Pesticide composition resistant to degradation of active ingredient and preparation process thereof

Abstract

The present invention provides compositions containing phosphoramidothioates that are resistant to degradation of the active ingredient.The present invention provides a process for preparing granular compositions containing acephate that are resistant to degradation of the active ingredient, the process comprising the use of a mixture of water and an electrolyte.

Description

[Technical field]

[0001] The present invention relates to an insecticide composition that is resistant to the decomposition of the active ingredient. The present invention provides a composition that includes a phosphoramidothioate that is resistant to the decomposition of the active ingredient. The present invention further provides a process for preparing a granular composition that includes a phosphoramidothioate that is resistant to the decomposition of the active ingredient, the process comprising the use of water and an electrolyte. [Background technology]

[0002] Phosphoramidothioates are known for their excellent insecticidal activity against a wide variety of insects in a variety of environments. Acephate, a systemic insecticide, is one of the widely used phosphoramidothioates to control a wide range of chewing and sap-sucking insects, such as aphids, thrips, lepidopteran larvae, sawflies, leafminers, leafhoppers, cutworms, etc., in fruits (including citrus), vines, hops, olives, cotton, soybeans, peanuts, macadamia nuts, beets, brassicas, celery, beans, potatoes, rice, tobacco, ornamentals, forests, and other crops.

[0003] Phosphoramidothioates are known to suffer from stability problems due to their hydrolytic sensitivity. Attempts have been made in the art to solve the problems related to the decomposition of acephate and to prepare stable pesticide products. Some of these methods include the use of solvents as extrusion aids, maintaining specific temperature conditions during extrusion, using specific equipment such as compression and other stabilizers, and employing special procedures.

[0004] US Patent No. 5,298,501 discloses a chemically stable insecticide composition of phosphoramidothioate, which contains at least 83% ammonium sulfate, which is effective for granulating the insecticide ingredient, without facing chemical stability problems due to hydrolytic and catalytic decomposition of phosphoramidothioate, which would shorten the shelf life of the product.

[0005] US Patent No. 5,464,623 discloses a method for preparing a stable pesticide composition containing acephate. The method involves mixing the dry pesticide composition with 3-25% solvent to form a mixture similar to moist sandy loam, followed by extrusion. The preferred solvent should have high volatility so that the pellets can be dried. The method further uses a dehydrating agent to absorb traces of water present in the pellets to prevent hydrolysis of the pesticide. The method is not very safe for the environment.

[0006] What is sometimes needed is a granulation technique that utilizes commonly operated granulation equipment and avoids the use of environmentally unsafe solvents, special techniques or equipment.

[0007] The present inventors have established a safe and environmentally friendly formulation method using water as a medium to obtain a stable insecticide composition containing acephate. Summary of the Invention

[0008] It is an object of the present invention to provide an environmentally safe granulation process for compositions containing phosphoramidothioates.

[0009] Another object of the present invention is to provide compositions containing phosphoramidothioates that are resistant to degradation of the active ingredient. [Means for solving the problem]

[0010] In one aspect, the present invention provides a method for producing a method for treating a cancer cell comprising: a) a phosphoramidothioate; and b) an electrolyte; The composition is formulated using a mixture of water and the electrolytes.

[0011] In another aspect, the present invention provides a method for producing a composition comprising: c) phosphoramidothioates as active ingredients; d) an electrolyte; and The composition is formulated using a mixture of water and the electrolyte.

[0012] In another aspect, the present invention provides a method for producing a composition comprising: a) acephate, b) an electrolyte; and The composition is formulated using a mixture of water and the electrolyte.

[0013] In another aspect, the present invention provides a method for producing a composition comprising: a) a phosphoramidothioate as an active ingredient; b) an electrolyte; c) one or more active ingredients; and The composition is formulated using a mixture of water and the electrolyte.

[0014] In another aspect, the present invention provides a process for preparing a phosphoramidothioate composition that is resistant to degradation of an active ingredient, the process comprising: Step 1: Preparing a mixture of water and electrolytes; Step 2: Preparing a blend of phosphoramidothioate, remaining electrolytes, if present, and other excipients; Step 3: preparing an admixture of step 2 by blending with the admixture of step 1; Step 4: Formulating into a suitable form using a suitable device.

[0015] In another aspect, the present invention provides a process for preparing a phosphoramidothioate composition that is resistant to degradation of an active ingredient, the process comprising: Step 1: Preparing a mixture of water and electrolytes; Step 2: Preparing a blend of phosphoramidothioate, remaining electrolytes, if present, one or more other active ingredients, and other excipients; Step 3: preparing the mixture of step 2 by blending with the mixture of step 1; Step 4: Formulating into a suitable form using a suitable device.

[0016] In another aspect, the present invention provides a process for preparing a composition of acephate that is resistant to degradation of the active ingredient, the process comprising: Step 1: Preparing a mixture of water and electrolytes; Step 2: Preparing a blend of acephate, remaining electrolytes, if present, and other excipients; Step 3: preparing the mixture of step 2 by blending with the mixture of step 1; Step 4: Formulating into a suitable form using a suitable device.

[0017] In another aspect, the present invention provides a method of combating insects comprising applying an effective amount of a composition according to the present invention to the area to be treated.

[0018] Further features and advantages of the proposed invention will become apparent from the following detailed description, which illustrates the most preferred features of the proposed invention, and should not be construed as limiting the scope of the invention as described herein. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS

[0019] Unless otherwise defined, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this invention belongs. It should be noted that as used herein, the singular forms "a," "an," and "the" include plural referents unless the content clearly dictates otherwise.

[0020] The term "about" as used to qualify the amounts of mancozeb and carbendazim shall be interpreted to mean "approximately" or "reasonably close" and any statistically significant variation therefrom.

[0021] As used herein, the terms "comprising," "including," "having," "containing," "involving," and the like, should be understood to be open-ended, i.e., to mean including but not limited to. The terms "preferred" and "preferably" refer to embodiments of the invention that may provide certain benefits, under certain circumstances.

[0022] In one embodiment, the aspects and embodiments described herein are also intended to be construed to replace the phrase "comprising" with either "consisting of," or "consisting essentially of," or "consisting substantially of."

[0023] The present invention provides a composition that is resistant to the decomposition of active ingredients. It has been observed that moisture-sensitive active ingredients require specific equipment and conditions to prepare a stable commercial product. Surprisingly, the inventors of the present invention have found that when moisture-sensitive active ingredients are used, a stable composition can be prepared by a suitable process that includes the use of water and electrolytes. The method can also be used when combination products are prepared with moisture-sensitive active ingredients.

[0024] Thus, the present invention provides compositions that are resistant to degradation of the active ingredient.

[0025] The present invention relates to a) a phosphoramidothioate as an active ingredient; b) an electrolyte; The composition is formulated using a mixture of water and the electrolyte.

[0026] In one embodiment, the phosphoramidothioate active ingredient is selected from acephate, chloramine phosphorus, isocarbophos, isofenphos, isofenphos-methyl, methamidophos, phosglycine, or propetamphos.

[0027] In a preferred embodiment, the phosphoramidothioate active ingredient is acephate.

[0028] The present invention relates to a) acephate, b) an electrolyte; and The composition is formulated using a mixture of water and the electrolyte.

[0029] The term degradation refers to chemical degradation, which includes hydrolysis, photolysis, and catalytic degradation.

[0030] In one embodiment, the present invention provides for controlled degradation of the active ingredient.

[0031] In another embodiment, the present invention provides for controlled degradation of acephate.

[0032] In another embodiment, the present invention provides that the decomposition of acephate is controlled to <5% by weight of acephate in the composition.

[0033] In one embodiment, the composition according to the present invention provides controlled degradation of acephate even after using water as a formulation medium.

[0034] In another embodiment, in the composition according to the present invention, the degradation of acephate is controlled to less than 5% even after using water as a medium for formulation.

[0035] In another embodiment, the composition according to the present invention controls the degradation of acephate to <3% even after using water as a formulation medium.

[0036] In one embodiment, the composition comprises acephate in an amount from about 0.1% to about 99% by weight of the composition.

[0037] In another embodiment, the composition comprises acephate in an amount from about 1% to about 97% by weight of the composition.

[0038] In one embodiment, water is used as a medium for formulating the compositions according to the present invention.

[0039] In one embodiment, the composition comprises an electrolyte.

[0040] In one embodiment, the composition comprises an electrolyte in an amount of about 1% to about 97% by weight of the composition.

[0041] In another embodiment, the composition comprises an electrolyte in an amount of about 1% to about 50% by weight of the composition.

[0042] In one embodiment, the electrolyte is selected from an inorganic salt or an organic salt.

[0043] In one embodiment, the inorganic salt is selected from the group including salts of strong acids with strong bases, salts of strong acids with weak bases, salts of weak acids with strong bases, and salts of weak acids with weak bases.

[0044] In a preferred embodiment, the inorganic salt is a salt of a strong acid with a weak base.

[0045] In one embodiment, the inorganic salts are selected from ammonium salts, alkali and alkaline earth metal salts, and the like.

[0046] In another embodiment, the inorganic salts are selected from phosphates, carbonates, sulfates, chlorides, nitrates, oxides, hydroxides, and the like.

[0047] In another embodiment, the organic salt is selected from alkali or alkaline earth metal salts of an organic acid.

[0048] In yet another embodiment, the organic salt is selected from alkaline earth metal salts of weak organic acids.

[0049] In another embodiment, the weak organic acids include acetic acid, oxalic acid, citric acid, tartaric acid, propionic acid, and the like.

[0050] In one embodiment, the electrolyte is selected from the group including sodium chloride, calcium chloride, potassium chloride, magnesium chloride, sodium acetate, calcium acetate, magnesium carbonate, sodium carbonate, calcium carbonate, potassium carbonate, calcium phosphate, sodium phosphate, ammonium phosphate, diammonium phosphate dihydrate, magnesium phosphate, ammonium sulfate, ammonium chloride, ammonium acetate, magnesium sulfate, sodium sulfate, calcium sulfate, zinc sulfate, sodium acetate, calcium oxalate, calcium acetate, trisodium citrate, and the like.

[0051] In one embodiment, the present invention provides a) a phosphoramidothioate as an active ingredient; b) an electrolyte; c) one or more active ingredients; and The composition is formulated using a mixture of water and the electrolyte.

[0052] In one embodiment, the composition according to the invention comprises one or more further active ingredients.

[0053] In one embodiment, further active ingredients that may be present in the composition according to the invention are selected from insecticides, attractants, bactericides, acaricides, nematicides, fungicides, herbicides and growth regulators.

[0054] In another embodiment, the active ingredients that may be present in the composition according to the invention are selected from organophosphorus compounds, chloronicotinyl compounds, diamide insecticides, benzoylphenylurea chitin synthesis inhibitors, or pyrethroid compounds.

[0055] In yet another embodiment, the organophosphorus compound may be any of the following: aspon, azinphos-methyl, carbofuran, carbophenothion, chlorfenvinphos, chlorpyrifos, coumaphos, crotoxyphos, crufomate, demeton, diazinon, dichlorvos, dicrotophos, methoate, dioxathion, disulfoton, EPN, ethion, ethoprop, famflu, fenamiphos, fenitrothion, fensulfothion, fenthion, fonofos, isofenphos, malathion, methamidophos, methidathion, methyl parathion, mevinphos, monocrotophos, metam sodium, naled, oxydemeton-methyl, parathion, phorate, phosalone, phosmet, phosphamidon, profenofos, temephos, TEPP, terbufos, tetrachlorvinphos, trichlorfon, The active ingredient may be selected from cypermethrin, fenvalerate, permethrin, alpha-cypermethrin, beta-cypermethrin, zeta-cypermethrin, deltamethrin, cyfluthrin, bifenthrin, lambda-cyhalothrin, and / or bioresmethrin, afoxolaner brofuranilide, chlorantraniliprole, cyantraniliprole, cyclaniliprole, cyhalodiamide, flubendiamide, fluralaner, lotilaner, tetrachlorantraniliprole, tetraniliprole, bistrifluron, chlorbenzuron, chlorfluazuron, dichlorbenzuron, diflubenzuron, flucycloxuron, flufenoxuron, hexaflumuron, lufenuron, novaluron, noviflumuron, penfluron, teflubenzuron, triflumuron, or mixtures thereof.

[0056] In another embodiment, the chloronicotinyl compound may be selected from, but is not limited to, acetamiprid, imidacloprid, thiacloprid, thiamethoxam, and combinations thereof.

[0057] In another embodiment, the pyrethroid may be selected from, but is not limited to, cypermethrin, fenvalerate, permethrin, alpha-cypermethrin, beta-cypermethrin, zeta-cypermethrin, deltamethrin, cyfluthrin, bifenthrin, lambda-cyhalothrin, and / or bioresmethrin, or mixtures thereof.

[0058] In another embodiment, the active ingredients that may be present in the composition according to the invention are nitrothar-isopropyl, myclobutanil, piproctanil bromide, jodofenphos, imazalil, lambda-cyhalothrin, triflumizole, vamidothion, xylylcarb, tolclofos-methyl, protoate, pyriproxyfen, propamocarb hydrochloride, tefluthrin, resmethrin, chlorpropham, cloethocarb, demeton-S, cyfluthrin, azinphos-ethyl, azinphos-methyl, benalaxyl, benazolin-ethyl, butocarboxim, benzoximate, bioresmethrin, bromopropylate, borax, biphenyl, fluoroglycofen-ethyl, fenbucarb, fenthioca

[0033] The compound is selected from the group consisting of rubu, fensulfothion, fosmetilan, furalaxyl, dikegulac, trinexapac-ethyl, ethiofencarb, etridiazole, fenamiphos, fenazaquin, EPN, dodemorph, mecarfone, etaconazole, fluorbenside, flumecyclox, fenfluthrin, fluenethyl, acequinocyl, schradan, transfluthrin, cyprodinil, phosphoran, crufomate, chlorphoxim, chloropropylate, di-alate, chlorofenprop, camphechlor, chlorbencide, chlordimeform, phosphonic acid, trifloxystrobin, picoxystrobin, gamma-cyhalothrin, codremon, spinetoram, and cyflumetofen.

[0059] The present invention relates to a) acephate as the active ingredient; b) an electrolyte; and c) one or more additional active ingredients, The composition is formulated using a mixture of water and the electrolyte.

[0060] In another embodiment, another active ingredient that may be present in the composition according to the invention is selected from an organophosphorus compound, a chloronicotinyl compound, or a pyrethroid compound.

[0061] In another embodiment, the active ingredients that may be present in the composition according to the invention are selected from acetamiprid, imidacloprid, thiacloprid, thiamethoxam, cypermethrin, fenvalerate, permethrin, alpha-cypermethrin, beta-cypermethrin, zeta-cypermethrin, deltamethrin, cyfluthrin, bifenthrin, lambda-cyhalothrin, bioresmethrin, or mixtures thereof.

[0062] In one embodiment, the electrolyte is selected from an inorganic salt or an organic salt.

[0063] In a preferred embodiment, the inorganic salt is a salt of a strong acid with a weak base.

[0064] In one embodiment, the inorganic salts are selected from ammonium salts, alkali and alkaline earth metal salts, and the like.

[0065] In another embodiment, the inorganic salts are selected from phosphates, carbonates, sulfates, chlorides, oxides, hydroxides, and the like.

[0066] In another embodiment, the weak organic acids include acetic acid, oxalic acid, citric acid, tartaric acid, propionic acid, and the like.

[0067] In one embodiment, the electrolyte is selected from the group including sodium chloride, calcium chloride, potassium chloride, magnesium chloride, sodium acetate, calcium acetate, magnesium carbonate, sodium carbonate, calcium carbonate, potassium carbonate, calcium phosphate, sodium phosphate, ammonium phosphate, diammonium phosphate dihydrate, magnesium phosphate, ammonium sulfate, ammonium chloride, ammonium acetate, magnesium sulfate, sodium sulfate, calcium sulfate, zinc sulfate, sodium acetate, calcium oxalate, calcium acetate, trisodium citrate, and the like.

[0068] Thus, in one embodiment, the present invention provides a method for producing a composition comprising: a) acephate, b) an electrolyte; c) one or more active ingredients selected from acetamiprid, imidacloprid, thiacloprid, thiamethoxam, cypermethrin, fenvalerate, permethrin, alpha-cypermethrin, beta-cypermethrin, zeta-cypermethrin, deltamethrin, cyfluthrin, bifenthrin, lambda-cyhalothrin, bioresmethrin, or mixtures thereof;

[0069] The composition is formulated using a mixture of water and the electrolyte. a) acephate, b) an electrolyte; c) providing a composition resistant to degradation of an active ingredient, the composition comprising: The composition is formulated using a mixture of water and the electrolyte.

[0070] In another embodiment, the present invention provides a) acephate, b) an electrolyte; c) beta-cypermethrin; and The composition is formulated using a mixture of water and the electrolyte.

[0071] In another embodiment, the present invention provides a) acephate, b) an electrolyte; c) providing a composition resistant to degradation of an active ingredient, the composition comprising: The composition is formulated using a mixture of water and the electrolyte.

[0072] In yet another embodiment, the present invention provides a method for producing a) acephate, b) an electrolyte; c) imidacloprid; and The composition is formulated using a mixture of water and the electrolyte.

[0073] In one embodiment, the present invention provides a process for preparing a composition that is resistant to degradation of an active ingredient, the process comprising: Step 1: Preparing a mixture of water and electrolytes; Step 2: Preparing a blend of phosphoramidothioate, remaining electrolytes, if present, and other excipients, if necessary; Step 3: preparing the mixture of step 2 by blending with the mixture of step 1; Step 4: Formulating the mixture into a suitable form using a suitable device.

[0074] In another embodiment, the present invention provides a process for preparing a composition that is resistant to degradation of an active ingredient, the process comprising: Step 1: Preparing a mixture of water and electrolytes in the required manner; Step 2: Preparing a blend of acephate, remaining electrolytes, if present, and other excipients, if necessary; Step 3: preparing the mixture of step 2 by blending with the mixture of step 1; Step 4: Formulating the mixture into a suitable form using a suitable device.

[0075] In one embodiment, the composition further comprises one or more other active ingredients.

[0076] In another embodiment, the present invention provides a process for preparing a composition that is resistant to degradation of an active ingredient, the process comprising: Step 1: Preparing a mixture of water and electrolytes in the required manner; Step 2: Preparing a blend of acephate, remaining electrolytes, if present, and one or more other active ingredients and other excipients, if necessary; Step 3: preparing the mixture of step 2 by blending with the mixture of step 1; Step 4: Formulating the mixture into a suitable form using a suitable device.

[0077] In one embodiment, the process involves the use of an electrolyte.

[0078] In one embodiment, the electrolyte is selected from an inorganic salt or an organic salt.

[0079] In one embodiment, the inorganic salt is selected from the group including salts of strong acids with strong bases, salts of strong acids with weak bases, salts of weak acids with strong bases, and salts of weak acids with weak bases.

[0080] In a preferred embodiment, the inorganic salt is a salt of a strong acid with a weak base.

[0081] In one embodiment, the inorganic salts are selected from ammonium salts, alkali and alkaline earth metal salts, and the like.

[0082] In another embodiment, the inorganic salts are selected from phosphates, carbonates, sulfates, chlorides, oxides, hydroxides, and the like.

[0083] In another embodiment, the organic salt is selected from alkali or alkaline earth metal salts of an organic acid.

[0084] In yet another embodiment, the organic salt is selected from alkali or alkaline earth metal salts of weak organic acids.

[0085] In another embodiment, the weak organic acids include acetic acid, oxalic acid, citric acid, tartaric acid, propionic acid, and the like.

[0086] In one embodiment, the electrolyte is used as a mixture in water in the process of making the composition.

[0087] In another embodiment, the mixture of electrolyte and water comprises a solution, a suspension, or the like.

[0088] In one embodiment, water is used in an amount of about 1% to about 40% by weight of the composition suitable for the process.

[0089] In another embodiment, water is used in an amount of about 1% to about 20% by weight of the composition suitable for the process.

[0090] In another embodiment, water is used in an amount of about 1% to about 10% by weight of the composition suitable for the process.

[0091] In another embodiment, the amount of electrolyte required to make a mixture in water varies from about 1% to about 25% by weight of the composition.

[0092] In yet another embodiment, the amount of electrolyte required to form a mixture in water varies from about 1% to about 15% by weight of the composition.

[0093] In one embodiment, suitable processing of the composition calls for a ratio of water and electrolyte of about 1:1 to about 1:20.

[0094] In another embodiment, suitable processing of the composition calls for a ratio of water and electrolyte of about 1:1 to about 1:10.

[0095] In one embodiment, in step 2, preparing a blend of acephate, electrolytes, and other excipients, and optionally other active ingredients, is not particularly limited.

[0096] In one embodiment, in step 3, the use of the mixture from step 1 to prepare a mixture of products from step 2 is not particularly limited.

[0097] In one embodiment, in step 3, the mixture is prepared by spraying the mixture of step 1 onto the product of step 2.

[0098] In another embodiment, in step 3, the mixture is prepared by adding the mixture of step 1 to the product of step 2 batchwise.

[0099] In one embodiment, in step 4, the formulation process is not particularly limited.

[0100] In a preferred embodiment, in step 4, the composition is formulated as a granule.

[0101] In one embodiment, step 4 of the process uses readily available commercial extrusion equipment.

[0102] In one embodiment, in step 4 of the process, the moisture in the granules is significantly reduced.

[0103] In one embodiment, the process provides a granule with at least a partial or complete moisture barrier on the surface of the material to prevent it from decomposing.

[0104] In one embodiment, the moisture barrier comprises an electrolyte.

[0105] In another embodiment, the term granules refers to solid pellets, granules, grains, and the like.

[0106] Typically, a process for preparing a composition resistant to degradation of an active ingredient includes preparing a mixture of water and electrolytes (Part A), preparing a blend of phosphoramidothioate, remaining electrolytes (Part B), and optionally one or more other active ingredients and other excipients, preparing the blend by mixing the mixture of Part A and Part B, and formulating the mixture into a suitable form using a suitable device.

[0107] Preferably, the process is carried out at room temperature and the blend is extruded using a basket extruder to obtain granules. The granules are dried (until the moisture content is <1%) and then packed.

[0108] The formulations are prepared by wet granulation methods known to those skilled in the art.

[0109] The stable pesticide compositions of the present invention may further comprise one or more dispersants, wetting agents, carriers, anticaking agents, pH adjusters, preservatives, biocides, defoamers, colorants, and other formulation aids.

[0110] The dispersants may be selected from ionic and non-ionic dispersants such as salts of polystyrene sulfonic acid, salts of polyvinyl sulfonic acid, salts of naphthalene sulfonic acid / formaldehyde condensates, salts of condensates of naphthalene sulfonic acid, phenol sulfonic acid, and formaldehyde, and salts of lignosulfonic 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, further polyvinyl alcohol, polyvinyl pyrrolidone, copolymers of polyvinyl alcohol and polyvinyl pyrrolidone, and copolymers of (meth)acrylic acid and (meth)acrylic acid esters, further alkyl ethoxylates and alkylaryl ethoxylates ethoxylated alkylaryl phosphated and sulfated esters.

[0111] Wetting agents may be selected from salts of aliphatic monoesters of sulfonic acid, including but not limited to sodium lauryl sulfate, sulfoakylamides and their salts, including but not limited to Na N-methyl-N-oleoyl taurate, akyl aryl sulfonates, including but not limited to akyl benzene sulfonates and their salts, and aryl naphthalene sulfonates and their salts, and salts of lignosulfonic acid.

[0112] Carriers may include clays, silicas, sulfates, chlorides, carbohydrates, alkylated celluloses, and the like.

[0113] In one embodiment, the present invention provides a method of combating insects comprising applying an effective amount of a composition according to the present invention to the area to be treated.

[0114] In one embodiment, a) a phosphoramidothioate; and b) an electrolyte; and c) an effective amount of a composition that is resistant to degradation of the active ingredient, the composition comprising: The composition is formulated using a mixture of water and the electrolyte.

[0115] In one embodiment, a) acephate, b) an electrolyte; and c) an effective amount of a composition that is resistant to degradation of the active ingredient, the composition comprising: The composition is formulated using a mixture of water and the electrolyte.

[0116] In another embodiment, a) a phosphoramidothioate; and b) an electrolyte; c) one or more active ingredients; and c) applying to the area to be treated an effective amount of a composition that is resistant to degradation of the active ingredients, the composition comprising: The composition is formulated using a mixture of water and the electrolyte.

[0117] In another embodiment, a) acephate, b) an electrolyte; c) one or more active ingredients; and c) applying to the area to be treated an effective amount of a composition that is resistant to degradation of the active ingredients, the composition comprising: The composition is formulated using a mixture of water and the electrolyte.

[0118] In one embodiment, the present invention may provide a method of controlling insects, such as those belonging to the Lepidopteran, Coleopteran, Dipteran, and Hemipteran classes of insects.

[0119] Thus, the present invention provides a) acephate, b) an electrolyte; c) optionally, applying to the area to be treated an effective amount of a composition comprising one or more active ingredients; The composition is formulated using a mixture of water and the electrolyte.

[0120] In another embodiment, the method comprises: a) acephate, b) an electrolyte; c) applying to the area to be treated an effective amount of a composition comprising one or more active ingredients; The composition is formulated using a mixture of water and the electrolyte.

[0121] In another embodiment, the present invention provides the use of the composition to combat insects.

[0122] The present invention will be described in more detail by the following examples. However, it should be understood that the scope of the present invention is not limited by the examples in any way. It will be understood by those skilled in the art that the present invention includes the following examples and can be further modified and altered within the technical scope of the present invention. EXAMPLES

[0123] Example 1: A composition of acephate and beta-cypermethrin according to the present invention was prepared as shown below.

[0124] a) The raw materials used in the composition are listed below: [Table 1]

[0125] b) The final composition of the product is shown in the table below: [Table 2]

[0126] c) Process: A weighed amount of sodium acetate was added to water (4 mL) to prepare a mixture (Part A). A weighed amount of acephate and precipitated silica were thoroughly mixed. Beta-cypermethrin, sodium lauryl sulfate, and styrene acrylic polymer dispersant were ground together and mixed with the acephate mixture (Part B) at room temperature. Part B was then mixed with the mixture of Part A to prepare a blend. The blend was then extruded using a basket extruder to obtain granules. The granules were dried (until moisture content was <1%) and then packed.

[0127] Example 2: Acephate compositions according to the present invention were prepared as shown below.

[0128] a) The raw materials used in the composition are listed below: [Table 3]

[0129] b) The final composition of the product is shown in the table below: [Table 4]

[0130] c) Process: Ammonium sulfate was added to water (5 mL) to prepare a mixture (Part A). A weighed amount of acephate and precipitated silica were milled using a suitable equipment to obtain the required particle size (Part B). Part B was then mixed with the mixture of Part A to prepare a blend. The blend was then extruded using a basket extruder to obtain granules. The granules were dried (until moisture content was <0.6%) and then packed.

[0131] Example 3: A composition of acephate and beta-cypermethrin according to the present invention was prepared as shown below.

[0132] a) The raw materials used in the composition are listed below: [Table 5]

[0133] b) The final composition of the product is shown in the table below: [Table 6]

[0134] c) A composition was prepared according to the process of Example 1.

[0135] Example 4: A composition of acephate and imidacloprid according to the present invention was prepared as follows.

[0136] a) The raw materials used in the composition are listed below: [Table 7]

[0137] b) The final composition of the product is shown in the table below: [Table 8]

[0138] c) A composition was prepared according to the process of Example 1.

[0139] Example 5: A composition of acephate and imidacloprid according to the present invention was prepared as follows.

[0140] a) The raw materials used in the composition are listed below: [Table 9]

[0141] b) The final composition of the product is shown in the table below: [Table 10]

[0142] C) Process: About 10 g of ammonium sulfate was mixed with water (10 mL) to obtain a mixture (Part A). A weighed amount of imidacloprid, ammonium sulfate and the remaining portion of the surfactant were milled using a suitable equipment to obtain a mixture of required particle size. A weighed amount of acephate was then mixed to obtain a mixture of Part B. Part A and Part B were then blended to prepare a blend. The blend was then extruded using an extruder. The resulting product was then dried and packed.

[0143] Example 6: A composition of acephate according to the invention was prepared as follows.

[0144] a) The raw materials used in the composition are listed below: [Table 11]

[0145] b) The final composition of the product is shown in the table below: [Table 12]

[0146] b) A composition was prepared according to the process of Example 2.

[0147] Example 7: A composition of acephate according to the invention was prepared as follows.

[0148] a) The raw materials used in the composition are listed below: [Table 13]

[0149] b) The final composition of the product is shown in the table below: [Table 14]

[0150] c) A composition was prepared according to the process of Example 2.

[0151] Example 8: A composition of acephate and beta-cypermethrin according to the present invention was prepared as shown below.

[0152] a) The raw materials used in the composition are listed below: [Table 15]

[0153] b) The final composition of the product is shown in the table below: [Table 16]

[0154] b) A composition was prepared according to the process of Example 1.

[0155] Example 9: A composition of acephate and beta-cypermethrin according to the present invention was prepared as shown below.

[0156] a) The raw materials used in the composition are listed below: [Table 17]

[0157] b) The final composition of the product is shown in the table below: [Table 18]

[0158] a) A composition was prepared according to the process of Example 1.

[0159] Example 10: A composition of acephate and beta-cypermethrin according to the present invention was prepared as shown below.

[0160] a) The raw materials used in the composition are listed below: [Table 19]

[0161] b) The final composition of the product is shown in the table below: [Table 20]

[0162] a) A composition was prepared according to the process of Example 1.

[0163] Example 11: A composition of acephate and beta-cypermethrin according to the present invention was prepared as shown below.

[0164] a) The raw materials used in the composition are listed below: [Table 21]

[0165] b) The final composition of the product is shown in the table below: [Table 22]

[0166] a) A composition was prepared according to the process of Example 1.

[0167] Example 12: A composition of acephate and beta-cypermethrin according to the present invention was prepared as shown below.

[0168] a) The raw materials used in the composition are listed below: [Table 23]

[0169] b) The final composition of the product is shown in the table below: [Table 24]

[0170] a) A composition was prepared according to the process of Example 1.

[0171] Example 13: A composition of acephate and bifenthrin according to the present invention was prepared as follows.

[0172] a) The raw materials used in the composition are listed below: [Table 25]

[0173] b) The final composition of the product is shown in the table below: [Table 26]

[0174] d) Process: The composition was prepared following the process of Example 1.

[0175] Stability testing of the compositions according to the invention: The compositions according to the invention were tested for stability: samples were kept at 54±2° C. for up to 14 days and tested for stability parameters such as suspendability, dispersibility, wet sieving analysis and degradation of the active ingredient.

[0176] Example 14: The physical parameters of the compositions containing acephate prepared as in Example 2 are presented in the table below.

[0177] [Table 27]

[0178] Example 15: The physical parameters of the compositions containing acephate and imidacloprid prepared as in Example 5 are presented in the table below.

[0179] [Table 28]

[0180] Active ingredient decomposition %: [Table 29]

[0181] Example 16: The physical parameters of the compositions containing Acephate and Bifenthrin prepared as in Example 13 are presented in the table below.

[0182] [Table 30]

[0183] Active ingredient decomposition %: [Table 31]

[0184] From the above experimental results, it is established that the present invention provides a stable composition containing acephate. The decomposition of acephate is substantially controlled, resulting in a composition that can be stored for a longer period of time. It is further noted by the inventors that the composition according to the present invention requires only a few inversions while dispersing the product. (The number of inversions of the formulation is an indication of the ease of dispersing the product). The suspending properties of the composition are also well maintained, resulting in an improved shelf life and a product that largely meets all the requirements regarding the intended activity of the composition.

[0185] Comparative Example Comparative Example 1: Acephate compositions were prepared as shown below.

[0186] a) The raw materials used in the composition are listed below: [Table 32]

[0187] b) The final composition of the product is shown in the table below: [Table 33]

[0188] c) Process: Weighed amounts of acephate and ammonium sulfate were mixed together and milled using a suitable device to obtain the required particle size. Water was added to prepare the blend. The blend was then extruded using a basket extruder to obtain granules. The granules were then dried and packed.

[0189] Comparative Example 2 Acephate and imidacloprid compositions were prepared as follows.

[0190] a) The raw materials used in the composition are listed below: [Table 34]

[0191] b) The final composition of the product is shown in the table below: [Table 35]

[0192] C) Process: A weighed amount of imidacloprid, ammonium sulfate, and surfactant are ground using a suitable device. The same process as Comparative Example-1 is followed to obtain a mixture of required particle size. A weighed amount of acephate is then mixed to obtain a premix mixture. Water is added to the premix mixture to prepare a blend. The blend is then extruded using an extruder. The resulting product is then dried and packed. The compositions of Comparative Examples 1 and 2 were tested for stability. Samples were maintained at 54±2° C. for up to 14 days and tested for stability parameters such as suspendability, dispersibility, wet sieving analysis, and degradation of active ingredients.

[0193] The physical parameters of the composition containing acephate according to Comparative Example 1 are given below.

[0194] [Table 36]

[0195] The physical parameters of the composition containing acephate and imidacloprid according to Comparative Example 2 are shown below.

[0196] [Table 37]

[0197] Active ingredient decomposition %: [Table 38]

[0198] Comparative Example 3: A composition of acephate and bifenthrin was prepared as follows.

[0199] [Table 39]

[0200] Process: A weighed amount of bifenthrin was mixed with Mfill A-100 to form a bifenthrin premix. The bifenthrin premix was milled in an air jet mill to obtain the desired particle size. A weighed amount of acephate and other surfactants were then added to the bifenthrin premix to obtain the bifenthrin-acephate premix. The bifenthrin-acephate premix was then extruded by hot melt extrusion process on a screw extruder. The granules thus obtained were then sieved to remove oversized and undersized granules. The finished granules were filled according to quality specifications.

[0201] The physical parameters of the composition containing acephate and imidacloprid according to Comparative Example 3 are shown below.

[0202] [Table 40]

[0203] The above experimental results show that following conventional procedures for preparing compositions containing acephate leads to the decomposition of acephate, which cannot be stored for a longer period of time.It is further noted that the compositions according to conventional procedures require many inversions while dispersing the formulation.The suspending property of the composition is also not within the acceptable limit, making it unsuitable for the intended activity of the product.

Claims

1. 1. A composition comprising: a) acephate, b) an electrolyte; and c) optionally with one or more active ingredients other than acephate; wherein said composition is formulated using a mixture of water and said electrolyte in a ratio of 1:1 to 1:20, and wherein degradation of said acephate in said composition is controlled to less than 5% of the weight of said acephate in said composition.

2. The composition of claim 1 , wherein the electrolyte is selected from an inorganic salt or an organic salt.

3. 3. The composition of claim 2, wherein the inorganic salt is selected from the group consisting of a salt of a strong acid with a strong base, a salt of a strong acid with a weak base, a salt of a weak acid with a strong base, and a salt of a weak acid with a weak base.

4. 4. The composition of claim 3, wherein the inorganic salt is selected from the group comprising ammonium salts, alkali and alkaline earth metal salts, phosphates, carbonates, sulfates, nitrates, chlorides, oxides, or hydroxides.

5. 3. The composition of claim 2, wherein the organic salt is selected from alkali or alkaline earth metal salts of organic acids and alkaline earth metal salts of weak organic acids selected from acetic acid, oxalic acid, citric acid, tartaric acid, and propionic acid.

6. 1. A composition comprising: a) acephate, b) an electrolyte; and c) one or more active ingredients other than acephate; The composition of claim 1 comprising:

7. 7. The composition of claim 6, wherein the one or more active ingredients are selected from an organophosphorus compound, a chloronicotinyl compound, a diamide insecticide, a benzoylphenylurea chitin synthesis inhibitor, or a pyrethroid compound.

8. 8. The composition of claim 7, wherein the composition comprises acetamiprid, imidacloprid, thiacloprid, thiamethoxam, cypermethrin, fenvalerate, permethrin, alpha-cypermethrin, beta-cypermethrin, zeta-cypermethrin, deltamethrin, cyfluthrin, bifenthrin, lambda-cyhalothrin, bioresmethrin, chlorantraniliprole, cyantraniliprole, cyclaniliprole, tetrachlorantraniliprole, lufenuron, novaluron, or mixtures thereof.

9. 10. A process for preparing the composition of claim 1, wherein the composition comprises acephate, and the decomposition of the acephate in the composition is controlled to less than 5% of the weight of the acephate in the composition; Step 1: preparing a mixture of water and electrolyte by mixing the water and electrolyte in a ratio of 1:1 to 1:20; Step 2: Preparing a blend of acephate, remaining electrolytes, if present, and other excipients; Step 3: preparing a mixture of the blend of step 2 with the mixture of step 1; Step 4: Formulating into a suitable form using a suitable device.

10. 10. A process for preparing the composition of claim 1, wherein the composition comprises acephate, and the decomposition of the acephate in the composition is controlled to less than 5% of the weight of the acephate in the composition; Step 1: preparing a mixture of water and electrolyte by mixing the water and electrolyte in a ratio of 1:1 to 1:20; Step 2: Preparing a blend of acephate, remaining electrolytes, if present, and one or more active ingredients other than acephate; Step 3: preparing a mixture of the blend of step 2 with the mixture of step 1; Step 4: Formulating into a suitable form.

11. 11. The process of claim 10, wherein the one or more active ingredients are selected from an organophosphorus compound, a chloronicotinyl compound, a diamide insecticide, a benzoylphenylurea chitin synthesis inhibitor, or a pyrethroid compound.

12. 13. A method for controlling insects comprising applying an effective amount of the composition of claim 1 to the area to be treated.

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