Stable synergistic insecticidal composition
A synergistic insecticidal composition of Ethion, 4-chloro-3-ethyl-1-methyl-N-[[4-(4-methylphenoxy)phenyl]methyl]-1H-pyrazole-5-carboxamide, and Fluxametamide addresses resistance and broad-spectrum pest control, offering enhanced efficacy and environmental safety.
Patent Information
- Application Number
- PCT/IB2025/051111
- Authority / Receiving Office
- WO · WO
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2024-02-02
- Filing Date
- 2025-02-02
- Publication Date
- 2025-08-07
AI Technical Summary
Existing insecticidal compositions often fail to achieve synergistic effects, leading to resistance development and reduced efficacy against a broad spectrum of insect pests, while also posing environmental risks and increasing costs.
A stable synergistic insecticidal composition comprising Ethion, 4-chloro-3-ethyl-1-methyl-N-[[4-(4-methylphenoxy)phenyl]methyl]-1H-pyrazole-5-carboxamide, and Fluxametamide, which act synergistically to provide broad-spectrum pest control with enhanced knockdown and residual activity, reducing the likelihood of resistance and environmental impact.
The composition effectively controls a wide range of insect pests, including resistant strains, with improved stability, safety, and reduced application frequency, enhancing plant health and yield without adverse environmental effects.
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Abstract
Description
[0001] STABLE SYNERGISTIC INSECTICIDAL COMPOSITION
[0002] FIELD OF THE INVENTION
[0003] The present invention relates to stable synergistic insecticidal composition for the control of plant and crop pests including insect pests. More particularly, the present invention relates to a stable synergistic insecticidal composition comprising A) Ethion or its agrochemically acceptable salts, esters and derivatives; B) Compound of Formula I, chemically known as 4-chloro-3-ethyl-l- methyl-N-[[4-(4-methylphenoxy)phenyl]methyl]-lH-pyrazole-5-carboxamide or its agrochemically acceptable salts, esters and derivatives; and C) Fluxametamide or its agrochemically acceptable salts, esters and derivatives .The present invention also relates to a process for preparation of such stable synergistic insecticidal composition for synergistic and efficacious control of insect pests.
[0004] BACKGROUND OF THE INVENTION
[0005] Background description includes information that may be useful in understanding the present invention. It is not an admission that any of the information provided herein is prior art or relevant to the present invention, or that any publication specifically or implicitly referenced is prior art.
[0006] The control of insect pests is a persistent challenge in various industries including agriculture and public health. The reliance on single insecticides has, in some instances, led to the development of resistance among pest populations, necessitating innovative approaches to overcome this limitation. The concept of combining multiple insecticides to leverage synergistic interaction offers a promising solution. However, it is important to acknowledge that not all combinations result in synergistic effects. In some cases, the interactions between different insecticides can lead to antagonism, reducing the overall effectiveness of combination. The present invention adopts a research driven approach to address the challenges associated with creating synergistic effect with the use of organophosphate insecticide with the combination of other insecticides which provides broad spectrum pest control. The present invention involves a ternary insecticidal composition that brings together aliphatic organophosphates insecticide in combination with other insecticides that exhibit different modes of action. This strategic combination aims to target pest through multiple physiological pathways, thereby increasing the potency of treatment and reducing the likelihood of resistance emergence. Aliphatic organophosphates are well known neurotoxins that have been extensively used in pest control due to their impact on nervous system of insects. The present invention primarily focusses on the combination of compound Ethion which belongs from aliphatic organophosphate insecticides class with other insecticides to provide broad spectrum pest control including knock down activity with prolonged insect control. There are various prior arts which disclose compositions comprising combination of aliphatic organophosphate insecticide with other insecticides.
[0007] Reliance can be placed on IN202117047669, which discloses combination of Pymetrozine with ethion wherein the weight percentage of ethion or its acceptable salt(s) thereof 80% to 2% and the weight percentage of additives is 10% to 90%.
[0008] To control insect pests, it is necessary to spray and use an insecticidal composition, effective for target insect pests at appropriate times throughout the cultivation period and insect life cycle. In the practice of pest control, particularly insect control, there are two main factors which determine the effectiveness of the treatment; 1) immediate action on the pests (known in the art as "knockdown action"), 2) long term action (known also as "residual action"). The effective insecticidal composition for insect control ought to qualify both these factors.
[0009] It is always preferable to be able to reduce the amount of chemical agents released into the environment while still ensuring effective pest control. Although insect pest control agent combinations have been studied, a high synergistic action has not always been found. There is however a need for improvement of these combinations. Single active compositions used over a long period of time has resulted in resistance. With the onset of resistance to certain pests, there is a need in the art for a combination of insecticidal actives that decrease the chances of resistance and improves the spectrum of disease and insect pest control.
[0010] Combination of insecticides are used to broaden the spectrum of control of insects, to improve the insect pest control with synergistic effect, reduce dosage, thereby reducing environmental impact, decrease chances of development and management of resistance and to enhance residual control so lesser the number of sprays for crop protections and minimizing the insecticidal load in ecosystem. Insecticidal compositions that can be applied at as low a dose as possible and be effective in controlling pest species of insects while causing as little harm as possible to beneficial insects and minimal disturbance in the environment are in demand by the farming community.
[0011] Although, many combinations of insecticidal agents have been studied, a synergistic effect is rarely attained. Therefore, there is still a need for novel insecticidal composition comprising combination of insecticides which have different chemistry but are broad spectrum to cover efficacious control of large number of insect pests including complex sucking pests which also exhibits synergistically enhanced action, a broader scope of activity at a reduced cost of treatment.
[0012] Therefore, there is a need for an insecticidal formulation that is highly efficient, non- toxic, covers a broader spectrum of insects and is environment friendly and economical. Accordingly, there exists a continuous need for new insecticidal combinations to be applied so as to provide an economical and effective solution in terms of insect control, yield, plant growth, broader crop protection spectrum, reduce the burden on the environment / farmers, healthy foliage, saves labour cost and is yet cost-effective to the end user.
[0013] Therefore, there is still a need for novel insecticidal composition comprising Organophosphate compound with insecticides which have different chemistry but are broad spectrum to cover efficacious control of large number of insect pests, which also exhibits synergistically enhanced action, a broader scope of activity at a reduced cost of treatment.
[0014] In light of the above, there is still a need for novel insecticidal composition that exhibit synergistically enhanced action, a broader scope of activity and reduced cost of treatment. So, there is a need for a composition comprising, which overcomes some of the existing problems and can be prepared easily without much complex manufacturing process.
[0015] Accordingly, the present invention provides a stable synergistic insecticidal composition comprising A) Ethion or its agrochemically acceptable salts, esters and derivatives; B) Compound of Formula I, chemically known as 4-chloro-3-ethyl-l-methyl-N-[[4-(4- methylphenoxy)phenyl]methyl]-lH-pyrazole-5-carboxamide or its agrochemically acceptable salts, esters and derivatives; and C) Fluxametamide or its agrochemically acceptable salts, esters and derivatives.
[0016] Ethion is an aliphatic organothiophosphate insecticides. The mode of action of is that it acts as acetylcholine esterase inhibitor and having non-systemic action with a predominate contact action. Ethion show effective control against Red spidermite (Tetranychus urticae), Planthoppers, Aphids, Scale insects, Codling moth. Chemical structure of Ethion is provided below:
[0017] Compound of Formula I, chemically known as 4-chloro-3 -ethyl- 1 -methyl -N-[[4-(4- methylphenoxy)phenyl]methyl]-lH-pyrazole-5-carboxamide. The mode of action of Compound of Formula I is that it act as mitochondrial complex I electron transport inhibitor and having broad spectrum with contact activity which exhibits antifeedant activity especially against Lepidoptera sp. This Formula I compound is a broad spectrum pyrazole class insecticide and a miticide, with contact activity against target pests on eggs, larvae, nymphs and adults. It also has anti-feeding activity on larvae of lepidopteran insects. It has activity against several economically important insect pests of vegetables, fruits, nuts, vines and row crops. Chemical structure of Compound of Formula I is provided below: Fluxametamide is an isoxazoline insecticide, chemically known as 4-[(5RS)-5-(3,5- dichlorophenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl]-N-[(EZ)-(methoxyimino)methyl]- 2-methylbenzamide. It has a role as a ligand-gated chloride channel (LGCC) antagonist. It is wide spectrum isoxazoline insecticide effective against houseflies, spider mite, leafhoppers. Chemical structure of Compound of Fluxametamide is provided below:
[0018] The present invention further provides a novel method of preparing composition comprising above mentioned active ingredients, which composition is stable as well as provide desired bio-efficacy, synergy. Embodiments of the present invention may therefore ameliorate one or more of the above- mentioned problems.
[0019] OBJECTS AND ADVANTAGES OF THE INVENTION
[0020] Accordingly, the main objective of the present invention is to provide a stable synergistic insecticidal composition for control of broad spectrum of insect pests affecting plants, crops.
[0021] Another object of the present invention is to provide a stable synergistic insecticidal composition comprising A) Ethion or its agrochemically acceptable salts, esters and derivatives; B) Compound of Formula I, chemically known as 4-chloro-3-ethyl-l-methyl-N-[[4-(4- methylphenoxy)phenyl]methyl]-lH-pyrazole-5-carboxamide or its agrochemically acceptable salts, esters and derivatives; and C) Fluxametamide or its agrochemically acceptable salts, esters and derivatives.
[0022] It is another object of the present invention to provide improved, stable and ready to use stable synergistic insecticidal composition having synergistic and superior properties compared to prior art formulations or mixtures or compositions. Another object of the present invention is to provide a process for the preparation of a stable synergistic insecticidal composition comprising A) Ethion or its agrochemically acceptable salts, esters and derivatives; B) Compound of Formula I, chemically known as 4-chloro-3-ethyl-l- methyl-N-[[4-(4-methylphenoxy)phenyl]methyl]-lH-pyrazole-5-carboxamide or its agrochemically acceptable salts, esters and derivatives; and C) Fluxametamide or its agrochemically acceptable salts, esters and derivatives.
[0023] Further object of the present invention is to provide a stable synergistic insecticidal composition that provides effective immediate and long-term pest control.
[0024] A further object of the present invention is to provide a method for pest control that is both effective in the short and long term.
[0025] It is another object of the present invention to provide a stable synergistic insecticidal composition which can be easily formulated.
[0026] Yet another object of the present invention is to provide a stable synergistic insecticidal composition that promotes plant health and increases plant yield in the field.
[0027] It is another object of the present invention to provide a novel and effective stable synergistic insecticidal composition which is environmentally safe, possesses broad spectrum bio-efficacy, is non-phytotoxic.
[0028] It is another object of the present invention to provide a novel and effective stable synergistic insecticidal composition, which improves plant health and provides increased crop yield.
[0029] It is yet another object of the present invention to provide a novel and effective stable synergistic insecticidal composition, which has improved stability during the desired shelf life.
[0030] It is another objective of the present invention to provide a novel and effective stable synergistic insecticidal composition, which is economically more beneficial. Yet another object of the present invention is to provide a method of synergistic and efficacious control of broad spectrum of insect pests by using a stable synergistic insecticidal composition comprising A) Ethion or its agrochemically acceptable salts, esters and derivatives; B) Compound of Formula I, chemically known as 4-chloro-3-ethyl-l-methyl-N-[[4-(4- methylphenoxy)phenyl]methyl]-lH-pyrazole-5-carboxamide or its agrochemically acceptable salts, esters and derivatives; and C) Fluxametamide or its agrochemically acceptable salts, esters and derivatives.
[0031] Advantages of the present invention are as below: The stable synergistic insecticidal composition of the present invention shows:
[0032] • Broad spectrum activity against various insect-pests including but not limited to Diamond back moth, Aphids, Jassids,Thrips, Whitefly, Hoppers, Red spider mites, Purple mites, Yellowmite, Thrips, Scale, Bollworms, Pod borer, Girdle beetle & stemfly , Eeaf hopper, Thrips, Fruit borer, Shoot Borer, Spotted pod Borer, Tobacco caterpillar, Semi looper etc. including insects resistant to chemicals, and shows excellent controlling effects (synergistic controlling effects) which could never be expected from a single component alone.
[0033] • Also, it shows high plant insects controlling effects against existing insects resistant to chemicals, and no chemical damage against plants is observed.
[0034] • The insecticidal composition of present invention is useful for treatment of plants and crops including but not limited to Cabbage, Okra (Bhindi), Cotton, Cumin, Chilli, Mango, Onion, Tea, Gram, Pigeon pea or Redgram (Arhar / Tur), Soybean, Brinjal, Tomato etc.
[0035] SUMMARY OF THE INVENTION:
[0036] Accordingly, the present invention relates to a stable synergistic insecticidal composition comprising A) Ethion or its agrochemically acceptable salts, esters and derivatives; B) Compound of Formula I, i.e. 4-chloro-3-ethyl-l-methyl-N-[[4-(4-methylphenoxy)phenyl]methyl]-lH- pyrazole-5-carboxamide or its agrochemically acceptable salts, esters and derivatives; and C) Fluxametamide or its agrochemically acceptable salts, esters and derivatives. The present invention also relates to a process for preparation of such stable synergistic insecticidal composition for control of insect pests.
[0037] Insecticidal composition of the present invention is stable, safe to handle, environmentally safe and cost effective. The insecticides used in composition of the present invention act synergistically to cover broader spectrum of insect pests of crops.
[0038] In one embodiment, the present invention provides a stable synergistic insecticidal composition comprising bioactive amounts of:
[0039] A) Ethion or its agrochemically acceptable salts, esters and derivatives;
[0040] B) Compound of Formula I i.e. 4-chloro-3-ethyl-l-methyl-N-[[4-(4- methylphenoxy)phenyl]methyl]-lH-pyrazole-5-carboxamide or its agrochemically acceptable salts, esters and derivatives; and
[0041] C) Fluxametamide or its agrochemically acceptable salts, esters and derivatives.
[0042] In one embodiment, the present invention provides a stable synergistic insecticidal composition comprising bioactive amounts of:
[0043] A) Ethion or its agrochemically acceptable salts, esters and derivatives;
[0044] B) Compound of Formula I i.e. 4-chloro-3-ethyl-l-methyl-N-[[4-(4- methylphenoxy)phenyl]methyl]-lH-pyrazole-5-carboxamide or its agrochemically acceptable salts, esters and derivatives;
[0045] C) Fluxametamide or its agrochemically acceptable salts, esters and derivatives;
[0046] D) One or more agrochemically acceptable excipients.
[0047] In a preferred embodiment, the present invention provides a stable synergistic insecticidal composition comprising:
[0048] A) Ethion or its agrochemically acceptable salts, esters and derivatives, in the range of 0.1 to 90% by weight of the composition;
[0049] B) Compound of Formula I i.e. 4-chloro-3-ethyl-l-methyl-N-[[4-(4- methylphenoxy)phenyl]methyl]-lH-pyrazole-5-carboxamide or its agrochemically acceptable salts, esters and derivatives, in the range of 0.1 to 90% by weight of the composition; and C) Fluxametamide or its agrochemically acceptable salts, esters and derivatives, in the range of 0.1 to 90% by weight of the composition.
[0050] In a more preferred embodiment, the present invention provides a stable synergistic insecticidal composition comprising:
[0051] A) Ethion or its agrochemically acceptable salts, esters and derivatives, in the range of 0.1 to 65% by weight of the composition;
[0052] B) Compound of Formula I i.e. 4-chloro-3-ethyl-l-methyl-N-[[4-(4- methylphenoxy)phenyl]methyl]-lH-pyrazole-5-carboxamide in the range of 0.1 to 65% by weight of the composition; and
[0053] C) Fluxametamide or its agrochemically acceptable salts, esters and derivatives, in the range of 0.1 to 65% by weight of the composition.
[0054] In one another embodiment, the stable synergistic insecticidal composition of the present invention further comprises one or more agrochemically acceptable excipients.
[0055] In yet another embodiment, the present invention provides a method of improving plant health and increasing crop yield by using stable synergistic insecticidal composition comprising:
[0056] A) Ethion or its agrochemically acceptable salts, esters and derivatives;
[0057] B) Compound of Formula I i.e. 4-chloro-3-ethyl-l-methyl-N-[[4-(4- methylphenoxy)phenyl]methyl]-lH-pyrazole-5-carboxamide or its agrochemically acceptable salts, esters and derivatives; and
[0058] C) Fluxametamide or its agrochemically acceptable salts, esters and derivatives.
[0059] In yet another embodiment of the present invention, there is also provided a process for the preparation of stable synergistic insecticidal composition comprising
[0060] A) Ethion or its agrochemically acceptable salts, esters and derivatives;
[0061] B) Compound of Formula I i.e. 4-chloro-3-ethyl-l-methyl-N-[[4-(4- methylphenoxy)phenyl]methyl]-lH-pyrazole-5-carboxamide or its agrochemically acceptable salts, esters and derivatives; and
[0062] C) Fluxametamide or its agrochemically acceptable salts, esters and derivatives. In another embodiment, the synergistic insecticidal composition of the present invention controls various insects including their eggs or larvae in field crops, vegetables, fruits, oil seed and pulses, horticulture & forestry, veterinary, etc.
[0063] In yet another embodiment of the present invention, the present insecticidal composition can be applied to crops but not limited to Cabbage, Rice, Okra (Bhindi), Cotton, Cumin, Chilli, Mango, Onion, Tea, Gram, Pigeon pea or Redgram (Arhar / Tur), Soybean, Brinjal, Tomato etc.
[0064] In an embodiment of the present invention the present insecticidal composition can be applied as a foliar spray, soil drenching, seed dressing, application as paste of the targeted plants / trees, broadcasting, spraying, rubbing, atomizing, irrigating, evaporating, dusting, fogging, broadcasting, pouring, mist blowing, soil mixing, foaming, painting, spreading-on, drenching, dipping or drip irrigation etc.
[0065] In yet another embodiment of the present invention, the present stable synergistic insecticidal composition can be applied to various plants including but not limited to Paddy(Rice),, sugarcane, cotton, cabbage, cumin, mango, onion, gram, tomato, cauliflower, tomato, chilli, brinjal, okra (Bhindi), soybean, Tea, Red Gram (Arhar / Tur), Chickpea, Grapes, Maize, Pigeon Pea, Groundnut, Bengal Gram, Black gram, Cucumber, Grains Millet, Pulses Dry Fruits, Nuts Spices & Oil Seeds ,turf and forage, cruciferous, cucurbits, grapevines, pepper, fodder beet, oil seed rape, pansy etc
[0066] In one embodiment of the present invention, the present insecticidal composition is stable and has enhanced shelf life.
[0067] DETAILED DESCRIPTION OF THE INVENTION
[0068] In describing the embodiments of the invention, specific terminology is resorted for sake of clarity. However, it is not intended that the invention be limited to specific terms so selected and it is to be understood that each specific term includes all technical equivalents that operate in a similar manner to accomplish a similar purpose. Discussed below are some representative embodiments of the present invention. The invention in its broader aspects is not limited to the specific details and representative methods.
[0069] All technical and scientific terms used herein have the same meanings as commonly understood by someone ordinarily skilled in the art to which the present subject matter belongs.
[0070] The terminology used, in the present disclosure, is only for the purpose of explaining a particular embodiment and such terminology shall not be considered to limit the scope of the present disclosure.
[0071] Variations or modifications to the composition of this invention, within the scope of the invention, may occur to those skilled in the art upon reviewing the disclosure herein. Such variations or modifications are well within the spirit of this invention.
[0072] The expression of various quantities in terms of “% w / w” or “%” means the percentage by weight, relative to the weight of the total formulation or composition unless otherwise specified.
[0073] The term “active ingredient” (a.i.) or “active agent” used herein refers to that component of the composition responsible for control and killing of pest.
[0074] The terms “plants” and “vegetation” include, but are not limited to, germinant seeds, emerging seedlings, plants emerging from vegetative propagules, and established vegetation.
[0075] The term “crop” shall include a multitude of desired crop plants or an individual crop plant growing at a locus.
[0076] The term “synergistic”, as used herein, refers to the combined action of two or more active agents blended together and administered conjointly that is greater than the sum of their individual effects.
[0077] “Bioactive amounts” as mentioned herein means that amount which, when applied for treatment of crops, is sufficient to give effect in such treatment.
[0078] The term “control” means to inhibit the ability of insect pests to survive, grow, feed and / or reproduce, or to limit the insect pests’ related damage or loss in crop plants. To “control” insect pests may or may not mean killing the insects although, it preferably means killing the insect pests. The term “health of a plant” or “plant health” is defined as a condition of the plant and / or its products. As a result of the improved health; yield, plant vigour, quality and tolerance to abiotic or biotic stress is increased. As a result, the health of a plant is increased even in the absence of pest pressure.
[0079] Accordingly, in an especially preferred embodiment according to the invention, the health of a plant is increased both in the presence and absence of biotic or abiotic stress factors. The above identified indicators for the health condition of a plant may be interdependent or they may result from each other. An increase in plant vigor may for example result in an increased yield and / or tolerance to abiotic or biotic stress.
[0080] One indicator for the condition of the plant is the yield. “Yield” is to be understood as any plant product of economic value that is produced by the plant such as grains, fruits, vegetables, nuts, grains, seeds, wood (e.g. in the case of silviculture plants) or even flowers (e.g. in the case of gardening plants, ornamentals). The plant products may in addition be further utilized and / or processed after harvesting.
[0081] In an especially preferred embodiment of the invention, the yield of the treated plant is increased.
[0082] In another preferred embodiment of the invention, the yield of the plants treated according to the method of the invention, is increased synergistically.
[0083] According to the present invention, “increased yield” of a plant, in particular of an agricultural, silvicultural and / or horticultural plant means that the yield of a product of the respective plant is increased by a measurable amount over the yield of the same product of the plant produced under the same conditions, but without the application of the composition according to the invention.
[0084] In another especially preferred embodiment of the invention, the plant vigour of the treated plant is increased. In another preferred embodiment of the invention, the plant vigour of the plants treated according to the composition of the present invention is increased synergistically.
[0085] Another indicator for the condition of the plant is the “quality” of a plant and / or its products.
[0086] In an especially preferred embodiment of the invention, the quality of the treated plant is increased.
[0087] In another preferred embodiment of the invention, the quality of the plants treated according to the method of the invention, is increased synergistically. The present invention includes within its scope, all possible salts, esters and derivatives of the active ingredients of the composition.
[0088] It has been observed by the inventors of the present invention that the composition of present invention not only has enhances bio-efficacy and provides synergistic effect but also gives control of insects for a longer duration as compared to solo and binary formulations of insecticides.
[0089] In one another embodiment of the present invention, stable synergistic insecticidal composition comprises:
[0090] A) Ethion or its agrochemically acceptable salts, esters and derivatives;
[0091] B) Compound of Formula I i.e. 4-chloro-3-ethyl-l-methyl-N-[[4-(4- methylphenoxy)phenyl]methyl]-lH-pyrazole-5-carboxamide or its agrochemically acceptable salts, esters and derivatives; and
[0092] C) Fluxametamide or its agrochemically acceptable salts, esters and derivatives.
[0093] In one another embodiment of the present invention, stable synergistic insecticidal composition comprises:
[0094] A) Ethion or its agrochemically acceptable salts, esters and derivatives;
[0095] B) Compound of Formula I i.e. 4-chloro-3-ethyl-l-methyl-N-[[4-(4- methylphenoxy)phenyl]methyl]-lH-pyrazole-5-carboxamide or its agrochemically acceptable salts, esters and derivatives;
[0096] C) Fluxametamide or its agrochemically acceptable salts, esters and derivatives; and
[0097] D) One or more agrochemically acceptable excipients.
[0098] In a preferred embodiment, the present invention provides a stable synergistic insecticidal composition comprising:
[0099] A) Ethion or its agrochemically acceptable salts, esters and derivatives, in the range of 0.1 to 90% by weight of the composition;
[0100] B) Compound of Formula I i.e. 4-chloro-3-ethyl-l-methyl-N-[[4-(4- methylphenoxy)phenyl]methyl]-lH-pyrazole-5-carboxamide or its agrochemically acceptable salts, esters and derivatives, in the range of 0.1 to 90% by weight of the composition; and C) Fluxametamide or its agrochemically acceptable salts, esters and derivatives, in the range of 0.1 to 90% by weight of the composition.
[0101] In a more preferred embodiment, the present invention provides a stable synergistic insecticidal composition comprising:
[0102] A) Ethion or its agrochemically acceptable salts, esters and derivatives, in the range of 0.1 to 65% by weight of the composition;
[0103] B) Compound of Formula I i.e. 4-chloro-3-ethyl-l-methyl-N-[[4-(4- methylphenoxy)phenyl]methyl]-lH-pyrazole-5-carboxamide in the range of 0.1 to 65% by weight of the composition; and
[0104] C) Fluxametamide or its agrochemically acceptable salts, esters and derivatives, in the range of 0.1 to 65% by weight of the composition.
[0105] In yet another embodiment, the present invention provides a method of improving plant health and increasing crop yield by using stable synergistic insecticidal composition comprising:
[0106] A) Ethion or its agrochemically acceptable salts, esters and derivatives;
[0107] B) Compound of Formula I i.e. 4-chloro-3-ethyl-l-methyl-N-[[4-(4- methylphenoxy)phenyl]methyl]-lH-pyrazole-5-carboxamide or its agrochemically acceptable salts, esters and derivatives; and
[0108] C) Fluxametamide or its agrochemically acceptable salts, esters and derivatives.
[0109] According to another embodiment of the present invention, there is also a process provided for the preparation of stable synergistic insecticidal composition comprising
[0110] A) Ethion or its agrochemically acceptable salts, esters and derivatives;
[0111] B) Compound of Formula I i.e. 4-chloro-3-ethyl-l-methyl-N-[[4-(4- methylphenoxy)phenyl]methyl]-lH-pyrazole-5-carboxamide or its agrochemically acceptable salts, esters and derivatives; and
[0112] C) Fluxametamide or its agrochemically acceptable salts, esters and derivatives.
[0113] In accordance with an embodiment of the present invention, there is provided a synergistic insecticidal composition comprising active ingredients present in the weight % range as given below:
[0114] In an embodiment, the stable synergistic insecticidal composition further comprises one or more agrochemically acceptable excipients.
[0115] In another embodiment, “agrochemically acceptable excipients” are substances used in agrochemical formulation that are compatible with the active substance and do not negatively impact the efficacy or safety of the active ingredient and do not pose any risk to the environment and health of non-target organisms.
[0116] In an embodiment, the present invention provides a kit-of-parts comprising a plurality of components, wherein said plurality of components comprises:
[0117] A) Ethion or its agrochemically acceptable salts, esters and derivatives;
[0118] B) Compound of Formula I i.e. 4-chloro-3-ethyl-l-methyl-N-[[4-(4- methylphenoxy)phenyl]methyl]-lH-pyrazole-5-carboxamide or its agrochemically acceptable salts, esters and derivatives; and
[0119] C) Fluxametamide or its agrochemically acceptable salts, esters and derivatives.
[0120] In another embodiment of the present invention, the present synergistic insecticidal composition can be used against various insect-pests including but not limited to Diamond back moth, Aphids, Jassids, Whitefly, Hoppers, Red spider mites, Purple mites, Yellow mite, Thrips, Scale, Bollworms, Pod borer, Fruit borer (Helicoverpa armigera), Girdle beetle & stemfly , Eeaf hopper, Thrips (Scirtothrips dorsalis), Fruit borer, Shoot Borer, Spotted pod Borer, Tobacco caterpillar, Semi looper etc. In yet another embodiment of the present invention, the present stable synergistic insecticidal composition can be applied to various plants including but not limited to Paddy(Rice),, sugarcane, cotton, cabbage, cumin, mango, onion, gram, tomato, cauliflower, tomato, chilli, brinjal, okra (Bhindi), soybean, Tea, Red Gram (Arhar / Tur), Chickpea, Grapes, Maize, Pigeon Pea, Groundnut, Bengal Gram, Black gram, Cucumber, Grains Millet, Pulses Dry Fruits, Nuts Spices & Oil Seeds ,turf and forage, cruciferous, cucurbits, grapevines, pepper, fodder beet, oil seed rape, pansy etc
[0121] In another embodiment of the present invention, the stable synergistic insecticidal composition of the present invention further comprises one or more agrochemically acceptable excipients including but not limited to the group comprising surfactant(s), dispersing agent(s), codispersants), anti-freezing agent(s), emulsifier(s), anti-foaming agent / defoamer(s), wetting agent(s), antimicrobial / anti-bacterial agent(s), thickening agent / thickener(s), quick coating agent(s) or sticking agents / sticker(s), spreader(s), binder(s), pH-adjusting agent(s), anti-caking agent(s), adjuvant(s), filler(s) / suspension aid(s), colorant(s), carrier(s), buffering agent(s), polymer(s), rheology modifier(s), solvent(s), co-solvent(s) or a combination thereof. Additional components may also be included, e.g., protective colloids, carriers, adhesives, thixotropic agents, penetration agents, stabilisers, sequestering agents. More generally, the active materials can be combined with any solid or liquid carrier / additive, which complies with usual formulation techniques.
[0122] An adjuvant used in the present invention is any material that is added to an agrochemical formulation to enhance or modify the performance of the formulation. An adjuvants used in the present invention to make it a safer to ecological environmental, having low toxicity and having no phytotoxicity effects on any part of the plant.
[0123] Examples of surfactant or dispersing agent and co-dispersant used herein include but not limited to polymeric anionic dispersant, polyarylphenyl ether phosphate, tristyryl phenol ethoxylate, Polymethyl methacrylate -polyethylene glycol graft copolymer, acrylate copolymer, acrylic graft copolymer, non-ionic proprietary surfactant, ethoxylated tristryl phenol Sulphate, alkyl naphthalene formaldehyde condensate , naphthalene sulfonic acid, phenol sulphonic acid, Mixture of Salt of Naphthalene Sulphonic Acid And Phenol Sulphonic Acid Condensation Product, Sodium Alkylnaphthalene Sulfonate Formaldehyde Condensate, sodium salt condensate with formaldehyde, ethoxylated oleyl cetyl alcohol, polyalkelene glycol ether, ethoxylated fatty alcohol, Sodium polymethyl methacrylate, sodium poly aery late, sodium lignosulphonate, calcium lignosulphonate, alkylphenol polyoxyethylene ether, sodium salt of naphthalene sulfonate condensate, polycarboxylate, Sodium Polycarboxylate, fatty alcohol polyoxyethylene ether, alcohol poly glycol ether or mixtures thereof and present in the range of 0.1-20% by weight of the composition.
[0124] Examples of wetting agent used herein include but not limited to tristyrylphenol ethoxylate nonionic emulsifier, mixture of non-ionic surfactants, alkoxylated alcohol, block copolymer, alcohol polyglycol ether, alkyl olefin sulphates, dioctyl sulpho succinate, alkyl naphthalene sulphate biisopropyl Napthalene sulphonate or its sodium salt, Polyalkoxy ethers, alkyl phenol ethoxylates, tri-styrenated phenol ethoxylate, EO / PO block co-polymers, butyl polyalkylene oxide block copolymer, sodium lauryl sulphate, sodium ligno sulphates or mixtures thereof and present in the range of 0.1-20% by weight of the total composition.
[0125] Examples of defoamer or antifoaming agent used herein include but not limited to silicon emulsion based anti-foam agents, Siloxane poly alkyleneoxide, Polydimethylsiloxane, trisiloxane ethoxylates, silicone oil, silicone compound, C10~C20 saturated fat acid compounds or C8~C10 aliphatic alcohols compound, vegetable oil based antifoam, tallow based fatty acids, polyalkyleneoxide polydimethylsiloxane emulsion and mixtures thereof and present in the range of 0.01-5.0 % by weight of the composition.
[0126] Examples of anti-freezing agent used herein include but not limited to glycol, propylene glycol, mono ethylene glycol, glycerine, diethylene glycol, sorbitol, urea, mannitol, polyethylene glycol or mixtures thereof and present in the range of 1.0-20% by weight of the composition.
[0127] Examples of fillers used herein include but not limited to silicon dioxide, china-clay, kaolin, starch, bentonite, precipitated silica, fumed silica, talcum powder, lactose, ammonium sulphate, water, sodium Sulphate, magnesium sulphate, sodium citrate, sodium chloride, potassium chloride and mixtures thereof and present in the range of 5-60 % by weight of the composition. Examples of anti -caking agent used herein include but not limited to group of talc, silica powder, hydrous magnesium silicate, magnesium carbonate, calcium carbonate, precipitate silica, hydrophobic fumed silica and mixtures thereof and present in the range of 2.0-20% by weight of the composition.
[0128] Examples of carrier used herein include but not limited to silicon dioxide, china clay, kaolin, starch, bentonite, precipitated silica, fumed silica, talcum powder, lactose, ammonium sulpha or mixture there of present in the range of 1.0-45 % by weight of the composition.
[0129] Examples of biocide or anti-microbial agent used herein include but not limited to 1, 2,- Benzisothiazolin -3-one, blends of 1,2,- benzisothiazolin-3-one and 2-methyl-4-isothiazolin-3- one, 5-chloro-2-methyl-4-isothiazolin-3-one, blends of 5-chloro-2-methyl-4-isothiazolin-3-one and 2-methyl-4-isothiazolin-3-one, zinc l-hydroxy-2(lH)-pyridinethione, blends of zinc 1- hydroxy-2(lH)-pyridinethione and zinc oxide, and 2-n-octyl-4- isothiazolin-3-one or mixture thereof and present in the range of 0.01 to 10 % by weight of the composition.
[0130] Examples of rheology modifier used herein include but not limited to polysaccharides, carboxymethyl cellulose, bentonite clay, aluminium magnesium silicate, hydroxy propyl cellulose, xanthan gum, gum arabic, gaur gum, carbomer, chitosan, precipitated silica or mixtures thereof and present in the range of 0.01-5.0 % by weight of the composition.
[0131] Examples of emulsifier(s) used herein include but not limited to araliphatic or aliphatic non-ionic emulsifier such as ethoxylated mono-, di- and trialkylphenols, ethoxylates of long-chain alcohols and polyethylene oxide / polypropylene oxide homo- and copolymers, EO / PO block copolymers, polymeric emulsifier, Ethoxylates of long-chain alkanols, Castor oil ethoxylate 40 mole , ethoxylated monoalkylphenol, ethoxylates of cetyl alcohol and / or stearyl alcohol ; Tristyrylphenol ethoxylate-20 mole, Ethoxylated Tristyrylphenol ,and Anionic emulsifier such as alkali metal and ammonium salts of alkyl sulfates, of hemisulfates of ethoxylated alkanols and ethoxylated alkylphenols, alkylsulfonic acids, bis(phenylsulfonic acid) ethers and their alkali metal or ammonium salts, sodiumlaurylsulfate, sodium (cetyl / stearyl) sulfate, blend of anionic an non-ionic or mixture thereof and present in the range of 0.01 -20 % by weight of the composition Examples of solvent(s) and co-solvent(s) used herein include but not limited to polar and nonpolar solvent from the group comprising heavy aromatic hydrocarbon, N methyl pyrollidone (NMP) , Solvent Naphtha (Solvent C-9), Di methyl sulfoxide (DMSO), Dimethylformamide (DMF), N- alcohol, 2-ethyl hexanol , alkyl amide, vegetable oil, mineral oil, distilled water, aromatic solvents, water or mixtures thereof and present in the range of 1.0 to 20 % by weight of the composition.
[0132] Examples of polymer(s) used herein include but not limited to isocyanate, polyisocyanate used is toluene -2, 4-diisocyanate (TDI), diethylenetriamine (DETA), ethylene diamine (EDA), triethylenetetramine (TETA), and / or hexamethylene diamine (HMDA), diethanolglycine sodium salt, ethanoldiglycine disodium salt, hydroxymonocarboxylic acid compounds, hydroxydicarboxylic acid compounds, tetrasodium N,N-bis(carboxylatomethyl)-L-glutamate (GLDA), methylene diisocyanate (MDI), and / or low molecular weight polydiisocynates present in the range of 0.01- 5.0 % by weight of the composition.
[0133] In an embodiment, the kit-of-parts comprises an instructions manual, said instructions manual comprising instructions directing a user to admix the components before being used.
[0134] The composition of the present invention is effective in controlling broad spectrum of insect but not limited to Diamond back moth, Aphids, Jassids,Thrips, Whitefly, Hoppers, Red spider mites, Purple mites, Yellowmite, Scale, Bollworms, Pod borer, Girdle beetle & stemfly , Leaf hopper, Thrips (Scirtothrips dorsalis), Fruit borer (Helicoverpa armigera) , Shoot Borer, Spotted pod Borer, Tobacco caterpillar, Semi looper etc. including insects resistant to chemicals, and shows excellent controlling effects (synergistic controlling effects) which could never be expected from a single component alone.
[0135] The composition of the present invention can also comprise or may be applied together and / or sequentially with further active compounds. These further compounds can be selected from fertilizers or micronutrient donors or microorganisms or other preparations that influence plant growth, such as inoculants (e.g. a strain of nitrogen-fixing bacteria), and plant inducers.
[0136] In yet another embodiment, the composition according to the invention can be applied to any and all developmental stages of insect pests, such as egg, nymph, larva, pupa, and adult. The insect pests may be controlled by contacting the target insect pest, habitat, breeding ground or its locus with a bioactive amount of the novel and inventive composition of the present invention.
[0137] In yet another embodiment of the present invention, the insecticidal composition is formulated as but not limited to 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), Microemulsion (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) suspension, Tablet (TB), Ultra-low volume (ULV) liquid, Water dispersible granules (WG), Wettable powder (WP), Water dispersible powder for slurry seed treatment (WS), Water dispersible tablet (WT), a mixed composition of CS and SC (ZC) or a mixed composition of CS and SE (ZE) or a mixed composition of CS and EW (ZW).
[0138] In yet another preferred embodiment of the present invention, the present stable synergistic insecticidal composition can be formulated as Suspo-emulsion (SE) and Emulsifiable Concentrate (EC)
[0139] In yet another embodiment of the present invention, the invention further provides the process for preparation of the said insecticidal composition wherein, the said composition can be one or more of 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), Oildispersion (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) suspension, Tablet (TB), Ultra-low volume (ULV) liquid, Water dispersible granules (WG), Wettable powder (WP), Water dispersible powder for slurry seed treatment (WS), Water dispersible tablet (WT), a mixed composition of CS and SC (ZC) or a mixed composition of CS and SE (ZE) or a mixed composition of CS and EW (ZW).
[0140] In an embodiment, the present invention provides that the use of said composition promotes plant health, growth and thus increases plant yield in the field.
[0141] In one embodiment, the composition according to the present invention acts synergistically to control insect pests in various crops, plants.
[0142] The composition of the present invention also provides control of diseases caused by a broad spectrum of insect plant pathogens preventatively or curatively by applying an effective amount of the composition either pre-or post-infection.
[0143] Plant disease control is ordinarily accomplished by applying an effective amount of a synergistic composition of the present invention either pre-or post-infection, to the portion of the plant to be protected such as the roots, stems, foliage, fruit, seeds, tubers or bulbs, or to the media (soil or sand) in which the plants to be protected are growing. The composition can also be applied to the seed to protect the seed and seedling.
[0144] Through the insecticidal composition of present invention, the number of applications to control wide range of insect pests appearing at the same time is minimised. The composition of present invention is highly safe to the user and to the environment. The composition offers the user a single homogenous application eliminating the need for tank mix. The composition also is cost-effective as it provides much greater simultaneous control and can be used in a variety of crops with a broader spectrum of protection.
[0145] The process for preparing the present novel synergistic composition can be modified accordingly by any person skilled in the art based on the knowledge of the manufacturing the formulation. However, all such variation and modification are still covered by the scope of present invention. Thus, before describing the present invention in detail, it is to be understood that this invention is not limited to particularly exemplified systems or process parameters that may of course, vary. It is also to be understood that the terminology used herein is for the purpose of describing particular embodiments of the invention only and is not intended to limit the scope of the invention in any manner. The use of examples anywhere in this specification including examples of any terms discussed herein is illustrative only, and in no way limits the scope and meaning of the invention or of any exemplified term. Likewise, the invention is not limited to various embodiments given in this specification.
[0146] Unless otherwise defined, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this invention pertains. In the case of conflict, the present document, including definitions will control.
[0147] Representative examples of the present composition of this invention is provided below and is not to be construed as limiting in any manner:
[0148] Compound of Formula I, pertains to 4-chloro-3-ethyl-l-methyl-N-[[4-(4- methylphenoxy)phenyl]methyl]-lH-pyrazole-5-carboxamide or its agrochemically acceptable salts, esters and derivatives;
[0149] Examples: General recipe:
[0150] Example 1. Ethion 38% + Compound of formula I 11.2% + Fluxametamide 2.8% EC
[0151] CHEMICAL COMPOSITION;
[0152] FORMULATION PROCESS
[0153] 1. Into a clean and dry reactor charged the solvent C-9 and started stirring.
[0154] 2. To the above, added Dimethylformamide (DMF) and mixed well. 3. Added technical Fluxametamide, technical Compound of formula I and technical
[0155] Ethion. Mixed well to dissolve and get the clear solution.
[0156] 4. Then to the above, added Emulsifier (Blend of Anionic and Non-ionic) and mixed well to form an emulsifiable concentrate.
[0157] 5. Filtered this solution through sparkler filter and collect the filtrate into another clean and dry vessel.
[0158] 6. Packed the formulation in QA approved containers.
[0159] STABILITY DATA: Ethion 38% + Compound of formula I 11.2% + Fluxametamide 2.8% EC
[0160] Example 2. Ethion 38% + Compound of formula I 11.2% + Fluxametamide 2.8% SE
[0161] CHEMICAL COMPOSITION
[0162] FORMULATION PROCESS:
[0163] A. Preparation of EW
[0164] 1. Mixed Solvent C-9 and Ethion technical to prepare a organic phase.
[0165] 2. In another vessel mixed DM water and Emulsifier (Blend of anionic & Non-ionic) to prepare aqueous phase.
[0166] 3. Mixed the two phases to prepare the EW part.
[0167] B.Preparation of SC
[0168] 1. Mixed DM water, l,2-Benzisothiazolin-3-one, Polydimethylsiloxane emulsion, Propylene Glycol, Sodium lauryl sulphate, Mixture of Salt of Naphthalene Sulphonic Acid and Phenol Sulphonic Acid Condensation Product, Compound of formula I technical and Fluxametamide technical.
[0169] 2. Milled this slurry to achieve particle size of D90 less than 10 micron.
[0170] C. Preparation of SE
[0171] 1. Mixed the two parts i.e., EW and SC part.
[0172] 2. Added xanthum gum and mixed well to prepare SE formulation
[0173] STABILITY DATA:_Ethion 38% + Compound of formula I 11.2% + Fluxametamide 2.8% SE
[0174] Evaluation of synergistic effect of insecticidal composition of the present invention
[0175] A synergistic effect of two or more products exists whenever the action of an active ingredient composition is greater than the sum of the actions of the individual components. Synergism was calculated by using Colby’s method (Weeds, vol. 15 No. 1 (Jan 1967), pp. 20-2.
[0176] The synergistic action expected for a given composition of two active components can be calculated as follows: XY
[0177] E = (X + Y) -
[0178] 100 The synergistic action expected for a given composition of three active components can be calculated as follows:
[0179] (XY+YZ+XZ) (XYZ)
[0180] E = (X + Y + Z) - - + -
[0181] 100 10000
[0182] Where:
[0183] E represents expected percentage of insecticidal control for the composition of the two or three actives ingredients at defined doses (for example equal to x, y and z, respectively).
[0184] X is the percentage of insecticidal control observed by the compound (Ethion) at a defined dose (equal to x).
[0185] Y is the percentage of insecticidal control observed by the compound (Compound of formula I) at a defined dose (equal to y).
[0186] Z is the percentage of insecticidal control observed by the compound (Fluxametamide) at a defined dose (equal to z).
[0187] When the percentage of insecticidal control observed for the composition is greater than the expected percentage, there is a synergism effect.
[0188] Observed control (%) Ratio = -
[0189] Expected control (%)
[0190] Ratio of O / E > 1, synergism observed
[0191] The present invention is illustrated by way of examples, the examples are meant for illustrative purposes and should not be construed as limiting.
[0192] Experiment for Synergistic activity of composition product of present invention:
[0193] Example 1- Details of experiment on Chilli crop:
[0194] Field experiment for synergistic activity of Ethion, Compound of formula I and Fluxametamide for the control of Fruit borer and Thrips pests on chilli crop was conducted. To evaluate the synergistic effect, Chilli (Variety: Kashi Anmol) crop was sown in 5 m x 5 m plots maintaining 45 cm x 45 cm plant distance with three replications and in Randomized Block Design (RBD). The treatments were applied as foliar application at the ETL level of insect population. Each active component was applied at recommended doses in different ternary and binary compositions. Solo compositions were also taken for comparison. The treatment details are as under:
[0195] The treatments T1 to T28 were used as foliar application whereas no treatment was done for T29 control treatment. Observations for Fruit borer (Helicoverpa armigera) and Thrips (Scirtothrips dorsalis) were recorded at Before spray, 7 and 15 days after sprays by observing 5 random plants per plot and based on number of larval population and reduction over control was calculated. The observations for Thrips (Scirtothrips dorsalis) were recorded at Before spray, 7 and 15 days after sprays was recorded on random 5 plants per 5 leaves (2 upper 2 middle and 1 lower leaves) per plant in each replication, thrips per cent control was calculated over control. Based on the per cent reduction in fruit borer larval population and thrips population the Expected control was calculated and compared with Observed control. The results of the trial have been presented here under in Table 1.
[0196] Table 1: Synergistic effect of composition product of the present invention (Ethion +Compound of formula I +Fluxametamide) against Fruit borer and thrips in Chilli crop
[0197]
[0198] It is clearly evident from the data shown in above Table 1 for per cent control fruit borer larval and thrips population in Chilli crop that the ternary composition of the present invention comprising Ethion + Compound of formula I + Fluxametamide T1 to T4 are synergistic for both Insect-pest control with > 1 Colby’s Ratio. The binary composition of two insecticide (Ethion +Compound of formula I, Ethion + Fluxametamide and Compound of formula I + Fluxametamide) T5 to T16 were compatible but no synergistic effect was observed for the control of fruit borer and thrips. All solo products and market samples were also less effective for the control of both insect -pest as compared to ternary composition of the present invention.
[0199] Experiment for Bio-efficacy evaluation of composition product of present invention:
[0200] For the ternary and binary compositions, based on Ethion, Compound of formula I and Fluxametamide evaluation under field conditions, the basic test composition as Ethion, Compound of formula I and Fluxametamide were manufactured specifically by the inventor. For ternary composition, Ethion 38% + Compound of formula I 11.2% + Fluxametamide 2.8% EC was used and for binary compositions, Ethion 38% + Compound of formula I 11.2% EC, Ethion 38% + Fluxametamide 2.8% EC and Compound of formula I 11.2% + Fluxametamide 2.8% EC and solo formulations of Ethion 38%, Compound of formula I 11.2% and Fluxametamide 2.8% EC were used. The market samples Ethion 50 % EC, Compound of formula 1 15% EC and Fluxametamide 10% EC were used for comparison.
[0201] Example 3: Evaluation of the composition product of the present invention on Chilli crop. The synergistic composition of the present invention Ethion 38% + Compound of formula 1 11.2% + Fluxametamide 2.8% EC was evaluated on Chilli crop. The experiment plots are design in Randomized Block Design (RBD) with three replications maintaining a distance of 45 cm x 45 cm between plants and rows.
[0202] The observations were recorded for the following objectives.
[0203] Objectives:
[0204] 1. Bio-efficacy evaluation against fruit borer on Chilli crop
[0205] 2. Bio-efficacy evaluation against thrips on Chilli crop 3. Bio-efficacy evaluation based on per cent reduction in fruit borer larval population over control.
[0206] 4. Bio-efficacy evaluation based on percent reduction in thrips population.
[0207] 5. Bio-efficacy evaluation based on crop yield and percent increase over control.
[0208] 6. Phytotoxicity evaluation on Chilli crop Treatment details:
[0209] Methodology:
[0210] The treatments T1 to T18 and T20 were used as foliar application whereas no treatment was done for T19 untreated control plots. The treatments were applied as foliar application at the ETL level of insect population. Each active component was applied at three doses in different ternary and binary compositions. Solo compositions were also taken for comparison.
[0211] Observations for Fruit borer (Helicoverpa armigera) and Thrips (Scirtothrips dorsalis) were recorded at Before spray, 7 and 15 days after sprays by observing 5 random plants per plot and based on number larval population of fruit borer and reduction over control was calculated. The observations for Thrips (Scirtothrips dorsalis) were recorded at Before spray, 7 and 15 days after sprays was recorded on 5 plants per 5 leaves (2 upper 2 middle and 1 lower leaf) per plant in each replication. Thrips per cent control was calculated over control. The green chilli yield was recorded at different picking as per harvest. The observations for natural enemies in crop ecosystem at Before, 7 and 15 days after crop sowing and phytotoxicity to Chilli crop at 0, 3, 7, 10 & 15 days after spray were also recorded. Results are presented in Table 3, 4, 5 and 6.
[0212] Results:
[0213] Table 3: Field bio-efficacy evaluation of Ethion 38% + Compound of formula 1 11.2% +
[0214] Fluxametamide 2.8% EC against Fruit borer of chilli crop
[0215] DAS - Days after spray
[0216] Table 4: Field bio-efficacy evaluation of Ethion 38% + Compound of formula 1 11.2% + Fluxametamide 2.8% EC against Thrips of chilli crop.
[0217] DAS - Days after spray
[0218] Table 5: Field bio-efficacy evaluation of Ethion 38% + Compound of formula 1 11.2% + Fluxametamide 2.8% EC based on yield of chilli crop.
[0219] Table 6: Phytotoxicity evaluation of Ethion 38% + Compound of formula I 11.2% + Fluxametamide 2.8% EC on Chilli crop.
[0220] From the example, it can be clearly seen that the ternary composition of the present invention is superior for controlling the Fruit borer (Helicoverpa armigera) at 7 and 15 days after spray (Table 3) and for controlling thrips (Scirtothrips dorsalis) at 7 and 15 days after spray (Table 4) in Chilli crop as compared to the binary and solo compositions at same dosage levels. Other registered formulated products available in the market, Ethion 50 % EC, Compound of formula I 15% EC and Fluxametamide 10% EC were also evaluated in terms of effectiveness but observed to be less effective as compared to ternary composition of the present invention. The yield of Chilli crop also improved in the ternary composition of Ethion 38% + Compound of formula I 11.2% + Fluxametamide 2.8% EC as compared to binary and solo compositions (Table 5). One of the reasons of higher green chilli yield may be due to better control of both insect pest.
[0221] The disclosed composition Ethion 38% + Compound of formula I 11.2% + Fluxametamide 2.8% EC @ 937.5 ml, 1250 ml and 2500 ml / ha further showed no phytotoxicity in the Chilli crop even after 0, 3, 5, 7, 10 and 15 days after spray (Table 6).
[0222] In particular, it has now been found, surprisingly that, for example, the insecticidal activity of the composition of present invention, compared with the insecticidal activity of individual components, is synergistic. In fact, various advantageous properties associated with the compositions according to the invention, include but are not limited to: knock down effect on insect pests at all developmental stages, with no phytotoxicity and enhanced shelf life, stability of the composition. From the above investigations, it will be observed that numerous modifications and variations can be effectuated without departing from the true spirit and scope of the novel concepts of the present invention. It is to be understood that no limitations with respect to the specific embodiments illustrated is intended or should be inferred. It should be understood that all such modifications and improvements have been deleted herein for the sake of conciseness and readability but are properly within the scope of the following claims.
Claims
I CLAIM:
1. . A stable synergistic insecticidal composition comprising:A) Ethion or its agrochemically acceptable salts, esters and derivatives;B) Compound of Formula I i.e. 4-chloro-3-ethyl-l-methyl-N-[[4-(4- methylphenoxy)phenyl] methyl] -lH-pyrazole-5 -carboxamide or its agrochemically acceptable salts, esters and derivatives; andC) Fluxametamide or its agrochemically acceptable salts, esters and derivatives.[CEAIM 2]. The stable synergistic insecticidal composition as claimed in claim 1, comprising:A) Ethion or its agrochemically acceptable salts, esters and derivatives, in the range of 0.1 to 90% by weight of the composition;B) Compound of Formula I i.e. 4-chloro-3-ethyl-l-methyl-N-[[4-(4- methylphenoxy)phenyl]methyl]-lH-pyrazole-5-carboxamide or its agrochemically acceptable salts, esters and derivatives, in the range of 0.1 to 90% by weight of the composition; andC) Fluxametamide or its agrochemically acceptable salts, esters and derivatives, in the range of 0.1 to 90% by weight of the composition.[CEAIM 3]. The insecticidal composition as claimed in claims 1 to 2, which further comprises one or more agrochemically acceptable excipients.[CEAIM 4]. The insecticidal composition as claimed in claim 3, wherein agrochemically acceptable excipients comprises surfactant(s), dispersing agent(s), co-dispersant, anti-freezing agent(s), emulsifier(s)( (anionic and non-ionic), anti-foaming agent / defoamer(s), wetting agent(s), antimicrobial / anti-bacterial agent(s), anti-caking agent , thickening agent / thickener(s), quick coating agent(s) or sticking agents / sticker(s), spreader(s), binder(s), pH-adjusting agent(s), anticaking agent(s), adjuvant(s), filler(s) / suspension aid(s), colorant(s), carrier(s), buffering agent(s), polymer(s), rheology modifier(s), solvent(s), co-solvent(s) , biocide or mixtures thereof.[CEAIM 5]. The composition as claimed in claim 4, wherein the surfactant(s) and / or dispersing agent and / or co-dispersant is / are selected from the group comprising polymeric anionic dispersant,polyarylphenyl ether phosphate, tristyryl phenol ethoxylate, Polymethyl methacrylatepolyethylene glycol graft copolymer, acrylate copolymer, acrylic graft copolymer, non -ionic proprietary surfactant, ethoxylated tristryl phenol Sulphate, alkyl naphthalene formaldehyde condensate , naphthalene sulfonic acid, phenol sulphonic acid, Mixture of Salt of Naphthalene Sulphonic Acid And Phenol Sulphonic Acid Condensation Product, Sodium Alkylnaphthalene Sulfonate Formaldehyde Condensate, sodium salt condensate with formaldehyde, ethoxylated oleyl cetyl alcohol, polyalkelene glycol ether, ethoxylated fatty alcohol, Sodium polymethyl methacrylate, sodium polyacrylate, sodium lignosulphonate, calcium lignosulphonate, alkylphenol polyoxyethylene ether, sodium salt of naphthalene sulfonate condensate, polycarboxylate, Sodium Polycarboxylate, fatty alcohol polyoxyethylene ether, alcohol polyglycol ether or mixtures thereof and present in the range of 0.1-20% by weight of the composition.
6. . The insecticidal composition as claimed in claim 4, wherein the wetting agent is / are selected form the group comprising tristyrylphenol ethoxylate non-ionic emulsifier, mixture of non-ionic surfactants, alkoxylated alcohol, block copolymer, alcohol polyglycol ether, alkyl olefin sulphates, dioctyl sulpho succinate, alkyl naphthalene sulphate , Di-isopropyl Napthalene sulphonate or its sodium salt, Polyalkoxy ethers, alkyl phenol ethoxylates, tri-styrenated phenol ethoxylate, EO / PO block co-polymers, butyl polyalkylene oxide block copolymer, sodium lauryl sulphate, sodium ligno sulphates or mixtures thereof and present in the range of 0.1 -20% by weight of the total composition.
7. . The insecticidal composition as claimed in claim 4, wherein the defoamer or antifoaming agent is / are selected from the group comprising silicon emulsion based anti -foam agents, Siloxane poly alkyleneoxide, Polydimethylsiloxane, trisiloxane ethoxylates, silicone oil, silicone compound, C10~C20 saturated fat acid compounds or C8~C10 aliphatic alcohols compound, vegetable oil based antifoam, tallow based fatty acids, polyalkyleneoxide polydimethylsiloxane emulsion and mixtures thereof and present in the range of 0.01-5.0 % by weight of the composition.
8. . The insecticidal composition as claimed in claim 4, wherein the anti -freezing agent is / are selected from the group comprising glycol, propylene glycol, mono ethylene glycol,glycerine, diethylene glycol, sorbitol, urea, mannitol, polyethylene glycol or mixtures thereof and present in the range of 1.0-20% by weight of the composition.
9. The insecticidal composition as claimed in claim 4, wherein the filler is / are selected from the group comprising silicon dioxide, china-clay, kaolin, starch, bentonite, precipitated silica, fumed silica, talcum powder, lactose, ammonium sulphate, water, sodium Sulphate, magnesium sulphate, sodium citrate, sodium chloride, potassium chloride and mixtures thereof and present in the range of 5-60 % by weight of the composition.
10. The insecticidal composition as claimed in claim 4, wherein the anti -caking agent is / are selected from the group comprising of group of talc, silica powder, hydrous magnesium silicate, magnesium carbonate, calcium carbonate, precipitate silica, hydrophobic fumed silica and mixtures thereof and present in the range of 2.0-20% by weight of the composition.
11. The insecticidal composition as claimed in claim 4, wherein the carrier is / are selected from the group consisting of silicon dioxide, china clay, kaolin, starch, bentonite, precipitated silica, fumed silica, talcum powder, lactose, ammonium sulpha or mixture there of present in the range of 1.0-45 % by weight of the composition.
12. . The insecticidal composition as claimed in claim 4, wherein the biocide or antimicrobial agent(s) is / are selected from 1, 2,- Benzisothiazolin -3-one, blends of 1,2,- benzisothiazolin-3-one and 2-methyl-4-isothiazolin-3-one, 5-chloro-2-methyl-4-isothiazolin-3- one, blends of 5-chloro-2-methyl-4-isothiazolin-3-one and 2-methyl-4-isothiazolin-3-one, zinc 1- hydroxy-2(lH)-pyridinethione, blends of zinc Lhydroxy-2(lH)-pyridinethione and zinc oxide, and 2-n-octyl-4- isothiazolin-3-one or mixture thereof and present in the range of 0.01 to 10 % by weight of the composition.
13. . The insecticidal composition as claimed in claim 4, wherein the rheology modifier or thickeners or thickening agents is / are selected from polysaccharides, carboxymethyl cellulose, bentonite clay, aluminium magnesium silicate, hydroxy propyl cellulose, xanthan gum, gum arabic, gaur gum, carbomer, chitosan, precipitated silica or mixtures thereof and present in the range of 0.01-5.0 % by weight of the composition.
14. . The insecticidal composition as claimed in claim 4, wherein the emulsifier(s) is / are selected from group consisting of araliphatic or aliphatic non-ionic emulsifier such as ethoxylated mono-, di- and trialkylphenols, ethoxylates of long-chain alcohols and polyethylene oxide / polypropylene oxide homo- and copolymers, EO / PO block copolymers, polymeric emulsifier, Ethoxylates of long-chain alkanols, Castor oil ethoxylate 40 mole , ethoxylated monoalkylphenol, ethoxilates of cetyl alcohol and / or stearyl alcohol ; Tristyrylphenol ethoxylate - 20 mole, Ethoxylated Tristyrylphenol ,and Anionic emulsifier such as alkali metal and ammonium salts of alkyl sulfates, of hemisulfates of ethoxylated alkanols and ethoxylated alkylphenols, alkylsulfonic acids, bis(phenylsulfonic acid) ethers and their alkali metal or ammonium salts, sodiumlaurylsulfate, sodium (cetyl / stearyl) sulfate, blend of anionic an non-ionic or mixture thereof and present in the range of 0.01 -20 % by weight of the composition.
15. . The insecticidal composition as claimed in claim 4 wherein the solvent(s) and cosolvent are selected from polar and non-polar solvent from the group comprising heavy aromatic hydrocarbon, N methyl pyrollidone (NMP) , Solvent Naphtha (Solvent C-9), Di methyl sulfoxide (DMSO), Dimethylformamide (DMF), N- alcohol, 2-ethyl hexanol , alkyl amide, vegetable oil, mineral oil, distilled water, aromatic solvents, water or mixtures thereof and present in the range of 1.0 to 20 % by weight of the composition.
16. . The insecticidal composition as claimed in claim 4, wherein the polymer(s) is / are selected from isocyanate, polyisocyanate used is toluene-2, 4-diisocyanate (TDI), diethylenetriamine (DETA), ethylene diamine (EDA), triethylenetetramine (TETA), and / or hexamethylene diamine (HMD A), diethanolglycine sodium salt, ethanoldiglycine disodium salt, hydroxymonocarboxylic acid compounds, hydroxydicarboxylic acid compounds, tetrasodium N,N-bis(carboxylatomethyl)-L-glutamate (GLDA), methylene diisocyanate (MDI), and / or low molecular weight polydiisocynates present in the range of 0.01- 5.0 % by weight of the composition.
17. . The insecticidal composition as claimed in claims 1 to 16, wherein the use of said composition promotes plant health, growth and thus increases plant yield in the field.
18. . The insecticidal composition as claimed in any one of the claims 1 to 17, wherein the composition is in form of 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) suspension, Tablet (TB), Ultra-low volume (ULV) liquid, Water dispersible granules (WG), Wettable powder (WP), Water dispersible powder for slurry seed treatment (WS), Water dispersible tablet (WT), a mixed composition of CS and SC (ZC) or a mixed composition of CS and SE (ZE) or a mixed composition of CS and EW (ZW).
19. A kit-of-parts comprising a plurality of components, wherein said plurality of components comprises:A) Ethion or its agrochemically acceptable salts, esters and derivatives;B) Compound of Formula I i.e. 4-chloro-3-ethyl-l-methyl-N-[[4-(4- methylphenoxy)phenyl]methyl]-lH-pyrazole-5-carboxamide or its agrochemically acceptable salts, esters and derivatives; andC) Fluxametamide or its agrochemically acceptable salts, esters and derivatives.
Citation Information
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