JPH04217906A - Skin external preparations - Google Patents

Abstract

(57) [Summary] This bulletin contains application data before electronic filing, so abstract data is not recorded.

Description

[Detailed description of the invention]

0001

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a skin preparation for external use. More specifically, the present invention relates to an external skin preparation containing tetrahydroabietate and/or a rosin hydrogenated salt. In other words, the present invention provides pharmaceuticals, quasi-drugs, and
Related to external skin preparations such as cosmetics.

0002

[Prior art] Acne (commonly known as Acne vulgaris)
vulgaris) is generally known to be caused by increased sebum secretion, bacterial infection, etc. In other words, comedones formed due to accumulation of sebum become infected with bacteria, causing inflammation of the hair follicles, resulting in pus or large lumps.

[0003] Conventionally, Propionibacterium acnes, a Gram-positive anaerobic bacterium considered to be the causative agent of acne, has been obtained by extracting natural plant components.
) Piciferic acid, berperine chloride, etc. are known to exhibit effective antibacterial activity.

0004

Problems with the Prior Art However, although the above-mentioned piciferic acid and berperine chloride have been recognized to have some effect on acne, the effect is not necessarily satisfactory.

Purpose of the Invention In view of the above-mentioned circumstances, the present inventors have conducted extensive research with the aim of developing a skin external preparation that is effective in suppressing acne. Tetrahydroabietate obtained by hydrogenating acid and/or rosin and/or salt of hydrogenated rosin are extremely safe and stable, and have extremely strong antibacterial properties against Propionibacterium acnes. admitted to having sex. No reports have been found regarding the antibacterial properties of tetrahydroabietate and/or rosin hydrogenated salts. The present inventors have completed the present invention based on the above findings.

[0006]

[Means for Solving the Problems] That is, the present invention provides an external skin preparation characterized by containing a tetrahydroabietate salt and/or a rosin hydrogenated salt.

[0007]

[Function] The function of the present invention will be explained below along with the detailed structure of the present invention.

The external skin preparation of the present invention contains a tetrahydroabietate salt or a rosin hydrogenated salt. Moreover, a salt of a tetrahydroabietate and a rosin hydrogenate may be used together.

As mentioned above, the present inventor has discovered that tetrahydroabietate or rosin hydrogenated salt exhibits strong antibacterial activity against acne-causing bacteria. This strong antibacterial power is
It was confirmed that the effect was maintained even in various external skin preparations. Therefore, the skin external preparation of the present invention exhibits excellent preventive and ameliorative effects on acne vulgaris. The external skin preparation of the present invention not only exhibits excellent preventive and ameliorative effects on acne vulgaris, but also has been found to have excellent preventive and ameliorative effects on various other bacterial skin diseases.

[0010] The content thereof is usually desirably 0.001 to 10% by weight as a dry residue in the total amount of the skin external preparation. Note that 0.1 to 3% by weight is appropriate as it exhibits strong antibacterial activity against acne-causing bacteria. If it is less than 0.001% by weight, the effects of the present invention cannot be obtained sufficiently, and
If it exceeds 10% by weight, it is disadvantageous in terms of formulation.

[0011] The tetrahydroabietate or rosin hydrogenated salt used in the present invention is preferably derived from plants (especially pinaceous plants).

Examples of the tetrahydroabietic acid salts and rosin hydrogenated salts used in the present invention include alkali metal salts such as sodium salts and potassium salts of tetrahydroabietic acid, monoethanolamine salts, diethanolamine salts, and triethanolamine salts. Examples include organic amine salts such as rosin hydrogenated salts, alkali metal salts such as sodium salts and potassium salts, organic amine salts such as monoethanolamine salts, diethanolamine salts, and triethanolamine salts, but sodium salts, potassium salts, Triethanolamine salts are preferred. One or more of these may be appropriately selected and used. In addition, the tetrahydroabietate salt and rosin hydrogenated salt are:
It can be manufactured by a known general method.

[0013] The tetrahydroabietic acid and rosin hydrogenated product used as starting materials in the present invention can be obtained by conventional methods. For example, it can be obtained by hydrogenating abietic acid or rosin at high temperature and high pressure in the presence of a noble metal catalyst.

[0014] In addition to the tetrahydroabietate and/or rosin hydrogenated salt, the external skin preparation of the present invention contains oil, water, etc. as a base for the external skin preparation, depending on the type of the external skin preparation. In addition, if necessary, surfactants, humectants, lower alcohols, thickeners,
Conventional ingredients used in external skin preparations such as fragrances, antioxidants, chelating agents, pigments, and preservatives and antifungal agents can be blended.

[0015] The dosage form of the skin external preparation of the present invention is arbitrary,
The preventive and ameliorating effect on bacterial skin diseases can be achieved regardless of the dosage form, such as a solution system, a solubilized system, a powder dispersion system, a water/oil two-layer system, or a water/oil/powder three-layer system. 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. For example, lotion, emulsion, cream, pack, hair tonic,
Examples include hair cream, shampoo, hair rinse, antiperspirant, water-based ointment, oil-based ointment, soap, and facial cleanser.

[0016]

EXAMPLES Next, the present invention will be explained in more detail with reference to Examples, but 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 %.

Test Example 1 (Growth-inhibiting effect on Gram-positive anaerobic bacteria) The growth-inhibiting effect of tetrahydroabietate on P. acnes, a Gram-positive anaerobic bacterium, was investigated in the following manner.

Using a GAM agar medium manufactured by Nissui as a medium, the pH of this medium was adjusted to 7.3±0.1, and then Propionibacterium acnes was prepared using sodium tetrahydroabietate and the sodium salt of rosin hydrogenate. The minimum inhibitory concentration (MIC) against a standard strain (ATCC 11827) was measured and evaluated.

As a comparative example, substances generally recognized to have antibacterial effects (biosol, berberine chloride,
The MIC of thioxolone, abietic acid) was also determined.

[0020] As a result, as shown in Table 1 below, it was confirmed that sodium tetrahydroabietate, the sodium salt of rosin hydrogenate, has much stronger antibacterial activity than other substances with antibacterial properties. .
Table 1────────────────────
────────── Substances with antibacterial properties MIC (ppm
)────────────────────────
────── Biosol

100 berberine chloride
100 thioxolone
50 abietic acid
20 Sodium tetrahydroabietate 5 Sodium salt of rosin hydrogenate 7────────────
────────────────────
Test Example 2 Using ABCM medium (manufactured by Eikensha) as an antibacterial active medium,
This medium was heated in an autoclave at 115°C for 15 minutes. A filter paper disk (8 mmφ) impregnated with 0.05 ml of 10% acetone solution of each sample was preliminarily soaked with Propionibacterium avidum (Propionibacterium avidum).
rium avidum, ATCC 25577) was allowed to adhere to the agar plate on which it had been inoculated and dispersed, and cultured anaerobically at 37°C for 3 days. The antibacterial activity was determined by measuring the diameter of the transparent zone (Propionibacterium avidum growth inhibition zone) formed around the filter paper at the end of the culture.

The above test results are shown in Table 2.

[0022]
Table 2────────────────────
──────────
Name of substance
Inhibition zone diameter (mm) Abietic acid

15 Sodium tetrahydroabietate 17──────────
──────────────────────
When similar tests were conducted on rosin hydrogenated product and sodium salt of rosin hydrogenated product as the substances shown in Table 2, the same results as shown in Table 2 were obtained.

Next, examples of the skin external preparation according to the present invention will be explained.

[0024] The external skin preparations in all Examples showed excellent preventive and ameliorative effects on various bacterial skin diseases such as acne vulgaris.

Example 1: Lotion Ingredients

% (1) Sodium tetrahydroabietate 0.2 (2
) glycerin
2.0
(3) 1,3 butylene glycol
2.0(4) Sodium citrate
0.1(5) Ethanol
10.0(6) Polyoxyethylene oleyl alcohol (EO15mol
Addition) 0.5 (7) Paraben

0.1 (8) Purified water

Remainder (manufacturing method) Above ingredients (1), (5
), (6), and (7) were mixed and dissolved at room temperature, and the components (2), (3), and (4) were also mixed and dissolved at room temperature.
And (8) was stirred and added to obtain a lotion.

Comparative Example 1: A lotion was obtained in the same manner as in Example 1, except that the component (1), sodium tetrahydroabietate, was omitted.

The antibacterial effects of the lotions of Example 1 and Comparative Example 1 against Propionibacterium acnes were measured as follows. After adjusting the pH to 7.3±0.1 using Nissui's GAM agar medium as a medium, the mixture was heated in an autoclave at 115° C. for 15 minutes to obtain a plate agar. Take 0.05 ml of the sample on a filter paper with a diameter of 8 mm, and prepare a sample of Propionibacterium acnes standard strain (ATCC118).
27) on a GAM agar medium inoculated and dispersed,
Anaerobic culture was carried out at 37° C. for 3 days, and 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 3.

[0028]
Table 3────────────────────
──────────
Example 1
Comparative Example 1 Growth prevention zone (mm)
14 9
──────────────────────────
───── As is clear from the results in Table 3, Example 1 containing sodium tetrahydroabietate has a larger anti-growth zone diameter than that of Comparative Example 1, indicating stronger antibacterial activity. .

Example 2: Cleansing foam Ingredients

% (1) Potassium tetrahydroabietate
0.5(2) Glycerin

18.0(3) Palmitic acid

10.0(4) Stearic acid
10.0
(5) Myristic acid
12.0(6) Lauric acid
4.0(7) Oleyl alcohol
1.0(8) Potassium hydroxide

6.0(9) Purified water

Residue (manufacturing method) Add component (8) to component (9) above and heat. Add component (2) to this and immediately heat to 70°C.
At the same time, heat and melt the components (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 neutralization reaction, and then cooled to obtain a cleansing foam.

Example 3: Acne cream ingredients

% (1) Sodium tetrahydroabietate
0.1(2) Photosensitive element 201

0.003 (3) 1,3 butylene glycol
5.0 (4) Beeswax

2.0(5) Setanol

4.0(6) Reduced lanolin
10.0(
7) Squalane
3
0.0(8) Paraben

0.2(9) Polyoxyethylene monosorbitan monolauric acid ester (3 mol of EO added)


2.0 (10) Purified water

Residue (manufacturing method) Component (3) was added to the above component (10) and heated and maintained at 70°C (aqueous phase). 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 4: Pack ingredients

% (1) Tetrahydroabietic acid triethanolamine 1.0 (2) Vinyl acetate resin emulsion
12.0(3) Polyvinyl alcohol
10.0 (4) Olive oil

3.0(5) Sorbit

5.0(6) Titanium oxide
15
．． 0(7) Ethanol
10.0 (8
) parabens
0.1 (9) Purified water
Residue (manufacturing method)
Mix component (5) with component (9) above, and 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 ingredients

% (1) Potassium tetrahydroabietate
0.2(2) Titanium oxide

13.0(3) Colloidal kaolin
25
．． 0(4) Talc
44.8
5 (5) Bengala
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) The above components (2) to (7) were mixed and pulverized to an average particle size of 1 to 5 μm using a pulverizer. This was transferred to a high-speed blender, and component (10) was added and mixed. Separately, the ingredients (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.

Example 6: Cream ingredients

% (1a) Sodium tetrahydroabietate
0.5(1b) Rosin Hydrogenate Sodium Salt
0.5(2) Liquid paraffin

10.0 (3) 1,3 butylene glycol

5.0 (4) Beeswax

2.0(5) Setanol

4.0 (6
) reduced lanolin

2.0(7) Squalane

30.0 (8) Paraben

0.2(9) Polyoxyethylene monosorbitan monolaurate (E
O3mol addition)

2.0(1
0) Purified water

Remainder (manufacturing method) Ingredient (1a) in the above ingredient (10),
(1b) and (3) were added and heated and kept at 70°C (
water phase). 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 7: Emulsion Ingredients

% (1) Potassium tetrahydroabietate 0
．． 5(2) Liquid paraffin
10
．． 0(3) Vaseline

4.0(4) Stearic acid

2.0(5) Setanol

1.0(6) Glycerin monostearate (self-emulsifying type) 2.0(7) Propylene glycol
7.0(8) Purified water

Residue (
9) Sodium hydroxide
0.4(
Manufacturing method) Components (1) to (6) were mixed, heated and dissolved, and then kept at 70°C (oil phase). Ingredients (7), (8) and (9)
) are mixed and dissolved, then heated and kept at 70°C (aqueous phase). The oil phase was added to the aqueous phase, and then uniformly emulsified using a homomixer and cooled to 30° C. while stirring well.

Example 8: Emulsion Ingredients

% (1) Sodium tetrahydroabietate
0.5 (2) Shortening oil
3.0 (3) Vaseline
96
．． 5 (Production method) The above components were mixed, heated to 80°C, and gradually cooled.

Example 9: Shampoo (1) Lauryl polyoxyethylene sulfate ester sodium salt (addition of 2 mol of EO) (30% aqueous solution)


30.0(2) Lauryl sulfate ester soda salt (30%
Aqueous solution) 15.0 (3) Ethylene glycol monostearate
3.0(4) Lauroylethanolamide
2.0(5) Lanolin derivatives

1.0(6) Protein derivative

3.0(7) Rosin hydrogenated sodium salt
0.5 (8) Purified water

46.5 (
9) Fragrance

Appropriate amount (10) dye

Appropriate amount (11) Preservatives, ultraviolet absorbers, sequestering agents
A suitable amount (manufacturing method) of purified water was heated, other ingredients were added thereto, dissolved, stirred well, and then cooled slowly.

Example 10 Antiperspirant - Stock solution formulation
%(1
) aluminum hydroxychloride
30.0% (2) Silicic anhydride

5.0% (3) Talc
1.
0% (4) Sodium tetrahydroabietate
1.0% (5) Isopropyl myristate ester 63.0% (6) Fragrance
Appropriate amount ・Filling prescription stock solution
10.0
%gas
90.
While stirring the isopropyl myristate ester, other components were gradually added to the 0% (manufacturing method) stock solution and uniformly dispersed using a homomixer. For filling, fill the can with the prescribed amount of undiluted solution,
This was done by filling the prescribed amount of gas after installing the valve.

[0038] In the above example, the case where tetrahydroabietate or rosin hydrogenated salt was contained alone was shown, but when both were contained together,
It showed a stronger antibacterial effect than when it was contained alone.

[0039]

Effects of the Invention The present invention provides an external skin preparation containing tetrahydroabietate and/or a rosin hydrogenated salt, which is extremely effective against various bacterial skin diseases such as acne vulgaris. It is possible to provide a skin external preparation that is effective and has excellent safety and stability.

Claims (1)

[Claims] 1. An external preparation for skin, comprising a tetrahydroabietate and/or a rosin hydrogenated salt.