JP2003081812A - Aerosol preparation - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a method for enhancing medicinal effects of a topical anesthetic ingredient, an antipruritic ingredient, an antihistaminic ingredient or an antiphlogistic ingredient contained in a chemical fluid in an aerosol preparation composed of the chemical fluid and a propellant, a composition for enhancing the medicinal effects and the aerosol preparation having the enhanced medicinal effects. SOLUTION: This aerosol preparation is prepared as follows. (A) At least one kind of active ingredient selected from the group consisting of the topical anesthetic ingredient, the antipruritic ingredient, the antihistaminic ingredient and the antiphlogistic ingredient, (B) at least one kind selected from the group consisting of urea, glycyrrhizic acid, a salt of the glycyrrhizic acid, a derivative of the glycyrrhizic acid, glycyrrhetic acid, a salt of the glycyrrhetic acid and a derivative of the glycyrrhetic acid, allantoin and a derivative of the allantoin, (C) an essential oil ingredient and (D) the propellant.

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to an aerosol preparation having an enhanced drug efficacy, a composition for enhancing the drug efficacy, and a method for enhancing the drug efficacy of an active ingredient in the aerosol formulation.

[0002]

2. Description of the Related Art Aerosol preparations are external preparations which contain a drug solution and a propellant as a content and can give a cooling sensation to the skin by the action of the propellant which is vaporized when sprayed onto the skin. The cooling action of such an aerosol formulation is widely used for the development of a formulation for the purpose of antipruritic, antiphlogistic, analgesic, etc., because itching can immediately suppress skin itch, inflammation or pain. Specifically, for example, JP-A-11-228398 and JP-A-11-22839.
No. 9 discloses an aerosol preparation containing crotamiton (an antipruritic ingredient), lidocaine (a local anesthetic ingredient), and diphenhydramine (an antihistamine ingredient) and glycerin or squalane as an active ingredient. It is described that an immediate antipruritic effect can be achieved by a synergistic action of the synergistic action of the active ingredient and the cooling action by the heat of vaporization of the propellant.

However, the propellant contained in the aerosol formulation has the above-mentioned advantage on the other hand, since the skin temperature is instantly lowered by vaporization of the liquefied gas immediately after the spraying. There are also problems that the penetration into the skin is inhibited and that the effects of the active ingredient are not sufficiently exerted due to the delay of blood flow and fluidity of tissue fluid.

[0004] Further, aerosol preparations, which are aqueous, have a drug absorbability immediately after application to the skin (immediate effect) as compared with creams and patches, as is generally seen in liquid preparations (especially aqueous preparations). However, there is a problem that it is inferior in sustainability.

Specifically, in the case of an antipruritic aerosol preparation containing an antipruritic component such as crotamiton, an antihistamine component or a local anesthetic component, the skin penetrability is lowered and the blood flow is lowered by the cooling action of the spray. Therefore, it takes time for the pruritic sensation to be removed due to the onset of the drug effect, and thus the patient may scratch the affected area by then. In addition, since the antihistamine component is a slow-acting component that exerts its effect after being transferred into the blood, the decrease in blood flow due to the cooling action further delays the expression of the antipruritic action of the antihistamine component.

Thus, there is a demand for an aerosol preparation capable of sufficiently exerting the desired effect of the active ingredient. However, while maintaining the cooling effect which is an excellent characteristic of the aerosol preparation,
The reality is that there is no aerosol formulation having such an effect.

[0007]

SUMMARY OF THE INVENTION An object of the present invention is to solve such conventional problems. That is, an object of the present invention is to provide an aerosol preparation having an enhanced drug effect so that the drug effect of the active ingredient does not decrease even when the aerosol drug is sprayed and used. Further, the present invention aims to provide a composition useful for enhancing the drug efficacy of an active ingredient in an aerosol formulation. Still another object of the present invention is to provide a method useful for enhancing the drug efficacy of an active ingredient in an aerosol formulation.

[0008]

[Means for Solving the Problems] In the process of intensive studies day and night in order to solve the above problems, the present inventors have found that at least one of a local anesthetic ingredient, an antipruritic ingredient, an antihistamine ingredient, or an antiphlogistic ingredient. As an active ingredient, further urea, glycyrrhizic acid, a salt of glycyrrhizic acid, a derivative of glycyrrhizic acid, glycyrrhetinic acid, a salt of glycyrrhetinic acid, a derivative of glycyrrhetinic acid, at least one of allantoin or a derivative of allantoin, an essential oil component, and a propellant. It has been found that an aerosol preparation prepared by blending the above-mentioned drug exhibits a strong drug effect promptly and is more durable than the case where the active ingredient itself is sprayed and used. The present invention was developed based on such knowledge.

That is, the present invention is an aerosol preparation listed in (1) or (2) below, and an aerosol product containing the preparation as a content: (1) A) a local anesthetic ingredient, an antipruritic ingredient, an antihistamine ingredient and At least one active ingredient selected from the group consisting of anti-inflammatory components, B) urea, glycyrrhizinic acid, a salt of glycyrrhizinic acid, a derivative of glycyrrhizinic acid, glycyrrhetinic acid, a salt of glycyrrhetinic acid, a derivative of glycyrrhetinic acid, allantoin and allantoin An aerosol formulation containing at least one selected from the group consisting of derivatives, C) an essential oil component, and D) a propellant. (2) The active ingredients are lidocaine, dibucaine, amino acid ethyl benzoate, crotamiton, ictamol, moctamol, thymol acid, chlorpheniramine, diphenhydramine, isothibenzyl, guaiazulene, bufexamac, dexamethasone, hydrocortisone, prednisolone, salts thereof, and these salts. The aerosol preparation according to (1), which is at least one selected from the group consisting of derivatives. (3) An aerosol product obtained by filling the aerosol container with the aerosol preparation described in (1) or (2) above.

The present invention also relates to a composition for enhancing the drug efficacy of an active ingredient in an aerosol preparation, which is listed in the following (4) or (5): (4) Local anesthetic ingredient, antipruritic ingredient, anti-antifungal ingredient in the aerosol preparation A composition for enhancing the efficacy of at least one active ingredient selected from the group consisting of a histamine component and an anti-inflammatory component, which comprises B) urea, glycyrrhizinic acid, a salt of glycyrrhizinic acid, a derivative of glycyrrhizinic acid, glycyrrhetinic acid, and glycyrrhetin. A composition comprising an acid salt, a derivative of glycyrrhetinic acid, at least one selected from the group consisting of allantoin and a derivative of allantoin, and C) an essential oil component. (5) The active ingredient is lidocaine, dibucaine, amino acid ethyl benzoate, crotamiton, ictamol, moctamol, thymol acid, chlorpheniramine, diphenhydramine, isothibenzyl, guaiazulene, bufexamac, dexamethasone, hydrocortisone, prednisolone, salts thereof, and these. The composition according to (3), which is at least one selected from the group consisting of derivatives.

The present invention is also a method for enhancing the efficacy of an active ingredient in an aerosol formulation, which is listed in (6) or (7) below: (6) A) Local anesthetic ingredient, antipruritic ingredient, antihistamine ingredient And at least one active ingredient selected from the group consisting of an anti-inflammatory component, B) urea, glycyrrhizic acid, a salt of glycyrrhizic acid, a derivative of glycyrrhizic acid, a salt of glycyrrhetinic acid, a salt of glycyrrhetinic acid, a derivative of glycyrrhetinic acid, A method for enhancing the efficacy of an active ingredient in an aerosol formulation, which comprises blending at least one selected from the group consisting of allantoin and a derivative of allantoin and an essential oil component C). (7) The active ingredients are lidocaine, dibucaine, amino acid ethyl benzoate, crotamiton, ictamol, moctamol, thymolic acid, chlorpheniramine, diphenhydramine, isothibenzyl, guaiazulene, bufexamac, dexamethasone, hydrocortisone, prednisolone, salts thereof, and these. The method for enhancing the efficacy of an active ingredient in an aerosol preparation according to (5), which is at least one selected from the group consisting of derivatives.

In the present specification, the term "medicine solution" means
It means a composition consisting of all the components other than the propellant component, which are incorporated into the aerosol formulation.

[0013]

BEST MODE FOR CARRYING OUT THE INVENTION (1) Aerosol preparation The aerosol preparation of the present invention comprises A) at least one active ingredient selected from the group consisting of a local anesthetic component, an antipruritic component, an antihistamine component and an anti-inflammatory component, B). Urea, glycyrrhizic acid, a salt of glycyrrhizic acid, a derivative of glycyrrhizic acid, glycyrrhetinic acid, a salt of glycyrrhetinic acid, a derivative of glycyrrhetinic acid, at least one selected from the group consisting of allantoin and a derivative of allantoin,
C) containing an essential oil component and D) a propellant,
As a result, the desired medicinal effect of the above-mentioned active ingredient can be sufficiently exerted during spraying regardless of the cooling action of the propellant. That is, in the present invention, at least one selected from the group consisting of B) urea, glycyrrhizic acid, a salt of glycyrrhizic acid, a derivative of glycyrrhizic acid, glycyrrhetinic acid, a salt of glycyrrhetinic acid, a derivative of glycyrrhetinic acid, allantoin and an allantoin derivative. , And C) a composition containing an essential oil component plays a role of a drug efficacy-enhancing component of an active ingredient in an aerosol preparation.

A) the aerosol formulation of the present invention is intended
The active ingredient is a local anesthetic ingredient, an antipruritic ingredient, an antihistamine ingredient or an anti-inflammatory ingredient. B) to these A) active ingredients
By using the component and the component C) together, the drug effect of the active ingredient can be enhanced when the aerosol formulation is sprayed and used, as compared with the case where these components are not used together.

Here, the local anesthetic component may be one that is usually used as a component of an external preparation, and specific examples thereof include lidocaine, dibucaine, the amino acid ethyl benzoate or derivatives thereof. These may be salts as long as they are pharmaceutically acceptable.
Specific examples of the salt include acid addition salts such as dibucaine hydrochloride. Further, these may be used alone or in any combination of two or more. Preferred are lidocaine (including salt) and dibucaine (including salt). The local anesthetic component is not limited, but each component is 0.0% in 100% by weight of the drug solution.
It is desirable that the compounding amount be 1 to 10% by weight, preferably 0.1 to 10% by weight, and more preferably 0.1 to 8% by weight. In addition, the compounding amount of the local anesthetic component with respect to the aerosol formulation is such that each component in the aerosol formulation is, for example, 0.003 to 7 mg / ml, preferably 0.03 to 7 mg / ml, and more preferably 0.3.
A range of up to 6.5 mg / ml can be mentioned.

The antipruritic component is not particularly limited as long as it is a component that can be added to the external preparation for the purpose of antipruritic, and specific examples thereof include crotamiton, ictamol, moctamol or thymolic acid or derivatives thereof. . These may be salts as long as they are pharmaceutically acceptable. Further, these may be used alone or in any combination of two or more. In pruritus caused by drying, destruction and damage of the keratin barrier layer of the skin are observed, and crotamiton is preferred as such an antipruritic component particularly effective for the skin.
The antipruritic ingredient is not limited, but the drug solution is 100% by weight.
0.1 to 15% by weight of each component, preferably 1
It is desirable to blend in a proportion of from 10 to 10% by weight, more preferably from 1 to 7.5% by weight. The amount of the antipruritic component to be added to the aerosol preparation is, for example, 0.03 to 11 mg / ml, preferably 0.3 to 7 mg / ml, and more preferably 0.3 to 11 mg of each component in the aerosol preparation.
An example is a range of 5 mg / ml.

The antihistamine component may be one normally used as a component of an external preparation, and specific examples thereof include chlorpheniramine, diphenhydramine, isothibenzyl, and derivatives thereof. These may be salts as long as they are pharmaceutically acceptable. Examples of the salt include acid addition salts such as chlorpheniramine maleate and diphenhydramine hydrochloride. Further, these may be used alone or in any combination of two or more.
The antihistamine component may be, but is not limited to, drug solution 10
0 to 10% by weight of each component is 0.01 to 10% by weight, preferably 0.05 to 10% by weight, more preferably 0.1 to 10% by weight.
It is desirable to mix it in a ratio of 5% by weight. Further, the compounding amount of the antihistamine component with respect to the aerosol preparation is such that each component in the aerosol preparation is, for example, 0.00
3 to 7 mg / ml, preferably 0.01 to 7 mg / m
1, more preferably 0.03 to 6.5 mg / ml.

The anti-inflammatory component may be any one which is usually used as a component of an external preparation, and specific examples thereof include guaiazulene, bufexamac, dexamethasone, hydrocortisone and prednisolone. Preferred are guaiazulene and bufexamac. These are limited to being pharmaceutically acceptable,
These derivatives or salts may be used. In particular,
Sodium guaiazulene sulfonate as an anti-inflammatory component,
Dexamethasone metasulfobenzoate, sodium dexamethasone phosphate, dexamethasone acetate, dexamethasone sodium metasulfobenzoate, dexamethasone valerate, dexamethasone propionate, hydrocortisone acetate, hydrocortisone sodium succinate, hydrocortisone phosphate sodium, hydrocortisone butyrate propionate hydrocortisone butyrate, butionate cortisone propionate butyrate Prednisolone sodium succinate, prednisolone sodium phosphate, prednisolone valerate acetate, prednisolone fernesylate and the like can be used. Also,
These may be used alone or in any combination of two or more. The anti-inflammatory component is
Although not limited, each component in 100% by weight of the chemical solution is 0.001 to 20% by weight, 0.01 to 20% by weight, preferably 0.001 to 15% by weight, 0.01 to 15% by weight,
It is desirable to add 0.01 to 10% by weight, 0.02 to 5% by weight, more preferably 0.1 to 10% by weight, and particularly preferably 0.1 to 5% by weight. Further, the compounding amount of the anti-inflammatory component with respect to the aerosol preparation is, for example, 0.003 to 15 mg /
ml, preferably 0.003 to 11 mg / ml, and more preferably 0.03 to 4 mg / ml. Further, each of these active ingredients may be used alone or in any combination of two or more. When two or more types are used in combination,
As a combination aspect, a combination of a local anesthetic component and an antipruritic component, a combination of a local anesthetic component and an antihistamine component, a combination of a local anesthetic component and an anti-inflammatory component, a combination of an antipruritic component and an antihistamine component, an antipruritic component and Examples thereof include a combined use of an anti-inflammatory component and a combined use of an antihistamine component and an anti-inflammatory component. From the viewpoint of enhancing the antipruritic effect, it is preferably a combined use of an antipruritic component and an antihistamine component, particularly a combined use of crotamiton and an antihistamine component.

In the aerosol preparation of the present invention, as component B), urea, glycyrrhizic acid, a salt of glycyrrhizic acid, a derivative of glycyrrhizic acid, glycyrrhetinic acid, a salt of glycyrrhetinic acid, a derivative of glycyrrhetinic acid, and allantoin and allantoin derivatives are used. Contained.

The glycyrrhizic acid salt is not particularly limited as long as it is pharmacologically acceptable, and examples thereof include alkali metal salts such as sodium and potassium and ammonium salts. Specifically, disodium glycyrrhizinate, trisodium glycyrrhizinate,
Examples thereof include dipotassium glycyrrhizinate or tripotassium glycyrrhizinate, and ammonium salts such as monoammonium glycyrrhizinate. Preferred salts of glycyrrhizinate include dipotassium glycyrrhizinate and monoammonium glycyrrhizinate.

The derivative of glycyrrhizinate is not particularly limited as long as it is a pharmacologically acceptable derivative of glycyrrhizinate, and specifically, methyl glycyrrhizinate,
Examples include stearyl glycyrrhizinate and nitric acid or acetic acid ester of glycyrrhizinate. Stearyl glycyrrhizinate is preferred. The glycyrrhizic acid derivative as used in the present invention also includes pharmaceutically acceptable salts thereof. Examples of such salts include alkali metal salts such as sodium and potassium, and ammonium salts.

The glycyrrhetinic acid salt is not particularly limited as long as it is pharmacologically acceptable, and examples thereof include alkali metal salts such as sodium and potassium, and ammonium salts. Specific examples thereof include alkali metal salts such as disodium glycyrrhetinate, trisodium glycyrrhetinate, dipotassium glycyrrhetinate, and tripotassium glycyrrhetinate, and ammonium salts such as monoammonium glycyrrhetinate.

The derivative of glycyrrhetinic acid is not particularly limited as long as it is a pharmacologically acceptable derivative of glycyrrhetinic acid, and specifically, stearyl glycyrrhetinic acid, pyridoxine glycyrrhetinic acid, glyceryl glycyrrhetinic acid, nitric acid or acetic acid of glycyrrhetinic acid. An ester can be illustrated. Stearyl glycyrrhetinate is preferred. The glycyrrhetinic acid derivative also includes pharmaceutically acceptable salts thereof. Examples of the salt include alkali metal salts such as sodium and potassium and ammonium salts.

The allantoin derivative is not particularly limited as long as it is pharmacologically acceptable, and specific examples thereof include allantoin glycyrrhetin, allantoin chlorhydroxyaluminum, and allantoin hydroxyaluminum.

Component B) [Urea; glycyrrhizic acid, glycyrrhizic acid salt, glycyrrhizic acid derivative, glycyrrhetinic acid, glycyrrhetinic acid salt, glycyrrhetinic acid derivative (hereinafter collectively referred to simply as "glycyrrhizic acid, etc." Allantoin and derivatives of allantoin (hereinafter also collectively referred to simply as “alantoin etc.”)] may be used alone or in any combination of two or more. You can also The combination aspect is not particularly limited,
For example, a combination of urea and allantoin, urea and glycyrrhizinic acid, glycyrrhizinic acid and allantoin and the like can be mentioned.

The proportion of component B) is 100% by weight of the chemical solution.
0.01-35 as the total amount of each group of components belonging to each group (urea, glycyrrhizinic acid, etc., and allantoin, etc.)
The content is appropriately selected so as to be contained in a weight ratio of preferably 0.1 to 30% by weight, more preferably 0.5 to 25% by weight, and 0.3 to 20% by weight. Specifically, when urea is used as the component B), 0.1 to 100% by weight of the chemical solution is used.
35% by weight, preferably 1 to 30% by weight, more preferably 3 to 25% by weight; when glycyrrhizic acid or the like is used, the total amount of these is 0.01% in 100% by weight of the drug solution.
-15% by weight, 0.01-5% by weight, preferably 0.1-
10% by weight, 0.1-5% by weight, 0.1-3% by weight, more preferably 0.5-5% by weight, 0.5-2% by weight, 0.2
~ 2% by weight; when using allantoin, etc., the chemical solution 10
0.01-5 wt% as a total amount of these in 0 wt%,
Preferably 0.1 to 3% by weight, more preferably 0.5 to 2
It can be blended in a ratio of wt%, 0.2-2 wt%.

The amount of component (B) to be added to the aerosol preparation is, for example, 0.003 in the aerosol preparation.
~ 24.5 mg / ml, preferably 0.003-10.
5 mg / ml, more preferably 0.007-10.5 m
An example is a range of g / ml. Specifically, when urea is used as the component B), 0.03 to 74.5 mg / ml, preferably 0.
07-24.5 mg / ml, more preferably 0.3-2
1 mg / ml; when using glycyrrhizic acid or the like, the total amount of these in the aerosol preparation is 0.003 to 10
mg / ml, preferably 0.003 to 7 mg / ml, more preferably 0.05 to 6 mg / ml; when using allantoin etc., 0.003 to 10 mg / ml as the total amount thereof in the aerosol preparation, preferably 0.03-
7 mg / ml, more preferably 0.05-6 mg / ml
Can be blended in the ratio.

The essential oil component to be blended as the component C) is not limited, but camphor, menthol, borneol, eugenol, cineol, thymol, bisabolol, α-pinene, or limonene can be exemplified. It is preferably camphor or menthol, more preferably menthol. The essential oil component may be of natural origin or synthetic origin, which is prepared by isolation from essential oil. Further, in the present invention, an essential oil containing the above essential oil component can be used as the component C). Such essential oils include eucalyptus oil, peppermint oil, clove oil, cinnamon oil, peppermint oil, mint oil, tea tree oil, chamomile oil, rosemary oil, lemon oil, orange oil,
Examples include thyme oil, sage oil, clove oil, and the like. Eucalyptus oil, peppermint oil or tea tree oil is preferable, and eucalyptus oil or peppermint oil is more preferable. These essential oil components may be used alone or in any combination of two or more.

The blending ratio of the essential oil component in the total amount of the chemical solution is, for example, in the range of 0.001 to 25% by weight. Specifically, the total amount of essential oil components is usually 0.00
It is 1 to 10% by weight, preferably 0.01 to 5% by weight.

The amount of the essential oil component in the aerosol preparation is 0.0003 to 7 mg / ml, preferably 0.003 as the total amount of the essential oil component in the aerosol preparation.
A range of 3 to 4 mg / ml can be mentioned.

In the present invention, the above-mentioned component B) and component C) are combined and blended with component A) to obtain an aerosol preparation having enhanced drug efficacy.

The blending ratio of the B) component and the C) component is a weight ratio (B component: C component), preferably from 1000: 1.
1: 500, 600: 1 to 1: 500, 500: 1 to
1: 500, 300: 1 to 1:50, more preferably 2
50: 1 to 1:50, 200: 1 to 1:10, particularly preferably 50: 1 to 1:10, 50: 1 to 1: 5.
Specifically, when the component B) is urea, 1000: 1 to
1: 500, 600: 1 to 1: 100, preferably 50
0: 1 to 1: 100, and more preferably 300: 1 to 1:
50, and when the component B) is other than urea, 1000: 1
˜1: 500, preferably 500: 1 to 1: 100,1
00: 1 to 1: 100, 100: 1 to 1:50, and more preferably 20: 1 to 1:50.

The D) propellant used in the present invention includes
It may be any that does not adversely affect the chemical liquid such as decomposition or deterioration, and specifically, liquefied petroleum gas (e.g., gas such as ethane, propane, ethylene, isobutane, normal butane, propylene, etc. that easily liquefy, Mixed gas [eg, mixed gas of isobutane and propane, mixed gas of propane and butane], ether propellant (dimethyl ether, etc.), fluorocarbon (eg, fluorocarbon,
Examples thereof include chlorofluorocarbon, bromochlorofluorocarbon), compressed gas (carbon dioxide, nitrogen, air, or mixed gas thereof), or freon gas (monochlorodifluoroethane, tetrafluoroethane, etc.). In addition, these propellants may be used alone or in any combination of two or more. Dimethyl ether or liquefied petroleum gas is preferable, and dimethyl ether or a mixed gas of dimethyl ether and liquefied petroleum gas is particularly preferable because it has excellent feeling in use including cooling feeling.

The aerosol preparation of the present invention may contain at least the above-mentioned components A) to D) as essential components, but other medicinal components are blended as long as the effects of the present invention are not impaired. There are no restrictions.

Examples of such medicinal components include external agents (cosmetics, external medicines) such as wound healing agents, antiphlogistic and analgesics, bactericidal and disinfectants, moisturizers, keratin softeners, acne treatment agents, armpit odor prevention agents, athlete's foot remedy agents and the like. , Quasi drugs for external use) can be used. Preferably, an ingredient having an effect of enhancing the drug efficacy of the active ingredient of the aerosol preparation of the present invention is desirable. Specifically, a vitamin component, a moisturizing component, a local paralytic component, a steroid, an animal and plant extract, an anti-inflammatory component, an antibacterial component, etc. can be illustrated. In addition, these 1 type or 2 types or more can be used in combination.

The vitamin component is preferably an NMF component or one having an effect of recovering damage to the skin or suppressing inflammation, such as vitamin E or its derivative such as tocopherol, vitamin B6 and its derivative such as pyridoxine, retinol and the like. Examples thereof include vitamin A or its derivative, vitamin C or its derivative such as ascorbic acid, pantothenic acid or its derivative, biotin and the like.

The moisturizing component is not particularly limited as long as it can be blended in the external preparation for the purpose of moisturizing (water retention), and specifically, squalane, liquid paraffin, avocado oil, soybean oil, castor oil, Examples thereof include liquid oils such as rice germ oil; amino acids such as glycine, alanine and aspartic acid; sugars such as sorbitol, maltitol, trehalose and glucose; organic acids such as lactic acid and pyrrolidonecarboxylic acid. These may be used alone or in any combination of two or more.

Examples of the local paralytic component include capsicum, mustard, cantharis, cantharidin, capsaicin and the like. These may be used alone or in any combination of two or more.

As the steroid, any one which is usually used as a component of an external preparation may be used, and specific examples thereof include hydrocortisone, dexamethasone, prednisolone and derivatives thereof. These may be used alone or in any combination of two or more.

As the animal and plant extract, those which are said to have a moisturizing action, an anti-inflammatory action, or a rough skin improving action are preferable, and specific examples thereof include keratins, collagens,
Hyaluronic acid, chondroitin sulphate, aloe extract, hamamelis extract, rosemary extract, horse chestnut extract, cucumber extract, quince extract, royal jelly extract, seaweed extract, tea extract, carrot extract, peach extract Substance, peach leaf extract, licorice extract, sardine extract, eucalyptus extract, peppermint extract, lavender extract, evening primrose extract, chamomile extract, Japanese laurel extract, rice fermented extract and the like. These may be used alone or in any combination of two or more.

The analgesic component may be any one which is usually used as a component of an external preparation, and specifically, salicylic acid or a derivative thereof (eg, methyl salicylate, salicylic acid monoglycol ester, etc.), indomethacin, ketoprofen, flurubi. Examples include profen, piroxicam, diclofenac, ibuprofen, mefenamic acid. These may be used alone or in any combination of two or more.

As the antibacterial component, undecylenic acid, pentachlorophenol, clotrimazole, tolnaftate, tricomycin, miconazole, potassium iodide, chlorhexidine, acrinol, benzalkonium, penicillin, tetracycline, sulconazole,
Examples include isopropylmethylphenol, fradiomycin, kanamycin, econazole, oxyconazole, bifonazole, thioconazole, tolcyclate, ciclopirox olamine, exalamide, siccanin, pyrrolenitrin or derivatives thereof. In addition, these may be salts (for example, acid addition salts such as chlorhexidine gluconate and miconazole nitrate) as long as they are pharmaceutically acceptable. These may be used alone or in any combination of two or more.

Further, the aerosol preparation of the present invention may be blended with a component such as a lower alcohol or a polyhydric alcohol, which contributes to the improvement of the feeling of use of the aerosol preparation, as long as the effect of the present invention is not impaired. it can.

Examples of the lower alcohol here include:
Examples thereof include linear or branched alcohols having 1 to 6 carbon atoms such as ethanol, propanol, isopropanol and butanol. Among them, ethanol or isopropanol is preferable from the viewpoint of formulation stability of the components. These lower alcohols may be used alone or in any combination of two or more.

The lower alcohol is useful for compensating for the reduction in the cooling feeling of the skin when the aerosol formulation is sprayed due to the reduction of the amount of the propellant, and for giving the skin a cooling feeling or a refreshing feeling when spraying. Further, the addition of lower alcohol is effective in increasing the stability of various components to be added to the drug solution. Particularly in the aerosol preparation of the present invention, a proper cooling sensation and its sustaining effect can be obtained by using a propellant and a lower alcohol in combination.

When lower alcohols are blended for the purpose of obtaining such effects, the total amount of the lower alcohols in 100% by weight of the chemical solution is 0.1% by weight or more, preferably 1% by weight or more, more preferably 5% by weight or more. It is preferable to use it in a ratio of. Further, the compounding amount (total amount) of the lower alcohol in the aerosol preparation is 0.03 mg / ml or more, preferably 0.3 mg / ml or more, and more preferably 0.7 mg / ml or more. It should be noted that the lower alcohol is mixed to obtain a cooling effect by dissipating the heat of vaporization, but at the same time, it tends to deprive sebum of the skin and cause the skin to dry. It is preferable to add 50% by weight, preferably 40% by weight, as an upper limit. In addition, the upper limit of the amount of lower alcohol blended in the aerosol preparation is 35 mg / ml, preferably 30 mg / ml.
Can be mentioned.

Specific examples of the polyhydric alcohol include propylene glycol, 1,3-butylene glycol, glycerin, diethylene glycol, triethylene glycol, dipropylene glycol, hexylene glycol,
Examples thereof include polyethylene glycol and ethoxydiglycol. These polyhydric alcohols may be used alone or in any combination of two or more. Preferably, from the viewpoint of safety and moisturizing effect, dipropylene glycol, polyethylene glycol, ethoxydiglycol, propylene glycol, 1,
3-butylene glycol or glycerin.

Since the polyhydric alcohol is effective in alleviating the cooling sensation caused by the dissipation of the heat of vaporization and protecting the skin from the dryness caused by degreasing, it is used in combination with the above lower alcohols. Is preferred.

When a polyhydric alcohol is blended, the chemical solution 1
The total amount of these in 0.1% by weight is 0.1 to 50% by weight, preferably 0.1 to 40% by weight, more preferably 1
It can be used in a proportion of up to 30% by weight. In addition, the compounding amount (total amount) of the polyhydric alcohol to the aerosol preparation is 0.03 to 35 mg / m in the aerosol preparation.
1, preferably 0.03 to 30 mg / ml, and more preferably 0.3 to 22 mg / ml.

Further, the aerosol preparation of the present invention may contain a solubilizing agent, a surfactant, a chelating agent, a pH, if necessary.
Various additives such as a regulator, an antiseptic, an antioxidant and a fragrance may be blended.

As the solubilizing agent, diisopropyl adipate, isopropyl myristate, 1,3-butylene glycol, propylene glycol, polyethylene glycol, glycerin, lactic acid, sodium hydroxide and the like; as the surfactant, polyoxyethylene sorbitan fatty acid Ester, sorbitan fatty acid ester, polyoxyethylene hydrogenated castor oil, polyoxyethylene polyoxypropylene alkyl ether, polyoxyethylene cetyl ether, glyceryl monostearate, etc .; as chelating agents, edetic acids, hydroxyethanediphosphonic acids,
Phytic acid, etc .; as preservatives, paraben, benzoate,
Isopropylmethylphenol and the like; examples of the antioxidant include tocopherol acetate, dibutylhydroxytoluene, butylhydroxytoluene and the like.

Each of the specific ingredients listed in the present specification is a pharmaceutically acceptable salt of the ingredient, particularly a pharmaceutically acceptable salt of the ingredient which is usually used in the art for the purpose of external application. Salt is also meant to be comprehensive.

The aerosol preparation of the present invention can be manufactured by a known method. For example, it is manufactured by mixing the above-mentioned various components to prepare a drug solution, and mixing the drug solution and D) a propellant.

Here, the drug solution is usually prepared by mixing the above-mentioned various components with water. Water is a suitable carrier for aerosol preparations because it is safe and has a good feeling in use. The proportion of water contained in 100% by weight of the drug solution is usually 10 to 99.8% by weight, preferably 10 to 75% by weight, more preferably 15 to 60% by weight, and particularly preferably 25 to 50% by weight.

The drug solution generally has a liquidity of pH 2 to 10, but preferably has a pH of 3 to 9, and more preferably a pH of 5 to 8 from the viewpoint of low irritation to the skin and good feel on the skin. It is preferably weakly acidic to weakly alkaline.

Further, if the viscosity of the liquid medicine is less than 0.5 cSt, the skin adhesiveness of the aerosol formulation is lowered and the viscosity is 20%.
If it exceeds cSt, the skin tends to remain sticky. Therefore, from the viewpoint of obtaining a good feeling in use, it is desirable to adjust the viscosity of the drug solution to a range of usually 1 cSt to 20 cSt. The viscosity here means the kinematic viscosity measured by a BL viscometer (using a BL adapter, rotation speed 30 rpm, measuring temperature 29 ° C., density measurement: using pycnometer). It is preferably 1 cSt to 10 cSt, more preferably 1 cSt to 5 cSt.

In the present invention, the aerosol preparation is a preparation in which the active ingredient is prepared in the form of finely dispersed mist, foam or semi-solid by utilizing the pressure of the propellant, and the content filled in the aerosol container is That is, it refers to a mixture of a chemical solution and a propellant. Further, the aerosol preparation of the present invention is a preparation in a dosage form for topical administration to the skin or mucous membranes.

The mixing ratio of the liquid medicine and the propellant in the aerosol preparation of the present invention is, based on the volume, liquid medicine: propellant = 10: 90-9.
It is preferably 0:10 (volume ratio). More preferably, the chemical liquid: propellant = 25: 75 to 90:10.
Here, the volume of the aerosol preparation corresponds to the inner volume of the container filled with the aerosol preparation, and the volume of the propellant means the volume obtained by subtracting the volume of the drug solution from the inner volume of the container.

If the proportion of the drug solution in the aerosol preparation is less than 10% by volume, the stability of the components tends not to be sufficiently maintained, while if the proportion of the propellant is less than 10% by volume,
When applied to the skin, sufficient cooling effect and good feeling of use cannot be obtained.

The aerosol preparation of the present invention is provided and used as an aerosol product by filling an aerosol container having a valve, a button and the like by a known method.

The aerosol container used for the aerosol product can be made of aluminum, stainless steel, metal such as tin plate, glass or plastic as a material.
An epoxy resin coating or a plastic coating may be applied to reinforce or improve pressure resistance, impact resistance, corrosion resistance, and formulation stability. The aerosol product can be manufactured by filling the aerosol container with the aerosol preparation by a known method. Examples of the filling method include a cooling filling method, a pressure filling method and an under cup filling method. Further, as long as the effect of the present invention is not impaired, not only the composition of the chemical solution, but also the injection amount or spraying / injection state of the content, the pressure in the aerosol container, the injection hole diameter in the valve of the aerosol container or the diameter of the stem passage, etc. Can be appropriately selected and used according to the purpose.

The aerosol preparation of the present invention can be used as an external preparation belonging to various fields of cosmetics, external medicines or quasi-drugs having various uses depending on the efficacy of the active ingredient to be mixed. As an example, an aerosol formulation containing a local anesthetic component, an antipruritic component, an antihistamine component or an antiphlogistic component as an active ingredient in a drug solution is atopic dermatitis, senile xerosis, and itching such as xerosis of dialysis patients. It may be applied to diseased skin accompanied by itching, dry skin accompanied by itch (xeroderma of old people / adults, dry skin of children) and skin after sunburn. In addition, as an active ingredient in the drug solution, a local anesthetic ingredient, an antipruritic ingredient,
An aerosol preparation containing an antihistamine component or an anti-inflammatory component can be applied to athlete's foot, fungus worm, zebra worm, etc. Furthermore, an aerosol formulation containing a local anesthetic component, an antihistamine component, an antipruritic component or an anti-inflammatory component as an active ingredient in a liquid medicine can be applied to a cutaneous wound surface such as a scratch, a scar, a scratch, a shoe shift. .

Thus, the aerosol preparation of the present invention comprises an antipruritic agent, a wound healing agent, an antiphlogistic analgesic agent, an antiphlogistic agent, a bactericide, a disinfectant, a moisturizing agent, a keratin softener, an acne treatment agent, an axillary odor prevention or treatment agent. , Deodorant for armpits and feet, athlete's foot remedy, local anesthetic,
It can be used as an external preparation such as a protective film agent.

(2) Composition for enhancing drug efficacy of active ingredient of aerosol preparation Furthermore, the present invention provides at least one selected from the group consisting of a local anesthetic ingredient, an antipruritic ingredient, an antihistamine ingredient and an antiphlogistic ingredient to be incorporated in the aerosol preparation. There is provided a composition (composition for potentiating drug effect) used for enhancing the drug effect of the active ingredient.

Such a composition comprises the above-mentioned component B): urea, glycyrrhizic acid, a salt of glycyrrhizic acid, a derivative of glycyrrhizic acid, glycyrrhetinic acid, a salt of glycyrrhetinic acid, a derivative of glycyrrhetinic acid, an allantoin and an allantoin derivative. It contains at least one selected and the above-mentioned component C: essential oil component.

Specific examples of the above-mentioned active ingredients to be enhanced in drug efficacy, and specific examples of the above-mentioned components B) and C) and their compounding ratios are as described above. The effect-enhancing composition of the present invention can obtain its effect when used in combination with an active ingredient in an aerosol preparation. Specifically, when a drug solution of an aerosol preparation is prepared, by adding a composition for enhancing a drug effect containing B) component and C) component in addition to the above-mentioned active ingredient, the drug effect of the active ingredient expressed in the aerosol formulation is improved. Can be enhanced. Here, the compounding ratio of the drug efficacy-enhancing composition of the present invention with respect to the component A) varies depending on the type of the component A), the type of the drug-efficiency enhancing composition of the present invention, the expected effect, etc., and should be specified uniformly. However, for example, the total amount of the components B) and C) is 0.2 with respect to 100 parts by weight of the component A).
~ 30000 parts by weight, 0.2 to 2000 parts by weight, preferably 1 to 20000 parts by weight, 0.3 to 1000 parts by weight,
More preferably 2 to 10000 parts by weight, 0.5 to 20
An example is a range of 0 parts by weight.

(3) Method for enhancing drug efficacy of active ingredient of aerosol preparation From another aspect of the present invention, in a drug solution of an aerosol preparation,
In an aerosol preparation, by combining B) component and C) component in combination with A) at least one active ingredient selected from the group consisting of local anesthetic component, antipruritic component, antihistamine component and antiphlogistic component It also provides a method for enhancing the efficacy of an active ingredient.

Regarding the above-mentioned A) active ingredient, B) ingredient and C) ingredient, specific examples of these ingredients, blending ratio in the chemical solution,
The concentration in the aerosol preparation, the mixing ratio of the B) component and the C) component, the mixing ratio of the B) component and the C) component with respect to the A) component, etc. are as described above.

In the present invention, the enhancement of the drug effect of the active ingredient in the aerosol preparation means that the expression of the drug effect of the above-mentioned active ingredient is promoted (immediate effect) as compared with the case where only the active ingredient is sprayed. There may be mentioned a case where at least one phenomenon is observed such that the drug effect itself of the above-mentioned active ingredient is enhanced, or the drug effect of the above-mentioned active ingredient is long-lasting (persistence).

[0070]

EXAMPLES The present invention will be described below in more detail based on Examples and Test Examples, but the present invention is not limited to these Examples and the like. In each prescription below,%
Unless otherwise specified, it means% by weight (W / W).

Examples 1 to 19 and Comparative Examples 1 and 2 Aerosol preparations having the formulations shown below were filled in an aerosol container according to a conventional method to prepare aerosol products.

Example 1 <Chemical Solution> Crotamiton 5.0 (%) Diphenhydramine 0.5 Urea 10.0 l-Menthol 1.0 1,3-Butylene glycol 5.0 Ethanol 38.5 Purified water 40.0 Total 100.0% <propellant> dimethyl ether 100.0% <chemical liquid>: <propellant> = 70:30 (volume ratio).

Example 2 <Chemical Solution> Crotamiton 3.5 (%) Lidocaine 0.3 Urea 1.0 Peppermint oil 2.0 Glycerin 5.0 Ethanol 30.0 Purified water 58.2 Total 100.0% <Injection Agent> Liquefied petroleum gas 100.0% <chemical liquid>: <propellant> = 60:40 (volume ratio).

Example 3 <Chemical Solution> Chlorpheniramine Maleate 0.2 (%) Dexamethasone Acetate 0.05 Glycyrrhetinic Acid 1.0 Bisabolol 0.4 l-Menthol 0.2 Hydroxyethyl Cellulose 0.3 Xanthan Gum 0.1 Propylene Glycol 5.0 Squalane 1.0 Cetanol 1.0 Glyceryl monostearate 0.2 Polyoxyethylene cetyl ether 0.3 KSG16 (Shin-Etsu Chemical) 0.5 Laurylmethyl taurine Na 3.0 Ethanol 1.0 Purified water 81. 75 total 100.00% <propellant> dimethyl ether 50.0 (%) liquefied petroleum gas 50.0 total 100.0% <chemical liquid>: <propellant> = 20:80 (volume ratio).

Example 4 <Medicinal solution> Miconazole nitrate 1.0 (%) Chlorhexidine gluconate 0.5 Diphenhydramine hydrochloride 1.0 Stearyl glycyrrhizinate 0.5 Urea 1.0 Mint oil 0.5 dl-camphor 1.0 Stearin Acid Polyglyceride 1.0 Dipropylene glycol 20.0 Stearic acid 0.5 Cetanol 2.0 Paraffin 0.5 Polyoxyethylene hydrogenated castor oil 1.0 Silicone KF-96A (20cs) (Shin-Etsu Chemical) 1.0 Hydroxyethyl cellulose 0.4 sodium hydroxide (adjusted to pH 7) Appropriate amount purified water Balance part total 100.0% <propellant> 100.0% liquid petroleum gas <chemical>: <propellant> = 30: 70 (volume ratio) .

Example 5 <Medicinal solution> Dibucaine hydrochloride 0.1 (%) crotamiton 6.0 chlorpheniramine maleate 1.0 allantoin 0.2 peppermint oil 2.0 isopropylmethylphenol 0.1 ethanol 40.0 purified water 50.6 total 100.0% <propellant> dimethyl ether 50.0 liquefied petroleum gas 50.0 total 100.0% <chemical liquid>: <propellant> = 40:60 (volume ratio).

Example 6 <Medicinal solution> Methyl salicylate 10.0 (%) Bufexamac 1.0 Urea 5.0 Eucalyptus oil 7.0 Ethanol 10.0 Purified water 67.0 Total 100.0% <Propellant> Dimethyl ether 90.0 (%) Liquefied petroleum gas 10.0 Total 100.0% <chemical liquid>: <propellant> = 50:50 (volume ratio).

Example 7 <Medicinal solution> Dibucaine hydrochloride 0.3 (%) Stearyl glycyrrhetinate 0.5 l-Menthol 0.3 Polyoxyethylene sorbitan fatty acid ester 1.0 Glycerin 3.0 Jojoba oil 5.0 Purified water 89 9.9 total 100.0% <propellant> dimethyl ether 40.0 (%) liquefied petroleum gas 60.0 total 100.0% <chemical liquid>: <propellant> = 20:80 (volume ratio).

Example 8 <Medicinal solution> Bufexamac 2.5 (%) Glycyrrhetinic acid 0.5 1-Menthol 0.1 Tri (capryl-capric acid) glyceryl 1.0 Ethanol 5.0 1,3-Butylene glycol 1. 0 Purified water 89.9 total 100.0% <propellant> liquefied petroleum gas 100.0 total 100.0% <chemical liquid>: <propellant> = 30:70 (volume ratio).

Example 9 < Chemical Solution > Dexamethasone 0.025 (%) Glycyrrhetinic acid 0.500 1-Menthol 0.500 Ethanol 2.000 Isopropyl palmitate 2.000 Xanthan gum 0.100 Purified water 94.875 Total 100. 0% <Propellant> Diethyl ether 50.0 (%) Liquefied gas 50.0 Total 100.0% <Chemical solution>: <Propellant> = 50:50 (volume ratio).

Test Example 1 Antipruritic Effect Test Thirty-five healthy persons (male, 20 to 30 years old) were subjected to the primary test, and the antipruritic effect test was conducted in a quiet laboratory at room temperature of 25 ° C.

The stratum corneum on the inside of the left and right forearms (area area: 20 mm x 50 mm) of 35 test subjects was thinly peeled off with sandpaper. Next, 50 μl of a 0.1% histamine solution was applied to the peeled skin. Among the 35 subjects of the primary test, 33 persons in whom itch was induced were used as subjects (subjects of the secondary test) of the next experiment for evaluating the antipruritic effect.

[0083]

[Table 1]

The antipruritic effect test was carried out by using a drug solution having the composition shown in the above Table 1 containing the antipruritic component (crotamiton), the antihistamine component (diphenhydramine) and the local anesthetic component (lidocaine) and the propellant shown in the above Table 50. : 50
An aerosol product was prepared by filling an aerosol container at a ratio of (volume ratio), and the aerosol product (11 types of test formulations; Examples 10 to 15 and Comparative Examples 1 to 6) was used. Specifically, a group of 3 subjects of the secondary test (total 11
Each test formulation was sprayed on the inside of the right forearm as a group), and after spraying, the degree of itchiness at 0.5, 1, 2, 5, 10 and 20 minutes after spraying was measured as a score value with reference to the following criteria. I got it listed. With respect to this score value, the average value of 3 persons was obtained, and the antipruritic effect of each test preparation was evaluated.

<Evaluation of pruritus sensation> 1: Does not feel itching 2: Slight itchiness, but not noticeable 3: Feel a little itchy and worry about itching 4: Itching 5: I feel an unbearable itch.

The results are shown in FIG. As you can see from the figure,
For histamine-induced pruritus, in addition to the active ingredient, the essential oil component (menthol, camphor) and either urea, dipotassium glycyrrhizinate, glycyrrhetinic acid or allantoin, the test preparation of the present invention (Example 10) 15 to 15) are for comparison, in which the basic ingredient is an active ingredient (Comparative Example 1), an active ingredient and an essential oil ingredient (Comparative Example 5), or an active ingredient and dipotassium glycyrrhizinate, glycyrrhetinic acid or allantoin (Comparative Examples 2-4). It was shown that the immediate antipruritic effect was enhanced and its durability was also enhanced as compared with the test formulation of.

Test Example 2 Anti-inflammatory and analgesic effect test In order to evaluate the anti-inflammatory and analgesic effect of the present invention against burns, sunburns, etc., the following test was conducted.

In the anti-inflammatory and analgesic effect test, the anti-inflammatory and analgesic ingredients (bufexamac, dexamethasone) as active ingredients are shown in Table 2 below.
An aerosol product was prepared by filling a drug solution having the composition shown in Table 2 and the propellant shown in Table 2 in a ratio of 50:50 (volume ratio) to prepare an aerosol product, and the aerosol product (9 types of test formulations (Examples 16 to 19, Comparative Examples 6 to 10)) were used. Specifically, moxibustion was performed on the inside of the right forearm of 5 subjects per group (9 groups in total), and then each test preparation was sprayed on the inside of the right forearm, and pain and tingling sensation due to moxibustion 5 minutes after spraying. Skin conditions such as heat, heat, inflammation (redness) and blisters were evaluated according to the following criteria. This judgment result is totaled,
The anti-inflammatory and analgesic effect of each test preparation was evaluated by using the skin condition with the highest number of subjects among the 5 subjects as a score.

<Evaluation of skin condition> A: Pain, tingling sensation, heat, inflammation (redness) disappeared, and no blistering was observed. ◯: Pain, tingling sensation, heat, inflammation (redness) disappeared. Δ: Pain, tingling sensation, heat disappeared ×: Only tingling sensation, heat disappeared.

[0090]

[Table 2]

The results are also shown in Table 2. As can be seen from Table 2, in the test preparations of the present invention (Examples 16 to 19) in which an essential oil component (menthol) and glycyrrhetinic acid or allantoin were added to the active ingredient, the basic ingredient was the active ingredient (Comparative Example 6), Or active ingredient and glycyrrhetinic acid,
It was revealed that the effect of improving skin symptoms such as pain and inflammation due to heat was superior to that of the test preparations containing the essential oil component or allantoin (Comparative Examples 7 to 10).

From the above results, it was clarified that the preparation of the present invention containing an anti-inflammatory and analgesic ingredient as an active ingredient has an enhanced anti-inflammatory and analgesic effect on pain and inflammation caused by burns and sunburn.

[0093]

EFFECTS OF THE INVENTION According to the aerosol preparation of the present invention, the pharmacological effect of the active ingredient is enhanced as compared with the case where only the active ingredient (A component) is prepared into an aerosol preparation and spray-administered. Can be sustained. Further, in the aerosol preparation of the present invention, not only the effect of the active ingredient is enhanced, but also added in addition to the active ingredient, urea, glycyrrhizinic acid, a salt of glycyrrhizinic acid, a derivative of glycyrrhizinic acid, glycyrrhetinic acid, glycyrrhetinic acid. Since the original effects of the components such as the salt, the glycyrrhetinic acid derivative, the allantoin or the allantoin derivative are also exerted, it is expected that the synergistic effect of the two can be exhibited.

[Brief description of drawings]

FIG. 1 shows the aerosol preparations of the present invention (A, B and C) for pruritus induced by histamine in Test Example 1.
It is a figure which shows the result which compared the antipruritic effect of the comparative aerosol formulation (Comparative Examples 1-5) which does not contain B component and / or C component with the antipruritic effect of containing a component and Examples 10-15. In this figure, the vertical axis represents the average score value (the degree of itch) for the evaluation of pruritus, and the horizontal axis represents the time after spraying each test preparation.

─────────────────────────────────────────────────── ─── Continuation of front page (51) Int.Cl. ⁷ Identification code FI theme code (reference) A61K 31/4704 A61K 31/4704 31/573 31/573 47/16 47/16 47/22 47/22 47 / 26 47/26 47/44 47/44 A61P 17/04 A61P 17/04 23/02 23/02 29/00 29/00 37/08 37/08 F term (reference) 4C076 AA24 BB31 CC04 CC05 CC18 DD54 DD60 DD69 EE53 4C086 AA01 AA02 AA10 BC17 BC28 EA19 MA05 MA13 MA63 NA05 ZA21 ZA89 ZB11 ZC13 4C206 AA01 AA02 AA10 FA10 GA19 GA31 HA16 MA33 MA83 NA05 ZA21 ZA89 ZB11 ZC13

Claims (5)

[Claims] 1. A) at least one active ingredient selected from the group consisting of local anesthetic components, antipruritic components, antihistamine components and anti-inflammatory components, B) urea, glycyrrhizinic acid, salts of glycyrrhizinic acid, and derivatives of glycyrrhizinic acid. At least one selected from the group consisting of glycyrrhetinic acid, a salt of glycyrrhetinic acid, a derivative of glycyrrhetinic acid, allantoin and a derivative of allantoin, C) an essential oil component,
And D) an aerosol formulation containing a propellant. 2. The active ingredient is lidocaine, dibucaine, amino acid ethyl benzoate, crotamiton, ictamol, moctamol, thymolic acid, chlorpheniramine, diphenhydramine, isothibenzyl, guaiazulene, bufexamac, dexamethasone, hydrocortisone, prednisolone, salts thereof, and The aerosol preparation according to claim 1, which is at least one selected from the group consisting of these derivatives. 3. An aerosol product obtained by filling an aerosol container with the aerosol preparation according to claim 1 or 2. 4. A composition for enhancing the drug efficacy of at least one active ingredient selected from the group consisting of a local anesthetic component, an antipruritic component, an antihistamine component and an antiphlogistic component in an aerosol preparation, which comprises B) urea and glycyrrhizin. Acid, a salt of glycyrrhizinic acid, a derivative of glycyrrhizic acid, glycyrrhetinic acid, a salt of glycyrrhetinic acid, a derivative of glycyrrhetinic acid, at least one selected from the group consisting of allantoin and allantoin derivatives, and C) a composition containing an essential oil component object. 5. In addition to A) at least one active ingredient selected from the group consisting of local anesthetic components, antipruritic components, antihistamine components and antiphlogistic components, B) urea, glycyrrhizinic acid, salts of glycyrrhizinic acid, and glycyrrhizin. At least one selected from the group consisting of an acid derivative, glycyrrhetinic acid, a salt of glycyrrhetinic acid, a derivative of glycyrrhetinic acid, allantoin and an allantoin derivative, and C) an essential oil component are combined and combined, and the aerosol is prepared. A method for enhancing the efficacy of an active ingredient in a preparation.