JPH0193519A - Antipigmentation drug for external use - Google Patents

Abstract

PURPOSE:To obtain the titled drug for external use, promoting recovery of sunburn by applying to pigmented parts on the skin surface and returning the color to normal skin color, having high safety and capable of withstanding use for a long period, by blending tranexamic acid, salts thereof or a mixture thereof with other ingredients. CONSTITUTION:An antipigmentation drug obtained by blending tranexamic acid, salts thereof or a mixture thereof as an active ingredient with other ingredients. In use, the above-mentioned active ingredient is prepared as a blend with a pharmaceutically acceptable base and other drugs for use. An excipient, such as lactose or starch, binder, such as carboximethyl cellulose, humectant, such as talc, are used as the base to provide a form, such as lotion powder or cream. The amount of the blended active ingredient in the titled drug for external use is 0.0001-50wt.%, preferably 0.2-1wt.%. Furthermore, the tranexamic acid or salts thereof are odorless white crystalline powder, normally used as an antiplasminic agent and having 262-267 deg.C melting point.

Description

DETAILED DESCRIPTION OF THE INVENTION [Industrial Field of Application] The present invention relates to a novel anti-pigmentation external preparation. More specifically, the present invention relates to a highly safe anti-pigmentation external preparation containing tranexamic acid, its salts, or a mixture thereof as an active ingredient.

[Conventional technology]

Pigmentation disorders include pigmentation after sunburn, sparrow spots, melasma,
Examples include melasma, senile pigment spot, petaloid pigmentation disease, actinic keratosis, pigmented nevus, Ota nevus, and Belllock dermatitis. There are still many unknowns about the mechanism by which these pigmentations occur, and in general, genetic predisposition, hormonal abnormalities, irritation from sunlight's ultraviolet rays, skin irritation from photodynamic substances, and aggravation of allergic contact dermatitis are generally involved. It is thought that melanin is abnormally deposited in the skin due to these factors.

Treatment methods for such hyperpigmentation disorders generally include oral administration of substances that suppress melanin production, such as vitamin C and glutathione, or external application of vitamin C1 cysteine, etc. Hydroquinone preparations are used as pharmaceuticals.

In addition, as crude drugs, extracts of Dokkatsu, Kyoukatsu, river cucumber, aloe, pollen, gardenia, mulberry bark, masu hemp, soybean, kudzu root, Cucurbitaceae, etc. (JP-A-56-92208, JP-A-50-13
5236, JP-A-57-77610) and the like are known as anti-pigmentation agents. Also, regarding vitamin C,
3-0-glucosyl-ascorbic acid, N-acyl amino acid ester ascorbic acid, 3-0-monoester ascorbic acid, hydroxypropiophenol ascorbic acid (JP-A-59-27825, JP-A-56-
135411, JP-A-56-161314, JP-A-51-101138), kojic acid related (JP-A-53-1988)
'3538, Unexamined Japanese Patent Publication No. 53-6432, Unexamined Publication No. 54-
92632, JP-A-56-7710, JP-A-56-79
616, JP-A-59-33207), other pantethine, pantethine and their derivatives (JP-A-56-7
3012, JP-A-57-74052, JP-A-58-13
4022, Special IJ No. 59-36606), hydroquinone fatty acid ester (Japanese Patent Application Laid-open No. 57445803, No. 58-154507), dicarboxylic acid ester (
JP-A-58-103319) etc. are known. It is also known that oral administration of tranexamic acid is effective in treating melasma. (West Japan Skin, 47.6., 1
101-1104) Among these drugs, ascorbic acids have problems in terms of stability and are unstable in systems containing water, causing discoloration and odor, and thiol compounds such as glutathione and cysteine have strong off-odors. Moreover, it is easily oxidized and is therefore avoided in external preparations. Furthermore, these compounds, with the exception of hydroquinone, exhibit very slow effects and are therefore not sufficiently effective.

Hydroquinone has been shown to be effective but is sensitizing, is too irritating to Japanese skin, and causes allergic contact dermatitis as a side effect, so its use is restricted in Japan, and its formulation is unstable. It is. Therefore, attempts have been made to monoesterify higher fatty acids in order to improve their safety, but these esters are not necessarily safe because they are decomposed by hydrolytic enzymes in the body.

On the other hand, treatment with oral administration of tranexamic acid is particularly effective for melasma, and is rarely effective for other pigmentation such as ovarian spots. , it is difficult to say that it is necessarily safe.

[Problems to be Solved by the Invention] In view of the above circumstances, the present inventors conducted intensive research to obtain a drug that is highly safe and truly has an excellent anti-pigmentation effect, and as a result, they have found a drug that has anti-plasmin action. The inventors have discovered that tranexamic acid or its salts exhibit sufficient antipigmentation effects and are extremely safe, and have completed the present invention based on this knowledge.

[Means for solving problems]

That is, the present invention provides tranexamic acid or a salt thereof, or
The gist of this invention is an anti-pigmentation external preparation containing a mixture of these as an active ingredient.

The present invention will be explained in detail below.

Tranexamic acid and its salts used in the present invention are generally used as anti-plasmin agents, and are known as components characterized by high safety in cosmetic applications (Japanese Patent Application No. 36,980/1989). The manufacturing method is the second patent
No. 40611, No. 242664, No. 480411,
It is known from No. 488168. Tranexamic acid has a melting point of 262-267°C (decomposition), is a white crystal or powder, has no odor, and has a bitter taste.

Salts of tranexamic acid are commonly used as Mgs
There are metal salts such as Cas K, phosphates, hydrochlorides, hydrobromic acid, sulfates, etc., and derivatives include vitamin A ester, vitamin A ester, vitamin E ester, vitamin C ester, vitamin D ester, etc. Examples include vitamin esters, phenyl esters, N,N-maleoylminotranexamic acid, but are not limited to these.

Hyperpigmentation here refers to sparrow spots, melasma, melasma, senile pigment spots, petaloid pigmentation, actinic keratosis, pigmented nevus, pigmentation due to sunburn, and post-inflammatory pigmentation. Hyperpigmentation, Nevus of Ota, Belllock dermatitis, and other hyperpigmentation disorders that involve pathological deposition of pigment in the body or symptoms similar to it.

External preparations of tranexamic acid, its salts, or mixtures thereof are effective for various types of pigmentation disorders.

(Toxicological properties) Next, the toxicological properties of this substance will be explained.

(1) Acute Toxicity Acute toxicity was investigated by various administration routes using Wister rats and TCP-JCL mice. For oral or transdermal administration, the substance was dissolved in distilled water, and for other administrations, the substance was dissolved in physiological saline, which was adjusted to a predetermined amount using a stomach probe or syringe.

After administration, the symptoms of toxicity were continued to be observed, and the mortality rate over time was determined for up to 7 days, and the LD5o value was determined. The findings were obtained through autopsy in both surviving and dead cases. LD5゜Litchfield-Wilcoxon
) was calculated using the graphical arithmetic method.

The above results indicate that this substance has a high LD in both administrations.
5o, indicating that it is safe as a medicine.

Table 1 No major changes were observed in general symptoms, body weight, feed and water intake, or autopsy findings.

(2) Sensitization Magnuss'on and Kligman (Magnuss'on B
, and Kligman, A.M.). That is, the following method is used.

■ Sensitization induction (1 induction) 20 guinea pigs
Prepare 10 mice for sensitization induction and the other 10 mice for control during induction. Near the guinea pig's shoulder blade, 4 x 6
The area of CN+ is a separate house, shaved, and the following a, b s c
Three pairs of sarcastic injections are performed simultaneously on the left and right sides with midline contrast.

a, FCA total of 0.1 1il in two places on the left and right, 0.05 m1 each (b, 0.05 m1 test sample in each of the two places on the left and right (sample content 10% aqueous solution) C3 test sample, 0.05 m1 each in two places on the left and right One week after the injection, the area near the shoulder blade is pricked again and vaseline containing 10% sodium lauryl sulfate is applied to cause slight inflammation. This treatment enhances sensitization. A test sample is then applied to this area and an occlusion patch is applied.

■Challenge On the 21st day after the start of the sensitization induction operation, the flanks of the guinea pigs in the sensitization treatment group and the control group, measuring 5 x 5 cm, were shaved.
The test sample is diluted with an appropriate solvent and applied as an occlusive for 24 hours. Perform the same operation for the control group.

■Rating i No macroscopic change O ii Mild or slight erythema 1 iii Moderate erythema 2iv Severe erythema and edema 3 ■Results No sensitization reaction was observed in all guinea pigs. This indicates that this substance is safe even when used percutaneously for a long period of time.

(Pharmacological effects) (1) Antipigmentation effects and side effects 8 MOP treatment phototoxic pigmentation Weiser Mapl
Using e-GP, a 50-test sample was applied to the shaved back area once a day in an area of about 4 aa for 8 weeks, and the anti-pigmentation effect and the degree of pigment enhancement that appeared as a side effect were evaluated using a 4-point evaluation method. (+ indicates bleaching effect, - indicates side effects)
The sample used was a suspension of 5% hydroquinone (PG melt) and 5% tranexamic acid PGv.

Table 2 Rating Depigmentation Effect and Pigmentation Table 3 Results Hydroquinone causes pigmentation as a side effect with long-term use, whereas tranexamic acid has an excellent depigmentation effect and does not cause any side effects with long-term use.

(Formulation) Next, the formulation of tranexamic acid, its salt, or a mixture thereof as an anti-pigmentation external preparation will be described.

The anti-pigmentation agent of the present invention is used as a mixture of tranexamic acid, a salt thereof, or a mixture thereof with a pharmaceutically acceptable base and other agents. In particular, the combination of tranexamic acid, its salt, or a mixture thereof with an ultraviolet absorber for the purpose of blocking ultraviolet rays is more effective in preventing sunburn, promoting recovery from sunburn, and preventing and treating hyperpigmentation.

The above-mentioned bases include lactose, starch, calcium carbonate,
Excipients such as magnesium aluminate metasilicate, magnesium aluminum hydroxide, calcium hydrogen phosphate, sugar, lactose, aluminum silicate, and microcrystalline cellulose. Carboxymethylcellulose, polyvinylpyrrolidone, gum arabic, gelatin, sodium alginate,
Binders such as hydroxypropyl starch. Boiling agents such as talc, magnesium stearate, and zinc stearate.

Moisturizers such as glycerin, propylene glycol, and sorbitol. Disintegrants such as agar, silicic anhydride, carboxymethyl cellulose calcium, etc. Other surfactants, buffers,
Preservatives, fragrances, dyes, oils, pigments, water, alcohol, thickeners, preservatives, antioxidants, chelating agents, etc.
These may be used alone or in combination of two or more. However, it is not limited to these.

Examples of the above-mentioned drugs include skin nutrients, enzymes, and current whitening agents.

For example, iodotyrosine and its derivatives, methionine,
Amino acids such as lysine and serine and their derivatives, vitamin A, pantothenic acid, biotin, vitamin 81%; vitamin preparations such as vitamin B2, nicotinic acid, vitamin C, vitamin E, vitamin F and their derivatives; female hormones; Enzymes and hormones such as pituitary hormones, phosphorylase, allantoin, salicylic acid, urea, yoquinin, various plant extracts, anti-inflammatory agents such as glycyrrhizin, glycyrrhizin and their acids and derivatives, inositol, orotic acid, thioctic acid, chondroitin sulfate , hyaluronic acid, etc., but are not limited to these.

Examples of the above-mentioned ultraviolet absorbers include benzoic acid-based para-aminobenzoic acid (hereinafter abbreviated as PABA), PABA monoglycerin diester, N,N-dipropoxy PABA
Ethyl ester, N,N-dimethyl PAnA butyl ester, N. N
-dimethyl PAIIA amyl ester, N,N-dimethyl PABA octyl ester, etc. Anthranilic acids include homomenthyl-N-acetylanthranilate. Salicylic acids include amyl salicylate, menthyl salicylate, homomenthyl salicylate, octyl salicylate,
Phenyl salicylate, pendyl salicylate, p-isoprobanol phenyl salicylate, etc. Cinnamic acid series include octyl cinnamate, ethyl-4-isopropyl cinnamate, methyl-2,5-diisopropyl cinnamate, ethyl-2,4-diisopropyl cinnamate, methyl-2,4-diisopropyl cinnamate, propyl-
p-methoxycinnamate, isopropyl-p-methoxycinnamate, isoamyl-p-methoxycinnamate, octylmethoxycinnamate, 2-ethoxyethylnyl-cinnamate, cyclohexyl-p-methoxycinnamate, ethyl-α-cyano -β-phenylcinnamate, 2-ethylhexyl-α-cyano-β-phenylcinnamate, glyceryl mono-2-ethylhexanoyl diparamethoxycinnamate, etc.

In the benzophenone series, 2,4-dihydroxybenzophenone, 2,2°-dihydroxy-4-methoxybenzophenone, 2.2°-dihydroxy-4.4'-dimethoxyhensiphenone, 2,2°, 4.4' -tetrahydroxybenzophenone, 2-hydroxy-4-methoxybenzophenone, 2-hydroxy-4-methoxy-4
゛-Methylbenzophenone, 2-hydroxy-4-methoxybenzophenone-5-sulfonate, 4-phenylbenzophenone, 2-ethylhexyl-4''-phenylbenzophenone-2-carboxylate, 2-hydroxy-4-n- Octoxybenzophenone, 4-hydroxy-3-carboxybenzophenone, etc.Other UV absorbers include 3-(4'-methylbenzylidene)-d
, 1-camphor, 3-benzylidene-d, 1-camphor, urocanic acid, urocanic acid ethyl ester, 2
-Phenyl-5-methylbenzoxazole, 2.2゛-
hydroxy-5-methylphenylbenzotriazole,
2-(2°-Hydroxy-5″-methylphenyl)benzotriazole, dibenzalazine, dibenzoylmethane, 4-methoxy-4°-t-butyl-dibenzoylmethane, 5-(3,3″-dimethyl-2- Norbornylidene)-3-pentan-2-one, benzalphthalide, and the like.

However, it is not limited to these.

The dosage form of the present invention may be any form used in ordinary pharmaceuticals, quasi-drugs, cosmetics, etc., as long as it is suitable for obtaining the medicinal effect as an anti-pigmentation topical agent, such as lotion, liniment, etc. Examples include liquid preparations for external use such as aqueous solutions and emulsions, solid preparations for external use such as powders and dissolving tablets, semi-solid preparations for external use such as creams, film-type products, ointments, pasta, and jelly, soaps, and the like. Note that internal medicines, injections, etc. may also be effective, and several methods may be used in combination.

The anti-pigmentation topical preparation of the present invention contains tranexamic acid, its salt, or a mixture thereof as an active ingredient at 0.00%.
01 to 50% by weight, preferably 0.01 to 10% by weight,
Particularly preferably, it is blended in an amount of 0.2 to 1% by weight.

If 50% by weight is added, the effect is sufficient; if more than 50% by weight is added, no enhancement of the effect is observed, and if it is less than 0.0001%, it is difficult to obtain a sufficient effect.

(Administration method and dosage) The anti-pigmentation topical agent of the present invention is mainly administered transdermally by directly applying it to the affected area, but other methods such as oral administration, subcutaneous administration, intravenous administration, and intramuscular administration may also be used. Can be done.

The dosage of the anti-pigmentation topical agent of the present invention depends on age, individual differences,
Since it may be affected by the medical condition etc., depending on the case or the purpose of use, doses outside the following range may be administered. However, for external use, tranexamic acid or its salts and mixtures thereof should be administered at o, oos to 20 mg/dose. Spray a small amount of the same amount as a cat on the affected area several times a day. However, it is not limited to this.

(Effect) Next, in order to clarify the anti-pigmentation effect of tranexamic acid, its salt, and a mixture thereof according to the present invention, a practical use test was conducted using an external preparation containing tranexamic acid.

(Test method) A panel of 50 subjects with facial hyperpigmentation was used.
As a comparative example, a product obtained by removing tranexamic acid from Example 1 and replacing it with water was used on the face 2 to 3 times a day, and after 3 months of continuous use, a doctor visually judged the lightening effect. I did it.

Table 4 Results As is clear from the above results, tranexamic acid 2.
It was confirmed that the anti-pigmentation agent containing 5% by weight had an excellent effect with an effectiveness rate of 76.0%.

This product is a highly safe anti-pigmentation prevention and treatment agent that is highly effective against not only melasma but also various types of pigmentation disorders and can withstand long-term use. It has no side effects and is effective in preventing sunburn and promoting recovery, so it can also be used for cosmetic purposes.

〔Example〕

Next, the present invention will be explained in more detail with reference to Examples.

The present invention is not limited to this.

The blending amount is in weight%.

(Example 1) Weight: 9 stones Stearic acid 6.0 Sorbitan monostearate 2.0 Polyoxyethylene (20 mol) 1.5 Sorbitan monostearate Propylene glycol 10.0 Tranexamic acid 2.5 Preservatives/oxidation Preventive agent Appropriate amount fragrance
i! ! quantity ion exchange water
Residue (!i! method) Add tranexamic acid and propylene glycol to ion-exchanged water, heat and keep at 70°C (water phase). Mix other ingredients, heat and melt and keep at 70°C (oil phase).

The oil phase is pre-emulsified by adding the oil phase to the aqueous phase, uniformly emulsified using a homomixer, and then cooled to 30°C while stirring well.

(Example 2) Weight % 95% ethanol 10.
0 Polyoxyethylene (15 moles) 2.0 Oleyl alcohol ether Olive oil 2.0 Preservatives Appropriate amount Fragrance
Appropriate amount polyvinyl alcohol 12.0 glycerin
3.0 Polyethylene glycol 1500 1.0 Tranexamic acid
1.0 ion exchange water
Residue (manufacturing method) Adjust the aqueous phase at 80°C and cool to 50°C. The alcohol phase excluding olive oil is adjusted at room temperature and added to the aqueous phase, then olive oil is added, mixed uniformly, and allowed to cool.

(Example 3) Weight % Stearyl alcohol 7.0 Stearic acid 2.0 Hydrogenated lanolin 2.0 Squalane 5.0 2-Octyldodecyl alcohol 6.0 Polyoxyethylene (25 mol) 3.0 Cetyl alcohol Ether Glycerin Monostearin Acid ester 2.0 Tranexamic acid-vitamin E ester 0.25 Propylene glycol 5.0 Preservative/antioxidant Light fragrance
Appropriate amount of ion exchange water
Residual (method i) Tranexamic acid-vitamin E ester in ion-exchanged water,
Add propylene glycol and heat and keep at 70°C (
aqueous phase). Mix other ingredients, heat and melt and keep at 70℃ (
Pre-emulsify by adding the oil phase to the aqueous phase, homogeneously emulsify with a homomixer, and cool to 30°C while stirring well.

(Example 4) M amount % Solid paraffin 5.0 Beeswax 10.0 Vaseline 15.0 Liquid paraffin 41.0 Glycerin heptanostearate 2.0 Polyoxyethylene (20 mol) 2.0 Sorbitan monolaurate ester Soap powder 0.1 Tranexamic acid 10.0 Borax 0.2 Preservative/antioxidant Percent fragrance
ion exchange water
Residual (M method) Add tranexamic acid, soap powder and borax to ion-exchanged water, heat and melt and keep at 70℃ (water phase), mix other ingredients, heat and dissolve and keep at 70℃ (oil phase) .

The oil phase is gradually added to the water phase while stirring and the reaction is carried out. After the reaction is completed, the mixture is uniformly emulsified with a homomixer, and after emulsification is cooled to 30°C while stirring well.

(Example 5) Weight % Stearic acid 2.5 Cetyl alcohol 2.0 Vaseline 5.0 Liquid paraffin 10.0 Polyoxyethylene (10 mol) 2.0 Monooleic acid ester polyethylene glycol 1500 3.0
Triethanolamine 1.0 Tranexam rR0,01 Preservative/Antioxidant Perfume
Ion-exchanged water Residue (manufacturing method) Add tranexamic acid, polyethylene glycol 1500, and triethanolamine to ion-exchanged water, dissolve by heating, and keep at 70°C (aqueous phase). Mix other ingredients, heat and melt and keep at 70°C (oil phase). Pre-emulsification is performed by adding the oil phase to the water phase, uniformly emulsifying with a homomixer, and after emulsification, cool to 30°C while stirring well.

(Example 6) Weight % Stearic acid 1.5 Cetyl alcohol 0.5 Beeswax
2.0 Polyoxyethylene (20 mol) 1.0 Monooleic acid ester Glycerin monostearate 1.0 Tranexamic acid 0.0001 Quince seed extract (5% aqueous solution) 20.0, Propylene glycol 5.0 Ethyl alcohol 10.0 Preservatives/Antioxidants/Fragrances
ion exchange water
Residue (manufacturing method) Add tranexamic acid and propylene glycol to ion-exchanged water, heat and dissolve, and keep at 70°C (water phase). Add fragrance and ultraviolet absorber to ethyl alcohol and dissolve. (alcohol phase), mix the other components except for the quince seed extract, heat and dissolve and keep at 70°C (oil phase), add the oil phase to the aqueous phase for preliminary emulsification, and uniformly emulsify with a homomixer.

While stirring, add the alcohol phase and quince seed extract. Then cool to 30°C while stirring well.

(Example 7) Weight % Microcrystalline wax 1.9 Beeswax 2.0 Lanolin
2.0 Liquid paraffin 20.0 Squalane
10.0 Sorbitan sesquioleate 4.0 Polyoxyethylene (20 mol) 4
．． 0 Sorbitan monooleate ester Magnesium tranexamate 0.5 Preservative/antioxidant Percent fragrance
Appropriate amount of ion exchange water
Residue (manufacturing method) Tranexamic acid and propylene glycol are heated and dissolved in ion-exchanged water and kept at 70°C (aqueous phase). Mix other ingredients, heat and dissolve and keep at 70°C (oil phase).

While stirring the oil phase, gradually add the water phase to it and uniformly emulsify with a homomixer. After emulsification, cool to 30°C while stirring well.

(Example 8) Weight% 95% ethanol 25.0 Polyoxyethylene (40 mol) 4.0 Hydrogenated castor oil ether Preservative/antioxidant Appropriate amount Fragrance
Dipropylene glycol 15.0 Glycerin
5.0 Sodium hexametaphosphate
Appropriate amount of UV absorber
Appropriate amount of tranexamic acid 0.
2 Ion-exchanged water Residual (manufacturing method) After adjusting the aqueous phase and alcohol phase, dissolve.

(Example 9) M amount% 95% ethanol 10.0
Dipropylene glycol 15.0 Ubiquinone-10, 0,005 Polyoxyethylene (15 mol) 5.0 Oleyl alcohol carboxyvinyl polymer 1.0 (trade name Dicarbopol 941) Tranexamic acid phenyl ester 0.4 Caustic soda 0.15 L -Arginine 0.1 UV absorber Appropriate amount of preservative/antioxidant
Appropriate amount of fragrance
Appropriate amount of ion exchange water
Residue (Production method) Carbopol 941 and tranexamic acid phenyl ester are uniformly dissolved in ion-exchanged water, while dipropylene glycol ether and other components are dissolved in 95% ethanol and added to the aqueous phase. Then, it is neutralized with W-based soda and L-arginine to thicken it.

(Example 10) Weight % Stearic acid 5.0 Stearyl alcohol 4.0 Stearic acid butyl alcohol ester 8.0 Glycerin heptanostearate 2.0 Tranexamic acid
2.0 propylene glycol
20.0 caustic potash
0.2 Preservatives/antioxidants
Appropriate amount of fragrance
Ion-exchanged water Residue (manufacturing method) Add tranexamic acid, propylene glycol and caustic potassium to ion-exchanged water, melt and heat and keep at 70°C (aqueous phase). Mix other ingredients, heat and dissolve and keep at 70°C (oil phase). Gradually add the oil phase to the aqueous phase, and once all has been added, keep at that temperature for a while to allow the reaction to occur. Then, emulsify the mixture uniformly using a homomixer, and cool to 30°C while stirring well.

(Example 11) M amount% 95% ethanol 2.0 Preservative Appropriate amount Fragrance
Appropriate amount of colorant
Appropriate amount of olive oil
2.0 propylene glycol
7.0 zinc white
25.0 kaolin
20.0 Calcium tranexamate
0.1 ion exchange water remainder (
Manufacturing method) Adjust the aqueous phase uniformly at room temperature. Next, the alcohol phase excluding olive oil is added to the aqueous phase adjusted at room temperature, and then olive oil is added and mixed uniformly.

(Example 12) Weight% Kaolin 30.5
Talc 5.0
Zinc white 3.5 Olive oil 2.0 Polyoxyethylene (40 mol) Sorbitan 1.0 Monolauric acid ester propylene glycol 8.0 Fragrance Appropriate amount Preservative
Appropriate amount of tranexamic acid
50.0 (Manufacturing method) Components other than the powder are melted, and this is uniformly sprayed onto the powder part and mixed.

The detailed mechanism of action of the antipigmentation effect of tranexamic acid, its salt, or a mixture thereof according to the present invention is still unclear.

However, the topical anti-pigmentation preparation of the present invention can be applied to pigmented areas of the skin to treat and improve them, and can also be applied to darkened skin after sunburn. This can promote recovery from sunburn and restore normal skin color. Furthermore, it is extremely safe and can withstand long-term operation, so it can prevent pigmentation,
Ideal for treatment.

Claims (1)

[Claims] (1) An anti-pigmentation external preparation characterized by containing tranexamic acid, its salts, or a mixture thereof.