JPH10265321A - Skin preparation for external use - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a skin preparation for external use having practically sufficient beautifying and whitening effects by including tranexamic acid or its derivative and a plant extract or a crude drug essence having the beautifying and whitening actions therein. SOLUTION: This skin preparation for external use is obtained by formulating (A) one or more selected from tranexamic acid and its derivative (a dimer, an ester derivative with hydroquinone, an ester derivative with gentisic acid, an amide derivative, etc.) with (B) at least one of a plant extract and a crude drug essence having beautifying and whitening actions (Gambir, Matricaria chamomilla L., Aloe, Scutellaria Radix, Saxifraga stolonifera Meerburg, Sophora angustifloria Sieb. et Zucc., Sophorae Radix, Betula platyphylla Sukatchev var. japonica Hara, birch, Phellodendri Cortex, Lithospermi Radix, etc.). The amounts of the ingredients based on the total amount of the skin preparation for external use are 0.001-20 wt.%, preferably 0.01-10 wt.%, especially preferably 0.1-7 wt.% ingredient A and 0.001-20 wt.%, preferably 0.1-5 wt.% ingredient B.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a highly safe external preparation for skin which has significantly improved skin whitening effect.

[0002]

2. Description of the Related Art Pigments such as skin spots and freckles are stimulated by abnormal hormones and ultraviolet rays, resulting in increased production of melanin in epidermal pigment cells and excessive deposition of melanin on the epidermis. Occurs. To prevent spots and freckles, it has been reported that tranexamic acid, a substance that suppresses the production of melanin, is applied topically in the form of an ointment, cream, lotion or the like.

[0003]

However, the expected effects of tranexamic acid have not yet been satisfactory. An object of the present invention is to provide a skin external preparation which enhances the whitening effect of tranexamic acid and has a practically sufficient whitening effect.

[0004]

In view of such circumstances, the present inventors have conducted intensive studies to obtain a skin external preparation having a truly excellent whitening effect. As a result, the present inventors have found that tranexamic acid and derivatives thereof are obtained. One or more selected from the group, and found that a synergistic whitening effect can be obtained by using at least one plant extract or crude drug extract having a whitening effect, and completed the present invention. . That is, claim 1 of the present invention is a skin external preparation characterized by containing one or more selected from tranexamic acid and derivatives thereof and at least one plant extract or crude drug extract having a whitening effect. is there.

[0005] In a second aspect of the present invention, the plant extract or herbal extract having a whitening effect in the external preparation for skin according to the first aspect is characterized in that the extract is Asenyaku, Chamomile, Aloe, Ogon, Yukinoshita, Clara, Kujin, Birch, Birch. , Oak, sicon, emisoso, age, rosemary,
Salvia, ginger, marronnier, perilla, koradekabaro, lumpuyan, kanokoso, cuckoo, licorice, shiitake, carrot, litchi, komenuka, senkyu, peach, ginkgo, senburi, apricot, saffron, mint,
An external preparation for skin characterized by being at least one of kyonin, goldfish, buttonpig, horsetail, gypsophila, peonies, butterflies, hamamelis or an extract thereof.

In a third aspect of the present invention, the amount of the plant extract or herbal extract having a whitening effect in the external preparation for skin according to the first or second aspect is 0.001 to 0.001 of the total amount of the external preparation for skin.
20% by weight of a skin external preparation.
According to a fourth aspect of the present invention, the amount of one or more tranexamic acids and derivatives thereof in the external preparation for skin according to the first to third aspects is 0.001 to 20% by weight based on the total amount of the external preparation for skin. An external preparation for skin, characterized in that:

Hereinafter, the configuration of the present invention will be described in detail. Tranexamic acid used in the present invention has an inhibitory effect on the tyrosinase reaction, which is the rate-limiting step of melanin production.
Examples of the tranexamic acid derivative used in the present invention include a tranexamic acid dimer (trans-4- (trans-4-aminomethylcyclohexanecarbonyl) aminomethylcyclohexanecarboxylic acid hydrochloride) and an ester form of tranexamic acid and hydroquinone (trans 4-aminomethylcyclohexanecarboxylic acid 4'-hydroxyphenyl ester), an ester form of tranexamic acid and gentisic acid (2- (trans-4-aminomethylcyclohexylcarbonyloxy) -5-hydroxybenzoic acid and a salt thereof), tranexam Amide of acid (trans-4-
Aminomethylcyclohexanecarboxylic acid methylamide and salts thereof, trans-4-acetylaminomethylcyclohexanecarboxylic acid and salts thereof, trans-4-
(P-methoxybenzoyl) aminomethylcyclohexanecarboxylic acid and salts thereof, trans-4-guanidinomethylcyclohexanecarboxylic acid and salts thereof, and the like.

The amount of one or more selected from tranexamic acid and its derivatives to be incorporated in the external preparation for skin according to the present invention is not particularly limited. 001 to 20% by weight, preferably 0.01 to 10% by weight, particularly preferably 0.1 to 7% by weight. If the amount is less than 0.001% by weight, the skin whitening effect of the external preparation tends to be poor.
Even if it is added in excess of 0% by weight, an increase in the effect cannot be substantially expected, and it tends to be difficult to incorporate it into an external preparation for skin.

[0009] The plant extract or herbal extract having a whitening effect to be incorporated in the external preparation for skin according to the present invention may be any one having a whitening effect.

The amount of the plant extract or herbal extract having a whitening effect is not particularly limited, but is generally 0.001 to 20% by weight, preferably 0.1 to 5% by weight, based on the total amount of the external preparation for skin. %. When the amount is less than 0.001% by weight, the skin whitening effect of the external preparation for skin and the effect of suppressing the skin irritation of the external preparation tend to be poor. Is substantially not expected, and it tends to be difficult to incorporate into skin external preparations.

The external preparation for skin of the present invention contains, in addition to the above essential components, other components usually used in external preparations for skin such as cosmetics and pharmaceuticals, such as oils, wetting agents, ultraviolet absorbers, antioxidants, and surfactants. , A preservative, a humectant, a fragrance, water, alcohol, a thickener and the like can be appropriately compounded as required. The dosage form of the external preparation for skin according to the present invention is arbitrary and, for example, a solubilizing system such as a lotion, an emulsion, an emulsifying system such as a cream,
Alternatively, any dosage form such as an ointment and a dispersion can be used.

[0012]

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 to these examples. In addition, in the following examples, the compounding amount is% by weight.

First, an effect test method and an evaluation method will be described prior to Examples. The whitening effect was determined from use tests such as the skin whitening effect by cumulative application, the removal of spots and freckles, and the like.

(1) Whitening effect (Testing method) A subject suffering from darkness, spots, freckles, etc., one sample lotion in the morning and evening
It was applied to the face every day for 3 months and its whitening effect was examined after 3 months. Examples 1 to 7 and Comparative Examples 1 to 7 with the following formulation
8 were tested. Samples of Examples 1 to 7 and Comparative Examples 1 to 8 (alcohol phase)% by weight 95% Ethanol 25.0 Polyoxyethylene (25 mol) hydrogenated castor oil ether 2.0 Preservative / Antioxidant Appropriate amount Fragrance Appropriate amount Drug (described in Table 1) (Aqueous phase) Glycerin 2.0 Propylene glycol 1.0 Ion-exchanged water Residue (Preparation method) Prepare aqueous phase and alcohol phase and solubilize.

[0015]

[Table 1]

(Evaluation Criteria) Significant Effect: Pigmentation became almost inconspicuous. Effective; very thin. Somewhat effective: Somewhat thin. Ineffective: no change (judgment) ◎: The proportion of the test subjects showing significant efficacy and effectiveness (effective rate) is 80% or more ○: The proportion of the test subjects showing significant efficacy and efficacy (effective rate) Is greater than or equal to 50% and less than 80% Δ: The proportion of effective and effective among testees (effective rate) is 30% or more and less than 50% ×: The proportion of excellent and effective among examinees (Effective rate) is less than 30%

[0017]

[Table 2]

As is evident from Table 2, it was recognized that the Examples had a better skin whitening effect than the Comparative Examples.

Example 8 Vanishing cream stearic acid 6.0 sorbitan monostearate 2.0 polyoxyethylene (20 mol) sorbitan monostearate 1.5 tranexamic acid 2.0 propylene glycol 10.0 5.0 Preservative / Antioxidant Appropriate amount Fragrance Appropriate amount Ion-exchanged water residue (Preparation method) Add enmeiso, tranexamic acid and propylene glycol to ion-exchanged water and heat to 70 ° C (aqueous phase). The other components are mixed, melted by heating and kept at 70 ° C. (oil phase). Add oil phase to water phase, pre-emulsify and homogenize with homomixer.
Cool down to

Example 9 Neutral Cream Stearyl Alcohol 7.0 Stearic Acid 2.0 Hydrogenated Lanolin 2.0 Squalane 5.0 2-Octyldo Deserial Call 6.0 Polyoxyethylene (25 mol) Cetyl Alcohol Ether 3 2.0 Glycerin monostearate 2.0 Placenta extract 0.1 Tranexamic acid 1.0 2-Ethylhexyl paramethoxycinnamate 2.5 Propylene glycol 5.0 Licorice extract 10.0 Perfume Appropriate preservative / antioxidant Appropriate amount Ion-exchanged water residue (Preparation method) Addition of licorice extract, placenta extract,
Add tranexamic acid and propylene glycol and heat to maintain at 70 ° C. (aqueous phase). The other components are mixed, melted by heating and kept at 70 ° C. (oil phase). The oil phase is added to the water phase to perform preliminary emulsification, and after uniform emulsification with a homomixer, the mixture is cooled to 30 ° C. while stirring well.

Example 10 Cold cream Solid paraffin 5.0 Beeswax 10.0 Vaseline 15.0 Liquid paraffin 41.0 Glycerin monostearate 2.0 Polyoxyethylene (20 mol) Sorbitan monolaurate 2.0 Tranexamic acid 4.0 Soap powder 0.1 Borax 0.2 Chamomile extract 0.1 Ion-exchanged water Residual perfume Appropriate amount Preservative / antioxidant Appropriate amount (Production method) Chamomile extract, ionized water, tranexamic acid, Soap powder and borax are added and dissolved by heating, and kept at 70 ° C. (aqueous phase). The other components are mixed, melted by heating and kept at 70 ° C. (oil phase). The oil phase is gradually added to the aqueous phase while stirring to carry out the reaction. After the completion of the reaction, the mixture is uniformly emulsified with a homomixer, and cooled to 30 ° C. while stirring well after emulsification.

Example 11 Emulsion Polyoxyethylene (20 mol) Polyoxypropylene (2 mol) Cetyl alcohol 1.0 Silicone KF96 (20 cs) (Shin-Etsu Chemical) 2.0 Liquid paraffin (medium viscosity) 3.0 Propylene glycol 5.0 Tranexamic acid 2.0 Glycerin 2.0 Ethanol 15.0 Carboxyvinyl polymer 0.3 Hydroxypropylcellulose 0.1 2-Aminomethylpropanol 0.1 Preservative Appropriate amount Aloe extract 20.0 Deionized water residue (Preparation method) The aqueous alcohol extract of the aloe extract and tranexamic acid are dissolved by heating in ion-exchanged water and ethanol, and the water-soluble components such as propylene glycol are dissolved, and the mixture is kept at 70 ° C. (aqueous phase). Mix with other oily ingredients,
Heat to melt and maintain at 70 ° C (oil phase). The oil phase is added to the water phase, preliminarily emulsified, homogenized with a homomixer, emulsified, and cooled to 30 ° C. while stirring well.

Example 12 Emulsion Polyoxyethylene (20 mol) Polyoxypropylene (2 mol) Cetyl alcohol 1.0 Silicone KF96 (20cs) (Shin-Etsu Chemical) 2.0 Liquid paraffin (medium viscosity) 3.0 Propylene glycol 5.0 Ascorbic acid-2-glucoside 5.0 Tranexamic acid 5.5 tert-butyl-4'-methoxybenzoylmethane 3.0 Glycerin 2.0 Ethanol 15.0 Carboxyvinyl polymer 0.3 Hydroxypropylcellulose 0.1 2-Aminomethylpropanol 0.1 Preservative Appropriate amount Marronnier extract 7.0 Ion-exchanged water residue (Preparation method)
The tranexamic acid is dissolved by heating, and the water-soluble component of propylene glycol or lower is dissolved, and kept at 70 ° C. (aqueous phase). The other oil components are mixed, heated and melted and kept at 70 ° C. (oil phase). The oil phase is added to the water phase, preliminarily emulsified, and uniformly emulsified by a homomixer. After emulsification, the mixture is cooled to 30 ° C. while stirring well.

The external preparation for skin according to the present invention is a highly safe external preparation for skin with significantly improved skin whitening effect.

Claims (4)

[Claims] 1. An external preparation for skin, comprising tranexamic acid and a derivative thereof, and a plant extract or herbal extract having a whitening effect. 2. The external preparation for skin according to claim 1, wherein the plant extract or herbal extract having a whitening effect is acacia catechu, chamomile, aloe, ogon, yukinosita, clara, kujin, birch, birch, oakaku, sicon, emmeiso, Ages, rosemary, salvia, ginger, marronnier, perilla, koradekabaro, rumpuyan, kanokoso, cuckoo, licorice, shiitake mushroom, carrot, reishi, komenuka, senkyu, peach, ginkgo, apricot, apricot, saffron, mentha, kyonin, goldfish An external preparation for skin, characterized by being at least one of buttoned pigeon, horsetail, diatom, peonies, clove, hammeris or an extract thereof. 3. The external preparation for skin according to claim 1 or 2, wherein the amount of the plant extract or herbal extract having a whitening effect is 0.001 to 20% by weight based on the total amount of the external preparation for skin. External preparation for skin. 4. The external preparation for skin according to claim 1, wherein
One or more of tranexamic acid and its derivatives are contained in an amount of 0.001 to 20% by weight based on the total amount of the external preparation for skin.
An external preparation for skin, characterized in that: