JP2009086619A - Contact lens fitting liquid - Google Patents
Contact lens fitting liquid Download PDFInfo
- Publication number
- JP2009086619A JP2009086619A JP2008041710A JP2008041710A JP2009086619A JP 2009086619 A JP2009086619 A JP 2009086619A JP 2008041710 A JP2008041710 A JP 2008041710A JP 2008041710 A JP2008041710 A JP 2008041710A JP 2009086619 A JP2009086619 A JP 2009086619A
- Authority
- JP
- Japan
- Prior art keywords
- contact lens
- lens mounting
- acid
- mounting liquid
- component
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 239000007788 liquid Substances 0.000 title claims abstract description 89
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 claims abstract description 15
- 150000001413 amino acids Chemical class 0.000 claims abstract description 15
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 claims abstract description 13
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims abstract description 13
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims abstract description 13
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims abstract description 13
- 239000004354 Hydroxyethyl cellulose Substances 0.000 claims abstract description 12
- 239000004372 Polyvinyl alcohol Substances 0.000 claims abstract description 8
- 229920002451 polyvinyl alcohol Polymers 0.000 claims abstract description 8
- 150000003839 salts Chemical class 0.000 claims description 33
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims description 22
- -1 fatty acid esters Chemical class 0.000 claims description 21
- 239000000463 material Substances 0.000 claims description 18
- 235000001014 amino acid Nutrition 0.000 claims description 15
- 239000004359 castor oil Substances 0.000 claims description 11
- XOAAWQZATWQOTB-UHFFFAOYSA-N taurine Chemical compound NCCS(O)(=O)=O XOAAWQZATWQOTB-UHFFFAOYSA-N 0.000 claims description 9
- SLXKOJJOQWFEFD-UHFFFAOYSA-N 6-aminohexanoic acid Chemical compound NCCCCCC(O)=O SLXKOJJOQWFEFD-UHFFFAOYSA-N 0.000 claims description 8
- 229960002684 aminocaproic acid Drugs 0.000 claims description 8
- 239000002736 nonionic surfactant Substances 0.000 claims description 8
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- 229920001214 Polysorbate 60 Polymers 0.000 claims description 7
- 239000012530 fluid Substances 0.000 claims description 7
- KIUKXJAPPMFGSW-DNGZLQJQSA-N (2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5S,6R)-3-Acetamido-2-[(2S,3S,4R,5R,6R)-6-[(2R,3R,4R,5S,6R)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 KIUKXJAPPMFGSW-DNGZLQJQSA-N 0.000 claims description 5
- 229920002674 hyaluronan Polymers 0.000 claims description 5
- 229960003160 hyaluronic acid Drugs 0.000 claims description 5
- 239000000017 hydrogel Substances 0.000 claims description 5
- SQDAZGGFXASXDW-UHFFFAOYSA-N 5-bromo-2-(trifluoromethoxy)pyridine Chemical compound FC(F)(F)OC1=CC=C(Br)C=N1 SQDAZGGFXASXDW-UHFFFAOYSA-N 0.000 claims description 4
- 229920001287 Chondroitin sulfate Polymers 0.000 claims description 4
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims description 4
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- OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 claims description 4
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- 235000014113 dietary fatty acids Nutrition 0.000 claims description 4
- 239000000194 fatty acid Substances 0.000 claims description 4
- 229930195729 fatty acid Natural products 0.000 claims description 4
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims description 4
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- 229920002503 polyoxyethylene-polyoxypropylene Polymers 0.000 claims description 4
- 229940068968 polysorbate 80 Drugs 0.000 claims description 4
- 229920000053 polysorbate 80 Polymers 0.000 claims description 4
- 235000002639 sodium chloride Nutrition 0.000 description 36
- 239000000243 solution Substances 0.000 description 21
- 230000000052 comparative effect Effects 0.000 description 20
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- 238000000034 method Methods 0.000 description 19
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- 239000000203 mixture Substances 0.000 description 14
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- 239000002253 acid Substances 0.000 description 12
- 238000007654 immersion Methods 0.000 description 12
- 239000000872 buffer Substances 0.000 description 10
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- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 8
- 239000006172 buffering agent Substances 0.000 description 8
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- 238000009472 formulation Methods 0.000 description 8
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 description 8
- 210000004087 cornea Anatomy 0.000 description 7
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 6
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 description 6
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 6
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- YKZPPPNXRZHVGX-PXYKVGKMSA-L dipotassium;(2s)-2-aminobutanedioate;hydron;hydrate Chemical compound [H+].[H+].O.[K+].[K+].[O-]C(=O)[C@@H](N)CC([O-])=O.[O-]C(=O)[C@@H](N)CC([O-])=O YKZPPPNXRZHVGX-PXYKVGKMSA-L 0.000 description 5
- 238000011156 evaluation Methods 0.000 description 5
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 description 5
- 239000003921 oil Substances 0.000 description 5
- 235000019198 oils Nutrition 0.000 description 5
- 230000003204 osmotic effect Effects 0.000 description 5
- 229940068988 potassium aspartate Drugs 0.000 description 5
- 230000002829 reductive effect Effects 0.000 description 5
- 101100365013 Arabidopsis thaliana SCL3 gene Proteins 0.000 description 4
- BTBUEUYNUDRHOZ-UHFFFAOYSA-N Borate Chemical compound [O-]B([O-])[O-] BTBUEUYNUDRHOZ-UHFFFAOYSA-N 0.000 description 4
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 description 4
- 239000004471 Glycine Substances 0.000 description 4
- 229920002683 Glycosaminoglycan Polymers 0.000 description 4
- 229910019142 PO4 Inorganic materials 0.000 description 4
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 description 4
- 229910052783 alkali metal Inorganic materials 0.000 description 4
- 229910000147 aluminium phosphate Inorganic materials 0.000 description 4
- 239000007864 aqueous solution Substances 0.000 description 4
- 229910021538 borax Inorganic materials 0.000 description 4
- 239000003795 chemical substances by application Substances 0.000 description 4
- OSASVXMJTNOKOY-UHFFFAOYSA-N chlorobutanol Chemical compound CC(C)(O)C(Cl)(Cl)Cl OSASVXMJTNOKOY-UHFFFAOYSA-N 0.000 description 4
- 229960001983 magnesium aspartate Drugs 0.000 description 4
- 239000000178 monomer Substances 0.000 description 4
- 235000021317 phosphate Nutrition 0.000 description 4
- 235000010339 sodium tetraborate Nutrition 0.000 description 4
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 description 3
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 description 3
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 description 3
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 3
- 235000006679 Mentha X verticillata Nutrition 0.000 description 3
- 235000002899 Mentha suaveolens Nutrition 0.000 description 3
- 235000001636 Mentha x rotundifolia Nutrition 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 description 3
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- 150000007513 acids Chemical class 0.000 description 3
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- 235000004279 alanine Nutrition 0.000 description 3
- 229910052784 alkaline earth metal Inorganic materials 0.000 description 3
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- 229920001400 block copolymer Polymers 0.000 description 3
- KXKPYJOVDUMHGS-OSRGNVMNSA-N chondroitin sulfate Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](OS(O)(=O)=O)[C@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](C(O)=O)O1 KXKPYJOVDUMHGS-OSRGNVMNSA-N 0.000 description 3
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- 239000001816 polyoxyethylene sorbitan tristearate Substances 0.000 description 1
- 229920001451 polypropylene glycol Polymers 0.000 description 1
- 229940068977 polysorbate 20 Drugs 0.000 description 1
- 229940113124 polysorbate 60 Drugs 0.000 description 1
- 229940099511 polysorbate 65 Drugs 0.000 description 1
- 235000011056 potassium acetate Nutrition 0.000 description 1
- 239000001103 potassium chloride Substances 0.000 description 1
- 235000011164 potassium chloride Nutrition 0.000 description 1
- 239000001508 potassium citrate Substances 0.000 description 1
- 229960002635 potassium citrate Drugs 0.000 description 1
- QEEAPRPFLLJWCF-UHFFFAOYSA-K potassium citrate (anhydrous) Chemical compound [K+].[K+].[K+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O QEEAPRPFLLJWCF-UHFFFAOYSA-K 0.000 description 1
- 235000011082 potassium citrates Nutrition 0.000 description 1
- 235000010241 potassium sorbate Nutrition 0.000 description 1
- 239000004302 potassium sorbate Substances 0.000 description 1
- 229940069338 potassium sorbate Drugs 0.000 description 1
- NMMVKSMGBDRONO-UHFFFAOYSA-N potassium;9-methyl-3-(1,2,4-triaza-3-azanidacyclopenta-1,4-dien-5-yl)pyrido[1,2-a]pyrimidin-4-one Chemical compound [K+].CC1=CC=CN(C2=O)C1=NC=C2C1=NN=N[N-]1 NMMVKSMGBDRONO-UHFFFAOYSA-N 0.000 description 1
- JVUYWILPYBCNNG-UHFFFAOYSA-N potassium;oxido(oxo)borane Chemical compound [K+].[O-]B=O JVUYWILPYBCNNG-UHFFFAOYSA-N 0.000 description 1
- 229960003101 pranoprofen Drugs 0.000 description 1
- 229960001309 procaine hydrochloride Drugs 0.000 description 1
- 229960001371 proparacaine hydrochloride Drugs 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 235000013772 propylene glycol Nutrition 0.000 description 1
- 235000007682 pyridoxal 5'-phosphate Nutrition 0.000 description 1
- 239000011589 pyridoxal 5'-phosphate Substances 0.000 description 1
- 229960001327 pyridoxal phosphate Drugs 0.000 description 1
- ZUFQODAHGAHPFQ-UHFFFAOYSA-N pyridoxine hydrochloride Chemical compound Cl.CC1=NC=C(CO)C(CO)=C1O ZUFQODAHGAHPFQ-UHFFFAOYSA-N 0.000 description 1
- 229960004172 pyridoxine hydrochloride Drugs 0.000 description 1
- 235000019171 pyridoxine hydrochloride Nutrition 0.000 description 1
- 239000011764 pyridoxine hydrochloride Substances 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 229960000342 retinol acetate Drugs 0.000 description 1
- QGNJRVVDBSJHIZ-QHLGVNSISA-N retinyl acetate Chemical compound CC(=O)OC\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C QGNJRVVDBSJHIZ-QHLGVNSISA-N 0.000 description 1
- 235000019173 retinyl acetate Nutrition 0.000 description 1
- 239000011770 retinyl acetate Substances 0.000 description 1
- 229940108325 retinyl palmitate Drugs 0.000 description 1
- 235000019172 retinyl palmitate Nutrition 0.000 description 1
- 239000011769 retinyl palmitate Substances 0.000 description 1
- XWGJFPHUCFXLBL-UHFFFAOYSA-M rongalite Chemical compound [Na+].OCS([O-])=O XWGJFPHUCFXLBL-UHFFFAOYSA-M 0.000 description 1
- 239000010666 rose oil Substances 0.000 description 1
- 235000019719 rose oil Nutrition 0.000 description 1
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 description 1
- 230000001953 sensory effect Effects 0.000 description 1
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- 229910001961 silver nitrate Inorganic materials 0.000 description 1
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- GQTHJBOWLPZUOI-FJXQXJEOSA-M sodium D-pantothenate Chemical compound [Na+].OCC(C)(C)[C@@H](O)C(=O)NCCC([O-])=O GQTHJBOWLPZUOI-FJXQXJEOSA-M 0.000 description 1
- WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 description 1
- 239000004299 sodium benzoate Substances 0.000 description 1
- 235000010234 sodium benzoate Nutrition 0.000 description 1
- 229960003885 sodium benzoate Drugs 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 239000001509 sodium citrate Substances 0.000 description 1
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 1
- 235000019259 sodium dehydroacetate Nutrition 0.000 description 1
- 229940079839 sodium dehydroacetate Drugs 0.000 description 1
- HRZFUMHJMZEROT-UHFFFAOYSA-L sodium disulfite Chemical compound [Na+].[Na+].[O-]S(=O)S([O-])(=O)=O HRZFUMHJMZEROT-UHFFFAOYSA-L 0.000 description 1
- 229940037001 sodium edetate Drugs 0.000 description 1
- 235000010267 sodium hydrogen sulphite Nutrition 0.000 description 1
- 235000011121 sodium hydroxide Nutrition 0.000 description 1
- 235000010262 sodium metabisulphite Nutrition 0.000 description 1
- 229940068459 sodium pantothenate Drugs 0.000 description 1
- 235000010265 sodium sulphite Nutrition 0.000 description 1
- AKHNMLFCWUSKQB-UHFFFAOYSA-L sodium thiosulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=S AKHNMLFCWUSKQB-UHFFFAOYSA-L 0.000 description 1
- 235000019345 sodium thiosulphate Nutrition 0.000 description 1
- DSOWAKKSGYUMTF-GZOLSCHFSA-M sodium;(1e)-1-(6-methyl-2,4-dioxopyran-3-ylidene)ethanolate Chemical compound [Na+].C\C([O-])=C1/C(=O)OC(C)=CC1=O DSOWAKKSGYUMTF-GZOLSCHFSA-M 0.000 description 1
- WTWSHHITWMVLBX-DKWTVANSSA-M sodium;(2s)-2-aminobutanedioate;hydron Chemical compound [Na+].[O-]C(=O)[C@@H](N)CC(O)=O WTWSHHITWMVLBX-DKWTVANSSA-M 0.000 description 1
- JGMJQSFLQWGYMQ-UHFFFAOYSA-M sodium;2,6-dichloro-n-phenylaniline;acetate Chemical compound [Na+].CC([O-])=O.ClC1=CC=CC(Cl)=C1NC1=CC=CC=C1 JGMJQSFLQWGYMQ-UHFFFAOYSA-M 0.000 description 1
- GEYJUFBPCGDENK-UHFFFAOYSA-M sodium;3,8-dimethyl-5-propan-2-ylazulene-1-sulfonate Chemical compound [Na+].CC(C)C1=CC=C(C)C2=C(S([O-])(=O)=O)C=C(C)C2=C1 GEYJUFBPCGDENK-UHFFFAOYSA-M 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 235000010199 sorbic acid Nutrition 0.000 description 1
- 239000004334 sorbic acid Substances 0.000 description 1
- 229940075582 sorbic acid Drugs 0.000 description 1
- 235000011076 sorbitan monostearate Nutrition 0.000 description 1
- 239000001587 sorbitan monostearate Substances 0.000 description 1
- 229940035048 sorbitan monostearate Drugs 0.000 description 1
- 235000011078 sorbitan tristearate Nutrition 0.000 description 1
- 239000001589 sorbitan tristearate Substances 0.000 description 1
- 229960004129 sorbitan tristearate Drugs 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 235000010356 sorbitol Nutrition 0.000 description 1
- 235000019721 spearmint oil Nutrition 0.000 description 1
- 239000012086 standard solution Substances 0.000 description 1
- 230000001954 sterilising effect Effects 0.000 description 1
- 238000004659 sterilization and disinfection Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 229940086735 succinate Drugs 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 description 1
- 125000001174 sulfone group Chemical group 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-N sulfuric acid Substances OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 1
- 150000003467 sulfuric acid derivatives Chemical class 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- 229960003080 taurine Drugs 0.000 description 1
- 150000003505 terpenes Chemical class 0.000 description 1
- 235000007586 terpenes Nutrition 0.000 description 1
- 229960002494 tetracaine hydrochloride Drugs 0.000 description 1
- BJORNXNYWNIWEY-UHFFFAOYSA-N tetrahydrozoline hydrochloride Chemical compound Cl.N1CCN=C1C1C2=CC=CC=C2CCC1 BJORNXNYWNIWEY-UHFFFAOYSA-N 0.000 description 1
- 229940021790 tetrahydrozoline hydrochloride Drugs 0.000 description 1
- 235000010384 tocopherol Nutrition 0.000 description 1
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- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 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
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- BSVBQGMMJUBVOD-UHFFFAOYSA-N trisodium borate Chemical compound [Na+].[Na+].[Na+].[O-]B([O-])[O-] BSVBQGMMJUBVOD-UHFFFAOYSA-N 0.000 description 1
- 229960000281 trometamol Drugs 0.000 description 1
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- 239000000341 volatile oil Substances 0.000 description 1
- 239000000811 xylitol Substances 0.000 description 1
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- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 1
- 229960002675 xylitol Drugs 0.000 description 1
- 239000011576 zinc lactate Substances 0.000 description 1
- 235000000193 zinc lactate Nutrition 0.000 description 1
- 229940050168 zinc lactate Drugs 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
Landscapes
- Eyeglasses (AREA)
- Compositions Of Macromolecular Compounds (AREA)
Abstract
Description
本発明は、コンタクトレンズが眼に及ぼす影響を軽減するためのコンタクトレンズ装着液に関し、さらに詳しくは、コンタクトレンズ装着時の使用感及び安全性が向上されたコンタクトレンズ装着液に関する。 The present invention relates to a contact lens mounting liquid for reducing the influence of a contact lens on the eyes, and more particularly to a contact lens mounting liquid with improved usability and safety when the contact lens is mounted.
近年、視力矯正や美容を目的として、コンタクトレンズが目覚しく普及している。コンタクトレンズは、涙液の存在下とは言え角膜に直接接触させて使用しなければならない特性から、装着時にコンタクトレンズと角膜との間でクッションとしての役割を果たすコンタクトレンズ装着液(以下、単に「装着液」と表記する事もある)を使用する人も多い。一方、コンタクトレンズ装着液を使用する事によって生じる問題点も提起されている。例えば、装着時の不快感(ベタベタ感など)や、装着直後に視界がぼやける事などの問題点が知られている(特許文献1、特許文献2)。また、多くのコンタクトレンズ使用者は、手指でコンタクトレンズを目に装着するが、コンタクトレンズ装着液の液性によっては、指先からレンズが離れ難くなって適切に装着できなかったり、逆にレンズが指から滑り落ちてしまう、あるいは指先からレンズを介してゴミや汚れ等が目に入ってしまう等の問題点もある。 In recent years, contact lenses have been remarkably widespread for the purposes of vision correction and beauty. A contact lens is a contact lens mounting liquid (hereinafter simply referred to as a cushion between the contact lens and the cornea when worn) due to the property that it must be used in direct contact with the cornea even in the presence of tears. Many people use "wearing fluid"). On the other hand, problems caused by using contact lens mounting liquid have also been raised. For example, there are known problems such as discomfort (such as a sticky feeling) at the time of wearing and blurring of the field of view immediately after wearing (Patent Documents 1 and 2). In addition, many contact lens users wear contact lenses with their fingers, but depending on the liquid nature of the contact lens mounting solution, the lens may not be able to be worn properly due to the difficulty of separating the lens from the fingertip. There are also problems such as slipping off the finger, or dust or dirt entering the eye from the fingertip through the lens.
本発明者らは、優れたコンタクトレンズ装着液を開発するために研究を重ねる過程で、装着液を使用してコンタクトレンズを装着した際に生じるゴロゴロ感や異物感、さらにはコンタクトレンズの装着し難さ等の問題の一因が、コンタクトレンズ装着液自体の液性や、コンタクトレンズとコンタクトレンズ装着液との組み合わせに関係しているという知見を得た。
そこで、本発明は、コンタクトレンズ装着液を使用してコンタクトレンズを装着した際の異物感・ゴロゴロ感が低減されており、コンタクトレンズ装着直後の視界が良好であり、かつ、使用者に、コンタクトレンズが角膜上に安定に保持されているとの自覚を与えるようなコンタクタクトレンズ装着液を提供することを目的としている。
また、本発明は、コンタクトレンズの眼への装着を容易にするという、コンタクトレンズ装着液の機能をより高めたコンタクタクトレンズ装着液を提供することを目的とするものである。
さらに、本発明は、手指の汚れがコンタクトレンズに付着し難く、安全性が高いのみならず、装着後に指に残る液の感触も良好なコンタクトレンズ装着液を提供することをも目的とするものである。
要するに、本発明は、コンタクトレンズの装着を円滑かつ安全に行うことができ、装着後もレンズを気持ちよく安定的に保持することができ、しかもレンズへの汚れの付着が抑制され、使用しやすいコンタクトレンズ装着液を提供することを目的とするものである。
In the process of repeated research to develop an excellent contact lens mounting solution, the present inventors have found that the contact lens is worn out and a foreign object, and that the contact lens is mounted. It was found that one of the causes such as difficulty is related to the liquidity of the contact lens mounting liquid itself and the combination of the contact lens and the contact lens mounting liquid.
Therefore, the present invention reduces the feeling of foreign matter and lingering feeling when a contact lens is mounted using a contact lens mounting liquid, has a good field of view immediately after the contact lens is mounted, and provides a contact to the user. It is an object of the present invention to provide a contact lens mounting liquid that gives a sense that the lens is stably held on the cornea.
It is another object of the present invention to provide a contact lens mounting liquid that further enhances the function of the contact lens mounting liquid, which facilitates mounting of the contact lens on the eye.
It is another object of the present invention to provide a contact lens mounting solution that is not only difficult to adhere to contact lenses and is highly safe, but also has a good feel of the liquid remaining on the finger after mounting. It is.
In short, the present invention makes it possible to smoothly and safely attach a contact lens, hold the lens comfortably and stably even after wearing, and the adhesion of dirt to the lens is suppressed, making contact easy to use. The object is to provide a lens mounting liquid.
本発明者らは、(A)ヒドロキシエチルセルロース、(B)アミノ酸類を含有し、実質的に(Z)ポリビニルピロリドン又はポリビニルアルコールを含まない、コンタクトレンズ装着液が、上記の課題を解決する優れた特性を有することを見出し、本発明を完成するに至った。 The present inventors have (A) hydroxyethyl cellulose, (B) amino acids, and a contact lens mounting liquid that substantially does not contain (Z) polyvinyl pyrrolidone or polyvinyl alcohol, which solves the above problems. It has been found that it has characteristics, and the present invention has been completed.
すなわち本発明は、下記に掲げる発明である。
(1)(A)ヒドロキシエチルセルロース、(B)アミノ酸類を含有し、実質的に(Z)ポリビニルピロリドン又はポリビニルアルコールを含まない、コンタクトレンズ装着液。
(2)(A)成分を0.0001〜25(w/v)%の割合で含有する、(1)に記載のコンタクトレンズ装着液。
(3)(B)成分が、コンドロイチン硫酸、ヒアルロン酸、アスパラギン酸、アミノエチルスルホン酸、イプシロンアミノカプロン酸、及びそれらの塩からなる群より選択される1種以上である、(1)又は(2)に記載のコンタクトレンズ装着液。
(4)(B)成分を0.0001〜10(w/v)%の割合で含有する、(1)〜(3)のいずれかに記載のコンタクトレンズ装着液。
(5)さらに(C)成分として非イオン性界面活性剤を含有する、(1)〜(4)のいずれかに記載のコンタクトレンズ装着液。
(6)(C)成分が、ポリオキシエチレンソルビタン脂肪酸エステル類、ポリオキシエチレン硬化ヒマシ油類及びポリオキシエチレンポリオキシプロピレン共重合体からなる群より選択される1種以上である、(5)に記載のコンタクトレンズ装着液。
(7)(C)成分が、ポリソルベート80である、(5)に記載のコンタクトレンズ装着液。
(8)(C)成分を0.001〜5(w/v)%の割合で含有する、(5)〜(7)のいずれかに記載のコンタクトレンズ装着液。
(9)コンタクトレンズが、ソフトコンタクトレンズである、(1)〜(8)のいずれかに記載のコンタクトレンズ装着液。
(10)ソフトコンタクトレンズが、原則としてソフトコンタクトレンズ分類グループIVのソフトコンタクトレンズである、(9)に記載のコンタクトレンズ装着液。
(11)ソフトコンタクトレンズが、シリコーンハイドロゲルレンズ素材のソフトコンタクトレンズである、(9)に記載のコンタクトレンズ装着液。
That is, this invention is the invention hung up below.
(1) A contact lens mounting liquid containing (A) hydroxyethyl cellulose, (B) amino acids, and substantially free of (Z) polyvinyl pyrrolidone or polyvinyl alcohol.
(2) The contact lens mounting liquid according to (1), which contains the component (A) at a ratio of 0.0001 to 25 (w / v)%.
(3) The component (B) is at least one selected from the group consisting of chondroitin sulfate, hyaluronic acid, aspartic acid, aminoethylsulfonic acid, epsilon aminocaproic acid, and salts thereof, (1) or (2 ) Contact lens mounting fluid.
(4) The contact lens mounting liquid according to any one of (1) to (3), which contains the component (B) at a ratio of 0.0001 to 10 (w / v)%.
(5) The contact lens mounting liquid according to any one of (1) to (4), further containing a nonionic surfactant as a component (C).
(6) The component (C) is at least one selected from the group consisting of polyoxyethylene sorbitan fatty acid esters, polyoxyethylene hydrogenated castor oils, and polyoxyethylene polyoxypropylene copolymers, (5) Contact lens mounting fluid according to 1.
(7) The contact lens mounting liquid according to (5), wherein the component (C) is polysorbate 80.
(8) The contact lens mounting liquid according to any one of (5) to (7), wherein the component (C) is contained at a ratio of 0.001 to 5 (w / v)%.
(9) The contact lens mounting liquid according to any one of (1) to (8), wherein the contact lens is a soft contact lens.
(10) The contact lens mounting liquid according to (9), wherein the soft contact lens is in principle a soft contact lens of soft contact lens classification group IV.
(11) The contact lens mounting liquid according to (9), wherein the soft contact lens is a soft contact lens made of a silicone hydrogel lens material.
本発明のコンタクトレンズ装着液によれば、コンタクトレンズ装着時の異物感・ゴロゴロ感が低減されており、コンタクトレンズ装着直後の視界が良好であり、かつ、使用者は、レンズが角膜上に安定に保持されているとの自覚を得ることができる。また、本発明のコンタクトレンズ装着液はコンタクトレンズの眼への装着を容易にする機能に優れており、円滑にコンタクトレンズを装着することができる。さらに、本発明のコンタクトレンズ装着液によれば、手指の汚れがコンタクトレンズに付着し難く、安全性が高いのみならず、装着後に指に残る液の感触も良好である。
要するに、本発明のコンタクトレンズ装着液は、コンタクトレンズの装着を円滑かつ安全に行うことができ、装着後もレンズを気持ちよく安定的に保持することができ、しかもレンズへの汚れの付着が抑制され、使用しやすい等の優れた効果を奏する。
According to the contact lens mounting liquid of the present invention, the feeling of foreign matter and lingering feeling when the contact lens is mounted is reduced, the field of view immediately after the contact lens is mounted is good, and the user can stabilize the lens on the cornea You can get a sense of being held in. Further, the contact lens mounting liquid of the present invention has an excellent function of facilitating mounting of the contact lens on the eye, and can smoothly mount the contact lens. Furthermore, according to the contact lens mounting liquid of the present invention, dirt on the finger is difficult to adhere to the contact lens, and not only is safety high, but also the touch of the liquid remaining on the finger after mounting is good.
In short, the contact lens mounting liquid of the present invention can smoothly and safely mount the contact lens, can hold the lens comfortably and stably even after mounting, and the adhesion of dirt to the lens is suppressed. Excellent effects such as easy to use.
以下、本発明を詳細に説明する。
本明細書中、「装着」と言う表記は、コンタクトレンズを「目に着ける」行為(操作)を表し、「装用」と言う表記は、コンタクトレンズが「角膜上にある」状態を表す。
また、本明細書中、「%」と言う表記は、特記しない限りw/v%、即ち溶液100mLに溶けている各成分(溶質)の重量gを意味するものである。
さらに、「コンタクトレンズ」という語句は、特記しない限り、ハード、酸素透過性ハード、ソフト等のあらゆるタイプのコンタクトレンズを包含する意味で用いる。以下、「コンタクトレンズ」を単に「レンズ」と表記する事もある。
また、本明細書において、「ソフトコンタクトレンズ分類」とは、平成11年3月31日付医薬審第645号厚生労働省(当時の厚生省)医薬安全局審査管理課長通知「ソフトコンタクトレンズ及びソフトコンタクトレンズ用消毒剤の製造(輸入)承認申請に際し添付すべき資料の取り扱い等について」において規定された「ソフトコンタクトレンズの分類方法について」に基づくSCLの分類である。ここでは、ソフトコンタクトレンズは、含水率や陰イオンを有するモノマーのモル%等を基準として分類される。例えば、グループIVに属するSCLは、含水率が50%以上であり、原材料ポリマーの構成モノマーのうち陰イオンを有するモノマーのモル%が1%以上であることを共通の性質として有する。尚、本分類はFDA(米国食品医薬品局)が行なっているソフトコンタクトレンズの分類方法に従っている。
Hereinafter, the present invention will be described in detail.
In this specification, the expression “wearing” represents an action (operation) of “contacting” a contact lens, and the expression “wearing” represents a state where the contact lens is “on the cornea”.
In the present specification, the notation “%” means w / v%, that is, the weight g of each component (solute) dissolved in 100 mL of the solution unless otherwise specified.
Further, the term “contact lens” is used to include all types of contact lenses such as hard, oxygen-permeable hard, and soft unless otherwise specified. Hereinafter, “contact lens” may be simply referred to as “lens”.
In addition, in this specification, “Soft contact lens classification” means “Pharmaceutical Examination No. 645 dated March 31, 1999” by the Ministry of Health, Labor and Welfare (Ministry of Health, Labor and Welfare) This is an SCL classification based on “How to classify soft contact lenses” defined in “Handling of materials to be attached when applying for manufacturing (import) approval of antiseptics for medical use”. Here, soft contact lenses are classified on the basis of moisture content, mole% of monomers having anions, and the like. For example, SCLs belonging to Group IV have a common property that the moisture content is 50% or more, and the mole% of monomers having anions among the constituent monomers of the raw material polymer is 1% or more. This classification follows the classification method for soft contact lenses performed by the FDA (Food and Drug Administration).
また、「原則として」とは、材質、機能等の点で、当業者が該分類に属するものと同等と理解しうるソフトコンタクトレンズを包含することを意味する。 Further, "in principle" means that a soft contact lens that can be understood by those skilled in the art as being equivalent to those belonging to the classification in terms of materials, functions, and the like is included.
また、シリコーンハイドロゲル素材のコンタクトレンズとは、シリコーンを含有する素材(例えばシリコーンとアクリレートの重合体であるTRIS又はTRIS誘導体等)に親水性モノマー(例えばヒドロキエシエチルメタクリレート、ジメチルアクリルアミド等)を共重合させた素材を用いたコンタクトレンズであり、USAN(United State Adopted Name)に基づく素材の名称としては、例えばLotrafilconA、LotrafilconB、BalafilconA、GalyfilconA、SenofilconAなどが挙げられる。
さらに、本明細書において、「コンタクトレンズ装着液」とは、基本的にコンタクトレンズの装着を容易にし、かつ角膜とレンズの間のクッション作用を有する眼科用組成物を意味する。本明細書中「コンタクトレンズ装着液」は、単に「装着液」と表記する事もある。
A silicone hydrogel contact lens is a silicone-containing material (such as TRIS or a TRIS derivative that is a polymer of silicone and acrylate) and a hydrophilic monomer (such as hydroxyethyl methacrylate, dimethylacrylamide). Contact lenses using polymerized materials, and examples of names of materials based on USAN (United State Adopted Name) include Lotrafilcon A, Lotrafilcon B, Balafilcon A, Galyfilcon A, and Senofilcon A.
Further, in the present specification, “contact lens mounting liquid” means an ophthalmic composition that basically facilitates mounting of a contact lens and has a cushioning action between the cornea and the lens. In the present specification, “contact lens mounting liquid” may be simply referred to as “mounting liquid”.
本発明におけるコンタクトレンズ装着液は、(A)ヒドロキシエチルセルロース、(B)アミノ酸類を含有し、実質的に(Z)ポリビニルピロリドン又はポリビニルアルコールを含まないことで、コンタクトレンズを眼に入れる際(装着時)の異物感・ゴロゴロ感が低減されており、且つ、レンズが角膜上に安定に保持されているという自覚が得られると共に、コンタクトレンズ装着直後の視界を良好に保つことができる。さらには、コンタクトレンズを眼に入れ易い(装着し易い)上、手指からコンタクトレンズへの汚れが付着し難く、装着後に指に残った液の感触も良好である。 The contact lens mounting liquid in the present invention contains (A) hydroxyethyl cellulose, (B) amino acids, and substantially does not contain (Z) polyvinyl pyrrolidone or polyvinyl alcohol, so that the contact lens is put into the eye (wearing). ) And a sense of foreignness and lingering feeling are reduced, and a sense that the lens is stably held on the cornea is obtained, and a field of view immediately after the contact lens is mounted can be kept good. Furthermore, it is easy to put the contact lens into the eye (easy to wear), and dirt from the finger to the contact lens is difficult to adhere, and the feel of the liquid remaining on the finger after wearing is also good.
本発明のコンタクトレンズ装着液は、ヒドロキシエチルセルロース(以下、単にHEC又は(A)成分と表記することもある)を含有する。
本発明に用いるヒドロキシエチルセルロースは、種々の分子量や粘度のものが例示され、好ましくは、ヒドロキシエチルセルロース のうち20℃、2%水溶液の粘度が100mPa・s〜50000mPa・sのものが用いられ、より好ましくは1000mPa・s〜50000mPa・s、特に好ましくは1000mPa・s〜30000mPa・sのヒドロキシエチルセルロースである。かかるヒドロキシエチルセルロース は市販のものを利用することができ、例えば住友精化株式会社から販売されているHEC−CF−G(20℃、2%水溶液の粘度が300mPa・s〜600mPa・s)、HEC−CF−V(20℃、2%水溶液の粘度が5000mPa・s〜10000mPa・s)、HEC−CF−W(20℃、2%水溶液の粘度が10000mPa・s〜16000mPa・s)等が利用できる。これらのヒドロキシエチルセルロースを1種または2種以上を組み合わせて使用してもよい。
The contact lens mounting liquid of the present invention contains hydroxyethyl cellulose (hereinafter sometimes simply referred to as HEC or (A) component).
Examples of the hydroxyethyl cellulose used in the present invention include those having various molecular weights and viscosities. Preferably, hydroxyethyl cellulose having a viscosity of 20% at 2 ° C. and a 2% aqueous solution of 100 mPa · s to 50000 mPa · s is more preferable. Is hydroxyethyl cellulose of 1000 mPa · s to 50000 mPa · s, particularly preferably 1000 mPa · s to 30000 mPa · s. Commercially available hydroxyethyl cellulose can be used, for example, HEC-CF-G (20 ° C., 2% aqueous solution viscosity is 300 mPa · s to 600 mPa · s) sold by Sumitomo Seika Co., Ltd., HEC -CF-V (viscosity of 2% aqueous solution at 20 ° C. is 5000 mPa · s to 10,000 mPa · s), HEC-CF-W (viscosity of 2% aqueous solution at 20 ° C. is 10,000 mPa · s to 16000 mPa · s), etc. can be used. . These hydroxyethyl celluloses may be used alone or in combination of two or more.
本発明におけるコンタクトレンズ装着液中のヒドロキシエチルセルロースの含有量は、化合物の種類や分子量によっても異なるので限定されるものではないが、コンタクトレンズ装着液の総量に対し、これらの化合物が総量で、通常0.0001〜25%、好ましくは0.001〜10%、より好ましくは0.005〜7%、更に好ましくは0.01〜5%、特に好ましくは0.01〜1%である。 The content of hydroxyethyl cellulose in the contact lens mounting liquid in the present invention is not limited because it varies depending on the type and molecular weight of the compound, but the total amount of these compounds relative to the total amount of the contact lens mounting liquid, usually It is 0.0001 to 25%, preferably 0.001 to 10%, more preferably 0.005 to 7%, still more preferably 0.01 to 5%, and particularly preferably 0.01 to 1%.
本発明のコンタクトレンズ装着液は、さらにアミノ酸類(以下、単に(B)成分と表記することもある)を含有する。
本発明に用いるアミノ酸類とは、アミノ酸又はその塩、及びアミノ酸類似体を包含し、分子内にアミノ基とカルボキシル基又はスルホン基を有する化合物又はその誘導体を意味する。具体的にはアミノ酸又はその塩、ムコ多糖又はその誘導体又はそれらの塩が例示される。
The contact lens mounting liquid of the present invention further contains amino acids (hereinafter sometimes simply referred to as component (B)).
The amino acid used in the present invention includes an amino acid or a salt thereof, and an amino acid analog, and means a compound having an amino group and a carboxyl group or a sulfone group in the molecule or a derivative thereof. Specific examples include amino acids or salts thereof, mucopolysaccharides or derivatives thereof, or salts thereof.
アミノ酸類は、例えば、グリシン、アラニン、アミノ酪酸、アミノ吉草酸、アミノカプロン酸等のモノアミノモノカルボン酸;アスパラギン酸、グルタミン酸等のモノアミノジカルボン酸又はそれらの塩;アルギニン、リジン等のジアミノモノカルボン酸又はそれらの塩;アミノエチルスルホン酸(タウリン);コンドロイチン硫酸、ヒアルロン酸などのムコ多糖又はその誘導体又はそれらの塩(ムコ多糖類とも言う。)等である。具体例として、グリシン、アラニン、γ―アミノ酪酸、γ―アミノ吉草酸、イプシロンアミノカプロン酸、アスパラギン酸、グルタミン酸、アルギニン、アミノエチルスルホン酸、コンドロイチン硫酸、ヒアルロン酸又はそれらの塩等が挙げられる。アミノ酸の塩又はムコ多糖類は、医薬上、薬理学的に又は生理学的に許容される塩を含む。そのような塩としては、有機酸との塩[例えば、モノカルボン酸塩(酢酸塩、トリフルオロ酢酸塩、酪酸塩、パルミチン酸塩、ステアリン酸塩など)、多価カルボン酸塩(フマル酸塩、マレイン酸塩など)、オキシカルボン酸塩(乳酸塩、酒石酸塩、クエン酸塩、コハク酸塩、マロン酸塩など)、有機スルホン酸塩(メタンスルホン酸塩、トルエンスルホン酸塩、トシル酸塩など)など]、無機酸との塩(例えば、塩酸塩、硫酸塩、硝酸塩、臭化水素酸塩、リン酸塩など)、有機塩基との塩(例えば、メチルアミン、トリエチルアミン、トリエタノールアミン、モルホリン、ピペラジン、ピロリジン、トリピリジン、ピコリンなどの有機アミンとの塩など)、無機塩基との塩[例えば、アンモニウム塩;アルカリ金属(ナトリウム、カリウムなど)、アルカリ土類金属(カルシウム、マグネシウムなど)、アルミニウムなどの金属との塩など]などが例示でき、化合物によって適宜選択される。例えば、モノアミノジカルボン酸の場合は、無機塩基との塩が好ましく、特にアルカリ金属塩やアルカリ土類金属塩が好ましい。 Amino acids include, for example, monoamino monocarboxylic acids such as glycine, alanine, aminobutyric acid, aminovaleric acid, and aminocaproic acid; monoaminodicarboxylic acids such as aspartic acid and glutamic acid or salts thereof; and diaminomonocarboxylic acids such as arginine and lysine. Acids or salts thereof; aminoethylsulfonic acid (taurine); mucopolysaccharides such as chondroitin sulfate and hyaluronic acid or derivatives thereof or salts thereof (also referred to as mucopolysaccharides). Specific examples include glycine, alanine, γ-aminobutyric acid, γ-aminovaleric acid, epsilon aminocaproic acid, aspartic acid, glutamic acid, arginine, aminoethylsulfonic acid, chondroitin sulfate, hyaluronic acid, and salts thereof. Amino acid salts or mucopolysaccharides include pharmaceutically, pharmacologically or physiologically acceptable salts. Examples of such salts include salts with organic acids [for example, monocarboxylates (acetate, trifluoroacetate, butyrate, palmitate, stearate, etc.), polyvalent carboxylate (fumarate , Maleate, etc.), oxycarboxylate (lactate, tartrate, citrate, succinate, malonate, etc.), organic sulfonate (methanesulfonate, toluenesulfonate, tosylate) Etc.], salts with inorganic acids (eg hydrochlorides, sulfates, nitrates, hydrobromides, phosphates etc.), salts with organic bases (eg methylamine, triethylamine, triethanolamine, Salts with organic amines such as morpholine, piperazine, pyrrolidine, tripyridine, picoline, etc.), salts with inorganic bases [eg ammonium salts; alkali metals (sodium, potassium, etc.), alkaline earths Metal (calcium, magnesium etc.), etc. and salts with metals such as aluminum] can be exemplified, it is appropriately selected depending on the compound. For example, in the case of monoaminodicarboxylic acid, a salt with an inorganic base is preferable, and an alkali metal salt or an alkaline earth metal salt is particularly preferable.
好ましいアミノ酸類は、グリシン、アラニン、γ―アミノ酪酸、γ―アミノ吉草酸、イプシロンアミノカプロン酸、アスパラギン酸ナトリウム、アスパラギン酸カリウム、アスパラギン酸マグネシウム、アスパラギン酸カルシウム、アスパラギン酸マグネシウム・カリウム(等量混合物)、グルタミン酸、塩酸グルタミン酸、グルタミン酸マグネシウム、アミノエチルスルホン酸、コンドロイチン硫酸ナトリウム、ヒアルロン酸、ヒアルロン酸ナトリウム等である。より好ましくは、イプシロンアミノカプロン酸、アスパラギン酸カリウム、アスパラギン酸マグネシウム、アスパラギン酸マグネシウム・カリウム(等量混合物)、アミノエチルスルホン酸、コンドロイチン硫酸ナトリウム、ヒアルロン酸ナトリウムである。なお、本発明のアミノ酸類は、D体、L体、DL体のいずれでもよい。また、本発明のアミノ酸類は、単独又は2種以上を組み合わせて用いることができる。 Preferred amino acids are glycine, alanine, γ-aminobutyric acid, γ-aminovaleric acid, epsilon aminocaproic acid, sodium aspartate, potassium aspartate, magnesium aspartate, calcium aspartate, magnesium and potassium aspartate (equal mixture) Glutamic acid, glutamic acid hydrochloride, magnesium glutamate, aminoethylsulfonic acid, sodium chondroitin sulfate, hyaluronic acid, sodium hyaluronate and the like. More preferred are epsilon aminocaproic acid, potassium aspartate, magnesium aspartate, magnesium / potassium aspartate (equal mixture), aminoethylsulfonic acid, sodium chondroitin sulfate, and sodium hyaluronate. The amino acids of the present invention may be any of D form, L form, and DL form. The amino acids of the present invention can be used alone or in combination of two or more.
本発明におけるコンタクトレンズ装着液中のアミノ酸類の含有量は、化合物の種類や分子量によっても異なるので限定されるものではないが、コンタクトレンズ装着液の総量に対し、これらの化合物の総量で、通常0.0001〜10%、好ましくは0.001〜10%、より好ましくは0.005〜8%、さらに好ましくは0.02〜5重量%、特に好ましくは0.02〜3重量%、さらに特に好ましくは、0.05〜2%である。 The content of amino acids in the contact lens mounting liquid in the present invention is not limited because it varies depending on the type and molecular weight of the compound, but the total amount of these compounds with respect to the total amount of the contact lens mounting liquid, It is 0.0001 to 10%, preferably 0.001 to 10%, more preferably 0.005 to 8%, still more preferably 0.02 to 5% by weight, particularly preferably 0.02 to 3% by weight, and still more preferably 0.05 to 2%.
本発明のコンタクトレンズ装着液は、必要に応じて適当な非イオン性界面活性剤(以下、単に(C)成分と表記することもある)を含有することができる。
本発明に用いる非イオン性界面活性剤としては、通常当業者がコンタクトレンズ用眼科組成物に利用しうるものを用いることができ、例えばポロクサマー407 、ポロクサマー235 、ポロクサマー188 などのポリオキシエチレン−ポリオキシプロピレンブロックコポリマー (以下、ポリオキシエチレンポリオキシプロピレン共重合体とも言う。);ポロキサミンなどのエチレンジアミンのPOE-POPブロックコポリマー付加物;モノラウリル酸POE(20)ソルビタン(ポリソルベート20) ,モノオレイン酸POE(20)ソルビタン (ポリソルベート80) ,POEソルビタンモノステアレート(ポリソルベート60),POEソルビタントリステアレート(ポリソルベート65) などのPOEソルビタン脂肪酸エステル類;POE硬化ヒマシ油5 ,POE硬化ヒマシ油10 ,POE硬化ヒマシ油20 ,POE硬化ヒマシ油40 ,POE硬化ヒマシ油50、POE硬化ヒマシ油60 ,POE硬化ヒマシ油100などのPOE硬化ヒマシ油類;POE(9) ラウリルエーテルなどのPOEアルキルエーテル類;POE(20)POP(4) セチルエーテルなどのPOE・POPアルキルエーテル類;POE(10)ノニルフェニルエーテルなどのPOEアルキルフェニルエーテル類などが挙げられる。なお、POEはポリオキシエチレンを示し、POPはポリオキシプロピレンを示し、括弧内の数字は付加モル数を示す。
The contact lens mounting liquid of the present invention can contain an appropriate nonionic surfactant (hereinafter, sometimes simply referred to as component (C)) as necessary.
As the nonionic surfactant used in the present invention, those that can be used by those skilled in the art for ophthalmic compositions for contact lenses can be used. For example, polyoxyethylene-polysiloxane such as Poloxamer 407, Poloxamer 235, Poloxamer 188, etc. Oxypropylene block copolymer (hereinafter also referred to as polyoxyethylene polyoxypropylene copolymer); POE-POP block copolymer adduct of ethylenediamine such as poloxamine; monolauric acid POE (20) sorbitan (polysorbate 20), monooleic acid POE sorbitan fatty acid esters such as POE (20) sorbitan (polysorbate 80), POE sorbitan monostearate (polysorbate 60), POE sorbitan tristearate (polysorbate 65); POE cured castor oil 5; POE cured castor POE cured castor oils such as oil 10, POE cured castor oil 20, POE cured castor oil 40, POE cured castor oil 50, POE cured castor oil 60, POE cured castor oil 100; POE alkyl such as POE (9) lauryl ether POE (20) POP (4) POE / POP alkyl ethers such as cetyl ether; POE alkyl phenyl ethers such as POE (10) nonyl phenyl ether. POE represents polyoxyethylene, POP represents polyoxypropylene, and the numbers in parentheses indicate the number of moles added.
なかでも好ましくは、ポリオキシエチレン−ポリオキシプロピレンブロックコポリマー、POEソルビタン脂肪酸エステル類又はPOE硬化ヒマシ油類であり、中でも特に好ましくは、ポロクサマー407、ポリソルベート80、POE硬化ヒマシ油60である。
本発明におけるコンタクトレンズ装着液中の非イオン性界面活性剤の含有量は、界面活性剤の種類などによって異なるので一概に規定できないが、コンタクトレンズ装着液の総量に対し、これらが総量で、通常0.001〜5%、好ましくは0.001〜1.5%、より好ましくは0.001〜1%、さらに好ましくは0.005〜0.5%、特に好ましくは0.05〜0.3%である。
Among these, polyoxyethylene-polyoxypropylene block copolymers, POE sorbitan fatty acid esters or POE hydrogenated castor oil are preferable, and poloxamer 407, polysorbate 80, and POE hydrogenated castor oil 60 are particularly preferable.
The content of the nonionic surfactant in the contact lens mounting liquid in the present invention varies depending on the type of the surfactant and the like, and thus cannot be defined unconditionally. 0.001 to 5%, preferably 0.001 to 1.5%, more preferably 0.001 to 1%, still more preferably 0.005 to 0.5%, and particularly preferably 0.05 to 0.3. %.
本発明のコンタクトレンズ装着液には、必要に応じて適当な緩衝剤を配合することが好ましい。本発明に用いる緩衝剤としては、ホウ酸緩衝剤、リン酸緩衝剤、炭酸緩衝剤、クエン酸緩衝剤、酢酸緩衝剤、HEPES緩衝剤、MOPS緩衝剤などが挙げられる。より具体的には、ホウ酸、ホウ酸ナトリウム、テトラホウ酸カリウム、ホウ砂、メタホウ酸カリウム、リン酸、リン酸水素ナトリウム、リン酸二水素ナトリウム、リン酸二水素カリウム、炭酸、炭酸水素ナトリウム、炭酸ナトリウム、クエン酸、クエン酸ナトリウム、クエン酸カリウム、酢酸、酢酸ナトリウム、HEPES、MOPSなどの化合物、これらの水和物、これらの群から選ばれる2種以上の化合物の組み合わせ等が挙げられる。 In the contact lens mounting liquid of the present invention, an appropriate buffer is preferably blended as necessary. Examples of the buffer used in the present invention include borate buffer, phosphate buffer, carbonate buffer, citrate buffer, acetate buffer, HEPES buffer, and MOPS buffer. More specifically, boric acid, sodium borate, potassium tetraborate, borax, potassium metaborate, phosphoric acid, sodium hydrogen phosphate, sodium dihydrogen phosphate, potassium dihydrogen phosphate, carbonic acid, sodium hydrogen carbonate, Examples thereof include compounds such as sodium carbonate, citric acid, sodium citrate, potassium citrate, acetic acid, sodium acetate, HEPES, and MOPS, hydrates thereof, and combinations of two or more compounds selected from these groups.
好ましい緩衝剤は、ホウ酸緩衝剤、リン酸緩衝剤、炭酸緩衝剤及びクエン酸緩衝剤である。特に好ましい緩衝剤は、ホウ酸緩衝剤またはリン酸緩衝剤である。特に好ましい緩衝剤は、より具体的には、ホウ酸緩衝剤としてはホウ酸、ホウ酸アルカリ金属塩,ホウ酸アルカリ土類金属塩などのホウ酸塩、ホウ酸とホウ酸塩との組み合わせが挙げられ、特にホウ酸、ホウ砂が好ましく、リン酸緩衝剤としては、リン酸、リン酸アルカリ金属塩,リン酸アルカリ土類金属塩などのリン酸塩、それらの水和物、リン酸とリン酸塩との組み合わせが挙げられ、特にリン酸水素ナトリウム、リン酸ニ水素ナトリウム、それらの水和物が好ましい。 Preferred buffering agents are borate buffer, phosphate buffer, carbonate buffer and citrate buffer. Particularly preferred buffering agents are borate buffers or phosphate buffers. Particularly preferred buffering agents include, more specifically, boric acid buffers such as boric acid, borate salts such as alkali metal borate salts and alkaline earth metal borate salts, and combinations of boric acid and borate salts. In particular, boric acid and borax are preferable, and phosphate buffering agents include phosphoric acid, phosphates such as alkali metal phosphates and alkaline earth metal phosphates, hydrates thereof, phosphoric acid and The combination with a phosphate is mentioned, Especially sodium hydrogenphosphate, sodium dihydrogenphosphate, and those hydrates are preferable.
本発明におけるコンタクトレンズ装着液中の緩衝剤の含有量は、緩衝剤の種類などによって異なるので一概に規定できないが、コンタクトレンズ装着液の総量に対し、これらが総量で、通常0.001〜5%、好ましくは0.001〜3%、より好ましくは0.005〜2.0%、さらに好ましくは0.005〜1.5%、特に好ましくは0.05〜1.5%である。 In the present invention, the content of the buffering agent in the contact lens mounting liquid varies depending on the type of the buffering agent and cannot be defined unconditionally. %, Preferably 0.001 to 3%, more preferably 0.005 to 2.0%, still more preferably 0.005 to 1.5%, and particularly preferably 0.05 to 1.5%.
本発明のコンタクトレンズ装着液には、必要に応じて適当な無機塩類を配合することが好ましい。無機塩類としては、塩化カリウム、塩化ナトリウム、炭酸水素ナトリウム、炭酸ナトリウムが挙げられ、これらの1種または2種以上を組み合わせて使用してもよい。
本発明におけるコンタクトレンズ装着液中の無機塩類の含有量は、無機塩類の種類などによって異なるので一概に規定できないが、コンタクトレンズ装着液の総量に対し、これらが総量で、通常0.001〜5%、好ましくは0.01〜1.5%、より好ましくは0.1〜0.7%で用いられる。
The contact lens mounting liquid of the present invention preferably contains an appropriate inorganic salt as required. Examples of inorganic salts include potassium chloride, sodium chloride, sodium hydrogen carbonate, and sodium carbonate, and these may be used alone or in combination.
The content of inorganic salts in the contact lens mounting liquid in the present invention varies depending on the kind of inorganic salts and the like, and thus cannot be specified unconditionally. However, these are the total amount with respect to the total amount of the contact lens mounting liquid, and usually 0.001 to 5 %, Preferably 0.01 to 1.5%, more preferably 0.1 to 0.7%.
本発明のコンタクトレンズ装着液には、必要に応じて適当なエチレンジアミン酢酸誘導体またはその塩を配合することが好ましい。かかるエチレンジアミン酢酸誘導体またはその塩としては、例えば、エデト酸(エチレンジアミン四酢酸,EDTA)、エチレンジアミン二酢酸(EDDA)、N−(2−ヒドロキシエチル)エチレンジアミン三酢酸(HEDTA)またはそれらの塩などが例示できる。エチレンジアミン酢酸誘導体の塩は、薬理学的に又は生理学的に許容される塩を含み、例えばアルカリ金属(ナトリウム、カリウムなど)との塩、アルカリ土類金属(カルシウムなど)との塩などが挙げられる。なかでも好ましくは、エチレンジアミン四酢酸またはその塩であり、例えばエチレンジアミン四酢酸カルシウム二ナトリウム、エチレンジアミン四酢酸二ナトリウム、エチレンジアミン四酢酸二ナトリウム・二水和物(以下、エデト酸ナトリウムともいう。)であり、特に好ましくはエチレンジアミン四酢酸二ナトリウム・二水和物である。これらは、1種又は2種以上を組み合わせて用いる事ができる。 The contact lens mounting liquid of the present invention preferably contains an appropriate ethylenediamineacetic acid derivative or a salt thereof as necessary. Examples of such ethylenediamineacetic acid derivatives or salts thereof include edetic acid (ethylenediaminetetraacetic acid, EDTA), ethylenediaminediacetic acid (EDDA), N- (2-hydroxyethyl) ethylenediaminetriacetic acid (HEDTA), and salts thereof. it can. Salts of ethylenediamineacetic acid derivatives include pharmacologically or physiologically acceptable salts such as salts with alkali metals (sodium, potassium, etc.) and salts with alkaline earth metals (calcium, etc.). . Among them, ethylenediaminetetraacetic acid or a salt thereof is preferable, for example, ethylenediaminetetraacetic acid calcium disodium, ethylenediaminetetraacetic acid disodium, ethylenediaminetetraacetic acid disodium dihydrate (hereinafter also referred to as sodium edetate). Particularly preferred is disodium ethylenediaminetetraacetate dihydrate. These can be used alone or in combination of two or more.
本発明におけるコンタクトレンズ装着液中のエチレンジアミン酢酸誘導体またはその塩の含有量は分子量や種類などによって異なるので一概に規定できないが、コンタクトレンズ装着液の総量に対し、これらが総量で、好ましくは0.0001〜1%、より好ましくは0.0005〜0.5%、さらに好ましくは0.001〜0.3%、特に好ましくは0.001〜0.05%である。 In the present invention, the content of the ethylenediamineacetic acid derivative or salt thereof in the contact lens mounting liquid varies depending on the molecular weight and type and cannot be defined unconditionally. However, these are the total amount, preferably 0. It is 0001 to 1%, more preferably 0.0005 to 0.5%, still more preferably 0.001 to 0.3%, and particularly preferably 0.001 to 0.05%.
また、さらに本発明の効果を発揮するために、エチレンジアミン酢酸誘導体またはその塩、非イオン性界面活性剤、無機塩類、緩衝剤を組み合わせて配合することがより好ましい。
本発明におけるコンタクトレンズ装着液中のエチレンジアミン酢酸誘導体またはその塩、非イオン性界面活性剤、無機塩類、緩衝剤の含有量は、コンタクトレンズ装着液の総量に対し、これらが総量で、0.01〜5%が好ましく、特に好ましくは0.05〜3%である。
Further, in order to further exert the effect of the present invention, it is more preferable to blend an ethylenediamineacetic acid derivative or a salt thereof, a nonionic surfactant, an inorganic salt, and a buffering agent in combination.
The content of the ethylenediamineacetic acid derivative or a salt thereof, a nonionic surfactant, an inorganic salt, and a buffering agent in the contact lens mounting liquid in the present invention is 0.01% of the total amount of the contact lens mounting liquid. -5% is preferable, and 0.05-3% is particularly preferable.
本発明のコンタクトレンズ装着液は、コンタクトレンズのなかでも特に、ソフトコンタクトレンズ用に用いるのが好適である。ソフトコンタクトレンズは、面積が大きく、柔軟性が高い為、前述のような問題点が生じ易く、本発明の装着液がより好適に使用され得る。中でも、柔軟性が高く眼に入れ難いソフトコンタクトレンズ分類グループIVのソフトコンタクトレンズや、異物感の高いシリコーンハイドロゲル素材のソフトコンタクトレンズにおいて、顕著な効果を発揮するため、これらのコンタクトレンズ用としてより好適に用いる事ができる。 The contact lens mounting liquid of the present invention is particularly suitable for use in soft contact lenses among contact lenses. Since the soft contact lens has a large area and high flexibility, the above-mentioned problems are likely to occur, and the mounting liquid of the present invention can be used more suitably. Especially for soft contact lenses of soft contact lens classification group IV, which is flexible and difficult to get into eyes, and soft contact lenses made of silicone hydrogel material with a high sense of foreign matter. It can be used more suitably.
本発明のコンタクトレンズ装着液は、種々の成分(薬理活性成分や生理活性成分を含む)を組み合わせて含有するのに適している。眼科組成物に通常用いられる充血除去成分、眼筋調節薬成分、抗炎症薬成分または収斂薬成分、抗ヒスタミン薬成分又は抗アレルギー薬成分、ビタミン類、局所麻酔薬成分などが例示できる。具体的には、以下に挙げる成分が例示できる。 The contact lens mounting liquid of the present invention is suitable for containing various components (including pharmacologically active components and physiologically active components) in combination. Examples thereof include a decongestant component, an eye muscle modulator component, an anti-inflammatory component or an astringent component, an antihistamine component or an antiallergic component, vitamins, and a local anesthetic component that are commonly used in ophthalmic compositions. Specifically, the following components can be exemplified.
充血除去成分:例えば、α−アドレナリン作動薬、具体的にはエピネフリン、塩酸エピネフリン、塩酸エフェドリン、塩酸オキシメタゾリン、塩酸テトラヒドロゾリン、塩酸ナファゾリン、塩酸フェニレフリン、塩酸メチルエフェドリン、酒石酸水素エピネフリン、硝酸ナファゾリンなど。これらはd体、l体又はdl体のいずれでもよい。
眼筋調節薬成分:例えば、アセチルコリンと類似した活性中心を有するコリンエステラーゼ阻害剤、具体的にはメチル硫酸ネオスチグミン、トロピカミド、ヘレニエン硫酸アトロピンなど。
Decongestant: For example, α-adrenergic agonists, specifically epinephrine, epinephrine hydrochloride, ephedrine hydrochloride, oxymetazoline hydrochloride, tetrahydrozoline hydrochloride, naphazoline hydrochloride, phenylephrine hydrochloride, methylephedrine hydrochloride, epinephrine hydrogen tartrate, naphazoline nitrate. These may be d-form, l-form or dl-form.
Eye muscle modulator component: For example, cholinesterase inhibitor having an active center similar to acetylcholine, specifically, neostigmine methyl sulfate, tropicamide, atropine sulfate helenien, and the like.
抗炎症薬成分または収斂薬成分:例えば、硫酸亜鉛、乳酸亜鉛、アラントイン、インドメタシン、塩化リゾチーム、硝酸銀、プラノプロフェン、アズレンスルホン酸ナトリウム、グリチルリチン酸二カリウム、ジクロフェナクナトリウム、ブロムフェナクナトリウム、塩化ベルベリン、硫酸ベルベリンなど。
抗ヒスタミン薬成分又は抗アレルギー薬成分:例えば、アシタザノラスト、アンレキサノクス、イブジラスト、トラニラスト、塩酸ジフェンヒドラミン、塩酸レボカバスチン、フマル酸ケトチフェン、クロモグリク酸ナトリウム、ペミロラストカリウム、マレイン酸クロルフェニラミンなど。
Anti-inflammatory component or astringent component: for example, zinc sulfate, zinc lactate, allantoin, indomethacin, lysozyme chloride, silver nitrate, pranoprofen, sodium azulenesulfonate, dipotassium glycyrrhizinate, diclofenac sodium, bromfenac sodium, berberine chloride , Berberine sulfate and so on.
Antihistamine component or antiallergic agent component: for example, acitazanolast, amlexanox, ibudilast, tranilast, diphenhydramine hydrochloride, levocabastine hydrochloride, ketotifen fumarate, sodium cromoglycate, pemirolast potassium, chlorpheniramine maleate and the like.
ビタミン類:例えば、酢酸レチノール、パルミチン酸レチノール、塩酸ピリドキシン、フラビンアデニンジヌクレオチドナトリウム、リン酸ピリドキサール、シアノコバラミン、パンテノール、パントテン酸カルシウム、パントテン酸ナトリウム、アスコルビン酸、酢酸トコフェロールなど。 Vitamins: for example, retinol acetate, retinol palmitate, pyridoxine hydrochloride, sodium flavin adenine dinucleotide, pyridoxal phosphate, cyanocobalamin, panthenol, calcium pantothenate, sodium pantothenate, ascorbic acid, tocopherol acetate, etc.
局所麻酔薬成分:例えば、クロロブタノール、塩酸オキシブプロカイン、塩酸コカイン、塩酸コルネカイン、塩酸ジブカイン、塩酸テトラカイン、塩酸パラブチルアミノ安息香酸ジエチルアミノエチル、塩酸ピペロカイン、塩酸プロカイン、塩酸プロパラカイン、塩酸ヘキソチオカイン、塩酸リドカインなど。 Local anesthetic ingredients: for example, chlorobutanol, oxybuprocaine hydrochloride, cocaine hydrochloride, cornecaine hydrochloride, dibucaine hydrochloride, tetracaine hydrochloride, diethylaminoethyl parabutylaminobenzoate, piperocaine hydrochloride, procaine hydrochloride, proparacaine hydrochloride, hexothiocaine hydrochloride, hydrochloric acid Lidocaine etc.
また、本発明のコンタクトレンズ装着液には、発明の効果を損なわない範囲でその用途や形態に応じて、常法に従い、様々な成分や添加物を適宜選択し、一種またはそれ以上を含有させてもよい。それらの成分または添加物として、例えば、半固形剤や液剤などの調製に一般的に使用される担体(水、水性溶媒、水性または油性基剤など)、増粘剤、糖類、糖アルコール類、界面活性剤、防腐剤、殺菌剤又は抗菌剤、pH調整剤、等張化剤、香料または清涼化剤、安定剤などの各種添加剤を挙げることができる。 Further, in the contact lens mounting liquid of the present invention, various components and additives are appropriately selected in accordance with conventional methods according to the use and form within a range not impairing the effects of the invention, and one or more of them are contained. May be. As those components or additives, for example, carriers (water, aqueous solvents, aqueous or oily bases, etc.) commonly used in the preparation of semi-solids and liquids, thickeners, sugars, sugar alcohols, Various additives such as surfactants, preservatives, bactericides or antibacterial agents, pH adjusters, tonicity agents, fragrances or refreshing agents, stabilizers and the like can be mentioned.
以下に本発明のコンタクトレンズ装着液に使用される代表的な成分を例示するが、これらに限定されない。
増粘剤:例えば、メチルセルロース、エチルセルロース、ヒドロキシメチルセルロース、ヒドロキシプロピルセルロース、ヒドロキシプロピルメチルセルロース、カルボキシメチルセルロース、カルボキシエチルセルロースまたはこれらの塩などのセルロース系高分子化合物、デキストラン、ポリエチレングリコールなど。
糖類:例えば、グルコース、シクロデキストリンなど。
糖アルコール類:例えば、キシリトール、ソルビトール、マンニトールなど。
界面活性剤:例えば、上記した非イオン性界面活性剤以外にも、アルキルジアミノエチルグリシンなどのグリシン型両性界面活性剤;アルキル4級アンモニウム塩(具体的には、塩化ベンザルコニウム、塩化ベンゼトニウムなどの陽イオン界面活性剤など。)など。
Although the typical component used for the contact lens mounting liquid of this invention is illustrated below, it is not limited to these.
Thickener: For example, cellulose-based polymer compounds such as methyl cellulose, ethyl cellulose, hydroxymethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, carboxymethyl cellulose, carboxyethyl cellulose or salts thereof, dextran, polyethylene glycol and the like.
Sugars: for example, glucose, cyclodextrin and the like.
Sugar alcohols: For example, xylitol, sorbitol, mannitol and the like.
Surfactant: For example, in addition to the above-mentioned nonionic surfactants, glycine type amphoteric surfactants such as alkyldiaminoethylglycine; alkyl quaternary ammonium salts (specifically, benzalkonium chloride, benzethonium chloride, etc.) Cationic surfactant etc.) etc.
防腐剤、殺菌剤又は抗菌剤:例えば、塩酸アルキルジアミノエチルグリシン、安息香酸ナトリウム、エタノール、塩化ベンザルコニウム、塩化ベンゼトニウム、グルコン酸クロルヘキシジン、クロロブタノール、ソルビン酸、ソルビン酸カリウム、デヒドロ酢酸ナトリウム、パラオキシ安息香酸メチル、パラオキシ安息香酸エチル、パラオキシ安息香酸プロピル、パラオキシ安息香酸ブチル、硫酸オキシキノリン、フェネチルアルコール、ベンジルアルコール、ビグアニド化合物(具体的には、ポリヘキサメチレンビグアニド又はその塩酸塩など)、塩化ポリドロニウム、グローキル(ローディア社製 商品名)など。 Preservatives, bactericides or antibacterials: for example, alkyldiaminoethylglycine hydrochloride, sodium benzoate, ethanol, benzalkonium chloride, benzethonium chloride, chlorhexidine gluconate, chlorobutanol, sorbic acid, potassium sorbate, sodium dehydroacetate, paraoxy Methyl benzoate, ethyl paraoxybenzoate, propyl paraoxybenzoate, butyl paraoxybenzoate, oxyquinoline sulfate, phenethyl alcohol, benzyl alcohol, biguanide compounds (specifically, polyhexamethylene biguanide or its hydrochloride), polydronium chloride , Glow Kill (trade name, manufactured by Rhodia).
pH調整剤:例えば、塩酸、ホウ酸、イプシロン−アミノカプロン酸、酢酸、水酸化ナトリウム、炭酸水素ナトリウム、炭酸ナトリウム、ホウ砂、トリエタノールアミン、モノエタノールアミンなど。
等張化剤:例えば、亜硫酸水素ナトリウム、亜硫酸ナトリウム、塩化マグネシウム、酢酸カリウム、酢酸ナトリウム、チオ硫酸ナトリウム、硫酸マグネシウム、グリセリン、プロピレングリコールなど。
pH adjuster: For example, hydrochloric acid, boric acid, epsilon-aminocaproic acid, acetic acid, sodium hydroxide, sodium hydrogen carbonate, sodium carbonate, borax, triethanolamine, monoethanolamine and the like.
Isotonizing agents: for example, sodium bisulfite, sodium sulfite, magnesium chloride, potassium acetate, sodium acetate, sodium thiosulfate, magnesium sulfate, glycerin, propylene glycol and the like.
安定剤:ジブチルヒドロキシトルエン、トロメタモール、ナトリウムホルムアルデヒドスルホキシレート(ロンガリット)、トコフェロール、ピロ亜硫酸ナトリウム、モノエタノールアミン、モノステアリン酸アルミニウムなど。
香料又は清涼化剤:テルペン類(例えば、アネトール、オイゲノール、カンフル、ゲラニオール、シネオール、ボルネオール、メントール、リモネン、リュウノウなど。これらはd体、l体又はdl体のいずれでもよい。)、精油(ウイキョウ油、クールミント油、ケイヒ油、スペアミント油、ハッカ水、ハッカ油、ペパーミント油、ベルガモット油、ユーカリ油、ローズ油など)など。
Stabilizer: Dibutylhydroxytoluene, trometamol, sodium formaldehyde sulfoxylate (Longalite), tocopherol, sodium pyrosulfite, monoethanolamine, aluminum monostearate, etc.
Perfume or refreshing agent: terpenes (for example, anethole, eugenol, camphor, geraniol, cineol, borneol, menthol, limonene, ryuuno, etc. These may be any of d-form, l-form, or dl-form), essential oil (Fennel) Oil, cool mint oil, cinnamon oil, spearmint oil, mint water, mint oil, peppermint oil, bergamot oil, eucalyptus oil, rose oil, etc.).
尚、本発明のコンタクトレンズ装着液は、ポリビニルアルコール(完全又は部分ケン化物)及び/又はポリビニルピロリドン(以下、単に(Z)成分と表記する事もある)を含有しない。これは、本発明者らが、これらの化合物が、成分(A)及び成分(B)を含有するよう構成された本発明の効果に負の影響を及ぼすとの知見を得たことによる。特に、コンタクトレンズ装着後、指に残存する液が好ましくない感触(ベタベタ感)を与え、使用感が良好でないという問題点を有することを見出した。その他、ポリビニルピロリドンはコンタクトレンズの直径(サイズ)への影響が大きく、またポリビニルアルコールは、ホウ酸緩衝剤の共存によりゲル化する事が知られており、製造上や使用感等の点で問題があるなど、処方上の制約がある。従来のコンタクトレンズ装着液は、多くの場合、クッション性を確保する為にこれら(Z)成分を含有していたが、成分(A)及び(B)を必須成分として含有する本発明のコンタクトレンズ装着液は、(Z)成分を積極的に排除して従来の装着液の上記問題点を解消し、且つ、装着液としての優れた機能を維持することに成功したものである。 In addition, the contact lens mounting liquid of the present invention does not contain polyvinyl alcohol (completely or partially saponified product) and / or polyvinyl pyrrolidone (hereinafter sometimes simply referred to as the (Z) component). This is because the present inventors have obtained knowledge that these compounds have a negative influence on the effects of the present invention configured to contain the component (A) and the component (B). In particular, the present inventors have found that after the contact lens is mounted, the liquid remaining on the finger gives an unpleasant feeling (sticky feeling) and the feeling of use is not good. In addition, polyvinyl pyrrolidone has a large effect on the diameter (size) of contact lenses, and polyvinyl alcohol is known to gel by the coexistence of borate buffer, which is problematic in terms of manufacturing and usability. There are prescription restrictions such as. Conventional contact lens mounting liquids often contain these components (Z) in order to ensure cushioning properties, but the contact lenses of the present invention contain components (A) and (B) as essential components. The mounting liquid has been successful in eliminating the above-mentioned problems of the conventional mounting liquid by actively removing the component (Z) and maintaining the excellent function as the mounting liquid.
本発明のコンタクトレンズ装着液は、所望の効果を得るために適切な粘度に初期設定して設定粘度を長期的に安定に保持することができる。コンタクトレンズ装着液の粘度を設定する場合において、20℃における粘度が1.1mPa・s以上に保持して設計することが好ましく、通常1.1〜300mPa・s、好ましくは、1.3〜100mPa・s、特に好ましくは1.5〜80mPa・sに設計することができる。 The contact lens mounting liquid of the present invention can be initially set to an appropriate viscosity in order to obtain a desired effect, and the set viscosity can be stably maintained over a long period of time. When setting the viscosity of the contact lens mounting liquid, it is preferable to design the liquid at 20 ° C. while maintaining the viscosity at 1.1 mPa · s or more, usually 1.1 to 300 mPa · s, preferably 1.3 to 100 mPa. · S, particularly preferably 1.5 to 80 mPa · s.
粘度の測定は、円すい一平板形回転粘度計を用いる方法(第十四改正日本薬局法に記載の、一般試験法、45.粘度測定法、第2法回転粘度計法、「(3)円すい−平板形回転粘度計」の項に記載の方法)に従い、具体的には、市販の円すい−平板形回転粘度計と適宜選択されたロータとを用いて測定することができる。例えば、市販のE型粘度計[トキメック(TOKIMEC)製、東機産業(日本)から販売]と適宜選択されたローターを用い、披検試料測定毎にJIS Z8809により規定されている石油系の炭化水素油(ニュートン流体)を校正用標準液として調整することにより、20℃における粘度を測定することができる。具体的には、特開2006-348055に記載の粘度測定方法に従う(測定条件については後述) Viscosity is measured by a method using a cone-and-plate rotational viscometer (general test method, 45. Viscosity measurement method, second method rotational viscometer method described in the 14th revised Japanese pharmacy method, “(3) conical According to the method described in the section of “Plate Rotational Viscometer”, specifically, it can be measured using a commercially available cone-plate rotational viscometer and an appropriately selected rotor. For example, a commercially available E-type viscometer [manufactured by TOKIMEC, sold by Toki Sangyo (Japan)] and a suitably selected rotor, petroleum carbonization specified by JIS Z8809 for each sample measurement. By adjusting hydrogen oil (Newtonian fluid) as a calibration standard solution, the viscosity at 20 ° C. can be measured. Specifically, the viscosity measurement method described in JP-A-2006-348055 is followed (measurement conditions are described later).
本発明のコンタクトレンズ装着液は、必要に応じて、生体に許容される範囲内の浸透圧に調整して用いる。浸透圧は、生理食塩液に対する浸透圧比として、通常、0.3〜4.1、好ましくは0.4〜4.1、より好ましくは0.3〜2.1、特に好ましくは0.5〜1.4である。浸透圧比の測定方法は、第15改正日本薬局方 一般試験法 浸透圧測定法を参考にする。 The contact lens mounting liquid of the present invention is used by adjusting to an osmotic pressure within a range acceptable for a living body, if necessary. The osmotic pressure is usually from 0.3 to 4.1, preferably from 0.4 to 4.1, more preferably from 0.3 to 2.1, and particularly preferably from 0.5 to 4.1 as the osmotic pressure ratio with respect to physiological saline. 1.4. For the method of measuring the osmotic pressure ratio, refer to the 15th revised Japanese Pharmacopoeia general test method osmotic pressure measurement method.
本発明のコンタクトレンズ装着液は、必要に応じて、生体に適用可能な範囲内のpHに調整して用いる。pHは、通常、pH4.0〜9.0、好ましくは5.0〜8.5、特に好ましくは5.5〜8.5である。pHの調整は、前記緩衝剤、pH調整剤などを用いて行うことができる。 The contact lens mounting liquid of the present invention is used after adjusting to a pH within a range applicable to a living body, if necessary. The pH is usually pH 4.0 to 9.0, preferably 5.0 to 8.5, and particularly preferably 5.5 to 8.5. Adjustment of pH can be performed using the said buffer, a pH adjuster, etc.
本発明のコンタクトレンズ装着液は、公知の方法により製造でき、必要により、ろ過滅菌処理工程や、容器への充填工程等を加えることができる。 The contact lens mounting liquid of the present invention can be produced by a known method, and if necessary, a filtration sterilization process, a filling process into a container, and the like can be added.
本発明のコンタクトレンズ装着液の使用方法としては、コンタクトレンズ装着時(装着する直前)に、コンタクトレンズ装着液を直接コンタクトレンズに滴下し、コンタクトレンズの両面もしくは片面を適量(例えば、好適には1回1〜3滴)で濡らしたのち、該コンタクトレンズを装着して使用する方法などが挙げられる。 As a method of using the contact lens mounting liquid of the present invention, when the contact lens is mounted (immediately before mounting), the contact lens mounting liquid is directly dropped onto the contact lens, and an appropriate amount (for example, preferably, both surfaces of the contact lens are applied). For example, there may be mentioned a method in which the contact lens is used after being wetted with 1 to 3 drops at a time.
以下に、実施例及び比較例に基づいて本発明を詳細に説明するが、本発明はこれらの実施例によって限定されるものではない。
尚、各実施例及び比較例の粘度は、E型粘度計の1種であるTVE−20L形粘度計コーンプレートタイプ(トキメック(TOKIMEC)製、東機産業(日本))を用いて、以下の測定条件の下で測定を行った。特記する以外は、特開2006-348055に記載の粘度測定方法に従う。ただし、測定条件は以下の通りである。
使用ローター:標準ローター(1°34′、R=2.4cm)
回転数 :100rpm (尚、粘度により回転数の許容範囲が異なる為、各処方に応じて測定可能な回転数のうち、最も高い回転数で測定する。)
試料量 :1ml
測定温度 :20℃
時間 :3分後の粘度を測定値とした。
Hereinafter, the present invention will be described in detail based on Examples and Comparative Examples, but the present invention is not limited to these Examples.
In addition, the viscosity of each Example and Comparative Example is the following using TVE-20L type viscometer cone plate type (TOKIMEC, Toki Sangyo (Japan)) which is one type of E type viscometer. Measurement was performed under measurement conditions. The viscosity measurement method described in JP-A-2006-348055 is followed unless otherwise specified. However, the measurement conditions are as follows.
Rotor used: Standard rotor (1 ° 34 ', R = 2.4 cm)
Rotational speed: 100 rpm (In addition, since the allowable range of the rotational speed varies depending on the viscosity, it is measured at the highest rotational speed among the rotational speeds that can be measured according to each prescription.)
Sample volume: 1ml
Measurement temperature: 20 ° C
Time: Viscosity after 3 minutes was taken as a measured value.
試験1:使用感試験(1)
表1に記載の処方に従い、各コンタクトレンズ装着液を点眼液等の調製方法(常法)に従って調製し、ポリエチレンテレフタレート製容器(容量10mL)に充填し、施栓した。コンタクトレンズの両面を各コンタクトレンズ装着液1〜3滴でぬらした後、目に装着し、使用感を評価した。被験者は、日常的にコンタクトレンズを使用している8〜10名とした。評価項目は、(1)眼への装着し易さ(眼に入り易さ)、(2)装着直後のレンズ安定感・異物感・ゴロゴロ感、(3)装着直後の視界良好性の3項目で、実施例2の処方と、比較例1、3、4、5、6の各処方とをそれぞれ比較し、より使用感が良いと思われる方を選択する方法で行った。また、追加の評価項目として、(4)指に残った液の感触(ベタベタ感)について、実施例2の処方と、比較例4、5、6とをそれぞれ比較し、より使用感が良いと思われる方を選択した。結果を表2〜6に示す。表中、結果の表記は、全体の人数に対する、それぞれの回答を選んだ人数の割合(%)である。「同じ」は実施例と比較例とに差異がないとの回答を意味する。尚、被験者の使用したコンタクトレンズの種類は、以下の通りである。
・SCL1:商品名:メダリスト、ボシュロム社製、主素材:Poly-HEMA、ソフトコンタクトレンズ分類グループI
・SCL2:商品名:ワンデーアキュビュー、ジョンソン&ジョンソン社製、主素材:EtafilconA、ソフトコンタクトレンズ分類グループIV
・SCL3:商品名:オーツーオプティクス、チバビジョン社製、主素材:LotrafilconA(シリコーンハイドロゲル素材)、ソフトコンタクトレンズ分類グループI
・SCL4:商品名:メニコンZ、メニコン社製、主素材:シロキサニルスチレン、フルオロメタクリレート等、酸素透過性ハードコンタクトレンズ
Test 1: Usability test (1)
In accordance with the formulation described in Table 1, each contact lens mounting solution was prepared according to a preparation method (ordinary method) such as ophthalmic solution, filled into a polyethylene terephthalate container (capacity 10 mL), and plugged. Both surfaces of the contact lens were wetted with 1 to 3 drops of each contact lens mounting solution, and then mounted on the eyes to evaluate the feeling of use. The subjects were 8 to 10 people who used contact lenses on a daily basis. The evaluation items were (1) Ease of wearing on the eye (ease of entering the eye), (2) Lens stability immediately after wearing, sense of foreign body, groovy feeling, and (3) Good visibility after wearing. Thus, the prescription of Example 2 was compared with the prescriptions of Comparative Examples 1, 3, 4, 5, and 6, respectively, and the method that selected the one that seems to have a better usability was selected. In addition, as an additional evaluation item, (4) About the feel of the liquid remaining on the finger (sticky feeling), the prescription of Example 2 is compared with Comparative Examples 4, 5, and 6, and the feeling of use is better. The one that seems to be selected. The results are shown in Tables 2-6. In the table, the result notation is the ratio (%) of the total number of people who selected each answer. “Same” means an answer that there is no difference between the example and the comparative example. The types of contact lenses used by the subjects are as follows.
・ SCL1: Product name: Medalist, manufactured by Bochrom, Main material: Poly-HEMA, Soft contact lens classification group I
・ SCL2: Product name: One Day Accuview, made by Johnson & Johnson, Main material: EtafilconA, Soft contact lens classification group IV
・ SCL3: Product name: Auto-Optics, Ciba Vision, main material: Lotrafilcon A (silicone hydrogel material), soft contact lens classification group I
・ SCL4: Product name: Menicon Z, manufactured by Menicon Corporation, main materials: siloxanyl styrene, fluoromethacrylate, etc., oxygen permeable hard contact lenses
いずれの試験においても、実施例は比較例と比べて、眼への装着し易さ、レンズの安定感・異物感・ゴロゴロ感、装着直後の視界良好性、指に残った液の感触等の全ての点で優れていた。即ち、コンタクトレンズを装着した際に生じる異物感やゴロゴロ感が低減されており、コンタクトレンズが安定に保持されていると感じ、コンタクトレンズ装着直後の視界が良好であった。尚、ポリビニルアルコール又はポリビニルピロリドンを含有する処方は、上記実施例と比較し、明らかに装着直後のレンズ安定性・異物感・ゴロゴロ感が悪いことに加えて、レンズ装着直後の視界が実施例と比較して顕著に劣り、さらに、指に残った液の感触(ベタベタ感)が良好でない等の問題点があった。
以上の傾向は、コンドロイチン硫酸ナトリウムに換えてアスパラギン酸カリウム(実施例1、比較例2)を用いた場合も同様の結果であった。また同様に、コンドロイチン硫酸ナトリウムに替えてアミノエチルスルホン酸、イプシロンアミノカプロン酸を用いることも可能であった。
In any test, compared to the comparative example, the examples are easier to wear on the eye, the lens has a sense of stability / foreignness / roughness, good visibility immediately after wearing, the feel of the liquid remaining on the finger, etc. It was excellent in all respects. That is, the feeling of foreign matter and the groovy feeling generated when the contact lens is worn is reduced, the contact lens is felt to be stably held, and the field of view immediately after the contact lens is worn is good. In addition, the formulation containing polyvinyl alcohol or polyvinyl pyrrolidone is clearly inferior to the above examples in terms of lens stability, foreign object feeling, and groovy feeling immediately after mounting, and the field of view immediately after lens mounting is as in the examples. There were problems such as remarkably inferior compared with each other, and further, the feeling (sticky feeling) of the liquid remaining on the finger was not good.
The above tendency was the same result when potassium aspartate (Example 1, Comparative Example 2) was used instead of sodium chondroitin sulfate. Similarly, aminoethylsulfonic acid and epsilon aminocaproic acid could be used instead of chondroitin sulfate sodium.
試験2:レンズ形状への影響(1)
ソフトコンタクトレンズ(SCL5:商品名:2ウィークアキュビュー、J&J社、主素材:EtafilconA、ソフトコンタクトレンズ分類グループIV)を生理食塩水に一晩以上浸漬(4mL/枚)したのち、レンズ直径を万能投影機 V−12A(株式会社ニコン)にて測定し、浸漬前直径とした。試験1で用いた各コンタクトレンズ装着液に前記ソフトコンタクトレンズを一晩以上浸漬(4mL/枚)したのち、同様にレンズ直径を測定し、浸漬後直径とした。次いで、直径変化を算出し、評価した。
浸漬後直径変化(mm)=浸漬後直径−浸漬前直径
Soft contact lens (SCL5: Product name: 2 week Accuview, J & J, main material: EtafilconA, soft contact lens classification group IV) is immersed in physiological saline for more than one night (4mL / piece), then the lens diameter is universal projection Measured with a machine V-12A (Nikon Corporation) and used as the diameter before immersion. After immersing the soft contact lens in each contact lens mounting solution used in Test 1 overnight (4 mL / sheet), the lens diameter was measured in the same manner as the post-immersion diameter. The diameter change was then calculated and evaluated.
Diameter change after immersion (mm) = Diameter after immersion-Diameter before immersion
試験3:脂質汚れ付着防止効果
ソフトコンタクトレンズ(前述のSCL3)を生理食塩液に一晩以上浸漬(4mL/枚)したのち、試験1で用いた各コンタクトレンズ装着液に一晩以上浸漬(4mL/枚)した。さらに、該ソフトコンタクトレンズを脂質汚れ液に8時間浸漬(4mL/枚)したのち、生理食塩液で軽くすすぎ、レンズに付着した脂質を溶出させて定量した。その結果、実施例における脂質付着量は僅かであり、脂質の付着が防止されていた。
以上の結果は、実施例処方が、手指などからの脂質がコンタクトレンズに付着することを防止する効果を有することを示している。脂質付着の防止効果は、本発明のコンタクトレンズ装着液の、ゴロゴロ感や異物感の抑制作用に寄与していると考えられる。
Test 3: Anti-fouling adhesion effect After soaking a soft contact lens (SCL3 mentioned above) in physiological saline overnight (4 mL / sheet), soak it overnight in each contact lens mounting solution used in test 1 (4 mL) /). Further, the soft contact lens was immersed in a lipid soil solution for 8 hours (4 mL / plate), then rinsed lightly with physiological saline, and the lipid adhering to the lens was eluted and quantified. As a result, the amount of lipid adhesion in the examples was small, and lipid adhesion was prevented.
The above result has shown that an Example prescription has the effect which prevents the lipid from fingers etc. adhering to a contact lens. It is considered that the effect of preventing lipid adhesion contributes to the action of suppressing contact with the contact lens mounting liquid of the present invention.
試験4:使用感試験(2)
表1の実施例1、2、比較例1〜3、表8の実施例3、4、比較例7、8に従い、各コンタクトレンズ装着液処方を点眼液等の調製方法(常法)に従って調製し、ポリエチレンテレフタレート製容器(容量10mL)に充填し、施栓した。コンタクトレンズの両面を各コンタクトレンズ装着液1〜3滴でぬらした後、目に装着し、使用感を評価した。被験者は、日常的にコンタクトレンズを使用している8〜9名とした。評価項目は、試験1と同様の項目を含む以下の6項目である。(1)目に装着する時のレンズの指からの離れ易さ、(2)レンズの眼への装着し易さ(眼に入り易さ)、(3)装着直後のレンズ安定感・異物感・ゴロゴロ感、(4)レンズ装着直後の視界良好性、(6)指に残った装着液の感触(ベタベタ感)、(6)レンズを装着し直す時の操作性(レンズが開き易い等)の6項目である。各表に示す組み合わせで実施例の処方と、比較例の各処方とをそれぞれ比較し、より使用感が良いと思われる方を選択する方法で評価を行った。結果を表9〜15に示す。表中、結果の表記は、全体の人数に対する、それぞれの回答を選んだ人数の割合(%)である。「同じ」は実施例と比較例とに差異がないとの回答を意味する。尚、被験者の使用したコンタクトレンズの種類は、SCL1、SCL2、SCL3、SCL4である。
Test 4: Usability test (2)
According to Examples 1 and 2 in Table 1, Comparative Examples 1 to 3 and Examples 3 and 4 in Table 8 and Comparative Examples 7 and 8, each contact lens mounting liquid formulation is prepared according to a preparation method (ordinary method) such as eye drops. Then, it was filled in a polyethylene terephthalate container (capacity 10 mL) and plugged. Both surfaces of the contact lens were wetted with 1 to 3 drops of each contact lens mounting solution, and then mounted on the eyes to evaluate the feeling of use. The subjects were 8 to 9 people who used contact lenses on a daily basis. The evaluation items are the following six items including the same items as in Test 1. (1) Easier to remove the lens from the finger when wearing the eye, (2) Ease of attaching the lens to the eye (ease of entering the eye), (3) Lens stability and foreign body feeling immediately after wearing・ Rough feeling, (4) Good visibility immediately after lens mounting, (6) Feeling of mounting fluid left on fingers (solid feeling), (6) Operability when re-installing lens (lens is easy to open, etc.) 6 items. The prescriptions of the examples and the prescriptions of the comparative examples were compared with each other in the combinations shown in each table, and evaluation was performed by selecting a method that seems to have a better usability. The results are shown in Tables 9-15. In the table, the result notation is the ratio (%) of the total number of people who selected each answer. “Same” means an answer that there is no difference between the example and the comparative example. The types of contact lenses used by the subjects are SCL1, SCL2, SCL3, and SCL4.
いずれの比較試験においても、実施例は比較例と比較し、全ての評価項目において優れた結果を示した。また、表には詳しく結果を示していないが、装着液を滴下した時のレンズの形状保持 についても、表9〜15の比較試験全てについて実施例のほうが良い結果となった。特に、表12(実施例3と比較例1の比較)では、実施例3のほうが良いと回答した被験者が75%以上と、効果が高かった。
尚、ポリビニルピロリドンを含む比較例では、ポリビニルピロリドンを含まない実施例と比較して明らかに試験結果が劣っており、ポリビニルピロリドンを含有しない事が好ましい、という事が明らかとなった。
In any of the comparative tests, the examples showed superior results in all the evaluation items as compared with the comparative examples. Further, although the results are not shown in detail in the table, the results of the examples were better for all of the comparative tests in Tables 9 to 15 for maintaining the shape of the lens when the mounting solution was dropped. In particular, in Table 12 (comparison between Example 3 and Comparative Example 1), 75% or more of the subjects who answered that Example 3 was better were highly effective.
The comparative example containing polyvinyl pyrrolidone was clearly inferior in test results as compared with the examples not containing polyvinyl pyrrolidone, and it was found that it is preferable not to contain polyvinyl pyrrolidone.
試験5:レンズ形状への影響(2)
前述のSCL2を生理食塩水に一晩以上浸漬(4mL/枚)したのち、レンズ直径を万能投影機 V−12A(株式会社ニコン)にて測定し、浸漬前直径とした。表1及び表8で使用した実施例1〜4及び比較例9の各試験液を用い、これらのコンタクトレンズ装着液に前記ソフトコンタクトレンズを一晩以上浸漬(4mL/枚)したのちレンズ直径を測定し、浸漬後直径とした。その後再び生理食塩液に前記ソフトコンタクトレンズを一晩以上浸漬(4mL/枚)したのち同様にレンズ直径を測定し、溶出後直径とした。直径変化を算出し、評価した。
浸漬後直径変化(mm)=浸漬後直径−浸漬前直径
溶出後直径変化(mm)=溶出後直径−浸漬前直径
また、生理食塩液に再浸漬した後、実施例処方ではレンズサイズがほぼ元に戻っており、サイズ変化が可逆的であったことを示している。これに対して、比較例8ではレンズサイズが戻り難く、サイズ変化が不可逆的であったと考えられる。このような不可逆的なサイズ変化は、特に、繰り返し使用するタイプのコンタクトレンズの場合、変化の累積による影響が問題となる。しかし、本発明のコンタクトレンズ装着液ではサイズ変化が小さいうえ、可逆的であるため、繰り返し使用するタイプのコンタクトレンズに対しても、好適に使用する事が可能である。実際、例示のSCL2(使い捨てタイプ)と同一素材のSCL5(非使い捨て(2週間交換)タイプ)を用いて同様の試験を行ったところ、SCL2と同様の結果が得られた。
Test 5: Effect on lens shape (2)
After the aforementioned SCL2 was immersed in physiological saline overnight (4 mL / sheet), the lens diameter was measured with a universal projector V-12A (Nikon Corporation) to obtain the diameter before immersion. Using each test solution of Examples 1 to 4 and Comparative Example 9 used in Table 1 and Table 8, the soft contact lens was immersed in these contact lens mounting solutions for more than one night (4 mL / sheet), and then the lens diameter was determined. Measured and made the diameter after immersion. Thereafter, the soft contact lens was again immersed in physiological saline for one night or more (4 mL / sheet), and the lens diameter was measured in the same manner to obtain a diameter after elution. The diameter change was calculated and evaluated.
Diameter change after immersion (mm) = Diameter after immersion-Diameter before immersion Diameter change after elution (mm) = Diameter after elution-Diameter before immersion
In addition, after re-immersing in physiological saline, the lens size was almost restored to the original in the prescriptions of Examples, indicating that the size change was reversible. On the other hand, in Comparative Example 8, it is considered that the lens size is difficult to return and the size change is irreversible. Such an irreversible size change is particularly problematic in the case of contact lenses that are repeatedly used. However, since the contact lens mounting liquid of the present invention has a small size change and is reversible, it can be suitably used for contact lenses that are used repeatedly. Actually, when the same test was performed using SCL5 (non-disposable (two-week exchange) type) of the same material as the exemplary SCL2 (disposable type), the same result as SCL2 was obtained.
試験3:脂質汚れ付着防止効果
表1の実施例1及び比較例2、及び、表8の実施例3、4、比較例7、8及び9に記載された処方に従い、各コンタクトレンズ装着液を調製した。ソフトコンタクトレンズ(前述のSCL3)を生理食塩液に一晩以上浸漬(4mL/枚)したのち、各コンタクトレンズ装着液に、4時間浸漬(2mL/枚)した。さらに、該ソフトコンタクトレンズを脂質汚れ液に4時間浸漬(2mL/枚)したのち、レンズを精製水で軽くすすぎ、室温で減圧下に16時間以上乾燥した。レンズに付着した脂質をエタノール:エーテル=3:1溶液にて室温で1時間抽出したのち(1mL/枚)、抽出溶媒を90度の湯浴で加熱して除去した。残留物に無水エタノール0.1mLおよび濃硫酸5mLを加えて90℃の湯浴で30分間加熱した。室温まで冷却した後、0.4mLを採取してバニリン溶液0.6mL(バニリン0.6gを無水エタノール8mLに溶解させたのち、精製水にて100mLに調製した液から50mLを採取し、リン酸200mLに添加する)を加えて37℃で15分間加温した。200μLを96ウェルマルチプレートに取り、分光光度計にて525nm吸光度を測定した。尚、オリーブ油(日光ケミカル製)を標準品として別途検量線を作成して求められた下記式により、脂質付着量を算出した。
以上の通り、実施例処方において、脂質付着抑制効果が確認された。またデータは示さないが、実施例2(表1)においても、実施例3と同等の効果が確認された。この結果は、本発明のコンタクトレンズ装着液が、手指などからの脂質がコンタクトレンズに付着することを防止する効果を有することを示している。脂質付着は、コンタクトレンズの見え易さにも影響する事から、脂質付着を防止することにより、コンタクトレンズが本来有している視機能を十分に発揮させる事が可能である。また、脂質付着によるコンタクトレンズ材質への影響も軽減される事から、材質劣化によるコンタクトレンズの寿命短縮を抑制し、安全にレンズを装用する事が可能となる。さらに、これらの機能的側面のみならず、コンタクトレンズ装着液の、ゴロゴロ感や異物感の抑制作用にも寄与していると考えられる。
Test 3: Effect of preventing lipid stain adhesion According to the formulations described in Example 1 and Comparative Example 2 in Table 1 and Examples 3 and 4 and Comparative Examples 7, 8 and 9 in Table 8, each contact lens mounting solution was used. Prepared. The soft contact lens (SCL3 described above) was immersed in physiological saline overnight (4 mL / sheet) and then immersed in each contact lens mounting solution for 4 hours (2 mL / sheet). Further, after the soft contact lens was immersed in a lipid soil solution for 4 hours (2 mL / sheet), the lens was lightly rinsed with purified water and dried at room temperature under reduced pressure for 16 hours or more. The lipid adhering to the lens was extracted with an ethanol: ether = 3: 1 solution at room temperature for 1 hour (1 mL / plate), and then the extraction solvent was removed by heating in a 90-degree water bath. To the residue were added anhydrous ethanol (0.1 mL) and concentrated sulfuric acid (5 mL), and the mixture was heated in a 90 ° C. water bath for 30 minutes. After cooling to room temperature, 0.4 mL is collected and 0.6 mL of vanillin solution (0.6 mL of vanillin is dissolved in 8 mL of absolute ethanol, then 50 mL is collected from the solution prepared to 100 mL with purified water and added to 200 mL of phosphoric acid. And heated at 37 ° C. for 15 minutes. 200 μL was taken in a 96-well multiplate, and the absorbance at 525 nm was measured with a spectrophotometer. In addition, the amount of lipid adhesion was calculated by the following formula obtained by preparing a separate calibration curve using olive oil (manufactured by Nikko Chemical) as a standard product.
As described above, the lipid adhesion inhibitory effect was confirmed in the example formulations. Moreover, although data are not shown, the same effect as Example 3 was confirmed also in Example 2 (Table 1). This result shows that the contact lens mounting liquid of the present invention has an effect of preventing lipids from fingers and the like from adhering to the contact lens. Since lipid adhesion also affects the visibility of the contact lens, it is possible to sufficiently exhibit the visual function inherent in the contact lens by preventing lipid adhesion. In addition, since the influence on the contact lens material due to lipid adhesion is reduced, it is possible to suppress the shortening of the life of the contact lens due to material deterioration and to wear the lens safely. Furthermore, it is thought that it contributes not only to these functional aspects but also to the suppression effect of the contact lens mounting liquid on the feeling of lingering and foreign objects.
処方例1−87
表18−23に記載の処方で、コンタクトレンズ装着液(処方例1−87)を調製した。処方例に記載するヒドロキシエチルセルロースは、商品名:CF-V (住友精化株式会社製)を使用し、ヒドロキシプロピルメチルセルロース2906は、商品名:65SH-4000 (信越化学工業株式会社製)を使用した。なお、表18−23中、各配合成分の単位はg/100mLである。
Formulation Example 1-87
A contact lens mounting solution (Formulation Example 1-87) was prepared according to the formulation shown in Table 18-23. The hydroxyethyl cellulose described in the formulation example used the product name: CF-V (manufactured by Sumitomo Seika Co., Ltd.), and the hydroxypropyl methylcellulose 2906 used the product name: 65SH-4000 (manufactured by Shin-Etsu Chemical Co., Ltd.). . In Table 18-23, the unit of each compounding component is g / 100 mL.
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WO2012066655A1 (en) * | 2010-11-17 | 2012-05-24 | 株式会社メニコン | Method for fitting soft contact lens, contact lens solution, and soft contact lens package |
JP2019142979A (en) * | 2012-09-27 | 2019-08-29 | 千寿製薬株式会社 | Aqueous liquid formulation |
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JP2014101391A (en) * | 2009-12-02 | 2014-06-05 | Rohto Pharmaceut Co Ltd | Ophthalmological composition for silicone hydrogel contact lens |
WO2012066655A1 (en) * | 2010-11-17 | 2012-05-24 | 株式会社メニコン | Method for fitting soft contact lens, contact lens solution, and soft contact lens package |
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