KR101348006B1 - Topical preparations for hair growth - Google Patents

Abstract

The present invention relates to a topical composition for promoting hair growth, and more specifically, henna extract, machi extract, Tabebuia averanedae (Tabebuia-Avellanedae) extract, 4-pyrrolidine 2, 6-diaminopyrimidine 1- A topical composition for preventing hair loss and promoting hair growth by containing 4-pyrrolidine 2, 6-diaminopyrimidine 1-oxide, zinc pyrithione, and orotic acid as an active ingredient. will be.
The composition according to the present invention can suppress normal male- or female-type hair loss and promote hair growth.

Description

Topical preparations for promoting hair growth {Topical preparations for hair growth}

The present invention relates to a topical composition for promoting hair growth, and more specifically, henna extract, machi extract, Tabebuia averanedae (Tabebuia-Avellanedae) extract, 4-pyrrolidine 2, 6-diaminopyrimidine 1- The present invention relates to an external preparation composition for preventing hair loss or promoting hair growth containing oxide, zinc pyrithione and orotic acid as an active ingredient.

Human hair is about 100,000 to 150,000 pieces, each hair is repeated to grow and degenerate through different cycles. Hair is a growing period (Anagen), a degenerative period (Catagen) where metabolic processes slow down while maintaining the shape of the hair, and hair papilla atrophy, hair follicles atrophy gradually, hair roots are pushed upwards, and the hair follicles become smaller (Telogen) The three-step cycle of) is repeated, and the hair cycle and lifespan may vary according to various conditions such as nutrition, medical history, heredity, constitution, hormone secretion or aging.

Alopecia is classified into androgenetic alopecia, female pattern hair loss, alopecia areata, and other causes of alopecia.

Androgenetic alopecia develops male sexual characteristics and is caused by a male hormone called testosterone, a hormone that acts on the development of muscles and the development of male organs during puberty, and this testosterone is a more powerful hormone, dihydrotestosterone, by the enzyme 5a-reductase. When converted to (DHT), the hormone acts on dermal papilla cells present in hair follicles, leading hair follicles to the resting phase from the hair growth phase, causing hair loss.

Gynecologic alopecia is mainly caused by a decrease in the amount of estrogen after menopause. Female alopecia is different from the shape of male alopecia, the head is not removed from the front part of the head is mainly hair loss. In women with alopecia, the association with 5a-reductase is less effective than in men. Thus, drugs that inhibit 5a-reductase have little effect on postmenopausal alopecia women.

The anti-hair loss products known to date are available as commercially available ingredients for promoting blood circulation, inhibiting testosterone action, enhancing hair root function, etc. And problems of side effects have been raised.

Among the existing anti-hair loss treatments, external minoxidil approved by the US FDA, in addition to its vasodilating function as its unique potassium channel opener, induces the growth phase in the resting hair cycle and maintains the induced growth hair cycle. Activity has been reported (British Journal of Dermatology. 2004; 150: 186-194). In addition, an oral administration drug, Finasteride (Propecia; MSD), which inhibits the action of 5 alpha-reductase and inhibits the production of the active male hormone dihydrotestosterone, is marketed as a hair regrowth with the approval of the US FDA.

However, there is a limit to use as the occurrence of expensive and side effects are reported. Thus, there has been a continuing need for drugs that are free of hair growth and side effects compared to the two major drugs previously developed.

The mechanism of the hair growth effect of the minoxidil (2,4-diamino-6 piperidino-pyrimidine-3-oxide), a pyrimidine derivative, is uncertain, due to vasodilation due to calcium channel opening at the time of initial drug development. It is recognized as one. Patents have been applied for hair growth of various derivatives of pyrimidine oxides (US Pat. Nos. 5,034,387 and 4,945,093). The patent for hair growth of pyrimidine oxide derivatives covers a wide range of inducible structures, including the structure of the minoxidil drug, and the hair growth of each individual derivative is generally accepted.

Henna extract has been used as a cosmetic ingredient such as tattoo or hair dye in ancient times in Egypt, the Middle East, Africa and India since ancient times.It has antipyretic, astringent and antibiotic ingredients to prevent headache, inflammation, burns, ulcers, fever and nail splitting. It is also used as a medicine. Henna as a hair dye has been handed down to Europe and has been widely used for hair dyeing and treatment since 1890.

Marcha (Portulaca oleracea) has long said that purslane is long-lived because it is called Jangmyeongchae, and the hair does not become white even when old. Commonly known pharmacological actions of Machi Prefecture include anti-aging, anti-dandruff, antioxidant, anti-inflammatory, anti-irritant, collagen production, and moisturizing.

Meanwhile, Tabebuia averanedae (Tabebuia-Avellanedae) is a plant native to South America that has a patent for "cosmetic composition containing the Tahibo extract and has anti-inflammatory and skin irritation efficacy", but has been disclosed to prevent hair loss The research is insufficient.

Orotic acid is a component that has a vitamin B ₁₃ effect. It is a precursor directly to the biosynthesis of the pyrimidine base, a nucleic acid component, and also a precursor of pyridine nucleotides with coenzymes in phosphatase, lipids, and carbohydrate metabolism. The chemical structure is uracil 4-carboxylic acid, white crystalline powder, and has a UV spectrum similar to that of the nucleic acid pyrimidine at melting point of 347 ° C. It is found primarily in milk and is Lactobacillus Lact . Essential for bulgaricus . However, it is not essential for most organisms and is synthesized in vivo. There is no report or patent on hair loss prevention effect.

Patent Publication No. 10-2009-0025497

The present inventors have found that henna extract, March extract, Tabebuia averlanedae extract, 4-pyrrolidine 2, 6-diaminopyrimidine 1-oxide, zinc pyrithione and orotic acid, in particular The composition comprising lotic acid was found to be effective in preventing hair loss and promoting hair growth, and the composition containing the extract was applied to mice having a hair cycle to confirm the function of promoting the transition from the resting phase to the growing hair cycle. The invention was completed.

Accordingly, the present invention is to provide a topical composition for inhibiting general male and female hair loss and promoting hair growth.

The present invention is an active ingredient of henna extract, portuguese extract, Tabebuia averanedae (Tabebuia-Avellanedae) extract, 4-pyrrolidine 2, 6-diaminopyrimidine 1-oxide, zinc pyrithione, and orotic acid It relates to an external preparation composition for preventing hair loss or for promoting hair growth.

The composition according to the present invention can suppress normal male- or female-type hair loss and promote hair growth.

1 is a graph showing the hair loss prevention effect of the composition according to the present invention.
Figure 2 is a graph showing the hair growth promoting effect of the composition of the present invention.
Figure 3 is a photograph showing the hair growth promoting effect of the composition of the present invention.

The present invention relates to a topical composition for promoting hair growth, and more specifically, henna extract, machi extract, Tabebuia averanedae (Tabebuia-Avellanedae) extract, 4-pyrrolidine 2, 6-diaminopyrimidine 1- The present invention relates to an external preparation composition which promotes hair growth by containing an oxide (4-pyrrolidine 2, 6-diaminopyrimidine 1-oxide), zinc pyrithione (Zinc Pyrithione), and orotic acid as an active ingredient.

In the henna extract used in the present invention, henna is a plant known as Lawsonia inermis, which grows to a height of 1 to 5 m. The leaf of the plant has a natural dyeing property called tannic acid, and the leaf is dried finely in the sun and used as a powder. The henna extract may be an organic solvent extract fraction of nonpolar or lower polarity than ethyl acetate.

The henna extract may include 0.1 to 10 parts by weight, 0.3 to 0.5 parts by weight, 0.5 parts by weight based on 100 parts by weight of the total composition.

Portulaca oleracea in the Portica extract used in the present invention is called purslane in Korean. Stems and leaves are fleshy, the leaves are long oval, and the stems are red. It is an annual plant, whose stems grow from the base to grow the ground, and the flowers bloom yellow from June to autumn, and the fruits ripen black after flowering. Purslane is also called the pentagram because it has all five colors, namely, the five auras of yin and yang.

The extract may be 0.1 to 10 parts by weight, 0.3 to 0.5 parts by weight, 0.5 parts by weight based on 100 parts by weight of the total composition.

Tabbevia-Avellanedae used in the present invention belongs to a botanical group of botanicals, botanicals of about 100 species of Jacaranda are native to South America, but among them, Tabebuia-Avellanedae in particular It is native to some parts of Brazil in South America, grows red and purple flowers, and is a source of tea, Tahibo. The Tavebuia averaneda extract may be an organic solvent extract fraction of a nonpolar or lower polarity than ethyl acetate.

The Tavebuia averaneda extract may be a secondary extraction fraction obtained by extracting a primary extraction fraction extracted with a primary extraction solvent as a secondary extraction solvent, and the primary extraction solvent may be water; Lower alcohols such as methanol, ethanol, isopropyl alcohol and n-butanol; Polyhydric alcohols of glycerol, ethylene glycol, propylene glycol, 1,3-butylene glycol; And methyl acetate, ethyl acetate, benzene, n-hexane, diethyl ether, dichloromethane, chloroform, or a mixture thereof or a mixture thereof. The secondary extracting solvent is petroleum ether, methyl acetate, benzene. , Hexane, chloroform, methylene chloride, dimethyl ether and ethyl acetate may be used alone or a mixture thereof.

The Tabebuia averanedae (Tabebuia-Avellanedae) extract may include 0.1 to 10 parts by weight, 0.3 to 0.5 parts by weight, 0.5 parts by weight based on 100 parts by weight of the total composition.

4-pyrrolidine 2, 6-diaminopyrimidine 1-oxide used in the present invention has a calcium channel opening effect and is represented by the following Chemical Formula 1.

[Formula 1]

The 4-pyrrolidine 2, 6-diaminopyrimidine 1-oxide (4-pyrrolidine 2, 6-diaminopyrimidine 1-oxide) is 0.1 to 10 parts by weight, 0.3 to 0.5 parts by weight, based on 100 parts by weight of the total composition, 0.5 parts by weight may be included.

Zinc pyrithione used in the present invention is a kind of antibacterial agent known to inhibit the growth of dandruff and anti-inflammatory action, and is represented by the following formula (2).

(2)

The zinc pyrithione may include 0.1 to 10 parts by weight, 0.3 to 0.5 parts by weight, and 0.5 parts by weight based on 100 parts by weight of the total composition.

Salicylic acid used in the present invention is represented by the following formula (3). Salicylic acid is a substance used in various skin diseases and has an anti-inflammatory effect and is used for the treatment of acne, dandruff, vitiligo, warts and corn.

(3)

The salicylic acid may include 0.1 to 10 parts by weight, 0.3 to 0.5 parts by weight, 0.5 parts by weight based on 100 parts by weight of the total composition.

Orotic acid used in the present invention is represented by the following formula (4). Orotic acid is an acid that is considered as an intermediate in the biosynthesis of pyrimidine bases, which are components of nucleic acids present in organisms, and is a precursor of pyrimidine nucleotides necessary for the biosynthesis of nucleic acids. To get involved. Indications are acute hepatitis, chronic hepatitis, fatty liver, cirrhosis, jaundice, and is also used for adjuvant treatment of general liver dysfunction and various anemias.

[Chemical Formula 4]

The orotic acid may be included in an amount of 0.1 to 10 parts by weight, 0.3 to 0.5 parts by weight, and 0.5 parts by weight based on 100 parts by weight of the total composition.

Hair or scalp cosmetic composition according to the present invention can be used alone or in combination of two or more of the active ingredients, all of the active ingredients, in particular, when used in combination containing orotic acid to prevent hair loss and hair growth promoting effect Improved.

According to the present invention, the external composition for preventing hair loss or promoting hair growth may be used as an active ingredient, henna extract, portulaca oleracea extract, Tabebuia averlanedae extract, zinc pyrithione solution, 4-pyrrolidine 2, 6- Diaminopyrimidine 1-oxide and orotic acid.

That is, the present invention includes, but is not limited to, the extract of Tabebuia-Avellanedae, or the extract of Tabebuia-Avellanedae and 4-pyrrolidine 2, 6-diaminopyri. Contains midine 1-oxide, Tabebuia-Avellanedae extract and zinc pyrithione solution, or Tabebuia-Avellanedae extract, 4-pyrrolidine 2, 6-dia Minopyrimidine 1-oxide and zinc pyrithione solution.

It also contains henna extract, henna extract and 4-pyrrolidine 2, 6-diaminopyrimidine 1-oxide, henna extract and zinc pyrithione solution, henna extract, 4-pyrrolidine 2, 6-diaminopyrimidine 1-oxide and zinc pyrithione solution.

In addition, it contains the gusset extract, or if the gusset extract and 4-pyrrolidine 2, 6-diaminopyrimidine 1-oxide, or contains the gusset extract and zinc pyrithione solution, or henna extract, 4-pyrrolidine 2, 6-diaminopyrimidine 1-oxide and zinc pyrithione solution.

It may also contain 4-pyrrolidine 2, 6-diaminopyrimidine 1-oxide, or 4-pyrrolidine 2, 6-diaminopyrimidine 1-oxide and zinc pyrithione solution.

In addition, it contains orotic acid or contains orotic acid and extract of machi, or contains orotic acid and 4-pyrrolidine 2, 6-diaminopyrimidine 1-oxide, or orotic acid and zinc pyrithione solution Or may contain orotic acid, henna extract, machi extract, Tabebuia avellanedae extract, 4-pyrrolidine 2, 6-diaminopyrimidine 1-oxide and zinc pyrithione solution. Can be.

According to one embodiment of the present invention, the composition according to the present invention may further contain a surfactant, a cationic polymer and a conditioning component commonly used in the art.

The surfactant used in the present invention is polyoxyethylene sorbitan fatty acid ester, sorbitan fatty acid ester, polyoxyethylene fatty acid ester, propylene glycol fatty acid ester, polyoxyethylene polyoxypropylene block copolymer, glyceride, polyoxyethylene glycolation Castor oil, polyoxyethylene glycolated (hydrogenated) castor oil, polyalkylene polyol transesterification products, hydroxyethylalkylamine, polyoxyethylene alkylamine, polyoxyethylene alkylamine fatty acid esters, glycero fatty acid esters, polyoxy Ethylene fatty alcohol esters, polyoxyethylene alkylphenyl ethers, alkylsulfonates, alkylbenzenesulfonates, alkylsulfates, alkylphosphates, tetraalkylammonium salts, trialkylbenzylammonium salts and alkylbetaines selected from the group consisting of It may be a compound. Preferably it may be alone or a mixture thereof selected from the group consisting of polyoxyethylene sorbitan fatty acid esters, sorbitan fatty acid esters and polyoxyethylene glycolated (hydrogenated) castor oil. The surfactant may be included in 3 to 40 parts by weight based on 100 parts by weight of the total composition.

Examples of the cationic polymer used in the present invention include polymeric quaternary ammonium salts of hydroxyethyl cellulose, guar hydroxypropyltriammonium chloride, and the like, but are not limited thereto.

The content of the cationic polymer may be 0.1 to 2.0 parts by weight, 0.1 to 0.5 parts by weight based on 100 parts by weight of the total composition. When the content of the cationic polymer is less than 0.1 parts by weight, the above effect cannot be expected, and when it exceeds 2.0 parts by weight, it is difficult to control the viscosity and excessively adheres to the hair, thereby significantly reducing the feeling of use.

Conditioning components used in the present invention include cyclomethicone, dimethicone (dimethyl polysiloxane), dimethicone copolyol, alkyldimethicone copolyol, silicone ester, fluorodimethicone, alkyldimethicone, dimethicone copolyolamine, carboxy Silicone, including silicone phosphate ester, silicone resin, silicone phospholipid, amodimethicone, aminopropyldimethicone and silicone quartz, but is not limited thereto. The content of the conditioning component may be 0.01 to 10.0 parts by weight, 1.5 to 2.0 parts by weight based on 100 parts by weight of the total composition. If the content of the conditioning component is less than 0.01 parts by weight, it is difficult to expect a conditioning effect, and if it exceeds 10.0 parts by weight, quality degradation due to destabilization of the formulation may be feared.

In addition, according to an embodiment of the present invention, the composition according to the present invention may further contain a suitable amount of pigments, preservatives, metal ion sequestrants and fragrances commonly used in the art within the range of maintaining stability.

The composition according to an embodiment of the present invention may be a hair cleanser composition, a hair shampoo, hair conditioner, hair conditioner, hair treatment, hair tonic, scalp treatment, hair lotion, hair cream, hair nourishing cosmetic or general ointment It can be formulated as.

BEST MODE FOR CARRYING OUT THE INVENTION Hereinafter, the present invention will be described in detail with reference to the following examples. However, the following examples are intended to illustrate the contents of the present invention, but the scope of the present invention is not limited to the following examples. Embodiments of the present invention are provided to more fully describe the present invention to those skilled in the art.

< Example >

Test Example  1: hair loss prevention effect test

Thirty subjects with initial hair loss were tested for hair loss prevention for 16 weeks. After using the compositions of Examples 1 to 6 and Comparative Examples 1 and 2 of Table 1 once a day for 16 weeks, 16 weeks after the hair was collected again when the hair was collected and the number was counted, the results It is shown in Table 2 and FIG.

ingredient Comparative Example 1 (% by weight) Comparative Example 2 (wt%) Example 1
(weight%) Example 2
(weight%) Example 3
(weight%) Example 4
(weight%) Example 5
(weight%) Example 6 (% by weight) 4-pyrrolidine 2, 6-diaminopyrimidine 1-oxide - 0.5 0.5 0.5 0.5 0.5
0.5 0.5 Zinc platinum-rich solution - - 0.5 0.5 0.5 0.5 05 0.5 Aberaneda (Tabebuia- Avellanedae) Extract - - - 0.3 0.3 0.3 0.5 Marchia extract - - - - 0.5 0.5 0.5 0.5 Henna extract - - - - - 0.5 0.5 Orotic acid 0.5 Wax 4.0 4.0 4.0 4.0 4.0 4.0 4.0 4.0 Polysorbate 60 1.0 1.0 1.0 1.0 1.0 1.0 1.0 1.0 Sorbitan sesquioleate 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 Liquid paraffin 5.0 5.0 5.0 5.0 5.0 5.0 5.0 5.0 glycerin 5.0 5.0 5.0 5.0 5.0 5.0 5.0 5.0 Caprylic 3.0 3.0 3.0 3.0 3.0 3.0 3.0 3.0 Butylene glycol 3.0 3.0 3.0 3.0 3.0 3.0 3.0 3.0 Propylene glycol 3.0 3.0 3.0 3.0 3.0 3.0 3.0 3.0 antiseptic Proper amount Proper amount Proper amount Proper amount Proper amount Proper amount Proper amount Proper amount Spices and Colors Proper amount Proper amount Proper amount Proper amount Proper amount Proper amount Proper amount Proper amount Purified water Balance (to 100) Balance (to 100) Balance (to 100) Balance (to 100) Balance (to 100) Balance (to 100) Balance (to 100) Balance (to 100)

Chiri-gun Number of Dropout Hats (Number) / Standard Deviation Comparative Example 1 90.20 + 12.20 Comparative Example 2 70.21 + 8.23 Example 1 62.24 + 9.21 Example 2 61.31 + 8.23 Example 3 58.21 + 7.24 Example 4 54.34 + 5.21 Example 5 59.21 + 7.32 Example 6 34.21 + 5.29

As can be seen from the results of Table 2 and Figure 1, when treated with the composition of Examples 1 to 6 according to the present invention, in particular the henna extract, Machiko extract, Tavevia averaneda (an active ingredient of the present invention) For Example 6, which includes Tabebuia-Avellanedae extract, 4-pyrrolidine 2, 6-diaminopyrimidine 1-oxide, zinc pyrithione and orotic acid, It was found to decrease significantly. In addition, in the case of the composition containing the orotic acid of the present invention (Example 6), it was found that the efficacy is remarkably superior to the composition (Example 4) containing no orotic acid. In conclusion, it can be seen that the composition containing oroic acid is excellent in preventing hair loss.

Test Example  2: hair growth effect test

In order to test the hair growth effect, the back hair of the 7-week-old mouse (C57BL / 6) was removed, and the back skin was selected to be clean and 10 animals were selected for each material group. The compositions of 1 and 2 were applied for 150 days at 150 μl per individual mouse group and washed. After 28 days, the weight of the newly grown hair was measured and compared, and the results are shown in Table 3 and FIG. 2.

Chiri-gun Hair weight average (mg) / standard deviation Comparative Example 1 10.21 + 5.20 Comparative Example 2 41.31 + 6.53 Example 1 58.24 + 6.40 Example 2 59.21 + 7.33 Example 3 62.31 + 8.55 Example 4 67.52 + 9.24 Example 5 60.21 + 5.69 Example 6 90.06 + 3.01

As can be seen from the results of Table 3 and Figure 2, the composition of Examples 1 to 6 according to the present invention acts on the mouse of the resting hair cycle to promote the transition to the growth phase hair cycle composition of Comparative Examples 1 and 2 It can be seen that there is a more excellent hair growth promoting effect. In addition, it can be seen that the composition containing Example 5 (or 6) is 1.5 times higher than the average value of the hair weight of 90.06 + 3.01 than the composition (O Example 4) containing no oroic acid. It was found that the acid hair growth promoting effect is excellent.

As a result of Test Examples 1 and 2, it was found that the composition containing orotic acid was superior to the hair loss preventing ability and the hair growth ability, and that each active ingredient was 0.3 to 0.5 parts by weight based on 100 parts by weight of the total composition. When included it was found that the efficacy is excellent.

Claims (10)

Henna extract, Machi extract, Tabebuia averlanedae extract, 4-pyrrolidine 2, 6-diaminopyrimidine 1-oxide, zinc pyrithione and orotic acid External preparation composition for preventing hair loss or promoting hair growth. The external composition for preventing hair loss or promoting hair growth according to claim 1, wherein the henna extract is included in an amount of 0.1 to 10 parts by weight based on 100 parts by weight of the total composition. The external composition for preventing hair loss or promoting hair growth according to claim 1, wherein the extract of Machi Prefecture is contained in an amount of 0.1 to 10 parts by weight based on 100 parts by weight of the total composition. According to claim 1, The Tabebuia averaneda (Tabebuia-Avellanedae) extract is an external preparation composition for preventing hair loss or promoting hair growth, characterized in that it comprises 0.1 to 10 parts by weight based on 100 parts by weight of the total composition. The external preparation for preventing hair loss or promoting hair growth according to claim 1, wherein the 4-pyrrolidine 2 and 6-diaminopyrimidine 1-oxides are included in an amount of 0.1 to 10 parts by weight based on 100 parts by weight of the total composition. Composition. According to claim 1, wherein the zinc pyrithione is an external composition for preventing hair loss or promoting hair growth, characterized in that it comprises 0.1 to 10 parts by weight based on 100 parts by weight of the total composition. The composition for preventing hair loss or promoting hair growth according to claim 1, wherein the orotic acid is included in an amount of 0.1 to 10 parts by weight based on 100 parts by weight of the total composition. According to claim 1, wherein the composition is selected from the group consisting of hair shampoo, hair rinse, hair conditioner, hair treatment, hair tonic, scalp treatment, hair lotion, hair cream, hair nourishing cosmetic or general ointment External preparation composition for preventing hair loss or promoting hair growth. The composition of claim 1, wherein the composition comprises a surfactant, a cationic polymer and a cyclomethicone, a dimethicone (dimethyl polysiloxane), a dimethicone copolyol, an alkyldimethicone copolyol, a silicone ester, a fluorodimethicone, an alkyldimethicone. Adding a conditioning component selected from silicones including chicone, dimethicone copolyolamine, carboxysilicon, silicone phosphate esters, silicone resins, silicone phospholipids, amodimethicone, aminopropyldimethicone and silicone quartz An external preparation composition for preventing hair loss or promoting hair growth, characterized in that it contains. The method of claim 9, wherein the surfactant is 3 to 40 parts by weight based on 100 parts by weight of the total composition, the cationic polymer is 0.1 to 2.0 parts by weight based on 100 parts by weight of the total composition, the conditioning component is 100 parts by weight of the total composition External preparation composition for preventing hair loss or promoting hair growth, characterized in that 0.01 to 10.0 parts by weight relative to.

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