Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Cosmetic – antiperspirant – dentifrice
Reexamination Certificate
2000-12-22
2002-07-30
Hartley, Michael G. (Department: 1617)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Cosmetic, antiperspirant, dentifrice
C424S078030, C424S078050, C514S002600, C514S946000
Reexamination Certificate
active
06426080
ABSTRACT:
The disclosed cosmetic preparation of active substances protects the skin in a particularly effective way against free radical aggression, both alone and in combination with other active substances.
Free radicals such as superoxide ions, hydroxy radicals, oxides are known as a major factor of degeneration and thus the ageing of the skin. They destruct the proteins and lipids of the cellular membrane, affect the DNA and also decompose the hyaluronic acid, a key substance of the skin. Under normal biological conditions there is an equilibrium ratio between the free radicals coming up and their embankment by endogenous chemical or enzymatic systems. Additional outside stress factors such as aggressive atmosphere, tobacco smoke, ultraviolet radiation etc. may overload these inherent immune systems and shift the equilibrium in favour of the free radicals. Inflammation or ageing phenomena of the skin may occur, indicating a need for compensation by cosmetic products.
There has already been proposed a series of products for this purpose, most of them containing mixtures of the vitamins A, C and E or additives of superoxide dismutase or extracts of certain plants or animals. Thus a cosmetic compound containing ultrasound decomposition products of yeast and other cellular dispersions is known from U.S. Pat. No. 5,629,185. From WO96/29048 a cosmetic containing condensed decomposition products of plants or animals is known. There is also a number of publications describing the use of pure plant extracts for cosmetic purposes, such as WO97/45100, where a mixture of seven different extracts is described for anti-cellulite treatment.
The search for other effective substances is a major element of cosmetic research. Another problem of many of these products is that the substances which are effective against free radicals often do not keep their catching properties within the ready cosmetic compound, i.e. it requires special formulations to permanently maintain the effectiveness of the radical catchers.
On the other hand it seems that it has not become widely known in the cosmetic industry yet that there is a possibility of measuring the antioxidant potential of the skin (DE 4328639) and recently also of determining the radical protection coefficient of a cosmetic preparation by using a relatively simple method and to purposefully add materials to such a preparation.
It is an object of the present invention to provide a cosmetic preparation of active substances which has a particularly high radical protection potential.
Another objective of the invention is to provide a preparation of active substances that keeps its radical protection potential over a long period of time.
Another objective of the invention is to provide special cosmetic compounds containing this preparation of active substances and especially such preparations of active substances which achieve further improvement of properties, in particular with regard to opening the pores of the skin.
According to the invention, the cosmetic preparation of active substances with a high radical protection factor is characterised by comprising
(a) a product obtained by extraction of the bark of
Quebracho blanco
and subsequent enzymatic hydrolysis, containing at least 90 percent by weight of proanthocyanidine oligomers and up to 10 percent by weight of gallic acid, wherein the content of (a), which is available in a concentration of 2 percent by weight linked to a microcapsules, ranges from 0.1 to 10 percent by weight;
(b) an extract of the silkworm obtained by extraction, containing the peptide Cecropine, amino acids and a vitamin mix, wherein the content of (b) may range from 0.1 to 10 percent by weight;
(c) a non-ionic, cationic or anionic hydrogel or mixture of hydrogels, wherein the content of (c) may range from 0.1 to 5 percent by weight;
(d) one or several phospholipids comprising 0.1 up to 30 percent by weight;
(e) up to 100 percent by weight of water related to the total weight of the active substance preparation each.
As applicable, the active substance preparation may also contain:
(f) an ultrasound decomposition product of a yeast containing 15 at least 150 units of superoxide dismutase per ml, wherein the content of the decomposition product (f) is in the range from 0 to 4 percent by weight;
(g) an extract of acerola fruits
Malpighia punidifolia
, wherein the content (g) is in the range from 0 to 20 percent by weight; and
(h) a mixture of 0.1 percent by weight of liposomal
Micrococcus luteus
extract, retinyle palmitate and tocopherylacetate prepared with phospholipids and free retinyle palmitate related to the total weight of the active substance preparation each.
For one embodiment of the invention comprising the active substance component (h) the portions of the preparation related to the total weight of the cosmetic are as follows: capsules of the active substance according to (a) ranging from 0.1 to 10 percent by weight, hydrogel according to (b) ranging from 0.1 to 5 percent by weight, encapsulated retinyle palmitate according to (h) 0.001 to 5 percent by weight, encapsulated tocopherylacetate according to (h): 0.001 to 2 percent by weight free retinyle palmitate according to (h): 0.1 to 5 percent by weight, phospholipids: 0.2 to 5 percent by weight, water as the remaining portion up to 100 percent by weight and/or other auxiliary or carrier substances.
The Quebracho bark extract according to the invention or its hydrolysis product has a very high portion of proantho-cyanidines representing condensed tannins. These compounds appearing as oligomers and the low portion of gallic acid in this combination and in a concentration between 1 and 10 percent by weight shows a clear radical protection effect, which by far exceeds the effect of superoxide dismutase (SOD). The activity against free radicals was compared with that of SOD and found to be 42% for a 1 percent by weight solution of the extract (SOD 4%), 83% for a 2.5% by weight solution (SOD 15%)and 100% for a 5% by weight solution (SOD 38%). Preferably the extract (a) contains at least 95 percent by weight of proanthocyanidine oligomers and up to 5 percent by weight of gallic acid, in particular at least 99 percent by weight of proanthocyanidine oligomers and up to 1 percent by weight of gallic acid.
The content of (a) is 1 to 10 percent by weight, wherein the active substance from the Quebracho bark is enclosed in microcapsules. The microcapsules may consist of petrolatum, sodium tristearat, agar, phenonip and water.
The silkworm extract (b) is obtained by extraction of the silkworm (
Bombvx mori
) with 1,2-propylene glycol and contains vitamins, amino acids and the Cecropine peptide, which has a special antibacterial functionality. A range of studies of the haemolymph and the cuticular matrix of the silkworm carried out during the last years showed that it does not only contain antibacterial peptides but also inhibitors, in particular fungal protease inhibitors. Such extracts also show oxygen consuming properties, thus activating the cellular metabolism, and they have moisture-keeping properties, a clear curative effect on lesions in the skin by reducing healing time and a skin-smoothing effect.
Preferably, the extract (b) includes the amino acids aspertinic acid, asparagine, threonine, serine, glutaminic acid, praline, glycine, alanine, valine, cysteine, methionine, isoleucine, leucine, tyrosine, phenylalanine, lysine, histidine, arginine.
Preferably extract (b) also contains a vitamin mixture including vitamins B
1
, B
2
, B
5
, B
6
, B
8
, B
9
, B
12
, PP, A, E and C.
The concentration of components (a) and (b) in the active substance preparation preferably ranges from 0.1 to 3 percent by weight each, in particular from 0.5 to 3 percent by weight. The gel contained according to the invention, which may also be a mixture of different gels, is a hydrogel soluble in water at temperatures above 40 up to 50° C., approximately, and which takes the gel structure at low temperatures between 10 and 30° C. Examples of such gels are non-ionic polymers such as polyvinyl alco
Golz-Berner Karin
Zastrow Leonhard
Collard & Roe P.C.
Coty B.V.
Hartley Michael G.
Willis Michael A.
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