Classifications

• • 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
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K33/00—Medicinal preparations containing inorganic active ingredients
  • A61K33/24—Heavy metals; Compounds thereof
  • A61K33/30—Zinc; Compounds thereof
• • 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
  • A61K31/74—Synthetic polymeric materials
  • A61K31/785—Polymers containing nitrogen
  • A61K31/787—Polymers containing nitrogen containing heterocyclic rings having nitrogen as a ring hetero atom
  • A61K31/79—Polymers of vinyl pyrrolidone
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
  • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
  • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
• • 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
  • 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
  • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
  • A61P31/04—Antibacterial agents
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
  • A61K47/02—Inorganic compounds

Definitions

• the present invention relates to ophthalmic compositions.
• An object of the present invention is to provide an ophthalmic composition that is preservative-free and has excellent preservative efficacy.
• the ophthalmic composition according to the present embodiment contains zinc chloride (also simply referred to as "(A) component”) and a polyvinyl-based polymer compound (also simply referred to as "(B) component”).
• polyvinylpyrrolidone is preferable, polyvinylpyrrolidone K25, polyvinylpyrrolidone K30 and polyvinylpyrrolidone K90 are more preferable, and polyvinylpyrrolidone K30 and polyvinylpyrrolidone K90 are more preferable, from the viewpoint of further enhancing the effects of the present invention.
• the content of the buffering agent in the ophthalmic composition according to the present embodiment is not particularly limited, and is appropriately set according to the type of buffering agent, the type and content of other compounding ingredients, the application and formulation form of the ophthalmic composition, and the like. be. From the viewpoint of exhibiting the effects of the present invention more remarkably, the total content of the buffer is 0.0001 w/v% or more, 0.001 w/v% or more, or 0.005 w/v% or more based on the total amount of the ophthalmic composition.
• nonionic surfactants are preferred, and POE sorbitan fatty acid esters, POE hydrogenated castor oil, POE castor oil, polyethylene glycol monostearate, and POE/POP block copolymers are more preferred.
• the content of the surfactant in the ophthalmic composition according to the present embodiment is not particularly limited, and is appropriately determined according to the type of surfactant, the type and content of other compounding ingredients, the application and formulation form of the ophthalmic composition, and the like. set.
• the total content of surfactants is 0.001 w/v% or more, 0.005 w/v% or more, or 0.01 w/v% or more, based on the total amount of the ophthalmic composition, from the viewpoint of exhibiting the effects of the present invention more remarkably.
• the content ratio of the chelating agent to the component (A) in the ophthalmic composition according to the present embodiment is not particularly limited. is set as appropriate. From the viewpoint of further enhancing the effects of the present invention, the content ratio of the chelating agent to the component (A) is, for example, 1 part by mass of the total content of the component (A) contained in the ophthalmic composition according to the present embodiment.
• the total content of the chelating agent may be 0 parts by mass or more, 2000 parts by mass or less, 100 parts by mass or less, or 20 parts by mass or less, 0 to 2000 parts by mass, 0 to 100 parts by mass parts, or 0 to 20 parts by mass.
• the ophthalmic composition according to the present embodiment can be adjusted to have an osmotic pressure ratio within a range acceptable to living organisms, if necessary.
• An appropriate osmotic pressure ratio can be appropriately set according to the application, formulation form, method of use, etc. of the ophthalmic composition. .0 or less, 3.0 or less, 2.2 or less, or 2.0 or less, 0.4 to 5.0, 0.6 to 3.0, 0.8 to 2.2, or It may be from 0.8 to 2.0.
• the ophthalmic composition according to the present embodiment contains, in addition to the above components, an appropriate amount of a combination of components selected from various pharmacologically active components and physiologically active components within a range that does not impair the effects of the present invention. good too.
• the ingredients are not particularly limited, and examples thereof include active ingredients in ophthalmic drugs described in the 2017 edition of the Standards for Manufacturing and Marketing Approval of Over-the-Counter Drugs (supervised by the Japanese Society of Regulatory Science). Specific examples of components used in ophthalmic drugs include the following components.
• Antiallergic agents for example, cromoglycate sodium, tranilast, pemirolast potassium, acitazanolast, amlexanox, ibudilast and the like.
• Antihistamines e.g.
• Amino acids for example, L-arginine, glutamic acid, glycine, alanine, lysine, ⁇ -aminobutyric acid, ⁇ -aminovaleric acid, trimethylglycine, taurine, aspartic acid and salts thereof.
• Astringents For example, zinc white, zinc lactate, zinc sulfate and the like.
• Others For example, sulfamethoxazole, sulfisoxazole, sulfisomidine and salts thereof and the like.
• menthol menthone, camphor, borneol, geraniol, cineol, citronellol, carvone, anethole, eugenol, limonene, linalool, linalyl acetate, thymol, cymene, terpineol, pinene, camphene, isoborneol, fenchen , nerol, myrcene, myrcenol, linalool acetate, lavandulol, eucalyptus oil, bergamot oil, peppermint oil, cool mint oil, spearmint oil, peppermint oil, fennel oil, cinnamon oil, rose oil, camphor oil, etc.
• Thickeners eg starch; chitin and its derivatives; chitosan and its derivatives; carrageenan; monosaccharides such as glucose and the like.
• Stabilizers For example, sodium formaldehyde sulfoxylate (Rongalite), aluminum monostearate, glyceryl monostearate, cyclodextrin, monoethanolamine, dibutylhydroxytoluene, sodium bisulfite, sodium pyrosulfite and the like.
• Preservatives e.g. quaternary ammonium salts of alkylpolyaminoethylglycines (e.g.
• the ophthalmic composition according to this embodiment can take various formulation forms depending on the purpose.
• Formulations include, for example, liquids, gels, semi-solids (ointments, etc.) and the like.
• the ophthalmic composition according to the present embodiment is preferably an eye drop (including an eye drop that can be instilled while wearing contact lenses) because the effect of the present invention can be exhibited more remarkably.
• the ophthalmic composition according to the present embodiment is an eye drop
• the usage and dosage are not particularly limited as long as they are effective and have few side effects.
• a method of using 1 to 3 drops, 1 to 2 drops, or 2 to 3 drops at a time, 2 to 4 times, or 5 to 6 times a day can be exemplified.
• the ophthalmic composition according to the present embodiment has the effect of suppressing dryness of contact lenses, the effect of reducing friction, the effect of increasing viscosity, and the survival rate of corneal epithelial cells against drying. can be suitably used for suppressing dryness of the eyes or dry eye.
• the container containing the ophthalmic composition according to the present embodiment may be of a multi-dose type that accommodates multiple doses, or may be of a unit dose type that accommodates a single dose. , the multi-dose type is preferable from the viewpoint of exhibiting the effect of the present invention.
• Escherichia coli which is a Gram-negative bacterium
• an ophthalmic composition containing both zinc chloride and polyvinylpyrrolidone is preserved, compared with an ophthalmic composition containing either zinc chloride or polyvinylpyrrolidone. It was confirmed that the efficacy was significantly improved. In addition, it is known that when sodium chondroitin sulfate is contained, the preservative efficacy is lowered. By comparison, it was confirmed that the ophthalmic composition containing zinc chloride and polyvinylpyrrolidone had significantly improved preservative efficacy.
• the ophthalmic composition containing both zinc chloride and polyvinylpyrrolidone had an increased viscosity compared to the ophthalmic composition containing either zinc chloride or polyvinylpyrrolidone.
• a similar tendency was also confirmed with ophthalmic compositions further containing sodium chondroitin sulfate, sodium hyaluronate, or hydroxypropylmethylcellulose. By increasing the viscosity of the ophthalmic composition, retention in the eye can be improved.

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• Health & Medical Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Life Sciences & Earth Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Epidemiology (AREA)
• Ophthalmology & Optometry (AREA)
• Chemical Kinetics & Catalysis (AREA)
• General Chemical & Material Sciences (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Organic Chemistry (AREA)
• Engineering & Computer Science (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Inorganic Chemistry (AREA)
• Communicable Diseases (AREA)
• Oncology (AREA)
• Medicinal Preparation (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

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Citations (16)

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• 2022
  • 2022-09-30 EP EP22876531.9A patent/EP4393510A4/en active Pending
  • 2022-09-30 US US18/695,745 patent/US20240390416A1/en active Pending
  • 2022-09-30 TW TW111137266A patent/TW202320815A/zh unknown
  • 2022-09-30 JP JP2023551894A patent/JPWO2023054669A1/ja active Pending
  • 2022-09-30 WO PCT/JP2022/036673 patent/WO2023054669A1/ja not_active Ceased

Patent Citations (16)

Non-Patent Citations (2)

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