JP2001288046A - Composition for scalp and hair - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a composition for scalp and hair, excellent in promoting effect on blood flow, hair-growing effects, and preventing effect on depilation, also excellent in preventing effects on scurf and itching, and having high safety. SOLUTION: This composition of the scalp and the hair contains a local irritant and adenosines. The local irritant is exemplified by capsicum tincture, cantharid is tincture and camphor, and 0.001-2.0 wt.% thereof is formulated therewith based on the whole amount of the composition. The adenosines are adenosine, adenosine 5'-phosphate or a salt thereof, and 0.0001-10.0 wt.% thereof is formulated therewith based on the whole amount of the composition.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a composition for external use, particularly to a composition for scalp and hair used on the scalp and hair.

[0002]

2. Description of the Related Art There are various types of compositions for scalp and hair, and products corresponding to various scalp and hair conditions are hair compositions,
It has been developed as a hair restorer and the like. For example, products have been developed that prevent hair loss by preventing dandruff and Kayumi on the scalp.

[0003] Various troubles on the scalp are increasing with the increase in social stress in the aging society, and the demand for scalp hair compositions corresponding to troubles on the scalp is rapidly increasing.

In general, baldness and alopecia of the head, thinning of hair, dandruff and kayumi of the scalp are caused by activation of androgens in organs such as sebaceous glands of hair root, excessive sebum secretion, and production of lipid peroxide. And a decrease in blood flow to the hair follicle and stress. In addition, when sufficient hair follicles cannot be supplied with nutrients for growing durable and beautiful hair, fine hair and thin hair may be caused. Also, a decrease in blood flow to the hair follicle results in nutritional deficiency and a reduced function of excreting waste products. From this point of view, improving the stratum corneum turnover and excessive sebum secretion in the scalp is indispensable in at least improving the blood flow function in the scalp and solving problems of the scalp and hair. It is a point that can not be done.

[0005] Conventional scalp hair compositions generally contain a substance having an action of removing or reducing the factors considered to be the cause of baldness and hair loss. For example,
Vitamins such as vitamin B and vitamin E; amino acids such as serine and methionine; assembly extracts; vasodilators such as acetylcholine derivatives; anti-inflammatory agents such as purple root extract;
Hormonal preparations for women such as estradiol, skin function enhancers such as cepharanthin, etc. are blended and used for prevention and treatment of baldness, hair loss and hair thinning.

[0006]

However, it is difficult to obtain a sufficient effect even if only a small amount of these components is incorporated in the composition for scalp hair. Since the tendency to accompany irritation and redness is increased, the amount of the compound is limited, and the desired effect cannot always be sufficiently obtained.

[0007]

Means for Solving the Problems The present inventors have conducted intensive studies in view of the above viewpoints. As a result, when a local stimulant and adenosine are combined and combined, the adenosine has a blood flow promoting effect and nourishment. The composition for scalp hair, which has an improved hair effect, has an excellent blood flow promoting effect and a hair nourishing effect, also has an excellent hair loss preventing effect and an anti-dandruff / kayumi effect, and is also excellent in safety and stability. The inventors have found that the present invention can be obtained, and have completed the present invention.

That is, the present invention is a composition for scalp hair containing a topical stimulant and adenosine (hereinafter, also referred to as the present composition for scalp hair). In the present invention, the “scalp hair composition” is an external composition used for the scalp or the hair, and its dosage form and form are directly restricted from the use “the scalp hair”. It does not matter whether the category of the composition for external use, such as cosmetics, quasi-drugs, and pharmaceuticals, falls under the Pharmaceutical Affairs Law.

[0009]

Embodiments of the present invention will be described below. Adenosines that can be included in the present scalp hair composition are adenosine, adenosine 5'-phosphate and / or salts of adenosine 5'-phosphate.

Adenosine is one of the ribonucleosides and contains adenine which is a purine derivative in the base portion. Adenosine 5'-phosphate is also called 5'-adenylic acid, and is a nucleotide in which one molecule of phosphate binds to the 5'-hydroxyl group of ribose of adenosine.

In the salt of adenosine 5'-phosphate, the counter ion that forms the salt may be any substance as long as it forms a counter ion with an acid, such as sodium, potassium and calcium. be able to. As the salt of adenosine 5'-phosphate, its hydrate can also be used.

[0012] In the present composition for scalp hair, adenosine, adenosine 5'-phosphate and / or adenosine 5 'are used.
-As the salt of phosphoric acid, a commercially available reagent can also be used.

The amount of adenosine in the present scalp hair composition is usually 0.0001 to 10.0% by mass, preferably 0.1% by mass, as a dry solid based on the total amount of the scalp hair composition. 05 to 5.0% by mass. If the dry solid content is less than 0.0001% by mass based on the total amount of the composition for scalp hair, the desired blood flow promoting effect, hair nourishing effect, hair loss preventing effect, etc. cannot be obtained, and 10.0% by mass of the same. Above this, formulation problems tend to occur.

On the other hand, the topical stimulant to be contained in the present composition for scalp hair is capable of stimulating that part of the human body by applying it on the skin, and is used as a component of the composition for external use. As long as there are no safety issues,
It is not particularly limited, and its mechanism of action should not be questioned.

Specifically, those conventionally blended as a local stimulant in hair cosmetics, such as pepper tincture, tincture tincture, camphor, vanillyl nonanoate, ginger tincture, and benzyl nicotinate, are appropriately selected. Can be incorporated into the scalp hair composition.

[0016] Pepper tincture is a tincture obtained by extracting pepper or a variety thereof fruit with ethanol, and is known to have a skin stimulating action, a hair root stimulating action, a scalp stimulating action and the like. Pepper tincture is commercially available (for example, Alps Pharmaceutical Industries, Koei Kogyo, Koshiro Pharmaceutical, etc.), and in the composition for hair of the scalp, tincture obtained by extracting fruits such as peppers with ethanol is also commercially available. Pepper tincture can also be added.

[0017] Cantaris tincture is a tincture obtained by extracting dried bean halibut with ethanol. Cantaris tincture is also known to have a skin stimulating action, a hair root stimulating action, a scalp stimulating action, and the like, and is already commercially available (eg, Ogi Pharmaceutical, Shiseido Pharmaceutical, etc.).
The scalp hair composition may include tincture obtained by extracting dried bean halibut with ethanol and commercially available tincture tincture.

[0018] Camphor is one of the bicyclic monoterpene ketones, and is known to have a local stimulating action, a central stimulating action, an antiseptic action and the like. The camphor includes d-camphor, 1-camphor and dl-camphor.
Camphor and dl-camphor are commonly used. d
-Camphor is obtained by steam distillation of pieces contained in camphor and the like, and dl-camphor is obtained by a known method, for example, synthesis from pinene. These camphors are already commercially available (for example, Nippon Seika Co., Ltd., Ogi Pharmaceutical, Nippon Terpen Chemical Co., Ltd.). The synthesized dl-camphor is also commercially available d-camphor and d-camphor.
l-Camphor can also be included.

Nonanilic acid vanillylamide is a compound also called nonylic acid vanillylamide, and its properties are white to white.
A whitish crystalline powder with a slight peculiar odor. It has a skin stimulating action and a peripheral vasodilating action, and is known to be used as an external preparation for muscle pain, neuritis, sciatica and the like. Although the method for producing vanillyl nonanoate is not known, it is commercially available (for example, Nagaoka Jitsugyo) and the composition for scalp hair contains commercially available vanillyl amide.

Ginger tincture is an extract obtained by extracting the ginger rhizome with an ethanol solution and is commercially available (eg, Koshiro Pharmaceutical, Maruzen Pharmaceutical, etc.). The composition for hair of the scalp may contain an extract obtained by extracting the ginger rhizome with ethanol and a commercially available ginger tincture.

Benzyl nicotinate is a compound known to have a blood flow promoting action and a cell activating action.
It can be produced by a known method, and is commercially available (for example, Merck Japan). The scalp hair composition also includes benzyl nicotinate produced by a known method.
Commercially available benzyl nicotinate can also be included.

The composition for scalp hair can be formulated with these topical stimulants alone or in combination of two or more. The amount of the topical stimulant used in the present invention is preferably 0.0
0.01 to 2.0% by mass. If the amount is less than 0.001% by mass with respect to the total amount of the scalp hair composition, the desired blood flow promoting effect, hair nourishing effect, hair loss preventing effect, etc. cannot be obtained, and 2.0% or less.
If the amount is more than 10% by mass, it may be difficult to formulate the composition or give an unpleasant irritating feeling to the scalp.

As described above, the present scalp hair composition containing a local stimulant and adenosine has an excellent blood flow promoting effect, a hair nourishing effect, and a hair loss preventing effect. It is a scalp hair composition that can be sufficiently prevented.

The scalp hair composition may contain, in addition to the above essential components, other components usually used in the external composition, for example, oil, as long as the effects of the present invention are not impaired.
Surfactants, thickeners, ultraviolet absorbers, antioxidants, preservatives, fragrances, dyes, solvents such as water, alcohols, etc. can be appropriately compounded as necessary.

The present composition for scalp hair can be produced by a conventional method according to the desired dosage form. The dosage form of the present composition for scalp hair is arbitrary, and may be any liquid form, emulsion, ointment, cream, gel, aerosol, or any other externally applicable dosage form. Further, the product form is also arbitrary, and for example, can be used in the form of tonic, scalp treatment, shampoo, rinse and the like.

[0026]

EXAMPLES Next, the present invention will be described more specifically with reference to examples, but the technical scope of the present invention is not limited to only these examples. In addition, in the following Examples, the compounding amount is mass% with respect to a compounding object, and adenosine is shown as a solid content.

[Examples 1 to 6, Comparative Examples 1 to 5, Control Example 1] Lotions for scalp hair were prepared according to the following production method using the formulations shown in Tables 1 and 2, and the following tests were carried out. The effects of these scalp and hair lotions on blood flow promotion, hair restoration, hair loss prevention and dandruff / kayumi were examined.

[0028]

[Table 1]

[0029]

[Table 2]

(1) Production method Adenosine, a local stimulant, dipropylene glycol, polyoxyethylene (40 mol) hydrogenated castor oil and a fragrance were dissolved in 95% ethanol (ethanol part).
Next, succinic acid and a dye were dissolved in purified water, added to the ethanol part, and stirred to obtain a transparent liquid lotion.

(2) Test for effect of promoting blood flow Samples (lotions) of Examples, Comparative Examples and Control Examples were
In each case, 10 μL was applied to the upper arm of a human, and the blood flow over time was measured with a laser Doppler meter (OMEGA-FLOW FLO-N1) until one hour after application. The test results are shown in Table 1 according to the following criteria.

<Judgment Criteria> ++: The blood flow at the sample application site significantly increased compared to the sample application site of control example 1 (very effective). +: An increase in blood flow at the sample application site relative to the sample application site of Control Example 1 was observed (effective). ±: The blood flow rate at the sample application site was slightly increased (slightly effective) compared to the sample application site of Control Example 1. -: The blood flow at the sample application site did not increase or decreased (ineffective) relative to the sample application site of Control Example 1.

(3) Test for Hair Growth Effect A tricogram test was conducted to examine the hair growth effect of the present composition for scalp hair. The test subjects were male, and each of the comparative example and the example was 10 persons in each group. The sample application period was 4 months, and the sample was applied to the scalp twice a day twice a day. Immediately before the start of the test and 4 months after the start of the test, 50 hairs were randomly removed from the crown of each subject, and the roots of the removed hairs were observed under a microscope. (%) Was calculated. With respect to the hair root telogen rate immediately before the start of the test, the degree of decrease in the hair root telogen rate four months after the start of the test was calculated, and judged based on the following criteria.

<Judgment Criteria> Remarkable effect: The hair root telogen rate four months after the start of the test was reduced by 30% or more with respect to the hair root telogen rate immediately before the start of the test.

Effective: hair root telogen rate 4 months after the start of the test, compared to hair root telogen rate immediately before the start of the test,
It decreased by 20% or more and less than 30%. Weak effect: hair root telogen rate 4 months after the start of the test was 10% or more relative to the hair root telogen rate immediately before the start of the test.
Less than 20%. No effect: The root telogen rate 4 months after the start of the test was reduced by less than 10% with respect to the root telogen rate immediately before the start of the test.

Table 3 shows the ratio (%) of subjects for each of the four stages of the effects, and the effective ratio (the ratio (%) of subjects with a significant effect and the ratio (%) of subjects with an effect). Total).

[0037]

[Table 3]

(4) Hair Removal Prevention Effect Test The change in the number of hair loss due to hair washing before and after use of the sample was measured.
The test subjects were male, and there were 10 subjects in each group of Examples and Comparative Examples. The test period was six months, the first two months were the period of no sample application, and the last four months were the sample application period. During the sample application period, 2 to 4 mL of the sample was applied to the scalp twice a day. During the test period, hair was washed every other day to collect hair loss, and the number of hair loss was counted for one week. From this number, the number of hair loss per hair washing (average value) was calculated, and the average value of the last week in the first half and the average value of the last week in the second half were compared. This result was determined based on the following criteria.

<Evaluation Criteria> ++: The number of hair loss was reduced by 70 or more, and a remarkable hair loss prevention effect was recognized. +: The number of hair loss was reduced by 40 or more, and a considerable hair loss prevention effect was observed. ±: The number of hair loss decreased by 10 or more, and a slight hair loss prevention effect was observed. -: The number of hair loss was less than 10 or the number of hair loss was increased, and no hair loss preventing effect was observed.

Table 4 shows the ratio (%) of subjects for each effect of these four stages, and the effective rate (total of the ratio (%) of ++ subjects and the ratio (%) of + subjects). Show.

[0041]

[Table 4]

(5) Dandruff and Kayumi Prevention Effect Test In particular, a male complaining of dandruff and Kayumi was taken as a test subject, and a dandruff and Kayumi on the scalp after the test were examined with respect to 10 subjects from each group of Comparative Examples and Examples. -Kayumi prevention effect was evaluated. The sample application period was 3 months. During this period, the hair was washed once a day with a shampoo containing no drug, and the sample was washed 2 days a day.
Each time, 2 to 4 mL was applied to the scalp.

Regarding the anti-dandruff effect, at the end of the test,
Before washing the hair from the subject, the head dander was collected by a suction device,
The amount of protein in dandruff (dandruff amount) was measured and evaluated by the average value.

At the end of the test, the scalp Kayumi prevention effect was examined by examining the scalp Kayumi of each tester, the degree of which was determined according to the following criteria, and the average value was evaluated. <Judgment criteria> 3: There is strong Kayumi. 2: There is Kayumi. 1: There is a little Kayumi. 0: There is no Kayumi. The results are shown in Table 5.

[0045]

[Table 5]

From these results, the scalp and hair lotion of the Example, which contains a local stimulant and adenosine,
It has been found to have excellent blood flow promoting effect, hair nourishing effect, hair loss preventing effect and dandruff / kayumi preventing effect.

That is, in the present scalp hair composition, which is prepared by combining a topical stimulant and adenosines,
It has been clarified that these synergistic effects remarkably show a blood flow promoting effect, a hair nourishing effect, a hair loss preventing effect and a dandruff / kayumi preventing effect. This is because a desired effect can be obtained by blending a small amount of the local stimulant and adenosine, and particularly, by causing a large amount of the local stimulant to be blended, in the application portion and its peripheral portion. This indicates that it has become possible to prevent unpleasant stimulus and redness.

Therefore, by using the present composition for scalp hair on the scalp or hair, blood flow can be promoted safely, hair growth can be promoted, and hair loss can be prevented. It became clear that dandruff and Kayumi could be prevented.

The following is an example of the formulation of the composition for scalp hair.
This is shown as an example. In addition, the composition for scalp hair of any of the examples also showed an excellent blood flow promoting effect in the above tests (blood flow promoting effect test, hair restoration effect test, hair loss preventing effect test and dandruff / kayumi preventing effect test), A hair-growing effect, a hair loss-preventing effect, and an anti-dandruff / kayumi effect were observed. These scalp hair compositions were also excellent in safety and stability.

[Example 7] Lotion compounding component compounding amount (% by mass) 95% ethanol 70.0 Adenosine 4.0 Pepper tincture 1.0 Glycerin 0.5 Polyoxyethylene (40 mol) hydrogenated castor oil 0.2 Apple Acid appropriate amount Perfume and pigment Appropriate amount Purified water residue <Production method> Adenosine, pepper tincture, glycerin, polyoxyethylene (40 mol) hydrogenated castor oil, malic acid and flavor are dissolved in 95% ethanol (ethanol part). ). Next, the dye was dissolved in purified water, added to the ethanol part, and dissolved by stirring to obtain a transparent liquid lotion.

Example 8 Lotion Compounding Component Mixing Amount (% by Mass) 95% Ethanol 45.0 Adenosine 5′-Phosphate 1.0 Cantaristinki 1.0 Camphor 0.5 Nonanoic Acid Vanillylamide 0.1 Propylene Glycol 1.0 Polyoxyethylene (60 mol) hydrogenated castor oil 0.3 Succinic acid qs Perfume and dye qs Purified water balance <Production method> 95% ethanol in adenosine 5'-phosphoric acid, cantharis tincture, camphor , Nonanilic acid vanillylamide, propylene glycol, polyoxyethylene (60
Mol) hydrogenated castor oil and perfume were dissolved (ethanol part). Next, the dye was dissolved in purified water, added to the ethanol part, and stirred and dissolved to obtain a transparent liquid lotion.

[Example 9] Emulsion compounding amount (% by mass) (1) Cetanol 1.8 (2) Stearic acid 1.0 (3) Palmitic acid 0.6 (4) Liquid lanolin 1.0 (5) ) Squalane 2.0 (6) glyceryl monostearate 1.6 (7) POE sorbitan monostearate 0.4 (8) adenosine 5'-disodium phosphate 2.0 (9) camphor 0.5 (10) Nonanilic acid vanillylamide 0.05 (11) 1,3-butylene glycol 3.0 (12) Polyethylene glycol 3.0 (13) Triethanolamine 1.0 (14) Residual purified water <Production method> (1)- A mixture was prepared by mixing the components of (10). Separately, a mixture was prepared by mixing the components (11) to (14). After each of these mixtures was separately heated to 70 ° C. and dissolved, the two were mixed and emulsified by an emulsifier, followed by heat exchange cooling to obtain an emulsion.

[0053]

According to the present invention, there is provided a highly safe composition for scalp hair which is excellent in blood flow promoting effect, hair nourishing effect and hair loss preventing effect and also excellent in dandruff and kayumi preventing effect. You.

 ────────────────────────────────────────────────── ─── Continued on the front page (72) Inventor Masahiro Tajima 1050 Nippa-cho, Kohoku-ku, Yokohama-shi, Kanagawa F-term in Shiseido Daiichi Research Center (reference) 4C083 AA071 AA072 AA111 AA112 AC022 AC072 AC102 AC122 AC242 AC292 AC302 AC422 AC432 AC442 AC542 AC642 AC851 AC852 AD042 AD112 AD391 AD392 AD512 AD531 AD601 AD602 CC31 CC32 EE22 EE23 4C086 AA01 AA02 MA05 NA05 ZA36 ZA92

Claims (4)

[Claims] 1. A composition for scalp hair containing a local stimulant and one or more adenosines selected from the group consisting of adenosine, adenosine 5'-phosphate and adenosine 5'-phosphate salts. object. 2. The local stimulant is one or more selected from a group of local stimulants selected from the group consisting of tincture tincture, tincture tincture, camphor, vanillyl nonanoate, tincture tincture and benzyl nicotinate.
The composition for scalp hair according to claim 1. 3. The scalp hair composition according to claim 1, wherein the content of the topical stimulant is 0.001 to 2.0% by mass based on the total amount of the scalp hair composition. 4. The content of adenosines is 0.0001 to 1 as a dry solid based on the total amount of the scalp hair composition.
The composition for scalp hair according to any one of claims 1 to 3, which is 0.0% by mass.