JPH11269058A - Bleaching preparation - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a preparation in such a dosage form as to extremely raise an inhibitory action on melanin production by formulating a substance having an inhibitory action on melanin production with an alkyl modified carboxyvinyl polymer and/or its salt. SOLUTION: This bleaching preparation comprises (A) a substance having an inhibitory action on melanin production (preferably hydroxyquinone) and (B) an alkyl modified carboxyvinyl polymer and/or its salt. Preferably the component B is wholly or partially neutralized with a basic substance such as an alkali metal salt or the like is used in a form containing a physiologically acceptable salt. Preferably the formulated amount of the component A based on the total of the cosmetic is 0.05-5 wt.% and that of the component B is 0.05-1 wt.%. Further addition of 10-30 wt.% of a polyhydric alcohol can preferably raise an inhibitory action on melanin production. Preferably >=30 wt.% of the polyhydric alcohol is 1,3-butanediol.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

The present invention relates to a cosmetic suitable as a whitening cosmetic.

[0002] Beautiful fair skin has been desired by all people since ancient times, and many efforts have been made to obtain such skin. In this, it was revealed that the cause of the whiteness of the color, in other words, the blackness of the color, was melanin contained in melanocytes. It was also clarified that depending on the amount of the melanin, the skin color became black or white. It is already known that proteins called tyrosinase and tyrosinase-related proteins are involved in the biosynthesis of melanin. In addition, materials for inhibiting the action of such enzymes and the like to realize fairness, such as glutathione derivatives, ascorbic acid and related substances, hydroquinone and related substances, phenolic substances, and cosmetics containing them Has been developed, and to a large extent it has become possible to whiten the color. However, such effects are often not as apparent as expected when compared with screening in a simple in vitro system. This is generally regarded as a problem of transdermal absorption of a substance having an inhibitory action on melanin production, but its detailed mechanism and solution have not been known yet, and elucidation and solution have been desired.

On the other hand, salts of alkyl-modified carboxyvinyl polymers have been used in the field of cosmetics as thickeners having an emulsifying action, but attempts to combine this with a substance having an inhibitory action on melanin production have been made. It has not been known at all that the combination with 10 to 30% by weight of a polyhydric alcohol causes further significant whitening effect.

[0004]

SUMMARY OF THE INVENTION The present invention has been made under such circumstances, and it is an object of the present invention to provide a dosage form which significantly enhances the effect of a substance having an inhibitory action on melanin production in actual applications. Make it an issue.

[0005]

DISCLOSURE OF THE INVENTION In view of such circumstances, the present inventors have intensively studied for a dosage form that significantly enhances the effect of a substance having an inhibitory effect on melanin production in actual application. The inventors have found that such a dosage form can be obtained by combining a substance having a production inhibitory action with an alkyl-modified carboxyvinyl polymer, and completed the invention. As a result of further studies, they have found that by combining this combination with 10 to 30% by weight of a polyhydric alcohol, this effect can be further enhanced, and the invention has been developed. This is considered to be because such a dosage form enhances percutaneous absorption of a substance having an inhibitory action on melanin production. Hereinafter, the present invention will be described in more detail focusing on embodiments.

[0006]

BEST MODE FOR CARRYING OUT THE INVENTION (1) Alkyl-modified carboxyvinyl polymer which is an essential component of the cosmetic of the present invention The alkyl-modified carboxyvinyl polymer which is another essential component of the present invention is a thickener having an emulsifying action. It is used in fields such as cosmetics. Alkyl-modified carboxyvinyl polymers include those already marketed by Goodrich under the trade name of Pemulen TR-1 or Pemulen TR-2, and the use of these polymers is stable in quality. Particularly preferred. The content of these alkyl-modified carboxyvinyl polymers in the cosmetic of the present invention is preferably 0.01 to 5% by weight, more preferably 0.0 to 5% by weight, based on the total amount of the cosmetic.
Particularly preferred is 5 to 1% by weight. It is used in a form containing a physiologically acceptable salt by neutralizing the whole or a part with an alkali metal such as sodium or potassium, an amine such as triethanolamine, or a basic substance such as a basic amino acid. Is preferred.

(2) Substance having an inhibitory action on melanin production which is an essential component of the cosmetic of the present invention The substance having an inhibitory action on melanin production which is an essential ingredient of the cosmetic of the present invention has a melanin production inhibitory action If it can be used without any particular limitation, for example, ascorbic acid, sodium ascorbate, ascorbic acid phosphate magnesium salt, ascorbic acid such as benzyl ascorbic acid and related substances, dipalmitoyl glutathione, dipalmitoyl glutathione Glutathione derivatives such as cyclodextrin conjugates, hydroquinone, hydroquinone glucoside,
Hydroquinones such as hydroquinone maltoside and related substances, kojic acid, isokojic acid, caffeic acid, acetosyringone, resorcinol, alkoxyresorcinol, alkylresorcinol, alkylcarbonylresorcinol, phenols such as hydroxychalcone, dehydrocawein, catechin, catechin gallate, etc. 1 selected from sexual substances
Preferred examples include two or more species. Among these, one or more selected from hydroquinone and related substances and phenolic substances are particularly preferred. The preferred content of these substances having a melanin production-suppressing action in the cosmetic of the present invention varies depending on the degree of each effect, but is generally close to the effective amount, and is preferably 0 to the total amount of the cosmetic. 0.01 to 10% by weight, more preferably 0.05 to 5% by weight.

(3) Cosmetic of the Present Invention The cosmetic of the present invention is characterized by containing the above-mentioned alkyl-modified carboxyvinyl polymer and a substance having an inhibitory action on melanin production. Here, as the cosmetic of the present invention, if it is a cosmetic, it is possible to select a dosage form without particular limitation, but from the characteristics of the present invention, an emulsifying system such as a cream or an emulsion is preferable. Among them, an emulsion is particularly preferred. Further. The cosmetic of the present invention may contain, in addition to these essential components, optional components usually used in cosmetics. Such optional components include, for example, hydrocarbons such as petrolatum and microcrystalline wax, esters such as jojoba oil and gay wax, triglycerides such as tallow, olive oil, higher alcohols such as cetanol and oleyl alcohol, and stearic acid. , Fatty acids such as oleic acid, polyhydric alcohols such as glycerin and 1,3-butanediol, nonionic surfactants, anionic surfactants, cationic surfactants, amphoteric surfactants,
Examples include thickeners such as ethanol and carbopol, preservatives, ultraviolet absorbers, antioxidants, pigments, powders, and the like. Among these optional components, particularly preferable are polyhydric alcohols such as 1,3-butanediol, propylene glycol, glycerin, polyethylene glycol, diglycerin, and dipropylene glycol, and preferably contain 10 to 30% by weight. . This is because when a polyhydric alcohol is contained in this concentration range, melanin production inhibitory action can be further enhanced. More preferably, 30% by weight or more of the polyhydric alcohol is 1,3-butanediol.

Furthermore, it should be noted that the addition of optional components is to reduce the amount of the surfactant, especially the nonionic surfactant, to 0.5% by weight or less, more preferably 0.3% by weight. % Or less. This is because if the amount of the surfactant, even if divided, the nonionic surfactant exceeds 0.5% by weight, the transdermal absorption of a substance having a melanin production inhibitory action is impaired.

[0010] The cosmetic of the present invention can be produced by treating the above components according to the above-mentioned precautions according to a conventional method.

[0011]

The present invention will be described in more detail with reference to the following examples, but it goes without saying that the present invention is not limited only to these examples.

Example 1 A cosmetic (lotion) of the present invention was produced according to the following formulation. That is, the components (a) and (b) were heated to 80 ° C., and (b) was neutralized by slowly adding to (b) while stirring, and the mixture was stirred and cooled to obtain a lotion. About this, together with Comparative Example 1 showing the prescription below,
The melanin production inhibitory effect was evaluated by a continuous administration test using the upper arm of a human (two panelists). That is, 1.5cm on the upper arm
Four X1.5 cm portions were provided, and the BED ultraviolet rays previously determined were radiated to the portions once a day for 3 consecutive days, and then the cosmetic of the present invention and the cosmetic of Comparative Example 1 were applied to each portion at 0%. .0
It was applied in 2 ml increments for 3 consecutive weeks. The remaining part was used for light irradiation control. On the day after the last administration, the color of the site was compared with that of the light-irradiated control and judged to evaluate the inhibitory effect on melanin production. The evaluation was performed by observing and determining according to the following criteria. That is, ++: remarkably less blackness than the light irradiation control, +: clearly less blackness than the light irradiation control, ±: compared to the light irradiation control,
Slightly less blackness,-: The criterion was that no difference in darkness was recognized as compared to the light irradiation control. Table 1 shows the results. This indicates that the cosmetic of the present invention is excellent in the melanin production inhibitory action. (Prescription of Example 1) i Arbutin 0.3 parts by weight Pemulene TR-2 0.2 parts by weight Water 49.45 parts by weight Potassium hydroxide 0.05 parts by weight Water 50 parts by weight (Comparative Example 1) Arbutin 0.0 parts by weight 3 parts by weight water 99.7 parts by weight

[0013]

[Table 1]

<Examples 2 to 6> Cosmetics (emulsion) of the present invention were prepared according to the formulations shown in Table 2 below. That is,
A, B, and C were each heated to 80 ° C., and A and B were mixed and neutralized. The mixture was gradually added to C with stirring, emulsified, and cooled by stirring to obtain an emulsion. The same light irradiation test as in Example 1 was performed on this emulsion. However, the control was changed from the light control to the cosmetic of Example 1. Table 2 shows the results. From this, it is preferable that the cosmetic of the present invention is in the form of an emulsifier such as an emulsion, and it is preferable that the polyhydric alcohol contains 10 to 30% by weight. Butanediol (13B
G), and it is found that the content of the surfactant and, if divided, the nonionic surfactant is preferably 0.5% by weight or less. Incidentally, the numerical values of the prescription represent parts by weight.

[0015]

[Table 2]

<Examples 7 to 13> Cosmetics (emulsion) of the present invention were prepared according to the following formulations. That is,
(B) and (c) were each heated to 80 ° C., and (a) and (b) were mixed and neutralized. The mixture was gradually added to (c) with emulsification, emulsified, and cooled by stirring to obtain an emulsion. The same light irradiation test as in Example 1 was performed on this emulsion. However, a 0.3 wt% aqueous solution of each substance having a melanin production inhibitory action was used as a control. Table 3 shows these substances and evaluation results. It is clear from this that the effect of the cosmetic of the present invention is exerted regardless of the type of the substance having the melanin production inhibitory action. I Pemulen TR-2 0.2 parts by weight 13BG 10 parts by weight Glycerin 5 parts by weight Substance having an inhibitory effect on melanin production * 0.3 part by weight Water 30 parts by weight B Water 49.25 parts by weight KOH 0.05 part by weight Hacetanol 1 part by weight liquid paraffin 9 parts by weight glyceryl monostearate 0.1 part by weight sucrose fatty acid ester 0.1 part by weight

[0017]

[Table 3]

Example 13 For the cosmetic of Example 5, an experiment similar to the evaluation experiment of Example 1 was conducted using 17 panelists. One week, two weeks, and three weeks, the color was immediately measured using a color difference meter, and the average value of the difference (ΔL) of the L value with respect to the control was calculated.
At 0.93 and 3 weeks, +1.11 was observed, indicating that the melanin production inhibitory action was excellent.

[0019]

According to the present invention, it is possible to provide a dosage form which significantly enhances the effect of a substance having an inhibitory action on melanin production in actual application.

──────────────────────────────────────────────────続 き Continued on the front page (51) Int.Cl. ⁶ Identification code FI A61K 7/00 A61K 7/00 X

Claims (6)

[Claims] 1. A cosmetic comprising a substance having an inhibitory action on melanin production and an alkyl-modified carboxyvinyl polymer and / or a salt thereof. 2. A cosmetic comprising a polyhydric alcohol in an amount of 10 to 30% by weight. 3. The substance having an inhibitory action on melanin production,
The cosmetic according to claim 1 or 2, wherein the cosmetic is at least one selected from glutathione derivatives, ascorbic acid and related substances, hydroquinone and related substances, and phenolic substances. 4. The cosmetic according to claim 1, wherein the polyhydric alcohol contains at least 5% by weight of 1,3-butanediol. 5. The cosmetic according to claim 1, wherein the content of the surfactant is 0.5% by weight or less. 6. The cosmetic according to claim 1, which is a whitening cosmetic.