JP2009126804A - Noxious insect repellent for human body - Google Patents
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Abstract
Description
本発明は、蚊、ブヨ、サシバエ、イエダニ、ナンキンムシ等の害虫から人体を守るための人体用害虫忌避剤に関する。 The present invention relates to an insect pest repellent for protecting a human body from insect pests such as mosquitoes, gnats, sand flies, house dust mites, bedbugs and the like.
害虫忌避剤について、従来より、使用感の改善、刺激性の軽減を目的とした様々な特許が出願されている。害虫忌避剤は基本的に腕、足、首筋等、人体の露出した肌、即ち、外的な刺激を受けやすい部分に塗布するものであり、近年では害虫忌避成分に皮膚を保護する目的で、化粧品原料に用いられている紫外線吸収剤や紫外線散乱剤を配合し、害虫忌避と日焼け防止を目的とした特許文献1(特開平5−92915号公報)及び特許文献2(特開平8−183720号公報)が、また、保湿効果が期待できる成分、例えばアロエエキスやモモエキスを配合し、ディートの異臭の軽減を目的とした特許文献3(特開2003−160413号公報)が出願されている。
更に、組成物中に水を配合した水性害虫忌避剤の特許も出願されている。例えば、害虫忌避成分、水溶性溶剤及び水を配合し、水溶性溶剤と水の配合比率を規定することにより、皮膚感触と臭気を改善した特許文献4(特開2003−192503号公報)や、忌避成分、アルコール又はグリコール、界面活性剤及び水を配合し、忌避成分の安定化と更に敏感な皮膚に対する乾燥及び刺激の軽減を目的とした特許文献5(特開平11−349409号公報)が挙げられる。
本発明者らは、更なる使用感の改善、ならびに刺激性の軽減を目指して検討を重ね、配合する水として天然ミネラル水を選択し、特許文献6(特開2005−132780号公報)において有用な人体用害虫忌避剤を開示した。一方、皮膚に塗布された忌避成分が日光等への曝露によって劣化するのを防止することも重要である。前記したように、通常の紫外線吸収剤や紫外線散乱剤の配合は、油性液剤には有効で相応の効果の得られることが知られている。しかしながら、マグネシウムイオンやカルシウムイオンを含む天然ミネラル水と併用されるような特殊な条件下では、そのまま適用できず検討の余地が残されていた。
Further, a patent for an aqueous pest repellent in which water is mixed in the composition has been filed. For example, a pest repellent component, a water-soluble solvent, and water are blended, and by defining the blending ratio of the water-soluble solvent and water, Patent Document 4 (Japanese Patent Laid-Open No. 2003-192503) that improves skin feel and odor, Patent Document 5 (Japanese Patent Application Laid-Open No. 11-349409) which contains a repellent component, alcohol or glycol, a surfactant and water and aims to stabilize the repellent component and reduce dryness and irritation to sensitive skin. It is done.
The present inventors have repeatedly studied for further improvement in usability and reduced irritation, and selected natural mineral water as water to be blended, which is useful in Patent Document 6 (Japanese Patent Laid-Open No. 2005-132780). A human pest repellent was disclosed. On the other hand, it is also important to prevent the repellent component applied to the skin from being deteriorated by exposure to sunlight or the like. As described above, it is known that the blending of ordinary ultraviolet absorbers and ultraviolet scattering agents is effective for oil-based liquids and can provide appropriate effects. However, under special conditions that are used in combination with natural mineral water containing magnesium ions and calcium ions, it cannot be applied as it is, leaving room for study.
本発明はかかる現状に鑑みなされたもので、使用感ならびに人体への刺激性が改善された天然ミネラル水配合の人体用害虫忌避剤において、忌避成分が日光等に曝されても劣化が防止され忌避効力の持続性を向上させ得る人体用害虫忌避剤を提供しようとするものである。 The present invention has been made in view of the current situation, and in a pest repellent for human body containing natural mineral water with improved usability and irritation to the human body, deterioration is prevented even if the repellent component is exposed to sunlight or the like. An object of the present invention is to provide a pest repellent for human body that can improve the persistence of the repellent effect.
上記課題を解決するため、本発明は、以下の構成を採用する。
(1)(a)害虫忌避成分、(b)C2〜C6のアルコール及び/又はグリコールから選ばれた1種又は2種以上、及び(c)硬度700以下の天然ミネラル水を含有する人体用害虫忌避剤において、更にp−メトキシ桂皮酸アルキル系紫外線吸収剤を配合してなる人体用害虫忌避剤。
(2)p−メトキシ桂皮酸アルキル系紫外線吸収剤が、p−メトキシ桂皮酸オクチルである(1)に記載の人体用害虫忌避剤。
(3)(a)害虫忌避成分が、ディート、3−(N−n−ブチル−N−アセチル)アミノプロピオン酸エチルエステル、1−メチルプロピル 2−(2−ヒドロキシエチル)−1−ピペリジンカルボキシラート、p−メンタン−3,8−ジオールから選ばれた1種又は2種である(1)又は(2)に記載の人体用害虫忌避剤。
(4)(c)硬度700以下の天然ミネラル水が、脱塩された海洋深層水である(1)ないし(3)のいずれかに記載の人体用害虫忌避剤。
In order to solve the above problems, the present invention employs the following configuration.
(1) (a) Pest repellent component, (b) One or more selected from C 2 to C 6 alcohols and / or glycols, and (c) Natural mineral water having a hardness of 700 or less A pest repellent for humans, which is obtained by further blending an alkyl p-methoxycinnamate ultraviolet absorber with a pest repellent for use.
(2) The pest repellent for human bodies according to (1), wherein the p-methoxyalkyl cinnamate ultraviolet absorber is octyl p-methoxycinnamate.
(3) (a) Pest repellent component is diet, 3- (Nn-butyl-N-acetyl) aminopropionic acid ethyl ester, 1-methylpropyl 2- (2-hydroxyethyl) -1-piperidinecarboxylate The pest repellent for human bodies according to (1) or (2), which is one or two selected from p-menthane-3,8-diol.
(4) (c) The human body pest repellent according to any one of (1) to (3), wherein the natural mineral water having a hardness of 700 or less is desalted deep sea water.
本発明の人体用害虫忌避剤は、使用感ならびに人体への刺激性が改善されるとともに、忌避成分が日光等に曝されても劣化が防止され、忌避効力の持続性に優れるので、その実用性は極めて高い。 The pest repellent for human body of the present invention has improved usability and irritation to the human body, and even when the repellent component is exposed to sunlight etc., the deterioration is prevented, and the repellent efficacy is excellent in sustainability. The nature is extremely high.
本発明で用いる(a)害虫忌避成分としては、害虫に対して忌避作用あるいは吸血阻害作用を有する合成あるいは天然の各種化合物が挙げられる。例えば、ディート、3−(N−n−ブチル−N−アセチル)アミノプロピオン酸エチルエステル[以降、IR3535と称す]、1−メチルプロピル
2−(2−ヒドロキシエチル)−1−ピペリジンカルボキシラート[以降、ピカリジンと称す]、p−メンタン−3,8−ジオール、ユーカリプトール、α―ピネン、ゲラニオール、シトロネラール、カンファー、リナロール、カランー3,4−ジオールなどを例示できる。更に天然物としては、桂皮、シトロネラ、レモングラス、クローバ、ベルガモット、月桂樹、ユーカリなどから採れる精油、抽出液などを例示でき、これらの1種または2種以上を選択して用いることができる。上記化合物及び天然物のなかでは、特に、ディート、IR3535、ピカリジン、及びp−メンタン−3,8−ジオールが好ましい。
害虫忌避成分は各薬剤の忌避効力等により異なるが、本発明の人体用害虫忌避剤全体量に対して1〜20質量%、好ましくは3〜10質量%配合される。
Examples of the pest repellent component (a) used in the present invention include various synthetic or natural compounds having a repellent action or blood sucking inhibitory action against pests. For example, diet, 3- (Nn-butyl-N-acetyl) aminopropionic acid ethyl ester [hereinafter referred to as IR3535], 1-methylpropyl 2- (2-hydroxyethyl) -1-piperidinecarboxylate [hereinafter referred to as IR3535] And p-menthane-3,8-diol, eucalyptol, α-pinene, geraniol, citronellal, camphor, linalool, caran-3,4-diol, and the like. Furthermore, examples of natural products include essential oils and extracts from cinnamon bark, citronella, lemongrass, clover, bergamot, laurel, eucalyptus, etc., and one or more of these can be selected and used. Of the above compounds and natural products, diet, IR3535, picaridin, and p-menthane-3,8-diol are particularly preferable.
The pest repellent component varies depending on the repellent efficacy and the like of each drug, but is 1 to 20% by mass, preferably 3 to 10% by mass based on the total amount of the pest repellent for human body of the present invention.
本発明で用いる(b)C2〜C6のアルコール及び/又はグリコールとしては、炭素数2〜3の低級一価アルコールであるエタノール、イソプロパノールや、グリコールであるエチレングリコール、ジエチレングリコール、プロピレングリコール、ジプロピレングリコール、1,3−ブチレングリコール等が挙げられ、これらを単独でまたは混合して使用することができる。C2〜C6のアルコール及び/又はグリコールは水に不溶の忌避成分を可溶化するために用いる。なお、エタノールを用いる場合、肌への作用が緩和で、かつ食品用として一般的な醸造エタノールが好ましい。 Examples of (b) C 2 -C 6 alcohol and / or glycol used in the present invention include ethanol, isopropanol, which are lower monohydric alcohols having 2 to 3 carbon atoms, and ethylene glycol, diethylene glycol, propylene glycol, dialkyl which are glycols. Examples thereof include propylene glycol and 1,3-butylene glycol, and these can be used alone or in combination. C 2 -C 6 alcohols and / or glycols are used to solubilize repellent components that are insoluble in water. In addition, when using ethanol, the effect | action on a skin is relieve | moderated and general brewed ethanol for foods is preferable.
本発明に用いる(c)天然ミネラル水としては、山麓の涌き水、地下深層水、海洋表層水、海洋深層水等が挙げられる。これらのミネラル水はマグネシウムイオン、カルシウムイオン、カリウムイオン等の金属イオンを含み、人体に不足しがちなミネラル成分を補給しやすいことから各方面で注目されている。例えば、逆浸透膜法等により濾過、脱塩処理を行い硬度を100〜1000程度に調整したものが飲料として販売されているが、本発明では硬度700以下のミネラル水が適合し、これらを皮膚に直接塗布することで、少量のミネラル成分による保湿感、さっぱり感が付与される。硬度が700を超えると、組成物の安定性に支障をきたすので好ましくない。
上記の天然ミネラル水のうち、特に海洋深層水はミネラル成分のバランスが良く、また水深200m以上の無光層より採取しているため、清浄性、安定性が良好で、製剤化した際、使用感、製剤安定性に優れる。本発明の更に好ましい組成物は硬度が5〜300に調整された海洋深層水を用いたものであり、一層良好な使用感を得ることができる。
Examples of (c) natural mineral water used in the present invention include foothill water, deep underground water, ocean surface water, ocean deep water, and the like. These mineral waters are attracting attention in various fields because they contain metal ions such as magnesium ions, calcium ions, and potassium ions, and are easy to replenish mineral components that tend to be deficient in the human body. For example, a beverage that is filtered and desalted by the reverse osmosis membrane method and adjusted to a hardness of about 100 to 1000 is sold as a beverage. In the present invention, mineral water having a hardness of 700 or less is suitable, and these are applied to the skin. Applying directly to the surface gives a moisturizing feeling and a refreshing feeling due to a small amount of mineral components. If the hardness exceeds 700, the stability of the composition will be hindered.
Among the above natural mineral waters, especially deep ocean water has a good balance of mineral components and is collected from a non-light layer with a depth of 200 m or more, so it has good cleanliness and stability and is used when formulated. Excellent feeling and formulation stability. A more preferred composition of the present invention uses deep ocean water whose hardness is adjusted to 5 to 300, and can provide a better feeling of use.
なお、本発明においては、(c)水に対する(b)アルコール及び/又はグリコールの重量比が1.1以下であることが好ましい。アルコールとして炭素数2〜3の低級一価アルコールを用いる場合、重量比が1.1を超えると塗布面にざらざらした感触が残り、一方、多価アルコールの場合、塗布面にべとつき感が残って使用感が悪くなる。 In the present invention, (c) the weight ratio of (b) alcohol and / or glycol to water is preferably 1.1 or less. When a lower monohydric alcohol having 2 to 3 carbon atoms is used as the alcohol, if the weight ratio exceeds 1.1, a rough feel remains on the coated surface, while in the case of a polyhydric alcohol, a sticky feeling remains on the coated surface. The feeling of use becomes worse.
本発明の人体用害虫忌避剤は、忌避成分が日光等に曝されても劣化が防止されるように、前記した組成物にp−メトキシ桂皮酸アルキル系紫外線吸収剤を配合したことに特徴を有する。
紫外線吸収剤としては、p−メトキシ桂皮酸アルキル系化合物の他、ベンゾフェノン系、フェニルベンズイミダゾール系化合物等種々のものがあり、エタノール等の有機溶剤の溶液中ではいずれも使用できることが知られている。
しかるに、本発明者らは、天然ミネラル水を含む製剤にこれらの紫外線吸収剤を適用したところ、p−メトキシ桂皮酸アルキル系化合物が特異的に有効で、他の紫外線吸収剤は不適であることを見出し、本発明を完成するに至ったものである。詳細なメカニズムは不明であるが、天然ミネラル水中のマグネシウムイオンやカルシウムイオン等が関与しているものと考えられる。なお、p−メトキシ桂皮酸アルキルの配合量は、人体用害虫忌避剤全体量に対して0.05〜1.0質量%程度が適当であり、p−メトキシ桂皮酸アルキルのなかでは、p−メトキシ桂皮酸オクチルが使いやすく、効果の点でも最も優れていることが認められた。
The pest repellent for human body according to the present invention is characterized in that a p-methoxycinnamic acid alkyl ultraviolet absorber is blended with the above composition so that deterioration is prevented even if the repellent component is exposed to sunlight or the like. Have.
There are various ultraviolet absorbers such as p-methoxycinnamic acid alkyl compounds, benzophenone compounds, phenylbenzimidazole compounds, etc., and it is known that any of them can be used in an organic solvent solution such as ethanol. .
However, when the present inventors applied these ultraviolet absorbers to a preparation containing natural mineral water, p-methoxycinnamate alkyl compounds are specifically effective, and other ultraviolet absorbers are unsuitable. And the present invention has been completed. Although the detailed mechanism is unknown, it is considered that magnesium ions and calcium ions in natural mineral water are involved. In addition, about 0.05 to 1.0 mass% is suitable for the compounding quantity of alkyl p-methoxycinnamate with respect to the total amount of pest repellents for human bodies. It was found that octyl methoxycinnamate was easy to use and was most effective.
本発明では、上記成分以外に内容液の安定性を確保するために界面活性剤を配合してもよい。界面活性剤としては、特にHLBが11〜16のノニオン系界面活性剤が好ましく、ポリオキシエチレン(10モル)オレイルエーテル{HLB=12.4}、ポリオキシエチレン(20モル)オレイルエーテル{HLB=15.1}、ポリオキシエチレン(9モル)ラウリルエーテル{HLB=13.6}、ポリオキシエチレン(10モル)セチルエーテル{HLB=12.9}、ポリオキシエチレン(15モル)ステアリルエーテル{HLB=14.2}、ポリオキシエチレン(15モル)イソステアリルエーテル{HLB=14.2}等のポリオキシエチレンアルキルエーテル類、ポリオキシエチレン(20モル)ソルビタンモノオレエート{HLB=15.7}、ポリオキシエチレン(10モル)ソルビタンモノラウレート{HLB=14.9}、ポリオキシエチレン(20モル)ソルビタンモノステアレート{HLB=15.7}等のポリオキシエチレンソルビタン脂肪酸エステル類、ポリオキシエチレン(14モル)モノオレエート{HLB=13.7}、ポリオキシエチレン(9モル)モノラウレート{HLB=13.3}、ポリオキシエチレン(14モル)ミリステート{HLB=14.6}等のポリオキシエチレンアルキルエステル類等が挙げられ、これらを単独でまたは混合して使用することができる。界面活性剤は肌への刺激性を考えると極力低減するのが好ましいが、HLBが11〜16のノニオン系界面活性剤は少量の配合で内容液の安定化に効果がある。また、使用感(塗布面のさらさら感等)の改善のため、無水ケイ酸、タルク、カオリン等の無機粉末及び変性デンプン、シルク繊維粉末等の有機粉末を配合することができる。更に、グリチルリチン酸ジカリウム、アラントイン、塩化アルキルトリメチルアンモニウム、酢酸トコフェロール、カンフル等の消炎剤等を内容液の安定性に影響のない範囲で配合することができる。 In the present invention, in addition to the above components, a surfactant may be blended in order to ensure the stability of the content liquid. As the surfactant, nonionic surfactants having HLB of 11 to 16 are particularly preferable, and polyoxyethylene (10 mol) oleyl ether {HLB = 12.4}, polyoxyethylene (20 mol) oleyl ether {HLB = 15.1}, polyoxyethylene (9 mol) lauryl ether {HLB = 13.6}, polyoxyethylene (10 mol) cetyl ether {HLB = 12.9}, polyoxyethylene (15 mol) stearyl ether {HLB = 14.2}, polyoxyethylene alkyl ethers such as polyoxyethylene (15 mol) isostearyl ether {HLB = 14.2}, polyoxyethylene (20 mol) sorbitan monooleate {HLB = 15.7} , Polyoxyethylene (10 mol) sorbitan monolaurate {HLB 14.9}, polyoxyethylene (20 mol) sorbitan monostearate {HLB = 15.7} and other polyoxyethylene sorbitan fatty acid esters, polyoxyethylene (14 mol) monooleate {HLB = 13.7}, poly Examples include polyoxyethylene alkyl esters such as oxyethylene (9 mol) monolaurate {HLB = 13.3} and polyoxyethylene (14 mol) myristate {HLB = 14.6}. Or it can be mixed and used. The surfactant is preferably reduced as much as possible considering the irritation to the skin, but the nonionic surfactant having an HLB of 11 to 16 is effective in stabilizing the content liquid with a small amount. Moreover, in order to improve the feeling of use (such as the dry feeling of the coated surface), inorganic powders such as silicic anhydride, talc and kaolin, and organic powders such as modified starch and silk fiber powder can be blended. Furthermore, flame retardants such as dipotassium glycyrrhizinate, allantoin, alkyltrimethylammonium chloride, tocopherol acetate, camphor, etc. can be blended within a range that does not affect the stability of the content liquid.
こうして調製された本発明の人体用害虫忌避剤の実用上の使用形態については特に制限はないが、具体的な使用例としては、非エアゾール型スプレー剤やロールオンタイプの容器に充填する形態、不織布等のシート基材に含浸させる形態などの他、液化石油ガス、ジメチルエーテル、圧縮ガス(窒素ガスや圧縮空気等)等を噴射剤に用いてエアゾール剤とすることももちろん可能であり、適用範囲は極めて広い。 Although there is no restriction | limiting in particular about the practical use form of the pest repellent for human bodies of this invention prepared in this way, As a concrete use example, the form filled with a non-aerosol type spray agent or a roll-on type container, a nonwoven fabric In addition to the form of impregnating the sheet base material such as liquefied petroleum gas, dimethyl ether, compressed gas (nitrogen gas, compressed air, etc.) etc. can also be used as a propellant to make an aerosol agent, and the applicable range is Extremely wide.
次に具体的な実施例ならびに試験例に基づき、本発明の人体用害虫忌避剤について更に詳細に説明する。 Next, the human body pest repellent of the present invention will be described in more detail based on specific examples and test examples.
害虫忌避成分としてディート5.0gと紫外線吸収剤としてp−メトキシ桂皮酸オクチル0.2gをエタノール44.8gに均一に溶解させた後、脱塩処理した硬度500の海洋深層水50.0g(水に対するアルコールの重量比0.9)を加え、本発明の人体用害虫忌避剤を得た。
この組成物は、5℃及び40℃の恒温槽に1ヶ月間保存しても均一澄明であった。次に、本害虫忌避剤を蓄圧式のポンプ容器に充填して使用した。手の甲に約1mL塗布し塗り延ばした後、1分経過後の塗布面の状態を観察したところ、べたつきはなく、さっぱりとした感触であった。また、塗布部は屋外で太陽光に曝される状況であったが、忌避効力は約10時間持続し、その間、蚊などの害虫に悩まされることはなかった。
After dissolving 5.0 g of diet as a pest repellent component and 0.2 g of octyl p-methoxycinnamate as a UV absorber in 44.8 g of ethanol, 50.0 g of water having a hardness of 500 seawater with a hardness of 500 (water The weight ratio of alcohol to 0.9) was added to obtain the human pest repellent of the present invention.
This composition was clear even when stored in a thermostatic bath at 5 ° C. and 40 ° C. for 1 month. Next, the pest repellent was filled into a pressure-accumulating pump container and used. After applying and spreading about 1 mL on the back of the hand, the state of the coated surface after 1 minute was observed, and there was no stickiness and it was a refreshing feel. Moreover, although the application part was exposed to sunlight outdoors, the repellent effect lasted for about 10 hours, and during that time, it was not bothered by pests such as mosquitoes.
実施例1に準じて表1に示す各種人体用害虫忌避剤を調製し、下記に示す試験を行った。
(1)使用感
手の甲に約1mL塗布し塗り延ばした後、1分経過後の塗布面に指先で触れ、感触を評価した。結果を〇(さっぱり感あり)、△、×(べたつく、肌がざらざらする)で示した。
(2)忌避効力試験
試験者の手の腕に約3mL塗布し、ヤブカが多数生息する屋外の試験地に佇み蚊が腕に止まるまでの時間を計った。試験は試験者を替えて4連行い、平均の効力持続時間を求めた。
According to Example 1, various human pest repellents shown in Table 1 were prepared, and the following tests were conducted.
(1) Feeling of use After about 1 mL was applied to the back of the hand and spread, the applied surface after 1 minute was touched with a fingertip to evaluate the feel. The results were indicated by ◯ (feeling refreshed), Δ, × (sticky, rough skin).
(2) Repelling efficacy test About 3 mL was applied to the arm of the examiner's hand, and it took time for the mosquito to stop on the arm in the outdoor test site where many aedes live. The test was repeated 4 times with different testers, and the average duration of efficacy was determined.
本発明の人体用害虫忌避剤は、手の甲に塗布し、使用感を確認したところ、ベタツキが無くさっぱりとした使用感で、害虫忌避効力の持続性も優れていることが認められた。なお、本発明1及び本発明4のように、p−メトキシ桂皮酸エステル系化合物のなかでは、p−メトキシ桂皮酸オクチルが好ましかった。
これに対し、比較例2及び比較例3のように、ミネラル水を含む製剤に、ベンゾフェノン系やフェニルベンズイミダゾール系紫外線吸収剤を配合しても、害虫忌避効力の持続性は改善されなかった。一方、ミネラル水を含まない人体用害虫忌避剤(比較例4及び比較例5)では、p−メトキシ桂皮酸エステル系化合物、ベンゾフェノン系化合物のいずれも害虫忌避効力の持続性を向上させたが、使用感は劣っていた。
The pest repellent for human body of the present invention was applied to the back of the hand and the feeling of use was confirmed. As a result, it was found that the pest repellent was excellent and the pest repellent efficacy was excellent. As in the present invention 1 and the present invention 4, octyl p-methoxycinnamate was preferred among the p-methoxycinnamic ester compounds.
On the other hand, as in Comparative Example 2 and Comparative Example 3, even when a benzophenone-based or phenylbenzimidazole-based ultraviolet absorber was added to a preparation containing mineral water, the sustainability of pest repellent efficacy was not improved. On the other hand, in the pest repellent for human body not containing mineral water (Comparative Example 4 and Comparative Example 5), both p-methoxycinnamic acid ester compound and benzophenone compound improved the sustainability of pest repellent efficacy. The feeling of use was inferior.
本発明の人体用害虫忌避剤は、人体用以外の害虫忌避分野に適用できる可能性がある。 The human body pest repellent of the present invention may be applicable to pest repellent fields other than those for human bodies.
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