JP2000256168A - Skin lotion - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a skin lotion excellent in skin-beautifying effect, having suppressed sticky sense of use without decreasing the skin-beautifying effect of alkoxysalicylic acid or its salt by including an alkoxysalicylic acid and a sugar alcohol. SOLUTION: This skin lotion includes (A) preferably 0.001-20 wt.%, more preferably 0.01-10.0% of the alkoxysalicylic acid expressed by formula (R is an alkyl) [e.g.; 3-methoxysalicylic acid (2-hydroxy-3-methoxybenzoic acid)] and (B) preferably 0.001-20.0%, more preferably 0.05-10.0% of the sugar alcohol (preferably solid at normal temperature, concretely erythritol, xylitol or the like), and the formulation ratio of the component B to the component A is >=0.01 times preferably >=0.1 times, more preferably >=0.5 times.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD [0001] The present invention relates to an external preparation for the skin. More specifically, the present invention relates to an external preparation for skin that has an excellent whitening effect and does not have a sticky feeling of use.

[0002]

2. Description of the Related Art "Whitening" means white and beautiful skin.
It is one of the most important themes for skin external preparations, especially cosmetics.

[0003] Cosmetics intended for "whitening" contain, for example, vitamin C and its derivatives, kojic acid, arbutin and the like as whitening components. In recent years, searches for whitening components have become more and more active, and as one of the results, alkoxysalicylic acid has been proposed as a component having an excellent whitening effect (Japanese Patent Publication No. 6-40886).

[0004]

However, there is a problem that a skin external preparation containing an alkoxysalicylic acid tends to have a sticky feeling when used.

The problem to be solved by the present invention is that the whitening effect is excellent, but a problem in terms of usability has been pointed out.
An object of the present invention is to provide means for improving the usability of a skin external preparation containing an alkoxysalicylic acid or the like.

[0006]

Means for Solving the Problems The present inventor has made intensive studies to solve this problem. As a result, together with the above-mentioned alkoxysalicylic acid or a salt thereof, a sugar alcohol is combined to form an active ingredient of a skin external preparation,
The present inventors have found that it is possible to provide an external preparation for skin having an excellent whitening effect without impairing the whitening effect of alkoxysalicylic acid or a salt thereof and having a reduced sticky feeling.

That is, the present invention provides the following general formula (A):

Embedded image (Wherein, R represents an alkyl group). The invention provides an external skin preparation (hereinafter, referred to as the external skin preparation of the present invention) containing an alkoxysalicylic acid or a salt thereof represented by the formula: is there.

[0008]

Embodiments of the present invention will be described below. A. Which is one of the active ingredients of the active ingredient present invention the external preparation for skin of the present invention the external preparation for skin, alkoxy salicylic acid represented by the general formula (A), 3-position of salicylic acid, either 4- or 5-position This is a salicylic acid-based compound in which such a hydrogen atom is substituted by an alkoxy group (-OR).

In the general formula (A), an alkoxy group (-
The alkyl group R constituting OR) is not particularly limited.
Specifically, for example, a methyl group (corresponding alkoxy group -OR: methoxy group), an ethyl group (the same ethoxy group), a propyl group (the same propoxy group), an isopropyl group (the same isopropoxy group), and a butyl group (the same Butoxy group) and isobutyl group (isobutoxy group), and more preferably methyl group (methoxy group).
Or an ethyl group (the same ethoxy group), but is not limited thereto.

Specifically, representative examples of the alkoxysalicylic acid (A) which can be blended in the external preparation for skin of the present invention include: 3-methoxysalicylic acid (2-hydroxy-3-methoxybenzoic acid).
acid) 3-ethoxysalicylic acid
cid) 4-Methoxysalicylic acid
acid) 4-ethoxysalicylic acid
cid) 4-propoxysalicylic acid (2-hydroxy-4-propoxybenzoi
c acid) 4-isopropoxysalicylic acid (2-hydroxy-4-isopropox
ybenzoic acid) 4-butoxysalicylic acid (2-hydroxy-4-butoxybenzoic a
cid) 5-methoxy-5-methoxybenzoic
acid) 5-ethoxysalicylic acid
cid) 5-propoxysalicylic acid (2-hydroxy-5-propoxybenzoi
c acid) and the like.

Alkoxysalicylic acid is a known substance. For example, 5-methoxysalicylic acid is described in Beil, 10
227,4-methoxysalicylic acid is described in Beil, 1037
The compound can be easily synthesized by the method described in No. 9. Further, it is commercially available as a reagent from Aldrich (Germany) or the like, and this can be used in the present invention.

The alkoxysalicylic acid which can be incorporated in the external preparation for skin of the present invention also includes its salt. The kind of the salt is not particularly limited as long as it is a pharmaceutically acceptable salt, and for example, sodium salts, potassium salts, alkali metal salts such as calcium salts or alkaline earth metal salts, ammonium salts And salts such as salts and amino acid salts.

In the skin external preparation of the present invention, one kind of alkoxysalicylic acid or a salt thereof (hereinafter, also collectively referred to as alkoxysalicylic acids) may be selected and blended, and two or more kinds may be combined. It is also possible to mix.

The amount of the alkoxysalicylic acid compound in the external preparation for skin of the present invention should be appropriately selected according to the specific dosage form of the external preparation for skin and the balance with other components. Although not particularly limited, it is generally preferred that the content is 0.001 to 20.0% by weight, more preferably 0.01 to 1% by weight, based on the whole agent.
0.0% by weight. If the compounding amount of the alkoxysalicylic acid is less than 0.001% by weight based on the whole agent, it is difficult to sufficiently exert a whitening effect, which is not preferable.
Even if the content exceeds 0.0% by weight, the improvement in whitening effect corresponding to the increase in the amount of compounding is difficult to be recognized, and the generation of a sticky feeling is strongly promoted. In addition, when the alkoxysalicylic acids are not combined with the sugar alcohol described below, the compounding amount of the alkoxysalicylic acids to the whole agent is set to about 0.01% by weight or more, which is considered to be particularly suitable in the present invention. Then, the tendency of the agent to become sticky increases.

The sugar alcohol compounded with the above-mentioned alkoxysalicylic acids in the skin preparation for external use of the present invention is a linear polyhydric alcohol in which the carbonyl group of the sugar is reduced, and is not particularly limited. , Maltitol, mannitol, erythritol, xylitol and the like. In the skin external preparation of the present invention, a sugar alcohol which is solid at ordinary temperature, specifically, erythritol, xylitol, etc., is preferably selected because it is excellent in the effect of reducing stickiness derived from the above-mentioned alkoxysalicylic acids.

In the skin external preparation of the present invention, one kind of sugar alcohol can be selected and blended, or two or more kinds can be blended in combination. In the skin preparation for external use of the present invention, the mixing ratio of the sugar alcohol to the above-mentioned alkoxysalicylic acids, or a specific mixing amount,
It is as follows.

First, the compounding ratio (weight ratio) of the sugar alcohol to the alkoxysalicylic acid is generally set at 0.0% of the compounding amount of the above-mentioned alkoxysalicylic acid.
It is at least 1 times, preferably at least 0.1 times, more preferably at least 0.5 times. In addition, the amount of the sugar alcohol in the skin external preparation of the present invention is 0.001 to 20 with respect to the total amount of the agent, in consideration of the effect of suppressing the stickiness of the alkoxysalicylic acids and the stickiness when the sugar alcohol is incorporated in a large amount. 0.0% by weight, more preferably 0.05 to 10.0% by weight.

The preferred amounts of the alkoxysalicylic acids and sugar alcohols, which are essential components in the skin preparation for external use of the present invention described above, are summarized as follows. %, Whereas the sugar alcohol is 0.001-2%
0.0% by weight, more preferably 0.05 to 10.0
% By weight. And the range of these blending amounts, the range of the blending ratio of the above-mentioned sugar alcohol and alkoxysalicylic acids, and further taking into account the specific dosage form and the like of the external preparation for skin of the present invention, of these essential components, The specific compounding amount in the skin external preparation of the present invention can be selected.

The skin according to the present invention, which is capable of exhibiting the whitening effect of alkoxysalicylic acids while suppressing the sticky feeling of use, by combining and combining alkoxysalicylic acids and sugar alcohols. An external preparation is provided.

B. Specific embodiments of the external preparation for skin of the present invention
In addition to the above-mentioned active ingredients, the skin external preparation of the present invention
If necessary, various components generally used for external preparations for skin can be blended as long as the desired effects of the present invention are not impaired.

The dosage form of the external preparation for skin of the present invention is arbitrary, and may be any of a solution system, a solubilizing system, an emulsifying system, a powder dispersing system, a water-oil two-layer system, a water-oil-powder three-layer system, and the like. Such a dosage form may be used. The use of the external preparation for skin of the present invention is also optional. Facial cosmetics such as lotions, emulsions, creams, packs and the like, makeup cosmetics such as foundations, lipsticks, eye shadows, etc., body cosmetics, aromatic cosmetics, detergents , Ointments and the like.

In the skin external preparation of the present invention, in order to mainly add a specific pharmacological effect, for example, vitamins,
Moisturizers, ultraviolet absorbers, anti-inflammatory agents, whitening agents other than alkoxysalicylic acid, various animal and plant extracts, activators, blood circulation promoters, antiseborrheic agents, and the like can be added.

In order to make the external preparation for skin of the present invention into a desired dosage form, for example, oils such as liquid fats and oils, solid fats and oils, waxes, hydrocarbon oils; higher fatty acids, higher alcohols and synthetic ester oils , Silicone, various surfactants,
Preservatives, various water-soluble polymers, various powder components, pigments, dyes, fragrances, water, and the like can be added as necessary.

The specific dosage form of the skin external preparation of the present invention will be described in Examples described later.

EXAMPLES The present invention will be described in more detail with reference to the following Examples, which by no means limit the technical scope of the present invention. In addition, the description of the compounding amount in this Example is represented by the weight% with respect to the whole compounded object, unless otherwise specified.

[Test Examples] In order to determine the intended effect of the present invention, a usability evaluation test and a whitening effect evaluation test were carried out.
Agents having compositions shown in Table 1 [Test Example 1, Comparative Examples 1 and 2: First
A (oil phase) and B (water phase) described in the table were each 70 ° C.
And completely dissolved. Next, A was added to B and emulsified by an emulsifier. Further, the emulsion was cooled using a heat exchanger to produce a cream as a test product].

1. Usability evaluation test A special product was applied to the face of 30 specialized panels, and the usability (stickiness) was evaluated by each specialized panel.
The sensory evaluation was performed, and the usability of the test article was evaluated according to the following evaluation criteria.

Usability evaluation criteria ：: Little stickiness Δ: Slight stickiness X: Feel sticky The results of this test are shown in Table 1 (the number of people who have performed each evaluation is shown).

2. Whitening Effect Evaluation Test The subjects who were exposed to the sunlight in the summer for 4 hours (2 hours a day for 2 days) were grouped into 10 subjects, and the subjects were exposed to the sunlight for 5 days.
From the day after, apply each test sample to the inner skin of the upper arm once in the morning and evening.
It was applied for a week.

After 8 weeks, whether or not the use of the test article had an inhibitory effect on the pigmentation induced by the ultraviolet rays of sunlight was visually evaluated to determine whether the effect was significant, effective, slightly effective or ineffective. Was evaluated according to the following evaluation criteria.

Evaluation criteria for whitening effect ◎: Eight or more panelists (80%
○: Excellent or effective panelists 5-7 or more (5
0% or more and less than 70%) Δ: 3-4 or more panelists (3
0: less than 50%) ×: Two or less panelists who were extremely effective or effective (30%
The results of this test are also shown in Table 1.

[0031]

[Table 1] Table 1-Composition Test Example 1 Comparative Example 1 Comparative Example 2 A. Oil phase Liquid paraffin 10.0 10.0 10.0 Squalane 3.0 3.0 3.0 Self-emulsifying monostearic acid 1.0 1.0 1.0 Glycerin Polyoxyethylene sorbitan 2.0 2.0 2 2.0 Monostearic acid ester (20EO) Pantothenyl ethyl ether 0.1 0.1 0.1 Jojoba oil 2.0 2.0 2.0 Fragrance Suitable amount Suitable amount B. Aqueous phase Hibiswako 105 0.3 0.3 0.3 KOH 0.1 0.1 0.1 Potassium 4-methoxysalicylate 2.0 2.0-Erythritol 3.0--Glycerin 5.0 5.05 5.0 Ethyl alcohol 5.0 5.0 5.0 Methyl paraben 0.1 0.1 0.1 Ion-exchange water Residue Residual residue ────────────────── ───────────────── Usability evaluation ○ 22 people 0 people 24 people △ 7 people 5 people 6 people × 1 person 25 people 0 people Evaluation of whitening effect ◎ ◎ × ───配合 As clearly shown in Table 1, erythritol, a sugar alcohol, is added Thereby, the stickiness of potassium 4-methoxysalicylate, which is an alkoxysalicylic acid, is suppressed. And revealed that agents excellent whitening effect is provided.

Hereinafter, various formulation examples of the skin external preparation of the present invention will be described. In addition, the above-mentioned test was performed on the skin external preparations of the present invention in these formulation examples, and the usability and whitening effect were tested. In any of the formulation examples, a panel with a sticky feeling was felt. Was very slight, and the evaluation of the whitening effect was “○”.

Formulation Example 1 Amount of Cream Compounding Component (% by Weight) Cetanol 4.0 Vaseline 7.0 Isopropyl myristate 8.0 Squalane 15.0 Monoglycerin stearate 2.2 POE (20) Sorbitan monostearate 2.8 5-Ethoxysalicylic acid 0.01 Vitamin E nicotinate 2.0 Fragrance 0.3 Antioxidant qs Preservative qs Glycerin 10.0 Sodium hyaluronate 0.02 Xylitol 1.0 Dipropylene glycol 4.0 Sodium pyrrolidonecarboxylate 1.0 Alanine 3.0 Disodium edetate 0.01 Purified water residue <Production method> A cream was obtained according to the method.

Formulation Example 2 Emulsion Compounding Component Mixing Amount (% by Weight) Squalane 5.0 Oleyl oleate 3.0 Vaseline 2.0 Sorbitan sesquioleate 0.8 Polyoxyethylene oleyl ether (20EO) 1.2 Evening primrose oil 0.5 Fragrance 0.3 Preservatives B. 1,3-butylene glycol 4.5 4-Sodium 4-propoxysalicylate 1.5 Maltitol 4.0 Ethanol 3.0 Carboxyvinylporlimer 0.2 Potassium hydroxide 0.1 L-Arginine L-aspartate 0.01 Serine 0.05 Purified water residue <Production method> An emulsion was obtained according to the method of Test Example 1 above.

Formulation Example 3 Compounding amount of foundation compounding component (% by weight) Cetanol 3.5 Deodorized lanolin 4.0 Jojoba oil 5.0 Vaseline 2.0 4-butoxysalicylic acid 10.0 Squalane 6.0 Stearic acid monoglycerin ester 2.5 POE (60) hydrogenated castor oil 1.5 POE (20 ) Cetyl ether 1.0 Pyridoxine tripalmitate 0.1 Preservatives Appropriate amount Fragrance 0.3 B. Propylene glycol 10.0 Erythritol 5.0 Compound powder 12.0 Histidine 5.0 dl-alanine 1.0 Purified water residue <Production method> A foundation was obtained according to the method of Test Example 1 above.

[Formulation Example 4] Blending amount of toner component (% by weight) Ethanol 5.0 POE oleyl alcohol ether 2.0 2-ethylhexyl-P-dimethylaminobenzoate 0.18 fragrance 0.05 B. 1,3-butylene glycol 9.5 sodium pyrrolidonecarboxylate 0.5 potassium 3-methoxysalicylate 0.5 xylitol 0.5 nicotinamide 0.3 glycerin 5.0 trimethylglycine 5.0 hydroxypropyl beta cyclodextrin 1. 0 Lysine 0.05 Remaining amount of purified water <Production method> The alcohol phase of A was added to the aqueous phase of B and solubilized to obtain a lotion.

[Formulation Example 5] Packing ingredients (% by weight) (1) polyvinyl alcohol 10.0 (2) sorbitol 4.0 (3) glycerin 3.0 (4) ethanol (95%) 8.0 (5) Sodium 3-ethoxysalicylate 1.0 (6) Alanine 0.1 (7) Preservative 0.1 (8) Fragrance 0.1 (9) Remaining purified water <Production method> (4) (7) ) And (8) were mixed and dissolved, and (1), (2) (3) and (5) (6) (9) were mixed and dissolved at 80 ° C, followed by stirring and then allowed to cool to room temperature to obtain a pack. Was.

[0038]

Industrial Applicability According to the present invention, there is provided an external preparation for skin which suppresses the sticky feeling while utilizing the excellent whitening effect of alkoxysalicylic acid or a salt thereof.

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Claims (2)

[Claims] (1) The following general formula (A): (Wherein, R represents an alkyl group) An external skin preparation comprising, as an active ingredient, an alkoxysalicylic acid or a salt thereof represented by the formula: 2. The external preparation for skin according to claim 1, wherein the sugar alcohol is a sugar alcohol which is solid at normal temperature.