JP4776282B2 - Contact lens composition - Google Patents

Description

  The present invention relates to a contact lens composition and a contact lens wetting enhancement method.

  To use contact lenses safely and comfortably, it is necessary to wear a tear film cushion to avoid damage to the cornea and conjunctiva due to physical friction with the lens, but hard contact lenses are hydrophobic. It is inherently difficult to get wet because it is made of sex material. In addition, the most frequently used ionic soft contact lenses tend to attract charged components (such as inorganic salts and surface-charged proteins) in tears, and thus easily become dirty, and the lenses are partially hydrophobic and difficult to get wet. Become. If the lens is difficult to wet, it may cause clouding of the contact lens, foreign matter sensation, water and oxygen permeation, inflammation, corneal staining, hyperemia, etc., so the development of a contact lens composition that wets the lens well is required. .

  As a method for improving the wettability of contact lenses, an ophthalmic composition for soft contact lenses containing a terpenoid in addition to a thickening agent such as polyvinyl alcohol or hydroxyethyl cellulose in the contact lens composition (Patent Document 1) : Patent No. 3090125), an ophthalmic composition containing polyoxyethylene polyoxypropylene-substituted ethylenediamine and a thickening agent (Patent Document 2: WO97 / 28827), an alkylene group having a hydroxyl group in the main chain, and 4 An ophthalmic solution containing a polymer containing a quaternary ammonium salt (Patent Document 3: WO00 / 28998) has been reported.

By the way, cromoglycic acid or a salt thereof is used as an antiallergic agent in eye drops, nasal drops, etc., and sorbic acid or a salt thereof is used as an antiseptic in internal use, eye drops, nasal drops, contact lens agents, etc. Lamin or a salt thereof is a substance widely used for internal use, eye drops, external preparations and the like. As an example of containing cromoglycic acid or a salt thereof and sorbic acid or a salt thereof, an ophthalmic solution that improves unpleasant eye irritation by further containing caffeine (Patent Document 4: JP 2003-137781 A) ) Is disclosed. Moreover, as an example containing cromoglycic acid or a salt thereof, and chlorpheniramine or a salt thereof, a topical preparation that improves various symptoms of allergic rhinitis at an early stage by further containing a vasoconstrictor (Patent Document 5) : JP-A-6-336429).
However, it is not known that cromoglycic acid or a salt thereof, sorbic acid or a salt thereof, and chlorpheniramine or a salt thereof enhance contact lens wetting.

An object of the present invention is to provide a contact lens composition that can reduce the discomfort during wearing by reducing the damage to the cornea and conjunctiva during wearing of the contact lens by enhancing the wetting of the contact lens. That is.
Another object of the present invention is to provide a contact lens wetting enhancement method.

  As a result of diligent studies to solve the above problems, the present inventors have found that cromoglycic acid or a salt thereof, sorbic acid or a salt thereof, and chlorpheniramine or a salt thereof have a wetting enhancing action. The present invention has been completed.

That is, the present invention is the composition for contact lenses listed in the following (1) to (3).
(1) A composition for contact lenses, comprising cromoglycic acid or a salt thereof, sorbic acid or a salt thereof, and chlorpheniramine or a salt thereof.
(2) The composition for contact lenses according to (1), wherein the composition for contact lenses is a liquid composition for contact lenses.
(3) The contact lens composition according to (1) or (2), wherein the contact lens composition is an eye drop for contact lens, an eye wash for contact lens, a contact lens mounting solution, or a contact lens care agent.
The present invention also encompasses a method for enhancing the contact lens wetting.
(4) A contact lens wetting enhancement method comprising contacting a contact lens with a composition containing cromoglycic acid or a salt thereof, sorbic acid or a salt thereof, and chlorpheniramine or a salt thereof.

  The present invention can enhance the wettability of contact lenses by including cromoglycic acid or a salt thereof, sorbic acid or a salt thereof, and chlorpheniramine or a salt thereof in the composition. For this reason, unpleasant symptoms such as dryness and foreign body sensation during contact lens wearing can be alleviated, and it contributes to the reduction of obstacles to the cornea and conjunctiva, which is useful for contact lens wearers.

BEST MODE FOR CARRYING OUT THE INVENTION

In the present specification, unless otherwise specified,% means W / V%. Further, the term “contact lens” is used in the meaning of including all types of contact lenses such as hard, oxygen-permeable hard, and soft unless otherwise specified.
In the present specification, “salt” means a pharmacologically or physiologically acceptable salt.

  In the contact lens composition of the present invention, cromoglycic acid is a known compound known as an antiallergic agent, and may be synthesized by a known method or obtained as a commercial product.

In the composition for contact lenses of the present invention, cromoglycic acid may be a pharmaceutically, pharmacologically (pharmaceutically) or physiologically acceptable salt. Such salts include salts with organic bases (eg, salts with organic amines such as methylamine, triethylamine, triethanolamine, morpholine, piperazine, pyrrolidine, tripyridine, picoline, etc.), salts with inorganic bases [eg, Ammonium salts; alkali metals (sodium, potassium, etc.), alkaline earth metals (calcium, magnesium, etc.), salts with metals such as aluminum, etc.], and the like.
These cromoglycic acids or salts thereof can be used alone or in combination of two or more. Moreover, cromoglycic acid or a salt thereof can be used in the form of a hydrate.

  In the contact lens composition of the present invention, the ratio of cromoglycic acid or a salt thereof to be blended in the composition is not particularly limited as long as the effect of the present invention is obtained, but is usually 0.0001 to 5%, preferably 0.001 to 5%. More preferably, it is 0.05 to 3% for eye drops, 0.01 to 0.3% for other compositions, particularly preferably 0.2 to 2% for eye drops, and about 0.02 to 0.2% for other compositions.

  In the composition for contact lenses of the present invention, sorbic acid is a known compound, and may be synthesized by a known method or obtained as a commercial product.

In the contact lens composition of the present invention, sorbic acid can be a pharmaceutically, pharmacologically (pharmaceutically) or physiologically acceptable salt. Examples of such salts include salts with inorganic bases [for example, ammonium salts; alkali metals (sodium, potassium, etc.), alkaline earth metals (calcium, magnesium, etc.), salts with metals such as aluminum, etc.], organic bases And the like (for example, salts with organic amines such as methylamine, triethylamine, triethanolamine, morpholine, piperazine, pyrrolidine, tripyridine, picoline, etc.), and sodium salt and potassium salt are particularly preferred.
These sorbic acids or salts thereof can be used alone or in combination of two or more.

  In the contact lens composition of the present invention, the ratio of sorbic acid or a salt thereof to be blended in the composition is not particularly limited as long as the effect of the present invention is obtained, but is usually 0.001 to 2%, preferably 0.01 to 0.2. %, More preferably 0.05 to 0.2%, particularly preferably about 0.1 to 0.2%.

  In the contact lens composition of the present invention, the compounding ratio of cromoglycic acid or a salt thereof and sorbic acid or a salt thereof (weight ratio: sorbic acid or a salt thereof / cromoglycic acid or a salt thereof) is usually 0.01 for an eye drop. -4, 0.1-20 for other compositions, preferably 0.05-1 for eye drops, 0.5-10 for other compositions, particularly preferably 0.05-0.2 for eye drops, 0.5-2 for other compositions. It is.

  In the contact lens composition of the present invention, chlorpheniramine is a known compound and may be synthesized by a known method or obtained as a commercial product.

In the contact lens composition of the present invention, chlorpheniramine can be a pharmaceutically, pharmacologically (pharmaceutically) or physiologically acceptable salt. Examples of such salts include organic acid salts [for example, monocarboxylate (acetate, trifluoroacetate, butyrate, palmitate, stearate, etc.), polyvalent carboxylate (fumarate, maleate). Acid salt), oxycarboxylate (lactate, tartrate, citrate, succinate, malonate, etc.), organic sulfonate (methanesulfonate, toluenesulfonate, tosylate, etc.) Etc.], and inorganic acid salts (for example, hydrochloride, sulfate, nitrate, hydrobromide, phosphate and the like), and maleate is particularly preferable.
These chlorpheniramines or salts thereof can be used alone or in combination of two or more.

  In the contact lens composition of the present invention, the ratio of chlorpheniramine or a salt thereof to be blended in the composition is not particularly limited as long as the effect of the present invention is obtained, but is usually 0.0001 to 3%, preferably 0.0001 to 0.3%, more preferably 0.001 to 0.3% for eye drops, 0.0001 to 0.03% for other compositions, particularly preferably 0.01 to 0.03% for eye drops, and 0.001 to 0.003% for other compositions .

  In the composition for contact lenses of the present invention, the compounding ratio of cromoglycic acid or a salt thereof and chlorpheniramine or a salt thereof is not particularly limited as long as the effect of the present invention is obtained. For example, cromoglycic acid or a salt thereof 1 The amount of chlorpheniramine or a salt thereof is 0.0003 to 5 parts by weight, preferably 0.005 to 0.15 parts by weight, particularly preferably 0.01 to 0.03 parts by weight with respect to parts by weight.

  The contact lens composition of the present invention further includes a nonionic surfactant, a thickener, a buffer, a pH adjuster, an inorganic salt, and an isotonic agent for the purpose of enhancing or supplementing the wettability of the contact lens. Can be blended in one kind or in combination of two or more kinds.

  The nonionic surfactant is not particularly limited as long as it is pharmaceutically, pharmacologically (pharmaceutically) or physiologically acceptable. For example, polyoxyethylene (hereinafter abbreviated as POE) -polyoxypropylene (hereinafter abbreviated as POP) block copolymer (eg, poloxamer 407, poloxamer 235, poloxamer 188, etc.), a POE-POP block copolymer adduct of ethylenediamine (eg, , Poloxamine), POE sorbitan fatty acid esters such as POE (20) sorbitan monolaurate (polysorbate 20), POE (20) sorbitan monooleate (polysorbate 80), polysorbate 60, POE such as POE (60) hydrogenated castor oil Hardened castor oil, POE alkyl ethers such as POE (9) lauryl ether, POE / POP alkyl ethers such as POE (20) POP (4) cetyl ether, POE alkyl phenyl ethers such as POE (10) nonylphenyl ether , POE (10) Nonionic surfactants such as POE alkylphenyl ethers such as nonylphenyl ether, polyoxyl stearate; glycine type such as alkyldiaminoethylglycine, betaine acetate type such as lauryldimethylaminoacetic acid betaine, imidazoline type Amphoteric surfactants; alkyl ether carboxylates, sulfonates such as sodium tetradecene sulfonate, alkyl sulfates such as sodium lauryl sulfate, N-acyl taurine salts such as sodium N-cocoylmethyl taurate, POE (10) lauryl POE alkyl ether phosphates such as sodium ether phosphate and salts thereof, N-acyl amino acid salts such as sodium lauroylmethylalanine, POE alkyl ether sulfates such as POE (3) sodium lauryl ether sulfate Anionic surfactants such as α-olefin sulfonates; alkylamine salts, alkyl quaternary ammonium salts (benzalkonium chloride, benzethonium chloride, etc.), alkylpyridinium salts (cetylpyridinium chloride, cetylpyridinium bromide, etc.), etc. Cationic surfactants and the like can be mentioned, and poloxamer 407, polysorbate 80, POE (60) hydrogenated castor oil, particularly preferably polysorbate 80 are preferable. The numbers in parentheses indicate the number of added moles.

  In the contact lens composition of the present invention, the ratio of the nonionic surfactant to be blended in the composition is not particularly limited as long as the effect of the present invention is obtained, but is usually 0.001 to 2%, preferably 0.01 to 2%, more preferably 0.05 to 1%, particularly preferably about 0.1 to 0.5%.

  Examples of the thickener include cellulose derivatives (carboxyethyl cellulose, carboxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, methyl cellulose, ethyl cellulose, cellulose, nitrocellulose, etc.), polysaccharides or derivatives thereof (alginic acid, agar, elastin). , Casein, carrageenan, chitin and its derivatives, chitosan and its derivatives, gum arabic, carob gum, karaya gum, xanthan gum, guar gum, guaiac fat, quince seed, collagen, chondroitin sulfate, ceramide, gelatin, dammar gum, tragacanth gum, benzoin gum, locust bean Gum, dextrin, dextran, starch, hyaluronic acid, pectin, Lanthanum sulfate, heparinoid, heparin, heparin sulfate, polygalacturonic acid, etc.), deoxyribonucleic acid, polyacrylic acid, polyethyleneimine, polyethylene oxide, macrogol (polyethylene glycol), polyvinyl alcohol (completely or partially saponified product), polyvinylpyrrolidone, Polyvinyl methacrylate, carboxy vinyl polymer, methyl vinyl ether / maleic anhydride copolymer, ribonucleic acid, and pharmacologically acceptable salts thereof (for example, sodium carboxymethyl cellulose, sodium alginate, sodium chondroitin sulfate, sodium hyaluronate, etc.) Preferably carboxymethylcellulose, sodium carboxymethylcellulose, hydroxyethylcellulose, hydroxy Cellulose, hydroxypropylmethylcellulose, sodium alginate, dextran, polyvinyl alcohol (completely or partially saponified), polyvinyl pyrrolidone, macrogol.

  In the contact lens composition of the present invention, the proportion of the thickener incorporated in the composition is not particularly limited as long as the effect of the present invention can be obtained, but is usually 0.0005 to 50%, preferably 0.00. It is about 001 to 10%, particularly preferably about 0.01 to 5%.

Examples of the buffer include citrate buffer, acetate buffer, carbonate buffer, borate buffer, phosphate buffer, aminoethylsulfonic acid, aspartic acid or salts thereof (potassium aspartate, magnesium aspartate, etc.). , Epsilon-aminocaproic acid, HEPES, MOPS and the like, and borate buffer and phosphate buffer are preferable.
As the citrate buffer, acetate buffer, carbonate buffer, borate buffer, and phosphate buffer, citric acid or a salt thereof (sodium citrate, potassium citrate, etc.), acetic acid or a salt thereof (potassium acetate, Sodium acetate, etc.), carbonic acid or a salt thereof (sodium bicarbonate, sodium carbonate, etc.), boric acid or a salt thereof (potassium tetraborate, sodium borate, borax, potassium metaborate, etc.), phosphoric acid or a salt thereof (phosphoric acid) Disodium hydrogen, sodium dihydrogen phosphate, potassium dihydrogen phosphate, dipotassium hydrogen phosphate, etc.).
The concentration of these buffering agents in the composition for contact lenses of the present invention is, for example, about 0.001 to 10%, preferably about 0.01 to 5%.

Examples of the pH adjuster include inorganic acids (hydrochloric acid, boric acid, polyphosphoric acid, sulfuric acid, phosphoric acid, etc.), organic acids (aspartic acid, aminoethylsulfonic acid, epsilon-aminocaproic acid, citric acid, gluconic acid, glutamic acid, Succinic acid, acetic acid, oxalic acid, tartaric acid, lactic acid, fumaric acid, propionic acid, malic acid, etc.), gluconolactone, ammonium acetate, inorganic base (calcium hydroxide, potassium hydroxide, sodium hydroxide, magnesium hydroxide, carbonate) Sodium hydrogen, sodium carbonate, borax, etc.), organic bases (diisopropanolamine, triisopropanolamine, triethanolamine, monoethanolamine, lysine, etc.), and pharmacologically acceptable salts thereof. Are hydrochloric acid and sodium hydroxide.
The concentration of these pH adjusting agents in the contact lens composition of the present invention is, for example, about 0.00001 to 5%, preferably about 0.0001 to 2%.

Examples of the isotonic agent include inorganic salts (for example, sodium bisulfite, sodium sulfite, potassium chloride, calcium chloride, sodium chloride, magnesium chloride, potassium acetate, sodium acetate, sodium bicarbonate, sodium carbonate, sodium thiosulfate, Magnesium sulfate, disodium hydrogen phosphate, sodium dihydrogen phosphate, potassium dihydrogen phosphate, dipotassium hydrogen phosphate, etc., polyhydric alcohols (eg, ethylene glycol, glycerin, 1,3-butylene glycol, propylene) Glycol), saccharides or sugar alcohols (for example, sorbitol, butter sugar, mannitol, etc.). Of these, sodium chloride and potassium chloride are preferred.
The concentration of these isotonic agents in the contact lens composition of the present invention is, for example, about 0.001 to 10%, preferably about 0.01 to 5%.

The composition for contact lenses of the present invention can be adjusted to a pH and / or osmotic pressure within a range that is acceptable to a living body, if necessary. Specifically, the pH is usually 4.0 to 8.0, preferably 4.5 to 7.5, particularly preferably 5.5 to 7.0, and the osmotic pressure ratio (physiology of the Japanese Pharmacopoeia). The ratio of the osmotic pressure when the osmotic pressure of the saline solution is 1, is usually 0.4 to 4.2, preferably 0.4 to 2.1, particularly preferably about 0.5 to 1.4. It is.
The pH can be adjusted using the buffering agent, the pH adjusting agent and the like, and the osmotic pressure can be adjusted using the isotonic agent and the like.

  The contact lens composition of the present invention may contain a combination of various components (including pharmacologically active components and physiologically active components) in addition to the components described above as long as the effects of the present invention are achieved. The type of such component is not particularly limited, and examples thereof include a decongestant component, an ocular muscle modulator component, an anti-inflammatory component or an astringent component, an antihistamine component or an antiallergic component, vitamins, amino acids, antibacterial agents. Examples thereof include a drug component or a bactericidal component, a saccharide, a local anesthetic component, a steroid component, a glaucoma therapeutic agent, and a cataract therapeutic agent. Examples of suitable components in the present invention include the following components.

  Decongestant: α-adrenergic drugs such as imidazoline derivatives (oxymetazoline, tetrahydrozoline, naphazoline, etc.), β-phenylethylamine derivatives (epinephrine, ephedrine, phenylephrine, methylephedrine, etc.), and their pharmacologically or physiologically (E.g., epinephrine hydrochloride, ephedrine hydrochloride, oxymetazoline hydrochloride, tetrahydrozoline hydrochloride, naphazoline hydrochloride, phenylephrine hydrochloride, methylephedrine hydrochloride, epinephrine hydrogen tartrate, tetrahydrozoline nitrate, naphazoline nitrate; epinephrine hydrogen tartrate; Etc.). These may be d-form, l-form or dl-form.

  Ocular muscle modulator component: Cholinesterase inhibitor having an active center similar to acetylcholine, for example, quaternary ammonium compounds such as neostigmine methylsulfate, atropine, tropicamide, helenien, and pharmaceutically or physiologically acceptable salts thereof ( For example, atropine sulfate).

  Anti-inflammatory component or astringent component: zinc salt (for example, zinc sulfate, zinc lactate, etc.), azulene sulfonic acid, aspirin, acemetacin, allantoin, ibuprofen, epsilon-aminocaproic acid, indomethacin, indomethacin farnesyl, lysozyme chloride, tiaramid hydrochloride, Glycyrrhizic acid, methyl salicylate, diclofenac, silver nitrate, celecoxib, thiaprofenic acid, piroxicam, pranoprofen, bromfenac, berberine, mefenamic acid, meloxicam, lysozyme, loxoprofen sodium, rofecoxib, etc. and their pharmaceutically or physiologically acceptable Salts (eg, sodium azulenesulfonate, dipotassium glycyrrhizinate, ammonium glycyrrhizinate, diclofenac sodium, brom E diclofenac sodium, berberine chloride, berberine sulfate), and the like.

  Antihistamine component or antiallergic agent component: for example, acitazanolast, astemizole, azelastine, amlexanox, ibudilast, iproheptin, emedastine, ebastine, epinastine, oxatomide, olopatadine, clemastine, ketotifen, diphenhydramine, splatastazin, splatastazine, Tranilast, fexofenadine, bepotastine, pemirolast, mequitazine, repirinast, levocabastine, loratadine, or salts thereof (e.g., azelastine hydrochloride, iproheptin hydrochloride, olopatadine hydrochloride, diphenhydramine hydrochloride, levocabastine hydrochloride, emedastine fumarate fenmalate, fumarate) , Pemirolast potassium, etc.).

  Vitamins: For example, vitamins A [eg, carotene, dehydroretinal, lycopene, retinal, retinol, retinoic acid and pharmacologically acceptable salts thereof (eg, retinol acetate, retinol palmitate, etc.), vitamin B [Dicetiamine hydrochloride, thiamine hydrochloride, pyridoxine hydrochloride, fursultiamine hydrochloride, octothiamine, chicotiamine, dicetiamine, thiamine nitrate, bistiamine nitrate, thiamine, thiamine disulfide, thiamine dicetyl nitrate, bisibutamine, bisbenchamine, full Sultiamine, prosultiamine, benfotiamine, flavin adenine dinucleotide, flavin adenine dinucleotide sodium, riboflavin butyrate, riboflavin, riboflavin sodium phosphate, Doxin, pyridoxal, pyridoxal phosphate, pyridoxal calcium phosphate, hydroxocobalamin hydrochloride, hydroxocobalamin acetate, cyanocobalamin, hydroxocobalamin, deoxyadecocobalamine, methylcobalamin, dihydrofolate, tetrahydrofolate, folate, nicotinic alcohol, nicotinic acid, nicotinic acid Amide, panthenol, pantothenic acid, calcium pantothenate, sodium pantothenate, inositol, choline, biotin, etc.], vitamin C [ascorbic acid and derivatives thereof, erythorbic acid and derivatives thereof and pharmacologically acceptable salts thereof ( For example, sodium ascorbate, sodium erythorbate, etc.)], vitamin D [eg, ergocalciferol, cholecalcifero , Dihydroxycholecalciferol, dihydrotaxosterol, hydroxycholecalciferol and pharmacologically acceptable salts thereof, etc.], vitamin E [for example, tocopherol and its derivatives, ubiquinone derivatives and their pharmacologically acceptable Salts (such as tocopherol succinate, tocopherol calcium succinate, tocopherol acetate, tocopherol nicotinate, etc.)], other vitamins [eg, eriocitrin, orotic acid, carnitine, γ-oryzanol, ferulic acid, hesperidin, rutin and the like Pharmacologically acceptable salts (such as carnitine chloride and methyl hesperidin).

  Amino acids: for example, asparagine, aspartic acid, aminoethylsulfonic acid (taurine), alanine, isoleucine, ornithine, glycylglycine, glycine, glutamine, glutamic acid, creatinine, chondroitin sulfate, cysteine, serine, tyrosine, tryptophan, threonine, valine , Histidine, hydroxyproline, hydroxylysine, phenylalanine, proline, methionine, lysine, leucine or a salt thereof (eg, potassium aspartate, magnesium aspartate, magnesium / aspartate mixture, cysteine hydrochloride, sodium glutamate, sodium chondroitin sulfate, etc.) . These may be d-form, l-form or dl-form.

  Antibacterial component or bactericidal component: Acrinol, aminoglycoside antibacterial agent [kanamycin (for example, aminodeoxykanamycin sulfate, kanamycin sulfate, etc.), gentamicin (for example, gentamicin sulfate), sisomycin (for example, sisomycin sulfate), streptomycin (for example, ), Tobramycin, micronomycin (eg, micronomycin sulfate), alkylpolyaminoethylglycine, chloramphenicol antibacterial agents (eg, chloramphenicol), sulfonamides [eg, Famethoxazole, sulfisoxazole, sulfisomidine and pharmacologically acceptable salts (sulfamethoxazole sodium, sulfisoxazole diethanolamine, sulfi Xazole monoethanolamine, sulfisomezole sodium, sulfisomidine sodium, etc.)], quaternary ammonium compounds [eg cetylpyridinium, benzalkonium, benzethonium and pharmacologically acceptable salts (cetylpyridinium chloride) , Benzalkonium chloride, benzethonium chloride, cetylpyridinium bromide)], tetracycline antibacterials (tetracycline hydrochloride, oxytetracycline hydrochloride, etc.), new quinolones (ciprofloxacin hydrochloride, ofloxacin hydrochloride, ciprofloxacin, norfloxacin, levofloxacin) , Lomefloxacin (eg, lomefloxacin hydrochloride)], β-lactam antibacterial [carbenicillin (eg, carbenicillin sodium), sulbenicillin (eg, Sulbenicin sodium, etc.), cefmenoxime (eg, cefmenoxime hydrochloride, etc.), penicillin (eg, benzylpenicillin potassium)], berberine or a salt thereof (eg, berberine sulfate, berberine chloride, etc.), boric acid or a salt thereof (borax) ), Polypeptide antibacterials (such as colistin and sodium colistin metasulfonate), macrolide antibacterials [such as erythromycin (eg, erythromycin lactobionate), kitasamycin, spiramycin], and fradiomycin (eg, sulfate) Fradiomycin, etc.), polymyxin (eg, polymyxin sulfate, etc.), dibekacin (eg, dibekacin sulfate, etc.), amikacin (eg, amikacin sulfate, etc.) and the like can be used. Antiviral drugs such as acyclovir, adenine arabinoside, iododeoxycytidine, idoxuridine, carbocyclic oxetanocin G, gancyclovir, cyclocytidine, cytosine arabinoside, cidophobia, trifluorothymidine, valacyclovir, bromo Amphotericin B, isoconazole, itraconazole, econazole, clotrimazole, nystatin, pimaricin, fluorocytosine, fluconazole, flucytosine, miconazole and the like can be used as deoxyuridine, foscarnet, polyvinyl alcohol iodine, iodine and antifungal agents.

  Sugars: monosaccharides (eg glucose), disaccharides (eg trehalose, fructose, lactose etc.), oligosaccharides (eg pullulan, lactulose, raffinose etc.), sugar alcohols (eg xylitol, sorbitol, mannitol etc.) Such.

  Local anesthetic ingredients: ethyl aminobenzoate, oxybuprocaine, cocaine, cornecaine, dibucaine, tetracaine, piperocaine, bupivacaine, procaine, proparacaine, hexothiocaine, mepivacaine, meprilucaine, lidocaine and their salts (oxybuprocaine hydrochloride, cocaine hydrochloride) , Cornecaine hydrochloride, Dibucaine hydrochloride, Tetracaine hydrochloride, Diethylaminoethyl parabutylaminobenzoate, Piperocaine hydrochloride, Procaine hydrochloride, Proparacaine hydrochloride, Hexothiocaine hydrochloride, Lidocaine hydrochloride, etc.).

  Steroid components: cortisol, dexamethasone, triamcinolone, parameterzone, hydrocortisone, fluorometholone, prednisolone, betamethasone, methylprednisolone, hydroxymesterone and salts thereof (hydrocortisone caproate, prednisolone caproate, cortisone acetate, hydrocortisone acetate, prednisolone acetate, Dexamethasone sodium metasulfobenzoate, dexamethasone sodium sulfate, dexamethasone sodium phosphate, triamcinolone acetonide, betamethasone sodium phosphate, dexamethasone sodium metasulfobenzoate, methylprednisolone) and the like.

  Glaucoma treatment ingredients: acetazolamide, unoprostone (eg, isopropyl unoprostone), epinephrine, apraclonidine hydrochloride, carteolol hydrochloride, dipivefrin hydrochloride, dorzolamide hydrochloride, pilocarpine hydrochloride, bunazosin hydrochloride, bupanolol hydrochloride, betaxolol hydrochloride, befnolol hydrochloride, carbachol, Levobunolol hydrochloride, epinephrine dipivalate, distigmine bromide, nipradilol, timolol maleate, metazolamide, latanoprost, and salts thereof.

  Cataract treatment component: glutathione, cineraria martima, salivary gland hormone, thiopronin, pirenoxine, dihydro azapentacene disulfonate and salts thereof (for example, sodium 5,12-dihydroazapentacene disulfonate).

The amount of these components in the composition for contact lenses is appropriately selected according to the type of formulation, the type of active ingredient, etc. Is known. For example, it can be selected from the range of about 0.0001 to 30%, preferably about 0.001 to 10% with respect to the whole preparation.
More specifically, the content of each component in the contact lens composition is, for example, as follows.

Decongestant component (vasoconstrictor or sympathomimetic): For example, 0.0001 to 0.5%, preferably 0.0005 to 0.3%, more preferably 0.001 to 0.1%.
Eye muscle modulator component: For example, 0.0001 to 0.5%, preferably 0.0005 to 0.1%, more preferably 0.0005 to 0.01%.
Anti-inflammatory component or astringent component: for example 0.0001-10%, preferably 0.0001-5%.
Antihistamine component or antiallergic component: for example 0.0001-10%, preferably 0.001-5%.
Vitamins: For example, 0.0001 to 1%, preferably 0.0001 to 0.5%.
Amino acids: For example, 0.0001 to 10%, preferably 0.001 to 3%.
Antibacterial component or bactericidal component: for example, 0.00001-10%, preferably 0.0001-10%.
Saccharides: For example, 0.0001 to 5%, preferably 0.001 to 5%, more preferably 0.01 to 2%.
Polysaccharides or derivatives thereof: for example, 0.0001-2%, preferably 0.01-2%, more preferably 0.01-1%.
Cellulose or a derivative thereof or a salt thereof: For example, 0.001 to 5%, preferably 0.01 to 1%.
Water-soluble polymers other than those described above: For example, 0.001 to 10%, preferably 0.001 to 5%, more preferably 0.01 to 3%.
Local anesthetic component: For example, 0.001-1%, preferably 0.01-1%.
Steroid component: For example, 0.001-1%, preferably 0.01-1%.
Glaucoma treatment component: for example, 0.001 to 5%, preferably 0.01 to 1%.
Cataract treatment component: for example, 0.0001 to 10%, preferably 0.001 to 5%.

In addition, in the composition for contact lenses of the present invention, various components and additives are appropriately selected according to conventional methods according to the use and form as long as the effects of the invention are not impaired. The above may be used in combination. As those components or additives, for example, carriers (water, aqueous solvents, aqueous or oily bases, etc.), sugars, preservatives, bactericides, or antibacterial agents that are commonly used in the preparation of semi-solids and liquids And various additives such as a fragrance or a refreshing agent and a chelating agent.
Although the typical component used for the composition for contact lenses of this invention below is illustrated, it is not limited to these.

Sugars: for example, arabinose, galactose, xylose, glucose, cyclodextrin, sucrose, cellobiose, deoxyribose, trehalose, fructose, pullulan, maltitol, maltose, mannose, lactulose, lactose, raffinose, lyxose, ribulose, ribose Physically acceptable salts.
Sugar alcohols: For example, xylitol, sorbitol, mannitol and the like.
These may be d-form, l-form or dl-form.

  Preservatives, bactericides or antibacterial agents: for example, acrinol, alkylpolyaminoethylglycine (such as alkyldiaminoethylglycine hydrochloride), benzoic acid or its salts (such as sodium benzoate), isopropanol, isopropylmethylphenol, undecylenic acid, ethanol, chloride Cetylpyridinium, benzalkonium chloride, benzethonium chloride, polydronium chloride, methylrosaniline chloride, orthophenylphenol, hydrogen peroxide, caprylic acid, chlorxylenol, chlorhexidine or its salts (chlorhexidine hydrochloride, chlorhexidine gluconate, etc.), chlorophene, chlorobutanol 5-chloro-2-methyl-4-isothiazolin-3-one, cetylpyridinium bromide, sulfamine, thiabendazole, thimerosal, chi , Dehydroacetic acid, sodium dehydroacetate, triclosan, paraoxybenzoic acid ester (methyl paraoxybenzoate, ethyl paraoxybenzoate, propyl paraoxybenzoate, butyl paraoxybenzoate, etc.), halocarban, biguanide compounds (polyhexamethylene biguanide, etc.) ), 8-hydroxyquinoline (oxyquinoline sulfate), hinokitiol, phenethyl alcohol, phenoxyethanol, propanol, propionic acid, benzyl alcohol, popiyon iodine, polydiallyldimethylammonium chloride, poly [oxyethylene (dimethyliminio) ethylene- (Dimethyliminio) ethylene dichloride], polyethylene polyamine / dimethylamine epichlorohydrin polycondensate (trade name, for example, Busan 1157 , Manufactured by Bachman), polymyxin B, polylysine, mercurochrome, 2-methyl-4-isothiazolin-3-one, lactoferrin, lysozyme, resorcin, Glokill (trade names such as Glokill PQ, manufactured by Rhodia), and the pharmacology thereof And salts which are acceptable.

  Perfume or refreshing agent: terpenes (for example, anethole, eugenol, camphor, geraniol, cineol, borneol, menthol, limonene, ryuuno, etc. These may be any of d-form, l-form or dl-form) , Cool mint oil, cinnamon oil, spearmint oil, mint water, mint oil, peppermint oil, bergamot oil, eucalyptus oil, rose oil, etc.).

  Chelating agents: for example, ascorbic acid, edetic acid, citric acid, succinic acid, trihydroxymethylaminomethane, nitrilotriacetic acid, 1-hydroxyethane-1,1-diphosphonic acid, hexametaphosphoric acid, polyphosphoric acid, metaphosphoric acid, and the like Pharmacologically acceptable salts and the like (for example, tetrasodium edetate, sodium edetate).

  Stabilizer: Dibutylhydroxytoluene, trometamol, sodium formaldehyde sulfoxylate (Longalite), tocopherol, sodium pyrosulfite, monoethanolamine, aluminum monostearate, etc.

  Solubilizer, base: octyldodecanol, olive oil, sesame oil, titanium oxide, potassium bromide, soybean oil, camellia oil, corn oil, rapeseed oil, paraffin, castor oil, plastibase, peanut oil, lanolin, petrolatum and the like.

Sugars: For example, 0.001 to 10%, preferably 0.01 to 5%.
Preservatives, bactericides or antibacterial agents: for example 0.00001-5%, preferably 0.0001-2%.
Perfume or refreshing agent: for example, 0.00001-5%, preferably 0.0001-2%.
Chelating agent: for example, 0.00001-5%, preferably 0.0001-2%.

  The composition for contact lenses of the present invention is not limited to a specific form, and in combination with various carriers (aqueous carrier, hydrophilic carrier, oily carrier, liquid carrier, etc.), depending on the purpose, a semisolid agent (ointment) Agent) and liquid preparations. However, from the viewpoint of ease of use, a liquid agent is preferable.

  Since the contact lens composition of the present invention has enhanced contact lens wettability and excellent safety, any composition that contacts the contact lens may be used. For example, in the case of a liquid agent, even a solution is suspended. The composition may be a liquid, or may be a composition to be applied as it is, or a composition in which two or more preparations are mixed or dissolved when necessary and contacted with a contact lens. Specific examples of liquid preparations include eye drops (agents) (including general eye drops, antibacterial eye drops and artificial tears type eye drops that can be used while wearing hard or soft contact lenses), eye wash for contact lenses (Agent) (including eye wash that can be used while wearing a hard or soft contact lens), contact lens mounting liquid, contact lens care composition (contact lens disinfectant, contact lens preservative, contact lens Cleaning agents, contact lens cleaning preservatives, and the like), but are not limited thereto.

  The method for using the contact lens composition of the present invention is not particularly limited as long as it is a known method having a step of bringing the contact lens composition into contact with the contact lens. For example, in the case of eye drops or eye wash, there may be mentioned a method of eye drop or eye wash with the contact lens composition of the present invention while wearing the contact lens. In addition, the contact lens composition of the present invention can be used for cleaning, storing, and wearing a contact lens, not only when the contact lens is worn but also when not worn.

  The composition for contact lenses of the present invention can be produced by a known method. For example, cromoglycic acid, sorbic acid and chlorpheniramine are dissolved using distilled water or purified water and additives, adjusted to a predetermined osmotic pressure and pH, filtered and sterilized in an aseptic environment, and washed and sterilized. It can be manufactured by aseptically filling a container.

  Examples of the resin of the plastic container that contains the composition for contact lenses of the present invention include olefin resins (polyethylene, polypropylene, etc.), polyester resins, polyphenylene ether resins, polycarbonate resins, polysulfone resins, polyamide resins. And polyimide resins, hard vinyl chloride resins, styrene resins (polystyrene, acrylonitrile-styrene copolymers (AS resins), etc.), cellulose acetates, and the like.

As the polyester resin, for example, a resin composed of a dicarboxylic acid component (such as an aromatic dicarboxylic acid component such as phthalic acid, terephthalic acid or naphthalenedicarboxylic acid) and a diol component can be used. Specifically, aromatic polyester resins such as polyalkylene terephthalate [poly C2-4 alkylene terephthalate such as polyethylene terephthalate (PET) and polybutylene terephthalate (PBT)], polyalkylene naphthalate [polyethylene naphthalate (PEN), etc. ), Poly C2-4 alkylene naphthalate such as polybutylene naphthalate], polycycloalkylene terephthalate [poly (1,4-cyclohexylenedimethylene terephthalate) (PCT) etc.], polyarylates (bisphenols (bisphenol- A) and a homopolyester such as a resin composed of phthalic acids (phthalic acid, terephthalic acid). The polyester resin also includes a copolyester containing the homopolyester unit as a main component (for example, 50% by weight or more), a copolymer of the homopolyester (such as a copolymer of PET and PCT), and the like. .
Examples of the polycarbonate-based resin include aromatic polycarbonates based on bisphenols (such as bisphenol-A).

  As a resin for a plastic container containing the composition for contact lenses of the present invention, an olefin resin, a polyester resin, a polycarbonate resin (specifically, polyethylene, polypropylene, polyethylene terephthalate, polyethylene naphthalate, polyarylate) Bisphenol-A), particularly preferably an olefin resin and a polyester resin (specifically, polypropylene, polyethylene terephthalate, polyethylene naphthalate, polyarylate).

  The plastic container may be a polymer alloy (polymer blend or the like) as long as there is no real harm in cost performance, strength, light permeability, gas or water vapor barrier properties (moisture permeability), and the like. Preferred polymer alloys include polymer blends of a plurality of synthetic resins (such as polymer blends of PET and PEN).

  The present invention also includes a method of enhancing contact lens wetting. In the method of the present invention, wetting enhancement of contact lenses can be achieved by using cromoglycic acid or a salt thereof, sorbic acid or a salt thereof, and chlorpheniramine or a salt thereof in combination. In the method of the present invention, cromoglycic acid or a salt thereof, sorbic acid or a salt thereof, chlorpheniramine or a salt thereof, a blending ratio, a blending amount, and the like are the same as those used in the composition.

The act of using the contact lens wetting enhancement method of the present invention is an act of contacting the contact lens with a composition that enhances wetting before or after or during wearing, regardless of direct or indirect application. It may be an act of applying as it is, or an action of mixing or dissolving and contacting with the contact lens. Therefore, although it may be contained in the same preparation, it can also be achieved by mixing those used in different preparations or mixing them immediately before use.
As a specific example, eye drops (agents) for contact lenses (including general eye drops, antibacterial eye drops, and artificial tears type eye drops that can be used while wearing hard or soft contact lenses) Eye drops, contact lens eyewashes (agents) (including eyewashes that can be used while wearing hard or soft contact lenses), eyewashes while wearing contact lenses, before wearing contact lenses Wet contact lens with contact lens mounting solution, contact lens care agent (contact lens disinfectant, contact lens preservative, contact lens cleaning agent, contact lens cleaning preservative, etc.) used after desorption of contact lens Although the act to perform can be mentioned, it is not limited to these. Preferably, eye drops (agents) for contact lenses (including general eye drops, antibacterial eye drops, and artificial tears type eye drops that can be used even when wearing hard or soft contact lenses) are applied while wearing contact lenses. Action: Eyewash for contact lenses (agent) (including eyewash that can be used while wearing hard or soft contact lenses).

  In the contact lens wetting enhancement method of the present invention, various components (including pharmacologically active components and physiologically active components) may be contained in combination as long as the wettability is not impaired. The type of such components is not particularly limited, but specific examples are the same as those of the above-described contact lens composition.

  EXAMPLES Hereinafter, although an Example and a comparative example are shown and this invention is demonstrated concretely, this invention is not restrict | limited to the following Example.

Test Example 1 Wetting test
In accordance with the formulations of Example 1 and Comparative Examples 1 to 5 shown in Table 1, each component was dissolved in sterilized purified water to prepare a test solution with a total amount of 100 mL.
Next, a contact lens (One Day Accuview (registered trademark) manufactured by Johnson & Johnson Co., Ltd.) is soaked in physiological saline all day and night and then divided into four equal parts, with one of the sections facing the front curve (the side not in contact with the cornea). It was placed on a flat surface and the lens surface was lightly wiped with lint-free (registered trademark: manufactured by Asahi Kasei Corporation). 3 μL of the test solution was gently dropped on the lens section, and the state 10 seconds after the dropping was photographed from the side of the contact lens with a CCD camera (2.1 MEGAPIEL VH8000 manufactured by KEYENCE).
The contact point of the contact lens surface, test solution, and air is P, and the angle between the tangent line drawn from P to the test solution and the tangent line drawn on the contact lens surface is the side containing the test solution as the contact angle θ. The difference Δ with the contact angle of purified water was calculated by the following equation. The test was performed 5 times for each test solution, and the average value was taken as Δ (average value).
Δ = θ of purified water-θ of each example and comparative example
The results are shown in Table 1.
It means that the smaller the θ is, the easier the surface of the contact lens gets wet. Therefore, the larger Δ is, the better the lens gets wet.

  From Comparative Examples 1 and 2, sodium cromoglycate and chlorpheniramine maleate alone did not show an effect of improving wetting compared to purified water, but from Comparative Example 4 sodium cromoglycate and maleic acid It was found that when chlorpheniramine was combined, it wets synergistically. Further, Comparative Example 5 shows that wetting is poor when potassium sorbate and chlorpheniramine maleate are combined, but Example 1 shows that wetting is significantly improved by further containing cromoglycic acid. It was.

  The formulation examples are given below.

Claims (6)

(A) cromoglycic acid or a salt thereof, (B) sorbic acid or a salt thereof, and (C) chlorpheniramine or a salt thereof , wherein the component (B) relative to 1 part by weight of the component (A) is 0.01 An eye drop for contact lenses, characterized in that it is -4 parts by weight . The eye drop for contact lenses according to claim 1, wherein the content of (A) cromoglycic acid or a salt thereof is 0.0001 to 5 w / v%. The eye drop for contact lenses according to claim 1 or 2, wherein the content of (B) sorbic acid or a salt thereof is 0.001 to 2 w / v%. The eye drop for a contact lens according to any one of claims 1 to 3, wherein the component (C) is 0.0003 to 5 parts by weight relative to 1 part by weight of the component (A). (C) The eye drop for contact lenses according to any one of claims 1 to 4, wherein the content of chlorpheniramine or a salt thereof is 0.0001 to 3 w / v%. (A) Cromoglycic acid or a salt thereof, (B) sorbic acid or a salt thereof, and (C) a composition containing chlorpheniramine or a salt thereof is brought into contact with the contact lens. Method.