CA1279016C - Whitening cosmetic - Google Patents

Abstract

Abstract A whitening cosmetic is disclosed, which comprises kojic acid and cyclodextrins in addition to cosmetic base materials. The kojic acid may be included by cyclodextrins before being incorporated therein. The cosmetic has an improved stability against coloring with the lapse of time and an enhance whitening effect. The cosmetic can be a toilet lotion, a cosmetic cream, a milky lotion, a pack, etc. to be applied to the human skin.

Description

i~79016 WHITENING COSMETIC
Background of the Invention l. Field of the Invention The present invention relates to a whitening cosmetic incorporated with kojic acid. In particular, it relates to a kojic acid-containing whitening cosmetic having not only an improved stability against coloring but also an enhance whitening effect.

2. Description of the Prior Art Kojic acid, i.e., 5-hydroxy-2-hydoxymethl-y-pyrone, is a compound which can be obtained by the fermentation of fungi of, e.g., Aspergillus genus. It is known that the compound functions as an tyrosinase inhibitor.
Whitening cosmetics utilizing the function of the compound are known and disclosed in Japanese Patent Publication No. 18,569/81 and Japanese Patent Application (Laid Open) No. 3,538/78.
Whitening cosmetics, in particular cosmetic creams, containing kojic acid as an active ingredient are liable to discoloration to yellowish brown when exposed to heat or light, and the density of the cosmetics tends to be increased with the lapse of time, thus impairing their value as an article to be marketed.
~escription of the Invention It is therefore an object of the present invention ; to provide a whiteninq cosmetic having an improved stability against coloring with the lapse of time.

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lZ790~6 It is another object of the present invention to provide a whitening cosmetic having an enhanced whitening effect.
It has now been found that the colori~g can be markedly reduced and the whitening effect by kojic acid can be intensified when cyclodextrins are incorporated into a cosmetic in combination with kojic acid, or when kojic acid included by cyclodextrins is incorporated into a cosmetic.
Accordingly, there is provided by the present invention a whitening cosmetic having not only an improved stability against coloring but also an enhanced whitening effect, which comprises cyclodextrins and kojic acid, or kojic acid included by cyclodextrins.
Detailed Description of the Invention Kojic acid is a known compound obtainable by the fermentation of fungi ~belonging to such generics as Aspergillus, Penicillium, Gluconobacter, and the like.
Cyclodextrins to be used in the present invention in combination with kojic acid include a-cyclodextrin, ~-cyclodextrin and y-cyclodextrin. Of these compounds, ~-cyclodextrin can be most preferable.
Cyclodextrins can be used in an amount of from 0.5 to 10 parts by weight, per 1 part by weight of kojic acid.
Xojic acid can be included by cyclodextrins in advance to its incorporation into cosmetic base materials.

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790~6 Inclusion of kojic acid by cyclodextrins can be carried out in the following manner: Cyclodextrins are dispersed into water, and then kojic acid iS gradually added thereinto with stirring until they are completely dissolved. The thus prepared included kojic acid, or kojic acid included by cyclodextrins, may be freeze dried.
In the above preparation, there can be used 0.5 to parts by weight of cyclodextrins, per 1 part by weight of ko~ic acid. Most preferably, 4 parts by weight of cyclodextrins is used per 1 part by weight of kojic acid.
In the present invention, the combination of kojic acid and cyclodextrins or included kojic acid is incorporated into ordinary cosmetic base materials to prepare toilet waters or toilet lotions, cosmetic creams, cosmetic emulsions or milky lotion, packs, etc., which are to be applied to the human skin. KoJic acid may be incorporated into cosmetic base materials in an amount of from 0. oi to 2% by weight not only in the case where it is used together with cyclodextrins but also in the case where it is included by cyclodextrins in advance to its incorporation into base materials.
The cosmetics of the present invention may be formulated into a toilet water or a cosmetic lotion. In preparing toilet waters or cosmetic lotions according to the present invention, moisturizers, skin nutrients, etc. are dissolved into purified water, and :
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12790~6 preservatives, perfumes, etc. are dissolved into an alcohol. The two solutions are then mixed at room temperature to give desired products. Kojic acid and cyclodextrins, or kojic acid included by cyclodextrins, can be added to the aqueous phase before the said mixing in an amount as described above.
The cosmetics of thè present invention may be formed into a cream, which may be prepared as follows: Into purified water is added hydrophilic ingredients, for example, moisturizers such as glycerol and sorbitol, to form an agueous phase. An oil phase is prepared by adding olephilic ingredients, such as preservatives~and surfactants, into an oil, for example, solid oils such as bees wax, paraffins, microcrystalline wax, ceresine, higher fatty acids and hardened oils; semisolid oils such as vaseline, lanolin and glycerides; or liquid oils, such as sgualane, liquid paraffin and various ester oils. The thus prepared aqueous and oil phases are heated to the same temperature, and the latter is gradually added to the former with gradual stirring and then emulsified to form a cream. Kojic acid and cyclodextrins, or kojic acid included by cyclodextrins, can be added ~to said a~ueous phase in an amount as defined above.
The cosmetics of the present invention may also be utilized in the form of an emulsion or a milky lotion.
In this case, the cosmetics of the invention may be prepared in accordance with the following method: Into ., .

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12790~6 puriied water are added a moisturizer, such as glycerol, a pH adjuster, such as an acid and an alkali, and the like, and the resulting mixture is heated with stirring. Thereafter, ethanol is additionally added to the mixture to obtain an aqueous phase. Oily ingredients, such as preservatives and surfactants, is then added into an oil, for example, solid oils such as bees wax and paraffins; semisolid oils such as vaseline and lanolin; or liquid oils such as squalane, liquid paraffins and ester oils; and the resulting mixture is heated to give an oil phase. The oil phase is then added into the aqueous phase and subjected to a preliminary emulsification. Into the thus formed mixture is added protective colloidal agents, such as carboxyvinyl polymers and carboxymethyl cellulose, and the resulting mixture is uniformly emulsi~ied by use of a homogenizing mixer to form a desired emulsion. Kojic acid and cyclodextrins, or kojic acid included by cyclodextrins, may be added to the liquid pnase in advance to said emulsification in an amount as described above.
The cosmetics of the invention may also be prepared ~in a pack form, which may be prepared in any manner - generally utilized for the production of packs. For example, into purified water are added moisturizers, such as glycerol, etc., film-forming agents, such as polyvinyl alcohols and bee gum, and other additives.
The resulting mixture is then subjected to swelling. If - . :

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i~7go~6 desired, powders of such materials as kaolin, talc and zinc oxide may be additionally added to the mixture.
Into ethanol are dissolved perfumes, preservatives, and the like. The ethanol solution is then mixed with the swelled product, and the resulting mixture is throughly kneaded to form a paste or cream. Kojic acid and cyclodextrins, or kojic acid included by cyclodextrins, can be added in any step of the above preparation, in an amount as stated hereinabove.
Preparation examples of included kojic acid, or kojic acid included by cyclodextrins, which is the active component in the cosmetics of the present invention, will be shown hereinbelow.
Preparation Example Into 0.5 to 4 parts by weight of ~-cyclodextrin is added 1.5 to 1~ parts by weight o purified water and stirred slowly. Thereafter, 1 part by weight of kojic acid is additionally added, and the resulting mixture is throughly stirred until a uniform dispersion is formed to give included kojic acid. The thus formed included kojic acid may be freeze dried.

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Percents by weiqht 20% included kojic acid 5.0 Bees wax 6.0 Cetanol 5.8 Hydrogenated lanolin 8.0 Squalane 30.0 Glyceryl esters of fatty acids 4.0 Oleophilic glyceryl monostearate 2.0 Polyoxyethylene sorbitan monolaurate 2.0 Propylene glycol 5.0 Perfume Appropriate amount Preservative Appropriate amount Antioxidant Appropriate amount Purified water 37.20 , .. . . , -. . . - .
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1.~790~6 Example 2: A cream Percents bY weiqht ~ojic acid 1.0 ~-cyclodextrin 4.0 Bees wax ; 6.0 Cetanol 5.8 ~ydrogenated lanolin 8.0 Squalane 30.0 Glyceryl esters of fatty acids 4.0 Oleophilic glyceryl monostearate 2.0 ` Polyoxyethylene sorbitan monolaurate 2.0 : Perfume Appropriate amount : Preservative Appropriate amount Antioxidant Appropriate amount Purified water 37.20 :' ~, .

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-, 1~7gO~6 Example 3: A milky lotion _ Percents bY weiaht 30% included kojic acid 2.5 Sgualane 5.0 Vaseline 2.0 Bees wax 0.5 Sorbitan sesquioleate 0.8 Polyoxyethylene oleyl ether 1.2 Propylene glycol 5.0 Ethanol 5.0 Carboxyvinyl polymer (1~ aqueous solution)20.0 Potassium hydroxide 0.1 Perfume Appropriate amount Preservative and antioxidant Appropriate amount Purified water 57.90 _ g _ ' '' ~ ;'' ~,;' - , .' ~ ` : ' ~Z790~L6 Example q: A milky lotion Percents by weiaht Kojic acid 0.75 ~cyclodex~in 1.75 Squalane 5.0 Vaseline 2.0 Bees wax 0.5 Sorbitan sesquioleate 0.8 Polyoxyethylene oleyl ether 1.2 Propylene glycol 5.0 Ethanol 5.0 Carboxyvinyl polymer (1% aqueous solution)20.0 Potassium hydroxide 0.1 Perfume Appropriate amount Preservative and antioxidant Appropriate amount Purified water 57.90 ~' ,,' ~
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12790i6 Example 5: A pack Percents bY weiaht 50% included kojic acid 1.0 Bee gum 5.0 Squalane 2.0 Propylene glycol 5.0 Zinc oxide 10.0 Kaolin 10.0 Ethanol 5.0 Perfume Appropriate amount Preservative Appropriate amount Purified water 62.0 Example 6: A pack Percents bv weiqht Kojic acid 0.5 cyclodextrin 0.5 Bee gum 5.0 Squalane 2.0 Propylene glycol 5.0 Zinc oxide 10.0 Kaolin 10.0 Ethanol 5.0 Perfume Appropriate amount Preservative Appropriate amount Purified water 62.0 . -- 11 --. ~. -~, ~ , . , : .

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~Z790~6 Example g: Test for coloring-preventing efects attainable by the active components of the invention (1) Samples A: A cream prepared in Example 1, incorporated with 5% by weight of 20% included kojic acid (i.e., 1% by weight as kojic acid) 8: A cream prepared in Example 2, incorporated with 1~ by weight of kojic acid and 4% by weight of ~-cyclodextrin C: A cream incorporated with 1% by weight of kojic acid but not incorporated with cyclodextrins (2) Method of test The samples, A, B and C were allowed to stand for 2 months at a temperature of 45C, and their lightness (L), redness (a), yellowness (b) and A E (color difference) were measured and compared with a control sample stored at a temperature OL 5C for the same period of time, using Color Difference Meter Z-1001 DP
produced by Nippon Denshoku Co., Ltd.
(3) Results of the test Results obtained are shown in Table 1.

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12790~6 It would be apparent from the results shown in Table 1 that Samples A and B, or cosmetics according to the present invention, have markedly reduced colorings compared with Sample C, in which kojic acid alone was incorporated.
Example 10: Test of decoloring effect in cultured dye-producing cells ( 1 ) Samples A: Kojic acid B: 20% included kojic acid prepared in Preparation Example C: Kojic acid and ~-cyclodextrin D: ~-cyclodextrin (2) Method of test The mouse melanoma B16 cells were cultured in the Eagle's MEM medium containing 10% fetal bovine serum and:
1) 2.5 mM of kojic acid [Test area A];
2) 2.5 mM (reduced to kojic acid) of 20% included kojic acid (or kojic acid included by cyclodextrins at a percentage of 20%) prepared in the Preparation Example [Test area B];
3) Xojic acid and ~-cyclodextrin each in the same amount as used in Test area B [Test area C];
4) ~-cyclodextrin in the same amount as that of ~-cyclodextrin contained in the inclusion compound ; used in Test area B [Test area D]; or 5) Nothing [Test area E].

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. : , ' -~ . , - The samples were cultured at 37C for 6 days in an atmosphere consisting of 5~ of CO2 and 9s% of air, then treated with tripsin, and subjected to centrifugation for 5 minutes at 2000 rpm to prepare cell pellets. The darkness of the thus prepared pellets were compared with the naked eyes.
(3) Results of test Test area A showed a moderate fading, compared with Test area E (control).
Test areas B and C showed fading apparently stronger than that in Test area A, and the pellets obtained from these areas were white to light yellow in color.
Test area D showed no fading.
It would be apparent from the above results that the active components of the present invention, namely included kojic acid and the combination of kojic acid - and cyclodextrins, have effects of inhibiting the formation of melanine dyes, compared with the case where kojic acid alone was used.

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Claims (12)

1. A whitening cosmetic comprising cosmetic base materials, kojic acid and cyclodextrins.

2. A whitening cosmetic as claimed in claim 1, wherein said kojic acid is included in said cyclodextrins.

3. A whitening cosmetic as claimed in claim 1, wherein said kojic acid is incorporated in an amount of 0.01 to 2% by weight, based on the total weight of said cosmetic.

4. A whitening cosmetic as claimed in claim 1, wherein said whitening cosmetic is a cosmetic cream.

5. A whitening cosmetic as claimed in claim 1, wherein said whitening cosmetic is a milky lotion.

6. A whitening cosmetic as claimed in claim 1, wherein said whitening cosmetic is a pack.

7. A whitening cosmetic as claimed in claim 1, wherein said whitening cosmetic is a toilet lotion.

8. A whitening cosmetic comprising cosmetic base materials, from 0.01 to, 2% by weight of kojic acid based on the total weight of the cosmetic and from 0.5 to 10 parts by weight of cyclodextrin per 1 part by weight of said kojic acid.

9. A cosmetic as in claim 8, wherein the cyclodextrin is .beta.- cyclodextrin.

10. A cosmetic as in claim 8, wherein the kojic acid is included in the cyclodextrin.

11. A cosmetic as in claim 8, wherein 4 parts by weight of cyclodextrin are present per 1 part by weight of kojic acid.

12. A cosmetic as in claim 8, wherein said cosmetic is selected from the group consisting of a cosmetic cream, a cosmetic emulsion, a milky lotion, a pack, a toilet water, and a toilet lotion.