JP2017001977A - Pharmaceutical composition, incense stick for insect pest control, and heat-transpiring preparation - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a novel and effective pharmaceutical composition for fundamentally reducing or moderating an odor or irritation caused by an insecticidal component, a perfume component, smoke, mist or the like, in using insect pest control products such as an incense stick for insect pest control and a heat-transpiring preparation, or aromatic products such as an incense stick for a Buddhist altar and a heat-transpiring aromatic agent.SOLUTION: A pharmaceutical composition includes a volatile chemical agent. The pharmaceutical composition further includes, as an irritation emollient for moderating irritation at use, an N-phenyl alkylamide derivative expressed by formula (I). (Ris hydrogen or an alkyl group, and Ris an alkyl group.)SELECTED DRAWING: None

Description

  The present invention relates to a pharmaceutical composition containing a volatile chemical, a pest control incense stick, and a preparation for heat evaporation.

  Examples of products using a pharmaceutical composition containing a volatile chemical include pest control incense (mosquito coils, etc.), heat transpiration preparations, Buddhist altar incense, and heat transpiration fragrance. These products are used by volatilizing the volatile chemical contained in the pharmaceutical composition into the space to be treated by soot or heat evaporation. For example, in a pest control product containing a pest control component as a volatile chemical, the pest control component volatilized in the space knocks down or kills the pest present in the space, and further eliminates or repels the pest from the space Acts as follows. In this kind of pest control product, for example, pyrethroid insecticidal components having volatility at room temperature such as empentrin, profluthrin, transfluthrin and the like are included as a volatile drug. Recently, fragrance products containing a fragrance agent such as a fragrance component as a volatile agent are also increasing. For example, a scented incense stick, a heated aroma diffuser, and the like are commercially available. In products containing such volatile chemicals, products with reduced odor and irritation caused by insecticidal components, perfume components, smoke and mist are required.

  Conventionally, as a pest control product with reduced irritation, there has been a mosquito coil that reduces the irritating odor of smoke generated during combustion (see, for example, Patent Document 1). The mosquito coil incense of Patent Document 1 is a blend of fragrance ingredients such as sandalwood extract, mandala extract, etc. When the mosquito coil is burned, the scent of sandalwood or mandala is released and an irritating odor generated simultaneously with combustion. It is intended to suppress.

JP-A-10-167903

  However, the mosquito coil incense of Patent Document 1 merely masks the irritating odor generated at the time of burning with a fragrance component such as sandalwood extract or mandala extract, and does not fundamentally reduce or reduce irritation. Moreover, the mosquito coil incense of patent document 1 is mainly aimed at reducing the irritating odor derived from the wood powder contained in the flame retardant, and reduces irritation caused by the insecticidal component which is a volatile chemical. Is not assumed.

  The present invention has been made in view of the above problems, and in using pest control products such as pest control incense, preparations for heat transpiration, and aromatic products such as Buddhist altar incense and heat transpiration fragrance, An object of the present invention is to provide a novel and useful pharmaceutical composition for fundamentally reducing or alleviating odors and irritation caused by perfume ingredients, smoke, mist and the like. Another object of the present invention is to provide a pest control incense stick and a heat transpiration preparation as a product using such a pharmaceutical composition.

The characteristic composition of the pharmaceutical composition according to the present invention for solving the above problems is as follows:
A pharmaceutical composition containing a volatile chemical,
The following formula (I) is used as a stimulant mitigating agent for reducing irritation during use.

（Ｒ_１：水素又はアルキル基，Ｒ_２：アルキル基）
で表されるＮ−フェニルアルキルアミド誘導体を含有することにある。

(R ₁ : hydrogen or alkyl group, R ₂ : alkyl group)
The N-phenylalkylamide derivative represented by these.

The inventors of the present invention describe odors and irritation caused by volatile chemicals (insecticidal components, fragrance components, etc.) contained in the pharmaceutical composition, and further smoke generated during smoke, mist generated during heat evaporation, etc. In order to reduce irritation and irritation, searching for effective substances, N-phenylalkylamide derivatives that have been used as antipyretic and analgesic ingredients in the past are superior to the odor and irritation of pharmaceutical compositions. It has been newly found that the reduction effect or relaxation effect can be exhibited. Therefore, based on this new knowledge, the present inventors have conceived that an N-phenylalkylamide derivative is used as a stimulant mitigating agent that relieves irritation during use of a pharmaceutical composition, and creates the present invention. It came to.
That is, according to the pharmaceutical composition of the present composition, the N-phenylalkylamide derivative represented by the above formula (I) is contained as an irritation mitigation agent, and therefore it is caused by smoke or mist generated during smoke. It is possible to effectively reduce or alleviate odors and irritation caused by insecticidal ingredients and perfume ingredients in addition to odors and irritation. Therefore, the pharmaceutical composition of the present invention is suitable as a raw material for low-irritant pest control products and fragrance products, and various products using the pharmaceutical composition of the present invention are safe even for infants and sensitive people. And it can be used comfortably.

In the pharmaceutical composition according to the present invention,
The stimulant mitigating agent has the following formula (II)

で表されるＮ−フェニルアセトアミド、又は、下記の式（ＩＩＩ）

N-phenylacetamide represented by the following formula (III)

で表されるＮ，２−ジメチル−Ｎ−フェニルブタンアミドであることが好ましい。

N, 2-dimethyl-N-phenylbutanamide represented by

  According to the pharmaceutical composition of this configuration, since the above-mentioned appropriate compound is contained as an irritation mitigating agent, when a pest control product or a fragrance product is configured using the pharmaceutical composition of the present invention, when smoked It is possible to more effectively reduce or alleviate odors and irritation caused by generated smoke, mist, and the like, as well as odors and irritation caused by insecticidal components and fragrance components.

In the pharmaceutical composition according to the present invention,
It is preferable to contain 0.0001-3 weight% of said irritation reducing agents.

  According to the pharmaceutical composition of this structure, since the irritation reducing agent is contained in the above-mentioned appropriate range, a necessary and sufficient irritation reducing effect or alleviating effect can be obtained.

In the pharmaceutical composition according to the present invention,
The low odor solvent preferably further contains at least one selected from the group consisting of benzyl benzoate, dipropylene glycol, hexylene glycol, triethyl citrate, and 3-methoxy-3-methylbutanol.

  According to the pharmaceutical composition of this configuration, since the appropriate low-odor solvent is contained, the effect of the stimulant mitigating agent is not impaired by the odor of the solvent, and the odor and irritation are surely reduced or alleviated. can do.

In the pharmaceutical composition according to the present invention,
It is preferable to contain 0.01 to 3 weight% of the said low odor solvent.

  According to the drug composition of this configuration, since the low odor solvent is contained in the above-mentioned appropriate range, the N-phenylalkylamide derivative can be uniformly dispersed in the product using the drug composition, In addition, a sufficient stimulus reduction effect or relaxation effect can be obtained.

In the pharmaceutical composition according to the present invention,
The volatile chemical is preferably a pest control component.

  According to the pharmaceutical composition of this configuration, since it contains a pest control component as a volatile chemical, it is particularly easy to feel the stimulus reducing effect or the mitigating effect of the stimulus mitigating agent, and it is suitable as a raw material for a hypoallergenic pest control product. .

The characteristic configuration of the pest control incense stick according to the present invention for solving the above problems is as follows:
The above pharmaceutical composition is used.

  According to the pest control incense stick of this configuration, because it is configured using the pharmaceutical composition of the present invention, it can effectively reduce or alleviate odors and irritation caused by smoke and insecticidal components generated during smoke Can do. Thus, the insect pest control incense of the present configuration can be used safely and comfortably as a low-irritant pest control product even for infants and persons sensitive to stimulation.

In the pest control incense stick according to the present invention,
As a flame retardant, it is preferable to contain at least one selected from the group consisting of wood powder, pesticide extracted chrysanthemum powder, citrus skin powder, tea powder, coconut shell powder, charcoal powder, bare ash, and talc.

  According to the pest control incense stick of this configuration, since it contains the appropriate flame retardant described above, it can be used in the same way as a normal mosquito coil, and the unique odor generated from the flame retardant is caused by the stimulus mitigation agent. It is reduced or alleviated and has high commercial value as a pest control incense with less odor and irritation.

In the pest control incense stick according to the present invention,
As the binder, it is preferable to contain at least one selected from the group consisting of tab powder, starch, methylcellulose, and carboxymethylcellulose.

  According to the pest control incense stick of this configuration, since it contains the appropriate binder described above, it can be used in the same way as a normal mosquito coil, and the effect of the stimulant mitigating agent is not hindered and reliably Odor and irritation can be reduced or alleviated.

The characteristic configuration of the preparation for heat transpiration according to the present invention for solving the above problems is
The above pharmaceutical composition is used.

  According to the preparation for heat transpiration of this configuration, since it is configured using the pharmaceutical composition of the present invention, it effectively reduces odors and irritation caused by mist, insecticidal components or fragrance components generated during heat transpiration, or Can be relaxed. As described above, the preparation for heat transpiration of this configuration can be used safely and comfortably as a hypoallergenic pest control product or a fragrance product, even for infants and persons sensitive to irritation.

  An embodiment using the pharmaceutical composition of the present invention will be described. However, the present invention is not intended to be limited to the following embodiments.

  In the present invention, an N-phenylalkylamide derivative that has been conventionally used as an antipyretic or analgesic exhibits an excellent reduction or mitigation effect against odors and stimuli generated from a pharmaceutical composition containing a volatile drug. The idea is to find out what can be done, and to use it as a stimulant mitigating agent for pest control products and fragrance products. Hereinafter, the characteristics of the pharmaceutical composition of the present invention will be described with reference to pest control incense, which is a typical pest control product, and a preparation for heat evaporation.

[Incense for pest control]
The pest control incense can be obtained by adding an appropriate amount of water to the pharmaceutical composition of the present invention and kneading it, forming it into a suitable shape such as a spiral or rod, and then drying it naturally or by heating. The pharmaceutical composition used for the pest control incense includes a low odor solvent, a volatile chemical, a flame retardant, a binder, and other components in addition to the stimulant mitigating agent. Of these, volatile chemicals are typically used as insecticides and perfume ingredients in pest control incense, but repellent ingredients such as diet, dimethyl phthalate, p-menthane-3,8-diol, hinokitiol, tetrahydro Antibacterial ingredients such as linalool, eugenol, citronellal, and allyl isothiocyanate, antifungal ingredients such as isopropylmethylphenol and orthophenylphenol, orange oil, lemon oil, lavender oil, peppermint oil, eucalyptus oil, citronella oil, lime oil, yuzu oil , Aromatic components such as jasmine oil, camellia oil, green tea essential oil, limonene, α-pinene, linalool, geraniol, phenylethyl alcohol, amylcinnamic aldehyde, cuminaldehyde, benzyl acetate, etc., and these components are also volatilized Included in sex drugs It is. In addition, green leaf alcohol (cis-3-hexenol) and green leaf aldehyde called “green fragrance” can be used as volatile agents. Hereinafter, the components constituting the pharmaceutical composition will be described.

<Insecticide ingredient>
A pyrethroid insecticidal component is preferably used as the insecticidal component which is a volatile chemical contained in the incense for controlling pests and is an active ingredient. Examples of pyrethroid insecticides include pyrethrin, allethrin, framethrin, praretrin, empentrin, teraleslin, transfluthrin, metfurthrin, profluthrin, 4-methoxymethyl-2,3,5,6-tetrafluorobenzyl 2,2,3 Examples include 3-tetramethylcyclopropanecarboxylate. When an optical isomer or a geometric isomer based on an asymmetric carbon or a double bond is present in the chemical structure of the pyrethroid insecticidal component, any isomer can be used. These pyrethroid insecticide components can be used alone or as a mixture of two or more.

  The content of the pyrethroid insecticidal component is 0.005 to 2% by weight, preferably 0.01 to 1.% by weight with respect to the weight of the whole pharmaceutical composition (in the case of this embodiment, the weight of the whole pest control incense stick). 5% by weight, more preferably 0.01 to 1% by weight. If the content of the pyrethroid insecticidal component is less than 0.005% by weight, a sufficient insecticidal effect may not be obtained. When the content of the pyrethroid insecticidal component exceeds 2% by weight, the pyrethroid insecticidal component is not a component that directly contributes to combustion, so that the extinction may occur.

<Perfume ingredients>
The pest control incense is usually given a fragrance appropriate to the incense, but recently, various fragrance components having volatility may be added for the purpose of obtaining an aroma effect and a relaxing effect. Also in the pharmaceutical composition of the present invention, various fragrance ingredients can be added as a volatile chemical. When the pharmaceutical composition is used as a pest control incense stick, it is preferable to use a heat diffusion fragrance as a fragrance component so that the scent spreads to every corner of the space when smoke is smoked. A heat-diffusion fragrance | flavor is a fragrance | flavor which has a property in which a fragrance | flavor component volatilizes efficiently extensively at the time of smoke, and a fragrance rises, and is a fragrance | flavor which has a boiling point at 250-400 degreeC. Examples of heated diffusion fragrances include galaxolide, musk ketone, hexyl cinnamic aldehyde, ethylene brushate, methyl atrate, hexyl salicylate, tricyclodecenyl acetate, oranger crystal, ambroxan, cachemelan, caron, heliotropin, dihydro Indenyl-2,4-dioxane, indole, methyl cedryl ketone, methyl β-naphthyl ketone, methyl dihydrojasmonate, rosephenone, coumarin, vanillin, stylus resinoid, 7-acetyl-1,2,3,4 , 5,6,7,8-octahydro-1,1,6,7-tetramethylnaphthalene, benzylbenzoate, benzyl salicylate, ionone, lilyaldehyde, isolongifolanone, acetoacetic acid-m-xylida Acetoacetate-o-toluidide, acetosyringone, acetyltriethyl citrate, benzophenone, benzyl caprylate, benzyl cinnamate, benzyl eugenol, benzyl laurate, benzyl methyl tiglate, benzyl phenyl ether, benzyl phenyl acetate, geranyl anthra Nileate, geranyl hexanoate, geranyl cyclopentanone, geranyl phenyl acetate, hexyl phenyl acetate, icosane, indane, cinnamyl butyrate, cinnamyl phenyl acetate, hexenyl benzoate, citral diethyl acetal, isoamyl benzoate, linalyl octanoate , 1-menthyl salicylate, citronellyl anthranilate, dimethylphenethylcarbinyl isobutylate , Diphenyl oxide, dodecyl butyrate, ethyl vanillate, ethyl vanillin, menthyl isovalerate, methoxyethyl phenyl glycidate, methyl 2,4-dihydroxy-3,6-dimethylbenzoate, nerolidyl acetate, neryl isovalerate, Octenyl cyclopentanone, octyl caprylate, phenethyl isoamyl ether, phenethyl octanoate, phenethyl phenyl acetate, ethyl vanillin acetate, ethyl vanillin propylene glycol acetal, ethyl hexyl palmitate, eugenyl benzoate, farnesol, farnesyl acetate, farnesyl methyl ether , Formaldehyde cyclododecylmethyl acetal, formylethyltetramethyltetralin, furfurylbenzene Zoeto, .gamma.-dodecalactone, phenethyl salicylate, phenoxyethyl propionate, phenyl benzoate, phenyl disulfide, Santa Lil butyrate, tetrahydro - pseudo - ionone, theobromine, valencene, and the like. In the case where an optical isomer or a geometric isomer based on an asymmetric carbon or a double bond exists in the chemical structure of the heat diffusion fragrance, any isomer can be used. These heat diffusion fragrance | flavors can be used individually or in mixture of 2 or more types.

  The content of the heated diffusion fragrance is 0.001 to 2% by weight, preferably 0.01 to 1% by weight, based on the weight of the whole pharmaceutical composition (in the case of the present embodiment, the weight of the whole pest controlling incense). More preferably, the content is 0.1 to 0.5% by weight. When the content of the heated diffusion fragrance is less than 0.001% by weight, there is a possibility that the fragrance cannot be produced sufficiently. If the content of the heated diffusion fragrance exceeds 2% by weight, the odor and irritation may become too strong and the effect of the stimulant mitigating agent may not be sufficiently achieved.

<Flame support agent and binder>
The flame retardant is blended in order to stably burn the pest control incense stick. The flame retardant also functions as a bulking agent for pest control incense sticks. The binder is blended as a binder that binds and hardens the raw materials. The flame retardant and the binder serve as a base material for pest control incense sticks. Examples of suitable flame retardants include wood powder, pesticide extracted chrysanthemum powder, citrus skin powder, tea powder, coconut shell powder, charcoal powder, bare ash, talc and the like. These flame retardants can be used alone or as a mixture of two or more. Examples of suitable binders include tab powder, starch (α starch, tapioca powder, etc.), methyl cellulose, carboxymethyl cellulose and the like. These binders can be used alone or as a mixture of two or more. The content of the flame retardant and the binder is usually 90% as the total content of the flame retardant and the binder with respect to the total weight of the pharmaceutical composition (in the case of this embodiment, the total weight of the pest control incense stick). % Or more.

<Irritation mitigation agent>
In order to relieve irritation at the time of use of the pest control incense (at the time of smoke or heat evaporation), the pharmaceutical composition of the present invention contains an N-phenylalkylamide derivative as an irritation mitigating agent. N-phenylalkylamide derivatives have the following formula (I)

で表される化合物である。ここで、Ｒ_１は水素又はアルキル基であり、アルキル基である場合は炭素数が１〜４の直鎖状又は分岐状のアルキル基が好ましい。Ｒ_２はアルキル基であり、炭素数が１〜８の直鎖状又は分岐状のアルキル基が好ましい。Ｒ_１がアルキル基である場合、Ｒ_１及びＲ_２は同一のアルキル基でもよく、異なるアルキル基でもよい。Ｎ−フェニルアルキルアミド誘導体は、芳香族環にアミド基が直接結合した化学構造を有しており、このような特定の化学構造が、害虫防除用線香の燻煙時に発生する煙や害虫防除用線香に含まれる殺虫成分に対して、本来の殺虫作用を阻害することなく拮抗作用を奏し、臭いや刺激のみを低減又は緩和しているものと推測される。

It is a compound represented by these. Here, R ₁ is hydrogen or an alkyl group, and when it is an alkyl group, a linear or branched alkyl group having 1 to 4 carbon atoms is preferable. R ₂ is an alkyl group, preferably a linear or branched alkyl group having 1 to 8 carbon atoms. When R ₁ is an alkyl group, R ₁ and R ₂ may be the same alkyl group or different alkyl groups. The N-phenylalkylamide derivative has a chemical structure in which an amide group is directly bonded to an aromatic ring, and such a specific chemical structure is used for controlling smoke and pests generated when a pest control incense is smoked. It is presumed that the insecticidal component contained in the incense stick has an antagonistic action without inhibiting the original insecticidal action, and reduces or alleviates only odor and irritation.

Among the N-phenylalkylamide derivatives, preferred compounds exhibiting particularly excellent reduction or mitigation effects against odor and irritation of pest control products are represented by formula (I) wherein R ₁ is hydrogen and R ₂ is methyl. The following formula (II)

で表されるＮ−フェニルアセトアミド（別名「アセトアニリド」）、又は、式（Ｉ）において、Ｒ_１がメチル基であり、Ｒ_２がブチル基である下記の式（ＩＩＩ）

Or N-phenylacetamide (also known as “acetanilide”) represented by the following formula (III): wherein R ₁ is a methyl group and R ₂ is a butyl group

で表されるＮ，２−ジメチル−Ｎ−フェニルブタンアミド（別名「ＧＡＲＤＡＭＩＤＥ」）である。

N, 2-dimethyl-N-phenylbutanamide (also known as “GARDAMIDE”).

  The details will be described in the following examples, but N-phenylacetamide or N, 2-dimethyl-N-phenylbutanamide is contained in a pharmaceutical composition in a predetermined formulation, and this pharmaceutical composition is used for controlling pests. When the incense was constituted, an effect of effectively reducing or mitigating odor and irritation caused by smoke generated when the incense for controlling insect pests was smoked and insecticidal components contained in the incense for controlling insects was recognized. In addition, the irritation reducing agent also functions as a dispersing agent or a holding agent for the volatile drug in the drug composition.

  The content of the N-phenylalkylamide derivative is 0.0001 to 3% by weight, preferably 0.001 to 1% by weight, more preferably 0.01 to 0.5% by weight, based on the weight of the whole pharmaceutical composition. %. The above content is necessary and sufficient for odors and irritation caused by smoke generated when smoke of pest control incense is smoked, and for odors and irritation caused by insecticidal components contained in pest control incense. Reduction effect or relaxation effect can be obtained. When the content of the N-phenylalkylamide derivative is less than 0.0001% by weight, the effect as an irritation reducing agent may not be sufficiently exerted. When the content of the N-phenylalkylamide derivative exceeds 3% by weight, the effect as an irritation reducing agent is naturally obtained, but the odor and irritation are sufficiently relieved, and the meaning of adding more irritation additives is diminished, There are no economic benefits.

<Low odor solvent>
In preparing the pharmaceutical composition of the present invention, it is preferable to use a low odor solvent. A low odor solvent is a solvent that does not contain substances with irritating odors (benzene, toluene, xylene, ethylbenzene, etc.). Since the low odor solvent is originally a substance with little irritation, the effect of the volatilizing drug does not decrease even if the drug composition contains a low odor solvent, and further, as a dispersant or retention agent for the stimulant mitigation agent. Less effective. Examples of suitable low odor solvents include benzyl benzoate, dipropylene glycol, hexylene glycol, triethyl citrate, 3-methoxy-3-methylbutanol and the like. These low odor solvents can be used alone or as a mixture of two or more.

  The content of the low odor solvent is 0.01 to 3% by weight, preferably 0.05 to 1% by weight with respect to the weight of the whole pharmaceutical composition (in the case of this embodiment, the weight of the whole pest controlling incense stick). %, More preferably 0.1 to 0.5% by weight. If it is said content, an N-phenylalkylamide derivative can be disperse | distributed uniformly in an incense for insect pest control, and also a sufficient irritation | stimulation reduction effect or relaxation effect can be acquired. When the content of the low odor solvent is less than 0.01% by weight, the dispersion of the N-phenylalkylamide derivative in the pharmaceutical composition may be insufficient. When the content of the low odor solvent exceeds 3% by weight, the effect as an irritation mitigating agent can be obtained. However, the flammability of the pest control incense is increased and smoke is excessively generated. It may not be enough.

<Other ingredients>
The pharmaceutical composition of the present invention may contain an antifungal agent, preservative, stabilizer, efficacy enhancer, deodorant and the like as other components. Examples of antifungal agents or preservatives include dehydroacetate, sorbate, p-hydroxybenzoate and the like. Illustrative stabilizers are 2,6-di-tertiarybutyl-4-methylphenol (BHT), 2,2′-methylenebis (4-methyl-6-tertiarybutylphenol), 2,2′-methylenebis (4 -Ethyl-6-tertiarybutylphenol), 4,4'-butylidenebis (3-methyl-6-tertiarybutylphenol), 4,4'-thiobis (3-methyl-6-tertiarybutylphenol), 2-tertiary Butyl-6- (3-tertiarybutyl-2-hydroxy-5-methylbenzyl) -4-methylphenyl acrylate, 2,4-ditertiarybutylphenyl 3,5-ditertiarybutyl-4-hydroxy Examples include benzoate. Examples of efficacy enhancers include piperonyl butoxide, N- (2-ethylhexyl) -bicyclo [2,2,1] hept-5-ene-2,3-dicarboximide, and the like. In addition, when the pharmaceutical composition of the present invention is used as a pest control incense, it contains a colorant such as malachite green, food additive (food blue 1, food yellow 4, food red 106, etc.). Is also possible.

[Formulation for heat evaporation]
The preparation for heat evaporation is prepared by using the pharmaceutical composition of the present invention as it is or by appropriately diluting the pharmaceutical composition of the present invention with water or a solvent. The preparation for heat evaporation is used as a liquid mosquito repellent chemical or a mosquito repellent mat impregnated in a fiber mat such as pulp or linter.

The pharmaceutical composition used in the preparation for heat evaporation includes a low odor solvent, a volatile chemical, a surfactant, a dispersant, and other components in addition to the stimulant mitigating agent. About an irritation | stimulation relaxation agent, a low odor solvent, a volatile chemical | medical agent, and another component, the component similar to what is used for an insect pest control incense can be used. In addition, in the preparation for heat evaporation, when a pyrethroid insecticide is used as the volatile agent, a pyrethroid insecticide having a vapor pressure of 2 × 10 ⁻⁴ to 1 × 10 ⁻² mmHg at 30 ° C. is preferable. Examples of such pyrethroid insecticidal components include metofluthrin, profluthrin, empentrin, transfluthrin, terrareslin, flamethrin, and the like.

  Surfactants or dispersants include ethers such as polyoxyethylene alkyl ethers, polyoxyethylene alkyl phenyl ethers, polyoxyethylene polyoxypropylene alkyl ethers, polyoxyethylene alkylamino ethers, polyethylene glycol fatty acid esters , Fatty acid esters such as polyoxyethylene sorbitan fatty acid esters and polyoxyethylene glycerin fatty acid esters, polyoxyethylene styrenated phenols, polyalkalolamides of fatty acids and the like can be used.

  Using the pharmaceutical composition of the present invention as a raw material, a pest control incense stick and a preparation for heat transpiration were prepared, and their performance was evaluated.

[Incense for pest control]
According to the composition shown in Table 1 below, pest control incense sticks according to Examples 1 to 7 and Comparative Examples 1 to 5 were prepared.

<Example 1>
N-phenylacetamide (0.01 parts by weight) as a stimulant mitigating agent, hexylene glycol (0.5 parts by weight) as a low odor solvent, dl · d-T80-aresulin (0.3 parts by weight) as a volatile agent , Pesticide chrysanthemum extract powder (45 parts by weight) and citrus skin powder (34 parts by weight) as flame retardant, and tab powder (4.2 parts by weight) and starch [α starch] (remainder) as binder Mixed powder (100 parts by weight) was prepared, and water (100 parts by weight) was added thereto and kneaded sufficiently. The kneaded product is formed into a sheet by using an extruder, punched into a spiral mold with a punching machine, and then dried and sealed until the water content becomes 7 to 10% by weight. An incense stick was prepared.

<Example 2>
N, 2-dimethyl-N-phenylbutanamide (3 parts by weight) as a stimulant mitigating agent, dipropylene glycol (3 parts by weight) as a low odor solvent, dl · d-T80-aresulin (0.3 Parts by weight), coconut shell powder (50 parts by weight) and wood flour [Toga] (27 parts by weight) as flame retardant, and starch [tapioca powder] (15 parts by weight) and carboxymethylcellulose (remainder) as binders Thus, mixed powder (100 parts by weight) was prepared, and water (100 parts by weight) was added thereto and kneaded sufficiently. And the pest control incense stick of Example 2 was produced by the same procedure as Example 1.

<Example 3>
N-phenylacetamide (0.1 part by weight) as a stimulant mitigating agent, benzyl benzoate (0.01 part by weight) and dipropylene glycol (0.5 part by weight) as a low odor solvent, and metfurthrin (0 0.01 parts by weight), pesticide extracted chrysanthemum powder (31 parts by weight) as a flame retardant, tea powder (45 parts by weight) and talc (4.8 parts by weight), and tab powder (2.6 parts by weight) as a binder And starch [α starch] (remainder) were mixed to prepare a mixed powder (100 parts by weight), and water (100 parts by weight) was added thereto and kneaded sufficiently. And the pest control incense stick of Example 3 was produced in the same procedure as Example 1.

<Example 4>
N-phenylacetamide (3 parts by weight) as a stimulant mitigating agent, triethyl citrate (0.05 parts by weight) and 3-methoxy-3-methylbutanol (0.6 parts by weight) as low odor solvents, as a volatile agent Transfluthrin (0.15 parts by weight), wood powder [fir] (49.2 parts by weight) and tea powder (29 parts by weight) as flame retardants, and starch [α-starch] (13 parts by weight) as a binder And methylcellulose (remainder) were mixed to prepare a mixed powder (100 parts by weight), and water (100 parts by weight) was added thereto and kneaded sufficiently. And the pest control incense stick of Example 4 was produced in the same procedure as Example 1.

<Example 5>
N-phenylacetamide (0.01 parts by weight) as a stimulant mitigating agent, d · d-T80-praretrin (0.15 parts by weight) as a volatile agent, charcoal (25 parts by weight) as a flame retardant, pesticide chrysanthemum extract powder ( 51 parts by weight) and talc (1.8 parts by weight), and tab powder (18 parts by weight) and carboxymethylcellulose (remainder) as a binder are mixed to prepare a mixed powder (100 parts by weight). (100 parts by weight) was added and kneaded thoroughly. And the pest control incense stick of Example 5 was produced in the same procedure as Example 1. The pest control incense stick of Example 5 does not contain a low odor solvent.

<Example 6>
N, 2-dimethyl-N-phenylbutanamide (0.01 parts by weight) as a stimulant mitigating agent, toluene (1 part by weight) as a solvent, galaxolide, cis-3-hexenol and minor components (total of 0. 5 parts by weight), citrus skin powder (38 parts by weight) as a flame retardant, tea powder (4.5 parts by weight) and coconut shell powder (39 parts by weight), and tab powder (8 parts by weight) and starch as binders [Α starch] (remainder) was mixed to prepare a mixed powder (100 parts by weight), and water (100 parts by weight) was added thereto and kneaded sufficiently. And the insect pest control incense of Example 6 was produced by the same procedure as Example 1. The pest control incense of Example 6 does not contain a low odor solvent and contains a normal solvent. In addition, the trace component of a volatile chemical | medical agent contains the insecticidal component, the fragrance | flavor component, etc. which are described in this specification.

<Example 7>
N, 2-dimethyl-N-phenylbutanamide (0.04 parts by weight) as a stimulant mitigating agent, hinokitiol, peppermint oil and trace components (total 2 parts by weight) as a volatile agent, and wood powder [Sugi] ( 49 parts by weight) and wood flour [pine] (30 parts by weight), and starch [α starch] (12 parts by weight) and methylcellulose (remainder) as a binder are mixed to prepare a mixed powder (100 parts by weight). Then, water (100 parts by weight) was added thereto and kneaded sufficiently. And the pest control incense stick of Example 7 was produced according to the procedure similar to Example 1. The pest control incense of Example 7 did not contain a low odor solvent. In addition, the trace component of a volatile chemical | medical agent contains the insecticidal component, the fragrance | flavor component, etc. which are described in this specification.

<Comparative Example 1>
Hexylene glycol (0.5 parts by weight) as a low odor solvent, dl · d-T80-aresulin (0.3 parts by weight) as a volatile chemical, insecticide chrysanthemum extract powder (45 parts by weight) and citrus epidermis as a flame retardant Powder (34 parts by weight) and tab powder (4.2 parts by weight) and starch [α starch] (remainder) as a binder are mixed to prepare a mixed powder (100 parts by weight). Parts by weight) was added and kneaded thoroughly. And the pest control incense stick of comparative example 1 was produced by the same procedure as Example 1. The insect pest controlling incense of Comparative Example 1 is obtained by excluding the stimulus relaxation agent in the blending of the insect controlling insect pest of Example 1.

<Comparative example 2>
Dimethylacetamide (0.01 parts by weight) which is a substance different from the stimulant mitigating agent, hexylene glycol (0.5 parts by weight) as a low odor solvent, dl · d-T80-aresulin (0.3 Parts by weight), pesticide extracted chrysanthemum extract powder (45 parts by weight) and citrus skin powder (34 parts by weight) as a flame retardant, and tab powder (4.2 parts by weight) and starch [α starch] (remainder) as binders Mixing was performed to prepare a mixed powder (100 parts by weight), and water (100 parts by weight) was added thereto and kneaded sufficiently. And the pest control incense stick of the comparative example 2 was produced by the procedure similar to Example 1. FIG. The insect pest controlling incense of Comparative Example 2 is obtained by adding dimethylacetamide in place of the stimulus mitigating agent in the formulation of the insect controlling insect pest of Example 1.

<Comparative Example 3>
Styrene (0.01 parts by weight) which is a substance different from the stimulant mitigating agent, hexylene glycol (0.5 parts by weight) as a low odor solvent, dl · d-T80-areslin (0.3 parts by weight) as a volatile agent Part), pesticide extracted chrysanthemum extract powder (45 parts by weight) and citrus skin powder (34 parts by weight) as a flame retardant, and tab powder (4.2 parts by weight) and starch [α starch] (remainder) as binder. Thus, mixed powder (100 parts by weight) was prepared, and water (100 parts by weight) was added thereto and kneaded sufficiently. And the pest control incense stick of the comparative example 3 was produced by the same procedure as Example 1. The pest control incense stick of Comparative Example 3 is a mixture of the pest control incense stick of Example 1 and styrene added in place of the stimulus relaxation agent.

<Comparative example 4>
D · d-T80-praretrin (0.15 parts by weight) as a volatile agent, charcoal (25 parts by weight), pesticide chrysanthemum extract powder (51 parts by weight) and talc (1.8 parts by weight), and viscosity As a binder, tab powder (18 parts by weight) and carboxymethylcellulose (remainder) were mixed to prepare a mixed powder (100 parts by weight), and water (100 parts by weight) was added thereto and kneaded sufficiently. And the pest control incense stick of the comparative example 4 was produced by the same procedure as Example 1. The pest control incense stick of Comparative Example 4 is obtained by excluding the stimulus relaxation agent in the blending of the pest control incense stick of Example 5.

<Comparative Example 5>
Hinokithiol, peppermint oil and trace components (2 parts by weight in total) as volatilizing agents, wood flour [Sugi] (49 parts by weight) and wood flour [pine] (30 parts by weight) as flame retardants, and starch as a binder [ [alpha] starch] (12 parts by weight) and methylcellulose (remainder) were mixed to prepare a mixed powder (100 parts by weight), and water (100 parts by weight) was added thereto and kneaded sufficiently. And the insect pest control incense of the comparative example 5 was produced in the same procedure as Example 1. The pest control incense stick of Comparative Example 5 is the same as the pest control incense stick of Example 7 except that the stimulus relaxation agent is excluded. In addition, the trace component of a volatile chemical | medical agent contains the insecticidal component, the fragrance | flavor component, etc. which are described in this specification.

  About the pest control incense stick of Example 1, when opening the package of the pest control incense stick for use at bedtime, the so-called “scent of comfort”, which is a unique scent of the incense stick, was emitted, and no irritating odor or odor was felt . When this pest control incense was installed in a 6 tatami-sized living room and ignited, the “pleasure scent” was continuously emitted from the pest control incense and no irritating odor or odor was generated until the end. . As a result, it was possible to bring a sense of relaxation to the sleeping user. As described above, the pest control incense stick of the present invention can suppress irritation and give a relaxing effect, but in order to confirm the performance of the pest control incense stick in more detail, the sensory test described below and EEG measurements were performed.

<Sensory test>
The pest control incense sticks of Examples 1 to 7 and Comparative Examples 1 to 5 were respectively introduced into glass cylinders (diameter 20 cm, height 40 cm), ignited and burned. Then, the scent emanating from the incense was evaluated by 10 panelists. The evaluation items were “stimulation relaxation” and “scent preference”, the highest point was 10 points, the lowest point was 1 point, and the average score of 10 panelists was obtained for each incense stick.

<Electroencephalogram measurement>
The pest control incense sticks of Examples 1 to 7 and Comparative Examples 1 to 5 were installed in a 6 tatami room where the subject was present, ignited and burned. Place the subject in the center of the room, wear an electroencephalograph, fast alpha wave, mid alpha wave (concentrated in a relaxed state), slow alpha wave, beta wave (tension, anxiety, irritated State), and θ wave. And these measurements were implemented with respect to five test subjects. For each brain wave, calculate the change in occupancy from the blank (normal state without incense sticks), and calculate “mid α wave change rate / β wave change rate” from here, The average value was obtained. It can be estimated that the greater the “change rate of mid α wave / change rate of β wave”, the greater the relaxed feeling of the subject.

  Table 2 above shows the results of the sensory test and the electroencephalogram measurement. The pest control incense sticks of the present invention (Examples 1 to 7) containing a stimulant mitigating agent have a great stimulus mitigating property regardless of the type of volatilizing agent contained, and the panelist feels an irritating odor or odor. There was no. Regarding the preference of scents, in general, the scent is largely dependent on individual preference, but the scent of the pest control incense sticks of the present invention (Examples 1 to 7) tends to be preferred by most people and is versatile. It could be a high product. Further, from the results of electroencephalogram measurement, the pest control incense sticks of the present invention (Examples 1 to 7) have a large “mid α wave change rate / β wave change rate” (ie, “consciousness in a relaxed state”). ”Concentrated” became larger than “stress, anxiety, irritated state”). From this result, it was suggested that when using the pest control incense stick of the present invention, a person can spend comfortably while relaxing without particularly feeling uncomfortable.

  On the other hand, the pest control incense stick of Comparative Example 1 in which no stimulant mitigating agent was blended resulted in a relatively good result for the scent preference for some people, but the irritation mitigation was small, It was difficult for a person sensitive to stimulation to use for a long time. A pest control incense in Comparative Example 2 containing an “amide compound not having an aromatic ring” (dimethylacetamide) different from an N-phenylalkylamide derivative that is an irritation mitigating agent, and N-phenyl that is an irritation mitigating agent The pest control incense stick of Comparative Example 3 blended with an “aromatic compound having no amide group” (styrene), which is different from the alkylamide derivative, has a relatively good result for the scent preference for some people. However, almost no irritation was observed. The pest control incense stick of Comparative Example 4 that does not contain an irritation mitigating agent and a low odor solvent gave a relatively good scent preference for some people, but the irritation mitigation was small. It was difficult to use for a long time for those who are sensitive to stimulation. Furthermore, the pest control incense of Comparative Example 5 that does not contain a stimulant mitigating agent and a low odor solvent has a strong bad odor and stimulating odor derived from wood flour, and the result is that the irritation mitigating property and taste preference of the scent are extremely poor. became. Regarding the electroencephalogram measurement, the pest control incense sticks of Comparative Examples 1 to 5 tend to decrease the “mid α wave change rate / β wave change rate” of the subject, and a person spends a long time relaxing. It was difficult.

[Formulation for heat evaporation]
According to the composition shown in Table 3 below, preparations for heat transpiration according to Examples 8 to 12 and Comparative Example 6 were prepared.

<Example 8>
Mixing N-phenylacetamide (0.001 parts by weight) as a stimulant mitigating agent, metfurthrin (0.4 parts by weight) as a volatilizing agent, and No. 1 kerosene and liquid paraffin (remainder) as solvents, totaling 100 parts by weight This was used as the preparation for heat transpiration of Example 8.

<Example 9>
Mixing N-phenylacetamide (0.1 parts by weight) as a stimulant mitigating agent, metfurthrin (0.4 parts by weight) as a volatilizing agent, and No. 1 kerosene and liquid paraffin (remainder) as a solvent, totaling 100 parts by weight This was used as the preparation for heat transpiration of Example 9.

<Example 10>
Mixing N, 2-dimethyl-N-phenylbutanamide (0.01 parts by weight) as a stimulant mitigating agent, metfurflurin (0.4 parts by weight) as a volatile agent, and No. 1 kerosene and liquid paraffin (remainder) as a solvent Then, the whole was prepared to be 100 parts by weight, and this was used as the preparation for heat transpiration of Example 10.

<Example 11>
Mix N, 2-dimethyl-N-phenylbutanamide (3 parts by weight) as a stimulant mitigating agent, metfurflurin (1.2 parts by weight) as a volatile agent, and No. 1 kerosene and liquid paraffin (remainder) as a solvent. The whole was prepared to be 100 parts by weight, and this was used as the preparation for heat transpiration of Example 11.

<Example 12>
N-phenylacetamide (0.1 parts by weight) as a stimulant mitigating agent, metfurflurin (0.5 parts by weight) as a volatile agent, and 2,6-ditertiarybutyl-4-methylphenol (BHT) as a solvent, Water and a glycol solvent (remainder) were mixed to prepare 100 parts by weight as a whole, and this was used as the preparation for heating and transpiration of Example 12.

<Comparative Example 6>
Metofluthrin (0.4 parts by weight) as a volatile agent and No. 1 kerosene and liquid paraffin (remainder) as a solvent are mixed to prepare a total of 100 parts by weight. It was set as the formulation. The preparation for heat transpiration of Comparative Example 6 is obtained by excluding the irritation reducing agent in the formulation of the preparation for heat transpiration of Example 8, 9 or 10.

  A sensory test was conducted on the preparations for heat evaporation of Examples 8 to 12 and Comparative Example 6. The method and evaluation of the sensory test were based on the sensory test on the insect pest controlling incense in Examples 1 to 7 and Comparative Examples 1 to 5 described above. The results of the sensory test are also shown in Table 3 showing the formulation of the heat transpiration preparation.

  The preparations for heat transpiration of the present invention (Examples 8 to 12) containing an irritation mitigating agent had large irritation mitigating properties, and the panelists did not feel an irritating odor or odor due to a solvent or a drug. On the other hand, the preparation for heat transpiration of Comparative Example 6 in which no irritation reducing agent was blended had low irritation mitigation properties, and it was difficult for humans to spend a long time while relaxing.

  The pharmaceutical composition of the present invention can be used in pest control products that control flying insects such as mosquitoes such as mosquitoes, chikaeka, and mosquitoes, moths, chironomids, flies, flies, butterflies, moths, and bees. However, it can also be used for controlling insect pests such as cockroaches and centipedes. In addition, the pest control incense using the pharmaceutical composition of the present invention, and the preparation for heat transpiration are pest control agents for use in stores, offices, factories, etc., as well as pest control agents used in general residences. Furthermore, it can be used as a pest control agent for animals such as pets and livestock.

Claims (10)

A pharmaceutical composition containing a volatile chemical,
The following formula (I) is used as a stimulant mitigating agent for reducing irritation during use.

(R ₁ : hydrogen or alkyl group, R ₂ : alkyl group)
The pharmaceutical composition containing N-phenylalkylamide derivative represented by these. The stimulant mitigating agent has the following formula (II)

N-phenylacetamide represented by the following formula (III)

The pharmaceutical composition according to claim 1, which is N, 2-dimethyl-N-phenylbutanamide represented by the formula:   The pharmaceutical composition according to claim 1 or 2, comprising 0.0001 to 3% by weight of the stimulant mitigating agent.   The low odor solvent further contains at least one selected from the group consisting of benzyl benzoate, dipropylene glycol, hexylene glycol, triethyl citrate, and 3-methoxy-3-methylbutanol. The pharmaceutical composition according to any one of the above.   The pharmaceutical composition according to claim 4, comprising 0.01 to 3% by weight of the low odor solvent.   The said volatile chemical | medical agent is a pest control component, The pharmaceutical composition as described in any one of Claims 1-5.   A pest control incense using the pharmaceutical composition according to claim 6.   The insect pest according to claim 7, comprising at least one selected from the group consisting of wood powder, pesticide extracted chrysanthemum powder, citrus skin powder, tea powder, coconut shell powder, charcoal powder, bare ash, and talc. Incense stick for control.   The pest control incense according to claim 7 or 8, comprising at least one selected from the group consisting of tab powder, starch, methylcellulose, and carboxymethylcellulose as a binder.   A preparation for heat evaporation using the pharmaceutical composition according to claim 6.