JPH0987159A - Skin lightening cosmetic - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a melanin production inhibitor excellent in skin lightening action. SOLUTION: This melanin production inhibitor comprises a complex of an oligogalacturonic acid as a pectin of the formula (M is a transition metal ion; (n), (o) and (p) are each 0 or a natural number) or its hydrolyzate and a transition metal. The oligogalacturonic acid is obtained by hydrolyzing a pectin with an enzyme and separating by ultrafiltration, etc., and purified to have 1-10 degree of polymerization. The equivalent ratio of the oligogalacturonic acid to the transition metal used in the complex is 1:2 to 1:6. The objective skin lightening cosmetic can be prepared by using 0.01-10wt.% of the melanin production inhibitor. The melanin production inhibitor can suppress formed melanin and lighten skin.

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to a whitening cosmetic composition.

[0002]

2. Description of the Related Art White and beautiful skin has been a dream of mankind for many years.
When born, white, fresh skin becomes darkened due to the deposition of pigments over time. The cause of this is the production of melanin by melanocytes. By suppressing the production of melanin by this melanocyte, or by removing the produced melanin, it is possible to restore darkened skin to white and beautiful skin.

From this point of view, various whitening substances have been developed. For example, although vitamin C derivatives and hydroquinone derivatives have been developed, it was hard to say that they are sufficient in terms of stability, bioavailability or their effect. That is, a novel melanin production inhibitor has been demanded.

On the other hand, it was known that the complex of pectin or its hydrolyzate with a transition metal has a mineral absorption promoting action, but it was not known that it has a melanin production inhibiting action.

[0005]

The present invention has been made under these circumstances, and an object thereof is to provide a novel melanin production inhibitor.

[0006]

In view of such a situation,
As a result of repeated screening of various compounds using the melanin production inhibitory action as an index, the present inventors have found an excellent melanin production inhibitory action in the complex of pectin and its hydrolyzate and a transition metal, and completed the discovery.
Hereinafter, the invention will be described in detail.

(1) Melanin production inhibitor of the present invention The melanin production inhibitor of the present invention comprises a complex of oligogalacturonic acid and a transition metal, which is pectin represented by the general formula (I) or a hydrolyzate thereof. Become. Of these, oligogalacturonic acid can be easily obtained by hydrolyzing pectin with an enzyme and separating it by ultrafiltration. Further, if this product is purified by gel filtration or the like, it can be separated and purified for each degree of polymerization.

[0008]

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The thus-obtained oligogalacturonic acid and a salt of a transition metal such as hydrochloride or nitrate are mixed in a solution to obtain the active oxygen scavenger of the present invention. The transition metal is not particularly limited, but iron, manganese, cobalt,
Nickel, copper, etc. can be exemplified, and among these, iron is most preferable. The composition ratio (equal ratio) of oligogalacturonic acid and transition metal in the complex is preferably 1: 2 to 1: 6, more preferably 1: 3 to 1: 5. This is because the melanin production inhibitory action is impaired if biased to either direction.

(2) Whitening Cosmetic of the Present Invention The whitening cosmetic of the present invention is characterized by containing the above-mentioned melanin production inhibitor. The preferred content of the melanin production inhibitor in the whitening cosmetic composition of the present invention is 0.01 to
It is 10% by weight. This is because if the amount is too large, the effect may reach the ceiling, and if it is too small, the effect may not be expected. The more preferable content is 0.05 to 1% by weight, at which the effect is efficiently exhibited.

The whitening cosmetic composition of the present invention may contain various optional components usually used in cosmetics, in addition to the melanin production inhibitor. As such optional ingredients, as optional ingredients, for example, hydrocarbons such as petrolatum and squalane, esters such as jojoba oil and gallow, beef tallow, triglycerides such as olive oil, stearic acid, fatty acids such as oleic acid, cetanol, Higher alcohols such as oleyl alcohol, nonionic surfactants, anionic surfactants, cationic surfactants, amphoteric surfactants, polyhydric alcohols, water-soluble polymers, ethanol, preservatives, UV absorbers, antioxidants Agents, various vitamins, medicinal ingredients, fragrances, coloring agents, powders and the like. Furthermore, ascorbic acid and its derivatives, hydroquinone derivatives, glutathione derivatives, and the like, which have already been known to suppress melanin production, can be contained.

[0012]

BEST MODE FOR CARRYING OUT THE INVENTION Hereinafter, the present invention will be described in more detail with reference to embodiments of the present invention, but it goes without saying that the present invention is not limited to these examples. In addition, the numerical value of a prescription represents a weight part.

Production Example To 1 kg of pectin, 5 liters of water and 5 g of pectinase were added and hydrolyzed by stirring at 37 ° C. for 2 hours. This was ultrafiltered to obtain 123 g of oligogalacturonic acid (crude solution). This is gel filtered and concentrated to give 30 galacturonic acid.
g, dimer 11 g, trimer 8 g, tetramer 5 g, pentamer 7
g, hexamer 5 g, heptamer 4 g, and octamer 3 g were obtained. The same weight of ferrous chloride was added to these as a 5% aqueous solution, and the mixture was stirred at room temperature for 1 hour and then concentrated to give 59 g of each complex (iron oligogalacturonic acid complex,
Melanin production inhibitor 1), 21 g (oligogalacturonic acid dimer iron complex, melanin production inhibitor 2), 16 g (oligogalacturonic acid trimer iron complex, melanin production inhibitor 3), 8 g (oligo Galacturonic acid tetramer iron complex, melanin production inhibitor 4), 13 g (oligogalacturonic acid pentamer iron complex, melanin production inhibitor 5), 10 g (oligogalacturonic acid hexamer iron complex, Melanin production inhibitor 6), 8 g (oligogalacturonic acid heptameric iron complex, melanin production inhibitor 7), 5 g (oligogalacturonic acid octamer iron complex, melanin production inhibitor 8) were obtained.

(Formulation Example 1) Whitening lotion The following prescription ingredients were weighed and dissolved by stirring at room temperature to obtain a lotion. Glycerin 10 1,3-butanediol 5 Ethanol 15 POE (60) hydrogenated castor oil 0.1 Melanin production inhibitor 1 0.1 Perfume 0.1 Arbutin 0.1 Benzalkonium chloride 0.1 Water 69.5

(Formulation Example 2) Whitening lotion The following prescription ingredients were weighed and dissolved under stirring at room temperature to obtain a lotion. Glycerin 10 1,3-butanediol 5 Ethanol 15 POE (60) hydrogenated castor oil 0.1 Melanin production inhibitor 2 0.1 Perfume 0.1 Arbutin 0.1 Benzalkonium chloride 0.1 Water 69.5

(Formulation Example 3) Whitening Cosmetic The following prescription ingredients were weighed and dissolved under stirring at room temperature to obtain a lotion. Glycerin 10 1,3-butanediol 5 Ethanol 15 POE (60) hydrogenated castor oil 0.1 Melanin production inhibitor 3 0.1 Perfume 0.1 Arbutin 0.1 Benzalkonium chloride 0.1 Water 69.5

(Formulation Example 4) Whitening cosmetics The following ingredients were weighed and dissolved at room temperature with stirring to obtain a lotion. Glycerin 10 1,3-butanediol 5 Ethanol 15 POE (60) hydrogenated castor oil 0.1 Melanin production inhibitor 4 0.1 Perfume 0.1 Arbutin 0.1 Benzalkonium chloride 0.1 Water 69.5

(Formulation Example 5) Whitening Cosmetics The following ingredients were weighed and dissolved at room temperature with stirring to obtain a lotion. Glycerin 10 1,3-butanediol 5 Ethanol 15 POE (60) hydrogenated castor oil 0.1 Melanin production inhibitor 5 0.1 Perfume 0.1 Arbutin 0.1 Benzalkonium chloride 0.1 Water 69.5

(Formulation Example 6) Whitening cosmetics The following ingredients were weighed and dissolved at room temperature with stirring to obtain a lotion. Glycerin 10 1,3-butanediol 5 Ethanol 15 POE (60) hydrogenated castor oil 0.1 Melanin production inhibitor 6 0.1 Perfume 0.1 Arbutin 0.1 Benzalkonium chloride 0.1 Water 69.5

(Formulation Example 7) Whitening Cosmetic The following prescription ingredients were weighed and dissolved at room temperature with stirring to obtain a lotion. Glycerin 10 1,3-butanediol 5 Ethanol 15 POE (60) hydrogenated castor oil 0.1 Melanin production inhibitor 7 0.1 Perfume 0.1 Arbutin 0.1 Benzalkonium chloride 0.1 Water 69.5

(Formulation Example 8) Whitening Cosmetic The following prescription ingredients were weighed and dissolved at room temperature with stirring to obtain a lotion. Glycerin 10 1,3-butanediol 5 Ethanol 15 POE (60) hydrogenated castor oil 0.1 Melanin production inhibitor 8 0.1 Perfume 0.1 Arbutin 0.1 Benzalkonium chloride 0.1 Water 69.5

(Formulation Example 9) Whitening Cosmetic The following prescription ingredients were weighed and dissolved at room temperature with stirring to obtain a lotion. Glycerin 10 1,3-butanediol 5 Ethanol 15 POE (60) hydrogenated castor oil 0.1 Melanin production inhibitor 1 0.05 Melanin production inhibitor 2 0.05 Perfume 0.1 Arbutin 0.1 Benzalkonium chloride 0.1. 1 water 69.5

(Formulation Example 10) Whitening cosmetics The following ingredients were weighed and dissolved at room temperature with stirring to obtain a lotion. Glycerin 10 1,3-butanediol 5 Ethanol 15 POE (60) Hydrogenated castor oil 0.1 Melanin production inhibitor 3 0.05 Melanin production inhibitor 4 0.05 Perfume 0.1 Arbutin 0.1 Benzalkonium chloride 0.1. 1 water 69.5

(Formulation Example 11) Whitening emulsion A whitening emulsion was prepared according to the following formulation. That is, A,
Each of B and C was weighed and dissolved by heating at 80 ° C., B was gradually added to A, and further C was gradually added to coarsely emulsify. This was uniformly emulsified with a homogenizer, stirred and cooled to obtain an emulsion. (A) Vaseline 10 Stearyl alcohol 3 Stearic acid 1 POE (45) Stearic acid ester 2 Butylparaben 0.1 Perfume 0.1 (B) Potassium hydroxide 0.2 Water 50 (C) Melanin production inhibitor 5 0.5 Melanin production inhibitor 6 0.5 Carbopol 0.2 1,3-Butanediol 8 Methylparaben 0.2 Water 24.2

(Formulation Example 13) Whitening powder A whitening powder was prepared according to the following formulation.
That is, the prescription ingredients were weighed and weighed in a Hensyl mixer, mixed at low speed for 1 minute, pulverized by a pulsarizer equipped with a 1 mm herringbone screen, filled in a metal plate and pressure-molded to obtain a whitening powder. Titanium oxide 10 Talc 30 Sericite 30 Lactose 20 Melanin production inhibitor 7 5 Melanin production inhibitor 8 5

[0026]

【Example】

Example 1 Melanin production inhibitory effect Melanin production inhibitor 1 of the present invention prepared in the above Production Example 1
Regarding 8, the melanin production inhibitory action was confirmed using melanoma B-16 cells. That is, melanoma B-16 in the logarithmic growth phase was treated with trypsin, and then added to MEM medium containing fetal bovine serum (FBS) at a concentration of 1.5 × 10 ³ cells / ml.
An M suspension was prepared. Dispense 10 ml of this suspension into 4 culture bottles for each sample,
The cells were placed in a 5% carbon dioxide gas incubator and cultured for 2 days. After that, the final concentration of the sample is 0.1 in 3 bottles.
%, 0.01%, and 0.001% were added as 5 ml of phosphate buffered saline solution. To the remaining one, only 5 ml of phosphate buffered saline was added to serve as a control. These bottles were cultured at 37 ° C. in a 5% carbon dioxide gas incubator for 2 days. Then, 15 ml of FBS-containing MEM was added to the culture bottle, and the final concentration of the specimen was 0.1%, 0.01%, 0.
5 ml of phosphate buffered saline solution was added so that the concentration would be 001%. To the remaining one, only 5 ml of phosphate buffered saline was added. This was further cultured for 2 days. After the culture was completed, the medium was removed from the bottle, washed with phosphate buffered saline, and then trypsinized to detach the cells from the culture bottle to obtain a cell suspension. The cell suspension was centrifuged to collect the cells. The cytotoxicity was determined from the number of cells obtained, and the melanin production inhibition value was determined from the change in cell color. The criteria are as follows. [Cytotoxicity] +: The number of cells is obviously smaller than that of the control. Cytotoxic. ±: The number of cells is slightly smaller than that of the control. Some cytotoxicity. -: The number of cells is the same as that of the control. No cytotoxicity. [Melanin production inhibitory action] +: Clearly bleached compared to the control.
Has melanin production inhibitory effect. ±: slightly whiter than the control. There is a slight effect of suppressing melanin production. -: The color is the same as the control. No melanin production inhibitory effect.

The results are shown in Table 1. From this, it is understood that each of the melanin production inhibitors of the present invention has little cytotoxicity and has a melanin production inhibitory action. Further, it is understood that the melanin production inhibitor of the present invention is excellent in the action of reducing the melanin produced and whitening the skin, that is, the whitening action.

[0028]

[Table 1]

Example 2 Skin Irritation Test The above-mentioned melanin production inhibitors 1 to 8 were examined for skin irritation with guinea pig closed patches. That is, these 1% aqueous solutions were closed-patched on a Hartley white guinea pig with a shaved back for 48 hours, and the sample was administered 49 times.
After a lapse of time, the skin reaction was observed according to the Draize standard shown below. As a result, the specimen with misalignment was also non-reactive (-). From this, it is understood that the melanin production inhibitor of the present invention is excellent in safety. [Criteria for Draize] ++: Reaction with edema +: Reaction with clear erythema ±: Reaction with slight erythema −: No reaction

Example 3 Inhibitory Effect on Blackening Using the inner part of the human upper arm, ultraviolet rays A were irradiated at 1.5 times the minimum erythema concentration (MED), and a test sample was administered. It judged based on the standard shown in.
The samples used were a 0.05% aqueous solution of melanin production inhibitor 8 (invention product) and a 0.1% aqueous solution of arbutin (comparative product).
As a control, water was administered. The result was + for the invention product and ± for the comparative product. It is understood that arbutin is excellent in the blackening suppression effect, but the product of the present invention is further excellent in the blackening suppression. From this, it is understood that the melanin production inhibitor of the present invention can be used for preventing blackening. Further, it is understood that the cosmetics containing them can be expected to have an excellent whitening effect.

[0031]

EFFECT OF THE INVENTION The melanin production inhibitor of the present invention is excellent in melanin production inhibitory action and safety, and a whitening cosmetic composition containing it can be expected to have an excellent whitening action.

Claims (7)

[Claims] 1. A melanin production inhibitor comprising a complex of pectin and its hydrolyzate and a transition metal. 2. The melanin production inhibitor according to claim 1, wherein the hydrolyzate of pectin is oligogalacturonic acid. 3. The degree of polymerization of oligogalacturonic acid is 1 to
10. The melanin production inhibitor according to claim 1 or 2, which is 10. 4. The melanin production inhibitor according to claim 1, wherein the transition metal is iron. 5. The ratio of pectin or its hydrolyzate to the transition metal is 1: 2 to 1: 6 (equivalent ratio).
The melanin production inhibitor according to any one of 1. 6. A whitening cosmetic containing the melanin production inhibitor according to any one of claims 1 to 5. 7. The whitening cosmetic composition according to claim 6, wherein the content of the melanin production inhibitor according to any one of claims 1 to 5 is 0.01 to 10% by weight.