Cosmetic compositions

Details Cosmetic compositions Cosmetic compositions

1999-02-12

2001-05-01

Page, Thurman K. (Department: 1615)

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Cosmetic, antiperspirant, dentifrice

C424S078030

Reexamination Certificate

active

06224888

ABSTRACT:

FIELD OF THE INVENTION
The present invention relates to cosmetics containing partially dissolved crystalline vitamin B
3
compounds.
BACKGROUND OF THE INVENTION
Niacin, also known as vitamin B
3
, is the common name for nicotinic acid. The physiologically active form of niacin is niacinamide, also a member of the vitamin B
3
family of compounds. Niacin and niacinamide (nicotinic acid amide) function in the body as components of two coenzymes: nicotinamide adenine dinucleotide (NAD) and nicotinamide adenine dinucleotide phosphate (NADP). Until recently, these vitamin B
3
compounds were used exclusively to treat niacin deficiency and pellegra.
Today, however, vitamin B
3
compounds have also found use in the area of skin care actives. British Patent 1,370,236 describes compositions for skin lightening containing 0.5% to 10% niacin. Similarly, U.S. Pat. No. 4,096,240 discloses the use of 0.1% to 10% niacinamide for skin lightening. Vitamin B
3
compounds have also been found useful in regulating the texture of human skin. See PCT application WO 97/39733, to Oblong et al.
However, when topically applied to the skin, only about 2-4% of the applied vitamin B
3
compound actually penetrates into the skin. Thus, there exists a need for cosmetic compositions comprising vitamin B
3
compounds which provide improved skin penetration of vitamin B
3
compounds. The present inventors have discovered that cosmetic compositions which incorporate vitamin B
3
compounds in a polar solvent such that the vitamin B
3
compound exceeds the saturation solubility of the polar solvent improves the overall skin penetration of the vitamin B
3
compound.
It is, therefore, an aspect of the present invention to provide cosmetic compositions comprising a polar solvent and vitamin B
3
compounds as undissolved crystals.
A further aspect of the present invention is to provide lipstick compositions comprising a polar solvent and vitamin B
3
compounds as undissolved crystals.
These and other aspects will become readily apparent from the detailed description which follows.
SUMMARY OF THE INVENTION
The present invention relates to cosmetic compositions, comprising:
a.) from about 0.01% to about 50%, by weight, of vitamin B
3
compound;
b.) from about 0% to about 90%, by weight, of an emollient component comprising from 0% to about 100%, by weight, of an oil liquid at ambient temperature;
c.) from about 0.01% to about 80%, by weight, of a polar solvent;
d.) from about 0%, to about 90%, by weight, of a surfactant;
e.) from about 0% to about 90%, by weight, of a solidifying agent; and
f.) from about 0% to about 90%, by weight, of a color wherein the vitamin B
3
compound is added to the composition such that the concentration of the vitamin B
3
compound exceeds the saturation solubility of the vitamin B
3
compound in the composition.
All percentages, parts and ratios are based upon the total weight of the cosmetic compositions of the present invention, unless otherwise specified. All such weights as they pertain to listed ingredients are based on the active level and, therefore, do not include carriers or by-products that may be included in commercially available materials, unless otherwise specified.
DETAILED DESCRIPTION OF THE INVENTION
As used herein the term “comprising” means that the composition can contain other ingredients which are compatible with the composition and which preferably do not substantially disrupt the compositions of the present invention. The term encompasses the terms “consisting of” and “consisting essentially of”.
As used herein, the term “cosmetics” includes make-up, foundation, and skin care products. The term “make-up” refers to products that leave color on the face, including foundations, blacks and browns, i.e., mascara, concealers, eye liners, brow colors, eye shadows, blushers, lip colors, and so forth. Skin care products are those used to treat or care for, or somehow moisturize, improve, or clean the skin. Products contemplated by the phrase “skin care products” include, but are not limited to, adhesives, bandages, toothpaste, anhydrous occlusive moisturizers, antiperspirants, deodorants, powder laundry detergent, fabric softener towels, occlusive drug delivery patches, nail polish, powders, tissues, wipes, solid emulsion compact, hair conditioners-anhydrous and the like. The term “foundation” refers to liquid, creme, mousse, pancake, compact, concealer or like product created or reintroduced by cosmetic companies to even out the overall coloring of the skin. Foundation is manufactured to work better over moisturized and/or oiled skin.
ESSENTIAL COMPONENTS
Vitamin B
3
Component
The compositions of the present invention comprise a safe and effective amount of a natural or synthetic vitamin B
3
compound. The compositions of the present invention preferably comprise from above 0.01% to about 50%, more preferably from about 0.1% to about 30%, even more preferably 0.5% to about 20%, more preferably from about 1% to about 10% of the vitamin B
3
compound.
As used herein, “vitamin B
3
compound” means a compound having the formula:
wherein R is —CONH
2
(i.e., niacinamide), —COOH (i.e., nicotinic acid) or —CH
2
OH (i.e., nicotinyl alcohol); derivatives thereof; and salts of any of the foregoing.
Exemplary derivatives of the foregoing vitamin B
3
compounds include nicotinic acid esters, including non-vasodilating esters of nicotinic acid, nicotinyl amino acids, nicotinyl alcohol esters of carboxylic acids, nicotinic acid N-oxide and niacinamide N-oxide.
Suitable esters of nicotinic acid include nicotinic acid esters of C
1
-C
22
, preferably C
1
-C
16
, more preferably c
1
-C
6
alcohols. The alcohols are suitably straight-chain or branched chain, cyclic or acyclic, saturated or unsaturated (including aromatic), and substituted or unsubstituted. The esters are preferably non-rubifacient. As used herein, “non-rubifacient” means that the ester does not commonly yield a visible flushing response after application to the skin in the subject compositions (the majority of the general population would not experience a visible flushing response, although such compounds may cause vasodilation not visible to the naked eye). Alternatively, a nicotinic acid material which is rubifacient at higher doses could be used at a lower dose to reduce the rubifacient effect. Non-rubifacient esters of nicotinic acid include tocopherol nicotinate and inositol hexanicotinate; tocopherol nicotinate is preferred.
Other derivatives of the vitamin B
3
compound are derivatives of niacinamide resulting from substitution of one or more of the amide group hydrogens. Nonlimiting examples of derivatives of niacinamide useful herein include nicotinyl amino acids, derived, for example, from the reaction of an activated nicotinic acid compound (e.g., nicotinic acid azide or nicotinyl chloride) with an amino acid, and nicotinyl alcohol esters of organic carboxylic acids (e.g., C1-C18). Specific examples of such derivatives include nicotinuric acid and nicotinyl hydroxamic acid, which have the following chemical structures:
nicotinuric acid:
nicotinyl hydroxamic acid:
Exemplary nicotinyl alcohol esters include nicotinyl alcohol esters of the carboxylic acids salicylic acid, acetic acid, glycolic acid, palmitic acid and the like. Other non-limiting examples of vitamin B
3
compounds useful herein are 2-chloronicotinamide, 6-aminonicotinamide, 6-methylnicotinamide, n-methyl-nicotinamide, n,n-diethylnicotinamide, n(hydroxymethyl)-nicotinamide, quinolinic acid imide, nicotinanilide, n-benzylnicotinamide, n-ethylnicotinamide, nifenazone, nicotinaldehyde, isonicotinic acid, methyl isonicotinic acid, thionicotinamide, nialamide, 1-(3-pyridylmethyl) urea, 2-mercaptonicotinic acid, nicomol, and niaprazine.
Examples of the above vitamin B
3
compounds are well known in the art and are commercially available from a number of sources, e.g., the Sigma Chemical Company (St. Louis, Mo.); ICN Biomedicals, Inc. (Irvin, Calif.) and Aldrich Chemical Company (Milwaukee, Wis.).
One or more vitamin B
3
compounds may be used herein. Pr

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