JP2005194239A - Ceramide synthesis promotor and skin care preparation for external use - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To obtain a ceramide synthesis promotor and to provide a skin care preparation for external use each containing one or more kinds of substances selected from extracts of Pterocarpus marsapium, Symplocos racemosa, Sterculia scaphigera Wall and Peucedanum japonicum. <P>SOLUTION: The ceramide synthesis promotor comprises one or more kinds of substances selected from extracts of Pterocarpus marsapium, Symplocos racemosa, Sterculia scaphigera Wall and Peucedanum japonicum and is excellent in ceramide synthesis-promoting effect and is safe and excellent also in improving effect on chapped skin and dried skin. The skin care preparation for external use is safe and excellent in improving effect on chapped skin and dried skin. <P>COPYRIGHT: (C)2005,JPO&NCIPI

Description

  The present invention relates to a ceramide synthesis promoter characterized by containing one or more selected from extracts of asana, rodda, hantaikai, and sacuna, and is particularly effective in preventing rough skin and dry skin. The present invention relates to a ceramide synthesis accelerator.

  Ceramide is the main component of lamellar granules produced and secreted in the upper spiny layer and granule layer when cells move from the basal layer of the skin to the stratum corneum. Forms keratinocyte lipids that play an important role. Causes of rough skin include dryness, contact with irritants, and skin irritation due to ultraviolet rays. It is said that promoting the production of ceramide is effective in restoring the barrier function that protects the skin from dryness and irritants. It has been confirmed that seven types of ceramide are present in human skin, and it is ideal that all kinds of ceramides are supplemented at a ratio of existing in the stratum corneum.

Conventionally, ceramide has been blended into various skin external preparations as a cosmetic that is effective in preventing and improving rough skin and dry skin, but supplements all types of ceramide present in human skin at an appropriate ratio. That was technically difficult. Patent Literature 1 and Patent Literature 2 have been reported as ceramide synthesis promoters for promoting ceramide synthesis in vivo, but it was difficult to say that the effect was sufficient. In addition, the ceramide synthesis promotion effect of the extracts of asana, rodda, hantaikai and sacuna has not been reported.
JP-A-8-217658 JP 2001-220345 A

  From the above, a ceramide synthesis accelerator and a skin external preparation excellent in the effect of improving rough skin and dry skin are desired.

  Under these circumstances, as a result of intensive studies, the present inventors have found that ceramide synthesis is promoted by extracts of asana, rodda, hantaikai, and sacuna, and further, one or two selected from these extracts As a result, the present inventors have completed the present invention by finding an effect of preventing and improving rough skin more than seeds and dry skin.

  Asana used in the present invention belongs to the leguminous family and has the scientific name: Pterocarpus marsapium, and its seed has been used for anti-inflammation, hemostasis, skin diseases and bruises. Rodda belongs to the cypress family and has the scientific name: Symplocos racemosa and is a plant native to the United States. Hanta Taikai is a deciduous tree belonging to the family Aogiri and has the scientific name: Sterculia scaphigera Wall. Sacna is an evergreen perennial plant belonging to the celery family, and its scientific name is Peucedanum japonicum, and its root has been used for recovery from fatigue and nourishment.

  The extraction method of asana, rodda, hantaikai, and sacuna of the present invention is not particularly limited. For example, it may be extracted by heating, or may be extracted at room temperature or low temperature. 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 above extract may be used as it is, or may be used after treatment such as concentration, dilution, filtration, decolorization with activated carbon, deodorization, etc., if necessary. Further, the extracted solution may be used as a dried product after being concentrated and dried, spray dried, freeze dried, etc., or may be used after concentrating or isolating the active ingredient by performing column purification or the like. good.

  In order to use the ceramide synthesis promoter characterized in that it contains one or more selected from the extracts of asana, rodda, hantaikai and sacuna of the present invention for the purpose of improving rough skin, it is usually systemic or topical. It is administered by internal or external use. The dose varies depending on age, body weight, symptoms, therapeutic effect, administration method, treatment time, etc., but is usually 1 mg to 1 g per adult, preferably 20 mg to 200 mg once to several times a day. Is done. Since the dosage varies depending on various conditions, an amount smaller than the above-mentioned administration range may be sufficient, or it may be necessary to administer beyond the range.

  Examples of the ceramide synthesis promoter for oral administration of the present invention include tablets, pills, powders, granules, capsules, emulsions, solutions, suspensions, syrups, and elixirs. The above extract may be used as it is, and the excipient, extender, binder, wetting agent, disintegrant, surfactant, lubricant, dispersant, buffer, as long as the effect of the extract is not impaired. Agents, fragrances, preservatives, solubilizers, solvents and the like can be used. Specifically, lactose, sucrose, sorbit, mannitol, starch, precipitated calcium carbonate, heavy magnesium oxide, talc, calcium stearate, magnesium stearate, cellulose or derivatives thereof, amylopectin, polyvinyl alcohol, gelatin, surface activity Agent, water, physiological saline, ethanol, glycerin, propylene glycol, cacao butter, laurin butter, petrolatum, paraffin, higher alcohol and the like.

  The skin external preparation of the present invention can be used for any of cosmetics, quasi drugs, and pharmaceuticals. Examples of the dosage form include skin lotions, creams, emulsions, gels, aerosols, essences, packs, Examples of the cleaning agent, bath preparation, foundation, dusting powder, lipstick, ointment, and poultice applied to the skin. The above-mentioned extract may be used as it is, and the components used for the external preparation are within the range not impairing the effect of the extract, oils, waxes, hydrocarbons, fatty acids, alcohols, esters, interfaces Components such as activators, metal soaps, pH adjusters, preservatives, fragrances, moisturizers, powders, ultraviolet absorbers, thickeners, dyes, antioxidants, whitening agents, chelating agents, and the like can also be blended.

  The amount of the extract used in the present invention is 0.0001% by weight or more, preferably 0.001 to 50% by weight, in terms of solid matter, based on the ceramide synthesis accelerator of the present invention. If it is less than 0.0001% by weight, a sufficient effect is hardly expected. When it exceeds 50% by weight, the effect is hardly increased and it is uneconomical. In addition, the addition method may be added in advance or during the production, and may be appropriately selected in consideration of workability.

  The extract of asana, rodda, hantaikai and sacuna of the present invention was excellent in ceramide synthesis promoting effect. Moreover, the skin external preparation containing these extracts was safe and rough, and was excellent in the improvement effect of dry skin.

  Next, in order to describe the present invention in detail, examples of producing the extract used in the present invention, formulation examples and experimental examples of the present invention will be given as examples, but the present invention is not limited thereto. The part of the amount shown in the examples indicates part by weight, and% indicates% by weight.

Production Example 1 Hot water extract of asana Add 2 L of purified water to 100 g of dried asana bark, extract at 95-100 ° C. for 2 hours, filter, concentrate the filtrate, freeze-dry and heat asana. 2.6 g of water extract was obtained.

Production Example 2 Asana ethanol extract 100 g of dried asana bark and stems were added with 2 L of ethanol, extracted at room temperature for 7 days, filtered, and the filtrate was concentrated to dryness to obtain 4 ethanol extracts of asana. .5 g was obtained.

Production Example 3 Asana 50% 1,3-butylene glycol aqueous extract Asana seeds and bark dried 20 g were added with 200 mL of purified water and 200 mL of 1,3-butylene glycol, extracted at room temperature for 7 days, and then filtered. , 360 g of asana 50% 1,3-butylene glycol extract was obtained.

Production Example 4 Hot Water Extract of Rodda 400 ml of purified water was added to 20 g of dried Rhoda leaves and fruits, extracted at 95-100 ° C. for 2 hours, filtered, and the filtrate was concentrated, freeze-dried and Rhoda 3.0 g of a hot water extract was obtained.

Production Example 5 Rhoda ethanol extract 100 g dry roda bark was added with 1 L of ethanol, extracted at room temperature for 7 days, filtered, and the filtrate was concentrated to dryness to obtain 5.8 g of Rhoda ethanol extract. It was.

Production Example 6 50% 1,3 Butylene Glycol Aqueous Extract of Rodda 200 ml of purified water and 200 ml of 1,3-butylene glycol were added to 20 g of dried Rodda leaves and bark, extracted for 7 days at room temperature, and then filtered. 380 g of 50% 1,3-butylene glycol extract of Rodda was obtained.

Production Example 7 Hot water extract of hantai kai 800 ml of purified water was added to 20 g of dried hantai kai seeds, extracted at 95-100 ° C. for 2 hours, filtered, and the filtrate was concentrated and freeze-dried. 3.4 g of water extract was obtained.

Production Example 8 Hantaikai Ethanol Extract 100 g of dried huntaikai seeds and roots was added with 1 L of ethanol, extracted at room temperature for 7 days, filtered, the filtrate was concentrated to dryness, and the Rhoda ethanol extract was obtained. 7 g was obtained.

Manufacture example 9 50% 1,3-butylene glycol aqueous extract of hantai kai 200 ml of purified water and 200 ml of 1,3-butylene glycol were added to 20 g of dried hantai kai leaves and seeds, extracted at room temperature for 7 days, and then filtered. 370 g of a 50% 1,3-butylene glycol extract of Rodda was obtained.

Production Example 10 Sacuna hot water extract 1 L of purified water was added to 50 g of dried sakuna branches and roots, extracted at 95-100 ° C. for 2 hours, filtered, and the filtrate was concentrated, freeze-dried, and dried. 12 g of a hot water extract was obtained.

Production Example 11 Sacuna Ethanol Extract 50 g of dried sakuna leaves and branches was added with 1 L of ethanol, extracted at room temperature for 7 days, filtered, and the filtrate was concentrated to dryness. 8 g was obtained.

Production Example 12 Extract of 50% 1,3-butylene glycol aqueous solution of sacuna 200 mL of purified water and 200 mL of 1,3-butylene glycol were added to 20 g of a dried product of sacna branches, extracted at room temperature for 7 days, filtered, and filtered. 350 g of 50% 1,3-butylene glycol extract was obtained.

Formulation Example 1 Cream 1
Formulation Formulation 1. 1. Asana hot water extract (Production Example 1) 1.0 part Squalane 5.5
3. Olive oil 3.0
4). Stearic acid 2.0
5). Beeswax 2.0
6). Octyldodecyl myristate 3.5
7). Polyoxyethylene cetyl ether (20E.O.) 3.0
8). Behenyl alcohol 1.5
9. Glycerol monostearate2.5
10. Fragrance 0.1
11.1,3-butylene glycol 8.5
12 Ethyl paraoxybenzoate 0.05
13. Methyl paraoxybenzoate 0.2
14 Purified water 67.15
[Manufacturing method] Components 2 to 9 are heated and dissolved and mixed, and kept at 70 ° C to obtain an oil phase. Ingredients 1 and 11 to 14 are heated and dissolved and mixed, and kept at 75 ° C. to obtain an aqueous phase. The aqueous phase is added to the oil phase to emulsify, and the mixture is cooled while stirring.

Formulation Example 2 Cream 2
Formulation Formulation 1. Roda hot water extract (Production Example 4) 1.0 part Hantai Kai hot water extract (Production Example 7) 1.0
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 66.15
[Manufacturing method] Components 3 to 10 are dissolved by heating and mixed, and kept at 70 ° C to obtain an oil phase. Ingredients 1 and 2 and ingredients 12-15 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.

Formulation Example 3 Cream 3
In Formulation Example 1, Cream 3 was obtained by replacing the hot water extract of asana with a 50% 1,3-butylene glycol aqueous solution extract of Sacna (Production Example 12).

Comparative Example 1 Conventional Cream In Formulation Example 1, a hot cream extract of asana was replaced with purified water to obtain a conventional cream.

Formulation Example 4 Lotion Formulation Formulation amount 1. Rhoda ethanol extract (Production Example 5) 0.1 part 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 84.47
[Manufacturing method] Components 2-6 and 11 and components 1 and 7-10 are uniformly dissolved, mixed and filtered to obtain a product.

Formulation Example 5 Latex 1
Formulation Formulation 1. 1. Asana 50% 1,3-butylene glycol aqueous solution extract (Production Example 3) 0.5 part Squalane 5.0
3. Olive oil 5.0
4). Jojoba oil 5.0
5). Cetanol 1.5
6). Glycerol monostearate 2.0
7). Polyoxyethylene cetyl ether (20E.O.) 3.0
8). Polyoxyethylene sorbitan monooleate (20E.O.) 2.0
9. Fragrance 0.1
10. Propylene glycol 1.0
11. Glycerin 2.0
12 Methyl paraoxybenzoate 0.2
13. Purified water 72.7
[Manufacturing method] Components 2 to 8 are dissolved by heating and mixed, and kept at 70 ° C to obtain an oil phase. Ingredients 1 and 10-13 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. The component 9 is added at 45 ° C., and further cooled to 30 ° C. to obtain a product.

Formulation Example 6 Latex 2
In Formulation Example 5, 0.5 part of 50% 1,3-butylene glycol aqueous extract of asana was mixed with 0.25 part of Rodda's hot water extract (Production Example 4) and hot water extract of Sacna (Production Example 10). The emulsion 2 was replaced with 0.25 part.

Formulation Example 7 Gel formulation Formulation amount 1. 50% 1,3-butylene glycol aqueous extract of hantaikai
(Production Example 9) 1.0 part Ethanol 5.0
3. Methyl paraoxybenzoate 0.1
4). Polyoxyethylene hydrogenated castor oil (60 EO) 0.1
5). Fragrance 0.05
6.1,3-Butylene glycol 5.0
7). Glycerin 5.0
8). Xanthan gum 0.1
9. Carboxyvinyl polymer 0.2
10. Potassium hydroxide 0.2
11. Purified water 83.25
[Manufacturing method] Components 2 to 5 and components 1 and 6 to 11 are uniformly dissolved and mixed to obtain a product.

Formulation Example 8 Pack Formulation Formulation 1. Hantaikai ethanol extract (Production Example 8) 0.1 part Sacna hot water extract (Production Example 10) 0.1
3. Polyvinyl alcohol 12.0
4). Ethanol 5.0
5.1,3-butylene glycol 8.0
6). Methyl paraoxybenzoate 0.2
7). Polyoxyethylene hydrogenated castor oil (20 EO) 0.5
8). Citric acid 0.1
9. Sodium citrate 0.3
10. Fragrance 0.05
11. Purified water 73.65
[Production method] Components 1 to 11 are uniformly dissolved to obtain a product.

Formulation Example 9 Foundation Formulation Formulation amount 1. Asana ethanol extract (Production Example 2) 0.5 part Sacuna ethanol extract (Production Example 11) 0.5
3. Stearic acid 2.4
4). Polyoxyethylene sorbitan monostearate (20E.O.) 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. Sodium carboxymethylcellulose 0.1
11. Bentonite 0.5
12 Propylene glycol 4.0
13. Triethanolamine 1.1
14 Methyl paraoxybenzoate 0.2
15. Titanium dioxide 8.0
16. Talc 4.0
17. Bengala 1.0
18. Yellow iron oxide 2.0
19. Fragrance 0.1
20. Purified water 60.1
[Production Method] Components 1 to 8 are heated and dissolved, and kept at 80 ° C. to obtain an oil phase. Swell component 10 well with component 20, then add components 12-14 and mix uniformly. To this, components 15 to 18 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 oily phase is added to the aqueous phase with stirring, cooled, and component 19 is added at 45 ° C, and cooled to 30 ° C with stirring to give a product.

Formulation Example 10 Ointment Formulation Formulation amount 1. Asana hot water extract (Production Example 1) 0.01 part2. 50% 1,3-butylene glycol extract of Rodda (Production Example 6) 0.5
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 66.39
[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 11 Beverage Formulation Formulation amount (% by weight)
1. Asana hot water extract (Production Example 1) 1.0
2. Stevia 0.05
3. Malic acid 5.0
4). Fragrance 0.1
5). Water 93.85
[Production Method] Components 2 and 3 are dissolved in a small amount of water. Components 1 and 4, 5 are then added and mixed.

Formulation Example 12 Tablet Formulation Formulation amount (% by weight)
1. Hantai Kai hot water extract (Production Example 7) 10.0
2. Corn starch 10.0
3. Purified white sugar 20.0
4). Carboxymethylcellulose 10.0
5). Microcrystalline cellulose 35.0
6). Polyvinylpyrrolidone 5.0
7). Talc 10.0
[Production Method] Components 1 to 5 were mixed, and then an aqueous solution of Component 6 was added as a binder and granulated by a conventional method. This was mixed with ingredient 7 as a lubricant, and then tableted into 100 mg tablets.

  Next, experimental examples will be given to explain the effects of the present invention in detail.

Experimental Example 1 Ceramide Synthesis Promotion Test 1 × 10 ⁵ Pam212 cells, a mouse keratinocyte-derived cell line, were seeded in a 6 cm dish and cultured for 4 days. Thereafter, the sample was added to a final concentration of 10 μg / mL, and the culture was further continued for 24 hours. Next, the cells were washed three times with PBS (−), collected by a rubber policeman, and lyophilized. Lipids were extracted from cells with 1 mL of chloroform: methanol (2: 1), and the amount of ceramide in the cells was determined by the fluorescence method of Kisic et al. (Kisic A. and Rapport MM, Journal of Lipid Research, 15, 179-180. (1974)). That is, the lipid was hydrolyzed with 0.15 mL of 3N hydrochloric acid at 100 ° C. for 2 hours, dried in a desiccator, removed with hydrochloric acid, and then added with 2 mL of ethyl acetate and 1.25 mL of 0.1 M acetate buffer (pH 3.7). Stir well. Next, 0.25 mL of a fluorescamine solution (fluorescamine 7 mg / 25 mL acetone) was added, stirred well, then centrifuged, and the fluorescence intensity of the ethyl acetate layer was measured at Ex 410 nm and Em 490 nm. The rate of ceramide synthesis acceleration was determined by the ratio to the amount of ceramide produced by the control.

  The results of these experiments are shown in Table 1. As a result, the extracts of asana, rodda, hantaikai and sacuna showed an excellent ceramide synthesis promoting effect as compared with the control.

  When two or more mixtures selected from asana, rhoda, hantaikai and sacuna extracts were similarly tested, the ceramide synthesis promotion test showed excellent ceramide synthesis promotion effects.

Experiment 2 Use test 1
30 women (19 to 48 years old) suffering from rough skin and dry skin using 1% aqueous solution of hot water extract of asana, hot water extract of rodda, 1: 1 hot water extract of hantaikai and sakuna ) Was used for 1 month. After use, the improvement effect of rough skin and dry skin was determined by questionnaire. As a control, purified water was used.

  The test results are shown in Table 2. As a result, when using 1% aqueous solution of hot water extract of asana, hot water extract of rodda, 1: 1 mixture of hot water extract of hantaikai and sakuna, compared to the case of using purified water as a control, Excellent skin roughness and dry skin improvement effect. That is, a 1% aqueous solution of a hot water extract of asana, a hot water extract of rodda, and a 1: 1 mixture of a hot water extract of hantaikai and sacuna showed remarkable effects. During the test period, there was no skin problem and there was no problem with safety.

  A similar test was conducted on other aqueous solutions containing one or more selected from the extracts of asana, rodda, hantaikai and sacuna. It was safe and had excellent effects on improving rough and dry skin. Indicated.

Experiment 3 Use test 2
Using the creams of Formulation Examples 1 to 3 and the conventional cream of Comparative Example 1, a one month use test was conducted on 30 women (19 to 49 years old) who suffer from rough skin and dry skin. After use, the improvement effect of rough skin and dry skin was determined by questionnaire.

  The test results are shown in Table 3. As a result, the creams obtained in Formulation Examples 1 to 3 were superior to the conventional cream obtained in Comparative Example 1 in the effect of preventing and improving rough skin and dry skin. During the test period, there was no skin problem and there was no problem with safety. There was also no problem with the deterioration of the prescription ingredients.

  When the usage test was similarly conducted for Formulation Examples 4 to 10, it was safe, and showed excellent rough skin prevention and dry skin prevention and improvement.

One or more selected from the extracts of asana, rodda, hantaikai and sacuna of the present invention can be used as an excellent ceramide synthesis accelerator. In addition, it is possible to provide an external preparation for skin that is safe, rough, and excellent in improving dry skin.

Claims (2)

A ceramide synthesis promoter characterized by containing one or more selected from extracts of asana, rodda, hantaikai and sacuna. A skin external preparation excellent in the effect of preventing or improving rough skin and dry skin, comprising the ceramide synthesis promoter according to claim 1.