Skin composition

Abstract

The present invention addresses the problem of providing a film-forming skin composition (such as a film-forming skin protective agent or a film-forming skin topical agent) that does not contain lower monohydric alcohols such as ethanol or isopropanol, has excellent quick-drying properties and water resistance, is less sticky, and has an excellent feel when used. The present invention relates to a film-forming composition for skin, which contains a specific acrylic polymer, a plasticizer, and water, and is substantially free of lower monohydric alcohols such as ethanol and isopropanol. The composition of the present invention is extremely useful for treating chronic skin diseases (i.e., skin diseases with impaired skin barrier function) such as hand eczema and atopic dermatitis.

Description

Technical Field

[0001] The present invention relates to a film-forming composition, specifically a film-forming skin protectant and a film-forming topical skin agent.

Background Art

[0002] Liquid bandages that form a thin film are said to be effective for symptoms with reduced skin barrier function (such as chapping, abrasions, cracks, etc.) and are commercially available for the purpose of protecting the skin from water work and the like. However, many of them contain lower monohydric alcohols such as ethanol and isopropanol to enhance quick-drying properties, and are accompanied by a sense of irritation during application. Similarly, in hand eczema, seborrheic dermatitis, atopic dermatitis, etc. where the skin barrier function is also reduced, the affected area is often more extensive, and film-forming compositions containing lower monohydric alcohols that cause skin dryness and a sense of irritation are difficult to use. Development of film-forming compositions that do not contain these lower monohydric alcohols (that is, have high skin safety) and maintain the film even by contact with water (that is, have a continuous protective effect) has been desired by patients and medical personnel.

[0003] Patent Documents 1 and 2 disclose topical agents for fingers that form a flexible film when applied to the entire finger, have excellent quick-drying properties and adhesiveness to the skin, and can be gently washed away without irritating the skin after use. However, this topical agent for fingers contains lower monohydric alcohols such as ethanol from the viewpoint of quick-drying properties and the like.

Prior Art Documents

Patent Documents

[0004]

Patent Document 1

Patent Document 2

Summary of the Invention

Problems to be Solved by the Invention

[0005] Therefore, an object of the present invention is to provide a film-forming skin composition, specifically a film-forming skin protectant and a film-forming topical skin preparation, which are excellent in quick-drying property and water resistance, have little stickiness, and have excellent usability even without containing lower monohydric alcohols such as ethanol and isopropanol. Means for Solving the Problems

[0006] As a result of repeated studies to solve the above problems, the present inventors have found that the above problems can be solved by a combination of a specific acrylic polymer and a plasticizer, and have completed the present invention.

[0007] That is, the present invention relates to [1] to

[10] . [1] (a) One or more acrylic polymers selected from the group consisting of ethyl acrylate / methyl methacrylate / ethyl trimethylammonium methacrylate copolymer, ethyl acrylate / methyl methacrylate copolymer, methyl acrylate / methyl methacrylate / methacrylic acid copolymer, and methacrylic acid / ethyl acrylate copolymer, (b) One or more plasticizers selected from the group consisting of an ester compound liquid at room temperature, an aromatic alcohol liquid at room temperature, a medium-polar solid ester compound, and terpenes, and (c) Water in an amount of 36% by weight or more based on the total amount of the composition (excluding the propellant in the case of an aerosol composition) A film-forming skin composition, characterized by containing substantially no lower monohydric alcohol. [2] The ester compound liquid at room temperature is selected from triethyl citrate, triacetin, dibutyl phthalate, diethyl sebacate, diisopropyl sebacate, diisopropyl adipate, and medium-chain fatty acid triglyceride, The aromatic alcohol liquid at room temperature is selected from ethylene glycol salicylate and phenoxyethanol, The medium-polar solid ester compound is selected from phospholipids and paraoxybenzoic acid esters, and The composition according to [1], wherein the terpenoids are selected from limonene and menthol. [3] The composition according to [1], comprising at least one plasticizer selected from triethyl citrate, triacetin, dibutyl phthalate, diethyl sebacate, diisopropyl sebacate, diisopropyl adipate, and medium-chain fatty acid triglyceride. [4] The composition according to [1], comprising at least one plasticizer selected from ethylene glycol salicylate and phenoxyethanol. [5] The composition according to [1], comprising at least one plasticizer selected from phospholipids and paraoxybenzoic acid esters. [6] The composition according to [1], comprising at least one plasticizer selected from limonene and menthol. [7] The composition according to any one of [1] to [6], wherein the content of the acrylic polymer is 6 to 35% by weight based on the total amount of the composition (excluding the propellant in the case of an aerosol composition). [8] The composition according to any one of [1] to [7], wherein the content of the plasticizer is 1.3 to 35% by weight based on the total amount of the composition (excluding the propellant in the case of an aerosol composition). [9] The composition according to any one of [1] to [8], further comprising a propellant.

[10] The composition according to any one of [1] to [9], further comprising light anhydrous silicic acid and / or titanium oxide. [Advantages of the Invention]

[0008] The composition of the present invention contains substantially no lower monohydric alcohols such as ethanol and isopropanol, so it has little skin irritation. In addition, since the composition of the present invention contains a large amount of water (36% by weight or more), it has a refreshing feeling of use. Further, although the composition of the present invention does not contain lower monohydric alcohols as described above and contains a large amount of water, it is excellent in quick-drying property. Furthermore, the formed film has water resistance, little stickiness, and surprisingly, has an excellent effect of suppressing water evaporation. The composition of the present invention can be used as a film-forming skin protectant and a film-forming topical skin preparation.

Brief Description of the Drawings

[0009]

Figure 1

Modes for Carrying Out the Invention

[0010] The composition of the present invention contains a specific acrylic polymer, a plasticizer, and water, and is characterized by substantially not containing lower monohydric alcohols such as ethanol and isopropanol. Specifically, the composition of the present invention can be used as a film-forming skin protectant and a film-forming topical skin preparation.

[0011] A film-forming skin protectant (without a medicinal ingredient) can form a thin film by spraying or applying it on the skin, and can effectively protect the skin. It can be used for the prevention and treatment of skin diseases such as hand eczema typified by housewife's eczema, seborrheic dermatitis, and atopic dermatitis. On the other hand, a film-forming topical skin preparation (containing a medicinal ingredient) can form a film by spraying or applying it on the skin, and can effectively deliver the medicinal ingredient to the skin. The same effect can also be expected when applied to nails, the skin around nails, and mucous membranes. This can be formulated into dosage forms such as solutions, lotions, gels, creams, and aerosols, and can be applied to antibacterial agents, antifungal agents, vitamins, anti-inflammatory agents, anti-allergy agents, moisturizing agents, wound healing agents, etc.

[0012] The acrylic polymers used in the present invention are preferably ethyl acrylate-methyl methacrylate-trimethylammonium chloride ethyl methacrylate copolymer, ethyl acrylate-methyl methacrylate copolymer, methyl acrylate-methyl methacrylate-methacrylic acid copolymer, and methacrylic acid-ethyl acrylate copolymer. These polymers have been conventionally used as film coating bases for pharmaceuticals and are known as Eudragit (EUDRAGIT (登録商標) ) RS type, Eudragit RL type, Eudragit NE type, Eudragit FS type, and Kollicoat (Kollicoat (登録商標) ) MAE type. The acrylic polymer used in the present invention is a water-insoluble acrylic polymer. In this specification, the water-insoluble acrylic polymer refers to not only an acrylic polymer that does not dissolve in water regardless of the pH of water (pH-independent - water-insoluble acrylic polymer), but also includes a pH-dependent - water-insoluble acrylic polymer. The pH-dependent - water-insoluble acrylic polymer preferably does not dissolve in water with an acidic pH (pH less than 7, particularly less than pH 5.5).

[0013] The Eudragit RS type is an ethyl acrylate-methyl methacrylate-trimethylammonium chloride ethyl methacrylate copolymer, and its composition ratio is 1:2:0.1. The average molecular weight (Mw) is about 32,000, and it is pH-independent and insoluble in water. The Eudragit RL type is an ethyl acrylate-methyl methacrylate-trimethylammonium chloride ethyl methacrylate copolymer, and its composition ratio is 1:2:0.2. The average molecular weight (Mw) is about 32,000, and it is pH-independent and insoluble in water. The Eudragit NE type is an ethyl acrylate-methyl methacrylate copolymer, and its composition ratio is 2:1. The average molecular weight (Mw) is about 750,000, and it is pH-independent and insoluble in water. Eudragit FS type is a methyl acrylate·methyl methacrylate·methacrylic acid copolymer, and its composition ratio is X:Y:1 (where X + Y = 10). The average molecular weight (Mw) is about 280,000, and it is insoluble in water with a pH less than 7. Kollicoat MAE type is a methacrylic acid·ethyl acrylate copolymer, and its composition ratio is 1:1. The average molecular weight (Mw) is about 250,000, and it is insoluble in water with a pH less than 5.5.

[0014] Eudragit RS type can be obtained, for example, as Eudragit RS100, Eudragit RSPO, Eudragit RS30D (an aqueous suspension containing 30% by weight of an ethyl acrylate·methyl methacrylate·ethyl trimethylammonium methacrylate chloride copolymer (composition ratio 1:2:0.1)) manufactured by EVONIK (Germany). Eudragit RL type can be obtained, for example, as Eudragit RL100, Eudragit RLPO, Eudragit RL30D (an aqueous suspension containing 30% by weight of an ethyl acrylate·methyl methacrylate·ethyl trimethylammonium methacrylate chloride copolymer (composition ratio 1:2:0.2)) manufactured by EVONIK (Germany). Eudragit NE type can be obtained, for example, as Eudragit NE30D (an aqueous suspension containing 30% by weight of an ethyl acrylate·methyl methacrylate copolymer (composition ratio 2:1)) manufactured by EVONIK (Germany). Eudragit FS type can be obtained, for example, as Eudragit FS30D (an aqueous suspension containing 30% by weight of a methyl acrylate·methyl methacrylate·methacrylic acid copolymer (composition ratio X:Y:1, X + Y = 10)) manufactured by EVONIK (Germany). Kollicoat MAE type can be obtained, for example, as Kollicoat MAE30DP (an aqueous suspension containing 30% by weight of a methacrylic acid·ethyl acrylate copolymer (composition ratio 1:1)) manufactured by BASF (Germany). The content of the polymer with respect to the total amount of the composition of the present invention (however, excluding the propellant in the case of an aerosol agent) is preferably 6 to 35% by weight, more preferably 10 to 30% by weight, and particularly preferably 14 to 28% by weight.

[0015] The acrylic polymer used in the present invention may be used alone or in combination. Since the composition of the present invention is excellent in water resistance, it may not particularly contain a silicone-based polymer.

[0016] The composition of the present invention substantially does not contain a lower monohydric alcohol (a monohydric alcohol having 1 to 3 carbon atoms, such as ethanol, isopropanol, etc.). Substantially not containing means that a lower monohydric alcohol is not intentionally added in the manufacturing process. Therefore, the content of the lower monohydric alcohol in the composition of the present invention is usually 0% by weight, and even if it is slightly mixed, the content is less than 1% by weight (more preferably less than 0.5% by weight).

[0017] Usually, a lower monohydric alcohol such as ethanol or isopropanol is used to dissolve an acrylic polymer which is a film-forming component. However, when used for the treatment of skin diseases with a reduced barrier function such as hand eczema or atopic dermatitis, it is preferable not to contain a lower monohydric alcohol which causes skin dryness and a sense of irritation. Since the composition of the present invention substantially does not contain a lower monohydric alcohol, it has high safety to the skin and is suitable for treating hand eczema and atopic dermatitis.

[0018] Examples of the plasticizer used in the present invention include an ester compound that is liquid at normal temperature (25°C; the same applies hereinafter), an aromatic alcohol that is liquid at normal temperature, a medium-polar solid ester compound, and terpenes. These may be used alone or in combination of a plurality of kinds.

[0019] Preferable examples of the ester compounds that are liquid at normal temperature include triethyl citrate, triacetin, dibutyl phthalate, diethyl sebacate, diisopropyl sebacate, diisopropyl adipate, and medium-chain fatty acid triglycerides (such as glyceryl triisooctanoate and glyceryl tri(caprylic / capric acid)). More preferable are fatty acid esters that are liquid at normal temperature and are selected from diethyl sebacate, diisopropyl sebacate, diisopropyl adipate, and medium-chain fatty acid triglycerides. Among these, diethyl sebacate and diisopropyl adipate are even more preferable, and diisopropyl adipate is particularly preferable.

[0020] Preferable examples of the aromatic alcohols that are liquid at normal temperature include ethylene glycol salicylate and phenoxyethanol.

[0021] Examples of the medium-polarity solid ester compounds include phospholipids (such as lecithin, especially hydrogenated lecithin) and ester compounds that are solid at normal temperature, such as paraoxybenzoic acid esters. In this specification, medium-polarity means that the α value according to the organic concept diagram is 35° to 55°. The organic concept diagram was proposed by Fujita Akira, and its details are described in "Pharmaceutical Bulletin", 1954, vol.2, 2, pp.163-173; "Chemical Field", 1957, vol.11, 10, pp.719-725; "Fragrance Journal", 1981, vol.50, pp.79-82, etc. That is, taking methane (CH4) as the origin of all organic compounds, and regarding all other compounds as derivatives of methane, certain numerical values are set for their carbon number, substituents, modified parts, rings, etc., and the scores are added to obtain the organic value and the inorganic value. The slope when plotting this value on a graph with the organic value on the X-axis and the inorganic value on the Y-axis, and the angle is the α value.

[0022] Examples of combinations of ester compounds that are liquid at room temperature include combinations of medium-chain fatty acid triglycerides (e.g., glyceryl triisooctanoate and glyceryl tri (caprylyl / capric acid)), and triethyl citrate, triacetin, dibutyl phthalate, diethyl sebacate, diisopropyl sebacate, or diisopropyl adipate.

[0023] Examples of combinations of ester compounds that are liquid at room temperature and aromatic alcohols that are liquid at room temperature include combinations of medium-chain fatty acid triglycerides (e.g., glyceryl triisooctanoate and glyceryl tri (caprylyl / capric acid)), and ethylene glycol salicylate or phenoxyethanol.

[0024] The content of the plasticizer with respect to the total amount of the composition of the present invention (excluding the propellant in the case of an aerosol) is preferably 1.3 to 35% by weight, more preferably 1.4 to 29% by weight, and particularly preferably 1.4 to 8% by weight. If the amount of the plasticizer is less than 1.3% by weight, the film-forming property and water resistance decrease, and if it exceeds 35% by weight, the film becomes sticky, which is not preferable.

[0025] The water used in the present invention is preferably particularly purified water. The content of water with respect to the total amount of the composition of the present invention (excluding the propellant in the case of an aerosol) is preferably 36% by weight or more, more preferably 50% by weight or more. The upper limit is preferably 93% by weight. More specifically, 36 to 92% by weight is preferable, 43 to 89% by weight is more preferable, 50 to 87% by weight is particularly preferable, and 64 to 85% by weight is even more preferable. Note that Eudragit RS30D, RL30D, NE30D, and FS30D, and Kollicoat MAE30DP are all provided as aqueous suspensions containing 30% by weight of an acrylic polymer. The water contained in these aqueous suspensions (corresponding to 70% by weight of the aqueous suspension) also corresponds to the water used in the present invention.

[0026] In order to suppress the shine of the film, the composition of the present invention can contain, for example, light anhydrous silicic acid and titanium oxide. The content of these substances with respect to the total amount of the composition of the present invention (however, excluding the propellant in the case of an aerosol agent) is preferably 0.8 to 3% by weight, and particularly preferably 1 to 3% by weight.

[0027] In addition to the above components, the composition of the present invention can contain a pH adjuster. Examples of the pH adjuster include phosphates, citrates, hydroxides, hydrochloric acid, and the like. The pH adjuster may be used alone or in combination of a plurality. The content of the pH adjuster with respect to the total amount of the composition of the present invention (however, excluding the propellant in the case of an aerosol agent) is preferably 0.01 to 1% by weight, and particularly preferably 0.1 to 0.5% by weight. When a pH-dependent water-insoluble acrylic polymer is used as the acrylic polymer, it is preferable to adjust the pH of the composition to a pH at which the acrylic polymer does not dissolve. For example, when using the Eudragit FS type, it is preferable to adjust the pH of the composition to less than 7, and when using the Kollicoat MAE type, it is preferable to adjust the pH of the composition to less than 5.5.

[0028] The composition of the present invention can contain a pharmaceutically active ingredient effective for the treatment of various skin diseases, including chronic skin diseases typified by atopic dermatitis. Examples of the pharmaceutically active ingredient include, but are not limited to, the following components. · Steroidal anti-inflammatory drugs such as hydrocortisone, dexamethasone, clobetasol 17-propionate, dexamethasone 17-valerate, fluocinonide, halcinonide, amcinonide, difluprednate, and betamethasone butyrate propionate; · Non-steroidal anti-inflammatory drugs such as indomethacin, ketoprofen, flurbiprofen, felbinac, piroxicam, ibuprofen piconol, benzadac, butyl flufenamate, and bufexamac; ·Antifungal agents such as lanoconazole, tolnaftate, clotrimazole, bifonazole, miconazole nitrate, econazole nitrate, ketoconazole nitrate, omoconazole nitrate, oxiconazole nitrate, exalamide, triclocarban, and sikkimin; ·Antibacterial agents such as ozenoxacin and clindamycin; ·Anti-allergic agents such as ketotifen, azelastine and their salts, chlorpheniramine maleate, oxitropium, tranilast, and sodium cromoglycate; ·Local anesthetics such as lidocaine and propitocaine; ·Moisturizing agents such as heparin-like substances, hyaluronic acid, and urea; ·Wound healing agents such as fibroblast growth factor and bucladesine sodium; ·Acne treatment agents such as benzoyl peroxide and adapalene; ·Therapeutic agents for keratosis such as maxacalcitol for psoriasis vulgaris The content of the active ingredient with respect to the total amount of the composition of the present invention (however, excluding the propellant in the case of an aerosol) is preferably 0.01 to 5% by weight, more preferably 0.1 to 1% by weight, and particularly preferably 0.2 to 0.5% by weight.

[0029] The composition of the present invention may be an aerosol containing a propellant. Examples of the propellant include, for example, dimethyl ether (DME), or a mixture of DME and liquefied natural gas (LPG). A more preferred example of the propellant is DME. The content of the propellant in the aerosol of the present invention is preferably 30 to 50 parts by weight, more preferably 35 to 50 parts by weight, and particularly preferably 40 to 46 parts by weight with respect to 100 parts by weight of the composition excluding the propellant.

[0030] The composition of the present invention is useful for the treatment of skin diseases such as hand eczema, seborrheic dermatitis, and atopic dermatitis. The amount and frequency of application of the composition of the present invention to the skin may be appropriately adjusted according to the skin symptoms, the concentration of the drug in the composition, the age of the patient, etc. Usually, application once to several times a day is appropriate.

[0031] Although the preferred compound names of the essential components and optional components used in the composition of the present invention have been described above, the composition of the present invention includes compositions obtained by arbitrarily combining these and compositions obtained by arbitrarily combining the concentration ranges of each component. In addition, the numerical ranges such as the above concentrations can be arbitrarily combined, and when a plurality of numerical ranges are described, the upper limit values or lower limit values of each numerical range can also be arbitrarily combined.

[0032] Hereinafter, the present invention will be described in more detail with reference to Examples, but the present invention is not limited to the Examples. <Preparation Method>

[0033] [Formulation Examples 1 and 2] Ethyl acrylate·methyl methacrylate·ethyl trimethylammonium methacrylate copolymer (composition ratio 1:2:0.2) and purified water were weighed, ethylene glycol salicylate was added, and the mixture was stirred until uniform.

[0034] [Formulation Examples 3 to 8] Ethyl acrylate·methyl methacrylate·ethyl trimethylammonium methacrylate copolymer (composition ratio 1:2:0.1) and purified water were weighed, diethyl sebacate was added, and the mixture was stirred until uniform. For Formulation Example 3, diethyl sebacate was not added, and the same operation was performed.

[0035] [Formulation Examples 9 to 15] Ethyl acrylate·methyl methacrylate·ethyl trimethylammonium methacrylate copolymer (composition ratio 1:2:0.1), medium-chain fatty acid triglyceride and purified water were weighed, triethyl citrate, triacetin, diisopropyl adipate, diisopropyl sebacate, diethyl sebacate, ethylene glycol salicylate or phenoxyethanol was added, and the mixture was stirred until uniform. This was placed in a pressure-resistant container, and DME was injected to obtain an aerosol.

[0036] [Formulation Examples 16 to 18] Ethyl acrylate·methyl methacrylate·ethyl trimethylammonium methacrylate copolymer (composition ratio 1:2:0.1) or ethyl acrylate·methyl methacrylate copolymer (composition ratio 2:1), and purified water were weighed, diethyl sebacate was added, and the mixture was stirred until homogeneous.

[0037] [Formulation Examples 19 - 21] Ethyl acrylate·methyl methacrylate·ethyl trimethylammonium methacrylate copolymer (composition ratio 1:2:0.1) and purified water were weighed, diethyl sebacate and light anhydrous silicic acid were added, and the mixture was stirred until homogeneous. This was placed in a pressure-resistant container, DME was injected under pressure, and an aerosol preparation was obtained. For Example 19, light anhydrous silicic acid was not added, and the same operation was performed.

[0038] [Formulation Examples 22 - 55] According to the preparation methods of Formulation Examples 1 - 21 described above, each acrylic polymer was used to prepare each formulation example shown in Tables 7 - 12. When a pH-dependent water-insoluble acrylic polymer was used as the acrylic polymer, the pH of the composition was adjusted to a range in which the acrylic polymer was insoluble.

[0039] The compositions of each formulation example are shown in Tables 1 - 12. [Test Example]

[0040] [Test Example 1] Evaluation of Quick Drying Property (Film Forming Property) The compositions of Formulation Examples 1 - 18 and 22 - 55 were applied to a preparate at 30°C, and the state of the film after 2 minutes and 5 minutes was visually observed, and the quick drying property was evaluated according to the following criteria. TIFF0007704509000001.tif35169

[0041] [Test Example 2] Evaluation of Water Resistance The compositions of Formulation Examples 1 - 18 and 22 - 55 were applied to a preparate at 30°C to form a film. Then, the lower half of the preparate with the film formed was immersed in water, and the state of the film after 1 minute and 10 minutes was visually observed, and the water resistance was evaluated according to the following criteria. TIFF0007704509000002.tif34169

[0042] [Test Example 3] Evaluation of Stickiness The compositions of Formulation Examples 1 to 18 and 22 to 55 were applied to a preparate at 30°C to form a film. Then, another preparate was pressed against the film-forming surface of the preparate, and the stickiness (adhesiveness) was evaluated according to the following criteria. TIFF0007704509000003.tif36169

[0043] [Test Example 4] Evaluation of Gloss The compositions of Formulation Examples 19 to 21 were applied to artificial leather (76×26 mm) at room temperature and a film was formed at 30°C. The gloss was evaluated according to the following criteria. The results are shown in Table 5. TIFF0007704509000004.tif35169

[0044] [Test Example 5] Evaluation of Moisture Evaporation Inhibiting Ability A circle with a diameter of 4 cm was opened in the center of the plastic cup lid, and a carrier film was attached to this part (see Figure 1). After placing this lid on a cup containing 50 g of water, 0.1 g of the composition of Formulation Example 19 was applied to the carrier film. Also, as a comparison, a carrier film without any formulation was used. As the carrier film, a hydrophobic polytetrafluoroethylene membrane filter (pore size 10 μm, diameter 47 mm) manufactured by Millipore was used. After 4 hours at 30°C / 40%RH, the amount of water vaporized from the cup in the formulation-coated group through the carrier film was designated as WL X (g / h), the amount of water vaporized from the cup in the non-formulation-coated group through the carrier film was designated as WL0 (g / h), and the moisture evaporation inhibition rate (%) which is a value indicating the blocking effect was calculated using the following formula. TIFF0007704509000005.tif15169

[0045] As shown in Table 1, by using a specific acrylic polymer and a specific plasticizer, Formulation Examples 1 and 2 were obtained, which had rapid film formation (excellent quick-drying property), excellent water resistance, no (or little) stickiness, and excellent usability even without containing lower monohydric alcohols.

[0046]

Table 1

[0047] As shown in Table 2, it was also clarified that when diethyl sebacate, which is a fatty acid ester liquid at room temperature, was used as a plasticizer, a desired formulation with rapid film formation, excellent water resistance, no (or little) stickiness, and excellent usability was obtained.

[0048]

Table 2

[0049] In addition to diethyl sebacate, it was examined whether a desired film could be obtained for ester compounds that are liquid at room temperature. As shown in Table 3, it was also clarified that when a liquid ester compound or a liquid aromatic alcohol at room temperature was combined based on medium-chain fatty acid triglycerides, a desired formulation with rapid film formation, excellent water resistance, little stickiness, and excellent usability was obtained.

[0050]

Table 3

[0051] Even when the amount of ethyl acrylate·methyl methacrylate·ethyl trimethylammonium methacrylate copolymer (composition ratio 1:2:0.1), which is a water-insoluble acrylic polymer, was increased or decreased, it was examined whether a similar desired film could be obtained. As shown in Table 4, Formulation Examples 16 and 17 had rapid film formation, excellent water resistance, no (or little) stickiness, and excellent usability. Furthermore, as a water-insoluble acrylic polymer, it was investigated whether a desired film could also be obtained in the same manner using an ethyl acrylate-methyl methacrylate copolymer (composition ratio 2:1). As shown in Table 4, Formulation Example 18 using an ethyl acrylate-methyl methacrylate copolymer (composition ratio 2:1) had rapid film formation, excellent water resistance, no stickiness, and excellent usability.

[0052]

Table 4

[0053] Generally, after applying an external preparation, it is preferable that the external preparation is not visually conspicuous at the application site. Glitter was considered as one of the factors that make it visually conspicuous. Therefore, investigations were conducted to further reduce the glitter of the film. As shown in Table 5, it was revealed that in Formulation Examples 20 and 21 containing light anhydrous silicic acid, the glitter could be completely suppressed.

[0054]

Table 5

[0055] As shown in Table 6, the water evaporation suppression rate (%) of Formulation Example 19 showed a surprisingly high value of 48.4%. The water evaporation suppression rate is one of the indicators for evaluating the occlusion effect. In skin diseases such as hand eczema, seborrheic dermatitis, and atopic dermatitis, the skin barrier function is reduced, and generally, the amount of water evaporation from the skin is large. By applying this composition, an occlusion effect on the skin can be obtained, and the water evaporation from the skin is suppressed, thus it is expected to prevent the worsening of the symptoms of the above diseases.

[0056]

Table 6

[0057] Even when the amounts of an acrylic polymer (ethyl acrylate·methyl methacrylate·ethyl trimethylammonium methacrylate copolymer) and a plasticizer (diethyl sebacate) were increased or decreased, it was also examined whether a desired film could be obtained in the same manner. As shown in Table 7, Formulation Examples 22 to 29 were rapid in film formation, excellent in water resistance, non-sticky (or less sticky), and excellent in usability. [Table 7]

[0058] Even when the amounts of another acrylic polymer (ethyl acrylate·methyl methacrylate copolymer) and a plasticizer (diethyl sebacate) were increased or decreased, it was also examined whether a desired film could be obtained in the same manner. As shown in Table 8, Formulation Examples 30 to 33 were rapid in film formation, excellent in water resistance, non-sticky (or less sticky), and excellent in usability.

[0059] [Table 8]

[0060] Furthermore, even when the amounts of yet another acrylic polymer (methacrylic acid·ethyl acrylate copolymer) and a plasticizer (diethyl sebacate) were increased or decreased, it was also examined whether a desired film could be obtained in the same manner. As shown in Table 9, Formulation Examples 34 to 38 were rapid in film formation, excellent in water resistance, non-sticky (or less sticky), and excellent in usability.

[0061] [Table 9]

[0062] Even when the amount of an acrylic polymer (methyl acrylate·methyl methacrylate·methacrylic acid copolymer) was increased or decreased using triethyl citrate as a plasticizer, it was also examined whether a desired film could be obtained in the same manner. As shown in Table 10, Formulation Examples 39 to 41 were rapid in film formation, excellent in water resistance, non-sticky, and excellent in usability.

[0063]

Table 10

[0064] Even when the type and / or amount of the plasticizer was changed and / or the amount of the acrylic polymer (ethyl acrylate / methyl methacrylate / ethyl trimethylammonium methacrylate copolymer) was increased or decreased, it was also examined whether a desired film could be obtained in the same manner. As shown in Tables 11 and 12, Formulation Examples 42 to 55 had rapid film formation, excellent water resistance, no (or little) stickiness, and excellent usability.

[0065]

Table 11

[0066]

Table 12

[0067] As a result of the above various tests, although the composition of the present invention did not contain lower monohydric alcohols such as ethanol and isopropanol, it had rapid film formation, excellent water resistance, no (or little) stickiness, and excellent usability.

[0068] In conventional film-forming skin compositions, lower monohydric alcohols such as ethanol and isopropanol have generally been used from the viewpoints of dissolution of acrylic polymers as film-forming components and quick drying property (film-forming property). In the present invention, an attempt was made to eliminate lower monohydric alcohols from the viewpoint of skin safety. As a result of intensive studies, a skin composition excellent in skin safety that can form a good film in a short time after application was found even without containing lower monohydric alcohols. In addition, since the composition of the present invention contains a large amount of water, it has a refreshing feeling of use. Moreover, surprisingly, it was confirmed that the formed film has excellent water transpiration suppressing ability. The composition of the present invention having excellent water transpiration suppressing ability is extremely useful for the treatment of chronic skin diseases such as hand eczema or atopic dermatitis (i.e., skin diseases with reduced skin barrier function).

Claims

Claim 1: A film-forming skin composition (excluding patches), comprising: (a) One or more acrylic polymers selected from the group consisting of ethyl acrylate / methyl methacrylate / trimethylammonium chloride ethyl methacrylate copolymer, ethyl acrylate / methyl methacrylate copolymer, methyl acrylate / methyl methacrylate / methacrylic acid copolymer, and methacrylic acid / ethyl acrylate copolymer; (b) One or more plasticizers selected from the group consisting of ester compounds that are liquid at room temperature, aromatic alcohols that are liquid at room temperature, medium-polarity solid ester compounds, and terpenes; and (c) Water in an amount of 36% by weight or more based on the total amount of the composition (excluding the propellant in the case of an aerosol composition). The composition contains: Substantially no lower monohydric alcohol, and Is a composition for forming a film on the skin by being applied or sprayed onto the skin. A film-forming skin composition, characterized by the above. Claim 2: The ester compound that is liquid at room temperature is selected from triethyl citrate, triacetin, dibutyl phthalate, diethyl sebacate, diisopropyl sebacate, diisopropyl adipate, and medium-chain fatty acid triglycerides; The aromatic alcohol that is liquid at room temperature is selected from ethylene glycol salicylate and phenoxyethanol; The medium-polarity solid ester compound is selected from phospholipids and paraoxybenzoic acid esters; and The terpenes are selected from limonene and menthol. The composition according to Claim 1. Claim 3: The composition according to Claim 1, comprising at least one plasticizer selected from triethyl citrate, triacetin, dibutyl phthalate, diethyl sebacate, diisopropyl sebacate, diisopropyl adipate, and medium-chain fatty acid triglycerides. Claim 4: The composition according to Claim 1, comprising at least one plasticizer selected from ethylene glycol salicylate and phenoxyethanol. Claim 5: The composition according to Claim 1, comprising at least one plasticizer selected from phospholipids and paraoxybenzoic acid esters. Claim 6: The composition according to Claim 1, comprising at least one plasticizer selected from limonene and menthol. Claim 7: The composition according to any one of claims 1 to 6, wherein the content of the acrylic polymer is 6 to 35% by weight based on the total amount of the composition (excluding the propellant in the case of an aerosol composition).

8. The composition according to any one of claims 1 to 7, wherein the content of the plasticizer is 1.3 to 35% by weight based on the total amount of the composition (excluding the propellant in the case of an aerosol composition).

9. The composition according to any one of claims 1 to 8, further containing a propellant.

10. The composition according to any one of claims 1 to 9, further containing light anhydrous silicic acid and / or titanium oxide.

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