JPH0794378B2 - Aerosol - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION 1) Field of Industrial Application The present invention relates to an aerosol agent used for cosmetics, quasi drugs, pharmaceuticals and the like. More specifically, an aerosol characterized by containing an acrylic and methacrylic copolymer as a film-forming agent to form a film by spraying or applying on the skin, and effectively applying the active ingredient to the skin. It is related to agents. The aerosol composition of the present invention can be applied to antibacterial agents, anti-inflammatory agents, anti-allergic agents, hair-growing agents, and insect repellents.

2) Conventional Technology As an external preparation composition having a film formation, a preparation in which a hydrophobic polymer is dissolved in acetone, ethyl acetate or the like has been heretofore known (JP-A-50-4914, JP-A-50-25725). ). However, these have problems in use, such as stickiness of the film-forming agent when dried and discomfort due to difficulty in removal from the skin. Further, since it is dissolved in an organic solvent such as acetone or ethyl acetate, it has a problem that it is harmful to the body when applied. Further, a preparation using a water-soluble polymer such as polyvinyl butyral and polyvinyl alcohol-soluble polyamide as a film-forming agent is also known (JP-A-54-14).
0714, JP-A-58-78633, JP-A-59-47269, JP-A-57-112
323). However, these also have poor transparency of the coating,
It had the drawbacks that it took a long time to form a film and the film was sticky and the ring used was poor.

3) Problems to be Solved by the Invention The prior art of external preparations for skin containing a film-forming agent has various problems as described above. Therefore, an object of the present invention is to obtain a skin external preparation, particularly an aerosol preparation, containing a film-forming agent having the following characteristics.

Immediately dry and non-greasy.

The film is strong and does not stain clothes.

It must be a highly safe composition.

Has good skin adhesion and does not come off easily.

4) Means for Solving the Problem The present inventors have conducted diligent research in view of such a situation, and as a result, the acrylic and methacrylic copolymers conventionally used as film coating agents for oral preparations have been used. The present invention has been completed by discovering that a formulation satisfying the above object can be obtained by adding a certain Eudragit as a film forming agent.

The present invention provides an acrylic and methacrylic copolymer 0.05
~ 5 wt% mixture, lower alcohol 5-60 wt% and / or water 20 wt% or less, and compounding ratio 50:50
-80: 20% by volume of a liquefied petroleum gas and a propellant consisting of dimethyl ether, 10 to 50% by weight, and an active ingredient mixed with a base component.

The present invention will be described in more detail below.

The active ingredients to be blended in the present invention include tolnaftate, clotrimazole, bifonazole, miconazole nitrate, econazole nitrate, ketoconazole nitrate, omoconazole nitrate, oxyconazole nitrate, exaramide,
Antibacterial agents such as tricyclate, siccanin, hydrocortisone, dexamethasone, clobetasol 17-propionate, dexamethasone 17-valerate, steroidal anti-inflammatory agents such as fluocinonide, halcinonide, amcinonide, indomethacin, ketoprofen, flurbiprofen, felbinac, piroxib, piroxicam, piroxib Non-steroidal anti-inflammatory drugs such as piconol, benzadac, butyl flufenamic acid, bufexamac,
l-menthol, camphor, nonyl acid vanillyl amide,
Topical stimulants such as capsaicin, ketotifen, azelastine and their salts, chromium pheniramine maleate,
Antiallergic agents such as oxaitomid, tranilast, sodium chromoglycolate, benzalkonium chloride,
Hair growth agents such as benzyl nicotinate, estradiol, capsicum tincture, and photosensitizer, and insect repellents such as diethyltoluamide, turpentine, and camphor are mixed. These active ingredients are 0.0001 depending on the effective amount of each active ingredient.
It is mixed in the range of 5 wt%. Eudragit used as a film-forming agent is methacrylic acid, methacrylic acid methyl ester, methacrylic acid ethyl ester,
It is a copolymer composed of two or more of methacrylic acid butyl ester, trimethylammonium methacrylic acid chloride, ethyl acrylate, dimethylaminoethyl methacrylate, and the like, and Eudragit E100 (methyl methacrylate / butyl methacrylate) manufactured by Reem Co.・ Dimethylaminoethyl methacrylate copolymer), Eudragit L30D-55, (methacrylic acid / ethyl acrylate copolymer, Eudragit L100-55 (methacrylic acid / ethyl acrylate copolymer), Eudragit L100 (methacrylic acid / methacrylic acid) Methyl acid copolymer),
Eudragit S100 (methacrylic acid / methacrylic acid methyl copolymer), Eudragit RS100L, Eudragit RSPML, Eudragit RS30DL, Eudragit R
Products such as S100, Eudragit RSPM, Eudragit RS30D (all of these RS types are ethyl acrylate / methyl methacrylate / trimethylammonium ethyl methacrylate chloride copolymer), Eudragit NE30D (methyl methacrylate / ethyl acrylate copolymer) Can be used.

The content of these Eudragit is 0.05 to 5% by weight,
Preferably 0.1 to 2% by weight is blended in one kind or in a combination of two or more kinds. As a solvent for dissolving Eudragit, a lower alcohol such as ethanol or isopropanol is mixed. Ethanol is most preferred as the lower alcohol.

The lower alcohol is blended in an amount sufficient to dissolve Eudragit, that is, 5 to 60% by weight, preferably 10 to 50% by weight. Water is 20% by weight or less, preferably
10% by weight or less is blended. As the propellant, for example, liquefied petroleum gas, dimethyl ether, carbon dioxide or Freon 1
Propellants such as 1, Freon 12, Freon 113, and Freon 114 can be used. Further, these propellants are injected in a range of 10 to 50% by weight so that the pressure of the preparation is 0.8 to 8.0 kg / cm. Among the above-mentioned propellants, a combination of liquefied petroleum gas and dimethyl ether is most preferable from the viewpoint of the solubility of Eudragit and the drying property of the coating. The mixing ratio of liquefied petroleum gas and dimethyl ether is preferably 50:50 to 80: 20% by volume from the viewpoint of flammability and solubility of the film forming agent.

In addition to the above essential ingredients, in order to dissolve the active ingredient,
Crotamiton, benzyl alcohol, resin acid ester,
It is also possible to mix a dissolving agent such as glycol, or powder such as talc, nylon powder, silicon powder, or polystyrene powder for the purpose of improving the feeling of use.

Next, the manufacturing method of the present invention will be described. The aerosol of the present invention is prepared by dissolving Eudragit in a lower alcohol, adding the active ingredient, other additives and / or purified water, and then putting it in a pressure resistant container, attaching a valve, and pressurizing a propellant. It can be manufactured.

Hereinafter, the present invention will be described more specifically with reference to examples.

Example 1 40 g of ethanol was added to 1 g of clotrimazole and dissolved by stirring. Add 1 g of Eudragit S100 to this solution,
Stir to dissolve. Next, after putting this in a pressure resistant container and attaching a valve, liquefied petroleum gas / dimethyl ether (65/3
5 wt%) 29.4 g was injected under pressure to obtain an aerosol formulation containing an antibacterial agent.

Example 2 To 2 g of 1-menthol and 0.5 g of glycol salicylate, 35 g of ethanol was added and dissolved by stirring. 1 g of Eudragit RSTML was added to this solution and dissolved by stirring. next,
After adding 5 g of purified water to this solution and stirring, put it in a pressure-resistant container, attach a valve, and then press-in 29.4 g of liquefied petroleum gas / dimethyl ether (65/35% by weight) to prepare an aerosol formulation containing an anti-inflammatory agent. Got

Example 3 To 1 g of ketoprofen, 40 g of ethanol was added and dissolved by stirring. 1 g of Eudragit RSPM was added to this solution and dissolved by stirring. Next, after putting this in a pressure resistant container and attaching a valve, liquefied petroleum gas / dimethyl ether (65/35
29.4 g (by weight) was injected under pressure to obtain an aerosol formulation containing an anti-inflammatory agent.

Example 4 1 g of clotrimazole and 40 g of ethanol and 1 of crotamiton
g was added and stirred to dissolve. 1 g of Eudragit L30D-55 was added to this solution and dissolved by stirring. Next, after putting this in a pressure resistant container and attaching a valve,
27.4 g of dimethyl ether (65/35% by weight) was press-fitted to obtain an aerosol formulation containing an antibacterial agent.

Example 5 To 1 g of ketoprofen, 40 g of ethanol and 2 g of diethyl sebacate were added and dissolved by stirring. 1 g of Eudragit L100 was added to this solution and dissolved by stirring. Next, this was put into a pressure resistant container, and after attaching a valve, 27.4 g of liquefied petroleum gas / dimethyl ether (65/35% by weight) was press-fitted to obtain an aerosol preparation containing an anti-inflammatory agent.

Example 6 Ethinyl estradiol 0.0004 g, benzyl nicotinate 0.01 g, ethanol 40 g and isopropyl myristate
1 g was added and dissolved by stirring.

1 g of Eudragit L100 was added to this solution and dissolved by stirring. Then put this in a pressure resistant container, attach a valve, and then liquefied petroleum gas / dimethyl ether (65/35 wt%) 2
7.4 g was press-fitted to obtain an aerosol formulation containing a hair restorer.

Example 7 0.5 g of ketotifen, 40 g of ethanol and 1 g of isopropyl myristate were added and dissolved by stirring. 1 g of Eudragit S100 was added to this solution and dissolved by stirring. Next, put this in a pressure resistant container, attach a valve, and then press fit 27.4 g of liquefied petroleum gas / dimethyl ether (65/35 wt%),
An aerosol formulation containing an anti-allergic agent was obtained.

Example 8 Diethylamide 1 g, dl-camphor 0.5 g, ethanol 40 g
And 1 g of isopropyl myristate were added and dissolved by stirring. 1 g of Eudragit S100 was added to this solution and dissolved by stirring. Next, this was put into a pressure resistant container, and after attaching a valve, 27.4 g of liquefied petroleum gas / dimethyl ether (65/35% by weight) was press-fitted to obtain an aerosol formulation containing an insect repellent.

Reference Example 1 To 70 g of ethanol, 1 g of clotrimazole and 5 g of soluble nylon (CM-9000) were added and dissolved, and this was put in a pressure resistant container and fitted with a valve, and then CFC 11 30 g and CFC 124 4
An aerosol formulation containing an antibacterial agent was obtained by press-fitting 5 g.

Test Example 1 The aerosol preparation of Example 1 of the present invention and the aerosol preparation of Reference Example 1 were sprayed on the forearm of a healthy adult male and tested for dryness and usability. The results are shown in Table 1.

As can be seen from Table 1, the film-forming agent-containing aerosol preparation of the present invention was superior to the aerosol preparation of Reference Example in terms of film drying property and feeling of use.

5) Effect of the Invention The aerosol obtained in the present invention containing an acrylic and methacrylic copolymer (Eudragit) as a film-forming agent has a dryness of the film which is not sticky when sprayed. Is very good. In addition, the formed film is a film that has good adhesiveness and is hard to peel off and has excellent sealing property. Since it promotes retention of the active ingredient or transdermal absorbability, it has an excellent pharmacological effect. Eudragit is also superior to other film forming agents in terms of safety.

From the above, the aerosol composition of the present invention containing an antibacterial agent, an anti-inflammatory agent, an antiallergic agent, a hair-growing agent, and an insect repellent as active ingredients is very useful industrially as cosmetics, quasi drugs, and pharmaceuticals. is there.

Continuation of front page (51) Int.Cl. ⁶ Identification number Office reference number FI technical display location // A01N 37/02

Claims (1)

[Claims] 1. Acrylic and methacrylic copolymer 0.05
~ 5 wt% mixture, lower alcohol 5-60 wt% and / or water 20 wt% or less, and compounding ratio 50:50
An aerosol agent in which an active ingredient is mixed with a base component consisting of 10 to 50% by weight of a propellant consisting of liquefied petroleum gas and dimethyl ether of 80:20.