WO2005076757A2

WO2005076757A2 - Hair and eyebrow, eyelashes growth stimulater

Info

Publication number: WO2005076757A2
Application number: PCT/KR2005/000198
Authority: WO
Inventors: Jong-Il Kim; Seung-Jin Kim; Hyung-Jin Kim; Sang-Nyun Kim; Sang-Jin Kang; Wan-Goo Cho; Jong-Tae Lee; Hyoung-Kook Park
Original assignee: Lg Household & Health Care Ltd.
Priority date: 2004-01-27
Filing date: 2005-01-25
Publication date: 2005-08-25
Also published as: WO2005076757A3; KR20050077310A

Abstract

Disclosed herein is a composition for stimulating hair, eyebrow and eyelash growth comprising an extract of Polygonum tinctorium or a plant belonging to the same genus as Polygonum tinctorium. The composition exhibits superior effects on hair, eyebrow and eyelash growth.

Description

HAIR AND EYEBROW, EYELASHES GROWTH STIMULATER Technical Field

[1] The present invention relates to a composition for stimulating hair, eyebrow and eyelash growth, and more particularly to a composition for stimulating hair, eyebrow and eyelash growth comprising an extract of Polygonum tinctorium or a plant belonging to the same genus as Polygonum tinctorium, as an active ingredient. Background Art

[2] Normal humans have about 100-150 thousand hairs on the scalp. Each hair undergoes a hair growth cycle consisting of anagen, catagen and telogen phases, and is finally shed. The period of this cycle lasts for 3-6 years. Humans lose 50-100 hairs on average per day. In general, alopecia is a disease caused when the proportion of hairs in the anagen phase is relatively small and that of hairs in the catagen and telogen phases is large in the hair growth cycle, resulting in abnormal hair loss.

[3] As main causes of alopecia, numerous hypotheses have been discussed, for example, poor blood circulation, excessive functioning of male sex hormones, excessive sebum secretion, scalp dysfunction due to the presence of peroxides or bacteria, hereditary factors, aging, stress and the like. Accurate causes of alopecia still remain unknown. People suffering from hair loss are steadily on the rise due to changes in dietary habits and increased stress by complex social environments, etc. Further, the age of alopecia patients is dropping and the proportion of females is increasing.

[4] The most widely used agents for the treatment and prevention of alopecia are minoxidil-containing preparations. Minoxidil is one of two hair growth agents which have been approved by the U.S. Food and Drug Administration (FDA). Minoxidil was originally developed as a drug for the treatment of hypertension with the aim of reducing blood pressure. Since hair growth was observed during use, minoxidil has been used as a hair growth agent. Although the hair growth mechanisms of minoxidil are not fully understood, it is believed that minoxidil expands blood vessels and increases blood flow therethrough to facilitate supply of nutrients to hair roots, resulting in stimulation of hair growth.

[5] Such a model regarding this increased blood flow is indirectly proven by a report that minoxidil enhances the expression of vascular endothelial growth factor (NEGF), which is a growth factor associated with vasodilatation in the dermal papilla as a main cell constituting hair roots (Br. J. of DermatoL, 1998, 138: 407-411). In addition to the vasodilatation effects of minoxidil in the hair growth mechanism, there have been presented reports that minoxidil promotes activation of dermal papilla cells in the hair roots during incubation in vitro (Skin Pharmacol., 1996, 9: 3-8), and promotion the growth of hair follicles in the tissue culture of follicles (J. Invest. DermatoL, 1989, 92: 315-320). These reports suggest that minoxidil may directly act as a growth factor on the hair roots.

[6] In addition, finasteride, a main ingredient of Propecia sold by Merck inhibits the conversion of the male hormone testosterone to dihydrotestosterone, which is a more potent male hormone than testosterone. 1 mg tablet of finasteride as a therapeutic agent against hair loss in men was approved by the U.S. FDA in December, 1997, and is currently present on the market. The tablet turned out to have significant clinical effects, but there has been reports that finasteride inhibits sexual functions of men as a side effect (J. Am. Acad. DermatoL, 1998; 39; 578-589). Since finasteride shows no satisfactory clinical effects, like minoxidil, and may cause the danger of side effects, studies to develop an agent with superior hair growth effects are actively being undertaken.

[7] The present inventors have screened a variety of natural products in order to locate substances with hair growth effects, and as a result, have found that extracts of Polygonum tinctorium belonging to the family Polygonaceae and plants belonging to the same genus as Polygonum tinctorium have superior efficacy on the stimulation of hair, eyebrow and eyelash growth. Polygonum tinctorium belonging to the family Polygonaceae is a 60-90 cm-tall annual grass. The leaves of the natural plant are used in the present invention. Polygonum tinctorium sap has been used to treat insect's bites and festering, and has been used originally as a natural dye. Representative plants belonging to the same genus as Polygonum tinctorium include Periscaria tinctoria H. Gross, Isatis tinctoria, Strobinlanthes flaccidifolius D.C, and the like, whose main ingredients are indican, indoxyl, tryptanthrin, kaempferol, gallic acid, caffeic acid, 3,5,4'-trihydroxy-6,7-methylenedioxy-flavone, 3,5,7,4'-tetrahydroxy-6-methoxy-flavone, indirubin, indigo, isatin, etc. Disclosure of Invention Technical Problem

[8] Therefore, the present invention has been made in view of the above problems, and the present invention provides a composition for stimulating hair, eyebrow and eyelash growth which comprises an extract of Polygonum tinctorium belonging to the family Polygonaceae or a plant belonging to the same genus as Polygonum tinctorium. Technical Solution

[9] The present inventors have earnestly and intensively conducted research to develop novel ingredients capable of stimulating hair, eyebrow and eyelash growth from a variety of natural products, and as a result, have found that extracts of Polygonum tinctorium belonging to the family Polygonaceae and plants belonging to the same genus as Polygonum tinctorium show stimulatory effects on hair, eyebrow and eyelash growth. Thus, it is an object of the present invention to provide a composition for stimulating hair, eyebrow and eyelash growth which comprises, as an active ingredient, an extract of Polygonum tinctorium belonging to the family Polygonaceae or a plant belonging to the same genus as Polygonum tinctorium.

[10] Specifically, the present invention provides a composition for stimulating hair, eyebrow and eyelash growth comprising a primary extract of Polygonum tinctorium leaves as an active ingredient, which is prepared by extracting dried Polygonum tinctorium leaves with at least one solvent selected from methanol (MeOH), ethanol (EtOH), propanol, methyl ethyl ketone, propylene glycol, acetonitrile, and acetone. Preferably, the present invention provides a composition for stimulating hair, eyebrow and eyelash growth comprising a secondary extract of Polygonum tinctorium, which is prepared by further extracting the primary extract with at least one solvent selected from dichloromethane, chloroform (CHC1 ), hexane, and ether.

[11] The composition of the present invention may be formulated into liquids, sprays, gels, pastes, emulsions, creams, conditioners, and shampoos.

[12] The extract of Polygonum tinctorium leaves or a plant belonging to the same genus as Polygonum tinctorium is prepared in accordance with the following procedure.

[13] First, Polygonum tinctorium leaves or a plant belonging to the same genus as Polygonum tinctorium are dried and pulverized, and then a solvent is added thereto. The resulting mixture is macerated at room temperature for 72 hours, filtered, and concentrated to obtain a primary extract. Examples of solvents that can be used in the present invention include distilled water, methanol, ethanol, propanol, methyl ethyl ketone, glycerol, ethylene glycol, propylene glycol, acetonitrile, 1,3-butyleneglycol, ethyl acetate, and acetone. These solvents may be used alone or in combination. Thereafter, the primary extract thus obtained as a crude solvent is suspended in water, and extracted with least one selected from dichloromethane, chloroform, hexane and ether, to obtain a secondary extract. Best Mode for Carrying Out the Invention

[14] The present invention will now be described in more detail with reference to the following examples, including preparative examples.

[15] Preparative Example 1: Preparation of extract from Polygonum tinctorium leaves

[16] After 2 kg of dried Polygonum tinctorium leaves were pulverized, 4L of ethanol (EtOH) was added thereto. The resulting mixture was dipped for 72 hours, filtered, and concentrated to obtain 46g of a primary extract. The primary extract as a crude extract was suspended in water, extracted (500 ml hexane), and purified to obtain 6g of a secondary extract.

[17] Preparative Example 2: Preparation of extract from Isatis tinctoria leaves [18] After 400g of dried Isatis tinctoria leaves were pulverized, 4L of ethanol (EtOH) was added thereto. The resulting mixture was dipped for 72 hours, filtered, and concentrated to obtain 41g of a primary extract. The primary extract as a crude extract was suspended in water, extracted (500 ml hexane), and purified to obtain 5g of a secondary extract.

[19] Example 1. Hair tonics [20] Example 1-1. Preparation of hair tonics containing extract of Polygonum tinctorium leaves

[21] The ingredients were mixed in compliance with the compositions indicated in Table 1 below, stirred, and completely dissolved to prepare three hair tonics.

[22] The effects of Formulation 1 on hair growth were evaluated through an animal experiment in Experimental Example 1 that follows.

[23] Table 1

[24] Example 1-2. Preparation of hair tonics containing extract of Isatis tinctoria leaves [25] The ingredients were mixed in compliance with the compositions indicated in Table 2 below, stirred, and completely dissolved to prepare three hair tonics. [26] The effects of Formulation 1 on hair growth were evaluated through an animal experiment in Experimental Example 2 that follows. [27] Table 2

[28] Example 1-3. Preparation of hair creams containing extract of Polygonum tinctorium leaves

[29] The oil-phase ingredients and aqueous-phase ingredients were mixed in compliance with the compositions indicated in Table 3 below and completely dissolved in separate containers by heating to 80°C. The dissolved oil-phase ingredients and aqueous-phase ingredients at 80°C were combined and emulsified. After completion of the emul- sifϊcation, the respective mixtures were allowed to cool to room temperature. To the mixtures were added a perfume and a colorant, followed by mixing, to prepare three hair creams. Water was added in such an amount that the total weight of the oil-phase and aqueous-phase ingredients was adjusted to 100% by weight.

[30] Table 3

13. Colorant q.s. q.s. q.s.

[31] Example 1-4. Preparation of hair creams containing extract of Isatis tinctoria leaves

[32] The oil-phase ingredients and aqueous-phase ingredients were mixed in compliance with the compositions indicated in Table 4 below and completely dissolved in separate containers by heating to 80°C. The dissolved oil-phase ingredients and aqueous-phase ingredients at 80°C were combined and emulsified. After completion of the emul- sifϊcation, the respective mixtures were allowed to cool to room temperature. To the mixtures were added a perfume and a colorant, followed by mixing, to prepare three hair creams. Water was added in such an amount that the total weight of the oil-phase and aqueous-phase ingredients was adjusted to 100% by weight.

[33] Table 4

[34] Example 1-5. Preparation of shampoos containing extract of Polygonum tinctorium leaves

[35] The ingredients, other than the perfume, colorant and water, were mixed in compliance with the compositions indicated in Table 5 below, and completely dissolved by heating with stirring. The respective mixtures were allowed to cool to room temperature, and then the perfume and colorant were added thereto. Finally, water was added in such an amount that the total weight was adjusted to 100% by weight, to prepare three shampoos.

[36] Table 5

[37] Example 1-6. Preparation of shampoos containing extract of Isatis tinctoria leaves

[38] The ingredients, other than the perfume, colorant and water, were mixed in compliance with the compositions indicated in Table 6 below, and completely dissolved by heating with stirring. The respective mixtures were allowed to cool to room temperature, and then the perfume and colorant were added thereto. Finally, water was added in such an amount that the total weight was adjusted to 100% by weight, to prepare three shampoos.

[39] Table 6

[40] Example 1-7. Preparation of hair conditioners containing extract of Polygonum tinctorium leaves

[41] The oil-phase ingredients and aqueous-phase ingredients were mixed in compliance with the compositions indicated in Table 7 below and completely dissolved in separate containers by heating to 80°C. The dissolved oil-phase ingredients and aqueous-phase ingredients at 80°C were combined and emulsified. After completion of the emul- sifϊcation, the respective mixtures were allowed to cool to room temperature. To the mixtures were added a perfume and a colorant, followed by mixing, to prepare three hair conditioners. Water was added in such an amount that the total weight of the oil- phase and aqueous-phase ingredients was adjusted to 100% by weight.

[42] Table 7

[43] Example 1-8. Preparation of hair conditioners containing extract of Isatis tinctoria leaves [44] The oil-phase ingredients and aqueous-phase ingredients were mixed in compliance with the compositions indicated in Table 8 below and completely dissolved in separate containers by heating to 80°C. The dissolved oil-phase ingredients and aqueous-phase ingredients at 80°C were combined and emulsified. After completion of the emul- sifϊcation, the respective mixtures were allowed to cool to room temperature. To the mixtures were added a perfume and a colorant, followed by mixing, to prepare three hair conditioners. Water was added in such an amount that the total weight of the oil- phase and aqueous-phase ingredients was adjusted to 100% by weight.

[45] Table 8 Unit: wt% (w/w)

[46] Example 2. Eyebrow growth agents [47] Example 2-1. Preparation of eyebrow growth tonics containing extract of Polygonum tinctorium leaves

[48] The ingredients were mixed in compliance with the compositions indicated in Table 9 below, stirred, and completely dissolved to prepare three eyebrow growth tonics.

[49] Table 9

[50] Example 2-2. Preparation of eyebrow growth tonics containing extract of Isatis tinctoria leaves

[51] The ingredients were mixed in compliance with the compositions indicated in Table 10 below, stirred, and completely dissolved to prepare three eyebrow growth tonics. [52] Table 10 Unit: wt% (w/w)

[53] Example 2-3. Preparation of eyebrow growth creams containing extract of Polygonum tinctorium leaves

[54] The oil-phase ingredients and aqueous-phase ingredients were mixed in compliance with the compositions indicated in Table 11 below and completely dissolved in separate containers by heating to 80°C. The dissolved oil-phase ingredients and aqueous-phase ingredients at 80°C were combined and emulsified. After completion of the emulsification, the respective mixtures were allowed to cool to room temperature. To the mixtures were added a perfume and a colorant, followed by mixing, to prepare three eyebrow growth creams. Water was added in such an amount that the total weight of the oil-phase and aqueous-phase ingredients was adjusted to 100% by weight.

[55] Table 11

[56] Example 2-4. Preparation of eyebrow growth creams containing extract of Isatis tinctoria leaves

[57] The oil-phase ingredients and aqueous-phase ingredients were mixed in compliance with the compositions indicated in Table 12 below and completely dissolved in separate containers by heating to 80°C. The dissolved oil-phase ingredients and aqueous-phase ingredients at 80°C were combined and emulsified. After completion of the emulsification, the respective mixtures were allowed to cool to room temperature. To the mixtures were added a perfume and a colorant, followed by mixing, to prepare three eyebrow growth creams. Water was added in such an amount that the total weight of the oil-phase and aqueous-phase ingredients was adjusted to 100% by weight.

[58] Table 12 Unit: wt% (w/w)

[59] Example 2-5. Preparation of eyebrow growth essences containing extract of Polygonum tinctorium leaves [60] The ingredients were mixed in compliance with the compositions indicated in Table 13 below, stirred, and completely dissolved to prepare three eyebrow growth essences. [61] Table 13 Unit: wt% (w/w)

[62] Example 2-6. Preparation of eyebrow growth essences containing extract of Isatis tinctoria leaves [63] The ingredients were mixed in compliance with the compositions indicated in Table 14 below, stirred, and completely dissolved to prepare three eyebrow growth essences.

[64] Table 14

[65] Experimental Example 1 [66] (Test for hair growth effects of Polygonum tinctorium leaf extract) [67] As animals for evaluating the stimulatory effects of the Polygonum tinctorium leaf extract on hair growth, mice (C57BL/6, female) were used. First, hairs around the back of the mice were shaved using an electric razor. Then, the weight of the mice was measured and all the mice were divided into several groups of 8 mice each in such a manner that the weight distribution in each group was constant. After the mice were acclimated to their environments for 1 day, Polygonum tinctorium leaf extract (1%) and Rogaine (containing 5% minoxidil) were applied in an amount of 100 D (0.1% w/v) once daily for 20 days on the shaved back area of each mouse. The level of hair growth in each mouse was determined by calculating a rate (effective area) of the area where new hairs grew in the shaved area, as observed by visual examination.

[68] As can be seen from Table 15, the Polygonum tinctorium leaf extract (1%, Formulation 1 shown in each table) shows noticeable stimulatory effects on hair growth, compared to a control group applied by a vehicle alone. Further, the Polygonum tinctorium leaf extract shows superior efficacy to Rogaine (containing 5% minoxidil). The appearance of the back of the mice in the control and all test groups was compared over the experimental period of 30 days, and as a result, no specific skin irritation was observed.

[69] Table 15

[70] Experimental Example 2 [71] (Test for hair growth effects of Isatis tinctoria leaf extract)

[72] The procedure of Experimental Example 1 was repeated, except that Isatis tinctoria leaf extract was used as a test group. [73] Table 16 Samples Effective area (%) Control group Vehicle 18 Test group Extract of Isatis tinctoria leaves 55 Comparative group | Rogaine (containing 5% minoxidil) | 40

[74] * Effective area (%) = (area where new hair grew)/(total area where hair are shaved) x 100

[75] Based on the above results, the composition of the present invention could be formulated into liquids, sprays, gels, pastes, emulsions, creams, conditioners, shampoos, and the like. In view of commercial applications, hair tonics, hair creams, hair conditioners, and hair shampoos were prepared herein. Further, tonics, creams and essences for eyebrow growth were provided herein. As is evident from the experimental results through the animal tests in Experimental Example 1 and 2, the test groups exhibit superior stimulatory effects on hair, eyebrow and eyelash growth, compared to the control group. Industrial Applicability

[76] The present invention provides a composition for stimulating hair, eyebrow and eyelash growth comprising an extract of Polygonum tinctorium or a plant belonging to the same genus as Polygonum tinctorium, as an active ingredient. The composition of the present invention exhibits excellent stimulatory effects on hair, eyebrow and eyelash growth.

Claims

[1] A composition for stimulating hair, eyebrow and eyelash growth comprising an extract of Polygonum tinctorium or Isatis tinctoria as an active ingredient.

[2] The composition according to claim 1, wherein the extract is present in an amount of 0.1% to 30% by weight, based on the total weight of the composition.

[3] The composition according to claim 1, wherein the extract is a primary extract prepared by using at least one solvent selected from methanol (MeOH), ethanol (EtOH), propanol, methyl ethyl ketone, propylene glycol, acetonitrile and acetone, as an extractant.

[4] The composition according to claim 1, wherein the extract is a secondary extract prepared by extracting the primary extract of claim 3 with at least one solvent selected from dichloromethane, chloroform (CHC1 ), hexane and ether. ₃

[5] The composition according to any one of claims 1 to 4, wherein the composition is formulated in the form of liquid, spray, gel, paste, emulsion, cream, conditioner or shampoo.