Agent for improving sagging pores

Abstract

The present disclosure pertains to: an agent for improving sagging pores and the like; and a beautification method, a non-therapeutic method, or the like that uses said agent. More specifically, it is possible to prepare an agent for improving sagging pores and the like by adopting a combination of glycylglycine and retinol, and to use the agent in a beautification method or a non-therapeutic method for improving sagging pores.

Description

Sagging pore improver

[0001] The present disclosure relates to an agent for improving sagging pores, more specifically to an agent for improving sagging pores comprising glycylglycine and retinol, and a cosmetic method using the same.

[0002] In recent years, concerns about the visibility of pores have become a growing concern, creating a need for topical skin care products that can improve this. However, the mechanism behind the visibility of pores is unclear, and the most common treatments are astringent lotions and the removal of blackheads. Alternatively, people often try to improve their appearance by using foundation.

[0003] However, for example, astringent lotions are intended to tighten the skin, and do so by temporarily lowering the skin surface temperature with alcohol and coagulating proteins with organic acids, etc. Therefore, because they only tighten the skin temporarily, they place a heavy burden on the skin and do not fundamentally solve the problem of visible pores, and their effectiveness is insufficient.

[0004] As one of the compositions for external use on the skin that reduces the visibility of pores, Patent Document 1 discloses a parakeratosis inhibitor and a pore-shrinking agent comprising one or more compounds selected from the group consisting of glycine derivatives, aminodicarboxylic acid derivatives, acylaminodicarboxylic acid derivatives, pyrrolidinecarboxylic acid derivatives, piperidinecarboxylic acid derivatives, hexamethyleneiminecarboxylic acid derivatives, β-alanine derivatives, and salts of the above-mentioned derivatives.

[0005] On the other hand, no care ingredients have been developed to date to address the sagging pores that occur with age.

[0006] Patent No. 5241058

[0007] An object of the present disclosure is to provide an agent for improving sagging pores, more specifically, an agent for improving sagging pores containing glycylglycine and retinol, and to provide a cosmetic method using the same.

[0008] The present inventors conducted extensive research to identify components that improve sagging pores, and discovered for the first time that a combination of glycylglycine and retinol is particularly effective in improving sagging pores. As a result, they developed an agent for improving sagging pores, which contains glycylglycine and retinol, and a cosmetic or non-therapeutic method for improving sagging pores.

[0009] Therefore, the present disclosure relates to the following aspects: [Aspect 1] A sagging pore improving agent comprising glycylglycine and retinol. [Aspect 2] The sagging pore improving agent according to Aspect 1, comprising 0.5% to 2.0% glycylglycine. [Aspect 3] A sagging pore improving agent according to Aspect 1, comprising 0.3 x 10 retinol. ２ IU / g or more 1.0×10 ５ The sagging pore improving agent according to Aspect 1 or 2, containing 1.1 IU / g or less. [Aspect 4] The sagging pore improving agent according to any one of Aspects 1 to 3, which improves the aspect ratio of pore shape. [Aspect 5] The sagging pore improving agent according to any one of Aspects 1 to 4, which reduces pore size. [Aspect 6] The sagging pore improving agent according to any one of Aspects 1 to 5, which improves wrinkles. [Aspect 7] The sagging pore improving agent according to any one of Aspects 1 to 6, which improves skin elasticity. [Aspect 8] The sagging pore improving agent according to any one of Aspects 1 to 7, which improves skin moisturizing properties. [Aspect 9] A topical skin preparation comprising the sagging pore improving agent according to any one of Aspects 1 to 8. [Aspect 10] A cosmetic method comprising the step of applying the sagging pore improving agent according to any one of Aspects 1 to 8 or the topical skin preparation according to Aspect 9 to the skin of a subject. [Aspect 11] A wrinkle improving agent comprising glycylglycine and retinol. [Aspect 12] A skin elasticity improving agent comprising glycylglycine and retinol. [Aspect 13] A skin moisturizing improving agent comprising glycylglycine and retinol.

[0010] According to the present disclosure, sagging pores and the like can be improved by applying to the skin a composition containing a combination of glycylglycine and retinol as active ingredients.

[0011] FIG. 1 is a graph showing the change in pore aspect ratio caused by application of the test formulation over 12 weeks. FIG. 2 is a graph showing the change in pore area (total pore area) caused by application of the test formulation over 12 weeks. FIG. 3 is a graph showing the change in pore score caused by application of the test formulation over 12 weeks. FIG. 4 is a graph showing the change in moisture content (corneometer value) caused by application of the test formulation over 12 weeks. FIG. 5 is a graph showing the change in softness (R0:Uf (maximum suction height)) caused by application of the test formulation over 12 weeks. FIG. 6 is a graph showing the change in elasticity (R5:Ur / Ue (instantaneous return after release of negative pressure / instant deformation upon suction)) caused by application of the test formulation over 12 weeks. FIG. 7 is a graph showing the change in questionnaire results caused by application of the test formulation over 12 weeks.

[0012] (Sagging Pore Improvement Agent) In one embodiment of the present disclosure, the sagging pore improvement agent according to the present disclosure comprises glycylglycine and retinol as active ingredients. From another aspect, one embodiment of the present disclosure relates to a composition for use in improving sagging pores, comprising glycylglycine and retinol as active ingredients. From yet another aspect, one embodiment of the present disclosure relates to the use of a combination of glycylglycine and retinol in the manufacture of a drug or cosmetic for use in improving sagging pores.

[0013] As used herein, the term "sagging pores" refers to pores that are oval in shape. Sagging pores are pores that have become teardrop-shaped (oval) due to sagging (loss of elasticity) of the cheeks and face line, which mainly occurs after the age of 40. In sagging pores, the minor axis / major axis value is less than 1, and in particular, if it is less than 0.6, the pores appear sagging. Furthermore, sagging pores are particularly noticeable on both cheeks in human facial skin.

[0014] (Glycylglycine) Glycylglycine has the chemical formula NH ２ CH ２ CONHCH ２ Glycylglycine is a dipeptide of glycine represented by COOH and is one of the peptides with a simple structure. High-purity glycylglycine is commercially available and easily available.

[0015] In some embodiments, the sagging pore improving agent preferably contains 0.05% to 3.0% of glycylglycine, more preferably 0.5% to 2.0%. In this specification, percentages (%) refer to mass % unless otherwise specified.

[0016] (Retinol) Retinol has the chemical formula C ２０ H ３０ It is a fat-soluble vitamin represented by the symbol O and is also known as vitamin A1. High-purity vitamins are commercially available and readily available.

[0017] In some embodiments, the sagging pore improving agent contains retinol at 1.0 IU / g or more, 5x10 ５ It is preferable that the content is 0.3×10 ２ IU / g or more, 1.0x10 ５ It is more preferable that the concentration is 1U / g or less, where IU stands for international unit.

[0018] (Shape and Size of Pores) In one embodiment, the sagging pore improving agent according to the present disclosure is used as a composition for improving the aspect ratio of pore shape. In the context of the present disclosure, the aspect ratio is defined as "minor axis / major axis", and the aspect ratio is evaluated as being improved when the value increases and approaches 1 (for example, when the aspect ratio value changes from 0.6 to 0.7). In other words, improvement of sagging pores means that the shape of the pores becomes closer to a perfect circle. The shape and size of pores can be evaluated using a three-dimensional pore measurement method, such as that described in Japanese Patent No. 4286724.

[0019] In one embodiment, the sagging pore improving agent according to the present disclosure is used as a composition for reducing the size of pores.For example, when the longitudinal length of sagging pores is reduced, the size of pores is reduced and the aspect ratio of pores is improved.In addition, the size of pores can also be evaluated by image analysis using a skin imaging diagnostic device (for example, Visia Evolution manufactured by Canfield Scientific).

[0020] As described above, pore evaluation can be performed using a three-dimensional pore measurement method, such as that described in Japanese Patent No. 4286724, which enables precise measurement of the three-dimensional shape of pores. Briefly, a replica of the skin surface is first collected and measured using a confocal microscope to obtain three-dimensional shape measurement data of the replica. Next, correction processes such as noise removal are performed, and then pores are extracted from the noise-removed data. Next, information regarding the skin texture in the pore area may be removed from the pore-extracted data. Pore evaluation can then be performed based on the pore 3D analysis data obtained as described above.

[0021] As described above, pore evaluation can also be performed by image analysis using a skin imaging diagnostic device (for example, Visia Evolution manufactured by Canfield Scientific).

[0022] (Wrinkle Improvement) In one embodiment, the sagging pore improving agent according to the present disclosure is used as a composition for improving wrinkles. Accordingly, one embodiment of the present disclosure relates to a composition for use in improving wrinkles, comprising glycylglycine and retinol as active ingredients. That is, one embodiment of the present disclosure also relates to a wrinkle improving agent comprising glycylglycine and retinol. From another perspective, one embodiment of the present disclosure relates to the use of a combination of glycylglycine and retinol in the manufacture of a drug or cosmetic for use in improving wrinkles. Wrinkle evaluation can be performed, for example, by image analysis using a skin imaging diagnostic device (e.g., Visia Evolution manufactured by Canfield Scientific), or by observation or visual assessment by an expert.

[0023] (Improvement of Elasticity or Firmness) In one embodiment, the sagging pore improving agent according to the present disclosure is used as a composition for improving skin elasticity (firmness). Accordingly, one embodiment of the present disclosure relates to a composition for use in improving elasticity (firmness), comprising glycylglycine and retinol as active ingredients. That is, one embodiment of the present disclosure also relates to a skin elasticity improving agent comprising glycylglycine and retinol. From another perspective, one embodiment of the present disclosure relates to the use of a combination of glycylglycine and retinol in the manufacture of a pharmaceutical or cosmetic product for use in improving elasticity (firmness). Skin elasticity can be evaluated, for example, by measuring the viscoelasticity of the skin using a commercially available device (e.g., Cutometer manufactured by Courage+Khazaka).

[0024] (Improvement of Moisture Retention) In one embodiment, the sagging pore improving agent according to the present disclosure is used as a composition for improving skin moisture retention. Thus, one embodiment of the present disclosure relates to a composition for use in improving skin moisture retention, comprising glycylglycine and retinol as active ingredients. That is, one embodiment of the present disclosure also relates to a skin moisture retention improving agent comprising glycylglycine and retinol. From another perspective, one embodiment of the present disclosure relates to the use of a combination of glycylglycine and retinol in the manufacture of a drug or cosmetic for use in improving skin moisture retention. Skin moisture retention can be evaluated, for example, by measuring the stratum corneum moisture content using a commercially available device (e.g., a Corneometer manufactured by Courage+Khazaka).

[0025] (External Skin Preparation) In one aspect, the present invention relates to an external skin preparation comprising a sagging pore improving agent according to the present disclosure. In some aspects, the external skin preparation can be prepared as a cosmetic, a quasi-drug, or a pharmaceutical. The cosmetic can be a sunscreen, a lotion, a beauty serum, a beauty cream, an aftercare lotion, a sun oil, or the like, but can be any cosmetic that is applied to the skin.

[0026] In addition to glycylglycine and retinol, such topical skin preparations can be appropriately blended with optional ingredients used in cosmetics, pharmaceuticals, etc., as needed. Furthermore, topical skin preparations can be prepared in any form, such as a solid preparation for topical use, a powder preparation for topical use, a liquid preparation for topical use, a liniment, a spray, an aerosol preparation for topical use, a pump spray, an ointment, a cream, a gel, a patch, a tape, or a cataplasm.

[0027] The sagging pore improving agent or topical skin preparation according to the present disclosure may contain optional ingredients used in cosmetics, pharmaceuticals, etc., as needed, provided that the effects are not impaired. Examples of optional ingredients include oils, surfactants, powders, coloring materials, water, alcohols, thickeners, chelating agents, silicones, antioxidants, UV absorbers, moisturizers, fragrances, various medicinal ingredients, preservatives, pH adjusters, and neutralizers. Other ingredients may also be included, such as other anti-inflammatory ingredients and whitening ingredients.

[0028] For example, a cream may contain, in addition to glycylglycine and retinol, water, alcohol, moisturizers, thickeners, film-forming agents, active agents, oils, stabilizers, transdermal absorption inhibitors, colorants, chelating agents, buffers, preservatives, fragrances, etc.

[0029] (Cosmetic Methods and Non-Therapeutic Methods) In one aspect, the present invention relates to a cosmetic method or a non-therapeutic method comprising the step of applying a sagging pore improving agent according to the present disclosure or an external skin preparation according to the present disclosure to the skin of a subject. The subject may be a mammal, but is preferably a human.

[0030] The sagging pore improving agent or topical skin preparation disclosed herein can be used in cosmetic or non-therapeutic methods for improving sagging pores, improving the aspect ratio of pore shape, reducing pore size, improving wrinkles, improving skin elasticity, or improving skin moisture retention. In the cosmetic or non-therapeutic methods disclosed herein, the topical skin preparation is applied to the area where the desired effect is desired, such as the face, neck, hands, arms, legs, etc. Application can be performed in any manner, such as by hand or with an applicator. The number, frequency, amount, etc. of application can be determined appropriately depending on the desired effect, etc. Note that the cosmetic or non-therapeutic methods disclosed herein do not include so-called medical procedures.

[0031] (Use) Furthermore, one embodiment of the present disclosure relates to the use of a combination of glycylglycine and retinol for improving sagging pores, improving the aspect ratio of pore shape, reducing pore size, improving wrinkles, improving skin elasticity, or improving skin moisturization. The data disclosed herein demonstrate that applying a composition containing a combination of glycylglycine and retinol to the skin improves sagging pores and leads to skin elasticity, moisturization, and wrinkle improvement. Therefore, a composition containing a combination of glycylglycine and retinol can be used to prepare topical skin preparations and other compositions for use in improving sagging pores, etc. That is, one embodiment of the present disclosure also relates to the use of a combination of glycylglycine and retinol in the manufacture of a topical skin preparation for improving sagging pores, improving the aspect ratio of pore shape, reducing pore size, improving wrinkles, improving skin elasticity, or improving skin moisturization.

[0032] All documents mentioned herein are incorporated by reference in their entirety.

[0033] The examples of the present disclosure described below are for illustrative purposes only and do not limit the technical scope of the present disclosure. The technical scope of the present disclosure is limited only by the description of the claims. The present disclosure may be modified, for example, by adding, deleting, or substituting the constituent elements of the present disclosure, provided that the modifications do not depart from the spirit of the present disclosure.

[0034] Example 1: Outline of the test for the effect of continuous use of a cream containing glycylglycine and retinol (Objective) A test for the effect of continuous use of a cream containing glycylglycine and retinol was conducted with the aim of "improving sagging pores," for which no active ingredient has been available to date. (Method) A cream containing glycylglycine and retinol, which is expected to be effective against sagging pores, was applied to 19 subjects for 12 weeks, and the pore shape and skin parameters were evaluated. The cream used contained 1.6% glycylglycine and 0.2 x 10 ４ The product contained IU / g retinol. The dosage was 0.2g (0.1g on each cheek), once in the morning and once in the evening. (Results) Analysis using cheek replicas and a skin imaging diagnostic device (VISIA) showed that application of the test formulation significantly improved the degree of pore sagging (aspect ratio) and significantly reduced some pore area. In addition, the moisture content and elasticity of the stratum corneum increased, improving skin condition.

[0035] Example 2: Test Protocol (Subjects) The test was conducted on 19 men and women (14 women, 5 men, 51.1±5.7 years old) (mean±SD) in their 40s or older who were troubled by sagging pores. (Continuous use period) 1.6% glycylglycine and 0.2×10 ４A cream formulation containing IU / g retinol was applied to both cheeks for 12 weeks (measurements were taken after 0, 4, 8, and 12 weeks). (Measurement Items) Measurement items included pore sagging and size (replica), stratum corneum moisture content, viscoelasticity (elasticity, softness), and external appearance images. Pore evaluation using replicas can be performed as described in Japanese Patent No. 4286724. A replica is taken of the skin surface and measured using a confocal microscope to obtain three-dimensional shape measurement data. SILFLO (Amic Group) can be used as the replica substrate. Stratum corneum moisture content and viscoelasticity (elasticity, softness) can be measured using commercially available instruments such as the Corneometer (CM825) and Cutometer (MPA580). (The Cutometer uses a 2-mm probe diameter and is suctioned at 400 mbar for measurement.) External appearance images can be analyzed using commercially available instruments such as the VISIA Evolution. The significance test for the measured values ​​was performed using a paired t-test if the measured values ​​followed a normal distribution, and using the Wilcoxon signed rank test if they did not, with a significance level of 0.05.

[0036] Example 3: Pore Analysis Results of Cheek Replicas 3D analysis of pore replicas taken 0, 4, 8, and 12 weeks after the start of application of the test formulation was performed. Statistical analysis revealed a significant improvement in the pore aspect ratio (mean) (p<0.001 at 8 weeks) (Figure 1). Furthermore, a trend toward a reduction in pore area (mean) was observed, although not significant (p=0.11) (Figure 2). These results demonstrate that a composition containing glycylglycine and retinol can be used to improve sagging pores, improve the aspect ratio of pore shape, and reduce pore size.

[0037] Example 4: Analysis results from VISIA images Analysis of the appearance images acquired with VISIA revealed significant or decreasing trends in pore and wrinkle scores, as shown in Table 1 below and Figure 3. These results demonstrate that a composition containing glycylglycine and retinol can be used to reduce pore size and improve wrinkles.

[0038]

[0039] Example 5: Analysis of measurement device data As a result of analyzing the stratum corneum moisture content, softness, and elasticity obtained by the measurement device, significant improvements or trends of improvement were observed in the stratum corneum moisture content, softness, and elasticity, as shown in Table 2 below and Figures 4 to 6 ( ＊ p<0.05, ＊＊ p<0.01, ＊＊＊ (Denotes a significance level of p<0.001.) These results demonstrate that compositions containing glycylglycine and retinol can be used to improve skin moisturization and elasticity (firmness).

[0040]

[0041] Example 6: Questionnaire results of test subjects As shown in Figure 7, the results of test subjects also show that they feel that pores are improving.The stacked graph on the left side of Figure 7 shows that the answer to the question of "pores are becoming less noticeable" is "somewhat agree" and "agree" after 12 weeks, and the total of these answers exceeds 80%.The graph on the right side shows the results of analyzing the average of answers by quantifying them, and this graph also shows that the feeling that pores are becoming less noticeable increases significantly.

Claims

1. An agent for improving sagging pores, comprising glycylglycine and retinol.

2. The agent for improving sagging pores according to Claim 1, comprising 0.5% or more and 2.0% or less of glycylglycine.

3. The agent for improving sagging pores according to Claim 1, comprising 0.3×10 ２ IU / g or more and 1.0×10 ５ IU / g or less of retinol.

4. The agent for improving sagging pores according to Claim 1, which improves the aspect ratio of the shape of pores.

5. The agent for improving sagging pores according to Claim 1, which reduces the size of pores.

6. The agent for improving sagging pores according to Claim 1, which improves wrinkles.

7. The agent for improving sagging pores according to Claim 1, which improves the elasticity of the skin.

8. The agent for improving sagging pores according to Claim 1, which improves the moisture retention of the skin.

9. The agent for improving sagging pores according to Claim 2, and any one of Claims 4 to 8, comprising 0.3×10 ２ IU / g or more and 1.0×10 ５ IU / g or less of retinol.

10. An external preparation for skin, comprising the agent for improving sagging pores according to any one of Claims 1 to 8.

11. A beauty method, comprising the step of applying the agent for improving sagging pores according to any one of Claims 1 to 8 or the external preparation for skin according to Claim 10 to the target skin.

12. An agent for improving wrinkles, comprising glycylglycine and retinol.

13. An agent for improving skin elasticity, comprising glycylglycine and retinol.

14. A skin moisturizing improver containing glycylglycine and retinol.