JP2003171204A - Gel-type insect repellent preparation - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a gel-like insect repellent preparation having good adhesion after application, low absorption from skin, and no white residue after application. SOLUTION: Insect repellent, 10 to 3 with respect to the total amount of the preparation
A gel-like insect repellent preparation is obtained by blending 0% by weight of a lower alcohol, a gel base, water and a silicate compound.

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to a gel preparation containing an insect repellent such as N, N-diethyl-m-toluamide (hereinafter referred to as "diet"), which has good adhesiveness and does not adhere to the skin. The present invention relates to a gel-like insect repellent preparation having low absorption, and further relates to a gel-like insect repellent preparation having no white residue after application with a compounded silicic acid compound.

[0002]

2. Description of the Related Art Conventionally, as an insect repellent preparation, a spray, an aerosol, a gel preparation and the like have been already on the market. However, each of the preparations has a drawback that the insect repellent efficacy time is short because the preparations run off by sweating of the skin and disappear from the skin by contact with clothes. In addition, some insect repellents such as diet are absorbed through the skin,
It is known that toxic brain damage may occur especially in infants when an excessive amount is used for a long period of time (D
L Edwards and CE Johnson,
Clin Pharm, 6: 496.1987).

As a gel preparation containing an insect repellent,
For example, JP-A-5-331033 and the like and spray agents are reported in, for example, JP-A-7-126104. Specifically, JP-A-5-33103
No. 3 discloses a gel preparation containing a gel base, a neutralizing agent, water, an insect repellent and a dispersant, and JP-A 7-1
In Japanese Patent No. 26104, a spray formulation containing a porous silicic acid compound adsorbing diet is intended to extend the insect repellent effect time.

However, any insect repellent has insufficient room for improvement because measures against the runoff of the preparation due to perspiration and the absorbability from the skin are insufficient. Also,
Insect repellents containing silicic acid compounds have been sought to be improved because white residue occurs during application.

Therefore, a gel-like insect repellent preparation having good adhesion after application, little absorption from the skin, and no white residue has not been obtained yet.

[0006]

SUMMARY OF THE INVENTION The present invention has been made from the above viewpoint, and an object of the present invention is to provide a gel insect repellent preparation which has good adhesion after application and little absorption from the skin. .

It is a further object of the present invention to provide a gel-like insect repellent preparation containing no white residue, which is peculiar to the insect repellent preparation containing a silicic acid compound.

[0008]

Means for Solving the Problems As a result of intensive studies in view of the above points, the present inventors have found that insect repellents, lower alcohols of 10 to 30% by weight with respect to the total amount of preparations, and gel bases. , Containing water and silicic acid compounds, found a formulation of a gel-like insect repellent formulation with good adhesiveness after application and less absorption from the skin, and by incorporating a cellulose-based polymer, the adhesiveness was improved. We have found a formulation that further enhances the absorption suppression effect. Furthermore, the present invention has been completed by finding a formulation containing a polyol or fats and oils that does not cause a white residue after application which is peculiar when a silicic acid compound is blended.

[0009]

BEST MODE FOR CARRYING OUT THE INVENTION The present invention is described in detail below.
Insect repellents include natural or synthetic compounds that have an insect repellent effect. For example, eucalyptol, α-pinene, geraniol, citronellal,
Camphor, linalool, dioctyl phthalate, dibutyl phthalate, naphthalene, diet, permethrin, N
-(2-Ethylhexyl) -bicyclo [2,2,1]-
Examples thereof include hepta-5-ene-2,3-dicarboximide. The compounding amount of the insect repellent varies depending on the kind of the insect repellent used, but is preferably 1 to 20% by weight, more preferably 3 to 15% by weight based on the total amount of the preparation. It is preferable that the amount of the insect repellent compounded is within the above range in order to exhibit a safe and sufficient insect repellent effect.

As the lower alcohol, use is made of any alcohol having up to about 3 carbon atoms which can be applied to the skin, depending on the dispersion of the insect repellent during the preparation of the preparation, the feel at the time of application of the preparation, the stability of the preparation and the like. Examples thereof include isopropanol and ethanol. Further, denatured alcohols obtained by adding a denaturing agent such as a fragrance to these lower alcohols and the like are also included. The lower alcohol content is 10 to 30% by weight, preferably 20 to 30% by weight, based on the total amount of the preparation. When the amount of the lower alcohol is within the above range, it is preferable in order to suppress the penetration of the preparation component into the skin and to improve the quick-drying property after application.

Examples of the gel base include acrylic acid polymer compounds such as carboxyvinyl polymer, vinyl polymer compounds such as polyvinyl alcohol and polyvinylpyrrolidone, and polysaccharides such as xanthan gum, alginic acid and salts thereof. . The content of the gel base is preferably 0.01 to 10% by weight, more preferably 0.1 to 5% by weight, based on the total amount of the preparation. When the amount of the gel base compounded is within the above range, suitable viscosity is exhibited without hindering the production and use of the preparation, and it is preferable for improving the usability during application.

[0012] Among the above-mentioned gel bases, those which are gelated by swelling in water and those which are swollen and gelated by neutralization are known, and any of them can be used in the present invention. However, when a gel base which gels by neutralization is used in the present invention, a neutralizing agent is used. The neutralizing agent is preferably selected according to the type of gel base,
In adjusting the pH of the preparation, one or more neutralizing agents can be added at the time of gelation of the gel base, or at any time different from the time of gelation.

Examples of the neutralizing agent include inorganic bases such as sodium hydroxide, potassium hydroxide and ammonia water, organic bases such as diisopropanolamine, diethylamine and triethylamine, inorganic acids such as hydrochloric acid, sulfuric acid and phosphoric acid, and citric acid. Examples thereof include organic acids such as tartaric acid, maleic acid, lactic acid, ascorbic acid and glycolic acid. The content of the neutralizing agent varies depending on the type and content of the gel base, but is preferably 0.01 to 5% by weight based on the total amount of the preparation.
When the content of the neutralizing agent is in the above range, it is preferable for sufficiently neutralizing the gel base material without causing destabilization such as aggregation of the gel base due to over-neutralization and expressing an appropriate viscosity. .

The amount of water to be added varies depending on the type and amount of the components to be added to the preparation, but is 30 to 80 relative to the total amount of the preparation.
% Is preferable, 35 to 70% by weight is more preferable, and 45 to 65% by weight is particularly preferable. It is preferable for the amount of water to be in the above range to form a stable and good gel.

The silicic acid compound is not particularly limited as long as it adsorbs a compounding ingredient such as an insect repellent and maintains the insect repellent effect. For example, hydrous silicon dioxide, hydrophobic silica, calcium silicate, diatomaceous Examples include soil, high-purity silica, and silicic acid anhydride. The specific surface area of the silicic acid compound is preferably 300 m ² / g or more, particularly preferably 500 m ² / g or more. The content of the silicic acid compound is preferably 0.01 to 20% by weight, more preferably 1 to 10% by weight, and particularly preferably 2 to 10% by weight, based on the total amount of the preparation. When the compounding amount of the silicic acid compound is within the above range, a sufficient persistence of the insect repellent effect is expected, and it is preferable for forming a stable preparation.

In order to further improve the durability of the insect repellent effect, the gel-like insect repellent preparation of the present invention preferably contains a cellulosic polymer. As the cellulosic polymer, carboxymethyl cellulose and salts thereof,
Examples thereof include methyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose and the like. Among them, hydroxypropyl methylcellulose is particularly preferable. The blending amount of the cellulosic polymer is preferably 0.01 to 10% by weight, more preferably 0.05 to 5% by weight, and particularly preferably 0.1 to 2% by weight based on the total amount of the preparation.
% By weight. The preferred molecular weight of the cellulosic polymer is 1500 to 40,000, more preferably 1
It is 500 to 10,000. It is preferable that the blending amount and the molecular weight of the cellulosic polymer are within the above ranges in order to sufficiently exhibit the effect of improving the adhesiveness of the preparation without impairing the stability and usability of the preparation.

The gel insect repellent preparation of the present invention may contain either one or both of a polyol and a fat and oil in order to prevent white residue after application, which is peculiar when a silicic acid compound is added. preferable.

Examples of polyols include polyethylene glycol, glycerin, propylene glycol and 1,3-butylene glycol. The content of the polyol is preferably 0.1 to 15% by weight, more preferably 0.5 to 10% by weight, based on the total amount of the preparation.
It is particularly preferably 1 to 5% by weight.

Examples of the oils and fats include hydrocarbons such as squalane and liquid paraffin, and esters such as isopropyl myristate, diisopropyl adipate and octyldodecyl myristate. The amount of fats and oils is preferably 0.1 to 15% by weight, more preferably 0.5 to 10% by weight, and particularly preferably 1 to 5% by weight, based on the total amount of the preparation.

It is preferable that the blending amount of the polyol or the oil and fat is within the above range in order to sufficiently exhibit the effect of preventing white residue without impairing the stability of the preparation and the feeling of use.

The gel-like insect repellent preparation of the present invention may optionally contain various optional components which are acceptable as a pharmaceutical additive and which can be transdermally administered. As such an additive, for example, a stabilizer, a preservative, a fragrance, a colorant, an ultraviolet protective agent, a surfactant, and the like can be added as desired, but not limited thereto. .

As the above-mentioned various optional components, examples of the stabilizer include sodium edetate and the like. Examples of preservatives include parabens. Further, as the fragrance, for example, peppermint oil, dl-camphor and L
-Menthol etc. can be illustrated. Examples of the colorant include indigo carmine, yellow ferric oxide and copper chlorophyll. Moreover, titanium oxide etc. can be illustrated as an ultraviolet protection agent. Examples of surfactants include fatty acid polyhydric alcohols, polyoxyethylene sorbitan fatty acid esters, and polyoxyethylene ethers such as polyoxyethylene hydrogenated castor oil.

The pH of the gel-like insect repellent preparation of the present invention is, for example, preferably 4-9, more preferably 5-8, from the viewpoints of the stability of the components and the preparation and the reduction of irritation during application. . The pH of the preparation can be adjusted with the above-mentioned neutralizing agents such as acids and alkalis, pH buffering agents and the like.

The method for producing the gel-like insect repellent preparation of the present invention is not particularly limited, but usually, a gel base and a cellulosic polymer are added to water and stirred to swell to form an aqueous phase, and a silicic acid compound and a lower alcohol are used as insects. After adding repellent, oil or polyol if necessary, and homogenizing, add to water phase and stir,
Further, if necessary, a neutralizing agent may be added to the aqueous phase, and then the mixture may be stirred until the mixture is uniform.

[0025]

The present invention will be described in more detail with reference to examples, but the present invention is not limited thereto.

<Example 1> 55.99 g of water, 0.5 g of carboxyvinyl polymer, 0.01 edetate sodium
g, and the mixture was stirred and swollen to form an aqueous phase. Hydrous silicon dioxide (Product name: Adsolider 102, Manufacturer: Freund Sangyo Co., Ltd., the same in the following examples and comparative examples)
After adding 12 g of diet to 4 g of ethanol and 25 g of ethanol to homogenize, add to the aqueous phase and stir, and further add 2.5 g of a 10% aqueous solution of diisopropanolamine to the aqueous phase, stir until uniform, and then gel insect A repellent formulation was obtained.

<Example 2> 55.49 g of water, 0.5 g of carboxyvinyl polymer, hydroxypropylmethyl cellulose (product name: Metroze 60SH-4000, manufacturer: Shin-Etsu Chemical Co., Ltd., the same in the following examples and comparative examples) ) 0.5 g and sodium edetate 0.01
g, and the mixture was stirred and swollen to form an aqueous phase. After adding 12 g of diet to 4 g of hydrous silicon dioxide and 25 g of ethanol to homogenize, add to the aqueous phase and stir, and further add 2.5 g of a 10% diisopropanolamine aqueous solution to the aqueous phase,
The mixture was stirred until it became uniform to obtain a gel insect repellent preparation.

<Example 3> 52.49 g of water, 0.5 g of carboxyvinyl polymer, 0.5 g of hydroxypropylmethyl cellulose, polyethylene glycol 400 (Product name: Macrogol 400, manufacturer: NOF Corporation, the following examples and comparative examples) 2 g), 0.5 g of diisopropyl adipate, 0.5 g of concentrated glycerin and 0.01 g of sodium edetate were added and stirred to swell to obtain an aqueous phase. 12 g of diet was added to 4 g of hydrous silicon dioxide and 25 g of ethanol to homogenize, and then added to the aqueous phase and stirred,
Furthermore, 2.5% diisopropanolamine 10% aqueous solution
After adding g to the aqueous phase, the mixture was stirred until it became uniform to obtain a gel insect repellent preparation.

Example 4 Water 59.49 g, carboxyvinyl polymer 0.5 g, hydroxypropylmethylcellulose 0.5 g, polyethylene glycol 400 2
g, 0.5 g of diisopropyl adipate, 0.5 g of concentrated glycerin and 0.01 g of sodium edetate were added and stirred to swell to obtain an aqueous phase. After adding 5 g of diet to 4 g of hydrous silicon dioxide and 25 g of ethanol to homogenize, add to the aqueous phase and stir, and further diisopropanolamine 1
After adding 2.5 g of 0% aqueous solution to the aqueous phase, the mixture was stirred until it became homogeneous to obtain a gel insect repellent preparation.

Comparative Example 1 Water 59.99 g, carboxyvinyl polymer 0.5 g and sodium edetate 0.0
1 g was added and stirred to swell to obtain an aqueous phase. Ethanol 2
After adding 12 g of diet to 5 g and homogenizing, adding to the aqueous phase and stirring, 2.5 g of a 10% aqueous solution of diisopropanolamine was further added to the aqueous phase, and then stirring until uniform.
A gel insect repellent formulation was obtained.

Comparative Example 2 Water 45.99 g, carboxyvinyl polymer 0.5 g and sodium edetate 0.0
1 g was added and stirred to swell to obtain an aqueous phase. After adding 12 g of diet to 4 g of hydrous silicon dioxide and 35 g of ethanol and homogenizing the mixture, the mixture was added to the aqueous phase and stirred, and 2.5 g of a diisopropanolamine 10% aqueous solution was added to the aqueous phase.
The mixture was stirred until it became uniform to obtain a gel insect repellent preparation.

<Comparative Example 3> Preparation was carried out according to the preparation method of Examples described in JP-A-5-331033.
Purified water was added to carboxyvinyl polymer as a gel base, and 5 g of diet as a repellent and isopropyl alcohol as a dispersant were added to 40 g of a 2% aqueous solution thereof.
g and 4 g of purified water were mixed. Next, 1 g of triethanolamine as a gelling agent was added to this solution with stirring to prepare a preparation, and a gel insect repellent preparation was obtained.

"Evaluation of Examples and Comparative Examples"<Experimental Example 1> Regarding Examples 1 to 3 and Comparative Examples 1 and 2,
The adhesiveness, the absorbability from the skin, and the white residue during use were examined.

The adhesion was evaluated by measuring the residual adhesion rate of the gel insect repellent preparation on the glass slide surface. That is, 0.2 g of the gel-like insect repellent preparation was evenly applied onto the slide glass, dried, and 10 mL of purified water was dripped from the top of the slide glass for 15 seconds in an almost vertical state to prepare the gel-like insect repellent preparation. The residual adhesion amount was measured and the residual adhesion rate was calculated.

The evaluation of the absorbability from the skin was carried out by applying the gel insect repellent preparation onto the skin of the rat and measuring the loss rate by the amount of diet in the preparation remaining after a certain period of time. . That is, after shaving the abdomen of the rat,
Apply 1g (4cm x 4cm) of gel insect repellent preparation,
After 6 hours, the amount of diet in the remaining preparation was measured, and the diet loss rate was calculated from the amount lost.

The white residue after use was evaluated by taking 0.5 g of a gel-like insect repellent preparation, applying it on the upper arm, and observing the applied surface after 15 minutes and making a judgment. That is, if even a part of the coated surface was white, it was determined that there was white residue. The results are shown in Table 1.

[0037]

[Table 1]

From the results in Table 1, it was found that when the silicic acid compound was not added, the residual adhesion rate was low and the diet loss was high, and the diet loss was high unless the lower alcohol was 30% by weight or less.

Further, the gel-like insect repellent preparation of Example 2 in which the cellulosic polymer was blended in the formulation of Example 1 had no significant difference in the amount of diet loss as compared with Example 1, but had higher adhesion. It was confirmed to have sex.
In addition, the gel-like insect repellent preparation of Example 3 in which the fat and oil and the polyols are added to the formulation of Example 2 does not show the white residue after use, which is observed in Examples 1 and 2.

From the above points, a gel-like insect repellent preparation containing an insect repellent, 10 to 30% by weight of a lower alcohol, a gel base, a neutralizing agent, water and a silicic acid compound has good adhesiveness after application. Therefore, it is a gel-like insect repellent formulation that is hardly absorbed from the skin, and the adhesive force is further enhanced by further containing a cellulosic polymer, and when a silicic acid compound is blended by containing a polyol and fats and oils. It was found that a gel-like insect repellent preparation without a characteristic white residue can be obtained.

<Experimental Example 2> The adhesiveness and absorbability from the skin of Example 4 and Comparative Example 3 and a commercially available gel-like insect repellent preparation were examined. The results are shown in Table 2.

[0042]

[Table 2]

From the results shown in Table 2, it is disclosed in Japanese Patent Laid-Open No. 5-331033.
The formulation of Example (Comparative Example 3) and the commercially available gel-like insect repellent preparation in JP-A No. 1993-121242 were poor in adhesiveness and high in absorbability as compared with the gel-like insect repellent preparation in Examples.

[0044]

According to the gel insect repellent preparation of the present invention,
A gel insect repellent preparation containing an insect repellent, a lower alcohol, a gel base, water and a silicic acid compound, wherein the content of the lower alcohol is 10 to 30% by weight based on the total amount of the preparation.
Therefore, it is possible to provide an insect repellent preparation having good adhesion after application and little absorption from the skin.

In the present invention, when the insect repellent is N, N-diethyl-m-toluamide, it is much more effective in providing an insect repellent preparation having a high insect repellent effect and excellent safety. .

In the present invention, the addition of a cellulosic polymer further enhances the adhesiveness of the preparation to the skin and is more effective in sustaining the insect repellent effect. The cellulosic polymer is hydroxypropylmethylcellulose. It is more effective from the above viewpoint.

In the present invention, the addition of one or both of a polyol and an oil / fat is more effective in preventing the white residue after application of the preparation, which is peculiar to the preparation containing a silicic acid compound.

   ─────────────────────────────────────────────────── ─── Continued front page    (72) Inventor Toshio Inaki             6-10-203 Nishiwakacho, Mishima City, Shizuoka Prefecture F-term (reference) 4H011 AC06 BA01 BB06 BC03 BC04                       BC06 BC18 BC19 DA17 DD07                       DF05 DG03 DH02 DH10 DH25

Claims (5)

[Claims] 1. A gel insect repellent preparation containing an insect repellent, a lower alcohol, a gel base, water and a silicic acid compound, wherein the lower alcohol is contained in an amount of 10 to 30% by weight based on the total amount of the preparation. Is a gel insect repellent formulation. 2. The gel insect repellent preparation according to claim 1, wherein the insect repellent is N, N-diethyl-m-toluamide. 3. The gel insect repellent preparation according to claim 1, further comprising a cellulosic polymer. 4. The gel insect repellent preparation according to any one of claims 1 to 3, further containing one or both of a polyol and an oil and fat. 5. The gel-like insect repellent preparation according to claim 3, wherein the cellulosic polymer is hydroxypropylmethylcellulose.