Abstract: The present disclosure relates to a composition and a formulation comprising active ingredients trifloxystrobin, difenoconazole and polymeric surfactant. Particularly, the present disclosure provides a suspension concentrate (SC) formulation comprising the active ingredients trifloxystrobin, difenoconazole and polymeric surfactant in combination with one or more excipients and a process for preparation thereof.
DESC:FIELD OF THE INVENTION
[0001] The present invention relates to the technical field of fungicides. In particular the present disclosure relates to a composition comprising combination of fungicides trifloxystrobin and difenoconazole, and polymeric surfactant(s); formulations and a process for preparing 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] Fungi, an extremely large and diverse group of eukaryotic microorganisms are responsible for a range of serious fungal diseases such as leaf blast, sheath blight, neck blast, powdery mildew, leaf spot, fruit rot, rust, anthracnose in crops.
[0004] To address problems associated with fungi infestation, researchers are trying to produce an extensive variety of active ingredients and active ingredient’s formulations effective in controlling the fungi. Chemical fungicides 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 decrease resistance development for active ingredients.
[0005] Propiconazole, difenoconazole, tricyclazole, azoxystrobin, tebuconazole, mancozeb, fludioxonil, picoxystrobin, kresoxim-methyl, metconazole and boscalid are compounds independently known in the art for their fungicidal potency. They are disclosed in ‘The Pesticide Manual’ 15th Edition, published 2009 by the British Crop Protection Council, and are also commercially available.
[0006] It is known that to seek and obtain registration for a new fungicide 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 fungicide when applied at the recommended level, also information about the recommended level of fungicide 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.
[0007] It is a common knowledge that with the use of a single fungicide over a period, the fungi develop resistance, rendering the particular fungicide ineffective for use against specific fungal diseases. Thus, on one hand even more stringent conditions are being placed on the type and use rate of fungicide, while on the other hand approved fungicides available in the art are becoming less and less effective over time in pests.
[0008] Due to such reasons including the lengthy and cost intensive process, resistance to single fungicide, combinations of known and approved fungicides are attempted.
[0009] Two-way combinations of difenoconazole with azoxystrobin, tebuconazole with trifloxystrobin are known in the art and are in commercial use.
[0010] However, certain fungi are becoming increasingly resistant to even a number of most widely used fungicides formulations with common combination of two ingredients available in the art. Hence, such combinations are also found to be ineffective in controlling fungi 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.
[0011] Thus, there still remains an unmet great need in the art for composition comprising combination of fungicides for providing environmentally safe, efficacious fungicide formulation which can show one or more of advantages such as stability, synergistic effect, faster onset of fungicide action, a broad-spectrum and longer-lasting action with phytotonic effect, reduced dosage of active ingredients, reduced application rate of the fungicide, reduce or delay the development of resistance and a process for preparing such fungicide formulation comprising the same.
SUMMARY OF THE INVENTION
[0012] The present invention provides a composition comprising combination of trifloxystrobin, difenoconazole and polymeric surfactant for providing fungicide formulation for overcoming one or more challenges in the existing art and providing one or more advantages such as stability, synergistic effect, faster onset of fungicide action, a broad-spectrum and longer-lasting action with phytotonic effect, reduced dosage of active ingredients, reduced application rate of the fungicide, reduce or delay the development of resistance.
[0013] In an aspect, the present invention provides a composition comprising combination of trifloxystrobin, difenoconazole and polymeric surfactant; and one or more inactive excipient(s).
[0014] In one aspect, the present disclosure provides a fungicide composition comprising trifloxystrobin in an amount of from about 0.1% to about 30% w/w, difenoconazole in an amount of from about 0.1% to about 45% w/w, and polymeric surfactant in an amount of from about 0.1% to about 25% w/w.
[0015] In another aspect, the present disclosure provides a fungicide formulation comprising trifloxystrobin, difenoconazole and polymeric surfactant.
[0016] In an aspect, the present invention provides a formulation comprising combination of trifloxystrobin, difenoconazole and polymeric surfactant; and one or more inactive excipient(s).
[0017] In one aspect, the present disclosure provides a fungicide formulation comprising trifloxystrobin in an amount of from about 0.1% to about 30% w/w, difenoconazole in an amount of from about 0.1% to about 45% w/w, and polymeric surfactant in an amount of from about 0.1% to about 25% w/w.
[0018] In another aspect, the fungicide formulation is selected from an oil-dispersion (OD), ZC formulation (ZC), suspension concentrate (SC), 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 water-soluble concentrate (SL), a flowable suspension (FS), soil applied granules (SAG), dustable powder (DP), a gel, a water-dispersible tablet (WT), a dispersible concentrate (DC) or a microencapsulated suspension (CS).
[0019] In one specific aspect, the fungicide formulation comprising trifloxystrobin, difenoconazole and polymeric surfactant is a suspension concentrate (SC).
[0020] In one aspect, the present disclosure provides a process for preparing suspension concentrate (SC) formulation comprising trifloxystrobin, difenoconazole and polymeric surfactant.
[0021] In one specific aspect, the process for preparing suspension concentrate (SC) formulation comprises the steps of:
a) adding active ingredients trifloxystrobin, difenoconazole, polymeric surfactant and one or more inactive excipient(s) in demineralised water and mixing for about 1 hour to about 2 hours to obtain a slurry;
b) passing the slurry through a mill for particle size reduction to obtain a milled slurry; and
c) charging the rheology modifier to the milled slurry and continuing to mix for about 4 hours to about 6 hours to obtain a homogeneous suspension concentrate (SC).
[0022] 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
[0023] 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.
[0024] 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.”
[0025] 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.
[0026] 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.
[0027] 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.
[0028] 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.
[0029] 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.
[0030] The headings and abstract of the invention provided herein are for convenience only and do not interpret the scope or meaning of the embodiments.
[0031] 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.
[0032] 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.
[0033] The present disclosure provides a composition comprising combination of fungicides trifloxystrobin, difenoconazole and polymeric surfactant(s), formulations therefore and process for preparing the same.
[0034] In one embodiment, the present disclosure provides a composition comprising fungicides trifloxystrobin and difenoconazole; and polymeric surfactant(s).
[0035] In one embodiment, the present disclosure provides a composition comprising combination of trifloxystrobin, difenoconazole and polymeric surfactant; and one or more inactive excipient(s).
[0036] In one embodiment, the present disclosure provides a composition comprising trifloxystrobin in an amount of from about 0.1% to about 30% w/w, difenoconazole in an amount of from about 0.1% to about 45% w/w, and polymeric surfactant in an amount of from about 0.1% to about 25% w/w.
[0037] In one embodiment, the present disclosure provides a formulation comprising fungicides trifloxystrobin and difenoconazole; and polymeric surfactant(s).
[0038] In one embodiment, the present disclosure provides a formulation comprising combination of trifloxystrobin, difenoconazole and polymeric surfactant; and one or more inactive excipient(s).
[0039] The present disclosure provides a fungicide formulation comprising composition provided in accordance with the present disclosure comprising trifloxystrobin in an amount from about 0.1% to about 30 % w/w, difenoconazole in an amount from about 0.1% to about 45% w/w, and polymeric surfactant in an amount from about 0.1% to about 25% w/w.
[0040] Trifloxystrobin chemically known as methyl(aE)-a-(methoxyimino)-2-[[[[(1E)-1-[3-(trifluoromethyl)phenyl]ethylidene]amino]oxy]methyl]benzeneacetate is a methoxyiminoacetate strobilurin fungicides. It is a systemic fungicide and is a potent inhibitor of fungal spore germination and mycelial growth. It acts by inhibiting mitochondrial electron transport (MET III) by inhibiting ubiquinol oxidase at the Qo (quinone outside) binding site on cytochrome bc1 (complex III), causing respiratory problem in fungi.
[0041] Difenoconazole chemically known as
1-[[2-[2-chloro-4-(4-chlorophenoxy)phenyl]-4-methyl-1,3-dioxolan-2-yl]methyl]-1H-1,2,4-triazole is a conazole fungicide. It is a systemic fungicide and it acts by inhibiting sterol demethylation, preventing the development of the fungus by inhibiting cell membrane ergosterol biosynthesis.
[0042] Polymeric surfactants are surfactants that consist of polymers in both head and tail groups. The polymers can be a block copolymer or a graft copolymer. The graft copolymers are macromolecules which consist of a main polymer chain or backbone covalently bonded to one or more side chains with a chemical composition different from that of the polymer chain or backbone.
[0043] The polymeric surfactant used in the composition or formulations of the present invention acts as both dispersant agent and anti-crystalline agent.
[0044] The polymeric surfactants comprised in the composition or formulation in accordance with the present invention are selected from the group consisting of but not limited to acrylate copolymers such as 2-acrylamide-2-methyl-1-propanesulfonic acid and alkyl methacrylamide, alkyl methacrylate or alkyl acrylate, poly (allylamine)-supported phases, poly(ethyleneimine), modified acrylic copolymer such as hydrophobically modified polyacrylate, modified styrene acrylic copolymer, hydrophilic methyl methacrylate graft copolymer, and acrylic graft copolymer (AtloxTM 4913 also known as polymethyl methacrylate-polyethylene glycol graft copolymer or acrylic copolymer solution).
[0045] Polymeric surfactants are advantageous over conventional anionic or non ionic surfactants where polymeric surfactants has high molecular weight, large repulsive barrier, multiple anchoring groups per molecule and strong surface adsorption thereby providing excellent particle stability due to steric stabilisation, prevent coalescence and agglomeration due to large repulsive barrier and provide superior interaction between surfactant and substrate due to multiple anchoring points of polymeric surfactants. In contrast, the conventional anionic or non ionic surfactants have lower molecular weight, small repulsive barrier, few anchoring groups per molecule and weaker surface adsorption.
[0046] The composition or formulation in accordance with the present disclosure can comprise trifloxystrobin, difenoconazole, polymeric surfactant in a different range of amounts effective to treat desired crops infested by different fungus.
[0047] In certain embodiments, the composition or formulation of the present invention comprises trifloxystrobin, difenoconazole and polymeric surfactant in total amount ranging from about 1% to about 60% by weight.
[0048] In certain embodiments, the fungicide composition comprises, by weight, from about 0.1% to about 30% w/w of trifloxystrobin, from about 0.1% to about 45% w/w of difenoconazole and from about 0.1% to about 25.0% w/w of polymeric surfactant.
[0049] In certain embodiments, the fungicide formulation comprises, by weight, from about 0.1% to about 30% w/w of trifloxystrobin, from about 0.1% to about 45% w/w of difenoconazole and from about 0.1% to about 25.0% w/w of polymeric surfactant.
[0050] In various embodiments, the fungicide formulation comprising the combination of trifloxystrobin, difenoconazole and polymeric surfactant can be provided in liquid or solid form.
[0051] In an embodiment, the solid or liquid formulation comprising active ingredient trifloxystrobin, difenoconazole and polymeric surfactant is combined with one or more excipients. The excipient can be an inactive excipient known in the art of agrochemicals.
[0052] Suitable excipients will depend upon such factors as the type of formulation and the manner of the end use of the formulation, and will be known to a person skilled in the art.
[0053] In some embodiments, the inactive excipients can be selected from the group comprising of but not limited to a wetting agent, an anti-freezing agent, an anti-foaming agent, a biocide, a rheology modifier, a solvent, an anti-crystalline agent, an emulsifier, a pH stabilizer, a spreading agent, a dispersing 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.
[0054] In a preferred embodiment, the inactive excipients are selected from the group comprising of a wetting agent, an anti-freezing agent, an anti-foaming agent, a biocide, a rheology modifier and a solvent.
[0055] 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, salts of polycarboxylic acids, salts of esters of sulfosuccinic acid, octyl phenol ether sulphate, anionic phosphate esters, disodium laureth sulfosuccinate, disodium hexadecyl sulphate, diisodecyl sodium sulfosuccinate, alkylnaphthalenesulfonates, alkylbenzenesulfonates, alkylpolyglycol ether sulfonates, alkyl ether phosphates, C12-15 ethoxylated alcohols, alcohol ethoxylate (AtloxTM 4894 also known as polyoxyethylene alkyl ether or nonionic proprietary surfactant blend), alkyl ether sulfates and alkyl sulfosuccinic monoesters or mixtures thereof.
[0056] The wetting agent can be present in an amount ranging from about 0.5 % to about 15% w/w of the composition or formulation.
[0057] Suitable anti-freezing agents include organic solvents which are completely miscible with water, such as ethylene glycol, glycerine, urea, propylene glycol or mixtures thereof.
[0058] The anti-freezing agent is present in an amount of from about 1.0% to about 20% w/w of the composition or formulation.
[0059] Suitable anti-foaming agents are selected from the group comprising of perfluroalkylphosphonic acids, polydimethyl siloxane or mixture thereof.
[0060] The anti-foaming agent can be present in an amount ranging from about 0.1% to about 5% w/w of the composition or formulation.
[0061] The biocide can be selected from formaldehyde, 1,2-benzisothiazolin-3-one or mixtures thereof
[0062] The biocide is present in an amount of from about 0.1% to about 5% w/w of the composition or formulation.
[0063] The rheology modifier can be selected from hydrophobic fumed silica, bentonite, diatomaceous earth, montmorillonite, attapulgites or hydroxymethyl cellulose, xanthan gum, polyvinyl alcohol, organic derivative of hectorite clay, benton, thickening silica, hydrated clay minerals, magnesium aluminium silicates, polysaccharide gel or mixtures thereof.
[0064] The rheology modifier can be present in an amount ranging from about 0.01 % to about 3% w/w of the composition or formulation.
[0065] Suitable solvents for use in the formulation can be selected from all customary organic solvents which dissolve one or more of the active ingredients of the fungicide formulation. Suitable aqueous and non aqueous organic solvents for the compounds trifloxystrobin and difenoconazole are known in the art. Preferred solvents can be selected from but not limiting to, deionized (DI) water, demineralised water, dimethylsulfoxide (DMSO), 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) or mixtures thereof.
[0066] The solvent can be present in an amount ranging from about 1% to about 90% w/ w of the composition or formulation.
[0067] The anti-crystalline agent can be selected from without limitation vinyl pyrrolidone polymer, polyvinyl alcohol, acrylic graft copolymer, sodium polyacrylate co-polymer or mixtures thereof.
[0068] The anti-crystalline agent can be present in an amount ranging from about 0% to about 25% w/w of the composition or formulation.
[0069] Suitable emulsifier can be selected from ionic or non-ionic emulsifier or surfactant. The ionic substances can be selected from cationic, or anionic or combination thereof.
[0070] The ionic emulsifier or surfactant can be selected from the group consisting of but not limited 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, polycarboxylate or mixtures thereof.
[0071] The non-ionic emulsifier or surfactant can be selected from the group consisting of but not limited 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 or mixtures thereof.
[0072] The emulsifier can be present in an amount ranging from about 0% to about 20 % w/w of the composition or formulation.
[0073] The pH stabilizer can be selected without limitation 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 or mixtures thereof.
[0074] The pH stabilizer can be present in an amount ranging from about 0% to about 10% w/w of the composition or formulation.
[0075] Suitable spreading agents can be selected without limitation from the group comprising of polyoxyethylene alkyl ether, trisiloxane ethoxylate, polysorbates, ethoxylated tristyrylphenol phosphate, tridecyl alcohol ethoxylate, sodium lauryl sulphate, sodium methyl oleoyl taurate or mixtures thereof.
[0076] Spreading agents can be present in an amount ranging from about 0% to about 10 % w/w of the composition or formulation.
[0077] The dispersing agent can be selected without limitation 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, polystyrenated acrylated co- polymer, random co-polymer of alcoxylated polyethylene glycol, polymethyl methacrylate-polyethylene glycol graft copolymer, ammonium salts of sulfonated naphthalene, salts of polyacrylic acids, salts of phenol sulfonic acids or mixtures thereof.
[0078] The dispersing agent can be present in an amount ranging from about 0% to about 25% w/w of the composition or formulation.
[0079] Suitable inert carrier(s) for use in the formulation 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, synthetic granules of inorganic and organic ground materials or mixtures thereof.
[0080] The inert carrier can be present in an amount ranging from about 0% to about 90% w/w of the composition or formulation.
[0081] The stabilizing agent can be selected without limitation from 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 gamma butyrolactone, butylated hydroxyl toluene and its derivatives, epichlorhydrin, quinone derivatives, hydrazine hydrates and its derivatives, glycols and its derivatives or mixtures thereof.
[0082] The stabilizing agent can be present in an amount ranging from about 0% to about 10% w/w of the composition or formulation.
[0083] The anti-caking agent can be selected from but not limited to kaolin clay, precipitate silica, colloidal silica, talc, gypsum, silicates, calcium carbonate, hydrophobic fumed silica, magnesium carbonate, magnesium sulphate or mixtures thereof.
[0084] The anti-caking agent can be present in an amount ranging from about 0% to about 10% w/w of the composition or formulation.
[0085] Suitable antioxidant is butylated hydroxytoluene.
[0086] The antioxidant is present in an amount from about 0% to about 5% w/w of the composition or formulation.
[0087] Suitable capsule forming agent can be selected from the group comprising of methylene diisocyanate, toluene diisocyanate or mixtures thereof.
[0088] The capsule forming agent can be present in an amount ranging from about 0% to about 5% w/w of the composition or formulation.
[0089] Suitable quenching agent can be selected from the group comprising of ammonia solution (25%), ethylene diamine (EDA), ethanol-amine, butadiene or mixture thereof.
[0090] The quenching agent can be present in an amount from about 0% to about 10% w/w of the composition or formulation.
[0091] Suitable super spreader can be selected from the group comprising of modified trisiloxane, trisiloxane alkoxylate or mixture thereof.
[0092] The super spreader can be present in an amount ranging from about 0% to about 10% w/w of the composition or formulation.
[0093] In certain embodiments, the disclosed fungicide formulation comprising the combination of trifloxystrobin, difenoconazole and polymeric surfactant can be selected from oil-dispersion (OD), ZC formulation (ZC), suspension concentrate (SC), 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 water-soluble concentrate (SL), a flowable suspension (FS), soil applied granules (SAG), dustable powder (DP), a gel, a water-dispersible tablet (WT), a dispersible concentrate (DC) or a microencapsulated suspension (CS).
[0094] In a preferred embodiment, the fungicide formulation comprising the combination of trifloxystrobin, difenoconazole and polymeric surfactant is a suspension concentrate (SC).
[0095] In one embodiment, the suspension concentrate (SC) formulation comprises:
a) about 0.1% to about 30.0% trifloxystrobin by weight of the formulation;
b) about 0.1% to about 45.0% difenoconazole by weight of the formulation;
c) about 0.1% to about 25.0% polymeric surfactant by weight of the formulation;
d) about 0.5% to about 15.0% wetting agent by weight of the formulation;
e) about 1.0 % to about 20.0% anti-freezing agent by weight of the formulation;
f) about 0.1% to about 5.0% antifoaming agent by weight of the formulation;
g) about 0.1 % to about 5.0% biocide by weight of the formulation;
h) about 0.01% to about 3.0% rheology modifier by weight of the formulation; and
i) about 1.0% to about 90.0% solvent by weight of the formulation.
[0096] In another embodiment, the suspension concentrate (SC) formulation comprises:
a) about 0.1% to about 30.0% trifloxystrobin by weight of the formulation;
b) about 0.1% to about 45.0% difenoconazole by weight of the formulation;
c) about 0.1% to about 25.0% polymeric surfactant by weight of the formulation selected from the group consisting of acrylate copolymers such as 2-acrylamide-2-methyl-1-propanesulfonic acid and alkyl methacrylamide, alkyl methacrylate or alkyl acrylate, poly (allylamine)-supported phases, poly(ethyleneimine), modified acrylic copolymer such as hydrophobically modified polyacrylate, modified styrene acrylic copolymer, hydrophilic methyl methacrylate graft copolymer, acrylic graft copolymer or mixtures thereof;
d) about 0.5% to about 15.0% wetting agent by weight of the formulation selected from the group comprising alkyl phenol ethoxylate, alkyl naphthalene sulfonates, polyoxyethoxylated fatty alcohols, alcohol ethoxylate or mixtures thereof;
e) about 1.0% to about 20.0% anti-freezing agent by weight of the formulation selected from the group comprising ethylene glycol, glycerine, urea, propylene glycol or mixtures thereof;
f) about 0.1% to about 5.0% antifoaming agent by weight of the formulation selected from the group comprising perfluroalkylphosphonic acids, polydimethyl siloxane or mixture thereof;
g) about 0.1 % to about 5.0% biocide by weight of the formulation selected from the group comprising formaldehyde, 1,2-benzisothiazolin-3-one or mixtures thereof;
h) about 0.01% to about 3.0% rheology modifier by weight of the formulation selected from the group comprising hydrophobic fumed silica, bentonite, hydroxymethyl cellulose, xanthan gum, polysaccharide gel or mixtures thereof; and
i) about 1.0% to about 90.0% solvent by weight of the formulation selected from the group comprising deionized (DI) water, dimethylsulfoxide (DMSO), demineralised water or mixtures thereof.
[0097] In one embodiment, the present disclosure provides process for preparing suspension concentrate (SC) formulation comprising the steps of:
a) adding active ingredients trifloxystrobin, difenoconazole, polymeric surfactant and one or more inactive excipient(s) in demineralised water and mixing for about 1 hour to about 2 hours to obtain a slurry;
b) passing the slurry through a mill for particle size reduction to obtain a milled slurry; and
c) charging the rheology modifier to the milled slurry and continuing to mix for about 4 hours to about 6 hours to obtain a homogeneous suspension concentrate (SC).
[0098] In one embodiment the mill for particle size reduction can be a bead mill with cold water circulation.
[0099] In one embodiment, the inactive excipients are selected from the group comprising of a wetting agent, an anti-freezing agent, an anti-foaming agent, a biocide, a rheology modifier and a solvent.
[00100] 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 fungicidal action, better efficacy, long duration of control with phytotonic effect, better control of broad spectrum of fungi 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 fungicidal efficacy.
[00101] The fungicide formulation according to the present disclosure can be advantageously applied for the protection of crops such as rice, chilli, soybean, fruits and vegetables.
[00102] In specific embodiments, the fungicide formulation in accordance with the present disclosure can be applied for protection of rice, chilli and soybean.
[00103] The fungicide formulation of the present disclosure can control phytopathogenic fungi such as ascomycetes, basidiomycetes, chytridiomycetes, deuteromycetes, oomycetes, plasmodiophoromycetes and zygomycetes by one time application.
[00104] The fungicide formulation of the present disclosure acts against the major diseases leaf blast, sheath blight, neck blast, powdery mildew, leaf spot, fruit rot and rust by one time application.
[00105] The fungicide formulation of the present invention can be applied to the fungi in a variety of ways, at various application timing and at various concentrations.
[00106] In one embodiment, the fungicide formulation of the present disclosure is applied to the fungi by foliar application. The application of the fungicide 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 trifloxystrobin, difenoconazole, polymeric surfactant can vary over a wide range, for example from 1 to 500g/ml per hectare (g/ml/ha).
[00107] In one embodiment, the formulation provided in accordance with the present disclosure can be applied at the application rate ranging from 450 to 500g/ml/ha.
[00108] The fungicide formulation thereof can be applied in a single treatment or in several treatments (sequential application).
EXAMPLES
[00109] 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 1-3.
Suspension Concentrate (SC) Formulation of the present invention.
I. Preparation of the suspension concentrate (SC) formulation:
1. Composition:
[00110] As per some specific exemplary embodiments suspension concentrate (SC) formulation was prepared with composition as per Table 1:
Table 1: Composition for suspension concentrate (SC) formulation of the present invention.
Ingredients Example 1 Example 2 Example 3
% w/w % w/w % w/w
Trifloxystrobin 10. 0 7.0 20.0
Difenoconazole 12.5 20.0 25.0
Polymeric surfactant
Acrylic graft copolymer
(AtloxTM 4913) 5.0 3.0 6.0
Alcohol ethoxylate (AtloxTM 4894) 3.0 2.5 3.0
Propylene glycol 5.0 5.0 5.0
Polydimethyl siloxane 1.0 0.5 0.8
1,2-benzisothiazolin-3-one 0.1 0.1 0.2
Polysaccharide Gel 0.3 0.25 0.18
Demineralised water QS QS QS
Total 100.00 100.00 100.00
2. Process for preparing the suspension concentrate (SC):
The active ingredients trifloxystrobin, difenoconazole and a polymeric surfactant an acrylic graft copolymer (AtloxTM 4913), and other inactive excipients alcohol ethoxylate (AtloxTM 4894), propylene glycol, polydimethyl siloxane, 1,2-benzisothiazolin-3-one and demineralised water as mentioned in Examples 1 to 3 in Table 1 were added into the dry pre-mixing vessel fitted with homogenizer and all the ingredients were mixed for 1 hour 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 as mentioned in Examples 1 to 3 were added to the milled slurry and continued to mix for about 4 hours to about 6 hours to obtain a homogeneous suspension concentrate (SC).
II. Accelerated Storage test (Stability Study):
[00111] 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.
[00112] The “ambient sample” is the sample at the room temperature which is before subjecting to the accelerated storage test.
[00113] The “accelerated storage sample” is the sample after subjecting to the accelerated storage test.
[00114] The ambient sample of the suspension concentrate (SC) formulation of the above Example 1 was subjected to the accelerated storage test to find out the product stability.
[00115] 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 White to off-white colour suspension Complies Complies
2 Active Ingredient /content test % w/w Trifloxystrobin Content: 9.50 – 10.50 10. 0 9.98 (0.2%*)
3 Difenoconazole Content: 11.875 – 13.125 12.5 12.42 (0.6%*)
4 Suspensibility
(% w/w) Trifloxystrobin
Min. 70
98.40
98.38
5 Difenoconazole Min. 70 99.26 99.11
6 Wet sieve passing through 75 micron % w/w Min. 98 99.98 99.98
7 Spontaneity of dispersion, % w/w Min. 70 98.55
98.49
8 Persistent foam after 1 min, mL Max. 40 15 15
9 pH of 1% aq. suspension 5.0 – 8.0 6.37 6.45
10 Pourability % w/w as rinse residue
Max. 1.0
0.42
0.51
11 Particle size distribution, µ d(90) Max. 15.0 8.0 10.2
Min. = Minimum and Max. = Maximum
[00116] 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 ‘white to off white color suspension’.
[00117] Further, the content of trifloxystrobin and difenoconazole was found to be 10% w/w and 12.5% 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 trifloxystrobin and difenoconazole was found to be the almost same, that is 9.98% w/w and 12.42% w/w respectively. This indicates that the content of trifloxystrobin and difenoconazole was degraded only by 0.2% and 0.6% respectively and falls within the product specification range and hence the active ingredients in the formulation are stable.
[00118] The pH of the ambient sample of the SC formulation before subjecting it to the accelerated storage test was found to be 6.37. However, even after subjecting the ambient sample to the accelerated storage test the pH was found to be almost same, that is 6.45. This indicates that the suspension concentrate (SC) was adhering to the pH range of 5.0 – 8.0 which indicates that the formulation is stable.
[00119] 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 0.42%w/w and 0.51%w/w indicating less wastage of the formulation.
[00120] 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 98.40% w/w and 98.38% w/w of trifloxystrobin, 99.26% w/w and 99.11% w/w of difenoconazole are uniformly distributed in water after dilution. The spontaneity of dispersion test results showed that 98.55%w/w and 98.49%w/w of formulation was dispersed uniformly and formed homogeneous suspension spontaneously.
[00121] The ambient sample of the suspension concentrate (SC) formulation 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 8.00µ and the particle size distribution of the accelerated storage sample was found to be almost same that is d (90) is 10.2µ and wet sieve passing test showed passing of 99.98%w/w of particles of the formulation through the 75µ wet sieve indicating the low particle size (10.2µ) of the formulation. Therefore, both the tests confirm the low particle size (10.2µ) and no crystal growth after the accelerated storage test.
[00122] Due to low melting point and slight water solubility of both the active ingredients, trifloxystrobin (72.9°C and 0.6 mg/L) and difenoconazole (76°C and 15 mg/L), the conventional suspension concentrate formulation (SC) shows huge crystal growth (>45?) after accelerated heat stability study at 54°C for 2 weeks, as the actives slowly starts melting at 54°C and combine with water resulting in huge crystals. These crystals are large enough to clog the spray equipment leading to non-homogenous spray and poor bio-efficacy.
[00123] Also, due to slight water solubility of both active ingredients, trifloxystrobin (0.6 mg/L) and difenoconazole (15 mg/L), the conventional suspension concentrate formulation (SC) exhibit ostwald ripening, which refers to the phenomena in which smaller particles in solution dissolve and deposit on larger particles in order to reach a more thermodynamically stable state. The small particles decrease in size until they disappear and large particles grow even larger. This shrinking and growing of particles will result in a larger mean diameter of a particle size distribution.
[00124] In contrast, the suspension concentrate (SC) formulation of the present invention shows low particle size of 10.2µ and no crystal growth even after the accelerated heat stability study at 54°C for 2 weeks, which is due to the addition of polymeric surfactant along with the active ingredients trifloxystrobin, difenoconazole in the suspension concentrate (SC) formulation of the present invention.
[00125] Due to the number of multiple anchoring points of polymeric surfactants, the polymeric surfactants binds to the active ingredients trifloxystrobin and difenoconazole and create the repulsion between the particles due to the mechanism referred to as steric stabilization, the steric stabilization absorbs a layer of a polymer on the particles to prevent them from getting close in the range of attractive forces thereby avoiding the particle size growth and formulation breakdown mechanisms such as ostwald ripening, flocculation and/or coalescence and hence, acts as a dispersing agent.
[00126] Further, the particle size distribution of suspension concentrate (SC) formulation is directly related to the efficacy, dispersion stability, and required dosage of the combination. That is the smaller particle size (10.2µ) 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 formulation which leads to the increased fungicidal activity.
[00127] Similarly, the polymeric surfactant binds and covers the active ingredients completely thereby avoiding melting of the actives which were combining with water and were forming the crystal. Therefore, the polymeric surfactant of the present invention acts as an anti-crystalline agent.
[00128] 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 formulation 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.
[00129] 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 fungicidal efficacy.
Example 4.
Field Tests.
[00130] The suspension concentrate (SC) of Example 1 was tested for its biological activity and the results are shown in Tables 3 to 6 below:
Table 3: Field test results of the Formulation of Example 1 applied against neck blast of rice at Mandya, Karnataka location in the Kharif season 2020.
Treatment Dosage % Disease infection %
control over UTC
g a.i./ha Formulation (g/ml/ha) Before 12 DAA
Example 1 Formulation 50 + 62.5 500 2.61 7.90 81.83
Trifloxystrobin 25%WG 50 200 2.95 12.60 71.03
Difenoconazole 25%EC 62.5 250 2.50 25.40 41.60
Azoxystrobin 18.2 + Difenoconazole 11.4%SC 91+ 57 500 2.70 18.90 56.55
Untreated check - - 3.40 43.50 0
DAA- Days after application
[00131] As seen from the above results, 12 days after application of the suspension concentrate (SC) of the fungicide formulation of Example 1 at the application rate of 500 g/ml per hectare (g/ml/ha) was found to be most effective treatment which reduced the neck blast incidence by 81.83% in comparison to the untreated check.
[00132] The results were better in comparison to the individual compounds trifloxystrobin and difenoconazole. That is the registered formulation of trifloxystrobin 25% WG alone at the application rate of 200 g/ml per hectare reduced the neck blast incidence only by 71.03%. And the registered formulation of difenoconazole 25% EC alone at the application rate of 250 g/ml per hectare reduced the neck blast incidence only by 41.60%.
[00133] Further, the results exhibited by the SC formulation of the present invention were better in comparison to the conventional combinations available in the market azoxystrobin 18.2 + difenoconazole 11.4%SC. That is azoxystrobin 18.2 + difenoconazole 11.4% SC, at the application rate of 500 g/ml per hectare reduced the neck blast incidence only by 56.55% which is 25.28% lesser than the neck blast reduction of the present invention (81.83%).
[00134] Similarly, the results of Tables 4, 5 and 6 shown below presents that the formulation of Example 1 of the present invention resulted in greater than 92% reduction of leaf blast disease, and greater than 87% control of sheath blast disease, also greater than 88% control of chilli powdery mildew disease in comparison to the untreated check. Also, the percentage control of leaf blast disease, sheath blast disease and chilli powdery mildew disease by the present composition and the formulation is higher than the individual compounds as well as conventional compositions.
Table 4: Field test results of the Formulation of Example 1 applied against leaf blast disease of rice at Mandya, Karnataka location in the Kharif season 2020.
Treatment Dosage % Disease infection %
control over UTC
g a.i./ha Formulation (g/ml/ha) Before 14 DAA
Example 1 Formulation 50 + 62.5 500 5.30 1.90 92.50
Trifloxystrobin 25%WG 50 200 3.80 3.80 85.03
Difenoconazole 25%EC 62.5 250 5.10 8.90 64.96
Azoxystrobin 18.2 + Difenoconazole 11.4%SC 91+ 57 500 2.90 4.60 85.82
Untreated check - - 5.20 25.40 0.00
DAA- Days after application
Table 5: Field test results of the Example 1 applied against sheath blight disease of rice at Mandya, Karnataka location in the Kharif season 2020.
Treatment Dosage % Disease infection %
control over UTC
g a.i./ha Formulation (g/ml/ha) Before 15 DAA
Example 1 Formulation 50 + 62.5 500 4.66 2.32 87.74
Trifloxystrobin 25%WG 50 200 3.09 4.88 74.22
Difenoconazole 25%EC 62.5 250 4.37 5.12 72.95
Azoxystrobin 18.2 + Difenoconazole 11.4%SC 91+ 57 500 3.42 4.15 78.07
Untreated check - - 3.72 18.93 0
DAA- Days after application
Table 6: Field test results of the Formulation of Example 1 applied against chilli powdery mildew disease of rice at Guntur, Andhra Pradesh location in the Rabi season 2020.
Treatment Dosage % Disease infection %
control over UTC
g a.i./ha Formulation (g/ml/ha) Before 12 DAA
Example 1 Formulation 50 + 62.5 500 2.10 2.47 88.97
Trifloxystrobin 25%WG 50 200 2.51 5.73 74.41
Difenoconazole 25%EC 62.5 250 1.06 6.87 69.33
Azoxystrobin 18.2 + Difenoconazole 11.4%SC 91+ 57 500 2.13 4.25 81.02
Untreated check - - 2.16 22.40 0
DAA- Days after application
[00135] Accordingly, 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 ingredients trifloxystrobin, difenoconazole and a polymeric surfactant in the reduction of neck blast disease, leaf blast disease, sheath blast disease and chilli powdery mildew disease in the rice fields. As can be seen from Tables 3 to 6, the combined application of trifloxystrobin, difenoconazole and a polymeric surfactant resulted in significant reduction in the neck blast disease, leaf blast disease, sheath blast disease and chilli powdery mildew disease as compared to application of the individual fungicides. It is also evident that the combination in accordance with the present invention exhibits a superior fungicidal effect as compared to other known registered fungicide combination products available in the market.
[00136] 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. A fungicide composition comprising
a) trifloxystrobin;
b) difenoconazole; and
c) polymeric surfactant.
2. The fungicide composition as claimed in claim 1, wherein the composition comprises one or more inactive excipients.
3. The fungicide composition as claimed in claim 2, wherein inactive excipients are selected from the group comprising of a wetting agent, an anti-freezing agent, an anti-foaming agent, a biocide, a rheology modifier and a solvent.
4. The fungicide composition as claimed in claim 1, wherein the composition comprises trifloxystrobin in an amount of from 0.1% to 30%w/w, difenoconazole in an amount of from 0.1% to 45% w/w, and polymeric surfactant in an amount of from 0.1% to 25% w/w.
5. A fungicide formulation comprising the active ingredients trifloxystrobin, difenoconazole, polymeric surfactant.
6. The fungicide formulation as claimed in claim 5, wherein the formulation comprises one or more inactive excipients.
7. The fungicide formulation as claimed in claim 6, wherein inactive excipients are selected from the group comprising of a wetting agent, an anti-freezing agent, an anti-foaming agent, a biocide, a rheology modifier and a solvent.
8. The fungicide formulation as claimed in claim 5, wherein the formulation comprises trifloxystrobin in an amount of from 0.1% to 30%w/w, difenoconazole in an amount of from 0.1% to 45% w/w, and polymeric surfactant in an amount of from 0.1% to 25% w/w.
9. The fungicide formulation as claimed in claim 5, wherein the formulation is selected from oil-dispersion (OD), ZC formulation (ZC), suspension concentrate (SC), 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 water-soluble concentrate (SL), a flowable suspension (FS), soil applied granules (SAG), dustable powder (DP), a gel, a water-dispersible tablet (WT), a dispersible concentrate (DC) or a microencapsulated suspension (CS).
10. The fungicide formulation as claimed in claim 9, wherein the formulation is a suspension concentrate (SC).
11. The fungicide formulation as claimed in claim 10, wherein the suspension concentrate (SC) comprises:
a) 0.1% to 30.0% trifloxystrobin by weight of the formulation;
b) 0.1% to 45.0% difenoconazole by weight of the formulation;
c) 0.1% to 25.0% polymeric surfactant by weight of the formulation;
d) 0.5% to 15.0% wetting agent by weight of the formulation;
e) 1.0 % to 20.0% anti-freezing agent by weight of the formulation;
f) 0.1% to 5.0% antifoaming agent by weight of the formulation;
g) 0.1 % to 5.0% biocide by weight of the formulation;
h) 0.01% to 3.0% rheology modifier by weight of the formulation; and
i) 1.0% to 90.0% solvent by weight of the formulation.
12. The fungicide formulation as claimed in claim 11, wherein the suspension concentrate (SC) comprises:
a) 0.1% to 30.0% trifloxystrobin by weight of the formulation;
b) 0.1% to 45.0% difenoconazole by weight of the formulation;
c) 0.1% to 25.0% polymeric surfactant by weight of the formulation selected from the group consisting of acrylate copolymers such as 2-acrylamide-2-methyl-1-propanesulfonic acid and alkyl methacrylamide, alkyl methacrylate or alkyl acrylate, poly (allylamine)-supported phases, poly(ethyleneimine), modified acrylic copolymer such as hydrophobically modified polyacrylate, modified styrene acrylic copolymer, hydrophilic methyl methacrylate graft copolymer, acrylic graft copolymer or mixtures thereof;
d) 0.5% to 15.0% wetting agent by weight of the formulation selected from the group comprising alkyl phenol ethoxylate, alkyl naphthalene sulfonates, polyoxyethoxylated fatty alcohols, alcohol ethoxylate or mixtures thereof;
e) 1.0% to 20.0% anti-freezing agent by weight of the formulation selected from the group comprising ethylene glycol, glycerine, urea, propylene glycol or mixtures thereof;
f) 0.1% to 5.0% antifoaming agent by weight of the formulation selected from the group comprising perfluroalkylphosphonic acids, polydimethyl siloxane or mixture thereof;
g) 0.1 % to 5.0% biocide by weight of the formulation selected from the group comprising formaldehyde, 1,2-benzisothiazolin-3-one or mixtures thereof;
h) 0.01% to 3.0% rheology modifier by weight of the formulation selected from the group comprising hydrophobic fumed silica, bentonite, hydroxymethyl cellulose, xanthan gum, polysaccharide gel or mixtures thereof; and
i) 1.0% to 90.0% solvent by weight of the formulation selected from the group comprising deionized (DI) water, dimethylsulfoxide (DMSO), demineralised water or mixtures thereof.
13. A process for preparing the suspension concentrate (SC) as claimed in claim 11, the process comprising:
a) adding active ingredients trifloxystrobin, difenoconazole, polymeric surfactant and one or more inactive excipient(s) in demineralised water and mixing for about 1 hour to about 2 hours to obtain a slurry;
b) passing the slurry through a mill for particle size reduction to obtain a milled slurry; and
c) charging the rheology modifier to the milled slurry and continuing to mix for about 4 hours to about 6 hours to obtain a homogeneous suspension concentrate (SC).
14. The process for preparing the suspension concentrate (SC) as claimed in claim 13, wherein inactive excipients are selected from the group comprising of a wetting agent, an anti-freezing agent, an anti-foaming agent, a biocide, a rheology modifier and a solvent.
| # | Name | Date |
|---|---|---|
| 1 | 202121055737-STATEMENT OF UNDERTAKING (FORM 3) [01-12-2021(online)].pdf | 2021-12-01 |
| 2 | 202121055737-PROVISIONAL SPECIFICATION [01-12-2021(online)].pdf | 2021-12-01 |
| 3 | 202121055737-FORM 1 [01-12-2021(online)].pdf | 2021-12-01 |
| 4 | 202121055737-DECLARATION OF INVENTORSHIP (FORM 5) [01-12-2021(online)].pdf | 2021-12-01 |
| 5 | 202121055737-FORM-26 [11-02-2022(online)].pdf | 2022-02-11 |
| 6 | 202121055737-Proof of Right [11-05-2022(online)].pdf | 2022-05-11 |
| 7 | 202121055737-RELEVANT DOCUMENTS [29-11-2022(online)].pdf | 2022-11-29 |
| 8 | 202121055737-FORM 13 [29-11-2022(online)].pdf | 2022-11-29 |
| 9 | 202121055737-ENDORSEMENT BY INVENTORS [01-12-2022(online)].pdf | 2022-12-01 |
| 10 | 202121055737-CORRESPONDENCE-OTHERS [01-12-2022(online)].pdf | 2022-12-01 |
| 11 | 202121055737-COMPLETE SPECIFICATION [01-12-2022(online)].pdf | 2022-12-01 |
| 12 | 202121055737-FORM 3 [15-12-2022(online)].pdf | 2022-12-15 |
| 13 | 202121055737-FORM-9 [02-01-2023(online)].pdf | 2023-01-02 |
| 14 | 202121055737-FORM 18A [03-01-2023(online)].pdf | 2023-01-03 |
| 15 | 202121055737-FORM-26 [17-01-2023(online)].pdf | 2023-01-17 |
| 16 | 202121055737-Covering Letter [17-01-2023(online)].pdf | 2023-01-17 |
| 17 | 202121055737-CORRESPONDENCE(IPO)-(CERTIFIED COPY OF WIPO DAS)-(20-01-2023).pdf | 2023-01-20 |
| 18 | 202121055737-FER.pdf | 2023-12-14 |
| 19 | 202121055737-FORM 3 [14-06-2024(online)].pdf | 2024-06-14 |
| 20 | 202121055737-FER_SER_REPLY [14-06-2024(online)].pdf | 2024-06-14 |
| 21 | 202121055737-CORRESPONDENCE [14-06-2024(online)].pdf | 2024-06-14 |
| 22 | 202121055737-CLAIMS [14-06-2024(online)].pdf | 2024-06-14 |
| 23 | 202121055737-US(14)-HearingNotice-(HearingDate-22-07-2024).pdf | 2024-06-24 |
| 24 | 202121055737-FORM-26 [18-07-2024(online)].pdf | 2024-07-18 |
| 25 | 202121055737-Correspondence to notify the Controller [18-07-2024(online)].pdf | 2024-07-18 |
| 26 | 202121055737-Response to office action [19-07-2024(online)].pdf | 2024-07-19 |
| 27 | 202121055737-Written submissions and relevant documents [06-08-2024(online)].pdf | 2024-08-06 |
| 28 | 202121055737-Annexure [06-08-2024(online)].pdf | 2024-08-06 |
| 29 | 202121055737-Response to office action [07-08-2024(online)].pdf | 2024-08-07 |
| 30 | 202121055737-Annexure [07-08-2024(online)].pdf | 2024-08-07 |
| 31 | 202121055737-US(14)-HearingNotice-(HearingDate-30-08-2024).pdf | 2024-08-09 |
| 32 | 202121055737-Correspondence to notify the Controller [27-08-2024(online)].pdf | 2024-08-27 |
| 33 | 202121055737-Written submissions and relevant documents [13-09-2024(online)].pdf | 2024-09-13 |
| 34 | 202121055737-Annexure [13-09-2024(online)].pdf | 2024-09-13 |
| 35 | 202121055737-PatentCertificate16-09-2024.pdf | 2024-09-16 |
| 36 | 202121055737-IntimationOfGrant16-09-2024.pdf | 2024-09-16 |
| 1 | 202121055737E_13-12-2023.pdf |