Use of complexes for the preparation of compositions for the...

Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Cosmetic – antiperspirant – dentifrice

Reexamination Certificate

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C424S520000, C424S195110, C514S002600, C514S023000, C514S458000, C514S844000, C514S937000

Reexamination Certificate

active

06352698

ABSTRACT:

The invention relates to new dermocosmetic and pharmaceutical compositions which are useful for improving and treating hyperreactive skin conditions and more generally allergic-type reactions and/or intolerance phenomena, whether they are caused by external factors or factors intrinsic to the individual.
Increasing numbers of children and adults are in fact exhibiting skin described as “sensitive”. During a recent study in France, 70% of the women questioned stated that they had sensitive facial skin. The notion of sensitive skin covers an array of outward signs comprising reactive skin and intolerant skin. Atopic skin can also be included therein. These skin types are sometimes incorrectly known as “allergic ” by the subjects; however, while an allergic component can sometimes be evoked in the symptoms of sensitive skin, it may not be restricted to it. The triggering factors can be environmental attacks such as wind, pollution, temperature variations, excessively hard water or ill-suited hygiene, cosmetic or care products; these phenomena can also be associated with stress or emotions felt by the subject, some diets or the taking of medicaments. In addition, there exists individual predisposing factors (in particular neurological or hormonal) or familial predisposing factors which amplify these reactions.
Generally, the subject feels cutaneous discomfort which can manifest itself by subjective and/or objective signs. The skin readily gives off stabbing pains, itches or smarts and the subject may experience feelings of warmth, pricking or burning on the skin. The skin can redden or desquamate. Xerosis, seborrhoeic dermatitis, telangiectasias, vesicles or even oedema is observed, on an irregular basis.
In the most serious cases, dermatological complaints of immunoallergic type, such as atopy, eczema or neurodermatitides, may be observed.
This condition can manifest itself on the skin, the mucous membranes or the scalp. In the latter case, it may be associated with a dandruff condition and/or alopecia.
Until now, attempts have been made to prevent the appearance of these reactions by limiting the presence, in dermocosmetological formulations, of components known to be allergizing. However, it would be desirable to be able to have available truly active compositions which are capable of preventing or of relieving these symptoms by decreasing the reactivity of the skin and by improving its resistance to the triggering factors.
The Applicant Company has now found, unexpectedly, that these aims could be achieved by the use of a composition containing a synergic combination producing an active hypoallergenic complex.
Such a complex will, in addition, improve the receptivity of the skin towards other active principles.
For this reason, the subject of the present invention is a dermocosmetic composition, characterized in that it contains an immunomodulatory or hypoallergenic synergic combination of at least two components, each of these components exhibiting at least one of the following activities:
a) anti-radical
b) anti-inflammatory
c) anti-allergic,
the said components being chosen so that at least two activities a), b) or c) are present in the composition.
The subject of the invention is more particularly the use of at least two compounds chosen from components having an a) anti-radical, b) anti-inflammatory and c) anti-allergic activity for the preparation of a composition, in particular an immunomodulatory composition, exhibiting at least two of the a), b) and c) activities intended for the treatment of sensitive and/or allergic skin; according to one of its aspects, the a), b) and c) activities are exerted in the composition.
Indeed, the Applicant Company has been able to show that the combination of active principles having complementary anti-allergic, anti-radical and/or anti-inflammatory activities made it possible to effectively combat the phenomena associated with the appearance of the symptoms of sensitive and/or intolerant skin or of immunoallergic complaints, preferably via a synergy of the activities of the components.
The components forming part of the formulations according to the invention can be purified or unpurified molecules, synthetic or extracted products, mixtures of active principles or extracts which have been subjected to one or a number of fractionation stages from a starting material of plant or animal origin.
Preferably, if two components present in the formulation show an activity of the same type, it will be exerted by the involvement of a different mechanism.
As regards the anti-inflammatory activity, it can in particular be provided by prostaglandin inhibitors (cyclooxygenase route), inhibitors of cytokine production and inhibitors of the production of leukotrienes (LTB, for example, lipoxygenase route).
The component or components with anti-inflammatory activity advantageously exhibit an inhibiting activity on the production of IL-1, IL-2, IL-4, IL-5, IL-12 and/or TNF-&agr; (Tumour Necrosis Factor).
The anti-inflammatory function can also have the consequence of decreasing the production of reactive nitro derivatives by the cells, limiting the generation of free radicals.
However, anti-radical activity is understood to mean components which are preferably chosen from free-radical scavengers, anti-lipoperoxidants and stimulants of the endogenous production of the enzymes which degrade free radicals.
Free radicals, by definition, are neutral or charged chemical species which have an unpaired electron. This “single electron” endows them with specific chemical properties and a short lifetime. They are reaction intermediates which will be stabilized by combination or transfer and can be the source of a chain reaction. Mention may be made, among free radicals, of the superoxide anion O
2
the hydroxyl radical OH , NO or peroxides.
Enzymes which are active in endogenous defense systems against free radicals are, for example, SOD (or superoxide dismutase), catalase or glutathione peroxidase; attempts will be made to stimulate the production of these enzymes or they can be introduced exogenously.
The components providing the anti-allergic function in the composition according to the invention are preferably chosen from inhibitors of lymphocyte proliferation, inhibitors of the internalization of the molecules of the major histocompatibility complex (HLA-DR, for example) or inhibitors of cytokine production. They are advantageously capable of decreasing the production of the mediators of the inflammation which occurs during allergic phenomena.
As indicated above, the composition will exhibit at least two of the anti-radical, anti-inflammatory and anti-allergic activities. In addition, the components of the active hypoallergenic complex will be chosen so that a synergy is exerted via different mechanisms at the basis of the same activity.
Each component will preferably contribute, via a number of parameters, to the overall activity of the composition according to the invention.
The composition according to the invention advantageously has a marked inhibiting activity on the synthesis and/or the expression of neuromediators, in particular with respect to cutaneous cells, resulting from a synergy of the activities of its different components. The neuromediators can be chosen from the group comprising neurokinines A (NKA) and B (NKB), vasoactive intestinal polypeptide (VIP), calcitonin gene related peptide (CGRP), neuropeptide Y (NPY), neurotensin (NT), somatostatin (SOM), gastrin releasing peptide (GRP), nerve growth factor (NGF), PGP 9.5 (Protein Gene Product 9.5) and bombesin.
Components making possible the preparation of dermocosmetic compositions according to the invention can advantageously be chosen from the following group: Ginkgo biloba and its extracts, iramine, D-panthenol, &bgr;-sitosterol, modulene, &agr;-tocopherol and its derivatives, &bgr;-glucan and its derivatives, eicosapentanoic acid, 18&bgr;-glycyrrhetinic acid, glycyrrhetinic acid monoglucuronide, stearyl glycyrrhetinate, Scutellaria extract, lactoferrin, green tea and its extracts, vitamin

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