DESC:Synergistic Fungicidal Combination of Myclobutanil and Validamycin
FIELD OF THE INVENTION
The present invention relates to a synergistic fungicidal composition comprising of triazole fungicide and antibiotic fungicide in EC / WDG / SC / SL / OD / OS / Solid Granules and other formulations in different percentages. More precisely, the subject matter of the present invention is a synergistic fungicidal composition based on a combination of myclobutanil and validamycin optionally with at least one agriculturally acceptable excipient which will facilitate in the preparation of desired formulations. The present invention also relates to the process for the preparation of synergistic fungicidal composition thereof and use of this combination for combating plant pathogenic fungi in and on the seeds and plants at different growth stages for crop protection and good yields.
BACKGROUND OF THE INVENTION
Crop protection is the practice of protecting the crop yields from pests, weeds, plant diseases, and other organisms that damage agricultural crops, which is critical from early stages of crop development. Preventing pests and diseases in the entire crop cycle, i.e., from root development to maturing crop, leading to increased crop quality and yield. The control of plant diseases caused by fungi is extremely important in achieving high crop efficiency. Plant diseases cause significant damage to vegetables, fields, cereal, fruit and other crops lead to reduction in productivity, yield and quality of the crops. Fungicides help to minimize this damage by controlling plant pathogenic fungi. The use of two or more appropriate active ingredient combinations in specific dose ratios leads to synergism in crop protection. In addition to this, often highly destructive plant diseases can be difficult to control and may develop resistance to commercial fungicides. Many products are commercially available for these purposes, but there is still a continues need to develop new fungicidal combinations which are more effective, less costly, less toxic, environmentally safer and have different sites of action.
The biggest challenge in the field of crop protection is to reduce the dosage rate of active ingredients to diminish or circumvent environmental or toxicological effects without compromising on effective crop protection against pathogenic fungi, in addition to long lasting and broad-spectrum protection from plant diseases. Another challenge is to reduce the excessive application of solo chemical compounds or fungicides which invariably helps in rapid selection of pathogenic fungi and aid in developing natural or adapted resistance against the active compound in question.
Therefore, it is indeed necessary to use the fungicidal combination in lower doses, fast acting with the different mode of action that can provide long lasting control against broad spectrum of pathogenic fungi and check the resistance development in fungi. The composition should have high synergistic action, no cross resistance to existing fungicides, avoid excess loading of the toxicant to the environment and negligible impact to environmental safety. Thus, there is a need for synergistic fungicidal combinations which could be physico-compatible formulations in the form of storage stability, safe packaging and ready to use formulations.
OBJECT OF THE INVENTION
The principal object of the present invention is to provide a fungicide mixture or combination which solves at least one of the major problems discussed above like reducing the dosage rate, broadening the spectrum of activity, or combining activity with prolonged pest control and resistance management with improved environmental safety by reducing toxicity and residue deposit in soil and in crops. Thus, the combination of the present invention is designed to target and eliminate a broader spectrum of pests, prevent the development of resistance, and potentially reduce the risk of negative environmental impacts associated with a single fungicide.
The details of one or more embodiments of this disclosure are set forth in the accompanying description below and other features, objects, and advantages will be apparent from the description and the claims.
DESCRIPTION OF THE INVENTION
The present disclosure / specification refers to a synergistic fungicidal or pesticidal composition and the process for the preparation for crop protection.
The term “combination” can be replaced with the words “mixture” or “composition” defined or refers to as combining two or more active ingredients formulated in desired formulations.
The term “pesticide” as used in this specification refers to a substance or mixture of substances intended for preventing, destroying, repelling, or mitigating any pest or weeds which causes damage to the crop. Herbicides, insecticides, and fungicides are mainly used as pesticides which control weeds and insect pests and disease-causing fungi pathogens respectively that eventually leads to high yield of crops.
The term “Fungicide” also called antimycotic, as used in this specification refers to a type of chemical compound or substance specifically designed to protect crops and kill or inhibit the growth of fungi and their spores that cause economic damage to crop, ornamental plants or endanger the health of domestic animals or humans.
The term “synergism” as used in this specification refers to the interaction between two or more active compounds or other factors to produce a combined effect greater than the sum of their separate effects. The present invention involves the mixture of two active ingredients which has increased efficacy when compared to individual use and admixture of those components.
The conventional fungicides have poor activity, limited to certain fungi, and are not satisfactorily maintained for prolonged periods. Even though some fungicides may bear satisfactory fungicidal effects, as they require improvements in respect of environment and health safety and are also required to achieve a high fungicidal effect at a smaller dosage and lack resistance management.
We found that this objective in part or complete can be achieved by the combination of active compounds defined at the outset. Thus, the present inventors have intensively studied to solve these problems and found that by combining fungicidal composition having myclobutanil and validamycin in different formulation and percentages have astonishing effects in controlling fungi and by reducing the amount of dosage than in a case of using an active compound alone.
Therefore, the present invention provides a novel synergistic fungicidal composition with myclobutanil and validamycin and purpose thereof. The synergy of this fungicidal composition having myclobutanil and validamycin with dual mode of action (ergo sterol biosynthesis pathway inhibition + trehalose-degrading enzyme inhibition) can generate efficient synergism and can enable broad spectrum satisfactory disease control from soil borne, seed borne and foliar plant diseases for prolonged period at lower dose, powered by preventive, curative and systemic activity, rain fastness, vapour activity and phytotonic effect.
This combination can be developed in the form of Emulsifiable Concentrates (EC), Dispersible Concentrates (DC), Oil Dispersions (OD), Suspension Concentrates (SC), Soluble Liquids (SL), Suspoemulsion (SE), Emulsion Concentrates (EW), Microemulsions, Wettable Powders (WP), Water-Dispersible Granules (WG), Soluble Powders (SP), Granules (G), Oil Solutions (OS), Aqueous Suspensions (AS), Aqueous Solutions (AS), Microencapsulated Suspensions (ME), and Microencapsulated Emulsions (MEC), mixed formulation of Suspension Concentrate and Capsule Suspension (ZC) and other conventional formulation and with different percentages and can be used for foliar applications or soil applications and seed treatment. This unique fungicide combination can also effectively check the resistance development in pathogen.
The present invention involves the mixture of two active ingredients which are classified under triazole fungicides and antibiotic fungicide are described herein thereof.
Triazole fungicides (TFs) are systemic fungicides that work by inhibiting the biosynthesis of sterols specifically ergosterol, which is a vital component of the fungal cell membrane. This inhibition disrupts the cell membrane structure, leading to the death of the fungus. Myclobutanil is classified as a triazole fungicide.
Myclobutanil (IUPAC name: 2-((1H-1,2,4-triazol-1-yl) methyl)-2-(4-chloro phenyl) hexanenitrile; molecular formula: C15H17ClN4; ¬molecular weight: 288.77 g/mol) is a broad spectrum systemic and effective fungicide that will translocate into new growth with preventative and curative effects against a wide range of plant pathogenic fungi.

Myclobutanil belongs to a substituted triazole chemical class of compound used in several crops and ornamental plants to control diseases like rust, powdery mildew, and canker etc. caused by fungi. Myclobutanil is a sterol demethylation inhibitor (DMI fungicide) specifically inhibiting ergosterol biosynthesis. Ergosterol is a critical component of fungal cell membranes.
Validamycin is an antibiotic fungicide that belongs to the chemical class of glucopyranoside. Trehalose disaccharide is an essential glucose derivative that plays a key role as an energy source in insects and fungal cells. Validamycin is a potent competitive inhibitor of the trehalose-degrading enzyme which led to inhibition of the metabolism of trehalose and destroys fungi by suppressing their ability to grow or reproduce. Such mode of action provides a desirable biological selectivity of validamycin. Because vertebrates are not dependent for their metabolism on disaccharide trehalose hydrolysis.
The synergistic fungicidal composition of the present invention controls different groups of fungi selected from ascomycota, deuteromycota, basidiomycota and oomycota on a wide variety of crops.
The synergistic fungicidal composition of the present invention is also used in seed treatment to protect against diseases which impair good seed germination and seedling development.
The synergistic fungicidal composition of the present invention controls many diseases in plants which include leaf spot, blight, dollar spot, rusts, scab, powdery mildew, downy mildew, net blotch, blight, summer patch, brown patch, stem canker, damping-off and rot.
The synergistic fungicidal composition of the present invention used to controls many diseases in several plants selected from but not limited to GMO (genetically modified organism) and non-GMO varieties selected from cotton (gossypium spp.), paddy (oryza sativa), wheat (triticum aestavum), barley (hordeum vulgare), maize (zea mays), sorghum (sorghum bicolor), pearl millet (pennisetum glaucum), sugarcane (saccharum officinarum), sugarbeet (beta vulgaris), soybean (glycin max), peanut (arachis hypogaea), sunflower (helianthus annuus), mustard (brassica juncea), rape seed (brassica napus), linseed (linum usitatissimum), sesame (sesamum indicum), green gram (vigna radiata), black gram (vigna mungo), chickpea (cicer aritinum), cowpea (vigna unguiculata), redgram (cajanus cajan), frenchbean (phaseolus vulgaris), indian bean (lablab purpureus), horse gram (macrotyloma uniflorum), field pea (pisum sativum), cluster bean (cyamopsis tetragonoloba), lentils (lens culinaris), brinjal (solanum melongena), cabbage (brassica oleracea var. capitata), cauliflower (brassica oleracea var. botrytis), okra (abelmoschus esculentus), onion (allium cepa l.), tomato (solanum lycopersicun), potato (solanum tuberosum), sweet potato (ipomoea batatas), chilly (capsicum annum), garlic (allium sativum), cucumber (cucumis sativus), muskmelons (cucumis melo), watermelon (citrullus lanatus), bottle gourd (lagenaria siceraria), bitter gourd (momordica charantia), radish (raphanus sativus), carrot (dacus carota subsp. sativus), turnip (brassic rapa subsp rapa), apple (melus domestica), banana (musa spp.), citrus groups (citrus spp.), grape (vitis vinifera), guava (psidium guajava), litchi (litchi chinensis), mango (mangifera indica), papaya (carica papaya), pineapple (ananas comosus), pomegranate (punica granatum) , sapota (manilkara zapota), tea (camellia sinensis), coffea (coffea arabica), turmeric (curcuma longa), ginger (zingiber officinale), cumin (cuminum cyminum), fenugreek (trigonella foenumgraecum), fennel (foeniculum vulgare), coriander (coriandrum sativum), ajwain (trachyspermum ammi), psyllium (plantago ovate), black pepper (piper nigrum), stevia (stevia rebaudiana), safed musli (chlorophytum tuberosum), drum stick (moringa oleifera), coconut (coco nucifera), mentha (mentha spp.), rose (rosa spp.), jasmine (jasminum spp.), marigold (tagetes spp.), common daisy (bellis perennis), dahlia (dahlia hortnesis), gerbera (gerbera jamesonii) and carnation (dianthus caryophyllus).
The first embodiment of the present invention provides a synergistic fungicidal composition comprising:
at least one triazole fungicide and
at least one antibiotic fungicide.
First aspect of the first embodiment, the triazole fungicide is selected from but not limited to the group comprising tebuconazole, propiconazole, epoxiconazole, difenoconazole, myclobutanil, imazalil, triadimefon, triadimenol, flusilazole and penconazole; preferably myclobutanil.
Second aspect of the first embodiment, the antibiotic fungicide is selected from but not limited to the group comprising aureofungin, blasticidin-S, cycloheximide, griseofulvin, kasugamycin, natamycin, ningnanmycin, streptomycin and validamycin; preferably validamycin.
Third aspect of the first embodiment, the triazole fungicide and antibiotic fungicide are present in the weight ratio of (1-60): (1-60); preferably in the ratio of (1-40): (1-40).
The second embodiment of the present invention provides a synergistic fungicidal composition comprising:
at least one triazole fungicide;
at least one antibiotic fungicide; and
at least one agriculturally acceptable excipient.
First aspect of the second embodiment, the triazole fungicide is selected from but not limited to the group comprising tebuconazole, propiconazole, epoxiconazole, difenoconazole, myclobutanil, imazalil, triadimefon, triadimenol, flusilazole and penconazole; preferably myclobutanil.
Second aspect of the second embodiment, the antibiotic fungicide is selected from but not limited to the group comprising aureofungin, blasticidin-S, cycloheximide, griseofulvin, kasugamycin, natamycin, ningnanmycin, streptomycin and validamycin; preferably validamycin.
Third aspect of the second embodiment, the ratio of triazole fungicide and antibiotic fungicide are present in the weight ratio of (1-80): (1-80); preferably in the ratio of (1-40): (1-40).
Fourth aspect of the second embodiment, agriculturally acceptable excipient selected from but not limited to the group comprising liquid medium, surfactants, stabilizer, anti-freezing agent, antifoaming agents, anticaking agent, dispersing agents, adjuvant, and antibacterial agents. These are selected according to the respective types of formulation requirements, and which will facilitate in the preparation different formulations.
Further aspect of the second embodiment, liquid medium acts as a carrier for the active ingredients and provides a stable environment for suspension selected form but not limited to water and organic solvents; preferably water.
Further aspect of the second embodiment, surfactant includes wetting agent and emulsifier.
Further aspect of the second embodiment, wetting agent is selected from but not limited to block copolymers.
Further aspect of the second embodiment, the block copolymers selected from the but not limited to styrene-butadiene block copolymer (SBS), butyl based block copolymer, poly(ethylene oxide)-poly(propylene oxide)-poly(ethylene oxide) (PEO-PPO-PEO), polystyrene-poly(ethylene oxide) (PS-PEO), poly(butadiene)-poly(styrene) (PB-PS), poly(methyl methacrylate)-poly(butadiene)-poly(methyl methacrylate) (PMMA-PB-PMMA), poly(caprolactone)-poly(ethylene glycol) (PCL-PEG) and poly(ethylene glycol)-poly(propylene glycol)-poly(ethylene glycol) (PEG-PPG-PEG); preferably butyl based block copolymer.
Further aspect of the second embodiment, stabilizer includes antioxidant, chelating agent, pH adjusters, UV absorber, stabilizing polymers, and inert filler.
Further aspect of the second embodiment, anti-freezing agent selected from but not limited to ethylene glycol, propylene glycol, glycerol, calcium chloride, sodium acetate, potassium acetate and urea; preferably propylene glycol.
Further aspect of the second embodiment, antifoaming agents selected from but not limited to silicone-based antifoams, polyethylene glycol-based antifoams, mineral oil-based antifoams, ethylene glycol-based antifoams, polysorbate-based antifoams, dimethicone-based antifoams, polypropylene glycol-based antifoams, vegetable oil-based antifoams, alkyl siloxane-based antifoams and fatty acid-based antifoams; preferably alkyl siloxane-based antifoams; more preferably siloxane polyalkyleneoxide.
Further aspect of the second embodiment, dispersing agents selected from but not limited to polyethylene glycol, polysorbate, poly acrylate, poly(methyl methacrylate), polyvinyl alcohol, poly ethoxylated alcohol, poly ethoxylated fatty acids, polyacrylic acid, polyvinylpyrrolidone, alkyl sulfonates, aryl sulfonates, sodium tripolyphosphate, sodium dodecyl sulfate, sodium lignosulfonate, sodium carboxymethyl cellulose, hydroxypropyl methylcellulose, sorbitan esters (e.g., sorbitan monolaurate, sorbitan monooleate), gum arabic and carbomer and/or their comb polymers; preferably poly(methyl methacrylate) and polyethylene glycol comb polymer.
Further aspect of the second embodiment, adjuvant includes but not limited to spreader, sticker, penetrant, drift control agent, preservative, buffering agent, thickener, compatibility agent, binder and safener.
Further aspect of the second embodiment, thickener selected from but not limited to polysaccharides / carboxymethyl cellulose / bentonite clay, hydroxy propyl cellulose montmorillonite, bentonite, magnesium aluminium silicate and attapulgite; preferably water-soluble polysaccharides.
Further aspect of the second embodiment, antibacterial agent selected from but not limited to triclosan, triclocarban, clotrimazole, miconazole, copper-based compounds, chlorothalonil, benzisothiazolin-3-one (BIT), 5-chloro-2-methyl-4-isothiazolin-3-one, 2-methyl-4-isothiazolin-3-one (MIT), octylisothiazolinone (OIT) and dodecylbenzenesulfonic acid sodium salt (DBSA); preferably benzisothiazolin-3-one (BIT).
The third embodiment of the present invention provides a synergistic fungicidal composition comprising:
myclobutanil;
validamycin;
liquid medium;
wetting agent;
antifreezing agent;
antifoaming agent;
dispersing agent;
adjuvant; and
antibacterial agent.
First aspect of the third embodiment, synergistic fungicidal composition comprising a combination of myclobutanil and validamycin; wherein myclobutanil and validamycin present in the weight ratio of (1-80): (1-80); preferably in the ratio of (1-40): (1-40); more preferably in the ratio of (1-20): (1-20).
Second aspect of the third embodiment, agriculturally acceptable excipient selected from but not limited to liquid medium, wetting agent, anti-freezing agent, antifoaming agents, dispersing agents, adjuvant, and antibacterial agents. These are selected according to the respective types of formulation requirements, and which will facilitate in the preparation different formulations.
Further aspect of the third embodiment, liquid medium acts as a carrier for the active ingredients and provides a stable environment for suspension selected form but not limited to water and organic solvents; preferably water.
Further aspect of the third embodiment, surfactant includes wetting agent and emulsifier.
Further aspect of the third embodiment, wetting agent is selected from but not limited to block copolymers.
Further aspect of the third embodiment, the block copolymers selected from the but not limited to styrene-butadiene block copolymer (SBS), butyl based block copolymer, poly(ethylene oxide)-poly(propylene oxide)-poly(ethylene oxide) (PEO-PPO-PEO), polystyrene-poly(ethylene oxide) (PS-PEO), poly(butadiene)-poly(styrene) (PB-PS), poly(methyl methacrylate)-poly(butadiene)-poly(methyl methacrylate) (PMMA-PB-PMMA), poly(caprolactone)-poly(ethylene glycol) (PCL-PEG) and poly(ethylene glycol)-poly(propylene glycol)-poly(ethylene glycol) (PEG-PPG-PEG); preferably butyl based block copolymer.
Further aspect of the third embodiment, anti-freezing agent selected from but not limited to ethylene glycol, propylene glycol, glycerol, calcium chloride, sodium acetate, potassium acetate and urea; preferably propylene glycol.
Further aspect of the third embodiment, antifoaming agents selected from but not limited to silicone-based antifoams, polyethylene glycol-based antifoams, mineral oil-based antifoams, ethylene glycol-based antifoams, polysorbate-based antifoams, dimethicone-based antifoams, polypropylene glycol-based antifoams, vegetable oil-based antifoams, alkyl siloxane-based antifoams and fatty acid-based antifoams; preferably alkyl siloxane-based antifoams; more preferably siloxane polyalkyleneoxide.
Further aspect of the third embodiment, dispersing agents selected from but not limited to polyethylene glycol, polysorbate, poly acrylate, poly(methyl methacrylate), polyvinyl alcohol, poly ethoxylated alcohol, poly ethoxylated fatty acids, polyacrylic acid, polyvinylpyrrolidone, alkyl sulfonates, aryl sulfonates, sodium tripolyphosphate, sodium dodecyl sulfate, sodium lignosulfonate, sodium carboxymethyl cellulose, hydroxypropyl methylcellulose, sorbitan esters (e.g., sorbitan monolaurate, sorbitan monooleate), gum arabic and carbomer and/or their comb polymers; preferably poly(methyl methacrylate) and polyethylene glycol comb polymer.
Further aspect of the third embodiment, adjuvant includes but not limited to spreader, sticker, penetrant, drift control agent, preservative, buffering agent, thickener, compatibility agent, binders and safener.
Further aspect of the third embodiment, thickener selected from but not limited to polysaccharides / carboxymethyl cellulose / bentonite clay, hydroxy propyl cellulose montmorillonite, bentonite, magnesium aluminium silicate and attapulgite; preferably water-soluble polysaccharides.
Further aspect of the third embodiment, antibacterial agent selected from but not limited to triclosan, triclocarban, clotrimazole, miconazole, copper-based compounds, chlorothalonil, benzisothiazolin-3-one (BIT), 5-chloro-2-methyl-4-isothiazolin-3-one, 2-methyl-4-isothiazolin-3-one (MIT), octylisothiazolinone (OIT) and dodecylbenzenesulfonic acid sodium salt (DBSA); preferably benzisothiazolin-3-one (BIT).
The fourth embodiment of the present invention provides a synergistic fungicidal composition comprising:
myclobutanil and
validamycin.
First aspect of the fourth embodiment, synergistic fungicidal composition comprising a combination of myclobutanil and validamycin; wherein myclobutanil and validamycin present in the weight ratio of (1-80): (1-80); preferably in the ratio of (1-20): (1-20); more preferably in the ratio of (1-10): (1-10).
Further aspect of the fourth embodiment, the composition of fourth embodiment comprising at least one agriculturally acceptable excipient there of which is / are used in preparation desired formulation.
Further aspect of the fourth embodiment, the composition of fourth embodiment is formulated as suspension concentrates (SC) / Soluble liquid (SL).
The fifth embodiment of the present invention provides a synergistic fungicidal composition comprising:
myclobutanil;
validamycin;
water;
butyl based block copolymer;
propylene glycol;
siloxane polyalkyleneoxide;
comb polymer;
polysaccharides; and
benzisothiazolin-3-one.
First aspect of the fifth embodiment, synergistic fungicidal composition comprising a combination of myclobutanil and validamycin; wherein myclobutanil and validamycin present in the weight ratio of (1-80): (1-80); preferably in the ratio of (1-20): (1-20); more preferably in the ratio of (1-10): (1-10).
Further aspect of the embodiment, the composition of fifth embodiment is formulated as suspension concentrates (SC) / Soluble liquid (SL).
Another embodiment of the present invention provides a process for the preparation of a fungicidal formulation comprising:
add water into premix vessel,
add wetting agent, anti-freezing, dispersing agent, anti-bacterial agent and antifoaming agent to the above vessel under continuous stirring.
add myclobutanil and validamycin to the above slurry and stirred for 30-60 minutes to get homogenous mixture.
after mixing the above material, optionally mill or grind to get the desired particle size of minimum 99% by passing through 500 bss by wet sieving method and remove any oversized particles or agglomerate.
the obtained wet milled slurry particles with size d50 <5-micron material, then transfer into the blender and add thickener 2% gum solution to get desired viscosity.
mix well until a homogenous mixture is obtained, pack the formulation and seal it.
Another embodiment of the present invention, the fungicidal composition of the present invention used to control fungal diseases in several crops specifically selected from rice, wheat, fruits, roots, tubers, vegetables, maize, grains, sugarcane, cereals and field crops and for various other pest control requirements.
Another embodiment of the present invention, the fungicidal composition further comprises at least another agrochemical selected from a fungicide, insecticide, herbicide, biocide, nutrient, plant growth regulator, plant activator, fertilizers and likewise.
Another embodiment of the present invention, the fungicidal composition of the present invention shows synergistic effects of better pest control with minimum fungal resistance and improved crop yield and quality.
Another embodiment of the present invention, the synergistic fungicidal composition is applied at different stages of crops for preventive, curative, systemic activity by conventional spraying methods, such as foliar applications or soil applications over the target areas of crops at same time avoiding excessive drift or runoff of the composition securing thorough coverage.
Another embodiment of the present invention, synergistic fungicidal combination decreases natural hazardous effect of single active ingredient and also minimizes the residue deposition in environment.
Advantages of the Present Invention:
The synergistic fungicidal composition of present invention is specifically designed to control fungal diseases in plants by targeting and eliminating the fungal pathogens with dual mode of action of ergo sterol biosynthesis pathway inhibition + trehalose-degrading enzyme inhibition there by enhance crop health and improve overall yields compare to single component of composition, market standards and admixture of those components.
The novel, innovative and synergistic fungicidal composition of present invention making them versatile and adaptable to different application methods and crops for various agricultural practices.
The synergistic fungicidal composition of the present invention has quick action on disease control after application. This quick action will help to prevent further disease spread and reduce crop damage.
Higher efficacy against broader spectrum of fungicides with different modes of action can be used in rotation or as part of an integrated pest management (IPM) strategy to reduce the risk of developing resistant fungal diseases.
The synergistic fungicidal composition of present invention can also be used in seed treatment which protects harvested crops during storage and transportation, preventing post-harvest diseases and ensuring the quality and marketability of the product.
The synergistic fungicidal composition of present invention minimizes the potential negative effects on the environment and non-target organisms. And which is absorbed by the plant system within two hours of the spray and it cannot be washed away by the post application rains.
The best mode of carrying present invention is described in the below given examples. These examples are merely for illustrative purposes only, not to determine the scope of the invention and in no way limit the scope or spirit of the present invention.
EXAMPLES:
EXAMPLE 1: SUSPENSION CONCENTRATES (SC) FORMULATION OF SYNERGISTIC FUNGICIDAL COMPOSITION OF THE PRESENT INVENTION:
TABLE 1:
S. No Ingredient Weight / Weight %
1 Myclobutanil 2.5
2 Validamycin 3.5
3 Butyl based block copolymer 2.5
4 Propylene Glycol 5
5 Siloxane polyalkyleneoxide 0.5
6 Comb polymer 2.5
7 Polysaccharides 0.3
8 Benzisothiazolin-3-one 0.1
9 Water QS
Total 100
EXAMPLE 2: PROCESS FOR PREPARATION OF SUSPENSION CONCENTRATES (SC) FORMULATION OF SYNERGISTIC FUNGICIDAL COMPOSITION OF THE PRESENT INVENTION
Add water, wetting agent, anti-freezing, dispersing agent, anti-bacterial agent and antifoaming agent into the pre blender in the above-mentioned ratios and mix well until a homogenous mixture is obtained. Add myclobutanil and validamycin in the above-mentioned ratios into the above mixture and mix well. Optionally mill or grind to get the desired particle size. Then add thickener to the above obtained material mixed well until to get the homogenous mixture with desired viscosity.
EXAMPLE 3: BIO EFFICACY AND PHYTOTOXICITY TESTS OF THE PRESENT INVENTION
Presently to evaluate the efficacy of myclobutanil 2.5% + validamycin 3.5% SC against different fungal pathogens on different crops and to test their phytotoxicity on the crop after the sprayings have been conducted. Powdery mildew in grape and sheath blight in paddy are taken for evaluation. Along with myclobutanil 2.5% + validamycin 3.5% SC as a combination formulation both the fungicides are tested individually, and with the market standards. The tests are conducted at three dose levels viz., low, medium, and high along with the sole molecule as individual treatments and their efficiency comparison is done with the current competitive market standards. The active ingredients are tested at three different formulation strengths i.e., myclobutanil 2.5% + validamycin 3.5% SC (@1500ml/ha), myclobutanil 2.5% + validamycin 3.5% SC (@1250ml/ha) and myclobutanil 2.5% + validamycin 3.5% SC (@1000ml/ha). To justify the results, the overall effect and other parameters are calculated over untreated check and to see their effect on crop, its yield is recorded. The crops are first divided into plots for each treatment and replicated three times following randomized block design. The spraying method followed was foliar application with the help of a knapsack sprayer and three sprays are with an interval of 10 days.
Method of Observations:
Disease observations: select 5 random plants in the plot and the disease symptoms are scored based on disease rating scale and then the percentage disease index will be calculated.
The observations were taken at 1 day before spraying and at 10 days after spraying.
Take the observation on the crop safety of the fungicide i.e., phytotoxicity / softener observation of fungicide after application at 5 and 10 days after application.
Parameters of Observations:
The disease severity is measured by an index, measured as Percent disease index (PDI) will be calculated by using following formula:–
PDI = (Sum of all disease ratings)/(Total no.of leaves x Maximum disease grade) x 100
The percent reduction is calculated by the following formula –
% Reduction = ( PDI in control plot-PDI in treated plot )/(PDI in control plot)× 100
The effect of these fungicides in combination and alone when applied on crops is assessed based on the yield (quintal per hectare or kg/vine). This parameter defines the crop quality.
Results:
The fungicide combination of myclobutanil 2.5%+validamycin 3.5% SC is effective against wide range of diseases, so the different diseases controlled in different crops in the field experiments were enlisted below,
Paddy– Sheath Blight (Rhizoctonia solanii)
Grape – Powdery mildew (Uncinula necator)
Example – 3.1: Paddy-Sheath Blight
Table 1. Efficacy of spray application of myclobutanil 2.5% + validamycin 3.5% SC formulation against sheath blight in paddy (vertical spread):
Treatments Dose
(g or ml / ha) Percent disease index (PDI) after every spray % Reduction in PDI
Pre 1 2 3 AVG 1 2 3 AVG
Myclobutanil 2.5% + validamycin 3.5% SC 1000 10.8 2 7 11 7.70 91.11 80.11 77.13 82.79
Myclobutanil 2.5% + validamycin 3.5% SC 1250 10.2 2.4 3.5 7 5.78 89.33 90.06 85.45 88.28
Myclobutanil 2.5% + validamycin 3.5% SC 1500 10.2 1.4 2.7 4.6 4.73 93.78 92.33 90.44 92.18
Myclobutanil 10% WP 400 9.3 10.2 8 8.6 9.03 54.67 77.27 82.12 71.35
Validamycin 3% L 650 11.4 9 14 19 13.35 60.00 60.23 60.50 60.24
Hexaconazole 5% + validamycin2.5% SC 1000 10.2 8 12 21 12.80 64.44 65.91 56.34 62.23
Propiconazole 10.7% + tricyclazole 34.2% SC 700 9.6 11.1 11.1 10.8 10.65 50.67 68.47 77.55 65.56
Untreated -- 10.5 22.5 35.2 48.1 29.08 0.00 0.00 0.00 0.00
The data presented in Table. 1 showed the effect of different fungicidal treatments in combination, alone and the effect of market standards on disease severity of horizontal spread of sheath blight disease in paddy. The percent reduction in disease incidence was also explained through the data represented in above table with treatments compared over control. In general, all treatments, at each rate of applications after three consecutive sprayings significantly reduced the disease severity comparing with the untreated control. The combination fungicidal treatments were more effective than sole molecules and market standards. The disease severity is measured as Percent Disease Index (PDI), this varied between 9.3 to 11.4 among all the treatments before spraying (pre-treatment/pre-spray). The disease severity was measured 10 days after spraying and the spraying was done thrice in the crop. Among the tested fungicidal treatments, myclobutanil 2.5% + validamycin 3.5% SC @ 1500 ml/ha and myclobutanil 2.5% + validamycin 3.5% SC @ 1250 ml/ha were the most effective treatments. The PDI recorded in myclobutanil 2.5% + validamycin 3.5% SC @ 1500 ml/ha was 10.2 before spray and reduced to 1.4, 2.7, 4.6 after 1st, 2nd and 3rd spraying. The second-best treatment was myclobutanil 2.5% + validamycin 3.5% SC @ 1250 ml/ha where the PDI recorded was recorded as 10.2 before spraying and came down to 2.4 after 1st spray and recorded as 3.5, 7 after 2nd and 3rd spray. The lowest dose of myclobutanil 2.5% + validamycin 3.5% SC @ 1000 ml/ha with 10.8 as pre-treatment PDI, followed by 2 after end of first spray and reduced to 7 after 2nd and 11 after 3rd spray. While the market standards did not show much reduction in PDI. When calculated as percent disease reduction over control regarding the examined rates of fungicidal combination and as expected, recommended rates reduced the disease severity compared with fungicides applied alone and with market standards too. The percent reduction recorded were 92.18% (myclobutanil 2.5% + validamycin 3.5% SC @ 1500 ml/ha), 88.28% (myclobutanil 2.5% + validamycin 3.5% SC @ 1250 ml/ha) and 82.79% (myclobutanil 2.5% + validamycin 3.5% SC @ 1000 ml/ha), respectively, and the market standards recorded a percent reduction of 65.56% (propiconazole 10.7% + tricyclazole 34.2% SC @ 700 ml/ha) and 62.23% (hexaconazole 5% + validamycin2.5% SC @ 1000 ml/ha) which was lower than the combination treatments.
Table 2. Efficacy of spray application of myclobutanil 2.5% + validamycin 3.5% SC formulation against sheath blight in paddy (horizontal spread):
Treatments Dose
(g or ml /ha) Percent disease index (PDI)
after every spray % Reduction in PDI
Pre 1 2 3 AVG 1 2 3 AVG
Myclobutanil 2.5% + validamycin 3.5% SC 1000 10.4 3 7 11 7.85 88.00 82.05 77.08 82.38
Myclobutanil 2.5% + validamycin 3.5% SC 1250 9.3 2 4.6 6 5.48 92.00 88.21 87.50 89.24
Myclobutanil 2.5% + validamycin 3.5% SC 1500 9.2 1.2 2 3.8 4.05 95.20 94.87 92.08 94.05
Myclobutanil 10% WP 400 10 4 9 13 9.00 84.00 76.92 72.92 77.95
Validamycin 3% L 650 9 5 10 14 9.50 80.00 74.36 70.83 75.06
Propiconazole 10.7% + tricyclazole 34.2% SC 700 9.5 6 11 16 10.63 76.00 71.79 66.67 71.49
Hexaconazole 5% + validamycin2.5% SC 1000 8.9 11.2 11.9 13.1 11.28 55.20 69.49 72.71 65.80
Untreated -- 10.3 25 39 48 30.58 0.00 0.00 0.00 0.00
The data presented in Table. 2 showed the effect of different fungicidal treatments in combination, alone and the effect of market standards on disease severity of horizontal spread of sheath blight disease in paddy. The percent reduction in disease incidence was also explained through the data represented in above table with treatments compared over control. In general, all treatments, at each rate of applications after three consecutive sprayings significantly reduced the disease severity comparing with the untreated control. The combination fungicidal treatments were more effective than sole molecules and market standards. The disease severity is measured as Percent Disease Index (PDI), this varied between 8.9 to 10.4 among all the treatments before spraying (pre-treatment / pre-spray). The disease severity was measured 10 days after spraying and the spraying was done thrice in the crop. Among the tested fungicidal treatments, myclobutanil 2.5% + validamycin 3.5% SC @ 1500 ml/ha and myclobutanil 2.5% + validamycin 3.5% SC @ 1250 ml/ha were the most effective treatments. The PDI recorded in myclobutanil 2.5% + validamycin 3.5% SC @ 1500 ml/ha was 9.2 before spray and reduced to 1.2, 2, 3.8 after 1st, 2nd and 3rd spraying. The second-best treatment was myclobutanil 2.5% + validamycin 3.5% SC @ 1250 ml/ha where the PDI recorded was recorded as 9.3 before spraying and came down to 2 after 1st spray and recorded as 4.6, 6 after 2nd and 3rd spray. The lowest dose of myclobutanil 2.5%+validamycin 3.5% SC @ 1000 ml/ha with 10.4 as pre-treatment PDI, followed by 3 after end of first spray and reduced to 7 after 2nd and 11 after 3rd spray. While the market standards did not show much reduction in PDI. When calculated as percent disease reduction over control regarding the examined rates of fungicidal combination and as expected, recommended rates reduced the disease severity compared with fungicides applied alone and with market standards too. The percent reduction recorded were 94.05% (myclobutanil 2.5% + validamycin 3.5% SC @ 1500 ml/ha), 89.24% (myclobutanil 2.5% + validamycin 3.5% SC @ 1250 ml/ha) and 82.38% (myclobutanil 2.5% + validamycin 3.5% SC @ 1000 ml/ha), respectively, and the market standards recorded a percent reduction of 65.08% (hexaconazole 5% + validamycin2.5% SC @ 1000 ml/ha) and 71.49% (propiconazole 10.7% + tricyclazole 34.2% SC @ 700 ml/ha) which was lower than the combination treatments.
Table 3. Effect of myclobutanil 2.5% + validamycin 3.5% SC formulation on yield in paddy:
Treatments Dose (g or ml / ha) Yield (q/ha)
Myclobutanil 2.5% + validamycin 3.5% SC 1000 45
Myclobutanil 2.5% + validamycin 3.5% SC 1250 48.2
Myclobutanil 2.5% + validamycin 3.5% SC 1500 50.6
Myclobutanil 10% WP 400 41
Validamycin 3% L 650 38.4
Propiconazole 10.7% + tricyclazole 34.2% SC 700 36.2
Hexaconazole 5% + validamycin2.5% SC 1000 33
Untreated -- 29
The yield of paddy recorded in different treatments as shown in the table above (Table 3.) implies that the combination molecule at the three doses positively affected the yield of the crop. The highest yield was recorded in myclobutanil 2.5% + validamycin 3.5% SC @ 1500 ml/ha with 50.6 q/ha, followed by myclobutanil 2.5% + validamycin 3.5% SC @ 1250 ml/ha with 48.2 q/ha and myclobutanil 2.5% + validamycin 3.5% SC @ 1000 ml/ha with 45 q/ha. While the individual molecules and market standards recorded yields ranging between 33-41 q/ha which were inferior to the yield recorded in the combination molecule treatments.
Table 4. Phytotoxicity of Myclobutanil 2.5% + Validamycin 3.5% SC formulation on Paddy:
Treatments Days Visual Rating Scale
Yellowing Necrosis Wilting Vein
Clearing Leaf Tip / Margin Dying Stunting / Dwarfing
Myclobutanil 2.5% + validamycin 3.5% SC@1000ml/ha 5 0 0 0 0 0 0
10 0 0 0 0 0 0
Myclobutanil 2.5% + validamycin 3.5% SC @1250ml/ha 5 0 0 0 0 0 0
10 0 0 0 0 0 0
Myclobutanil 2.5% + validamycin 3.5% SC @1500ml/ha 5 0 0 0 0 0 0
10 0 0 0 0 0 0
Myclobutanil 10% WP @ 400ml/ha 5 0 0 0 0 0 0
10 0 0 0 0 0 0
Validamycin 3% L @650ml/ha 5 0 0 0 0 0 0
10 0 0 0 0 0 0
Propiconazole 10.7% + tricyclazole 34.2% SC @ 700ml/ha 5 0 0 0 0 0 0
10 0 0 0 0 0 0
Hexaconazole 5% + validamycin2.5% SC @1000ml/ha 5 0 0 0 0 0 0
10 0 0 0 0 0 0
Untreated 5 0 0 0 0 0 0
10 0 0 0 0 0 0
The phytotoxicity effect of the fungicide combination i.e., myclobutanil 2.5% + validamycin 3.5% SC on paddy crop was tested after 5 and 10 days after spraying. The crop was checked for symptoms like yellowing, necrosis, wilting, vein clearing, leaf tip or leaf margin dying and stunting or dwarfing of plants. After thorough observations, it could be concluded that the crop did not show any symptoms of phytotoxicity. Therefore, the present fungicide combination can be considered a safe molecule.
Example – 3.2: Grape – powdery mildew
Table 5. Efficacy of spray application of myclobutanil 2.5% + validamycin 3.5% SC formulation against powdery mildew in grape:
Treatments Dose
(g or ml / ha) Percent disease index (PDI)
after every spray % Reduction in PDI
Pre 1 2 3 AVG 1 2 3 AVG
Myclobutanil 2.5% + validamycin 3.5% SC 1000 17 6 12.4 13.2 12.15 81.54 77.37 81.33 80.08
Myclobutanil 2.5% + validamycin 3.5% SC 1250 16 6 9 13 11.00 81.54 83.58 81.61 82.24
Myclobutanil 2.5% + validamycin 3.5% SC 1500 16.2 5.2 8 10 9.85 84.00 85.40 85.86 85.09
Myclobutanil 10% WP 400 17.2 15 17 18 16.80 53.85 68.98 74.54 65.79
Validamycin 3% L 650 16.6 14 15 16 15.40 56.92 72.63 77.37 68.97
Validamycin 8.3%+ mancozeb 66.7% WP 1500 17 12 18 20 16.75 63.08 67.15 71.71 67.31
Hexaconazole 5% + validamycin2.5% SC 1000 16.7 15 18 22 17.93 53.85 67.15 68.88 63.29
Untreated -- 16.8 32.5 54.8 70.7 43.70 0.00 0.00 0.00 0.00
The data presented in Table. 5 showed the effect of different fungicidal treatments in combination, alone and the effect of market standards on disease severity of powdery mildew disease in grape crop. The percent reduction in disease incidence was also explained through the data represented in above table with treatments compared over control. In general, all treatments, at each rate of applications after three consecutive sprayings significantly reduced the disease severity comparing with the untreated control. The combination fungicidal treatments were more effective than sole molecules and market standards. The disease severity is measured as percent disease index (PDI), this varied between 16 to 17.2 among all the treatments before spraying (pre-treatment/pre-spray). The disease severity was measured 10 days after spraying and the spraying was done thrice in the crop. Among the tested fungicidal treatments, myclobutanil 2.5% + validamycin 3.5% SC @ 1500 ml/ha and myclobutanil 2.5% + validamycin 3.5% SC @ 1250 ml/ha were the most effective treatments. The PDI recorded in myclobutanil 2.5% + validamycin 3.5% SC @ 1500 ml/ha was 16.2 before spray and reduced to 5.2, 8, 10 after 1st, 2nd and 3rd spraying. The second-best treatment was myclobutanil 2.5% + validamycin 3.5% SC @ 1250 ml/ha where the PDI recorded was recorded as 16 before spraying and came down to 6 after 1st spray and recorded as 9, 13 after 2nd and 3rd spray. The lowest dose of myclobutanil 2.5% + validamycin 3.5% SC @ 1000 ml/ha with 17 as pre-treatment PDI, followed by 6 after end of first spray and reduced to 12.4 after 2nd and 13.2 after 3rd spray. While the market standards did not show much reduction in PDI. When calculated as percent disease reduction over control regarding the examined rates of fungicidal combination and as expected, recommended rates reduced the disease severity compared with fungicides applied alone and with market standards too. The percent reduction recorded were 85.09% (myclobutanil 2.5% + validamycin 3.5% SC @ 1500 ml/ha), 82.24% (myclobutanil 2.5% + validamycin 3.5% SC @ 1250 ml/ha) and 80.08% (myclobutanil 2.5% + validamycin 3.5% SC @ 1000 ml/ha), respectively, and the market standards recorded market standards recorded a percent reduction of 63.29% (hexaconazole 5% + validamycin2.5% SC @ 1000 ml/ha) and 67.31% (validamycin 8.3%+mancozeb 66.7% WP @ 1500 ml/ha) which was lower than the combination treatments.
Table 6. Effect of myclobutanil 2.5% + validamycin 3.5% SC formulation on yield of grape:
Treatments Dose (g or ml/ha) Yield (kg/vine)
Myclobutanil 2.5% + validamycin 3.5% SC 1000 18
Myclobutanil 2.5% + validamycin 3.5% SC 1250 21
Myclobutanil 2.5% + validamycin 3.5% SC 1500 23
Myclobutanil 10% WP 400 15
Validamycin 3% L 650 11
Validamycin 8.3% + mancozeb 66.7% WP 1500 8
Hexaconazole 5% + validamycin2.5% SC 1000 7.40
Untreated -- 6
The yield of grape recorded in different treatments as shown in the table above (Table 6.) implies that the combination molecule at the three doses positively affected the yield of the crop and the quality of pods was also superior. The highest yield was recorded in myclobutanil 2.5% + validamycin 3.5% SC @ 1500 ml/ha with 23 kg/vine, followed by myclobutanil 2.5% + validamycin 3.5% SC @ 1250 ml/ha with 21 kg/vine and myclobutanil 2.5% + validamycin 3.5% SC @ 1000 ml/ha with 18 kg/vine. While the individual molecules and market standards recorded yields ranging between 7.4-15 kg/vine were inferior to the yield recorded in the combination molecule treatments.
Table 7. Phytotoxicity of myclobutanil 2.5% + validamycin 3.5% SC formulation on grape:
Treatments Days Visual Rating Scale
Yellowing Necrosis Wilting Vein
Clearing Leaf tip / Margin Dying Stunting / Dwarfing
Myclobutanil 2.5% + validamycin 3.5% SC @900ml/ha 5 0 0 0 0 0 0
10 0 0 0 0 0 0
Myclobutanil 2.5% + validamycin 3.5% SC @750ml/ha 5 0 0 0 0 0 0
10 0 0 0 0 0 0
Myclobutanil 2.5% + validamycin 3.5% SC @600ml/ha 5 0 0 0 0 0 0
10 0 0 0 0 0 0
Myclobutanil 10% WP @ 400ml/ha 5 0 0 0 0 0 0
10 0 0 0 0 0 0
Validamycin 3% L @650ml/ha 5 0 0 0 0 0 0
10 0 0 0 0 0 0
Validamycin 8.3% + mancozeb 66.7% WP @ 700 g/ha 5 0 0 0 0 0 0
10 0 0 0 0 0 0
Hexaconazole 5% + validamycin2.5% SC @ 1000 ml/ha 5 0 0 0 0 0 0
10 0 0 0 0 0 0
Untreated 5 0 0 0 0 0 0
10 0 0 0 0 0 0
The phytotoxicity effect of the fungicide combination i.e., myclobutanil 2.5% + validamycin 3.5% SC on grape was tested after 5 and 10 Days after spraying. The crop was checked for symptoms like yellowing, necrosis, wilting, vein clearing, leaf tip or leaf margin dying and stunting or dwarfing of plants. After thorough observations, it could be concluded that the crop did not show any symptoms of phytotoxicity. Therefore, the present fungicide combination can be considered a safe molecule.
It is to be understood that this disclosure is not limited to a particular compositions or specific constituents, which can, of course, vary and that the terminology used herein is for the purpose of describing embodiments only and is not intended to be limiting the scope of the invention. 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, and equivalents thereof known to those skilled in the art and so forth.
Unless defined otherwise, all technical and scientific terms used herein have the same meaning as commonly understood by those skilled in the art to which this disclosure pertains. Although any methods and materials similar or equivalent to those described herein can be used in the practice for testing of the disclosure(s), specific examples of appropriate materials and methods are described herein. The examples set forth above are provided to give those of ordinarily skilled in the art a complete description of how to make and use the embodiments of the compositions or specific constituents, methods of practice, and are not intended to limit the scope of what the inventors regard as their invention. Modifications of the above-described modes for carrying out the invention that is obvious to persons skilled in the art are intended to be within the scope of the following claims. All patents and publications mentioned in the specification are indicative of the levels of skill of those skilled in the art to which the disclosure pertains.
While specific embodiments of the present invention are explicitly disclosed herein, the above specification and examples herein are illustrative and not restrictive. It will be understood that various modifications may be made without departing from the spirit and scope of the invention. Many variations of the disclosure will become apparent to those skilled in the art upon review of this specification and the embodiments below. The full scope of the invention should be determined by reference to the embodiments, along with their full scope of equivalents and the specification, along with such variations. Accordingly, other embodiments are within the scope of the following claims. ,CLAIMS:CLAIMS:
We Claim:
A synergistic fungicidal composition comprising:
at least one triazole fungicide;
at least one antibiotic fungicide; and
at least one agriculturally acceptable excipient.
The composition as claimed in claim 1, wherein the triazole fungicide is myclobutanil and the antibiotic fungicide is validamycin.
The composition as claimed in preceding claims, wherein myclobutanil and validamycin are present in the weight ratio of (1-20): (1-20).
The composition as claimed in claim 1, wherein the agriculturally acceptable excipient selected from the group comprising liquid medium, wetting agent, anti-freezing agent, antifoaming agent, dispersing agents, antibacterial agent and/or adjuvant.
The synergistic fungicidal composition as claimed in preceding claim wherein the formulation is suspension concentrate (SC) / Soluble liquid (SL).
The composition as claimed in preceding claims, wherein the composition controls different groups of fungi selected from ascomycota, deuteromycota, basidiomycota and oomycota on a wide variety of crops selected rice, wheat, fruits, roots, tubers, vegetables, maize, grains, sugarcane, cereals and field crops.
The composition as claimed in preceding claims, wherein the composition is applied at different stages of crops for preventive, curative and systemic activity by conventional spraying methods over the target areas of crops.