WO2006003965A1

WO2006003965A1 - Skin-whitening compositions

Info

Publication number: WO2006003965A1
Application number: PCT/JP2005/012025
Authority: WO
Inventors: Yoshinobu Morimoto; Asami Watake
Original assignee: Daiichi Sankyo Healthcare Co., Ltd.
Priority date: 2004-06-30
Filing date: 2005-06-30
Publication date: 2006-01-12
Also published as: JPWO2006003965A1

Abstract

The invention provides compositions for the whitening of the skin or the prevention and/or treatment of melanopathies which exhibit excellent efficacy against melanopathies such as melasma, ephelis, sunburn, dark skin, or melanosis caused by drugs such as steroids. Namely, (1) a composition containing (i) tranexamic acid or a salt thereof (preferably tranexamic acid) and (ii) a pantethine (preferably pantethine); and (2) a composition containing (i) tranexamic acid or a salt thereof (preferably tranexamic acid), (ii) a pantethine (preferably pantethine), (iii) L-cysteine, a derivative thereof, a salt of either (preferably L-cysteine), and (iv) L-ascorbic acid, a derivative thereof, or a salt of either (preferably L-ascorbic acid).

Description

Specification

Whitening composition

Technical field

[0001] The present invention relates to a novel composition, and more particularly to a whitening composition (whitening agent).

Background art

[0002] Pigmentation such as skin melanosis caused by drugs such as stains, freckles, sunburn, dark skin and steroids, is caused by excessive deposition of melanin pigment on the skin. It is a cytoplasmic granule melanoma in melanocytes. Tyrosine is oxidized by tyrosinase, biosynthesis of dopa and dopaquinone. Furthermore, dopaquinone is converted to indoquinone by auto-oxidation by ultraviolet rays, and melanin is produced through complicated pathways. It is known to be synthesized. Such pigmentation is particularly cosmetically favorable for women.

Conventionally, as a pigmentation prevention / treatment agent (whitening agent), L-ascorbic acid and its derivatives (see Patent Document 1), kojic acid (see Patent Document 2), L-cysteine (see Patent Document 3), arbutin ( Known are Patent Document 4), Arctostaphylos uva-ursi, an extract thereof (see Patent Document 5), a combination of tranexamic acid and ascorbic acid (Patent Document 6), and the like.

However, the above is not always satisfactory in terms of its effect.

Patent Document 1: JP-A-49-86554

Patent Document 2: JP-A-53-3538

Patent Document 3: Japanese Patent Application Laid-Open No. 59-128320

Patent Document 4: Japanese Patent Application Laid-Open No. 60-56912

Patent Document 5: JP-A-6-166609

Patent Document 6: Japanese Patent Laid-Open No. 4-243825

Disclosure of the invention

Problems to be solved by the invention

[0003] The present invention provides a novel composition, specifically, a whitening composition (whitening agent) having an excellent effect. To do.

Means for solving the problem

[0004] As a result of intensive studies, the present inventors have used tranexamic acid or a salt thereof, and panthetins in combination, as well as L-cysteine, a derivative thereof or a salt thereof, L-ascorbic acid, a derivative thereof. Or, when these salts are further used in combination, it has been newly found out that an excellent whitening effect is exhibited, and the present invention has been completed.

[0005] That is, the present invention relates to the following.

(1) A composition comprising (i) tranexamic acid or a salt thereof, and (ii) panthetins.

(2) (i) tranexamic acid or a salt thereof, (ii) panthetins, (iii) L cysteine, a derivative thereof or a salt thereof, and (iv) a composition containing L ascorbic acid, a derivative thereof or a salt thereof object.

(3) Use of the composition of (1) or (2) above for whitening agent, prevention of pigmentation and production of Z or therapeutic agent.

(4) A whitening method characterized by administering an effective amount of (i) tranexamic acid or a salt thereof, and (ii) a panthetin, and a method for preventing and / or treating pigmentation.

(5) An effective amount of (i) tranexamic acid or a salt thereof, (ii) panthetins, (iii) L cysteine, a derivative thereof or a salt thereof, and (iv) L ascorbic acid, a derivative thereof or a salt thereof. A whitening method characterized by administering, and a prevention and Z or treatment of pigmentation.

The invention's effect

[0006] The composition of the present invention has an excellent melanin pigmentation inhibitory effect as described in Examples below. Therefore, the composition of the present invention can be used as a whitening composition (whitening agent), as well as for prevention of pigmentation such as skin darkening caused by drugs such as spots, freckles, sunburn, dark skin and steroids, and Z or Useful as a therapeutic composition.

BEST MODE FOR CARRYING OUT THE INVENTION

[0007] Tranexamic acid (trans-4 aminomethylcyclohexanecarboxylic acid) or a salt thereof, which is useful in the present invention, is a known compound, and a commercially available product may be used as a method for obtaining the same. Can also be manufactured. As a salt of tranexamic acid, List mineral salts such as hydrochloride, nitrate and sulfate, organic acid salts such as methanesulfonate, alkali metal salts such as sodium salt, potassium salt, calcium salt and magnesium salt, alkaline earth metal salts, etc. Can do. In the present invention, tranexamic acid or a salt thereof is preferably tranexamic acid.

[0008] The pantethins that are useful in the present invention are known compounds, and as a method for obtaining them, commercially available products may be used, or they can be produced based on known methods. Panthetins include pantothenyl alcohol, pantothenyl ether, acetyl pantotenyl ether, benzoyl pantotenyl ether, dicarboethoxy pantothenic acid ethyl ester, nontethein, panthetin, phosphopanthetin, pantothenic acid And a salt of pantothenic acid. Examples of the salt of pantothenic acid include mineral salts such as hydrochloride, nitrate and sulfate, alkali metal salts such as sodium salt, potassium salt, calcium salt and magnesium salt, and alkaline earth metal salt. . In the present invention, pantethine, pantothenic acid, and pantothenic acid salt are preferred as pantetins, and as pantothenic acid salt, calcium pantothenate is preferred.

[0009] L-cysteine, a derivative thereof, or a salt thereof that is useful in the present invention is a known compound, and as a method for obtaining the L-cysteine, a commercially available product may be used, or it can be produced based on a known method. . L-cysteine derivatives include N-acetyl-L-cysteine, L-homocistine, L-cysteic acid, L-homocysteic acid, L-cysteine sulfinic acid, S-sulfino-L L-cysteine, S-sulfo-L-cysteine, cystine (systemine). Dimer) and the like. As salts of L-cysteine and its derivatives, mineral salts such as hydrochloride, nitrate and sulfate, alkali metal salts such as sodium salt, potassium salt, calcium salt and magnesium salt, and alkaline earth metal salts and the like can be used. Can be mentioned. In the present invention, L-cysteine is preferred as L-cysteine, a derivative thereof, or a salt thereof.

[0010] L-ascorbic acid, a derivative thereof or a salt thereof, which is useful in the present invention, is a known compound, and a commercially available product may be used as a method for obtaining the product, or the production may be performed based on a known method. You can also. As salts of L-ascorbic acid and its derivatives, mineral salts such as hydrochloride, nitrate, sulfate, sodium salt, potassium salt, calcium salt, magnesium Examples thereof include alkali metal salts such as salts and alkaline earth metal salts. L-ascorbic acid, its derivatives or salts thereof include L-ascorbic acid; L-ascorbate such as sodium L-ascorbate, magnesium L-ascorenolevate, potassium L-ascorenolate, calcium L-ascorbate; L-ascorbic acid monostearate Ascorbic acid monofatty acid esters such as Late, L-ascorbic acid monopalmitate, L-ascorbic acid monooleate; L-ascorbic acid difatty acid esters such as L-ascorbic acid distearate, L-ascorbic acid dinormitate, L-ascorbic acid dioleate; L-ascorbic acid trifatty acid esters such as acid tristearate, L-ascorbic acid tripalmitate, L-ascorbic acid trioleate; L-ascorbyl sulfate, L-ascorbi L-corcorbic acid sulfates such as sodium sulfate, potassium L-corcorbyl sulfate, magnesium L-corcorbyl sulfate, calcium L-corcorbyl sulfate; L-corcorbyl phosphate, sodium L-corcorbyl phosphate, L- potassium potassium corsyl phosphate And L-ascorbic acid phosphates such as L-ascorbyl magnesium phosphate and L-ascorbyl calcium phosphate; and ascorbic acid glycosides such as L-ascorbylglycoside. In the present invention, L-ascorbic acid, a derivative thereof, or a salt thereof is preferably L-ascorbic acid. [0011] The whitening composition (whitening agent) of the present invention includes stains, freckles, sunburn, dark black, steroids, etc. For the prevention and Z or treatment of pigmentation diseases such as skin melanosis caused by drugs

V, to be administered to a person.

[0012] The composition of the present invention may further contain a component that exhibits a known whitening effect and a component that enhances the whitening effect. These components include, for example, pyridoxine, derivatives thereof or salts thereof (pyridoxine; pyridoxine salts such as pyridoxine hydrochloride; pyridoxamine, pyridoxal, etc.), hydroquinone or derivatives thereof (nodroquinone; hydroquinone 1 J3-D-glucose ( Hydone quinone glycosides such as arbutin), dalcosamine or derivatives thereof (darcosamine; darcosamine esters such as acetyl darcosamine; darcosamine ethers such as glucosamine methyl ether), hinokitiol or its Derivatives (hinokitiol; hinokitiol glycosides such as hinokitiol darcoside) , Azelaic acid, derivatives thereof or salts thereof (azelaic acid; azelaic acid monoesters such as azelaic acid monoalkyl ester; azelaic acid diesters such as azelaic acid dialkyl ester), tocopherols ( _α -tocopherol, 13 tocopherol, Ύ Tocopheronole, δ Tocopheronole, etc.), Tocotrienoles (α Tocotrienol, 13-Tocotrienol, γ-Tocotrienol, δ-Tocotrienol, etc.), Ubiquinones (Coenzyme Q (CoQ)) , Cohenzym Q (CoQ), Cohenzyme Q (CoQ

6 6 7 7 8 8

), Coenzyme Q (CoQ), Coenzyme Q (CoQ)), carotene (carotene,

9 9 10 10

Noretin, violaxanthin, spiroloxanthin, spheroidene, etc.), flavones (flavone, apigenin, luteolin and glycosides thereof), isoflavones or derivatives thereof (isoflavones; isoflavone glycosides, etc.), flavanone or derivatives thereof Ringenin, eriodictyol, naringin, etc.), catechins (catechin, force tegugalate, gallocatechin, etc.), flavonols (eg, kaempferol, taercetin, myricetin and their glycosides), glycyrrhizic acid, its derivatives or their salts (Dalicylic retinoic acid; glycyrrhizic acid salts such as dipotassium glycyrrhizinate and monoammonium glycyrrhizinate), glycyrrhetinic acid, its derivatives or their salts (daricyrrhetinic acid; glycyrrhetin Glycyrrhizic acid alkyl esters such as stearyl), kojic acid, derivatives thereof or salts thereof (kojic acid; kojic acid monobutyrate, kojic acid monocaprate, kojic acid monopalmitate, kojic acid monostearate, etc.) Esters: Kojic acid dibutyrate, kojic acid dipalmitate, kojic acid distearate, kojic acid difatty acid esters such as kojic acid dioleate), ellagic acid, its derivatives or salts thereof (ellagic acid; ellagic acid tetramethyl ether, etc.) Ellagic acid ethers; Elacic acid tetraacetate, ellagic acid acyl derivatives such as ellagic acid tetrabenzoate, etc., dartathione, its derivatives or their salts (Dalthathione; S Lactoylglutathione, etc. Sacylglutathiones; N, S Di Kutanoyl glutathione distearyl, N, S dipalmitoyl glutathione dicetyl and other N, S diacyl glutathione diesters, resorcinol or its derivatives (resorcinol; 4 n butyl resorcinol, 4-isoamylresorcinol, 4- Alkylated resorcinols such as cyclohexylresorcinol, 5-methylresorcinol; 4-chlororesorcinol, 4 -Halogenated resorcinol such as bromoresorcinol), glycogen, quincein or its extract, Hammamelis or its extract, yukinoshita or its extract, zinc or its extract, chia or its extract, itadori or its extraction , Melissa or extract thereof, Thyme or extract thereof, Strawberry or extract thereof, Seinokogi or extract thereof, Hypericum or extract thereof, Hypericum or extract thereof, Peonies or extract thereof, Button or its Extract, Spanish licorice or its extract, licorice or its extract, cucumber or its extract, Madawa or its extract, Shimadawa or its extract, Clara or its extract, walrus or its extract Things, Herayano, Zuma Is, its extract, wild, lye or its extract, hijiki or its extract, fushitsugi or its extract, lobster or its extract, duls or its extract, janamoku or its extract, Yezo no Nemoku Is an extract thereof, Fusizimoku or an extract thereof, Ishimozuku or an extract thereof, Mosengoke or an extract thereof, Komoza or an extract thereof, lavender or an extract thereof, oren or an extract thereof, pearl or an extract thereof, Its extract, American sardine or its extract, Japanese pine / Chillon 'flower or its extract, Kudamonotoke or its extract, Water lemon or its extract, Toiiso or its extract, Moon leaf west lotus or its extract , Snake King Wisteria or its extract Gobyo Nishiban lotus or extract thereof, wild pansy or extract thereof, violet violet or extract thereof, violet or extract thereof, cosme or extract thereof, noji violet or extract thereof, -choice violet or extract thereof, Ciss violet or its extract, Shiro violet or its extract, Ezonotachibos violet or its extract, Nepal violet or its extract, White violet or its extract, Marbake violet or its extract, Fuchsia or its extract , Tachibbosu or its extract, ground grass or its extract, Sumiresaicin or its extract, Tabosmille or its extract, Wei Sen or its extract, Tetsusen or its extract, Kazadarma or its extract, Sen- Nso or its extract, Tochu or its extract Things, Togeminomasaki or extracts thereof, Rriba Na or extracts thereof, asparagus or an extract thereof, Ibukitoranoo or extracts thereof, Endu beans or an extract thereof, Eiji' or an extract thereof, Ougon or extract Extract, onionis or extract thereof, raspberry or extract thereof, cucumber or extract thereof, cuckoo or extract thereof, gokahi or extract thereof, saicin or extract thereof, hawthorn or extract thereof, sunpens or extract thereof , Shirayuri or its extract, Sengku power or its extract, Sohakuhi or its extract, Soy or its extract, Tea or its extract, Toki extract, Molasses or its extract, Beechlen or its extract , Beech tree or extract thereof, grape seed or extract thereof, flodema or extract thereof, hop or extract thereof, maikai force or extract thereof, mochi force or extract thereof, rahan fruit or extract thereof, Aloe or its extract, Altea or its extract, Al-force or its extract , Ashtapa or its extract, Inchinko or its extract, nettle or its extract, turmeric or its extract, obata or its extract, force mitlet or its extract, kinggin force or its extract, tareson or its Extract, Comfrey or its extract, Salvia or its extract, Shikon or its extract, Perilla or its extract, Birch or its extract, Tokinsen force or its extract, ヮ Toko or its extract, Who or its extract, Mukuroji or its extract, Lotus root or its extract, Mugwort or its extract, Eucalyptus or its extract, Neubara or its extract, Yew or its extract, Yashaji or its extract , Dicotubi or its extract, Micromerum lum minutum) or an extract thereof, Micromelum pubescens or an extract thereof, Bahakuji or an extract thereof, Bow force or an extract thereof, Sparrow or an extract thereof, Raspberry or an extract thereof, Kiyota or an extract thereof Ability to mention extracts, placenta extracts, etc. It should not be limited to the above. Only one of these components may be blended, or two or more may be blended. The whitening composition (whitening agent) of the present invention may further contain components other than the components showing the known whitening effect and the components that enhance the whitening effect.

The composition of the present invention may be administered orally or parenterally. Examples of preparations for oral administration (oral administration preparations) include dosage forms such as tablets, capsules, powders, fine granules, liquids, troches, and jelly. Formulation for parenteral administration Oral preparations) include extract, plaster, spirit, suppository, suspension, tincture, ointment, poultice, liniment, lotion, aerosol, eye drop, injection, etc. Parenteral preparations include dosage forms such as extracts, plasters, spirits, suspensions, tinctures, ointments, poultices, liniments, lotions, aerosols, etc. Is preferred. The composition of the present invention is preferably an orally administered preparation (orally administered preparation). The whitening composition of the present invention can also be in the form of a cosmetic composition such as lotion, cream, lotion, emulsion, foam, foundation, knocking agent, skin cleanser, shampoo, rinse, conditioner, etc. It is.

[0014] Formulation can be performed by a known formulation technique, and appropriate formulation additives can be added to the formulation. Formulation additives include excipients, binders, disintegrants, lubricants, fluidizing agents, suspending agents, emulsifiers, stabilizers, moisturizing (wetting) agents, preservatives, solvents, solubilizing agents, Preservatives, flavoring agents, sweeteners, pigments, fragrances, propellants and the like can be mentioned, and the formulation additives are appropriately selected within the range without impairing the effects of the present invention, and an appropriate amount is added. .

[0015] In the composition of the present invention, the mixing ratio of (i) tranexamic acid or a salt thereof and (ii) panthetins may be appropriately determined and an appropriate mixing ratio may be determined. i): (ii) = l: 0.01 to 25 force S, preferably 1: 0.03: L 5 force S, more preferably 1: 0.08 to 0.12 force S In addition, (i) tranexamic acid or its salt, (ii) panthetin, (iii) L-cysteine, its derivative or their salt and (iv) L-ascorbic acid, its derivative or their salt Should be studied appropriately and an appropriate mixing ratio should be determined. (I): (ii): (iii): (iv) = l: 0.01-25: 0.01-15: 0.01-60 1: 0.03-: L 5: 0.07-: L 5: 0.1-5 force is more preferable, 1: 0.08-0.12: 0.32: 0.4-1.4 force is particularly preferable.

[0016] The whitening composition (whitening agent) of the present invention is appropriately examined according to the sex, age, symptoms, administration (medication) method, frequency of administration (medication), administration (medication) time, etc. The dosage (dose) can be determined. For example, in the case of internal use, tranexamic acid or a salt thereof is preferably administered (taken) in an amount of 50 to 2500 mg per day, more preferably 400 to 2000 mg (taken). It is preferable to administer (take) 30-1200 mg of pantethine. It is more preferable to administer (take) 60-6 OO mg. L-cystine, its derivatives and These salts are preferably administered (taken) at 30 to 750 mg per day, more preferably 150-48 Omg (taken). L-ascorbic acid, a derivative thereof or a salt thereof is preferably administered in an amount of 50 to 3000 mg (taken) per day, more preferably 300 to 2000 mg (taken).

[0017] That is, in the whitening composition (whitening agent) of the present invention containing tranexamic acid or a salt thereof and panthetins, the compounding amount thereof is 50-2500 mg of tranexamic acid or a salt thereof per day, and 30 pantetins. It is preferred to be formulated so that it will be administered (taken) up to 1200 mg. It is formulated so that 400-2000 mg of tranexamic acid or its salt per day and 60-600 mg of pantethine will be administered (taken). Things Force S More preferable.

[0018] In the whitening composition (whitening agent) of the present invention comprising tranexamic acid or a salt thereof, panthetins, L-cysteine, a derivative thereof or a salt thereof, and L-ascorbic acid, a derivative thereof or a salt thereof, Formulation amount is 50-2500 mg of tranexamic acid or its salt per day, 30-1200 mg of non-tetins, 30-750 mg of L-cysteine, its derivatives or their salts, and L-ascorbic acid, its derivatives or theirs It is preferable to formulate so that 50 to 3000 mg of salt will be administered (taken). 400 to 2000 mg of tranexamic acid or its salt per day, 60 to 600 mg of non-tetins, L-cystine, its derivatives or those 150 to 480 mg of the above-mentioned salt and 300 to 2000 mg of L-ascorbic acid, its derivatives or their salts were formulated (taken) I prefer something even more.

The composition of the present invention may be manufactured as a single preparation containing all the components according to the present invention and administered (taken), or each component according to the present invention may be divided into separate preparations. It is also possible to make a kit preparation that allows these preparations to be administered (taken) simultaneously or sequentially!

Hereinafter, the present invention will be further described with reference to examples. However, the present invention should not be limited to these examples.

Example

[0020] 1. Inhibition of pigmentation

1.1 Test method 1.1.1 Examination of ultraviolet (UVB) irradiation time

Two 6-week-old female Kwl: A-1 brown guinea pigs (SPF) were used to examine the duration of ultraviolet (UVB) irradiation. In other words, one guinea pig was fixed in the abdominal position, and a 2cm X 2cm square ultraviolet irradiation site was set in total, 6 places in total, 3 places each across the back midline. Light was shielded from areas other than the ultraviolet irradiation area, and ultraviolet rays (UVB) irradiation was performed with a distance of 40 cm using five SE lamps (wavelength 250 to 350 nm, FL20S-E, manufactured by Toshiba). The irradiation time was 8, 10, 12, 14, 16, 18 minutes, and the skin reaction (presence / absence and degree of erythema) of the irradiated site was observed the next day.

Next, using another guinea pig, set the irradiation time at an interval of 15 seconds between the minimum time when skin reaction was observed and the maximum time when skin reaction was not observed. After providing eight irradiation sites, the skin reaction was observed, and the ultraviolet (UVB) irradiation time in this test was set to 12 minutes and 30 seconds.

[0021] 1. 1. 2 Test sample

A test specimen was prepared by dissolving in water for injection so that the following dosage was obtained.

Sample (1): Control (no addition)

Specimen (2): Panthetin 1200mgZkgZday

Specimen (3): Tranexamic acid 375mgZkgZday + Panthetine 1200mgZkgZday Specimen (4): Tranexamic acid 1500mgZkgZday + Nontetin 1200mgZkgZday Specimen (5): Tranexamic acid 1500mgZkgZday + Nonthetin 1200mgZkgZday + L —Cystein 240mgZkgZday

[0022] 1. 1. 3 UV irradiation

Six-week-old female Kwl: Five A-1 brown guinea pigs (SPF) were divided into 1 group (4 groups per group in the specimen (1) administration group) and examined. That is, the guinea pig was fixed in the abdominal position using a fixing plate on the day of ultraviolet irradiation (sample administration start date, 2nd and 4th days: total number of times of ultraviolet irradiation 3 times). One square 2cm x 2cm square on either side of the guinea pig back midline was used as the UV irradiation site, and the rest of the UV irradiation site was shielded from light. Using five SE lamps (wavelength 250 to 350 nm, FL20S-E, manufactured by Toshiba), ultraviolet rays (UVB) were irradiated for 12 minutes 30 seconds from a distance of 40 cm. Test specimens were orally administered twice daily during the study period (28 days). Na On the day of UV irradiation, administration was performed after UV irradiation, and on the day of determination of pigmentation, after the determination.

[0023] 1. 1. 4 Determination of pigmentation

Before irradiation on the test sample administration start date and on the test end date, the irradiation site was measured for L value (brightness) using a color difference meter (CR-300, manufactured by Minolta Co., Ltd.). Value—L value before irradiation). The results are shown in Table 1. (The larger the AL value, the higher the effect.)

[0024] [Table 1]

[0025] 1.2 Results

As is clear from Table 1, the specimens (3), (4) and (5) according to the present invention showed an excellent pigmentation inhibitory effect.

[0026] 2. Formulation Example

2.1 tablets

Tablets were produced in the usual manner with the following composition (6 tablets per day).

Tranexamic acid 750mg

L cysteine 240mg

L Asconolevic acid 300mg

Pantethine 90mg

Crystalline cellulose / relose lOOmg

Corn starch 40mg

Low substituted hydroxypropylcellulose 50mg Hydroxypropylcellulose 30mg Magnesium stearate 20mg Hydroxypropylmethylcellulose 2910 60mg Macrogol 6000 12mg Talc 10mg Titanium oxide 18mg [0027] 2.2 Tablets

Tranexamic acid with the following composition (6 tablets as a daily dose)

L—Sistine 240mg

L Asconolevic acid 600mg

90 mg Crystalline senorelose 250 mg Low-substituted hydroxypropyl cellulose 90 mg Hydroxypropenorescenellose 30 mg Magnesium stearate 25 mg Hydroxypropyl methylcellulose 2910 80 mg Macrogol 6000 16 mg Tanolec 14 mg Titanium oxide 24 mg

[0028] 2.3 tablets

_C Tranexamic acid 1500mg Pantethine 600mg Crystalline Senorelose 170mg Corn starch 200mg Low substituted hydroxypropylcellulose 70mg Hydroxypropylcellulose 30mg The following composition (6 tablets as a daily dose) Magnesium stearate 20mg

Hydroxypropyl methylcellulose 2910 60mg

Macrogol 6000 12mg

Tanorek 10mg

Titanium oxide 18mg

Industrial applicability

The composition of the present invention showed an excellent inhibitory effect on melanin pigmentation, as is clear in the examples. Therefore, the composition of the present invention can be used as a whitening composition (whitening agent), as well as for prevention of pigmentation such as skin darkening caused by drugs such as stains, freckles, sunburn, dark skin and steroids. It is useful as a therapeutic composition.

Claims

The scope of the claims

[I] A composition comprising (i) tranexamic acid or a salt thereof, and (ii) panthetins.

[2] Daily dose (dose) of (i) tranexamic acid or its salt

And (ii) a composition containing 30 to 1200 mg of panthetins.

[3] A composition comprising tranexamic acid and pantethine.

[4] A composition containing 50 to 2500 mg of tranexamic acid and 30 to 1200 mg of panthetine as daily administration (dose) amounts.

[5] Contains (i) tranexamic acid or a salt thereof, (ii) panthetins, (iii) L-cysteine, a derivative thereof or a salt thereof, and (iv) L-ascorbic acid, a derivative thereof or a salt thereof Composition.

[6] The daily dose (dose) is: (i) tranexamic acid or its salt 50-2500 mg, (ii) pantethine 30-1200 mg, (iii) L-cystine, its derivatives or their salts A composition containing 30 to 750 mg, and (iv) 50 to 3000 mg of L-ascorbic acid, a derivative thereof or a salt thereof.

[7] A composition containing tranexamic acid, pantethine, L-cystine and L-ascorbic acid.

[8] Composition containing 50 to 2500 mg of tranexamic acid, 30 to 1200 mg of nonethin, 30 to 750 mg of L-cystine, and 50 to 300 Omg of L-ascorbic acid as daily doses .

[9] The composition according to any one of claims 1 to 8, which is used for whitening.

[10] The composition according to any one of claims 1 to 8, which is used for prevention and Z or treatment of pigmentation.

[II] The composition according to any one of claims 1 to 10, wherein the dosage form is a preparation for oral administration.

[12] Use of the composition according to any one of claims 1 to 8 for producing a whitening agent.

[13] Use of the composition according to any one of claims 1 to 8 for prevention of pigmentation and production of a Z or therapeutic agent.

[14] A whitening method comprising administering (i) tranexamic acid or a salt thereof, and (ii) an effective amount of panthetins.

[15] As a daily dose (dose), (i) tranexamic acid or its salt is 50-2500mg

And (ii) the pantethine is 30 to 1200 mg.

[16] A whitening method comprising administering an effective amount of tranexamic acid and pantethine.

[17] The method according to claim 16, wherein the daily dose (dose) is 50 to 2500 mg of tranexamic acid and 30 to 1200 mg of panthetin.

[18] An effective amount of (i) tranexamic acid or a salt thereof, (ii) panthetins, (iii) L cysteine, a derivative thereof or a salt thereof, and (iv) L ascorbic acid, a derivative thereof or a salt thereof. A whitening method characterized by administering.

[19] Daily dose (dose) of (i) tranexamic acid or its salt is 50-2500mg

, (Ii) 30-1200 mg of pantethine, (iii) L-cystine, its derivatives or their salt strength S30-750 mg, and (iv) L-ascorbic acid, its derivatives or their salt strength 0-3000 mg The method of claim 18.

[20] A whitening method characterized by administering an effective amount of tranexamic acid, pantethine, L-cystine and L-ascorbic acid.

[21] The daily dose (dose) is 50-2500 mg tranexamic acid and 3 pantethine.

0 ~ 1200mg, Cysteine power S30 ~ 750mg, J-Birth = f Norebic acid power 50 ~ 30

21. The method of claim 20, wherein said method is OOmg.

[22] A method for preventing and / or treating pigmentation, comprising administering (i) tranexamic acid or a salt thereof, and (ii) an effective amount of panthetins.

[23] As a daily dose (dose), (i) tranexamic acid or its salt is 50-2500mg

The method according to claim 22, wherein (ii) the pantethine is 30 to 1200 mg.

[24] Prevention and Z or treatment of pigmentation characterized by administering an effective amount of tranexamic acid and pantethine.

25. The method according to claim 24, wherein the daily administration (dose) is 50 to 2500 mg of tranexamic acid and 30 to 1200 mg of panthetin.

[26] An effective amount of (i) tranexamic acid or a salt thereof, (ii) panthetins, (iii) L-cysteine, a derivative or a salt thereof, and (iv) L ascorbic acid, a derivative or a salt thereof. A prevention and Z or treatment of pigmentation characterized by administration.

[27] The daily dose (dose) is as follows: (i) tranexamic acid or its salt 50 to 2500 mg, (ii) pantethine 30 to 1200 mg, (iii) L-cystine, its derivatives or their salt strength The method according to claim 26, wherein S is 30 to 750 mg, and (iv) L-ascorbic acid, a derivative thereof, or a salt strength thereof is 0 to 3000 mg.

[28] Prevention and Z or treatment of pigmentation characterized by administering an effective amount of tranexamic acid, pantethine, L-cysteine and L-ascorbic acid.

[29] The daily dose (dose) is tranexamic acid 50 to 2500 mg, panthetin 30 to 1200 mg, cystine power S30 to 750 mg, and J-bias = norebic acid power 50 to 30 OOmg. 28. The method according to 28.