TW202114521A - Flupyrimin-containing solid formulation for rice pest control - Google Patents

Flupyrimin-containing solid formulation for rice pest control Download PDF

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TW202114521A
TW202114521A TW109120819A TW109120819A TW202114521A TW 202114521 A TW202114521 A TW 202114521A TW 109120819 A TW109120819 A TW 109120819A TW 109120819 A TW109120819 A TW 109120819A TW 202114521 A TW202114521 A TW 202114521A
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aforementioned
pests
rice pests
solid preparation
controlling rice
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TW109120819A
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Chinese (zh)
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堀越亮
武內晴香
小野保道
佐藤篤志
薮崎光之
尾山和彦
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日商明治製菓藥業股份有限公司
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    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/34Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom
    • A01N43/40Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N25/00Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests
    • A01N25/08Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests containing solids as carriers or diluents
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N25/00Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests
    • A01N25/12Powders or granules
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N25/00Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests
    • A01N25/12Powders or granules
    • A01N25/14Powders or granules wettable
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N25/00Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests
    • A01N25/26Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests in coated particulate form
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01PBIOCIDAL, PEST REPELLANT, PEST ATTRACTANT OR PLANT GROWTH REGULATORY ACTIVITY OF CHEMICAL COMPOUNDS OR PREPARATIONS
    • A01P17/00Pest repellants
    • AHUMAN NECESSITIES
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01PBIOCIDAL, PEST REPELLANT, PEST ATTRACTANT OR PLANT GROWTH REGULATORY ACTIVITY OF CHEMICAL COMPOUNDS OR PREPARATIONS
    • A01P7/00Arthropodicides
    • A01P7/04Insecticides

Abstract

Provided is a solid formulation for rice pest control, which is a coated granule or extruded granule and comprises at least one effective component selected from the group consisting of flupyrimin as represented by formula (1): and salts thereof, and also a solid carrier, a surfactant, and a binder.

Description

含有氟吡嘧(flupyrimin)之水稻害蟲防除用固形製劑A solid preparation for controlling rice pests containing flupyrimine (flupyrimin)

本發明係關於含有氟吡嘧之水稻害蟲防除用固形製劑,更詳細而言,係關於被覆型粒劑或擠出型粒劑之水稻害蟲防除用固形製劑,及使用其之水稻害蟲防除方法、以及前述水稻害蟲防除用固形製劑之製造方法。The present invention relates to a solid preparation for controlling rice pests containing flupirazine, more specifically, it relates to a solid preparation for controlling rice pests of coated granules or extruded granules, and a method for controlling rice pests using the same, And the manufacturing method of the aforementioned solid preparation for controlling rice pests.

亞洲地域的主食之稻米,90%以上為在亞洲所生產,尤其是中國、印度、印尼3國的生產量佔有全世界之60%(非專利文獻1)。在此等之地域的稻米栽培(水稻栽培),因攝食損害地上部之蝶蛾目害蟲,及吸汁莖葉部之半翅目害蟲的損害導致之收量降低已成為問題,尤其是蝶蛾目害蟲之二化螟類、半翅目害蟲之飛蝨類帶來莫大的損害。因病害蟲導致之稻米的生產量損害約高達45%(非專利文獻2),為了提昇稻米的生產量,此等水稻害蟲的防除變必須。More than 90% of rice, the staple food of the Asian region, is produced in Asia. In particular, China, India, and Indonesia account for 60% of the world's production (Non-Patent Document 1). In rice cultivation (rice cultivation) in these areas, it has become a problem to reduce the yield due to ingestion damage to the above-ground Pterodactyl pests and damage to the hemipteran pests of the sap-sucking stems and leaves, especially Pterodactyls. Pests such as Chilo suppressalis, and planthoppers of Hemiptera pests cause great damage. The damage to rice production due to diseases and pests is as high as 45% (Non-Patent Document 2). In order to increase rice production, the control of these rice pests has become necessary.

現在,對於不同時期所發生之此等之水稻害蟲,藉由對各害蟲分別或是混合使用有效之藥劑,來進行防除(體系防除),進行複數次之處理時,耗費有關藥劑處理之人事費或勞力。又,對於既存藥劑之感受性降低之害蟲的發生成為問題(非專利文獻3、4)外,有機磷、苯基胺基甲酸酯(Carbamate)、合成除蟲菊酯等之既存藥劑,由於對非目標生物的不利影響而限制使用。據此,期望防除活性之通用性廣泛且其持續期間長,與既存藥劑未顯示交差耐藥性,進而對環境的影響亦低之新穎製劑的創出。At present, for these rice pests that occur in different periods, the effective pesticides are used separately or in combination to control the pests (system control). When multiple treatments are performed, the personnel costs related to the treatment of the pesticides are consumed. Or labor. In addition, the occurrence of pests with reduced susceptibility to existing drugs is a problem (Non-Patent Documents 3 and 4). Existing drugs such as organophosphorus, phenyl carbamate (Carbamate), and synthetic pyrethrins are not The use is restricted due to the adverse effects of non-target organisms. Accordingly, it is expected that the control activity has a wide range of versatility and a long duration, does not show cross-drug resistance with existing drugs, and has a low impact on the environment.

已報告氟吡嘧作為有害生物防除劑,對於水稻(Rice等)所發生之飛蝨類等之半翅目害蟲或二化螟類等之蝶蛾目害蟲,具有殺蟲效力,或與既存藥劑未顯示交差耐藥性,且對環境的影響低(專利文獻1),又,亦報告有於飛蝨類、二化螟類等之防除用,可混合其他殺蟲劑或殺菌劑來使用(專利文獻2)。然而,針對在稻米之生產的實用場面之具體的製劑形態或使用方法,尤其是防除活性的持續期間,研究仍然不足。 [先前技術文獻] [專利文獻]It has been reported that flurpyrazine is used as a pest control agent. It has insecticidal effect against hemipteran pests such as planthoppers and chilo suppressalis that occur on rice (Rice, etc.), or it has insecticidal effect against existing pesticides. It does not show cross drug resistance and has a low impact on the environment (Patent Document 1). It has also been reported to be used for the control of planthoppers, Chilo suppressalis, etc. It can be mixed with other insecticides or fungicides ( Patent Document 2). However, there are still insufficient researches on the specific formulation form or use method in the practical scene of rice production, especially the duration of the control activity. [Prior Technical Literature] [Patent Literature]

[專利文獻1]國際公開第2012/029672號 [專利文獻2]國際公開第2013/129688號 [非專利文獻][Patent Document 1] International Publication No. 2012/029672 [Patent Document 2] International Publication No. 2013/129688 [Non-Patent Literature]

[非專利文獻1]AMIS Market Database,2018年9月20日檢索,網際網路,<URL:http://statistics.amis-outlook.org/data/ index.html> [非專利文獻2]India Crop Protection Chemicals (Pesticides) Market-Growth,Trends and Forecast(2017-2022), Mordor Intelligence報告(2017年12月) [非專利文獻3]Pest Management Science,Vol.73(6), 1169-1178(2017) [非專利文獻4]Scientific Reports,(2018)8:4586|DOI:10.1038/s41598-018-22906-5[Non-Patent Document 1] AMIS Market Database, retrieved on September 20, 2018, Internet, <URL: http://statistics.amis-outlook.org/data/ index.html> [Non-Patent Document 2] India Crop Protection Chemicals (Pesticides) Market-Growth, Trends and Forecast (2017-2022), Mordor Intelligence report (December 2017) [Non-Patent Document 3] Pest Management Science,Vol.73(6), 1169-1178(2017) [Non-Patent Document 4] Scientific Reports, (2018) 8: 4586|DOI: 10.1038/s41598-018-22906-5

[發明欲解決之課題][The problem to be solved by the invention]

本發明係鑑於這般的狀況而完成者,以提供一種用以防除有害生物,尤其是水稻害蟲之防除活性的持續期間非常長之嶄新的固形製劑,及使用其之水稻害蟲防除方法、以及前述水稻害蟲防除用固形製劑之製造方法作為目的。 [用以解決課題之手段]The present invention was completed in view of such a situation, to provide a novel solid preparation for controlling pests, especially rice pests, with a very long duration of control activity, and a method for controlling rice pests using the same, and the foregoing The purpose is to produce a solid preparation for controlling rice pests. [Means to solve the problem]

本發明者們為了解決前述課題進行努力研究時,發現作為固形製劑,藉由於選自由氟吡嘧及其鹽所成之群組中之至少1種的有效成分,組合特定之固體載體、界面活性劑及結合劑,並成為特定之被覆型粒劑或擠出型粒劑,對水稻害蟲顯示優異之防除活性,且前述防除活性特別長期間持續,而終至完成本發明。亦即,本發明係提供以下者。When the inventors of the present invention made diligent research to solve the aforementioned problems, they found that as a solid preparation, at least one active ingredient selected from the group consisting of flupyrazine and its salts is combined with a specific solid carrier and interfacial activity. The compound and the binding agent become specific coated granules or extruded granules, which show excellent control activity against rice pests, and the aforementioned control activity lasts for a particularly long period of time, and the present invention is finally completed. That is, the present invention provides the following.

[1] 一種水稻害蟲防除用固形製劑,其係含有選自由下述式(1)表示之氟吡嘧及其鹽所成之群組中之至少1種的有效成分、固體載體、界面活性劑、以及結合劑,[1] A solid preparation for controlling rice pests, which contains at least one active ingredient selected from the group consisting of flupyrazine and its salts represented by the following formula (1), a solid carrier, a surfactant, and a combination Agent,

Figure 02_image001
Figure 02_image001

並為被覆型粒劑或擠出型粒劑。And for coated granules or extruded granules.

[2] 如[1]所記載之水稻害蟲防除用固形製劑,其係被覆型粒劑,前述固體載體包含核粒子及增量劑。[2] The solid preparation for controlling rice pests as described in [1] is a coated granule, and the solid carrier includes core particles and an extender.

[3] 如[2]所記載之水稻害蟲防除用固形製劑,其中,前述核粒子的粒徑為63μm~6mm。[3] The solid preparation for controlling rice pests as described in [2], wherein the particle diameter of the core particles is 63 μm to 6 mm.

[4] 如[2]或[3]所記載之水稻害蟲防除用固形製劑,其中,前述核粒子係選自由矽砂、粒狀碳酸鈣、矽藻土粒、粒狀黏土及浮石所成之群組中之至少1種。[4] The solid preparation for controlling rice pests as described in [2] or [3], wherein the aforementioned nuclear particles are selected from the group consisting of silica sand, granular calcium carbonate, diatomaceous earth particles, granular clay, and pumice At least one of them.

[5] 如[2]~[4]中任一項所記載之水稻害蟲防除用固形製劑,其中,前述增量劑係選自由黏土、碳酸鈣、高嶺土及二氧化矽所成之群組中之至少1種。[5] The solid preparation for controlling rice pests as described in any one of [2] to [4], wherein the extender is at least 1 selected from the group consisting of clay, calcium carbonate, kaolin and silica Kind.

[6] 如[2]~[5]中任一項所記載之水稻害蟲防除用固形製劑,其中,前述結合劑係選自由流動石蠟、植物油脂、聚乙二醇及聚丙二醇所成之群組中之至少1種。[6] The solid formulation for controlling rice pests as described in any one of [2] to [5], wherein the aforementioned binding agent is selected from the group consisting of fluid paraffin, vegetable oil, polyethylene glycol, and polypropylene glycol At least one.

[7] 如[1]所記載之水稻害蟲防除用固形製劑,其係擠出型粒劑,前述固體載體包含增量劑,前述界面活性劑包含造粒性改良劑及崩壞・分散劑。[7] The solid preparation for controlling rice pests as described in [1] is an extruded granule, the solid carrier includes an extender, and the surfactant includes a granulation improver and a collapse/dispersant.

[8] 如[7]所記載之水稻害蟲防除用固形製劑,其中,前述增量劑係選自由黏土、滑石、碳酸鈣、高嶺土、二氧化矽及膨潤土所成之群組中之至少1種。[8] The solid formulation for controlling rice pests as described in [7], wherein the extender is at least one selected from the group consisting of clay, talc, calcium carbonate, kaolin, silica, and bentonite.

[9] 如[7]或[8]所記載之水稻害蟲防除用固形製劑,其中,前述造粒性改良劑係選自由月桂基硫酸鈉、二烷基磺基琥珀酸鈉及烷基苯磺酸鈉所成之群組中之至少1種。[9] The solid formulation for controlling rice pests as described in [7] or [8], wherein the granulation improving agent is selected from the group consisting of sodium lauryl sulfate, sodium dialkylsulfosuccinate, and sodium alkylbenzene sulfonate At least 1 in the group.

[10] 如[7]~[9]中任一項所記載之水稻害蟲防除用固形製劑,其中,前述崩壞・分散劑係選自由木質素磺酸鈉、木質素磺酸鈣、萘磺酸鈉福爾馬林縮合物、聚丙烯酸鈉、聚氧乙烯烷基醚硫酸鈉、聚氧化烯苯乙烯苯基醚硫酸鈉、聚氧化烯苯乙烯苯基醚磷酸鈉,及聚氧乙烯・聚氧丙烯聚合物硫酸鈉所成之群組中之至少1種。[10] The solid formulation for controlling rice pests as described in any one of [7] to [9], wherein the aforementioned collapse and dispersing agent is selected from sodium lignosulfonate, calcium lignosulfonate, sodium naphthalenesulfonate Ermalin condensate, sodium polyacrylate, sodium polyoxyethylene alkyl ether sulfate, sodium polyoxyalkylene styrene phenyl ether sulfate, sodium polyoxyalkylene styrene phenyl ether phosphate, and polymerization of polyoxyethylene and polyoxypropylene At least one of the group consisting of sodium sulfate.

[11] 如[7]~[10]中任一項所記載之水稻害蟲防除用固形製劑,其中,前述結合劑係選自由聚乙烯醇、糊精、糖類、羧基甲基纖維素鈉、羥基丙基甲基纖維素及甲基纖維素所成之群組中之至少1種。[11] The solid preparation for controlling rice pests as described in any one of [7] to [10], wherein the aforementioned binding agent is selected from polyvinyl alcohol, dextrin, sugars, sodium carboxymethyl cellulose, and hydroxypropyl methylcellulose. At least one of the group consisting of base cellulose and methyl cellulose.

[12] 一種水稻害蟲防除方法,其係包含將如[1]~[11]中任一項所記載之水稻害蟲防除用固形製劑的有效量,施用在選自由水稻害蟲、水稻、土壤及田水面所成之群組中之至少1種的步驟。[12] A method for controlling rice pests, which comprises applying an effective amount of the solid preparation for controlling rice pests as described in any one of [1] to [11] to a method selected from the group consisting of rice pests, rice, soil, and field water. At least one step in the group.

[13] 如[12]所記載之水稻害蟲防除方法,其中,前述水稻害蟲係選自由飛蝨類及二化螟類所成之群組中之至少1種。[13] The method for controlling rice pests as described in [12], wherein the aforementioned rice pests are selected from at least one of the group consisting of planthoppers and Chilo suppressalis.

[14] 如[12]或[13]所記載之水稻害蟲防除方法,其中,前述水稻害蟲為藥劑抵抗性害蟲。[14] The method for controlling rice pests as described in [12] or [13], wherein the rice pests are pesticide-resistant pests.

[15] 如[12]~[14]中任一項所記載之水稻害蟲防除方法,其中,前述水稻害蟲防除用固形製劑的有效量,以前述有效成分量為耕地每10公畝1g~1kg。[15] The method for controlling rice pests as described in any one of [12] to [14], wherein the effective amount of the solid preparation for controlling rice pests is 1 g to 1 kg per 10 ares of cultivated land.

[16] 一種水稻害蟲防除用固形製劑之製造方法,其係如[2]~[6]中任一項所記載之水稻害蟲防除用固形製劑之製造方法,其特徵為包含: 於前述核粒子加入前述結合劑,或前述結合劑及前述界面活性劑,使其濕潤,而得到濕潤核粒子之濕潤步驟、與 混合前述有效成分、前述界面活性劑及前述增量劑,或前述有效成分及前述增量劑並粉碎,而得到第1混合粉碎物之混合粉碎步驟、與 混合前述濕潤核粒子與第1混合粉碎物,而得到前述濕潤核粒子的表面以第1混合粉碎物被覆的被覆型粒劑之步驟。[16] A method for manufacturing a solid preparation for controlling rice pests, which is the method for manufacturing a solid preparation for controlling rice pests as described in any one of [2] to [6], which is characterized by comprising: Adding the aforementioned binding agent, or the aforementioned binding agent and the aforementioned surfactant to the aforementioned core particles to make them wet to obtain the wetting step of wetting the core particles, and Mixing the aforementioned active ingredient, the aforementioned surfactant and the aforementioned extender, or the aforementioned active ingredient and the aforementioned extender and pulverizing to obtain the first mixing and pulverizing step of mixing and pulverizing, and The step of mixing the wet core particles and the first mixed and pulverized product to obtain a coated granule in which the surface of the wet core particles is coated with the first mixed and pulverized product.

[17] 一種水稻害蟲防除用固形製劑之製造方法,其係如[7]~[11]中任一項所記載之水稻害蟲防除用固形製劑之製造方法,其特徵為包含: 混合前述有效成分、前述增量劑及前述結合劑並粉碎,或混合前述有效成分、前述增量劑及前述結合劑與前述造粒性改良劑及/或前述崩壞・分散劑並粉碎,而得到第2混合粉碎物之混合粉碎步驟、與 捏合第2混合粉碎物及水,或捏合第2混合粉碎物及水與前述造粒性改良劑及/或前述崩壞・分散劑,而得到捏合物之捏合步驟、與 將前述捏合物以擠出型造粒機成型,而得到擠出型粒劑之步驟。 [發明效果][17] A method for manufacturing a solid preparation for controlling rice pests, which is the method for manufacturing a solid preparation for controlling rice pests as described in any one of [7] to [11], characterized in that it comprises: Mix the aforementioned active ingredient, the aforementioned extender, and the aforementioned binder and pulverize, or mix the aforementioned active ingredient, the aforementioned extender, and the aforementioned binder with the aforementioned granulation modifier and/or the aforementioned collapse/dispersant and pulverize, and The mixing and pulverizing step of obtaining the second mixed and pulverized product, and Kneading the second mixed and pulverized product and water, or kneading the second mixed and pulverized product and water with the aforementioned granulation modifier and/or the aforementioned collapse and dispersant to obtain a kneaded product, and The step of forming the aforementioned kneaded mixture with an extrusion granulator to obtain extruded granules. [Effects of the invention]

根據本發明,使得提供一種用以防除有害生物,尤其是水稻害蟲之防除活性的持續期間非常長之嶄新的固形製劑,及使用其之水稻害蟲防除方法、以及前述水稻害蟲防除用固形製劑之製造方法變可能。According to the present invention, it is possible to provide a novel solid preparation with a very long duration of the control activity for controlling harmful organisms, especially rice pests, and a method for controlling rice pests using the same, and the manufacture of the aforementioned solid preparation for controlling rice pests The method becomes possible.

又,氟吡嘧及/或其鹽(較佳為酸加成鹽),與其他藥劑未顯示交差耐藥性,對非目標生物之安全性高,且以低濃度發揮充分優異之防除活性,但根據本發明,此等皆可特別持續長期間。例如,藉由將含有有效成分之氟吡嘧及/或其酸加成鹽的本發明之固形製劑進行1次處理,包含不同時期所發生,且對水稻帶來莫大損害之二化螟類及飛蝨類之2種類以上的水稻害蟲,亦可長期間抑制在低密度。因此,根據本發明,有望提昇稻米的收穫量,變成可解決藥劑感受性的降低、對環境的影響、效果的持續性、對非目標生物的影響、農作業從事者的勞力減低化之既存藥劑所面臨的課題。In addition, flupyrazine and/or its salt (preferably an acid addition salt) does not show cross drug resistance with other drugs, is highly safe to non-target organisms, and exhibits sufficient and excellent control activity at low concentrations, However, according to the present invention, all of these can last particularly long periods of time. For example, by subjecting the solid preparation of the present invention containing the active ingredient fluorpyrazine and/or its acid addition salt to one treatment, it includes the Chilo suppressalis and Chilo suppressalis that occur at different times and cause great damage to rice. Two or more rice pests, such as planthoppers, can also be suppressed at low densities for a long period of time. Therefore, according to the present invention, it is expected that the yield of rice will be increased, and it will be able to solve the problems faced by existing chemicals that reduce the sensitivity to chemicals, the impact on the environment, the continuity of the effects, the effects on non-target organisms, and the reduction in labor of agricultural workers. Subject.

以下,將本發明根據其合適之實施形態進行詳細說明。Hereinafter, the present invention will be described in detail based on its suitable embodiment.

<固形製劑> 本發明係提供一種水稻害蟲防除用固形製劑(以下視情況單稱為「固形製劑」),其係含有選自由下述式(1)表示之氟吡嘧及其鹽所成之群組中之至少1種的有效成分、固體載體、界面活性劑、以及結合劑,<Solid preparations> The present invention provides a solid preparation for the control of rice pests (hereinafter referred to as "solid preparation" as appropriate), which contains selected from the group consisting of flupyrazine and its salts represented by the following formula (1) At least one active ingredient, solid carrier, surfactant, and binding agent,

Figure 02_image003
Figure 02_image003

為被覆型粒劑或擠出型粒劑。For coated granules or extruded granules.

根據本發明之固形製劑的一種態樣,提供一種固形製劑(以下視情況單稱為「被覆型粒劑」),其係被覆型粒劑,前述固體載體包含核粒子及增量劑。又,根據本發明之固形製劑的其他態樣,提供一種固形製劑(以下視情況單稱為「擠出型粒劑」),其係擠出型粒劑,前述固體載體包含增量劑,前述界面活性劑包含造粒性改良劑及崩壞・分散劑。According to one aspect of the solid preparation of the present invention, there is provided a solid preparation (hereinafter referred to as "coated granules" as appropriate), which is a coated granule, and the solid carrier includes a core particle and an extender. In addition, according to another aspect of the solid preparation of the present invention, there is provided a solid preparation (hereinafter referred to as "extruded granules" as appropriate), which is an extruded granule, and the solid carrier contains an extender. Surfactants include granulation modifiers and collapse and dispersants.

尚,在本發明,於「水稻害蟲防除用固形製劑」,除了用以殺蟲或衰弱下述之水稻害蟲的劑之外,包含用以從下述之水稻排除水稻害蟲之劑、用以防治水稻害蟲對水稻的寄生之劑、用以保護水稻免受水稻害蟲侵害之劑。Furthermore, in the present invention, in the "solid formulation for controlling rice pests", in addition to the agent for killing or debilitating the following rice pests, it also includes an agent for excluding rice pests from the following rice, and for controlling A parasitic agent of rice pests on rice, and an agent used to protect rice from rice pests.

(氟吡嘧) 有關本發明之有效成分之氟吡嘧,為上述式(1)所示之化合物,亦即為N-[1-((6-氯吡啶-3-基)甲基)吡啶-2(1H)-亞基]-2,2,2-三氟乙醯胺。氟吡嘧例如可依照國際公開第2012/029672號(專利文獻1)所記載之製造方法合成。(Floperidine) The fluoropyridine, which is the active ingredient of the present invention, is the compound represented by the above formula (1), that is, N-[1-((6-chloropyridin-3-yl)methyl)pyridine-2(1H) -Subunit]-2,2,2-trifluoroacetamide. Flupyrazine can be synthesized in accordance with the production method described in International Publication No. 2012/029672 (Patent Document 1), for example.

又,作為有關本發明之有效成分的氟吡嘧之鹽,較佳為酸加成鹽,作為氟吡嘧之酸加成鹽,更佳為農藥上可容許的酸加成鹽。作為前述酸加成鹽,可列舉鹽酸鹽、硝酸鹽、硫酸鹽、磷酸鹽或乙酸鹽等。In addition, the salt of flupyrazine as the active ingredient of the present invention is preferably an acid addition salt, and the acid addition salt of flupyrazine is more preferably an acid addition salt that is acceptable for agricultural chemicals. Examples of the acid addition salt include hydrochloride, nitrate, sulfate, phosphate, acetate, and the like.

作為有關本發明之有效成分,可單獨為氟吡嘧及前述氟吡嘧之鹽當中的1種,亦可為2種以上的組合。As the active ingredient related to the present invention, it may be one of flupirazine and the aforementioned salt of flupirazine alone, or a combination of two or more kinds.

(水稻害蟲) 所謂本發明之固形製劑顯示防除活性之水稻害蟲,係表示可食水稻之葉、莖、根、穗的害蟲;可從水稻之葉、莖、穗吸汁之害蟲。作為這般的水稻害蟲,雖並非被特別限定者,但例如作為農園藝上之害蟲,可列舉鱗翅目(蝶蛾目)害蟲(分秘夜蛾(Mythimna Separata)、瘤野螟、Cnaphalocrocis patnalis(Marasmia patnalis)、紅帶黃夜蛾(Naranga aenescens)、稻弄蝶(Parnara guttata)、鱗翅夜蛾(Plusia festucae)、勞氏黏蟲(Mythimna loreyi)、稻尺蠖(Protodeltote distinguenda)、斜紋夜蛾(Spodoptera depravata)、隱紋穀弄蝶(Pelopidas mathias)等;二化螟(二化螟蟲、Chilo suppressalis)、三化螟(三化螟蟲、Scirpophaga incertulas)、盜污陰夜蛾(Sesamia inferens)、Scirphophaga innotata、Chilo polychrysus、Chilo auricilius等之二化螟類)、半翅目(半翅目)害蟲(稻麥蚜、長角麥蚜、稻根蚜蟲、粗長毛禾根蚜等之蚜蟲類;黑尾葉蟬、電光葉蟬等之葉蟬類;灰飛蝨、褐飛蝨、白背飛蝨等之飛蝨類;紅條盲椿、稻黑椿象、中華稻緣椿、白星蝽、長肩棘緣椿象、白星椿象、稻綠蝽、水稻葉蝽等之椿象類等)、鞘翅目害蟲(水稻水象鼻蟲、稻象鼻蟲、豆芫菁、稻負泥蟲、稻鐵甲蟲(Dicladispa armigera)等)、蜱蟎亞綱(Steneotarsonemus spinki等)、膜翅目害蟲、直翅目害蟲(小翅稻蝗、黑頸鉤額螽類、螻蛄等)、雙翅目害蟲(水稻潛葉蠅、稻稈潛蠅、稻癭蚊(Orseolia oryzae)等)、纓翅目害蟲(稻薊馬、稻管薊馬等)、植物寄生性線蟲(貝西滑刃線蟲、水稻根瘤線蟲((Meloidogynae graminicola)等)等,可為此等當中之1種單獨,亦可為2種以上的組合。其中,較佳可列舉蝶蛾目害蟲、半翅目害蟲、纓翅目害蟲、雙翅目害蟲,及鞘翅目害蟲,更佳為飛蝨類、二化螟類及葉蟬類,更佳可列舉二化螟、三化螟、灰飛蝨、褐飛蝨、白背飛蝨、黑尾葉蟬、電光葉蟬,再更佳可列舉此等當中之飛蝨類及二化螟類。(Rice pests) The so-called rice pests for which the solid preparation of the present invention exhibits control activity refers to pests that can eat leaves, stems, roots, and ears of rice; pests that can suck juice from leaves, stems, and ears of rice. Such rice pests are not particularly limited, but for example, pests in agriculture and horticulture include lepidopteran (Pteromorpha) pests (Mythimna Separata, S. chinensis, Cnaphalocrocis patnalis (Mythimna Separata), Cnaphalocrocis patnalis ( Marasmia patnalis, Naranga aenescens, Parnara guttata, Plusia festucae, Mythimna loreyi, Protodeltote distinguenda, Spodoptera litura ( Spodoptera depravata), Pelopidas mathias, etc.; Chilo suppressalis (Chilo suppressalis, Chilo suppressalis), Chilo suppressalis (Scirpophaga incertulas), Sesamia inferens, Scirphophaga Innotata, Chilo polychrysus, Chilo auricilius, etc.), Hemiptera (Hemiptera) pests (rice wheat aphid, wheat aphid, rice phylloxera, phylloxera vulgaris, etc.; black tail Leafhoppers, electro-optical leafhoppers, etc.; planthoppers such as Laodelphax striatellus, brown planthopper, white-backed planthopper, etc.; red-striped blind stink bug, rice black stink bug, Chinese rice edge stink bug, white star stink bug, long shoulder spine stink bug , White star stink bug, rice green stink bug, rice leaf stink bug, etc.), coleopteran pests (rice water weevil, rice weevil, bean coriander, rice sludge, rice iron beetle (Dicladispa armigera), etc. ), Acarina (Steneotarsonemus spinki, etc.), Hymenoptera pests, Orthoptera pests (Small winged rice locust, Black-necked frontal chicks, mole crickets, etc.), Diptera pests (rice leaf miners, rice stalks) Liriomyza, Orseolia oryzae, etc.), Thysanoptera pests (rice thrips, rice tube thrips, etc.), plant parasitic nematodes (bessi, Meloidogynae graminicola, etc.) Etc., one of these may be singly, or a combination of two or more. Among them, preferable examples include Pteromorpha pests, Hemiptera pests, Thysanoptera pests, Diptera pests, and Coleoptera Pests, more preferably planthoppers, Chilo suppressalis and leafhoppers, more preferably include Chilo suppressalis, Chilo suppressalis, Laodelphax striatellus, brown planthopper, white-backed planthopper, black-tailed leafhopper, electric leafhopper, More preferably, the planthoppers and Chilo suppressalis among these can be cited.

又,作為前述水稻害蟲,可為對於益達胺(Imidacloprid)等之尼古丁性乙醯膽鹼受體作用藥;芬普尼、益斯普等之GABA受體作用性化合物;剋安勃等之二醯胺化合物等之既存藥劑,降低感受性之藥劑抵抗性害蟲。In addition, as the aforementioned rice pests, there may be drugs that act on nicotine acetylcholine receptors such as Imidacloprid; compounds that act on GABA receptors such as Fipronil and Isp; and Kambo, etc. Existing agents such as diamide compounds, reduce the susceptibility of agents to resist pests.

(其他有害生物防除劑) 作為本發明之固形製劑,由於有效成分之氟吡嘧及其鹽為以其本身對於上述水稻害蟲顯示優異之防除活性者,雖若含有該氟吡嘧及/或其鹽即可,但由於藉由與其他有害生物防除劑混合使用,亦可對更多之害蟲顯示更為優異之防除活性,故可進一步含有其他有害生物防除劑。作為可含有之其他有害生物防除劑,可列舉殺蟲劑(包含殺蟎劑及殺線蟲劑)、殺菌劑、除草劑及植物成長調節劑等,作為具體的藥劑,例如可列舉農藥手冊(The Pesticide Manual,第17版 The British Crop Protection Council 發行)及(SHIBUYA INDEX,2014年,SHIBUYA INDEX RESEARCH GROUP發行)所記載者。此等當中,作為前述其他有害生物防除劑較佳者為殺蟲劑及殺菌劑。(Other pest control agents) As the solid preparation of the present invention, since the active ingredient of flupirazine and its salts are those that show excellent control activity against the above-mentioned rice pests by themselves, it is sufficient if they contain the flupirazine and/or its salt. By mixing with other pest control agents, it can also show more excellent control activity against more pests, so it can further contain other pest control agents. Examples of other pest control agents that may be contained include insecticides (including acaricides and nematicides), fungicides, herbicides, and plant growth regulators. Examples of specific agents include pesticide manuals (The Pesticide Manual, 17th edition issued by The British Crop Protection Council) and (SHIBUYA INDEX, 2014, issued by SHIBUYA INDEX RESEARCH GROUP). Among these, insecticides and fungicides are preferable as the aforementioned other pest control agents.

作為前述其他有害生物防除劑的較佳之例,例如可列舉有機磷酸酯系化合物、苯基胺基甲酸酯系化合物、沙蠶毒素衍生物、有機氯系化合物、除蟲菊酯系化合物、苯甲醯脲系化合物、保幼激素樣化合物、蛻皮酮樣化合物、類尼古丁系化合物、神經細胞之鈉通道阻滯劑、殺蟲性大環狀內酯、γ-胺基丁酸(GABA)拮抗劑、蘭諾定受體(Ryanodine receptor)作用性化合物、殺蟲性尿素類、BT劑、昆蟲病原病毒劑、聚醚系抗生物質、硫胺素拮抗藥,及磺胺(Sulfa)劑・葉酸拮抗藥摻合劑等。As preferred examples of the aforementioned other pest control agents, for example, organophosphate compounds, phenyl carbamate compounds, worm toxin derivatives, organochlorine compounds, pyrethroid compounds, benzene Formaldehyde compounds, juvenile hormone-like compounds, ecdysone-like compounds, nicotine-like compounds, neuronal sodium channel blockers, insecticidal macrocyclic lactones, γ-aminobutyric acid (GABA) antagonists Agents, Ryanodine receptor (Ryanodine receptor) action compounds, insecticidal ureas, BT agents, insect pathogenic virus agents, polyether antibiotics, thiamine antagonists, and sulfa (Sulfa) agents and folic acid antagonists Drug admixtures, etc.

更具體而言,作為殺蟲劑,可列舉如歐殺松(acephate)、二氯松(dichlorvos)、EPN、撲滅松(fenitrothion)、芬滅松(fenamifos)、普硫松(prothiofos)、佈飛松(profenofos)、白克松(pyraclofos)、甲基毒死蜱(chlorpyrifos-methyl)、大利松(diazinon)、福賽絕(fosthiazate)、依米塞松(imicyafos)、褔瑞松(phorate)之有機磷酸酯系化合物;如納乃得(methomyl)、硫敵克(thiodicarb)、得滅克(aldicarb)、歐殺滅(oxamyl)、安丹(propoxur)、加保利(carbaryl)、丁基滅必蝨(fenobucarb)、乙硫苯威(ethiofencarb)、芬硫克(fenothiocarb)、比加普(pirimicarb)、加保扶(carbofuran)、丁基加保扶(carbosulfan)、免扶克(benfuracarb)之苯基胺基甲酸酯系化合物;如培丹(cartap)、硫賜安(thiocyclam)之沙蠶毒素衍生物;如大克蟎(dicofol)、四氯殺蟎碸(tetradifon)之有機氯系化合物;如百滅靈(permethrin)、七氟菊酯(tefluthrin)、賽滅寧(cypermethrin)、第滅靈(deltamethrin)、三氟氯氰菊酯(cyhalothrin)、芬化利(fenvalerate)、氟氰胺菊酯(fluvalinate)、依芬寧(ethofenprox)、矽護芬(silafluofen)、三氟氯氰菊酯(cyhalothrin)之除蟲菊酯系化合物;如二福隆(diflubenzuron)、得福隆(teflubenzuron)、二福隆(flufenoxuron)、克福隆(chlorfluazuron)之苯甲醯脲系化合物;如美賜平(methoprene)之保幼激素樣化合物;如可芬諾(Chromafenozide)之蛻皮酮樣化合物;如益達胺(imidacloprid)、可尼丁(clothianidin)、噻蟲嗪(thiamethoxam)、亞滅培(acetamiprid)、烯啶蟲胺(nitenpyram)、噻蟲啉(thiacloprid)、達特南(dinotefuran)、速殺氟(sulfoxaflor)、氟吡呋喃酮(flupyradifurone)、二克滅(dicloromezotiaz)、三氟苯嘧啶(triflumezopyrim)之尼古丁性乙醯膽鹼受體作用藥;如氟蟲胺(flubendiamide)、剋安勃(chlorantraniliprole)、氰蟲醯胺(cyantraniliprole)、環溴蟲醯胺(cyclaniliprole)、氟氰蟲醯胺(tetraniliprole)之二醯胺化合物;如益斯普(ethiprole)、芬普尼(fipronil)、吡蟲腈(pyrafluprole)、吡瑞蟲腈(pyriprole)、溴氟苯胺(broflanilide)、氟米塔麥(fluxametamide)之GABA受體作用性化合物;如嗒蟎酮(pyridaben)、芬普蟎(fenpyroxymate)、嘧蟎醚(pyrimidifen)、吡蟎胺(tebufenpyrad)、唑蟲醯胺(tolfenpyrad)之呼吸鏈電子傳達系複合體I抑制化合物;如丁氟蟎酯(cyflumetofen)、塞比芬(cyenopyrafen)、氟他胺(pyflbumide)之呼吸鏈電子傳達系複合體II抑制化合物;如嘧蟎酯(fluacrypyrim)、亞醌蟎(acequinocyl)、氟米克(flometoquin)之呼吸鏈電子傳達系複合體III抑制化合物;如賜派芬(spirodiclofen)、螺甲蟎酯(spiromesifen)、螺蟲乙酯(spirotetramat)之ACCase抑制化合物;如賜諾殺(spinosad)、阿維菌素(avermectin)、倍脈心(milbemycin)、司平托列(spinetoram)、列比美汀(lepimectin)、因滅汀苯甲酸鹽(emamectin benzoate)之大環內酯(Macrolide)化合物。More specifically, as insecticides, for example, acephate, dichlorvos, EPN, fenitrothion, fenamifos, prothiofos, cloth Organophosphate series of profenofos, pyraclofos, chlorpyrifos-methyl, diazinon, fosthiazate, imicyafos, phorate Compounds; such as methomyl, thiodicarb, aldicarb, oxamyl, propoxur, carbaryl, fenobucarb ), ethiofencarb, fenothiocarb, pirimicarb, carbofuran, carbosulfan, benfuracarb phenylamine Carboxylic acid ester compounds; such as cartap and thiocyclam's oxworm toxin derivatives; such as dicofol and tetradifon's organochlorine compounds; such as Permethrin, tefluthrin, cypermethrin, deltamethrin, cyhalothrin, fenvalerate, fluvalinate ), ethofenprox, silafluofen, cyhalothrin, pyrethroid compounds; such as diflubenzuron, teflubenzuron, flufenoxuron ), chlorfluazuron (chlorfluazuron) benzylurea compounds; such as methoprene juvenile hormone-like compounds; such as Chromafenozide (Chromafenozide) ecdysone-like compounds; such as imidacloprid (imidacloprid) , Clothianidin, thiamethoxam, acetamiprid, nitenpyram, thiacloprid, dinotefuran, sulfoxaflor , Fluopyridone (f Lupyradifurone, dicloromezotiaz, triflumezopyrim nicotine acetylcholine receptor acting drugs; such as flubendiamide, chlorantraniliprole, cyantraniliprole ), cyclaniliprole (cyclaniliprole), tetraniliprole (tetraniliprole) two amide compounds; such as Ethiprole (ethiprole), Fipronil (fipronil), pyrafluprole (pyrafluprole), Pyridoxa GABA receptor-acting compounds of pyriprole, broflanilide, and fluxametamide; such as pyridaben, fenpyroxymate, pyrimidifen, pyrimidifen Tebufenpyrad (tebufenpyrad), tolfenpyrad (tolfenpyrad) respiratory chain electron transport system complex I inhibitory compound; such as cyflumetofen (cyflumetofen), cyenopyrafen (cyenopyrafen), flutamide (pyflbumide) respiratory chain Electron transport complex II inhibitory compounds; such as fluacrypyrim, acequinocyl, flometoquin, respiratory chain electron transport complex III inhibitors; such as spirodiclofen, ACCase inhibitory compounds of spiromesifen and spirotetramat; such as spinosad, avermectin, milbemycin, spinetoram 1. Macrolide compounds of lepimectin and emamectin benzoate.

進而,作為其他化合物,可列舉布酚淨(buprofezin)、噻蟎酮(hexythiazox)、三亞蟎(amitraz)、殺蟲脒(chlordimeform)、依殺蟎(ethoxazole)、派滅淨(pymetrozine)、聯苯肼(bifenazate)、氟尼胺(flonicamid)、蟲蟎腈(chlorfenapyr)、百利普芬(pyriproxyfen)、茚蟲威(indoxacarb)、三氟甲吡醚(pyridalyl)、哌氟喹腙(pyrifluquinazon)、氰氟蟲腙(metaflumizone)、愛美松(hydramethylnon)、唑蚜威(triazamate)、雙丙環蟲酯(afidopyropen)、瑞那富寧(renofluthrin)、氯普亞列寧(chloroprallethrin)、氯氟氰蟲醯胺(cyhalodiamide)、氟吲哚辛(fluazaindolizine)、ε-甲氧苄氟菊酯(epsilon-metofluthrin)、ε-沒氟菊酯(epsilon-momfluorothrin)、κ-畢芬寧(kappa-bifenthrin)、κ-七氟菊酯(kappa-tefluthrin)、氟殺逢(fluhexafon)、替奧沙芬(tioxazafen)、沒氟菊酯(momfluorothrin)、右旋七氟甲醚菊酯(heptafluthrin)、嘧蟎胺(pyriminostrobin)、環氧蟲啶(cycloxaprid)、異環賽蘭(isocycloseram)、歐賽菲(oxazosulfyl)、替克樂比薩佛(tyclopyrazoflor)、賜派酮(spiropidion)、阿克那比(acynonapyr)、敵普派達(dimpropyridaz)、有機金屬系化合物、二硝基系化合物、有機硫化合物、尿素系化合物、三嗪系化合物、肼系化合物,亦可列舉如BT劑、昆蟲病原病毒劑等之微生物農藥。又,作為前述殺蟲劑,亦可列舉此等之農藥上可容許的酸加成鹽。Furthermore, as other compounds, buprofezin (buprofezin), hexythiazox, amitraz, chlordimeform, ethoxazole, pymetrozine, combined Bifenazate, flonicamid, chlorfenapyr, pyriproxyfen, indoxacarb, pyridalyl, pyrifluquinazon ), metaflumizone, hydramethylnon, triazamate, afidopyropen, renofluthrin, chloroprallethrin, chlorofluoro Cyhalodiamide, fluazaindolizine, epsilon-metofluthrin, epsilon-momfluorothrin, kappa-bifenthrin , Kappa-tefluthrin (kappa-tefluthrin), fluhexafon (fluhexafon), tioxazafen (tioxazafen), momfluorothrin (momfluorothrin), dextefluthrin (heptafluthrin), pyrimate Pyriminostrobin, cycloxaprid, isocycloseram, oxazosulfyl, tyclopyrazoflor, spiropidion, acynonapyr ), dimpropyridaz, organometallic compounds, dinitro compounds, organic sulfur compounds, urea compounds, triazine compounds, hydrazine compounds, such as BT agents, insect pathogenic virus agents, etc. Of microbial pesticides. In addition, as the aforementioned pesticides, acid addition salts that are acceptable on these pesticides can also be cited.

作為前述殺蟲劑,雖可為上述當中之1種單獨,亦可為2種以上的組合,但其中,作為較佳之殺蟲劑,可列舉培丹(cartap)、硫賜安(thiocyclam)、褔瑞松(phorate)、氟蟲胺(flubendiamide)、剋安勃(chlorantraniliprole)、氰蟲醯胺(cyantraniliprole)、加保扶(carbofuran)、芬普尼(fipronil)。As the aforementioned insecticide, although one of the above-mentioned insecticides may be used alone or in combination of two or more types, among them, preferred insecticides include cartap, thiocyclam, and thiocyclam. Phorate, flubendiamide, chlorantraniliprole, cyantraniliprole, carbofuran, fipronil.

又,更具體而言,作為殺菌劑,例如可列舉如嘧菌酯(azoxystrobin)、克收欣(kresoxym-methyl)、三氟敏(trifloxystrobin)、苯氧菌胺(metominostrobin)、肟醚菌胺(orysastrobin)等之甲氧基丙烯酸酯(strobilurin)系化合物;滅派林(mepanipyrim)、嘧黴胺(pyrimethanil)、賽普洛(cyprodinil)之苯胺嘧啶(anilinopyrimidine)系化合物;如三泰芬(triadimefon)、比多農(bitertanol)、氟菌唑(triflumizole)、滅特座(metoconazole)、丙環唑(propiconazole)、戊菌唑(penconazole)、氟矽唑(flusilazole)、邁克尼(myclobutanil)、環克唑(cyproconazole)、戊唑醇(tebuconazole)、己唑醇(hexaconazole)、咪鮮安(prochloraz)、矽氟唑(simeconazole)之唑系化合物;如滅蟎猛(quinomethionate)之喹喔啉系化合物;如代森猛(maneb)、代森鋅(zineb)、代森錳鋅(mancozeb)、聚苯基胺基甲酸酯(polycarbamate)、丙森鋅(propineb)之二硫代苯基胺基甲酸酯系化合物;如乙黴威(diethofencarb)之苯基苯基胺基甲酸酯系化合物;如四氯異苯(chlorothalonil)、五氯硝基苯(quintozene)之有機氯系化合物;如苯菌靈(benomyl)、甲基硫菌靈(thiophanate-methyl)、卡苯達唑(carbendazole)之苯并咪唑系化合物;如甲霜靈(metalaxyl)、悉霜靈(oxadixyl)、甲呋醯胺(ofurase)、苯霜靈(benalaxyl)、呋霜靈(furalaxyl)、酯菌胺(cyprofuram)之苯基醯胺系化合物;如苯氟醯胺(dichlofluanid)之次磺酸系化合物;如氫氧化銅(copper hydroxide)、快得寧(oxine-copper)之銅系化合物;如羥基異噁唑(hydroxyisoxazole)之異噁唑系化合物;如福賽得(fosetyl-aluminium)、脫克松(tolclofos-methyl)之有機磷系化合物;如克菌丹(captan)、四氯丹(captafol)、滅菌丹(folpet)之N-鹵素硫代烷基系化合物;如二甲菌核利(procymidone)、異菌脲(iprodione)、乙烯菌核利(vinchlozolin)之二碳二亞胺(Dicarboximide)系化合物;如福多寧(flutolanil)、滅普寧(mepronil)、福拉比(furametpyr)、噻呋醯胺(thifluzamide)、白克列(boscalid)、平硫瑞(penthiopyrad)之羧基苯胺系化合物;如丁基嗎啉(fenpropimorph)、烯醯嗎啉(dimethomorph)之嗎啉系化合物;如三苯基氫氧化錫(fenthin hydroxide)、三苯基乙酸錫(fenthin acetate)之有機錫系化合物;如咯菌腈(fludioxonil)、拌種咯(fenpiclonil)之氰基吡咯系化合物。Also, more specifically, as the fungicide, for example, azoxystrobin (azoxystrobin), kresoxym-methyl, trifloxystrobin, metominostrobin, orysastrobin can be cited. (orysastrobin) and other strobilurin compounds; mepanipyrim, pyrimethanil, cyprodinil, anilinopyrimidine (anilinopyrimidine) compounds; such as strobilurin triadimefon, bitertanol, triflumizole, metoconazole, propiconazole, penconazole, flusilazole, myclobutanil , Cyproconazole, tebuconazole, hexaconazole, prochloraz, simeconazole azole compounds; such as quinomethionate (quinomethionate) Phrinoid compounds; such as maneb, zineb, mancozeb, polycarbamate, propineb dithiobenzene Carbamate series compounds; such as diethofencarb's phenyl phenyl carbamate series compounds; such as chlorothalonil (chlorothalonil), pentachloronitrobenzene (quintozene) organochlorine series Compounds; such as benomyl, thiophanate-methyl, and carbendazole benzimidazole compounds; such as metalaxyl, oxadixyl, Phenylamide compounds of ofurase, benalaxyl, furalaxyl, cyprofuram; such as dichlofluanid sulfonic acid compounds ; Such as copper hydroxide (copper hydroxide), oxine-copper (oxine-copper) copper compounds; such as hydroxyisoxazole (hydroxyisoxazole) isoxazole compounds; such as fosetyl-aluminium (fosetyl-aluminium), dec Pine (tolclofos-methyl) organophosphorus compounds; such as captan (captan), captafol, folpet N-halogen thioalkyl compounds; such as procymidone, iprodione, vinchlozolin ) Of two carbodiimide (Dicarboximide) compounds; such as flutolanil, mepronil, furametpyr, thifluzamide, boscalid, flat Carboxyaniline compounds of penthiopyrad; morpholine compounds such as fenpropimorph and dimethomorph; such as fenthin hydroxide and triphenyltin acetate (fenthin acetate) organotin compounds; such as fludioxonil (fludioxonil), fenpiclonil (fenpiclonil) cyanopyrrole compounds.

進而,作為其他化合物,可列舉三環唑(tricyclazole)、咯喹酮(pyroquilon)、環丙醯菌胺(carpropamid)、雙氯氰菌胺(diclocymet)、氰菌胺(fenoxanil)、四氯苯酞(fthalide)、扶吉胺(fluazinam)、霜脲氰(cymoxanil)、賽福寧(triforine)、比芬諾(pyrifenox)、氯苯嘧啶醇(fenarimol)、苯銹啶(fenpropidin)、戊菌隆(pencycuron)、富米綜(ferimzone)、賽座滅(cyazofamid)、丙森鋅(iprovalicarb)、苯噻菌胺(benthiavalicarb-isopropyl)、雙胍苯磺酸鹽(iminoctadin-albesilate)、賽芬胺(cyflufenamid)、嘉賜徵素(kasugamycin)、井岡黴素(validamycin)、鏈黴素(streptomycin)、噁喹酸(oxolinic-acid)、特布弗喹(tebufloquin)、烯丙苯噻唑(probenazole)、噻醯菌胺(tiadinil)、亞汰尼(isotianil)、亞賜圃(isoprothiolane)、托普洛卡(tolprocarb)、氟唑菌醯羥胺(pydiflumetofen)、皮卡布西(picarbutrazox)、杏仁菌酯(mandestrobin)、大芬滅替松(dipymetitrone)、必記福敏(pyraziflumid)、奧賽普林(oxathiapiprolin)、平氟芬(penflufen)、fluoxapiprolin、吡啶醯菌胺(florylpicoxamid)、氟醚菌醯胺(fluopimomide)、ipfenoquin、氟因菌唑(fluindapyr)、異氟西波(isoflucypram)、昆諾浮美林(quinofumelin)、methyltetraprole、必噠克緹(pyridachlometyl)、吡普洛潑尼(pyrapropoyne)、胺基吡芬(aminopyrifen)、inpyrifluxam、二氯苯賽鐸(dichlobentiazox)等。又,作為前述殺菌劑,亦可列舉此等之農藥上可容許的酸加成鹽。Furthermore, as other compounds, tricyclazole, pyroquilon, carpropamid, diclocymet, fenoxanil, and tetrachlorobenzene can be cited. Phthalide, fluazinam, cymoxanil, triforine, pyrifenox, fenarimol, fenpropidin, pentobacter Pencycuron, ferimzone, cyazofamid, iprovalicarb, benthiavalicarb-isopropyl, iminoctadin-albesilate, cyazofamid (cyflufenamid), kasugamycin, validamycin, streptomycin, oxolinic-acid, tebufloquin, probenazole , Tiadinil, isotianil, isoprothiolane, tolprocarb, pydiflumetofen, picarbutrazox, amygdalin (mandestrobin), dipymetitrone, pyraziflumid, oxathiapiprolin, penflufen, fluoxapiprolin, florylpicoxamid, flufenoxamid (fluopimomide), ipfenoquin, fluindapyr, isoflucypram, quinofumelin, methyltetraprole, pyridachlometyl, pyrapropoyne, Aminopyrifen, inpyrifluxam, dichlobentiazox, etc. Moreover, as the above-mentioned bactericide, the acid addition salt which is acceptable on these agricultural chemicals can also be mentioned.

作為前述殺菌劑,雖可為上述當中之1種單獨,亦可為2種以上的組合,但其中,作為較佳之殺菌劑,可列舉嘧菌酯(azoxystrobin)、肟醚菌胺(orysastrobin)、噻呋醯胺(thifluzamide)、福拉比(furametpyr)、四氯苯酞(fthalide)、烯丙苯噻唑(probenazole)、阿拉酸式苯-S-甲基(acibenzolar-S-methyl)、噻醯菌胺(tiadinil)、亞汰尼(isotianil)、亞賜圃(isoprothiolane)、托普洛卡(tolprocarb)、環丙醯菌胺(carpropamid)、雙氯氰菌胺(diclocymet)、氰菌胺(fenoxanil)、三環唑(tricyclazole)、咯喹酮(pyroquilon)、富米綜(ferimzone)、特布弗喹(tebufloquin)、矽氟唑(simeconazole)、井岡黴素(validamycin)、嘉賜徵素(Kasugamycin)、戊菌隆(pencycuron)、平氟芬(penflufen)、二氯苯賽鐸(dichlobentiazox)。As the aforementioned bactericide, although one of the above-mentioned bactericides may be used alone or in combination of two or more types, among them, azoxystrobin (azoxystrobin), orysastrobin (orysastrobin), orysastrobin (orysastrobin) may be cited as preferred bactericides. Thifluzamide, furametpyr, fthalide, probenazole, acibenzolar-S-methyl, thifluzamide Tiadinil, isotianil, isoprothiolane, tolprocarb, carpropamid, diclocymet, fenoxanil ( fenoxanil, tricyclazole, pyroquilon, ferimzone, tebufloquin, simeconazole, validamycin, Jiacizhengsu (Kasugamycin), pencycuron, penflufen, dichlobentiazox.

(添加劑) 本發明之固形製劑可藉由於有效成分之氟吡嘧使用添加劑(較佳為農藥上可容許之添加劑)來製造。作為其形態,可列舉粒劑,更具體而言,為含有固體載體、界面活性劑及結合劑之被覆型粒劑或擠出型粒劑。(additive) The solid preparation of the present invention can be manufactured by using an additive (preferably an additive that is acceptable for pesticides) due to the active ingredient of flupirazine. Examples of the form include granules, and more specifically, coated granules or extruded granules containing a solid carrier, a surfactant, and a binding agent.

[固體載體] 作為前述固體載體,可列舉滑石、膨潤土、黏土、高嶺土、矽藻土、蛭石、沸石、二氧化矽、碳酸鈣、硫酸銨、矽砂、矽石、浮石等。[Solid Carrier] Examples of the aforementioned solid carrier include talc, bentonite, clay, kaolin, diatomaceous earth, vermiculite, zeolite, silica, calcium carbonate, ammonium sulfate, silica sand, silica, pumice, and the like.

本發明之被覆型粒劑係前述固體載體當中,含有核粒子及增量劑。又,本發明之擠出型粒劑係前述固體載體當中,含有增量劑,進而,較佳為未含有前述核粒子,亦即前述固體載體僅包含前述增量劑而成。The coated granule of the present invention is the aforementioned solid carrier and contains core particles and an extender. In addition, the extruded granule of the present invention contains an extender in the solid carrier, and preferably does not contain the core particles, that is, the solid carrier only contains the extender.

在本發明,所謂「核粒子」,係表示粒徑為63μm以上之固體載體,作為前述粒徑,較佳為63μm~6mm的範圍內,更佳為75μm~2mm的範圍內,再更佳為106μm~2mm的範圍內。有關本發明之核粒子或固體載體的「粒徑」,係指將粒子對平面投影時之圓的直徑,投影面並非圓形的情況(粒子為平板狀、板狀等、棒狀、多角狀等之形狀時),係指其外接圓的直徑。作為這般的核粒子,若為滿足前述粒徑者雖並未特別限制,但可列舉粒狀之矽砂、矽藻土、浮石、黏土、碳酸鈣等,可為此等當中之1種單獨,亦可為2種以上的組合。又,在本發明,粒狀之碳酸鈣(粒狀碳酸鈣)及粒狀之黏土(粒狀黏土)中,除了各礦物之粉碎物的粒子之外,亦包含分別將粒徑小之礦物微粉與膨潤土或下述之結合劑等混合並進行捏合,並藉由擠出造粒或破碎造粒等,而成為粒狀之造粒物的粒子。In the present invention, the so-called "core particle" refers to a solid carrier with a particle size of 63μm or more. As the aforementioned particle size, it is preferably in the range of 63μm to 6mm, more preferably in the range of 75μm to 2mm, and still more preferably Within the range of 106μm~2mm. The "particle size" of the core particle or solid carrier of the present invention refers to the diameter of the circle when the particle is projected onto the plane. The projection surface is not circular (the particle is flat, plate, etc., rod-shaped, polygonal, etc.). When the shape is equal to), it refers to the diameter of its circumscribed circle. As such core particles, there are no particular restrictions if they meet the aforementioned particle size, but granular silica sand, diatomaceous earth, pumice, clay, calcium carbonate, etc. can be cited. One of these particles can be used alone. It can also be a combination of two or more types. In addition, in the present invention, in the granular calcium carbonate (granular calcium carbonate) and granular clay (granular clay), in addition to the particles of the pulverized product of each mineral, it also includes mineral fine powders with small particle diameters. It is mixed with bentonite or the following binders, kneaded, and granulated by extrusion or crushing to form granular granules.

在本發明,所謂「增量劑」,係主要以稀釋有效成分為目的使用者,具體而言,係表示粒徑為未滿63μm之固體載體。作為這般的增量劑,若為滿足前述粒徑者,雖並未特別限制,但在前述被覆型粒劑較佳,從在下述之被覆型粒劑之製造方法的粉碎步驟變容易的觀點來看,係選自由黏土、碳酸鈣、高嶺土及二氧化矽所成之群組中之至少1種。又,在前述擠出型粒劑較佳,從同樣的觀點來看,係選自由黏土、滑石、碳酸鈣、高嶺土、二氧化矽及膨潤土所成之群組中之至少1種。In the present invention, the so-called "extender" refers to a user whose purpose is to dilute the active ingredient. Specifically, it refers to a solid carrier with a particle size of less than 63 μm. As such an extender, if it satisfies the aforementioned particle size, it is not particularly limited, but it is preferable for the aforementioned coated granules. From the viewpoint of ease of the pulverization step in the manufacturing method of the following coated granules In view, it is at least one selected from the group consisting of clay, calcium carbonate, kaolin and silica. In addition, the aforementioned extruded granules are preferable. From the same viewpoint, they are at least one selected from the group consisting of clay, talc, calcium carbonate, kaolin, silica, and bentonite.

[界面活性劑] 作為前述界面活性劑,可列舉陰離子性界面活性劑、陽離子性界面活性劑及非離子性界面活性劑等。[Surfactant] Examples of the aforementioned surfactant include anionic surfactants, cationic surfactants, and nonionic surfactants.

作為本發明之被覆型粒劑所含有之界面活性劑,於上述當中,較佳為具有前述核粒子之濕潤作用者,具體而言,例如可列舉木質素磺酸鈉、月桂基硫酸鈉、萘磺酸鈉福爾馬林縮合物、聚氧化烯烷基醚硫酸鈉、烷基苯磺酸鈉、二烷基磺基琥珀酸鈉、聚氧化烯苯乙烯苯基醚硫酸鈉、聚氧化烯苯乙烯苯基醚磷酸鈉等之陰離子性界面活性劑;聚氧化烯山梨糖醇脂肪酸酯(聚氧化烯山梨糖醇單月桂酸酯等)、山梨糖醇脂肪酸酯、蔗糖脂肪酸酯、聚氧化烯蓖麻油、聚氧化烯硬化蓖麻油、聚氧化烯烷基醚、聚氧化烯烷基苯基醚、聚氧化烯苯乙烯基苯基醚、聚氧乙烯・聚氧丙烯嵌段聚合物、聚氧化烯烷基胺等之非離子性界面活性劑,可為此等當中之1種單獨,亦可為2種以上的組合。前述界面活性劑當中,前述非離子界面活性劑或其組合,在本發明之被覆型粒劑,可與下述之結合劑以相同目的使用。As the surfactant contained in the coated granules of the present invention, among the above, those having the wetting effect of the aforementioned core particles are preferred. Specifically, for example, sodium lignosulfonate, sodium lauryl sulfate, and naphthalene can be mentioned. Sodium sulfonate formalin condensate, polyoxyalkylene alkyl ether sodium sulfate, sodium alkylbenzene sulfonate, sodium dialkylsulfosuccinate, polyoxyalkylene styrene phenyl ether sodium sulfate, polyoxyalkylene benzene Anionic surfactants such as sodium vinyl phenyl ether phosphate; polyoxyalkylene sorbitol fatty acid esters (polyoxyalkylene sorbitol monolaurate, etc.), sorbitol fatty acid esters, sucrose fatty acid esters, polyoxyalkylene sorbitol fatty acid esters, etc. Oxyalkylene castor oil, polyoxyalkylene hardened castor oil, polyoxyalkylene alkyl ether, polyoxyalkylene alkyl phenyl ether, polyoxyalkylene styryl phenyl ether, polyoxyethylene and polyoxypropylene block polymer, Nonionic surfactants such as polyoxyalkylene alkyl amines may be one of them alone or a combination of two or more. Among the aforementioned surfactants, the aforementioned nonionic surfactants or combinations thereof can be used for the same purpose as the following binders in the coated granules of the present invention.

尚,在本說明書,「聚氧化烯」係表示聚氧乙烯及聚氧丙烯當中之1種或此等之混合物。In addition, in this specification, "polyoxyalkylene" means one or a mixture of polyoxyethylene and polyoxypropylene.

本發明之擠出型粒劑係前述界面活性劑當中,含有造粒性改良劑及崩壞・分散劑。The extruded granules of the present invention are the aforementioned surfactants, and contain a granulation improving agent and a collapse and dispersing agent.

在本發明,所謂「造粒性改良劑」,係表示上述界面活性劑當中,在下述之製造方法之捏合步驟,具有提昇水與其他成分之相容的作用者,具體而言,表示定為0.1%水溶液時,在25℃,顯示10~35mN/m的表面張力值之界面活性劑。作為這般的造粒性改良劑,若為滿足上述表面張力者,雖並未特別限制,但在前述擠出型粒劑,較佳為選自由月桂基硫酸鈉、二烷基磺基琥珀酸鈉及烷基苯磺酸鈉所成之群組中之至少1種。In the present invention, the so-called "granulation modifier" means that among the surfactants mentioned above, in the kneading step of the following manufacturing method, it has the effect of enhancing the compatibility of water with other ingredients. Specifically, it means that it is defined as In the case of 0.1% aqueous solution, it is a surfactant with a surface tension value of 10~35mN/m at 25°C. As such a granulation improver, if it satisfies the above-mentioned surface tension, it is not particularly limited, but in the aforementioned extruded granules, it is preferably selected from sodium lauryl sulfate and dialkyl sulfosuccinic acid. At least one of the group consisting of sodium and sodium alkylbenzene sulfonate.

在本發明,所謂「崩壞・分散劑」,係表示上述界面活性劑當中,除了相當於前述造粒性改良劑者之外,具有提昇對前述有效成分之其他成分之分散性及崩壞性當中的至少任一個之作用者。作為這般的崩壞・分散劑,可列舉較佳為陰離子性界面活性劑,更佳為木質素磺酸鈉、木質素磺酸鈣、萘磺酸鈉福爾馬林縮合物、聚丙烯酸鈉、聚氧乙烯烷基醚硫酸鈉、聚氧化烯苯乙烯苯基醚硫酸鈉、聚氧化烯苯乙烯苯基醚磷酸鈉、聚氧乙烯・聚氧丙烯聚合物硫酸鈉,可為此等當中之1種單獨,亦可為2種以上的組合。In the present invention, the so-called "collapsing and dispersing agent" means that among the above-mentioned surfactants, in addition to the above-mentioned granulation modifier, it has the ability to improve the dispersibility and disintegration of the other ingredients of the above-mentioned active ingredient. The role of at least one of them. As such a collapse and dispersant, anionic surfactants are preferred, and sodium lignosulfonate, calcium lignosulfonate, sodium naphthalenesulfonate formalin condensate, sodium polyacrylate are more preferred. , Polyoxyethylene alkyl ether sodium sulfate, polyoxyalkylene styrene phenyl ether sodium sulfate, polyoxyalkylene styrene phenyl ether phosphate sodium, polyoxyethylene・polyoxypropylene polymer sodium sulfate, can be among these One type alone may also be a combination of two or more types.

[結合劑] 在本發明,「結合劑」主要係以增加固形製劑的強度,及/或增強固體原料彼此之連接為目的來使用。作為這般的結合劑,可列舉羧基甲基纖維素鈉、羥基丙基甲基纖維素或甲基纖維素等之纖維素衍生物;聚丙烯酸鈉等之聚丙烯酸酯類;聚甲基丙烯酸甲酯等之聚甲基丙烯酸酯類;聚乙烯醇或聚乙烯吡咯烷酮等之聚乙烯衍生物;黃原膠、瓜爾膠、阿拉伯膠等之橡膠類(植物橡膠類等);澱粉;糊精;單糖類(果糖、葡萄糖、半乳糖等)或二糖類(蔗糖、麥芽糖、乳糖等)等之糖類;膠;酪蛋白;明膠;流動石蠟;大豆油或菜籽油等之植物油脂;聚乙二醇或聚丙二醇等之甘醇類,可為此等當中之1種單獨,亦可為2種以上的組合。[Binding agent] In the present invention, the "binding agent" is mainly used for the purpose of increasing the strength of the solid preparation and/or enhancing the connection between the solid raw materials. Examples of such binding agents include cellulose derivatives such as sodium carboxymethyl cellulose, hydroxypropyl methyl cellulose, or methyl cellulose; polyacrylates such as sodium polyacrylate; polymethyl methacrylate Polymethacrylates such as esters; polyethylene derivatives such as polyvinyl alcohol or polyvinylpyrrolidone; rubbers (vegetable rubbers, etc.) such as xanthan gum, guar gum, and gum arabic; starch; dextrin; Sugars such as monosaccharides (fructose, glucose, galactose, etc.) or disaccharides (sucrose, maltose, lactose, etc.); gums; casein; gelatin; fluid paraffin; vegetable oils such as soybean oil or rapeseed oil; polyethylene glycol Glycols such as alcohol or polypropylene glycol may be one of these alone or a combination of two or more.

作為本發明之被覆型粒劑所含有之結合劑,上述當中,較佳為選自由流動石蠟、植物油脂、聚乙二醇及聚丙二醇所成之群組中之至少1種。又,作為本發明之擠出型粒劑所含有之結合劑,上述當中,較佳為選自由聚乙烯醇、糊精、糖類、羧基甲基纖維素鈉、羥基丙基甲基纖維素及甲基纖維素所成之群組中之至少1種。As the binder contained in the coated granule of the present invention, among the above, at least one selected from the group consisting of fluid paraffin, vegetable oil, polyethylene glycol, and polypropylene glycol is preferred. Furthermore, as the binder contained in the extruded granules of the present invention, among the above, it is preferable to be selected from the group consisting of polyvinyl alcohol, dextrin, sugars, sodium carboxymethyl cellulose, hydroxypropyl methyl cellulose and methyl cellulose. At least one of the group of base cellulose.

[其他] 進而,作為本發明之固形製劑(較佳為被覆型粒劑),可進一步含有紅色色素或藍色色素等之著色劑。[other] Furthermore, as the solid preparation of the present invention (preferably coated granules), it may further contain a coloring agent such as a red pigment or a blue pigment.

又,作為本發明之固形製劑,於不阻礙本發明之效果的範圍內,如有必要可進一步含有上述以外之界面活性劑、乳化劑、分散劑、崩壞劑、濕潤劑、展著劑、增黏劑、結合劑、防凍結劑、消泡劑、著色劑、防黴劑等之其他添加劑當中之至少1種。In addition, the solid preparation of the present invention may further contain surfactants, emulsifiers, dispersants, disintegrants, wetting agents, spreading agents, etc. other than the above, if necessary, within a range that does not hinder the effects of the present invention. At least one of other additives such as tackifier, bonding agent, anti-freezing agent, defoamer, coloring agent, and anti-mold agent.

[組成] 作為本發明之固形製劑所含有之有效成分量(氟吡嘧或其鹽,含有2種以上的情況下,為該等之合計量,以下相同),由於亦為取決於使用目的或處理方法者,雖並未特別限定,但通常以氟吡嘧之自由體換算為0.1~80重量%,較佳為0.1~10重量%。[composition] As the amount of active ingredients contained in the solid preparation of the present invention (if flupyrazine or its salt contains two or more, the total amount is the same, the same applies below), because it also depends on the purpose of use or processing method Although it is not particularly limited, it is usually 0.1 to 80% by weight, preferably 0.1 to 10% by weight, in terms of free body of fluorpyrazine.

作為本發明之固形製劑的較佳之態樣,可列舉以下者。 (1)含有氟吡嘧0.1~10重量%、核粒子(矽砂等之粒狀固體載體)20~98重量%、增量劑、界面活性劑及結合劑分別為0.2~30重量%(更佳為0.5~30重量%),合計成為100重量%之被覆型粒劑(Coated granule)、 (2)含有氟吡嘧0.1~10重量%、界面活性劑及結合劑分別為0.5~30重量%、增量劑(固體載體)20~98重量%,合計成為100重量%之擠出型粒劑(Extruded granule)、 (3)含有氟吡嘧0.1~10重量%、增量劑(固體載體)20~98重量%、造粒性改良劑0.1~2.0重量%、崩壞・分散劑0.5~5.0重量%、結合劑0.5~30重量%,合計成為100重量%之擠出型粒劑。As a preferable aspect of the solid preparation of the present invention, the following can be cited. (1) Containing 0.1-10% by weight of flupyrazine, 20-98% by weight of nuclear particles (granular solid carrier such as silica sand), and 0.2-30% by weight of extenders, surfactants and binding agents, respectively (more Preferably 0.5~30% by weight), the total becomes 100% by weight of coated granule, (2) Extrusion pellets containing 0.1-10% by weight of flupyrazine, 0.5-30% by weight of surfactant and binding agent, 20-98% by weight of extender (solid carrier), and a total of 100% by weight Extruded granule, (3) Contains 0.1 to 10% by weight of flupiramide, 20 to 98% by weight of extender (solid carrier), 0.1 to 2.0% by weight of granulation improver, 0.5 to 5.0% by weight of collapsing and dispersing agent, and binding agent 0.5-30% by weight, totaling 100% by weight extruded granules.

<固形製劑之製造方法> 本發明作為本發明之固形製劑之製造方法的一態樣,係提供一種製造方法(以下,視情況稱為「被覆型粒劑之製造方法」),其係包含: 於前述核粒子加入前述結合劑或前述結合劑及前述界面活性劑,使其濕潤,而得到濕潤核粒子之濕潤步驟、與 混合前述有效成分、前述界面活性劑及前述增量劑,或前述有效成分及前述增量劑並粉碎,而得到第1混合粉碎物之混合粉碎步驟、與 混合前述濕潤核粒子與第1混合粉碎物,而得到前述濕潤核粒子的表面以第1混合粉碎物被覆的被覆型粒劑之步驟、以及一種製造方法(以下,視情況稱為「擠出型粒劑之製造方法」),其係包含: 混合前述有效成分、前述增量劑及前述結合劑並粉碎,或混合前述有效成分、前述增量劑及前述結合劑與前述造粒性改良劑及/或前述崩壞・分散劑並粉碎,而得到第2混合粉碎物之混合粉碎步驟、與 捏合第2混合粉碎物及水,或捏合第2混合粉碎物及水與前述造粒性改良劑及/或前述崩壞・分散劑,而得到捏合物之捏合步驟、與 將前述捏合物以擠出型造粒機成型,而得到擠出型粒劑之步驟。<Method of manufacturing solid preparation> The present invention, as an aspect of the manufacturing method of the solid preparation of the present invention, provides a manufacturing method (hereinafter, as the case may be referred to as "the manufacturing method of coated granules"), which includes: Adding the aforementioned binding agent or the aforementioned binding agent and the aforementioned surfactant to the aforementioned core particles to make them wet to obtain the wetting step of the wet core particles, and Mixing the aforementioned active ingredient, the aforementioned surfactant and the aforementioned extender, or the aforementioned active ingredient and the aforementioned extender and pulverizing to obtain the first mixing and pulverizing step of mixing and pulverizing, and The step of mixing the wet core particles with the first mixed and pulverized product to obtain coated granules whose surface is covered with the first mixed and pulverized product, and a manufacturing method (hereinafter, as the case may be referred to as "extrusion type") The manufacturing method of granules"), which includes: Mix the aforementioned active ingredient, the aforementioned extender, and the aforementioned binder and pulverize, or mix the aforementioned active ingredient, the aforementioned extender, and the aforementioned binder with the aforementioned granulation modifier and/or the aforementioned collapse/dispersant and pulverize, and The mixing and pulverizing step of obtaining the second mixed and pulverized product, and Kneading the second mixed and pulverized product and water, or kneading the second mixed and pulverized product and water with the aforementioned granulation modifier and/or the aforementioned collapse and dispersant to obtain a kneaded product, and The step of forming the aforementioned kneaded mixture with an extrusion granulator to obtain extruded granules.

[被覆型粒劑之製造方法] 本發明之被覆型粒劑係於前述核粒子表面,將前述有效成分及前述增量劑等以結合劑被覆而成為粒劑者。前述核粒子以容易被被覆的方式,於事前藉由前述結合劑使其濕潤(濕潤步驟)。在該濕潤步驟,可進一步加入前述界面活性劑(較佳為非離子界面活性劑)。作為這般的濕潤步驟,並未特別限制,雖可適當採用以往公知之方法或依照其之方法,但例如可列舉一邊對前述核粒子噴霧前述結合劑及如有必要之前述界面活性劑,一邊進行混合之方法。作為此時之結合劑,可藉由水或乙醇等之溶媒進行稀釋來使用。[Manufacturing method of coated granules] The coated granule of the present invention is a granule formed by coating the active ingredient and the extender with a binder on the surface of the core particle. The core particles are wetted with the binder in advance (wetting step) in a way that they can be easily coated. In this wetting step, the aforementioned surfactant (preferably a nonionic surfactant) can be further added. The wetting step is not particularly limited. Although a conventionally known method or a method according to it can be suitably used, for example, the core particles may be sprayed with the binder and, if necessary, the surfactant. Method of mixing. As the binding agent in this case, it can be used after being diluted with a solvent such as water or ethanol.

另外,被被覆之成分係於事前加入增量劑,均一進行混合並粉碎。亦即,混合前述有效成分、前述界面活性劑及前述增量劑,並粉碎(至少粉碎前述有效成分及前述增量劑),而得到第1混合粉碎物(混合粉碎步驟)。此時,在前述濕潤步驟,加入前述界面活性劑的情況下,混合前述有效成分及前述增量劑並粉碎,而得到第1混合粉碎物。作為前述界面活性劑,可分成濕潤步驟及混合粉碎步驟之兩步驟使用。作為這般的粉碎方法,並未特別限制,可適當採用以往公知之方法或依照其之方法,例如可列舉使用針磨機、錘磨機等之衝撃式粉碎機或射流粉碎機等之氣流式粉碎機之方法。In addition, the coated ingredients are added with extenders beforehand, uniformly mixed and crushed. That is, the active ingredient, the surfactant, and the extender are mixed, and pulverized (at least the active ingredient and the extender are pulverized) to obtain a first mixed and pulverized product (mixing and pulverizing step). At this time, when the surfactant is added in the wetting step, the active ingredient and the extender are mixed and pulverized to obtain a first mixed and pulverized product. As the aforementioned surfactant, it can be used in two steps, a wetting step and a mixing and pulverizing step. There are no particular restrictions on such a pulverization method. A conventionally known method or a method according to it can be suitably used. For example, a jet mill using a pin mill, a hammer mill, etc., or a jet mill, etc. The method of the shredder.

前述濕潤步驟與混合粉碎步驟可任一者先進行,又,亦可為同時。接著,混合前述濕潤核粒子與第1混合粉碎物,而得到前述濕潤核粒子的表面以第1混合粉碎物被覆的被覆型粒劑。作為這般的混合方法,並未特別限制,可適當採用以往公知之方法或依照其之方法,例如可列舉使用混凝土攪拌機等之容器回轉型混合機;帶型攪拌機或圓錐型螺旋式混合機等之容器固定型混合機之方法。The aforementioned wetting step and the mixing and pulverizing step can be performed either first, or at the same time. Next, the wet core particles and the first mixed and pulverized product are mixed to obtain a coated granule in which the surface of the wet core particles is covered with the first mixed and pulverized product. Such a mixing method is not particularly limited, and a conventionally known method or a method according to it can be appropriately used. For example, a container rotary mixer using a concrete mixer, etc.; a belt mixer or a conical screw mixer can be mentioned. The method of the container fixed type mixer.

作為被覆型粒劑之製造方法,如有必要可進一步包含乾燥前述被覆型粒劑之乾燥步驟。作為這般的乾燥方法,並未特別限制,可適當採用以往公知之方法或依照其之方法。As a manufacturing method of the coated granules, if necessary, a drying step of drying the aforementioned coated granules may be further included. There are no particular restrictions on such a drying method, and a conventionally known method or a method according to it can be suitably used.

[擠出型粒劑之製造方法] 本發明之擠出型粒劑係於均一混合前述有效成分及前述增量劑等之成分並粉碎者加入水並進行捏合,將其成型而成為粒劑者。亦即,首先,混合前述有效成分、前述增量劑、前述造粒性改良劑、前述崩壞・分散劑及前述結合劑並粉碎(至少粉碎前述有效成分及前述增量劑),而得到第2混合粉碎物(混合粉碎步驟)。於該混合粉碎步驟,未加入前述造粒性改良劑及/或前述崩壞・分散劑,可於下一捏合步驟加入。作為這般的粉碎方法,可適當採用與被覆型粒劑之製造方法所列舉之粉碎方法相同的方法。又,作為此時之結合劑,可使用水或乙醇等之溶媒進行溶解而成為溶液狀來使用。[Method of manufacturing extruded granules] The extruded granules of the present invention are those obtained by uniformly mixing the aforementioned active ingredient and the aforementioned extender, etc., and pulverizing them, adding water and kneading them to shape them into granules. That is, first, the active ingredient, the extender, the granulation improver, the collapse/dispersant, and the binder are mixed and pulverized (at least the active ingredient and the extender are pulverized) to obtain the first 2 Mix and pulverize (mixing and pulverizing step). In this mixing and pulverizing step, the granulation improving agent and/or the collapsing and dispersing agent are not added, and can be added in the next kneading step. As such a pulverization method, the same method as the pulverization method exemplified in the manufacturing method of coated granules can be suitably adopted. In addition, as the binding agent in this case, it can be used in the form of a solution by dissolving it in a solvent such as water or ethanol.

接著,未加入第2混合粉碎物及水,或是於前述粉碎步驟未加入前述造粒性改良劑及/或前述崩壞・分散劑的情況下,捏合(捏合)第2混合粉碎物及水與前述造粒性改良劑及/或前述崩壞・分散劑,而得到捏合物。又,作為前述造粒性改良劑及前述崩壞・分散劑,可分別獨立分成混合粉碎步驟及捏合步驟之兩步驟使用。作為這般的捏合方法,並未特別限制,可適當採用以往公知之方法或依照其之方法,例如可列舉使用帶型攪拌機、圓錐型螺旋式混合機、亨舍爾式攪拌機、雙腕型捏合機等之混合捏合機的方法。Next, kneading (kneading) the second mixed and pulverized product and water without adding the second mixed and pulverized product and water, or without adding the granulation modifier and/or the aforementioned collapse and dispersing agent in the aforementioned pulverization step With the aforementioned granulation improving agent and/or the aforementioned collapsing and dispersing agent, a kneaded compound is obtained. In addition, as the granulation improving agent and the collapsing/dispersing agent, they can be used separately in two steps, a mixing and pulverizing step and a kneading step. The kneading method is not particularly limited, and a conventionally known method or a method according to it can be suitably used. Examples include the use of a belt mixer, a conical screw mixer, a Henschel mixer, and a double-wrist type kneading machine. The method of mixing and kneading machine, etc.

接著,將前述捏合物以擠出型造粒機成型,而得到擠出型粒劑。作為這般的成型方法,並未特別限制,可適當採用以往公知之方法或依照其之方法。例如,作為前述擠出型造粒機,可列舉藉由擠出之構造,對橫擠出型、前擠出型、堅型、滾筒擠出型,可列舉前述捏合物以螺絲或滾筒等施加壓力,從篩網或模具(Die)擠出之方法。Next, the aforementioned kneaded product is molded with an extrusion-type pelletizer to obtain extruded pellets. As such a molding method, there is no particular limitation, and a conventionally known method or a method according to it can be suitably used. For example, as the aforementioned extrusion type granulator, a structure by extrusion can be mentioned. For horizontal extrusion type, front extrusion type, hard type, roller extrusion type, the aforementioned kneaded material can be applied with screws or rollers. Pressure, a method of extruding from a screen or die (Die).

前述擠出型粒劑之成型後,如有必要可進一步包含將此乾燥之乾燥步驟。作為這般的乾燥方法,並未特別限制,可適當採用以往公知之方法或依照其之方法。After the molding of the aforementioned extruded granules, if necessary, a drying step of drying the granules may be further included. There are no particular restrictions on such a drying method, and a conventionally known method or a method according to it can be suitably used.

根據本發明之另一較佳的態樣,作為組合之物,係提供本發明之固形製劑即第1組成物、與包含將其他有害生物防除劑作為有效成分而成之組成物即第2組成物的組合。此情況,第2組成物可加入適當之添加劑可成為任意之劑形。該組合之物可以藥劑套組等之形態提供。According to another preferred aspect of the present invention, as a composition, there is provided the solid preparation of the present invention, namely the first composition, and the composition containing other pest control agents as effective ingredients, namely the second composition The combination of things. In this case, the second composition can be made into any dosage form by adding appropriate additives. The composition can be provided in the form of a pharmaceutical kit or the like.

根據本發明之又另一態樣,其係用以保護水稻免受水稻害蟲侵害之方法,提供一種包含將本發明之固形製劑、與其他有害生物防除劑的至少一種,同時或分別(較佳為同時適用各成分)適用在適用對象(應處理之區域)而成之方法。在此方法,「同時」適用亦包含將本發明之固形製劑與其他有害生物防除劑的至少一種施用在對象之前進行混合,適用其混合物。「分別」適用係包含不會預先混合該等,將本發明之固形製劑較其他成分優先適用、將本發明之固形製劑較其他成分更後適用。According to yet another aspect of the present invention, which is a method for protecting rice from rice pests, it provides a method comprising combining the solid preparation of the present invention and at least one of other pest control agents, simultaneously or separately (preferably In order to apply each component at the same time), the method is applied to the applicable object (the area to be treated). In this method, "simultaneous" application also includes mixing the solid formulation of the present invention and at least one of other pest control agents before applying to the subject, and applying the mixture thereof. The "respectively" application includes not mixing these in advance, applying the solid preparation of the present invention prior to other ingredients, and applying the solid preparation of the present invention more later than other ingredients.

<水稻害蟲防除方法> 本發明係提供一種水稻害蟲防除方法(以下,視情況單稱為「防除方法」),其係包含將上述之本發明之固形製劑施用在選自由前述水稻害蟲、水稻、土壤及田水面所成之群組中之至少1種之步驟。<Methods of controlling rice pests> The present invention provides a method for controlling rice pests (hereinafter, referred to as "controlling method" as appropriate), which comprises applying the above-mentioned solid formulation of the present invention to the rice pests, rice, soil, and field surface. At least one step in the group.

尚,在本發明,「水稻害蟲防除方法」中,除了殺蟲或衰弱前述水稻害蟲的方法之外,包含從下述之水稻排除水稻害蟲之方法、防止水稻害蟲對水稻之寄生之方法、保護水稻免受水稻害蟲侵害之方法。Still, in the present invention, the "method for controlling rice pests", in addition to the method of killing or debilitating the aforementioned rice pests, includes the method of eliminating rice pests from the following rice, the method of preventing the parasitic of rice pests on rice, and the protection Methods of protecting rice from pests of rice.

[水稻] 作為可施用本發明之固形製劑的植物,雖並未特別限定,但較佳為水稻(Oryza sativa, Oryzaglaberrima)。水稻為禾本科水稻屬之植物,具體而言,分成粳稻種(O.sativa subsp.japonica)與秈稻種(O.sativa subsp.indica)的2種生態型,及藉由此等之雜交的中間性品種。爪哇稻米包含在粳稻種。[Rice] Although the plant to which the solid preparation of the present invention can be applied is not particularly limited, rice (Oryza sativa, Oryzaglaberrima) is preferred. Rice is a plant belonging to the genus Oryza in the Gramineae family. Specifically, it is divided into two ecotypes of japonica species (O.sativa subsp.japonica) and indica species (O.sativa subsp.indica), and the intermediate Sexual variety. Java rice is included in the japonica rice species.

水稻係將亞洲之季風地帶為中心於非常廣泛範圍的地域,於各種氣候條件下栽培。栽培在北邊從俄羅斯與中國之國境的黑龍江河畔,南邊則渡過阿根廷。於尼泊爾、印度之山岳地帶;巴基斯坦、伊朗、埃及的砂漠地帶,已藉由灌溉栽培,而於亞洲的一部分與非洲、拉丁美洲,則未灌溉栽培。又,於亞洲之三角洲地帶,則作為浮稻栽培。The rice line is cultivated in a very wide range of areas centered on the Asian monsoon zone and is cultivated under various climatic conditions. It is cultivated on the Heilongjiang River on the border between Russia and China in the north, and crosses Argentina in the south. In the mountainous areas of Nepal and India; the sandy desert areas of Pakistan, Iran, and Egypt have been cultivated by irrigation, while in parts of Asia, Africa and Latin America, they have not been cultivated. In addition, it is cultivated as floating rice in the deltas of Asia.

藉由栽培方法,稻米被分成陸稻與水稻。陸稻係直接播種在田間,以田間狀態栽培。水稻雖亦有對水田直接播種之直播栽培,但於日本,一般是將幼苗移植至稻田(田種植)的栽培法。By the cultivation method, rice is divided into upland rice and rice. Upland rice is sown directly in the field and cultivated in the field. Although there is also direct seeding cultivation of rice directly sown in the paddy field, in Japan, the cultivation method is generally to transplant the seedlings to the paddy field (field planting).

通常可栽培的溫度為20℃以上,水稻係以湛水條件(水田)栽培。生育最低溫度為10~12℃,開花結實必須為23℃。反之,提高至35℃以上時,產生高溫障礙。The temperature that can be cultivated is usually above 20°C, and rice is cultivated under Zhanshui conditions (paddy fields). The minimum temperature for growth is 10~12℃, and it must be 23℃ for flowering and fruiting. Conversely, when the temperature is increased to 35°C or higher, a high temperature barrier occurs.

原本為水生植物之水稻係水量要求大的作物之一,不灌水,土壤水分於表面層為水分10%以下,於下層土為12%以下時,則發生乾旱損害。惟,亦可於鹽類集積土壤、鹼或酸性土壤栽培。Originally aquatic plants, rice plants are one of the crops that require a large amount of water. Without irrigation, the soil moisture at the surface layer is below 10%, and when the underlying soil is below 12%, drought damage will occur. However, it can also be cultivated in salt accumulation soil, alkali or acid soil.

本發明之固形製劑在米栽培,特佳為在水稻栽培,可施用在從播種(較佳為從移植後)至收穫為止的任意期間。例如,移植苗2~5週後,藉由將本發明之固形製劑對移植後之稻田(水稻稻田)的水面(田水面)施用,可一次防除不同時期所發生之前述水稻害蟲。尚,前述田水面中亦包含在瓦氏盆等之水耕栽培器材的水面。本發明之固形製劑除了前述田水面之外,可施用在包含移植前之栽培載體的土壤,或栽培前述陸稻等之土壤等,亦可直接施用在前述水稻害蟲或水稻(較佳為莖葉部)。此等當中,作為施用本發明之固形製劑之對象,較佳為前述土壤(移植前之栽培土壤及栽培載體、栽培陸稻等之土壤等)及前述田水面當中的至少1種。The solid preparation of the present invention is cultivated in rice, particularly preferably in rice cultivation, and can be applied in any period from sowing (preferably after transplantation) to harvest. For example, 2 to 5 weeks after transplanting seedlings, by applying the solid preparation of the present invention to the water surface (field water surface) of the transplanted rice field (rice paddy field), the aforementioned rice pests that occur in different periods can be controlled at one time. Furthermore, the aforementioned field water surface also includes the water surface of hydroponic cultivation equipment such as the Wasabi basin. The solid preparation of the present invention can be applied to the soil containing the cultivation carrier before transplantation, or the soil for cultivating the aforementioned upland rice, etc., in addition to the aforementioned field water surface. It can also be directly applied to the aforementioned rice pests or rice (preferably stems and leaves). unit). Among these, as the object to which the solid preparation of the present invention is applied, at least one of the aforementioned soil (cultivation soil and cultivation carrier before transplantation, soil for cultivating upland rice, etc.) and the aforementioned field water surface is preferred.

又,在本發明之防除方法,可將本發明之固形製劑以成為有效量的方式,將前述固形製劑直接或是稀釋來施用。Furthermore, in the control method of the present invention, the solid preparation of the present invention can be applied as it is or diluted in such a way that the solid preparation of the present invention becomes an effective amount.

根據本發明之其他態樣,提供一種保護水稻免受水稻害蟲侵害之方法,其係包含將本發明之固形製劑的有效量,施用在選自由前述水稻害蟲、前述水稻(較佳為莖葉部)、前述土壤及前述田水面所成之群組中之至少1種之步驟。According to another aspect of the present invention, there is provided a method for protecting rice from rice pests, which comprises applying an effective amount of the solid preparation of the present invention to the rice pests and the rice (preferably stems and leaves). ), a step of at least one of the groups formed by the aforementioned soil and the aforementioned field water surface.

又,根據本發明之其他態樣,提供一種用以保護水稻免受水稻害蟲侵害之本發明之固形製劑的使用。Furthermore, according to another aspect of the present invention, there is provided a use of the solid preparation of the present invention for protecting rice from rice pests.

作為將本發明之固形製劑施用在對象之手法,可列舉散布處理、田面水處理、土壤處理(散布、混和、灌注等)等,較佳可列舉田面水處理及土壤處理。The method of applying the solid preparation of the present invention to an object includes spray treatment, field water treatment, soil treatment (spreading, mixing, pouring, etc.), and preferably field water treatment and soil treatment.

作為將本發明之固形製劑使用在田面水處理及土壤處理之方法,雖可直接將固形製劑散布在田水面或土壤表面,但於與肥料或砂混和後,可將任意的量散布在耕地(稻田)。作為藉由田面水處理及土壤處理施用時的處理量(亦即有效量),期望以本發明之固形製劑中之有效成分量(以氟吡嘧或其鹽之自由體換算的量,含有此等之2種以上的情況下,為該等之合計量,以下相同),耕地每10公畝為0.1g~10kg,較佳為1g~1kg。As a method of using the solid preparation of the present invention in field water treatment and soil treatment, although the solid preparation can be directly spread on the field water or soil surface, after mixing with fertilizer or sand, any amount can be spread on the cultivated land ( paddy). As the treatment amount (that is, the effective amount) when applied by field water treatment and soil treatment, it is desirable to use the amount of the active ingredient in the solid preparation of the present invention (the amount converted to the free body of flupyrazine or its salt, containing this In the case of two or more types, the total amount is the same, and the following is the same.) The cultivated land is 0.1 g to 10 kg per 10 ares, preferably 1 g to 1 kg.

又,作為藉由本發明之固形製劑之土壤處理方法,雖並未特別限定,但較佳可列舉將本發明之固形製劑直接施用在土壤中或土壤表面上之方法。更佳之土壤處理方法為散布、帶、溝及種植穴適用法。In addition, as a soil treatment method by the solid preparation of the present invention, although not particularly limited, a method of directly applying the solid preparation of the present invention to the soil or on the surface of the soil is preferably mentioned. The better soil treatment method is the application method of spreading, belt, furrow and planting hole.

作為其他施用方法,可列舉對在如薄膜水耕(NFT)或輸液水耕(DFT)等之水耕栽培、如岩棉耕等之固體培養基耕栽培之養液栽培系統的養液之本發明之固形製劑的施用,或對包含蛭石之人工培土及包含育苗用人工墊之固體培養基的直接施用。又,從長期間持續防除活性的觀點來看,雖不佳,但本發明之固形製劑可藉由分散在水中,或是將經乳化或溶解之溶液灌注在土壤來施用。 [實施例]As other application methods, the present invention can be used for the nutrient solution of the hydroponic cultivation system such as thin film hydroponics (NFT) or infusion hydroponics (DFT), solid medium cultivation such as rock wool cultivation. The application of the solid preparation, or the direct application to the artificial soil containing vermiculite and the solid medium containing artificial pad for raising seedlings. In addition, although it is not good from the viewpoint of continuous control activity over a long period of time, the solid preparation of the present invention can be applied by dispersing in water or pouring an emulsified or dissolved solution into soil. [Example]

以下,雖列舉實施例具體說明本發明,但本發明並非被限定於此等之實施例。尚,各製劑例之原料全部使用市售品。又,在各製劑例,僅粒徑為63μm以上之固體載體(核粒子)記為粒徑。Hereinafter, although the present invention will be specifically described with examples, the present invention is not limited to these examples. However, the raw materials of each preparation example are all commercially available products. In addition, in each preparation example, only solid carriers (core particles) having a particle size of 63 μm or more are referred to as particle size.

(製劑例) 製劑例1 [擠出型粒劑] 氟吡嘧                      2重量% 木質素磺酸鈉                 3重量% 月桂基硫酸鈉                0.5重量% 二氧化矽                    2重量% 聚乙烯醇                   1.5重量% 黏土                       91重量% 將上述成分均一混合粉碎,加入水充分捏合後,將此捏合物通過擠出型造粒機,進行造粒乾燥而得到粒劑。(Preparation example) Formulation example 1 [Extrudable granules] Flupyrazine 2% by weight Sodium lignosulfonate 3% by weight Sodium lauryl sulfate 0.5% by weight Silicon dioxide 2% by weight Polyvinyl alcohol 1.5% by weight Clay 91% by weight The above components are uniformly mixed and pulverized, and water is added to fully knead, and the kneaded product is passed through an extrusion-type granulator for granulation and drying to obtain granules.

製劑例2 [擠出型粒劑] 氟吡嘧                    2重量% 木質素磺酸鈣               3重量% 烷基苯磺酸鈉              0.5重量% 二氧化矽                   2重量% 聚乙烯醇                   1重量% 黏土                    91.5重量% 將上述成分均一混合粉碎,加入水充分捏合後,將此捏合物通過擠出型造粒機,進行造粒乾燥而得到粒劑。Formulation example 2 [Extrudable granules] Flupyrazine 2% by weight Calcium lignosulfonate 3% by weight Sodium alkylbenzene sulfonate 0.5% by weight Silicon dioxide 2% by weight Polyvinyl alcohol 1% by weight Clay 91.5% by weight The above components are uniformly mixed and pulverized, and water is added to fully knead, and the kneaded product is passed through an extrusion-type granulator for granulation and drying to obtain granules.

製劑例3 [擠出型粒劑] 氟吡嘧                    2重量% 聚丙烯酸鈉                 2重量% 二烷基磺基琥珀酸鈉         0.3重量% 羧基甲基纖維素鈉           1.5重量% 碳酸鈣                  94.2重量% 排除聚丙烯酸鈉,並將上述之成分均一混合粉碎,對其加入聚丙烯酸鈉與水並充分捏合後,將此捏合物通過擠出型造粒機,進行造粒乾燥而得到粒劑。Formulation example 3 [Extrudable granules] Flupyrazine 2% by weight Sodium polyacrylate 2% by weight Sodium dialkylsulfosuccinate 0.3% by weight Sodium carboxymethylcellulose 1.5% by weight Calcium carbonate 94.2% by weight The sodium polyacrylate is removed, the above-mentioned ingredients are uniformly mixed and crushed, the sodium polyacrylate and water are added to the sodium polyacrylate and water and fully kneaded, the kneaded product is passed through an extrusion granulator to granulate and dry to obtain granules.

製劑例4 [擠出型粒劑] 氟吡嘧                    2重量% 木質素磺酸鈉               3重量% 烷基苯磺酸鈉              0.3重量% 糊精                     5重量% 高嶺土                   10重量% 黏土                   79.7重量% 將上述成分均一混合粉碎,加入水充分捏合後,將此捏合物通過擠出型造粒機,進行造粒乾燥而得到粒劑。Formulation example 4 [Extruded granules] Flupyrazine 2% by weight Sodium lignosulfonate 3% by weight Sodium alkylbenzene sulfonate 0.3% by weight Dextrin 5 wt% Kaolin 10% by weight Clay 79.7 wt% The above components are uniformly mixed and pulverized, and water is added to fully knead, and the kneaded product is passed through an extrusion-type granulator for granulation and drying to obtain granules.

製劑例5 [擠出型粒劑] 氟吡嘧                    2重量% 萘磺酸鈉福爾馬林縮合物       3重量% 月桂基硫酸鈉              0.3重量% 羧基甲基纖維素鈉           1.5重量% 滑石                     30重量% 碳酸鈣                  63.2重量% 將上述成分均一混合粉碎,加入水充分捏合後,將此捏合物通過擠出型造粒機,進行造粒乾燥而得到粒劑。Formulation Example 5 [Extruded granules] Flupyrazine 2% by weight Sodium naphthalenesulfonate formalin condensate 3% by weight Sodium lauryl sulfate 0.3% by weight Sodium carboxymethylcellulose 1.5% by weight Talc 30% by weight Calcium carbonate 63.2% by weight The above components are uniformly mixed and pulverized, and water is added to fully knead, and the kneaded product is passed through an extrusion-type granulator for granulation and drying to obtain granules.

製劑例6 [被覆型粒劑] 氟吡嘧                    2重量% 矽砂(粒狀:粒徑0.3~1.4mm)  95.55重量% 月桂基硫酸鈉              0.1重量% 二氧化矽                 0.5重量% 流動石蠟                 1.15重量% 紅色色素                 0.2重量% 高嶺土                   0.5重量% 將上述之矽砂及流動石蠟以外的成分均一混合粉碎,而得到粉碎物。於矽砂加入流動石蠟並使其均一濕潤後,加入前述粉碎物,進行均一混合,並於前述核粒子被覆前述粉碎物,而得到粒劑。Formulation example 6 [Coated granules] Flupyrazine 2% by weight Silica sand (granular: particle size 0.3~1.4mm) 95.55 wt% Sodium lauryl sulfate 0.1% by weight Silicon dioxide 0.5% by weight Flowing paraffin wax 1.15 wt% Red pigment 0.2% by weight Kaolin 0.5% by weight The components other than the above-mentioned silica sand and fluid paraffin are uniformly mixed and pulverized to obtain a pulverized product. After adding fluidized paraffin to the silica sand and making it uniformly wet, the aforementioned pulverized product is added and uniformly mixed, and the aforementioned core particles are coated with the aforementioned pulverized product to obtain granules.

製劑例7 [被覆型粒劑] 氟吡嘧                    2重量% 矽砂(粒狀:粒徑0.3~1.4mm)  95.85重量% 月桂基硫酸鈉              0.1重量% 二氧化矽                 0.75重量% 聚丙二醇                  1.1重量% 紅色色素                  0.2重量% 將上述之矽砂及聚丙二醇以外的成分均一混合粉碎,而得到粉碎物。於矽砂加入聚丙二醇並使其均一濕潤後,加入前述粉碎物,進行均一混合,並於前述核粒子被覆前述粉碎物,而得到粒劑。Formulation example 7 [Coated granules] Flupyrazine 2% by weight Silica sand (granular: particle size 0.3~1.4mm) 95.85 wt% Sodium lauryl sulfate 0.1% by weight Silicon dioxide 0.75% by weight Polypropylene glycol 1.1% by weight Red pigment 0.2% by weight The components other than the aforementioned silica sand and polypropylene glycol are uniformly mixed and pulverized to obtain a pulverized product. After adding polypropylene glycol to the silica sand and making it uniformly wet, the pulverized product is added and uniformly mixed, and the core particles are coated with the pulverized product to obtain granules.

製劑例8 [被覆型粒劑] 氟吡嘧                    2重量% 烷基苯磺酸鈉              0.1重量% 高嶺土                    1重量% 紅色色素                 0.2重量% 聚乙二醇                 1.15重量% 粒狀碳酸鈣 (粒徑0.42~0.85mm)         95.55重量% 將上述之粒狀碳酸鈣及聚乙二醇以外的成分均一混合粉碎,而得到粉碎物。於粒狀碳酸鈣加入聚乙二醇並使其均一濕潤後,加入粉碎物,進行均一混合,並於前述核粒子被覆前述粉碎物,而得到粒劑。Formulation example 8 [Coated granules] Flupyrazine 2% by weight Sodium alkylbenzene sulfonate 0.1% by weight Kaolin 1% by weight Red pigment 0.2% by weight Polyethylene glycol 1.15 wt% Granular calcium carbonate (Particle size 0.42~0.85mm) 95.55 wt% The above-mentioned granular calcium carbonate and components other than polyethylene glycol are uniformly mixed and pulverized to obtain a pulverized product. After adding polyethylene glycol to the granular calcium carbonate and making it uniformly wet, the pulverized product is added and uniformly mixed, and the core particle is coated with the pulverized product to obtain a granule.

製劑例9 [被覆型粒劑] 氟吡嘧                     2重量% 烷基苯磺酸鈉               0.1重量% 二氧化矽                   0.5重量% 高嶺土                    0.5重量% 藍色色素                  0.2重量% 聚丙二醇                  1.15重量% 矽砂(粒狀:粒徑0.25~1.0mm)  95.55重量% 將上述矽砂及聚丙二醇以外的成分均一混合粉碎,而得到粉碎物。於矽砂加入聚丙二醇並使其均一濕潤後,加入粉碎物,進行均一混合,並於前述核粒子被覆前述粉碎物,而得到粒劑。Formulation example 9 [Coated granules] Flupyrazine 2% by weight Sodium alkylbenzene sulfonate 0.1% by weight Silicon dioxide 0.5% by weight Kaolin 0.5% by weight Blue pigment 0.2% by weight Polypropylene glycol 1.15 wt% Silica sand (granular: particle size 0.25~1.0mm) 95.55 wt% The components other than the aforementioned silica sand and polypropylene glycol are uniformly mixed and pulverized to obtain a pulverized product. After adding polypropylene glycol to the silica sand and making it uniformly wet, the pulverized product is added and uniformly mixed, and the core particles are coated with the pulverized product to obtain granules.

製劑例10 [被覆型粒劑] 氟吡嘧                     2重量% 高嶺土                    1.5重量% 藍色色素                  0.2重量% 二烷基磺基琥珀酸鈉          0.1重量% 聚氧化烯山梨糖醇脂肪酸酯     0.2重量% 大豆油                     1重量% 矽砂(粒狀:粒徑0.25~1.0mm)    95重量% 將氟吡嘧、高嶺土、藍色色素均一混合粉碎,而得到粉碎物。於矽砂加入預先混合之二烷基磺基琥珀酸鈉、聚氧化烯山梨糖醇脂肪酸酯及大豆油的混合物並使其均一濕潤後,加入粉碎物,進行均一混合,並於前述核粒子被覆前述粉碎物,而得到粒劑。Formulation example 10 [Coated granules] Flupyrazine 2% by weight Kaolin 1.5% by weight Blue pigment 0.2% by weight Sodium dialkylsulfosuccinate 0.1% by weight Polyoxyalkylene sorbitol fatty acid ester 0.2% by weight Soybean oil 1% by weight Silica sand (granular: particle size 0.25~1.0mm) 95% by weight Flupyrazine, kaolin, and blue pigment are uniformly mixed and pulverized to obtain a pulverized product. Add the pre-mixed mixture of sodium dialkyl sulfosuccinate, polyoxyalkylene sorbitol fatty acid ester, and soybean oil to the silica sand and make it uniformly moisturized, then add the pulverized product, mix it uniformly, and add to the aforementioned core particles The pulverized product is covered to obtain granules.

比較製劑例1 [流動劑] 氟吡嘧                        10重量% 木質素磺酸鈉                   2.5重量% 二烷基磺基琥珀酸鈉               0.2重量% 丙二醇                        10重量% 黃原膠                         0.3重量% 聚矽氧系消泡劑                   0.5重量% 防黴劑 (有機氮硫系複合物、有機溴系化合物)  0.03重量% 水                           76.47重量% 於水加入氟吡嘧、木質素磺酸鈉、二烷基磺基琥珀酸鈉、丙二醇及聚矽氧系消泡劑並混合後,進行藉由珠磨機之濕式粉碎,而得到漿料(A液)。其次,混合黃原膠、防黴劑及水並溶解,而得到水溶液(B液)。混合經調製之A液780重量份與B液230重量份,而得到流動劑。Comparative preparation example 1 [Flowing agent] Flupyrazine 10% by weight Sodium lignosulfonate 2.5% by weight Sodium dialkylsulfosuccinate 0.2% by weight Propylene glycol 10% by weight Xanthan gum 0.3% by weight Polysiloxane-based defoamer 0.5% by weight Antifungal agent (Organic nitrogen-sulfur compound, organic bromine compound) 0.03% by weight Water 76.47% by weight After adding fluperazine, sodium lignosulfonate, sodium dialkyl sulfosuccinate, propylene glycol and polysiloxane defoaming agent to water and mixing, perform wet pulverization by a bead mill to obtain slurry (A liquid). Next, xanthan gum, antifungal agent, and water are mixed and dissolved to obtain an aqueous solution (liquid B). 780 parts by weight of the prepared liquid A and 230 parts by weight of the liquid B were mixed to obtain a fluidizing agent.

比較製劑例2 [顆粒水合劑] 氟吡嘧                    20重量% 二烷基磺基琥珀酸鈉           1重量% 木質素磺酸鈉                7重量% 二氧化矽                   1重量% 黏土                      71重量% 將上述成分均一混合粉碎,加入水充分捏合後,將此捏合物通過擠出型造粒機,進行造粒乾燥而得到顆粒水合劑。Comparative preparation example 2 [granule hydrating agent] Flupyrazine 20% by weight Sodium dialkylsulfosuccinate 1% by weight Sodium lignosulfonate 7 wt% Silicon dioxide 1% by weight Clay 71% by weight The above components are uniformly mixed and pulverized, water is added and kneaded sufficiently, and the kneaded product is passed through an extrusion-type granulator for granulation and drying to obtain a granular hydrating agent.

(試驗例1 對於二化螟類及飛蝨類之田間試驗) 對田間種植25日後之水稻田間,以原體量(有效成分量、在氟吡嘧劑,為氟吡嘧量,以下相同)成為指定量的方式,將製劑例1之粒劑(擠出型粒劑)藉由水面施用進行處理(田面水處理)。針對對照製劑,同樣於田間種植25日後,將二化螟類防除用製劑之培丹4%粒劑以原體量(培丹量)成為指定量的方式,藉由水面施用進行處理,進而從該處理3週(21日)後,將飛蝨類防除用製劑之布酚淨25%流動劑以原體量(布酚淨量)成為指定量的方式,藉由莖葉散布進行處理。針對無處理區,任何製劑皆未施用。(Test Example 1 Field test for Chilo suppressalis and planthoppers) For the rice field 25 days after the field planting, the original body amount (the amount of active ingredient, the amount of flupyrazine is the same as the amount of flupyrazine, the same below) becomes the specified amount, and the granules of formulation example 1 (extruded type) Granules) are treated by water surface application (field surface water treatment). For the control formulation, after 25 days of planting in the field, the Pedan 4% granules of Chilo suppressalis control formulations were treated with the original amount (the amount of Pedan) as the specified amount, and then treated by surface application, and then After 3 weeks (21 days) of the treatment, the 25% flow agent of the planthopper control agent was sprayed on the stems and leaves so that the original amount (the net amount of butofol) became the designated amount. For the untreated area, no formulations were applied.

於經製劑處理之日(田間種植25日後)的14、21、28、35日後,集計在各區隨機選出之20株的分蘗數,及因二化螟類(主要為三化螟)導致之損害莖數。依照以下之式,算出損害莖率。 損害莖率(%)=(各處理日之損害莖數/20株之總分蘗數)×100 將結果示於下述之表1。又,同於14、21、28、35、42日後,集計寄生在各區隨機選出之20株的各株之飛蝨類(褐飛蝨及白背飛蝨的合計)的固體數(成蟲及幼蟲數的合計),作為飛蝨類之寄生蟲數。將結果示於下述之表2。On the 14th, 21st, 28th, and 35th days after the preparation treatment (25 days after planting in the field), the number of tillers of 20 randomly selected plants in each district and the number of tillers caused by Chilo suppressalis (mainly Chilo suppressalis) Number of damaged stems. According to the following formula, calculate the damaged stem rate. Damaged stem rate (%)=(number of damaged stems on each treatment day/total number of tillers of 20 plants)×100 The results are shown in Table 1 below. Also, after 14, 21, 28, 35, and 42 days, the total number of planthoppers (the total number of brown planthoppers and white-backed planthoppers) parasitic in each of 20 randomly selected plants in each district (the number of adults and larvae) The total number of parasites as planthoppers. The results are shown in Table 2 below.

Figure 02_image005
Figure 02_image005

Figure 02_image007
Figure 02_image007

試驗的結果,如表1~2所示,於本發明之固形製劑即氟吡嘧粒劑,在100g/ha的處理量,確認不僅顯示相較對於二化螟類之對照製劑更高之損害抑制效果,亦顯著抑制飛蝨類之寄生蟲數。另一方面,在對照製劑之培丹粒劑及布酚淨流動劑之處理區(體系防除處理區),因二化螟類導致之損害莖率雖較無處理區抑制在更低,但為飛蝨類之寄生蟲數的減少率較少,對於飛蝨類之密度抑制效果較低的結果。如此,確認本發明之氟吡嘧粒劑僅以1次的處理即具有長期之持續性,相較對照製劑之二化螟類防除用製劑及飛蝨類防除用製劑之體系處理,對於二化螟類及飛蝨類顯示更高之防除活性。The results of the test, as shown in Tables 1 and 2, in the solid preparation of the present invention, flupirazine granules, at a treatment amount of 100g/ha, it was confirmed that it not only showed higher damage compared to the control preparations of Chilo suppressalis The inhibitory effect also significantly suppresses the number of parasites such as planthoppers. On the other hand, in the treatment area (system control treatment area) of Peidan granules and Bufenjing fluid agent of the control formulation, the rate of damaged stems caused by Chilo suppressalis is lower than that in the untreated area, but it is The reduction rate of the number of parasites of planthoppers is small, and the effect of suppressing density of planthoppers is low. In this way, it is confirmed that the flupirazine granules of the present invention have long-term continuity after only one treatment. Compared with the control formulations of the control formulations of Chilo suppressalis and planthoppers, the system treatment of Chilo suppressalis and planthoppers is more effective Stem borers and planthoppers show higher control activity.

又,藉由比較從各處理區所收穫之稻米的重量,評估對各製劑之稻米的收量的影響。將結果示於下述之表3。In addition, by comparing the weight of rice harvested from each treatment area, the effect on the yield of rice of each formulation was evaluated. The results are shown in Table 3 below.

Figure 02_image009
Figure 02_image009

如表3所示,於氟吡嘧粒劑之處理區,確認相較對照製劑之體系防除處理區更高,對於無處理區提昇12%之收量的效果。藉由以上之結果,根據本發明之固形製劑(擠出型粒劑),確認藉由1次的處理,不僅減低化水稻害蟲防除作業的勞力,相較對照製劑亦顯示更為優異之增收效果。As shown in Table 3, in the treatment area of flupirazine granules, it was confirmed that the system control treatment area was higher than that of the control formulation, and the effect of increasing the yield by 12% for the untreated area was confirmed. Based on the above results, according to the solid preparation (extruded granules) of the present invention, it was confirmed that the single treatment not only reduces the labor of rice pest control operations, but also shows a more excellent income-increasing effect than the control preparation. .

(試驗例2 對於褐飛蝨之室內試驗) 將播種3週後之水稻移植至瓦氏盆(1/5000a),於移植3日後,以原體量成為指定量的方式,將製造例1之粒劑(擠出型粒劑)或是製造例6之粒劑(被覆型粒劑),或氟吡嘧原體藉由水面施用進行處理(田面水處理)。針對無處理區,任何製劑及藥劑皆未施用。於經製劑或藥劑處理之日(移植3日後)之3、29、42日後,對各盆放飼褐飛蝨之二齡幼蟲,於該放飼6日後或是7日後觀察幼蟲生死,依照以下之式算出修正死蟲率。 修正死蟲率(%)=[{(無處理區之生存蟲數/放飼蟲數)-(處理區之生存蟲數/放飼蟲數)}/(無處理區之生存蟲數/放飼蟲數)]×100 試驗係以2連制進行。將結果示於下述之表4。(Test Example 2 Indoor test for brown planthopper) Transplant the rice 3 weeks after sowing into a Waschner basin (1/5000a), and 3 days after transplantation, use the granules (extruded granules) of Manufacturing Example 1 or manufacture them in such a way that the amount of the original body becomes the specified amount. The granules of Example 6 (coated granules), or flupyrazine, were treated by surface application (field surface water treatment). For the untreated area, no preparations and medicaments were applied. Feed the second-instar larvae of Nilaparvata lugens on the 3rd, 29th, and 42nd day after the preparation or medicament treatment (3 days after transplantation), and observe the life and death of the larvae after 6 days or 7 days after the feeding, according to the following formula Calculate the modified death rate. Modified rate of dead insects (%)=[{(Number of surviving insects in no-treatment area/Number of feeding insects)-(Number of surviving insects in treatment area/Number of feeding insects)}/(Number of surviving insects in no-treatment area/Release Feeding insects)]×100 The test is carried out in a 2-continuous system. The results are shown in Table 4 below.

Figure 02_image011
Figure 02_image011

試驗的結果,如表4所示,於本發明之固形製劑即氟吡嘧之被覆型粒劑及擠出型粒劑,於各處理之29、42日後,即使放飼水稻害蟲,亦顯示較氟吡嘧原體更高之修正死蟲率。因此,確認藉由成為此等之粒劑,相較原體,長期的持續性更為優異。The results of the test, as shown in Table 4, in the solid preparations of the present invention, namely the coated granules and extruded granules of flupyrazine, after 29 and 42 days of each treatment, even if the rice pests were fed, they also showed better results. Flurpyrazine has a higher modified mortality rate. Therefore, it is confirmed that by using these granules, the long-term sustainability is better than that of the original body.

(試驗例3 對於二化螟類之田間試驗) 將製劑例1之粒劑(擠出型粒劑)與適當量之砂混和後,對移植25日後之水稻田間,以原體量成為指定量的方式,藉由均一水面施用,進行處理(田面水處理)。又,於同日,將比較製劑例1之流動劑以成為40L/10a的處理水量的方式以水進行稀釋,並以原體量成為指定量的方式,藉由噴霧器對莖葉部進行噴霧處理。針對無處理區,任何製劑皆未施用。於製劑處理時,雖未觀察到因二化螟類(優勢種三化螟)導致之對莖部的損害,但於處理之28日後及42日後,藉由目視計數各株之莖數及因二化螟類(優勢種三化螟)導致之芯枯莖數。進行25m2 之區每30株的調査,依然以下之式,算出損害莖率。 損害莖率(%)={(每30株之芯枯莖數)/(每30株之總莖數)}×100 將結果示於下述之表5。(Test Example 3 Field test for Chilo suppressalis) After mixing the granules (extruded granules) of Formulation Example 1 with an appropriate amount of sand, the rice field after transplantation 25 days after transplantation, the original amount becomes the designated amount The way, by uniform water surface application, for treatment (field surface water treatment). Also, on the same day, the fluid agent of Comparative Formulation Example 1 was diluted with water so that the treatment water amount was 40 L/10a, and the stem and leaf parts were sprayed with a sprayer so that the original body amount became a predetermined amount. For the untreated area, no formulations were applied. During the preparation treatment, although no damage to the stems caused by Chilo suppressalis (the dominant species of Chilo suppressalis) was observed, the number of stems and their causes were counted visually after 28 days and 42 days after treatment. The number of core withered stems caused by Chilo suppressalis (the dominant species of Chilo suppressalis). The survey was conducted for every 30 plants in a 25m 2 area, and the damaged stem rate was calculated using the following formula. Damaged stem rate (%)={(Number of core dead stems per 30 plants)/(Total number of stems per 30 plants)}×100 The results are shown in Table 5 below.

Figure 02_image013
Figure 02_image013

試驗的結果,如表5所示,本發明之擠出型粒劑對於二化螟類(優勢種三化螟),相較流動劑經過長期間,亦顯示高防除活性。As shown in Table 5, the extruded granules of the present invention also showed high control activity against Chilo suppressalis (the dominant species of Chilo suppressalis) over a longer period of time than the flow agent.

(試驗例4 對於褐飛蝨之田間試驗) 將製劑例1之粒劑(擠出型粒劑)與適當量之砂混和後,對移植25日後之水稻田間,以原體量成為指定量的方式,藉由均一水面施用,進行處理(田面水處理)。又,於同日,將比較製劑例1之流動劑以成為40L/10a的處理水量的方式以水進行稀釋,並以原體量成為指定量的方式,藉由噴霧器對莖葉部進行噴霧處理。針對無處理區,任何製劑皆未施用。於製劑處理時,雖未觀察到因飛蝨類對稻的寄生,但於處理之31、49、56日後,藉由目視計數寄生在各株頭之褐飛蝨成蟲及幼蟲數。將進行25m2 之區每30株的調査的結果,以每株之寄生蟲數(成蟲及幼蟲的合計)示於下述之表6。(Test Example 4 Field test for brown planthopper) After mixing the granules (extruded granules) of Formulation Example 1 with an appropriate amount of sand, the rice field after transplantation 25 days after transplantation, the original amount becomes the specified amount, Treatment (field surface water treatment) is carried out by uniform water surface application. Also, on the same day, the fluid agent of Comparative Formulation Example 1 was diluted with water so that the treated water amount was 40 L/10a, and the stems and leaves were sprayed with a sprayer so that the original amount became a specified amount. For the untreated area, no formulations were applied. During the preparation treatment, although no parasitism of rice planthoppers by planthoppers was observed, the number of adults and larvae of the brown planthopper parasitic on each plant head was counted visually after 31, 49, and 56 days of treatment. The results of the survey per 30 plants in an area of 25 m 2 are shown in Table 6 below in terms of the number of parasites per plant (total of adults and larvae).

Figure 02_image015
Figure 02_image015

試驗的結果,如表6所示,本發明之擠出型粒劑對於褐飛蝨,相較流動劑經過長期間,亦顯示高防除活性。As a result of the test, as shown in Table 6, the extruded granules of the present invention also showed high control activity against brown planthoppers over a longer period of time than the flowable agent.

(參考試驗例 顆粒水合劑與流動劑之對比試驗) 將比較製劑例1之流動劑或比較製劑例2之顆粒水合劑以成為150L/10a的處理水量的方式以水進行稀釋,並以原體量成為指定量的方式,藉由噴霧器對移植48日後之水稻莖葉部進行噴霧處理。針對無處理區,任何製劑皆未施用。於各處理前及處理之4、7、19、33日後,對A4尺寸之黏著板擦落寄生在各株頭之飛蝨類,藉由目視計數灰飛蝨成蟲及幼蟲數。將進行24m2 之區每30株的調査的結果以每株之寄生蟲數(成蟲及幼蟲的合計)示於下述之表7。(Reference test example for comparison test of granular hydrating agent and fluidizing agent) The fluidizing agent of Comparative Preparation Example 1 or the granular hydrating agent of Comparative Preparation Example 2 was diluted with water so that the treated water volume was 150L/10a, and the original body When the amount becomes the specified amount, spray the rice stems and leaves 48 days after transplantation with a sprayer. For the untreated area, no formulations were applied. Before each treatment and 4, 7, 19, and 33 days after the treatment, wipe off the planthoppers parasitic on each plant head on the A4 size adhesive board, and count the number of adults and larvae of Laodelphax striatellus by visual observation. The results of the survey per 30 plants in an area of 24 m 2 are shown in Table 7 below in terms of the number of parasites per plant (total of adults and larvae).

Figure 02_image017
Figure 02_image017

試驗的結果,如表7所示,於流動劑與顆粒水合劑,對於灰飛蝨,顯示同程度之防除活性。因此,藉由上述之結果,本發明之擠出型粒劑與顆粒水合劑相比較,可說經過長期間,亦顯示高防除活性。 [產業上之可利用性]The results of the test, as shown in Table 7, showed that the fluidizing agent and the granular hydrating agent showed the same level of control activity against Laodelphax striatellus. Therefore, based on the above results, the extruded granules of the present invention, compared with the granular hydrating agent, can be said to show high control activity over a long period of time. [Industrial availability]

如以上說明,根據本發明,變成可提供一種用以防除有害生物、尤其是水稻害蟲之防除活性的持續期間長之嶄新的固形製劑,及使用其之水稻害蟲防除方法、以及前述水稻害蟲防除用固形製劑之製造方法。例如,於本發明之水稻害蟲防除用固形製劑,於水稻之移植2~5週後藉由進行田面水處理,使得於以往一次之藥劑處理無法充分防除之飛蝨類及二化螟類的防除變成可一次防除,亦有效減低施加在米栽培農家之藥劑防除之勞力及提昇收穫率。As explained above, according to the present invention, it becomes possible to provide a novel solid preparation for controlling pests, especially rice pests, with a long duration of the control activity, and a method for controlling rice pests using the same, and the aforementioned rice pest control The manufacturing method of solid preparations. For example, in the solid preparation for controlling rice pests of the present invention, the field water treatment is carried out 2 to 5 weeks after rice transplantation, so that planthoppers and chilo suppressalis that cannot be fully controlled by the previous chemical treatment It becomes a one-time control, which also effectively reduces the labor of pesticide control applied to rice cultivation farmers and increases the harvest rate.

Figure 109120819-A0101-11-0002-2
Figure 109120819-A0101-11-0002-2

Claims (17)

一種水稻害蟲防除用固形製劑,其係含有選自由下述式(1)表示之氟吡嘧(flupyrimin)及其鹽所成之群組中之至少1種的有效成分、固體載體、界面活性劑、以及結合劑,並為被覆型粒劑或擠出型粒劑
Figure 03_image001
A solid preparation for controlling rice pests, which contains at least one active ingredient selected from the group consisting of flupyrimin represented by the following formula (1) and its salts, a solid carrier, and a surfactant , And binding agent, and coated granules or extruded granules
Figure 03_image001
.
如請求項1之水稻害蟲防除用固形製劑,其係被覆型粒劑,前述固體載體包含核粒子及增量劑。For example, the solid preparation for controlling rice pests of claim 1, which is a coated granule, and the solid carrier includes core particles and an extender. 如請求項2之水稻害蟲防除用固形製劑,其中,前述核粒子的粒徑為63μm~6mm。Such as the solid preparation for controlling rice pests of claim 2, wherein the particle diameter of the aforementioned nuclear particles is 63 μm-6 mm. 如請求項2或3之水稻害蟲防除用固形製劑,其中,前述核粒子係選自由矽砂、粒狀碳酸鈣、矽藻土粒、粒狀黏土及浮石所成之群組中之至少1種。The solid preparation for controlling rice pests according to claim 2 or 3, wherein the aforementioned nuclear particles are at least one selected from the group consisting of silica sand, granular calcium carbonate, diatomaceous earth particles, granular clay, and pumice . 如請求項2~4中任一項之水稻害蟲防除用固形製劑,其中,前述增量劑係選自由黏土、碳酸鈣、高嶺土及二氧化矽所成之群組中之至少1種。The solid formulation for controlling rice pests according to any one of claims 2 to 4, wherein the aforementioned extender is at least one selected from the group consisting of clay, calcium carbonate, kaolin, and silica. 如請求項2~5中任一項之水稻害蟲防除用固形製劑,其中,前述結合劑係選自由流動石蠟、植物油脂、聚乙二醇及聚丙二醇所成之群組中之至少1種。The solid formulation for controlling rice pests according to any one of claims 2 to 5, wherein the aforementioned binding agent is at least one selected from the group consisting of flowing paraffin, vegetable oil, polyethylene glycol, and polypropylene glycol. 如請求項1之水稻害蟲防除用固形製劑,其係擠出型粒劑,前述固體載體包含增量劑,前述界面活性劑包含造粒性改良劑及崩壞・分散劑。Such as the solid preparation for controlling rice pests of claim 1, which is an extruded granule, the solid carrier includes an extender, and the surfactant includes a granulation modifier and a collapse/dispersant. 如請求項7之水稻害蟲防除用固形製劑,其中,前述增量劑係選自由黏土、滑石、碳酸鈣、高嶺土、二氧化矽及膨潤土所成之群組中之至少1種。Such as the solid preparation for controlling rice pests of claim 7, wherein the aforementioned extender is at least one selected from the group consisting of clay, talc, calcium carbonate, kaolin, silica and bentonite. 如請求項7或8之水稻害蟲防除用固形製劑,其中,前述造粒性改良劑係選自由月桂基硫酸鈉、二烷基磺基琥珀酸鈉及烷基苯磺酸鈉所成之群組中之至少1種。The solid formulation for controlling rice pests according to claim 7 or 8, wherein the aforementioned granulation improving agent is selected from the group consisting of sodium lauryl sulfate, sodium dialkylsulfosuccinate and sodium alkylbenzene sulfonate At least one of them. 如請求項7~9中任一項之水稻害蟲防除用固形製劑,其中,前述崩壞・分散劑係選自由木質素磺酸鈉、木質素磺酸鈣、萘磺酸鈉福爾馬林縮合物、聚丙烯酸鈉、聚氧乙烯烷基醚硫酸鈉、聚氧化烯苯乙烯苯基醚硫酸鈉、聚氧化烯苯乙烯苯基醚磷酸鈉及聚氧乙烯・聚氧丙烯聚合物硫酸鈉所成之群組中之至少1種。Such as the solid formulation for controlling rice pests in any one of claims 7-9, wherein the aforementioned collapse and dispersing agent is selected from the group consisting of sodium lignosulfonate, calcium lignosulfonate, and sodium naphthalenesulfonate formalin condensation It is made of sodium polyacrylate, sodium polyoxyethylene alkyl ether sulfate, polyoxyalkylene styrene phenyl ether sodium sulfate, polyoxyalkylene styrene phenyl ether sodium phosphate, and polyoxyethylene/polyoxypropylene polymer sodium sulfate At least 1 in the group. 如請求項7~10中任一項之水稻害蟲防除用固形製劑,其中,前述結合劑係選自由聚乙烯醇、糊精、糖類、羧基甲基纖維素鈉、羥基丙基甲基纖維素及甲基纖維素所成之群組中之至少1種。The solid preparation for controlling rice pests according to any one of claims 7 to 10, wherein the aforementioned binding agent is selected from polyvinyl alcohol, dextrin, sugars, sodium carboxymethyl cellulose, hydroxypropyl methyl cellulose and At least one of the group formed by methyl cellulose. 一種水稻害蟲防除方法,其係包含將如請求項1~11中任一項之水稻害蟲防除用固形製劑的有效量,施用在選自由水稻害蟲、水稻、土壤及田水面所成之群組中之至少1種之步驟。A method for controlling rice pests, which comprises applying an effective amount of a solid preparation for controlling rice pests according to any one of claims 1 to 11 to the group selected from the group consisting of rice pests, rice, soil, and field surface At least one of the steps. 如請求項12之水稻害蟲防除方法,其中,前述水稻害蟲係選自由飛蝨類及二化螟類所成之群組中之至少1種。According to claim 12, the method for controlling rice pests, wherein the aforementioned rice pests are selected from at least one of the group consisting of planthoppers and Chilo suppressalis. 如請求項12或13之水稻害蟲防除方法,其中,前述水稻害蟲為藥劑抵抗性害蟲。According to claim 12 or 13, the method for controlling rice pests, wherein the aforementioned rice pests are pesticide-resistant pests. 如請求項12~14中任一項之水稻害蟲防除方法,其中,前述水稻害蟲防除用固形製劑的有效量以前述有效成分量計為耕地每10公畝1g~1kg。According to the method for controlling rice pests in any one of claims 12 to 14, wherein the effective amount of the solid preparation for controlling rice pests is 1 g-1 kg per 10 ares of cultivated land based on the amount of the effective ingredients. 一種水稻害蟲防除用固形製劑之製造方法,其係如請求項2~6中任一項之水稻害蟲防除用固形製劑之製造方法,其特徵為包含: 於前述核粒子加入前述結合劑,或前述結合劑及前述界面活性劑使其濕潤,而得到濕潤核粒子之濕潤步驟、與 混合前述有效成分、前述界面活性劑及前述增量劑,或前述有效成分及前述增量劑並粉碎,而得到第1混合粉碎物之混合粉碎步驟、與 混合前述濕潤核粒子與第1混合粉碎物,得到前述濕潤核粒子的表面以第1混合粉碎物被覆的被覆型粒劑之步驟。A method for manufacturing a solid preparation for controlling rice pests, which is the method for manufacturing a solid preparation for controlling rice pests according to any one of Claims 2 to 6, characterized by comprising: Adding the aforementioned binding agent, or the aforementioned binding agent and the aforementioned surfactant to the aforementioned core particles to make them wet to obtain the wetting step of the wet core particles, and Mixing the aforementioned active ingredient, the aforementioned surfactant and the aforementioned extender, or the aforementioned active ingredient and the aforementioned extender and pulverizing to obtain the first mixing and pulverizing step of mixing and pulverizing, and The step of mixing the wet core particles and the first mixed and pulverized product to obtain a coated granule in which the surface of the wet core particles is covered with the first mixed and pulverized product. 一種水稻害蟲防除用固形製劑之製造方法,其係如請求項7~11中任一項之水稻害蟲防除用固形製劑之製造方法,其特徵為包含: 混合前述有效成分、前述增量劑及前述結合劑並粉碎,或混合前述有效成分、前述增量劑及前述結合劑與前述造粒性改良劑及/或前述崩壞・分散劑並粉碎,而得到第2混合粉碎物之混合粉碎步驟、與 捏合第2混合粉碎物及水,或捏合第2混合粉碎物及水與前述造粒性改良劑及/或前述崩壞・分散劑,而得到捏合物之捏合步驟、與 將前述捏合物以擠出型造粒機成型,而得到擠出型粒劑之步驟。A method for manufacturing a solid preparation for controlling rice pests, which is the method for manufacturing a solid preparation for controlling rice pests according to any one of Claims 7 to 11, which is characterized by comprising: Mix the aforementioned active ingredient, the aforementioned extender, and the aforementioned binder and pulverize, or mix the aforementioned active ingredient, the aforementioned extender, and the aforementioned binder with the aforementioned granulation modifier and/or the aforementioned collapse/dispersant and pulverize, and The mixing and pulverizing step of obtaining the second mixed and pulverized product, and Kneading the second mixed and pulverized product and water, or kneading the second mixed and pulverized product and water with the aforementioned granulation modifier and/or the aforementioned collapse and dispersant to obtain a kneaded product, and The step of forming the aforementioned kneaded mixture with an extrusion granulator to obtain extruded granules.
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