Classifications

• • 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
  • A61K9/08—Solutions
• • 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
  • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
  • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
  • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• • 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
  • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
  • A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
  • A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
• • 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
  • A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
• • 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
  • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
• • 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
  • A61K47/44—Oils, 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
• • G—PHYSICS
  • G02—OPTICS
  • G02C—SPECTACLES; SUNGLASSES OR GOGGLES INSOFAR AS THEY HAVE THE SAME FEATURES AS SPECTACLES; CONTACT LENSES
  • G02C13/00—Assembling; Repairing; Cleaning

Definitions

• the present invention relates to an ophthalmic composition.
• the present invention also relates to an ophthalmic composition for silicone hydrogel contact lenses.
• solubilizers are blended in many formulations, and one of them is a surfactant. It is known that a preparation containing a surfactant is easy to foam, and foam is generated by applying vibration or impact during production or distribution.
• Silicone hydrogel contact lenses have recently been developed as soft contact lenses having high oxygen permeability under such a background. Silicone hydrogel contact lenses achieve oxygen permeability several times that of conventional hydrogel contact lenses by blending silicone with hydrogel. Therefore, it is highly expected that the oxygen supply shortage, which is a weak point of the soft contact lens, can be improved and the adverse effects on the cornea due to the oxygen shortage can be greatly suppressed.
• the silicone hydrogel contact lens is significantly more easily adsorbed with lipid stains derived from the tear film and cosmetics compared to conventional hydrogel contact lenses (Patent Document 1).
• Such lipid contamination of the contact lens induces cloudiness of the lens, causing discomfort to the wearer and harming QOL (Quality of Life). Further, such lipid contamination of the contact lens may adversely affect the vision correction power that the lens should originally have. Furthermore, such lipid contamination of contact lenses may induce corneal epithelial disorders such as corneal staining.
• the lens can be prevented from being clouded to improve the feeling of wearing, maintain the original vision correction power of the lens, and further prevent corneal epithelial damage.
• Patent Document 1 discloses an ophthalmic composition for a silicone hydrogel contact lens containing polyhexanide, chlorpheniramine and the like.
• An object of the present invention is an ophthalmic composition, in particular, an ophthalmic composition that is easily foamed in which a solubilizing agent such as a surfactant is blended. Even if foam is generated by vibration or impact, the ophthalmic composition has a high defoaming rate. Is to provide things.
• Another object of the present invention is to provide an ophthalmic composition for a silicone hydrogel contact lens capable of effectively washing lipid adsorbed on the silicone hydrogel contact lens.
• the inventors of the present invention have made extensive studies to solve the above problems, and surprisingly, (A) arginine or a salt thereof and (B) a nonionic surfactant are simultaneously blended in the ophthalmic composition. As a result, it was found that the defoaming speed is remarkably improved even if bubbles are generated by vibration or impact. Furthermore, the present inventors have found that the ophthalmic composition for a silicone hydrogel contact lens containing (A) arginine or a salt thereof can effectively wash the lipid adsorbed on the silicone hydrogel contact lens. .
• the present invention is based on these findings and provides the following inventions.
• An ophthalmic composition comprising (A) one or more selected from the group consisting of arginine and a salt thereof, and (B) a nonionic surfactant.
• the component (B) is selected from the group consisting of polyoxyethylene sorbitan fatty acid esters, polyoxyethylene hydrogenated castor oil, polyoxyethylene castor oil, polyethylene glycol monostearate, and polyoxyethylene polyoxypropylene glycol.
• the ophthalmic composition according to [1-1] which is at least one selected.
• [1-7] The ophthalmic composition according to any one of [1-1] to [1-6], further comprising (D) a polysaccharide.
• [2-3] The ophthalmic composition for silicone hydrogel contact lenses according to [2-1] or [2-2], further comprising (B) a nonionic surfactant.
• the ophthalmic composition of the present invention contains (A) arginine or a salt thereof and (B) a nonionic surfactant, the defoaming rate in the ophthalmic composition can be improved. As a result, it is possible to perform dissolution confirmation or foreign substance inspection during the production of the ophthalmic composition in a short time, and the production efficiency can be improved.
• the ophthalmic composition of the present embodiment comprises (A) one or more selected from the group consisting of arginine and a salt thereof, and (B) a nonionic surfactant. And (A) one or more selected from the group consisting of arginine and salts thereof (hereinafter referred to as “ophthalmic composition”). (2) ").
• the unit of content “%” means “w / v%” and is synonymous with “g / 100 mL”.
• the abbreviation “POE” means polyoxyethylene
• the abbreviation “POP” means polyoxypropylene.
• the ophthalmic composition (1) includes (A) one or more selected from the group consisting of arginine and a salt thereof (also simply referred to as “component (A)”) and (B) a nonionic interface. Contains an activator (also simply referred to as “component (B)”).
• Arginine may be a free form or a pharmaceutically, pharmacologically (pharmaceutically) or physiologically acceptable salt.
• arginine salt examples include inorganic acid salts such as hydrochloride.
• Arginine and its salt may be any of D-form, L-form and DL-form, but L-form is preferred.
• Arginine and its inorganic acid salt are preferable as arginine and its salt, arginine and arginine hydrochloride are more preferable, and arginine is still more preferable.
• arginine or a salt thereof can also be used.
• Arginine or its salt may be used individually by 1 type, or may be used in combination of 2 or more type.
• the content of the component (A) in the ophthalmic composition (1) according to the present embodiment is not particularly limited, and the type of the component (A), the types and contents of other compounding components, and the use of the ophthalmic composition (1) And it sets suitably according to a formulation form etc.
• the content of the component (A) is, for example, from the viewpoint of more prominently achieving the effects of the present invention, for example, based on the total amount of the ophthalmic composition (1), the total content of the component (A) is 0.001 to It is preferably 10 w / v%, more preferably 0.01 to 10 w / v%, still more preferably 0.05 to 5 w / v%, and 0.1 to 3 w / v%. Is more preferable, and 0.1 to 2 w / v% is particularly preferable.
• nonionic surfactant examples include, for example, monolauric acid POE (20) sorbitan (polysorbate 20), monopalmitic acid POE (20) sorbitan (polysorbate 40), and monostearic acid POE (20) sorbitan (polysorbate 60).
• POE sorbitan fatty acid esters such as tristearic acid POE (20) sorbitan (polysorbate 65), monooleic acid POE (20) sorbitan (polysorbate 80); POE (5) hydrogenated castor oil (polyoxyethylene hydrogenated castor oil 5) POE (10) hydrogenated castor oil (polyoxyethylene hydrogenated castor oil 10), POE (20) hydrogenated castor oil (polyoxyethylene hydrogenated castor oil 20), POE (30) hydrogenated castor oil (polyoxyethylene hydrogenated castor oil 30) ), POE (4 ) Hydrogenated castor oil (polyoxyethylene hydrogenated castor oil 40), POE (60) hydrogenated castor oil (polyoxyethylene hydrogenated castor oil 60), POE (80) hydrogenated castor oil (polyoxyethylene hydrogenated castor oil 80), POE ( 100) POE hydrogenated castor oil such as hydrogenated castor oil (polyoxyethylene hydrogenated castor oil 100); POE (3) castor oil (polyoxyethylene castor oil 3), POE
• Nonionic surfactants are preferably POE sorbitan fatty acid esters, polyoxyethylene hydrogenated castor oil, polyoxyethylene castor oil, polyethylene glycol monostearate, POE / POP glycol, POE sorbitan fatty acid esters, polyoxyethylene cured Castor oil, polyoxyethylene castor oil, polyethylene glycol monostearate, POE / POP glycol are more preferable, POE sorbitan fatty acid esters, polyoxyethylene hydrogenated castor oil, POE / POP glycol are more preferable, polysorbate 80, polyoxyethylene Hardened castor oil 60, POE (120) POP (40) glycol, POE (196) POP (67) glycol are even more preferred, polysorbate 80, polyoxy Ethylene hydrogenated castor oil 60, POE (196) POP (67) glycol are particularly preferred, polyoxyethylene hydrogenated castor oil 60 Gayori particularly preferred.
• POE / POP glycol When POE / POP glycol is used as a nonionic surfactant, POE (42) POP (67) glycol, POE (120) POP (40) glycol, POE (160) POP (30) glycol, POE (196) POP (67) glycol, POE (200) POP (70) glycol is preferred, POE (42) POP (67) glycol, POE (196) POP (67) glycol is more preferred, and POE (196) POP (67) glycol is preferred. Further preferred. In another embodiment, POE (120) POP (40) glycol and POE (196) POP (67) glycol are preferable, and POE (196) POP (67) glycol is more preferable.
• a commercially available nonionic surfactant can also be used.
• a nonionic surfactant may be used individually by 1 type, or may be used in combination of 2 or more type.
• the content of the component (B) is, for example, from the viewpoint of more prominently achieving the effects of the present invention, for example, based on the total amount of the ophthalmic composition (1), the total content of the component (B) is 0.001 to It is preferably 10 w / v%, more preferably 0.005 to 5 w / v%, still more preferably 0.01 to 1 w / v%, and 0.01 to 0.4 w / v%.
• 0.01 to 0.2 w / v% is still more preferable, 0.01 to 0.1 w / v% is particularly preferable, and 0.01 to 0.1%. Most preferably, it is 05 w / v%.
• the content ratio of the component (B) to the component (A) is not particularly limited, and the types of the components (A) and (B), the types of other compounding components, and It is appropriately set according to the content, the use of the ophthalmic composition (1), the preparation form, and the like.
• the content ratio of the component (B) relative to the component (A) is, for example, from the viewpoint of exhibiting the effects of the present invention more remarkably, for example, the total content of the component (A) included in the ophthalmic composition (1) according to this embodiment.
• the total content of component (B) is preferably 0.001 to 20 parts by mass, more preferably 0.005 to 10 parts by mass, and 0.005 to 5 parts per 1 part by mass. More preferably, it is from 0.01 to 3 parts by weight, even more preferably from 0.01 to 1 part by weight, and from 0.01 to 0.5 part by weight. Is more particularly preferred.
• the ophthalmic composition (1) according to this embodiment may further contain (C) a chelating agent (also simply referred to as “(C) component”).
• a chelating agent also simply referred to as “(C) component.
• chelating agents examples include ethylenediaminediacetic acid (EDDA), ethylenediaminetriacetic acid, ethylenediaminetetraacetic acid (edetic acid (EDTA)), N- (2-hydroxyethyl) ethylenediaminetriacetic acid (HEDTA), and diethylenetriaminepentaacetic acid (DTPA). And etidronic acid.
• EDDA ethylenediaminediacetic acid
• EDTA ethylenediaminetriacetic acid
• HEDTA ethylenediaminetetraacetic acid
• DTPA diethylenetriaminepentaacetic acid
• ethylenediaminetetraacetic acid is preferable from the viewpoint of more prominently achieving the effects of the present invention.
• a commercially available chelating agent can also be used.
• a chelating agent may be used individually by 1 type, or may be used in combination of 2 or more type.
• the content of (C) component in the ophthalmic composition (1) which concerns on this embodiment is not specifically limited, The kind of (C) component, the kind and content of another compounding component, Use of ophthalmic composition (1) And it sets suitably according to a formulation form etc.
• the content of the component (C) is, for example, from the viewpoint of more prominently achieving the effects of the present invention, for example, based on the total amount of the ophthalmic composition (1), the total content of the component (C) is 0.001 to It is preferably 1 w / v%, more preferably 0.005 to 0.5 w / v%, still more preferably 0.01 to 0.2 w / v%.
• the content ratio of the component (C) to the component (A) is not particularly limited, and the types of the components (A) and (C), the types of other compounding components, and It is appropriately set according to the content, the use of the ophthalmic composition (1), the preparation form, and the like.
• the content ratio of the component (C) relative to the component (A) is, for example, from the viewpoint of exhibiting the effects of the present invention more remarkably, for example, the total content of the component (A) included in the ophthalmic composition (1) according to the present embodiment.
• the total content of component (C) is preferably 0.001 to 10 parts by mass, more preferably 0.005 to 5 parts by mass, and 0.005 to 3 parts per 1 part by mass.
• the amount is more preferably part by mass, still more preferably 0.01 to 1 part by mass, and particularly preferably 0.01 to 0.5 part by mass.
• the ophthalmic composition (1) according to the present embodiment may further contain (D) a polysaccharide (also simply referred to as “(D) component”).
• (D) a polysaccharide also simply referred to as “(D) component.
• Polysaccharide includes dextran, mucopolysaccharide, xanthan gum, gellan gum, cellulosic polymer compound and salts thereof.
• the polysaccharide can be appropriately selected from known polysaccharides.
• dextran examples include dextran 40 and dextran 70.
• mucopolysaccharides include hyaluronic acid, chondroitin sulfate, chitosan, heparin, heparan, alginic acid, and derivatives thereof (for example, acetylated compounds).
• hyaluronic acid, chondroitin sulfate and salts thereof are preferable, and hyaluronic acid or salts thereof are more preferable from the viewpoint of more prominently achieving the effects of the present invention.
• the salt of hyaluronic acid and the salt of chondroitin sulfate are not particularly limited as long as they are pharmaceutically, pharmacologically (pharmaceutically) or physiologically acceptable.
• alkali metal salts are preferable, sodium salts, potassium salts and the like are more preferable, and sodium salts are further preferable.
• sodium hyaluronate and sodium chondroitin sulfate are preferable, and sodium hyaluronate is more preferable.
• Mucopolysaccharides may be used singly or in combination of two or more.
• a cellulose polymer compound obtained by replacing the hydroxyl group of cellulose with another functional group can be used.
• the functional group that substitutes the hydroxyl group of cellulose include a methoxy group, an ethoxy group, a hydroxymethoxy group, a hydroxyethoxy group, a hydroxypropoxy group, a carboxymethoxy group, and a carboxyethoxy group.
• a commercially available cellulose-based polymer compound can also be used.
• cellulose-based polymer compound examples include methyl cellulose, ethyl cellulose, hydroxyethyl cellulose, hydroxymethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose (hypromellose), carboxymethyl cellulose, carboxyethyl cellulose, and salts thereof.
• any salt may be used as long as it is pharmaceutically, pharmacologically (pharmaceutically) or physiologically acceptable.
• alkali metal salts are preferable, and sodium salts, potassium salts, and the like are more preferable.
• cellulose polymer compounds methyl cellulose, hydroxyethyl cellulose, hydroxypropyl methyl cellulose (2208, 2906, 2910, etc.), hydroxypropyl cellulose, carboxymethyl cellulose or salts thereof are preferable from the viewpoint of more prominently achieving the effects of the present invention.
• Hydroxypropyl methylcellulose, hydroxyethylcellulose, or sodium carboxymethylcellulose is more preferred, hydroxypropylmethylcellulose, hydroxyethylcellulose is still more preferred, hydroxypropylmethylcellulose is still more preferred, and hydroxypropylmethylcellulose 2906 is particularly preferred.
• Cellulose polymer compounds may be used singly or in combination of two or more.
• polysaccharide mucopolysaccharides, cellulose polymer compounds and salts thereof are preferable, hyaluronic acid, chondroitin sulfate, hydroxypropylmethylcellulose, hydroxyethylcellulose, carboxymethylcellulose and salts thereof are more preferable, and hydroxypropylmethylcellulose is more preferable.
• Hydroxypropylmethylcellulose 2208, hydroxypropylmethylcellulose 2906, and hydroxypropylmethylcellulose 2910 are even more preferred, and hydroxypropylmethylcellulose 2906 is particularly preferred.
• a commercially available polysaccharide can also be used.
• a polysaccharide may be used individually by 1 type or may be used in combination of 2 or more type.
• the content of the component (D) is, for example, from the viewpoint of more prominently achieving the effects of the present invention, for example, based on the total amount of the ophthalmic composition (1), the total content of the component (D) is 0.001 to It is preferably 2 w / v%, more preferably 0.005 to 1 w / v%, still more preferably 0.01 to 0.5 w / v%, and 0.01 to 0.1 w / v Even more preferably, it is v%.
• the content ratio of the component (D) to the component (A) is not particularly limited, and the types of the components (A) and (D), the types of other compounding components, and It is appropriately set according to the content, the use of the ophthalmic composition (1), the preparation form, and the like.
• the content ratio of the component (D) relative to the component (A) is, for example, from the viewpoint of exhibiting the effects of the present invention more remarkably, for example, the total content of the component (A) included in the ophthalmic composition (1) according to this embodiment.
• the total content of component (D) is preferably 0.001 to 20 parts by weight, more preferably 0.005 to 10 parts by weight, and 0.01 to 5 parts by weight per 1 part by weight.
• the amount is more preferably part by mass, and still more preferably 0.01 to 1 part by mass.
• the ophthalmic composition (1) according to the present embodiment may further contain (E) a bactericidal agent or a preservative (also simply referred to as “(E) component”).
• a bactericidal agent or a preservative also simply referred to as “(E) component.
• Bactericides or preservatives are compounds having a bactericidal or bacteriostatic action, and salts thereof.
• the disinfectant or preservative can be appropriately selected from known antiseptics or antibacterial agents.
• bactericides or preservatives include, for example, cationic fungicides (preservatives) (benzalkonium, benzethonium, chlorhexidine, alexidine, polyhexanide), alkylpolyaminoethylglycine, benzoic acid, chlorobutanol, sorbic acid, dehydro Acetic acid, parabens (for example, paraoxybenzoic acid esters such as methyl paraoxybenzoate, ethyl paraoxybenzoate, propyl paraoxybenzoate and butyl paraoxybenzoate), oxyquinoline, phenethyl alcohol, benzyl alcohol, polyquaterniums, glowul (rhodia) Zinc, sulfisoxazole, sulfisomidine and sulfamethoxazole, and salts thereof.
• preservatives benzalkonium, benzethonium, chlorhexidine, alexidine, polyhexanide
• bactericides or antiseptic salts include, for example, alkyldiaminoethylglycine hydrochloride, sodium benzoate, benzalkonium chloride, benzethonium chloride, chlorhexidine gluconate, potassium sorbate, sodium dehydroacetate, oxyquinoline sulfate, hydrochloric acid Polyhexanide, zinc chloride, sulfisomidine sodium and sulfamethoxazole sodium.
• cationic disinfectants preservatives
• polyquaternium chloride benzalkonium chloride
• chlorhexidine gluconate alexidine
• polyhexanide hydrochloride and polydronium chloride are more preferable
• polyhexanide hydrochloride alexidine and chloride
• Polydronium is more preferred
• polyhexanide hydrochloride is even more preferred.
• fungicides or preservatives it is more preferable to use a combination of two or more fungicides or preservatives from the viewpoint of achieving the effects of the present invention more remarkably.
• a combination of cationic fungicide (preservative) and polyquaternium is preferable, a combination of polydronium chloride and cationic fungicide (preservative) is more preferable, a combination of polydronium chloride and polyhexanide hydrochloride, or polydronium chloride and alexidine. Is more preferable.
• a commercially available thing can also be used for a disinfectant or a preservative.
• a bactericidal agent or preservative may be used individually by 1 type, or may be used in combination of 2 or more type.
• the content of the (E) component in the ophthalmic composition (1) according to the present embodiment is not particularly limited, and the type of the (E) component, the type and content of other compounding components, and the use of the ophthalmic composition (1) And it sets suitably according to a formulation form etc.
• the content of the component (E) for example, the total content of the component (E) is 0.00001 to It is preferably 2 w / v%, more preferably 0.00001 to 1 w / v%, still more preferably 0.00005 to 0.5 w / v%, and 0.00005 to 0.1 w / v. Even more preferably, it is v%.
• component (E) is alexidine, polyhexanide hydrochloride or polydronium chloride
• the total content of component (E) is 0.000001 to 0.01 w / v based on the total amount of ophthalmic composition (1).
• % Especially 0.000001-0.005 w / v%, especially 0.000005-0.002 w / v%, especially 0.000005-0.001 w / v%, especially 0.00001-0.0005 w / v%, In particular, 0.00005 to 0.0004 w / v%, particularly 0.00007 to 0.0002 w / v% is preferable.
• the ophthalmic composition (1) according to this embodiment preferably further contains amino acids other than the component (A) from the viewpoint of further enhancing the effects of the present invention.
• amino acids other than the component (A) examples include aspartic acid, glutamic acid, aminoethylsulfonic acid (taurine), alanine, asparagine, glutamine, proline, glycine, lysine, histidine, serine, methionine, threonine, cysteine, aminoacetic acid. , Valine, tryptophan, phenylalanine, leucine, isoleucine and salts thereof.
• aspartic acid, glutamic acid, aminoethylsulfonic acid, glycine and salts thereof are preferable from the viewpoint of more prominently achieving the effects of the present invention.
• the amino acids other than the component (A) may be any of D-form, L-form and DL-form, but L-form is preferred.
• Amino acids other than the component (A) may be commercially available. As the amino acids other than the component (A), one type may be used alone, or two or more types may be used in combination.
• the content of amino acids other than the component (A) in the ophthalmic composition (1) according to this embodiment is not particularly limited, and the types of amino acids other than the component (A), the types and contents of other compounding components, It is appropriately set according to the use and formulation form of the ophthalmic composition (1).
• the content of amino acids other than component (A) is, for example, from the viewpoint of more prominently achieving the effects of the present invention, for example, the total amount of amino acids other than component (A) on the basis of the total amount of ophthalmic composition (1).
• the content is preferably 0.001 to 5 w / v%, more preferably 0.01 w / v% to 2 w / v%, and still more preferably 0.1 to 1 w / v%. .
• the content ratio of amino acids other than the component (A) to the component (A) is not particularly limited, and the types of amino acids other than the component (A) and the component (A) are not limited. It is set as appropriate according to the type and content of other compounding ingredients, the use and formulation form of the ophthalmic composition (1).
• the content ratio of amino acids other than the component (A) to the component (A) is included in the ophthalmic composition (1) according to the present embodiment, for example, from the viewpoint of more prominently achieving the effects of the present invention (A).
• the total content of amino acids other than the component (A) is preferably 0.001 to 5 parts by mass and preferably 0.01 to 2 parts by mass with respect to 1 part by mass of the total component. More preferred is 0.1 to 1 part by mass.
• the ophthalmic composition (1) according to this embodiment preferably further contains a buffering agent from the viewpoint of further enhancing the effects of the present invention.
• the buffer is not particularly limited as long as it is pharmaceutically, pharmacologically (pharmaceutically) or physiologically acceptable. Examples of such a buffer include borate buffer, phosphate buffer, carbonate buffer, citrate buffer, acetate buffer, and Tris buffer. These buffering agents may be used alone or in any combination of two or more.
• boric acid buffer examples include boric acid or salts thereof (alkali metal borate, alkaline earth metal borate, etc.).
• phosphate buffer examples include phosphoric acid or a salt thereof (such as an alkali metal phosphate or an alkaline earth metal phosphate).
• carbonate buffer examples include carbonic acid or a salt thereof (an alkali metal carbonate, an alkaline earth metal carbonate, etc.).
• citrate buffer include citric acid or salts thereof (alkali metal citrate, alkaline earth metal citrate, etc.).
• acetate buffer examples include acetic acid or a salt thereof (alkali metal acetate, alkaline earth metal acetate, etc.).
• borate, phosphate, carbonate, citrate or acetate hydrate may be used as borate buffer, phosphate buffer, carbonate buffer, citrate buffer or acetate buffer.
• boric acid or a salt thereof sodium borate, potassium tetraborate, potassium metaborate, ammonium borate, borax, etc.
• a phosphate buffer, phosphoric acid or a salt thereof Salt sodium hydrogen phosphate, sodium dihydrogen phosphate, potassium dihydrogen phosphate, trisodium phosphate, tripotassium phosphate, calcium monohydrogen phosphate, calcium dihydrogen phosphate, etc.
• a salt thereof sodium bicarbonate, sodium carbonate, ammonium carbonate, potassium carbonate, calcium carbonate, potassium bicarbonate, magnesium carbonate, etc.
• citric acid or a salt thereof sodium citrate, potassium citrate, citric acid, etc.
• boric acid buffering agents for example, a combination of boric acid and borax
• phosphoric acid buffering agents for example, a combination of disodium hydrogen phosphate and sodium dihydrogen phosphate
• An acid buffer is more preferred.
• the content of the buffering agent in the ophthalmic composition (1) according to this embodiment is, for example, the total amount of the ophthalmic composition (1) from the viewpoint of more prominently achieving the effects of the present invention.
• the total content of the buffer is preferably 0.001 to 10 w / v%, more preferably 0.005 to 5 w / v%, and 0.01 to 3 w / v%. More preferably, it is still more preferably 0.1 to 2 w / v%.
• the ophthalmic composition (1) according to this embodiment preferably further contains a terpenoid from the viewpoint of further enhancing the effect of the present invention.
• the terpenoid is not particularly limited as long as it is pharmaceutically, pharmacologically (pharmaceutically) or physiologically acceptable.
• examples of such terpenoids include menthol, menthone, camphor, borneol, geraniol, cineol, citronellol, carvone, anethole, eugenol, limonene, linalool, linalyl acetate, and derivatives thereof. These compounds may be D-form, L-form or DL-form.
• an essential oil containing the above compound may be used as a terpenoid.
• essential oils include eucalyptus oil, bergamot oil, peppermint oil, cool mint oil, spearmint oil, peppermint oil, camphor oil, fennel oil, cinnamon oil, and rose oil. These terpenoids may be used alone or in any combination of two or more.
• terpenoids menthol, camphor and borneol are preferable, and menthol is more preferable.
• Preferred essential oils containing these include cool mint oil, peppermint oil, peppermint oil, camphor oil and the like.
• the content of the terpenoid in the ophthalmic composition (1) according to the present embodiment is, for example, based on the total amount of the ophthalmic composition (1) from the viewpoint of more prominently achieving the effects of the present invention.
• the total terpenoid content is preferably 0.00005 to 1 w / v%, more preferably 0.0001 to 0.5 w / v%, and 0.001 to 0.1 w / v%. More preferably it is.
• the ophthalmic composition (1) according to this embodiment preferably further contains a polyhydric alcohol from the viewpoint of further enhancing the effects of the present invention.
• polyhydric alcohol examples include propylene glycol, glycerin, polyethylene glycol (400, 4000, 6000, etc.) and the like.
• propylene glycol is preferable from the viewpoint of more prominently achieving the effects of the present invention.
• polyhydric alcohol can also be used.
• a polyhydric alcohol may be used individually by 1 type, or may be used in combination of 2 or more type.
• the content of the polyhydric alcohol in the ophthalmic composition (1) according to the present embodiment is not particularly limited, the type of polyhydric alcohol, the type and content of other compounding components, the use and formulation of the ophthalmic composition (1). It is set appropriately according to the form and the like.
• the content of the polyhydric alcohol is, for example, from the viewpoint of more prominently achieving the effects of the present invention, for example, based on the total amount of the ophthalmic composition (1), the total content of the polyhydric alcohol is 0.01 to 5 w / It is preferably v%, more preferably 0.05 to 2 w / v%, still more preferably 0.1 to 1 w / v%.
• the pH of the ophthalmic composition (1) according to this embodiment is not particularly limited as long as it is within a range that is pharmaceutically, pharmacologically (pharmaceutically), or physiologically acceptable.
• the pH of the ophthalmic composition (1) according to this embodiment may be, for example, 4.0 to 9.5, preferably 4.0 to 9.0, and 4.5 to 9.0. Is more preferably 4.5 to 8.5, even more preferably 5.0 to 8.5, and particularly preferably 5.5 to 8.5.
• the ophthalmic composition (1) according to the present embodiment can be adjusted to an osmotic pressure ratio within a range acceptable for a living body, as necessary.
• the appropriate osmotic pressure ratio varies depending on the application site, dosage form, and the like, but can be, for example, 0.4 to 5.0, preferably 0.6 to 3.0, and 0.7 to 2.0. More preferably.
• the osmotic pressure can be adjusted by a method known in the art using inorganic salts, polyhydric alcohols, and the like.
• the osmotic pressure ratio is the ratio of the osmotic pressure of the sample to 286 mOsm (0.9 w / v% sodium chloride aqueous solution) based on the 16th revised Japanese Pharmacopoeia.
• the standard solution for osmotic pressure ratio measurement (0.9 w / v% sodium chloride aqueous solution) was prepared by drying sodium chloride (Japanese Pharmacopoeia standard reagent) at 500 to 650 ° C. for 40 to 50 minutes, and then in a desiccator (silica gel). The solution is allowed to cool and 0.900 g is accurately weighed and dissolved in purified water to prepare exactly 100 mL, or a commercially available standard solution for osmotic pressure ratio measurement (0.9 w / v% sodium chloride aqueous solution) can be used.
• the viscosity of the ophthalmic composition (1) according to the present embodiment is not particularly limited as long as it is within a pharmaceutically, pharmacologically (pharmaceutical) or physiologically acceptable range.
• a rotational viscometer (RE550 viscometer, manufactured by Toyo Sangyo Co., Ltd., rotor: 1 ° 34 ′ ⁇ R24) is 0.01 to 10000 mPa ⁇ s is preferable, 0.05 to 8000 mPa ⁇ s is more preferable, 0.1 to 1000 mPa ⁇ s is further preferable, and 1 to 100 mPa ⁇ s is still more preferable. 1 to 10 mPa ⁇ s is particularly preferable, and 1 to 5 mPa ⁇ s is particularly preferable.
• the ophthalmic composition (1) according to the present embodiment contains an appropriate amount of a combination of components selected from various pharmacologically active components and physiologically active components in addition to the above components, as long as the effects of the present invention are not impaired. You may do it.
• the said component is not specifically limited, For example, the active ingredient in the ophthalmic medicine described in the over-the-counter medicine manufacture sale approval standard 2012 version (supervised by General Society of Regulatory Science) can be illustrated.
• Specific examples of components used in ophthalmic drugs include the following components.
• Antihistamines for example, iproheptin, diphenhydramine hydrochloride, chlorpheniramine maleate, ketotifen fumarate, olopatadine hydrochloride, levocabastine hydrochloride, etc.
• Antiallergic agents for example, sodium cromoglycate, tranilast, pemirolast potassium and the like.
• Steroid agents For example, fluticasone propionate, fluticasone furancarboxylate, mometasone furancarboxylate, beclomethasone propionate, flunisolide and the like.
• Anti-inflammatory agents for example, glycyrrhetinic acid, dipotassium glycyrrhizinate, pranoprofen, methyl salicylate, glycol salicylate, allantoin, tranexamic acid, ⁇ -aminocaproic acid, berberine chloride, sodium azulenesulfonate, lysozyme chloride, zinc sulfate, zinc lactate, Licorice etc.
• Decongestant Tetrahydrozoline hydrochloride, tetrahydrozoline nitrate, naphazoline hydrochloride, naphazoline nitrate, epinephrine, epinephrine hydrochloride, ephedrine hydrochloride, phenylephrine hydrochloride, dl-methylephedrine hydrochloride, etc.
• Eye muscle modulating agent for example, cholinesterase inhibitor having an active center similar to acetylcholine, specifically, neostigmine methyl sulfate, tropicamide, helenien, atropine sulfate, etc.
• Vitamins For example, flavin adenine dinucleotide sodium, cyanocobalamin, pyridoxine hydrochloride, panthenol, calcium pantothenate, sodium pantothenate, retinol palmitate, retinol acetate, tocopherol acetate, etc.
• Inorganic salts For example, metal chlorides such as calcium chloride, magnesium chloride, sodium chloride, potassium chloride and ammonium chloride, and metal sulfates such as calcium sulfate, magnesium sulfate, sodium sulfate, potassium sulfate and ammonium sulfate.
• Astringent For example, zinc white, zinc lactate, zinc sulfate and the like.
• Local anesthetics for example, lidocaine, procaine, etc. Other: rebamipide.
• additives are appropriately selected according to a conventional method according to the use and the formulation form, as long as the effects of the present invention are not impaired. Or you may make it contain in an appropriate amount using together or more.
• additives include various additives described in Pharmaceutical Additives Encyclopedia 2007 (edited by Japan Pharmaceutical Additives Association).
• Typical additives include the following additives.
• Carrier An aqueous solvent such as water or hydrous ethanol.
• Base for example, octyldodecanol, titanium oxide, potassium bromide, plastibase, liquid paraffin, light liquid paraffin, purified lanolin, white petrolatum, etc.
• pH adjuster hydrochloric acid, acetic acid, sodium hydroxide, potassium hydroxide, calcium hydroxide, magnesium hydroxide, trometamol, triethanolamine, monoethanolamine, diisopropanolamine and the like.
• Sugars For example, monosaccharides, disaccharides, specifically glucose, maltose, trehalose, sucrose, cyclodextrin, xylitol, sorbitol, mannitol and the like.
• Stabilizer Dibutylhydroxytoluene, butylhydroxyanisole, sodium formaldehyde sulfoxylate (Longalite), sodium hydrogen sulfite, sodium pyrosulfite, monoethanolamine, aluminum monostearate, glycerin monostearate, cyclodextrin and the like.
• Anionic surfactant polyoxyethylene alkyl ether phosphate, polyoxyethylene alkyl ether sulfate, alkylbenzene sulfonate, alkyl sulfate, N-acyl taurate, etc.
• Amphoteric surfactant lauryldimethylaminoacetic acid betaine and the like.
• Vinyl polymer compounds polyvinylpyrrolidone, polyvinyl alcohol, carboxyvinyl polymer, etc.
• the ophthalmic composition (1) which concerns on this embodiment does not contain pyrrolidone carboxylic acid substantially, and it is more preferable not to contain pyrrolidone carboxylic acid.
• the ophthalmic composition (1) according to the present embodiment is prepared, for example, by adding and mixing the components (A) and (B) and other components as necessary so as to obtain a desired content. can do.
• the components can be dissolved or suspended in purified water, adjusted to a predetermined pH and osmotic pressure, and sterilized by filtration sterilization or the like.
• the ophthalmic composition (1) according to the present embodiment can take various dosage forms depending on the purpose, and examples thereof include a liquid agent, a gel agent, and a semi-solid agent (such as an ointment). Among these, a liquid agent is preferable. Moreover, an aqueous liquid agent is preferable among liquid agents.
• the ophthalmic composition (1) according to the present embodiment is an aqueous liquid, the water content is, for example, 50 w / v% or more and 70 w / v% or more with respect to the total amount of the ophthalmic composition (1).
• water used in the ophthalmic composition (1) is 80 w / v% or more, more preferably 90 w / v% or more, and even more preferably 95 w / v% or more.
• water used in the ophthalmic composition (1) according to the present embodiment water that is pharmaceutically, pharmacologically (pharmaceutical) or physiologically acceptable may be used. , Distilled water, normal water, purified water, sterilized purified water, water for injection, and distilled water for injection.
• the ophthalmic composition (1) according to the present embodiment is used in the ophthalmic field and is not limited in its formulation form as long as it is used so as to come into contact with the eye.
• eye drops (however, eye drops include eye drops that can be instilled while wearing contact lenses), eye ointments, eye wash (however, eye wash includes eye wash that can be washed while wearing contact lenses) ),
• Contact lens mounting solution contact lens care solution (contact lens disinfectant, contact lens storage solution, contact lens cleaning solution, contact lens cleaning storage solution, contact lens disinfection / cleaning / storage solution (multipurpose solution) Etc.).
• eye drops, eye wash, contact lens mounting liquid, and contact lens care liquid are preferable.
• the ophthalmic composition (1) according to this embodiment has an improved defoaming speed and less variation in the amount of dripping during use. Preferably used. From another point of view, the ophthalmic composition (1) according to this embodiment has an improved defoaming speed, and thus the eyewash is used by the user transferring a certain amount of the liquid to another container.
• Contact lens care solutions are also suitable formulations for the ophthalmic composition (1).
• the term “contact lens” includes all contact lenses including hard contact lenses, oxygen-permeable hard contact lenses, soft contact lenses, and silicone hydrogel contact lenses.
• the ophthalmic composition (1) according to the present embodiment is used according to a method of use corresponding to the formulation form.
• the ophthalmic composition is an eye drop (including an eye drop for contact lenses)
• an appropriate amount of the eye drop may be applied to the naked eye or an eye wearing a contact lens.
• the ophthalmic composition is an eye wash (including an eye wash for contact lenses)
• an appropriate amount of the eye wash may be used for washing the eyes with the naked eye or the eye wearing a contact lens.
• the ophthalmic composition is a contact lens mounting liquid, it is used by contacting an appropriate amount of the contact lens and the mounting liquid when the contact lens is mounted.
• the contact lens is immersed in an appropriate amount of the care solution, or the contact lens is contacted with the care solution and washed. used.
• the immersion time is usually 1 minute or longer, preferably 10 minutes or longer, more preferably 1 hour or longer, and still more preferably 4 hours or longer.
• a container which accommodates the ophthalmic composition (1) according to the present embodiment a container usually used as a container which accommodates the ophthalmic composition (1) can be used, and it may be made of glass or made of plastic. It may be.
• the constituent material of the plastic container is not particularly limited.
• polyethylene naphthalate, polyarylate, polyethylene terephthalate, Any one of polypropylene, polyethylene, polyimide, and polycarbonate, a copolymer thereof, or a mixture of two or more thereof can be given.
• the copolymer is mainly composed of any one of ethylene-2,6-naphthalate units, arylate units, ethylene terephthalate units, propylene units, ethylene units, and imide units, and other polyester units and imide units.
• Examples of the copolymer include.
• a container made of polyethylene terephthalate may contain polyethylene terephthalate with respect to the total weight of the constituent material of the container, but is usually 10 w / w% or more, preferably 50 w / w%. That means the above.
• the structure, constituent materials and the like of the peripheral portion of the container inlet such as a nozzle provided in the container for storing the ophthalmic composition (1) according to the present embodiment are not particularly limited.
• the structure of the container spout peripheral part such as a nozzle it may be a structure generally adopted as a spout (for example, a nozzle) of a container for an ophthalmic composition (for example, an eye drop container), and is integrated with the container body. It may be molded or may be molded separately from the container body.
• the constituent material of the peripheral part of the spout or the spout for example, nozzle
• the same material as that of the plastic container is exemplified.
• a spout containing polyethylene as a constituent material is suitable.
• polyethylene examples include high-density polyethylene and low-density polyethylene, among which a spout containing low-density polyethylene as a constituent material is suitable. Moreover, as a spout, the nozzle used for an eye drop container is suitable.
• a combination of a polyethylene terephthalate container and a peripheral portion of the polyethylene container mouth more preferably an ophthalmic container made of polyethylene terephthalate And a polyethylene nozzle, particularly preferably a combination of a polyethylene terephthalate eye drop container and a low density polyethylene nozzle.
• the combination of the container which accommodates the ophthalmic composition which concerns on this embodiment, and a container spout peripheral part the combination of the container made from a polyethylene terephthalate and a polypropylene nozzle, and the combination of the container made from a polypropylene and a polypropylene nozzle are also preferable.
• a combination of the container for storing the ophthalmic composition according to the present embodiment and the peripheral portion of the container mouth a combination of a polyethylene container and a polyethylene nozzle, or an integrally molded container thereof, among them, a low density polyethylene container, A combination of low density polyethylene nozzles or an integrally molded container thereof is also preferred.
• the filling amount of the ophthalmic composition (1) according to this embodiment into the container is usually 0.01 to 1000 mL, preferably 0.1 to 500 mL, preferably 1 mL, from the viewpoint of more prominently achieving the effects of the present invention.
• -500 mL are more preferable, 2 mL-100 mL are further preferable, 2 mL-50 mL are still more preferable, 3 mL-25 mL are especially preferable, and 5 mL-20 mL are more especially preferable.
• 10 to 1000 mL is preferable, 50 to 700 mL is more preferable, 70 to 600 mL is still more preferable, and 100 to 500 mL is even more preferable.
• the ophthalmic composition (1) according to the present embodiment it is possible to improve the defoaming speed in the ophthalmic composition, thereby suppressing variation in the dropping amount when the ophthalmic composition such as eye drops is dropped. Can be expected.
• Ophthalmic Composition (2) (Ophthalmic Composition for Silicone Hydrogel Contact Lens)
• the ophthalmic composition (2) according to this embodiment contains (A) one or more selected from the group consisting of arginine and a salt thereof (also simply referred to as “component (A)”).
• the types and preferred examples of the component (A) used in the ophthalmic composition (2) according to this embodiment and the content of the component (A) are the same as those in the case of the ophthalmic composition (1).
• the ophthalmic composition (2) according to the present embodiment may further contain (B) a nonionic surfactant.
• (B) component used by the ophthalmic composition (2) which concerns on this embodiment content of (B) component, and the content ratio of (B) component with respect to (A) component, the above The same as in the case of the ophthalmic composition (1).
• the ophthalmic composition (2) according to this embodiment may further contain (E) a bactericide or a preservative.
• (E) a bactericide or a preservative about the kind and suitable example of (E) component used by the ophthalmic composition (2) which concerns on this embodiment, content of (E) component, and the content ratio of (E) component with respect to (A) component, the above The same as in the case of the ophthalmic composition (1).
• the ophthalmic composition (2) according to the present embodiment may further contain (C) a chelating agent.
• (C) component used by the ophthalmic composition (2) which concerns on this embodiment content of (C) component, and the content ratio of (C) component with respect to (A) component, the above The same as in the case of the ophthalmic composition (1).
• the ophthalmic composition (2) according to this embodiment may further contain (D) a polysaccharide.
• (D) component used by the ophthalmic composition (2) which concerns on this embodiment content of (D) component, and the content ratio of (D) component with respect to (A) component, it is the above The same as in the case of the ophthalmic composition (1).
• the ophthalmic composition (2) according to this embodiment may further contain amino acids other than the component (A).
• amino acids other than the component (A) used in the ophthalmic composition (2) according to this embodiment and the content of amino acids other than the component (A), the ophthalmic composition (1 ).
• the ophthalmic composition (2) according to this embodiment may further contain a buffer.
• a buffer about the kind of buffering agent used by the ophthalmic composition (2) which concerns on this embodiment, a suitable example, and the content of a buffering agent, it is the same as that of the case of the said ophthalmic composition (1).
• the ophthalmic composition (2) according to the present embodiment may further contain a terpenoid.
• the types and preferred examples of terpenoids used in the ophthalmic composition (2) according to this embodiment, and the terpenoid content are the same as those in the ophthalmic composition (1).
• the ophthalmic composition (2) according to this embodiment may further contain a polyhydric alcohol.
• a polyhydric alcohol used by the ophthalmic composition (2) which concern on this embodiment, and content of a polyhydric alcohol, it is the same as that of the case of the said ophthalmic composition (1).
• the ophthalmic composition (2) according to this embodiment contains an appropriate amount of a combination of components selected from various pharmacologically active components and physiologically active components in addition to the above components, as long as the effects of the present invention are not impaired. You may do it.
• various additives are appropriately selected according to a conventional method according to the use and the formulation form, as long as the effects of the present invention are not impaired.
• One or more types may be used in combination to contain an appropriate amount. These types are the same as in the case of the ophthalmic composition (1).
• the pH, osmotic pressure and viscosity of the ophthalmic composition (2) according to this embodiment are the same as those of the ophthalmic composition (1).
• the ophthalmic composition (2) according to the present embodiment can be prepared, for example, by adding and mixing the component (A) and, if necessary, other components to a desired content.
• the production method and dosage form of the ophthalmic composition (2) according to this embodiment are the same as those of the ophthalmic composition (1).
• the ophthalmic composition (2) according to the present embodiment is not limited as long as it is used in the ophthalmic field and used to come into contact with the silicone hydrogel contact lens.
• eye drops for silicone hydrogel contact lenses eye drops that can be used while wearing silicone hydrogel contact lenses
• eye drops for silicone hydrogel contact lenses eye drops that can be used while wearing silicone hydrogel contact lenses
• Silicone hydrogel contact lens mounting solution Silicone hydrogel contact lens care solution (Silicone hydrogel contact lens disinfectant solution, Silicone hydrogel contact lens storage solution, Silicone hydrogel contact lens cleaning solution, Silicone hydrogel contact lens cleaning storage solution , Silicone hydrogel contact lens cleaning / disinfecting / preserving solution (multipurpose solution), etc.).
• silicone hydrogel contact lens care solution Silicone hydrogel contact lens disinfectant solution, Silicone hydrogel contact lens storage solution, Silicone hydrogel contact lens cleaning solution, Silicone hydrogel contact lens cleaning storage solution , Silicone hydrogel contact lens cleaning / disinfecting / preserving solution (multipurpose solution), etc.
• silicone hydrogel contact lens care siliconeone hydro
• the method for using the ophthalmic composition (2) according to this embodiment is not particularly limited as long as it is a known method having a step of bringing the ophthalmic composition (2) into contact with a silicone hydrogel contact lens. .
• a silicone hydrogel contact lens an appropriate amount of the eye drop may be instilled before or during wearing of the silicone hydrogel contact lens.
• an appropriate amount of the eye wash may be used for eye washing before or during wearing of the silicone hydrogel contact lens.
• eye drops for silicone hydrogel contact lenses or eye washes for silicone hydrogel contact lenses should be used for the purpose of eye drops and eye wash not only when wearing silicone hydrogel contact lenses, but also when not wearing them.
• the silicone hydrogel contact lens is used by bringing an appropriate amount of the mounting liquid into contact with the silicone hydrogel contact lens. Further, in the case of a silicone hydrogel contact lens care solution, the silicone hydrogel contact lens is immersed in an appropriate amount of the care solution, or the silicone hydrogel contact lens is brought into contact with the care solution and washed. Used by doing etc. When the contact lens is immersed, the immersion time is usually 1 minute or longer, preferably 10 minutes or longer, more preferably 1 hour or longer, and still more preferably 4 hours or longer.
• the type of silicone hydrogel contact lens to be applied is not particularly limited, and is currently commercially available regardless of whether it is ionic or nonionic, or All silicone hydrogel contact lenses marketed in the future can be applied.
• the lipid adsorbed on the silicone hydrogel contact lens can be effectively washed.
• “ion” means that the content of ionic components in the contact lens material is 1 mol% or more in accordance with US FDA (US Food and Drug Administration) standards, and “non-ion” means the US According to FDA (Food and Drug Administration) standards, the ionic component content in the contact lens material is less than 1 mol%.
• the water content of the silicone hydrogel contact lens to which the ophthalmic composition (2) according to the present embodiment is applied is not particularly limited, and may be, for example, 90% or less, and 60% or less. Preferably, it is 50% or less. Since the silicone hydrogel contact lens contains a hydrogel material, it contains at least more than 0% water.
• the water content of the silicone hydrogel contact lens indicates the ratio of water in the silicone hydrogel contact lens, and is specifically obtained by the following calculation formula.
• Moisture content (%) (weight of hydrated water / weight of hydrated silicone hydrogel contact lens) ⁇ 100 Such moisture content can be measured by a gravimetric method according to the description of ISO 18369-4: 2006.
• the container for housing the ophthalmic composition (2) according to this embodiment is the same as the case of the ophthalmic composition (1).
• the ophthalmic composition (1) according to the present embodiment has an effect that the defoaming speed in the ophthalmic composition can be improved.
• the composition comprises (A) one or more selected from the group consisting of arginine and a salt thereof, and (B) a nonionic surfactant in an ophthalmic composition.
• a method is provided for improving the defoaming rate in the ophthalmic composition.
• an ophthalmic composition containing a nonionic surfactant includes (A) one or more selected from the group consisting of arginine and a salt thereof, An antifoaming rate improver is provided.
• the type and content of component (A), the type and content of component (B), the type and content of other components, etc. [1. As described in the ophthalmic composition (1)].
• the ophthalmic composition (2) according to the present embodiment has an effect that the lipid adsorbed on the silicone hydrogel contact lens can be washed. Thereby, a corneal epithelial disorder can be prevented effectively. Thereby, the wearing feeling of the silicone hydrogel contact lens can be improved.
• the silicone hydrogel contact lens comprising (A) one or more selected from the group consisting of arginine and a salt thereof in an ophthalmic composition for a silicone hydrogel contact lens.
• a method is provided for providing an ophthalmic composition with an action of washing lipid adsorbed on a silicone hydrogel contact lens.
• a silicone hydrogel contact lens comprising an ophthalmic composition for a silicone hydrogel contact lens, containing at least one selected from the group consisting of arginine and a salt thereof.
• Lipid cleaning agents are provided.
• an ophthalmic composition for a silicone hydrogel contact lens containing at least one selected from the group consisting of arginine and a salt thereof is brought into contact with the silicone hydrogel contact lens.
• a method of washing the lipid adsorbed on the silicone hydrogel contact lens comprising the step of: The contacting step may be performed while the silicone hydrogel contact lens is worn, or may be performed while the silicone hydrogel contact lens is not worn.
• the ophthalmic composition (2) according to the present embodiment has an effect of sterilizing Acanthamoeba (for example, Acanthamoeba castellanii, Acanthamoeba polyphaga, etc.) that causes Acanthamoeba corneal infection.
• Acanthamoeba for example, Acanthamoeba castellanii, Acanthamoeba polyphaga, etc.
• the silicone hydrogel contact lens comprising (A) one or more selected from the group consisting of arginine and a salt thereof in an ophthalmic composition for a silicone hydrogel contact lens.
• a method for imparting an action of sterilizing Acanthamoeba to an ophthalmic composition is provided.
• an Acanthamoeba fungicide comprising an ophthalmic composition for a silicone hydrogel contact lens, comprising (A) one or more selected from the group consisting of arginine and a salt thereof. Is done.
• one or more selected from the group consisting of (A) arginine and a salt thereof for the production of an ophthalmic composition for a silicone hydrogel contact lens for sterilization of Acanthamoeba Use is provided.
• an ophthalmic composition for a silicone hydrogel contact lens containing at least one selected from the group consisting of arginine and a salt thereof is brought into contact with the silicone hydrogel contact lens.
• a method of sterilizing an acanthamoeba comprising the step of: The contacting step may be performed while the silicone hydrogel contact lens is worn, or may be performed while the silicone hydrogel contact lens is not worn.
• Test (1) for defoaming speed Each test solution (ophthalmic composition) was prepared by a conventional method according to the formulation described in Table 1. The unit of each component amount in Table 1 is w / v%. Using these test solutions, a test on the defoaming speed was performed. Each test solution was filled into a glass centrifuge tube having a capacity of 50 mL by 30 mL, and immediately after the bubbles were generated by shaking 1500 times using RECIPAD SHAKER SR-2w (TAITEC), The aqueous solution part was confirmed and the volume of the foam part was measured. The defoaming speed was evaluated by the time required (minutes) until the generated bubbles were halved.
• the corresponding test examples are Comparative Example 1-1 for Example 1-1 and Comparative Example 1-2 for Example 1-2. The results are shown in Table 1.
• Test (2) regarding defoaming speed Each test liquid (ophthalmic composition) was prepared by a conventional method according to the formulation described in Table 2. The unit of each component amount in Table 2 is w / v%. Using these test solutions, a test on the defoaming speed was performed in the same manner as in Test Example 1. The corresponding test example is Comparative Example 2-1. The results are shown in Table 2.
• Example 2-2 As shown in Table 2, in the test solutions of Examples 2-1 and 2-2 containing arginine, it was confirmed that the time until the bubbles were reduced by half was shortened and the defoaming rate was improved. Further, it was confirmed that the defoaming speed was further improved in the test solution of Example 2-2 further containing sodium edetate.
• Test Example 3 Test for Defoaming Speed (3)
• Each test solution (ophthalmic composition) was prepared by a conventional method according to the formulation described in Table 3.
• the unit of each component amount in Table 3 is w / v%.
• a test on the defoaming speed was performed in the same manner as in Test Example 1.
• the corresponding test example is Example 3-1.
• the results are shown in Table 3.
• Example 3 As shown in Table 3, in the test solutions of Examples 3-1 and 3-2 containing arginine, it was confirmed that the time until the bubbles were reduced by half was shortened and the defoaming rate was improved. In addition, in the test solution of Example 3-2 further containing hydroxypropylmethylcellulose, it was confirmed that the time until the bubbles were reduced by half was further improved by 93.9%, and the defoaming rate was more significantly improved.
• each test solution (ophthalmic composition) was prepared according to the formulation described in Table 4.
• the unit of each component amount in Table 4 is w / v%.
• Each prepared test solution (2 mL) was put into a glass vial.
• a silicone hydrogel contact lens shaken in the lipid suspension was put in the test solution, and the mixture was shaken at room temperature for 12 hours for washing treatment.
• the silicone hydrogel contact lens was taken out, rinsed with about 100 mL of physiological saline, placed in an Eppendorf tube (capacity 2 mL), and dried. Lipids are extracted by immersing a silicone hydrogel contact lens in a mixed solution of ethanol and diethyl ether (3: 1 (v / v), 1 mL) for at least 10 minutes, and the extracted solution (0.5 mL) is placed in a centrifuge tube. And the solvent was removed.
• the obtained solution was put into a 96-well multiplate in an amount of 200 ⁇ L, the absorbance at 540 nm was measured, and the amount of lipid remaining in the silicone hydrogel contact lens was calculated.
• the calibration curve was prepared using olive oil.
• Test Example 5 Evaluation of bactericidal activity against Acanthamoeba (1)
• Each test solution (ophthalmic composition) was prepared according to the formulation described in Table 5.
• the unit of each component amount in Table 5 is w / v%.
• the bactericidal power of Acanthamoeba against trophotype was evaluated for each test solution immediately after preparation and each test solution after storage at 60 ° C. for 3 weeks.
• Acanthamoeba castellanii was cultured in PYG liquid medium at 32.5 ° C. for 3 days, and 1 / 4RS (sodium chloride: 0.215 g / 100 mL, potassium chloride: 0.0075 g / 100 mL, CaCl 2 .2H 2 O: 0.0083 g / 100 mL) was washed three times, and adjusted to about 2 ⁇ 10 6 to 5 ⁇ 10 6 cells / mL to obtain a microbial solution. Aseptically take the test solution (10 mL) in each of the three sterilized test containers, inoculate it with the microbial solution (0.1 mL), and finally about 2.0 ⁇ 10 4 to 5.0 ⁇ 10 4. cells / mL.
• the obtained microbial solution-containing test solution was allowed to stand at 25 ° C. for 4 hours, and then 0.5 mL was taken out from the microbial solution-containing test solution.
• the obtained culture solution was cultured at 25 ° C. for 7 days, and the presence or absence of growth of the test microorganism was confirmed under an inverted microscope. The number of wells in which growth was observed was counted, and the number of viable trophotypes of Acanthamoeba was calculated by the Spearman-Karber method. Subsequently, the number of contacted bacteria was compared with the number of viable bacteria after 7 days of culture, and the amount of decrease in the number of bacteria was calculated as Log reduction.
• the improvement rate (%) of amoeba bactericidal power relative to Comparative Example 4-1 was calculated using the following formula.
• Amoeba bactericidal power improvement rate (%) ⁇ (Log reduction of each test example—Log reduction of “Comparative example 5-1”) / Log reduction of “Comparative example 5-1” ⁇ 100
• Table 5 shows the calculated amoeba bactericidal power improvement rate.
• test solutions of Examples 5-1 and 5-2 containing L-arginine showed excellent bactericidal activity against Acanthamoeba tropho type and cyst type.
• Test Example 6 Evaluation of bactericidal activity against Acanthamoeba (2)
• Each test solution (ophthalmic composition) was prepared according to the formulation described in Table 6.
• the unit of each component amount in Table 6 is w / v%.
• the improvement rate (%) of amoeba bactericidal power with respect to Reference Example 6-1 was calculated using the following formula.
• Amoeba bactericidal power improvement rate (%) ⁇ (Log reduction in Example 6-1—Log reduction in “Reference Example 6-1”) / Log reduction in “Reference Example 6-1” ⁇ 100
• Example 6-1 blended with L-arginine showed excellent bactericidal activity against Acanthamoeba tropho type and cyst type.
• Test Example 7 Test on defoaming speed (4)
• Each test solution (ophthalmic composition) was prepared by a conventional method according to the formulation described in Table 7.
• the unit of each component amount in Table 7 is w / v%.
• a test on the defoaming speed was performed in the same manner as in Test Example 1.
• the corresponding test examples are Comparative Example 7-1 for Example 7-1 and Comparative Example 7-2 for Example 7-2.
• the results are shown in Table 7.
• Ophthalmic compositions were prepared according to the formulations described in Tables 8 and 9, and formulation examples 1 to 18 were obtained.
• the units in the table are all (w / v%) except those described in the table.

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• 2016
  • 2016-11-16 JP JP2017553761A patent/JP6560764B2/ja active Active
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• 2019
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