Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/12—Ketones
  • A61K31/122—Ketones having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/01—Hydrocarbons
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/0012—Galenical forms characterised by the site of application
  • A61K9/0048—Eye, e.g. artificial tears
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/10—Dispersions; Emulsions
  • A61K9/127—Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P27/00—Drugs for disorders of the senses
  • A61P27/02—Ophthalmic agents
  • A61P27/04—Artificial tears; Irrigation solutions
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P27/00—Drugs for disorders of the senses
  • A61P27/02—Ophthalmic agents
  • A61P27/06—Antiglaucoma agents or miotics
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P27/00—Drugs for disorders of the senses
  • A61P27/02—Ophthalmic agents
  • A61P27/12—Ophthalmic agents for cataracts

Definitions

• the present invention has as subject pharmaceutical compounds useful as eyewash and/or tear substitute comprising carotenoids such as natural lycopene and/or organic lycopene, lutein, zeaxanthine, astaxanthine, plant and synthetic lipids, phospholipids and linear and/or cross-linked hyaluronic acid and/or its salts or other viscosifying agents (for example carboxymethylcellulose, carbomer, and the like).
• carotenoids such as natural lycopene and/or organic lycopene, lutein, zeaxanthine, astaxanthine, plant and synthetic lipids, phospholipids and linear and/or cross-linked hyaluronic acid and/or its salts or other viscosifying agents (for example carboxymethylcellulose, carbomer, and the like).
• carotenoids such as natural lycopene and/or organic lycopene, lutein, zeaxanthine, astaxanthine, plant
• compositions of the invention are also useful both as per se active ingredients (for the treatment of retinal degenerations, like the diabetic retinal degeneration or AMD - Age-related macular degeneration), and as cicatrizants and/or carriers for other active ingredients in ophthalmology (for example antibiotics or cortisones or NSAIDs - Non-steroidal anti-inflammatory drugs).
• the technical problem resolved by the present invention is the creation of a tear substitute and/or eyewash which, in addition to the typical characteristics of the tear substitutes consisting of hydrating, lubricating and moistening capacity/effect, has further characteristics linked to the anti-oxidant activity of the carotenoids and the specific UVA/UVB radiation absorption activity of organic lycopene.
• Dry eye syndrome is an eye disease characterised by the alteration of the natural lachrymal film, with serious discomfort and annoyance by the subject affected with such disorder.
• There are multiple causes of this disease in particular phenomena tied to aging, environmental and atmospheric factors, use of contact lenses, autoimmune pathologies, trigeminal paralysis, oncological diseases, systemic pharmacological therapies, eye surgery operations (for example, various laser therapies or cornea transplants, palpebral operations or operations on the nerve ending level). Dry eye syndrome is currently treated systemically or topically.
• Systemic treatments are known at the state of the art comprising, for example, oral compositions based on unsaturated fatty acids (US7029712) or cysteine (WO02055068).
• tear substitutes are used in the form of eyewash or gel based on detergent, lubricating and possibility disinfecting compounds. Nevertheless, these products only act on the symptomatological level, and sometimes the preservatives contained therein tend to worsen the condition rather than resolve it.
• Treatments are also known at the state of the art which use glucocorticoids, like rimexolone (EPl 575597; US2006069075) and other anti-inflammatory agents (U.S. 6.506.412) for the treatment of possible inflammatory processes underlying the dry eye syndrome.
• Antibiotics are also used, for example tricyclic macrolide compounds (WO0066122) or peptides like duramycin (US2006035811).
• the present invention regards topical compositions comprising the association of carotenoids (organic lycopene) with phospholipids and/or plant or synthetic lipids with a viscoelastic agent, in particular as a tear substitute.
• carotenoids organic lycopene
• phospholipids and/or plant or synthetic lipids with a viscoelastic agent in particular as a tear substitute.
• This combination of substances has shown to be particularly effective in the topical treatment of the dry eye syndrome and of the retinal degenerations, such as for example diabetic retinopathy or AMD (Age-related macular degeneration).
• the compositions of the invention are also useful as carriers or as preservatives for other active ingredients. Said compositions have activities favouring the cicatrising or tissue regeneration processes.
• the composition of the tear substitute containing organic lycopene, subject of the present invention is also capable of protecting the eye from dangerous UVAAJVB radiations.
• carotenoids comprise lycopene, lutein, zeaxanthine, astaxanthine, which can be used on their own or mixed with each other, each in percentages by weight generally in the range of 0.001 - 1%, preferably 0.01 - 0.5%.
• the plant lipids such as for example olive oil and/or almond oil, are present in the compositions of the invention in percentages by weight generally in the range of 0.001 - 5%, preferably 0.001 - 4%. Said lipids can also be of synthetic origin.
• the phospholipids which can be employed according to the invention comprise soy lecithin or egg lecithin, phosphatidylcholine, phosphatidylserine, phosphatidylethanolamine, phosphatidylinositol, polar lipid complexes (for example glycosyl ceramides and digalactosyl glycerides, etc.), various plant seed extracts and/or their mixtures in all proportions.
• the percentages by weight of said phospholipids or phospholipid mixtures or various lipid mixtures in the compositions of the invention vary from 0.001 to 10%.
• compositions of the invention contain linear and/or cross-linked hyaluronic acid and/or its salts at a concentration in the range of 0.001% - 10% by weight, depending on the molecular weight, variable from 200 kDalton to 30 MDalton: a greater molecular weight corresponds with a smaller concentration, and vice versa.
• compositions of the present invention can moreover contain linear and/or cross- linked hyaluronic acid and/or its salts, saturated or unsaturated fatty acids, antioxidant agents (Vitamin A, Vitamin E, Vitamin C, Resveratrol etc.), honey/royal jelly, antibiotics, antiinflammatory agents, cortisones and other active and/or proactive ingredients, Aloe vera extracts.
• the compositions of the present invention can may also contain or not a buffer solution. Said buffer solution, where existing, can be citrate, phosphate, borate or other.
• the present invention also has as subject the use of carotenoids (for example lycopene, lutein, zeaxanthine and/or astaxanthine), free or encapsulated in liposomes/cerasomes, in association with phospholipids and/or plant or synthetic lipids with linear and/or cross-linked hyaluronic acid and/or its salts, for the preparation of medications with cicatrizant/tissue repair activity in ophthalmology.
• carotenoids for example lycopene, lutein, zeaxanthine and/or astaxanthine
• association of the invention can be used as a carrier and preservative for active ingredients of ophthalmic interest, for example beta-blocking (timolol, carteolol, etc.), prostaglandin, glucocorticoids, antibiotics, membrane stabilisers, metals, plant extracts (in particular Aloe vera, Ginkgo biloba).
• active ingredients of ophthalmic interest for example beta-blocking (timolol, carteolol, etc.), prostaglandin, glucocorticoids, antibiotics, membrane stabilisers, metals, plant extracts (in particular Aloe vera, Ginkgo biloba).
• the compositions of the invention can be formulated according to well-known conventional methods, such as those described in "Remington's Pharmaceutical Handbook" Mack Publishing Co., N. Y., USA, using excipients, diluents, viscosifiers, isotonic agents and similar substances acceptable for their final use.
• viscoelastic substances will be advantageously used, such as sodium hyaluronate, polyvinyl alcohol, polyvinylpyrrolidone, hydroxypropylmethylcellulose, polyacrylic acids (Carbopol), and beta-glucan.
• suitable formulations comprise eyewashes, sterile eye drops, gel, foams and ointments.
• Plant lipids (olive oil and/or almond oil) 2 Phosphatidylcholine (50%)-Phosphatidylserine (50%) 5
• Vitamin A 0.1 Vitamin E 0.1
• Plant lipids (olive oil and/or almond oil) 2
• Plant lipids (olive oil and/or almond oil) 2 Vitamin E 0.1 Cross-linked and/or linear hyaluronic acid and/or its salts ⁇ 5
• Hydroxypropylmethylcellulose (Hypromellose-HPMC) ⁇ 5
• Lactated Ringer's Solution (F.U.) 1 WFI bidistilled water q.s. to 100
• Hydroxypropylmethylcellulose (Hypromellose-HPMC) ⁇ 5
• Lactated Ringer's Solution (F.U.) 1 WFI bidistilled water q.s. to 100
• Plant lipids (olive oil and/or almond oil) 4
• Plant lipids (olive oil and/or almond oil) 4
• Plant lipids (olive oil and/or almond oil) 2
• Resveratrol 0.1 Cross-linked and/or linear sodium hyaluronate
• Plant lipids (olive oil and/or almond oil) 2 WFI bidistilled water q.s. to 100

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• Health & Medical Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Veterinary Medicine (AREA)
• Life Sciences & Earth Sciences (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Ophthalmology & Optometry (AREA)
• Epidemiology (AREA)
• Organic Chemistry (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Bioinformatics & Cheminformatics (AREA)
• General Chemical & Material Sciences (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Engineering & Computer Science (AREA)
• Dispersion Chemistry (AREA)
• Medicinal Preparation (AREA)
• Cosmetics (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

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Cited By (13)

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• 2008
  • 2008-01-02 IT IT000003A patent/ITMI20080003A1/it unknown
  • 2008-12-23 WO PCT/IT2008/000793 patent/WO2009084069A2/en not_active Ceased

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