JP3027838B2 - Eyazole composition - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

FIELD OF THE INVENTION The present invention relates to an azole composition. More particularly, the present invention relates to an eazole composition capable of imparting a warm feeling.

[0002]

2. Description of the Related Art Generally, an eazole product for human body includes:
Since liquefied gas or compressed gas is used as a propellant, when it is applied to hair, scalp, skin, mucous membranes, etc., the propellant removes heat of vaporization from the surface of the propellant, thereby giving a cooling feeling. This cooling sensation is not only the greatest advantage of the Eyazole product, but also its greatest drawback.

[0003] The advantages of cooling sensation include burns on the skin,
Rapid anti-inflammatory action against inflammation and hot flashes,
Exercise is given when body temperature rises after exercise.

[0004] Also, as a disadvantage, such as in winter,
If you use it when the body temperature is low in the open air,
The feeling of cooling causes discomfort, and physiologically, cooling causes contraction of capillaries such as epidermis and mucous membranes, cells and the like, and the incorporated active ingredient does not immediately penetrate into the body.

[0005]

Therefore, in view of the above prior art, the present inventors have focused on the cooling sensation which is a drawback of the conventional eazol products, and have been able to impart a warm feeling to the epidermis and mucous membrane. After extensive research to find products, surprisingly, polyhydric alcohol contained 50% by weight in the stock solution.
A stock solution containing the above and further having a specific composition, and the stock solution
It has been found that a comfortable warm feeling can be imparted to the skin and the like when an air-jet composition containing a specific proportion of a propellant is used, thereby completing the present invention.

[0006]

Means for Solving the Problems That is, the present invention has many advantages.
Polyhydric alcohol 50% by weight or more, lower alcohol 1-45% by weight
%, Active ingredient 20% by weight or less and adjuvant 50% by weight or less
50-90% by weight of the undiluted solution and 50-10% by weight of the propellant
It does not form a foam when sprayed,
Gives a cool feeling to the skin, and polyhydric alcohol gradually
Absorbs moisture in the upper skin layer and generates an exothermic reaction, giving a warm feeling
Eyazole composition and polyhydric alcohol 50 weight
%, Foam stabilizer 1-30% by weight, active ingredient 20% by weight or less
95 to 99.8% by weight of a stock solution consisting of 10% by weight and auxiliary agents
And CO ₂ , N ₂ O or N _{2 as} propellant _{5 to} 0.2 weight
% To form a low foaming fragile foam,
Polyhydric alcohol absorbs moisture in the upper layer of the skin, causing an exothermic reaction
The present invention relates to an air-jet composition which gives a feeling of warmth .

[0007]

Action and Examples As described above, the air-soluble composition of the present invention comprises a polyhydric alcohol of 50% by weight or more and a lower alcohol.
1-45% by weight of alcohol, 20% by weight or less of active ingredient and supplement
50-90% by weight of undiluted solution consisting of 50% by weight or less of auxiliaries
50 to 10% by weight.
Without cooling the skin, giving the skin a cooling sensation and gradually
Polyhydric alcohol absorbs moisture in the upper layer of the skin, causing an exothermic reaction
Eyazole composition that gives off a warm feeling
Sol composition I) and polyhydric alcohol 50-fold
% Or more, foam stabilizer 1-30% by weight, active ingredient 20% by weight or less
95-99.8% by weight of undiluted solution consisting of 10% by weight and auxiliary
And CO ₂ , N ₂ O or N _{2 as} propellant _{5 to} 0.2 weight
% To form a low foaming fragile foam,
Polyhydric alcohol absorbs moisture in the upper layer of the skin, causing an exothermic reaction
Eyazole composition that gives off a warm feeling
Sol composition II) .

[0008] As described above, the eazole composition of the present invention.
I and II contain 50% by weight or more of polyhydric alcohol in the stock solution
It is a thing.

Examples of the polyhydric alcohol include glycerin, propylene glycol, 1,4-butylene glycol, 1,3-butylene glycol, diethylene glycol, triethylene glycol, dipropylene glycol, hexylene glycol, polyethylene glycol and the like. These polyhydric alcohols may be used alone or in combination of two or more. Among these polyhydric alcohols, glycerin, propylene glycol and 1,3-butylene glycol impart an effective warm feeling and are highly safe for the human body, and they are widely used as moisturizing ingredients. Therefore, it is particularly preferable because it is also a good humectant.

When the polyhydric alcohol adheres to the skin in an anhydrous or nearly anhydrous state, it absorbs the water in the upper layer of the skin, at which time a mild exothermic reaction occurs. The heat generated at this time gives a feeling of warmth.

In order to sufficiently exhibit such an effect, the polyhydric alcohol is filled with the propellant in an aerosol container in an anhydrous state or a state close to the polyalcohol so as to prevent moisture in the air from entering. Is preferred. Therefore, it is desirable that the air-jet composition of the present invention is substantially non-aqueous.

[0012] The amount of the polyhydric alcohol to be used cannot be determined unconditionally because it varies depending on the form of the obtained aerosol composition. Form of the Eyazoru composition is defined by the state of Eyazoru composition ejected from Eyazoru vessel, (b) which does not form a foam sprayers (Eyazoru composition I), and (ii) fragile low foaming What forms a foam (Eyazole composition
It is roughly divided into two types of objects II).

The above-mentioned ( a ) the mist-forming, non-foamed aerosol composition I comprises 50 to 90% by weight of a stock solution and a propellant 10
Ru der consist of 50% by weight.

The stock solution is 50% by weight of the polyhydric alcohol.
Above, lower alcohol 1-45% by weight, active ingredient 20% by weight
And up to 50% by weight of adjuvants.

The amount of the polyhydric alcohol used is 50% by weight.
If it is less than 3, sufficient exothermic reaction does not easily occur, and it is difficult to give a warm feeling. In order to improve the mixing with the propellant and facilitate the injection as an azole, the amount of the polyhydric alcohol used is preferably 99% by weight or less. The amount of the polyhydric alcohol used is preferably 60 to 95% by weight.

The lower alcohols include, for example, ethyl alcohol, isopropyl alcohol, normal propyl alcohol and the like, and these lower alcohols are used alone or in combination of two or more. Incidentally, particularly preferred since Of these, ethyl alcohol and isopropyl alcohol may help solubilization of a high-grade alcohol, and allowing the formulation of various active ingredients prevents the solidified at low temperatures, ease to give a uniform dope It can be used for When the use amount of the lower alcohol is less than 1% by weight, solidification of the higher alcohol to be compounded occurs, it becomes difficult to mix non-polar active ingredients and the like, and when the amount exceeds 45% by weight, On the other hand, the cooling sensation accompanying the vaporization of the lower alcohol tends to make it difficult to feel the warmth. The lower alcohol is preferably used in an amount of 5 to 45% by weight, more preferably 3 to 20% by weight.

The active ingredient is,BookInventive eazol composition
objectIIs appropriately selected and used in accordance with the purpose of use, and specifically,
The following are mentioned. The active ingredient of the present invention
Eyazole compositionIFor example a shaving cream
It does not need to be used when it is used.
However, if you need the active ingredient,
In order to fully express the effect of adding
The amount of the active ingredient used is 0.01% by weight or more based on the stock solution.
Preferably, there is. In addition, the amount of active ingredient used20weight
%, The compatibility with propellants etc. or
Stability is reduced. As the auxiliary,Was
For example, fragrance, silicone oil, various esters, various
Ketones, thickeners, pH adjusters, solvents, etc.Besides,for example
Alkyl sulfate, polyoxyethylene alkyl ether
Sulphate, N-acylamino acids and salts thereof,
Tiltaurine salt, polyoxyethylene alkyl ether
Acetate, α-olefin sulfonate, alkyl sulfo
Carboxylates, alkyl phosphates, polyoxyethylene
Anionic surfactants such as alkyl ether phosphates
Agent: sorbitan fatty acid ester, glycerin fatty acid ester
Ter, polyoxyethylene sorbitan fatty acid ester
, Polyoxyethylene sorbite fatty acid, polyoxy
Echile Castor oil, polyoxyethylene hydrogenated castor oil,
Polyoxyethylene alkylamine, polyoxyethylene
Fatty acid amide esters, polyoxyethylene glycerides
Fatty acid ester, polyoxyethylene alkyl ether
Nonionic surfactants such as alkyl; alkyl ammonium
Alkyl benzyl ammonium salt, die stearic acid
Cylaminoethylamide, lanolin-derived quaternary ammonium
Cationic surfactants such as sodium salts; caprylic alcohol
Le, lauryl alcohol, myristyl alcohol, cet
10 to 10 carbon atoms such as alcohol and stearyl alcohol
18 higher alcoholsFoam stabilizers and the like. Previous
If the amount of the auxiliary is more than 50% by weight,
The amount of polyhydric alcohol used is reduced, and a sufficient exothermic reaction occurs.
It is usually less than 30% by weight
You.

As the propellant, dimethyl ether is particularly preferably used.

The mixing ratio of the stock solution and the propellant is usually 50 / 50-90 / 10, especially 70/70 (weight ratio).
Adjusted to be 30-80 / 20. When the composition is smaller than the above range, the mist generated by ejecting the aerosol composition I from the aerosol container becomes fine, and when contacting the skin, the cooling sensation becomes too strong and the warm feeling is immediately provided. Will not be. In addition, when it exceeds the above range, the mist generated by ejecting the aerosol composition I from the aerosol container becomes coarse, which tends to cause unevenness, making it difficult to obtain a uniform spray state.

[0020] Incidentally, the (i) Eyazoru composition I which do not form foam in mist, when jetted from Eyazoru container becomes atomized, gives a cooling sensation to the skin, gradually warming sensation Which has the property of giving Therefore, by utilizing this property of the composition I, the composition I can be suitably used for other applications such as an anti-inflammatory analgesic massage oil.

[0021] Eyazoru composition to form a fragile form of the (b) low-foaming II is Ru der made from a stock solution 95 to 99.8 wt% and propellant from 0.2 to 5 wt%.

In one embodiment of the invention, the original solution, the polyvalent alcohol 50% by weight
As described above, 1 to 30% by weight of a foam stabilizer, 20% by weight or less of an active ingredient
And up to 10% by weight of adjuvants.

The amount of the polyhydric alcohol used is 50% by weight.
If less, the exothermic reaction occurs only slightly and does not produce a noticeable warmth. In addition,
In order to form a good foam, the amount of the polyhydric alcohol used is preferably 95% by weight or less. The amount of the polyhydric alcohol used is preferably 60 to 90% by weight.

As the foam stabilizer, the above (a) is used in the form of a mist.
Used in the non-form-forming eyazole composition I
These components may be used alone or in combination of two or more.
Used by mixing the above. In addition, blend higher alcohol
In some cases, it is desirable to use a lower alcohol in combination.
In this case, depending on the carbon number of the higher alcohol,
30 to 3000 parts by weight of low-grade alcohol per 100 parts by weight of coal
It is particularly desirable to use a combination of tools. In addition, among these
Is ethyl alcohol and isopropyl alcohol
Can help solubilize the higher alcohols and
Enables the formulation of active ingredients, and makes it easier to obtain a uniform stock solution.
It is particularly suitable for use. Use of the foam stabilizer
The dose is good when less than 1% by weight.
If it exceeds 30% by weight,
Separation of grade alcohol, solidification of stock solution, increase in foam hardness
Tend to The amount of the foam stabilizer used is preferably
2 to 20% by weight.

The active ingredient is an azole composition of the present invention.
It is appropriately selected and used depending on the use of the product II, and specifically,
The following are mentioned. The active ingredient of the present invention
Eyazole composition II is used, for example, for shaving foam.
It does not need to be used if it is used. Only
If you need active ingredients, add them
In order to fully express the effect expressed by
In addition, the amount used should be 0.01% by weight or more based on the stock solution.
Is preferred. In addition, the amount of active ingredients used is less than 20% by weight.
If there are many, the compatibility and stability with propellants etc. are low
It comes down .

As the auxiliary agent, the above-mentioned (A) in the form of a mist
Used in the non-form-forming eyazole composition I
And the like. 10% by weight of the auxiliary agent
If this is exceeded, a sufficient exothermic reaction is unlikely to occur.
Tend not to give a sense of warmth
Therefore, the content is usually 10% by weight or less.

As the propellant, CO ₂ , N ₂ O or
Is needed use is N _2.

The mixing ratio of the stock solution and the propellant is usually adjusted so that the stock solution / propellant (weight ratio) is 95/5 to 99.8 / 0.2, especially 98/2 to 99.8 / 0.2. If the compounding ratio is smaller than the above range, the internal pressure is low, so that the content is difficult to be jetted.If the compounding ratio is larger than the above range, further compounding becomes difficult due to the properties of the compressed gas. , Liquid properties and pH tend to change.

Examples of the use of the air-soluble composition of the present invention include various ones. Representative examples thereof include, for example, a wiping agent, a therapeutic agent for frost acne, an anti-inflammatory analgesic agent, a keratin softener, an antipruritic agent, and an antifungal agent. Preparations, antihistamines, sunscreens, hormonal agents, vitamins, deodorants, massage creams, cold creams, cleansing creams, hair treatments, packs, depilatory agents, depigmenting agents, shaving creams, and the like.

The active ingredient used in the air-jet composition of the present invention is appropriately selected and used depending on the intended use.

First, the case where the air-jet composition of the present invention is used as a wiping agent will be described.

Most of the conventional wiping agents are in a liquid state, so that they bring a feeling of cooling to the skin and often cause irritation. In particular, considering that diseases such as hemorrhoids worsen in winter, conventional wiping agents that impart a cooling sensation are not preferred. However, when the eazol composition of the present invention is used as a cleansing agent, it not only eliminates the irritation caused by the cooling sensation of the affected area, but also imparts a warm feeling to the skin, so that diseases such as hemorrhoids and wounds can be prevented. The effect of relieving pain and promoting blood circulation by warming, and alleviating local congestion, which is the biggest cause of diseases such as hemorrhoids, is exhibited. In addition, since the polyhydric alcohol has a moisturizing effect, it can be expected to prevent explosion due to drying of the affected part and to alleviate pain during defecation. In addition, when glycerin or the like is used as the polyhydric alcohol, there is an advantage that a topical external application moderating effect is exhibited.

When the eazol composition of the present invention is used as a cleaning agent, the active ingredients include, for example, lidocaine, glycyrrhetinic acid, chlorohexidine hydrochloride, tocopherol acetate, aluminum chlorohydroxy allantoinate, crotamine, allantoin, ephedrine hydrochloride, touki, Sicon, hydrocortisone acetate, fradiomycin sulfate, prednisolone hydrochloride, dl-methylephedrine hydrochloride, hydrocortisone, fradiomycin sulfate, dibucaine hydrochloride, escroside, phenylephrine hydrochloride, diphenhydramine hydrochloride and the like are used. In addition,
These active ingredients may be used alone or in combination of two or more.

The case where the airborne composition of the present invention is used as a therapeutic agent for frostbite will be described.

[0034] Frost swelling (moyage) is a disease caused by poor blood circulation due to contraction of peripheral blood vessels of the limbs. For this reason, agents having a peripheral vasodilatory action, a blood circulation promoting action or a secondary blood circulation promoting action by skin irritation are used as therapeutic agents. In addition, a drug with an antipruritic effect that suppresses pruritus, the most prominent symptom of frost acne, and a drug with a skin tissue activating effect against tissue necrosis due to poor blood flow in the affected area, which is seen in moderate to severe symptoms Is done.

When these drugs are applied to the affected area as an external preparation, it takes a considerable amount of time to penetrate the skin and exert a medicinal effect. For this reason, some patients may apply more than an appropriate amount, and in some cases, may cause other skin diseases such as rash.

In order to solve such a problem, it is considered that a preparation which is applied to an affected area and immediately feels its effect is required.

As described above, the airborne composition of the present invention contains a polyhydric alcohol in an anhydrous state or a state close to the polyalcohol, and absorbs moisture in the upper layer of the skin when applied to the skin. An exothermic reaction occurs, and the heat of the reaction causes a feeling of warmth, and at the same time, dilates the capillaries of the skin, thereby speeding the penetration of the active ingredient into the skin. Further, the reaction heat exhibits a blood circulation promoting action in the affected area, and accordingly, the time required for the active ingredient to reach the local area is shortened.

It should be noted that the propellant contained in the eazazole composition is vaporized when applied to the skin, so that it exhibits a local irritating action and a blood circulation promoting action at that time. Absent.

If these actions are considered as a primary action, the action of the compounded active ingredient will be manifested before the primary action is completed (secondary action), and the synergistic action of the two will result. Fast acting and long lasting action.

When the eazol composition of the present invention is used as a therapeutic agent for frostbite, as active ingredients, for example, tocopherol acetate, pyridoxine dipalmitate, allantoin, retinol palmitate, dl-camphor, l-menthol, eucalyptus oil, Diphenhydramine, pyridoxine hydrochloride, ergocalciferol, panthenol, triclocarban, isopropyl myristate, powdered oak, turmeric powder, sulfadiazine, lidocaine, cortisone acetate, sulfisomidine, sicon extract, diethylstilbestrol, prednisolone, asenyaku, zio, hydrocortisone acetate, Examples thereof include chlorophenylamine maleate, dipotassium glycyrrhizinate, and corn. These components are used alone or in combination of two or more.

The aerosol composition of the present invention is used after being filled in a commonly used aerosol container. When filling, it is important to keep as little excess water as possible. If water is contained, the polyhydric alcohol and water contained in the eazole composition react at that point and do not generate heat when used, so that a sufficient warm feeling cannot be given.

As described above, the aerosol composition of the present invention is excellent in portability since it is used after being filled in an aerosol container. This has the advantage that it is possible to promptly deal with such situations.

Next, the present invention will be described in more detail with reference to Examples, but the present invention is not limited to these Examples.

Example 1 A stock solution comprising the components shown in Table 1 was prepared without containing water. Next, the obtained undiluted solution and the propellant were blended in the proportions shown in Table 1 to obtain an eazole composition.

After 100 g of the obtained aerosol composition was filled in an aerosol container (full volume: 200 ml), a valve was attached, and the discharge condition, warm feeling, feeling of use and overall evaluation were examined according to the following methods. . The results are also shown in Table 1 .

(A) Discharge Condition The aerosol container stored at a low temperature (5 ° C.) or a high temperature (38 ° C.) was shaken well, discharged, and visually observed, and evaluated based on the following evaluation criteria. .

(Evaluation Criteria) ：: Desirable discharge state at both low temperature (5 ° C.) and high temperature (38 ° C.). Δ: Either low temperature (5 ° C.) or high temperature (38 ° C.), slightly insufficient discharge state. ×: Insufficient discharge state at both low temperature (5 ° C.) and high temperature (38 ° C.).

(B) Thermal sensation The contents discharged from the Eyazole product were applied to the back of the hands of 10 male and 10 female panelists in their 30s and evaluated according to the following evaluation criteria.

(Evaluation Criteria) A: More than 18 people felt warmth. B: 13 to 17 people felt warmth. C: 8 to 12 people felt warmth. D: 3 to 7 people felt warmth. E: No more than two people felt warmth.

(C) Feeling of Use A paneler who felt a feeling of warmth was presented with a control product in which half of the total amount of polyhydric alcohol was replaced with water (one having no feeling of warmth), and the texture of each dosage form was determined. The feeling was evaluated.

(Evaluation Criteria) A: More than 80% of the people who felt the warmth felt the texture. B: More than 50% of the people who felt warmth felt the texture. C: 30% or more of the people who felt warmth felt the texture. D: Everyone who felt the feeling of warmth did not feel the texture. E: More than 50% of the people who felt the feeling of warmth evaluated that the texture was poor. -: Not tested

(D) Comprehensive evaluation The discharge condition, warm feeling and feeling of use were evaluated comprehensively based on the following evaluation criteria.

(Evaluation Criteria) A: When there is no problem in the ejection state, the warm feeling is A, and the usability is A or-. B: When there is no problem in the ejection state, the warm feeling is B or more, and the usability is B or more or-. C: When there is no problem in the discharge state, the warm feeling is C or more, and the usability is C or more or-. D: When the ejection is not performed, the warm feeling is D or E, or when the feeling of use is D, E or −.

[0055]

[Table 1]

As is evident from the results shown in Table 1, it can be seen that each of the aerosol compositions of the present invention gives a comfortable warm feeling to the skin.

Example 2 A stock solution comprising the components shown in Table 2 was prepared without containing water. Next, the obtained undiluted solution and the propellant were blended in the proportions shown in Table 2 to obtain an eazole composition.

[0058] 100 g of the obtained aerosol composition was filled in an aerosol container (full volume: 200 ml), a valve was attached, and the physical properties were examined in the same manner as in Example 1. The results are also shown in Table 2 .

[0059]

[Table 2]

As is evident from the results shown in Table 2 , it can be seen that the aerosol composition of the present invention is excellent in warm feeling.

Formulation Examples 1 and 2 The aerosol container of the present invention was filled in an aerosol container in the same manner as in Example 1 except that an active ingredient was added as necessary as shown in Table 3 and a valve was used. Various products were manufactured by mounting.

The physical properties of the air-filled composition filled in the obtained product were examined in the same manner as in Example 1. The result is displayed
Also described in 3 .

[0063]

[Table 3]

As is evident from the results shown in Table 3 , the various products obtained using the inventive azole compositions were:
It can be seen that all of them are excellent in warmth and feeling of use.

[0065]

EFFECTS OF THE INVENTION The aerosol composition of the present invention can be suitably used as an aerosol product which is convenient to carry and gives a feeling of warmth to the skin. For example, it can be suitably used as an eazol product such as a shaving cream, a massage cream, a cold cream, a keratin softener, and an anti-inflammatory analgesic.

──────────────────────────────────────────────────続 き Continued on front page (58) Field surveyed (Int.Cl. ⁷ , DB name) C09K 3/30 A61K 7/00 A61K 9/12

Claims (2)

(57) [Claims] An undiluted solution comprising 50 to 90% by weight of a polyhydric alcohol, 1 to 45% by weight of a lower alcohol, 20% by weight or less of an active ingredient, and 50% by weight or less of an auxiliary agent.
~ 10% by weight, and becomes a mist when squirting.
Without forming the beam, giving a cooling sensation to the skin, gradually multi
Polyhydric alcohol absorbs moisture in the upper layer of the skin, causing an exothermic reaction.
Rue Yazoru composition given hyperthermia feeling stiff. 2. A polyhydric alcohol of 50% by weight or more, a foam stabilizer 1
30 wt%, and the stock solution 95 to 99.8% by weight consisting of the active ingredient 20% by weight and auxiliaries 10 wt% or less, C as propellant
O _2, consists N ₂ O or N ₂ 5-.2% by weight, low-originating
Forms a fragile foam of foam, with polyhydric alcohol peeling
Absorbs moisture in the upper skin layer and generates an exothermic reaction, giving a feeling of warmth
Obtain Eyazoru composition.