Use of a substance agonist of a receptor associated with a...

Drug – bio-affecting and body treating compositions – Topical body preparation containing solid synthetic organic...

Reexamination Certificate

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C424S078050, C424S078070, C424S401000, C514S221000, C514S275000, C514S302000, C514S353000, C514S354000, C514S355000, C514S356000, C514S561000, C514S711000, C514S861000, C514S863000, C514S864000, C514S887000, C514S937000, C514S944000

Reexamination Certificate

active

06572848

ABSTRACT:

BACKGROUND OF THE INVENTION
1. Technical Field of the Invention
The present invention relates to the use of a substance which is an agonist of a receptor associated with a chlorine channel or with a potassium channel, except for amino acids and derivatives thereof, in a cosmetic and/or dermatological composition, for treating sensitive skin, including the scalp, and mucous membranes, of human beings. The invention also relates to a process for treating sensitive skin.
2. Description of the Prior Art
It is known that certain skin types are more sensitive than others. The symptoms of sensitive skin were hitherto poorly characterized and the problem of these skin types was consequently poorly defined; no-one knew exactly what process was involved in skin sensitivity. Some thought that sensitive skin was skin which reacted to cosmetic products, while others thought that it was skin which reacted to several external factors, not necessarily associated with cosmetic products.
Certain tests have been developed in an attempt to define sensitive skin, for example tests with lactic acid and with DMSO (dimethyl sulphoxide) which are known to be irritant substances: see for example the article by K. Lammintausta et al., Dermatoses, 1988, 36, pages 45-49; and the article by T. Agner and J. Serup, Clinical and Experimental Dermatology, 1989, 14, pages 214-217. However, these tests did not make it possible to correctly characterize sensitive skin.
Moreover, sensitive skin was likened to allergic skin.
Since the characteristics of sensitive skin were not well known, it was hitherto very difficult to treat such skin types, and they were treated indirectly, for example by limiting the use of products of irritant nature, such as surfactants, preserving agents or fragrances, in cosmetic compositions.
The Applicant has carried out many clinical tests and has been able to determine the symptoms associated with sensitive skin. These symptoms are, in particular, subjective signs, which are essentially dysaesthetic sensations. The term dysaesthetic sensations is understood to refer to the more or less painful sensations experienced in a region of skin, such as stinging, tingling, itching or pruritus, burning, heating, discomfort, tautness, etc. The Applicant has also been able to show that sensitive skin was not allergic skin (see in this respect patent FR-A-2 719 474).
Document WO 91/18608 describes the use of triazolobenzodiazepines as PAF (Platelet-Activating Factor) antagonists for treating pruritus. The Applicant has thus found that sensitive skin can be divided into two major clinical forms: irritable and/or reactive skin, and intolerant skin.
Irritable and/or reactive skin is skin which reacts by pruritus, i.e. by itching or stinging, to various factors such as the environment, emotions, foods, the wind, rubbing, shaving, soap, surfactants, hard water with a high calcium concentration, temperature variations or wool. In general, these signs are associated with dry skin with or without dry patches, or with skin which displays erythema.
Intolerant skin is skin which reacts, by sensations of heating, tautness, tingling and/or redness, to various factors such as the environment, emotions and foods. In general, these signs are associated with hyperseborrhoeic or acneic skin with or without dry patches, and with erythema.
“Sensitive” scalps have a more univocal clinical semeiology: the sensations of pruritus and/or of stinging and/or heating are essentially triggered by local factors such as rubbing, soap, surfactants, hard water with a high calcium concentration, shampoos or lotions. These sensations are also sometimes triggered by factors such as the environment, emotions and/or foods. Erythema and hyperseborrhoea of the scalp and the presence of dandruff are often associated with the above signs.
Moreover, in certain anatomical regions such as the major folds (groin, genital, axillary, popliteal, anal and submammary regions and in the crook of the elbow) and the feet, sensitive skin is reflected in pruriginous sensations and/or dysaesthetic sensations (heating, stinging) associated in particular with sweat, rubbing, wool, surfactants, hard water with a high calcium concentration and/or temperature variations.
To determine whether or not a skin is sensitive, the Applicant has also developed tests, in particular with capsaicin and triethanolamine.
SUMMARY OF THE INVENTION
The Applicant has now discovered that sensitive skin is associated with a modification in the skin's nerve excitability. Consequently, the use of agonists of the receptors associated with the chlorine and/or potassium channels present in skin tissue can make it possible to obtain a preventive and/or curative effect on sensitive skin.
Specifically, the cell membranes of each nerve fibre comprise many ion channels, and in particular chlorine or potassium channels. The role of these various channels is to allow the chloride and potassium ions to pass from both sides of the nerve cell membrane, these ion exchanges (influx of negatively charged chlorides and exit of positively charged potassium) leading to electrical changes which make the sensitive nerve fibres less excitable (this phenomenon is known as membrane hyperpolarization). The neuronal receptors associated with the chlorine or potassium channels are, in particular for the chlorine channels, glycine receptors (glycine-strychnine sensitive receptors) and GABA receptors (GABA
A
receptors).
Moreover, it is known that, in the central nervous system, it is possible to reduce the cellular excitability with various pharmacological agents which have an effect on the glycine-strychnine sensitive receptors or on the GABA
A
receptors associated with the chlorine channels of the central nervous system (see W. Sieghart, Trends in Pharmacological Science, December 1992, vol. 131, pages 446 to 450). Furthermore, it is also possible to reduce the cellular excitability with various pharmacological agents which have an effect on the potassium channels (see S. D. Longman, Medicinal Research Reviews, 1992, vol. 12, page 73).
After numerous clinical tests, the Applicant has found that skin tissue comprises receptors associated with the chlorine or potassium channels, which had not been envisaged hitherto, and that a link exists between the chlorine or potassium channels of sensitive nerve fibres of the cutaneous peripheral nervous system and sensitive skin. The Applicant has thus found that it is possible to act on these channels to treat sensitive skin.
No-one had hitherto established a link between the chlorine or potassium channels of the sensitive nerve fibres of the cutaneous peripheral nervous system and sensitive skin, and no-one had found that sensitive skin could be treated by acting on the chlorine or potassium channels by activating the receptors in or in the region of these channels. Substances which can activate the chlorine or potassium channel receptors, and thus lead to the influx of chloride or potassium ions into the cells, are known as agonist substances.
Thus, the present invention relates to the use of at least one substance which is an agonist of at least one receptor associated with at least one chlorine or potassium channel, present in skin tissue, except for amino acids and derivatives thereof and triazolobenzodiazepines, in and/or for the manufacture of a topical cosmetic or dermatological composition for treating sensitive skin.
The subject of the invention is also the use of at least one substance which is an agonist of at least one receptor associated with at least one chlorine or potassium channel, present in skin tissue, except for amino acids and derivatives thereof and triazolobenzodiazepines, in and/or for the manufacture of a topical cosmetic or dermatological composition for treating, or even eliminating, itching, pruritus, tingling, heating, tautness, stinging and/or erythema.
The invention also relates to the use of at least one substance which is an agonist of at least one receptor associated with at least one chlorine or potassium channel of at least

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