JPH10139676A - Antiallergic composition for skin lotion - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain an antiallergic composition for skin lotion, effective to an allergic disease, especially atopic dermatitis and containing nontoxic extract of a plant. SOLUTION: This composition includes an extract extracted from whole plant such as a leaf, a flower, a stem and a root of Calanthe belonging to genus calanthe of orchid family by hydrated ethyl alcohol as an effective ingredient. The addition of sodium pantothenate, nicotinamide, tocopherol acetate, ascorbic acid, biotin, vitamins such as vitamin B6 , oils of animals and plants such as germ oil and oil of a horse, glycolic acid, sodium chloride, etc., can synergistically improve the effect. The composition has activities for skin care in addition to the antiallergic activities, and has fragrance when only the extract from the flower of the Calanthe is used. The composition is used as a skin lotion, a lotion, an emulsion, a cream, an ointment, etc., and further as a bathing agent.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to a novel antiallergic external skin composition containing a plant extract as an active ingredient,
Particularly, the present invention relates to an antiallergic skin external composition suitable for treating atopic diseases.

[0002]

2. Description of the Related Art Heretofore, as a treatment for allergic diseases such as atopic dermatitis, oral use of antihistamines, subcutaneous injection of immunoglobulin preparations, and external preparations such as steroid ointments have been used. However, these medicinal therapies have remarkable effects, but have strong side effects and are not suitable for long-term treatment. On the other hand, anti-allergic skin external composition, bath agent, which can be easily used at any time by anyone
Cosmetics and the like have been widely proposed. Many use plant extracts as active ingredients. For example, one using hibiscus leaf and aloe leaf juice (Japanese Unexamined Patent Publication No.
No. 306210), an extract using an amateur extract (JP-A-5-43445), an extract using a Labiatae plant (JP-A-6-293652), and an extract using a loquat leaf extract ( Japanese Patent Application Laid-Open No. 8-73314), those using extracts of Amaranthus (Japanese Patent Application Laid-Open No. 8-99889), and the like.
Many are known.

[0003] These plant-derived antiallergic extracts are different from a single isolated compound even when derived from a natural product, and are characterized in that their physiological and pharmacological actions are complicated and relatively mild. The daily care of such sensitive skin atopic diseases has the advantage of being accessible over the long term. In the case of a plant extract, the physiological and pharmacological activities thereof are usually slightly different depending on the type of the raw material plant, and some of them have a cosmetic effect on the skin. Therefore,
The dosage forms also vary, such as lotions, emulsions, creams, packs, ointments, lotions, bath preparations, and the like.

[0004]

In recent years, despite the development of many anti-allergic compositions, changes in dietary habits, environmental destruction, pharmaceuticals, cosmetics, and other personal items have been reported. People who complain of allergic symptoms such as dietary allergy, pollen allergy, drug allergy, contact allergy and the like due to contact with many chemicals such as synthetic resins, fibers and additives to foods are still increasing.

In view of the above situation, the present inventors have conducted intensive studies on various plants, particularly orchids, and surprisingly found that an extract of a certain genus orchid plant has an atopic dermatitis such as atopic dermatitis. The present inventors have found that the compound has a remarkable effect on allergic diseases and has no toxicity.

[0006] The present invention is based on this finding and has an object to provide a non-toxic external skin composition having an antiallergic effect.

[0007]

The antiallergic skin external composition of the present invention, which has achieved the above object, comprises, as an active ingredient, an extract from at least one species of Ebine belonging to the genus Ebine of the orchid family. Features.

[0008] The extract containing the active ingredient as an active ingredient includes various antiallergic compositions, therapeutic agents for atopic dermatitis,
It is useful as an antiallergic bath agent and antiallergic cosmetic. It is also effective in skin external compositions other than anti-allergic agents, for example, hemorrhoid treating agents, weeding, lacquering, insect repelling agents, bedsores, athlete's foot, and burns. In addition, it is extremely effective to use the undiluted solution as it is or diluted appropriately with water as an oral composition, especially a gargle for the treatment of alveolar pyorrhea and stomatitis. Lactic acid bacteria have a selective growth inhibitory effect.

[0009]

BEST MODE FOR CARRYING OUT THE INVENTION In the present invention, the following can be exemplified as Ebine of the genus Ebine of the family Orchidaceae. (1). Diebine type: diebine (C. discocol)
r), C. sieboldii, C. aristulifera, C. amamiana, C. ezine (C. iz)
u-insularis), Salmen ebine (C. tr
icarinata), Skull shrimp (C. tok)
unoshimaensis), Alisan Ebine (C.
arisanensis), Hosobanana ebine (C. gr)
aciliflora), Himalayan house lobster (C.
plantginea), chlororeuka (C. chl)
oroleuca), Togaribaebin (C. cauda)
tilabella). (2). Tin flea vine type: tin flea vine (C. li
ukiensis), Tamazaki ebine (C. dens)
iflora), Pulchra. (3). Taganelan type: Taganelan (C. bungoa)
na), Whiteana (C. whiteana). (4). Sakurajima shrimp type: Sakurajima shrimp (C.
oblanceolata), Mannii (C. mann)
i). (5). Kisoebin type: Kisoebin (C.schlec)
hteri), Alpina (C. alpina). (6). Kinseiran type: Kinseiran (C.nipp
onica). (7). Hirohanokaran type: Hirohanokaran (C. ja
ponica). (8). Asahyebine type: Asahyebine (C. hatt
orii). (9). Natsuebine type: Natsuebine (C. reflex
a). (10). Truran type: Turran (C. furcat
a), Long-tailed shrimp (C. longicarat)
a), Okinawa shrimp (C. okinawaensi)
s), masker (C. mascara), Madagascariensis, C. natalensis. (11). Toxalan type: Toxalan (C. venus)
ta), C. longipes, C. biloba. (12). Pasteta type: Vesteta (C. vesti
ta), Rosea (C. rosea), Hermerie (C. e)
lmeri), C. rubens, C. cardiolossa.

[0010] The prawn extract, which is an active ingredient of the present invention, comprises:
At least one flower of Ebine belonging to the genus Ebine,
It is an extract obtained from roots, stems, leaves or whole plants.
As the extraction solvent, lower alkyl alcohol, particularly ethyl alcohol is desirable from the viewpoint of safety. Ethyl alcohol may be pure ethyl alcohol, but industrially, hydrated ethyl alcohol is preferred. Spirits such as distilled spirits can also be used. The alcohol concentration in the hydrated ethyl alcohol is not particularly limited, but is about 30 to 9
0%, preferably about 40-70% is practical.

In the present invention, these ebine extracts are used in a mixture with the following additives rather than used alone, except in exceptional cases such as a composition for oral cavity. The effect is greatly improved. Examples of the additives include vitamins, animal and vegetable oils, glycolic acid, sodium chloride and the like. As vitamins, vitamin A
(Accessible Roff Torr), vitamin _{B 1} (thiamine), vitamin _{B 2} (riboflavin), vitamin _{B 6} (pyridoxine), vitamin C (L-ascorbic acid), vitamin E (tocopherol), vitamin H (biotin), nicotinic acid Nicotinamide, pantothenic acid, sodium pantothenate and potassium pantothenate. Animal and vegetable oils include horse oil, germ oil, egg oil, olive oil, camellia oil, rapeseed oil, sesame oil, and the like, and a combination of horse bath and germ oil is preferred.

The type and amount of the additive cannot be specified because it differs depending on the purpose of use. However, in the case of the antiallergic composition solution, about 5 to 10 g of tocophenol acetate and horse About 7-13 g of oil,
About 1 to 4 g of sodium pantothenate, about 1 to 4 g of nicotinamide, about 5 to 10 g of ascorbic acid, about 0.5 to 2 g of glycolic acid, and about 0.5 to 1 g of biotin
g, vitamin _{B 6} is approximately 0.5 to 2 g, desirably sodium chloride is about 12～18G. In addition, in the antiallergic cosmetic composition solution, preferably, about 1,000 to 1,000 ml of tocophenol acetate is used for 1,000 ml of the shrimp extract.
12g, horse oil about 4-8g, sodium pantothenate about 1-4g, nicotinamide about 1-3g, ascorbic acid about 8-15g, glycolic acid about 0.5-2g,
Vitamin _{B 6} is about 0.5~2g. In addition to the above substances, auxiliary additives usually added to antiallergic composition liquids and cosmetics can be appropriately used. Also lotions, emulsions, creams, packs, ointments, lotions,
Materials commonly used, such as bath agents, may be optionally used depending on the purpose of use or dosage form.

The mixing ratio of the shrimp extract and the additive composition solution is as follows:
Although it cannot be specified because it differs depending on the purpose of use, in the composition solution for anti-allergy, the shrimp extract
20% by volume, 5 to 10 for antiallergic lotion
% Is preferred.

The production of the shrimp extract is carried out, for example, as follows. Remove mud adhering to the rhizomes of Ebine and wash the whole plant with water. Next, the pieces are cut into small pieces with a cutter, a mixer or the like, and compressed and squeezed with a press. The pressing pressure of the press is about 500 to 5,000 kg / cm ² . 20-90% aqueous ethyl alcohol is mixed in the juice at a ratio of about 1: 1 (volume). Depending on the purpose of use, for example, in the case of an anti-allergic cosmetic, it is desirable to treat only fragrant Ebine flowers in the same manner as described above to obtain an extract. In the same manner as described above, the whole grass of the ebine that had been dropped and washed with water was cut into small pieces with a cutter, and then ground with a mixer.
About 20-90% ethyl alcohol about 20,000
0 ml may be mixed and stored tightly in a cool dark place for 7 to 10 days, followed by solid-liquid separation and filtration. These extracts are
Aged for about 1-2 weeks in a cool, dark place for further aging.

The mixture of the shrimp extract and other additives may be water-soluble or oil-soluble for vitamins, and the solvent may be water or hot water, including the relationship with the animal and vegetable oils used. , Ethyl alcohol or a mixed solution thereof, and it is preferable to substantially follow the examples described later. As an operation, heating is performed in principle with hot water and stirring if necessary.

The action of each additive is not always clear, but vitamins generally help mucous membrane and nerve health,
It has the function of preventing keratinization of the skin. Vitamin B ₁ , Vitamin B ₂ Stabilizes and activates nerves on the skin and mucous membranes and helps cell respiration. Vitamin C promotes skin metabolism, and vitamin E promotes blood circulation and activates cells.
Vitamin H, nicotinic acid, nicotinamide, pantothenic acid and salts thereof all improve metabolic functions, and biotin has a protective effect on skin diseases. Animal and vegetable oils soften the skin, and Mabyu and germ oil are particularly effective. Glycolic acid is used for pH adjustment, and sodium chloride, due to its osmotic action, makes it easier for the extract to be absorbed deep into the skin.

[0017]

Embodiment 1 (1). Preparation of Ebine extract: Diebine native to Yamano, Miyazaki Prefecture was used as a raw material. First, mud attached to the rhizomes of shrimp was dropped, and the whole plant was washed with water. Then, it was crushed with a mixer. 10,000 g of crushed pieces were compressed and squeezed by a press to obtain a squeezed liquid. Press compression pressure is 1,0
It was 00 kg / cm ² . About 20,000 ml of 70% aqueous ethyl alcohol was added to the squeezed liquid, and the mixture was aged in a cool and dark place for 10 days. After aging, solid-liquid separation and filtration,
Ebine extract was obtained. (2). Preparation of additive composition liquid: Shrimp extract 1,000
For each ml, each component was individually prepared by the following steps. . 453 ml of purified water and 99% ethyl alcohol were prepared. Only purified water was heated in hot water. . Put 7.3 g of tocophenol acetate in a container,
Ethyl alcohol (250 ml) was added, and the mixture was dissolved in a water bath at 70 ° C. Then, 7 g of germ oil was added. . 10.3 g of horse oil was put in a container, 247 ml of 99% ethyl alcohol was added, and the mixture was dissolved in a 70 ° C water bath. . 100 ml of heated purified water was put in a container, 2.3 g of sodium pantothenate and 2.3 g of nicotinamide were added, and the mixture was stirred. . 120 ml of heated purified water was put in a container, 7.7 g of ascorbic acid and 1 g of glycolic acid were added and stirred. . 70 ml of purified water and 99% ethyl alcohol 5 in a container
0 ml was added, and 0.8 g of biotin was added. The mixture was immersed in water at 70 ° C. and dissolved until it became transparent. . Put warm purified water 50ml, it was added to the kettle and stirred added vitamin _{B 6} of 1g. . 113 ml of heated purified water was put in a container, and 15.4 g of sodium chloride was added and stirred. . Put the solution in the container, add the solution to this,
The remainder was added in this order to obtain a mixture. The mixture was added to make up to 1,000 ml. 1,000ml
Was aged for 2 weeks. (3). Preparation of antiallergic composition liquid: The shrimp extract of (1) was diluted twice with purified water and added to the additive composition liquid of (2). The shrimp extract and the additive composition solution were mixed at a ratio of 1: 1. The shrimp extract had a ratio of 15% by volume (1,000%).
(150 ml per ml).

[0018]

COMPARATIVE EXAMPLE 1 A composition liquid having the same composition as in Example 1 was prepared in the same manner as in Example 1 except that only the shrimp extract was used.

[0019]

[Trial Example 1] The compositions of Example 1 and Control Example 1 were directly applied twice a day to the affected part of atopic dermatitis. Investigators are 4 each
Of the 0 patients, 20 of each were patients within 1 to 5 years of onset of atopic symptoms (medical history group A), and the remaining 20 were 6 to 15 years (medical history group B). The study period was up to 6 months. Table 1 shows the results.

[0020]

[Table 1]

[0021]

Embodiment 2 (1). Preparation of Ebine extract: An Ebine extract was obtained in the same manner as in Example 1 except that only the flower of the odorant was used as a raw material. (2). Preparation of additive composition solution: This flower shrimp extract 1,
For 000 ml, the following components were individually prepared in the same manner as in Example 1. . 900 ml of purified water 100 ml of 99% ethyl alcohol Germ oil 4.0 g Tocopherol acetate 8.5 g 99% ethyl alcohol 50.0 ml. Horse oil 6.0 g 99% ethyl alcohol 50.0 ml. Sodium pantothenate 2.5 g Nicotinamide 1.8 g Purified water 400.0 ml. Ascorbic acid 11.4 g Glycolic acid 1.0 g Purified water 400.0 ml. Vitamin B6 1.0 g Purified water 100.0 ml. The solution was put in a container, and the rest was added in this order to obtain a mixed solution. Add this mixture to 1,000
ml. 1,000 ml of the mixture was aged for 2 weeks. (3). Preparation of anti-allergic composition solution: (1) the flower shrimp extract solution and the additive composition solution of (2) are mixed at a ratio of 1: 2, and the ratio of the flower shrimp extract solution in the mixture is 7% by volume ( 1,
(70 ml in 000 ml). The obtained lotion was made from only ebine flowers. The lotion was applied to the hands and faces of 40 test subjects (female only) once every morning and evening for 6 months. As a result, Trial Example 1
Almost the same anti-allergic effect was obtained. In addition, there was no bulkiness on the skin, the skin was moist and shiny, the fragrance was good, and it was suitable as an antiallergic cosmetic.

[0022]

[Safety test] As a test on the safety of Ebine whole plant extract, it is included in the guidelines on drug toxicity test method (Revision of Single and Repeated Dose Toxicity Test Guideline for Drug Shinyaku No. 88, August 10, 1993). Based on the above, the extract of Ebine whole plant was orally administered once to male and female rats. This test was carried out in accordance with Yakuhin 313, March 31, 1982, “Standards for Conducting Safety Tests for Drugs” and its revised standards. The test method and results are as follows. (1). Test substance: Ebine whole plant extract that has been stable for more than one year after production. (2). Control substance: water for injection (Otsuka Pharmaceutical Co., Ltd.). (3). Animals used: Crj: CD (SD) male and female rats (SPF). Fourteen-week old males and females fourteen. Male weight 77-8
6 g, female 68-77 g. (4). Administration method: The above-mentioned whole plant extract of Ebine was forcibly administered orally to rats using a syringe. The dose was calculated at 2 ml / g based on the body weight on the day of administration. The administration was performed once a day at about 10 am and continued for 14 days. (5). Observation and inspection methods and results: The general condition was observed before and after the administration on the day of administration, and once a day from the next day. As shown in Table 2, no abnormality was observed in any of the male and female groups. . Body weight measurement: Body weight was measured on the day of administration and 1 day after administration, 3 days,
Measurements were taken on days 7, 10, and 14. As a result, as shown in Tables 3 and 4, both male and female groups showed almost the same transition as the control group, and no significant difference was observed in the body weight. In the significance test, the average value and the standard deviation are calculated in each group, and after confirming the equivalence of the variance by the P test, if the variances are equal,
Using the Student's t test, the test was performed between the control group and the test substance administration group. The significance level is less than 5% (p <
0.05). . Necropsy: At the end of the observation, all the animals were killed by exsanguination from the abdominal aorta under ether anesthesia under ether anesthesia. Necropsy was performed. As shown in Table 5, no abnormalities were observed in any of the male and female groups. As a result, 2, which is usually used as the upper limit of the safety test,
Even at 000 g / kg, no mortality was observed in both sexes, and no effect was observed in the body weight change or necropsy due to the administration of Ebine whole plant extract. Therefore, the Ebine extract is safe without toxicity. It is estimated to be.

[0023]

[Table 2]

[0024]

[Table 3]

[0025]

[Table 4] Note: TT in Tables 3 and 4 = Analysis of
Student's-test

[0026]

[Table 5]

[0027]

[Temporary irritation test on human skin] As a test on the safety of the extract of the whole plant extract of Ebine, a temporary irritation test on human skin using a closed batch was carried out as follows. (1). Test substance: Ebine whole plant extract (containing 8.8%). API, unadjusted, stored at room temperature. (2). Control substance: bandage for batch test (manufactured by River Tape Co., Ltd.) circular fabric part (blank) (3). Test system: human skin (4). Test method: For a total of 20 male and female subjects (including 12 males and 8 females), 0.1 ml of test substance (Ebine whole plant extract) was adhered to the upper arm skin surface, and a human batch was placed thereon. It was fixed with a test plaster (manufactured by River Tape Co., Ltd.). Further, as a blank control, a circular bandage of a bandage for a batch test was adhered to the skin surface in parallel with the test substance. After 48 hours, the bandage was removed, and the skin symptoms of the test substance and the control loading area were visually observed and evaluated. Regarding the skin findings of the test substance-loaded part, the presence or absence of irritation symptoms (erythema, edema, chickenpox) was confirmed, and judged according to the criteria of the Japan Batch Test Study Group. (5). Test results: The results of the 48-hour closed batch test of the test substance on human skin showed that no irritative reaction was observed immediately after the bandage was removed. Therefore, the test substance is evaluated as non-irritant.

[0029]

[Table 6]

[0030]

EFFECTS OF THE INVENTION According to the composition for external use on skin comprising the shrimp extract according to the present invention as an active ingredient, and because it has no toxicity,
It can be safely used as a topical medicine, cosmetic, or bath agent for a long time at home. Especially. It has a remarkable effect in the treatment of allergic diseases such as redness, eczema, hives, edema, swelling, and especially atopic dermatitis. In addition to this,
It has skin care effects such as improving rough skin, roughening, texture of skin, giving skin moisture and luster, and preventing skin aging.

──────────────────────────────────────────────────続 き Continued on the front page (51) Int.Cl. ⁶ Identification code FI A61K 31/19 A61K 31/19 31/355 ABF 31/355 ABF 31/375 31/375 31/415 31/415 31/44 31 / 44 31/455 31/455 33/14 33/14

Claims (3)

[Claims] 1. An antiallergic skin external composition comprising, as an active ingredient, an extract from at least one species of Ebine belonging to the genus Ebine of the orchid family. 2. The antiallergic external skin composition according to claim 1, further comprising vitamins, animal and vegetable oils, glycolic acid, and sodium chloride in addition to the shrimp extract. 3. The method according to claim 1, wherein the vitamins are sodium pantothenate,
Nicotinamide, tocopherol acetate, ascorbic acid, biotin, a vitamin B _6, anti-allergic skin external composition according to claim 2, wherein the animal or vegetable oil is germ oil and horse oil.