Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Cosmetic – antiperspirant – dentifrice
Reexamination Certificate
2002-04-26
2003-01-07
Dodson, Shelley A. (Department: 1616)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Cosmetic, antiperspirant, dentifrice
C424S400000, C514S725000, C514S844000, C514S863000, C514S864000
Reexamination Certificate
active
06503523
ABSTRACT:
The invention relates to topical preparations with ubiquinones and/or plastoquinones.
The aging of the skin is caused by endogenous, genetically determined influences. Exogenous factors, such as UV light and noxious chemicals can have a cumulative effect and accelerate the natural aging process. Numerous degenerative processes occur which, depending on the extent of the influence factors, lead, amongst other things, to the following structural changes and damage to the dermis and epidermis (dermatoheliosis):
a) Retroplasia of the microvascular system.
b) Looseness and formation of wrinkles, partly due to the loss, and cross-linking, of collagen, and accumulation of glucose aminoglycane (basic substance).
c) Flattening of the reticular system. This is connected with a narrowing of the surface between dermis and epidermis, through which substances are exchanged for nourishment and purification of the epidermis.
d) Limited regenerative turnover in the epidermis, combined with defective formation of the horny layer (keratinization disorders) which leads to the drying-out of the skin.
e) Defective regulation of cell distribution (proliferation) and cell maturation (differentiation) in the epidermis, resulting in atypical cells and loss of polarity.
f) Local hyper-, hypo- and defective pigmentation (age spots).
In the pathogenesis of acne, which occurs especially in young people, but also in later life, both the over-production of sebaceous gland lipids by over-developed sebaceous glands (sebaceous gland hyperplasia) and keratinization disorders of the sebaceous gland outlet play an essential role. In both cases there is accumulation of sebum lipids that provide the breeding ground for acne-producing bacteria.
Pigmentation of the skin is due, for example, to melanocytes, which are found in the bottom layer of the epidermis, the basal stratum, next to the basal cells, which—depending on skin type—are present as pigment-forming cells either individually or in relatively large numbers. Melanocytes contain melanosomes as characteristic cell organelles, which produce more melanin when stimulated by UV radiation. This is transported into the cells of the horny layer (keratinocytes) and causes more or less pronounced brownish or brown skin colouring.
Melanin is formed as the final stage in an oxidation process, in which tyrosine, with the aid of the enzyme tyrosinase, is converted via 3,4-dihydroxyphenyl-2-aminopropionic acid (dopa), dopa-quinone, leucodopachrome, dopachrome, 5,6-dihydroxyindol and indole-5,6-quinone finally to melanin.
Problems with hyperpigmentation of the skin have many causes and/or are side effects of many biological processes, e.g. UV radiation (e.g. freckles, ephelides), genetic disposition, defective pigmentation of the skin and/or scarring during the healing of wounds, or skin aging (e.g. lentigines seniles).
Substances and preparations are known which counteract skin pigmentation. Those in practical use are essentially preparations based on hydroquinone, which however on the one hand only begin to show an effect after several weeks of use, whilst on the other hand their use over a very long period is not always safe for toxicological reasons. The inhibition of tyrosinase with substances such as koji acid, ascorbic acid, azelaic acid and their derivatives is also common, but has cosmetic and dermatological disadvantages.
The present invention relates in particular to products for the care and prophylaxis of skin aged by light or with a tendency towards acne, and for the treatment in particular of the types of damage listed under a)-f) caused by light aging and especially for cosmetic lightening (“skin whitening”) of undesired skin pigmentation.
Products for the care, prophylaxis and treatment of light-aged skin and for the prophylactic treatment of acne are known. They contain, for example, vitamin A acid. Their effect on the structural damage of light-aging and/or reduction of the risk of acne is however largely limited. In addition the use of products containing vitamin A acid often causes strong erythematous skin irritations. Vitamin A acid in particular can therefore only be used in low concentrations.
Cosmetic preparations containing coenzyme Q-10 are also known from DE-A-33 09 850. This preparation is suitable for the treatment of skin diseases, the prophylaxis of dystrophic and dysmetabolic skin conditions and for application in the case of chemical and physical respiration damage or delayed respiration associated with age and wear and tear.
The published Japanese patent application 58,180,410 describes the suitability of coenzyme Q-10 for cosmetics. It is believed to activate the skin cell metabolism and suppress oxidation. Coenzyme Q-10 has proved to perform an important function in the prevention of skin damage by UV radiation and the prevention of skin aging. In 20-40 year olds, skin roughness is improved adding moisture to the skin.
From WO95/26180, topical preparations are known, which contain retinols, retinals, beta-carotene and ubiquinones or plastoquinones.
The aim of the present invention was therefore to find ways of avoiding the disadvantages of the state of the art. In particular the prophylactic effect on acne and the restructuring effect in the case of light-aging should be permanent, disadvantageous [sic] and without the risk of side effects.
According to the invention these aims are achieved by skin preparations containing vitamin A acid or its derivatives combined with ubiquinones and/or plastoquinones.
The object of the invention is topical preparations containing one or more compounds chosen from group (A), which consists of vitamin A acid or its derivatives, combined with one or more compounds chosen from group (B), which consists of ubiquinones and their derivatives and plastoquinones and their derivatives.
Preferred preparations are those containing one, two or three compounds chosen from group (A), combined with one, two or three compounds from group (B).
The inventive topical preparations can be cosmetic or dermatological preparations, and they are also described here as skin care products or dermatological products. They and their active agents are used for prophylaxis in the case of acne and for care and prophylaxis in the case of light-aging and for the treatment of light-aged skin and to lighten undesired skin pigmentation.
The object of the invention is also the use of topical preparations containing one or more compounds chosen from group (A), which consists of of vitamin A acid or its derivatives, combined with one or more compounds chosen from group (B), which consists of ubiquinones and their derivatives and plastoquinones and their derivatives, for the care and prophylactic treatment of acne and for the care and prophylaxis of light-aging and for the treatment of light-aged skin and for the lightening of undesired skin pigmentation.
The object of the invention is therefore also the use of the aforementioned preparations and active agents for the purposes described, but preferably their use for prophylaxis and treatment of the following phenomena a)-f), especially dermatoheliosis:
a) Retroplasia of the microvascular system.
b) Looseness and formation of wrinkles, partly due to the loss, and cross-linking, of the collagen, and accumulation of glucose aminoglycane (basic substance).
c) Flattening of the reticular system. This is connected with a narrowing of the surface between dermis and epidermis, through which substances are exchanged for nourishment and purification of the epidermis.
d) Limited regenerative turnover in the epidermis, combined with defective formation of the horny layer (keratinization disorders) which leads to the drying-out of the skin.
e) Defective regulation of cell distribution (proliferation) and cell maturation (differentiation) in the epidermis, resulting in atypical cells and loss of polarity.
f) Local hyper-, hypo- and defective pigmentation (age spots).
The term “vitamin A acid and its derivatives” covers all-trans retinoic acid, also known as tretinoin, and its isomers, erg. 13-cis
Hoppe Udo
Schreiner Volker
Stäb Franz
Dodson Shelley A.
GS Development A.B.
Nixon & Vanderhye P.C.
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