Description:FIELD OF THE INVENTION
[0001] The present invention relates to the technical field of herbicides. In particular the present disclosure relates to a composition comprising combination of herbicides mesotrione and tembotrione, and one or more agriculturally acceptable excipients and a formulation thereof.

BACKGROUND OF THE INVENTION
[0002] The background description includes information that may be useful in understanding the present invention. It is not an admission that any of the information provided herein is prior art or relevant to the presently claimed invention, or that any publication specifically or implicitly referenced is prior art.
[0003] Protection of crops from weeds and other vegetation which inhibit crop growth is a constantly recurring problem in agriculture. To address this problem, researchers are trying to produce an extensive variety of active agents and active agent formulations effective in the control of such undesirable plant growth. Chemical herbicides of many types have been disclosed in the art and a large number are in commercial use. In crop protection, it is desirable in principle to increase specificity and reliability of action of herbicidal active agents. In particular, it is desirable for a crop protection product to control undesirable plants effectively and, at the same time, to be tolerated by useful plants in question.
[0004] Tembotrione, mesotrione, bicyclopyrone, dioxopyritrione, fenquinotrione, ketospiradox, lancotrione, quintrione, sulcotrione, tefuryltrione, and atrazine are compounds independently known in the art for their herbicidal potency. They are disclosed in ‘The Pesticide Manual’ 15th Edition, published 2009 by the British Crop Protection Council, and are also commercially available.
[0005] It is known that to seek and obtain registration for a new herbicide compound, including its proposed use rate, is very expensive and time-consuming process. Approval data required must not only include evidence of efficacy at the application rates proposed but also safety of herbicide when applied at the recommended level, also information about the recommended level of herbicide that may be applied per unit of area needs to be provided in view of pressure from governmental, as well as for economic and environmental reasons.
[0006] It is a common knowledge that with the use of a single herbicide over a period, the undesirable broadleaf weeds, grassy weeds and sedges develop resistance, rendering the particular herbicide ineffective for use against the specific weeds. Thus, on one hand even more stringent conditions are being placed on the type and use rate of herbicide, while on the other hand approved herbicides available in the art are becoming less and less effective over time in certain species of undesirable plants.
[0007] Due to such reasons including the lengthy and cost intensive process, resistance to single herbicide, combinations of known and approved herbicides are attempted.
[0008] Two-way combination of mesotrione and atrazine is known in the art and is in commercial use.
[0009] However, certain undesirable species, broadleaf weeds, grassy weeds and sedges are becoming increasingly resistant to even a number of most widely used herbicides formulations with common combination of two ingredients available in the art. Hence, such combinations are also found to be ineffective in controlling the undesirable broadleaf weeds, grassy weeds and sedges in effective manner. Other problems with the combination of such two active ingredients can be lack of stability, development of resistance and in certain cases increased toxicity for human, and animals.
[0010] Thus, there still remains an unmet great need in the art for composition comprising combination of herbicides for providing environmentally safe, efficacious herbicidal formulation which is showing one or more of advantages such as stability, synergistic effect, faster onset of herbicidal action, a broad-spectrum and longer-lasting action with phytotonic effect, reduced dosage of active ingredients, reduced application rate of the herbicide.

SUMMARY OF THE INVENTION
[0011] In an aspect the present disclosure is directed to provide a composition comprising herbicide mesotrione in combination with other herbicide and a formulation thereof for overcoming one or more challenges in the existing art and providing one or more advantages such as stability, synergistic effect, reduced dosage of active ingredients, reduced application rate of the herbicide, reduce or delay the development of resistance, faster onset of herbicidal action, a broad-spectrum and longer-lasting action.
[0012] In an aspect the present disclosure provides a composition comprising combination of mesotrione, tembotrione and one or more agriculturally acceptable excipients.
[0013] In one aspect the present disclosure provides a composition comprising combination of mesotrione, tembotrione and one or more agriculturally acceptable excipients selected from the group comprising of dispersing agent, wetting agent, anti-freezing agent, anti-foaming agent, biocide, rheology modifier and solvent.
[0014] In another aspect the present disclosure provides a formulation comprising combination of mesotrione, tembotrione and one or more agriculturally acceptable excipients selected from the group comprising of dispersing agent, wetting agent, anti-freezing agent, anti-foaming agent, biocide, rheology modifier and solvent.
[0015] In an aspect, the herbicide composition in accordance with the present disclosure is formulated or is the form selected from a water-dispersible granule (WDG), a water-soluble granule (SG), a wettable powder (WP), a water-dispersible powder (WDP), a water-soluble powder (SP), a granule (GR), an encapsulated granule (CG), a fine granule (FG), a macrogranule (GG), a microgranule (MG), a suspension concentrate (SC), a water-soluble concentrate (SL), an emulsifiable concentrate (EC), an emulsion (EW), a micro-emulsion (ME), a flowable suspension (FS), a suspoemulsion (SE), ZC formulation (ZC), Soil Applied Granules (SAG), dustable powder (DP), a gel, a water-dispersible tablet (WT), a dispersible concentrate (DC), an oil-dispersion (OD) or a microencapsulated suspension (CS).
[0016] In one specific aspect, the herbicide formulation comprising mesotrione, tembotrione and one or more agriculturally acceptable excipients selected from the group comprising of dispersing agent, wetting agent, anti-freezing agent, anti-foaming agent, biocide, rheology modifier and solvent is a suspension concentrate (SC).
[0017] In yet another aspect, the present disclosure provides a process for preparing suspension concentrate (SC) comprising mesotrione, tembotrione and one or more agriculturally acceptable excipients selected from the group comprising of dispersing agent, wetting agent, anti-freezing agent, anti-foaming agent, biocide, rheology modifier and solvent.
Various objects, features, aspects and advantages of the inventive subject matter will become more apparent from the following detailed description of preferred embodiments.

DETAILED DESCRIPTION OF THE INVENTION
[0018] The following is a detailed description of embodiments of the present disclosure. The embodiments are in such detail as to clearly communicate the disclosure. However, the amount of detail offered is not intended to limit the anticipated variations of embodiments; on the contrary, the intention is to cover all modifications, equivalents, and alternatives falling within the spirit and scope of the present disclosure as defined by the appended claims.
[0019] Unless the context requires otherwise, throughout the specification which follow, the word “comprise” and variations thereof, such as, “comprises” and “comprising” are to be construed in an open, inclusive sense that is as “including, but not limited to.”
[0020] Reference throughout this specification to “one embodiment” or “an embodiment” means that a particular feature, structure or characteristic described in connection with the embodiment is included in at least one embodiment. Thus, the appearances of the phrases “in one embodiment” or “in an embodiment” in various places throughout this specification are not necessarily all referring to the same embodiment. Furthermore, the particular features, structures, or characteristics may be combined in any suitable manner in one or more embodiments.
[0021] As used in this specification and the appended claims, the singular forms “a,” “an,” and “the” include plural referents unless the content clearly dictates otherwise. It should also be noted that the term “or” is generally employed in its sense including “and/or” unless the content clearly dictates otherwise.
[0022] In some embodiments, the numbers expressing quantities of ingredients, properties such as concentration, process conditions, and so forth, used to describe and claim certain embodiments of the invention are to be understood as being modified in some instances by the term “about.” Accordingly, in some embodiments, the numerical parameters set forth in the written description are approximations that can vary depending upon the desired properties sought to be obtained by a particular embodiment. In some embodiments, the numerical parameters should be construed in light of the number of reported significant digits and by applying ordinary rounding techniques. Notwithstanding that the numerical ranges and parameters setting forth the broad scope of some embodiments of the invention are approximations, the numerical values set forth in the specific examples are reported as precisely as practicable.
[0023] The recitation of ranges of values herein is merely intended to serve as a shorthand method of referring individually to each separate value falling within the range. Unless otherwise indicated herein, each individual value is incorporated into the specification as if it were individually recited herein.
[0024] All methods described herein is performed in suitable order unless otherwise indicated herein or otherwise clearly contradicted by context. The use of any and all examples, or exemplary language (e.g., “such as”) provided with respect to certain embodiments herein is intended merely to better illuminate the invention and does not pose a limitation on the scope of the invention otherwise claimed. No language in the specification should be construed as indicating any non-claimed element essential to the practice of the invention.
[0025] The headings and abstract of the invention provided herein are for convenience only and do not interpret the scope or meaning of the embodiments.
[0026] The following discussion provides many example embodiments of the inventive subject matter. Although each embodiment represents a single combination of inventive elements, the inventive subject matter is considered to include all possible combinations of the disclosed elements. Thus, if one embodiment comprises elements A, B, and C, and a second embodiment comprises elements B and D, then the inventive subject matter is also considered to include other remaining combinations of A, B, C, or D, even if not explicitly disclosed.
[0027] The present invention does not use any ‘biological materials’ that is the materials which are capable of reproducing itself or being reproduced in a biological system.
[0028] The present disclosure provides a composition comprising combination of herbicides mesotrione and tembotrione and one or more agriculturally acceptable excipients, a formulation therefore and process for preparing the same.
[0029] In one embodiment, the present disclosure provides a composition comprising herbicides mesotrione and tembotrione and one or more agriculturally acceptable excipients.
[0030] Mesotrione chemically known as 2-[4-(methylsulfonyl)-2-nitrobenzoyl]-1,3-cyclohexanedione is a triketone herbicide. It is a systemic herbicide and acts by inhibiting 4-hydroxyphenylpyruvate dioxygenase (HPPD) enzyme.
[0031] Tembotrione chemically known as
2-[2-chloro-4-(methylsulfonyl)-3-[(2,2,2-trifluoroethoxy)methyl]benzoyl]-1,3-cyclohexanedione is a triketone herbicide. It is a systemic herbicide and it acts by inhibiting 4-hydroxyphenylpyruvate dioxygenase (HPPD) enzyme.
[0032] In one embodiment, the mesotrione is present in an amount of from about 0.1% to about 30 % w/w.
[0033] In one embodiment, the tembotrione is present in an amount of from about 0.1% to about 30% w/w.
[0034] Suitable agriculturally acceptable excipients can depend upon such factors as the type of formulation to be formulated from the composition and the manner of the end use of the formulation, and will be known to a person skilled in the art.
[0035] In some embodiments, the agriculturally acceptable excipients can be selected from the group consisting of but not limiting to a dispersing agent, a wetting agent, an anti-freezing agent, an anti-foaming agent, a biocide, a rheology modifier and a solvent, an anti-crystalline agent, an emulsifier, a pH stabilizer, a spreading agent, an inert carrier, a stabilizing agent, an anti-caking agent, an antioxidant, a capsule forming agent, a quenching agent, a super spreader which includes combination thereof.
[0036] The dispersing agent can be selected from, lignosulphonates, phenyl naphthalene sulphonates, ethoxylated alkyl phenols, polyalkoxylated butyl ether ethopropoxylated polyarylphenol phosphate amine salt, ethoxylated fatty acids, alkoxylated linear alcohols, polyaromatic sulfonates, sodium alkyl aryl sulfonates, maleic anhydride copolymers, phosphate esters, condensation products of aryl/alkyl sulphonic acids and formaldehyde, sodium lignosulfonate, addition products of ethylene oxide and fatty acid esters, sulfonates of condensed naphthalene, lignin derivatives, naphthalene formaldehyde condensates, polycarboxylates, sodium alkyl benzene sulfonates, alkali earth metal salt of alkylbenzene sulfonate, alkali earth metal salt of naphthalene formaldehyde condensate, calcium dodecylbenzene sulfonate, salts of sulfonated naphthalene, salts of phenol sulfonic acids, polymethyl methacrylate-polyethylene glycol graft copolymer, polystyrenated acrylated co- polymer, random co-polymer of alcoxylated polyethylene glycol, lignosulphonates, ammonium salts of sulfonated naphthalene, salts of polyacrylic acids, sodium salt of naphthalene sulfonate formaldehyde condensate and mixtures thereof. The dispersing agent can be present in an amount ranging from about 0.1% to about 25% w/w of the composition.
[0037] The wetting agent can be selected from, alkyl phenol ethoxylate, fatty oil ethoxylate, phenyl naphthalene sulphonates, alkyl naphthalene sulfonates, sodium alkyl naphthalene sulfonate, sodium salt of sulfonated alkyl carboxylate, dioctyl sulfosuccinate sodium salt, polyoxyalkylated ethyl phenols, polyoxyethoxylated fatty alcohols, polyoxyethoxylated fatty amines, alkane sulfonates, alpha olefin sulfonates, alkylbenzene sulfonates, octyl phenol ether sulphate, anionic phosphate esters, disodium laureth sulfosuccinate, disodium hexadecyl sulphate, diisodecyl sodium sulfosuccinate, alkylnaphthalenesulfonates, alkylbenzenesulfonates, alkylpolyglycol ether sulfonates, alkyl ether phosphates, alcohol ethoxylate (AtloxTM 4894 also known as polyoxyethylene alkyl ether or nonionic proprietary surfactant blend), and alkyl sulfosuccinic monoesters, lignin derivatives, salts of polycarboxylic acids, salts of esters of sulfosuccinic acid, C12-15 ethoxylated alcohols, alkyl ether sulphates, sodium isopropyl naphthalene sulfonate and mixtures thereof.
[0038] The wetting agent can be present in an amount ranging from about 0.5 % to about 15% w/w of the composition.
[0039] Suitable anti-freezing agents include organic solvents such as ethylene glycol, glycerine, urea, propylene glycol, other glycols, and mixtures thereof. The anti-freezing agent is present in the composition in an amount of from about 6.0% to about 20% w/w of the composition.
[0040] Suitable anti-foaming agents to be included can be selected from substances which normally be used for this purpose in agrochemical formulations. In certain preferred embodiments, anti-foaming agents can be perfluroalkylphosphonic acids or polydimethyl siloxanes. The anti-foaming agent can be present in an amount ranging from about 0.1% to about 5% w/w of the composition.
[0041] The biocide is selected from formaldehyde or 1,2-benzisothiazolin-3-one. The biocide is present in an amount of from about 0.1% to about 5% w/w of the composition.
[0042] The rheology modifier can be selected from attapulgites, xanthan gum, polyvinyl alcohol, organic derivative of hectorite clay, benton, thickening silica, hydrated clay minerals, magnesium aluminium silicates, hydrophobic fumed silica, bentonite, diatomaceous earth, montmorillonite, polysaccharide gel and mixtures thereof.
[0043] The rheology modifier can be present in an amount ranging from about 0.01 % to about 3% w/w of the composition.
[0044] Suitable solvents can be selected from all customary organic solvents which dissolve one or more of the active ingredients. Suitable aqueous and non aqueous organic solvents for the compounds mesotrione and tembotrione are known in the art. Preferred solvents can be selected from but not limiting to, dimethylsulfoxide (DMSO), vegetable oils, methylated vegetable oils, oil medium selected from the group comprising, esterified fatty acids selected from methyl ester of triglycerides containing C12 –C22 saturated and unsaturated fatty acids, ethyl ester of triglycerides containing C12 –C22 saturated and unsaturated fatty acids such as methyl soyate, ethyl soyate, rapeseed methyl ester, rapeseed ethyl ester, bio-diesels, tall oil, Rhodiasolv® match 111(blend of solvents), Rhodiasolve Green 25 (diisobutyl ester), Rhodiasolv® polar clean (methyl 5-(dimethylamino)-2-methyl-5-oxopentanoate), deionized (DI) water, demineralised water and mixtures thereof. The solvent can be present in an amount ranging from about 1.0% to about 90% w/ w of the composition.
[0045] In an embodiment, the anti-crystalline agent can be selected from without limitation vinyl pyrrolidone polymer, polyvinyl alcohol, acrylic graft copolymer and sodium polyacrylate co-polymer including combination thereof.
[0046] In one embodiment, the anti-crystalline agent can be present in an amount ranging from about 0 % to about 25% w/w of the composition.
[0047] Suitable emulsifier includes all substances which normally can be used for this purpose in agrochemical formulations. Examples of the excipient include substances which can be ionic or non-ionic emulsifier or surfactant. The ionic substances can be selected from cationic, or anionic or combination thereof.
[0048] The ionic emulsifier or surfactant can be selected from the group consisting of but not limiting to calcium salt of alkylaryl sulfonates, calcium dodecylbenzene sulfonate, ethoxylated and/or propoxylated di- or tri-styrylphenol phosphate, ethoxylated and/or propoxylated di- or tri-styrylphenol sulfate, phenyl sulfonate, alkynaphtalenesulphonate ethoxylated and/or propoxylated alcohol phosphate ester, ethoxylated and/or propoxylated alkylaryl phosphate ester, suphosuccinate, salts of polyacrylic acids, salts of lignosulphonic acid, salts of phenylsulphonic or naphthalenesulphonic acids, polycondensates of ethylene oxide with fatty alcohols or with fatty acids or with fatty amines, substituted phenols, especially alkylphenols, sulphosuccinic ester salts, taurine derivatives, especially alkyl taurates, and phosphoric esters of polyethoxylated phenols or alcohols or polycarboxylate.
[0049] The non-ionic emulsifier or surfactant can be selected from the group consisting of but not limiting to alkoxylated alcohols, ethoxylated alcohols, ethoxylated propoxylated alcohols, alkylphenolethoxylates, alkoxylated tristyrylphenols, tristyryphenol ethoxylate, alkoxylated tributylphenols, alkylaminethoxylates, ethoxylated propoxylated polyaryl phenol, ethoxylated poly adducts of ethylene oxide and propylene oxide, ethoxylated fatty acids, sorbitan esters and their ethoxylates, sorbitol esters, propylene glycol esters of fatty acids and polyglycerol esters, ethoxylated ricinoleic acid triglycerides or castor oil ethoxylate.
[0050] In one embodiment, the emulsifier can be present in an amount ranging from about 0% to about 20 % w/w of the composition.
[0051] The pH stabilizer can be selected from sodium silicate, potassium silicate, magnesium silicate, manganese silicate, sodium pyrophosphate, sodium acetate, sodium oxalate, sodium carbonate, sodium bicarbonate, sodium bentonite, sodium acetate, attapulgite, diatomaceous earth, sodium zeolite, trisodium phosphate, trisodium citrate, magnesium carbonate, magnesium sulphate, monoethanol amine, triethanol amine, triethylamine, dibasic esters selected from dimethyl succinate, dimethyl glutarate, dimethyl adipate, ortho phosphoric acid, oxalic acid, citric acid anhydrous, hydrochloric acid and mixtures thereof.
[0052] The pH stabilizer can be present in an amount ranging from about 0% to about 10% w/w of the composition.
[0053] Suitable spreading agents can be selected from the group comprising of polyoxyethylene alkyl ether, trisiloxane ethoxylate, polysorbates, ethoxylated tristyrylphenol phosphate, tridecyl alcohol ethoxylate, sodium lauryl sulphate or sodium methyl oleoyl taurate. Spreading agents can be present in an amount ranging from about 0% to about 10 % w/w of the composition.
[0054] Suitable inert carrier(s) include without limitation natural ground minerals selected from but not limiting to kaolin or china clay, alumina, talc, chalk, quartz, attapulgite, montmorillonite; or crushed and fractionated natural minerals, such as calcite, marble, pumice, precipitated silica, sepiolite, bentonite, river sand, zeolites, starch, sand, talc, quartz and dolomite and diatomaceous earth; or synthetic ground minerals selected from but not limiting to highly dispersed silicic acid, aluminium oxide, corn starch, silicates, and calcium phosphates and calcium hydrogen phosphates; or synthetic granules of inorganic and organic ground materials. The inert carrier can be present in an amount ranging from about 0% to about 90% w/w of the composition.
[0055] The stabilizing agent can be selected from without limitation modified hydrophobic silica, colloidal silica, precipitated silica, hydrophobic silica powder, polyvinylpyrrolidone (PVP) and mixtures thereof. Preferably, the stabilizing agent is dimethyldichlorosilane treated fumed silica. In another embodiment, the stabilizing agent is selected from epoxidized soybean oil, gamma butyrolactone, butylated hydroxyl toluene and its derivatives, epichlorhydrin, quinone derivatives, hydrazine hydrates and its derivatives, general class UV stabilizers, glycols and its derivatives and mixtures thereof. The stabilizing agent can be present in an amount ranging from about 0% to about 10% w/w of the composition.
[0056] The anti-caking agent can be selected from but not limiting to kaolin clay, precipitate silica, colloidal silica, talc, gypsum, silicates, calcium carbonate, hydrophobic fumed silica, magnesium carbonate, magnesium sulfate, and mixtures thereof. The anti-caking agent can be present in an amount ranging from about 0% to about 10% w/w of the composition.
[0057] Suitable antioxidants are all substances which normally be used for this purpose in agrochemical formulations, as is known in the art. Preferred antioxidant is butylated hydroxytoluene. Antioxidant is present in an amount of from about 0% to about 5% w/w of the composition.
[0058] Suitable capsule forming agent can be selected from the group comprising of methylene diisocyanate, toluene diisocyanate or mixtures thereof. The capsule forming agent can be present in an amount ranging from about 0 % to about 5% w/w of the composition.
[0059] Suitable quenching agent can be selected from the group comprising of ammonia solution (25%), ethylene diamine (EDA), ethanol-amine, butadiene or mixture thereof. The quenching agent can be present in an amount ranging from about 0 % to about 10% w/w of the composition.
[0060] Suitable super spreader can be selected from the group comprising of modified trisiloxane, trisiloxane alkoxylate or mixture thereof. The super spreader can be present in an amount ranging from about 0 % to about 10% w/w of the composition.
[0061] In one embodiment the agriculturally acceptable excipients can be selected from the group comprising of dispersing agent, wetting agent, anti-freezing agent, anti-foaming agent, biocide, rheology modifier and solvents.
[0062] In an embodiment, the composition in accordance with the present disclosure comprises mesotrione, tembotrione, one or more agriculturally acceptable excipients selected from the group comprising of dispersing agent, wetting agent, anti-freezing agent, anti-foaming agent, biocide, rheology modifier and solvent in a wide range of amounts effective for treating the undesirable broadleaf weeds, grassy weeds and sedges.
[0063] In certain embodiments, the composition comprises mesotrione, tembotrione in total amount ranging from about 0.1% to about 60% by weight.
[0064] In certain embodiments, the herbicide composition comprising mesotrione in an amount of from about 0.1% to about 30 % w/w, tembotrione in an amount of from about 0.1% to about 30% w/w, dispersing agent in an amount of from about 0.1% to about 25% w/w, wetting agent in an amount of from about 0.5% to about 15% w/w, anti-freezing agent in an amount of from about 6.0 % to about 20% w/w, anti-foaming agent in an amount of from about 0.1% to about 5% w/w, biocide in an amount of from about 0.1% to about 5% w/w, rheology modifier in an amount of from about 0.01% to about 3% w/w and solvent in an amount of from about 1.0% to about 90% w/w.
[0065] In another embodiment, the present disclosure provides an herbicidal formulation comprising the herbicide composition in accordance with the present disclosure.
[0066] In various embodiments, the herbicide formulation comprises the combination of mesotrione, tembotrione and one or more agriculturally acceptable excipients selected from the group comprising of dispersing agent, wetting agent, anti-freezing agent, anti-foaming agent, biocide, rheology modifier and solvent.
[0067] The present disclosure provides a herbicide formulation comprising mesotrione in an amount of from about 0.1% to about 30 % w/w, tembotrione in an amount of from about 0.1% to about 30% w/w, dispersing agent in an amount of from about 0.1% to about 25% w/w, wetting agent in an amount of from about 0.5% to about 15% w/w, anti-freezing agent in an amount of from about 6.0 % to about 20% w/w, anti-foaming agent in an amount of from about 0.1% to about 5% w/w, biocide in an amount of from about 0.1% to about 5% w/w, rheology modifier in an amount of from about 0.01% to about 3% w/w and solvent in an amount of from about 1.0% to about 90% w/w.
[0068] In certain embodiment, the herbicidal formulation can be provided in liquid or solid form.
[0069] In certain embodiments, the herbicide composition is formulated or is in the form selected from but not limiting to a water-dispersible granule (WDG), a water-soluble granule (SG), a wettable powder (WP), a water-dispersible powder (WDP), a water-soluble powder (SP), a granule (GR), an encapsulated granule (CG), a fine granule (FG), a macrogranule (GG), a microgranule (MG), a suspension concentrate (SC), a water-soluble concentrate (SL), an emulsifiable concentrate (EC), an emulsion (EW), a micro-emulsion (ME), a flowable suspension (FS), a suspoemulsion (SE), ZC formulation (ZC), Soil Applied Granules (SAG), dustable powder (DP), a gel, a water-dispersible tablet (WT), a dispersible concentrate (DC), an oil-dispersion (OD) or a microencapsulated suspension (CS).
[0070] In a preferred embodiment, the herbicide composition comprising the combination of mesotrione, tembotrione and one or more agriculturally acceptable excipient(s) selected from the group comprising of dispersing agent, wetting agent, anti-freezing agent, anti-foaming agent, biocide, rheology modifier and solvent is a suspension concentrate (SC).
[0071] In one aspect, the suspension concentrate (SC) comprises:
a) about 0.1% to about 30% mesotrione by weight;
b) about 0.1% to about 30% tembotrione by weight;
c) about 0.1% to about 25% dispersing agent by weight
d) about 0.5% to about 15% wetting agent by weight;
e) about 6.0 to about 20% anti-freezing agent by weight
f) about 0.1 to about 5% anti-foaming agent by weight;
g) about 0.1 to about 5% biocide by weight;
h) about 0.01 to about 3% rheology modifier by weight; and
i) about 1 to about 90% solvent by weight.
[0072] In one specific aspect, the suspension concentrate (SC) comprises:
a) 12% mesotrione by weight;
b) 12% tembotrione by weight;
c) 4 % dispersing agent by weight;
d) 0.5% wetting agent by weight;
e) 10% anti-freezing agent by weight;
f) 0.5% anti-foaming agent by weight;
g) 0.1% biocide by weight;
h) 0.2% rheology modifier by weight; and
i) 60.7 % solvent by weight.
[0073] In another aspect, the present disclosure provides process for preparing suspension concentrate (SC) comprising the steps of:
a) adding active ingredients mesotrione, tembotrione, one or more agriculturally acceptable excipients selected from the group comprising of dispersing agent, wetting agent, anti-freezing agent, anti-foaming agent and biocide in the solvent demineralised water and mixing for about 30 minutes to about 1 hour to obtain the slurry.
b) passing the slurry through the mill for particle size reduction to obtain the milled slurry.
c) charging the rheology modifier to the milled slurry and continuing to mix for about 4 hours to about 6 hours to obtain the homogeneous suspension concentrate (SC).
[0074] In one embodiment the mill for particle size reduction can be a bead mill with cold water circulation.
[0075] The composition and formulation of the present invention are capable of providing one or more of advantages such as a reduction in application rate of individual active ingredients, a faster onset of herbicidal action, better efficacy, environmentally safe, long duration of control, better control of broad spectrum of weeds with only one or a few applications. It was an unexpected finding that the dose of each active ingredient markedly reduced, when both the compounds are comprised in combination in a single formulation, while maintaining a high level of herbicidal efficacy.
[0076] The herbicide formulation thereof according to the present disclosure can be advantageously applied for the protection of crops such as maize and sugarcane.
[0077] The herbicide formulation of the present disclosure can control the growth of undesirable vegetation such as broadleaf weeds, grassy weeds and sedges by post-emergence application
[0078] The herbicide formulation of the present invention can be applied to the weeds in a variety of ways, at various application timing and at various concentrations.
[0079] In one embodiment, the herbicide formulation of the present disclosure is applied to the weeds by foliar application. The application of the herbicide formulation is done on the crops from vegetative phase to reproductive phase. The total application rate of the formulation provided in accordance with the present disclosure comprising mesotrione, tembotrione, one or more agriculturally acceptable excipients selected from the group comprising of dispersing agent, wetting agent, anti-freezing agent, anti-foaming agent, biocide, rheology modifier and solvent can vary over a wide range, for example from 1 to 500gram or ml per hectare.
[0080] In one embodiment, the formulation provided in accordance with the present disclosure can be applied at the application rate ranging from 450 to 500 gram or ml per hectare.
[0081] The herbicide formulation thereof can be applied in a single treatment or in several treatments (sequential application).
[0082] The present disclosure is further explained in the form of following examples. However, it is to be understood that the following examples are merely illustrative and are not to be taken as limiting to the invention. Various changes and modifications to the disclosed embodiments will be apparent to those skilled in the art. Such changes and modifications may be made without departing from the disclosure of the present application.

EXAMPLES
I. Preparation of the suspension concentrate (SC):
[0083] SC were prepared according to the ingredients and concentrations mentioned in the following Table 1:
Examples 1-3: Tembotrione +Mesotrione SC in accordance with the present disclosure.
Table 1: Compositions for Suspension Concentrate (SC)
Ingredients Example 1 Example 2 Example 3
% w/w % w/w % w/w
Mesotrione 12. 0 6.0 24.0
Tembotrione 12.0 6.0 24.0
Sodium salt of naphthalene sulfonate formaldehyde condensate 4.0 3.0 6.0
Sodium isopropyl naphthalene sulfonate 0.5 2.5 3.0
Propylene glycol 10.0 7.0 8.0
Polydimethyl siloxane 0.5 0.5 0.8
1,2-Benzisothiazolin-3-one 0.1 0.1 0.2
Polysaccharide Gel 0.2 0.25 0.18
Demineralised water QS QS QS
Total 100.00 100.00 100.00

Process for preparing the suspension concentrate (SC):
The active ingredients mesotrione, tembotrione and other agriculturally acceptable excipients sodium salt of naphthalene sulfonate formaldehyde condensate, sodium isopropyl naphthalene sulfonate, propylene glycol, polydimethyl siloxane, 1,2-benzisothiazolin-3-one and demineralised water as mentioned in Examples 1 to 3 were added into the dry pre-mixing vessel fitted with homogenizer and all the ingredients were mixed for 30 minutes with the homogenizer to obtain a slurry. The slurry was passed through bead mill under cold water circulation (temp 15ºC) for particle size reduction (d90 < 15 microns) to obtain a milled slurry. The milled slurry was transferred to post mixing vessel and the rheology modifier polysaccharide gel in the amounts as mentioned in Table 1 were added to the milled slurry and continued to mix for about 4 hours to about 6 hours to obtain the homogeneous suspension concentrate (SC).

II. Accelerated Storage test (Stability Study):
[0084] According to the FAO/WHO manual, the “accelerated storage test” is considered as an indicative of product stability. That is accelerated storage test data provides an indication that the product is stable for at least two years at ambient temperature. Further, the FAO/WHO manual indicates storage at 54°C ± 2°C for 14 days as the default test conditions.
[0085] The “ambient sample” is the sample at the room temperature which is before subjecting to the accelerated storage test.
[0086] The “accelerated storage sample” is the sample after subjecting to the accelerated storage test.
[0087] The ambient sample of the suspension concentrate (SC) of the above Example 1 was subjected to the accelerated storage test to find out the product stability.
[0088] Table 2 shows the physical and chemical properties of the suspension concentrate (SC) of Example 1 before and after the accelerated storage test.

Table 2: Physical and chemical properties of the suspension concentrate (SC) of Example 1 before and after the accelerated storage test:

S. No. Tests Product specifications Ambient sample
(before) Accelerated storage sample tested @ 54±2°c for 14 days
(after)
1 Appearance off-white to beige colour suspension Complies Complies
2 Active Ingredient /content test % w/w Mesotrione Content: 11.40 – 12.60 12.0 11.96 (0.40%)
Tembotrione Content: 11.40 – 12.60 12.0 11.91 (0.75%)
3 Suspensibility
(% w/w) Mesotrione
Min. 70
98.80
96.77
Tembotrione Min. 70 98.76 95.72
4 Spontaneity of dispersion, % w/w Min. 70 98.62
98.59
5 Particle size distribution, µ d(90) Max. 15.0 9.0 11.7
6 Wet sieve passing through 75 micron % w/w Min. 98 99.89 99.85
7 Persistent foam after 1 min, mL Max. 40 15 15
8 Pourability % w/w as rinse residue
Max. 1.0
0.30
0.33
9 pH of 1% aq. suspension 3.0 – 6.0 3.5 3.7
Min. = Minimum and Max. = Maximum

[0089] The results in Table 2 show that the appearance of the ambient sample of the suspension concentrate (SC) before and after the accelerated storage test (@54±2°C for 14 days) remained the same that is ‘off-white to beige colour suspension’.
[0090] Further, the content of mesotrione and tembotrione was found to be 12% w/w and 12% w/w respectively before subjecting the ambient sample to the accelerated storage test. After subjecting the ambient sample to the accelerated storage test the content of mesotrione and tembotrione was found to be the almost same, that is 11.96% w/w and 11.91% w/w respectively. This indicates that the content of mesotrione and tembotrione was degraded only by 0.4% and 0.75% respectively and falls within the product specification range and hence the active ingredients are stable.
[0091] The suspensibility test and spontaneity of dispersion test was conducted for the ambient sample of the suspension concentrate (SC), before and after accelerated storage test. The results of the suspensibility test indicated that 98.80% w/w and 96.77% w/w of mesotrione, 98.76% w/w and 95.72% w/w of tembotrione are uniformly distributed in water after dilution. The spontaneity of dispersion test results showed that 98.62%w/w and 98.59%w/w of SC was dispersed uniformly and formed homogeneous suspension spontaneously.
[0092] The ambient sample of the suspension concentrate (SC) was tested for its particle size by particle size distribution test by using laser diffraction method using Malvern MS3000 and wet sieve passing test by using 75µ wet sieve. The particle size distribution test showed that particle size distribution of the ambient sample was d(90) is 9.00µ and the particle size distribution of the accelerated storage sample was found to be almost same that is d (90) is 11.7µ and wet sieve passing test showed passing of and 99.89% w/w and 99.85%w/w of particles of the SC through the 75µ wet sieve indicating the low particle size (11.7µ) of the SC. Therefore, both the tests confirm the low particle size (11.7µ) and no crystal growth after the accelerated storage test.
[0093] Tests such as persistent foam and pourability were conducted for the ambient sample of the suspension concentrate (SC), before and after accelerated storage test. The results indicated that persistent foam test showed low persistent foam of 15ml indicating the less froth formation and pourability test showed low rinse residue of 0.30 %w/w and 0.33%w/w indicating less wastage of the SC.
[0094] The pH of the ambient sample of the SC before subjecting it to the accelerated storage test was found to be 3.5. However, even after subjecting the ambient sample to the accelerated storage test the pH was found to be almost same, that is 3.7. This indicates that the suspension concentrate (SC) was adhering to the pH range of 3.0 – 6.0 which indicates that the SC is stable.
[0095] Further, the particle size distribution of suspension concentrate (SC) is directly related to the efficacy, dispersion stability, and required dosage of the combination. That is the smaller particle size (11.7µ) of the suspension concentrate (SC) of the present invention provide better dispersion stability, since small particle sizes enable the Brownian motion to dominate over gravitational force, provides a larger specific surface area, which will further increase the dissolution rate, adhesion, and penetrability to the target pest, improving the efficacy and bioavailability of the active ingredients which leads to the increased herbicidal activity.
[0096] In view of the above test results which showed that values of the tests remained almost same before and after accelerated storage test indicates that the SC is stable. Therefore, suspension concentrate (SC) of the present invention prepared in accordance with the above examples are extrapolated to be stable for 2 years.
[0097] The advantages of the suspension concentrate (SC) of the present invention include no long-term storage stability issues and no crystal growth problem, environmental friendly as water is the solvent, easy to handle and measure, provides improved safety while maintaining herbicidal efficacy.

Example 4: Field Tests
[0098] The suspension concentrate (SC) of Example 1 was tested for its biological activity and the results are shown in Tables 3 and 4 below:

Table 3: Field test results of the mesotrione + tembotrione suspension concentrate (SC) applied against major weeds in sugarcane at the Karnataka location in the Kharif season 2021.

Treatment Dosage Mean no. of weeds/0.25sq.mt area (25 DAA)
g a.i./ha SC
(g/mL/ha) Grasses Sedges Broad leaved weeds Total
Example 1
Mesotrione 12%+
Tembotrione 12%SC 60 + 60 500 1.33 1.77 1.33 4.43

Individual ingredients

Mesotrione 10%SC 60 600 8.83 7.20 7.17 23.2
Tembotrione 34.4% SC

60 142.85 10.00 7.30 7.17 24.47
Conventional Combinations Tembotrione
34.4%SC+
Tembotrione activator (Rapeseed fatty acid ester) + Atrazine 50%WP + (Tank-Mix) 120 + 50 286 + 2000+1000

4.22 3.20 2.17 9.59
Metribuzin 70%WP + 2,4-D Dimethyl Amine salt 58% SL (Tank Mix) 700 + 1305 1000 + 2250 2.06 2.87 3.33 8.26
Mesotrione 2.27% + Atrazine 22.7% SC (Pre-Mix) 79.45 + 794.5 3500 3.94 2.33 2 .17 8.44
Ametryn 80% WDG 2000 2500 2.67 3.47 3.50 9.64
Untreated check - - - 27.56 17.03 19.33 63.92
DAA- Days after application

[0099] From the above results, after 25 days of application of the suspension (SC) of the herbicide composition comprising mesotrione in an amount of 12% and tembotrione in an amount of 12%, the number of weeds were reduced to a greater extent (4.43 weeds/0.25sq.mt area) that is at least 16 times in comparison to the untreated check (without herbicide treatment) (63.92 weeds/sq.mt area).
[00100] Also, the results were better in comparison to the individual compounds Mesotrione 10%SC (23.2 weeds/0.25sq.mt area), Tembotrione 34.4% SC (24.47 weeds/0.25sq.mt area).
[00101] Also, the results were better in comparison to conventional tank mix combinations Tembotrione 34.4%SC + Tembotrione activator (Rapeseed fatty acid ester) + Atrazine 50%WP (9.59 weeds/0.25sq.mt area), Metribuzin 70%WP + 2,4-D Dimethyl Amine salt 58% SL (8.26 weeds/0.25sq.mt area), and the conventional pre-mix combination Mesotrione 2.27% + Atrazine 22.7% SC (8.44 weeds/0.25sq.mt area) and conventional individual active ingredient Ametryn 80% WDG (9.64 weeds/0.25sq.mt area).
[00102] As shown above, in the conventional tank mix combination such as Tembotrione 34.4%SC + Tembotrione activator (Rapeseed fatty acid ester) + Atrazine 50%WP, the tembotrione activator (Rapeseed fatty acid ester) additionally is always used along with the active ingredient tembotrione to achieve the better weed control. Whereas, in the present invention tembotrione activator is not used along with the active ingredient tembotrione for the weed control. That is, even in the absence of the tembotrione activator, the present invention surprisingly shows superior weed control (4.43 weeds/0.25sq.mt area) in comparison to the conventional tank mix combination Tembotrione 34.4%SC and Atrazine 50%WP which uses tembotrione activator (Rapeseed fatty acid ester) along with it (9.59 weeds/0.25sq.mt area).

Table 4: Field test results of the mesotrione + tembotrione SC applied against major weeds in sugarcane at the Karnataka location in the Kharif season 2021 (% Weed control relative to untreated check).

Treatment Dosage % Control over untreated check (25 DAA)
g a.i./ha SC
(g/mL/ha) Grasses Sedges Broad leaved weeds % Mean control
Example 1
Mesotrione 12%+
Tembotrione 12%SC 60 + 60 500 95.17 89.60 93.11 92.62
Individual ingredients Mesotrione 10%SC 60 600 67.96 57.92 62.90 62.79
Tembotrione 34.4% SC 60 142.85 63.71 57.13 62.90 61.24
Conventional combinations Tembotrione 34.4%SC+ Tembotrione activator (Rapeseed fatty acid ester) +Atrazine 50%WP (Tank-Mix) 120 + 50 286 +2000+ 1000 84.68 81.20 88.77 84.88
Metribuzin 70%WP + 2,4-D Dimethyl Amine salt 58% SL (Tank-Mix) 700 + 1305 1000 + 2250 92.52 83.14 82.77 84.14
Mesotrione 2.27% + Atrazine 22.7% SC (Pre-Mix) 875 3500 85.70 86.31 88.77 86.92
Ametryn 80% WDG 2000 2500 90.31 79.62 81.89 83.94
Untreated check - - - 0.00 0.00 0.00 0.00
DAA- Days after application

[00103] From the above results, the compositions comprising mesotrione and tembotrione formulated into SC resulted in more than 92% reduction of weeds in comparison to the untreated check. The percentage reduction of weeds by the present composition is higher than the individual compounds as well as conventional combinations.
[00104] From the test results shown above, it is evident that there is an unexpected and surprising result i.e., synergistic effect of the combination of mesotrione and tembotrione in the control of weeds in the sugarcane fields. As can be seen from Tables 3 to 4, the combined administration of mesotrione and tembotrione resulted in significant reduction in weeds population as compared to single administration of the individual herbicides. It is also evident that the combination preparation in accordance with the present invention exhibits a superior herbicidal effect as compared to other known herbicidal products available in the market.
[00105] The foregoing examples are merely illustrative and are not to be taken as limitations upon the scope of the invention. Various changes and modifications to the disclosed examples will be apparent to those skilled in the art. Such changes and modifications may be made without departing from the scope of the invention.

, Claims:1. An herbicide composition comprising
a. mesotrione;
b. tembotrione; and
c. one or more agriculturally acceptable excipients selected from the group comprising of a dispersing agent, a wetting agent, an anti-freezing agent, an anti-foaming agent, a biocide, a rheology modifier and a solvent.
2. The herbicide composition as claimed in claim 1, wherein the composition comprises mesotrione in an amount of from 0.1% to 30% w/w, tembotrione in an amount of from 0.1% to 30% w/w, dispersing agent in an amount of from 0.1% to 25% w/w, wetting agent in an amount of from 0.5% to 15% w/w, anti-freezing agent in an amount of from 6.0 % to 20% w/w, anti-foaming agent in an amount of from 0.1% to 5% w/w, biocide in an amount of from 0.1% to 5% w/w, rheology modifier in an amount of from 0.01% to 3% w/w and solvent in an amount of from 1.0% to 90% w/w.
3. The herbicide composition as claimed in claim 1, wherein the composition is formulated as a water-dispersible granule (WDG), a water-soluble granule (SG), a wettable powder (WP), a water-dispersible powder (WDP), a water-soluble powder (SP), a granule (GR), an encapsulated granule (CG), a fine granule (FG), a macrogranule (GG), a microgranule (MG), a suspension concentrate (SC), a water-soluble concentrate (SL), an emulsifiable concentrate (EC), an emulsion (EW), a micro-emulsion (ME), a flowable suspension (FS), a suspoemulsion (SE), ZC formulation (ZC), Soil Applied Granules (SAG), dustable powder (DP), a gel, a water-dispersible tablet (WT), a dispersible concentrate (DC), an oil-dispersion (OD) or a microencapsulated suspension (CS).
4. The herbicide composition as claimed in claim 1 or 3, wherein the composition is in the form of a suspension concentrate (SC).
5. The herbicide composition as claimed in claim 4, wherein the suspension concentrate (SC) comprises:
a) 0.1-30% mesotrione by weight;
b) 0.1-30% tembotrione by weight;
c) 0.1- 25 dispersing agent by weight;
d) 0.5-15% wetting agent by weight;
e) 6.0-20% anti-freezing agent by weight;
f) 0.1-5% anti-foaming agent by weight;
g) 0.1-5% biocide by weight;
h) 0.01-3% rheology modifier by weight; and
i) 1-90% solvent by weight.
6. The herbicide composition as claimed in claim 5, wherein the suspension concentrate (SC) comprises:
a) 12% mesotrione by weight;
b) 12% tembotrione by weight:
c) 4 % dispersing agent by weight:
d) 0.5% wetting agent by weight;
e) 10% anti-freezing agent by weight;
f) 0.5% anti-foaming agent by weight;
g) 0.1% biocide by weight;
h) 0.2% rheology modifier by weight; and
i) 60.7 % solvent by weight.
7. The herbicide composition as claimed in claims 1 or 6, wherein the dispersing agent is selected from the group comprising of polystyrenated acrylated co- polymer, random co-polymer of alcoxylated polyethylene glycol, lignosulphonates, ammonium salts of sulfonated naphthalene, salts of polyacrylic acids or sodium salt of naphthalene sulfonate formaldehyde condensate.
8. The herbicide composition as claimed in claim 1 or 6, wherein the wetting agent is selected from the group comprising of lignin derivatives, salts of polycarboxylic acids, salts of esters of sulfosuccinic acid, C12-15 ethoxylated alcohols, alkyl ether sulphates or sodium isopropyl naphthalene sulfonate.
9. The herbicide composition as claimed in claim 1 or 6, wherein the anti-freezing agent is selected from the group comprising of ethylene glycol, glycerine, urea or propylene glycol.
10. The herbicide composition as claimed in claim 1 or 6, wherein the anti-foaming agent is selected from the group comprising of perfluroalkylphosphonic acids or polydimethyl siloxane.
11. The herbicide composition as claimed in claim 1 or 6, wherein the biocide is selected from the group comprising of formaldehyde or 1,2-benzisothiazolin-3-one.
12. The herbicide composition as claimed in claim 1 or 6, wherein the rheology modifier is selected from the group comprising of hydrophobic fumed silica, bentonite, diatomaceous earth, montmorillonite or polysaccharide gel.
13. The herbicide composition as claimed in claim 1 or 6, wherein the solvent is selected from the group comprising of deionized (DI) water or demineralised water.