Anthranilamide Compositions

Abstract

The present disclosure provides a pesticide composition comprising a pesticidal active ingredient, an enhancer comprising a salt of a dialkyl sulfosuccinate, a salt of lauryl sulfate, a salt of lauryl benzene sulfonate, a fatty alcohol derivative, a salt of an alkyl naphthyl sulfonate, or a salt of an alkyl naphthyl sulfate, or a mixture thereof, and a dispersant comprising a polycarboxylate, a phenolsulfonic acid condensate, a polyoxypropylene-polyoxyethylene block copolymer, or a naphthalenesulfonic acid condensate, or a mixture thereof. The present invention also provides a method for controlling pests in crops, comprising the step of applying an agriculturally effective amount of the composition to the crop or its environment in need thereof.

Description

[Technical Field]

[0001] CROSS-REFERENCE TO RELATED APPLICATIONS This application claims priority to U.S. Provisional Patent Application No. 62 / 906,801, filed September 27, 2019.

[0002] The present disclosure relates to novel compositions comprising anthranilamides and methods comprising applying said compositions to control pests. [Background technology]

[0003] Anthranilamides (also known as anthranilic acid diamides) are an important synthetic class of insecticides that affect calcium homeostasis with high selectivity at insect ryanodine receptors over mammalian receptors. Chlorantraniliprole, in particular, is the most widely used insecticide of its class. It has high biological activity against pests belonging to the orders Lepidoptera and some Coleoptera, Diptera, and Isoptera, as well as very low toxicity to non-target arthropods. Chlorantraniliprole is active against chewing pests primarily by ingestion and secondarily by contact.

[0004] Commonly developed formulations of chlorantraniliprole include SC (supervised release), water dispersible granules (WDG), flowable concentrates (FS) for seed dressing, and granules (GR). These pesticide formulations are often applied by spraying. Manual application of the pesticide as an aqueous solution or suspension is labor-intensive and time-consuming. Current labor-saving techniques, such as ultra-low volume (ULV) spraying and aerial spraying, are limited by the requirement for higher technical skill and equipment costs and are therefore not always feasible for standard grower applications. ULV and aerial spraying can also be associated with wind drift issues, depending on the weather conditions at the time of spraying, which could potentially introduce the pesticide into the environment. Therefore, it is highly desirable to develop new pesticide formulations that are easy to apply by growers and farmers and demonstrate high levels of pest control efficacy with a reduced environmental impact. Summary of the Invention [Means for solving the problem]

[0005] The inventors of the present disclosure have discovered that when an anthranilamide as an active ingredient is formulated with a suitable combination of one or more dispersants and one or more enhancers, the formulation achieves the desired uniform dispersion effect without the use of equipment, thereby relieving farmers from time-consuming and labor-intensive manual spraying. Provided herein are novel compositions, e.g., in tablet form, that disperse uniformly when applied directly to, for example, rice paddies, and that provide more effective pest control at recommended dosages.

[0006] In one aspect, the present disclosure provides herein: (a) a pesticide active ingredient; (b) an enhancer, wherein the enhancer comprises a salt of a dialkyl sulfosuccinate, a salt of lauryl sulfate, a salt of lauryl benzene sulfonate, a fatty alcohol derivative, a salt of an alkyl naphthyl sulfonate, or a salt of an alkyl naphthyl sulfate, or a mixture thereof; (c) a dispersant, wherein the dispersant comprises a polycarboxylate, a phenolsulfonic acid condensate, a polyoxypropylene-polyoxyethylene block copolymer, or a naphthalenesulfonic acid condensate, or a mixture thereof; (d) binder and; (e) optionally a filler; The present invention provides a formulation comprising a composition comprising:

[0007] In one aspect, the present disclosure provides herein a composition comprising, by weight, based on the total weight of the composition: (a) about 0.1% to about 20% of a pesticide active ingredient; (b) about 0.1% to about 5% of at least one enhancer, wherein the enhancer comprises a salt of a dialkyl sulfosuccinate, a salt of lauryl sulfate, a salt of lauryl benzene sulfonate, a fatty alcohol derivative, a salt of an alkyl naphthyl sulfonate, or a salt of an alkyl naphthyl sulfate, or a mixture thereof; (c) from about 0.1% to about 10% of at least one dispersing agent, wherein the dispersing agent comprises a polycarboxylate, a phenolsulfonic acid condensate, a polyoxypropylene-polyoxyethylene block copolymer, or a naphthalenesulfonic acid condensate, or a mixture thereof; (d) about 0.1% to about 20% of at least one binder; (e) about 0.1% to about 50% of at least one filler; The present invention provides a formulation comprising a composition comprising:

[0008] In certain embodiments, the composition is in the form of a tablet.

[0009] In certain embodiments, the pesticidal active ingredient is a herbicide or insecticide. In certain embodiments, the pesticidal active ingredient is a diamide, a neonicotinoid, or a nereistoxin analog insecticide, or a mixture thereof. In certain embodiments, the pesticidal active ingredient is a diamide.

[0010] In certain embodiments, the composition further comprises, by weight, based on the total weight of the composition, component (f) from about 0.1% to about 40% of at least one acid and / or (g) from about 0.1% to about 40% of at least one alkali.

[0011] In certain embodiments, the enhancer comprises sodium dialkyl sulfosuccinate, sodium lauryl sulfate, sodium laurylbenzene sulfonate, fatty alcohol derivatives, sodium alkyl naphthyl sulfonate, dioctyl sodium sulfosuccinate, or sodium alkyl naphthyl sulfate, or mixtures thereof.

[0012] In one aspect, the present disclosure provides a composition comprising, by weight, based on the total weight of the composition: (a) about 0.1% to about 20% of a pesticidal active ingredient comprising one or more anthranilamides; (b) about 0.1% to about 5% of at least one enhancer, wherein the enhancer comprises a salt of a dialkyl sulfosuccinate, a salt of lauryl sulfate, a salt of lauryl benzene sulfonate, a fatty alcohol derivative, a salt of an alkyl naphthyl sulfonate, or a salt of an alkyl naphthyl sulfate, or a mixture thereof; (c) from about 0.1% to about 10% of at least one dispersing agent, wherein the dispersing agent comprises a polycarboxylate, a phenolsulfonic acid condensate, a polyoxypropylene-polyoxyethylene block copolymer, or a naphthalenesulfonic acid condensate, or a mixture thereof; (d) about 0.1% to about 20% of at least one binder; (e) about 0.1% to about 50% of at least one filler; A tablet composition comprising:

[0013] In certain embodiments, the pesticidal active ingredient is a herbicide or insecticide, hi certain embodiments, the pesticidal active ingredient is a diamide, neonicotinoid, or nereistoxin analogue insecticide, or a mixture thereof.

[0014] In certain embodiments, component (a) comprises chlorantraniliprole, cyantraniliprole, tetraniliprole, cyclaniliprole, cyhalodiamide, tetra-chlorantraniliprole, thiamethoxam, clothianidin, thiacloprid, monosultap, or bisultap, or a mixture thereof. In certain embodiments, component (a) comprises chlorantraniliprole.

[0015] In certain embodiments, component (a) is from about 1% to about 10%, from about 1% to about 8%, from about 1% to about 7%, from about 1% to about 6%, from about 1% to about 5.5%, about 1%, about 2.5%, or about 5% by weight of the composition.

[0016] In certain embodiments, the enhancer comprises sodium dialkyl sulfosuccinate, sodium lauryl sulfate, sodium laurylbenzenesulfonate, a fatty alcohol derivative, sodium alkyl naphthyl sulfonate, dioctyl sodium sulfosuccinate, or sodium alkyl naphthyl sulfate, or a mixture thereof. In certain embodiments, the enhancer comprises a salt of dioctyl sulfosuccinate.

[0017] In certain embodiments, component (b) comprises Geropon® SDS, Aerosol® OT-B, or Aerosol® OT-75, or a mixture thereof. In certain embodiments, component (b) is a substance selected from the group consisting of Geropon® SDS, Aerosol® OT-B, and Aerosol® OT-75. In certain embodiments, component (b) comprises Geropon SDS. In certain embodiments, component (b) is Geropon® SDS.

[0018] In certain embodiments, component (b) is from about 0.1% to about 4%, from about 0.1% to about 3%, from about 0.1% to about 2%, from about 0.2% to about 2%, from about 0.3% to about 2%, from about 0.3% to about 1.8%, from about 0.3% to about 1.5%, from about 0.3% to about 1.2%, from about 0.3% to about 1%, from about 0.5% to about 1%, from about 0.6% to about 1%, from about 0.7% to about 1%, or about 0.8% by weight of the composition.

[0019] In certain embodiments, component (c) is Tersperse® 2700, Atlox metasperse TM In certain embodiments, component (c) comprises Tersperse 2700, Atlox metasperse 550S, Geropon® Ultrasperse, Duramax® D-205, or Geropon® T / 36, or mixtures thereof. TM 550S, Geropon® Ultrasperse, Duramax® D-205, and Geropon® T / 36. In certain embodiments, component (c) comprises Tersperse® 2700. In certain embodiments, component (c) is Tersperse® 2700.

[0020] In certain embodiments, component (c) is about 0.5% to about 10%, about 0.5% to about 8%, about 0.5% to about 7%, about 0.5% to about 6%, about 0.5% to about 5%, about 0.8% to about 5%, about 1% to about 5%, about 1.2% to about 5%, about 1.5% to about 5%, about 1.7% to about 5%, about 2% to about 5%, about 2% to about 4.5%, about 2% to about 4%, about 2% to about 3.5%, about 2% to about 3%, about 2.2% to about 2.8%, about 2.4% to about 2.6%, or about 2.5% by weight of the composition.

[0021] In certain embodiments, the composition further comprises component (f) from about 0.1% to about 40% of at least one acid and / or (g) from about 0.1% to about 40% of at least one alkali.

[0022] In certain embodiments, component (f) comprises at least one substance selected from the group consisting of citric acid, malonate, adipic acid, maleic acid, and D,L-tartaric acid. In certain embodiments, component (f) comprises D,L-tartaric acid. In certain embodiments, component (f) is D,L-tartaric acid.

[0023] In certain embodiments, component (f) is from about 0.5% to about 25%, from about 1% to about 25%, from about 5% to about 25%, from about 10% to about 25%, from about 15% to about 25%, from about 16% to about 25%, from about 17% to about 25%, from about 18% to about 25%, from about 19% to about 25%, from about 20% to about 25%, from about 20% to about 24%, from about 20% to about 23%, from about 20% to about 22%, or about 21% by weight of the composition.

[0024] In certain embodiments, component (g) comprises at least one substance selected from the group consisting of bicarbonate and carbonate. In certain embodiments, component (g) comprises at least one substance selected from the group consisting of sodium bicarbonate, potassium bicarbonate, sodium carbonate, and potassium carbonate. In certain embodiments, component (g) comprises a mixture of sodium bicarbonate and sodium carbonate. In certain embodiments, component (g) is a mixture of sodium bicarbonate and sodium carbonate.

[0025] In certain embodiments, the ratio of sodium bicarbonate to sodium carbonate, or potassium bicarbonate to potassium carbonate, by weight is about 1:10-10:1, about 1:5-10:1, about 1:3-10:1, about 1:2-10:1, about 1:1-10:1, about 2:1-10:1, about 3:1-10:1, about 3:1-9:1, about 3:1-8:1, about 3:1-7:1, about 3:1-6:1, about 3:1-5:1, about 3:1-4:1, about 3.5:1-4:1, or about 3.7:1.

[0026] In certain embodiments, component (g) comprises a mixture of sodium bicarbonate and sodium carbonate, wherein the sodium bicarbonate comprises from about 0.5% to about 40%, from about 1% to about 40%, from about 5% to about 40%, from about 10% to about 40%, from about 15% to about 40%, from about 20% to about 40%, from about 25% to about 40%, from about 25% to about 35%, from about 27%, or from about 30% to about 35% by weight of the composition. % to about 33%, or about 30%, and sodium carbonate is about 1% to about 40%, about 1% to about 30%, about 1% to about 20%, about 2% to about 20%, about 3% to about 20%, about 3% to about 18%, about 3% to about 15%, about 3% to about 12%, about 3% to about 10%, about 5% to about 10%, about 6% to about 10%, about 7% to about 10%, or about 8% by weight of the composition.

[0027] In certain embodiments, component (g) comprises a mixture of potassium bicarbonate and potassium carbonate, wherein the potassium bicarbonate comprises from about 0.5% to about 40%, from about 1% to about 40%, from about 5% to about 40%, from about 10% to about 40%, from about 15% to about 40%, from about 20% to about 40%, from about 25% to about 40%, from about 25% to about 35%, or from about 27% by weight of the composition. and potassium carbonate is about 1% to about 40%, about 1% to about 30%, about 1% to about 20%, about 2% to about 20%, about 3% to about 20%, about 3% to about 18%, about 3% to about 15%, about 3% to about 12%, about 3% to about 10%, about 5% to about 10%, about 6% to about 10%, about 7% to about 10%, or about 8% by weight of the composition.

[0028] In certain embodiments, component (g) is from about 0.5% to about 40%, from about 1% to about 40%, from about 5% to about 40%, from about 10% to about 40%, from about 15% to about 40%, from about 20% to about 40%, from about 25% to about 40%, from about 30% to about 40%, from about 35% to about 40%, or about 38% of the composition by weight.

[0029] In certain embodiments, component (d) comprises at least one substance selected from the group consisting of polyethylene glycol (PEG), maltose, trehalose, sorbitol, maltitol, polyvinylpyrrolidone, dibasic calcium phosphate, sucrose, glucose, corn (maize) starch, modified cellulose, alginic acid, sodium carboxymethylcellulose, and copovidone. In certain embodiments, component (d) comprises PEG. In certain embodiments, component (d) is PEG, in certain embodiments, PEG is selected from the group consisting of PEG2000, PEG4000, PEG6000, PEG8000, and PEG10000. In certain embodiments, PEG is PEG6000.

[0030] In certain embodiments, component (d) is about 1% to about 15%, about 1% to about 10%, about 1% to about 8%, about 1% to about 7%, about 1% to about 6%, about 1% to about 5.5%, about 2% to about 5.5%, about 3% to about 5.5%, about 3%, or about 5.5% of the composition by weight.

[0031] In certain embodiments, component (e) comprises at least one substance selected from the group consisting of lactose, lactose monohydrate, mannitol, sucrose, talcum, maltodextrin, dextrin, maltitol, sorbitol, xylitol, powdered cellulose, cellulose gum, microcrystalline cellulose, starch, or calcium phosphate. In certain embodiments, component (e) comprises talcum, maltodextrin, or a mixture thereof. In certain embodiments, component (e) comprises a mixture of talcum and maltodextrin. In certain embodiments, component (e) comprises from about 1% to about 15%, from about 1% to about 10%, from about 1% to about 8%, from about 2% to about 8%, from about 3% to about 8%, from about 4% to about 8%, from about 5% to about 8%, from about 6% to about 8%, or about 6% talcum by weight of the composition and from about 1% to about 40%, from about 1% to about 30%, from about 5% to about 30%, from about 8% to about 30%, from about 10% to about 30%, from about 15% to about 30%, from about 18% to about 30%, from about 18% to about 27%, or from about 20% to about 27% maltodextrin by weight of the composition.

[0032] In certain embodiments, component (e) is from about 0.5% to about 50%, from about 1% to about 50%, from about 5% to about 50%, from about 10% to about 50%, from about 15% to about 50%, from about 20% to about 50%, from about 20% to about 45%, from about 20% to about 40%, from about 20% to about 35%, from about 25% to about 35%, from about 26% to about 33%, about 26%, about 29%, or about 33% by weight of the composition.

[0033] In certain embodiments, the composition further comprises from about 0.1% to about 5% by weight of the composition of at least one lubricant component (h).

[0034] In certain embodiments, component (h) comprises at least one substance selected from the group consisting of white carbon, talcum powder, magnesium stearate, calcium stearate, sodium stearate, zinc stearate, stearic acid, metal stearates, sodium stearyl fumarate, fatty acids, fatty alcohols, fatty acid esters, glyceryl behenate, canola oil, mineral oil, vegetable oil, glyceryl palmitostearate, hydrogenated vegetable oil, hydrogenated vegetable oil, magnesium oxide, poloxamer, paraffin, leucine, propylene glycol fatty acid esters, polyvinyl alcohol sodium benzoate, sodium lauryl sulfate, sodium stearyl fumarate, polyethylene glycol, polypropylene glycol, and polyalkylene glycol. In certain embodiments, component (h) comprises a stearate. In certain embodiments, component (h) is a stearate. In certain embodiments, component (h) comprises magnesium stearate. In certain embodiments, component (h) is magnesium stearate.

[0035] In certain embodiments, component (h) is about 0.1% to about 4.5%, about 0.1% to about 4.0%, about 0.1% to about 3.5%, about 0.1% to about 3.0%, about 0.1% to about 2.5%, about 0.1% to about 2.0%, about 0.1% to about 1.5%, about 0.1% to about 1.0%, about 0.5% to about 1.0%, about 0.5% to about 0.7%, about 0.5%, or about 0.7% by weight of the composition.

[0036] In certain embodiments, the composition further comprises from about 0.01% to about 5% by weight of the composition of at least one bitter component (i).

[0037] In certain embodiments, component (i) comprises at least one substance selected from the group consisting of benzodiazepine, denatonium, sucrose octaacetate, quercetin, brucine, and quassin, hi certain embodiments, component (i) comprises denatonium benzoate.

[0038] In certain embodiments, component (i) is from about 0.01% to about 4.5%, from about 0.01% to about 4.0%, from about 0.01% to about 3.5%, from about 0.01% to about 3.0%, from about 0.01% to about 2.5%, from about 0.01% to about 2.0%, from about 0.01% to about 1.5%, from about 0.01% to about 1.0%, from about 0.01% to about 0.5%, from about 0.01% to about 0.4%, from about 0.01% to about 0.3%, from about 0.01% to about 0.2%, from about 0.01% to about 0.1%, from about 0.01% to about 0.05%, about 0.05%, or about 0.1% of the composition by weight.

[0039] In certain embodiments, the composition further comprises from about 0.1% to about 1.5% by weight of the composition of at least one dispersant, component (j).

[0040] In certain embodiments, component (j) comprises at least one material selected from the group consisting of disperse 131, polyfon H, disperse 132, and disperse 140. In certain embodiments, component (i) comprises polyfon H.

[0041] In certain embodiments, component (j) is from about 0.1% to about 4.0%, from about 0.1% to about 3.5%, from about 0.1% to about 3.0%, from about 0.1% to about 2.5%, from about 0.1% to about 2.0%, from about 0.1% to about 1.5%, from about 0.1% to about 1.0%, from about 0.1% to about 0.5%, from about 0.1% to about 0.4%, from about 0.1% to about 0.3%, from about 0.1% to about 0.2%, from about 0.1% to about 0.1%, from about 0.1% to about 0.5%, about 0.5%, or about 1.0% by weight of the composition.

[0042] In one aspect, the present disclosure provides herein a composition comprising, by weight, based on the total weight of the composition: (a) about 0.1% to about 20% chlorantraniliprole, or cyantraniliprole, or a mixture thereof; (b) about 0.1% to about 5% Geropon® SDS; (c) about 0.1% to about 10% Tersperse® 2700; (d) about 0.1% to about 20% PEG-6000; (e) a mixture comprising about 0.1% to 50% talcum and maltodextrin; (f) about 0.1% to 40% D,L-tartaric acid; (g) a mixture containing about 0.1% to about 40% sodium bicarbonate and sodium carbonate; A tablet composition comprising:

[0043] In one aspect, the present disclosure provides herein a composition comprising, by weight, based on the total weight of the composition: (a) about 1% to 5.5% chlorantraniliprole, or cyantraniliprole, or a mixture thereof; (b) about 0.5% to 1.8% Geropon® SDS; (c) about 1.5% to 3.5% Tersperse® 2700; (d) with about 1% to 8% PEG-6000; (e) about 3% to 8% talcum and about 20 to 30% maltodextrin; (f) about 15% to 25% D,L-tartaric acid; (g) about 20% to 40% sodium bicarbonate and about 5% to 10% sodium carbonate; A tablet composition comprising:

[0044] In certain embodiments, the composition further comprises (h) about 0.5% to about 0.7% magnesium stearate. In certain embodiments, the composition further comprises (i) about 0.04% to about 0.06% denatonium benzoate. In certain embodiments, the composition further comprises (i) about 0.06% to about 0.12% denatonium benzoate. In certain embodiments, the composition further comprises about 0.1% to about 1.5% by weight of the composition of at least one dispersant component (j).

[0045] In one aspect, the present disclosure provides herein a composition comprising, by weight, based on the total weight of the composition: (a) about 1.05% chlorantraniliprole; (b) about 0.8% Geropon® SDS; (c) about 2.5% Tersperse® 2700; (d) with about 3.0% PEG-6000; (e) about 6.0% talcum and about 27.1% maltodextrin; (f) about 21% D,L-tartaric acid; (g) about 30% sodium bicarbonate and about 8% sodium carbonate A tablet composition comprising:

[0046] In certain embodiments, the composition further comprises (h) about 0.5% magnesium stearate. In certain embodiments, the composition further comprises (i) about 0.05% denatonium benzoate. In some embodiments, the composition further comprises (i) about 0.1% denatonium benzoate. In certain embodiments, the composition further comprises component (j) of polyfon H at about 1.0%.

[0047] In one aspect, the present disclosure provides herein a composition comprising, by weight, based on the total weight of the composition: (a) with approximately 2.6% chlorantraniliprole; (b) about 0.8% Geropon® SDS; (c) about 2.5% Tersperse® 2700; (d) with approximately 5.5% PEG-6000; (e) about 6.0% talcum and about 22.85% maltodextrin; (f) about 21% D,L-tartaric acid; (g) about 30% sodium bicarbonate and about 8% sodium carbonate A tablet composition comprising:

[0048] In certain embodiments, the composition further comprises (h) about 0.7% magnesium stearate. In certain embodiments, the composition further comprises (i) about 0.05% denatonium benzoate. In certain embodiments, the composition further comprises (i) about 0.1% denatonium benzoate. In certain embodiments, the composition further comprises about 1.0% of component (j) of polyfon H.

[0049] In one aspect, the present disclosure provides herein a composition comprising, by weight, based on the total weight of the composition: (a) with approximately 5.1% chlorantraniliprole; (b) about 0.8% Geropon® SDS; (c) about 2.5% Tersperse® 2700; (d) with approximately 5.5% PEG-6000; (e) about 6.0% talcum and about 20.35% maltodextrin; (f) about 21% D,L-tartaric acid; (g) about 30% sodium bicarbonate and about 8% sodium carbonate A tablet composition comprising:

[0050] In certain embodiments, the composition further comprises (h) about 0.7% magnesium stearate. In certain embodiments, the composition further comprises (i) about 0.05% denatonium benzoate. In certain embodiments, the composition further comprises (i) about 0.1% denatonium benzoate. In certain embodiments, the composition further comprises about 1.0% of component (j) of polyfon H.

[0051] In another aspect, the present disclosure provides herein a method for controlling pests in crops, comprising applying an agriculturally effective amount of the formulation or composition provided herein to the crop or its environment in need thereof.

[0052] In certain embodiments, the formulation or composition is applied at a rate of 10 grams active ingredient per hectare (gai / ha) to about 10,000 gai / ha, about 10 to about 5,000 gai / ha, about 10 to about 1,000 gai / ha, about 10 to about 500 gai / ha, about 10 to about 200 gai / ha, about 10 to about 100 gai / ha, about 10 to about 90 gai / ha, about 10 to about 80 gai / ha, about 10 to about 70 gai / ha, about 10 to about 60 gai / ha, about 10 to about 50 gai / ha, about 20 to about 50 gai / ha, about 30 to about 50 gai / ha, or about 40 gai / ha.

[0053] In certain embodiments, a single tablet of the present disclosure comprises about 0.0004 g to about 1 g, about 0.001 g to about 0.5 g, about 0.002 g to about 0.4 g, about 0.003 g to about 0.3 g, about 0.004 g to about 0.2 g, about 0.005 g to about 0.2 g, about 0.01 g to about 0.3 g, about 0.05 g to about 0.3 g, about 0.07 g to about 0.3 g, about 0.1 g to about 0.3 g, about 0.1 g to about 0.25 g, about 0.1 g to about 0.2 g, about 0.0034 g, about 0.0775 g, or about 0.15 g of component (a).

[0054] In certain embodiments, the crop is selected from the group consisting of rice, vegetables, and corn. In certain embodiments, the crop is rice. In certain embodiments, the crop is rice and the formulation or composition is applied to paddy fields. [Brief explanation of the drawings]

[0055] [Figure 1] The sampling locations where the active ingredient was collected to determine the distribution profile of the tablets are indicated. [Figure 2] The content of the active ingredient at the sampling location is shown. [Figure 3] The concentration of chlorantraniliprole absorbed in rice stems 3 and 20 days after pesticide application is shown. [Figure 4] 1 shows the concentration of chlorantraniliprole absorbed in rice stems collected at different distances from the application site. DETAILED DESCRIPTION OF THE INVENTION

[0056] As used herein, the terms "comprises," "comprising," "includes," "including," "has," "having," or any other variation thereof, are intended to cover a non-exclusive inclusion. For example, a composition, mixture, process, method, article, or device that includes a list of elements is not necessarily limited to only those elements and may include other elements not expressly listed or inherent in such composition, mixture, process, method, article, or device. Furthermore, unless expressly stated to the contrary, "or" means an inclusive or, not an exclusive or. For example, condition A or B can be satisfied by any one of the following: A is true (exists) and B is false (or does not exist), A is false (or does not exist) and B is true (or exists), and both A and B are true (or exist).

[0057] Additionally, the use of "a" or "an" is employed to describe elements and components of the invention. This is done merely for convenience and to give a general sense of the invention. This description should be read to include one or at least one, and the singular also includes the plural unless expressly stated otherwise.

[0058] When a range of values ​​is listed, the entire range should be considered to include the end values ​​indicated. Also, any numerical range listed herein should be understood to include all values ​​from the lower limit to the upper limit. For example, if a weight ratio range is presented as 1:50, values ​​such as 2:40, 10:30, or 1:3 are intended to be expressly recited herein. These are merely examples of what is specifically intended, and all possible combinations of numerical values ​​between and including the lowest and highest values ​​listed should be considered to be expressly stated in this application.

[0059] As used herein, the term "about" means plus or minus 10% of the value.

[0060] In one aspect, the disclosure provides herein a formulation comprising a composition comprising: a pesticidal active ingredient; an enhancer (wherein the enhancer comprises a salt of a dialkyl sulfosuccinate, a salt of lauryl sulfate, a salt of lauryl benzene sulfonate, a fatty alcohol derivative, a salt of an alkyl naphthyl sulfonate, or a salt of an alkyl naphthyl sulfate, or a mixture thereof); a dispersant (wherein the dispersant comprises a polycarboxylate, a phenolsulfonic acid condensate, a polyoxypropylene-polyoxyethylene block copolymer, or a naphthalenesulfonic acid condensate, or a mixture thereof); a binder; and optionally a filler.

[0061] In another aspect, the disclosure provides herein a formulation comprising a composition comprising, by weight, based on the total weight of the composition: from about 0.1% to about 20% of a pesticidal active ingredient; from about 0.1% to about 5% of at least one enhancer (wherein the enhancer comprises a salt of a dialkyl sulfosuccinate, a salt of lauryl sulfate, a salt of lauryl benzene sulfonate, a fatty alcohol derivative, a salt of an alkyl naphthyl sulfonate, or a salt of an alkyl naphthyl sulfate, or a mixture thereof); from about 0.1% to about 10% of at least one dispersant (wherein the dispersant comprises a polycarboxylate, a phenolsulfonic acid condensate, a polyoxypropylene-polyoxyethylene block copolymer, or a naphthalenesulfonic acid condensate, or a mixture thereof); from about 0.1% to about 20% of at least one binder; and from about 0.1% to about 50% of at least one filler.

[0062] In another aspect, the disclosure provides herein a tablet formulation comprising, by weight, based on the total weight of the composition: about 0.1% to about 20% of a pesticidal active ingredient; about 0.1% to about 5% of at least one enhancer (wherein the enhancer comprises a salt of a dialkyl sulfosuccinate, a salt of lauryl sulfate, a salt of lauryl benzene sulfonate, a fatty alcohol derivative, a salt of an alkyl naphthyl sulfonate, or a salt of an alkyl naphthyl sulfate, or a mixture thereof); about 0.1% to about 10% of at least one dispersant (wherein the dispersant comprises a polycarboxylate, a phenolsulfonic acid condensate, a polyoxypropylene-polyoxyethylene block copolymer, or a naphthalenesulfonic acid condensate, or a mixture thereof); about 0.1% to about 20% of at least one binder; and about 0.1% to about 50% of at least one filler.

[0063] The use of drones or unmanned aerial vehicles (UAVs) in agricultural applications, such as for treating fields with chemical products, is expanding rapidly.

[0064] In one aspect of the present invention, the compositions and formulations disclosed herein are useful for delivery by drone or unmanned aerial vehicle (UAV).

[0065] The term "pesticidally active ingredient" as used herein includes those selected from the following classes: herbicides, fungicides, bactericides, insecticides, nematicides, acaricides, and growth regulators, including mixtures thereof.

[0066] Insecticides useful in the present invention include abamectin, acephate, acequinocyl, acetamipyrid, acrinathrin, acinonapyr, afidopyropen ([(3S,4R,4aR,6S,6aS,12R,12aS,12bS)-3-[(cyclopropylcarbonyl)oxy]-1,3,4,4a,5,6,6a,12,12a,12b-decahydro-6,12-dihydroxy-4,6a,12b-trimethyl-11-oxo-9-(3-pyridinyl)- 2H,11H-Naphtho[2,1-b]pyrano[3,4-e]pyran-4-yl]methylcyclopropanecarboxylate), amidoflumet, amitraz, avermectin, azadirachtin, azinphos-methyl, benfuracarb, bensultap, benzpyrimoxan, bifenthrin, kappa-bifenthrin, bifenazate, bistrifluron, borate, brofuranilide, buprofezin, cadusafos, carbaryl, carbofuran, cartap , Carsol, chlorantraniliprole, chlorfenapyr, chlorfluazuron, chlorprallethrin, chlorpyrifos, chlorpyrifos-e, chlorpyrifos-methyl, chromafenozide, clofentezine, chlorprallethrin, clothianidin, cyantraniliprole, (3-bromo-1-(3-chloro-2-pyridinyl)-N-[4-cyano-2-methyl-6-[(methylamino)carbonyl]phenyl]-1H-pyrazole-5-carboxamide boxamide), cyclaniliprole (3-bromo-N-[2-bromo-4-chloro-6-[[(1-cyclopropylethyl)amino]carbonyl]phenyl]-1-(3-chloro-2-pyridinyl)-1H-pyrazole-5-carboxamide), cycloprothrin, cycloxapride ((5S,8R)-1-[(6-chloro-3-pyridinyl)methyl]-2,3,5,6,7,8-hexahydro-9-nitro-5,8-epoxy-1H-imidazo[1,2-a]azepine), cyenopyrafen, cyflumetofen, cyfluthrin, beta-cyfluthrin, cyhalodiamide, cyhalothrin, gamma-cyhalothrin, lambda-cyhalothrin, cypermethrin, alpha-cypermethrin, zeta-cypermethrin, cyromazine, deltamethrin, diafenthiuron, diazinon, dichloromethiaz, dieldrin, diflubenzuron, dimefluthrin, dimehypo, dimethoate, dipropylidaz, dinotefuran, diofenolan, emamectin, emamectin benzoate, endosulfan, esfenvalerate, ethiprole, etofenprox, epsilon-metofluthrin, etoxazole, fenbutatin oxide, fenitrothion, fenothiocarb, fenoxycarb, fenpropathrin, fenvalerate, fipronil, flometoquin (2-ethyl-3,7-dimethyl-6-[4-(trifluoromethoxy)phenoxy]-4-quinolinylmethyl carbonate), flonicamid, fluazaindolizine, flubendiamide, flucytrin methyl methacrylate, flufenerim, flufenoxuron, flufenoxystrobin ((αE)-2-[[2-chloro-4-(trifluoromethyl)phenoxy]methyl]-α-(methoxymethylene)benzeneacetate), fluensulfone (5-chloro-2-[(3,4,4-trifluoro-3-buten-1-yl)sulfonyl]thiazole), fluhexafon, fluopyram, flupiprole (1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-5-[(2-methyl-2-propen-1-yl)acetate]). amino]-4-[(trifluoromethyl)sulfinyl]-1H-pyrazole-3-carbonitrile), flupyradifurone (4-[[(6-chloro-3-pyridinyl)methyl](2,2-difluoroethyl)amino]-2(5H)-furanone), flupirimine, fluvalinate, taufluvalinate, fluxametamide, fonofos, formetanate, fosthiazate, gamma-cyhalothrin, halofenozide, heptafluthrin ([2,3,5,6-tetrafluoro-4-(methoxymethyl)phenyl]methyl 2,2-dimethyl-3-[(1Z)-3,3,3-trifluoro-1-propen-1-yl]cyclopropanecarboxylate), hexaflumuron, hexythiazox, hydromethylnon, imidacloprid, indoxacarb, insecticidal soap, isofenphos, isocycloceram, kappa-tefluthrin, lambda-cyhalothrin, lufenuron, malathion, meperfluthrin ([2,3,5,6-tetrafluoro-4-(methoxymethyl)phenyl]methyl(1R,3S)-3-( 2,2-Dichloroethenyl)-2,2-dimethylcyclopropanecarboxylate), metaflumizone, metaldehyde, methamidophos, methidathion, methiocarb, methomyl, methoprene, methoxychlor, metofluthrin, methoxyfenozide, epsilon-metofluthrin, epsilon-monfluorothrin, monocrotophos, monofluorothrin ([2,3,5,6-tetrafluoro-4-(methoxymethyl)phenyl]methyl 3-(2-cyano-1-propen-1-yl)-2,2-dimethylcyclopropanecarboxylate), nicotine, nitenpyram, nithiazine, novaluron, noviflumuron, oxamyl, oxazosulfil, parathion, parathion-methyl, permethrin, phorate, phosalone, phosmet, phosphamidon, pirimicarb, profenofos, profluthrin, propargite, protrifenbutr, piflub amide (1,3,5-trimethyl-N-(2-methyl-1-oxopropyl)-N-[3-(2-methylpropyl)-4-[2,2,2-trifluoro-1-methoxy-1-(trifluoromethyl)ethyl]phenyl]-1H-pyrazole-4-carboxamide), pymetrozine, pyrafluprole, pyrethrins, pyridaben, pyridalyl, pyrifluquinazone, pyriminostrobin ((αE)-2-[[[2-[(2,4-dichlorophenyl)amino]-6-(trifluoromethyl)-4-pyrimidinyl]oxy]methyl]-α-(methoxymethylene)benzeneacetate), pyriprole, pyriproxyfen, rotenone, ryanodine, silafluofen, spinetoram, spinosad, spirodiclofen, spiromesifen, spiropydione, spirotetramat, sulprofos, sulfoxaflor (N-[methyloxide[1-[6-(trifluoromethyl)-3-pyridinyl]ethyl]-λ4-sulfanylidene]cyanamide), tebufenozide, tebufenpyrad, teflubenzuron, tefluthrin, kappa-tefluthrin, terbufos, tetrachlorantraniliprole, tetrachlorvinphos, tetramethrin, tetramethylfluthrin ([2,3,5,6-tetrafluoro-4-(methoxymethyl)phenyl]methyl Insecticides such as 2,2,3,3-tetramethylcyclopropanecarboxylate, tetraniliprole, thiacloprid, thiamethoxam, thiodicarb, thiosultap-sodium, thioxazafen (3-phenyl-5-(2-thienyl)-1,2,4-oxadiazole), tolfenpyrad, tralomethrin, triazamate, trichlorfon, triflumezopyrim (2,4-dioxo-1-(5-pyrimidinylmethyl)-3-[3-(trifluoromethyl)phenyl]-2H-pyrido[1,2-a]pyrimidinium inner salt), triflumuron, cyclopyrazoflor, zeta-cypermethrin, Bacillus thuringiensis delta-endotoxin, entomopathogenic bacteria, entomopathogenic viruses, or entomopathogenic fungi.

[0067] Herbicides useful in the present invention include (b1) photosystem II inhibitors, (b2) acetohydroxyacid synthase (AHAS) inhibitors, (b3) acetyl-CoA carboxylase (ACCase) inhibitors, (b4) auxin mimetics, (b5) 5-enolpyruvylshikimate-3-phosphate (EPSP) synthase inhibitors, (b6) photosystem I electron diverters, (b7) protoporphyrinogen oxidase (PPO) inhibitors, (b8) glutamine synthetase (GS) inhibitors, (b9) very long chain fatty acid (VLCFA) elongase inhibitors, (b10) auxin transport inhibitors, (b11) phytoene desaturase (PDS) inhibitors, (b12) 4-hydroxybenzoates (4-hydroxybenzoates), and (b13) hydroxybenzoates. (b13) homogentisic acid solenesyltransferase (HST) inhibitors, (b14) cellulose biosynthesis inhibitors, (b15) mitotic disruptors, organic arsenic compounds, other herbicides such as asulam, bromobutide, cinmethylin, cumyluron, dazomet, difenzoquat, dymron, etobenzanide, flurenol, fosamine, fosamine ammonium, hydantocidin, metam, methyldymron, oleic acid, oxaziclomefone, pelargonic acid, and pyributicarb, and (b16) herbicide safeners; and herbicides selected from salts of the compounds (b1) to (b16).

[0068] "Photosystem II inhibitors (b1)" are compounds that bind to the D1 protein in the QB-binding niche, thus blocking electron transport from QA to QB in the chloroplast thylakoid membrane. Electrons blocked from passing through photosystem II are transferred through a series of reactions to form toxic compounds that disrupt the cell membrane, causing chloroplast swelling, membrane leakage, and ultimately cell destruction. The QB-binding niche has three distinct binding sites: site A binds triazines such as atrazine, triazinones such as hexazinone, and uracils such as bromacil; site B binds phenylureas such as diuron; and site C binds benzothiadiazoles such as bentazone, nitriles such as bromoxynil, and phenylpyridazines such as pyridate. Examples of photosystem II inhibitors include ametryn, amicarbazone, atrazine, bentazon, bromacil, bromofenoxime, bromoxynil, chlorbromuron, chloridazon, chlorotoluron, chloroxuron, cumyluron, cyanazine, dymron, desmedipham, desmetrin, dimefuron, dimethamethrin, diuron, ethidimuron, fenuron, fluometuron, hexazinone, ioxynil, and isoproturon. Examples of compounds that may be used include benzophenone, isouron, lenacil, linuron, metamitron, methabenzthiazuron, metobromuron, methoxuron, metribuzin, monolinuron, nebron, pentanochlor, phenmedipham, prometon, prometryn, propanil, propazine, pyridafol, pyridate, siduron, simazine, simetryn, tebuthiuron, terbacil, terbumeton, terbuthylazine, terbutryn, and trietazine.

[0069] "AHAS inhibitors (b2)" are compounds that inhibit acetohydroxyacid synthase (AHAS), also known as acetolactate synthase (ALS), thereby killing plants by preventing the production of branched-chain aliphatic amino acids such as valine, leucine, and isoleucine, which are required for protein synthesis and cell growth.Examples of AHAS inhibitors include amidosulfuron, azimsulfuron, bensulfuron methyl, bispyribac sodium, cloransulam methyl, chlorimuron ethyl, chlorsulfuron, cinosulfuron, cyclosulfamuron, diclosulam, ethametsulfuron methyl, ethoxysulfuron, flazasulfuron, florasulam, flucarbazone sodium, flumetsulam, flupyrsulfuron methyl, flupyrsulfuron sodium, foramsulfuron, halosulfuron methyl, and imazametabunz methyl. , Imazamox, Imazapic, Imazapyr, Imazaquin, Imazethapyr, Imazosulfuron, Iodoflufuron-methyl (including sodium salt), Iofensulfuron (2-iodo-N-[[(4-methoxy-6-methyl-1,3,5-triazin-2-yl)amino]carbonyl]benzenesulfonamide), Mesosulfuron-methyl, Metazosulfuron (3-chloro-4-(5,6-dihydro-5-methyl-1,4,2-dioxazin-3-yl)-N-[[(4,6-dimethoxy-2-pyrimidinyl)amino] amino]carbonyl]-1-methyl-1H-pyrazole-5-sulfonamide), metosulam, metsulfuron methyl, nicosulfuron, oxasulfuron, penoxsulam, primisulfuron methyl, propoxycarbazone sodium, propyrisulfuron (2-chloro-N-[[(4,6-dimethoxy-2-pyrimidinyl)amino]carbonyl]-6-propylimidazo[1,2-b]pyridazine-3-sulfonamide), prosulfuron, pyrazosulfuron ethyl, pyribenzoxime, pyriftalid, pyrimidin These include novac-methyl, pyrithiobac-sodium, rimsulfuron, sulfometuron-methyl, sulfosulfuron, thiencarbazone, thifensulfuron-methyl, triafamone (N-[2-[(4,6-dimethoxy-1,3,5-triazin-2-yl)carbonyl]-6-fluorophenyl]-1,1-difluoro-N-methylmethanesulfonamide), triasulfuron, tribenuron-methyl, trifloxysulfuron (including the sodium salt), triflusulfuron-methyl, and tritosulfuron.

[0070] "ACCase inhibitors (b3)" are compounds that inhibit the acetyl-CoA carboxylase enzyme, which is involved in catalyzing the early steps of lipid and fatty acid synthesis in plants. Lipids are essential components of cell membranes; without them, new cells cannot be generated. Inhibition of acetyl-CoA carboxylase and the subsequent lack of lipid production results in a loss of cell membrane integrity, particularly in areas of active growth such as meristems. Ultimately, shoot and rhizome growth ceases, and shoot meristems and rhizome buds begin to die back. Examples of ACCase inhibitors include alloxydim, butroxydim, clethodim, clodinafop, cycloxydim, cyhalofop, diclofop, fenoxaprop, fluazifop, haloxyfop, pinoxaden, profoxydim, propaquizafop, quizalofop, sethoxydim, tepraloxydim and tralkoxydim, including resolved forms such as fenoxaprop P, fluazifop P, haloxyfop P and quizalofop P and ester forms such as clodinafop propargyl, cyhalofop butyl, diclofop methyl and fenoxaprop P ethyl.

[0071] Auxin is a plant hormone that regulates growth in many plant tissues. "Auxin mimetics (b4)" are compounds that mimic the plant growth hormone auxin, thus causing uncontrolled and unregulated growth and resulting in plant death in sensitive species. Examples of auxin mimetics include aminocyclopyrachlor (6-amino-5-chloro-2-cyclopropyl-4-pyrimidinecarboxylic acid) and its methyl and ethyl esters and its sodium and potassium salts, aminopyralid, benazolin ethyl, chloramben, clasifos, clomeprop, clopyralid, dicamba, 2,4D, 2,4DB, dichlorprop, fluroxypyr, haloxifen (4-amino-3-chloro-6-(4-chloro-2-fluoro-3- methyl 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)-2-pyridinecarboxylate), haloxifene methyl (methyl 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)-2-pyridinecarboxylate), MCPA, MCPB, mecoprop, picloram, quinclorac, quinmerac, 2,3,6TBA, triclopyr, and methyl 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)-5-fluoro-2-pyridinecarboxylate.

[0072] "EPSP synthase inhibitors (b5)" are compounds that inhibit the enzyme 5-enolpyruvylshikimate-3-phosphate synthase, which is involved in the synthesis of aromatic amino acids such as tyrosine, tryptophan, and phenylalanine. EPSP inhibitor herbicides are readily absorbed through plant foliage and translocated to the phloem to the growing point. Glyphosate is a relatively nonselective postemergence herbicide that belongs to this group. Glyphosate includes esters and salts such as ammonium, isopropylammonium, potassium, sodium (including sesquisodium), and trimesium (also named sulfosate).

[0073] "Photosystem I electron diverters (b6)" are compounds that accept electrons from photosystem I and, after several cycles, generate hydroxyl radicals. These radicals are highly reactive and readily destroy unsaturated lipids, such as membrane fatty acids and chlorophyll. This disrupts cell membrane integrity, resulting in "leaky" cells and organelles, leading to rapid leaf wilting and desiccation, and ultimately plant death. Examples of this second type of photosynthesis inhibitor include diquat and paraquat.

[0074] "PPO inhibitors (b7)" are compounds that inhibit protoporphyrinogen oxidase, rapidly leading to the formation of highly reactive compounds in plants that rupture cell membranes and cause the leakage of cell sap. Examples of PPO inhibitors include acifluorfen sodium, azafenidin, benzfendizone, bifenox, butafenacil, carfentrazone, carfentrazone ethyl, clomethoxyfen, cinidon ethyl, fluazolate, flufenpyr ethyl, flumiclorac pentyl, flumioxazin, fluoroglycofen ethyl, fluthiacet methyl, fomesafen, halosafen, lactofen, oxadiargyl, oxadiazon, oxyfluorfen, pentoxazone, profluazol, pyraclonil, pyraflufen ethyl, saflufenacil, sulfonyl benzoate, and sulfonyl benzoate. These include entrazone, thidiazimine, trifludimoxazine (dihydro-1,5-dimethyl-6-thioxo-3-[2,2,7-trifluoro-3,4-dihydro-3-oxo-4-(2-propyn-1-yl)-2H-1,4-benzoxazin-6-yl]-1,3,5-triazine-2,4(1H,3H)-dione), and thiafenacil (N-[2-[[2-chloro-5-[3,6-dihydro-3-methyl-2,6-dioxo-4-(trifluoromethyl)-1(2H)-pyrimidinyl]-4-fluorophenyl]thio]-1-oxopropyl]-β-methyl alanine).

[0075] "GS inhibitors (b8)" are compounds that inhibit the activity of the glutamine synthetase enzyme, which plants use to convert ammonia to glutamine. As a result, ammonia accumulates and glutamine levels decrease. Plant injury likely occurs due to the combined effects of ammonia toxicity and a shortage of amino acids needed for other metabolic processes. GS inhibitors include glufosinate and its esters and salts, such as glufosinate ammonium, as well as other phosphinothricin derivatives, glufosinate P ((2S)-2-amino-4-(hydroxymethylphosphinyl)butanoic acid), and biranafos.

[0076] "VLCFA elongase inhibitors (b9)" are herbicides with a wide variety of chemical structures that inhibit elongases, which are enzymes located in or near chloroplasts that are involved in the biosynthesis of VLCFAs. In plants, very long-chain fatty acids are the main components of hydrophobic polymers that prevent desiccation on leaf surfaces and provide stability to pollen grains. Such herbicides include acetochlor, alachlor, anilophos, butachlor, cafenstrole, dimethachlor, dimethenamid, diphenamid, fenoxasulfone (3-[[(2,5-dichloro-4-ethoxyphenyl)methyl]sulfonyl]-4,5-dihydro-5,5-dimethylisoxazole), fentrazamide, flufenacet, indanofan, mefenacet, metazachlor, metolachlor, naproanilide, napropamide, napropamide-M ((2R)-N,N-diethyl-2-(1-naphthalenyloxy)propanamide), petoxamide, piperophos, pretilachlor, propachlor, propisochlor, pyroxasulfone, and thenylchlor, including resolved forms such as S-metolachlor and chloroacetamide and oxyacetamide.

[0077] "Auxin transport inhibitors (b10)" are chemicals that inhibit auxin transport in plants, such as by binding to auxin carrier proteins. Examples of auxin transport inhibitors include diflufenzopyr and naptalam (also known as N-(1-naphthyl)phthalamic acid and 2-[(1-naphthalenylamino)carbonyl]benzoic acid).

[0078] "PDS inhibitors (b11)" are compounds that inhibit the carotenoid biosynthetic pathway at the phytoene desaturase step. Examples of PDS inhibitors include m-beflubutamid, beflubutamid, diflufenican, fluridone, flurochloridone, flurtamone norflurzon, and picolinafen.

[0079] "HPPD inhibitors (b12)" are chemical substances that inhibit the biosynthesis of 4-hydroxyphenyl-pyruvate dioxygenase. Examples of HPPD inhibitors include benzobicyclone, benzofenap, bicyclopyrone (4-hydroxy-3-[[2-[(2-methoxyethoxy)methyl]-6-(trifluoromethyl)-3-pyridinyl]carbonyl]bicyclo[3.2.1]oct-3-en-2-one), and fenquinotrione (2-[[8-chloro-3,4-dihydro-4-(4-methoxyphenyl)-3-oxo-2-quinoxalinyl]carbonyl]-1,3-cyclohexanedione). ), isoxaclorthol, isoxaflutole, mesotrione, pyrasulfotole, pyrazolinate, pyrazoxyfen, sulcotrione, tefuryltrione, tembotrione, tolpyralate (1-[[1-ethyl-4-[3-(2-methoxyethoxy)-2-methyl-4-(methylsulfonyl)benzoyl]-1H-pyrazol-5-yl]oxy]ethyl methyl carbonate), topramezone, 5-chloro-3-[(2-hydroxy-6-oxo-1- cyclohexen-1-yl)carbonyl]-1-(4-methoxyphenyl)-2(1H)-quinoxalinone, 4-(2,6-diethyl-4-methylphenyl)-5-hydroxy-2,6-dimethyl-3(2H)-pyridazinone, 4-(4-fluorophenyl)-6-[(2-hydroxy-6-oxo-1-cyclohexen-1-yl)carbonyl]-2-methyl-1,2,4-triazine-3,5(2H,4H)-dione, 5-[(2-hydroxy-6-oxo -1-cyclohexen-1-yl)carbonyl]-2-(3-methoxyphenyl)-3-(3-methoxypropyl)-4(3H)-pyrimidinone, 2-methyl-N-(4-methyl-1,2,5-oxadiazol-3-yl)-3-(methylsulfinyl)-4-(trifluoromethyl)benzamide and 2-methyl-3-(methylsulfonyl)-N-(1-methyl-1H-tetrazol-5-yl)-4-(trifluoromethyl)benzamide.

[0080] "HST inhibitors (b13)" disrupt the plant's ability to convert homogentisate to 2-methyl-6-solanyl-1,4-benzoquinone, thereby disrupting carotenoid biosynthesis. Examples of HST inhibitors include haloxydine, pyrichlor, 3-(2-chloro-3,6-difluorophenyl)-4-hydroxy-1-methyl-1,5-naphthyridin-2(1H)-one, 7-(3,5-dichloro-4-pyridinyl)-5-(2,2-difluoroethyl)-8-hydroxypyrido[2,3-b]pyrazin-6(5H)-one, and 4-(2,6-diethyl-4-methylphenyl)-5-hydroxy-2,6-dimethyl-3(2H)-pyridazinone.

[0081] HST inhibitors also include compounds of Formulas A and B: [ka] In the formula, R d1 is H, Cl or CF; R d2 is H, Cl or Br; R d3 is H or Cl; R d4 is H, Cl or CF; R d5 is CH3, CH2CH3 or CH2CHF2; R d6 is OH or -OC(=O)-i-Pr; R e1 is H, F, Cl, CH3 or CH2CH3; R e2 is H or CF; R e3 is H, CH3 or CH2CH3; R e4 is H, F or Br; R e5 is Cl, CH3, CF3, OCF3 or CH2CH3; R e6 is H, CH, CHCHF or C≡CH; R e7 is OH, —OC(═O)Et, —OC(═O)-i-Pr or —OC(═O)-t-Bu; A e8 is N or CH.

[0082] "Cellulose biosynthesis inhibitors (b14)" inhibit the biosynthesis of cellulose in certain plants. They are most effective when applied to young or rapidly growing plants pre-emergence or early post-emergence. Examples of cellulose biosynthesis inhibitors include chlorthiamid, dichlobenil, flupoxam, indaziflam (N2-[(1R,2S)-2,3-dihydro-2,6-dimethyl-1H-inden-1-yl]-6-(1-fluoroethyl)-1,3,5-triazine-2,4-diamine), isoxaben, and triaziflam.

[0083] "Other herbicides (b15)" includes herbicides that operate by a variety of different modes of action, such as mitotic disruptors (e.g., flamprop M methyl and flamprop M isopropyl), organic arsenic compounds (e.g., DSMA and MSMA), 7,8-dihydropteroate synthase inhibitors, chloroplast isoprenoid synthesis inhibitors, and cell wall biosynthesis inhibitors. Other herbicides include those herbicides that have an unknown mode of action, or that do not fall into the specific categories listed in (b1) through (b14), or that operate by a combination of the modes of action listed above. Examples of other herbicides include aclonifen, asulam, amitrole, bixlozone, bromobutide, cinmethylin, clomazone, cumyluron, cyclopyrimorate (6-chloro-3-(2-cyclopropyl-6-methylphenoxy)-4-pyridazinyl-4-morpholinecarboxylate), dymron, difenzoquat, etobenzanide, fluometuron, flurenol, fosamine, fosamine ammonium, dazomet, dymron, ipfencarbazone (1-(2,4- dichlorophenyl)-N-(2,4-difluorophenyl)-1,5-dihydro-N-(1-methylethyl)-5-oxo-4H-1,2,4-triazole-4-carboxamide), metam, methyldaimron, oleic acid, oxaziclomefone, pelargonic acid, pyributicarb, and 5-[[(2,6-difluorophenyl)methoxy]methyl]-4,5-dihydro-5-methyl-3-(3-methyl-2-thienyl)isoxazole, and tetflupyrolimet.

[0084] Fungicides useful in the present invention include acibenzolar-S-methyl, aldimorph, ametoctrazine, aminopyrifen, amisulbrom, anilazine, azaconazole, azoxystrobin, benalaxyl (including benalaxyl-M), benodanil, benomyl, benthiavalicarb (including benthiavalicarb-isopropyl), benzovindiflupyr, bethoxadin, binapacryl, biphenyl, bitertanol, bixafen, blasticidin-S, boscalid, bromuconazole, bupirimate, buthiobate, carboxin, carpropanol, and the like. amide, captafol, captan, carbendazim, chloroneb, chlorothalonil, chlozolinate, copper hydroxide, copper oxychloride, copper sulfate, cumoxystrobin, cyazofamid, cyflufenamid, cymoxanil, cyproconazole, cyprodinil, diclobenthiazox, dichlofluanid, diclocymet, diclomedine, dicloran, diethofencarb, difenoconazole, diflumetrim, dimethirimol, dimethomorph, dimoxystrobin, diniconazole (including diniconazole M), dinocap, dipimethitron, dithianon, di Thiolane, dodemorph, dodine, econazole, etaconazole, edifenphos, enoxastrobin (also known as enestrobin), epoxiconazole, ethaboxam, ethirimol, etridiazole, famoxadone, fenamidone, phenaminestrobin, fenarimol, fenbuconazole, fenfuram, fenhexamid, fenoxanil, fenpiclonil, fenpicoxamide, fenpropidin, fenpropimorph, fenpyrazamine, fentin acetate, fentin hydroxide, ferbam, ferimzone, flometoxin fluphenoxystrobin, flurylpicoxamide, fluopimomide, fluazinam, fludioxonil, flufenoxystrobin, fluindapyr, flumorph, fluopicolide, fluopyram, fluoxapiprolin, fluoxastrobin, fluquinconazole, flusilazole, flusulfamide, flutianil, flutolanil, flutriafol, fluxapyroxad, folpet, fthalide (also known as phthalide), fuberidazole, furalaxyl, furametpyr, hexaconazole, hymexazole, guazatine, imazalil, imibenconazole,Iminoctadine albesilate, Iminoctadine triacetate, Impirfluxam, Iodicarb, Ipconazole, Ipfentrifluconazole, Ipflufenoquine, Isofetamide, Iprobenfos, Iprodione, Iprovalicarb, Isoflucipram, Isoprothiolane, Isopyrazam, Isotianil, Kasugamycin, Kresoxim-methyl, Lancotrione, Mancozeb, Mandipropamide, Mandestrobin, Maneb, Mapanipirin, Mefentrifluconazole, Mepronil, Meptildinocap, Metalaxyl (Metalaxyl-M / Mefenoxam), metconazole, methasulfocarb, metiram, metominostrobin, methyltetraprole, metrafenone, myclobutanil, naphthitine, neo-asozin (ferric methanearsonate), nuarimol, octhilinone, ofrace, orysastrobin, oxadixyl, oxathiapiprolin, oxolinic acid, oxpoconazole, oxycarboxin, oxytetracycline, penconazole, pencycuron, penflufen, penthiopyrad, perfurazoate, phosphorous acid (salts thereof, e.g., fosetylaluminum), (including), picoxystrobin, piperalin, polyoxins, probenazole, prochloraz, procymidone, propamocarb, propiconazole, propineb, proquinazide, prothiocarb, prothioconazole, pydiflumetofen (Adepidyn®), pyraclostrobin, pyrametostrobin, pyrapropoin, pyroxystrobin, pyraziflumide, pyrazophos, pyribencarb, pyributacarb, pyridaclomethyl, pyrifenox, pyriophenone, perisoxazole, pyrimethanil, pyrifenox, pyrrolnitrite Phosphorus, pyroquilon, quinconazole, quinmethionate, quinofumelin, quinoxyfen, quintozene, silthiofam, sedaxane, simeconazole, spiroxamine, streptomycin, sulfur, tebuconazole, tebufloquine, tecloftalam, tecloftalam, tecnazene, terbinafine, tetraconazole, thiabendazole, thifluzamide, thiophanate, thiophanate-methyl, thiram, tiadinil, tolclofos-methyl, tolprocarb, trifluanid, triadimefon, triadimenol, triarimol, triazoxide,Tribasic copper sulfate, triclopyricarb, tridemorph, trifloxystrobin, triflumizole, trimoprhamide tricyclazole, trifloxystrobin, triforine, triticonazole, uniconazole, validamycin, valifenalate (also known as valifenal), vinclozolin, zineb, ziram, zoxamide, and 1-[4-[4-[5-(2,6-difluorophenyl)-4,5-dihydro-3-isoxazolyl]-2-thiazolyl]-1-piperidinyl]-2-[5-methyl- Fungicides such as ethyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]ethanone; fluopyram, spirotetramat, thiodicarb, fosthiazate, abamectin, iprodione, fluensulfone, dimethyl disulfide, thioxazaphen, 1,3-dichloropropene (1,3-D), metam (sodium and potassium), dazomet, chloropicrin, fenamiphos, ethoprophos, cadusafos, terbufos, imicyafos, oxamyl, carbofuran, thioxazaphen, Bacillus firmus (Bacillus Nematicides such as Streptomycin, quinomethionate, chlorobenzilate, cyhexatin, dicofol, dienochlor, etoxazole, fenazaquin, fenbutatin oxide, fenpropathrin, fenpyroximate, hexythiazox, propargite, pyridaben, and tebufenpyrad are also included.

[0085] In certain embodiments, the pesticidal active ingredient is an insecticide.

[0086] The term "insecticide" as used herein includes all agents that have a controlling or modifying effect on insect development, including, but not limited to, killing, injuring, retarding, inhibiting growth, disorienting, inhibiting reproduction, and the like.

[0087] In certain embodiments, the pesticidally active ingredient is a diamide, neonicotinoid, or nereistoxin analog insecticide, or a mixture thereof. In some embodiments, the pesticidally active ingredient is chlorantraniliprole, cyantraniliprole, tetraniliprole, cyclaniliprole, cyhalodiamide, tetra-chlorantraniliprole, bromoantraniliprole, dichlorantraniliprole, thiamethoxam, clothianidin, thiacloprid, monosultap, or bisultap, or a mixture thereof.

[0088] In certain embodiments, the pesticidal active ingredient is an anthranilamide.

[0089] The term "anthranilamide," as used herein, refers to a class of carboxamide arthropodicides that have insecticidal activity against numerous economically important agricultural and non-agricultural invertebrate pests. Anthranilamides affect calcium homeostasis by binding to ryanodine receptors, a class of intracellular calcium channels. Upon binding, the calcium channels open, releasing calcium ions into the cytoplasm. Depletion of calcium ion stores results in insect paralysis and death. Anthranilamides are chemically characterized by a molecular structure containing a vicinal carboxamide substituent attached to a carbon atom of an aryl ring, typically a phenyl, where one carboxamide moiety is attached through the carbonyl carbon and the other carboxamide moiety is attached through the nitrogen atom.

[0090] In some embodiments, the anthranilamide is selected from compounds of Formula I, their N-oxides and salts. [ka] wherein X is N, CF, CCl, CBr, or Cl; R 1 is H, CH3, Cl, Br or F; R 2 is H, F, Cl, Br or —CN; R 3is F, Cl, Br, C1-C4 haloalkyl or C1-C4 haloalkoxy; R 4a is H, C1-C4 alkyl, cyclopropylmethyl or 1-cyclopropylethyl; R 4b is H or CH; R 5 is H, F, Cl or Br; R 6 is H, F, Cl or Br.

[0091] In some embodiments, the anthranilamide is chlorantraniliprole, cyantraniliprole, tetraniliprole, cyclaniliprole, cyhalodiamide, bromoantraniliprole, dichlorantraniliprole, or tetra-chlorantraniliprole, or a mixture thereof. Other anthranilamides and methods for their preparation are described in detail in U.S. Pat. No. 6,747,047, WO 2003 / 015519, WO 2004 / 067528, WO 2006 / 062978, and WO 2008 / 069990, which are incorporated herein by reference.

[0092] In some embodiments, the anthranilamide is chlorantraniliprole, or cyantraniliprole, or a mixture thereof.

[0093] Chlorantraniliprole is an insecticide of the anthranilic acid diamide class, with the chemical name 5-bromo-N-[4-chloro-2-methyl-6-(methylcarbamoyl)phenyl]-2-(3-chloropyridin-2-yl)pyrazole-3-carboxamide, and is registered as a trademark by FMC Corporation under the trademark Rynaxypyr®. Chlorantraniliprole is a ryanodine receptor agonist and is used to protect a wide variety of crops, including corn, cotton, grapes, rice, and potatoes. Insects exposed to chlorantraniliprole exhibit generalized lethargy and muscle paralysis, which ultimately leads to death. Research results indicate that chlorantraniliprole exhibits superior differential selectivity for insect ryanodine receptors over mammalian ryanodine receptors. This selectivity appears to be a major factor in the mammalian safety observed with chlorantraniliprole.

[0094] Cyantraniliprole has the chemical name 3-bromo-1-(3-chloro-2-pyridinyl)-N-[4-cyano-2-methyl-6-[(methylamino)carbonyl]phenyl]-1H-pyrazole-5-carboxamide and is registered as a trademark by FMC Corporation under the trademark Cyazypyr®. Cyantraniliprole is a carboxamide of chlorantraniliprole, in which the chlorine atom on the phenyl ring is replaced with a cyano group. Cyantraniliprole can be used as an insecticide for the control of whiteflies, thrips, aphids, fruit flies, and fruitworms in crops such as onions, potatoes, and tomatoes. It acts as a ryanodine receptor agonist.

[0095] In certain embodiments, the compositions provided herein comprise an anthranilamide in an amount by weight of about 1% to about 10%, about 1% to about 8%, about 1% to about 7%, about 1% to about 6%, about 1% to about 5.5%, about 1%, about 2.5%, or about 5% of the composition. In certain embodiments, the anthranilamide is chlorantraniliprole.

[0096] The efficacy and chemical stability of the active ingredient and the physical stability of the formulation can be affected by the inactive ingredients in the formulation, and suitable inactive ingredients should not cause the active ingredient to decompose, not substantially reduce its activity upon application, or cause noticeable precipitation or crystal formation upon long-term storage. Furthermore, inactive ingredients should be non-phytotoxic and environmentally safe. In certain formulations, inactive ingredients can even enhance the biological performance of the active ingredient by facilitating penetration or absorption into plants or arthropod pests, or by increasing resistance to wash-off.

[0097] In certain embodiments, the enhancer comprises sodium dialkyl sulfosuccinate, sodium lauryl sulfate, sodium lauryl benzenesulfonate, fatty alcohol derivatives, sodium alkyl naphthyl sulfonate, dioctyl sodium sulfosuccinate, sodium alkyl naphthyl sulfate, or mixtures thereof.

[0098] In certain embodiments, the enhancer is selected from the group consisting of Geropon® SDS, Aerosol® MA-80I, Aerosol® OT series, MULTIWET TM MO-85P, MORWET® EFW, BEROL TM 790A, RHODACAL® DS 10, STEPWET® DF-90, Tergitol TM W-610, GEROPON® L WET F, GEROPON® L WET P, Terwet® 1004, Terwet® 1010, PETRO® AA, MORWET® IP, SUPRAGIL® WP, or SURFOM® HRB, or mixtures thereof.

[0099] In certain embodiments, the compositions provided herein comprise from about 0.1% to about 5%, by total weight, of at least one enhancer comprising sodium dialkyl sulfosuccinate.

[0100] The term "enhancer comprising sodium dialkyl sulfosuccinate," as used herein, refers to any enhancer containing sodium dialkyl sulfosuccinate and, optionally, one or more other substances, regardless of whether sodium dialkyl sulfosuccinate is the major component of the enhancer, so long as the enhancer can facilitate effective absorption of the active ingredient by the crop or pasture to a level that is effective for controlling pests. In certain embodiments, sodium dialkyl sulfosuccinate is the major component of the enhancer. In certain embodiments, the enhancer comprises more than about 50%, 55%, 60%, 65%, 70%, 75%, 80%, 85%, 90%, 95%, or 98% sodium dialkyl sulfosuccinate by weight. In certain embodiments, the enhancer is in solid form after being mixed with other components of the composition. In certain embodiments, the enhancer is in solid form before being mixed with any components of the composition.

[0101] Suitable enhancers include sodium dialkyl sulfosuccinates, such as Geropon® SDS, Aerosol® MA-80I, Aerosol® OT series, MULTIWET TM Including, but not limited to, MO-85P, and MORWET® EFW.

[0102] In certain embodiments, the enhancer is Geropon® SDS, a low use rate, high performance wetting agent for dry formulations.

[0103] In certain embodiments, the enhancer is Aerosol® OT-B or Aerosol® OT-75. Aerosol® OT-B and Aerosol® OT-75 are multipurpose anionic surfactants, such as wetting agents, emulsifiers, antistatic agents / emollients, etc., that can be utilized to reduce surface tension and increase absorbency and penetration, and provide very rapid migration to interfaces.

[0104] In certain embodiments, the enhancer is from about 0.1% to about 4%, from about 0.1% to about 3%, from about 0.1% to about 2%, from about 0.2% to about 2%, from about 0.3% to about 2%, from about 0.3% to about 1.8%, from about 0.3% to about 1.5%, from about 0.3% to about 1.2%, from about 0.3% to about 1%, from about 0.5% to about 1%, from about 0.6% to about 1%, from about 0.7% to about 1%, or about 0.8% of the composition by weight.

[0105] In certain embodiments, the dispersant is Geropon® T / 36, Geropon® TA-72, Geropon® SC-213, Geropon® Ultrasperse, Duramax® D-205, Duramax® D-305, Duramax® D-518, Tersperse® 2500, Tersperse® 2700, Atlox metasperse TM 550S, Tamol TM 731 SD, Tamol TM DN, YUS-TXC, Pluronic® PE 10400, MORWET TM D-360, MORWET TM D-110, Morwet® D-425, Tamol TM FB P1 or Tamol TM Includes NN8906.

[0106] In certain embodiments, the compositions disclosed herein comprise from about 0.1% to about 10%, by total weight, of at least one dispersing agent comprising a polycarboxylate.

[0107] As used herein, the term "polycarboxylate-containing dispersion" refers to any dispersion containing a polycarboxylate and, optionally, one or more other substances, regardless of whether the polycarboxylate is the primary component of the dispersion, so long as the dispersion can facilitate the diffusion and uniform distribution of the active ingredient in the liquid body. In certain embodiments, the polycarboxylate is the primary component of the dispersion. In certain embodiments, the dispersion comprises more than about 50%, 55%, 60%, 65%, 70%, 75%, 80%, 85%, 90%, 95%, or 98% polycarboxylate by weight. In certain embodiments, the dispersion is in solid form after being mixed with other components of the composition. In certain embodiments, the dispersion is in solid form before being mixed with any components of the composition.

[0108] Dispersants, as used herein, can facilitate the spreading and even distribution of the active ingredient in a liquid body, such as cold, hard water (e.g., containing more than about 300 ppm calcium carbonate, especially when the composition is to be applied unevenly).

[0109] Suitable dispersants containing polycarboxylates are known and include Geropon® T / 36, Geropon® TA-72, Geropon® SC-213, Geropon® Ultrasperse, Duramax® D-205, Duramax® D-305, Duramax® D-518, Tersperse® 2500, Tersperse® 2700, Atlox metasperse TM 550S and Tamol TM Including, but not limited to, 731 SD.

[0110] In certain embodiments, the dispersant is Tersperse® 2700. Tersperse® 2700 is an acid-resin copolymer-based dispersant (surfactant) developed primarily for use in water-dispersible granule formulations.

[0111] In certain embodiments, the dispersing agent is Geropon® T / 36, a multipurpose sodium polycarboxylate, very high performance dispersant, compatible chelating agent.

[0112] In a particular embodiment, the dispersant is Duramax® D-205.

[0113] In certain embodiments, the dispersing agent is from about 0.5% to about 10%, from about 0.5% to about 8%, from about 0.5% to about 7%, from about 0.5% to about 6%, from about 0.5% to about 5%, from about 0.8% to about 5%, from about 1% to about 5%, from about 1.2% to about 5%, from about 1.5% to about 5%, from about 1.7% to about 5%, from about 2% to about 5%, from about 2% to about 4.5%, from about 2% to about 4%, from about 2% to about 3.5%, from about 2% to about 3%, from about 2.2% to about 2.8%, from about 2.4% to about 2.6%, or about 2.5% by weight of the composition.

[0114] In certain embodiments, the enhancer is Geropon® SDS and the dispersant is Tersperse® 2700. In certain embodiments, the enhancer is Aerosol® OT-B and the dispersant is Duramax® D-205. In certain embodiments, the enhancer is Aerosol® OT-75 and the dispersant is Geropon® T / 36.

[0115] The preferred ranges of enhancer and dispersant can improve the efficacy of chlorantraniliprole-containing tablet compositions in terms of diffusivity or penetration. In certain embodiments, the ratio between enhancer and dispersant can be in the range of about 1:1 to 1:5, 1:1 to 1:4, 1:2 to 1:4, or 1:3 to 1:4 by weight. In certain embodiments, the ratio is 8:25 by weight. In certain embodiments, the ratio is about 1:3 by weight.

[0116] In certain embodiments, the compositions provided herein further comprise from about 0.1% to about 40% of at least one acid; and from about 0.1% to about 40% of at least one alkali.

[0117] As used herein, acids and alkalis generally work together to generate a gas upon contact with water, facilitating the disintegration of the composition and the diffusion of the active ingredient. In certain embodiments, the composition includes a solid acid that can react with the carbonate component of the composition to liberate carbon dioxide. The acid can be a water-soluble acidic substance, particularly a polyhydric organic acid, such as succinic acid, D,L-tartaric acid, L-tartaric acid, tartaric acid, alkali metal acid sulfate, lactic acid, adipic acid, citric acid, alkali metal acid citrate, alkali metal acid phosphate, alkali metal acid phthalate, and p-toluenesulfonic acid, malic acid, maleic acid, malonic acid, and oxalic acid. In certain embodiments, the acid is D,L-tartaric acid.

[0118] In certain embodiments, the compositions provided herein comprise between about 0.5% and about 25%, between about 1% and about 25%, between about 5% and about 25%, between about 10% and about 25%, between about 15% and about 25%, between about 16% and about 25%, between about 17% and about 25%, between about 18% and about 25%, between about 19% and about 25%, between about 20% and about 25%, between about 20% and about 24%, between about 20% and about 23%, between about 20% and about 22%, or about 21% of the composition by weight of the acid.

[0119] An alkali is an inorganic base that reacts with an acid to provide a source of carbon dioxide. Among these salts, sodium and potassium salts are preferred due to their good solubility and low cost. The alkali can be an alkali metal or alkaline earth metal carbonate, such as sodium carbonate, potassium carbonate, sodium bicarbonate, potassium bicarbonate, calcium carbonate, and calcium bicarbonate.

[0120] In certain embodiments, the compositions provided herein comprise alkali in an amount by weight of the composition of about 0.5% to about 40%, about 1% to about 40%, about 5% to about 40%, about 10% to about 40%, about 15% to about 40%, about 20% to about 40%, about 25% to about 40%, about 30% to about 40%, about 35% to about 40%, or about 38%.

[0121] In certain embodiments, the alkali is a mixture of bicarbonate and carbonate, such as sodium bicarbonate and sodium carbonate, or potassium bicarbonate and potassium carbonate. The ratio between bicarbonate and carbonate by weight can be in the range of about 1:10-10:1, about 1:5-10:1, about 1:3-10:1, about 1:2-10:1, about 1:1-10:1, about 2:1-10:1, about 3:1-10:1, about 3:1-9:1, about 3:1-8:1, about 3:1-7:1, about 3:1-6:1, about 3:1-5:1, about 3:1-4:1, about 3.5:1-4:1, or about 3.7:1.

[0122] In certain embodiments, the bicarbonate and carbonate are sodium bicarbonate and sodium carbonate, respectively, wherein the sodium bicarbonate comprises from about 0.5% to about 40%, from about 1% to about 40%, from about 5% to about 40%, from about 10% to about 40%, from about 15% to about 40%, from about 20% to about 40%, from about 25% to about 40%, from about 25% to about 35%, from about 27% to about 33%, or about 30%, and sodium carbonate is about 1% to about 40%, about 1% to about 30%, about 1% to about 20%, about 2% to about 20%, about 3% to about 20%, about 3% to about 18%, about 3% to about 15%, about 3% to about 12%, about 3% to about 10%, about 5% to about 10%, about 6% to about 10%, about 7% to about 10%, or about 8% by weight of the composition. In certain embodiments, the bicarbonate and carbonate are potassium bicarbonate and potassium carbonate, respectively, wherein the potassium bicarbonate comprises from about 0.5% to about 40%, from about 1% to about 40%, from about 5% to about 40%, from about 10% to about 40%, from about 15% to about 40%, from about 20% to about 40%, from about 25% to about 40%, from about 25% to about 35 ... 7% to about 33%, or about 30%, and potassium carbonate is about 1% to about 40%, about 1% to about 30%, about 1% to about 20%, about 2% to about 20%, about 3% to about 20%, about 3% to about 18%, about 3% to about 15%, about 3% to about 12%, about 3% to about 10%, about 5% to about 10%, about 6% to about 10%, about 7% to about 10%, or about 8% by weight of the composition.

[0123] The ratio of bicarbonate and / or carbonate to acid can vary within wide limits. For example, the compositions described herein may contain 0.05 to 2 (e.g., 0.1, 0.2, 0.3, 0.4, 0.5, 0.55, 0.6, 0.7, 0.8, 0.9, 1, 1.1, 1.2, 1.3, 1.4, 1.5, 1.6, 1.7, 1.8, or 1.9) equivalents of water-soluble acidic material per equivalent of bicarbonate and / or carbonate.

[0124] The term "equivalent" is used herein in an acid-base sense, with 1 gram molecular weight of solid acid being considered equivalent to 1 gram molecular weight of NaHCO or 0.5 gram molecular weight of NaCO. However, smaller amounts may be used, and the amount is not critical. It is only necessary that there be more than about 0.05 equivalents of acid for each equivalent of bicarbonate. In other words, when the alkali metal carbonate is bicarbonate, any amount greater than 0.05 equivalents of acid per equivalent of bicarbonate is sufficient to cause some foaming of the composition.

[0125] The compositions disclosed herein comprise, by total weight, about 0.1% to about 20% (e.g., about 1% to about 15%, about 1% to about 10%, about 1% to about 8%, about 1% to about 7%, about 1% to about 6%, about 1% to about 5.5%, about 2% to about 5.5%, about 3% to about 5.5%, about 3%, or about 5.5%) of at least one binder. The binder binds the various components of the composition together to aid in the integrity of the composition and reduce the generation of particulates during manufacturing, packaging, shipping, and delivery of the composition. Suitable binders include polyethylene glycol (PEG), maltose, trehalose, sorbitol, maltitol, polyvinylpyrrolidone (PVP), polyvinylpyrrolidone crosslinker (PVPP), dibasic calcium phosphate, sucrose, glucose, corn (maize) starch, modified cellulose, alginic acid, sodium carboxymethylcellulose, sodium hydroxymethylcellulose, or copovidone, or mixtures thereof. In certain embodiments, the binder comprises PEG. In certain embodiments, the binder comprises at least one selected from the group consisting of PEG200, PEG1000, PEG2000, PEG4000, PEG6000, PEG8000, and PEG10000. In certain embodiments, the binder comprises PEG6000.

[0126] The compositions disclosed herein comprise, by total weight, about 0.1% to about 50% (e.g., about 0.1% to about 45%, about 0.5% to about 45%, about 1% to about 45%, 1% to about 40%, about 1% to about 35%, about 1% to about 30%, about 5% to about 30%, about 8% to about 30%, about 10% to about 30%, about 15% to about 30%, about 20% to about 30%, about 25% to about 30%, about 5% to about 25%, about 5% to about 20%, about 5% to about 15%, or about 5% to about 10%) of at least one filler.

[0127] As used herein, the term "filler" refers to a substance added to a composition to increase its weight and / or size. Some suitable fillers are known and include, but are not limited to, sodium sulfate, ammonium sulfate, starch, bentonite, diatomaceous earth, kaolin, dextrin, maltodextrin, glucose, cellulose, microcrystalline cellulose, chitosan, lactose, lactose monohydrate, mannitol, sucrose, talcum, maltitol, sorbitol, xylitol, powdered cellulose, cellulose gum, starch, or calcium phosphate.

[0128] In certain embodiments, the compositions provided herein include at least two fillers. In certain embodiments, the ratio between the first filler and the second filler can vary from about 1:10 to 10:1 by weight (e.g., 1:9, 1:8, 1:7, 1:6, 1:5, 1:4.5, 1:4, 1:3.5, 1:3, 1:2, 1:1, 2:1, 3:1, 3.5:1, 4:1, 4.5:1, 5:1, 6:1, 7:1, 7:1, 8:1, or 9:1).

[0129] In certain embodiments, the filler comprises talcum, maltodextrin, or a mixture thereof. In certain embodiments, the filler comprises a mixture of talcum and maltodextrin. In certain embodiments, the ratio between talcum and maltodextrin is in the range of about 1:1 to 1:10, 1:1 to 1:9, 1:1 to 1:8, 1:1 to 1:7, 1:2 to 1:7, 1:2 to 1:6, 1:3 to 1:6, 1:3 to 1:5, 1:3 to 1:4, 1:4 to 1:5, 1:5, 1:4.5, 1:4, 1:3.5, 1:3, or 1:2 by weight. In some embodiments, the ratio between talcum and maltodextrin is about 1:3.3 by weight. In some embodiments, the ratio between talcum and maltodextrin is about 1:4.5 by weight.

[0130] Various minor components can be added to the composition of the present disclosure, but are not required. Examples of such minor components include lubricants such as magnesium stearate; bitters; fragrances; optical brighteners; dyes; and sodium carboxymethylcellulose. If necessary, the composition can also be coated with a water-soluble film, such as a polyvinyl alcohol film.

[0131] Lubricants can be used to improve tablet release from the tablet-forming apparatus, for example, by preventing adhesion to the face of the upper punch ("picking") or the face of the lower punch ("sticking"). Suitable lubricants include, for example, white carbon, talcum powder, magnesium stearate, calcium stearate, sodium stearate, zinc stearate, stearic acid, boric acid, metal stearates, sodium stearyl fumarate, fatty acids, fatty alcohols, fatty acid esters, glyceryl behenate, canola oil, mineral oil, vegetable oil, glyceryl palmitostearate, hydrogenated vegetable oil, hydrogenated vegetable oil, magnesium oxide, poloxamer, paraffin, leucine, propylene glycol fatty acid esters, polyvinyl alcohol sodium benzoate, sodium lauryl sulfate, sodium stearyl fumarate, polyethylene glycol, polypropylene glycol, and polyalkylene glycol. Preferably, the lubricant comprises stearic acid and salts thereof, such as calcium, magnesium, and aluminum stearates. In certain embodiments, the lubricant comprises magnesium stearate. In one embodiment, magnesium stearate is included as a lubricant in an amount by weight of the composition of about 0.1% to about 5% (e.g., about 0.1% to about 4.5%, about 0.1% to about 4.0%, about 0.1% to about 3.5%, about 0.1% to about 3.0%, about 0.1% to about 2.5%, about 0.1% to about 2.0%, about 0.1% to about 1.5%, about 0.1% to about 1.0%, about 0.5% to about 1.0%, about 0.5% to about 0.7%, about 0.5%, or about 0.7%).

[0132] Bitters can also be used as aversive agents in the compositions provided herein to discourage inappropriate ingestion by humans or non-target animals. Suitable bitters include, but are not limited to, benzodiazepines, denatonium, sucrose octaacetate, quercetin, brucine, and quassin. In certain embodiments, the bitters include denatonium benzoate. In certain embodiments, the bitters is denatonium benzoate. In one embodiment, denatonium benzoate is included as a bitter in an amount of about 0.01% to about 5% (about 0.01% to about 4.5%, about 0.01% to about 4.0%, about 0.01% to about 3.5%, about 0.01% to about 3.0%, about 0.01% to about 2.5%, about 0.01% to about 2.0%, about 0.01% to about 1.5%, about 0.01% to about 1.0%, about 0.01% to about 0.5%, about 0.01% to about 0.4%, about 0.01% to about 0.3%, about 0.01% to about 0.2%, about 0.01% to about 0.1%, about 0.01% to about 0.05%, about 0.05%, or about 0.1% by weight of the composition.

[0133] In certain embodiments, the compositions provided herein are substantially free of any organic solvents, e.g., in an amount less than 10%, 5%, 3%, 1%, 0.5%, 0.2%, 0.1%, 0.05%, 0.01%, 0.001%, 0.0001%, 0.00001%, or 0.000001% of the composition by weight.

[0134] In certain embodiments, the composition is substantially free of any fines within the tablet, e.g., in an amount less than 10%, 5%, 3%, 1%, 0.5%, 0.2%, 0.1%, 0.05%, 0.01%, 0.001%, 0.0001%, 0.00001%, or 0.000001% of the composition by weight.

[0135] In certain embodiments, the compositions may optionally contain one or more additional active ingredients selected from herbicides, fungicides, bactericides, insecticides, nematicides, acaricides, and growth regulators.

[0136] In certain embodiments, the compositions provided herein can be formulated as tablet compositions. In certain embodiments, each single tablet contains about 0.0004 g to about 1 g, about 0.001 g to about 0.5 g, about 0.002 g to about 0.4 g, about 0.003 g to about 0.3 g, about 0.004 g to about 0.2 g, about 0.005 g to about 0.2 g, about 0.01 g to about 0.3 g, about 0.05 g to about 0.3 g, about 0.07 g to about 0.3 g, about 0.1 g to about 0.3 g, about 0.1 g to about 0.25 g, about 0.1 g to about 0.2 g, about 0.0034 g, about 0.0775 g, or about 0.15 g of the active ingredient component (a).

[0137] The term "tablet composition" as used herein means a solid form that can be prepared by compacting or compressing a powder in a tablet press, as is well known in the pharmaceutical art.

[0138] The tablet compositions of the present disclosure may be homogeneous or heterogeneous. The term "homogeneous" as used herein refers to a tablet made by molding or compressing a single particulate composition, but does not imply that the particles of that composition will necessarily all be of the same composition. The term "heterogeneous" as used herein refers to a tablet having multiple discrete regions, such as layers, inserts, or coatings around inserts.

[0139] The tablets can be prepared using conventional tablet manufacturing equipment and can be of any suitable size and shape, e.g., round, oval, polygonal, or pillow-shaped, and optionally have non-functional surface markings. The tablets of the present invention can be packaged in a container with a package insert providing pertinent information, such as dosage and administration information, contraindications, precautions, drug interactions, and adverse drug reactions.

[0140] The compositions provided herein can be manufactured by known conventional methods, preferably involving blending, sieving, and compressing the components. Typically, a powder blend is prepared by blending to uniformity, passing through a sieve, typically having a mesh size of about 70-200 mesh, and compressing to the desired tablet size and density in a tablet machine (e.g., a 5,000-10,000 pound force hydraulic press).

[0141] In certain embodiments, the compositions provided herein have a density greater than the density of water (specific gravity greater than 1.00) such that the tablets sink when contacted with water.

[0142] In embodiments, tablets of the present disclosure may further comprise a coating, e.g., a non-functional coating. The non-functional coating may include a polymer component, e.g., HPMC, optionally with other components, e.g., one or more plasticizers, colorants, etc. In such embodiments, the tablet will be subjected to an additional coating step after compression. The term "non-functional," as used herein, means a means that has substantially no effect on the release characteristics of the tablet and should not be interpreted to imply that the coating serves no useful purpose. For example, such a coating may impart a unique appearance to the tablet, provide protection from abrasion during packaging and shipping, and / or have other benefits.

[0143] The tablet composition can be manufactured into any size suitable for its application. In certain embodiments, the tablet is about 0.01 g to about 20 g, about 0.05 g to about 20 g, about 0.1 g to about 20 g, about 0.2 g to about 20 g, about 0.5 g to about 20 g, about 0.5 g to about 15 g, about 0.5 g to about 10 g, about 1 g to about 10 g, about 1 g to about 5 g, about 2 g to about 5 g, about 3 g to about 5 g, about 3 g to about 4.5 g, about 3 g to about 4 g, or about 3.0 g to 3.4 g.

[0144] In certain embodiments, the tablet has a diameter of about 5 mm to about 100 mm, about 5 mm to about 50 mm, about 5 mm to about 40 mm, about 5 mm to about 35 mm, about 5 mm to about 30 mm, about 10 mm to about 15 mm, about 10 mm to about 30 mm, about 15 mm to about 30 mm, about 20 mm to about 30 mm, about 20 mm to about 25 mm, about 20 to about 22 mm, about 20 mm, or about 22 mm.

[0145] In certain embodiments, the compositions provided herein have a pH value in the range of 5.0 to 8.0, optionally 6.0 to 7.0, when the composition is diluted in water at 1% by weight. In certain embodiments, the compositions provided herein have a pH value of about 6.5, 6.7, or 6.8 (diluted 1% by weight in water).

[0146] Hardness is the amount of force required to cause compact fracture under conditions of storage, transportation, and handling prior to use, and is typically expressed in units such as kiloponds (kp), Strong-Cobb units (SCU), or Newtons (N). A hardness of about 1 SCU roughly represents a force of 0.7 kp or about 7 N. Uncoated tablets, or pre-coated tablet cores, containing at least one filler provided herein that serves as a matrix for a water-soluble pesticide may need to have a certain minimum hardness to withstand breakage and / or abrasion due to mechanical stress imposed during high-speed tableting operations (including all steps up to and including filling of tablets into containers). The minimum acceptable hardness will depend on numerous factors, such as the severity of the mechanical stress, but is typically at least about 70 N (e.g., greater than 80 N, 90 N, 100 N, or 105 N). In certain embodiments, the tablet compositions provided herein have a tablet hardness of 106, 79, or 75 N.

[0147] The formulation components may be dried before blending, milling, and compressing. Drying in a vacuum oven at 45-60°C for 16 hours is sufficient to reduce the moisture content of the premix to less than about 3.0%. This helps prevent residual moisture from foaming and initiating a reaction during storage. The components are typically ground and mixed in a mill, such as an air mill or hammer mill. The ground premix is ​​brushed through a 70-200 mesh screen. In certain embodiments, the moisture content of the composition is less than 3.0%, 2.5%, 2.0%, 1.9%, 1.8%, 1.7%, 1.6%, 1.5%, 1.0%, or 0.5%.

[0148] The present disclosure also provides a method for controlling pests in crops, comprising applying an agronomically effective amount of the composition to the crop or its environment in need thereof.

[0149] The term "agriculturally effective amount," as used herein, means the amount or rate of application of a pesticide composition that, when applied to a crop or pasture, will kill or substantially damage a substantial portion of the pest or weed or fungal population present therein and / or substantially reduce damage to the crop or pasture at any stage of its growth cycle.

[0150] In certain embodiments, the crop is agricultural or non-agricultural.

[0151] The term "agricultural crops" means agricultural crops, such as those used for food and fiber, and includes corn; soybeans and other legumes; grains (e.g., wheat, oats, barley, rye, rice, and corn); vegetables, such as leafy vegetables (e.g., lettuce, cabbage, and other greens), fruiting vegetables (e.g., tomatoes, peppers, eggplant, crucifers, and cucurbits), potatoes, sweet potatoes; cotton; fruits, grapes, tree fruits (e.g., pome fruits, stone fruits, and citrus fruits), small fruits (e.g., berries and cherries); and other specialty crops (e.g., canola, sunflowers, and olives).

[0152] The term "non-agricultural crops" refers to other horticultural crops (e.g., greenhouse plants, nursery plants, or ornamental plants not grown in fields, plants in residential and commercial structures in urban and industrial environments), turf (e.g., turf farms, pastures, golf courses, lawns, residential, recreational, and sports fields), wood products, storage products, agroforestry and vegetation for public health (i.e., humans) and animal health (e.g., non-domesticated animals such as pets, livestock, poultry, and wildlife) related uses.

[0153] Invertebrate pests are controlled in agricultural and non-agricultural applications by applying an effective amount of a composition provided in this disclosure to the pest's environment, such as the agricultural and / or non-agricultural locus of infestation, to the area to be protected, or directly on the pest to be controlled.

[0154] The term "invertebrate pests," as used herein, includes arthropods, gastropods, and nematodes that are economically important as pests. The term "arthropods" includes insects, mites, spiders, scorpions, centipedes, millipedes, woodlice, and symphysophorans. The term "gastropods" includes snails, slugs, and other Stylommatophora. The term "nematodes" includes roundworms, heartworms, and all parasitic helminths, such as herbivorous nematodes (Nematoda), trematodes (Tematoda), Acanthocephala, and tapeworms (Cestoda).

[0155] Agricultural applications include protecting agricultural crops from invertebrate pests by typically applying a composition or mixture of compositions of the present disclosure between rows during sowing, to crop seeds before sowing, to the foliage, stems, flowers, and / or fruits of crop plants, or to the soil or other growing medium (e.g., rice paddies) before, after, or while the crop is planted. Non-agricultural applications refer to invertebrate pest control in areas other than those related to crop plants. The term non-agricultural includes invertebrate pest control in stored grains, beans, and other foodstuffs, and in textiles such as clothing and carpets. Non-agricultural applications also include invertebrate pest control in ornamental plants, forests, gardens, along roadsides and railroad rights-of-way, and on turf soils such as lawns, golf courses, and pastures. Non-agricultural applications also include invertebrate pest control in homes and other buildings that may be occupied by humans and / or pets, farms, ranches, zoos, or other animals. Non-agricultural uses also include the control of pests such as termites that can damage wood or other structural materials used in buildings. Non-agricultural uses also include protecting human and animal health by controlling invertebrate pests that are parasitic or transmit infectious diseases. Such pests include, for example, chiggers, ticks, lice, mosquitoes, flies, and fleas.

[0156] One embodiment of composition application is by spraying. Alternatively, tablet compositions comprising the disclosed compositions can be applied to plant foliage or soil. The disclosed compositions can also be effectively delivered through plant uptake by contacting the plant with the disclosed compositions applied as a tablet formulation to the soil, nursery box treatment, or transplanted plants as a soil drench. In certain embodiments, the crop is rice and the composition is applied to a rice field. In certain embodiments, the composition can be manually or mechanically sprinkled onto or poured from the rice field, i.e., by manually pouring from a narrow path between rice fields without entering the rice field.

[0157] The method is applicable to any cropping situation where control of a pest or pest life stage is required. The method can be useful when combined with seeding or transplanting operations, but can also be used in mature crops, especially established rice fields.

[0158] Pests that may be controlled by the compositions include larvae of the order Lepidoptera, such as armyworms, cutworms, loopers, and heliothins in the family Noctuidae (e.g., Spodoptera fugiperda J.S. Smith, Spodoptera exigua Huebner, Agrotis ipsilon Hufnagel, Trichoplusia ni Huebner, and Heliothis virescens Fabricius); borers, cocooning insects, webworms, pine coneworms, caterpillars, and leaf-eating larvae from the family Pyralidae (e.g., Ostrinia nubilalis Huebner), navel orangeworm (Amyelois transitella Walker), corn root webworm (Crambus caliginosellus Clemens), and sod webworm (Herpetogramma licarsisalis Walker); tortricid moths in the Tortricidae family, caterpillars that feed on plant buds, seedworms, and fruitworms (e.g., codling moth (Cydia pomonella L. (L. stands for Linnaeus), grape berry moth (Endopiza viteana Clemens), and pear fruit moth (Grapholita molesta Busck)); and many other economically important Lepidoptera (e.g., diamondback moth (Plutella xylostella L. in the Plutellidae family), cotton bollworm (Pectinophora gossypiella Saunders), and the gypsy moth (Lymantria dispar L. of the Lymantriidae family).)); foliar-feeding larvae and adults of the order Coleoptera, such as weevils from the families Anthribidae, Bruchidae, and Curculionidae (e.g., boll weevil (Anthonomus grandis Boheman), rice water weevil (Lissorhoptrus oryzophilus Kuschel), and rice weevil (Sitophilus oryzae L.)); flea beetles, cucumber beetles, rootworms, leaf beetles, Colorado potato beetles, and leafminers in the family Chrysomelidae (e.g., Colorado potato beetle (Leptinotarsa ​​decemlineata Say) and western corn rootworm (Diabrotica virgifera LeConte); scarab beetles and other beetles from the family Scarabaeidae (e.g., bean beetle (Popillia japonica Newman) and European scarab beetle (Rhizotrogus majalis Razoumowsky)); click beetle larvae from the family Elateridae and bark beetles from the family Scolytidae; earwig beetles from the family Forficulidae (e.g., European earwig (Forficula auricularia L.) and black earwig (Chelisoches morio Adults and larvae of the order Dermaptera, such as earwigs from the family Fabricius; mirid bugs from the family Miridae, cicadas from the family Cicadidae, leafhoppers from the family Cicadellidae (e.g. Empoasca spp.), planthoppers from the families Fulgoroidae and Delphacidae, treehoppers from the family Membracidae, psyllids from the family Psyllidae, whiteflies from the family Aleyrodidae, aphids from the family Aphididae, mealybugs from the family Phylloxeridae, mealybugs from the family Pseudococcus mealybugs from the families Coccidae, Diaspididae and Margarodidae, scale insects from the families Tingidae, stink bugs from the family Pentatomidae, American long-horned stink bugs from the family Lygaeidae (e.g., Blissus spp.), adults and nymphs of the orders Hemiptera and Homoptera, such as the migratory grasshoppers (e.g., Melanoplus sanguinipes Fabricius and M. differentialis Thomas), American grasshoppers (e.g., Schistocerca americana Drury), desert grasshoppers (Schistocerca gregaria Forskal), migratory grasshoppers (Locusta migratoria L.), and mole crickets (Gryllotalpa spp.). spp.), adults and nymphs; leafminers, midges, fruit flies (Family Tephritidae), and fruit flies (e.g., Oscinella frit L.Adults and nymphs of the order Diptera, such as onion thrips (Thrips tabaci Lindeman) and other foliar-feeding thrips; and adults and nymphs of the order Thysanoptera, such as onion thrips (Thrips tabaci Lindeman) and other foliar-feeding thrips.

[0159] In certain embodiments, pests that can be controlled by the compositions include rice water weevil (lissorhoptrus oryzophilus), fall armyworm, Spodoptera frugiperda, sugarcane borer, sugarcane borer (diatraea saccharalis), rice leaf borer (scirpophaga incertulas), chilo polychrysa, rice armyworm (sesamia inferens), green rice leafhopper (nephotettix virescens), black-striped rice leafhopper (nephotettix nigropictus), brown planthopper (nilaparvata lugens), narrow-headed stink bug (leptocorisa acuta), white-backed planthopper (sogatella furcifera, lightning leafhopper (Recilia dorsalis), rice thrips (thrips oryzae), armyworm (Mythimna separata), armyworm (Spodoptera mauritia), rice spur beetle (Dicladispa armigera), rice leafroller (Cnaphalocricis medinalis), nymphula depunctalis, skipper butterfly (Parnara guttata), and rice gall midge (Orseolia oryzae).

[0160] The rate of application required for effective control (i.e., "agriculturally effective amount") will depend on factors such as the active ingredient, the operator, the invertebrate species to be controlled, the pest life cycle, life stage, its size, location, time of year, host crop or animal feeding behavior, mating behavior, crop sowing or planting density and pattern, environmental humidity, temperature, and whether the composition is applied as a preventative or salvage operation. Under normal circumstances, the compositions may be applied in an agroecosystem at a rate ranging from about 10 grams active ingredient per hectare (gai / ha) to about 10,000 gai / ha (e.g., about 10 to about 5000 gai / ha, about 10 to about 1000 gai / ha, about 10 to about 500 gai / ha, about 10 to about 200 gai / ha, about 10 to about 100 gai / ha, about 10 to about 90 gai / ha, about 10 to about 80 gai / ha, about 10 to about 70 gai / ha, about 10 to about 60 gai / ha, about 10 to about 50 gai / ha, about 20 to about 50 gai / ha, about 30 to about 50 gai / ha, or about 40 gai / ha), although as little as 0.1 gai / ha may be sufficient or as much as 80,000 gai / ha may be required. In certain embodiments, the composition is applied at a rate of about 40 gai / ha. For non-agricultural applications, effective use rates are about 1.0 to 50 mg / m². 2 ) (e.g., about 1 to 40 mg / m 2 , about 1~35mg / m 2 , about 1~30mg / m 2 , about 1~25mg / m 2 , about 1~20mg / m 2 , about 1~15mg / m 2 , about 1~10mg / m 2 , or about 1 to 5 mg / m 2 ) range, but 0.1 mg / m 2 As little as 150 mg / m may be sufficient. 2 Those skilled in the art can readily determine the agriculturally effective amount needed for the desired level of invertebrate pest control. [Example]

[0161] The present invention will now be described in more detail by way of specific examples. The following examples are provided for illustrative purposes and are not intended to limit the present invention in any way. Those skilled in the art will readily identify a variety of non-critical parameters that can be changed or modified to yield essentially the same results.

[0162] Example 1. Anthranilamide Tablet Screening preparation The tablets tested in the examples were prepared according to the following steps: all ingredients were weighed, thoroughly mixed, and sieved to obtain particles in the range of 70-200 mesh, then pressed in a 60 kilonewton (kN) tablet press. The resulting tablets, weighing 3.0-3.5 g and having a diameter of approximately 20-22 mm, were then formed.

[0163] Preliminary Screening Prior to screening enhancers and dispersants for use in chlorantraniliprole-containing formulations, the following preliminary screening procedure was performed.

[0164] Acid and alkali. Different combinations of acid and alkali were screened based on (a) their ability to generate a desired amount of foam upon contact with water that lasts for a desired period of time and facilitates complete dispersion of the active ingredient in the water where the plants are grown, (b) cost, and (c) industrial processability (e.g., from a safety perspective). Based on the screening, preferred combinations of acid and alkali were identified and used in the following examples.

[0165] Lubricants, Binders, and Fillers. Different types of lubricants, binders, and fillers were screened. Based on the screening, preferred lubricants, binders, and fillers were identified and used in the following examples.

[0166] Enhancer and dispersant screening Tablets with different recipes (e.g., containing both enhancer and dispersant, enhancer only, dispersant only, or different types of enhancer and dispersant) were prepared and compared in terms of tablet bubble degree and diffusivity upon contact with water. The bubble degree was observed visually, and pigments were used to track tablet diffusion. The recipes and results are summarized in Table 1 below. It can be seen that Recipes 1-4, 1-5, and 1-7 performed better than the remaining recipes in terms of bubble degree and diffusivity, with more + indicating better performance.

[0167] [Table 1]

[0168] The distribution profiles of Recipes 1-4, 1-5, 1-7, and 1-8 were further investigated by the following method: (a) a circular pool with a radius of 1.2 m was prepared, and watch glasses were placed under each of the sampling locations shown in Figure 1, where the distance between each two adjacent outer lines was 15 cm. Four spots (such as A1, A2, A3, and A4) evenly spaced on one outer line were selected as sampling locations; (b) the pool was filled with tap water to a depth of approximately 5 cm; (c) one tablet (3 g) was added to the pool; (d) after 30 minutes, the watch glass was covered and removed from the pool; (e) the content of the active ingredient (such as the dissolved active ingredient, the suspended active ingredient, and the deposited active ingredient on the watch glass) in the collected watch glass was analyzed by HPLC; (e) the average value of the active ingredient collected from the four pots was calculated. The results are shown in Figure 2. It can be seen that the tablets having both an enhancer containing sodium dialkyl sulfosuccinate and a dispersant containing polycarboxylate (i.e., recipes 1-4, 1-5, and 1-7) achieved much better results compared to the other recipes.

[0169] Example 2. New anthranilamide tablets Based on the screening in Example 1, the recipes were further optimized to add bitter or aversive agents to the tablet compositions to prevent aspiration by humans or animals. The optimized recipes with different concentrations of chlorantraniliprole (Rynaxypyr® AI) are shown in Table 2. Tablets were prepared in the same manner as described in Example 1.

[0170] [Table 2]

[0171] Distribution profile analysis Using the same method described in Example 1 to examine the distribution profile of the tablets in Table 2, it was found that the tablets in Table 2 achieved improved efficacy.

[0172] Stability testing The stability of the tablets in Table 2 was tested after 14 days of storage, and the data are shown in Table 3.

[0173] [Table 3]

[0174] Efficacy analysis (21 days after tablet application) Rice seedlings were transplanted into paddy fields at the 4.5-leaf stage and grown for 7 days to allow the seedlings to green up before insecticide application. The chlorantraniliprole tablets in Table 2 and the commercially available chlorantraniliprole products Ferterra® and CORAGEN® (control) were applied separately to selected fields under consistent field conditions. Both the tablets and Ferterra® were applied by broad-spectrum application, while CORAGEN® was applied by foliar application. Chlorantraniliprole tablets and Ferterra® were generally applied uniformly 7 days after transplanting at a rate of 40 gai / ha. CORAGEN® was usually mixed with water and applied by foliar application at the early stage of striped stem borer egg hatching at a rate of 30 gai / ha. One control (no treatment, "CK") paddy field was selected for efficacy benchmarking. The efficacy of the tablets was further investigated 21 days after tablet application. A whole-plot survey was adopted to count the rice seedlings showing heart dieback caused by the rice striped borer in each treatment plot, and the efficacy was calculated by the following formula: % Efficacy = ((Number of heart wither in CK group) - (Number of heart wither in treatment group)) / (Number of heart wither in CK group) * 100.

[0175] The results are shown in Table 4.

[0176] [Table 4]

[0177] The results, shown in Table 4, demonstrated that chlorantraniliprole tablets applied at 40 gai / ha could effectively control rice stem borers. The 1%, 2.5%, and 5% chlorantraniliprole tablets achieved similar or slightly better control than both the granular (Ferterra®) and SC formulations ("SC", CORAGEN®) containing the same dose of chlorantraniliprole, while requiring more labor for application of the tablet formulations.

[0178] Residues of the active ingredient, chlorantraniliprole, in physical examinations of fields 1% chlorantraniliprole tablets (4 g), 2.5% chlorantraniliprole tablets (1.6 g), 5% chlorantraniliprole tablets (0.8 g), Ferterra® (0.04 g / 25 m 2 Calculated based on 0.4% granules), and CORAGEN (0.04g / 25m 2 A 200g / L SC formulation (calculated for the 200g / L formulation) was applied to a 5x5m plot. Rice seedlings were sampled 3 days (3 DAA) and 20 days (20 DAA) after formulation application. Since the rice stem borer primarily attacks rice stems, the amount of chlorantraniliprole residue in the rice stems was tested to verify the absorption of the active ingredient, which can be ingested by the rice stem borer and cause toxic effects. To extract the active ingredient, chlorantraniliprole, rice seedlings were cut, the stems were removed, and soaked in acidic acetonitrile for 24 hours. The resulting solution was further shaken for 2 hours, then filtered and analyzed by GC-MS to determine the amount of the active ingredient, chlorantraniliprole, absorbed by the rice seedlings.

[0179] According to the GC-MS test results, the residual amounts of chlorantraniliprole (μg / kg) in rice are summarized in Table 5 and illustrated in Figure 3. Seedlings treated with 1% chlorantraniliprole tablets (4 g), 2.5% chlorantraniliprole tablets (1.6 g), or 5% chlorantraniliprole tablets (0.8 g) absorbed higher amounts of the active ingredient chlorantraniliprole than those treated with Ferterra® or CORAGEN® at 3 and 20 days after formulation application, suggesting that the tablet formulations containing the claimed enhancer and dispersant disperse more effectively in paddy water.

[0180] [Table 5]

[0181] The concentration of chlorantraniliprole in seedlings collected at different distances from the application site was measured as described above, and the results are summarized in Tables 6 and 7 and shown in Figure 4.

[0182] [Table 6]

[0183] [Table 7]

[0184] Example 3. More tablets Several tablets are prepared containing similar components to the tablets in Table 2, but containing different pesticide active ingredients. It is expected that those tablets containing the claimed enhancer and dispersant will be able to achieve improved effects similar to those of the tablets in Table 2 in terms of diffusibility and penetration.

[0185] The present invention may also be broadly said to consist in the moieties, elements and features referred to or shown herein, individually or collectively, and in any or all combinations of two or more moieties, elements, members or features, where specific integers are referred to herein and which have known equivalents, and such equivalents are deemed to be incorporated herein as if individually set forth.

[0186] The present invention has been described with particular reference to certain embodiments thereof. It will be understood that various modifications of the above-described embodiments may be made without departing from the scope of the invention. Those skilled in the art will also understand the concept of what is meant by object syntax.

Claims

1. The following components (a) through (e), by weight, based on the total weight of the tablet composition: (a) 0.1% to 20% of a pesticidal active ingredient comprising chlorantraniliprole, cyantraniliprole, tetraniliprole, cyclaniliprole, cyhalodiamide, tetra-chlorantraniliprole, bromoantraniliprole, dichlorantraniliprole, thiamethoxam, clothianidin, thiacloprid, monosultap, or bisultap, or a mixture thereof; (b) 0.1% to 5% of an enhancer comprising a salt of a dialkyl sulfosuccinate; (c) 0.1% to 10% of a dispersant, wherein the dispersant comprises a polycarboxylate, a phenolsulfonic acid condensate, a polyoxypropylene-polyoxyethylene block copolymer, or a naphthalenesulfonic acid condensate, or a mixture thereof; (d) 0.1% to 20% of a binder; (e) 0.1% to 50% of an optional filler; A tablet composition comprising:

2. 10. The tablet composition of claim 1, wherein component (a) comprises chlorantraniliprole.

3. 3. The tablet composition of claim 1 or 2, wherein component (d) comprises at least one substance selected from the group consisting of polyethylene glycol (PEG), maltose, trehalose, sorbitol, maltitol, polyvinylpyrrolidone, dibasic calcium phosphate, sucrose, glucose, corn (maize) starch, modified cellulose, alginic acid, sodium carboxymethylcellulose, and copovidone, and optionally, component (d) comprises PEG.

4. The component (d) is PEG2000, PEG4000, PEG6000, PEG8 4. The tablet composition of claim 1, wherein component (d) comprises at least one PEG selected from the group consisting of PEG 10000 and PEG 10000, and optionally component (d) comprises PEG 6000.

5. 5. The tablet composition of claim 1, wherein component (e) comprises at least one substance selected from the group consisting of lactose, lactose monohydrate, mannitol, sucrose, talcum, maltodextrin, dextrin, maltitol, sorbitol, xylitol, powdered cellulose, cellulose gum, microcrystalline cellulose, starch, and calcium phosphate.

6. 6. The tablet composition of any one of claims 1 to 5, wherein component (e) comprises talcum or maltodextrin, or a mixture thereof.

7. 7. The tablet composition of any one of claims 1 to 6, wherein component (e) comprises a mixture of talcum and maltodextrin.

8. 8. The tablet composition of claim 5, wherein the talcum, if used, is in an amount of 1% to 15% by weight of the composition, and the maltodextrin, if used, is in an amount of 1% to 40% by weight of the composition.

9. By weight, based on the total weight of the composition: Component (f) 0.1% to 40% of at least one acid selected from polyhydric organic acids; and 9. The tablet composition of any one of claims 1 to 8, further comprising component (g) 0.1% to 40% of at least one alkali selected from alkali metal or alkaline earth metal carbonates.

10. 10. The tablet composition of any one of claims 1 to 9, further comprising, by weight based on the total weight of the composition: component (i) 0.01% to 5% of at least one bitter.

11. A method for controlling pests in crops, comprising the step of applying an agriculturally effective amount of the tablet composition according to any one of claims 1 to 10 to the crops or the environment of the crops in need thereof.

12. 12. The method of claim 11, wherein the crop is rice and the tablet composition is applied to a paddy field.

13. 12. The method of claim 11, wherein the crop is selected from the group consisting of rice, vegetables, and corn.

14. The method of claim 11 , wherein the crop is rice.

Images