External preparation for skin
A topical skin preparation with heparinoids addresses dermal skin issues by enhancing skin elasticity and reducing sagging through dermal effects, showing substantial efficacy in improving skin condition after continuous use.
Patent Information
- Application Number
- JP2025219079
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- Filing Date
- 2025-12-02
- Publication Date
- 2026-02-16
AI Technical Summary
Topical skin preparations can only deliver active ingredients to the stratum corneum, failing to address skin elasticity and sagging issues caused by problems in the dermis layer.
A topical skin preparation containing heparinoids, which are polysulfated mucopolysaccharides, is formulated to improve skin elasticity and alleviate sagging by promoting dermal effects beyond the stratum corneum.
The topical skin preparation effectively improves skin elasticity and alleviates sagging skin by utilizing heparinoids, demonstrating significant improvements in nearly everyone after 30 days of use.
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Abstract
Description
[Technical Field]
[0001] The present invention relates to an external skin preparation used to improve skin elasticity or alleviate sagging skin. [Background technology]
[0002] From the surface, skin is composed of the stratum corneum, epidermis, dermis, and subcutaneous tissue. The stratum corneum retains moisture through interfollicular lipids, NMF, and sebum film, protecting the skin from external stimuli and preventing moisture evaporation from the stratum corneum. Meanwhile, a decrease in interfollicular lipids, NMF, and sebum film in the stratum corneum facilitates moisture evaporation, leading to skin problems such as dryness and roughness. Furthermore, fibroblasts in the dermis produce collagen, elastin, and hyaluronic acid, synthesizing a structure containing collagen and elastin fibers known as the extracellular matrix, thereby maintaining skin elasticity. Meanwhile, a decline in fibroblasts leads to a decrease in collagen, elastin, and hyaluronic acid in the dermis, resulting in a decrease in skin elasticity and sagging.
[0003] Topical skin preparations are used to improve skin troubles by delivering active ingredients to the stratum corneum. Heparinoids, as active ingredients in topical skin preparations, have attracted attention for their excellent moisturizing effects. The moisturizing mechanism of heparinoids is thought to be based on promoting the recovery of the lamellar structure of intercellular lipids in the stratum corneum and increasing the amount of secondary bound water (Non-Patent Document 1), or inducing basal sweating and increasing the moisture content of the stratum corneum (Non-Patent Document 2). [Prior art documents] [Non-patent literature]
[0004] [Non-Patent Document 1] The Nishinihon journal of dermatology 69(1), 44-50, 2007-02-01 [Non-patent document 2] Journal of the Japanese Dermatological Association 129(10), 2165-2172, 2019 Summary of the Invention [Problem to be solved by the invention]
[0005] Loss of skin elasticity gives the impression of aging, and if it leads to sagging skin, this impression becomes even more pronounced. Therefore, there are many calls for improving skin elasticity and alleviating sagging skin. However, because topical skin preparations can only deliver active ingredients that improve skin problems to the stratum corneum, it is generally recognized that loss of skin elasticity and sagging skin caused by problems in the dermis layer cannot be improved by topical preparations.
[0006] Therefore, an object of the present invention is to provide an external skin preparation that is effective in improving skin elasticity and / or improving sagging skin. [Means for solving the problem]
[0007] The present inventors have conducted extensive research to solve the above-mentioned problems and have unexpectedly discovered that heparinoids, which are known only for their effects on the stratum corneum, also have the effect of improving skin elasticity and / or alleviating sagging skin. Based on this finding, the present invention was completed through further research.
[0008] That is, the present invention provides the following aspects. Item 1. A topical skin preparation containing heparinoids that is used to improve skin elasticity. Item 2. A topical skin preparation containing heparinoids that is used to improve sagging skin. [Effects of the Invention]
[0009] The topical skin preparation of the present invention can improve skin elasticity and / or alleviate sagging skin. DETAILED DESCRIPTION OF THE INVENTION
[0010] The topical skin preparation of the present invention is characterized by containing a heparinoid. The topical skin preparation of the present invention will be described in detail below.
[0011] Heparinoids Heparinoids are polysulfated mucopolysaccharides such as chondroitin polysulfate, and are known drugs known to have moisturizing effects, blood flow increasing effects, and the like.
[0012] The origin of the heparinoid used in the present invention is not particularly limited, and examples thereof include those obtained by polysulfating mucopolysaccharides, and those extracted from the tissues of edible animals (e.g., lungs containing tracheal cartilage from cattle, pigs, etc.). In the TGase expression promoter of the present invention, heparinoids listed in the Japanese Pharmacopoeia Non-Drug Standards are preferably used.
[0013] The amount of heparinoid in the topical skin preparation of the present invention may be appropriately determined depending on the formulation form of the preparation, etc., but may be, for example, 0.01 to 5 wt %, preferably 0.03 to 3 wt %, and more preferably 0.1 to 1 wt %.
[0014] Other ingredients The topical skin preparation of the present invention may contain, as necessary, pharmacological ingredients other than the above-mentioned heparinoid component, provided that the effects of the present invention are not impaired. Examples of such pharmacological ingredients include antihistamines, local anesthetics, anti-inflammatory agents, anti-aging agents, astringents, antioxidants, moisturizers, 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.
[0015] Furthermore, the topical skin preparation of the present invention may contain bases or additives as necessary to obtain a desired formulation. Such bases and additives are not particularly limited as long as they are pharmaceutically acceptable, and examples thereof include aqueous bases such as water, lower alcohols, and polyhydric alcohols; oils, mineral oils, waxes, ester oils, fatty acid alkyl esters, fatty acids, fatty acid esters, higher alcohols, cholesterol, glyceryl tri-2-ethylhexanoate, cetyl 2-ethylhexanoate, and silicone oils; and additives such as surfactants, thickeners, buffers, chelating agents, antioxidants, stabilizers, preservatives, fragrances, cooling agents, colorants, dispersants, fluidizing agents, and humectants.
[0016] Formulation The form of the external skin preparation of the present invention is not particularly limited as long as it can be applied transdermally, and examples thereof include liquid, solid, and semi-solid (gel, ointment, paste) forms.
[0017] Furthermore, the formulation form of the topical skin preparation of the present invention is not particularly limited as long as it can be applied transdermally, and examples thereof include topical skin pharmaceuticals, topical skin quasi-drugs, cosmetics, skin cleansers, etc. More specific examples include topical skin pharmaceuticals such as creams, lotions, gels, emulsions, liquids, patches, aerosols, ointments, and packs; topical skin quasi-drugs such as creams, lotions, gels, emulsions, liquids, patches, aerosols, ointments, and packs; cosmetics such as foundations, creams, lotions, gels, emulsions, liquids, ointments, and packs; and skin cleansers such as body shampoos, hair shampoos, and rinses.
[0018] Purpose The topical skin preparation of the present invention is used for the purpose of improving skin elasticity and / or alleviating sagging skin. Examples of the form of improving sagging skin include lifting the entire face and / or alleviating areas where sagging is a concern.
[0019] The dose of the topical skin preparation of the present invention may be appropriately determined depending on the dosage form, preparation type, severity of symptoms, etc. For example, the dose may be applied to 1 cm of skin per dose. 2 The topical skin preparation of the present invention can be applied once to several times a day in an amount that provides about 0.001 to 5 μg of heparinoid per dose. In order to effectively improve skin elasticity and / or alleviate sagging skin, it is preferable to apply the topical skin preparation of the present invention continuously for, for example, 15 days or more, preferably 30 days or more. [Example]
[0020] The present invention will be explained in more detail below by showing examples, but the present invention is not limited to these examples.
[0021] Twenty-eight men and women in their 30s to 50s who reported experiencing loss of skin elasticity and / or sagging skin (all but two had no particular problems with the stratum corneum, such as dry skin and / or inflammation) applied a cream containing 0.3% heparinoid twice daily to areas where they were concerned about loss of skin elasticity and / or sagging. Subjects were evaluated for satisfaction with their skin condition after 15 and 30 days of use, compared to their skin condition before use. Specifically, subjects were rated on a 7-point scale (very satisfied, satisfied, somewhat satisfied, neither satisfied nor unsure, somewhat dissatisfied, dissatisfied, and very dissatisfied) for the degree of improvement in skin elasticity and improvement in sagging (lifting of the entire face (face line) and improvement in areas of concern). The percentages (%) of subjects who responded with each rating were calculated. Furthermore, the combined percentages (%) of subjects who responded as very satisfied, satisfied, and somewhat satisfied were calculated as an efficacy index. The results after 15 days are shown in Table 1, and the results after 30 days are shown in Table 2. In the table, the units of each value are %.
[0022] [Table 1]
[0023] [Table 2]
[0024] As is clear from Tables 1 and 2, most people experienced an improvement in skin elasticity, and especially after 30 days, nearly everyone experienced an improvement in skin elasticity. Furthermore, not only did skin elasticity improve, but more than 70% of people also experienced an improvement in sagging skin.
Claims
1. A topical skin preparation containing heparinoids that is used to improve skin elasticity.
2. A topical skin preparation containing heparin-like substances used to improve sagging skin.