Anthranilamide compositions

Abstract

The present disclosure provides an agrochemical composition comprising a pesticidal active ingredient, an enhancer comprising a dialkyl sulfosuccinate, a dodecyl sulfate, a dodecyl benzene sulfonate, a fatty alcohol derivative, an alkyl naphthalene sulfonate, or an alkyl naphthalene sulfate, or a mixture thereof, and a dispersing agent comprising a polycarboxylate, a phenol sulfonic acid condensate, a polyoxypropylene-polyoxyethylene block copolymer, or a naphthalene sulfonic acid condensate, or a mixture thereof. The present disclosure also provides a method for controlling pests in crops, the method comprising applying an agriculturally effective amount of the composition to the crops or their environment in need.

Description

[0001] Cross-reference to related applications

[0002] This application claims the benefit of U.S. Provisional Application No. 62 / 906801, filed on September 27, 2019. Technical Field

[0003] This disclosure relates to a novel composition comprising o-aminobenzamide and a method comprising applying said composition for the control of pests. Background Technology

[0004] Anthranilamide (also considered anthranilic acid diamide) is an important synthetic insecticide that affects calcium homeostasis, exhibiting high selectivity for insect reniform receptors compared to mammalian receptors. Chlorantraniliprole is the most widely used insecticide in this class. It has high bioactivity against pests belonging to the orders Lepidoptera and some Coleoptera, Diptera, and Isoptera, and exhibits very low toxicity to non-target arthropods. Chlorantraniliprole is primarily active through ingestion and secondarily through contact with chewing pests.

[0005] Typically, developed chlorantraniliprole formulations include suspension concentrates (SC), water-dispersible granules (WDG), suspension seed coatings (FS), and granules (GR). These pest control agents are usually applied by spraying. Manual spraying of pest control agents as aqueous solutions or suspensions is labor-intensive and time-consuming. Current labor-saving technologies, such as ultra-low volume (ULV) and aerial spraying, are limited by the high technical skills and equipment costs required, and therefore are not always feasible for standard growers. ULV and aerial spraying may also be associated with wind drift issues, depending on weather conditions at the time of spraying, potentially releasing pest control agents into the environment. Therefore, there is a strong need to develop novel pest control formulations that are easy for growers and farmers to apply and demonstrate high levels of pest control efficacy while reducing environmental impact. Summary of the Invention

[0006] The inventors of this disclosure have discovered that when o-aminobenzamide, as the active ingredient, is formulated with a suitable combination of one or more dispersants and one or more enhancers, the formulation achieves the desired effect of uniform dispersion without the use of equipment, thereby freeing farmers from time-consuming and labor-intensive manual spraying. This document provides a novel composition (e.g., in tablet form) that disperses uniformly when directly applied, for example, to rice paddies, and achieves greater efficacy in pest control at recommended dosages.

[0007] In one aspect, the present disclosure provides a formulation comprising a composition, the composition comprising:

[0008] (a) a pesticidal active ingredient;

[0009] (b) an enhancer, wherein the enhancer comprises a dialkyl sulfosuccinate, a dodecyl sulfate, a dodecylbenzenesulfonate, a fatty alcohol derivative, an alkyl naphthalene sulfonate, or an alkyl naphthalene sulfate, or a mixture thereof;

[0010] (c) a dispersing agent, wherein the dispersing agent comprises a polycarboxylate, a phenolsulfonic acid condensate, a polyoxypropylene-polyoxyethylene block copolymer, or a naphthalene sulfonic acid condensate, or a mixture thereof;

[0011] (d) a binder; and

[0012] (e) optionally a filler.

[0013] In one aspect, the present disclosure provides a formulation comprising a composition, the composition comprising by weight based on the total weight of the composition:

[0014] (a) from about 0.1% to about 20% of a pesticidal active ingredient;

[0015] (b) from about 0.1% to about 5% of at least one enhancer, wherein the enhancer comprises a dialkyl sulfosuccinate, a dodecyl sulfate, a dodecylbenzenesulfonate, a fatty alcohol derivative, an alkyl naphthalene sulfonate, or an alkyl naphthalene sulfate, or a mixture thereof;

[0016] (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 naphthalene sulfonic acid condensate, or a mixture thereof;

[0017] (d) from about 0.1% to about 20% of at least one binder; and

[0018] (e) from about 0.1% to about 50% of at least one filler.

[0019] In certain embodiments, the composition is in the form of a tablet.

[0020] In certain embodiments, the pesticidal active ingredient is a herbicide or an 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.

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

[0022] In certain embodiments, the enhancer comprises sodium dialkylsulfosuccinate, sodium dodecyl sulfate, sodium dodecylbenzenesulfonate, fatty alcohol derivatives, sodium alkylnaphthalenesulfonate, sodium dioctylsulfosuccinate, or sodium alkylnaphthalenesulfonate, or mixtures thereof.

[0023] In one aspect, the present disclosure provides a tablet composition comprising, by weight based on the total weight of the composition:

[0024] (a) from about 0.1% to about 20% of a pesticidal active ingredient comprising one or more anthranilic acid amides;

[0025] (b) from about 0.1% to about 5% of at least one enhancer, wherein the enhancer comprises dialkylsulfosuccinates, dodecylsulfates, dodecylbenzenesulfonates, fatty alcohol derivatives, alkylnaphthalenesulfonates, or alkylnaphthalenesulfonates, or mixtures thereof;

[0026] (c) from about 0.1% to about 10% of at least one dispersing agent, wherein the dispersing agent comprises polycarboxylates, phenolsulfonic acid condensates, polyoxypropylene-polyoxyethylene block copolymers, or naphthalenesulfonic acid condensates, or mixtures thereof;

[0027] (d) from about 0.1% to about 20% of at least one binder; and

[0028] (e) from about 0.1% to about 50% of at least one filler.

[0029] In certain embodiments, the pesticidal active ingredient is a herbicide or an insecticide. In certain embodiments, the pesticidal active ingredient is a diamide, a neonicotinoid, or a nereistoxin analog insecticide, or mixtures thereof.

[0030] In certain embodiments, the component (a) comprises chlorantraniliprole, cyantraniliprole, tetraniliprole, cyclaniliprole, cyanthoate, tetraniliprole, thiamethoxam, clothianidin, thiacloprid, spinosad, or spinetoram, or mixtures thereof. In certain embodiments, the component (a) comprises chlorantraniliprole.

[0031] In certain embodiments, the 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%, from about 1%, from about 2.5%, or from about 5% by weight of the composition.

[0032] In certain embodiments, the enhancer comprises sodium dialkyl sulfosuccinate, sodium dodecyl sulfate, sodium dodecyl benzene sulfonate, fatty alcohol derivatives, sodium alkylnaphthalene sulfonate, sodium dioctyl sulfosuccinate, or sodium alkylnaphthalene sulfonate, or mixtures thereof. In certain embodiments, the enhancer comprises dioctyl sulfosuccinate.

[0033] In certain embodiments, the component (b) comprises SDS, OT-B, or OT-75, or mixtures thereof. In certain embodiments, the component (b) is a material selected from the group consisting of SDS, OT-B, and OT-75. In certain embodiments, the component (b) comprises Geropon SDS. In certain embodiments, the component (b) is SDS.

[0034] In certain embodiments, the component (b) is about 0.1% to about 4%, about 0.1% to about 3%, about 0.1% to about 2%, about 0.2% to about 2%, about 0.3% to about 2%, about 0.3% to about 1.8%, about 0.3% to about 1.5%, about 0.3% to about 1.2%, about 0.3% to about 1%, about 0.5% to about 1%, about 0.6% to about 1%, about 0.7% to about 1%, or about 0.8% by weight of the composition.

[0035] In certain embodiments, the component (c) comprises 2700, Atlox metasperse TM 550S, Ultrasperse, D-205, or T / 36, or mixtures thereof. In certain embodiments, the component (c) is a material selected from the group consisting of 2700, Atlox metasperse TM 550S, Ultrasperse, D-205, and T / 36. In certain embodiments, the component (c) comprises 2700. In certain embodiments, the component (c) is 2700.

[0036] In certain embodiments, the 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.

[0037] In certain embodiments, the composition further comprises component (f) about 0.1% to about 40% of at least one acid and / or (g) about 0.1% to about 40% of at least one base.

[0038] In certain embodiments, the component (f) comprises at least one species selected from the group consisting of citric acid, malonic acid ester, adipic acid, maleic acid, and D,L-tartaric acid. In certain embodiments, the component (f) comprises D,L-tartaric acid. In certain embodiments, the component (f) is D,L-tartaric acid.

[0039] In certain embodiments, the component (f) is about 0.5% to about 25%, about 1% to about 25%, about 5% to about 25%, about 10% to about 25%, about 15% to about 25%, about 16% to about 25%, about 17% to about 25%, about 18% to about 25%, about 19% to about 25%, about 20% to about 25%, about 20% to about 24%, about 20% to about 23%, about 20% to about 22%, or about 21% by weight of the composition.

[0040] In certain embodiments, the component (g) comprises at least one species selected from the group consisting of bicarbonate and carbonate. In certain embodiments, the component (g) comprises at least one species selected from the group consisting of sodium bicarbonate, potassium bicarbonate, sodium carbonate, and potassium carbonate. In certain embodiments, the component (g) comprises a mixture of sodium bicarbonate and sodium carbonate. In certain embodiments, the component (g) is a mixture of sodium bicarbonate and sodium carbonate.

[0041] In certain embodiments, the ratio of sodium bicarbonate and sodium carbonate, or the ratio of potassium bicarbonate and potassium carbonate, 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 by weight.

[0042] In certain embodiments, the component (g) comprises a mixture of sodium bicarbonate and sodium carbonate, wherein the sodium bicarbonate is 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 25% to about 35%, about 27% to about 33%, or about 30% by weight of the composition, and the 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.

[0043] In certain embodiments, the component (g) comprises a mixture of potassium bicarbonate and potassium carbonate, wherein the potassium bicarbonate is 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 25% to about 35%, about 27% to about 33%, or about 30% by weight of the composition, and the 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.

[0044] In certain embodiments, the component (g) is 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% by weight of the composition.

[0045] In certain embodiments, the 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 (zea mays) starch, modified cellulose, alginic acid, sodium carboxymethylcellulose, and copovidone. In certain embodiments, the component (d) comprises PEG. In certain embodiments, the component (d) is PEG. In certain embodiments, the PEG is one selected from the group consisting of PEG 2000, PEG 4000, PEG 6000, PEG 8000, and PEG 10000. In certain embodiments, the PEG is PEG 6000.

[0046] In certain embodiments, the 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% by weight of the composition.

[0047] In certain embodiments, the component (e) comprises at least one substance selected from the group consisting of lactose, lactose monohydrate, mannitol, sucrose, talc, maltodextrin, dextrin, maltitol, sorbitol, xylitol, powdered cellulose, cellulose gum, microcrystalline cellulose, starch, or calcium phosphate. In certain embodiments, the component (e) comprises talc, or maltodextrin, or a mixture thereof. In certain embodiments, the component (e) comprises a mixture of talc and maltodextrin. In certain embodiments, the component (e) comprises talc about 1% to about 15%, about 1% to about 10%, about 1% to about 8%, about 2% to about 8%, about 3% to about 8%, about 4% to about 8%, about 5% to about 8%, about 6% to about 8%, or about 6% by weight of the composition, and maltodextrin 1% to about 40%, 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 18% to about 30%, about 18% to about 27%, or about 20% to about 27% by weight of the composition.

[0048] In certain embodiments, the component (e) is about 0.5% to about 50%, about 1% to about 50%, about 5% to about 50%, about 10% to about 50%, about 15% to about 50%, about 20% to about 50%, about 20% to about 45%, about 20% to about 40%, about 20% to about 35%, about 25% to about 35%, about 26% to about 33%, about 26%, about 29%, or about 33% by weight of the composition.

[0049] In certain embodiments, the composition further comprises component (h) at least one lubricant about 0.1% to about 5% by weight of the composition.

[0050] In certain embodiments, the component (h) comprises at least one substance selected from the group consisting of white carbon, talc, magnesium stearate, calcium stearate, sodium stearate, zinc stearate, stearic acid, metallic 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 ester, sodium polyvinyl alcohol benzoate, sodium lauryl sulfate, sodium stearyl fumarate, polyethylene glycol, polypropylene glycol, and polyalkylene glycol. In certain embodiments, the component (h) comprises a stearate salt. In certain embodiments, the component (h) is a stearate salt. In certain embodiments, the component (h) comprises magnesium stearate. In certain embodiments, the component (h) is magnesium stearate.

[0051] In certain embodiments, the 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.

[0052] In certain embodiments, the composition further comprises component (i): at least one bittering agent in an amount of about 0.01% to about 5% by weight of the composition.

[0053] In certain embodiments, the component (i) comprises at least one substance selected from the group consisting of benzodiazepine, denatonium, sucrose octaacetate, quercetin, brucine, and picrolonic acid. In certain embodiments, the component (i) comprises denatonium benzoate.

[0054] In certain embodiments, the component (i) is 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%, about 0.1% by weight of the composition.

[0055] In certain embodiments, the composition further comprises component (j): at least one dispersing agent in an amount of about 0.1% to about 1.5% by weight of the composition.

[0056] In certain embodiments, the component (j) comprises at least one material selected from the group consisting of dysperse 131, polyfon H, disperse 132, and disperse 140. In certain embodiments, the component (i) comprises polyfon H.

[0057] In certain embodiments, the component (j) is 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 0.1% to about 0.5%, about 0.1% to about 0.4%, about 0.1% to about 0.3%, about 0.1% to about 0.2%, about 0.1% to about 0.1%, about 0.1% to about 0.5%, about 0.5%, about 1.0%, by weight of the composition.

[0058] In one aspect, the present disclosure provides a tablet composition comprising, by weight based on the total weight of the composition:

[0059] (a) about 0.1% to about 20% of chlorantraniliprole, or cyantraniliprole, or a mixture thereof;

[0060] (b) about 0.1% to about 5% of SDS;

[0061] (c) about 0.1% to about 10% of 2700;

[0062] (d) about 0.1% to about 20% of PEG-6000;

[0063] (e) about 0.1%-50% of a mixture comprising talc and maltodextrin;

[0064] (f) about 0.1%-40% of D,L-tartaric acid; and

[0065] (g) about 0.1% to about 40% of a mixture comprising sodium bicarbonate and sodium carbonate.

[0066] In one aspect, the present disclosure provides a tablet composition comprising, by weight based on the total weight of the composition:

[0067] (a) about 1%-5.5% of chlorantraniliprole, or cyantraniliprole, or a mixture thereof;

[0068] (b) about 0.5%-1.8% of SDS;

[0069] (c) about 1.5% - 3.5% of 2700;

[0070] (d) about 1% - 8% of PEG-6000;

[0071] (e) about 3% - 8% talc and about 20% - 30% maltodextrin;

[0072] (f) about 15% - 25% D,L-tartaric acid; and

[0073] (g) about 20% - 40% sodium bicarbonate and about 5% - 10% sodium carbonate.

[0074] 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 component (j): about 0.1% to about 1.5% by weight of the composition of at least one dispersant.

[0075] In one aspect, the present disclosure provides a tablet composition comprising by weight based on the total weight of the composition:

[0076] (a) about 1.05% of chlorantraniliprole;

[0077] (b) about 0.8% of SDS;

[0078] (c) about 2.5% of 2700;

[0079] (d) about 3.0% of PEG-6000;

[0080] (e) about 6.0% talc and about 27.1% maltodextrin;

[0081] (f) about 21% D,L-tartaric acid; and

[0082] (g) about 30% sodium bicarbonate and about 8% sodium carbonate.

[0083] 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): about 1.0% polyfon H.

[0084] In one aspect, the present disclosure provides a tablet composition comprising, by weight based on the total weight of the composition:

[0085] (a) about 2.6% chlorantraniliprole;

[0086] (b) about 0.8% SDS; SDS;

[0087] (c) about 2.5% Avicel® PHT 2700; 2700;

[0088] (d) about 5.5% PEG-6000;

[0089] (e) about 6.0% talc and about 22.85% maltodextrin;

[0090] (f) about 21% D,L-tartaric acid; and

[0091] (g) about 30% sodium bicarbonate and about 8% sodium carbonate.

[0092] 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 component (j): about 1.0% polyfon H.

[0093] In one aspect, the present disclosure provides a tablet composition comprising, by weight based on the total weight of the composition:

[0094] (a) about 5.1% chlorantraniliprole;

[0095] (b) about 0.8% SDS; SDS;

[0096] (c) about 2.5% Avicel® PHT 2700; 2700;

[0097] (d) about 5.5% PEG-6000;

[0098] (e) about 6.0% talc and about 20.35% maltodextrin;

[0099] (f) about 21% D,L-tartaric acid; and

[0100] (g) about 30% sodium bicarbonate and about 8% sodium carbonate.

[0101] 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 component (j) about 1.0% polyfon H.

[0102] In another aspect, the disclosure provides a method for controlling pests in a crop, the method comprising applying an agronomically effective amount of the formulation or composition provided herein to a crop or its environment in need thereof.

[0103] 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.

[0104] In certain embodiments, the single tablet of the 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).

[0105] 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 a rice field. BRIEF DESCRIPTION OF DRAWINGS

[0106] Figure 1 Sampling locations where active ingredient was collected for examination of tablet distribution profile are shown.

[0107] Figure 2 Content of active ingredient in sampling locations is shown.

[0108] Figure 3 Concentration of chlorantraniliprole absorbed in rice stem 3 days and 20 days after pesticide application is shown.

[0109] Figure 4 shows concentration of chlorantraniliprole absorbed in rice stem collected at different distances from application point. DETAILED DESCRIPTION

[0110] 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, a mixture, a process, a method, an article, or an apparatus that comprises a list of elements is not necessarily limited to only those elements but can include other elements not expressly listed or inherent to such composition, mixture, process, method, article, or apparatus. Further, unless expressly stated to the contrary, "or" refers to an inclusive or and not to an exclusive or. For example, a condition A or B is satisfied by any one of the following: A is true (or 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).

[0111] Also, use of "a" and "an" are employed to describe elements and components of the application. This is done merely for convenience and to give a general sense of the application. This description should be read to include one and / or at least one and the singular also includes the plural unless it is explicitly stated otherwise and vice versa.

[0112] When referring to ranges of values, it is to be understood that the entire range includes the endpoints. Also, it is to be understood that any numerical range recited is intended to include all values from the lower limit to the upper limit. For example, if a weight ratio range is stated as 1 :50, it is to be understood that values such as 2:40, 10:30, or 1 :3, are expressly enumerated in this specification. These are only examples of what is specifically anticipated herein, and all possible combinations of values between the lowest value and the highest value enumerated are to be considered to be expressly stated in this application in the numerical range fraction.

[0113] As used herein, the term "about" means plus or minus 10% of the value.

[0114] In one aspect, the present disclosure provides a formulation comprising a composition, the composition comprising: a pesticidal active ingredient; an enhancer, wherein the enhancer comprises a dialkyl sulfosuccinate, a dodecyl sulfate, a dodecylbenzene sulfonate, a fatty alcohol derivative, an alkyl naphthalene sulfonate, or an alkyl naphthalene sulfate, or a mixture thereof; a dispersant, wherein the dispersant comprises a polycarboxylate, a phenol sulfonic acid condensate, a polyoxypropylene-polyoxyethylene block copolymer, or a naphthalene sulfonic acid condensate, or a mixture thereof; a binder; and optionally a filler.

[0115] In another aspect, the present disclosure provides a formulation comprising a composition, the 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 dialkyl sulfosuccinate, a dodecyl sulfate, a dodecylbenzene sulfonate, a fatty alcohol derivative, an alkyl naphthalene sulfonate, or an alkyl naphthalene sulfate, or a mixture thereof; from about 0.1% to about 10% of at least one dispersant, wherein the dispersant comprises a polycarboxylate, a phenol sulfonic acid condensate, a polyoxypropylene-polyoxyethylene block copolymer, or a naphthalene sulfonic 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.

[0116] In another aspect, the present disclosure provides a tablet formulation, 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 dialkyl sulfosuccinate, a dodecyl sulfate, a dodecylbenzene sulfonate, a fatty alcohol derivative, an alkyl naphthalene sulfonate, or an alkyl naphthalene sulfate, or a mixture thereof; from about 0.1% to about 10% of at least one dispersant, wherein the dispersant comprises a polycarboxylate, a phenol sulfonic acid condensate, a polyoxypropylene-polyoxyethylene block copolymer, or a naphthalene sulfonic 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.

[0117] The use of unmanned aerial vehicles or drones (UAVs) in agricultural applications, such as with chemical products for field treatment, is rapidly expanding.

[0118] In one aspect of the invention, the compositions and formulations disclosed herein can be used for delivery by unmanned aerial vehicles or drones (UAVs).

[0119] The term "pesticidal active ingredient" as used herein encompasses those selected from the group consisting of herbicides, fungicides, bactericides, insecticides, nematicides, miticides, and growth regulators (including mixtures thereof).

[0120] Insecticides that can be used in the present application are: insecticides such as abamectin, acephate, acifluorfen, acetamiprid, acrinathrin, acynonapyr, 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]pyranopyran-4-yl]methyl cyclopropanecarboxylate), amidoflumet, amitraz, avermectin, azadirachtin, azinphos-methyl, benfuracarb, bensultap, benzpyrimoxan, bifenthrin, R-bifenthrin, bifenazate, bistrifluron, borate, broflanilide, buprofezin, cadusafos, carbaryl, carbofuran, cartap, chlordimeform, chlorfenapyr, chlorfluazuron, chloroprallethrin, chlorpyrifos, chlorpyrifos-e, chlorpyrifos-methyl, chromafenozide, clofentezine, chloroprallethrin, clothianidin, cyantraniliprol, (3-bromo-1-(3-chloro-2-pyridinyl)-N-[4-cyano-2-methyl-6-[(methylamino)carbonyl]phenyl]-1H-pyrazole-5-carboxamide), cyclaniliprole (3-bromo-N-[2-bromo-4-chloro-6-[[(1-cyclopropylethyl)amino]carbonyl]phenyl]-1-(3-chloro-2-pyridinyl)-1H-pyrazole-5-carboxamide), cycloprothrin, cycluron ((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, lambda-cyhalothrin, cypermethrin, zeta-cypermethrin, diacloden, dicofol, diazinon, diclometizole, dieldrin, diflubenzuron, dimehypo, dimethoate, dimpropyridaz, dinotefuran, diofenolan, emamectin, emamectin benzoate, endosulfan, esfenvalerate, ethiprole, etofenprox, epsilon-metofluthrin, etoxazole, fenbutatin oxide, fenitrothion, fenothiocarb, fenoxycarb, fenpropathrin, fenvalerate, fipronil, flumetover (2-ethyl-3,7-dimethyl-6-[4-(trifluoromethoxy)phenoxy]-4-quinolinylmethyl carbonate), flonicamid, fluazaindolizine, flubendiamide, flucythrinate, flufenerim, flufenoxuron, flufenoxystrobin ((alphaE)-2-[[2-chloro-4-(trifluoromethyl)phenoxy]methyl]-alpha-(methoxymethylidene)benzenepropanoic acid methyl ester), flumetsulam (5-chloro-2-[(3,4,4-trifluoro-3-buten-1-yl)sulfonyl]thiazole), fluazinam, fluazuron, flupiprole (1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-5-[(2-methyl-2-propen-1-yl)amino]-4-[(trifluoromethyl)sulfinyl]-1H-pyrazole-3-carbonitrile), flupyradifurone (4-[[(6-chloro-3-pyridinyl)methyl](2,2-difluoroethyl)amino]-2(5H)-furanone), flupyrimin, flupyroximate, flupyradifurone, fluxametamide, formothion, 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, hydramethylnone, imidacloprid, indoxacarb, insecticidal soap, isofenphos, isocycloseram, kappa-tefluthrin, lambda-cyhalothrin, lufenuron, malathion, meperfluthrin ([2,3,5,6-tetrafluoro-4-(methoxymethyl)phenyl]methyl (1R,3S)-3-(2,2-dichlorovinyl)-2,2-Dimethylcyclopropane carboxylate, cyfluthrin, metaldehyde, methamidophos, chlorpyrifos, thiophanate-methyl, methomyl, tebufenozide, methoxydimethalin, methoxybenzylfluthrin, ethoxyfenozide, epsilon-momfluorothrin, phosmet, [2,3,5,6-tetrafluoro-4-(methoxymethyl)phenyl]methyl 3-(2-cyano-1-propen-1-yl)-2,2-dimethylcyclopropane carboxylate, nicotine, acetamiprid, nitenpyram, flufenoxuron, polyfluorourea, chlorpyrifos, oxazosulfyl, parathion, methyl parathion, permethrin, phorate Phosphate, phosmet, phosmet, pirimicarb, profenofos, propargite, propargite, propargite, propargite, pyrethroid (1,3,5-trimethyl-N-(2-methyl-1-oxypropyl)-N-[3-(2-methylpropyl)-4-[2,2,2-trifluoro-1-methoxy-1-(trifluoromethyl)ethyl]phenyl]-1H-pyrazole-4-carboxamide), pymetrozine, pyridaben, pyrethroid, pyridaben, pyrimethanil, pyrimethanil, pyrimethanil ((αE)-2-[[[2-[(2,4-dichlorophenyl)amino]-6-(trifluoromethyl)-4-pyrimidinyl]oxy]methyl]-α-(methoxymethylene)phenylacetic acid methyl ester), pyrazole Pyriproxyfen, rotenone, lanyl alkaloid, flusilazole, ethyl spinosad, spinosad, spirodiclofen, spirodiclofen, methoxypiperidine ethyl ester, spirotetramat, thiophanate-methyl, flonicamid (N-[methyloxide[1-[6-(trifluoromethyl)-3-pyridyl]ethyl]-λ4-sulfinamide] cyanamide), tebufenozide, pyridaben, flufenoxuron, heptafluthrin, R-heptafluthrin, terbufos, tetrachlorantraniliprole, chlorpyrifos, pyrethroid, tetrafluoro-4-(methoxymethyl)phenyl]methyl2,2,3,3-tetramethylcyclohexane Propane carbamate), tetrazolium acetamiprid, thiamethoxam, thiamethoxam, thiamethoxam, thiamethoxam, thiazoxazine (3-phenyl-5-(2-thienyl)-1,2,4-oxadiazole), acetamiprid, tetrabromopyrethrin, pymetrozine, trichlorfon, trifluralin (2,4-dioxo-1-(5-pyrimidinylmethyl)-3-[3-(trifluoromethyl)phenyl]-2H-pyrido[1,2-a]pyrimidine inner salt), chlorfenapyr, tyclopyrazoflor, zeta-cypermethrin, Bacillus thuringiensis δ-endotoxin, entomopathogenic bacteria, entomopathogenic viruses, or entomopathogenic fungi.

[0121] Herbicides that can be used in the present application are: herbicides selected from the group consisting of (bl) photosystem II inhibitors, (b2) acetyl hydroxy acid synthase (AHAS) inhibitors, (b3) acetyl CoA carboxylase (ACCase) inhibitors, (b4) auxin mimics, (b5) 5-enolpyruvyl-shikimate-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, (blO) auxin transport inhibitors, (bl l) phytoene desaturase (PDS) inhibitors, (bl2) 4-hydroxyphenyl-pyruvate-dioxygenase (HPPD) inhibitors, (bl3) homogentisate solalytransferase (HST) inhibitors, (bl4) cellulose biosynthesis inhibitors, (bl5) other herbicides including mitotic disrupters, organic arsenical compounds, asulam, bromobutide, cinmethylin, dichloroacetate, dymron, flurenol, indanofan, molexan, monofluron, oligosacchararyl, oxaziclomefone, perfluidone, phthal avicin A, pyribencarb, triapentaphos, and (bl6) herbicide safeners; and salts of the compounds of (bl) to (bl6).

[0122] "Photosystem II inhibitors (bl)" are chemical compounds that bind to the Dl protein at the QB binding site and thus block the transfer of electrons from QA to QB in the chloroplast thylakoid membrane. The electrons blocked from passing through photosystem II are diverted through a series of reactions to form toxic compounds that destroy cell membranes and cause chloroplast swelling, membrane leakage, and ultimately cell rupture. The QB binding site has three different binding sites: binding site A binds triazines such as atrazine, triazinones such as hexazinone, and uracils such as terbucarb, binding site B binds phenylureas such as diuron, and binding site C binds benzothiadiazoles such as bentazon, nitriles such as bromoxynil, and phenylpyridazines such as pyridafol. Examples of photosystem II inhibitors include amitrol, amicarbazone, atrazine, bentazon, bromofenoxim, bromobutide, chloreturon, chlorotoluron, chloroxuron, diuron, dymron, endothall, fluometuron, isoproturon, linuron, methazole, methoxone, monuron, naproanilide, neburon, oxaziclomefone, phenisopham, siduron, sulfallat, terbumeton, terbumoxon, terbucarb, terbutol, terbutryn, terbumeton, terbutylazine, tertrazine, thiazafluron, triadimefon, triaziflan, triazin, triazoxide, and xylylcarb.

[0123] AHAS inhibitors (b2) are chemical compounds that inhibit acetohydroxy acid synthase (AHAS), also known as acetolactate synthase (ALS), and thus kill plants by inhibiting 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, bensulfuron-sodium, chlorimuron-ethyl, chlorsulfuron, cinmethylin, cyclosulfamuron, double metal cyanide, flazasulfuron, flupyrsulfuron, flupyrsulfuron-sodium, foramsulfuron, halosulfuron-methyl, imazamox, imazamethapyr, imazapic, imazapyr, imazethapyr, imazosulfuron, iodosulfuron, iodosulfuron-methyl-sodium, iofensulfuron, mesosulfuron, metazachlor, metosulam, metsulfuron-methyl, nicosulfuron, oxasulfuron, penoxsulam, prosulfuron, propyrisulfuron, pyrimisulfan, pyribenzoxim, pyriftalid, pyrimethanil, pyrithiobac, pyroxasulfone, rimsulfuron, sulfometuron-methyl, sulfosulfuron, thiazopyr, thifensulfuron-methyl, trifloxysulfuron, triflusulfuron-methyl, and tritosulfuron.

[0124] “ACCase inhibitors (b3)” are chemical compounds that inhibit acetyl-Coenzyme A carboxylase, the enzyme responsible for catalyzing an early step in the synthesis of lipids and fatty acids in plants. Lipids are the major component of cell membranes, and without lipids, new cells cannot be produced. Inhibition of acetyl-Coenzyme A carboxylase and the subsequent lack of lipid production results in loss of cell membrane integrity, especially in actively growing areas such as the meristem. Ultimately, seedling and rhizome growth stops, and the seedling meristem and rhizome buds begin to die. Examples of ACCase inhibitors include alloxydim, butroxydim, clethodim, cloproxydim, cycloxydim, haloxyfop, fluazifop, fenoxaprop, pinoxaden, fluazifop-P, haloxyfop-P, propaquizafop, profoxydim, quizalofop, sethoxydim, tralkoxydim, including resolved forms such as fenoxaprop-P, fluazifop-P, haloxyfop-P, and quizalofop-P, and ester forms like cloproxydim, haloxyfop, fluazifop, and fenoxaprop-P.

[0125] Auxins are plant hormones that regulate the growth of many plant tissues. “Auxin mimics (b4)” are compounds that mimic the plant growth hormone auxin, thus causing uncontrolled and disorganized growth, leading to death of the plant in susceptible species. Examples of auxin mimics include clopyralid (3- chloro-2,6-dihydroxy-pyridine), picloram, triclopyr, aminopyralid, cloquintocet, dichlorprop, 2,4-D, 2,4-DB, dichlorprop-P, fluroxypyr, halauxifen (4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)-2-pyridinecarboxylic acid), halauxifen-methyl (4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)-2-pyridinecarboxylic acid methyl ester), MCPA, MCPB, mecoprop, picloram, quinclorac, 2,3,6-TBA, triclopyr, and 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)-5-fluoro-2-pyridinecarboxylic acid methyl ester.

[0126] “EPSP synthase inhibitors (b5)” are chemical compounds that inhibit the enzyme 5-enolpyruvyl-shikimate-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 the plant leaf and translocated in the phloem to the growing point. Glyphosate is a relatively nonselective post-emergence herbicide belonging to this group. Glyphosate includes esters and salts such as the ammonium, isopropylammonium, potassium, sodium (including sesquisodium), and trimethylsulfonium salts (alternatively known as sulfosate).

[0127] "Photosystem I electron diverters (b6)" are compounds that receive electrons from photosystem I and generate hydroxyl radicals after several cycles. These radicals are highly reactive and readily destroy unsaturated lipids, including membrane fatty acids and chlorophyll. This disrupts cell membrane integrity, causing cells and organelles to "leak," leading to rapid leaf wilting and drying, and ultimately plant death. Examples of this second type of photosynthesis inhibitor include diquat and paraquat.

[0128] "PPO inhibitors (b7)" are compounds that inhibit the enzyme protoporphyrinogen oxidase, which rapidly leads to the formation of highly reactive compounds in plants that damage cell membranes, resulting in cell sap leakage. Examples of PPO inhibitors include trifluralin sodium, pyrazosulfuron, pyrazosulfuron, methoxyfenozide, flufenoxuron, trifluralin, methoxyfenozide, indole-methyl, isopyrazosulfuron, flupyridaben, flumetsulam, propyzoxystrobin, ethoxysulfuron, flufenoxuron, flufenoxuron, flufenoxuron, halosafen, quizalofop-P-ethyl, propyzoxystrobin, oxadiazon, ethoxysulfuron, cyclopentoxuron, flupyrazosulfuron, pyrazosulfuron, pyrazosulfuron, mesotrione, thiamethoxam, trifluralin. dimoxazin (dihydro-1,5-dimethyl-6-thio-3-[2,2,7-trifluoro-3,4-dihydro-3-oxo-4-(2-propyn-1-yl)-2H-1,4-benzoxazin-6-yl]-1,3,5-triazin-2,4(1H,3H)-dione) and flupyrazosulfuron (N-[2-[[2-chloro-5-[3,6-dihydro-3-methyl-2,6-dioxo-4-(trifluoromethyl)-1(2H)-pyrimidinyl]-4-fluorophenyl]thio]-1-oxopropyl]-β-alanine methyl ester).

[0129] "GS inhibitors (b8)" are compounds that inhibit the activity of glutamine synthase, an enzyme used by plants to convert ammonia into glutamine. As a result, ammonia accumulates and glutamine levels decrease. Plant damage may occur due to the combined effects of ammonia toxicity and the lack of amino acids required for other metabolic processes. GS inhibitors include glufosinate and its esters and salts, such as glufosinate and other glufosinate derivatives, glufosinate P ((2S)-2-amino-4-(hydroxymethylphosphono)butyric acid), and bilanaphos.

[0130] “VLCFA elongase inhibitors (b9)” are herbicides with various chemical structures that inhibit elongase enzymes. Elongase enzymes are one of the enzymes located in or near the chloroplast that are involved in the biosynthesis of VLCFAs. In plants, very long chain fatty acids are the main constituents of hydrophobic polymers that prevent drying at the leaf surface and provide stability to pollen grains. Such herbicides include acetochlor, alachlor, anilofos, butachlor, cafenstrole, dimethachlor, dimethenamid, dimethenamid-P, fenoxasulfone (3-[[(2,5-dichloro-4-ethoxyphenyl)methyl]sulfonyl]-4,5-dihydro-5,5-dimethylisoxazole), flupoxam, fluorotolan, mefenstrole, metazachlor, metobenzuron, metosulam, metoxuron, napropamide, napropamide-M ((2R)-N,N-diethyl-2-(l-naphthyloxy)propanamide), pethoxamid, pyrazolynate, propachlor, pronamid, propisochlor, pyroxasulfone, and thenylchlor, including resolved forms such as pure isomethiochlor and chloro- and oxy-acetamides.

[0131] “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, naphtalamic acid (also known as N-(l-naphthyl)-phthalamic acid and 2-[(l-naphthylamino)carbonyl]benzoic acid).

[0132] “PDS inhibitors (b11)” are compounds that inhibit the carotenoid biosynthetic pathway at the phytoene desaturase step. Examples of PDS inhibitors include m-fluorobutyroldin, fluridone, diflufenican, fluridone, fluridol, furilazole, norflurzon, and picolinafen.

[0133] "HPPD inhibitors (b12)" are chemicals that inhibit the biosynthesis of 4-hydroxyphenyl-pyruvate dioxygenase. Examples of HPPD inhibitors include bicyclopyrone, pyrazolynate, pyrazoxyfen (4-hydroxy-3-[[2-[(2-methoxyethoxy)methyl]-6-(trifluoromethyl)-3-pyridinyl]carbonyl]bicyclo[3.2.1]oct-3-en-2-one), fenquinotrione (2-[[8-chloro-3,4-dihydro-4-(4-methoxyphenyl)-3-oxo-2-quinoxalinyl]carbonyl]-1,3-cyclohexanedione), isoxachlortole, isoxaflutole, mesotrione, sulcotrione, pyrazolate, benzofluor, sulfentrazone, tefuryltrione, oxadiargyl, tolpyralate (1-[[1-ethyl-4-[3-(2-methoxyethoxy)-2-methyl-4-(methylsulfonyl)benzoyl]-1H-pyrazol-5-yl]oxy]ethyl methyl carbonate), benzoic acid (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.

[0134] "HST inhibitors (b13)" disrupt the ability of plants to convert homogentisic acid to 2-methyl-6-tigloyl-1,4-benzoquinone, thereby disrupting carotenoid biosynthesis. Examples of HST inhibitors include fluridone, norflurazon, 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.

[0135] HST inhibitors also include compounds of Formula A and B.

[0136]

[0137] Where R d1 It is H, Cl, or CF3; R d2 It is H, Cl, or Br; R d3 It is H or Cl; R d4 It is H, Cl, or CF3; R d5 It is CH3, CH2CH3, or CH2CHF2; and R d6 It is OH, or -OC(=O)-i-Pr; and R e1 It is H, F, Cl, CH3 or CH2CH3; R e2 It is H or CF3; R e3 It is H, CH3, or CH2CH3; R e4 It is H, F, or Br; R e5 It is Cl, CH3, CF3, OCF3, or CH2CH3; R e6 It is H, CH3, CH2CHF2 or C≡CH; R e7 It is OH, -OC(=O)Et, -OC(=O)-i-Pr or -OC(=O)-t-Bu; and A e8 It is N or CH.

[0138] Cellulose biosynthesis inhibitors (b14) inhibit cellulose biosynthesis in certain plants. They are most effective when applied to young or rapidly growing plants before or early after emergence. Examples of cellulose biosynthesis inhibitors include glyphosate, chlorpyrifos, flumetsulam, indomethacin (N2-[(1R,2S)-2,3-dihydro-2,6-dimethyl-1H-indo-1-yl]-6-(1-fluoroethyl)-1,3,5-triazine-2,4-diamine), isoxaflutole, and triazine-flumetsulam.

[0139] “Other herbicides (b15)” include herbicides that act through a variety of different modes of action, such as mitotic disrupters (e.g., high efficacy dichlorprop-methyl and high efficacy dichlorprop-isopropyl), organic arsenical compounds (e.g., DSMA and MSMA), 7,8-dihydrofolate synthetase inhibitors, chloroplast isoprenoid synthesis inhibitors, and cell wall biosynthesis inhibitors. Other herbicides include those with unknown modes of action or that do not fall into the specific classes listed under (b1) through (b14) or that act through a combination of the modes of action listed above. Examples of other herbicides include benoxacor, bensulfuron-methyl, bifenox, bixlozone, bromobutide, cinmethylin, clomazone, dichlorbenzuron, cyclopyrimorate (6-chloro-3-(2-cyclopropyl-6-methylphenoxy)-4-pyridazinyl 4-morpholinecarboxylate), daimuron, difenzoquat, etofenprox, fenclorim, flamprop-methyl, flamprop-isopropyl, flurenol, isoxaben, mefenpyr-diethyl, metamifop, metam-sodium, monuron, triazifentyl (1-(2,4-dichlorophenyl)-N-(2,4-difluorophenyl)-1,5-dihydro-N-(1-methylethyl)-5-oxo-4H-1,2,4-triazole-4-carboxamide), metamifop-P, oil of meritate, oxaziclomefone, pelargonic acid, pyributicarb, and 5-[[(2,6-difluorophenyl)methoxy]methyl]-4,5-dihydro-5-methyl-3-(3-methyl-2-thienyl)isoxazole, and tetflupyrolimet.

[0140] Fungicides which can be used in the present application are: fungicides such as acibenzolar-S-methyl, ametoctradin, amisyn, anilazim, azoxystrobin, benalaxyl, benodanil, benomyl, benthiavalicarb, bethoxazin, bixpyrazine, blasticidin-S, boscalid, bromocyclen, bronopol, bupirimate, captafol, captan, carbendazim, carpropamid, carvaxym, chloroneb, chlorothalonil, chlozolinate, copper hydroxide, copper oxychloride, copper sulfate, coumoxystrobin, cyazofamid, cyflufenamid, cymoxanil, cyprosifad, cyprodinil, dichlobentiazox, diclomezine, diclocymet, diclomezine, dicloran, diethofencarb, dimetan, dimethirimol, dimethomorph, dimoxystrobin, diniconazole, dinocap, dipymetitrone, dithianon, dodine, dodemorph, edifenphos, emtine, enoxastrobin, epoxiconazole, etaconazole, etacelasil, ethaboxam, ethoxyquin, etridiazole, famoxadone, fenamidone, fenarimol, fenhexamid, fenoxasulfone, fenpiclonil, fenpropidin, fenpropimorph, fenpropidine, fenpyrazamine, ferimzone, ferbam, flusilazole, flutriafol, fluquinconazole, flutriafol, fludioxonil, flumetover, flumorph, fluopicolide, fluoroimid, fluoxasulfam, fluquinconazole, flusulfamide, folpet, formaldehyde, fthalin, furalaxyl, furophanate, guazatine, hexachlorend, hymexazol, iminoctad, iprobenfen, iprodione, iprovalicarb, isoprothiolane, isopyrazam, kasugamycin, kresoxim-methyl, mancopper, maneb, mepronil, metiram, metrafenone, metyl-(E)-cyclopropanecarboximidate, metyl-(Z)-cyclopropanecarboximidate, milneb, myclobutanil, nabam, nitrophenide, nuarimol, ofurace, orysastrobin, oxolinic acid, pefurazoate, pentachlorophenol, penthiopyrad, phenazine, phenamacril, phenisopham, phenylmercury sulfate, phthalide, picarbutrazox, piperalin, polycarbamate, polyoxin, probenazole, proquinazid, propamocarb, propiconazole, propineb, propomocarb hydrochloride, proquinazid, pyracarbolid, pyrametostrobin, pyrametostrobin, pyramethanil, pyridinitr, pyrimethanil, pyroxyfur, quaternary ammonium compounds, quinomethionate, quinoxyfen, quintozene, spiroxamine, sulfur, sulfuric acid, tebufloquin, tebufloquin, tebufenpyrad, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloftalam, tecloAlso known as enestroburin), epoxiconazole, ethaboxam, ethirimol, etridiazole, famoxadone, fenamidone, fenaminstrobin, fenarimol, fenbuconazole, fenhexamid, fenoxanil, fenpicolnil, fenpropidin, fenpropimorph, fenpyrazamine, fentin acetate, fentin hydroxide, ferbam, ferimzone, flutolanil, florylpicoxamid, fluazamam, fluazinam, flubeneteram, fludioxonil, flufenzine, fluindapyr, flumorph, fluopicolide, fluopyram, fluoxapiprolin, fluquinconazole, flusilazole, flusulfamide, fluotrimazole, flutolanil, flutriafol, folpet, fluxapyroxad, fthalide,Also known as phthalide, furaxyl, furapyramide, hexaconazole, hymexazole, guazatine, imidazolium, iminoctadine albesilate, iminoctadine triacetate, inpyrfluxam, thiodicarb, tebuconazole, ipfentrifluconazole, ipflufenoquin, isopyrazam, iprobenfos, iprofen, propineb, isoflurane, isopyran, isopycyram, isopyroxil, isopyrazam, isopyrazin, kasugamycin, azoxystrobin, lancotrione, mancozeb, and dimethomorph. ndipropamid), mandestrobin, mancozeb, mapanipyrin, chlorfluazuron, methamidophos, meptyldinocap, metalaxyl-M (including mefenoxam), tebuconazole, methasulfuron-methyl, mancozeb, benomyl, metyltetraprole, cyproconazole, naftitine, ferric methylarsinate Methanearsonate), flufenoxuron, octazol, furazolidone, oxadixyl, oxathiapiprolin, oxopropyl acid, oxpoconazole, oxytetracycline, tebuconazole, pencycuron, fluopyram, penthiophanate, perfurazoate, phosphorous acid (including its salts, e.g., fosetyl-aluminum), azoxystrobin, piperalin, polyoxin, thiabendazole, imazalil, procymidone, propamocarb, propiconazole, zinc methyl thiophanate, proquinazid, prothiocarb, prothioconazole, fluopyram, azoxystrobin, pyraclostrobin, pyrapropoyne, pyraoxystrobin, pyraziflumid, pyrazophos, pyribencarb, pyributacarb, pyridachlometyl, pyrifenox, pyriofenone, perisoxazole, pyrimethanil, pyrifenox, pyrolnitrin, pyroquilon, quinofumelin, quinomethionate, quinoxylen, quintozene, silthiofam, sedaxane, simeconazole, spiroxamine, streptomycin, sulfur, tebuconazole, tecloftalam, tecloftalam, tecnazene, terbinafine, tetraconazole, thifluzamide, tolclofos-methyl, tolclofos-methyl, thiram, tiadinil, toclofos-methyl, tolylfluanid, trifloxystrobin, triforine, triflumizole, triticonazole, valifenalate, vinclozoline, zineb, ziram, zoxamide and 1-[4-[4-[5-(2,6-difluorophenyl)-4,5-dihydro-3-isoxazolyl]-2-thiazolyl]-1-piperidinyl]-2-[5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]ethanone; nematicides such as fluopyram, ethaboxam, fosthiazate, abamectin, ipconazole, dinocap-p, dimethyldithiocarbamate, thiabendazole, 1,3-dichloropropene (1,3-D), metam (sodium and potassium), dazomet, chloropicrin, fenamiphos, ethoprop, cadusaphos, terbufos, imicyafos, oxamyl, carbofuran, tioxazafen, bacillus firmus and pasteuria zeaxanthinifida; bactericides such as streptomycin;Miticides such as amitraz, binxadiazol, clofentezine, cyhexatin, dicofen, diafenthiuron, etoxazole, fenazaquin, fenbutatin oxide, fenpropathrin, fenpyroximate, hexythidazole, propargite, pyridaben, and tebufenpyrad.

[0141] In certain embodiments, the pesticidal active ingredient is an insecticide.

[0142] The term "insecticide" as used herein encompasses all agents having a controlling or altering effect on the growth of insects, including but not limited to killing, injuring, retarding, impeding growth, directional impairment, inhibiting reproduction, and the like.

[0143] In certain embodiments, the pesticidal active ingredient is a diamide, neonicotinoid, or nereistoxin analog insecticide, or mixtures thereof. In some embodiments, the pesticidal active ingredient is chlorantraniliprole, cyantraniliprole, tetraniliprole, cyclaniliprole, cyantraniliprole, tetraniliprole, broflanilide, dichlorantraniliprole, thiamethoxam, clothianidin, thiacloprid, spinosad, or spinetoram, or mixtures thereof.

[0144] In certain embodiments, the pesticidal active ingredient is an anthranilamide.

[0145] The term "anthranilamide" as used herein refers to a carboxamide class of arthropodicides having insecticidal activity against a number of economically important agricultural and non-agricultural invertebrate pests. Anthranilamides affect calcium homeostasis by binding to ryanodine receptors, a class of intracellular calcium ion channels. Upon binding, the calcium ion channels open and release calcium ions into the cytoplasm. The reduction in calcium ion stores results in paralysis and death of the insect. Anthranilamides are chemically characterized by a molecular structure containing adjacent carboxamide substituents bonded to carbon atoms of an aromatic ring, typically a benzene ring, wherein one carboxamide moiety is bonded through the carbonyl carbon and the other carboxamide moiety is bonded through the nitrogen atom.

[0146] In some embodiments, the anthranilamide is selected from the group consisting of compounds of Formula I, N-oxides, and salts thereof

[0147]

[0148] wherein X is N, CF, CCl, CBr, or CI; R 1 is H, CH3, CI, Br, or F; R 2 is H, F, CI, Br, or -CN; R 3 is F, CI, Br, C1-C4 haloalkyl, or C1-C4 haloalkoxy; R 4ais H, C1-C4 alkyl, cyclopropylmethyl or 1-cyclopropylethyl; R 4b is H or CH3; R 5 is H, F, Cl or Br; and R 6 is H, F, Cl or Br.

[0149] In some embodiments, the anthranilamide is chlorantraniliprole, cyantraniliprole, tetraniliprole, cyclaniliprole, sulfoxaflor, broflanvalerate, dicloranvilpride, or tetraniliprole, or mixtures thereof. Other anthranilamides and methods for their preparation are described in detail in U.S. Patent No. 6,747,047, WO 2003 / 015519, WO 2004 / 067528, WO 2006 / 062978, and WO 2008 / 069990, which are incorporated herein by reference.

[0150] In some embodiments, the anthranilamide is chlorantraniliprole, or cyantraniliprole, or mixtures thereof.

[0151] Chlorantraniliprole is an anthranilic diamide class of insecticide and has the chemical name 5-bromo-N-[4-chloro-2-methyl-6-(methylcarbamoyl)phenyl]-2-(3-chloropyridin-2- yl)pyrazole-3-carboxamide, and is registered under the trademark Coromex® by FMC Corporation Chlorantraniliprole is a ryanodine receptor agonist and is used to protect a variety of crops, including corn, cotton, grapes, rice, and potatoes. Insects exposed to chlorantraniliprole generally exhibit lethargy and muscle paralysis followed by eventual death. Findings indicate that chlorantraniliprole exhibits a high degree of selectivity for the insect ryanodine receptor over the mammalian ryanodine receptor. This selectivity is likely a major contributor to the mammalian safety observed using chlorantraniliprole.

[0152] 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 under the trademark Cyazypyr® by FMC Corporation Cyantraniliprole is a carboxamide that is chlorantraniliprole with the chloro atom attached to the phenyl ring replaced by a cyano group. Cyantraniliprole can be used as an insecticide to control whiteflies, thrips, aphids, fruit flies, and fruit worms in crops such as onions, potatoes, and tomatoes. It acts as a ryanodine receptor agonist.

[0153] In certain embodiments, the compositions provided herein comprise 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%, by weight of the composition, of an anthranilamide. In certain embodiments, the anthranilamide is chlorantraniliprole.

[0154] Since the efficacy and chemical stability of the active ingredient and the physical stability of the formulated composition can be influenced by the inert ingredients in the formulation, suitable inert ingredients should not cause decomposition of the active ingredient, not cause a substantial reduction in its activity at the time of application, or cause appreciable precipitation or crystal formation on long-term storage. In addition, the inert ingredients should be non-phytotoxic and safe for the environment. In certain formulations, the inert ingredients can even enhance the biological performance of the active ingredient by facilitating penetration or uptake into the plant or arthropod pest or by increasing tolerance to wash-off.

[0155] In certain embodiments, the enhancer comprises sodium dialkylsulfosuccinate, sodium dodecyl sulfate, sodium dodecylbenzenesulfonate, fatty alcohol derivatives, sodium alkylnaphthalenesulfonate, sodium dioctylsulfosuccinate, or sodium alkylnaphthalenesulfonate, or mixtures thereof.

[0156] In certain embodiments, the enhancer comprises SDS, MA-80I, OT series, MULTIWET TM MO-85P, EFW, BEROL TM 790A, DS 10, DF-90, Tergitol TM W-610, L WET F, L WET P, 1004, 1010, AA, IP, WP, or HRB, or mixtures thereof.

[0157] In certain embodiments, the compositions provided herein comprise about 0.1% to about 5%, by total weight, of at least one enhancer comprising sodium dialkylsulfosuccinate.

[0158] As used herein, the term "enhancer comprising sodium dialkylsulfosuccinate" means any enhancer containing sodium dialkylsulfosuccinate and optionally one or more other substances, whether sodium dialkylsulfosuccinate is the primary component of the enhancer or not, so long as the enhancer can facilitate the effective uptake of the active ingredient by the crop or pasture to a level effective to control the pest. In certain embodiments, sodium dialkylsulfosuccinate is the primary component of the enhancer. In certain embodiments, the enhancer comprises greater than about 50%, 55%, 60%, 65%, 70%, 75%, 80%, 85%, 90%, 95%, or 98% by weight of sodium dialkylsulfosuccinate. In certain embodiments, the enhancer is in solid form after mixing with other components of the composition. In certain embodiments, the enhancer is in solid form before mixing with any component of the composition.

[0159] Suitable enhancers comprising sodium dialkylsulfosuccinate are known and include, but are not limited to SDS, MA-80I, OT series, MULTIWET TM MO-85P, and EFW.

[0160] In certain embodiments, the enhancer is SDS. SDS is a low use rate, high performance wetting agent for dry formulations.

[0161] In certain embodiments, the enhancer is OT-B or OT-75. OT-B and OT-75 are multipurpose anionic surfactants (such as wetting agents, emulsifiers, antistatic / softening agents) which can be used to reduce surface tension as well as to increase absorbency and penetration and can provide very fast migration at interfaces.

[0162] In certain embodiments, the enhancer is about 0.1% to about 4%, about 0.1% to about 3%, about 0.1% to about 2%, about 0.2% to about 2%, about 0.3% to about 2%, about 0.3% to about 1.8%, about 0.3% to about 1.5%, about 0.3% to about 1.2%, about 0.3% to about 1%, about 0.5% to about 1%, about 0.6% to about 1%, about 0.7% to about 1%, or about 0.8% by weight of the composition.

[0163] In certain embodiments, the dispersant comprises T / 36, TA-72, SC-213, Ultrasperse D-205 D-305 D-518 2500 2700, Atlox metasperse TM 550S, Tamol TM 731 SD, Tamol TM DN, YUS-TXC, PE 10400, MORWET TM D-360, MORWET TM D-110 D-425, Tamol TM FB P1, or Tamol TM NN8906.

[0164] In some embodiments, the compositions disclosed herein comprise about 0.1% to about 10% by weight of at least one polycarboxylate-containing dispersant.

[0165] As used herein, the term "dispersant containing a polycarboxylate" refers to any dispersant containing a polycarboxylate and optionally one or more other substances, whether or not the polycarboxylate is the major component of the dispersant, as long as the dispersant can promote the diffusion and uniform distribution of the active ingredient in a liquid. In some embodiments, the polycarboxylate is the major component of the dispersant. In some embodiments, the dispersant comprises more than about 50%, 55%, 60%, 65%, 70%, 75%, 80%, 85%, 90%, 95%, or 98% polycarboxylate by weight. In some embodiments, the dispersant is in solid form after being mixed with other components of the composition. In some embodiments, the dispersant is in solid form before being mixed with any component of the composition.

[0166] The dispersants used in this article can promote the diffusion and uniform distribution of the active ingredients in liquids such as cold, hard water (e.g., containing more than about 300 ppm of calcium carbonate, to which the composition is applied, especially when the composition is not uniformly dispersed).

[0167] Suitable dispersants containing polycarboxylate salts are known, and include, but are not limited to, those containing polycarboxylate salts. T / 36, TA-72 SC-213 Ultrasperse D-205 D-305 D-518 2500、 2700, Atlox metasperse TM 550S, and Tamol TM 731SD.

[0168] In certain embodiments, the dispersant is 2700. 2700 is an acid resin copolymer based dispersant (surfactant) primarily developed for use in water dispersible granule formulations.

[0169] In certain embodiments, the dispersant is T / 36. T / 36 is a multipurpose sodium polycarboxylate, which is a very high performance dispersing, compatibilizing, chelating agent.

[0170] In certain embodiments, the dispersant is D-205.

[0171] In certain embodiments, the dispersant 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.

[0172] In certain embodiments, the enhancer is SDS, and the dispersant is 2700. In certain embodiments, the enhancer is OT-B, and the dispersant is D-205. In certain embodiments, the enhancer is OT-75, and the dispersant is T / 36.

[0173] The preferred ranges of enhancer and dispersant can improve the efficacy of the tablet composition containing chlorantraniliprole in terms of diffusion or permeability. In certain embodiments, the ratio between the enhancer and the dispersant can be in the range of about 1 : 1-1 :5, 1 : 1-1 :4, 1 :2-1 :4, or 1 :3-1 :4 by weight. In certain embodiments, the ratio is about 8:25 by weight. In certain embodiments, the ratio is about 1 :3 by weight.

[0174] 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 base.

[0175] The acids and bases used herein generally act in concert 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 capable of reacting with the carbonate component of the composition to release carbon dioxide. The acid can be a water-soluble acidic material, especially a polyprotic organic acid such as succinic acid, D,L-tartaric acid, L-tartaric acid, tartaric acid, alkali metal acid sulfates, lactic acid, adipic acid, citric acid, alkali metal acid citrates, alkali metal acid phosphates, alkali metal acid phthalates, and p-toluene sulfonic acid, malic acid, maleic acid, malonic acid, and oxalic acid, among others. In certain embodiments, the acid is D,L-tartaric acid.

[0176] In certain embodiments, the compositions provided herein comprise 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 from about 21% of the acid by weight of the composition.

[0177] The base is an inorganic base that reacts with the acid to provide a source of carbon dioxide. Of these salts, the sodium and potassium salts are preferred due to their good solubility and low cost. The base can be an alkali or alkaline earth metal carbonate such as sodium carbonate, potassium carbonate, sodium bicarbonate, potassium bicarbonate, calcium carbonate, and calcium bicarbonate.

[0178] In certain embodiments, the compositions provided herein comprise 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 from about 38% of the base by weight of the composition.

[0179] In certain embodiments, the base is a mixture of bicarbonate and carbonate salts, for example, a mixture of sodium bicarbonate and sodium carbonate, or potassium bicarbonate and potassium carbonate. The ratio between the bicarbonate and carbonate salts, 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.

[0180] In certain embodiments, the bicarbonate and carbonate salts are sodium bicarbonate and sodium carbonate, respectively, wherein the sodium bicarbonate is 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 25% to about 35%, about 27% to about 33%, about 30%, by weight of the composition, and the 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 salts are potassium bicarbonate and potassium carbonate, respectively, wherein the potassium bicarbonate is 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 25% to about 35%, about 27% to about 33%, about 30%, by weight of the composition, and the 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.

[0181] The ratio of bicarbonate and / or carbonate salt to acid can vary within wide limits. For example, the compositions described herein can contain from 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 salt.

[0182] The term "equivalent" is used herein in the acid-base sense, 1 gram molecular weight of solid acid is considered as the equivalent of 1 gram molecular weight of NaHC03, or 0.5 gram molecular weight of Na2C03. However, lesser amounts can be used, and these amounts are not critical. For each equivalent of bicarbonate, more than about 0.05 equivalent of acid is needed. That is, when the alkali metal carbonate is bicarbonate, any amount of acid in excess of 0.05 equivalent per equivalent of bicarbonate is sufficient to cause the composition to effervesce somewhat.

[0183] The compositions disclosed herein comprise 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 by total weight. The binder binds the different components of the composition together to assist with the integrity of the composition and to reduce the generation of powder during manufacture, 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 (zea mays) starch, modified cellulose, alginic acid, hydroxyl sodium methylcellulose, 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 PEG 200, PEG 1000, PEG 2000, PEG 4000, PEG 6000, PEG 8000, and PEG 10000. In certain embodiments, the binder comprises PEG 6000.

[0184] The compositions disclosed herein comprise 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 by total weight.

[0185] As used herein, the term "filler" refers to a substance added to a composition to increase the weight and / or size of the composition. Several suitable fillers are known and include, but are not limited to, sodium sulfate, ammonium sulfate, starch, bentonite, diatomaceous earth, kaolin, dextrin, maltodextrin, dextrose, cellulose, microcrystalline cellulose, chitosan, lactose, lactose monohydrate, mannitol, sucrose, talc, maltitol, sorbitol, xylitol, powdered cellulose, cellulose gum, starch, or calcium phosphate.

[0186] In certain embodiments, the compositions provided herein comprise at least two fillers. In certain embodiments, the ratio between the first filler and the second filler can vary in the range of 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).

[0187] In certain embodiments, the filler comprises talc or maltodextrin, or a mixture thereof. In certain embodiments, the filler comprises a mixture of talc and maltodextrin. In certain embodiments, the ratio between talc and maltodextrin is in the range of about 1 : 1-1 : 10, 1 : 1-1 : 9, 1 : 1-1 : 8, 1 : 1-1 : 7, 1 :2-1 : 7, 1 :2-1 : 6, 1 :3-1 : 6, 1 :3-1 : 5, 1 :3-1 : 4, 1 :4-1 : 5, 1 : 5, 1 :4.5, 1 :4, 1 :3.5, 1 :3, or 1 :2 by weight. In some embodiments, the ratio between talc and maltodextrin is about 1 :3.3 by weight. In some embodiments, the ratio between talc and maltodextrin is about 1 :4.5 by weight.

[0188] Different secondary ingredients can be added to the compositions of the disclosure, but are not necessary. Examples of such secondary ingredients are: lubricants, such as magnesium stearate; bittering agents; flavorants; optical brighteners; dyes; sodium carboxymethylcellulose. If desired, the compositions can also be film-coated with a water-soluble film, such as a polyvinyl alcohol film.

[0189] Lubricants can be used to enhance release of the tablet from the equipment in which it is formed, for example by preventing sticking to the surface of the upper punch ("pick-up") or lower punch ("adhesion"). Suitable lubricants include, for example, white carbon, talc, magnesium stearate, calcium stearate, sodium stearate, zinc stearate, stearic acid, boric acid, metallic 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 ester, sodium polyvinyl alcohol benzoate, sodium lauryl sulfate, sodium stearyl fumarate, polyethylene glycol, polypropylene glycol, and polyalkylene glycol. Preferably, the lubricant comprises stearic acid and its salts, such as calcium stearate, magnesium stearate, and aluminum stearate. In certain embodiments, the lubricant comprises magnesium stearate. In one embodiment, an amount of magnesium stearate as a lubricant comprising from about 0.1% to about 5% (e.g., from about 0.1% to about 4.5%, 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 0.5% to about 1.0%, from about 0.5% to about 0.7%, about 0.5%, or about 0.7%) by weight of the composition is included.

[0190] A bittering agent can also be used as an aversive agent in the compositions provided herein to deter inappropriate ingestion by humans or non-target animals. Suitable bittering agents include, but are not limited to, benzodiazepine, denatonium, sucrose octaacetate, quercetin, brucine, and quassine. In certain embodiments, the bittering agent comprises denatonium benzoate. In certain embodiments, the bittering agent is denatonium benzoate. In one embodiment, an amount of denatonium benzoate as a bittering agent comprising from about 0.01% to about 5% (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%, about 0.1%) by weight of the composition is included.

[0191] In certain embodiments, the compositions provided herein are substantially free of any inorganic solvent, 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% by weight of the composition.

[0192] In certain embodiments, the compositions are substantially free of dusting agents in 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% by weight of the composition.

[0193] In certain embodiments, the compositions can optionally further comprise one or more active ingredients selected from the group consisting of herbicides, fungicides, bactericides, insecticides, nematocides, miticides, and growth regulators.

[0194] In certain embodiments, the compositions provided herein can be formulated as a tablet composition. In certain embodiments, each single tablet contains from 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).

[0195] As is well known in the pharmaceutical art, the term "tablet composition" as used herein refers to a solid form that can be produced by molding or compacting a powder on a tableting machine.

[0196] The tablet compositions of the present disclosure can be either homogeneous or heterogeneous. The term "homogeneous" as used herein refers to a tablet produced by molding or compacting a single particulate composition, but does not mean that all the particles of the composition will necessarily be the same composition. The term "heterogeneous" as used herein refers to a tablet having multiple discrete regions, e.g., layers around an insert, an insert, or a film coating.

[0197] The tablets can be prepared using conventional tablet-making equipment and can be of any suitable size and shape, such as round, oval, polygonal, or pillow-shaped, and may optionally have non-functional surface markings. The tablets of this invention can be packaged in containers with accompanying instructions providing relevant information such as, for example, dosage and administration information, concentration, precautions, drug interactions, and adverse reactions.

[0198] The compositions provided herein can be manufactured by known conventional methods, preferably involving mixing ingredients, sieving, and compression. Typically, powder blends are prepared by mixing until homogeneous, passing them through a sieve with a mesh size primarily from about 70 to 200 mesh, and compression into desired tablet sizes and densities in a tablet press (e.g., a hydraulic press with a force of 5,000 to 10,000 pounds).

[0199] In some embodiments, the compositions provided herein have a density greater than that of water (specific gravity greater than 1.00), so that the tablets will sink when in contact with water.

[0200] In some embodiments, the tablets of this disclosure may further comprise a coating, such as a nonfunctional coating. A nonfunctional coating may comprise a polymeric component (e.g., HPMC), optionally together with other components, such as one or more plasticizers, colorants, etc. In some embodiments, the tablet undergoes an additional coating step after compression molding. The term "nonfunctional" as used herein refers to a means that substantially does not affect the release of tablet properties and should not be construed as meaning that the coating has no beneficial effect. For example, such a coating may impart a distinctive appearance to the tablet, provide protection against abrasion during packaging and transportation, and / or other benefits.

[0201] The tablet composition can be manufactured in any size suitable for its application. In some embodiments, the tablet is about 0.01g to about 20g, about 0.05g to about 20g, about 0.1g to about 20g, about 0.2g to about 20g, about 0.5g to about 20g, about 0.5g to about 15g, about 0.5g to about 10g, about 1g to about 10g, about 1g to about 5g, about 2g to about 5g, about 3g to about 5g, about 3g to about 4.5g, about 3g to about 4g, or about 3.0g to about 3.4g.

[0202] In some 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 mm to about 22 mm, about 20 mm, or about 22 mm.

[0203] In certain embodiments, the compositions provided herein, when diluted 1% by weight in water, have a pH range from 5.0 to 8.0, optionally from 6.0 to 7.0. In certain embodiments, the compositions provided herein have a pH of about 6.5, 6.7, or 6.8 (1% by weight diluted in water).

[0204] Hardness is a measure of the force required to cause a tablet to crush under conditions of pre-use storage, handling, and operation, and is typically expressed in units such as kilopounds (kp), Strong-Cobb Units (SCU), or Newtons (N). A hardness of about 1 SCU represents a force of about 0.7 kp or about 7 N. Uncoated tablets or tablet cores prior to coating that include at least one water-soluble pesticidal agent substrate provided herein can need to have a particular minimum hardness in order to be able to withstand breakage and / or attrition due to mechanical stresses applied during the course of high-speed tableting operations, including all steps up to and including filling of the tablets into containers. The minimum acceptable hardness will depend on several factors, including the severity of the mechanical stresses, but it 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.

[0205] Prior to blending, milling, and compaction, the formulation ingredients can be dried. Drying in a vacuum oven at 45 °C to 60 °C for 16 hours is sufficient to reduce the water content of the premix to less than about 3.0%. This helps to ensure that residual moisture does not cause effervescent reactions during storage. Typically, the ingredients are ground and mixed in a mill (e.g., an air mill or a hammer mill). The ground premix is brushed through a 70- to 200-mesh screen. In certain embodiments, the water content of the composition is less than about 3.0%, 2.5%, 2.0%, 1.9%, 1.8%, 1.7%, 1.6%, 1.5%, 1.0%, or 0.5%.

[0206] The present disclosure also provides a method of controlling pests in a crop, the method comprising applying an agronomically effective amount of the composition to the crop or its environment in need thereof.

[0207] The term "agronomically effective amount" as used herein means an amount or application rate of a pesticidal agent composition that, when applied to a crop or pasture, kills or substantially injures a significant portion of a pest or weed or fungal population present therein and / or substantially reduces damage to the crop or pasture at any stage of the growth cycle.

[0208] In certain embodiments, the crop is agronomic or non-agronomic.

[0209] The term "agronomic crops" refers to field crops such as those used for food and fiber and includes corn; soybeans and other legumes; cereals (e.g., wheat, oats, barley, rye, rice, and maize); vegetables, e.g., leafy vegetables (e.g., lettuce, cabbage, and other brassica crops), fruiting vegetables (e.g., tomatoes, peppers, eggplants, crucifers, and cucurbits), potatoes, sweet potatoes; cotton; fruits, grapes, tree fruits (e.g., pomes, drupes, and citrus), small fruits (e.g., berries and cherries); and other specialty crops (e.g., rapeseed, sunflower, and olives).

[0210] The term "non-agronomic crops" refers to other horticultural crops (e.g., greenhouse, nursery, or ornamental plants not grown in the field, plants in residential and commercial structures and industrial sites in towns, turf (e.g., sod farms, pastures, golf courses, lawns, residential areas, recreational areas, and sports fields), wood products, stored products, forestry and vegetation for public health (i.e., human) and animal health (e.g., pets, livestock, and poultry as well as non-domesticated animals such as wildlife) applications.

[0211] In agronomic and non-agronomic applications, the invertebrate pests are controlled by applying an effective amount of the compositions provided in the present disclosure to the pest environment, including the locus to be protected from infestation, to the area to be protected, or directly to the pest to be controlled.

[0212] The term "invertebrate pest" as used herein encompasses economically important arthropods, mollusks, and nematodes that are pests. The term "arthropod" encompasses insects, mites, spiders, scorpions, centipedes, millipedes, pill bugs, and symphylans. The term "mollusk" encompasses snails, slugs, and other Stylommatophora. The term "nematode" encompasses all worms such as: roundworms, heartworms, and plant-parasitic nematodes (Nematoda), flukes (Tematoda), acanthocephalans (Acanthocephala), and tapeworms (Cestoda).

[0213] Agronomic applications include protecting field crops from invertebrate pests by applying a composition or mixture of compositions of the disclosure to crop seeds prior to planting, to furrows during planting, to the foliage, stems, flowers, and / or fruits of crop plants, or to the soil or other growing medium (e.g., rice paddy) before or after the crop is planted or while the crop is growing. Non-agronomic applications refer to invertebrate pest control in areas other than crop plants. Non-agronomic applications include invertebrate pest control in stored grains, legumes, and other foodstuffs, and in textiles such as clothing and carpets. Non-agronomic applications also include invertebrate pest control in ornamental plants, forests, gardens, road and railroad rights-of-way, and turf such as lawns, golf courses, and pastures. Non-agronomic applications also include invertebrate pest control in houses and other structures that can be occupied by humans and / or companion animals, farm animals, pasture animals, zoo animals, or other animals. Non-agronomic applications also include control of pests such as termites that can damage wood or other structural materials in buildings. Non-agronomic applications also include protection of human and animal health by controlling invertebrate pests that are parasitic or that transmit infectious diseases. Such pests include, for example, chiggers, ticks, lice, mosquitoes, flies, and fleas.

[0214] One embodiment of the application of the composition is by spraying. Alternatively, a tablet composition comprising a composition of the disclosure can be applied to plant foliage or to soil. The compounds of the disclosure are also effectively delivered by plant uptake by contacting the plant with a composition of the disclosure applied as a soil drench, a plug tray treatment, or a transplant dip to the soil in which the tablet formulation is placed. In certain embodiments, the crop is rice and the composition is applied to a rice paddy. In certain embodiments, the composition is manually or mechanically dispersed onto the rice paddy, i.e., by hand tossing from a path between rice paddies, or can be tossed from the rice paddy.

[0215] The method is applicable to any situation where a crop is in need of control of a pest or a life stage of a pest. The method can be useful when combined with the process of planting or transplanting, and can also be used on a mature crop, particularly an established rice paddy.

[0216] Harmful organisms that can be controlled by the composition include, but are not limited to, larvae of Lepidoptera, such as armyworms, cutworms, loopers, and heliothines in Noctuidae (e.g., fall armyworm (Spodoptera fugiperda J.E. Smith), beet armyworm (Spodoptera exigua Hübner), black cutworm (Agrotis ipsilon Hufnagel), cabbage looper (Trichoplusia ni Hübner), and tobacco budworm (Heliothis virescens Fabricius)); borers, casebearers, webworms, coneworms, cabbageworms, and skeletonizers from Pyralidae (e.g., European corn borer (Ostrinia nubilalis Hübner), navel orangeworm (Amyelois transitella Walker), corn root-leaf webber (Crambus caliginosellus Clemens), and rice leaffolder (Herpetogramma licarsisalis Walker)); leafrollers, budworms, seed worms, and fruit worms in Tortricidae (e.g., codling moth (Cydia pomonella L. (L. means Linnaeus)), grape berry moth (Endopiza viteana Clemens), and oriental fruit moth (Grapholita molesta Busck)); and many other economically important Lepidoptera (e.g., diamondback moth (Plutella xylostella L. of the family Pieridae), pink bollworm (Pectinophora gossypiella Saunders of the family Gelechiidae), and gypsy moth (Lymantria dispar L. of the family Lymantriidae).))) ; leaf-feeding larvae and adults from the order Coleoptera, including weevils (e.g., cotton curculio (Anthonomus grandis Boheman), rice water weevil (Lissorhoptrus oryzophilus Kuschel), and rice weevil (Sitophilus oryzae L.)) from the families Anthribidae, Bruchidae, and Curculionidae; flea beetles, cucumber beetles, rootworms, leaf beetles, potato beetles, and leafminers (e.g., Colorado potato beetle (Leptinotarsa decemlineata Say), and western corn rootworm (Diabrotica virgifera LeConte)) in the family Chrysomelidae; scarabs and other beetles from the family Scaribaeidae (e.g., Japanese beetle (Popillia japonica Newman) and European chafer (Rhizotrogus majalis Razoumowsky)); wireworms from the family Elateridae and bark beetles from the family Scolytidae; adults and larvae of the order Dermaptera, including earwigs (e.g., European earwig (Forficula auricularia L.) and black earwig (Chelisoches morio Fabricius)) from the family Forficulidae; adults and nymphs of the orders Hemiptera and Homoptera, such as plant bugs from the family Miridee, cicadas from the family Cicadidae, and leafhoppers (e.g., Empoasca spp.) from the family Cicadellidae;), planthoppers from Fulgoroidae and Delphacidae, treehoppers from Membracidae, psyllids from Psyllidae, whiteflies from Aleyrodidae, aphids from Aphididae, phylloxeras from Phylloxeridae, mealybugs from Pseudococcidae, scales from Coccidae, Diaspididae, and Margarodidae, lace bugs from Tingidae, stink bugs from Pentatomidae, cinch bugs (e.g., Blissus spp.) and other seed bugs from Lygaeidae, spittlebugs from Cercopidae, squash bugs from Coreidae, and red bugs and cotton stainers from Pyrrhocoridae; adults and immature of Orthoptera, including grasshoppers, locusts, and crickets (e.g., migratory grasshoppers (e.g., Melanoplus sanguinipes Fabricius and M. differentialis Thomas), American grasshoppers (e.g., Schistocerca americana Drury), desert locusts (Schistocerca gregaria Forskal), migratory locusts (Locusta migratoria L.), and camel crickets (Gryllotalpa spp.)); adults and immature of Diptera, including leafminers, midges, fruit flies (Tephritidae), yellowheaded caterpillars (e.g., Oscinella frit L.), soil grubs, and other Nematocera; adults and immature of Thysanoptera, including onion thrips (Thrips tabaci Lindeman) and other leaf-feeding thrips.

[0217] In certain embodiments, the pests that can be controlled by the composition include, but are not limited to, lissorhoptrus oryzophilus, fall armyworm, spodoptera frugiperda, sugarcane borer, diatrea saccharalis, scirpophaga incertulas, chilo polychrysa, sesamia inferens, nephotettix virescens, nephotettix nigropictus, nilaparvata lugens, leptocarisa acuta, sogatella furcifera, recilla dorsalis, thrips oryzae, mythimna separata, spodoptera mauritia, dicladispa armigera, cnaphalocrisis medinalis, nymphyla depunctalis, parnara guttata, and orseolia oryzae.

[0218] The application rate (i.e., "agriculturally effective amount") required for effective control will depend on such factors as the active ingredient(s), operator, species of invertebrate to be controlled, life cycle, stage of life, size, location, time of year, host crop or animal feeding behavior, mating behavior, density and pattern of crop planting or planting, environmental humidity, temperature, and whether the composition is applied as a preventative or rescue operation. Under normal circumstances, the composition can be applied in the agricultural ecosystem at a rate ranging from about 10 grams of active ingredient per hectare (g ai / ha) to about 10,000 g ai / ha (e.g., about 10 to about 5000 g ai / ha, about 10 to about 1000 g ai / ha, about 10 to about 500 g ai / ha, about 10 to about 200 g ai / ha, about 10 to about 100 g ai / ha, about 10 to about 90 g ai / ha, about 10 to about 80 g ai / ha, about 10 to about 70 g ai / ha, about 10 to about 60 g ai / ha, about 10 to about 50 g ai / ha, about 20 to about 50 g ai / ha, about 30 to about 50 g ai / ha, or about 40 g ai / ha), although as little as 0.1 g ai / ha can be sufficient, or as much as 80,000 g ai / ha can be needed. In certain embodiments, the composition is applied at a rate of about 40 g ai / ha. For non-agronomic applications, the effective use rate range will be from about 1.0 to 50 milligrams per square meter (mg / m2) (e.g., about 1-40 mg / m2, about 1-35 mg / m2, about 1-30 mg / m2, about 1-25 mg / m2, about 1-20 mg / m2, about 1-15 mg / m2, about 1-10 mg / m2, or about 1-5 mg / m2), although as little as 0.1 mg / m2may be sufficient, or as much as 150 mg / m2may be needed. One skilled in the art can readily determine the agriculturally effective amount necessary to achieve the desired level of invertebrate pest control. 2 2 2 2 2 2 2 2 2 2 2 One skilled in the art can readily determine the agriculturally effective amount necessary to achieve the desired level of invertebrate pest control.

[0219] Examples

[0220] The application will be described in greater detail by way of specific examples. The following examples are provided for illustrative purposes and are not intended to limit the application in any way. One skilled in the art will readily recognize a wide variety of non- critical parameters that can be changed or modified to yield essentially the same results.

[0221] Example 1. Screening of anthranilamide tablets​​​​​​​​​​

[0222] Preparation

[0223] Tablets tested in the examples were prepared according to the following procedure: all ingredients were weighed and mixed thoroughly, then sieved to obtain granules in the 70 to 200 mesh range, and then compressed flat by a 60 kilo Newton (kN) tablet press. Tablets having a weight of 3.0-3.5 g and having a diameter of about 20-22 mm were then formed from the granules thus obtained.

[0224] Primary screening

[0225] Prior to screening the enhancer and dispersant used in the formulation containing chlorantraniliprole, the following preliminary screening procedure was performed.

[0226] Acids and bases Different combinations of acids and bases were screened in terms of (a) the ability to generate an appropriate amount of effervescence for an appropriate period of time when in contact with water and to facilitate complete dispersion of the active ingredient in the water in which the plants are growing, (b) cost, and (c) industrial processability (such as from the standpoint of safety). Based on the screening, the preferred combination of acid and base was identified and used in the following examples.

[0227] Lubricants, binders, and fillers Different classes of lubricants, binders, and fillers were screened. Based on the screening, the preferred lubricant, binder, and filler were identified and used in the following examples.

[0228] Enhancer and dispersant screening

[0229] Tablets of different formulations (including, for example, both enhancer and dispersant, enhancer only, dispersant only, or different types of enhancer and dispersant) were prepared and compared in terms of the amount of effervescence and the rate of diffusion of the tablets when in contact with water. The amount of effervescence was checked visually, and the diffusion of the tablets was tracked using a pigment. These formulations and results are summarized in Table 1 below. It can be found that Formulations 1-4, 1-5, and 1-7 showed better performance than other formulations in terms of the amount of effervescence and the rate of diffusion, which is indicated by the symbol +, with more + indicating better performance.

[0230] Table 1

[0231]

[0232] The distribution profile of Formulations 1-4, 1-5, 1-7, and 1-8 was further examined by the following method: (a) a circular water pool having a radius of 1.2 m was provided, and as Figure 1As shown in the diagram, an observation microscope was placed at each sampling location, with a distance of 15 cm between every two adjacent perimeters. Four points (such as A1, A2, A3, and A4) evenly distributed on one perimeter were selected as sampling locations; (b) a pool was filled with tap water to a depth of approximately 5 cm; (c) a tablet (3 g) was dropped into the pool; (d) after 30 minutes, the observation microscope was covered and removed from the pool; (e) the content of active ingredients (including those dissolved and suspended in water and those deposited on the observation microscope) collected in the observation microscope was analyzed by HPLC; and (f) the average value of the active ingredients collected from the four points was calculated. Results were presented in... Figure 2 As shown in the figure, tablets containing both a reinforcing agent of sodium dialkyl sulfosuccinate and a dispersant containing a polycarboxylate (i.e., formulations 1-4, 1-5, and 1-7) achieve better results compared to other formulations.

[0233] Example 2. Novel o-aminobenzamide tablets

[0234] Based on the screening in Example 1, the formulation was further optimized and a bittering or aversive agent was added to the tablet composition to prevent accidental ingestion by humans or animals. Optimized concentrations of chlorantraniliprole (…) The AI ​​formulation is shown in Table 2. Tablets were prepared in the same manner as described in Example 1.

[0235] Table 2

[0236]

[0237] Distribution profile analysis

[0238] The distribution profile of the tablets in Table 2 was examined using the same method described in Example 1. It was found that the tablets in Table 2 achieved the improved effect.

[0239] Stability test

[0240] The stability of the tablets in Table 2 was tested after 14 days of storage. The data are shown in Table 3.

[0241] Table 3

[0242]

[0243] Efficacy analysis (21 days after tablet application)

[0244] Transplant rice seedlings to the paddy field at the 4.5-leaf stage and allow them to grow for 7 days to allow them to potentially turn green before the application of insecticides. Use chlorantraniliprole tablets from Table 2 and commercially available chlorantraniliprole products. and (For reference only) Apply separately to selected fields with consistent field conditions. This tablet and... each by broadcast application, each by foliar application. Chlorantraniliprole tablets and each were typically applied at an application rate of 40 g ai / ha uniformly by broadcast application at 7 days after rice transplanting.

[0245] Efficacy % = ((number of dead hearts in CK group) - (number of dead hearts in treatment group)) / (number of dead hearts in CK group) * 100.

[0246] Results are shown in Table 4.

[0247] Table 4

[0248]

[0249] The results shown in Table 4 indicate that chlorantraniliprole tablets applied at 40 g ai / ha can effectively control rice borer. The 1% chlorantraniliprole tablets, 2.5% chlorantraniliprole tablets, and 5% chlorantraniliprole tablets achieved similar control or even slightly better control than granules and suspension concentrates ("SC", "SC", respectively, ) containing the same dose of chlorantraniliprole, while the tablets formulation is more labor saving to apply.

[0250] Residual of active ingredient chlorantraniliprole in test subjects in the field

[0251] The 1% chlorantraniliprole tablets (4 g), 2.5% chlorantraniliprole tablets (1.6 g), 5% chlorantraniliprole tablets (0.8 g), calculated as 0.04 g ai / 25 m 2 , 0.4% granules), and calculated as 0.04 g ai / 25 m 2, 200 g / L SC) was applied to 5*5 m plots. Rice seedlings were sampled on the 3rd day after the formulation application (3DAA) and the 20th day (20DAA). Since the striped stem borer mainly attacks rice stems, the residue of chlorantraniliprole in rice stems was tested to confirm the uptake of the active ingredient, which can be ingested by the striped stem borer and cause intoxication. To extract the active ingredient, chlorantraniliprole, the rice seedlings were cut and the stems were picked out and immersed in acidic acetonitrile for 24 hours. The resulting solution was further shaken for 2 hours and then filtered and analyzed by GC-MS to measure the amount of the active ingredient, chlorantraniliprole, taken up by the rice seedlings.

[0252] The residue amount of chlorantraniliprole in rice (pg / kg) according to the test results of GC-MS is summarized in Table 5 and is shown in Figure 3 On the 3rd day and the 20th day after the formulation application, the seedlings to which 1% chlorantraniliprole tablets (4 g), 2.5% chlorantraniliprole tablets (1.6 g), or 5% chlorantraniliprole tablets (0.8 g) were applied took up more of the active ingredient, chlorantraniliprole, than those to which or were applied, indicating that the tablet formulations containing the claimed enhancer and dispersant are more effectively dispersed in the water of the rice field.

[0253] Table 5

[0254]

[0255] The concentration of chlorantraniliprole in the seedlings collected at different distances from the application point was measured as described above, and the results are summarized in Tables 6 and 7 and shown in FIG. 4.

[0256] Table 6

[0257]

[0258] Table 7

[0259]

[0260] Example 3. More tablets

[0261] Several tablets containing similar ingredients to those in Table 2, but different pesticidal active ingredients, were prepared. Those containing the claimed enhancer and dispersant are expected to achieve similar improved effects in terms of diffusivity and permeability to those of the tablets in Table 2.

[0262] The application can also be generally stated as including parts, elements and features referred to or indicated in the specification individually or collectively, and any or all combinations of any two or more of the parts, elements, components or features, and where specific integers are mentioned in this specification and a combination of those integers is not specifically stated, the combination is nevertheless expressly addressed. The specific integers are considered to be combinable to form the stated combination.

[0263] The application has been described with particular reference to certain embodiments thereof. It will be understood that various modifications can be made to the above-described embodiments without departing from the scope of the present application. It will also be understood by the person of ordinary skill in the art that concepts expressed by the purposeful construction.

Claims

1. A tablet composition comprising, by weight based on the total weight of the composition: (a) 0.1% to 20% of a pesticidal active ingredient, wherein the pesticidal active ingredient comprises chlorantraniliprole, cyantraniliprole, tetraniliprole, cyclaniliprole, halofenozide, teflubenzuron, bromide, clothianidin, thiamethoxam, thiacloprid, dinotefuran, or a mixture thereof; (b) 0.1% to 5% of an enhancer, wherein the enhancer comprises a dialkyl sulfosuccinate; (c) 0.1% to 10% of a dispersing agent, wherein the dispersing agent comprises a polycarboxylate; (d) 0.1% to 20% of a binder; and (e) 0.1% to 50% of an optional filler.

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

3. The tablet composition according to claim 1, wherein, The 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 (zea mays) starch, modified cellulose, alginic acid, sodium carboxymethylcellulose, and copovidone.

4. The tablet composition according to claim 3, wherein, The component (d) comprises PEG.

5. The tablet composition according to claim 4, wherein, The component (d) comprises at least one PEG selected from the group consisting of PEG 2000, PEG 4000, PEG 6000, PEG 8000, and PEG 10000.

6. The tablet composition according to claim 5, wherein, The component (d) comprises PEG 6000.

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

8. The tablet composition according to claim 7, wherein, The component (e) comprises talc or maltodextrin, or a mixture thereof.

9. The tablet composition according to claim 8, wherein, The component (e) comprises a mixture of talc and maltodextrin.

10. The tablet composition according to any one of claims 7 to 9, wherein, The talc, when used, is 1% to 15%, 1% to 10%, 1% to 8%, 2% to 8%, 3% to 8%, 4% to 8%, 5% to 8%, 6% to 8%, or 6% by weight of the composition, and the maltodextrin, when used, is 1% to 40%, 1% to 30%, 5% to 30%, 8% to 30%, 10% to 30%, 15% to 30%, 18% to 30%, 18% to 27%, or 20% to 27% by weight of the composition.

11. The tablet composition according to any one of claims 1 to 9, wherein, The composition further comprises, by weight based on the total weight of the composition: component (f) 0.1% to 40% of at least one acid and component (g) 0.1% to 40% of at least one base, wherein the acid is selected from polyprotic organic acids and the base is selected from alkali or alkaline earth metal carbonates.

12. The tablet composition according to claim 11, wherein, The acid is selected from succinic acid, D,L-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-toluene sulfonic acid, malic acid, maleic acid, malonic acid, and oxalic acid.

13. The tablet composition according to claim 11, wherein, The base is selected from sodium carbonate, potassium carbonate, sodium bicarbonate, potassium bicarbonate, calcium carbonate, and calcium bicarbonate.

14. The tablet composition according to any one of claims 1 to 9, wherein, The composition further comprises, based on the total weight of the composition, by weight: component (h) 0.1% to 5% of at least one lubricant.

15. The tablet composition according to any one of claims 1 to 9, wherein, The composition further comprises, based on the total weight of the composition, by weight: component (i) 0.01% to 5% of at least one bittering agent.

16. A method for controlling pests in a crop, the method comprising applying to the crop or its environment in need thereof an agronomically effective amount of the tablet composition according to any one of claims 1 to 15.

17. The method of claim 16, wherein, The crop is rice and the composition is applied to a rice field.

18. The method of claim 16, wherein, The crop is selected from the group consisting of rice, vegetables, and corn.

19. The method of claim 18, wherein, The crop is rice.

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