JP2009073828A - 点眼剤 - Google Patents
点眼剤 Download PDFInfo
- Publication number
- JP2009073828A JP2009073828A JP2008220671A JP2008220671A JP2009073828A JP 2009073828 A JP2009073828 A JP 2009073828A JP 2008220671 A JP2008220671 A JP 2008220671A JP 2008220671 A JP2008220671 A JP 2008220671A JP 2009073828 A JP2009073828 A JP 2009073828A
- Authority
- JP
- Japan
- Prior art keywords
- gellan gum
- trometamol
- eye drop
- ophthalmic solution
- sulfa
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 239000002997 ophthalmic solution Substances 0.000 title claims abstract description 15
- 229940054534 ophthalmic solution Drugs 0.000 title claims abstract description 15
- 229920002148 Gellan gum Polymers 0.000 claims abstract description 35
- 239000000216 gellan gum Substances 0.000 claims abstract description 34
- 235000010492 gellan gum Nutrition 0.000 claims abstract description 34
- 229940079593 drug Drugs 0.000 claims abstract description 31
- 239000003814 drug Substances 0.000 claims abstract description 31
- 150000003839 salts Chemical class 0.000 claims abstract description 22
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 claims abstract description 22
- 229960000281 trometamol Drugs 0.000 claims abstract description 22
- 229910052751 metal Inorganic materials 0.000 claims abstract description 19
- 239000002184 metal Substances 0.000 claims abstract description 19
- HZAXFHJVJLSVMW-UHFFFAOYSA-N 2-Aminoethan-1-ol Chemical compound NCCO HZAXFHJVJLSVMW-UHFFFAOYSA-N 0.000 claims abstract description 14
- 238000013329 compounding Methods 0.000 claims abstract description 8
- 239000003889 eye drop Substances 0.000 claims description 46
- 229940012356 eye drops Drugs 0.000 claims description 15
- 238000002360 preparation method Methods 0.000 claims description 15
- 229960005404 sulfamethoxazole Drugs 0.000 claims description 7
- JLKIGFTWXXRPMT-UHFFFAOYSA-N sulphamethoxazole Chemical group O1C(C)=CC(NS(=O)(=O)C=2C=CC(N)=CC=2)=N1 JLKIGFTWXXRPMT-UHFFFAOYSA-N 0.000 claims description 7
- NHUHCSRWZMLRLA-UHFFFAOYSA-N Sulfisoxazole Chemical compound CC1=NOC(NS(=O)(=O)C=2C=CC(N)=CC=2)=C1C NHUHCSRWZMLRLA-UHFFFAOYSA-N 0.000 claims description 4
- 229960000654 sulfafurazole Drugs 0.000 claims description 4
- 239000002244 precipitate Substances 0.000 abstract description 17
- 230000000844 anti-bacterial effect Effects 0.000 abstract description 10
- 230000014759 maintenance of location Effects 0.000 abstract description 8
- 238000003860 storage Methods 0.000 abstract description 5
- 239000000243 solution Substances 0.000 abstract description 4
- 210000004400 mucous membrane Anatomy 0.000 abstract 1
- 238000002156 mixing Methods 0.000 description 21
- 239000000499 gel Substances 0.000 description 14
- 230000000052 comparative effect Effects 0.000 description 13
- -1 alkali metal salts Chemical class 0.000 description 12
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 12
- 239000000203 mixture Substances 0.000 description 12
- 239000003795 chemical substances by application Substances 0.000 description 11
- 210000004877 mucosa Anatomy 0.000 description 10
- 238000012360 testing method Methods 0.000 description 10
- 239000000872 buffer Substances 0.000 description 9
- 239000011734 sodium Substances 0.000 description 9
- 239000003513 alkali Substances 0.000 description 8
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 6
- KGBXLFKZBHKPEV-UHFFFAOYSA-N boric acid Chemical compound OB(O)O KGBXLFKZBHKPEV-UHFFFAOYSA-N 0.000 description 6
- 239000004327 boric acid Substances 0.000 description 6
- 150000001768 cations Chemical class 0.000 description 6
- 230000000694 effects Effects 0.000 description 6
- 238000001914 filtration Methods 0.000 description 6
- BTBUEUYNUDRHOZ-UHFFFAOYSA-N Borate Chemical compound [O-]B([O-])[O-] BTBUEUYNUDRHOZ-UHFFFAOYSA-N 0.000 description 5
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 5
- 239000007788 liquid Substances 0.000 description 5
- 239000000126 substance Substances 0.000 description 5
- XOAAWQZATWQOTB-UHFFFAOYSA-N taurine Chemical compound NCCS(O)(=O)=O XOAAWQZATWQOTB-UHFFFAOYSA-N 0.000 description 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 5
- 239000000654 additive Substances 0.000 description 4
- 239000002585 base Substances 0.000 description 4
- 230000015572 biosynthetic process Effects 0.000 description 4
- 239000007979 citrate buffer Substances 0.000 description 4
- 239000001509 sodium citrate Substances 0.000 description 4
- 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 4
- 159000000000 sodium salts Chemical class 0.000 description 4
- 239000002562 thickening agent Substances 0.000 description 4
- SLXKOJJOQWFEFD-UHFFFAOYSA-N 6-aminohexanoic acid Chemical compound NCCCCCC(O)=O SLXKOJJOQWFEFD-UHFFFAOYSA-N 0.000 description 3
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- 229910052783 alkali metal Inorganic materials 0.000 description 3
- 229910052784 alkaline earth metal Inorganic materials 0.000 description 3
- 229960002684 aminocaproic acid Drugs 0.000 description 3
- 239000000607 artificial tear Substances 0.000 description 3
- 229910021538 borax Inorganic materials 0.000 description 3
- 239000006172 buffering agent Substances 0.000 description 3
- 238000009472 formulation Methods 0.000 description 3
- 238000004519 manufacturing process Methods 0.000 description 3
- 230000003204 osmotic effect Effects 0.000 description 3
- 238000001556 precipitation Methods 0.000 description 3
- 239000008213 purified water Substances 0.000 description 3
- 235000010339 sodium tetraborate Nutrition 0.000 description 3
- 230000001954 sterilising effect Effects 0.000 description 3
- 238000004659 sterilization and disinfection Methods 0.000 description 3
- UCTWMZQNUQWSLP-VIFPVBQESA-N (R)-adrenaline Chemical compound CNC[C@H](O)C1=CC=C(O)C(O)=C1 UCTWMZQNUQWSLP-VIFPVBQESA-N 0.000 description 2
- WRMNZCZEMHIOCP-UHFFFAOYSA-N 2-phenylethanol Chemical compound OCCC1=CC=CC=C1 WRMNZCZEMHIOCP-UHFFFAOYSA-N 0.000 description 2
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 2
- GLZPCOQZEFWAFX-UHFFFAOYSA-N Geraniol Chemical compound CC(C)=CCCC(C)=CCO GLZPCOQZEFWAFX-UHFFFAOYSA-N 0.000 description 2
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 2
- FQISKWAFAHGMGT-SGJOWKDISA-M Methylprednisolone sodium succinate Chemical compound [Na+].C([C@@]12C)=CC(=O)C=C1[C@@H](C)C[C@@H]1[C@@H]2[C@@H](O)C[C@]2(C)[C@@](O)(C(=O)COC(=O)CCC([O-])=O)CC[C@H]21 FQISKWAFAHGMGT-SGJOWKDISA-M 0.000 description 2
- DJDFFEBSKJCGHC-UHFFFAOYSA-N Naphazoline Chemical compound Cl.C=1C=CC2=CC=CC=C2C=1CC1=NCCN1 DJDFFEBSKJCGHC-UHFFFAOYSA-N 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
- GUGOEEXESWIERI-UHFFFAOYSA-N Terfenadine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 GUGOEEXESWIERI-UHFFFAOYSA-N 0.000 description 2
- 235000010443 alginic acid Nutrition 0.000 description 2
- 239000000783 alginic acid Substances 0.000 description 2
- 229920000615 alginic acid Polymers 0.000 description 2
- 229960001126 alginic acid Drugs 0.000 description 2
- 150000004781 alginic acids 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
- 235000001014 amino acid Nutrition 0.000 description 2
- 150000001413 amino acids Chemical class 0.000 description 2
- 230000001387 anti-histamine Effects 0.000 description 2
- 230000003110 anti-inflammatory effect Effects 0.000 description 2
- 239000000739 antihistaminic agent Substances 0.000 description 2
- 239000003899 bactericide agent Substances 0.000 description 2
- 229960000686 benzalkonium chloride Drugs 0.000 description 2
- 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 2
- 229960001950 benzethonium chloride Drugs 0.000 description 2
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 description 2
- 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 2
- 150000001642 boronic acid derivatives Chemical class 0.000 description 2
- 239000004359 castor oil Substances 0.000 description 2
- 235000019438 castor oil Nutrition 0.000 description 2
- OSASVXMJTNOKOY-UHFFFAOYSA-N chlorobutanol Chemical compound CC(C)(O)C(Cl)(Cl)Cl OSASVXMJTNOKOY-UHFFFAOYSA-N 0.000 description 2
- 150000001860 citric acid derivatives Chemical class 0.000 description 2
- DDRJAANPRJIHGJ-UHFFFAOYSA-N creatinine Chemical compound CN1CC(=O)NC1=N DDRJAANPRJIHGJ-UHFFFAOYSA-N 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
- 239000000850 decongestant Substances 0.000 description 2
- 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 2
- JYGXADMDTFJGBT-VWUMJDOOSA-N hydrocortisone Chemical compound O=C1CC[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 JYGXADMDTFJGBT-VWUMJDOOSA-N 0.000 description 2
- CGIGDMFJXJATDK-UHFFFAOYSA-N indomethacin Chemical compound CC1=C(CC(O)=O)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 CGIGDMFJXJATDK-UHFFFAOYSA-N 0.000 description 2
- 239000003589 local anesthetic agent Substances 0.000 description 2
- 230000007721 medicinal effect Effects 0.000 description 2
- 239000001525 mentha piperita l. herb oil Substances 0.000 description 2
- 229960004584 methylprednisolone Drugs 0.000 description 2
- 210000003205 muscle Anatomy 0.000 description 2
- 239000003002 pH adjusting agent Substances 0.000 description 2
- 235000019477 peppermint oil Nutrition 0.000 description 2
- 239000008363 phosphate buffer Substances 0.000 description 2
- 239000003755 preservative agent Substances 0.000 description 2
- NGVDGCNFYWLIFO-UHFFFAOYSA-N pyridoxal 5'-phosphate Chemical compound CC1=NC=C(COP(O)(O)=O)C(C=O)=C1O NGVDGCNFYWLIFO-UHFFFAOYSA-N 0.000 description 2
- 230000000717 retained effect Effects 0.000 description 2
- 239000004328 sodium tetraborate Substances 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- 239000003381 stabilizer Substances 0.000 description 2
- 150000003431 steroids Chemical class 0.000 description 2
- 235000000346 sugar Nutrition 0.000 description 2
- 150000008163 sugars Chemical class 0.000 description 2
- 239000004094 surface-active agent Substances 0.000 description 2
- 230000002459 sustained effect Effects 0.000 description 2
- 229940088594 vitamin Drugs 0.000 description 2
- 235000013343 vitamin Nutrition 0.000 description 2
- 239000011782 vitamin Substances 0.000 description 2
- 229930003231 vitamin Natural products 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
- YLXIPWWIOISBDD-NDAAPVSOSA-N (2r,3r)-2,3-dihydroxybutanedioic acid;4-[(1r)-1-hydroxy-2-(methylamino)ethyl]benzene-1,2-diol Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O.CNC[C@H](O)C1=CC=C(O)C(O)=C1 YLXIPWWIOISBDD-NDAAPVSOSA-N 0.000 description 1
- 229930182837 (R)-adrenaline Natural products 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
- VAZJLPXFVQHDFB-UHFFFAOYSA-N 1-(diaminomethylidene)-2-hexylguanidine Polymers CCCCCCN=C(N)N=C(N)N VAZJLPXFVQHDFB-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
- OVSKIKFHRZPJSS-UHFFFAOYSA-N 2,4-D Chemical compound OC(=O)COC1=CC=C(Cl)C=C1Cl OVSKIKFHRZPJSS-UHFFFAOYSA-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
- BFUUJUGQJUTPAF-UHFFFAOYSA-N 2-(3-amino-4-propoxybenzoyl)oxyethyl-diethylazanium;chloride Chemical compound [Cl-].CCCOC1=CC=C(C(=O)OCC[NH+](CC)CC)C=C1N BFUUJUGQJUTPAF-UHFFFAOYSA-N 0.000 description 1
- LEACJMVNYZDSKR-UHFFFAOYSA-N 2-octyldodecan-1-ol Chemical compound CCCCCCCCCCC(CO)CCCCCCCC LEACJMVNYZDSKR-UHFFFAOYSA-N 0.000 description 1
- ZXSGQNYQJIUMQN-UHFFFAOYSA-N 3-(2-methylpiperidin-1-ium-1-yl)propyl benzoate;chloride Chemical compound Cl.CC1CCCCN1CCCOC(=O)C1=CC=CC=C1 ZXSGQNYQJIUMQN-UHFFFAOYSA-N 0.000 description 1
- FHVDTGUDJYJELY-UHFFFAOYSA-N 6-{[2-carboxy-4,5-dihydroxy-6-(phosphanyloxy)oxan-3-yl]oxy}-4,5-dihydroxy-3-phosphanyloxane-2-carboxylic acid Chemical class O1C(C(O)=O)C(P)C(O)C(O)C1OC1C(C(O)=O)OC(OP)C(O)C1O FHVDTGUDJYJELY-UHFFFAOYSA-N 0.000 description 1
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- 208000035143 Bacterial infection Diseases 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
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- BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 1
- 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 1
- 241000723346 Cinnamomum camphora Species 0.000 description 1
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- 206010010741 Conjunctivitis Diseases 0.000 description 1
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- 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
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- 239000005792 Geraniol Substances 0.000 description 1
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- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 description 1
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Abstract
【解決手段】(a)金属塩を形成していないサルファ剤、(b)ジェランガム、及び(c)トロメタモール、を配合することを特徴とする点眼剤。及び
(a)金属塩を形成していないサルファ剤、(b)0.001W/V%以上0.07W/V%以下のジェランガム、及び(c)トロメタモール及び/又はモノエタノールアミン、を配合することを特徴とする点眼剤。
【選択図】 なし
Description
(1)(a)金属塩を形成していないサルファ剤、(b)ジェランガム、及び(c)トロメタモール、を配合することを特徴とする点眼剤。
(2)(a)金属塩を形成していないサルファ剤、(b)0.001W/V%以上0.07W/V%以下のジェランガム、及び(c)トロメタモール及び/又はモノエタノールアミン、を配合することを特徴とする点眼剤。
(3)ジェランガムの配合量が0.07W/V%より大きく1.0W/V%以下である(1)に記載の点眼剤。
(4)0.0001W/V%以上0.9W/V%以下のモノエタノールアミンを更に配合することを特徴とする(3)に記載の点眼剤。
(5)pHが7.6以上であることを特徴とする(1)〜(4)のいずれか1つに記載の点眼剤。
(6)トロメタモールの配合量が0.3W/V%以上10W/V%以下である(1)〜(5)
のいずれかに記載の点眼剤。
(7)トロメタモールの配合量が2W/V%以上10W/V%以下である(1)〜(5)
のいずれかに記載の点眼剤。
(8)金属塩を形成していないサルファ剤が、スルファメトキサゾールまたはスルフイソキサゾールである(1)〜(7)のいずれかに記載の点眼剤。
ニンなどが挙げられる。これらはd体、l体又はdl体のいずれでもよい。
糖アルコール類:例えば、キシリトール、ソルビトール、マンニトールなどが挙げられる。
試験に用いた各実施例及び比較例の調製は、表1−1〜1−3に示す処方に従った。具体的には、実施例1の調製方法を示す。0.1gのエデト酸二ナトリウム、0.5gのクエン酸ナトリウムを350mLの精製水中にて攪拌溶解し、さらに加熱しながらジェランガムを2.0g加え、攪拌溶解した(調製液A)。100gのトロメタモールを500mLの精製水中にて攪拌溶解し、さらに40gのスルファメトキサゾールを攪拌溶解した(調製液B)。調製液Bを調製液Aに加え、さらに精製水を加えて全体を1000mLとした。さらに実施例1に従い、他の実施例及び比較例も調製した。
各実施例及び比較例の調製直後の状態は目視観察により行った。判定は以下の基準で行った。結果を表1−1〜1−3に示した。
×:ゲルと認められる大きな沈殿物が存在する
△:微小な粒子状の沈殿物が存在する
○:沈殿物が全く存在しない
「ドライアイのすべて」(文光堂、1998)、「Ocular Surfaceの診断と治療」(メディカル葵出版、1993)、「点眼剤」(南山堂、1984)等を参考に、表2の組成の人工涙液を調製した。人工涙液にピペットを用いてサンプルを挿入し、1分間その形状を観察した後、その形状を判定し、ゲル化力を評価した。判定を容易にするため、各試験例の点眼剤に成分と相互作用のない色素(青色1号:ブリリアントブルーFCF:和光純薬製)を添加した。結果を表1−2及び1−3に示した。なお、評価基準は下記の通りである。
○:瞬時にゲルを形成し、1分後もゲルの形状に変化が見られなかった
△:瞬時にゲルを形成したものの、1分後、ゲルの形状は保持しなかった
×:ゲルを形成しなかった
Claims (8)
- (a)金属塩を形成していないサルファ剤、(b)ジェランガム、及び(c)トロメタモール、を配合することを特徴とする点眼剤。
- (a)金属塩を形成していないサルファ剤、(b)0.001W/V%以上0.07W/V%以下のジェランガム、及び(c)トロメタモール及び/又はモノエタノールアミン、を配合することを特徴とする点眼剤。
- ジェランガムの配合量が0.07W/V%より大きく1.0W/V%以下である請求項1に記載の点眼剤。
- 0.0001W/V%以上0.9W/V%以下のモノエタノールアミンを更に配合することを特徴とする請求項3に記載の点眼剤。
- pHが7.6以上であることを特徴とする請求項1〜4のいずれか1項に記載の点眼剤。
- トロメタモールの配合量が0.3W/V%以上10W/V%以下である請求項1〜5のいずれか1項に記載の点眼剤。
- トロメタモールの配合量が2W/V%以上10W/V%以下である請求項1〜5のいずれか1項に記載の点眼剤。
- 金属塩を形成していないサルファ剤が、スルファメトキサゾールまたはスルフイソキサゾールである請求項1〜7のいずれか1項に記載の点眼剤。
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Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2020125258A (ja) * | 2019-02-04 | 2020-08-20 | 富士フイルム株式会社 | 組成物、スプレー、ワイパー |
WO2020221839A1 (fr) * | 2019-05-02 | 2020-11-05 | Unither Pharmaceuticals | Composition à base de gomme gellane et de phényléphrine, procédé de fabrication et utilisation comme produit ophtalmique |
JPWO2020090546A1 (ja) * | 2018-10-31 | 2021-09-09 | 富士フイルム株式会社 | 組成物、スプレー、ワイパー |
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JPH08510731A (ja) * | 1993-06-02 | 1996-11-12 | フアーマシア・アクチエボラーグ | 治療使用のためのその場で生成するゲル |
JP2004196787A (ja) * | 2002-12-04 | 2004-07-15 | Santen Pharmaceut Co Ltd | 結膜下デポによるドラッグデリバリーシステム |
JP2005343894A (ja) * | 2004-05-07 | 2005-12-15 | Rohto Pharmaceut Co Ltd | 抗菌点眼剤 |
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2008
- 2008-08-29 JP JP2008220671A patent/JP5304108B2/ja active Active
Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
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JPH08510731A (ja) * | 1993-06-02 | 1996-11-12 | フアーマシア・アクチエボラーグ | 治療使用のためのその場で生成するゲル |
JP2004196787A (ja) * | 2002-12-04 | 2004-07-15 | Santen Pharmaceut Co Ltd | 結膜下デポによるドラッグデリバリーシステム |
JP2005343894A (ja) * | 2004-05-07 | 2005-12-15 | Rohto Pharmaceut Co Ltd | 抗菌点眼剤 |
Cited By (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPWO2020090546A1 (ja) * | 2018-10-31 | 2021-09-09 | 富士フイルム株式会社 | 組成物、スプレー、ワイパー |
JP7168678B2 (ja) | 2018-10-31 | 2022-11-09 | 富士フイルム株式会社 | 組成物、スプレー、ワイパー |
JP2020125258A (ja) * | 2019-02-04 | 2020-08-20 | 富士フイルム株式会社 | 組成物、スプレー、ワイパー |
JP7173888B2 (ja) | 2019-02-04 | 2022-11-16 | 富士フイルム株式会社 | 組成物、スプレー、ワイパー |
WO2020221839A1 (fr) * | 2019-05-02 | 2020-11-05 | Unither Pharmaceuticals | Composition à base de gomme gellane et de phényléphrine, procédé de fabrication et utilisation comme produit ophtalmique |
FR3095592A1 (fr) * | 2019-05-02 | 2020-11-06 | Unither Pharmaceuticals | Composition à base de gomme gellane et de phényléphrine, procédé de fabrication et utilisation comme produit ophtalmique |
CN113939287A (zh) * | 2019-05-02 | 2022-01-14 | 优尼特尔制药公司 | 基于结冷胶和苯肾上腺素的组合物、生产方法以及用作眼科产品的用途 |
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