JP5557973B2 - Topical skin preparation - Google Patents

Description

  The present invention relates to an external preparation for skin which is excellent in skin aging prevention, rough skin and acne improving action by blending a specific plant extract.

  In recent years, free radicals and active oxygen have been taken up as factors that oxidize biological components, and their adverse effects have become a problem. It is said that free radicals and active oxygen are generated in the living body, decompose or crosslink biological tissues such as collagen, and oxidize fats and oils to form lipid peroxides that damage cells. Such disorders are thought to cause aging such as skin wrinkles and firmness, and one of the methods to prevent aging is to incorporate an antioxidant that removes free radicals and active oxygen. It has been. Conventional free radical scavengers used to prevent aging include ascorbic acid (vitamin C), tocopherol (vitamin E), 3,5-tert-butyl-4-hydroxytoluene (BHT), superoxide dismutase (SOD) Etc. have been used.

  It is known that hyaluronidase is activated during inflammation and lowers the molecular weight of hyaluronic acid, thereby reducing skin elasticity and causing aging such as wrinkles.

  There is skin inflammation caused by ultraviolet rays or the like as a cause of rough skin, and an external preparation for skin that subsides the inflammation and improves rough skin is desired. As one of the treatment methods, there is a method for suppressing the release of histamine, which is a inflammatory substance that occurs during inflammation. Conventionally, external treatments such as steroids and indomethacin have been performed for the treatment of rough skin.

  Acne and pimples are partly due to the fact that microbial metabolites in the sebaceous glands induce inflammation and hardening of the skin. For the treatment, an external preparation for skin containing salicylic acid or the like is used as an antibacterial agent.

Problems to be solved by the invention

  Vitamin C and SOD used for the purpose of preventing skin aging or anti-oxidation are unstable, difficult to formulate, and vitamin E cannot be said to have sufficient effects. Moreover, since BHT etc. which are synthetic compounds have a problem in safety | security and there exists a restriction | limiting in compounding quantity, it is not a chemical synthetic product but the natural raw material which is stable and has few side effects is desired. Similarly, since steroids and the like conventionally used as histamine release inhibitors have a risk of side effects, a skin external preparation derived from natural products with high safety and excellent effects is desired. In addition, it preferably has a safe and stable hyaluronidase inhibitory action and antibacterial action. In view of the above, there is a demand for a multifunctional external preparation for skin that is safe and excellent in stability and excellent in preventing skin aging, rough skin, and improving acne.

Means for solving the problem

  Under these circumstances, as a result of intensive studies, the present inventors have found that the extract of cat beard and betel wax is excellent in reactive oxygen scavenging action, histamine release inhibitory action, hyaluronidase inhibitory action and antibacterial action, and in stability. I found out. Furthermore, the topical skin preparation containing an extract selected from one or two types of cat beard and betel wax is found to be safe and excellent in preventing skin aging, rough skin and acne, and to complete the present invention. It came.

  That is, this invention is a skin external preparation characterized by containing the extract of a cat beard and / or betel wax.

  The cat beard (scientific name: Orthosiphon staminium Benth) used in the present invention is a Labiatae plant. Areca (Areca catebu L.) is a palm family plant. These are mainly distributed in Southeast Asia and are widely used as herbal medicines.

  The extract of the cat beard used in the present invention is extracted from a part of the plant body such as the leaves, stems, flowers, roots or the whole plant, but is not particularly limited, and is appropriately selected according to the purpose. Just choose. The extraction method is not particularly limited, and for example, it may be extracted by heating or may be extracted at room temperature.

  The extract of betel wax used in the present invention is one obtained by extracting a part of a plant body such as the above-mentioned leaf, stem, bark, fruit, or two or more parts, but is not particularly limited, What is necessary is just to select suitably according to the objective. The extraction method is not particularly limited, and for example, it may be extracted by heating or may be extracted at room temperature.

  Examples of the solvent to be extracted include water, lower alcohols (methanol, ethanol, 1-propanol, 2-propanol, 1-butanol, 2-butanol, 1-heptanol, 2-heptanol, etc.), liquid polyhydric alcohol (propylene) Glycol, glycerin, 1,3-butylene glycol, etc.), ketones (acetone, methyl ethyl ketone, etc.), acetonitrile, esters (ethyl acetate, butyl acetate, etc.), hydrocarbons (hexane, heptane, liquid paraffin, etc.), ethers (Ethyl ether, propyl ether, tetrahydrofuran, etc.). Preferred are polar solvents such as water, lower alcohols and liquid polyhydric alcohols, and particularly preferred are water, ethanol, propylene glycol and 1,3-butylene glycol. These solvents may be used alone or in combination of two or more.

  The said extract may be used with the extracted solution as it is, and may be used after processing, such as concentration, dilution, and filtration, as needed. Further, the extracted solution may be subjected to a treatment such as concentration to dryness, spray drying, freeze drying, etc., and used as a dried product.

  In the external preparation for skin of the present invention, the above extract may be used as it is, and within the range not impairing the effect of the extract, oils and fats, waxes and hydrocarbons which are components used in normal external preparations , Fatty acids, alcohols, esters, surfactants, metal soaps, pH adjusters, preservatives, fragrances, moisturizers, powders, UV absorbers, thickeners, dyes, antioxidants, whitening agents, chelates Components such as an agent can also be blended.

  The external preparation for skin of the present invention can be used for any of cosmetics, quasi-drugs, and pharmaceuticals. Examples of the dosage form include skin lotion, cream, emulsion, gel, aerosol, ointment, and poultice. , Essence, pack, cleaning agent, bath preparation, foundation, dusting powder, lipstick, and the like.

  The amount of the extract used in the present invention is 0.0001% by weight or more, preferably 0.001 to 10% by weight in terms of solid matter, based on the total amount of the external preparation for skin of the present invention. If it is less than 0.0001% by weight, a sufficient effect is hardly expected. When it exceeds 10% 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.

  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 Neko Beard Add 400 mL of purified water to 20 g of the dried product of the entire chapter of Neko No mustache, extract at 95-100 ° C. for 2 hours, filter, concentrate the filtrate, freeze dry, 2.4 g of water extract was obtained.

Production Example 2 50% Ethanol Extract of Cat Beard Beard 1 kg of purified water and 1 kg of ethanol were added to 100 g of dried cat whole mustard plant, extracted at room temperature for 7 days, filtered, and the filtrate was concentrated to dryness. 6.4 g of% ethanol extract was obtained.

Production Example 3 1,3-Butylene Glycol Extract of Cat Beard Beard 1 kg of 1,3-Butylene Glycol was added to 100 g of dried Nekono Beard whole plant, extracted at room temperature for 7 days, filtered, and filtered. 900 g of extract was obtained.

Production Example 4 Betel wax hot water extract 20 g of dried betel wax seeds were extracted in the same manner as in Production Example 1 to obtain 1.8 g of betel wax hot water extract.

Production Example 5 50% Ethanol Extract of Betel Nut 100g of dried betel seed was extracted in the same manner as in Production Example 2 to obtain 8.1g of 50% ethanol extract of pin wax.

Production Example 6 1,3-Butylene Glycol Extract of Betel Nut 100 g of dried beeswax seeds were extracted in the same manner as in Production Example 3 to obtain 900 g of Betel Nut 1,3-butylene glycol extract.

Example 1 Cream 1
Formulation amount
1. Nekono Beard hot water extract (Production Example 1) 1.0 part
2. 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 monostearate 2.5
10. Fragrance 0.1
11. 1,3-Butylene glycol 8.5
12. Ethyl paraoxybenzoate 0.05
13. Methyl paraoxybenzoate 0.2
14. Make the total amount to 100 with purified water [Production method] Components 2 to 9 are dissolved by heating and mixed, and kept at 70 ° C to obtain an oil phase. Ingredients 1 and 11-14 are dissolved by heating and mixed, and kept at 75 ° C. to form an aqueous phase. Add the water phase to the oil phase, emulsify, cool with stirring, add component 10 at 45 ° C, and cool to 30 ° C to make the product.

Example 2 Cream 2
A cream 2 was obtained by replacing the hot water extract of the cat beard with the hot water extract of betel wax (Production Example 4) in Example 1.

Comparative Example 1 Conventional Cream A conventional cream was prepared by replacing the hot water extract of Nekonohige with purified water in Example 1.

Example 3 Formulation for lotion
1. 50% ethanol extract of Nekonohige (Production Example 2) 0.1 part
2. Betel wax 50% ethanol extract (Production Example 5) 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. Perfume appropriate amount
12. Make the total amount to 100 with purified water [Production method] Components 1-7 and 12 and components 8-11 are uniformly dissolved, mixed and filtered to make a product.

Example 4 Emulsion Formulation Amount
1. 1,3-butylene glycol extract of cat beard (Production Example 3) 0.5 part
2. 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. Make the total amount to 100 with purified water [Production method] Components 2 to 7 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. Add the aqueous phase to the oil phase, emulsify, cool with stirring, add component 9 at 45 ° C, and cool to 30 ° C to make the product.

Example 5 Gel formulation formulation
1. Betel wax hot water extract (Production Example 4) 0.05 parts
2. Ethanol 5.0
3. Methyl paraoxybenzoate 0.1
4. Polyoxyethylene hydrogenated castor oil (60E.O.) 0.1
5. Perfume appropriate amount
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. Make the total amount 100 with purified water [Manufacturing method] Components 2 to 5 and components 1 and 6 to 11 are uniformly dissolved and mixed to make a product.

Example 6 Ointment Formulation Amount
1. Nekono Beard hot water extract (Production Example 1) 1.0 part
2. 1,3-butylene glycol extract of cat beard (Production Example 3) 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. Make the total amount to 100 with purified water [Production method] Components 3 to 6 are heated and dissolved and mixed, and kept at 70 ° C to form 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. Add the water phase to the oil phase, emulsify, and cool to 30 ° C with stirring to make the product.

Example 7 Pack formulation
1. 50% ethanol extract of betel wax (Production Example 5) 0.1 part
2. Betel wax hot water extract (Production Example 4) 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 (20E.O.) 0.5
8. Citric acid 0.1
9. Sodium citrate 0.3
10. Perfume appropriate amount
11. Make the total amount to 100 with purified water. [Production method] Ingredients 1 to 11 are uniformly dissolved to make a product.

Example 8 Foundation formulation
1. Betel wax 1,3-butylene glycol extract (Production Example 6) 1.0 part
2. Stearic acid 2.4
3. Polyoxyethylene sorbitan monostearate (20E.0.) 1.0
4. Polyoxyethylene cetyl ether (20E.0.) 2.0
5. Cetanol 1.0
6. Liquid lanolin 2.0
7. Liquid paraffin 3.0
8. Isopropyl myristate 6.5
9. Butyl paraoxybenzoate 0.1
10. Carboxymethylcellulose sodium 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. Perfume appropriate amount
20. Make the total amount to 100 with purified water [Production method] Components 2 to 9 are heated and dissolved, and kept at 80 ° C to form an oil phase. Swell component 10 well with component 20, then add components 1 and 11-14 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. Add the oil phase to this aqueous phase with stirring, cool, add component 19 at 45 ° C, and cool to 30 ° C with stirring to make the product.

Example 9 Formulation for bath preparation
1. 50% ethanol extract of Nekonohige (Production Example 2) 5.0 parts
2. Sodium bicarbonate 50.0
3. Yellow No. 202 (1) Appropriate amount
4. Perfume appropriate amount
5. Make the total amount 100 with anhydrous sodium sulfate. [Production method] Ingredients 1-5 are mixed uniformly to make a product.

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

Experimental Example 1 Active oxygen scavenging action (antioxidant action)
Using the extracts of Production Examples 1, 2, 4, and 5 as samples, the scavenging action of superoxide, which is a kind of active oxygen, was measured. SOD was used as a positive control. Further, in order to confirm the stability of the sample, the same measurement was performed using a solution obtained by heating an aqueous solution of the sample at 95 ° C. for 1 hour.

Method for measuring the rate of elimination of active oxygen 0.45 mL of coloring reagent (0.24 mM nitroblue tetrazolium, 0.1 M phosphate buffer containing 0.4 mM xanthine; pH 8.0) and 0.45 mL of enzyme solution (0.1 U / mL xanthine oxidase) was added and reacted at 37 ° C. for 20 minutes to form diformazan. After adding 1.0 mL of a reaction stop solution (69 mM sodium dodecyl sulfate aqueous solution) to this solution, the absorbance (At) at a wavelength of 560 nm was measured. Similarly, a blank solution (0.1 M phosphate buffer; pH 8.0) was added in place of the enzyme solution to cause a reaction, and the absorbance (As) was measured. On the other hand, the absorbance (Bt) and (Bs) were measured in the same manner using purified water instead of the sample solution as a control. The active oxygen elimination rate of each sample was calculated from the following equation.
Active oxygen elimination rate (%) = [1− (As−At) ÷ (Bs−Bt)] × 100

  The test results are shown in Table 1. In addition, when SOD was heated at 95 ° C. for 1 hour, the active oxygen quenching action was drastically reduced. However, the extract of cat beard shown in Production Examples 1 and 2 and the extract of betel wax shown in Production Examples 4 and 5 were almost free from the scavenging action. There was no change. From the above, the extract of cat beard and betel wax was stable and excellent in scavenging active oxygen even when heated at 95 ° C.

Experimental Example 2 Histamine release inhibitory action (anti-inflammatory action)
Using the extracts of Production Examples 1, 2, 4 and 5 as samples, the effect of suppressing histamine release was measured using mast cells collected from the abdominal cavity of male Spraque-Dawley rats. That is, the effect of inhibiting the release of histamine from mast cells by 1 μg / mL compound 48/80 was determined as the release inhibition rate. Mast cells were collected by the method of Sullivan et al. [J. Immunology, 114, 1473 (1975)], and histamine was quantified by the method of May et al. [J. Allergy, 46, 12 (1970)].

  The test results are shown in Table 2. The extract of cat beard shown in Production Examples 1 and 2 and the betel wax extract shown in Production Examples 4 and 5 were found to have an excellent histamine release inhibitory action.

Experimental Example 3 Hyaluronidase inhibitory action (anti-aging action)
The extracts of Production Examples 1, 2, 4 and 5 were measured for hyaluronidase inhibitory activity according to a method applying the Morgan-Elson method [Food Hygiene Journal, 31, 3 (1990)]. Specifically, 175 mL of 0.1 M acetate buffer (pH 4.0) was added to the sample solution, and the enzyme activity of hyaluronidase was 400 U / mL, the concentration of hyaluronic acid was 0.4 mg / mL, and compound 48/80 of the activator was 0.06 mg / mL. After adjusting the total volume to 500 mL, the hyaluronidase reaction was carried out at 37 ° C. for 40 minutes. After the reaction, p-dimethylaminobenzaldehyde reagent was added for color development, and the absorbance at 585 nm was measured. Moreover, the inhibitory action of each sample was calculated by the inhibition rate calculated | required from the following formula. For the control, purified water was used instead of the sample, and purified water was used instead of hyaluronidase as a blank.
Inhibition rate (%) = [1- (C−D) / (A−B)] × 100
A: Absorbance at 585 nm of control (OD585)
B: Control blank OD585
C: OD585 of sample
D: OD585 of sample blank

  These test results are shown in Table 3. An excellent hyaluronidase inhibitory action was observed in the extract of cat beard shown in Production Examples 1 and 2 and the extract of betel wax shown in Production Examples 4 and 5.

Experimental Example 4 Antibacterial Test For the extracts of Production Examples 1, 2, 4 and 5, the minimum growth inhibitory concentration was measured according to the revised method of Chemotherapy Society of Japan (Chemotheraphy, 29, 76 (1981)). That is, one platinum loop of the bacterial solution was smeared on a test medium containing a sample of each concentration and then cultured to confirm the presence or absence of bacterial growth. The test bacteria used were Staphylococus aureus FDA209P and acne bacteria (Propionibacterium acnes GA15419), which cause acne and pimples. Preparation of bacteria solution, for Staphylococcus aureus in Mueller-Hinton (MH) broth, in GAM broth for P. acnes, 37 ° C., with those grown for 24 hours, so as to be 10 ⁶ cells / mL before use Diluted and prepared. In addition, the test medium and culture conditions were 37 ° C. for 24 hours using MH agar for S. aureus, and 37 ° C. for 48 hours using GAM agar under anaerobic conditions for acne.

  The test results are shown in Table 4. The anti-bacterial activity was confirmed against the Staphylococcus aureus and the Acne fungus in both the extract of the cat beard shown in Production Examples 1 and 2 and the extract of betel wax shown in Production Examples 4 and 5.

Experiment 5 Use test 1
Using the cream 1 of Example 1, the cream 2 of Example 2, and the conventional cream of Comparative Example 1, a use test for one month was conducted for 30 women (30 to 45 years old). After use, a questionnaire survey was conducted to comprehensively determine the effects of improving skin moisture, firmness and wrinkles.

  As a result, the external preparation for skin of the present invention showed an excellent effect for improving the moisture, firmness and wrinkles of the skin (Table 5). 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.

  Tests were also conducted on the lotion of Example 3, the emulsion of Example 4, the gel of Example 5, the ointment of Example 6, the pack of Example 7, the foundation of Example 8, and the bath preparation of Example 9. As a result, it was safe and excellent in improving the moisture, firmness and wrinkles of the skin.

Experiment 6 Use test 2
Using the cream 1 of Example 1, the cream 2 of Example 2, and the conventional cream of Comparative Example 1, a one month use test was conducted on 30 women (20 to 40 years old) suffering from acne and pimples. It was. After use, a questionnaire survey was conducted to comprehensively judge acne and breakthrough improvement.

  As a result, the external preparation for skin of the present invention showed an excellent effect on improving acne and pimples (Table 6). 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.

  Tests were also conducted on the lotion of Example 3, the emulsion of Example 4, the gel of Example 5, the ointment of Example 6, the pack of Example 7, the foundation of Example 8, and the bath preparation of Example 9. As a result, it was safe and excellent in improving acne and pimples.

Effect of the invention

  From the above, the extract of the cat beard and betel wax of the present invention has excellent active oxygen scavenging action, histamine release inhibiting action, hyaluronidase inhibiting action and antibacterial action, and was excellent in stability. Furthermore, the external preparation for skin containing these extracts was safe and excellent in the effects of preventing skin aging, rough skin and acne.

Claims (5)

Use of an extract of Nekosiphon stamineus in topical skin topical preparations for antibacterial activity against Propionibacterium acnes .
Use according to claim 1, characterized in that the extract is extracted using a solvent selected from one, two or more of water, lower alcohols and liquid polyhydric alcohols.
Use according to claim 1 or 2 , characterized in that the extract of the cat beard is used in an amount of 0.001 to 10% by weight.
The use according to any one of claims 1 to 3 , characterized in that the topical skin preparation also contains an extract of areca (Areca catechu).
The use according to any one of claims 1 to 4 , wherein the topical skin external preparation is a cosmetic.