EP1210077A1 - Compositions and systems for the treatment of hyperpigmentation - Google Patents
Compositions and systems for the treatment of hyperpigmentationInfo
- Publication number
- EP1210077A1 EP1210077A1 EP99928685A EP99928685A EP1210077A1 EP 1210077 A1 EP1210077 A1 EP 1210077A1 EP 99928685 A EP99928685 A EP 99928685A EP 99928685 A EP99928685 A EP 99928685A EP 1210077 A1 EP1210077 A1 EP 1210077A1
- Authority
- EP
- European Patent Office
- Prior art keywords
- composition
- ascorbityl
- tocopherol
- derivative
- ascorbic acid
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Withdrawn
Links
Definitions
- This invention relates to pigmentation disorders, specifically hyperpigmentation.
- Melanin a pigment found in human skin, is produced by cells known as melanocytes. Melanocytes produce melanin in granules called melanosomes. Melanosomes are transferred from the melanocytes to keratinocytes, a layer of keratin-producing cells that is closer to the outer surface of the skin. The more melanosomes that are transferred to the keratinocytes, the darker the skin appears. This process can be altered in persons of any skin type or race. Alteration that results in excessive darkening is known as hyperpigmentation.
- Hyperpigmentation can take a variety of forms. Melasma is a form of hyperpigmentation in pregnant women that is characterized by dark patches on the cheeks and forehead, and is sometimes called “pregnancy mask”. With age, many persons develop dark spots sometimes known as “liver spots.” Hyperpigmentation is sometimes a side effect of birth control pills, and can be a persistent result of acne, burns, bites and other skin injuries.
- hydroquinone 1 ,4-benzenediol
- Hydroquinone acts by suppressing melanocyte activity.
- Hydroquinone by itself or in combination with glycolic acid, is sold without prescription at strengths of up to 2% and at strengths of up to 4% by prescription.
- Hydroquinone preparations are effective, but not without drawbacks. They can cause burning, redness, sensitization and irritation in some persons. Close supervision of the patient by a physician is recommended when prescription strength preparations are used. It is desirable to provide a treatment for hyperpigmentation that is at least as effective as hydroquinone, but lacks hydroquinone' s side effects.
- Tocopherol also known as Vitamin E, is well known and commercially available. Dermally available derivatives of tocopherol may also be used in this invention. A dermally available derivative of tocopherol is a compound that makes tocopherol or a biological active form of tocopherol available to the skin. In preparing compositions in accordance with the invention, tocopherol acetate was used as the source of tocopherol, although free tocopherol, tocopherol linoleate or other sources can be used.
- ascorbic acid can be used in this invention, among them ascorbityl palmitate, magnesium ascorbityl phosphate, and ascorbityl linoleate.
- lipid esters especially ascorbityl palmitate, are preferred.
- Either C 18 unsaturated fatty acids such as oleic, linoleic and linolenic acids, or other essential fatty acids, including arachadonic acid, may be used in connection with this invention.
- linoleic acid is preferred. In the embodiments described below, linoleic acid was used.
- the liquid is prepared as follows. Part A is prepared by warming to 40°C and
- B is prepared by separately mixing components (2), (3), (4) and (6)which are warmed to
- the gel is prepared as follows. Part A is prepared by warming to 45°C and
- Part B is prepared by heating to 70°C and mixing until
- Part A is added to Part B, with careful
- the cream is prepared as follows. Part A is prepared by separately heating to
- Component (2) is added to Part A just before adding Part B.
- Part B is prepared by heating
- component (20) to 70°C, and adding and dissolving component (21). Then components (20)
- Part C is prepared by stirring and then, with either an internal or external homogenizer operating, adding Part B to Part A until uniform. The speed
- 0.50g of the above described cream should be applied to each 100 cm 2 of affected skin.
- the effectiveness of the present invention in the treatment and prevention of hyperpigmentation was demonstrated by use of the Melanoderm assay.
- the Melanoderm assay is a recognized in vitro assay, performed on skin grown from human epidermal cells in vitro (a "human skin equivalent"). It stimulates melanogenesis by the addition of dopamine, the natural precursor of melanin within skin, producing visual color in the human skin equivalent.
- the purpose of the Melanoderm assay is two-fold. First, it determines the ability of test materials to inhibit melanogenesis, the formation of melanin. Second, it determines the ability of test materials to reduce pigmentation ("lighten/whiten skin”) after melanogenesis has occurred.
- a Melanoderm assay the substance to be tested is combined with the dopamine and resultant changes in the formation of melanin are compared with a positive dopamine control without the test material. Any visible reduction in melanin formation is due to the ability of the test material to inhibit melanogenesis.
- the test material is added to the skin equivalent after it has been treated with dopamine to induce pigmentation An active, effective test agent produces a visual reduction in pigmentation.
- compositions of the invention blocked visual formation of color after it had been mixed with dopamine, thus indicating that they prevent melanin formation.
- compositions of the invention “whitened” the pigmented human skin equivalent when it was added after pigmentation had been preformed, thus indicating that it reduces pre-existing pigmentation.
- Placebo 4 Bla 0 -16% - 7% - 3%
Landscapes
- Cosmetics (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
Claims
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
PCT/US1999/013525 WO2000076494A1 (en) | 1997-08-05 | 1999-06-15 | Compositions and systems for the treatment of hyperpigmentation |
Publications (2)
Publication Number | Publication Date |
---|---|
EP1210077A1 true EP1210077A1 (en) | 2002-06-05 |
EP1210077A4 EP1210077A4 (en) | 2002-12-18 |
Family
ID=22272978
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP99928685A Withdrawn EP1210077A4 (en) | 1999-06-15 | 1999-06-15 | Compositions and systems for the treatment of hyperpigmentation |
Country Status (3)
Country | Link |
---|---|
EP (1) | EP1210077A4 (en) |
JP (1) | JP2003516311A (en) |
CA (1) | CA2377334A1 (en) |
Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH01186811A (en) * | 1988-01-20 | 1989-07-26 | Sunstar Inc | Skin beautifying cosmetic |
US5078989A (en) * | 1990-03-28 | 1992-01-07 | Sunstar K.K. | Skin whitening cosmetics |
GB2259014A (en) * | 1991-08-23 | 1993-03-03 | Fischer Pharma Ltd | Compositions containing flavonoids |
GB2265086A (en) * | 1992-03-06 | 1993-09-22 | Pacific Chem Co Ltd | Skin whitening agents formulated as patches |
US5807561A (en) * | 1996-05-23 | 1998-09-15 | Elizabeth Arden Co., Division Of Conopco, Inc. | Emulsifying system for a whitening cosmetic composition |
-
1999
- 1999-06-15 JP JP2001502827A patent/JP2003516311A/en active Pending
- 1999-06-15 EP EP99928685A patent/EP1210077A4/en not_active Withdrawn
- 1999-06-15 CA CA002377334A patent/CA2377334A1/en not_active Abandoned
Patent Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH01186811A (en) * | 1988-01-20 | 1989-07-26 | Sunstar Inc | Skin beautifying cosmetic |
US5078989A (en) * | 1990-03-28 | 1992-01-07 | Sunstar K.K. | Skin whitening cosmetics |
GB2259014A (en) * | 1991-08-23 | 1993-03-03 | Fischer Pharma Ltd | Compositions containing flavonoids |
GB2265086A (en) * | 1992-03-06 | 1993-09-22 | Pacific Chem Co Ltd | Skin whitening agents formulated as patches |
US5807561A (en) * | 1996-05-23 | 1998-09-15 | Elizabeth Arden Co., Division Of Conopco, Inc. | Emulsifying system for a whitening cosmetic composition |
Non-Patent Citations (2)
Title |
---|
PATENT ABSTRACTS OF JAPAN vol. 13, no. 472 (C-647), 25 October 1989 (1989-10-25) & JP 01 186811 A (SUNSTAR INC.), 26 July 1989 (1989-07-26) * |
See also references of WO0076494A1 * |
Also Published As
Publication number | Publication date |
---|---|
JP2003516311A (en) | 2003-05-13 |
EP1210077A4 (en) | 2002-12-18 |
CA2377334A1 (en) | 2000-12-21 |
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Legal Events
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PUAI | Public reference made under article 153(3) epc to a published international application that has entered the european phase |
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17Q | First examination report despatched |
Effective date: 20080917 |
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STAA | Information on the status of an ep patent application or granted ep patent |
Free format text: STATUS: THE APPLICATION IS DEEMED TO BE WITHDRAWN |
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18D | Application deemed to be withdrawn |
Effective date: 20090328 |