US 2013 0089632A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2013/0089632 A1 Kang et al. (43) Pub. Date: Apr. 11, 2013
(54) COSMETIC COMPOSITION FOR Publication Classification INHIBITING HARLOSS AND ENHANCED HAR GROWTH (51) Int. Cl. A6R8/97 (2006.01) (75) Inventors: Byung Ha Kang, Gyeonggi-do (KR); A61O 700 (2006.01) Woori Bae, Gyeonggi-do (KR); Su Na A68/60 (2006.01) Kim, Gyeonggi-do (KR): Ah Reum (52) U.S. Cl. Kim, Gyeonggi-do (KR); Kyoung Mi USPC ...... 424/770; 514/27: 514/34 Jung, Gyeonggi-do (KR); Eun Joo Kim, Gyeonggi-do (KR); John Hwan Lee, (57) ABSTRACT Gyeonggi-do (KR) The present disclosure provides a cosmetic composition (73) Assignee: AMOREPACIFIC CORPORATION, which includes at least one of Scutellaria baicalensis essence, Seoul (KR) licorice essence, and mixture of Scutellaria baicalensis extract and licorice extract as active ingredient and, option (21) Appl. No.: 13/440,533 ally, further includes at least one of zinc pyrithione, panthenol and thuja semen extract. The cosmetic composition of the (22) Filed: Apr. 5, 2012 present disclosure is capable of inhibiting hair loss and enhancing hair growth by inhibiting binding with the andro (30) Foreign Application Priority Data gen receptor and regulating the hair growth factor so as to Oct. 5, 2011 (KR) ...... 10-2011-O1 O1270 induce transition from telogen to anagen and prolong anagen. Patent Application Publication Apr. 11, 2013 Sheet 1 of 2 US 2013/0089632 A1
FIG. 1 Androgen Receptor Inhibition ASSay 120 100 8O 60 40
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FIG. 2 Growth Factor of TGF- B
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FIG 3 Average number of lost hairs
85 8O 75 70 65 60 s e e s . t NS My Sy - Ny: $$$$$$$$$ssN- N'-' N. N. N. N. N. N. N & act as a & A& & 4 s' s' & S. & & & <'s'ssss & st” s” & & 8 & *S SSis esses Average number of lost hairs US 2013/0O89632 A1 Apr. 11, 2013
COSMETC COMPOSITION FOR Although they show hair loss inhibiting effect clinically, their INHIBITING HARLOSS AND ENHANCED mechanism action is not clearly understood. (see Korean HAR GROWTH Patent No. 10-058.1316 and Korean Patent No. 10-0609210) CROSS REFERENCE TO RELATED SUMMARY OF THE INVENTION APPLICATION 0008. The present disclosure is directed to providing a 0001. This application claims priority based on Korean cosmetic composition and a method for application of a cos patent application KR 10-2011-0101270, filed Oct. 5, 2011. metic composition to hair and scalp which includes at least one of Scutellaria baicalensis essence, licorice essence, and FIELD OF THE INVENTION mixture of Scutellaria baicalensis extract and licorice extract as active ingredient. In addition, the cosmetic composition for 0002 The present disclosure relates to a cosmetic compo application to hair and Scalp may further include at least one sition for inhibiting hair loss or enhancing hair growth, and of Zinc pyrithione, panthenol and thuja semen extract for more particularly to a cosmetic composition for inhibiting inhibiting hair loss and enhancing hair growth by inhibiting hair loss or enhancing hair growth including at least one of binding with the androgen receptor and inhibiting the activity Scutellaria baicalensis essence, licorice essence, and mixture of Scutellaria baicalensis extract andlicorice extract as active of the hair growth factor. ingredient. 0009. In one general aspect, the present disclosure pro vides a cosmetic composition including at least one of Scutel BACKGROUND OF THE INVENTION laria baicalensis essence, licorice essence, and mixture of Scutellaria baicalensis extract and licorice extract as active 0003 Hair is generated with skin and the hair growth cycle ingredient. In an exemplary embodiment of the present dis consists of anagen (3-5 years), catagen (1-2 months) and closure, the Scutellaria baicalensis essence may include at telogen (3-5 months). During the anagen phase, the dermis least 4 wt % of baicalin based on the total weight of the and the hypodermis are developed. Hair follicles grow in the Scutellaria baicalensis essence and the licorice essence may papillary dermis of the dermis. During the catagen phase, the include at least 3 wt % of glycyrrhizic acid based on the total hair follicles come closer to the epidermis as the thickness of weight of the licorice essence. the dermis decreases. Dermal papilla fall off from the hair 0010. In an exemplary embodiment of the present disclo follicles and a new hair growth cycle begins. sure, the Scutellaria baicalensis extract may include 0.01 0004 Hair loss can be classified into telogen effluvium 100 ppm of baicalin and the licorice extract may include and anagen effluvium according to the stage of hair shedding. 0.01-100 ppm of glycyrrhizic acid. Telogen effluvium may be caused by the male hormone 0011. In an exemplary embodiment of the present disclo androgen, childbirth or endocrine disease. Anagen effluvium Sure, the composition may further include at least one includes alopecia greata, cicatricial greata and hair loss selected from a group consisting of zinc pyrithione, panthenol caused by tinea capitis. Also, focal infection, endocrine dis and thuja semen extract. order, genetic factors, autoimmunity, etc. are known to cause 0012. In an exemplary embodiment of the present disclo loss of hair. Sure, the composition may include Scutellaria baicalensis 0005. A variety of signal transduction factors induce hair essence, licorice essence, Zinc pyrithione, panthenol and loss during the hair growth cycle. Growth factors such as thuia semen extract. Insulin-like growth factor 1 (IGF-1), epidermal growing fac 0013. In an exemplary embodiment of the present disclo tor (EGF), fibroblast growth factor (FGF), etc. promote hair Sure, the composition may include Scutellaria baicalensis growth and prevent death of hair cells, whereas Interleukin-1 extract, licorice extract, Zinc pyrithione, panthenol and thuia (IL-1) and tumor necrosis factor (TNF) cause hair loss by Semen eXtract. inducing death of hair cells and transforming growth factor 0014. In an exemplary embodiment of the present disclo B1 (TGF-31) inhibits hair growth. Among the male hor Sure, the composition may be for inhibiting hair loss or mones, androgen is known to reduce the hair growth and enhancing hair growth. cause degeneration of hair. 0015. In an exemplary embodiment of the present disclo 0006 Currently, representative treatments for hair loss Sure, the composition and method may inhibit hair loss or include Propecia and minoxidil approved by the USFDA. enhance hair growth by inhibiting the activity of the hair Although these drugs show obvious clinical effects, they have growth factor. side effects such as sexual dysfunction and skin irritation and 0016. In an exemplary embodiment of the present disclo are unavailable or limited for use in women. Recently, natural Sure, the composition and method may inhibit hair loss or products which are safe can be used regardless of sex and enhance hair growth by inhibiting the proliferation of the have been actively explored. androgen receptor. 0007 Korean Patent No. 10-058.1316 discloses a compo 0017. In an exemplary embodiment of the present disclo sition for inhibiting hair kiss and enhancing hair growth, Sure, the Scutellaria baicalensis essence and the licorice which comprises a herbal extract mixture of Leonurus sibiri essence may be respectively included in an amount of 0.01 cus, spikenard, mother chrysanthemum, peach kernel, cornus 2.0 wt % based on the total weight of the composition. fruit, cuscuta semen, Schisandra chinensis, atractylodes rhi 0018. In an exemplary embodiment of the present disclo Zome, pine needle and Angelica gigas. Korean Patent No. Sure, the Scutellaria baicalensis extract and the licorice 10-0609210 discloses a shampoo composition for inhibiting extract may be respectively included in an amount of 0.01-2.0 hair loss, which comprises ethanol extracts of Angelica gigas wt % based on the total weight of the composition. root and burdock root wherein B-sitosterol included in the 0019. In an exemplary embodiment of the present disclo Angelica gigas root Suppresses 5C-reductase and inulin Sure, the Zinc pyrithione may be included in an amount of included in the burdock root improves blood circulation. 0.01-2.0 wt % based on the total weight of the composition. US 2013/0O89632 A1 Apr. 11, 2013
0020. In an exemplary embodiment of the present disclo 0031. The main ingredient baicalin of the Scutellaria sure, the panthenol may be included in an amount of 0.01-2.0 baicalensis essence is represented by the chemical formula 1: wt % based on the total weight of the composition. 0021. In an exemplary embodiment of the present disclo (I) Sure, the thuja semen extract may be included in an amount of O OH 0.01-2.0 wt % based on the total weight of the composition. HO ul- OH BRIEF DESCRIPTION OF THE DRAWINGS O 0022 FIG. 1 shows the effect of a composition according OH to an embodiment of the present disclosure on the binding with the androgen receptor, O O 0023 FIG. 2 shows the effect of a composition according to an embodiment of the present disclosure on the hair growth HO factor, and 0024 FIG. 3 shows the hair loss inhibiting effect of a OH O composition according to an embodiment of the present dis closure. 0032 Scutellaria baicalensis Georgi is a perennial herb in the Lamiaceae family. The root of Scutellaria baicalensis is DETAILED DESCRIPTION OF THE INVENTION used as medicine. In Oriental medicine, Scutellaria baicalen sis is frequently prescribed for the people who have high body 0025 Hereinafter, exemplary embodiments will be temperatures and feel fever and severe thirst. According to the described in detail with reference to the accompanying draw External Medicine chapter of Dongui Bogam, “Those who go ings. bald or lose hair when young tend to have dry blood owing to strong fire.” Indeed, more than 90% of those with male pattern 0026. The present disclosure provides a cosmetic compo baldness Suffer from inflammatory conditions on the scalp sition and a method for applying a cosmetic composition Such as fever and troubles. Accordingly, Scutellaria baicallen comprising at least one of Scutellaria baicalensis essence, sis having fever-relieving effect is prescribed for many licorice essence, and mixture of Scutellaria baicalensis patients with hair loss and antifebrile prescriptions such as extract and licorice extract as active ingredient. Xie Jin Dan described in Jing Yue Quan Shu and Samulhae 0027. The composition may further comprise at least one gitang described in Dongui Bogam contain Scutellaria selected from a group consisting of zinc pyrithione, panthenol baicalensis. and thuja semen extract. More specifically, the composition 0033. The Scutellaria baicalensis essence used in the may comprise Scutellaria baicalensis essence, licorice present disclosure may be extracted in various ways or pur essence, Zinc pyrithione, panthenol and thuja semen extract. chased. The Scutellaria baicalensis essence may be extracted Also, it may comprise Scutellaria baicalensis extract, licorice by the commonly employed method. Also, commercially extract, Zinc pyrithione, panthenol and thuia semen extract. available Scutellaria baicalensis essence may be purchased 0028. The cosmetic composition according to the present for use. For example, the Scutellaria baicalensis essence may disclosure may be for inhibiting hair loss or enhancing hair be prepared in the following manner. Distilled water (10 L) is growth. The composition may inhibithair loss or enhance hair added to dried Scutellaria baicalensis (1 kg) and reflux growth by inhibiting the activity of the hair growth factor. extraction is performed 3 times for at least 2 hours at 70-100° Also, the composition may inhibit hair loss or enhance hair C. Then, following sedimentation at 15° C. for 1 day and growth by inhibiting the proliferation of the androgen recep separation of filtrate and residue via filtration through filter tor. Test examples below disclose the effect. cloth and centrifugation, the separated filtrate is concentrated 0029. The Korean Pharmacopoeia defines essence as a under reduced pressure at 60° C. or below to obtain 400 g of preparation obtained by concentrating a herb leachate. It is Scutellaria baicalensis extract. The obtained Scutellaria prepared by leaching herb by cold leaching or hot leaching baicalensis extract has weight after drying of between 36% after adding a leaching agent, followed by filtration and con and 54%. It is finally sterilized at 121°C. for 30 minutes to centration or drying. The pharmacopoeia also prescribes that, obtain the Scutellaria baicalensis essence. Thus prepared differently from normal extracts, the essence contains the Scutellaria baicalensis essence may comprise 4 wt % or more main ingredient of the herb with a specific content. Whereas of baicalin as main ingredient. the normal extract contains the main ingredient in a trace 0034. In the present disclosure, the Scutellaria baicalensis amount of several ppm and a large amount of water Such that essence may be included in an amount of 0.01-2.0 wt % based the weight after drying is only 2-3% or less, the essence on the total weight of the composition for inhibiting hair loss contains the main ingredient in an amount of several % or and enhancing hair growth. When the content of the Scutel more, with the weight after drying up to 50%. That is to say, laria baicalensis essence is less than 0.01 wt %, the desired the essence is highly concentrated and has a high content of effect may be only slight. And, when the content exceeds 2 wt thousands to tens of thousands times that of the normal %, safety problems such as scalp irritation and trouble are eXtract. likely to occur. 0030 The Scutellaria baicalensis essence may contain 4 0035. The licorice essence may contain 3 wt % or more, wt % or more, specifically 4-30 wt %, of baicalin as main specifically 3-30 wt %, of glycyrrhizic acid as main ingredi ingredient. ent. US 2013/0O89632 A1 Apr. 11, 2013
0036. The mainingredient glycyrrhizic acid of the licorice 0041. The Scutellaria baicalensis extract and the licorice essence is represented by the chemical formula 2: extract used in the present disclosure may be prepared by the commonly employed extraction method. 0042. The Scutellaria baicalensis extract contains baica (2) lin inless content than the Scutellaria baicalensis essence and the licorice extract contains glycyrrhizic acid in less content than the licorice essence. The Scutellaria baicalensis extract may contain less than 4 wt %, more specifically 0.01-100 ppm, most specifically 1-10 ppm, of baicalin, although the content of the ingredients for general extract varies depending on many conditions such as extracting method and origin of HOOC herb etc so not being particularly limited thereto. And, the HO HO licorice extract may contain less than 3 wt %, more specifi HOOC cally 0.01-100 ppm, most specifically 1-10 ppm, of glycyr HO rhizic acid, although not being particularly limited thereto. HO 0043. A mixture of Scutellaria baicalensis extract and licorice extract used in the present disclosure may be either one obtained by extracting Scutellaria baicalensis and lico 0037 Licorice belongs to the Fabaceae family. In Korea rice together or one obtained by extracting Scutellaria and Japan, the root and stem of licorice (Glycyrrhiza uralen baicalensis extract and licorice extract separately and mixing sis Fischer), European licorice (Glycyrrhiza glabra L.) or them. other plants of the same genus are used with or without the 0044 Zinc pyrithione used in the present disclosure is bark removed. In China, the dried root of Glycyrrhiza uralen represented by the chemical formula 3: sis Fischer, Glycyrrhiza glabra L. or Glycyrrhiza inflata Batal is used. In Oriental medicine, licorice is known to improve the medicinal efficacy of other medicine by harmonizing the (3) effect thereof and to improve blood circulation by controlling chillness, fever and poison of internal organs. Since it has anti-inflammatory effect, it is prescribed for dermatitis, n Zn2 eczema, peptic ulcer, or the like. 0038 Si Jun Zi Tang described in Yi Fang Ji Jie or Si Ni Tang described in Yixue Rumen includes licorice. Si Jun Zi Tang is known to be effective for hair loss and Si Ni Tang is prescribed for hair dryness. 0045 Zinc pyrithione is an antifungal agent having anti 0039. The licorice essence used in the present disclosure fungal effect of inhibiting the growth of the dandruff-causing may be extracted in various ways or purchased. The licorice fungus. It is included in various haircare products Such as essence may be extracted by the commonly employed shampoo, rinse, etc. for treating dandruff and scalp irritation. method. Also, commercially available licorice essence may In the present disclosure, the Zinc pyrithione may be included be used. For example, the licorice essence may be prepared as in an amount of 0.01-2.0 wt % based on the total weight of the follows. Driedlicorice (1 kg) is cut and crushed into appro composition for inhibiting hair loss and enhancing hair priate size and, after adding purified water (5 L), macerated at growth. When the content of the licorice essence is less than room temperature for at least 48 hours. Then, after separating 0.01 wt %, the desired effect may be only slight. And, when filtrate and residue using cotton filter cloth, followed by con the content exceeds 2 wt %, stability problem may occur. centration under reduced pressure at 60° C. or below, the 0046 Panthenol used in the present disclosure may either product is macerated again for 12 hours by adding purified D-panthenol or DL-panthenol and is represented by the water (3 L) and filtered through cotton filter cloth. This pro chemical formula 4: cedure is repeated 3 times. Thus obtained filtrate is combined and concentrated under reduced pressure to a total Volume of 3 L. After adding ethanol (1 L), keeping at cool place for at (4) least 48 hours, residue and filtrate are separated by filtering CH3 through cotton filter cloth. The obtained filtrate is concen trated under reduced pressure at 60°C. and finally sterilized at 121° C. for 30 minutes to obtain the licorice essence. Thus CH, OH preparedlicorice essence may comprise 3 wt % or more, more specifically 4 wt % or more, of glycyrrhizic acid as main 0047 Panthenol, which is an analog of pantothenic acid, is ingredient. a provitamin of Bs. In organisms, it is quickly converted to 0040. In the present disclosure, the licorice essence may Vitamin Bs. In cosmetics, panthenol is commonly used as be included in an amount of 0.01-2.0 wt % based on the total humectant, emollient and moisturizer. It is used to prevent weight of the composition for inhibiting hair loss and enhanc inflammation and irritation, soften hair and enhance hair ing hair growth. When the content of the licorice essence is strength. less than 0.01 wt %, the desired effect may be only slight. 0048. In the present disclosure, the panthenol may be And, when the content exceeds 2 wt %, safety problems such included in an amount of 0.01-2.0 wt % based on the total as Scalp irritation and trouble are likely to occur. weight of the composition for inhibiting hair loss and enhanc US 2013/0O89632 A1 Apr. 11, 2013
ing hair growth. When the content of the licorice essence is 0056. The cosmetic composition of the present disclosure less than 0.01 wt %, the desired effect may be only slight. may further comprise an anionic Surfactant. Alkyl Sulfate, And, when the content exceeds 2 wt %, stability problem may ethoxylated alkyl sulfate, alkyl ethoxycarboxylate, alkyl OCCU. glyceryl ether Sulfonate, ethoxyether Sulfonate, methyl acyl 0049. Thuja semen is the seed of Thuja Orientalis of the taurate, alkyl SulfoSuccinate, alkyl ethoxysulfoSuccinate, Curpressaceae family. It is oval, elliptical or cylindrical in C-Sulfonated fatty acid, salts and/oresters thereof, alkylphos shape, about 3-5 mm long and about 2-3 mm in diameter. phate ester, ethoxylated alkyl phosphate ester, straight-chain According to Dongui Bogam, thuja semen is used in Sam alkyl benzenesulfonate, paraffin Sulfonate, C-olefin Sul Senggo to grow lost mustache or hair. It is also included in Si fonate, alkyl alkoxysulfate and mixtures thereof may be used Sheng Bu Lao Dan or Ban Long Wan, which are prescribed as the anionic Surfactant. The Surfactant may have an alkyl for lack of vitality or symptoms of aging. Also, in modern and/or acyl chain which is Cls, specifically C2a, long. Scientific experiments using two animal models, thuja semen When the chain length is shorter than C2, Surfactant power was proven to have high hair growth activity by regulating the decreases. And, when the chain length exceeds Cs, foaming conversion of androgen. power decreases. In an exemplary embodiment of the present 0050 For example, the thuia semen extract may be pre disclosure, the anionic Surfactant may be included in an pared as follows. Thuja semen is extracted with 2 equivalent amount of 1-50 wt %, specifically 5-20 wt %, based on the volume of 95% ethanol, filtered, concentrated, and then agi total weight of the composition. When the content is less than tated in 5 equivalent volume of water and 5 equivalent volume 1 wt %, cleansing power may be insufficient. And, when the of ethyl acetate for phase separation. The ethyl acetate layer is content exceeds 50 wt %, excessive cleansing power and irritation to the human body are undesirable. dried with magnesium sulfate, filtered and concentrated to 0057 The cosmetic composition of the present disclosure obtain the thuia semen extract. may further comprise a cationic polymer Such as polymeric 0051. In the present disclosure, the thuja semen extract quaternary ammonium salt of hydroxyethyl cellulose, guar may be included in an amount of 0.01-2.0 wt % based on the hydroxypropyl triammonium chloride, or the like. The cat total weight of the composition for inhibiting hair loss and ionic polymer conditions hair, Smoothens hair Surface and enhancing hair growth. When the content of the thuia semen improves foaming power. In an exemplary embodiment of the extract is less than 0.01 wt %, the desired effect may be only present disclosure, the cationic polymer may be included in slight. And, when the content exceeds 2 wt %, stability prob an amount of 0.1-1.0 wt %, specifically 0.1-0.5 wt %, based lem may occur. on the total weight of the composition. When the content is 0052 That is to say, the present disclosure provides a less than 0.1 wt %, the desired effects cannot be expected. cosmetic composition for application to hair and Scalp having And, when the content exceeds 1.0 wt %, viscosity control is hair loss inhibiting effect, which comprises at least one of the difficult and the user may feel uncomfortable because of Scutellaria baicalensis essence that inhibits binding with the excessive adhesiveness to hair. androgen receptor, the licorice essence that inhibits the activ 0058. The cosmetic composition of the present disclosure ity of the hair growth factor inducing catagen, the Zinc may comprise silicone as conditioning ingredient. The sili pyrithione that prevents dandruff and hyperkeratinization, the cone for hair conditioning may include cyclomethicone, panthenol that provides nutrients to hair, and the thuia semen dimethicone (polydimethylsiloxane), dimethicone copolyol. extract that inhibits 5C-reductase. alkyl dimethicone copolyol, silicone ester, fluorodimethi 0053. When the Scutellaria baicalensis extract and the cone, alkyldimethicone, dimethicone copolyolamine, car licorice extractare included together in the composition of the boxysilicone, silicone phosphate ester, silicone resin, silicone present disclosure, they provide excellent synergic effect of phospholipid, amodimethicone, aminopropyl dimethicone inhibiting hair loss and enhancing hair growth as compared to and silicone quartz. The silicone may be included in an when each extract is included alone. amount of 0.01-5.0 wt %, specifically 1.3-3.0 wt %, based on 0054 When any one of the Scutellaria baicalensis essence the total weight of the composition. When the content is less and the licorice essence is included alone in the composition than 0.01 wt %, the desired conditioning effect cannot be of the present disclosure, it provides excellent effect of inhib expected. And, when the content exceeds 5.0 wt %, stability itinghair loss and enhancing hair growth in case ofessence. In and quality problems may arise. addition, when at least one selected from a group consisting 0059. The composition according to the present disclosure of Zinc pyrithione, panthenol and thuja semen extract is fur may further comprise pigment, antiseptic, sequestrant, flavor, ther added to the cosmetic composition comprising at least etc. in an amount not negatively affecting stability. one of Scutellaria baicalensis essence, licorice essence, and 0060. The examples and experiments will now be mixture of Scutellaria baicalensis extract and licorice extract described. The following examples and experiments are for as active ingredient, they provide better effect of inhibiting illustrative purposes only and not intended to limit the scope hair loss and enhancing hair growth as compared to when of this disclosure. only one of Zinc pyrithione, panthenol and thuia semen extractis included or when none of zinc pyrithione, panthenol Comparative Example 1 and thuja semen extract is added to one or more of Scutellaria 0061 Preparation of Scutellaria baicalensis extract 80% baicalensis essence, licorice essence, and mixture of Scutel ethanol aqueous solution (5 L) and other ingredients laria baicalensis extract and licorice extract. described in Table 1 were added to dried Scutellaria baicallen 0055. The cosmetic composition of the present disclosure sis (1 kg). After performing reflux extraction for 3 times, is for application to the scalp and hair. The cosmetic compo followed by sedimentation at 15° C. for 1 day, residue and sition of the present disclosure may be in the form of hair filtrate were separated by filtration through filter cloth and cleanser, hair lotion, shampoo or rinse, but is not limited centrifugation. The separated filtrate was concentrated under thereto. reduced pressure to obtain Scutellaria baicalensis extract. US 2013/0O89632 A1 Apr. 11, 2013
Comparative Example 2 0068. The LNCaP cells that had been cultured for 24 hours 0062 Preparation of licorice extract 80% ethanol aqueous were treated with the compositions of Comparative Examples solution (5 L) and other ingredients described in Table 1 were 1-2 and Examples 1-14 on a 96-well plate and then cultured added to driedlicorice (1 kg). After performing reflux extrac for 48 hours in an incubator. Cell viability of the cultured cells tion for 3 times, followed by sedimentation at 15°C. for 1 day, was measured using the WST-1 reagent. The result is shown residue and filtrate were separated by filtration through filter in Table 2 and FIG. 1. cloth and centrifugation. The separated filtrate was concen trated under reduced pressure to obtain licorice extract. TABLE 2 Example 1 Cell viability (%) 0063. The composition of Example 1 was prepared by Non-treated1 IMDHT group 1OO118.7 adding 0.1 wt % of the Scutellaria baicalensis extract pre- 1 IM flutamide 89.2 pared in Comparative Example 1 and 0.1 wt % of the licorice Comparative Example 1 119.1 extract prepared in Comparative Example 2. Comparative Example 2 120.3 Example 1 117.4 Examples 2-14 Example 2 98.9 Example 3 99.1 0064. The compositions of Examples 2-14 were prepared Example 4 87.2 as described in Table 1. TABLE 1.
Comp. Comp. Ex. Ex. Ex. Ex. Ex. Ex. Ex. Ex. Ex. Ex. Ex. Ex. Ex. Ex. Ex. 1 Ex. 2 1 2 3 4 5 6 7 8 9 10 11 12 13 14 Ingredients (unit wt %) Purified water To 100 Scuteilaria baicaiensis O.1 O.1 O.1 O.1 O.1 O.1 O.O09 2.01 (SSECC Licorice essence O.1 O.1 O.1 O.1 O.1 O.1 O.O09 2.01 Thitia semen O.2 O2 O2 — 02 O2 O2 extract Zinc pyrithione O6 O.6 0.6 — O6 O6 solution (48%) Panthenol 1 1 1 Scuteilaria baicaiensis O.1 O.1 O.1 O.1 O.1 extract Licorice extract O.1 O.1 O.1 O.1 O.1 Ammonium lauryl 30 30 30 30 30 30 30 30 30 30 30 30 30 30 30 30 Sulfate solution (25%) Ammonium laureth 2O 2O 2O 2O 2O 2O 2O 2O 2O 2O 2O 2O 2O 2O 2O 2O Sulfate solution (25%) Lauryl dimethyl 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 amine oxide solution (35%) Cocamide MEA 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 Cetyl alcohol O.S O.S O.S O.S O.S O.S 5 5 5 5 5 O.S 5 5 5 5 Polyguaternium 10 O.S O.S O.S O.S O.S O.S O.S O.S O.S O.S O.S O.S O.S O.S O.S O.S Fragrance 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1
Test Example 1 TABLE 2-continued Androgen Receptor Inhibition Assay Cell viability (%) Example 5 116.8 0065 Androgen receptor inhibition assay was carried out Example 6 116.6 in vitro using LNCaP cells having the androgen receptor and Example 7 110.9 using the compositions of Comparative Examples 1-2 and Example 8 95.1 Examples 1-14. Example 9 93.9 Example 10 83.1 0066. Since LNCaP cells show increased proliferation Example 11 80.9 when treated with dihydrotestosterone (DHT), DHT was used Example 12 75.5 as negative control. And, since treatment with flutamide Example 13 115.1 reduces proliferation of the cells, the androgen receptor Example 14 88.1 inhibitor flutamide was used as positive control. 0067. The human prostate cancer cell line LNCaP cells 0069. As seen from Table 2 and FIG. 1, Examples 2 and 3, were acquired from the American Type Culture Collection in which the cells were treated respectively with the Scutel (Manassas, Va., USA) and cultured for 24 hours in RPMI laria baicalensis essence and the licorice essence of the 1640 medium containing 10% fetal bovine serum (FBS) and present disclosure, and Example 5, in which the cells were 2 mM 1-glutamine in an incubator maintained at 5% CO and treated with the Scutellaria baicalensis essence and the lico 370 C. rice essence at the same time, showed significantly increased US 2013/0O89632 A1 Apr. 11, 2013 inhibition of cell viability as compared to Comparative pyrithione+panthenol in addition to the Scutellaria baicalen Examples 1 and 2, in which the cells were treated the Scutel sis essence and the licorice essence showed much better inhi laria baicalensis extract and the licorice extract. Examples bition effect against TGF-3. Although Examples 13 and 14 10, 11 and 12, in which the cells were further treated respec also showed better inhibition effect than Comparative tively with thuja semen extract, thuia semen extract+Zinc Examples 1 and 2, the best effect was attained when the pyrithione or thuia semen extract+Zinc pyrithione+panthenol contents of the Scutellaria baicalensis essence and the lico in addition to the Scutellaria baicalensis essence and the rice essence were 0.1 wt %, respectively. licorice essence showed much better inhibition effect. Although Examples 13 and 14 also showed better inhibition Test Example 3 effect than Comparative Examples 1 and 2, the best effect was attained when the contents of the Scutellaria baicallensis Hair Loss Inhibiting Effect essence and the licorice essence were 0.1 wt %, respectively. 0074 Hair loss inhibiting effect was tested for 16 weeks Test Example 2 on 30 subjects who show early hair loss. After use of the compositions of Comparative Examples 1-2 and Examples Activity of Hair Growth Factor 1-14 once a day for 16 weeks, the hairs lost during hair 0070 The effect of the compositions of Comparative washing were collected and counted. The result is shown in Examples 1-2 and Examples 1-14 on the activity of hair Table 4 and FIG. 3. growth factor TGF-B was tested. 0071 iDPc cells (human immortalized dermal papilla TABLE 4 cells) were prepared by transducing human dermal papilla Average number of lost cells into a vector comprising simian virus 40 large T hairSistandard deviation (SV40T) and c-myc. The cells were cultured in Dulbecco's Non-treated group 85.70,1O.S6 modified Eagle's medium (DMEM; Gibco BRL, Gaithers Comparative Example 1 84.99.10.54 burg, Md., USA) containing 20% FBS (Hyclone, Logan, Comparative Example 2 85.30, 10.47 Utah). Example 1 84.23.10.41 0072. The iDPc cells were cultured on a 12-well plate for Example 2 83.12 9.78 24 hours in an incubator at 37° C. and then treated with the Example 3 83.95,981 Example 4 82.248.98 compositions of Comparative Examples 1-2 and Examples Example 5 83.99; 10.39 1-14. 18 hours later, TGF-B inhibition activity was measured Example 6 83.77 10.35 using the ELIZA kit (R&D Systems). The result is shown in Example 7 83.75/10.25 Table 3 and FIG. 2. Example 8 83.09,9.72 Example 9 83.88.9.79 Example 10 82.O3,8.78 TABLE 3 Example 11 81.86,8.79 Example 12 81.23,867 Concentration of Example 13 84.77.9.76 human TGF-B (pg/mL) Example 14 83.SS,924 Non-treated group 224031 Comparative Example 1 1166.26 Comparative Example 2 1422.69 (0075. As seen from Table 4 and FIG.3, Examples 2 and 3, Example 1 1070.59 in which the cells were treated respectively with the Scutel Example 2 880.SS laria baicalensis essence and the licorice essence of the Example 3 890.97 present disclosure, and Example 5, in which the cells were Example 4 750.21 Example 5 1OOO.99 treated with the Scutellaria baicalensis essence and the lico Example 6 999.87 rice essence at the same time, showed significantly decreased Example 7 954.23 number of lost hairs as compared to Comparative Examples 1 Example 8 870.51 and 2, in which the cells were treated the Scutellaria Example 9 880.99 Example 10 740.34 baicalensis extract and the licorice extract. Examples 10, 11 Example 11 730.99 and 12, in which the cells were further treated respectively Example 12 700.78 with thuia semen extract, thuja semen extract+Zinc Example 13 900.12 pyrithione or thuia semen extract+Zinc pyrithione+panthenol Example 14 702.12 in addition to the Scutellaria baicalensis essence and the licorice essence showed much better hair loss inhibition 0073. As seen from Table 3 and FIG. 2. Examples 2 and 3, effect. Although Examples 13 and 14 also showed better hair in which the cells were treated respectively with the Scutel loss inhibition effect than Comparative Examples 1 and 2, the laria baicalensis essence and the licorice essence of the best effect was attained when the contents of the Scutellaria present disclosure, and Example 5, in which the cells were baicalensis essence and the licorice essence were 0.1 wt %, treated with the Scutellaria baicalensis essence and the lico respectively. rice essence at the same time, showed significantly increased inhibition of TGF-3, which inhibits hair growth, as compared Test Example 4 to Comparative Examples 1 and 2, in which the cells were treated the Scutellaria baicalensis extract and the licorice Irritation to Eye extract. Examples 10, 11 and 12, in which the cells were further treated respectively with thuia semen extract, thuja 0076 Eye irritation test was carried out for the composi semen extract+Zinc pyrithione or thuia semen extract--Zinc tions of Comparative Examples 1-2 and Examples 1-14. US 2013/0O89632 A1 Apr. 11, 2013
0077. The compositions of Comparative Examples 1-2 TABLE 7-continued and Examples 1-14 tested on 16-week-old male rabbits (9 per each group). For the rabbits of non-washed groups, 0.1 mL of M.I.O.I. test Substance was introduced into the conjunctival sac of the right eye and observation was made for lesions in the cornea, Day 1 2 3 4 7 I.A.O.I. iris and conjunctiva on days 1, 2, 3, 4 and 7. The rabbits of Example 11 O O O O O O Example 12 O O O O O O washed groups were treated with 0.1 mL of the test substance Example 13 O O O O O O and the treated eyes were washed 30 seconds later. Eye irri Example 14 O 1 1 2 2 8 tancy of the test Substance was evaluated according to Draize's scale for scoring of ocular lesions with reference to Guillots ocular irritation score index. 0079. As seen from Table 6, the composition of Example 7 0078. The scale for scoring of ocular lesions is described was moderately irritating and the composition of Example 14 in Table 5. The evaluation result is shown in Table 6 (non was irritating for the non-washed groups. All the other com washed groups) and Table 7 (washed groups). positions excluding those of Example 7 and Example 14 were non-irritating for the non-washed groups. TABLE 5 0080 And, as seen from Table 7, the composition of the non-treated group, Comparative Examples 1-2 and Example Score 1-14 were non-irritating for the washed groups. I0081. The composition of Example 14 could also be evalu I.A.O.I.* M.I.O.I.** ated as moderately irritating from the I.A.O.T. and M.I.O.I. Non-irritating O-5 0 (after 48 hours) values. Moderately irritating 5-15 s5 (after 48 hours) Irritating 15-30 s5 (after 4 days) Formulation Example 1 *I.A.O.I. (index of acute ocular irritation); maximum value of M.I.O.I. on days 1,2,3,4 and 7 **M.I.O.I. (mean index of ocular irritation); sum of scores for each animal for each obser Preparation of Hair Lotion wation time I0082 Hair lotion was prepared with the following ingre dients and contents according to the commonly employed TABLE 6 method.
M.I.O.I.
Day 1 2 3 4 7 I.A.O.I. Ingredients Contents (%) Non-treated group Comparative Example 1 Beeswax 4.OO Comparative Example 2 Polysorbate 60 1...SO Example 1 Sorbitan sesquiolate O.70 Example 2 Mineral oil 4SO Example 3 Squalane 3.00 Example 4 Isocetyl myristate 3.SO Example 5 Caffeine O.80 Example 6 Glycerin 3.00 Example 7 Dipropylene glycol 3.00 Example 8 Carboxyvinyl polymer O.12 Example 9 Triethanolamine O.24 Example 10 Composition of Example 10 120 Example 11 Antiseptic Adequate Example 12 Fragrance and pigment Adequate Example 13 Purified water To 100 Example 14 Formulation Example 2 TABLE 7 Preparation of Shampoo M.I.O.I. I0083. Shampoo was prepared with the following ingredi Day 1 2 3 4 7 I.A.O.I. ents and contents according to the commonly employed method. Non-treated group Comparative Example 1 Comparative Example 2 Example 1 Example 2 Ingredients Contents (%) Example 3 Example 4 Sodium laureth sulfate 20.60 Example 5 Sodium cocoamphoacetate 14.50 Example 6 Cocamidopropyl betaine 4.30 Example 7 Propylene glycol 1...SO Example 8 Caffeine OSO Example 9 Composition of Example 11 O4O Example 10 Citric acid Adequate US 2013/0O89632 A1 Apr. 11, 2013
-continued 3. The cosmetic composition of claim 1 wherein the Scutel laria baicalensis extract includes 0.01-100 ppm of baicalin Ingredients Contents (%) and the licorice extract includes 0.01-100 ppm of glycyrrhizic Antiseptic Adequate acid. Sodium chloride Adequate 4. The cosmetic composition of claim 1 wherein the com Purified water To 100 position further comprises at least one selected from a group consisting of Zinc pyrithione, panthenol and thuja semen 0084. The cosmetic composition of the present disclosure eXtract. is capable of inhibitinghair loss and enhancing hair growth by 5. The cosmetic composition of claim 4 wherein the com inhibiting binding with the androgen receptor and regulating position comprises Scutellaria baicalensis essence, licorice the hair growth factor So as to induce transition from telogen essence, Zinc pyrithione, panthenol and thuja semen extract. to anagen and prolong anagen. 6. The cosmetic composition of claim 4 wherein the com 0085. Reference throughout this specification to “the position comprises Scutellaria baicalensis extract, licorice embodiment,” “this embodiment,”99 “the&g previous embodi extract, Zinc pyrithione, panthenol and thuia semen extract. ment,” “one embodiment,” “an embodiment,” “an exemplary 7. The cosmetic composition of claim 1 wherein the com embodiment,” “another exemplary embodiment,” “a pre position is for inhibiting hair loss or enhancing hair growth. ferred embodiment” "another preferred embodiment” or 8. The cosmetic composition of claim 7 wherein the com similar language means that a particular feature, structure, or position inhibits hair loss or enhances hair growth by inhib characteristic described in connection with the embodiment iting the activity of the hair growth factor. is included in at least one embodiment of the present disclo 9. The cosmetic composition of claim 7 wherein the com Sure. Thus, appearances of the phrases "in the embodiment.” position inhibits hair loss or enhances hair growth by inhib “in this embodiment.” “in the previous embodiment,” “in one iting the proliferation of the androgen receptor. embodiment,”99 “in& an embodiment.”99 “in& an exemplary 10. The cosmetic composition of claim 1 wherein the embodiment,”99 “in& another exemplary embodiment,”99 “in& a Scutellaria baicalensis essence is included in an amount of preferred embodiment,” “in another preferred embodiment.” 0.01-2.0 wt % based on the total weight of the composition. and similar language throughout this specification may, but 11. The cosmetic composition of claim 1 wherein the lico do not necessarily, all refer to the same embodiment. rice essence is included in an amount of 0.01-2.0 wt % based I0086. Furthermore, the described features, advantages, on the total weight of the composition. and characteristics of the disclosure may be combined in any 12. The cosmetic composition of claim 1 wherein the suitable manner in one or more embodiments. One skilled in Scutellaria baicalensis extract is included in an amount of the relevant art will recognize that the disclosure may be 0.01-2.0 wt % based on the total weight of the composition. practiced without one or more of the specific features or 13. The cosmetic composition of claim 1 wherein the lico advantages of a particular embodiment. In other instances, rice extract is included in an amount of 0.01-2.0 wt % based additional features and advantages may be recognized in on the total weight of the composition. certain embodiments that may not be present in all embodi 14. The cosmetic composition of claim 4 wherein the zinc ments of the disclosure. pyrithione is included in an amount of 0.01-2.0 wt % based on I0087 While the present disclosure has been described in the total weight of the composition. connection with certain exemplary, preferred or specific 15. The cosmetic composition of claim 4 wherein the pan embodiments, it is to be understood that the disclosure is not thenol is included in an amount of 0.01-2.0 wt.% based on the limited to the disclosed embodiments, but, on the contrary, is total weight of the composition. intended to cover various modifications, alternatives, modi fications and equivalent arrangements as will be apparent to 16. The cosmetic composition of claim 4 wherein the thuja those skilled in the art. Any such changes, modifications, semen extract is included in an amount of 0.01-2.0 wt % alternatives, modifications, equivalents and the like may be based on the total weight of the composition. made without departing from the spirit and scope of the 17. A method for inhibiting hair loss or enhancing hair disclosure. growth comprising administering an effective amount of the What is claimed is: composition of claim 1 to a Subject in Such need, wherein the 1. A cosmetic composition comprising at least one of method is for inhibiting hair loss or enhancing hair growth. Scutellaria baicalensis essence, licorice essence, and mixture 18. The method for inhibiting hair loss or enhancing hair of Scutellaria baicalensis extract andlicorice extract as active growth of claim 17, which inhibits hair loss or enhances hair ingredient. growth by inhibiting the activity of the hair growth factor. 2. The cosmetic composition of claim 1 wherein the Scutel 19. The method for inhibiting hair loss or enhancing hair laria baicalensis essence includes at least 4 wt % of baicalin growth of claim 17, which inhibits hair loss or enhances hair based on the total weight of the Scutellaria baicalensis growth by inhibiting the proliferation of the androgen recep essence and the licorice essence includes at least 3 wt % of tOr. glycyrrhizic acid based on the total weight of the licorice SSCC.