JP2002047194A - Microbial lipase inhibitor, skin care preparation for common acne and skin care preparation for dandruff comprising the same - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a microbial lipase inhibitor having high safety and capable of effectively exhibiting inhibitory effects on microbial lipases by topical application and a skin care preparation for common acne and a skin care preparation for dandruff effective in prophylaxis and treatment of the common acne and dandruff. SOLUTION: This microbial lipase inhibitor is obtained by including an extract from one or more species of plants selected from a plant of Urtica L., a plant of Tilia L., a plant of Sambucus L., Lini Semen, one or more species selected from Asarum caulescens Maxim. and Asiasarum Sieboldii Miq. and a leaf of a plant of Citrus L. as an active ingredient.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to a novel microbial lipase inhibitor, an external preparation for acne and an external preparation for dandruff containing the same. More specifically, safely prevent diseases caused by microbial lipase,
The present invention relates to a microbial lipase inhibitor which can be prevented, a skin external preparation for acne containing the same as an active ingredient, which is effective for preventing and treating acne, and a skin external preparation for dandruff which is effective for suppressing dandruff.

[0002]

2. Description of the Related Art When sebum accumulates due to hyperplasia of sebaceous glands and hyperkeratinization of hair follicles, acne bacilli and staphylococci, which are resident bacteria in the hair follicle, increase in the hair funnel of the hair follicle. Then, the lipase of these bacteria decomposes triglycerides in the cortical components constituting sebum into free fatty acids,
It is said that the free fatty acids act on the epithelium to produce various enzymes, which cause acne, dermatitis, dandruff, etc. (Takeo Mitsui, "New Cosmetic", p29-30, 1993).

On the other hand, development of a drug for inhibiting or preventing acne, dermatitis, dandruff and the like by inhibiting microbial lipase has not been advanced much yet, and tetracycline and metal salts (JP-A-59-1887619) have not been developed. Japanese Patent Application Laid-Open No. 10-265364), loquat extract (JP-A-10-265364),
De Caballo extract (JP-A-11-228338)
Are merely disclosed. However, these drugs could not exert a microbial lipase inhibitory effect due to the relationship with other components, and were not always satisfactory in terms of safety and efficacy in topical application.

[0004]

SUMMARY OF THE INVENTION Accordingly, the present invention provides a microbial lipase inhibitor which is highly safe and can effectively exert an inhibitory effect on microbial lipase when applied topically, and an external skin acne containing the same. The purpose of the present invention is to obtain an external preparation for skin and dandruff.

[0005]

As a result of various studies to solve the above-mentioned problems, an effective microbial lipase inhibitory action was found in specific plant extracts such as nettle plants. When applied to the skin, an external preparation containing a microbial lipase inhibitor consisting of these plant extracts is effective in treating acne, and when applied to the scalp, an dandruff-inhibiting effect is observed. ,
The present invention was completed after confirming that it did not show any skin irritation and skin sensitization.

[0006] That is, in the present invention, one or two selected from the nettle plant, the linden plant, the elder plant, the amanin, the cycins, and the leaves of the mandarin plant.
Extracts of more than one species of plant, containing as an active ingredient to obtain a microbial lipase inhibitor, further containing this,
A skin external preparation for acne and a skin external preparation for dandruff are obtained.

[0007]

DETAILED DESCRIPTION OF THE INVENTION First, a plant used for obtaining an extract in the present invention will be described.

[0008] Urtica (Urtica L.) plant is a dicotyledonous plant belonging to the nettle family (Urticaceae), in particular, but the type is not limited, nettle (Urtica thunbergiana S
ieb.et Zucc.), Urtica angustifolia
Fisch. Et Zucc.), Urtica cannabin
a L.), nettle ( Urtica dioica L.), nettle ( Urtica platyphylla Wedd.), and nettle ( Urt.
ica urense L.). Among these nettle plants, Nettle ( Urtica thunbe)
rgiana Sieb. et Zucc.) and nettle ( Urtica )
dioica L.) is preferably used. Although whole plants or various parts such as flowers, leaves, stems, fruits and roots can be used, it is particularly preferable to use whole plants or roots and leaves.

[0009] Tilia (Tilia L.) is a dicotyledonous plant belonging to the linden family plant (Tiliaceae), but the type is not particularly limited, the United States linden (Tilia america
na L.;. Tilia glabra Vent) , Tilia cordata (Tilia
cordata Mill .; Tilia ulmifolia Scop .; Tilia parv
ifolia Ehrh.), Tilia europaea
L.), linden ( Tilia japonica (Miq.) Simonk.), Herring tree ( Tilia kiusiana Makino et Shiras.), Burdock ( Tilia maximowicziana Shiras.), Bodaiju ( T
ilia miqueliana Maxim.), Natsubodaiju ( Tilia plat
yphyllos Scop .; Tilia grandifolia Ehrh.). Among these linden plants, from the viewpoint of its effect, sclerophylline ( Tilia cordata Mill .; Tilia ulmifol
ia Scop .; Tilia parvifolia Ehrh.) , western linden (Tilia europaea L.), Natsu linden (Tilia platyp
hyllos Scop .; Tilia grandifolia Ehrh.). flower,
Although various parts such as leaves, stems and roots can be used, it is particularly preferable to use leaves or flowers.

[0010] Sambucus (Sambucus L.) plant is a dicotyledonous plant that belongs to the honeysuckle family (Caprifoliceae), but the type is not particularly limited, the United States elder (Sambu
cus canadensis L.), Sambucus javanica
Reinw ex Bl subsp chinensis;.. . Sambucus chinens
is Lindl.), Sambucus nigra ( Sambucus nigra L.),
Elderberry ( Sambucus racemosa L. subsp.sieboldiana
(Miq.) Hara), Sambucus williamsii Han
se) and the like. Among these Elderberry plants, Sambucus nigra ( Sambucus nigra L.) and elderberry ( Sambucus racemosa L. subsp.sieboldiana (Miq.)
It is preferable to use one or two selected from Hara). Although each part such as fruit, flower, leaf, stem, root and the like can be used, it is particularly preferable to use fruit, leaf or flower.

Amanin ( Lini Semen ) is a linseed ( Linacea)
e ) Linseum ( Linium L.) seeds of flax ( Linium usitatissimum L.), which can be used as they are or defatted residues.

The cycins are of the family Aristrophy ( Aristro
chiaceae ), a dicotyledonous plant, Asarum caule
scens Maxim.), Canadian cycin ( Asarum canadensis Mi)
ch.), Asarabakka (Asarum europaeum L.) Futabaaoi genus such as (Asarum L.) plants, thin blade asiasarum (Asiasarum
Sieboldii Miq.), Oquezocysin ( Asiasarum hetero
tropoides Fr. Schum.), Keirin Saishin ( Asiasarum )
heterotropoides Fr.Schum. var. mandshuricum (Maxi
m.) Kitagawa) Ashiasarumu genus such as (Asiasarum L.) can be used a plant, in terms of its effect, Futabaaoi (A
sarum caulescens Maxim.) and Usuba saicin ( Asiasar
um Sieboldii Miq.) is preferably used. Although various parts such as whole plants, leaves, stems and roots can be used, it is preferable to use roots.

Citrus L. plants are of the Citrus family ( Ru).
taceae ), which is an evergreen fruit tree of any kind, for example, lime ( Citrus aurantifolia Swingl
e), Hichilime ( Citrus latifolia Tanaka), Sweet Rime ( Citrus limettioides Tanaka), Bergamot ( C
itrus bergamia Risso et Poit.), Citron ( Citrus me )
dica L.), lemon (Citrus limon Burm.), sweet lemon (Citrus limetta Risso), Rough Lemon (Citrus jambhi
ri Lush.), Meier lemon ( Citrus meyeri Y. Tanak)
a), Pomelo ( Citrus grandis Osbeck), Oyu ( Citrus p
seudogulgul Hort. ex Shirai), grapefruit ( Cit
rus paradisi Macf.), Kinukawa ( Citrus glab errima Ho
ex. Tanaka), Yamamikan ( Citrus intermedia Hort.
ex Tanaka), Hassaku ( Citrus hassaku Hort. ex Tana)
ka), Naruto ( Citrus medioglobosa Hort. ex Tanaka),
Natsumikan ( Citrus natsudaidai Hayata), Kinkouji
( Citrusobovoidea Hort. Ex Takahashi), Otachibana
(Citrus otachibana Hort. Ex Y. Tanaka ), Sanpoukan (Citrus sulcata Hort. Ex Takahashi) , orange (Ci
trus aurantium L.), Chinot ( Citrus myritifolia Ra)
fin.), Satsuma Kikoku ( Citrus neoaurantium Hort. ex T
anaka), sweet orange ( Citrus sinensis Osbeck),
Funadoko (Citrus funadoko Hort. Ex Y. Tanaka ), Tankan (Citrus tankan Hayata), iyokan (Citrus iyo Ho
ex Tanaka), Hyuga Natsu ( Citrus tamurana Hort.
ex Tanaka), Shunkokan ( Citurs shunkokan Hort.
ex Tanaka), Echan Chi ( Citrus ichangensis Swi)
ngle), Yuzu ( Citrus junos Sieb. exTanaka), Hanayu ( C
itrus hanaju Hort. ex Shirai), Citrus sudac
hi Hort. ex Shirai), Yuko ( Citurs yuko Hort. ex T)
anaka), Naoshi ( Citrus takuma-sudachi Hort. ex Ta
naka), Cabos ( Citrus sphaerocarpa Hort. ex Tanak
a), King ( Citrus nobilis Lour.), Unshu Mandarin
( Citrus unshiu Mar.), Yatsushiro ( Citrus yatsushiro H
ort. ex Tanaka), Keraj ( Citrus keraji Hort.ex Tana)
ka), Ponkan ( Citrus reticulata Blanco), Chicken mandarin ( Citrus deliciosa Tenore), Dancy tangerine ( Citrus tangerina Hort. ex Tanaka), Alzerian ( Citrus clementina Hort. ex Tanaka), Benikoji ( Citrus benikoji Hort. ex Tanaka) , Manchutsu ( C
itrus tardiferax Hort. ex Tanaka), Tachibana ( Citrus
tachibana Tanaka), Citrus kinokuni
Hort. Ex Tanaka), Sunki ( Citrus sunki Hort. Ex
Tanaka), Cleopatra ( Citrus reshni Hort. Ex Tanak)
a), Humutia Tenga ( Citrus indica Tanaka), Shiikuwasha ( Citrus depressa Hayata), Koji ( Citrus le
iocarpa Hort. ex Tanaka), Fukuromikan ( Citrus tumi )
da Hort. ex Tanaka), Toukinkan ( Citrus madurensi )
s Lour.), and among these Citrus plants, one or two selected from sweet orange ( Citrus sinensis Osbeck) and Unshu mandarin ( Citrus unshiu Mar.) are preferably used. The leaves of these Citrus plants are used.

In the present invention, the above-mentioned plant may be subjected to extraction as it is, but in consideration of extraction efficiency, it is preferable to perform extraction after performing processing such as shredding, drying, and pulverization. The extraction is performed by immersion in an extraction solvent. Stirring may be performed to increase the extraction efficiency, or homogenization may be performed in an extraction solvent. It is appropriate that the extraction temperature is set to a temperature of about 5 ° C. to the boiling point of the extraction solvent or lower. The extraction time varies depending on the type of the extraction solvent and the extraction temperature, but is suitably about 4 hours to 2 weeks.

As an extraction solvent, in addition to water, methanol,
Lower alcohols such as ethanol, propanol and isopropanol; polyhydric alcohols such as 1,3-butylene glycol, propylene glycol, dipropylene glycol and glycerin; ethers such as ethyl ether and propyl ether; esters such as ethyl acetate and butyl acetate And polar organic solvents such as ketones such as acetone and ethyl methyl ketone, and one or more of these can be selected and used. Further, physiological saline, phosphate buffer, phosphate buffered saline, or the like may be used. The ratio of the plant to the solvent at the time of extraction is not particularly limited, but the solvent is preferably 0.1 to 1000 times by weight, particularly 0.5 to 100 times by weight, from the viewpoint of the extraction operation and efficiency with respect to the plant 1.

The extract of the above-mentioned plant such as nettle can be used as it is as the microbial lipase inhibitor of the present invention, but the concentrated and dried extract can be redissolved in water or a polar solvent. Alternatively, it may be used after a purification treatment such as decolorization, deodorization, desalting or the like is performed as long as the microbial lipase inhibitory action is not impaired, or after a fractionation treatment by column chromatography. For preservation, it can be freeze-dried after the purification treatment and dissolved in a solvent before use.

In the present invention, an extract of the above plant such as nettle or the like or a processed product thereof with the above solvent may be used as it is, or may be contained in an aqueous carrier such as water or lower alcohol, or a base such as an emulsion, a gel, a cream or an ointment. , Powdered or granulated to obtain a microbial lipase inhibitor. Moreover, it can also be encapsulated in vesicles such as liposomes, microcapsules and the like.

The amount of the microbial lipase inhibitor to be added to the external preparation for acne and the external preparation for dandruff should be 0.0001 to 0.0001 in view of its effect, odor and color tone when added.
It is desirable that the concentration range be 10% by weight.

The skin external preparation for acne and the skin external preparation for dandruff of the present invention may contain, if necessary, oils, fats, humectants, powders and the like which are usually added to pharmaceuticals, quasi-drugs, skin cosmetics and cleansing agents. A body, a pigment, an emulsifier, a solubilizer, a detergent, an ultraviolet absorber, a thickener, a drug, a fragrance, a resin, an alcohol, and the like can be appropriately blended. Further, the dosage form of the external preparation for acne and the external preparation for aging skin of the present invention is arbitrary, and is provided, for example, as a solubilizing system such as a lotion, an emulsifying system such as a cream or an emulsion, or a dispersion system such as a calamine lotion. Alternatively, it may be in the form of an aerosol filled with a propellant.

[0020]

EXAMPLES Further, the features of the present invention will be described in detail with reference to examples. First, a preparation example of a microbial lipase inhibitor used in the present invention will be described.

Examples 1 to 6 Microbial lipase inhibitors 250 g of each of the plants shown in Table 1 were dried and pulverized, and 50% by volume.
Immerse in 1.0 liter of aqueous ethanol
For 7 days to extract. The extract was filtered to collect the filtrate, which was then sterilized with a Millipore filter to obtain Examples 1 to 6 which were aqueous preparations.

[0022]

[Table 1]

In Examples 1 to 6, the effect of inhibiting microbial lipase activity was evaluated. The evaluation was performed by adding 4-methylumbelliferyl oleate, which emits fluorescence by deesterification, to microbial lipase (Acne bacteria ( Propion
ibacterium acnes )), and quantified the resulting 4-methylumbelliferone having fluorescence using a fluorescence intensity meter. In detail, a lipase solution derived from a microorganism is added to a 96-well microplate at a final concentration of 1%.
mg / ml, each example was added to be 0.1 mg / ml, and 4-methylumbelliferyl oleate was further added to be 100 μM. 20 in the dark
After reacting for 4 minutes, 4-methylumbelliferone obtained by decomposition was measured with a fluorescence intensity meter under the conditions of excitation wavelength: 355 nm and fluorescence wavelength: 460 nm. The effect of inhibiting microbial lipase activity is 4-
The amount of 4-methylumbelliferone produced when only methyl umbelliferyl oleate and the microorganism-derived lipase solution were reacted was taken as 100, and the amount of 4-methylumbelliferone produced when the example was added was used. expressed. The results are shown in Table 2.

[0024]

[Table 2]

As is clear from Table 2, Examples 1 to 6 of the present invention all showed a high microbial lipase activity inhibitory effect.

Next, an example of an external preparation for acne skin containing the microbial lipase inhibitor shown in Examples 1 to 6 will be described.

[Examples 7 to 12] Skin lotion (1) Ethanol 10.0 (wt%) (2) Hydroxyethylcellulose 1.0 (3) Microbial lipase inhibitor 5.0 shown in Table 3 5.0 (4) Glycerin 7.0 (5) Sodium guaiazulene sulfonate 0.5 (6) Purified water 76.5 Production method: Mix (1) to (6) to make uniform.

[0028]

[Table 3]

In order to show the acne symptom-relieving effect of the skin lotions shown in Examples 7 to 12, a group of 20 male and female panelists in their teens and twenties with acne symptoms was acne twice a day. Were used continuously for one month, and the condition of acne before and after use was observed. For reference, Comparative Example 1 in which the microbial lipase inhibitor was replaced with purified water was prepared and similarly evaluated. The results were evaluated in terms of the improvement of acne symptoms in four stages of “improvement”, “slight improvement”, “no change”, and “deterioration”. Table 4 shows the number of panelists who obtained each evaluation.

[0030]

[Table 4]

As is evident from Table 4, none of the panelists who used Examples 7 to 12 of the present invention had any acne symptom-exacerbated panelists, and 8 or more panelists tended to improve. Was. In contrast, Comparative Example 1
In the use group, none of the panelists showed a clear improvement in the symptoms, and 10% of the panelers worsened.

In Examples 7 to 12 of the present invention, the precipitation, separation, and
No change in the state of the preparation such as aggregation, discoloration or discoloration was observed. In addition, in each group used in Examples, there was no paneler showing a skin irritating reaction or a skin sensitizing reaction.

Next, the formulation of another skin external preparation for acne of the present invention will be described.

Example 13 O / W emulsified beauty solution (1) Squalane 5.0 (% by weight) (2) White petrolatum 2.0 (3) Beeswax 0.5 (4) Sorbitan sesquioleate 8 (5) Polyoxyethylene oleyl ether (20EO) 1.2 (6) Methyl paraoxybenzoate 0.1 (7) Propylene glycol 5.0 (8) Purified water 59.1 (9) 1.0% by weight of carboxyvinyl polymer Aqueous solution 20.0 (10) Potassium hydroxide 0.1 (11) Ethanol 5.0 (12) Microbial lipase inhibitor shown in Example 1 1.0 (13) Fragrance 0.2 Production method: (1)- The oil phase component (5) is mixed and heated to 75 ° C. to dissolve and homogenize. On the other hand, the aqueous phase components (6) to (8) are mixed and dissolved, and the mixture is heated to 75 ° C., and the above-mentioned oil phase component is gradually added to carry out preliminary emulsification. After adding (9), the mixture is uniformly emulsified with a homomixer, and (10) is added to adjust the pH. After cooling, add (11) to (13) at 40 ° C, mix and homogenize.

[Example 14] Gel for skin (1) Purified water 90.9 (wt%) (2) Carboxyvinyl polymer 0.5 (3) Microbial lipase inhibitor 0.5 shown in Example 2 (4) Dipropylene glycol 8.0 (5) Potassium hydroxide 0.1 Production method: (2) and (3) are uniformly dissolved in (1), (4) is added, and then (5) is added. In addition, increase the viscosity.

Example 15 Skin Cream (1) Beeswax 6.0 (% by weight) (2) Cetanol 5.0 (3) Reduced Lanolin 3.0 (4) Squalane 29.5 (5) Lipophilic type Glyceryl monostearate 4.0 (6) Polyoxyethylene (20EO) sorbitan monolaurate 5.0 (7) Propylene glycol 5.0 (8) Microbial lipase inhibitor 1.0 (shown in Example 3) 9) Purified water 41.5 Production method: Mix and dissolve the oil phase components (1) to (6) and heat to 75 ° C. On the other hand, the aqueous phase components (7) to (9) are mixed and dissolved and heated to 75 ° C. Next, the oil phase component is added to the water phase component and pre-emulsified, and then uniformly emulsified by a homomixer.

Example 16 Jelly-like peel-off pack (1) Polyvinyl alcohol 15.0 (% by weight) (2) Carboxymethyl cellulose 5.0 (3) 1,3-butylene glycol 3.0 (4) Ethanol 0 (5) Polyoxyethylene (20EO) oleyl ether 0.5 (6) Microbial lipase inhibitor shown in Example 4 0.5 (7) Purified water 70.0 Production method: (3) was added to (7) In addition, heat to 75 ° C. Add (1) and (2) to this to dissolve, and add (4) to (6) to solubilize.

Example 17 Cleansing Gel (1) Purified water 63.5 (% by weight) (2) Carboxyvinyl polymer 0.5 (3) Silicic anhydride 7.0 (4) Microorganism shown in Example 5 Lipase inhibitor 1.0 (5) glycerin 10.0 (6) 1,3-butylene glycol 5.0 (7) polyoxyethylene (20EO) lauryl ether 5.0 (8) polyoxyethylene (50EO) curing Castor oil 2.5 (9) Diethylene glycol monoethyl ether 5.0 (10) Potassium hydroxide 0.5 Manufacturing method: (1) is heated to 75 ° C., and the components (2) to (10) are sequentially added. Mix and homogenize.

Example 18 Massage Gel (1) Dipropylene glycol 7.0 (% by weight) (2) Glycerin 8.0 (3) Polyoxyethylene (15EO) oleyl ether 1.0 (4) Carboxyvinyl polymer 0.4 (5) Methylcellulose 0.2 (6) Microbial lipase inhibitor shown in Example 6 1.0 (7) Potassium hydroxide 0.1 (8) Purified water 82.3 Production method: heated to 75 ° C To (8), the components (1) to (7) are sequentially added, dissolved and homogenized.

[Example 19] Face wash (1) Stearic acid 2.0 (% by weight) (2) Cetanol 3.0 (3) Vaseline 10.0 (4) Liquid paraffin 33.0 (5) Isopropyl myristate 7.5 (6) Glyceryl monostearate 2.5 (7) Polyoxyethylene (20EO) sorbitan monostearate 2.5 (8) Glycerin 5.0 (9) Microbial lipase shown in Example 1 Inhibitor 0.5 (10) Microbial lipase inhibitor shown in Example 2 0.5 (11) Potassium hydroxide 0.1 (12) Purified water 33.4 Production method: Oil of (1) to (7) The phase components are mixed and dissolved by heating to 70 ° C. On the other hand, the aqueous phase components (8) to (12) are mixed and dissolved by heating to 70 ° C. The oil phase component is gradually added to the aqueous phase component to perform preliminary emulsification, and then homogenized using a homomixer.

Using the external preparations for acne shown in Examples 7 to 19, the effect of alleviating acne symptoms was evaluated by the above method. As a result, an acne symptom alleviating effect was observed in all Examples. In addition, in each group used in Examples, there was no paneler showing a skin irritating reaction or a skin sensitizing reaction.

Next, the formulations of the examples relating to the dandruff skin external preparation containing the microbial lipase inhibitor shown in Examples 1 to 6 are shown.

[Examples 20 to 25] Tonic lotion (1) Ethanol 50.0 (% by weight) (2) Microbial lipase inhibitor shown in Table 5 5.0 (3) Fragrance 0.2 (4 ) Purified water 44.8 Production method: Mix and homogenize components (1) to (4).

[0044]

[Table 5]

In order to show the dandruff symptom-relieving effect of the tonic lotions shown in Examples 20 to 25, 20 male panelists in their 20s to 40s having dandruff symptoms were treated as a group twice a day for 1 month. They were used continuously, and the state of dandruff before and after use was observed. For reference, Comparative Example 2 in which the microbial lipase inhibitor was replaced with purified water was prepared and similarly evaluated. The results were evaluated in terms of the improvement status of the dandruff symptom in four stages of “improvement”, “slight improvement”, “no change”, and “deterioration”. Table 6 shows the number of panelists who obtained each evaluation.

[0046]

[Table 6]

As is evident from Table 6, none of the panelists using Examples 20 to 25 of the present invention had any dandruff symptom exacerbated, and 8 or more panelists tended to improve. Was. On the other hand, Comparative Example 2
In the use group, none of the panelists had a clear improvement in the symptoms, and 40% of the panelists had worsened.

In Examples 20 to 25 of the present invention, no change in the state of the preparation such as precipitation, separation, aggregation, discoloration, and discoloration of the components was found during the use test period. In addition, in each group used in Examples, there was no paneler showing a skin irritating reaction or a skin sensitizing reaction.

Example 26 Hair lotion (1) Purified water 40.4 (% by weight) (2) Polyoxyethylene (50EO) hydrogenated castor oil 2.0 (3) Ethanol 50.0 (4) Avocado oil 1 0.0 (5) Microbial lipase inhibitor shown in Example 3 1.0 (6) Pyridoxine hydrochloride 0.5 (7) 1,3-butylene glycol 5.0 (8) Fragrance 0.1 Production method: (1) After dissolving (2) in (1), components (3) to (8) are sequentially added and uniformly dissolved.

Example 27 Hair restorer (1) Purified water 30.9 (% by weight) (2) Polyoxyethylene (50EO) hydrogenated castor oil 3.0 (3) Ethanol 60.0 (4) Fragrance 0.1 (5) Tocopherol acetate 0.5 (6) Microbial lipase inhibitor 0.5 shown in Example 4 (7) Hop 50% by weight ethanol extract 3.0 (8) Propylene glycol 2.0 Production method: (1) ) Is dissolved in (2), and the components (3) to (8) are sequentially added and mixed to dissolve uniformly.

[Example 28] Hair foam (stock solution formulation) (1) Silicone oil 5.0 (wt%) (2) Pantothenyl alcohol 0.5 (3) Polyoxyethylene (50EO) hydrogenated castor oil 1.0 (4) Dipropylene glycol 7.0 (5) Methylcellulose 2.5 (6) Purified water 67.9 (7) Ethanol 15.0 (8) Microbial lipase inhibitor shown in Example 5 1.0 (9 ) Fragrance 0.1 (filling formula) Undiluted solution 90.0 Liquefied petroleum gas 10.0 Manufacturing method: Add the mixture of (1) to (3) to the melt of (4) to (8) and homogenize with a homomixer. Emulsify. Add (9) to this and mix to make uniform. Filling is performed by filling the can with the undiluted solution, installing a valve, and then filling with liquefied petroleum gas.

Example 29 Hair gel (1) Carboxyvinyl polymer 0.50 (% by weight) (2) Glycerin 2.00 (3) Microbial lipase inhibitor shown in Example 6 1.00 (4) Ethanol 20.00 (5) Polyoxyethylene (20EO) stearyl ether 0.20 (6) Fragrance 0.10 (7) Purified water 76.15 (8) Sodium hydroxide 0.05 Production method: (1) to (2) ). Then, (3) to (6) are dissolved in (7), added and mixed, and (8) is added to increase the viscosity.

Example 30 Set lotion (1) Polyvinylpyrrolidone / vinyl acetate copolymer 5.0 (% by weight) (2) Fragrance 0.1 (3) Ethanol 30.0 (4) Purified water 58.9 (5) Polyoxyethylene / polyoxypropylene modified dimethylpolysiloxane 2.0 (6) Glycerin 2.0 (7) Microbial lipase inhibitor 2.0 shown in Example 1 Production method: (1), (2) Is added to (3) and uniformly dissolved. To this, the components (4) to (7) previously dissolved are added and uniformly dissolved.

Example 31 Hair Treatment (1) Liquid paraffin 20.00 (% by weight) (2) Vaseline 10.00 (3) Beeswax 2.00 (5) Polyoxyethylene (50EO) hydrogenated castor oil 00 (6) Glycerin 2.00 (7) Carboxyvinyl polymer 0.05 (8) Xanthan gum 0.05 (9) Disodium ethylenediaminetetraacetate 0.10 (10) Microbial lipase inhibitor 1 shown in Example 2 0.000 (11) Purified water 61.60 (12) Fragrance 0.20 Production method: Heat and dissolve the oil phase components (1) to (4) to 80 ° C. On the other hand, the aqueous phase components (5) to (11) are mixed and dissolved by heating to 80 ° C. The oil phase is added thereto with stirring, and the mixture is uniformly emulsified by a homogenizer. After cooling, add (12) at 40 ° C and mix.

Example 32 Hair Shampoo (1) Purified water 53.85 (% by weight) (2) Polyoxyethylene (3E.O.) lauryl sulfate sodium salt (30% by weight aqueous solution) 30.00 (3 ) Lauryl sulfate sodium salt (30% by weight aqueous solution) 10.00 (4) Coconut oil fatty acid diethanolamide 4.00 (5) Glycerin 1.00 (6) Disodium ethylenediaminetetraacetate 0.05 (7) Example 3 1.00 (8) Fragrance 0.10 Production method: (1) is heated to 70 ° C., (2) to (7) are added, uniformly dissolved and cooled, and At 0 ° C, add (8), mix and dissolve uniformly.

Example 33 Hair rinse (1) Silicone oil 5.000 (% by weight) (3) Cetanol 1.000 (4) Stearyl alcohol 0.800 (5) Stearyl trimethyl ammonium chloride 0.700 (6) Glycerin 3.000 (7) Green No. 3 0.002 (8) Microbial lipase inhibitor shown in Example 4 2.000 (9) Purified water 87.348 (10) Fragrance 0.150 Production method: (5) The aqueous phase components of (9) to (9) are mixed and dissolved, and heated to 70 ° C. On the other hand, the oil phase components (1) to (4) are mixed and heated to 70 ° C. The oil phase is added to the aqueous phase and emulsified with a homomixer. After cooling, (10) is added and mixed at 40 ° C.

Using the external preparations for dandruff shown in Examples 26 to 33, the effect of alleviating dandruff symptoms was evaluated by the above method. As a result, in all the examples, the effect of alleviating dandruff symptoms was observed. In each example use group,
None of the panelists showed a skin irritation or skin sensitization reaction.

[0058]

As described in detail above, according to the present invention, a microbial lipase inhibitor which is highly safe and can effectively exert an inhibitory effect on microbial lipase by topical application, and contains the microbial lipase inhibitor as an active ingredient An external preparation for acne and an external preparation for dandruff were obtained.

──────────────────────────────────────────────────続 き Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI Theme coat ゛ (Reference) A61K 7/06 A61K 7/06 A61P 17/00 A61P 17/00 17/10 17/10 43/00 111 43 / 00 111 (72) Inventor Hitoshi Masaki 6-13-1, Minatojima-Nakamachi, Chuo-ku, Kobe-shi, Hyogo F-term in Noevir Kobe Research Laboratories Co., Ltd. 4C083 AA111 AA112 AA122 AB032 AB172 AC012 AC022 AC072 AC102 AC122 AC182 AC242 AC352 AC422 AC432 AC442 AC482 AC532 AC642 AC692 AC782 AC792 AD072 AD092 AD112 AD162 AD262 AD282 AD352 AD512 AD632 AD662 CC02 CC04 CC05 CC07 CC23 CC32 CC33 CC37 CC38 DD08 DD22 DD23 DD27 DD33 DD41 EE14 EE23 4C088 AB12 AB62 AC03 AC04 AC05 MA06 CA06 MA63 NA14 ZA89 ZC20

Claims (3)

[Claims] 1. Microbial activity comprising an extract of one or more plants selected from the nettle plant, linden plant, elder plant, amanin, cycins, and mandarin plant leaves as an active ingredient. Lipase inhibitors. 2. An external preparation for acne containing the microbial lipase inhibitor according to claim 1 as an active ingredient. 3. An external preparation for dandruff comprising the microbial lipase inhibitor according to claim 1 as an active ingredient.