Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Reexamination Certificate
1999-04-16
2003-07-08
Qazi, Sabiha (Department: 1616)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
C514S178000, C514S182000, C552S540000, C552S544000
Reexamination Certificate
active
06589945
ABSTRACT:
FIELD OF THE INVENTION
This invention relates to the use of sterol sulfates as active principles for controlling wrinkling of the skin and skin diseases, for example psoriasis and UV erythemas.
DISCUSSION OF THE RELATED ART
Wrinkling of the skin with age is caused by the degradation of various macromolecules, such as for example elastin and collagen, for which elastases in the stratum corneum are responsible. Various inflammatory skin diseases, for example psoriasis or UV erythrema, can also be attributed to a high concentration of elastase in the upper layers of the skin [cf. R. Voegeli et al in Cosm. Toil. 111, 51 (1996)].
In general, wrinkling of the skin is not counteracted by physiologically active principles, but rather by cosmetic compositions. Many so-called anti-aging products contain liposomes charged with water or aqueous active principles which enter the epidermis through the fatty layer of the skin, gradually dissolve there, fill the wrinkles through the continuous release of water and regulate the moisture content of the skin. However, this effect has nothing to do with fighting the causes, but is merely a so-called repair effect which, moreover, only lasts for a short time.
In contrast to this purely cosmetic application, cytostatic agents for example, such as selenium sulfide, cadmium sulfide, zinc pyrithione or corticosteroids, are used in the treatment of psoriasis, their medicinal effect being attributable, for example, to a reduction in mitose activity in the basal membrane. On account of their well-known side effects, however, these substances should not be used over long periods. In addition, psoriasis can be treated but not cured by antiseptic agents, for example selenium oxide, salicylic acid, pyrithione derivatives, hexachlorophene or quaternary ammonium compounds, or by cell-dissolving and defatting agents such as, for example, benzoyl peroxide or tar extracts.
Accordingly, very difficult solutions are known from the prior art for smoothing the skin and strengthening the barrier function either from the cosmetic or from the medicinal standpoint. Unfortunately, they solve only part of the problem and, in addition, can be accompanied by strong side effects. Accordingly, the complex problem addressed by the present invention was to provide active principles which could be used both against wrinkling of the skin (cosmetic effect) and against skin diseases (medicinal effect) and which, at the same time, would have high dermatological and toxicological compatibility.
DESCRIPTION OF THE INVENTION
The present invention relates to the use of sterol sulfates as active principles for the production of compositions for inhibiting serine proteases, preferably elastases.
It has surprisingly been found that sterol sulfates deactivate serine proteases in general and elastases in particular and thus slow down the degradation of macromolecules, such as elastin, collagen, etc., in the connective tissue. In this way, wrinkling of the skin with age is reduced. In addition, the topical application of sterol sulfates ensures a high concentration of the active principle in the stratum corneum so that the cohesion of the corneocytes is increased and the upper layers are thickened. This effect is particularly important in the case of damaged skin because the stratum corneum is unable to perform its barrier function if the skin is damaged. The invention also includes the observation that sterol sulfates, by inhibiting elastase, also lead to the prevention or reduction of inflammatory reactions and may therefore be used for treating skin diseases. Finally, sterol sulfates which occur in concentrations of up to 4% by weight in the upper layers of the stratum corneum are known to be highly compatible with the skin and toxicologically safe.
Sterol sulfates
Sterol sulfates are known substances which may be prepared, for example, by sulfation of sterols with a complex of sulfur trioxide and pyridine in benzene [cf. J. Am. Chem. Soc. 63, 1259 (1941)]. Sterols—which may be used as starting materials for the production of sterol sulfates—are understood to be steroids which contain only a hydroxyl group but no other functional groups at C-3. Formally, therefore, they are alcohols which would explain why this group of compounds is sometimes also referred to as sterols. Generally, sterols contain 27 to 30 carbon atoms and one double bond in the 5/6 position and optionally in the 7/8, 8/9 or other positions. Besides these unsaturated species, however, other suitable starting materials are the saturated compounds obtainable by hydrogenation. Typical examples of suitable sterol sulfates are those based on zoosterols, for example animal cholesterol, lanosterols from wool fat, spongosterols from sponges of stellasterols from starfish. However, phytosterol sulfates, for example those based on ergosterols, campesterols, stigmasterols and sitosterols, are preferably used by virtue of the lighter color of the sulfation products. The sterol sulfates may be used in the form of alkali metal and/or alkaline earth metal salts, ammonium, alkylammonium, alkanolammonium and/or glucammonium salts. They are generally used in the form of the sodium salts.
The sterol sulfates may be marketed in pure solid form. However, they may also be marketed in the form of solutions in suitable solvents, for example propylene glycol or butylene glycol, or as compounds, for example together with fatty alcohol ether sulfates, as raw materials for the production of cosmetic or pharmaceutical compositions. In these concentrated formulations, the sterol sulfate content may be in the range from 0.1 to 10% by weight and is preferably is in the range from 1 to 5% by weight and more preferably in the range from 2 to 8% by weight.
Commercial Applications
According to the invention, the sterol sulfates may be used as active principles for the production of cosmetic and/or pharmaceutical compositions. Typical examples of such compositions are skin-care products such as, for example, anti-wrinkle cremes, anti-cellulite cremes or sun protection lotions and ointments for the treatment of skin diseases such as, for example, cradle cap, psoriasis, seborrhoeic dermatitis, seborrhoea sicca, seborrhoea oleosa, psoriasis vulgaris, ichtyoses or UV erythemas. The sterol sulfates are normally used in quantities of 0.0001 to 5% by weight, preferably in quantities of 0.001 to 1% by weight and more preferably in quantities of 0.01 to 0.1% by weight, based on the particular composition.
The compositions may contain small quantities of anionic, nonionic, cationic and/or amphoteric or zwitterionic surfactants compatible with the other ingredients. Typical examples of anionic surfactants are soaps, alkyl benzenesulfonates, alkanesulfonates, olefin sulfonates, alkylether sulfonates, glycerol ether sulfonates, &agr;-methyl ester sulfonates, sulfofatty acids, alkyl sulfates, fatty alcohol ether sulfates, glycerol ether sulfates, hydroxy mixed ether sulfates, monolyceride (ether) sulfates, fatty acid amide (ether) sulfates, mono- and dialkyl sulfosuccinates, mono- and dialkyl sulfosuccinamates, sulfotriglycerides, amide soaps, ether carboxylic acids and salts thereof, fatty acid isethionates, fatty acid sarcosinates, fatty acid taurides, N-acylamino acids such as, for example, acyl lactylates, acyl tartrates, acyl glutamates and acyl aspartates, alkyl oligoclugocide sulfates, protein fatty acid condensates (particularly wheat-based vegetable products) and alkyl (ether) phosphates. If the anionic surfactants contain polyglycol ether chains, they may have a conventional homolog distribution although they preferably have a narrow-range homolog distribution. Typical examples of nononic surfactants are fatty alcohol polyglycol ethers, alkylphenyl polyglycol ethers, fatty acid polyglycol esters, fatty acid amide polyglycol ethers, fatty amine polyglycol ethers, alkoxylated triglycerides, mixed ethers and mixed formals, alk(en)yl oligoglycosides, fatty acid N-alkyl glucamides, protein hydrolyzates (particularly wheat-based vegetable products),
Behler Ansgar
Maurer Karl-Heinz
Tesmann Holger
Wachter Rolf
Cognis Deutschland GmbH & Co. KG
Drach John E.
Murphy Glenn E.
Qazi Sabiha
Trzaska Steven J.
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