JP3038837B2 - Aerosol for skin cooling - Google Patents

Description

Description: BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an aerosol which forms a sherbet-like foam gel at the time of injection and has strong skin cooling properties.

2. Description of the Related Art Cooling the affected area is effective in rapidly relieving pain caused by bruises, sprains, and muscle fatigue, and itching caused by athlete's foot and insect bites. Conventionally, for such pain and itching, an aerosol spraying out in a mist has been used.

Problems to be Solved by the Invention However, when the aerosol sprayed out in the form of a mist adheres to the skin, Freon and LP are used as refrigerants.
Since G, dimethyl ether and the like evaporate instantaneously, a continuous cooling property cannot be obtained. Therefore, pain and itch cannot be completely relieved. It is an object of the present invention to solve the disadvantages of the prior art and to provide an aerosol having a strong and sustained skin cooling when spray applied.

Means for Solving the Problems The present invention is an aerosol comprising a stock solution obtained by mixing the following components (A) and (B) with a solvent comprising water and / or a lower alcohol, and a liquefied gas propellant.

(A) One or two or more selected from polyoxyethylene sorbitan fatty acid ester and sorbitan fatty acid ester are dissolved and mixed, and become a paste or semi-solid at room temperature. (B) Active ingredient In the present invention, Or a mixture of one or more selected from polyoxyethylene sorbitan fatty acid ester and sorbitan fatty acid ester, which is a paste or semi-solid at room temperature is polyoxyethylene (6) sorbitan Monostearate alone or a mixture of polyoxyethylene (20) sorbitan monostearate, polyoxyethylene (20) sorbitan tristearate and sorbitan monostearate is preferred, and the blending amount thereof is 0.1 to 8% by weight.
Preferably it is 0.5-4% by weight. The important thing here is that
Even if one or two or more selected from polyoxyethylene sorbitan fatty acid esters and sorbitan fatty acid esters are dissolved and mixed, they are not paste or semi-solid at room temperature (for example, solid or liquid at room temperature). ), The effect of the present invention cannot be obtained.

The solvent is water, a lower alcohol or a mixture of water and a lower alcohol, and most preferably a mixture of water and a lower alcohol having a weight ratio of 30:70 to 70:30. The amount of the solvent is preferably 20 to 40% by weight.
If the amount of the solvent is less than 10% by weight, a mist is formed when the aerosol is injected. On the other hand, when the content exceeds 60% by weight, a foam like a shaving foam is formed at the time of spraying the aerosol, and the feeling of cooling is lost. As the lower alcohol, ethanol, isopropanol and the like can be used.

As a liquefied gas that is a propellant, dimethyl ether,
n-butane, isobutane, propane, or a mixture thereof can be used. The amount of the liquefied gas is preferably 50 to 70% by weight. If the amount of the propellant is less than 40% by weight, a foam like a shaving foam is formed at the time of spraying the aerosol, and the feeling of cooling is lost. On the other hand, if it exceeds 80% by weight, it will be atomized when the aerosol is injected.

The active ingredients include anti-inflammatory analgesics (indomethacin, methyl salicylate, glycol salicylate, ketoprofen, diclofenac, ibuprofen, mefenamic acid, etc.), antipruritics (crotamiton, icutamol, moctamol, thymolic acid, etc.), antifungals (tolnaftate, miconazole nitrate, etc.) ), Antihistamines (diphenhydramine, diphenhydramine hydrochloride, isotipendyl hydrochloride, etc.), local anesthetics (lidocaine, dibucaine hydrochloride, etc.),
Bactericides (potassium iodide, chlorhexidine gluconate, acrinol, benzalkonium chloride, etc.) and cooling agents (I-menthol, camphor, peppermint oil, etc.) can be used. 0.001 to 5% by weight of active ingredient
It is.

The aerosol of the present invention may contain an antioxidant (such as dibutylhydroxytoluene), a solubilizer (such as diisopropyl adipate, isopropyl myristate, lactic acid, and sodium hydroxide), a fragrance, and a dye, if necessary.

The aerosol of the present invention is prepared by heating, mixing, stirring and dissolving or uniformly dispersing components other than the propellant (liquefied gas) to prepare a liquid, and then filling the aerosol container with the propellant. Can be manufactured.

Effect of the Invention According to the present invention, it has become possible to provide an aerosol agent that forms a sherbet-like foam gel when spray-applied onto the skin and has a sustained and strong skin cooling property.

As a result, pain caused by bruises, sprains, and muscle fatigue, or itching caused by athlete's foot or insect bites can be immediately and continuously alleviated.

Examples Next, the present invention will be described more specifically with reference to Examples and Test Examples.

Example 1 (Components) (Blending amount W%) Indomethacin 0.31 Diisopropyl adipate 4.07 Polyoxyethylene (20) sorbitan monostearate 1.22 Polyoxyethylene (20) sorbitan tristearate 0.81 Sorbitan monostearate 1.22 Dibutyl hydroxytoluene 0.04 I-Menthol 0.08 Denatured alcohol 14.23 Purified water 15.82 LPG 2.71 Dimethyl ether 59.49 Components other than the propellant were heated, mixed and stirred to uniformly disperse to prepare a stock solution. The undiluted solution was filled in a pressure-resistant container, fitted with a valve, and filled with a propellant. The product was equipped with a spout for injection.

Example 2 (Components) (Blending amount w%) Miconazole nitrate 0.40 Polyoxyethylene (6) sorbitan monostearate 2.02 Lactic acid 0.09 Sodium hydroxide 0.04 I-menthol 0.40 Denatured alcohol 17.52 Purified water 17.26 Dimethyl ether 62.26 An aerosol was prepared according to Example 1.

Comparative Example 1 (Ingredients) (Blending amount W%) Indomethacin 0.30 Diisopropyl adipate 3.97 Sorbitan monostearate 3.18 (Solid at room temperature) Dibutylhydroxytoluene 0.04 Denatured alcohol 13.91 Purified water 16.17 Dimethyl ether 62.43 To produce an aerosol.

Comparative Example 2 (Components) (Blending amount W%) indomethacin 0.30 diisopropyl adipate 3.97 glyceryl monostearate 3.18 (solid at room temperature) dibutylhydroxytoluene 0.04 denatured alcohol 13.91 purified water 16.17 dimethyl ether 62.43 To produce an aerosol.

Comparative Example 3 (Components) (Blending amount W%) Indomethacin 0.30 Diisopropyl adipate 3.97 Polyoxyethylene (60) hydrogenated castor oil 3.18 Dibutylhydroxytoluene 0.04 Denatured alcohol 13.91 Purified water 16.17 Dimethyl ether 62.43 The above components are the same as in Example 1. To produce an aerosol.

Comparative Example 4 (Components) (Blending amount W%) Fluorocarbon 11 80.00 Fluorocarbon 12 20.00 Production Method The content components were filled in a pressure-resistant container, and a valve was attached. The product was equipped with an injection button.

Comparative Example 5 (Components) (Blending amount W%) Glycol salicylate 5.4 L-menthol 5.4 Modified alcohol 51.4 LPG 37.8 An aerosol was produced according to Example 1 for the above components.

Test Example In Examples 1 and 2 and Comparative Examples 1 to 5, when spray-applied to the skin, the presence / absence of formation of a sherbet-like foam gel having high cooling properties and a change in skin temperature after the spray-application were measured. The measurement of the skin temperature was performed by fixing a thermocouple sensor on the skin with a tape and spraying an aerosol agent thereon for 3 seconds.

 Table 1 shows the results.

From the results in Table 1, Examples 1 and 2 form sherbet-like foam gels, but Comparative Examples 1 to 5 do not form sherbet-like foam gels. Regarding the change in skin temperature, in Comparative Examples 1 to 5, the skin temperature decreased by about 10 ° C. as compared to before the spray application, and returned to the original skin temperature about 10 minutes after the spray application. On the other hand, in Examples 1 and 2, the temperature was lowered by about 30 ° C. as compared to before the spray coating, and was lowered by about 6 ° C. even 20 minutes after the spray coating. From these results, it can be seen that Examples 1 and 2 have strong and continuous skin cooling properties.

──────────────────────────────────────────────────続 き Continued on the front page (72) Fumio Urushizaki 3-24-1, Takada, Toshima-ku, Tokyo Taisho Pharmaceutical Co., Ltd. (72) Toshimitsu Seki 3- 24-1, Takada, Toshima-ku, Tokyo Taisho Pharmaceutical (56) References JP-A-48-94682 (JP, A) JP-A-48-92282 (JP, A) JP-A-63-201118 (JP, A) (58) Fields investigated (Int. Cl. ⁷ , DB name) A61K 9/12 A61K 47/10 A61K 47/14 A61K 47/32 CA (STN)

Claims (3)

(57) [Claims] (1) The mixing ratio of water and lower alcohol is 30: 70-7.
It is composed of a stock solution obtained by mixing the following components (A) and (B) in a mixed solvent at 0:30, and a liquefied gas propellant, wherein the propellant is mixed in an amount of 50 to 70% by weight. A skin cooling aerosol that forms a foamy gel. (A) a component selected from a polyoxyethylene sorbitan fatty acid ester and a sorbitan fatty acid ester, which is a paste or semi-solid at room temperature, or two or more selected from a polyoxyethylene sorbitan fatty acid ester and a sorbitan fatty acid ester (B) The active ingredient which is a paste or semi-solid at room temperature when dissolved and mixed. 2. A skin cooling aerosol according to claim 1, wherein the liquefied gas is dimethyl ether, n-butane, isobutane, propane or a mixture thereof. 3. The skin cooling aerosol according to claim 1, wherein the amount of the solvent is 20 to 40% by weight of the whole preparation.