WO2018154811A1 - 発毛用皮膚外用剤 - Google Patents

発毛用皮膚外用剤 Download PDF

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Publication number
WO2018154811A1
WO2018154811A1 PCT/JP2017/027536 JP2017027536W WO2018154811A1 WO 2018154811 A1 WO2018154811 A1 WO 2018154811A1 JP 2017027536 W JP2017027536 W JP 2017027536W WO 2018154811 A1 WO2018154811 A1 WO 2018154811A1
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WIPO (PCT)
Prior art keywords
hair growth
saponin
quillaja
mass
hair
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Application number
PCT/JP2017/027536
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English (en)
French (fr)
Japanese (ja)
Inventor
幸蔵 佐藤
佐藤　忠久
哲郎 小島
Original Assignee
株式会社Ｎｉｌ
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Priority claimed from JP2017030996A external-priority patent/JP7051074B2/ja
Application filed by 株式会社Ｎｉｌ filed Critical 株式会社Ｎｉｌ
Priority to CN201780087094.2A priority Critical patent/CN110366409A/zh
Publication of WO2018154811A1 publication Critical patent/WO2018154811A1/ja

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/60—Sugars; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q7/00—Preparations for affecting hair growth

Definitions

  • the present invention relates to an external preparation for hair growth which can exhibit excellent hair growth effect.
  • Patent Documents 1 and 2 there are many commercialized ones such as minoxidil, finasteride, etc.
  • Patent Documents 3 to 6 natural products derived from hair growth and hair growth agents have been developed reflecting the health preference
  • Patent Document 1 describes that minoxidil has a hair growth effect.
  • Minoxidil was developed as an oral drug for high blood pressure, but is currently used as a main effect of the side effect of thickening the hair from its inherent effect. However, it is inherently vasodilating and there is a risk of taking severe symptoms with high doses. The hair growth effect is also limited, and further improvement has been desired.
  • finasteride described in Patent Document 2 is developed by Merck as a prostatic hypertrophy drug that inhibits an enzyme that converts testosterone, which is an androgen, into DHT (dihydrotestosterone), at present, male pattern hair loss It has come to be used as a treatment for AGA.
  • finasteride improves AGA with high probability, it has the side effects of hypogonadism such as decreased libido, erectile dysfunction, and decreased sperm, and is not effective for hair loss by mechanisms other than AGA.
  • finasteride has no effect on women, and even dangerous side effects may occur.
  • Patent Document 3 describes that t-flavanone has a hair growth effect, and although it has been commercialized, the effect is not clear. Furthermore, Patent Document 4 describes a hair restorer containing forskolin as an active ingredient. Patent Document 5 describes a composition for promoting coat-type tissue production, which contains an Erika multiflora derived from the azalea family Erika plant. Patent Document 6 describes a hair loss preventing or hair growth promoting composition containing a secoiridoid glucoside derivative as an active ingredient.
  • the known hair growth agents as described above have certain effects, they have poor efficacy and adaptability, and have side effects, so they have high hair growth effects and are used widely without any side effects.
  • the hair growth agent which can be done has been envyed.
  • an object of the present invention is to provide a safe external hair growth preparation for external use which can be used by both men and women and has an excellent hair growth effect.
  • the inventors of the present invention conducted intensive studies on a hair growth test system in small animals and humans, and found that naturally derived Quillaja saponins and steroid saponins have high hair growth effects, and have completed the present invention.
  • the hair growth skin external preparation of the present invention is characterized in that it contains at least one of quillaja saponins and steroid saponins as an active ingredient.
  • the skin external preparation for hair growth of the present invention exerts an excellent hair growth effect by using at least one of quillaja saponins and steroid saponins as an active ingredient, and since it is a component of natural origin, it is a stimulus to the skin Less is.
  • the steroid saponins are particularly preferably at least one selected from the group consisting of sarsasaponin, timosaponin, digitalis saponin, yamanoimosaponin, and bacmond usaponin. It is preferable at the point which is excellent in the hair effect.
  • the active ingredient when the active ingredient is Quillaja saponin, the concentration of the quillaja saponin is 0.01 to 10.0% by mass, and the steroid saponins as the active ingredient is sarsasaponin.
  • the concentration of salsa saponin is 0.02 to 10.0% by mass, the hair growth effect is more excellent.
  • the skin external preparation for hair growth of the present invention is further preferable because it exhibits remarkable effects when it contains both quillaja saponin and sarsasaponin as active ingredients.
  • the hair growth skin external preparation of the present invention contains, as an active ingredient, at least one of quillaja saponins and steroid saponins. Below, each component of the skin external preparation for hair growth of this invention is explained in full detail.
  • the quillaja saponin used in the present invention is a saponin contained in an extract of quillaja (Quillaja saponaria) bark which is a kind of oleanan saponin and is called a soap tree native to Chile, Peru and Peru in South America. is there.
  • the main aglycone (sapogenin) of quillaja saponin is a triterpene compound (quilayaic acid), and the mixture of its glycosides is called quillaja saponin.
  • the glycoside structure of quillaja saponin is said to be 100 or more.
  • Quillaja saponin is a mixture of many glycosides, so it is preferable to use it in the form of an extract without isolation.
  • the extract contains polyphenols, tannins, sugars and calcium oxalate in addition to quillaja saponins.
  • An extract may be used after filtration and concentration as it is, or a porous adsorption resin or the like may be used to reduce peculiar unpleasant odor contained in the extract.
  • Quillaja saponins have a strong surfactant activity, and have been used for a long time as medicines and soap substitutes, and as emulsifiers in cosmetics and food additives.
  • the hair coloring agent and hair coloring preparation based on the Quillaria product are described in JP-2000-512647, the hair-raising effect is not described, and the hair-raising effect of Quillaja saponin. Has never been known at all.
  • Steroidal saponins are saponins contained in plants such as liliaceae, yamanoimosumi, and solanaceaaceae, and salsa saponin, timosaponin, digitalis saponin, yamanoimo saponin, bacmond usaponin etc. are representative, and they are contained in the molecule. It is a common feature to have a cyclic acetal structure. These steroidal saponins have long been used as herbal medicines because they exhibit strong physiological activities such as cardiac action and diuretic action, but no hair-raising effect has been known so far.
  • the above sarsasaponin is a saponin contained in a yucca extract obtained by extracting with hot water or room temperature to slightly warm water-containing ethanol or water-containing isopropyl alcohol from whole grass of Russicaceae Yucca-Alaborense or L. thulsii-Yucca-Shidigera And 10 or more types of saponins (refer to the 8th edition Food Additives Official Standard (2007)).
  • Salsa saponin is sometimes called yucca saponin.
  • the main saponin of sarsasaponin is S.
  • japonicum-Saponin D1 25 (R, S)-5 b-spirostan-3 b-ol 3-Ob D-xylopyranosyl-(1 ⁇ 3)-[b D-glucopyranosyl-(1 ⁇ 2)]-b D (Glucopyranoside), whose aglycone (sapogenin) is salsasapogenin (a steroid compound) and whose glycoside is salsasaponin (Y. Uematsu et al., J. AOAC International, 83, 1451 (2000) reference).
  • sarsasaponin is a mixture of a plurality of glycosides, it is preferably used in the form of an extract without isolation. Most of the components other than saponin contained in the extract are sugars.
  • the extract may be used as it is or may be used after reducing its color with activated carbon or the like.
  • the timosaponin is a saponin contained in the rhizome of evening primrose, which is a perennial herb of the family Liliaceae, which is native to northern China, and timosaponin AIII, timosaponin BII and the like are known.
  • timosaponin AIII is more preferably used.
  • the above-mentioned digitalis saponin is a saponin obtained from plants of the annual, biennial and perennial plants distributed in more than 20 species from Central Asia to North Africa and Europe mainly on the Mediterranean coast.
  • the Yamanoimosaponin is a saponin contained in a perennial herb of the Yamanoimo family Yamanoimo genus.
  • the above-mentioned Bachmond usaponin is a saponin contained in a root called Janohige of a Liliaceae plant.
  • sarsasaponin and timosaponin are preferable, and sarsasaponin is more preferable.
  • the quillaja saponins and the steroid saponins may be used alone or in combination.
  • the mass ratio of quillaja saponin (A) to steroid saponins (B) is preferably 100: 1 to 1: 100, and more preferably 10: 1 to 1:10.
  • the external preparation for hair growth of the present invention is used in the form of a solution (for example, tonic or lotion), gel, mousse or cream, but is preferably used in the form of solution or mousse.
  • the content of the active ingredient Quillajasaponin and steroid saponins can be appropriately set according to the mode of use.
  • the form of solution eg, tonic
  • it is preferably 0.01 to 20% by mass, more preferably 0.1 to 10% by mass.
  • the content has a clear effect on the content.
  • the content of quillaja saponin is 0.01 to 10.0% by mass
  • that of salsasaponin is 0.02 to 10.0% by mass, respectively. Is preferred.
  • the quillaja saponin is 0.05 to 5.0% by mass and the salsasaponin is 0.1 to 5.0% by mass, respectively.
  • the quillaja saponin is 0.05 to 5.0% by mass and the salsasaponin is 0.1 to 5.0% by mass, respectively.
  • the mass% ratio (A / B) of quillaja saponin (A) to sarsasaponin (B) is preferably 0.01 to 5.0, and particularly preferably 0.05 to 3.0.
  • quillaja saponins and steroid saponins are known hair growth agents such as minoxidil, finasteride, t-flavanone, ginseng extract, chixatetsu carrot extract, cerebrum extract, 6-benzylaminopurine , Adenosine, ethynyl estradiol, forskolin and the like.
  • Organic solvent which can be used include ethanol, isopropanol, propylene glycol, butylene glycol, glycerin and the like, with preference given to ethanol, propylene glycol and butylene glycol.
  • ком ⁇ онен ingredients in the skin external preparation for hair growth of the present invention, if necessary, other components as a surfactant, a penetration accelerator, a moisturizer, a blood circulation enhancer, an anti-inflammatory agent, an antioxidant, an ultraviolet light inhibitor, an antibacterial agent Agents, cell growth promoters, cell differentiation inducers, flavors, oils and fats, enzymes, refreshing agents, vitamins, amino acids, proteins, carbohydrates and the like may be included.
  • quillaja saponin content of quillaja extract shown below is a method of quantifying the four main quillaja saponins using reverse phase high pressure liquid chromatography (RP-HPLC), and taking the total as the content of quillaja saponin (reference document; J Food Agric., 80, 2063-2068 (2000)) or "partially hydrolyzed saponin" obtained as a main product by partially hydrolyzing Quillaja extract is quantified using RP-HPLC, It is determined by any of the methods of multiplying the content of quillaja saponin by multiplying it by a factor (1.67) to convert it to glycosides (D-438 “Quiraya in the Seventh Edition of Food Additives Regulations (1997) Extract)).
  • RP-HPLC reverse phase high pressure liquid chromatography
  • the salsa saponin (yucca saponin) content of yucca extract shown below is a method of extracting the aqueous solution of yucca extract with n-butanol several times, quantifying the amount of saponin extracted and using it as the content (cotton half trading Co., Ltd.'s method, or fractionating the saponin component of Yucca extract with styrene-divinylbenzene adsorption resin, acid hydrolysis under acid heat after heating to convert it to salsasapogenin of common structural part of saponin, and then acidic condition
  • the absorbance at 430 nm of the reaction solution obtained by reaction with p-anisaldehyde below is measured to determine the content of sarsasapogenin, which is multiplied by a factor (2.10) to convert it into a glucoside to obtain sarsasaponin ( D-1652 (Eighth Edition Food Additives Official Standard (2007)) Yucca foam extract "reference)
  • Examples 1 to 31, Comparative Examples 1 to 6 -Hair growth test using a shaved mouse- (1) Preparation of skin external preparation for hair growth
  • the sample solution of the Example and the comparative example was prepared with the following composition.
  • Active ingredient-containing composition An amount (mass%) of the active ingredient to be added as shown in Table 1 -5% by mass of propylene glycol Adjust the total amount of water to 100% by mass
  • a steroid saponin extract other than salsasaponin is prepared by extracting and purifying it from a sample plant according to the method described in JP-A-2000-512647, and the Erika multiflora extract used in the comparative example is disclosed in JP-A 2008-
  • the t-flavanone was synthesized according to the method described in JP-A-2000-198779, and minoxidil, finasteride, and oleuropein were commercially available reagents.
  • mice Eight mice were used per test sample, and digital photography (Nikon COOLPIX S6100) and observation were performed before the start of the test.
  • the analysis of the test results was performed using a digital image of the mouse of each day on a personal computer using "image analysis software NIH-Image". First, the image area of the shaved area of the mouse was counted, and then the image area of the haired area from the image obtained by binarizing the image was counted. From the measured area count of the shaved area and the area count of the hair growth area, the hair growth ratio was calculated by the following equation. For analysis of the results, of the total of 8 mice in each sample, excluding the hair growth ratio of the most frequent haired mouse and the hair growth ratio of the least haired mouse, average the hair growth ratio of 6 mice It was defined as the hair growth rate of the test sample. In addition, the condition of the skin of each mouse was observed to examine the presence or absence of a rash, a rash and the like. The results are shown in Table 1 below.
  • a significant hair growth effect is recognized (hair growth rate of 50% or more in 30 days), and the concentration at which no rash or cabble is observed is 0.01 to 10.0% by mass for quillaja saponin and for sarsasaponin It was 0.02 to 10.0% by mass.
  • finasteride used as an oral drug has a remarkably low hair growth effect under the conditions of this test, as can be understood from its mechanism of action.
  • Examples 32-37 Combined effect of the saponin of the present invention and a known hair growth agent
  • the combined effect of the saponins of the present invention, quillaja saponin and salsasaponin, with a known hair growth agent was examined.
  • Example 1 to Example 1 were used except that Kirayana saponin or salsasaponin, which is an active ingredient, and a known hair growth agent were mixed and used at a ratio shown in Table 2 using Kirayanain D-100 and Sarakeep ALS.
  • the hair growth test was conducted in the same manner as described in 31. The results are shown in Table 2 together with the results of Examples 7 and 21.
  • the effect is determined by taking photographs of the top of the head before and after the test, measuring the rate at which hair growth was observed and ⁇ when 50% or more hair growth, ⁇ when 20 to 50% hair growth In the case of less than 20%, it was considered as x.
  • the feeling of use at the time of the test (Harley, Kosi, combs and others) was evaluated in three levels of ⁇ , ⁇ and x. The evaluation results are shown in Table 3.
  • the preparation method of the hair tonic V shown in Table 4 is shown below.
  • (Preparation of hair tonic V) 19 g of quillaja saponin D-100 (containing 3 g of quillaja saponin) and 44 g of yucca sala saponin (containing 3 g of salsa saponin) were added to 137 g of water to prepare 200 g of Heartonic V (1.5 wt% of quillaja saponin, salsa) Saponin 1.5 wt% solution).
  • Other hair tonics were also prepared according to this method.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
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  • Cosmetics (AREA)
PCT/JP2017/027536 2017-02-22 2017-07-28 発毛用皮膚外用剤 WO2018154811A1 (ja)

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Application Number Priority Date Filing Date Title
CN201780087094.2A CN110366409A (zh) 2017-02-22 2017-07-28 生发用皮肤外用剂

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JP2017-030996 2017-02-22
JP2017030996A JP7051074B2 (ja) 2016-02-24 2017-02-22 発毛用皮膚外用剤

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023238945A1 (ja) * 2022-06-10 2023-12-14 Ｍｅｄ Ｒ＆Ｄ株式会社 繊毛誘導剤

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0386809A (ja) * 1989-06-09 1991-04-11 Dowa Mining Co Ltd アスパラガスサポニン含有化粧品組成物
JPH06505750A (ja) * 1991-03-14 1994-06-30 エル・ヴェー・エム・アッシュ・ルシェルシュ 育毛刺激または抜け毛を抑制するために特に意図されたオキシアカンチン含有化粧用または製薬用、特に皮膚病用組成物
JP2000169320A (ja) * 1998-12-03 2000-06-20 Nippon Zetokku Kk 細胞賦活剤、それを含む皮膚外用剤及び皮膚洗浄剤
JP2002308790A (ja) * 2001-04-06 2002-10-23 Maruzen Pharmaceut Co Ltd テストステロン５α−レダクターゼ阻害剤、アンドロゲン受容体結合阻害剤、抗男性ホルモン剤及び養毛化粧料。
WO2016175559A2 (ko) * 2015-04-28 2016-11-03 (주) 메드빌 지모와 두릅의 복합 추출물을 함유하는 탈모 방지 및 발모 개선용 조성물
JP2017100976A (ja) * 2015-11-30 2017-06-08 株式会社ナノイノベーション研究所 白髪防止用皮膚外用剤並びに白髪防止及び発毛用皮膚外用剤

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2180490A1 (en) * 1972-04-18 1973-11-30 Hemene Luzena Extract of Quillaja saponaria - for treatment of seborrhoea and hair loss
LU81256A1 (fr) * 1979-05-15 1980-12-16 Oreal Composition cosmetique capillaire notamment pour le lavage et/ou le demelage des cheveux,a base d'un extrait de plantes contenant des saponosides
US20060286062A1 (en) * 2005-06-06 2006-12-21 Schep Raymond A Completely natural plant based shampoo and body wash devoid of synthetic ingredients

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0386809A (ja) * 1989-06-09 1991-04-11 Dowa Mining Co Ltd アスパラガスサポニン含有化粧品組成物
JPH06505750A (ja) * 1991-03-14 1994-06-30 エル・ヴェー・エム・アッシュ・ルシェルシュ 育毛刺激または抜け毛を抑制するために特に意図されたオキシアカンチン含有化粧用または製薬用、特に皮膚病用組成物
JP2000169320A (ja) * 1998-12-03 2000-06-20 Nippon Zetokku Kk 細胞賦活剤、それを含む皮膚外用剤及び皮膚洗浄剤
JP2002308790A (ja) * 2001-04-06 2002-10-23 Maruzen Pharmaceut Co Ltd テストステロン５α−レダクターゼ阻害剤、アンドロゲン受容体結合阻害剤、抗男性ホルモン剤及び養毛化粧料。
WO2016175559A2 (ko) * 2015-04-28 2016-11-03 (주) 메드빌 지모와 두릅의 복합 추출물을 함유하는 탈모 방지 및 발모 개선용 조성물
JP2017100976A (ja) * 2015-11-30 2017-06-08 株式会社ナノイノベーション研究所 白髪防止用皮膚外用剤並びに白髪防止及び発毛用皮膚外用剤

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023238945A1 (ja) * 2022-06-10 2023-12-14 Ｍｅｄ Ｒ＆Ｄ株式会社 繊毛誘導剤

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