KR101321045B1 - Composition of preventing hair loss and promoting hair growth - Google Patents

Abstract

The present invention relates to a hair loss prevention and hair growth promoting composition, the composition comprising one or more of the compounds of the following formula (1) or (2) as an active ingredient has an excellent effect on promoting hair growth phase induction, accordingly using a conventional additive When prepared in a formulation to be applied to the scalp can be used as a composition for preventing hair loss and promoting hair growth having an excellent effect.

[Formula 1]

Wherein R is a C ₁ ~C ₅ alcohol, aldehyde, acid, or an alkylene group.

(2)

Hair loss prevention, hair growth promotion, 2-methyl-hept-2-ene derivative, linalool oxide

Description

Hair Loss Prevention and Hair Growth Promoting Composition {COMPOSITION OF PREVENTING HAIR LOSS AND PROMOTING HAIR GROWTH}

The present invention relates to a hair loss prevention and hair growth promoting composition, more specifically 2-methyl-hept-2- with excellent effect of shortening the period of transition from the resting phase to the growth phase of the hair growth cycle to grow new hair The present invention relates to a composition containing as an active ingredient at least one kind of a 2-methyl-hept-2-ene derivative and a linalool oxide.

The human hair is about 100,000 to 150,000 pieces, each hair has a different cycle and grow and drop out through the anagen, catagen, telogen. This cycle is repeated over three to six years, with the result that on average 50 to 100 hairs fall out normally. In general, alopecia refers to an increase in the number of abnormal hair loss due to shortening of hair growth rate in the growing period and increased number of hair in the retrogressive or resting period among these cycles.

The causes of hair loss have been discussed, such as excessive secretion of male hormones, seborrheic scalp, stress, obesity, peroxides, deterioration of the scalp function due to bacteria, etc., but no clear cause for hair loss is known. In recent years, a growing number of people are suffering from hair loss due to stress caused by changes in diet, social environment, etc., and the age is also decreasing, and the hair loss population of women is also increasing.

Minoxidil and finastride have been approved by the US FDA to treat or prevent such alopecia. Minoxidil was originally intended for the treatment of hypertension, and pinastride was developed as an agent for the treatment of enlarged prostates. Although the mechanism of minoxidil's hair growth is not known exactly, it is thought to promote hair growth by nourishing hair roots by increasing blood flow caused by vasodilation.

The effects of a commercially available product as a hair growth or hair loss preventing agent on the hair include hair growth phase induction effect, hair growth phase extension effect, 5α-reductase inhibitory effect, blood circulation promoting effect, bactericidal effect, anti-dandruff effect, moisturizing effect, antioxidant effect, etc. There is, however, the effect of preventing hair loss and promoting hair growth in such a conventional formulation is not sufficient. This is because the causes of hair loss are very complicated and variously entangled, while these preparations focus on only one or two types of hair loss or hair growth phenomena to improve them. That is, to date, preparations focusing on various and complicated hair growth mechanisms are rare.

Japanese Patent Application Laid-Open No. 2000-169326 (June 20, 2000) discloses a blood flow promoter containing at least one selected from benzoic acid, alkali metal salts of benzoic acid, benzaldehyde, cuminaldehyde, myrenal, and hydroxy citronellal as an active ingredient. It is starting. These blood stimulators improve the large intestinal sensation of local tissues due to peripheral blood flow and exert an excellent blood flow promoting effect. Therefore, it is compounded in oral compositions, medicines, cosmetics, hair growth agents, bath solvents, external preparations, periodontal disease, soot, hair loss It is described that it can be used to improve shoulder stiffness, muscle pain and the like. However, only the blood flow promoting effects of hydroxy citronellal and the like are shown here, and in fact, the effect on the improvement of hair loss is not specifically demonstrated.

On the other hand, terpene compounds, which are the main components of plant essential oils, are used as raw materials for fragrances and pest repellents. For example, Korean Patent Publication No. 10-2002-0092774 (Dec. 12, 2002) discloses hinokithiol, terpineol, citronellal, and the like as natural preservative and insect repellent components in maleic anhydride adducts of terpene compounds. The antiseptic and insect repellent compositions formed by blending are disclosed. In addition, Korean Patent Publication No. 10-2004-7001866 (February 6, 2004) discloses a psychomodifying perfume composition comprising terpineol, linarol, citronellol, and the like. 2004-7009485 (June 17, 2004) discloses a method of using terpineol, citronellol and the like as a pesticide. That is, these ingredients have been mainly used in insecticides, pest repellents, fragrances, etc. in addition to the raw material of the perfume, and the technology related to hair growth is not known.

The inventors have found that a particular terpene-based compound has a growth-induction promoting action of hair, among other mechanisms related to hair growth, and thus aims to provide a composition having a very good hair loss prevention and hair growth promoting effect without side effects. It is done.

Hair loss prevention and hair growth promoting composition of the present invention for achieving the above object is characterized in that it comprises one or more of the compounds of the formula (1) or (2) as an active ingredient.

Wherein R is a C ₁ to C ₅ alcohol, aldehyde, acid, or alkylene

Here, it is preferable that the content of these active ingredients is 0.01 to 10 weight%.

The compound of Formula 1 is a compound in which C ₁ to C ₅ alcohol, aldehyde, acid, or alkylene is added to carbon 6 of 2-methyl-hept-2-ene. Beta-citronellol (β-citronellol, 3,7-dimethyloct-6-en-1-ol), citronellal (3,7-dimethyloct-6-en-1-al), citro Citronellene ((S)-(+)-3,7-dimethyl-1,6-octadiene) and citronellic acid (citronellic acid, 3,7-dimethyl-6-octenoic acid), including but not limited to It doesn't work. The compound of formula 2 is linalool oxide (linalool oxide, cis-2- (tetrahydro-5-methyl-5-vinylfuran-2-yl) -propan-2-ol).

Hereinafter, the compound group of Formula 1 and Formula 2 will be described in detail. However, these compounds are only illustrative for demonstrating this invention, The scope of the present invention is not limited only to these.

Beta-citronellol (β-citronellol, 3,7-dimethyloct-6-en-1-ol) is a CAS No. 106-22-9 and the structural formula is:

Citronellal (3,7-dimethyloct-6-en-1-al) is a CAS No. 106-23-0 and the structural formula is:

Citronellene ((S)-(+)-3,7-Dimethyl-1,6-octadiene) is a CAS No. 2436-90-0 and the structural formula is:

Citronellic acid (3,7-Dimethyl-6-octenoic acid) is CAS No. 502-47-6 and the structural formula is:

Linalool oxide (cis-2- (Tetrahydro-5-methyl-5-vinylfuran-2-yl) -propan-2-ol) is CAS No. 5989-33-3 and the structural formula is:

(2)

These active ingredients are preferably contained in 0.01 to 10% by weight of the total weight of the composition for preventing hair loss and promoting hair growth according to the present invention. If it is less than 0.01% by weight, the hair growth phase induction promoting effect is not satisfactory, and at a concentration higher than 10% by weight, its effect does not appear sufficiently compared to the dose, which is not preferable.

The composition of the present invention can be prepared in any formulation that can be applied to the scalp, such as liquid, cream, paste, or solid phase, shampoo, hair conditioner, hair lotion, liquid to promote hair growth by adding a conventional additive And aerosol types of these formulations.

As described above, the terpene-based compounds of Formulas 1 and 2 have an excellent effect on promoting hair growth phase induction, and thus, hair loss prevention and hair having excellent effects when prepared in a formulation applied to the scalp using conventional additives It can be used as a composition for promoting growth.

Hereinafter, the present invention will be described in more detail with reference to Examples. However, these Examples are only illustrative of the present invention, and the scope of the present invention is not limited to these.

In the effect test examples below, the C57BL / 6 mouse model was used as an animal test model for evaluating hair growth induction promoting effect. The C57BL / 6 mouse has black hair and has spontaneous alopecia. In addition, melanocytes (melanocytes) are present only in the hair follicles, and melanin synthesis matches well with the hair growth cycle, which has the advantage of determining the hair growth cycle in terms of skin color. It is widely used for research.

Effect Test Example : Experiment to evaluate hair growth induction promoting action

The terpene-based compounds used as active ingredients in the composition according to the present invention were purchased from Sigma (USA).

Hair growth induction promoting effect experiment was used in the 7-week-old mouse (C57BL / 6, female) which is widely used for the evaluation of hair growth induction action.

First, the hair on the back of the mouse was removed using an electric razor, and each mouse was weighed and divided into six pieces so that the weight was evenly distributed. From the next day with the adaptation period for one day, excipients, control drugs and each test drug prepared according to the prescription of Table 1 below were applied to the hair removal site of the mouse once a day for 4 weeks, with a brush.

ingredient Compounding ratio (% by weight) Addiction Treaty Test drug 1 Test drug 2 Test drug 3 Test drug 4 Test about 5 ethanol 40 40 40 40 40 40 40 Minoxidil - One - - - - - Beta-citronellol - - One - - - - Citronellene - - - One - - - Citronellal - - - - One - - Citronellinic acid - - - - - One - Linalool oxide - - - - - - One Polysorbate 60
(Tween 60) 0.5 0.5 0.5 0.5 0.5 0.5 0.5 Purified water Balance (total 100)

The overall treatment effect was evaluated by comparing the wool and hair growth at 4 weeks after the start of the experiment into four stages of improvement (++), improvement (+), slight improvement (±) and no response (-). It was.

Table 1 and Figure 1 below shows the results of the hair growth phase induction promoting action measured using the mouse as described above.

Test drug Marie ++ + ± - Addiction 0 One 2 3 Treaty One 3 0 2 Test drug 1 5 0 0 One Test drug 2 2 4 0 0 Test drug 3 2 2 0 2 Test drug 4 2 One 3 - Test about 5 3 2 0 One

As shown in Table 2, it was confirmed that in the mice coated with the respective test drugs, the transition from the resting hair cycle to the growing hair cycle was promoted, thereby promoting hair growth. This result can also be confirmed in FIG.

Based on the results of the above effect test, various formulation examples of the composition according to the present invention will be described in detail. However, these formulation examples are only examples of the composition of the present invention, it will be apparent to those skilled in the art that the scope of the composition of the present invention is not limited only to these formulations.

Formulation Example  One: hair tonic

Hair tonic was prepared by a conventional method according to the prescription below.

Compounding ingredient Weight ratio (%) ethanol 55 Castor oil 5 glycerin 3 Pyrotonolamine 0.1 Beta-citronellol One Spices and Colors Suitable amount Purified water Balance (total 100)

Formulation Example  2: hair  Lotion

The hair lotion was prepared by the conventional method according to the prescription below.

Compounding ingredient Weight ratio (%) Cetostearyl alcohol 2 Stearyl Triethyl Ammonium Chloride 2 Hydroxyethyl cellulose 0.5 Pyrrothonol amine 0.1 Citronellene One Spices and Colors Suitable amount Purified water Balance (total 100)

Formulation Example  3: hair nourishing lotion

A hair nourishing lotion was prepared in a conventional manner according to the prescription below.

Compounding ingredient Weight ratio (%) Wax 4.0 Polysorbate 60 1.5 Sorbitan sesquioleate 0.7 Liquid paraffin 5.0 Squalane 5.0 Caprylic / capric triglyceride 5.0 glycerin 3.0 Butylene glycol 3.0 Propylene glycol 3.0 Carboxyvinyl polymer 0.1 Triethanolamine 0.2 Citronellal 0.5 antiseptic Suitable amount Spices and Colors Suitable amount Purified water Balance (total 100)

Formulation Example  4: flexible lotion

A flexible lotion was prepared in a conventional manner according to the prescription below.

Compounding ingredient Weight ratio (%) Citronellinic acid 0.2 Pentadecane Glyceride 0.1 Butylene glycol 2.0 Propylene glycol 2.0 Carboxyvinyl polymer 0.1 PEG-12 nonylphenyl ether 0.2 Polysorbate 80 0.4 ethanol 10.0 Triethanolamine 0.1 antiseptic Suitable amount Pigment Suitable amount Spices Suitable amount Purified water Balance (total 100)

Formulation Example  5: nutrition lotion

A nutritional lotion was prepared in a conventional manner according to the prescription below.

Compounding ingredient Weight ratio (%) Linalool oxide 5.0 Nicotinic acid amide 0.1 Wax 4.0 Polysorbate 60 1.5 Sorbitan sesquioleate 1.5 Liquid paraffin 0.5 Caprylic / capric triglyceride 5.0 glycerin 3.0 Butylene glycol 3.0 Propylene glycol 3.0 Carboxyvinyl polymer 0.1 Triethanolamine 0.2 antiseptic Suitable amount Pigments and spices Suitable amount Purified water Balance (total 100)

As described above, the terpene-based compounds of Formulas 1 and 2 have an excellent effect on promoting hair growth phase induction, and thus, hair loss prevention and hair having excellent effects when prepared in a formulation applied to the scalp using conventional additives It can be used as a composition for promoting growth.

1 is a photograph showing the results of the hair growth stage induction promoting action measured using a mouse.

Claims (8)

Β-citronellol (β-citronellol, 3,7-dimethyloct-6-en-1-ol) of Formula 1, citronellal (citronellal, 3,7-dimethyloct-6-en-1-al), Citronellene ((S)-(+)-3,7-dimethyl-1,6-octadiene), citronellic acid (citronellic acid, 3,7-dimethyl-6-octenoic acid) Hair loss comprising at least one of linalool oxide (cis-2- (tetrahydro-5-methyl-5-vinylfuran-2-yl) -propan-2-ol) compounds as an active ingredient Preventive and hair growth promoting composition. [Formula 1]

Wherein R is a C ₁ ~C ₅ alcohol, aldehyde, acid, or an alkylene group. (2)

The composition of claim 1, wherein the compound is 0.01 to 10% by weight of the total weight of the composition. delete delete delete delete delete delete

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