Drug – bio-affecting and body treating compositions – Topical body preparation containing solid synthetic organic... – Skin cosmetic coating
Reexamination Certificate
2000-10-03
2002-08-06
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Topical body preparation containing solid synthetic organic...
Skin cosmetic coating
C424S401000
Reexamination Certificate
active
06428779
ABSTRACT:
Skin ages as a result of endogenous, genetically determined influences. Exogenous factors, such as UV light and chemical noxae, can have a cumulative effect and accelerate the natural ageing processes. This results in numerous degenerative processes which lead, depending on the extent of the influencing factors, inter alia, to the following structural changes and damage in the dermis and epidermis (e.g. also to dermatoheliosis):
a) Degeneration of the microvascular system.
b) Flaccidity and development of wrinkles, partly due to a decrease in and crosslinking of collagen, accumulation of glucosaminoglycans (base substance) and solar elastosis (elastin clumping).
c) Flattening of the retial cones. This is associated with the reduction in the area between the dermis and epidermis via which substances are exchanged for nutrition and purification of the epidermis.
d) Restricted regenerative turnover in the epidermis, associated with defective development of the horny layer (disturbed hornification), leading to drying out of the skin, to roughness of the skin and to chapping of the skin.
e) Defective regulation of cell division (proliferation) and cell maturation (differentiation) in the epidermis, which results in cellular atypia and atrophies and the loss in polarity.
f) Local hyper- and hypopigmentation and abnormal pigmentation (age spots).
The present invention relates to products for the care and prophylaxis of ageing skin, in particular skin which has been aged by light and skin which has been chronologically aged by endogenous mechanisms, and also to the treatment of damage caused by light-ageing and ageing of the skin caused endogenously, in particular of the phenomena listed under a) to f), and, preferably, to the treatment and prophylactic treatment of wrinkles and roughness of the skin.
Products for the care, prophylaxis and treatment of skin which has been aged by light are known per se. They comprise, for example, retinoids (vitamin A acid and/or derivatives thereof) or vitamin A and/or derivatives thereof. However, the extent of their action on the structural damage in cases of light-ageing is limited. The use of products containing vitamin A acid furthermore often causes severe erythematous skin irritations.
Also known, from DE-A-33 09 850, are cosmetic formulations containing coenzyme Q-10, which are suitable for the treatment of skin diseases, for the prophylaxis of dystrophic and dysmetabolic states of the skin and for use on chemical and physical respiratory damage or in cases of delayed respiration associated with age and wear.
JP-A-58,180,410 describes the suitability of coenzyme Q-10 for cosmetics. It is said to activate skin cell metabolism and to suppress oxidation. As a result, coenzyme Q-10 has an important function in the prevention of skin damage caused by UV rays and the prevention of skin ageing. The roughness of the skin of 20- to 40-year olds is improved by giving the skin moisture.
The object of the present invention was thus to find ways of avoiding the disadvantages of the prior art. In particular, the prophylactic effect and the restructuring action in cases of skin ageing was to be permanent, sustained and without the risk of side effects.
According to the invention, these objects are achieved by skincare preparations and active substance combinations which contain sterols and biochemical precursors thereof in combination with ubiquinones and/or plastoquinones.
The invention relates to topical formulations containing one or more compounds chosen from the group (A) consisting of sterols and biochemical precursors thereof in combination with a content of one or more compounds chosen from the group (B) consisting of ubiquinones and derivatives thereof and plastoquinones and derivatives thereof.
Examples of highly suitable sterols are zoosterols, phytosterols and mycosterols.
Preferred zoosterols are cholesterol, dihydrocholesterol, 7-dehydrocholesterol, lanosterol, dihydrolanosterol, spongosterol and stellasterol.
Preferred phytosterols are ergosterol, sitosterol, stigmasterol, fucosterol, brassicasterol and campesterol.
Preferred mycosterols are ergosterol, fungisterol and zymosterol.
Preferred biochemical precursors of sterols are mevalonic acid, farnesol and squalane.
Particularly preferred compounds of the group (A) are cholesterol, 7-dehydrocholesterol, dihydrocholesterol, lanosterol, dihydrolanosterol, spongosterol and stellasterol.
Preferred formulations contain one, two or three compounds chosen from the group (A) combined with one, two or three compounds from the group (B).
The topical formulations according to the invention can be cosmetic or dermatological formulations. They are used, as are also the active substances, for the care and prophylaxis in cases of light-ageing and chronological skin ageing and for the treatment of light-aged skin and chronologically aged skin.
The invention also relates to the use of topical formulations containing one or more compounds chosen from the group (A) consisting of sterols and biochemical precursors thereof in combination with a content of one or more compounds chosen from the group (B) consisting of ubiquinones and derivatives thereof and plastoquinones and derivatives thereof for the care and prophylaxis in cases of light-ageing and chronological skin ageing and for the treatment of light-aged skin and chronologically aged skin.
The active substance combinations according to the invention and the formulations obtainable therewith effect restructuring of light-aged skin or skin aged chronologically by endogenous mechanisms, in particular of wrinkled, rough, dry, chapped and/or flaky skin.
The invention thus also relates to the use of the above formulations and active substances for the purposes described, but preferably to the use for the prophylaxis and treatment of the following symptoms a) to f), in particular of dermatoheliosis and of chronologically aged skin:
a) Degeneration of the microvascular system.
b) Flaccidity and development of wrinkles, partly due to a decrease in and crosslinking of collagen, accumulation of glucosaminoglycans (base substance) and solar elastosis (elastin clumping).
c) Flattening of the retial cones. This is associated with the reduction in the area between the dermis and epidermis via which substances are exchanged for nutrition and purification of the epidermis.
d) Restricted regenerative turnover in the epidermis, associated with defective development of the horny layer (disturbed hornification), leading to drying out of the skin, to roughness of the skin, chapping of the skin and flaking.
e) Defective regulation of cell division (proliferation) and cell maturation (differentiation) in the epidermis, which results in cellular atypia and atrophies and the loss in polarity.
f) Local hyper- and hypopigmentation and abnormal pigmentation (age spots).
Particular preference is given to combinations of cholesterol with ubiquinones, in particular coenzyme Q-6, Q-9 or Q-10, but in particular to combinations of cholesterol with coenzyme Q-10, to formulations therewith, and to the uses for the above purposes.
Ubiquinones (also coenzymes Q
n
) are a group of substances which have n isoprene units bonded in the form of a chain on their quinone ring (Q
0
-Q
10
). Ubiquinones function as electron transfer agents in biological, mitochondrial oxidation and thus play an important role in energy metabolism of the cells. Plastoquinones are analogous compounds from the plant kingdom, which play a role in photosynthesis. Ubiquinones have been used for a long time in cosmetic formulations as antioxidants for protection of oxidation-sensitive substances against decay induced by oxygen free radicals.
“Ubiquinones” and “plastoquinones” here also mean “ubiquinones and derivatives thereof” and “plastoquinones and derivatives thereof”.
Ubiquinones are known from the literature (for example “Römpp Chemie Lexikon” [Römpp's Chemical Dictionary], Georg Thieme Verlag Stuttgart, New York, 9th Edition, pages 4784-4785 or “The Merck Index”, 11th Edition, Merck & Co., Inc. Rahway, N
Hoppe Udo
Sauermann Gerhard
Schreiner Volker
Stäb Franz
Beiersdorf AG
Howard S.
Norris & McLaughlin & Marcus
Page Thurman K.
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