EP4452202A1 - Topische zusammensetzung und applikator dafür zur linderung von chazion - Google Patents

Topische zusammensetzung und applikator dafür zur linderung von chazion

Info

Publication number
EP4452202A1
EP4452202A1 EP22844153.1A EP22844153A EP4452202A1 EP 4452202 A1 EP4452202 A1 EP 4452202A1 EP 22844153 A EP22844153 A EP 22844153A EP 4452202 A1 EP4452202 A1 EP 4452202A1
Authority
EP
European Patent Office
Prior art keywords
advantageously
composition
oil
chalazion
coconut oil
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
EP22844153.1A
Other languages
English (en)
French (fr)
Inventor
Luc Lebreton
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Laboratoires Thea SAS
Original Assignee
Laboratoires Thea SAS
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Laboratoires Thea SAS filed Critical Laboratoires Thea SAS
Publication of EP4452202A1 publication Critical patent/EP4452202A1/de
Pending legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/92Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
    • A61K8/922Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of vegetable origin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/47Euphorbiaceae (Spurge family), e.g. Ricinus (castorbean)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K35/00Medicinal preparations containing materials or reaction products thereof with undetermined constitution
    • A61K35/02Medicinal preparations containing materials or reaction products thereof with undetermined constitution from inanimate materials
    • A61K35/04Tars; Bitumens; Mineral oils; Ammonium bituminosulfonate
    • A61K35/06Mineral oils, e.g. paraffinic oils or aromatic oils based on aromatic hydrocarbons
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/88Liliopsida (monocotyledons)
    • A61K36/889Arecaceae, Palmae or Palmaceae (Palm family), e.g. date or coconut palm or palmetto
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/44Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/31Hydrocarbons
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/37Esters of carboxylic acids
    • A61K8/375Esters of carboxylic acids the alcohol moiety containing more than one hydroxy group
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/06Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/14Decongestants or antiallergics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
    • A61Q17/005Antimicrobial preparations
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/59Mixtures
    • A61K2800/592Mixtures of compounds complementing their respective functions
    • A61K2800/5922At least two compounds being classified in the same subclass of A61K8/18

Definitions

  • the present invention relates to the field of dermatological care linked to eye health, more particularly to the treatment of swellings present in the eyelid. More specifically, the invention relates to a topical composition for the treatment of chalazion.
  • the origin of the swelling of the eyelid is variable and makes it possible to qualify the pathology according to its origin:
  • Blepharitis is a skin inflammation of the eyelid, caused by an infection or an allergy, responsible for swelling.
  • the stye is an infection, in particular bacterial, of the Meibomian gland located in the thickness of the eyelid, responsible for swelling.
  • the chalazion is caused by a non-infectious occlusion of the Meibomian glands, responsible for the inflammatory swelling.
  • the cause of chalazion is not of infectious origin, unlike blepharitis and stye.
  • the Meibomian glands are sebaceous glands located in the epidermis of the eyelids. More precisely, they are located in the cartilage of the eyelids, 30 to 40 per eyelid, oriented perpendicular to the free edge protected by the eyelashes. They secrete an oily, sebum-like substance, which usually mixes with tears to lubricate the surface of the eye. In the event that they do not function correctly, particularly in the case of the chalazion, an excessive accumulation of secretions from the Meibomian glands causes them to become engorged, in particular at the level of their evacuation orifice located on the free edge of the eyelid.
  • the chalazion can be internal or external. External chalazion causes thickening of the eyelid, visible on the eyelid. The eyelid may thus be red and swollen. Internal chalazion causes tearing and mild swelling under the eyelid.
  • Banal benign and not serious
  • the chalazion which has no infectious cause, can resolve itself in several weeks.
  • the chalazion can become bothersome, painful, or even indent the cornea and/or cause blurred vision. In case of persistence, the chalazion must thus be surgically removed, by making an incision in the gland via the conjunctival route and under local anesthesia.
  • the invention relates to a topical composition comprising judiciously chosen ingredients to be associated with a massage gesture, advantageously using a “roll-on” type application device.
  • this constitutes a particularly suitable solution for the management of chalazion, resulting in a reduction of irritation, redness and swelling of the eyelid and therefore improved comfort for the patient.
  • the articles “a” and “an” are used to designate one or more (that is to say at least one) of the grammatical objects of the article.
  • an element designates at least one element, that is to say one or more elements.
  • a range should be taken to have specifically disclosed all possible sub-ranges as well as the individual numerical values within that range.
  • the description of a range such as "from 1 to 6" should be considered to have specifically disclosed sub-ranges such as from 1 to 3, from 1 to 4, from 1 to 5, from 2 to 4, from 2 to 6, from 3 to 6, etc. as well as the individual numbers within that range, for example 1, 2, 2.7, 3, 4, 5, 5.3 and 6. This applies regardless of the extent of the range.
  • abnormal when used in the context of organisms, tissues, cells or components thereof, means those organisms, tissues, cells or components thereof which differ in at least one observable or detectable characteristic (e.g. age, treatment, time of day, etc.) of organisms, tissues, cells or components thereof that exhibit the respective "normal” (expected) characteristic.
  • observable or detectable characteristic e.g. age, treatment, time of day, etc.
  • features that are normal or expected for one type of cell or tissue may be abnormal for another type of cell or tissue.
  • patient refers to any animal or cell thereof, in vitro or in situ, that may be subjected to the methods described herein. document.
  • patient, subject or individual is an animal, preferably a mammal, more preferably a human.
  • a “disease” or “pathology” is a state of health of an animal in which its homeostasis is negatively affected and which, if the disease is not treated, continues to deteriorate.
  • a “disorder” or “dysfunction” is a state of health in which the animal is able to maintain its homeostasis but in which the state of health of the animal is less favorable than it would be in the absence of the disorder. In the absence of treatment, a disorder does not necessarily lead to a deterioration in the state of health of the animal over time.
  • a disease or disorder is "attenuated”("reduced") or “improved” if the severity of a symptom of the disease or disorder, the frequency with which that symptom is experienced by the subject, or both, are reduced . It also includes reversal of disease progression, i.e. stopping the progression of the disease or disorder.
  • a disease or disorder is "cured"("cured") if the severity of a symptom of the disease or disorder, the frequency with which such a symptom is experienced by the patient, or both, are eliminated.
  • a “therapeutic” treatment is a treatment administered to a subject who presents the symptoms (signs) of a pathology, with the aim of reducing or eliminating these symptoms.
  • “treating a disease or disorder” means reducing the frequency or severity of at least one sign or symptom of a disease or disorder experienced by the subject.
  • a treatment is said to be prophylactic when it is administered to prevent the development, spread or aggravation of a disease, in particular if the subject does not or does not yet show the symptoms of the disease and/or for which the disease does not has not been diagnosed.
  • treating a disease or disorder means reducing the frequency or severity of at least one sign or symptom of a disease or disorder experienced by a subject.
  • Disease and disorder are used interchangeably in the context of treatment according to the invention.
  • an “effective amount” or “effective amount” of a compound is that amount of compound that is sufficient to provide a beneficial effect to the subject to whom the compound is administered.
  • the term “therapeutically effective amount” refers to an amount which is sufficient or effective to prevent or treat (in other words delay or prevent development, prevent progression, inhibit, reduce, lessen or reverse) a disease or disorder, including the relief of the symptoms of that disease or disorder.
  • the present invention relates to a topical composition based on:
  • composition according to the invention comprises:
  • coconut oil advantageously refined coconut oil, jojoba oil or avocado oil
  • composition according to the invention may comprise:
  • One of the ingredients of a composition according to the invention is castor oil.
  • Castor oil is a non-food vegetable oil, improperly called “castor oil”. It is obtained from castor bean seeds (Ricinus communis) and is in the form of a colorless or light yellow viscous liquid. The triglycerides of which it is made account, for about 90% of its fatty acids, a Cl 8 fatty acid, ricinoleic acid (or (R)-(+)-12-hydroxy-9Z-octadecenoic acid) which is a hydroxylated omega-9 and forms ricinolein, the major triglyceride of this oil. Its use in cosmetics is largely dedicated to the care of hair, eyelashes and eyebrows.
  • the castor oil represents from 40 to 60%, advantageously from 45 to 55%, even more advantageously 50% by weight of the composition.
  • a second ingredient of a composition according to the invention is a vegetable oil such as coconut oil, advantageously refined coconut oil.
  • coconut oil is available in two main forms, depending on how it is produced:
  • copra oil - Refined coconut oil, known as copra oil, is obtained by hot pressing of the dried albumen, then refined and deodorized. Very rich in saturated fatty acids, refined copra oil is used for its emollient properties.
  • coconut oil is generally in solid form at a temperature below 25°C.
  • it may be useful to heat this ingredient, or even the composition or its application device, above this temperature, as will be described below.
  • jojoba oil or avocado oil can be used.
  • such an oil represents from 20 to 40%, advantageously from 25 to 35%, even more advantageously 30% by weight of the composition.
  • Vaseline constitutes the third ingredient of a composition according to the invention.
  • Vaseline (or petroleum jelly) is a fatty substance of mineral origin, more precisely a petroleum distillate. It is essentially formed of alkanes, of general formula (C n H 2n +2) and is fluid or even pasty at room temperature. Vaseline officinalis is an ointment used as an adjunctive treatment for irritation, burning and dry skin lesions. Its most famous use is the form used for lip care. It also enters into the composition of the majority of cosmetic lotions, used as an excipient.
  • the petroleum jelly represents from 5 to 30% or even from 5 to 20%, advantageously from 10 to 15%, even more advantageously 12% by weight of the composition.
  • a composition according to the invention comprises at least 3 fatty substances.
  • the fatty substances can be of mineral, animal, vegetable or synthetic origin.
  • the composition according to the invention comprises the following 3 fatty substances: a) castor oil; b) coconut oil, advantageously refined coconut oil, jojoba oil or avocado oil; and c) petroleum jelly.
  • the composition according to the invention comprises only the 3 fatty substances mentioned above (a, b and c).
  • composition according to the invention comprises only 2 fatty substances of vegetable origin, advantageously the 2 vegetable oils mentioned above (a and b).
  • the castor oil represents from 40 to 60%, advantageously from 45 to 55%, even more advantageously 50% by weight of the composition; and/or the coconut oil, advantageously refined coconut oil, represents from 20 to 40%, advantageously from 25 to 35%, even more advantageously 30% by weight of the composition; and or
  • - Vaseline represents from 5 to 30% or even from 5 to 20%, advantageously from 10 to 15%, even more advantageously 12% by weight of the composition.
  • a therapeutic active ingredient (or active substance or active principle or active ingredient) is defined as a compound or substance possessing a pharmacological activity recognized in its own right in connection with a given pathology, which is generally associated with the status medicine and obtaining a marketing authorization.
  • the composition according to the invention does not contain a therapeutic agent, in particular for ophthalmological or dermatological purposes.
  • the composition according to the invention may contain a therapeutic agent intended for the treatment of the same pathology as those referred to in the present application or of a different pathology, advantageously ophthalmological or dermatological.
  • a therapeutic agent intended for the treatment of the same pathology as those referred to in the present application or of a different pathology, advantageously ophthalmological or dermatological.
  • a therapeutic agent can be administered separately and therefore not be contained in the composition according to the invention.
  • Such an administration can be carried out simultaneously or staggered over time.
  • a corticosteroid for example dexamethasone or hydrocortisone
  • an antibiotic for example azithromycin, neomycin, norfloxacin, oxytetracycline, ofloxacin or rifamycin
  • a suitable antibiotic will advantageously be used.
  • the composition according to the invention does not contain selenium disulphide (SeS 2 ), glycerol monolaurate, caffeine and/or silk fibroin.
  • composition of the invention may comprise, in addition to the 3 aforementioned ingredients of interest of fatty substance type, a pharmaceutically acceptable carrier.
  • pharmaceutically acceptable means approved by a federal or state government regulatory agency or listed in the United States or European Pharmacopeia or other generally recognized pharmacopoeia for use in animals and humans.
  • carrier means a diluent, adjuvant, excipient or vehicle with which the aforementioned products are administered.
  • the composition comprises at least one agent making it possible to stabilize and homogenize the mixture of the 3 aforementioned ingredients of interest, of fatty substance type, present.
  • one or more agents make it possible to improve the stability of this mixture of fatty substances and/or to improve the miscibility of these fatty substances with each other, in particular of castor oil and petroleum jelly, for avoid a phase shift over time of these fatty substances.
  • agents are typically thickeners, consistency agents or thickening agents (or viscosity agents).
  • Such agents are for example:
  • Glyceryl stearate for example Kolliwax® GMS II from BASF
  • Glyceryl stearate (-20%) + cottonseed oil (-80%) (for example GreenSoft ® 330 Cotton from Greentech);
  • Keto stearlyic alcohol for example Lanette® O from BASF
  • PEG sorbitan monooleate for example Tween® 80 from MERCK
  • Octyldodecanol for example Octyldodecanol from Sigma Aldrich
  • Sorbitan Laurate, Sorbitan Stearate, Sorbitan Oleate e.g. MontaneTM
  • Polyoxyl castor oil for example Kolliphor® RH40 from BASF
  • Glycerol monostearate for example GELEOL® MONO AND DIGLYCERIDES from GATTEFOSSE; or mixtures thereof.
  • a thickening agent is to increase the viscosity of a composition.
  • the quantity of thickening agent is adjusted according to the desired viscosity for the composition, as indicated below.
  • it advantageously represents from 0.5 to 10%, advantageously from 3 to 7%, even more advantageously 5% by weight of the composition.
  • GOTA Gattefossé
  • DIGLYCERIDES DIGLYCERIDES
  • the quantity of emulsifying agent is adjusted according to the hold desired for the composition according to the invention.
  • it advantageously represents from 0.5 to 10%, advantageously from 1 to 5%, even more advantageously 3% by weight of the composition.
  • the composition comprises:
  • coconut oil advantageously refined coconut oil, jojoba oil or avocado oil
  • Compritol® represents from 0.5 to 10%, advantageously from 3 to 7%, even more advantageously 5% by weight of the composition;
  • - glycerol monostearate represents from 0.5 to 10%, advantageously from 1 to 5%, even more advantageously 3% by weight of the composition.
  • glyceryl behenate (Compritol®) and glycerol monostearate (Gangool®) are also fatty substances.
  • a composition according to the invention comprises the 3 fatty substances corresponding to the 3 aforementioned ingredients of interest, including 2 of vegetable origin, and 1 or 2 fatty substances, advantageously 2 fatty substances corresponding to pharmaceutically acceptable carriers, advantageously one or two agents making it possible to stabilize and homogenize the mixture of the 3 ingredients of interest.
  • a composition according to the invention does not contain preservatives, in particular those commonly used in connection with products of the cream and ointment type to be applied to the skin.
  • the composition according to the invention is formulated according to routine procedures for a composition suitable for topical administration in humans.
  • the zone targeted by the administration is advantageously the skin, and more particularly the eyelids.
  • the mucous membranes, the conjunctiva and/or the cornea are not targeted.
  • the composition according to the invention is in the form of a gel, an emulsion, an oil, a balm, a cream or an ointment, of consistency homogeneous and suitable for spreading in a wide range of temperatures, while avoiding its flow, especially in the eyes and without leaving a greasy film on the targeted area.
  • the composition according to the invention is homogeneous and does not phase-shift between 4°C to 40°C.
  • the composition according to the invention has a homogeneous consistency at a temperature of between 20° C. and 30° C., typically at room temperature.
  • such a composition contains no aqueous phase or a reduced quantity of aqueous phase in order to maintain microbiological stability without adding a preservative.
  • this composition is compatible with administration using a device of the “roll-on applicator” type (also called “roll-on”).
  • a “roll-on” is a receptacle or container, such as a tube or a bottle, the outlet orifice of which is an advantageously rotating ball and which releases the composition which it contains during contact between the ball and the surface to be treated. This release can be aided by a slight pressure exerted on the container.
  • a device makes it possible to preserve a composition and to apply it locally, in a controlled manner (deposition of a determined quantity of the composition not soiled by contact with the fingers on a targeted zone).
  • it can be equipped with a cap or cover making it possible to keep the composition protected from air, water and any external contamination (pollutants, dust, etc.).
  • the container transparent or opaque, is made of plastic material, for example polyethylene (PE), advantageously high density polyethylene (HDPE) such as the Polyfoil® device marketed by Neopac.
  • PE polyethylene
  • HDPE high density polyethylene
  • COEX tubes can also be used: these are coextruded polyethylene (PE) tubes lined with a barrier layer of ethylene vinyl alcohol (EVOH).
  • EVOH ethylene vinyl alcohol
  • the ball for example with a diameter of 10 mm, can be made of ceramic, plastic or metal.
  • the metal ball for example stainless steel, makes it possible to obtain a more effective massaging effect.
  • the cap is advantageously made of plastic material which can be covered with a metal layer, for example polypropylene (PP), with an advantageously rigid structure.
  • PP polypropylene
  • composition according to the invention has a texture suitable for topical application around the eye, advantageously using such a device.
  • the composition according to the invention can be sterilized before and/or after its packaging in the application device, advantageously the roll-on applicator.
  • the sterilization techniques that can be implemented are well known to those skilled in the art.
  • a composition according to the invention can be filtered before it is packaged.
  • the present invention also relates to compositions and devices as defined above for the prevention, including the prevention of recurrence, the management and/or the treatment of certain pathologies, in particular swelling of the eyelid.
  • the pathologies linked to, associated with, resulting from or caused by a dysfunction of the Meibomian glands are particularly targeted in the context of the present invention.
  • the present invention also concerns:
  • compositions as described above for the treatment of swelling of the eyelid advantageously of pathologies linked to a dysfunction of the Meibomian glands, even more advantageously of the chalazion;
  • a roll-on applicator comprising a composition as described above for the management of swelling of the eyelid, advantageously of pathologies linked to a dysfunction of the Meibomian glands, even more advantageously of the chalazion;
  • the amount of the composition of the invention, in particular of the three ingredients of interest mentioned above, effective in the targeted treatment can be determined by standard clinical techniques. Additionally, in vivo and/or in vitro assays, such as those described in the examples below, may optionally be used to help predict optimal dosage ranges. The precise dose to be employed may also depend on the severity of the disease, and should be decided according to the judgment of the practitioner and the conditions of each patient.
  • the composition according to the invention is administered daily, with a minimum of twice a day, advantageously in the morning and in the evening, and up to 6 times a day. It should be noted that apart from the sequences administration of the composition, the roll-on applicator can be used alone, without releasing the composition, for the advantageous physical effect of the massage, in particular the decongestion of the Meibomian glands.
  • the treatment is implemented as soon as the pathology appears (swelling, redness, irritation, ... at the level of the lower or upper eyelid), even more advantageously after diagnosis by a doctor or an ophthalmologist.
  • the treatment can last several days or even weeks or even months, advantageously until the symptoms completely disappear.
  • the treatment can also be taken as a preventive measure, in particular of recurrence.
  • the area to be treated can be:
  • composition according to the invention advantageously the administration device containing it, are brought to a suitable temperature, for example by friction between the hands.
  • the composition according to the invention is advantageously applied by massage using the ball-point applicator, namely back and forth, circular and/or longitudinal movements on and /or along the eyelid to be treated.
  • a longitudinal massage is recommended but a circular massage is possible.
  • a composition according to the invention ensures an easy and pleasant massage function of the eyelids in order to unclog the large meibomian glands at the origin of the chalazion; ensures a function of reinforcement of the cutaneous barrier function making it possible to limit the evaporation of water, and thus protect the eyelid from dehydration; is compatible with a roll-on tube, allowing a delicate massage of the eyelids by simply rolling the ball over the eyelids to apply the product; has a soft and viscose ointment-like texture so as not to run out of the tube at room temperature; liquefies from the start of the massage to ensure the lubrication necessary for massaging the eyelids; does not leave a greasy and sticky finish on the skin.
  • the invention is further illustrated using a composition based on castor oil, coconut oil and petroleum jelly packaged in a metal ball applicator and in connection with the treatment of chalazion.
  • composition according to the invention may have the following formula:
  • composition in table 1 above has a viscosity value equal to 3800 mPa.s, suitable for application using a ball-point applicator.
  • the composition in Table 1 is packaged in a ball-point applicator, namely a Polyfoil® tube (capacity, for example, 10 mL) equipped with a metal ball in stainless steel with a diameter of 10 mm.
  • a removable polypropylene (PP) cap is placed on the ball to allow the closure of the applicator.
  • composition in Table 1 is applied using the ball-point applicator described in point 3-1 as soon as the first signs of chalazion appear.
  • the cap should be removed.
  • the ball of the applicator is placed on the chalazion and on the skin of the eyelid to be treated. Gently press the tube and begin a longitudinal massage along the eyelid for 1 minute, then possibly continue with a rotational massage centered on the swelling.

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EP22844153.1A 2021-12-23 2022-12-23 Topische zusammensetzung und applikator dafür zur linderung von chazion Pending EP4452202A1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR2114348A FR3131214A1 (fr) 2021-12-23 2021-12-23 Composition topique et son applicateur, destines a soulager le chalazion
PCT/EP2022/087784 WO2023118591A1 (fr) 2021-12-23 2022-12-23 Composition topique et son applicateur, destines a soulager le chalazion

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EP4452202A1 true EP4452202A1 (de) 2024-10-30

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EP22844153.1A Pending EP4452202A1 (de) 2021-12-23 2022-12-23 Topische zusammensetzung und applikator dafür zur linderung von chazion

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US (1) US20250064881A1 (de)
EP (1) EP4452202A1 (de)
CA (1) CA3240302A1 (de)
FR (1) FR3131214A1 (de)
MX (1) MX2024007805A (de)
WO (1) WO2023118591A1 (de)

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BRPI0808410A2 (pt) * 2007-02-28 2015-06-23 Aciex Therapeutics Inc Métodos e composições para normalizar secreções da glândula meibomiana
US20090130220A1 (en) * 2007-11-20 2009-05-21 Johnson Pamela A Cosmetic composition having pomace olive oil
ITFI20130128A1 (it) * 2013-05-30 2014-12-01 Biodue S P A Soluzione per l'igiene dei margini palpebrali e dispositivo per la sua applicazione.
CN105792848B (zh) * 2013-11-29 2021-04-09 乐敦制药株式会社 眼科用或耳鼻科用水性组合物

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FR3131214A1 (fr) 2023-06-30
WO2023118591A1 (fr) 2023-06-29
CA3240302A1 (fr) 2023-06-29
US20250064881A1 (en) 2025-02-27
MX2024007805A (es) 2024-07-09

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