WO1995003811A1 - Therapeutic skin composition - Google Patents

Therapeutic skin composition Download PDF

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Publication number
WO1995003811A1
WO1995003811A1 PCT/US1994/008549 US9408549W WO9503811A1 WO 1995003811 A1 WO1995003811 A1 WO 1995003811A1 US 9408549 W US9408549 W US 9408549W WO 9503811 A1 WO9503811 A1 WO 9503811A1
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WO
WIPO (PCT)
Prior art keywords
weight
acid
stearate
alpha hydroxy
skin cream
Prior art date
Application number
PCT/US1994/008549
Other languages
French (fr)
Inventor
Jinger Heath
Clifton Sanders
John H. Murphy
Rhonda Atkins
Original Assignee
Beauticontrol Cosmetics, Inc.
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 Beauticontrol Cosmetics, Inc. filed Critical Beauticontrol Cosmetics, Inc.
Publication of WO1995003811A1 publication Critical patent/WO1995003811A1/en

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Classifications

    • 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
    • A61K8/365Hydroxycarboxylic acids; Ketocarboxylic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • 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
    • A61K8/40Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/44Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/007Preparations for dry skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/08Anti-ageing preparations
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/74Biological properties of particular ingredients
    • A61K2800/75Anti-irritant

Abstract

Therapeutic and preventive compositions that treat dull, dry and rough skin, improve skin smoothness and elasticity, diminish fine lines and wrinkles, prevent acne and promote renewed skin vibrance. The compositions include an alpha hydroxy acid and a preservative.

Description

THERAPEUTIC SKIN COMPOSITION
FIELD OF THE INVENTION
The present invention relates generally to topical applications for human skin conditions and more specifically to therapeutic and preventive compositions that treat dull, dry and rough skin, exfoliate skin, improve skin smoothness and elasticity, diminish fine lines and wrinkles, prevent acne and promote renewed skin vibrance. BACKGROUND OF THE INVENTION
It is well known in the art that alpha hydroxy acids are useful in the treatment of various skin maladies such as dry skin, ichthyosis, eczema, palmar keratoses, plantar keratoses, dandruff, acne, warts, herpes, pruritis, psoriasis, age spots, wrinkles and disturbed keratinization. Repeated application of topical formulations including alpha hydroxy acids, however, has undesirably resulted in mild to sometimes severe skin irritation. The cause of the skin irritation is likely attributable to a lowering of the pH of the skin. As mentioned in U.S. Patent No. 5,091,171 to Yu et al., the upper layers of normal skin have a pH of 4.2 to 5.6 while the compositions containing alpha hydroxy acids typically have a pH of less than 3.0. Repeated topical application of such compositions can cause a decrease in the pH of the skin. Various attempts have been made to overcome this drawback of alpha hydroxy acids but such attempts largely have been unsuccessful. For instance, the alpha hydroxy acids have been reacted with organic primary, secondary or tertiary alkylamines, alkanol amines, diamines, dialkylamines, dialkanolamines, alkylalkanolamines, trialkylamines, trialkanolamines, dialkyl alkanolamines and alkyl dialkanolamines. For instance, see U.S. Patents Nos. 4,234,599, 4,197,316, 4,021,572, 4,105,782 and 4,105,783. The products of such reactions, however, lose most of their therapeutic effects, probably because the penetration and distribution of the active ingredient to the target site in the skin is greatly diminished. SUMMARY OF THE INVENTION
The foregoing problems are solved and a technical advance is achieved by therapeutic skin compositions comprising an alpha hydroxy acid and a preservative comprising sodium hydroxymethylglycinate.
In preferred embodiments, the compositions include one or more alpha hydroxy acids selected from glycolic acid, citric acid, lactic acid, malic acid, tartronic acid, tartaric acid and glucuronic acid.
In other preferred embodiments, the compositions include one or more alpha hydroxy acids selected from citric acid, lactic acid and tartaric acid.
The compositions of the present invention are provided in a cream base that also includes additional preservatives to increase the shelf life of the compositions.
A technical advantage achieved with compositions of the present invention is that the compositions treat dull, dry and rough skin, exfoliate skin, improve skin smoothness and elasticity, diminish fine lines and wrinkles, prevent acne and promote renewed skin vibrance without the concomitant skin irritation associated with other alpha hydroxy acid compositions. DESCRIPTION OF THE PREFERRED EMBODIMENTS
The composition of the present invention comprises one or more alpha hydroxy acids selected from glycolic acid, citric acid, lactic acid, malic acid, tartronic acid, tartaric acid and glucuronic acid. Preferably, the compositions include one or more alpha hydroxy acids selected from citric acid, lactic acid and tartaric acid. In a preferred embodiment, the composition includes a triple alpha hydroxy acid complex including lactic acid, citric acid and tartaric acid in a concentration of from about 0.05 weight % up to about 15.00 weight % and a concentration of from about 0.01 weight % up to about 15.00 weight % of a composition comprising about 28.00 weight % to about 35.00 weight % of lactic acid.
A suitable source of a triple alpha hydroxy acid complex including lactic acid, citric acid and tartaric acid is Lemon/Passion Fruit Complex™ which is commercially available from Centerchem. A suitable source of a composition comprising about 28.00 weight % to about 35.00 weight % of lactic acid is Biolac™ which consists of about 28.00 weight % to about 35.00 weight % of lactic acid and about 65.00 weight % to about 72.00 weight % of inert ingredients and is commercially available from Barnet Products.
Sodium hydroxymethylglycinate is provided in the composition to neutralize the alpha hydroxy acid and reduce skin irritation. The sodium hydroxymethylglycinate may be provided in a concentration of from about 0.20 weight % to about 1.50 weight %.
A suitable source of sodium hydroxymethylglycinate is Suttocide A® which is commercially available from Sutton Labs, a division of ISP Technology Inc.
Although a simple solution of the alpha hydroxy acids and the sodium hydroxymethylglycinate in water is effective as a skin treating composition according to the present invention, various well known and conventional topical cosmetic carriers such as suspending agents, thickeners, humectants, preservatives, emollients, emulsifiers, film formers and fragrant oils are provided for cosmetic effects and/or to improve the physical consistency of the formulation and to serve as a diluent for the alpha hydroxy acids and the sodium hydroxymethylglycinate.
The compositions of the present invention may include a suspending agent such as magnesium aluminum silicate in a concentration of from about 0.20 weight % to about 2.00 weight %. A suitable source of magnesium aluminum silicate is Veegum® which is commercially available from R.T. Vanderbilt Company, Inc.
The compositions of the present invention may include one or more thickeners such as hydroxyethylcellulose in a concentration of from about 0.05 weight % to about 0.50 weight %, xanthan gum in a concentration of from about 0.01 weight % to about 0.70 weight % and stearyl alcohol in a concentration of from about 0.50 weight % to about 5.00 weight %. A suitable source of hydroxyethylcellulose is Natrosol® 250 which is commercially available from Aqualon Company. A. suitable source of xanthan gum is Keltrol® which is commercially available from Kelco. A suitable source of stearyl alcohol is commercially available from Sherex Chemical Company.
The compositions of the present invention may include a humectant such as propylene glycol U.S.P. in a concentration of from about 1.00 weight % to about 8.00 weight %. A suitable source of propylene glycol USP is B.A. S.F.
The compositions of the present invention may include one or more preservatives such as phenoxyethanol in a concentration of from about 0.01 weight % to about 0.50 weight % and benzyl alcohol in a concentration of from about 0.01 weight % to about 1.00 weight %. A suitable source of phenoxyethanol is Phenoxetol® which is commercially available from Nipa Laboratories, Ltd. Benzyl alcohol is commercially available from Creative Fragrances. The preservatives are provided to improve the shelf life of the compositions.
The compositions of the present invention may include one or more emollients such as caprylic capric triglyceride in a concentration of from about 1.00 weight % to about 12.00 weight %, isopropyl palmitate in a concentration of from about 1.00 weight % to about 10.00 weight %, dimethicone in a concentration of from about 0.10 weight % to about 4.00 weight %, a branched chain hydrocarbon obtained by hydrogenation of shark liver oil or other natural oils in a concentration of from about 1.00 weight % to about 6.00 weight % and cyclomethicone which is a cyclic dimethyl polysiloxane compound in a concentration of from about 1.00 weight % to about 6.00 weight %. A suitable source of caprylic/capric triglyceride is Myritol® 318 which is commercially available from Caschem Inc. A suitable source of isopropyl palmitate is Wickenol® 111 which is commercially available from Wickhen Products, Inc. A suitable source of dimethicone is Dow Corning® 225 Fluid which is a mixture of fully methylated linear siloxane polymers and blocked with trimethyl siloxane units and which is commercially available from Dow Corning Corporation. A suitable source of a branched chain hydrocarbon obtained by hydrogenation of shark liver oil or other natural oils is Squalane™ which is commercially available from Robeco Chemical. A suitable source of cyclomethicone is commercially available from Dow Corning Corporation. The compositions of the present invention may include one or more emulsifiers such as stearic acid in a concentration of from about 1.00 weight % to about 10.00 weight %, glyceryl stearate/polyethylene glycol 100 stearate in a concentration of from about 2.50 weight % to about 10.00 weight %, cetyl alcohol in a concentration of from about 0.20 weight % to about 4.00 weight %, sorbitan stearate in a concentration of from about 0.20 weight % to about 2.00 weight % and stearyl alcohol and ceteareth-20 in a concentration of from about 0.50 weight % to about 9.00 weight %. A suitable source of stearic acid is Emersol® 132 which is commercially available from Henkel Corporation. A suitable source of glyceryl stearate/polyethylene glycol 100 stearate is Lipomulse 165™ which is commercially available from Lipo Chemicals. A suitable source of cetyl alcohol is Adol® 52 which is commercially available from Sherex Chemical Company. A suitable source of sorbitan stearate is Liposorb S™ which is commercially available from Lipo Chemicals. A suitable source of stearyl alcohol and ceteareth-20 is Promulgen G™ which is commercially available from Amerchol.
The compositions of the present invention may include a film former such as a mixture of liquid hydroxyl terminated polymers and polyethylene glycol in a concentration of from about 1.00 weight % to about 5.00 weight . A suitable source of a mixture of liquid hydroxyl terminated polymers and polyethylene glycol is Polyolprepolymer-2™ which is commercially available from Barnet Products.
The compositions of the present invention may include one or more fragrant oils such as almond oil in a concentration of from about 0.01 weight % to about 0.30 weight % and jasmine oil in a concentration of from about 0.01 weight % to about 0.50 weight %. .Almond Oil is commercially available from Creative Fragrances. A suitable source of jasmine oil is Jasmine Oil 1524-A which is commercially available from Creative Fragrances.
Deionized water may be provided in the compositions of the present invention as an inert carrier which acts as a diluent and which also has some moisturizing properties.
It is understood that the compositions of the present invention may include other conventional and well known topical cosmetic carriers such as suspending agents, thickeners, humectants, preservatives, emollients, emulsifiers, film formers and fragrant oils. It is also understood that the specifically enumerated cosmetic carriers may be freely substituted with other conventional and well known carriers to achieve a desired texture and lubricity of the compositions.
The present invention will now be described in more detail with reference to the following examples. These examples are merely illustrative of the compositions and methods of the present invention and are not intended to be limiting.
EXAMPLE 1
Face and Neck Creme
Phase Material % bv Wt.
A Deionized Water 54.09
Veegum® 0.80
Natrosol® 250 0.20
Propylene Glycol U.S.P. 5.00
Phenoxetol® 0.30
Benzyl Alcohol 0.50
B Myritol® 318 8.00
Emersol® 132 5.00
Wickenol® 111 5.80
Lipomulse 165™ 7.00
Adol® 52 0.60
Liposorb S™ 0.50
Dow Corning® 225 Fluid 1.30
C Biolac™ 10.00
Lemon/Passion Fruit Complex™ 0.10
D Suttocide A® 0.75
E Almond Oil 0.03
Jasmine Oil 1524-A™ 0.03
TOTAL 100.00 The Veegum® and Natrosol® 250 were combined and sifted into the deionized water with high speed mixing in a Lee™ Kettle stainless steel mixing vessel equipped with a Lightnin™ propeller-type mixer. Mixing was continued until an adequately dispersed homogeneous solution was obtained then the propylene glycol was added and the solution was heated to 78°C. When the solution reached a temperature of 78°C. the remainder of the Phase A ingredients were added. The Phase B ingredients were mixed in a side vessel and heated to 80°C. When the Phase A and B solutions reached temperatures of 78°C. and 80°C, respectively, the Phase B solution was added to the Phase A solution and the resultant solution was mixed well until an adequately dispersed homogeneous solution was obtained. The temperature of the solution was then maintained at 75°C. for 10 minutes with mixing. After the expiration of the 10 minute period, the solution was cooled to 40°C. When the solution reached 40°C, Phase C was added and the resultant mixture was mixed well until an adequately dispersed homogeneous solution was obtained. This mixture was cooled to 35°C. at which point Phase D was added. The resultant mixture was mixed well until an adequately dispersed homogeneous mixture was obtained. Finally the composition was cooled to 30°C When the mixture reached 30°C, Phase E was added and the resultant mixture was mixed well until an adequately dispersed homogeneous mixture was obtained.
Clinical trials were conducted to evaluate the changes in human skin condition as a consequence of the topical application of the composition prepared according to this example. According to the clinical trials, 30 panelists were assigned to Group A which received the product of Example 1 while 28 panelists were assigned to Group B which received a placebo. The Group A and Group B panelists were examined after 2 weeks and after 4 weeks of usage of the product of Example 1 and the placebo, respectively. All 30 of the Group A panelists and all 28 of the Group B panelists were examined after 2 weeks while 21 of the Group A panelists and 16 of the Group B panelists were examined after 4 weeks. Table A below shows the results of such examinations. The percentages indicated in Table A for panelists showing improvement after 4 weeks were based on the actual number of panelists examined after 4 weeks of usage of the product of Example 1 or the placebo rather than the total number of panelists in Group A or Group B, respectively.
TABLE A
The Percentage of Panelists Showing Improvement Following Two and Four Weeks of Usage
( 3ROUP A GROUP B
N=30 N=21 N=28 N=16
Skin two four two four Changes weeks weeks weeks weeks
reduced roughness NC* 15% 3.6% NC firmness NC NC NC NC reduced 36.7% 52.6% 25% 6.2% hyperpigmentation reduced appearance 90% 100% 42.9% 6.2% of fine lines reduced appearance 13% 31% 5.6% 6.2% of major lines reduced dryness 36.7% 36.8% 25% 12.5% sallowness 6.7% 10% 7.1% NC
*No change
The results of the clinical trials demonstrate significant positive changes in skin condition in terms of reduced roughness, reduced hyperpigmentation, reduced appearance of fine lines, reduced appearance of major lines and reduced dryness for those panelists receiving the composition according to example 1 when compared to those panelists receiving the placebo composition. - y -
EXAMPLE 2
Hand and Bodv Creme
Phase Material % bv Wt.
A Deionized Water 54.09 Veegum® 0.80 Natrosol® 250 0.20 Propylene Glycol U.S.P. 5.00 Phenoxetol® 0.30 Benzyl Alcohol 0.50
B Myritol® 318 8.00
Emersol® 132 6.00
Wickenol® 111 5.00
Lipomulse 165™ 7.00
Adol® 52 0.80
Liposorb S™ 0.50
Dow Corning® 225 Fluid 1.00
C Lemon/Passion Fruit Complex™ 10.00
D Suttocide A® 0.75
E Almond Oil 0.03 Jasmine Oil 1524-A™ 0.03
TOTAL 100.0(
The Veegum® and Natrosol® 250 were combined and sifted into the deionized water with high speed mixing in a Lee™ Kettle stainless steel mixing vessel equipped with a Lightnin™ propeller-type mixer. Mixing was continued until an adequately dispersed homogeneous solution was obtained then the propylene glycol was added and the solution was heated to 78°C. When the solution reached a temperature of 78°C. the remainder of the Phase A ingredients were added. The Phase B ingredients were mixed in a side vessel and heated to 80°C. When the Phase A and B solutions reached temperatures of 78βC. and 80°C, respectively, the Phase B solution was added to the Phase A solution and the resultant solution was mixed well until an adequately dispersed homogeneous solution was obtained. The temperature of the solution was then maintained at 75°C. for 10 minutes with mixing. After the expiration of the 10 minute period, the solution was cooled to 40 °C When the solution reached 40°C., Phase C was added and the resultant mixture was mixed well until an adequately dispersed homogeneous solution was obtained. This mixture was cooled to 35°C. at which point Phase D was added. The resultant mixture was mixed well until an adequately dispersed homogeneous mixture was obtained. Finally the composition was cooled to 30°C. When the mixture reached 30°C, Phase E was added and the resultant mixture was mixed well until an adequately dispersed homogeneous mixture was obtained.
Clinical trials were conducted to evaluate the changes in human skin condition as a consequence of the topical application of the composition prepared according to this example. According to the clinical trials, 32 panelists were assigned to Group A which received the product of Example 2 while 28 panelists were assigned to Group B which received a placebo. The Group A and Group B panelists were examined after 2 weeks and after 4 weeks of usage of the product of Example 2 and the placebo, respectively. All 32 of the Group A panelists and all 28 of the Group B panelists were examined after 2 weeks while 21 of the Group A panelists and 16 of the Group B panelists were examined after 4 weeks. Table B below shows the results of such examinations. The percentages indicated in Table B for panelists showing improvement after 4 weeks were based on the actual number of panelists examined after 4 weeks of usage of the product of Example 2 or the placebo rather than the total number of panelists in Group A or Group B, respectively.
TABLE B
The Percentage of Panelists Showing Improvement Following Two and Four Weeks of Usage
< G.ROUP A GROUP B N=32 N=21 N=28 N=16
Skin two four two four Changes weeks weeks weeks weeks
reduced roughness 25% 14.3% 3/6% NC firmness NC NC NC NC reduced 46% 57% 25% 6.2% hyperpigmentation
reduced appearance 81% 90% 42.9% 6.2% of fine lines reduced appearance 31.3% 28.6% 5.6% 6.2% of major lines reduced dryness 31.3% 33.3% 25% 12.5% sallowness 15.6% 9.6% 7.1% NC
*No change
The results of the clinical trials demonstrate significant positive changes in skin condition in terms of reduced roughness, reduced hyperpigmentation, reduced appearance of fine lines, reduced appearance of major lines and reduced dryness for those panelists receiving the composition according to example 2 when compared to those panelists receiving the placebo composition.
EXAMPLE 3
7% lactic Acid Creme
Seq. Material % bv Wt. Grams
A Deionized Water 62.60 313.00
Propylene Glycol U.S.P. 4.00 20.00
Xanthan Gum 0.50 2.50
Phenoxetol® 0.30 1.50
Benzyl Alcohol 0.50 2.50
B Squalane™ 4.00 20.00
Polyolprepolymer-2™ 3.00 15.00
Myritol® 318 5.00 25.00
Emersol® 132 3.20 16.00
Cyclomethicone 4.00 20.00
Dow Corning® 225 Fluid 1.00 5.00
Promulgen G™ 1.85 9.25
Lipomulse 165™ 2.30 11.50
C Biolac™ 7.00 35.00
D Suttocide A® 0.75 3.75
TOTAL 500.00
The xanthan gum was sifted into the deionized water with high speed mixing in a Lee™ Kettle stainless steel mixing vessel equipped with a Lightnin™ propeller-type mixer. Mixing was continued until an adequately dispersed homogeneous solution was obtained and then the remainder of the Phase A ingredients were added. This mixture was heated to 75°C. The Phase B ingredients were mixed in a side vessel and heated to 75°C. When the Phase A and B solutions reached a temperature of 75 °C, the Phase B solution was added to the Phase A solution and the resultant solution was mixed well until an adequately dispersed homogeneous solution was obtained. The temperature of the solution was then maintained at 70°C. for 10 minutes with mixing. After the expiration of the 10 minute period, the solution was cooled to 40°C. When the solution reached 40°C., Phase C was added and the resultant mixture was mixed well -until an adequately dispersed homogeneous solution was obtained. This mixture was cooled to 35°C. at which point Phase D was added. The resultant mixture was mixed well until an adequately dispersed homogeneous mixture was obtained. Finally the composition was cooled to 30°C.
EXAMPLE 4 15% Lactic Acid Creme
Seq. Material % bv Wt. Grams
A Deionized Water 50.05 1501.50 Phenoxetol® 0.30 9.00 Benzyl Alcohol 0.50 15.00 Propylene Glycol U.S.P. 4.00 120.00 Xanthan Gum 0.80 24.00
B Adol® 52 2.00 60.00 Squalane 4.00 120.00
Polyolprepolymer-2 3.00 90.00 Myritol® 318 5.00 150.00 Emersol® 132 3.80 114.00 Cyclomethicone 4.00 120.00 Dow Corning® 225 Fluid 1.20 36.00 Promulgen G 2.30 69.00 Lipomulse 165™ 2.50 75.00 Stearyl Alcohol 0.80 24.00
C Biolac™ 15.00 450.00
D Suttocide A® 0.75 22.50
TOTAL 3000.00
The deionized water was heated to 80°C. and the phenoxyethanol and the benzyl alcohol were added to the deionized water and mixed at high speed in a Lee™ Kettle stainless steel mixing vessel equipped with a Lightnin™ propeller-type mixer. Mixing was continued until an adequately dispersed homogeneous solution was obtained and then the remainder of the Phase A ingredients were added. This mixture was heated to 75°C. The Phase B ingredients were mixed in a side vessel and heated to 75°C. When the Phase A and B solutions reached a temperature of 75 °C., the Phase B solution was added to the Phase A solution and the resultant solution was mixed well until an adequately dispersed homogeneous solution was obtained. The temperature of the solution was then maintained at 70°C for 10 minutes with mixing. After the expiration of the 10 minute period, the solution was cooled to 40°C. When the solution reached 40°C., Phase C was added and the resultant mixture was mixed well until an adequately dispersed homogeneous solution was obtained. This mixture was cooled to 35°C. at which point Phase D was added. The resultant mixture was mixed well until an adequately dispersed homogeneous mixture was obtained. Finally the composition was cooled to 30°C.
EXAMPLE 5 Neutralization of Alpha hydroxy Acids
BIOLAC™ NEUTRALIZATION:
To 3.30 grams of Biolac™ which has a pH of 1.56 (Barnet Lot #8238) were added 4.14 grams of Suttocide A® which has a pH of 10.00 (Sutton Lot #1013330) and the mixture was stirred for 10 seconds. The results of this neutralization process were that the temperature of the mixture was increased by 2°C (from 28 to 30°C) and the pH of the mixture at the end was 5.43. LEMON/PASSION FRUIT™ NEUTRALIZATION:
To 3.60 grams Lemon/Passion Fruit Complex™ which has a pH of 1.28 (Centerchem Lot #320201) were added 4.52 grams Suttocide A® which has a pH of 10.00 (Lot #1013330) and the mixture was stirred for 10 seconds. The results of this neutralization process were that the temperature of the mixture was increased by 2°C (from 28 to 30°C) and the pH of the mixture at the end was 5.03.
The temperature increase and the pH increase involved in the neutralization experiments conducted according to Example 5 may be caused by one of two mechanisms. The most likely possibility is that a neutralization reaction is taking place in which the lactic acid is neutralizing the a ine function of the hydroxymethylglycinate. The other possibility is the formation of a charge transfer complex, which is an extremely stable association between two molecules caused by multiple hydrogen or other non-covalent bonds.
It is understood that the present invention can take many forms and embodiments. The embodiments described herein are intended to illustrate rather than to Umit the invention, it being appreciated that variations may be made without departing from the spirit or the scope of the invention.
Although illustrative embodiments of the invention have been described, a wide range of modification, change and substitution is intended in the foregoing disclosure and in some instances some features of the present invention may be employed without a corresponding use of the other features. Accordingly, it is appropriate that the appended claims be construed broadly and in a manner consistent with the scope of the invention.

Claims

WHAT IS CLAIMED IS:
1. A topical skin cream composition, comprising: a) one or more alpha hydroxy acids; and, b) sodium hydroxymethylglycinate.
2. A topical skin cream composition according to claim 1, wherein said composition comprises one or more alpha hydroxy acids selected from the group consisting of glycolic acid, citric acid, lactic acid, malic acid, tartronic acid, tartaric acid and glucuronic acid.
3. A topical skin cream composition according to claim 1, wherein said composition comprises one or more alpha hydroxy acids selected from the group consisting of citric acid, lactic acid and tartaric acid.
4. A topical skin cream composition according to claim 1 wherein said alpha hydroxy acid comprises lactic acid.
5. A topical skin cream composition, comprising: a) from about 0.05% to about 15.00% by weight of an alpha hydroxy acid complex comprising citric acid, lactic acid and tartaric acid; b) from about 0.01% to about 15.00% by weight of a composition comprising about 28.00% to about 35.00% by weight of lactic acid; c) from about 0.20% to about 1.50% by weight of sodium hydroxymethylglycinate; and d) a diluent or carrier for the composition comprising one or more compounds selected from the group consisting of water, suspending agents, thickeners, humectants, preservatives, emollients, emuslsifiers, film formers and fragrant oils. 6. A topical skin cream composition according to claim 5, wherein said diluent or carrier comprises: a) a suspending agent comprising between about 0.20% and 2.00% by weight of magnesium aluminum silicate; b) at least one thickener comprising between about 0.05% and 0.50% by weight of hydroxyethylcellulose, between about 0.01% and 0.70% by weight of xanthan gum and between about 0.50% and 5.00% by weight of stearyl alcohol; c) a humectant comprising between about 1.00% to about 8.00% by weight of propylene glycol; d) at least one preservative comprising between about 0.01% to 0.50% by weight of phenoxyethanol and between about 0.01% to 1.00% by weight of benzyl alcohol; e) at least one emollient comprising between about 1.00% and 12.00% by weight of capryHc capric triglyceride, between about 1.00% and 10.00% by weight of isopropyl palmitate, between about 0.10% and 4.00% by weight of dimethicone, between about 1.00% and 6.00% by weight of a saturated branched chain hydrocarbon obtained by hydrogenation of shark hver oil or other natural oils and between about 1.00% and 6.00% by weight of cychc dimethyl polysiloxane; f) at least one emulsifier comprising between about 1.00% and 10.00% by weight of stearic acid, between about 2.50% and 10.00% by weight of glyceryl stearate/polyethylene glycol 100 stearate, between about 0.20% and 4.00% by weight of cetyl alcohol, between about 0.20% and 2.00% by weight of sorbitan stearate and between about 0.50% and 9.00% by weight of stearyl alcohol and ceteareth-20; g) a film former comprising between about 1.00% and 5.00% by weight of a mixture of liquid hydroxyl terminated polymers and polyethylene glycol; h) at least one fragrant oil comprising between about 0.01% and 0.30% by weight of almond oil and between about 0.01% and 0.50% by weight of jasmine oil; and i) water forming the balance.
7. A topical skin cream composition according to claim 5, wherein said diluent or carrier comprises: a) a suspending agent comprising between about 0.20% and 2.00% by weight of magnesium aluminum silicate; b) a thickener comprising between about 0.05% and 0.50% by weight of hydroxyethylcellulose; c) a humectant comprising between about 1.00% to about 8.00% by weight of propylene glycol; d) at least one preservative comprising between about 0.01% to 0.50% by weight of phenoxyethanol and between about 0.01% to 1.00% by weight of benzyl alcohol; e) at least one emollient comprising between about 1.00% and 12.00% by weight of caprylic/capric triglyceride, between about 1.00% and 10.00% by weight of isopropyl palmitate and between about 0.10% and 4.00% by weight of dimethicone; ϊ) at least one emulsifier comprising between about 1.00% and 10.00% by weight of stearic acid, between about 2.50% and 10.00% by weight of glyceryl stearate/polyethylene glycol 100 stearate, between about 0.20% and 4.00% by weight of cetyl alcohol and between about 0.20% and 2.00% by weight of sorbitan stearate; g) at least one fragrant oil comprising between about 0.01% and 0.30% by weight of almond oil and between about 0.01% and 0.50% by weight of jasmine oil; and h) water forming the balance. 8. A topical skin cream composition according claim 7, comprising:
0.10% by weight of said alpha hydroxy acid complex comprising citric acid, lactic acid and tartaric acid;
10.00% by weight of said composition comprising 28.00% to about 35.00% by weight of lactic acid;
0.75% by weight of said sodium hydroxymethylglycinate;
0.80% by weight of said magnesium aluminum silicate;
0.20% by weight of said hydroxyethylcellulose;
8.00% by weight of said propylene glycol;
0.30% by weight of said phenoxyethanol;
0.50% by weight of said benzyl alcohol;
8.00% by weight of said caprylic/capric triglyceride;
5.80% by weight of said isopropyl palmitate;
1.30% by weight of said dimethicone;
5.00% by weight of said stearic acid;
7.00% by weight of said glyceryl stearate/polyethylene glycol 100 stearate;
0.60% by weight of said cetyl alcohol;
0.50% by weight of said sorbitan stearate;
0.03% by weight of said almond oil;
0.03% by weight of said jasmine oil; and
54.09% of said deionized water.
9. A tropical skin cream composition according to claim 7, comprising:
10.00% by weight of said alpha hydroxy acid complex comprising citric acid, lactic acid and tartaric acid;
0.75% by weight of said sodium hydroxymethylglycinate;
0.80% by weight of said magnesium aluminum silicate;
0.20% by weight of said hydroxyethylcellulose;
5.00% by weight of said propylene glycol;
0.30% by weight of said phenoxyethanol;
0.50% by weight of said benzyl alcohol;
8.00% by weight of said caprylic/capric triglyceride;
5.00% by weight of said isopropyl palmitate;
1.00% by weight of said dimethicone;
6.00% by weight of said stearic acid;
7.00% by weight of said glyceryl stearate/polyethylene glycol 100 stearate;
0.80% by weight of said cetyl alcohol;
0.50% by weight of said sorbitan stearate;
0.30% by weight of said almond oil;
0.03% by weight of said jasmine oil; and
54.09% of said deionized water.
PCT/US1994/008549 1993-07-30 1994-07-27 Therapeutic skin composition WO1995003811A1 (en)

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