JPH10114665A - Improver for aqueous body fluid and composition for oral administration comprising the same - Google Patents

Abstract

PROBLEM TO BE SOLVED: To prepare the subject improving agent, comprising a specific compound, capable of stimulating secretory organs and promoting actions of aqueous body fluids (water), having actions such as skin beautifying actions and therapeutic actions on atopic dematitis and useful as a food or a medicine. SOLUTION: This improver for aqueous body fluids (water) comprises bile acid and/or its physiologically permissible salt, preferably cholic acid. For example, the improving agent is preferably orally administered in 1-10,000mg daily dose for an adult in one to several divided portions at the time of administration. In the case of a food composition, the content of the improver for the aqueous body fluids (water) is preferably 0.001-50wt.% based on the whole composition. In the case of a pharmaceutical composition, the content thereof is preferably 0.1-60wt.% based on the whole composition.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an agent for improving tsunami which has an effect of improving the effect of tsunami, and a composition containing the same for oral administration of foods, medicines and the like.

[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 foods, medicines, etc. that bring about this has been desired.

[0004]

DISCLOSURE OF THE INVENTION The present invention has been made in view of such circumstances, and clarifies the true action of tsuju, and can improve the tsuju action, and foods, medicines and the like containing the same. It is an object of the present invention to provide a composition for oral administration.

[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, they found a tsumuco-ameliorating agent, which is a substance capable of stimulating such secretory organs and promoting / improving the action of tsumuju, and completed the present invention.

[0006] That is, the present invention provides a tsutsumitsu improving agent comprising bile acid and / or a physiologically acceptable salt thereof. In addition, the present invention provides a composition for oral administration containing the above-mentioned tsukumo-improving agent.

[0007] The tsumuco-ameliorating agent of the present invention is a substance having an effect of stimulating an organ responsible for the secretion of water to the outside of the body to promote the secretion of body water to the outside of the body, thereby promoting and improving the effect of the tsuno-solution, that is, a substance having an effect of improving tsuku-solution. Say. The present inventors have proposed a tanning effect that promotes the secretion of water from the dermis to the epidermis and retains sufficient water in the epidermis, a beautiful skin effect, atopic dermatitis, eczema, dermatomycosis, warts, and pigmentation. It is caused by promoting the treatment of various skin diseases such as psoriasis vulgaris, senile xeroderma, senile keratoma, and burns, promoting hair growth, promoting sweating, and promoting water secretion in the stomach wall, kidneys and intestinal tract. It has been found that it is an action related to digestive juice secretion promoting action, diuretic action, and bowel movement promoting action.

[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 the index of skin beautiful action, atopic dermatitis treatment action, hair growth promotion action, eczema treatment action, digestive juice secretion promotion action, sweat promotion action. It has been found that bile acids and / or their physiologically acceptable salts are excellent in such effects. Although it is known that bile acid and / or its physiologically acceptable salt has a percutaneous absorption promoting action, a liver function improving action and an immune function improving action, a true sense of tsuyu There was no room for improvement. Furthermore, bile acids and / or physiologically acceptable salts thereof may be used as a skin beautifier, atopic dermatitis, eczema, dermatomycosis, warts, pigmentation, psoriasis vulgaris, senile xerosis, senile horn It has never been known that it has an action of treating skin diseases such as chemosis and burns, an action of promoting hair growth, an action of promoting sweating, an action of promoting digestive secretion, a diuretic action, and an action of promoting bowel movement.

[0010]

BEST MODE FOR CARRYING OUT THE INVENTION

(1) Tsutsumi-improving agent of the present invention The tsumumo-improving agent of the present invention comprises bile acid and / or a physiologically acceptable salt thereof. Bile acids include cholic acid, deoxycholic acid, ursodeoxycholic acid, lithocholic acid, dehydrocholic acid, lithocholic acid, glycocholic acid, taurocholic acid, tauroglycocholic acid, taurochenodeoxycholic acid, taurodeoxycholic acid, glycochenodeoxychol Examples thereof include acid, glycodeoxycholic acid, glycolicholic acid, chenodeoxycholic acid, and 7-ketolithocholic acid, and any of these can be used. Examples of physiologically acceptable salts of bile acids include, for example, alkali metal salts such as sodium and potassium, alkaline earth metal salts such as calcium and magnesium, ammonium salts, organic amine salts such as triethylamine and triethanolamine, and lysine. And basic amino acid salts such as arginine and the like. These counterbases may be used alone or in combination of two or more. These bile acids and / or
Alternatively, all physiologically acceptable salts thereof are commercially available and available.

[0011] The agent for improving a tsunami of the present invention comprising a bile acid and / or a physiologically acceptable salt thereof has an effect of accelerating and improving the activity of a tsuju. 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 medicine having these effects, if it is a shampooing effect, rhubarb, banshayou, rokai, machinin, kengoshi, kansui,
Genka, Zokuzushi, Ryukyu compi and the like are known, and as a Chinese herbal medicine having a water-utilizing effect, Chorei, Bukuryo, Taksha, Inchinko, Yokuinin, Toukanin, Difushi, Toukihi, Kinsenso etc. are known and have a complementing effect. As a herbal medicine, shajin,
Known as Chinese herbal medicines such as Hawthorn, Krenkompi, Hishi and Kakushitsu are known as Chinese herbal medicines having a dissipating effect. , Lygan, Areca, Nankashi, Taisan and the like are known.

Examining the literature etc. 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 essence improving agent of the present invention can be used as a skin beautifying agent, atopic dermatitis treatment, dermatitis group represented by eczema, dermatomycosis treatment, wart treatment, and pigmentation represented by hepatitis. Therapeutic action, psoriasis vulgaris treatment, senile xeroderma, senile keratomas treatment, skin damage treatment due to physical causes, hair growth promotion, digestive juice secretion promotion, sweating promotion, bowel movement promotion It has an effect of improving at least one selected from the group consisting of an action and a urination-promoting (diuretic) action, and by administering it, prevents and ameliorates skin deterioration, and treats atopic dermatitis. Effects such as prevention of onset and deterioration, promotion of hair growth and prevention of hair loss, improvement of eczema and prevention of deterioration, promotion of bowel movement and promotion of urination are exhibited. The preferred dose of the tsukumo ameliorating agent varies depending on the type of disease and the characteristics of the patient, but is preferably 1 to 1000 per adult per day.
0 mg may be orally administered once or divided into several times.

In particular, it should be noted in the present invention that bile acids and / or physiologically acceptable salts thereof have multiple actions at the same time, for example, by oral administration, the skin becomes beautiful and the hair growth is promoted. The point that can be prepared.
That is, preferably, the essence improving agent of the present invention is represented by a skin beautifying effect, a therapeutic effect on atopic dermatitis, a therapeutic effect on a dermatitis group represented by eczema, a therapeutic effect on dermatomycosis, a therapeutic effect on warts, and a hepatitis. Treatment for pigmentation, treatment for psoriasis vulgaris, treatment for senile xerosis, treatment for senile keratoma, treatment for skin damage due to physical causes, hair growth promotion, digestive secretion promotion, sweating promotion, It has the effect of improving two or more actions selected from the group consisting of a bowel movement promoting action and a diuretic action. There is no known substance capable of simultaneously achieving such an effect by oral administration.

(2) The composition for oral administration of the present invention The composition for oral administration of the present invention is characterized by containing the above-mentioned tsuyu improving agent of the present invention. The above-mentioned Tsutsumi improving agent may contain one kind or two or more kinds.

Examples of the composition for oral administration include food compositions and pharmaceutical compositions processed into granules, powders, tablets, capsules, candies, gums, gummy gums and the like. The preferred content of the tsukumo improver of the present invention, in the case of a food composition,
0.001 to 50% by weight based on the whole composition;
The content is more preferably from 0.01 to 20% by weight, even more preferably from 0.01 to 15% by weight. Moreover, in the case of a pharmaceutical composition, 0.1 to
It is preferably 60% by weight, more preferably 0.5 to 50% by weight, and still more preferably 1 to 30% by weight.

[0017] The composition of the present invention may contain, in addition to the above-mentioned tsutsumi-improving agent, optional components commonly used in food compositions and pharmaceutical compositions. As such an optional component, if it is a pharmaceutical composition, an excipient, a binder, a coating agent, a lubricant, a sugar coating, a disintegrant, a bulking agent, a flavoring agent, an emulsifying / solubilizing / dispersing agent, Stabilizers, pH adjusters, isotonic agents, etc. can be exemplified, and in the case of food compositions, antioxidants, flavoring agents, thickeners, emulsion stabilizers, preservatives, flavoring agents, sweeteners, sour agents Etc. can be exemplified. The composition of the present invention can be produced by treating these optional components and the above-mentioned tsukumo improver according to a conventional method.

[0018] The composition of the present invention can be used for improving the essence of Tsutsumi. Specifically, beautiful skin action, atopic dermatitis treatment action, dermatitis group treatment action 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 can be used for improving an action selected from the group consisting of a hair growth promoting action, a digestive juice secretion promoting action, a sweat promoting action, a bowel movement promoting action, and a diuretic action.

[0019]

Embodiments of the present invention will be described below.

[0020]

Examples 1 to 5 <Formulation Examples> Tablets were prepared according to the formulations shown in Table 1. That is, the prescription components were weighed into a grading apparatus, and mixed by spraying 50 parts by weight of a 20% aqueous ethanol solution to prepare coarse granules. The coarse granules were blow-dried at 40 ° C. for 48 hours, and were compressed with a tableting machine to obtain 250 mg tablets. The units of the numerical values in Table 1 are parts by weight.

[0021]

[Table 1]

[0022]

Examples 6 to 10 <Formulation Examples> Using the components shown in Table 2, candy was prepared according to the formulation. That is, the prescription components were heated and melted at 120 ° C. and molded while cooling to obtain a candy.
The units of the numerical values in Table 2 are parts by weight.

[0023]

[Table 2]

[0024]

Examples 11 to 15 <Formulation Examples> Candies were prepared using the components shown in Table 3 according to the formulation. That is, the prescription components were heated and melted at 120 ° C. and molded while cooling to obtain a candy.
The units of the numerical values in Table 3 are parts by weight.

[0025]

[Table 3]

[0026]

Example 16 <Test Example 1: Improving Skin Beauty> Ten groups of panelists aged 24-36 years old suffering from rough skin,
g tablets) was evaluated twice a day in the morning and evening twice, one tablet only for two months, to evaluate the effect of improving skin roughness. The evaluation criteria were very improved (gradation 5) to not improved (gradation 0). As a control, lactose was used in place of the liquor improving agent of the present invention. The results are shown in Table 4 as average scores. From this, it can be seen that the rubbing liquid improving agent of the present invention has an effect of improving skin roughness by internal use, that is, has a beautiful skin effect.

[0027]

[Table 4]

[0028]

Example 17 <Test Example 2: Hair growth promoting action> The back of a group of five C3H mice was shaved, and 10 mg of a sample shown in Table 5 was added to physiological saline 20.
It was dissolved or dispersed in 0 μl and orally administered, and the subsequent hair growth was observed to evaluate the hair growth promoting effect. 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 5 as average scores. From this, it can be seen that the tsukumo improver of the present invention is excellent in hair growth promoting action.

[0029]

[Table 5]

[0030]

Example 18 <Test Example 3: Effect on atopic dermatitis> Ten groups of panelists aged 21 to 39 years old suffering from atopic dermatitis
The improvement effect of atopic dermatitis was evaluated only for the tablets (1 g tablets) of the above Examples 1 to 3 twice a day for 2 months. The evaluation criteria were very improved (gradation 5) to not improved (gradation 0). As a control, lactose was used in place of the liquor improving agent of the present invention. The results are shown in Table 6 as average scores. From this, it can be seen that the tsumugi improver of the present invention has an effect of improving atopic dermatitis by taking it internally.

[0031]

[Table 6]

[0032]

Example 19 <Test Example 4: Eczema Treatment> Ten groups of panelists aged 19 to 29 years old suffering from eczema were given the tablets (1 g) of Examples 1 to 3 above.
Tablets) was evaluated twice a day, in the morning and evening, one tablet at a time for 2 months only, to evaluate the effect of improving eczema. The evaluation criteria were very improved (gradation 5) to not improved (gradation 0). As a control,
A liquor of the present invention in which lactose was substituted was used. The results are shown in Table 7 as average scores. From this, it can be seen that the tsukutsu improver of the present invention has an effect of improving eczema by taking it internally.

[0033]

[Table 7]

[0034]

Example 20 <Test Example 5: Gastric secretion promoting effect> 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 sample was treated as shown in Table 8.
10 mg of the tsukumo improver of the present invention shown in
The solution was administered by dissolving or dispersing the solution in the gastric acid, and the secretion of gastric juice before and after the administration 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 8 shows the results. From this, it can be seen that the tsumugi improving agent of the present invention is excellent in gastric secretion promoting action.

[0035]

[Table 8]

[0036]

Example 21 <Test Example 6: Promotion of bowel movement and urination> ICR mice were bred in metabolic cages. In the administration group, the compositions of Examples 1 to 3 were orally administered at a dose of 0.5 g twice daily in the morning and evening at 1 g / day / animal. Urine and fecal volume were monitored for 24 hours. The control group received no specimen. Each group consisted of 10 animals. Table 9 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 fecal volume of the sample administration group by the total fecal volume of the control group. This indicates that the bile acid and / or a physiologically acceptable salt thereof of the present invention is excellent in a bowel movement promoting action and a urination promoting action (diuretic action).

[0037]

[Table 9]

[0038]

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 The present invention can provide a tsumucolytic agent having an effect of improving a tsukusei effect 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.

────────────────────────────────────────────────── ─── Continued on the front page (51) Int.Cl. ⁶ Identification code FI A61K 31/575 ACX A61K 31/575 ACX ADA ADA ADZ ADZ (72) Inventor Shin Fukushima 560 Kashiocho Kashio-cho, Totsuka-ku, Yokohama-shi, Kanagawa-ken Inside the Totsuka Research Laboratory, Inc. Polar Chemical Industry Co., Ltd. Yokohama Research Laboratory

Claims (7)

[Claims] 1. An agent for improving tsunami comprising a bile acid and / or a physiologically acceptable salt thereof. 2. The method of claim 1, wherein said bile acid is cholic acid.
The rubbing improver according to the above. 3. A composition for oral administration, comprising the tsukumo ameliorating agent according to claim 1 or 2. 4. The composition according to claim 3, which is a food. 5. The composition according to claim 3, which is a medicament. 6. The method according to claim 3, which is used for improving a tsufluid action.
The composition according to any one of claims 1 to 5. 7. The tanning solution is effective for beautifying skin, treating atopic dermatitis, treating dermatitis, treating dermatomycosis, treating warts, treating pigmentation, treating psoriasis vulgaris, and the elderly. Xeroderma sclerosis, senile keratoma treatment action, skin damage treatment action, hair growth promotion action, digestive secretion promotion action, perspiration promotion action, bowel movement promotion action, and an action selected from the group consisting of diuretic action, A composition according to claim 6.