JPH10330243A - Skin-whitening cosmetic - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a skin-whitening cosmetic that shows excellent melanin- formation inhibitory action and has good skin whitening effect with high safety by using an extract of a specific plant. SOLUTION: This skin-whitening cosmetic contains an extract of a plant, Zingiber zerumbet Smith, or a chemical compound, zerumbone represented by the formula. This extract is obtained by extracting leaves, roots, stems, subterranean stems or the whole body of the plant with water or a solvent as methanol, ethanol, propanol or the like or their mixed solvent. The amount of the extract is 0.0001-10 wt.% of the whole cosmetic on the dry basis. The zerumbone is obtained by extracting the plant body of Zingiber zerumbet with ethanol or the like, distilling off the solvent and purifying the residue with the column chromatography. The content of the zerumbone in the cosmetic is 0.0000001-0.1 wt.%.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a cosmetic containing a ginger extract or zerumbon. In addition, the present invention can also be used as a pharmaceutical containing a ginger extract or zerumbone.

[0002]

2. Description of the Related Art In general, skin pigmentation observed in spots, freckles, sunburn, etc. is caused by excessive production of melanin by melanin-producing cells present in the skin. For the treatment of this pigmentation, treatments using hydroquinone externally have been conventionally performed.

[0003]

However, although hydroquinone has been shown to be effective, it is sensitizing and has allergic contact dermatitis as a side effect. It is stable.

[0004] In view of such circumstances, the inventors of the present invention have conducted repeated studies to obtain cosmetics having high safety and excellent whitening effect. As a result, Hana ginger (scientific name: Zingiber zerumbet Smit)
It was found that the extract of h) or zerumbon contained in Ginger ginger exhibited a remarkable whitening effect and was extremely excellent in safety, and based on this finding, completed the present invention.

[0005]

That is, the present invention relates to a whitening cosmetic comprising a ginger extract or zerumbon contained in ginger.

The ginger used in the present invention has a scientific name of Zingiber zerumbet Smith, and its main component is zerumbon. Ordinary ginger, scientific name: Zingiber
Officinale Roscoe, which has Zingiberol, Zingiberen, etc. as its main components, the components and composition are completely different from Hana ginger, and the fragrance is completely different between Hana ginger and Ginger, so Hana ginger is distinguished from Ginger.

The zerumbone used in the present invention is a compound represented by the general formula (Chemical Formula 1).

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[0008] The ginger extract is prepared by adding leaves, roots, stems, rhizomes or whole plants of ginger to water or a solvent such as methanol, ethanol, propanol, propylene glycol, 1,3-butylene glycol, hexane or a mixture thereof. It can be obtained in the form of an extract by extracting with a solvent, or the extract can be dried to obtain in the form of a dry powder.

The amount of the ginger extract in the present invention can be 0.0001 to 10% by weight, preferably 0.01 to 1.0% by weight, as a dry matter, based on the total amount of the cosmetic of the present invention. If the concentration is less than 0.0001%, sufficient effects cannot be obtained.
If the concentration is more than weight%, no enhancement of the effect is observed, which is uneconomical.

[0010] Zerumbon consists of leaves, roots,
The stem, rhizome or whole plant is extracted with a solvent such as hexane, dichloromethane, ethyl ether, ethyl acetate, acetone, ethanol, methanol and water, preferably ethanol and methanol. Next, the residue obtained by evaporating the solvent of the obtained extract is subjected to column chromatography using silica gel, alumina, or the like with hexane, dichloromethane, ethyl ether, ethyl acetate, acetone, ethanol, methanol, water, or the like as an eluting solvent. The desired product can be obtained by purification by chromatography. In some cases, purification by recrystallization may be performed using a solvent such as hexane, dichloromethane, ethyl ether, ethyl acetate, acetone, ethanol, methanol, or water.

The amount of zerumbone in the present invention can be 0.0000001 to 0.1% by weight, preferably 0.00001 to 0.01% by weight, based on the total amount of the cosmetic of the present invention. 0.0000
When the concentration is less than 001% by weight, a sufficient effect cannot be obtained, and when the concentration is more than 0.1% by weight, no enhancement of the effect is observed, which is uneconomical.

The cosmetics of the present invention also contain components used in cosmetics and pharmaceuticals, such as other whitening agents, oily components, and ultraviolet absorbers, as long as the effects of the ginger extract and zerumbong are not impaired. Raw materials such as agents, antioxidants, water, alcohols, surfactants, thickeners, powders, and coloring materials can be blended.

The cosmetics of the present invention may be in the form of basic cosmetics such as creams, lotions, emulsions and packs, makeup cosmetics such as foundations and lipsticks, bath preparations and soaps. Also, pharmaceutical forms such as ointments and external preparations can be used.

[0014]

EXAMPLES Next, the present invention will be described in detail with reference to Examples, but the present invention is not limited thereto. The parts of the amounts shown in the examples are parts by weight.

Example 1 Hot water extract of Ginger ginger [0015] To 50 g of dried ginger ginger leaves, 1000 ml of water was added, and 100 g of water was added.
After extraction at 2 ° C. for 2 hours, the mixture was filtered, and the filtrate was concentrated and dried to obtain 1.3 g of a hot water extract of Hana ginger.

Example 2 Escherichia ginger ethanol extract 900 ml of water was added to 100 g of dried whole ginger of Hana ginger.
After extraction at 0 ° C. for 8 hours, the mixture was filtered, and the filtrate was concentrated and dried to obtain 3.1 g of an ethanol extract of Hana ginger.

Example 3 Hana-ginger 1,3-butylene glycol extract To 30 g of dried ginger and stem leaves, 1000 ml of a mixture of 1,3-butylene glycol and water (1: 1) was added. After extraction at room temperature for 5 days, the mixture was filtered to obtain 995 g of Ginger ginger 1,3-butylene glycol extract.

Example-4 850 g of a dried rhizome of zerumbon hana ginger was ground and extracted with 2000 ml of methanol at room temperature for 7 days. After drying the extract under reduced pressure, silica gel chromatography (Wakogel C-20)
0) and a mixture of ethyl acetate and hexane (1: 1
Elution was performed in 5) to obtain 4.5 g of zerumbon.

Example-5 100 g of dried whole plant of Zerombom Hana ginger is ground and extracted with 300 ml of ethanol at 70 ° C. for 8 hours. After drying the extract under reduced pressure, silica gel chromatography (Wakogel C-20)
0) and a mixture of ethyl acetate and hexane (1: 1
Elution was performed in 5) to obtain 0.8 g of zerumbon.

Example-6 Lotion-1 Formulation Formulation amount 1. Ethanol 5.0 parts 2. Methyl parahydroxybenzoate 0.1 3. Polyoxyethylene (40) hydrogenated castor oil 0.1 4. Perfume proper amount 5. Purified water 10.0 6. Execution Hana ginger extract of Example 1 0.1 7.1,3-butylene glycol 3.0 8. Glycerin 2.0 9. Xanthan gum 0.02 10. Purified water 79.5 Production method: Components 1 to 5 and Components 6 to 10 are uniformly dissolved, mixed, and filtered. And make it a product.

Example-7 Lotion-2 Formulation Formulation amount 1. Ethanol 5.0 parts 2. Methyl parahydroxybenzoate 0.1 3. Polyoxyethylene (40) hydrogenated castor oil 0.1 4. Perfume proper amount 5. Purified water 10.0 6. Execution Zerumbone of Example 4 0.01 7.1,3-butylene glycol 3.0 8. Glycerin 2.0 9. Xanthan gum 0.02 10. Purified water 79.5 Production method: Components 1 to 5 and Components 6 to 10 are uniformly dissolved, mixed and filtered to obtain a product. And

Comparative Example 1 Conventional Lotion A product obtained by replacing purified Ginger in Example 6 with purified water.

Example-8 Cream Formulation Formulation amount 1. Liquid paraffin 6.5 parts 2. Vaseline 10.0 3. Stearic acid 4.0 4. Cetyl alcohol 3.0 5. Stearyl alcohol 1.0 6. Polyoxyethylene (25) monostearate 3.0 7. Sorbitan monostearate 2.5 8.1,3-butylene glycol 5.0 9. Potassium hydroxide 0.1 10. Hana ginger extract of Example 2 1.0 11. Methyl paraoxybenzoate 0.2 12. Purified water 63.5 13. Appropriate perfume Production method: oil phase Components 1 to 7 and aqueous phase components 8 to 12 are heated and dissolved at 70 to 75 ° C, respectively, and then the aqueous phase components
Add 8 to 12 to emulsify, add and mix component 13 while cooling, and cool to 30 ° C to obtain a product.

Example-9 Emulsion-1 Formulation Formulation amount 1. Liquid paraffin 8.0 parts 2. Squalane 2.0 3. Stearyl alcohol 2.0 4. Sorbitan monooleate 2.5 5. Glycerin monostearate 2.3 6. Polyoxyethylene (10) sorbitan Monooleate 0.8 7. Glycerin 6.0 8. Antelope ginger extract of Example 3 0.1 9. Methyl parahydroxybenzoate 0.2 10. Purified water 76.0 11. Appropriate amount of perfume Production method: Oil phase components 1 to 6 and aqueous phase components 7 to 10 After heating and dissolving each to 70-75 ° C, the aqueous phase components 1-6
Add 7 to 10 to emulsify, add component 11 while mixing, mix and cool to 30 ° C to obtain a product.

Example-10 Emulsion-2 Formulation Compounding amount 1. Liquid paraffin 8.0 parts 2. Squalane 2.0 3. Stearyl alcohol 2.0 4. Sorbitan monooleate 2.5 5. Glycerin monostearate 2.3 6. Polyoxyethylene (10) sorbitan Monoolate 0.8 7. Glycerin 6.0 8. Zerumbone of Example 5 0.001 9. Methyl paraoxybenzoate 0.2 10. Purified water 76.0 11. Appropriate amount of fragrance Production method: Oil phase components 1 to 6 and aqueous phase components 7 to 10 are each 70. After heating and melting at ~ 75 ° C, the aqueous phase component is added to the oil phase component
Add 7 to 10 to emulsify, add component 11 while mixing, mix and cool to 30 ° C to obtain a product.

Comparative Example 2 Conventional Emulsion A product obtained by replacing the extract of Hana ginger with purified water in Example-9 was used.

Example-11 Pack Prescription Formulation Amount 1. Polyvinyl alcohol 12.0 parts 2. Ethyl alcohol 5.0 3.1,3-butylene glycol 8.0 4. Methyl parahydroxybenzoate 0.2 5. Polyoxyethylene (40) hydrogenated castor oil 0.5 6. Zerumbone of Example 4 0.01 7. Citric acid 0.1 8. Sodium citrate 0.3 9. Fragrance 0.1 10. Purified water 73.79 Production method: Each component is uniformly dissolved to give a product.

Example-12 Foundation Prescription Formulation amount 1.2.4 parts of stearic acid 2.polyoxyethylene (20) sorbitan monostearate 1.0 3.polyoxyethylene (20) cetyl ether 2.0 4.cetyl alcohol 1.0 5.liquid lanolin 2.0 6. Liquid paraffin 3.0 7. Isopropyl myristate 6.5 8. Butyl paraoxybenzoate 0.1 9. Purified water 58.2 10. Hana ginger extract of Example 1 0.01 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 oxide 8.0 17. Talc 4.0 18. Color pigment 5.0 19. Perfume qs Production method: Components 10 to 13 and 15 are heated to 70 ° C to swell well. Components 9 and 14 are dissolved in this to form an aqueous phase. Components 1 to 8 are dissolved by heating and kept at 80 ° C. to form an oil phase. The components 16 to 18 mixed well and passed through a pulverizer are added to the aqueous phase, and the mixture is stirred with a homomixer and kept at 75 ° C. The oil phase is added to the aqueous phase with stirring, cooled, and the component 19 is added at 45 ° C., and cooled with stirring to obtain a product.

Example -13 Bath agent Prescription Compounding amount 1. Sodium sulfate 46.0 parts 2. Sodium bicarbonate 53.0 3. Zerumbon 0.001 of Example 5 4. Yellow 202 No. (1) proper amount 5. Fragrance proper amount Production method: each The components are mixed well to form a product.

Example -14 Oil-based ointment-1 Formulation Formulation amount 1. Purified lanolin 5.0 parts 2. Salami beeswax 5.0 3. Hana ginger extract of Example 2 4. White petrolatum 89.9 Production method: Mix well each component And make it a product.

Example -15 Oil-based ointment-2 Formulation Formulation amount 1. Purified lanolin 5.0 parts 2. Salami beeswax 5.0 3. Zerumbon 0.01 of Example 4 4. White petrolatum 89.99 Production method: Mixing each component well and producing a product And

Comparative Example-3 Conventional oil-and-fat ointment A product obtained by replacing the ginger extract of Example 14 with white petrolatum was used as a product.

Example -16 Emulsion ointment-1 Formulation Formulation amount 1. White petrolatum 25.0 2. Stearyl alcohol 22.0 3. Propylene glycol 12.0 4. Sodium lauryl sulfate 1.5 5. Ethyl paraoxybenzoate 0.025 6. Propyl paraoxybenzoate 0.015 7. Hana ginger extract of Example 3 0.2 8. Purified water 39.26 Production method: Oil phase components 1-2 and aqueous phase components 3-8
After heating and melting at 70-75 ° C, the aqueous phase component 3
Add ~ 8 to emulsify and cool to 30 ° C to make the product.

Example -17 Emulsion ointment-2 Formulation Formulation amount 1. Cholesterol 3.0 2. Stearyl alcohol 3.0 3. Salami beeswax 8.0 4. Zerumbone 0.005 in Example 5. 5. White petrolatum 85.995 Production method: Mix each component After heating and melting at 70-75 ° C,
Cool to 30 ° C to obtain a product.

Example-18 Water-soluble ointment Formulation Formulation amount 1. Polyethylene glycol 4000 (PEG 4000) 49.9 2. Polyethylene glycol 400 (PEG 400) 49.9 3. Hana ginger extract of Example 1 0.2 Production method: Dissolve uniformly to form a product.

Example-19 Lotion Formulation Formulation Amount 1. Stearyl alcohol 2.5 2. Liquid paraffin 25.0 3. Sodium lauryl sulfate 1.0 4. Propylene glycol 12.0 5. Methyl parahydroxybenzoate 0.025 6. Propyl paraoxybenzoate 0.025 7. Implementation Zerumbon of Example 4 0.01 8. Purified water 59.44 Production method: Oil phase components 1 and 2 and aqueous phase components 3 to 8 were heated and dissolved at 70 to 75 ° C., respectively, and then aqueous phase components were added to oil phase components 1 and 2.
Add 3 to 8 to emulsify and cool to 30 ° C to obtain a product.

[0037]

Industrial Applicability The ginger extract or zerumbon of the present invention has excellent melanin production-suppressing and whitening effects. Next, the effects of the cosmetic and whitening agent of the present invention will be described in more detail with reference to experimental examples.

Experimental Example 1 Melanin Production Inhibition Test Using B16 Mouse Melanoma A melanoma in a logarithmic growth phase was seeded on a 60 mm dish at 2 × 10 ⁴ cells, and the melanoma was adjusted to a final concentration of 0.1, 0.3, and 1.0 mg / ml. Eagles' MEM containing ginger extract (containing 10% FCS)
Alternatively, add Eagles' MEM (containing 10% FCS) containing zerumbon to a final concentration of 0.1, 0.3, 1.0 μM, and add
The cells were cultured at 5 ° C. and 5% CO ₂ . Dish cells after 5 days of culture
After sonication of the cells, 2N NaOH was added and the cells were treated at 60 ° C. for 2 hours, and OD 475 nm was measured with a spectrophotometer. The cell lysate after sonication was quantified for protein by the method of Lowry (J. Biol. Chem., 193, 265-275, 1951), and the melanin production inhibitory effect was compared by comparing the amount of melanin per protein amount. The index was used. As a result, as shown in Table 1, the Ginger ginger extract and zerumbone showed excellent melanin production inhibitory action.

[0039]

[Table 1] Table 1 Melanin production inhibitory activity 生成 Sample Sample concentration Melanin Amount Inhibition rate (μg / mg protein) (%) ──────────────────────────────────── Control 24.5 Hana ginger extract of Example 1 0.1 mg / ml 23.0 6 0.3 mg / ml 15.2 38 1.0 mg / ml 10.2 58 ────────────────────────────────── below margin

EXPERIMENTAL EXAMPLE 2 Use Test Lotion-1 and Lotion-2 of Example-6 and Example-7, Emulsion-1 and Emulsion-2 of Example-10 and Comparative Example- Using one conventional lotion and the conventional milky lotion of Comparative Example-2, a use test for 30 months (30 to 45 years old) was performed for each of the women. After use, the whitening effect was determined by a questionnaire survey on the improvement of skin spots, freckles, transparency and dullness. As a result, the cosmetic containing the ginger extract or zerumbone exhibited an excellent whitening effect (Tables 2 to 7).

[0041]

Table 2 Whitening effect of lotion-1 of the present invention (number of persons in questionnaire results)化粧 Evaluation of the lotion of the present invention (Example-6) ────────────────────────── Very good Good Normalし Skin spots, freckles 18 9 3 Skin clarity 19 7 4 Dullness of skin 189 3 ─────────────────────────────────── or less margin

[0042]

[Table 3] Whitening effect of lotion-2 of the present invention (number of persons in questionnaire results)化粧 Lotion of the present invention (Example-7) Evaluation ────────────────────────── Very good Good Normalし Skin spots, freckles 19 9 2 Skin clarity 16 10 4 Dullness of skin 18 8 4 ───────────────────────────────────

[0043]

[Table 4] Whitening effect of conventional lotion (number of people surveyed) 結果──── Conventional lotion (Comparative Example-1) Evaluation ────────────────────────── Very good Good Normal ────し Skin spots, freckles 1 8 21 Skin clarity 3 9 18 Skin dullness 2 Margin below 919 mm

[0044]

[Table 5] Whitening effect of emulsion-1 of the present invention (number of persons in questionnaire results)乳 Emulsion of the present invention (Example-9) Evaluation ────────────────────────── Very good Good Normal ──し Skin spots and freckles 20 7 3 Skin clarity 13 13 4 Skin Dullness 197 4 ───────────────────────────────────

[0045]

Table 6 Whitening effect of the emulsion-2 of the present invention (the number of persons in the questionnaire results)乳 Emulsion of the present invention (Example-10) Evaluation ────────────────────────── Very good Good Normal ──し Skin spots, freckles 20 8 2 Skin clarity 16 10 4 Skin Dullness 198 3 ─────────────────────────────────── or less margin

[0046]

[Table 7] Table 7 Whitening effect of conventional emulsion (number of people surveyed) 結果─── Conventional emulsion (Comparative Example-2) Evaluation ────────────────────────── Very good Good Normal ──────し Skin spots and freckles 3 11 16 Skin clarity 5 8 17 Skin dullness 3 6 21 ───────────────────────────────────

Experimental Example-3 Clinical Example Example-1 for 4 patients with pigmentation after sunburn inflammation
The oily ointment-1 shown in FIG. 4 and the oily ointment-2 shown in Example-15 were applied to the affected area once a day and observed for up to three months. At the same time, the conventional oil-based ointment of Comparative Example-3 was similarly tested. Judgment of the effect is-: unchanged, +: faint, ++: almost disappeared, ++
+: Four stages of complete disappearance. No side effects were observed in all cases. As a result, as shown in Tables 8 and 9, in the oil-based ointment of Example-14 and Example-15, the effect was recognized in 3 out of 4 cases. For it,
No effect was observed in the oily ointment of Comparative Example-3 (Table 10). Below margin

[0048]

Table 8 Whitening action of oily ointment-1 of the present invention油 Oil-based ointment of the present invention (Example-14) Subject Gender Age Skin findings ───────────────────────────────男 A male 38 ++ effective B male 31 + effective C female 32 ++ effective D female 28-no effect ────────────────────── ─────────────

[0049]

TABLE 9 Whitening action of oily ointment-2 of the present invention油 Oil-based ointment of the present invention (Example-15) Subject Gender Age Skin findings ─────────────────────────────── Ｅ E male 28 ++ effective F male 30-no effect G female 38 + effective H female 31 ++ effective ────────────────────── ───────────── below margin

[0050]

[Table 10] Table 10 Whitening effect of conventional oil-based ointment ─────────────────────────────────── Conventional Oil-based ointment (Comparative Example-3) Subject Gender Age Skin findings ─────────────────────────────────── I Male 35-No effect J Male 27-No effect K Woman 30-No effect L Woman 25-No effect ────────────────────────── ─────────

Cream of Example-8, pack of Example-11, foundation of Example-12, Example-13
When a use test was carried out for the bath agent in the same manner as in Experimental Example 2, an excellent whitening effect was exhibited. Example 1
Experimental examples of emulsion ointments -1, 2 of Examples 6 and 17, water-soluble ointment of Example -18, and lotion of Example -19
When a clinical test was conducted in the same manner as in Example 3, an excellent whitening effect was exhibited.

As described above, the Ginger ginger extract and zerumbon show excellent melanin production inhibitory action,
In addition, the cosmetic containing the Ginger ginger extract or zerumbone of the present invention exhibited an excellent whitening effect and was also excellent in safety. Below margin

Claims (2)

[Claims] 1. A whitening cosmetic comprising a ginger extract. 2. A whitening cosmetic comprising zerumbon.