CA1336762C - Method and composition for treating and preventing dry skin disorders - Google Patents
Method and composition for treating and preventing dry skin disordersInfo
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- CA1336762C CA1336762C CA 608066 CA608066A CA1336762C CA 1336762 C CA1336762 C CA 1336762C CA 608066 CA608066 CA 608066 CA 608066 A CA608066 A CA 608066A CA 1336762 C CA1336762 C CA 1336762C
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
- A61Q19/007—Preparations for dry skin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/20—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/66—Phosphorus compounds
- A61K31/683—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
- A61K31/685—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/36—Carboxylic acids; Salts or anhydrides thereof
- A61K8/361—Carboxylic acids having more than seven carbon atoms in an unbroken chain; Salts or anhydrides thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/55—Phosphorus compounds
- A61K8/553—Phospholipids, e.g. lecithin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/63—Steroids; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/68—Sphingolipids, e.g. ceramides, cerebrosides, gangliosides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
- A61K8/98—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution of animal origin
- A61K8/981—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution of animal origin of mammals or bird
- A61K8/985—Skin or skin outgrowth, e.g. hair, nails
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
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- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Birds (AREA)
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- Pharmacology & Pharmacy (AREA)
- Chemical & Material Sciences (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Dermatology (AREA)
- Emergency Medicine (AREA)
- Zoology (AREA)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
A method and composition for treating and preventing dry skin includes a lipid concentrate blended from a combination of the three naturally-occurring lipid groups found in the stratum corneum. The concentrate may be applied topically as prepared, or may be blended with a therapeutically acceptable vehicle suitable for topical application.
Description
METHOD AND COMPOSITION FOR
TREATING AND PREVENTING DRY SKIN DISORDERS
This invention relates generally to dermatological preparations and, more particularly, to methods and compositions for treating and preventing dry skin.
Background of the Invention Dry skin, also known as xerosis or asteatosis affects millions of Americans each year. Attempts to treat or prevent dry skin have led to the development of a large assortment of skin creams and lotions. All of these creams and lotions have been developed from either the point of view that applying an occlusive lipid such as petrolatum or mineral oil can retard moisture loss from the skin, or that the incorporation of water-soluble materials, such as free amino acids, organic acids, inorganic ions or urea, into the cream, ointment, gel or lotion can trap or retain water in the skin.
It has been demonstrated over the last few years that the stratum corneum of the skin contains certain lipids which may form complicated layers within the stratum corneum thus forming a "water barrier" which prevents water loss from the skin. It has been discovered that formulations may be prepared composed of components of the skin's natural water barrier forming lipid complex and that when these formulations are used by themselves or when they are incorporated into creams, ointments, gels and lotions, the resulting products provide unsurpassed protection against and treatment for dry skin conditions.
D
~ 1336762 ' la - 28268-1 In preparing the formulations disclosed herein, combinations of components from three separate classes of stratum corneum lipids were utilized: (1) fatty acids;
TREATING AND PREVENTING DRY SKIN DISORDERS
This invention relates generally to dermatological preparations and, more particularly, to methods and compositions for treating and preventing dry skin.
Background of the Invention Dry skin, also known as xerosis or asteatosis affects millions of Americans each year. Attempts to treat or prevent dry skin have led to the development of a large assortment of skin creams and lotions. All of these creams and lotions have been developed from either the point of view that applying an occlusive lipid such as petrolatum or mineral oil can retard moisture loss from the skin, or that the incorporation of water-soluble materials, such as free amino acids, organic acids, inorganic ions or urea, into the cream, ointment, gel or lotion can trap or retain water in the skin.
It has been demonstrated over the last few years that the stratum corneum of the skin contains certain lipids which may form complicated layers within the stratum corneum thus forming a "water barrier" which prevents water loss from the skin. It has been discovered that formulations may be prepared composed of components of the skin's natural water barrier forming lipid complex and that when these formulations are used by themselves or when they are incorporated into creams, ointments, gels and lotions, the resulting products provide unsurpassed protection against and treatment for dry skin conditions.
D
~ 1336762 ' la - 28268-1 In preparing the formulations disclosed herein, combinations of components from three separate classes of stratum corneum lipids were utilized: (1) fatty acids;
(2) sterols and sterol esters; and (3) phospholipids and glycolipids.
D
13367~2 Summary of the Invention The present invention provides an improved method and composition for prophylaxis for or treatment of dry skin, consisting of preparing a formulation composed of representative lipids from the three classes of lipids naturally found in the stratum corneum. Such a formulation may be applied directly or may be incorporated into a cream, ointment, gel or lotion and the resulting product applied in order to prevent or treat dryness of the skin.
Accordingly, the present invention provides a method for prophylaxis or treatment of dry skin, said method comprising topical application to the skin of a concentrate of one or more constituents from each of the three classes of naturally-occurring stratum corneum lipids.
The present invention also provides a lipid concentrate for the prophylaxis and treatment of dry skin, said concentrate comprising at least one constituent from each of the following groups of naturally-occurring stratum corneum lipids: fatty acids, sterols and sterol esters, and phospholipids and glycolipids.
The present invention further provides a pharmaceutical composition comprising the concentrate as described above and a pharmaceutically acceptable vehicle suitable for topical application of said concentrate.
The present invention yet also provides a use of the above described concentrate or composition for the prophylaxis or treatment of dry skin.
B
_ 1336762 2a ~ 28268-1 The present invention also provides a commercial ingredient, a concentrate or composition as described above together with instructions for the use thereof for the prophylaxis or treatment of dry skin.
DETAILED DESCRIPTION OF PREFERRED EMBODIMENTS
While other lipids may be utilized, the following members of the three stratum corneum lipid classes combined under this invention have been successfully utilized:
This invention provides a lipid concentrate for the prophylaxis or treatment of dry skin, said concentrate comprising at least one constituent from each of the following groups of naturally-occurring stratum corneum lipids: a fatty acid, a sterol or sterol ester, and a phospholipid or glycolipid, said fatty acid being present in a proportion of about 25% to about 75% by weight of concentrate, said fatty acid preferably being selected as one or more of the group consisting of arachidonic acid, linoleic acid, linolenic acid, palmitic acid, stearic acid, oleic acid and docosanoic acid; said sterol or sterol ester being present in a proportion of about 10% to about 40% by weight of concentrate, said sterol or sterol ester preferably being selected as one or more of the group consisting of cholesterol and cholesterol sulfate, and said phospholipid or glycolipid preferably being present in a proportion from about 5% to about 40% by weight of concentrate, said phospholipid or glycolipid preferably being selected as one or more of the group consisting of a ceramide, lecithin and cephalin.
t D
2b 28268-1 The fatty acids may be present as free acids or triglycerides or a mixture thereof.
This invention also provides the use of a concentrate of naturally occurring stratum corneum lipids for prophylaxis or treatment of dry skin said concentrate comprising:
(a) a fatty acid in a proportion of about 25% to about 75%
by weight of concentrate, said fatty acid being in triglyceride form, free form or a mixture thereof and preferably selected as one or more of the group consisting of arachidonic acid, linoleic acid, linolenic acid, palmitic acid, stearic acid, oleic acid and docosanoic acid;
(b) a sterol or sterol ester in a proportion of about 10%
to about 40% by weight of concentrate, said sterol or sterol ester preferably being selected as one or more of the group consisting of cholesterol and cholesterol sulfate; and (c) a phospholipid or glycolipid in a proportion of about 5% to about 40% by weight of concentrate, said phospholipid or glycolipid preferably being selected as one or more of the group consisting of ceramides, lecithin and cephalin.
This invention further provides commercial packages of the concentrate or the composition together with instructions for use thereof for prophylaxis or treatment of dry skin.
1. Fatty acids: arachidonic, linoleic, linolenic, palmitic, stearic, oleic and docosanoic;
2. Sterols and sterol esters: cholesterol and cholesterol sulfate; and 3. Phospholipids and glycolipids: ceramide, lecithin and cephalin.
D`;
. ~ 2c 1336762 28268-1 The proportions of the three classes vary in selected lipid concentrate formulations but generally fall within the following ranges:
Fatty acids: 25 to 75%
Sterols and sterol esters: 10 to 40%
Phospholipids and glycolipids: 5 to 40%
The resulting lipid concentrate formulation may then be added to cream, ointment, gel or lotion vehicles in weight/weight concentrations ranging from about 1% to about 50%.
The following examples further illustrate the invention:
Example 1 A therapeutic skin formula to treat and prevent dry skin was formulated by adding 15 gm of a lipid concentrate composed of 30% W/W cholesterol (obtained under the trade designation Loralan- CH from the Lanaetex Products, Inc., Elizabeth, New Jersey), 20%
W/W lecithin [obtained from American Lecithin Company, Inc., Atlanta Georgia), and 50% W/W of a mixture of linoleic acid, linolenic acid and arachidonic acid (obtained under the trade designation of EFA complex from Phillip Rockley, Ltd., New York, New York) to a lotion base as follows:
Isopropyl Myristate 5.0% 7.5 gm Cetyl Alcohol 2.0% 3.0 gm Glycery~ Stearate and lS PEG-100 Stearate (Arlacel~165) 5.0% 7.5 gm Benzyl Alcohol 1.0% 1.5 gm Lipid Concentrate 10.0% 15.0 gm 70% Sorbitol solution 25.0% 37.5 gm Distilled Water 52.0% 78.0 qm TOTAL 100.0% 150.0 gm This formulation was applied to the dry skin of a 44 year old male and produced noticeably softer more supple skin after only one application.
Example 2 A therapeutic moisturizing formulation was prepared consisting of a lipid concentrate containing 10 ml of linoleic acid (obtained from Emery Industries, Cincinnati, Ohio), 10 ml linolenic acid (obtained from Fluka Chemical Corporation, Ronkonkoma, New York), 10 gm of a mixture of lecithin, cephalin and lipositol (obtained under the trade designation of Asolectin from Fluka Chemical Corporation, Ronkonkoma, New York), and 10 gm of cholesterol (obtained under the trade designation of Loralan- CH from the Lanaetex Products, ~ e- ~a-~
D
13367~2 Summary of the Invention The present invention provides an improved method and composition for prophylaxis for or treatment of dry skin, consisting of preparing a formulation composed of representative lipids from the three classes of lipids naturally found in the stratum corneum. Such a formulation may be applied directly or may be incorporated into a cream, ointment, gel or lotion and the resulting product applied in order to prevent or treat dryness of the skin.
Accordingly, the present invention provides a method for prophylaxis or treatment of dry skin, said method comprising topical application to the skin of a concentrate of one or more constituents from each of the three classes of naturally-occurring stratum corneum lipids.
The present invention also provides a lipid concentrate for the prophylaxis and treatment of dry skin, said concentrate comprising at least one constituent from each of the following groups of naturally-occurring stratum corneum lipids: fatty acids, sterols and sterol esters, and phospholipids and glycolipids.
The present invention further provides a pharmaceutical composition comprising the concentrate as described above and a pharmaceutically acceptable vehicle suitable for topical application of said concentrate.
The present invention yet also provides a use of the above described concentrate or composition for the prophylaxis or treatment of dry skin.
B
_ 1336762 2a ~ 28268-1 The present invention also provides a commercial ingredient, a concentrate or composition as described above together with instructions for the use thereof for the prophylaxis or treatment of dry skin.
DETAILED DESCRIPTION OF PREFERRED EMBODIMENTS
While other lipids may be utilized, the following members of the three stratum corneum lipid classes combined under this invention have been successfully utilized:
This invention provides a lipid concentrate for the prophylaxis or treatment of dry skin, said concentrate comprising at least one constituent from each of the following groups of naturally-occurring stratum corneum lipids: a fatty acid, a sterol or sterol ester, and a phospholipid or glycolipid, said fatty acid being present in a proportion of about 25% to about 75% by weight of concentrate, said fatty acid preferably being selected as one or more of the group consisting of arachidonic acid, linoleic acid, linolenic acid, palmitic acid, stearic acid, oleic acid and docosanoic acid; said sterol or sterol ester being present in a proportion of about 10% to about 40% by weight of concentrate, said sterol or sterol ester preferably being selected as one or more of the group consisting of cholesterol and cholesterol sulfate, and said phospholipid or glycolipid preferably being present in a proportion from about 5% to about 40% by weight of concentrate, said phospholipid or glycolipid preferably being selected as one or more of the group consisting of a ceramide, lecithin and cephalin.
t D
2b 28268-1 The fatty acids may be present as free acids or triglycerides or a mixture thereof.
This invention also provides the use of a concentrate of naturally occurring stratum corneum lipids for prophylaxis or treatment of dry skin said concentrate comprising:
(a) a fatty acid in a proportion of about 25% to about 75%
by weight of concentrate, said fatty acid being in triglyceride form, free form or a mixture thereof and preferably selected as one or more of the group consisting of arachidonic acid, linoleic acid, linolenic acid, palmitic acid, stearic acid, oleic acid and docosanoic acid;
(b) a sterol or sterol ester in a proportion of about 10%
to about 40% by weight of concentrate, said sterol or sterol ester preferably being selected as one or more of the group consisting of cholesterol and cholesterol sulfate; and (c) a phospholipid or glycolipid in a proportion of about 5% to about 40% by weight of concentrate, said phospholipid or glycolipid preferably being selected as one or more of the group consisting of ceramides, lecithin and cephalin.
This invention further provides commercial packages of the concentrate or the composition together with instructions for use thereof for prophylaxis or treatment of dry skin.
1. Fatty acids: arachidonic, linoleic, linolenic, palmitic, stearic, oleic and docosanoic;
2. Sterols and sterol esters: cholesterol and cholesterol sulfate; and 3. Phospholipids and glycolipids: ceramide, lecithin and cephalin.
D`;
. ~ 2c 1336762 28268-1 The proportions of the three classes vary in selected lipid concentrate formulations but generally fall within the following ranges:
Fatty acids: 25 to 75%
Sterols and sterol esters: 10 to 40%
Phospholipids and glycolipids: 5 to 40%
The resulting lipid concentrate formulation may then be added to cream, ointment, gel or lotion vehicles in weight/weight concentrations ranging from about 1% to about 50%.
The following examples further illustrate the invention:
Example 1 A therapeutic skin formula to treat and prevent dry skin was formulated by adding 15 gm of a lipid concentrate composed of 30% W/W cholesterol (obtained under the trade designation Loralan- CH from the Lanaetex Products, Inc., Elizabeth, New Jersey), 20%
W/W lecithin [obtained from American Lecithin Company, Inc., Atlanta Georgia), and 50% W/W of a mixture of linoleic acid, linolenic acid and arachidonic acid (obtained under the trade designation of EFA complex from Phillip Rockley, Ltd., New York, New York) to a lotion base as follows:
Isopropyl Myristate 5.0% 7.5 gm Cetyl Alcohol 2.0% 3.0 gm Glycery~ Stearate and lS PEG-100 Stearate (Arlacel~165) 5.0% 7.5 gm Benzyl Alcohol 1.0% 1.5 gm Lipid Concentrate 10.0% 15.0 gm 70% Sorbitol solution 25.0% 37.5 gm Distilled Water 52.0% 78.0 qm TOTAL 100.0% 150.0 gm This formulation was applied to the dry skin of a 44 year old male and produced noticeably softer more supple skin after only one application.
Example 2 A therapeutic moisturizing formulation was prepared consisting of a lipid concentrate containing 10 ml of linoleic acid (obtained from Emery Industries, Cincinnati, Ohio), 10 ml linolenic acid (obtained from Fluka Chemical Corporation, Ronkonkoma, New York), 10 gm of a mixture of lecithin, cephalin and lipositol (obtained under the trade designation of Asolectin from Fluka Chemical Corporation, Ronkonkoma, New York), and 10 gm of cholesterol (obtained under the trade designation of Loralan- CH from the Lanaetex Products, ~ e- ~a-~
4 13367~2 Inc., Elizabeth, New Jersey). The resulting mixture was blended to make a cream composed as follows:
Isopropyl Myristate5.0% 7.5 gm Cetyl Alcohol 3.0% 4.5 gm Glyceryl stearate and PEG -100 stearate (Arlacel 165) 5.0% 7.5 gm Benzyl Alcohol 1.0% 1.5 gm Lipid Concentrate 5.0% 7.5 gm 70% Sorbitol solution 25.0% 37.5 gm Distilled Water 56.0% 84.0 gm TOTAL 100.0% 150.0 gm This formulation was applied to the very dry skin on the lower legs of a 43 year old woman. Within 24 hours of twice daily application the treated skin was noticeably softer, more moist and supple.
Tests were also performed to assess the efficacy of the present invention in preventing water loss. Baseline measurements of 15 healthy adult test subjects were performed to determine the barrier-forming properties of different formulations of the present invention, and to compare these properties with those of two commercially-available skin creams, Eucerin*, manufactured by Beiersdorf, Inc., Norwalk, Connecicut, and Moisturel*, manufactured by Westwood Pharmaceuticals, Inc. Buffalo, N.Y.. A Servo Med Evaporimeter was used to measure rate of water loss from , ~ a 4.9 cm2~ patch of unprotected skin. Thereafter, formulations of the present invention were applied to the test subjects at separate 4.9 cm2~ test sites, as were applications of Eucerin* and Moisturel* skin creams. Each application consisted of 25 microliters of each formulation.
Lipid Concentrate I consisted of 30% w/w of cholesterol, 20% w/w of lecithin and ceramides, and 50%
w/w of the linoleic, linolenic and arachidonic acid mix.
f~a~e~ k - 13367~2 Lipid Concentrate II consisted of 15% w/w of cholesterol, 10% w/w lecithin and ceramides, and 75% w/w of the linoleic, linolenic and arachidonic acid mix.
The formulations tested were prepared as follows:
Percent by Weiqht Isopropyl Myristate 5.0 Cetyl Alcohol 3.0 Arlacel 165 5.0 Benzyl Alcohol 1.0 Lipid Concentrate II 10.0 70% Sorbitol Solution 25.0 Distilled Water 51.0 TOTAL100.0 Percent by Weight Isopropyl Myristate 5.0 Cetyl Alcohol 3.0 Arlacel 165 5.0 Benzyl Alcohol 1.0 Lipid Concentrate II 5.0 70% Sorbitol Solution 25.0 Distilled Water 56.0 TOTAL 100.0 - 13367~2 Percent by Weight Isopropyl Myristate 5.0 Cetyl Alcohol 3.0 Arlacel 165 5.0 Benzyl Alcohol 1.0 Lipid Concentrate I 10.0 Vitamin E 1.0 70% Sorbitol Solution 25.0 Distilled Water 50.0 TOTAL 100.0 Water loss measurements showed that all five formulations tested reduced water loss as compared to the untreated site, with the formulations of the present invention establishing a stronger barrier to water loss than the commercially available preparations. The test results were as follows:
% change in evaporative water loss Formula 1 3.4 Formula 2 3.5 Formula 3 3.6 EucerinR 3.7 MoisturelR 3.9 Untreated Site 4.5 While the foregoing has presented specific embodiments of the present invention, it is to be understood that these embodiments have been presented by way of example only. It is expected that others will perceive variations which, while varying from the foregoing, do not depart from the spirit and scope of the invention as herein described and claimed. None of the foregoing is attempted to in any manner limit the scope of the present invention.
Isopropyl Myristate5.0% 7.5 gm Cetyl Alcohol 3.0% 4.5 gm Glyceryl stearate and PEG -100 stearate (Arlacel 165) 5.0% 7.5 gm Benzyl Alcohol 1.0% 1.5 gm Lipid Concentrate 5.0% 7.5 gm 70% Sorbitol solution 25.0% 37.5 gm Distilled Water 56.0% 84.0 gm TOTAL 100.0% 150.0 gm This formulation was applied to the very dry skin on the lower legs of a 43 year old woman. Within 24 hours of twice daily application the treated skin was noticeably softer, more moist and supple.
Tests were also performed to assess the efficacy of the present invention in preventing water loss. Baseline measurements of 15 healthy adult test subjects were performed to determine the barrier-forming properties of different formulations of the present invention, and to compare these properties with those of two commercially-available skin creams, Eucerin*, manufactured by Beiersdorf, Inc., Norwalk, Connecicut, and Moisturel*, manufactured by Westwood Pharmaceuticals, Inc. Buffalo, N.Y.. A Servo Med Evaporimeter was used to measure rate of water loss from , ~ a 4.9 cm2~ patch of unprotected skin. Thereafter, formulations of the present invention were applied to the test subjects at separate 4.9 cm2~ test sites, as were applications of Eucerin* and Moisturel* skin creams. Each application consisted of 25 microliters of each formulation.
Lipid Concentrate I consisted of 30% w/w of cholesterol, 20% w/w of lecithin and ceramides, and 50%
w/w of the linoleic, linolenic and arachidonic acid mix.
f~a~e~ k - 13367~2 Lipid Concentrate II consisted of 15% w/w of cholesterol, 10% w/w lecithin and ceramides, and 75% w/w of the linoleic, linolenic and arachidonic acid mix.
The formulations tested were prepared as follows:
Percent by Weiqht Isopropyl Myristate 5.0 Cetyl Alcohol 3.0 Arlacel 165 5.0 Benzyl Alcohol 1.0 Lipid Concentrate II 10.0 70% Sorbitol Solution 25.0 Distilled Water 51.0 TOTAL100.0 Percent by Weight Isopropyl Myristate 5.0 Cetyl Alcohol 3.0 Arlacel 165 5.0 Benzyl Alcohol 1.0 Lipid Concentrate II 5.0 70% Sorbitol Solution 25.0 Distilled Water 56.0 TOTAL 100.0 - 13367~2 Percent by Weight Isopropyl Myristate 5.0 Cetyl Alcohol 3.0 Arlacel 165 5.0 Benzyl Alcohol 1.0 Lipid Concentrate I 10.0 Vitamin E 1.0 70% Sorbitol Solution 25.0 Distilled Water 50.0 TOTAL 100.0 Water loss measurements showed that all five formulations tested reduced water loss as compared to the untreated site, with the formulations of the present invention establishing a stronger barrier to water loss than the commercially available preparations. The test results were as follows:
% change in evaporative water loss Formula 1 3.4 Formula 2 3.5 Formula 3 3.6 EucerinR 3.7 MoisturelR 3.9 Untreated Site 4.5 While the foregoing has presented specific embodiments of the present invention, it is to be understood that these embodiments have been presented by way of example only. It is expected that others will perceive variations which, while varying from the foregoing, do not depart from the spirit and scope of the invention as herein described and claimed. None of the foregoing is attempted to in any manner limit the scope of the present invention.
Claims (24)
1. A lipid concentrate comprising at least one constituent from each of the following groups of naturally-occurring stratum corneum lipids: a fatty acid, a sterol or sterol ester, and a phospholipid or glycolipid, said fatty acid being present in a proportion of about 25% to about 75% by weight of concentrate, said sterol or sterol ester being present in a proportion of about 10% to about 40% by weight of concentrate, and said phospholipid or glycolipid being present in a proportion from about 5% to about 40% by weight of concentrate.
2. A concentrate according to claim 1 wherein said fatty acid is present in triglyceride form.
3. A concentrate according to claim 1 wherein said fatty acid is present in free acid form.
4. A concentrate according to claim 1 wherein said fatty acid is present as a mixture of free acid forms and triglyceride forms.
5. A concentrate according to claim 1 wherein said fatty acid is selected as one or more of the group consisting of arachidonic acid, linoleic acid, linolenic acid, palmitic acid, stearic acid, oleic acid and docosanoic acid.
6. A concentrate according to claim 1 wherein said sterol or sterol ester is selected as one or more of the group consisting of cholesterol and cholesterol sulfate.
7. A concentrate according to claim 1 wherein said phospholipid or glycolipid is selected as one or more of the group consisting of ceramide, lecithin and cephalin.
8. The concentrate of any one of claims 1 to 7 in a composition including a pharmaceutically acceptable vehicle suitable for topical application of said concentrate.
9. The composition of claim 8 wherein said vehicle is selected from the group of creams, gels, lotions and ointments.
10. The composition of claim 8 wherein said lipid concentrate comprises, by weight, about 30% cholesterol, about 20% lecithin and about 50% of a mixture of linoleic acid, linolenic acid and arachidonic acid.
11. The composition of claim 10 wherein said lipid concentrate is present in a weight proportion of about 1% to about 50%.
12. The composition of claim 11 wherein said lipid concentration is present in a weight proportion of about 5% to about 10%.
13. The composition of claim 8 wherein said lipid concentrate comprises, by weight, about 15% cholesterol, about 10% lecithin and ceramides, and about 75% linoleic, linolenic and arachidonic acids.
14. The composition of claim 13 wherein said lipid concentrate is present in a weight proportion of about 1% to about 50%.
15. The composition of claim 14 wherein said lipid concentrate is present in a weight proportion of about 5% to about 10%.
16. The composition of claim 8 wherein said lipid concentrate is present in a weight proportion of about 1% to about 50%.
17. The composition of claim 16 wherein said lipid concentrate is present in a weight proportion of about 5%
to 10%.
to 10%.
18. The use of a concentrate of naturally occurring stratum corneum lipids for prophylaxis or treatment of dry skin said concentrate comprising:
(a) a fatty acid in a proportion of about 25% to about 75%
by weight of concentrate, said fatty acid being in triglyceride form, free form or a mixture thereof;
(b) a sterol or sterol ester in a proportion of about 10%
to about 40% by weight of concentrate; and (c) a phospholipid or glycolipid in a proportion of about 5% to about 40% by weight of concentrate.
(a) a fatty acid in a proportion of about 25% to about 75%
by weight of concentrate, said fatty acid being in triglyceride form, free form or a mixture thereof;
(b) a sterol or sterol ester in a proportion of about 10%
to about 40% by weight of concentrate; and (c) a phospholipid or glycolipid in a proportion of about 5% to about 40% by weight of concentrate.
19. The use according to claim 18 wherein said fatty acid is selected as one or more of the group consisting of arachidonic acid, linoleic acid, linolenic acid, palmitic acid, stearic acid, oleic acid and docosanoic acid.
20. The use according to claim 18 wherein said sterol or sterol ester is selected as one or more of the group consisting of cholesterol and cholesterol sulfate.
21. The use according to claim 18 wherein said phospholipid or glycolipid is selected as one or more of the group consisting of ceramide, lecithin and cephalin.
22. The use of a composition according to any one of claims 9 to 17 for prophylaxis or treatment of dry skin.
23. A commercial package containing, as active ingredient, a concentrate according to any one of claims 1 to 7 together with instructions for use thereof for prophylaxis or treatment of dry skin.
24. A commercial package containing, as active ingredient, a composition according to any one of claims 9 to 17 together with instructions for use thereof for prophylaxis or treatment of dry skin.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US23184888A | 1988-08-12 | 1988-08-12 | |
| US231,848 | 1988-08-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA1336762C true CA1336762C (en) | 1995-08-22 |
Family
ID=22870857
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA 608066 Expired - Lifetime CA1336762C (en) | 1988-08-12 | 1989-08-11 | Method and composition for treating and preventing dry skin disorders |
Country Status (3)
| Country | Link |
|---|---|
| AU (1) | AU4216089A (en) |
| CA (1) | CA1336762C (en) |
| WO (1) | WO1990001323A1 (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8710034B2 (en) | 2000-04-04 | 2014-04-29 | Color Access, Inc. | Method and composition for improving skin barrier function |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8829025D0 (en) * | 1988-12-13 | 1989-01-25 | Le May Edwina J | Veterinary composition |
| DE4022644A1 (en) * | 1990-07-17 | 1992-01-23 | Beiersdorf Ag | SKIN CARE COMBINATIONS |
| GB9124360D0 (en) * | 1991-11-15 | 1992-01-08 | Unilever Plc | Cosmetic compositions |
| CA2087691A1 (en) * | 1992-01-23 | 1993-07-24 | Peter Critchley | Cosmetic compositon |
| US5372814A (en) * | 1992-02-05 | 1994-12-13 | Kao Corporation | Sterol derivative, process for producing the same and dermatologic external preparation |
| CA2137001C (en) * | 1992-06-19 | 1999-05-04 | Peter M. Elias | Lipids for epidermal moisturization and repair of barrier function |
| CA2099188C (en) * | 1992-07-24 | 2005-12-13 | Paul A. Bowser | Use of a cosmetic composition |
| US5310556A (en) * | 1993-06-09 | 1994-05-10 | Chesebrough-Pond's Usa Co., Division Of Conopco, Inc. | Cosmetic composition |
| FR2710527B1 (en) * | 1993-09-30 | 1995-12-08 | Roussel Uclaf | New cosmetic and dermatological compositions combining ceramides and linoleic acid, their preparation. |
| DE4401102A1 (en) * | 1994-01-17 | 1995-07-20 | Henkel Kgaa | Pseudoceramides |
| JP3344822B2 (en) * | 1994-05-02 | 2002-11-18 | 株式会社資生堂 | External preparation for skin |
| SE9402453D0 (en) * | 1994-07-12 | 1994-07-12 | Astra Ab | New pharmaceutical preparation |
| GB9421185D0 (en) * | 1994-10-20 | 1994-12-07 | Unilever Plc | Personal car composition |
| CA2161388A1 (en) | 1994-12-02 | 1996-06-03 | Alexander Znaiden | Cosmetic emulsions with a deposition triggering lipid.system |
| FR2728164B1 (en) * | 1994-12-14 | 1997-03-21 | Oreal | COSMETIC OR DERMATOLOGICAL COMPOSITION CONTAINING A MIXTURE OF CERAMIDS, ITS USE FOR HYDRATING THE SKIN |
| US5552147A (en) * | 1995-04-25 | 1996-09-03 | Chesebrough-Pond's Usa Co., Division Of Conopco, Inc. | Petroleum jelly with alpha hydroxy carboxylic acids |
| US5552148A (en) * | 1995-06-07 | 1996-09-03 | Chesebrough-Pond's Usa Co., Division Of Conopco, Inc. | Petroleum jelly with inositol phosphates |
| DE19523479C1 (en) * | 1995-06-28 | 1996-10-10 | Henkel Kgaa | Synthetic ceramide barrier lipid cpds. for use in skin or hair care prods. e.g. moisturising agents |
| GB9602111D0 (en) * | 1996-02-02 | 1996-04-03 | Unilever Plc | Personal care composition |
| DE19642872C1 (en) * | 1996-10-17 | 1998-02-12 | Henkel Kgaa | Use of sterol sulphate compounds to inhibit serine protease |
| FR2763843B1 (en) * | 1997-05-30 | 1999-08-20 | Marie Pratt | COMPOSITION HAVING PARTICULARLY ANTI-AGING SKIN ACTION |
| DE19744703C1 (en) * | 1997-10-10 | 1999-02-11 | Henkel Kgaa | Phyto-sterol ester useful as emollient agent in skin and hair care formulation |
| DE19751550C2 (en) * | 1997-11-20 | 2001-03-08 | Kao Corp | Use of an active ingredient composition in hair care products |
| EP0943324A3 (en) * | 1998-03-17 | 2002-01-02 | Shiseido Company, Ltd. | External skin treatment composition |
| US20020098207A1 (en) * | 1999-02-08 | 2002-07-25 | Daniel H. Maes | Cholesterol sulfate compositions for enhancement of stratum corneum function |
| TWI225398B (en) * | 1999-07-14 | 2004-12-21 | R Tech Ueno Ltd | Composition for treatment of external secretion disorders |
| US6824785B1 (en) * | 2000-02-09 | 2004-11-30 | C. Neil Kitson | Skin treatment composition and methods of use |
| US20020142013A1 (en) * | 2001-01-31 | 2002-10-03 | Maes Daniel H. | Cholesterol sulfate and amino sugar compositions for enhancement of stratum corneum function |
| SE0102087D0 (en) * | 2001-06-13 | 2001-06-13 | Knut Haadem Med Haadem Invest | Skin preparation |
| GB0517043D0 (en) * | 2005-08-19 | 2005-09-28 | York Pharma Plc | Improvements in pharmaceutical compositions |
| WO2020190015A1 (en) * | 2019-03-21 | 2020-09-24 | 주식회사 리포바이오메드 | Dermally applicable composition having controlled melting point and phase transition temperature of fat molecules, preparation method therefor, and application method thereof |
| CN110179730B (en) * | 2019-06-19 | 2020-07-14 | 广东默默化妆品有限公司 | Repair cream |
| WO2021008678A1 (en) | 2019-07-12 | 2021-01-21 | Symrise Ag | Use of n-acylhydroxy amino acid ester for inducing the expression of superoxide-dismutase and/or hem oxygenase |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5533451A (en) * | 1978-08-30 | 1980-03-08 | Shugo Morita | Preparation of cosmetic |
| JPH0676308B2 (en) * | 1985-06-18 | 1994-09-28 | ポーラ化成工業株式会社 | External skin preparation |
| US4760096A (en) * | 1985-09-27 | 1988-07-26 | Schering Corporation | Moisturizing skin preparation |
-
1989
- 1989-08-09 WO PCT/US1989/003551 patent/WO1990001323A1/en unknown
- 1989-08-09 AU AU42160/89A patent/AU4216089A/en not_active Abandoned
- 1989-08-11 CA CA 608066 patent/CA1336762C/en not_active Expired - Lifetime
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8710034B2 (en) | 2000-04-04 | 2014-04-29 | Color Access, Inc. | Method and composition for improving skin barrier function |
Also Published As
| Publication number | Publication date |
|---|---|
| WO1990001323A1 (en) | 1990-02-22 |
| AU4216089A (en) | 1990-03-05 |
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