DESC:FORM 2

THE PATENTS ACT 1970
(SECTION 39 OF 1970)

&

THE PATENT RULES, 2003

COMPLETE SPECIFICATION
(Section 10 and Rule 13)

1. Title of the invention:

SYNERGISTIC FUNGICIDAL COMPOSITION CONTAINING PICOXYSTROBIN AND COPPER OXYCHLORIDE

2. Applicant(s):
NAME NATIONALITY ADDRESS
COROMANDEL INTERNATIONAL LIMITED Indian Coromandel House, 1-2-10,
Sardar Patel Road, Secunderabad,
Telangana-500003, India.
3. Preamble to the description

The following specification particularly describes the invention and the manner in which it is to be performed.

FIELD OF THE INVENTION
The present invention is related to a stable synergistic fungicidal composition comprising synergistically effective amount of Picoxystrobin and Copper oxychloride that providing significant broad-spectrum efficacy without causing any phytotoxicity to any part of the plant.

BACKGROUND OF THE INVENTION
In the field of crop protection, the use of a particular active substance for the control of specific fungi may become increasingly difficult in time, because of the adaptation of the mentioned fungi to the fungicide being used. This leads to the loss of effectiveness in the control of the pathogen, and, consequently, downfall in crop production and profitability.

Fungicides are compounds, of natural or synthetic origin, which act to protect plants against damage caused by fungi. Current methods of agriculture rely heavily on the use of fungicides. In fact, some crops cannot be grown usefully without the use of fungicides. Using fungicides allows a grower to increase the yield and the quality of the crop, and consequently, increase the value of the crop. In most situations, the increase in value of the crop is worth at least three times the cost of the use of the fungicide.

A very well-known and widely used form of approaching this problem is by using a combination of different active substances presenting different mechanisms of action.

Combinations of fungicides are often used to facilitate disease control, to broaden spectrum of control and to retard resistance development. Accordingly, new advantageous combinations are needed to provide a variety of options to best satisfy plant disease control needs. Furthermore, certain rare combinations of fungicides demonstrate a greater-than-additive (i.e., synergistic) effect to provide commercially important levels of plant disease control.

When two or more substances in combination demonstrate unexpectedly high biological activity, for example fungicidal activity, the resultant phenomenon may be referred to as synergism.
Picoxystrobin is a fungicide belonging to the strobilurin group of chemicals. It is a preventative and curative fungicide with systemic and translaminar movement, acting by inhibition of mitochondrial respiration by blocking electron transfer at the Qo centre of cytochrome Bc1. It is used for control of a range of fungal diseases, including brown rust, tan spot, powdery mildew, and net blotch in cereals, pulses, and oilseeds.

Copper oxychloride is an agricultural fungicide and bactericide used as a foliar spray. Since Copper oxychloride is an organic copper compound, it manifests greater systemic toxicity than inorganic compounds. It exists in several forms with different appearances that can be prepared by different routes, but all are the same compound. Copper oxychloride finds real-world applications as a fungicide and as a blue or green colouring agent in pyrotechnics, while also being used in niche applications as a catalyst for various reactions, such as the production of vinyl chloride.

Various compositions have been developed to control fungi and in practice have been used as a single or a mixed agent.

WO2007104677A1 discloses a combination of a strobilurin compound with copper-based fungicides. However, it neither discloses nor exemplifies the specific combination of picoxystrobin and copper oxychloride as active ingredients.

Practical agricultural experience has shown that the repeated and exclusive application of an individual active compound in the control of harmful fungi leads in many cases to a rapid selection of those fungus strains which have developed natural or adapted resistance against the active compound in question. Effective control of these fungi with the active compound in question is very difficult in such cases. Active compounds having different mechanisms of action are combined to delay the generation of resistance and reduce the application amount and prevention and treatment costs. Consequently, research is being conducted to produce fungicides and combinations of fungicides that are safer, that have better performance, that require lower dosages, that are easier to use, and that cost less.

SUMMARY OF THE INVENTION
Accordingly, the present invention provides a synergistic fungicidal composition comprising as its active ingredients Picoxystrobin and Copper oxychloride, which exhibits improved antifungal activity compared to either compound used alone.

In another aspect of the present invention provides a synergistic fungicidal composition comprising of Picoxystrobin and Copper oxychloride along with suitable agrochemical additives or mixture thereof.

In another aspect of the present invention provides a synergistic fungicidal suspension concentrate (SC) composition comprising:
a) Picoxystrobin is present in the range from 1% to 10% (w/w),
b) Copper oxychloride is present in the range from 20% to 70% (w/w), and
c) suitable agrochemical additives or mixture thereof in effective amounts.

In another aspect of the present invention, a synergistic fungicidal suspension concentrate (SC) composition comprising:
a) Picoxystrobin is present in the range from 1% to 10% (w/w),
b) Copper oxychloride is present in the range from 20% to 70% (w/w),
c) defoamer is present in the range from 0.1% to 2.0% (w/w),
d) preservative is present in the range from 0.01% to 0.5% (w/w),
e) anti-freezing agent is present in the range from 3% to 10% (w/w),
f) wetting agent is present in the range from 1% to 5% (w/w),
g) dispersing agent is present in the range from 1% to 10% (w/w),
h) emulsifier is present in the range from 0% to 5% (w/w),
i) rheology modifier is present in the range from 1% to 10% (w/w), and
j) Filler is present in Q.S. (quantum satis) to 100%.

In another aspect of the present invention provides a fungicidal composition that results into reduced fungal disease incidence in the crops to which it is applied.

In another aspect of the present invention provides a fungicidal composition that results into increased yield of the treated plant.

In another aspect of the present invention provides a synergistic fungicidal composition with an improved stability and ready to use fungicidal composition, having superior bio-efficacy compared to the individual formulations.

In yet another aspect of the present invention provides a synergistic fungicidal composition that results in an improved plant health and increases the plant longevity.

DETAILED 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 the purposes of detailed explanation, specific nomenclature is set forth to provide a thorough understanding of the present application.

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.

The terms "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.

The expression of various quantities in terms of “% (w/w)” or “%” means the percentage by weight, relative to the weight of the total solution or composition unless otherwise specified.

As used herein, the term “fungicidal” or “fungicide” refers to pesticides specifically used to destroy one or more species of fungal and fungal-like diseases incidence in the crops to which it is applied.

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, mature vegetation, and established vegetation.

As used herein, the terms “immature vegetation” refers to small vegetative plants prior to reproductive stage, and “mature vegetation” refers to vegetative plants during and after the reproductive stage.

As used herein, an "effective amount" refers to an amount of an active ingredient that causes a "fungicidal effect," i.e., an adversely modifying effect including, for instance, a deviation from natural growth or development, killing, regulation, desiccation, growth inhibition, growth reduction, and retardation of fungi.

As used herein, the term “synergistic composition” refers to 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” refers to a range of surfactants, dispersing agents, pigments, solvents, co-solvents, defoamers, emulsions, crystallization inhibitors, viscosity modifiers, suspending agents, dyes, antioxidants, 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, preservatives, sterilization agents, biocide, adjuvant among others.

As used herein, the term “yield” refers to the economic value that is produced by the plant such as grains, fruits in the proper sense, vegetables, nuts, grains, seeds, wood or even flowers.

In an embodiment of the present invention, a synergistic fungicidal composition comprising as its active ingredient’s Picoxystrobin, and Copper oxychloride along with suitable agrochemical additives or mixture thereof.

The compositions of the present invention are formulated into various formulations such as Granular composition (GR), Capsule suspension (CS), Dispersible concentrate (DC), Dustable powder (DP), Powder for dry seed treatment (DS), Emulsifiable concentrate (EC), Emulsifiable granule (EG), Emulsifiable water-in-oil (EO), Emulsifiable powder (EP), Emulsifiable for seed treatment (ES), Emulsifiable oil-in-water Soluble concentrate (SL), Spreading oil (SO), Water soluble powder (SP), Water soluble tablet (ST), Ultra-low volume (ULV), Suspension Concentrate (SC), Tablet (TB), Ultra-low volume (ULV) liquid, Water dispersible granules (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).

The present invention provides a synergistic fungicidal composition comprising as its active ingredient’s Picoxystrobin and Copper oxychloride along with suitable agrochemical additives or mixture thereof.

In a preferred embodiment of the present invention provides a synergistic fungicidal composition comprising:
a) Picoxystrobin is present in the range from 1% to 10% (w/w),
b) Copper oxychloride is present in the range from 20% to 70% (w/w), and
c) suitable agrochemical additives or mixture thereof in effective amounts.

In another embodiment, the synergistic fungicidal composition of the present invention is formulated as Suspension concentrate (SC) or Wettable powder (WP) or Water dispersible granule (WDG).

The agrochemically additives of the present synergistic fungicidal composition are selected from defoamer, preservative, anti-freezing agents, wetting agents, dispersing agents, disintegrating agents, anti-caking agents, emulsifiers, rheology modifiers, binders, co-filler and fillers.

In another embodiment of the present invention, a synergistic fungicidal suspension concentrate (SC) composition comprising:
a) Picoxystrobin is present in the range from 1% to 10% (w/w),
b) Copper oxychloride is present in the range from 20% to 70% (w/w),
c) defoamer is present in the range from 0.1% to 2.0% (w/w),
d) preservative is present in the range from 0.01% to 0.5% (w/w),
e) anti-freezing agent is present in the range from 3% to 10% (w/w),
f) wetting agent is present in the range from 1% to 5% (w/w)
g) dispersing agent is present in the range from 1% to 10% (w/w)
h) emulsifier is present in the range from 0% to 5% (w/w),
i) rheology modifier is present in the range from 1% to 10% (w/w), and
j) filler is present in Q.S. (quantum satis) to 100%.

In another embodiment of the present invention, a synergistic fungicidal wettable powder (WP) composition comprising:
a) Picoxystrobin is present in the range from 1% to 10% (w/w),
b) Copper oxychloride is present in the range from 20% to 70% (w/w),
c) wetting agent is present in the range from 1% to 5% (w/w),
d) dispersing agent is present in the range from 1% to 10% (w/w),
e) anti-caking agent is present in the range from 0.1% to 5% (w/w),
f) co-filler is present in the range from 1% to 10% (w/w), and
g) filler is present in Q.S. (quantum satis) to 100%.

In another embodiment of the present invention, a synergistic fungicidal water dispersible granule (WDG) composition comprising:
a) Picoxystrobin is present in the range from 1% to 10% (w/w),
b) Copper oxychloride is present in the range from 20% to 70% (w/w),
c) dispersing agent is present in the range from 1% to 10% (w/w),
d) wetting agent is present in the range from 1% to 5% (w/w),
e) defoamer is present in the range from 0% to 2.0% (w/w),
f) anti-caking agent is present in the range from 0.1% to 5% (w/w), and
g) filler is present in Q.S. (quantum satis) to 100%.

As used herein, the term “defoamer” refers to a chemical additive which is used to reduce and hinder the formation of foam in the liquid formulations.

In another embodiment of the invention provides suitable defoamer is selected from silicon emulsion, precipitated silica, fumed silica, modified phyllosilicate, either alone or mixtures thereof, present in an amount in the range from 0.1% to 2.0% (w/w).

As used herein, the term “preservative” refers to a critical component in agrochemical formulations, especially those containing water, such as suspension concentrates (SC), and soluble liquids (SL). The main purpose of preservative is to prevent microbial contamination which can degrade the product and reduce its effectiveness.

In another embodiment of the invention provides suitable preservative is 1,2-benzisothiazol-3(2H)-one, present in an amount in the range from 0.01% to 0.5% (w/w).

As used herein, the term “anti-freezing agent” refers to a chemical substance which prevents the said formulation from freezing.

In another embodiment of the invention provides suitable anti-freezing agent is selected from propylene glycol, glycerol or combinations thereof, present in an amount in the range from 3% to 10% (w/w).

As used herein, the term “wetting agent” refers to a type of surfactant that reduces the surface tension of a liquid, allowing sprays to spread evenly over waxy leaf surfaces and penetrate soil more effectively. This improves the coverage, adhesion, and efficacy of pesticides, herbicides, and fertilizers by ensuring uniform application, better contact with plant surfaces, and improved movement of water and nutrients.

In another embodiment of the invention provides suitable wetting agent is selected from polyoxyalkylene fatty alcohol ether (TENSIOFIX 96DB 08), sodium isopropyl naphthalene sulfonate, sodium lauryl sulphate, or combination thereof, present in an amount in the range from 1% to 5% (w/w).

TENSIOFIX 96DB 08 contains a polyoxyalkylene fatty alcohol ether (e.g., a fatty alcohol alkoxylate or a polyalkylene glycol fatty alkyl ether) which is an EO-PO copolymer ether prepared from a fatty alcohol, ethylene oxide (oxirane) and propylene oxide (methyl oxirane). The fatty alcohol may include one or more of a C2 -C15 linear or branched, fully saturated, carbon chain, and the EO (ethylene oxide) and PO (propylene oxide) units may be in a random or block arrangement in the copolymer chain. Examples of fatty alcohols may include, lauryl alcohol (e.g., 1-dodecanol), tridecyl alcohol (e.g., I-tridecanol) myristyl alcohol (e.g., 1-tetradecanol), pentadecyl alcohol (e.g., 1-pentadecanol), and mixtures thereof.

As used herein, the term “dispersing agent” refers to a chemical substance, which is typically a surfactant, that is added to a suspension of solid or liquid particles in a liquid (such as a colloid or emulsion) to improve the separation of the particles and to prevent their settling or clumping. They can disperse active ingredients in the formulation and prevent agglomeration after dispersal in water.

In another embodiment of the invention provides suitable dispersing agent is selected from sodium ligno sulphonate, kraft lignin sulphonate, acrylic copolymer, polyoxyethylene alkyl ether (ATLOX 4894), sodium salt of alkyl naphthalene sulphonate, mixture of naphthalene sulfonic acid and phenol sulphonic acid condensate sodium salt, kraft lignin polymer or combination thereof, present in an amount in the range from 1% to 10% (w/w).

As used herein, the term “emulsifier” refers to surfactants that create stable mixtures of oil-based active ingredients and water, enabling even distribution and absorption by plants for effective pest, weed, and disease control.

In another embodiment of the present invention, suitable emulsifier is selected from tristyryl phenyl ethoxylate (SOPROPHOR BSU), calcium alkyl benzene sulfonate, either alone or mixtures thereof, present in an amount in the range from 0% to 5% (w/w).

As used herein, the term “rheology modifier” refers to substances designed to bring superior structuring to formulations, allowing to control the viscosity and are easy to use and provide better stability, and suspensibility performance. Flowable formulations require a rheology modifier to prevent sedimentation phenomena.

In another embodiment of the invention provides suitable rheology modifier is selected from xanthan gum, aluminium magnesium silicate, either alone or mixtures thereof, present in an amount in the range from 1% to 10% (w/w).

As used herein, the term “disintegrating agent” refers to an additive that can be sometime useful for improving dispersibility of herbicide formulation.

In another embodiment of the invention provides suitable disintegrating agents selected from ammonium sulphate, and sodium sulphate anhydrous, either alone or mixtures thereof, present in an amount in the range from 15% to 25% (w/w).
As used herein, the term “anti-caking agent” refers to an additive used in the pesticide industry to avoid the formation of lumps.

In another embodiment of the invention provides suitable anti-caking agent is selected from silicon dioxide, precipitated silica powder, polydimethylsiloxane, silicon-based agents, either alone or mixtures thereof, present in an amount in the range from 0.1% to 5% (w/w).

As used herein, the term “binder” refers to a substance that holds other ingredients together to form larger, cohesive granules or particles

In another embodiment of the invention provides suitable binder is polyvinyl pyrrolidone, present in an amount in the range from 0% to 2% (w/w).

As used herein, the term “co-filler” refers to substance added to a pesticide product other than the active ingredient. These ingredients are crucial for enhancing the product's performance, improving stability, and ensuring the active compound is delivered effectively.

In another embodiment of the invention provides suitable co-filler is lactose monohydrate, present in an amount in the range from 1% to 10% (w/w).

As used herein, the term “filler” refers to solid chemicals that are added to a pesticide formulation to aid in the delivery of the active ingredient.

In another embodiment of the invention provides suitable filler selected from distilled water, china clay, kaolin, and starch, either alone or mixtures thereof, present in Q.S.

In yet another embodiment of the present invention, a process for preparation of fungicidal composition of Picoxystrobin, and Copper oxychloride along with suitable agrochemical additives or mixture thereof in a different formulations such as Suspension concentrate (SC), Wettable powder (WP) or Water dispersible granule (WDG), wherein these formulations/compositions prepared by mixing required quantity of active ingredients with agrochemical additives/excipients under certain appropriate conditions. The process for preparation of each composition is provided in the example section.

In another embodiment of the present invention, use of a fungicidal composition of Picoxystrobin, and Copper oxychloride along with suitable agrochemical additives or mixture thereof.

In yet another embodiment of the present invention, use of said fungicidal composition, which demonstrates a high controlling effect with reduced environmental load and reduced cost in crop production as well as crop protection.

In yet another embodiment of the present invention, use of said synergistic fungicidal composition which can decrease the cost of application, save fuel cost, labour cost and therefore very economical.

In yet another embodiment of the present invention, said synergistic fungicidal decreases application rates of each of the active ingredients and is non-phytotoxic. Thus, it is effective to reduce the environmental load on an area where the composition is applied or a surrounding area thereof.

In yet another embodiment of the present invention, the said synergistic suspension concentrate (SC) formulation of Picoxystrobin and Copper oxychloride of the present invention provides multiple advantages includes,

• Broader spectrum of activity (better preventive + curative activity),
• Stronger and broader disease control across both external and internal pathogen phases,
• Improved resistance rainfastness or residual protection,
• Potentially fewer sprays, more residual protection,
• Potential improvement in crop health beyond disease control, and
• Possible yield & quality gains
In yet another embodiment of the present invention, the said synergistic fungicidal formulation of Picoxystrobin and Copper oxychloride in wettable powder (WP) or water dispersible granule (WDG) can offer very good disease control by combining preventive surface protection plus internal systemic protection, and high loading, cost effectiveness, good residual control, reduced dust (especially with WDG), safer handling, etc.

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

EXAMPLES:

Example 1: Picoxystrobin 7.5% + Copper oxychloride 50% SC
S. No. Composition Function Charge in (%)
1. Picoxystrobin Active Ingredient 7.5
2. Copper oxychloride Active Ingredient 50.0
3. Silicone emulsion Defoamer 0.50
4. 1,2-Benzisothiazol-3(2H)-one Preservative 0.10
5. Propylene Glycol Anti-freezing Agent 5.0
6. Polyoxyalkylene fatty alcohol ether (TENSIOFIX 96DB 08) Wetting Agent 3.0
7. Tri styryl phenol ethoxylates Emulsifier 2.0
8. Kraft Lignin Sulphonate Dispersing Agent 1.0
9. Xanthan gum Rheology Modifier 9.0
10. Distilled Water Filler Q. S.

Preparation Method of Picoxystrobin 7.5% + Copper oxychloride 50% SC:
Step 1: Based on the batch size, the raw materials charged into the mixing vessel in the following order:
• Filler
• Rheology modifier
• Anti-freezing agent
• Defoamer
• Preservative
• Wetting agent
• Dispersing agent
• Emulsifier
• Picoxystrobin Technical
• Copper oxychloride Technical
Step 2: Pre-mix the resulting slurry in a mixing chamber to achieve uniform dispersion.
Step 3: Passed the pre-mixed slurry through a bead mill for wet milling.
Step 4: Collected the milled slurry, washed the bead mill with the remaining distilled water, and added the washings to the slurry. Checked the particle size of the milled slurry. If the particle size meets the specification (d50 value < 5 µm), transfer the material to the mixing chamber and commence mixing.
Step 5: In a separate high-speed shear mixer, prepared a 2% xanthan gum solution.
Step 6: The prepared 2% xanthan gum solution was added to the milled slurry under continuous stirring, and continued stirring for 1 hour, then collected a sample for analysis.
Step 7: Upon confirmation of the analysis results, proceed with packing of the formulation.

Example 2: Picoxystrobin 5.0% + Copper oxychloride 60% SC
S. No. Composition Function Charge in (%)
1. Picoxystrobin Active Ingredient 5.0
2. Copper oxychloride Active Ingredient 60.0
3. Silicone emulsion Defoamer 1.0
4. 1,2-Benzisothiazol-3(2H)-one Preservative 0.1
5. Propylene Glycol Anti-freezing Agent 5.0
6. Acrylic Copolymer Dispersing Agent 3.0
7. Sodium ligno sulphonate Dispersing Agent 2.0
8. Polyoxyethylene alkyl ether (NPE-free) (ATLOX 4894) Wetting Agent 3.0
9. Xanthan gum Rheology Modifier 5.0
10. Water Filler Q. S.

Preparation method similar to the one described in Example 1.

Example 3: Picoxystrobin 7.5% + Copper oxychloride 50% WP
S. No. Composition Function Charge in (%)
1. Picoxystrobin Active Ingredient 7.5
2. Copper oxychloride Active Ingredient 50.0
3. Isodecyl alcohol ethoxylate Wetting agent 1.0
4. Sodium Ligno Sulphonates Dispersing agent 2.0
5. Sodium salt of Alkyl Naphthalene Sulphonate Dispersing agent 8.0
6. Silicon dioxide Anti-caking Agent 3.0
7. Lactose monohydrate Co-filler 5.0
8. China clay Filler Q.S.

Preparation method of Picoxystrobin 7.5% + Copper oxychloride 50% WP
Step 1: According to the batch size, all raw materials were mixed in the following order:
• Picoxystrobin Technical
• Copper oxychloride Technical
• Wetting agent
• Dispersing agent
• Anticaking Agent
• Co-filler
• Filler
Step 2: The sample was pre-mixed in a blender.
Step 3: The sample was milled using an Air Jet Mill.
Step 4: The air jet milled sample was collected and post-blended in a blender.
Step 5: The sample was submitted for analysis.
Step 6: The product was packed.

Example 4: Picoxystrobin 7.5% + Copper oxychloride 50% WDG
S. No. Composition Function Charge in (%)
1. Picoxystrobin Active Ingredient 7.5
2. Copper oxychloride Active Ingredient 50.0
3. Mixture of Naphthalene sulfonic acid and phenol sulphonic acid condensate Sodium salt Dispersing Agent 5.0
4. Naphthalene sulfonic acid and phenol sulphonic acid Sodium salt Dispersing Agent 3.0
5. Sodium Lauryl Sulphate Wetting Agent 3.0
6. Proprietary Blend Defoamer 0.5
7. Silicon dioxide Anti caking agent 1.0
8. Aluminium silicate Filler Q.S.

Preparation method of Picoxystrobin 7.5% + Copper oxychloride 50% WDG:
Step 1: According to the batch size, all raw materials were mixed in the following order:
• Picoxystrobin Technical
• Copper oxychloride Technical
• Wetting agent
• Dispersing agent
• Anticaking Agent
• Dispersing agent
• Defoamer
• Filler
Step 2: The sample was pre-mixed in a blender.
Step 3: The sample was milled using an Air Jet Mill.
Step 4: The air jet milled sample was collected and post-blended in a blender.
Step 5: A mixture of water, binder, and defoamer was prepared for dough preparation.
Step 6: The granules were extruded using a basket extruder, ensuring that the temperature did not exceed 45°C.
Step 7: The WDG was collected and dried in a fluid bed dryer (FBD) at 50°C. The moisture content was checked to ensure it was below 3.0%.
Note: During FBD drying, the air flow rate was maintained between 50–70.
Step 8: The sample was submitted for analysis.
Step 9: The product was packed.

SYNERGY STUDIES:
A synergistic effect exists wherever the action of a combination of active ingredient is greater than the sum of the action of each of the components alone. Therefore, a synergistically effective amount or an effective amount of a synergistic composition or combination is an amount that exhibits greater pesticidal activity than the sum of the pesticidal activities of the individual components.

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

If A1 = the percent inhibition of growth by insecticide A at given rate
B1 = the percent inhibition of growth by insecticide B at given rate then,

If observed value is greater than expected result (Obs. > E): synergy
If observed value is less than expected result (Obs. < E): antagonism

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

Efficacy study for combination of Picoxystrobin 7.5% + Copper oxychloride 50% in Suspension concentrate (SC) form:

Trial 1: Bio-efficacy against Tomato Late blight
The late blight is caused by the Oomycete group of fungal pathogen Phytophthora infestans. This is potentially devasting disease can infect tomato foliage and fruit at any stage of crop development. The first symptoms of late blight in the field are small, light to dark green, circular to irregular-shaped water-soaked spots. These lesions usually appear first on the lower leaves. Lesions often begin to develop near the leaf tips or edges, where dew is retained the longest. During cool, moist weather, these lesions expand rapidly into large, dark brown or black lesions, often appearing greasy. The lesions are not limited by leaf veins, and as new infections occur and existing infections coalesce, entire leaves can become blighted and killed within just a few days. The lesions also may be present on petioles and stems of the plant. Maximum and minimum temperatures in the range of 16-20°C and 1-6°C were found favourable for Tomato blight disease. Similarly, relative humidity, rainfall, and wind speed in the range of 63-71%, 1.5-3.75 mm and 1-5.5 Km/h, respectively, were conducive for PLB disease which are helpful in disease development.

The field trial was conducted to evaluate the efficacy of innovative mixtures of Picoxystrobin and Copper oxychloride against phytophthora infestans fungus in tomato crop. Trial was conducted with randomized block design with net plot size of 5m x 6m. Tomato crop was raised with all standard agronomic practices. Spraying was done with manual operated backpack knapsack sprayer with 500 L of water spray volume per hectare at 45 days after planting.
The visual observations were recorded for % disease control from ten plants per plot. The observations were recorded at before spraying, 7 DAA (Days after application) and 14 DAA (Days after application).

Table 1: Late blight disease control in Tomato:
Compositions Dose gm or ml/ha Percent disease control – Phytophthora infestans.
07 DAA 14 DAA
Picoxystrobin 22.52% SC 100 55 50
Copper oxychloride 50% WG 1000 70 60
Picoxystrobin 7.5% +
Copper oxychloride 50% SC 1100 90 85

The trial results demonstrated that the formulation of Picoxystrobin 7.5% + Copper oxychloride 50% SC provided excellent efficacy against late blight disease in tomato. In contrast, the solo applications of the individual active ingredients did not deliver satisfactory control. The combination was found to be highly promising not only in terms of disease control efficacy but also in providing effective residual protection against tomato late blight.

Table 2: Percent late blight disease control at 14 DAA:
Compositions Dose gm or ml/ha % late blight disease control
Expected Actual
Picoxystrobin 22.52% SC 100 50
Copper oxychloride 50% WG 1000 60
Picoxystrobin 7.5% +
Copper oxychloride 50% SC 1100 80.3 85
Ratio of O/E 1.05

The results presented in Table 2 clearly demonstrate the synergistic effect of the fungicidal combination of Picoxystrobin 7.5% + Copper oxychloride 50% SC in controlling late blight disease in Tomato. The substantial difference observed between the expected and actual efficacy highlights the enhanced performance of the combination, confirming a strong synergistic interaction between the two active ingredients.

Trial 2: Bio-efficacy against Tomato Early blight
The early blight is caused by the fungal pathogen Alternaria solani. This is potentially devasting disease. Warm, humid (24-29°C/ 75-84°F) environmental conditions are conducive to infection. Its major threat to many vegetable and fruit crops and can also affect the crop stand and yield. The first symptoms of early blight appear as small, circular, or irregular, dark brown to black spots on the older (lower) leaves. These spots enlarge up to 3/8 inch in diameter and gradually may become angular-shaped. These first lesions appear about two to three days after infection, with further sporulation on the surface of these lesions occurring three to five days later. Early blight lesions can be diagnosed in the field easily due to the dark concentric rings alternating with bands of light-tan tissue, giving them a distinctive target spot appearance. Multiple lesions on the same leaf also may coalesce, or grow together, to form one mass. As lesions coalesce, chlorosis (yellowing of plant tissue) may be visible due to clusters of infection. Elongated, brown to black lesions also may develop on stems and petioles of infected plants.

The field trial was conducted to evaluate the efficacy of innovative mixtures of Picoxystrobin and Copper oxychloride against Alternaria solani fungus in Tomato crop. Trial was conducted with randomized block design with net plot size of 5m x 6m. Tomato crop was raised with all standard agronomic practices. Spraying was done with manual operated backpack knapsack sprayer with 500 L of water spray volume per hectare at 45 days after planting.

The visual observations were recorded for % disease control from ten plants per plot. The observations were recorded at before spraying, 7 DAA (Days after application) and 14 DAA (Days after application).

Table 3: Early blight disease control in Tomato:
Compositions Dose gm or ml/ha Percent disease control – Alternaria solani.
07 DAA 14 DAA
Picoxystrobin 22.52% SC 100 65 60
Copper oxychloride 50% WG 1000 50 45
Picoxystrobin 7.5% +
Copper oxychloride 50% SC 1100 85 80

The trial results demonstrated that the formulation of Picoxystrobin 7.5% + Copper oxychloride 50% SC provided excellent efficacy against early blight disease in tomato. In contrast, the solo applications of the individual active ingredients did not deliver satisfactory control. The combination was found to be highly promising not only in terms of disease control efficacy but also in providing effective residual protection against tomato early blight.

Table 4: Percent Early blight disease control at 14 DAA:
Compositions Dose gm or ml/ha % Early blight disease control
Expected Actual
Picoxystrobin 22.52% SC 100 60
Copper oxychloride 50% WG 1000 45
Picoxystrobin 7.5% +
Copper oxychloride 50% SC 1100 78.27 80
Ratio of O/E 1.02

The results presented in Table 4 clearly demonstrate the synergistic effect of the fungicidal combination of Picoxystrobin 7.5% + Copper oxychloride 50% SC in controlling early blight disease in Tomato. The substantial difference observed between the expected and actual efficacy highlights the enhanced performance of the combination, confirming a strong synergistic interaction between the two active ingredients.

Trial 3: Bio-efficacy against Potato Late blight
The late blight is caused by the Oomycete group of fungal pathogen Phytophthora infestans. This is potentially devasting disease can infect Potato foliage and fruit at any stage of crop development. The first symptoms of late blight in the field are small, light to dark green, circular to irregular-shaped water-soaked spots. These lesions usually appear first on the lower leaves. Lesions often begin to develop near the leaf tips or edges, where dew is retained the longest. During cool, moist weather, these lesions expand rapidly into large, dark brown or black lesions, often appearing greasy. The lesions are not limited by leaf veins, and as new infections occur and existing infections coalesce, entire leaves can become blighted and killed within just a few days. The lesions also may be present on petioles and stems of the plant. Maximum and minimum temperatures in the range of 16-20°C and 1-6°C were found favourable for Potato blight disease. Similarly, relative humidity, rainfall, and wind speed in the range of 63-71%, 1.5-3.75 mm and 1-5.5 Km/h, respectively, were conducive for PLB disease which are helpful in disease development.

The field trial was conducted to evaluate the efficacy of innovative mixtures of Picoxystrobin and Copper oxychloride against phytophthora infestans fungus in Potato crop. Trial was conducted with randomized block design with net plot size of 5m x 6m. Potato crop was raised with all standard agronomic practices. Spraying was done with manual operated backpack knapsack sprayer with 500 L of water spray volume per hectare at 45 days after planting.
The visual observations were recorded for % disease control from ten plants per plot. The observations were recorded at before spraying, 7 DAA (Days after application) and 14 DAA (Days after application).

Table 5: Late blight disease control in Potato:
Compositions Dose gm or ml/ha Percent disease control – Phytophthora infestans.
07 DAA 14 DAA
Picoxystrobin 22.52% SC 100 60 55
Copper oxychloride 50% WG 1000 70 60
Picoxystrobin 7.5% +
Copper oxychloride 50% SC 1100 90 85

The trial results demonstrated that the formulation of Picoxystrobin 7.5% + Copper oxychloride 50% SC provided excellent efficacy against late blight disease of Potato. In contrast, the solo applications of the individual active ingredients did not deliver satisfactory control. The combination was found to be highly promising not only in terms of disease control efficacy but also in providing effective residual protection against potato late blight.

Table 6: Percent late blight disease control at 14 DAA:
Compositions Dose gm or ml/ha % late blight disease control
Expected Actual
Picoxystrobin 22.52% SC 100 55
Copper oxychloride 50% WG 1000 60
Picoxystrobin 7.5% +
Copper oxychloride 50% SC 1100 82.33 85
Ratio of O/E 1.03

The results presented in Table 6 clearly demonstrate the synergistic effect of the fungicidal combination of Picoxystrobin 7.5% + Copper oxychloride 50% SC in controlling late blight disease in Potato. The substantial difference observed between the expected and actual efficacy highlights the enhanced performance of the combination, confirming a strong synergistic interaction between the two active ingredients.

Trial 4: Bio-efficacy against Potato Early blight
The early blight is caused by the fungal pathogen Alternaria solani. This is potentially devasting disease. Warm, humid (24-29°C/ 75-84°F) environmental conditions are conducive to infection. Its major threat to many vegetable and fruit crops and can also affect the crop stand and yield. The first symptoms of early blight appear as small, circular, or irregular, dark brown to black spots on the older (lower) leaves. These spots enlarge up to 3/8 inch in diameter and gradually may become angular-shaped. These first lesions appear about two to three days after infection, with further sporulation on the surface of these lesions occurring three to five days later. Early blight lesions can be diagnosed in the field easily due to the dark concentric rings alternating with bands of light-tan tissue, giving them a distinctive target spot appearance. Multiple lesions on the same leaf also may coalesce, or grow together, to form one mass. As lesions coalesce, chlorosis (yellowing of plant tissue) may be visible due to clusters of infection. Elongated, brown to black lesions also may develop on stems and petioles of infected plants.

The field trial was conducted to evaluate the efficacy of innovative mixtures of Picoxystrobin and Copper oxychloride against Alternaria solani fungus in Potato crop. Trial was conducted with randomized block design with net plot size of 5m x 6m. Potato crop was raised with all standard agronomic practices. Spraying was done with manual operated backpack knapsack sprayer with 500 L of water spray volume per hectare at 45 days after planting.

The visual observations were recorded for % disease control from ten plants per plot. The observations were recorded at before spraying, 7 DAA (Days after application) and 14 DAA (Days after application).

Table 7: Early blight disease control in Potato:
Compositions Dose gm or ml/ha Percent disease control – Alternaria solani.
07 DAA 14 DAA
Picoxystrobin 22.52% SC 100 65 55
Copper oxychloride 50% WG 1000 60 50
Picoxystrobin 7.5% +
Copper oxychloride 50% SC 1100 85 80

The trial results demonstrated that the formulation of Picoxystrobin 7.5% + Copper oxychloride 50% SC provided excellent efficacy against early blight disease of Potato. In contrast, the solo applications of the individual active ingredients did not deliver satisfactory control. The combination was found to be highly promising not only in terms of disease control efficacy but also in providing effective residual protection against potato early blight.
Table 8: Percent Early blight disease control at 14 DAA:
Compositions Dose gm or ml/ha % Early blight disease control
Expected Actual
Picoxystrobin 22.52% SC 100 55
Copper oxychloride 50% WG 1000 50
Picoxystrobin 7.5% +
Copper oxychloride 50% SC 1100 77.5 80
Ratio of O/E 1.03

The results presented in Table 8 clearly demonstrate the synergistic effect of the fungicidal combination of Picoxystrobin 7.5% + Copper oxychloride 50% SC in controlling early blight disease in potato. The substantial difference observed between the expected and actual efficacy highlights the enhanced performance of the combination, confirming a strong synergistic interaction between the two active ingredients.

,CLAIMS:We Claim:
1. A synergistic fungicidal suspension concentrate (SC) composition comprising:
a) Picoxystrobin is present in the range from 1% to 10% (w/w),
b) Copper oxychloride is present in the range from 20% to 70% (w/w),
c) Defoamer is present in the range from 0.1% to 2.0% (w/w),
d) Preservative is present in the range from 0.01% to 0.5% (w/w),
e) Anti-freezing agent is present in the range from 3% to 10% (w/w),
f) Wetting agent is present in the range from 1% to 5% (w/w)
g) Dispersing agent is present in the range from 1% to 10% (w/w)
h) Emulsifier is present in the range from 0% to 5% (w/w),
i) Rheology modifier is present in the range from 1% to 10% (w/w), and
j) Filler is present in Q.S. (quantum satis) to 100%.

2. The composition as claimed in claim 1, wherein the defoamer is selected from silicon emulsion, precipitated silica, fumed silica, modified phyllosilicate, either alone or mixtures thereof.

3. The composition as claimed in claim 1, wherein the preservative is 1,2-benzisothiazol-3(2H)-one.

4. The composition as claimed in claim 1, wherein the anti-freezing agent is selected from propylene glycol, glycerol or combinations thereof.

5. The composition as claimed in claim 1, wherein the wetting agent is selected from polyoxyalkylene fatty alcohol ether (TENSIOFIX 96DB 08), sodium isopropyl naphthalene sulfonate, sodium lauryl sulphate, or combination thereof.

6. The composition as claimed in claim 1, wherein the dispersing agent is selected from sodium ligno sulphonate, kraft lignin sulphonate, acrylic copolymer, polyoxyethylene alkyl ether (ATLOX 4894), sodium salt of alkyl naphthalene sulphonate, mixture of naphthalene sulfonic acid and phenol sulphonic acid condensate sodium salt, kraft lignin polymer or combination thereof.

7. The composition as claimed in claim 1, wherein the emulsifier is selected from tristyryl phenyl ethoxylate (SOPROPHOR BSU), calcium alkyl benzene sulfonate, either alone or mixtures thereof.

8. The composition as claimed in claim 1, wherein the rheology modifier is selected from xanthan gum, aluminium magnesium silicate, either alone or mixtures thereof.

9. The composition as claimed in claim 1, wherein the filler selected from distilled water, china clay, kaolin, and starch, either alone or mixtures thereof.

Dated this Twenty-Fourth (24th) day of September 2025


Sahadev Katam
Sr. General Manager, Legal-IPR
Coromandel International Limited
Registered Patent Agent No. IN/PA/5560