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Synergistic Insecticidal Compositions

Abstract: The present disclosure relates to a synergistic insecticidal composition comprising Indoxacarb and fipronil. The composition shows synergistic insecticidal activity. The composition of the present disclosure has high bioefficacy, is cost-effective and environment friendly.

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Patent Information

Application #
Filing Date
21 August 2015
Publication Number
08/2017
Publication Type
INA
Invention Field
AGROCHEMICALS
Status
Email
dewan@rkdewanmail.com
Parent Application

Applicants

GHARDA CHEMICALS LIMITED
B-27/29, MIDC Dombivli (East), Thane – 421203, Maharashtra, India.

Inventors

1. SINGH Kailash Nath
B-27/29, MIDC DOMBIVLI (EAST) THANE 421203, MAHARASHTRA, INDIA
2. GUPTA Heena
B-27/29, MIDC DOMBIVLI (EAST) THANE 421203, MAHARASHTRA, INDIA
3. PANWAR Sandeep Singh
B-27/29, MIDC DOMBIVLI (EAST) THANE 421203, MAHARASHTRA, INDIA
4. AMBIKE Vinayak Ramchandra
B-27/29, MIDC DOMBIVLI (EAST) THANE 421203, MAHARASHTRA, INDIA

Specification

Claims:1. A synergistic insecticidal composition comprising Indoxacarb (I) and Fipronil (II) as active ingredients; wherein the amount of Indoxacarb (I) ranges from 0.001 to 90% on mass basis; and
(I)
the amount of Fipronil (II) ranges from 0.0001 to 90% on mass basis.
(II)
2. The synergistic insecticidal composition as claimed in claim 1, wherein the ratio of the amount of Indoxacarb and the amount of Fipronil ranges from 9:1 to 1:9.
3. The synergistic insecticidal composition as claimed in claim 1, wherein the ratio of the amount of Indoxacarb and the amount of Fipronil is 1:1.
4. The synergistic insecticidal composition as claimed in any of the claims 1 to 3, wherein the agrochemically acceptable additive is selected from the group consisting of vehicles, carriers, fillers, alkalizing agents, acidifying agents, antifreezing agents, anti-settling agents, dispersing agents, disintegrants, lubricants, wetting agents, binding agents, emulsifiers, oils, waxes and surfactants.
5. The synergistic insecticidal composition as claimed in claim 4, wherein the ratio of the amount of the active ingredients to the amount of the agrochemically acceptable additives ranges from 1:66,666 to 9:1.
6. The synergistic insecticidal composition as claimed in claim 1 in the form of a wettable powder formulation, which includes active ingredients ranging from 1 % to 95 % on mass basis; at least one agrochemically acceptable additive selected from the group consisting of emulsifying agents, wetting agents and dispersing agents; and a solid matrix selected from a group consisting of Fuller's earth, kaolin clays, and silica.
7. The synergistic insecticidal composition as claimed in claim 1 in the form of an emulsifiable concentrate formulation, which includes the active ingredients ranging from 0.0001 % to 50 % on mass basis; and at least one agrochemically acceptable additive selected from the group consisting of emulsifiers and non-aqueous fluid media.
8. The synergistic insecticidal composition as claimed in claim 1 in the form of a granular formulation, which includes the active ingredients ranging from 0.01 % to 40 % on mass basis; and at least one agrochemically acceptable additive selected from the group consisting of carriers and binding agents.
9. The synergistic insecticidal composition as claimed in claim 1 in the form of a dust or powder formulation, which includes at least one finely devided solid as an agrochemically acceptable additive.
10. The synergistic insecticidal composition as claimed in claim 1 in the form of a microcapsule formulation, which includes the active ingredients ranging from 5 % to 80 % on mass basis; and at least one agrochemically acceptable additive selected from the group consisting of fluid media, carriers and polymeric materials.
11. The synergistic insecticidal composition as claimed in claim 1 in the form of a suspension concentrate formulation, which includes the active ingredients ranges from 1 % to 80 % on mass basis; and at least one agrochemically acceptable additive selected from the group consisting of wetting agents, antifreeze compounds, and anti-settling agents.

12. The synergistic insecticidal composition as claimed in claim 1 in the form of a suspo-emulsion formulation, which includes at least one agrochemically acceptable additive selected from the group consisting of water and at least one non-aqeuous liquids.
13. The synergistic insecticidal composition as claimed in claim 1 in the form of a microemulsion formulation, which includes at least one agrochemically acceptable additive selected from the group consisting of surfactant solubilizers and co-surfactants.
14. The synergistic insecticidal composition as claimed in claim 1 in the form of a tablet formulation, which includes at least one agrochemically acceptable additive selected from the group consisting of binders, flow aid, lubricants, dispersing agents, fillers and disintegrants.
15. A method for achieving desired bioefficacy on a locus of infestation using the synergistic insecticidal composition as claimed in any of the preceding claims, said method comprising the step of applying an insecticidally effective amount of the synergistic insecticidal composition to the locus of infestation.
16. The method as claimed in claim 15, wherein the amount of the synergistic insecticidal composition applied to the locus is in the range from 10 g a.i./ha to 300 g a.i./ha.

17. The method as claimed in claim 15 or claim 16, wherein the amount of the synergistic insecticidal composition applied to the locus is at least 65 g a.i./ha; wherein the amount of Indoxacarb is at least 15 g /ha. , Description:FIELD
The present disclosure relates to an insecticidal composition.
DEFINITIONS
As used in the present disclosure, the following words and phrases are generally intended to have the meaning as set forth below, except to the extent that the context in which they are used indicate otherwise.
The expression ‘crops’ and/or ‘crop plants’ refer to all physical parts of a plant, including seeds, seedlings, saplings, roots, tubers, stems, stalks, inflorescence, foliage, and fruits. The expression also includes genetically modified crops and conventional crop hybrids.
The expression ‘locus’ refers to soil, crop plants, established vegetation as well as other insect infested living or non-living surfaces where insect control is desired. The locus of infestation also refer to human dwelling, livestock and their dwelling, companion animals and their dwelling and home garden, parks and any surface infested with termites, crickets, ants or like.
The expression ‘insecticide’ refers to any substance or a combination of substances intended for preventing, destroying, or controlling any insect pests, including vectors of human or animal disease, or animals causing harm during or otherwise interfering with the production, processing, storage, transport or marketing of food, agricultural commodities, wood and wood products or animal feedstuffs, or substances which may be administered to animals for the control of insects, arachnids or other pests in or on their bodies. The term ‘insecticide’ remains valid even if substance/s, in addition to above stated purpose, are intended for use in combination of a plant growth regulator, defoliant, desiccant, an agent for thinning fruit, an agent for preventing the premature fall of fruit, and substance(s) applied to crops either before or after harvest to protect them from deterioration during storage and transport.
The expression ‘Insecticidal effective amount’ refers to the quantity of such a substance or a combination of substances, which is capable of producing a decrease in an insect population or a decrease in the damage done by the insect population or causes mortality of the targeted insects.
The expression ‘bioefficacy’ refers to the effect on insects in terms of reduction in the insect population or a reduction in the damage done by insects or causing the mortality of targeted insect across the broad range of situations in which insecticides are generally recommended.
The expression “synergism” refers to the ability of combinations of substances to produce a superior efficacy than the added effect of each substance applied separately. A combination of insecticides is called “synergistic” when it produces a superior efficacy than the added effects of each insecticide applied separately.
The expression “phytotoxicity’ denotes the capacity of a crop protection product to cause temporary or long-lasting damage/injury to crops.
The expression ‘antidote’ describes a substance or a mixture of substance(s) which has the effect of establishing insecticide selectivity, i.e., continued insecticidal bioefficacy, and reduced or non-phytotoxicity to the cultivated crop species.
The expression ‘antidotally effective amount’ describes an amount of an antidote substance(s) which counteracts, to some degree, the phytotoxic response of an a beneficial crop to an insecticide.
BACKGROUND
A variety of insects inhabiting crops pose economic threat to the crops. The most common and widely used method of protection against these harmful insect pests is the use of synthetic insecticides. Synthetic insecticides of many types have been disclosed in the literature and an extensive variety of formulations based on these synthetic insecticides are being marketed by various producers to help combat against insect pest problems.
Insecticides are either recommended as solo formulation or in combination. Some insecticide combinations which shows synergistic effect, had added benefits because lower application rates of synergistic mixture are required to achieve desired bioefficacy and therefore smaller amounts of individual insecticides enter the environment.
Therefore, there is a need to provide an insecticide combination having an improved insecticidal activity, and is cost-effective and less harmful to the environment.
OBJECTS
Some of the objects of the present disclosure, which at least one embodiment herein satisfies, are as follows.
It is an object of the present disclosure to ameliorate one or more problems of the prior art or to at least provide a useful alternative.
An object of the present disclosure is to provide an insecticidal composition having an improved insecticidal activity.
Other objects and advantages of the present disclosure will be more apparent from the following description, which is not intended to limit the scope of the present disclosure.
SUMMARY
The present disclosure provides a synergistic insecticidal composition comprising Indoxacarb and Fipronil as active ingredients. The amount of Indoxacarb in the composition ranges from 0.001 % to 90 % on mass basis and the amount of Fipronil in the composition ranges from 0.0001 % to 90 % on mass basis wherein the ratio between Indoxacarb and Fipronil varies between 9:1 and 1:9.
The synergistic insecticidal composition of the present disclosure can be formulated in the form of wettable powder, granules, water dispersible granules, suspension concentrate, emulsifiable concentrate, powder, dust, flowables, solution, suspo-emulsion, gel, oil dispersion, encapsulated formulations, micro emulsion, multiple emulsions, tablets microcapsule and the like.
The synergistic insecticidal composition of the present disclosure was found to have high insecticidal activity against various insects. Further, to achieve the desired bioefficacy against an insecticidal population, a reduced amount of each insecticide was required, thereby leading to lower environmental loading of insecticide(s) and lower cost during referred combination use.
DETAILED DESCRIPTION
The present disclosure envisages insecticidal composition(s) having synergistic insecticidal activity.
In one aspect, the present disclosure provides a synergistic insecticidal composition comprising synergistically effective amounts of Indoxacarb and Fipronil.
The synergistic insecticidal composition of the present disclosure comprises Indoxacarb (I) and Fipronil (II) as active ingredients.
The amount of Indoxacarb (I) ranges from 0.001% to 90% on mass basis; and

The amount of Fipronil (II) ranges from 0.0001% to 90% on mass basis.

It was surprisingly found that the insecticidal composition of the present disclosure has a synergistic insecticidal activity.
Indoxacarb is an oxadiazine compound. It is a pro-insecticide that transforms in a potent insecticide after its bio-activation inside the body of an insect. It acts by blocking the voltage-gated sodium channels of the nerve cells of insects or pests resulting in ataxia, inhibition of feeding, paralysis, and eventually death of the insects. Indoxacarb is active against lepidopteron larvae and some sucking insects.
Fipronil is a phenyl pyrazole compound having a broad spectrum insecticidal activity. It acts by inhibition of ligand-gated chloride channels of insects.
In accordance with the embodiments of the present disclosure, the ratio of the amount of Indoxacarb and the amount of Fipronil in the synergistic insecticidal composition of the present disclosure ranges from 9:1 to 1:9.
In one embodiment of the present disclosure, the ratio of the amount of Indoxacarb and the amount of Fipronil in the synergistic insecticidal composition is 1:1.
In accordance with the embodiments of the present disclosure, the synergistic insecticidal composition of the present disclosure further comprises agrochemically acceptable additives.
In accordance with the embodiments of the present disclosure, the agrochemically acceptable additives are selected from the group consisting of carriers, vehicles, fillers, alkalizing agents, acidifying agent, anti-freezing agents, anti-settling agents, dispersing agents, disintegrants, lubricants, wetting agents, binding agents, emulsifiers, oils, waxes, surfactants, co-surfactants and other compatible ingredient(s) which ensure optimum performance of the combination of the active ingredients of the present disclosure.
Carrier is a medium used to carry the active ingredients of a composition. The carrier can be a solid, liquid or gaseous medium. The solid mediums include, but are not limited to, mineral clays. Vehicle is a fluid medium selected from the group consisting of water, aliphatic alcohols, aromatic alcohols, acetonitrile, methylene dichloride, hexane, ethers, esters, ketones, and other compatible ingredient(s) which ensure optimum performance of the combination of the active ingredients of the present disclosure.
Alkalizing agent is selected from the group consisting of ammonia solution, potassium hydroxide, sodium bicarbonate, sodium hydroxide, and other compatible ingredient(s) which ensure optimum performance of the combination of the active ingredients of the present disclosure.
Acidifying agent is selected from the group consisting of organic acids and mineral acids, and other compatible ingredient(s) which ensure optimum performance of the combination of the active ingredients of the present disclosure.
Dispersing agent is selected from the group consisting of polyvinyl pyrrolidone, ethoxylated fatty acids, phenyl naphthalene sulphonates, glyceryl esters, and other compatible ingredient(s) which ensure optimum performance of the combination of the active ingredients of the present disclosure.
Wetting agent is selected from the group consisting of alkyl sulfonates, alkyl aryl sulfonates, and sulfates and salts thereof, polyoxyethoxylated fatty amines, lignin derivatives, polyoxyalkylated ethyl phenols, and other compatible ingredient(s) which ensure optimum performance of the combination of the active ingredients of the present disclosure.
Binding agent is selected from the group consisting of starch, gelatin, xanthun gum, cellulose acetate phthalate, and other compatible ingredient(s) which ensure optimum performance of the combination of the active ingredients of the present disclosure.
Emulsifier is selected from the group consisting of sodium lauryl sulphate, sodium dodecyl sulphate, polyoxyethylene stearate, polysorbate, cetyl alcohol, and other compatible ingredient(s) which ensure optimum performance of the combination of the active ingredients of the present disclosure.
In other aspect, the present disclosure provides the synergistic insecticidal composition in a form selected from the group consisting of granules, wettable powders, wettable granules, emulsifiable concentrate, dusts or powders, flowables, solution, suspension concentrate, oil dispersion, suspo-emulsion, and microcapsules.
In accordance with the embodiments of the present disclosure, some formulations of the synergistic insecticidal composition of the present disclosure have special release properties such as extended release, sustained release, and controlled release.
In accordance with the embodiments of the present disclosure, the above mentioned formulations of the synergistic insecticidal composition comprise active ingredient and at least one agrochemically acceptable additive. The term ‘active ingredient’ with respect to the present disclosure refers to the mixture of insecticides Indoxacarb and Fipronil.
The ratio of the amount of the active ingredient to the amount of the agrochemically acceptable additive/s in these formulations ranges from 1:66,666 to 9:1.
The formulations of the synergistic insecticidal composition of the present disclosure are described herein below. Wettable powders are finely-divided solid pesticide formulations which disperse readily in water or other liquid carriers.
The wettable powder formulations of the present disclosure comprise the active ingredients in an amount ranging from 1 % to 95 % on mass basis, and agrochemically acceptable additive/s selected from a group consisting of emulsifying agent, wetting agent and dispersing agent. The active ingredients are retained on a solid matrix. The solid matrix is at least one selected from a group consisting of Fuller's earth, kaolin clays, silica, other readily available wet organic and inorganic solids, absorbent fillers such as diatomaceous earth, and high surface area synthetic silica.
Emulsifiable concentrate (EC) formulations are homogeneous liquid formulations that are emulsifiable in water or dispersible in other fluid medium. Emulsifiable concentrate (EC) formulations of the present disclosure comprise the active ingredient, at least one emulsifier, and at least one non-aqueous fluid medium.
The emulsifiable concentrate formulations of the present disclosure contain the active ingredients in an amount ranging from 0.0001 % to 50 % on mass basis. The non-aqueous fluid medium is selected from the group consisting of xylene, C9 fraction distillate, heavy aromatic naphtha, C6-10 fatty acid methyl ester caprylate/caparate, isophorone, and other non-volatile organic and inorganic fluid mediums.
The EC formulations may contain surfactant emulsifier blends to ensure spontaneous emulsification of EC into water before use.
The ability of an EC formulation to form an emulsion is dependent on the hardness of water. In an embodiment of the present disclosure, the water, used for the preparation of an emulsion, has a hardness of less than 1000 ppm.
Granular formulations include impregnates and coated coarse particles and typically with a size range from 12-60 British Standard (BS) mesh (250- 1405 microns) with at least 80% of the granules within the specified mesh size range. Granular formulations are usually applied without dilution to the locus where bioefficacy is desired.
The amount of active ingredients in the granular formulations of the present disclosure ranges from 0.01 % to 40 % on mass basis.
The granules are composed of at least one carrier material selected from a group consisting of attapulgite, montmorillonite, clay, Kaolin, talc, diatomite, calcite, dolomite, precipitated silica, fumed silica, sand, Fuller's earth, bentonite clay, vermiculite, perlite, corn cob grits, rice hulls, coconut shells and other organic or inorganic materials which can absorb and/or adsorb and/or can be coated with the active ingredients.
The granular formulations further comprise at least one binding agent selected from the group consisting of dextrins, glue, synthetic resins and the like.
In some specialized granular formulations, the active ingredients are dissolved or dispersed in a low volatile oil or a fluid medium, and the resulting liquid is then incorporated on a suitable granular carrier. The granular formulations may comprise at least one low volatile oil or a fluid medium selected from the group consisting of heavy aromatic naphthas, kerosene, petroleum fractions, and vegetable oils. Some specialized granules are designed to sink in water and release oil containing the active ingredient. The released oil floats on the surface of water. Water dispersible granules (WDG, WG or SG) are diluted in water before applying to the insect infested locus or crop. The water dispersible granules are also known as dry flowables.
The amount of active ingredients in the water dispersible granules of the present disclosure ranges from 1 % to 90 % on mass basis.
Water dispersible granules of the present disclosure comprise wetting agents and dispersing agents similar to those used in wettable powders and suspension concentrates mentioned herein above. However, the amount of the dispersing agent is usually higher as compared to their amounts in the wettable powders and suspension concentrates. The water dispersible granules may contain a disintegrant which assists the granules to break in the spray tank.
Dusts or powders are free-flowing admixtures of the active ingredients with finely divided solids such as talc, clays, flours, and other organic and inorganic solids which act as dispersants and earners.
Microcapsule formulations contain the active ingredients in the form of droplets or granules which are enclosed in an inert porous shell, which allows the escape of the enclosed active ingredients to the surroundings at controlled rates.
The amount of active ingredients present in the microcapsule formulations ranges from 5 % to 80% of the total weight.
The encapsulated droplets have a diameter in the range from l micron to 50 microns. The encapsulated droplets may further comprise fluid medium/s in addition to the active ingredients.
The inert porous shells are composed of at least one carrier material selected from the group comprising vermiculite, sintered clay, kaolin, attapulgite clay, sawdust, and granular carbon. The granules can be formed by extrusion, agglomeration, or prilling.
The active ingredients are held in the pores of the inert porous shells with porous membranes sealing the granule pore openings, retaining the active species in liquid form inside the granule pores. Shell or membrane materials include at least one material selected from the group consisting of natural and synthetic rubbers, cellulosic materials, styrene­butadiene copolymers, polyacrylonitriles, polyacrylates, polyesters, polyamides, polyureas, polyurethanes, and starch xanthates.
Microencapsulated formulations comprise products where the active ingredients are surrounded by a barrier or membrane of polymeric or similar material in order to give controlled or delayed release of the active ingredients.
In accordance with one embodiment of the present disclosure, the Microencapsulated formulations are Microcapsule suspensions (CS) in which small spherical particles (typically 1- 20µm in diameter) composed of a core material of active ingredient and an outer shell wall of polymeric material, are suspended in water.
Microcapsule suspensions are usually produced as concentrates that are diluted in water and sprayed conventionally. However, the microcapsule suspension can also be used undiluted as seed treatments.
Microcapsule suspensions can also be combined with other more conventional formulations such as suspension concentrates.
Apart from the capsule suspensions, the formulations can also be prepared in the form of powders or granules (CG), which can either be used directly or re-dispersed into water and sprayed as an aqueous dispersion. The amount of active ingredient in the microencapsulated formulations ranges from 5 % to 39 %.
Suspension concentrate (SC) formulations are stable suspensions of very small particles of active ingredients in a fluid medium. The fluid medium can be either water or oil. Suspension concentrates are also known as flowables.
The suspension concentrate formulations of the present disclosure contain the active ingredients in an amount ranging from 1 % to 80 % on mass basis.
The suspension concentrate formulations comprise at least one additive selected from the group consisting of wetting or dispersing agent, antifreeze compound, and anti-settling agent. The wetting or dispersing agents used in the suspension concentrate formulations is at least one selected from the group consisting of sodium lignosulphonates, sodium naphthalene sulphonate-formaldehyde condensates, calcium dodecyl benzene sulfonates, aromatic alcohol ethoxylates, tristyrylphenol ethoxylate phosphate esters, EO/PO block copolymers, graft copolymers, and the like.
The suspension concentrate of the present disclosure impart its anti-settling property by the addition of a mixture of the following components:
(1) a very fine dispersed phase selected from a group consisting of sodium montmorillonite clays, attapulgite, high surface area silica, and other suitable and agriculturally compatible thixotropic agents; and
(2) a water soluble polymer selected from a group consisting of xanthan gum, cellulose derivatives, natural gums, modified starches, polyvinyl alcohol, polyethylene oxide and the like, or, oil based medium such as polyethylene glycol stearate and the like, which helps in building up a structure or a gel network in the suspension.
The suspension concentrate formulations of the present disclosure further contains an anti-freezing agent. In accordance with one embodiment of the present disclosure, alkylene glycol is used as an anti-freezing agent in the suspension concentrates.
Suspo-emulsion formulation of the present disclosure is a mixture of a suspension concentrate with an oil-in-water emulsion.
The synergistic insecticidal composition of the present disclosure can be in the form of a dispersion in a non-aqeuous liquids such as water-immiscible aliphatic hydrocarbons and vegetable oil base liquids. The typical formulations of this type include oil-miscible flowable suspension (OF), ultra-low volume suspension (SU) and oil dispersion (OD).
Microemulsions are water based formulations and are thermodynamically stable over a wide temperature range due to its very fine droplet size, which is in the range of 0.05 microns to 0.1 microns. The very small droplet size makes these formulations transparent, so that they are regarded as solubilized micellar solutions.
Microemulsion of the present disclosure consists of four components (a) liquid active ingredient or solid active ingredient dissolved in a fluid medium (preferably water immiscible fluid medium); (b) surfactant solubilizers (blend); (c) co-surfactant; and (d) water.
Multiple emulsion is a formulation in which one internal phase is emulsified into a second phase of a different polarity, and the resulting primary emulsion is further emulsified in an external phase that is identical to or different from the initial phase. The final product is, depending on the nature of the different phases, either a water/oil/water (W/O/W) multiple emulsion or an oil/water/oil (O/W/O) multiple emulsion. The surfactants used for the formulation of multiple emulsions are the same as those used for the production of stable concentrated emulsions, both oil-in-water (EW) and water-in-oil (EO).
Gel formulations are structured or thickened solvent-based emulsifiable concentrates, aqueous solutions or dispersions, and are designed to be re-dispersed into water or used undiluted as seed treatments and baits. The gel formulations include CL (contact liquid or gel), GF (gel for seed treatment), GL (emulsifiable gel), GW (water soluble gel) and PC (gel or paste concentrate) formulations.
The Gel formulations of the present disclosure contain the active ingredients in an amount ranging from 0.0005 % to 60% on mass basis.
Tablets are formed by compressing the active ingredients and additives in the form of wet slurry, dry powder, or granules into a range of shapes and sizes, and can be multi-layered or coated. The tablet formulations of the present disclosure contain at least one additive selected from the group consisting of binder, flow aid, lubricant, dispersing agent, filler and disintegrant to ensure satisfactory processing, long-term storage properties, and dissolution into water.
The formulation of the present disclosure can also be prepared as “Jumbo Granules” which can be applied in bad weather conditions.
Specialized applications of the synergistic insecticidal composition of the present disclosure include solutions of the active ingredient in a solvent in which it is completely soluble at the desired concentration. Such solvents are acetone, alkylated naphthalenes, xylene and certain other organic solvents.
In pressurized sprayers the active ingredient is dispersed in a finely-divided form as a result of vaporization of a low boiling dispersant solvent carrier.
The pressurized sprayers are particularly useful for aerial spraying and application by aircraft.
The formulations of the present disclosure can be prepared as a package containing the stated compositions of the formulation together with agrochemically acceptable ingredients of the formulation.
The formulations of the stated compositions can be prepared by a tank mix method, in which the ingredients are obtained separately and combined at the grower site or application site.
An important factor influencing the usefulness of synergistic insecticidal compositions of the present disclosure is its safety or non-phytotoxicity towards crops. In some cases, a beneficial crop is susceptible to the higher concentrations of the insecticide, combination and/or formulation leading to phytotoxicity. To be effective, an insecticide, combination and/or formulation must cause minimal damage (preferably no damage) to the beneficial crop and have the desired bioefficacy towards insects which infest the locus.
Fipronil is known to cause phytotoxicity in green algae through suppression of chlorophyll production. It is also observed that oxadiazine and fiprole compounds may cause undesirable damage to certain crop species, particularly few vegetables, at relatively high application rates. To preserve the beneficial aspects of their use and to minimize crop damage, it becomes a necessity to apply synergistic compositions in combination with an antidote.
If necessary for a particular application, the composition of the present invention may contain an antidotally effective amount of an antidote for any components. Those skilled in the art will be familiar with antidotes which are suitable for use with components of composition and can readily determine an antidotally effective amount for a particular compound and application.
In one embodiment of the present disclosure, an insecticidal composition is combined with an effective amount of an antidote.
In yet another aspect, the present disclosure provides, a method for achieving the desired bioefficacy on a locus of infestation using the synergistic insecticidal composition(s) of the present disclosure. The method comprises applying an insecticidally effective amount of the synergistic insecticidal composition(s) to the locus of infestation.
The compositions of the present disclosure are applied by conventional methods to the locus where insect control is desired. Dust and liquid compositions, for example, can be applied by the use of power-dusters, broom, hand sprayers and spray dusters. The formulations can also be applied from airplanes in a form such as dust or spray, or applied using a rope wick applicator. To protect the growth of the germinating seeds or emerging seedlings, dust and liquid formulations can be distributed in the soil to a depth of at least one-half inch below the soil surface or applied to the soil surface only by spraying or sprinkling. The formulations can also be applied by addition to the irrigation water. This permits penetration of the formulations into the soil together with the irrigation water. This is a very useful attribute in controlling soil insect pests. Dust compositions, granular compositions or liquid formulations applied to the surface of the soil can be distributed below the surface of the soil by conventional means such as discing, dragging or mixing operations.
The present disclosure also provides a method for preventing infestation on a locus using the synergistic insecticidal composition of the present disclosure. The method comprises applying an insecticidally effective amount of the synergistic composition to the locus.
The synergistic insecticidal composition of the present disclosure can be used prophylactically, therapeutically, and curatively.
The choice of formulation and mode of application may affect its bioactivity. Therefore, the selection is made on the basis of the insect type and the severity of the infestation on the crop.
The insecticidal formulations containing a synergistic composition of the present disclosure provides a number of advantages over the use of the formulations comprising Indoxacarb alone and Fipronil alone. First, the amount of the individual insecticide is markedly reduced while achieving a desired level of insecticidal bioefficacy. Second, due to the administration of a lower amount of the insecticides for achieving desired bioefficacy the environmental loading of insecticides is reduced. Third, the synergistic insecticidal composition is considerably more cost-effective as compared to the use of Indoxacarb alone and Fipronil alone.
The synergistic insecticidal composition of the present disclosure is applied by using a technique selected from a group consisting of spraying, pouring, dipping, rubbing, dusting, air-blasting, bait, plant injections, mist-blowing, oiling and the like.
The rate at which the synergistic insecticidal composition of the present disclosure is applied to the locus depends upon the particular type of insect to be controlled, degree of bioefficacy required, the timing, and the method of application.
In accordance with the embodiments of the present disclosure, the synergistic insecticidal composition of the present disclosure is applied to the locus of the infestation in an amount ranging from 10 g a.i./ha to 300 g a.i./ha on mass basis.
The application of the synergistic insecticidal composition is carried out sequentially or simultaneously.
In accordance with the embodiments of the present disclosure, the synergistic insecticidal formulation is applied in an amount ranging from 37.5+37.5 g a.i./ha (37.5g Indoxacarb and 37.5g of fipronil) to 100+100 g a.i./ha (100g Indoxacarb and 100g of fipronil) based on the total amount of the active ingredients present in the insecticidal composition. The synergistic insecticidal compositions of the present disclosure demonstrated synergistic bioefficacy. The stated components can be applied to crops or plants either separately or combined as part of a two-part insecticidal system.
In one embodiment of the present disclosure, the amount of the synergistic insecticidal composition applied to the locus is 65 g a.i./ha. The amount of Indoxacarb in the formulation is at least 15 g a.i./ha.
In another embodiment of the present disclosure, the amount of the synergistic insecticidal composition applied to the locus is upto 200 g a.i./ha. The amount of Indoxacarb in the formulation is upto 125 g a.i./ha.
The synergistic insecticidal compositions of the present disclosure have prophylactic, curative, and therapeutic effectiveness up to 15 days of treatment which may extend longer for certain kind of insects under certain conditions.
In the present disclosure, the use of optimum amounts of the active ingredient in the formulation will depend upon the formulation type, mode of application, equipment used, insect to be controlled and the nature of the crop plant on which the insect is to be controlled.
In accordance with the embodiments of the present disclosure, the locus is a crop selected from the group consisting of cotton, corn, cereals (including wheat, barley, rye, and rice), vegetables (including fruiting vegetable, such as tomatoes, bulb vegetables, leafy vegetables, brassicas and vegetable roots), clovers, legumes (including beans, soybeans, peas and alfalfa), sugar cane, sugarbeets, tobacco, rapeseed (canola), fruits (such as bananas, cherries, oranges, lemons, grapefruit, mandarins, citrus, grapes, stone fruits), perennial crops, deciduous plants, sunflower, safflower, and sorghum.
In accordance with the embodiments of the present disclosure, the locus is a genetically modified crop or a conventional crop hybrid.
The insects affected by the present synergistic insecticidal composition(s) belongs to the group consisting of, but are not limited to, insects that damage or cause injury to the locus through feeding by biting, chewing, piercing and sucking, rasping and sucking, tunneling, grasping, grinding, cutting, sponging, chewing and lapping, siphoning, scrapping, making shelter, breeding, mating, migration and the like.
Further, other biologically active ingredients or compositions may be combined with the synergistic insecticidal composition(s) of the present disclosure in order to broaden the spectrum of activity. For example, the insecticidal compositions may contain other insecticides, fungicides, bactericides, acaracides, nematicides, insect growth regulators, plant glowth regulators, and the like.
All compositions of Indoxacarb and Fipronil showed synergistic insecticidal activity. Due to the higher bioefficacy, the amount of individual insecticides required to achieve the desired control on a locus is lesser. The use of lesser amount of insecticides is ecofriendly. Further, the use of lesser amount of insecticides leads to lower cost of treatment and hence is cost-effective and commercially attractive.
The present disclosure is further illustrated herein below with the help of the following experiments. The experiments used herein are intended merely to facilitate an understanding of ways in which the embodiments herein may be practiced and to further enable those of skill in the art to practice the embodiments disclosed herein.
These examples are not necessarily intended as representative of the overall testing performed and is not intended to limit the invention in any way. As one skilled in the art is aware, in insecticide testing, a significant number of factors that are not readily controllable can affect the results of individual tests and render them non-reproducible. For example, the results may vary depending on environmental factors, such as amount of sunlight and water, soil type, pH of the soil, temperature, and humidity among other factors. Apart from this, the type of application machinery, the application rate of individual and combined insecticides, the application rate of any antidote, and the ratio of the individual insecticides to one another and/or to an antidote, as well as the nature of crops or insect pests being tested, can affect the results. Results may also vary from crop to crop and within the crop varieties.
Accordingly, the examples should not be construed as limiting the scope of the embodiments described herein.
These laboratory scale experiments can be scaled up to industrial/commercial scale.
Examples
Experimental details:
Synergistic insecticidal compositions of the present disclosure were prepared by mixing Indoxacarb and Fipronil in appropriate amount of the active ingredients with suitable amounts of additives, followed by forming a homogeneous mixture. Each composition was further diluted with a suitable fluid medium to obtain the composition of desired concentrations.
The bioefficacy of each composition containing Indoxacarb and Fipronil was evaluated in controlled conditions. The results were recorded in terms of percent attribute of the bioefficacy ranging from 0% to 100%, with 0% representing no bioefficacy to the tested insect population and 100% representing complete destruction of the tested insect population.
The experimentally observed (O) results for the individual treatments were recorded along with the expected (E) results. The expected (E) results were calculated by using Limpels’ formula (provided in Limpel et al., 1962, "Weed Control by Dimethylchlorote nephthalate Alone and in Certain Combinations", Proc. NEWCC., Vol. 16:48-53) to determine the synergy among the active ingredients.
Limpel’s formula is E = X + Y - (XY / 100),
Where,
X = observed percent efficacy when Indoxacarb is used alone, and
Y = observed percent efficacy when Fipronil is used alone.
E= expected percent control
If the combination of Indoxacarb and Fipronil produces percent control higher than the expected percent control estimated by above given formula, then it is concluded that the synergism of insecticidal activity exists.

Example
A battery of experiments was carried out in a polyhouse under the scheme of randomized block design (RBD). The treatment units were treated with Indoxacarb alone, Fipronil alone and a combination of Indoxacarb and Fipronil in predetermined amounts as indicated in Tables 1-3.
The results of each treatment (calculated on the mean of three replications) along with the expected results from the Limpel’s formula are presented as percent control below in Tables 1-3. The obtained numbers are rounded off towards nearest two decimal points.

Experiment 1:
Treatments Dose
g *a.i. /ha . Percent Control of Podborer Helicoverpa
(as per Abbot’s formula)
Experimental value Estimated by Limpels’ formula
Indoxacarb 37.5 50.00 -
50 68.33 -
75 78.33 -
112.5 88.33 -
Fipronil 37.5 20.00 -
50 36.67 -
75 46.67 -
112.5 61.67 -
Indoxacarb + Fipronil 37.5 + 37.5 78.33 60.00
37.5 + 75 91.67 73.33
37.5 + 112.5 93.33 80.83
75 + 37.5 98.33 82.67
112.5 + 37.5 100.00 90.67
*a.i.-Active ingredients


Experiment 2:
Treatments Dose
g *a.i. /ha Percent Control of Jassids
(as per Abbot’s formula)
Experimental value Estimated by Limpels’ formula
Indoxacarb 37.5 1.18 -
50 2.35 -
75 5.88 -
112.5 7.06 -
Fipronil 37.5 54.12 -
50 67.06 -
75 68.24 -
112.5 81.18 -
Indoxacarb + Fipronil 37.5 + 37.5 70.59 54.66
37.5 + 75 92.94 68.61
37.5 + 112.5 98.82 81.40
75 + 37.5 78.82 56.82
112.5 + 37.5 80.00 57.36
*a.i.-Active ingredients

Experiment 3:
Treatments Dose
g *a.i. /ha Percent Control of Aphids
(as per Abbot’s formula)
Experimental value Estimated by Limpels’ formula
Indoxacarb 37.5 2.30 -
50 4.60 -
75 4.60 -
112.5 5.75 -
Fipronil 37.5 31.03 -
50 56.32 -
75 73.56 -
112.5 87.36 -
Indoxacarb + Fipronil 37.5 + 37.5 42.53 32.62
37.5 + 75 81.61 74.17
37.5 + 112.5 96.55 87.65
75 + 37.5 44.83 34.21
112.5 + 37.5 49.43 35.00
*a.i.-Active ingredients
The data in Tables 1-3 revealed that, Indoxacarb alone provided efficacy in the range from 50 to 88.33% against Helicoverpa in treatments at doses ranging from 37.5g a.i./ha to 112.5 g a.i./ha. However, Indoxacarb alone was found to be ineffective against Aphid (2.30-5.75%), and Jassids (1.18-7.06) at all the doses in the same range.
Fipronil alone was found highly effective against Jassid (54.12-81.18%), and Aphid (31.03-87.36%) in doses ranging from 37.5 g a.i/ha to 112.5 g a.i./ha and comparatively less effective (20.00-61.67%) against Helicoverpa in the doses ranging from 37.5 g a.i./ha to 112.5 g a.i./ha.
The treatments with composition(s) containing both Indoxacarb and Fipronil had shown better bioefficacy against Helicoverpa, Jassid and Aphid in comparison to the treatments with Indoxacarb alone and Fipronil alone compositions. This observed increase in bioefficacy was higher than the expected efficacy estimated by Limpel’s formula. Therefore, it is concluded that all compositions of Indoxacarb and Fipronil showed synergistic insecticidal activity. It is also observed that, the bioefficacy increases with increasing the amount of Indoxacarb and Fipronil in the combination formulation.
TECHNICAL ADVANCES AND ECONOMICAL SIGNIFICANCE
The composition of the present disclosure described herein above has technical advantage, including but not limited to the realization of a synergistic insecticidal composition that
-has better bioefficacy,
- is ecofriendly,
- is cost effective, and
- is commercially attractive.
The exemplary embodiment herein quantifies the benefits arising out of this disclosure and the various features and advantageous details thereof are explained with reference to the non-limiting embodiments in the description. Descriptions of well-known components and processing techniques are omitted so as to not unnecessarily obscure the embodiments herein. The examples used herein are intended merely to facilitate an understanding of ways in which the embodiments herein may be practiced and to further enable those of skill in the art to practice the embodiments herein. Accordingly, the examples should not be construed as limiting the scope of the embodiments herein.
The foregoing description of the specific embodiments fully reveal the general nature of the embodiments herein that others can, by applying current knowledge, readily modify and/or adapt for various applications such specific embodiments without departing from the generic concept, and, therefore, such adaptations and modifications should and are intended to be comprehended within the meaning and range of equivalents of the disclosed embodiments. It is to be understood that the phraseology or terminology employed herein is for the purpose of description and not of limitation. Therefore, while the embodiments herein have been described in terms of preferred embodiments, those skilled in the art will recognize that the embodiments herein can be practiced with modification within the spirit and scope of the embodiments as described herein.
Any discussion of documents, acts, materials, devices, articles and the like that has been included in this specification is solely for the purpose of providing a context for the disclosure. It is not to be taken as an admission that any or all of these matters form a part of the prior art base or were common general knowledge in the field relevant to the disclosure as it existed anywhere before the priority date of this application.
While considerable emphasis has been placed herein on the particular features of this disclosure, it will be appreciated that various modifications can be made, and that many changes can be made in the preferred embodiments without departing from the principles of the disclosure. These and other modifications in the nature of the disclosure or the preferred embodiments will be apparent to those skilled in the art from the disclosure herein, whereby it is to be distinctly understood that the foregoing descriptive matter is to be interpreted merely as illustrative of the disclosure and not as a limitation.

Documents

Application Documents

# Name Date
1 3202-MUM-2015-ORIGINAL UR 6(1A) FORM 26-270120.pdf 2020-01-29
1 Form 3 [21-08-2015(online)].pdf 2015-08-21
2 Description(Complete) [21-08-2015(online)].pdf 2015-08-21
2 3202-MUM-2015-ExtendedHearingNoticeLetter-(DateOfHearing-03-02-2020).pdf 2020-01-21
3 3202-MUM-2015-REQUEST FOR ADJOURNMENT OF HEARING UNDER RULE 129A [20-01-2020(online)].pdf 2020-01-20
3 3202-MUM-2015-Form 1-180915.pdf 2018-08-11
4 3202-MUM-2015-FORM-26 [18-01-2020(online)].pdf 2020-01-18
4 3202-MUM-2015-FER.pdf 2018-08-11
5 3202-MUM-2015-HearingNoticeLetter-(DateOfHearing-21-01-2020).pdf 2019-12-26
5 3202-MUM-2015-Correspondence-180915.pdf 2018-08-11
6 3202-MUM-2015-FORM-26 [04-09-2018(online)].pdf 2018-09-04
6 3202-MUM-2015-ABSTRACT [01-10-2018(online)].pdf 2018-10-01
7 3202-MUM-2015-OTHERS [01-10-2018(online)].pdf 2018-10-01
7 3202-MUM-2015-CLAIMS [01-10-2018(online)].pdf 2018-10-01
8 3202-MUM-2015-FER_SER_REPLY [01-10-2018(online)].pdf 2018-10-01
9 3202-MUM-2015-OTHERS [01-10-2018(online)].pdf 2018-10-01
9 3202-MUM-2015-CLAIMS [01-10-2018(online)].pdf 2018-10-01
10 3202-MUM-2015-ABSTRACT [01-10-2018(online)].pdf 2018-10-01
10 3202-MUM-2015-FORM-26 [04-09-2018(online)].pdf 2018-09-04
11 3202-MUM-2015-HearingNoticeLetter-(DateOfHearing-21-01-2020).pdf 2019-12-26
11 3202-MUM-2015-Correspondence-180915.pdf 2018-08-11
12 3202-MUM-2015-FORM-26 [18-01-2020(online)].pdf 2020-01-18
12 3202-MUM-2015-FER.pdf 2018-08-11
13 3202-MUM-2015-REQUEST FOR ADJOURNMENT OF HEARING UNDER RULE 129A [20-01-2020(online)].pdf 2020-01-20
13 3202-MUM-2015-Form 1-180915.pdf 2018-08-11
14 Description(Complete) [21-08-2015(online)].pdf 2015-08-21
14 3202-MUM-2015-ExtendedHearingNoticeLetter-(DateOfHearing-03-02-2020).pdf 2020-01-21
15 Form 3 [21-08-2015(online)].pdf 2015-08-21
15 3202-MUM-2015-ORIGINAL UR 6(1A) FORM 26-270120.pdf 2020-01-29

Search Strategy

1 SearchStrategy_11-07-2018.pdf