JP2007039420A - Highly stable agent - Google Patents
Highly stable agent Download PDFInfo
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- JP2007039420A JP2007039420A JP2005243380A JP2005243380A JP2007039420A JP 2007039420 A JP2007039420 A JP 2007039420A JP 2005243380 A JP2005243380 A JP 2005243380A JP 2005243380 A JP2005243380 A JP 2005243380A JP 2007039420 A JP2007039420 A JP 2007039420A
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- rodenticide
- active ingredient
- stabilizing
- antioxidant
- epigallocatechin
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Abstract
Description
本発明は、殺そ剤の有効成分安定化方法、特に小麦粉等油脂を含有する穀紛に抗凝血剤を有効成分として配合調整した殺そ剤に関する。The present invention relates to a method for stabilizing an active ingredient of a rodenticide, and more particularly to a rodenticide prepared by blending and adjusting an anticoagulant as an active ingredient in a cereal powder containing fats and oils such as wheat flour.
殺そ剤は、有効成分である毒物劇物を鼠の食物に混合した毒えさとして調整され、ネズミ駆除に用いられる。The rodenticide is prepared as a poison that mixes the poisonous and deleterious substances, which are active ingredients, with the food of frogs, and is used to control rats.
殺そ剤には、その使用する範囲によって農地等に用いられる農薬と家屋内等で用いられる医薬部外品が存在する。There are agrochemicals used in agricultural land and quasi-drugs used in households and the like, depending on the range used.
また、製剤の形態も、単に粉末状のもの、穀物の表面を有効成分でコーティングしたもの、ロウなどで固めたもの、小麦粉や砂糖などを有効成分とともに練り、焼き上げたもの等様々なものが存在する。これらの殺そ剤はネズミのみならず人を含む哺乳動物一般に有効であるため、誤食防止の目的で、色素および誤食防止剤が混ぜられることが法規上で決められている。In addition, there are various forms of preparations, such as powders, grains coated with active ingredients, hardened with wax, etc., flour and sugar kneaded with active ingredients and baked To do. Since these rodenticides are effective not only for mice but also for mammals including humans, it is stipulated by the law that pigments and anticorrosive agents are mixed for the purpose of preventing accidental eating.
殺そ剤の歴史は古く、かつてはかなり毒性の強いものがもちいられていた事もあったが、誤用による危険性が認識され比較的毒性の低い穏やかな製剤が好まれる様になってきた。Although the history of rodenticides has been long and once used to be quite toxic, the danger of misuse has been recognized and mild formulations with relatively low toxicity have come to be preferred.
殺そ剤に用いられる有効成分には様々なものがあるが、その中で特に汎用されているのが抗凝血剤すなわち血液凝固阻止作用をもつ蓄積性のある有機化合物を配合した殺そ剤である。クマリン系のワルファリンはその中でも最も有名なものであり、ネズミがワルファリン0.1%含有の殺そ剤を少量ずつ連続して食べることにより、内出血にて10日前後で死亡する。この成分の問題は、一回の摂取では死なないこと、連続して摂取しない場合は致死までの日数が長くなること、そしてワルファリンに対する抵抗性のネズミが生じることである。There are various active ingredients used in rodenticides. Among them, the most widely used is an anticoagulant, that is, a rodenticide containing an organic compound with an anticoagulant or anticoagulant action. . Coumarin-based warfarin is the most famous among them, and mice die in about 10 days due to internal bleeding when they eat small amounts of a killer containing 0.1% of warfarin continuously. The problem with this component is that it does not die after a single ingestion, if it is not taken continuously, the days to death are increased, and a rat with resistance to warfarin is produced.
そのために、少量の摂取でネズミの体内に蓄積しやすく、より短時間で致死する新成分の研究が進められ、クマテトラリル、クロロファシノン、ダイファシノン、ブロマジオロン、ブロディファコム等の成分が各国にて開発、使用されてきた。For this reason, research on new ingredients that are easy to accumulate in the body of a mouse with a small amount of ingestion and kill in a shorter time is underway, and ingredients such as coumatetralyl, chlorofacinone, difacsinone, bromadiolone, brodifacom are developed in each country, Have been used.
これらの有効成分は、より低濃度で、より短期間でネズミに対して致死効果を示すように研究され、特にダイファシノン、ブロマジオロン、ブロディファコム等はその製剤中の含有量が0.005%すなわち50ppmと少なくても、ワルファリンより短期間でネズミが致死するものである。These active ingredients have been studied to have a lethal effect on rats at lower concentrations and in a shorter period of time. In particular, difacsinone, bromadiolone, brodiffacom, etc. have a 0.005% or 50 ppm content in the formulation. At least, rats will be killed in a shorter period of time than warfarin.
しかしながら製剤中の含有量が極めて少量であるがために、様々な要因の物理的化学的影響を受けやすく製剤中の安定性に欠ける場合がある。特許文献1は、有効成分の安定化を目的としたものである。However, since the content in the preparation is extremely small, it is easily affected by physical and chemical influences of various factors and may lack stability in the preparation. Patent document 1 aims at stabilization of an active ingredient.
殺そ剤を製造する場合、ネズミの好む油脂を含有する穀粉に有機化合物である有効成分を加え、造粒し、製品と成したものは、時間の経過と共に有効成分が分解してしまう。長期の保存、流通に耐えるものとしては従来、脱酸素剤を用いている。しかしながら、これらの従来法においては、長期間の保存に耐えるものとしては未だ不十分であり、又生産性の低下を避けられなかった。When manufacturing a rodenticide, the active ingredient which is an organic compound is added to the flour containing the fats and oils which a mouse likes, and it granulates, and what was formed into a product will decompose | disassemble an active ingredient with progress of time. Conventionally, an oxygen scavenger is used to withstand long-term storage and distribution. However, these conventional methods are still insufficient to withstand long-term storage, and a reduction in productivity cannot be avoided.
本発明は、上記の方法の如く製品を充填する際に脱酸素剤を添付する等、生産性の低下をもたらさず、容易に有効成分が長期間安定する薬剤及びその製造方法を提供する。The present invention provides a drug in which an active ingredient is easily stabilized for a long period of time without causing a decrease in productivity, such as attaching an oxygen scavenger when filling a product as in the above method, and a method for producing the same.
本発明者等は、上記薬剤を製造する方法について鋭意研究開発を行った結果、油脂を含む穀紛を使用する場合に、カテキン類と酸化防止剤を組み合わせて配合することが、有効成分を安定に保つことの知見を得た。即ち定法に従い、穀紛と有効成分を配合するその際に、カテキン類及び酸化防止剤を添加し薬剤として製することにより、無添加品またはカテキン類のみの配合品に比較して4〜5倍の期間、有効成分の安定性を保持することができる。As a result of earnest research and development on the method for producing the above-mentioned drug, the present inventors have formulated a combination of catechins and antioxidants when using cereal flour containing fats and oils. Gained the knowledge of keeping In other words, according to the regular method, when blending cereal flour and active ingredients, catechins and antioxidants are added and manufactured as a drug, which is 4-5 times compared to additive-free products or catechin-only products. During this period, the stability of the active ingredient can be maintained.
本発明に用いることのできる殺そ剤の有効成分は、クマリン系化合物として、例えばワルファリン、クマリン、クマテトラリルなど、インダンジオン系化合物としては、例えばクロロファシノン、ダイファシノン、ピンドン、バロンなど、トリアリール系化合物としては例えばジフェチアロン、ジフェナクム、ブロディファコム、ブロマジオロン、フロクマフェンなどである。これらの有効成分は、製剤中にその用途と種類に応じて0.0001%から1%まで配合することができる。The active ingredient of the rodenticide that can be used in the present invention is a coumarin-based compound, for example, warfarin, coumarin, coumatetralyl, etc., and the indandione-based compound, for example, chlorofacinone, difacsinone, pindon, baron, etc., triaryl-based compounds Examples thereof include difetialone, diphenacum, brodiffacom, bromazirone, furocumafen and the like. These active ingredients can be blended in the preparation from 0.0001% to 1% depending on the use and type.
本発明には油脂を含む穀紛として、小麦粉、トウモロコシ粉、大豆粉、生ヌカ、破砕ピーナッツ、落花生等が使用できるが、この他にも油脂類を含む穀紛であれば使用することができる。In the present invention, wheat flour, corn flour, soybean flour, raw nutka, crushed peanuts, peanuts, etc. can be used as cereal flour containing fats and oils, but cereal flour containing fats and oils can also be used. .
本発明に用いられるカテキン類とは、食品添加物の既存添加物名簿に掲載されているカテキンのことであり、その規格に適合するものならばどのようなものでも使用できる。その成分はカテキン、エピガロカテキン、カテキンガレート、エピガロカテキンガレートの混合物である。カテキン類は殺そ剤の製剤中に0.006〜0.020重量%、好ましくは0.008〜0.013重量%加えることができる。The catechins used in the present invention are catechins listed in the existing additive list of food additives, and any catechin can be used as long as it conforms to the standard. The component is a mixture of catechin, epigallocatechin, catechin gallate, epigallocatechin gallate. The catechins can be added in an amount of 0.006 to 0.020% by weight, preferably 0.008 to 0.013% by weight, in the preparation of the rodenticide.
また、本発明に用いる酸化防止剤には、食品添加物として使用されている脂溶性の酸化防止剤であればいずれも使用できるが、特に好ましくはブチルヒドロキシアニソール(BHA)が有効である。酸化防止剤(ブチルヒドロキシアニソール)は製剤中に0.01〜0.04重量%、好ましくは0.02〜0.03重量%となるよう加えられる。In addition, as the antioxidant used in the present invention, any fat-soluble antioxidant used as a food additive can be used, but butylhydroxyanisole (BHA) is particularly effective. Antioxidant (butylhydroxyanisole) is added to the preparation in an amount of 0.01 to 0.04% by weight, preferably 0.02 to 0.03% by weight.
殺そ剤は、その必要上、喫食剤、結合剤、防腐剤、色素、誤食防止剤等が配合される。喫食剤としては、油脂を含む穀紛の他、糖類、魚粉、澱粉等も加えることができる。The rodenticide is blended with an eating agent, a binder, an antiseptic, a pigment, an anticorrosive agent, and the like. As a edible agent, saccharides, fish meal, starch, etc. can be added in addition to cereal flour containing fats and oils.
本発明により、有効成分の分解を長期間防止することができ、製造コストの低減、商品サイクルの延長および資源の有効利用が可能となる。According to the present invention, the active ingredient can be prevented from being decomposed for a long period of time, and the manufacturing cost can be reduced, the product cycle can be extended, and the resources can be effectively used.
以下、上記知見を基に完成された本発明を実施する最良の形態を記述する。先ず、錬合機に油脂を含む穀紛、有効成分、カテキン及び酸化防止剤を投入し、攪拌する。続いて水を添加し、錬合する。錬合物を圧延機により、板状に成型する。次にカッターを用いて粒状にカットし、加熱乾燥して適当な容器に充填し、密封して完成品とする。Hereinafter, the best mode for carrying out the present invention completed based on the above knowledge will be described. First, cereal powder containing fats and oils, active ingredients, catechins and antioxidants are charged into a kneader and stirred. Then add water and smelt. The kneaded product is formed into a plate shape by a rolling mill. Next, it is cut into granules using a cutter, dried by heating, filled into a suitable container, and sealed to obtain a finished product.
以下、実施例を示すがこれに限定されるものではない。
錬合機に小麦粉62.38Kg、砂糖5Kg、トウモロコシ粉32.375Kg、デヒドロ酢酸ナトリウム0.02Kg、ダイファシノン(有効成分)0.005Kg、カテキン類0.01Kg、ブチルヒドロキシアニソール0.02Kgを入れ、10分間攪拌混合する。続いて、ポリビニルアルコール0.2Kgを溶かした水3リットルを加え、20分間錬合する。次に、圧延し、カットして、150℃で30分間乾燥し、適当な容器に充填し、密封して完成品とする。カテキン類およびブチルヒドロキシアニソールという安定化剤を加えない比較処方品も同様にして製する。該薬剤(完成品および比較処方品)を40℃、湿度75%の環境に放置したときの有効成分の経時的残存率を表1に示す。Examples are shown below, but are not limited thereto.
Add 62.38 kg of wheat flour, 5 kg of sugar, 32.375 kg of corn flour, 0.02 kg of sodium dehydroacetate, 0.005 kg of difacsinone (active ingredient), 0.01 kg of catechins, 0.02 kg of butylhydroxyanisole to the kneader. Stir and mix for a minute. Subsequently, 3 liters of water in which 0.2 kg of polyvinyl alcohol is dissolved is added and smelted for 20 minutes. Next, it is rolled, cut, dried at 150 ° C. for 30 minutes, filled into a suitable container, and sealed to obtain a finished product. Comparative formulations without the addition of stabilizers such as catechins and butylhydroxyanisole are produced in the same manner. Table 1 shows the residual ratio of the active ingredient over time when the drug (finished product and comparative prescription product) is left in an environment of 40 ° C. and 75% humidity.
Claims (4)
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JP2005243380A JP2007039420A (en) | 2005-07-29 | 2005-07-29 | Highly stable agent |
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Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP2933290A4 (en) * | 2012-12-11 | 2016-11-09 | Lotte Fine Chemical Co Ltd | Composition for forming complex, complex formed therefrom, and composition for oral administration including said complex |
CN116158428A (en) * | 2021-11-25 | 2023-05-26 | 沈阳中化农药化工研发有限公司 | Liquid preparation containing biphenyl structure |
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2005
- 2005-07-29 JP JP2005243380A patent/JP2007039420A/en active Pending
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP2933290A4 (en) * | 2012-12-11 | 2016-11-09 | Lotte Fine Chemical Co Ltd | Composition for forming complex, complex formed therefrom, and composition for oral administration including said complex |
CN116158428A (en) * | 2021-11-25 | 2023-05-26 | 沈阳中化农药化工研发有限公司 | Liquid preparation containing biphenyl structure |
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