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PATENT ABSTRACTS OF JAPAN 

(11)Publication number : 10-017458 
(43)Date of publication of application : 20.01 .1998 

(51)lnt.CI. A«{ J/« 

v ' A61K 7/00 

A61K 35/78 
A61K 35/78 
A61K 35/78 

I ■ ' ' 

(21) Application number : 08-185665 (71 Applicant : POLA CHEM IND INC 

(22) Dateof filing : 26.06.1996 (72)lnventor : KITADAYOSHIO 

OSHIMAHIROSHI 
ANDO NOBUHIRO 

(54) AGENT FOR IMPROVING UNUNIFORMITY OF SKIN AND COSMETIC CONTAINING 
THE SAME 

(57)Abstract: 

PROBLEM TO BE SOLVED: To obtain a composition containing the essence of a plant, 
capable of improving the ununiformity of skin and improving and preventing skin darkness 
caused by ageing, etc., and useful for cosmetics, etc. 

SOLUTION: This agent for improving the ununiformity of skin contains the essences of one or 
more kinds of plants selected from among Betula pendula Roth., Zizyphus jujuba Mill., Rosa 
multiflora Thun., Hypericum erectum Thun., Hypericum perforatum L., Salvia officinalis L., 
Paeonia lactiflora Pall, Urtica thunbergiana Sie., and Nelumbonaceae Nelumbo. The essence 
includes the plant itself, its processed product and/or solvent extract or solvent-removed 
extract obtained by drying, grinding, finely cutting, etc., a part or all parts of the plant, and their 
fractions. A polar solvent such as 1 ,3-butanediol is used for the solvent extraction. The 
cosmetic contains the skin ununiformity-improving agent in an amount of 0.001 -10wt.%, and 
may be prepared into a basic cosmetic, a make-up cosmetic, a hair cosmetic, a nail- 
beautifying agent, a cleanser, a bathing agent, etc. 



LEGAL STATUS 

[Date of request for examination] 16.1 1 .2000 

[Date of sending the examiner's decision of 12.11 .2002 



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rejection] 

[Kind of final disposal of application other than 
the examiner's decision of rejection or 
application converted registration] 

[Date of final disposal for application] 

[Patent number] 3615312 

[Date of registration] 12.1 1 .2004 

[Number of appeal against examiner's 2002-23853 
decision of rejection] 

[Date of requesting appeal against examiner's 12.12.2002 
decision of rejection] 

[Date of extinction of right] 



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* NOTICES * 

JPO and NCIPI are not responsible for any 
damages caused by the use of this translation. 

1 .This document has been translated by computer. So the translation may not reflect the original 
precisely. 

2 **** shows the word which can not be translated. 
3. In the drawings, any words are not translated. 



DETAILED DESCRIPTION 



[Detailed Description of the Invention] 
[0001] 

[Field of the Invention] This invention relates to the cosmetics containing the ununiformity 
improvement agent of the suitable skin concerned to carry out improvement prevention of the dullness 
resulting from the ununiformity improvement agent of the skin, aging, etc. 
[0002] 

[Description of the Prior Art] It has the wish said that he wants for anyone to see more beautifully than 
others. For this reason, the mechanism for looking beautifully was studied and the various cosmetics 
based on that result have been developed. For example, the cosmetics which the cosmetics containing 
moisturizing components, such as hyaluronate sodium, can raise the amount of moisture maintenance of 
the skin, can prevent formation of a wrinkling, and contain an ascorbic-acid derivative can prevent 
controlling generation of melanin and the color of the skin becoming black. The present condition is that 
the phenomenon called so-called "dullness" into such technological innovation is not clarified more, and 
the mechanism is not developed yet in it by the cosmetics to improve. The "dullness" said here is in the 
condition that there is no sensibility which redness decreased, and the color of the skin looked dark and 
was lively, and sag is sensed, increasing as the badness and age of condition are piled up is already 
known, and it does not want to be in such [ anyone ] a condition. Although it can be improved by 
"dullness" by taking a measure by the cosmetics developed until now, to the forge fire by which 
whitening cosmetics suppress generation of melanin and maintain whiteness at the forge fire which 
moisturization cosmetics improve a wrinkling or prevent, the effectiveness is not large. This is said to be 
because for "dullness" to differ in these physiological phenomena and classes, and a cause. 
[0003] Under such a situation, this invention person etc. found out that "dullness" originated in the 
heterogeneity of the fine structure of the skin, as a result of repeating research wholeheartedly in quest 
of the cause of "dullness." However, the present condition was not known at all about the material which 
improves the heterogeneity of such the skin. 

[0004] Improving "dullness" that the essence of the vegetation shown below improves the heterogeneity 
of such the skin on the other hand and its result was not known at all. The Betulaceae birch (Betula 
pendula Roth.), The department zizyphi fructus of a jujube tree (Zizyphus jujuba Mill.), Rosaceae Rose 
Fruit (Rosa multiflora Thun.), The Guttiferae St. John's wort (Hypericum erectum Thun.), The 
Guttiferae SEIYOU St. John's wort (Hypericum perforatum L.) ? The Lamiaceae SAGE (Salvia 
officinalis L.) 3 the Paeoniaceae peony (Paeonia lactiflora Pall), the Urticaceae nettle (Urtica 
thunbergiana Sie. or Urtica dioica L.) and Nelumbonaceae — a lotus (Nelumbonaceae Nelumbo) 
[0005] 

[Problem(s) to be Solved by the Invention] This invention is performed under this situation and let it be 

a technical problem to offer the material which improves the heterogeneity of the skin. 

[0006] 

[Means for Solving the Problem] As a result of this invention person's etc. repeating research 
wholeheartedly in quest of the cause of "dullness" in view of this situation, the heterogeneity of the skin 



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found out that it was a big element. As a result of repeating the further research in quest of the matter 
which has the operation which improves the heterogeneity of the skin based on this knowledge, such an 
operation was found out to the essence of the plant body shown below. Furthermore, when examination 
was repeated, it checks that the prominent effect which improves "dullness" is in the cosmetics 
containing these compounds, and came to complete invention. Hereafter, this invention is explained to a 
detail focusing on the gestalt of implementation of invention. The Betulaceae birch (Betula pendula 
Roth.), The department zizyphi fructus of a jujube tree (Zizyphus jujuba Mill.), Rosaceae Rose Fruit 
(Rosa multiflora Thun.), The Guttiferae St. John's wort (Hypericum erectum Thun.), The Guttiferae 
SEIYOU St. John's wort (Hypericum perforatum L.), The Lamiaceae SAGE (Salvia officinalis L.), the 
Paeoniaceae peony (Paeonia lactiflora Pall), the Urticaceae nettle (Urtica thunbergiana Sie. or Urtica 
dioica L.) and Nelumbonaceae — a lotus (Nelumbonaceae Nelumbo) 
[0007] 

[Embodiment of the Invention] 

(1) The heterogeneity improvement agent of the skin of heterogeneity improvement agent this invention 
of the skin of this invention consists of essence of the vegetation shown below. Essence is the generic 
name of the plant body itself, the workpiece with which desiccation, grinding, a fragment, etc. carried 
out some or all of a plant body, some or all of a plant body, the solvent extraction object of those 
workpieces or its solvent removal object, and also those fractionation objects here. The most desirable 
thing is the solvent extraction object or its solvent removal object of some or all of a plant body, or those 
workpieces among these essence. As a solvent used for solvent extraction, a polar solvent is desirable, 
and polyhydric alcohol, such as ketones, such as halogenated hydrocarbon, such as ether, such as nitril, 
such as ester, such as alcohols, such as a methanol and ethanol, ethyl acetate, and methyl formate, and 
an acetonitrile, diethylether, and a tetrahydrofuran, chloroform, and a methylene chloride, an acetone, 
and a methyl ethyl ketone, 1,3-butanediol, and a glycerol, and water can illustrate preferably as a polar 
solvent, for example. Even if it uses these independently and they mix and use two or more sorts, they 
are not cared about. An among these more desirable thing is the approach of extracting using one sort 
chosen from alcohols, polyhydric alcohol, and water, or two sorts or more. That what is necessary is just 
to carry out according to the usual approach, the approach of an extract adds a 1 to 10 times as many 
solvent as this to the workpiece of a plant body or a plant body, and if it is a room temperature, if it is 
the temperature near the boiling point, it should just be immersed several days for several hours. Stirring 
can also be added suitably. The extract obtained in this way may be used as it is, and even if it removes a 
solvent by reduced pressure distilling out etc. or it refines and uses it by the silica gel column 
chromatography, liquid-liquid extraction, etc., it is not cared about. Below, the example of manufacture 
is shown. The Betulaceae birch (Betula pendula Roth.), The department zizyphi fructus of a jujube tree 
(Zizyphus jujuba Mill.), Rosaceae Rose Fruit (Rosa multiflora Thun.), The Guttiferae St. John's wort 
(Hypericum erectum Thun.), The Guttiferae SEIYOU St. John's wort (Hypericum perforatum L.), The 
Lamiaceae SAGE (Salvia officinalis L.), the Paeoniaceae peony (Paeonia lactiflora Pall), the Urticaceae 
nettle (Urtica thunbergiana Sie. or Urtica dioica L.) and Nelumbonaceae « a lotus (Nelumbonaceae 
Nelumbo) 

[0008] [Example 1 of manufacture] After adding 1,3-butanediol 1kg to the leaf of a birch, a bark, and 
lkg of xylem and heating at 90 degrees C for 3 hours, insoluble matter was carried out the ** exception 
and 0.8kg of heterogeneity improvement agents 1 of the skin was obtained. 

[0009] [Example 2 of manufacture] 101. of ethanol water solutions was added to the leaf of a birch, a 
bark, and lkg of xylem 50%, it flowed back for 2 hours, insoluble matter was carried out the ** 
exception, the solvent was distilled out, and the heterogeneity improvement agent 2 of the 68g skin was 
obtained. 

[0010] [Example 3 of manufacture] 101. of ethanol water solutions was added to lkg of dry matters of 
the fruit of zizyphi fructus 50%, it flowed back for 2 hours, insoluble matter was carried out the ** 
exception, the solvent was distilled out, and the heterogeneity improvement agent 3 of the 430g skin was 
obtained. 

[001 1] [Example 4 of manufacture] 101. of ethanol water solutions was added to lkg of dry matters of 



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the fruits of Rose Fruit 50%, it flowed back for 2 hours, insoluble matter was carried out the ** 
exception, the solvent was distilled out, and the heterogeneity improvement agent 4 of the 180g skin was 
obtained. 

[0012] [Example 5 of manufacture] 101. of ethanol water solutions was added to 1kg of entire plants of a 
St. John's wort 50%, it flowed back for 2 hours, insoluble matter was carried out the ** exception, the 
solvent was distilled out, and the heterogeneity improvement agent 5 of the 144g skin was obtained. 
[0013] [Example 6 of manufacture] 101. of ethanol water solutions was added to 1kg of entire plants of a 
SEIYOU St. John's wort 50%, it flowed back for 2 hours, insoluble matter was carried out the ** 
exception, the solvent was distilled out, and the heterogeneity improvement agent 6 of the 138g skin was 
obtained. 

[0014] [Example 7 of manufacture] 101. of ethanol water solutions was added to 1kg of roots of a peony 
50%, it flowed back for 2 hours, insoluble matter was carried out the ** exception, the solvent was 
distilled out, and the heterogeneity improvement agent 7 of the 25 lg skin was obtained. 
[0015] [Example 8 of manufacture] 101. of ethanol water solutions was added to 1kg of leaves of a nettle 
50%, it flowed back for 2 hours, insoluble matter was carried out the ** exception, the solvent was 
distilled out, and the heterogeneity improvement agent 8 of the 165g skin was obtained. 
[0016] [example 9 of manufacture] Nelumbonaceae -- ethanol 101. was added to 1kg of rhizomes of a 
lotus 50%, it flowed back for 2 hours, insoluble matter was carried out the ** exception, the solvent was 
distilled out, and the heterogeneity improvement agent 9 of the 123g skin was obtained. 
[0017] (2) It is characterized by the cosmetics of cosmetics this invention of this invention containing 
the heterogeneity improvement agent of the above-mentioned skin. The heterogeneity improvement 
agent of the skin may make a seed contain uniquely, and may make two or more sorts contain. If the 
classes of cosmetics of this invention are cosmetics usually known generally, special limitation is not 
received, for example, baths, such as charges of washing, such as nail enamels, such as hair cosmetics, 
such as makeup cosmetics, such as basic cosmetics, such as a cream and a milky lotion, foundation, and 
a lip color, hair oil, a hair tonic, a shampoo, and a rinse, a manicure, and a pedicure, a body shampoo, 
and soap, a bus bubble, and bus essence, etc. can illustrate it preferably. This is because the 
heterogeneity improvement agent of the skin of this invention can improve not only the heterogeneity of 
the skin but the heterogeneity of the body organization near the skin, so a desirable operation can be 
discovered also on the hair and the pawl of hair. It is 0.001 - 10 % of the weight, the desirable content of 
the heterogeneity improvement agent of the skin in the cosmetics of this invention has 0.01 - 5 more 
desirable % of the weight, and its 0.05 - 1 % of the weight is still more desirable. The cosmetics of this 
invention can contain the arbitration component usually used by cosmetics in addition to the 
heterogeneity improvement agent of these skins. As such an arbitration component, thickeners, such as 
polyhydric alcohol, such as fatty acids, such as higher alcohol, such as triglyceride, such as ester, such 
as hydrocarbons, such as vaseline and a micro crystallin wax, jojoba oil, and spermaceti, beef tallow, 
and olive oil, cetanol, and oleyl alcohol, stearin acid, and oleic acid, a glycerol, and 1,3-butanediol, a 
nonionic surface active agent, an anionic surface active agent, a cationic surface active agent, an 
amphoteric surface active agent, ethanol, and Carbopol, antiseptics, an ultraviolet ray absorbent, an anti- 
oxidant, coloring matter, and fine particles can be illustrated. The cosmetics of this invention can be 
manufactured by processing these raw materials by the usual approach. The cosmetics of this invention 
have the operation which improves the heterogeneity of the skin and carries out improvement prevention 
of the dullness. Therefore, the cosmetics of this invention can show those who make up their face more 
youthfully than real age, and are suitable also as cosmetics for the prevention improvement of aging. 
[0018] 
[Example] 

Face toilet was created according to the [example 1 ] following formula. That is, the heating dissolution 
of the formula component was carried out at 80 degrees C, stirring cooling was carried out and face 
toilet was obtained. 

1,3-butanediol 5 Weight section glycerol 5 Weight section hyaluronate sodium The 0.1 weight section 
methylparaben The heterogeneity improvement agent 1 of 0.1 weight **** 0.1 weight section 



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benzalkonium chloride 0.1 weight section sodium dihydrogenphosphate 0.1 weight section ethanol 7 
Weight section POE (60) hydrogenated castor oil 0.1 weight sections perfume 0.1 weight **** The 82.3 
weight sections [0019] Face toilet was created according to the [example 2] following formula. That is, 
the heating dissolution of the formula component was carried out at 80 degrees C, stirring cooling was 
carried out and face toilet was obtained. 

1,3-butanediol 5 Weight section glycerol 5 Weight section hyaluronate sodium The 0.1 weight section 
methylparaben The heterogeneity improvement agent 2 of 0.1 weight **** The heterogeneity 
improvement agent 30.5 weight section benzalkonium chloride of 0.1 weight **** 0.1 weight section 
sodium dihydrogenphosphate 0.1 weight section ethanol 7 Weight section POE (60) hydrogenated castor 
oil 0.1 weight sections perfume 0.1 weight **** The 81.8 weight sections [0020] Face toilet was created 
according to the [example 3] following formula. That is, the heating dissolution of the formula 
component was carried out at 80 degrees C, stirring cooling was carried out and face toilet was obtained. 

1,3-butanediol 5 Weight section glycerol 5 Weight section sodium chondroitin sulfate The 0.1 weight 
section methylparaben The heterogeneity improvement agent 4 of 0.1 weight **** 0.5 weight section 
benzalkonium chloride 0.1 weight sections sodium dihydrogenphosphate 0.1 weight section ethanol 7 
Weight section POE (60) hydrogenated castor oil 0.1 weight sections perfume 0.1 weight **** The 81.9 
weight sections [0021] The cream was created according to the [example 4] following formula. That is, 
the heating dissolution of each component of I, RO, and Ha was carried out at 80 degrees C, I was 
kneaded well, RO was added and diluted, and Ha was added gradually and emulsified. Stirring cooling 
of this was carried out and the cream was obtained. 

I 1,3-butanediol 5 70% maltitol water solution of weight sections 10 Weight section methylparaben The 
0.3 weight section butylparaben 0.1 weight section triglycerinediisostearate 4 Weight section RO liquid 
paraffin 7 Weight section carnauba wax 3 Weight section dimethicone 4 (lc.s.) Weight section Ha water 
Heterogeneity improvement agent 5 of 66.5 weight **** Heterogeneity improvement agent 6 of 0.5 
weight **** 0.5 weight sections hyaluronate sodium The 0.1 weight sections [0022] Foundation was 
created according to the [example 5] following formula. That is, the heating dissolution of each 
component of I, RO, and Ha was carried out at 80 degrees C, I was kneaded well, and RO was added 
and diluted, NI was added and it distributed, and Ha was added gradually and emulsified. Stirring 
cooling of this was carried out and foundation was obtained. 

I 1,3-butanediol 5 70% maltitol water solution of weight sections 10 Weight section methylparaben The 
0.3 weight section butylparaben 0.1 weight section triglycerinediisostearate 4 Weight section RO liquid 
paraffin 7 Weight section carnauba wax 3 Weight section dimethicone 4 (lc.s.) Weight section Ha water 
49 The heterogeneity improvement agent 7 of weight **** 0.5 weight section hyaluronate sodium 0.1 
weight section NI titanium oxide 8 Weight section talc 3 Weight section sericite 2 Weight section 
Synthetic Ochre 3 Weight section red ocher 2 Weight section [0023] The hair tonic was created 
according to the [example 6] following formula. That is, stirring solubilization of the formula 
component was carried out at the balance lump and the room temperature, and the hair tonic was 
obtained. 

Ethinylestradiol 0.1 weight section capsicum tincture 0.1 weight section menthol The heterogeneity 
improvement agent 8 of 0.1 weight **** 0.1 weight section ethanol 40 Weight section 1,3-butanediol 5 
Weight **** The 54.6 weight sections [0024] Baths were created according to the [example 7] 
following formula. That is, it lump [ balance ] and was good for the kneader, the formula component 
was kneaded, and baths were obtained. 

A sodium sulfate 70 Weight section lavender oil 10 Weight section 1,3-butanediol 10 Heterogeneity 
improvement agent 9 of weight **** 1 Weight section glycerol Nine weight sections [0025] The 
heterogeneity improvement operation of the skin was measured about the heterogeneity improvement 
agents 1-9 of the skin of [example 8] this invention. That is, the ultraviolet-rays B exposure of 0.8MED 
(s) was performed twice to 20 volunteers' overarm, the uneven skin model was created, the specimen 
was prescribed for the patient here for four weeks, and the gestalt was observed after five weeks. The 
observations of a gestalt were the heterogeneity of the distribution judging of a low brightness part, the 



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judgment of melanin distribution, and horny layer exfoliation, the homogeneity of distribution of the 
low brightness part at the time of the distribution judging of a low brightness part irradiating light to the 
skin from 45 slant, and incorporating as an image with a CCD camera — score 2: — very homogeneity, 
score 1 :homogeneity, and score 0.5: — a little — homogeneity and score 0: — it was uneven and judged 
with the naked eye. Distribution of melanin stripped the horny layer on the cellophane tape, performed 
the Fontana Masson dyeing and a hematoxylin and eosin stain, observed the melanin distribution for 
every bottom cell of a microscope with the naked eye, and judged it on the following criteria. Score 2: 
For homogeneity and 0.5:distribution, homogeneity and 0:distribution are [ distribution / homogeneity 
and score 1 distribution ] an ununiformity a little very much. Moreover, the method of exfoliation of a 
horny layer was also judged on the following criteria to coincidence at this time. Score 2: For 
homogeneity and the method of 0.5:exfoliation, homogeneity and the method of 0:exfoliation are [ the 
method of exfoliation / homogeneity and the method of score 1 : exfoliation ] an ununiformity a little 
very much. A result is shown in Table 1 as an average score. In addition, a specimen is what melted the 
heterogeneity improvement agent of each skin in the ethanol water solution 50% by 1% of 
concentration, and control used the ethanol water solution 50%. Moreover, no taking a measure did not 
perform UV irradiation, and did not prescribe it for the patient at all. This shows that the heterogeneity 
improvement agent of the skin of this invention is excellent in a heterogeneity improvement operation of 
the skin. 



[0026] 
Table 11 






*7 








i . 


4 


1 . 


2 


l. 


2 


3 y Y a — )\> 


0. 


4 


0. 


6 


0. 


5 




0. 


9 


0. 


9 


1. 


0 




1. 


0 


0. 


9 


0. 


7 




0. 


8 


0. 


9 


0. 


8 




0. 


9 


0. 


8 


0. 


9 




0. 


8 


0. 


7 


0. 


9 




0. 


7 


0. 


9 


0. 


8 




0. 


8 


0. 


7 


0. 


8 




0. 


9 


1 . 


0 


0. 


7 




1. 


0 


0. 


8 


0. 


9 



[0027] The use test was performed using 20 female 1 groups which worry about dullness using the face 
toilet of the [example 9] example 1. That is, I had face toilet of a specimen applied for evening bis die 
two months in the morning, and had the improvement of dullness answer by the questionnaire. The 
comparison group 1 used that to which the comparison group 2 permuted the heterogeneity 
improvement agent 1 of the skin of an example 1 by the ascorbic acid using what permuted the 
heterogeneity improvement agent 1 of the skin of an example 1 by hyaluronate sodium using that to 
which the control group permuted the heterogeneity improvement agent 1 of the skin of an example 1 by 
water. A result is shown in Table 2. This shows that the cosmetics of this invention are excellent in an 
improvement operation of dullness. 
[0028] 
[Table 2] 



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JFK 


SB It 


mmmi 


9 


6 


5 








5 


1 


5 


9 




th«gf 1 


6 


2 


4 


8 




itnm2 


7 


3 


2 


8 





[0029] 

[Effect of the Invention] According to this invention, the material which improves the heterogeneity of 
the skin and improves dullness can be offered. 



[Translation done.] 



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