DE102010026696A1 - Use of a grease pencil for medical application of active ingredients on the edge of the eyelid, for e.g. treating allergic diseases of the eye, changes in intraocular pressure, preferably glaucoma, and inflammations of the eye - Google Patents

Abstract

Use of a grease pencil for medical application of active ingredients on the edge of the eyelid, is claimed. The effect is made on the eyelid itself, in the lacrimal film, on the eye surface, in the eyelid, on the meibomian glands, in and around the eye and/or in the lacrimal duct by acting upon the tissue or by resorption. The pencil mass is a composition of carrier substance from all lipids, or from lipids and at least one active ingredient, which is in a position to act on the above-mentioned tissues. The active ingredient comprises e.g. lipids with special properties. Use of a grease pencil for medical application of active ingredients on the edge of the eyelid, is claimed. The effect is made on the eyelid itself, in the lacrimal film, on the eye surface, in the eyelid, on the meibomian glands, in and around the eye and/or in the lacrimal duct by acting upon the tissue or by resorption. The pencil mass is a composition of carrier substance from all lipids, or from lipids and at least one active ingredient, which is in a position to act on the above-mentioned tissues. The active ingredient comprises lipids with special properties (e.g. anti-inflammatory lipids), surface active proteins, lipid-transporting proteins, pigments, medicinal charcoal or soil, active ingredients for influencing the eye pressure, antihistamines and/or other active ingredients to combat allergies, antifungal, keratolytic, steroids, vitamins, lipophilic active ingredients, local anesthetic agents, sunscreens, antioxidants, anti-inflammatory active ingredients (antiphlogistics), anti-microbial peptides for defense against infection and tissue regeneration, other proteins or peptides for tissue differentiation and/or regeneration, anti-viral agents, hormones, active ingredients for improving or inhibiting the innervation, narcotics, alkaloids, antibiotics, essential oils, aphrodisiacs, hallucinogens, active ingredients inhibiting or promoting the blood circulation, mucous membrane decongestant active ingredients, active ingredients acting on nitric oxide production, vaccines and/or adjuvants, substances, which strengthen or dampen the immune reaction (immunomodulator). ACTIVITY : Antiinlammatory; Opthalmological. No biological data given. MECHANISM OF ACTION : None given.

Description

State of the art

Numerous active ingredients are applied directly (topically) to the ocular surface, ie colloquially "into the eye" (eg as a drop, gel, ointment or as a spray), since many active substances are directly targeted or resorbed by target tissue in the area of the eye reach in relatively higher concentrations, as can be achieved in a systemic application, ie by ingestion with the food via the mouth or via the bloodstream by injection. By topical application, therefore, the active ingredients typically achieve their effect on the eye itself without significant systemic side effects.

However, conventional greases ("kohl" or "eyeliner" etc.) applied to the edge of the eyelid have primarily a cosmetic function and are typically not effective on the tear film and / or on the lid margin itself and / or on the ocular surface, and / or in the eyelid and / or on the meibomian glands and / or on and in the eye and / or in the lacrimal ways. Especially a medical effect is therefore typically not intended but even undesirable. Furthermore, common fat sticks have a lipid composition that has little resemblance to the normal, body-own lipid pattern of the lid margins and the tear film, and thus z. B. is unsuitable for lipid substitution of the tear film.

Grease sticks, the pharmacologically active substances (drugs) and / or other specific active ingredients and / or lipids, in a normal, the body's own lipid pattern on the edge of the eyelid and / or the tear film similar type and composition, with application on the edge of the eyelid for acting on the The lid margin itself and / or on the tear film and / or on the ocular surface and / or in the eyelid and / or on the meibomian glands and / or on and in the eye and / or in the lacrimal ways are not known to us.

The disadvantages of the previous application forms of substances on the ocular surface are that in this case a, compared to the amount of tears on the eye, relatively larger amount of substance (as drops, gel, ointment strand, or as a spray) directly on the ocular surface, so colloquially " in the eye ", is introduced. However, this is perceived by many people as unpleasant and as a "fright", since this introduction triggers the eyelid reflex and / or these substances often represent a cold. In addition, excess substance or tear fluid runs out of the eye through the eyelid, and it is not uncommon for the user to be "struck" by the eye and its surroundings smeared and excess substance or tears to be wiped off. Often the visual acuity is at least temporarily limited. All this makes the use of drugs locally (topically) on the eye, which is actually pharmacologically useful and desirable, uncomfortable and cumbersome for many patients.

task

The invention described herein is based on the object of finding an application form of medicinal active substances on the ocular surface ("on the eye") which avoids the disadvantages of previous application forms and at the same time permits simple, pleasant and precise application.

The solution to this problem is, surprisingly, that the application takes place in the form of a stick of fat, from a carrier which is solid at room temperature, which applies the active substance (s) to the edge of the lid. On the edge of the lid, the carrier substances and the active ingredients temporarily form a depot and then reach the naturally occurring lipid film on the edge of the lid by melting the carrier at body temperature and from there to and / or into the tear film and / or on the ocular surface and / or in the eyelid and / or the lid margins (especially the meibomian glands) and / or on and / or in the eye and / or into the lacrimal system. As a result, a new application for oily pencils on the eye is invented for the substitution of the natural lipids of the tear film and / or the ocular surface and / or for the introduction of active ingredients on and / or in the eye and / or its appendages.

This application of the carriers and active ingredients to the lid edge offers various advantages over conventional application forms. On the one hand, the eyelid reflex, which is very pronounced in many people, is avoided because the eyeball itself and / or the transparent cornea is not touched. Furthermore, no cold irritation occurs, which could cause additional frightening. In addition, hardly any lacrimal stimulus is triggered, and no excess amount of substance or tear runs out of the eye over the edge of the lid and must be wiped off. These advantages facilitate the application for the user Significant and make it in the normal daily routine without special tools much easier and more pleasant, as this allows a simple repeated application of the substances.

As a further decisive advantage is applied by the application with the fat stick of the invention, the carrier and / or drug in a temporary depot on the edge of the lid, from which it is continuously released during melting at body temperature on the tear film and / or on the ocular surface and / or in the eyelid and / or the lid margins (especially the meibomian glands) and / or on and / or in the eye and / or into the lacrimal system.

In this way, by the pen according to the invention various active ingredients, as described in the main claim, via an application to the edge of the lid to act on the lid margin itself and / or in the tear film, and / or other tissues of the eye and / or the eye appendage tissue by direct action the tissue or be brought by absorption.

The matrix for carrier materials of fatty sticks typically consists of predominantly anhydrous fat blends with solid or semi-solid waxes and liquid oils. The pen according to the invention should be solid at room temperature. At body temperature, however, after application to the lid margin, the pen base should melt completely or largely. Typical base materials for stick-form preparations of lipids are, for example, liquid oils (eg almond oil, paraffin oil, castor oil), semi-solid constituents (eg coconut fat, cocoa butter, butterfat, vaseline, lanolin), solid constituents (eg water-free wool wax , Beeswax) or high-melting waxes (eg carnauba wax, candelilla wax). In order to produce a satisfactory physical, mechanical and optical quality can continue to be incorporated into the pen mass various adjuvants and additives such. As bodying agents, fillers, perfume, dyes, emulsifiers, additional active ingredients such as vitamins or proteins, light stabilizers, stabilizers, preservatives, antioxidants of various kinds, insect repellants, alcohols, water, antimicrobial agents.

In a preferred form of the pen according to the invention for application to the edge of the lid are fats melting substantially at body temperature, such as. B. butter pure fat, cocoa butter, almond oil used. In a particularly preferred form, substantially the lipids of a type and / or composition are used, which is approximated to the naturally occurring on the lid margin and / or tear film lipids.

The active substance or the combination of active substances is selected from lipids with special properties (eg anti-inflammatory lipids), surface-active proteins, lipid-transporting proteins, pigments, medical coal or earth, active substances for influencing the ocular pressure, antihistamines and / or other active substances for the control of allergies, antimycotics, keratolytics, steroids, vitamins, lipophilic drugs, topical anesthetics, sunscreens, antioxidants, antiinflammatory agents, anti-microbial peptides for the defense against infection and tissue regeneration, other proteins or peptides for tissue differentiation and / or Regeneration, antivirals, hormones, agents that improve or inhibit the innervation, narcotic, alkaloid, antibiotic, essential oils, aphrodisiac, hallucinogen, the blood circulation inhibiting or promoting agents, mucosal decongestants, active ingredients acting on nitric oxide production, vaccines and / or adjuvants, substances that enhance or attenuate the immune response (immunomodulatory agents).

In a preferred form of the pen according to the invention this serves for the lipid substitution of missing and / or lacking natural lipids on the lid margin and / or tear film and / or on and / or in the eye and / or other tissues of the eye and / or the eye appendages. This is at various dysfunctions of the ocular surface and the eye, z. B. in so-called 'dry eye' of importance.

A lipid substitution is so far only performed by preparations containing lipids in the form of lipid-containing solutions as eye drops, ointment, gel or spray. The problem of prior lipid substitution preparations is that the lipids they contain do not correspond in their nature and / or composition to the normal lipids and / or lipid pattern as produced by the marginal glands and ocular surface and / or in and / or on the tear film occurs. In addition, the effect of previous lipid supplement preparations is only relatively short-term, as they are washed out again as part of the constant physiological tear film renewal.

The solution to the problem of adequate lipid substitution lies in the delivery of typical lipids to the typical site, the edge of the eyelid. The lipids are similar in nature and / or composition to those formed by the lid margins, in particular the meibomian glands, in typical proportions and / or occurring in and / or on the tear film. Furthermore, the application brings by the inventive breast these lipids in the natural position on the lid margin. There they can typically form a temporary depot from which they are continuously delivered into and / or onto the tear film and / or the ocular surface and / or into and / or on the eye and / or into the lacrimal ducts.

Mechanical form and equipment of the pencil:

Of particular importance for the fat stick according to the invention for the application of medical active ingredients to the lid margin is a sufficiently small application area, which allows a targeted application of the pen mass on the lid margin, without touching the eye surface (eyeball) or the outer skin of the eyelid appreciable or smear ,

For this purpose, various shapes of the pencil mass of the pen according to the invention are suitable. These are, for example, cylindrical pin bodies with a round diameter which is typically smaller than in a conventional lipstick and is about 0.1 to 2 cm in diameter. In a preferred form, the pencil mass has an oblique cross-section at the top, which allows a targeted and clean application of the pencil mass by the resulting edges. Furthermore, the fat stick according to the invention can also be manufactured as a cylinder with an angular, preferably triangular, cross-section of constant circumference. This makes it possible by applying the fat body, alternating with one of the corners, even with larger pin circumference, which allows greater mechanical stability of the pin to produce a targeted clean order on the lid margin. The shell of the pen according to the invention can be carried out in various ways. It can be wrapped by wood or plastic or other materials.

Various pen bodies, refill cartridges, wrapping materials, pen sleeves, and / or propulsion systems and / or sharpening systems to compensate for abrasion and / or to renew the tip of the pen, which are known in the art, can be prepared according to the invention. It is only essential to the pen according to the invention that it is a fatty stick with which active ingredients are applied to the edge of the lid for acting on the lid margin itself and / or in and / or on the tear film and / or on the ocular surface and / or in the eye Eyelid and / or on the meibomian glands and / or on and / or in the eye and / or in the lacrimal passages by action on the tissue or by resorption.

The pen according to the invention can be combined with a mechanical cleaning device made of suitable material (eg a sponge of suitable hardness, made eg of plastic or other suitable materials), which is used to remove encrustations and / or excess lipid and / or Keratin material is suitable on the lid margin.

This cleaning device can be directly on and / or in the pen, z. B. at the opposite end of the pin side to order the carrier material, and / or be used separately. This cleaning device can be used multiple times or even replaced for single use.

embodiments

The following example is intended to illustrate the invention without limiting it.

Pen for application of active ingredients to the edge of the eyelid, the composition of which is as follows: a. Clarified butter 20-98% b. Waxes of plant and / or chemical origin 0.1-50% c. Other fats of plant and / or chemical origin 0.1-50% d. Vitamin E 0.001-5% e. active substance 0.001-30% f. antioxidant 0.001-10% G. additives 0-5% H. Oils (vegetable, animal or chemical origin) ad 100% (The quantities used are in percent by volume)

Claims (18)

The use of a grease stick for the medical application of active ingredients to the edge of the eyelid. The effect is achieved on the lid margin itself and / or in the tear film and / or on the ocular surface and / or in the eyelid and / or on the meibomian glands and / or on and in the eye and / or in the lacrimal ducts by acting on the tissue or by absorption. The stick composition is a composition of excipients, especially lipids, or of lipids and at least one active ingredient capable of acting on said tissues. The active substance is selected from lipids having particular properties (eg anti-inflammatory lipids), surface-active proteins, lipid-transporting proteins, pigments, medical coal or earth, active substances for influencing the ocular pressure, antihistamines and / or other agents for combating allergies, Antifungals, keratolytics, steroids, vitamins, lipophilic drugs, topical anesthetics, sunscreens, antioxidants, antiinflammatory agents, anti-microbial anti-infective and tissue regeneration peptides, other proteins or peptides for tissue differentiation and / or regeneration, antiviral agents, hormones , Agents that improve or inhibit the innervation, narcotic, alkaloid, antibiotic, essential oils, aphrodisiac, hallucinogen, the blood circulation inhibiting or promoting agents, mucosal decongestants, drugs that nitric oxide produi on vaccines and / or adjuvants, substances that enhance or attenuate the immune response (immunomodulatory agents). Use according to claim 1, whose composition approximates the lipids naturally occurring on the edge of the lid and / or in and / or on the tear film and / or on the ocular surface, for the supplementation and / or substitution of lipids. Use according to claims 1 or 2 for the lipid substitution in and / or on the tear film and / or on the ocular surface, and / or for the substitution of other substances and / or for the application of pharmaceutical active ingredients for the therapy in the case of the so-called dry eye (Keratokonjunctivitis sicca, Sicca syndrome). Use according to claims 1 to 3 for lipid substitution in and / or on the tear film and / or on the ocular surface and / or on and / or in the eyelid and / or on the meibomian glands, and / or for substitution of other substances and / or for application of Pharmaceutical Drugs for Therapy in the Condition of the Dry Eye Induced by Meibomian Gland Dysfunction (MGD) Use according to claims 1 or 2 of the hormones or other active ingredients for influencing the functional state and / or the tissue differentiation of the meibomian glands of the eyelid Use according to claims 1 or 2 of the keratolytic and / or other active ingredients which are suitable for reducing the cornification of the lid margin. Use according to claims 1 or 2 of the hormones and / or other active ingredients for influencing the functional state of other glands of the eye Use according to claims 1 or 2 for the treatment and / or influencing of allergic diseases of the eye Use according to claims 1 or 2 for the treatment of changes in intraocular pressure (especially glaucoma) Use according to claims 1 or 2 for the treatment of terminal inflammations of the eye Use according to claims 1 or 2 containing as active ingredients pigments and / or earths and / or antimicrobial peptides and / or other active substances which are suitable for antibacterial prophylaxis and / or treatment of the eye. Use according to claims 1 or 2 containing as active ingredients pigments and / or earths and / or antimicrobial peptides and / or other substances which are suitable for supporting tissue regeneration on and / or in the eye and / or the appendages of the eye. Use according to claims 1 or 2 for the treatment of infections of the eye Use according to claims 1 or 2, containing vaccines or adjuvants for carrying out and / or imparting ocular vaccinations. Use according to claims 1 or 2 of the active ingredients which are suitable for diagnosis Use of a stick composition as described in claims 1 to 15 or a refill cartridge containing it for producing or refilling a pen according to the invention for the application of active ingredients to the eyelid edge. Use according to claims 1 to 16, in which the active substances are packaged in liposomes or nanotechnological materials or contain the liposomes or nanotechnological materials. Use according to claims 1-17 combined with a mechanical cleaning device of suitable material (eg a sponge of suitable hardness) suitable for the removal of encrustations and / or excess lipid and / or keratinous material on the edge of the lid.