Lip components

A lip composition with an oily base and ascorbyl tetrahexyldecanoate addresses lip dullness and wrinkles by enhancing transdermal absorption, resulting in improved lip appearance and health.

JP7784224B2Active Publication Date: 2025-12-11KOBAYASHI PHARMA CO LTD
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Patent Information

Application Number
JP2018240097
Authority / Receiving Office
JP · JP
Patent Type
Patents
Current Assignee / Owner
Filing Date
2018-12-21
Publication Date
2025-12-11
Estimated Expiration
2038-12-21

AI Technical Summary

Technical Problem

Lips are inherently sensitive and prone to dullness due to low melanocyte count and exposure to external factors, yet existing lip compositions do not effectively address this issue.

Method used

A lip composition containing an oily base and ascorbyl tetrahexyldecanoate, which improves dullness by enhancing transdermal absorption and efficacy despite the absence of sebum on the lips.

Benefits of technology

The composition significantly improves lip dullness, uniformity, and reduces wrinkles, providing a healthier lip appearance.

✦ Generated by Eureka AI based on patent content.

Smart Images

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Patent Text Reader

Abstract

To provide a composition for lips capable of improving dullness of lips.SOLUTION: There is provided a composition for lips comprising an oily base in which an effect of improving dullness of lips can be imparted to a composition for lips by blending ascorbyl tetrahexyldecanoate. Preferably, the composition for lips comprises at least any one selected from the group consisting of allantoins, pyridoxines and panthenols and comprises glycyrrhetic acids and / or tocopherols.SELECTED DRAWING: None
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Description

[Technical Field]

[0001] The present invention relates to a lip composition. More specifically, the present invention relates to a lip composition that has the effect of improving lip dullness. [Background technology]

[0002] The lips are formed by the outward inversion of the labial mucosa in the oral cavity, and are usually referred to anatomically as the vermilion border. Thus, the lips are fundamentally different from normal skin on the face or body in that their basic structure is mucous membrane rather than skin. For example, the lips have tissue characteristics such as the absence of sebaceous glands present in normal skin, only scattered sebaceous glands present and virtually no fat present on the stratum corneum, an extremely thin stratum corneum compared to normal skin, and a marked lack of melanocytes. Furthermore, the lips also have morphological characteristics in that, despite being mucous membrane tissue, they are exposed to the outside of the body and are constantly exposed to the external environment.

[0003] Due to the overlap of these histological and morphological characteristics, lips are inherently very sensitive and prone to problems, which is a unique problem. For this reason, external compositions applied to lips (lip compositions) are characterized by containing a very large amount of an oily base such as petrolatum, which protects the stratum corneum of the lips by forming an oil film.

[0004] It is known that in general topical compositions, the transdermal absorbability of a drug (distribution into the stratum corneum) is significantly affected by the "affinity between the base and the skin" (ease of the base blending with the skin) and the "affinity between the base and the drug" (ease of dissolving the drug in the base) (Non-Patent Document 1), and the formulation of a topical skin composition is designed taking these two factors into consideration. For example, in the case of a water-soluble drug, the use of an oily base improves both "transdermal absorbability due to the affinity between the base and the skin" and "transdermal absorbability due to the affinity between the base and the drug," while the use of a water-soluble base reduces both "transdermal absorbability due to the affinity between the base and the skin" and "transdermal absorbability due to the affinity between the base and the drug." In addition, in the case of fat-soluble drugs, it is known that the use of an oily base improves "transdermal absorbability due to the affinity between the base and the skin" but decreases "transdermal absorbability due to the affinity between the base and the drug," while the use of a water-soluble base decreases "transdermal absorbability due to the affinity between the base and the skin" but improves "transdermal absorbability due to the affinity between the base and the drug."

[0005] Therefore, in lip compositions that use a large amount of oily bases, water-soluble drugs, which have improved "transdermal absorbability due to the affinity between the base and the skin" and "transdermal absorbability due to the affinity between the base and the drug," are more advantageous in terms of transdermal absorption than fat-soluble drugs, which have reduced "transdermal absorbability due to the affinity between the base and the drug."

[0006] On the other hand, L-ascorbic acid is a water-soluble drug known to exhibit beneficial effects on skin, such as its excellent melanin production inhibitory effect and reducing properties against produced melanin, and has traditionally been incorporated into topical compositions. However, L-ascorbic acid has a structure that easily donates hydrogen due to its enediol group, and its susceptibility to oxidation makes it unstable in formulations. To address these issues of poor oil solubility and formulation stability, L-ascorbic acid ester derivatives, in which the hydroxyl groups of L-ascorbic acid are esterified, have been developed. However, as described in Patent Document 1, L-ascorbic acid ester derivatives are insufficiently effective in improving poor oil solubility and formulation stability due to the remaining hydroxyl groups at the 2- and 3-positions. Therefore, L-ascorbic acid tetra-branched fatty acid ester derivatives, in which all hydroxyl groups of L-ascorbic acid are esterified, have been developed, thereby improving oil solubility. Patent Document 1 also describes that L-ascorbic acid tetra-branched fatty acid ester derivatives are easily absorbed transdermally through the stratum corneum. Patent Document 1 discloses that the whitening effect is improved by using L-ascorbyl tetra-2-hexyldecanoate as an L-ascorbic acid tetra-branched fatty acid ester derivative in combination with arbutin, kojic acid, tranexamic acid, dipotassium glycyrrhizinate, magnesium L-ascorbyl phosphate, and 2-O-α-glucosyl-L-ascorbic acid. L-ascorbyl tetra-2-hexyldecanoate has a structure in which isopalmitic acid, a sebaceous fatty acid, is bonded to L-ascorbic acid. [Prior art documents] [Patent documents]

[0007] [Patent Document 1] Japanese Patent Application Laid-Open No. 2003-306419 [Non-patent literature]

[0008] [Non-Patent Document 1] Edited by Michiteru Otani, "Topical Medicine Trivia Vol. 1," [online], Maruho Co., Ltd., [Retrieved November 30, 2018], Internet <URL: https: / / www.maruho.co.jp / medical / pharmacist / infostore / vol01 / 05.html> Summary of the Invention [Problem to be solved by the invention]

[0009] Lips are inherently highly sensitive and have the unique problem of being prone to problems. One example of such a problem is lip dullness. Lips have a significantly low number of melanocytes and are easily exposed to external factors such as ultraviolet rays, so they become dull due to direct damage from external factors. While the entire face is often treated with lotions and creams, the lips are not given appropriate care, which exacerbates the problem of lip dullness. However, no lip compositions capable of improving dullness have been investigated to date.

[0010] Therefore, an object of the present invention is to provide a lip composition that can improve lip dullness. [Means for solving the problem]

[0011] Lip compositions differ significantly in base composition from compositions normally applied to the skin in that they use a large amount of oily base. Furthermore, in light of common technical knowledge regarding transdermal absorption, even the same medicinal ingredient will have varying transdermal absorbability depending on the type of base. Naturally, differences in transdermal absorbability affect the effects exhibited. Therefore, in light of common technical knowledge regarding transdermal absorbability, even if a medicinal ingredient can exert its effects when incorporated into a topical composition normally applied to the skin, it cannot be said that the same effects can be expected in a lip composition.

[0012] As mentioned above, L-ascorbyl tetra-2-hexyldecanoate is used in topical compositions as a useful skin-beautifying ingredient. However, no topical compositions specifically for use on the lips containing L-ascorbyl tetra-2-hexyldecanoate are known; only those intended for normal skin are known. Given that L-ascorbyl tetra-2-hexyldecanoate is formulated to be more oil-soluble, its transdermal absorption should be lower when incorporated into an oily base. Given common general knowledge regarding transdermal absorption, its use in lip compositions would not provide the benefits previously touted in conventional topical skin compositions. Patent Document 1 also describes how L-ascorbic acid tetra-branched fatty acid ester derivatives are readily absorbed transdermally through the stratum corneum. However, this ease of transdermal absorption is due to the fact that the L-ascorbic acid tetra-branched fatty acid ester derivatives contain isopalmitic acid, a sebaceous fatty acid, in their molecules, which allows them to have affinity with sebum present on the skin to which they are applied. Since there is essentially no sebum on the lips, the effect of affinity with sebum, as seen in normal skin, cannot be expected. In other words, even if L-ascorbic acid tetra-branched fatty acid ester derivatives are known to facilitate percutaneous absorption, their incorporation into a lip composition cannot be expected to facilitate percutaneous absorption, as can be expected from normal compositions for external use on the skin.

[0013] Under these circumstances, the present inventors conducted extensive research and surprisingly found that by incorporating L-ascorbyl tetra-2-hexyldecanoate into a lip composition, which is not expected to be effective in lip compositions in light of common technical knowledge, dullness of the lips can be significantly improved.The present invention was completed through further research based on this finding.

[0014] That is, the present invention provides the following aspects. Item 1. A lip composition containing (A) an oily base and (B) ascorbyl tetrahexyldecanoate, which is used to improve dullness of the lips. Item 2. The lip composition according to Item 1, wherein the content of the component (A) is 50 to 99.5% by weight. Item 3. The lip composition according to Item 1 or 2, wherein the component (A) includes a solid oil. Item 4. The lip composition according to Item 3, wherein the content of the solid oil is 30 to 70% by weight. Item 5. The lip composition according to any one of Items 1 to 4, further comprising at least one selected from the group consisting of allantoins, pyridoxines, and panthenols. Item 6. The lip composition according to any one of Items 1 to 5, further comprising glycyrrhetinic acids and / or tocopherols. Item 7. A method for imparting an effect of improving lip dullness to a lip composition, characterized by blending ascorbyl tetrahexyldecanoate in a lip composition containing an oily base. [Effects of the Invention]

[0015] The lip composition of the present invention can improve dullness of the lips. [Brief explanation of the drawings]

[0016] [Figure 1] 1 shows the measurement results showing the effect of the lip composition of Test Example 1 in improving the unevenness of melanin (effect of improving dullness). [Figure 2] 1 shows the measurement results showing the effect of the lip composition of Test Example 1 in improving the average melanin concentration (effect of improving dullness). [Figure 3] 1 shows the measurement results showing the effect of the lip composition of Test Example 1 in improving the roughness of the lip surface texture (effect of improving lip wrinkles). [Figure 4] 1 shows the measurement results showing the effect of the lip composition of Test Example 1 in improving the depth of lip wrinkles (lip wrinkle improving effect). [Figure 5] 1 is a photograph of lips (enlarged photograph of the lower lip) showing the effect of improving dullness and lip wrinkles by the lip composition of Test Example 2. DETAILED DESCRIPTION OF THE INVENTION

[0017] 1. Lip composition The lip composition of the present invention is characterized by containing (A) an oily base (hereinafter also referred to as component (A)) and (B) ascorbyl tetrahexyldecanoate (hereinafter also referred to as (B)), and is used to improve dullness of the lips. The lip composition of the present invention will be described in detail below.

[0018] (A) Oily base The lip composition of the present invention contains an oily base as component (A). Because oily bases have a strong affinity with oil-soluble drugs, they inherently result in poor transdermal penetration and poor efficacy of the oil-soluble drugs, but the lip composition of the present invention, despite containing an oily base, can achieve a significant improvement effect on lip dullness.

[0019] Examples of oily bases include (A1) solid oil and (A2) liquid oil. Furthermore, it is preferable that the oily base contains at least a solid oil. When the oily base contains a solid oil, the fluidity is either zero or extremely poor, which is preferable in that it facilitates the adhesion of the oil film of the lip composition to the localized area, the lips. On the other hand, in an oily base with no or extremely poor fluidity, the dispersibility of oil-soluble drugs is inherently poor, resulting in poor transdermal distribution of the oil-soluble drug and poor efficacy. However, the lip composition of the present invention can achieve a significant improvement in lip dullness even when the oily base contains a solid oil.

[0020] (A1) solid oil (hereinafter also referred to as component (A1)) is an oil that maintains a solid form at 25° C. The solid oil used in the present invention may be any oil that is typically used in cosmetics, topical medicines, etc., and examples thereof include solid fats and oils, waxes, synthetic waxes, solid hydrocarbons, higher alcohols, and higher fatty acids. Examples include solid fats and oils such as cocoa butter, lanolin, ozokerite, hydrogenated jojoba oil, and hydrogenated castor oil; waxes such as candelilla wax, rice bran wax, beeswax, white beeswax, cotton wax, carnauba wax, shellac wax, Japan wax, and jojoba wax; synthetic waxes such as myristyl myristate, cetyl myristate, stearyl stearate, cetyl stearate, cetyl palmitate, cholesteryl stearate, cholesteryl oleate, dextrin palmitate, and inulin stearate; solid hydrocarbons such as petrolatum, polyethylene wax, paraffin wax, ceresin wax, microcrystalline wax, and gelled hydrocarbons; higher alcohols such as cetyl alcohol, stearyl alcohol, behenyl alcohol, and batyl alcohol; higher fatty acids such as lauric acid, myristic acid, palmitic acid, stearic acid, behenic acid, 12-hydroxystearic acid, and undecylenic acid; and silicone wax.

[0021] Among these solid oils, solid fats and oils, waxes, synthetic waxes, and solid hydrocarbons are preferred in that they provide a more favorable effect of improving lip dullness; waxes and solid hydrocarbons are more preferred; white beeswax, petrolatum, microcrystalline wax, and gelled hydrocarbons are even more preferred; and petrolatum and microcrystalline wax are particularly preferred.

[0022] These solid oils may be used alone or in combination of two or more.

[0023] (A2) Liquid oil (hereinafter also referred to as component (A2)) is an oil that remains in a liquid state at 25°C. The liquid oil used in the present invention may be any oil commonly used in cosmetics, topical pharmaceuticals, etc., and examples thereof include vegetable oils such as avocado oil, camellia oil, macadamia nut oil, olive oil, and jojoba oil; fatty acids such as oleic acid and isostearic acid; ester oils such as cetyl ethylhexanoate, ethylhexyl palmitate, octyldodecyl myristate, neopentyl glycol diethylhexanoate, glyceryl tri-2-ethylhexanoate, octyldodecyl oleate, isopropyl myristate, glyceryl triisostearate, and glyceryl di-methylmethoxycinnamate-monoethylhexanoate; silicone oils such as dimethylpolysiloxane, methylhydrogenpolysiloxane, methylphenylpolysiloxane, and octamethylcyclotetrasiloxane; and liquid hydrocarbon oils such as liquid paraffin, squalene, and squalane.

[0024] Among these liquid oils, preferred are liquid hydrocarbon oils, and more preferred are liquid paraffins.

[0025] These liquid oils may be used alone or in combination of two or more.

[0026] The content of component (A) in the lip composition of the present invention is not particularly limited, as long as it occupies a relatively large proportion in the lip composition, but is preferably 50 to 99.5% by weight, more preferably 60 to 99.5% by weight, even more preferably 70 to 99.5% by weight, and even more preferably 75 to 99.5% by weight. In topical compositions containing a majority of an oily base, the transdermal penetration and efficacy of oil-soluble drugs are inherently further impaired. However, the lip composition of the present invention, even if it contains a majority of an oily base, can achieve a significant improvement in lip dullness.

[0027] Furthermore, when the lip composition of the present invention contains component (A1), the content of component (A1) in the lip composition is not particularly limited. From the viewpoint of better adhesion of the oil film of the lip composition to the lips and the feel when used, for example, 30 to 70% by weight, preferably 30 to 65% by weight, more preferably 30 to 60% by weight, even more preferably 40 to 60% by weight, and even more preferably 50 to 60% by weight. Lip compositions containing such a large amount of solid oil have no or very poor fluidity, which inherently reduces the dispersibility of oil-soluble drugs, further worsening the transdermal distribution of the oil-soluble drug and the manifestation of its efficacy. However, the lip composition of the present invention can achieve a significant improvement in lip dullness, even when containing a large amount of solid oil.

[0028] When the lip composition of the present invention contains the component (A2), the content thereof is not particularly limited, but may be, for example, 15 to 60% by weight, preferably 20 to 55% by weight, and more preferably 20 to 50% by weight.

[0029] Furthermore, when the lip composition of the present invention contains both the component (A1) and the component (A2), the ratio of the component (A1) to the component (A2) is determined by the content of each of the above components, and the content of the component (A1) per 1 part by weight of the component (A2) is, for example, 0.5 to 3.5 parts by weight, preferably 0.5 to 3 parts by weight, and more preferably 1 to 3 parts by weight.

[0030] (B) Ascorbyl tetrahexyldecanoate The lip composition of the present invention contains ascorbyl tetrahexyldecanoate as component (B). Ascorbyl tetrahexyldecanoate is an L-ascorbic acid derivative in which all hydroxyl groups of L-ascorbic acid are esterified with isopalmitic acid (2-hexyldecanoic acid), and refers to L-ascorbyl tetra-2-hexyldecanoate (ascorbyl tetraisopalmitate).

[0031] Because ascorbyl tetrahexyldecanoate has a very strong affinity with oily bases, topical compositions containing oily bases inherently have poor percutaneous penetration and poor efficacy, but the lip composition of the present invention can achieve a significant improvement in lip dullness. Furthermore, ascorbyl tetrahexyldecanoate contains isopalmitic acid, a sebaceous fatty acid, in its molecule, which inherently improves efficacy by affinity with sebum present on the skin to which it is applied. However, because the lips to which the lip composition of the present invention is applied are essentially free of sebum, the affinity with sebum that is seen on normal skin cannot be expected. However, the lip composition of the present invention can achieve a significant improvement in lip dullness.

[0032] The content of component (B) in the lip composition of the present invention is not particularly limited and can be set appropriately depending on the desired effect of improving lip dullness, but examples include 0.5 to 5 parts by weight, preferably 0.7 to 4 parts by weight, and more preferably 1 to 3 parts by weight.

[0033] The ratio of component (A) to component (B) is determined by the content of each of the above components, and the content of component (B) per 100 parts by weight of component (A) can be, for example, 1 to 4.5 parts by weight. The lip composition of the present invention can achieve a significant improvement effect on lip dullness, so even if the content of component (B) per 100 parts by weight of component (A) is, for example, 1 to 3 parts by weight, 1 to 2.5 parts by weight, 1 to 2 parts by weight, or 1 to 1.5 parts by weight, the significant improvement effect on lip dullness can be effectively achieved.

[0034] When component (A) contains component (A1), the ratio of component (A1) to component (B) is determined by the content of each of the above components, but the content of component (B) per 100 parts by weight of component (A1) is, for example, 1.5 to 7.5 parts by weight, preferably 2 to 7.5 parts by weight. The lip composition of the present invention can provide a significant improvement effect on lip dullness, so even if the content of component (B) per 100 parts by weight of component (A1) is, for example, 1.5 to 6 parts by weight, 1.5 to 5 parts by weight, 1.5 to 4 parts by weight, 1.5 to 3 parts by weight, or 1.5 to 2.5 parts by weight, the significant improvement effect on lip dullness can be effectively obtained.

[0035] (C) Allantoins, pyridoxines, and / or panthenols The lip composition of the present invention can further contain, as component (C), at least one selected from the group consisting of allantoins, pyridoxines, and panthenols. These components are water-soluble and have good transdermal absorption when used with an oily base. In the lip composition of the present invention, in combination with ascorbyl tetrahexyldecanoate, the lip composition can improve the effect of improving lip dullness.

[0036] The lip composition of the present invention may contain one or more of allantoins, pyridoxines, and panthenols, either singly or in combination. From the viewpoint of obtaining a more effective effect of improving lip dullness, it is preferable that the composition contains all of the above-mentioned allantoins, pyridoxines, and panthenols.

[0037] The allantoins are allantoin and its derivatives, and specifically include allantoin, allantoin chlorhydroxyaluminum, allantoin hydroxyaluminum, etc. Among these allantoins, allantoin is preferred. These allantoins may be used alone or in combination of two or more.

[0038] When the lip composition of the present invention contains allantoins, the content of the allantoins in the lip composition is, for example, 0.01 to 2% by weight, and preferably 0.3 to 1% by weight.

[0039] Pyridoxines are vitamin B6, its derivatives, and their salts, specifically pyridoxine, pyridoxal, pyridoxamine, and inorganic acid salts thereof (e.g., hydrochloride, sulfate, nitrate, hydrobromide, phosphate, etc.). Among these pyridoxines, pyridoxine hydrochloride is preferred. These pyridoxines may be used alone or in combination of two or more.

[0040] When the lip composition of the present invention contains a pyridoxine, the content of the pyridoxine in the lip composition is, for example, 0.01 to 2% by weight, and preferably 0.05 to 0.5% by weight.

[0041] Panthenols include panthenol, its derivatives, and salts thereof, and specific examples thereof include panthenol, pantothenyl ethyl ether, alkaline earth metal pantothenate salts (e.g., calcium salt, etc.), alkali metal pantothenate salts (e.g., sodium salt, etc.), acetylpantothenyl ethyl ether, etc. Among these panthenols, panthenol is preferred. These panthenols may be used alone or in combination of two or more.

[0042] When the lip composition of the present invention contains panthenols, the content of panthenols in the lip composition is, for example, 0.01 to 5% by weight, and preferably 0.1 to 2% by weight.

[0043] (D) Glycyrrhetinic acids and / or tocopherols The lip composition of the present invention can further contain glycyrrhetinic acids and / or tocopherols as component (D). These ingredients are oil-soluble drugs and inherently have poor percutaneous absorption when used with an oily base. However, in the lip composition of the present invention, in combination with ascorbyl tetrahexyldecanoate, they can improve the effect of improving lip dullness.

[0044] The lip composition of the present invention may contain one kind of glycyrrhetinic acids and tocopherols alone or in combination of two or more kinds thereof. From the viewpoint of obtaining a more effective effect of improving lip dullness, it is preferable to contain both glycyrrhetinic acids and tocopherols.

[0045] Glycyrrhetinic acids include glycyrrhetinic acid, its derivatives, and salts thereof, and specific examples thereof include glycyrrhetinic acid, glycerin glycyrrhetinate, stearyl glycyrrhetinate, pyridoxine glycyrrhetinate, etc. Among these glycyrrhetinic acids, glycyrrhetinic acid is preferred. These glycyrrhetinic acids may be used alone or in combination of two or more.

[0046] When the lip composition of the present invention contains glycyrrhetinic acids, the content of the glycyrrhetinic acids in the lip composition is, for example, 0.01 to 5% by weight, and preferably 0.1 to 2% by weight.

[0047] Tocopherols refer to tocopherol and its derivatives, and specific examples thereof include α-tocopherol, β-tocopherol, γ-tocopherol, δ-tocopherol, α-tocotrienol, β-tocotrienol, γ-tocotrienol, δ-tocotrienol, tocopherol acetate, tocopherol linoleate, tocopherol nicotinate, tocopherol (linoleate / oleate), etc. Among these tocopherols, tocopherol acetate is preferred. These tocopherols may be used alone or in combination of two or more.

[0048] From the viewpoint of obtaining an even better effect of improving lip dullness, the lip composition of the present invention preferably contains at least one selected from the group consisting of allantoins, pyridoxines, panthenols, glycyrrhetinic acids, and tocopherols, more preferably contains all of allantoins, pyridoxines, panthenols, glycyrrhetinic acids, and tocopherols, and even more preferably contains all of allantoin, pyridoxine hydrochloride, panthenol, glycyrrhetinic acid, and tocopherol acetate.

[0049] Other ingredients The lip composition of the present invention may contain, as necessary, medicinal ingredients other than the above-mentioned components (B), (C), and (D), provided that the effects of the present invention are not impaired. Examples of such medicinal ingredients include anti-inflammatory agents, anti-aging agents, astringents, antioxidants, moisturizing agents, blood circulation promoters, antibacterial agents, disinfectants, drying agents, cooling agents, warming agents, vitamins, amino acids, wound healing promoters, irritation soothing agents, analgesics, cell activators, enzyme components, and herbal ingredients.

[0050] Furthermore, the lip composition of the present invention may contain additives such as surfactants, thickeners, aqueous bases, buffers, chelating agents, antioxidants, stabilizers, preservatives, fragrances, refreshing agents, colorants, dispersants, fluidizing agents, moisturizers, humectants, etc., as needed, provided that the effects of the present invention are not impaired. Of these components, surfactants, thickeners, and aqueous bases are preferred.

[0051] Examples of surfactants include nonionic surfactants, anionic surfactants, cationic surfactants, and zwitterionic surfactants, with nonionic surfactants being preferred. Examples of nonionic surfactants include lipophilic nonionic surfactants and hydrophilic nonionic surfactants. As the nonionic surfactant, either or both of lipophilic nonionic surfactants and hydrophilic nonionic surfactants may be used.

[0052] Examples of lipophilic nonionic surfactants include sorbitan fatty acid esters such as sorbitan monostearate, sorbitan monoisostearate, and sorbitan sesquioleate; glycerin polyglycerin fatty acids such as glycerin monostearate; propylene glycol fatty acid esters such as propylene glycol monostearate; hydrogenated castor oil derivatives; and glycerin alkyl ethers. Among these lipophilic nonionic surfactants, preferred are sorbitan fatty acid esters and glycerin polyglycerin fatty acids, and more preferred are sorbitan monostearate and glycerin monostearate. These lipophilic nonionic surfactants may be used alone or in combination of two or more.

[0053] When the lip composition of the present invention contains a lipophilic nonionic surfactant, the content of the lipophilic nonionic surfactant is, for example, 0.5 to 10 parts by weight, and preferably 0.8 to 8 parts by weight.

[0054] Hydrophilic nonionic surfactants include polyoxyethylene (hereinafter abbreviated as POE), POE sorbitan fatty acid esters such as POE sorbitan monostearate; POE sorbit fatty acid esters such as POE sorbit monooleate; POE glycerin fatty acid esters such as POE glycerin monoisostearate; POE alkyl ethers such as POE stearyl ether and POE cholestanol ether; POE alkyl phenyl ethers such as POE nonylphenyl ether; Pluronic types such as Pluronic; and POE polyoxypropylene. Examples of hydrophilic nonionic surfactants include POE-POP alkyl ethers such as POE cetyl ether, tetraPOE-tetraPOP ethylenediamine condensates such as Tetronic; POE castor oil, POE hydrogenated castor oil derivatives such as POE castor oil and POE hydrogenated castor oil; POE beeswax-lanolin derivatives; alkanolamides; POE propylene glycol fatty acid esters; POE alkylamines; POE fatty acid amides, sucrose fatty acid esters; POE nonylphenyl formaldehyde condensates; alkylethoxydimethylamine oxide, trioleyl phosphate, etc. Among these hydrophilic nonionic surfactants, POE sorbitan fatty acid esters are preferred, and POE sorbitan monostearate is more preferred. These hydrophilic nonionic surfactants may be used alone or in combination of two or more.

[0055] When the lip composition of the present invention contains a hydrophilic nonionic surfactant, the content of the hydrophilic nonionic surfactant is, for example, 0.5 to 7 parts by weight, and preferably 0.8 to 2.5 parts by weight.

[0056] Examples of thickeners include oil-soluble thickeners and water-soluble thickeners, with oil-soluble thickeners being preferred. Examples of oil-soluble thickeners include dextrin fatty acid esters such as dextrin palmitate, dextrin oleate, and dextrin stearate; sucrose fatty acid esters in which three or fewer of the eight hydroxyl groups are esterified with higher fatty acids, with the higher fatty acids being stearic acid and palmitic acid; and benzylidene derivatives of sorbitol such as monobenzylidene sorbitol and dibenzylidene sorbitol. Among these oil-soluble thickeners, dextrin fatty acid esters are preferred, with dextrin palmitate being more preferred. These oil-soluble thickeners may be used alone or in combination of two or more.

[0057] When the lip composition of the present invention contains a thickener, the content of the thickener is, for example, 0.2 to 5 parts by weight, and preferably 0.5 to 1.5 parts by weight.

[0058] Examples of the aqueous base include water, polyethylene glycol, propylene glycol, glycerin, 1,3-butylene glycol, and dipropylene glycol, and preferably water and glycerin.

[0059] When the lip composition of the present invention contains an aqueous base, the content of the aqueous base can be, for example, more than 0 parts by weight and not more than 20 parts by weight, and preferably more than 0 parts by weight and not more than 18 parts by weight. When the lip composition of the present invention contains water as an aqueous base, the content of water can be, for example, more than 0 parts by weight and not more than 7 parts by weight, and preferably more than 0 parts by weight and not more than 5 parts by weight.

[0060] Formulation The formulation form of the lip composition of the present invention is not particularly limited, and examples include gel, paste, and solid forms. Specific forms of the lip composition of the present invention include oily formulations that do not contain water and water-in-oil emulsions that contain a small amount of water. Further specific formulations of the lip composition of the present invention include lip balm, lip gloss, lipstick, etc. Furthermore, the lip composition of the present invention may be any of general skin cosmetics, medicinal cosmetics, quasi-drugs, and pharmaceuticals, but is preferably a pharmaceutical.

[0061] Method for producing lip composition The lip composition of the present invention is prepared by mixing desired amounts of the above-mentioned components (A) and (B), the components (C) and (D) which are blended as needed, the above-mentioned other medicinal ingredients, additives, etc.

[0062] Method of using lip compositions The lip composition of the present invention can be applied to the lips for the purpose of improving lip dullness. Therefore, the lip composition of the present invention can be used by people who are aware of lip dullness. The lip composition of the present invention can also be used as part of daily care to prevent lip dullness. The lip composition of the present invention can be applied to the lips, for example, 1 to 3 times a day, preferably 1 to 2 times a day. To achieve desirable effects, the lip composition of the present invention is preferably applied continuously, and the application period can be, for example, 3 weeks or more, preferably 4 weeks or more, and more preferably 8 weeks or more.

[0063] 2. A method for improving dull lips As described above, in lip compositions containing an oily base, ascorbyl tetrahexyldecanoate exhibits an effect of improving lip dullness. Therefore, the present invention further provides a method for imparting an effect of improving lip dullness to a lip composition, which comprises blending ascorbyl tetrahexyldecanoate in a lip composition containing an oily base.

[0064] In the present invention, lip dullness refers to a condition in which lips, which have a significantly low melanocyte count, are directly damaged by external factors such as ultraviolet rays, resulting in a darkened color in certain areas of the lip surface. Specifically, this is visible as uneven color (uneven color) due to spots, darkening, etc. In addition, in the present invention, improving lip dullness refers to lightening the darkened areas of the lips in a lip composition containing an oily base, thereby lowering the average color intensity and making the uneven color more uniform, compared to a lip composition that does not contain ascorbyl tetrahexyldecanoate.

[0065] Furthermore, in lip compositions containing an oily base, ascorbyl tetrahexyldecanoate not only has the effect of improving lip dullness, but also has the effect of improving lip wrinkles when used by people who are aware of lip wrinkles. "Improving lip wrinkles" refers to making lip wrinkles shallower and / or less noticeable in lip compositions containing an oily base compared to when ascorbyl tetrahexyldecanoate is not included, and particularly refers to the effect achieved on vertical lip wrinkles.

[0066] Furthermore, in lip compositions containing an oily base, ascorbyl tetrahexyldecanoate not only improves dull lip color, but also improves poor lip color when used by individuals who are aware of poor lip color. Poor lip color refers to a state in which the lips lack color (redness) throughout the entire lip. The poorer the lip color, the closer the boundary between the lips (the part with the underlying mucous membrane) and the skin becomes to the skin color, resulting in a smaller area of ​​reddish lip color when viewed from the front, and as a result, the lips tend to be thinner in the vertical direction. In some cases, the lips may actually be thin and lack volume. "Improving poor lip color" refers to enhancing the overall color (redness) of the lips in lip compositions containing an oily base compared to those that do not contain ascorbyl tetrahexyldecanoate. When poor lip color is improved even more significantly, the redness increases up to the boundary between the lips (the part with the mucous membrane as its underlying structure) and the skin, and the area of ​​the reddish part when viewed from the front of the lips increases, resulting in a visible increase in the thickness of the lips in the vertical direction (a feeling of increased lip volume). This feeling of increased lip volume is particularly noticeable in the lower lip. Furthermore, a lip volume increase effect may actually be achieved.

[0067] By providing a lip composition with an action of improving not only lip wrinkles but also poor lip color and / or lip dullness, these actions can be combined to bring about an even healthier lip condition.

[0068] In the method for imparting the effect of improving lip dullness, the types and amounts of components used, the form of the lip composition, the method of use, etc. are as shown in the section "1. Lip composition" above. [Example]

[0069] The present invention will be explained in more detail below by showing examples, but the present invention is not limited to these examples.

[0070] Test Example 1 [Preparation of Lip Composition] Lip compositions having the compositions shown in Table 1 were prepared. Specifically, the component (A) and the surfactant were mixed and heated and dissolved in a water bath at 85°C to obtain a premix. After adding the component (B) to the premix while sufficiently stirring, it was cooled to 35°C while stirring to obtain a lip composition.

[0071] Each of the obtained lip compositions was applied to the lips once a day for 8 weeks to 10 women who perceived lip dullness (lip color unevenness). In addition, these 10 subjects also perceived poor lip blood color (poor lip blood color throughout the lips) and wrinkles. [[ID=?]] [[ID=?]]

[0072] [[ID=?]] [Evaluation of Improvement Effect] (Sensory Evaluation) After applying the lip composition for 8 weeks, the number of people who felt that the lip color unevenness was eliminated and the appearance was improved with a uniform color tone was classified according to the following criteria to evaluate the lip dullness improvement effect. In addition, the number of people who felt that the lip color was improved to a good pink color with good blood color was similarly classified according to the following criteria to evaluate the poor blood color improvement effect. Furthermore, the number of people who felt that the lip wrinkles became shallower and the surface of the lips was improved to a smooth appearance was also classified according to the following criteria to evaluate the lip wrinkle improvement effect. The results are shown in Table 1. ○: 7 or more people △: 4 - 6 people ×: 3 or fewer people

[0073] (Measurement Evaluation) Before applying the lip composition of Example 1 (initial) and after applying the lip composition for 8 weeks, using the skin analyzer ANTERA3D TM It should be noted that there seem to be some missing numbers in the original text for the tags between and . I've left them as they are in the translation for the sake of following the instruction precisely. If you can provide the complete correct text, it would be better for a more accurate translation.The unevenness of melanin and the average concentration of melanin were measured using the ANTERA3D skin analyzer. Specifically, measurements were taken three times for each subject, initially and after 8 weeks, and the worst (highest) measurement of the three was taken as the final measurement (initial) and final measurement (after 8 weeks) for that subject. Furthermore, the final measurements (initial) and final measurement (after 8 weeks) for the 10 subjects were averaged. The results obtained are shown in Figure 1 (unevenness of melanin) and Figure 2 (average concentration of melanin), respectively. The smaller the average of the final measurement after 8 weeks compared to the average of the initial final measurement, the greater the improvement effect on dullness of the lips. Furthermore, the skin analyzer ANTERA3D TM In addition to the measurements mentioned above, lip surface roughness (roughness of the texture of the lip surface) and lip wrinkles (depth of lip wrinkles) were also measured and averaged using the same method. The smaller the average confirmed measurement value after 8 weeks compared to the initial average confirmed measurement value, the greater the improvement effect on lip wrinkles. The results obtained are shown in Figure 3 (lip surface roughness) and Figure 4 (lip wrinkles), respectively.

[0074] [Table 1]

[0075] As is clear from Table 1, lip compositions containing ascorbyl tetrahexyldecanoate in an oily base (Examples 1 to 7) exhibited a significant improvement in lip dullness compared to lip compositions not containing ascorbyl tetrahexyldecanoate (Comparative Examples 1 to 4). This significant improvement was observed not only on lip wrinkles, but also on poor lip color and wrinkles. Furthermore, as is clear from Figures 1 and 2, objectively, the uniformity of melanin and the average melanin concentration were significantly improved, demonstrating a significant improvement in dullness. Furthermore, in addition to the improvement in lip dullness, as is clear from Figures 3 and 4, objectively, the roughness of the lip surface and the depth of lip wrinkles were significantly improved, demonstrating a significant improvement in lip wrinkles.

[0076] Test Example 2 [Preparation of lip composition] Lip compositions were prepared according to the formulations shown in Table 2. Specifically, components (A), (C), and (D) and a surfactant were mixed and heated to dissolve in a water bath at 85°C to obtain a premix. Component (B) was added to the premix while thoroughly stirring, and the mixture was then cooled to 35°C while stirring to obtain a lip composition.

[0077] The obtained lip composition was applied to the lips of women who were aware of dull lips once a day for 8 weeks. In addition to dull lips, these women also noticed poor lip color and / or lip wrinkles. Of these women, the lip composition of Example 13 was applied to Women 2 and 3. Woman 2 was aware of not only dull lips (particularly spot-like blemishes present below the lower lip) but also lip wrinkles. Woman 3 was highly aware of dull lips (particularly dark spots present over a relatively wide area above the lower lip), and objectively, the dullness was a relatively serious problem, as well as poor lip color. Enlarged photographs of a portion of Woman 2's lower lip are shown in Figure 5 (Woman 2; initial, after 4 weeks of application, and after 8 weeks of application).

[0078] [Table 2]

[0079] As a result, when the lip compositions of Examples 8 to 13 were applied, an even better improvement effect on lip dullness was achieved. Furthermore, not only was an improvement effect on lip dullness observed, but also an improvement effect on lip pallor was observed in people who were aware of lip wrinkles, and an improvement effect on lip wrinkles was observed in people who were aware of lip wrinkles.

[0080] Specifically, as shown in Figure 5, for the lip composition of Example 13, for Woman 2, spot-like blemishes were initially observed in the area indicated by the white triangle in the photograph, but after just four weeks, they were clearly lighter, and after eight weeks, they had almost completely disappeared, resulting in a more significant improvement in dullness. Also, as shown in Figure 5, for Woman 2, the deepest vertical wrinkles, particularly those indicated by the black arrow in the photograph, became significantly shallower even after just four weeks, and the overall unevenness of the lip surface became significantly smoother, resulting in a more significant improvement in lip wrinkles.

[0081] For Woman 3, who applied the lip composition of Example 13, the darkening of the lips, which had been strongly noticeable over a relatively large area, became less noticeable after just four weeks, and was further significantly resolved after eight weeks. Furthermore, Woman 3 also observed a clear improvement in the color of her lips after just four weeks, and was further significantly resolved after eight weeks. As a result, the area of ​​redness on Woman 3's lips increased, and in particular, the maximum thickness of the lower lip in the vertical direction increased from 7 mm at the beginning to 9 mm after eight weeks of application, providing a feeling of fuller lips.

[0082] Prescription example Lip compositions were prepared according to the formulations shown in Tables 3 and 4. Specifically, component (A), component (D), surfactant, and thickener were mixed and dissolved by heating in a water bath at 85°C. Then, component (C), which had been separately dissolved by heating in a water bath at 85°C, and an aqueous base were mixed to obtain a premix. Component (B) was added to the premix while thoroughly stirring, and the mixture was cooled to 35°C while stirring to obtain lip compositions of Formulation Examples 1 to 15. The lip compositions of all of the Formulation Examples provided the effects of further improving lip dullness, further improving lip wrinkles, and further improving poor lip color, as well as the feeling and / or effect of fuller lips, as observed in Test Example 2.

[0083] [Table 3]

[0084] Table 4

Claims

1. A lip composition containing (A) an oily base containing white petrolatum, microcrystalline wax, and liquid paraffin, (B) ascorbyl tetrahexyldecanoate, (C) allantoins and / or pyridoxines, and (D) glycyrrhetinic acids, and used to improve uneven color due to spots or darkening of the lips (excluding those containing tocopherol acetate, water-soluble collagen crosspolymer, water-soluble collagen, hydrolyzed collagen, hydroxypropyltrimonium hyaluronate, sodium hyaluronate, hydrolyzed hyaluronic acid, argania spinosa kernel oil, baobab seed oil, wild rose oil, jojoba seed oil, shea butter, and squalane).

2. 2. The lip composition according to claim 1, wherein the content of component (A) is 50 to 99.5% by weight.

3. The lip composition according to claim 1 or 2, wherein the component (A) comprises a solid oil.

4. 4. The lip composition according to claim 3, wherein the content of the solid oil is 30 to 70% by weight.

5. The lip composition according to any one of claims 1 to 4, further comprising a panthenol.

6. The lip composition according to any one of claims 1 to 5, further comprising tocopherols.

7. A method for imparting to a lip composition an effect of improving discoloration caused by spots or darkening of the lips, characterized in that (A) the lip composition contains an oily base including white petrolatum, microcrystalline wax, and liquid paraffin (excluding those containing tocopherol acetate, water-soluble collagen crosspolymer, water-soluble collagen, hydrolyzed collagen, hydroxypropyltrimonium hyaluronate, sodium hyaluronate, hydrolyzed hyaluronic acid, argania spinosa kernel oil, baobab seed oil, wild rose oil, jojoba seed oil, shea butter, and squalane), and further comprising blending (B) ascorbyl tetrahexyldecanoate, (C) allantoins and / or pyridoxines, and (D) glycyrrhetinic acids.

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