JP2000229834A - Cosmetic - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a cosmetic excellent in preventing effect from getting older, activating metabolism of hair roots on a scalp and having excellent effect improving growth of the hair roots. SOLUTION: This cosmetic includes (A) a component originated in pine bark including proanthocyanidin of formula I (n is 1-1,000; R is H or OH) as a main component and preferably (B) diisopropylaminedichloroacetate. The component A is a substance extracted from pine bark of French beach pine growing in the Bordeaux area of France and Atlantic coast of Pyrenean mountains and its dosage is preferably 0.01-10 wt.% based on total weight of the objective cosmetic and the dosage of component B is preferably 0.01-10 wt.%.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention has excellent skin aging prevention effects (active oxygen suppression, lipid peroxide suppression, rough skin improvement, keratin improvement, fast turnover effect), and hair root metabolism in the scalp. Has an excellent effect of activating and promoting the growth of hair roots, and has excellent moisturizing properties,
The present invention relates to a novel cosmetic having excellent non-sticky organoleptic properties.

[0002]

2. Description of the Related Art In general, aging skin is skin that is dry and has no smoothness and in which exfoliation of keratinocytes is observed. It is said that the aging skin has a slow turnover speed, and the turnover speed increases when the skin has an anti-aging effect. Many skin cosmetics (for example, JP-A-7-304639, JP-A-9-118611, JP-A-9-176008, etc.) have been proposed from the viewpoint of rough skin, aging, etc., but are still satisfactory. It cannot be done.

[0003] In addition, conventionally, hair restoration cosmetics containing a blood circulation promoting substance and amino acids and vitamins which are nutritional components of hair are known. Further, many medical hair restorers and cosmetics containing a component having an effect of preventing sebaceous gland hypertrophy and a component having an androgenic inhibitory effect have been proposed.

[0004] However, conventionally used blood circulation promoting substances are highly irritating to the skin, and their amounts are limited.
The disadvantage is that the duration of blood circulation promotion is short.

[0005] By the way, male pattern baldness is said to be one of the causes of the excessive action of male hormones. However, phenomena such as poor circulation, decreased activity of hair matrix cells, enlargement of sebaceous glands, fibrosis of the scalp, and the like. It is presumed that it is caused by complicated intertwining.

[0006] However, in order to suppress the decrease in hair matrix activity and the enlargement of sebaceous glands, which are said to be caused by the excessive action of male hormones, the hair growth effect is exhibited even if an anti-androgen agent is simply used as a hair restorer. At present it does not reach. Also, using a hair matrix activator or a blood circulation promoter,
Good results are not obtained.

As means for solving the above-mentioned problems, a number of hair-growing and hair-growing agents (for example, JP-A-5-58850, JP-A-5-139936, JP-A-5-170)
625) has been proposed, but no remarkable hair-growth effect has been found even with the use of a substance that promotes peripheral blood flow and activates hair matrix cells, and the composition should be sufficiently satisfactory. In fact, there is still room for improvement in the hair-growing effect and the hair loss-preventing effect without achieving the effect.

On the other hand, cosmetics contain a moisturizing agent for the purpose of maintaining skin homeostasis and protecting the skin from drying in winter. Conventionally used humectants include glycerin, water-soluble polyhydric alcohols represented by propylene glycol and sorbitol, water-soluble polymers represented by hyaluronic acid and xanthan gum, pyrrolidone carboxylate and amino acids. Examples include natural moisturizing factors and intercellular lipids represented by ceramide.

Conventional cosmetics containing a humectant have a certain effect, but water-soluble polyhydric alcohols and water-soluble polymers are often sticky at the time of application and immediately after application. It is not always satisfactory, and there is a need for a cosmetic that improves this.

[0010]

SUMMARY OF THE INVENTION Accordingly, an object of the present invention is to provide a skin aging prevention effect (active oxygen suppression effect, lipid peroxide suppression effect, rough skin improvement effect, keratin improvement effect, effect of increasing turnover speed). An object of the present invention is to provide a novel cosmetic which has excellent effects of stimulating hair root metabolism on the scalp to promote the growth of hair roots, and having excellent moisturizing properties and excellent non-sticky sensory characteristics.

[0011]

In view of the above circumstances, the present inventor has found that excellent skin aging prevention effects (active oxygen suppression effect, lipid peroxide suppression effect, rough skin improvement effect, keratin improvement effect, turnover speed) The effect of accelerating the growth of hair roots) and the effect of promoting the growth of hair roots, as well as excellent moisturizing properties.
The above-mentioned excellent effect is obtained in a cosmetic containing a pine bark-derived component containing proanthocyanidin as a main component, and preferably a cosmetic containing a pine bark-derived component containing proanthocyanidin as a main component in combination with diisopropylamine dichloroacetate. The present invention has been found to be applicable to a wide range of preparations as well as to the present invention.

That is, the present invention provides a cosmetic comprising a pine bark derived from a pine bark having the following general formula as a main component and a pine bark derived from a pine bark comprising a proanthocyanidin as a main component and diisopropylamine. A cosmetic comprising dichloroacetate.

[0013]

Embedded image

(Wherein, in the formula, n is a number of 1 to 1000, and R is a hydrogen atom or a hydroxyl group.)

[0015]

DESCRIPTION OF THE PREFERRED EMBODIMENTS The details of the structure of the present invention will be described below.

The pine bark derived from pine bark containing proanthocyanidin as the main component used in the present invention includes pine bark having a high proanthocyanidin content of about 20 to 70% or more, such as water or specific pine bark from French coastal pine. The extract may be prepared by extraction using an organic solvent described above, or the extract may be prepared by concentration, molecular sieving, purification by chromatography or the like as far as the cost is acceptable. Specifically, a raw material Pycnogenol (trade name, powder form) manufactured by Hofer Research Laboratory (Switzerland) is particularly preferable. The Pycnogenol is a substance extracted from the bark of a pine bark called PINUS PINSTER, which grows on the Atlantic coast in the Bordeaux region of France and the Pyrenees Mountains. The pycnogenol contains 60% or more of proanthocyanidins as a main component, and further contains 40 or more kinds of organic acids (such as polyphenols).

The component derived from pine bark containing proanthocyanidin as the main component used in the present invention is a proanthocyanidin contained in other grains and fruits (for example, JP-A-06-336421) and JP-A-2006-336421. Unlike procyanidin described in JP-A-02-134309, it is a component in which anti-tyrosinase (mushroom tyrosinase) activity is not recognized.

As an extraction solvent for preparing the pine bark derived from pine bark containing proanthocyanidin as the main component used in the present invention, for example, the bark of a French pine is extracted with water, ethanol, an aqueous ethanol solution, benzene, acetone or the like. And those prepared.

The amount of the pine bark-derived component containing proanthocyanidin as the main component used in the present invention (in terms of the dry solid content of the extract) is 0.01 to 10% by weight based on the total amount of the cosmetic. Is suitable, especially 0.05 ~
5% by weight is preferred. If the amount is less than 0.01% by weight, the manifestation of the effect may not be sufficient, and if the amount is more than 10% by weight, no further effect may be expected.

The diisopropylamine dichloroacetate (abbreviated as DADA) used in the present invention is represented by the following formula, is in the form of a white crystalline powder, has almost no smell, has little bitter taste, Easy to dissolve in ethanol, etc. The melting point is 118-122 ° C, and the pH of a 5% aqueous solution is 5.6-6.8.

[0021]

Embedded image

The compounding amount of diisopropylamine dichloroacetate used in the present invention is suitably 0.01 to 10% by weight, particularly preferably 0.05 to 5% by weight, based on the total amount of the cosmetic. If the amount is less than 0.01% by weight, the effect may not be sufficiently developed.
If the amount is more than 0% by weight, no further effect may be expected.

The form of the cosmetic of the present invention includes lotion,
Creams, emulsions, foundations, packs, bath preparations,
Examples include hair tonic, hair lotion, hair treatment, hair cream, hair conditioner, hair gel, hair mist, hair foam, colon, facial cleanser, body shampoo, shampoo, rinse and bath agent.

In addition to the active ingredients used in the present invention, bases, fragrances, preservatives, preservatives, preservatives, humectants, medicinal substances, surfactants and the like for constituting compositions generally acceptable in cosmetics are included. They can be appropriately blended.

[0025]

The present invention will be described in more detail with reference to the following examples. Unless otherwise specified, the percentages shown below are
Indicates the weight%. Prior to the examples, (1) a method for measuring the turnover speed of the stratum corneum, (2) a test method for measuring the effect of improving rough skin, (3) a test method for measuring the effect of improving stratum corneum, and (4) a test method for measuring the effect of promoting growth of mouse hair. , (5) Human hair growth promotion effect test method, (6) Active oxygen generation suppression test, (7) Lipid peroxide suppression test, (8) Moisturizing test, (9) Sensory (stickiness) test .

(1) Method of measuring the turnover speed of the stratum corneum An ointment containing 5% of a fluorescent dye, dansyl chloride, in white petrolatum was prepared, and was occlusively applied to the skin of the forearm of the subject for 24 hours, and dansyl chloride was applied to the stratum corneum. Was allowed to penetrate. Thereafter, a test sample was applied to the same site twice a day (morning and evening), the fluorescence of dansyl chloride was examined every day, and the number of days until the fluorescence disappeared was defined as the turnover speed of the stratum corneum of the skin.

(2) Measurement Test Method for Improvement Effect of Rough Skin The effect of continuous application for four weeks was examined on 20 middle-aged and elderly subjects having rough skin on the lower leg. About 1 g of the sample was applied to the test site of the left leg of the subject twice a day, and the skin condition before and after the start of the test was determined according to the criteria shown in Table 1. The lower leg on the right side was used as a target without applying the sample.

[0028]

[Table 1]

The results of judgment between the test site and the control site before and after the test are compared, and when the degree of dryness of the skin is improved by two or more stages (for example, + →-, ++ → ±), “effective”, and when the skin is improved by one stage Is "Slightly valid", and the case where there is no change is "Invalid". The test results were indicated by the number of subjects who became “effective” and “slightly effective”.

(3) Measuring test method for the effect of improving keratin (enhancing the exfoliative properties of keratinocytes) Scotch tape (Nichiban Mending tape) is applied to the skin of the test part before and after the above-mentioned measurement test for measuring rough skin improvement.
Was adhered to the tape, and when the tape was peeled off, the state of the keratinous cells attached to the tape was examined in detail by a scanning electron microscope.

[0031]

[Table 2]

The judgment was "effective" when the difference between the evaluation point of the test site and that of the control site after continuous application for 4 weeks was two points higher,
The case of 1 point was "slightly valid", and the case of 0 point was "invalid". The test results were indicated by the number of subjects who became “effective” and “slightly effective”.

(4) Mouse Hair Growth Promoting Effect Test Method The skin at the center of the back of a C3H mouse (male, 8 weeks old, average body weight: 35 g) was cut with an electric clipper, and the hair was completely removed with a shaver. From the next day, each sample of Example and Comparative Example was applied to the skin of the test part once a day, 0.2 ml per animal. A group of 10 animals was used for one sample. On the 14th day after the start of the experiment, the animals were sacrificed and photographs of the skin of the test area were taken. Next, take the picture into the image analysis device,
First, the shaved area (A) and the hair growth area (B) were determined, and mouse hair growth promoting effect = (B) / (A) was calculated for each animal.

(5) Human hair growth promoting effect test method Male test subject 1 in his 30s and 40s with decreased hair growth
The hair at the top of the head was shaved into a circular shape having a diameter of about 7 mm. One and three days after shaving, the method of Hayashi et al. (British Journal of Dermatology, 12
5, p. 123, 1991), the hair growth rate was determined for the hair at the target site (about 30 to 40 hairs), and the average value (A) was calculated. Next, about 3 ml of the sample of the example or the comparative example was applied to each subject twice a day every morning and evening around the test site.
Apply and massage well. The hair growth rate at the same site was measured in the same manner three months after the start of the test, and the average value (B) was calculated. The effect was determined by comparing the ratio (B) / (A) before and after use of each hair nourishing cosmetic.

(6) Active oxygen production suppression test 0.05 M sodium carbonate buffer (pH 10.2) 2.4
ml, 3 mM xanthine 0.1 ml, 3 mM EDTA 0.1 m
1, 0.15% bovine serum albumin 0.1 ml, 0.75
0.1 ml of a sample solution (0.001 to 0.05% aqueous solution of 50% ethanol) is added to a composition of 0.1 ml of mM nitro blue tetrazolium, and heated at 25 ° C. for 10 minutes. 0.1 ml of 150-fold diluted xanthine oxidase derived from buttermilk (manufactured by Sigma) was added thereto, and 25
React at ℃ for 20 minutes. 0.1 ml of 6 mM copper chloride
The reaction is stopped and the absorbance is measured at a wavelength of 560 nm using a spectrophotometer. Instead of the sample solution, 0.1 ml of a 50% ethanol solution was added as a control, and the absorbance was measured. The inhibition rate (%) for this control was determined, and 5
The concentration of 0% inhibition was expressed as IC ₅₀ (%).

(7) Lipid peroxide suppression test Methyl linoleate 0.3 ml, 1 mM hypoxanthine (0.1% Triton X-100), sample solution (0.01 to 0.1)
% Of 50% ethanol aqueous solution), distilled water, and 0.15 ml of 10-fold diluted xanthine oxidase derived from buttermilk (manufactured by Sigma) at 37 ° C. for 24 hours with shaking reaction. 0.5 ml of 10% phosphotungstic acid and 1.0 ml of 0.67% thiobarbituric acid were added to 0.3 ml of the composition, stirred, heated at 95 to 100 ° C. for 30 minutes, and rapidly cooled to remove n-butanol. After adding and shaking, centrifugation (3000 rpm, 10 minutes) was performed, and the absorbance of the supernatant was measured at a wavelength of 535 nm using a spectrophotometer. Instead of the sample solution, 0.4 ml of a 50% ethanol solution was added as a control, and the absorbance was measured. The inhibition rate (%) for this control was determined, and the concentration of 50% inhibition was determined as IC ₅₀
(%).

(8) Moisturizing Test An aqueous solution with the sample concentration adjusted to 2.0% was applied to the forearm flexion side of a healthy person, and the water content after 30 minutes was measured as electrical conductivity by an impedance meter. The result was 1 before application.
The values are shown as relative values when 00 is set.

(9) Sensory test A sensory test was conducted by 20 female panelists to evaluate whether or not they felt sticky at the time of applying the cosmetic and after the application, and the results were indicated by the number of panelists who answered "not felt". Was.

Examples 1-2, Comparative Examples 1-3

(Effect of Inhibiting Active Oxygen Production and Inhibiting Lipid Peroxide) The active oxygen production inhibiting effect was determined by using a 50% ethanol aqueous solution of Pycnogenol [raw material manufactured by Hofer Research Laboratory (Switzerland)] having the concentration described in the above method. Prepared (Example 1). For the effect of suppressing lipid peroxide, a 50% ethanol aqueous solution of Pycnogenol at the concentration described in the above method was prepared (Example 2). A 50% aqueous ethanol solution as each comparative example was used as Comparative Example 1 and Comparative Example 2, respectively. As a result, as shown in Table 3, as compared with Comparative Examples 1 and 2, Examples 1 and 2 exhibited excellent active oxygen production suppressing effects and lipid peroxide suppressing effects.

[0041]

[Table 3]

Examples 3-4, Comparative Examples 3-5 (Sensory test) Pycnogenol [Activator (Polysorbate 80) aqueous solution containing 2.0% of a raw material manufactured by Hofer Research Laboratory (Switzerland) was prepared (Example) 3) Then, an aqueous solution of an activator (Polysorbate 80) containing 1.0% each of Pycnogenol and diisopropylamine dichloroacetate was prepared (Example 4). Further, as Comparative Examples 3 and 4, aqueous solutions containing 2.0% of glycerin and sodium pyrrolidonecarboxylate were prepared, and water was used as Comparative Example 5.

[0043]

[Table 4]

As is evident from the results in Table 4, compared to the water of Comparative Example 5, Picgenol used in the present invention (Example 3) and the combination of Pycnogenol and DADA (Example 4) were moisturizing and sticky. Was excellent. On the other hand, glycerin (Comparative Example 3) and sodium pyrrolidonecarboxylate (Comparative Example 4) were inferior in moisture retention and stickiness.

Examples 5 to 9 and Comparative Example 6 (skin cream) Pycnogenol [powder raw material manufactured by Hofer Research Laboratory, Switzerland] was used.

Composition Composition (%) ------------------------------------------ --------------- (A) Self-emulsifying glyceryl monostearate 3.5 Sorbitan monostearate 1.5 (B) Liquid paraffin 25.0 Whale wax 5.0 Lanolin 5 2.0 Cetanol 2.0 (C) Glycerin 3.0 Carboxyvinyl polymer 5.0 Active ingredient Table 5 P-oxybenzoic acid ester 0.2 Purified water Remaining amount (D) Fragrance 0.2

Preparation Method The raw materials of the above group (A) were melted at 70 ° C., mixed with the raw material (B), and heated to 78 ° C. Then, this was gradually added to the raw material (C) heated to 75 ° C. with stirring to perform preliminary emulsification. Thereafter, the mixture was completely emulsified with a homogenizer, cooled to 50 ° C., added (D), and cooled to 30 ° C.

Table 5 shows the results of various tests conducted on the skin cream. Pycnogenol (Examples 5, 6, 7) and a blend of Pycnogenol and DADA (Examples 8 and 9) were compared with Comparative Example 6 in terms of turnover speed,
Both the rough skin improving effect and the keratin improving effect showed excellent effects.

[0049]

[Table 5]

Example 10 (Lotion)

Composition% --------------------------------------------- Ethanol 10.0 Polyoxyethylene hydrogenated castor oil 0.2 Paraben 0.1 Pycnogenol described in Example 5 2.0 Fragrance 0.01 Glycerin 3.0 Disodium hydrogen phosphate 0.02 Potassium dihydrogen phosphate 0.08 100% water

The lotion of the present invention was prepared by the usual method as described above and subjected to various tests for the turnover speed, the effect of improving rough skin, the effect of improving keratin, the moisturizing property and the functionality. Lotion (Example 10)
Was superior in all respects to lotion containing no active ingredient, and 14 out of 20 panelists had a moist feeling and no sticky feeling.

Example 11 (Emulsion)

Composition% --------------------------------------------- -Squalane 5.0 monogly 1.2 behenyl alcohol 0.5 petrolatum 2.0 paraben 0.2 pycnogenol 1.0 xanthan gum described in Example 5 0.1 1,3-BG 5.0 sodium acylglutamate 0.5 water 100% of the total amount

Examples 12 to 16, Comparative Example 7 (Heart Tonic)

Composition% --------------------------------------------- -Ethanol 40.0 Active ingredient Listed in Table 6 Glycerin 1.0 Menthol 0.03 Fragrance 0.01 Isopropylmethylphenol 0.1 Water 100%

The hair tonic of the present invention was prepared by the conventional method as shown in the above composition, and the respective tests were carried out for the mouse hair growth promoting effect and the human hair growth promoting effect (Table 6). Hair tonic (Example 1
2-16) were superior in all respects to the hair tonic containing no active ingredient (Comparative Example 7). In addition, as a result of conducting each test for the moisturizing property and the sensory property, 16 out of 20 panelists evaluated that they had a moist feeling and no sticky feeling.

[0058]

[Table 6]

Example 17 (Shampoo)

Composition% ---------------------------------------------- ----------------- Coconut oil fatty acid diethanolamide 5.0 Sodium polyoxyethylene lauryl sulfate 12.0 Sodium polyoxyethylene alkyl sulfosuccinate 7.0 Coconut fatty acid propyldimethylamino acid Betaine acetate 10.0 Pycnogenol described in Example 5 1.0 Fragrance 0.3 Water 100% of total amount

Example 18 (bath agent)

Composition% --------------------------------------------- --- Sodium chloride 10.0 Potassium chloride 6.0 Sodium bicarbonate 35.0 Glycerin 0.2 Pycnogenol described in Example 5 1.0 Silicic anhydride 1.0 1,3-BG 0.001 Fragrance 0.5 100% dry sodium sulfate

The shampoo of the present invention of Example 17 was evaluated as moisturizing the hair as compared with shampoos containing no active ingredient in the range of 11 to 14 out of 20 panelists. Of the bathing agents of 11 panelists out of 20 panelists, compared with bathing agents containing no active ingredient, were superior in rough skin improving effect, keratin improving effect and sensory test, and were evaluated as moist skin. Met.

[0064]

As described above, according to the present invention, the skin aging prevention effect (active oxygen suppression effect, lipid peroxide suppression effect,
Excellent effect of improving rough skin, improving keratin, and increasing turnover speed), has an excellent effect of stimulating hair root metabolism in the scalp and promoting hair root growth, and is excellent in moisture retention and non-stickiness. It is clear to provide new cosmetics with excellent organoleptic properties.

──────────────────────────────────────────────────続 き Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI Theme coat ゛ (Reference) A61K 7/00 A61K 7/00 W A61P 17/00 31/00 617 17/16 617J A61K 35/78 35 / 78 C // A61K 7/06 7/06 7/075 7/075 7/50 7/50 C07D 311/62 C07D 311/62 (72) Inventor Sayuri Yamaguchi 5-3-28 Kotobukicho, Odawara City, Kanagawa Prefecture F-term in Kanebo Co., Ltd. Basic Research Laboratory (reference) AD532 CC04 CC05 CC25 CC33 CC38 DD23 DD27 DD31 EE07 EE12 EE13 EE22 EE42 FF05 4C088 AB03 AC06 AC08 BA08 BA09 BA10 CA05 CA06 CA07 CA08 CA09 CA14 MA17 MA22 MA28 MA63 NA 14 ZA89 ZC33 ZC75

Claims (2)

[Claims] 1. A cosmetic comprising a pine bark derived from a pine bark having a proanthocyanidin represented by the following general formula as a main component. Embedded image (However, in the formula, n represents the number of 1 to 1,000, and R represents a hydrogen atom or a hydroxyl group.) 2. A cosmetic comprising a pine bark-derived component mainly composed of proanthocyanidin and diisopropylamine dichloroacetate.