Drug – bio-affecting and body treating compositions – Inorganic active ingredient containing – Alkali or alkaline earth chloride
Utility Patent
1996-04-10
2001-01-02
Fay, Zohreh (Department: 1614)
Drug, bio-affecting and body treating compositions
Inorganic active ingredient containing
Alkali or alkaline earth chloride
C424S665000, C514S912000
Utility Patent
active
06168809
ABSTRACT:
The present invention relates to the use of an alkaline-earth metal salt for the preparation of a pharmaceutical composition for treating, especially via the topical route, ocular and/or palpebral pruritus and/or ocular and/or palpebral dysesthesia. It also relates to the use of an alkaline-earth metal salt in a cosmetic composition intended for the care of or for applying make-up to the eyes or to the eyelids as well as to a process for the care of and/or for applying make-up to sensitive eyes.
Some patients very frequently have itching sensations or pruritus and dysesthetic sensations at the level of the eyes and the eyelids without always knowing their precise cause. They may also be pruritus or dysesthetic sensations of allergic origin.
Dysesthetic sensations are understood to mean sensations of burning or of overheating, pricking, formication, discomfort and stabbing pain. These sensations may be combined with reddening.
All these ophthalmic signs may, in addition, be combined with rosacea and optionally with conjunctivitis.
Among the factors which initiate ophthalmic or palpebral prurigenous or dysesthetic crises, there may be mentioned rapid temperature variations, heat and especially exposure to ultraviolet or infrared radiation, relatively low humidity, exposure to violent winds or to air currents (fan, air conditioner), application of surfactants (shampoo), exposure to toxic or irritant vapours (solvents) or to dust, drops or irritant ophthalmological topical drugs, irritant dermatological or cosmetic palpebral topical drugs (alpha-hydroxyacids, retinoids), or the use of some cosmetics even when these are not known to be particularly irritant. Like other factors which initiate ocular or palpebral pruriginous or dysesthetic crises, there should be included, in addition, allergens such as especially pollen, animal hair, acarians and moulds.
Up until now, the pathological mechanism of these signs was poorly known and ocular and/or palpebral dysesthesia was treated with corticoids and also local antiseptics in the form of an ophthalmic ointment or as drops.
Corticoids are relatively effective for reducing the above symptoms but unfortunately they have side effects which are very often detrimental, such as atrophies. Furthermore, they create sensitivity to mycotic or bacterial infections and their kinetics of action is often slow (several minutes to a few hours). Moreover, their chronic use may lead to drug dependence. In addition, their action is not immediate and the dysesthetic sensations last for several minutes.
The need therefore exists for a treatment of ocular and palpebral pruritus and dysesthesia having immediate effect, which does not have the above disadvantages.
The subject of the present invention is precisely the use of one or more alkaline-earth metal salts for treating these conditions.
The Applicant observed that ocular and/or palpebral dysthesthesia was linked to the stimulation of the nerve fibres and to the release, by the sensitive nerve endings, of neuropeptides such as for example substance P and CGRP (Calcitonin Gene Related Peptide) as well as pro-inflammatory mediators liberated as a result of the attachment of certain neuropeptides (especially substance P) onto the mastocyte receptors. These pro-inflammatory mediators are more particularly histamine, heparin, serotonin, interleukin-1 (IL1), interleukin-6 (IL6), interleukin-8 (IL8) and Tumor Necrosis Factor-alpha (TNF-alpha). Recruitment of the neutrophilic white blood cells by certain neuropeptides (especially CGRP) is also involved in this inflammatory process.
No-one had envisaged using, up till now, alkaline-earth metal salts to treat ocular or palpebral pruritus and/or dysesthesia.
Accordingly, the subject of the present invention is the use of at least one salt of at least one alkaline-earth metal for the preparation of a pharmaceutical or dermatological composition for treating ocular or palpebral pruritus and/or ocular or palpebral dysesthesia.
The application of compositions containing one or more salts of one or more alkaline-earth metals to the eyes or the eyelids makes it possible to obtain a marked decrease or even a complete disappearance of the dysesthetic sensations and ocular pruritus; a preventive and curative, soothing and alleviating effect is very rapidly observed, and in any case much more rapidly than with corticoids, on the eyes and the eyelids. In addition, no drug dependence is noted.
By virtue of the alkaline-earth metal salts, it is in addition possible to conceive cosmetic products for sensitive eyes and in particular lotions for removing make-up or for cleaning the eyes, make-up products for sensitive eyes and especially eye shadows, mascaras, pencils or eye liners for sensitive eyes.
Accordingly, the subject of the invention is also the use of at least one salt of at least one alkaline-earth metal in a cosmetic composition containing a cosmetically acceptable medium, intended for sensitive eyes.
The subject of the invention is thus a process for the care of or for applying make-up to sensitive eyes and a process for the treatment of sensitive eyes, which consists in applying, to the eyelids, the eyelashes or under the sensitive eyes, a composition containing at least one salt of at least one alkaline-earth metal in a cosmetically or pharmaceutically acceptable medium.
The object of the invention is also a cosmetic, pharmaceutical or dermatological composition for sensitive eyes containing, in a cosmetically or pharmaceutically or dermatologically acceptable medium, at least one alkaline-earth metal and at least one neuropeptide antagonist and/or at least one inflammation mediator antagonist.
The composition of the invention contains a cosmetically, pharmaceutically or dermatologically acceptable medium, that is to say a medium compatible with the skin and the eyes. The composition containing the salt(s) of (an) alkaline-earth metal(s) is applied especially via the topical route.
As alkaline-earth metal salts which can be used in the invention, there may be mentioned barium, calcium, magnesium, strontium and/or beryllium salts. These salts may be for example carbonates, bicarbonates, sulphates, glycerophosphates, borates, chlorides, nitrates, acetates, hydroxides, persulphates as well as salts of &agr;-hydroxyacids (citrates, tartrates, lactates, maleates) or of fruit acids, or alternatively aminoacid salts (aspartate, arginate, glycocholate, fumarate) or fatty acid salts (palmitate, oleate, caseinate, behenate). For example, the salt is chosen from calcium or magnesium nitrate, calcium or magnesium borate, calcium or magnesium chloride, calcium or magnesium sulphate and calcium or magnesium acetate. Advantageously, the salt is a magnesium or better still a strontium salt and in particular a chloride or a nitrate.
The Applicant found surprisingly that the ability of the alkaline-earth metal salts to treat sensitive eyes was due especially to the fact that these salts were inhibitors of the release of TNF-alpha, or even inhibitors of the release of neuropeptides such as CGRP and substance P.
In the compositions according to the invention, the alkaline-earth metal salts are used preferably in a quantity ranging from 0.01 to 20% of the total weight of the composition, and in particular in a quantity ranging from 0.1 to 15% of the total weight of the composition or even better from 0.5% to 8%.
The compositions according to the invention can be provided in any gallenic form normally used for a topical application; the composition can be provided especially in the form of aqueous, aqueous-alcoholic or oily solutions, or of lotion or serum type dispersions, of emulsions of liquid or semiliquid consistency of the milk type, which are obtained by dispersing a fatty phase in an aqueous phase (O/W) or conversely (W/O), or of suspensions or emulsions of soft, semisolid or solid consistency of the cream or aqueous or anhydrous gel type, of microemulsions, of microcapsules, of microparticles, of vesicular dispersions of the ionic and/or nonionic type, of compacted or cast powder
Breton Lionel
De Lacharriere Olivier
Burns Doane Swecker & Mathis L.L.P.
Fay Zohreh
Societe L'Oreal S.A.
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