Abstract: The present invention relates to a solid composition comprising two or more agrochemically active ingredients and a process for preparing the same.
DESC:Field of Invention
The present invention relates to a solid composition comprising two or more agrochemically active ingredients.
Background of the Invention
Agrochemicals are chemical products comprised of fertilizers, plant-protection chemicals or pesticides, and plant-growth hormones used in agriculture. Agrochemicals significantly contributes to efficient and economical crop production for meeting the food requirement of the fast-growing global population. Different agrochemicals have different modes of action, due to the distinctive attributes of the two types of agrochemicals, farmers often adopt a combination of two or more agrochemicals. However, a combination of two active ingredients sometimes leads to incompatibility. It is not uncommon for physical and biological incompatibility to occur, for example insufficient stability of a combination formulation, decomposition of an active ingredient or antagonism of the active ingredients. Incompatibility can even lead to degradation of one or both of the active ingredients thereby resulting in poor efficacy. For an instance, it is well known that sulfonylurea herbicidal active ingredient has high activity in an extremely small amount. Though the conventional agricultural solid formulations, such as powders, wettable powders, granules, etc. are stable with little degradation, the formulation for combination of two or more active ingredients may result in significantly accelerated degradation during storage. It is therefore important for formulators to prepare stable formulations that allow for two or more incompatible actives to be combined in a single formulation, giving a desired active profile, high stability and in some cases enhanced synergy, thus permitting reduced rate of application as compared with the individual application of the active compounds.
There is therefore a need in the art for a formulation which is stable especially when two or more incompatible active compounds are combined providing a broader spectrum of control while reducing rate of application.
Objectives of the invention
It is a primary objective of the present invention to solve the above-mentioned problems by providing a solid composition comprising two or more incompatible active ingredients without leading to degradation of any active ingredient.
Another objective of the present invention is to provide a solid composition comprising two or more active ingredients having good efficacy.
Yet another objective of the present invention is to provide a process for preparing a solid composition comprising two or more incompatible active ingredients.
Additional objectives and advantages of the invention will be presented in part in the description which follows, and in part will be obvious from the description, or may be learned by practice of the invention, the objects and advantages being realized and attained by means of the methods, processes, and improvements disclosed in the present invention.
Summary of the Invention
In an aspect of present invention, there is provided a solid composition comprising,
i) particles of a first active ingredient encapsulated in alkylated melamine -formaldehyde crosslinked polymer having a low degree of alkylation;
ii) a second active ingredient; and
iii) at least one agrochemically acceptable excipient;
wherein either one or both active ingredient(s) are susceptible to degradation.
In an aspect, there is provided a process for preparing a solid composition according to present invention comprising,
a) preparing an encapsulated particles comprising first active ingredient and alkylated melamine -formaldehyde crosslinked polymer having a low degree of alkylation; and
b) mixing the encapsulated particles with a second active ingredient and agrochemically acceptable excipient (s).
In an aspect, there is provided a method of controlling undesired pest(s) using the solid composition according to the present invention.
In an aspect, there is provided a method of controlling undesired vegetation using the solid composition according to the present invention.
In an aspect, there is provided method of use of the solid composition according to the present invention for controlling pest(s) and/or undesired vegetation.
Detailed Description of the invention
Those skilled in art will be aware that invention described herein is subject to variations and modifications other than those specifically described. It is to be understood that the invention described herein includes all such variations and modifications. The invention also includes all such steps, features, compositions and methods referred to or indicated in this specification, individually or collectively, and any and all combinations of any two or more said steps or features.
Definitions:
For convenience, before further description of the present invention, certain terms employed in the specification, examples are described here. These definitions should be read in light of the remainder of the disclosure and understood as by a person of skill in the art. Unless defined otherwise, all technical and scientific terms used herein have the same meaning as commonly understood by a person of ordinary skill in the art. The terms used throughout this specification are defined as follows, unless otherwise limited in specific instances.
The terms used herein are defined as follows.
As used in the specification and the claims, the singular forms "a", "an", and "the" include plural referents unless the context clearly dictates otherwise.
The term "about" shall be interpreted to mean "approximately" or "reasonably close to" and any statistically insignificant variations therefrom. The term refers to a measurable value such as a parameter, an amount, a temporal duration, and the like and is meant to include variations of +/-15% or less, specifically variations of +/-10% or less, more specifically variations of +/-5% or less, even more specifically variations of +/-1% or less, and still more specifically variations of +/-0.1% or less of and from the particularly recited value, in so far as such variations are appropriate to perform in the disclosure described herein.
As used herein, the terms “comprising” “including,” “having,” “containing,” “involving,” and the like are to be understood to be open-ended, i.e., to mean including but not limited to.
The terms “preferred” and “preferably” refer to embodiments of the invention that may afford certain benefits, under certain circumstances. In an embodiment, the aspects and embodiments described herein shall also be interpreted to replace the clause “comprising” with either “consisting of” or with “consisting essentially of” or with “consisting substantially of”.
As used herein, the term “effective amount” refers to the amount of an active ingredient sufficient to produce the desired biological effect when applied to (i.e. contacted with) a pest to be controlled or their environment or to a plant, or to a seed from which plant is grown, or to locus of plant to protect the plant from injury by the pest or for other desired effect. In general, an effective amount is of about 0.001 to 20kg/ha.
As used herein, a “D10 value” means that the portion of particle with diameters smaller than this value is 10%.
As used herein, a “D50 value” means that the portion of particle with diameters smaller than this value is 50%.
As used herein, a “D90 value” means that the portion of particle with diameters smaller than this value is 90%.
As used herein, the term “prepolymer” means a compound having formula (I) which can form a polymer by undergoing self-condensation/ self-crosslinking.
The phrase “susceptible to degradation” is used herein with respect to active ingredient(s) means active ingredient(s) which are sensitive and are prone to degradation when in contact with another active ingredient(s) or excipient(s) i.e., they are incompatible with each other.
The phrase “particles of a first active ingredient encapsulated in alkylated melamine -formaldehyde crosslinked polymer having low degree of alkylation” means a capsule comprising a core of first active ingredient and a shell comprising alkylated melamine -formaldehyde crosslinked polymer having low degree of alkylation.
The phrase “particles of a first active ingredient encapsulated in alkylated melamine -formaldehyde crosslinked polymer having low degree of alkylation” is used interchangeably with the term “encapsulated particles” throughout the specification and have same meanings.
The use of any and all examples, or exemplary language (e.g., “such as”), is intended merely to better illustrate the disclosure and does not pose a limitation on the scope of the disclosure unless otherwise claimed. No language in the specification should be construed as indicating any non-claimed element as essential to the practice of the disclosure as used herein.
While the disclosure has been described with reference to an exemplary embodiment, it will be understood by those skilled in the art that various changes may be made, and equivalents may be substituted for elements thereof without departing from the scope of the disclosure. In addition, many modifications may be made to adapt a particular situation or material to the teachings of the disclosure without departing from the essential scope thereof. Therefore, it is intended that the disclosure is not limited to the particular embodiment disclosed as the best mode contemplated for carrying out this disclosure, but that the disclosure will include all embodiments falling within the scope of the appended claims.
In an aspect of present invention there is provided a solid composition comprising
i) particles of a first active ingredient encapsulated in alkylated melamine -formaldehyde crosslinked polymer having low degree of alkylation,
ii) a second active ingredient, and
iii) at least one agrochemically acceptable excipient;
wherein either one or both active ingredient(s) are susceptible to degradation.
In an embodiment, the first active ingredient is selected from group comprising of pesticides such as insecticides, herbicides, fungicides, nematicides and the likes; fertilizers; pheromones; plant-growth regulators; nutrients; and the likes.
In an embodiment, the first active ingredient is a pesticide such as insecticide, herbicide, fungicide, nematicide and the likes.
In an embodiment, the first active ingredient is selected from an insecticide or an herbicide.
In an embodiment, the first active ingredient is an insecticide selected from group comprising of, but not limited to, Acetylcholinesterase (AChE) inhibitors, GABA -gated chloride channel blockers, Sodium channel modulators, Nicotinic acetylcholine receptor (nAChR) competitive modulators, Nicotinic acetylcholine receptor (nAChR) allosteric modulators, Glutamate -gated chloride channel (GluCl) allosteric modulators, Juvenile hormone mimics, Chordotonal organ TRPV channel modulators, Mite growth inhibitors, Microbial disrupters of insect midgut membranes, Inhibitors of mitochondrial ATP synthase, Uncouplers of oxidative phosphorylation via disruption of the proton gradient, Nicotinic acetylcholine receptor (nAChR) channel blockers, Inhibitors of chitin biosynthesis , Moulting disrupters, Ecdysone receptor agonists, Octopamine receptor agonists, Mitochondrial complex electron transport inhibitors, Voltage-dependent sodium channel blockers, Inhibitors of acetyl CoA carboxylase, Chordotonal organ Modulators, multi-site miscellaneous insecticides, or bioinsecticides.
In an embodiment, the insecticide is selected from the group comprising Nicotinic acetylcholine receptor (nAChR) competitive modulators.
In an embodiment, the insecticide is a neonicotinoid insecticide selected from the group comprising of acetamiprid, clothianidin, dinotefuran, imidacloprid, nitenpyram, thiacloprid or thiamethoxam.
In an embodiment, the first active ingredient is an herbicide selected from group comprising of, but not limited to, lipid biosynthesis inhibitors, amino acid biosynthesis inhibitors, plant growth regulators, photosynthesis inhibitors, nitrogen-metabolism inhibitors, pigment inhibitors, cell-membrane disruptors, or seedling-growth inhibitors.
In an embodiment, the herbicide is an amino acid biosynthesis inhibitor.
In an embodiment, the herbicide is a sulfonylurea herbicide.
In an embodiment, the herbicide is a sulfonylurea herbicide selected from the group comprising halosulfuron, bensulfuron methyl, chlorsulfuron, ethametsulfuron methyl, foramsulfuron, mesosulfuron methyl, metsulfuron methyl, Nicosulfuron, oxasulfuron, primisulfuron methyl, prosulfuron, rimsulfuron, sulfometuron methyl, sulfosulfuron, thifensulfuron methyl, triasulfuron or triflusulfuron methyl.
In an embodiment, the first active ingredient is selected from an insecticide or an herbicide; wherein the insecticide is a neonicotinoid insecticide selected from the group comprising of acetamiprid, clothianidin, dinotefuran, imidacloprid, nitenpyram, thiacloprid or thiamethoxam; and the herbicide is a sulfonylurea herbicide selected from the group comprising of halosulfuron, bensulfuron methyl, chlorsulfuron, ethametsulfuron methyl, foramsulfuron, mesosulfuron methyl, metsulfuron methyl, Nicosulfuron, oxasulfuron, primisulfuron methyl, prosulfuron, rimsulfuron, sulfometuron methyl, sulfosulfuron, thifensulfuron methyl, triasulfuron or triflusulfuron methyl
In an embodiment, the first active ingredient is imidacloprid.
In another embodiment, the first active ingredient is halosulfuron-methyl.
In an embodiment, the first active ingredient is susceptible to degradation, i.e. the active ingredient tends to degrade faster making the formulation unstable and inefficient; when used with other active ingredients.
In an embodiment, the first active ingredient displays improved physico-chemical stability when used with the second active ingredient.
In an embodiment, the average particle size of first active ingredient is less than 10 microns. Preferably, the particle size is in the range of about 1 micron to about 8 microns. More preferably, it is in a range of about 2 microns to about 5 microns. The particle size given is the so-called average particle diameter, also called D50 – value.
In an embodiment, the D90 particle size of first active ingredient is less than 30 microns. Preferably, the particle size is in the range of about 3 microns to about 30 microns.
In an embodiment there is provided an encapsulated particles comprising first active ingredient; alkylated melamine -formaldehyde crosslinked polymer having a low degree of alkylation; and an anionic surfactant.
In an embodiment, the encapsulated particles comprise first active ingredient having particle size (D90) in range of 3 microns to about 30 microns.
In an embodiment, the alkylated melamine -formaldehyde crosslinked polymer is formed by self-condensation of a prepolymer of formula (I)
Formula (I)
wherein R is hydrogen or C1 to C5 alkyl group.
In an embodiment, the alkylated melamine -formaldehyde crosslinked polymer is methylated melamine -formaldehyde crosslinked polymer.
In an embodiment, the alkylated melamine -formaldehyde crosslinked polymer constitutes from about 0.1% to about 20% by total weight of the encapsulated particle of first active ingredient.
In an embodiment, the alkylated melamine -formaldehyde crosslinked polymer constitutes from about 0.1% to about 10% by total weight of the encapsulated particle.
In an embodiment, the alkylated melamine -formaldehyde crosslinked polymer constitutes from about 1% to about 10% by total weight of the encapsulated particle of first active ingredient. Preferably from about 1% to about 5% by total weight of the encapsulated particle of first active ingredient.
In an embodiment, the first active ingredient constitutes from about 60% to 99.9% by total weight of the encapsulated particle.
In an embodiment, the first active ingredient constitutes from about 90% to 99.9% by total weight of the encapsulated particle.
In an embodiment, the ratio of the alkylated melamine -formaldehyde crosslinked polymer to the first active ingredient in the encapsulated particle is in the range of about 1: 10 to 1: 100. Preferably, 1: 20 to 1: 80.
In an embodiment, the encapsulated particles further comprise an anionic surfactant.
In an embodiment, the encapsulated particle comprises of first active ingredient, alkylated melamine -formaldehyde crosslinked polymer having low degree of alkylation and an anionic surfactant.
In an embodiment, the particles of the first active ingredient are encapsulated in alkylated melamine -formaldehyde crosslinked polymer having low degree of alkylation and an anionic surfactant.
In an embodiment, an insecticide is encapsulated in alkylated melamine -formaldehyde crosslinked polymer having low degree of alkylation and anionic surfactant.
In an embodiment, a nicotinic acetylcholine receptor (nAChR) competitive modulator is encapsulated in alkylated melamine -formaldehyde crosslinked polymer having low degree of alkylation and anionic surfactant.
In an embodiment, a neonicotinoid insecticide is encapsulated in alkylated melamine -formaldehyde crosslinked polymer having a low degree of alkylation and an anionic surfactant.
In an embodiment, imidacloprid is encapsulated in alkylated melamine -formaldehyde crosslinked polymer having a low degree of alkylation and an anionic surfactant.
In an embodiment, an herbicide is encapsulated in alkylated melamine -formaldehyde crosslinked polymer having a low degree of alkylation and an anionic surfactant.
In an embodiment, an amino acid biosynthesis inhibitor is encapsulated in alkylated melamine -formaldehyde crosslinked polymer having a low degree of alkylation and an anionic surfactant.
In an embodiment, a sulfonylurea herbicide is encapsulated in alkylated melamine -formaldehyde crosslinked polymer having low degree of alkylation and an anionic surfactant.
In an embodiment, a halosulfuron-methyl is encapsulated in alkylated melamine -formaldehyde crosslinked polymer having a low degree of alkylation and an anionic surfactant.
In an embodiment, the anionic surfactant is selected from group comprising of, but not limited to, anionic derivatives of fatty alcohols having 10-24 carbon atoms in the form of ether carboxylates, sulfonates, sulfates, and phosphates, and their inorganic salts (e.g., alkali metal salts and alkaline earth metal salts) and organic salts (e.g., salts based on amine or alkanolamine); anionic derivatives of copolymers consisting of ethylene oxide (EO), propylene oxide (PO) and/or butylene oxide (BO) units, in the form of ether carboxylates, sulfonates, sulfates, and phosphates, and their inorganic salts (e.g., alkali metal salts and alkaline earth metal salts) and organic salts (e.g., salts based on amine or alkanolamine); derivatives of alkylene oxide adducts of alcohols, in the form of ether carboxylates, sulfonates, sulfates and phosphates, and their inorganic salts (e.g., alkali metal salts and alkaline earth metal salts) and organic salts (e.g., salts based on amine or alkanolamine); derivatives of fatty acid alkoxylates, in the form of ether carboxylates, sulfonates, sulfates and phosphates, and their inorganic salts (e.g., alkali metal salts and alkaline earth metal salts) and organic salts (e.g., salts based on amine or alkanolamine); alkyl ether phosphate, alkyl sulfate and its salts, alkyl sulfosuccinate mono ester and diester salts, olefin sulfonic acid salts; derivatives of lignin, in form of sulfonates, phenolic, organosolv, kraft and its salts; or combinations thereof.
In an embodiment, the anionic surfactant used is selected from derivatives of lignin, in form of sulfonates, phenolic, kraft or its salts; or combinations thereof.
In an embodiment, the anionic surfactant constituting from about 1% to about 20% by total weight of the encapsulated particle of first active ingredient.
In an embodiment, the particle size of encapsulated particles of first active ingredient is less than 100 microns. Preferably, it is less than 50 microns.
In an embodiment, the solid composition according to present invention comprises from about 0.1% w/w to about 25% w/w encapsulated first active ingredient of the total weight of the solid composition.
In another embodiment, the composition comprises about 0.1% w/w to about 10% w/w encapsulated first active ingredient of the total weight of the solid composition.
In an embodiment, the second active ingredient selected is susceptible to degradation i.e. the active ingredient tends to degrade fasters making the formulation unstable and inefficient; when used with other active ingredients.
In an embodiment, in the solid formulation of present invention, the second active ingredient exhibits improved physico-chemical stability with the first active ingredient.
In an embodiment, the second active ingredient is selected from group comprising of pesticides such as insecticides, herbicides, fungicides, nematicides and the likes; fertilizers; pheromones; plant-growth regulators; nutrients; and the likes.
In an embodiment, the composition comprises about 1% w/w to about 90% w/w second active ingredient of the total weight of the solid composition.
In an embodiment, the composition comprises about 10% w/w to about 80% w/w second active ingredient of the total weight of the solid composition.
In an embodiment, the first and second active ingredients both are insecticides.
In an embodiment, the second insecticide is selected in accordance with embodiment provided above.
In an embodiment, the first active ingredient is a neonicotinoid insecticide and the second active ingredient is an organophosphate insecticide.
In an embodiment, the second active ingredient is acephate.
In an embodiment, the first active ingredient is imidacloprid and second active ingredient is acephate.
In an embodiment, the first and second active ingredients both are herbicides.
In an embodiment, the second herbicide is selected in accordance with embodiment provided above.
In an embodiment, both first and the second active ingredient exhibits improved physico-chemical stability.
In an embodiment, the present solid composition further comprises one or more additional agrochemical ingredients.
The solid composition comprises one additional agrochemical ingredients i.e., a third active ingredient.
In an embodiment, the solid composition further comprises a third active ingredient.
In an embodiment, the third active ingredient is selected from group comprising of pesticides such as insecticides, herbicides, fungicides, nematicides and the likes; fertilizers; pheromones; plant-growth regulators; nutrients; and the likes.
In an embodiment, the composition comprises about 0.1% w/w to about 20% w/w third active ingredient of the total weight of the solid composition.
In an embodiment, the first, second and third active ingredients are herbicides.
In an embodiment, second and third active ingredients are the herbicide is selected from group comprising of, but not limited to, lipid biosynthesis inhibitors, amino acid biosynthesis inhibitors, plant growth regulators, photosynthesis inhibitors, nitrogen-metabolism inhibitors, pigment inhibitors, cell-membrane disruptors, or seedling-growth inhibitors.
In an embodiment, second active ingredient is the herbicide is selected from group comprising of, photosynthesis inhibitors such as triazines, triazinones, phenylureas, benzothiadiazole, nitriles, phenyl-carbamates.
In an embodiment, second active ingredient is triazine herbicide.
In an embodiment, second active ingredient is atrazine.
In an embodiment, third active ingredient is the herbicide is selected from group comprising of pigment inhibitors such as pyridazinone, isoxazolidinone, triketone, isoxazole.
In an embodiment, third active ingredient is a Triketone.
In an embodiment, third active ingredient is topramezone.
In an embodiment, the first active ingredient is selected from a sulfonylurea herbicide, second active ingredient is selected from a triazine herbicide and third active ingredient is selected from a triketone herbicide.
In an embodiment, the first active ingredient is halosulfuron-methyl, second active ingredient is atrazine; and third active ingredient is topramezone.
In an embodiment, the agrochemically acceptable excipient is selected from the group comprising aqueous or organic solvent(s), buffering agent(s), acidifier(s), surfactant(s), wetting agent(s), spreading agent(s), tackifier(s), sticker(s), carrier(s), filler(s), thickener(s), emulsifier(s), dispersant(s), sequestering agent(s), anti-settling agent(s), coalescing agent(s), rheology modifier(s), defoaming agent(s), photo-protector(s), anti-freeze agent(s), biocide(s), penetrant(s), mineral or vegetable oil(s), pigment(s) and drift control agent(s), or combinations thereof.
In an embodiment, the agrochemically acceptable excipient is carrier.
In an embodiment, the carrier may be selected from group comprising of, but not limited to, the carrier comprises minerals like clay such as china clay, acid clay, kaolin such as kaolinite, dickite, nacrite, and halloysite, serpentines such as chrysotile, lizardite, antigorite, and amesite, synthetic and diatomaceous silicas, precipitated silica, colloidal silica, attapulgite, bentonite, white carbon black, dolomite, montmorillonite minerals such as sodium montmorillonite, smectites, such as saponite, hectorite, sauconite, and hyderite, micas, such as pyrophyllite, talc, agalmatolite, muscovite, phengite, sericite, and illite, silicas such as cristobalite and quartz, such as sepiolite; vermiculite, laponite, pumice, bauxite, hydrated aluminas, perlite, sodium bicarbonate, volclay, vermiculites, limestone, natural and synthetic silicates, charcoal, wet process silicas, dry process silicas, calcined products of wet process silicas, surface-modified silicas, mica, zeolite, diatomaceous earth, derivatives thereof; chalks, fuller's earth, loess, mirabilite, white carbon, slaked lime, synthetic silicic acid, starch, modified starch, cellulose, plant carriers such as cellulose, chaff, wheat flour, wood flour, starch, rice bran, wheat bran, and soyabean flour, casein sodium, sucrose, salt cake, ammonium sulphate, dibasic ammonium phosphate, potassium pyrophosphate, sodium tripolyphosphate, their derivatives, or combinations thereof. Commercially available silicates can also be used.
In an embodiment of present invention, there is provided a solid composition comprising;
i) particles of first active ingredient encapsulated in alkylated melamine -formaldehyde crosslinked polymer having a low degree of alkylation and an anionic surfactant
ii) a second active ingredient; and
iii) an agrochemically acceptable excipient,
wherein either one or both active ingredient(s) are susceptible to degradation; and wherein the first active ingredient is selected from sulfonylurea herbicides or neonicotinoid insecticides.
In an embodiment of present invention, there is provided a solid composition comprising;
i) 0.1% w/w to about 25% w/w encapsulated particles of first active ingredient selected from sulfonylurea herbicides or neonicotinoid insecticides;
ii) about 1% w/w to about 90% w/w second active ingredient; and
iii) an agrochemically acceptable excipient,
wherein either one or both active ingredient(s) are susceptible to degradation; and wherein the first active ingredient is encapsulated in an alkylated melamine -formaldehyde crosslinked polymer having low degree of alkylation.
In an embodiment, the solid composition, optionally comprises a third active ingredient in an amount of about 0.1% w/w to about 20% w/w of the total weight of the solid composition
According to an embodiment of the present disclosure, the solid composition is preferably including, but not limited to, dust, powder, granules, pellets, tablets, dry flowable, wettable powder, water effervescent granules, water dispersible granules (WDG) and water emulsifiable granules.
In an embodiment, the present invention provides a solid insecticidal composition comprising;
i) a neonicotinoid insecticide encapsulated in alkylated melamine -formaldehyde crosslinked polymer having low degree of alkylation;
ii) a second active ingredient; and
iii) at least one agrochemically acceptable excipient;
wherein either one or both active ingredient(s) are susceptible to degradation.
In a preferred embodiment, the present invention provides a solid insecticidal composition comprising;
i) imidacloprid encapsulated in alkylated melamine -formaldehyde crosslinked polymer having low degree of alkylation;
ii) a second active ingredient; and
iii) at least one agrochemically acceptable excipient;
wherein either one or both active ingredient(s) are susceptible to degradation.
In a more preferred embodiment, the present invention provides a solid insecticidal composition comprising;
i) imidacloprid encapsulated in alkylated melamine -formaldehyde crosslinked polymer having low degree of alkylation;
ii) acephate; and
iii) at least one agrochemically acceptable excipient.
In a more preferred embodiment, the present invention provides a solid insecticidal composition comprising;
i) from about 0.1% w/w to about 10% w/w imidacloprid encapsulated in alkylated melamine -formaldehyde crosslinked polymer having low degree of alkylation;
i) about 10% w/w to about 80% w/w acephate; and
ii) at least one agrochemically acceptable excipient.
In an embodiment, the present invention provides a soluble powder formulation comprising;
i) a neonicotinoid insecticide encapsulated in alkylated melamine - formaldehyde crosslinked polymer having a low degree of alkylation;
ii) a second active ingredient; and
iii) at least one agrochemically acceptable excipient;
wherein either one or both active ingredient(s) are susceptible to degradation.
In a preferred embodiment, the present invention provides a soluble powder formulation comprising;
i) imidacloprid encapsulated in alkylated melamine -formaldehyde crosslinked polymer having a low degree of alkylation;
ii) a second active ingredient; and
iii) at least one agrochemically acceptable excipient;
wherein either one or both active ingredient(s) are susceptible to degradation.
In a more preferred embodiment, the present invention provides a soluble powder formulation comprising;
i) imidacloprid encapsulated in alkylated melamine -formaldehyde crosslinked polymer having a low degree of alkylation,
ii) acephate, and
iii) at least one agrochemically acceptable excipient.
In a preferred embodiment, the present invention provides a soluble powder formulation comprising;
i) from about 0.1% w/w to about 10% w/w imidacloprid encapsulated in an alkylated melamine -formaldehyde crosslinked polymer having low degree of alkylation;
ii) about 10% w/w to about 80% w/w acephate; and
iii) at least one agrochemically acceptable excipient.
In an embodiment, the present invention provides a solid herbicidal composition comprising;
i) a sulfonylurea herbicide encapsulated in alkylated melamine -formaldehyde crosslinked polymer having low degree of alkylation;
ii) a second active ingredient; and
iii) at least one agrochemically acceptable excipient;
wherein either one or both active ingredient(s) are susceptible to degradation.
In a preferred embodiment, the present invention provides a solid herbicidal composition comprising;
i) halosulfuron-methyl encapsulated in alkylated melamine -formaldehyde crosslinked polymer having low degree of alkylation;
ii) a second active ingredient;
iii) a third active ingredient and
iv) at least one agrochemically acceptable excipient;
wherein either one, two or all the active ingredient(s) are susceptible to degradation.
In a preferred embodiment, the present invention provides a solid herbicidal composition comprising;
i) halosulfuron-methyl encapsulated in alkylated melamine -formaldehyde crosslinked polymer having low degree of alkylation;
ii) atrazine;
iii) topramezone; and
iv) at least one agrochemically acceptable excipient.
In a more preferred embodiment, the present invention provides a solid herbicidal composition comprising;
i) from about 0.1% w/w to about 10% w/w halosulfuron-methyl encapsulated in alkylated melamine -formaldehyde crosslinked polymer having low degree of alkylation;
ii) from about 10% w/w to about 80% w/w atrazine;
iii) from about 0.1% w/w to about 20% w/w topramezone; and
iv) at least one agrochemically acceptable excipient.
In an embodiment, the present invention provides a water dispersible granular (WDG) formulation comprising;
i) a sulfonylurea herbicide encapsulated in alkylated melamine -formaldehyde crosslinked polymer having a low degree of alkylation;
ii) a second active ingredient;
iii) a third active ingredient; and
iv) at least one agrochemically acceptable excipient;
wherein either anyone, two or all active ingredient(s) are susceptible to degradation.
In a preferred embodiment, the present invention provides a water dispersible granular (WDG) formulation comprising;
i) halosulfuron-methyl encapsulated in alkylated melamine -formaldehyde crosslinked polymer having a low degree of alkylation;
ii) a second active ingredient;
iii) a third active ingredient; and
iv) at least one agrochemically acceptable excipient;
wherein either anyone, two or all active ingredient(s) are susceptible to degradation.
In a more preferred embodiment, the present invention provides a water dispersible granular (WDG) formulation comprising;
i) halosulfuron-methyl encapsulated in alkylated melamine -formaldehyde crosslinked polymer having a low degree of alkylation;
ii) atrazine;
iii) topramezone; and
iv) at least one agrochemically acceptable excipient.
In a more preferred embodiment, the present invention provides a water dispersible granular (WDG) formulation comprising;
i) from about 0.1% w/w to about 10% w/w halosulfuron-methyl encapsulated in an alkylated melamine -formaldehyde crosslinked polymer having a low degree of alkylation;
ii) from about 10% w/w to about 80% w/w atrazine;
iii) from about 0.1% w/w to about 20% w/w topramezone; and
iv) at least one agrochemically acceptable excipient.
In an aspect there is provided a process for preparing a solid composition according to present invention comprising;
a) preparing encapsulated particles comprising first active ingredient and alkylated melamine -formaldehyde crosslinked polymer having a low degree of alkylation; and
b) mixing the encapsulated particles with a second active ingredient and agrochemically acceptable excipient (s).
In an embodiment, the step a) of the process comprises
i) mixing the first active ingredient with the anionic surfactant;
ii) milling the mixture obtained in step i) to particle size (D90) in range of 3 microns to about 30 microns; and
iii) encapsulating the mixture obtained in step ii) with an alkylated melamine -formaldehyde crosslinked polymer having a low degree of alkylation.
In an embodiment, the step a) of the process also involves a step of formation of alkylated melamine -formaldehyde crosslinked polymer comprising self-condensation a prepolymer of formula (I)
Formula (I)
wherein R is hydrogen or C1 to C5 alkyl group.
In an embodiment, heating the prepolymer of formula (I) results in self-condensation of the prepolymer.
In an embodiment, the prepolymer is heated above 35°C to obtain self-condensed polymer. Preferably at a temperature ranging from about 35°C to about 200°C.
In an embodiment, the self-condensation of the prepolymer of formula (I) is carried out in presence of a catalyst and a solvent.
In an embodiment, the prepolymer of formula (I) is a compound wherein R is hydrogen or methyl group.
In an embodiment, the catalyst is acid or base.
The acid used is organic or inorganic acid, selected from group comprising of, but not limited to, hydrochloric acid, sulfuric acid, nitric acid, formic acid, acetic acid, citric acid and the like.
The base used is organic or inorganic base. The inorganic base is selected from group comprising of, but not limited to, alkali metal or alkaline earth metal carbonates, bicarbonates, hydroxides and the like, wherein the alkali metal and alkaline earth metal is selected from a group comprising of lithium, sodium, potassium, magnesium, calcium, cesium, barium, and the like. The organic base is selected from the group comprising of triethylamine, diisopropylamine, diisopropylethylamine, piperidine, pyridine N-methyl morpholine N, N-dimethylbenzylamine, picoline, lutidine and the like.
In an embodiment, the solvent used is selected from water or an organic solvent.
In an embodiment, the alkylated melamine -formaldehyde crosslinked polymer is methylated melamine -formaldehyde crosslinked polymer having a low degree of alkylation.
In an embodiment, the step a) of the process provides a slurry comprising encapsulated particles and water.
In an embodiment, the slurry obtained may further comprise an inert agrochemically acceptable excipient such as kaolin.
In an embodiment, the slurry obtained is directly used in next step b); or the slurry is dried to obtain encapsulated particles.
In an embodiment, in step b) the slurry comprising encapsulated particles and water is directly mixed with the second active ingredient and agrochemically acceptable excipient(s).
In an embodiment, in the step b) the dried encapsulated particles are mixed with the second active ingredient and agrochemically acceptable excipient (s).
In an embodiment, the step b) comprises additional active ingredient(s).
In an embodiment there is provided a process for preparing a soluble powder formulation according to present invention comprising;
a) preparing an encapsulated particles comprising first active ingredient and alkylated melamine -formaldehyde crosslinked polymer having a low degree of alkylation;
b) mixing the encapsulated particles with a second active ingredient and agrochemically acceptable excipient(s) to obtain said soluble powder formulation.
In an embodiment there is provided a process for preparing a soluble powder formulation according to present invention comprising:
a) preparing an encapsulated particles comprising imidacloprid and methylated melamine -formaldehyde crosslinked polymer having a low degree of alkylation; and
b) mixing the encapsulated particles with acephate and agrochemically acceptable excipient(s) to obtain said soluble powder formulation.
In an embodiment there is provided a process for preparing a water dispersible granules (WDG) composition according to present invention comprising;
a) preparing an encapsulated particles comprising first active ingredient and alkylated melamine -formaldehyde crosslinked polymer having a low degree of alkylation;
b) mixing the encapsulated particles with a second active ingredient and agrochemically acceptable excipient (s) to obtain a mixture;
c) preparing a dough by adding water to the mixture obtained in step b); and
d) extruding the dough to obtain water dispersible granules.
In an embodiment, the step b) comprises additional active ingredient (s).
In an embodiment there is provided a process for preparing a water dispersible granules (WDG) composition according to present invention comprising;
a) preparing an encapsulated particles comprising halosulfuron-methyl and methylated melamine -formaldehyde crosslinked polymer having a low degree of alkylation;
b) mixing the encapsulated particles with atrazine; topramezone and agrochemically acceptable excipient (s) to obtain a mixture;
c) preparing a dough by adding water to the mixture obtained in step b); and
d) extruding the dough to obtain water dispersible granules.
In an embodiment there is provided a process for preparing solid composition according to present invention comprising;
a) preparing an encapsulated particles comprising first active ingredient, alkylated melamine -formaldehyde crosslinked polymer having a low degree of alkylation and anionic surfactant; and
b) mixing the encapsulated particles with a second active ingredient and agrochemically acceptable excipient (s).
In an aspect of present invention there is provided a phosphorus composition having particles of phosphorus encapsulated in alkylated melamine -formaldehyde crosslinked polymer having low degree of alkylation and anionic surfactant.
In an embodiment, the phosphorus is red phosphorus or yellow phosphorus.
It is well known that phosphorus is highly inflammable. At elevated temperature in the presence of moisture and atmospheric oxygen it emits highly toxic phosphine which is spontaneously flammable in air. The encapsulation of phosphorus according to present invention ensures reduction of emission of phosphine to atmosphere, making the handling of phosphorus convenient.
In an aspect, there is provided a method of controlling undesired pest(s) using the solid composition according to present invention.
In an embodiment, there is provided a method of controlling undesired pest(s) by applying to the plants/pest or to their locus/environment, an effective amount of the solid composition according to present invention, comprising
i) particles of a first active ingredient encapsulated in alkylated melamine -formaldehyde crosslinked polymer having a low degree of alkylation,
ii) a second active ingredient, and
iii) at least one agrochemically acceptable excipient;
wherein either one or both active ingredient(s) are susceptible to degradation.
The undesired pests herein are defined as being living organisms that occur where they are not wanted or that cause damage to crop or humans or other animals. Examples include insects, and mice, unwanted plants (weeds/ undesired vegetation), fungi, microorganisms such as bacteria and viruses, and prions.
In an aspect, there is provided a method of controlling insects using the solid composition according to present invention.
In an embodiment, a method of controlling insects by applying to the insect or to their environment, an effective amount of a soluble powder formulation comprising;
i) imidacloprid encapsulated in alkylated melamine -formaldehyde crosslinked polymer having a low degree of alkylation,
ii) acephate, and
iii) at least one agrochemically acceptable excipient.
In an aspect, there is provided a method of controlling undesired vegetation using the solid composition according to present invention.
In an embodiment, a method of controlling undesired vegetation by applying to the plants or to their locus, a water dispersible granular (WDG) formulation comprising:
i) halosulfuron-methyl encapsulated in alkylated melamine -formaldehyde crosslinked polymer having a low degree of alkylation;
ii) atrazine;
iii) topramezone; and
iv) at least one agrochemically acceptable excipient.
In an aspect, there is provided a method of use of the solid composition according to present invention for controlling pest(s) and/or undesired vegetation.
In an embodiment, the active content of all the active ingredients of the present composition remained quite stable in composition with good suspensibility upon dilution before application.
EXAMPLES
The following examples are presented to provide what is believed to be the most useful and readily understood description of procedures and conceptual aspects of this invention. The examples provided below are merely illustrative of the invention and are not intended to limit the same to disclosed embodiments. Variations and changes obvious to one skilled in the art are intended to be within the scope and nature of the invention.
I. Analytical Methods
Particle size Distribution (PSD) was determined by Malvern mastersizer 3000 using laser diffraction to measure the particle size and size distribution. (Refractive index particle - 1.56; Dispersant media – water; and Refractive index dispersant media -1.33)
II. Ingredients
Anionic surfactant: sodium lignosulfonate;
Dispersing agent: Modified styrene acrylic polymer; naphthalene sulfonate condensate or salts thereof;
Wetting agent: Fatty alcohol ethoxylate; dialkyl naphthalene sulphonate or its salt;
Defoamer: silicone antifoam emulsion;
Carrier: kaolin; precipitated silica; ammonium sulphate, dibasic ammonium phosphate
Base: sodium hydroxide, sodium carbonate, sodium bicarbonate, potassium hydroxide, potassium carbonate, potassium bicarbonate and the likes.
Stabilizer: Sodium hydrogen Phosphate, Ammonium hydroxide, Ammonium chloride, Acetic acid and Sodium acetate
Alkylated melamine -formaldehyde crosslinked prepolymer having low degree of alkylation: Methylated melamine -formaldehyde crosslinked prepolymer
III. Preparation of the compositions
Example 1: Encapsulation of active ingredient
To the mixture of active ingredient, sodium lignosulfonate and water, which has been previously bead milled to particle size (D90) in range of about 7 to 10 microns was added about 50% aqueous solution of alkylated melamine -formaldehyde crosslinked prepolymer having low degree of alkylation and pH was adjusted to about 8.5 to 9.5 using a base resulting in-situ formation of crosslinked polymer having low degree of alkylation. The mixture was stirred at about 25°C to 35°C for about 3 to 5 hours to obtain a slurry. The composition of said slurry is provided in table 1. The mixture was then subjected to separation by centrifugation or by known technique to obtain the solid wet cake comprising encapsulated active ingredient. The wet cake was then dried at 50°C under vacuum to get encapsulated active ingredient having less than 0.8 % moisture content.
The quantities of active ingredient, sodium lignosulfonate, water, base and alkylated melamine -formaldehyde crosslinked polymer for each example to obtain a slurry is as provided in table 1.
Table 1 (Composition of the slurry obtained)
Ingredient Example No.
1A
(%w/w) 1B
(%w/w) 1C
(%w/w) 1D
(%w/w)
Halosulfuron-methyl technical
(purity 98%) 50 50 - -
Imidacloprid technical
(purity 98%) - - 50 50
Anionic surfactant 5 5 5 5
20% aqueous Sodium hydroxide (Base) 5 5 5 5
alkylated melamine -formaldehyde polymer 1 2 1 2
Water Q.S Q.S Q.S Q.S
*Quantities in above table is provided in weight percentages
*Q.S. is an abbreviation for Quantum satis
Example 2: General process for preparation of Water dispersible granule (WDG) formulation
Desired quantities of active ingredient(s) (except for encapsulated active ingredient) and excipients were mixed to obtain a homogenous mixture. The mixture was then milled to obtain desired particle size i.e. D90 is less than 30 microns. To the milled mixture was added a desired quantity of encapsulated active ingredient and 17 – 22 % of water to obtain a dough. The dough was extruded to result in granules, granules were dried till the residual moisture content was in range of 1 to 1.5 %.
The examples of Water dispersible granule (WDG) formulation are presented in table 2 below
Table 2
Ingredients Examples
2A
(%w/w) 2B
(%w/w)
Encapsulated particle of Halosulfuron-methyl
(Example 1A) 3.56
-
Encapsulated Halosulfuron-methyl
(Example 1B) - 3.62
Atrazine 41.45 41.45
Topramezone 1.75 1.75
Dispersing agent 4.50 4.50
Wetting agent 4.00 4.00
Sodium Hydrogen Phosphate 4.00 4.00
Defoamer 0.20 0.20
Carrier Q.S. Q.S.
Comparative example 1:
Water dispersible granule (WDG) formulation was prepared according to process provided in example 2, except that the Halosulfuron-methyl active ingredient was not encapsulated. The composition is provided as follows
Table 3
Ingredients Comparative example 1
(%w/w)
Halosulfuron-methyl technical 3.51
Atrazine 41.45
Topramezone 1.75
Dispersing agent 4.5
Wetting agent 4
Stabilizer 4
Defoamer 0.20
Carrier Q.S.
Example 3: General process for preparation of soluble powder (SP) formulation
Desired quantities of active ingredient(s) (except for encapsulated active ingredient) and excipients were mixed to obtain a homogenous mixture. To this mixture was added a premix of encapsulated active ingredient and a carrier, the mixture was mixed at low rpm to get soluble powder (SP) formulation.
The examples of soluble powder (SP) formulation are presented in table 4 below
Table 4
Ingredients Example 3
(%w/w)
Encapsulated particle of Imidacloprid
(Example 1C) 2.02
Acephate technical
(97% purity) 53.09
Carrier Q.S
Comparative example 2:
Soluble powder (SP) formulation was prepared according to process provided in example 3, except for Imidacloprid active ingredient was not encapsulated. The composition is provided as in table 5 as follows
Table 5
Ingredients Comparative example 2
(%w/w)
Imidacloprid technical
1.98
Acephate technical
(97% purity) 53.09
Carrier Q.S
Evaluation of physiochemical parameters
The composition of above examples was evaluated for various physicochemical parameters.
i) Water dispersible granule (WDG) formulation
The composition provided in example 2 and comparative example 1 were evaluated. Water dispersible granules appeared as beige coloured granules free from extraneous matter and remained as such in accelerated heat storage (AHS) study conducted at 54°C for 14 days. The active content of all the three active ingredients, i.e. atrazine, topramezone and halosulfuron-methyl remained quite stable in composition according to example 2. Suspensibility of all the three active ingredients, was quite acceptable for the composition of the present invention. The detailed evaluation can be provided as in Table 6 below
Table 6
Parameters Example 2A Example 2B Comparative Example 1
0 days 14 days AHS 0 days 14 days AHS 0 days 14 days AHS
Appearance Beige colored granules Beige colored granules Off-White colored granules
A.I content
(%w/w) Halosulfuron-methyl 3.6 3.35 3.66 3.47 1.84 0.02
Atrazine 41.25 40.9 41.2 40.75 41.78 41.48
Topramezone 1.7 1.68 1.72 1.7 1.61 1.59
Degradation Halosulfuron-methyl 6.94% 5.19% 98.91%
Atrazine 0.85% 1.09% 0.72%
Topramezone 1.18% 1.16% 1.24%
pH 1% suspension 7.62 7.55 7.74 7.72 4.49 4.27
Suspensibility 85 84.3 87.5 85.9 54.2 55.4
Wet sieve content (%) 0.13 0.14 0.12 0.14 0.17 0.2
The inventors of the present invention successfully developed various stable solid compositions in the form of water dispersible granules of halosulfuron-methyl with other active ingredients by encapsulating a.i. according to present invention. The stable solid compositions according to present invention not only demonstrated excellent suspensibility but also had about 90% less degradation as compared to composition prepared without encapsulation of halosulfuron-methyl. The active ingredients were found to remain quite stable after preparation and even during storage studies.
ii) Soluble powder (SP) formulation
The composition provided in example 3 and comparative example 2 were evaluated. Soluble powder formulation appeared stable and remained as such in accelerated heat storage (AHS) study conducted at 54°C for 14 days. The active content of both active ingredients, i.e. acephate and imidacloprid remained quite stable in composition according to example 3. Moisture content remained below 1 in both ambient as well as AHS. The powder of the composition exhibited excellent wettability profile with wetting time as 15 seconds in ambient and 10 seconds in AHS. The detailed evaluation can be provided as in Table 7 below
Table 7
Parameters Example 3 Comparative example 2
0 days 14 days AHS 0 days 14 days AHS
Acephate (%w/w) 52.05 50.42 51.85 45.1
Imidacloprid (%w/w) 2.01 1.86 1.92 0.56
Degradation of Acephate 3.13% 13.02%
Degradation of Imidacloprid 7.46% 70.83%
wettability
(in sec) 15 10 30 25
pH 1% aqueous solution 5.5 4.35 5.3 2.84
moisture content (%w/w) 0.38 0.4 0.39 1.9
The inventors of the present invention successfully developed solid compositions in the form of soluble powder formulation of acephate and imidacloprid by encapsulating imidacloprid according to present invention. The stable solid compositions according to present invention demonstrated about 60% less degradation for imidacloprid and about 10% less degradation for acephate as compared to composition prepared without encapsulation of imidacloprid. The active ingredients were found to remain quite stable after preparation and even during storage studies.
,CLAIMS:
1. A solid composition comprising:
i) particles of a first active ingredient encapsulated in alkylated melamine -formaldehyde crosslinked polymer having low degree of alkylation;
ii) a second active ingredient; and
iii) at least one agrochemically acceptable excipient;
wherein either one or both active ingredient(s) are susceptible to degradation.
2. The composition as claimed in claim 1, wherein the first active ingredient is selected from an insecticide or an herbicide.
3. The composition as claimed in claim 2, wherein the insecticide is a neonicotinoid insecticide selected from the group comprising of acetamiprid, clothianidin, dinotefuran, imidacloprid, nitenpyram, thiacloprid or thiamethoxam; and the herbicide is a sulfonylurea herbicide selected from the group comprising of halosulfuron, bensulfuron methyl, chlorsulfuron, ethametsulfuron methyl, foramsulfuron, mesosulfuron methyl, metsulfuron methyl, nicosulfuron, oxasulfuron, primisulfuron methyl, prosulfuron, rimsulfuron, sulfometuron methyl, sulfosulfuron, thifensulfuron methyl, triasulfuron or triflusulfuron methyl.
4. The composition as claimed in claim 1, wherein the alkylated melamine -formaldehyde crosslinked polymer is formed by self-condensation of a prepolymer of formula (I)
Formula (I)
wherein R is hydrogen or C1 to C5 alkyl group.
5. The composition as claimed in claim 4, wherein the alkylated melamine -formaldehyde crosslinked polymer is methylated melamine -formaldehyde crosslinked polymer.
6. The composition as claimed in claim 1, wherein the ratio of the alkylated melamine -formaldehyde crosslinked polymer to the first active ingredient in the encapsulated particle is in the range of about 1: 10 to 1: 100.
7. The composition as claimed in claim 1, wherein the encapsulated particles further comprises an anionic surfactant selected from group comprising of anionic derivatives of fatty alcohols having 10-24 carbon atoms in the form of ether carboxylates, sulfonates, sulfates, and phosphates, and their inorganic salts and organic salts; anionic derivatives of copolymers consisting of ethylene oxide (EO), propylene oxide (PO) and/or butylene oxide (BO) units, in the form of ether carboxylates, sulfonates, sulfates, and phosphates, and their inorganic salts and organic salts, derivatives of alkylene oxide adducts of alcohols, in the form of ether carboxylates, sulfonates, sulfates and phosphates, and their inorganic salts and organic salts; derivatives of fatty acid alkoxylates, in the form of ether carboxylates, sulfonates, sulfates and phosphates, and their inorganic salts and organic salts, alkyl ether phosphate, alkyl sulfate and its salts, alkyl sulfosuccinate mono ester and diester salts, olefin sulfonic acid salts; derivatives of lignin, in form of sulfonates, phenolic, organosolv, kraft and its salts; or combinations thereof.
8. The composition as claimed in claim 1, wherein the second active ingredient is selected from group comprising of insecticides, herbicides, fungicides, nematicides, fertilizers, pheromones, plant-growth regulators, or nutrients.
9. The composition as claimed in claim 1, wherein the first and second active ingredients both are insecticides.
10. The composition as claimed in claim 9, wherein the first active ingredient is a neonicotinoid insecticide and the second active ingredient is an organophosphate insecticide.
11. The composition as claimed in claim 1, wherein the first and second active ingredients both are herbicides.
12. The composition as claimed in claim 1, wherein the composition further comprises a third active ingredient.
13. The composition as claimed in claim 12, wherein the first active ingredient is selected from a sulfonylurea herbicide; second active ingredient is selected from a triazine herbicide; and third active ingredient is selected from a triketone herbicide.
14. The composition as claimed in claim 1, wherein the agrochemically acceptable excipient is carrier selected from group comprising minerals like clay such as china clay, acid clay, kaolin such as kaolinite, dickite, nacrite, and halloysite, serpentines such as chrysotile, lizardite, antigorite, and amesite, synthetic and diatomaceous silicas, precipitated silica, colloidal silica, attapulgite, bentonite, white carbon black, dolomite, montmorillonite minerals such as sodium montmorillonite, smectites, such as saponite, hectorite, sauconite, and hyderite, micas, such as pyrophyllite, talc, agalmatolite, muscovite, phengite, sericite, and illite, silicas such as cristobalite and quartz, such as sepiolite; vermiculite, laponite, pumice, bauxite, hydrated aluminas, perlite, sodium bicarbonate, volclay, vermiculites, limestone, natural and synthetic silicates, charcoal, silicas, wet process silicas, dry process silicas, calcined products of wet process silicas, surface-modified silicas, mica, zeolite, diatomaceous earth, derivatives thereof; chalks, fuller's earth, loess, mirabilite, white carbon, slaked lime, synthetic silicic acid, starch, modified starch, cellulose, plant carriers such as cellulose, chaff, wheat flour, wood flour, starch, rice bran, wheat bran, and soyabean flour, casein sodium, sucrose, salt cake, ammonium sulphate, dibasic ammonium phosphate, potassium pyrophosphate, sodium tripolyphosphate, their derivatives, or combinations thereof.
15. A solid composition comprising;
i) 0.1% w/w to about 25% w/w encapsulated particles of first active ingredient selected from sulfonylurea herbicides or neonicotinoid insecticides;
ii) about 1% w/w to about 90% w/w second active ingredient; and
iii) an agrochemically acceptable excipient;
wherein either one or both active ingredient(s) are susceptible to degradation; and wherein the first active ingredient is encapsulated in an alkylated melamine -formaldehyde crosslinked polymer having low degree of alkylation.
16. The solid composition as claimed in claim 15, optionally comprises a third active ingredient in an amount of about 0.1% w/w to about 20% w/w of the total weight of the solid composition.
17. A soluble powder formulation comprising
i) from about 0.1% w/w to about 10% w/w imidacloprid encapsulated in an alkylated melamine -formaldehyde crosslinked polymer having low degree of alkylation;
ii) about 10% w/w to about 80% w/w acephate; and
iii) at least one agrochemically acceptable excipient.
18. A water dispersible granular (WDG) formulation comprising
i) from about 0.1% w/w to about 10% w/w halosulfuron-methyl encapsulated in an alkylated melamine -formaldehyde crosslinked polymer having a low degree of alkylation;
ii) from about 10% w/w to about 80% w/w atrazine;
iii) from about 0.1% w/w to about 20% w/w topramezone; and
iv) at least one agrochemically acceptable excipient.
19. An encapsulated particle comprising a first active ingredient; an alkylated melamine -formaldehyde crosslinked polymer having a low degree of alkylation; and an anionic surfactant.
20. The encapsulated particle as claimed in claim 19, comprise first active ingredient having particle size (D90) in range of 3 microns to about 30 microns.
21. A process for preparing a solid composition comprising:
a) preparing encapsulated particles comprising first active ingredient and an alkylated melamine -formaldehyde crosslinked polymer having a low degree of alkylation; and
b) mixing the encapsulated particles with a second active ingredient and agrochemically acceptable excipient (s).
22. The process as claimed in claim 21, wherein the encapsulated particles comprise first active ingredient; alkylated melamine -formaldehyde crosslinked polymer having a low degree of alkylation; and an anionic surfactant.
23. The process as claimed in claim 21, wherein the step a) of the process comprises
i) mixing the first active ingredient with the anionic surfactant;
ii) milling the mixture obtained in step i) to particle size (D90) in range of 3 microns to about 30 microns; and
iii) encapsulating the mixture obtained in step ii) with an alkylated melamine -formaldehyde crosslinked polymer having a low degree of alkylation.
24. The process as claimed in claim 21, wherein the step a) of the process also involves a step of formation of alkylated melamine -formaldehyde crosslinked polymer comprising self-condensation of a prepolymer of formula (I).
Formula (I)
wherein R is hydrogen or C1 to C5 alkyl group.
25. The process as claimed in claim 21, wherein the step b) comprises additional active ingredient(s).
26. A method of controlling undesired pest(s) by applying to the plants/pest or to their locus/environment, an effective amount of the solid composition, comprising
i) particles of a first active ingredient encapsulated in alkylated melamine -formaldehyde crosslinked polymer having a low degree of alkylation;
ii) a second active ingredient; and
iii) at least one agrochemically acceptable excipient;
wherein either one or both active ingredient(s) are susceptible to degradation.
| # | Name | Date |
|---|---|---|
| 1 | 202421025070-STATEMENT OF UNDERTAKING (FORM 3) [28-03-2024(online)].pdf | 2024-03-28 |
| 2 | 202421025070-PROVISIONAL SPECIFICATION [28-03-2024(online)].pdf | 2024-03-28 |
| 3 | 202421025070-POWER OF AUTHORITY [28-03-2024(online)].pdf | 2024-03-28 |
| 4 | 202421025070-FORM 1 [28-03-2024(online)].pdf | 2024-03-28 |
| 5 | 202421025070-Proof of Right [26-04-2024(online)].pdf | 2024-04-26 |
| 6 | 202421025070-REQUEST FOR CERTIFIED COPY [11-09-2024(online)].pdf | 2024-09-11 |
| 7 | 202421025070-Response to office action [23-09-2024(online)].pdf | 2024-09-23 |
| 8 | 202421025070-CORRESPONDENCE(IPO)-(CERTIFIED LATTER)-09-10-2024.pdf | 2024-10-09 |
| 9 | 202421025070-FORM-5 [28-03-2025(online)].pdf | 2025-03-28 |
| 10 | 202421025070-FORM 18 [28-03-2025(online)].pdf | 2025-03-28 |
| 11 | 202421025070-COMPLETE SPECIFICATION [28-03-2025(online)].pdf | 2025-03-28 |
| 12 | 202421025070-Covering Letter [15-04-2025(online)].pdf | 2025-04-15 |
| 13 | 202421025070-Response to office action [18-09-2025(online)].pdf | 2025-09-18 |