Agricultural chemical components
Patent Information
- Application Number
- TH2601000779
- Authority / Receiving Office
- TH · TH
- Patent Type
- Applications
- Current Assignee / Owner
- Filing Date
- 2024-08-02
- Publication Date
- 2026-09-07
AI Technical Summary
Existing agrochemical compositions containing kasugamycin face stability issues, particularly at higher temperatures and in alkaline conditions, which affects their efficacy and shelf life.
The development of an agrochemical composition comprising kasugamycin hydrochloride, a non-ionic surfactant, and agrochemically acceptable excipients, formulated at a pH ranging from 2 to 4, which enhances stability and maintains broad-spectrum anti-microbial properties.
The composition achieves improved stability and maintains its anti-fungal and antibacterial properties at reduced dosages, even under challenging storage conditions, thereby enhancing its effectiveness and shelf life.
Abstract
Description
[0001] TITLE: AGROCHEMICAL COMPOSITION
[0002] TECHNICAL FIELD
[0003] The present disclosure relates to an agrochemical composition. More particularly, the present invention relates to an agrochemical composition comprising kasugamycin or salts thereof.
[0004] BACKGROUND
[0005] Kasugamycin, an aminoglycoside antibiotic, has been used widely in agriculture and medicine to combat microbial pathogens by binding the ribosome to inhibit translation. Kasugamycin is an agricultural antibiotic bactericide that inhibits the proliferation of bacteria by tampering with their ability to make new proteins with ribosome being the major target. It exhibits both antibacterial and fungicidal properties and has been widely used. The mechanism of action of kasugamycin is to disturb the esterase system of pathogen metabolism of amino acid; destroy the biosynthesis of protein; the growth that suppresses mycelia also causes cell granulations, makes pathogen lose breeding and infection ability.
[0006] Kasugamycin is obtained by aerobic fermentation of the microorganism Streptomyces kasugaensis. The active ingredient kasugamycin hydrochloride hydrate is isolated from a kasugamycin fermentation product. It is more stable than the free base and does not deteriorate upon storage at 50°C for 10 days. It tolerates weak acids, decomposes slowly at pH 7, but decomposes within weeks in alkaline solutions even at ambient temperature. Therefore, there is a need in the art to provide a stable agrochemical.
[0007] The present inventors have aimed to develop a stable agricultural composition including a component such as kasugamycin or a salt that may overcome the drawbacks associated with the existing agricultural combinations or compositions The present composition provides broad-spectrum anti-microbial properties such as antifungal and antibacterial properties at a reduced dosage. SUMMARY OF THE INVENTION
[0008] The present disclosure provides an agrochemical composition comprising kasugamycin and a process for preparing the same.
[0009] In an aspect, the present disclosure provides an agrochemical composition comprising kasugamycin or salts thereof, wherein said composition is having low pH.
[0010] In an aspect, the present disclosure provides a soluble concentrate composition comprising kasugamycin or salts thereof, wherein said composition is having low pH.
[0011] In another aspect, the present disclosure provides a soluble concentrate composition comprising kasugamycin hydrochloride, wherein the composition is having pH ranging from 2 to 4.
[0012] In an aspect, the present disclosure provides an agrochemical composition comprising; a) kasugamycin hydrochloride, b) a non-ionic surfactant, and c) agrochemically acceptable excipient(s), wherein said composition is having pH ranging from 2 to 4.
[0013] In an aspect, kasugamycin hydrochloride and the non-ionic surfactant present in a ratio ranging from 0.1: 1 to 5 : 1.
[0014] In another aspect, the present invention provides use of the agrochemical composition for controlling phytopathogenic infestation in crops.
[0015] In another aspect, the present disclosure provides a method of controlling or inhibiting phytopathogens comprising applying at the locus of the infection by the phytopathogen or a plant or a plant part or a plant propagation material a composition comprising;
[0016] (i) kasugamycin or a salt thereof, and (ii) a non-ionic surfactant, wherein the weight ratio of kasugamycin or the salt thereof and the non-ionic surfactant is ranging from 0.1: 1 to 5 : 1 , and pH is ranging from 2 to 4.
[0017] DETAILED DESCRIPTION OF THE INVENTION
[0018] The following is a detailed description of embodiments of the present invention. The embodiments are in such detail as to clearly communicate the invention. 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 invention 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 the description herein and throughout the claims that follow, the meaning of “a,” “an,” and “the” includes plural reference unless the context clearly dictates otherwise. Also, as used in the description herein, the meaning of “in” includes “in” and “on” unless the context clearly dictates otherwise. As used herein, the terms “comprising” “including,” “having,” “containing,” “involving,” and the like are to be understood to be open-ended, i.e., to mean including but not limited to. The terms “preferred” and “preferably” refer to embodiments of the invention that may afford certain benefits, under certain circumstances.
[0022] The aspects and embodiments described herein shall also be interpreted to replace the clause “comprising” with either “consisting of or with “consisting essentially of’ or with “consisting substantially of.
[0023] “About” or “approximately” as used herein is inclusive of the stated value and means within an acceptable range of deviation for the particular value as determined by one of ordinary skill in the art, considering the measurement in question and the error associated with measurement of the particular quantity (i.e., the limitations of the measurement system). For example, “about” can mean within one or more standard deviations, or within ± 10% or ± 5% of the stated value. Recitation of ranges of values are merely intended to serve as a shorthand method of referring individually to each separate value falling within the range, unless otherwise indicated herein, and each separate value is incorporated into the specification as if it were individually recited herein. The endpoints of all ranges are included within the range and independently combinable. It is understood that where a parameter range is provided, all integers within that range, and tenths thereof, are also provided. For example, “0.1-80%” includes 0.1%, 0.2%, 0.3%, etc. up to 80%.
[0024] All methods described herein can be performed in a 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”), is intended merely to better illustrate the invention and does not pose a limitation on the scope of the invention unless otherwise claimed. No language in the specification should be construed as indicating any non-claimed element as essential to the practice of the invention as used herein. As used herein the term "plant" or “crop” refers to whole plants, plant organs (e.g., leaves, stems, twigs, roots, trunks, limbs, shoots, fruits etc.), plant cells, or plant seeds. This term also encompasses plant crops such as fruits. The term “plant” may further include the propagation material thereof, which may include all the generative parts of the plant such as seeds and vegetative plant material such as cuttings and tubers, which can be used for the multiplication of the plant. This includes seeds, tubers, spores, corms, bulbs, rhizomes, sprouts basal shoots, stolons, and buds and other parts of plants, including seedlings and young plants, which are to be transplanted after germination or after emergence from soil.
[0025] The term “locus” as used herein denotes the vicinity or area designated for growth of a desired crop, and in which control of the growth and / or spread of undesirable vegetation is desired. The locus includes the vicinity of desired crop plants wherein undesirable vegetation growth has either occurred, is most likely to occur, or is yet to occur.
[0026] As used herein, the term “stable” refers to chemical and / or physical stabilization of an active compound.
[0027] The salts referred to herein are agriculturally acceptable salts. As used herein, an "agriculturally acceptable salt" means a salt which is acceptable for use in agricultural or horticultural use.
[0028] As used herein, the term “ratio” refers to a weight ratio. Within the said ratio range, the active, i.e. kasugamycin and the non-ionic surfactant, i.e. isotridecyl alcohol ethoxylate, prevents degradation of the active in the liquid composition and has high stability during the preparation, storage and application process of the composition.
[0029] In some embodiments, the numbers expressing quantities of ingredients, properties such as concentration, 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.
[0030] 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. 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] All methods described herein can be performed in any 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.
[0032] The present disclosure is based on the premise of an unexpected finding by the inventors relating to the superior stability of the agrochemical composition comprising kasugamycin at a low pH, compared to the kasugamycin formulations available in literature. Further, the present inventors have also aimed to depict that the combination of kasugamycin and a preservative provides enhanced anti-bacterial and anti-fungal properties. The present inventors have also provided a suitable surfactant to improve the stability of the kasugamycin formulation.
[0033] Accordingly, the present disclosure provides an agricultural composition including kasugamycin or salt thereof that exhibits antifungal and antibacterial properties. Further, aspects of the present disclosure relate to an aqueous pre-mix agricultural formulation and a method of preparation thereof.
[0034] In an embodiment, the present disclosure provides an agrochemical composition comprising kasugamycin.
[0035] In an embodiment, the present disclosure provides an agrochemical composition comprising; a) kasugamycin or a salt thereof, b) a non-ionic surfactant, and c) agrochemically acceptable excipient(s), wherein the composition is having a pH ranging from 2 to 4.
[0036] In an embodiment, the present disclosure provides an agrochemical composition comprising; a) kasugamycin hydrochloride, b) a non-ionic surfactant, and c) agrochemically acceptable excipient(s), wherein the composition is having a pH ranging from 2 to 4.
[0037] In an embodiment, kasugamycin hydrochloride and the non-ionic surfactant present in a ratio ranging from 0.1: 1 to 5 : 1.
[0038] In a preferred embodiment, kasugamycin hydrochloride and the non-ionic surfactant present in a ratio ranging from 0.1 : 1 to 3: 1. In a preferred embodiment, kasugamycin hydrochloride and the non-ionic surfactant present in a ratio ranging from 0.1:1 to 2: 1.
[0039] In an embodiment, the present agrochemical composition is a liquid formulation.
[0040] In an embodiment, the stable agrochemical composition is selected from a soluble concentrate (SL), Capsule suspension (CS), Dispersible concentrate (DC), Emulsion, water in oil (EO), Emulsion, oil in water (EW), Oil dispersion (OD), Oil miscible flowable concentrate (oil miscible suspension (OF), Oil miscible liquid (OL), Suspension concentrate (SC), Suspo-emulsion (SE).
[0041] In an embodiment, the agrochemical composition is a soluble concentrate formulation.
[0042] In an embodiment, the present disclosure provides a soluble concentrate composition comprising kasugamycin or a salt thereof, wherein the composition is having a pH ranging from 2 to 4.
[0043] In an embodiment, the present disclosure provides a soluble concentrate composition comprising kasugamycin hydrochloride, wherein the composition is having a pH ranging from 2 to 4.
[0044] In an embodiment, the present disclosure provides a soluble concentrate composition comprising; a) kasugamycin or a salt thereof, b) a non-ionic surfactant, and c) agrochemically acceptable excipient(s).
[0045] In an embodiment, the present disclosure provides a soluble concentrate composition comprising; a) kasugamycin hydrochloride, b) a non-ionic surfactant, and c) agrochemically acceptable excipient(s).
[0046] In an embodiment, the present disclosure provides a soluble concentrate composition comprising; a) kasugamycin or a salt thereof, b) a non-ionic surfactant, c) an anti-microbial agent, and d) agrochemically acceptable excipient(s).
[0047] In an embodiment, the present disclosure provides a soluble concentrate composition comprising; a) kasugamycin hydrochloride, b) a non-ionic surfactant, c) an anti-microbial agent, d) a pH modifier, and e) agrochemically acceptable excipient(s).
[0048] In an embodiment, the present disclosure provides a soluble concentrate composition comprising; a) kasugamycin or a salt thereof, b) a non-ionic surfactant, and c) agrochemically acceptable excipient(s), wherein the composition is having a pH ranging from 2 to 4.
[0049] In an embodiment, the non-ionic surfactants are not molecularly charged (positive or negative) and do not form ions in water. Non-limiting examples of nonionic surfactants include polymeric surfactants such as block copolymers, random copolymers, graft copolymer and star polymers, amine ethoxylates, alkanolamides and ethoxylated alkanolamides; alkoxylated triglycerides (such as ethoxylated soybean, castor and rapeseed oils); polyethoxylate esters such as polyethoxylated sorbitan fatty acid esters, polyethoxylated sorbitol fatty acid esters and poly ethoxylated glycerol fatty acid esters; alkylphenol alkoxylates (e.g., octyl- (such as the Tritonpropylene oxide, butylene oxide or mixtures thereof); amine ethoxylates, alkanolamides and ethoxylated alkanolamides; alkoxylated triglycerides (such as ethoxylated soybean, castor and rapeseed oils); alkylphenol alkoxylates (e.g., octyl- (such as the Tritonpropylene oxide, butylene oxide or mixtures thereof); sugar-derivatives such as sucrose esters, alkyl polyglycosides and alkyl polysaccharides; amine ethoxylates, alkanolamides and ethoxylated alkanolamides; alkoxylated triglycerides (such as ethoxylated soybean, castor and rapeseed oils); alkylphenol alkoxylates (e.g., octyl-, nonyl-), dinonyl-, or dodecyl-)); ethoxylated fatty acids; ethoxylated fatty esters and oils; fatty acid esters, ethoxylated methyl esters; glycerol esters, lanolin-based derivatives, other sorbitan derivatives such as sorbitan esters; ethoxylated fatty acids), alkyd PEG (polyethylene glycol) resins, alkyd type copolyesters; polyethylene glycols (PEG) polyethylene glycol fatty acid esters; silicone -based surfactants; and combinations thereof.
[0050] In one embodiment, the non-ionic surfactant is preferably selected from an alcohol alkoxylate preferably alcohol ethoxylate.
[0051] In a preferred embodiment, the non-ionic surfactant is ethoxylated isotridecyl alcohol.
[0052] In an embodiment, kasugamycin hydrochloride and ethoxylated isotridecyl alcohol is present in a weight ratio ranging from 0.1:1 to 5 : 1.
[0053] In a preferred embodiment, kasugamycin hydrochloride and ethoxylated isotridecyl alcohol is present in a weight ratio ranging from 0.1:1 to 3 : 1. In a preferred embodiment, kasugamycin hydrochloride and ethoxylated isotridecyl alcohol is present in a weight ratio ranging from 0.1:1 to 2: 1.
[0054] In an embodiment, the anti-microbial agent is selected from chlorphensin, benzoic acid or a salt or ester thereof (e.g. sodium benzoate), propionic acid or a salt thereof, salicylic acid or a salt thereof, sorbic acid or a salt thereof (e.g. potassium sorbate), formaldehyde, paraformaldehyde, zinc pyrithione, inorganic sulphites, hydrogen sulphites, chlorobutanol, 4-hydroxybenzoic acid or a salt or ester thereof (e.g. methylparaben, ethylparaben, propylparaben), dehydroacetic acid and / or a salt thereof (e.g. sodium dehydroacetate), formic acid or a salt thereof, dibromohexamidine isethionate; thimerosal, phenylmecuric salts, undecylenic acid or a salt thereof, hexetidine, bronopol, 5-bromo-5-nitro-l,3-dioxane, dichlorobenzyl alcohol, benzyl alcohol, triclocarban, chlororesol, triclosan, chloroxylenol, imidazolidinyl urea, polyaminopropyl biguanide, phenoxyethanol, methenamine, quaternium-15, climbazole, DMDM hydantoin, l-hydroxy-4-methyl-6-(2,4,4- trimethylenepentyl)-2 pyridon, piroctone olamine, bromochlorophene, O-cymen-5-ol, methylchloroisothiazolinone, methylisothiazololinone, mixtures of methylchloroisothiazolinone and methylisothiazololinone, chlorophene, chloroacetamide, phenoxyisoproponol, alkyl (C12-C22) trimethyl ammonium bromide, alkyl (C12-C22) trimethyl ammonium chloride, dimethyl oxazolidine, diazolidinyl urea, hexamidine, hexamidine diisethionate, hexamidine diparaben, hexamidine paraben, glutaral, 7- ethylbicyclooxazolidine, sodium hydroxymethylaminoacetate, silver chloride, benzethonium chloride, benzalkonium chloride, benzalkonium bromide, benzalkonium saccharinate, benzylhemiformal, iodopropynyl butylcarbamate, silver citrate, or combinations thereof.
[0055] In an embodiment, the anti-microbial agent is sorbic acid, its calcium, potassium, and sodium salts In a preferred embodiment, the anti-microbial agent is potassium sorbate.
[0056] In an embodiment, the composition comprises, by weight of the formulation, kasugamycin or a salt thereof in an amount ranging from 0.1% to 40% w / w, and one or more excipients in an amount ranging from 5 % to 99% w / w.
[0057] In an embodiment, the composition comprises, by weight of the formulation, kasugamycin or a salt thereof in an amount ranging from 0.1% to 20% w / w, and one or more excipients in an amount ranging from 10% to 70% w / w.
[0058] In an embodiment, kasugamycin hydrochloride is present in a concentration ranging from 0.1% w / w to 10% w / w.
[0059] In a preferred embodiment, kasugamycin hydrochloride is present in a concentration ranging from 0.5% w / w to 5% w / w.
[0060] In another preferred embodiment, kasugamycin hydrochloride is present in a concentration ranging from 0.5% w / w to 3% w / w.
[0061] In an embodiment, the non-ionic surfactant is present in a concentration ranging from 0.1% to 3% w / w.
[0062] In an embodiment, the non-ionic surfactant is present in a concentration ranging from 0.5 % to 2% w / w.
[0063] In an embodiment, the alcohol ethoxylate is present in a concentration ranging from 0.1% to 3% w / w. In an embodiment, the alcohol ethoxylate is present in a concentration ranging from 0.5 % to 2% w / w.
[0064] In an embodiment, the ethoxylated isotridecyl alcohol is present in a concentration ranging from 0.1% to 3% w / w.
[0065] In an embodiment, the ethoxylated isotridecyl alcohol is present in a concentration ranging from 0.5 % to 2% w / w.
[0066] In another embodiment, said composition further comprises at least one agrochemically suitable excipient.
[0067] According to an embodiment of the present disclosure, the agrochemically acceptable excipients are selected from one or more of emulsifiers, colorants, thickeners / binders, antifreeze agents, antifoaming agents, antioxidants, solvents, preservatives, glidants, anticaking agents, pH-regulating agents, buffering agents, formulation aids, disintegrants, or combinations thereof.
[0068] In another embodiment, emulsifiers which can be advantageously employed herein can be readily determined by those skilled in the art and include various non-ionic, anionic, cationic, and amphoteric emulsifiers, or a blend of two or more emulsifiers. Examples of non-ionic emulsifiers useful in preparing the emulsifiable concentrates include the polyalkylene glycol ethers and condensation products of alkyl and aryl phenols, aliphatic alcohols, aliphatic amines or fatty acids with ethylene oxide, propylene oxides such as the ethoxylated alkyl phenols and carboxylic esters solubilized with the polyol or polyoxyalkylene. Cationic emulsifiers include quaternary ammonium compounds and fatty amine salts. Anionic emulsifiers include the oil-soluble salts (e.g., calcium) of alkylaryl sulfonic acids, oil-soluble salts or sulfated polyglycol ethers and appropriate salts of phosphated polyglycol ether.
[0069] In an embodiment, colorants may be selected from iron oxide, titanium oxide and Prussian Blue, and organic dyestuffs, such as alizarin dyestuffs, azo dyestuffs or metal phthalocyanine dyestuffs, and trace elements, such as salts of iron, manganese, boron, copper, cobalt, molybdenum and zinc.
[0070] In another embodiment, antifreeze agent(s) added to the composition may be alcohols selected from the group comprising of but not limited to ethylene glycol, 1 ,2-propylene glycol, 1,3-propylene glycol, 1,2-butanediol, 1,3-butanediol, 1,4-butanediol, 1,4- pentanediol, 3-methyl-l,5-pentanediol, 2,3-dimethyl-2,3-butanediol, trimethylol propane, mannitol, sorbitol, glycerol, pentaerythritol, 1 ,4-cyclohexanedimethanol, xylenol, bisphenols such as bisphenol A or the like. In addition, ether alcohols such as diethylene glycol, triethylene glycol, tetraethylene glycol, polyoxyethylene or polyoxypropylene glycols of molecular weight up to about 4000, diethylene glycol monomethylether, diethylene glycol monoethylether, triethylene glycol monomethylether, butoxyethanol, butylene glycol monobutylether, dipentaerythritol, tripentaerythritol, tetrapentaerythritol, diglycerol, triglycerol, tetraglycerol, pentaglycerol, hexaglycerol, heptaglycerol, octaglycerol.
[0071] In an embodiment, the antifreeze agent is monoethylene glycol.
[0072] According to an embodiment, antifoam agent may be selected from polydimethoxysiloxane, polydimethylsiloxane, alkyl poly acrylates, castor oil, fatty acids, fatty acids esters, fatty acids sulfate, fatty alcohol, fatty alcohol esters, fatty alcohol sulfate, foot olive oil, mono & di glyceride, paraffin oil, paraffin wax, poly propylene glycol, silicones oil, vegetable fats, vegetable fats sulfate, vegetable oil, vegetable oil sulfate, vegetable wax, vegetable wax sulfate, agents based on silicon or magnesium stearate. The agrochemical composition may also comprise one or more antioxidants. Preferably, the agrochemical formulation comprises an antioxidant. Antioxidants are, for example, amino acids (e.g., glycine, histidine, tyrosine, tryptophan) and derivatives thereof, imidazole and imidazole derivatives (e.g., urocanic acid), peptides, such as, for example, D,L-carnosine, D- carnosine, L-carnosine and derivatives thereof (e.g., anserine), carotenoids, carotenes (e.g., a-carotene, P-carotene, lycopene) and derivatives thereof, lipoic acid and derivatives thereof (e.g., dihydrolipoic acid), aurothioglucose, propylthiouracil and further thio compounds (e.g., thioglycerol, thiosorbitol, thioglycolic acid, thioredoxin, glutathione, cysteine, cystine, cystamine and the glycosyl, N-acetyl, methyl, ethyl, propyl, amyl, butyl, lauryl, palmitoyl, oleyl, y-linoleyl, cholesteryl and glyceryl esters thereof), and salts thereof, dilauryl thiodipropionate, distearyl thiodipropionate, thiodipropionic acid and derivatives thereof (esters, ethers, peptides, lipids, nucleotides, nucleosides and salts), and sulfoximine compounds (e.g., buthionine sulfoximines, homocysteine sulfoximine, buthionine sulfones, penta-, hexa-, heptathionine sulfoximine) in very low tolerated doses (e.g., pmol / kg to pmol / kg), also metal chelating agents (e.g., a-hydroxy fatty acids, EDTA, EGTA, phytic acid, lactoferrin), a-hydroxy acids (e.g., citric acid, lactic acid, malic acid), humic acids, bile acid, bile extracts, gallic esters (e.g., propyl, octyl and dodecyl gallate), flavonoids, catechins, bilirubin, biliverdin and derivatives thereof, unsaturated fatty acids and derivatives thereof (e.g., y-linolenic acid, linoleic acid, arachidonic acid, oleic acid), folic acid and derivatives thereof, hydroquinone and derivatives thereof (e.g., arbutin), ubiquinone and ubiquinol, and derivatives thereof, vitamin C and derivatives thereof (e.g., ascorbyl palmitate, stearate, dipalmitate, acetate, Mg ascorbyl phosphates, sodium and magnesium ascorbate, disodium ascorbyl phosphate and sulfate, potassium ascorbyl tocopheryl phosphate, chitosan ascorbate), isoascorbic acid and derivatives thereof, tocopherols and derivatives thereof (e.g., tocopheryl acetate, linoleate, oleate and succinate, tocophereth-5, tocophereth-10, tocophereth-12, tocophereth-18, tocophereth-50, tocopher solan), vitamin A and derivatives (e.g., vitamin A palmitate), the coniferyl benzoate of benzoin resin, rutin, rutinic acid and derivatives thereof, disodium rutinyl disulfate, cinnamic acid and derivatives thereof (e.g., ferulic acid, ethyl ferulate, caffeeic acid), kojic acid, chitosan glycolate and salicylate, butylhydroxy toluene, butylhydroxyanisol, nordihydroguaiacic acid, nordihydroguaiaretic acid, trihydroxybutyrophenone, uric acid and derivatives thereof, mannose and derivatives thereof, selenium and selenium derivatives (e.g., selenomethionine), stilbenes and stilbene derivatives (e.g., stilbene oxide, trans-stilbene oxide).
[0073] According to the disclosure, suitable derivatives (salts, esters, sugars, nucleotides, nucleosides, peptides, and lipids) and mixtures of these specified active ingredients or plant extracts (e.g., teatree oil, rosemary extract and rosemarinic acid) which comprise these antioxidants can be used. In general, mixtures of the aforementioned antioxidants are possible.
[0074] According to an embodiment, examples of suitable solvents are water. In principle, solvent mixtures may also be used.
[0075] In an embodiment, the present soluble concentrate composition is stable at room temperature for a period ranging from 1 week to 24 months.
[0076] According to an embodiment of the present disclosure, the recovery of the amount of active i.e. kasugamycin remaining in the stable agrochemical composition of the present disclosure after storing the composition for 24 months is consistent with the initial concentration of kasugamycin in the composition.
[0077] In an embodiment, the present disclosure provides a process for preparing an agrochemical composition comprising kasugamycin hydrochloride. According to an embodiment of the present disclosure, the stable agrochemical composition comprising kasugamycin is used to control a wide range of phytopathogenic pests.
[0078] According to an embodiment of the present disclosure, the stable agrochemical composition is used to control a broad spectrum of microbes at pre-emergence and post-emergence stages.
[0079] According to an embodiment of the present disclosure, the form of the stable agrochemical composition allows the active compounds to be effectively taken up by the plants.
[0080] The combinations of the present invention may be developed as a pre-mix composition or a kit or kit of parts such that individual actives may be mixed before applying.
[0081] According to an embodiment of the present disclosure, a kit comprising a stable agrochemical composition is provided. The kit comprises a plurality of components, including at least one of the ingredients of the stable agrochemical composition comprising kasugamycin of the present invention.
[0082] According to an embodiment of the present disclosure, a kit comprises kasugamycin or an agriculturally acceptable salt thereof; and a non-ionic surfactant in a ratio of 0.1: 1 to 5:1.
[0083] In one embodiment of the present disclosure, the kit may include at least one, or all of components that may be used to prepare the stable agrochemical composition. For example, the kit may include kasugamycin, a non-ionic surfactant, an anti-microbial agent, a pH modifier, and agrochemically acceptable excipient(s).
[0084] One or more of the components may already be combined or pre-formulated. In those embodiments where more than two components are provided in a kit, the components may already be combined and as such are packaged in a single container such as a vial, bottle, can, pouch, bag and / or canister. In other embodiments, two or more components of a kit may be packaged separately, i.e., not pre-formulated. As such, a kit may include one or more separate containers such as vials, cans, bottles, pouches, bags and / or canisters, each container containing a separate component for stable herbicidal composition.
[0085] In both forms, a component of the kit may be applied separately from or together with the further components or as a component of a combination composition according to the invention for preparing the stable herbicidal composition according to the invention.
[0086] In an embodiment the present compositions further comprising an herbicide, fungicide, insecticide, nematicide, acaricides or combinations thereof.
[0087] The method of the present disclosure may be used to control a broad spectrum of plant diseases.
[0088] Diseases in rice include blast (Magnaporthe grisea), Helminthosporium leaf spot (Cochliobolus miyabeamis), sheath blight (Rhizoctonia solani), and bakanae disease (Gibberella fujikuroi ).
[0089] Diseases in wheat include powdery mildew (Erysiphe graminis), Fusariuin head blight (Fusarium graminearum, F. avenacerum, F. culmorum, Microdochium nivale) , rust (Puccinia striiformis, P. graminis, P. recondita) , pink snow mold (Micronectriella nivale), Typhula snow blight (Typhula sp.), loose smut (Ustilago tritici), bunt (Tilleda caries), eyespot (Pseudocercosporella herpotrichoides), leaf blotch (Mycosphaerella graminicola), glume blotch (Stagonospora nodorum) , septaria, and yellow spot (Pyrenophora tritici- repentis).
[0090] Diseases of barley include powdery mildew (Erysiphe graminis), Fusarium head blight (Fusarium graminearum, F. avenacerum, F. culmorum, Microdochium nivale), rust (Puccinia striiformis, P. graminis, P. hordei), loose smut (Ustilago nuda), scald (Rhynchosporium secalis), net blotch (Pyrenophora teres), spot blotch (Cochliobolus sativus), leaf stripe Pyrenophora graminea), and Rhizoctonia damping-off (Rhizoctonia solani ).
[0091] Diseases in corn include smut {Ustilago maydis), brown spot Cochlioholus hetero strophus), copper spot {Gloeocercospora sorghi), southern rust (Puccinia polysora), gray leaf spot (Cercospora zeae-maydis), white spot {Phaeosphaeria mydis and / or Pantoea ananatis), and Rhizoctonia damping-off {Rhizoctonia solani ).
[0092] Diseases of citrus include melanose {Diaporthe citri), scab {Elsinoefawcetti), penicillium rot (Penicillium digitatum, P. italicum), and brown rot {Phytophthora parasitica, Phytophthora citrophthora ).
[0093] Diseases of apple include blossom blight (Monilinia mail), canker {Valsa ceratosperma), powdery mildew {Podosphaera leucotricha), Alternaria leaf spot {Altemaria alternate apple pathotype), scab {Venturia inaequalis), powdery mildew, bitter rot {Colle to trichum acutatum), crown rot {Phytophtora cactorum), blotch {Diplocarpon malt), and ring rot {Botryosphaeria berengeriana ).
[0094] Diseases of pear include scab {Venturia nashicola, V. pirina), powdery mildew, black spot (Alternaria alternata Japanese pear pathotype), rust (Gymnosporangium haraeanum), and phytophthora fruit rot (Phytophtora cactorum).
[0095] Diseases of peach include brown rot (Monilinia fructicola), powdery mildew, scab ( Cladosporium carpophilum), and phomopsis rot (Phomopsis sp.). Diseases of grape include anthracnose (Elsinoe ampelina), ripe rot (Glomerella cingulata), powdery mildew (Uncinula necator), rust (Phakopsora ampelopsidis), black rot ( Guignardia bidwellii), botrytis, and downy mildew (Plasmopara viticola).
[0096] Diseases of Japanese persimmon include anthracnose (Gloeosporium kaki), and leaf spot ( Cercospora kaki, Mycosphaerella nawae ).
[0097] Diseases of gourd include anthracnose (Colletotrichum lagenarium), powdery mildew (Sphaerotheca fidiginea), gummy stem blight (Mycosphaerella melonis), Fusarium wilt (Fusarium oxysporum), downy mildew (Pseudoperonospora cubensis), Phytophthora rot (Phytophthora sp.), and damping-off (Pythium sp.).
[0098] Diseases of tomato include early blight (Altemaria solani), leaf mold (Cladosporium fulvum), and late blight Phytophthora inf estans).
[0099] Diseases of eggplant include brown spot (Phomopsis v exans), and powdery mildew (Erysiphe cichoracearum )
[0100] Diseases of cruciferous vegetables include Alternaria leaf spot (Altemaria japonica), white spot (Cercosporella brassicae), clubroot (Plasmodiophora brassicae), and downy mildew (Peronospora parasitica).
[0101] Diseases of onion include rust (Puccinia allii), and downy mildew (Peronospora destructor)
[0102] Diseases of soybean include purple seed stain (Cercospora kikuchii), sphaceloma scad (Elsinoe glycines), pod and stem blight (Diaporthe phaseolorum var. sojae), septoria brown spot (Septoria glycines), frogeye leaf spot (Cercospora sojina), rust (Phakopsora pachyrhizi), Yellow rust, brown stem rot (Phytophthora sojae), and Rhizoctonia damping- off (Rhizoctonia solani).
[0103] Diseases of kidney bean include anthracnose (Colletotrichum lindemthianum).
[0104] Diseases of peanut include leaf spot (Cercospora personata), brown leaf spot (Cercospora arachidicola) and southern blight (Sclerotium rolfsii).
[0105] Diseases of garden pea include powdery mildew (Erysiphe pisi), and root rot (Fusarium solani f sp. pisi).
[0106] Diseases of potato include early blight (Altemaria solani), late blight (Phytophthora inf estans), pink rot (Phytophthora erythroseptica), and powdery scab (Spongospora subterranean , sp. subterranea).
[0107] Diseases of strawberry include powdery mildew (Sphaerotheca humuli), and anthracnose ( Glomerella cingulata).
[0108] Diseases of tea include net blister blight (Exobasidium reticulatum), white scab (Elsinoe leucospila), gray blight (Pestalotiopsis sp. , and anthracnose (Colletotrichum theae- sinensis).
[0109] Diseases of tobacco include brown spot (Altemaria longipes), powdery mildew (Erysiphe cichoracearum), anthracnose (Colletotrichum tabacum), downy mildew (Peronospora tabacina), and black shank (Phytophthora nicotianae).
[0110] Diseases of rapeseed include sclerotinia rot (Sclerotinia sclerotiorum), and Rhizoctonia damping-off (Rhizoctonia solani). Diseases of cotton include Rhizoctonia damping-off (Rhizoctonia solani).
[0111] Diseases of sugar beet include Cercospora leaf spot (Cercospora beticola), leaf blight (Thanatephorus cucumeris), root rot (Thanatephorus cucumeris), and Aphanomyces root rot (Aphanomyces cochlioides).
[0112] Diseases of rose include black spot (Diplocarpon rosae), powdery mildew (Sphaerotheca pannosd), and downy mildew (Peronospora sparsa).
[0113] Diseases of chrysanthemum and asteraceous plants include downy mildew (Premia lactucae), leaf blight (Septaria chrysanthemi-indici), and white rust (Puccinia horiana).
[0114] Diseases of various groups include diseases caused by Pythium spp. (Pythium aphanidermatum, Pythium debarianum, Pythium graminicola, Pythium irregulare, Pythium ultimum), gray mold. (Botrytis cinerea), and Sclerotinia rot (Sclerotinia sclerotiorum).
[0115] Disease of Japanese radish include Alternaria leaf spot (Altemaria brassicicola).
[0116] Diseases of turf grass include dollar spot (Sclerotinia homeocarpa), and brown patch and large patch (Rhizoctonia solani).
[0117] Disease of banana include black sigatoka (Mycosphaerella fijiensis), and yellow sigatoka (Mycosphaerella musicola).
[0118] Disease of sunflower include downy mildew (Plasmopara halstedii ).
[0119] Seed diseases or diseases in the early stages of the growth of various plants may be caused by Aspergillus spp., Penicillium spp., Fusarium spp., Gibberella spp., Tricoderma spp., Thielaviopsis spp., Rhizopus spp., Mucor spp., Corticium spp., Phoma spp., Rhizoctonia spp. and Diplodia spp.
[0120] Viral diseases of various plants may be mediated by Polymyxa spp. or Olpidium spp. and so on.
[0121] Most plant pathogenic bacteria belong to the following genera: Erwinia, P ectobacterium, Pantoea, Agrobacterium, Pseudomonas, Ralstonia, Burkholderia, Acidovorax, Xanthomonas, Clavibacter, Streptomyces, Xylella, Spiroplasma, and Phytoplasma.
[0122] Particularly, the composition of the present disclosure is effective against Pseudomonas syringae, Xanthomonas spp., Erwinia amylovora, Erwinia carotovora, Pyricularia oryzae, Xanthomonas axonopodispv. Vesicatoria, Burkholderia andropogonis, and Streptomyces scabies.
[0123] Examples of the crops on which the present compositions may be used include, are not limited to, corn, rice, wheat, barley, rye, oat, sorghum, cotton, soybean, peanut, buckwheat, beet, rapeseed, sunflower, sugar cane, tobacco, etc.; vegetables: solanaceous vegetables such as eggplant, tomato, pimento, pepper, potato, etc., cucurbit vegetables such as cucumber, pumpkin, zucchini, water melon, melon, squash, etc., cruciferous vegetables such as radish, white turnip, horseradish, kohlrabi, Chinese cabbage, cabbage, leaf mustard, broccoli, cauliflower, etc., asteraceous vegetables such as burdock, crown daisy, artichoke, lettuce, etc, liliaceous vegetables such as green onion, onion, garlic, and asparagus, ammiaceous vegetables such as carrot, parsley, celery, parsnip, etc., chenopodiaceous vegetables such as spinach, Swiss chard, etc., lamiaceous vegetables such as Perillafrutescens, mint, basil, etc, strawberry, sweet potato, Dioscorea japonica, colocasia, etc., flowers, foliage plants, turf grasses, fruits: pome fruits such apple, pear, quince, etc, stone fleshy fruits such as peach, plum, nectarine, Prunus mume, cherry fruit, apricot, prune, etc., citrus fruits such as orange, lemon, rime, grapefruit, etc., nuts such as chestnuts, walnuts, hazelnuts, almond, pistachio, cashew nuts, macadamia nuts, etc. berries such as blueberry, cranberry, blackberry, raspberry, etc., grape, kaki fruit, olive, plum, banana, coffee, date palm, coconuts, etc., trees other than fruit trees; tea, mulberry, flowering plant, trees such as ash, birch, dogwood, Eucalyptus, Ginkgo biloba, lilac, maple, Quercus, poplar, Judas tree, Liquidambar formosana, plane tree, zelkova, Japanese arborvitae, fir wood, hemlock juniper, Pinus, Picea, and Taxus cuspidate, etc.
[0124] In an embodiment, the present disclosure provides a method of controlling or inhibiting phytopathogens, comprising applying the compositions described herein to the said plant or plant part or plant propagation material or to the locus thereof.
[0125] In an embodiment, the present disclosure provides a method of controlling or inhibiting phytopathogens comprising applying at the locus of the infection by the phytopathogen or a plant or a plant part or a plant propagation material a composition comprising;
[0126] (i) kasugamycin or a salt thereof, and
[0127] (ii) a non-ionic surfactant, wherein the weight ratio of kasugamycin or the salt thereof and the non-ionic surfactant is ranging from 0.1: 1 to 5 : 1 , and the pH is ranging from 2 to 4.
[0128] In an embodiment, the present disclosure provides a method of controlling or inhibiting phytopathogens comprising applying at the locus of the infection by the phytopathogen or a plant or a plant part or a plant propagation material a composition comprising;
[0129] (i) kasugamycin hydrochloride, and
[0130] (ii) a non-ionic surfactant, wherein the weight ratio of kasugamycin or the salt thereof and the non-ionic surfactant is ranging from 0.1: 1 to 5 : 1 and the pH is ranging from 2 to 4. The composition of the present invention maybe applied simultaneously as a tank mix or a formulation or may be applied sequentially. The application may be made to the soil before emergence of the plants, either pre-planting or post-planting. The application may be made as a foliar spray at different timings during crop development, with either one or two applications early or late post-emergence.
[0131] The compositions according to the disclosure can be applied before or after infection of the useful plants or the propagation material thereof by fungi or bacteria or any other microbe. The soluble concentrate formulation significantly improved disease control, reduced occurrence of resistance in microbes as well as improved yield.
[0132] The invention shall now be described with reference to the following specific examples. It should be noted that the examples appended below illustrate rather than limit the invention and that those skilled in the art will be able to design many alternative embodiments without departing from the scope of the present invention.
[0133] Examples:
[0134] Example 1: Soluble concentrate composition Process: In a formulation tank the required amount of the water was added followed by stirring with addition of the amount of kasugamycin hydrochloride, ethoxylated isotridecyl alcohol, potassium Sorbate, and monoethylene glycol as shown in the table above. The system was kept under stirring after each addition. The pH is adjusted with hydrochloric acid aqueous solution. In case, where the pH was adjusted, the mixture was continuously stirred to obtain the soluble concentrate composition.
[0135] Example 2:
[0136] Stability data:
[0137] M refers to the months. The stability of the present agrochemical composition is evident from table 2 above. The stability of the present composition was evaluated for over a period of 24 months at room temperature. As is evident from the table above, the stability parameters over a period are in keeping with the specification provided for each parameter. The retention of kasugamycin is consistent in each month with minimum degradation. The low pH in the range of 2.80 to 3.10 is maintained and contributes to the stability of kasugamycin.
[0138] Example 3: Surfactant screening studies
[0139] The surfactant screening studies were performed to determine the surfactant and the concentration best suited to the stable kasugamycin soluble concentrate composition of the present invention. Accordingly, an anionic surfactant, i.e. sodium dioctyl sulfosuccinate in propylene glycol was used to prepare the formulation in compositions A and B as depicted in Table 3 below. The present composition used the non-ionic surfactant, i.e. Isotridecyl alcohol ethoxylate. The compositions were subjected to AHS conditions, i.e. accelerated heat stability conditions of 14 days at 54°C.
[0140] Table 3: Accordingly, compositions A and B using the anionic surfactant showed sedimentation at AHS conditions. However, the present composition using Isotridecyl alcohol ethoxylate, showed no sedimentation and was used for preparing the kasugamycin formulation.
Claims
DEPCT691. An agricultural chemical composition which includes a) kasugamycin or its salts, b) a nonionic surfactant, and c) an agriculturally acceptable bulking agent in which the pH of such composition is in the range of 2 to 4.
2. A composition as proposed in Claim 1 in which kasugamycin is in the form of kasugamycin hydrochloride.
3. A composition as proposed in Claim 1 in which the composition is a water-soluble concentrate.
4. A composition as proposed in Claim 1 in which a nonionic surfactant is present.
5. Composition as claimed in claim 4 where the ethoxylate alcohol consists of isotridezil alcohol that has undergone ethoxylation.
6. Composition as claimed in claim 1 where the weight ratio of kasugamycin to nonionic surfactant ranges from 0.1:1 to 5:
1.
7. Composition as claimed in claim 6 where the weight ratio of kasugamycin hydrochloride to isotridezil alcohol ethoxylate ranges from 0.1:1 to 5:
1. 8.
9. The composition as proposed in claim 1 where acceptable agrochemical adjuvants are selected from a group comprising surfactants, pH regulators, buffers, preservatives, disintegrants, or combinations thereof.
10. The composition as proposed in claim 1 where kasugamycin is present at a concentration ranging from 0.1% to 20% by weight / weight.
11. The composition as proposed in claim 1 where nonionic surfactants are present at a concentration ranging from 0.1% to 3% by weight / weight.
12. The composition A concentrated solution containing a) kasugamycin or its salts, b) a nonionic surfactant, c) an antimicrobial agent, d) a pH regulator, and e) an agriculturally acceptable bulking agent.
12. A concentrated solution as claimed in claim 11 in which the water-soluble concentration has a pH range from 2 to 4.
13. A composition as claimed in claim 1, which includes an additional pesticide of choice from fungicides, herbicides, insecticides, and biostimulants. 14.Methods for controlling plant diseases caused by plant pathogens, which involve the application of agricultural chemical compounds containing kasugamycin or its salts, with a pH ranging from 2 to 4, to areas of plants, plant parts, or plant propagation material.
15. The use of agricultural chemical compounds as claimed in claim 1 to control the infestation of plant pathogens in crops;