JP2006219448A - External preparation for skin for acne - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a safer and effective preparation for acne by effectively utilizing an extract of Conyza filaginoides having high effectiveness. <P>SOLUTION: The present inventors found that the extract of Conyza filaginoides significantly inhibits production of lipase. As a result, effective various external preparations inhibiting formation of acne are provided by using the extract of Conyza filaginoides. Further, present inventors found that various troubles of skin such as dullness of skin and chapped skin are further improved by combining and formulating the extract of Conyza filaginoides with specific agents selected from a humectant, a cell-activating agent, an antiinflammatory agent, an antioxidant, a beautifying and whitening agent, an antiplasmin agent, an active oxygen inhibitor and an antihistamic agent. <P>COPYRIGHT: (C)2006,JPO&NCIPI

Description

The product of the present invention is an extract extracted from a plant of a specific genus, which suppresses lipase production in the skin epidermis tissue, thereby suppressing acne formation, and a moisturizer, cell activator, anti-inflammatory agent Further, the present invention relates to an external preparation for skin which improves various skin problems such as dull skin and rough skin by combining and combining the specified agents of antioxidants, whitening agents, antiplasmin agents, active oxygen inhibitors and antihistamines.

Simonylo (Conyza filaginoides) is a plant belonging to the family Asteraceae that is used as a herbal medicine in Mexican plants and is known as a raw material for cosmetics. (See Patent Document 1)

Acne is an inflammatory disease of the follicular gland system that occurs in areas with many sebaceous glands such as the face and back, and is mainly caused by three factors: endocrine factor, keratinization factor of hair funnel, and bacterial factor. Can be mentioned. P. acnes, which is deeply involved in acne pathology, is a resident skin resident in healthy human skin and produces bacterial lipase. The produced lipase breaks down triglycerides in sebum to produce free fatty acids, which not only march and form comed but also cause acne inflammation. Furthermore, oleic acid, the main component of the free fatty acid produced, promotes the growth of P. acnes.
JP 2001-048739 A

The object of the present invention has been variously studied in order to make effective use of highly effective extract of Simnillo. There has also been a demand for safer and more effective preparations for acne.

  In order to achieve the above-mentioned object, the present inventors have intensively studied and found that lipase production is preferentially suppressed. Furthermore, by blending specific drugs (humectants, cell activators, anti-inflammatory agents, antioxidants, whitening agents, antiplasmin agents, active oxygen inhibitors, antihistamines, etc.), wrinkles, dullness, rough skin, etc. It has been found to improve various skin problems.

  The form of the extract of Simonil is not limited in any way, but preferably, the Simnillo (whole plant) is shade-dried, ground and then soaked for 3 days with an extraction solvent (for example, alcohol such as ethanol, water or a mixture thereof) Use the solution heated, cooled and filtered at 100 degrees for 2 hours.

Test example: Lipase inhibition test Substrate Pentanoic acid 4-nitrophenyl eater is hydrolyzed by enzyme lipase, and lipase inhibition test measures the absorption of 4-nitrophenyl ester produced. Examined. Add 500 μl of the same buffer solution 3 ml, 2 mg / ml lipase [SIGMA] enzyme-50 mM Tris buffer solution (pH 7.7) 500 μl to 500 μl of the test product prepared with 0.04% olefin sulfonic acid-50 mM Tris buffer solution (pH 7.7), and stir Thereafter, it was incubated at 40 ° C. for 5 minutes. Further, 1 ml of 1 mM PNP-valerate was added, stirred and incubated at 40 ° C. for 15 minutes, and then the absorbance (A) was measured at Abs. 425 nm. Similarly, Absorbance (B) when buffer is used as an alternative to enzyme solution, Absorbance (C) when buffer is used as alternative to test product, Buffer solution is used instead of enzyme solution, and Test product is used instead The absorbance (D) when a buffer solution was used was measured, and the lipase activity inhibition rate (%) was calculated from the following formula.
Lipase activity inhibition rate (%) = [1- (AB) / (CD)] × 100
○ Test items are shown below,
Shimoniro E: Shimoniro (whole plant) (100g) ethanol (300ml) extract (lyophilized)
Shimoniro EW: Shimoniro (whole plant) (100g) 50% ethanol-water (300ml) extract (lyophilized)
Shimoniro W: Shimoniro (whole plant) (100g) hot water (300ml) extract (freeze-dried)
The working concentration was 0.10%. The test results are shown in Table 1.

  Since the extract of Simonylo (Conyza filaginoides) exerts its effects and the like sufficiently when blended at 0.001 to 10% by weight, it is desirable to blend at this concentration.

In addition, wrinkles, stains and freckles can be obtained by adding specific agents (humectants, cell activators, anti-inflammatory agents, antioxidants, whitening agents, antiplasmin agents, active oxygen inhibitors, antihistamines, etc.) to the extract of Similillo. It was found to improve various skin problems such as dullness and rough skin.
Listed in particular are the whole plant of morning glory, Asam wood, Adhatoda vasica wood, Yellow Merchant wood, Ixcate (Hippocratea celastroides) bark, Ibonashi ヅ rafu branch, Indian salsa root, bark of neem, Woodfordia fruticosa flowers and leaves, lumberwood, lagerstroemia speciosa leaves, CASCA-DOCE (CASCA-DOCE) (scientific name Pradosia lactescens or Lucumaglyciphloea Or Chrysophyllum buranhem), wig, kapool, stems and branches of the burdock, genus Kawaraketsume (Kemeko, Senna, Wangjiang South, mountain pea, Nanbansaikachi), whole spinach, cinnamon blossom, Cuachalalate (Cuachalalate) Juliania adstringens Schl) bark, guava leaf, Quercus pidankrate Quercus pedunculate fruit, cumin seeds, cubraco heartwood, coustigaya rhizome, costillas (Acalypha diversifolia Jacq.) Trunk and branch, bark of melanoleuca leucadendron, Gordolobo (Gnaphalium) sphacellatum), saffron pistil, Saraka indica bark, JEQUITIBA (Carinianabrasiliensis or Couratari legalis or Pyxidaria macrocarpa) bark, Jatoba (JATOBA) (Hymenaea coubaril) bark, nia jambolana bark, white-spotted seed, Sphaeranthus indicus whole plant, Spruce bark, Smilax zeylanica root, scepter wood, tablin bark, tea planta root, desmodium Termina, the whole plant of Desmodium gangeticm Fruit of Terminalia horrida, whole plant of Tragia involucrata, seed of Nigella sativa, whole plant of Habibishi, whole plant of Hierba del sapo (Eryngium comosum), root of hijatu, Pirul ) (Schinus molle), Phyllanthus nuriri, Fusenkazura, PUCA (Cissus antiparaliticus), Vetiver root, Hedesalum austrosibiricus Roots, Herpestris monnies whole plant, VERONICA (Veronica officinalis) bark, Borrelia hispida root and stem, Pongamia glabra root, Mizuki bark, Mizusop bark (Mimusops elengi), Muraya Koenigii shoots, Munronia pumila, Memories Pea wood, magnoliaceae bark, bark wood, lambo wood, Rumex cyprius leaf, wattle bark, Ai Tamago, Ichione root, indeterminate, fossil grass, shell mother, perforated People, Iwabenkei roots, Paeonia anomala roots, chestnuts, chestnut leaves, chicken blood wisteria, Saya, messenger, small gold crab, crust, spicy, Saiheyanagi, Ishirenko, Ishigane root bark, stone persimmon skin, Ishiki bark, Senzaku grass, Blasting stone, Agate, Valley essence, Chinese white camellia, Iron wrapping, Winter coconut tree, Kashiwa leaf, Hishimi, Kashio grass, Ryo Wang, Lotus leaf, Zushi, Akatsuki Seawater of the ocean, toothpick, coconut tree, Saito, potato infestation, scallops; pearl powder, conchiolin, conchiolin hydrolyzate, conquiolin hydrolyzate treated with succinic anhydride, hydrolyze shellfish mucus Substances obtained from shellfish, sterols obtained from shellfish meat, acidic polysaccharides obtained from shellfish meat, obtained from shellfish meat Collagen, glycogen obtained from shellfish meat, phospholipid obtained from shellfish meat, deoxyribonucleic acid obtained from shellfish meat, thiosalicylic acid and its salt, magnolol, honokiol, 1- (4-hydroxyphenythio) 2-propanol, 2- (4-hydroxyphenyl) -1,3-dithiane, 2- (4-acetoxyphenyl) -1,3-dithiane, 2,5-dihydroxybenzamide, 2,6-dihydroxybenzamide, 4 -Aminophenol, 4-hydroxythiophenol, 4-hydroxybenzamide, 5-hydroxyindole, 6-dihydroxy) -dihydrobenzofuran-3-yl- (3'4'-dihydroxy) -phenyl ketone, stilbengaloyl glycoside, Citracin C, ethylenediamine derivatives, carahanaenone derivatives, cashew nut shell liquid, cardanol, cardo , Anacardic acid, sennoside, α-arbutin, peptide containing the sequence of Glu-Glu-Met-Gln-Arg-Arg, or the carboxyl group terminal of this peptide is converted to an amide or / and the amino group terminal is acylated Peptides converted into are mentioned.
Examples of ethylenediamine derivatives include N-phenyl-N- (2,3,3 trimethyl-1-cyclopentene-1-ethyl) -N ′, N′-dimethylethanediamine, N-2-pyridyl-N- (3 , 7-Dimethyl-6-octen-1-yl) -N ', N'-dimethylethanediamine, N-2-pyridyl-N- (2-pinen-10-yl) -N', N'-dimethylethane Mention may be made of diamines, N-2-pyridyl-N- (1,8-p-menthadien-7-yl) -N ', N'-dimethylethanediamine.
For example, N-p-hydroxyphenyl-3,3,6-trimethyl-5-cycloheptan-2-one-1-carboxamide, 2-hydroxy-Np-hydroxyphenyl-3,3 , 6-trimethyl-5-cycloheptene-1-carboxamide. Examples of stilbene galloyl glycosides include 3,5,4'-trihydroxystilbene 4'-0-β-D- (6 "galloyl) glucopyranoside, 3,5,4'-trihydroxystilbene 4'- Mention may be made of 0-β-D- (2 ″ galloyl) glucopyranoside.

Furthermore, it has also been found that the effect can be further obtained by blending one or more of polyhydric alcohols containing two or more hydroxyl groups, lower alcohols, surfactants, and low molecular betaines.

  The polyhydric alcohol that can be used is not particularly limited, and examples thereof include glycerin, 1,3 butylene glycol, propylene glycol, isoprene glycol, sorbitol, trehalose, maltose and the like. These are blended in an amount of 0.1 to 80% by weight, preferably 1 to 30% by weight. Needless to say, the blending amount varies depending on the type of polyhydric alcohol, and a plurality of polyhydric alcohols can be used.

Absorbability improves by mix | blending a lower alcohol. Although there are various kinds of lower alcohols, ethanol is usually used. The blending amount is not particularly limited but is preferably 2 to 70% by weight.
It is also effective to combine a surfactant with a combination of polyhydric alcohols containing an extract of Simnillo, and it is also effective to combine the lower alcohol.
There is no particular limitation on the surfactant, and the type and amount may be selected depending on the application and dosage form.
Surfactants are used for emulsification and solubilization of oils, etc., and are anionic (alkyl carboxylates, alkyl sulfonates, alkyl sulfate esters, alkyl phosphate esters), nonionic (ether type) Nonionic surfactant, ether ester type nonionic surfactant, ester type nonionic surfactant, block polymer type nonionic surfactant, nitrogen-containing type nonionic surfactant) and amphoteric (carboxylic acid type amphoteric surfactant) Agents (amino type, betaine type), sulfate ester type amphoteric surfactant, sulfonic acid type amphoteric surfactant, phosphate ester type amphoteric surfactant) and other surfactants (natural surfactants, protein hydrolysates) Derivatives, polymer surfactants, surfactants containing titanium and silicon, and fluorocarbon surfactants) can be used as appropriate.

Low molecular weight betaine is also one of the raw materials to be selected, and by blending this, the effect is further improved and the feeling of application is improved, and the effectiveness as an external preparation for skin is increased.
Low molecular weight betaines that can be utilized may include those that form zwitterions with internal salts such as quaternary ammonium bases, sulfonium bases, phosphonium bases and the like having a molecular weight of 200 or less. Examples include trimethylglycine, N, N, N-trimethylalanine, N, N, N-trimethylglutamic acid, triethylglycine, and the like, with trimethylglycine being preferred.
Those having a molecular weight of 200 or more have a surface-active ability, which is different from the effect of low molecular betaine. As described above, the use of a surfactant enhances the effect of the present invention, but the effect of low molecular betaine is Is different.

  The external preparation for skin of the present invention can be prepared by blending with various forms of base materials known as normal external preparations for skin according to conventional methods.

It does not specifically limit as a form of an external preparation, For example, arbitrary dosage forms, such as a milky lotion, cream, aqueous solution, a pack, can be selected.

In the external preparation for skin of the present invention, in addition to the above-mentioned essential components, components that are blended in normal external preparations, such as oils, powders, purified water, polymer compounds, gelling agents, UV absorbers, UV scattering Agents, antioxidants, pigments, preservatives, fragrances, and cosmetic ingredients can be appropriately selected and used within a range not impairing the effects of the present invention.

EXAMPLES Next, although an Example and a comparative example are given and this invention is demonstrated still in detail, this invention is not restrict | limited at all to these. Moreover, the extraction method about the extract of the used chemical | medical agent is not limited at all.
Tables 2 to 4 show the formulations of Examples and Comparative Examples. The preparation method was performed by a conventional method. Table 2 shows the lotion, Table 3 shows the serum, and Table 4 shows the cream. The amount is shown in parts by weight.

(Note 1) Simmonillo extract 1 was prepared by adding 200 ml of purified water to 10 g of Simoniro (whole herb dried product) and boiling for 1 hour, and then using the filtered extract.
(Note 2) Simmonillo extract 2 was prepared by adding 100 ml of purified water and 100 ml of ethanol to 10 g of Simoniro (whole plant dried product) and stirring for 3 days, and then using the filtered extract.
(Note 3) Simmoniro extract 3 was obtained by adding 200 ml of ethanol to 10 g of Simmoniro (whole plant dried product) and stirring for 3 days, and then using the filtered extract.

(Note 4) The hydrolyzed conchiolin solution used was a hydrolyzed conchyolin that had a molecular weight of 1000 or less.
(Note 5) As the tablinus extract, a Matils extract [manufactured by Maruzen Pharmaceutical Co., Ltd.] was used.
(Note 6) Falco Rex Honoki E [Ichimaru Falcos Co., Ltd.] was used as the honoki extract.
(Note 7) As the guava extract, 300 ml of ethanol was added to 10 g of guava leaves and allowed to stand for 5 days, and then the filtered extract was used.
(Note 8) Nishi-Haruyanagi extract used Nishi-Haruyanagi extract [Nippon Seika Co., Ltd.].
(Note 9) Marine purge [manufactured by Ichimaru Falcos Co., Ltd.] was used as the seaweed extract.
(Note 10) As the acacia bark extract, 300 ml of ethanol was added to 10 g of bark and left for 5 days, and then the filtered extract was used.
(Note 11) The Murayako Engii extract used was the Murayako Engii extract [Yamakawa Trading Co., Ltd.].
(Note 12) As for the extract of the giant crape myrtle, the extract of the giant crape myrtle (produced by Yamakawa Trading Co., Ltd.) was used.

The effect test of the Example of Table 2-Table 4, and a comparative example was implemented. The test method consisted of 20 females aged 18 to 25 years as a panel, and an appropriate amount of a topical preparation was applied to the face after washing the face twice a morning and night for 12 weeks. Table 5 shows the results of acne improvement effect by application.

Claims (5)

A topical skin preparation for acne characterized by containing an extract of Simonylo (Conyza filaginoides) Lipase inhibitor characterized by containing an extract of Simonylo (Conyza filaginoides) Skin external application containing one or more of extract of momillo (Conyza filaginoides), moisturizer, cell activator, anti-inflammatory agent, antioxidant, whitening agent, antiplasmin agent, active oxygen inhibitor, antihistamine Agent Moisturizers, cell activators, anti-inflammatory agents, anti-oxidants, whitening agents, anti-plasmin agents, active oxygen suppressors, anti-histamine agents are whole grasses of Asagakarakakusa, materials of Asam, materials of Adhatoda vasica, materials of yellow ume Lunch lumber Ixcate (Hippocratea celastroides) bark, Ibonashi ヅ rafuji branch, Indian salsa root, Neem bark, Woodfordia fruticosa flower and leaf, Woodpecker lumber lagerstroemia speciosa) leaves, CASCA-DOCE (scientific names Pradosia lactescens or Lucumaglyciphloea or Chrysophyllum buranhem) Peas, peanuts, whole spinach, cinnabar flower, Cuachalalat e) bark of (Juliania adstringens Schl), guava leaves, berries of Quercus pedunculate, seeds of cumin, heartwood of quebraco, rhizomes of Coustigaya (Costillas) (Acalypha diversifolia Jacq.), trunks and branches, Bark of black-breasted tree (Melaleuca leucadendron), whole plant of Gordolobo (Gnaphalium sphacellatum), bark of saffron, bark of Saraka indica (JEQUITIBA) (Carinianabrasiliensis macrocarpaxarial or Carpayarisma) Bark, JATOBA (Hymenaea coubaril) bark, Eugenia jambolana bark, white-spotted seed, Sphaeranthus indicus whole grass, Spruce bark, Smilax zeylanica (Smilax zeylanica) Root, scepter material, tablin bark, chabaco Show root, whole plant of Desmodium gangeticm, fruit of Terminalia horrida, whole plant of Tragia involucrata, whole plant of Nigella sativa, whole plant of Hamabishi, Hierba del sapo (Hierba del sapo) Eryngium comosum whole plant, chickpea root, Pirul (Schinus molle) whole plant, Phyllanthus nuriri whole plant, Fusenkazura whole plant, PUCA (Cissus antiparaliticus) fruit, Vetiver root, Hedysarum austrosibiricus root, Herpestris monnies whole grass, VERONICA (Veronica officinalis) bark, Borrelia hispida root and stem, Pongamia glabra ) Roots, dogwood bark, earthworm bark, Mimusops elengi Nohana), Murraya koenigii stalks, Munronia pumila, melapie, magnolia bark, wild cherry, lumbo, Rumex cyprius leaves, Watle's bark, Ai Tamago, Ichikone, Wang-no-Moto, Fossil grass, Shellfish mother, Invasion, Iwabenkei root, Paeonia anomala root, Chestnut, Chestnut leaf, Chicken blood wisteria, Saya, Ambassador , Small gold cocoon, husk, bonito, saikawa willow, stone lotus, sarcophagus bark, sarcophagus bark, sarcophagus bark, sanctuary, pierced stone, coral, valley essence, Chinese white birch, iron wrapping, winter lion, Kashiwa, Hishimi, Kashiwaso, Ryoo, Lotus leaves, Yuzu, Kashiwa Oumi, Kashiwa, Kashiwa, Saito, Kakinohyakusa, Ishigeae seaweed, pearl powder, conchiolin, conchiolin water Hydrolyzate of hydrolyzate, hydrolyzate of conchiolin with succinic anhydride, and slime of shellfish Substances, sterols obtained from shellfish meat, acidic polysaccharides obtained from shellfish meat, collagen obtained from shellfish meat, glycogen obtained from shellfish meat, phospholipids obtained from shellfish meat, obtained from shellfish meat Deoxyribonucleic acid, thiosalicylic acid and its salt, magnolol, honokiol, 1- (4-hydroxyphenthio) -2-propanol, 2- (4-hydroxyphenyl) -1,3-dithiane, 2- (4 -Acetoxyphenyl) -1,3-dithiane, 2,5-dihydroxybenzamide, 2,6-dihydroxybenzamide, 4-aminophenol, 4-hydroxythiophenol, 4-hydroxybenzamide, 5-hydroxyindole, 6-dihydroxy) -dihydrobenzofuran-3-yl- (3'4'-dihydroxy) -phenyl ketone, stilbengaloyl glycoside, citracin C Peptide containing the sequence of ethylenediamine derivative, carahanaenone, cashew nut shell liquid, cardanol, cardol, anacardic acid, sennoside, α-arbutin, Glu-Glu-Met-Gln-Arg-Arg or the carboxyl group terminal of this peptide in the amide form A skin external preparation comprising the peptide of claim 3, wherein the peptide is a peptide having an amino group terminal and / or an amino group terminal converted to an acylated form. Furthermore, the skin external preparation of Claim 3 thru | or 4 which contains any 1 type, or 2 or more types of the polyhydric alcohol containing two or more hydroxyl groups, a lower alcohol, surfactant, and low molecular betaine.