JP2011084520A - Ophthalmic composition for soft contact lens - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide an ophthalmic composition for soft contact lenses, which prevents germs to be deposited on soft contact lenses while it contains aspartic acid and/or a salt thereof and a boric acid buffer. <P>SOLUTION: The ophthalmic composition for soft contact lenses is formulated by concurrently using (A) at least one selected from the group consisting of aspartic acid and salts thereof, (B) a boric acid buffer, and (C) a polymer having a phosphorylcholine analogous group in the side chain. <P>COPYRIGHT: (C)2011,JPO&INPIT

Description

  The present invention relates to an ophthalmic composition for a soft contact lens that can suppress the adhesion of bacteria to the soft contact lens. More specifically, the present invention relates to an ophthalmic composition for soft contact lenses that contains aspartic acid and / or a salt thereof and a borate buffer, and that can suppress bacterial adhesion to the soft contact lens.

  In recent years, the number of wearers of contact lenses has increased, and among them, the number of wearers of soft contact lenses has increased. Since the contact lens is used in direct contact with the ocular mucosa, it is important to maintain a clean state without wearing foreign substances such as bacteria during wearing. Therefore, it is important that the ophthalmic composition for contact lenses is designed so that foreign substances such as bacteria do not adhere to the contact lenses.

  On the other hand, a polymer having a phosphorylcholine-like group in the side chain is known as a compound having high biocompatibility. In addition, the polymer is known to be effective for skin care because it has functions such as keratin protection and moisture retention (see Patent Document 1). Furthermore, it has been found that the polymer is effective in prevention or treatment of dry eye (see Patent Document 2) and improvement in retention of active ingredients (see Patent Document 3) in the ophthalmic field. Thus, the polymer has not only biocompatibility but also various pharmacological actions, and has attracted attention as a functional material. In particular, in recent years, the use of the polymer in the field of ophthalmology has been actively attempted, and an ophthalmic composition formulated with the polymer has also been reported (see Patent Documents 4-5).

  Moreover, the boric acid buffer is used for the purpose of imparting a buffering action to the ophthalmic composition and imparting formulation stability. Furthermore, aspartic acid or a salt thereof is known to have a cell activation action or the like in the ophthalmic field, and is also used as an amino acid for nutritional supplementation to the eye.

  However, there is no appreciable effect on the bacterial adherence to soft contact lenses when the aforementioned polymer having a phosphorylcholine-like group in the side chain, borate buffer, and aspartic acid or a salt thereof are used in combination. is the current situation.

JP 9-52848 A Japanese Patent Laid-Open No. 10-324634 JP 11-335301 A JP 2008-273959 A JP 7-166154 A

  As a result of various studies for the purpose of creating a new ophthalmic composition for soft contact lenses, the present inventors have unexpectedly adopted a borate buffer as a buffer, which is used aspartic acid and / or. It has been found that when used in combination with the salt, the adhesion of bacteria to a soft contact lens (hereinafter sometimes referred to as SCL) is significantly increased. Many conjunctival resident bacteria are non-pathogenic, but if bacteria attach excessively to SCL, a biofilm is formed on the SCL surface by extracellular substances secreted from the attached bacteria, Will increase the risk of bacterial infections. Under such a background, in designing an ophthalmic composition containing aspartic acid and / or a salt thereof and a borate buffer, it is also necessary to develop a means for suppressing bacterial adhesion to SCL.

  Therefore, an object of the present invention is to provide an ophthalmic composition for SCL that contains aspartic acid and / or a salt thereof, and a borate buffer, and in which bacterial adhesion to SCL is suppressed. .

  As a result of intensive studies to solve the above problems, the present inventors have surprisingly found that phosphorylcholine-like groups are present together with aspartic acid and / or a salt thereof and a boric acid buffer in an ophthalmic composition for SCL. It has been found that by using a polymer having a side chain in combination, bacterial adhesion to SCL can be effectively suppressed. The present invention has been completed by further studies based on this finding.

That is, this invention provides the ophthalmic composition for SCL and the method of the aspect hung up below.
Item 1. (A) at least one selected from the group consisting of aspartic acid and salts thereof;
(B) a borate buffer,
(C) a polymer obtained by polymerizing the monomer represented by the general formula (I) alone or with another monomer capable of copolymerization;

[Wherein, n1 is an integer of 2 to 4, R ₁ is a hydrogen atom or a methyl group, R ₂ is a group represented by — (R ₆ O) _n2 —R ₆ — (R ₆ has 1 to 4 carbon atoms] And n2 represents an integer of 0 to 5), and R _{3 to} R ₅ are the same or different and represent a hydrogen atom or an alkyl group having 1 to 4 carbon atoms. ]
An ophthalmic composition for soft contact lenses, comprising:
Item 2. Component (C) is a polymer of a monomer represented by the general formula (I), or a copolymer of a monomer represented by the general formula (I) and a monomer represented by the following general formula (II). Item 5. An ophthalmic composition for soft contact lenses according to Item 1.

[Wherein, R ₇ represents a hydrogen atom or a methyl group, and R ₈ represents a hydrogen atom or a linear or branched alkyl group having 1 to 6 carbon atoms. ]
Item 3. Item 3. The ophthalmic composition for soft contact lenses according to Item 1 or 2, wherein the component (C) is a copolymer of 2-methacryloyloxyethyl phosphorylcholine and butyl methacrylate.
Item 4. Item 4. The ophthalmic composition for soft contact lenses according to any one of Items 1 to 3, wherein the content ratio of the component (A) is 0.001 to 3 w / v%.
Item 5. Item 5. The ophthalmic composition for soft contact lenses according to any one of Items 1 to 4, wherein the content ratio of the component (B) is 0.01 to 3 w / v%.
Item 6. Item 5. The ophthalmic composition for soft contact lenses according to any one of Items 1 to 4, wherein the content of the component (C) is 0.0001 to 5 w / v%.
Item 7. Item 7. The ophthalmic composition for soft contact lenses according to any one of Items 1 to 6, further comprising (D) at least one selected from the group consisting of ethylenediamineacetic acid, derivatives thereof, and salts thereof.
Item 8. Item 8. The ophthalmic composition for soft contact lenses according to Item 7, comprising at least one selected from the group consisting of ethylenediamineacetic acid and salts thereof as component (D).
Item 9. Item 9. The ophthalmic composition for soft contact lenses according to Item 7 or 8, wherein the content ratio of the component (D) is 0.0005 to 0.2 w / v%.
Item 10. Item 10. The ophthalmic composition for soft contact lenses according to any one of Items 1 to 9, which is an eye drop or a contact lens mounting solution.
Item 11. (A) at least one selected from the group consisting of aspartic acid and salts thereof, (B) a boric acid buffer, and (C) a monomer represented by the general formula (I) that can be used alone or in copolymerization A method for inhibiting bacterial adhesion to SCL, comprising contacting an SCL ophthalmic composition containing the monomer and polymerized polymer with SCL.
Item 12. Item 12. The adhesion suppression method according to Item 11, wherein the ophthalmic composition for SCL further comprises (D) at least one selected from the group consisting of ethylenediamineacetic acid, derivatives thereof, and salts thereof.
Item 13. (C) a monomer represented by the general formula (I) in the ophthalmic composition for SCL, which comprises at least one selected from the group consisting of aspartic acid and salts thereof, and (B) a borate buffer. A method for imparting an effect of inhibiting bacterial adhesion to SCL to the ophthalmic composition for SCL, comprising blending a polymer obtained by polymerizing a polymer with other monomers capable of being alone or copolymerized.
Item 14. Item 14. The method according to Item 13, wherein the SCL ophthalmic composition further comprises (D) at least one selected from the group consisting of ethylenediamineacetic acid, derivatives thereof, and salts thereof.

  According to the present invention, since the adhesion of bacteria to SCL can be suppressed while containing aspartic acid and / or a salt thereof and a borate buffer, the risk of bacterial infection caused by SCL wearing can be reduced. An ophthalmic composition for SCL that can use SCL more safely is provided. Furthermore, according to the present invention, by suppressing the adhesion of bacteria to SCL, it is possible to inhibit the formation of biofilms that serve as a hotbed for other microorganisms, and thus to eliminate the adverse effects of microorganisms other than bacteria. Become.

In the reference test example 1, it is a figure which shows the result of having measured the number of adhesion bacteria of Pseudomonas aeruginosa with respect to SCL processed with the test liquid (comparative example 1-2), and having calculated the bacterial adhesion rate (%). In Test Example 1, it is a figure which shows the result of having measured the adhesion bacteria number of Pseudomonas aeruginosa with respect to SCL processed with the test liquid (Example 1-3 and Comparative Example 3-9), and having calculated the bacterial adhesion rate (%). . In Test Example 2, it is a figure which shows the result of having measured the number of adhesion bacteria of Pseudomonas aeruginosa with respect to SCL processed with the test liquid (Example 4 and Comparative Example 10-11), and having calculated the bacterial adhesion rate (%). In the reference test example 2, it is a figure which shows the result of having measured the number of adhesion bacteria of Pseudomonas aeruginosa with respect to SCL processed with the test liquid (comparative example 12-15), and having calculated the bacterial adhesion rate (%).

1. Ophthalmic Composition for SCL The ophthalmic composition for SCL of the present invention contains at least one selected from the group consisting of aspartic acid and salts thereof (hereinafter sometimes simply referred to as component (A)).

  Among the components (A), the salt of aspartic acid is not particularly limited as long as it is pharmaceutically, pharmacologically (pharmaceutically) or physiologically acceptable. For example, alkali metal such as sodium salt and potassium salt Salts: Alkaline earth metal salts such as magnesium salts and calcium salts. These aspartic acid salts may be used alone or in combination of two or more. As aspartic acid and salts thereof, any of D-form, L-form and DL-form may be used, but L-form is particularly preferred.

  In the ophthalmic composition for SCL of the present invention, as component (A), aspartic acid and salts thereof may be used alone, or two or more may be used in combination. Among the components (A), preferred are salts of aspartic acid, more preferably magnesium aspartate, potassium aspartate, combinations thereof, particularly preferably potassium aspartate, and still more preferably potassium L-aspartate. In addition, when using a combination of magnesium aspartate and potassium aspartate as the component (A), these ratios are not particularly limited. For example, potassium aspartate is usually 70 to 150 per 100 parts by weight of magnesium aspartate. A weight part grade is illustrated.

  In the ophthalmic composition for SCL of the present invention, the content ratio of the component (A) is appropriately set according to the type of the component (A), the type of other components to be blended, etc., as an example, the ophthalmic composition for SCL The total amount of the component (A) is 0.001 to 3 w / v%, preferably 0.01 to 2 w / v%, more preferably 0.1 to 2 w / v%, particularly preferably 0.1 to 1 w / v%. Illustrated.

  The ophthalmic composition for SCL of the present invention further contains a borate buffer (hereinafter sometimes simply referred to as component (B)).

  The borate buffer used as component (B) is not particularly limited as long as it is pharmaceutically, pharmacologically (pharmaceutically) or physiologically acceptable. For example, boric acid (orthoboric acid), metaboric acid Hypoboric acid, tetraboric acid, and salts thereof. Examples of these salts include alkali metal salts, alkaline earth metal salts, ammonium salts, and the like. Specific examples of boric acid buffers used as the component (B) include boric acid, metaboric acid, hypoboric acid, sodium borate, potassium tetraborate, sodium tetraborate, potassium metaborate, ammonium borate, boron Examples include sand. These may be hydrates. These boric acid buffers may be used alone or in combination of two or more. The component (B) is preferably a combination of boric acid and borax. In addition, as for boric acid and borax, Japanese Pharmacopoeia conformity goods are used suitably and these can use a commercially available thing.

  As the component (B), for example, when boric acid and borax are used in combination, these ratios are not particularly limited. However, the borax is generally 0. 1-200 weight part, Preferably it is 1-100 weight part, More preferably, 5-50 weight part is mentioned.

  In the ophthalmic composition for SCL of the present invention, as long as the content ratio of the component (B) is within a range where the effects of the present invention can be achieved, the component (B) alone may be set in a range where the buffering action cannot be exerted. , (B) is appropriately set according to the type of component, the type of other components to be blended, and the like. For example, as the content ratio of the component (B), the total amount of the component (B) is 0.01 to 3 w / v%, preferably 0.1 to 2.5 w / v% with respect to the total amount of the ophthalmic composition for SCL. More preferably, 0.5 to 2 w / v% is exemplified.

  Further, in the ophthalmic composition for SCL of the present invention, the ratio of the component (B) to the component (A) is not particularly limited as long as the content ratio described above is satisfied, but the total amount of the component (A) is 100 weights. It is desirable to satisfy a ratio in which the total amount of component (B) is 1 to 20000 parts by weight, preferably 50 to 2000 parts by weight, more preferably 100 to 1500 parts by weight, and particularly preferably 20 to 1200 parts by weight per part. .

  In addition to the components (A) and (B), the ophthalmic composition for SCL of the present invention is a polymer obtained by polymerizing a monomer represented by the following general formula (I) with another monomer that is singly or copolymerizable ( Hereinafter, it may be simply expressed as “component (C)”. As described above, by using the component (C), it is possible to effectively suppress bacterial adhesion to the SCL caused by the combination of the components (A) and (B).

  In general formula (I), n1 represents an integer of 2 to 4, preferably 2 or 3, and more preferably 2.

In general formula (I), R ₁ represents a hydrogen atom or a methyl group, preferably a methyl group.

Further, in the general formula _{(I), R 2} is - shows a group represented by _{- (R 6 O) n2 -R} 6. Here, R < ₆ > shows a C1-C4 alkylene group. Specific examples of such an alkylene group include a methylene group, an ethylene group, a propylene group, and a butylene group. R ₆ is preferably an alkylene group having 1 to 3 carbon atoms, more preferably an alkylene group having 2 carbon atoms (ethylene group). N2 represents an integer of 0 to 5, preferably an integer of 0 to 2, and more preferably 0.

Moreover, in general formula (I), R < ₃ > -R < ₅ > is the same or different and shows a hydrogen atom and a C1-C4 alkyl group. Examples of such an alkyl group include a methyl group, an ethyl group, an n-propyl group, and an n-butyl group. As R < ₃ > -R < ₅ >, Preferably, a hydrogen atom or a C1-C2 alkyl group, More preferably, a C1-C1 alkyl group (methyl group) is mentioned.

Formula Preferable examples of the monomer represented by (I), 2-methacryloyloxyethyl phosphorylcholine (MPC; n1 is 2, _{R 1} is methyl, _{R 2} is an ethylene _group, R 3 to R ₅ is a methyl group) , 2-methacryloyloxyethyl phosphoryl ethanolamine (MPE; n1 is 2, _{R 1} is methyl, _{R 2} is an ethylene _group, R 3 to R ₅ is a hydrogen atom), particularly preferably exemplified 2-methacryloyloxyethyl phosphorylcholine The

  In the ophthalmic composition for SCL of the present invention, the component (C) is a polymer of a monomer represented by the general formula (I) (hereinafter sometimes simply referred to as “monomer (I)”). It may also be a copolymer of monomer (I) and another monomer, or a mixture of a polymer of monomer (I) and a copolymer of monomer (I) and another monomer. There may be.

  When a copolymer is used as the component (C), as the other monomer other than the monomer (I), the finally obtained copolymer is pharmaceutically, pharmacologically (pharmaceutically) or physiologically. Although it does not restrict | limit as long as it is accept | permitted, As a suitable example, the monomer (henceforth only described as "monomer (II)") represented by the following general formula (II) is illustrated.

In the general formula (II), R ₇ represents a hydrogen atom or a methyl group, preferably a methyl group.

In general formula (II), R ₈ represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms. Examples of such an alkyl group include a methyl group, an ethyl group, an n-propyl group, an n-butyl group, an n-pentyl group, and an n-hexyl group. R ₈ is preferably an alkyl group having 1 to 5 carbon atoms, more preferably an alkyl group having 1 to 4 carbon atoms, and particularly preferably an alkyl group having 4 carbon atoms (n-butyl group).

Preferred examples of monomer (II) include butyl methacrylate (BMA; R ₇ is methyl group, R ₈ is n-butyl group), methyl methacrylate (MMA; R ₇ is methyl group, R ₈ is methyl group), 2- Hydroxyethyl methacrylate (HEMA; R ₇ is methyl group, R ₈ is hydroxyethyl group); more preferably, 2-hydroxyethyl methacrylate, butyl methacrylate; and particularly preferably butyl methacrylate.

When monomer (II) can take the form of a salt (for example, when R ₇ is a hydrogen atom), monomer (II) may be a salt. Examples of the salt form of monomer (II) include alkali metal salts such as sodium and potassium.

  When using a copolymer as the component (C), the composition ratio of the monomer (I) and other monomers varies depending on the structure of the monomer used, etc., but effectively exerts a preventive or therapeutic effect on dry eye. From the viewpoint, the monomer (I) is usually 50 to 95 mol%, preferably 60 to 90 mol%, more preferably 75 to 85 mol%, based on the total amount of the copolymer.

  In addition, the molecular weight of the polymer used as the component (C) varies depending on the type of monomer, etc., and is limited as long as it is pharmaceutically, pharmacologically (pharmaceutically) or physiologically acceptable. However, for example, the weight average molecular weight is 5,000 to 2,000,000, preferably 40,000 to 1,200,000, more preferably 100,000 to 1,000,000, and particularly preferably 400,000 to 800,000. The weight average molecular weight is measured by GPC analysis.

  Monomer (I) and monomer (II) are known compounds or known methods from known compounds (for example, JP-A-58-154591, JP-A-60-184093, polymer articles) Vol.35, 423-427, 1978, published by the Society of Polymer Science, Japan).

  The polymer used as the component (C) can be obtained by polymerizing the monomer (I) and, if necessary, other monomers according to a known method in the field of polymer chemistry. Specifically, the polymerization reaction is carried out in the presence of a polymerization initiator in an appropriate solvent such as water, methanol, ethanol, propanol, t-butanol, benzene, toluene, dimethylformamide, tetrahydrofuran, chloroform, or a mixed solvent thereof. The polymerization may be performed for a certain period of time under appropriate temperature conditions.

  In the ophthalmic composition for SCL of the present invention, among the components (C), a polymer of monomer (I), a copolymer of monomer (I) and monomer (II); more preferably MPC or MPE Polymer, copolymer of MPC or MPE and HEMA or BMA; even more preferably, homopolymer of MPC, copolymer of MPC and HEMA, copolymer of MPC and BMA; particularly preferably copolymer of MPC and BMA Examples are polymers. In the present specification, the MPC homopolymer or the copolymer of MPC and monomer (II) may be referred to as MPC polymer.

  The polymer used as the component (C) can also be a commercially available product. The commercially available component (C) includes the Lipidure series (trade name: “LIPIDURE-PMB (BG ) ”,“ LIPIDURE-PMB (Ph10) ”,“ LIPIDURE-PMB ”,“ LIPIDURE-HM ”,“ LIPIDURE-HM-500 ”) and the like.

  In the ophthalmic composition for SCL of the present invention, the content ratio of the component (C) is appropriately set according to the type of polymer to be the component (C), but as an example, the ophthalmic composition for SCL The total amount of component (C) is 0.0001 to 5 w / v%, preferably 0.001 to 1 w / v%, more preferably 0.01 to 0.5 w / v%, particularly preferably 0. 0.02-0.2 w / v%, more particularly 0.06-0.2 w / v% is exemplified. The content rate of (C) component illustrated here is effective from a viewpoint of suppressing the adhesion of the microbe to SCL more effectively.

  Further, in the ophthalmic composition for SCL of the present invention, the ratio of the component (C) to the component (A) is not particularly limited as long as the content ratio described above is satisfied, but the total amount of the component (A) is 100 weights. The ratio that the total amount of component (C) is 0.01 to 10000 parts by weight, preferably 0.1 to 1000 parts by weight, more preferably 2 to 200 parts by weight, and particularly preferably 2 to 100 parts by weight per part is satisfied. It is desirable to do. The ratio of the component (A) and the component (C) exemplified here is effective from the viewpoint of more effectively suppressing the adhesion of bacteria to SCL.

  Furthermore, the ophthalmic composition for SCL of the present invention comprises at least one selected from the group consisting of ethylenediamineacetic acid, derivatives thereof, and salts thereof in addition to the components (A) to (C) (hereinafter simply referred to as ( D) may be described as a component). When the component (D) is used in combination with the components (A) and (B) above, the adhesion of bacteria to the SCL is unexpectedly promoted and the bacterial adhesion to the SCL is enhanced. According to the ophthalmic composition, by including the component (C), even if the component (D) coexists with the components (A) and (B), it can effectively suppress bacterial adhesion to the SCL. It is possible.

  Among the components (D), ethylenediamineacetic acid is a compound in which 1 to 4 carboxymethyl groups are bonded to the two amino groups of ethylenediamine. Regarding the ethylenediamineacetic acid used as the component (D) in the present invention, There is no particular limitation as long as it is pharmaceutically, pharmacologically (pharmaceutically) or physiologically acceptable. Specific examples of ethylenediamineacetic acid used in the present invention include ethylenediaminediacetic acid (EDDA), ethylenediaminetriacetic acid, ethylenediaminetetraacetic acid (edetic acid, EDTA), and the like. Examples of the ethylenediamineacetic acid derivative include N- (2-hydroxyethyl) ethylenediaminetriacetic acid (HEDTA) and diethylenetriaminepentaacetic acid (DTPA). Among these ethylenediamineacetic acids and derivatives thereof, ethylenediaminetetraacetic acid is preferable. These ethylenediamineacetic acids and / or their derivatives may be used alone or in any combination of two or more.

  In addition, the salt of ethylenediamineacetic acid and / or a derivative thereof among the component (D) is not particularly limited as long as it is pharmaceutically, pharmacologically (pharmaceutically) or physiologically acceptable. Specifically, organic acid salts [for example, monocarboxylate (acetate, trifluoroacetate, butyrate, palmitate, stearate, etc.), polyvalent carboxylate (fumarate, maleate, Succinate, malonate, etc.), oxycarboxylate (lactate, tartrate, citrate, etc.), organic sulfonate (methanesulfonate, toluenesulfonate, tosylate, etc.)], Inorganic acid salts (eg, hydrochloride, sulfate, nitrate, hydrobromide, phosphate, etc.), salts with organic bases (eg, methylamine, triethylamine, triethanolamine, morpholine, piperazine, pyrrolidine) Salts with organic amines such as tripyridine and picoline), salts with inorganic bases [eg ammonium salts; alkali metals (sodium, potassium, etc.), alkaline earth metals (calcium, magnesium, etc.), metals such as aluminum, etc. Salt, etc.]. Among these salts, preferred are salts with inorganic bases, more preferred are alkali metal salts, still more preferred are sodium salts and potassium salts, and particularly preferred are sodium salts. These salts may be used alone or in any combination of two or more.

  The ethylenediamineacetic acid, its derivative and / or salt used as the component (D) may be in the form of a hydrate.

  When the component (D) is blended in the ophthalmic composition for SCL of the present invention, one kind may be selected from ethylenediamineacetic acid, derivatives thereof, and salts thereof and used alone. Any combination of the above may be used. The component (D) used in the present invention is preferably ethylenediaminetetraacetic acid and / or a salt thereof, more preferably ethylenediaminetetraacetic acid and / or a sodium salt thereof, still more preferably disodium ethylenediaminetetraacetic acid and / or ethylenediaminetetraacetate. Examples include disodium acetate dihydrate.

  When the component (D) is added to the ophthalmic composition for SCL of the present invention, the content ratio of the component (D) is appropriately set according to the type of the component (D), the type of other components, etc. For example, the total amount of component (D) is 0.0001 to 2 w / v%, preferably 0.001 to 1 w / v%, more preferably 0.005 to 0.07 w / v%, and particularly preferably 0.01 to 0.07 w / v%. .

  In the ophthalmic composition for SCL of the present invention, the ratio of the component (D) to the component (A) is not particularly limited as long as the content ratio described above is satisfied, but per 100 parts by weight of the total amount of the component (A) The ratio of the total amount of component (D) is 0.05 to 5000 parts by weight, preferably 0.1 to 500 parts by weight, more preferably 1 to 100 parts by weight, and particularly preferably 1 to 50 parts by weight. Is desirable.

  The SCL ophthalmic composition of the present invention may further contain a buffering agent other than the boric acid buffering agent in addition to the components (A) to (C). The buffer that can be incorporated into the ophthalmic composition for SCL of the present invention is not particularly limited as long as it is pharmaceutically, pharmacologically (pharmaceutically) or physiologically acceptable. Examples of such buffers include phosphate buffer, carbonate buffer, citrate buffer, acetate buffer, Tris buffer, epsilon-aminocaproic acid, and the like. These buffering agents may be used in combination. As buffering agents other than boric acid buffering agents, phosphate buffering agents, carbonate buffering agents, and citrate buffering agents are preferable, and phosphate buffering agents are more preferable. Examples of the phosphate buffer include phosphates such as alkali metal phosphates and alkaline earth metal phosphates. Examples of the carbonate buffer include carbonates such as alkali metal carbonates and alkaline earth metal carbonates. Examples of the citrate buffer include alkali metal citrate and alkaline earth metal citrate. Moreover, you may use the hydrate of a phosphate as a phosphate buffer. More specific examples include phosphoric acid or a salt thereof (disodium hydrogen phosphate, sodium dihydrogen phosphate, potassium dihydrogen phosphate, trisodium phosphate, dipotassium phosphate, calcium monohydrogen phosphate, diphosphate phosphate, Calcium hydrogen, etc.), carbonic acid or a salt thereof (sodium hydrogen carbonate, sodium carbonate, ammonium carbonate, potassium carbonate, calcium carbonate, potassium hydrogen carbonate, magnesium carbonate, etc.), citric acid or a salt thereof (sodium citrate, potassium citrate, citric acid, etc.) And calcium acetate, sodium dihydrogen citrate, disodium citrate, etc.), acetic acid or a salt thereof (ammonium acetate, potassium acetate, calcium acetate, sodium acetate, etc.). These buffering agents may be used alone or in any combination of two or more.

  When a buffering agent other than a boric acid buffer is blended in the ophthalmic composition for SCL of the present invention, the content of the buffering agent other than the boric acid buffering agent, the type of buffering agent used, the type and amount of other components However, for example, the total amount of buffering agents other than borate buffering agent is 0.01 to 10 w / v%, preferably, with respect to the total amount of the ophthalmic composition for SCL. Examples include a ratio of 0.1 to 5 w / v%, more preferably 0.5 to 2 w / v%.

  The ophthalmic composition for SCL of the present invention preferably further contains a surfactant from the viewpoint of further suppressing bacterial adhesion to SCL. The surfactant that can be incorporated into the ophthalmic composition for SCL of the present invention is not particularly limited as long as it is pharmaceutically, pharmacologically (pharmaceutically) or physiologically acceptable, and is a nonionic surfactant. Any of an agent, an amphoteric surfactant, an anionic surfactant, and a cationic surfactant may be used.

  Specific examples of the nonionic surfactant that can be incorporated in the ophthalmic composition for SCL of the present invention include monolauric acid POE (20) sorbitan (polysorbate 20), monopalmitic acid POE (20) sorbitan (polysorbate 40) POE sorbitan fatty acid esters such as monostearic acid POE (20) sorbitan (polysorbate 60), tristearic acid POE (20) sorbitan (polysorbate 65), monooleic acid POE (20) sorbitan (polysorbate 80); POE / POP block copolymers such as poloxamer 235, poloxamer 188, poloxamer 403, poloxamer 237 and poloxamer 124; POE cured castor oil such as POE (60) hydrogenated castor oil (polyoxyethylene hydrogenated castor oil 60); POE ( 9) POE alkyl ethers such as lauryl ether; POE-POP alkyl ethers such as POE (20) POP (4) cetyl ether POE alkylphenyl ethers such as POE (10) nonylphenyl ether; In the compounds exemplified above, POE is polyoxyethylene, POP is polyoxypropylene, and the numbers in parentheses indicate the number of moles added. Specific examples of the amphoteric surfactant that can be blended in the ophthalmic composition for SCL of the present invention include alkyldiaminoethylglycine. Specific examples of the cationic surfactant that can be incorporated into the SCL ophthalmic composition of the present invention include benzalkonium chloride and benzethonium chloride. Specific examples of the anionic surfactant that can be blended in the ophthalmic composition for SCL of the present invention include alkylbenzene sulfonate, alkyl sulfate, polyoxyethylene alkyl sulfate, and aliphatic α-sulfomethyl. Examples include esters and α-olefin sulfonic acids. In the ophthalmic composition for SCL of the present invention, these surfactants may be used alone or in combination of two or more. Among these surfactants, nonionic surfactants are preferable, and POE (60) hydrogenated castor oil (polyoxyethylene hydrogenated castor oil 60), poloxamer 407, monooleic acid POE (20) are more preferable. Sorbitan (polysorbate 80), particularly preferably monooleic acid POE (20) sorbitan (polysorbate 80).

  When a surfactant is blended in the SCL ophthalmic composition of the present invention, the content of the surfactant can be appropriately set according to the type of surfactant, the type and amount of other components, and the like. As an example of the content ratio of the surfactant, the total amount of the surfactant is 0.001 to 1.0 w / v%, preferably 0.005 to 0.5 w / v with respect to the total amount of the ophthalmic composition for SCL. %, More preferably 0.01 to 0.5 w / v%, particularly preferably 0.05 to 0.5 w / v%.

  The ophthalmic composition for SCL of the present invention preferably further contains an isotonic agent. The isotonic agent that can be added to the ophthalmic composition for SCL of the present invention is not particularly limited as long as it is pharmaceutically, pharmacologically (pharmaceutically) or physiologically acceptable. Specific examples of such isotonic agents include, 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 , Glycerin, propylene glycol and the like. These isotonic agents may be used alone or in any combination of two or more.

  When an isotonic agent is added to the SCL ophthalmic composition of the present invention, the content of the tonicity agent varies depending on the type of tonicity agent used and cannot be uniformly defined. For example, with respect to the total amount of the ophthalmic composition for SCL, the total amount of the tonicity agent is 0.01 to 10 w / v%, preferably 0.05 to 5 w / v%, more preferably 0.1 to 2 w / The ratio of v% is exemplified.

  The pH of the ophthalmic composition for SCL of the present invention is not particularly limited as long as it is within a pharmaceutically, pharmacologically (pharmaceutically) or physiologically acceptable range. An example of the pH of the ophthalmic composition for SCL of the present invention is 4.0 to 9.5, preferably 5.0 to 8.5, and more preferably 5.5 to 8.0.

  Moreover, the osmotic pressure of the ophthalmic composition for SCL of the present invention is not particularly limited as long as it is within a range acceptable for a living body. As an example of the osmotic pressure ratio of the ophthalmic composition for SCL of the present invention, the range is preferably 0.7 to 5.0, more preferably 0.9 to 3.0, and particularly preferably 1.0 to 2.0. Can be mentioned. The osmotic pressure can be adjusted by a method known in the art using inorganic salts, polyhydric alcohols, sugar alcohols, saccharides and the like. The osmotic pressure ratio is the ratio of the osmotic pressure of the sample to the osmotic pressure of 0.9w / v% sodium chloride aqueous solution based on the 15th revised Japanese Pharmacopoeia. The osmotic pressure is the osmotic pressure measurement method described in the Japanese Pharmacopoeia (freezing point depression method) Measure with reference to. The standard solution for measuring the osmotic pressure ratio was sodium chloride (Japanese Pharmacopoeia standard reagent) dried at 500-650 ° C for 40-50 minutes, and then allowed to cool in a desiccator (silica gel). Dissolve in water to prepare exactly 100 mL, or use a commercially available standard solution for osmotic pressure ratio measurement (0.9 w / v% sodium chloride aqueous solution).

  In addition to the above components, an active ingredient (such as a pharmacologically active ingredient or a physiologically active ingredient) can be added to the ophthalmic composition for SCL of the present invention. The type of such component is not particularly limited, and examples thereof include a decongestant component, an eye 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 drug components or bactericidal components, saccharides, polymer compounds or derivatives thereof, cellulose or derivatives thereof, and local anesthetic components. Examples of the pharmacologically active component and physiologically active component suitable in the present invention include the following components.

  Decongestant: For example, α-adrenergic agonists, specifically epinephrine, epinephrine hydrochloride, ephedrine hydrochloride, oxymetazoline hydrochloride, tetrahydrozoline hydrochloride, naphazoline hydrochloride, phenylephrine hydrochloride, methylephedrine hydrochloride, epinephrine hydrogen tartrate, naphazoline nitrate. These may be d-form, l-form or dl-form.

  Ocular muscle modulator component: For example, cholinesterase inhibitor having an active center similar to acetylcholine, specifically, neostigmine methyl sulfate, tropicamide, helenien, atropine sulfate and the like.

  Anti-inflammatory component or astringent component: for example, zinc sulfate, zinc lactate, allantoin, epsilon-aminocaproic acid, indomethacin, lysozyme chloride, silver nitrate, pranoprofen, sodium azulenesulfonate, dipotassium glycyrrhizinate, diammonium glycyrrhizinate, Diclofenac sodium, bromfenac sodium, berberine chloride, berberine sulfate, etc.

  Antihistamine component or antiallergic component: for example, acitazanolast, diphenhydramine hydrochloride, chlorpheniramine maleate, ketotifen fumarate, levocabastine hydrochloride, amlexanox, ibudilast, tazanolast, tranilast, oxatomide, suplatast tosylate, sodium cromoglycate Pemirolast potassium etc.

  Vitamins: for example, retinol acetate, retinol palmitate, pyridoxine hydrochloride, flavin adenine dinucleotide sodium, pyridoxal phosphate, cyanocobalamin, panthenol, calcium pantothenate, sodium pantothenate, ascorbic acid, tocopherol acetate, tocopherol nicotinate, succinic acid Tocopherol, tocopherol calcium succinate, ubiquinone derivatives, etc.

  Amino acids: for example, aminoethylsulfonic acid (taurine), glutamic acid, creatinine, glutamic acid, sodium glutamate, magnesium glutamate, epsilon-aminocaproic acid, glycine, alanine, arginine, lysine, γ-aminobutyric acid, γ-aminovaleric acid, chondroitin Sodium sulfate etc. These may be d-form, l-form or dl-form.

  Antibacterial component or bactericidal component: for example, alkylpolyaminoethylglycine, chloramphenicol, sulfamethoxazole, sulfisoxazole, sulfamethoxazole sodium, sulfisoxazole diethanolamine, sulfisoxa Zole monoethanolamine, sodium sulfisomezole, sodium sulfisomidine, ofloxacin, norfloxacin, levofloxacin, lomefloxacin hydrochloride, acyclovir and the like.

  Sugars: For example, monosaccharides, disaccharides, specifically glucose, maltose, trehalose, sucrose, cyclodextrin, xylitol, sorbitol, mannitol and the like.

  Polymer compound or derivative thereof: for example, alginic acid, sodium alginate, dextrin, dextran, pectin, hyaluronic acid, chondroitin sulfate, polyvinyl alcohol (completely or partially saponified product), polyvinylpyrrolidone, polyacrylic acid, carboxyvinyl polymer, macrogol And pharmaceutically acceptable salts thereof.

  Cellulose or derivatives thereof: for example, ethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropylmethyl cellulose, methyl cellulose, carboxymethyl cellulose, carboxymethyl cellulose sodium, carboxyethyl cellulose, nitrocellulose and the like.

  Local anesthetic components: for example, chlorobutanol, procaine hydrochloride, lidocaine hydrochloride, etc.

  In the field of the ophthalmic composition for SCL, the blending ratio of various components is known, and the blending ratio of the above-described components in the ophthalmic composition for SCL of the present invention is the dosage form, pharmacologically active ingredient or It is set as appropriate according to the type of the physiologically active ingredient. For example, the blending ratio of the pharmacologically active ingredient or physiologically active ingredient can be selected from the range of about 0.0001 to 30% by weight, preferably about 0.001 to 10% by weight, based on the total amount of the ophthalmic composition for SCL.

  In addition, in the ophthalmic composition for SCL of the present invention, various components and additives are appropriately selected according to conventional methods according to the use and form as long as they do not impair the effects of the invention. The above can be used in combination. As those components or additives, for example, carriers (aqueous solvents, aqueous or oily bases, etc.) commonly used in the preparation of semi-solids and liquids, fragrances or refreshing agents, preservatives, fungicides or Various additives, such as an antibacterial agent, a pH adjuster, a chelating agent, and a stabilizer, can be mentioned.

  Although the typical component used for the ophthalmic composition for SCL of this invention is illustrated below, it is not limited to these.

  Carrier: An aqueous solvent such as water or hydrous ethanol.

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

  Preservatives, bactericides or antibacterials: for example, polydronium chloride, alkyldiaminoethylglycine hydrochloride, sodium benzoate, ethanol, benzalkonium chloride, benzethonium chloride, chlorhexidine gluconate, chlorobutanol, sorbic acid, potassium sorbate, dehydroacetic acid Sodium, methyl paraoxybenzoate, ethyl paraoxybenzoate, propyl paraoxybenzoate, butyl paraoxybenzoate, oxyquinoline sulfate, phenethyl alcohol, benzyl alcohol, biguanide compounds (specifically, polyhexamethylene biguanide or its hydrochloride) , Glow Kill (trade name, manufactured by Rhodia).

  pH adjuster: For example, hydrochloric acid, sodium hydroxide, potassium hydroxide, calcium hydroxide, magnesium hydroxide, triethanolamine, monoethanolamine, diisopropanolamine, sulfuric acid, phosphoric acid and the like.

  Chelating agent: for example, ascorbic acid, citric acid and the like.

  Stabilizers: for example, dibutylhydroxytoluene, trometamol, sodium formaldehyde sulfoxylate (Longalite), tocopherol, sodium pyrosulfite, monoethanolamine, aluminum monostearate, glyceryl monostearate and the like.

  The ophthalmic composition for SCL of the present invention is prepared by adding a desired amount of the above components (A) to (C) and, if necessary, other components to a desired concentration.

  The dosage form of the ophthalmic composition for SCL of the present invention is not particularly limited as long as it can be used in the ophthalmic field, and examples thereof include liquid and ointment. Among these, liquid is preferable. When the ophthalmic composition for SCL of the present invention is made into a liquid, pharmaceutically, pharmacologically (pharmaceutically) or physiologically acceptable water may be used as an aqueous carrier. Examples include distilled water, normal water, purified water, sterilized purified water, water for injection, distilled water for injection, and the like. These definitions are based on the 1st 5th Japanese Pharmacopoeia.

  Further, the ophthalmic composition for SCL of the present invention can be applied to eye drops that can be instilled while wearing SCL (eye drops for SCL), eye wash that can be washed while wearing SCL (eye drops for SCL), and SCL. Eye ointment (eye ointment for SCL), SCL mounting solution, SCL care agent (SCL disinfectant, SCL preservative, SCL cleaner, SCL cleaner preservative, SCL multipurpose solution, etc.) etc. Can be used. Among these, the eye drops for SCL, the eye wash for SCL, and the SCL mounting solution, in particular, the eye drops for SCL are suitable formulation forms of the ophthalmic composition for SCL of the present invention. In the present specification, when the notation is simply SCL, regardless of whether it is ionic or nonionic, and whether the water content is high or low water content, silicone hydrogel Regardless of whether they are contact lenses (hereinafter also referred to as SHCL) or non-silicone hydrogel contact lenses, all SCLs are included.

  Of the SCLs, the high water content SCL is a lens that is susceptible to oxygen permeability due to bacterial adhesion to the lens, etc., because oxygen permeability is ensured through the water contained in the lens. . In particular, since lenses of SCL classification group IV are relatively easily soiled, they are more easily affected and there is a strong demand for suppression of bacterial adhesion to the lenses. On the other hand, according to the ophthalmic composition for SCL of the present invention, since bacterial adhesion to the lens surface can be effectively suppressed, it also has an adverse effect on oxygen permeability even for lenses of SCL classification group IV. Applicable without any problem. In view of such advantages, examples of SCL that is a suitable application target of the ophthalmic composition for SCL of the present invention include high water content SCL, particularly lenses of SCL classification group IV.

  Here, the high water content lens is a contact lens having a water content of 50% or more. The ophthalmic composition for SCL of the present invention can be more suitably used for soft contact lenses having a water content of 55% or more.

  Here, the moisture content of SCL indicates the ratio of water in SCL, and is specifically determined by the following calculation formula.

Moisture content (%) = (weight of hydrated water / weight of SCL in hydrated state) x 100
Such moisture content can be measured by a gravimetric method according to the description of ISO18369-4: 2006.

  The ophthalmic composition for SCL of the present invention is useful for use in activating oocyte cells and supplying nutrition to the eye based on the component (A). In addition, the component (A) also has a buffering action, and thus is useful for stabilizing the ophthalmic composition for SCL. Further, the ophthalmic composition for SCL of the present invention is effective for preventing or treating dry eye and dry eyes based on the above component (C), and is also useful as an agent for improving dry eye and dry eyes.

2. Method for inhibiting bacterial adhesion to SCL, method for imparting bacterial adhesion inhibiting action to SCL Also, as described above, by using (C) component together with (A) and (B) components, Adhesion can be suppressed. Therefore, the present invention also provides methods of the following embodiments I and II from another viewpoint.
I. (A) at least one selected from the group consisting of aspartic acid and salts thereof, (B) a boric acid buffer, and (C) a monomer represented by the general formula (I) that can be used alone or in copolymerization A method for inhibiting bacterial adhesion to SCL, comprising contacting an SCL ophthalmic composition containing the monomer and polymerized polymer with SCL.
II. (C) a monomer represented by the general formula (I) in the ophthalmic composition for SCL containing at least one selected from the group consisting of aspartic acid and salts thereof and (B) a boric acid buffer A method for imparting an effect of inhibiting bacterial adhesion to SCL to the ophthalmic composition for SCL, which comprises blending a polymer obtained by polymerizing with other monomers capable of being alone or copolymerized.

  In these methods, the types and content ratios of the components (A) to (C) to be used, the types and content ratios of the other components, the formulation form of the ophthalmic composition for SCL, etc. are described in “1. .. Ophthalmic composition for SCL ".

Hereinafter, the present invention will be described in detail based on test examples, examples, and the like, but the present invention is not limited to these examples.
Reference Test Example 1: Bacterial adhesion inhibition test for SCL-1
About the adhesion of Pseudomonas aeruginosa (ATCC9027) (bacteria) to SCL (SCL classification: GLOF IV, main material: etafilconA, moisture content: 58%) using the test solution shown in Table 1 (Comparative Example 1-2) evaluated.

Each lens was immersed in 5 mL of sterile physiological saline overnight (lens pretreatment). 1 mL of each test solution was placed in a 24-well multiplate, and one lens was placed in each. As a control, physiological saline was used (n = 5). After 24 hours, lightly blot each lens with a non-woven fabric and place it in a 6-well multiplate containing 5 mL of 10 ^6-7 CFU / mL Pseudomonas aeruginosa bacterial solution (suspended in physiological saline) for 30 minutes. Stored at room temperature. Next, each lens was placed in a 6-well plate containing 5 mL of physiological saline with tweezers and shaken for 1 minute. Transfer the lens to a Spitz tube containing 5 mL of new physiological saline, apply ultrasonic waves (38 kHz) for 3 minutes, and then stir with a test tube mixer for 1 minute to remove the bacteria attached to each SCL and attach the bacteria. Liquid.

  The obtained adherent bacterial solution was diluted to an appropriate concentration for measurement, seeded on soybean / casein / digest / agar medium (SCDLP agar medium), and observed after overnight culture at 33 ° C. The number of colonies was counted, and the number of bacteria attached to each lens (viable cell count) was determined by correcting with the dilution factor. The number of attached bacteria when the test solution of Comparative Example 1 was used was calculated as 100%, and the relative value of the number of attached bacteria of each test solution was calculated as the bacterial adhesion rate (%).

  The results are shown in FIG. Compared with the case where the borate buffer was included alone (Comparative Example 1), the case where the borate buffer and the MPC polymer were included (Comparative Example 2), the bacterial adhesion rate was equal to or higher than that. That is, the effect of inhibiting bacterial adhesion by adding the MPC polymer to the borate buffer was not observed.

Test Example 1: Suppression test for bacterial adhesion to SCL-2
Using the test solutions shown in Table 2 (Examples 1-3 and Comparative Examples 3-9), bacteria adherence to SCL (SCL classification: GLOVE IV, main material: etafilcon A, moisture content: 58%) Evaluation was performed in the same manner as in Reference Test Example 1 above. The bacterial adherence rate (%) of each test solution is calculated as the bacterial adherence rate (%), where the number of adherent bacteria when the test solution of Comparative Example 3 is used is 100%, did.

  The results are shown in FIG. In comparison with the case of containing the borate buffer alone (Comparative Example 3), the bacterial adhesion rate was significantly increased in the case of containing the borate buffer and potassium aspartate (Comparative Example 8). On the other hand, when the MPC polymer was included in addition to the borate buffer and potassium aspartate (Example 1), the bacterial adhesion rate was significantly reduced.

  Moreover, in the case of containing boric acid, potassium aspartate, and sodium edetate (Comparative Example 9), the bacterial adhesion rate was further increased more than Comparative Example 8. On the other hand, when the MPC polymer is contained in addition to boric acid, potassium aspartate and sodium edetate (Example 2), the bacterium is reduced to a value lower than that when the boric acid buffer is contained alone (Comparative Example 3). The adhesion rate was significantly reduced. Similarly, even when polysorbate 80 was used instead of edetic acid (Example 3), the bacterial adhesion rate was significantly reduced to a value lower than that when the boric acid buffer was included alone (Comparative Example 3). .

Moreover, even if it converts the result of FIG. 2 into the suppression rate of the number of adhesion bacteria by MPC polymer, the adhesion rate suppression number of the comparative example 2 with respect to the above-mentioned comparative example 1 is -23.7% (it is not suppressing). Thus, it is clear that the adherent cell number inhibition rate of Example 1 with respect to Comparative Example 8 is 68.6%, and the adherent cell number inhibition rate of Example 2 with respect to Comparative Example 9 is 79.7%, which is a very good value. . The adhesion bacterial count suppression rate was calculated by the following formula.
Adherent bacteria count inhibition rate (%) = [1- (Test solution containing MPC polymer (Comparative Example 2, Example 1 or 2) / Test solution containing no MPC polymer (Comparative Example 1, 8 or 9) ) Number of attached bacteria)] × 100

  In addition, when it replaced with potassium aspartate and the same test was implemented using components, such as a pyridoxine hydrochloride and chlorpheniramine maleate, the increase in the bacterial adhesion rate like the case of potassium aspartate was not seen.

Test Example 2: Bacterial adhesion inhibition test for SCL-3
Using the test solutions shown in Table 3 (Example 4 and Comparative Example 10-11), the above-mentioned reference was made regarding the adherence of bacteria to SCL (SCL classification: Gruof IV, main material: etafilconA, moisture content: 58%). Evaluation was performed in the same manner as in Test Example 1. The bacterial adherence rate (%) of each test solution is calculated as the bacterial adherence rate (%) with the number of adherent bacteria in the case of using the test solution of Comparative Example 10 as 100% and the relative value of the number of adherent bacteria in each test solution. did.

  The results are shown in FIG. Even when a borate buffer, aspartic acid and potassium 0.1% were included (Comparative Example 11), the bacterial adhesion rate was significantly increased. On the other hand, when the MPC polymer was contained in addition to the boric acid buffer, aspartic acid and potassium (Example 4), the bacterial adhesion rate was significantly reduced.

Moreover, even if it converts the result of FIG. 3 into the suppression rate of the number of adherent bacteria by MPC polymer, the adherence number suppression rate of Example 4 with respect to the comparative example 11 has shown a very good value with 60.9%. Is clear. The adhesion bacterial count suppression rate was calculated by the following formula.
Adherent count suppression rate (%) = [1− (number of adherent bacteria in test liquid containing MPC polymer (Example 4) / number of adherent bacteria in test liquid not containing MPC polymer (Comparative Example 11))] × 100

Reference Test Example 2: Bacterial adhesion inhibition test for SCL-4
Using the test solution shown in Table 4 (Comparative Examples 12-15), the adhesion of bacteria to SCL (SCL classification: Grove IV, main material: etafilcon A, water content: 58%) Evaluation was made in the same manner. The bacterial adherence rate (%) of each test solution was calculated as a relative value (%) of the number of adherent bacteria of each test solution, assuming that the number of adherent bacteria when the test solution of Comparative Example 12 was used was 100%.

  The results are shown in FIG. Even when it contains potassium aspartate and a phosphate buffer (Comparative Example 14), when it contains a phosphate buffer alone (Comparative Example 12) and when it contains a phosphate buffer and MPC polymer (Comparative Example 13) In comparison, the bacterial adhesion rate was significantly increased. However, in the case where MPC polymer, phosphate buffer and potassium aspartate are contained (Comparative Example 15), the bacterial adhesion rate is increased as compared with Comparative Example 14, and the bacterial adhesion to the lens is inhibited by potassium aspartate. No effect was observed.

  From the above results, the bacterial adhesion inhibitory action to SCL realized by using MPC polymer is a specific action compared to the case of using a combination of aspartic acid and / or its salt and borate buffer. It became clear that there was.

Formulation Example In the formulation shown in Table 5, eye drops for SCL (Example 5-11), SCL wearing solution (Example 12), SCL eyewash (Example 13), and SCL multipurpose solution (Example) 14) is prepared. The MPC polymers blended in Examples 5-8 and 10-11 are the same as those used in Table 1. In addition, the MPC polymer blended in Example 9 was blended using the trade name “LIPIDURE-HM” (manufactured by NOF Corporation) so that the concentration of the MPC polymer was a prescribed amount.

Claims (4)

(A) at least one selected from the group consisting of aspartic acid and salts thereof;
(B) a borate buffer,
(C) a polymer obtained by polymerizing the monomer represented by the general formula (I) alone or with another monomer capable of copolymerization;

[Wherein, n1 is an integer of 2 to 4, R ₁ is a hydrogen atom or a methyl group, R ₂ is a group represented by — (R ₆ O) _n2 —R ₆ — (R ₆ has 1 to 4 carbon atoms] And n2 represents an integer of 0 to 5), and R _{3 to} R ₅ are the same or different and represent a hydrogen atom or an alkyl group having 1 to 4 carbon atoms. ]
An ophthalmic composition for soft contact lenses, comprising: The ophthalmic composition for soft contact lenses according to claim 1, which is an eye drop or a contact lens mounting liquid. The ophthalmic composition for soft contact lenses according to claim 1 or 2, which is used for silicon hydrogel contact lenses. The ophthalmic composition for soft contact lenses according to any one of claims 1 to 3, further comprising (D) at least one selected from the group consisting of ethylenediamineacetic acid, derivatives thereof, and salts thereof.

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