WO2014192738A1 - Compositions ophtalmiques pour lentilles de contact souples zwittérioniques - Google Patents
Compositions ophtalmiques pour lentilles de contact souples zwittérioniques Download PDFInfo
- Publication number
- WO2014192738A1 WO2014192738A1 PCT/JP2014/063960 JP2014063960W WO2014192738A1 WO 2014192738 A1 WO2014192738 A1 WO 2014192738A1 JP 2014063960 W JP2014063960 W JP 2014063960W WO 2014192738 A1 WO2014192738 A1 WO 2014192738A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- zwitterionic
- pranoprofen
- scl
- ophthalmic composition
- salt
- Prior art date
Links
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- JLKIGFTWXXRPMT-UHFFFAOYSA-N sulphamethoxazole Chemical compound O1C(C)=CC(NS(=O)(=O)C=2C=CC(N)=CC=2)=N1 JLKIGFTWXXRPMT-UHFFFAOYSA-N 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 229940104261 taurate Drugs 0.000 description 1
- 229960000337 tetryzoline Drugs 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- RTKIYNMVFMVABJ-UHFFFAOYSA-L thimerosal Chemical compound [Na+].CC[Hg]SC1=CC=CC=C1C([O-])=O RTKIYNMVFMVABJ-UHFFFAOYSA-L 0.000 description 1
- 229940033663 thimerosal Drugs 0.000 description 1
- 235000010384 tocopherol Nutrition 0.000 description 1
- 229960001295 tocopherol Drugs 0.000 description 1
- 229930003799 tocopherol Natural products 0.000 description 1
- 239000011732 tocopherol Substances 0.000 description 1
- 229940042585 tocopherol acetate Drugs 0.000 description 1
- 229940100613 topical solution Drugs 0.000 description 1
- NZHGWWWHIYHZNX-CSKARUKUSA-N tranilast Chemical compound C1=C(OC)C(OC)=CC=C1\C=C\C(=O)NC1=CC=CC=C1C(O)=O NZHGWWWHIYHZNX-CSKARUKUSA-N 0.000 description 1
- 229960005342 tranilast Drugs 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 229920003169 water-soluble polymer Polymers 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
- 229940082509 xanthan gum Drugs 0.000 description 1
- 239000011592 zinc chloride Substances 0.000 description 1
- 235000005074 zinc chloride Nutrition 0.000 description 1
- 229960001939 zinc chloride Drugs 0.000 description 1
- 239000011576 zinc lactate Substances 0.000 description 1
- 229940050168 zinc lactate Drugs 0.000 description 1
- 235000000193 zinc lactate Nutrition 0.000 description 1
- NWONKYPBYAMBJT-UHFFFAOYSA-L zinc sulfate Chemical compound [Zn+2].[O-]S([O-])(=O)=O NWONKYPBYAMBJT-UHFFFAOYSA-L 0.000 description 1
- 229960001763 zinc sulfate Drugs 0.000 description 1
- 229910000368 zinc sulfate Inorganic materials 0.000 description 1
- GVJHHUAWPYXKBD-IEOSBIPESA-N α-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/08—Solutions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/436—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
- A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- C—CHEMISTRY; METALLURGY
- C11—ANIMAL OR VEGETABLE OILS, FATS, FATTY SUBSTANCES OR WAXES; FATTY ACIDS THEREFROM; DETERGENTS; CANDLES
- C11D—DETERGENT COMPOSITIONS; USE OF SINGLE SUBSTANCES AS DETERGENTS; SOAP OR SOAP-MAKING; RESIN SOAPS; RECOVERY OF GLYCEROL
- C11D3/00—Other compounding ingredients of detergent compositions covered in group C11D1/00
- C11D3/0005—Other compounding ingredients characterised by their effect
- C11D3/0078—Compositions for cleaning contact lenses, spectacles or lenses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0048—Eye, e.g. artificial tears
Definitions
- the present invention relates to an ophthalmic composition for a zwitterionic soft contact lens that exhibits a clear appearance and can suppress adsorption of pranoprofen and / or a salt thereof to the zwitterionic soft contact lens.
- the present invention also relates to a method for suppressing adsorption of pranoprofen and / or a salt thereof to a zwitterionic soft contact lens.
- Planoprofen and / or its salts have the effect of suppressing the biosynthesis of prostaglandins that cause inflammation and pain.
- alleviation of symptoms such as redness of the eyes and itching, blepharitis, and conjunctivitis It is widely used for the purpose of prevention or treatment of scleritis including suprasclitis, postoperative inflammation, anterior uveitis, and the like.
- Various preparation formulations of ophthalmic compositions using pranoprofen and / or salts thereof have also been reported.
- Patent Document 1 reports that an aqueous topical solution containing pranoprofen and / or a salt thereof and an antihistamine can exhibit excellent anti-inflammatory and antipruritic effects.
- Patent Document 2 contains pranoprofen and / or its salt 0.01 to 2.0 w / v% and a specific vasoconstrictor 0.0005 to 0.1 w / v% such as naphazoline. It has also been reported that eye drops can effectively exert the action of removing or reducing the hyperemia of the external eye part.
- the zwitterionic SCL eye drops need to be formulated so as not to adversely affect the zwitterionic SCL.
- a drug in an eye drop for zwitterionic SCL is adsorbed to SCL, the lens may be deformed, the feeling of use may be reduced, and the desired pharmacological effect may not be exerted on the ocular mucosa.
- suppression of drug adsorption on zwitterionic SCL is a particularly important issue.
- Patent Document 3 discloses, as a pharmaceutical formulation that can suppress the adsorption of a basic drug composed of an amine compound having a secondary or tertiary amino group to SCL, together with the basic drug, an amino acid, a salt thereof, and an acidic mucopolysaccharide. , A salt thereof, or a cyclodextrin, and a composition for SCL having a pH set to 3.5 to 4.8 has been reported.
- Patent Document 3 attention is paid to pranoprofen and / or a salt thereof, and no study has been made on its adsorption property to zwitterionic SCL. Since amine compounds having secondary or tertiary amino groups include a wide variety of drugs, the adsorption properties of drugs on SCL vary depending on the structure other than amino groups. Furthermore, since the characteristics of the lens surface of SCL vary greatly depending on the presence or absence of ionicity, the type of ionicity, etc., examination of the drug adsorption characteristics on SCL according to the SCL material is required.
- zwitterionic SCL has a specific problem that, unlike nonionic SCL and anionic SCL, the adsorptivity of pranoprofen and / or its salt is extremely high. (See Test Example 1 below).
- Patent Document 3 it is essential to set the pH to 4.8 or less.
- the present inventors have determined that the ophthalmic composition for SCL containing pranoprofen and / or a salt thereof has a pH of 4.8. When adjusted to the following extent, it has been confirmed that there is a problem that white turbidity occurs and the appearance properties that can be put into practical use cannot be exhibited (see Test Example 2 described later).
- the present invention provides a zwitterionic SCL ophthalmic composition containing pranoprofen and / or a salt thereof, which has a clear appearance property, and pranoprofen and / or a salt thereof to zwitterionic SCL. It aims at providing the technique which suppresses adsorption
- the present inventor has formulated trometamol in an ophthalmic composition for zwitterionic SCL containing pranoprofen and / or a salt thereof, and has a pH of 5.5. It has been found that, by setting as described above, a clear appearance property can be realized, and adsorption of pranoprofen and / or a salt thereof to zwitterionic SCL can be effectively suppressed.
- the present invention has been completed by further studies based on this finding.
- Item 1 An ophthalmic composition for a zwitterionic soft contact lens, comprising pranoprofen and / or a pharmaceutically acceptable salt thereof and trometamol and having a pH of 5.5 or more.
- Item 2. The ophthalmic composition for zwitterionic soft contact lenses according to Item 1, which contains 0.0001 to 5 w / v% of trometamol.
- Item 3. Item 3. The ophthalmic composition for zwitterionic soft contact lenses according to Item 1 or 2, wherein the pH is 5.5 to 9. Item 4.
- an ophthalmic composition for zwitterionic soft contact lenses containing pranoprofen and / or a pharmaceutically acceptable salt thereof trometamol is added and the pH is adjusted to 5.5 or more
- a method for suppressing adsorption of pranoprofen and / or a pharmaceutically acceptable salt thereof to a zwitterionic soft contact lens Item 7.
- an ophthalmic composition for zwitterionic soft contact lenses comprising a solution containing pranoprofen and / or a pharmaceutically acceptable salt thereof and trometamol and having a pH of 5.5 or more use.
- the ophthalmic composition for zwitterionic SCL of the present invention it is possible to suppress the adsorption of pranoprofen and / or a salt thereof to the zwitterionic SCL, so that the planopro without adversely affecting the zwitterionic SCL.
- the medicinal effects of phen and / or a salt thereof can be effectively exhibited.
- adsorption of pranoprofen and / or its salt to zwitterionic SCL is suppressed by blending and adjusting pH of trometamol used as a pH adjuster.
- the presence or absence of other pharmacological components and additives can be arbitrarily set, there is an advantage that there are few restrictions on the formulation.
- ophthalmic composition for zwitterionic SCL of the present invention while containing pranoprofen and / or a salt thereof, white turbidity caused by setting to about pH 4.8 or less can be suppressed, An ophthalmic composition for zwitterionic SCL that exhibits a clear appearance can be provided.
- “clear” refers to a state in which white turbidity is not caused by pranoprofen and / or a salt thereof, and is not limited to colorless and clear, but is colored and clear that is colored by other components. It is a concept that also includes.
- Ophthalmic Composition for Zwitterionic SCL contains pranoprofen and / or a pharmaceutically acceptable salt thereof and trometamol and has a pH of 5. It is 5 or more.
- the ophthalmic composition for zwitterionic SCL of the present invention will be described in detail.
- the “ophthalmic composition for zwitterionic SCL” refers to a composition that is used in the ophthalmic field and used in contact with zwitterionic SCL.
- the unit of concentration of each component “w / v%” indicates mass to volume percentage and is synonymous with g / 100 mL.
- the ophthalmic composition for zwitterionic SCL of the present invention contains pranoprofen and / or a salt thereof.
- Planoprofen is also known as ⁇ -methyl-5H- [1] benzopyrano [2,3-b] pyridine-7-acetic acid, and is a known compound known to have an anti-inflammatory action in the ophthalmic field. .
- the salt of pranoprofen is not particularly limited as long as it is pharmaceutically acceptable.
- metal salts such as sodium salt, potassium salt, calcium salt, magnesium salt, aluminum salt; triethylamine salt, diethylamine salt, Examples thereof include organic base salts such as morpholine salt and piperazine salt.
- These pranoprofen salts may be used alone or in combination of two or more.
- one kind selected from pranoprofen and a salt thereof may be used alone, or two or more kinds may be used in combination.
- pranoprofen is preferable.
- the concentration of pranoprofen and / or a salt thereof is appropriately set according to the use of the ophthalmic composition for zwitterionic SCL, for example, 0.001 to 0.5 w / v%, preferably 0.01 to 0.2 w / v%, more preferably 0.01 to 0.1 w / v%.
- the ophthalmic composition for zwitterionic SCL of the present invention further contains trometamol.
- Trometamol is also known as trishydroxymethylaminomethane and is a known compound that is also used as a buffer in the ophthalmic field.
- the concentration of trometamol is, for example, 0.0001 to 5 w / v%.
- the concentration of trometamol is preferably 0.001 to 5 w / v%, more preferably 0. 0.001 to 2 w / v%.
- the pH of the ophthalmic composition for zwitterionic SCL of the present invention is set to 5.5 or more.
- trometamol coexists with the pranoprofen and / or salt thereof and is set to such a pH range, so that pranoprofen and / or salt thereof is While suppressing adsorption to zwitterionic SCL, it becomes possible to suppress white turbidity and exhibit a clear appearance.
- the pH of the ophthalmic composition for zwitterionic SCL of the present invention is to provide a clear appearance property while further effectively suppressing the adsorption of pranoprofen and / or its salt to the zwitterionic SCL. From the viewpoint, it is preferably 5.5 to 9, more preferably 6 to 8, still more preferably 6.5 to 8, and particularly preferably 6.5 to 7.5.
- a pH adjuster generally used in ophthalmic compositions may be used.
- the pH adjuster include alkalis such as sodium hydroxide and potassium hydroxide; acids such as acetic acid, citric acid, hydrochloric acid, phosphoric acid and tartaric acid. These pH adjusters may be used alone or in combination of two or more.
- the ophthalmic composition for zwitterionic SCL of the present invention contains trometamol exhibiting a buffering action, it can have a buffering capacity without including other buffering agents.
- Other buffers may be included as needed, as long as they do not interfere. Examples of such other buffers include phosphate buffer, borate buffer, citrate buffer, tartaric acid buffer, acetate buffer, amino acid, and the like. These buffering agents may be used alone or in combination of two or more.
- the ophthalmic composition for zwitterionic SCL of the present invention may contain a pharmacological component other than pranoprofen and / or a salt thereof, if necessary, in addition to the above components.
- pharmacological components include dipotassium glycyrrhizinate, allantoin, epsilon aminocaproic acid, bromfenac, ketorolac tromethamine, nepafenac, berberine chloride, berberine sulfate, sodium azulene sulfonate, zinc sulfate, zinc lactate, lysozyme hydrochloride
- Anti-histamines such as chlorpheniramine maleate and diphenhydramine hydrochloride; antiallergic agents such as cromoglycate sodium, ketotifen fumarate, acitazanolast, amlexanox, pemirolast potassium, tranilast, ibudilast; , Ofloxaci
- concentration of these pharmacological components is appropriately set according to the type of the pharmacological component and the use of the ophthalmic composition for zwitterionic SCL.
- the ophthalmic composition for zwitterionic SCL of the present invention contains, as necessary, isotonic agents, solubilizers, thickeners, chelating agents, cooling agents, preservatives. Further, additives such as stabilizers and surfactants may be contained.
- isotonic agent examples include saccharides such as sorbitol, glucose and mannitol; polyhydric alcohols such as glycerin and propylene glycol; salts such as sodium chloride; boric acid and the like. These isotonic agents may be used alone or in combination of two or more.
- solubilizer examples include nonionic surfactants such as polyoxyethylene sorbitan monooleate, polyoxyethylene hydrogenated castor oil, tyloxapol, and pluronic; polyhydric alcohols such as glycerin and macrogol. These solubilizers may be used alone or in combination of two or more.
- the thickener examples include water-soluble polymers such as polyvinylpyrrolidone, polyethylene glycol, polyvinyl alcohol, carboxyvinyl polymer, xanthan gum, sodium chondroitin sulfate, sodium hyaluronate; hypromellose, hydroxyethyl cellulose, methyl cellulose, hydroxypropyl cellulose, hydroxypropyl Examples thereof include celluloses such as methyl cellulose and sodium carboxymethyl cellulose. These thickeners may be used alone or in combination of two or more.
- chelating agent examples include edetate, citric acid or a salt thereof. These chelating agents may be used individually by 1 type, and may be used in combination of 2 or more type.
- Examples of the refreshing agent include l-menthol, borneol, camphor, and eucalyptus oil. These refreshing agents may be used alone or in combination of two or more.
- preservatives examples include sorbic acid or a salt thereof, benzoic acid or a salt thereof, methyl paraoxybenzoate, ethyl paraoxybenzoate, propyl paraoxybenzoate, chlorobutanol, chlorhexidine gluconate, boric acid, dehydroacetic acid or a salt thereof Benzalkonium chloride, benzethonium chloride, benzyl alcohol, zinc chloride, parachlorometaxylenol, chlorcresol, phenethyl alcohol, polydronium chloride, thimerosal, dibutylhydroxytoluene and the like. These preservatives may be used individually by 1 type, and may be used in combination of 2 or more type.
- stabilizer examples include polyvinyl pyrrolidone, sulfite, monoethanolamine, glycerin, propylene glycol, cyclodextrin, dextran, ascorbic acid, edetate, taurine, tocopherol, dibutylhydroxytoluene and the like. These stabilizers may be used individually by 1 type, and may be used in combination of 2 or more type.
- surfactant examples include nonionic surfactants such as tyloxapol, polyoxyethylene hydrogenated castor oil, polyoxyethylene polyoxypropylene block copolymer, polyoxyethylene sorbitan fatty acid ester, octoxynol; alkyldiaminoethylglycine, Amphoteric surfactants such as lauryldimethylaminoacetic acid betaine; anionic surfactants such as alkyl sulfate, N-acyl taurate, polyoxyethylene alkyl ether phosphate, polyoxyethylene alkyl ether sulfate; alkyl pyridinium salts; And cationic surfactants such as alkylamine salts. These surfactants may be used individually by 1 type, and may be used in combination of 2 or more type.
- nonionic surfactants such as tyloxapol, polyoxyethylene hydrogenated castor oil, polyoxyethylene polyoxypropylene block copolymer, polyoxyethylene sorbitan fatty
- concentration of these additives is appropriately set according to the type of additive and the use of the ophthalmic composition for zwitterionic SCL.
- the formulation form of the ophthalmic composition for zwitterionic SCL of the present invention is not limited as long as it contains water as a base, and may be any of an aqueous solution, an emulsion, etc., preferably an aqueous solution. Is mentioned.
- the ophthalmic composition for zwitterionic SCL of the present invention may be produced according to a known preparation method according to its use, for example, using the method described in the 16th revised Japanese Pharmacopeia General Rules for Preparation. can do.
- the ophthalmic composition for zwitterionic SCL of the present invention comprises eye drops that can be instilled even while wearing zwitterionic SCL (eye drops for zwitterionic SCL); eyewash that can be washed even while wearing zwitterionic SCL (zwitterionic) SCL eyewash); used as a contact lens care product such as a zwitterionic SCL mounting solution, a zwitterionic SCL multipurpose solution, a zwitterionic SCL cleaning solution, and a zwitterionic SCL storage solution.
- a contact lens care product such as a zwitterionic SCL mounting solution, a zwitterionic SCL multipurpose solution, a zwitterionic SCL cleaning solution, and a zwitterionic SCL storage solution.
- the zwitterionic SCL to which the present invention is applied is an SCL composed of a polymer containing a monomer containing a cationic group and a monomer containing an anionic group as an ionic monomer.
- Specific examples of the zwitterionic SCL include SCLs composed of a polymer containing a cationic group such as a quaternary ammonium salt and an anionic group such as a carboxyl group, a sulfonic acid group, and a phosphoric acid group.
- the material and production method thereof are described in, for example, JP-A-10-197831.
- the zwitterionic SCL to which the present invention is applied may have either a high water content or a low water content, but preferably a high water content, that is, a group IV ( Examples thereof include those classified into ionic monomers of 1 mol% or more and water content of 50% or more.
- the present invention relates to an ophthalmic composition for zwitterionic SCL containing pranoprofen and / or a pharmaceutically acceptable salt thereof, containing trometamol and adjusting the pH to 5.5 or more.
- a method for suppressing adsorption of pranoprofen and / or a salt thereof to a zwitterionic SCL which is characterized.
- the adsorption inhibiting method is useful for imparting the adsorption inhibiting action of pranoprofen and / or a salt thereof to the zwitterionic SCL to the ophthalmic composition for zwitterionic SCL.
- the type and concentration of pranoprofen and / or pharmaceutically acceptable salt thereof, the concentration of trometamol, the pH of the ophthalmic composition for zwitterionic SCL, the zwitterionic SCL The types of pharmacological components and additives to be blended in the ophthalmic composition, the formulation form and use of the zwitterionic SCL ophthalmic composition, the type of zwitterionic SCL to be applied, etc. As described in the column of “ophthalmic composition for zwitterionic SCL”.
- the present invention also includes a step of contacting a zwitterionic SCL with a solution containing pranoprofen and / or a pharmaceutically acceptable salt thereof and trometamol and having a pH of 5.5 or more.
- the present invention provides a method for suppressing adsorption of pranoprofen and / or a salt thereof to zwitterionic SCL.
- the type and concentration of pranoprofen and / or its pharmaceutically acceptable salt, the concentration of trometamol, the pH of the solution, the types of pharmacological ingredients and additives incorporated in the solution The formulation form and use of the liquid agent, the type of zwitterionic SCL to be applied, and the like are as described in the column of “1. Ophthalmic composition for zwitterionic SCL”. Moreover, what is necessary is just to set suitably the method of making the said liquid agent contact zwitterionic SCL in the adsorption
- pranoprofen is manufactured by API Corporation
- trometamol is trometamol (UE-E) (manufactured by Kanto Chemical Co., Inc.) or special grade tris (hydroxymethyl) amino. Methane (manufactured by Nacalai Tesque) was used.
- Test example 1 The test liquid was prepared by mixing each component shown in Table 1 by a conventional method. While observing the appearance of each of the obtained test solutions, the presence or absence of white turbidity was evaluated by measuring the turbidity (absorbance at 660 nm).
- each test solution was put in a vial, and one SCL was immersed in it, and shaken at 25 ° C. for 2 hours or more. Further, 2 mL of each test solution was put in a vial and shaken at 25 ° C. for 2 hours or more without immersing SCL.
- the pranoprofen content in each test solution was measured by liquid chromatography, and the amount of pranoprofen adsorbed on SCL was calculated according to the following formula.
- the shaking time is set to 2 hours or more, pranoprofen on SCL is reached. It has been confirmed that there is no effect on the measured value of the amount of adsorbed.
- Lens 1 Group IV, trade name “Seed 1dayPure” (registered trademark) manufactured by Seed Co., Ltd.), zwitterionic, lens material: 2-hydroxyethyl methacrylate (HEMA), quaternary ammonium group-containing methacrylate compound, Carboxyl group-containing methacrylate compounds, methyl methacrylate (MMA), ethylene glycol dimethacrylate (EGDMA)
- Lens 2 Group IV, trade name “Seed 1dayPure UP” (registered trademark) manufactured by Seed Co., Ltd.), zwitterionic, lens material: 2-hydroxyethyl methacrylate (HEMA), quaternary ammonium group -Containing methacrylate compounds, carboxyl group-containing methacrylate compounds, methyl methacrylate (MMA), ethylene glycol dimethacrylate (EGDMA)
- Lens 3 Group IV, trade name “Seed 1dayPure” (registered trademark) manufactured by Seed Co., Ltd.), zwitterio
- Test example 2 A test solution was prepared by mixing each component shown in Table 2 by a conventional method. While observing the appearance of each of the obtained test solutions, the presence or absence of white turbidity was evaluated by measuring the turbidity (absorbance at 660 nm). Further, the amount of pranoprofen adsorbed on zwitterionic SCL was measured for each of the obtained test solutions by the same method as in Test Example 1.
- Table 2 shows the results obtained. From this result, it was confirmed that when the pH was 4.5 or less, the test solution became cloudy and the appearance property was deteriorated, but at pH 5.5 or more, a clear appearance property was exhibited. In addition, as the pH increased, the amount of pranoprofen adsorbed on zwitterionic SCL tended to increase, but in the test solution containing trometamol, pranoprofen adsorbed on zwitterionic SCL. was effectively suppressed. From the above results, it was confirmed that by containing trometamol together with pranoprofen and having a pH of 5.5 or more, it has a clear appearance and can suppress the adsorption of pranoprofen to zwitterionic SCL. It was.
- Test example 3 A test solution was prepared by mixing each component shown in Table 3 by a conventional method. While observing the appearance of each of the obtained test solutions, the presence or absence of white turbidity was evaluated by measuring the turbidity (absorbance at 660 nm). Further, the amount of pranoprofen adsorbed on zwitterionic SCL was measured for each of the obtained test solutions by the same method as in Test Example 1. In this test, as the zwitterionic SCL, the lens 2 (group IV, zwitterionic) used in Test Example 1 was used.
- Table 3 shows the obtained results. As is apparent from Table 3, even when a buffer component other than trometamol was used, the amount of pranoprofen adsorbed on zwitterionic SCL could not be sufficiently reduced. That is, from this test result, it is clear that the suppression of pranoprofen adsorption to zwitterionic SCL is a unique effect recognized by selecting trometamol as a component and setting the pH to 5.5 or higher. became.
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Abstract
Priority Applications (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
RU2015154023A RU2669570C2 (ru) | 2013-05-30 | 2014-05-27 | Офтальмологическая композиция для цвиттерионных мягких контактных линз |
JP2015519868A JP6401699B2 (ja) | 2013-05-30 | 2014-05-27 | 両性イオン性ソフトコンタクトレンズ用眼科用組成物 |
CN201480029909.8A CN105392481B (zh) | 2013-05-30 | 2014-05-27 | 两性离子性软性隐形眼镜用眼科用组合物 |
HK16105849.4A HK1217901A1 (zh) | 2013-05-30 | 2016-05-23 | 兩性離子性軟性隱形眼鏡用眼科用組合物 |
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PCT/JP2014/063960 WO2014192738A1 (fr) | 2013-05-30 | 2014-05-27 | Compositions ophtalmiques pour lentilles de contact souples zwittérioniques |
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JP (1) | JP6401699B2 (fr) |
CN (1) | CN105392481B (fr) |
HK (1) | HK1217901A1 (fr) |
RU (1) | RU2669570C2 (fr) |
TW (1) | TWI623314B (fr) |
WO (1) | WO2014192738A1 (fr) |
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TWI630931B (zh) * | 2017-04-10 | 2018-08-01 | 明基材料股份有限公司 | 眼用鏡片及其製造方法 |
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JPH08291065A (ja) * | 1995-04-20 | 1996-11-05 | Santen Pharmaceut Co Ltd | 有機アミンを配合したプラノプロフェン点眼液 |
JP2007008928A (ja) * | 2005-06-01 | 2007-01-18 | Rohto Pharmaceut Co Ltd | アシタザノラスト含有水性組成物 |
WO2007077783A1 (fr) * | 2005-12-27 | 2007-07-12 | Lion Corporation | Composition pour lentilles de contact souples et procede permettant la suppression de l’adsorption |
JP2011098960A (ja) * | 2009-10-09 | 2011-05-19 | Rohto Pharmaceutical Co Ltd | 水性組成物 |
JP2013010754A (ja) * | 2011-06-02 | 2013-01-17 | Rohto Pharmaceutical Co Ltd | トラニラストを含有する水性組成物 |
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JP4919666B2 (ja) * | 2005-01-26 | 2012-04-18 | ロート製薬株式会社 | プラノプロフェン含有組成物 |
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2014
- 2014-05-27 CN CN201480029909.8A patent/CN105392481B/zh not_active Expired - Fee Related
- 2014-05-27 RU RU2015154023A patent/RU2669570C2/ru not_active IP Right Cessation
- 2014-05-27 JP JP2015519868A patent/JP6401699B2/ja not_active Expired - Fee Related
- 2014-05-27 WO PCT/JP2014/063960 patent/WO2014192738A1/fr active Application Filing
- 2014-05-29 TW TW103118779A patent/TWI623314B/zh not_active IP Right Cessation
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2016
- 2016-05-23 HK HK16105849.4A patent/HK1217901A1/zh unknown
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JPH08291065A (ja) * | 1995-04-20 | 1996-11-05 | Santen Pharmaceut Co Ltd | 有機アミンを配合したプラノプロフェン点眼液 |
JP2007008928A (ja) * | 2005-06-01 | 2007-01-18 | Rohto Pharmaceut Co Ltd | アシタザノラスト含有水性組成物 |
WO2007077783A1 (fr) * | 2005-12-27 | 2007-07-12 | Lion Corporation | Composition pour lentilles de contact souples et procede permettant la suppression de l’adsorption |
JP2011098960A (ja) * | 2009-10-09 | 2011-05-19 | Rohto Pharmaceutical Co Ltd | 水性組成物 |
JP2013010754A (ja) * | 2011-06-02 | 2013-01-17 | Rohto Pharmaceutical Co Ltd | トラニラストを含有する水性組成物 |
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HIROE ITAKURA ET AL.: "Interaction with Zwitterionic Soft Contact Lens (SEED 2week Pure) and Ketotifen Fumarate Opthalmic Solution (Zaditen, Zaditen UD", JOURNAL OF THE EYE, vol. 23, no. 8, 2006, pages 1058 - 1061 * |
NOBUHITO TABUCHI ET AL.: "Adsorption of Actives in Ophthalmological Drugs for Over-The-Counter on Soft Contact Lens Surfaces", JOURNAL OF OLEO SCIENCE, vol. 58, no. 1, 2009, pages 43 - 52, XP009123928 * |
TORU MATSUNAGA ET AL.: "Ryosei Ion-sei SCL (SEED 2week Pure) no Tengan'yaku Tekigosei ni Kansuru Kenkyu (II", DAI 48 KAI JAPAN CONTACT LENS SOCIETY SOKAI, 2005, pages 89, 5 - 09 * |
YOSHIKO YAMAZAKI ET AL.: "Analysis and evaluation of the ionic interaction of the novel soft contact lenses using the zwitterionic polymer gel", JOURNAL OF APPLIED POLYMER SCIENCE, vol. 114, no. 5, 2009, pages 2764 - 2768 * |
Also Published As
Publication number | Publication date |
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RU2669570C2 (ru) | 2018-10-12 |
CN105392481A (zh) | 2016-03-09 |
RU2015154023A3 (fr) | 2018-03-14 |
CN105392481B (zh) | 2018-10-12 |
JP6401699B2 (ja) | 2018-10-10 |
HK1217901A1 (zh) | 2017-01-27 |
RU2015154023A (ru) | 2017-07-06 |
TW201517904A (zh) | 2015-05-16 |
JPWO2014192738A1 (ja) | 2017-02-23 |
TWI623314B (zh) | 2018-05-11 |
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