CA1142854A - Method and compositions for the treatment of seborrhea - Google Patents

Method and compositions for the treatment of seborrhea

Info

Publication number
CA1142854A
CA1142854A CA000330577A CA330577A CA1142854A CA 1142854 A CA1142854 A CA 1142854A CA 000330577 A CA000330577 A CA 000330577A CA 330577 A CA330577 A CA 330577A CA 1142854 A CA1142854 A CA 1142854A
Authority
CA
Canada
Prior art keywords
skin
seborrhea
fatty acid
composition
carrier
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired
Application number
CA000330577A
Other languages
French (fr)
Inventor
Theodor Eckert
Fritz H. Kemper
Karl Nolting
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Dr August Wolff GmbH and Co KG Arzneimittel
Original Assignee
Dr August Wolff GmbH and Co KG Arzneimittel
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Dr August Wolff GmbH and Co KG Arzneimittel filed Critical Dr August Wolff GmbH and Co KG Arzneimittel
Application granted granted Critical
Publication of CA1142854A publication Critical patent/CA1142854A/en
Expired legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/008Preparations for oily skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36Carboxylic acids; Salts or anhydrides thereof
    • A61K8/361Carboxylic acids having more than seven carbon atoms in an unbroken chain; Salts or anhydrides thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders

Abstract

ABSTRACT OF THE DISCLOSURE

Novel compositions and the method of their use is disclosed. The compositions and method of the invention are useful for treating seborrhea in mammals including humans. The compositions comprise cosmetically acceptable topical carriers having dispersed therein as the primary and essential active ingredient, medium chain-length fatty acids.

Description

L2~35~

The invention concerns cosmetic and pharmaceutical compositions and more particularly is concerned with topically applied cosmetic/pharmaceutical compositions having incorporated therein as the essential active ingredient a fatty acid.
Seborrhea is a functional disturbance of mammalian skin marked by an excessive discharge of cutaneous sebum from the sebaceous glands. The physical manifestation of the hypersteatosis is an excessively "oily" skin or scalp accompanied`
by itching or burning sensations. The secretion of sebum in normal, healthy skin is desirable since it serves to keep the skin soft and pliant, prevents excessive water evaporation from the stratum corneum and water absorption into the skin, serves as a thermal insulator and keeps the hair supple. However, excessively oily skin and scalp may present aesthetic and health problems,such as skin infections. Excessive oiliness of the skin concerns many humans. The popular concept of too much sebum on the skin surface includes "greasiness" and "shininess"
of the skin complexion. Heretofore, the most common means of removing excess sebum from the skin surface has been by mechanical removal. Means of mechanical removal include washing with the assistance of alkali, soap, detergents, etc. (see for example U.S. Patent No. 3,326,808), by the application of ~-cleansing lotions, astringent lotions, astringent creams and by the application of mud packs and steamingO The difficulty with the aforesaid methods of treating excessively oily skin resides in the possibility that when vigorously applied such treatments also tend to ultimately lead to a dehydration of the stratum corneum, a condition which is manifested by "dry skin". Thus the individual who is concerned about excessive skin oils may be continually doing battle with cycles of "dry skin" as well as with "oily skin" problems.
By the method of our invention~ and by the use of the compositions of our invention it is now possible to remove excessive skin oils from mammalian skin and to treat seborrhea without disadvantages associated with the prior art. The treatment in no way interferes with normal secretions of sebum, and therefore, the natural and desired activity of sebum secretion is not interfered with. The compositions of our invention are also cosmetically and aesthetically acceptable and may be employed by fastidious individuals during the normal course of their daily activity.
The present invention provides a composition for cosmetically treating the physical manifestations of oily skin resulting from seborrhea in humans, comprising a fatty acid selected from the group consisting of pelargonic~ capric, n-undecyclic, lauric and n-tridecyclic acid dispersed in a topical application carrier which is non-toxic and non-irritating to the skin, the fatty acid being present in an amount which, when the composition is applied to the skin affected with seborrhea, is effective to reduce excess sebaceous secretions of seborrhea on the affected skin surface.
The term "a cosmetically and pharmaceutically acceptable topical carrier" as employed throughout the specification means a vehicle or base for topical (skin) application and into which the essential active ingredient may be incorporated. The vehicle or base comprises various cosmetically and physiologically suitable additives for the ~4~8~41 purpose of facilitating the formulation of said primary active ingredients into the desired topical forms. By the term "physiologically suitable",wemean that they are generally non-toxic and non-irritating to mammalian skin in the quantities employed.
The term "topical application" as used herein means an application to the skin surface. The vehicles andbases which comprise topical carriers for use in compoundingthe compositions of the invention are represented by conventional topical forms, such as ointments, lotions, pastes, soaps, shampoos, jellies, powders, solutions for wet application, paints, sprays, aexosols and the like. The term "ointment" as used herein is intended to be embracive of formulations having oleoginous, absorption, water soluble and emulsion type bases such as creams, vanishing creams and the like.
The term "an effective amount" as used herein means that quantity which re`duces excess sebaceous secretions of sebum on the skin. In general, the quantity may be within the range of from about 0.0001 to 50 mgs. per square centimeterofaffected skin area.
The compositions of the invention are useful in carrying out the method of the invention.
The essential active ingredients of the compositions of the invention are generally well known as is their preparation. Representative of medium chain-length fatty acids are fatty acids having 8 to 12 carbon atoms such as pelargonic, capric, n-undecylic, lauric, n-tridecylic and like acids.
Preferred as the medium chain-length fatty acids employed in the method and compositions of the invention are capric and lauric acids.

The method of the invention may be carried out by applying the medium chain-length fatty acid to the seborrhea affected area of the mammal's skin. Preferably, the fatty acid as the essential active ingredient is contained in a pharmaceutically acceptable topical carrier, i.e.; in a composition of the invention.
The cosmetically/pharmaceutically acceptable carrier component of the compositions makes possible a dispersion of the essential active ingredient for close and intimate contact with the affected skin. In this sense, there is cooperation between essential active ingredient and the carrier adjuvant.
The carrier is the means by which the inherent properties of the essential active ingredient are fully realized. In general, the proportion of essential active ingredient dispersed in the carrier is within the range of from about 0.1 to about40 percent by weight of the total formulation.
The cosmetically and pharmaceutically acceptable topical carriers employed in preparing the compositions of the invention are compounded from conventionally employedin~redients for topical applications, using conventional techniques and apparatus. For example, topical emulsions may be prepared by dispersing the essential active ingxedient in a suitable emulsion base. Advantageously, the essential actlve ingredient is finely divided, for example by means of a colloid mill, utilizing light liquid polyols as a levigating agent prior to dispersion in the topical base. Topical creams and lotions are prepared by dispersing the active ingredient in the finished product after the oil phase and water phase have formed the emulsion. Adjuvants, such as secondary active ingredients, i.e.; germicides, insect repellants, vitamins, hormones, deodorants and the like,may be
2~3`Si4~

added as desired. Inert adjuvants~such as emulsifiers,solvents, colorants, sun screens, sequestrants, perfumes and where necessary, propellants,may be added.
Face powders, such as pressed powders,maybe prepared, for example,by blending from about 1 to 10 parts by weight of the essential active ingredient with from about 90 to 95 parts of the pressed powder vehicle. Representative of pressed powder vehicles which may be employed are those comprising opacifying agents such as titanium dioxide, zinc oxide, magnesium oxide and mixtures thereof with kaolin; lubricants such as talc,mica, zinc stearate, magnesium stearate and the like; binders such as magnesium and zinc stearate, hydrocarbon oils, fatty materials and the like; blooming agents such as chalk, starch and the like, anti-oxidants such as butylated hydroxyanisole and the like; preservatives such as methylparaben, propylparaben and the like; emollients such as hydrophyllic lanolin derivatives such as ethoxylated lanolin, cetyl alcohol and the like, colorants, perfumes and like adjuvants.
Topical fluid preparations,such as aqueous and alcoholic suspensions,may be prepared by suspendingthe essential active ingredient in the aqueous or alcoholic solutions.
Advantageously,a surfactant or wetting agent is included in the compositions to facilitate uniform distribution of the active ingredient.
Skin freshening astringent lotions are prepared by preparing an emulsion of the essential active ingredient in a mixture of water-alcohol to which an astringent,such as witch hazel and the like,are advantageously added.
Aqueous shampoos containing the essential active ingredient may be prepared in conventional manner by suspension ~2~1$~

in the presence of surface active agents, opacifying agents, viscosity controlling fillers, foam stabilizers and like conventional adjuvants. In addition, secondary active ingredients such as germicidal agents may be incorporated in the formulations.
The preferred form of cosmetically acceptable carrier employed in the preparation of compositions within the scope of the invention are aqueous and/or alcoholic suspensions or solutions. Representative of alcohols which may be employed as 10~ alcoholic carrier means in compositions of the invention are ethyl alcohol, isopropyl alcohol, propylene glycol, ethylene glycol, mixtures thereof and the like.
The following examples describe the manner and process of making and using the invention and set forth the best mode contemplated by the inventors of carrying out the invention but are not to be construed as limiting. All parts are by weight unless otherwise stated.
Example 1 To 95 parts of ethanol (96~),there is added with stirring 5 parts of capric acid. The resulting solution is applied to the seborrhea affected skin of a human, three times daily. After 7 days there is a noticeable improvement of the seborrheic condition. Similarly, repeating the above procedure but replacing the capric acid as used therein with an equal proportion of pelargonic, n-undecylic and n-tridecylic acids, respectively, similar results are obtained.
Example 2 To 95 parts of isopropyl alcohol~there is added 5 parts of lauric acid. The resulting solution is applied to the seborrhea affected skin of a human, twice a day. After 7 days there isanoticeable improvement of the seborrheic condition.
Example 3 To 95 parts of propylene glycol,there is added with stirring 5 parts of capric acid. The resulting solution is applied to the seborrhea affected skin of a human twice daily.
After 7 days an(~ticeable improvement in the seborrheic condition is observed.
Example 4 To 90 parts of polyethylene glycol (M.W. 400),there is added with stirring 10 parts of capric acid. The resulting solution is applied once daily to the seborrhea affected area of a human?s skin. After 7 days, an improvementofthe seborrheic condition is observed.
Example 5 A pressed powder is prepared having the following formulation:
Parts pigments qs zinc stearate 2.00 Mica l.O0 methylparaben, USP 0.15 propylparaben, USP 0.15 butylated hydroxyanisole 0.02 light mineral oil, NF 3.00 polyoxyethylene derivative of acetylated lanolin* 2.00 lauric acid 1.00 ~ 10.00 * Solulan 98, American Cholesterol Products Incorporated Edison, New Jersey.
The dry ingredients are introduced into a ribbon S~

blender and thoroughly blended. The oil binders and perfume are sprayed into the thoroughly blended dry ingredients. The total mixed ingredients are then passed through a micro pulverizer and ultimately pressed into suitable pans. The resulting face powder is effective for simultaneously absorbing sebum and moisturizing facial skin when applied in a thin covering upon the face.
Example 6 Face mask preparations may be prepared by the following procedures:

A B C D E
1% 5% 10% 15%_ 20%

Pluronic F127 15.00lS.0020.00 (BASF-Wyandotte, Supra) propylene glycol 21.0011.0030.0030.00 10.00 alcohol SD40 25.0034.0025~00~0.00 69.95 glycerol - - 10.00 5.00 -menthol 0.05 0.050.05 0.05 0-05 Methocel 60HG (4000 cps)3.003.00 lauric acid 1.00 5.0010.0015.00 20.00 water 35.9531.954.959.95 Procedure:
To prepare each of the face masks of formulaeA-E,disperse the lauric acid and the Methocel,when required,into the alcohol in which the menthol has been previously dissolved. When thoroughly dispersed, add the water. This forms the first component. The second component is made by first blending the polyols (Pluronic, propylene glycol and glycerol). The blend is heated to 60C when Pluronic is used (otherwise,mix polyols at room temperature). The two components are thereafter admixed -7~r~ a~

8S9~

at room temperature with a homogenizer, or passed through a roller mill if the product is too heavy for a homogenizer to conveniently process The face mask may be applied once daily to simultaneously remove excess oiliness and moisturize the skin of a mammal such as a human.
xample 7 Parts propylene glycol 6.00 witch hazel 20.00 alcohol SD40 40.00 ethoxylated oleyl alcohol (10 mols ethylene oxide) 3.G0 capric acid 1.00 - 10.00 water qs to 100 parts Mix the propylene glycol, alcohol, ethoxylated oleyl alcohol, and then slowly add the capric acid at room temperature.
When the capric acid is thoroughly wetted and dispersed, then add witch hazel, water and homogenize the resulting mixture.
The lotion may be applied twice daily for the control of excess sebum secretion.
Example 8 --An after-shave lotion is formulated with the following ingredients:
Parts propylene glycol 5.00 ethoxylated oleyl alcohol (5 mols of ethylene oxide) 4.00 alcohol SD40 65.00 capric acid 1.00 - 10.00 perfume 2.00 water qs to 100 parts Mix propylene glycol, ethoxylated oleyl alcohol, alcohol and perfume at room temperature. Add the capric acid to the resulting mixtures and stir until thoroughly dispersed, then add water and homogenize the final mixture.
Applied after each shave, the lotion helps control excess skin oil.
Example 9 A face de-oiling stick is prepared according to the following formulation:
Parts Pluronic F-127 (BASF-Wyandotte Corp., Supra) 10.00 sodium stearate 5.00 propylene glycol 20.00 alcohol S~A40 40~C0 lauric acid 1.00 - 10.00 water qs up to 100 parts Mix the propylene glycol, alcohol, sodium stearate, Pluronic F-127 and water in a reflux apparatus and heat to 50C - 60C. Stir until a uniform homogenous system is produced. Then add with constant stirring the lauric acid as rapidly as possible to avoid any loss of alcohol. The resulting mixture is then cast into a mold and allowed to cool to form a face de-oiling stick.
The face de-oiling stick is intended to absorb oil from the oily skin keeping it oil free for an appreciable period without the fear of causing a dry skin condition.
Example 10 An alternate face de-oiling stick formul~tion may be prepared according to the following:

~L~L4285~

Parts sodium stearate 7.50 propylene glycol 6.00 alcohol SDA~0 70.00 capric acid 1.00 - 10.00 water qs up to 100 parts Mix the propylene glycol, alcohol, sodium stearate ~; and water in a reflux apparatus and heat to 50 - 60C. Stir until a uniform homogenous system is produced. Then add with 1~0 constant stirring the capric acid as rapidly as possible to avoid any loss of alcohol. The resulting mixture is then cast into a mold and allowed to cool to form an anti-acne stick.
Example 11 A ~acial cleanser is prepared from the following formula:
; Parts Pluronic F-127 (Supra.) 22.00 Miranol 2MCAS 10.00 propylene glycol 15.00 lauric acid 1.00 - 10.00 water qs to 100 parts Mix the Pluronic, Miranol and propylene glycol. Heat the mixture to 60C. and continue stirring until a homogenous mixture results. Then slowly add the lauric acid with constant stirring. When thoroughly blended, add water to the resulting mixture and continue stirring while allowing the mixture to cool down to 30 QC . The mixture is then allowed to cool to room temperature.
The facial cleanser so prepared may be applied one to three times daily to facial skin to remove excess sebum.

~2~35~1~

* Trademark for an equimolar muxture of:
2-cocoyl - l (sodium carboxymethyl) - l, [2 - (sodium carboxy-methoxy) ~ ethyl] - 2 - imidazolinium lauryl sulfate and 2 - cocoyl - l (sodium carboxymethyl) - l, ~2 - (sodium carboxy-methoxy) - ethyl] - 2 - imidazolinium polyoxy - ethylene - (3) -dodecyl sulfate.
Example 12 A series of night creams are prepared according to the follcwing formulation:

Parts Formula A B C D
triethanolamane 1.50 1.50 1.50 1.50 stearic acid 3.00 3.00 3.00 3.00 propylene glycol 15.00 30.00 30.00 30.00 Edenol 302 ** 5.00 5.00 5.00 5.00 Tetronic 1508 *** 20.00 lO.00 lO.00 5.00 capric ad d l.00 2.00 5.00 10.00 water qs qs qs qs ** Trademark for a diester of short chained fatty acids.
*** Trademark for a tetrafunctional polyo~yalkylene polyether block copolymer derivative of ethylenediamine, M.W. 27,000 E~SF-Wyandotte Corporation, Wyandotte, Michigan.
In each of the formulae A-D, mLx the stearic acid, Edenol, Tetronic, propylene glycol together and then heat the resulting mixture to 75C. This constitutes the oil phase.
Mix the water and triethanolamine together and heat to 75& . mis constitutes the water phase.
Add the oil phase to the water phase at 75&. to prepare an emul-sion. When emulsion is ccmpleted, add the _,~j,, ~.

capric acid slowly with constant stirring.
The creams A-D may be applied to excessively oily skin or to dry skin having patches of oiliness, once in the evening before retiring to alleviate the condition.
Example 13 A shampoo may be formulated of the following:
Parts Pluronic L64 * 28.00 Miranol 2MCAS (Example 11, Supra.) 40.00 -lauric acid 1.00 - 10.00 water qs. to 100 parts * Polyoxyethylene polyoxypropylene polyoxyethylene block copolymer - average molecular weight of 2900 (BASF-Wyandotte Corporation, Wyandotte, Michigan).
The Pluronic L64, Miranol 2MAS and lauric acid is mixed at room temperature until the mass is thoroughly mixed and homogenous. The water is then added until the entire product is smoothly uniformr The shampoo so obtained may be used two or three times a week to control seborrheic scalps.

Claims (4)

THE EMBODIMENTS OF THE INVENTION IN WHICH AN EXCLUSIVE
PROPERTY OR PRIVILEGE IS CLAIMED ARE DEFINED AS FOLLOWS:
1. A composition for cosmetically treating the physical manifestations of oily skin resulting from seborrhea in humans, comprising a fatty acid selected from the group consisting of polargonic, capric, n-undecyclic, lauric and n-tridecyclic acid dispersed in a topical application carrier which is non-toxic and non-irritating to the skin, the fatty acid being present in an amount which, when the composition is applied to the skin affected with seborrhea, is effective to reduce excess sebaceous secretions of seborrhea on the affected skin surface.
2. A composition as recited in claim 1, wherein the fatty acid is dispersed in a carrier for facilitating application to the skin which carrier is non-toxic and non-irritating to the skin, the fatty acid constituting 0.1 to 40 percent by weight of the total composition.
3. A composition for cosmetically treating the physical manifestations of oily skin resulting from seborrhea in humans, comprising a fatty acid selected from the group consisting of capric acid and lauric acid and dispersed in a topical application carrier which is non-toxic and non-irritating to the human skin, the fatty acid constituting between 0.1 and 40 percent by weight of the total composition.
4. A composition as recited in claim 1, 2 or 3 wherein the carrier is one selected from the group consisting of ethyl alcohol, isopropyl alcohol, propylene glycol and ethylene glycol.
CA000330577A 1978-06-28 1979-06-26 Method and compositions for the treatment of seborrhea Expired CA1142854A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE2828352A DE2828352C3 (en) 1978-06-28 1978-06-28 Agents for treating seborrheic conditions
DEP2828352.5-41 1978-06-28

Publications (1)

Publication Number Publication Date
CA1142854A true CA1142854A (en) 1983-03-15

Family

ID=6043011

Family Applications (1)

Application Number Title Priority Date Filing Date
CA000330577A Expired CA1142854A (en) 1978-06-28 1979-06-26 Method and compositions for the treatment of seborrhea

Country Status (14)

Country Link
JP (1) JPS559069A (en)
AT (1) AT365450B (en)
BE (1) BE877351A (en)
CA (1) CA1142854A (en)
CH (1) CH641042A5 (en)
CS (1) CS275816B6 (en)
DE (1) DE2828352C3 (en)
DK (1) DK153738C (en)
FR (1) FR2437210A1 (en)
GB (1) GB2024010B (en)
IT (1) IT1124116B (en)
LU (1) LU81429A1 (en)
NL (1) NL7904776A (en)
SE (1) SE7905659L (en)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2912438A1 (en) * 1979-03-29 1980-10-16 Eckert Theodor Topical treatment of skin diseases - with alcoholic soln. of fatty acid
US4406884A (en) * 1981-06-23 1983-09-27 The Procter & Gamble Company Topical antimicrobial composition
EP0116439A3 (en) * 1983-02-02 1986-01-29 Suntory Limited Fatty acid containing hair tonic composition
JPS59175425A (en) * 1983-03-25 1984-10-04 Otsuka Pharmaceut Co Ltd Vessel strengthening agent
DE3603595A1 (en) * 1986-02-06 1987-08-13 Beiersdorf Ag HAIR COSMETIC AGENTS
DE4229737C2 (en) * 1992-09-05 1996-04-25 Beiersdorf Ag Deodorizing cosmetic products containing fatty acids
EP0702950A1 (en) * 1994-09-26 1996-03-27 Beiersdorf Aktiengesellschaft Use of fatty acids against skin superinfections
FR2752421B1 (en) * 1996-08-13 2001-05-04 Fabre Pierre Dermo Cosmetique SALTS OF ANTI-SEBORRHEIC GUANIDINES
US20070142255A1 (en) * 2005-12-16 2007-06-21 Conopco, Inc., D/B/A Unilever Skin benefit composition and a method for using the same
JP5850453B2 (en) * 2012-01-04 2016-02-03 洋一 赤間 External skin analgesics, skin puncture pain relievers and subcutaneous vein vasodilators

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR46241E (en) * 1935-04-03 1936-04-02 Ig Farbenindustrie Ag Cosmetic product
GB801726A (en) * 1956-01-25 1958-09-17 Havva Rabinovitch Improvements in or relating to pharmaceutical preparations
GB1137125A (en) * 1965-12-08 1968-12-18 Unilever Ltd Improved soap products

Also Published As

Publication number Publication date
DE2828352B2 (en) 1980-09-25
BE877351A (en) 1979-10-15
NL7904776A (en) 1980-01-03
SE7905659L (en) 1979-12-29
DK153738B (en) 1988-08-29
AT365450B (en) 1982-01-11
FR2437210B1 (en) 1983-02-18
CS439379A3 (en) 1992-03-18
IT1124116B (en) 1986-05-07
DE2828352A1 (en) 1980-01-17
DK271279A (en) 1979-12-29
CH641042A5 (en) 1984-02-15
FR2437210A1 (en) 1980-04-25
DK153738C (en) 1989-01-09
ATA419279A (en) 1981-06-15
JPS559069A (en) 1980-01-22
GB2024010A (en) 1980-01-09
GB2024010B (en) 1982-11-10
LU81429A1 (en) 1979-10-30
CS275816B6 (en) 1992-03-18
DE2828352C3 (en) 1981-08-20
IT7912655A0 (en) 1979-06-27

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