Drug – bio-affecting and body treating compositions – Manicure or pedicure compositions
Reexamination Certificate
2001-07-27
2003-12-09
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Manicure or pedicure compositions
C424S401000
Reexamination Certificate
active
06660251
ABSTRACT:
The invention relates to topically applicable galenic formulations which contain one or more compounds selected from biotin, the physiologically tolerable salts of biotin, biotin esters and the stereoisomeric forms of these compounds and one or more compounds selected from urea and urea derivatives and are suitable for the cosmetic or medicinal treatment of skin, hair and/or nails, for example for the treatment of diseases or functional disorders of human or animal skin, hair and/or nails.
The chemical name for biotin is hexahydro-2-oxiothieno [3,4-d]imidazole-4-valeric acid. Its chemical structure corresponds to the formula
The efficacy of biotin in skin, hair and nail diseases has been assessed in different ways in the past. Although, by means of continuous biotin therapy, it was possible to show the efficacy in the case of soft, brittle and splitting nails, different forms of alopecia and atopic and seborrheic dermatitis in a detectable manner, use remained sparing, as this is associated, despite no side effects at all, with the necessity of an extended treatment period of several months (R. Bitsch et al. (1994) Biotin, Wissenschaftliche Verlagsgesellschaft mbH, Stuttgart; V. E. Colombo et al. (1990) Treatment of brittle fingernails and onychoschizia with biotin: scanning electron microscopy. J. Am. Acad. Dermatol. 23: 1127-1132; G. L. Floersheim (1989) Behandlung brüchiger Fingernägel mit Biotin [Treatment of brittle fingernails with biotin]. Z. Hautkr. 64: 41-48; G. L. Floersheim (1992) Prüfung der Wirkung von Biotin auf Haarausfall und Haarqualität [Testing the action of biotin on hair loss and hair quality]. Z. Hautkr. 67: 246-255; W. Gehring (1996) Der Einfluss von Biotin bei reduzierter Nagelqualität. Eine plazebokontrollierte doppelblinde klinische Studie [The influence of biotin on reduced nail quality. A placebo-controlled double-blind clinical study]. Akt. Dermatol. 22: 20-25; U. Siebert et al. (1996) Zur Dosierung und Wirkung von Biotin bei Nagel- und Haarwachstumsstörungen [The dosage and action of biotin in nail and hair growth disorders]. Zeitschrift Hautnah 6: 438-443).
It is known that topically applied biotin-containing formulations having a biotin content of 0.25% and 0.50% lead to a visible reduction in the development of wrinkles on the skin of old people (L. Gilli et al. (1995) Beeinflussung der Fältchenausprägung bei Altershaut durch topisch appliziertes Biotin [Influencing the development of wrinkles on the skin of old people by means of topically applied biotin]. Z. Hautkr. 70 (6): 419-425). In these investigations, it was not possible to show any epithelial and histopathological changes at all in the areas treated.
Regardless of the positive clinical experience with biotin, knowledge about the mechanism of action is incomplete. From the present state of knowledge, biotin, as a coenzyme, has a number of carboxylases which are linked in with various vital metabolic functions (R. Bitsch et al. (1994) Biotin. Wissenschaftliche Verlagsgesellschaft mbH, Stuttgart). In addition to its function as a coenzyme, the independent pharmacological effects of biotin, e.g. the influence on the keratin structure, are of interest for therapeutic use. The underlying mechanism of the influence on the growth and differentiation behavior of the keratinocytes, however, is controversial (A. Fritsche (1990) Biotin verändert das Zytokeratinmuster von kultivierten Keratinozyten [Biotin changes the cytokeratin pattern of cultured keratinocytes], inaugural dissertation, University of Zurich; A. Fritsche et al. (1991) Pharmakologische Wirkungen von Biotin auf Epidermiszellen [Pharmacological effects of biotin on epidermal cells]. Schweiz. Arch. Tierheilk. 133: 277-283; A. Limat et al. (1996) Proliferation and differentiation of cultured human follicular keratinocytes are not influenced by biotin. Arch. Dermatol. Res. 288: 31-38).
Owing to its hydrophilic properties, biotin belongs to the substances for which the horny layer, with its lipophilicity and the low hydration in the normal state, represents a penetration barrier of particular size.
For the topic application of biotin there thus exist particular galenic requirements.
The object was thus to make available topically applicable galenic formulations which contain compounds selected from biotin, the physiologically tolerable salts of biotin, biotin esters and the stereoisomeric forms of these compounds and are suitable for the cosmetic or medicinal treatment of skin, hair and/or nails.
Surprisingly, it has now been found that this object is achieved by the provision of galenic formulations comprising
a) one or more compounds selected from biotin, the physiologically tolerable salts of biotin, biotin esters and the stereoisomeric forms of these compounds and
b) one or more compounds selected from urea and urea derivatives.
The invention furthermore relates to
the use of one or more compounds selected from biotin, the physiologically tolerable salts of biotin, biotin esters and the stereoisomeric forms of these compounds and of one or more compounds selected from urea and urea derivatives for the production of a topically applicable galenic formulation,
a process for the production of a topically applicable galenic formulation, characterized in that one or more compounds selected from biotin, the physiologically tolerable salts of biotin, biotin esters and the stereoisomeric forms of these compounds and one or more compounds selected from urea and urea derivatives are brought into a suitable formulation form, if appropriate with further active compounds, excipients and/or vehicles.
The application of the galenic formulations according to the invention can take place both to humans and to animals. The galenic formulations according to the invention can be used both in cosmetics and in human and in veterinary medicine. The areas of use of the galenic formulations according to the invention relate to the therapy, prophylaxis and/or metaphylaxis of skin diseases, of functional disorders of the skin, of skin-ageing processes and of dry skin conditions.
The invention furthermore relates to the use of
a) one or more compounds selected from biotin, the physiologically tolerable salts of biotin, biotin esters and the stereoisomeric forms of these compounds and
b) one or more compounds selected from urea and urea derivatives
for the production of a topically applicable galenic formulation
for improving the penetration of the compounds selected from biotin, the physiologically acceptable salts of biotin, biotin esters and the stereoisomeric forms of these compounds into deeper layers of human or animal skin, mucous membrane and/or nails,
for the protection, for the maintenance and/or for the reconstruction of the normal function and structure of human or animal skin and/or for the prevention of environmentally related skin damage, for example UV-related skin damage,
for the treatment of diseases of the hair, sebaceous and/or sweat glands of human or animal skin and/or
for cosmetic skin treatment, in particular for skin care.
In particular, “penetration of biotin into deeper layers of human skin”, for example, in the context of the present invention means that biotin penetrates through the horny layer of the human skin. Without a penetration enhancer, biotin does not penetrate or does not penetrate in an efficacious concentration through the horny layer of the human skin. However, it has been found, for example, that the penetration of topically applied biotin through the horny layer into human skin is improved if biotin is combined with a penetration enhancer, preferably with urea and particularly preferably with urea in an emulsion. It has been found that the combination of biotin with a penetration enhancer of this type makes possible, for example, the penetration of biotin into the living epidermis in an efficacious concentration.
In the context of the present invention, penetration enhancers are designated as substances which, for example, increase the p
Bünger Joachim
Driller Hansjürgen
Huschka Christoph
Motitschke Lothar
Neubert Reinhard
Howard S.
Merck Patent GmbH
Millen White Zelano & Branigan P.C.
Page Thurman K.
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