JP4632687B2 - 点鼻剤 - Google Patents
点鼻剤 Download PDFInfo
- Publication number
- JP4632687B2 JP4632687B2 JP2004127541A JP2004127541A JP4632687B2 JP 4632687 B2 JP4632687 B2 JP 4632687B2 JP 2004127541 A JP2004127541 A JP 2004127541A JP 2004127541 A JP2004127541 A JP 2004127541A JP 4632687 B2 JP4632687 B2 JP 4632687B2
- Authority
- JP
- Japan
- Prior art keywords
- nasal drop
- nasal
- acid
- flunisolide
- salts
- 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 - Lifetime
Links
- 239000007923 nasal drop Substances 0.000 title claims description 59
- 229940100662 nasal drops Drugs 0.000 title description 17
- OSASVXMJTNOKOY-UHFFFAOYSA-N chlorobutanol Chemical compound CC(C)(O)C(Cl)(Cl)Cl OSASVXMJTNOKOY-UHFFFAOYSA-N 0.000 claims description 36
- -1 polyoxyethylene Polymers 0.000 claims description 28
- MIXMJCQRHVAJIO-TZHJZOAOSA-N qk4dys664x Chemical compound O.C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@@H]1[C@@H]2[C@@H]2C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]2(C)C[C@@H]1O.C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@@H]1[C@@H]2[C@@H]2C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]2(C)C[C@@H]1O MIXMJCQRHVAJIO-TZHJZOAOSA-N 0.000 claims description 28
- 229960000676 flunisolide Drugs 0.000 claims description 26
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 claims description 24
- 229940041616 menthol Drugs 0.000 claims description 19
- 150000003839 salts Chemical class 0.000 claims description 19
- GLZPCOQZEFWAFX-UHFFFAOYSA-N Geraniol Chemical compound CC(C)=CCCC(C)=CCO GLZPCOQZEFWAFX-UHFFFAOYSA-N 0.000 claims description 18
- 229960004926 chlorobutanol Drugs 0.000 claims description 18
- DSSYKIVIOFKYAU-XCBNKYQSSA-N (R)-camphor Chemical compound C1C[C@@]2(C)C(=O)C[C@@H]1C2(C)C DSSYKIVIOFKYAU-XCBNKYQSSA-N 0.000 claims description 16
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 16
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims description 16
- 241000723346 Cinnamomum camphora Species 0.000 claims description 13
- 229960000846 camphor Drugs 0.000 claims description 13
- 229930008380 camphor Natural products 0.000 claims description 13
- 239000002562 thickening agent Substances 0.000 claims description 13
- NNJVILVZKWQKPM-UHFFFAOYSA-N Lidocaine Chemical compound CCN(CC)CC(=O)NC1=C(C)C=CC=C1C NNJVILVZKWQKPM-UHFFFAOYSA-N 0.000 claims description 12
- HDSBZMRLPLPFLQ-UHFFFAOYSA-N Propylene glycol alginate Chemical compound OC1C(O)C(OC)OC(C(O)=O)C1OC1C(O)C(O)C(C)C(C(=O)OCC(C)O)O1 HDSBZMRLPLPFLQ-UHFFFAOYSA-N 0.000 claims description 12
- 229960004194 lidocaine Drugs 0.000 claims description 12
- 235000010409 propane-1,2-diol alginate Nutrition 0.000 claims description 11
- 239000000770 propane-1,2-diol alginate Substances 0.000 claims description 11
- DTGKSKDOIYIVQL-WEDXCCLWSA-N (+)-borneol Chemical compound C1C[C@@]2(C)[C@@H](O)C[C@@H]1C2(C)C DTGKSKDOIYIVQL-WEDXCCLWSA-N 0.000 claims description 9
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 9
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 9
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims description 9
- REPVLJRCJUVQFA-UHFFFAOYSA-N (-)-isopinocampheol Natural products C1C(O)C(C)C2C(C)(C)C1C2 REPVLJRCJUVQFA-UHFFFAOYSA-N 0.000 claims description 8
- 239000005792 Geraniol Substances 0.000 claims description 8
- GLZPCOQZEFWAFX-YFHOEESVSA-N Geraniol Natural products CC(C)=CCC\C(C)=C/CO GLZPCOQZEFWAFX-YFHOEESVSA-N 0.000 claims description 8
- 239000002202 Polyethylene glycol Substances 0.000 claims description 8
- CKDOCTFBFTVPSN-UHFFFAOYSA-N borneol Natural products C1CC2(C)C(C)CC1C2(C)C CKDOCTFBFTVPSN-UHFFFAOYSA-N 0.000 claims description 8
- 229940116229 borneol Drugs 0.000 claims description 8
- PUFQVTATUTYEAL-UHFFFAOYSA-N cinchocaine Chemical compound C1=CC=CC2=NC(OCCCC)=CC(C(=O)NCCN(CC)CC)=C21 PUFQVTATUTYEAL-UHFFFAOYSA-N 0.000 claims description 8
- 229960001747 cinchocaine Drugs 0.000 claims description 8
- DTGKSKDOIYIVQL-UHFFFAOYSA-N dl-isoborneol Natural products C1CC2(C)C(O)CC1C2(C)C DTGKSKDOIYIVQL-UHFFFAOYSA-N 0.000 claims description 8
- 229940113087 geraniol Drugs 0.000 claims description 8
- 235000011187 glycerol Nutrition 0.000 claims description 8
- 229920001223 polyethylene glycol Polymers 0.000 claims description 8
- BBEJNBLSSWFDSN-UHFFFAOYSA-N methylamino benzoate Chemical compound CNOC(=O)C1=CC=CC=C1 BBEJNBLSSWFDSN-UHFFFAOYSA-N 0.000 claims description 7
- 238000002360 preparation method Methods 0.000 claims description 7
- REQCZEXYDRLIBE-UHFFFAOYSA-N procainamide Chemical compound CCN(CC)CCNC(=O)C1=CC=C(N)C=C1 REQCZEXYDRLIBE-UHFFFAOYSA-N 0.000 claims description 7
- 229960000244 procainamide Drugs 0.000 claims description 7
- MFDFERRIHVXMIY-UHFFFAOYSA-N procaine Chemical compound CCN(CC)CCOC(=O)C1=CC=C(N)C=C1 MFDFERRIHVXMIY-UHFFFAOYSA-N 0.000 claims description 7
- 229960004919 procaine Drugs 0.000 claims description 7
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims description 6
- 150000002148 esters Chemical class 0.000 claims description 4
- 239000000843 powder Substances 0.000 claims description 4
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 claims description 3
- LNAZSHAWQACDHT-XIYTZBAFSA-N (2r,3r,4s,5r,6s)-4,5-dimethoxy-2-(methoxymethyl)-3-[(2s,3r,4s,5r,6r)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxy-6-[(2r,3r,4s,5r,6r)-4,5,6-trimethoxy-2-(methoxymethyl)oxan-3-yl]oxyoxane Chemical compound CO[C@@H]1[C@@H](OC)[C@H](OC)[C@@H](COC)O[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@H]2[C@@H]([C@@H](OC)[C@H](OC)O[C@@H]2COC)OC)O[C@@H]1COC LNAZSHAWQACDHT-XIYTZBAFSA-N 0.000 claims description 2
- 241000416162 Astragalus gummifer Species 0.000 claims description 2
- 229920000858 Cyclodextrin Polymers 0.000 claims description 2
- 239000001856 Ethyl cellulose Substances 0.000 claims description 2
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 claims description 2
- 229920000084 Gum arabic Polymers 0.000 claims description 2
- 239000004354 Hydroxyethyl cellulose Substances 0.000 claims description 2
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 claims description 2
- 239000004372 Polyvinyl alcohol Substances 0.000 claims description 2
- 229920002125 Sokalan® Polymers 0.000 claims description 2
- 229920001615 Tragacanth Polymers 0.000 claims description 2
- 235000010489 acacia gum Nutrition 0.000 claims description 2
- 239000000205 acacia gum Substances 0.000 claims description 2
- 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 claims description 2
- SNAAJJQQZSMGQD-UHFFFAOYSA-N aluminum magnesium Chemical compound [Mg].[Al] SNAAJJQQZSMGQD-UHFFFAOYSA-N 0.000 claims description 2
- CQFNOACVVKSEOJ-VBQPQCOESA-N bronilide Chemical compound O.C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@@H]1[C@@H]2[C@@H]2C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]2(C)C[C@@H]1O CQFNOACVVKSEOJ-VBQPQCOESA-N 0.000 claims 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 claims description 2
- 150000002170 ethers Chemical class 0.000 claims description 2
- 235000019325 ethyl cellulose Nutrition 0.000 claims description 2
- 229920001249 ethyl cellulose Polymers 0.000 claims description 2
- 229960000442 flunisolide hemihydrate Drugs 0.000 claims description 2
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 claims description 2
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 2
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 2
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 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 claims description 2
- 229920000609 methyl cellulose Polymers 0.000 claims description 2
- 235000010981 methylcellulose Nutrition 0.000 claims description 2
- 239000001923 methylcellulose Substances 0.000 claims description 2
- 229920002451 polyvinyl alcohol Polymers 0.000 claims description 2
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims description 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 2
- 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 claims description 2
- 239000012453 solvate Substances 0.000 claims description 2
- 235000010487 tragacanth Nutrition 0.000 claims description 2
- 239000000196 tragacanth Substances 0.000 claims description 2
- 229940116362 tragacanth Drugs 0.000 claims description 2
- 239000000230 xanthan gum Substances 0.000 claims description 2
- 235000010493 xanthan gum Nutrition 0.000 claims description 2
- 229920001285 xanthan gum Polymers 0.000 claims description 2
- 229940082509 xanthan gum Drugs 0.000 claims 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 claims 1
- 241000978776 Senegalia senegal Species 0.000 claims 1
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 33
- 230000007794 irritation Effects 0.000 description 26
- NOOLISFMXDJSKH-KXUCPTDWSA-N (-)-Menthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@H]1O NOOLISFMXDJSKH-KXUCPTDWSA-N 0.000 description 22
- NBMKJKDGKREAPL-DVTGEIKXSA-N beclomethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(Cl)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O NBMKJKDGKREAPL-DVTGEIKXSA-N 0.000 description 21
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 21
- 229940092705 beclomethasone Drugs 0.000 description 20
- 239000008213 purified water Substances 0.000 description 19
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 15
- 229960004063 propylene glycol Drugs 0.000 description 11
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 10
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 description 10
- 229940068968 polysorbate 80 Drugs 0.000 description 10
- 229920000053 polysorbate 80 Polymers 0.000 description 10
- 239000000872 buffer Substances 0.000 description 9
- 239000003002 pH adjusting agent Substances 0.000 description 9
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 8
- KGBXLFKZBHKPEV-UHFFFAOYSA-N boric acid Chemical compound OB(O)O KGBXLFKZBHKPEV-UHFFFAOYSA-N 0.000 description 8
- XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 description 7
- 239000003795 chemical substances by application Substances 0.000 description 7
- 230000000052 comparative effect Effects 0.000 description 7
- 238000011156 evaluation Methods 0.000 description 7
- 239000000203 mixture Substances 0.000 description 7
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 6
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 6
- 239000004327 boric acid Substances 0.000 description 6
- 235000010338 boric acid Nutrition 0.000 description 6
- 150000001875 compounds Chemical class 0.000 description 6
- 238000002156 mixing Methods 0.000 description 6
- BTBUEUYNUDRHOZ-UHFFFAOYSA-N Borate Chemical compound [O-]B([O-])[O-] BTBUEUYNUDRHOZ-UHFFFAOYSA-N 0.000 description 5
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 5
- 229910019142 PO4 Inorganic materials 0.000 description 5
- 239000000043 antiallergic agent Substances 0.000 description 5
- 235000015165 citric acid Nutrition 0.000 description 5
- 230000000694 effects Effects 0.000 description 5
- 235000021317 phosphate Nutrition 0.000 description 5
- 239000008363 phosphate buffer Substances 0.000 description 5
- 230000003637 steroidlike Effects 0.000 description 5
- 230000000638 stimulation Effects 0.000 description 5
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 5
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 description 4
- 239000002253 acid Substances 0.000 description 4
- 229910000147 aluminium phosphate Inorganic materials 0.000 description 4
- 229960000686 benzalkonium chloride Drugs 0.000 description 4
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 description 4
- 239000004359 castor oil Substances 0.000 description 4
- 235000019438 castor oil Nutrition 0.000 description 4
- XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 description 4
- 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 4
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 4
- 238000000034 method Methods 0.000 description 4
- 210000003928 nasal cavity Anatomy 0.000 description 4
- 210000002850 nasal mucosa Anatomy 0.000 description 4
- 150000003431 steroids Chemical class 0.000 description 4
- FERIUCNNQQJTOY-UHFFFAOYSA-N Butyric acid Chemical compound CCCC(O)=O FERIUCNNQQJTOY-UHFFFAOYSA-N 0.000 description 3
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 3
- 239000006173 Good's buffer Substances 0.000 description 3
- 235000006679 Mentha X verticillata Nutrition 0.000 description 3
- 235000002899 Mentha suaveolens Nutrition 0.000 description 3
- 235000001636 Mentha x rotundifolia Nutrition 0.000 description 3
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 3
- 229910002651 NO3 Inorganic materials 0.000 description 3
- NHNBFGGVMKEFGY-UHFFFAOYSA-N Nitrate Chemical compound [O-][N+]([O-])=O NHNBFGGVMKEFGY-UHFFFAOYSA-N 0.000 description 3
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 description 3
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 description 3
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 description 3
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 description 3
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 description 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 3
- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical compound CCN(CC)CC ZMANZCXQSJIPKH-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
- 229960001950 benzethonium chloride Drugs 0.000 description 3
- 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 3
- 229910021538 borax Inorganic materials 0.000 description 3
- 239000006172 buffering agent Substances 0.000 description 3
- 239000007979 citrate buffer Substances 0.000 description 3
- KWGRBVOPPLSCSI-UHFFFAOYSA-N d-ephedrine Natural products CNC(C)C(O)C1=CC=CC=C1 KWGRBVOPPLSCSI-UHFFFAOYSA-N 0.000 description 3
- 229960000289 fluticasone propionate Drugs 0.000 description 3
- WMWTYOKRWGGJOA-CENSZEJFSA-N fluticasone propionate Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@@H](C)[C@@](C(=O)SCF)(OC(=O)CC)[C@@]2(C)C[C@@H]1O WMWTYOKRWGGJOA-CENSZEJFSA-N 0.000 description 3
- 238000009472 formulation Methods 0.000 description 3
- 239000007788 liquid Substances 0.000 description 3
- 229940097496 nasal spray Drugs 0.000 description 3
- 239000007922 nasal spray Substances 0.000 description 3
- 239000003921 oil Substances 0.000 description 3
- 235000019198 oils Nutrition 0.000 description 3
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 3
- 239000010452 phosphate Substances 0.000 description 3
- 230000035807 sensation Effects 0.000 description 3
- 235000010339 sodium tetraborate Nutrition 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
- JNYAEWCLZODPBN-JGWLITMVSA-N (2r,3r,4s)-2-[(1r)-1,2-dihydroxyethyl]oxolane-3,4-diol Chemical compound OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O JNYAEWCLZODPBN-JGWLITMVSA-N 0.000 description 2
- 239000001306 (7E,9E,11E,13E)-pentadeca-7,9,11,13-tetraen-1-ol Substances 0.000 description 2
- KBPLFHHGFOOTCA-UHFFFAOYSA-N 1-Octanol Chemical compound CCCCCCCCO KBPLFHHGFOOTCA-UHFFFAOYSA-N 0.000 description 2
- MPDGHEJMBKOTSU-YKLVYJNSSA-N 18beta-glycyrrhetic acid Chemical compound C([C@H]1C2=CC(=O)[C@H]34)[C@@](C)(C(O)=O)CC[C@]1(C)CC[C@@]2(C)[C@]4(C)CC[C@@H]1[C@]3(C)CC[C@H](O)C1(C)C MPDGHEJMBKOTSU-YKLVYJNSSA-N 0.000 description 2
- JKMHFZQWWAIEOD-UHFFFAOYSA-N 2-[4-(2-hydroxyethyl)piperazin-1-yl]ethanesulfonic acid Chemical compound OCC[NH+]1CCN(CCS([O-])(=O)=O)CC1 JKMHFZQWWAIEOD-UHFFFAOYSA-N 0.000 description 2
- LVYLCBNXHHHPSB-UHFFFAOYSA-N 2-hydroxyethyl salicylate Chemical compound OCCOC(=O)C1=CC=CC=C1O LVYLCBNXHHHPSB-UHFFFAOYSA-N 0.000 description 2
- SZNYYWIUQFZLLT-UHFFFAOYSA-N 2-methyl-1-(2-methylpropoxy)propane Chemical compound CC(C)COCC(C)C SZNYYWIUQFZLLT-UHFFFAOYSA-N 0.000 description 2
- VUVQBYIJRDUVHT-UHFFFAOYSA-N 3,6-dimethyl-5,6,7,7a-tetrahydro-4h-1-benzofuran-2-one Chemical compound C1C(C)CCC2=C(C)C(=O)OC21 VUVQBYIJRDUVHT-UHFFFAOYSA-N 0.000 description 2
- DVLFYONBTKHTER-UHFFFAOYSA-N 3-(N-morpholino)propanesulfonic acid Chemical compound OS(=O)(=O)CCCN1CCOCC1 DVLFYONBTKHTER-UHFFFAOYSA-N 0.000 description 2
- IYLLULUTZPKQBW-UHFFFAOYSA-N Acrinol Chemical compound CC(O)C(O)=O.C1=C(N)C=CC2=C(N)C3=CC(OCC)=CC=C3N=C21 IYLLULUTZPKQBW-UHFFFAOYSA-N 0.000 description 2
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- 229960003447 pseudoephedrine hydrochloride Drugs 0.000 description 1
- BALXUFOVQVENIU-KXNXZCPBSA-N pseudoephedrine hydrochloride Chemical compound [H+].[Cl-].CN[C@@H](C)[C@@H](O)C1=CC=CC=C1 BALXUFOVQVENIU-KXNXZCPBSA-N 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- USDOQCCMRDNVAH-UHFFFAOYSA-N sigma-cadinene Natural products C1C=C(C)CC2C(C(C)C)CC=C(C)C21 USDOQCCMRDNVAH-UHFFFAOYSA-N 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 description 1
- 239000004299 sodium benzoate Substances 0.000 description 1
- 235000010234 sodium benzoate Nutrition 0.000 description 1
- 235000017557 sodium bicarbonate Nutrition 0.000 description 1
- 229910000030 sodium bicarbonate Inorganic materials 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
- 235000011083 sodium citrates Nutrition 0.000 description 1
- AJPJDKMHJJGVTQ-UHFFFAOYSA-M sodium dihydrogen phosphate Chemical compound [Na+].OP(O)([O-])=O AJPJDKMHJJGVTQ-UHFFFAOYSA-M 0.000 description 1
- 235000011121 sodium hydroxide Nutrition 0.000 description 1
- 239000001540 sodium lactate Substances 0.000 description 1
- 235000011088 sodium lactate Nutrition 0.000 description 1
- 229940005581 sodium lactate Drugs 0.000 description 1
- 235000019721 spearmint oil Nutrition 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 229940086735 succinate Drugs 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 description 1
- 150000003459 sulfonic acid esters Chemical class 0.000 description 1
- 229950001956 suplatast Drugs 0.000 description 1
- 238000002636 symptomatic treatment Methods 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- 229940116411 terpineol Drugs 0.000 description 1
- 229940021790 tetrahydrozoline hydrochloride Drugs 0.000 description 1
- BJORNXNYWNIWEY-UHFFFAOYSA-N tetrahydrozoline hydrochloride Chemical compound Cl.N1CCN=C1C1C2=CC=CC=C2CCC1 BJORNXNYWNIWEY-UHFFFAOYSA-N 0.000 description 1
- 229960000337 tetryzoline Drugs 0.000 description 1
- DSNBHJFQCNUKMA-SCKDECHMSA-N thromboxane A2 Chemical compound OC(=O)CCC\C=C/C[C@@H]1[C@@H](/C=C/[C@@H](O)CCCCC)O[C@@H]2O[C@H]1C2 DSNBHJFQCNUKMA-SCKDECHMSA-N 0.000 description 1
- 229960000790 thymol Drugs 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
- GYDJEQRTZSCIOI-LJGSYFOKSA-N tranexamic acid Chemical compound NC[C@H]1CC[C@H](C(O)=O)CC1 GYDJEQRTZSCIOI-LJGSYFOKSA-N 0.000 description 1
- 229960000401 tranexamic acid Drugs 0.000 description 1
- CRDAMVZIKSXKFV-UHFFFAOYSA-N trans-Farnesol Natural products CC(C)=CCCC(C)=CCCC(C)=CCO CRDAMVZIKSXKFV-UHFFFAOYSA-N 0.000 description 1
- XMLSXPIVAXONDL-UHFFFAOYSA-N trans-jasmone Natural products CCC=CCC1=C(C)CCC1=O XMLSXPIVAXONDL-UHFFFAOYSA-N 0.000 description 1
- 238000011282 treatment Methods 0.000 description 1
- BSVBQGMMJUBVOD-UHFFFAOYSA-N trisodium borate Chemical compound [Na+].[Na+].[Na+].[O-]B([O-])[O-] BSVBQGMMJUBVOD-UHFFFAOYSA-N 0.000 description 1
- HRXKRNGNAMMEHJ-UHFFFAOYSA-K trisodium citrate Chemical compound [Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O HRXKRNGNAMMEHJ-UHFFFAOYSA-K 0.000 description 1
- 229940038773 trisodium citrate Drugs 0.000 description 1
- 229940005605 valeric acid Drugs 0.000 description 1
- 239000005526 vasoconstrictor agent Substances 0.000 description 1
- 239000011576 zinc lactate Substances 0.000 description 1
- 229940050168 zinc lactate Drugs 0.000 description 1
- 235000000193 zinc lactate Nutrition 0.000 description 1
- 239000011787 zinc oxide Substances 0.000 description 1
- 235000014692 zinc oxide Nutrition 0.000 description 1
- NWONKYPBYAMBJT-UHFFFAOYSA-L zinc sulfate Chemical compound [Zn+2].[O-]S([O-])(=O)=O NWONKYPBYAMBJT-UHFFFAOYSA-L 0.000 description 1
- 229960001763 zinc sulfate Drugs 0.000 description 1
- 229910000368 zinc sulfate Inorganic materials 0.000 description 1
- USDOQCCMRDNVAH-KKUMJFAQSA-N β-cadinene Chemical compound C1C=C(C)C[C@H]2[C@H](C(C)C)CC=C(C)[C@@H]21 USDOQCCMRDNVAH-KKUMJFAQSA-N 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Description
ステロイド点鼻剤の刺激を緩和する方法としては、プロピレングリコール、ポリエチレングリコール400およびポリソルベート20を含む刺痛のない経鼻投与に適した水性抗炎症ステロイド製剤(特許文献1:特許第2521291号公報)が開示されているが、メントール、クロロブタノールについては言及していない。
(1)(A)フルニソリド、ベクロメタゾンおよびこれらの誘導体からなる群より選ばれる1種又は2種以上、(B)メントール、カンフル、ボルネオールおよびゲラニオールからなる群より選ばれる1種又は2種以上、および(C)クロロブタノール、リドカイン、ジブカイン、プロカイン、プロカインアミドおよびアミノ安息香酸メチルからなる群より選ばれる1種又は2種以上を含有する点鼻剤。
(2)さらに粘稠化剤を含有する(1)に記載の点鼻剤。
(3)粘稠化剤が、ポリエチレングリコール、グリセリン、ヒドロキシプロピルセルロースまたはアルギン酸プロピレングリコールの少なくとも1種以上である(1)または(2)に記載の点鼻剤。
(4)pHが4.0〜9.0の範囲にある(1)乃至(3)に記載の点鼻剤。
なお、本明細書中、特に言及しない限り、%はw/v%を意味するものとする。
また、本発明に用いるフルニソリド、ベクロメタゾンおよびこれらの誘導体は、水和物などの溶媒和物の形態で使用することもできる。
本発明に用いるフルニソリド、ベクロメタゾンおよびこれらの誘導体のうち、特にフルニソリド、フルニソリド1/2水和物、プロピオン酸ベクロメタゾンが好ましい。
本発明の点鼻剤中におけるメントール、カンフル、ボルネオールおよびゲラニオールの配合量は、各成分の総量として、0.0001〜0.5%が好ましく、0.001〜0.1%がより好ましく、0.003〜0.05%がさらに好ましい。
本発明において、リドカイン、ジブカイン、プロカイン、プロカインアミドおよびアミノ安息香酸メチルは、医薬上、薬理学的に又は生理学的に許容される塩であっても良い。このような塩としては、無機酸塩(例えば、塩酸塩、硫酸塩、硝酸塩、臭化水素酸塩、リン酸塩など)などが例示でき、好ましくは塩酸塩、硫酸塩、硝酸塩であり、特に好ましくは塩酸塩であり、具体的には塩酸リドカイン等が挙げられる。
本発明の点鼻剤中におけるクロロブタノール、リドカイン、ジブカイン、プロカイン、プロカインアミドおよびアミノ安息香酸メチルの配合量は、0.01〜5.0%が好ましく、0.05〜1%がより好ましく、0.1〜0.5%がさらに好ましい。
本発明の点鼻剤中における粘稠化剤の配合量は、0.001〜20%が好ましく、0.005〜18%がより好ましく、0.01〜15%がさらに好ましい。
また、本発明の点鼻剤のpH調整は緩衝剤を用いてもよい。緩衝剤としては、公知のホウ酸緩衝剤、リン酸緩衝剤、炭酸緩衝剤、クエン酸緩衝剤、酢酸緩衝剤、グッド緩衝剤などが挙げられ、好ましくは、グッド緩衝剤、ホウ酸緩衝剤、リン酸緩衝剤、炭酸緩衝剤またはクエン酸緩衝剤、特に好ましくは、グッド緩衝剤、ホウ酸緩衝剤、リン酸緩衝剤またはクエン酸緩衝剤である。「グッド緩衝剤」とは、緩衝能を有する双性イオン構造のアミノエタンスルホン酸誘導体及びアミノプロパンスルホン酸誘導体の総称であり、グッドらにより考案された緩衝剤である。グッド緩衝剤としては、MES、MOPS(3−モルホリノプロパンスルホン酸)、PIPES、HEPES(2−[4−(2−ヒドロキシエチル)−1−ピペラジニル]エタンスルホン酸)、BES、TESなどが挙げられる。ホウ酸緩衝剤としては、ホウ酸、ホウ酸アルカリ金属塩、ホウ酸アルカリ土類金属塩などのホウ酸塩、ホウ酸及びホウ酸塩の組み合わせなどが挙げられる。リン酸緩衝剤としては、リン酸、リン酸アルカリ金属塩、リン酸アルカリ土類金属塩などのリン酸塩、リン酸及びリン酸塩の組み合わせなどが挙げられる。クエン酸緩衝剤としては、クエン酸、クエン酸アルカリ金属塩、クエン酸アルカリ土類金属塩などのクエン酸塩、クエン酸及びクエン酸塩の組み合わせなどが挙げられる。また、ホウ酸緩衝剤、リン酸緩衝剤又はクエン酸緩衝剤として、ホウ酸塩、リン酸塩又はクエン酸塩の水和物を用いてもよい。より具体的には、ホウ酸又はその塩(ホウ酸ナトリウム、テトラホウ酸カリウム、メタホウ酸カリウムなど)、リン酸又はその塩(リン酸水素ナトリウム、リン酸二水素ナトリウム、リン酸二水素カリウムなど)、炭酸又はその塩(炭酸水素ナトリウム、炭酸ナトリウムなど)、クエン酸またはその塩(クエン酸一ナトリウム、クエン酸三ナトリウムなど)などが挙げられる。
フルニソリド1/2水和物 0.0255g
l−メントール 0.03g
クロロブタノール 0.2g
ポリエチレングリコール 10g
塩化ベンザルコニウム 0.01g
プロピレングリコール 20g
ポリソルベート80 0.2g
pH調製剤 適量
精製水 適量
100ml
上記の各成分を秤量し適当量の精製水に溶解し、pHを5.5に調整した後、点鼻容器に充填して点鼻剤を得た。
フルニソリド 0.02g
l−メントール 0.02g
クロロブタノール 0.3g
リドカイン 0.1g
グリセリン 5g
塩化ベンザルコニウム 0.01g
プロピレングリコール 10g
ポリソルベート80 0.1g
pH調製剤 適量
精製水 適量
100ml
上記の各成分を秤量し適当量の精製水に溶解し、pHを5.5に調整した後、点鼻容器に充填して点鼻剤を得た。
フルニソリド 0.0125g
l−メントール 0.01g
クロロブタノール 0.1g
アルギン酸プロピレングリコール 0.1g
塩酸ナファゾリン 0.05g
塩化ベンゼトニウム 0.01g
プロピレングリコール 15g
ポリソルベート80 0.1g
pH調製剤 適量
精製水 適量
100ml
上記の各成分を秤量し適当量の精製水に溶解し、pHを5.5に調整した後、点鼻容器に充填して点鼻剤を得た。
フルニソリド 0.0125g
d−カンフル 0.01g
塩酸ジブカイン 0.5g
アルギン酸プロピレングリコール 0.1g
塩酸テトラヒドロゾリン 0.05g
塩化セチルピリジニウム 0.025g
プロピレングリコール 15g
ポリソルベート80 0.1g
pH調製剤 適量
精製水 適量
100ml
上記の各成分を秤量し適当量の精製水に溶解し、pHを5.5に調整した後、点鼻容器に充填して点鼻剤を得た。
フルニソリド 0.0125g
d−ボルネオール 0.03g
塩酸プロカイン 0.5g
アルギン酸プロピレングリコール 0.1g
塩酸シュードエフェドリン 0.03g
アクリノール 0.05g
プロピレングリコール 15g
ポリソルベート80 0.1g
pH調製剤 適量
精製水 適量
100ml
上記の各成分を秤量し適当量の精製水に溶解し、pHを5.5に調整した後、点鼻容器に充填して点鼻剤を得た。
プロピオン酸ベクロメタゾン 0.05g
プロピオン酸フルチカゾン 0.026g
l−メントール 0.03g
クロロブタノール 0.2g
ヒドロキシプロピルセルロース 0.1g
塩化ベンザルコニウム 0.01g
プロピレングリコール 10g
ポリソルベート80 0.1g
pH調製剤 適量
精製水 適量
100ml
上記の各成分を秤量し適当量の精製水に溶解し、pHを6.0に調整した後、点鼻容器に充填して点鼻剤を得た。
フルニソリド 0.0063g
プロピオン酸フルチカゾン 0.013g
dl−カンフル 0.01g
塩酸リドカイン 0.3g
ヒドロキシプロピルセルロース 0.1g
塩化ベンザルコニウム 0.01g
プロピレングリコール 10g
ポリソルベート80 0.1g
pH調製剤 適量
精製水 適量
100ml
上記の各成分を秤量し適当量の精製水に溶解し、pHを6.0に調整した後、点鼻容器に充填して点鼻剤を得た。
プロピオン酸ベクロメタゾン 0.1g
l−メントール 0.01g
クロロブタノール 0.1g
アルギン酸プロピレングリコール 0.1g
塩化ベンゼトニウム 0.01g
プロピレングリコール 8g
ポリソルベート80 0.2g
pH調製剤 適量
精製水 適量
100ml
上記の各成分を秤量し適当量の精製水に溶解し、pHを6.0に調整した後、点鼻容器に充填して点鼻剤を得た。
プロピオン酸ベクロメタゾン 0.1g
dl−カンフル 0.01g
リドカイン 0.5g
アルギン酸プロピレングリコール 0.1g
塩化ベンゼトニウム 0.01g
プロピレングリコール 8g
ポリソルベート80 0.2g
pH調製剤 適量
精製水 適量
100ml
上記の各成分を秤量し適当量の精製水に溶解し、pHを6.0に調整した後、点鼻容器に充填して点鼻剤を得た。
表1に記載の処方に従い、各成分を精製水に溶解しpH調整後、全量を100mLとし、点鼻スプレー容器に充填し点鼻剤を調製した。これを6人のパネラーに1回100μlを点鼻し、点鼻直後に感じる刺激感を評価した。評価は下記4段階評価基準に従って採点してもらい、その平均値をスコアとして算出した。
3:非常に痛い、2:痛い、1:わずかに痛い、0:痛みがない
結果を表1に示す。
したがって、ステロイド化合物は単独では使用感に問題があり、メントールの単独配合ではより刺激を増大させるなど、非ステロイド性抗アレルギー剤とは異なる挙動を示すことが明らかになった。
実施例10に各種粘稠化剤を配合した場合の刺激感について、さらに評価を行った。表2に記載の処方に従い、試験例1と同様に点鼻剤を調製し、これを6人のパネラーに1回100μlを点鼻し、試験例1と同様の基準にて評価した。さらに刺激の持続する時間についても測定し、6人の平均値を平均持続時間として算出した。結果を表2に示す。
表3に記載の処方に従い、試験例1と同様に点鼻剤を調製し、これを6人のパネラーに1回100μlを点鼻し、試験例1と同様の基準にて評価した。
また、刺激の持続する時間についても測定し、6人の平均値を平均持続時間として算出した。
結果を表3に示す。
また、プロピオン酸ベクロメタゾンには独特のにおいがあるが、メントール、カンフルを配合することで、製剤のにおいについても改善することができた。
さらに、ポリエチレングリコール、グリセリン、ヒドロキシプロピルセルロース、アルギン酸プロピレングリコールなどの粘稠化剤を配合することにより、より使用感の良い点鼻剤が得られることが確認された。
Claims (9)
- (A)フルニソリド、そのエステル誘導体及びエーテル誘導体、それらの溶媒和物、並びにそれらの塩からなる群より選ばれる1種又は2種以上、
(B)メントール、カンフル、ボルネオールおよびゲラニオールからなる群より選ばれる1種又は2種以上、および
(C)クロロブタノール、リドカイン、ジブカイン、プロカイン、プロカインアミド、アミノ安息香酸メチル及びそれらの塩からなる群より選ばれる1種又は2種以上
を含有する点鼻剤。 - (A)成分として、フルニソリド、フルニソリド1/2水和物、及びそれらの塩からなる群より選ばれる1種又は2種以上を含む、請求項1に記載の点鼻剤。
- 点鼻剤中において、(A)成分を総量で0.001〜0.05%含有する、請求項1又は2に記載の点鼻剤。
- 点鼻剤中において、(B)成分を総量で0.0001〜0.5%含有する、請求項1〜3のいずれかに記載の点鼻剤。
- 点鼻剤中において、(C)成分を総量で0.01〜5.0%含有する、請求項1〜4のいずれかに記載の点鼻剤。
- pHが4.0〜9.0である、請求項1〜5のいずれかに記載の点鼻剤。
- さらに粘稠化剤を含有する請求項1〜6のいずれか記載の点鼻剤。
- 粘稠化剤として、ポリエチレングリコール、ポリオキシエチレングリコール、ポリビニルアルコール、ポリビニルピロリドン、カルボキシビニルポリマー、ヒドロキシエチルセルロース、ヒドロキシプロピルセルロース、メチルセルロース、エチルセルロース、ヒドロキシプロピルメチルセルロース、アルギン酸プロピレングリコール、アラビアゴム末、カルメロースナトリウム、キサンタンガム、グリセリン、ケイ酸マグネシウムアルミニウム、コンドロイチン硫酸ナトリウム、シクロデキストリン、及びトラガント末からなる群より選ばれる少なくとも1種以上を含む、請求項7に記載の点鼻剤。
- 点鼻剤中において、粘稠化剤を総量で0.001〜20%含有する、請求項7又は8に記載の点鼻剤。
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JP2004127541A JP4632687B2 (ja) | 2003-04-25 | 2004-04-23 | 点鼻剤 |
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JP2004127541A JP4632687B2 (ja) | 2003-04-25 | 2004-04-23 | 点鼻剤 |
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JP2010208416A Division JP5238779B2 (ja) | 2003-04-25 | 2010-09-16 | 点鼻剤 |
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CN104027542A (zh) * | 2014-06-27 | 2014-09-10 | 陈建福 | 一种用于鼻腔疾病的搽剂 |
Families Citing this family (6)
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JP2005097221A (ja) * | 2003-09-26 | 2005-04-14 | Sato Pharmaceutical Co Ltd | 点鼻薬 |
JP2006248960A (ja) * | 2005-03-10 | 2006-09-21 | Rohto Pharmaceut Co Ltd | 水性外用組成物 |
WO2007072923A1 (ja) * | 2005-12-22 | 2007-06-28 | Kowa Company, Ltd. | ステロイドの経時的安定性が改善された外用製剤 |
JP5252846B2 (ja) * | 2007-07-06 | 2013-07-31 | ロート製薬株式会社 | 水性医薬組成物 |
JP6279337B2 (ja) * | 2013-02-04 | 2018-02-14 | ロート製薬株式会社 | 点鼻用組成物 |
CN105188758A (zh) * | 2013-03-15 | 2015-12-23 | 梅迪奇斯医药公司 | 氟尼缩松的局部组合物及治疗方法 |
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JPS51144719A (en) * | 1975-05-27 | 1976-12-13 | Syntex Inc | Preparation of crystalline frunisolide and ittcontaining composition |
JPS63101318A (ja) * | 1986-10-16 | 1988-05-06 | Toko Yakuhin Kogyo Kk | 点鼻剤 |
JPH04235923A (ja) * | 1991-01-16 | 1992-08-25 | Kyowa Hakko Kogyo Co Ltd | 経鼻投与用製剤 |
JP2521291B2 (ja) * | 1986-05-22 | 1996-08-07 | シンテックス・ファーマシューティカルズ・インターナショナル・リミテッド | 経鼻投与用水性ステロイド製剤 |
JPH0952826A (ja) * | 1995-08-10 | 1997-02-25 | Showa Yakuhin Kako Kk | 消炎点眼剤 |
WO2000016771A1 (fr) * | 1998-09-24 | 2000-03-30 | Fujisawa Pharmaceutical Co., Ltd. | Preparations liquides a usage externe contenant du cromoglycate de sodium et traitement ou prevention des symptomes allergiques oculaires |
JP2002205942A (ja) * | 2000-11-07 | 2002-07-23 | Taisho Pharmaceut Co Ltd | 局所適用組成物 |
JP2002241278A (ja) * | 1998-09-24 | 2002-08-28 | Fujisawa Pharmaceut Co Ltd | クロモグリク酸ナトリウムを含有する洗眼液及び点鼻液 |
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JPS51144719A (en) * | 1975-05-27 | 1976-12-13 | Syntex Inc | Preparation of crystalline frunisolide and ittcontaining composition |
JP2521291B2 (ja) * | 1986-05-22 | 1996-08-07 | シンテックス・ファーマシューティカルズ・インターナショナル・リミテッド | 経鼻投与用水性ステロイド製剤 |
JPS63101318A (ja) * | 1986-10-16 | 1988-05-06 | Toko Yakuhin Kogyo Kk | 点鼻剤 |
JPH04235923A (ja) * | 1991-01-16 | 1992-08-25 | Kyowa Hakko Kogyo Co Ltd | 経鼻投与用製剤 |
JPH0952826A (ja) * | 1995-08-10 | 1997-02-25 | Showa Yakuhin Kako Kk | 消炎点眼剤 |
WO2000016771A1 (fr) * | 1998-09-24 | 2000-03-30 | Fujisawa Pharmaceutical Co., Ltd. | Preparations liquides a usage externe contenant du cromoglycate de sodium et traitement ou prevention des symptomes allergiques oculaires |
JP2002241278A (ja) * | 1998-09-24 | 2002-08-28 | Fujisawa Pharmaceut Co Ltd | クロモグリク酸ナトリウムを含有する洗眼液及び点鼻液 |
JP2002205942A (ja) * | 2000-11-07 | 2002-07-23 | Taisho Pharmaceut Co Ltd | 局所適用組成物 |
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Publication number | Priority date | Publication date | Assignee | Title |
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CN104027542A (zh) * | 2014-06-27 | 2014-09-10 | 陈建福 | 一种用于鼻腔疾病的搽剂 |
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