Ophthalmic composition
A high-concentration ophthalmic composition with chondroitin sulfate, castor oil, sesame oil, or liquid paraffin, and a nonionic surfactant effectively removes proteins from contact lenses, addressing the lack of study on high-concentration compositions.
Patent Information
- Application Number
- JP2025097663
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2019-11-07
- Filing Date
- 2025-06-11
- Publication Date
- 2025-08-26
AI Technical Summary
Ophthalmic compositions containing high concentrations of chondroitin sulfate or its salts have not been extensively studied, limiting their effectiveness in removing proteins adhering to contact lenses.
An ophthalmic composition comprising chondroitin sulfate or its salts, combined with castor oil, sesame oil, or liquid paraffin, and a nonionic surfactant, with a concentration of chondroitin sulfate at 0.7 w/v% or more, effectively cleans proteins from contact lenses.
The composition significantly cleans proteins adhering to contact lenses, providing a novel and effective solution for lens hygiene.
Smart Images

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Abstract
Description
[Technical Field]
[0001] The present invention relates to ophthalmic compositions. [Background technology]
[0002] Chondroitin sulfate or a salt thereof is incorporated into ophthalmic compositions for the purposes of promoting energy metabolism, relieving eye fatigue by promoting metabolism and cellular respiration, and replenishing tear components (e.g., Patent Document 1). [Prior art documents] [Patent documents]
[0003] [Patent Document 1] Japanese Patent Application Laid-Open No. 2011-148791 Summary of the Invention [Problem to be solved by the invention]
[0004] While ophthalmic compositions containing low concentrations (e.g., less than 0.5 w / v%) of chondroitin sulfate or its salts have been relatively well studied, ophthalmic compositions containing high concentrations (e.g., 0.7 w / v% or more, preferably 1.0 w / v% or more) of chondroitin sulfate or its salts have not been studied much.
[0005] An object of the present invention is to provide a novel ophthalmic composition containing chondroitin sulfate or a salt thereof at a high concentration. [Means for solving the problem]
[0006] The present inventors have found that by incorporating a high concentration of chondroitin sulfate and its salts into an ophthalmic composition containing an oily component such as castor oil, sesame oil, or liquid paraffin and a nonionic surfactant, proteins adhering to contact lenses can be remarkably removed. The present invention is based on this finding and provides the following inventions.
[0007] [1] An ophthalmic composition comprising (A) at least one selected from the group consisting of chondroitin sulfate and its salts, (B) at least one selected from the group consisting of (B-1) castor oil, (B-2) sesame oil, and (B-3) liquid paraffin, and (C) a nonionic surfactant, wherein the content of component (A) is 0.7 w / v% or more based on the total amount of the ophthalmic composition. [2] The ophthalmic composition according to [1], wherein the content of component (A) is 1.0 w / v% or more based on the total amount of the ophthalmic composition. [3] The ophthalmic composition according to [1], wherein the content of component (A) is 3.0 w / v% or more based on the total amount of the ophthalmic composition. [4] The ophthalmic composition according to any one of [1] to [3], further comprising (D) a buffering agent. [5] The ophthalmic composition according to any one of [1] to [4], which is for use in contact lenses. [Effects of the Invention]
[0008] According to the present invention, an ophthalmic composition containing a high concentration of chondroitin sulfate or a salt thereof and capable of significantly cleaning proteins adhering to contact lenses can be provided. DETAILED DESCRIPTION OF THE INVENTION
[0009] DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS The following describes in detail the embodiments of the present invention, but the present invention is not limited to the following embodiments.
[0010] In this specification, unless otherwise specified, the unit of content "%" means "w / v%" and is synonymous with "g / 100 mL".
[0011] [1. Ophthalmic composition] The ophthalmic composition according to this embodiment contains at least one selected from the group consisting of chondroitin sulfate and salts thereof (also simply referred to as "component (A)").
[0012] [Component (A)] The ophthalmic composition according to this embodiment contains (A) at least one selected from the group consisting of chondroitin sulfate and salts thereof (also simply referred to as "component (A)").
[0013] Chondroitin sulfate and its salts, which are component (A), are not particularly limited as long as they are pharmaceutically, pharmacologically (pharmaceutical), or physiologically acceptable. The molecular weight of chondroitin sulfate and its salts is not particularly limited as long as they are pharmaceutically, pharmacologically (pharmaceutical), or physiologically acceptable, but typically, those with a weight-average molecular weight of about 1,000 to 100,000, preferably about 5,000 to 50,000, and more preferably about 10,000 to 40,000 can be used.
[0014] Examples of salts of chondroitin sulfate include alkali metal salts and alkaline earth metal salts. Examples of alkali metal salts include sodium salt and potassium salt. Examples of alkaline earth metal salts include magnesium salt and calcium salt.
[0015] As chondroitin sulfate and salts thereof, chondroitin sulfate and alkali metal salts of chondroitin sulfate are preferred, chondroitin sulfate and sodium chondroitin sulfate are more preferred, and sodium chondroitin sulfate is even more preferred.
[0016] Chondroitin sulfate and salts thereof may be commercially available. One type of chondroitin sulfate and salts thereof may be used alone, or two or more types may be used in combination.
[0017] The content of component (A) in the ophthalmic composition according to this embodiment is 0.7 w / v% or more, based on the total amount of the ophthalmic composition. The lower limit of the content of component (A) is not particularly limited as long as it is 0.7 w / v% or more, and is set appropriately depending on the type of component (A), the types and amounts of other components added, the intended use and formulation of the ophthalmic composition, etc. From the viewpoint of more significantly achieving the effects of the present invention, the lower limit of the content of component (A) is, for example, preferably 0.7 w / v% or more, more preferably 1.0 w / v% or more, even more preferably 2.0 w / v% or more, even more preferably 2.5 w / v% or more, and particularly preferably 3.0 w / v% or more. The upper limit of the content of component (A) is not particularly limited, and is set appropriately depending on the type of component (A), the types and amounts of other components added, the intended use and formulation of the ophthalmic composition, etc. The upper limit of the content of component (A) is, for example, preferably 5.0 w / v% or less, more preferably 4.0 w / v% or less, even more preferably 3.5 w / v% or less, and even more preferably 3.0 w / v% or less, from the viewpoint of more pronounced effects of the present invention and the feeling when used. The content of component (A) in the ophthalmic composition according to this embodiment may be, for example, 0.7 to 5.0 w / v%, 0.7 to 4.0 w / v%, 0.7 to 3.5 w / v%, 0.7 to 3.0 w / v%, 0.7 to 1.5 w / v%, 0.7 to 1.0 w / v%, 1.0 to 5.0 w / v%, 1.0 to 4.0 w / v%, 1.0 to 3.5 w / v%, 1.0 to 3.0 w / v%, 2.0 to 5.0 w / v%, 2.0 to 4.0 w / v%, 2.0 to 3.5 w / v%, 2.0 to 3.0 w / v%, 2.5 to 5.0 w / v%, 2.5 to 4.0 w / v%, 2.5 to 3.5 w / v%, or 2.5 to 3.0 w / v%, based on the total amount of the ophthalmic composition. In another aspect, the content of component (A) in the ophthalmic composition of this embodiment may be, for example, 1.0 w / v%, 2.0 w / v%, or 3.0 w / v%, based on the total amount of the ophthalmic composition.
[0018] [(B) component] In addition to component (A), the ophthalmic composition according to this embodiment further contains at least one selected from the group consisting of (B)(B-1) castor oil (also simply referred to as "component (B-1)"), (B-2) sesame oil (also simply referred to as "component (B-2)"), and (B-3) liquid paraffin (hereinafter, components (B-1), (B-2), and (B-3) are collectively referred to as "component (B)"). One component (B) may be used alone, or two or more components may be used in combination.
[0019] The content of component (B) in the ophthalmic composition according to this embodiment is not particularly limited and is set appropriately depending on the types and contents of other blended components, the intended use of the ophthalmic composition, the formulation form, etc. From the viewpoint of more significantly exhibiting the effects of the present invention, the content of component (B) is, for example, preferably 0.0001 to 5 w / v%, more preferably 0.001 to 1 w / v%, even more preferably 0.003 to 0.5 w / v%, and even more preferably 0.005 to 0.1 w / v%, based on the total amount of the ophthalmic composition.
[0020] The content ratio of component (B) relative to component (A) in the ophthalmic composition according to this embodiment is not particularly limited and is set appropriately depending on the type of component (A), the types and contents of other blended components, the intended use and formulation of the ophthalmic composition, etc. From the viewpoint of further enhancing the effects of the present invention, the content ratio of component (B) relative to component (A) is, for example, preferably 0.0001 to 5 parts by mass, more preferably 0.0005 to 2.5 parts by mass, even more preferably 0.001 to 1 part by mass, even more preferably 0.005 to 0.5 parts by mass, particularly preferably 0.01 to 0.1 parts by mass, and particularly more preferably 0.01 to 0.05 parts by mass, relative to 1 part by mass of the total content of component (A) contained in the ophthalmic composition according to this embodiment.
[0021] [(B-1) component] There are no particular limitations on the castor oil used as component (B-1), so long as it is medicamentally, pharmacologically (pharmaceutical) or physiologically acceptable.
[0022] The content of component (B-1) in the ophthalmic composition according to this embodiment is not particularly limited and is set appropriately depending on the types and contents of other blended components, the intended use of the ophthalmic composition, the formulation, etc. From the viewpoint of more significantly exhibiting the effects of the present invention, the content of component (B-1) is, for example, preferably 0.0001 to 5 w / v%, more preferably 0.001 to 1 w / v%, even more preferably 0.003 to 0.5 w / v%, and even more preferably 0.005 to 0.1 w / v%, based on the total amount of the ophthalmic composition.
[0023] The content ratio of component (B-1) relative to component (A) in the ophthalmic composition according to this embodiment is not particularly limited and is set appropriately depending on the type of component (A), the types and contents of other blended components, the intended use and formulation of the ophthalmic composition, etc. From the viewpoint of further enhancing the effects of the present invention, the content ratio of component (B-1) relative to component (A) is, for example, preferably 0.0001 to 5 parts by mass, more preferably 0.0005 to 2.5 parts by mass, even more preferably 0.001 to 1 part by mass, even more preferably 0.005 to 0.5 parts by mass, particularly preferably 0.01 to 0.1 parts by mass, and particularly more preferably 0.01 to 0.05 parts by mass, relative to 1 part by mass of the total content of component (A) contained in the ophthalmic composition according to this embodiment.
[0024] [(B-2) component] The sesame oil used as component (B-2) is not particularly limited as long as it is medicamentarily, pharmacologically (pharmaceutical) or physiologically acceptable.
[0025] The content of component (B-2) in the ophthalmic composition according to this embodiment is not particularly limited and is set appropriately depending on the types and contents of other blended components, the intended use of the ophthalmic composition, the formulation, etc. From the viewpoint of more significantly exhibiting the effects of the present invention, the content of component (B-2) is, for example, preferably 0.0001 to 5 w / v%, more preferably 0.001 to 1 w / v%, even more preferably 0.003 to 0.5 w / v%, and even more preferably 0.005 to 0.1 w / v%, based on the total amount of the ophthalmic composition.
[0026] The content ratio of component (B-2) relative to component (A) in the ophthalmic composition according to this embodiment is not particularly limited and is set appropriately depending on the type of component (A), the types and contents of other blended components, the intended use and formulation of the ophthalmic composition, etc. From the viewpoint of further enhancing the effects of the present invention, the content ratio of component (B-2) relative to component (A) is, for example, preferably 0.0001 to 5 parts by mass, more preferably 0.0005 to 2.5 parts by mass, even more preferably 0.001 to 1 part by mass, even more preferably 0.005 to 0.5 parts by mass, particularly preferably 0.01 to 0.1 parts by mass, and particularly more preferably 0.01 to 0.05 parts by mass, relative to 1 part by mass of the total content of component (A) contained in the ophthalmic composition according to this embodiment.
[0027] [(B-3) component] The liquid paraffin of component (B-3) is not particularly limited as long as it is medicamentarily, pharmacologically (pharmaceutical), or physiologically acceptable. Examples of liquid paraffin include liquid paraffin and light liquid paraffin, and among these, liquid paraffin is preferred.
[0028] The content of component (B-3) in the ophthalmic composition according to this embodiment is not particularly limited and is set appropriately depending on the types and contents of other blended components, the intended use of the ophthalmic composition, the formulation, etc. From the viewpoint of more significantly exhibiting the effects of the present invention, the content of component (B-3) is, for example, preferably 0.0001 to 5 w / v%, more preferably 0.001 to 1 w / v%, even more preferably 0.003 to 0.5 w / v%, and even more preferably 0.005 to 0.1 w / v%, based on the total amount of the ophthalmic composition.
[0029] The content ratio of component (B-3) relative to component (A) in the ophthalmic composition according to this embodiment is not particularly limited and is set appropriately depending on the type of component (A), the types and contents of other blended components, the intended use and formulation of the ophthalmic composition, etc. From the viewpoint of further enhancing the effects of the present invention, the content ratio of component (B-3) relative to component (A) is, for example, preferably 0.0001 to 5 parts by mass, more preferably 0.0005 to 2.5 parts by mass, even more preferably 0.001 to 1 part by mass, even more preferably 0.005 to 0.5 parts by mass, particularly preferably 0.01 to 0.1 parts by mass, and particularly more preferably 0.01 to 0.05 parts by mass, relative to 1 part by mass of the total content of component (A) contained in the ophthalmic composition according to this embodiment.
[0030] [(C) component] The ophthalmic composition according to this embodiment further contains, in addition to the components (A) and (B), a nonionic surfactant (C) (also referred to simply as "component (C)"). One type of component (C) may be used alone, or two or more types may be used in combination.
[0031] The nonionic surfactant serving as component (C) is not particularly limited as long as it is medicamentarily, pharmacologically (pharmaceutical) or physiologically acceptable.
[0032] Examples of nonionic surfactants include polyoxyethylene (20) sorbitan monolaurate (polysorbate 20), polyoxyethylene (20) sorbitan monopalmitate (polysorbate 40), polyoxyethylene (20) sorbitan monostearate (polysorbate 60), polyoxyethylene (20) sorbitan tristearate (polysorbate 65), and polyoxyethylene (20) sorbitan monooleate (polysorbate 80). ), polyoxyethylene sorbitan fatty acid esters such as polyoxyethylene (5) hydrogenated castor oil (polyoxyethylene hydrogenated castor oil 5), polyoxyethylene (10) hydrogenated castor oil (polyoxyethylene hydrogenated castor oil 10), polyoxyethylene (20) hydrogenated castor oil (polyoxyethylene hydrogenated castor oil 20), polyoxyethylene (30) hydrogenated castor oil (polyoxyethylene hydrogenated castor oil 30), polyoxyethylene (40) hydrogenated castor oil (polyoxyethylene hydrogenated castor oil Polyoxyethylene hydrogenated castor oils such as polyoxyethylene (60) hydrogenated castor oil (polyoxyethylene hydrogenated castor oil 60), polyoxyethylene (80) hydrogenated castor oil (polyoxyethylene hydrogenated castor oil 80), and polyoxyethylene (100) hydrogenated castor oil (polyoxyethylene hydrogenated castor oil 100); polyoxyethylene castor oils such as polyoxyethylene (3) castor oil (polyoxyethylene castor oil 3), polyoxyethylene (10) castor oil (polyoxyethylene castor oil 10), polyoxyethylene (35) castor oil (polyoxyethylene castor oil 35), and polyoxyethylene (70) castor oil (polyoxyethylene castor oil 70); polyoxyethylene alkyl ethers such as polyoxyethylene (9) lauryl ether; polyoxyethylene-polyoxypropylene alkyl ethers such as polyoxyethylene (20) polyoxypropylene (4) cetyl ether;Polyoxyethylene (20) polyoxypropylene (20) glycol (Pluronic L44), polyoxyethylene (42) polyoxypropylene (67) glycol (Poloxamer 403, Pluronic P123), polyoxyethylene (54) polyoxypropylene (39) glycol (Poloxamer 235, Pluronic P85), polyoxyethylene (120) polyoxypropylene (40) glycol (Pluronic F87), polyoxyethylene (160) poly Examples include polyoxyethylene-polyoxypropylene glycols such as oxypropylene (30) glycol (Poloxamer 188, Pluronic F68), polyoxyethylene (196) polyoxypropylene (67) glycol (Poloxamer 407, Pluronic F127), and polyoxyethylene (200) polyoxypropylene (70) glycol; and polyethylene glycol monostearates such as polyoxyl 10 stearate and polyoxyl 40 stearate. In the compounds exemplified above, the numbers in parentheses indicate the number of moles added.
[0033] Preferred nonionic surfactants are polyoxyethylene sorbitan fatty acid esters, polyoxyethylene hydrogenated castor oil, polyoxyethylene castor oil, polyoxyethylene-polyoxypropylene glycol, and polyethylene glycol monostearate, more preferred are polyoxyethylene hydrogenated castor oil and polyoxyethylene-polyoxypropylene glycol, and even more preferred are polyoxyethylene hydrogenated castor oil 60 and polyoxyethylene (196) polyoxypropylene (67) glycol.
[0034] The nonionic surfactant may be a commercially available one. The nonionic surfactant may be used alone or in combination of two or more.
[0035] The content of component (C) in the ophthalmic composition according to this embodiment is not particularly limited and is set appropriately depending on the type of component (C), the types and contents of other blended components, the intended use and formulation of the ophthalmic composition, etc. From the viewpoint of more significantly exhibiting the effects of the present invention, the content of component (C) is, for example, preferably 0.0001 to 5 w / v%, more preferably 0.001 to 3 w / v%, even more preferably 0.005 to 2 w / v%, even more preferably 0.01 to 1.5 w / v%, and particularly preferably 0.02 to 1 w / v%, based on the total amount of the ophthalmic composition.
[0036] The content ratio of component (C) relative to component (A) in the ophthalmic composition according to this embodiment is not particularly limited and is set appropriately depending on the types of components (A) and (C), the types and contents of other blended components, the intended use and formulation of the ophthalmic composition, etc. From the viewpoint of further enhancing the effects of the present invention, the content ratio of component (C) relative to component (A) is, for example, preferably 0.0001 to 10 parts by mass, more preferably 0.0005 to 5 parts by mass, even more preferably 0.001 to 3 parts by mass, even more preferably 0.003 to 1 part by mass, particularly preferably 0.01 to 0.5 parts by mass, and particularly more preferably 0.01 to 0.25 parts by mass, relative to 1 part by mass of the total content of component (A) contained in the ophthalmic composition according to this embodiment.
[0037] [(D) component] The ophthalmic composition according to this embodiment may further contain a buffer (D) (also simply referred to as "component (D)"). When the ophthalmic composition further contains component (D), the effects of the present invention are more pronounced.
[0038] The buffering agent is not particularly limited as long as it is pharmaceutically, pharmacologically (pharmaceutical) or physiologically acceptable.
[0039] Examples of the buffer include inorganic buffers, which are buffers derived from inorganic acids, and organic buffers, which are buffers derived from organic acids or organic bases.
[0040] Examples of inorganic buffers include borate buffers, phosphate buffers, and carbonate buffers. Examples of borate buffers include boric acid or its salts (alkali metal borates, alkaline earth metal borates, etc.). Examples of phosphate buffers include phosphoric acid or its salts (alkali metal phosphates, alkaline earth metal phosphates, etc.). Examples of carbonate buffers include carbonic acid or its salts (alkali metal carbonates, alkaline earth metal carbonates, etc.). Furthermore, hydrates of borate, phosphate, or carbonate may be used as borate buffers, phosphate buffers, or carbonate buffers. More specific examples of borate buffers include boric acid or salts thereof (sodium borate, potassium tetraborate, potassium metaborate, ammonium borate, borax, etc.); phosphate buffers include phosphoric acid or salts thereof (disodium hydrogen phosphate, sodium dihydrogen phosphate, potassium dihydrogen phosphate, trisodium phosphate, tripotassium phosphate, calcium monohydrogen phosphate, calcium dihydrogen phosphate, etc.); and carbonate buffers include carbonic acid or salts thereof (sodium bicarbonate, sodium carbonate, ammonium carbonate, potassium carbonate, calcium carbonate, potassium bicarbonate, magnesium carbonate, etc.).
[0041] Examples of organic buffers include citrate buffers, acetate buffers, lactate buffers, succinate buffers, Tris buffers, and AMPD buffers. Examples of citrate buffers include citric acid or salts thereof (such as alkali metal citrates and alkaline earth metal citrates). Examples of acetate buffers include acetic acid or salts thereof (such as alkali metal acetates and alkaline earth metal acetates). Examples of lactate buffers include lactic acid or salts thereof (such as alkali metal lactates and alkaline earth metal lactates). Examples of succinate buffers include succinic acid or salts thereof (such as alkali metal succinates). Furthermore, hydrates of citrate, acetate, lactate, or succinate may be used as citrate buffers, acetate buffers, lactate buffers, or succinate buffers. More specific examples of citrate buffers include citric acid or its salts (sodium citrate, potassium citrate, calcium citrate, sodium dihydrogen citrate, disodium citrate, etc.); acetate buffers include acetic acid or its salts (ammonium acetate, sodium acetate, potassium acetate, calcium acetate, etc.); lactate buffers include lactic acid or its salts (sodium lactate, potassium lactate, calcium lactate, etc.); and succinate buffers include succinic acid or its salts (monosodium succinate, disodium succinate, etc.). Examples of Tris buffers include trometamol or its salts (trometamol hydrochloride, etc.). Examples of AMPD buffers include 2-amino-2-methyl-1,3-propanediol or its salts.
[0042] As the buffer, boric acid buffer (e.g., a combination of boric acid and borax), phosphate buffer (e.g., a combination of disodium hydrogen phosphate and sodium dihydrogen phosphate), and Tris buffer (e.g., trometamol) are preferred, with boric acid buffer being more preferred, boric acid and its salts being even more preferred, and a combination of boric acid and borax being even more preferred.
[0043] The buffering agent may be a commercially available product. One type of buffering agent may be used alone, or two or more types may be used in combination.
[0044] The content of component (D) in the ophthalmic composition according to this embodiment is not particularly limited and is set appropriately depending on the type of component (D), the types and contents of other blended components, the intended use and formulation of the ophthalmic composition, etc. From the viewpoint of more significantly exhibiting the effects of the present invention, the content of component (D) is, for example, preferably 0.01 to 10 w / v%, more preferably 0.05 to 5 w / v%, and even more preferably 0.1 to 3 w / v%, based on the total amount of the ophthalmic composition.
[0045] The content ratio of component (D) relative to component (A) in the ophthalmic composition according to this embodiment is not particularly limited and is set appropriately depending on the types of components (A) and (D), the types and contents of other blended components, the intended use and formulation of the ophthalmic composition, etc. From the viewpoint of further enhancing the effects of the present invention, the content ratio of component (D) relative to component (A) is, for example, preferably 0.01 to 10 parts by mass, more preferably 0.1 to 5 parts by mass, even more preferably 0.3 to 4 parts by mass, and even more preferably 0.5 to 3 parts by mass, of the total content of component (D) relative to 1 part by mass of the total content of component (A) contained in the ophthalmic composition according to this embodiment.
[0046] [(E) component] The ophthalmic composition according to this embodiment may further contain a chelating agent (E). When the ophthalmic composition further contains component (E), the effects of the present invention are more pronounced. The chelating agent is not particularly limited as long as it is medicamentarily, pharmacologically (pharmaceutical), or physiologically acceptable. Examples of the chelating agent include edetic acid and its salts, ethylenediaminediacetic acid (EDDA), ethylenediaminetriacetic acid, N-(2-hydroxyethyl)ethylenediaminetriacetic acid (HEDTA), and diethylenetriaminepentaacetic acid (DTPA). Among these, edetic acid or its salts are preferably used.
[0047] Edetic acid, also known as ethylenediaminetetraacetic acid (EDTA), is 10 H 16 It is a known compound represented by the formula N2O8.
[0048] Examples of salts of edetic acid include alkali metal salts such as sodium edetate, disodium edetate, and tetrasodium edetate, and among these, disodium edetate is preferably used.
[0049] The content of component (E) in the ophthalmic composition according to this embodiment is not particularly limited and is appropriately determined depending on the type of component (E), the types and contents of other components, the intended use of the ophthalmic composition, the formulation, etc. Regarding the content of component (E), from the viewpoint of further enhancing the preservative effect, the total content of component (E) is preferably 0.01 w / v% or more, more preferably 0.03 w / v% or more, even more preferably 0.05 w / v% or more, even more preferably 0.07 w / v% or more, and particularly preferably 0.09 w / v% or more, based on the total amount of the ophthalmic composition. Furthermore, regarding the content of component (E), from the viewpoint of more significantly achieving the effects of the present invention, the total content of component (E) is preferably 10 w / v% or less, more preferably 5 w / v% or less, even more preferably 3 w / v% or less, even more preferably 1 w / v% or less, and particularly preferably 0.5 w / v% or less, based on the total amount of the ophthalmic composition. Furthermore, the content of component (B-2) in the ophthalmic composition according to this embodiment may be, for example, 0.01 to 10 w / v%, 0.03 to 5 w / v%, 0.05 to 3 w / v%, 0.07 to 1 w / v%, or 0.09 to 0.5 w / v%, based on the total amount of the ophthalmic composition.
[0050] The content ratio of component (E) relative to component (A) in the ophthalmic composition according to this embodiment is not particularly limited and is set appropriately depending on the types of components (A) and (E), the types and contents of other blended components, the intended use and formulation of the ophthalmic composition, etc. From the viewpoint of further enhancing the effects of the present invention, the content ratio of component (E) relative to component (A) is, for example, preferably 0.003 to 10 parts by mass, more preferably 0.01 to 5 parts by mass, even more preferably 0.017 to 3 parts by mass, even more preferably 0.023 to 1 part by mass, and particularly preferably 0.03 to 0.5 parts by mass, of the total content of component (E) relative to 1 part by mass of the total content of component (A) contained in the ophthalmic composition according to this embodiment.
[0051] [Component (F)] The ophthalmic composition according to this embodiment may further contain an isotonic agent (F) (also simply referred to as "component (F)"). When the ophthalmic composition further contains component (F), the effects of the present invention are more pronounced. There are no particular limitations on component (F), so long as it is medicamentally, pharmacologically (pharmaceutical), or physiologically acceptable.
[0052] The tonicity adjusting agent, which is the component (F), includes, for example, ionic tonicity adjusting agents and non-ionic tonicity adjusting agents.
[0053] Examples of ionic tonicity agents include inorganic salts such as calcium chloride, magnesium chloride, sodium chloride, potassium chloride, ammonium chloride, calcium sulfate, magnesium sulfate, sodium sulfate, and potassium sulfate, as well as monoethanolamine, diethanolamine, and triethanolamine. Among the ionic tonicity agents, sodium chloride and monoethanolamine are preferred from the viewpoint of more significantly exhibiting the effects of the present invention.
[0054] Examples of nonionic tonicity agents include alcohols such as glycerin, propylene glycol, polyethylene glycol (400, 4000, 6000, etc.), glucose, sorbitol, mannitol, xylitol, and trehalose. Among nonionic tonicity agents, mannitol is preferred from the viewpoint of more significantly exhibiting the effects of the present invention and preventing the preparation from becoming sticky.
[0055] The tonicity agent may be a commercially available one. One type of tonicity agent may be used alone, or two or more types may be used in combination.
[0056] The total content of component (F) in the ophthalmic composition according to this embodiment is not particularly limited and is set appropriately depending on the type of component (F), the types and contents of other blended components, the intended use and formulation of the ophthalmic composition, etc. From the viewpoint of more significantly exhibiting the effects of the present invention, the content of component (F) is, for example, preferably 0.0001 to 10 w / v%, more preferably 0.0005 to 7 w / v%, even more preferably 0.001 to 6 w / v%, even more preferably 0.005 to 5 w / v%, particularly preferably 0.005 to 4 w / v%, more particularly preferably 0.005 to 3 w / v%, even more particularly preferably 0.01 to 2 w / v%, even more particularly preferably 0.01 to 1.5 w / v%, and most preferably 0.05 to 1 w / v%, based on the total amount of the ophthalmic composition.
[0057] The content ratio of component (F) relative to component (A) in the ophthalmic composition according to this embodiment is not particularly limited and is set appropriately depending on the types of components (A) and (F), the types and contents of other blended components, the intended use and formulation of the ophthalmic composition, etc. From the viewpoint of more significantly exhibiting the effects of the present invention, the content ratio of component (F) relative to component (A) is, for example, preferably 0.00003 to 10 parts by mass, more preferably 0.00017 to 7 parts by mass, even more preferably 0.0003 to 6 parts by mass, even more preferably 0.0017 to 5 parts by mass, particularly preferably 0.0017 to 4 parts by mass, more particularly preferably 0.0017 to 3 parts by mass, even more particularly preferably 0.003 to 2 parts by mass, even more particularly preferably 0.003 to 1.5 parts by mass, and most preferably 0.016 to 1 part by mass, of the total content of component (F) contained in the ophthalmic composition according to this embodiment.
[0058] The pH of the ophthalmic composition according to this embodiment is not particularly limited as long as it is within a medicamentarily, pharmacologically (pharmaceutical), or physiologically acceptable range. The pH of the ophthalmic composition according to this embodiment may be, for example, 4.0 to 9.5, preferably 4.0 to 9.0, more preferably 4.5 to 9.0, even more preferably 4.5 to 8.5, even more preferably 5.0 to 8.5, particularly preferably 5.5 to 8.0, and particularly more preferably 6.0 to 7.8.
[0059] The ophthalmic composition according to this embodiment can be adjusted to an osmotic pressure ratio within a biologically acceptable range, as needed. The appropriate osmotic pressure ratio varies depending on the application site, dosage form, etc.; however, to more significantly exhibit the effects of the present invention, it is preferably 0.05 to 6, more preferably 0.4 to 5, even more preferably 0.6 to 3, and even more preferably 0.8 to 2. The osmotic pressure ratio may also be 0.3 to 4, 0.5 to 3, or 0.7 to 1.4. The osmotic pressure can be adjusted using inorganic salts, polyhydric alcohols, etc., by methods known in the art. The osmotic pressure ratio is defined as the ratio of the osmotic pressure of the sample to 286 mOsm (the osmotic pressure of a 0.9 w / v% sodium chloride aqueous solution) according to the 17th Edition of the Japanese Pharmacopoeia. The osmotic pressure is measured using the osmotic pressure measurement method (freezing-point depression method) described in the Japanese Pharmacopoeia. The standard solution for measuring osmolality ratios (0.9 w / v% sodium chloride aqueous solution) can be prepared by drying sodium chloride (Japanese Pharmacopoeia standard reagent) at 500-650°C for 40-50 minutes, allowing it to cool in a desiccator (silica gel), accurately weighing 0.900 g of the solution, and dissolving it in purified water to make exactly 100 mL; alternatively, a commercially available standard solution for measuring osmolality ratios (0.9 w / v% sodium chloride aqueous solution) can be used.
[0060] The viscosity of the ophthalmic composition according to this embodiment is not particularly limited as long as it is within a medicamentarily, pharmacologically (pharmaceutical), or physiologically acceptable range. For example, the viscosity of the ophthalmic composition according to this embodiment, as measured at 20°C using a rotational viscometer (TV-20 viscometer, manufactured by Toki Sangyo Co., Ltd., rotor: 1°34' x R24), is preferably 0.1 to 10,000 mPa·s, more preferably 1 to 3,000 mPa·s, even more preferably 1 to 1,000 mPa·s, even more preferably 1 to 100 mPa·s, particularly preferably 1 to 50 mPa·s, particularly more preferably 1 to 10 mPa·s, and even more preferably 1.3 to 5 mPa·s. Alternatively, the viscosity may be 1 to 5 mPa·s, 1 to 4 mPa·s, or 1 to 3 mPa·s.
[0061] The ophthalmic composition according to this embodiment may contain, in addition to the above-mentioned components, a combination of various pharmacologically active components and physiologically active components in appropriate amounts, as long as the effects of the present invention are not impaired. The components are not particularly limited, and examples thereof include active ingredients in ophthalmic drugs listed in the 2012 edition of the OTC Drug Manufacturing and Marketing Approval Standards (supervised by the Japan Society of Regulatory Science). Specific examples of components used in ophthalmic drugs include the following: Antiallergic agents: for example, sodium cromoglycate, tranilast, pemirolast potassium, etc. Antihistamines: for example, diphenhydramine hydrochloride, iproheptine, chlorpheniramine maleate, levocabastine hydrochloride, ketotifen fumarate, pemirolast potassium, olopatadine hydrochloride, etc. Anti-inflammatory agents: for example, methyl salicylate, glycol salicylate, allantoin, tranexamic acid, lysozyme, lysozyme chloride, indomethacin, pranoprofen, ibuprofen, ibuprofen piconol, ketoprofen, felbinac, bendazac, piroxicam, bufexamac, butyl flufenamate, epsilon-aminocaproic acid, berberine chloride, berberine sulfate, sodium azulene sulfonate, etc. Steroids: for example, fluticasone propionate, fluticasone furoate, mometasone furoate, beclomethasone propionate, flunisolide, etc. Decongestants: for example, tetrahydrozoline hydrochloride, tetrahydrozoline nitrate, naphazoline hydrochloride, naphazoline nitrate, epinephrine, epinephrine hydrochloride, ephedrine hydrochloride, phenylephrine hydrochloride, dl-methylephedrine hydrochloride, etc. Ocular muscle regulating agents: For example, cholinesterase inhibitors having an active center similar to that of acetylcholine, specifically neostigmine methylsulfate, tropicamide, helenien, atropine sulfate, etc. Vitamins: for example, retinol acetate, retinol palmitate, tocopherol acetate, flavin adenine dinucleotide sodium, cyanocobalamin, pyridoxine hydrochloride, panthenol, calcium pantothenate, ascorbic acid, sodium ascorbate, etc. Amino acids: for example, glutamic acid, aspartic acid, arginine, glycine, aminoethylsulfonic acid (taurine), trimethylglycine and salts thereof. Astringents: for example, zinc oxide, zinc lactate, zinc sulfate, etc. Others: For example, sulfamethoxazole, sulfisoxazole, sulfisomidine and their salts.
[0062] The ophthalmic composition according to this embodiment may contain one or more additives selected appropriately in a conventional manner depending on the intended use and formulation, as long as the effects of the present invention are not impaired. Examples of such additives include those listed in the Pharmaceutical Additives Dictionary 2007 (edited by the Japan Pharmaceutical Additives Association). Representative additives include the following: Carrier: For example, an aqueous solvent such as water or aqueous ethanol. Bases: for example, octyldodecanol, titanium oxide, potassium bromide, plastibase, etc. pH adjusters: for example, hydrochloric acid, acetic acid, sodium hydroxide, potassium hydroxide, calcium hydroxide, magnesium hydroxide, triethanolamine, diisopropanolamine, etc. Stabilizers: for example, sodium formaldehyde sulfoxylate (Rongalit), sodium hydrogen sulfite, sodium pyrosulfite, aluminum monostearate, glycerin monostearate, cyclodextrin, monoethanolamine, dibutylhydroxytoluene, etc. Thickeners other than component (A): for example, cellulose-based polymer compounds (e.g., methyl cellulose, ethyl cellulose, hydroxypropyl methyl cellulose, hydroxyethyl cellulose, sodium carboxymethyl cellulose, etc.), polyvinyl-based polymer compounds (e.g., polyvinylpyrrolidone, polyvinyl alcohol, etc.), carboxyvinyl polymers, guar gum, hydroxypropyl guar gum, gum arabic, karaya gum, xanthan gum, agar, alginic acid and its salts (e.g., sodium salt), mucopolysaccharides (e.g., heparinoids, heparin, heparin, heparin sulfate, heparan sulfate, heparinoid, hyaluronic acid and its salts (e.g., sodium salt)), starch, chitin and its derivatives, chitosan and its derivatives, carrageenan, etc. Sugars: for example, glucose, cyclodextrin, etc. Anionic surfactants: for example, polyoxyethylene alkyl ether phosphates, polyoxyethylene alkyl ether sulfates, alkylbenzenesulfonates, alkyl sulfates, N-acyltaurine salts, etc. Amphoteric surfactants: for example, lauryl dimethylaminoacetic acid betaine. Preservatives: for example, alkyldiaminoethylglycine hydrochloride, sodium benzoate, ethanol, chlorhexidine and its salts (specifically, chlorhexidine hydrochloride, chlorhexidine acetate, chlorhexidine gluconate, etc.), zinc chloride, dibutylhydroxytoluene, chlorobutanol, sorbic acid, potassium sorbate, sodium dehydroacetate, methyl parahydroxybenzoate, ethyl parahydroxybenzoate, propyl parahydroxybenzoate, butyl parahydroxybenzoate, oxyquinoline sulfate, phenethyl alcohol, benzyl alcohol, benzalkonium chloride, biguanide compounds (specifically, polyhexanide hydrochloride (polyhexamethylene biguanide), alexidine hydrochloride, etc.), Gloquil (trade name manufactured by Rhodia), etc.
[0063] From the viewpoint of being able to significantly exhibit the effects of the present invention, the ophthalmic composition of this embodiment preferably does not contain chlorhexidine gluconate, polyhexanide hydrochloride, neostigmine methylsulfate, lecithin, petrolatum, two or more metal salts of L-aspartic acid, 0.3% or more of sodium hyaluronate, and dipotassium glycyrrhizinate.
[0064] The ophthalmic composition according to this embodiment may be an aqueous composition (mainly containing an aqueous or hydrophilic base or carrier) or an oil-based composition (mainly containing an oil-based or hydrophobic base or carrier). When the ophthalmic composition is an aqueous composition, the water content is, for example, preferably 50% by weight or more, more preferably 75% by weight or more, even more preferably 80% by weight or more, even more preferably 85% by weight or more, and particularly preferably 90% by weight or more, based on the total weight of the ophthalmic composition. When the ophthalmic composition is an aqueous composition, the water content is, for example, preferably less than 100% by weight, more preferably 99.5% by weight or less, even more preferably 99.2% by weight or less, even more preferably 99.0% by weight or less, particularly preferably 97.0% by weight or less, and most preferably 96.5% by weight or less, based on the total weight of the ophthalmic composition. When the ophthalmic composition is an oily composition, the water content is, for example, preferably less than 50% by weight, more preferably 30% by weight or less, and even more preferably 20% by weight or less, based on the total weight of the ophthalmic composition. The ophthalmic composition according to this embodiment is preferably an aqueous composition.
[0065] The water used in the ophthalmic composition according to this embodiment may be any water that is medicamentally, pharmacologically (pharmaceutical), or physiologically acceptable. Examples of such water include distilled water, tap water, purified water, sterile purified water, water for injection, and distilled water for injection. These definitions are based on the Japanese Pharmacopoeia, 17th Edition.
[0066] The ophthalmic composition according to the present embodiment can be prepared, for example, by adding and mixing the components (A), (B), and (C), and, if necessary, other components, to a desired content. Specifically, the composition can be prepared, for example, by dissolving or suspending the components in purified water, adjusting the pH and osmotic pressure to a predetermined value, and sterilizing the mixture by filtration or the like.
[0067] The ophthalmic composition according to the present embodiment can be in various dosage forms depending on the purpose, such as a liquid, a gel, a semi-solid (ointment, etc.), etc. Among these, a liquid is preferred, and an aqueous liquid is more preferred.
[0068] The ophthalmic composition according to this embodiment can be used, for example, as eye drops (also referred to as eye drops or eye drops; eye drops include artificial tears and eye drops that can be applied to the eyes while wearing contact lenses), eyewash (also referred to as eyewash or eyewash; eyewashes include eyewashes that can be applied to the eyes while wearing contact lenses), or a contact lens composition (contact lens wetting solution, contact lens care composition (contact lens disinfectant, contact lens preservative, contact lens cleaner, contact lens cleaning and preservative), contact lens wetting solution that can be used both as a contact lens wetting solution and as an eye drop while wearing contact lenses, etc.). Suitable examples of the ophthalmic composition according to this embodiment include eye drops, eyewash, and contact lens compositions, more suitable examples include eye drops that can be applied to the eyes while wearing contact lenses, eyewashes that can be applied to the eyes while wearing contact lenses, contact lens wetting solution, and contact lens wetting solution, and even more suitable examples include eye drops that can be applied to the eyes while wearing contact lenses. The term "contact lenses" includes hard contact lenses and soft contact lenses (including both ionic and non-ionic contact lenses, and both silicone hydrogel contact lenses and non-silicone hydrogel contact lenses). In this specification, "soft contact lenses" refers to a classification of soft contact lenses based on the "Classification Method for Soft Contact Lenses" stipulated in the Notification of the Director of the Evaluation and Licensing Division, Pharmaceutical and Medical Safety Bureau, Ministry of Health, Labour and Welfare (then the Ministry of Health and Welfare), dated March 31, 1999, entitled "Handling of Documents to be Attached to Applications for Approval to Manufacture (Import) Soft Contact Lenses and Soft Contact Lens Disinfectants," No. 645. Here, soft contact lenses are classified based on criteria such as water content and the mole percentage of anionic monomers. For example, soft contact lenses belonging to Group IV have common properties of having a water content of 50% or more and having 1% or more mole percentage of anionic monomers among the constituent monomers of the raw material polymer. This classification follows the classification method for soft contact lenses established by the FDA (U.S. Food and Drug Administration).
[0069] When the ophthalmic composition according to this embodiment is in the form of eye drops, the effects of the present invention can be more significantly exhibited, so the ophthalmic composition is preferably an eye drop that can be instilled while wearing contact lenses, more preferably an eye drop that can be instilled while wearing soft contact lenses (eye drops for soft contact lenses), and even more preferably an ophthalmic composition for soft contact lenses of Group IV in the FDA contact lens classification. When the ophthalmic composition according to this embodiment is in the form of eye drops, the dosage and administration method are not particularly limited as long as they are effective and have few side effects. For example, for adults (15 years of age or older) and children aged 7 years of age or older, 1 to 2 drops at a time, 2 to 4 times a day, or 4 times a day, or 1 to 2 drops, 1 to 3 drops, or 2 to 3 drops at a time, 5 to 6 times a day, can be exemplified.
[0070] The ophthalmic composition according to this embodiment is preferably an artificial tear, since this allows the effects of the present invention to be more pronounced. When the ophthalmic composition according to this embodiment is an artificial tear, it is preferable that the ophthalmic composition does not contain any of an anti-inflammatory agent, an antiallergic agent, an antihistamine, a steroid, a decongestant, an eye muscle regulating agent, a vitamin, an astringent, sulfamethoxazole, sulfisoxazole, or sulfisomidine.
[0071] The ophthalmic composition according to this embodiment is provided in any container. The container for containing the ophthalmic composition according to this embodiment is not particularly limited and may be made of, for example, glass or plastic. Plastic is preferred. Examples of plastic include polyethylene terephthalate, polyarylate, polyethylene naphthalate, polycarbonate, polyethylene, polypropylene, polyimide, copolymers of monomers constituting these, and mixtures of two or more of these. Polypropylene, polyethylene, and polyethylene terephthalate are preferred, and polyethylene terephthalate is more preferred. Furthermore, the container for containing the ophthalmic composition according to this embodiment may be a transparent container that allows the interior of the container to be seen, or an opaque container that makes it difficult to see the interior of the container. A transparent container is preferred. Here, the term "transparent container" includes both colorless transparent containers and colored transparent containers.
[0072] A nozzle may be attached to the container that contains the ophthalmic composition according to this embodiment. The material of the nozzle is not particularly limited and may be, for example, glass or plastic. Plastic is preferred. Examples of plastic include polybutylene terephthalate, polyethylene, polypropylene, polyethylene naphthalate, copolymers of monomers constituting these, and mixtures of two or more of these. From the viewpoint of further enhancing the effects of the present invention, polypropylene, polyethylene, polyethylene terephthalate, and polyethylene naphthalate are preferred as the material of the nozzle, with polyethylene being more preferred.
[0073] The container for holding the ophthalmic composition of this embodiment may be a multi-dose type that holds an amount for multiple uses, or a unit-dose type that holds an amount for a single use, but it is preferable that it be a multi-dose type as this allows the effects of the present invention to be more pronounced. [Example]
[0074] The present invention will be specifically explained below based on test examples, but the present invention is not limited to these.
[0075] [Test Example 1: Protein Cleaning Test] Each ophthalmic composition (eye drops; 100 mL) shown in Table 1 was prepared by a conventional method. The unit of each component in Table 1 is w / v %. In accordance with FDA guidelines, 2 mL of protein solution (a buffer solution (sodium chloride: 0.9 w / v%, sodium dihydrogen phosphate dihydrate: 0.045 w / v%) supplemented with egg white lysozyme at 0.120 w / v%, bovine serum albumin at 0.388 w / v%, and bovine globulin at 0.161 w / v%) was dispensed into 10 mL glass vials (hereinafter referred to as screw vials). Next, soft contact lenses (etafilcon A lenses (Johnson & Johnson, trade name: 2 Week Acuvue, FDA contact lens classification: Group IV)) were washed with 100 mL of saline solution in a beaker, wiped dry with Bemcot® Lint-Free, and then immersed individually in the protein solution and shaken at 34°C and 120 rpm for 8 hours. The contact lenses were removed, immersed in 100 mL of saline for approximately 1 second to rinse off excess protein, then drained and wiped with Bemcot® Lint-Free. Each lens was then immersed individually in 2 mL of each ophthalmic composition in a 10 mL screw vial, and shaken at 34°C and 120 rpm for approximately 16 hours. The contact lenses were then removed, immersed in 100 mL of saline for approximately 1 second to rinse off excess ophthalmic composition, drained, wiped with Bemcot® Lint-Free, and then immersed in 2 mL of protein separation solution (aqueous solution containing 1% sodium carbonate and 1% SDS) in a 10 mL screw vial. The lenses were shaken at room temperature for approximately 1 hour in a shaker set at 120 rpm, and the proteins adsorbed on the contact lenses were recovered in the protein separation solution. Using a BCA assay kit (Thermo Scientific, Pierce #23225), the amount of protein in the protein separation solution was quantified as an albumin equivalent value by quantifying it using albumin as a standard, and this was taken as the amount of protein adsorbed onto the contact lens. The improvement rate of protein removal for each ophthalmic composition relative to Reference Example 1-1 was calculated according to the following formula 1. The results are shown in Table 1. [Formula 1] Protein cleaning improvement rate (%)={(protein adsorption amount of Reference Example 1-1−protein adsorption amount of each ophthalmic composition) / protein adsorption amount of Reference Example 1-1}×100 The sodium chondroitin sulfate used was non-standard sodium chondroitin sulfate (Seikagaku Corporation, weight-average molecular weight 20,000).
[0076] [Table 1]
[0077] In Comparative Examples 1-1, 1-2, and 1-3, which contained castor oil, sesame oil, or liquid paraffin, the protein cleaning effect was significantly reduced compared to Reference Example 1-1, which did not contain castor oil, sesame oil, or liquid paraffin. On the other hand, in Examples 1-1, 1-2, and 1-3, which contained castor oil, sesame oil, or liquid paraffin and 3.0 w / v% sodium chondroitin sulfate, the protein cleaning improvement rate was significantly improved compared to Reference Example 1-1, which did not contain castor oil, sesame oil, or liquid paraffin.
[0078] [Test Example 2: Evaluation of Variation in Drop Amount] Each ophthalmic composition (eye drops; 100 mL) shown in Table 2 was prepared by a conventional method. The unit of each component in Table 2 is w / v %. Next, 10 mL of each prepared ophthalmic composition was filled into a 10 mL polyethylene terephthalate eye drop container, and a polyethylene nozzle was attached to the container. The polyethylene nozzle used was suitable for dispensing 30 to 50 μL. The eye drops in the container were dispensed horizontally, and the weight of each drop was measured. This procedure was repeated 10 times to determine the average dispensed amount (AVG: mg) and standard deviation (SD: mg), and the variation in dispensed amount (coefficient of variation CV: %) was calculated using the following formula 2. Using each obtained coefficient of variation, the suppression rate of variation in dispensed amount for each ophthalmic composition relative to Comparative Example 2-1 was calculated according to the following formula 3. The results are shown in Table 2. [Formula 2] Variation in drip volume (coefficient of variation CV:%) = (SD / AVG) x 100 [Equation 3] Dropping amount variation suppression rate (%)={(Variation coefficient of Comparative Example 2-1−Variation coefficient of each ophthalmic composition) / Variation coefficient of Comparative Example 2-1}×100 The sodium chondroitin sulfate used was non-standard sodium chondroitin sulfate (Seikagaku Corporation, weight-average molecular weight 20,000).
[0079] [Table 2]
[0080] It was confirmed that the addition of sesame oil or liquid paraffin to an ophthalmic composition containing 3.0 w / v % sodium chondroitin sulfate significantly reduced the variation in the amount dispensed.
[0081] [Test Example 3: Protein Cleaning Test (2)] Each ophthalmic composition (eye drops; 100 mL) shown in Table 3 was prepared by a conventional method. The unit of each component in Table 3 is w / v %. The amount of protein adsorbed to contact lenses for each ophthalmic composition was quantified using the same method as in Test Example 1 above, and the protein cleaning improvement rate for each ophthalmic composition relative to Reference Example 3-1 was calculated according to the following formula 3. The viscosity and osmotic pressure of each ophthalmic composition were also measured. The viscosity was measured at 20°C using a rotational viscometer (TV-20 type viscometer, manufactured by Toki Sangyo Co., Ltd., rotor: 1°34' x R24) at a rotation speed of 100 rpm. The osmotic pressure was measured with reference to the osmotic pressure measurement method (freezing point depression method) described in the Japanese Pharmacopoeia. The results are shown in Table 3. [Formula 3] Protein cleaning improvement rate (%)={(protein adsorption amount of Reference Example 3-1−protein adsorption amount of each ophthalmic composition) / protein adsorption amount of Reference Example 3-1}×100 The sodium chondroitin sulfate used was non-standard sodium chondroitin sulfate (Seikagaku Corporation, weight-average molecular weight 20,000).
[0082] [Table 3]
[0083] In Comparative Examples 3-1, 3-2, and 3-3, which contained castor oil, sesame oil, or liquid paraffin, the protein cleaning effect was significantly reduced compared to Reference Example 3-1, which did not contain castor oil, sesame oil, or liquid paraffin. On the other hand, in Examples 3-1, 3-2, and 3-3, which contained castor oil, sesame oil, or liquid paraffin and 1.0 w / v% sodium chondroitin sulfate, the protein cleaning improvement rate was significantly improved compared to Reference Example 3-1, which did not contain castor oil, sesame oil, or liquid paraffin.
[0084] [Formulation example] Formulation examples are shown in Table 4 below. The units for each ingredient in Table 4 are all w / v % unless otherwise specified in the table.
[0085] [Table 4]
Claims
[Claim 1] An ophthalmic composition comprising (A) at least one component selected from the group consisting of chondroitin sulfate and salts thereof, (B) at least one component selected from the group consisting of (B-1) castor oil, (B-2) sesame oil, and (B-3) liquid paraffin, and (C) a nonionic surfactant, wherein the content of component (A) is 0.7 w / v% or more based on the total amount of the ophthalmic composition.
Citation Information
Patent Citations
Ophthalmologic composition for silicone hydrogel contact lens
JP2011148791A