JP7304282B2 - Ophthalmic composition for colored contact lenses - Google Patents

Description

The present invention relates to an ophthalmic composition for colored contact lenses.

In recent years, the number of people wearing colored contact lenses is increasing. Problems such as discoloration of pigments and low oxygen permeability have been pointed out for colored contact lenses. In addition, it is known that the design of colored contact lenses and incorrect use by the wearer are factors that tend to cause corneal epithelial disorders such as corneal erosion, corneal infiltration, and superficial punctate keratopathy (SPK). Patent document 1).

Kiyoshi Watanabe, Atarashii Ophthalmology, Vol. 28, No. 5, pp. 653-654 (2011)

While problems with colored contact lenses have been pointed out as in Non-Patent Document 1, studies on ophthalmic compositions particularly suitable for colored contact lenses are still insufficient.

Further, according to the study of the present inventor, a new problem was found that the color contact lens has higher hardness than the clear contact lens made of the same material.

SUMMARY OF THE INVENTION Accordingly, an object of the present invention is to provide an ophthalmic composition for color contact lenses that can improve the hardness peculiar to color contact lenses.

The present inventors have made intensive studies to solve the above problems, and found that an ophthalmic composition in which geraniol is combined with at least one selected from the group consisting of hydroxypropylmethylcellulose, hyaluronic acid and salts thereof, is unique to color contact lenses. It was found that the hardness of can be improved (reduced). The present invention is based on this finding.

Specifically, the present invention relates to, for example, the following inventions.
[1] An ophthalmic composition for color contact lenses, containing (A) a terpenoid and (B) one or more selected from the group consisting of vinyl-based polymer compounds and saccharides.
[2] The color contact lens according to [1], wherein the component (A) contains geraniol and the component (B) contains at least one selected from the group consisting of hydroxypropylmethylcellulose, hyaluronic acid and salts thereof. Ophthalmic composition.
[3] The component (B) contains hydroxypropylmethylcellulose, and the content of (B) hydroxypropylmethylcellulose is 35 parts by mass or less per 1 part by mass of (A) geraniol. An ophthalmic composition for colored contact lenses as described.
[4] Component (B) contains at least one selected from the group consisting of hyaluronic acid and salts thereof, and the total amount of (B) hyaluronic acid and salts thereof per 1 part by mass of the content of (A) geraniol The ophthalmic composition for color contact lenses according to [2], wherein the content is 3 parts by mass or less.
[5] (A) a terpenoid, and (B) one or more selected from the group consisting of vinyl-based polymer compounds and saccharides, in an ophthalmic composition for a colored contact lens. A method for imparting an effect of reducing the hardness of a colored contact lens to an ophthalmic composition.
[6] (A) a terpenoid, and (B) one or more selected from the group consisting of vinyl-based polymer compounds and saccharides, in an ophthalmic composition for a colored contact lens. A method for providing an ophthalmic composition with the action of reducing the poor wearing feeling of colored contact lenses.

The ophthalmic composition for colored contact lenses of the present invention can remarkably improve (reduce) the hardness peculiar to colored contact lenses. In addition, it is possible to remarkably improve the poor wearing feeling (discomfort when wearing) due to colored contact lenses.

4 is a graph showing the results of evaluating the hardness of various soft contact lenses in Test Example 1. FIG. 4 is a graph showing the results of evaluating the effects of each prescription liquid on the hardness of a color soft contact lens in Test Example 2. FIG.

BEST MODE FOR CARRYING OUT THE INVENTION Hereinafter, embodiments for carrying out the present invention will be described in detail. However, the present invention is not limited to the following embodiments. In this specification, the abbreviation "POE" means polyoxyethylene and the abbreviation "POP" means polyoxypropylene, unless otherwise specified.

[1. Ophthalmic composition for colored contact lenses]
The ophthalmic composition for color contact lenses according to the present embodiment is selected from the group consisting of (A) a terpenoid (also referred to simply as "(A) component") and (B) a vinyl polymer compound and a saccharide. 1 or more types (also simply referred to as "component (B)").

As used herein, a colored contact lens means a contact lens that alters the appearance (color, pattern or shape) of the iris or pupil. Specifically, for example, contact lenses are defined as lenses that change the appearance (color, pattern, or shape) of the iris or pupil as a purpose of use and effect. The color contact lens may or may not be for vision correction. Colored contact lenses may be classified as soft contact lenses (SCL) or hard contact lenses. It is preferably one classified as a contact lens (also referred to as "color SCL"). In addition, the lens material of the color contact lens is not particularly limited, and color contact lenses made of any lens material are included.

(A) Terpenoids include, for example, menthol, menthone, camphor (also referred to as "camphor" or "camphor"), borneol (also referred to as "ryunou" or "carneol"), geraniol, nerol, cineole, citronellol, carvone, and anethole , eugenol, limonene, linalool and linalyl acetate. The terpenoid may be any of d-, l- and dl-forms. However, some terpenoids, such as geraniol, nerol and cineole, do not have optical isomers. (A) A terpenoid may be used individually by 1 type, or may be used in combination of 2 or more type.

The content of component (A) in the ophthalmic composition for colored contact lenses according to this embodiment is appropriately set according to the type of the compound. As for the content of component (A), from the viewpoint of further enhancing the effects of the present invention, for example, the total content of component (A) is usually 0.0001 based on the total amount of the ophthalmic composition for color contact lenses. ~0.5 w/v%, preferably 0.0002 to 0.1 w/v%, more preferably 0.0005 to 0.05 w/v%, and 0.001 to 0.03w /v %, and even more preferably 0.002 to 0.02 w/v %.

The component (A) may be blended in the ophthalmic composition for colored contact lenses according to the present embodiment as an essential oil containing terpenoids. Examples of essential oils containing terpenoids include eucalyptus oil, bergamot oil, peppermint oil, fennel oil, rose oil, cinnamon oil, spearmint oil, camphor oil, cool mint, palmarosa oil, citronella oil, lavender oil, lemongrass oil, Geranium oil and peppermint oil may be mentioned. When a terpenoid-containing essential oil is used as the component (A), it is preferable that the terpenoid contained in the essential oil is blended so as to satisfy the above-described content.

As the component (A), geraniol is preferable because it exhibits the effects of the present invention more remarkably. Geraniol is a known compound also called 3,7-dimethyl-2,6-octadien-1-ol. As geraniol, as long as it is pharmaceutically, pharmacologically (pharmaceutical) or physiologically acceptable, it may be synthesized by a known method or obtained as a commercial product. good.

When geraniol is used as component (A), the content of geraniol is usually 0.00, based on the total amount of the ophthalmic composition for colored contact lenses, since the effects of the present invention are exhibited more remarkably. 0001 to 0.5 w/v%, preferably 0.0002 to 0.1 w/v%, more preferably 0.0005 to 0.05 w/v%, and 0.001 to 0.05 w/v%. 01 w/v % is more preferred, and 0.002 to 0.008 w/v % is even more preferred.

Component (B) is one or more selected from the group consisting of vinyl polymer compounds and saccharides. (B) component may be used individually by 1 type, or may be used in combination of 2 or more types.

As the vinyl polymer compound, compounds applicable to color contact lenses can be used. A commercial thing can also be used for a vinyl-type high molecular compound.

Examples of vinyl polymer compounds include vinyl alcohol polymers such as polyvinyl alcohol (completely or partially saponified), vinylpyrrolidone polymers such as polyvinylpyrrolidone, and carboxyvinyl polymers.

Among the vinyl-based polymer compounds, polyvinylpyrrolidone K17, polyvinylpyrrolidone K25, polyvinylpyrrolidone K30, polyvinylpyrrolidone K90, polyvinyl alcohol (partially saponified product) or carboxyvinyl polymer is preferred from the viewpoint of further enhancing the effects of the present invention. Alcohol (partially saponified) or carboxyvinyl polymer is more preferred, and polyvinyl alcohol (partially saponified) is even more preferred.

The vinyl polymer compound may be used singly or in combination of two or more.

The content of the vinyl polymer compound in the ophthalmic composition for color contact lenses according to this embodiment is appropriately set according to the type and molecular weight of the compound. From the viewpoint of further enhancing the effect of the present invention, the content of the vinyl polymer compound is usually 0 based on the total amount of the ophthalmic composition for color contact lenses. .001 to 25 w/v%, preferably 0.001 to 10 w/v%, more preferably 0.005 to 5 w/v%, and 0.01 to 5 w/v% is more preferred, and 0.1 to 3 w/v% is even more preferred.

As sugars, compounds applicable to color contact lenses can be used. Examples of sugars include polysaccharides (e.g., cellulose-based polymer compounds, glycosaminoglycans, dextran, gellan gum, alginic acid and salts thereof), oligosaccharides (e.g., cyclodextrin), and monosaccharides (e.g., glucose). mentioned. A commercially available saccharide can also be used. Saccharides may be used individually by 1 type, or may be used in combination of 2 or more types.

As the cellulose-based polymer compound, a cellulose-based polymer compound obtained by replacing the hydroxyl group of cellulose with another functional group and applicable to color contact lenses can be used. Functional groups that substitute hydroxyl groups of cellulose include, for example, methoxy, ethoxy, hydroxymethoxy, hydroxyethoxy, hydroxypropoxy, carboxymethoxy and carboxyethoxy groups. Commercially available cellulose-based polymer compounds can also be used.

Examples of cellulosic polymer compounds include methylcellulose, ethylcellulose, hydroxyethylcellulose, hydroxymethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose (hypromellose), carboxymethylcellulose, carboxyethylcellulose and salts thereof. Here, any salt may be used as long as it is pharmaceutically, pharmacologically (pharmaceutical) or physiologically acceptable. Among them, alkali metal salts are preferred, and sodium salts, potassium salts and the like are more preferred.

Among cellulosic polymer compounds, from the viewpoint of further enhancing the effects of the present invention, methylcellulose, hydroxyethylcellulose, hydroxypropylmethylcellulose, hydroxypropylcellulose, carboxymethylcellulose, or salts thereof are preferred, and hydroxypropylmethylcellulose or sodium carboxymethylcellulose is more preferred. preferable. Moreover, among cellulose-based polymer compounds, hydroxypropylmethylcellulose is more preferable because the effects of the present invention are exhibited more remarkably.

A cellulose polymer compound may be used individually by 1 type, or may be used in combination of 2 or more type.

The content of the cellulose-based polymer compound in the ophthalmic composition for colored contact lenses according to the present embodiment is appropriately set according to the type and molecular weight of the compound. As for the content of the cellulose-based polymer compound, from the viewpoint of further enhancing the effects of the present invention, for example, the total content of the cellulose-based polymer compound is usually 0 based on the total amount of the ophthalmic composition for color contact lenses. .0001 to 25 w/v%, preferably 0.001 to 10 w/v%, more preferably 0.001 to 2 w/v%, and 0.002 to 1 w/v% is more preferred, and 0.01 to 0.2 w/v% is even more preferred.

When hydroxypropylmethylcellulose is used as component (B), the content of hydroxypropylmethylcellulose should be based on the total amount of the ophthalmic composition for colored contact lenses, for example, since the effect of the present invention is exhibited more remarkably. , usually 0.0001 to 2 w/v%, preferably 0.0005 to 1 w/v%, more preferably 0.001 to 0.5 w/v%, and 0.002 to 0.5%. 5 w/v % is more preferred, and 0.01 to 0.1 w/v % is even more preferred.

Glycosaminoglycans include, for example, hyaluronic acid and chondroitin sulfate.

Among the glycosaminoglycans, those having no sulfate group such as hyaluronic acid are preferable, and hyaluronic acid or a salt thereof is more preferable, since the effects of the present invention are exhibited more remarkably. The salt of hyaluronic acid is not particularly limited as long as it is pharmaceutically, pharmacologically (pharmaceutical) or physiologically acceptable. As the salt of hyaluronic acid, for example, alkali metal salts are preferable, and sodium salts, potassium salts and the like are more preferable.

Glycosaminoglycans may be used singly or in combination of two or more.

The content of glycosaminoglycan in the ophthalmic composition for colored contact lenses according to this embodiment is appropriately set according to the type and molecular weight of the compound. As for the content of glycosaminoglycans, from the viewpoint of further enhancing the effects of the present invention, for example, the total content of glycosaminoglycans is usually 0.00001 based on the total amount of the ophthalmic composition for color contact lenses. ~5 w/v%, preferably 0.00005 to 3 w/v%, more preferably 0.0001 to 2 w/v%, and further preferably 0.0005 to 1 w/v% Preferably, 0.001 to 0.6 w/v% is even more preferred.

When hyaluronic acid or a salt thereof is used as the component (B), the content of hyaluronic acid or a salt thereof should be such that the effects of the present invention are exhibited more remarkably. Based on the total amount, it is usually 0.00001 to 1 w/v%, preferably 0.00005 to 0.5 w/v%, more preferably 0.0001 to 0.1 w/v%, More preferably 0.0005 to 0.05 w/v%, even more preferably 0.001 to 0.02 w/v%.

Examples of dextran include dextran 40 and dextran 70, with dextran 70 being particularly preferred.

As alginic acid, alginic acid and salts of alginic acid are preferred, and alginic acid and sodium alginate are particularly preferred.

The content of sugars in the ophthalmic composition for colored contact lenses according to the present embodiment is appropriately set according to the type and molecular weight of the compound. As for the content of saccharides, from the viewpoint of further enhancing the effects of the present invention, for example, the total content of saccharides is usually 0.00001 to 25 w/v% based on the total amount of the ophthalmic composition for color contact lenses. It is preferably 0.00005 to 10 w/v%, more preferably 0.0001 to 10 w/v%, even more preferably 0.0005 to 7 w/v%, and 0.001 to Even more preferably 5 w/v %.

Among the component (B), polysaccharides are preferable, among them, it is more preferable to use a combination of a cellulose-based polymer compound and a glycosaminoglycan, and more preferable to use a combination of hydroxypropylmethylcellulose and hyaluronic acid or a salt thereof. .

The content of component (B) in the ophthalmic composition for colored contact lenses according to the present embodiment is, from the viewpoint of further enhancing the effect of the present invention, for example, based on the total amount of the ophthalmic composition for colored contact lenses, The total content of component (B) is usually 0.00001 to 25 w/v%, preferably 0.00005 to 10 w/v%, more preferably 0.0001 to 10 w/v%. , more preferably 0.0005 to 7 w/v%, and even more preferably 0.001 to 5 w/v%.

The content ratio of component (B) to component (A) in the ophthalmic composition for colored contact lenses according to the present embodiment is not particularly limited, and is appropriately set according to the types of components (A) and (B). be. From the viewpoint of further enhancing the effect of the present invention, the content ratio of component (B) to component (A) is, for example, the total content of component (A) contained in the ophthalmic composition for colored contact lenses according to the present embodiment. The total content of component (B) is more preferably 0.1 to 10,000 parts by weight, still more preferably 1 to 1,000 parts by weight, and 1 to 300 parts by weight, based on 1 part by weight. more preferably 2 to 100 parts by mass, particularly preferably 10 to 35 parts by mass.

Further, for example, when geraniol is used as the component (A) and hydroxypropylmethylcellulose is used as the component (B), the effects of the present invention are exhibited more remarkably. , The content of hydroxypropylmethylcellulose is preferably 1 to 200 parts by weight, more preferably 1 to 100 parts by weight, and 5 to 50 parts by weight with respect to 1 part by weight of geraniol. is more preferable, 5 to 35 parts by mass is even more preferable, and 10 to 35 parts by mass is particularly preferable.

Further, for example, when using geraniol as the component (A) and at least one selected from the group consisting of hyaluronic acid and salts thereof as the component (B), the effects of the present invention are exhibited more remarkably. As the content ratio of hyaluronic acid and its salts to, for example, the total content of hyaluronic acid and its salts is more preferably 0.1 to 50 parts by mass with respect to 1 part by mass of geraniol content, It is more preferably 0.1 to 10 parts by mass, even more preferably 0.1 to 3 parts by mass, and particularly preferably 0.2 to 2 parts by mass.

The ophthalmic composition for color contact lenses according to this embodiment preferably further contains a surfactant from the viewpoint of further enhancing the effects of the present invention. In addition, the surfactant is used to dissolve various pharmacologically active ingredients, physiologically active ingredients, additives, etc., which will be described later, according to the purpose of use of the ophthalmic composition for colored contact lenses according to the present embodiment. It is also effective as a dissolution aid to improve the solubility.

The surfactant that can be contained in the ophthalmic composition for colored contact lenses according to the present embodiment is not particularly limited as long as it is pharmaceutically, pharmacologically (pharmaceutical) or physiologically acceptable. Either nonionic surfactants or ionic (amphoteric, negative, positive) surfactants may be used. One type of surfactant may be used alone, or two or more types may be used in combination.

Examples of nonionic surfactants include POE (20) sorbitan monourarate (polysorbate 20), POE (20) sorbitan monopalmitate (polysorbate 40), POE (20) sorbitan monostearate (polysorbate 60), tristearin. POE sorbitan fatty acid esters such as acid POE (20) sorbitan (polysorbate 65), monooleic acid POE (20) sorbitan (polysorbate 80); POE (40) hydrogenated castor oil (polyoxyethylene hydrogenated castor oil 40), POE (60) ) POE hydrogenated castor oil such as hydrogenated castor oil (polyoxyethylene hydrogenated castor oil 60); POE (10) castor oil (polyoxyethylene castor oil 10), POE (35) castor oil (polyoxyethylene castor oil 35), etc. POE castor oil of POE (9) POE alkyl ether such as lauryl ether; POE (20) POP (4) POE-POP alkyl ether such as cetyl ether; POE (196) POP (67) glycol (poloxamer 407, Pluronic F127 ), POE (200) POP (70) glycol, and other polyoxyethylene/polyoxypropylene block copolymers; and polyoxyl 40 stearate and other polyethylene glycol monostearate. The numbers in parentheses indicate the number of added moles.

Examples of amphoteric surfactants include N-[2-[[2-(alkylamino)ethyl]amino]ethyl]glycine and salts thereof (eg, hydrochlorides, etc.). N-[2-[[2-(alkylamino)ethyl]amino]ethyl]glycine is also called alkyldiaminoethylglycine or alkylpolyaminoethylglycine.

Examples of anionic surfactants include alkylbenzenesulfonates, alkylsulfates, polyoxyethylene alkylsulfates, α-sulfofatty acid ester salts, and α-olefinsulfonic acids.

Examples of cationic surfactants include benzalkonium chloride and benzethonium chloride.

As the surfactant, a nonionic surfactant is preferred. The nonionic surfactant is preferably POE sorbitan fatty acid ester, POE hydrogenated castor oil, POE castor oil, polyethylene glycol monostearate or POE/POP block copolymer, polysorbate 80, POE castor oil 10, POE castor oil 35, POE hydrogenated castor oil 40, POE hydrogenated castor oil 60, polyoxyl 40 stearate or poloxamer 407 are more preferred.

When a surfactant is contained, the content of the surfactant in the ophthalmic composition for colored contact lenses according to the present embodiment is, for example, the ophthalmic composition for colored contact lenses, from the viewpoint of further enhancing the effects of the present invention. Based on the total amount of, the total content of component (A) is usually 0.0001 to 8 w/v%, preferably 0.001 to 4 w/v%, and 0.002 to 2 w/v% is more preferably 0.01 to 1 w/v%, and even more preferably 0.05 to 0.5 w/v%.

The ophthalmic composition for color contact lenses according to the present embodiment preferably further contains a buffer from the viewpoint of further enhancing the effects of the present invention. The buffering agent is not particularly limited as long as it is pharmaceutically, pharmacologically (pharmaceutical) or physiologically acceptable. Such buffers include, for example, borate buffers, phosphate buffers, carbonate buffers, citrate buffers, acetate buffers, Tris buffers, aspartic acid, aspartate, edetate. . These buffering agents may be used singly or in any combination of two or more.

Boric acid buffers include boric acid or salts thereof (alkali metal borates, alkaline earth metal borates, etc.). Phosphate buffers include phosphoric acid and salts thereof (alkali metal phosphate, alkaline earth metal phosphate, etc.). Carbonic acid buffers include carbonic acid or salts thereof (alkali metal carbonates, alkaline earth metal carbonates, etc.). Citric acid buffers include citric acid or salts thereof (alkali metal citrate, alkaline earth metal citrate, etc.). Borate or phosphate hydrates may also be used as the borate buffer or phosphate buffer. More specific examples include boric acid or a salt thereof (sodium borate, potassium tetraborate, potassium metaborate, ammonium borate, borax, etc.) as a borate buffer; Salts (disodium hydrogen phosphate, sodium dihydrogen phosphate, potassium dihydrogen phosphate, trisodium phosphate, tripotassium phosphate, calcium monohydrogen phosphate, calcium dihydrogen phosphate, etc.); or salts thereof (sodium hydrogen carbonate, sodium carbonate, ammonium carbonate, potassium carbonate, calcium carbonate, potassium hydrogen carbonate, magnesium carbonate, etc.); acetic acid buffer, sodium dihydrogen citrate, disodium citrate, etc.); acetic acid or a salt thereof (ammonium acetate, potassium acetate, calcium acetate, sodium acetate, etc.) as an acetic acid buffer; aspartic acid or a salt thereof (sodium aspartate, magnesium aspartate, potassium aspartate, etc.). Among these buffers, borate buffers (for example, a combination of boric acid and borax) and phosphate buffers (for example, a combination of disodium hydrogen phosphate and sodium dihydrogen phosphate) are preferred. Acid buffers are more preferred.

When a buffering agent is contained, the content of the buffering agent in the ophthalmic composition for colored contact lenses according to the present embodiment is, for example, the total amount of the ophthalmic composition for colored contact lenses, from the viewpoint of further enhancing the effects of the present invention. The total content of the buffering agent is usually 0.05 to 10 w/v%, preferably 0.1 to 5 w/v%, and preferably 0.3 to 3 w/v%. It is more preferably 0.5 to 2 w/v%, even more preferably 0.6 to 1.5 w/v%.

The pH of the ophthalmic composition for colored contact lenses according to this embodiment is not particularly limited as long as it is within a pharmaceutically, pharmacologically (pharmaceutical) or physiologically acceptable range. The pH of the ophthalmic composition for colored contact lenses is, for example, preferably 4.0 to 9.5, more preferably 5.0 to 9.0, and 5.5 to 8.5. is more preferred, and 5.5 to 8.0 is particularly preferred.

Moreover, the osmotic pressure of the ophthalmic composition for colored contact lenses according to the present embodiment is not particularly limited as long as it is within a range that is tolerated by living organisms. The osmotic pressure ratio of the ophthalmic composition for color contact lenses is, for example, preferably 0.5 to 5, more preferably 0.6 to 3.0, and 0.7 to 2.0. is more preferred, and 1.0 to 1.8 is even more preferred. Adjustment of osmotic pressure can be performed by methods known in the art using inorganic salts, polyhydric alcohols, sugar alcohols, sugars, or the like. The osmotic pressure ratio is the ratio of the osmotic pressure of the sample to 286 mOsm (osmotic pressure of 0.9 w/v% sodium chloride aqueous solution) based on the 16th revision of the Japanese Pharmacopoeia, and the osmotic pressure is the osmotic pressure measurement method described in the Japanese Pharmacopoeia. (freezing point depression method). In addition, for the standard solution for osmotic pressure ratio measurement (0.9 w/v% sodium chloride aqueous solution), after drying sodium chloride (Japanese Pharmacopoeia standard reagent) at 500 to 650 ° C. for 40 to 50 minutes, in a desiccator (silica gel) Allow to cool, accurately weigh 0.900 g, dissolve in purified water to prepare exactly 100 mL, or use a commercially available standard solution for osmotic pressure ratio measurement (0.9 w / v% sodium chloride aqueous solution). .

The ophthalmic composition for colored contact lenses according to the present embodiment may contain, in addition to the above components, various pharmacologically or physiologically active components in combination in appropriate amounts as long as the effects of the present invention are not impaired. Examples of pharmacologically active ingredients or physiologically active ingredients include active ingredients in various drugs described in the 2012 version of the Standards for Approval of Manufacturing and Marketing of OTC Drugs (supervised by the Japanese Society of Regulatory Science). Specifically, the components used in ophthalmic drugs include the following components.
Anti-allergic agents: for example, cromoglycate sodium, tranilast, pemirolast potassium and the like.
Steroid agents: for example, fluticasone propionate, fluticasone furoate, mometasone furoate, beclomethasone propionate, flunisolide and the like.
Decongestants: tetrahydrozoline hydrochloride, tetrahydrozoline nitrate, naphazoline hydrochloride, naphazoline nitrate, epinephrine, epinephrine hydrochloride, ephedrine hydrochloride, phenylephrine hydrochloride, dl-methylephedrine hydrochloride and the like.
Ocular muscle modulating agents: For example, cholinesterase inhibitors having an active center similar to that of acetylcholine, specifically neostigmine methyl sulfate, tropicamide, helenien, atropine sulfate, and the like.
Bactericides: For example, acrinol, cetylpyridinium, benzalkonium chloride, benzethonium chloride, chlorhexidine, polyhexamethylenebiguanide, alkyldiaminoethylglycine hydrochloride, and the like.
Vitamins: For example, flavin adenine dinucleotide sodium, cyanocobalamin, pyridoxine hydrochloride, panthenol, calcium pantothenate and the like.
Amino acids: for example, potassium aspartate, magnesium aspartate, magnesium-potassium aspartate, aminoethylsulfonic acid and the like.
Astringents: For example, zinc white, zinc lactate, zinc sulfate and the like.

In addition, in the ophthalmic composition for colored contact lenses according to the present embodiment, various additives are appropriately selected in accordance with conventional methods according to the application or formulation form, as long as they do not impair the effects of the present invention. , one or more may be used in combination and contained in an appropriate amount. Examples of such additives include various additives described in the Encyclopedia of Pharmaceutical Excipients 2007 (edited by the Japan Pharmaceutical Excipients Association). Typical ingredients include the following additives.
Carrier: For example, an aqueous carrier such as water or hydrous ethanol.
Sugar alcohols: For example, xylitol, sorbitol, mannitol and the like. These may be D-, L- or DL-forms.
Preservatives, bactericides or antibacterial agents: for example zinc chloride, alkyldiaminoethylglycine hydrochloride, sodium benzoate, ethanol, benzalkonium chloride, benzethonium chloride, chlorhexidine gluconate, chlorobutanol, sorbic acid, potassium sorbate, dehydroacetic acid sodium, methyl parahydroxybenzoate, ethyl parahydroxybenzoate, propyl parahydroxybenzoate, butyl parahydroxybenzoate, oxyquinoline sulfate, phenethyl alcohol, benzyl alcohol, biguanide compounds (specifically, polyhexamethylene biguanide, polyhexanide hydrochloride, etc.), Glowkill (manufactured by Rhodia, product name), etc.
Chelating agents: for example, ethylenediaminediacetic acid (EDDA), ethylenediaminetriacetic acid, ethylenediaminetetraacetic acid (edetic acid, EDTA), N-(2-hydroxyethyl)ethylenediaminetriacetic acid (HEDTA), diethylenetriaminepentaacetic acid (DTPA) and the like.
Stabilizers: For example, dibutylhydroxytoluene, trometamol, sodium formaldehyde sulfoxylate (Rongalite), tocopherol, sodium pyrosulfite, monoethanolamine, aluminum monostearate, glyceryl monostearate and the like.
Base: For example, octyldodecanol, titanium oxide, potassium bromide, liquid paraffin, plastibase, lanolin, propylene glycol and the like.
Others: Lipidure-PMB (2-methacryloyloxyethylphosphorylcholine/butyl methacrylate copolymer), Lipidure-HM and the like.

The ophthalmic composition for colored contact lenses according to the present embodiment can be prepared, for example, by adding and mixing the components (A), (B), and, if necessary, other components so as to achieve desired contents. can be prepared. Specifically, for example, it can be prepared by dissolving or suspending the above components in purified water, adjusting to a predetermined pH and osmotic pressure, and sterilizing by filtration sterilization or the like.

The ophthalmic composition for colored contact lenses according to the present embodiment has a water content of, for example, 50 w/v% or more, and 70 w/v% or more, relative to the total amount of the ophthalmic composition for colored contact lenses. is preferably 80 w/v% or more, more preferably 90 w/v% or more, and even more preferably 95 w/v% or more. The water used in the ophthalmic composition for colored contact lenses according to the present embodiment may be pharmaceutically, pharmacologically (pharmaceutical) or physiologically acceptable water. Examples include distilled water, ordinary water, purified water, sterile purified water, water for injection, and distilled water for injection.

The ophthalmic composition for color contact lenses according to this embodiment is provided in an arbitrary container. The container for containing the ophthalmic composition for color contact lenses according to this embodiment is not particularly limited, and may be made of glass or plastic, for example. It is preferably made of plastic. Examples of plastics include polyethylene terephthalate, polyarylate, polyethylene naphthalate, polycarbonate, polyethylene, polypropylene, polyimide, copolymers of these monomers, and mixtures of two or more thereof. Preferred is polyethylene terephthalate. Moreover, the container containing the ophthalmic composition for color contact lenses according to the present embodiment may be a transparent container in which the inside of the container can be visually recognized, or an opaque container in which the inside of the container is difficult to visually recognize. A transparent container is preferred. Here, the "transparent container" includes both a colorless transparent container and a colored transparent container. The ophthalmic composition for color contact lenses according to the present embodiment can be used, for example, in a multi-dose form that can be used repeatedly in a colorless and transparent plastic container.

A nozzle may be attached to the container. The material of the nozzle is not particularly limited, and may be, for example, glass or plastic. It is preferably made of plastic. Examples of plastics include polybutylene terephthalate, high-density polyethylene, low-density polyethylene, polypropylene, copolymers of these monomers, and mixtures of two or more thereof. Low density polyethylene and polybutylene terephthalate are preferred. In particular, polybutylene is more preferable from the viewpoint of suppressing the reduction of the effect due to the adsorption of the component (A) in the ophthalmic composition for colored contact lenses according to the present embodiment to the nozzle and further enhancing the effect of the present invention. It is terephthalate.

The ophthalmic composition for colored contact lenses according to the present embodiment can take various dosage forms depending on the intended purpose, and examples thereof include liquid formulations and semi-solid formulations (eg, ointments).

The ophthalmic composition for colored contact lenses according to the present embodiment is not limited in its formulation form as long as it is used in the field of ophthalmology and is used so as to come into contact with colored contact lenses. For example, eye drops for colored contact lenses (eye drops that can be used while wearing colored contact lenses), eye washes for colored contact lenses (eye wash that can be used while wearing colored contact lenses), colored contact lens wetting solutions, Liquid agents for color contact lens care (color contact lens antiseptic solution, color contact lens storage solution, color contact lens cleaning solution, color contact lens cleaning solution, etc.) and the like can be mentioned. Above all, when used as an eye drop for colored contact lenses, it is easy to use, so when the feeling of wearing is poor, it is possible to take it promptly within the range permitted by the usage method. In view of this effect, it can be suitably used as an eye drop for color contact lenses. In addition, when used as a color contact lens wetting solution, it is possible to improve the poor wearing feeling peculiar to wearing. In view of this effect, it can also be suitably used as a color contact lens wetting solution.

The method of using the ophthalmic composition for colored contact lenses according to the present embodiment is not particularly limited as long as it is a known method having a step of bringing the ophthalmic composition for colored contact lenses into contact with the colored contact lenses. . For example, in the case of eye drops for colored contact lenses, an appropriate amount of the eye drops may be applied before or during wearing of the colored contact lenses. Also, in the case of an eye wash for colored contact lenses, an appropriate amount of the eye wash may be used for washing the eyes before or during wearing of the colored contact lenses. The eye drops for colored contact lenses or the eye washes for colored contact lenses can be used not only when wearing colored contact lenses but also when not wearing them for the purpose of dropping or washing the eyes. In the case of a colored contact lens wetting solution, it is used by bringing an appropriate amount of the wetting solution into contact with the colored contact lens when wearing the colored contact lens. Furthermore, in the case of a colored contact lens care solution, it can be used by immersing the colored contact lens in an appropriate amount of the care solution, or by contacting the colored contact lens with the care solution and rubbing the lens. be.

Moreover, the water content of the colored contact lens to which the ophthalmic composition for colored contact lenses according to the present embodiment is applied is not particularly limited, and may be, for example, 20% or more, preferably 30% or more. , is more preferably 40% or more, still more preferably 50% or more, even more preferably 60% or more, and even more preferably 65% or more. Although the upper limit of the water content of the color contact lens is not particularly limited, it is usually 90% or less.

Here, the water content of the color contact lens indicates the proportion of water in the color contact lens, and is specifically determined by the following formula.
Moisture content (%) = (weight of hydrated water/weight of colored contact lens in hydrated state) x 100
Such moisture content can be measured gravimetrically as described in ISO 18369-4:2006.

[2. Method for imparting action to reduce hardness of color contact lens]
The ophthalmic composition for colored contact lenses according to the present invention has the effect of improving the hardness peculiar to colored contact lenses.

Therefore, as one embodiment of the present invention, (A) a terpenoid and (B) one or more selected from the group consisting of vinyl-based polymer compounds and saccharides are contained in an ophthalmic composition for colored contact lenses. A method for imparting an effect of reducing the hardness of a colored contact lens to the ophthalmic composition for a colored contact lens, comprising:

Further, as one embodiment of the present invention, a colored contact lens comprising an ophthalmic composition containing (A) a terpenoid and (B) one or more selected from the group consisting of vinyl polymer compounds and saccharides. is provided.

Furthermore, as one embodiment of the present invention, an ophthalmic composition for color contact lenses containing (A) a terpenoid and (B) one or more selected from the group consisting of vinyl-based polymer compounds and saccharides, A method of reducing hardness of a colored contact lens is provided comprising contacting the colored contact lens. The contacting step may be performed while wearing colored contact lenses or while not wearing colored contact lenses.

Regarding the types and contents of components (A) and (B), the types and contents of other components, and the formulation form and application of the ophthalmic composition for colored contact lenses, [1. ophthalmic composition for colored contact lenses].

The hardness-reducing agent for color contact lenses is referred to as a hardness-reducing agent for color contact lenses, containing (A) a terpenoid and (B) one or more selected from the group consisting of vinyl-based polymer compounds and saccharides. can also Specific aspects of the hardness-lowering agent for colored contact lenses in this case are substantially the same as those of the ophthalmic composition for colored contact lenses described above.

[3. Method for imparting an action to reduce the poor wearing feeling of colored contact lenses]
The ophthalmic composition for colored contact lenses according to the present invention has the effect of reducing the poor feeling of wearing (discomfort upon wearing, for example, rough feeling) caused by colored contact lenses.

Therefore, as one embodiment of the present invention, (A) a terpenoid and (B) one or more selected from the group consisting of vinyl-based polymer compounds and saccharides are contained in an ophthalmic composition for colored contact lenses. A method for imparting an effect of reducing the poor wearing feeling of colored contact lenses to the ophthalmic composition for colored contact lenses, comprising:

Further, as one embodiment of the present invention, a colored contact lens comprising an ophthalmic composition containing (A) a terpenoid and (B) one or more selected from the group consisting of vinyl polymer compounds and saccharides. is provided.

Furthermore, as one embodiment of the present invention, an ophthalmic composition for color contact lenses containing (A) a terpenoid and (B) one or more selected from the group consisting of vinyl-based polymer compounds and saccharides, A method of reducing discomfort caused by colored contact lenses is provided, comprising contacting the colored contact lenses. The contacting step may be performed while wearing colored contact lenses or while not wearing colored contact lenses.

Regarding the types and contents of components (A) and (B), the types and contents of other components, and the formulation form and application of the ophthalmic composition for colored contact lenses, [1. ophthalmic composition for colored contact lenses]. The invention according to each of the above embodiments can also be regarded as an invention related to improving the feeling of wearing a colored contact lens.

The agent for reducing the poor wearing feeling of colored contact lenses contains (A) a terpenoid and (B) one or more selected from the group consisting of vinyl-based polymer compounds and saccharides. It can also be said that it is an agent for reducing the bad feeling of wearing. In this case, the specific aspects of the agent for reducing the poor wearing feeling of colored contact lenses are substantially the same as those of the ophthalmic composition for colored contact lenses described above.

EXAMPLES Hereinafter, the present invention will be described more specifically with reference to Examples and the like. However, the present invention is not limited by these examples and the like.

[Test Example 1: Evaluation of hardness of various soft contact lenses (SCL)]
Using various soft contact lenses shown in Table 1, the following tests were carried out to evaluate the hardness of the soft contact lenses. The soft contact lenses used in this test are all commercial products. A clear contact lens also refers to a uniformly transparent (including colored and uncolored) contact lens that is not a contact lens that alters the appearance of the iris or pupil.

A bubble tester T-1T (manufactured by TECHNO HASHIMOTO Co., Ltd.) was used to measure the hardness of SCL. Specifically, after rinsing the SCL taken out from the package liquid with physiological saline, the liquid on the surface of the SCL was wiped off, and the SCL was placed in a convex shape on a glass stand (the back of the beaker). Using a stainless steel jig with a diameter of 5 cm, the force generated when the jig pushes the contact lens was measured. The measurement conditions are as follows.
・Cycle test (number of cycles 1)
・Round-trip width: 2 mm
・Movement speed: 2mm/s
・Acceleration speed: 0.1G
・Start position: 126.20 mm

Based on the obtained measurement results, the relative hardness of the color SCL was obtained when the hardness of the clear SCL made of the same material was defined as 100%. The results are shown in FIG. It was found that the lens A, which is a color SCL, is about 1.2 times harder than the lens B, which is a clear SCL made of the same material. Similarly, it was found that the lens C, which is a color SCL, is about 1.5 times harder than the lens D, which is a clear SCL made of the same material.

[Test Example 2: Hardness measurement after immersion in formulation solution]
The lens A was immersed for one week in the prescription liquid having the composition shown in Table 2, and the hardness was measured in the same manner as in Test Example 1 to evaluate the effect of each prescription liquid on the hardness of the color SCL.

The results are shown in FIG. In FIG. 2, the hardness ratio (%) indicates the hardness ratio of each prescription liquid when the hardness when immersed in the prescription liquid of Comparative Example 1 is taken as 100%. By coming into contact with the prescription liquid containing geraniol, the hardness peculiar to color contact lenses decreased and improved (Reference Example 1). On the other hand, the prescription solution in which geraniol was combined with hydroxypropylmethylcellulose significantly improved the hardness peculiar to color contact lenses (Example 1).

[Test Example 3: Hardness measurement after immersion in formulation solution]
Hardness was measured in the same manner as in Test Example 2 except that the immersion time was 18 hours using the formulation liquids having the compositions shown in Table 3, and the effect of each formulation liquid on the hardness of the color SCL was evaluated.

The results are also shown in Table 3. It was confirmed that even the prescription liquid of Example 2 containing 33.3 parts by mass of hydroxypropylmethylcellulose per 1 part by mass of geraniol significantly improved the hardness specific to color contact lenses.

[Test Example 4: Hardness measurement after immersion in formulation solution]
Hardness was measured in the same manner as in Test Example 2 except that the immersion time was 18 hours using the formulation liquids having the compositions shown in Table 4, and the effect of each formulation liquid on the hardness of the color SCL was evaluated.

The results are also shown in Table 4. It was confirmed that the prescription liquid of Example 3 in which sodium hyaluronate was combined with geraniol also remarkably improved the hardness peculiar to colored contact lenses.

[Test Example 5: Evaluation of contact lens wearing feeling]
Three monitors wearing soft contact lenses (lens A, lens B) in each eye, using a 10 cm straight line with a scale of 0 to 10 shown in Table 5, the feeling of wearing the contact lens by the VAS method It was evaluated for the badness (roughness, etc.). Specifically, each monitor assigns a scale of 10 to indicate that the wearer feels the worst when wearing contact lenses, and a scale of 0 to indicate that the wearer feels no discomfort when wearing contact lenses. The degree of wearing comfort was recorded on a straight line, and the length (mm) from the 0 scale was used as the score for each monitor. Table 6 shows the average scores of the wearing comfort evaluations by three persons. Soft contact lenses (lens C and lens D) were also tested in the same manner, and the results are shown in Table 7.

From the obtained measurement results, it became clear that the color SCL gives a significantly worse wearing feeling (rough feeling, etc.) than the clear SCL made of the same material.

[Test Example 6: Evaluation of contact lens wearing feeling]
Three monitors wearing colored soft contact lenses (lens A) in both eyes instilled 1 to 2 drops of the prescription solution shown in Table 8 five times a day, and evaluated the results according to the following evaluation items. The feeling of wearing the colored soft contact lenses after daily wear was evaluated. Table 9 shows the results. Lens C was also tested in the same manner, and the results are shown in Table 10.

Evaluation item ◎: No bad feeling of wearing (rough feeling etc.) ○: Almost no feeling of poor wearing feeling (rugging feeling etc.) △: Slightly feeling poor wearing feeling (rough feeling etc.) ×: Wearing feeling clearly feel the badness of

It was confirmed that the formulation solution of Example 2 in which geraniol was combined with hydroxypropylmethylcellulose remarkably improved the poor wearing feeling (such as rough feeling) peculiar to color soft contact lenses.

[Formulation example]
Using the formulations shown in Tables 11 to 13, colored contact lens eye drops, colored contact lens wetting solutions, colored contact lens wetting solutions, and colored contact lens cleaning and storage solutions are prepared. All units in the table are (w/v%). Formulation Examples 1 to 19, 22 to 24, and 26 to 27 were filled in polyethylene terephthalate containers, Formulation Examples 20 and 21 were filled in polypropylene containers, and Formulation Example 25 was filled in polyethylene containers.
Further, a nozzle made of polyethylene was attached to the container for Formulation Examples 1 to 12, and a nozzle made of polybutylene terephthalate was attached to the container for Formulation Examples 13 to 23.

Claims (10)

(A) a terpenoid, and (B ) one or more selected from the group consisting of cellulose -based polymer compounds and glycosaminoglycans, eye drops for color soft contact lenses (however, the following Except for (1) to (3):
(1) containing alginic acid or a salt thereof;
(2) containing sodium carboxymethylcellulose; and (3) having a viscosity of 200 mPa·s or more. ). 2. The eye drop for a color soft contact lens according to claim 1, wherein component (B) contains at least one selected from the group consisting of hydroxypropylmethylcellulose, hyaluronic acid and salts thereof. 2. The eye drop for color soft contact lenses according to claim 1, wherein the component (A) contains menthol. (A) component contains menthol,
The eye drop for color soft contact lenses according to any one of claims 1 to 3, wherein component (B) contains at least one selected from the group consisting of hydroxypropylmethylcellulose, hyaluronic acid and salts thereof. The eye drop for color soft contact lenses according to any one of claims 1 to 4, wherein the component (A) contains menthol, and the content of menthol is 0.0001 to 0.5 w/v%. The ophthalmic solution for color soft contact lenses according to any one of claims 1 to 5, further comprising boric acid. The eye drop for color soft contact lenses according to any one of claims 1 to 6, further comprising a surfactant. The ophthalmic solution for color soft contact lenses according to any one of claims 1 to 7, which is for alleviating discomfort when wearing color soft contact lenses. (A) a terpenoid and (B) one or more selected from the group consisting of vinyl-based polymer compounds and saccharides in ophthalmic compositions for color soft contact lenses (provided that those containing alginic acid or a salt thereof, carboxymethyl cellulose excluding those containing sodium and those having a viscosity of 200 mPa·s or more). . (A) a terpenoid, and (B) one or more selected from the group consisting of cellulose-based polymer compounds and glycosaminoglycans in an ophthalmic composition for color soft contact lenses (provided that the composition contains alginic acid or a salt thereof) , containing sodium carboxymethylcellulose, and those having a viscosity of 200 mPa·s or more. A method of imparting the effect of reducing

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