JP2009155222A - Pimple improving agent and pimple improving skin external preparation - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a pimple improving agent which is mild for the skin to fully achieve the treatment of pimples without requiring combined use of a drug such as an antibacterial agent for propionibacterium acnes. <P>SOLUTION: The pimple improving agent comprises (a) a solvent extract of Bergenia ciliata Sternb. , (b) an ascorbic acid derivative, and (c) a salt of glycyrrhizinic acid. The skin external preparation for improving pimples comprises this pimple improving agent. <P>COPYRIGHT: (C)2009,JPO&INPIT

Description

  The present invention relates to an acne improving agent and an external skin preparation for improving acne, and more particularly to an acne improving agent for preventing and preventing skin diseases such as acne and an external skin preparation for improving acne containing the same.

  Acne is a skin disease that occurs mainly in puberty. Its official name is acne vulgaris, clinically defined as "chronic inflammatory changes that occur in the pores of the follicular sebaceous system" Yes. Although the pathogenesis is still unclear, it is generally considered to be a skin disease in which various factors are intricately intertwined while excessive sebum secretion, hair follicle keratinization, and bacteria in the hair follicle play an important role. ing. Therefore, as an external preparation for acne treatment, creams and ointments containing a sebum secretion inhibiting component, a keratin dissolving component, an anti-inflammatory component and / or an antibacterial substance are generally used in accordance with the above factors.

  However, various drawbacks have been reported in the existing acne treatments containing the various components described above. For example, a female hormone that is a sebum secretion inhibitory component suppresses epidermal growth and decreases sebum secretion, but the side effects caused by this type of hormone are not particularly favorable for adolescent men and women. Also, herbal medicines such as pyridoxine hydrochloride, peony extract, and burdock extract, which have sebum-inhibiting action, do not show sufficient sebum-inhibiting effect even when used alone in creams or ointments. There wasn't. In addition, sulfur compounds such as sulfur and selenium disulfide, which are representative examples of keratolytic components, do not have side effects such as the above-mentioned female hormones, but they may cause skin irritation and skin roughness when used continuously. Many.

On the other hand, it is known that the Fuyu Begonia extract of the herbal medicine used in the present invention is used as an anti-aging agent or a whitening agent (see Patent Documents 1 and 2). In recent years, an external skin preparation for acne in combination with a lipase inhibitor or an antibacterial agent for acne is known (see Patent Document 3).
However, this acne external preparation for skin is effective when used in combination with drugs such as lipase inhibitors and antibacterial antibacterial agents, and combined use with such drugs is essential.

JP 11-335229 A JP 2004-315491 A JP 2006-241059 A

  In view of such circumstances, an object of the present invention is to provide an acne improving agent and a skin external preparation for improving acne that have no hormone-like side effects, are mild to the skin, and have an excellent acne treatment effect. .

  In light of the above circumstances, the present inventors have conducted extensive research, and as a result, if combined with a specific component in the Fuyu Begonia extract, it has no hormone-like side effects, is mild to the skin, and It has been found that an acne ameliorating agent can be obtained in which the purpose of acne treatment can be satisfactorily achieved without the need to combine drugs such as antibacterial antibacterial agents, and the present invention has been completed.

  The present invention is an acne improver characterized by comprising (a) a solvent extract of Bergenia ciliata Sternb., (B) an ascorbic acid derivative, and (c) a glycyrrhizinate.

  The present invention relates to a skin external preparation for improving acne, which comprises (a) a solvent extract of Bergenia ciliata Sternb., (B) an ascorbic acid derivative, and (c) glycyrrhizinate. is there.

The acne-improving agent of the present invention has an effect of preventing and improving acne formation, and is excellent in safety.
According to the external preparation for acne improvement of the present invention, there is no side effect like a hormone, it is mild to the skin, and it is not necessary to combine drugs such as antibacterial antibacterial agents, and the purpose of acne treatment is Well achieved.

The best mode of the present invention will be described below.
Fuebegonia (Bergenia ciliata Sternb.) Used in the present invention is an evergreen perennial belonging to the genus Bergenia, which is distributed in cashmere, Bhutan, Nepal, India, and the like.

  The acne-improving agent of the present invention can be obtained by soaking or heating and refluxing any of the above-mentioned plant leaves, stems, flowers, roots, or a mixture thereof, followed by filtration and concentration. The extraction solvent can be arbitrarily used as long as it is a solvent that is usually used for extraction, for example, organic solvents such as alcohols such as methanol and ethanol, hydrous alcohols, acetone, ethyl acetate, and 1,3-butylene glycol. Can be used alone or in combination. In addition, an extract obtained by applying a treatment such as partitioning or adsorption chromatography to the extract using the above-mentioned solvent can be used.

  The acne-improving agent of the present invention comprises (b) an ascorbic acid derivative and (c) glycyrrhizinate together with the solvent extract of (a) fuebegonia.

  (B) Ascorbic acid derivatives include, for example, L-ascorbic acid monostearate, L-ascorbic acid monopalmitate, L-ascorbic acid monoalkyl esters such as L-ascorbic acid monooleate, L-ascorbic acid monophosphate, L-ascorbic acid monoesters such as L-ascorbic acid-2-sulfate; L-ascorbic acid dialkyl esters such as L-ascorbic acid distearate, L-ascorbic acid dipalmitate, L-ascorbic acid diolate; L-ascorbic acid L-ascorbic acid diesters such as diphosphates; L-ascorbic acid tristearate, L-ascorbic acid tripalmitate, L-ascorbic acid triolate, etc. Esters; such as L- ascorbic acid glucosides such as L- ascorbic acid 2-glucoside, and the like, of which L- ascorbic acid glucoside or a salt thereof is preferably used. One or more ascorbic acid derivatives can be used.

  (C) Glycyrrhizinate can be extracted from licorice or synthesized by a known method. Examples of glycyrrhizinate include alkali metal salts such as sodium salt and potassium salt, ammonium salts, basic amino acids, alkanolamine salts, etc., and specifically, monoammonium glycyrrhizinate, dipotassium glycyrrhizinate, trisodium glycyrrhizinate, etc. Is exemplified. These glycyrrhizinates can be used singly or in combination of two or more. Of these, dipotassium glycyrrhizinate is particularly preferably used.

  The acne-improving agent of the present invention is preferably composed of (a) a solvent extract of fuebegonia, (b) an ascorbic acid derivative, and (c) glycyrrhizinate, but may contain other components. .

  The blending ratio of (a) fuebegonia solvent extract (dry residue), (b) ascorbic acid derivative, and (c) glycyrrhizinate of the acne-improving agent of the present invention is (0.01-0. 5): (5-40): It is preferable to mix | blend by 1: 1, More preferably, it is (0.01-0.02) :( 30-40): 1. By blending the three components within this range, the acne improving action is most effectively achieved.

  When using the acne improving agent of the present invention as a skin external preparation for acne improvement, 0.0005 to 0.02% by mass of the above-mentioned (a) fuebegonia solvent extract as a dry product in the total amount of the external preparation is blended. Of these, 0.001 to 0.02 mass% is more preferable. (B) About an ascorbic acid derivative, it is preferable to mix | blend 0.5-4 mass%, and it is more preferable to mix | blend 0.5-2 mass%. (C) About glycyrrhizinate, it is preferable to mix | blend 0.025-0.1 mass%, and it is more preferable to mix | blend 0.05-0.1 mass%. Within such a range, the acne improving action is most effective.

  In the present invention, in addition to the above essential components, it is preferable to further blend (d) vitamin B6 or a derivative thereof. Examples of vitamin B6 derivatives include vitamin B6 hydrochloride. By adding vitamin B6 or a derivative thereof, the acne improving effect is further enhanced.

  In addition to the above essential components, the acne-improving skin external preparation of the present invention includes components usually used in external preparations for skin, such as cosmetics and pharmaceuticals, such as aqueous components, oily components, powder components, alcohols, moisturizers, thickening agents. An agent, an ultraviolet absorber, a whitening agent, an antiseptic, an antioxidant, a surfactant, a fragrance, a colorant, various skin nutrients, and the like can be appropriately blended as necessary.

  The form of the external preparation for acne improvement of the present invention may be any form as long as it can be applied to conventional external preparations for skin, such as creams, lotions, ointments, emulsions, packs, bath preparations, etc., and the dosage form is not particularly limited.

  EXAMPLES Next, although a test example and an Example are given and this invention is demonstrated still in detail, this invention is not limited by this. Further, unless otherwise specified, the blending amount is mass% with respect to the whole external preparation for skin. First, the test method and standard used for evaluating the acne skin external preparation of the present invention will be described.

Test methods and standards
(1) Drugs Used Based on the formulation of each of the external preparations for skin described later, the acne suppressing effect and the acne scar improving effect of the external preparation for skin manufactured by a conventional method were measured by the test methods described later.
In addition, the solvent extract of Fuyu Begonia was prepared by the following method.

(Sample preparation)
A rhizome of Nepalese Fugue Begonia (Bergenia ciliata Sternb.) Was heated and extracted with 80% ethanol, and then the extract obtained by filtration was concentrated to dryness. This solid was dissolved in 50% 1,3-butylene glycol to prepare a 1% solution.

Formulation Example 1 (Lotion)
(Prescription) Mass%
(Phase A)
Mixed composition A 1.5
(Mixture of dipropylene glycol, glyceryl tri-2-ethylhexanoate, polyoxyethylene hydrogenated castor oil, polyglyceryl diisostearate)
Perfume appropriate amount (phase B)
95% ethyl alcohol 10.0
Glycerin 5.0
Citric acid 0.05
Sodium citrate 0.2
Caustic potash 0.4
Fuebegonia 50% 1,3-butylene glycol extract (dry residue) 0.0005
Ascorbic acid glucoside 2.0
Dipotassium glycyrrhizinate 0.05
Ethylparaben Appropriate amount Ion-exchanged water Residual

(Manufacturing method)
After the A phase is uniformly heated and dissolved, an appropriate amount of ion-exchanged water is added and added to the B phase and dissolved uniformly.

Formulation Example 2 (Cosmetic liquid)
(Prescription) Mass%
95% ethyl alcohol 10.0
Glycerin 5.0
Polyoxyethylene (50 mol) oleyl alcohol ether 0.5
Carboxyvinyl polymer 0.2
Caustic potash 0.5
Fuyu Begonia 50% 1,3-butylene glycol extract (dry residue) 0.001
Ascorbic acid glucoside 2.0
Dipotassium glycyrrhizinate 0.05
Vitamin B6 hydrochloride 0.05
Ethyl paraben Appropriate amount Perfume Appropriate amount Ion-exchanged water Residual

(Manufacturing method)
Dissolve the carboxyvinyl polymer uniformly in ion-exchanged water, while dissolving polyoxyethylene (50 mol) oleyl alcohol ether in 95% ethanol and add to the aqueous phase. Next, after adding other components, the mixture is neutralized with caustic potash and thickened.

Formulation Example 3 (Emulsion)
(Prescription) Mass%
Stearic acid 2.5
Cetyl alcohol 1.5
Vaseline 5.0
Liquid paraffin 10.0
Polyoxyethylene (10 mol) monooleate 2.0
Polyethylene glycol 1500 3.0
Caustic potash 1.0
Carboxyvinyl polymer 0.05
Fuebegonia 50% 1,3-butylene glycol extract (dry residue) 0.0005
Ascorbic acid glucoside 2.0
Dipotassium glycyrrhizinate 0.05
Ethyl paraben Appropriate amount Perfume Appropriate amount Ion-exchanged water Residual

(Manufacturing method)
Dissolve the carboxyvinyl polymer in a small amount of ion-exchanged water (A phase). Polyethylene glycol 1500 and caustic potash are added to the remaining ion exchange water, heated and dissolved, and then kept at 70 ° C. (aqueous phase). The other ingredients are mixed, heated and melted, and kept at 70 ° C. (oil phase). Add the oil phase to the water phase, preliminarily emulsify, add the A phase, uniformly emulsify with a homomixer, and cool to 30 ° C. while stirring well after emulsification.

(2) Test method For 40 women suffering from acne from age 22 to 39 Each external preparation for skin shown in (Emulsion) was applied 2-3 times a day in the order of lotion → beauty serum → milk (every time), and observed after 8 weeks.
The evaluation was made according to the following evaluation criteria, divided into two stages of (a) improved or unchanged or deteriorated (b) compared with the drug used before use. In addition, acne and the number of acne scars were measured by experts to evaluate the acne improvement effect. These results are shown in Table 1.

[Evaluation criteria for acne improvement]
<Questionnaire evaluation>
(Usability evaluation criteria)
A: Overall improvement is 28 or more in 40 (a).
○: The overall improvement degree is 20 to 27 in 40 (a).
(Triangle | delta): (a) is 15-24 in 40 people by general improvement degree.
X: In general improvement degree, (a) is 14 or less in 40 people.

<Measurement evaluation of acne and number of acne scars>
The number of acne and acne marks was measured and evaluated by four experts, and the number of evaluations was averaged. (The number of acne was the total number of red acne-comed.)

(Usability evaluation criteria)
○: The total number of acne and acne scars of 40 people is less than 15.
Δ: The total number of acne and acne scars of 40 people is less than 15 to 25.
X: The total number of acne and acne scars of 40 people is 25 or more.

  As can be seen from Table 1, the skin external preparation of the present invention showed an excellent acne suppression effect and an acne scar improvement effect.

Next, formulation examples of the external preparation for acne improvement according to the present invention will be given.
Example 1 Essence (Prescription) Mass%
95% ethyl alcohol 10.0
Glycerin 5.0
Polyoxyethylene (50 mol) oleyl alcohol ether 0.5
Carboxyvinyl polymer 0.2
Caustic potash 0.5
Fuyu Begonia 95% ethanol extract (dry residue) 0.001
Ascorbic acid glucoside 2.0
Dipotassium glycyrrhizinate 0.05
Vitamin B6 hydrochloride 0.05
Ethyl paraben Appropriate amount Perfume Appropriate amount Ion-exchanged water Residual

(Manufacturing method)
Dissolve the carboxyvinyl polymer uniformly in ion-exchanged water, while dissolving polyoxyethylene (50 mol) oleyl alcohol ether in 95% ethanol and add to the aqueous phase. Next, after adding other components, the mixture is neutralized with caustic potash and thickened.

Example 2 Lotion (Prescription) Mass%
(Phase A)
Mixed composition A 1.5
(Mixture of dipropylene glycol, glyceryl tri-2-ethylhexanoate, polyoxyethylene hydrogenated castor oil, polyglyceryl diisostearate)
Perfume appropriate amount (phase B)
95% ethyl alcohol 10.0
Glycerin 5.0
Citric acid 0.05
Sodium citrate 0.2
Caustic potash 0.4
Fuebegonia 50% 1,3-butylene glycol extract (dry residue) 0.0005
Ascorbic acid sulfate 2Na 2.0
Dipotassium glycyrrhizinate 0.05
Ethylparaben Appropriate amount Ion-exchanged water Residual

(Manufacturing method)
After the A phase is uniformly heated and dissolved, an appropriate amount of ion-exchanged water is added and added to the B phase and dissolved uniformly.

Example 3 Latex (Prescription) Mass%
Stearic acid 2.5
Cetyl alcohol 1.5
Vaseline 5.0
Liquid paraffin 10.0
Polyoxyethylene (10 mol) monooleate 2.0
Polyethylene glycol 1500 3.0
Caustic potash 1.0
Carboxyvinyl polymer 0.05
Fuebegonia 50% 1,3-butylene glycol extract (dry residue) 0.0005
Ascorbic acid glucoside 2.0
Monoammonium glycyrrhizinate 0.05
Ethyl paraben Appropriate amount Perfume Appropriate amount Ion-exchanged water Residual

(Manufacturing method)
Dissolve the carboxyvinyl polymer in a small amount of ion-exchanged water (A phase). Polyethylene glycol 1500 and caustic potash are added to the remaining ion exchange water, heated and dissolved, and then kept at 70 ° C. (aqueous phase). The other ingredients are mixed, heated and melted, and kept at 70 ° C. (oil phase). Add the oil phase to the water phase, preliminarily emulsify, add the A phase, uniformly emulsify with a homomixer, and cool to 30 ° C. while stirring well after emulsification.

Example 4 Cream (formulation) Mass%
Stearic acid 2.0
Stearyl alcohol 7.0
Hydrogenated Lanolin 2.0
Squalane 5.0
2-Octyldodecyl alcohol 6.0
Polyoxyethylene (25 mol) cetyl alcohol ether 3.0
Glycerin monostearate ester 2.0
Propylene glycol 5.0
Fuyu Begonia 50% ethanol extract (dry residue) 0.005
Magnesium ascorbate phosphate 0.5
Monoammonium glycyrrhizinate 0.1
4-methoxysalicylic acid potassium salt 1.0
Ethyl paraben Appropriate amount Fragrance Appropriate amount Ion-exchanged water Residual

(Manufacturing method)
Propylene glycol is added to ion-exchanged water and heated to 70 ° C. (aqueous phase). The other ingredients are mixed, heated and melted, and kept at 70 ° C. (oil phase). Preliminarily emulsify by adding an oil phase to the aqueous phase, uniformly emulsify with a homomixer, and then cool to 30 ° C. while stirring well.

Example 5 Cream (formulation) Mass%
Solid paraffin 5.0
Beeswax 10.0
Vaseline 15.0
Liquid paraffin 41.0
Glycerin monostearate ester 2.0
Polyoxyethylene (20 mol) sorbitan monolaurate 2.0
Soap powder 0.1
Borax 0.2
Fuyu Begonia 50% 1,3-butylene glycol extract (dry residue) 0.01
Ascorbic acid sulfate 2Na 1.0
Dipotassium glycyrrhizinate 0.05
Tranexamic acid methylamide hydrochloride 0.7
Sodium bisulfite 0.03
Ethyl paraben Appropriate amount Perfume Appropriate amount Ion-exchanged water Residual

(Manufacturing method)
Add soap powder and borax to ion-exchanged water and heat to maintain at 70 ° C. (aqueous phase). The other ingredients are mixed, heated and melted, and kept at 70 ° C. (oil phase). The reaction is gradually added while stirring the oil phase in the aqueous phase. Thereafter, the mixture is uniformly emulsified with a homomixer and cooled to 30 ° C. while stirring well.

Example 6 Latex (Prescription) Mass%
Microcrystalline wax 1.0
Beeswax 2.0
Lanolin 20.0
Liquid paraffin 10.0
Squalane 5.0
Sorbitan sesquioleate ester 4.0
Polyoxyethylene (20 mol) sorbitan monooleate 1.0
Propylene glycol 7.0
Fuyu Begonia 30% ethanol extract (dry residue) 0.02
Ascorbic acid glucoside 0.5
Dipotassium glycyrrhizinate 0.05
Tranexamic acid 2.0
Sodium bisulfite 0.01
Ethyl paraben Appropriate amount Perfume Appropriate amount Ion-exchanged water Residual

(Manufacturing method)
Propylene glycol is added to ion-exchanged water and heated to 70 ° C. (aqueous phase). The other ingredients are mixed, heated and melted, and kept at 70 ° C. (oil phase). The water phase is gradually added while stirring the oil phase, and the mixture is uniformly emulsified with a homomixer, and then cooled to 30 ° C. while stirring well.

Claims (3)

(A) a solvent extract of Fuergegonia (Bergenia ciliata Sternb.);
(B) an ascorbic acid derivative;
(C) glycyrrhizinate,
An acne-improving agent characterized by comprising: (A) a solvent extract of Fuergegonia (Bergenia ciliata Sternb.);
(B) an ascorbic acid derivative;
(C) A skin external preparation for acne improvement characterized by containing glycyrrhizinate.   (D) The skin external preparation for acne improvement of Claim 2 which further contains vitamin B6 or its derivative (s).