SK7084Y1 - Eye drops containing broad-spectrum antibiotics and local glucocorticoid - Google Patents
Eye drops containing broad-spectrum antibiotics and local glucocorticoid Download PDFInfo
- Publication number
- SK7084Y1 SK7084Y1 SK50088-2014U SK500882014U SK7084Y1 SK 7084 Y1 SK7084 Y1 SK 7084Y1 SK 500882014 U SK500882014 U SK 500882014U SK 7084 Y1 SK7084 Y1 SK 7084Y1
- Authority
- SK
- Slovakia
- Prior art keywords
- sodium
- acid
- adjusting
- preparation according
- ophthalmic preparation
- Prior art date
Links
- 239000003862 glucocorticoid Substances 0.000 title claims abstract description 7
- 239000003889 eye drop Substances 0.000 title description 6
- 229940012356 eye drops Drugs 0.000 title description 2
- 239000003242 anti bacterial agent Substances 0.000 title 1
- 229940088710 antibiotic agent Drugs 0.000 title 1
- UREBDLICKHMUKA-CXSFZGCWSA-N dexamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-CXSFZGCWSA-N 0.000 claims abstract description 16
- 229960003957 dexamethasone Drugs 0.000 claims abstract description 14
- 238000002360 preparation method Methods 0.000 claims abstract description 11
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical group O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 8
- 230000003115 biocidal effect Effects 0.000 claims abstract description 7
- 239000008215 water for injection Substances 0.000 claims abstract description 7
- KIUKXJAPPMFGSW-DNGZLQJQSA-N (2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5S,6R)-3-Acetamido-2-[(2S,3S,4R,5R,6R)-6-[(2R,3R,4R,5S,6R)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 KIUKXJAPPMFGSW-DNGZLQJQSA-N 0.000 claims abstract description 6
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims abstract description 6
- 229920002674 hyaluronan Polymers 0.000 claims abstract description 6
- 229960003160 hyaluronic acid Drugs 0.000 claims abstract description 6
- SUIQUYDRLGGZOL-RCWTXCDDSA-N levofloxacin hemihydrate Chemical compound O.C([C@@H](N1C2=C(C(C(C(O)=O)=C1)=O)C=C1F)C)OC2=C1N1CCN(C)CC1.C([C@@H](N1C2=C(C(C(C(O)=O)=C1)=O)C=C1F)C)OC2=C1N1CCN(C)CC1 SUIQUYDRLGGZOL-RCWTXCDDSA-N 0.000 claims abstract description 6
- 150000003839 salts Chemical class 0.000 claims abstract description 4
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims abstract description 3
- 150000003013 phosphoric acid derivatives Chemical class 0.000 claims abstract description 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims description 21
- 239000000203 mixture Substances 0.000 claims description 13
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims description 10
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 9
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 9
- GSDSWSVVBLHKDQ-JTQLQIEISA-N Levofloxacin Chemical compound C([C@@H](N1C2=C(C(C(C(O)=O)=C1)=O)C=C1F)C)OC2=C1N1CCN(C)CC1 GSDSWSVVBLHKDQ-JTQLQIEISA-N 0.000 claims description 6
- 229960003376 levofloxacin Drugs 0.000 claims description 6
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 5
- 239000011780 sodium chloride Substances 0.000 claims description 5
- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 claims description 4
- WCUXLLCKKVVCTQ-UHFFFAOYSA-M Potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 claims description 4
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims description 4
- BNIILDVGGAEEIG-UHFFFAOYSA-L disodium hydrogen phosphate Chemical compound [Na+].[Na+].OP([O-])([O-])=O BNIILDVGGAEEIG-UHFFFAOYSA-L 0.000 claims description 4
- 229910000403 monosodium phosphate Inorganic materials 0.000 claims description 4
- 235000019799 monosodium phosphate Nutrition 0.000 claims description 4
- AJPJDKMHJJGVTQ-UHFFFAOYSA-M sodium dihydrogen phosphate Chemical compound [Na+].OP(O)([O-])=O AJPJDKMHJJGVTQ-UHFFFAOYSA-M 0.000 claims description 4
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 3
- 239000004372 Polyvinyl alcohol Substances 0.000 claims description 3
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims description 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 3
- 229920002451 polyvinyl alcohol Polymers 0.000 claims description 3
- HELHAJAZNSDZJO-OLXYHTOASA-L sodium L-tartrate Chemical compound [Na+].[Na+].[O-]C(=O)[C@H](O)[C@@H](O)C([O-])=O HELHAJAZNSDZJO-OLXYHTOASA-L 0.000 claims description 3
- 239000001509 sodium citrate Substances 0.000 claims description 3
- 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 claims description 3
- 239000001433 sodium tartrate Substances 0.000 claims description 3
- 229960002167 sodium tartrate Drugs 0.000 claims description 3
- 235000011004 sodium tartrates Nutrition 0.000 claims description 3
- 239000000600 sorbitol Substances 0.000 claims description 3
- 239000011975 tartaric acid Substances 0.000 claims description 3
- 235000002906 tartaric acid Nutrition 0.000 claims description 3
- NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 claims description 2
- UXVMQQNJUSDDNG-UHFFFAOYSA-L Calcium chloride Chemical compound [Cl-].[Cl-].[Ca+2] UXVMQQNJUSDDNG-UHFFFAOYSA-L 0.000 claims description 2
- 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 claims description 2
- 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 claims description 2
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims description 2
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims description 2
- 229930195725 Mannitol Natural products 0.000 claims description 2
- VMHLLURERBWHNL-UHFFFAOYSA-M Sodium acetate Chemical compound [Na+].CC([O-])=O VMHLLURERBWHNL-UHFFFAOYSA-M 0.000 claims description 2
- 229920002125 Sokalan® Polymers 0.000 claims description 2
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims description 2
- 229930006000 Sucrose Natural products 0.000 claims description 2
- 229930003427 Vitamin E Natural products 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
- 239000003963 antioxidant agent Substances 0.000 claims description 2
- 235000006708 antioxidants Nutrition 0.000 claims 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 claims description 2
- KGBXLFKZBHKPEV-UHFFFAOYSA-N boric acid Chemical compound OB(O)O KGBXLFKZBHKPEV-UHFFFAOYSA-N 0.000 claims description 2
- 239000004327 boric acid Substances 0.000 claims description 2
- 239000001110 calcium chloride Substances 0.000 claims description 2
- 229910001628 calcium chloride Inorganic materials 0.000 claims description 2
- 229960001631 carbomer Drugs 0.000 claims description 2
- 235000015165 citric acid Nutrition 0.000 claims description 2
- 229910000397 disodium phosphate Inorganic materials 0.000 claims description 2
- 235000019800 disodium phosphate Nutrition 0.000 claims description 2
- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 claims description 2
- 239000008103 glucose Substances 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
- 235000010979 hydroxypropyl methyl cellulose Nutrition 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
- 239000000594 mannitol Substances 0.000 claims description 2
- 235000010355 mannitol Nutrition 0.000 claims description 2
- 239000001103 potassium chloride Substances 0.000 claims description 2
- 235000011164 potassium chloride Nutrition 0.000 claims description 2
- 239000001632 sodium acetate Substances 0.000 claims description 2
- 235000017281 sodium acetate Nutrition 0.000 claims description 2
- 235000011083 sodium citrates Nutrition 0.000 claims description 2
- AKHNMLFCWUSKQB-UHFFFAOYSA-L sodium thiosulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=S AKHNMLFCWUSKQB-UHFFFAOYSA-L 0.000 claims description 2
- 235000019345 sodium thiosulphate Nutrition 0.000 claims description 2
- 239000005720 sucrose Substances 0.000 claims description 2
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 claims description 2
- 229960000281 trometamol Drugs 0.000 claims description 2
- 235000019165 vitamin E Nutrition 0.000 claims description 2
- 229940046009 vitamin E Drugs 0.000 claims description 2
- 239000011709 vitamin E Substances 0.000 claims description 2
- 239000004133 Sodium thiosulphate Substances 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 229910021538 borax Inorganic materials 0.000 claims 1
- 235000010338 boric acid Nutrition 0.000 claims 1
- UQGFMSUEHSUPRD-UHFFFAOYSA-N disodium;3,7-dioxido-2,4,6,8,9-pentaoxa-1,3,5,7-tetraborabicyclo[3.3.1]nonane Chemical compound [Na+].[Na+].O1B([O-])OB2OB([O-])OB1O2 UQGFMSUEHSUPRD-UHFFFAOYSA-N 0.000 claims 1
- 229940098201 hyaluronic acid 1 mg Drugs 0.000 claims 1
- 239000004328 sodium tetraborate Substances 0.000 claims 1
- 235000010339 sodium tetraborate Nutrition 0.000 claims 1
- 239000000126 substance Substances 0.000 abstract description 5
- 239000000243 solution Substances 0.000 description 11
- 239000004480 active ingredient Substances 0.000 description 6
- 239000003755 preservative agent Substances 0.000 description 6
- 230000002335 preservative effect Effects 0.000 description 6
- 238000009472 formulation Methods 0.000 description 4
- 238000004519 manufacturing process Methods 0.000 description 4
- 229920002385 Sodium hyaluronate Polymers 0.000 description 3
- 229940010747 sodium hyaluronate Drugs 0.000 description 3
- 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 3
- PDFKFLNYRFAWOA-UHFFFAOYSA-N 1-fluoroquinolin-2-one Chemical class C1=CC=C2C=CC(=O)N(F)C2=C1 PDFKFLNYRFAWOA-UHFFFAOYSA-N 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 238000004090 dissolution Methods 0.000 description 2
- 210000003560 epithelium corneal Anatomy 0.000 description 2
- 229940068984 polyvinyl alcohol Drugs 0.000 description 2
- 208000035143 Bacterial infection Diseases 0.000 description 1
- 206010020751 Hypersensitivity Diseases 0.000 description 1
- 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 1
- 108010044349 Maxitrol Proteins 0.000 description 1
- SBKRTALNRRAOJP-BWSIXKJUSA-N N-[(2S)-4-amino-1-[[(2S,3R)-1-[[(2S)-4-amino-1-oxo-1-[[(3S,6S,9S,12S,15R,18R,21S)-6,9,18-tris(2-aminoethyl)-15-benzyl-3-[(1R)-1-hydroxyethyl]-12-(2-methylpropyl)-2,5,8,11,14,17,20-heptaoxo-1,4,7,10,13,16,19-heptazacyclotricos-21-yl]amino]butan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxobutan-2-yl]-6-methylheptanamide (6S)-N-[(2S)-4-amino-1-[[(2S,3R)-1-[[(2S)-4-amino-1-oxo-1-[[(3S,6S,9S,12S,15R,18R,21S)-6,9,18-tris(2-aminoethyl)-15-benzyl-3-[(1R)-1-hydroxyethyl]-12-(2-methylpropyl)-2,5,8,11,14,17,20-heptaoxo-1,4,7,10,13,16,19-heptazacyclotricos-21-yl]amino]butan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxobutan-2-yl]-6-methyloctanamide sulfuric acid Polymers OS(O)(=O)=O.CC(C)CCCCC(=O)N[C@@H](CCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCN)C(=O)N[C@H]1CCNC(=O)[C@@H](NC(=O)[C@H](CCN)NC(=O)[C@H](CCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCN)NC1=O)[C@@H](C)O.CC[C@H](C)CCCCC(=O)N[C@@H](CCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCN)C(=O)N[C@H]1CCNC(=O)[C@@H](NC(=O)[C@H](CCN)NC(=O)[C@H](CCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCN)NC1=O)[C@@H](C)O SBKRTALNRRAOJP-BWSIXKJUSA-N 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 1
- 230000002411 adverse Effects 0.000 description 1
- 230000007815 allergy Effects 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 208000022362 bacterial infectious disease Diseases 0.000 description 1
- 229960000686 benzalkonium chloride Drugs 0.000 description 1
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 description 1
- 239000002738 chelating agent Substances 0.000 description 1
- WIIZWVCIJKGZOK-RKDXNWHRSA-N chloramphenicol Chemical compound ClC(Cl)C(=O)N[C@H](CO)[C@H](O)C1=CC=C([N+]([O-])=O)C=C1 WIIZWVCIJKGZOK-RKDXNWHRSA-N 0.000 description 1
- 239000003246 corticosteroid Substances 0.000 description 1
- 229960002344 dexamethasone sodium phosphate Drugs 0.000 description 1
- PLCQGRYPOISRTQ-FCJDYXGNSA-L dexamethasone sodium phosphate Chemical compound [Na+].[Na+].C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)COP([O-])([O-])=O)(O)[C@@]1(C)C[C@@H]2O PLCQGRYPOISRTQ-FCJDYXGNSA-L 0.000 description 1
- 238000001914 filtration Methods 0.000 description 1
- PGBHMTALBVVCIT-VCIWKGPPSA-N framycetin Chemical compound N[C@@H]1[C@@H](O)[C@H](O)[C@H](CN)O[C@@H]1O[C@H]1[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](N)C[C@@H](N)[C@@H]2O)O[C@@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CN)O2)N)O[C@@H]1CO PGBHMTALBVVCIT-VCIWKGPPSA-N 0.000 description 1
- ZWCXYZRRTRDGQE-SORVKSEFSA-N gramicidina Chemical compound C1=CC=C2C(C[C@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CC=3C4=CC=CC=C4NC=3)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CC=3C4=CC=CC=C4NC=3)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CC=3C4=CC=CC=C4NC=3)NC(=O)[C@H](C(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](C(C)C)NC(=O)[C@H](C)NC(=O)[C@H](NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC=O)C(C)C)CC(C)C)C(=O)NCCO)=CNC2=C1 ZWCXYZRRTRDGQE-SORVKSEFSA-N 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 229940029062 maxitrol Drugs 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- 230000003204 osmotic effect Effects 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- HFPGULMERUXXDW-UHFFFAOYSA-M sodium;2-carboxybenzenesulfonate Chemical compound [Na+].OS(=O)(=O)C1=CC=CC=C1C([O-])=O HFPGULMERUXXDW-UHFFFAOYSA-M 0.000 description 1
- 229910021653 sulphate ion Inorganic materials 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 238000011200 topical administration Methods 0.000 description 1
- LEAHFJQFYSDGGP-UHFFFAOYSA-K trisodium;dihydrogen phosphate;hydrogen phosphate Chemical compound [Na+].[Na+].[Na+].OP(O)([O-])=O.OP([O-])([O-])=O LEAHFJQFYSDGGP-UHFFFAOYSA-K 0.000 description 1
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
Description
Riešenie sa týka očnej instilácie na báze kombinácie flurochinolónového derivátu (širokospektrálneho antibiotika) s glukokortikoidom, s prídavkom viskoelastickej látky bez prítomnosti konzervačnej látky.The invention relates to an eye instillation based on the combination of a fluroquinolone derivative (broad spectrum antibiotic) with a glucocorticoid, with the addition of a viscoelastic agent in the absence of a preservative.
Doterajší stav technikyBACKGROUND OF THE INVENTION
Doteraz sa v oftalmologii používajú viaceré kombinované preparáty na báze širokospektrálneho antibiotika a lokálneho glukokortikoidu, ako sú Spersadex comp. (účinné látky: dexamethasoni natrii phosphas, chloramphenicolum), Maxitrol (účinné látky: dexamethasonum, neomycini sulfas, polymyxini-B sulfas), Sofŕadex (účinné látky: dexamethasoni natrii sulfobenzoas, framycetini sulfas, gramicidinum), Tobradex (účinné látky: dexamethasonum, tobramycinum).To date, several combination preparations based on a broad-spectrum antibiotic and a local glucocorticoid, such as Spersadex comp. (active ingredients: dexamethasone sodium phosphate, chloramphenicolum), Maxitrol (active ingredients: dexamethasone, neomycin sulphate, polymyxin-B sulphate), Sofàadex (active ingredients: dexamethasone sodium sulphobenzoate, framycetini sulphate, gramicidinum), dumradex (active ingredients) ).
GR1007745B1, ktorý opisuje očné farmaceutické kompozície na topické podávanie s kombináciou účinných látok ako levofloxacín a dexametazón. Kombinovaný prostriedok obsahuje benzalkonium chlorid ako konzervačné činidlo, ktoré spôsobuje rôzne typy alergií pri dlhodobom používaní.GR1007745B1, which describes ophthalmic pharmaceutical compositions for topical administration with a combination of active ingredients such as levofloxacin and dexamethasone. The combination formulation contains benzalkonium chloride as a preservative, causing various types of allergies in long-term use.
Cieľom tohto technického riešenia je pripraviť očnú instiláciu s obsahom kombinácie účinných látok levofloxacínu a dexametazónu, ktorá by bola dostatočne stabilná aj bez prítomnosti konzervačného činidla a poskytla pritom väčší komfort a lepšiu znášanlivosť bez negatívneho porušenia rohovkového epitelu.The object of the present invention is to provide an ophthalmic instillation comprising a combination of the active ingredients levofloxacin and dexamethasone, which is sufficiently stable even in the absence of a preservative and provides greater comfort and better tolerability without negatively affecting the corneal epithelium.
Podstata technického riešeniaThe essence of the technical solution
Ponuka doterajších známych oftalmologických prípravkov na báze širokospektrálneho antibiotika a lokálneho glukokortikoidu sa rozšíri o prípravok podľa tohto technického riešenia, ktorého podstata spočíva v tom, že obsahuje 0,1 až 2 % hmotn. levofloxacínu (flurochinolónový derivát) alebo jeho farmaceutický prijateľnej soli alebo derivátu a 0,01 až 1% hmotn. dexametazónu (glukokortikoid), prípadne jeho fosfátovú soľ s kyselinou fosforečnou, ďalej 0,01 až 3 % hmotn. pomocných látok udržujúcich viskozitu roztoku a zvyšok do 100 % hmotn. tvorí voda na injekciu.The range of prior art ophthalmic preparations based on a broad-spectrum antibiotic and a local glucocorticoid is expanded to include the preparation according to the invention, which consists in that it contains 0.1 to 2 wt. % levofloxacin (fluroquinolone derivative) or a pharmaceutically acceptable salt or derivative thereof; % dexamethasone (glucocorticoid), or its phosphate salt with phosphoric acid, further 0.01 to 3 wt. % of auxiliary substances to maintain solution viscosity and the remainder to 100 wt. forms water for injection.
Predmetom tohto technického riešenia je formulácia s obsahom levofloxacínu a dexametazónu s prídavkom vysokoelastickej látky zvyšujúcej predĺžený účinok a bez prítomnosti konzervačnej látky pre lepšiu znášanlivosť.The object of the present invention is a formulation comprising levofloxacin and dexamethasone with the addition of a high-elastic agent for prolonged action and in the absence of a preservative for better compatibility.
Ďalšími farmaceutickými pomocnými látkami môžu byť látky zo skupiny anorganických a organických pufračných látok (upravujúce pH roztoku) 0,01 až 3 % hmotn., anorganické a organické soli, látky upravujúce osmolalitu roztoku 0,01 až 3 % hmotn., chelatačné činidlá, antioxidanty (vitamín E a tiosíran sodný) 0,01 až 3 % hmotn. a zmesi uvedených látok.Other pharmaceutical auxiliaries may be substances from the group of inorganic and organic buffer substances (adjusting the pH of the solution) 0.01 to 3% by weight, inorganic and organic salts, substances adjusting the osmolality of the solution 0.01 to 3% by weight, chelating agents, antioxidants % (vitamin E and sodium thiosulfate) 0.01 to 3 wt. and mixtures thereof.
Pomocné látky na úpravu viskozity sú sodná soľ karmelózy, hydroxypropylmetylcelulóza, polyvinyl alkohol, karbomér alebo kyselina hyalurónová jednotlivo alebo v zmesi.Viscosity-adjusting aids are carmellose sodium, hydroxypropylmethylcellulose, polyvinyl alcohol, carbomer or hyaluronic acid individually or in admixture.
Pomocnými látkami udržujúcimi pH prostredie v rozmedzí 6 až 8 sú kyselina boritá, tertaboritan sodný, octan sodný, hydrogénfosforečnan sodný, dihydrogénfosforečnan sodný, citrát sodný, kyselina citrónová, kyselina vínna, vínan sodný, trometamol, kyselina sírová, kyselina chlorovodíková, hydroxid sodný jednotlivo alebo v zmesi.Excipients which maintain the pH range of 6-8 are boric acid, sodium tertaborate, sodium acetate, sodium hydrogen phosphate, sodium dihydrogen phosphate, sodium citrate, citric acid, tartaric acid, sodium tartrate, trometamol, sulfuric acid, hydrochloric acid, sodium hydroxide individually or in the mixture.
Pomocné látky na úpravu osmotickeho tlaku sú chlorid sodný, chlorid draselný, chlorid vápenatý, sorbitol, manitol, glycerol, glukóza a sacharóza jednotlivo alebo v zmesi.The excipients for adjusting the osmotic pressure are sodium chloride, potassium chloride, calcium chloride, sorbitol, mannitol, glycerol, glucose and sucrose individually or in a mixture.
Indikáciou kombinovaného prípravku s obsahom kortikosteroidu a antibiotika sú zápalové procesy štruktúr oka, kde sa vyžaduje protizápalový účinok spolu so súčasným potlačením vzniku (resp. vzniku rizika) sekundárnej bakteriálnej infekcie. Výhodou očných kvapiek podľa predmetného riešenia je zároveň dobrá účinnosť a znášanlivosť formulácie, ktorá sa dosahuje tým, že neobsahuje konzervačné činidlo, pri dostatočnej stabilite prostriedku.Combined corticosteroid / antibiotic preparations are indicated by inflammatory processes in the structures of the eye where an anti-inflammatory effect is required together with a concomitant suppression (or risk) of secondary bacterial infection. The advantage of the eye drops of the present invention is also good effectiveness and tolerability of the formulation, which is achieved by not containing a preservative, with sufficient stability of the formulation.
Príklady uskutočneniaEXAMPLES
Príklad 1Example 1
Zloženie očnej instilácie: Levofloxacín hemihydrát Dexametazón s.Ph.Composition of eye instillation: Levofloxacin hemihydrate Dexamethasone s.Ph.
Chlorid sodnýSodium chloride
Hydrogénfosforečnan disodný Dihydrogénfosforečnan sodnýDisodium hydrogen phosphate Sodium dihydrogen phosphate
5,12 mg (0,5 %) mg/ml (0,1 %) mg/ml (0,8 %)5.12 mg (0.5%) mg / ml (0.1%) mg / ml (0.8%)
0,474 mg/ml (0,05 %)0.474 mg / ml (0.05%)
0,460 mg/ml (0,05 %)0.460 mg / ml (0.05%)
SK 7084 Υ1SK 7084 Υ1
Kyselina hyalurónová HCL/NaOHHyaluronic acid HCL / NaOH
Voda na injekciu mg/ml (0,1 %)Water for injection mg / ml (0.1%)
q.s. pH = 7 lmlqs pH = 7 ml
Príklad 2Example 2
Zloženie očnej instilácie: Levofloxacín hemihydrát Dexametazon s.Ph.Composition of eye instillation: Levofloxacin hemihydrate Dexamethasone s.Ph.
Sorbitolsorbitol
Kyselina citrónováCitric acid
Citrát sodnýSodium citrate
Kyselina hyalurónová HCL/NaOHHyaluronic acid HCL / NaOH
Voda na injekciuWater for injections
5,12 mg (0,5 %) mg/ml (0,1 %) mg/ml (0,8 %)5.12 mg (0.5%) mg / ml (0.1%) mg / ml (0.8%)
0,474 mg/ml (0,05 %)0.474 mg / ml (0.05%)
0,460 mg/ml (0,05 %) mg/ml (0,1 %) q.s. pH = 7,1 lml0.460 mg / ml (0.05%) mg / ml (0.1%) q.s. pH = 7.1 lml
Príklad 3Example 3
Zloženie očnej instilácie: Levofloxacín hemihydrát Dexametazon s.Ph.Composition of eye instillation: Levofloxacin hemihydrate Dexamethasone s.Ph.
Glycerolglycerol
Kyselina vínnaTartaric acid
Vínan sodnýSodium tartrate
Kyselina hyalurónová Polyvinyl alkohol HCL/NaOHHyaluronic acid Polyvinyl alcohol HCL / NaOH
Voda na injekciuWater for injections
5,12 mg (0,5 %) mg/ml (0,1 %) mg/ml (0,8 %)5.12 mg (0.5%) mg / ml (0.1%) mg / ml (0.8%)
0,474 mg/ml (0,05 %)0.474 mg / ml (0.05%)
0,460 mg/ml (0,05 %)0.460 mg / ml (0.05%)
0,9 mg/ml (0,1 %) 1 mg/ml (0,1 %) q.s. pH = 7 lml0.9 mg / ml (0.1%) 1 mg / ml (0.1%) q.s. pH = 7 ml
Všetky pripravené kompozície boli dostatočne stabilné aj bez prítomnosti konzervačného činidla a poskytovali pritom väčší komfort pre používateľa a prejavila sa lepšia znášanlivosť bez negatívneho vplyvu na rohovkový epitel.All prepared compositions were sufficiently stable even in the absence of a preservative, providing greater comfort to the user, and improved tolerability without adversely affecting the corneal epithelium.
Príklad 4Example 4
Výroba roztoku hyaluronátu sodného:Production of sodium hyaluronate solution:
Odvážené množstvo zložiek (chlorid sodný, hydrogénfosforečnan disodný, dihydrogénfosforečnan sodný, hydroxid sodný) podľa veľkosti výrobnej šarže sa za aseptických podmienok rozpustia v injekčnej vode. Po rozpustení sa pridá množstvo hyaluronátu sodného odpovedajúce výrobnej šarži. Po rozpustení sa roztok sterilizuje pri 121 °C 20 minút. Skontroluje sa pH roztoku pri teplote 25 °C (7,0 - 7,1).The weighed amount of the components (sodium chloride, disodium hydrogen phosphate, sodium dihydrogen phosphate, sodium hydroxide) according to the size of the production batch is dissolved under aseptic conditions in injection water. After dissolution, an amount of sodium hyaluronate corresponding to the production batch is added. After dissolution, the solution is sterilized at 121 ° C for 20 minutes. Check the pH of the solution at 25 ° C (7.0 - 7.1).
Výroba roztoku levofloxacínu a dexametazónu:Production of levofloxacin and dexamethasone solution:
Odvážené množstvo zložiek (levofloxacín hemihydrát, Dexametazon s.Ph.) sa rozpustia v roztoku, ktorý sa sterilizuje filtráciou cez membránový filter s veľkosťou pórov 0,2 pm a za aseptických podmienok sa pridá k roztoku hyaluronátu sodného. Výsledný roztok upraví na požadovaný objem v súlade s veľkosťou šarže.A weighed amount of the components (levofloxacin hemihydrate, Dexamethasone s.Ph.) is dissolved in a solution which is sterilized by filtration through a 0.2 µm membrane filter and added to a solution of sodium hyaluronate under aseptic conditions. The resulting solution is adjusted to the desired volume in accordance with the batch size.
NÁROKY NA OCHRANUPROTECTION REQUIREMENTS
Claims (6)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SK50088-2014U SK7084Y1 (en) | 2014-06-30 | 2014-06-30 | Eye drops containing broad-spectrum antibiotics and local glucocorticoid |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SK50088-2014U SK7084Y1 (en) | 2014-06-30 | 2014-06-30 | Eye drops containing broad-spectrum antibiotics and local glucocorticoid |
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| Publication Number | Publication Date |
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| SK500882014U1 SK500882014U1 (en) | 2014-11-04 |
| SK7084Y1 true SK7084Y1 (en) | 2015-04-01 |
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