JP4997054B2 - 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

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

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. Among them, l-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, the present invention
An adsorption inhibitor comprising a monoterpene, which suppresses adsorption of a polymeric antibacterial agent to a contact lens.

The monoterpene can also be used in the state of being contained in an essential oil, preferably,
Eucalyptus oil, bergamot oil, peppermint oil, cool mint oil, spearmint oil and the like can also 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 for eye drops.
% By weight, and 0.0001-0.03% by weight for contact lens care compositions. 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), BUSAN11
57 (trade name, polyethylene polyamine / dimethylamine epichlorohydrin polycondensate containing about 50% by weight, manufactured by Bachman Laboratories), Croquat L (trade name, collagen hydrolyzate derived from collagen hydrolyzate having lauryltrimethylammonium chloride group) A quaternary ammonium-substituted polypeptide containing about 50% by weight, available from 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 polymer antibacterial agent in the ophthalmic composition of the present invention is 0.00001 to 0.5% by weight.
Is preferable, and 0.00001 to 0.01% by weight is particularly preferable. 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) 80) POE sorbitan fatty acid esters such as POE (60) hydrogenated castor oil such as hydrogenated castor oil, POE (9
POE alkyl ethers such as lauryl ether, POE (20) POP (4) POE / POP alkyl ethers such as cetyl ether, POE such as POE (10) nonylphenyl ether
Nonionic surfactants such as E alkylphenyl ethers, amphoteric surfactants such as glycine type such as alkyldiaminoethylglycine, betaine acetate type such as lauryldimethylaminoacetic acid betaine, imidazoline type, POE (10) lauryl ether phosphorus POE such as sodium acid
Alkyl ether phosphates and salts thereof, N-acyl amino acid salts such as sodium lauroylmethylalanine, alkyl ether carboxylates, N-acyl taurine salts such as N-cocoylmethyl taurine sodium, and sulfonates such as sodium tetradecenesulfonate And alkyl sulfates such as sodium lauryl sulfate, POE (3) POE alkyl ether sulfates such as sodium lauryl ether sulfate, and anionic surfactants such as α-olefin sulfonate. 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.

The pharmaceutically active ingredient can be used as an active ingredient of eye drops,
For example, decongestants, muscle regulating agents, anti-inflammatory and astringents, antihistamines, vitamins,
Examples include sulfa drugs, antiallergic agents, cell activators, and the like. Specifically, decongestion of epinephrine, epinephrine hydrochloride, ephedrine hydrochloride, tetrahydrozoline hydrochloride, naphazoline hydrochloride, nafazoline nitrate, phenylephrine hydrochloride, dl-methylephedrine hydrochloride, etc. Ingredients, muscle regulating functional agents such as neostigmine methylsulfate, epsilon-aminocaproic acid,
Anti-histamines such as allantoin, berberine chloride, berberine sulfate, sodium azulenesulfonate, dipotassium glycyrrhizinate, zinc sulfate, zinc lactate, lysozyme chloride, diphenhydramine hydrochloride, chlorpheniramine maleate, flavin adenine dinucleotide sodium , Vitamins such as cyanocobalamin, retinol acetate, retinol palmitate, pyridoxine hydrochloride, panthenol, calcium pantothenate, sodium pantothenate, tocopherol acetate, riboflavin, sulfamethoxazole, sulfamethoxazole sodium, sulfisoxa Sulfa drugs such as sol and sulfisomidine sodium, sodium cromoglycate, ketotifen fumarate, amlexanox, pemirolast potassium Antiallergic agents such as tranilast, potassium L- aspartic acid, L- magnesium aspartate, magnesium potassium L- aspartic acid, aminoethyl sulfonic acid, cell-activating agent such as sodium chondroitin sulfate and the like, without limitation.

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 using a borate buffer or phosphate buffer as a buffer,
The concentration of these buffering agents 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 pH regulators include sodium hydroxide, potassium hydroxide, hydrochloric acid, citric acid, phosphoric acid,
Examples include acetic acid.

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 thereof include eye drops (general eye drops, antibacterial eye drops, eye drops for contact lenses, contact lens mounting solutions, eye wash solutions),
Examples include, but are not limited to, contact lens care compositions (contact lens disinfectant, contact lens preservative, contact lens cleaning agent, contact lens cleaning preservative). 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 for 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.
Then, the pH was adjusted to 7 with a sodium hydroxide solution, and further sterilized purified water was added to make the total volume to 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 90 g of sterile purified water
After adding 0.001 g of 1-menthol dissolved in 0.05 g of Tween80 and adjusting the pH to 8 with sodium hydroxide solution, add sterilized purified water to make a total volume of 100 ml.
A cleaning preservative for contact lenses was prepared.

Example 3 [Preparation of contact lens mounting solution]
Polyhexamethylene biguanide hydrochloride 0.0001g, Sodium chloride 0.5g, Boric acid 0.3g
0.09 g of borax and 0.1 g of hydroxypropylmethylcellulose were dissolved in 90 g of sterilized purified water, and another solution of 0.01 g of l-menthol in 0.5 g of Tween 80 was added, and the pH was adjusted to 6 with sodium hydroxide solution. Further, sterilized purified water was added to make up 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. In detail, it carried out 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, and absorb the liquid with dust-free paper.
Place the reus ATCC6583 on a Mueller Hinton agar plate inoculated with 10 ⁶ / ml, culture at 30 ° C for 72 hours, measure the diameter of the inhibition circle, and calculate the adsorption inhibition rate (%) based on the following formula.
In addition, saturated adsorption conditions to the contact lens of the polymer antibacterial agent (1 contact lens is immersed in 30 mL of test liquid without addition of monoterpene, and stored under temperature conditions around 25 ° C. 24
Repeat the operation to change to a new test solution at intervals of more than an hour. Using the method of [4] in Test Example 1 above, measure the blocking circle of contact lenses that have been subjected to different replacement times, and use the number of replacements where the size of the blocking circle does not increase any more as the saturated adsorption condition). The number of days of immersion of the contact lens in the test solution is set as appropriate.

Evaluation criteria:
+: Blocking circle formation is suppressed at a rate of 5% or more as a diameter, and an adsorption suppressing 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 (5)

(A) at least one monoterpene selected from the group consisting of camphor, borneol and geraniol, and / or at least one essential oil selected from the group consisting of eucalyptus oil, bergamot oil and peppermint oil;
(B) selected from the group consisting of polyhexamethylene biguanide hydrochloride, poly [oxyethylene (dimethyliminio) ethylene- (dimethyliminio) ethylenediglolide], polydronium chloride, and polyethylenepolyamine / dimethylamine epichlorohydrin polycondensate At least one polymeric antibacterial agent,
(A) component is 0.0001-0.032 weight%,
(B) component is 0.00003-0.1 weight%,
Ophthalmic composition for soft contact lenses in which the weight ratio [(B) / (A)] of the component (B) to the component (A) is 0.00625-50 (however, from the group consisting of camphor, borneol and geraniol) Excluding non-heat disinfectant for soft contact lens containing 0.0005 to 0.02 W / V% of at least one selected monoterpenoid and 0.0001 to 0.01 W / V% of polyhexamethylene biguanidine hydrochloride ).   The ophthalmic composition according to claim 1, which is an eye drop.   The ophthalmic composition according to claim 1, which is a contact lens care composition. (B) selected from the group consisting of polyhexamethylene biguanide hydrochloride, poly [oxyethylene (dimethyliminio) ethylene- (dimethyliminio) ethylenediglolide], polydronium chloride, and polyethylenepolyamine / dimethylamine epichlorohydrin polycondensate (A) at least one monoterpene selected from the group consisting of camphor, borneol and geraniol, and / or eucalyptus, in a composition containing 0.00003 to 0.1% by weight of at least one polymeric antibacterial agent And at least one essential oil selected from the group consisting of oil, bergamot oil and peppermint oil in an amount of 0.0001 to 0.032% by weight, and the weight ratio of component (B) to component (A) [(B) / ( A)] is present at 0.00625-50, and the polymer antibacterial agent Method for suppressing adsorption to soft contact lens (however, non-heat disinfectant for soft contact lens containing 0.0001 to 0.01 W / V% of polyhexamethylene biguanidine hydrochloride, comprising camphor, borneol and geraniol Except when 0.0005 to 0.02 W / V% of at least one monoterpenoid selected from the group is blended). (A) at least one monoterpene selected from the group consisting of camphor, borneol and geraniol, and / or at least one essential oil selected from the group consisting of eucalyptus oil, bergamot oil and peppermint oil, (B) poly At least one selected from the group consisting of hexamethylene biguanide hydrochloride, poly [oxyethylene (dimethyliminio) ethylene- (dimethyliminio) ethylenediglolide], polydronium chloride, and polyethylenepolyamine / dimethylamine epichlorohydrin polycondensate Is an adsorption inhibitor that suppresses the adsorption of the polymer antibacterial agent to the soft contact lens, wherein the concentration of the component (A) is 0.0001 to 0.032 wt%, and the concentration of the component (B) is 0.00003 to 0.1% by weight and the concentration of component (B) and component (A) The ratio fouling agent [(B) / (A)] is characterized by the use such that 0.00625 to 50 (however, the polyhexamethylenebiguanidine hydrochloride 0.0001~0.01W / V % , Except for the case where 0.0005 to 0.02 W / V% of at least one monoterpenoid selected from the group consisting of camphor, borneol and geraniol is added to the non-heat disinfectant for soft contact lenses .