JPH072944B2 - Cooling azole composition - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION (a) Field of Industrial Application The present invention relates to a cooling aerosol composition and a cooling agent which are useful as a cooling first aid for an affected area such as a bruise or a sprain during sports, and a cooling treatment agent in the orthopedic region. The present invention relates to an aerosol formulation for use.

(B) Conventional technology Conventional aerosol type instant cooling agents (hereinafter, simply referred to as cooling aerosol preparations) have a formulation in which the cooling effect is given the highest priority, and most of them are CFCs alone.
Also, as described in Japanese Examined Patent Publication No. 45-35797, trichloromonofluoromethane and dichlorodifluoromethane are mixed 9: 1.
Aerosol for cooling anesthesia mixed at a ratio of
As described in No. 06 publication, 1,1-dichloro-1,2,2-trifluoroethane, 1,1,2-trichloro-1,2,2-trifluoroethane, 1,1,1-trichloroethane, etc. Only a compounding recipe of an organic compound having a specific physical property value and carbon gas which is a compressed gas is known. Moreover, the cooling aerosol preparations of these formulations are sprayed in a large amount at one time and are intended only for a temporary cooling effect, and have the following drawbacks.

 The spraying property of the injected gas during use is remarkable.

Due to lack of consideration for the skin after use, skin irritation occurs, especially the skin on the skin surface is easily damaged, and the skin is rough.

Although there is a cooling effect during use, the maintenance of the cooling sensation after use is temporary, and the sustaining effect is too short.

Since it consists of a gas composition, there is no moist feeling on the skin.

It does not have a moisturizing effect on the skin because it consists of gas components.

(C) Problems to be Solved by the Invention As described in the preceding paragraph, conventional cooling aerosol preparations have various drawbacks, and it cannot be said that they are sufficiently satisfactory.

Therefore, in order to overcome the above-mentioned various drawbacks, the present inventors have earnestly conducted development and research of a cooling aerosol preparation, and found a practically satisfactory formulation of the cooling aerosol preparation, This has led to the completion of an aerosol composition.

That is, the problem to be solved by the present invention is the above-mentioned various drawbacks, and is to provide a useful cooling aerosol preparation.

(D) Means for Solving Problems The present invention relates to a cooling aerosol composition prepared by formulating each of the bases and components described in detail below, and various additives and the like in a specific mixing ratio, if necessary. It is a thing. More specifically, the present invention provides (a) Freon gas 60-
90% by weight, (b) dimethyl ether 10 to 30% by weight,
(C) 0.01 to 5% by weight of a moisturizing agent and / or a skin roughness preventive agent,
(D) 0.1 to 3% by weight of a cooling agent and (e) a lower alcohol
The present invention relates to a cooling aerosol composition comprising 0.1 to 10% by weight. The present invention also provides
(A) Freon gas 60 to 90% by weight, (b) dimethyl ether 10 to 30% by weight, (c) moisturizing agent and / or skin roughness preventive agent
A container for aerosol formulation is filled with a cooling aerosol composition comprising 0.01 to 5% by weight, (d) a cooling agent of 0.1 to 3% by weight, and (e) a lower alcohol of 0.1 to 10% by weight. The present invention relates to a cooling aerosol preparation.

A more detailed description will be given below.

First of all, as the low boiling point non-combustible gas used for satisfying the cooling effect instantaneously as a propellant, that is, as a CFC gas, trichloromonofluoromethane (generic name: CFC1
1), dichlorodifluoromethane (generic name: Freon 1
2), 1,1,2-trichlorotrifluoroethane (generic name:
Freon 113) or dichlorotetrafluoroethane (generic name: Freon 114) is used alone or in combination of two or more. The amount used is 60 to 90% by weight, preferably 70 to 85
An optimum cooling aerosol composition can be prepared by blending the composition in an amount of, by weight, more preferably 75 to 85% by weight.

In addition, as the other propellant, dimethyl ether, a propellant that has been widely used as an aerosol propellant can be appropriately used. In addition, the aerosol formulation for human body must be slightly flammable or less flammable, and its use amount is limited due to flammability regulation etc., but is within the limit range of 10 to 30. It is suitable to blend in a weight percentage, preferably 12 to 27 wt%, more preferably 15 to 20 wt%.

Incidentally, the total amount of the propellant consisting of chlorofluorocarbon gas and dimethyl ether is preferably 90% by weight or more, more preferably 95% by weight or more gas composition and stock solution composition of the cooling aerosol formulation, or the internal pressure, etc. It is desirable for making a comprehensive judgment.

Next, as a moisturizer, benzyl alcohol, lanolin fatty acid isopropyl, polyethylene glycol, propylene glycol, dipropylene glycol, diethylene glycol, triethylene glycol, 1,3-butylene glycol, a water-soluble polymer (for example, methyl cellulose,
Ethyl cellulose, polyvinylpyrrolidone, poval,
(Hydroxypropyl cellulose, carboxyvinyl polymer, etc.), squalane, coconut oil, clove oil, olive oil, castor oil, camellia oil, soybean oil and the like are used alone or in combination of two or more.

Next, vitamins are used as an anti-skin agent, but fat-soluble vitamins are particularly preferable for the present invention. For example, vitamin A oils such as vitamin A oil, retinol acetate, retinol palmitate, etc.
Ergocalciferol or the like is used as the class, and dl-α-tocopherol, dl-α-tocopherol acetate, dl-α-tocopherol nicotinate, natural vitamin E or the like is used as the vitamin Es. In addition, vitamins B, vitamins C, vitamins K, etc. are also used.

The blending of the present invention of a moisturizer and / or skin anti-rash agent is used for the purpose of softening the feeling of use or irritation to the skin or skin roughening, and the amount thereof is an amount that gives moisturizing and moist feeling to the skin. Of course, an amount that does not affect the feeling of use such as stickiness or dryness and an amount that alleviates skin irritation or rough skin are blended. Specifically, the amount is 0.01 to 5% by weight, preferably 0.01 to 3% by weight, and more preferably 1% by weight.

Next, as a cooling agent, menthol, menthone, citronellal, etc. having a cooling effect are blended alone or in combination of two or more, and the amount thereof is 0.1 to 3% by weight, preferably 0.1 to 1% by weight, more preferably 0.1 to 0.5 wt% is desirable.

Next, examples of the lower alcohol include alcohols having 1 to 6 carbon atoms. Among them, ethanol, propanol or isopropanol is particularly preferable. Also, these anhydrous alcohols or denatured alcohols can be used. If the content is 10% or more, the drying on the skin will be slow, the use feeling will be impaired, and the irritation to the skin will be strong, which may cause damage to the skin. It is desirable that the agent and the cooling agent are dissolved in an amount capable of being dissolved, that is, 0.1 to 10% by weight, preferably 0.1 to 5% by weight, and more preferably 0.1 to 1% by weight.

Incidentally, in the present invention, a fragrance may be blended if necessary. For example, improve the usability by blending one or more citrus-based (orange, lemon, lime, grapefruit, etc.) or mint-based (peppermint, spearmint, etc.) fragrances that have a sensation of coldness or freshness. Is possible.

The present invention relates to a cooling aerosol composition composed of a blending formulation in which the above-mentioned respective bases and components are specified as described above, and this blending composition was found for the first time as a result of intensive studies by the present inventors. It is a new one not yet listed.

Next, a method for producing the cooling aerosol composition of the present invention will be described.

First, 5% by weight or less of a moisturizing agent and / or skin roughness preventive agent, or if necessary, a slight amount of a fragrance and 10% by weight or less of a lower alcohol are stirred and mixed at room temperature or under heating to form a uniform solution, and then at room temperature. Or, add 5% by weight or less of a cooling agent under heating,
Further, they are mixed by stirring to form a uniform solution. Next, put this solution in an appropriate pressure resistant container, attach a valve that can be used upside down,
The total amount of propellant composed of 60 to 90% by weight of chlorofluorocarbon and 10 to 30% by weight of dimethyl ether is adjusted to 90% by weight or more, and the mixture is press-filled by a known method. Then, the desired cooling aerosol formulation is prepared by stopping the press-fitting and filling at a suitable pressure (3.5 to 3.6 kg / cm ^{2 at} 25 ° C.) and attaching an appropriate push button capable of ejecting.

(E) Action The cooling aerosol composition of the present invention has a remarkable cooling sensation action and a continuous action during spraying. In addition, it gives a moist feeling during spraying and has an excellent moisturizing effect.

In addition, it has a preventive action against skin roughening, a protective action for reducing skin roughening, and an action for alleviating skin irritation.

(F) Example Below, the Example and comparative example of this invention are shown.

Example 1 1-Menthol 1.5 Propylene glycol 0.5 Ethanol 3.0 Fragrance Trace Freon 11 31.5 Freon 12 47.3 Dimethyl ether 16.2 Total 100.0 (% by weight) 1-Menthol, propylene glycol, and a fragrance are stirred and dissolved in ethanol. A valve that can be used upside down is attached, a propellant is press-fitted, and an appropriate push button that ejects the propellant at a desired pressure is attached.

Example 2 1-Menthol 1.0 Isopropyl myristate 0.3 dl-α-tocopherol 0.2 Ethanol 2.5 Fragrance Freon 11 31.9 Freon 12 47.8 Dimethyl ether 16.3 Total 100.0 (% by weight) Isopropyl myristate was added in place of propylene glycol of Example 1. Further, dl-α-tocopherol was further added, the following production was carried out in the same manner as in Example 1, and the use was evaluated.

Example 3 1-Menthol 0.5 Squalane 0.3 Tocopherol acetate 0.2 Ethanol 2.0 Fragrance Trace Freon 11 32.2 Freon 12 48.3 Dimethyl ether 16.5 Total 100.0 (wt%) Squalane was added instead of isopropyl myristate of Example 2 to give dl-α-tocopherol. Instead, tocopherol acetate was added, and the following production was performed in the same manner as in Example 1 and use evaluation was performed.

Example 4 1-Menthol 0.2 Squalane 0.03 Tocopherol acetate 0.02 Denatured ethanol 0.75 Fragrance Freon 11 32.9 Freon 12 49.3 Dimethyl ether 16.8 Total 100.0 (wt%) Ethanol of Example 3 was replaced with denatured ethanol, and produced in the same manner as in Example 1 below. , Evaluated for use.

Comparative Example 1 Commercially available aerosol formulation for cooling Freon 11 40 Freon 12 60 Total 100 (% by weight) A suitable pressure-resistant container was equipped with a valve that can be used upside down.
The propellant was press-fitted, and an appropriate push button for ejecting the propellant at a preferable pressure was attached to obtain a desired aerosol agent, which was evaluated for use.

COMPARATIVE EXAMPLE 2 Commercially available aerosol formulation for cooling Freon 11 33.2 Freon 12 49.8 Dimethyl ether 17.0 Total 100.0 (wt%) In Comparative Example 1, dimethyl ether was further added as a propellant, and the same production as in Comparative Example 1 was carried out and evaluated.

Test Example Below, the cooling sensation during spraying of the aerosol compositions of Examples 1 to 4 of the present invention and the commercially available aerosol formulations of Comparative Examples 1 and 2, the persistence and duration of the cooling sensation, or the moistening during use Twenty-five test subjects were tested for feeling and moisturizing condition, and further for stimulating action on the skin.
The test results are shown in Table 1.

(G) Effects The cooling aerosol composition of the present invention has the following effects which conventional existing products do not have.

It has an excellent cooling effect in the cooling state during spraying.

It has a remarkable effect on the persistence and duration of the cold sensation.

It has a favorable effect on the feeling of use (moisturization).

 It also has a very favorable effect on the moisturizing effect.

It has a significant effect on skin irritation (skin roughening) and has an effect of significantly suppressing skin roughening.

 In terms of odor, it has a favorable effect in use.

The present invention also has excellent physical and chemical stability in the formulation.

As described in detail above, the present invention has a very preferable composition and effect as a cooling aerosol composition, and can be said to be an industrially useful cooling aerosol preparation as an emergency treatment agent for bruise, sprain, etc. during sports. .

Claims (2)

[Claims] (1) 60 to 90% by weight of chlorofluorocarbon gas, (b) 10 to 30% by weight of dimethyl ether, (c) 0.01 to 5% by weight of moisturizing agent and / or skin roughness preventive agent, and (d) 0.1 to 10% of cooling agent. A cooling aerosol composition comprising 3% by weight and (e) a lower alcohol of 0.1 to 10% by weight. 2. (a) 60 to 90% by weight of chlorofluorocarbon gas, (b) 10 to 30% by weight of dimethyl ether, (c) 0.01 to 5% by weight of moisturizing agent and / or skin roughness inhibitor, and (d) 0.1 to 10% of cooling agent. A cooling aerosol composition comprising a container for aerosol preparation filled with a cooling aerosol composition comprising 3% by weight and (e) 0.1 to 10% by weight of lower alcohol.