WO2018013732A1 - Composition d'écran solaire ophtalmique non irritante, non masquante et photostable - Google Patents

Composition d'écran solaire ophtalmique non irritante, non masquante et photostable Download PDF

Info

Publication number
WO2018013732A1
WO2018013732A1 PCT/US2017/041784 US2017041784W WO2018013732A1 WO 2018013732 A1 WO2018013732 A1 WO 2018013732A1 US 2017041784 W US2017041784 W US 2017041784W WO 2018013732 A1 WO2018013732 A1 WO 2018013732A1
Authority
WO
WIPO (PCT)
Prior art keywords
solution
percent
active ingredient
ophthalmic
weight
Prior art date
Application number
PCT/US2017/041784
Other languages
English (en)
Inventor
A. Ebbie SOROUDI
Original Assignee
Soroudi A Ebbie
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 Soroudi A Ebbie filed Critical Soroudi A Ebbie
Priority to EP17828416.2A priority Critical patent/EP3484586A4/fr
Priority to CN201780056098.4A priority patent/CN109803725A/zh
Priority claimed from US15/648,107 external-priority patent/US10695290B2/en
Publication of WO2018013732A1 publication Critical patent/WO2018013732A1/fr

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/27—Zinc; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/28—Zirconium; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/29—Titanium; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/35—Ketones, e.g. benzophenone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
    • A61K8/365—Hydroxycarboxylic acids; Ketocarboxylic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/37—Esters of carboxylic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/41—Amines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
    • A61K8/445—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof aromatic, i.e. the carboxylic acid directly linked to the aromatic ring
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/46—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing sulfur
    • A61K8/466—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing sulfur containing sulfonic acid derivatives; Salts
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/494—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom
    • A61K8/4946—Imidazoles or their condensed derivatives, e.g. benzimidazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/494—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom
    • A61K8/496—Triazoles or their condensed derivatives, e.g. benzotriazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/494—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom
    • A61K8/4966—Triazines or their condensed derivatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00—Barrier 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
    • A61Q17/04—Topical preparations for affording protection against sunlight or other radiation; Topical sun tanning preparations

Definitions

  • the present invention generally relates to a sunscreen formulation designed for protecting the eyes including the conjunctiva, cornea, lens, and retina. More particularly, the present invention relates to a non-irritating sunscreen that is applied directly onto the ocular surface of the eye for protection from ultraviolet radiation.
  • UVA Ultraviolet radiation is part of the electromagnetic spectrum that reaches the earth from the sun. It has wavelengths shorter than visible light, making it invisible to the naked eye. These wavelengths are classified as UVA, UVB, or UVC. UVA has the longest of the three at 320-400 nanometers. UVA is further divided into two wave ranges, UVA I, which measures 340-400 nanometers (nm, or billionths of a meter), and UVA II which extends from 320-340 nanometers. UVB ranges from 290 to 320 nm. With even shorter rays, most UVC is inevitably absorbed by the ozone layer and does not reach the earth.
  • Photoconjunctivitis and Photokeratitis describe conditions where ultraviolet radiation inflames and/or damages the delicate structures of the ocular surface (the conjunctiva and the cornea, respectively). UV exposure to the eyes (either direct or indirect) can cause severe redness, dryness, irritation, tearing, photosensitivity, and pain. This pain can be so severe as to cause chemosis and sloughing of the corneal epithelium with resultant scarring and even permanent vision loss.
  • Baron (Patent Number 5,041 ,244) described an ophthalmic liquid sunglass that is composed of dosages of chromophores in aqueous gel to block transmission of all or various spectrums of UV from the eyes. He has described the use of high molecular weight polymers which form viscous dispersions and can be used to prolong the curation of the chromophore when the gel is applied to the eye. This alone would cause significant blurring of the users' vision. Further, there is no mention of the irritation that's caused once this mixture is directly applied to the eye. This makes Baron's invention not entirely practical for frequent use by the public.
  • the formulation must take into effect the fact that the ingredients used must be photostable (i.e., that the UV filters don't break down or degrade once exposed to UV light).
  • the Smith patent proposes the use of avobenzone or octisalate, two of the most unstable sunscreen agents. This would further render this formulation ineffective for its proposed use.
  • This present disclosure describes the composition of a sunscreen solution, suspension, emulsion, and/or an ointment that is designed to be directly applied to the eye itself to protect it from UV damage without causing significant irritation to the eye or affecting the users' vision.
  • the present invention fulfills these needs for a new form of UV radiation protection and provides other related advantages.
  • compositions that are manufactured as ophthalmic solutions, emollients, creams, or ointments that can be instilled directly on the eyes. It is understood that the use of the term "ophthalmic solution” shall include emollients, creams and ointments that can be instilled directly on the eyes.
  • An embodiment of the present invention of an ophthalmic sunscreen solution comprises: a first portion comprising 0.25 percent to 15 percent by weight, wherein the first portion comprises at least one of the following: bemotrizinol;
  • inventions may include a third portion comprising an inorganic active ingredient comprising 0.25 percent to 15 percent by weight.
  • the inorganic active ingredient may be selected from the group consisting of titanium dioxide, zinc oxide, iron oxide, zirconium oxide, cerium oxide and mixtures thereof and wherein the inorganic active ingredient is in micronized form or nanoparticle form.
  • Other embodiments may include a third portion comprising an organic active ingredient comprising 0.25 percent to 15 percent by weight and wherein the organic active ingredient is in micronized form or nanoparticle form.
  • the organic active ingredient may be selected from the group consisting of dioxybenzone, octinoxate, octisalate, homosalate, avobenzone, octocrylene, para-aminobenzoic acid, cinoxate, methyl anthranilate, octocrylene, padimate O, ensulizole,
  • the first portion may comprise 0.25 percent to 1 0 percent by weight.
  • the first portion may comprise 0.25 percent to 5 percent by weight.
  • the liquid vehicle base may be water-based or oil-based.
  • emulsifiers may be selected from the group consisting of a silicone-based emulsifier, a polyethylene glycol emulsifier, a polysiloxane emulsifier, a glyscoside emulsifier, an acrylic-based emulsifier and combinations thereof.
  • the emulsifier may comprise polysorbate, carbomer and/or castor oil.
  • emollients may be selected from the group consisting of aloe extracts, oleaginous esters, ethers and combinations thereof.
  • the emollient may comprises an anhydrous lanolin and/or an oleaginous ingredient.
  • Other embodiments may include a preservative, wherein the preservative is an ionic-buffered preservative, a detergent or an oxidizing detergent.
  • the ophthalmic sunscreen solution may be in the form of an eye drop, a suspension, an emulsion, or an ointment, all of which are synthesized specifically to be applied onto the ocular surface.
  • ophthalmic demulcent may include an ophthalmic demulcent, wherein the ophthalmic demulcent is a cellulose derivative demulcent or a liquid polyol.
  • Other embodiments may include a hypertonicity agent, wherein the hypertonicity agent is sodium chloride.
  • FIG. 29 Other embodiments may include an ophthalmic lubricant or an ophthalmic astringent.
  • the first portion may be in micronized or nanoparticle form.
  • Another embodiment of the present invention includes an ophthalmic solution comprised of diluted forms of an inorganic active ingredient such as titanium dioxide, zinc oxide, iron oxide, zirconium oxide, cerium oxide, or mixtures thereof.
  • This composition may also contain a weak concentration of an organic active ingredient such as avobenzone, octinoxate, octisalate, homosalate, octocrylene, para- aminobenzoic acid, cinoxate, dioxybenzone, methyl anthranilate, octocrylene, padimate O, ensulizole, sulisobenzone, trolamine salicylate, ecamsule, and mixtures thereof.
  • an organic active ingredient such as avobenzone, octinoxate, octisalate, homosalate, octocrylene, para- aminobenzoic acid, cinoxate, dioxybenzone, methyl anthranilate, octocry
  • An example embodiment of the present invention includes an ophthalmic sunscreen composition which is comprised of anywhere from 0.25% to up to 15% zinc oxide by weight.
  • Another example of this invention includes embodiments comprised of octinoxate and/or octisalate.
  • Another example of this invention includes embodiments comprised of an emulsifier, silicone- or acrylic-based, glycosides, polyethylene glycols, or a mixture thereof.
  • sunscreen composition comprising an emulsifier selected from the group consisting of Arlacel P 135, DC 901 1 silicone elastomer, Abil WE 09, Abil EM-90, Emulgade 68/50, Simulgel A, Simulgel EG, and mixtures thereof.
  • an emulsifier selected from the group consisting of Arlacel P 135, DC 901 1 silicone elastomer, Abil WE 09, Abil EM-90, Emulgade 68/50, Simulgel A, Simulgel EG, and mixtures thereof.
  • Another example of this invention includes embodiments comprised of an emollient.
  • Said emollient may be selected from the group consisting of Aloe extracts, ethers, oleaginous esters, and mixtures thereof.
  • Another example of this invention includes embodiments comprised of an emollient selected from the group consisting of actiphyte of aloe vera, Cetiol OE, Lexol IPL, octyl palmitate, neopentyl glycol heptanoate, neopentyl glycol
  • Trivent NP-13 is alkyl benzoate, and mixtures thereof.
  • Examples of ophthalmic sunscreen compositions of the present invention provide an SPF of up to 50 or higher. As the eyes are usually not in direct exposure to UV radiation as opposed to the skin, such high SPF ratings may not be necessary for the present invention, and as such, the concentration of the active (and inactive) ingredients may be much lower than those proposed for dermal use.
  • compositions of the present invention are now described, but are not limited to these embodiments.
  • Ophthalmic sunscreen compositions according to the present invention may contain a liquid vehicle base, such as an artificial tear formulation, which may be water and/or oil-based, or an ophthalmic suspension or ointment and include at least one inorganic and at least one organic active ingredient.
  • a liquid vehicle base such as an artificial tear formulation, which may be water and/or oil-based, or an ophthalmic suspension or ointment and include at least one inorganic and at least one organic active ingredient.
  • Inorganic active ingredients may include, but not be limited to zinc oxide, titanium dioxide, iron oxide, zirconium oxide, and cerium oxide, optionally in micronized form as to prevent blurred vision when applied.
  • Organic active ingredients may include, but not be limited to
  • dioxybenzone octinoxate, octisalate, homosalate, avobenzone, octocrylene, para- aminobenzoic acid, cinoxate, methyl anthranilate, octocrylene, padimate O, ensulizole, sulisobenzone, trolamine salicylate, and ecamsule.
  • the inactive ingredients of the present invention shall also include emulsifier(s) and/or emollient(s). Silicone-based emulsifiers like polyethylene glycols, polysiloxanes, glycosides are excellent choices. Acrylic-based emulsifiers, and mixtures thereof may also be used safely for the present preparation.
  • Emollients may include, but not be limited to aloe extracts, oleaginous esters, and ethers, or a combination thereof.
  • the composition of the present invention shall also include, but not be limited to preservatives, chelating agents, and/or antioxidants.
  • An ophthalmic sunscreen solution can be synthesized by mixing 5% micronized zinc oxide and 3% octinoxate in an ophthalmic artificial tear formulation.
  • This solution may contain carboxymethylcellulose sodium 0.1 %; glycerin 0.25%; boric acid; calcium chloride dihydrate; erythritol; levocarnitine; magnesium chloride hexahydrate; potassium chloride; purified water; sodium borate decahydrate; and sodium citrate dihydrate.
  • An ophthalmic sunscreen solution can be synthesized by mixing a range of 5% micronized titanium dioxide and 3% octisalate in an ophthalmic artificial tear solution.
  • An ophthalmic sunscreen ointment can be synthesized by mixing a range of 5% micronized zinc oxide and 3% octinoxate in an ophthalmic ointment consisting of hypromellose, boric acid, sodium perborate, phosphonic acid, potassium chloride, purified water, and sodium chloride.
  • Tinosorb® preferably Tinosorb M, lUPAC name 2,2'- methanediylbis[6-(2H-benzotriazol-2-yl)-4-(2,4,4-trimethylpentan-2-yl)phenol]
  • Tinosorb® is the trade name of a number of UV absorbers including the following: bemotrizinol (Tinosorb® S); bisoctrizole (Tinosorb® M); tris- biphenyl triazine (Tinosorb® A2B); and octyl methoxycinnamate (Tinosorb® OMC).
  • Tinosorb® M is a photostable sunscreen composition that possesses multiple chemical characteristics over all other sunscreen agents currently available, that render it as an ideal candidate for use in a sunscreen formulation that is designed specifically to be directly applied to the ocular surface.
  • Bisoctrizole (marketed by BASF as Tinosorb® M and by MPI as Milestab 360, INCI methylene bis-benzotriazolyl tetramethylbutylphenol) is a benzotriazole-based organic compound that is added to sunscreens to absorb UV rays.
  • Bisoctrizole is a broad-spectrum ultraviolet radiation absorber, absorbing UVB as well as UVA rays, which makes it an ideal active ingredient for an ophthalmic sunscreen composition. It also reflects and scatters UV adding to its SPF capability for this specific application.
  • Bisoctrizole is a hybrid UV absorber, the only organic UV filter produced and microfine organic particles ( ⁇ 200 nm), like microfine zinc oxide and titanium dioxide.
  • bisoctrizole dissolves poorly in both.
  • Bisoctrizole is added to the water phase of a sunscreen as a 50% suspension, whereas mineral micropigments are usually added to the oil phase.
  • the bisoctrizole particles are stabilized by the surfactant decyl glucoside. This allows for an ideal ophthalmic preparation that could be used in suspension form.
  • Sunscreens it should impregnate the surface layers of the Conjunctiva & Cornea so that its not washed out by blinking or the natural tears constantly irrigating the ocular surface.
  • Bisoctrizole may penetrate the Conjunctiva and build a concentration in the episcleral connective tissue, and permeate through the Cornea and build an effective concentration in the eye's anterior chamber (aqueous humour) and serve as an effective barrier for UVA & UVB light that enters the eye, potentially preventing cataract formation and/or macular degeneration.
  • Tinosorb® has shown no estrogenic effects in vitro. Although there is very little systemic absorption of such agents when used on the ocular surface, it is a positive finding that this agent is safe in this regard. Tinosorb® one of the first UV filters that have been made available in micronized "nano" form, and used in this format, it will minimize significant irritation to the eye or affecting the users' vision. Further, Tinosorb® used in Particulate form (smaller than 100 nanometers) causes significantly less/no blurring for the user. From a preparation standpoint, Nanoparticle easily dispersible in oil or glycol systems, making it an ideal preparation for an ophthalmic emulsion.
  • compositions that are manufactured as ophthalmic solutions, emollients, creams, or ointments that can be instilled directly on the eyes. It is understood that the use of the term "ophthalmic solution” shall include emollients, creams and ointments that can be instilled directly on the eyes.
  • An embodiment of the present invention includes an ophthalmic solution comprised of diluted forms of Tinosorb® an inorganic active ingredient by itself, or mixed with a weak concentration of another organic active ingredient.
  • An example embodiment of the present invention includes an ophthalmic sunscreen composition, which is comprised of Tinosorb® in an artificial tear vehicle.
  • Another example embodiment of the present invention includes an ophthalmic sunscreen composition, which is comprised of Tinosorb® with an organic sunscreen (e.g., Avobenzone) in an artificial tear vehicle.
  • an organic sunscreen e.g., Avobenzone
  • Another example embodiment of the present invention includes an ophthalmic sunscreen composition, which is comprised of Tinosorb® with an inorganic sunscreen (e.g., Zinc Oxide) in an artificial tear vehicle.
  • an ophthalmic sunscreen composition which is comprised of Tinosorb® with an inorganic sunscreen (e.g., Zinc Oxide) in an artificial tear vehicle.
  • Another example embodiment of the present invention includes an ophthalmic sunscreen composition, which is comprised of Tinosorb® with an organic, as well as an inorganic sunscreen an artificial tear
  • sunscreen composition comprising an emulsifier selected from the group consisting of Arlacel P 135, DC 901 1 silicone elastomer, Abil WE 09, Abil EM-90, Emulgade 68/50, Simulgel A, Simulgel EG, and mixtures thereof.
  • an emulsifier selected from the group consisting of Arlacel P 135, DC 901 1 silicone elastomer, Abil WE 09, Abil EM-90, Emulgade 68/50, Simulgel A, Simulgel EG, and mixtures thereof.
  • Another example of this invention includes embodiments comprised of an emollient.
  • Said emollient may be selected from the group consisting of Aloe extracts, ethers, oleaginous esters, and mixtures thereof.
  • Another example of this invention includes embodiments comprised of an emollient selected from the group consisting of actiphyte of aloe vera, Cetiol OE, Lexol IPL, octyl palmitate, neopentyl glycol heptanoate, neopentyl glycol
  • Trivent NP-13 is alkyl benzoate, and mixtures thereof.
  • compositions of the present invention are now described, but are not limited to these embodiments.
  • Ophthalmic sunscreen compositions according to the present invention may contain a liquid vehicle base, such as an artificial tear formulation, which may be water and/or oil-based, or an ophthalmic suspension or ointment and include at least one form of Tinosorb® (e.g., Tinosorb® M) by itself, or mixed with an organic- and/or an inorganic molecule with UV protecting features.
  • a liquid vehicle base such as an artificial tear formulation, which may be water and/or oil-based, or an ophthalmic suspension or ointment and include at least one form of Tinosorb® (e.g., Tinosorb® M) by itself, or mixed with an organic- and/or an inorganic molecule with UV protecting features.
  • Tinosorb® can be used in nano form, and refers to a number of UV absorbers: Bemotrizinol (Tinosorb® S), Bisoctrizole (Tinosorb® M), Tris-Biphenyl Triazine (Tinosorb® A2B), Octyl methoxycinnamate (Tinosorb® OMC).
  • Inorganic active ingredients may include, but not be limited to zinc oxide, titanium dioxide, iron oxide, zirconium oxide, and cerium oxide, optionally in micronized form as to prevent blurred vision when applied.
  • Organic active ingredients may include, but not be limited to dioxybenzone, octinoxate, octisalate, homosalate, avobenzone, octocrylene, para- aminobenzoic acid, cinoxate, methyl anthranilate, octocrylene, padimate O, ensulizole, sulisobenzone, trolamine salicylate, and ecamsule.
  • the inactive ingredients of the present invention shall also include emulsifier(s) and/or emollient(s). Silicone-based emulsifiers like polyethylene glycols, polysiloxanes, glycosides are excellent choices.
  • Emollients may include, but not be limited to aloe extracts, oleaginous esters, and ethers, or a combination thereof.
  • composition of the present invention shall also include, but not be limited to preservatives, chelating agents, and/or antioxidants.
  • Example 1 An ophthalmic sunscreen solution can be synthesized by mixing 5% micronized Tinosorb® M in an ophthalmic artificial tear formulation. This solution may contain carboxymethylcellulose sodium 0.1 %; glycerin 0.25%; boric acid; calcium chloride dihydrate; erythritol; levocarnitine; magnesium chloride hexahydrate; potassium chloride; purified water; sodium borate decahydrate; and sodium citrate dihydrate.
  • Example 2 An ophthalmic sunscreen solution can be synthesized by mixing a range of 5% Tinosorb® with micronized titanium dioxide and 3% octisalate in an ophthalmic artificial tear solution. This solution may contain
  • Example 3 An ophthalmic sunscreen ointment can be synthesized by mixing 5% micronized Tinosorb® M in an ophthalmic ointment consisting of hypromellose , boric acid, sodium perborate, phosphonic acid, potassium chloride, purified water, and sodium chloride.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Birds (AREA)
  • Chemical & Material Sciences (AREA)
  • Inorganic Chemistry (AREA)
  • Emergency Medicine (AREA)
  • Dermatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Cosmetics (AREA)

Abstract

La présente invention concerne une composition d'écran solaire ophtalmique non irritante, non masquante et photostable qui contient au moins l'un des composants suivants : bémotrizinol; bisoctrizole; tris-biphényltriazine; et/ou méthoxycinnamate d'octyle. Une base de véhicule liquide est alors le reste de la solution en poids. La composition est une formulation de larmes artificielles ou une suspension ou une pommade ophtalmique. La composition peut comprendre au moins une substance active inorganique et/ou au moins une substance active organique. Les substances actives inorganiques peuvent comprendre, mais ne sont pas limitées à, l'oxyde de zinc, le dioxyde de titane, l'oxyde de fer, l'oxyde de zirconium et l'oxyde de cérium. Les substances actives organiques peuvent comprendre, mais ne sont pas limitées à, la dioxybenzone, l'ocinoxate, l'octisalate, l'homosalate, l'avobenzone, l'octocrylène, l'acide para-aminobenzoïque, le cinoxate, l'anthranilate de méthyle, l'octocrylène, le padimate O, l'ensulizole, la sulisobenzone, le salicylate de trolamine et l'écamsule.
PCT/US2017/041784 2016-07-12 2017-07-12 Composition d'écran solaire ophtalmique non irritante, non masquante et photostable WO2018013732A1 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
EP17828416.2A EP3484586A4 (fr) 2016-07-12 2017-07-12 Composition d'écran solaire ophtalmique non irritante, non masquante et photostable
CN201780056098.4A CN109803725A (zh) 2016-07-12 2017-07-12 无刺激性、不致模糊、光稳定的眼用防晒组合物

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201662361189P 2016-07-12 2016-07-12
US62/361,189 2016-07-12
US15/648,107 US10695290B2 (en) 2014-05-19 2017-07-12 Non-irritating, non-blurring, photostable ophthalmic sunscreen composition
US15/648,107 2017-07-12

Publications (1)

Publication Number Publication Date
WO2018013732A1 true WO2018013732A1 (fr) 2018-01-18

Family

ID=60952195

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2017/041784 WO2018013732A1 (fr) 2016-07-12 2017-07-12 Composition d'écran solaire ophtalmique non irritante, non masquante et photostable

Country Status (1)

Country Link
WO (1) WO2018013732A1 (fr)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3437626A1 (fr) * 2017-08-01 2019-02-06 Beiersdorf AG Agent de protection solaire à faible potentiel d'irritation oculaire
US11369812B2 (en) 2014-05-19 2022-06-28 A. Ebbie Soroudi, M.D., M.S., A Professional Medical Corporation Non-irritating, non-blurring ophthalmic sunscreen
US11690800B2 (en) 2014-05-19 2023-07-04 A. Ebbie Soroudi, M.D., M.S., A Professional Medical Corporation Non-irritating, non-blurring, photostable ophthalmic sunscreen composition

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4603046A (en) * 1985-08-23 1986-07-29 Charles Of The Ritz Group Ltd. Improved sunscreen or sunblock composition
US4765977A (en) * 1986-11-28 1988-08-23 Baron Neville A Ophthalmic liquid sunglasses
US20130028853A1 (en) * 2010-02-09 2013-01-31 Kathryn Nurse High spf sunscreen compositions
US20150272848A1 (en) * 2014-03-27 2015-10-01 Louise Holyfield Topical skin care formulations
US20150328098A1 (en) * 2014-05-19 2015-11-19 A. Ebbie Soroudi Non-irritating, non-blurring ophthalmic sunscreen
US20150328148A1 (en) * 2012-06-06 2015-11-19 Brian J. Smith Ophthalmic Solution for Absorbing Ultraviolet Radiation and Method for Absorbing Ultraviolet Radiation
US20160008237A1 (en) * 2013-02-28 2016-01-14 Tagra Biotechnologies Ltd. Microcapsules comprising sunscreen agents

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4603046A (en) * 1985-08-23 1986-07-29 Charles Of The Ritz Group Ltd. Improved sunscreen or sunblock composition
US4765977A (en) * 1986-11-28 1988-08-23 Baron Neville A Ophthalmic liquid sunglasses
US20130028853A1 (en) * 2010-02-09 2013-01-31 Kathryn Nurse High spf sunscreen compositions
US20150328148A1 (en) * 2012-06-06 2015-11-19 Brian J. Smith Ophthalmic Solution for Absorbing Ultraviolet Radiation and Method for Absorbing Ultraviolet Radiation
US20160008237A1 (en) * 2013-02-28 2016-01-14 Tagra Biotechnologies Ltd. Microcapsules comprising sunscreen agents
US20150272848A1 (en) * 2014-03-27 2015-10-01 Louise Holyfield Topical skin care formulations
US20150328098A1 (en) * 2014-05-19 2015-11-19 A. Ebbie Soroudi Non-irritating, non-blurring ophthalmic sunscreen

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See also references of EP3484586A4 *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11369812B2 (en) 2014-05-19 2022-06-28 A. Ebbie Soroudi, M.D., M.S., A Professional Medical Corporation Non-irritating, non-blurring ophthalmic sunscreen
US11690800B2 (en) 2014-05-19 2023-07-04 A. Ebbie Soroudi, M.D., M.S., A Professional Medical Corporation Non-irritating, non-blurring, photostable ophthalmic sunscreen composition
EP3437626A1 (fr) * 2017-08-01 2019-02-06 Beiersdorf AG Agent de protection solaire à faible potentiel d'irritation oculaire

Similar Documents

Publication Publication Date Title
US11369812B2 (en) Non-irritating, non-blurring ophthalmic sunscreen
US11690800B2 (en) Non-irritating, non-blurring, photostable ophthalmic sunscreen composition
Wang et al. Photoprotection: a review of the current and future technologies
ES2786264T3 (es) Composición de protección solar
JP2013056903A (ja) 非刺激組成物
JP2010539234A (ja) 眼部刺痛が少なく高いｓｐｆを有する日焼け止め組成物
US20070218021A1 (en) Non-irritating sunscreen composition
WO2018013732A1 (fr) Composition d'écran solaire ophtalmique non irritante, non masquante et photostable
EP3484586A1 (fr) Composition d'écran solaire ophtalmique non irritante, non masquante et photostable
CN109908004B (zh) 一种多重乳液防晒化妆品及其制备方法
EP1642560A1 (fr) Compositions antisolaires et de soin contenant des enzymes réparatrices d'ADN
AU2015258135B2 (en) Cosmetic product
US9486397B2 (en) Dermocosmetic compositions based on a synergistic combination of colloidal silver and deoxyribonucleic acid
CN105726351B (zh) 降低紫外线引起的脂质过氧化的协同组合物、制剂及相关方法
CN115279458A (zh) 组合物和敏感性说明
ES2850366T3 (es) Composición para el tratamiento de blefaritis que contiene terpinen-4-ol
ES2262527T3 (es) Composicion de dos componentes para uso cosmetico o farmaceutico.
EP1608331B1 (fr) Composition d'ecran solaire renfermant un melange de silices
Tomar et al. Clinical Applications of Sunscreens and Formulation Advancements
WO2023198800A1 (fr) Nouvelles compositions associant au moins un filtre solaire inorganique et leur utilisation
ES2631191B1 (es) Composición para la protección solar y reparación de la piel mediante complejos protectores
KR20220032203A (ko) 마이크로 입자 또는 나노 입자를 이용한 모발의 자외선 차단용 조성물
KR101723249B1 (ko) 자외선 방지제
CN117064781A (zh) 一种安全温和的防晒组合物及其应用

Legal Events

Date Code Title Description
121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 17828416

Country of ref document: EP

Kind code of ref document: A1

NENP Non-entry into the national phase

Ref country code: DE

ENP Entry into the national phase

Ref document number: 2017828416

Country of ref document: EP

Effective date: 20190212