CN111405848A - Stable agrochemical compositions and methods thereof - Google Patents
Stable agrochemical compositions and methods thereof Download PDFInfo
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- CN111405848A CN111405848A CN201880049879.5A CN201880049879A CN111405848A CN 111405848 A CN111405848 A CN 111405848A CN 201880049879 A CN201880049879 A CN 201880049879A CN 111405848 A CN111405848 A CN 111405848A
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- active ingredient
- additive
- agrochemical composition
- melting point
- low melting
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- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N25/00—Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests
- A01N25/08—Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests containing solids as carriers or diluents
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- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N37/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids
- A01N37/44—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing at least one carboxylic group or a thio analogue, or a derivative thereof, and a nitrogen atom attached to the same carbon skeleton by a single or double bond, this nitrogen atom not being a member of a derivative or of a thio analogue of a carboxylic group, e.g. amino-carboxylic acids
- A01N37/50—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing at least one carboxylic group or a thio analogue, or a derivative thereof, and a nitrogen atom attached to the same carbon skeleton by a single or double bond, this nitrogen atom not being a member of a derivative or of a thio analogue of a carboxylic group, e.g. amino-carboxylic acids the nitrogen atom being doubly bound to the carbon skeleton
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- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N53/00—Biocides, pest repellants or attractants, or plant growth regulators containing cyclopropane carboxylic acids or derivatives thereof
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- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N57/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic phosphorus compounds
- A01N57/26—Biocides, pest repellants or attractants, or plant growth regulators containing organic phosphorus compounds having phosphorus-to-nitrogen bonds
- A01N57/28—Biocides, pest repellants or attractants, or plant growth regulators containing organic phosphorus compounds having phosphorus-to-nitrogen bonds containing acyclic or cycloaliphatic radicals
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- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N2300/00—Combinations or mixtures of active ingredients covered by classes A01N27/00 - A01N65/48 with other active or formulation relevant ingredients, e.g. specific carrier materials or surfactants, covered by classes A01N25/00 - A01N65/48
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- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N25/00—Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests
- A01N25/12—Powders or granules
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- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N25/00—Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests
- A01N25/22—Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests containing ingredients stabilising the active ingredients
Abstract
The present invention discloses an agrochemical composition comprising at least one low melting point active ingredient; at least one moisture sensitive active ingredient; and an additive, characterized in that the additive has a softening or melting point lower than the melting point of the low-melting active ingredient; methods of making the same, methods of using the same, and kits comprising the agrochemical compositions.
Description
Technical Field
The present invention relates to stable agrochemical compositions. The present invention more particularly relates to stable agrochemical compositions comprising a low melting point active ingredient and a moisture sensitive active ingredient.
Background and Prior Art
Physically compatible agrochemical mixtures exhibit better pest management. These mixtures show several advantages compared to when applied alone. However, achieving physical compatibility becomes a major challenge when combining two or more agrochemicals. The problem of physical compatibility is further exacerbated when a low melting active ingredient needs to be formulated with another active ingredient.
Some of the low melting active ingredients, such as pyrethroids (pyrethroids), are known to control agricultural pests on crops. Pyrethroids interfere with the ionic conductance of neurons by prolonging sodium current. This stimulates repeated discharges from the nerves, resulting in over-excitation of the poisoned animal.
Active ingredients with pest control ability selected from fungicides such as strobilurins and insecticides such as organophosphates are advantageously co-formulated with low melting point actives to better control pests. Some of these active ingredients are moisture sensitive and therefore degrade rapidly when processed into suitable formulations or compositions.
Moisture sensitive active ingredients such as acephate (organophosphate) are systemic and contact insecticides with moderate persistence, with residual activity lasting about 10-15 days. Acephate is highly susceptible to moisture and is not very stable in conventional insecticidal formulations, whereby severe decomposition of acephate in conventional formulations occurs depending on storage conditions, and therefore, the insecticidal activity of acephate is sometimes not fully utilized.
While it is advantageous to co-formulate moisture sensitive active ingredients with low melting point active ingredients to better control pests, it is challenging to develop stable and effective formulations.
There are a large number of low-melting active ingredient formulations used to combat attack on plants by pests. Useful formulations include Emulsion Concentrates (EC), aqueous Emulsions (ES). However, these formulations cannot be prepared when the other active ingredient is moisture sensitive and readily exposed to water.
Dry particulate formulations of low melting active ingredients such as pyrethroids, such as water dispersible granules, are known and in practice. Conventional methods for preparing granules include methods such as extrusion granulation, in which water is used to prepare an agglomerate, which is then granulated. Another method of preparing granules is to prepare a slurry in water and then spray-dry it.
This is a challenge when low melting ingredients (such as pyrethroids) must be mixed with moisture sensitive ingredients (such as organophosphates) in the premix, as moisture sensitive ingredients cannot be granulated using water. Furthermore, the temperature increase during extrusion granulation can melt the low melting point active. Once the granules are extruded and maintained at ambient conditions, the low melting active becomes solid again. This solid-liquid-solid phase transition leads to a change in morphology, which leads to a change in the crystal form, or a layering of components on the surface of the granule or a hardening of the granule. When applied in the field by dilution/tank mixing, such granular compositions produce an unsatisfactory uneven dissolution (dispersion) of the mixture and lack homogeneity in the resulting mixture, and prevent the distribution of a constant concentration of the desired active in the field. The lack of a desirable means of dispersion will reduce the availability of the active ingredient for its intended use as a pesticide, rendering the product ineffective.
Another method for preparing a premix of such ingredients is to dissolve the low melting ingredient in a suitable solvent and then mix it with the moisture sensitive ingredients and then pelletize. This process requires the use of large amounts of organic solvents, which are not only expensive but also environmentally unfriendly. It may be necessary to subject the granules to a longer drying period in order to remove traces of solvent from the final product.
WO2015142609 a1 discloses microparticles comprising a water-soluble organic phosphorothioate (e.g. acephate) and a pyrethroid (e.g. bifenthrin). The present invention provides effective odor control solutions by adding odor absorbing and odor masking components.
US20090208423 discloses synergistic pesticidal compositions comprising imidacloprid, lambda-cyhalothrin and conventional agriculturally acceptable carriers or excipients formulated as aqueous or dry-based formulations. The application also discloses a process for mixing the active substance and excipients to obtain a homogeneous mixture of all ingredients, which is micronized and granulated to produce a granular formulation. Although this process is acceptable, micronization of inert fillers in which the liquid active is absorbed can cause several problems because the liquid naturally tends to run off during fine grinding. Such compositions obtained generally do not exhibit good dispersibility and shelf life, especially because low melting point actives undergo phase changes during ambient storage temperatures (-5 ℃ to 50 ℃), resulting in caking and crystal growth.
Indian patent application No. 1709/MUM/2010 discloses synergistic insecticidal compositions of acephate and bifenthrin, wherein a bifenthrin technical dissolved in a solubilizer is sprayed onto a mixture of acephate technical and formulation aids to obtain granules. The problem with this approach is that bifenthrin requires a large amount of solubilizer to impart softness to the finished granules. In this case, a high loading of active ingredient is not possible due to the undesirable softness of the granules.
WO2002076213 a1 discloses an insecticidal composition comprising a specific pyrethroid selected from deltamethrin, fenvalerate, esfenvalerate, cyfluthrin, β -cyfluthrin and bifenthrin in a weight ratio of 50:1 to 1:5 and an organophosphate insecticide selected from triazophos, profenofos, chlorfenthion, monocrotophos, acephate, methamidophos, and diethyl 1-phenyl-1H-1, 2, 4-triazol-3-yl phosphate.
While various efforts have been made in the past to develop stable pesticidal compositions comprising low melting point active ingredients and moisture sensitive active ingredients, the need to develop alternative, simple and effective products and a method for developing stable pesticidal compositions of these active ingredients has long been felt. In addition, there is a need to develop such formulations, wherein the formulations overcome the disadvantages of the prior art and exhibit increased stability with respect to the combination of degradation of moisture sensitive actives and dispersibility/suspendability of low melting active ingredients. Physical stability of the formulation during storage/use is a critical issue in the art and likewise remains to be solved.
Purpose(s) to
It is an object of the present invention to provide an agrochemical composition comprising a low melting point active ingredient and a moisture sensitive active ingredient.
It is another object of the present invention to provide a stable agrochemical composition comprising a low melting point active ingredient and a moisture sensitive active ingredient.
It is another object of the present invention to provide a method for controlling pests using the composition of the present invention.
It is another object of the present invention to provide a dust-free, free-flowing, storage-stable dry composition comprising at least one low-melting active ingredient and a moisture-sensitive active ingredient.
Disclosure of Invention
In accordance with the above objects, the present invention provides a stable agrochemical composition comprising:
a) at least one low melting active ingredient;
b) at least one moisture sensitive active ingredient; and
c) an additive;
characterized in that the additive has a softening or melting point lower than the melting point of the low-melting active ingredient.
In accordance with the above objects, the present invention provides a method of preparing a stable agrochemical composition comprising at least one low melting active ingredient, at least one moisture sensitive active ingredient and an additive, wherein the additive has a softening or melting point lower than the melting point of the low melting active ingredient.
In accordance with the above objects, the present invention provides the use of the stabilized composition according to the invention as an agrochemical composition.
In accordance with the above objects, the present invention also provides a method for controlling undesired pests, which comprises applying an agrochemically effective amount of the stabilized composition according to the present invention to the pests or the locus thereof.
Additional features and advantages of the invention will be apparent from the following detailed description, which shows by way of example the most preferred features of the invention, which should not be taken as limiting the scope of the invention described herein.
Detailed Description
The inventors of the present invention have surprisingly found that stable agrochemical compositions in the form of granular compositions of a low melting active ingredient and a moisture sensitive active ingredient can be prepared by mixing the low melting active ingredient with the moisture sensitive active ingredient in the presence of an additive and exposing the premix to extrusion granulation.
It has surprisingly been found that the additives used by the present inventors prevent the low melting active ingredient from undergoing crystal modification or forming encrustations on the granules. Indeed surprisingly, the additive of the invention allows to store the product under any conditions and still maintain the quality of the product without any deterioration in the dispersibility, suspendability and usability of the active substance.
An accepted method to test the long term stability and performance of a formulation is to leave the formulation at 54 degrees for 14 days, which is known as the accelerated thermal stability (AHS) test, and then test for dispersibility, suspendability, and wet sieve tests. A decrease in suspendability and dispersibility indicates poor performance of the formulation in the field after long term storage, and an increase in the wet sieve test indicates the formation of large particles that will clog the nozzles in the field.
The inventors have observed that the formulation of the present invention passes all tests after AHS, demonstrating its effectiveness in the field even after long term storage. It is believed that the additives used during the process enable the formulation to remain stable for a longer storage duration.
As used herein, the term "composition" is used interchangeably with the term "formulation" and is intended to refer to a stable solid dry suspension agent intended to protect crops and their products from damage by insects and pests.
The compounds are referred to herein as "low melting active ingredients" which are terms recognized in the relevant art, specifically in the field of agrochemical compositions. In particular, low melting active compounds according to the present invention are compounds that have a melting point of less than about 100 ℃, less than about 90 ℃, less than about 85 ℃, less than about 80 ℃, less than about 75 ℃, or less than about 70 ℃, or the ability to cure at room temperature. In certain embodiments, low melting compounds according to the present invention are compounds having a melting point of from about 20 ℃ to about 100 ℃. In particular embodiments, the low melting point compound is a compound having a melting point in the range of about 25 ℃ to about 100 ℃, about 30 ℃ to about 90 ℃, about 30 ℃ to about 80 ℃, about 30 ℃ to about 70 ℃, about 40 ℃ to about 90 ℃, about 40 ℃ to about 80 ℃, about 50 ℃ to about 90 ℃, about 50 ℃ to about 80 ℃, or about 50 ℃ to about 70 ℃.
The term "moisture-sensitive active ingredient" refers to a compound that has the ability to absorb moisture and undergo degradation or other changes in physico-chemical parameters.
As used herein, the term "extrusion granulation" refers to a process of granulation in which a composition comprising an active ingredient is extruded by applying pressure separately, sequentially or simultaneously and granulated by a suitable mechanism such as extrusion.
As used herein, the term "degradation" refers to the loss of active ingredient due to exposure to moisture and/or upon storage.
The term "softening point" refers to the temperature at which an additive achieves a particular degree of softness. The "softening point" is close to but below the melting point of the additive.
The term "locus" as used herein refers to a location to which a combination according to the invention is applied. It includes application to an individual plant, a group of plants such as the plant and/or its surroundings, and an area where the plant can be grown, as well as direct application to one or more insects and/or their vicinity.
In the context of the present invention, the term "agrochemical" refers to any agent used to destroy insects, arachnids, fungi, undesirable vegetation, rodents and other pests.
The term "insect" includes all organisms in the class "insects". "insecticidal" refers to the ability of a substance to increase the mortality rate or inhibit the growth rate of an insect.
The term "plant" refers to all physical parts of a plant, including seeds, seedlings, saplings, roots, tubers, stalks, stems, leaves, and fruits.
The term "agrochemically effective amount of active substance" means an amount of active substance that kills or inhibits the desired control of plant diseases, which amount is not significantly toxic to the plant being treated.
By "controlling" an insect is meant inhibiting the ability of the pest to survive, grow, feed and/or reproduce, or limiting insect-related damage or loss in crop plants, through toxic effects. "controlling" an insect may or may not mean killing the insect, but preferably it means killing the insect.
The inventors of the present invention have found that the addition of additives to a combination of a moisture sensitive active ingredient (preferably an organophosphorus insecticide) and a low melting active ingredient results in a highly stable composition. The stable composition obtained by the addition of the additive helps to form granules in the absence of water. Thus, the present invention provides a composition that allows avoiding the use of water.
Without being bound by theory, the inventors of the present invention have surprisingly found that the addition of a low softening point or low melting point additive to a combination of a low melting point active ingredient such as a pyrethroid and a moisture sensitive active ingredient such as an organophosphorus insecticide results in a stable particulate composition.
The dry suspending agent or the granules are easy to prepare and store, and have good dispersibility and suspensibility under the storage condition. The additives are used in the absence of water to obtain the stable pesticidal composition, avoiding moisture which causes degradation of moisture sensitive actives such as acephate, and extrusion below the melting point of the low melting point pyrethroid (i.e. 30-58 degrees celsius) avoids adhesion problems due to melting and gradual cooling during temperature changes in the process and on storage.
Accordingly, in one aspect, the present invention may provide a stable agrochemical composition comprising:
a) at least one low melting active ingredient;
b) at least one moisture sensitive active ingredient; and
c) an additive;
characterized in that the additive has a softening or melting point lower than the melting point of the low-melting active ingredient.
In another aspect, the present invention may provide a stable pesticidal composition comprising:
a) at least one low melting pyrethroid;
b) at least one moisture sensitive insecticide; and
c) an additive;
characterised in that the additive has a softening or melting point below the melting point of the low melting pyrethroid.
In one embodiment, the low melting active ingredient of the present invention may be selected from the group consisting of insecticides, attractants, disinfectants, bactericides, acaricides, nematicides, fungicides, growth regulators, herbicides, fertilizers and mixtures.
In a preferred embodiment, the low melting active ingredients of the present invention are selected from the group consisting of insecticides, attractants, disinfectants, bactericides, acaricides, nematicides, fungicides and growth regulators.
In one embodiment, the low melting active ingredient of the present invention is selected from the group consisting of phthalazinone ester, myclobutanil, mepiquat chloride, iodophos, imazalil, lambda-cyhalothrin, triflumizole, aphidicolor, methiocarb, tolfenphos-methyl, pomade, pyriproxyfen, propamocarb hydrochloride, tefluthrin, resmethrin, chlorpropham-methyl, dinotefuran, bencarb, demeton-S, cyfluthrin, cypermethrin, ethoprophos, glutethion, benalaxyl, benazolin, butoxycarb, fenthiocarb, fenphos, fenthion, furalaxyl, clofurazonic acid, trinexapac-ethyl, ethiofencarb, clomazole, fenamiphos, fenazaquin, EPN, dodemorph, methidathion, ethoprophos, fenflurazon, fenflurazofen, fenflurazone, flumetofen, fenflurazone, cyhalonil, cyhalon, cy, Octamethiphos, transfluthrin, cyprodinil, gossypos, fosthien, chlorfenapyr, propylate miticide, avencide, chlorofenprox, toxaphene, chloromite, chlordimeform, phosphonic acid, trifloxystrobin, picoxystrobin, gamma-cyhalothrin, alemondin, spinetoram and cyflumetofen.
In one embodiment, the low melting active ingredients of the present invention are selected from strobilurins or pyrethroids.
The low melting pyrethroid may be selected from, but is not limited to, cypermethrin, fenvalerate, permethrin, α -cypermethrin, β -cypermethrin, zeta-cypermethrin, deltamethrin, cyhalothrin, bifenthrin, lambda cyhalothrin, and/or resmethrin or mixtures thereof.
In another preferred embodiment of the invention, the low melting pyrethroid is selected from the group consisting of bifenthrin, cypermethrin, α -cypermethrin, β -cypermethrin, and zeta-cypermethrin.
Thus, in another preferred embodiment, the low melting pyrethroid may be bifenthrin.
In one embodiment, the low melting strobilurins may be selected from trifloxystrobin or picoxystrobin.
In one embodiment, the present invention may provide a stable agrochemical composition comprising from about 0.1% to about 30% and preferably from about 0.2% to about 20% low melting pyrethroid by weight of the total weight of the stable agrochemical composition.
Another embodiment of the present invention may provide a stable pesticidal composition comprising from about 0.1% to about 30% and preferably from about 0.2% to about 20% low melting pyrethroid by weight of the total weight of the stable pesticidal composition.
In a preferred embodiment of the invention, the stable pesticidal composition comprises from about 1% to about 10% weight/weight of the low melting pyrethroid, based on the total weight of the stable pesticidal composition.
In one embodiment, the moisture-sensitive active ingredient present in the composition may be selected from organophosphorus insecticides.
In one embodiment, the moisture sensitive organophosphate pesticide may be selected from, but is not limited to, acephate, methyl valefos, carbofuran, chlorfenafos, coumaphos, fosthier, dimethoate, fenamiphos, phosmet, fenamiphos, isofenphos (isofenfos), methamidophos, methidathion, methyl parathion, metocloprid, monocrotophos, metham, flufenthion, phosmet, phosphamidon, profenofos, TEPP, terbufos, chlorfenapyr, trichlorfon, and combinations thereof.
Preferred organophosphorus insecticides may be selected from acephate, profenofos, phosphamidon or mixtures thereof.
Accordingly, one embodiment of the present invention may provide a stable pesticidal composition comprising from about 0.5% to about 95% and preferably from about 10% to about 85% organophosphate pesticide by total weight of the stable pesticidal composition.
In a preferred embodiment of the present invention, the stable pesticidal composition comprises from about 40% to about 85% organophosphate pesticide by weight of the total weight of the stable pesticidal composition.
In one embodiment, the invention comprises an additive having a softening or melting point that is lower than the melting point of the low melting active ingredient.
In another embodiment, the invention comprises an additive having a melting point that is lower than the melting point of the low melting active ingredient.
In one embodiment, the softening point of the additive is lower than the melting point of the low melting active ingredient.
In a preferred embodiment, the present invention comprises a water-soluble additive.
In one embodiment, the additive of the present invention may be selected from, but is not limited to, polyethylene glycol (PEG)6000, PEG4000, PEG8000, nonylphenol 30EO or high molecular weight ethoxylates or propoxylates of fatty acids, fatty acid alcohols, vegetable oils, polyvinyl alcohols, polyacrylates, starches, carboxymethylcellulose, alginic acid, agar, gum arabic and xanthan gum.
In another embodiment, the additive of the present invention may preferably be selected from the group consisting of polyethylene glycol (PEG)6000, PEG4000, PEG8000, vegetable oil and cellulose ether.
In a preferred embodiment, the additive of the invention may be selected from polyethylene glycols.
In one embodiment, in the composition according to the invention, the additive is present in an amount of from about 1% to about 30% by weight of the composition. Preferably, the additive is present in an amount of about 3% to about 20% by weight of the formulation.
The stabilized pesticidal compositions of the present invention may further comprise one or more dispersants, wetting agents, fillers, surfactants, anti-caking agents, pH adjusters, preservatives, biocides, antifoams, colorants and other formulation aids.
The dispersing agent may be selected from ionic and non-ionic dispersing agents which enable the granules to disintegrate easily in water, such as salts of polystyrene sulphonic acid, salts of polyvinyl sulphonic acid, salts of naphthalene sulphonic acid/formaldehyde condensates, salts of condensates of naphthalene sulphonic acid, phenol sulphonic acid and formaldehyde, and salts of lignosulphonic acid, polyethylene oxide/polypropylene oxide block copolymers, polyethylene glycol ethers of linear alcohols, reaction products of fatty acids with ethylene oxide and/or propylene oxide, furthermore polyvinyl alcohol, polyvinylpyrrolidone, copolymers of polyvinyl alcohol with polyvinylpyrrolidone, and copolymers of (meth) acrylic acid and (meth) acrylic esters, furthermore alkyl ethoxylates and alkyl aryl ethoxylates, ethoxylated alkyl aryl phosphates and sulphates. Preferred dispersants include derivatives of ethoxylates of vegetable oils or mixtures of one or more of these; or a styrene acrylic polymer or a mixture thereof.
The wetting agent may be selected from soap; salts of fatty monoesters of sulfuric acid, including but not limited to sodium lauryl sulfate; sulfoalkyl amides and salts thereof, including but not limited to N-methyl-N-oleoyl taurate sodium salt; alkyl aryl sulfonates including, but not limited to, alkyl benzene sulfonates, alkyl naphthalene sulfonates, and salts thereof; and salts of lignosulfonic acid.
In one embodiment, the filler may be selected from insoluble fillers and soluble fillers.
In one embodiment, the filler may preferably be selected from precipitated silica and diatomaceous earth kaolin.
In one embodiment, the pesticidal composition according to the present invention is preferably prepared in the form of a dry suspension (DF).
In one embodiment, suitable antifoaming agents may preferably be salts of siloxanes, long chain alcohols and fatty acids.
Suitable colorants (e.g., red, blue and green) are preferably sparingly water-soluble pigments and water-soluble dyes. Examples are inorganic colorants (e.g., iron oxide, titanium oxide, and iron hexacyanoferrate) and organic colorants (e.g., alizarin, azo, and phthalocyanine colorants).
According to a preferred embodiment, the present invention may provide a stable insecticidal composition comprising acephate, bifenthrin, and an additive having a softening or melting point lower than the melting point of the low melting active ingredient.
According to a particular embodiment, the stabilized pesticidal composition of the present invention may comprise from about 0.5% to about 95% per weight of acephate, from about 0.1% to about 30% per weight of bifenthrin, from about 1.0% to 30% per weight of an additive having a softening or melting point lower than the melting point of the low melting active ingredient.
According to another specific embodiment, the stabilized pesticidal composition of the present invention may comprise about 5.0 wt/wt% to about 80 wt/wt% of acephate, about 1.0 wt/wt% to about 20 wt/wt% of bifenthrin, about 5.0 wt/wt% to about 20 wt/wt% of PEG 6000 as additives.
According to one embodiment of the present invention, there is provided a stable agrochemical composition comprising acephate, trifloxystrobin and an additive having a softening or melting point lower than the melting point of the low melting active ingredient.
According to a specific embodiment, the stable agrochemical composition of the present invention may comprise from about 0.5% to about 95% acephate, from about 0.1% to about 30% trifloxystrobin, from about 1.0% to 30% additives having a softening or melting point lower than the melting point of the low melting active ingredient.
In another embodiment, the present invention provides a method for preparing a stable agrochemical composition. The method comprises the following steps:
1) premixing at least one low melting active ingredient, at least one moisture sensitive active ingredient, and an additive, wherein the additive has a softening or melting point that is lower than the melting point of the low melting active ingredient; and
2) and extruding and granulating the premix.
In one embodiment, the method of the present invention includes additional conventional steps that may be necessary, but not essential, to achieve the advantages of the present invention.
According to another embodiment of the present invention, in the method of preparing a stable agrochemical composition, extrusion granulation may be performed in such a manner that the composition may be extruded and granulated separately, sequentially or simultaneously.
In one embodiment, the present invention provides a method of preparing a stable agrochemical composition. The method comprises the following steps:
1) premixing at least one low melting active ingredient, at least one moisture sensitive active ingredient, and an additive, wherein the additive has a softening or melting point that is lower than the melting point of the low melting active ingredient; and
2) the premixes are extruded and granulated separately, sequentially or simultaneously.
In a preferred embodiment, the process for preparing a stable pesticidal composition comprises the steps of:
1) mixing an active ingredient selected from at least one low melting pyrethroid with a desired amount of precipitated silica to obtain a premix;
2) milling the premix in a jet mill with or without other additives to obtain a milled low melting pyrethroid of a desired particle size;
3) adding an organophosphorus active ingredient and an additive to the ground low-melting pyrethroid, wherein the additive has a softening point or a melting point that is lower than the melting point of the low-melting active ingredient, and any other necessary additive or additives, and mixing them to obtain a premix;
4) subjecting the premix to extrusion granulation to obtain the granules.
Preferably, the granules thus obtained are tested for the desired quality specifications. Once the granules pass the quality specifications, they are preferably filled in the form of a dry suspension and packaged in the desired packaging.
Premixes of low melting actives with moisture sensitive actives and additives may also be processed by pre-extrusion followed by roll extrusion. This premixing of the moisture sensitive active ingredient and the low melting active ingredient with the additive prevents the moisture sensitive active ingredient from deteriorating in the composition; and the pre-extrusion prevents the low melting active ingredient from melting during the extrusion process.
The compositions of the invention enjoy all the advantages described above, making them advantageous from an economic and handling point of view, and show very good performance during application. As will be demonstrated in the examples, the compositions of the present invention exhibit good suspendability, stability, dispersibility and free-flow and pass the wet sieve test.
According to one embodiment, the present invention provides the use of a stable agrochemical composition as an agrochemical active composition, said agrochemical composition comprising at least one low melting active ingredient, at least one moisture sensitive active ingredient and an additive, wherein said additive has a softening or melting point which is lower than the melting point of the low melting active ingredient.
In one embodiment, the stabilized composition according to the invention is used as a pesticide.
Therefore, the stable pesticidal composition of the present invention rapidly kills pests. It is especially effective against crop pests such as leps, stink bugs and lygus bugs, preferably against potent lethal weapons of lepidoptera, coleoptera, diptera, hemiptera, which are difficult to kill.
In one embodiment, the crop on which the composition of the invention can be used may be selected from, but is not limited to, cereals, such as wheat, oats, barley, spelt, triticale, rye, maize, millet, rice, crops, such as sugarcane, soybean, sunflower, rape (rape), canola, tobacco, sugar beet, fodder beet; tuber crops such as potatoes, sweet potatoes, and the like; crops such as asparagus, hop seeds, etc.; fruit plants such as apples, pears, stony fruits such as, for example, peaches, nectarines, cherries, plums, apricots, citrus fruits such as oranges, grapefruits, limes, lemons, kumquats, mandarins in china, seedless mandarins; nuts such as pistachios, almonds, walnuts, pecans; tropical fruits such as mango, papaya, pineapple, jujube, banana, etc., grapes, vegetables such as chicory, sheep lettuce, lettuce (lette), fennel, global pine leaf salad, beet, spinach, chicory, cauliflower, broccoli, chinese cabbage, cabbage (winter cabbage) or kale (curly kale)), kohlrabi, brussel sprout, red cabbage, bok choy and wrinkled cabbage, fruit vegetables such as eggplant, cucumber, paprika, zucchini, tomato, green peel pumpkin, sweet corn, root vegetables such as celery, turnip, carrot, kohlrabi, radish, horseradish, beetroot, salsify, celery, beans such as pea, bean, etc., bulb vegetables such as leek, onion, etc., oil crops such as mustard, poppy, olive, sunflower, coconut, castor oil plants, cacao beans, peanut; fibre crops such as cotton, jute, flex, hemp, crops such as tea, coffee, rubber, ornamentals including shrubs and flowering plants, grapevines, rangelands and pastures.
In one embodiment, the compositions of the present invention may be optionally mixed with other insecticides, attractants, disinfectants, bactericides, acaricides, nematicides, fungicides, growth regulators, herbicides, fertilizers, and mixtures thereof.
In one embodiment, the present invention provides a method of controlling an undesirable pest, said method comprising applying a stable composition according to the present invention to the pest or the locus thereof.
Accordingly, in one embodiment, the present invention can provide a method of controlling pests at a locus, said method comprising applying a pesticidally effective amount of a composition comprising:
a) at least one low melting pyrethroid;
b) at least one moisture sensitive organophosphorus insecticide; and
c) an additive;
characterised in that the additive has a softening or melting point below the melting point of the low melting pyrethroid.
In one embodiment, the present invention may provide a method of controlling pests, such as those belonging to the lepidoptera, coleoptera, diptera, hemiptera classes of insects.
In another aspect, the invention provides a kit. The kit comprises a plurality of components, each of which may comprise at least one or more of the ingredients of the composition of the invention.
In one embodiment, the components of the kit can be mixed just prior to use in any of the methods of their use described herein.
In one embodiment, the kit contains an instruction manual instructing the user of the kit to mix the components in predetermined amounts or in their predetermined ratios prior to use.
In one embodiment, the instruction manual instructs the user of the kit to use the composition against predetermined insects on certain predetermined crops.
Accordingly, in one embodiment, the present invention provides a kit comprising:
(a) at least one low melting active ingredient component;
(b) at least one moisture sensitive active ingredient component; and
(c) an additive component, characterized in that the additive has a softening or melting point lower than the melting point of the low-melting active ingredient.
In another embodiment, the present invention provides a kit comprising:
(a) at least one low melting pyrethroid component;
(b) at least one moisture sensitive pesticide component; and
(c) an additive component, characterised in that the additive has a softening or melting point below the melting point of the low-melting pyrethroid.
In one embodiment, the low melting active ingredient component of the present invention comprises a strobilurin or a pyrethroid.
The low melting pyrethroid may be selected from, but is not limited to, cypermethrin, fenvalerate, permethrin, α -cypermethrin, β -cypermethrin, zeta-cypermethrin, deltamethrin, cyhalothrin, bifenthrin, lambda cyhalothrin, and/or resmethrin or mixtures thereof.
In another preferred embodiment of the invention, the low melting pyrethroid is selected from the group consisting of bifenthrin, cypermethrin, α -cypermethrin, β -cypermethrin, and zeta-cypermethrin.
Thus, in another preferred embodiment, the low melting pyrethroid may be bifenthrin.
In one embodiment, the low melting strobilurins may be selected from trifloxystrobin or picoxystrobin.
In one embodiment, the kit contains an instruction manual instructing the user to use from about 0.1% to about 30% weight/weight of the low melting pyrethroid component.
In one embodiment, the kit comprises a moisture sensitive active ingredient component selected from the group consisting of organophosphorus insecticides.
In one embodiment, the kit comprises an instruction manual instructing the user to use from about 0.5% to about 95% weight/weight of the organophosphorous pesticide component.
In one embodiment, the kit comprises an additive component, wherein the additive is selected from the group consisting of polyethylene glycol (PEG)6000, PEG4000, PEG8000, nonylphenol 30EO or high molecular weight ethoxylates or propoxylates of fatty acids, fatty acid alcohols, vegetable oils, polyvinyl alcohols, polyacrylates, starches, carboxymethylcellulose, alginic acid, agar, gum arabic, and xanthan gum.
In one embodiment, the kit comprises an instruction manual instructing the user to mix from about 1% to about 30% of the additive components.
According to a preferred embodiment, the present invention may provide a kit comprising a acephate component, a bifenthrin component, and an additive component having a softening or melting point lower than the melting point of bifenthrin.
According to another preferred embodiment, the present invention provides a kit comprising an instruction manual instructing a user to mix about 0.5 wt/wt% to about 95 wt/wt% of a acephate component, about 0.1 wt/wt% to about 30 wt/wt% of a bifenthrin component, and about 1.0 wt/wt% to 30 wt/wt% of an additive having a softening point or melting point below the melting point of bifenthrin.
According to another specific embodiment, the present invention provides a kit comprising about 5.0% w/w to about 80% w/w of the acephate component indicated for use, about 1.0% w/w to 20% w/w of the bifenthrin component indicated for use, and about 5.0% w/w to about 20% w/w of the PEG 6000 component indicated for use.
In one embodiment, a kit comprises a acephate component, a trifloxystrobin component, and an additive component having a softening or melting point lower than trifloxystrobin.
In one embodiment, the kit comprises instructions for mixing about 0.5 wt/wt% to about 95 wt/wt% of the acephate component, about 0.1 wt/wt% to about 30 wt/wt% of the trifloxystrobin component, and about 1.0 wt/wt% to 30 wt/wt% of the additive component, wherein the additive has a softening point or melting point lower than the melting point of trifloxystrobin.
In one embodiment, the kit comprises instructions for using the components of the kit as a pesticide or fungicide.
In one embodiment, the kit comprises instructions for using the components against lepidoptera, coleoptera, diptera, hemiptera, preferably leps, stink bug and lygus bugs.
In one embodiment, the kit comprises instructions for using the components in a crop selected from the group consisting of: cereals, such as wheat, oats, barley, spelt, triticale, rye, maize, millet, rice, crops such as sugar cane, soybeans, sunflowers, rape, canola, tobacco, sugar beet, fodder beet; tuber crops such as potatoes, sweet potatoes, and the like; crops such as asparagus, hop seeds, etc.; fruit plants, such as apples, pears, stone fruits, such as, for example, peaches, nectarines, cherries, plums, apricots; citrus fruits such as oranges, grapefruit, lime, lemon, kumquat, mandarin orange, and seedless mandarin orange; nuts such as pistachios, almonds, walnuts, pecans; tropical fruits such as mango, papaya, pineapple, jujube, banana, etc., grapes, vegetables such as chicory, sheep lettuce, fennel, global pine salad, beet, spinach, chicory, cauliflower, broccoli, chinese cabbage, cabbage (winter cabbage (winterkale) or kale (curly kale)), kohlrabi, brussel sprout, red cabbage, bok choy and cabbage, fruit vegetables such as eggplant, cucumber, paprika, zucchini, tomato, zucchini, sweet corn, root vegetables such as celery, turnip, carrot, kohlrabi, radish, horseradish, beetroot, salsify, celery, such as beans, etc., bulb vegetables such as leek, onion, etc., oil crops such as mustard, poppy, olive, sunflower, coconut, castor oil plants, cocoa beans, peanuts; fibre crops such as cotton, jute, flex, hemp, crops such as tea, coffee, rubber, ornamentals including shrubs and flowering plants, grapevines, rangelands and pastures.
The present inventors have successfully prepared stable compositions by carefully combining the at least one moisture sensitive active ingredient, at least one low melting active ingredient and additives, wherein the additives have a softening or melting point lower than the melting point of the low melting active ingredient, and methods for their preparation. Optimal concentrations of active substance and formulation ingredients that result in stable DF formulations have been obtained by experiments as exemplified below.
These examples are merely illustrative and should not be construed as limiting the scope and underlying principles of the invention in any way. Indeed, various modifications of the invention in addition to those shown and described herein will become apparent to those skilled in the art from the following examples and the foregoing description.
While the foregoing written description of the invention enables one of ordinary skill to make and use what is presently considered to be the best mode thereof, those of ordinary skill will understand and appreciate the existence of variations, combinations, and equivalents of the specific embodiments, methods, and examples herein. Accordingly, the present invention should not be limited by the above-described embodiments, methods and examples, but by all embodiments and methods within the scope and spirit of the present invention.
Experimental examples：
The following examples illustrate the basic method and versatility of the present invention.
Example 1: 74 w/w% acephate and 6 w/w% bifenthrin DF were prepared as follows：
| Composition (I) | Quantity (g) |
| Acephate | 76.02 |
| Biphenthrin | 6.63 |
| Castor oil ethoxylate | 4 |
| PEG-6000 | 11.50 |
| Precipitated silica (PPT silica) | 1.85 |
| Total of | 100.00 |
The procedure is as follows: the bifenthrin technical is mixed with precipitated silica to prepare a bifenthrin premix. The bifenthrin premix was milled in a jet mill to obtain the desired particle size. Acephate, castor oil ethoxylate, PEG-6000 and precipitated silica were added to the bifenthrin premix to obtain a bifenthrin-acephate premix. Then, the bifenthrin-acephate premix is granulated by extrusion by passing the premix through a roll extruder so that it passes through several times below the melting point of bifenthrin to obtain granules.
Example 2: 74 w/w% acephate and 6 w/w% bifenthrin DF were prepared as follows：
| Composition (I) | Quantity (g) |
| Acephate | 76.02 |
| Biphenthrin | 6.63 |
| Metasperse 550S | 3.00 |
| Castor oil ethoxylate | 2.5 |
| Dialkyl naphthalene sulfonic acid sodium salt | 1.00 |
| PEG-6000 | 9.00 |
| PPT silica | 1.85 |
| Total of | 100.00 |
The procedure is as follows: bifenthrin was mixed with silica to make a bifenthrin premix. The premix is milled in a jet mill to obtain the desired particle size. Acephate, Metasperse 550S, castor oil ethoxylate, sodium salt of dialkyl naphthalene sulfonate, PEG 6000 and precipitated silica were added to the bifenthrin premix to obtain a bifenthrin-acephate premix. Then, the bifenthrin-acephate premix is granulated by extrusion by passing the premix through a roll extruder so that it passes through several times below the melting point of bifenthrin to obtain granules.
Example 3: 74 w/w% acephate and 6 w/w% bifenthrin DF were prepared as follows：
| Composition (I) | Quantity (g) |
| Acephate | 76.02 |
| Biphenthrin | 6.53 |
| Metasperse 550S | 3.00 |
| Dialkyl naphthalene sulfonic acid sodium salt | 1.00 |
| PEG-8000 | 13.10 |
| PPT silica | 0.35 |
| Total of | 100.00 |
The procedure is as follows: bifenthrin was mixed with silica to make a bifenthrin premix. The bifenthrin premix was milled in a jet mill to obtain the desired particle size. Acephate, Metasperse 550S, dialkyl naphthalene sulfonic acid sodium salt, PEG8000 and precipitated silica were added to the bifenthrin premix to obtain a bifenthrin-acephate premix. Then, the bifenthrin-acephate premix is granulated by extrusion by passing the premix through a roll extruder so that it passes through several times below the melting point of bifenthrin to obtain granules.
Example 4 preparation of 74 w/w% acephate and 6 w/w% β -cypermethrin DF：
| Composition (I) | Quantity (g) |
| Acephate | 76.02 |
| β -cypermethrin | 6.53 |
| Metasperse 550S | 3.00 |
| Dialkyl naphthalene sulfonic acid sodium salt | 2.00 |
| PEG-4000 | 9.00 |
| Ammonium sulfate | 3.10 |
| PPT silica | 0.35 |
| Total of | 100.00 |
The procedure is β -cypermethrin mixed with silica to make β -cypermethrin premix β -cypermethrin was milled in an air jet mill to obtain the desired particle size acephate, Metasperse 550S, sodium salt of dialkyl naphthalene sulfonate, PPT silica, ammonium sulfate and PEG4000 were added to β -cypermethrin premix to obtain β -cypermethrin-acephate premix, then β -cypermethrin-acephate premix was granulated by extrusion through a roll extruder to make multiple passes below the melting point of bifenthrin to obtain granules.
Example 5: 74 w/w% acephate and 6.5 w/w% trifloxystrobin DF were prepared as follows：
| Composition (I) | Quantity (g) |
| Acephate | 76.02 |
| Trifloxystrobin | 7.04 |
| Metasperse 550S | 3.00 |
| Dialkyl naphthalene sulfonic acid sodium salt | 2.00 |
| PEG-6000 | 9.00 |
| Ammonium sulfate | 2.59 |
| PPT silica | 0.35 |
| Total of | 100.00 |
The procedure is as follows: trifloxystrobin was mixed with silica to prepare a trifloxystrobin premix. The trifloxystrobin premix was milled in a jet mill to obtain the desired particle size. Acephate, Metasperse 550S, sodium salt of dialkyl naphthalene sulfonate, PPT silica, ammonium sulfate, and PEG 6000 were added to the trifloxystrobin premix to obtain a trifloxystrobin-acephate premix. Then, the trifloxystrobin-acephate premix was subjected to extrusion granulation by passing the premix through a roll extruder to obtain granules.
Stability data
Dispersibility test
The compositions according to the invention (examples 6 to 10) were tested for stability. Samples were prepared using different amounts of active ingredient and other ingredients as listed in the following table (table 1). Samples were prepared according to the method given in example 1. The samples were tested for dispersibility by observing the number of inversions required to achieve complete dispersion.
TABLE 1：
Additive selected from PEG 6000, PEG4000 and PEG8000
The number of inversions required to achieve complete dispersion of the granules was determined by the following procedure: a 250ml graduated cylinder was taken and 2gm of sample was added to the cylinder. It was allowed to soak for 2 minutes. The graduated cylinder was then closed by placing a plug and tilted to 180 ℃ and allowed to return to the original position within 2 seconds.
It was observed that the compositions of the invention achieved good dispersion within about 12-15 inversions and were well suited for storage.
Testing the suspensibility and stability of the active ingredients
The suspendability of DF formulations prepared according to the present invention, the degradation of the active ingredient and its effect on the stability of the composition were investigated. Samples were prepared according to example 1 (examples 7 and 11).
The samples were kept at 54 ± 2 ℃ for up to 14 days and tested for stability parameters such as suspensibility, wet sieve analysis and degradation of the active ingredient. The results are summarized in table 2.
TABLE 2
As is clear from table 2, no degradation of active acephate and active bifenthrin in the DF composition was observed when kept at 54 ± 2 ℃ for 14 days. The suspendability of the formulation does not change significantly, thus keeping the formulation according to the invention stable according to physicochemical parameters. This indicates that the DF or particulate compositions of acephate and bifenthrin so obtained not only have excellent stability of the active ingredients, but also retain dispersibility and therefore the availability of the active ingredients for the intended use. From the results of the wet sieve analysis, it was further confirmed that the crystal modification of bifenthrin was prevented. The combination of active substance and excipients prepared according to the disclosed method results in a stable DF composition that does not undergo any chemical and physical changes upon storage and is also easy to handle for further use.
For comparison purposes, a comparative sample (example 12) was prepared without the additive of the invention. The samples were tested for dispersibility by observing the number of inversions required to achieve complete dispersion.
| Composition (I) | Example 12 |
| Acephate | 76.02 |
| Biphenthrin | 6.33 |
| PEG-6000 | 0.00 |
| PPT silica | 1.00 |
| Castor oil ethoxylate | 0.00 |
| Soprophor-4D384 | - |
| Dialkyl naphthalene sulfonic acid sodium salt | 2.00 |
| Metasperse 550S | 3.00 |
| Ammonium sulfate | 11.65 |
| Number of inversions | >30 |
| Wet Screen analysis (Retention on 75 μ test Screen) | 3.52 wt/wt% |
| Suspensibility | 45.8 wt/wt% (based on bifenthrin) |
| Availability of bifenthrin | 45.8% total active substance |
It has been observed that the sample prepared without additives having a softening or melting point lower than the melting point of the low melting active ingredient (example 12) does not provide good dispersibility. Thus, the formulation fails to deliver the desired dispersibility and results in an unstable formulation.
Usability test for bifenthrin for insecticidal activity
DF formulations prepared according to the present invention were further investigated to find the amount of bifenthrin still available to act as an insecticide. The suspensibility of the formulation can directly infer that the active ingredient is still available for the intended use of the active ingredient. The suspendability of the formulations prepared according to the invention was tested in comparison to formulations prepared without additives. Samples were prepared according to example 1 and held at 54 ± 2 ℃ for 14 days and suspendability was measured.
A review of table 3, given below, shows that the measured suspensibility was unexpectedly high for examples 15-17 prepared according to the invention, which clearly indicates that the formulation can be effectively used for the intended insecticidal activity. The% availability of bifenthrin achieved is the same as the% availability of bifenthrin at the initial concentration in the formulation. In the case of examples 13-14, which were prepared without additives, the measured suspensibility was very low, indicating that bifenthrin was available only about 50% of what was expected from those formulations.
Table 3: availability of bifenthrin in the formulation
Additive selected from PEG 6000, PEG4000 and PEG8000
Thus, the present inventors have successfully prepared formulations of low melting active ingredients that are susceptible to undergoing morphological changes with moisture sensitive agrochemicals. The compositions according to the invention have been found to be stable and effective for the intended use.
Claims (20)
1. An agrochemical composition comprising:
a) at least one low melting active ingredient;
b) at least one moisture sensitive active ingredient; and
c) an additive, characterized in that the additive has a softening or melting point lower than the melting point of the low-melting active ingredient.
2. An agrochemical composition according to claim 1, wherein the low melting active ingredient is selected from pyrethroid insecticides and strobilurin fungicides.
3. The agrochemical composition according to claim 1, wherein said low melting active ingredient is selected from the group consisting of bifenthrin, cypermethrin, fenvalerate, permethrin, α -cypermethrin, β -cypermethrin, zeta-cyhalothrin, deltamethrin, cyfluthrin, lambda cyhalothrin, and resmethrin and mixtures thereof.
4. The agrochemical composition according to claim 1, wherein said low melting active ingredient is bifenthrin.
5. The agrochemical composition according to claim 1, wherein said low melting active ingredient is trifloxystrobin.
6. The agrochemical composition according to claim 1, wherein said composition comprises from about 0.1% to about 30% weight/weight of low melting point active ingredient, based on the total weight of said agrochemical composition.
7. The agrochemical composition according to claim 1, wherein said moisture sensitive active ingredient is selected from the group consisting of: acephate, methyl valefos, carbofuran, chlorfenapyr, coumaphos, fosthier, dimethoate, fenamiphos, disulfoton, fenamiphos, isopropylamidophos, methamidophos, methidathion, methyl parathion, methamidophos, monocrotophos, metam, futhion, phosmet, phosphamidon, profenofos, TEPP, terbufos, chlorfenvinphos, trichlorfon, and combinations thereof.
8. The agrochemical composition according to claim 1, wherein said moisture sensitive active ingredient is acephate.
9. The agrochemical composition according to claim 1, wherein said composition comprises from about 0.5% to about 95% moisture sensitive active ingredient by weight of the total weight of said agrochemical composition.
10. The agrochemical composition according to claim 1, wherein said additive is selected from the group consisting of polyethylene glycol (PEG)6000, PEG4000, PEG8000, nonylphenol 30EO or high molecular weight ethoxylates or propoxylates of fatty acids, fatty acid alcohols, vegetable oils, polyvinyl alcohols, polyacrylates, starches, carboxymethylcellulose, alginic acid, agar, gum arabic and xanthan gum.
11. The agrochemical composition according to claim 1, wherein said additive is selected from the group consisting of polyethylene glycol (PEG)6000, PEG4000 and PEG 8000.
12. The agrochemical composition according to claim 1, wherein said composition comprises from about 1% to about 30% additives by weight per weight of the total weight of said agrochemical composition.
13. The agrochemical composition according to claim 1, wherein said composition is formulated in the form of a dry formulation dry suspension (DF).
14. A method for preparing a stable agrochemical composition, wherein said method comprises:
(a) mixing at least one low melting active ingredient, at least one moisture sensitive active ingredient, and an additive to obtain a premix, wherein the additive has a softening or melting point that is lower than the melting point of the low melting active ingredient;
(b) optionally adding one or more performance enhancing agents to the premix; and
(c) and extruding and granulating the premix.
15. The method of claim 14, wherein said extrusion granulating the premix comprises extruding and granulating the premix separately, sequentially, or simultaneously.
16. The method of claim 14, comprising:
(a) mixing an active ingredient selected from at least one low melting pyrethroid with a desired amount of precipitated silica to obtain a premix;
(b) milling the premix in a jet mill with or without other additives to obtain a milled low-melting pyrethroid of a desired particle size;
(c) adding an organophosphorus active ingredient and an additive to the ground low-melting pyrethroid, wherein the additive has a softening point or a melting point that is lower than the melting point of the low-melting active ingredient, and any other necessary additive or additives, and mixing them to obtain a premix;
(d) subjecting the premix to extrusion granulation to obtain the granules.
17. A method of controlling pests, the method comprising applying an agrochemical composition to a pest at a locus, the agrochemical composition comprising:
a) at least one low melting active ingredient;
b) at least one moisture sensitive active ingredient; and
c) an additive, characterized in that the additive has a softening or melting point lower than the melting point of the low-melting active ingredient.
18. The method of claim 17, wherein the agrochemical composition is applied to control a pest at the locus, said pest being selected from insects of the order lepidoptera, coleoptera (Coleoptran), diptera and hemiptera.
19. A kit, comprising:
(a) at least one low melting active ingredient component;
(b) at least one moisture sensitive active ingredient component; and
(c) an additive component, characterized in that the additive has a softening or melting point lower than the melting point of the low-melting active ingredient.
20. A kit comprising from about 5.0 wt/wt% to about 80 wt/wt% of a acephate component indicated for use, from about 1.0 wt/wt% to about 20 wt/wt% of a bifenthrin component indicated for use, and from about 5.0 wt/wt% to about 20 wt/wt% of a PEG 6000 component indicated for use.
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| GB9018227D0 (en) * | 1990-08-20 | 1990-10-03 | Wellcome Found | Pesticidal formulations |
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2018
- 2018-05-16 EP EP18804969.6A patent/EP3629733A4/en active Pending
- 2018-05-16 CN CN201880049879.5A patent/CN111405848A/en active Pending
- 2018-05-16 CA CA3064494A patent/CA3064494C/en active Active
- 2018-05-16 EA EA201992813A patent/EA201992813A1/en unknown
- 2018-05-16 WO PCT/IB2018/053406 patent/WO2018215883A1/en active Application Filing
- 2018-05-16 AU AU2018272316A patent/AU2018272316B2/en active Active
- 2018-05-16 MX MX2019013942A patent/MX2019013942A/en unknown
- 2018-05-16 UA UAA201912233A patent/UA126500C2/en unknown
- 2018-05-22 BR BR102018010395-4A patent/BR102018010395A2/en not_active Application Discontinuation
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2019
- 2019-11-21 CL CL2019003350A patent/CL2019003350A1/en unknown
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| CN105010355A (en) * | 2015-06-30 | 2015-11-04 | 郑州郑氏化工产品有限公司 | Antimicrobial insecticidal composition used for paddy rice field and preparation method of its water dispersible granules |
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Also Published As
| Publication number | Publication date |
|---|---|
| EA201992813A1 (en) | 2020-03-19 |
| AU2018272316B2 (en) | 2022-06-02 |
| WO2018215883A1 (en) | 2018-11-29 |
| CL2019003350A1 (en) | 2020-04-17 |
| CA3064494C (en) | 2023-01-31 |
| CA3064494A1 (en) | 2018-11-29 |
| EP3629733A1 (en) | 2020-04-08 |
| EP3629733A4 (en) | 2021-03-10 |
| MX2019013942A (en) | 2020-07-20 |
| BR102018010395A2 (en) | 2018-12-26 |
| AU2018272316A1 (en) | 2019-12-12 |
| UA126500C2 (en) | 2022-10-19 |
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