Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Cosmetic – antiperspirant – dentifrice
Reexamination Certificate
2000-03-07
2003-03-11
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Cosmetic, antiperspirant, dentifrice
C424S400000, C424S450000, C424S059000, C424S078020, C424S078030, C424S078050, C514S844000, C514S937000, C514S938000
Reexamination Certificate
active
06531141
ABSTRACT:
FIELD OF THE INVENTION
The present invention relates to an oil-in-water emulsion containing tretinoin and the use thereof in mitigating skin disorders such as acne, photodamaged skin, wrinkles, mottled hyperpigmentation, tactile roughness, and yellowing of facial skin.
BACKGROUND OF THE INVENTION
Tretinoin, or all-trans-retinoic acid, is a naturally occurring retinoid and is the major metabolite of Vitamin A. Tretinoin modulates the expression and function of numerous genes by binding to intracellular receptors, termed retinoic acid receptors, both in the cytosol and nucleus. The action of tretinoin at the receptor level accounts for its wide-ranging effects on skin function, and tretinoin acts on many skin cell types. The ability of tretinoin to pharmacologically regulate multiple skin cells likely explains why it decreases fine and coarse wrinkles, reduces melanocytic hyperpigmentation, and improves skin texture (tactile smoothening).
Although the exact mechanism of action is unknown, tretinoin is also the only topical anti-acne agent available by prescription that is believed to be effective against the microcomedo, the precursor to the lesion in acne. Topical tretinoin products ranging in concentration from 0.01% to 0.1% in different vehicles, including an oil-in-water emulsion cream, have been marketed in the United States for the treatment of acne vulgaris under the brand name Retin-A® since 1971.
While the above formulations have been effective in mitigating the above mentioned skin disorders, skin irritation of varying severity may be observed. The present invention, thus, relates to a novel oil-in-water emulsion composition containing tretinoin that has reduced skin irritation properties.
SUMMARY OF THE INVENTION
In one aspect, the invention features an oil-in-water emulsion comprising: (i) about 0.001% to about 1%, by weight, of tretinoin; (ii) about 5% to about 20%, by weight, of caprylic/capric triglyceride; (iii) about 1% to about 10%, by weight, of a C
30
-C
100
polyalkylene glycol ether of a C
10
-C
30
fatty alcohol such as the C
40
polyethylene ether of a C
10
-C
30
fatty alcohol such as steareth-20, isoceteth-20, beheneth-20, oleth-20, ceteth-20, laureth-20, and ceteareth-20; (iv) about 0.1% to about 5%, by weight, of a C
4
-C
30
polyalkylene glycol ether of a C
10
-C
30
fatty alcohol such as the C
4
polyethylene ether of a C
10
-C
30
fatty alcohol such as steareth-2, ceteth-2, laureth-2, and oleth-2, the C
8
polyethylene ethers of a C
10
-C
30
fatty alcohol such as laureth-4, and the C
24
polyethylene ethers of a C
10
-C
30
fatty alcohol such as ceteareth-24; (v) about 0% to about 10%, by weight, of a C
10
-C
30
fatty acid such as stearic acid, capric acid, lauric acid, myristic acid, pentadecanoic acid, palmitic acid, isostearic acid, behenic acid, margaric acid, novadecanoic acid, cerotic acid, montanic acid, and melissic acid) (e.g., the emulsion may not comprise of a C
10
-C
30
fatty acid); (vi) about 1% to about 10%, by weight, of a first C
10
-C
30
fatty alcohol (e.g., cetyl alcohol, decyl alcohol, isodecyl alcohol, lauryl alcohol, isostrearyl alcohol, stearyl alcohol, behenyl alcohol, cetearyl alcohol, myristyl alcohol, and isocetyl alcohol); (vii) about 0% to about 10%, by weight, of a second C
10
-C
30
fatty alcohol; and (viii) about 50% to about 90%, by weight, of water.
The C value before the polyalkylene glycol ether is the average number of carbons in the polyethylene glycol group. In one embodiment, the C
30
-C
100
polyalkylene glycol ether of a C
10
-C
30
fatty alcohol is a hydrophilic compound and the C
4
-C
30
polyalkylene glycol ether of a C
10
-C
30
fatty alcohol is a lipophilic compound.
In one embodiment, the oil-in-water emulsion further comprises: (ix) about 0.1% to about 1%, by weight, of xanthan gum; (x) about 0.001% to about 1%, by weight, of a preservative (e.g., benzyl alcohol or a paraben such as propylparaben, methylparaben, ethylparaben, and butylparaben, sorbic acid, and chlorocresol); (xi) about 0.001% to about 1%, by weight, of an antioxidant (e.g., butylated hydroxytoluene, tocopherols, and ascorbic acid); (xii) about 0.001% to about 1%, by weight, of a chelating agent (e.g., edetate disodium); and (xiii) about 0% to about 1%, by weight, of a fragrance (e.g, Chemoderm 6401B).
In one aspect, the invention features a method of mitigating a skin condition in a human selected from the group consisting of acne, photodamaged skin, wrinkles (e.g., fine wrinkles), mottled hyperpigmentation, tactile roughness, and yellowing of facial skin, the method comprising topically administering to the skin of the human the above oil-in-water emulsion.
Other features and advantages of the present invention will be apparent from the detailed description of the invention and from the claims.
DETAILED DESCRIPTION OF THE INVENTION
It is believed that one skilled in the art can, based upon the description herein, utilize the present invention to its fullest extent. The following specific embodiments are to be construed as merely illustrative and are not limited by the remainder of the disclosure in any way whatsoever.
Unless defined otherwise, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which the invention belongs. Also, all publications, patent applications, patents, and other references mentioned herein are incorporated by reference.
The present invention relates to an oil-in-water emulsion containing tretinoin and the use thereof in mitigating skin disorders such as acne, photodamaged skin, wrinkles, mottled hyperpigmentation, tactile roughness, and yellowing of facial skin. The amount of tretinoin in the emulsion varies depending on the skin condition being treated, the manner of administration, and the age and body weight of the subject.
The compositions of the present invention can be administered topically to a human, e.g., by the direct laying on or spreading of the emulsion on the skin of a human (e.g., daily before retiring). Examples of suitable antioxidants (e.g., ascorbic acid, tocopherols, butylated hydroxyanisole (“BHA”), and butylated hydroxytoluene (“BHT”)), preservatives (e.g., parabens such as methylparaben and propylparaben), and chelating agents (e.g., such as EDTA and edetate disodium) are listed in the International Cosmetic Ingredient Dictionary and Handbook, eds. Wenninger and McEwen, pp. 1612-13, 1626, and 1654-55 (The Cosmetic, Toiletry, and Fragrance Assoc., Washington, D.C., 7
th
Edition, 1997) (hereinafter “ICI Handbook”).
In one embodiment, the emulsion further comprises another dermatologically active agent. What is meant by a “dermatologically active agent” is a compound that has a cosmetic or therapeutic effect on the skin. In one embodiment, the agent is selected from the group consisting of hydroxy acids, benzoyl peroxide, sulfur resorcinol, ascorbic acid, D-panthenol, hydroquinone, sunscreen agents, anti-inflammatory agents, skin lightening agents, antimicrobial and antifungal agents, estrogens, and derivatives and mixtures thereof. The dermatologically active agent will typically be present in the composition of the invention in an amount of from about 0.001% to about 20% by weight of the composition, e.g., about 0.01% to about 10%, e.g., about 0.1% to about 5%.
Examples of hydroxy acids include, but are not limited, to (i) alpha-hydroxy acids such as glycolic acid, lactic acid, malic acid, citric acid, and tartaric acid, (ii) beta-hydroxy acids such as salicylic acid, and/or (iii) polyhydroxy acids. See, e.g., European Patent Application No. 273,202.
Examples of derivatives of ascorbic acid include, but are not limited to, ascorbyl palmitate, magnesium ascorbyl phosphate, sodium ascorbyl phosphate, zinc ascorbyl phosphate, ascorbyl glucoside, sodium ascorbate, and ascorbyl polypeptide. An example of a derivative of hydroquinone includes, but is not limited to, arbutin.
The emulsions of the subject invention may contain, in addition to the aforementioned components, a wide variety of additional oil-solubl
Evans Charesse
McGowan William E.
Ortho-McNeil Pharmaceutical , Inc.
Page Thurman K.
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