JP5455292B2 - Skin external composition - Google Patents

Description

  The present invention relates to an external composition for skin. More specifically, the present invention relates to an external composition for skin showing a high moisture retention effect and moisture transpiration suppression effect.

  For people with dryness sensitive skin that is easily affected by external irritation, dryness, etc., sufficiently moisturizing the skin using cosmetics or the like is effective in improving rough skin.

  For moisturizing, it is effective to suppress the transpiration of moisture from the skin (decrease in the amount of horny moisture transpiration TEWL) and to retain moisture in the skin itself.

  Conventionally, as a humectant, a polyhydric alcohol (for example, 1,3-butylene glycol, dipropylene glycol, glycerin, etc.), an amino acid or a salt thereof, a sugar chain (for example, xylitol, etc.), a mucopolysaccharide (for example, hyaluronic acid or a salt thereof) Salts, etc.), gums and carboxyvinyl polymers (acrylic acid / alkyl acrylate (C10-30) copolymers and other water-soluble polymers, organic acids or salts thereof, ceramides, extracts of animals and plants, etc.) It has been.

  For example, Patent Document 1 describes a skin cosmetic containing an amino acid.

  Patent Document 2 describes a skin external preparation containing ceramide.

However, conventional skin cosmetics and external preparations for skin have insufficient moisture retention effect and moisture transpiration suppression effect, and development of a composition for external use that can provide high moisture retention effect and moisture transpiration suppression effect is eagerly desired. Yes.
JP-A-11-292751 JP2003-160462

  In view of the above situation, an object of the present invention is to provide a composition for external use on skin, which exhibits high moisturizing power, that is, moisture retention effect and moisture transpiration suppression effect.

  As a result of intensive studies to solve the above problems, the present inventor showed that a composition for external use containing ceramide and an amino acid at a specific ratio showed a high moisture retention effect and a moisture transpiration suppression effect. It has been found that a high moisturizing effect can be obtained by use. The present invention is based on such novel findings.

Accordingly, the present invention relates to a composition for external use for skin shown in the following section:
Item 1. The composition contains 0.00022 to 0.15% by weight of ceramide and 0.0015 to 0.75% by weight of amino acid, and more than 4 parts by weight and less than 16 parts by weight with respect to 1 part by weight of ceramide. An external composition for skin containing an amino acid.

  Item 2. Item 5. The external composition for skin according to Item 1, wherein 5 to 15 parts by weight of amino acid is blended with 1 part by weight of ceramide.

  Item 3. Item 3. The external composition for skin according to Item 1 or 2, which is a cosmetic.

  Item 4. Item 4. The external composition for skin according to any one of Items 1 to 3, wherein the ceramide is at least one selected from the group consisting of ceramide I, ceramide II, ceramide III, and ceramide VI.

  Item 5. Item 5. The external composition for skin according to any one of Items 1 to 4, wherein the amino acid is at least one selected from the group consisting of serine, glycine, glutamic acid, alanine, lysine, arginine, threonine, and proline.

  By using the external composition for skin of the present invention, a high moisturizing effect, that is, a moisture retention effect and a moisture transpiration suppression effect can be obtained. In addition to the moisturizing effect, the composition for external use of the present invention has an advantage that it has no stickiness or squeaky feeling and shows a moist feeling.

Composition of the present invention The present invention comprises 0.00022 to 0.15% by weight of ceramide and 0.0015 to 0.75% by weight of amino acid in the composition, and 4 parts by weight with respect to 1 part by weight of ceramide. Provided is a composition for external use containing more and less than 16 parts by weight of an amino acid.

Ceramide, which is an active ingredient of the composition for external use of the skin of the present invention, is composed of a sphingosine or similar base of sphingosine such as phytosphingosine, a fatty acid having no OH by an amide bond, α-hydroxy fatty acid or ω- It is a compound that binds to hydroxy fatty acids.

  Examples of the ceramide include (2S, 3R) -ceramide 1 (hereinafter referred to as ceramide I) which is natural or natural ceramide, and (2S, 3R) -ceramide 2 (hereinafter referred to as ceramide II) which is natural or natural ceramide. (2S, 3R) -ceramide 3 (hereinafter referred to as ceramide III), (2S, 3R) -ceramide 4 (hereinafter referred to as ceramide IV) which is a natural or natural ceramide. ), Natural or natural ceramide (2S, 3R) -ceramide 5 (hereinafter referred to as ceramide V), natural or natural ceramide (2S, 3R) -ceramide 6 (hereinafter referred to as ceramide VI), etc. Can be mentioned.

  In the present invention, among these ceramides, it is preferably at least one selected from the group consisting of ceramide I, ceramide II, ceramide III and ceramide VI, and it is more preferable to add all four of these ceramides. . When these four kinds of ceramides are used in combination, ceramide I in the total ceramide is preferably 0.1 to 30% by weight, more preferably 0.2 to 2.5% by weight, and 0.2 to 20% by weight. The ceramide II is preferably 10 to 80% by weight, more preferably 10 to 70% by weight, still more preferably 20 to 60% by weight, and the ceramide III is preferably 5 to 50% by weight and 10 to 45% by weight. More preferably, 15 to 45% by weight is further preferable, and ceramide VI is preferably 5 to 50% by weight, more preferably 10 to 45% by weight, and further preferably 15 to 45% by weight.

  The skin external composition of the present invention preferably contains these various ceramides in a total amount of 0.00022 to 0.15% by weight, more preferably 0.0015 to 0.12% by weight.

  It is preferable to set the mixing ratio of ceramide in the composition of the present invention in such a range and use it together with an amino acid because the keratin moisture retention rate, the keratin moisture transpiration suppression rate and the like can be effectively improved.

  In the present invention, these ceramides also include optical isomers thereof.

Amino acid An amino acid, which is an active ingredient of the composition for external skin of the present invention, is a compound having a carboxyl group and an amino group in the molecule.

  In the present invention, an amino acid refers to a main amino acid constituting a protein, a monoamino monocarboxylic acid exemplified by glycine, alanine, valine, leucine and isoleucine; an oxyamino acid exemplified by serine and threonine; cysteine, cystine and methionine Sulfur-containing amino acids exemplified by: monoaminodicarboxylic acids (acidic amino acids) exemplified by aspartic acid and glutamic acid; aliphatic amino acids (1) such as diaminomonocarboxylic acids (basic amino acids) exemplified by lysine and arginine; Aromatic amino acids (2) exemplified by phenylalanine and tyrosine; heterocyclic amino acids (3) exemplified by histidine (basic amino acids), tryptophan, proline and oxyproline can be mentioned.

  These amino acids may be salts such as sodium salt and hydrochloride. These amino acids or salts thereof may be used alone or in combination of two or more. In the present invention, at least one amino acid selected from the group consisting of serine, glycine, glutamic acid, alanine, lysine, arginine, threonine and proline is preferable, and it is more preferable to use these eight amino acids in combination. Moreover, when using these 8 types of amino acids in combination, serine is preferably 5 to 60% by weight, more preferably 10 to 50% by weight, even more preferably 20 to 50% by weight, and glycine is preferably 5 to 50% in the total amino acids. % By weight is preferred, 5 to 40% by weight is more preferred, 10 to 35% by weight is more preferred, glutamic acid is preferably 5 to 40% by weight, more preferably 5 to 30% by weight, and even more preferably 10 to 30% by weight. , Alanine is preferably 1 to 20% by weight, more preferably 2 to 15% by weight, further preferably 5 to 15% by weight, lysine is preferably 1 to 20% by weight, more preferably 2 to 15% by weight, 15 wt% is more preferable, arginine is preferably 0.5 to 10 wt%, more preferably 1 to 8 wt%, further preferably 2 to 8 wt%, The leonine is preferably 0.5 to 10% by weight, more preferably 1 to 8% by weight, further preferably 2 to 8% by weight, and the proline is preferably 0.02 to 8% by weight, and 0.05 to 5% by weight. More preferred is 0.1 to 5% by weight.

  The external composition for skin of the present invention preferably contains these various amino acids in a total amount of 0.0015 to 0.75% by weight, preferably 0.0015 to 0.7% by weight.

  It is preferable that the mixing ratio of the amino acid in the composition of the present invention is in such a range and combined with ceramide can effectively improve the keratin moisture retention rate, the keratin moisture transpiration suppression rate, and the like.

  The composition for external use of the skin of the present invention is more than 4 parts by weight and less than 16 parts by weight, preferably 5 to 15 parts by weight, more preferably 5 to 8 parts by weight, based on 1 part by weight of ceramide. More preferably, it contains 5 to 7 parts by weight, most preferably 6 parts by weight.

  The content of ceramide and amino acid in the external composition for skin of the present invention is as described above. In a preferred embodiment, the weight ratio of ceramide and amino acid, and the content of ceramide and amino acid are shown in Table 1 below. Embodiment 1 is preferable and Embodiment 2 is more preferable.

  In a more preferred embodiment, the weight ratio between ceramide and amino acid and the content of ceramide and amino acid are more preferably Embodiment 3 shown in Table 2 below, and most preferably Embodiment 4.

  Further, the blending amount of ceramide and amino acid in the external composition for skin of the present invention is as described above, but the total amount of ceramide and amino acid is preferably 0.0017 to 0.9% by weight in the composition. 0.002 to 0.8% by weight is more preferable, 0.002 to 0.6% by weight is further preferable, and 0.002 to 0.4% by weight is particularly preferable. Within this range, the stratum corneum moisture retention rate and the moisture retention effect per unit amount, the stratum corneum moisture transpiration suppression rate, and the stratum corneum moisture transpiration suppression effect per unit amount can be improved in a balanced manner.

  When the composition for external use of the present invention is used, a high moisturizing effect, that is, a keratin moisture retention rate and a moisture retention effect per unit amount and a keratin moisture transpiration suppression rate and a unit amount as demonstrated in the following examples. It can satisfy the effect of suppressing keratin moisture transpiration.

  Specifically, for keratin water, the keratin water retention rate is 120% or more, preferably 140% or more, more preferably 300% or more, further preferably 400% or more, and particularly preferably 500%. That's it. The upper limit is not particularly limited, but is usually 1100%. Moreover, the moisture retention effect per unit amount is 1000 or more, preferably 2000 or more, and more preferably 3000 or more. Although an upper limit is not specifically limited, Usually, it is 110000 or less.

  In addition, regarding the suppression of keratin moisture transpiration, the keratin moisture transpiration suppression rate is 10% or more, preferably 15%, more preferably 20%, and even more preferably 25%. The upper limit is not particularly limited, but is usually 55%. Moreover, the moisture transpiration suppression effect per unit amount is 50 or more, preferably 200 or more, more preferably 500 or more, still more preferably 1000 or more, and particularly preferably 2000 or more. Although an upper limit is not specifically limited, Usually, it is 6500 or less.

Other components Examples of the base of the external composition for skin of the present invention include water, polyol, alcohol, silicone oil, hydrocarbon oil, ester oil, vegetable oil, higher alcohol, higher fatty acid and the like.
In addition to the ceramide, amino acid and base, the external composition for skin of the present invention may appropriately contain an active ingredient and an additive according to each application.

  Examples of active ingredients include UV protection agents, whitening agents, anti-inflammatory agents, anti-aging agents, blood circulation promoters, fragrances, bactericides / disinfectants, antiperspirants, deodorants / deodorants, hair growth / hair restorers, hair removers , Hair dyes, permanent wave agents, repellents, anti-inflammatory analgesics and the like.

  Examples of additives include sterols, fluorine-based oils, surfactants, hydroxy acids, guanidine derivatives or salts thereof, film-forming polymers, sugars, plant extracts, antioxidants or singlet oxygen scavengers, and sebum secretion suppression. Agent, vitamin, gelling agent, powder, inorganic salt, pH adjusting agent, viscosity adjusting agent, antioxidant, antiseptic, sequestering agent, cooling agent, pigment, solid / semi-solid oil, water-soluble polymer, Examples thereof include oil-soluble polymers, biocompatible polymers, liposome preparations, capsule preparations, pearlescent agents, and micro / nanoemulsion preparations.

Production method of the composition of the present invention The present invention can be produced by a method usually used in the art. For example, it can be produced by adding the above-mentioned ceramide and amino acid and, if necessary, other components to the base so that the blending amount of ceramide and amino acid is in the above range and mixing them.

Method for enhancing stratum corneum moisture retention and moisture transpiration suppression ability In a composition containing ceramide and amino acid, by adding ceramide and amino acid in the above range, the composition retains keratin moisture retention and moisture transpiration suppression. Can be enhanced. Therefore, the present invention also provides a method for enhancing keratin moisture retention ability and moisture transpiration inhibition ability.

Use of composition of the present invention The composition for external use of the present invention has an advantage of exhibiting a high moisturizing effect, that is, a moisture retention effect and a moisture transpiration suppression effect.

  Therefore, the composition for external use of the skin of the present invention is a cosmetic applied to the skin, for example, cosmetic soap, facial cleanser, makeup remover, eye cream, eye shadow, cream, milky lotion, perfume, foundation, funnier, makeup Oil, perfume, powder, pack, tanning oil, sunscreen oil, tanning lotion, sunscreen lotion, tanning cream, sunscreen cream, shaving cream, shaving lotion, blusher, mascara, bath cosmetic, lipstick, lip balm, It can be used as an eyeliner, deodorant agent, bathing agent.

  Moreover, the composition for external use of the skin of the present invention can be used not only as a cosmetic applied to the skin but also as a cosmetic for hair or nails.

  Examples of hair cosmetics include shampoos, rinses, hair dyes, hair nourishing agents, hair restoring agents, eyebrows, and the like.

  Examples of nail cosmetics include nail cream, beautiful nail enamel, and beautiful nail enamel remover.

  The external composition for skin of the present invention can be used as a transdermal pharmaceutical composition or the like in addition to cosmetic use.

  Examples of the transdermal pharmaceutical composition include bactericidal antiseptics, mosquitoes, redheads, purulent diseases, topical analgesics, topical antipruritics, topical astringents, topical antiphlogistics, wormworms, and insecticides. And emollients, hair drugs and the like.

  The external composition for skin of the present invention can take the form of cream, ointment, lotion, gel, liquid and the like.

  Hereinafter, specific embodiments of the present invention will be illustrated using examples.

Preparation of skin external composition Component A (ceramide), Component B (amino acid), Component C (emulsifier, etc.) and Component D (stabilizer, etc.) were added to water according to Table 3 below and mixed. 84 and compositions of Comparative Examples 1-96 were prepared.

  For each of the Examples and Comparative Examples thus prepared, the amount of keratin water and the amount of horny water transpiration were measured by the following procedure.

Measurement of horny water content and horny water transpiration The external environment of the test room was kept at a constant condition of room temperature 20 ± 1 ° C. and humidity 40 ± 5%.

  First, cotton skin soaked with 5% aqueous sodium lauryl sulfate (SDS) was applied to the inner side of the forearm and left blocked for 1 hour to create pseudo rough skin for subjects with dry skin (n = 10). .

  After the cotton was peeled off and the cotton sticking part was washed with water, the test subject was allowed to enter the test room, acclimated for 30 minutes, and the keratin water content and keratin water transpiration amount of the part treated with 5% SDS aqueous solution were measured (after SDS treatment). measured value).

  30 μl of the composition for topical skin or water (negative comparison control) of Comparative Example or Example was applied to the site treated with 5% SDS aqueous solution, and the amount of horny water and the amount of horny water transpiration were measured 1 hour after application (sample application) After measurement).

  In addition, the amount of keratin moisture was measured using SKICON-200 (made by IB S Co., Ltd.), and the amount of keratin moisture transpiration was measured according to the manual of each apparatus using Tewmeter (made by Integral Co., Ltd.) The same).

Calculation of keratin moisture content retention rate The keratin moisture content retention rate was calculated according to the following formula from the measured value of the keratin moisture content after SDS treatment and sample application measured as described above.

Keratin moisture retention rate = 100 × (moisture retention after 1 hour of sample application / moisture retention after SDS treatment)
Calculation of water retention effect per unit amount In order to show the water retention effect of the composition of the present invention, as an index showing the synergistic effect of ceramide and amino acid, the water retention rate converted to a total amount of 1% by weight of component A and component B ( Hereinafter, the moisture retention effect per unit amount was calculated. Specifically, the moisture retention effect per unit amount was calculated from the keratin moisture retention rate calculated as described above and the total concentrations of the A and B components according to the following formula.

Moisture retention effect per unit amount = stratum corneum moisture retention rate / [total concentration of component A and component B (% by weight)]
Calculation of stratum corneum moisture transpiration inhibition rate From the measured values of the amount of horny water transpiration after SDS treatment and sample application measured as described above, the stratum corneum moisture transpiration inhibition rate was calculated according to the following formula.

Keratin moisture transpiration suppression rate = 100 × (Keratin moisture transpiration after 1 hour of sample application−Keratin moisture transpiration after 1 hour of sample application−Keratin moisture transpiration) / Keratin moisture transpiration after SDS treatment
Calculation of keratin moisture transpiration inhibiting effect per unit amount In order to show the keratin moisture transpiration inhibiting effect of the composition of the present invention, the total amount of component A and component B was converted to 1% by weight as an index showing the synergistic effect of ceramide and amino acid. The stratum corneum moisture transpiration inhibiting effect (hereinafter referred to as the moisture transpiration inhibiting effect per unit amount) was calculated. Specifically, the moisture transpiration suppression effect per unit amount was calculated from the keratin moisture transpiration suppression rate calculated as described above and the total concentrations of Component A and Component B according to the following formula.

Moisture transpiration control effect per unit amount = stratum corneum transpiration suppression rate / [total concentration of component A and component B (% by weight)]
Tables 4 to 16 show the keratin moisture retention rate, the moisture retention effect per unit amount, the keratin moisture transpiration suppression rate, and the keratin moisture transpiration suppression effect per unit amount of each Example and Comparative Example.

  Moreover, the component A (ceramide) content (horizontal axis) and the content (vertical axis) of component B (amino acid) of each Example and Comparative Example are shown in logarithmic form in FIG. Furthermore, regarding the total concentration (% by weight) ratio of component A (ceramide) and component B (amino acid), the relational expressions are illustrated by linear expressions.

  In FIG. 1, ● represents a plot of Examples 2, 6, 16, 27, 38, 49, 60, 71 and 82.

  In FIG. 1, ■ indicates Examples 1, 3, 4, 5, 7, 8, 15, 17, 18, 26, 28, 29, 37, 39, 40, 48, 50, 51, 59, 61, 62, 70, 72, 73, 81, 83 and 84 are plotted.

  In FIG. 1, ♦ is a plot of Examples 8 to 14, 19 to 25, 30 to 36, 41 to 47, 52 to 58, 63 to 69, and 74 to 80.

  In FIG. 1, ▲ is a plot of a comparative example.

  Moreover, although not described in Tables 4-16, the thing with the compounding ratio of A component and B component being 1: 2 or less is (triangle | delta), and the compounding ratio of A component and B component is 1:30 or more. Plotted with ×. About these, it was the tendency similar to the comparative example at the point of the keratin moisture retention, the moisture retention effect per unit amount, the keratin moisture transpiration suppression rate, and the keratin moisture transpiration suppression effect per unit amount.

Each composition of each sensory test example and comparative example was applied to the inner part of 10 forearms, and the usability was evaluated in the following 5 levels. The average of the obtained evaluations was rounded off, and “use feeling evaluation” was calculated in 5 stages. The results of the sensory test are shown in Tables 4-16.

(Evaluation)
5 Moist and not sticky or squeaky 4 Moist and almost sticky or squeaky 3 Moist but slightly sticky or squeaky 2 Moist but sticky or squeaky There is.
1 There is no moist feeling

  As shown in Tables 4 to 16 and FIG. 1, the composition has 0.00022 to 0.15% by weight of ceramide and 0.0015 to 0.75% by weight of amino acid, and 1 part by weight of ceramide. On the other hand, the composition for external use of skin containing more than 4 parts by weight and less than 16 parts by weight of amino acid has a keratin moisture retention rate, a moisture retention effect per unit amount, a keratin moisture transpiration suppression rate, and a keratin moisture transpiration per unit amount. The inhibitory effect was high and the moisturizing effect was excellent.

  Specifically, within the above concentration range of ceramide and amino acid in the composition, for example, comparison between Comparative Example 30 (ceramide: amino acid = 1: 4) and Example 71 (ceramide: amino acid = 1: 5), When Comparative Example 31 (ceramide: amino acid = 1: 16) and Example 80 (ceramide: amino acid = 1: 15) were compared, the difference in the blending amount of ceramide and amino acid was very slight. By prescribing the blending ratio of keratin, even for very small amounts of ceramide and amino acids, the keratin moisture retention rate, moisture retention effect per unit amount, keratin moisture transpiration inhibition rate and moisture transpiration inhibition effect per unit amount It can be seen that everything could be improved and that the feeling of use was excellent.

  As shown in FIGS. 2 and 3, when ceramide is added alone (not containing amino acids) in an amount of 0.5% by weight in the composition, the keratin moisture retention is 738%, and 1010 when 1.0% by weight is added. In addition, it was 738% when 1.9% by weight of an amino acid alone (ceramide was not included) and 1002% when 3.05% by weight was added. As can be seen from the results of 0286% by weight of ceramide, 0.171% by weight of amino acid) and Example 82 (0.114% by weight of ceramide, 0.686% by weight of amino acid), the mixing ratio of ceramide and amino acid is defined. Thus, it can be seen that even if the concentration in the composition was low, an excellent keratin moisture retention effect was achieved.

Formulation Examples According to the formulations described in Tables 17 to 24, compositions were prepared as usual.

It is the graph which plotted content of the component A (ceramide) and the component B (amino acid) of each composition of an Example and a comparative example. It is a graph which shows the keratin moisture retention of the composition which mix | blended only ceramide. It is a graph which shows the keratin moisture retention of the composition which mix | blended only the amino acid.

Claims (2)

Skin containing 0.00022 to 0.15% by weight of ceramide and 0.0015 to 0.75% by weight of amino acid in the composition, and 5 to 15 parts by weight of amino acid per 1 part by weight of ceramide Composition for external use. The external composition for skin according to claim 1, which is a cosmetic.

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