WO1996008244A1 - Eye drops for repairing corneal disturbance - Google Patents
Eye drops for repairing corneal disturbance Download PDFInfo
- Publication number
- WO1996008244A1 WO1996008244A1 PCT/JP1995/001830 JP9501830W WO9608244A1 WO 1996008244 A1 WO1996008244 A1 WO 1996008244A1 JP 9501830 W JP9501830 W JP 9501830W WO 9608244 A1 WO9608244 A1 WO 9608244A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- chloride
- ophthalmic solution
- sodium
- taurine
- osmotic pressure
- Prior art date
Links
- 239000003889 eye drop Substances 0.000 title abstract description 7
- 229940012356 eye drops Drugs 0.000 title abstract description 7
- XOAAWQZATWQOTB-UHFFFAOYSA-N taurine Chemical compound NCCS(O)(=O)=O XOAAWQZATWQOTB-UHFFFAOYSA-N 0.000 claims abstract description 32
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims abstract description 24
- 230000003204 osmotic effect Effects 0.000 claims abstract description 16
- 229960003080 taurine Drugs 0.000 claims abstract description 16
- 235000002639 sodium chloride Nutrition 0.000 claims abstract description 14
- 239000011780 sodium chloride Substances 0.000 claims abstract description 12
- 239000002997 ophthalmic solution Substances 0.000 claims description 29
- 229940054534 ophthalmic solution Drugs 0.000 claims description 29
- CSNNHWWHGAXBCP-UHFFFAOYSA-L Magnesium sulfate Chemical compound [Mg+2].[O-][S+2]([O-])([O-])[O-] CSNNHWWHGAXBCP-UHFFFAOYSA-L 0.000 claims description 10
- 208000021921 corneal disease Diseases 0.000 claims description 7
- UXVMQQNJUSDDNG-UHFFFAOYSA-L Calcium chloride Chemical compound [Cl-].[Cl-].[Ca+2] UXVMQQNJUSDDNG-UHFFFAOYSA-L 0.000 claims description 6
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims description 6
- 239000001110 calcium chloride Substances 0.000 claims description 6
- 229910001628 calcium chloride Inorganic materials 0.000 claims description 6
- 235000011148 calcium chloride Nutrition 0.000 claims description 6
- 239000008103 glucose Substances 0.000 claims description 6
- 229910052943 magnesium sulfate Inorganic materials 0.000 claims description 5
- 235000019341 magnesium sulphate Nutrition 0.000 claims description 5
- UIIMBOGNXHQVGW-DEQYMQKBSA-M Sodium bicarbonate-14C Chemical compound [Na+].O[14C]([O-])=O UIIMBOGNXHQVGW-DEQYMQKBSA-M 0.000 claims description 3
- 150000003839 salts Chemical class 0.000 claims description 2
- IXCSERBJSXMMFS-UHFFFAOYSA-N hcl hcl Chemical compound Cl.Cl IXCSERBJSXMMFS-UHFFFAOYSA-N 0.000 claims 1
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 abstract description 18
- WCUXLLCKKVVCTQ-UHFFFAOYSA-M Potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 abstract description 16
- 235000017557 sodium bicarbonate Nutrition 0.000 abstract description 9
- 229910000030 sodium bicarbonate Inorganic materials 0.000 abstract description 9
- 239000001103 potassium chloride Substances 0.000 abstract description 8
- 235000011164 potassium chloride Nutrition 0.000 abstract description 8
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 17
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 15
- 239000008213 purified water Substances 0.000 description 15
- 230000000694 effects Effects 0.000 description 8
- 102000003855 L-lactate dehydrogenase Human genes 0.000 description 7
- 108700023483 L-lactate dehydrogenases Proteins 0.000 description 7
- 238000005259 measurement Methods 0.000 description 6
- 208000028006 Corneal injury Diseases 0.000 description 5
- 238000009281 ultraviolet germicidal irradiation Methods 0.000 description 4
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
- 229910021538 borax Inorganic materials 0.000 description 3
- 210000004087 cornea Anatomy 0.000 description 3
- 239000004328 sodium tetraborate Substances 0.000 description 3
- 235000010339 sodium tetraborate Nutrition 0.000 description 3
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 2
- 239000002253 acid Substances 0.000 description 2
- POJWUDADGALRAB-UHFFFAOYSA-N allantoin Chemical compound NC(=O)NC1NC(=O)NC1=O POJWUDADGALRAB-UHFFFAOYSA-N 0.000 description 2
- KGBXLFKZBHKPEV-UHFFFAOYSA-N boric acid Chemical compound OB(O)O KGBXLFKZBHKPEV-UHFFFAOYSA-N 0.000 description 2
- 239000004327 boric acid Substances 0.000 description 2
- 239000006196 drop Substances 0.000 description 2
- -1 etc.) Substances 0.000 description 2
- 229910017053 inorganic salt Inorganic materials 0.000 description 2
- KWGKDLIKAYFUFQ-UHFFFAOYSA-M lithium chloride Chemical compound [Li+].[Cl-] KWGKDLIKAYFUFQ-UHFFFAOYSA-M 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
- 229960000342 retinol acetate Drugs 0.000 description 2
- 235000019173 retinyl acetate Nutrition 0.000 description 2
- 239000011770 retinyl acetate Substances 0.000 description 2
- 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 2
- 239000011734 sodium Substances 0.000 description 2
- 229910052708 sodium Inorganic materials 0.000 description 2
- 159000000000 sodium salts Chemical class 0.000 description 2
- NOOLISFMXDJSKH-UTLUCORTSA-N (+)-Neomenthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@@H]1O NOOLISFMXDJSKH-UTLUCORTSA-N 0.000 description 1
- DTGKSKDOIYIVQL-WEDXCCLWSA-N (+)-borneol Chemical compound C1C[C@@]2(C)[C@@H](O)C[C@@H]1C2(C)C DTGKSKDOIYIVQL-WEDXCCLWSA-N 0.000 description 1
- REPVLJRCJUVQFA-UHFFFAOYSA-N (-)-isopinocampheol Natural products C1C(O)C(C)C2C(C)(C)C1C2 REPVLJRCJUVQFA-UHFFFAOYSA-N 0.000 description 1
- RBCOYOYDYNXAFA-UHFFFAOYSA-L (5-hydroxy-4,6-dimethylpyridin-3-yl)methyl phosphate Chemical compound CC1=NC=C(COP([O-])([O-])=O)C(C)=C1O RBCOYOYDYNXAFA-UHFFFAOYSA-L 0.000 description 1
- DSSYKIVIOFKYAU-XCBNKYQSSA-N (R)-camphor Chemical compound C1C[C@@]2(C)C(=O)C[C@@H]1C2(C)C DSSYKIVIOFKYAU-XCBNKYQSSA-N 0.000 description 1
- CIVCELMLGDGMKZ-UHFFFAOYSA-N 2,4-dichloro-6-methylpyridine-3-carboxylic acid Chemical compound CC1=CC(Cl)=C(C(O)=O)C(Cl)=N1 CIVCELMLGDGMKZ-UHFFFAOYSA-N 0.000 description 1
- SLXKOJJOQWFEFD-UHFFFAOYSA-N 6-aminohexanoic acid Chemical compound NCCCCCC(O)=O SLXKOJJOQWFEFD-UHFFFAOYSA-N 0.000 description 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 1
- POJWUDADGALRAB-PVQJCKRUSA-N Allantoin Natural products NC(=O)N[C@@H]1NC(=O)NC1=O POJWUDADGALRAB-PVQJCKRUSA-N 0.000 description 1
- 241000272875 Ardeidae Species 0.000 description 1
- VKJGBAJNNALVAV-UHFFFAOYSA-M Berberine chloride (TN) Chemical compound [Cl-].C1=C2CC[N+]3=CC4=C(OC)C(OC)=CC=C4C=C3C2=CC2=C1OCO2 VKJGBAJNNALVAV-UHFFFAOYSA-M 0.000 description 1
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 1
- 241000723346 Cinnamomum camphora Species 0.000 description 1
- ZAKOWWREFLAJOT-CEFNRUSXSA-N D-alpha-tocopherylacetate Chemical compound CC(=O)OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C ZAKOWWREFLAJOT-CEFNRUSXSA-N 0.000 description 1
- SNPLKNRPJHDVJA-ZETCQYMHSA-N D-panthenol Chemical compound OCC(C)(C)[C@@H](O)C(=O)NCCCO SNPLKNRPJHDVJA-ZETCQYMHSA-N 0.000 description 1
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 description 1
- 208000003556 Dry Eye Syndromes Diseases 0.000 description 1
- 206010013774 Dry eye Diseases 0.000 description 1
- 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 1
- BIVBRWYINDPWKA-VLQRKCJKSA-L Glycyrrhizinate dipotassium Chemical compound [K+].[K+].O([C@@H]1[C@@H](O)[C@H](O)[C@H](O[C@@H]1O[C@H]1CC[C@]2(C)[C@H]3C(=O)C=C4[C@@H]5C[C@](C)(CC[C@@]5(CC[C@@]4(C)[C@]3(C)CC[C@H]2C1(C)C)C)C(O)=O)C([O-])=O)[C@@H]1O[C@H](C([O-])=O)[C@@H](O)[C@H](O)[C@H]1O BIVBRWYINDPWKA-VLQRKCJKSA-L 0.000 description 1
- 102000006835 Lamins Human genes 0.000 description 1
- 108010047294 Lamins Proteins 0.000 description 1
- 102000016943 Muramidase Human genes 0.000 description 1
- 108010014251 Muramidase Proteins 0.000 description 1
- 108010062010 N-Acetylmuramoyl-L-alanine Amidase Proteins 0.000 description 1
- DJDFFEBSKJCGHC-UHFFFAOYSA-N Naphazoline Chemical compound Cl.C=1C=CC2=CC=CC=C2C=1CC1=NCCN1 DJDFFEBSKJCGHC-UHFFFAOYSA-N 0.000 description 1
- 239000004372 Polyvinyl alcohol Substances 0.000 description 1
- AUNGANRZJHBGPY-SCRDCRAPSA-N Riboflavin Chemical compound OC[C@@H](O)[C@@H](O)[C@@H](O)CN1C=2C=C(C)C(C)=CC=2N=C2C1=NC(=O)NC2=O AUNGANRZJHBGPY-SCRDCRAPSA-N 0.000 description 1
- 235000002595 Solanum tuberosum Nutrition 0.000 description 1
- 244000061456 Solanum tuberosum Species 0.000 description 1
- 229930003270 Vitamin B Natural products 0.000 description 1
- CANRESZKMUPMAE-UHFFFAOYSA-L Zinc lactate Chemical compound [Zn+2].CC(O)C([O-])=O.CC(O)C([O-])=O CANRESZKMUPMAE-UHFFFAOYSA-L 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 229960000458 allantoin Drugs 0.000 description 1
- 229940024606 amino acid Drugs 0.000 description 1
- 150000001413 amino acids Chemical class 0.000 description 1
- 229960002684 aminocaproic acid Drugs 0.000 description 1
- 229940121363 anti-inflammatory agent Drugs 0.000 description 1
- 239000002260 anti-inflammatory agent Substances 0.000 description 1
- 229940125715 antihistaminic agent Drugs 0.000 description 1
- 239000000739 antihistaminic agent Substances 0.000 description 1
- 239000000607 artificial tear Substances 0.000 description 1
- 229960000686 benzalkonium chloride Drugs 0.000 description 1
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 description 1
- OJVABJMSSDUECT-UHFFFAOYSA-L berberin sulfate Chemical compound [O-]S([O-])(=O)=O.C1=C2CC[N+]3=CC4=C(OC)C(OC)=CC=C4C=C3C2=CC2=C1OCO2.C1=C2CC[N+]3=CC4=C(OC)C(OC)=CC=C4C=C3C2=CC2=C1OCO2 OJVABJMSSDUECT-UHFFFAOYSA-L 0.000 description 1
- CKDOCTFBFTVPSN-UHFFFAOYSA-N borneol Natural products C1CC2(C)C(C)CC1C2(C)C CKDOCTFBFTVPSN-UHFFFAOYSA-N 0.000 description 1
- 229940116229 borneol Drugs 0.000 description 1
- 244000309464 bull Species 0.000 description 1
- 239000011575 calcium Substances 0.000 description 1
- 229910052791 calcium Inorganic materials 0.000 description 1
- 229930008380 camphor Natural products 0.000 description 1
- 229960000846 camphor Drugs 0.000 description 1
- 150000001805 chlorine compounds Chemical class 0.000 description 1
- 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 1
- ZAKOWWREFLAJOT-UHFFFAOYSA-N d-alpha-Tocopheryl acetate Natural products CC(=O)OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C ZAKOWWREFLAJOT-UHFFFAOYSA-N 0.000 description 1
- 239000000850 decongestant Substances 0.000 description 1
- 229940124581 decongestants Drugs 0.000 description 1
- 229960000525 diphenhydramine hydrochloride Drugs 0.000 description 1
- 229940101029 dipotassium glycyrrhizinate Drugs 0.000 description 1
- IKALZAKZWHFNIC-JIZZDEOASA-L dipotassium;(2s)-2-aminobutanedioate Chemical compound [K+].[K+].[O-]C(=O)[C@@H](N)CC([O-])=O IKALZAKZWHFNIC-JIZZDEOASA-L 0.000 description 1
- DTGKSKDOIYIVQL-UHFFFAOYSA-N dl-isoborneol Natural products C1CC2(C)C(O)CC1C2(C)C DTGKSKDOIYIVQL-UHFFFAOYSA-N 0.000 description 1
- 229940071106 ethylenediaminetetraacetate Drugs 0.000 description 1
- VWWQXMAJTJZDQX-UYBVJOGSSA-N flavin adenine dinucleotide Chemical compound C1=NC2=C(N)N=CN=C2N1[C@@H]([C@H](O)[C@@H]1O)O[C@@H]1CO[P@](O)(=O)O[P@@](O)(=O)OC[C@@H](O)[C@@H](O)[C@@H](O)CN1C2=NC(=O)NC(=O)C2=NC2=C1C=C(C)C(C)=C2 VWWQXMAJTJZDQX-UYBVJOGSSA-N 0.000 description 1
- 235000019162 flavin adenine dinucleotide Nutrition 0.000 description 1
- 239000011714 flavin adenine dinucleotide Substances 0.000 description 1
- 229940093632 flavin-adenine dinucleotide Drugs 0.000 description 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 description 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 210000005053 lamin Anatomy 0.000 description 1
- 239000004325 lysozyme Substances 0.000 description 1
- 235000010335 lysozyme Nutrition 0.000 description 1
- 229960000274 lysozyme Drugs 0.000 description 1
- RXMQCXCANMAVIO-CEOVSRFSSA-L magnesium;(2s)-2-amino-4-hydroxy-4-oxobutanoate Chemical compound [H+].[H+].[Mg+2].[O-]C(=O)[C@@H](N)CC([O-])=O.[O-]C(=O)[C@@H](N)CC([O-])=O RXMQCXCANMAVIO-CEOVSRFSSA-L 0.000 description 1
- LVBRFZFUCKKGDJ-HJWRJIQTSA-J magnesium;dipotassium;(2s)-2-aminobutanedioate;hydron Chemical compound [Mg+2].[K+].[K+].OC(=O)[C@@H](N)CC([O-])=O.OC(=O)[C@@H](N)CC([O-])=O.[O-]C(=O)[C@@H](N)CC(O)=O.[O-]C(=O)[C@@H](N)CC(O)=O LVBRFZFUCKKGDJ-HJWRJIQTSA-J 0.000 description 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
- 229940041616 menthol Drugs 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 229960004760 naphazoline hydrochloride Drugs 0.000 description 1
- 239000003002 pH adjusting agent Substances 0.000 description 1
- 229940101267 panthenol Drugs 0.000 description 1
- 235000020957 pantothenol Nutrition 0.000 description 1
- 239000011619 pantothenol Substances 0.000 description 1
- 229960003733 phenylephrine hydrochloride Drugs 0.000 description 1
- OCYSGIYOVXAGKQ-FVGYRXGTSA-N phenylephrine hydrochloride Chemical compound [H+].[Cl-].CNC[C@H](O)C1=CC=CC(O)=C1 OCYSGIYOVXAGKQ-FVGYRXGTSA-N 0.000 description 1
- 239000002504 physiological saline solution Substances 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 238000011176 pooling Methods 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- JUJWROOIHBZHMG-UHFFFAOYSA-O pyridinium Chemical compound C1=CC=[NH+]C=C1 JUJWROOIHBZHMG-UHFFFAOYSA-O 0.000 description 1
- 238000005070 sampling Methods 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
- 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
- SRWFBFUYENBCGF-UHFFFAOYSA-M sodium;chloride;hydrochloride Chemical compound [Na+].Cl.[Cl-] SRWFBFUYENBCGF-UHFFFAOYSA-M 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 150000005846 sugar alcohols Polymers 0.000 description 1
- 238000010998 test method Methods 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
- 229940042585 tocopherol acetate Drugs 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 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
- 229940088594 vitamin Drugs 0.000 description 1
- 235000019156 vitamin B Nutrition 0.000 description 1
- 239000011720 vitamin B Substances 0.000 description 1
- 238000005303 weighing Methods 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
Classifications
-
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
-
- 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
-
- 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
- A61K31/13—Amines
- A61K31/14—Quaternary ammonium compounds, e.g. edrophonium, choline
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/14—Alkali metal chlorides; Alkaline earth metal chlorides
-
- 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
Definitions
- the present invention relates to an ophthalmic solution comprising a specific inorganic salt, taurine, and the like for the purpose of repairing a corneal disorder.
- Corneal damage is caused by wearing a contact lens, ultraviolet rays, dry eye, etc. Conventionally, in repairing such corneal damage, artificial tears composed of boric acid, sodium chloride, potassium chloride, calcium chloride, etc. are used. Had been.
- the conventional technology has insufficient corneal damage repair effect or has a problem in safety.
- An object of the present invention is to provide an ophthalmic solution which has a high effect of repairing corneal disorders and is safe even when continuously instilled.
- the present invention comprises (a) sodium chloride, sodium chloride chloride and sodium bicarbonate, and (b) 0.5 to 3% by weight of taurine, ⁇ H is 5.5 to 8.0, and osmotic pressure is It is an ophthalmic solution for repairing a corneal disorder having a diameter of 250 to 45 OmO sm.
- the effects of the present invention cannot be obtained with an ophthalmic solution from which either the component (a) or the component (b) has been omitted, and an ophthalmic solution having a pH or osmotic pressure outside the above ranges. But the same is true.
- the pH is preferably in the range of 6.5 to 7.5, and the osmotic pressure is preferably in the range of 250 to 35 OmOsm, with pH 7.4 and osmotic pressure of 286 mOsm being most preferred.
- the ophthalmic solution of the present invention is prepared by dissolving the inorganic salt containing the component (a), the component (b) and preferably glucose in an amount such that the osmotic pressure becomes 250 to 450 mOsm in sterilized purified water. Then, it can be easily prepared by adjusting the pH to 5.58.0 with a pH adjuster (for example, borax, cunic acid, sodium citrate, hydrochloric acid, sodium hydroxide, etc.).
- a pH adjuster for example, borax, cunic acid, sodium citrate, hydrochloric acid, sodium hydroxide, etc.
- anti-inflammatory agents eg, dipotassium glycyrrhizinate, epsilon aminocaproic acid, allantoin, berberine chloride, berberine sulfate, sodium azulene sulfonate, zinc sulfate) , Zinc lactate, lysozyme chloride, etc.
- antihistamines eg, diphenhydramine hydrochloride, chlorfeniramine maleate, etc.
- decongestants such as naphazoline hydrochloride, tetrahydrozoline hydrochloride, phenylephrine hydrochloride
- various vitamins eg, activity type vitamin B 2 (flavin adenine dinucleotide Cleo Tide sodium), vitamin B 6 (HCl pyridinium Dokishin), vitamin B i 2 (Shianoko lamin), vitamin A acetate
- the ophthalmic solution of the present invention acts synergistically on the cornea damaged by sodium bicarbonate and taurine. Also, it does not use boric acid or other irritating ingredients for the eyes, so it is safe to instill continuously. Therefore, the present invention has made it possible to provide an ophthalmic solution useful for repairing corneal disorders.
- Example 2 The ophthalmic solution prepared in Example 2 was instilled into the right eye (3 drops a day, 4 times a day) for 5 days. The left eye was non-instilled.
- LDH leakage was measured before, immediately after, and from 1 to 5 days after irradiation. The measurement was performed by applying 250 drops of physiological saline and pooling for 1 minute as it was, then sampling 50 ⁇ 1 and using an automatic analyzer (7150 Automatic Analyzer, manufactured by HITACHI).
- Table 1 shows the results. At 2 days and 4 days after UV irradiation, the ophthalmic solution prepared in Example 2 was instilled, and a decrease in LDH leakage was observed. That is, when the ophthalmic solution prepared in Example 2 was instilled, the total amount of leaked LDH from immediately after UV irradiation to after 5 after UV irradiation was significantly reduced. This confirmed the effect of the ophthalmic solution of the present invention on corneal damage repair.
- the osmotic pressure of this ophthalmic solution was measured to be 286 mO sm.
- the osmotic pressure of this ophthalmic solution was measured to be 286 mO sm.
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- Health & Medical Sciences (AREA)
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- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Inorganic Chemistry (AREA)
- Ophthalmology & Optometry (AREA)
- Molecular Biology (AREA)
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Description
Claims
Priority Applications (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
AU34848/95A AU3484895A (en) | 1994-09-14 | 1995-09-14 | Eye drops for repairing corneal disturbance |
KR1019970701686A KR970705985A (ko) | 1994-09-14 | 1995-09-14 | 각막 장해 복구용 점안제(Eye Drops for Repairing Corneal Disturbance) |
EP95931411A EP0778021A4 (en) | 1994-09-14 | 1995-09-14 | DROPS TO CARE FOR THE CORNEA |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP6/219917 | 1994-09-14 | ||
JP21991794 | 1994-09-14 |
Publications (1)
Publication Number | Publication Date |
---|---|
WO1996008244A1 true WO1996008244A1 (en) | 1996-03-21 |
Family
ID=16743053
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/JP1995/001830 WO1996008244A1 (en) | 1994-09-14 | 1995-09-14 | Eye drops for repairing corneal disturbance |
Country Status (6)
Country | Link |
---|---|
EP (1) | EP0778021A4 (ja) |
KR (1) | KR970705985A (ja) |
CN (1) | CN1160346A (ja) |
AU (1) | AU3484895A (ja) |
CA (1) | CA2199610A1 (ja) |
WO (1) | WO1996008244A1 (ja) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
RU2733392C1 (ru) * | 2019-08-28 | 2020-10-01 | Федеральное государственное унитарное предприятие "Московский эндокринный завод" | Комбинированное офтальмологическое средство |
Families Citing this family (16)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB2336109A (en) * | 1998-04-07 | 1999-10-13 | Univ Bristol | Ophthalmic Irrigating Solution |
DE10035620B4 (de) * | 2000-07-21 | 2005-07-14 | *Acri.Tec Gesellschaft für ophthalmologische Produkte mbH | Verwendung von Taurin als neuroprotektives Agens in der Ophthalmologie |
GB0123115D0 (en) | 2001-09-26 | 2001-11-14 | Pharma Sol Int Ltd | Saline solutions for clinical use |
US6881750B2 (en) * | 2003-03-04 | 2005-04-19 | Nutrition Corp. Of America, Ltd. | Potassium taurate bicarbonate and ascorbate |
WO2006035969A1 (ja) | 2004-09-28 | 2006-04-06 | Senju Pharmaceutical Co., Ltd. | キサンタンガムおよびアミノ酸を含有する眼科用組成物 |
US8569367B2 (en) * | 2004-11-16 | 2013-10-29 | Allergan, Inc. | Ophthalmic compositions and methods for treating eyes |
KR101401353B1 (ko) * | 2005-07-01 | 2014-05-29 | 시그마타우 인두스트리에 파르마슈티케 리우니테 에스.피.에이. | 점안약의 형태로 안구 사용을 위한 생리적 보조제 또는의약품의 제조를 위한 l-카르니틴 또는 알카노일l-카르니틴의 용도 |
US8168206B1 (en) | 2005-10-06 | 2012-05-01 | Allergan, Inc. | Animal protein-free pharmaceutical compositions |
US8957048B2 (en) | 2011-10-06 | 2015-02-17 | Allergan, Inc. | Compositions for the treatment of dry eye |
US9907826B2 (en) | 2011-12-07 | 2018-03-06 | Allergan, Inc. | Efficient lipid delivery to human tear film using a salt-sensitive emulsion system |
PL2787969T3 (pl) | 2011-12-07 | 2021-12-20 | Allergan, Inc. | Skuteczne dostarczanie lipidów do ludzkiego filmu łzowego z zastosowaniem układu emulsji wrażliwej na sól |
US10279005B2 (en) | 2014-11-25 | 2019-05-07 | Allergan, Inc. | Stabilized omega-3 ophthalmic compositions |
CN107028973B (zh) * | 2017-05-12 | 2020-11-24 | 浙江工贸职业技术学院 | 一种缓解视疲劳用滴眼液及其制备方法 |
EP3829640A4 (en) * | 2018-08-01 | 2022-05-25 | McMaster University | METHOD OF INHIBITING MICROBIAL GROWTH |
FR3088196B1 (fr) * | 2018-11-08 | 2022-03-25 | Abdeslem Alain Kitkit | Dispositif permettant d'ameliorer la vue compose d'une solution dans un flacon avec un traitement et un lavage |
TWI801618B (zh) * | 2019-06-27 | 2023-05-11 | 晶碩光學股份有限公司 | 具有抗氧化功能的隱形眼鏡產品 |
Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS59101421A (ja) * | 1982-11-29 | 1984-06-12 | Kaken Pharmaceut Co Ltd | 眼科用潅流液 |
JPS63208516A (ja) * | 1986-09-04 | 1988-08-30 | ビジヨン フアーマシユーテイカルス、インコーポレーテツド | ビタミンa組成物含有眼科用製剤及びそれによる乾燥及び炎症を起こした眼の治療法 |
JPS6442424A (en) * | 1987-08-08 | 1989-02-14 | Taisho Pharmaceutical Co Ltd | Ophthalmic solution |
-
1995
- 1995-09-14 KR KR1019970701686A patent/KR970705985A/ko not_active Application Discontinuation
- 1995-09-14 AU AU34848/95A patent/AU3484895A/en not_active Abandoned
- 1995-09-14 EP EP95931411A patent/EP0778021A4/en not_active Withdrawn
- 1995-09-14 WO PCT/JP1995/001830 patent/WO1996008244A1/ja not_active Application Discontinuation
- 1995-09-14 CA CA002199610A patent/CA2199610A1/en not_active Abandoned
- 1995-09-14 CN CN95195627A patent/CN1160346A/zh active Pending
Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS59101421A (ja) * | 1982-11-29 | 1984-06-12 | Kaken Pharmaceut Co Ltd | 眼科用潅流液 |
JPS63208516A (ja) * | 1986-09-04 | 1988-08-30 | ビジヨン フアーマシユーテイカルス、インコーポレーテツド | ビタミンa組成物含有眼科用製剤及びそれによる乾燥及び炎症を起こした眼の治療法 |
JPS6442424A (en) * | 1987-08-08 | 1989-02-14 | Taisho Pharmaceutical Co Ltd | Ophthalmic solution |
Non-Patent Citations (1)
Title |
---|
See also references of EP0778021A4 * |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
RU2733392C1 (ru) * | 2019-08-28 | 2020-10-01 | Федеральное государственное унитарное предприятие "Московский эндокринный завод" | Комбинированное офтальмологическое средство |
Also Published As
Publication number | Publication date |
---|---|
EP0778021A1 (en) | 1997-06-11 |
CN1160346A (zh) | 1997-09-24 |
CA2199610A1 (en) | 1996-03-21 |
AU3484895A (en) | 1996-03-29 |
EP0778021A4 (en) | 1998-06-03 |
KR970705985A (ko) | 1997-11-03 |
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