Drug – bio-affecting and body treating compositions – Anti-perspirants or perspiration deodorants
Reexamination Certificate
2002-02-08
2002-12-24
Dodson, Shelley A. (Department: 1616)
Drug, bio-affecting and body treating compositions
Anti-perspirants or perspiration deodorants
C424S400000, C424S401000, C424S404000, C424S405000, C424S195160, C514S054000
Reexamination Certificate
active
06497863
ABSTRACT:
FIELD OF THE INVENTION
The invention belongs to the field of deodorising preparations which contain selected polysaccarides of the type &bgr;-(1,3) glucans; aluminium chlorohydrate, esterase inhibitors and/or bactericidal, respectively bacteriostatic, active agents, and the use of the particular glucans for the manufacture of deodorising praparations.
PRIOR ART
In the area of body, care deodorants are used for elimination of troublesome body odours. These odours are developing during the bacterial decomposition of sweat
which as such is odourless—especially in the humid and warm axillas or by similar conditions which offer the micro organisms good living conditions. Body odours can be masked by means of suitable odour substances. They can also be combated by use of preparations which inhibit the sweat secretion as such or which inhibit the decomposition of the sweat (so-called antihidrotica, antiperspirants or antitranspirants). Typical examples of such substances are aluminium compounds such as aluminium sulphate or aluminium chlorohydrate, zinc salts an citric acid compounds. A survey with regard to this can e.g. be found in Umbach (ed.) “
Kosmetik
”, p. 141f, Thieme Verlag, Stuttgart/FRG, 1988.
From the experience of everyday life it is, however, evident that the problem of odour inhibition, especially by high temperatures or substantial activity, is not completely solved. The products on the market cannot permanently prevent the emission of sweat or the formation of odours. In fact the inhibition is limited in time and dependent on the amount of sweat which is discharged.
In this connection reference is made to the U.S. Pat. No. 5,223,491, which suggests to employ a carboxymethylated &bgr;-1,3 glucan, which has been extracted from the yeast fungus
Saccharomyces cerevisiae,
for topical application. The glucan is, however, insoluble in water and can accordingly only be formulated with great difficulties. From the teachings in the two papers DE-A1 3744345 (Lomapharm) and EP-B1 0175667 (Lam) are glucans well suited for stimulation of the activity of the macrophages. The pharmaceutical effect of different glucans is further known from the two European patent applications EP-A1 045338 (Debat) and EP-A1 0561408 (Kaken). Object of the European patent EP-B1 0500718 (Donzis) is the use of water insoluble &bgr;-(1,3) glucans, which are obtained from the cell walls of yeast, for revitalisation of the skin.
Therefore there is a continuous need for products which in regard to the minimisation of the secretion of sweat and attenuation of odour are enhanced and at the same time feature an increased skin cosmetic tolerance, i.e. a lowered potential of irritation in relation to especially sensible skin. The object of the invention was therefore to make such products available.
DESCRIPTION OF THE INVENTION
The object of the invention are deodorising preparations, containing
(a) water soluble &bgr;-(1,3) glucans, which are substantially free from &bgr;-(1,6) linkages,
(b) aluminium chlorohydrate,
(c) esterase inhibitors, and/or
(d) bactericidal, respectively bacteriostatic, agents.
A further object of the invention is the use of water soluble &bgr;-(1,3) glucans, which are substantially free from &bgr;-(1,6) linkages, for the manufacture of deodorising preparations.
The use of aluminium chlorohydrates, esterase inhibitors (e.g. triethyl citrate) and bactericidal active agents (e.g. chitosan) for preparation of deodorising and/or sweat inhibiting preparations is known from the state of the art. Surprisingly it was found that the particular glucans inhibit the activity of esterolytic enzymes already in the low ppm area, and that together with the above mentioned components a synergistic effect is achieved. The polysaccarides have a selective effect on serine esterases, respectively serine proteases, without disturbing the biological equilibrium of the skin flora. At the same time the use of glucans leads to a immunestimulation and an improvement of the skin cosmetic compatibility of the products, which means that they also can be used in cosmetic preparations.
Water Soluble &bgr;-(1,3) Glucans
The term glucans means homopolysaccharides based on glucose. Depending on sterical linking there is a difference between &bgr;-(1,3), &bgr;-(1,4) and &bgr;-(1,6) glucans. &bgr;-(1,3) Glucans normally show a helical structure, whereas glucans with a (1,4) linkage generally have a linear structure. The &bgr;-glucans of the invention have a (1,3) structure, i.e. they are substantillay free from undesired (1,6) linkages. Preferably such &bgr;-(1,3) glucans are used where the side chains exclusively show (1,3) linkages. Especially the agents contain glucans which are obtained on the basis of yeasts from the family Sacchaomyces, especially
Saccharomyces cerevisiae
. Glucans of this type are available in technical amounts according to known methods. The international patent application WO 95/30022 (Biotec-Mackzymal) describes a method for producing such substances, wherein glucans with &bgr;-(1,3) and &bgr;-(1,6) linkages are brought in contact with &bgr;-(1,6) glucanases in such a way, that practically all &bgr;-(1,6) linkages are loosened. Preferably used for the manufacture of these glucans are glucanases based on
Trichodermia harzianum
. As to the manufacture and availability of the glucans contained in these agents, reference is made to the above cited publication. The glucans can be contained in the preparations in amounts of 0.1 to 5, preferably 0.2 to 5, and especially 0.5 to 1% by weight, based on the agents.
Aluminium Chlorohydrate
The aluminium chlorohydrates of component (b) are colourless, hygroscopic crystals, which easily melt in air, and which are obtained through evaporation of solutions of aluminium chloride in water. Aluminium chlorohydrate is used for manufacturing of perspiration inhibiting and deodorising preparations and has probably its effect through the partial closure or stick together of the perspiratory glands by means of precipitation of proteins and/or removal of moisture [see
J.Soc. Cosm.Chem.
24, 281 (1973)]. Under the trade name Locron® of Hoechst AG, Frankfurt/FRG, an aluminium chlorohydrate is for example on the market, which corresponds to the formula [Al
2
(OH)
5
Cl].2.5 H
2
O, and use of this is especially preferred (see
J.Pharm.Pharmacol.
26, 531 (1975)].
Esterase Inhibitors
By the presence of sweat in the axillary area extracellular enzymes—esterases, preferentially proteases and/or lipases—are formed by means of bacteria, and they are decomposing the esters contained in the sweat and thereby odour substances are set free. Esterase inhibitors of component (c), preferably trialkyl—citrates such as trimethyl citrate, tripropyl citrate, tributyl citrate and especially triethyl citrate (Hydagen® CAT, Henkel KGaA, Düsseldorf/FRG) inhibit the enzyme activity and thereby reduce the formation of odours. Probably the free acid is thereby set free through the cleavage of the citric acid ester, and this acid lowers the pH value of the skin so much that the enzymes thereby are inactivated through acylation. Further substances which can be used as estersase inhibitors are dicarboxylic acids and their esters, such as for example glutaric acid, glutaric acid monoethyl ester, glutaric acid diethyl ester, adipic acid, adipic acid monoethyl ester, adipic acid diethyl ester, malonic acid and malonic acid diethyl ester, hydroxy carboxylic acids and their esters, such as for example citric acid, malic acid, tartaric acid or tartaric acid diethyl ester.
Bactericidal, Respectively Bacteriostatic Active Agents
Bactericidal, respectively bacteriostatic, active substances of component (d), which influence the germ flora and kill sweat destroying bacterias or inhibit their growth, can also be contained in the preparations. Typical examples are especially chitosan and phenoxyethanol. 5-Chloro-2-(2,4-dichlorophenoxy)phenol has shown to have an especially good effect, and this product is marketed under the trade name Irgasan® by Ciba-Geigy, Basel/CH.
Commercial Applic
Engstad Rolf E.
Fabry Bernd
Griesbach Ute
Wachter Rolf
Biotec Pharmacon ASA
Dodson Shelley A.
Ladas & Parry
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