JP5437350B2 - Ophthalmic composition - Google Patents

Description

  The present invention relates to an ophthalmic composition, a method for suppressing adsorption of a polymer antibacterial agent to a contact lens, and an adsorption inhibitor.

  In general, widely used contact lenses are divided into two categories: hard contact lenses and soft contact lenses. Hard contact lenses are classified as non-gas permeable lenses and oxygen permeable lenses, and soft contact lenses are classified as low water content lenses, high water content lenses and non water content lenses. Conventionally, low molecular weight antibacterial agents such as benzalkonium chloride and chlorhexidine gluconate have been used as antiseptics for eye drops and contact lens care compositions (Patent Document 1, Patent Document 2, Non-Patent Document 1, etc.) . Although these have high antibacterial activity, they may weaken the hydrophilicity of the lens surface or cause lens modification, which is not satisfactory. In addition, these low molecular weight antibacterial agents are adsorbed on oxygen permeable hard contact lenses and soft contact lenses, and are liable to cause eye disorders such as keratoconjunctival disorders. In particular, soft contact lenses are highly adsorbable, concentrated on the lens, and cause eye damage. Therefore, repeated use for the same contact lens has a problem in terms of safety. Also, sorbic acids that have been used as preservatives have a low adsorptivity to contact lenses, but have a problem of low preservative power when various bacteria are mixed.

  Therefore, in recent years, for contact lenses containing novel high molecular antibacterial agents such as quaternary ammonium polymers and biguanide polymers with low eye irritation, low adsorption to soft contact lenses and high antibacterial activity. Compositions have been developed (Patent Documents 3 to 5 etc.). Although these contact lens compositions have improved safety compared to compositions containing low molecular weight antibacterial agents, eye disorders associated with adsorption to contact lenses are still reported (for example, non-patents). Reference 2).

  Therefore, in contact lens compositions, it is desired to solve the problems of adsorption such as binding and concentration of the polymeric antibacterial agent to the contact lens surface, and to improve irritation to the eye tissue and eye damage.

JP-A-11-130667 Japanese Patent Laid-Open No. 11-180858 Japanese Patent Publication No. 6-49642 Japanese Patent Publication No. 6-49060 Japanese National Patent Publication No. 10-505067

Nikore Magazine, Vol. 37, No.2, pp.154-157 Academic Exhibits P8, P9, Program / Abstract Collection of the 43rd Annual Meeting of the Japanese Contact Lens Society

  The object of the present invention is to provide an ophthalmic composition that suppresses adsorption of a polymer antibacterial agent to a contact lens, a method for suppressing adsorption of a polymer antibacterial agent to a contact lens, and adsorption of a polymer antibacterial agent to a contact lens. It is providing the adsorption inhibitor which suppresses.

  The inventors of the present invention have made various studies in order to solve the above problems, and when monoterpene is used in combination with a polymer antibacterial agent, the adsorption of the polymer antibacterial agent to the contact lens is completely suppressed. The present invention was completed by finding new findings.

That is, the gist of the present invention is as follows.
[1] an ophthalmic composition containing a monoterpene and a polymer antibacterial agent,
[2] A method for suppressing the adsorption of the polymeric antibacterial agent to a contact lens, wherein the monoterpene is present in a composition containing the polymeric antibacterial agent, and [3] The present invention relates to an adsorption inhibitor that suppresses adsorption of a molecular antibacterial agent to a contact lens.

  By using the ophthalmic composition of the present invention, the adsorption of the polymeric antibacterial agent to the contact lens can be remarkably suppressed, and the effect that the contact lens can be used more safely over a long period of time is obtained. Played. In addition, by using the ophthalmic composition of the present invention, uncomfortable symptoms (irritation, redness, scouring, etc.) due to the polymeric antibacterial agent, not only when wearing a contact lens, but also when not wearing it. The effect of improving monoterpenes is achieved.

  Examples of the monoterpene contained in the ophthalmic composition of the present invention include menthol, camphor, borneol, geraniol, cineol, anethole, limonene, eugenol and the like. These monoterpenes may be any of d-form, l-form, or dl-form. Above all, from the functional aspect such as refreshing sensation and fragrance and safety, 1-menthol, d-menthol, dl-menthol. , D-camphor, dl-camphor, d-borneol and dl-borneol are preferred, geraniol, l-menthol, d-camphor and d-borneol are particularly preferred.

  In this invention, adsorption | suction of the polymeric antimicrobial agent with respect to a contact lens can be suppressed by using this monoterpene together with the below-mentioned polymeric antimicrobial agent. Therefore, this invention provides the adsorption inhibitor which suppresses adsorption | suction to the contact lens of a polymeric antibacterial agent which consists of monoterpenes.

  In addition, the monoterpene can be used in a state of being contained in an essential oil, and preferably, eucalyptus oil, bergamot oil, peppermint oil, cool mint oil, spearmint oil and the like can be used. These monoterpenes can be used alone or in combination of two or more.

  The concentration of monoterpene in the ophthalmic composition of the present invention is preferably 0.00001 to 0.1% by weight, more preferably 0.0001 to 0.05% by weight, and most preferably 0.001 to 0.05% by weight for eye drops. In the product, it is 0.0001 to 0.03% by weight. The concentration is preferably 0.1% by weight or less from the viewpoint of suppressing the risk of eye damage, and is preferably 0.00001% by weight or more from the viewpoint of obtaining a sufficient antibacterial agent adsorption suppressing effect.

  The polymer antibacterial agent contained in the ophthalmic composition of the present invention may be a monomer type polymer compound or a polymer type polymer compound, and those having an average molecular weight of about 800 or more are used. The average molecular weight is preferably about 1500 or more, more preferably about 1500 to 500,000. When the polymer type polymer compound is a polymer, the number of polymerizations may vary, and a plurality of monomers may be included. More specifically, polydronium chloride (polyquarterium-1), poly [oxyethylene (dimethyliminio) ethylene- (dimethyliminio) ethylene dichloride], poly (hydroxypropyldialkylammonium chloride), polyethylene polyamine dimethyl Examples thereof include quaternary ammonium compounds such as amine epichlorohydrin polycondensate or salts thereof, biguanide compounds such as polyhexamethylene biguanide hydrochloride or salts thereof, and glycine type surfactants such as alkylpolyaminoethylglycine. For example, a quaternary ammonium compound or a salt thereof is Glokill PQ (trade name, poly (β-hydroxypropyldimethylammonium chloride), manufactured by Rhodia), Unisense CP (trade name, poly (diallyldimethylammonium chloride), Senka ), WSCP (trade name, poly [oxyethylene (dimethyliminio) ethylene- (dimethyliminio) ethylene dichloride] containing about 60% by weight, manufactured by Bachman Laboratories), BSAN1157 (trade name, polyethylene polyamine About 50% by weight of dimethylamine epichlorohydrin polycondensate, manufactured by Bachman Laboratories, Inc., Croquat L (trade name, quaternary ammonium substituted polypeptide derived from collagen hydrolyzate having lauryltrimethylammonium chloride group) 50 layers % Content, available from manufactured by Croda). The biguanide compound or a salt thereof can be obtained from Cosmosil CQ (trade name, containing about 20% by weight of polyhexamethylene biguanide hydrochloride, manufactured by ICI Americas).

  The concentration of the polymeric antibacterial agent in the ophthalmic composition of the present invention is preferably 0.00001 to 0.5% by weight, particularly preferably 0.00001 to 0.01% by weight. The concentration is preferably 0.00001% by weight or more from the viewpoint of obtaining sufficient bactericidal power, and more than 0.5% by weight from the viewpoint of easily obtaining a good adsorption suppression effect by monoterpene and reducing the occurrence of eye damage. Is preferred.

  In addition, the blending ratio of the polymer antibacterial agent and the monoterpene (weight ratio: polymer antibacterial agent / monoterpene) in the ophthalmic composition of the present invention is preferably 0.0001 to 2000, more preferably 0.0005 to 500, and 0.005 to 100 is particularly preferred. The blending ratio is preferably 0.0001 or more from the viewpoint of not feeling uncomfortable due to the too strong cooling feeling of the monoterpene, and preferably 2000 or less from the viewpoint of reducing the occurrence of eye damage of the polymer antibacterial agent. .

  In addition, the concentration in the monoterpene, the polymer antibacterial agent, and the ophthalmic composition used as needed indicates the concentration when the ophthalmic composition is used, and may be adjusted to a higher concentration during storage.

  The ophthalmic composition of the present invention preferably contains inorganic salts from the viewpoint of obtaining an excellent effect of suppressing adsorption to contact lenses. Examples of inorganic salts include sodium chloride, potassium chloride, calcium chloride, magnesium sulfate, magnesium chloride and the like. The concentration of the inorganic salt in the ophthalmic composition of the present invention is preferably 0.01 to 2.0% by weight, more preferably 0.1 to 1.2% by weight. The concentration is preferably 0.01% by weight or more from the viewpoint of enhancing the suppression of the adsorption of the polymer antibacterial agent to the contact lens, and preferably 2.0% by weight or less from the viewpoint that the parameters of the contact lens do not change.

  The ophthalmic composition of the present invention preferably further contains a surfactant in order to suppress adsorption of the polymeric antibacterial agent to the contact lens. POE / POP block copolymer (for example, poloxamer 407, poloxamer 235, poloxamer 188, poloxamer 403, poloxamer 237, poloxamer 124, etc.), monolauric acid POE (20) sorbitan (polysorbate 20), monooleic acid POE (20) sorbitan (polysorbate) POE sorbitan fatty acid esters such as 80), POE hydrogenated castor oil such as POE (60) hydrogenated castor oil, POE alkyl ethers such as POE (9) lauryl ether, POE such as POE (20) POP (4) cetyl ether, etc. -Nonionic surfactants such as POE alkyl ethers, POE alkylphenyl ethers such as POE (10) nonylphenyl ether, glycine types such as alkyldiaminoethylglycine, betaine acetate types such as lauryldimethylaminoacetic acid betaine, imidazoline Mold etc. Surfactants, POE alkyl ether phosphates such as POE (10) sodium lauryl ether phosphate and salts thereof, N-acyl amino acid salts such as sodium lauroylmethylalanine, alkyl ether carboxylates, N-cocoyl methyl taurate sodium, etc. N-acyl taurine salts, sulfonates such as sodium tetradecenesulfonate, alkyl sulfates such as sodium lauryl sulfate, POE (3) POE alkyl ether sulfates such as sodium lauryl ether sulfate, α-olefin sulfonates, etc. And anionic surfactants. POE is an abbreviation for polyoxyethylene and POP is an abbreviation for polyoxypropylene. The number in parentheses indicates the number of added moles.

  The concentration of the surfactant in the ophthalmic composition of the present invention is preferably 0.001% by weight or more from the viewpoint of enhancing the wearing feeling of the contact lens, and from the viewpoint of suppressing adsorption of the surfactant itself to the lens. % By weight or less is preferred. The concentration is preferably 0.001 to 10% by weight, more preferably 0.01 to 5% by weight, most preferably 0.01 to 0.3% by weight for eye drops, and 0.1 to 5% by weight for contact lens care compositions.

  The ophthalmic composition of the present invention comprises, in addition to the monoterpene and the polymer antibacterial agent, as necessary, a pharmaceutically active ingredient, a buffer, an isotonic agent, a thickener, a chelating agent, a stabilizer, pH adjustment. Additives such as preservatives, preservatives, preservatives, cooling agents, suspending agents, etc., as appropriate, within a concentration range that does not affect the physicochemical parameters of contact lenses and does not cause problems such as eye irritation Can do. Although a specific example is given below, it is not limited to these.

  As the pharmaceutically active ingredient, an ingredient used as an active ingredient of eye drops can be used. For example, a decongestant, a muscle regulating agent, an anti-inflammatory / astringent, an antihistamine, vitamins, sulfa, an antiallergic agent, Examples include cell activators, and specifically, epinephrine, epinephrine hydrochloride, ephedrine hydrochloride, tetrahydrozoline hydrochloride, naphazoline hydrochloride, naphazoline nitrate, phenylephrine hydrochloride, dl-methylephedrine hydrochloride, and the like, neostigmine methyl sulfate, etc. Anti-muscle regulating agent, epsilon-aminocaproic acid, allantoin, berberine chloride, berberine sulfate, sodium azulenesulfonate, dipotassium glycyrrhizinate, zinc sulfate, zinc lactate, lysozyme chloride, diphenhydramine hydrochloride, male Antihistamines such as chlorpheniramine acid, flavin adenine dinucleotide sodium, cyanocobalamin, retinol acetate, retinol palmitate, pyridoxine hydrochloride, panthenol, calcium pantothenate, sodium pantothenate, tocopherol acetate, riboflavin and other vitamins, sulfamethoxa Sulfa drugs such as sol, sulfamethoxazole sodium, sulfisoxazole, sulfisomidine sodium, anti-allergic drugs such as sodium cromoglycate, ketotifen fumarate, amlexanox, pemirolast potassium, tranilast, L-aspartic acid Potassium, magnesium L-aspartate, magnesium-potassium L-aspartate, aminoethylsulfonic acid, sodium chondroitin sulfate, etc. Although cell activator include, but are not limited to.

  Examples of the buffer include borate buffer, phosphate buffer, carbonate buffer, citrate buffer, acetate buffer, epsilon aminocaproic acid, aspartate and the like. Preferred are borate buffer, phosphate buffer, carbonate buffer and citrate buffer. Among these, borate buffers include borate salts such as alkali metal borate and alkaline earth metal borate. Examples of the phosphate buffer include phosphates such as alkali metal phosphates and alkaline earth metal phosphates. Moreover, you may use the borate or the hydrate of a phosphate as a borate buffer or a phosphate buffer. When a borate buffer or a phosphate buffer is used as the buffer, the concentration of these buffers in the ophthalmic composition of the present invention is preferably about 0.0001 to 10.0% by weight. More specifically, boric acid or a salt thereof (sodium borate, potassium tetraborate, potassium metaborate, etc.), phosphoric acid or a salt thereof (sodium hydrogen phosphate, sodium dihydrogen phosphate, potassium dihydrogen phosphate, etc.) , Carbonic acid or a salt thereof (sodium hydrogencarbonate, sodium carbonate, etc.), citric acid or a salt thereof (sodium citrate, potassium citrate, etc.).

  Examples of isotonic agents include glycerin, propylene glycol, glucose, mannitol, sorbitol and the like.

  Thickeners include gum arabic powder, sodium alginate, propylene glycol alginate, sodium chondroitin sulfate, sorbitol, dextran 70, tragacanth powder, methylcellulose, carboxymethylcellulose, hydroxyethylcellulose, hydroxypropylmethylcellulose, carboxyvinyl polymer, polyvinyl alcohol, polyvinyl Examples include pyrrolidone and macrogol 4000.

  Chelating agents include edetic acid, edetates (disodium edetate, disodium calcium edetate, trisodium edetate, tetrasodium edetate), nitrilotriacetic acid and its salts, trihydroxymethylaminomethane, sodium hexametaphosphate Citric acid and the like.

  Examples of the stabilizer include the edetic acid, the edetic acid salts, and sodium bisulfite.

  Examples of the pH adjuster include sodium hydroxide, potassium hydroxide, hydrochloric acid, citric acid, phosphoric acid, acetic acid and the like.

  Examples of preservatives and preservatives include sorbic acid, potassium sorbate, sodium sorbate, butyl paraoxybenzoate, propyl paraoxybenzoate, methyl paraoxybenzoate, ethyl paraoxybenzoate, chlorohexidine gluconate, chlorohexidine hydrochloride, benzalkonium chloride Benzethonium chloride, alkyldiaminoethylglycine, chlorobutanol and the like.

  Examples of the refreshing agent include caffeine, menthol, camphor, borneol, geraniol, cineole, anethole, limonene, eugenol, eucalyptus oil, bergamot oil, peppermint oil, cool mint oil, spearmint oil and the like.

  The ophthalmic composition of the present invention can be produced according to a known method by appropriately blending the monoterpene and the polymer antibacterial agent and, if necessary, various additives. For example, the method etc. which mix | blend a monoterpene with the composition containing a polymeric antibacterial agent are mentioned.

  The pH of the ophthalmic composition of the present invention is not particularly limited, but is preferably about 5.0 to 9.0, and more preferably 5.5 to 8. It is desirable to adjust to the range of 5. Adjustment of pH is performed by using the said pH adjuster.

  The osmotic pressure ratio between the ophthalmic composition and physiological saline (osmotic pressure of ophthalmic composition / osmotic pressure of physiological saline) is preferably 0.5 to 2.5, more preferably 0.7 to 1. It is desirable to adjust to 5. The osmotic pressure of the ophthalmic composition is preferably about 140 to 700 mOsm, more preferably 200 to 420 mOsm. The osmotic pressure can be measured with an osmometer.

  The ophthalmic composition of the present invention may be any composition that can be contacted in contact with a contact lens in a liquid state. For example, a solution or a suspension may be mixed or dissolved to be contacted. The composition may be in contact with the lens. Specific examples include eye drops (general eye drops, antibacterial eye drops, eye drops for contact lenses, contact lens mounting solutions, eye wash solutions), contact lens care compositions (disinfectants for contact lenses, storage for contact lenses). Agents, contact lens cleaning agents, contact lens cleaning preservatives) and the like, but are not limited thereto. This ophthalmic solution can be used before, during or during wearing of the contact lens. The contact lens care composition can be used for disinfection, storage, washing, washing and storage of contact lenses.

  The ophthalmic composition of the present invention can be used for any contact lens including hard contact lenses and soft contact lenses. However, since the oxygen permeable hard contact lens or soft contact lens easily absorbs an antibacterial agent, It is preferably used for an oxygen-permeable hard contact lens or soft contact lens.

  The ophthalmic composition of the present invention may be stored in any container, but a container having a low water permeability is preferable, and a container that does not easily adsorb each component is preferably used. It is preferable to use a container that is difficult to perform. In particular, it is preferable to use a hard plastic container as the container. For example, the hard plastic container is made of polycarbonate, polyethylene terephthalate, polyethylene naphthalate, U-polymer, polypropylene, or two or more selected from these groups. It is preferable to be formed including a plastic having the same.

  The method for using the ophthalmic composition is not particularly limited as long as it is a known method having a step of bringing the ophthalmic composition into contact with a contact lens. For example, when the ophthalmic composition is a contact lens care composition, a method of immersing the contact lens in the ophthalmic composition of the present invention added to a care container can be mentioned.

By using the ophthalmic composition of the present invention, the adsorption of the polymer antibacterial agent to the contact lens can be remarkably suppressed, and the effect that the contact lens can be used more safely over a long period of time is obtained. Expressed. In addition, since the ophthalmic composition of the present invention is difficult to adsorb the polymer antibacterial agent on the surface of the contact lens, it is used as it is without further removing operation (eg, rinsing) of the polymer antibacterial agent from the contact lens. There is also an excellent advantage that it can be worn on the eyes. Furthermore, since the adsorption of the polymer antibacterial agent is suppressed, the ophthalmic composition of the present invention can be instilled while wearing the contact lens.
In addition, the ophthalmic composition of the present invention has an unpleasant symptom (irritation, redness, scouring, etc.) caused by the polymeric antibacterial agent even when the contact lens is worn or not. Since the effect of improving is obtained, it can be used.

  In addition, suppression of the adsorption of the polymer antibacterial agent to the contact lens can be evaluated based on the method described in Examples described later.

  Further, the method for suppressing the adsorption of the polymeric antibacterial agent of the present invention to the contact lens comprises contacting the contact lens with a composition containing the polymeric antibacterial agent, and allowing the monoterpene to be present in the composition. It is a feature.

  The polymeric antibacterial agent, contact lens, and monoterpene used in the method may be the same as those used in the ophthalmic composition. The types of the polymeric antibacterial agent, monoterpene, and contact lens may be the same as those used for the ophthalmic composition. Moreover, the said composition may also contain the other additive contained in the said ophthalmic composition.

  In the above method, the method for bringing the contact lens into contact with the composition containing the polymeric antibacterial agent is not particularly limited and may be any known method. For example, in the method, it is preferable to use the ophthalmic composition of the present invention.

  Hereinafter, the present invention will be described in detail with reference to examples, but the present invention is not limited thereto.

Example 1 [Preparation of eye drops for contact lenses]
Polyhexamethylene biguanide hydrochloride 0.00003 g, sodium chloride 0.9 g, sodium dihydrogen phosphate 2.0 g were dissolved in 90 g of sterilized purified water, and 0.05 g of 1-menthol was added to 0.3 g of Tween 80, and sodium hydroxide was added. After adjusting the pH to 7 with the solution, sterilized purified water was further added to make up a total volume of 100 ml to prepare eye drops for contact lenses.

Example 2 [Preparation of cleaning preservative for contact lens care]
Polydronium chloride (average molecular weight about 1200-3100) 0.001 g, Poloxamer 407 (POE-POP block copolymer) 0.1 g, sodium chloride 0.9 g, citric acid 1 g were dissolved in 90 g of sterilized purified water, and separately Tween80 0.05 g was added to 1-menthol. A solution in which 0.001 g was dissolved was added, the pH was adjusted to 8 with a sodium hydroxide solution, and sterilized purified water was further added to make a total volume of 100 ml to prepare a contact lens cleaning preservative.

Example 3 [Preparation of contact lens mounting solution]
Dissolve 0.0001 g polyhexamethylene biguanide hydrochloride, 0.5 g sodium chloride, 0.3 g boric acid, 0.09 g borax, 0.1 g hydroxypropylmethylcellulose in 90 g sterilized purified water, and dissolve 0.01 g l-menthol separately in 0.5 g Tween80. After adjusting the pH to 6 with a sodium hydroxide solution, sterilized purified water was further added to make a total volume of 100 ml to prepare a contact lens mounting solution.

Examples 4 to 9, Comparative Examples 1 and 2
Eye drops for contact lenses having the formulation shown in Table 1 were prepared in the same manner as in Example 1, and each eye drop was filled in a hard plastic container (material: polyethylene terephthalate), and then each eye drop according to the following test method. An antibacterial agent adsorption inhibition test was conducted and evaluated.

Test Example 1 [Antimicrobial Agent Adsorption Suppression Test]
The antibacterial agent adsorption inhibition test was performed by applying the disk method used in the drug susceptibility test (issued by the Public Health Association of Japan, referring to the item “Bacterial / Fungus Test“ Drug Sensitivity Test ”). Staphylococcus aureus ATCC6583 bacteria were used as test bacteria, and the lenses used were SCL1 [main material is methyl methacrylate + glyceryl methacrylate (classified in contact lens classification group I)], SCL2 [main material is hydroxyethyl methacrylate + Methacrylic acid (classified as contact lens classification group IV) was used. The details were as follows.
[1] Put 30 mL of the prepared test solution (ophthalmic composition) in a screw tube (capacity 50 mL, made of polyethylene terephthalate), immerse one lens lightly wiped off, and store at 25 ° C.
[2] On the fifth day, transfer the lens to a screw tube containing 30 mL of fresh test solution and store at 25 ° C.
[3] Do the same as [2] on the 11th day.
[4] On the 15th day, remove the lens from the immersion liquid, absorb the liquid with dust-resistant paper, and place it on a Mueller Hinton agar plate inoculated with 10 ⁶ / ml of S. aureus ATCC6583. After incubation, the diameter of the inhibition circle is measured, and the adsorption inhibition rate (%) is calculated based on the following formula.
Saturation adsorption conditions for contact lenses of polymeric antibacterial agents (1 contact lens is immersed in 30 mL of monoterpene-free test solution and stored under temperature conditions around 25 ° C. New at intervals of 24 hours or more. Repeat the operation of changing to the test solution Measure the blocking circle of the contact lens with different number of replacements by the method of [4] in Test Example 1, and saturate the number of replacements where the size of the blocking circle does not increase any more. The number of days of immersion of the contact lens in the test solution is set as appropriate using the adsorption conditions) as a guide.

Evaluation criteria:
+: The inhibition circle formation is suppressed at a ratio of 5% or more as a diameter, and an adsorption suppression effect is recognized (adsorption suppression rate of 5% or more).
±: Inhibition circle formation is suppressed as a diameter at a ratio of less than 5%, and a slight adsorption suppression effect is observed (adsorption suppression rate of less than 5%).
-: Blocking circle formation is not suppressed, and no adsorption suppression effect is observed (adsorption suppression rate 0%).

  From the results shown in Table 1, the eye drops obtained in Examples 4 to 7 were compared with the eye drop of Comparative Example 1 containing no monoterpene, and the eye drops obtained in Examples 8 and 9 were monoterpenes. Compared to the ophthalmic solution of Comparative Example 2 that does not contain, the polymer antibacterial agent adsorption suppression effect was better. In addition, for 8 subjects, 2 to 3 drops of the prescriptions of Examples 4 to 7 were instilled on one eye, and 2 to 3 drops of the prescription of Comparative Example 1 were applied to the opposite eye, Were examined for unpleasant symptoms (irritation, redness, eye contact, etc.) caused by the polymer antibacterial agent. Each eye drop was instilled at intervals of 1 day or more. Moreover, the test was similarly conducted for the eye drops formulated in Examples 8 and 9 and Comparative Example 2. In the formulations of Examples 4 to 9, there was no unpleasant symptom due to the polymer antibacterial agent, but in the formulations of Comparative Examples 1 and 2, irritation sensation, hyperemia and eye contact were observed with the polymer antibacterial agent.

Examples 10-45, Comparative Examples 3-7
Ophthalmic compositions having the formulations shown in Tables 2 to 7 are prepared in the same manner as in Example 1, and each ophthalmic composition is filled in each hard plastic container.

  The ophthalmic compositions of Examples 10 to 45 were all excellent in the adsorption inhibitory effect of the polymer antibacterial agent.

Claims (10)

(A) menthol, and (B) polyhexamethylene biguanide hydrochloride, poly [oxyethylene (dimethyliminio) ethylene- (dimethyliminio) ethylene dichloride], polydronium chloride, and polyethylenepolyamine / dimethylamine epichlorohydrin polycondensate Containing at least one polymeric antibacterial agent selected from the group consisting of:
(A) component is 0.00001 to 0.1 wt%,
(B) component is 0.00001-0.5 weight%,
A liquid composition for soft contact lenses in which the weight ratio of the component (B) to the component (A) [(B) / (A)] is 0.0001 to 2000,
(C) In a rigid plastic container formed of polycarbonate, polyethylene terephthalate, polyethylene naphthalate, U-polymer, or polypropylene, or formed of plastic having two or more selected from these groups Ophthalmic composition for soft contact lenses, filled
(However, a non-heat disinfectant for soft contact lenses containing menthol 0.0005 to 0.02 W / V% and polyhexamethylene biguanide hydrochloride 0.0001 to 0.01 W / V%, and menthol 0.0001 to A hard plastic container made of polyethylene terephthalate is filled with a liquid composition for soft contact lens care containing 0.03% by weight and 0.00005 to 0.0005% by weight of a polymer antibacterial agent composed of polyhexamethylene biguanide or a salt thereof. Excluding soft contact lens care products) .   The ophthalmic composition according to claim 1, wherein the component (A) is l-menthol.   (B) at least one polymer antibacterial agent selected from the group consisting of polyhexamethylene biguanide hydrochloride, poly [oxyethylene (dimethyliminio) ethylene- (dimethyliminio) ethylene dichloride], and polydronium chloride The ophthalmic composition according to claim 1 or 2, wherein   The ophthalmic composition according to any one of claims 1 to 3, wherein (C) is a hard plastic container formed containing polyethylene terephthalate.   The ophthalmic composition according to any one of claims 1 to 4, which is an eye drop.   The ophthalmic composition according to any one of claims 1 to 4, which is a soft contact lens care composition.   The ophthalmic composition according to any one of claims 1 to 6, wherein the pH of the liquid composition is 5.5 to 8.5.   The ophthalmic composition according to any one of claims 1 to 7, wherein the osmotic pressure of the liquid composition is 140 to 700 mOsm. (C) In a rigid plastic container formed of polycarbonate, polyethylene terephthalate, polyethylene naphthalate, U-polymer, or polypropylene, or formed of plastic having two or more selected from these groups In a filled composition, the composition comprises (B) polyhexamethylene biguanide hydrochloride, poly [oxyethylene (dimethyliminio) ethylene- (dimethyliminio) ethylene dichloride], polydronium chloride, and polyethylene polyamine dimethylamine. When 0.00001-0.5 wt% of at least one polymer antibacterial agent selected from the group consisting of epichlorohydrin polycondensates is contained, (A) menthol is 0.00001-0.1 wt%, And the weight of (B) component and (A) component Ratio [(B) / (A)] is present in the range of 0.0001 to 2000, a method for suppressing adsorption of the polymer antibacterial agent to a soft contact lens (however, polyhexamethylene biguanide hydrochloride) Is added to a non-heat disinfectant for soft contact lenses containing 0.0001 to 0.01 W / V%, and menthol is added to 0.0005 to 0.02 W / V%, and a high amount of polyhexamethylene biguanide or a salt thereof. (Except when 0.0001-0.03% by weight of menthol is blended in a liquid composition for soft contact lens care in which 0.00005-0.0005% by weight of a molecular antibacterial agent is filled in a polyethylene terephthalate hard plastic container) . (A) menthol, (B) polyhexamethylene biguanide hydrochloride, poly [oxyethylene (dimethyliminio) ethylene- (dimethyliminio) ethylene dichloride], polydronium chloride, and polyethylenepolyamine / dimethylamine epichlorohydrin polycondensate An adsorption inhibitor for soft contact lenses of at least one polymer antibacterial agent selected from the group consisting of: (A) the concentration of the component is 0.00001 to 0.1% by weight; The component (A) is such that the concentration is 0.00001 to 0.5% by weight, and the concentration ratio [(B) / (A)] of the component (B) to the component (A) is 0.0001 to 2000. And (B) component are used together, and (C) polycarbonate, polyethylene terephthalate, polyethylene naphthalate, U-polymer, or poly Adsorption inhibitor formed in a hard plastic container formed with a plastic containing two or more selected from these groups (but polyhexamethylene biguanide hydrochloride) Is added to a non-heat disinfectant for soft contact lenses containing 0.0001 to 0.01 W / V%, and menthol is added to 0.0005 to 0.02 W / V%, and a high amount of polyhexamethylene biguanide or a salt thereof. (Except when 0.0001-0.03% by weight of menthol is blended in a liquid composition for soft contact lens care in which 0.00005-0.0005% by weight of a molecular antibacterial agent is filled in a polyethylene terephthalate hard plastic container) .