JPS63150208A - External drug for skin - Google Patents

Abstract

PURPOSE:To obtain an external drug for skin effective in suppressing acne, dandruff, itchiness, etc., by using an extract of a plant belonging to Thujopsis genus, Thuja genus or Juniperus genus of Cupressaceae family, as an active component. CONSTITUTION:A plant belonging to Thujopsis genus (e.g. Thujopsis dolabrata, etc.), Thuja genus (e.g. Thuja standishii) or Juniperus genus (e.g. Juniperus rigida, Juniperus conferta, Juniperus chinensis, Juniperus chinensis var. procumbens, etc.) of Cupressaceae family is extracted with a solvent such as ethanol, propylene glycol, water, hexane, etc., and the extract (solution as extracted or concentrated extract produced by distilling out the solvent) is used as a component of the objective external agent for skin, e.g. drug, quasi- drug, cosmetic, etc. It is preferable to use the extract in an amount of 0.1-3wt% in terms of dried residue in the whole external agent, because the agent obtained thereby exhibits fungicidal activity against fungi causing acne, dandruff or itchiness.

Description

[Detailed Description of the Invention] [Industrial Application Field] The present invention relates to skin products such as pharmaceuticals, quasi-drugs, and cosmetics containing extracts of plants belonging to the Cupressaceae family, the genus Asunaro, the genus Arborvitae, or the genus Juniper. Regarding external preparations.

[Conventional technology] Plants of the cypress family, such as ship hiba, asunaro, and arborvitae, are
It is a plant that is relatively resistant to environmental pollution.

Biciferic acid, 0
- Contains diterpenes such as methylbisifuniphosphate, and these substances were found to have antibacterial activity (e.g., "Seminar on Fragrances, Terpenes, and Essential Oil Chemistry", 1985 Lecture Abstracts, Antibacterial Activity of Shiphiba) Ingredients: Koji Kobayashi, Chikao Nishino). However, its antibacterial activity is limited to Durham-negative enterobacteria (Proteus vulgaris).
It has only been reported that it belongs to bacteria such as U1gari゛S), Gram-positive Staphylococcus aureus, and Bacillus subtilis, and there have been no reports on the causative bacteria of acne, dandruff, itching, etc.

Furthermore, no reports of this species have been found in the other genera Asunaro, Arborvitae, and Juniper within the Cupressaceae family.

[Problems to be solved by the invention] In view of the above circumstances, the present inventors have solved acne, dandruff,
In the process of conducting research with the aim of developing ingredients that are effective in suppressing itchy skin, we have conducted extensive research into the antibacterial activity and body odor suppressing effects of plants and their extracts. Alternatively, extracts of plants belonging to the genus Juniperina can be used to treat acne (acne vulgaris).
Propionibacterium acnes (Prop.
ionibacterium acnes) and the scalp resident yeast Viteirosporum opal (Pityrosporum oval), which is thought to be the cause of scalp dandruff and itching.
It has been found that it exhibits effective antibacterial activity against e). It has also been confirmed that the substance exhibiting this antibacterial activity is completely different from the biciferic acid contained in the above-mentioned shipshiba. These matters have not been suggested in any previous reports, and were discovered for the first time by the present inventors.Based on these findings, the present inventors have completed the present invention. .

That is, the present invention provides an external skin preparation containing an extract of a plant belonging to the Cupressaceae family, the genus Asunaro, the genus Riabe, or the genus Juniper.

The configuration of the present invention will be explained in detail below.

The plants used in the present invention include Cupressaceae, Asunaro genus, Arborvitae genus,
Or a plant belonging to the Juniper genus, specifically, Asunaro, Ate, or Hinoki Asunaro of the Asuna genus, Arborvitae of the Arborvitae genus, Junniper juniper of the Juniper genus, Japanese juniper, Japanese juniper, Japanese juniper, or Myanthia juniper.

In the present invention, these plants are used in the form of extracts. In producing the extract, conventional methods for plant extracts are used. That is, first, leaves or twigs of the above-mentioned plants are collected and crushed as is or after drying to obtain a crushed product. Next, the pulverized product is extracted using a solvent described below. Although the ratio of extracted contents of leaves changes somewhat depending on the time of collection, leaves from any time of collection can be used. There are no restrictions on the use of the extraction solvent as long as it is a solvent commonly used for plant extraction.

However, depending on the combination of solvents, the ratio of extracted contents may change or the degree of coloring may vary, so ethanol, propylene gelcol, water, hexane, etc. are preferable. Extraction conditions are not particularly limited as long as they are conditions commonly used for plant extraction. However, since the degree of pulverization of the leaves affects the extraction time and extraction efficiency, it is preferable to use a comb that can pass particles with a diameter of 2 mm and use the pulverized material that has passed through the comb. Although the ratio of extracted contents changes depending on the extraction temperature, there is no particular restriction. However, if you also want to obtain aroma components, it is preferable to avoid it because there is a concern that it will volatilize at high temperatures.

There is no particular restriction on the amount of extraction solvent, but for extraction efficiency and ease of post-processing such as filtration, it is recommended to use 1 part or 1 part of extraction solvent for 1 part of leaves.
0 parts is most desirable. It may be used as a substance or powder.

The skin external preparation of the present invention may contain any amount of the extract obtained by the above-mentioned method, etc., but it usually contains 0.01 to 10% by weight as a dry residue in the total amount of the skin external preparation. It is desirable that the content is 0.1-3% by weight, more preferably 0.1-3% by weight.
It is suitable because it shows antibacterial activity against bacteria that cause acne, dandruff, and itching.

In addition to the above-mentioned extracts, the external skin preparation of the present invention may contain oil, water, etc. as a base for the external skin preparation, depending on the type of the external skin preparation. Conventional ingredients used in external skin preparations such as agents, humectants, lower alcohols, thickeners, fragrances, antioxidants, chelating agents, pigments, and antifungal agents can be blended.

The dosage form of the skin external preparation of the present invention is arbitrary, and any dosage form may be used, including a solution type, solubilized type, emulsion type, powder dispersion type, water-oil two-layer type, water-oil and powder three-layer type. I don't mind.

Further, the use of the skin external preparation of the present invention is arbitrary, and it is widely used in pharmaceuticals, quasi-drugs, cosmetics, toiletry products, etc. Examples include lotions, emulsions, creams, packs, hair tonics, hair creams, shampoos, hair rinses, aqueous ointments, oil-based ointments, and the like.

[Example] Next, the present invention will be explained in more detail with reference to Examples.
It goes without saying that the scope of the present invention is not limited to these examples. In addition, in the following examples, the blending amount is shown in weight %.

Preparation Example 1 Leaves and twigs of Asunaro are crushed in a speed mill, and the diameter is 2
The powder was passed through a comb that could pass through millimeter particles, and only the crushed material that passed through the core was collected. Next, 5 parts of ethanol was added to 1 part of the pulverized product, and the mixture was extracted for 4 weeks indoors at 25 to 35°C and filtered through a glass filter to obtain a brown extract.

Preparation Example 2 Ate leaves and twigs were ground in a speed mill to a diameter of 2 mm.
Only the crushed material that passed through the core was collected by passing it through a comb that could pass through the particles. Next, 3 parts of propylene glycol was added to 1 part of the pulverized product, and the mixture was extracted for 3 weeks indoors at 20 to 40°C and filtered through a glass filter to obtain a green extract.

Preparation Example 3 After air-drying Arborvitae leaves and twigs, they were ground in a speed mill, passed through a comb that could pass particles with a diameter of 2+ nm, and only the ground material that had passed through the core was collected. Next, 5 parts of n-hexane was added to 1 part of the pulverized material, and the mixture was heated in a room at 20 to 40°C for 4 hours.
The extract was extracted for a week and filtered through a glass filter to obtain a green extract. N-hexane was distilled off from the extract to obtain a dark green viscous substance.

Next, the antibacterial activity and deodorizing effect of the plant extract obtained as described above will be described below.

Test Example 1 ABCM medium (Eiken) was used as an antibacterial activity medium, and heat treated in an autoclave at 115°C for 15 minutes.

Soak 0.05 ml of 10% acetone solution of each sample into a mouthpiece disc (8 mmφ), and preliminarily prepare Propionibacterium avidum
avidum.

ATCC2557? ) was inoculated and dispersed on an agar plate and cultured anaerobically at 37°C for 3 days. At the end of the culture, the diameter of the pellucid zone (Propionibacterium avidum growth inhibition zone) formed around the opening was measured, and the antibacterial activity was determined.

The results are shown in Table 1.

Table 1 Extract of Preparation Example 1 18 Extract of Preparation Example 2 20 Extract of Preparation Example 3 28 Example 1: Lotion Ichisei Iri Tomoko --%- (1) Asunaro extract (Preparation Example 1) 0
．． 5(2) Glycerol 2.
0(3) 1,3 butylene gellicol
2.0(4) Sodium citrate
0.1 (5) Ethanol 1
0.0(6) Polyoxyethylene oleyl alcohol 0.5(7) Paraben 0.1(8) Purified water
Residue (manufacturing method) Component (2) obtained by mixing and dissolving the above components (1), (5), (6), and (7) at room temperature, and also mixing and dissolving at room temperature.
, (3), (4) and (8) were added with stirring to obtain a lotion.

Comparative Example 1: Lotion A lotion was obtained in the same manner as in Example 1 except that the Asunaro extract as component (1) was removed.

The antibacterial effects of the lotions of Example 1 and Comparative Example 1 against Propionibacterium acnes were measured as follows.

Nissui's GAM agar medium was used as the medium, pH 7.3±
After adjusting the temperature to 0.1, it was heated in an autoclave at 115°C for 15 minutes to obtain agar plate. Sample 0.05m in diameter 8m
M filter paper and inoculated and dispersed with Propionibacterium acnes standard strain (ATCC11827) in advance.
The samples were placed on AM agar and cultured anaerobically at 37°C for 3 days. At the end of the culture, the diameter of the transparent zone (propionibacterium acnes growth prevention zone) formed around the filter paper was measured to determine the antibacterial activity.

The results are shown in Table 2.

Growth prevention zone (mm) 16 9 As is clear from the results in Table 2, Example 1 containing Asunaro extract has a larger growth prevention zone diameter than that of Comparative Example 1, indicating that it has stronger antibacterial activity. There is.

(Left below) Example 2: Cleansing foam formulation 1 minute (1) Ate extract (Preparation example 2) 0
．． 5(2) Glycerin 18
．． 0(3) Palmitic acid 10
．． 0(4) Stearic acid 10
．． 0 (5) myristic acid 1
2.0(6) Lauric acid 4
．． 0(7) Oleyl alcohol 1.
0(8) Potassium hydroxide 6.0
(9) Purified water Remaining water (manufacturing method) Component (8) is added to component (9) above and heated. Component (2) is added to this and immediately heated to 70°C. Ingredients (1) (3) (4)
(5) (6) and (7) were gradually added while stirring. After the addition, the temperature was kept at about <70°C for a while to complete the saponification reaction and obtain a cleansing foam.

Example 3: Acne Cream Ikki Kinpiko--%- (1) Arborvitae extract (Preparation Example 3) 0.1
(2) Photosensitive element 201 0.0
03(3)1.3 Butylene glycol
5.0 (4) Beeswax 2
．． 0(5) Setanol 4
．． 0(6) Reduced lanolin 10
．． 0(7) Squalane 30
．． 0(8) Paraben 0.
2 (9) Polyoxyethylene monosorbitan monolauric acid ester 2.0 (10) Purified water Remainder (manufacturing method) Add component (3) to the above component (10) and heat to 70°C
(aqueous phase). Other components were mixed and heated to 70° C. (oil phase). This oil phase is added to the aqueous phase for preliminary emulsification, uniformly emulsified with a homomixer, and O/
I got W cream.

Example 4: Pack -Distribution U friend-j (1) Asunaro extract (Preparation Example 1) f.

(2) Vinyl acetate resin emulsion 12.0 (
3) Polyvinyl alcohol 10.0 (
4) Olive oil 3.0 (5)
) Sorvit 5.0 (6)
Titanium oxide 15.0 (7)
Ethanol 10.0 (8)
Paraben 0.1 (9) Purified water Residue (manufacturing method) Mix component (5) with component (9) above, add component (6)
) and (2) were added, and component (3) moistened with a portion of component (7) was further added, and the mixture was heated to 70° C. to dissolve. Next, components (1) and (8) were added to the remaining component (7) and mixed, and finally component (4) was added and cooled to obtain a pack.

Example 5: Foundation - "Healing Flames - 11t" (1) Ate Extract (Preparation Example 2) 0.
2(2) Titanium oxide 13.
0(3) Colloidal Kaolin 25.0
(4) Talc 44.7
(5) Bengal 0.8 (
6) Yellow iron oxide 2.5 (7)
Black iron oxide 0.1 (8) Liquid paraffin 8.0 (9) Sorbitan sesquioleate 3.5 (10) Glycerin 2.0 (11) Paraben 0.2 (Production method) Above components (5) to (7) were mixed and pulverized through a pulverizer to an average particle size of 1 to 5 μm. This was transferred to a high-speed blender, and component (10) was added and mixed. Separately, component (1),
(8), (9) and (11) were mixed and homogenized, and the resulting mixture was added to the above mixture and further mixed uniformly.

After processing this in a crusher and passing it through a sieve to equalize the particle size,
Compression molding was performed to obtain a cake-shaped foundation.

: : Yeast Pityrosvorum Opal (Pi
tyrosporu +++ ovale) decomposes lipids in the scalp and produces fatty acids. This fatty acid causes erythema and itching on the scalp. Furthermore, as an ecological defense reaction against this, skin turnover begins to accelerate, resulting in exfoliation and accumulation of the epidermal cornified layer, resulting in dandruff. Based on these facts, dandruff and itching can be prevented by blocking or combining the activity of Vityrosvorum opal. The antibacterial activity of arborvitae extract against Pityrosporum opal was investigated.

(1) Arborvitae extract (preparation example 1) 5 (2) Acetone remaining amount (1
) was added and dissolved in (2) to obtain a 5-cup arborvitae extract acetone solution. This solution was diluted with acetone to obtain Nori abe extract acetone solutions of various concentrations up to C 0,625X.

°° Yumi's;'- medium (potato extract 2%, yeast extract IX, peptone I
3 volumes of L olive oil and 2 volumes of agar) were placed in a 100-shelf flask and heat-treated at 121°C for 15 minutes in an autoclave. Furthermore, 11 nt of an acetone solution of the test solution (i) of each adjusted concentration was added to prepare a flat plate. Pityrosvorum opal standard strain (IFo 0656) was inoculated into this, and 3
Static culture was carried out at 7°C for 48 hours, and the presence or absence of bacterial cell growth was observed at the end of the culture to determine the minimum concentration that could inhibit bacterial cell growth. This concentration was designated as old C.

In the above test, 1χ zinc pyrithione or 1χ hinokitiol was used instead of arborvitae extract, and a control test solution was obtained in the same manner except for MIC.
I asked for

The results are shown in Table 3.

1-2-” Arborvitae extract 200 Control example Zinc pyrithione 50 As is clear from the results in Table 3, arborvitae extract is inferior to the anti-dandruff drugs commonly used in anti-dandruff drugs at present, but it is still effective as a plant. As an extract, it is found to be a strong anti-dandruff agent.

Example 6: Hair Tonic Shikin Saratachi X (1) Asunaro extract (Preparation Example 1) 2.0
(2) Assemble style extract 0.5 (3
) Salicylic acid 0.3 (4) Ethinyl estradiol 0.0005 (5) Pantothenyl ethyl ether 0.1 (6) Ethanol 40.0 (7) Purified water
Residue (manufacturing method) Add (1), (3), (4) and (5) to the above component (6), mix and dissolve at room temperature, and add components (7) and (2) that were also mixed and dissolved at room temperature. A hair tonic was obtained by stirring and adding the mixture to (6) which had been previously @Med.

Comparative Example 2: Hair Tonic A hair tonic was prepared in the same manner as in Example 6, except that the Asunaro extract as component (1) was not blended in, and used in the following evaluation test.

Out of 30 people who had dandruff or were prone to dandruff, 10 people who had a lot of dandruff were selected by visual judgment to serve as test panels. These 10 people were divided into two groups of 5 people each, group A and group B. Group A used the hair tonic of Example 6, and group B used the hair tonic of Comparative Example 2. The conditions of use and evaluation were as follows.

In other words, both groups A and B repeatedly washed their hair every 3 days with a shampoo that does not contain drugs such as anti-dandruff agents, and visually judged the amount of dandruff just before washing their hair. However, there were no obvious differences between groups A and B or between individual panels. Therefore, starting from the next day, each group applied their respective hair tonics to their scalps once a day, and repeated the same cycle of hair washing and visual evaluation every three days. The results are shown in Table 4.

(Left below) 1 Pi Table 4 Example 7: Shampoo y Gold Difference (1) Ate extract (Preparation example 2) 2.0
(2) POE-alkyl sulfate 10.
0(3) Lauric acid jetanolamide 10.0(
4) Propylene glycol 2.0 (5)
Paraben 0.2 (6) Purified water Residue (manufacturing method) Ingredients (2) and (3) above were dissolved by heating at 60℃ (
6) was added and further mixed and dissolved (1), (4) and (
5) was added with stirring to obtain Shi and Yanbu.

Example 8: Chrytum-L degree-1 (1) Ate extract (Preparation example 2) 1.
0(2) Liquid paraffin 10.0
(3) 1,3 butylene glycol
5.0 (4) Mitsumira 2.
0(5) Setanol 4,0
(6) Reduced lanolin 2.0
(7) Squalane 30.0
(8) Paraben 0.2 (
9) Polyoxyethylene monosorbitan monolaurate 2.0 (10) Purified water Residue (manufacturing method) Components (1) and (3) were added to the above component (10) and heated and kept at 70°C (water phase Department). Other components were mixed and heated to 70° C. (oil phase). This oil phase was added to the aqueous phase for preliminary emulsification, and the mixture was uniformly emulsified using a homomixer to obtain a 0/W cream.

Example 9: Emulsion-n gold degree--%- (1) Arborvitae extract (Preparation Example 3) 0.
5(2) Liquid paraffin 10.
0(3) Vaseline 4.0
(4) Stearic acid 2.0 (
5) Setanol 1.0 (6
) Glyceryl monostearate (self-emulsifying type) 2.0 (7) Propylene glycol 7.0 (
8) Purified water Remainder (9) Sodium hydroxide 0.4 (manufacturing method) Mix (1) or 6) and maintain at 70°C after heating and dissolving (oil phase). After mixing and dissolving (7) or 9), heat 7
Keep at 0°C (aqueous phase). The oil phase is added to the aqueous phase, then uniformly emulsified using a homomixer, and cooled to 30°C while stirring well.

Example 10: Oil-based ointment-n-Kuuridate-1 (1) Arborvitae extract (Preparation Example 31 0.5 (
2) Shortening oil 3.0 (3
) Vaseline 96.5 (Production method) The above ingredients are mixed, heated to 80°C, and gradually cooled.

Claims (1)

[Claims] (1) A skin external preparation containing an extract of a plant belonging to the genus Asunaro, arborvitae, or juniper in the family Cupressaceae.