Composition containing meconazole, ethirimol and derivatives of meconazole and ethirimol

Abstract

The invention discloses a composition containing meconazole, ethirimol and derivatives thereof, relates to the technical field of pesticide bactericides, and is used for solving the problems that the dosage is large when the existing composition containing meconazole, ethirimol and bupirimate is independently used, and related reports are not reported when the components are mutually compounded. The composition is prepared by reasonably compounding an active component A, namely the meconazole, and an active component B, namely the ethirimol or a derivative of the ethirimol, the composition is applied to crops, the composition is absorbed by the crops after application, disease control can be performed on the crops through two action mechanisms at the same time, the synergistic and persistent effects are good, the control effect is higher than that of a single agent, the pesticide dosage can be remarkably reduced, the residual amount of the pesticide on the crops is reduced, and environmental pollution is relieved; and moreover, the generation of drug resistance of diseases can be effectively avoided, the action duration of the composition is prolonged, the bactericidal spectrum is expanded, and a good prevention and treatment effect is achieved.

Description

Technical Field

[0001] The invention relates to the technical field of pesticide fungicides, and in particular to a composition containing clofoconazole, pyrifos and derivatives thereof. Background Art

[0002] With the widespread use of chemical control, the resistance of plant pathogenic fungi to single fungicides has shown a rapid upward trend. For example, pathogens such as Botrytis cinerea and powdery mildew have shown resistance to mainstream fungicides such as succinate dehydrogenase inhibitors and pyrimidines through gene mutations or changes in metabolic pathways, and the frequency of resistance has exceeded 60%. The spread of this resistance has led to a decline in field control efficacy and an increase in the cost of using drugs.

[0003] As a new succinate dehydrogenase inhibitor, clofoconazole has excellent efficacy against ascomycete diseases such as powdery mildew and rust. However, long-term single use can cause mutations in the SDH gene of some strains (such as the wheat fusarium spore).

[0004] Ethiopyrimidine, a pyrimidine fungicide, primarily works by inhibiting adenine synthesis. However, it has a narrow spectrum of activity, with limited efficacy against imperfect fungi such as gray mold. Furthermore, single-dose use can easily induce multidrug resistance in pathogens. Ethiopyrimidine sulfonate is a highly effective, low-toxic, systemic fungicide from the pyrimidine class that comprehensively controls powdery mildew development by inhibiting spore formation, demonstrating significant control effectiveness against a wide range of crops.

[0005] In the actual process of agricultural production, the most common problem in preventing and controlling diseases is the development of disease resistance. Compounding different ingredients is a very common method for preventing and controlling resistant diseases. Compounding different ingredients is often used to determine whether a particular compound has a synergistic, additive, or antagonistic effect based on actual application results. In most cases, the compounding effect of pesticides is additive, with few compounds showing a truly synergistic effect, and even fewer with very significant synergistic effects and high synergistic ratios. Research by the inventors has revealed that compounding cyfluthrin with pyrimidine or pyrimidine sulfonate has a good synergistic effect within a certain range. However, there are currently no reports on compounding cyfluthrin with pyrimidine or pyrimidine sulfonate, either domestically or internationally.

[0006] Therefore, it is of great significance to develop a composition containing clofoconazole, pyrifos and its derivatives. Summary of the Invention

[0007] In order to overcome the above technical problems, the purpose of the present invention is to provide a composition containing chlorfluanidazole and pyrifos and their derivatives, which solves the problems that the existing chlorfluanidazole, pyrifos and pyrifos sulfonate require large dosages when used alone, and there are no reports on their combination.

[0008] The purpose of the present invention can be achieved through the following technical solutions:

[0009] A composition containing clofoconazole, pyrifos and derivatives thereof, comprising 1 to 90% by weight of active ingredients and the remainder being auxiliary materials;

[0010] Among them, the active ingredients include active ingredient A and active ingredient B;

[0011] Wherein, the weight ratio of active ingredient A to active ingredient B is 1:60 to 60:1;

[0012] Among them, the active ingredient A is clofoconazole;

[0013] The active ingredient B is ethidol or a derivative of ethidol; wherein the derivative of ethidol is ethidol sulfonate.

[0014] As a further solution of the present invention: the weight ratio of the active ingredient A to the active ingredient B is 1:40 to 40:1.

[0015] As a further solution of the present invention: the weight ratio of the active ingredient A to the active ingredient B is 1:2.

[0016] As a further embodiment of the present invention, the dosage form of the composition includes but is not limited to wettable powder, soluble liquid, emulsifiable concentrate, aqueous emulsion, microemulsion, suspoemulsion, suspension, microcapsule suspension, dispersible oil suspension, and water-dispersible granules.

[0017] As a further embodiment of the present invention: the dosage form of the composition is water-dispersible granules, and the excipients include a dispersant, a wetting agent, a disintegrant, a binder and a filler; wherein the dispersant is one of polycarboxylate super-efficient dispersant SP-2888 and polycarboxylate super-efficient dispersant SP-2852; wherein the wetting agent is sodium lauryl sulfate; wherein the disintegrant is one of sodium carbonate and sodium bicarbonate; wherein the binder is starch; wherein the filler is one of white carbon black and high clay.

[0018] As a further embodiment of the present invention: the dosage form of the composition is a suspension, and the excipients include a dispersing emulsifier, a wetting agent, a defoaming agent, a thickener, an antifreeze agent and deionized water; wherein the dispersing emulsifier is one of dispersing emulsifier 601A and dispersing emulsifier SC-0204C; wherein the wetting agent is one of sodium lauryl sulfate and sodium dodecylbenzene sulfonate; wherein the defoaming agent is silicone oil; wherein the thickener is methyl cellulose; wherein the antifreeze agent is glycerol.

[0019] As a further solution of the present invention: the dosage form of the composition is a dispersible oil suspension, and the excipients include an emulsifier and methyl oleate; wherein the emulsifier is one of the dispersing emulsifier SP-OF3473 and the dispersing emulsifier SP-OF3498D.

[0020] As a further embodiment of the present invention: the composition containing clofoconazole, pyrifos and derivatives thereof is used for preventing and controlling crop diseases.

[0021] As a further embodiment of the present invention: the disease is powdery mildew.

[0022] Beneficial effects of the present invention:

[0023] The present invention discloses a composition containing clofoconazole, ethylpyrifos and derivatives thereof. The composition is prepared by rationally compounding clofoconazole, ethylpyrifos and derivatives thereof, and then the composition is applied to crops. After application, the composition is absorbed by the crops and can simultaneously prevent and control crop diseases through two mechanisms of action. The composition has excellent synergistic and long-lasting effects, and the prevention effect is higher than that of a single dose. The amount of pesticide used can be significantly reduced, the amount of pesticide residues on crops can be reduced, and environmental pollution can be alleviated. Furthermore, the compounding can effectively avoid the development of drug resistance in diseases, prolong the action time of the composition, expand the fungicidal spectrum, have high activity against powdery mildew, and have good prevention and control effects. DETAILED DESCRIPTION

[0024] The following will be combined with the embodiments of the present invention to clearly and completely describe the technical solutions in the embodiments of the present invention. Obviously, the embodiments described are only part of the embodiments of the present invention, not all of the embodiments. Based on the embodiments of the present invention, all other embodiments obtained by ordinary technicians in this field without making any creative efforts shall fall within the scope of protection of the present invention.

[0025] Application Example 1

[0026] The dosage forms of Examples 1 to 6 are water-dispersible granules. The specific preparation method of a composition containing clofoconazole, pyrifos and its derivatives is as follows:

[0027] The clofoconazole, pyrifos or pyrifos sulfonate, dispersant, wetting agent, disintegrant, binder and filler are uniformly mixed, and the particles are pulverized by air flow to obtain the required particle size to obtain granulation material. The granulation material is then quantitatively fed into a fluidized bed, granulated and dried by a granulation dryer to obtain the product.

[0028] The specific formulas of Examples 1 to 6 are shown in the following table:

[0029]

[0030] Application Example 2

[0031] The dosage forms of Examples 7 to 12 are suspension concentrates. The specific preparation method of a composition containing clofoconazole, pyrifos and its derivatives is as follows:

[0032] The preparation method is prepared by uniformly mixing clofoconazole, pyrifos or pyrifos sulfonate, a dispersing emulsifier, a wetting agent, a defoaming agent, a thickener and an antifreeze agent, making up the balance to 100% with deionized water, and milling the mixture in a ball mill for 3 hours to control the particle size to 5 μm.

[0033] The specific formulas of Examples 7 to 12 are shown in the following table:

[0034]

[0035] Application Example 3

[0036] The dosage forms of Examples 13 to 18 are dispersible oil suspensions. The specific preparation method of a composition containing clofoconazole, pyrifos and its derivatives is as follows:

[0037] The preparation method is prepared by uniformly mixing clofoconazole, pyrifos or pyrifos sulfonate and an emulsifier, and making up the balance to 100% with methyl oleate, and milling the mixture in a ball mill for 3 hours to control the particle size to 5 μm.

[0038] The specific formulations of Examples 13 to 18 are shown in the following table:

[0039]

[0040] The toxicity of the composition against grape powdery mildew was tested indoors, and the synergistic ratio (SR) of active ingredient A and active ingredient B after compounding in a certain proportion was calculated according to the Wadley method. SR < 0.5 indicates antagonism, 0.5 ≤ SR ≤ 1.5 indicates additive effect, and SR > 1.5 indicates synergistic effect. On this basis, field tests were conducted, in which the composition was diluted 2000 times with water. The dosage of the composition was 10 g / mu / time. The first application was made at the early stage of the disease, and the application was continued every 7 days, for a total of 2 applications. The disease prevention efficacy was investigated 7 and 14 days after the last application.

[0041] The experimental results are shown below:

[0042]

[0043] According to the above data, it can be seen that the combination of active ingredient A and active ingredient B shows a synergistic effect in controlling grape powdery mildew. When the ratio of active ingredient A to active ingredient B is between 1:20 and 20:1, the synergistic effect is more prominent, and the synergistic ratio is above 2.2.

[0044] The experiments showed that the optimal ratios were 1:20 for clofluconazole and thiamethoxam, 1:10 for clofluconazole and thiamethoxam, 1:2 for clofluconazole and thiamethoxam, 20:1 for clofluconazole and thiamethoxam, 1:20 for clofluconazole and thiamethoxam, and 1:30 for clofluconazole and thiamethoxam. In particular, when the ratio of clofluconazole and thiamethoxam was 1:2, the synergistic ratio was the largest and the protective effect was the most obvious.

[0045] Experiments have shown that the combination of clofoconazole and active ingredient B has a control effect of over 97% on powdery mildew on various crops, which is better than the control effect of a single agent and has a significant synergistic effect.

[0046] Throughout this specification, references to terms such as "one embodiment," "example," or "specific example" indicate that the specific features, structures, materials, or characteristics described in conjunction with that embodiment or example are included in at least one embodiment or example of the present invention. In this specification, schematic representations of these terms do not necessarily refer to the same embodiment or example. Furthermore, the specific features, structures, materials, or characteristics described may be combined in any suitable manner in any one or more embodiments or examples.

[0047] The above contents are merely examples and explanations of the present invention. Those skilled in the art may make various modifications or additions to the described specific embodiments or replace them in similar ways. As long as they do not deviate from the invention or exceed the scope defined in this application, they should all fall within the scope of protection of the present invention.

Claims

1. A composition containing clofoconazole, pyrifos and derivatives thereof, characterized in that: It contains 1 to 90% active ingredients by weight, and the rest are excipients; Among them, the active ingredients include active ingredient A and active ingredient B; Wherein, the weight ratio of active ingredient A to active ingredient B is 1:60 to 60:1; Among them, the active ingredient A is clofoconazole; The active ingredient B is ethidol or a derivative of ethidol; wherein the derivative of ethidol is ethidol sulfonate.

2. A composition containing clofoconazole, pyrifos and derivatives thereof according to claim 1, characterized in that: The weight ratio of the active ingredient A to the active ingredient B is 1:40 to 40:

1.

3. A composition containing clofoconazole, pyrifos and derivatives thereof according to claim 2, characterized in that: The weight ratio of the active ingredient A to the active ingredient B is 1:

2.

4. A composition containing clofoconazole, pyrifos and derivatives thereof according to claim 1, characterized in that: The dosage form of the composition includes, but is not limited to, wettable powder, soluble liquid, emulsifiable concentrate, aqueous emulsion, microemulsion, suspoemulsion, suspension, microcapsule suspension, dispersible oil suspension, and water-dispersible granules.

5. A composition containing clofoconazole, pyrifos and derivatives thereof according to claim 4, characterized in that: The dosage form of the composition is water-dispersible granules, and the excipients include a dispersant, a wetting agent, a disintegrant, a binder, and a filler; wherein the dispersant is one of polycarboxylate super-efficient dispersant SP-2888 and polycarboxylate super-efficient dispersant SP-2852; wherein the wetting agent is sodium lauryl sulfate; wherein the disintegrant is one of sodium carbonate and sodium bicarbonate; wherein the binder is starch; and wherein the filler is one of white carbon black and high clay.

6. A composition containing clofoconazole, pyrifos and derivatives thereof according to claim 4, characterized in that: The dosage form of the composition is a suspension, and the excipients include a dispersing emulsifier, a wetting agent, a defoaming agent, a thickener, an antifreeze agent and deionized water; wherein the dispersing emulsifier is one of dispersing emulsifier 601A and dispersing emulsifier SC-0204C; wherein the wetting agent is one of sodium lauryl sulfate and sodium dodecylbenzene sulfonate; wherein the defoaming agent is silicone oil; wherein the thickener is methyl cellulose; wherein the antifreeze agent is glycerol.

7. The composition containing clofoconazole, pyrifos and derivatives thereof according to claim 4, characterized in that: The dosage form of the composition is a dispersible oil suspension, and the auxiliary materials include an emulsifier and methyl oleate; wherein the emulsifier is one of the dispersing emulsifier SP-OF3473 and the dispersing emulsifier SP-OF3498D.

8. Use of the composition containing clofoconazole, pyrifos and derivatives thereof according to claim 1 for preventing and controlling crop diseases.

9. The use according to claim 8, characterized in that The disease is powdery mildew.

Images