JPH10120561A - Skin preparation for improving sputum for external use - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain the subject skin preparation containing a hydroxy fatty acid and capable of improving the action of sputum. SOLUTION: The skin preparation contains a hydroxy fatty acid or its salt as an active ingredient. The hydroxy fatty acid includes 10-hydroxydecenoic acid, and is contained in an amount to 0.001-10wt.%, preferably 0.01-5wt.%, based on the whole amount of the skin preparation. The skin preparation has a beautifully skin-whitening action, an atopic dermatitis-treating action, a dermatitis group-treating action, a dermatomycosis-treating action, a verruca-treating action, a dyspigmentation-treating action, a psoriasis vulgaris-treating action, a senile xeroderma-treating action, a senile keratoma-treating action, a skin damage-treating action, a hair growth-stimulating action, a perspiration- stimulating action, a digestive juice secretion-stimulating action, a diuretic action, a dejection-stimulating action, etc. The preparation is effective for preventing the decline of skin, treating atopic dermatitis, preventing the crisis and exacerbation of the atopic dermatitis, stimulating the growth of hair, preventing the falling of hair, improving eczema, preventing the exacerbation of the eczema, stimulating bowel movement and urination, etc.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an external preparation for skin such as cosmetics and medicines, which is useful for improving the action of tsukusu.

[0002]

2. Description of the Related Art The concept of qi, blood, and water in Chinese medicine has long been studied because of its uniqueness in understanding its pharmacological action and a rational index for selecting Chinese medicine. Of these, many have been elucidated about the meanings of qi and blood. For example, it is known that blood is a keyword that represents the supply and metabolism mainly of energy such as oxygen and nutrition, and ki is a keyword that represents the status of the homeostasis of life activity and the status of the driving force of life activity. Have been.

[0003] However, only the metabolism and excretion of waste products is known for the function of water (tsu liquor).
Since the recognition was delayed in the logical form of water, the elucidation of its true action (Tsukumi action) was incomplete. Also, little is known about the relationship between the pulp action and the various pharmacological actions recognized in modern medicine, and the role of pulp in modern medicine. The development of cosmetics, medicines, etc. that bring about such problems has been desired.

[0004]

DISCLOSURE OF THE INVENTION The present invention has been made in view of such circumstances, and has as its object to clarify the true function of a tsuju and to provide an external preparation for skin used to improve the action of a tsuku. And

[0005]

Means for Solving the Problems In view of such a situation, the present inventors have conducted intensive studies in search of the true function of tsuju. It was found that it stimulates the organs responsible for extracorporeal secretion and promotes the secretion of body water out of the body. Then, as a result of examining substances capable of stimulating such secretory organs and promoting / improving the action of the pulp, the present invention was completed.

[0006] That is, the present invention relates to a compound selected from the group consisting of hydroxy fatty acids and physiologically acceptable salts thereof.
It is intended to provide a skin external preparation for tsumugi improvement containing one or more kinds of active ingredients.

[0007] The present inventors have found that the essence of the tanning solution, which promotes the secretion of water from the dermis to the epidermis and causes the epidermis to retain sufficient moisture, atopic dermatitis, eczema,
Dermatomycosis, warts, pigmentation, psoriasis vulgaris, senile xeroderma, senile keratoma, therapeutic effects on various skin diseases such as burns,
It has been found that the action is related to a hair growth promoting action, a sweat promoting action, a digestive juice secretion promoting action, a diuretic action and a bowel movement promoting action caused by promoting water secretion in the stomach wall, kidney and intestinal tract.

[0008] That is, the medicinal classification of Chinese herbal medicines was examined in detail, and compared with modern medicine classifications.
It is said that the effects of the herbs such as shampoo, irrigation, conduction and prosthesis are related to beautiful skin effect, atopic dermatitis treatment, and dermatitis group treatment represented by eczema in the modern pharmaceutical classification. , Dermatomycosis treatment, wart treatment, pigmentation such as hepatitis, psoriasis vulgaris, senile xeroderma, senile keratoma treatment, skin damage treatment due to physical causes It has been found that it is closely related to the action, the hair growth promoting action, the digestive juice secretion promoting action, the sweating promoting action, the diuretic action and the bowel movement promoting action.

Based on this finding, screening was carried out on various substances based on their beautifying effect, therapeutic effect on atopic dermatitis, promoting hair growth, treating eczema, promoting secretion of digestive juice, and promoting sweating. It has been found that hydroxy fatty acids or physiologically acceptable salts thereof are excellent in such effects. More surprisingly, it has been found that the topical administration of a hydroxy fatty acid or a physiologically acceptable salt thereof has an effect of promoting secretion of digestive juices such as stomach acid, and has led to the completion of the present invention. Was.

Although it is known that hydroxy fatty acids or physiologically acceptable salts thereof have a transdermal absorption-promoting action, a liver function-improving action and an immune function-improving action, the essence of Tsutsumi There was no room for improvement. Furthermore, hydroxy fatty acids or physiologically acceptable salts thereof are effective in skin beautifulning, atopic dermatitis, eczema, dermatomycosis, warts, pigmentation, psoriasis vulgaris, senile xerosis, senile keratoma It has never been known that it has an action for treating skin diseases such as burns, an action for promoting hair growth, an action for promoting sweating, an action for promoting digestive juice secretion, an action for diuresis, and an action for promoting bowel movement.

[0011]

Embodiments of the present invention will be described below. The skin external preparation for tsumuage improvement of the present invention contains one or more active ingredients selected from the group consisting of hydroxy fatty acids and physiologically acceptable salts thereof. Examples of the hydroxy fatty acid include 10-hydroxydecenoic acid, iprolic acid, hydroxymyristic acid, 9,10-dihydroxyoleic acid, and the like, and any of them can be used. Among these, hydroxymyristic acid has various isomers depending on the position of the hydroxyl group, and among them, those derived from commercial land, which is a Chinese herbal medicine, are particularly preferable.

Examples of physiologically acceptable salts of hydroxy fatty acids include alkali metal salts such as sodium and potassium, alkaline earth metal salts such as calcium and magnesium, ammonium salts, and organic amines such as triethylamine and triethanolamine. Preferred examples include salts, basic amino acid salts such as lysine and arginine. These counterbases may be used alone or in combination of two or more. All of these hydroxy fatty acids or physiologically acceptable salts thereof are commercially available and available.

Examples of the external preparation for skin of the present invention include cosmetics such as basic cosmetics, make-up cosmetics, hair cosmetics, bath preparations and the like, and skin external pharmaceutical compositions such as anti-inflammatory external preparations. The preferred content of the hydroxy fatty acid or the physiologically acceptable salt thereof in the skin external preparation of the present invention is 0.001 to 10% by weight, more preferably 0.01 to 5% by weight, based on the whole skin external preparation. And more preferably 0.01 to 3% by weight.

The external preparation for skin of the present invention may contain, in addition to the hydroxy fatty acid or a physiologically acceptable salt thereof, optional components commonly used in cosmetics, external pharmaceutical compositions for skin and the like. Such optional components include hydrocarbons such as petrolatum and microcrystalline wax, esters such as jojoba oil and gay wax, triglycerides such as tallow, olive oil, higher alcohols such as cetanol and oleyl alcohol, and stearic acid. Fatty acids such as oleic acid, polyhydric alcohols such as glycerin and 1,3-butanediol, nonionic surfactants, anionic surfactants, cationic surfactants, amphoteric surfactants, ethanol, carbopol, etc. Examples include a thickener, a preservative, an ultraviolet absorber, an antioxidant, a pigment, and powders. The external preparation for skin of the present invention can be produced by treating these optional components with a hydroxy fatty acid or a physiologically acceptable salt thereof according to a conventional method.

[0015] The skin external preparation for improving tidal fluid of the present invention is used for promoting and improving the tidal fluid action. It is known that the tsuju action is expressed in a living body as a mode of expression, such as a shampooing action, a water-supplying action, a prosthesis action, and a conduction action. As a herbal crude drug having these effects, if it is a shampooing effect, rhubarb, banshayou, rokai, machinin, kengoshi, Kansui, Genka, Zokuzuishi, kyukyu compi, etc. Chorei, Bukuryo, Taksha, Inchinko, Jokuinin, Toukanin, Difushi, Tokhihi, Kinsenso and the like are known, and as herbal crude drugs having a prosthetic effect, Shajin, Eurasia, Tenmondou, Bakumondou,
Ginseng, arctic, antelope, sycamore, renren, jotenishi, sesame, kokuzu, kiban, bekko are known, and as a herbal crude drug having an antidepressant effect, hawthorn, krenkonpi, hishi, kakushitsu, reigan, areca, nankashi, Taisan and the like are known.

Examining the literature and the like about these,
It has been found that pharmacological actions such as beautifying action, hair growth-promoting action, anti-allergic action, anti-inflammatory action, and digestion promoting action overlap. Here, the present inventors pay attention, and consider "water" (Tsu liquid).
Works in modern medicine to treat skin disorders such as skin beautification, atopic dermatitis, eczema, dermatomycosis, warts, pigmentation, psoriasis vulgaris, senile xeroderma, senile keratoma and burns It has been found that the action, the hair growth promoting action, the therapeutic action of pimples, the digestive juice secretion promoting action, the sweat promoting action, the diuretic action, the bowel movement promoting action and the like can be used as indices. In addition, substances having one of these actions often have other actions to a greater or lesser degree. Therefore, if screening is performed using one of these actions as an index, other actions can be estimated.

The skin external preparation for improving a tanning solution of the present invention is represented by a skin beautiful action, an atopic dermatitis treatment action, a dermatitis group treatment action represented by eczema, a dermatomycosis treatment action, a wart treatment action, and hepatitis. Therapeutic action for pigmentation disease, psoriasis vulgaris, senile xeroderma, senile keratoma, skin damage treatment due to physical causes, hair growth promoting action, digestive secretion promoting action, sweat promoting action Has a function to improve at least one selected from the group consisting of a bowel movement promoting action, and a urination promoting (diuretic) action, and by using this,
Exhibits the effects of preventing and improving skin deterioration, treating atopic dermatitis and preventing the onset and worsening, promoting hair growth and preventing hair loss, improving and preventing eczema, promoting bowel movements and promoting urination. Is done.

The preferred dosage of the external preparation for skin of the present invention is
The appropriate amount may be applied once or several times a day to a part or the whole of the affected skin or healthy skin, depending on the kind of the disease and the characteristics of the patient.

In particular, it should be noted that the hydroxy fatty acid of the present invention or a physiologically acceptable salt thereof has effects such as promotion of secretion of digestive juices such as stomach acid by transdermal administration. However, there is no known substance capable of simultaneously expecting such an effect by transdermal administration.

[0020]

Embodiments of the present invention will be described below. The unit of the numerical value of the prescription in the table is part by weight.

[0021]

Examples 1 to 5 <Formulation Examples> Skin external preparations (creams) were prepared according to the formulations shown in Table 1 below. That is, each of the component groups (a), (b) and (c) is heated at 80 ° C., (a) is kneaded well, (b) is added thereto, diluted, and (c) Was gradually added and emulsified, followed by stirring and cooling to obtain a skin external preparation.
It is highly safe and has an excellent essence as shown in the following test examples, and is therefore useful as a pharmaceutical composition and as a cosmetic.

[0022]

[Table 1]

[0023]

Examples 6 to 10 <Formulation Examples> A skin external preparation (ointment) was prepared using the components shown in Table 2 below and according to the formulation. That is, each prescription component was weighed into a kneader and kneaded well to obtain an ointment.

[0024]

[Table 2]

[0025]

Examples 11 to 15 <Formulation Example> An external preparation for hair for hair (hair tonic) was prepared using the components shown in Table 3 below and according to the formulation. That is, each formulation component was stirred and solubilized at room temperature to obtain a hair tonic.

[0026]

[Table 3]

[0027]

Examples 16 to 20 <Formulation Examples> Bath ingredients were prepared using the components shown in Table 4 below and according to the formulations. That is, the respective components were kneaded with a kneader to obtain a bath agent.

[0028]

[Table 4]

[0029]

Example 21 <Test Example 1: Improving Beautiful Skin> Ten panelists, 29 to 39 years old, suffering from rough skin, applied the skin external preparations (0.02 g) of Examples 1 to 3 twice daily in the morning and evening. Each was applied to the affected area for two months, and the effect of improving skin roughness was evaluated. The evaluation criteria were very improved (gradation 5) to not improved (gradation 0). As a control, a hydroxy fatty acid or a physiologically acceptable salt thereof, which is an active ingredient of the present invention, was replaced with water. The results are shown in Table 5 as average scores. This indicates that the external preparation for skin of the present invention has an effect of improving rough skin, that is, has a skin beautiful effect. That is,
It is understood that the hydroxy fatty acid of the present invention or a physiologically acceptable salt thereof has such an effect.

[0030]

[Table 5]

[0031]

Example 22 <Test Example 2: Hair growth promoting action> The back of 5 mice per group of C3H mice was shaved, and 10 mg of a sample shown in Table 6 below was dissolved or dispersed in 200 µl of physiological saline and applied. The hair growth promoting effect was evaluated by observing the hair growth. The control was vehicle saline only. The evaluation criteria are ++ (score 4): significantly earlier than the control, + (score 2): earlier than the control, ± (score 1): slightly earlier than the control,
-(Score 0): Not earlier than control. The results are shown in Table 6 as average scores. This shows that hydroxy fatty acid or a physiologically acceptable salt thereof, which is an active ingredient of the external preparation for skin of the present invention, has an excellent hair growth promoting action.

[0032]

[Table 6]

[0033]

Example 23 <Test Example 3: Effect on atopic dermatitis> A group of 10 panelists aged 23 to 39 years old suffering from atopic dermatitis
The external preparation for skin (0.02 g) of the above Examples 1 to 3 was applied to the affected area twice a day and twice a day for 2 months to evaluate the effect of improving atopic dermatitis. The evaluation criteria were very improved (gradation 5) to not improved (gradation 0). As a control, the hydroxy fatty acid of the present invention or a physiologically acceptable salt thereof was replaced with water. The results are shown in Table 7 as average scores. This indicates that the external preparation for skin of the present invention has an effect of improving atopic dermatitis.
That is, it is understood that the hydroxy fatty acid of the present invention or a physiologically acceptable salt thereof has such an effect.

[0034]

[Table 7]

[0035]

Example 24 <Test Example 4: Eczema treatment> 19-25 suffering from breakout
A group of 10-year-old panelists applied the skin external preparations of Examples 1 to 3 (0.02 g) twice a day for 2 months to evaluate the eczema improving effect. The evaluation criteria were very improved (gradation 5) to not improved (gradation 0).
As a control, the hydroxy fatty acid of the present invention or a physiologically acceptable salt thereof was replaced with water. The results are shown in Table 8 as average scores. This indicates that hydroxy fatty acid or a physiologically acceptable salt thereof, which is an active ingredient of the external preparation for skin of the present invention, has an effect of improving eczema.

[0036]

[Table 8]

[0037]

Example 25 <Test Example 5: Gastric secretion promoting action> The secretion of gastric juice was examined using an anesthetized dog. That is, an endoscope with an administration device was introduced into the stomach of a dog anesthetized with a pentobarbitur, and the specimen was used as a sample.
50% of a hydroxy fatty acid or a physiologically acceptable salt thereof as an active ingredient of the external preparation for skin of the present invention shown in
It was dissolved or dispersed in 200 μl of an aqueous ethanol solution and transdermally administered to the back, and the secretion of gastric juice before and after the dissolution was observed to evaluate the gastric secretion promoting action. As a control, only physiological saline was used. Evaluation criteria were as follows: ++ (score 4): gastric secretion increased significantly compared to control, + (score 2): increased gastric secretion compared to control, ± (score 1): slightly increased compared to control ,-(Score 0): the secretion did not increase compared to the control. Table 9 shows the results. This indicates that the hydroxy fatty acid or a physiologically acceptable salt thereof, which is an active ingredient of the present invention, has an excellent gastric secretion promoting action.

[0038]

[Table 9]

[0039]

Example 26 <Test Example 6: Effect of promoting bowel movement and urination> ICR mice were bred in metabolic cages. In the administration group, the skin external preparations of Examples 1 to 3 were applied to the shaved back skin as a specimen at a rate of 1 g / day / animal, 0.5 g twice daily in the morning and evening, and transdermally administered for 7 days. . The amount of urine and feces 24 hours after the last dose was monitored. The control group received no specimen. Each group consisted of 10 animals. Table 10 shows the value obtained by dividing the total urine volume of the sample administration group by the total urine volume of the control group and the value obtained by dividing the total feces volume of the sample administration group by the total feces volume of the control group. This shows that the hydroxy fatty acid of the present invention or a physiologically acceptable salt thereof is excellent in the bowel movement promoting action and urination promoting action (diuretic action).

[0040]

[Table 10]

[0041]

According to the present invention, a beautiful skin effect, a therapeutic effect on atopic dermatitis, a therapeutic effect on a dermatitis group represented by eczema,
Treatment for dermatomycosis, treatment for warts, treatment for pigmentation such as hepatitis, treatment for psoriasis vulgaris, treatment for senile xeroderma, senile keratoma, treatment for skin damage due to physical causes It is possible to provide a skin external preparation capable of improving a tsukusu action selected from the group consisting of a hair growth promoting action, a digestive juice secretion promoting action, a sweating promoting action, a bowel movement promoting action, and a diuretic action.

──────────────────────────────────────────────────の Continued on the front page (51) Int.Cl. ⁶ Identification code FI A61K 31/20 ABE A61K 31/20 ABE (72) Inventor Nobuhiro Ando 27-1, Takashimadai, Kanagawa-ku, Yokohama-shi, Kanagawa Prefecture Pola Chemical Industry Co., Ltd. (72) Inventor Yoshie Muramatsu Yoshikazu Muramatsu 27-1 Takashimadai, Kanagawa-ku, Yokohama-shi, Kanagawa Pref.Pola Chemical Industry Co., Ltd. Inside Totsuka Laboratory Co., Ltd.

Claims (6)

[Claims] 1. A skin external preparation for improving a tanning solution, comprising one or more active ingredients selected from the group consisting of hydroxy fatty acids and physiologically acceptable salts thereof. 2. The external preparation for skin according to claim 1, wherein the hydroxy fatty acid is cholic acid. 3. The improvement according to claim 1, wherein the hydroxy fatty acid and one or more selected from the group consisting of physiologically acceptable salts thereof are contained in an amount of 0.001 to 10% by weight. External preparation for skin. 4. The external preparation for skin according to claim 1, which is a cosmetic. 5. The external preparation for skin according to claim 1, which is a medicament. 6. A beautiful skin effect, an atopic dermatitis treatment effect,
Dermatitis group treatment, dermatomycosis treatment, wart treatment, pigmentation treatment, psoriasis vulgaris, senile xerosis, senile keratoma treatment, skin damage treatment, hair growth The external preparation for skin according to any one of claims 1 to 5, which is used for improving a tsutsuma action selected from the group consisting of a promoting action, a digestive juice secretion promoting action, a sweating promoting action, a bowel movement promoting action, and a diuretic action.