KR102027348B1 - Composition for skin whitening comprising Acarbose - Google Patents
Composition for skin whitening comprising Acarbose Download PDFInfo
- Publication number
- KR102027348B1 KR102027348B1 KR1020130067976A KR20130067976A KR102027348B1 KR 102027348 B1 KR102027348 B1 KR 102027348B1 KR 1020130067976 A KR1020130067976 A KR 1020130067976A KR 20130067976 A KR20130067976 A KR 20130067976A KR 102027348 B1 KR102027348 B1 KR 102027348B1
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- KR
- South Korea
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- acarbose
- composition
- present
- active ingredient
- skin whitening
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
- A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/60—Sugars; Derivatives thereof
- A61K8/602—Glycosides, e.g. rutin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
- A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
Abstract
The present invention relates to a composition containing acarbose (Acarbose) as an active ingredient, and more particularly to a composition for skin whitening by showing the skin whitening effect by inhibiting the melanin production of the skin containing acarbose as an active ingredient It is about.
Description
The present invention relates to a composition containing acarbose (Acarbose) as an active ingredient, and more particularly to a composition for skin whitening by showing the skin whitening effect by inhibiting the melanin production of the skin containing acarbose as an active ingredient It is about.
Melanin, which determines human skin color, is made from skin cells called melanocytes and migrates to epidermal cells called keratinocytes. Here, melanin plays an important role such as forming a hat-like structure around the nucleus to protect genes from ultraviolet rays and to remove free radicals to protect intracellular proteins. These melanin-degrading enzymes are not present in vivo but are removed by falling off the skin as keratinocytes fall off the epidermis. However, if the melanin is produced more than necessary, such as blemishes, freckles, spots, such as hyperpigmentation will cause a cosmetically bad result. In addition, as the leisure population increases, more people enjoy working outside, and the demand to prevent melanin pigmentation due to ultraviolet rays is increasing. Therefore, it was necessary to develop a whitening agent that prevents excessive melanin production and many efforts have been made.
Until now, the development of whitening agents has been mainly focused on finding a substance that reduces melanin by inhibiting the enzyme activity of tyrosinase, a basic and most important enzyme in melanin biosynthesis. The whitening agent thus developed includes kojic acid, arbutin, glutathione, vitamin A, vitamin C, etc., but it does not have a satisfactory whitening effect for consumers and has a limited problem in its amount due to side effects. Therefore, it is urgent to develop a whitening agent that is more effective and safer than ever before.
Acarbose is used as an antihyperglycemic agent to inhibit glucose absorption in the intestine by inhibiting digestive enzymes (maltase), but the effect of inhibiting melanin production is not known.
Accordingly, the present inventors have completed the present invention by finding that acarbose can effectively inhibit melanin production, as a result of researching to provide a new whitening agent exhibiting excellent whitening effect.
Therefore, an object of the present invention is to provide a composition for skin whitening, which contains acarbose as an active ingredient and suppresses melanin production of the skin, thereby exhibiting a skin whitening effect.
In order to achieve the above object, the present invention provides a composition for skin whitening containing acarbose as an active ingredient.
The composition for skin whitening according to the present invention contains acarbose as an active ingredient, thereby effectively inhibiting skin melanin production without side effects, thereby providing an excellent skin whitening effect.
Figure 1 shows the results of confirming the melanin production inhibitory effect by the color of the cells in human melanoma cells.
Fig. 2 shows the results obtained by measuring absorbance after melanin content in human melanoma cells.
The present invention relates to a composition for skin whitening containing acarbose as an active ingredient.
Hereinafter, the present invention will be described in more detail.
Acarbose used in the present invention is a type of soil microorganism ( Actinoplanes) sp . It is obtained from the secondary metabolite of), is a structural unit of cellulose, and has a structure of the following general formula (1).
The composition according to the present invention may contain the acarbose in an amount of 0.001 to 20% by weight based on the total weight of the composition. If the content is less than 0.001% by weight, the efficacy and effect by the acarbose component is weak, and if it exceeds 20% by weight, there is a problem of skin stability or formulation.
The composition according to the present invention can be used as a composition for skin whitening, which can provide an excellent whitening effect by inhibiting tyrosinase activity and inhibiting melanin production.
The composition according to the invention can be formulated into a topical skin composition, in particular a cosmetic composition, and can be formulated containing a cosmetically or dermatologically acceptable medium or base. In addition, the compositions of the present invention may be provided in all formulations suitable for topical application, for example, emulsions obtained by dispersing an oil phase in a solution, an aqueous phase, emulsions obtained by dispersing an aqueous phase in an oil phase, suspensions, solids, gels, powders, It may be provided in the form of a paste, foam or aerosol composition. Compositions of such formulations may be prepared according to conventional methods in the art.
In addition, the composition according to the present invention may include other ingredients in addition to the above-mentioned materials within a range not impairing the main effect, preferably a synergistic effect on the main effect. In addition, the composition according to the present invention may further include a moisturizer, an emulsifier, a UV absorber, a preservative, a fungicide, an antioxidant, a pH adjuster, organic and inorganic pigments, flavoring, cooling agent or limiting agent. The blending amount of the above components can be easily selected by those skilled in the art within the range that does not impair the object and effect of the present invention, the blending amount may be 0.01 to 5% by weight, preferably 0.01 to 3% by weight relative to the total weight of the composition. have.
In addition, the compositions of the present invention may be formulated into pharmaceutical compositions. When the composition according to the present invention is applied to a pharmaceutical product, it may be formulated as an oral or parenteral dosage form in the form of a solid, semi-solid or liquid by adding a commercially available inorganic or organic carrier to the active ingredient used in the present invention. , The pharmaceutical composition according to the invention can be administered orally, parenteral, rectal, topical, transdermal, intravenous, intramuscular, intraperitoneal, subcutaneous.
Formulations for oral administration include tablets, pills, granules, capsules, powders, fine granules, powders, emulsions, syrups, pellets and the like. In addition, the formulation for parenteral administration includes injections, drops, ointments, lotions, sprays, suspensions, emulsions, suppositories, and the like. The composition according to the present invention can be easily formulated by carrying out according to a conventional method, and at this time, surfactants, excipients, coloring agents, spices, preservatives, stabilizers, buffers, suspending agents, and other commercially available auxiliaries can be suitably used. have.
The dosage of the active ingredient of the pharmaceutical composition of the present invention will vary depending on the age, sex, weight, pathology and severity of the subject to be administered, the route of administration or the judgment of the prescriber. Determination of a suitable dose based on these factors is within the level of one of skill in the art and its daily dosage may be, for example, 0.1 mg / kg / day to 100 mg / kg / day, more specifically 5 mg / kg / day to 50 mg / kg. May be, but is not limited to.
Hereinafter, the present invention will be described in more detail with reference to Examples. These examples are only for illustrating the present invention, it will be apparent to those of ordinary skill in the art that the scope of the present invention is not to be construed as being limited by these examples.
[Test Example 1] inhibitory effect of melanin production using MNT1 human melanoma cells
MNT1 cells, a human melanoma cell line, were placed in minimal essential medium (MEM) containing 20% fetal bovine serum and grown under 37 ° C and 5% CO 2 , and then the number of cells was 1 × 10 5 . The plate was placed in a 60 mm dish, and the cells were allowed to adhere to the wall overnight, and then, the acarbose was changed to the same medium added with 1 mM and 2 mM, respectively. The fresh medium containing the sample was changed every 2 days and incubated for 4 days until the cells were filled in a dish. When the cells were grown, lysis buffer (1% NP-40, 50 mM Tris-HCl; pH7.5, 150 mM NaCl) was treated with 300 μl, collected in a microtube using a cell scraper, and centrifuged at 15,000 rpm for 10 minutes. No treatment was used as a control, photographs were taken for color comparison, and the results are shown in FIG. 1. In addition, in order to objectively confirm the content of melanin present in the cells, the absorbance was measured at 450 nm for the separated precipitate. The results are shown in FIG.
Referring to Figure 1, when the acarbose treated color was lighter than the control group did not process anything, in particular, when treated with acarbose 2mM color is significantly more than when treated with acarbose 1mM You can see that it is lightened. In addition, referring to Figure 2, when the acarbose treated, the absorbance value was reduced compared to the control group not treated at all, especially when the acarbose treated with 2mM compared to the case where the acarbose treated with 1mM It is objectively confirmed that the difference in values is large and the melanin content in the cells is considerably reduced. Therefore, it can be seen that a composition containing acarbose as an active ingredient can provide a very good whitening effect.
Preparation Example 1 Soft Capsule
Acarbose 1mg, palm oil 2mg, palm hardened oil 8mg, lead 4mg and lecithin 6mg were mixed and 400mg per capsule was filled according to a conventional method to prepare a soft capsule.
Preparation Example 2 Tablet
1 mg of acarbose, 100 mg of glucose, 50 mg of red ginseng extract, 96 mg of starch, and 4 mg of magnesium stearate were mixed and 40 mg of 30% ethanol was added to form granules, dried at 60 ° C., and compressed into tablets using a tablet press.
Preparation Example 3 Granule
1 mg of acarbose, 100 mg of glucose, 50 mg of red ginseng extract, and 600 mg of starch were mixed, and 100 mg of 30% ethanol was added to form granules, and dried at 60 ° C. to form granules and then filled into fabrics. The final weight of the content was 1 g.
[Example 4] Softening Cosmetic (Skin Lotion)
According to the composition shown in Table 1 below to prepare a flexible cosmetic water in a conventional manner.
[Example 5] Nutritional Longevity (Milk Lotion)
Nutritional longevity was prepared according to the composition described in Table 2 below in a conventional manner.
Preparation Example 6 Nutrition Cream
Nutritional cream was prepared in a conventional manner according to the composition shown in Table 3.
[Example 7] Massage Cream
To prepare a massage cream in a conventional manner according to the composition described in Table 4.
[Example 8] Pack
To prepare a pack in a conventional manner according to the composition described in Table 5.
[Example 9] Ointment
The ointment was prepared in a conventional manner according to the composition described in Table 6.
As described above in detail the specific parts of the present invention, it is apparent to those skilled in the art that such specific description is merely a preferred embodiment, thereby not limiting the scope of the present invention. something to do.
Thus, the substantial scope of the present invention will be defined by the appended claims and their equivalents.
Claims (4)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR1020130067976A KR102027348B1 (en) | 2013-06-13 | 2013-06-13 | Composition for skin whitening comprising Acarbose |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR1020130067976A KR102027348B1 (en) | 2013-06-13 | 2013-06-13 | Composition for skin whitening comprising Acarbose |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR20140145479A KR20140145479A (en) | 2014-12-23 |
| KR102027348B1 true KR102027348B1 (en) | 2019-10-01 |
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| Application Number | Title | Priority Date | Filing Date |
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| KR1020130067976A KR102027348B1 (en) | 2013-06-13 | 2013-06-13 | Composition for skin whitening comprising Acarbose |
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Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20210115745A (en) | 2020-03-16 | 2021-09-27 | (주)아모레퍼시픽 | Composition for skin whitening comprising isolindleyin |
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- 2013-06-13 KR KR1020130067976A patent/KR102027348B1/en active IP Right Grant
Non-Patent Citations (2)
| Title |
|---|
| Experimental deramtology, 22(8), pp.541-546(20130831) |
| Journal of biological chemistry, 278(21), pp.19378-19386(20030523) |
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| KR20140145479A (en) | 2014-12-23 |
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