JP2008031140A - Mosquito repelling incense coil for controlling infectious disease-mediating mosquito - Google Patents
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Abstract
Description
本発明は、感染症媒介蚊防除用蚊取線香に関するものである。 The present invention relates to a mosquito coil for controlling infection-borne mosquitoes.
世界には多種の蚊が生息し、人を刺咬・吸血するだけでなく、感染症を媒介して重大な被害をもたらす。例えば、いくつかの感染症とこれを媒介する蚊の種類について、下記の関連性が知られている。
・マラリア：ハマダラカ類（Anopheles dirus, A. minimus, A. gambiae, A. sinensis）、
・デング熱：ネッタイシマカ、ヒトスジシマカ、
・黄熱病：ネッタイシマカ、
・フィラリア症：ネッタイイエカ、アカイエカ、チカイエカ、
・日本脳炎：コガタアカイエカ、
・ウエストナイル熱：イエカ、ヤブカなど３０〜４０種、
・チクングンヤ：ネッタイシマカ、ヒトスジシマカ。
これらの感染症から身を守る方法は、適当なワクチンが完成されていない今日、蚊に刺されないことが第一で、特に開放的な住居では蚊取線香の使用が最適である。蚊帳にピレスロイドを含浸させたものも使用されているが、就寝中しか使えないこと、蚊帳の中は暑苦しいことなど、使用性に問題が多い。
There are many types of mosquitoes in the world that not only bite and suck blood, but also cause serious damage through infection. For example, the following relationships are known for several infectious diseases and the types of mosquitoes that carry them.
Malaria: Anopheles dirus, A. minimus, A. gambiae, A. sinensis
・ Dengue fever: Aedes aegypti, Aedes aegypti,
・ Yellow fever: Aedes aegypti
• Filariasis: Attached squid, squid, chikaeka,
・ Japanese encephalitis: Culex mosquito,
・ West Nile fever: 30-40 kinds such as squid and yabuka,
Chikungunya: Aedes aegypti, Aedes aegypti.
The best way to protect yourself from these infections is to avoid mosquito bites today, when appropriate vaccines have not been completed, and the use of mosquito coils is the best choice, especially in open houses. Although mosquito nets impregnated with pyrethroids are also used, there are many problems in usability, such as being usable only while sleeping and being hot in mosquito nets.
これまで蚊取線香の有効成分としては、ピレスロイド系殺虫成分のアレスリン類が世界的に使用されてきたが、主要種のネッタイイエカ、ネッタイシマカ、ヒトスジシマカ類に対して効力が十分でないことがあり、より的確な新しい殺虫成分の開発が求められている。例えば、文献［Biosci. Biotechnol. Biochem., 68(1) 170, 2004］（非特許文献１）によれば、新規ピレスロイド系殺虫成分のメトフルトリン［４−メトキシメチル−２，３，５，６−テトラフルオロベンジル ２，２−ジメチル−３−（１−プロペニル）シクロプロパンカルボキシラート］を含有する蚊取線香がネッタイイエカやアカイエカに対して、ｄ−アレスリンの１／４０〜１／２０の濃度で、ｄ−アレスリン蚊取線香とほぼ同等のノックダウン効果を示したことが報告されている。しかしながら、メトフルトリンは、合成が複雑で製造コストも高く、ｄ−アレスリン蚊取線香よりも数倍殺虫効力の高い蚊取線香を得ようとすると、安価に供給できないという難点を有している。 Up to now, the active ingredient of mosquito coils has been the pyrethroid insecticidal ingredient, Alleslin, which has been used globally. However, it may not be effective enough against the major species of Aedes aegypti, Aedes aegypti, and Aedes aegypti, making them more accurate New insecticidal ingredients are being sought. For example, according to the document [Biosci. Biotechnol. Biochem., 68 (1) 170, 2004] (Non-Patent Document 1), a novel pyrethroid insecticide component, metfurthrin [4-methoxymethyl-2,3,5,6- The mosquito coil incense containing tetrafluorobenzyl 2,2-dimethyl-3- (1-propenyl) cyclopropanecarboxylate] has a concentration of 1/40 to 1/20 of d-arethrin, compared to Aedes mosquitoes and squids, It has been reported that the knockdown effect was almost the same as that of d-alleslin mosquito coils. However, metofluthrin has a difficulty in that it cannot be supplied at low cost when it is attempted to obtain a mosquito coil incense that is complicated in synthesis and high in production cost and has several times higher insecticidal efficacy than d-areslin mosquito coil.
かかる現状において、ネッタイイエカやネッタイシマカ等に卓効を示し、かつ製造コストが安価な殺虫成分の探索は、特に東南アジアやアフリカ等の熱帯地域住民を感染症の被害から守っていくうえで極めて効果的な対策手段であり、そのためには現地において実際にネッタイイエカやネッタイシマカ等に対する殺虫効力試験を行ってはじめて効力評価が可能となる。本発明者らが着目した４−メトキシメチル−２，３，５，６−テトラフルオロベンジル ２，２，３，３−テトラメチルシクロプロパンカルボキシレートは、特開昭５７−１６５３４３号公報（特許文献１）にて公知の化合物として開示されており、特開２００１−３０２５９１号公報（特許文献２）にはこの化合物を含有する蚊取線香が開示されている。しかしながら、特許文献２の蚊取線香は、単に製剤の一例として開示されたに過ぎず、感染症媒介蚊対策を意図したものでなく、しかも効力増強のために、他の薬剤を配合することについては、格別の検討が行われているわけではない。
そこで、本発明者らは、４−メトキシメチル−２，３，５，６−テトラフルオロベンジル ２，２，３，３−テトラメチルシクロプロパンカルボキシレートを殺虫成分として採用したうえで、これとある特定の効力増強剤との組み合わせについて鋭意検討を重ね、本発明を完成するに至った。
Therefore, the present inventors have adopted 4-methoxymethyl-2,3,5,6-tetrafluorobenzyl 2,2,3,3-tetramethylcyclopropanecarboxylate as an insecticidal component and have this. The present invention has been completed through extensive studies on combinations with specific potency enhancers.
本発明は、ネッタイイエカやネッタイシマカ等に卓効を示し、かつ安価に製造でき、しかも人畜に対する安全性に優れた感染症媒介蚊防除用蚊取線香を提供することを目的とする。 An object of the present invention is to provide a mosquito coil for controlling infectious disease mosquitoes that exhibits excellent effects on Aedes mosquitoes, Aedes aegypti, etc., can be manufactured at low cost, and is excellent in safety for human livestock.
本発明は、上記課題を解決するため、次のような構成を採用する。
（１）有効成分として、下記化学式
で表される、４−メトキシメチル−２，３，５，６−テトラフルオロベンジル ２，２，３，３−テトラメチルシクロプロパンカルボキシレートを０．０１〜０．５質量％含有し、かつ、効力増強剤として、Ｎ−（２−エチルヘキシル）−ビシクロ［２，２，１］−ヘプタ−５−エン−２，３−ジカルボキシイミドを、有効成分量に対して０．１倍量以上配合してなる感染症媒介蚊防除用蚊取線香。
（２）効力増強剤として、Ｎ−（２−エチルヘキシル）−ビシクロ［２，２，１］−ヘプタ−５−エン−２，３−ジカルボキシイミドを、有効成分量に対して２．０倍量以上配合してなる（１）記載の感染症媒介蚊防除用蚊取線香。
In order to solve the above problems, the present invention employs the following configuration.
(1) As an active ingredient, the following chemical formula
Containing 4-methoxymethyl-2,3,5,6-tetrafluorobenzyl 2,2,3,3-tetramethylcyclopropanecarboxylate represented by the formula: As an effect enhancer, N- (2-ethylhexyl) -bicyclo [2,2,1] -hept-5-ene-2,3-dicarboximide is added in an amount of 0.1 times or more with respect to the amount of active ingredient. A mosquito coil for controlling infection vector mosquitoes.
(2) As an efficacy enhancer, N- (2-ethylhexyl) -bicyclo [2,2,1] -hept-5-ene-2,3-dicarboximide is 2.0 times the active ingredient amount. A mosquito coil for controlling infectious disease mosquitoes as described in (1), which is formulated in an amount or more.
本発明の感染症媒介蚊防除用蚊取線香は、前記有効成分と前記効力増強剤との相乗効果に基づき、ネッタイイエカやネッタイシマカ等に卓効を示し、かつ安価に製造でき、しかも人畜に対する安全性に優れているので、その実用性は極めて高い。 The mosquito coil for controlling infectious disease mosquitoes of the present invention is based on the synergistic effect of the active ingredient and the potency enhancer, and is effective for Aedes aegypti, Aedes aegypti, etc., can be manufactured at low cost, and is safe for human animals Therefore, its practicality is extremely high.
本発明の感染症媒介蚊防除用蚊取線香においてベースとなる有効成分は、４−メトキシメチル−２，３，５，６−テトラフルオロベンジル ２，２，３，３−テトラメチルシクロプロパンカルボキシラート（以降、化合物Ａと称する）である。
この化合物は既に公知であり、特許文献１に記載の合成方法に基づき、当該シクロプロパンカルボン酸、又はその反応性誘導体と、４−メトキシメチル−２，３，５，６−テトラフルオロベンジルアルコール、又はその反応性誘導体とを反応させることによって調製しえる。
カルボン酸の反応性誘導体としては、例えば酸ハライド、酸無水物、カルボン酸低級アルキルエステル、アルカリ金属塩、あるいは有機第３級塩基との塩があげられる。一方、アルコールの反応性誘導体としては、例えばクロライド、ブロマイド、ｐ−トルエンスルホン酸エステル等があげられる。反応は適当な溶媒中で必要により脱酸剤又は触媒としての有機又は無機塩基又は酸の存在下に必要により加熱下に行われる。
The active ingredient which is the base in the mosquito coil for controlling infection-borne mosquitoes of the present invention is 4-methoxymethyl-2,3,5,6-tetrafluorobenzyl 2,2,3,3-tetramethylcyclopropanecarboxylate (Hereinafter referred to as Compound A).
This compound is already known, and based on the synthesis method described in Patent Document 1, the cyclopropanecarboxylic acid or a reactive derivative thereof, 4-methoxymethyl-2,3,5,6-tetrafluorobenzyl alcohol, Alternatively, it can be prepared by reacting with a reactive derivative thereof.
Examples of the reactive derivative of carboxylic acid include acid halides, acid anhydrides, carboxylic acid lower alkyl esters, alkali metal salts, and salts with organic tertiary bases. On the other hand, examples of the reactive derivative of alcohol include chloride, bromide, and p-toluenesulfonic acid ester. The reaction is carried out in a suitable solvent, if necessary, in the presence of an organic or inorganic base or acid as a deoxidizing agent or catalyst as necessary.
化合物Ａは、常温で液状を呈し有機溶剤に一般に容易に溶解するが、当該有機溶剤に溶解した化合物Ａと木粉等の蚊取線香基材と混合して本発明の感染症媒介蚊防除用蚊取線香を構成する。
蚊取線香中の有効成分含量は、各種感染症媒介蚊に対する殺虫効力ならびに経済性等を考慮して０．０１〜０．５質量％、好ましくは０．０３〜０．２質量％に設定される。
Compound A is liquid at room temperature and is generally easily dissolved in an organic solvent. However, compound A dissolved in the organic solvent and a mosquito coil incense base material such as wood powder are mixed to control the infection vector mosquito of the present invention. Consists of mosquito coils.
The active ingredient content in the mosquito coil is set to 0.01 to 0.5% by mass, preferably 0.03 to 0.2% by mass, taking into account the insecticidal efficacy against various infectious disease mosquitoes and economic efficiency. The
本発明の感染症媒介蚊防除用蚊取線香は、効力増強剤として、Ｎ−（２−エチルヘキシル）−ビシクロ［２，２，１］−ヘプタ−５−エン−２，３−ジカルボキシイミド（以降、効力増強剤Ａと称する）を、有効成分量に対して０．１倍量以上、好ましくは２．０倍量以上配合することを特徴とする。 The mosquito coil for controlling infection-borne mosquitoes of the present invention has N- (2-ethylhexyl) -bicyclo [2,2,1] -hept-5-ene-2,3-dicarboximide ( Hereinafter, the effect enhancer A) is blended in an amount of 0.1 times or more, preferably 2.0 times or more of the amount of the active ingredient.
従来、種々製剤において、ピペロニルブトキサイド、Ｎ−（２−エチルヘキシル）−ビシクロ［２，２，１］−ヘプタ−５−エン−２，３−ジカルボキシイミド、Ｎ−（２−エチルヘキシル）−１−イソプロピル−４−メチルビシクロ［２，２，２］−オクト−５−エン−２，３−ジカルボキシイミド、オクタクロロジプロピルエーテルなどのピレスロイド用共力剤を混用することがしばしば行われてきた。
すなわち、上記ピレスロイド用共力剤は、例えば液剤や粉剤等に用いた場合、それ自体では生物活性を示さないが、ピレスロイドと混用した場合、ピレスロイドの効力を増強することが知られている。共力剤のメカニズムについては多くの報告があり、例えば、昆虫体内で自らが代謝分解を受けてピレスロイドの酸化的解毒代謝を阻害したり、あるいはピレスロイドの皮膚への浸透を促進し、神経系作用点への到達を容易にすることによって、ピレスロイドの殺虫効力を高めることなどが知られている。しかしながら、かかる共力剤の作用機構は当然のことながら昆虫の種類に大きく依存し、共力剤による共力効果は通常１０〜２０％程度にとどまるのが一般的である。
Conventionally, in various preparations, piperonyl butoxide, N- (2-ethylhexyl) -bicyclo [2,2,1] -hept-5-ene-2,3-dicarboximide, N- (2-ethylhexyl) Often, pyrethroid synergists such as -1-isopropyl-4-methylbicyclo [2,2,2] -oct-5-ene-2,3-dicarboximide and octachlorodipropyl ether are mixed. I have been.
That is, when the above-mentioned synergist for pyrethroid is used for, for example, a liquid or a powder, it does not exhibit biological activity by itself, but is known to enhance the efficacy of pyrethroid when mixed with pyrethroid. There are many reports on the mechanism of synergists. For example, the body itself undergoes metabolic degradation to inhibit the oxidative detoxification metabolism of pyrethroids, or promote the penetration of pyrethroids into the skin, acting on the nervous system. It is known to increase the insecticidal efficacy of pyrethroids by making it easy to reach the point. However, the mechanism of action of such a synergist depends naturally on the type of insect, and the synergistic effect of the synergist is generally only about 10 to 20%.
これに対し、本発明者らは線香形態でのある種配合剤の作用を鋭意検討し、化合物Ａに効力増強剤Ａを配合することによって、蚊取線香の殺虫効力が驚くべきことに２〜３倍増強されることを発見した。この事実は、従来ピレスロイド製剤に使用されている共力剤のメカニズム、即ち上述した昆虫生理学的機構だけでは説明できず、別の原因として、ある物質が有効成分の揮散率上昇に寄与し有効成分の気中濃度を高めたことや、揮散した有効成分の拡散をある物質が助長したことなど、物理的な作用も貢献しているものと考えられる。更に、化合物Ａに効力増強剤Ａを加えることによって、化合物Ａの揮散率が５〜１０％上昇することを実験により確認した。
即ち、本願発明は、線香形態において、化合物Ａが効力増強剤Ａと適量な組み合わせで併用した場合、線香に含まれる水や効力増強剤Ａとともに一種の水蒸気蒸留によって、最も効率的に揮散し、拡散が助長され、昆虫生理学的な効力増強効果と相まって、顕著な相乗効果を奏し得ることを基本的技術思想としており、このことは今までにない全く新規な知見である。
On the other hand, the present inventors diligently studied the action of a certain compounding agent in the form of an incense stick, and by adding the efficacy enhancer A to Compound A, the insecticidal efficacy of the mosquito coil is surprisingly 2 to 2. It was found to be 3 times stronger. This fact cannot be explained only by the mechanism of the synergist conventionally used in pyrethroid preparations, that is, the insect physiological mechanism described above. As another cause, a certain substance contributes to an increase in the volatilization rate of the active ingredient and the active ingredient. It is thought that the physical action also contributes, such as raising the concentration in the air and promoting the diffusion of the volatilized active ingredient. Furthermore, it was confirmed by experiments that the volatilization rate of Compound A is increased by 5 to 10% by adding the potency enhancer A to Compound A.
That is, in the incense form, when the compound A is used in combination with the potency enhancer A in an appropriate amount, it is most efficiently volatilized by a kind of steam distillation together with water and potency enhancer A contained in the incense stick, The basic technical idea is that diffusion is facilitated and a remarkable synergistic effect can be achieved in combination with the effect of enhancing the physiological effects of insects. This is a completely new finding that has never been seen before.
ところで、Ｎ−（２−エチルヘキシル）−１−イソプロピル−４−メチルビシクロ［２，２，２］−オクト−５−エン−２，３−ジカルボキシイミド（以降、共力剤Ｓと称する）は、効力増強剤Ａと化学構造が類似するものの、化合物Ａの線香に併用した場合、効力増強効果は極めて低かった。この原因として、共力剤Ｓの加熱燻煙下での蒸散性が効力増強剤Ａに比べてかなり低いことが一因と考えられ、線香形態においては、有効成分と配合剤の蒸散物性が殺虫効力に密接に関与していることを裏付ける試験結果と評価することができる。 By the way, N- (2-ethylhexyl) -1-isopropyl-4-methylbicyclo [2,2,2] -oct-5-ene-2,3-dicarboximide (hereinafter referred to as synergist S) is Although the chemical structure is similar to that of potency enhancer A, the potency enhancing effect was extremely low when used in combination with compound A incense. This is thought to be due to the fact that the transpiration of the synergist S under heated soot is considerably lower than that of the potency enhancer A. In the incense incense form, the transpiration properties of the active ingredient and the compounding agent are insecticidal. It can be evaluated as a test result that confirms that it is closely related to efficacy.
本発明では、化合物Ａと効力増強剤Ａとの量的比率も重要である。即ち、効力増強剤Ａの有効成分量に対する配合量が０．１〜２．０倍量の範囲では、ＫＴ50値の指標で示されるノックダウン効果で高い効力増強効果が得られるものの、ＫＴ90値や致死率における効力増強効果は比較的小さい傾向が認められた。次に、効力増強剤Ａの配合量を２．０倍量以上に高めると、ＫＴ50値での改善は配合量に相応するほど大幅ではないが、ＫＴ90値や致死率における効力増強効果は顕著に増大し、効力増強剤Ａが確実、かつ相乗的にノックダウン効果ならびに致死作用を増強せしめ得ることが明らかとなった。このように、効力増強剤Ａの有効成分量に対する配合量は、２．０倍以上が好ましいが、桁違いの量を配合しても無意味であることはもちろんである。 In the present invention, the quantitative ratio between compound A and potency enhancer A is also important. That is, in the range amount of from 0.1 to 2.0 times relative to the amount of active ingredient enhancer A, although higher potency enhancing effect knockdown effect represented by an index of KT 50 values are obtained, KT 90 There was a relatively small tendency for the potency-enhancing effect on value and mortality. Next, when the compounding amount of the efficacy enhancer A is increased to 2.0 times or more, the improvement in the KT 50 value is not so large as to correspond to the compounding amount, but the efficacy enhancing effect on the KT 90 value and lethality is It was found that the potency enhancer A can remarkably increase the knockdown effect and lethal action synergistically and synergistically. Thus, although the compounding quantity with respect to the active ingredient amount of the efficacy enhancer A is preferably 2.0 times or more, it is of course meaningless even if an extraordinary quantity is blended.
本発明の実施形態として、効力増強剤の補助剤として、効力増強剤Ａに加えて更にアルキルベンゼンスルホン酸の低級アルキルアミン塩を配合してもよい。ここで、アルキルベンゼンスルホン酸のアルキル基はＣ8〜Ｃ14程度、一方、アルキルアミン塩の低級アルキル基はＣ２〜Ｃ4程度がよく、例えば、ドデシルベンゼンスルホン酸イソプロピルアミン塩やドデシルベンゼンスルホン酸エチルアミン塩を代表例としてあげることができる。
アルキルベンゼンスルホン酸の低級アルキルアミン塩の効力増強剤Ａに対する比率は、０．２〜１．０倍量の範囲が適当である。
As an embodiment of the present invention, in addition to the efficacy enhancer A, a lower alkylamine salt of alkylbenzene sulfonic acid may be further blended as an adjuvant for the efficacy enhancing agent. Wherein the alkyl group of the alkyl benzene sulfonic acid is about C 8 -C 14, whereas, lower alkyl group of the alkyl amine salt may be about C 2 -C 4, for example, dodecylbenzenesulfonic acid isopropylamine salt and dodecyl benzene sulfonic acid A typical example is an ethylamine salt.
The ratio of the alkylbenzenesulfonic acid lower alkylamine salt to the efficacy enhancer A is suitably in the range of 0.2 to 1.0 times.
蚊取線香基材としては、支燃剤や粘結剤があり、前者には、木粉、除虫菊抽出粕粉、茶葉の抽出粕粉、柑橘類の表皮粉、ココナッツシェル粉末等の植物性粉末や、木炭粉、素灰等の炭素粉末があげられる。また、後者の粘結剤としては、タブ粉、澱粉、メチルセルロース、カルボキシメチルセルロース等を例示できる。 As mosquito coils, there are flame retardants and binders, the former includes plant powders such as wood powder, pesticide extracted chrysanthemum powder, tea leaf extracted powder, citrus skin powder, coconut shell powder, Carbon powders such as charcoal powder and elementary ash are listed. Examples of the latter binder include tab powder, starch, methyl cellulose, carboxymethyl cellulose and the like.
本発明の感染症媒介蚊防除用蚊取線香には、必要により、色素、防腐剤、安定剤等が含有されてもよい。色素としては、例えばマラカイトグリーン等の有機染料があげられ、防腐剤としては、例えばソルビン酸、デヒドロ酢酸、ｐ−ヒドロキシ安息香酸等の酸、あるいはそれらの塩等が代表的である。また、安定剤としては、２,６−ジ−ターシャリーブチル−４−メチルフェノール（ＢＨＴ）や２,２’−メチレンビス（４−エチル−６−ターシャリーブチルフェノール）等があげられるがこれらに限定されない。 The mosquito coil for infectious disease control mosquito control according to the present invention may contain a dye, an antiseptic, a stabilizer and the like, if necessary. Examples of the pigment include organic dyes such as malachite green, and typical examples of the preservative include acids such as sorbic acid, dehydroacetic acid, p-hydroxybenzoic acid, and salts thereof. Examples of the stabilizer include 2,6-di-tert-butyl-4-methylphenol (BHT) and 2,2′-methylenebis (4-ethyl-6-tertiary butylphenol), but are not limited thereto. Not.
更に、本発明の趣旨を妨げない限りにおいて、他の殺虫、防虫成分、例えばピレトリン、アレスリン、プラレトリン、フラメトリン、トランスフルトリン、メトフルトリン、エムペントリン等の従来のピレスロイド系殺虫剤、殺菌剤、抗菌剤、忌避剤、あるいは芳香剤、消臭剤等を混合し、効力のすぐれた多目的組成物を得ることもできる。 Furthermore, as long as the gist of the present invention is not hindered, other insecticides and insect repellent components, such as conventional pyrethroid insecticides such as pyrethrin, allethrin, praretrin, flamethrin, transfluthrin, metfluthrin, empentrin, fungicides, antibacterial agents, A multipurpose composition having excellent efficacy can also be obtained by mixing repellents, fragrances, deodorants and the like.
本発明の感染症媒介蚊防除用蚊取線香を調製するにあたっては、何ら特別の技術を必要とせず、公知の製造方法を採用できる。例えば、プレミックス粉（有効成分や効力増強剤等を支燃剤の一部に含有させたもの）と残部の蚊取線香基材を混合したものに水を加えて混練し、続いて、押出機、打抜機によって成型後、乾燥して蚊取線香を製すればよい。また、蚊取線香基材のみを用いて成型後、これに有効成分等を含む液剤をスプレーあるいは塗布するようにしても構わない。 In preparing the mosquito coil for controlling infectious disease-mediated mosquitoes of the present invention, no special technique is required and a known production method can be employed. For example, premix powder (containing active ingredients and potency enhancer in part of the flame retardant) and the remaining mosquito coil base material mixed with water and kneaded, followed by an extruder After molding with a punching machine, it can be dried to produce a mosquito coil. Further, after molding using only the mosquito coil incense base material, a liquid agent containing an active ingredient or the like may be sprayed or applied thereto.
本発明の感染症媒介蚊防除用蚊取線香は、ネッタイイエカ、ネッタイシマカ、ハマダラカ類、ヒトスジシマカ、アカイエカ等の感染症媒介蚊類に特異的に卓効を示すが、もちろん、他種の蚊やハエ、ゴキブリ、屋内塵性ダニ類等の衛生害虫等の種々の害虫にも有効であり、その実用性は極めて高い。 The mosquito coil for controlling infection vector mosquitoes of the present invention is particularly effective for infection vector mosquitoes such as Aedes aegypti, Aedes aegypti, Anopheles, Aedes albopictus, Culex, etc. It is also effective against various pests such as cockroaches and sanitary pests such as indoor dust mites, and its practicality is extremely high.
次に、具体的実施例に基づいて本発明の感染症媒介蚊防除用蚊取線香を更に詳細に説明する。 Next, the mosquito coil for controlling infection vector mosquitoes according to the present invention will be described in more detail based on specific examples.
化合物Ａ（０．１部）及び効力増強剤Ａ（０．２部）を、除虫菊抽出粕粉、木粉、澱粉等の蚊取線香基材９９．７部に均一に混合後、色素と防腐剤を含む水を加え、公知の方法によって本発明の感染症媒介蚊防除用蚊取線香を得た。 Compound A (0.1 part) and potency enhancer A (0.2 part) were uniformly mixed with 99.7 parts of a mosquito coiled incense base such as pesticide extracted chrysanthemum powder, wood powder, starch, etc. The water containing the agent was added, and the mosquito coil for controlling infection vector mosquitoes of the present invention was obtained by a known method.
化合物Ａ（０．０５部）、効力増強剤Ａ（０．１５部）、ドデシルベンゼンスルホン酸イソプロピルアミン塩０．０８部、及び２,６−ジ−ターシャリーブチル−４−メチルフェノール０．１部を、ココナッツシェル粉末、木粉、タブ粉、澱粉等の蚊取線香基材９９．６２部に均一に混合後、防腐剤を含む水を加え、公知の方法によって本発明の感染症媒介蚊防除用蚊取線香を得た。 Compound A (0.05 parts), Efficacy Enhancer A (0.15 parts), 0.08 parts of dodecylbenzenesulfonic acid isopropylamine salt, and 2,6-ditertiarybutyl-4-methylphenol 0.1 The mosquito shell powder, wood powder, tab powder, starch, etc. are uniformly mixed with 99.62 parts of mosquito coil, and water containing an antiseptic is added, and the infection-borne mosquito of the present invention is added by a known method. A mosquito coil for control was obtained.
［蚊取線香を用いた基礎効力試験］
７０ｃｍ立方のガラスチャンバー内に、実施例１又は実施例２に準じて得られた本発明の感染症媒介蚊防除用蚊取線香の０．５ｇを点火したものを入れ、ネッタイイエカ雌成虫又はネッタイシマカ雌成虫２０匹を放った。２０分間暴露させ、時間経過に伴い落下仰転したネッタイイエカ雌成虫又はネッタイシマカ雌成虫を数え、ＫＴ90値を求めたところ表１のとおりであった。
[Basic efficacy test using mosquito coils]
Into a 70 cm cubic glass chamber, 0.5 g of a mosquito coil for controlling infection vector mosquitoes obtained in accordance with Example 1 or Example 2 according to the present invention was placed. 20 adults were released. Table 1 shows the KT 90 value obtained by counting adult female Aedes aegypti or Aedes aegypti that were exposed for 20 minutes and fallen over time.
・効力増強剤Ｂ：ドデシルベンゼンスルホン酸イソプロピルアミン塩
・共力剤Ｓ ：Ｎ−（２−エチルヘキシル）−１−イソプロピル−４−メチルビシクロ［２，２，２］−オクト−５−エン−２，３−ジカルボキシイミド
試験の結果、化合物Ａを０．０１質量％以上含有し、かつ、これに効力増強剤として効力増強剤Ａ｛Ｎ−（２−エチルヘキシル）−ビシクロ［２，２，１］−ヘプタ−５−エン−２，３−ジカルボキシイミド｝を配合した本発明の蚊取線香は、相乗効果によってノックダウン効果が増強し、特に、効力増強剤Ａの化合物Ａに対する配合量が２．０倍以上のものは、その増強効果が顕著であった。前記の点は、有効成分の量がともに０．０１質量％の本発明１と比較例２とを対比した場合、本発明１は、有効成分の３倍の効力増強剤Ａを配合することによって、ＫＴ90値が約１／２となり、ノックダウン効果として約２倍の増強効果を示したこと、また、本発明１と比較例３とを対比した場合、有効成分の量（質量％）において前者は後者の１／１０であるにも拘らず、本発明１において、比較例３と概略同等のＫＴ90値が得られたことによっても明らかである。従って、効力増強剤Ａのコストが化合物Ａに比べて非常に安価なことを考慮すると、本発明の蚊取線香は、極めて有用な感染症媒介蚊防除用蚊取線香であることが明らかである。
これに対し、効力増強剤Ａを併用しない化合物Ａの蚊取線香（比較例１〜３）は、ノックダウン効果が劣った。比較例４に示すように、共力剤Ｓ｛Ｎ−（２−エチルヘキシル）−１−イソプロピル−４−メチルビシクロ［２，２，２］−オクト−５−エン−２，３−ジカルボキシイミド｝は、効力増強剤Ａと化学構造が類似し、従来からピレスロイドの共力剤として汎用されているにもかかわらず、化合物Ａと組み合わせた本発明の蚊取線香形態では十分な効力増強効果を示さなかった。
また、ｄｌ，ｄ−Ｔ８０−アレスリンは、比較例５及び６に示すように、本発明で用いる効力増強剤Ａを加えることによってそのノックダウン効果は向上するものの本発明の蚊取線香には及ばず、メトフルトリン線香（比較例７）もノックダウン効果は十分でなかった。
As a result of the test, compound A was contained in an amount of 0.01% by mass or more, and efficacy enhancer A {N- (2-ethylhexyl) -bicyclo [2,2,1] -hepta-5- The mosquito coils of the present invention blended with ene-2,3-dicarboximide} have an enhanced knockdown effect due to a synergistic effect, and in particular, the blending amount of the efficacy enhancer A with respect to compound A is 2.0 times or more. As for thing, the enhancement effect was remarkable. The above point is that when the present invention 1 in which the amount of the active ingredient is both 0.01% by mass and the comparative example 2 are compared, the present invention 1 is obtained by blending the potentiating agent A three times the active ingredient. , The KT 90 value was about ½, showing about twice the enhancement effect as the knockdown effect, and when the present invention 1 and comparative example 3 were compared, the amount of active ingredient (mass%) Although the former is 1/10 of the latter, it is clear that the KT 90 value substantially equal to that of Comparative Example 3 was obtained in the present invention 1. Therefore, in view of the fact that the cost of the potency enhancer A is very low compared with the compound A, it is clear that the mosquito coil of the present invention is a very useful mosquito coil for controlling infection vector mosquitoes. .
On the other hand, the mosquito coiled incense of the compound A (Comparative Examples 1-3) which does not use the efficacy enhancer A in combination has a poor knockdown effect. As shown in Comparative Example 4, the synergist S {N- (2-ethylhexyl) -1-isopropyl-4-methylbicyclo [2,2,2] -oct-5-ene-2,3-dicarboximide } Has a chemical structure similar to that of potency enhancer A, and has a sufficient potency enhancing effect in the mosquito coil form of the present invention combined with compound A even though it has been widely used as a synergist for pyrethroids. Not shown.
In addition, as shown in Comparative Examples 5 and 6, dl, d-T80-alleslin is effective for the mosquito coil of the present invention although its knockdown effect is improved by adding the efficacy enhancer A used in the present invention. In addition, the metfurthrin incense stick (Comparative Example 7) also did not have a sufficient knockdown effect.
［２５ｍ3の部屋での実地効力試験］
前記実施例３の効力試験は、７０ｃｍ立方のガラスチャンバー（０．３４３ｍ3）で実施したので、実際に蚊取線香が使用される２５ｍ3の部屋と比べると空間容積は１／７３に過ぎない。そこで、蚊取線香の性能を実際使用条件に即して評価するために、２５ｍ3の部屋で実地効力試験を行った。
すなわち、閉めきった２５ｍ3の部屋にアカイエカ雌成虫１００匹を放った後、部屋の中央に点火した供試蚊取線香（実施例１又は実施例２に準じて調製）を置いた。２時間暴露させ、時間経過に伴い落下仰転したアカイエカ雌成虫を数え、ＫＴ50値、ＫＴ90値及び致死率を求めたところ表２のとおりであった。
[Practical test in 25m 3 room]
Since the efficacy test of Example 3 was conducted in a 70 cm cubic glass chamber (0.343 m 3 ), the space volume was only 1/73 compared to a 25 m 3 room where mosquito coils were actually used. . Therefore, in order to evaluate the performance of the mosquito coil in accordance with the actual use conditions, a field efficacy test was conducted in a 25 m 3 room.
That is, after releasing 100 adult female mosquitoes in a closed 25 m 3 room, a test mosquito coil (prepared according to Example 1 or Example 2) was placed in the center of the room. Table 2 shows the KT 50 value, the KT 90 value, and the mortality rate obtained by counting the female adult mosquitoes that had been exposed for 2 hours and fallen over time.
試験の結果、化合物Ａを０．０１質量％以上含有し、かつ、これに効力増強剤として効力増強剤Ａ｛Ｎ−（２−エチルヘキシル）−ビシクロ［２，２，１］−ヘプタ−５−エン−２，３−ジカルボキシイミド｝を化合物Ａに対して０．１倍量又は１．０倍量配合した本発明の蚊取線香（本発明３、４）は、ＫＴ50値の指標で示されるノックダウン効果の増強が認められた。また、効力増強剤Ａの化合物Ａに対する配合量が２．０〜５．０倍量のもの（本発明１、２、５、６）は、ＫＴ90値の指標で示されるノックダウン効果ならびに致死率の点でも効力増強が顕著で、より確実で安定した殺虫効力を奏しうることが認められた。従って、効力増強剤Ａのコストが化合物Ａに比べて非常に安価なことを考慮すると、本発明の蚊取線香は、極めて有用な感染症媒介蚊防除用蚊取線香であることが明らかである。
これに対し、効力増強剤Ａを併用しない化合物Ａの蚊取線香（比較例１〜３）は、ノックダウン効果、致死効果ともに劣った。
As a result of the test, compound A was contained in an amount of 0.01% by mass or more, and efficacy enhancer A {N- (2-ethylhexyl) -bicyclo [2,2,1] -hepta-5- The mosquito coils of the present invention (present inventions 3 and 4) containing 0.1-2 or 1.0-fold amount of ene-2,3-dicarboximide} with respect to compound A is an index of KT 50 value. The shown enhanced knockdown effect was observed. In addition, when the compounding amount of the potentiator A is 2.0 to 5.0 times that of Compound A (Invention 1, 2, 5, 6), the knockdown effect and lethality indicated by the KT 90 value index In terms of rate, the increase in efficacy was remarkable, and it was confirmed that a more reliable and stable insecticidal effect could be achieved. Therefore, in view of the fact that the cost of the potency enhancer A is very low compared with the compound A, it is clear that the mosquito coil of the present invention is a very useful mosquito coil for controlling infection vector mosquitoes. .
On the other hand, the mosquito coils of Comparative Compound A (Comparative Examples 1 to 3) not using the potency enhancer A were inferior in both the knockdown effect and the lethal effect.
［２５ｍ3の部屋での実地効力試験］
実施例４の試験を、ネッタイイエカ雌成虫についても実施した。その結果を表３に示す。
[Practical test in 25m 3 room]
The test of Example 4 was also conducted on adult female mosquitoes. The results are shown in Table 3.
試験の結果、本発明の感染症媒介蚊防除用蚊取線香においては、化合物Ａに対して効力増強剤Ａを２．０倍量配合することによって、ネッタイイエカに対するノックダウン効果はKT50値で約２倍増強した。KT90値でみると、比較例の線香ではKT90値を算出できなかったので、本発明線香の増強効果は２、３倍を大きく超え、また、致死率における増強効果も約３〜４倍に達した。従って、本発明の感染症媒介蚊防除用蚊取線香は、アカイエカと同様にネッタイイエカに対しても、KT50値だけでなく、KT90値や致死率の点でも高い効力増強効果を示し、本発明の有用性は明らかである。 As a result of the test, in the mosquito coil for controlling infection vector mosquitoes according to the present invention, the compound A has 2.0 times the potency enhancer A, so that the knockdown effect on the nettle squid is about KT 50 value. Increased 2 times. In terms of the KT 90 value, the incense stick of the comparative example could not calculate the KT 90 value, so the incense effect of the incense stick of the present invention greatly exceeded 2 to 3 times, and the enhancement effect in lethality was also about 3 to 4 times. Reached. Therefore, the mosquito coil for controlling infection vector mosquitoes of the present invention shows not only the KT 50 value, but also the KT 90 value and the lethality of the mosquito coil as well as the squid, The usefulness of the invention is clear.
本発明は、蚊取線香の製造販売分野において、須らく利用可能である。 The present invention can be used in the field of manufacturing and selling mosquito coils.
Claims (2)
で表される、４−メトキシメチル−２，３，５，６−テトラフルオロベンジル ２，２，３，３−テトラメチルシクロプロパンカルボキシレートを０．０１〜０．５質量％含有し、かつ、効力増強剤として、Ｎ−（２−エチルヘキシル）−ビシクロ［２，２，１］−ヘプタ−５−エン−２，３−ジカルボキシイミドを、有効成分量に対して０．１倍量以上配合してなることを特徴とする感染症媒介蚊防除用蚊取線香。 As an active ingredient, the following chemical formula
Containing 4-methoxymethyl-2,3,5,6-tetrafluorobenzyl 2,2,3,3-tetramethylcyclopropanecarboxylate represented by the formula: As an effect enhancer, N- (2-ethylhexyl) -bicyclo [2,2,1] -hept-5-ene-2,3-dicarboximide is added in an amount of 0.1 times or more with respect to the amount of active ingredient. A mosquito coil for controlling infection-borne mosquitoes, characterized by
Priority Applications (4)
| Application Number | Priority Date | Filing Date | Title |
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| JP2006304879A JP3926836B1 (en) | 2006-07-05 | 2006-11-10 | Mosquito coil for infectious disease control mosquito control |
| MYPI20070811 MY142829A (en) | 2006-07-05 | 2007-05-23 | Mosquito coil stick against infectious disease-carrying mosquitoes |
| CN2007101269227A CN101099470B (en) | 2006-07-05 | 2007-07-03 | Mosquito-driving joss stick for preventing infectious disease medium mosquito |
| HK08106773.2A HK1116625A1 (en) | 2006-07-05 | 2008-06-18 | Mosquito-driving joss stick for preventing infectous disease medium mosquito |
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| JP2006185048 | 2006-07-05 | ||
| JP2006304879A JP3926836B1 (en) | 2006-07-05 | 2006-11-10 | Mosquito coil for infectious disease control mosquito control |
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| JP3926836B1 JP3926836B1 (en) | 2007-06-06 |
| JP2008031140A true JP2008031140A (en) | 2008-02-14 |
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| JP (1) | JP3926836B1 (en) |
| HK (1) | HK1116625A1 (en) |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2010013360A (en) * | 2008-07-01 | 2010-01-21 | Dainippon Jochugiku Co Ltd | Medicine for incense stick for repelling mosquito or fly |
| JP2010100603A (en) * | 2008-09-25 | 2010-05-06 | Dainippon Jochugiku Co Ltd | Mosquito coil for controlling infectious disease-carrying mosquito |
| JP2010120903A (en) * | 2008-11-21 | 2010-06-03 | Dainippon Jochugiku Co Ltd | Mosquito repellent incense for controlling infection-mediating mosquito |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2009132668A (en) * | 2007-11-08 | 2009-06-18 | Dainippon Jochugiku Co Ltd | Effect-enhancing agent of incense stick for repelling mosquito or fly, and method for producing the same |
| CN101467528B (en) * | 2007-12-27 | 2014-06-04 | 大日本除虫菊株式会社 | Incense stick for expelling mosquito or fly |
-
2006
- 2006-11-10 JP JP2006304879A patent/JP3926836B1/en not_active Expired - Fee Related
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2007
- 2007-05-23 MY MYPI20070811 patent/MY142829A/en unknown
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2010013360A (en) * | 2008-07-01 | 2010-01-21 | Dainippon Jochugiku Co Ltd | Medicine for incense stick for repelling mosquito or fly |
| JP2010100603A (en) * | 2008-09-25 | 2010-05-06 | Dainippon Jochugiku Co Ltd | Mosquito coil for controlling infectious disease-carrying mosquito |
| JP2010120903A (en) * | 2008-11-21 | 2010-06-03 | Dainippon Jochugiku Co Ltd | Mosquito repellent incense for controlling infection-mediating mosquito |
Also Published As
| Publication number | Publication date |
|---|---|
| MY142829A (en) | 2011-01-14 |
| JP3926836B1 (en) | 2007-06-06 |
| HK1116625A1 (en) | 2009-01-02 |
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