JPH09255551A - Skin preparation for external use - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a highly safe skin preparation for external use capable of preventing and improving skin roughness, having whitening effect to skin. SOLUTION: This skin preparation for external use contains 0.005-20wt.-% (dried weight) based on the total weight of one or more of extracts obtained from a plant belonging to the genus Larrea of the family Zygohyllaceae(e.g. Larrea divaricata) and a plant belonging to the genus Guaiacum(e.g. Guaiacum offinale). Further, 0.01-10wt.% of one or more of compounds selected from among tranexamic acid, or its salts or its derivatives is blended. When needed, an aqueous component, an oil component, a powdery component, a humectant, a thickener, a UV absorber, an antiseptic, an antioxidant, a perfume, a coloring agent, various skin nutrients, etc., can be blended and prepared into a formulation such as a solubilized system, an emulsified system, a power dispersed system, a water-oil double layer system and a water-oil-powder three layer system.

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to an external preparation for skin,
More specifically, the present invention relates to a highly safe external preparation for skin which prevents and improves rough skin and has an excellent whitening effect on the skin.

[0002]

2. Description of the Related Art Various external medicines have been incorporated into external preparations for skin. Preventing rough skin and improving rough skin are one of its medicinal effects.
As the active ingredient of external preparations for skin such as cosmetics for the purpose of these medicinal effects, amino acids and polysaccharides, lipids, extracted extracts, etc., which have an anti-inflammatory effect or have a high moisturizing effect, have conventionally been used in the skin. It has been used because of its excellent ability to prevent inflammation and loss of water in the stratum corneum. However, in any of these cases, the effect of improving and preventing skin roughness is not always sufficient, and development of superior medicinal agents has been expected.

The whitening effect is also one of the characteristics required for external preparations for skin. Although there are some unclear points regarding the mechanism of development such as skin spots, in general, melanin pigment is formed due to abnormal hormones and ultraviolet ray stimulation from sunlight, which is caused by abnormal deposition in the skin. It is believed that. Known methods for treating such spots and bruises include a method of administering a substance that suppresses the production of melanin, and specifically, a method of administering a large amount of vitamin C, a method of injecting glutathione and the like. Alternatively, a method of locally applying L-alcorbic acid, cysteine or the like in the form of an ointment, cream, lotion or the like is used.

However, there is still no external preparation for the skin having the effects of preventing rough skin, improving skin roughening effect and whitening effect, and it has been desired to develop a skin external preparation having more excellent effects.

[0005]

SUMMARY OF THE INVENTION The present invention has been made in view of the above circumstances, and an object thereof is to provide a skin external preparation which is more excellent in the effects of preventing rough skin and improving rough skin, and also has a whitening effect. It is in.

[0006]

[Means for Solving the Problems] In order to solve the above-mentioned problems, the present inventors have selected from among substances having excellent safety, substances having excellent effects of preventing and improving skin roughness and also having a whitening effect. As a result of repeated intensive research to obtain, an extract extracted from a specific plant belonging to the family Zygohyllaceae shows an improving / preventing effect on skin roughness, roughness and pigmentation of healthy people, and further, these plant extract extracts It was found that the combination of 1 or 2 or more selected from tranexamic acid, its salts, or its derivatives shows a more excellent rough skin improving effect and a whitening effect, and the present invention is completed based on this. Came to.

That is, the present invention relates to the family Zygohylla (Zygohylla).
ceae) Laarrea and Guaicam
The present invention provides a skin external preparation containing, as an active ingredient, one or more plant extracts selected from the group consisting of acum).

Here, the plants belonging to the genus Larrea are Larrea divaricat.
a) is preferred. In addition, the above-mentioned genus Guaiacu (Guaiacu
m) is a plant belonging to Guaicam
acum offinale), Guaiacum Sanctum
anctum).

In the present invention, it is preferable that the above plant extract further contains one or more selected from tranexamic acid, salts thereof, or derivatives thereof.

[0010]

BEST MODE FOR CARRYING OUT THE INVENTION Hereinafter, the present invention will be described in detail.

[0012] Zygohylla used in the present invention
Ceae) plants include those belonging to the genus Larrea and the genus Guaiacum, and any one or two or more of them can be used.

As a plant belonging to the genus Larrea, Larrea divaricata is particularly preferably used. This L. diva
ricata) is widely produced in Mexico and is known to contain norguaiaconic acid used as an antioxidant.

As a plant belonging to the genus Guaiacum, there are Guaiacum offina
le) and Guayacam Sanctum are particularly preferably used. Produced in South America and the West Indies, they are used as anti-inflammatory and syphilis drugs, and their main ingredients are guaiaconic acid and guaiaretic acid.
retic acid) and guaiacic acid are known to be contained.

Most preferable among the above-mentioned plants of the family Anopheles is L. divaricata.

The extract of the Anatomicidae used in the present invention can be obtained by a conventional method. For example, whole plants such as leaves, stems, roots and fruits of the Anatomicidae can be dipped or heated with an extraction solvent. It can be obtained by refluxing, filtering and concentrating. As the extraction solvent, any solvent that is usually used for extraction can be used, for example, alcohols such as methanol and ethanol, hydroalcohol,
Organic solvents such as acetone and ethyl acetate can be used alone or in combination.

In the present invention, the extract of the Anopheles family plant has a dry weight of 0.005 to 20% in the total amount of the external preparation.
It is preferable to add 0% by weight, more preferably 0.0
It is 1 to 10.0% by weight. If it is less than 0.005% by weight, sufficient skin roughening preventing / ameliorating effect and whitening effect are not exhibited, while if it exceeds 20.0% by weight, formulation is difficult.
Further, even if the content is 10.0% by weight or more, the effect is not so much improved.

In the present invention, it is preferable to add one or more selected from tranexamic acid or salts thereof or derivatives thereof to the plant extract of the family Anopheles.

Tranexamic acid or a salt thereof or a derivative thereof is generally used as an antiplasmin agent and is known as a highly safe component for cosmetic use (JP-A-42-36980). Moreover, these manufacturing methods are disclosed in, for example, Japanese Patent No. 230611 and Japanese Patent No. 2426.
No. 64, Japanese Patent No. 488168 and the like.

Tranexamic acid has a melting point of 386-390.
C, white crystals or powder, odorless, taste bitter.

The tranexamic acid salts used in the present invention may be those commonly used in cosmetics and the like, and examples thereof include metal salts of magnesium, calcium, potassium and the like, sulfates and the like. It is not limited. Among these, hydrochloride or calcium salt is particularly preferable.

Further, as the derivative of tranexamic acid,
What is normally used for cosmetics, etc., for example,
Vitamin A ester, vitamin E ester, vitamin C
Examples include vitamin esters such as esters and vitamin D esters; alkyl amides such as methyl amide and ethyl amide; N, N-maleyl minotranexamic acid and the like, but the present invention is not limited thereto. Of these, alkyl amides such as methyl amide and ethyl amide are particularly preferable.

In the present invention, the use of one or two selected from the above-mentioned tranexamic acid, its salts, or its derivatives in combination with an extract of the Anopheles family has the effect of preventing and improving skin roughness. The whitening effect can be further improved.

In the present invention, when tranexamic acid or a salt thereof or a derivative thereof is blended, the blending amount thereof is preferably 0.01 to 10.0% by weight in the total amount of the external preparation for skin, more preferably 0. .1 to 5.0% by weight
It is. If it is less than 0.01% by weight, it is difficult to obtain the further improved effect of the present invention, while if it exceeds 10.0% by weight, the effect corresponding to the blending amount cannot be obtained.

The external preparation for skin of the present invention, in addition to the above-mentioned components, may be added, if necessary, within a range that does not impair the effects of the present invention.
Ingredients commonly used in external preparations for skin such as cosmetics, quasi drugs, and pharmaceuticals, for example, aqueous ingredients, oily ingredients, powder ingredients, moisturizers, thickeners, ultraviolet absorbers, preservatives, antioxidants, Fragrances, coloring agents, various skin nutrition agents and the like can be added.

Besides, sequestering agents such as disodium edetate, trisodium edetate, sodium citrate, sodium polyphosphate, sodium metaphosphate, gluconic acid, caffeine, tannin, verapamil, licorice extract,
Grabridine, hot water extract of karin fruit, various crude drugs,
A drug such as tocopherol acetate, glycyrrhizic acid and its derivative or a salt thereof, vitamin C, magnesium ascorbyl phosphate, ascorbyl glucoside, arbutin, kojic acid, glucose, fructose, trehalose and the like saccharides can be appropriately mixed.

The dosage form of the external preparation for skin of the present invention is arbitrary,
For example, any formulation such as a solubilizing system such as lotion, an emulsifying system such as emulsion or cream, an ointment, a powder dispersion system, a water-oil two-layer system, a water-oil-powder three-layer system may be used. .

[0027]

The present invention will be described in more detail with reference to the following examples, but it goes without saying that the technical scope of the present invention is not limited by these examples. The blending amounts are all weight%.

Prior to the Examples, the effect of the external preparation for skin of the present invention applied to the outer skin was evaluated from the improvement rate for rough skin, razor loss and pigmentation. The test method and its evaluation criteria are as follows. I. Skin Roughness Improvement Effect Test (1) Actual Use Test The effect of external skin application of the skin external preparation according to the present invention was evaluated from the improvement rate for rough skin and razor loss.

As a sample, as shown in Table 1,
As the product of the present invention, L. divaricata
Or 2 kinds of guaiacum offalale (G. of finale) alone, 1 kind of laurea divaricata and tranexamic acid are mixed, and as a comparative product, tranexamic acid alone and already applied to rough skin are known. A mixture of the methanol extract of peony is used. (Rough skin improvement rate) A panel of 75 women suffering from rough skin
Fifteen kinds of lotions having the composition (% by weight) shown in Table 1 were applied to the face for each group, with 15 people as one group, and the skin condition was visually determined after 2 weeks. The criteria for judgment are as follows. <Criteria for improvement effect on rough skin> Remarkable effect: Those with disappeared symptoms Effective: Those with weakened symptoms Somewhat effective: Those with slightly weakened symptoms Ineffective: Those with no change in symptoms [Effect of improvement on rough skin [Evaluation] ⊚: The rate at which the test subject is markedly effective, effective and slightly effective (effective ratio) is 80% or more. ○: The ratio at which the test subject is markedly effective, effective and slightly effective (effective ratio) is 50% or more and less than 80%. △ : The rate at which the subject is markedly effective, effective and slightly effective (effective rate) is 30% or more and less than 50% ×: The ratio at which the subject is markedly effective, effective and slightly effective (effective rate) is less than 30% (for razor loss Improving rate) A lotion of 60 male panelists losing razors was applied with a lotion having the composition shown in Table 1 immediately after shaving, and the effect of improving razor loss was evaluated. The criteria for judgment are as follows. <Criteria for improvement effect on razor loss> Remarkable effect: Those who lost razor loss Effective: Those whose razor loss was weakened Somewhat effective: Those whose razor loss was slightly weakened Invalid: Those whose razor loss was not changed [ Evaluation of Improvement Effect Against Razor Loss] ◎: 80% or more of the subjects exhibiting excellent response, effective and moderately effective (efficiency rate) ○: 50% of subjects exhibiting excellent efficacy, effective and moderately effective (effective rate) % Or more and less than 80% Δ: Subject shows a marked response, efficacy and moderate efficacy (efficiency rate) of 30% or more and less than 50% ×: Subject exhibits a significant response, efficacy and moderate efficacy (efficiency rate) of 30 The results are shown in Table 1.

[0030]

[Table 1] As is clear from Table 1, the sample of the product of the present invention containing the plant extract of the family Anopheles is rougher than the sample of the comparative product,
It showed an excellent effect on razor loss, especially when used in combination with tranexamic acid. (2) Actual Use Test by Replica Method Using the present invention products 1, 2 and 3 and comparative products 1 and 2 shown in Table 1, a skin roughness improving effect test was conducted on a human body panel. That is, the skin surface morphology of a healthy female person (face) was taken using a replica method using a milli resin and a skin replica was taken and observed with a microscope (17 times). Twenty people (rough skin panel) judged to have rough skin evaluations 1 and 2 based on the following criteria based on the state of the skin pattern and the peeling state of the stratum corneum were used, and the products of the present invention 1, 2, and 3 were applied to the left and right half of the face. And lotions of Comparative Products 1 and 2 were applied once a day for 2 weeks. Two weeks later, the skin condition was observed again according to the replica method described above, and evaluated according to the following criteria. Table 2 shows the results. <Criteria> 1: Disappearance of sulcus and crust, wide area of corneal swelling are observed 2: Unsmooth sulcus and crest, horny corneal swelling are observed 3: Skin sulcus and crust are observed However, it is flat 4: Crusts and crests are clear. 5: Crusts and crests are clear and well-ordered.

[0031]

[Table 2] As is clear from Table 2, the lotion of the product of the present invention had a remarkable effect of improving rough skin, as compared with the lotion of the comparative product. II. Whitening test (1) Anti-pigmentation effect and side effects 8-MOP-treated phototoxic pigmentation Weiser Map
Using le GP (guinea pig), 50 μl of the sample was applied to the shaved back once a day in the range of about 4 cm ² for 8 weeks, and the anti-pigmentation effect and the degree of pigment enhancement appearing as a side effect are shown in Table 3. The evaluation was carried out by the 4-point evaluation method shown below (+ evaluation point is decolorizing effect, − evaluation point is side effect), and the results of both of these were comprehensively evaluated. The sample was 1% ascorbic acid solution,
The invention product 1 shown in Table 1 was used. The results are shown in Table 4.

[0032]

[Table 3]

[0033]

[Table 4] As is clear from Table 4, long-term continuous use of ascorbic acid causes pigmentation as a side effect, whereas the product 1 of the present invention (mixed solution of Laurea divaricata extract and tranexamic acid) has an excellent decolorizing effect and a long-term effect. There were no side effects from repeated use. (2) Practical use test The effect of external application of the external preparation for skin according to the present invention was evaluated from the improvement rate for pigmentation of spots, freckles and the like.

As the samples, as shown in Table 5, two kinds of Lara divaricata or L. divaricata or G. One kind of compound containing tranexamic acid was used as a comparative product, and one containing tranexamic acid alone and a methanol extract of cyperaceae, which is already known to be used as a whitening agent, was used. (Percentage of improvement in pigmentation) A panel of 75 people suffering from dark skin on the face, stains, freckles, etc. was set as 15 groups, and Table 5
5 types of lotions having the composition (% by weight) shown in each group were applied to the face 2 to 3 times a day for each group, and the whitening effect was evaluated after continuous use for 3 months. The criteria for judgment are as follows. <Criteria for whitening effect on spots, freckles, etc.> Remarkable effect: Those with disappearance of symptoms Effective: Those with weakened symptoms Somewhat effective: Those with slightly weakened symptoms Ineffective: Those with no change in symptoms [Blemish, Evaluation of whitening effect on freckles] ◎: 80% or more of the subjects exhibiting excellent efficacy, effective and moderately effective (effective rate) ○: 50% of subjects exhibiting excellent efficacy, effective and moderately effective (effective ratio) % Or more and less than 80% Δ: Subject shows a marked response, efficacy and moderate efficacy (efficiency rate) of 30% or more and less than 50% ×: Subject exhibits a significant response, efficacy and moderate efficacy (efficiency rate) of 30 The results are shown in Table 5.

[0035]

[Table 5] As is clear from Table 5, the lotion of the product of the present invention exhibited a whitening effect superior to that of the lotion of the comparative product, and the effect was further improved when used in combination with tranexamic acid.

Example 1: Toner lotion blending ingredients wt% Laria divaricata methanol extract 0.01 tranexamic acid 5.0 glycerin 1.0 ethanol 7.0 polyoxyethylene (20 mol) oleyl alcohol 0.5 ether methylparaben 0 .05 citric acid 0.01 sodium citrate 0.1 perfume 0.01 purified water balance A skin external preparation (lotion) was produced by a conventional method with the above composition,
When evaluated according to each of the above criteria, good effects of preventing and improving rough skin and whitening effects were obtained.

Example 2: Cream formulation ingredients wt% cetostearyl alcohol 3.5 squalane 30.0 beeswax 3.0 reduced lanolin 5.0 ethylparaben 0.3 polyoxyethylene (20 mol) oleyl alcohol 2.0 ether stearin Acid monoglyceride 2.0 Guayacum offinale Methanol extract 1.0 Glycerin 15.0 Fragrance 0.03 Purified water balance A skin external preparation (cream) having the above composition was prepared by a conventional method, and evaluated according to the above criteria. Good skin roughening prevention / improvement effect and whitening effect were obtained.

Example 3: Packing agent composition% by weight Laria divaricataacetone extract 3.0 Tranexamic acid vitamin E ester 8.0 Polyvinyl alcohol 10.9 Propylene glycol 7.0 Ethanol 10.0 Methylparaben 0.05 Perfume 0.05 Purified water balance A skin external preparation (packing agent) was produced by the usual method with the above composition and evaluated according to each of the above criteria. As a result, good skin roughening preventing / ameliorating effect and whitening effect were obtained.

Example 4: Emulsion blending ingredients% by weight Microcrystalline wax 1.0 Beeswax 2.0 Lanolin 20.0 Liquid paraffin 10.0 Squalane 5.0 Sorbitan sesquioleate 4.0 Polyoxyethylene (20 mol) Sorbitan 1.0 Monooleic acid ester Guayacam Sanctam Ethanol extract 10.0 Propylene glycol 7.0 Sodium bisulfite 0.01 Preservative / Antioxidant Appropriate amount Fragrance Appropriate amount Purified water Residual skin When an external preparation (milky lotion) was produced and evaluated according to the above criteria, good prevention of rough skin
An improving effect and a whitening effect were obtained.

Example 5: Composition of cosmetic lotion wt% 95% ethanol 25.0 polyoxyethylene (40 mol) hydrogenated castor oil 4.0 preservative / antioxidant proper amount perfume proper amount dipropylene glycol 12.0 glycerin 5 0.0 Arapitol 7.0 Guayacam Sanctum methanol extract 1.0 Tranexamic acid methylamide 0.1 Purified water balance A skin external preparation (lotion) is produced by a conventional method with the above composition,
When evaluated according to each of the above criteria, good effects of preventing and improving rough skin and whitening effects were obtained.

Example 6: Ingredients for beauty solution wt% 95% ethanol 10.0 polyoxyethylene (20 mol) octyl 1.0 dodecanol pantothenyl ethyl ether 0.1 Laria divaricata acetone extract 1.5 methylparaben 0. 15 Potassium hydroxide 0.1 Glycerin 5.0 Dipropylene glycol 10.0 Sodium bisulfite 0.03 Carboxyvinyl polymer 0.2 (“Carbopol 940”, manufactured by BF Goodrich) Purified water balance The skin external preparation (beauty solution) is manufactured by the method,
When evaluated according to each of the above criteria, good effects of preventing and improving rough skin and whitening effects were obtained.

Example 7: Lipstick compounding ingredients% by weight Microcrystalline wax 1.0 Beeswax 2.0 Lanolin 2.0 Liquid paraffin 20.0 Squalane 10.0 Sorbitan sesquioleate 4.0 Polyoxyethylene (20 mol) Sorbitan monooleate 4.0 Tranexamic acid calcium salt 0.5 Laria divaricata ethanol extract 0.01 Preservative / antioxidant Appropriate amount Fragrance Appropriate amount Purified water Remainder Using the above composition, a skin external preparation (lipstick) ) Was manufactured and evaluated according to each of the above criteria.
An improving effect and a whitening effect were obtained.

Example 8: Jelly compounding ingredients wt% 95% ethanol 10.0 dipropylene glycol 15.0 polyoxyethylene (50 mol) oleyl alcohol ether 2.0 carboxyvinyl polymer 1.0 ("Carbopol 940", BF Goodrich) caustic soda 0.15 L-arginine 0.1 tranexamic acid ethylamide 1.0 guaiacum offinale 50% ethanol aqueous solution extract 0.2 2-hydroxy-4-methoxybenzophenone sodium sulfonate 0.05 ethylenediaminetetraacetate・ 3 Sodium ・ 2 water 0.05 Preservative / antioxidant Proper amount Perfume Proper amount Purified water Remainder A skin external preparation (jelly) is produced by the conventional method with the above composition,
When evaluated according to each of the above criteria, good effects of preventing and improving rough skin and whitening effects were obtained.

[0044]

As described in detail above, according to the present invention,
It is possible to provide a highly safe external preparation for skin, which has excellent effects of preventing and improving rough skin and also having a whitening effect on the skin.

──────────────────────────────────────────────────続 き Continued on the front page (51) Int.Cl. ⁶ Identification code Agency reference number FI Technical display location A61K 35/78 ADA A61K 35/78 ADAC

Claims (8)

[Claims] 1. A skin external preparation containing as an active ingredient an extract of one or more plants selected from the genus Larrea and the genus Guaiacum of the family Zygohyllaceae. 2. The external preparation for skin according to claim 1, wherein the plant belonging to the genus Larrea is Larrea divaricata. 3. The external preparation for skin according to claim 1 or 2, wherein the plant belonging to the genus Guaiacum is at least one of Guaiacum offinale and Guaiacum sanctum. 4. The blending amount of the extract is 0.005 to 20.0% by weight (dry weight) in the total amount of the external preparation for skin.
The external preparation for skin according to any one of claims 1 to 3. 5. The external preparation for skin according to any one of claims 1 to 3, further comprising one or more selected from tranexamic acid or a salt thereof or a derivative thereof. 6. The external skin preparation according to claim 5, wherein the salt of tranexamic acid is tranexamic acid hydrochloride or calcium salt. 7. The external skin preparation according to claim 5, wherein the derivative of tranexamic acid is an alkylamide derivative such as methylamide or ethylamide. 8. The compounding amount of one or more selected from tranexamic acid or a salt thereof or a derivative thereof is 0.01 to 10.0% by weight in the total amount of the external preparation for skin. The external preparation for skin according to any one of 1 to 7.