Immediate Release Pesticide Formulations

Abstract

The present invention relates to an agricultural chemical tablet comprising an agricultural chemical active ingredient, a bulking agent having a water solubility of 10-250 g / 100 ml, and a disintegrant. The present invention can provide an agricultural chemical tablet that can minimize the risk of a user being exposed to the agricultural chemical due to scattering and dust generation, eliminate the inconvenience of having to weigh the product every time because the weight of each tablet is fixed, prevent misuse and abuse of the agricultural chemical due to the difficulty of weighing the agricultural chemical, and solve the trouble of collecting the packaging material of the used agricultural chemical.

Description

[Technical field]

[0001] The present invention relates to a dilute pesticide tablet that maximizes the safety of pesticide users, the convenience of use, and the profits of pesticide producers. [Background technology]

[0002] Representative methods of diluting and spraying pesticides include sprayers that put 20 liters of water in a container and spray while the user is carrying it on his / her back, high-pressure sprayers that dilute the pesticide with 500 liters of water and spray it using high-pressure power, and riding SS (speed spray) sprayers and drones used in orchards. With the above sprayers, water is put into a container of a specific volume (20 liters to 2,000 liters) and the pesticide is diluted according to the dilution rate before use. However, solid pesticides such as wettable powders and granular wettable powders can cause safety problems for workers due to problems with scattering and dust.

[0003] The pesticide tablets currently used around the world are effervescent tablets made by combining organic acids, carbonates, and other ingredients, which, when added to water, produce carbon dioxide gas, which causes the tablet to disintegrate and the pesticide ingredients to diffuse. Conventional effervescent tablets take a fairly long time, about 5 to 15 minutes, to completely dissolve or disperse in water.

[0004] In addition, effervescent tablets have the problem that when they come into contact with moisture in the air during storage, they release carbon dioxide gas, causing a decline in product performance. For example, even if the tablet is wrapped in a water-soluble film, moisture may penetrate into the packaging during storage, causing a decline in product performance. After a certain period of time, products that have reached their expiration date cannot be reprocessed and must be discarded in their entirety. To solve this problem, methods are used to suppress contact with moisture in the air, such as coating organic acids and carbonates with effervescent functions with binders; however, the manufacturing method is complicated, leading to increased manufacturing costs.

[0005] Therefore, there is a need for a specific method for significantly shortening the disintegration and / or dispersion time of effervescent tablets, maintaining tableting ease and storage stability, while at the same time ensuring good fineness and suspension in pesticide spray containers. [Prior art documents] [Patent documents]

[0006] [Patent Document 1] Korean Patent No. 10-0994183 Summary of the Invention [Problem to be solved by the invention]

[0007] Disclosure of the Invention technical challenges The object of the present invention is to provide a pesticide tablet which minimizes the risk of exposure of users to pesticides due to scattering and dust generation of conventional solid pesticide formulations, eliminates the inconvenience of having to weigh the product every time since the weight of each tablet is fixed, eliminates the cause of misuse and abuse of pesticides due to the difficulty in weighing the pesticide, and eliminates the trouble of collecting packaging materials for used pesticides. [Means for solving the problem]

[0008] Solutions to the challenges In order to achieve the above object, an embodiment of the present invention provides an agrochemical tablet comprising: an agrochemical active ingredient; a filler having a water solubility of 10 to 250 g / 100 ml; and a disintegrant.

[0009] Another embodiment of the present invention provides a method for producing an agrochemical tablet, comprising: mixing an agrochemically active ingredient and a first filler and grinding them to prepare a first mixture; mixing the first mixture, a second filler, and a disintegrant to prepare a second mixture; and compressing the second mixture into a tablet, wherein each of the first filler and the second filler has a water solubility of 10-250 g / 100 ml. Effect of the Invention

[0010] Advantageous Effects of the Invention The pesticide tablet according to the present invention is commercially useful as a tablet that disintegrates or disperses in water within 60 seconds after being added to water.In addition, it can minimize the risk of users being exposed to pesticides due to scattering and dust generation of conventional solid pesticide formulations, eliminate the inconvenience of having to measure the product every time because the weight of each tablet is fixed, eliminate the cause of misuse and abuse of pesticides due to the difficulty of measuring the pesticide, and eliminate the trouble of collecting the packaging material of used pesticides, thereby solving various problems arising from the use of conventional pesticides at once. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS

[0011] BEST MODE FOR CARRYING OUT THEINVENTION Various embodiments are described below in detail to enable those skilled in the art to easily practice the present invention, however, the embodiments may be embodied in several different forms and are not limited to the embodiments described herein.

[0012] In this specification, when a moiety is referred to as "comprising" an element, unless otherwise specified, it is understood that the moiety can include other elements as well.

[0013] In this specification, the singular terms "a," "an," and "the" are to be construed as covering the singular or plural as the context requires, unless otherwise indicated.

[0014] Furthermore, all numbers and expressions, such as amounts of ingredients, reaction conditions, and the like, used herein are understood to be modified by the term "about" unless otherwise specified.

[0015] In this specification, terms such as first and second are used to describe various components, and the components should not be limited by the terms. The terms are used only to distinguish one component from another component.

[0016] One embodiment of the present invention provides an agrochemical tablet comprising: an agrochemically active ingredient; a filler having a water solubility of 10 to 250 g / 100 ml; and a disintegrant.

[0017] The pesticide active ingredient may be an insecticide, acaricide, nematicide, fungicide, herbicide, insect growth regulator, or herbicidal plant growth regulator. Further, the pesticide active ingredient may include a water-insoluble pesticide ingredient or a water-soluble pesticide ingredient.

[0018] The term "tablet" in this invention includes what is considered in the art to be a tablet, including solid compressed forms such as briquettes and pellets.

[0019] The tablets have good dispersibility in water and good storage stability.

[0020] In certain embodiments of the present invention, the tablet contains an agricultural active ingredient for use in crops, homes, gardens, or lawns. In such cases, it may further contain other ingredients, such as fertilizers.

[0021] In a particular embodiment of the present invention, the pesticidal active ingredient is selected from the group consisting of glufosinate P, MCPA, glyphosate, oxolinic acid, flucetosulfuron, dymron, mefenacet, pyrazosulfuron ethyl, imazosulfuron, oxaziclomefone, penoxsulam, pretilachlor, mesotrione, pyriftalid, bensulfuron methyl, thiobencarb, indanofan, pyriminobac methyl, oxaziclomefone, carfentrazone ethyl, fentrazamide, pyributicarb, benzobicyclon, metamifop, benfuresate, cyclosulfamuron, anilofos, azimsulfuron, pyrazolate, metazosulfuron, orysastrobin, isoprothiolane, carpropamid, fludioxonil, tiadinil, It may be at least one selected from the group consisting of, but is not limited to, tricyclazole, thifluzamide, probenazole, fthalide, difenoconazole, propiconazole, validamycin, azoxystrobin, edifenphos, fenoxanil, acibenzolar S-methyl, ferimzone, pencycuron, hexaconazole, diazinon, dinotefuran, etofenprox, methoxyfenozide, bensultap, clothianidin, buprofezin, isoprocarb, fenobucarb, benfuracarb, imidacloprid, carbofuran, carbosulfan, cartap, thiamethoxam, tebufenozide, fenobucarb, phenthoate, fipronil, and chlorantraniliprole.

[0022] In another specific embodiment of the present invention, the content of the pesticide active ingredient may be 10 to 80 parts by weight based on 100 parts by weight of the pesticide tablet. Specifically, the content of the pesticide active ingredient may be 10 parts by weight or more, 13 parts by weight or more, 16 parts by weight or more, 19 parts by weight or more, or 22 parts by weight or more based on 100 parts by weight of the pesticide tablet, and 80 parts by weight or less, 75 parts by weight or less, 70 parts by weight or less, 65 parts by weight or less, 60 parts by weight or less, 55 parts by weight or less, 50 parts by weight or less, 45 parts by weight or less, or 40 parts by weight or less based on 100 parts by weight of the pesticide tablet. More specifically, the content of the pesticide active ingredient may be 13 to 75 parts by weight, 16 to 70 parts by weight, 19 to 65 parts by weight, 22 to 60 parts by weight, 22 to 55 parts by weight, 22 to 50 parts by weight, 22 to 45 parts by weight, or 22 to 40 parts by weight based on 100 parts by weight of the pesticide tablet, but is not limited to these numerical ranges.

[0023] When the content of the pesticide active ingredient is outside the above range, there is a problem in that it is difficult to exert the desired efficacy of the tablet.On the other hand, when the content of the pesticide active ingredient is within the above range, it can disperse and disintegrate in water within a desired time and exert excellent pesticide efficacy.

[0024] The bulking agent can be at least one selected from the group consisting of, but is not limited to, calcium carbonate, sodium carbonate, lactose, maltose, sucrose, xylose, sorbitol, glucose, ammonium sulfate, ammonium chloride, sodium chloride, urea, potassium sulfate, potassium formate, sodium sulfate, potassium chloride, citric acid, succinic acid, tartaric acid, and maleic acid.

[0025] In a specific embodiment of the present invention, the content of the extender may be 10 to 80 parts by weight based on 100 parts by weight of the agrochemical tablet. Specifically, the content of the extender may be 10 parts by weight or more, 15 parts by weight or more, 18 parts by weight or more, 21 parts by weight or more, 24 parts by weight or more, or 25 parts by weight or more based on 100 parts by weight of the agrochemical tablet, and 80 parts by weight or less, 75 parts by weight or less, 70 parts by weight or less, 67 parts by weight or less, 64 parts by weight or less, 61 parts by weight or less, or 58 parts by weight or less based on 100 parts by weight of the agrochemical tablet. More specifically, the content of the extender may be 18 to 67 parts by weight, 21 to 64 parts by weight, 24 to 61 parts by weight, or 25 to 58 parts by weight based on 100 parts by weight of the agrochemical tablet, but is not limited to these numerical ranges.

[0026] When the content of the filler is outside the above range, the tablet disintegration and dispersion time is long, or the hardness is too high or low, making it difficult to commercialize the tablet.On the other hand, when the content of the filler meets the above range, the tablet has the disintegration and dispersion time that maximizes its effect, and can produce a product with appropriate hardness.

[0027] In another specific embodiment of the present invention, the bulking agent may have a water solubility of 10 to 250 g / 100 ml.Specifically, the water solubility of the bulking agent may be 10 g / 100 ml or more, 11 g / 100 ml or more, 12 g / 100 ml or more, 15 g / 100 ml or more, or 20 g / 100 ml or more, and 250 g / 100 ml or less, 230 g / 100 ml or less, 210 g / 100 ml or less, 190 g / 100 ml or less, 170 g / 100 ml or less, 150 g / 100 ml or less, 130 g / 100 ml or less, 120 g / 100 ml or less, 110 g / 100 ml or less, 100 g / 100 ml or less, or 80 g / 100 ml or less. More specifically, the water solubility of the bulking agent may be, but is not limited to, 10 to 230 g / 100 ml, 10 to 210 g / 100 ml, 10 to 190 g / 100 ml, 10 to 170 g / 100 ml, 10 to 150 g / 100 ml, 11 to 150 g / 100 ml, 10 to 130 g / 100 ml, 11 to 130 g / 100 ml, 10 to 120 g / 100 ml, 11 to 120 g / 100 ml, 10 to 110 g / 100 ml, or 11 to 110 g / 100 ml.

[0028] When the water solubility of the filler is outside the above range, there is a problem in that the tablet disintegration and dispersion time is extended or the storage stability is significantly reduced. On the other hand, when the water solubility of the filler is within the above range, the tablet disintegration and dispersion time can be shortened and the storage stability of the product can be improved.

[0029] In another specific embodiment of the present invention, the content of at least one selected from the group consisting of ammonium sulfate, ammonium chloride, sodium chloride, potassium chloride, potassium sulfate, potassium formate, and urea contained in the extender may be 30 to 100 parts by weight based on 100 parts by weight of the extender. Specifically, the content of at least one selected from the group consisting of ammonium sulfate, ammonium chloride, sodium chloride, potassium chloride, potassium sulfate, potassium formate, and urea may be 30 parts by weight or more, 34 parts by weight or more, 38 parts by weight or more, 42 parts by weight or more, or 45 parts by weight or more, and 100 parts by weight or less, based on 100 parts by weight of the extender. More specifically, the content of at least one selected from the group consisting of ammonium sulfate, ammonium chloride, sodium chloride, potassium chloride, potassium sulfate, potassium formate, and urea may be 30 to 100 parts by weight, 34 to 100 parts by weight, 38 to 100 parts by weight, 42 to 100 parts by weight, or 45 to 100 parts by weight based on 100 parts by weight of the extender, but is not limited to these numerical ranges.

[0030] In another specific embodiment of the present invention, the content of at least one selected from the group consisting of ammonium sulfate, ammonium chloride, sodium chloride, potassium chloride, potassium sulfate, potassium formate, and urea may be 10 to 80 parts by weight based on 100 parts by weight of the agrochemical tablet. Specifically, the content of at least one selected from the group consisting of ammonium sulfate, ammonium chloride, sodium chloride, potassium chloride, potassium sulfate, potassium formate, and urea may be 10 parts by weight or more, 15 parts by weight or more, 18 parts by weight or more, or 20 parts by weight or more, and 80 parts by weight or less, 75 parts by weight or less, 70 parts by weight or less, 65 parts by weight or less, or 60 parts by weight or less based on 100 parts by weight of the agrochemical tablet. More specifically, the content of at least one selected from the group consisting of ammonium sulfate, ammonium chloride, sodium chloride, potassium chloride, potassium sulfate, potassium formate, and urea may be 10 to 75 parts by weight, 15 to 70 parts by weight, 18 to 65 parts by weight, or 20 to 60 parts by weight based on 100 parts by weight of the pesticide tablet, but is not limited to these numerical ranges.

[0031] When the content of at least one selected from the group consisting of ammonium sulfate, ammonium chloride, sodium chloride, potassium chloride, potassium sulfate, potassium formate, and urea is within the above range, the tablet has a disintegration and dispersion time that maximizes its effect, and a product with appropriate hardness can be produced.

[0032] In another specific embodiment of the present invention, the tablet may further comprise at least one effervescent filler selected from the group consisting of sodium bicarbonate and anhydrous ammonium alum. In such a case, the tablet may be an effervescent pesticide tablet. The effervescent pesticide tablet may essentially comprise at least one effervescent filler selected from the group consisting of sodium carbonate and sodium bicarbonate. The effervescent pesticide tablet may comprise at least one effervescent filler selected from the group consisting of sodium carbonate and sodium bicarbonate in an amount of 10-40 parts by weight, 10-30 parts by weight, 15-30 parts by weight, or 15-25 parts by weight based on 100 parts by weight of the effervescent pesticide tablet, but is not limited to these numerical ranges.

[0033] The disintegrant may be at least one selected from the group consisting of, but is not limited to, combinations of carbonates and solid acids, agar, starch, hydroxypropyl starch, sodium alginate, carboxymethyl starch ether, gum arabic, tragacanth, gelatin, casein, crystalline cellulose, carboxymethylcellulose calcium, sodium laurate, carboxyl resin, croscarmellose sodium, sodium starch glycolate, polyvinylpolypyrrolidone, ammonium sulfate, potassium chloride, table salt, urea, anionic surfactants, ammonium chloride, calcium chloride, magnesium chloride, aluminum chloride, glucose, lactose, sodium glutamate, sodium inosinate, and dextrin.

[0034] In a specific embodiment of the present invention, the content of the disintegrant may be 3.5 parts by weight or more or 3.5 to 40 parts by weight based on 100 parts by weight of the filler (relative to 100 parts by weight of the filler). Specifically, the content of the disintegrant may be 3.6 parts by weight or more, 3.7 parts by weight or more, 3.8 parts by weight or more, 3.9 parts by weight or more, or 4.0 parts by weight or more, and 40 parts by weight or less, 35 parts by weight or less, 30 parts by weight or less, or 25 parts by weight or less, based on 100 parts by weight of the filler. More specifically, the content of the disintegrant may be 3.6 to 35 parts by weight, 3.7 to 35 parts by weight, 3.8 to 30 parts by weight, 3.9 to 30 parts by weight, or 4.0 to 25 parts by weight based on 100 parts by weight of the filler, but is not limited to these numerical ranges.

[0035] In another specific embodiment of the present invention, the content of the disintegrant may be 3 parts by weight or more or 3 to 20 parts by weight based on 100 parts by weight of the pesticide tablet. Specifically, the content of the disintegrant may be 3.5 parts by weight or more, 4 parts by weight or more, 4.5 parts by weight or more, or 5 parts by weight or more, and 20 parts by weight or less, 17 parts by weight or less, 14 parts by weight or less, 11 parts by weight or less, or 8 parts by weight or less, based on 100 parts by weight of the pesticide tablet. More specifically, the content of the disintegrant may be 3.5 to 17 parts by weight, 4 to 14 parts by weight, 4.5 to 11 parts by weight, 5 to 8 parts by weight, or 3.5 to 6.5 parts by weight based on 100 parts by weight of the pesticide tablet, but is not limited to these numerical ranges.

[0036] In another specific embodiment of the present invention, the content of the disintegrant may be 5 parts by weight or more or 5 to 80 parts by weight based on 100 parts by weight of the pesticide active ingredient (relative to 100 parts by weight of the pesticide active ingredient). Specifically, the content of the disintegrant may be 6 parts by weight or more, 7 parts by weight or more, or 8 parts by weight or more, and 80 parts by weight or less, 70 parts by weight or less, 60 parts by weight or less, 50 parts by weight or less, 40 parts by weight or less, or 30 parts by weight or less, based on 100 parts by weight of the pesticide active ingredient. More specifically, the content of the disintegrant may be 5 to 70 parts by weight, 5 to 60 parts by weight, 6 to 50 parts by weight, 7 to 40 parts by weight, or 8 to 30 parts by weight based on 100 parts by weight of the pesticide active ingredient, but is not limited to these numerical ranges.

[0037] If the content of the disintegrant is outside the above range, problems arise in that the time required for disintegration and dispersion of the tablet becomes long or the storage stability is significantly reduced.

[0038] In another specific embodiment of the present invention, the bulking agent may be ammonium chloride, and the content of the disintegrant may be 8 to 40 parts by weight based on 100 parts by weight of ammonium chloride (relative to 100 parts by weight of ammonium chloride). Specifically, the content of the disintegrant may be 8 parts by weight or more, 8.5 parts by weight or more, or 9 parts by weight or more, and 40 parts by weight or less, 35 parts by weight or less, 32 parts by weight or less, 30 parts by weight or less, or 28 parts by weight or less, based on 100 parts by weight of ammonium chloride. More specifically, the content of the disintegrant may be 8.5 to 35 parts by weight, 8.5 to 32 parts by weight, 9 to 30 parts by weight, or 9 to 28 parts by weight based on 100 parts by weight of ammonium chloride, but is not limited to these numerical ranges.

[0039] In another specific embodiment of the present invention, the disintegrant may be polyvinylpolypyrrolidone, and the content of the filler may be 2,857 parts by weight or less or 250 to 2,857 parts by weight based on 100 parts by weight of polyvinylpolypyrrolidone (relative to 100 parts by weight of polyvinylpolypyrrolidone). Specifically, the content of the filler may be 250 parts by weight or more, 350 parts by weight or more, 450 parts by weight or more, 550 parts by weight or more, or 650 parts by weight or more, and 2,500 parts by weight or less, 2,200 parts by weight or less, 1,800 parts by weight or less, 1,500 parts by weight or less, or 1,250 parts by weight or less, based on 100 parts by weight of polyvinylpolypyrrolidone. More specifically, the content of the extender may be 350 to 2,500 parts by weight, 450 to 2,200 parts by weight, 540 to 1,500 parts by weight, 550 to 1,350 parts by weight, or 555 to 1,250 parts by weight based on 100 parts by weight of polyvinylpolypyrrolidone, but is not limited to these numerical ranges.

[0040] In certain embodiments of the present invention, the pesticide tablet may further comprise at least one additive selected from the group consisting of surfactants, binders, and lubricants.

[0041] Surfactants have the function of assisting the diffusion of the pesticide active ingredient in water and good adhesion to crops and the like, and can also function as a binder or disintegrant (for example, to increase the strength of the pesticide composition).

[0042] Specifically, the surfactant may be a fatty acid salt, an alkyl sulfosuccinate, a dialkyl sulfosuccinate, a polycarboxylate, an alkyl sulfate ester salt, an alkyl sulfate, an alkyl aryl sulfate, an alkyl diglycol ether sulfate, an alcohol sulfate ester salt, an alkyl sulfonate, an alkyl aryl sulfonate, an aryl sulfonate, a lignin sulfonate, an alkyl diphenyl ether disulfonate, a polystyrene sulfonate, an alkyl phosphate ester salt, an alkyl aryl phosphate, a styryl aryl phosphate, a polyoxyethylene alkyl ether sulfate ester salt, a polyoxyethylene alkyl aryl ether sulfate, a polyoxyethylene alkyl ether sulfate ester salt, a polyoxyethylene alkyl ether phosphate, a polyoxyethylene alkyl aryl phosphate ester, a naphthalene sulfonate formalin condensation product, The surfactant may be an anionic surfactant such as a salt of a carboxylic acid ...

[0043] In a specific embodiment of the present invention, the content of the surfactant may be 1 to 30 parts by weight based on 100 parts by weight of the extender (relative to 100 parts by weight of the extender). Specifically, the content of the surfactant may be 1 part by weight or more, 5 parts by weight or more, 10 parts by weight or more, or 15 parts by weight or more, and 30 parts by weight or less, 25 parts by weight or less, or 20 parts by weight or less, based on 100 parts by weight of the extender. More specifically, the content of the surfactant may be 5 to 25 parts by weight, 10 to 25 parts by weight, 10 to 20 parts by weight, 15 to 25 parts by weight, or 15 to 20 parts by weight, based on 100 parts by weight of the extender, but is not limited to these numerical ranges.

[0044] In another specific embodiment of the present invention, the content of the surfactant may be 1 to 30 parts by weight based on 100 parts by weight of the agrochemical tablet. Specifically, the content of the surfactant may be 1 part by weight or more, 2 parts by weight or more, 3 parts by weight or more, or 4 parts by weight or more based on 100 parts by weight of the agrochemical tablet, and 30 parts by weight or less, 25 parts by weight or less, 20 parts by weight or less, or 15 parts by weight or less based on 100 parts by weight of the agrochemical tablet. More specifically, the content of the surfactant may be 2 to 25 parts by weight, 3 to 20 parts by weight, or 4 to 15 parts by weight based on 100 parts by weight of the agrochemical tablet, but is not limited to these numerical ranges.

[0045] Binders may function to control tablet hardness.

[0046] Specifically, the binder can be various gums such as guar gum, locust bean gum, tragacanth gum, xanthan gum, and gum arabic; alginic acid derivatives such as sodium alginate, ammonium alginate, and propylene glycol alginate; organic polymer compounds such as polyvinyl alcohol, polyvinyl methacrylate, polyethylene oxide, polyacrylic acid, sodium polyacrylate, and polyacrylic acid amide; animal or vegetable water-soluble proteins such as egg white, albumin, casein, and gelatin; cellulose derivatives such as methylcellulose, carboxymethylcellulose, sodium carboxymethylcellulose, carboxyethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, and hydroxypropylmethylcellulose; starches such as dextrin, starch, sodium carboxymethyl starch, hydroxyethyl starch, and hydroxypropyl starch; or lignin sulfonic acid derivatives such as sodium lignin sulfonate and calcium lignin sulfonate. These can be used alone or in combination of two or more of them. When mixing these, the ratio can also be appropriately selected. Some of these also function as disintegrants.More specifically, binders can include, but are not limited to, hydroxypropyl methylcellulose.

[0047] In a specific embodiment of the present invention, the content of the binder may be 1 to 20 parts by weight based on 100 parts by weight of the extender (relative to 100 parts by weight of the extender). Specifically, the content of the binder may be 1 part by weight or more, 3 parts by weight or more, 5 parts by weight or more, or 7 parts by weight or more, and 20 parts by weight or less, 15 parts by weight or less, 13 parts by weight or less, or 11 parts by weight or less, based on 100 parts by weight of the extender. More specifically, the content of the binder may be 3 to 15 parts by weight, 5 to 13 parts by weight, or 7 to 11 parts by weight based on 100 parts by weight of the extender, but is not limited to these numerical ranges.

[0048] In a specific embodiment of the present invention, the content of the binder may be 1 to 20 parts by weight based on 100 parts by weight of the agrochemical tablet. Specifically, the content of the binder may be 1 part by weight or more, 1.5 parts by weight or more, 2 parts by weight or more, 2.5 parts by weight or more, or 3 parts by weight or more based on 100 parts by weight of the agrochemical tablet, and 20 parts by weight or less, 16 parts by weight or less, 13 parts by weight or less, 10 parts by weight or less, or 7 parts by weight or less based on 100 parts by weight of the agrochemical tablet. More specifically, the content of the binder may be 1.5 to 16 parts by weight, 2 to 13 parts by weight, 2.5 to 10 parts by weight, or 3 to 7 parts by weight based on 100 parts by weight of the agrochemical tablet, but is not limited to these numerical ranges.

[0049] The lubricant may function to facilitate the flow of the filler.

[0050] Specifically, the lubricant may be polyethylene glycol, propylene glycol, glycerin ester, calcium stearate, magnesium stearate, talc, etc. These may be used alone or in combination of two or more thereof. When mixing these, the ratio may also be appropriately selected. More specifically, the lubricant may include, but is not limited to, magnesium stearate.

[0051] In another specific embodiment of the present invention, the content of the lubricant may be 0.1 to 5 parts by weight based on 100 parts by weight of the extender (relative to 100 parts by weight of the extender). Specifically, the content of the lubricant may be 0.1 parts by weight or more, 0.5 parts by weight or more, 1.0 parts by weight or more, or 1.5 parts by weight or more, and 5 parts by weight or less, 4 parts by weight or less, 3 parts by weight or less, or 2 parts by weight or less, based on 100 parts by weight of the extender. More specifically, the content of the lubricant may be 0.5 to 4 parts by weight, 1.0 to 3 parts by weight, or 1.5 to 2 parts by weight based on 100 parts by weight of the extender, but is not limited to these numerical ranges.

[0052] In another specific embodiment of the present invention, the content of the lubricant may be 0.1 to 5 parts by weight based on 100 parts by weight of the pesticide tablet. Specifically, the content of the lubricant may be 0.1 parts by weight or more, 0.2 parts by weight or more, 0.3 parts by weight or more, 0.4 parts by weight or more, or 0.5 parts by weight or more, and 5 parts by weight or less, 4 parts by weight or less, 3 parts by weight or less, 2 parts by weight or less, or 1 part by weight or less, based on 100 parts by weight of the pesticide tablet. More specifically, the content of the lubricant may be 0.2 to 4 parts by weight, 0.3 to 3 parts by weight, 0.4 to 2 parts by weight, or 0.5 to 1.5 parts by weight based on 100 parts by weight of the pesticide tablet, but is not limited to these numerical ranges.

[0053] When the contents of the surfactant, binder, and lubricant are outside the above ranges, there may be problems in terms of tablet hardness and production efficiency of the product.

[0054] In certain embodiments of the present invention, the tablet may have a disintegration and dispersion time of 60 seconds or less. Specifically, the disintegration and dispersion time of the tablet may be 60 seconds or less, 58 seconds or less, 56 seconds or less, 54 seconds or less, 52 seconds or less, 50 seconds or less, 48 ​​seconds or less, or 45 seconds or less, but is not limited to these numerical ranges.

[0055] For example, the disintegration and dispersion time of a tablet is measured by placing one tablet (5 grams) in a container, adding 10 liters of water at a temperature of about 22°C to the container, and measuring the time it takes for one tablet to completely disintegrate and disperse. In such a case, to determine whether the tablet has completely disintegrated and dispersed, 100 ml is taken from five random locations of the solution in which the tablet has disintegrated and dispersed, and the concentration of the five solution samples is measured. If the standard deviation is 25 mg / L or less, the tablet is evaluated as being completely disintegrated and dispersed.

[0056] When the tablet disintegration and dispersion times are within the above ranges, the tablet disintegrates in a short time in the pesticide spray container, which can shorten the working time of the worker and improve the efficiency of the tableting work. Furthermore, the pesticide active ingredient is uniformly dispersed in the spray container, which can achieve excellent efficacy.

[0057] In a specific embodiment of the present invention, the tablet may have a hardness of 50 to 200 Newtons (N). Specifically, the hardness of the tablet may be 50 N or more, 60 N or more, 70 N or more, 80 N or more, 90 N or more, or 100 N or more, and 200 N or less, 180 N or less, 160 N or less, 150 N or less, 140 N or less, or 130 N or less. More specifically, the hardness of the tablet may be 60 to 180 N, 70 to 160 N, 80 to 150 N, 90 to 140 N, or 100 to 130 N, but is not limited to these numerical ranges.

[0058] When the tablet hardness is within the above range, the storage stability can be maximized. On the other hand, when the tablet hardness is outside the above range, there are problems in terms of productivity and commercialization of the tablet.

[0059] The shape of the tablet may be, but is not limited to, cylindrical, square, polygonal, donut-shaped, or oval.

[0060] When the tablet is cylindrical, the average diameter may be 1.5 cm to 3 cm, specifically, 2 cm to 3 cm, but is not limited to these numerical ranges.

[0061] The mass of one tablet can be, but is not limited to, 3 grams to 20 grams, 3 grams to 15 grams, 3 grams to 10 grams, or 3 grams to 8 grams.

[0062] In a specific embodiment of the present invention, the tablet may have a suspension rate of 60 to 80%. Specifically, the suspension rate of the tablet may be 60% or more, 65% or more, or 70% or more. More specifically, the suspension rate of the tablet may be 65 to 80% or 70 to 80%, but is not limited to these numerical ranges.

[0063] If the suspension rate of the tablet is outside the above range, problems arise in terms of efficacy and physical properties.

[0064] In a specific embodiment of the present invention, the tablet may have a fineness of 95-100%. Specifically, the fineness of the tablet may be 95% or more, 96% or more, 97% or more, or 98% or more. More specifically, the fineness of the tablet may be 96-100%, 97-100%, or 98-100%, but is not limited to these numerical ranges.

[0065] When the powderiness of the tablet is out of the above range, it may cause the failure of the sprayer and there is a problem in terms of efficacy of the tablet.

[0066] The pesticide tablet according to the present invention is in the form of a tablet that disperses and disintegrates in a short time, which can minimize the risk of exposure of users to pesticides, and enables simple quantitative measurement, reducing the misuse and abuse of pesticides, and solving various problems caused by the use of conventional pesticides.

[0067] Furthermore, the above-mentioned pesticide tablet can be applied as a technology for incorporating useful fertilizers or ingredients into pesticide tablets in crop cultivation, so that it can be established as a technology for safe use, low labor input, and environmentally friendly crop cultivation.

[0068] Another embodiment of the present invention provides a method for producing an agricultural chemical tablet. Specifically, the method for producing an agricultural chemical tablet according to the present invention includes: mixing an agricultural chemical active ingredient and a first filler and grinding them to prepare a first mixture; mixing the first mixture, a second filler, and a disintegrant to prepare a second mixture; and compressing the second mixture into tablets, where each of the first filler and the second filler has a water solubility of 10 to 250 g / 100 ml.

[0069] In a specific embodiment of the present invention, the first bulking agent and the second bulking agent each have a water solubility of 10 to 250 g / 100 ml.Specifically, the water solubility of each of the first bulking agent and the second bulking agent can be 10 g / 100 ml or more or 11 g / 100 ml or more, and 250 g / 100 ml or less, 230 g / 100 ml or less, 210 g / 100 ml or less, 190 g / 100 ml or less, 170 g / 100 ml or less, 150 g / 100 ml or less, 130 g / 100 ml or less, 120 g / 100 ml or less, or 110 g / 100 ml or less. More specifically, the water solubility of each of the first bulking agent and the second bulking agent may be, but is not limited to, 10 to 230 g / 100 ml, 10 to 210 g / 100 ml, 10 to 190 g / 100 ml, 10 to 170 g / 100 ml, 10 to 150 g / 100 ml, 11 to 150 g / 100 ml, 10 to 130 g / 100 ml, 11 to 130 g / 100 ml, 10 to 120 g / 100 ml, 11 to 120 g / 100 ml, 10 to 110 g / 100 ml, or 11 to 110 g / 100 ml.

[0070] In the method for producing an agrochemical tablet according to the present invention, the descriptions of the first filler and the second filler are the same as those of the fillers in the agrochemical tablet, and the descriptions of the agrochemical active ingredient, the disintegrant, the surfactant, the binder, and the lubricant are the same as those of the agrochemical tablet.

[0071] In the method for producing an agrochemical tablet according to the present invention, first, a step of mixing an agrochemically active ingredient and a first filler and grinding them to prepare a first mixture is carried out.

[0072] The step of preparing the first mixture may further include adding an additive. The additive may be at least one selected from the group consisting of a surfactant, a binder, and a lubricant.

[0073] The grinding may be carried out by a dry grinding method.

[0074] The dry grinding method may be a method known as a general dry grinding method.

[0075] In the dry grinding, grinders such as a power mill, a coffee mill, a hammer mill, a pin mill, a jet mill, and a neer mill can be used, and an appropriate grinder can be selected according to the characteristics and purpose of the material to be ground. Specifically, a jet mill can be used.

[0076] The particles contained in the first mixture may have an average particle size of 5 to 30 microns. Specifically, the average particle size of the particles may be 5 to 25 microns, 5 to 20 microns, 5 to 15 microns, or 5 to 10 microns, but is not limited to these numerical ranges.

[0077] Next, the first mixture, a second filler, and a disintegrant are mixed to prepare a second mixture.

[0078] The step of preparing the second mixture may further include adding an additive. The additive may be at least one selected from the group consisting of a surfactant, a binder, and a lubricant.

[0079] The second mixture is then compressed into agrochemical tablets.

[0080] Tableting can be carried out using a general tablet manufacturing method.

[0081] The description of the pesticide tablet produced by the above-mentioned production method of the present invention is as described above. EXAMPLES

[0082] Form for the invention The present invention is described in detail below. However, the following test examples are for illustrative purposes and the scope of the present invention is not limited thereto.

[0083] Test Example 1: Manufacturing of non-effervescent pesticide tablets (1) 26 parts by weight of chlorantraniliprole (common name) as a pesticide active ingredient and 25 parts by weight of ammonium chloride as a first extender were mixed and ground to an average particle size of 8 microns or less, thereby preparing a first mixture. (2) 51 parts by weight of the first mixture; 7 parts by weight of naphthalene sulfonate and 2 parts by weight of propane sulfonate as surfactants; 10 parts by weight of urea and 19 parts by weight of ammonium chloride as second extenders; 5 parts by weight of hydroxypropylmethylcellulose as a binder; 5 parts by weight of polyvinylpolypyrrolidone as a disintegrant; and 1 part by weight of magnesium stearate as a lubricant were uniformly mixed to prepare a second mixture. (3) The second mixture was made into tablets with a diameter of 2.5 cm, a mass of 5 grams, and a hardness of 120 N (Newtons).

[0084] Test Examples 2-25: Manufacturing of non-foaming pesticide tablets In Test Examples 2 to 25, tablets were prepared in the same manner as Test Example 1, except that the pesticide active ingredient, the first filler, and the second filler were each prepared in the components and weight parts shown in Table 1 below. [Table 1-1] [Table 1-2] [Table 1-3]

[0085] Test Example 26: Production of effervescent pesticide tablets (1) 26 parts by weight of chlorantraniliprole (generic name) as a pesticide active ingredient; and 10 parts by weight of sodium carbonate and 15 parts by weight of sodium bicarbonate as a first extender were mixed and ground to an average particle size of 8 microns or less, thereby preparing a first mixture. (1)-2 15 parts by weight of tartaric acid was added as a first extender to the first mixture, which was then dried at about 70° C. for about 30 minutes with stirring to keep the moisture content below 1%, thereby preparing a second mixture. (2) 51 parts by weight of the second mixture; 7 parts by weight of naphthalene sulfonate and 2 parts by weight of propane sulfonate as surfactants; 14 parts by weight of ammonium chloride as a second filler; 5 parts by weight of hydroxypropylmethylcellulose as a binder; 5 parts by weight of polyvinylpolypyrrolidone as a disintegrant; and 1 part by weight of magnesium stearate as a lubricant were uniformly mixed to prepare a third mixture. (3) The third mixture was made into tablets with a diameter of 2.5 cm, a mass of 5 grams, and a hardness of 120 N (Newtons).

[0086] The components, water solubility, and parts by weight of each of the first and second bulking agents used in Test Example 26 are shown in Table 2 below. [Table 2]

[0087] Test Example 27: Production of effervescent pesticide tablets (1) 26 parts by weight of chlorantraniliprole (generic name) as a pesticide active ingredient; and 10 parts by weight of sodium carbonate and 15 parts by weight of sodium bicarbonate as a first extender were mixed and ground to an average particle size of 8 microns or less, thereby preparing a first mixture. (1)-2 15 parts by weight of tartaric acid was added as a first extender to the first mixture, which was then dried at about 70° C. for about 30 minutes with stirring to keep the moisture content below 1%, thereby preparing a second mixture. (2) 51 parts by weight of the second mixture; 7 parts by weight of naphthalene sulfonate and 2 parts by weight of propane sulfonate as surfactants; 14 parts by weight of anhydrous ammonium alum as a second extender; 5 parts by weight of hydroxypropylmethylcellulose as a binder; 5 parts by weight of polyvinylpolypyrrolidone as a disintegrant; and 1 part by weight of magnesium stearate as a lubricant were uniformly mixed to prepare a third mixture. (3) The third mixture was made into tablets with a diameter of 2.5 cm, a mass of 5 grams, and a hardness of 120 N (Newtons).

[0088] The components, water solubility, and parts by weight of each of the first and second bulking agents used in Test Example 27 are shown in Table 3 below. [Table 3]

[0089] Test Examples 28-30 In Test Examples 28 to 30, tablets were prepared in the same manner as Test Example 1, except that the first filler and the second filler were each prepared in the components and weight parts shown in Table 4 below. [Table 4]

[0090] Test Examples 31-34 In Test Examples 31 to 34, tablets were prepared in the same manner as Test Example 1, except that the first filler, second filler, binder, and disintegrant were each prepared in the components and weight parts shown in Table 5 below. [Table 5]

[0091] Evaluation example 1: Evaluation of powderiness According to the Pesticide Control Law's Pesticide Testing Method (Notice No. 1999-3 of the Rural Development Agency), in principle, pesticides whose main ingredients and extenders swell with water or are water-soluble shall be measured for powderiness by the dry method. Other pesticides shall be measured by the wet method. In the present invention, the wet method was used.

[0092] 1) 50 g of sample was placed in a 200 ml beaker, 60-80 ml of water was added to it, and the mixture was stirred well with a stir bar to disperse evenly. The sample was transferred onto a 325 mesh sieve.

[0093] 2) The remaining sample was transferred onto the sieve using 100 ml of water in the same manner. This procedure was repeated until the sample was completely transferred onto the sieve.

[0094] 3) Then, water was added little by little through the rubber tube, and the sieve was shaken horizontally to allow the sample to pass through. If necessary, it was lightly brushed. When it was confirmed that the discharged liquid contained almost no sample, the sample remaining on the sieve was combined and collected. The remaining sample was washed and transferred to a watch glass with a small amount of water and left to stand for a while. The supernatant was decanted and the sample was dried in a water bath, the residue was weighed, and the passing amount of the sample was calculated as a percentage. The results are shown in Table 6 below.

[0095] Evaluation example 2: Evaluation of suspension A gram of the active ingredient of the sample was placed in a beaker, and 50 ml of water at 20°C was added to it, and the mixture was thoroughly stirred to disperse evenly. It was transferred to a 250 ml stoppered graduated cylinder, and water at 20°C was added to make it 250 ml. After standing for 15 minutes, it was vigorously rotated 30 times per minute to mix well, and then stood for 5 minutes. Then, a 25 ml volumetric pipette was slowly placed in the liquid so that its tip was in the center of the liquid. 25 ml of the test liquid was gently taken, and the content of the active ingredient was measured (B grams). Alternatively, when it was impossible to analyze the active ingredient, the weight of the dried solid was weighed. The suspension rate was then calculated by the following formula:

number

[0096] Generally, a suspension rate of 70% or more is considered to be good, and a suspension rate of 75% or more is considered to be excellent.

[0097] The suspensibility (suspension rate) tested as described above is shown in Table 6 below.

[0098] Evaluation example 3: Evaluation of disintegration and dispersion time One tablet (5 grams) was placed in a 10 liter clear container. The time it took for one tablet to completely disintegrate and disperse was measured while adding 10 liters of water (water temperature 22°C) to the container. The results are shown in Table 6 below.

[0099] Evaluation Example 4: Evaluation of tablet hardness The hardness of each tablet was measured using an OPTECH model DS2-200N, and the results are shown in Table 6 below.

[0100] Evaluation Example 5: Evaluation of tableting workability Each mixture of the test examples was transferred to a rotary bundle tablet press and compressed at a pressure of 100 psi to produce immediate release tablets with a weight of 5 grams, a diameter of 2.5 centimeters, and a thickness of 0.7 centimeters. The immediate release tablets were visually observed to see whether they easily separated from the mold or whether the mixture adhered to the upper and lower punches and dies. The tableting workability of each immediate release tablet was measured. The results are shown in Table 6 below.

[0101] Evaluation Example 6: Evaluation of storage stability The tablets produced in the test examples were stored in aluminum packaging or exposed to air. When each tablet packaged in aluminum packaging had no change in appearance, hardness, and mechanical strength even after 6 weeks or more at 50°C, it was evaluated as being very stable. When the hardness of the tablet exposed to air was reduced by 10% or more compared to the initial level after 24 hours, it was evaluated as having a reduced hardness. When the appearance of the tablet exposed to air was changed by the naked eye after 72 hours or 1 hour, it was evaluated as having a changed appearance.

[0102] Evaluation example 7: Evaluation of pesticide efficacy and toxicity Test packages were selected to measure the efficacy and toxicity of the immediate release tablets prepared in Test Examples 4, 8, 21, and 28. In the test packages, the immediate release tablets prepared in the test examples were diluted to a standard amount, and the leaves of the target crops were then treated with the diluted solutions. As treatment methods, pepper tobacco moth was treated twice at 10-day intervals at the early stage of emergence, pear and peach shoot moth was treated twice at 7-day intervals at the early stage of emergence, cabbage cutworm was treated once at the early stage of emergence, and apple oyster moth was treated twice at 10-day intervals at the early stage of emergence. After the pesticide treatment, the control value of each pest was measured to measure the pesticide efficacy. The toxicity to the target crops was measured on a scale of 0 to 5. The results are shown in Table 7 below. [Table 6-1] [Table 6-2] [Table 6-3] [Table 6-4] [Table 7]

[0103] As a result of the above evaluation examples, it was confirmed that the pesticide tablet of the present invention not only maintains hardness, tableting workability, efficacy, and storage stability, but also exhibits excellent powderiness and suspendability, and has the excellent effect of completely disintegrating and dispersing within a short period of time (60 seconds) when added to water.

Claims

1. A pesticide tablet comprising: a pesticide active ingredient; a filler having a water solubility of 10-250 g / 100 ml; and a disintegrant.

2. The active pesticide ingredients are glufosinate-P, MCPA, glyphosate, oxolinic acid, flucetosulfuron, dymron, mefenacet, pyrazosulfuron-ethyl, imazosulfuron, oxaziclomefone, penoxsulam, pretilachlor, mesotrione, pyriftalid, bensulfuron-methyl, thiobencarb, indanofan, pyriminobac-methyl, oxaziclomefone, carfentrazone-ethyl, fentrazamide, pyributicarb, benzobicyclon, metamifop, benfuresate, cyclosulfamuron, anilofos, azimsulfuron, pyrazolate, metazosulfuron, orysastrobin, isoprothiolane, carpropamid, fludioxonil, tiadinil, and tricyclazole. , thifluzamide, probenazole, fthalide, difenoconazole, propiconazole, validamycin, azoxystrobin, edifenphos, fenoxanil, acibenzolar S-methyl, ferimzone, pencycuron, hexaconazole, diazinon, dinotefuran, etofenprox, methoxyfenozide, bensultap, clothianidin, buprofezin, isoprocarb, fenobucarb, benfuracarb, imidacloprid, carbofuran, carbosulfan, cartap, thiamethoxam, tebufenozide, fenobucarb, phenthoate, fipronil, and chlorantraniliprole.

3. 2. The pesticide tablet according to claim 1, wherein the filler is at least one selected from the group consisting of calcium carbonate, sodium carbonate, lactose, maltose, sucrose, xylose, sorbitol, glucose, ammonium sulfate, ammonium chloride, sodium chloride, urea, potassium sulfate, potassium formate, sodium sulfate, potassium chloride, citric acid, succinic acid, tartaric acid, and maleic acid.

4. The content of at least one selected from the group consisting of ammonium sulfate, ammonium chloride, sodium chloride, potassium chloride, potassium sulfate, potassium formate, and urea is 30 to 100 parts by weight based on 100 parts by weight of the extender. The pesticide tablet according to claim 3.

5. 2. The pesticide tablet according to claim 1, wherein the disintegrant is at least one selected from the group consisting of a combination of carbonates and solid acids, agar, starch, hydroxypropyl starch, sodium alginate, carboxymethyl starch ether, gum arabic, tragacanth, gelatin, casein, crystalline cellulose, carboxymethylcellulose calcium, sodium laurate, carboxyl resin, croscarmellose sodium, sodium starch glycolate, polyvinylpolypyrrolidone, ammonium sulfate, potassium chloride, table salt, urea, anionic surfactants, ammonium chloride, calcium chloride, magnesium chloride, aluminum chloride, glucose, lactose, sodium glutamate, sodium inosinate, and dextrin.

6. 10. The pesticide tablet of claim 1, wherein the pesticide tablet further comprises at least one additive selected from the group consisting of surfactants, binders, and lubricants.

7. 7. The pesticide tablet according to claim 6, wherein the content of the surfactant is 1 to 30 parts by weight based on 100 parts by weight of the extender.

8. 7. The pesticide tablet according to claim 6, wherein the content of the binder is 1 to 20 parts by weight based on 100 parts by weight of the filler.

9. The pesticide tablet according to claim 6, wherein the content of the lubricant is 0.1 to 5 parts by weight based on 100 parts by weight of the extender.

10. 2. The pesticide tablet according to claim 1, wherein the content of the disintegrant is 3.5 parts by weight or more based on 100 parts by weight of the filler.

11. 2. The pesticide tablet of claim 1, wherein the filler comprises ammonium chloride.

12. The pesticide tablet according to claim 11, wherein the content of the disintegrant is 8 to 40 parts by weight based on 100 parts by weight of ammonium chloride.

13. 2. The pesticide tablet of claim 1, wherein the disintegrant comprises polyvinylpolypyrrolidone.

14. 14. The pesticide tablet according to claim 13, wherein the content of the filler is 2,857 parts by weight or less based on 100 parts by weight of polyvinylpolypyrrolidone.

15. 2. The pesticide tablet of claim 1, wherein the disintegration and dispersion time of the pesticide tablet is 60 seconds or less.

16. 2. The pesticide tablet according to claim 1, wherein the hardness of the pesticide tablet is 50 to 200 Newtons (N).

17. 2. The pesticide tablet according to claim 1, wherein the suspension rate of the pesticide tablet is 60-80%.

18. 2. The pesticide tablet according to claim 1, wherein the fineness of the pesticide tablet is 95-100%.

19. 10. The pesticide tablet of claim 1, wherein the pesticide tablet further comprises at least one effervescent filler selected from the group consisting of sodium bicarbonate and anhydrous ammonium alum.

20. mixing the pesticide active ingredient and a first filler and grinding them to prepare a first mixture; mixing the first mixture, a second filler, and a disintegrant to prepare a second mixture; and Compressing the second mixture into tablets. wherein each of the first bulking agent and the second bulking agent has a water solubility of 10 to 250 g / 100 ml; A method for producing a pesticide tablet.

21. 21. The method for producing an agrochemical tablet according to claim 20, wherein each of the first and second fillers has a water solubility of 10-110 g / 100 ml.

22. 21. The method for manufacturing an agrochemical tablet according to claim 20, wherein the step of preparing the first mixture further comprises adding an additive; and the additive is at least one selected from the group consisting of a surfactant, a binder, and a lubricant.

Images