JP2013049634A - Acne treatment agent - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide an acne treatment agent having a high effect on the treatment of acne without inducing stinging by high concentration vitamin C or its derivative.SOLUTION: The acne treatment agent includes vitamin C or its derivative and the extract of "sanshichi ninjin", a kind of carrot, and by using the extract of "sanshichi ninjin" which has an effect of enhancing glutathione reductase activity together with vitamin C or its derivative, the acne treatment effect is synergistically enhanced without inducing stinging.

Description

  [Technical Field] The present invention relates to an acne improving agent and a skin external preparation for improving acne, characterized by containing vitamin C or a derivative thereof and a sancinin ginseng extract.

  Acne is an inflammatory disease of the skin caused by various causes and is medically called acne vulgaris. It occurs mainly on the face, head, chest, and back with many sebaceous glands. Various factors are thought to be intricately intertwined with the development of acne, with excessive sebum secretion, keratinization of hair follicles, and bacteria in hair follicles playing important roles. Therefore, as an external preparation for acne treatment, creams and ointments containing a sebum secretion inhibiting component, a keratolytic component, an anti-inflammatory component and an antibacterial substance are generally used.

  In recent years, it has been clarified that treatment with a preparation containing vitamin Cs has an effect of improving acne clinically (Patent Document 1). Since vitamin C is an antioxidant component having a strong reducing action, it is considered that oxidative protection of the skin is effective in improving acne. However, increasing the concentration of vitamin C increases the effect of improving acne. There is a problem that stinging due to vitamin C is likely to be induced, which is not practical. Stinging is a tingling or tingling sensation that is felt temporarily when a cosmetic or the like is applied, and there are many cases in which the use of the cosmetic or the like must be stopped. Therefore, it has been desired to develop a means for improving the acne improvement effect in addition to increasing the concentration of vitamin Cs.

  On the other hand, glutathione is a tripeptide composed of glutamic acid, cysteine, and glycine, and is an antioxidant component present in cells. Glutathione exhibits a reducing action by acting as an electron donor, but is converted to oxidized glutathione in this process. Oxidized glutathione is converted to reduced glutathione by the action of glutathione reductase, and again exhibits a reducing action. That is, increasing the intracellular glutathione reductase activity is thought to lead to an increase in the antioxidant level of the cell, and a glutathione reductase activity enhancer has been disclosed (Patent Document 2).

  In recent years, research on the extract of sanchinin ginseng has been promoted, and a collagen synthesis accelerator (patent document 3) and a composition for hair growth (patent document 4) have been disclosed. The glutathione reductase activity of the sancinin carrot extract is disclosed. An enhancing action and an acne improving action have not been reported.

JP2004-244370 JP 2006-206513 A JP-A-2005-139141 JP 2009-167121 A

  The acne improvement effect of vitamin C or its derivative alone is not sufficient at a low concentration, but the effect is increased at a high concentration, but there is a problem of stinging induction. An object of the present invention is to provide an acne improving agent and a skin external preparation for improving acne having high effects without inducing stinging.

  As a result of intensive studies to solve this problem, the present inventor has found that it is useful for improving acne to enhance glutathione reductase activity in skin cells and increase the antioxidant level of cells. In addition, the combined use of vitamin C or a derivative thereof and a glutathione reductase activity enhancer can synergistically enhance the acne-improving effect without inducing stinging, and the extract of sanchinin ginseng is glutathione. It has been found that the reductase activity enhancing action is exerted, and the present invention has been completed.

  The present invention is an acne ameliorating agent and a skin external preparation for acne amelioration characterized by containing vitamin C or a derivative thereof and a sancinin ginseng extract.

  By using the vitamin C of the present invention or a derivative thereof in combination with the sancinin ginseng extract, the acne improvement effect can be synergistically enhanced without inducing stinging.

  Vitamin C or a derivative thereof in the present invention is not particularly limited, and examples thereof include ascorbic acid, ascorbic acid phosphate ester, ascorbic acid fatty acid ester, ascorbic acid glucoside and other ascorbic acid glycosides and salts thereof, and the like. Can be mentioned. Examples of the salt include alkali metal salts such as sodium salt and potassium salt, alkaline earth metal salts such as calcium salt and magnesium salt, organic amine salts such as ammonium salt, triethanolamine salt and triethylamine salt, lysine salt, arginine salt and the like The basic amino acid salt of Among these vitamin C or derivatives thereof, particularly preferred are ascorbic acid or ascorbic acid phosphate ester and salts thereof. These may be used alone or in combination of two or more.

  The Sancytin carrot as referred to in the present invention belongs to the genus Carrot family and has the scientific name Panax not-ginseng. It is cultivated on an alpine slope at an altitude of about 1500m near Yunnan Province in southern China, and is used as a herbal medicine for hemostasis and nutritional tonic. Herbal medicines have names such as 37 ginseng, red ginseng, thirty seven, seven seven, ginseng lacquer, gold lacquer, etc. Steamed and heat-treated and then dried roughly, it can be broadly divided into ripening ginseng and ginseng ginseng.

  The sancytin carrot extract used in the present invention is a product extracted from a part of the plant body such as leaves, stems, flowers, fruits, seeds and roots of the plant body or whole plant. What is obtained by extracting from a root is preferable. This is marketed under the name of Ginseng, so you can use it.

The extraction method of the sancinin ginseng of this invention is not specifically limited, For example, what was extracted by heating may be used, and what was extracted at normal temperature or low temperature may be used.
Examples of the solvent to be extracted include water, lower alcohols (methanol, ethanol, 1-propanol, 2-propanol, 1-butanol, 2-butanol, etc.), liquid polyhydric alcohols (1,3-butylene glycol, propylene glycol). , Glycerin, etc.), ketones (acetone, methyl ethyl ketone, etc.), acetonitrile, esters (ethyl acetate, butyl acetate, etc.), hydrocarbons (hexane, heptane, liquid paraffin, etc.), ethers (ethyl ether, tetrahydrofuran, propyl ether) Etc.). Preferred are polar solvents such as water, lower alcohols and liquid polyhydric alcohols, and particularly preferred are water, ethanol, 1,3-butylene glycol and propylene glycol. These solvents may be used alone or in combination of two or more.

  The extract may be used as it is, or may be used after concentration, dilution, filtration, decolorization with activated carbon, deodorization, or the like, if necessary. Furthermore, the extracted solution may be used as a dried product after being concentrated, dried, spray-dried, freeze-dried, etc., or the active ingredient may be concentrated or isolated by column purification. good.

  In order to use an acne ameliorating agent characterized by containing vitamin C of the present invention or a derivative thereof and a sancinin ginseng extract, it is usually administered by external use. The dose varies depending on age, body weight, symptoms, therapeutic effect, administration method, treatment time, etc., but is usually 1 mg to 5000 mg, preferably 5 mg to 1000 mg, more preferably 20 mg to 200 mg per adult. It is administered once to several times a day. Since the dosage varies depending on various conditions, an amount smaller than the above dosage range may be sufficient, or it may be necessary to administer beyond the range.

  The acne-improving agent characterized by containing vitamin C of the present invention or a derivative thereof and a sancinin ginseng extract can be used for any of cosmetics, quasi-drugs, and pharmaceuticals. Is applied to skin such as lotion, cream, emulsion, gel, aerosol, ointment, poultice, paste, plaster, essence, pack, cleaning agent, bath preparation, foundation, powder, lipstick, etc. Things. Fats and oils, waxes, hydrocarbons, fatty acids, alcohols that are components used in external preparations may be used as they are, as long as vitamin C or a derivative thereof and the above extract may be used as they are. , Esters, surfactants, metal soaps, pH adjusters, preservatives, fragrances, moisturizers, thickeners, pigments, antioxidants, chelating agents, and the like can be blended.

  The compounding amount of vitamin C or a derivative thereof used in the present invention is converted into a solid with respect to the total amount of the acne improver characterized by containing the vitamin C of the present invention or a derivative thereof and a sanchinin ginseng extract. Therefore, 0.0001% by weight or more, preferably 0.001 to 5% by weight is good. If it is less than 0.0001% by weight, a sufficient effect is hardly expected. When it exceeds 5% by weight, stinging tends to be induced. In addition, the addition method may be added in advance or during the production, and may be appropriately selected in consideration of workability.

  The compounding amount of the citrus carrot extract used in the present invention is converted into a solid with respect to the total amount of the acne improving agent characterized by containing the vitamin C of the present invention or a derivative thereof and the sancinin carrot extract. Therefore, 0.0001% by weight or more, preferably 0.001 to 50% by weight is good. If it is less than 0.0001% by weight, a sufficient effect is hardly expected. When it exceeds 50% by weight, it is uneconomical that the effect is hardly increased. In addition, the addition method may be added in advance or during the production, and may be appropriately selected in consideration of workability.

  In order to explain the present invention in detail, examples of the production of the extract used in the present invention, formulation examples and experimental examples of acne improving agents or skin external preparations for improving acne are given as examples, but the present invention is limited to these examples. It is not a thing.

Manufacture example 1 The hot water extract of a sanchinin carrot The dried material of the root of the sanchinin carrot was cut | disconnected finely, and after adding 800 mL water to 40g, it extracted at 95-100 degreeC for 2 hours. The obtained extract was filtered, concentrated, and freeze-dried to obtain 7.5 g of a hot water extract of sanchinin carrot.

Production Example 2 Sancithin Carrot 50% Ethanol Extract A dried product of Sanci carrot root was cut into small pieces, 500 mL of water and 500 mL of ethanol were added to 100 g, and extracted at room temperature for 7 days. The obtained extract was filtered and then concentrated to dryness to obtain 9.8 g of a 50% ethanol extract of sanchinin carrot.

Manufacture example 3 50% 1,3-butylene glycol extract of sanchinin carrot The dried product of leaves and stems of sanchinin carrot was cut finely, and 200 g of a 50 wt% aqueous solution of 1,3-butylene glycol was added to 20 g. For 7 days. After the extraction, the extract was filtered to obtain 160 g of a 50% 1,3-butylene glycol extract of sanchinin carrot.

  The following formulation can be performed as a formulation example of an acne ameliorating agent or a skin external preparation for acne amelioration characterized by containing vitamin C of the present invention or a derivative thereof and a sancinin ginseng extract.

Formulation Example 1 Lotion 1
Ingredient Amount (wt%)
1. Sodium ascorbate phosphate 1.0
2. Sancithin carrot hot water extract (Production Example 1) 0.1
3. 1,3-butylene glycol 8.0
4). Glycerin 2.0
5. Xanthan gum 0.02
6). Citric acid 0.01
7). Sodium citrate 0.1
8). Ethanol 5.0
9. Methyl paraoxybenzoate 0.1
10. Polyoxyethylene hydrogenated castor oil (40E.O.) 0.1
11. Fragrance 0.1
12 Purified water 83.47
[Production method] Components 1 to 7 and 12 and components 8 to 11 are uniformly dissolved, and both are mixed and filtered to obtain a product.

Comparative Example 1 Conventional lotion 1
In Formulation Example 1, a conventional lotion 1 was obtained by substituting purified water for the hot water extract of sancinin ginseng.

Comparative Example 2 Conventional lotion 2
In Formulation Example 1, a conventional lotion 2 was obtained by replacing sodium ascorbate phosphate with purified water.

Comparative Example 3 Conventional lotion 3
Ingredient Amount (wt%)
1. Sodium ascorbate phosphate 6.0
2. 1,3-butylene glycol 8.0
3. Glycerin 2.0
4). Xanthan gum 0.02
5. Citric acid 0.01
6). Sodium citrate 0.1
7). Ethanol 5.0
8). Methyl paraoxybenzoate 0.1
9. Polyoxyethylene hydrogenated castor oil (40E.O.) 0.1
10. Fragrance 0.1
11. Purified water 78.57
[Production method] Components 1 to 6 and 11 and components 7 to 10 are uniformly dissolved, and both are mixed and filtered to obtain a product.

Comparative Example 4 Conventional lotion 4
In Formulation Example 1, conventional lotion 4 was obtained by replacing the hot water extract of sodium ascorbate phosphate and sancinin ginseng with purified water.

Formulation Example 2 Cream component Formulation amount (% by weight)
1. Magnesium ascorbate phosphate 0.5
2. 50% ethanol extract of sanchinin carrot
(Production Example 2) 0.1
3. Squalane 5.5
4). Olive oil 3.0
5. Stearic acid 2.0
6). Beeswax 2.0
7). Octyldodecyl myristate 3.5
8). Polyoxyethylene cetyl ether (20E.O.) 3.0
9. Behenyl alcohol 1.5
10. Glycerol monostearate2.5
11. Fragrance 0.1
12.1,3-Butylene glycol 8.5
13. Ethyl paraoxybenzoate 0.05
14 Methyl paraoxybenzoate 0.2
15. Purified water 67.55
[Manufacturing method] Components 3 to 10 are heated and mixed to maintain an oil phase at 70 ° C. Ingredients 12 to 15 are dissolved by heating and mixed, and kept at 75 ° C. to form an aqueous phase. The aqueous phase is added to the oil phase to emulsify, and the mixture is cooled while stirring. Component 11 is added at 45 ° C., and the mixture is further cooled to 30 ° C. and components 1 and 2 are added to obtain a product.

Formulation Example 3 Emulsion component amount (% by weight)
1. Ascorbic acid 0.5
2. 50% 1,3-butylene of sanchinin carrot
Glycol extract (Production Example 3) 0.05
3. Squalane 5.0
4). Olive oil 5.0
5. Jojoba oil 5.0
6). Cetanol 1.5
7). Glycerol monostearate 2.0
8). Polyoxyethylene cetyl ether (20E.O.) 3.0
9. Polyoxyethylene sorbitan monooleate 2.0
10. Fragrance 0.1
11. Propylene glycol 1.0
12 Glycerin 2.0
13. Methyl paraoxybenzoate 0.2
14 Purified water 72.65
[Manufacturing method] Components 3 to 9 are dissolved by heating and mixed, and kept at 70 ° C to obtain an oil phase. Ingredients 11-14 are dissolved by heating and mixed, and kept at 75 ° C. to form an aqueous phase. The aqueous phase is added to the oil phase to emulsify, and the mixture is cooled with stirring. Then, component 10 is added at 45 ° C, and further cooled to 30 ° C, and components 1 and 2 are added to obtain a product.

Formulation Example 4 Ointment component Amount (% by weight)
1. Sodium ascorbate phosphate 1.0
2. Sancitin carrot hot water extract (Production Example 1) 1.0
3. Polyoxyethylene cetyl ether (30E.O.) 2.0
4). Glycerol monostearate 10.0
5. Liquid paraffin 5.0
6). Cetanol 6.0
7). Methyl paraoxybenzoate 0.1
8). Propylene glycol 10.0
9. Purified water 64.9
[Production Method] Components 3 to 6 are dissolved by heating and mixed, and kept at 70 ° C. to obtain an oil phase. Ingredients 1, 2, and 7-9 are dissolved by heating and mixed, and kept at 75 ° C. to form an aqueous phase. The aqueous phase is added to the oil phase to emulsify, and the mixture is cooled to 30 ° C. with stirring to obtain a product.

Formulation Example 5 Foundation component Amount (% by weight)
1. Magnesium ascorbate phosphate 1.0
2. Sancitin carrot hot water extract (Production Example 1) 1.0
3. Stearic acid 2.4
4). Polyoxyethylene sorbitan monostearate
(20 EO) 1.0
5. Polyoxyethylene cetyl ether (20E.O.) 2.0
6). Cetanol 1.0
7). Liquid lanolin 2.0
8). Liquid paraffin 3.0
9. Isopropyl myristate 6.5
10. Butyl paraoxybenzoate 0.1
11. Sodium carboxymethylcellulose 0.1
12 Bentonite 0.5
13. Propylene glycol 4.0
14 Triethanolamine 1.1
15. Methyl paraoxybenzoate 0.2
16. Titanium dioxide 8.0
17. Talc 4.0
18. Bengala 1.0
19. Yellow iron oxide 2.0
20. Fragrance 0.1
21. Purified water 59.0
[Production method] Components 3 to 10 are heated and dissolved, and kept at 80 ° C to obtain an oil phase. Swell component 11 well in component 21, then add components 1, 2 and 12-15 and mix uniformly. To this, components 16 to 19 pulverized and mixed with a pulverizer are added, and the mixture is stirred with a homomixer and kept at 75 ° C. to obtain an aqueous phase. The oil phase is added to this aqueous phase with stirring, cooled, component 20 is added at 45 ° C., and cooled to 30 ° C. with stirring to give a product.

Formulation Example 6 Bath agent component Formulation amount (% by weight)
1. Ascorbic acid 2.0
2. 50% ethanol extract of sanchinin carrot
(Production Example 2) 5.0
3. Sodium bicarbonate 50.0
4). Yellow No. 202 (1) 0.05
5. Fragrance 0.25
6). Anhydrous sodium sulfate 42.7
[Production Method] Components 1 to 6 are uniformly mixed to obtain a product.

  In order to effectively explain the present invention, experimental examples are given below. In addition, this invention is not limited by this.

Experimental Example 1 Activation Test of Intracellular Glutathione Reductase The activation effect of intracellular glutathione reductase was measured under the following conditions.

  Confluent human epidermal keratinocytes were further cultured in DMEM medium containing 1 μg / mL sample for 24 hours, then the cells were detached, and 1 mL of 50 mM phosphate buffer (pH 7.5) containing 1 mM EDTA was added. The mixture was sonicated and centrifuged at 15,000 rpm for 15 minutes, and the supernatant was used as a sample solution. To 900 μL of the sample solution, 100 μL of 9.5 mM oxidized glutathione / phosphate buffer solution and 120 μL of 2 mM NADPH / phosphate buffer solution were added, and the time-dependent change in absorbance at 340 nm (φA 340 nm / min, 3 minutes) was measured, and standard glutathione reductase was measured. The glutathione reductase activity of the sample solution was calculated from a calibration curve prepared from 0, 5, 10 and 20 mU / mL. At the same time, the protein concentration of the sample solution was measured, and the glutathione reductase activity per unit protein was calculated. The glutathione reductase activity of the cells to which no sample was added was used as a control, and the value of the glutathione reductase activity after addition of the sample when the control was 100 was calculated by the following formula 1 and used as the intracellular glutathione reductase activity.

  The test results are shown in Table 1. Sancytin carrot extract showed excellent activation of intracellular glutathione reductase.

Experimental Example 2 Use Test Using the skin lotion of Formulation Example 1 and Comparative Examples 1 to 4, a use test was conducted for 1 month for 75 women in their 20s to 30s who suffer from mild acne. The test subjects were divided into 5 groups of 15 people, and the skin lotions of Prescription Example 1 and Comparative Examples 1 to 4 were used twice daily, morning and evening, respectively. After completion of the test, the degree of improvement of acne was markedly improved: score 3, improvement: score 2, slightly improved: score 1, unchanged: score 0, exacerbation: score -1. We also investigated the feeling of sting.

  The test results are shown in Table 2. In the group using the conventional lotion 1 of Comparative Example 1 blended with the derivative of vitamin C and the conventional lotion 2 of Comparative Example 2 blended with the extract of sanchinin ginseng, the conventional lotion 4 of Comparative Example 4 was used. The acne improvement score was increased compared to the group using. In the group using the conventional lotion 3 of Comparative Example 3 containing a high concentration of a vitamin C derivative, the acne improvement score was further increased, but staging was induced in more than half of the subjects. On the other hand, in the group using the skin lotion of Formulation Example 1 in which a vitamin C derivative and sancinin ginseng extract were blended, no stinging was induced, and in Comparative Example 3 in which a vitamin C derivative was blended at a high concentration. The acne improvement score increased over the group using the conventional lotion 3, and the effect was synergistic with the effects of the vitamin C derivative and the sancinin ginseng extract alone. During the test period, there was no trouble and there was no problem in safety. In addition, for the prescription examples 2 to 6, an excellent acne improving effect was observed, and no induction of stinging was observed.

  Based on the above results, the extract of the citrus carrot of the present invention exhibits an effect of enhancing glutathione reductase activity, and also contains the vitamin C of the present invention or a derivative thereof and the extract of sanchinin carrot. It has been clarified that the improver exhibits an excellent acne improving effect without inducing stinging.

  The acne-improving agent characterized by containing vitamin C of the present invention or a derivative thereof and a sancinin ginseng extract exhibits an excellent acne-ameliorating action without inducing stinging.

Claims (2)

  An acne-improving agent comprising vitamin C or a derivative thereof and a sancinin ginseng extract.   A skin external preparation for improving acne, comprising the acne improving agent according to claim 1.