Ophthalmic composition

Abstract

To provide an ophthalmic solution for a contact lens, wherein, a contact lens treated with the ophthalmic solution is worn by a user, a tear film during wearing of the contact lens is stabilized, and a dry eye is suppressed and a good feeling in use is given.SOLUTION: The present invention provides an ophthalmic solution for a contact lens containing (A) at least one selected from the group consisting of a cellulose polymer compound, a vinyl polymer compound, polyethylene glycol and dextran, and (B) terpenoid.SELECTED DRAWING: None

Description

[Technical field]

[0001] The present invention relates to an ophthalmic composition for reducing the effects of contact lenses on the eye, More specifically, it is effective in stabilizing the tear film, especially the oil layer, and suppressing dryness when wearing contact lenses. The present invention also relates to a contact lens wetting solution - eye drops which are excellent in preventing the decline of visual function. [Background technology]

[0002] In recent years, contact lenses, especially soft contact lenses, have become popular for the purpose of vision correction and cosmetic purposes. (hereinafter sometimes referred to as SCL) has become remarkably popular. Although this varies from person to person, wearing eyeglasses places a strain on the eyes. Dry eyes are a typical complaint among contact lens wearers. The normal tear layer is a thin layer about 7 μm thick, and consists of three layers from the eyeball side: a mucus layer, an aqueous layer, and an oily layer. The cornea is made up of a structure that protects it from dryness and external stimuli. The oily layer prevents the tear film from evaporating, but the tear film becomes thin and unstable, and the oily layer also evaporates. It is easy for the tear film to thin, become uneven and unstable, and promote evaporation of tears, which leads to dry eyes and other problems. This causes dry eye symptoms. Furthermore, the tear film is destroyed (destabilized) and the oil layer becomes Dry spots occur on the surface of the tear film, which are extremely thin or absent. Dry spots were observed in some areas, but the time it took for dry spots to appear was longer than the tear film breakup time. Dry spots are used as a diagnostic criterion for dry eyes and dry eye syndrome, and are also used to calculate the BUT (Blind Spot Time). It is considered to be one of the important indicators for the standard (Non-Patent Document 1). It delays the onset of dry spots and suppresses the number and area of ​​dry spots from spreading even when the eyelid opening time is the same. If this becomes possible, it will lead to the suppression of dry eye symptoms such as dry eyes and tired eyes, which is an important is thought to have meaning.

[0003] In addition, even if the eye is healthy when wearing contact lenses, the tear layer becomes uneven. It is known that people who wear SCLs are more likely to experience dry eyes and dry eyes. In this case, the tear film on the SCL tends to be very thin, and the lipid layer is often very thin on the SCL. In some cases, the oil layer is either partially or entirely absent. This accelerates the evaporation of tears, which then spreads to the water in the SCL and even below the SCL. This can sometimes lead to dry eyes and corneal disorders (Non-Patent Document 2). Therefore, to ensure the safety of contact lens wearers' eyes, it is necessary to keep the tear fluid on the outer surface of the lens. There is a need for sustained and effective stabilization of formations, particularly oil formations.

[0004] In the past, methods such as applying artificial tears to the eyes have been used to treat dry eyes. The method of applying tear drops to the eyes was not effective enough because it was not possible to stabilize the tear film. Therefore, polyvinylpyrrolidone was adsorbed onto the surface of ionic contact lenses, A system that stabilizes the tear film around contact lenses by increasing the water retention of the lens surface. and contact lens eye drops and contact lens wetting solution for use therein have been proposed (Patent Document 1). In addition, long-chain alkyl derivatives of polysaccharides were used to promote and maintain the formation of the three-layer structure of the tear film. Ophthalmic liquid compositions for this purpose have also been proposed (Patent Document 2). The systems and compositions described above do not necessarily provide sufficient, sustained and efficient stability of the tear film, particularly the lipid layer. However, it could not be said that the effect of

[0005] Another problem associated with contact lens wear is the loss of contrast sensitivity. Contrast sensitivity is one of the visual function evaluation axes, and is the ability to distinguish subtle differences in brightness. When contrast sensitivity decreases, for example, while walking, Contrasts of obstacles are difficult to recognize, which can lead to accidents. The contrast between the ball and the background can be difficult to recognize, which can cause inconvenience. The causes of the decrease in the power of the eyes have traditionally been eye surgery such as corneal refractive surgery using excimer lasers, In addition to aging, wearing contact lenses was also known to be a cause. Loss of last sensitivity can occur when wearing bifocal contact lenses or soft contact lenses for a long period of time. There have been reports that it is related to the use of soft contact lenses and continuous wear. As a solution to these problems, there have been attempts to change the contact lenses themselves. However, there is nothing known about the improvement of contrast sensitivity by ophthalmic compositions.

[0006] By the way, ophthalmic solutions such as eye drops, eyewashes, and contact lens solutions are basically The purpose of contact lenses is different and they are treated separately. For example, users need to store contact lens solution and eye drops separately and use them appropriately. However, although these liquid preparations have different purposes (purposes), the dosage and other details are the same. In many cases, the appearance of the products is similar, and there is a risk of misuse. There was a risk that consumers would misuse the product due to misunderstandings about the time or mix-ups of products. The development of products that are easy to use and safe to use is widely demanded by users and sellers alike. was. [Prior art documents] [Patent documents]

[0007] [Patent Document 1] Patent Publication No. 2001-247466 [Patent Document 2] Patent Publication No. 2007-77053 [Non-patent literature]

[0008] [Non-Patent Document 1] New Ophthalmology 22(3):279-287,2005 [Non-Patent Document 2] New Ophthalmology 22(3):311-316,2005 Summary of the Invention [Problem to be solved by the invention]

[0009] As mentioned above, ophthalmic liquids such as eye drops and contact lens solutions were previously handled separately. The individual performance of these preparations was examined, but the eye drops and contact lens wear The suitability of the combination with the liquid has not been fully examined. The authors surprisingly found that contact lenses could be worn using conventional contact lens wearing solutions. When a separate prescription eye drop is applied after wearing the lenses, it has a sufficient effect of stabilizing the tear film and improving eye fatigue. Not only was there no improvement in contrast sensitivity observed, but the product also caused unpleasant sensations such as astringency and dryness. I found that it can even produce a sensation. Therefore, the present invention is a method for stabilizing the tear film during contact lens wear and suppressing dry eyes. This ophthalmic composition also eliminates eye fatigue and reduced contrast sensitivity, and is comfortable to use. The purpose is to provide goods. The present invention also provides an ophthalmic composition which is convenient, has no risk of misuse, and is highly safe. The purpose of this document is to Furthermore, the present invention provides an ophthalmic solution that is highly efficient and safe at every stage, from manufacturing to distribution and sales. The object of the present invention is to provide a composition for use. [Means for solving the problem]

[0010] As a result of intensive research to solve the problems, the present inventors have discovered that: A) a cellulose-based polymer compound, A vinyl polymer compound, a polyethylene glycol, a dextran, A contact lens wetting solution - eye drops comprising one or more of the above-mentioned compounds and B) a terpenoid. It has been found that this solves all of the above problems.

[0011] That is, the present invention is the invention described below. (1) (A) Cellulosic polymer compounds, vinyl polymer compounds, polyethylene glycol (B) one or more selected from the group consisting of terpenoids, dextran, and (C) terpenoids. A contact lens-wearing eye drop. (2) The contact lens according to (1), wherein the component (A) is a cellulose-based polymer compound. Eye drops for wearing. (3) The cellulose-based polymer compound is hydroxyethyl cellulose, hydroxypropyl cellulose, The compound according to (2), which is at least one selected from the group consisting of methylcellulose and salts thereof. The above-mentioned eye drops are for use with contact lenses. (4) (1) to (3) containing component (A) in a proportion of 0.0001 to 25 (w / v)%. 2. The wetting solution—eye drops for contact lenses according to claim 1 . (5) The contact lens according to any one of (1) to (4), wherein the terpenoid is menthol. Eye drops for contact lenses. (6) (B) component is contained in an amount of 0.0001 to 0.1 (w / v)%, (1) to (5 2. The wetting solution—eye drops for contact lenses according to any one of claims 1 to 11. (7) The composition according to any one of (1) to (6), further comprising (C) a nonionic surfactant. Eye drops for contact lenses. (8) (C) component is polyoxyethylene sorbitan fatty acid esters, polyoxyethylene The group consisting of hydrogenated castor oils and polyoxyethylene polyoxypropylene copolymers The wetting solution—eye drops for contact lenses according to (7), wherein the wetting solution is one or more selected from the following: (9) The contact lens according to (7) or (8), wherein the component (C) is polysorbate 80. Eye drops for contact lenses. (10) (7) to (9) containing component (C) in an amount of 0.001 to 5 (w / v) %. The wetting solution - eye drops for contact lenses according to any one of the preceding claims. (11) Any of (1) to (10) above, wherein the contact lenses are soft contact lenses. The wetting solution - eye drops for contact lenses described above. (12) Soft contact lenses are, in principle, soft contact lens classification group IV The wetting solution—eye drops for contact lenses according to (11), (13) The soft contact lenses are made of silicone hydrogel lens material. The wetting solution—eye drops for contact lenses according to (11), which is a contact lens. (14) The composition according to any one of items (1) to (13), which is for suppressing dry eyes or dry eye. Eye drops for use with tact lenses. (15) The composition according to any one of items (1) to (13), which is for improving eye fatigue or contrast sensitivity. Eye drops for contact lenses. Effect of the Invention

[0012] The contact lens wetting solution of the present invention is capable of improving the tear film while wearing contact lenses. It efficiently stabilizes the eyes and effectively prevents dry eyes, eye fatigue, and reduced contrast sensitivity. This can be done. The contact lens wetting solution of the present invention is also effective in preventing eye damage caused by contact lens wear. It also has a stress-reducing effect. For dry eyes and tired eyes when wearing contact lenses, corneal microscopy is used. It is believed that stress on the bleb is also involved, and the contact lens wetting solution of the present invention The improvement of dry eyes and tired eyes caused by contact lenses is accompanied by a reduction in the stress caused by wearing contact lenses. It is believed that there are. Moreover, the contact lens wetting solution of the present invention has a good feel when used, and is not like the conventional contact lenses. Since there is no need to prepare separate contact lens solution and eye drops, it is convenient and portable, and there is no risk of mistakes. There is no need to worry about its use and it is highly safe. Furthermore, it is possible to reduce costs at the manufacturing stage and transportation and display costs at the distribution stage. The advantages of the present invention include improved efficiency and improved safety in handling products at the sales stage. Contact lens wetting and eye drops contribute to reducing energy consumption and are therefore energy-saving. This is useful for reducing the amount of wastewater and also has the effect of reducing adverse effects on the environment. Thus, according to the present invention, it is possible to suppress dry eyes and improve eye fatigue while wearing contact lenses. It is highly effective in improving contrast sensitivity, is highly safe, and has excellent convenience. It also ensures safety and improves efficiency at all stages from manufacturing to sales. The present invention provides a contact lens-wearing eye drop solution that improves the convenience and safety of contact lens users and is easy to manufacture, transport, and use. This will make it possible to simultaneously achieve efficiency at each stage leading up to sales. [Brief description of the drawings]

[0013] [Figure 1] 1 is a graph showing the improving effect of the wetting solution—eye drops for contact lenses of the present invention on the decrease in contrast sensitivity during contact lens wear. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS

[0014] The present invention will be described in detail below. In this specification, the term "wearing" refers to the act (operation) of "putting contact lenses on the eye." The term "wearing" refers to the state in which the contact lens is "on the cornea." In this specification, unless otherwise specified, the expression "%" means w / v%, i.e., the amount dissolved in 100 mL of solution. This refers to the weight in grams of each component (solute) present.

[0015] In the present specification, the term "contact lens wetting solution" refers to a contact lens wetting solution. Functions both as a contact lens wetting solution and as an eye drop that can be applied while wearing contact lenses Furthermore, the wetting eye drop of the present invention has the same composition. The product is used as a contact lens insertion solution when the contact lens is inserted, and the contact lens is then inserted. The present invention is an ophthalmic composition that can be used as an eye drop for the eye in which the ophthalmic solution is worn. In the fine print, "contact lens wetting solution" is sometimes simply referred to as "wetting solution."

[0016] Additionally, the term "contact lenses" refers to hard, oxygen-permeable lenses unless otherwise specified. The term is used to encompass all types of contact lenses, including hard and soft. In addition, in this specification, the "soft contact lens classification" refers to the Pharmaceutical and Medical Devices Agency (Ministry of Health, Labor and Welfare at that time) Pharmaceutical and Medical Devices Agency (Medical and Medical Devices Agency) Notification of Director of the Inspection and Management Division "Soft Content Attached to the application for approval of manufacture (import) of disinfectants for tact lenses and soft contact lenses The classification method for soft contact lenses is stipulated in the "Handling of Materials to be Used" The classification of SCL is based on the "Act on the Use of Chemical Substances for the Prevention of Crude Oils and Chemical Substances of the Destruction of Natural Gases" and SCLs that belong to Group IV in this classification are those that contain water. The monomers that make up the raw material polymer have an anion ratio of 50% or more. The common property is that the mole percentage of is 1% or more. This classification follows the soft contact lens classification method established by the Food and Drug Administration.

[0017] In addition, "in principle" means that a person skilled in the art would consider the product to be equivalent to the product in question in terms of material, function, etc. The term "soft contact lenses" is intended to include soft contact lenses that can be understood as such.

[0018] Silicone hydrogel contact lenses are made of materials that contain silicone. A hydrophilic moiety is added to the material (e.g., TRIS or a TRIS derivative, which is a polymer of silicone and acrylate). Copolymerization of monomers (e.g., hydroxyethyl methacrylate, dimethylacrylamide, etc.) It is a contact lens made of a material that combines the two, and is called USAN (United State Adopted Name). Examples of names of materials based on this are LotrafilconA, LotrafilconB, BalafilconA, Galyf Examples include ilconA and SenofilconA.

[0019] The wetting solution—eye drops for contact lenses according to the present invention comprises: (A) a cellulose-based polymer compound; A vinyl polymer compound, a polyethylene glycol, and a dextran are selected from the group consisting of the vinyl polymer compound, the polyethylene glycol, and the dextran. and (B) one or more terpenoids. This stabilizes the tear film while wearing contact lenses, thereby preventing dry eyes. This is effective in reducing eye fatigue and improving contrast sensitivity, while at the same time improving usability. In addition, the present invention can be used as a contact lens wetting solution and as an eye drop solution. By using the same prescription of the invention, different liquid solutions are delivered to the cornea and the eye through the contact lens. Although the mechanism has not been fully elucidated, it is likely that the drug solution and the conjunctiva are not mixed together. Contact lens interactions with the eye and tears are minimized, resulting in a better tear film. It keeps the quality of your eyes stable, and is effective in reducing eye fatigue and improving contrast sensitivity. It is believed to have the aforementioned effects such as a good feeling when used.

[0020] The contact lens wetting solution of the present invention is a wetting solution containing a cellulose-based polymer compound, a vinyl-based polymer compound, One or more selected from the group consisting of aryl compounds, polyethylene glycol, and dextran (hereinafter, sometimes simply referred to as component (A)). As for cellulose-based polymer compounds, the hydroxyl groups of cellulose are replaced with other functional groups. The cellulose-based polymer compound obtained by the above-mentioned conversion imparts viscosity to the aqueous composition. The compound can be applied to contact lenses. The functional groups that substitute for the hydroxyl group of the hydroxyl group are methoxy, ethoxy, and hydroxymethyl groups. hydroxyl, hydroxyethoxy, hydroxypropoxy, carboxymethoxy, Examples of cellulose-based polymer compounds include methylcellulose, cellulose, ethyl cellulose, hydroxyethyl cellulose, hydroxymethyl cellulose, Hydroxypropyl cellulose, Hydroxypropyl methylcellulose, Carboxymethyl Examples of the binder include cellulose, carboxyethyl cellulose, and salts thereof. Here, the salt is preferably a pharmacologically acceptable salt, and among them, an alkali metal salt is more preferable. The cellulose-based cellulose used in the present invention is preferably a sodium salt or a potassium salt. There are no restrictions on the degree of substitution or molecular weight of the polymer compound, but for example, a weight average molecular weight of 0. 50,000 to 1,000,000, preferably 10,000 to 500,000, and more preferably 10,000 to 100,000 These cellulose-based polymer compounds can be used as commercially available products. These compounds may be used alone or in combination of two or more. Among these, from the viewpoint of further enhancing the effects of the present invention, methyl cellulose, hydroxypropyl cellulose, etc. are preferable. Hydroxyethylcellulose, Hydroxypropylmethylcellulose, Hydroxypropylcellulose One or more selected from the group consisting of cellulose, carboxymethylcellulose, and salts thereof More preferably, hydroxypropyl methylcellulose, hydroxyethyl cellulose, cellulose, sodium carboxymethylcellulose, and particularly preferably hydroxypropyl Methyl cellulose and hydroxyethyl cellulose.

[0021] Content of Cellulose-Based Polymer Compound in the Contact Lens Wetting Solution (Eye Drops) of the Present Invention is not limited because it depends on the type and molecular weight of the compound. The total amount of these compounds is usually 0.0001 to 25% of the total amount of the lens wetting solution. , preferably 0.001 to 10%, more preferably 0.001 to 7%, and further preferably 0 It is preferably 0.005 to 5%, and more preferably 0.01 to 1%.

[0022] As the vinyl polymer compound, a contact lens which can impart viscosity to the aqueous composition is used. Compounds applicable to the above-mentioned lenses can be used. Examples of vinyl polymer compounds are: and vinyl alcohol polymers such as polyvinyl alcohol (completely or partially saponified), Vinylpyrrolidone polymers such as polyvinylpyrrolidone, carboxyvinyl polymers, etc. There is no limitation on the molecular weight of the vinyl polymer compound used in the present invention. However, for example, the weight average molecular weight is 5,000 to 1,000,000, preferably 10,000 to 500,000, and more preferably In addition, vinyl-based polymers having a molecular weight of about 10,000 to 400,000 can be used. The compounds may be commercially available, and one or more of these compounds may be used in combination. Among them, from the viewpoint of further enhancing the effect of the present invention, preferably Polyvinylpyrrolidone K25, Polyvinylpyrrolidone K30, Polyvinylpyrrolidone K9 0, polyvinyl alcohol (partially saponified), and carboxyvinyl polymer are more preferred. Preferable are polyvinyl alcohol (partially saponified) and carboxyvinyl polymer. Particularly preferred is polyvinyl alcohol (partially saponified).

[0023] The content of the vinyl polymer compound in the contact lens wetting solution of the present invention is Although there are no limitations as it depends on the type and molecular weight of the compound, contact lenses are The total amount of these compounds is usually 0.001 to 25%, preferably 0.001 to 25%, based on the total amount of the eye drops for contact lenses. or 0.001 to 10%, more preferably 0.005 to 5%, and even more preferably 0.01 The content is preferably from 0.1 to 3%.

[0024] Dextran is a partially hydrolyzed polysaccharide produced by certain lactic acid bacteria using sucrose as a raw material. Dextran is a water-soluble polymer compound obtained by decomposition. 000,000, preferably 10,000 to 500,000, and more preferably 10,000 to 100,000. In addition, these dextrans can be commercially available and one or more kinds can be used. In particular, the effect of the present invention can be further enhanced by using a combination of two or more of them. From the viewpoint of enhancing the above-mentioned effect, dextran, dextran 70, dextran 40, and particularly Dextran 70 is preferred.

[0025] The content of dextran in the contact lens wetting solution of the present invention is The total amount of these components is usually 0.001 to 25% of the total amount of the contact lens eye drops, preferably is 0.001 to 10%, more preferably 0.01 to 10%, and even more preferably 0.01 to 5 %, particularly preferably 0.01 to 1%, and further particularly preferably 0.01 to 0.1%.

[0026] Polyethylene glycol is also known as macrogol, and is classified according to the degree of substitution and molecular weight of the substituent. There is no restriction, but the weight average molecular weight is 100 to 50,000, preferably 400 to 20,000, and more preferably The polyethylene glycol glycerides used are about 2,000 to 10,000. Coal can be commercially available and can be used alone or in combination of two or more types. Among them, from the viewpoint of further enhancing the effect of the present invention, macrogo is preferable. Macrogol 6000, Macrogol 4000, Macrogol 400, particularly preferably Macrogol The serum glucose level is 6000 and the macrogol level is 4000.

[0027] The content of polyethylene glycol in the contact lens wetting solution of the present invention is The total amount of these is usually 0.001 to 25% of the total amount of contact lens wetting solution. , preferably 0.001 to 10%, more preferably 0.01 to 10%, and even more preferably The content is preferably 0.05 to 5%, and more preferably 0.05 to 2%.

[0028] The component (A) in the present invention may be used alone or in combination of two or more. From the viewpoint of further enhancing the effects of the present invention, the preferred component (A) is a cellulose-based polymer. Compounds, particularly hydroxypropyl methylcellulose, hydroxyethyl cellulose, Loin is preferred. The content of the component (A) in the contact lens wetting solution - eye drops of the present invention is The total amount of these components is usually 0.0001 to 25%, preferably 0.0001 to 25%, based on the total amount of the lens wetting solution. is 0.001 to 10%, more preferably 0.005 to 10%, and even more preferably 0.01 The content is preferably from 0.01 to 5%.

[0029] The wetting solution—eye drops for contact lenses of the present invention further comprises a terpenoid (hereinafter, simply referred to as (B) component). (sometimes written as minutes). The terpenoids used in the contact lens wetting solution of the present invention include menthol, Menthol (l-menthol, dl-menthol, etc.), menthone, camphor (d-camphor, dl-camphor, etc.), flu, etc.), borneol (d-borneol, dl-borneol, etc.), geraniol , cineole, citral, linalool, anethole, limonene, eugenol, etc. These may be d-, l- or dl-isomers, but in order to enhance the effect of the present invention, From the viewpoint of enhancing the effect, l-menthol, d-camphor, dl-camphor, d-borneol, It is preferable to use dl-borneol and geraniol. Among them, l-menthol and d -camphor, dl-camphor, and geraniol are preferred, and l-mentho are more preferred. The terpenoids may also be used in the form of an essential oil, which is preferred. The essential oils are peppermint oil, eucalyptus oil, bergamot oil, fennel oil, These terpenoids are used alone or in combination with one or more other types. It can also be used in combination.

[0030] The content of terpenoid in the contact lens wetting solution of the present invention is In order to further enhance the effect, these are based on the total amount of contact lens wetting solution-eye drops. The total amount is usually preferably 0.0001 to 0.1%, more preferably 0.0001 to 0.07%. The content is more preferably 0.0005 to 0.05%, and particularly preferably 0.0005 to 0.01%. In addition, when using essential oils containing terpenoids as component (B), the blending ratio of said essential oils is set so that the terpenoid content in the blended essential oil satisfies the above ratio.

[0031] Furthermore, the contact lens wetting solution of the present invention may contain a suitable nonionic surfactant, if necessary. A surfactant (hereinafter, sometimes simply referred to as component (C)) may be contained. The nonionic surfactant used in the present invention is a surfactant that is generally known in the art for use in ophthalmology for contact lenses. Any compound that can be used in the composition can be used, for example, poloxamer 407, poloxamer 23 5. Polyoxyethylene-polyoxypropylene block copolymers such as Poloxamer 188 (hereinafter, also referred to as polyoxyethylene polyoxypropylene copolymer); POE-POP block copolymer adducts of ethylenediamine such as monolauryl Polysorbate 20, POE(20) sorbitan monooleate ( Polysorbate 80), POE Sorbitan Monostearate (Polysorbate 60), POE POE sorbitan fatty acid esters such as sorbitan tristearate (polysorbate 65) Polyethers; POE hydrogenated castor oil 5, POE hydrogenated castor oil 10, POE hydrogenated castor oil 20, PO POE hydrogenated castor oil 40, POE hydrogenated castor oil 50, POE hydrogenated castor oil 60, POE hydrogenated castor oil POE hydrogenated castor oils such as Oil 100; POE alkyl ethers such as POE (9) lauryl ether Ethers; POE(20)POP(4) Cetyl ether and other POE-POP alkyl ethers POE alkyl phenyl ethers such as POE(10) nonyl phenyl ether, etc. In addition, POE stands for polyoxyethylene, and POP stands for polyoxypropylene. The numbers in parentheses indicate the number of moles added. Among these, polyoxyethylene-polyoxypropylene block copolymers are preferred. POE sorbitan fatty acid esters or POE hydrogenated castor oils are particularly preferred. Examples include poloxamer 407, polysorbate 80, and POE hydrogenated castor oil 60.

[0032] The content of the nonionic surfactant in the contact lens wetting solution—eye drops of the present invention is It is difficult to define the exact amount because it depends on the type of surfactant, but it is recommended to use contact lenses. The total amount of these components is usually 0.001 to 5%, preferably 0.001 to 5%, based on the total amount of the ophthalmic solution to be applied. ~1.5%, more preferably 0.001 ~ 1%, even more preferably 0.005 ~ 0.5%, The content is particularly preferably 0.05 to 0.3%.

[0033] The contact lens wetting solution of the present invention may contain a suitable buffering agent as required. The buffer used in the present invention is preferably a borate buffer, a phosphate buffer, a carbonate buffer, or the like. Examples of buffers include citrate buffer, acetate buffer, HEPES buffer, and MOPS buffer. More specifically, boric acid, sodium borate, potassium tetraborate, borax, metaborate, Potassium phosphate, phosphoric acid, sodium hydrogen phosphate, sodium dihydrogen phosphate, dihydrogen phosphate Potassium, Carbonic acid, Sodium bicarbonate, Sodium carbonate, Citric acid, Sodium citrate , potassium citrate, acetic acid, sodium acetate, HEPES, MOPS and other compounds. and combinations of two or more compounds selected from this group.

[0034] Preferred buffers are borate buffers, phosphate buffers, carbonate buffers and citrate buffers. Particularly preferred buffers are borate buffers or phosphate buffers. More specifically, the borate buffer includes boric acid, alkali metal borate, and boric acid alumina. Borates such as alkaline earth metal salts and combinations of boric acid and borates are particularly preferred. As the phosphate buffer, phosphoric acid, alkali metal phosphate, phosphoric acid, borax, etc. are preferable. Phosphates such as alkaline earth metal salts of phosphoric acid, their hydrates, and combinations of phosphoric acid and phosphates. In particular, sodium hydrogen phosphate, sodium dihydrogen phosphate, and their hydrates are preferable.

[0035] The content of the buffer in the contact lens wetting solution of the present invention may vary depending on the type of buffer. It is difficult to define the amount in general because it varies depending on the amount of contact lens wetting solution. The total amount of these is usually 0.001 to 5%, preferably 0.001 to 3%, and more preferably Preferably, the content is 0.005 to 2.0%, more preferably 0.005 to 1.5%, and particularly preferably 0. .05~1.5%.

[0036] The contact lens wetting solution of the present invention may contain suitable inorganic salts as required. The inorganic salts are preferably potassium chloride, sodium chloride, sodium bicarbonate, These may be used alone or in combination of two or more. good. The content of inorganic salts in the contact lens wetting solution of the present invention is determined by the type of inorganic salt. Although it is difficult to define the amount in general because it varies depending on the type, the total amount of contact lens wetting solution is The total amount of these is usually 0.001 to 5%, preferably 0.01 to 1.5%, more preferably It is preferably used at 0.1 to 0.7%.

[0037] The contact lens wetting solution of the present invention may contain, if necessary, an appropriate ethylenediamine acetate. It is preferable to incorporate an ethylenediamine acetic acid derivative or a salt thereof. Examples of the salts thereof include edetic acid (ethylenediaminetetraacetic acid, EDTA), ethyl Diethylenediaminediacetic acid (EDDA), diethylenetriaminepentaacetic acid (DTPA), N-(2- Hydroxyethyl)ethylenediaminetriacetic acid (HEDTA) or its salts are examples. The salts of the ethylenediamine acetic acid derivatives are pharmacologically or physiologically acceptable salts. Contains, for example, salts with alkali metals (sodium, potassium, etc.), alkaline earth metals (ca Among them, ethylenediaminetetraacetic acid is preferable. or a salt thereof, such as calcium disodium ethylenediaminetetraacetate, ethylene Disodium diaminetetraacetate, disodium ethylenediaminetetraacetate dihydrate (hereinafter, Also called sodium edetate.) Disodium ethylenediaminetetraacetate is particularly preferred. These can be used alone or in combination of two or more. .

[0038] The ethylenediamine acetic acid derivative or The amount of salt contained varies depending on the molecular weight and type, so it cannot be specified in general terms. The total amount of these components is preferably 0.0001 to 1% of the total amount of the contact lens eye drops. More preferably, it is 0.0005 to 0.5%, further preferably, it is 0.001 to 0.3%, and particularly preferably, it is 0.0005 to 0.5%, The content is preferably 0.001 to 0.05%.

[0039] In order to further exert the effects of the present invention, an ethylenediamineacetic acid derivative or It is more preferable to combine salts, nonionic surfactants, inorganic salts, and buffers. stomach. The ethylenediamine acetic acid derivative or The content of salts, non-ionic surfactants, inorganic salts, and buffering agents is determined based on the contact lens wearer's specifications. The total amount of these is preferably 0.01 to 5% of the total amount of the eye drops, and particularly preferably 0. 05~3%.

[0040] The contact lens wetting solution of the present invention is suitable for contact lenses, particularly soft contact lenses. It is suitable for use with contact lenses. Soft contact lenses tend to feel dry. This is because it is said that it is difficult to drink and can easily strain the eyes. Soft contact lenses, especially soft contact lenses of the soft contact lens classification group IV Surprisingly, silicone hydrogel materials are also useful for contact lenses. In order to achieve a remarkable effect of the invention in soft contact lenses made of the material, Use in tact lenses is also preferred.

[0041] The contact lens wetting solution of the present invention contains various ingredients (pharmacologically active ingredients and physiologically active ingredients). The combination of the decongestant commonly used in ophthalmic compositions is suitable. component, ophthalmoregulatory component, anti-inflammatory component or astringent component, antihistamine component or antiallergic component Examples of the active ingredient include pharmaceutical ingredients, vitamins, amino acids, and local anesthetic ingredients. Examples of the components include the following:

[0042] Decongestant component: For example, α-adrenergic agonists, specifically epinephrine, epinephrine hydrochloride Nephrine, ephedrine hydrochloride, oxymetazoline hydrochloride, tetrahydrozoline hydrochloride, sodium hydrochloride Fazoline, phenylephrine hydrochloride, methylephedrine hydrochloride, epinephrine bitartrate, Naphazoline nitrate, etc. These may be in the d-, l- or dl-form. Ocular muscle regulating agent component: For example, cholinesterases having an active center similar to acetylcholine. enzyme inhibitors, specifically neostigmine methylsulfate, tropicamide, helenien sulfate Lopin et al.

[0043] Anti-inflammatory or astringent ingredients: For example, zinc sulfate, zinc lactate, allantoin, ipsilateral L-aminocaproic acid, indomethacin, lysozyme chloride, silver nitrate, pranoprofen , Sodium azulene sulfonate, Dipotassium glycyrrhizinate, Diclofenac sodium Berberine sulfate, bromfenac sodium, berberine chloride, etc.

[0044] Antihistamine or antiallergic ingredients: e.g., azadazanolast, amlexa Nox, ibudilast, tranilast, diphenhydramine hydrochloride, levocabastine hydrochloride, Ketotifen fumarate, sodium cromoglycate, pemirolast potassium, maleic acid Chlorpheniramine, etc.

[0045] Vitamins: e.g., retinol acetate, retinol palmitate, pyridoxine hydrochloride, Flavin adenine dinucleotide sodium, pyridoxal phosphate, cyanocobalamin , Panthenol, Calcium Pantothenate, Sodium Pantothenate, Ascorbic Acid, Tocopherol acetate, etc.

[0046] Amino acids: e.g. potassium aspartate, sodium aspartate, asparagine Magnesium and potassium phosphate, glutamic acid, monosodium glutamate, aminoethyl phosphate sulfonic acid, etc. Acid mucopolysaccharides: for example, sodium chondroitin sulfate.

[0047] Local anesthetic ingredients: e.g., chlorobutanol, oxybuprocaine hydrochloride, cocaine hydrochloride , cornecaine hydrochloride, dibucaine hydrochloride, tetracaine hydrochloride, parabutylaminobenzoic acid hydrochloride Diethylaminoethyl acetate, Piperocaine hydrochloride, Procaine hydrochloride, Proparacaine hydrochloride, Salt Hexothiocaine hydrochloride, lidocaine hydrochloride, etc.

[0048] In addition, the contact lens wetting solution of the present invention may contain other ingredients within the scope of the invention that does not impair the effects of the invention. Depending on the purpose and form of the product, various ingredients and additives are appropriately selected according to the usual method, and one or more The above may be contained. As these components or additives, for example, semi-solid agents, liquid agents, etc. Carriers commonly used in the preparation (e.g. water, aqueous solvents, aqueous or oily bases), thickeners , sugars, sugar alcohols, acidic mucopolysaccharides, surfactants, preservatives, bactericides or antibacterial agents, p Examples of additives include H regulators, isotonicity agents, and stabilizers.

[0049] Representative components used in the contact lens wetting solution of the present invention are listed below. , but not limited to these. Sugars: e.g. glucose, cyclodextrin, etc. Sugar alcohols: for example, xylitol, sorbitol, mannitol, etc. Acidic mucopolysaccharides: alginic acid, sodium alginate, etc. Surfactants: In addition to the nonionic surfactants listed above, alkyldiaminoethyl Glycine-type amphoteric surfactants such as alkyl glycine; alkyl quaternary ammonium salts (specifically , cationic surfactants such as benzalkonium chloride, benzethonium chloride, etc.

[0050] Preservatives, disinfectants or antibacterial agents: e.g., alkyldiaminoethylglycine hydrochloride, benzoic acid Sodium, ethanol, benzalkonium chloride, benzethonium chloride, chlorogluconate Hexidine, Chlorobutanol, Sorbic Acid, Potassium Sorbate, Sodium Dehydroacetate Sodium, methyl parahydroxybenzoate, ethyl parahydroxybenzoate, propranolol propyl, butyl paraoxybenzoate, oxyquinoline sulfate, phenethyl alcohol, benzoyl diethyl alcohol, biguanide compounds (specifically, polyhexamethylene biguanide or hydrochloride, polydonium chloride, Gloquil (trade name manufactured by Rhodia), etc.

[0051] pH adjusters: e.g., hydrochloric acid, boric acid, epsilon-aminocaproic acid, acetic acid, sodium hydroxide Thorium, Sodium Bicarbonate, Sodium Carbonate, Borax, Triethanolamine, Mono Ethanolamine, etc. Isotonicity agents: e.g. sodium bisulfite, sodium sulfite, magnesium chloride, vinegar Potassium acetate, sodium acetate, sodium thiosulfate, magnesium sulfate, glycerin, Propylene glycol, etc.

[0052] Stabilizers: Dibutylhydroxytoluene, trometamol, sodium formaldehyde Sulfoxylate (Rongalite), Tocopherol, Sodium Metabisulfite, Monoethoxyethanol Nolamine, aluminum monostearate, etc.

[0053] The contact lens wetting solution of the present invention has an initial viscosity appropriate for achieving the desired effect. The viscosity can be set and maintained stably for a long period of time. Ophthalmic composition for contact lenses When setting the viscosity of a material, maintain the viscosity at 20°C at 1.1 mPa s or more. It is preferable to design the viscosity so that the viscosity is generally 1.1 to 300 mPa·s, and preferably 1.3 to 10 The viscosity can be designed to be 0 mPa·s, and particularly preferably 1.5 to 80 mPa·s.

[0054] The viscosity is measured using a cone-plate type rotational viscometer (described in the 14th revised Japanese Pharmacopoeia). General Test Methods, 45. Viscosity Measurement Methods, Method 2 Rotational Viscometer Method, (3) Cone-plate Rotational Viscometer ") and, specifically, a commercially available cone-plate type rotational viscometer was used. For example, a commercially available E-type viscometer [Tokimec (TOKIMEC, sold by Toki Industries, Japan) and a rotor selected appropriately. Petroleum-based hydrocarbon oil (Newtonian fluid) specified by JIS Z8809 for each test sample measurement By preparing the standard solution for calibration, the viscosity at 20°C can be measured. Specifically, the viscosity was measured according to the method described in JP-A-2006-348055 (measurement conditions are described later). ).

[0055] The contact lens wetting solution of the present invention may be, if necessary, adjusted to a level within a range acceptable to the body. The osmotic pressure is adjusted to 0.3 as the osmotic pressure ratio to physiological saline. 0.4 to 4.1, preferably 0.3 to 2.1, and particularly preferably The osmotic pressure ratio is 0.5 to 1.4. The method for measuring the osmotic pressure ratio is based on the 15th revised Japanese Pharmacopoeia, General Test Method, Osmotic Pressure Ratio. Refer to the pressure measurement method.

[0056] The contact lens wetting solution of the present invention may be, if necessary, The pH is usually adjusted to 4.0 to 9.0, preferably 5.0 to 8.5. Particularly preferably, the pH is 5.5 to 8.5. The pH can be adjusted using the above-mentioned buffers, pH adjusters, etc. This can be done.

[0057] The wetting solution—eye drops for contact lenses of the present invention can be produced by a known method, and if necessary, Additional steps such as filtration sterilization and filling into containers can be added.

[0058] The method of using the contact lens wetting solution of the present invention is as follows: When putting on the contact lenses, apply contact lens eye drops directly onto the contact lenses. Wet both or one side of the contact lens with an appropriate amount (e.g., preferably 1 to 2 drops at a time). After that, wear the contact lenses. In addition, there is a method of using contact lenses as a While wearing contact lenses, apply an appropriate amount of contact lens wetting solution (for example, preferably 1 to 2 times at a time). (Drops) for use as eye drops.) (The above quotation marks may hereafter be referred to as "eye drop use.") There is no restriction on the number of times per day, but generally 1 to 10 times is sufficient. The number of times is preferably 1 to 6, and more preferably 5 to 6.

[0059] The method of using the contact lens wetting solution is particularly recommended as described above. As shown above, from using contact lens solution to the first application after wearing contact lenses. The interval is within 5 hours, preferably within 2 hours, more preferably within 1 hour, and even more preferably The time is preferably within 30 minutes, more preferably within 10 minutes, and even more preferably within 2 minutes. The administration of eye drops after this is similar to that of regular eye drops.

[0060] Further, the present invention includes the following contact lens treatment steps: When putting on contact lenses (just before putting them on), apply contact lens eye drops directly to the contact lenses. The solution is dropped onto the contact lens, and an appropriate amount is applied to both or one side of the contact lens (for example, preferably 1 to 2 drops at a time). 2. Wetting the contact lens with 2 drops of eye drops; 2. Putting the contact lens on the eye; 3. Contact lens A step of wetting the contact lens by instilling the solution into the eye while the contact lens is being worn. The following contact lens treatment steps may be included: 4. Removing the contact lens from the eye 4. Wetting the contact lenses by instilling the solution into the eyes when removing the contact lenses from the eyes (just before removing the contact lenses); 6. The process of removing contact lenses from the eyes. A process in which contact lens wetting solution is applied to the eye. An appropriate step may be selected from the above steps accordingly.

[0061] The wetting solution for contact lenses of the present invention is preferably Preferably, the liquid is used as a contact lens wetting solution and as an eye drop while wearing contact lenses. It is intended to be used for both, but can also be used for just one or the other. EXAMPLES

[0062] The present invention will be described in detail below based on test examples and examples. The examples are not intended to be limiting. In the test example, in order to keep the measurement conditions, especially the condition of the subjects, almost constant, The tests were carried out continuously for as long as possible. Each test example was carried out independently. The viscosity in each of the Examples and Comparative Examples was measured using a TVE-20L type viscometer, which is a type of E-type viscometer. A mould plate type (made by TOKIMEC, Toki Industries, Japan) was used. Measurements were performed under the following measurement conditions according to the manufacturer's instructions. The viscosity was measured according to the method described in 48055, except that the measurement conditions were as follows:

[0063] Measurement conditions: Rotation speed: 100 rpm (Note that the permissible range of rotation speed varies depending on the viscosity, so The measurement shall be performed at the highest possible rotation speed according to the requirements.) Sample volume: 1ml Measurement temperature: 20℃ Time: The viscosity after 3 minutes was recorded as the measured value.

[0064] Test 1: Evaluation using a dry eye observation device (DR-1, Kowa Co., Ltd.) (Test Method) According to the formulations in Table 1, the contact lens wetting solutions of Examples 1 to 6 and Comparative Examples 1 to 3 were The solution was prepared according to the usual method for preparing eye drops, etc., and placed in a polyethylene terephthalate container. The solution was filled into a container (capacity 10 mL) and sealed with a nozzle and cap. TRENZ is a brand name of soft contact lens group I (Si) manufactured by CIBA VISION. Lotrafilcon A) (hereinafter referred to as "SCL1") (Product name: Johnson & Johnson, soft contact lens classification group) PIV Main material: EtafilconA (hereinafter sometimes referred to as "SCL2") was used. Wet both sides of the contact lens with one drop of the contact lens solution, then insert the contact lens. The contact lenses were then placed on the subjects, and after 2 minutes, eye drops of the same prescription were instilled into the eyes. After that, the evaluation was carried out according to the test conditions (1) to (3). Three people who wear contact lenses on a daily basis and experience dryness (people with a tendency towards dry eyes) were selected. After testing with one test solution, the patient was given a sufficient rest before Tests were carried out with the following test solutions:

[0065] (1) Evaluation of dry spot area -1 Under the above conditions, the contact lens wetting solution is used as a contact lens wetting solution. After that, the solution was instilled into the eyes while the contact lenses were still in place, and then dry spots were examined under the following conditions. The number of samples was evaluated. To observe dry spots, we used a dry eye observation device (DR-1, (Kowa Co., Ltd.) was used. Specifically, the blinking time was 1 second after the start of blinking about 2 minutes after instillation. The number and size of dry spots on the ocular surface were measured. Analysis A: For each of the contact lens wetting solutions of Example 1, Comparative Examples 1 and 2, 3 The number of spots of each size was counted according to the type and size. Finally, the subtotals for each size were added together to determine the "Dragon" score for that prescription. The average "total dry spot score" for the three subjects is shown in Table 3. They were therefore evaluated and the results are shown in Table 4. Analysis B: In each of the contact lens wetting solutions of Examples 1 to 6 and Comparative Examples 1 to 2, each dry For the pots, the area values ​​were calculated from the images, and the sum of the area values ​​for each formulation was calculated as the total area. The results of the three subjects were then averaged, and the total area of ​​each example was calculated assuming that the total area of ​​Example 1 was 1. The relative value of the total area of ​​the formulation and the comparative formulation was calculated, and the "relative evaluation of the total area of ​​dry spots" was obtained. The results are shown in Table 5.

[0066] [Table 1]

[0067] [Table 2]

[0068] [Table 3]

[0069] [Table 4]

[0070] [Table 5] Dry spots are recognized in the ophthalmology field as an indicator of dry eyes and dry eyes. The occurrence time of dry spots is short, the number of dry spots is large, and the number of dry spots is large. It can be said that the eyes of people with dry eyes are more likely to be dry. In the case of the comparative formulation, the total area of ​​dry spots was significantly smaller than that of the comparative formulation. In the example prescription, the tear film on the contact lens surface was stabilized, making dry spots less likely to occur. This also indicates that eye dryness was significantly suppressed, and dry eye symptoms were This shows improvement in condition.

[0071] (2) Evaluation of dry spot area -2 Under the above conditions, the contact lens wetting solution is used as a contact lens wetting solution. After that, the solution was instilled into the eyes while the contact lenses were still in place, and then dry spots were examined under the following conditions. The area of ​​the to was evaluated. Using a dry eye observation device (DR-1), blinking was measured from the start of blinking to the next blink about 11 minutes after instillation. The area of ​​the largest dry spot observed during the period from the start of blinking to the start of blinking was analyzed using an image analyzer. The area ratio (%) of the ocular surface to the entire observation area was calculated. In the case of prescriptions, the dryness is particularly advanced and the dry spots are in the form of one dry area. The average of the total scores of the three subjects and the area ratio of each treatment when the area ratio of Example 1 is set to 1 are shown below. The relative value of the area rate of each was calculated, and the results were listed as "Evaluation of dry spot area-2" in Table 6. As shown in.

[0072] [Table 6] As mentioned above, the larger the dry spot, the drier the eye is. The results showed that the formulations used in the examples did not cause dry spots even after sufficient time had passed since application. The proportion of the surface area of ​​the contact lens is small, the tear film on the contact lens surface is stabilized, and dry eyes are prevented. This also indicates an improvement in dry eye symptoms.

[0073] (3) Evaluation of tear stability Under the above conditions, the contact lens wetting solution is used as a contact lens wetting solution. The solution was then instilled into the eyes while the contact lenses were still in place, and tear stability was evaluated under the following conditions: Evaluated. The movement of the tear lipid layer from the start of blinking to the start of the next blink approximately 3 minutes after instillation was observed in dry eyes. The eyes were observed using a DR-1 observation device and were scored according to the criteria shown in Table 7. The movement of the oil layer was also scored. The higher the score, the greater the oiliness of the tear layer. This indicates that the tear film is thin or uneven, making it unstable. The difference in the scores between the above was regarded as the degree of improvement in tear stability, and was evaluated according to the criteria shown in Table 8. The average evaluation scores are shown in Table 9.

[0074] [Table 7]

[0075] [Table 8]

[0076] [Table 9] From the test results, it was found that the lipid layer in the tear film was not easily disturbed and was stable in the formulation of the example. In the comparative formulation, the lipid layer in the tear film is easily disturbed, causing the tear film to become unstable. As mentioned above, when the lipid layer in the tear film becomes thinner, the evaporation of tears is promoted. It is known that the eyes become dry easily when using the formulation of the embodiment. Compared to the comparative formulation, the dry eye symptoms were significantly suppressed. It shows improvement in yippee symptoms.

[0077] Test 2: Evaluation of usability The following evaluation was carried out on 10 subjects. The contact lenses were applied to both sides of the eye using eye drops. After wetting the contact lenses with a drop of each solution, the contact lenses were put into the eyes. After 2 minutes of putting the contact lenses on, the same eye drops were applied to the contact lenses. After that, the participants were asked to rate their astringency, preference for coolness, and dryness in Table 1. The subjects were scored according to the evaluation criteria in Tables 11 and 12. The subjects' average was evaluated according to the criteria in Table 13. The results are shown in Table 14.

[0078] [Table 10]

[0079] [Table 11]

[0080] [Table 12]

[0081] [Table 13]

[0082] [Table 14] As a result of the test, the subjective symptoms of the example formulation were astringency (bitterness) and dryness. The taste was significantly suppressed, and the refreshing sensation was also highly preferred.

[0083] Test 3: Confirmation of the usefulness of the combination by prescription According to the prescriptions in Table 15, prescriptions 1 to 3 are eye drops, contact lens wetting solution, The contact lens wetting solution was prepared according to the usual preparation method for eye drops, etc. Fill into a polyethylene terephthalate container (capacity 10 mL) and apply with a nozzle and cap. The test methods were the same as those in Test 1 and Test 2, except where otherwise specified. A study was conducted to confirm the usefulness of the combination of the two methods. The results are shown in Table 16. Formulations 1 and 3 are formulations of the ophthalmic composition of the present invention. Specifically, Formulation 1 and Formulation 3 are Example 1, Formulation 3, and Example 4 in Table 1 are the same formulation. Comparative Example 3 has the same formulation.

[0084] [Table 15]

[0085] [Table 16]

[0086] When the formulation of the present invention was used as an ophthalmic solution, (Examples 1 and 2) showed different results from the present invention. When the formulation was used as an ophthalmic solution (Comparative Test Example 3), the results were better in the practical tests 1 and 2. The stability of the tear lipid layer was high, and the area of ​​dry spots was significantly smaller. Dry eyes were significantly suppressed. In addition, there was an excellent effect on the subjective symptoms of astringency and dryness. Moreover, it also showed excellent results in terms of preference for a refreshing sensation. Even if the composition is within the scope of the present invention, the composition of the eye drops to be applied is the same when applied and when applied to the eye. When the product was used on the same contact lenses or eyes (Examples 1 and 2), and when worn When comparing the cases where different compositions were used for instillation (Comparative Test Examples 4 and 5), showed a significantly superior effect.

[0087] Test 4: Evaluation of effect on improving eye fatigue (Test Method) A contact lens wetting solution with formulation 1 in Table 15 (same formulation as in Example 1) was used. The effect of improving eye fatigue was evaluated using the flicker value as an index of evaluation. Specifically, four subjects who wear contact lenses five or more days a week and are prone to eye fatigue were The subjects were asked to wear contact lenses for at least 8 hours throughout the day, and then the contact lenses were removed. The flicker value was measured while the device was being worn (pre-administration flicker value). The contact lenses used are: (1) Johnson & Johnson (Main material: Senofilcon A) Silicone hydrogel material) Soft contact lens classification group IV, (2) John Son & Johnson Main material: EtafilconA Soft contact lens classification group IV, (3) The contact lenses were oxygen-permeable hard contact lenses.

[0088] Next, wait a sufficient amount of time, remove the contact lenses from both eyes, and then replace the contact lenses in prescription 1. Apply the contact lens eye drops directly to the concave surface of one lens (the inner surface that comes into contact with the cornea). After applying one drop to each eye, the contact lenses were put back into both eyes and after 15 minutes, the prescription was One drop of the contact lens eye drops No. 1 was applied to each eye, and the flicker value (flicker value after administration) was measured. The Kerr value was measured (Example Test 3). On another day, the pre-administration flicker value was measured using the same procedure, and the subjects were then asked to keep wearing contact lenses. Apply one drop of prescription 1 eye drops to each eye, then apply prescription 1 eye drops to both eyes again 15 minutes later. One drop was instilled into each eye, and the flicker value (post-administration flicker value) was measured (Comparative Test Example 6). The flicker value improvement rate was calculated from the measured flicker value using the formula 1 described below.

[0089] The flicker value is the difference between the flicker frequency of the blinking light and the flicker level detected by the naked eye when the blinking frequency is gradually increased. The flicker value is the critical frequency at which blinking cannot be distinguished. It is possible to measure the deterioration of the perceptual function. fatigue (especially eye fatigue caused by physical or mental fatigue accompanied by a decrease in perceptual function) and eye strain This is an indicator of improvement in work. In this test, the flicker value was measured using the following device and conditions. Device name: Roken Digital Flicker Value Meter RDF-1 (manufactured by Shibata Scientific Co., Ltd.) Illuminance: Set to an illuminance that is easy for the person measuring to see. Distance: Set at a position that is easy for the person taking the measurement to see (the position where the letter "K" is most clearly visible). SCAN knob (initial flicker frequency to be lowered): 60Hz MANU-AUTO: Set to AUTO From the measured flicker value, the improvement value for eye fatigue (improvement of flicker value) was calculated using the following formula 1. (Good rate).

number

[0090] The average results of the four subjects are shown in Table 17. As a result, the actual results were good in all four subjects. In the test example 3, a remarkable increase in the improvement rate of the flicker value was observed compared to the comparative test example 6. In this industry, the standard for the improvement rate of flicker value is about 3%, and the effect (clear From the above results, it is considered that the presence or absence of the change in the concentration of the stimulant is generally judged. Contact lens eye drops are more effective than conventional eye drops when used only for instillation. , and has a remarkable effect in improving tired eyes, eye strain, and physical and mental fatigue. It was confirmed that the method is highly useful.

[0091] [Table 17]

[0092] Examples 7-11 Contact lens wetting solutions (Examples 7-11) were prepared according to the formulations shown in Table 18. In Table 18, the units of each compounding component are g / 100 mL. In the above-mentioned Tests 1 to 4, the same effects of the present invention as in Example 1 were observed. [Table 18]

[0093] Test 5: Evaluation of contrast sensitivity improvement effect (Test Method) The contact lens wetting solutions of Examples 1 to 11 in Tables 1 and 18 were used. The effect of improving contrast sensitivity was evaluated. Specifically, eight subjects who wear contact lenses five or more days a week were While wearing contact lenses, the Vision Contrast Test System (VCTS (registered trademark)) Contrast sensitivity was measured using a chart test (blank). Instructions attached to the VCTS Chart Examination Procedure, Vistech Cons The contrast sensitivity values ​​were calculated based on the Contrast Sensitivity The calculation was done from the sitivity Value Key table. The evaluation points are A (1.5cpd), B (3cpd), C (6cpd), and D. (12cpd), E (18cpd), and 5 points. First, using the contact lens wetting solution of Formulation 1 (Example 1) in Table 15, The contact lenses were then used as contact lens solution, and two minutes later, the contact lenses were still in place. The liquid was instilled into the eyes, and the contrast sensitivity was measured one minute later (Example 4 of Experimental Test). The contact lenses used by the patients were SCL1 (as mentioned above) for four patients and SCL2 for four patients.

[0094] The average results for the eight subjects are shown in Figure 1. As a result, the prescription was In Example 4, in which Example 1 was used as a contact lens wetting solution, the results were compared with the blank. , contrast sensitivity was significantly improved.

[0095] Similarly, the difference was greatest for the contact lens wetting solutions of Examples 2 to 11. Contrast sensitivity values ​​were measured at the B (3 cpd) point and the average results are shown in Table 19. The contact lenses used by the subjects were the aforementioned SCL1 for 10 subjects and SCL2 for 10 subjects. It was. [Table 19] As is clear from the above results, the contact lens wetting solutions of Examples 2 to 11 were used As in Example 1, the contrast sensitivity was significantly improved compared to the blank. there was.

[0096] Prescription Example 1-10 A contact lens wetting solution (Formulation Example 1-10) was prepared according to the formulation shown in Table 20. In Table 20, the units of each ingredient are g / 100 mL. [Table 20-1]

[0097] [Table 20-2] [Industrial Applicability]

[0098] The ophthalmic composition of the present invention stabilizes the tear film during contact lens wear and relieves dry eyes. It is easy to use, convenient, and has no risk of misuse. Its high efficiency makes it highly valuable for industrial use.

Claims

[Claim 1] The invention described in the specification.

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