JP2001064145A - Composition for external use - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a composition for external use applicable to various fields such as medicines, quasi-drugs and cosmetics and having high safety and further protecting actions on biotissues against injury and activating actions on the biotissues. SOLUTION: This composition for external use contains one or more species of plants selected from the group consisting of plants of the genera Xylopia, Caryocar, Guazuma, Cuphea, Heteropteris, Sciadotenia, Ampelozizyphus, Luehea, Juglans and Lippia or extracts thereof. The composition for external use is stable and excellent in prophylactic or ameliorating effects on biological hypofunction caused by environmental stress or aging, especially hypofunction of skin, hair and tissues in an oral cavity. Thereby, the composition has an extremely wide application range.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to the reduction of biological functions caused by environmental stress and aging,
The present invention relates to a composition for external use having a high effect of preventing or improving the function of hair and oral tissues.

[0002]

BACKGROUND OF THE INVENTION Generally,
BACKGROUND ART Biological tissues such as skin, hair, and oral cavity can rapidly improve functional deterioration and structural changes caused by various factors due to metabolism. However,
Injuries accumulate in living tissues due to excessive exposure to aging, such as ultraviolet rays, dryness and harmful chemical substances, thereby impairing the original function and causing various troubles. Skin suffers from spots, wrinkles, rough skin, and atopic symptoms. In hair, it causes hair loss, thin hair, gray hair, and the like. In the oral field, they show pathological conditions such as gingival regression and bleeding from the gums. In this way, for living tissues that show functional and structural deterioration, the generation of reactive oxygen species and the chronic inflammation that cause functional deterioration are prevented, and living tissues with reduced functions are activated by reactivating the tissues themselves. A method of repairing and regenerating to healthy tissue is being considered.

[0003] In order to prevent the generation of reactive oxygen species, vitamins and various plant extracts have been proposed to eliminate singlet oxygen, which is one of the reactive oxygen species that damages living tissues. JP-A-7-133216). Further, as a substance for suppressing chronic inflammation and allergic reaction, a substance having a hyaluronidase inhibitory activity has been actively searched for, and some seaweeds and plant components have been found (JP-A-8-53360). No.). As a means to activate the tissue itself, many methods have been shown to increase the collagen synthesis ability of skin tissue and gingival tissue,
A method using an extract of a bacterium or a plant, or an amino acid composition (Japanese Patent Application Laid-Open No. 7-194375) has been proposed.

[0004] However, it seems that all of these methods require the use of a limited amount in terms of safety, are insufficient in action and effect, and are difficult to stably compound in a preparation while maintaining the activity. Problems remain.

The present invention has been made in view of the above circumstances, and can be applied to various fields such as pharmaceuticals, quasi-drugs, and cosmetics, has high safety, and has an excellent injury protection action and activation action for living tissues. It is intended to provide a composition for external use having the same.

[0006]

Means for Solving the Problems and Embodiments of the Invention The present inventors have conducted intensive studies on the excellent injury protective action and activation action of natural products on living tissues.
Xylopia genus plant, Butternut tree (Caryocar) genus plant, Guazuma (Guazu)
ma) genus plant, Cuphea genus plant, Heteropteris genus plant, Sciadotenia genus plant, Ampelodizifusus genus plant, Luhea genus plant, Walnut (Jug)
It has been found that a plant belonging to the genus lans, a plant belonging to the genus Lippia, or an extract thereof has an excellent injury-protecting effect and an activating effect on living tissue, and the present invention has been completed.

Accordingly, the present invention provides an external composition containing one or more of the above-mentioned plants or their extracts. The composition for external use of the present invention has an excellent injury-protecting action and an activating action on skin / hair tissue and oral tissues, and has high safety, and is suitably used for pharmaceuticals, quasi-drugs, cosmetics, and the like. Can be.

Hereinafter, the present invention will be described in more detail.
The plant of the genus Xylopia used in the present invention is used as a seasoning, carminative, stomachic, etc. in tropical America, and among them, the local name Invieiro: Im
biero (Xylopia benthami)
i), Pindiva de Folia Pequena: Pi
ndaiba-de-folha-pequena
(X. brasiliensis), Pindiva-Vermelha: Pindaiba-vermelha
(X. carminative), core gel coo: C
Oagerucu (X. flutescens) has an excellent action and is particularly desirable. Butternut tree (Ca
Ryocar) plants are used in tropical and Central and South America for purposes such as astringency, bronchial disease, and diarrhea control. Among them, the local name Piqui (Caryocar brass) is used.
liense), Pichia: Piqia (C.co.)
riaceum), Pichiarana-da-terra-fir
me (C. glabrum), Pichia-Verdadeiro (P.
losum) has an excellent action and is particularly desirable. Guazuma genus plants are used as decoctions in tropical America for syphilis, liver disease, skin disease and wound medicine. The bark syrup is used for respiratory diseases, cough, asthma, pneumonia, etc., and among them, the local name Mutamba: Mutamba
(Guazuma ulmifolia) has an excellent effect, and is particularly desirable. BACKGROUND ART Plants of the genus Cuphea have a blood purifying action mainly as a tea agent in tropical America, and are used for antipyresis, sweating, diuresis, and the like. Among them, the local name Sete-Sangrias: Sete-sangria
s (Cuphe antisyphilitic
a), Balsamona: Balsamona (C. cart
hagenensis), Mota Cana: Meta-ca
na (C. ingrata) has an excellent effect, and is particularly desirable. Heteropteris
s) The genus plant is used as a tea or decoction for tonicity, aphrodisiac, etc. in South America.
Cashilo: No-de-cacharo (Heté
ropteris aphrodisiaa), Marapuama: H. campestri
s), Poia-mineir
a (H. pragua), Sarabatsk: Saraba
tucu (H.suberosa), pluger: Pr
agua (H. syrungiforia) has an excellent effect and is particularly desirable. Skiadtenia
otenia) plants are tonic as a tea in Brazil,
It is used as a stimulant and, among others, the local name Sipo-amargoso (Sciadoten)
ia candicans), Abuta: Abuta
(S. paraensis), which is particularly desirable. Ampelodizys
Phus) plants are used in Brazil as tonic, antipyretic and anti-inflammation agents, with the local name Sarakula Muiler:
Saracura-muira (Amperozizy
phas amazonicus has an excellent effect and is particularly desirable. Luheea plants are used in South America for arthritis and rheumatism in the skin, and leaves and flowers are used as a tea or decoction for astringency and blood stasis. Among them, Asoita-cabaro:
alo (Luehea divaricata), Ivitinga: Ivintinga (L. grandifl)
ora) has an excellent effect and is particularly desirable. The walnut (Juglans) genus plant is used for food in Asia and North and South America, and in particular, the local name Nogueira (Juglans regi) in South America.
a) has an excellent effect and is particularly desirable. Plants belonging to the genus Lippia are used in tropical America for aroma, sedation, disinfection, rheumatism, etc., and among them, the local name Erva-cidreira (L)
ipia alba), Alecrin Pimenta: Al
ecrim-pimenta (L. alnifoli
a), Alecrim-d-Chappada: Alecrim-d
a-chapada (L. gracilis), Alecrim-do-campo: Alecrim-do-campo
(L. microphylla), Capitón de mat: Capitao-do-mat (L. pseudo
o-thea), Estrepa Cavallo: Estrep
It has an excellent effect on a-cavalo (L. sideoids) and is desirable.

As the above-mentioned plant group, xylem, heartwood, bark, stem, branch, leaf, root, seed, fruit, flower and the like can be used.

[0010] The plant extract may be an extract extract or a product separated and purified from the extract. In the case of an extract extract, the plant can be obtained by solvent extraction of a dried or crushed plant,
If the extraction solvent is non-toxic for use, the extract may be used as it is, or may be used as a diluent diluted with an appropriate solvent, or as a concentrated extract, or as a dry powder by freeze-drying, or paste. And the like prepared in a state can be used.

Examples of the solvent used to obtain the above plant extract include commonly used organic solvents such as methanol, ethanol, butanol, hexane, heptane, cyclohexane, ethyl acetate, acetone and the like, and water. One of these can be used alone, or two or more can be used as a mixture. Among these solvents, methanol, ethanol and water are particularly preferred. In addition, the extraction treatment can be performed by a conventional method at a temperature of usually about 3 to 70 ° C.

In addition to the solvent extraction, an extract obtained by supercritical extraction in which carbon dioxide is brought into a supercritical state can be similarly used. At this time, hexane, ethanol, or the like can be used as an extraction aid. Separation and purification of the active ingredient from the extract can be performed by purifying the extract by column chromatography, liquid chromatography, or the like.

The composition for external use of the present invention contains one or more of the above plants or extracts thereof as an active ingredient. The compounding amount is an effective amount and is appropriately selected depending on the use of the composition, the dosage form, and the like.
It is preferred to mix 0001 to 20% by weight. Preferably, the content is 0.0001 to 10% by weight. If the compounding amount is less than 0.00001% by weight, the effects of the present invention cannot be exerted, and production may become difficult depending on the dosage form. Therefore, it is better not to exceed 20% by weight.

The composition for external use of the present invention is applied to skin, mucous membrane for oral cavity, hair, etc., for example, cream, hand cream, milky lotion, lotion, soap, hand soap, body soap, antiperspirant , Athlete's foot medicine, acne treatment,
As a skin external preparation such as a hand disinfectant, a whitening agent, a patch, or a skin cosmetic, a hair cosmetic such as a shampoo, a rinse, a tonic, a hair restorer, an oral composition such as a toothpaste, a mouthwash, and a gum massage cream. Can be prepared.

In this case, the composition for external use of the present invention can be prepared by a conventional method using known components according to the type, dosage form and the like of the composition for external use. Incidentally, the composition of the present invention,
In addition to the above-mentioned active ingredients, commonly used cell activators, for example, crude drug extracts such as hormones, vitamins and saponins, placenta extracts, plant lectins and the like can be used.

[0016]

The composition for external use of the present invention is stable and has a reduced biological function caused by environmental stress and aging.
In particular, it has an excellent effect of preventing or improving the function of skin, hair, and oral tissues, and thus has a very wide range of application.

[0017]

EXAMPLES The present invention will be specifically described below with reference to Preparation Examples, Experimental Examples and Examples, but the present invention is not limited to the following Examples.

[Preparation Example 1] Xylopia
a) Extraction of plants of the genus Plant Invieiro: Imbieiro (Xylopia b
enthamii) 10 kg of 7 kg of crushed fruit
0% ethanol was added and extracted for 2 days. After the extract was filtered, ethanol was distilled off under reduced pressure, and the extract 102
g was obtained. Also, Pindiva-de-folha-pequ
ena (X. brasiliensis), Pindiva Vermelha: Pindaiba-vermel
ha (X. carminative), Coagerucu: Xagefrutescens
10 L of methanol was added to 1 kg of each crushed fruit, and extracted for 2 days. After filtering the extract, methanol was distilled off under reduced pressure, and 96 g of each extract was extracted.
11 g and 106 g were obtained.

[Preparation Example 2] Butternut tree (Cary)
ocar) Extraction of plants of the genus Pici: Piqui (Caryocar brasil)
iense) and Pichiarana da Terra Filme: P
equianana-da-terra-film
1k of each crushed fruit of (C. glabrum)
10 g of methanol was added to g, and the mixture was extracted at room temperature for 2 days. After filtering the extract, methanol was distilled off under reduced pressure.
114 g and 101 g of the extract were obtained. Also, Pichia: Piqia (C. coliaceum), Pichia Verdadeiro: Piqia-verdadei
ro (C. illussum) from each 1 kg of the crushed fruit, by supercritical extraction, 123 g, 1
42 g of extract were obtained.

[Preparation Example 3] Guazuma
Extraction of genus plants Mutamba: Mutamba (Guazuma ulmi)
10 liters of 9 per kg of crushed bark and leaf of folia)
5% ethanol was added, and the mixture was extracted at room temperature for 2 days. After the extract was filtered, ethanol was distilled off under reduced pressure to obtain 95 g of an extract.

[Preparation Example 4] Tobacco Saw (Cuphea)
Extraction of genus plants Sete-sangrias: Sete-sangrias
(Cuphe antisyphilitica) and balsamona: Balsamona (C. carthag)
enensis) and Mota Cana: Meta-cana
10 L of 95% ethanol was added to 1 kg of the crushed tree and leaf of (C. ingrata), and extracted at room temperature for 2 days. After filtering the extract, ethanol was distilled off under reduced pressure to obtain 102 g, 87 g and 96 g of the extract.

[Preparation Example 5] Heteropteris (Heter
opteris) Extraction of plants of the genus No-de-cachoro
(Heteropteris aphrodisiac
a), Murapuama: Marapuama (H.camp)
estris), Poia Minera: Poia-m
ineira (H. Pragua), Sarabatsk: S
arabatucu (H.suberosa) and pluger: Pragua (H. syrungiforia)
, 10 L of 95% ethanol was added to 1 kg of the ground material, and the mixture was extracted at room temperature for 2 days. After the extract was filtered, ethanol was distilled off under reduced pressure, and 99 g of the extract was extracted.
10 g, 90 g, 75 g and 81 g were obtained.

[Preparation Example 6] Sciad tenia (Sciad)
otenia) Extraction of plants of the genus Sipo-Amargoso: Cipo-amargoso
10 kg of 70% ethanol was added to 1 kg of the ground and stem pulps of (Siadotenia candicans) and Abuta: Abuta (S. paraensis), and extracted at room temperature for 2 days. After the extract was filtered, ethanol was distilled off under reduced pressure, and 108 g of extract was obtained.
132 g were obtained.

[Preparation Example 7] Amperodisifus (Ampe
Extraction of plants of the genus lozizyfus) Saracula-muira
(Ampelozizyphus amazonicu
s) of 10 l of 9 g of ground pulverized root and leaf
5% ethanol was added, and the mixture was extracted at room temperature for 2 days. After filtering the extract, ethanol was distilled off under reduced pressure to obtain 103 g and 80 g of the extract.

[Preparation Example 8] Extraction of plants belonging to the genus Luhea Asoita-cavalo (L
uehea divaricata) and Ivitinga:
10 L of 95% ethanol was added to 1 kg of each crushed root and leaf of Ivintinga (L. grandiflora) and extracted at room temperature for 2 days. After the extract was filtered, ethanol was distilled off under reduced pressure to obtain an extract 106.
g and 87 g were obtained.

[Preparation Example 9] Extraction of plants of the genus Walnut (Juglans) Nogueira (Juglans reg)
1 kg of the bark pulverized product of ia) was subjected to supercritical extraction to obtain 72 g of an extracted extract.

[Preparation Example 10]
a) Extraction of genus plants Erva-cidreira: Erva-cidreira
(Lippia alba), Alecrin Pimenta:
Alecrim-pimenta (L. alnifol
ia), Alecrin da Chapada: Alecrim-
da-chapada (L. gracilis), Alecrim-do-campo: Alecrim-do-camp
o (L. microphylla), Capitan de Matt: Capitao-do-mat (L. pseudo
do-thea) and Estrepa Cavallo: Estre
10 L of 95% ethanol was added to 1 kg of each pulverized root of pa-cavalo (L. sideoids) and extracted at room temperature for 2 days. After the extract was filtered, ethanol was distilled off under reduced pressure, and 80 g, 104 g of the extracted extract,
89 g, 110 g, 95 g and 81 g were obtained.

[Experimental Example 1] Using the extract of each plant obtained according to the Preparation Example, the following method was used to evaluate the ability to scavenge singlet oxygen that damages living tissues. Table 1 shows the results. Method: Singlet oxygen was generated by irradiating Rose Bengal (Wako Pure Chemical Industries, Ltd.) with a fluorescent lamp, and the singlet oxygen scavenging ability was measured using the degree of oxidation of squalene as an index. A solution was prepared by adding an appropriate amount of the sample and methanol so as to obtain 3 mM squalene and 25 μM rose bengal. Control only received methanol. 4
Irradiated with fluorescent light at 18 ° C. for 18 hours. A blank with an irradiation time of 0 hours was used as a blank. The resulting squalene peroxide was quantified by the TBA method. 1,1,3,3-tetraethoxypropane (Wako Pure Chemical Industries, Ltd.) was used as a standard substance. 1m
2 ml of TBA reagent (0.375% thiobarbitolic acid, 15% trichloroacetic acid, 0.04% butylhydroxytoluene, 2% ethanol, 0.25N hydrochloric acid)
After stirring, the mixture was heated on a boiling water bath for 1 hour. After cooling with ice and cooling to room temperature, the mixture was extracted with butanol, and the absorbance at 535 nm was measured using a blank as a control. The degree of singlet oxygen scavenging ability is represented by a relative value when the TBA value of the control is set to 100, and 90% or more is represented by ◎, 60 to 89.
% Is represented by ○, 30 to 59% by Δ, and less than 30% by X.

[0029]

[Table 1]

As is clear from the results in Table 1, the high singlet oxygen scavenging ability of each plant extract was proved.

[Experimental Example 2] Using the extract of each plant obtained according to the Preparation Example, the inhibitory activity of hyaluronidase involved in the development of inflammation and allergy was evaluated by the following method. Table 2 shows the results. Method: Enzyme (type IV-S from Bovi)
ne testis, SIGMA) 100 μl solution
(4,000 units / ml), 200 μl of each extract extract sample obtained in the above Preparation Example was added, and incubated at 37 ° C. for 20 minutes. Next, an enzyme activator (Compou)
nd 48/80, manufactured by SIGMA) solution (0.1 mg
/ Ml) and incubated at 37 ° C. for 20 minutes, followed by potassium hyaluronate (fr) as a substrate.
om rooster comb, Wako Pure Chemical Industries, Ltd.) solution (0.4 mg / ml) at 37 ° C.
Incubated for minutes.

Then, a 0.4 M sodium hydroxide solution 2
After adding 00 μl to stop the reaction, Morgan-
A modified version of the Elson method (J. Biol. Chem., 21
7,959 (1955)) and the resulting N- acetylhexosamine weight was determined from the absorbance _OD 585n _m in.

In addition, a 0.1 mM acetate buffer (pH 3.5) was used for the enzyme reaction, and the hyaluronidase inhibitory activity was calculated by the inhibition rate determined by the following equation.

[0034]

(Equation 1) ◎, 90-90% or more, ○, 30-5
9% was represented by Δ, and less than 30% was represented by ×.

[0035]

[Table 2]

As is clear from the results in Table 2, the high hyaluronidase inhibitory activity of each plant extract was proved.

EXPERIMENTAL EXAMPLE 3 Using the extract of each plant obtained according to the Preparation Example, the ability to synthesize collagen involved in tissue activation was evaluated by the following method. Table 3 shows the results
Shown in Method: Human skin-derived fibroblasts (Kurabo Co., Ltd.) were seeded on a 24-well cell culture plate so as to have a confluence of 25%. Until confluent, 37 ° C., 5% carbon dioxide in a DMEM medium containing 10% fetal bovine serum. Culture was performed in the presence of gas. After adding an appropriate amount of the sample, it was cultured under the same conditions for 18 hours. Controls received the same volume of medium. Type I collagen contained in the culture supernatant was quantified by ELISA. 100 μl of the culture supernatant was added to the ELISA plate and stored at room temperature for 18 hours. 0.05% Twe
After washing with PBS containing en-20 (PBS-T), 1%
Block with skim milk / PBS-T for 2 hours.
The cells were treated with an anti-human type I collagen antibody and a peroxidase-labeled anti-rat IgG antibody, and developed using a peroxidase coloring kit. The amount of type I collagen contained in the culture supernatant was determined from the absorbance at 450 nm. When the amount of type I collagen is 120% or more, ◎ 1
01 to 119% were represented by ○, and less than 100% were represented by x.

[0038]

[Table 3]

As apparent from the results in Table 3, the high collagen synthesis ability of each plant extract was proved.

Hereinafter, Examples in which the composition for external use of the present invention is blended will be described. The following examples were all excellent in the effects of preventing and improving skin, hair and oral troubles, and also excellent in safety. In addition, each plant extract is based on the extraction method of the method of Preparation Examples 1-10.

[0041]

[Table 4]

[0042]

[Table 5]

[0043]

[Table 6]

[0044]

[Table 7]

[0045]

[Table 8]

[0046]

[Table 9]

[0047]

[Table 10]

[0048]

[Table 11] * 1 Lion Chemical XM-503LN * 2 Mitsubishi Yuka Yuka Former AM75201

[0049]

[Table 12]

[0050]

[Table 13]

[0051]

[Table 14]

[0052]

[Table 15]

[0053]

[Table 16]

[0054]

[Table 17]

[0055]

[Table 18]

[0056]

[Table 19]

[0057]

[Table 20]

[0058]

[Table 21] The mixture was mixed with a kneader until a paste was formed to give a patch composition. The patch composition was uniformly applied on the nonwoven fabric until the pressure became 150 g / cm ² , and a polyethylene film was applied to prepare a patch.

[0059]

[Table 22]

[0060]

[Table 23]

[0061]

[Table 24]

[0062]

[Table 25] * 1 Shin-Etsu Chemical Co., Ltd. Metroose 65SH-1
500 * 2 Lion Chemical XM-503LN or Leogard GP or UCC Polymer JR400

──────────────────────────────────────────────────続 き Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI Theme coat ゛ (Reference) A61K 7/075 A61K 7/075 7/08 7/08 7/26 7/26 7/32 7/32 7 / 50 7/50 9/70 401 9/70 401 35/78 35/78 C W A61P 17/00 A61P 17/00 43/00 111 43/00 111 F term (reference) 4C076 AA12 AA16 BB31 CC18 CC20 DD28 DD30 DD34 DD37 DD38 DD46 DD50 DD51 DD59 DD60 EE09 EE23 4C083 AA111 AA112 AA122 AB032 AB052 AB172 AB222 AB442 AC012 AC022 AC072 AC102 AC122 AC212 AC242 AC302 AC312 AC342 AC352 AC422 AC432 AC442 AC472 AC482 AC532 AC542 AC582 AC642 AC662 AC162 AD172 AD282 AD352 AD532 AD572 AD662 CC02 CC04 CC05 CC17 CC23 CC37 CC38 CC39 CC41 CC42 DD08 DD11 DD23 DD27 DD31 EE13 EE14 EE16 EE21 EE22 EE32 EE33 EE35 4C088 AB12 AC03 AC04 AC05 AC06 BA08 NA06 ZA90 ZB35

Claims (1)

[Claims] 1. A plant of the genus Xylopia,
Butternut (Caryocar) genus plant, Guazuma (Guazuma) genus plant, tobacco plant (Cuphe)
a) Genus plant, Heteropteri
s) Genus plant, Sciadoteni
a) A genus plant, Ampelodizis
phus), Luhea,
Walnut (Juglans) genus plant and Iwadareso (L
An external composition containing one or more plants selected from the group consisting of ipsia) plants or extracts thereof.