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Pesticidal Composition Containing Thiamethoxam, Chlorothalonil And Fluxapyroxad

Abstract: ABSTRACT PESTICIDAL COMPOSITION CONTAINING THIAMETHOXAM, CHLOROTHALONIL AND FLUXAPYROXAD The present invention relates to a synergistic composition comprising of combination of pesticides specifically insecticides and fungicides. Particularly the present invention relates to a synergistic pesticidal composition comprising of at least one insecticide specifically thiamethoxam and more than one fungicide specifically chlorothalonil and fluxapyroxad with one or more agrochemical additives in synergistically effective amounts whereby the combined effect of the active ingredients is improved to reduce the environmental load on a site where the said agrochemical is applied or the periphery thereof, more than ever, and its dose can be reduced effectively.

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Patent Information

Application #
Filing Date
18 October 2022
Publication Number
42/2023
Publication Type
INA
Invention Field
CHEMICAL
Status
Email
Parent Application

Applicants

COROMANDEL INTERNATIONAL LIMITED
Coromandel House, Sardar Patel Road, Secunderabad, Telangana, India 500003

Inventors

1. Aminul ISLAM
Coromandel House, Sardar Patel Road, Secunderabad, Telangana, India 500003
2. Nikumbhe SAGAR
Coromandel House, Sardar Patel Road, Secunderabad, Telangana, India 500003
3. Raghavendra GANGASANI
Coromandel House, Sardar Patel Road, Secunderabad, Telangana, India 500003
4. Rajul EDOLIYA
Coromandel House, Sardar Patel Road, Secunderabad, Telangana, India 500003
5. Rajan Kumar TRIVEDI
Coromandel House, Sardar Patel Road, Secunderabad, Telangana, India 500003
6. Ramakant PATIL
Coromandel House, Sardar Patel Road, Secunderabad, Telangana, India 500003

Specification

DESC:FORM 2

THE PATENTS ACT 1970
(SECTION 39 OF 1970)

&

THE PATENT RULES, 2003

COMPLETE SPECIFICATION
(Section 10 and Rule 13)

PESTICIDAL COMPOSITION CONTAINING THIAMETHOXAM, CHLOROTHALONIL AND FLUXAPYROXAD

We, COROMANDEL INTERNATIONAL LIMITED,
an Indian company incorporated under the Companies Act, 1956, and validly existing under the Companies Act, 2013. Having its registered office at Coromandel House, Sardar Patel Road,
Secunderabad – 500 003, Telangana, India

The following specification particularly describes the invention, and the manner in which it is to be performed.
FIELD OF THE INVENTION
The present invention relates to a novel synergistic composition comprising of pesticides, particularly insecticides and fungicides. More particularly the present invention relates to a synergistic composition comprising of at least one insecticide specifically thiamethoxam and at least two fungicides specifically chlorothalonil and fluxapyroxad with suitable agrochemical additives in synergistically effective amounts.

The present invention also relates to an agrochemical combination for protecting plants against diseases and insects using the synergistic pesticidal composition comprising of thiamethoxam, chlorothalonil and fluxapyroxad.

BACKGROUND OF THE INVENTION
Pesticides are chemical compounds that are used to kill pests, including insects, rodents, fungi, and unwanted plants (weeds). Pesticides are mainly used for benefits like crops protection, preservation of food materials and prevention of vector borne diseases. They are also used in different fields like agriculture, forestry, aquaculture, food industry, processing, transportation, and storage of wood and other biological products. They are classified based on various criteria. Most used criteria for classification of pesticides are its mode of entry, its chemical composition and target it kill.

Insecticides are agrochemicals in the pesticide family used to control insects by killing them or preventing the establishment or proliferation of those considered harmful. They play a key role in agriculture and public health by improving the yield and productivity of crops caused by pests and by reducing the rate of vector-borne diseases by killing or affecting growth and development of vectors such as mosquitoes, houseflies, tsetse flies, sand flies, cockroaches, etc.

They are formulated for repelling, killing, harming, or mitigating insects from crops and other agri-food sources such as ranches, poultry farms, etc. Insecticides work differently based on their mode of actions; some disrupt the nervous system, whereas others damage the exoskeletons, others repel or control them. Insecticides application helps in managing and mitigating insects; thereby guaranteeing crop protection and preventing yield loss.

Fungicides are biocidal chemical compounds or biological organisms used to kill parasitic fungi or their spores. Fungi can cause serious damage in agriculture, resulting in critical losses of yield, quality, and profit. Fungicides are used both in agriculture and to fight fungal infections in animals. These are also a category of pesticides used in the protection of plants against diseases.

Although pesticides remain indispensable in agriculture, a great potential still exists to improve their efficiency and thus reduce their input into the environmental and food chain.

In many economically important crops and cash crops such as rice, peppers, grapes and other agricultural crops, fungal infection and insect infestation may occur simultaneously. To control this farmer usually applies compositions comprising either single active or combinations of actives. Control of plant diseases and pests is an inevitable work in efficiently performing the agricultural production, and to achieve this purpose, synthetic pesticides have been used, resulting in making a remarkable achievement.

The mixing of insecticides with fungicides results in incompatibility of physical nature and may alter efficacy of the active ingredients. Hence, it requires due trial and experimentation to assess the compatibility of fungicides with insecticides and their influence on crops. Many pesticides with combination of one or more actives have been used by farmers. But still there is requirement for new combinations which can provide efficacy, low-cost benefit ratio, broad spectrum protection and decreased environmental load.

With increased use of chemical compounds as insecticides, herbicides, fungicides it has been observed that crops are becoming tolerant and resistant to use of composition comprising single active. Hence, there is a need for combination of actives belonging to different classes and groups to allow for broader disease control spectrum that combines curative and preventive actives and has a lower dosage. There is a need in the art for new combinations of systemic insecticide compounds like thiamethoxam with different fungicides that help improve spectrum.

Thiamethoxam is a systemic insecticide of the neonicotinoid class, developed by Syngenta and is a broad-spectrum, systemic insecticide, which means it is absorbed quickly by plants and transported to all its parts, including pollen, where it acts to deter insect feeding. An insect can absorb it in its stomach after feeding, or through direct contact, including through its tracheal system. The compound gets in the way of information transfer between nerve cells by interfering with nicotinic acetylcholine receptors in the central nervous system, and eventually paralyzes the muscles of the insects.

Thiamethoxam is chemically known as {3-[(2-Chloro-1,3-thiazol-5-yl)methyl]-5-methyl-1,3,5-oxadiazinan-4-ylidene}nitramide.It has the following chemical structure:

Chlorothalonil is a broad-spectrum organochlorine fungicide used to control fungi that infect vegetables, trees, small fruits, turf, ornamentals, and other agricultural crops. It also controls fruit rots in cranberry bogs. It reduces fungal intracellular glutathione molecules to alternate forms which cannot participate in essential enzymatic reactions, ultimately leading to cell death. It has very low toxicity to mammals, broad activity against decay fungi and insects, relatively low cost, and good stability and leach resistance in wood.

Chlorothalonil is chemically known as 2,4,5,6-Tetrachlorobenzene-1,3-dicarbonitrile and has the following chemical structure:

Fluxapyroxad is a broad-spectrum pyrazole-carboxamide fungicide used on a large variety of commercial crops. It stunts fungus growth by inhibiting the succinate dehydrogenase (SQR) enzyme. Fluxapyroxad is a succinate dehydrogenase inhibitor (SDHI). It interferes with several key fungal life functions, including spore germination, germ tube growth, appressoria formation and mycelium growth. It is commonly used as a fungicide for grains, row crops, vegetable crops, and fruit trees (pome and prunus).

Fluxapyroxad chemically known as 3-(Difluoromethyl)-1-methyl-N-(3',4',5'-trifluoro[1,1'-biphenyl]-2-yl)-1H-pyrazole-4-carboxamide. It has the following chemical structure:

Synergistic effects allow the application rates of the individual active substances to be reduced, a more potent action against the same species of harmful plant combined with the same application rate, the control of species to which the action has hitherto not extended (zero effect), an extended application period and/or a reduced number of required individual applications and as a result for the user economical and ecologically more advantageous control systems against pests.

OBJECT OF THE INVENTION
One object of the present invention is to provide a synergistic pesticidal composition comprising of one insecticide and two or more fungicides.

Another object of the present invention provides a synergistic pesticidal composition comprising of thiamethoxam insecticide in combination with two fungicides consisting of chlorothalonil and fluxapyroxad.

Another object of the present invention is to provide a synergistic pesticidal composition comprising of thiamethoxam, chlorothalonil and fluxapyroxad with suitable agrochemical additives in synergistically effective amounts.

Yet another object of the present invention is to provide a wettable powder composition comprising of thiamethoxam, chlorothalonil and fluxapyroxad with suitable agrochemical additives in synergistically effective amounts, and process for the preparation thereof.

Yet another object of the present invention is to provide improved combinations of insecticides for the control of Collar rot disease which is an important seed and soil borne disease of groundnut, and white grub diseases in groundnut crop.

In yet another object of the present invention is to provide improved combinations of insecticides that promote plant health.

SUMMARY OF THE INVENTION
The present invention provides a synergistic pesticidal composition comprising of thiamethoxam insecticide in combination with two fungicides consisting of chlorothalonil and fluxapyroxad.

In one aspect of the present invention provides a pesticidal composition comprising of (a) thiamethoxam, (b) chlorothalonil, and (c) fluxapyroxad with suitable agrochemical additives in synergistically effective amounts.

In another aspect of the present invention provides, a wettable powder composition comprising of:
a) thiamethoxam in a range from 40% (w/w) to 60% (w/w),
b) chlorothalonil in a range from 15% (w/w) to 35% (w/w),
c) fluxapyroxad in a range from 1% (w/w) to 7% (w/w), and
d) agrochemical additives.

In an aspect of the present invention, the suitable agrochemical additives are selected from a wetting agent, a dispersing agent, a defoamer, an anti-caking agent, a chelating agent, and a filler.

In an aspect of the present invention, the wetting agent is selected from the group comprising an alkyl naphthalene sulfonate, dialkyl naphthalene sulphonate sodium salt, Propol 990N, Jeemol IP, and sodium salt of dibutyl naphthalene sulphonate, present in a range from 1% to 5% (w/w).

In an aspect of the present invention, the dispersing agent is selected from the group comprising of sodium polycarboxylate, blend of dispersing agent (Jeemol DW18), alkyl naphthalene sulfonate condensate, and sodium lignosulfonate, and combination thereof, present in a range from 1% to 10% (w/w).

In an aspect of the present invention, the defoamer is polydimethylsiloxane, present in a range from 0.1% to 1.5% (w/w).

In an aspect of the present invention, the anti-caking agent is silicon dioxide, present in an amount of 1% to 2% (w/w).

In an aspect of the present invention, the chelating agent is citric acid, present in an amount of 0.1% to 0.5% (w/w).

In an aspect of the present invention, the filler is aluminum silicate, present in Q.S.

In another aspect of the present invention provides a synergistic pesticidal composition comprising of insecticide and fungicide mixtures that are mutually complement each other when used together and exhibit activity that is greater than the activities of individual components when used alone.

In yet another aspect of the present invention provides a process for the preparation of a wettable powder composition comprising of thiamethoxam, chlorothalonil, and fluxapyroxad, wherein the process comprises the following steps:
a) weighing the filler, an anticaking agent, a chelating agent, a wetting agent, a dispersing agent, thiamethoxam technical, chlorothalonil technical, fluxapyroxad technical and a defoamer in a pre-blender and mixing it for 1 hour,
b) milling the sample through air jet mill instrument at inlet pressure 2-3 kg/cm2, grinding pressure 6 kg/ cm2 and checking for the particle size < 15 micron,
c) collecting the milled material, and post blending the sample for 1 hour,
d) sending the sample to the quality analysis, and
e) packing the formulated material in a suitable package.

DESCRIPTION OF THE INVENTION
The following detailed description is presented to enable any person skilled in the art to make and use the invention. For purposes of explanation, specific nomenclature is set forth to provide a thorough understanding of the present application. However, it will be apparent to one skilled in the art that these specific details are not required to practice the invention. Descriptions of specific applications are provided only as representative examples. The present application is not intended to be limited to the embodiments shown but is to be accorded the widest possible scope consistent with the principles and features disclosed herein.

Similarly, the words "comprise," "comprises," and "comprising" are to be interpreted inclusively rather than exclusively. Likewise, the terms "include," "including" and "or" should all be construed to be inclusive, unless such a construction is clearly prohibited from the context. However, the embodiments provided by the present disclosure may lack any element that is not specifically disclosed herein. Thus, a disclosure of an embodiment defined using the term "comprising" is also a disclosure of embodiments "consisting essentially of” and "consisting of” the disclosed components. Where used herein, the term "example," particularly when followed by a listing of terms, is merely exemplary and illustrative, and should not be deemed to be exclusive or comprehensive. Any embodiment disclosed herein can be combined with any other embodiment disclosed herein unless explicitly indicated otherwise.

It is to be noted that, as used in the specification, the singular forms "a", "an" and "the" include plural referents unless the context clearly dictates otherwise. Thus, for example, reference to a composition containing “a compound” includes a mixture of two or more compounds. It should also be noted that the term “or” is generally employed in its sense including “and/or” unless the content clearly dictates otherwise.

As used herein, the terms "crops" and "vegetation" can include, for instance, dormant seeds, germinant seeds, emerging seedlings, plants emerging from vegetative propagules, immature vegetation, and established vegetation.

As used herein, immature vegetation may be understood to include small vegetative plants prior to reproductive stage, and mature vegetation may be understood to include vegetative plants during and after the reproductive stage.

As used herein, the term “pesticide” may be understood as the natural or synthetic agents designed to kill all types of pests.

As used herein, the terms “insecticide” may be understood to include pesticides specifically used to destroy one or more species of insects.

As used herein, the terms “fungicide” may be understood as a pesticide specifically biocidal chemical compounds or biological organisms used to kill parasitic fungi or their spores.

As used herein, the term “synergistic composition” may be understood to include effective combination of more than one agrochemical that allows the application of the said agrochemical in a much lower dosage, which results in a less dosage treatment for the crops.

As used herein, the term “agrochemical additives” may be understood to include a range of surfactants, dispersing agents, organic or inorganic pigments, solvents, de-solvents, defoamers, and emulsions, crystallization inhibitors, viscosity modifiers, suspending agents, dyes, antioxidants, foaming agents, light absorbers, mixing aids, neutralizers or pH adjusting substances and buffers, corrosion inhibitors, fragrances, wetting agents, absorption enhancers, micronutrients, plasticizers, lubricants, thickeners, anti-freezing agents, sterilization agents among others.

As used herein, the synergistic composition of the present invention may be formulated as Capsule suspension (CS), Dispersible concentrate (DC), Dustable powder (DP), Powder for dry seed treatment (DS), Emulsifiable concentrate (EC), Emulsifiable granule (EG), Emulsion water in-oil (EO), Emulsifiable powder (EP), Emulsion for seed treatment (ES), Emulsion oil-in-water (EW), Flowable concentrate for seed treatment (FS), Granules (GR), Micro-emulsion (ME), Oil-dispersion (OD), Oil miscible flowable concentrate (OF), Oil miscible liquid (OL), Oil dispersible powder (OP), Suspension concentrate (SC), Suspension concentrate for direct application (SD), Suspo-emulsion (SE), Water soluble granule (SG), Soluble concentrate (SL), Spreading oil (SO), Water soluble powder (SP), Water soluble tablet (ST), Ultra-low volume (ULV) Tablet (TB), Water dispersible granules (WG or WDG), Wettable powder (WP), Water dispersible powder for slurry seed treatment (WS), Water dispersible tablet (WT), a mixed formulation of CS and SC (ZC), a mixed formulation of CS and SE (ZE), a mixed formulation of CS and EW (ZW) among others. Preferably, the composition of the present invention is formulated as wettable powder (WP).

In another embodiment of the present invention provides a synergistic pesticidal composition comprising of thiamethoxam insecticide in combination with two fungicides consisting of chlorothalonil and fluxapyroxad.

In another embodiment of the present invention provides a pesticidal composition comprising of (a) thiamethoxam, (b) chlorothalonil, and (c) fluxapyroxad with suitable agrochemical additives in synergistically effective amounts.

In another embodiment of the present invention provides a wettable powder composition comprising of:
a) thiamethoxam in a range from 40% (w/w) to 60% (w/w),
b) chlorothalonil in a range from 15% (w/w) to 35% (w/w),
c) fluxapyroxad in a range from 1% (w/w) to 7% (w/w), and
d) agrochemical additives.

According to the present invention, the suitable agrochemical additives are selected from a wetting agent, a dispersing agent, a defoamer, an anti-caking agent, a chelating agent, and a filler.

According to the present invention, the wetting agent is selected from an alkyl naphthalene sulfonate, dialkyl naphthalene sulphonate sodium salt, Propol 990N, Jeemol IP, and sodium salt of dibutyl naphthalene sulphonate, present in a range from 1% to 5% (w/w).

According to the present invention, the dispersing agent is selected from sodium polycarboxylate, blend of dispersing agent (Jeemol DW18), alkyl naphthalene sulfonate condensate, and sodium lignosulfonate, and combination thereof, present in a range from 1% to 10% (w/w).

According to the present invention, the defoamer is polydimethylsiloxane, present in a range from 0.1% to 1.5% (w/w).

According to the present invention, the anti-caking agent is silicon dioxide, present in an amount of 1% to 2% (w/w).

According to the present invention, the chelating agent is citric acid, present in an amount of 0.1% to 0.5% (w/w).

According to the present invention, the filler is aluminum silicate, present in Q.S.

In another embodiment of the present invention provides a process for the preparation of a wettable powder composition comprising of thiamethoxam, chlorothalonil, and fluxapyroxad, wherein the process comprises the following steps:
a) weighing the filler, an anticaking agent, a chelating agent, a wetting agent, a dispersing agent, thiamethoxam technical, chlorothalonil technical, fluxapyroxad technical and a defoamer in a pre-blender and mixing it for 1 hour,
b) milling the sample through air jet mill instrument at inlet pressure 2-3 kg/cm2, grinding pressure 6 kg/ cm2 and checking for the particle size < 15 micron,
c) collecting the milled material, and post blending the sample for 1 hour,
d) sending the sample to the quality analysis, and
e) packing the formulated material in a suitable package.

The present invention can be effectively used for the protection of crop plants such as rice, wheat, vegetables, fruit trees, peanuts, tea leaves, rubber trees, forests and golf course grasses, cabbages, citrus, cocoa, coffee, cotton, cucurbits, vegetables, lettuces, ornamentals, peppers, pome fruits, popcorn, potatoes, stone fruits, tobacco, tomatoes, vines, brassicas, cereals, legumes, maize, oilseed rape, sorghum, sugar beet, sunflowers, soya beans, tobacco, row and vegetable crops such as shelled peas and beans, edible-pod legume vegetables, oil seed crops such as flax seeds, rapeseed, safflower, soya beans, fruit trees such as pome and prunus, apples, crab apples, oriental pears, pears, apricots, cherries, nectarines, peaches ,plums (all varieties) barley, corn(all types),oats, rye, triticale, almonds and pecan.

In addition, by treating the crop plants with the synergistic pesticidal composition of the present invention, it becomes possible to simultaneously control insects and fungi inhabiting the soil and the ground. Also, since the dosage and the number of times of application of the active ingredient are reduced and the long-lasting effect persists, it is possible to provide a comprehensive control method.

The present invention is further illustrated by the following examples which are provided merely to be exemplary of the inventions and is not intended to limit the scope of the invention. Certain modifications and equivalents will be apparent to those skilled in the art and are intended to be included within the scope of the present invention.

EXAMPLES:

Example-1: The illustrative embodiments show the composition of thiamethoxam + chlorothalonil + fluxapyroxad in wettable powder form in different amount as follows:

Table-1:
S. No Compositions Function Charge in (%)
1. Thiamethoxam Active ingredient 50.0
2. Chlorothalonil Active ingredient 30.0
3. Fluxapyroxad Active ingredient 5.0
4. Sodium polycarboxylate Dispersing agent 2.0
5. Blend of dispersing agent (Jeemol DW18) Dispersing agent 2.0
6. Alkyl naphthalene sulfonate Wetting agent 3.0
7. Polydimethylsiloxane Defoamer 1.0
8. Citric Acid chelating agent 0.5
9. Silicon dioxide Anti caking agent 2.0
10. Aluminium silicate (China clay) Filler Q. S

Process for manufacture of composition is as follows: 50.0 gm of thiamethoxam, 30.0 gm of chlorothalonil, 5.0 gm of fluxapyroxad, 2.0 gm of Sodium polycarboxylate, 2.0 gm of blend of dispersing agent (Jeemol DW18), 3.0 gm of alkyl naphthalene sulfonate, 1.0 gm of polydimethylsiloxane, 0.5 gm of citric acid, 2.0 gm of silicon dioxide, and required quantity of aluminum silicate (china clay) were weighed in the pre-blender reactor and mixed for 1 hour. The mixture was milled through air jet mill instrument (Inlet pressure 2-3 kg/cm2, grinding pressure 6 kg/ cm2) to obtain the desired particle size (D90 < 15 microns). Collecting the milled material and post blending the material for 1 hour followed by packing the material in a suitable package.

Table-2:
S. No Compositions Function Charge in (%)
1. Thiamethoxam Active ingredient 40.0
2. Chlorothalonil Active ingredient 20.0
3. Fluxapyroxad Active ingredient 3.0
4. Alkyl naphthalene sulfonate (ANS) condensate Dispersing agent 5.0
5. Alkyl naphthalene Sulfonate Wetting agent 2.5
6. Polydimethylsiloxane Defoamer 0.2
7. Citric Acid chelating agent 0.1
8. Silicon dioxide Anti caking agent 1.0
9. Aluminium silicate (China clay) Filler Q.S.

Process for manufacture of composition is as follows: 40.0 gm of thiamethoxam, 20.0 gm of chlorothalonil, 3.0 gm of fluxapyroxad, 5.0 gm of alkyl naphthalene sulfonate condensate, 2.5 gm of alkyl naphthalene sulfonate, 0.2 gm of polydimethylsiloxane, 0.1 gm of citric acid, 1.0 gm of silicon dioxide, and required quantity of aluminum silicate (china clay) were weighed in the pre-blender reactor and mixed for 1 hour. The mixture was milled through air jet mill instrument (Inlet pressure 2-3 kg/cm2, grinding pressure 6 kg/ cm2) to obtain the desired particle size (D90 < 15 microns). Collecting the milled material and post blending the material for 1 hour followed by packing the material in a suitable package.

Table-3
S. No Compositions Function Charge in (%)
1. Thiamethoxam Active ingredient 55.0
2. Chlorothalonil Active ingredient 25.0
3. Fluxapyroxad Active ingredient 7.0
4. Sodium lignosulfonate Dispersing agent 4.0
5. Propol 990 N Wetting agent 2.0
6. Polydimethylsiloxane Defoamer 0.1
7. Citric Acid chelating agent 0.2
8. Silicon dioxide Anti caking agent 1.0
9. Aluminium silicate (China clay) Filler Q.S.

Process for manufacture of composition is as follows: 55.0 gm of thiamethoxam, 25.0 gm of chlorothalonil, 7.0 gm of fluxapyroxad, 4.0 gm of sodium lignosulfonate, 2.0 gm of Propol 990N, 0.1 gm of polydimethylsiloxane, 0.2 gm of citric acid, 1 gm of silicon dioxide, 0.2 gm of citric acid, and required quantity of aluminum silicate (china clay) were weighed in the pre-blender reactor and mixed for 1 hour. The mixture was milled through air jet mill instrument (Inlet pressure 2-3 kg/cm2, grinding pressure 6 kg/ cm2) to obtain the desired particle size (D90 < 15 microns). Collecting the milled material and post blending the material for 1 hour followed by packing the material in a suitable package.

Tabel-4
S. No Compositions Function Charge in (%)
1. Thiamethoxam Active ingredient 45.0
2. Chlorothalonil Active ingredient 20.0
3. Fluxapyroxad Active ingredient 4.0
4. Jeemol IP Wetting agent 3.0
5. Sodium polycarboxylate Dispersing agent 6.0
6. Polydimethylsiloxane Defoamer 1.2
7. Silicon dioxide Anti caking agent 2.0
8. Citric Acid chelating agent 0.5
9. Aluminium silicate (China clay) Filler Q.S.

Process for manufacture of composition is as follows: 45.0 gm of thiamethoxam, 20.0 gm of chlorothalonil, 4.0 gm of fluxapyroxad, 3.0 gm of Jeemol IP, 6.0 gm of Sodium polycarboxylate, 1.2 gm of polydimethylsiloxane, 0.5 gm of citric acid, 2.0 gm of silicon dioxide, and required quantity of aluminum silicate (china clay) were weighed in the pre-blender reactor and mixed for 1 hour. The mixture was milled through air jet mill instrument (Inlet pressure 2-3 kg/cm2, grinding pressure 6 kg/ cm2) to obtain the desired particle size (D90 < 15 microns). Collecting the milled material and post blending the material for 1 hour followed by packing the material in a suitable package.

Table-5
S. No Compositions Function Charge in (%)
1. Thiamethoxam Active ingredient 60.0
2. Chlorothalonil Active ingredient 35.0
3. Fluxapyroxad Active ingredient 1.0
4. Alkyl naphthalene sulfonate Wetting agent 1.0
5. Alkyl naphthalene sulfonate (ANS) condensate Dispersing agent 1.0
6. Polydimethylsiloxane Defoamer 0.1
7. Silicon dioxide Anti caking agent 1.0
8. Citric Acid chelating agent 0.1
9. Aluminium silicate (China clay) Filler Q.S.

Process for manufacture of composition is as follows: 60.0 gm of thiamethoxam, 35.0 gm of chlorothalonil, 1.0 gm of fluxapyroxad, 1.0 gm of alkyl naphthalene sulfonate, 1.0 gm of alkyl naphthalene sulfonate condensate, 0.1 gm of polydimethylsiloxane, 1.0 gm of silicon dioxide, 0.1 gm of citric acid, and required quantity of aluminum silicate (china clay) were weighed in the pre-blender reactor and mixed for 1 hour. The mixture was milled through air jet mill instrument (Inlet pressure 2-3 kg/cm2, grinding pressure 6 kg/ cm2) to obtain the desired particle size (D90 < 15 microns). Collecting the milled material and post blending the material for 1 hour followed by packing the material in a suitable package.

Example 2: Efficacy study of thiamethoxam 50% + chlorothalonil 30% + fluxapyroxad 5% in wettable powder form:

SYNERGY STUDIES:

After calculating % disease control, the synergism was calculated by below formula:

The synergistic pesticidal action of the inventive mixtures calculated by Colby’s formula as follows:

Appropriate analysis of plant response to Fungicide combination is critical in determining the type of activity observed. The most widely used model is the one Gowing* derived and Colby** modified. Gowing described a mathematical formula for calculating the predicting response values for pesticide mixtures. He suggested the expected (E) percent inhibition of growth induced by pesticide A plus pesticide B and plus pesticide C is as follows, *(Jerry Flint et al, 1988) ***

(AB+AC+BC) ABC
Expected (E) = A + B + C - +
100 10000

Where,
A = observed efficacy of active ingredient A at the same concentration as used in the mixture.
B = observed efficacy of active ingredient B at the same concentration as used in the mixture.
C = observed efficacy of active ingredient C at the same concentration as used in the mixture.

When the percentage of pesticidal control observed for the combination is greater than the expected percentage, there is a synergistic effect. (Ratio of O/E > 1, means synergism observed.)

Reference:
*Gowing, D. P. 1960. Comments on tests of Fungicide mixtures. Weeds 8:379–391.
**Colby, S. R. 1967. Calculating synergistic and antagonistic responses of Fungicide combinations. Weeds 15:20–22
*** Jerry Flint et al, 1988. Analyzing Fungicide Interactions: A Statistical Treatment of Colby's Method. Weed Technology 2: 304-309

FIELD AND SYNERGY STUDIES:
There is always a co-occurrence of insects and diseases in rice crops. Hence farmers usually do tank-mix insecticide and fungicide. The improper tank mixing sequence of chemicals may lead to incompatibility which adversely affects crop safety and pest control.

Trial 1: Bio-efficacy against groundnut collar rot:
This disease was first reported from Java in 1926. In India, the disease is prevalent in all groundnut tracts and is usually most severe in light sandy soils. Aspergillus niger Van Tieghem is the causal agent of crown/collar rot. Mycelium is hyaline to sub-hyaline. The conidiophores arise directly from the substrate and are septate, smooth, and thick-walled and hyaline to olive brown in colour. The vesicles are mostly globose and have two rows of hyaline phialides viz., primary, and secondary phialides. The conidial heads are dark brown to black. The conidia are produced in long chains and are globose, spinulose and dark brown on maturity.

The pathogen is carried on the seed surface and in or under the tissues of the testa. The primary sources of inoculum are a) mycelium and spores carried on the seeds. b) plant debris in the soil and c) infected cotyledons or embryos. Seeds become infected during the last days of maturation in the soil and during harvesting, handling and particularly during shelling.

The disease perpetuates through contaminated soil also. Soil infection spreads to cotyledons or directly to hypocotyl. The seedlings become more susceptible when they are injured. The fungus can tolerate low moisture levels and develops well at temperatures between 30° and 35°C. It builds up in soils continuously cropped with groundnuts.

In moist soil, seeds may be attacked immediately after sowing leading to pre-emergence rotting. If the ungerminated seeds are removed from the soil, they are found covered with masses of black conidia which give the seed a sooty appearance. Post-emergence infection often culminates in death and rapid decay of seedlings. The first symptom in emerging seedlings is usually rapid drying of the entire plant. Affected tissues are covered by sporulating fungus at the soil surface.

The field trial was conducted to evaluate the efficacy of innovative mixtures of Thiamethoxam, Chlorothalonil, and Fluxapyroxad against Aspergills niger fungus in Groundnut crop. The trial was conducted with randomized block design with net plot size of 5m x 6m. Tomato crops were raised with all standard agronomic practices. Seed treatment was done with slurry method by preparing 10 ml slurry volume of chemical at the time of sowing. The visual observations were recorded for % disease control from fifty plants per plot. The observations were recorded at 7 DAA (Days after application), 14 DAA and 28 DAA.

Table 6: collar rot disease control in groundnut:
Compositions Dose
(g AI/100 kg seed) Percent disease control – collar rot.
14 DAS 28 DAS
Thiamethoxam 50% + Chlorothalonil 30% +
Fluxapyroxad 5% WP 340 90 85
Fluxapyroxad 33.3% FS 20 65 50
Chlorothalonil 75% WP 120 75 65
Thiamethoxam 30% FS 200 0 0
WP – Wettable Powder; FS – flowable suspension; and DAA - Days after application.

The trial results show excellent efficacy of thiamethoxam 50% + chlorothalonil 30% + fluxapyroxad 5% WP combinations against collar rot disease of groundnut. The solo application of three active ingredients tested here, were also not able to provide satisfactory control of collar rot disease. The combination of thiamethoxam 50% + chlorothalonil 30% + fluxapyroxad 5% WP found very promising against groundnut collar rot in terms of efficacy as well as residual control.

Table 7: Percent Groundnut Collar rot disease control at 28 DAA
Compositions Dose
(g or ml/ha) % Collar rot disease control
Expected Actual
Thiamethoxam 50% + Chlorothalonil 30% + Fluxapyroxad 5% WP 340 76 85
Fluxapyroxad 33.3% FS 20 60
Chlorothalonil 75% WP 120 40
Thiamethoxam 30% FS 200 00
Ratio of O/E 1.20
WP – Wettable Powder; FS – flowable suspension; and DAA - Days after application.

The results in table 7 clearly demonstrate synergy between thiamethoxam 50% + chlorothalonil 30% + fluxapyroxad 5% WP in controlling groundnut Collar rot disease. The large difference between the observed and the expected efficacy clearly demonstrates the synergistic effect of the combination.

Trial 2: Bio-efficacy against groundnut white grub:
The important species of white grubs which infest groundnut belong to three sub-families: Melolonthinae, Rutelinae and Dynastinae. The genus Holotrichia includes the major species of white grubs inflicting serious damage to groundnut cultivation in rainy season. H. consanguinea is pre-dominant in Rajasthan, Gujarat, Haryana, Punjab, Bihar, and Uttar Pradesh whereas, H. serrata is most destructive in states like, Karnataka, Andhra Pradesh, Tamil Nadu, and Maharashtra and later it has spread to western and peninsular India. The species of white grub that are endemic to Saurashtra region of Gujarat are Apogonia rauca, Schizonycha ruficollis and Adoretus sp.

Apart from groundnuts, they are known to attack roots of guava, sugarcane, coconut, areca nut, tobacco, potato and many other oilseeds, pulses, and vegetable crops.

White grubs are present throughout the year; however, their activity can be seen only during the rainy season (May/June-December). Adults emerge in large numbers for mating after the first monsoon rains in mid-May or June months and again they return to soil for the rest of their life cycle. White grubs prefer light clay soils rich in organic matter; aeration; moisture and soil temperature around 25ºC. They have a single generation in a year where grub (larvae) is the damaging stage and adults are free living.

The field trial was conducted to evaluate the efficacy of innovative mixtures of thiamethoxam, chlorothalonil and fluxapyroxad against white grub insect in Groundnut crop. The trial was conducted with randomized block design with net plot size of 5m x 6m. Tomato crops were raised with all standard agronomic practices. Seed treatment was done with slurry method by preparing 10 ml slurry volume of chemical at the time of sowing. The visual observations were recorded for % disease control from fifty plants per plot. The observations were recorded at 7 DAA (Days after application), 14 DAA and 28 DAA.

Table 8: white grub insect control in groundnut:
Compositions Dose
(g AI/100 kg seed) Percent disease control – collar rot.
14 DAS 28 DAS
Thiamethoxam 50% + Chlorothalonil 30% + Fluxapyroxad 5% WP 340 90 80
Fluxapyroxad 33.3% FS 20 00 00
Chlorothalonil 75% WP 120 00 00
Thiamethoxam 30% FS 200 75 65
WP – Wettable Powder; FS – flowable suspension; and DAA - Days after application.

The trial results show excellent efficacy of thiamethoxam 50% + chlorothalonil 30% + fluxapyroxad 5% WP combinations against white grub insect of groundnut. The solo application of three active ingredients tested here, were also not able to provide satisfactory control of collar rot disease. The combination of thiamethoxam 50% + chlorothalonil 30% + fluxapyroxad 5% WP found very promising against groundnut white grub insect in terms of efficacy as well as residual control.

Table 9: Percent groundnut white grub insect control at 28 DAA
Compositions Dose
(g or ml/ha) % Collar rot disease control
Expected Actual
Thiamethoxam 50% + Chlorothalonil 30% + Fluxapyroxad 5% WP 340 65 80
Fluxapyroxad 33.3% FS 20 00
Chlorothalonil 75% WP 120 00
Thiamethoxam 30% FS 200 65
Ratio of O/E 1.23
WP – Wettable Powder; FS – flowable suspension; and DAA - Days after application.

The results in table 9 clearly demonstrate synergy between thiamethoxam 50% + chlorothalonil 30% + fluxapyroxad 5% WP in controlling Groundnut Collar rot disease. The large difference between the observed and the expected efficacy clearly demonstrates the synergistic effect of the combination.

The combination of thiamethoxam 50% + chlorothalonil 30% + fluxapyroxad 5% WP provided excellent control of collar rot disease and white grub insect control in groundnut, as the same combination is also able control disease like, sclerotium rot, fusarium wilt and Termite and wire worm pests.

The combinations had shown synergistic effect on insect and disease control in groundnut, soybean, Potato, Cumin. ,CLAIMS:WE CLAIM:

1. A synergistic pesticidal composition comprising of (a) thiamethoxam, (b) chlorothalonil, and (c) fluxapyroxad with suitable agrochemical additives.

2. The composition as claimed in claim 1, wherein the composition is formulated as wettable powder (WP) form.

3. The composition as claimed in claim 2, wherein the composition comprising of:
a) thiamethoxam in a range from 40% (w/w) to 60% (w/w),
b) chlorothalonil in a range from 15% (w/w) to 35% (w/w),
c) fluxapyroxad in a range from 1% (w/w) to 7% (w/w), and
d) suitable agrochemical additives.

4. The composition as claimed in claim 3, wherein the agrochemical additives are selected from a wetting agent, a dispersing agent, a defoamer, an anti-caking agent, a chelating agent, and a filler.

5. The composition as claimed in claim 4, wherein the wetting agent is selected from an alkyl naphthalene sulfonate, dialkyl naphthalene sulphonate sodium salt, Propol 990N, Jeemol IP, and sodium salt of dibutyl naphthalene sulphonate, present in a range from 1% to 5% (w/w).

6. The composition as claimed in claim 4, wherein the dispersing agent is selected from sodium polycarboxylate, blend of dispersing agent (Jeemol DW18), alkyl naphthalene sulfonate condensate, and sodium lignosulfonate, and combination thereof, present in a range from 1% to 10% (w/w).

7. The composition as claimed in claim 4, wherein the defoamer is polydimethylsiloxane, present in a range from 0.1% to 1.5% (w/w).

8. The composition as claimed in claim 4, wherein the anti-caking agent is silicon dioxide, present in an amount of 1% to 2% (w/w).

9. The composition as claimed in claim 4, wherein the chelating agent is citric acid, present in an amount of 0.1% to 0.5% (w/w).

10. The process for preparation of a wettable powder composition as claimed in claim 2, wherein the process comprising the steps of:
a) weighing the filler, an anticaking agent, a chelating agent, a wetting agent, dispersing agent, thiamethoxam technical, chlorothalonil technical, fluxapyroxad technical and a defoamer in a pre-blender and mixing it for 1 hour,
b) milling the sample through air jet mill instrument at inlet pressure 2-3 kg/cm2, grinding pressure 6 kg/ cm2 and checking for the particle size < 15 micron,
c) collecting the milled material, and post blending the sample for 1 hour,
d) sending the sample to the quality analysis, and
e) packing the formulated material in a suitable package.

Dated this Twelfth (12th) day of October, 2023

_____________________________
Dr. S. Padmaja
Agent for the Applicant
IN/PA/883

Documents

Application Documents

# Name Date
1 202241059434-PROVISIONAL SPECIFICATION [18-10-2022(online)].pdf 2022-10-18
2 202241059434-POWER OF AUTHORITY [18-10-2022(online)].pdf 2022-10-18
3 202241059434-FORM 1 [18-10-2022(online)].pdf 2022-10-18
4 202241059434-Proof of Right [18-11-2022(online)].pdf 2022-11-18
5 202241059434-FORM 3 [12-10-2023(online)].pdf 2023-10-12
6 202241059434-ENDORSEMENT BY INVENTORS [12-10-2023(online)].pdf 2023-10-12
7 202241059434-COMPLETE SPECIFICATION [12-10-2023(online)].pdf 2023-10-12
8 202241059434-FORM-9 [14-10-2023(online)].pdf 2023-10-14
9 202241059434-FORM 18 [14-10-2023(online)].pdf 2023-10-14
10 202241059434-Covering Letter [02-11-2023(online)].pdf 2023-11-02