Composition for preventing hair removal and promoting hair growth

A composition containing specific plant-derived compounds addresses the limitations of current hair loss treatments by inhibiting male hormone activity and promoting hair growth, offering superior efficacy and safety compared to existing products.

JP7688038B2Active Publication Date: 2025-06-03エルジー·エイチアンドエイチ·カンパニー·リミテッド
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Patent Information

Application Number
JP2022547754
Authority / Receiving Office
JP · JP
Patent Type
Patents
Current Assignee / Owner
Filing Date
2020-02-05
Publication Date
2025-06-03
Estimated Expiration
2040-02-05

AI Technical Summary

Technical Problem

Current hair loss prevention and promotion products often have side effects, limited efficacy, and require cautious use, failing to effectively address the complex causes of hair loss such as genetic factors, hormonal influences, and stress.

Method used

A composition containing gypogenin 3-O-β-D-glucuronopyranoside, deapioplatycodine D, Congmunoside X, or Chikusetsusaponin IVa as active ingredients, which inhibits male hormone activity and suppresses the expression of Dkk-1, promoting a transition from the resting phase to the growth phase in the hair cycle.

Benefits of technology

The composition effectively prevents hair loss and promotes hair growth by extending the growth phase and reducing the resting phase of the hair cycle, outperforming existing products like minoxidil in terms of efficacy and safety.

✦ Generated by Eureka AI based on patent content.

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Abstract

The present invention relates to a composition for preventing hair loss and promoting hair growth, which contains an ingredient that induces new hair growth or promotes hair growth. The composition for preventing hair loss and promoting hair growth of the present invention shortens the period during which hair grows from the telogen phase to the anagen phase, thereby promoting hair growth and delaying the transition to the catagen phase, and is therefore highly effective in preventing hair loss and promoting hair growth.
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Description

Technical Field

[0001] The present invention relates to a composition for promoting hair growth, and more particularly to a composition for preventing hair loss and promoting hair growth, which contains a component that induces new hair growth or promotes hair growth.

Background Art

[0002] Recently, as interest in beauty has been increasing, hair also occupies an important part. Hair is produced on the surface of the skin and has a thin and keratinized structure. This serves as a cushion against external impacts, protects the human body from external stimuli such as direct sunlight, cold, friction, and danger, functions to excrete heavy metals such as arsenic, mercury, and zinc harmful to the body outside the body, and is also emphasized in modern times in terms of its aesthetic aspect such as decoration. However, the number of people complaining of hair loss is increasing due to various causes such as changes in diet and increased internal and external stress. Hair loss is known to be mainly caused by genetic factors, but as described above, increased social stress, environmental pollution, frequent perms and hair colors, or improper scalp management are also cited as causes of hair loss.

[0003] Human hair is about 100,000 to 150,000 in number, and each hair has a different growth cycle. The hair growth cycle is composed of three stages, which are classified into the anagen stage where hair grows most actively, the catagen stage where hair degeneration begins, and the telogen stage where hair growth stops or enters a resting period.

[0004] In the regulation of such a hair growth cycle, the activity of outer root sheath cells, including dermal papilla cells and hair follicle stem cells that make up the hair follicle, and various cytokines and growth factors produced by these cells are known to play important roles. For example, DKK-1 (Dickkopf-1) plays an important role in the inhibition and death of hair follicle growth (J Invest.Dermatol, 2008:128(2)). On the other hand, for periodic hair growth, the regeneration of hair follicles and the activation of stem cells must occur, which is known to be carried out by the production and activation of Wnt / β-catenin (Nature 2007:447(7142)).

[0005] Generally, alopecia refers to the situation where, in such a cycle, the proportion of growing-phase hair decreases, the proportion of regressing-phase or resting-phase hair increases, and the abnormal number of hair losses increases. Normal people have more growing-phase hair, while people with alopecia have more resting-phase hair and show a visible hair loss phenomenon to the naked eye. The characteristic of people with alopecia is the miniaturization of hair. As hair loss progresses, the duration of the growing phase becomes shorter, the transition to the regressing phase and the resting phase is promoted, and then the volume of the dermal papilla becomes smaller and the hair follicle becomes increasingly miniaturized. Therefore, for the treatment of hair loss, it is important to quickly return the resting-phase hair follicles to the growing phase and extend the shortened growing phase.

[0006] Male pattern hair loss, which is the type of hair loss that the largest number of hair loss patients belong to, is also called "androgenetic alopecia". Male pattern hair loss commonly appears in young men in their 20s to 30s on average. This is because androgenetic alopecia is affected not only by genetic factors, but also by the action of male hormones and age. The main cause of hair loss in male pattern hair loss has been studied as the male hormone testosterone, and it can be classified in various ways according to the form and progression of the hair loss patches. Male pattern hair loss caused by testosterone occurs when dihydrotestosterone (DHT), which is generated by the binding of the male hormone and the active enzyme 5α-reductase, acts on the hair follicles to suppress cell division and inhibit hair growth.

[0007] The form of hair loss appears differently depending on the distribution pattern of the active enzyme 5α-reductase in the scalp. In the crown area where the active enzyme is highly distributed, cell division is dulled under the influence of DHT, the hair cycle becomes shorter, and vellus hair transformation and hair loss phenomena appear. On the other hand, in the case of the temples and the occipital region, the activity of the active enzyme is relatively weak, and it is less likely to show hair loss under the influence of female hormones. As current management methods for male pattern hair loss, hair transplantation surgery or drug therapy, etc. are being utilized.

[0008] Regarding the causes of hair loss, theories such as excessive male hormone theory, excessive sebum secretion theory, poor blood circulation theory, scalp function decline theory due to peroxides, bacteria, etc., genetic factors, aging, stress, etc. have been proposed, but the cause of hair loss is still not clearly known at present. For such diverse and complex causes of hair loss, currently known hair loss prevention products contain, as active ingredients, components aimed at promoting blood circulation, strengthening hair root function, scalp moisturizing effect, dandruff prevention effect, antioxidant effect, extending the hair growth phase effect, or suppressing male hormone action, etc., but there is still no product that shows remarkable effects, and the problem of side effects may also be raised.

[0009] As preparations for the treatment or prevention of alopecia developed so far, there are preparations mainly containing female hormones for promoting blood circulation, strengthening hair follicle function, moisturizing the scalp, and suppressing male hormones, minoxidil, finasteride, and preparations containing trichosaccharide. Minoxidil (2,4-diamino-6-piperidinopyrimidine-3-oxide), a typical topical alopecia treatment agent, increases blood flow to the scalp, and finasteride, an oral alopecia treatment agent, functions to inhibit the activity of 5α-reductase and reduce the production of DHT, an active form of male hormone. However, the above preparations have many restrictions in use due to side effects or precautions for use.

[0010] On the other hand, Gypsogenin 3-O-β-D-glucuronopyranoside is a component derived from Gypsophila paniculata Linn. and is known to inhibit the action of pancreatic lipase (Chemical and Pharmaceutical Bulletin. Vol 55, 2007, Issue 7).

[0011] Also, Deapioplatycodin D is a component derived from Platycodon grandiflorum (Jacq.) A.DC. and is known to have an effect of suppressing the growth of hepatitis C virus (Evid Based Complement Alternat Med. 2013), an anti-inflammatory effect (Natural Product Sciences, 2008, 14(4): 274~80.), and a bronchoprotective effect by promoting airway mucus secretion (Phytomedicine. 2014 Mar 15; 21(4)).

[0012] In addition, Congmunoside X (also known as Congmuyanoside X and Araloside X) is a component derived from the buds of Aralia chinensis L. of the Aralia genus and is known to have a protective effect on nerve cells (Biomedicine & Pharmacotherapy, Vol 97, January 2018, 152 - 161).

[0013] In addition, Chikusetsusaponin IVa is a component derived from Panax japonicas C.A.Mey. and has an anti - obesity effect by regulating the differentiation of adipocytes (Nutrients 2018, 10(9), 1221), an anti - inflammatory effect (Int J of Immunopathology and Pharmacology 2015, Vol 28(3), 308 - 317), and a protective effect on heart cells (protecting against myocardial damage induced by hyperglycemia) (Scientific Reports vol 5, Article number, 2015, 18123).

[0014] However, the effects of gypogenin 3 - O - β - D - glucuronopyranoside, deapioplatycodin D, Congmunoside X, or Chikusetsusaponin IVa on preventing hair loss or promoting hair growth have not yet been clarified.

Prior Art Documents

Non - Patent Documents

[0015]

Non - Patent Document 1

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Non-Patent Document 9

Summary of the Invention

Problems to be Solved by the Invention

[0016] An object of the present invention is to provide a composition for preventing hair loss or promoting hair growth that is safe for the human body, has no side effects, and has an excellent effect of preventing hair loss or promoting hair growth.

[0017] Another object of the present invention is to provide a product for hair or scalp containing the composition for preventing hair loss or promoting hair growth.

Means for Solving the Problems

[0018] The inventor of the present invention has earnestly studied for the development of a composition that improves problems such as side effects of conventional hair removal agents and precautions in use, is safe for the human body without drawbacks such as negligible hair growth promoting effects of hair removal prevention / hair nourishing agents, and effectively acts on hair growth and hair growth promotion. As a result, it has been found that a composition containing gypso genin 3-O-β-D-glucuronopyranoside, deapioplatycodine D, comminoside X or ticksesaponin IVa as an active ingredient exhibits extremely excellent effects in preventing hair loss and promoting hair growth, and the present invention has been completed.

[0019] Specifically, the inventor of the present invention confirmed that each of the above active ingredients inhibits male hormone activity and has the effect of inhibiting the expression of Dkk-1, which is a regression factor of hair follicles. That is, it was confirmed from in-vitro experiments that each of the above active ingredients inhibits male hormone activity and inhibits the expression of the regression factor of hair follicles, thereby playing an important role in the transition from the regression phase to the active phase of the hair cycle.

[0020] In addition, the inventor of the present invention confirmed that when a hair removal treatment composition containing the above active ingredient is treated on patients with alopecia, it exhibits extremely excellent effects in improving hair thickness, density and elasticity. Furthermore, as a result of a comparative experiment with minoxidil, a commercially available product, it was confirmed that the hair removal treatment composition containing the above active ingredient of the present invention is significantly superior to minoxidil in terms of hair loss prevention and hair growth effects.

[0021] The present invention provides a composition for preventing hair loss or promoting hair growth, which contains one or more selected from the group consisting of gypso genin 3-O-β-D-glucuronopyranoside, deapioplatycodine D, comminoside X and ticksesaponin IVa as an active ingredient.

[0022] In one embodiment, the four active ingredients may be plant-derived components. The gypogenin 3-O-β-D-glucuronopyranoside is a component derived from Gypsophila paniculata Linn., the deapioplatycodin D is a component derived from Platycodon grandiflorum (Jacq.) A.DC., the Congmunoside X is a component derived from the buds of Aralia chinensis L. of the Aralia genus, and the chikusetsusaponin IVa is a component derived from Panax japonicas C.A.Mey.

[0023] In one embodiment, the gypogenin 3-O-β-D-glucuronopyranoside may be contained in an amount of 0.0001 to 50% by weight, preferably 0.001 to 10% by weight, based on the total weight of the composition. The deapioplatycodin D may be contained in an amount of 0.0001 to 50% by weight, preferably 0.001 to 10% by weight, based on the total weight of the composition. The Congmunoside X may be contained in an amount of 0.0001 to 50% by weight, preferably 0.001 to 10% by weight, based on the total weight of the composition. The chikusetsusaponin IVa may be contained in an amount of 0.0001 to 50% by weight, preferably 0.001 to 10% by weight, based on the total weight of the composition.

[0024] When the content of each of the active ingredients is 0.0001 to 50% by weight, preferably 0.001 to 10% by weight, based on the total weight of the composition, it has been found to have excellent effects in preventing hair loss and promoting hair growth in in-vitro experiments or clinically. When the content of the active ingredient is less than 0.0001% by weight based on the total weight of the composition, the effect of promoting hair growth is negligible, and when it exceeds 50% by weight, the stability of the dosage form decreases, which is not desirable.

[0025] In addition, the present invention provides a pharmaceutical composition, a composition for quasi-drugs, a cosmetic composition, or a health functional food composition containing the composition for preventing hair loss or promoting hair growth. The composition of the present invention can be formulated into any form that can be usually applied to the skin, but preferably can be formulated into the form of a topical preparation for the skin. The composition of the present invention can be manufactured into a dosage form applicable to the skin, such as, for example, liquid, cream, paste, or solid form.

[0026] One or more selected from the group consisting of gypgenin 3-O-β-D-glucuronopyranoside, deapioplatycodine D, comminoside X, and ticksusaponin IVa of the present invention may be included as an anti-hair loss agent or a hair growth promoter in the composition or dosage form.

[0027] In one embodiment, when the dosage form of the present invention is a liquid phase, a solvent, a solubilizer, an emulsifier, etc. can be used as a carrier component. For example, water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, 1,3-butyl glycol oil, glycerol fatty acid ester, polyethylene glycol, or sorbitan fatty acid ester, etc. can be used. The alcohol means one or more of the alcohols, and preferably is a linear or branched C2-C4 monoalcohol. In particular, ethanol and isopropanol are preferable, but not limited thereto.

[0028] In one embodiment, when the dosage form of the present invention is a paste, cream, or gel, an animal oil, a vegetable oil, wax, paraffin, starch, tragacanth, a cellulose derivative, polyethylene glycol, silicone, bentonite, silica, talc, or zinc oxide, etc. can be used as a carrier component, and an alcohol can be used. The alcohol is preferably isopropanol, but not limited thereto.

[0029] In one embodiment, when the dosage form of the present invention is a powder or a spray, lactose, talc, silica, aluminum hydroxide, calcium silicate, polyamide powder, or the like can be used as the carrier component. In particular, in the case of a spray dosage form, it may further contain a propellant such as chlorofluorohydrocarbon, propane / butane, or dimethyl ether.

[0030] In one embodiment, the components included in the composition of the present invention may include, in addition to gypogenin 3-O-β-D-glucuronopyranoside, deapioplatymukoside D, comminoside X, and ticksusaponin IVa, components commonly used in topical agents applicable to the skin. For example, it may further contain one or more additives selected from the group consisting of water, surfactants, humectants, alcohols, chelating agents, bactericides, antioxidants, preservatives, pigments, and fragrances.

[0031] The present invention also provides a hair or scalp product containing the composition for preventing hair loss or promoting hair growth. The hair or scalp product may be any one selected from the group consisting of hair tonics, scalp cleansing agents, scalp scaling agents, scalp massage agents, scalp care agents, detergents, shampoos, tonics, hair conditioners, hair lotions, gels, packs, creams, essences, powders, sprays, oils, soaps, ointments, hair styling agents, hair dyes, and perm agents, but is not limited thereto.

[0032] In one embodiment, the composition for preventing hair loss or promoting hair growth of the present invention can be manufactured in the dosage form of a hair tonic or a hair lotion. The composition for promoting hair growth of the present invention can preferably be used by a transdermal administration method such as direct application or sprinkling on the skin.

[0033] In addition, the present invention provides a health functional food composition containing the composition for preventing hair loss or promoting hair growth. The health functional food can be manufactured by a method commonly used in the art, and during the manufacturing process, raw materials and components commonly added in the art can be added for manufacturing. Also, as long as the dosage form of the health functional food is a dosage form recognized as a health functional food, it can be manufactured without limitation. The health functional food of the present invention can be manufactured in various dosage forms, and unlike general drugs, it has the advantage of having no side effects that may occur during long-term administration of drugs using food as a raw material, and is excellent in portability. The health functional food of the present invention can be ingested as an adjuvant for enhancing the effect of preventing hair loss and promoting hair growth.

[0034] In addition, the present invention provides a method for preventing hair loss or promoting hair growth, which includes the step of administering to a subject a composition for preventing hair loss or promoting hair growth, which contains one or more selected from the group consisting of gypgenin 3-O-β-D-glucuronopyranoside, deapioplatycodine D, comminoside X, and ticksussaponin IVa of the present invention as an active ingredient.

[0035] The term "administration" used in the present invention means introducing the composition of the present invention by any appropriate method. The administration route of the composition of the present invention can be by any general route as long as it can reach the intended composition. The composition of the present invention can be administered transdermally or orally, preferably transdermally, and among them, topical application is most preferred. The number of applications of the composition of the present invention can be determined according to the prescription, necessity, or desire.

[0036] The dosage of the composition of the present invention can be appropriately adjusted according to individual differences such as age and the degree of lesions, as well as the dosage form. Usually, it is desirable to apply an appropriate amount to the scalp once to several times a day and use it for one week to several months. In the experimental examples of the present invention, Composition 1 for hair removal treatment was used 7 times a week for 6 months, and as a result, it was confirmed that an excellent effect of promoting hair growth was shown. In particular, a higher effect of preventing hair loss and promoting hair growth was confirmed from the dosage form containing ethanol (Experimental Example 3). The ethanol contained in the dosage form can promote the transdermal absorption of gypogenin 3-O-β-D-glucuronopyranoside, deapioplatycodine D, comminoside X, and ticksusaponin IVa used as active ingredients of the present invention.

[0037] From the above, it was demonstrated that the composition for preventing hair loss or promoting hair growth of the present invention containing gypogenin 3-O-β-D-glucuronopyranoside, deapioplatycodine D, comminoside X, and ticksusaponin IVa as active ingredients can be very effectively used for hair removal treatment. It is obvious to those with ordinary knowledge in the industry that dosage forms such as the above-mentioned hair tonic or hair lotion are only examples of the composition for preventing hair loss or promoting hair growth of the present invention, and the scope of the composition of the present invention is not limited to these dosage forms.

Effects of the Invention

[0038] The composition for preventing hair loss and promoting hair growth of the present invention promotes hair growth by shortening the period of transition from the resting phase to the growth phase in the hair growth cycle, delays the conversion to the regression phase, and has excellent effects of preventing hair loss and promoting hair growth.

Brief Description of the Drawings

[0039]

Figure 1

Figure 2

Figure 3

Figure 4

Mode for Carrying Out the Invention

[0040] Hereinafter, the present invention will be described with reference to specific examples. However, the examples according to the present invention can be changed into other various forms, and it should not be construed that the scope of the present invention is limited to the examples described below. The examples of the present invention are provided to more fully explain the present invention to those having average knowledge in the art.

[0041] Experimental Example 1: Evaluation of Anti-Male Hormone Activity In this experiment, a stable cell line was used, which was obtained by permanently transfecting the androgen receptor-positive 22Rv1 human prostate cancer cell line with the pGL4.36-MMTV-Luc vector containing two androgen response elements and the firefly luciferase reporter gene. This stable cell line was maintained by subculturing using RPMI1640 and 10% fetal bovine serum (Gibco BRL, Gaithersburg, MD, USA). For the transcriptional activation assay, when seeding 25,000 cells per well in a 96-well plate, the culture medium was replaced with phenol red-free RPMI1640 containing 5% charcoal-treated fetal bovine serum. After culturing in an incubator at 37 °C for 48 hours, gypso genin 3-O-β-D-glucuronopyranoside, deapioplatycodine D, comminoside X, or tickesaponin IVa was treated together with 1 nM DHT, and after further culturing for 24 hours, the degree to which the luciferase activity increased by DHT was measured using a Luciferase assay system (Promega). The result values were expressed with the luminescence value of the luciferase increased by 1 M DHT treatment set as 100%, showing the values inhibited by gypso genin 3-O-β-D-glucuronopyranoside, deapioplatycodine D, comminoside X, or tickesaponin IVa. Bicalutamide (casodex) was used as an anti-androgen positive control group, and CCK-8 analysis was performed in parallel to confirm the cytotoxicity by substance treatment. The CCK-8 reagent was treated with the culture medium at a ratio of 1:10 and incubated for 2 hours. After 2 hours, the absorbance of each well was measured at 450 nm. All experiments were repeated three times, the average of the absorbance values was obtained, the value of the 1 nM DHT treatment group was set as 100%, and the values of the treatment groups relative thereto were obtained. The experimental results are shown in Table 1, Table 2, and Figures 1 to 4.

[0042]

Table 1

[0043]

Table 2

[0044] Experimental Example 2: Evaluation of Inhibition of Expression of Follicular Telogen Factor In this experiment, inhibition of the expression of Dkk-1, a follicular telogen marker, was confirmed using human dermal papilla cells (hDPCs). The human dermal papilla cells were purchased from PromoCell. The hDPCs were subcultured at 37 °C and 5% CO 2 under conditions in a follicle dermal papilla cell growth medium (PromoCell, Heidelberg, Germany) containing a supplement mix (PromoCell, Heidelberg, Germany), 100 units / mL of penicillin, and 100 μg / mL of streptomycin. After seeding 1 million of the cultured hDPCs into each 100 mm cell culture dish, they were cultured in an incubator at 37 °C. After 48 hours, they were treated with gypso genin 3-O-β-D-glucuronopyranoside, deapioplatycodine D, comminoside X, or ticksusaponin IVa at 2 ppm or 20 ppm respectively. After 24 hours, the cell culture fluid was obtained and Dkk-1 ELISA analysis (R&D systems, USA) was performed. The amount of protein in each experimental group was confirmed by BCA analysis and corrected by applying it to the Dkk-1 ELISA result value. The analysis results are shown in Table 3 below.

[0045]

Table 3

[0046] Experimental Example 3: Confirmation Test of Hair Growth Effect of Hair Growth Composition 1 (Hair Tonic) Manufacture of Composition 1 (Hair Tonic) for Hair Removal Treatment According to the formulation shown in Table 4 below, a hair tonic composition containing gypogenin 3-O-β-D-glucuronopyranoside, deapioplatymikoside D, comminoside X or ticksessaponin IVa was prepared as Examples 1 to 4-2 by a conventional method.

[0047]

Table 4

[0048] Production of Composition 2 (Hair Lotion) for Hair Removal Treatment According to the formulation shown in Table 5 below, a hair lotion composition containing gypogenin 3-O-β-D-glucuronopyranoside, deapioplatymikoside D, comminoside X or ticksessaponin IVa was prepared by a conventional method.

[0049]

Table 5

[0050] The hair removal treatment composition 1 (hair tonic) of the present invention was divided into 10 groups of 11 people each for a total of 110 men and women with significantly fewer hairs than normal or with weak hairs showing hair loss symptoms. Comparative Examples 1 and 2 and Examples 1 to 4-2 were used on the hair and scalp 7 times a week for 6 months. After use, the degree of improvement (greatly improved: +3, improved: +2, slightly improved: +1, no change: 0, slightly worsened: -1, worsened: -2, greatly worsened: -3) for the items of hair thickness, density, elasticity and overall evaluation was determined by interviewing the users after 6 months and taking the average value, and the results are shown in Table 6.

[0051]

Table 6

Claims

【Claim 1】 An inhibitor of the activity of DHT and the expression of Dkk-1, which is a hair follicle regression factor, comprising one or more selected from the group consisting of gypso genin 3-O-β-D-glucuronopyranoside, deapioplatycodine D, comminoside X, and ticksessaponin IVa.

Citation Information

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