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"Skin Whitening Cosmetic Composition Containing Extracts Of Indian Natural Materials"

Abstract: The present invention relates to a skin-whitening cosmetic composition, and more particularly, to a skin-whitening cosmetic composition containing a Commiphora   mukul   resin extract and a Terminalia   chebula   extract.  The present invention also relates to a cosmetic composition containing a Commiphora mukul  resin extract, a Terminalia  chebula extract, a Withania  somnifera  {Ashwagandha)  root extract, an Andrographis paniculata  extract and a Phyllanthus  emblica  extract, which provide a skin-whitening effect by inhibiting melanin production.

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Notices, Deadlines & Correspondence

Patent Information

Application #
Filing Date
20 November 2012
Publication Number
27/2014
Publication Type
INA
Invention Field
PHARMACEUTICALS
Status
Email
Parent Application

Applicants

AMOREPACIFIC CORPORATION
181, 2-GA HANGANG-RO, YONGSAN-GU, SEOUL, REPUBLIC OR KOREA

Inventors

1. KIM, HAN BYUL
314-1, BORA-DONG, GIHEUNG-GU, YONGIN-SI, GYEONGGI-DO, REPUBLIC OF KOREA
2. CHOI, HYANG TAE
314-1, BORA-DONG, GIHEUNG-GU, YONGIN-SI, GYEONGGI-DO, REPUBLIC OF KOREA
3. LIM, HYUNG JUN
314-1, BORA-DONG, GIHEUNG-GU, YONGIN-SI, GYEONGGI-DO, REPUBLIC OF KOREA
4. KIM, JI SEONG
314-1, BORA-DONG, GIHEUNG-GU, YONGIN-SI, GYEONGGI-DO, REPUBLIC OF KOREA
5. LEE, JIN YOUNG
314-1, BORA-DONG, GIHEUNG-GU, YONGIN-SI, GYEONGGI-DO, REPUBLIC OF KOREA
6. BAE, JI HYUN
314-1, BORA-DONG, GIHEUNG-GU, YONGIN-SI, GYEONGGI-DO, REPUBLIC OF KOREA

Specification

FORM 2
THE PATENTS ACT, 1970 (39 of 1970)
&
THE PATENTS RULES, 2003
COMPLETE SPECIFICATION
[See section 10, Rule 13]
SKIN-WHITENING COSMETIC
COMPOSITION CONTAINING EXTRACTS OF INDIAN NATURAL MATERIALS;
AMOREPACIFIC CORPORATION, A CORPORATION ORGANIZED AND EXISTING UNDER THE LAWS OF REPUBLIC OF KOREA WHOSE ADDRESS IS 181, 2-GA HANGANG-RO, YONGSAN-GU, SEOUL, REPUBLIC OF KOREA
THE FOLLOWING SPECIFICATION PARTICULARLY DESCRIBES THE INVENTION AND THE MANNER IN WHICH IT IS TO BE PERFORMED.

BACKGROUND OF THE INVENTION
Field of the Invention
The present invention relates to a skin-whitening cosmetic composition, and more particularly, to a skin-whitening cosmetic composition containing a Commiphora mukul resin extract and a Terminalia chebula extract. Moreover, the present invention relates to a cosmetic composition containing a Commiphora mukul resin extract, a Terminalia chebula extract, a Withania somnifera {Ashwagandha) root extract, an Andrographis paniculata extract and a Phyllanthus emblica extract, which provide a skin-whitening effect by inhibiting melanin production.
Description of the Prior Art
Various factors are involved in determining human skin color, and among them, factors, such as the activity of melanocytes, which make melanin pigments, the distribution of blood vessels, the thickness of the skin, and the presence or absence of pigments (e.g., carotenoid, bilirubin, etc.) in the human body, are of importance.
Among them, the most important factor is the black pigment

melanin which is produced by the action of various enzymes (e.g., tyrosinase) in melanocytes in the human body. The production of the melanin pigment is influenced by genetic factors, physiological factors associated with hormone secretion and stress, and environmental factors such as UV radiation.
The melanin pigment, which is produced in melanocytes in the skin of the body, is a phenolic polymer in the form of a black pigment/protein composite and has useful functions to protect skin organs under the dermis by blocking UV light radiation from the sun and simultaneously to capture free radicals from the skin, thus protecting proteins and genes in the skin.
Melanin produced in the skin due to intrinsic and extrinsic stresses as described above is a stable material, which does not appear even when the stresses disappear, until it is discharged to the outside through skin keratinization. However, if melanin is produced in unnecessarily large amounts, hyperpigmentations such as discoloration, freckles and spots are induced, resulting in unfavorable results in beautiful terms.
These days, women in oriental countries prefer a white and clean skin like a white gem and consider this skin as an important beauty standard. For this reason, the demand to solve therapeutic and cosmetic problems for hyperpigmentations

has increased.
To satisfy this demand, ascorbic acid, kojic acid, arbutin, hydroquinone, glutathione, their derivatives, or materials having tyrosinase inhibitory activity, have been used in cosmetics or drugs. However, the use thereof is limited due to the insufficient whitening effect thereof, a problem of skin safety, and problems associated with formulation and stability, which occur when they are added to cosmetic products.
SUMMARY OF THE INVENTION
The present inventors have conducted repeated and various experiments and, as a result, have found that a cosmetic composition containing either extracts of Commiphora mukul resin extract and Terminalia chebula or extracts of Withania somnifera (Ashwagandha) root, Andrographis paniculata and Phyllanthus emblica extract in addition to Commiphora mukul resin and Terminalia chebula among Indian natural materials is safe for the skin and, at the same time, can exhibit an excellent whitening effect, thereby completing the present invention.
Therefore, it is an object of the present invention to a skin-whitening cosmetic composition containing a Commiphora mukul resin extract and a Terminalia chebula extract.

To achieve the above object, the present invention provides a skin-whitening cosmetic composition containing a Commiphora mukul resin extract and a Terminalia chebula extract. The present invention also provides a skin-whitening cosmetic composition containing a Withania somnifera (Ashwagandha) root extract, an Andrographis paniculata extract and a Phyllanthus emblica extract in addition to the Commiphora mukul resin extract and the Terminalia chebula extract.
BRIEF DESCRIPTION OF THE DRAWINGS
FIG. 1 is a graphic diagram showing a comparison of the skin-whitening effects of a Commiphora mukul resin extract, a Terminalia chebula extract, a Withania somnifera (Ashwagandha) root extract, an Andrographis paniculata extract and a Phyllanthus emblica extract, measured in Test Example 1.
FIG. 2 is a graphic diagram showing a comparison of the skin-whitening effects of a Commiphora mukul resin extract and a Terminalia chebula extract, mixed with each other at various ratios, and the whitening effects of a Commiphora mukul resin extract, a Terminalia chebula extract, a Withania somnifera [Ashwagandha) root extract, an Andrographis paniculata extract and a Phyllanthus emblica extract, mixed with each other at a specific ratio, in which the whitening effects were measured in Test Example 1.

DETAILED DESCRIPTION OF THE INVENTION
The present invention provides a skin-whitening cosmetic composition containing a Commiphora mukul resin extract and a Terminalia chebula extract as active ingredients.
The present invention also provides a skin-whitening cosmetic composition containing a Commiphora mukul resin extract, a Terminalia chebula extract, a Withania somnifera '(Ashwagandha) root extract, an Andrographis paniculata extract and a Phyllanthus emblica extract as active ingredients.
Hereinafter, the present invention will be described in detail.
Among Indian natural materials which are contained as active ingredients in the composition of the present invention, Commiphora mukul resin native to India, Northeast Africa and Afghanistan has been used in the Indian traditional ayurvedic medicine system for about 3,000 years. It produces the natural resin guggul gum, and the major active material thereof is guggulsterone that is a steroid. It is used for anti-inflammation, fever relief, disinfection, insect extermination, stimulus relief, diaphoretic treatment, diuretic treatment and so on, and is known as a farnesoid X receptor (FXR) antagonist to inhibit cholesterol synthesis in the liver. However, it was also reported that the above resin increases the level of low-

density lipoprotein which is harmful to many persons, while the resin does not decrease the total level of cholesterol.
Terminalia chebula native to India, Sri Lanka, Southeast Asia and China is known as catholicon in the Indian traditional ayurvedic medicine system and famous for treatment of blind persons. It is used for treatment of infectious diseases, chronic ulcer and fungal skin infection, aging prevention, immune enhancement and so on.
Withania somnifera (Ashwagandha) root native to India is a Sanskrit term that means "smelling like a horse". It is called "Indian ginseng" or "king of herbs" and is one of the most important ayurveda herbs, which has been used for 4,000 years or more in India. It contains alkaloids and withanolides as main components, which belong to the steroid family and have the functions and structures similar to those of gensenosides that are the main components of ginseng. It helps in recovering from diseases or is used as a tonic and for treatment of tumors, inflammatory and infectious diseases.
Andrographis paniculata native to India and Sri Lanka is bitter, hot and cold in nature. It is known as a wonder drug in the traditional ayurvedic medicine system in India and Sri Lanka and is usually used as a purgative and for trauma treatment, fever relief, anti-inflammation, digestion, insect extermination and so on. Andrographolide that is the main component of Andrographis paniculata is abundantly contained in

the leaves and is known as an agent having an excellent liver-protecting function. Recently, it has been studied as an agent having excellent physiological activity. In addition, it has been used in the treatment of human cancers and immune cells, studies on cell activity processes, and drug targeting studies. The LD50 of andrographolide is 11.46 gm/kg (ip) .
Phyllanthus emblica is native to India, western Afghanistan and Myanmar. It is sour and bitter in taste and has a high content of vitamin C. The main components thereof include vitamin C, tannin, flavonoids, kaempferol, ellagic acid and gallic acid. It is believed that Phyllanthus emblica has an antioxidant effect caused by vitamin C, but it was also reported to an antioxidant effect caused by a high content of tannin. It is mainly used for antioxidation, protection of scalp and hairs, removal of skin wrinkles, treatment of constipation, prevention of stroke, etc.
Extracts of the above Indian natural materials that are used in the present invention can be prepared using solvents under the conditions of temperature and pressure according to conventional methods.
Specifically, the extracts of the present invention are obtained by extraction from various organs or portions of natural materials (e.g., leaves, flowers, roots, stems and barks) and can be prepared according to conventional methods known in the art. Specifically, the extracts can be obtained

from natural materials using various extraction solvents, for example, an extraction solvent selected from the group consisting of water, anhydrous or hydrated lower alcohols having 1 to 4 carbon atoms (methanol, ethanol, propanol and butanol), acetone, ethyl acetate, chloroform, 1,3-butyleneglycol and butyl acetate.
Meanwhile, it will be obvious to those skilled in the art that, even when extraction solvents other than the above-described extraction solvents are used, extracts exhibiting substantially the same effects as those of the extracts obtained by the above-described extraction solvents can be obtained. The scope of the extracts of the present invention includes not only the extracts obtained by the above-described extraction solvents, but also extracts subjected to conventional purification processes. For example, fractions obtained through various additional purification methods, for example, separation with an ultrafiltration membrane having a given molecular weight cut-off, separation by various chromatography systems (manufactured for separation according to size, charge, hydrophobicity or affinity), are also included in the scope of the extracts of the present invention.
Preferably, the extracts of the present invention can be prepared according to methods as described in the following Reference Examples 1 to 5.

The Commiphora mukul resin extract of the present invention is contained in an amount of 0.0001-20 wt% based on the total weight of the composition. If the content of the extract is less than 0.0001 wt%, its effect on the skin will be insufficient, and if the content is more than 20 wt%, it will reduce formulation stability, and an increase in the content thereof will not lead to a significant increase in the effect thereof.
The Terminalia chebula extract of the present invention is contained in an amount of 0.0001-20 wt% based on the total weight of the composition. If the content of the extract is less than 0.0001 wt%, its effect will be insufficient, and if the content is more than 20 wt%, it will reduce formulation stability, and an increase in the content thereof will not lead to a significant increase in the effect thereof.
The Withania somnifera (Ashwagandha) root extract of the present invention is contained in an amount of 0.0001-20 wt% based on the total weight of the composition. If the content of the extract is less than 0.0001 wt%, its effect on the skin will be insufficient, and if the content is more than 20 wt%, it will reduce formulation stability, and an increase in the content thereof will not lead to a significant increase in the effect thereof.
The Andrographis paniculata extract of the present invention is contained in an amount of 0.0001-20 wt% based on

the total weight of the composition. If the content of the extract is less than 0.0001 wt%, its effect on the skin will be insufficient, and if the content is more than 20 wt%, it will reduce formulation stability, and an increase in the content thereof will not lead to a significant increase in the effect thereof.
The Phyllanthus emblica extract of the present invention is contained in an amount of 0.0001-20 wt% based on the total weight of the composition. If the content of the extract is less than 0.0001 wt%, its effect on the skin will be insufficient, and if the content is more than 20 wt%, it will reduce formulation stability, and an increase in the content thereof will not lead to a significant increase in the effect thereof.
When the composition of the present invention contains the extracts in the above-described content ranges, it will exhibit the effects intended by the present invention and can both satisfy stability and safety. In addition, the composition will be advantageous in terms of costs and effects.
The Withania somnifera {Ashwagandha) root extract, the Andrographis paniculata extract and the Phyllanthus emblica extract are used at limited concentrations because of the odors and properties thereof, but enhance the effect of the composition even when they are used in small amounts.

In addition, the Commiphora mukul resin extract, the Terminalia chebula extract, the Withania somnifera (Ashwagandha) root extract, the Andrographis paniculata extract and the Phyllanthus emblica extract are preferably contained at a weight ratio of 1-20: 1-20: 1-5: 1-5: 1-5, and more preferably 11:11:1:1:1.
Hereinafter, the present invention will be described in further detail with reference to examples, but are not intended to limit the scope of the present invention.
Reference Example 1: Preparation of Commiphora mukul resin extract (C)
To 1 kg of Commiphora mukul resin was added 5 ethanol aqueous solution, extracted three times under reflux,
and then dipped at 15 °C for 3 days. Next, the dipped solution
was filtered through filter cloth and centrifuged into residue and a filtrate, and the separated filtrate was concentrated under reduced pressure, thereby obtaining 10 g of a Commiphora mukul resin extract.
Reference Example 2: Preparation of Terminalia chebula extract (T)
To 1 kg of Terminalia chebula - was added 5 ethanol aqueous solution, extracted three times under reflux,
and then dipped at 15 °C for 1 day. Next, the dipped solution was filtered through filter cloth and centrifuged into residue

and a filtrate, and the separated filtrate was concentrated under reduced pressure, thereby obtaining 50 g of a Terminalia chebula extract.
Reference Example 3: Preparation of Andrographis paniculata extract (A)
To 1 kg of Andrographis paniculata was added 5 ethanol aqueous solution, extracted three times under reflux,
and then dipped at 15 °C for 1 day. Next, the dipped solution
was filtered through filter cloth and centrifuged into residue and a filtrate, and the separated filtrate was concentrated under reduced pressure, thereby obtaining 25 g of an Andrographis paniculata extract.
Reference Example 4: Preparation of Withania somnifera (Ashwagandha) root extract (W)
To 1 kg of Withania somnifera (Ashwagandha) was added 5 of 70% ethanol aqueous solution, extracted three times under
reflux, and then dipped at 15 °C for 1 day. Next, the dipped
solution was filtered through filter cloth and centrifuged into residue and a filtrate, and the separated filtrate was concentrated under reduced pressure, thereby obtaining 30 g of an Andrographis paniculata extract.
Reference Example 5: Preparation of Phyllanthus emblica extract (W)

To 1 kg of Phyllanthus emblica extract was added 5 70% ethanol aqueous solution, extracted three times under
reflux, and then dipped at 15°C for 1 day. Next, the dipped
solution was filtered through filter cloth and centrifuged into residue and a filtrate, and the separated filtrate was concentrated under reduced pressure, thereby obtaining 25 g of a Phyllanthus emblica extract.
Test Example 1: Inhibitory effect on tyrosinase activity In order to examine the skin-whitening effect of the composition of the present invention, a mushroom tyrosinase activity assay was performed.
The enzyme tyrosinase used in this Test Example was a tyrosinase (SIGMA) extracted from mushrooms. First, the substrate tyrosine was dissolved in distilled water at a
concentration of 0.3 mg/Me, and the solution was placed in a 1.0-Me test tube. Then, 1.0 Me of potassium-phosphate buffer
(0.1 M, pH 6.8) and 0.7 Me of distilled water were added
thereto, thereby forming a mixed solution.
Each of the Commiphora mukul resin extract (Comparative Example 1), the Terminalia chebula extract (Comparative Example 2), the Andrographis paniculata extract (Comparative Example 3) , the Withania somnifera {Ashwagandha) root extract (Comparative Example 4), the Phyllanthus emblica extract

(Comparative Example 5) , and mixtures thereof (Examples 1 to 4), which are Indian natural materials, was dissolved in
ethanol at concentrations of 100 ug/Me, 10 ug/Me. and lug/Me, and 0.2 Me of each of the extract sample solutions was added to the
mixed solution, and then incubated in an incubator at 37 °C for
10 minutes. As a negative control, 0.2 ml of a solvent alone was used instead of each extract sample, and as a positive control, kojic acid (KA) known as a tyrosinase inhibitor was
used. 0.1 Me of a tyrosinase solution {2500 unit/Mi!) was added to each of the reaction solutions and incubated in an incubator
at 37 °C for 10 minutes. Then, the test tube containing the
reaction solution was quenched with ice water to stop the reaction, and the absorbance at 475 nm was measured with a photoelectric spectrophotometer. Then, tyrosinase activity for each of the extracts was calculated using the following equation, and the results of the calculation are shown in FIG. 1.
[Equation 1]
Tyrosinase activity (%) = (absorbance of group containing test sample / absorbance of group containing no test sample) x 100

As can be seen in FIG. 1, when the Commiphora mukul resin extract (Comparative Example 1), the Terminalia chebula extract (Comparative Example 2), the Andrographis paniculata extract (Comparative Example 3), the Withania somnifera {Ashwagandha) root extract (Comparative Example 4) and the Phyllanthus emblica extract (Comparative Example 5) were used alone, tyrosinase activities were not inhibited, except for the case in which the . Terminalia chebula extract was used at a
concentration of 100 uq/Me Thus, the tyrosinase activities of
the extracts of Comparative Examples 1 to 5 were similar to that of the negative control. Therefore, it can be seen that, when the extracts are used alone, they have little or no skin-whitening effect.
Meanwhile, as can be seen in FIG. 2, when the Commiphora mukul resin extract having no inhibitory effect was mixed with the Terminalia chebula extract at various ratios (Examples 1 to 3) , the mixtures exhibited inhibitory effects on tyrosinase activity, unlike when the Commiphora mukul resin extract was used alone. In addition, when the Withania somnifera {Ashwagandha) root extract, the Andrographis paniculata extract and the Phyllanthus emblica extract were mixed with the Commiphora mukul resin extract and the Terminalia chebula extract (Example 4), the mixture had a better inhibitory effect on tyrosinase activity and thus an excellent skin-whitening

effect (C: Commiphora mukul resin extract, T: Terminalia chebula extract, A: Andrographis paniculata extract, W: Wi thania somnifera (Ashwagandha) root extract, and P: Phyllanthus emblica extract).
As described above, the composition of the present invention contains the Commiphora mukul resin extract, the Terminalia chebula extract, the Withania somnifera {Ashwagandha) root extract, the Andrographis paniculata extract and the Phyllanthus emblica extract, which exhibit skin-whitening effects. Thus, the composition of the present invention can be effectively used in the cosmetic field.

We Claim :
1. A skin-whitening cosmetic composition containing a Commiphora mukul resin extract and a Terminalia chebula extract.
2. The skin-whitening cosmetic composition of claim 1, further containing a Withania somnifera (Ashwagandha) root extract, an Andrographis paniculata extract and a Phyllanthus emblica extract.
3. The skin-whitening cosmetic composition of claim 1, wherein each of the Commiphora mukul resin extract and the Terminalia chebula extract is contained in an amount of 0.0001-20 wt% based on the total weight of the composition.
i
4. The skin-whitening cosmetic composition of claim 2,
wherein each of the Withania somnifera {Ashwagandha) root extract, the Andrographis paniculata extract and the Phyllanthus emblica extract is contained in an amount of 0.0001-20 wt% based on the total weight of the composition.
5. The skin-whitening cosmetic composition of claim 2,
wherein the Commiphora mukul resin extract, the Terminalia
chebula extract, the Withania somnifera {Ashwagandha) root
extract, the Andrographis paniculata extract and the

Phyllanthus emblica extract are contained at a weight ratio of 1-20: 1-20: 1-5: 1-5: 1-5.

Documents

Application Documents

# Name Date
1 3329- MUM -2012 - AFR - 21-1-2013.pdf 2023-10-26
1 ABSTRACT1.jpg 2018-08-11
2 3329- MUM -2012 -KOREAN PRIORITY- 4-4-2013.pdf 2023-10-26
2 3329-MUM-2012-POWER OF ATTORNEY(4-4-2013).pdf 2018-08-11
3 3329-MUM-2012-FORM 5.pdf 2018-08-11
3 3329-MUM-2012-AbandonedLetter.pdf 2019-12-09
4 3329-MUM-2012-FORM 3.pdf 2018-08-11
4 3329-MUM-2012-FER.pdf 2019-01-31
5 3329-MUM-2012-FORM 2[TITLE PAGE].pdf 2018-08-11
5 3329-MUM-2012-ABSTRACT.pdf 2018-08-11
6 3329-MUM-2012-FORM 2.pdf 2018-08-11
6 3329-MUM-2012-CLAIMS.pdf 2018-08-11
7 3329-MUM-2012-FORM 1.pdf 2018-08-11
7 3329-MUM-2012-CORRESPONDENCE(4-4-2013).pdf 2018-08-11
8 3329-MUM-2012-FORM 1(4-4-2013).pdf 2018-08-11
8 3329-MUM-2012-CORRESPONDENCE.pdf 2018-08-11
9 3329-MUM-2012-DESCRIPTION(COMPLETE).pdf 2018-08-11
9 3329-MUM-2012-ENGLISH TRANSLATION VERIFICATION(4-4-2013).pdf 2018-08-11
10 3329-MUM-2012-DRAWING.pdf 2018-08-11
11 3329-MUM-2012-DESCRIPTION(COMPLETE).pdf 2018-08-11
11 3329-MUM-2012-ENGLISH TRANSLATION VERIFICATION(4-4-2013).pdf 2018-08-11
12 3329-MUM-2012-CORRESPONDENCE.pdf 2018-08-11
12 3329-MUM-2012-FORM 1(4-4-2013).pdf 2018-08-11
13 3329-MUM-2012-CORRESPONDENCE(4-4-2013).pdf 2018-08-11
13 3329-MUM-2012-FORM 1.pdf 2018-08-11
14 3329-MUM-2012-CLAIMS.pdf 2018-08-11
14 3329-MUM-2012-FORM 2.pdf 2018-08-11
15 3329-MUM-2012-ABSTRACT.pdf 2018-08-11
15 3329-MUM-2012-FORM 2[TITLE PAGE].pdf 2018-08-11
16 3329-MUM-2012-FER.pdf 2019-01-31
16 3329-MUM-2012-FORM 3.pdf 2018-08-11
17 3329-MUM-2012-AbandonedLetter.pdf 2019-12-09
17 3329-MUM-2012-FORM 5.pdf 2018-08-11
18 3329- MUM -2012 -KOREAN PRIORITY- 4-4-2013.pdf 2023-10-26
18 3329-MUM-2012-POWER OF ATTORNEY(4-4-2013).pdf 2018-08-11
19 ABSTRACT1.jpg 2018-08-11
19 3329- MUM -2012 - AFR - 21-1-2013.pdf 2023-10-26

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