# US 10,500,146 B2 · Composition for skin whitening comprising amorphigeni as effective ingredient

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- Number: US 10,500,146 B2
- Document ID: US10500146B2
- Status: Granted
- Kind: B2
- Application number: 15/768,609
- Filed: 2016-10-13
- Published: 2018-10-25
- Granted: 2019-12-10
- Earliest claimed: 2015-10-16
- Assignees: Industry-Academic Cooperation Foundation Gyeongsang National University
- Applicants: Industry-Academic Cooperation Foundation Gyeongsang National University
- Inventors: Kwang Dong Kim; Ji Yun Yoo; Soojong Park; Sangseok Oh; Dae Wook Kim; Ki Hun Park; Kiwon Lee
- Web page: https://patentgrep.com/patent/US10500146B2

## CPC

- A61K 8/498: {having 6-membered rings or their condensed derivatives, e.g. coumarin}
- A23L 33/10: using additives (addition of substantially indigestible substances A23L33/21)
- A61K 8/9783: Angiosperms [Magnoliophyta]
- A61K 8/9789: Magnoliopsida [dicotyledons]
- A61K 9/0014: {Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00)}
- A61K 31/352: condensed with carbocyclic rings, e.g. methantheline {(cannabinoids A61K31/658)}
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/02: for treating wounds, ulcers, burns, scars, keloids, or the like
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61Q 19/02: for chemically bleaching or whitening the skin
- A23V 2002/00: Food compositions, function of food ingredients or processes for food or foodstuffs
- A23V 2200/318: having an effect on skin health and hair or coat
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A23L: FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF (preservation thereof A23B)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61Q: SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A23V: INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION

## Abstract

A skin whitening composition includes amorphigeni or a salt thereof as an effective ingredient. Amorphigeni suppresses the expression of tyrosinase and induces autophagy on melanosomes. As such, it was confirmed that amorphigeni not only suppresses melanin production but also exhibits the effect of removing melanin previously produced by α-MSH (melanocyte-stimulating hormone). Accordingly, amorphigeni can be advantageously used as a functional material for skin whitening and skin lightening.

## Claims

### Claim 1

A method of whitening the skin of a subject, the method comprising:
preparing a composition comprising amorphigeni represented by Chemical Formula 1 or a salt thereof as an effective ingredient:
and
applying the composition to the skin of the subject,
wherein the amorphigeni is prepared by a process comprising:
obtaining an extract from roots of Amorpha fruticosa;
concentrating the extract;
eluting the extract to obtain fractions; and
obtaining a fraction containing the amorphigeni in the largest amount.

### Claim 2 (depends on 1)

The method of claim 1, wherein the composition is a cosmetic composition which is a formulation selected from the group consisting of a solution, a suspension, an emulsion, a paste, a gel, a créme, a lotion, a powder, a soap, a surfactant-containing cleanser, an oil, a powder foundation, a foundation, a wax foundation and a spray.

### Claim 3 (depends on 1)

The method of claim 1, wherein the composition comprises the salt, and the salt is an acid addition salt formed with a free acid.

### Claim 4 (depends on 2)

The method of claim 2, wherein the formulation is the paste, the creme, or the gel; and the formulation composition comprises an animal fiber, a plant fiber, wax, paraffin, starch, tragacanth, a cellulose derivative, polyethylene glycol, silicone, bentonite, silica, talc, zinc oxide, or a combination thereof as a carrier component.

### Claim 5 (depends on 2)

The method of claim 2, wherein the formulation is the powder or the spray; and the formulation comprises lactose, talc, silica, aluminum hydroxide, calcium silicate, polyamide powder or a combination thereof as a carrier component.

### Claim 6 (depends on 2)

The method of claim 2, wherein the formulation is the spray; and the formulation further comprises chlorofluorohydrocarbon, propane-butane, or dimethyl ether.

### Claim 7 (depends on 2)

The method of claim 2, wherein the formulation is the solution or the emulsion; and the formulation comprises a solvent, a solubilizing agent, or an emulsifying agent as a carrier component.

### Claim 8 (depends on 2)

The method of claim 2, wherein the formulation is the suspension; and the formulation comprises a liquid phase diluent, a suspending agent, microcrystalline cellulose, aluminum metahydroxide, bentonite, agar, or tragacanth as a carrier component.

### Claim 9 (depends on 2)

The method of claim 2, wherein the formulation is the surfactant-containing cleanser; and the formulation comprises aliphatic alcohol sulfate, aliphatic alcohol ether sulfate, sulfonsuccinic acid monoester, acethionate, an imidazoilum derivative, methyl taurate, sarcosinate, fatty acid amide ether sulfate, alkylamidobetain, aliphatic alcohol, fatty acid glyceride, fatty acid diethanolamide, plant oil, a linolin derivative, or ethoxylated glycerol fatty acid ester.

### Claim 10 (depends on 2)

The method of claim 2, wherein the formulation further comprises an additional skin whitening active component selected from the group consisting of kojic acid, albutin, ascorbic acid, hydroquinone, resorcinol, cycloalkanone, methylene dioxyphenylalkanol, 2,7-dinitroindazole, a bearberry extract, a rice extract, a liquorice extract, and a derivative thereof.

### Claim 11 (depends on 1)

The method of claim 1, wherein the composition further comprises a vehicle including a fluorescent material, a bactericidal agent, a hydrotrope, a moisturizing agent, an aroma, an aromatic carrier, a protein, a solubilizing agent, a sugar derivative, a sunshine blocking agent, a vitamin, a plant extract, or a combination thereof.

### Claim 12 (depends on 1)

The method of claim 1, wherein the composition is a pharmaceutical composition that is a formulation selected from the group consisting of an injection solution, a créme, a patch, a spray, an ointment, a hard solid, a lotion, a liniment, a paste, and a cataplasma.

### Claim 13 (depends on 12)

The method of claim 12, wherein the pharmaceutical composition further comprises a pharmaceutically acceptable carrier selected from the group consisting of lactose, dextrose, sucrose, sorbitol, mannitol, starch, acacia gum, calcium phosphate, alginate, gelatin, calcium silicate, microcrystalline cellulose, polyvinyl pyrrolidone, cellulose, water, syrup, methyl cellulose, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate, mineral oil, and a combination thereof.

### Claim 14 (depends on 12)

The method of claim 12, wherein the pharmaceutical composition further comprises a lubricating agent, a humidifying agent, a sweetening agent, a flavoring agent, an emulsifying agent, a suspending agent, a preservative, or a combination thereof.

### Claim 15 (depends on 1)

The method of claim 1, wherein the subject has a melanin hyperpigmentation disorder.

### Claim 16 (depends on 15)

The method of claim 15, wherein the melanin hyperpigmentation disorder is freckles, senile spots, chloasma, small brown spots, brown or black moles, sunshine pigment spots, cyanic melisma, hyperpigmentation after drug use, gravidic chloasma, or hyperpigmentation after inflammation caused by lesions or skin inflammation.

### Claim 17 (depends on 15)

The method of claim 15, wherein the composition is prepared as any one formulation selected from an injection solution, créme, a patch, a spray, an ointment, a hard solid, a lotion, a liniment, a paste, and a cataplasma.

### Claim 18 (depends on 15)

The method of claim 15, wherein the composition is a pharmaceutical composition comprising a pharmaceutical carrier.

### Claim 19

A method of whitening the skin of a subject, the method comprising:
preparing an isolated amorphigeni represented by Chemical Formula 1 or a salt thereof:
preparing a composition comprising the isolated amorphigeni; and
applying the composition to the skin of the subject.

### Claim 20 (depends on 19)

The method of claim 19, wherein the isolated amorphigenin has a purity of at least 70%.