine, piperazole or propionazole were prepared, which solved the shortcomings of pesticide preparations in the prior art in terms of environmental friendliness and prevention and treatment effects, and achieved efficient and economical prevention and treatment effects.

CN119908362AActive Publication Date: 2025-05-02SHANGHAI SHENGNONG PESTICIDE

Patent Information

Application Number
CN202510085903.2
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2025-01-20
Publication Date
2025-05-02
Estimated Expiration
2045-01-20

AI Technical Summary

Technical Problem

The lack of research on the preparation of microemulsions for the compound preparation of biphenopyramidine and piperazole or propionazole in the prior art has led to insufficient environmental friendliness and prevention and treatment effects of pesticide preparations.

Method used

Through systematic screening of emulsifiers, a microemulsion formula with simple formula composition and low emulsifier usage is obtained. The specific ingredients include biphenopyramidine, piperazole or propionazole, Termul 5030, Atlox 4912, ethylene glycol and cyclohexanone, forming excellent preparation performance.

Benefits of technology

The emulsifier compounding reduces the amount of emulsifier, reduces production costs, and improves the stability and prevention and treatment effect of microemulsions, which has excellent prevention and treatment effect on wheat gibberellia.

✦ Generated by Eureka AI based on patent content.

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Patent Text Reader

Abstract

The invention belongs to the field of pesticide preparations, and particularly relates to a bactericidal composition containing bixafen and application of the bactericidal composition. The bixafen bactericidal composition comprises the following components in percentage by weight: 3-10% of bixafen, 5-20% of triazole bactericide, 8-12% of Termul 5030, 1-3% of Atlox 4912, 1-5% of ethylene glycol, 13-18% of cyclohexanone and the balance of deionized water, wherein the total percentage is 100%. And the triazole bactericide is tebuconazole or prothioconazole. The microemulsion prepared by the invention has excellent preparation performance, and the emulsifier is compounded, so that compact micelles can be formed, the solubilizing amount can be increased, the dosage of the emulsifier can be reduced, the production cost can be reduced, and the microemulsion has an excellent prevention and treatment effect on wheat scab.
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Description

Technical Field

[0001] The invention belongs to the field of pesticide preparations, and particularly relates to a fungicide composition comprising bixafen and an application thereof. Background Art

[0002] Bixafen is a pathogen respiration inhibitor that inhibits mitochondrial function by interfering with the tricarboxylic acid cycle on complex II of the respiratory electron transport chain, preventing them from producing energy, inhibiting the growth of pathogens, and ultimately leading to their death. Bixafen has a broad bactericidal spectrum and has both preventive and therapeutic effects, and can inhibit spore germination, hyphae growth, and spore formation.

[0003] Tebuconazole is a systemic triazole fungicide pesticide. It is a sterol demethylation inhibitor that can inhibit the demethylation of ergosterol on the bacterial cell membrane, making it impossible for the bacteria to form a cell membrane, thereby killing the bacteria; prothioconazole is a triazolethione fungicide, a sterol demethylation (biosynthesis of ergosterol) inhibitor, with selectivity, protection, and therapeutic properties.

[0004] CN201510991965.6 discloses a fungicide composition containing bixafen and prothioconazole, characterized in that the fungicide composition contains bixafen and prothioconazole as main active ingredients, wherein the mass ratio of bixafen to prothioconazole is 1-70:1-50. It has a high synergistic effect, overcomes and delays the drug resistance of pathogens, has a fast sterilization speed, a long lasting effect, reduces the application cost, and has a significantly better control effect than its single-dose use. CN201610353890.3 discloses a fungicide composition containing bixafen and tebuconazole and its application. The fungicide composition contains bixafen and tebuconazole as main active ingredients, wherein the mass ratio of bixafen to tebuconazole is 1-70:1-50. It has a high synergistic effect, overcomes and delays the drug resistance of pathogens, has a fast sterilization speed, a long lasting effect, reduces the application cost, and the prevention and control effect is significantly better than its single-dose use. The above patent documents do not conduct research on preparations.

[0005] Pesticide microemulsion (ME) is a new pesticide formulation developed in the 1970s. It is a transparent single-phase liquid preparation with water as the dispersion medium, no or only a small amount of organic solvent, and an appropriate amount of surfactant and other adjuvants. Microemulsion replaces a large amount of organic solvent with water, which reduces the pressure on the environment during the production process and after application of the agent. It is an environmentally friendly pesticide formulation. Microemulsion is a thermodynamically stable, transparent and isotropic dispersion system spontaneously formed by two immiscible liquids. It has the characteristics of good physical stability, long shelf life, strong diffusion and penetration ability, and high biological activity.

[0006] There is no related research report on preparing microemulsion by compounding bixafen and tebuconazole or prothioconazole in the existing literature. The present invention systematically screens emulsifiers to obtain a microemulsion formula with simple formula composition and low emulsifier usage, and at the same time verifies the field control effect of the microemulsion. Summary of the invention

[0007] The present invention provides a fungicide composition containing bixafen and its application, and the specific technical scheme is as follows:

[0008] A fungicide composition containing bixafen, comprising the following components in percentage by weight: 3-10% of bixafen, 5-20% of a triazole fungicide, 8-12% of Termul 5030, 1-3% of Atlox 4912, 1-5% of ethylene glycol, 13-18% of cyclohexanone, and deionized water to make up to 100%; the triazole fungicide is tebuconazole or prothioconazole.

[0009] The present invention provides a fungicide composition, comprising the following components in percentage by weight: 4-8% of bixafen, 10-15% of a triazole fungicide, 8-12% of Termul 5030, 1-3% of Atlox4912, 1-5% of ethylene glycol, 13-18% of cyclohexanone, and deionized water to make up to 100%;

[0010] The invention provides a bactericidal composition, comprising the following components in percentage by weight: 5% of bixafen, 10% of a triazole bactericide, 10% of Termul 5030, 2% of Atlox 4912, 3% of ethylene glycol, 15% of cyclohexanone, and deionized water to make up to 100%.

[0011] The fungicide composition of the present invention is used for preventing and controlling diseases of gramineous crops, and preferably the disease is wheat scab.

[0012] Compared with the prior art, the present invention has the following beneficial effects:

[0013] Compared with a single emulsifier, a compound emulsifier can not only form dense micelles and increase the solubilization amount, but also reduce the amount of emulsifier used and reduce production costs.

[0014] Both prothioconazole and tebuconazole are triazole fungicides with similar physical and chemical properties. The bixafen-prothioconazole microemulsion prepared using the same microemulsion adjuvant formula also has excellent formulation performance. DETAILED DESCRIPTION

[0015] The present invention can be better understood according to the following examples. However, it is easy for those skilled in the art to understand that the contents described in the examples are only used to illustrate the present invention, and should not and will not limit the present invention described in detail in the claims.

[0016] Example 1: Preparation of 15% Bixafen and Tebuconazole Microemulsion

[0017] Materials and Methods

[0018] Drugs: bifenthion, tebuconazole, Termul 5030, Nongru 600#, EL-40, EthylanNS-500LQ, NP-10, Atlox 4912, cyclohexanone, ethanol; all were purchased from the market.

[0019] Preparation method of microemulsion: dissolve the original drug with appropriate solvent cyclohexanone, then add co-solvent ethanol, and after fully dissolving, add surfactant and mix evenly, add water dropwise while stirring to transform the system from oil-in-water phase to water-in-oil phase to obtain microemulsion. Analyze the preparation effect of adding different emulsifiers to determine the best emulsifier formula.

[0020] Index performance test method:

[0021] Emulsion stability: refer to GB / T 1601-2001 "Test method for stability of pesticide emulsion";

[0022] pH value determination: refer to GB / T 1601-1993 "Determination of pH of pesticides";

[0023] Transparent temperature range: Take 10mL of homemade microemulsion in a 25mL test tube and gradually cool it down in a low-temperature bath until it becomes turbid or frozen. This turning temperature point is the lower limit of transparent temperature T1. Then place the test tube in a water bath and heat it at a rate of 2℃ / min. Record the temperature when turbidity appears as the upper limit of transparent temperature T2. The transparent temperature range is T1-T2.

[0024] Hot storage and cold storage stability test: The microemulsion was stored at (54±2)℃ for 14 days and (0±2)℃ for 7 days, and then various indicators were tested.

[0025] Test results:

[0026] Emulsifier screening

[0027] Emulsifier is an important component of microemulsion and plays a key role in the formation and stabilization of microemulsion. Emulsifier molecules are usually composed of hydrophilic and lipophilic groups, which assemble into micelles of various shapes in aqueous solution, thereby solubilizing hydrophobic substances into aqueous media. First, the amount of emulsifier in the formula is set to 20%, and it is fully mixed with the cosolvent and solvent containing the original drug, and water is added to make up the balance. Observe whether the resulting solution is clear and transparent, and carry out hot storage and cold storage stability tests at the same time, and record the test results after hot storage for 14 days and cold storage for 7 days respectively.

[0028] As can be seen from Table 1, the microemulsions prepared using emulsifiers Termul 5030, Nongru 600# and Atlox 4912 can all form clear and transparent solutions. In the transparent temperature range test, Termul 5030 and Atlox 4912 have higher upper limits of transparent temperature, so Termul 5030 and Atlox 4912 are selected as alternative emulsifiers for microemulsions.

[0029] Table 1 Emulsifier type screening

[0030] Emulsifier Initial appearance Appearance after hot storage Appearance after cold storage Transparent temperature limit Termul 5030 Clarity and transparency Clarity and transparency Clarity and transparency 70 Agricultural milk 600# Clarity and transparency Clarity and transparency Clarity and transparency 50 EL-40 Clarity and transparency White translucent A small amount of crystals precipitated - EthylanNS-500LQ White turbidity - - - NP-10 White turbidity - - - Atlox 4912 Clarity and transparency Clarity and transparency Clarity and transparency 65

[0031] The alternative emulsifiers Termul 5030 and Atlox 4912 were set at 18%, 15%, 12% and 10% as gradients, and the stability at room temperature, hot storage and cold storage was tested respectively. As can be seen from Table 2, when the emulsifier dosage is the same, the performance of the microemulsion prepared by Termul 5030 is better than that of Atlox 4912, so Termul 5030 is selected as the main emulsifier of the microemulsion, and Atlox 4912 is used as the auxiliary emulsifier of the microemulsion.

[0032] Table 2 Emulsifier content screening

[0033]

[0034]

[0035] As can be seen from Table 3, the microemulsion prepared when the emulsifier Termul 5030 + Atlox 4912 content is (8:1) 15%, (5:1) 15%, (5:1) 12% has better performance, and the formula with the least amount of emulsifier is selected as the emulsifier of the present invention. Compared with a single emulsifier, the compound emulsifier can not only form dense micelles and increase the solubilization amount, but also reduce the amount of emulsifier and reduce the production cost.

[0036] Table 3 Emulsifier compound screening

[0037]

[0038] By screening solvents and emulsifiers, a 15% bixafen and tebuconazole microemulsion was obtained, which contained the following weight percentage components: 5% bixafen, 10% tebuconazole, 10% Termul5030, 2% Atlox 4912, 3% ethylene glycol, 15% cyclohexanone, and deionized water to make up 100%. The quality indicators were tested and the performance indicators were qualified.

[0039] Table 4 Microemulsion performance index measurement results

[0040] project Measurement results Emulsion stability No oil, no sediment Dispersion Quick dispersion, transparent appearance pH 7.02 Cold storage stability qualified Thermal storage stability qualified

[0041] Example 2: Test on the efficacy of bixafen and tebuconazole or prothioconazole microemulsion against wheat scab

[0042] Test object: wheat fusarium wilt.

[0043] Test drug:

[0044] Agent 1: 15% bixafen and tebuconazole microemulsion in Example 1;

[0045] Agent 2: 15% bixafen·prothioconazole microemulsion (bixafen 5%, prothioconazole 10%, Termul 5030 10%, Atlox 4912 2%, ethylene glycol 3%, cyclohexanone 15%, deionized water to 100%; microemulsion performance indicators qualified)

[0046] Test method: The soil fertility of the test field was medium, and the previous crop was corn. The test set up a treatment group and a control group. The pesticide was sprayed at the heading stage of wheat (more than 50% of the wheat head emerged), and the control was sprayed with the same amount of water. The specific spraying dosage is shown in the table below. The test was arranged in random blocks, repeated 4 times, and the area of ​​the plot was 50m 2 .

[0047] Disease investigation methods and standards: In the late stage of wheat filling, samples were taken in each plot using the five-point sampling method, with 100 plants selected at each point. The disease status of each ear was investigated and the control effect was calculated.

[0048] Grading standards for severity of wheat fusarium rust:

[0049] Level 0, the whole ear is disease-free;

[0050] Level 1: diseased spikelets account for less than 25% of the whole spike;

[0051] Level 3: diseased spikelets account for 26% to 50% of the whole spike;

[0052] Level 5: diseased spikelets account for 51% to 75% of the whole spike;

[0053] Level 7: diseased spikelets account for more than 75% of the whole spike.

[0054] Disease index = [Σ(number of diseased ears at each level × corresponding disease level) / (total number of ears surveyed × 7)] × 100

[0055] Control effect = [(disease index of control area - disease index of treated area) / disease index of control area] × 100%;

[0056] Test results

[0057] It can be seen from Table 5 that the microemulsion of the present invention has an excellent control effect on wheat fusarium head blight.

[0058] Table 5 Test on the efficacy of bixafen and triazole compound microemulsion against wheat fusarium head blight

[0059] deal with Active ingredient dosage g / mu Effectiveness% Potion 1 8 98.8 Potion 2 10 97.5 CK - -

[0060] The above description is only a preferred embodiment of the present invention. For those skilled in the art, appropriate improvements can be made without departing from the raw materials of the present invention, and these improvements are also within the scope of protection of the present invention.

Claims

1. A fungicidal composition comprising bixafen, characterized in that: The invention comprises the following components in percentage by weight: 3-10% of bixafen, 5-20% of a triazole fungicide, 8-12% of Termul 5030, 1-3% of Atlox 4912, 1-5% of ethylene glycol, 13-18% of cyclohexanone, and deionized water to make up to 100%; the triazole fungicide is tebuconazole or prothioconazole.

2. The bactericidal composition according to claim 1, characterized in that The invention comprises the following components in percentage by weight: 4-8% of bixafen, 10-15% of triazole fungicide, 8-12% of Termul 5030, 1-3% of Atlox 4912, 1-5% of ethylene glycol, 13-18% of cyclohexanone, and deionized water to make up to 100%.

3. The bactericidal composition according to claim 2, characterized in that Bixafen 5%, triazole fungicide 10%, Termul 5030 10%, Atlox 4912 2%, ethylene glycol 3%, cyclohexanone 15%, deionized water to make up 100%.

4. Use of the fungicidal composition according to any one of claims 1 to 3 for preventing and controlling diseases of gramineous crops.

5. The use according to claim 4, characterized in that The disease is wheat fusarium rust.

Citation Information

Patent Citations

  • Bixafen and prothioconazole containing bactericidal composition and application thereof

    CN105766933A

  • Sterilizing composition containing bixafen and tebuconazole and application thereof

    CN105941416A

  • Pesticide composition and application thereof

    CN107318850A

  • Weeding composition containing butachlor, metamifop and clomazone and application thereof

    CN117770251A

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