JPS61215307A - External agent for skin - Google Patents

Abstract

PURPOSE:To provide the titled agent having remarkably improved antiinflammatory effect without causing side effects, by compounding glycyrrhezic acid and/or its derivative having anti-inflammatory effect with 4-t-butyl-4'-methoxybenzoylmethane. CONSTITUTION:(A) One or more compounds selected from glycyrrhezic acid which is a main component of KANZO (root of Glycyrrhiza glabra) used widely as a Chinese herb and/or its derivative (e.g. glycyrrhezic acid stearyl ester, 3-succinyloxyglycyrrhezic acid, etc.) is compounded together with (B) 4-t-butyl-4'- methoxybenzoylmethane of formula II to the objective external agent. The amount of the component A in the whole external agent is 0.001-5wt%, preferably 0.05-0.1wt%, and that of the component B is >=1/100pts.wt., preferably >=1pt.wt. per 1pt. of the compound A.

Description

DETAILED DESCRIPTION OF THE INVENTION [Industrial Application Field] The present invention provides an external skin preparation with excellent anti-inflammatory effects, more specifically, a skin preparation containing glycyrrhetinic acid and/or its derivatives.
The present invention relates to an external preparation for skin, characterized in that it contains one or more species and 4-tert-butyl-4'-methoxydibenzoylmethane.

[Conventional technology] Conventional 9 For inflammation such as sunburn and eczema, astringents such as calamine and vitamins such as vitamin C are used.

Antihistamines such as sulfadiazine, antibiotics such as bacitracin, corticosteroids such as fluocinolone acetonide, and azulene are used, but these drugs are not effective due to their relationship with other ingredients. I couldn't do it.

The safety and efficacy of topical applications are not always satisfactory.

On the other hand, glycyrrhetinic acid is a main component of licorice, which is known as a Chinese herbal medicine, and is known to have anti-inflammatory effects. However, its effect is mild and when used in external skin preparations expected to have anti-inflammatory effects, the effect could not be obtained unless it was incorporated in a high proportion.

[Problems to be Solved by the Invention] As a result of intensive research into whether there is a way to significantly enhance the anti-inflammatory effect of glycyrrhetinic acid and/or its derivatives, the present inventors found that The present invention was completed based on the discovery that this object can be achieved by blending 4-tert-butyl-4°-methoxydibenzoylmethane with one or more species.

[Means for solving the problem] That is, the present invention involves blending one or more types of glycyrrhetinic acid and/or its derivatives with 4-ter·,-butyl-4°-methoxydibenzoylmethane. It is a skin external preparation characterized by:

Hereinafter, the configuration of the present invention will be explained in detail.

Glycyrrhetinic acid used in the present invention is a main component of licorice widely used in Chinese medicine, and is a compound represented by the following structural formula.

Further, as derivatives of glycyrrhetinic acid, stearyl glycyrrhetinate, 3-succinyloxyglycyrrhetinic acid, and the like are famous.

The blending amount is 0.001 to 5% by weight of the total amount of the skin external preparation.
Preferably 0601 to 7% by weight, more preferably 0.05 to 0.1! i amount%.

Less than 0.001% by weight, glyderrettic acid and/or
The effect of 4-tert-butyl-4'-methoxydibenzoylmethane cannot be expected, and if the amount exceeds 5% by weight, there is no need to incorporate 4-tert-butyl-4'-methoxydibenzoylmethane.

4-tert-butyl-4°-methoxydibenzoylmethane used in the present invention is a compound having the structure, and is produced by the method shown in JP-A-55-66535. In addition, from Shibodan Co., Ltd., “Pulsol '17
It is sold under the product name 89J.

The amount incorporated into the skin external preparation is 1/100 times or more, preferably 1/10 times or more, and most preferably 1 times or more by weight of glycyrrhetinic acid and/or its derivatives.

If the amount is less than 1/100 times the amount, the effect of increasing the effect of glycyrrhetinic acid and/or its derivatives will be small and will not be sufficient. one or more glycyrrhetinic acid and/or its derivatives and 4-ter=,-butyl-4'
- Skin external preparation bases that can contain methoxydibenzoylmethane include commonly thought skin external preparation bases, such as solubilized systems, emulsified systems, powder systems, powder dispersion systems, water/oil based two-layer cosmetics, and water/oil systems. Any base material may be used, such as a 3-layer /oil/powder type cosmetic.

The skin external preparation of the present invention may optionally contain natural extracts such as animal and vegetable oils, ester oils, triglycerides, higher fatty acids, and higher alcohols, within a quantitative and qualitative range that does not impair the effects of the present invention. Hydrolic alcohols, other sugar derivatives, humectants such as pyrrolidone carboxylic acid, thickeners such as water-soluble polymer compounds and clay minerals, preservatives, surfactants, sequestering agents, ultraviolet absorbers, inorganic or
Organic powders, pigments, medicinal ingredients, dyes, fragrances, etc. can be added.

[Effects of the Invention] The skin external preparation of the present invention has the following advantages.

The anti-inflammatory effect of glycyrrhetinic acid and/or its derivatives can be significantly increased without side effects.

[Example] Next, the present invention will be roughly explained in detail using test examples and examples. Note that the present invention is not limited to this.

Test Example 1 A cream with the following formulation was used to evaluate its effectiveness in healing inflammation caused by sunburn on a panel of 50 people at the beach in summer.

A. Setanol 0.5% Vaseline 2. Q Squalane 7.0 Self-emulsifying glyceryl monostearate 2.5 Polyoxyethylene sorbitan monostearate (20E.O,) 1.54-tert-
Butyl-4'-methoxydibenzoylmethane
260 glycyrrhetinic acid
0-0.2B.

Glycerin 10.0 Veegum (
Montmorillonite) 5.0 Potassium hydroxide 0.3 Edetate trisodium salt 0°o2 water
Residue - Manufacturing method - Heat A (oil phase) and B (aqueous phase) to 70'C,
Completely dissolve. Add A to B and emulsify with an emulsifier.

The emulsion was cooled using a heat exchanger to obtain cream.

The results are shown in Table-1.

The evaluation of inflammation recovery is expressed by the following display.

One day later, more than 40 out of 50 patients had recovered.

0. One day later, more than 30 of the 50 people had recovered.

Δ One day later, more than 20 out of 50 patients recovered.

× One day later, less than 10 out of 50 patients had recovered.

A in the table indicates glycyrrhetinic acid B indicates 4-tert-butyl-4°-methoxydibenzoylmethane.

Example 1 Cream A, stearic acid 10.0% stearyl alcohol 4.0 Butyl stearate 8.0 Stearic acid monoglycerin ester 2,0 4-(1,1-dimethylethyl)-4"-methoxydibenzoylmethane 2 .0 Stearyl glycyrrhetinate 0.8 Fragrance 0.
4 Preservatives appropriate amount B, propylene glycol 1o. 0 glycerin
460 maltitol
1°0 Potassium hydroxide 0.4 Purified water Heat the remaining oil phase part of A and the water phase part of B to 70°C to completely dissolve them. Add phase A to phase B and emulsify with an emulsifier. The emulsion was cooled using a heat exchanger to obtain vanishing cream.

Example 2 Cream A, Setanol 4.0% Petrolatum 7°O Isopropyl myristate 8.0 Squalane 15.0 Stearic acid monoglycerol ester 2.2 POE (20) Sorbitan monostearate 2.8 4- (1,1 -dimethylethyl)-4'-methoxydibenzoylmethane 0.05 glycyrrhetinic acid
5.0 fragrance
O03 antioxidant Appropriate amount preservative
Appropriate amount B, glycerin
10.0 dipropylene glycol
5.0 Edetate trisodium salt 0. o1 Purified water A night cream was obtained according to the remainder of Example 1.

Example 3 Emulsion A, squalane 5.096 oleyl oleate 3.0 Wa:! Phosphorus 2.○ Sorbitan sesquioleate 0.8 Polyoxyethylene oleyl ether (20E, 02) 1.2 4-(1゜1-dimethylethyl)-4'-methoxydibenzoylmethane 1.53-succinyloxyglycyrrhetine Acid 0.5 Fragrance O03 Preservative
Appropriate amount B. 1゜3 Butylene Glycol 5,0 Ethanol
3゜0 carboxyvinylborrimer-0.2 Potassium hydroxide 0.1 Purified water
A milky lotion was obtained according to the rest of Example 1.

(Left below) Example 4 Foundation A, Cetanol 3.5% deodorized lanolin 4°0 jojoba oil
5.0 Vaseline
2.0 Squalane 6゜0 Stearic Acid Monoglycerin Esthe J 2.5 POE (60) Hydrogenated Castor Oil 1.5 POE (
20) Cetyl ether 1.04-(1,1-dimethylethyl)-4'-methoxydibenzoylmethane
10.0 Glycyrrhetinic acid 0,001 Preservatives Appropriate amount fragrance
0.3B, propylene glycol
10.0 Mixed powder 12.
O edetate trisodium salt 0゜5 purified water
One fathom of foundation was added according to the rest of Example 1.

Example 5 Soft lotion A6 ethanol 5.0% PO
E oleyl alcohol ether 2.02-ethylhexyl-P-dimethylaminobenzoate
06184-(1,1-dimethylethyl)-4
°-Methoxydibenzoylmethane 0.001 Glycyrrhetinic acid 0.1 Fragrance
0.05B, 1°3 butylene glycol 10. .

Glycerin 5.0 Edetate trisodium salt 0.01 Purified water
Adding the remaining alcoholic phase of A to the aqueous phase of B;
It was solubilized and a lotion was obtained.

Claims (1)

[Claims] An external preparation for skin, characterized in that it contains one or more glycyrrhetinic acid and/or its derivatives and 4-tert-butyl-4'-methoxydibenzoylmethane.