Cosmetic preparation with a peptide addition

Details Cosmetic preparation with a peptide addition Cosmetic preparation with a peptide addition

1999-05-28

2001-06-12

Carlson, Karen Cochrane (Department: 1653)

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Cosmetic, antiperspirant, dentifrice

C424S401000, C424S094400, C424S060000, C424S059000, C424S049000, C424S400000, C424S047000, C435S003000, C435S259000, C435S287300, C435S193000, C435S420000, C435S205000, C435S173700, C435S430000, C530S350000, C530S403000, C530S370000, C530S371000, C426S574000, C426S049000, C514S222500

Reexamination Certificate

active

06245342

ABSTRACT:

BACKGROUND OF THE INVENTION
1. Field of the Invention
This invention concerns a new cosmetic preparation containing peptide derivatives derived from &agr;-MSH (melanocyte stimulating hormone) and other active ingredients.
2. The Prior Art
&agr;-MSH has already been investigated by a number of research groups, without so far being able to develop a pharmaceutical drug from it. A specific direction of effect was disclosed in French Patent 2,710,340 A, where certain peptide derivatives derived from &agr;-MSH were described and claimed as active ingredients which stimulate melanogenesis. Topical use against inflammatory reactions of the skin is also described.
SUMMARY OF THE INVENTION
The object of this invention is to develop a new cosmetic preparation especially with melanogenesis-stimulating and anti-inflammatory properties with improved effectiveness.
According to this invention, a cosmetic preparation with a peptide additive consists of a combination of the following active ingredients:
a) a peptide derivative of the formula [Lip]X-His-Phe-Arg-Y, where
Lip stands for thioctic acid or one of its derivatives,
X denotes Glu, OH, or NH
2
,
Y is Trp-Gly-OH,
 Trp-Gly-NH
2
,
 Trp-NH
2
or
 Trp-OH,
Phe is homo-Phe or P-fluoro-Phe,
and the amino acids may be in the form D, L or DL, or mixtures thereof, in a ratio of 0.05 to 2.5 mg pure peptide derivative per kg total weight, where the peptide derivative is associated with xanthine in a ratio of 0.5 to 2 mol per 100 mol peptide;
b) at least 0.5 wt % of a mixture of enzymes and vitamins containing at least 150 units/mL (U/mL) peroxide dismutase;
c) the usual excipients and vehicles in the amount of 65 to 99.5 wt %, and
d) and additional active ingredients in the amount of 0 to 12 wt %.
The percentage amounts are based on the total weight of the cosmetic preparation in each case.
A lipoyl peptide or peptide mixture known from French Patent No. 2,710,340 A was used as the peptide; it has in particular at least one of the following sequences:
I. [(DL)Lip]-Glu-His-D.HomoPhe-Arg-Trp-Gly-NH
2
II. [(DH)Lip]-Glu-His-D.HomoPhe-Arg-Trp-Gly-NH
2
III. [(DL)Lip]-Glu-His-parafluoro-Phe-Arg-Trp-Gly-NH
2
IV. [(DH)Lip]-His-D.HomoPhe-Arg-Trp-Gly-NH
2
V. [N.Lipoyl-lysine]-Glu-His-D.HomoPhe-Arg-Trp-Gly-NH
2
VI. [N.Lipoyl-lysine]-His-D.HomoPhe-Arg-Trp-Gly-NH
2
VII. [N.Lipoyl-lysine]-His-D.HomoPhe-Arg-Trp-NH
2
as well as derivatives of these molecules in the form of salts of the esters or amides, wherein the peptide derivative is mixed with xanthine in a ratio of 0.5 to 2 mol per 100 mol peptide.
In commercial peptides, e.g., MAP® or MAP-X® (from Laboratories Seporga, France), a lipoylaminopeptide of the above peptide derivative, the pure peptide content is about 50 mg/kg, and approximately 0.01 to 5 wt % of this is used in the cosmetic preparation. This yields the above-mentioned peptide content for this invention.
The mixture of enzymes and vitamins used is preferably the digestion product of a yeast prepared by an ultrasonic treatment, with the digestion product containing peroxide dismutase, protease, vitamin B
2
, vitamin B
6
, vitamin B
12
, vitamin D
2
, and vitamin E. It preferably contains at least 150 U/mL peroxide dismutase (POD), protease, and vitamins B and D, with the POD/protease radio in international units being at least in the range of 3:1 to 8:1.
An ultrasonic digestion method, such as that described in German Patent No. 4,241,154 C1 is especially advantageous for preparation of the enzyme/vitamin mixture according to this invention; in this process, a cell dispersion or suspension is passed through an ultrasonic treatment area in an ultrasonic flow-through cell, with the sonotrode extending into the flow-through cell by one-half to two-thirds of its length so that it is submerged in the medium to be treated ultrasonically. The sonotrode here has an angle of 80.5° to 88.5°, and the ratio of the submersion length of the sonotrode in mm to the ultrasonically treated volume in mL is adjusted to a value of 1:1.1 to 1:20. The solids content in the medium to be ultrasonically treated is in the range of 1:0.02 to 1:2.2 (in wt %).
Yeasts, such as baker's yeast, brewer's yeast, wine yeast, as well as specially treated yeasts such as POD-enriched yeasts, for example, can be used as the cell dispersion. A cell dispersion that is advantageous to use may contain
Saccharomyces cerevisiae,
for example.
A particularly advantageous component a) of the cosmetic preparation according to this invention consists of a mixture of the peptide derivative of the following formula, mixed with xanthine:
[Lip]X-His-Phe-Arg-Y
manufactured with semisynthetic marine peptides and polypeptides which are a bioengineered protein fraction produced from microalgae of the Chlorella genus and with macroalgae of the Ulva genus associated with byssus (silk filament from mollusks) and subsequently associated with a vegetable glucose polymer, and where the semisynthetic marine peptides are associated with 0.5 to 5 wt % marine mineral salts and trace elements.
An example of such a mixture is the product available under the brand name “Sun Marine Complex” (from Laboratories Seproge, Sophia-Antipolis Cedex, France).
This mixture, which is advantageous to use, contains xanthine-associated peptides and semisynthetic marine peptides, the latter associated with glucose polymers, e.g., dextrin, and mineral salts/trace elements from sea water, hereinafter referred to designated SMC (Sun Marine Complex); it is produced by simply mixing the two ingredients together. The semisynthetic marine peptides are produced by enzymatic purification of the tyrosine-rich peptides and polypeptides from byssus, i.e., from the marine mollusks. Then the vegetable cellulose component (microalgae and macroalgae) is treated enzymatically to extract the various mineral and organic elements. Then, under slightly basic conditions and under a relatively high pressure and high temperature, the association with a glucose polymer is induced, e.g., with dextrin to achieve stabilization of the individual elements of the mixture on the gludosidic carrier as a “transport molecule” for the organism.
In SMC the ratio of xanthine-associated peptides is in the range of 0.5 to 10 wt %, preferably 0.5 to 5 wt %. The remainder consists of the semisynthetic marine peptides (associated with dextrin, for example) plus mineral salts and trace elements.
As the conventional additives and vehicles of the topical preparation according to this invention, the following can be used, e.g., isopropyl myristate, isopropyl palmitate, isopropyl stearate, carbomer, cetearyl alcohol, lecithin, copolymers, paraffin oil, cetyl alcohol, propylene glycol, polyglycol, jojoba oil, silicone oil, coconut oil, kaolin modified according to WO 95/17,157, cetyl palmitate, C10-C30 alkyl acrylate cross polymer, magnesium aluminum silicate, hydroxyethylcellulose, as well as other substances suitable for the specific use forms, such as lipstick, eye cosmetics, hair mask products, etc., with which those skilled in the art are familiar.
The preparation may contain as additional active ingredients 1,3- and 1,6-&bgr;-glucan, CM-Glucan®, allantoin, TiO
2
, ZnO and UVA and UVB-blocking substances.
New agglomerates of nonporous spherical SiO
2
particles of 0.05-1.5 &mgr;m and spherical TiO
2
or ZnO particles in which the agglomerates have a particle size of 0.06-5 &mgr;m can also be used in the emulsion in the amount of 0.1-30 wt %. Such agglomerates are produced by mixing the particles while stirring at 300-400 rpm and adding some water until achieving a pasty consistency and then adding the remaining water and homogenizing at 3000 to 5000 rpm for 20-60 minutes.
The cosmetic preparation according to this invention surprisingly has a synergistic anti-inflammatory action which goes far beyond the potential of the individual ingredients, and therefore it can be used successfully in cosmetic compositions such as sunscreen emulsions, after-sun emulsi

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