CN105530936B - 两性离子性软隐形眼镜用眼科用组合物 - Google Patents
两性离子性软隐形眼镜用眼科用组合物 Download PDFInfo
- Publication number
- CN105530936B CN105530936B CN201480050749.5A CN201480050749A CN105530936B CN 105530936 B CN105530936 B CN 105530936B CN 201480050749 A CN201480050749 A CN 201480050749A CN 105530936 B CN105530936 B CN 105530936B
- Authority
- CN
- China
- Prior art keywords
- scl
- amphoteric ion
- salt
- pranoprofen
- ophthalmic composition
- 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.)
- Expired - Fee Related
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 64
- 150000002500 ions Chemical class 0.000 claims abstract description 110
- 150000003839 salts Chemical class 0.000 claims abstract description 108
- TVQZAMVBTVNYLA-UHFFFAOYSA-N Pranoprofen Chemical compound C1=CC=C2CC3=CC(C(C(O)=O)C)=CC=C3OC2=N1 TVQZAMVBTVNYLA-UHFFFAOYSA-N 0.000 claims abstract description 79
- 229960003101 pranoprofen Drugs 0.000 claims abstract description 79
- 235000019410 glycyrrhizin Nutrition 0.000 claims abstract description 31
- VTAJIXDZFCRWBR-UHFFFAOYSA-N Licoricesaponin B2 Natural products C1C(C2C(C3(CCC4(C)CCC(C)(CC4C3=CC2)C(O)=O)C)(C)CC2)(C)C2C(C)(C)CC1OC1OC(C(O)=O)C(O)C(O)C1OC1OC(C(O)=O)C(O)C(O)C1O VTAJIXDZFCRWBR-UHFFFAOYSA-N 0.000 claims abstract description 30
- LPLVUJXQOOQHMX-UHFFFAOYSA-N glycyrrhetinic acid glycoside Natural products C1CC(C2C(C3(CCC4(C)CCC(C)(CC4C3=CC2=O)C(O)=O)C)(C)CC2)(C)C2C(C)(C)C1OC1OC(C(O)=O)C(O)C(O)C1OC1OC(C(O)=O)C(O)C(O)C1O LPLVUJXQOOQHMX-UHFFFAOYSA-N 0.000 claims abstract description 30
- 229960004949 glycyrrhizic acid Drugs 0.000 claims abstract description 30
- UYRUBYNTXSDKQT-UHFFFAOYSA-N glycyrrhizic acid Natural products CC1(C)C(CCC2(C)C1CCC3(C)C2C(=O)C=C4C5CC(C)(CCC5(C)CCC34C)C(=O)O)OC6OC(C(O)C(O)C6OC7OC(O)C(O)C(O)C7C(=O)O)C(=O)O UYRUBYNTXSDKQT-UHFFFAOYSA-N 0.000 claims abstract description 30
- 239000001685 glycyrrhizic acid Substances 0.000 claims abstract description 30
- LPLVUJXQOOQHMX-QWBHMCJMSA-N glycyrrhizinic acid Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@H](O[C@@H]1O[C@@H]1C([C@H]2[C@]([C@@H]3[C@@]([C@@]4(CC[C@@]5(C)CC[C@@](C)(C[C@H]5C4=CC3=O)C(O)=O)C)(C)CC2)(C)CC1)(C)C)C(O)=O)[C@@H]1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O LPLVUJXQOOQHMX-QWBHMCJMSA-N 0.000 claims abstract description 30
- 239000007788 liquid Substances 0.000 claims description 48
- 238000000034 method Methods 0.000 claims description 29
- 238000002360 preparation method Methods 0.000 claims description 29
- 239000003889 eye drop Substances 0.000 claims description 17
- 229940012356 eye drops Drugs 0.000 claims description 17
- 230000002401 inhibitory effect Effects 0.000 claims description 11
- 238000004519 manufacturing process Methods 0.000 claims description 4
- -1 Inorganic base salts Chemical class 0.000 description 22
- 239000003795 chemical substances by application Substances 0.000 description 14
- 238000012360 testing method Methods 0.000 description 13
- 238000010521 absorption reaction Methods 0.000 description 12
- 239000003814 drug Substances 0.000 description 11
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 9
- 206010018612 Gonorrhoea Diseases 0.000 description 9
- 229960003291 chlorphenamine Drugs 0.000 description 9
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 9
- 210000001508 eye Anatomy 0.000 description 9
- 239000004615 ingredient Substances 0.000 description 9
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Natural products CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 8
- 239000000872 buffer Substances 0.000 description 8
- 229940079593 drug Drugs 0.000 description 8
- DBAKFASWICGISY-BTJKTKAUSA-N Chlorpheniramine maleate Chemical compound OC(=O)\C=C/C(O)=O.C=1C=CC=NC=1C(CCN(C)C)C1=CC=C(Cl)C=C1 DBAKFASWICGISY-BTJKTKAUSA-N 0.000 description 7
- 239000002253 acid Substances 0.000 description 7
- 230000000694 effects Effects 0.000 description 7
- 238000001179 sorption measurement Methods 0.000 description 7
- 239000000017 hydrogel Substances 0.000 description 6
- 239000000463 material Substances 0.000 description 6
- 239000005426 pharmaceutical component Substances 0.000 description 6
- 229920001296 polysiloxane Polymers 0.000 description 6
- 125000000129 anionic group Chemical group 0.000 description 5
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 4
- 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 4
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 4
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 4
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical class CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 4
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical class C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 description 4
- 238000002835 absorbance Methods 0.000 description 4
- 239000000654 additive Substances 0.000 description 4
- 238000013461 design Methods 0.000 description 4
- 229940101029 dipotassium glycyrrhizinate Drugs 0.000 description 4
- 239000011521 glass Substances 0.000 description 4
- 239000000178 monomer Substances 0.000 description 4
- FDDDEECHVMSUSB-UHFFFAOYSA-N sulfanilamide Chemical compound NC1=CC=C(S(N)(=O)=O)C=C1 FDDDEECHVMSUSB-UHFFFAOYSA-N 0.000 description 4
- 229940124530 sulfonamide Drugs 0.000 description 4
- XOAAWQZATWQOTB-UHFFFAOYSA-N taurine Chemical compound NCCS(O)(=O)=O XOAAWQZATWQOTB-UHFFFAOYSA-N 0.000 description 4
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 description 3
- HEFNNWSXXWATRW-UHFFFAOYSA-N Ibuprofen Chemical compound CC(C)CC1=CC=C(C(C)C(O)=O)C=C1 HEFNNWSXXWATRW-UHFFFAOYSA-N 0.000 description 3
- 206010061218 Inflammation Diseases 0.000 description 3
- WCUXLLCKKVVCTQ-UHFFFAOYSA-M Potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 description 3
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 description 3
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 description 3
- 230000000996 additive effect Effects 0.000 description 3
- 239000003513 alkali Substances 0.000 description 3
- 235000001014 amino acid Nutrition 0.000 description 3
- 150000001413 amino acids Chemical class 0.000 description 3
- 230000001387 anti-histamine Effects 0.000 description 3
- 239000000739 antihistaminic agent Substances 0.000 description 3
- 239000002738 chelating agent Substances 0.000 description 3
- SOYKEARSMXGVTM-UHFFFAOYSA-N chlorphenamine Chemical compound C=1C=CC=NC=1C(CCN(C)C)C1=CC=C(Cl)C=C1 SOYKEARSMXGVTM-UHFFFAOYSA-N 0.000 description 3
- 230000000052 comparative effect Effects 0.000 description 3
- 150000001875 compounds Chemical class 0.000 description 3
- 239000006184 cosolvent Substances 0.000 description 3
- 239000002552 dosage form Substances 0.000 description 3
- 230000000857 drug effect Effects 0.000 description 3
- 229960001680 ibuprofen Drugs 0.000 description 3
- 230000004054 inflammatory process Effects 0.000 description 3
- 239000007951 isotonicity adjuster Substances 0.000 description 3
- 239000003002 pH adjusting agent Substances 0.000 description 3
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 3
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 3
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 3
- 239000001103 potassium chloride Substances 0.000 description 3
- 235000011164 potassium chloride Nutrition 0.000 description 3
- 239000003755 preservative agent Substances 0.000 description 3
- 238000011160 research Methods 0.000 description 3
- 239000004094 surface-active agent Substances 0.000 description 3
- KWGRBVOPPLSCSI-WPRPVWTQSA-N (-)-ephedrine Chemical compound CN[C@@H](C)[C@H](O)C1=CC=CC=C1 KWGRBVOPPLSCSI-WPRPVWTQSA-N 0.000 description 2
- CNIIGCLFLJGOGP-UHFFFAOYSA-N 2-(1-naphthalenylmethyl)-4,5-dihydro-1H-imidazole Chemical compound C=1C=CC2=CC=CC=C2C=1CC1=NCCN1 CNIIGCLFLJGOGP-UHFFFAOYSA-N 0.000 description 2
- DBCAQXHNJOFNGC-UHFFFAOYSA-N 4-bromo-1,1,1-trifluorobutane Chemical compound FC(F)(F)CCCBr DBCAQXHNJOFNGC-UHFFFAOYSA-N 0.000 description 2
- WVDDGKGOMKODPV-UHFFFAOYSA-N Benzyl alcohol Chemical compound OCC1=CC=CC=C1 WVDDGKGOMKODPV-UHFFFAOYSA-N 0.000 description 2
- 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 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- 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
- 239000002202 Polyethylene glycol Substances 0.000 description 2
- VYGQUTWHTHXGQB-FFHKNEKCSA-N Retinol Palmitate Chemical compound CCCCCCCCCCCCCCCC(=O)OC\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C VYGQUTWHTHXGQB-FFHKNEKCSA-N 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- 229920002385 Sodium hyaluronate Polymers 0.000 description 2
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 2
- UCTWMZQNUQWSLP-UHFFFAOYSA-N adrenaline Chemical compound CNCC(O)C1=CC=C(O)C(O)=C1 UCTWMZQNUQWSLP-UHFFFAOYSA-N 0.000 description 2
- 150000001447 alkali salts Chemical class 0.000 description 2
- POJWUDADGALRAB-UHFFFAOYSA-N allantoin Chemical compound NC(=O)NC1NC(=O)NC1=O POJWUDADGALRAB-UHFFFAOYSA-N 0.000 description 2
- 229910000147 aluminium phosphate Inorganic materials 0.000 description 2
- 150000001450 anions Chemical class 0.000 description 2
- 230000003110 anti-inflammatory effect Effects 0.000 description 2
- 239000007864 aqueous solution Substances 0.000 description 2
- 235000010323 ascorbic acid Nutrition 0.000 description 2
- 229960005070 ascorbic acid Drugs 0.000 description 2
- 239000011668 ascorbic acid Substances 0.000 description 2
- 239000002585 base Substances 0.000 description 2
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-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
- 159000000007 calcium salts Chemical class 0.000 description 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 2
- 125000002091 cationic group Chemical group 0.000 description 2
- 238000012512 characterization method Methods 0.000 description 2
- 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 2
- 238000005352 clarification Methods 0.000 description 2
- 239000000470 constituent Substances 0.000 description 2
- RMRCNWBMXRMIRW-BYFNXCQMSA-M cyanocobalamin Chemical compound N#C[Co+]N([C@]1([H])[C@H](CC(N)=O)[C@]\2(CCC(=O)NC[C@H](C)OP(O)(=O)OC3[C@H]([C@H](O[C@@H]3CO)N3C4=CC(C)=C(C)C=C4N=C3)O)C)C/2=C(C)\C([C@H](C/2(C)C)CCC(N)=O)=N\C\2=C\C([C@H]([C@@]/2(CC(N)=O)C)CCC(N)=O)=N\C\2=C(C)/C2=N[C@]1(C)[C@@](C)(CC(N)=O)[C@@H]2CCC(N)=O RMRCNWBMXRMIRW-BYFNXCQMSA-M 0.000 description 2
- 229940009662 edetate Drugs 0.000 description 2
- MTZQAGJQAFMTAQ-UHFFFAOYSA-N ethyl benzoate Chemical compound CCOC(=O)C1=CC=CC=C1 MTZQAGJQAFMTAQ-UHFFFAOYSA-N 0.000 description 2
- STVZJERGLQHEKB-UHFFFAOYSA-N ethylene glycol dimethacrylate Substances CC(=C)C(=O)OCCOC(=O)C(C)=C STVZJERGLQHEKB-UHFFFAOYSA-N 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 2
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 2
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 2
- 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 2
- 230000005764 inhibitory process Effects 0.000 description 2
- 150000002632 lipids Chemical class 0.000 description 2
- 238000004811 liquid chromatography Methods 0.000 description 2
- 159000000003 magnesium salts Chemical class 0.000 description 2
- 210000004877 mucosa Anatomy 0.000 description 2
- 229960001699 ofloxacin Drugs 0.000 description 2
- 229920001983 poloxamer Polymers 0.000 description 2
- 229920001223 polyethylene glycol Polymers 0.000 description 2
- 230000002335 preservative effect Effects 0.000 description 2
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 2
- 235000018102 proteins Nutrition 0.000 description 2
- 108090000623 proteins and genes Proteins 0.000 description 2
- 102000004169 proteins and genes Human genes 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
- 229940010747 sodium hyaluronate Drugs 0.000 description 2
- 159000000000 sodium salts Chemical class 0.000 description 2
- YWIVKILSMZOHHF-QJZPQSOGSA-N sodium;(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- Chemical compound [Na+].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 YWIVKILSMZOHHF-QJZPQSOGSA-N 0.000 description 2
- 239000003381 stabilizer Substances 0.000 description 2
- 150000005846 sugar alcohols Polymers 0.000 description 2
- 239000011975 tartaric acid Substances 0.000 description 2
- 235000002906 tartaric acid Nutrition 0.000 description 2
- 229960003080 taurine Drugs 0.000 description 2
- BYJAVTDNIXVSPW-UHFFFAOYSA-N tetryzoline Chemical compound N1CCN=C1C1C2=CC=CC=C2CCC1 BYJAVTDNIXVSPW-UHFFFAOYSA-N 0.000 description 2
- 229920001664 tyloxapol Polymers 0.000 description 2
- MDYZKJNTKZIUSK-UHFFFAOYSA-N tyloxapol Chemical compound O=C.C1CO1.CC(C)(C)CC(C)(C)C1=CC=C(O)C=C1 MDYZKJNTKZIUSK-UHFFFAOYSA-N 0.000 description 2
- 229960004224 tyloxapol Drugs 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- JIAARYAFYJHUJI-UHFFFAOYSA-L zinc dichloride Chemical compound [Cl-].[Cl-].[Zn+2] JIAARYAFYJHUJI-UHFFFAOYSA-L 0.000 description 2
- QSLPNSWXUQHVLP-UHFFFAOYSA-N $l^{1}-sulfanylmethane Chemical compound [S]C QSLPNSWXUQHVLP-UHFFFAOYSA-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
- NOOLISFMXDJSKH-KXUCPTDWSA-N (-)-Menthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@H]1O NOOLISFMXDJSKH-KXUCPTDWSA-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
- 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
- XUBOMFCQGDBHNK-JTQLQIEISA-N (S)-gatifloxacin Chemical compound FC1=CC(C(C(C(O)=O)=CN2C3CC3)=O)=C2C(OC)=C1N1CCN[C@@H](C)C1 XUBOMFCQGDBHNK-JTQLQIEISA-N 0.000 description 1
- VAZJLPXFVQHDFB-UHFFFAOYSA-N 1-(diaminomethylidene)-2-hexylguanidine Polymers CCCCCCN=C(N)N=C(N)N VAZJLPXFVQHDFB-UHFFFAOYSA-N 0.000 description 1
- VCNKUCWWHVTTBY-UHFFFAOYSA-N 18alpha-Oleanane Natural products C1CCC(C)(C)C2CCC3(C)C4(C)CCC5(C)CCC(C)(C)CC5C4CCC3C21C VCNKUCWWHVTTBY-UHFFFAOYSA-N 0.000 description 1
- SPSPIUSUWPLVKD-UHFFFAOYSA-N 2,3-dibutyl-6-methylphenol Chemical compound CCCCC1=CC=C(C)C(O)=C1CCCC SPSPIUSUWPLVKD-UHFFFAOYSA-N 0.000 description 1
- HZAXFHJVJLSVMW-UHFFFAOYSA-N 2-Aminoethan-1-ol Chemical compound NCCO HZAXFHJVJLSVMW-UHFFFAOYSA-N 0.000 description 1
- HNLXNOZHXNSSPN-UHFFFAOYSA-N 2-[2-[2-[2-[2-[2-[2-[4-(2,4,4-trimethylpentan-2-yl)phenoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethanol Chemical compound CC(C)(C)CC(C)(C)C1=CC=C(OCCOCCOCCOCCOCCOCCOCCO)C=C1 HNLXNOZHXNSSPN-UHFFFAOYSA-N 0.000 description 1
- WRMNZCZEMHIOCP-UHFFFAOYSA-N 2-phenylethanol Chemical compound OCCC1=CC=CC=C1 WRMNZCZEMHIOCP-UHFFFAOYSA-N 0.000 description 1
- MIJYXULNPSFWEK-GTOFXWBISA-N 3beta-hydroxyolean-12-en-28-oic acid Chemical compound C1C[C@H](O)C(C)(C)[C@@H]2CC[C@@]3(C)[C@]4(C)CC[C@@]5(C(O)=O)CCC(C)(C)C[C@H]5C4=CC[C@@H]3[C@]21C MIJYXULNPSFWEK-GTOFXWBISA-N 0.000 description 1
- SVYBEBLNQGDRHF-UHFFFAOYSA-N 4-amino-N-(5-ethyl-1,3,4-thiadiazol-2-yl)benzenesulfonamide Chemical compound S1C(CC)=NN=C1NS(=O)(=O)C1=CC=C(N)C=C1 SVYBEBLNQGDRHF-UHFFFAOYSA-N 0.000 description 1
- OSDLLIBGSJNGJE-UHFFFAOYSA-N 4-chloro-3,5-dimethylphenol Chemical compound CC1=CC(O)=CC(C)=C1Cl OSDLLIBGSJNGJE-UHFFFAOYSA-N 0.000 description 1
- SQDAZGGFXASXDW-UHFFFAOYSA-N 5-bromo-2-(trifluoromethoxy)pyridine Chemical compound FC(F)(F)OC1=CC=C(Br)C=N1 SQDAZGGFXASXDW-UHFFFAOYSA-N 0.000 description 1
- SLXKOJJOQWFEFD-UHFFFAOYSA-N 6-aminohexanoic acid Chemical compound NCCCCCC(O)=O SLXKOJJOQWFEFD-UHFFFAOYSA-N 0.000 description 1
- GSDSWSVVBLHKDQ-UHFFFAOYSA-N 9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid Chemical compound FC1=CC(C(C(C(O)=O)=C2)=O)=C3N2C(C)COC3=C1N1CCN(C)CC1 GSDSWSVVBLHKDQ-UHFFFAOYSA-N 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
- 239000005711 Benzoic acid Substances 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
- BTBUEUYNUDRHOZ-UHFFFAOYSA-N Borate Chemical compound [O-]B([O-])[O-] BTBUEUYNUDRHOZ-UHFFFAOYSA-N 0.000 description 1
- OQRYWJHKYLPGOZ-UHFFFAOYSA-M C(CCCCCCCCCCC)C(=C(OC)OC)[N+](C)(C)C.[OH-] Chemical compound C(CCCCCCCCCCC)C(=C(OC)OC)[N+](C)(C)C.[OH-] OQRYWJHKYLPGOZ-UHFFFAOYSA-M 0.000 description 1
- 229920001287 Chondroitin sulfate Polymers 0.000 description 1
- 241000723346 Cinnamomum camphora Species 0.000 description 1
- 206010010741 Conjunctivitis Diseases 0.000 description 1
- 229920000858 Cyclodextrin Polymers 0.000 description 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 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
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-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
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 1
- 241001465251 Ephedra sinica Species 0.000 description 1
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 description 1
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 1
- CEAZRRDELHUEMR-URQXQFDESA-N Gentamicin Chemical compound O1[C@H](C(C)NC)CC[C@@H](N)[C@H]1O[C@H]1[C@H](O)[C@@H](O[C@@H]2[C@@H]([C@@H](NC)[C@@](C)(O)CO2)O)[C@H](N)C[C@@H]1N CEAZRRDELHUEMR-URQXQFDESA-N 0.000 description 1
- 229930182566 Gentamicin Natural products 0.000 description 1
- 229920001503 Glucan Polymers 0.000 description 1
- 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 description 1
- 229920002683 Glycosaminoglycan Polymers 0.000 description 1
- 239000004354 Hydroxyethyl cellulose Substances 0.000 description 1
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 description 1
- WOBHKFSMXKNTIM-UHFFFAOYSA-N Hydroxyethyl methacrylate Chemical compound CC(=C)C(=O)OCCO WOBHKFSMXKNTIM-UHFFFAOYSA-N 0.000 description 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 1
- 206010020565 Hyperaemia Diseases 0.000 description 1
- ZJVFLBOZORBYFE-UHFFFAOYSA-N Ibudilast Chemical compound C1=CC=CC2=C(C(=O)C(C)C)C(C(C)C)=NN21 ZJVFLBOZORBYFE-UHFFFAOYSA-N 0.000 description 1
- ZCVMWBYGMWKGHF-UHFFFAOYSA-N Ketotifene Chemical compound C1CN(C)CCC1=C1C2=CC=CC=C2CC(=O)C2=C1C=CS2 ZCVMWBYGMWKGHF-UHFFFAOYSA-N 0.000 description 1
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 description 1
- 229930195725 Mannitol Natural products 0.000 description 1
- VVQNEPGJFQJSBK-UHFFFAOYSA-N Methyl methacrylate Chemical compound COC(=O)C(C)=C VVQNEPGJFQJSBK-UHFFFAOYSA-N 0.000 description 1
- SKVLYVHULOWXTD-UHFFFAOYSA-N N-succinylsulfathiazole Chemical compound C1=CC(NC(=O)CCC(=O)O)=CC=C1S(=O)(=O)NC1=NC=CS1 SKVLYVHULOWXTD-UHFFFAOYSA-N 0.000 description 1
- 229910019142 PO4 Inorganic materials 0.000 description 1
- OTIWYSKRSMXGNK-VHJGTCNUSA-K Polidronium chloride Chemical compound [Cl-].[Cl-].[Cl-].OCC[N+](CCO)(CCO)C/C=C/C[N+](C)(C)C\C=C\C[N+](CCO)(CCO)CCO OTIWYSKRSMXGNK-VHJGTCNUSA-K 0.000 description 1
- 229920002413 Polyhexanide Polymers 0.000 description 1
- 229920001214 Polysorbate 60 Polymers 0.000 description 1
- 239000004372 Polyvinyl alcohol Substances 0.000 description 1
- 208000003251 Pruritus Diseases 0.000 description 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 description 1
- 240000000528 Ricinus communis Species 0.000 description 1
- 235000004443 Ricinus communis Nutrition 0.000 description 1
- 101150075681 SCL1 gene Proteins 0.000 description 1
- NWGKJDSIEKMTRX-AAZCQSIUSA-N Sorbitan monooleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O NWGKJDSIEKMTRX-AAZCQSIUSA-N 0.000 description 1
- QKLSCPPJEVXONT-UHFFFAOYSA-N Sulfametomidine Chemical compound CC1=NC(OC)=CC(NS(=O)(=O)C=2C=CC(N)=CC=2)=N1 QKLSCPPJEVXONT-UHFFFAOYSA-N 0.000 description 1
- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical class CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 description 1
- 206010046851 Uveitis Diseases 0.000 description 1
- HCHKCACWOHOZIP-UHFFFAOYSA-N Zinc Chemical compound [Zn] HCHKCACWOHOZIP-UHFFFAOYSA-N 0.000 description 1
- HYBIBLNGGIWWAY-UHFFFAOYSA-N [K].[K].OC(=O)C(O)=O Chemical compound [K].[K].OC(=O)C(O)=O HYBIBLNGGIWWAY-UHFFFAOYSA-N 0.000 description 1
- 238000009825 accumulation Methods 0.000 description 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 1
- VWQZJJZGISNFOE-UHFFFAOYSA-N acitazanolast Chemical compound OC(=O)C(=O)NC1=CC=CC(C2=NNN=N2)=C1 VWQZJJZGISNFOE-UHFFFAOYSA-N 0.000 description 1
- 229950001122 acitazanolast Drugs 0.000 description 1
- 230000002411 adverse Effects 0.000 description 1
- 238000004220 aggregation Methods 0.000 description 1
- 230000002776 aggregation Effects 0.000 description 1
- 229910052783 alkali metal Inorganic materials 0.000 description 1
- 150000001336 alkenes Chemical class 0.000 description 1
- 229960000458 allantoin Drugs 0.000 description 1
- 159000000013 aluminium salts Chemical class 0.000 description 1
- 229910000329 aluminium sulfate Inorganic materials 0.000 description 1
- 150000001412 amines Chemical class 0.000 description 1
- 229960002684 aminocaproic acid Drugs 0.000 description 1
- SGRYPYWGNKJSDL-UHFFFAOYSA-N amlexanox Chemical compound NC1=C(C(O)=O)C=C2C(=O)C3=CC(C(C)C)=CC=C3OC2=N1 SGRYPYWGNKJSDL-UHFFFAOYSA-N 0.000 description 1
- 229960003731 amlexanox Drugs 0.000 description 1
- 150000003863 ammonium salts Chemical class 0.000 description 1
- 239000003242 anti bacterial agent Substances 0.000 description 1
- 230000001741 anti-phlogistic effect Effects 0.000 description 1
- 229940055075 anticholinesterase parasympathomimetics Drugs 0.000 description 1
- 229940125715 antihistaminic agent Drugs 0.000 description 1
- 235000003704 aspartic acid Nutrition 0.000 description 1
- 208000003464 asthenopia Diseases 0.000 description 1
- 150000003851 azoles Chemical class 0.000 description 1
- UREZNYTWGJKWBI-UHFFFAOYSA-M benzethonium chloride Chemical compound [Cl-].C1=CC(C(C)(C)CC(C)(C)C)=CC=C1OCCOCC[N+](C)(C)CC1=CC=CC=C1 UREZNYTWGJKWBI-UHFFFAOYSA-M 0.000 description 1
- 229960001950 benzethonium chloride Drugs 0.000 description 1
- 235000010233 benzoic acid Nutrition 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
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
- OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 229920001400 block copolymer Polymers 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
- ZBPLOVFIXSTCRZ-UHFFFAOYSA-N bromfenac Chemical compound NC1=C(CC(O)=O)C=CC=C1C(=O)C1=CC=C(Br)C=C1 ZBPLOVFIXSTCRZ-UHFFFAOYSA-N 0.000 description 1
- 229960003655 bromfenac Drugs 0.000 description 1
- 210000005252 bulbus oculi Anatomy 0.000 description 1
- 235000010354 butylated hydroxytoluene Nutrition 0.000 description 1
- FAPWYRCQGJNNSJ-UBKPKTQASA-L calcium D-pantothenic acid Chemical compound [Ca+2].OCC(C)(C)[C@@H](O)C(=O)NCCC([O-])=O.OCC(C)(C)[C@@H](O)C(=O)NCCC([O-])=O FAPWYRCQGJNNSJ-UBKPKTQASA-L 0.000 description 1
- 229960002079 calcium pantothenate Drugs 0.000 description 1
- 229930008380 camphor Natural products 0.000 description 1
- 229960000846 camphor Drugs 0.000 description 1
- 150000001720 carbohydrates Chemical class 0.000 description 1
- 235000014633 carbohydrates Nutrition 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 150000001732 carboxylic acid derivatives Chemical class 0.000 description 1
- 239000004359 castor oil Substances 0.000 description 1
- 229960001777 castor oil Drugs 0.000 description 1
- 235000019438 castor oil Nutrition 0.000 description 1
- 239000003093 cationic surfactant Substances 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- 235000010980 cellulose Nutrition 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 229960003333 chlorhexidine gluconate Drugs 0.000 description 1
- YZIYKJHYYHPJIB-UUPCJSQJSA-N chlorhexidine gluconate Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O.OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O.C1=CC(Cl)=CC=C1NC(=N)NC(=N)NCCCCCCNC(=N)NC(=N)NC1=CC=C(Cl)C=C1 YZIYKJHYYHPJIB-UUPCJSQJSA-N 0.000 description 1
- OSASVXMJTNOKOY-UHFFFAOYSA-N chlorobutanol Chemical compound CC(C)(O)C(Cl)(Cl)Cl OSASVXMJTNOKOY-UHFFFAOYSA-N 0.000 description 1
- 239000000544 cholinesterase inhibitor Substances 0.000 description 1
- 229940059329 chondroitin sulfate Drugs 0.000 description 1
- QZHPTGXQGDFGEN-UHFFFAOYSA-N chromene Chemical compound C1=CC=C2C=C[CH]OC2=C1 QZHPTGXQGDFGEN-UHFFFAOYSA-N 0.000 description 1
- 238000004140 cleaning Methods 0.000 description 1
- 235000009508 confectionery Nutrition 0.000 description 1
- 210000004087 cornea Anatomy 0.000 description 1
- 238000012937 correction Methods 0.000 description 1
- 239000006071 cream Substances 0.000 description 1
- 235000000639 cyanocobalamin Nutrition 0.000 description 1
- 229960002104 cyanocobalamin Drugs 0.000 description 1
- 239000011666 cyanocobalamin Substances 0.000 description 1
- GVJHHUAWPYXKBD-UHFFFAOYSA-N d-alpha-tocopherol Natural products OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 description 1
- KWGRBVOPPLSCSI-UHFFFAOYSA-N d-ephedrine Natural products CNC(C)C(O)C1=CC=CC=C1 KWGRBVOPPLSCSI-UHFFFAOYSA-N 0.000 description 1
- 150000005332 diethylamines Chemical class 0.000 description 1
- VLARUOGDXDTHEH-UHFFFAOYSA-L disodium cromoglycate Chemical compound [Na+].[Na+].O1C(C([O-])=O)=CC(=O)C2=C1C=CC=C2OCC(O)COC1=CC=CC2=C1C(=O)C=C(C([O-])=O)O2 VLARUOGDXDTHEH-UHFFFAOYSA-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
- 230000004064 dysfunction Effects 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 229960002179 ephedrine Drugs 0.000 description 1
- 210000000981 epithelium Anatomy 0.000 description 1
- BEFDCLMNVWHSGT-UHFFFAOYSA-N ethenylcyclopentane Chemical compound C=CC1CCCC1 BEFDCLMNVWHSGT-UHFFFAOYSA-N 0.000 description 1
- RTZKZFJDLAIYFH-UHFFFAOYSA-N ether Substances CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 1
- 229940044949 eucalyptus oil Drugs 0.000 description 1
- 239000010642 eucalyptus oil Substances 0.000 description 1
- 235000019162 flavin adenine dinucleotide Nutrition 0.000 description 1
- 229910052731 fluorine Inorganic materials 0.000 description 1
- 239000011737 fluorine Substances 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 239000012634 fragment Substances 0.000 description 1
- 239000003205 fragrance Substances 0.000 description 1
- 229940050411 fumarate Drugs 0.000 description 1
- 229960003923 gatifloxacin Drugs 0.000 description 1
- 229960002518 gentamicin Drugs 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 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 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 description 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
- SIOMFBXUIJKTMF-UHFFFAOYSA-N hypoglauterpenic acid Natural products C1CC(O)C(C)(C)C2=CCC3(C)C4(C)CCC5(C(O)=O)CCC(C)(C)CC5C4=CCC3C21C SIOMFBXUIJKTMF-UHFFFAOYSA-N 0.000 description 1
- 229960002491 ibudilast Drugs 0.000 description 1
- BWHLPLXXIDYSNW-UHFFFAOYSA-N ketorolac tromethamine Chemical compound OCC(N)(CO)CO.OC(=O)C1CCN2C1=CC=C2C(=O)C1=CC=CC=C1 BWHLPLXXIDYSNW-UHFFFAOYSA-N 0.000 description 1
- 229960004384 ketorolac tromethamine Drugs 0.000 description 1
- 229960004958 ketotifen Drugs 0.000 description 1
- ZEKZLJVOYLTDKK-UHFFFAOYSA-N lomefloxacin Chemical compound FC1=C2N(CC)C=C(C(O)=O)C(=O)C2=CC(F)=C1N1CCNC(C)C1 ZEKZLJVOYLTDKK-UHFFFAOYSA-N 0.000 description 1
- 229960002422 lomefloxacin Drugs 0.000 description 1
- 229960003511 macrogol Drugs 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 229910052751 metal Inorganic materials 0.000 description 1
- 239000002184 metal Substances 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 239000004292 methyl p-hydroxybenzoate Substances 0.000 description 1
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 235000010981 methylcellulose Nutrition 0.000 description 1
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 description 1
- 230000000116 mitigating effect Effects 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 229960005016 naphazoline Drugs 0.000 description 1
- 229940105623 neo-synephrine Drugs 0.000 description 1
- 229960002362 neostigmine Drugs 0.000 description 1
- LULNWZDBKTWDGK-UHFFFAOYSA-M neostigmine bromide Chemical compound [Br-].CN(C)C(=O)OC1=CC=CC([N+](C)(C)C)=C1 LULNWZDBKTWDGK-UHFFFAOYSA-M 0.000 description 1
- QEFAQIPZVLVERP-UHFFFAOYSA-N nepafenac Chemical compound NC(=O)CC1=CC=CC(C(=O)C=2C=CC=CC=2)=C1N QEFAQIPZVLVERP-UHFFFAOYSA-N 0.000 description 1
- 229960001002 nepafenac Drugs 0.000 description 1
- 239000002736 nonionic surfactant Substances 0.000 description 1
- 230000000474 nursing effect Effects 0.000 description 1
- 229950004053 octoxinol Drugs 0.000 description 1
- 229940066429 octoxynol Drugs 0.000 description 1
- 229920002113 octoxynol Polymers 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- BPAWXSVOAOLSRP-UHFFFAOYSA-N oleanane Natural products CCCCCCCCCCCCCCCC(=O)OC1CCC2(C)C(CCC3(C)C2CC=C4C5CC(C)(C)CCC5(C)C(O)CC34C)C1(C)C BPAWXSVOAOLSRP-UHFFFAOYSA-N 0.000 description 1
- 230000010355 oscillation Effects 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 239000001301 oxygen 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
- HIANJWSAHKJQTH-UHFFFAOYSA-N pemirolast Chemical compound CC1=CC=CN(C2=O)C1=NC=C2C=1N=NNN=1 HIANJWSAHKJQTH-UHFFFAOYSA-N 0.000 description 1
- 229960004439 pemirolast Drugs 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- WVDDGKGOMKODPV-ZQBYOMGUSA-N phenyl(114C)methanol Chemical compound O[14CH2]C1=CC=CC=C1 WVDDGKGOMKODPV-ZQBYOMGUSA-N 0.000 description 1
- SONNWYBIRXJNDC-VIFPVBQESA-N phenylephrine Chemical compound CNC[C@H](O)C1=CC=CC(O)=C1 SONNWYBIRXJNDC-VIFPVBQESA-N 0.000 description 1
- 235000021317 phosphate Nutrition 0.000 description 1
- 229920001523 phosphate polymer Polymers 0.000 description 1
- PBMSWVPMRUJMPE-UHFFFAOYSA-N phthalylsulfathiazole Chemical compound OC(=O)C1=CC=CC=C1C(=O)NC1=CC=C(S(=O)(=O)\N=C\2SC=CN/2)C=C1 PBMSWVPMRUJMPE-UHFFFAOYSA-N 0.000 description 1
- 150000004885 piperazines Chemical class 0.000 description 1
- 229960000420 polidronium chloride Drugs 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 230000002980 postoperative effect Effects 0.000 description 1
- 238000003825 pressing Methods 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 description 1
- 239000004405 propyl p-hydroxybenzoate Substances 0.000 description 1
- 229960003415 propylparaben Drugs 0.000 description 1
- 150000003180 prostaglandins Chemical class 0.000 description 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 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
- 125000001453 quaternary ammonium group Chemical group 0.000 description 1
- 150000003242 quaternary ammonium salts Chemical group 0.000 description 1
- 229960000342 retinol acetate Drugs 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
- 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
- 210000003786 sclera Anatomy 0.000 description 1
- 125000000467 secondary amino group Chemical group [H]N([*:1])[*:2] 0.000 description 1
- 229940083542 sodium Drugs 0.000 description 1
- 235000015424 sodium Nutrition 0.000 description 1
- NLAIHECABDOZBR-UHFFFAOYSA-M sodium 2,2-bis(2-methylprop-2-enoyloxymethyl)butyl 2-methylprop-2-enoate 2-hydroxyethyl 2-methylprop-2-enoate 2-methylprop-2-enoate Chemical compound [Na+].CC(=C)C([O-])=O.CC(=C)C(=O)OCCO.CCC(COC(=O)C(C)=C)(COC(=O)C(C)=C)COC(=O)C(C)=C NLAIHECABDOZBR-UHFFFAOYSA-M 0.000 description 1
- 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
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 229940068459 sodium pantothenate Drugs 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
- 239000000243 solution 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
- 229960005379 succinylsulfathiazole Drugs 0.000 description 1
- SEEPANYCNGTZFQ-UHFFFAOYSA-N sulfadiazine Chemical compound C1=CC(N)=CC=C1S(=O)(=O)NC1=NC=CC=N1 SEEPANYCNGTZFQ-UHFFFAOYSA-N 0.000 description 1
- 229960004306 sulfadiazine Drugs 0.000 description 1
- ZZORFUFYDOWNEF-UHFFFAOYSA-N sulfadimethoxine Chemical compound COC1=NC(OC)=CC(NS(=O)(=O)C=2C=CC(N)=CC=2)=N1 ZZORFUFYDOWNEF-UHFFFAOYSA-N 0.000 description 1
- 229960000973 sulfadimethoxine Drugs 0.000 description 1
- 229960003288 sulfaethidole Drugs 0.000 description 1
- VLYWMPOKSSWJAL-UHFFFAOYSA-N sulfamethoxypyridazine Chemical compound N1=NC(OC)=CC=C1NS(=O)(=O)C1=CC=C(N)C=C1 VLYWMPOKSSWJAL-UHFFFAOYSA-N 0.000 description 1
- 229960004936 sulfamethoxypyridazine Drugs 0.000 description 1
- 229960001873 sulfametomidine Drugs 0.000 description 1
- LSNNMFCWUKXFEE-UHFFFAOYSA-L sulfite Chemical compound [O-]S([O-])=O LSNNMFCWUKXFEE-UHFFFAOYSA-L 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 125000001302 tertiary amino group Chemical group 0.000 description 1
- 229960000337 tetryzoline Drugs 0.000 description 1
- RTKIYNMVFMVABJ-UHFFFAOYSA-L thimerosal Chemical compound [Na+].CC[Hg]SC1=CC=CC=C1C([O-])=O RTKIYNMVFMVABJ-UHFFFAOYSA-L 0.000 description 1
- 229940033663 thimerosal Drugs 0.000 description 1
- 235000010384 tocopherol Nutrition 0.000 description 1
- 229960001295 tocopherol Drugs 0.000 description 1
- 229930003799 tocopherol Natural products 0.000 description 1
- 239000011732 tocopherol Substances 0.000 description 1
- 229940042585 tocopherol acetate Drugs 0.000 description 1
- 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
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- 229960000281 trometamol Drugs 0.000 description 1
- 239000005526 vasoconstrictor agent Substances 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 229920003169 water-soluble polymer Polymers 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
- 229940082509 xanthan gum Drugs 0.000 description 1
- 229910052725 zinc Inorganic materials 0.000 description 1
- 239000011701 zinc Substances 0.000 description 1
- 239000011592 zinc chloride Substances 0.000 description 1
- 235000005074 zinc chloride Nutrition 0.000 description 1
- 229960001939 zinc chloride Drugs 0.000 description 1
- NWONKYPBYAMBJT-UHFFFAOYSA-L zinc sulfate Chemical compound [Zn+2].[O-]S([O-])(=O)=O NWONKYPBYAMBJT-UHFFFAOYSA-L 0.000 description 1
- 229960001763 zinc sulfate Drugs 0.000 description 1
- 229910000368 zinc sulfate Inorganic materials 0.000 description 1
- GVJHHUAWPYXKBD-IEOSBIPESA-N α-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/08—Solutions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/436—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7012—Compounds having a free or esterified carboxyl group attached, directly or through a carbon chain, to a carbon atom of the saccharide radical, e.g. glucuronic acid, neuraminic acid
-
- 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
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
- A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
- A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/28—Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/04—Artificial tears; Irrigation solutions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61L—METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
- A61L12/00—Methods or apparatus for disinfecting or sterilising contact lenses; Accessories therefor
- A61L12/08—Methods or apparatus for disinfecting or sterilising contact lenses; Accessories therefor using chemical substances
- A61L12/12—Non-macromolecular oxygen-containing compounds, e.g. hydrogen peroxide or ozone
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Ophthalmology & Optometry (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
本发明的目的是提供，在包含普拉洛芬和/或其盐的两性离子性SCL用眼科用组合物中，抑制普拉洛芬和/或其盐吸附至两性离子性SCL的技术。在包含普拉洛芬和/或其盐的两性离子性SCL用眼科用组合物中，通过使其含有甘草酸和/或其盐，能够有效地抑制普拉洛芬和/或其盐吸附至两性离子性SCL。
Description
技术领域
本发明涉及能够抑制普拉洛芬和/或其盐吸附至两性离子性软隐形眼镜的两性离子性软隐形眼镜用眼科用组合物。此外，本发明涉及抑制普拉洛芬和/或其盐吸附至两性离子性软隐形眼镜的方法。
背景技术
近年来，开发了一次性、能够长期连续佩戴的软隐形眼镜(以下，有时简写为SCL)，SCL佩戴者在不断增加。以往，SCL大多使用非离子性、阴离子性的材料，但是近年来，作为能够抑制泪液中的蛋白质、脂质、细胞碎片等在眼镜表面聚集的SCL，两性离子性SCL也被实用化。因此，为了提高两性离子性SCL佩戴者的便利性，要求能够在佩戴了两性离子性SCL的状态下使用的滴眼剂(两性离子性SCL用滴眼剂)。
对于SCL用滴眼剂，除了发挥所期望的药效以外，需要以不对SCL产生不良影响的方式进行制剂设计。特别是如果SCL用滴眼剂中的药物吸附于SCL，则导致眼镜的变形、使用感的降低等，进而有时变得不能对眼粘膜发挥所期望的药理效果，因此在SCL用滴眼剂的制剂设计上，抑制药物对SCL的吸附成为特别重要的课题。此外，由于药物的吸附特性还随着SCL的表面特性不同而变化，因此对于SCL用滴眼剂，需要与所应用的SCL的材料对应的制剂设计。
另一方面，普拉洛芬和/或其盐具有抑制成为炎症、疼痛的原因的前列腺素的生物合成的作用，在眼科领域中，以眼的充血、发痒等症状的缓和、睑缘炎、结膜炎、包括巩膜外层炎的巩膜炎、术后的炎症、前眼部葡萄膜炎等的预防或治疗为目的而被广泛使用。此外，关于包含普拉洛芬和/或其盐的SCL用滴眼剂的制剂技术，也有若干报道。例如，专利文献1中公开了包含普拉洛芬或其盐以及聚六亚甲基双胍或其盐的硅酮水凝胶隐形眼镜用眼科组合物能够抑制在非离子性硅酮水凝胶隐形眼镜上的脂质吸附、花粉蛋白质的蓄积。然而，在专利文献1中，关于普拉洛芬对SCL的吸附没有进行研究，此外没有公开能够应用于两性离子性SCL的技术。专利文献2中公开了包含普拉洛芬或其盐以及甘草酸盐类的组合物对改善眼睛疲劳有效，能够作为SCL用滴眼剂使用。然而，专利文献2中，没有形成任何关于普拉洛芬对SCL的吸附的研究，此外没有公开作为两性离子性SCL用滴眼剂能够实用化的技术。
此外，针对抑制药物对SCL的吸附的制剂技术也进行研究。例如，专利文献3中公开了包含(A)抗组胺剂、(B)甘草酸和/或其盐、(C)硫酸软骨素和/或其盐、以及(D)0.5w/v％以上的聚乙烯基吡咯烷酮、且pH值为5.5～6.8的SCL用眼科组合物能够抑制抗组胺剂对SCL的吸附。专利文献4中公开了含有(A)氯苯吡胺和/或其盐、以及(B)多元羧酸和/或其盐的离子性硅酮水凝胶隐形眼镜用滴眼剂能够抑制氯苯吡胺和/或其盐对SCL的吸附。然而，在专利文献3和专利文献4中，只是公开了以抑制氯苯吡胺和/或其盐吸附至SCL为目的制剂技术，并没有公开能够应用于普拉洛芬的制剂技术。专利文献5中公开了含有(A)选自具有仲氨基和/或叔氨基的胺及其盐的碱性药物、(B)选自氨基酸及其盐、酸性粘多糖及其盐以及环糊精中的1种或2种以上、且pH值为3.5～4.8的软隐形眼镜用组合物能够抑制碱性药物吸附至SCL。然而，在专利文献5中，没有形成任何关于抑制普拉洛芬吸附至两性离子性SCL的研究，而且由于必须将pH值设定为3.5～4.8，因此在制剂设计上的制约方面也存在问题。
现有技术文献
专利文献
专利文献1：日本特开2011-136980号公报
专利文献2：日本特开2006-232823号公报
专利文献3：日本特开2011-246449号公报
专利文献4：日本特开2010-280649号公报
专利文献5：国际公开第2007/77783号
发明内容
发明所要解决的课题
以往，着眼于普拉洛芬和/或其盐，完全没有形成关于它们对两性离子性SCL的吸附特性的研究。在这样的状况下，本发明者确认了，两性离子性SCL与非离子性SCL、阴离子性SCL不同，存在普拉洛芬和/或其盐的吸附性极高这样特有的课题(参照后述的试验例1)。
因此，本发明的目的在于提供，在包含普拉洛芬和/或其盐的两性离子性SCL用眼科用组合物中，抑制普拉洛芬和/或其盐对两性离子性SCL的吸附的技术。
用于解决课题的方法
本发明者为了解决前述课题而进行了深入研究，结果发现，通过在包含普拉洛芬和/或其盐的两性离子性SCL用眼科用组合物中，使其含有甘草酸和/或其盐，能够有效地抑制普拉洛芬和/或其盐吸附至两性离子性SCL。还发现，通过将前述两性离子性SCL用眼科用组合物中的pH值设定为5.5以上，能够实现澄清的外观性状。本发明是基于以上见解、进而通过反复研究而完成的。
即，本发明提供下述公开的形式的发明。
项1.一种两性离子性软隐形眼镜用眼科用组合物，其特征在于，含有普拉洛芬和/或其可药用的盐、以及甘草酸和/或其可药用的盐。
项2.根据项1所述的两性离子性软隐形眼镜用眼科用组合物，pH值为5.5以上。
项3.根据项1或项2所述的两性离子性软隐形眼镜用眼科用组合物，pH值为5.5～9。
项4.根据项1～3中任一项所述的两性离子性软隐形眼镜用眼科用组合物，含有0.01～1w/v％的甘草酸和/或其可药用的盐。
项5.根据项1～4中任一项所述的两性离子性软隐形眼镜用眼科用组合物，含有0.001～0.5w/v％的普拉洛芬和/或其可药用的盐。
项6.根据项1～5中任一项所述的两性离子性软隐形眼镜用眼科用组合物，是两性离子性软隐形眼镜用滴眼剂。
项7.一种抑制普拉洛芬和/或其可药用的盐吸附至两性离子性软隐形眼镜的方法，其特征在于，在包含普拉洛芬和/或其可药用的盐的两性离子性软隐形眼镜用眼科用组合物中，配合甘草酸和/或其可药用的盐。
项8.下述液体制剂在两性离子性软隐形眼镜用眼科用组合物的制造中的应用，所述液体制剂含有普拉洛芬和/或其可药用的盐、以及甘草酸和/或其可药用的盐。
项9.一种抑制普拉洛芬和/或其可药用的盐吸附至两性离子性软隐形眼镜的方法，包括使下述液体制剂接触两性离子性软隐形眼镜的工序，所述液体制剂含有普拉洛芬和/或其可药用的盐、以及甘草酸和/或其可药用的盐。
发明的效果
通过本发明的两性离子性SCL用眼科用组合物，能够抑制普拉洛芬和/或其盐吸附至两性离子性SCL，因此能够在对两性离子性SCL不产生不良影响的条件下有效地发挥普拉洛芬和/或其盐的药效。此外，通过本发明的两性离子性SCL用眼科用组合物，甘草酸和/或其盐不仅发挥抑制普拉洛芬和/或其盐吸附至两性离子性SCL的作用，还发挥消炎作用，因此还能够联合普拉洛芬和/或其盐的药效，有效地预防或治疗眼的炎症。
此外，通过将本发明的两性离子性SCL用眼科用组合物中的pH值设定为5.5以上，能够抑制普拉洛芬和/或其盐引起的白浊，能够提供呈现澄清的外观性状的两性离子性SCL用眼科用组合物。另外，在本说明书中，所谓“澄清”，是指没有因为普拉洛芬和/或其盐而产生白浊的状态，不限于无色澄清，还包含因其他含有成分而呈现颜色的有色澄清的概念。
具体实施方式
1.两性离子性SCL用眼科用组合物
本发明的两性离子性SCL用眼科用组合物的特征在于，含有普拉洛芬和/或其可药用的盐、以及甘草酸和/或其可药用的盐。以下，对本发明的两性离子性SCL用眼科用组合物进行详述。另外，在本说明书中，所谓“两性离子性SCL用眼科用组合物”，表示在眼科领域中使用的，以与两性离子性SCL接触的形式使用的组合物。此外，在本说明书中，各成分的浓度的单位“w/v％”表示质量对体积的百分率，与g/100mL含义相同。
本发明的两性离子性SCL用眼科用组合物含有普拉洛芬和/或其盐。所谓普拉洛芬，也称为α-甲基-5H-[1]苯并吡喃并[2,3-b]吡啶-7-乙酸，是在眼科领域中已知具有消炎作用的公知的化合物。
作为普拉洛芬的盐，作为可药用的限度，没有特别限制，可举出例如，钠盐、钾盐、钙盐、镁盐、铝盐等金属盐；三乙胺盐、二乙胺盐、吗啉盐、哌嗪盐等有机碱盐等。这些普拉洛芬的盐可以单独使用1种，此外也可以组合2种以上使用。
在本发明的两性离子性SCL用眼科用组合物中，可以从普拉洛芬及其盐中选择1种而单独使用，也可以组合2种以上使用。普拉洛芬及其盐中，优选可举出普拉洛芬。
在本发明的两性离子性SCL用眼科用组合物中，对于普拉洛芬和/或其盐的浓度，根据该两性离子性SCL用眼科用组合物的用途等进行适当设定，可举出例如，0.001～0.5w/v％，优选为0.01～0.2w/v％，更优选为0.01～0.1w/v％。
本发明的两性离子性SCL用眼科用组合物还含有甘草酸和/或其盐。在本发明的两性离子性SCL用眼科用组合物中，通过使甘草酸和/或其盐与前述普拉洛芬和/或其盐一起共存，能够抑制普拉洛芬和/或其盐吸附至两性离子性SCL。
所谓甘草酸，也称为20β-羧基-11-氧代-30-正齐墩果烷-12-烯-3β-基2-O-(β-D-吡喃葡糖基)-α-D-吡喃葡糖醛酸([20β-Carboxy-11-oxo-30-norolean-12-en-3β-yl]2-O-β-D-glucopyranuronosyl-α-D-glucopyranosiduronic acid)，是在眼科领域也作为消炎剂使用的公知的化合物。
作为甘草酸的盐，以可药用为限度就不特别限制，可举出例如，钠盐、钾盐等碱金属盐；镁盐、钙盐等碱土金属盐；铵盐等无机碱盐等。这些甘草酸的盐可以单独使用1种，此外也可以组合2种以上使用。
在本发明的两性离子性SCL用眼科用组合物中，可以从甘草酸及其盐中选择1种单独使用，也可以组合2种以上使用。甘草酸及其盐中，优选为甘草酸的盐，更优选为甘草酸的碱金属盐，进一步优选为甘草酸的钾盐(甘草酸二钾)。
在本发明的两性离子性SCL用眼科用组合物中，对于甘草酸和/或其盐的浓度，可举出例如，0.01～1w/v％。特别是从更进一步有效地抑制普拉洛芬和/或其盐吸附至两性离子性SCL的观点出发，作为甘草酸和/或其盐的浓度，优选为0.01～0.5w/v％，更优选为0.05～0.5w/v％，进一步优选为0.05～0.3w/v％，最优选为0.05～0.25w/v％。
对于本发明的两性离子性SCL用眼科用组合物的pH值，以能够应用于眼粘膜为限度，不特别限制。但是，如后述的试验例所示，确认了：在包含普拉洛芬和/或其盐的组合物中，如果pH值变为4.5以下，则产生普拉洛芬和/或其盐引起的白浊；如果将pH值设定为5.5以上，则能够实现澄清的外观性状。此外，如后述的试验例所示，确认了：在本发明的两性离子性SCL用眼科用组合物中，pH值越高，越能够进一步有效地抑制普拉洛芬和/或其盐吸附至两性离子性SCL。鉴于这些方面，作为本发明的两性离子性SCL用眼科用组合物的pH值，从更进一步有效地抑制普拉洛芬和/或其盐吸附至两性离子性SCL、并且使其具备澄清的外观性状的观点出发，可举出优选为5.5～9，更优选为6.5～9，进一步优选为6.5～8，特别优选为6.5～7.7。
为了将本发明的两性离子性SCL用眼科用组合物的pH值调节到前述范围，只要在眼科用组合物中使用通常使用的pH调节剂、缓冲剂即可。作为pH调节剂，可举出例如，氢氧化钠、氢氧化钾等碱；乙酸、柠檬酸、盐酸、磷酸、酒石酸等酸。这些pH调节剂可以单独使用1种，此外可以组合2种以上使用。此外，作为缓冲剂，可举出例如，磷酸缓冲剂、硼酸缓冲剂、柠檬酸缓冲剂、酒石酸缓冲剂、乙酸缓冲剂、氨基酸、氨丁三醇等。这些缓冲剂可以单独使用1种，此外可以组合2种以上使用。
本发明的两性离子性SCL用眼科用组合物中，除了前述成分以外，可以根据需要含有普拉洛芬和/或其盐以外的药理成分。作为这样的药理成分，可举出例如，尿囊素、ε-氨基己酸、溴芬酸、酮咯酸氨丁三醇、奈帕芬胺、盐酸小檗碱、硫酸小檗碱、薁磺酸钠、硫酸锌、乳酸锌、盐酸溶菌酶等消炎剂；马来酸氯苯那敏、盐酸苯海拉明等抗组胺剂；色甘酸钠、酮替芬富马酸盐、阿扎司特、氨来呫诺、吡嘧司特钾、曲尼司特、异丁司特等抗变态反应剂；诺氟沙星、氧氟沙星、洛美沙星、左氧氟沙星、庆大霉素、加替沙星等抗菌剂；抗坏血酸、黄素腺嘌呤二核苷酸钠、氰钴胺素、盐酸吡哆素、生育酚乙酸酯、视黄醇乙酸酯、视黄醇棕榈酸酯、泛醇、泛酸钙、泛酸钠等维生素类；天冬氨酸、牛磺酸、硫酸软骨素钠等氨基酸类、新斯的明甲基硫酸盐等抗胆碱酯酶剂；萘甲唑啉、四氢唑啉、肾上腺素、麻黄碱、去氧肾上腺素、dl-甲基麻黄碱等血管收缩剂；透明质酸钠等角膜结膜上皮障碍治疗药；磺胺嘧啶、磺胺异唑、磺胺索嘧啶、磺胺二甲氧哒嗪、磺胺甲氧哒嗪、磺胺甲唑、磺胺乙二唑、磺胺托嘧啶、磺胺苯吡唑、磺胺脒、酞磺胺噻唑、琥珀磺胺噻唑等磺胺剂等。这里示例的化合物，作为可药用的限度，可以是盐的形态，此外也可以是其他的盐的形态。这些药理成分可以单独使用1种，此外也可以组合2种以上使用。
对于这些药理成分的浓度，根据药理成分的种类、两性离子性SCL用眼科用组合物的用途等进行适当设定。
此外，本发明的两性离子性SCL用眼科用组合物中，除了前述成分以外，也可以根据需要含有等张剂、助溶剂、粘稠剂、螯合剂、清凉剂、防腐剂、稳定剂、表面活性剂等添加剂。
作为等张剂，可举出山梨糖醇、葡萄糖、甘露糖醇等糖类；甘油、丙二醇等多元醇类；氯化钠等盐类；硼酸等。这些等张剂可以单独使用1种，此外也可以组合2种以上使用。
作为助溶剂，可举出例如，聚氧乙烯失水山梨糖醇单油酸酯、聚氧乙烯硬化蓖麻油、泰洛沙泊、普朗尼克(Pluronic)等非离子性表面活性剂；甘油、聚乙二醇(macrogol)等多元醇等。这些助溶剂可以单独使用1种，此外也可以组合2种以上使用。
作为粘稠剂，可举出例如，聚乙烯基吡咯烷酮、聚乙二醇、聚乙烯醇、羧基乙烯基聚合物、黄原胶、硫酸软骨素钠、透明质酸钠等水溶性高分子；羟丙甲纤维素、羟乙基纤维素、甲基纤维素、羟丙基纤维素、羟丙基甲基纤维素、羧甲基纤维素钠等纤维素类等。这些粘稠剂可以单独使用1种，此外也可以组合2种以上使用。
作为螯合剂，可举出例如，乙二胺四乙酸盐、柠檬酸或其盐等。这些螯合剂可以单独使用1种，此外也可以组合2种以上使用。
作为清凉剂，可举出例如，l-薄荷醇、冰片、樟脑、桉树油等。这些清凉剂可以单独使用1种，此外也可以组合2种以上使用。
作为防腐剂，可举出例如，山梨酸或其盐、苯甲酸或其盐、对羟基苯甲酸甲酯、对羟基苯甲酸乙酯、对羟基苯甲酸丙酯、氯丁醇、氯己定葡糖酸盐、硼酸、脱氢乙酸或其盐、苯扎氯铵、苄索氯铵、苯甲醇、氯化锌、对氯间二甲苯酚、氯甲酚、苯乙醇、泊利氯铵、硫柳汞、二丁基羟基甲苯等。这些防腐剂可以单独使用1种，此外也可以组合2种以上使用。
作为稳定剂，可举出例如，聚乙烯基吡咯烷酮、亚硫酸盐、单乙醇胺、甘油、丙二醇、环糊精、葡聚糖、抗坏血酸、乙二胺四乙酸盐、牛磺酸、生育酚、二丁基羟基甲苯等。这些稳定剂可以单独使用1种，此外也可以组合2种以上使用。
作为表面活性剂，可举出例如，泰洛沙泊、聚氧乙烯硬化蓖麻油、聚氧乙烯聚氧丙烯嵌段共聚物、聚氧乙烯失水山梨糖醇脂肪酸酯、辛苯昔醇(octoxynol)等非离子性表面活性剂；烷基二氨基乙基甘氨酸、月桂基二甲基氨基乙酸甜菜碱等两性表面活性剂；烷基硫酸盐、N-酰基牛磺酸盐、聚氧乙烯烷基醚磷酸盐、聚氧乙烯烷基醚硫酸盐等阴离子表面活性剂；烷基吡啶盐、烷基胺盐等阳离子表面活性剂等。这些表面活性剂可以单独使用1种，此外也可以组合2种以上使用。
对于这些添加剂的浓度，根据添加剂的种类、两性离子性SCL用眼科用组合物的用途等进行适当设定。
对于本发明的两性离子性SCL用眼科用组合物的制剂形态，只要是包含水作为基剂的液体制剂即可，例如，可以是水溶液状、乳液状等中的任一种，但是优选可举出水溶液状。
本发明的两性离子性SCL用眼科用组合物，只要根据其用途，按照自身公知的调制法制造即可，例如，可以使用第十六版改正日本药典制剂总则所记载的方法来制造。
本发明的两性离子性SCL用眼科用组合物可以以下述形式使用：即使在佩戴两性离子性SCL中也能够滴眼的滴眼剂(两性离子性SCL用滴眼剂)；即使在佩戴两性离子性SCL中也能够洗眼的洗眼剂(两性离子性SCL用洗眼剂)；两性离子性SCL用佩戴液、两性离子性SCL用多功能护理液、两性离子性SCL用洗涤液、两性离子性SCL用保存液等隐形眼镜护理用品等。其中，可优选举出两性离子性SCL用滴眼剂、两性离子性SCL用洗眼剂，更优选两性离子性SCL用滴眼剂。
成为本发明的适用对象的两性离子性SCL，是以含有包含阳离子性基团的单体和包含阴离子性基团的单体作为离子性单体的聚合物作为构成材料的SCL。作为两性离子性SCL，具体地可举出以包含季铵盐等阳离子性基团和羧基、磺酸基、磷酸基等阴离子性基团的聚合物为构成材料的SCL，对于该材料、制法，例如，日本特开平10-197831号公报等有所记载。
此外，成为本发明的适用对象的两性离子性SCL，可以是高含水率或低含水率，但可优选举出高含水率，即美国食品药品局(FDA)中分类为组IV(离子性单体1摩尔％以上，含水率50％以上)的SCL。
2.抑制普拉洛芬和/或其盐吸附至两性离子性SCL的方法(1)
此外，本发明提供抑制普拉洛芬和/或其盐吸附至两性离子性SCL的方法，其特征在于，在包含普拉洛芬和/或其可药用的盐的两性离子性SCL用眼科用组合物中，配合甘草酸和/或其可药用的盐。该吸附抑制方法在赋予两性离子性SCL用眼科用组合物抑制普拉洛芬和/或其盐吸附至两性离子性SCL的作用方面是有用的。
在本发明的吸附抑制方法中，对于所使用的普拉洛芬和/或其可药用的盐的种类、浓度、甘草酸和/或其可药用的盐的种类、浓度、两性离子性SCL用眼科用组合物的pH值、配合在两性离子性SCL用眼科用组合物中的药理成分、添加剂的种类、两性离子性SCL用眼科用组合物的制剂形态、用途、成为适用对象的两性离子性SCL的种类等，如前述“1.两性离子性SCL用眼科用组合物”栏所记载的那样。
3.抑制普拉洛芬和/或其盐吸附至两性离子性SCL的方法(2)
此外，本发明提供抑制普拉洛芬和/或其可药用的盐吸附至两性离子性SCL的方法，包含使下述液体制剂接触两性离子性SCL的工序，所述液体制剂含有普拉洛芬和/或其可药用的盐、以及甘草酸和/或其可药用的盐。
在本发明的吸附抑制方法中，对于所使用的普拉洛芬和/或其可药用的盐的种类、浓度、甘草酸和/或其可药用的盐的种类、浓度、液体制剂的pH值、配合在液体制剂中的药理成分、添加剂的种类、液体制剂的制剂形态、用途、成为适用对象的两性离子性SCL的种类等，如前述“1.两性离子性SCL用眼科用组合物”栏所记载的那样。此外，在本发明的吸附抑制方法中，使前述液体制剂接触两性离子性SCL的方法，只要根据该液体制剂的用途进行适当设定即可。例如，在前述液体制剂为滴眼剂的情况下，只要对佩戴了两性离子性SCL的眼睛滴加前述液体制剂即可。
实施例
以下举出实施例对本发明进行具体地说明，但本发明不受这些实施例任何限定。
试验例1
通过用常法将表1所示的各成分混合，来调制试验液。通过观察所得的各试验液的外观，并且测定浊度(660nm下的吸光度)来评价白浊的有无。
此外，将各试验液3mL放入小瓶中，在其中浸渍SCL1片，在25℃下振荡2小时以上。此外，将各试验液3mL放入小瓶中并且在不浸渍SCL的状态下，在25℃下振荡2小时以上。通过液相色谱法测定振荡后各试验液中的普拉洛芬含量，按照下述式，算出普拉洛芬对SCL的吸附量。另外，如果在将SCL浸渍于试验液的条件下振荡，则2小时以内普拉洛芬对SCL的吸附达到平衡状态，因此，如果将振荡时间设定为2小时以上，则可以确认对普拉洛芬对SCL的吸附量的测定值无影响。
吸附于1片SCL的普拉洛芬量(μg)＝(CC-CT)×V
CC：未浸渍SCL的试验液中的普拉洛芬含量(μg/mL)
CT：浸渍了SCL的试验液中的普拉洛芬含量(μg/mL)
V：试验中使用的试验液的量(mL)
另外，本试验中，使用下述3种SCL，求出了普拉洛芬对各SCL的吸附量。
眼镜1：组IV、商品名“シード1dayPure”(注册商标)株式会社シード社制)、两性离子性、眼镜材料：甲基丙烯酸2-羟基乙酯(HEMA)、含有季铵基的甲基丙烯酸酯系化合物、含有羧基的甲基丙烯酸酯系化合物、甲基丙烯酸甲酯(MMA)、乙二醇二甲基丙烯酸酯(EGDMA)
眼镜2：组IV、商品名“ワンデーアキュビュー(注册商标)”(ジョンソンエンドジョンソン株式会社制)、阴离子性、USAN名：etafilcon A
眼镜3：硅酮水凝胶隐形眼镜、组I、商品名“エアオプティクス2ウィーク(注册商标)”(チバビジョン株式会社制)、USAN名：lotrafilcon B
将所得的结果示于表1。如比较例1的结果表明那样，两性离子性SCL中的普拉洛芬的吸附量，与阴离子性SCL和非离子性SCL相比显著增多，可知两性离子性SCL具有极其容易吸附普拉洛芬的特有的特性。此外，在与普拉洛芬一起含有甘草酸二钾的试验液(实施例1)中，能够显著抑制普拉洛芬对两性离子性SCL的吸附。与此相对，在与普拉洛芬一起含有甘草酸二钾以外的具有消炎作用的药物的试验液(比较例2和比较例3)中，几乎不能观察到或者仅能观察到微量的普拉洛芬对两性离子性SCL的吸附抑制效果。以上结果表明，抑制普拉洛芬吸附至两性离子性SCL的效果是甘草酸和/或其盐特有的性质。此外，在pH值为7.7的全部试验液中，显示不能观察到白浊的澄清的外观性状。
[表1]
表中，各配合成分的配合量的单位是“w/v％”。此外，n.m.表示未测得。
试验例2
通过将表2所示的各成分用常法混合来调制试验液。通过观察所得的各试验液的外观，并且测定浊度(660nm下的吸光度)来评价白浊的有无。此外，对于所得的各试验液，通过与前述试验例1同样的方法，测定了普拉洛芬对两性离子性SCL的吸附量。
将所得的结果示于表2。根据该结果，在包含甘草酸二钾的试验液中，能够有效地抑制普拉洛芬吸附至两性离子性SCL。此外确认了，在任一试验液中，均呈现澄清的外观性状。
[表2]
试验例3
通过用常法将表3所示的各成分混合来调制试验液。通过观察所得的各试验液的外观，并且测定浊度(660nm下的吸光度)来评价白浊的有无。
将所得的结果示于表3。如表3表明那样，在pH值为4.5以下的情况下，在任一包含普拉洛芬的试验液中均可以观察到白浊。根据上述试验例1和试验例2的结果，明确了，通过与普拉洛芬一起使其含有甘草酸和/或其盐、且将pH值设定为5.5以上，能够在使其呈现澄清的外观性状的同时，抑制普拉洛芬吸附至两性离子性SCL。
[表3]
表中，各配合成分的配合量的单位是“w/v％”。
参考试验例1
通过用常法将表4所示的各成分混合来调制试验液。通过观察所得的各试验液的外观，并且测定浊度(660nm下的吸光度)来评价白浊的有无。此外，对于所得的各试验液，测定氯苯吡胺马来酸盐的吸附量来代替普拉洛芬的吸附量，除此以外，通过与前述试验例1同样的方法，求出氯苯吡胺马来酸盐在两性离子性SCL和硅酮水凝胶隐形眼镜上的吸附量。另外，氯苯吡胺马来酸盐含量利用液相色谱法测定。
将所得的结果示于表4。由该结果可知，氯苯吡胺马来酸盐对两性离子性SCL的吸附由于甘草酸二钾而增强。即，本结果表明，对于氯苯吡胺马来酸盐和普拉洛芬，对两性离子性SCL的吸附特性不同，氯苯吡胺马来酸盐对硅酮水凝胶隐形眼镜的吸附抑制方法不能适用于普拉洛芬对两性离子性SCL的吸附抑制方法。
[表4]
表中，各配合成分的配合量的单位是“w/v％”。
Claims (8)
1.下述液体制剂在两性离子性软隐形眼镜用眼科用组合物的制造中的应用，所述液体制剂含有普拉洛芬和/或其可药用的盐、以及甘草酸和/或其可药用的盐。
2.根据权利要求1所述的应用，其中，所述液体制剂的pH值为5.5以上。
3.根据权利要求1或2所述的应用，其中，所述液体制剂的pH值为5.5～9。
4.根据权利要求1或2所述的应用，其中，所述液体制剂含有0.01～1w/v％的甘草酸和/或其可药用的盐。
5.根据权利要求1或2所述的应用，其中，所述液体制剂含有0.001～0.5w/v％的普拉洛芬和/或其可药用的盐。
6.根据权利要求1或2所述的应用，其中，所述两性离子性软隐形眼镜用眼科用组合物是两性离子性软隐形眼镜用滴眼剂。
7.一种抑制普拉洛芬和/或其可药用的盐吸附至两性离子性软隐形眼镜的方法，其特征在于，在含有普拉洛芬和/或其可药用的盐的两性离子性软隐形眼镜用眼科用组合物中，配合甘草酸和/或其可药用的盐，并且将pH值调整为5.5以上。
8.一种抑制普拉洛芬和/或其可药用的盐吸附至两性离子性软隐形眼镜的方法，包括使下述液体制剂接触两性离子性软隐形眼镜的工序，所述液体制剂含有普拉洛芬和/或其可药用的盐、以及甘草酸和/或其可药用的盐，并且pH值为5.5以上。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2013191715 | 2013-09-17 | ||
| JP2013-191715 | 2013-09-17 | ||
| PCT/JP2014/074347 WO2015041193A1 (ja) | 2013-09-17 | 2014-09-16 | 両性イオン性ソフトコンタクトレンズ用眼科用組成物 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN105530936A CN105530936A (zh) | 2016-04-27 |
| CN105530936B true CN105530936B (zh) | 2019-01-04 |
Family
ID=52688844
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201480050749.5A Expired - Fee Related CN105530936B (zh) | 2013-09-17 | 2014-09-16 | 两性离子性软隐形眼镜用眼科用组合物 |
Country Status (6)
| Country | Link |
|---|---|
| JP (1) | JP6449774B2 (zh) |
| CN (1) | CN105530936B (zh) |
| HK (1) | HK1220922A1 (zh) |
| RU (1) | RU2670100C2 (zh) |
| TW (2) | TW201936173A (zh) |
| WO (1) | WO2015041193A1 (zh) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2017105752A (ja) * | 2015-08-31 | 2017-06-15 | ロート製薬株式会社 | 眼科組成物 |
| CN114761022B (zh) * | 2019-11-29 | 2024-02-13 | 千寿制药株式会社 | 药物组合物 |
| KR20210072720A (ko) * | 2019-12-09 | 2021-06-17 | 니치유 가부시키가이샤 | 소프트 콘택트렌즈용 화분 흡착 억제제 및 화분 단백 흡착 억제제 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2006232823A (ja) * | 2005-01-26 | 2006-09-07 | Rohto Pharmaceut Co Ltd | プラノプロフェン含有組成物 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5693337A (en) * | 1994-07-13 | 1997-12-02 | Wakamoto Pharmaceutical Co., Ltd. | Stable lipid emulsion |
| JP4789479B2 (ja) * | 2004-02-23 | 2011-10-12 | ロート製薬株式会社 | プラノプロフェン含有水性組成物 |
| CN101222939B (zh) * | 2005-07-13 | 2010-11-24 | 参天制药株式会社 | 眼科用防腐组合物 |
| CN101351199B (zh) * | 2005-12-27 | 2013-01-02 | 狮王株式会社 | 软性接触镜用组合物及吸附抑制方法 |
| JP2008024701A (ja) * | 2006-06-21 | 2008-02-07 | Rohto Pharmaceut Co Ltd | アルギン酸又はその塩を含有するソフトコンタクトレンズ用組成物 |
| JPWO2008001872A1 (ja) * | 2006-06-28 | 2009-11-26 | ロート製薬株式会社 | アルギン酸又はその塩を含有する眼科用組成物 |
| JP5340498B1 (ja) * | 2013-03-11 | 2013-11-13 | 千寿製薬株式会社 | ソフトコンタクトレンズ用眼科用組成物 |
-
2014
- 2014-09-16 TW TW108119026A patent/TW201936173A/zh unknown
- 2014-09-16 TW TW103131934A patent/TW201542241A/zh unknown
- 2014-09-16 JP JP2015537912A patent/JP6449774B2/ja not_active Expired - Fee Related
- 2014-09-16 WO PCT/JP2014/074347 patent/WO2015041193A1/ja active Application Filing
- 2014-09-16 RU RU2016111957A patent/RU2670100C2/ru not_active IP Right Cessation
- 2014-09-16 CN CN201480050749.5A patent/CN105530936B/zh not_active Expired - Fee Related
-
2016
- 2016-08-01 HK HK16109148.4A patent/HK1220922A1/zh unknown
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2006232823A (ja) * | 2005-01-26 | 2006-09-07 | Rohto Pharmaceut Co Ltd | プラノプロフェン含有組成物 |
Non-Patent Citations (1)
| Title |
|---|
| Adsorption of Actives in Ophthalmological Drugs for Over-The-Counter on Soft Contact Lens Surfaces;Nobuhito Tabuchi等;《Journal of Oleo Science》;20091231;第58卷(第1期);第43-52页 |
Also Published As
| Publication number | Publication date |
|---|---|
| RU2670100C2 (ru) | 2018-10-18 |
| RU2016111957A3 (zh) | 2018-04-03 |
| JPWO2015041193A1 (ja) | 2017-03-02 |
| TW201936173A (zh) | 2019-09-16 |
| TW201542241A (zh) | 2015-11-16 |
| JP6449774B2 (ja) | 2019-01-09 |
| HK1220922A1 (zh) | 2017-05-19 |
| WO2015041193A1 (ja) | 2015-03-26 |
| CN105530936A (zh) | 2016-04-27 |
| RU2016111957A (ru) | 2017-10-23 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP5616620B2 (ja) | 非イオン性シリコーンハイドロゲルコンタクトレンズ用眼科組成物 | |
| JP5616618B2 (ja) | シリコーンハイドロゲルコンタクトレンズ用眼科組成物 | |
| JP5627294B2 (ja) | コンタクトレンズ用眼科組成物 | |
| CN105530936B (zh) | 两性离子性软隐形眼镜用眼科用组合物 | |
| JP5725786B2 (ja) | 非イオン性シリコーンハイドロゲルコンタクトレンズ用眼科組成物 | |
| CN105555268B (zh) | 阴离子性软隐形眼镜用眼科用组合物 | |
| TWI626049B (zh) | Ophthalmic composition for soft contact lenses | |
| CN105392481B (zh) | 两性离子性软性隐形眼镜用眼科用组合物 | |
| CN105283183B (zh) | 两性离子性软性隐形眼镜用眼科用组合物 | |
| JP5879410B2 (ja) | コンタクトレンズ用眼科組成物 | |
| JP6687781B1 (ja) | 刺激感が抑制された眼科組成物 | |
| JP2020109121A (ja) | シリコーンハイドロゲルコンタクトレンズ用眼科組成物 | |
| JP2021187857A (ja) | ソフトコンタクトレンズ用眼科組成物 | |
| JP2016222727A (ja) | シリコーンハイドロゲルコンタクトレンズ用眼科組成物 | |
| JP2016056213A (ja) | コンタクトレンズ用眼科組成物 | |
| JP2014205717A (ja) | シリコーンハイドロゲルコンタクトレンズ用眼科組成物 | |
| JP2015098473A (ja) | シリコーンハイドロゲルコンタクトレンズ用眼科組成物 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| REG | Reference to a national code |
Ref country code: HK Ref legal event code: DE Ref document number: 1220922 Country of ref document: HK |
|
| CB02 | Change of applicant information |
Address after: Japan's Osaka Prefecture, Osaka, Central District, three, 1, 9, 5410048 Applicant after: SENJU PHARMA CO(JP) Address before: Osaka Japan Applicant before: SENJU PHARMA CO(JP) |
|
| CB02 | Change of applicant information | ||
| GR01 | Patent grant | ||
| GR01 | Patent grant | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20190104 Termination date: 20200916 |
|
| CF01 | Termination of patent right due to non-payment of annual fee | ||
| REG | Reference to a national code |
Ref country code: HK Ref legal event code: WD Ref document number: 1220922 Country of ref document: HK |