Topical skin components

Abstract

To provide a topical skin composition that can be applied as an overcoat. [Solution] The present invention provides a topcoatable topical skin composition comprising a liquid composition containing a betamethasone ester, contained in a roll-on container having an application ball. The diameter of the application ball may be 3 mm to 25 mm. Furthermore, the roll-on container has a discharge port that exposes the top of the application ball to the outside, and the ratio of the diameter of the discharge port to the diameter of the application ball may be 1:1.1 to 1:1.6.

Description

Technical Field

[0001] The present invention relates to a composition for external use on the skin. More specifically, it relates to a coatable composition for external use on the skin.

Background Art

[0002] Conventionally, as an application container for applying a composition such as a drug to an application site, there is a container in which the application part is of a sponge type. However, it is known that wear and deterioration occur due to friction during application in such a container. As a means for solving this problem, there is a roll-on type container that applies the filled composition by rolling a ball.

[0003] Here, for example, Patent Document 1 discloses an aerosol container filled with a content containing a liquefied gas and having a stem at the upper end, and an application member provided on the upper part of the aerosol container. The application member includes a cylindrical main body having a rolling element holding part, a rolling element rotatably held in a state where a part thereof protrudes by the rolling element holding part, a base material attached to the stem and moving up and down together with the stem, and a liquid-retaining elastic body having air and liquid permeability disposed between the lower surface of the rolling element and the base material. A roll-on type coating device is disclosed.

[0004] Further, Patent Document 2 discloses an external anti-inflammatory and analgesic agent product including a liquid composition containing (A) an anti-inflammatory and analgesic component, (B) a lower alcohol, and (C) menthol, and the content of component (B) is 30 to 70% by mass, and a roll-on container having a metal coating ball filled with this liquid composition.

Prior Art Documents

Patent Documents

[0005]

Patent Document 1

Patent Document 2

Summary of the Invention

[0006] However, with roll-on type applicators, the contained composition is applied to the skin by rolling a ball, which means that sebum, dust, dirt, and cosmetics on the skin can potentially lead to contamination of the contained composition.

[0007] Therefore, in view of these circumstances, the main objective of the present invention is to provide a topical skin composition that can be applied as an overcoat. [Means for solving the problem]

[0008] As a result of diligent experimental research conducted by the inventors of this invention, it was discovered that by focusing on specific components, it is possible to apply the product to the skin even in a roll-on container, thus completing the present invention.

[0009] In other words, the present invention provides a topcoatable topical skin composition comprising a liquid composition containing a betamethasone ester, contained in a roll-on container having an application ball. In the topical skin composition according to the present invention, the diameter of the application ball may be 3 mm to 25 mm. In the topical skin composition according to the present invention, the roll-on container has a discharge port that exposes the upper part of the application ball outward, and the ratio of the diameter of the discharge port to the diameter of the application ball may be 1:1.1 to 1:1.6. In the topical skin composition according to the present invention, the application ball may be made of a thermoplastic resin. In this case, the thermoplastic resin may be polypropylene and / or polyethylene. In the topical skin composition according to the present invention, the betamethasone ester may be betamethasone valerate ester. [Effects of the Invention]

[0010] According to the present invention, it is possible to provide a topcoatable topical skin composition. The effects described herein are not necessarily limited to those described herein and may include any of the effects described herein. [Brief explanation of the drawing]

[0011] [Figure 1] This is a front view of the roll-on container 1 according to the present invention. [Figure 2] This is a front cross-sectional view of the roll-on container 1 according to the present invention. [Modes for carrying out the invention]

[0012] Hereinafter, preferred embodiments for carrying out the present invention will be described in detail with reference to the drawings. The embodiments described below are merely examples of typical embodiments of the present invention, and this should not be interpreted as narrowing the scope of the present invention.

[0013] <<Skin external composition>> The topical skin composition according to the present invention is characterized in that a liquid composition containing a betamethasone ester is contained in a roll-on container 1 having an application ball.

[0014] Generally, when applying topical skin compositions, the affected area is usually cleaned before use, but it is common for foreign substances that are difficult to remove to remain on the application site.

[0015] For example, if a cosmetic product is applied to the skin and then further applied using a roll-on container, the cosmetic product may mix with the liquid composition contained in the roll-on container, potentially leading to the following problems: UV absorbers and scattering agents used as components in the cosmetic product may react with components in the liquid composition contained in the roll-on container, inactivating the liquid composition and reducing its effectiveness. In addition, there is a risk that components of the cosmetic product may react with the liquid composition to form undesirable and harmful by-compositions.

[0016] In addition, there is a risk that the usability deteriorates due to impairment of the smoothness and uniformity of the liquid composition contained in the roll-on container. Furthermore, due to changes in color and transparency, there may be a sense of incongruity in the appearance of the liquid composition, or the odor of the liquid composition may change, causing discomfort. These are problems that can occur similarly, for example, even when sebum, dirt, and dust on the skin are mixed into the container.

[0017] On the other hand, the skin external composition according to the present invention has the above-described characteristics, so that even if there is sebum, dust, dirt, cosmetics, etc. on the skin, it is possible to apply it without卷入 them into the container. Therefore, it is possible to prevent the deterioration of the above-described active ingredient and the generation of harmful substances. In addition, the above-described changes in usability, appearance, and odor can be similarly suppressed.

[0018] In the present invention, the "foreign matter" refers to substances other than the liquid composition contained in the roll-on container. Specifically, for example, sebum, dust, dirt, cosmetics, etc. on the skin described above can be mentioned, but the present invention is not limited thereto.

[0019] Also, when the foreign matter is fine particles such as talc, the skin external composition according to the present invention can prevent the fine particles from being mixed into the container even if the fine particles have a particle size (d50) of 15 μm or less, as shown in the examples described later.

[0020] <Betamethasone ester> It should be noted that the word "卷入" in the translation of is probably a misspelling in the original text. It might be intended to be something like "entering" or "mixing in". The translation is adjusted as best as possible based on the context.Betamethasone ester is a synthetic corticosteroid (steroid) and a drug with anti-inflammatory and immunosuppressive effects. Specifically, "betamethasone ester" refers to ester derivatives of betamethasone (for example, carboxylic acid esters such as acetate, pivalate, propionate, butyrate, valerate, etc.; phosphate esters, etc.) and salts thereof (for example, alkali metal salts such as sodium salt, potassium salt, etc.) and one or more selected from the group consisting of their solvates (for example, hydrates, etc.). More specifically, examples of betamethasone esters include components listed in the 18th revised Japanese Pharmacopoeia such as betamethasone valerate, betamethasone dipropionate, betamethasone butyrate propionate, sodium betamethasone phosphate, etc. These may be used alone or in combination of two or more. In the present invention, among these, betamethasone valerate is particularly preferred.

[0021] The amount of betamethasone ester contained in the liquid composition contained in the topical skin composition according to the present invention is not particularly limited and can be appropriately adjusted according to the intended use and purpose. However, as the lower limit value of betamethasone ester contained in the liquid composition, for example, it can be 0.01% by mass or more, preferably 0.05% by mass or more, more preferably 0.1% by mass or more. Also, as the upper limit value of betamethasone ester contained in the liquid composition, for example, it can be 3% by mass or less, preferably 1% by mass or less, more preferably 0.5% by mass or less.

[0022] <Use> The topical skin composition according to the present invention can be suitably used to treat (including improving) or prevent skin diseases. The skin diseases are not particularly limited as long as betamethasone ester can act as an active ingredient, but for example, it can be used as an antipruritic and anti-inflammatory agent, a topical hemorrhoid agent, etc. More specifically, it can be used as an antipruritic and anti-inflammatory agent for symptoms such as eczema, dermatitis, sores, heat rash, rashes, itching, chilblains, insect bites, and hives; and it can be suitably used to treat or prevent pain, itching, swelling, bleeding, and sores associated with anal fissures and hemorrhoids.

[0023] <Liquid composition> The present invention relates to a topical skin composition, which is in the form of a liquid and can be prepared by compounding it with a base component suitable for a liquid.

[0024] Any of the conventionally known substances used for such purposes can be used as the base for the liquid formulation contained in the topical skin composition according to the present invention. Specifically, for example, hydrocarbons such as white petrolatum, gelling hydrocarbons, paraffin, liquid paraffin, α-olefin oligomers and squalane, higher fatty acids such as lauric acid, myristic acid, palmitic acid, stearic acid, behenic acid, oleic acid, linoleic acid, linolenic acid, 12-hydroxystearic acid, lanolin fatty acid, and isostearic acid, higher fatty alcohols such as 2-hexyldecanol and 2-octyldodecanol, diisobutyl adipate, diisopropyl adipate, adipate polyester, and oleate Fatty acid ester oils such as sil, diisopropyl sebacate, diethyl sebacate, isopropyl palmitate, cetyl palmitate, isopropyl myristate, octyldecyl myristate, hexyl laurate, isopropyl linoleate, ethyl linoleate, propylene glycol monostearate, propylene glycol dioleate, cetyl 2-ethylhexanoate, medium-chain triglycerides, glycerin triisooctanoate, triacetin, and polyhydric alcohol fatty acids such as tri(caprylic / capric acid) glycerin. Higher fatty alcohols such as sterol, cetanol, stearyl alcohol and behenyl alcohol, glyceryl monostearate, glyceryl monooleate, sorbitan monostearate, sorbitan monooleate, sorbitan sesquioleate, polyoxyethylene sorbitan monostearate, polyoxyethylene sorbitan monooleate, polyoxyethylene sorbitan tetrastearate, polyoxyethylene sorbitan tetraoleate, polyoxyethylene castor oil, polyoxyethylene hydrogenated castor oil, polyethylene glycol monostearate, polyethylene glycol monooleate, nonionic surfactants such as polyoxyethylene lauryl ether, polyoxyethylene cetyl ether and polyoxyethylene oleyl ether, ionic surfactants such as sodium lauryl sulfate and sodium cetyl sulfate, carboxyvinyl polymer, hydroxypropyl cellulose, hydrophobized hydroxypropyl methylcellulose, acrylic starch 300, polyvinylpyrrolidone and sodium hyaluronate, and other polymer compounds.Examples of suitable ingredients include polyhydric alcohols such as glycerin, propylene glycol, 1,3-butylene glycol, and macrogol 400; pH adjusters such as diisopropanolamine, sodium hydroxide, potassium dihydrogen phosphate, and sodium hydrogen phosphate; stabilizers such as sodium chloride, sodium thiosulfite, sodium sulfite, and sodium edetate; preservatives such as methylparaben, propylparaben, benzalkonium chloride, and benzethonium chloride; and humectants such as urea, sucrose, D-sorbitol, and lactic acid. Lower alcohols such as ethanol and isopropanol are also used. These may be used individually or in combination of two or more, but the present invention is not limited to these.

[0025] The method for preparing the liquid composition contained in the topical skin composition according to the present invention is not particularly limited and can be prepared using generally known preparation methods. Specifically, for example, when preparing a liquid formulation, the above-mentioned components and a medium such as water are mixed together, but there are no particular restrictions on the mixing ratio. For example, it can be prepared by mixing in the following ranges: water 0-80% by mass, hydrocarbons 0-99% by mass, higher fatty acids 0-25% by mass, fatty acid ester oils 0-50% by mass, polyhydric alcohol fatty acid esters 0-30% by mass, polymer compounds 0-10% by mass, polyhydric alcohols 0-30% by mass, pH adjusters 0-10% by mass, stabilizers 0-10% by mass, preservatives 0-5% by mass, humectants 0-40% by mass, surfactants 0-10% by mass, 0-80% by mass, etc.

[0026] Furthermore, the amount and method of use of the topical skin composition according to the present invention are not particularly limited, and it can be used in the usual amounts used for conventional pharmaceuticals and quasi-drugs used to treat various symptoms and diseases.

[0027] The application site for the topical skin composition according to the present invention is the skin (including the scalp), and it can be suitably applied to areas accompanied by skin diseases. Furthermore, the topical skin composition according to the present invention is preferably a topical skin application formulation.

[0028] <Other drugs> The topical skin composition according to the present invention may contain other drugs besides betamethasone ester, to the extent that they do not interfere with the effects of the present invention. Other drugs include, for example, anti-inflammatory agents such as bufexamac, ufenamate, ibuprofen piconol, indomethacin, felbinac, ketoprofen, piroxicam, diclofenac sodium, loxoprofen sodium, glycyrrhetinic acid, glycyrrhizic acid and its salts, Angelica acutiloba extract and Lithospermum erythrorhizon extract; fat-soluble vitamins such as retinol acetate, retinol palmitate, ascorbic acid palmitate, tocopherol acetate, ergocalciferol, and tacasitol; water-soluble vitamins such as ascorbic acid, pyridoxine hydrochloride, and nicotinamide; and isopropyl Examples of disinfectants include methylphenol, chlorhexidine hydrochloride, benzethonium chloride, benzalkonium chloride, and cetrimide; local anesthetics such as lidocaine and its salts, dibucaine and its salts, procaine and its salts, tetracaine and its salts, and ethyl aminobenzoate; cooling agents such as l-menthol, dl-camphor, peppermint oil, and borneol; vasoconstrictors such as naphazoline hydrochloride, tetrahydrozoline hydrochloride, and methyl ephedrine hydrochloride; redness-inducing agents such as benzyl nicotinate, nonyl vanillylamide, and capsicum tincture; and astringents such as tannic acid. However, the present invention is not limited to these.

[0029] <Roll-on container 1> The roll-on container 1 used for a topical skin preparation according to the present invention has an application ball 11. The roll-on container 1 equipped with the application ball 11 is such that the application ball 11 is rotatably held, and when the application ball 11 is pressed against the area to be applied and rolled, the liquid composition contained in the container is applied to the area to be applied.

[0030] In this invention, "container" refers to a packaging body that directly contains a liquid composition. The shape of the roll-on container 1 itself is not particularly limited as long as it can contain the liquid composition, and can be appropriately designed according to the specific properties of the liquid composition, administration route, application, etc.

[0031] Furthermore, the material used to form the roll-on container 1 is not particularly limited and can be appropriately selected depending on its compatibility with the liquid composition to be contained, the shape of the container, etc. Specifically, examples include glass, plastic, cellulose, pulp, rubber, etc., but resin is preferred from the viewpoint of processability, durability, etc. As for the resin, it is preferable to use a thermoplastic resin, whether it is a synthetic resin or a natural resin. Specifically, examples include polyolefin resins, polyester resins, polyphenylene ether resins, polycarbonate resins, polysulfone resins, polyamide resins, polyvinyl chloride resins, styrene resins, etc., and these may be used individually, in combination of two or more, or as a mixture thereof (polymer alloy).

[0032] The shape of the coating ball 11 is not particularly limited, but from the viewpoint of facilitating rotation, it is preferable that it be a perfect sphere or nearly perfect sphere. Also, in the roll-on container 1, the number of coating balls 11 may be one or multiple.

[0033] The lower limit of the diameter L1 of the coating ball 11 (see Figure 2) is preferably 3 mm or more, more preferably 5 mm or more, and even more preferably 7.5 mm or more. The upper limit of the diameter L1 of the coating ball 11 is preferably 25 mm or less, more preferably 15 mm or less, and even more preferably 12.5 mm or less. By setting the diameter of the coating ball to 3 mm to 25 mm, the inclusion of foreign matter (e.g., sebum, dust, dirt, cosmetics, etc.) into the container can be further suppressed, and the topcoat can be applied more effectively.

[0034] Furthermore, in the present invention, the roll-on container 1 has a discharge port 10 that exposes the upper part of the coating ball 11 to the outside, and the ratio of the hole diameter L2 of the discharge port 10 (see Figure 2) to the diameter L1 of the coating ball 11 (=L2:L1) is preferably 1:1.1 to 1:1.6, more preferably 1:1.1 to 1:1.4, and even more preferably 1:2 to 1:3. By setting the ratio of the hole diameter L2 of the discharge port 10 to the diameter L1 of the coating ball 11 to 1:1.1 to 1:1.6, the entrapment of foreign matter into the container can be further suppressed, and the topcoat can be applied more effectively.

[0035] The lower limit of the hole diameter L2 of the discharge port 10 is preferably 2 mm or more, more preferably 4 mm or more, and even more preferably 6.5 mm or more. The upper limit of the hole diameter L2 of the discharge port 10 is preferably 22 mm or less, more preferably 16 mm or less, and even more preferably 9.5 mm or less.

[0036] Examples of materials for forming the coated balls 11 include metals and resins. Examples of metals include iron, steel, and stainless steel. The metals may be surface-treated as needed. Examples of surface treatments include corrosion-resistant treatment and rust-preventive treatment. As for resins, examples include those mentioned above, so their explanation will be omitted here.

[0037] In the present invention, the material used to form the coated ball 11 is preferably a resin, and among resins, a thermoplastic resin is preferred. Furthermore, among thermoplastic resins, a polyolefin resin is particularly preferred.

[0038] Examples of polyolefin resins include polypropylene (PP), polyethylene (PE), and polybutylene (PB). In the present invention, among polyolefin resins, polypropylene and / or polyethylene are particularly preferred as the material for forming the coated ball 11. Polypropylene and / or polyethylene have a high affinity for betamethasone esters (especially betamethasone valerate), which can further suppress the incorporation of foreign matter into the container and allow for more effective topcoating.

[0039] Furthermore, the present invention can also employ the following embodiments. [1] A stain-resistant agent containing betamethasone ester as the active ingredient. [2] An antifouling agent for coating balls, comprising a liquid composition containing a betamethasone ester, contained in a roll-on container having a coating ball. [3] A method for preventing contamination of the application ball in a roll-on container using betamethasone ester. [4] A foreign body entrapment inhibitor containing betamethasone ester as the active ingredient. [5] A foreign matter entanglement inhibitor for roll-on containers, comprising a liquid composition containing a betamethasone ester, contained in a roll-on container having a coating ball. [6] A method for suppressing the entrapment of foreign matter by a coating ball in a roll-on container using betamethasone ester. [Examples]

[0040] The present invention will be described in more detail below based on examples. The embodiments described below are merely examples of typical embodiments of the present invention, and this should not be interpreted as narrowing the scope of the present invention.

[0041] <<Test Example 1>> The liquid compositions described in Table 1 below (Example 1 and Comparative Example 1) were prepared. The topcoat effect of these compositions, when applied as a base coat to a sunscreen cosmetic with the component composition described in Table 2 below, was evaluated using the transmittance measurement test described below. Note that in Tables 1 and 2 below, the content of each component is expressed in "mass percent".

[0042] <Transmittance Measurement Test> As a substitute for skin, artificial leather (Sapura®; manufactured by Idemitsu Technofine Co., Ltd.) was used. 0.2g of sunscreen cosmetic (Sunscreen Milk UV Mild; manufactured by Chifure Cosmetics Co., Ltd.) was applied to a 10cm square piece of artificial leather and dried. After drying, the liquid composition was applied back and forth over a 10cm area using a roll-on container of the topical skin composition. After shaking, the transmittance (wavelength: 480nm) was measured, and the transmittance was compared to that of a roll-on container containing 100% ethanol, which was used as a control. A lower transmittance indicates that the sunscreen cosmetic components are trapped within the container.

[0043] [Table 1]

[0044] [Table 2]

[0045] <Consideration> Compared to the topical skin composition of Comparative Example 1, the topical skin composition of Example 1, in which betamethasone ester was contained in a roll-on container, showed excellent permeability. Therefore, it was found that a topical skin composition containing a liquid composition of betamethasone ester, contained in a roll-on container with an application ball, can be applied as a topcoat even when cosmetics or other ingredients other than betamethasone ester are applied to the substrate.

[0046] <<Test Example 2>> The liquid compositions described in Tables 3 and 4 below (Examples 2-4 and Comparative Examples 2-4) were prepared. The topcoat effect of these compositions was evaluated using the transmittance measurement test described below, when talc (Crown Talc Pharmacopoeia PP; manufactured by Matsumura Sangyo Co., Ltd.; particle size (d50) is 14.0 μm) was applied as a base coat. Note that in Tables 3 and 4 below, the content of each component is expressed in "mass percent".

[0047] <Transmittance Measurement Test> The test was conducted using the same method as in Test Example 1, except that the sunscreen cosmetic was replaced with talc.

[0048] [Table 3]

[0049] [Table 4]

[0050] <Consideration> Compared with the topical skin compositions of Comparative Examples 2-4, the topical skin compositions of Examples 2-4, in which betamethasone ester was contained in a roll-on container, showed excellent permeability even when the diameter of the discharge port, the diameter of the application ball, and the material of the application ball were changed. Therefore, it was found that a topical skin composition containing a liquid composition of betamethasone ester contained in a roll-on container with an application ball can be applied as a topcoat even when fine particles other than betamethasone ester, such as talc, are applied to or attached to the substrate.

[0051] The following are examples of formulations for topical skin compositions related to this technology. Note that the units of the values ​​in Table 5 below are "mass%".

[0052] <Manufacturing Examples 1-9 (Examples of Liquid Formulations)> The topical skin compositions listed in Table 5 below were prepared by conventional methods and converted into liquid formulations.

[0053] [Table 5] [Industrial applicability]

[0054] The topical skin composition according to the present invention can be applied as a topcoat even if there is a cosmetic base coat or if there are foreign substances on the skin such as sebum, dust, dirt, or cosmetic products, without incorporating these into the container. Therefore, the present invention is extremely useful, for example, in the pharmaceutical industry. [Explanation of symbols]

[0055] 1: Roll-on container 10:Discharge port 11: Coating ball L1: Diameter of the application ball L2: Diameter of the discharge port

Claims

1. A topcoatable topical skin composition comprising a liquid composition containing a betamethasone ester, contained in a roll-on container having an application ball.

2. The skin external composition according to claim 1, wherein the diameter of the application ball is 3 mm to 25 mm.

3. The roll-on container has a discharge port that exposes the upper part of the coating ball to the outside, The topical skin composition according to claim 1, wherein the ratio of the diameter of the discharge port to the diameter of the application ball is 1:1.1 to 1:1.

6.

4. The topical skin composition according to claim 1, wherein the application ball is made of a thermoplastic resin.

5. The skin composition according to claim 4, wherein the thermoplastic resin is polypropylene and / or polyethylene.

6. The topical skin composition according to claim 1, wherein the betamethasone ester is betamethasone valerate.

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