TR201402298A2 - Ophthalmic pharmaceutical compositions. - Google Patents
Ophthalmic pharmaceutical compositions. Download PDFInfo
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- TR201402298A2 TR201402298A2 TR2014/02298A TR201402298A TR201402298A2 TR 201402298 A2 TR201402298 A2 TR 201402298A2 TR 2014/02298 A TR2014/02298 A TR 2014/02298A TR 201402298 A TR201402298 A TR 201402298A TR 201402298 A2 TR201402298 A2 TR 201402298A2
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- pharmaceutical composition
- feature
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- acid
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- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 32
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 claims abstract description 13
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims abstract description 13
- 238000001356 surgical procedure Methods 0.000 claims abstract description 12
- 208000002177 Cataract Diseases 0.000 claims abstract description 11
- 230000003110 anti-inflammatory effect Effects 0.000 claims abstract description 8
- 230000003637 steroidlike Effects 0.000 claims abstract description 8
- 206010061218 Inflammation Diseases 0.000 claims abstract description 7
- 230000004054 inflammatory process Effects 0.000 claims abstract description 7
- 208000001344 Macular Edema Diseases 0.000 claims abstract description 6
- 206010025415 Macular oedema Diseases 0.000 claims abstract description 6
- 239000013543 active substance Substances 0.000 claims abstract description 6
- 201000010230 macular retinal edema Diseases 0.000 claims abstract description 6
- 230000002980 postoperative effect Effects 0.000 claims abstract description 6
- 206010015958 Eye pain Diseases 0.000 claims abstract description 5
- 208000004550 Postoperative Pain Diseases 0.000 claims abstract description 5
- 206010012601 diabetes mellitus Diseases 0.000 claims abstract description 5
- 230000000069 prophylactic effect Effects 0.000 claims abstract description 5
- 230000001225 therapeutic effect Effects 0.000 claims abstract description 5
- 239000000203 mixture Substances 0.000 claims description 23
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims description 21
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims description 20
- QEFAQIPZVLVERP-UHFFFAOYSA-N nepafenac Chemical compound NC(=O)CC1=CC=CC(C(=O)C=2C=CC=CC=2)=C1N QEFAQIPZVLVERP-UHFFFAOYSA-N 0.000 claims description 20
- 229960001002 nepafenac Drugs 0.000 claims description 19
- 239000003795 chemical substances by application Substances 0.000 claims description 17
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 17
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 claims description 16
- 235000002639 sodium chloride Nutrition 0.000 claims description 16
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 14
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 14
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 14
- 229960000686 benzalkonium chloride Drugs 0.000 claims description 10
- 239000011780 sodium chloride Substances 0.000 claims description 10
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 claims description 9
- 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 8
- 229930195725 Mannitol Natural products 0.000 claims description 8
- 239000003889 eye drop Substances 0.000 claims description 8
- 235000010355 mannitol Nutrition 0.000 claims description 8
- 239000000594 mannitol Substances 0.000 claims description 8
- 239000003755 preservative agent Substances 0.000 claims description 8
- 239000004094 surface-active agent Substances 0.000 claims description 8
- 239000003109 Disodium ethylene diamine tetraacetate Substances 0.000 claims description 7
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 7
- -1 alkyl sulfonate esters Chemical class 0.000 claims description 7
- 239000002738 chelating agent Substances 0.000 claims description 7
- 235000019301 disodium ethylene diamine tetraacetate Nutrition 0.000 claims description 7
- 229960001484 edetic acid Drugs 0.000 claims description 7
- 238000009472 formulation Methods 0.000 claims description 7
- 229920000136 polysorbate Polymers 0.000 claims description 7
- 229950008882 polysorbate Drugs 0.000 claims description 7
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims description 6
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 6
- KGBXLFKZBHKPEV-UHFFFAOYSA-N boric acid Chemical compound OB(O)O KGBXLFKZBHKPEV-UHFFFAOYSA-N 0.000 claims description 6
- 239000004327 boric acid Substances 0.000 claims description 6
- 235000010338 boric acid Nutrition 0.000 claims description 6
- 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 claims description 6
- 239000003002 pH adjusting agent Substances 0.000 claims description 6
- 230000002335 preservative effect Effects 0.000 claims description 6
- 150000003839 salts Chemical class 0.000 claims description 6
- 239000002904 solvent Substances 0.000 claims description 6
- 239000012929 tonicity agent Substances 0.000 claims description 6
- 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 claims description 5
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 claims description 4
- WRMNZCZEMHIOCP-UHFFFAOYSA-N 2-phenylethanol Chemical compound OCCC1=CC=CC=C1 WRMNZCZEMHIOCP-UHFFFAOYSA-N 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 4
- 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 4
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims description 4
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 4
- DLRVVLDZNNYCBX-UHFFFAOYSA-N Polydextrose Polymers OC1C(O)C(O)C(CO)OC1OCC1C(O)C(O)C(O)C(O)O1 DLRVVLDZNNYCBX-UHFFFAOYSA-N 0.000 claims description 4
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims description 4
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims description 4
- OSASVXMJTNOKOY-UHFFFAOYSA-N chlorobutanol Chemical compound CC(C)(O)C(Cl)(Cl)Cl OSASVXMJTNOKOY-UHFFFAOYSA-N 0.000 claims description 4
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 4
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 4
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 4
- FGIUAXJPYTZDNR-UHFFFAOYSA-N potassium nitrate Chemical compound [K+].[O-][N+]([O-])=O FGIUAXJPYTZDNR-UHFFFAOYSA-N 0.000 claims description 4
- 239000008213 purified water Substances 0.000 claims description 4
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 claims description 4
- CDBYLPFSWZWCQE-UHFFFAOYSA-L sodium carbonate Substances [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 claims description 4
- 239000000600 sorbitol Substances 0.000 claims description 4
- 235000010356 sorbitol Nutrition 0.000 claims description 4
- 239000004480 active ingredient Substances 0.000 claims description 3
- 239000007864 aqueous solution Substances 0.000 claims description 3
- 229960001259 diclofenac Drugs 0.000 claims description 3
- DCOPUUMXTXDBNB-UHFFFAOYSA-N diclofenac Chemical compound OC(=O)CC1=CC=CC=C1NC1=C(Cl)C=CC=C1Cl DCOPUUMXTXDBNB-UHFFFAOYSA-N 0.000 claims description 3
- 239000012153 distilled water Substances 0.000 claims description 3
- 229960002390 flurbiprofen Drugs 0.000 claims description 3
- SYTBZMRGLBWNTM-UHFFFAOYSA-N flurbiprofen Chemical compound FC1=CC(C(C(O)=O)C)=CC=C1C1=CC=CC=C1 SYTBZMRGLBWNTM-UHFFFAOYSA-N 0.000 claims description 3
- 235000011187 glycerol Nutrition 0.000 claims description 3
- 229960000905 indomethacin Drugs 0.000 claims description 3
- 229960004752 ketorolac Drugs 0.000 claims description 3
- OZWKMVRBQXNZKK-UHFFFAOYSA-N ketorolac Chemical compound OC(=O)C1CCN2C1=CC=C2C(=O)C1=CC=CC=C1 OZWKMVRBQXNZKK-UHFFFAOYSA-N 0.000 claims description 3
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 claims description 3
- JNYAEWCLZODPBN-KVTDHHQDSA-N (2r,3r,4r)-2-[(1r)-1,2-dihydroxyethyl]oxolane-3,4-diol Chemical class OC[C@@H](O)[C@H]1OC[C@@H](O)[C@H]1O JNYAEWCLZODPBN-KVTDHHQDSA-N 0.000 claims description 2
- 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
- NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 claims description 2
- 239000005711 Benzoic acid Substances 0.000 claims description 2
- CXRFDZFCGOPDTD-UHFFFAOYSA-M Cetrimide Chemical compound [Br-].CCCCCCCCCCCCCC[N+](C)(C)C CXRFDZFCGOPDTD-UHFFFAOYSA-M 0.000 claims description 2
- NVTRPRFAWJGJAJ-UHFFFAOYSA-L EDTA monocalcium salt Chemical compound [Ca+2].OC(=O)CN(CC([O-])=O)CCN(CC(O)=O)CC([O-])=O NVTRPRFAWJGJAJ-UHFFFAOYSA-L 0.000 claims description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 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
- 108010010803 Gelatin Proteins 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
- 229920002907 Guar gum Polymers 0.000 claims description 2
- 239000004354 Hydroxyethyl cellulose Substances 0.000 claims description 2
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 claims description 2
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 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 claims description 2
- 240000007472 Leucaena leucocephala Species 0.000 claims description 2
- 235000010643 Leucaena leucocephala Nutrition 0.000 claims description 2
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 2
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims description 2
- 229920001100 Polydextrose Polymers 0.000 claims description 2
- 239000004372 Polyvinyl alcohol Substances 0.000 claims description 2
- TVQZAMVBTVNYLA-UHFFFAOYSA-N Pranoprofen Chemical compound C1=CC=C2CC3=CC(C(C(O)=O)C)=CC=C3OC2=N1 TVQZAMVBTVNYLA-UHFFFAOYSA-N 0.000 claims description 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 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
- 235000010443 alginic acid Nutrition 0.000 claims description 2
- 239000000783 alginic acid Substances 0.000 claims description 2
- 229920000615 alginic acid Polymers 0.000 claims description 2
- 229960001126 alginic acid Drugs 0.000 claims description 2
- 150000004781 alginic acids Chemical class 0.000 claims description 2
- 229940101006 anhydrous sodium sulfite Drugs 0.000 claims description 2
- BYFMCKSPFYVMOU-UHFFFAOYSA-N bendazac Chemical compound C12=CC=CC=C2C(OCC(=O)O)=NN1CC1=CC=CC=C1 BYFMCKSPFYVMOU-UHFFFAOYSA-N 0.000 claims description 2
- 229960005149 bendazac Drugs 0.000 claims description 2
- 229960003872 benzethonium Drugs 0.000 claims 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 claims description 2
- KHSLHYAUZSPBIU-UHFFFAOYSA-M benzododecinium bromide Chemical compound [Br-].CCCCCCCCCCCC[N+](C)(C)CC1=CC=CC=C1 KHSLHYAUZSPBIU-UHFFFAOYSA-M 0.000 claims description 2
- 229940073464 benzododecinium bromide Drugs 0.000 claims description 2
- 235000010233 benzoic acid Nutrition 0.000 claims description 2
- 229960004365 benzoic acid Drugs 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
- 229960002645 boric acid Drugs 0.000 claims description 2
- 229960001631 carbomer Drugs 0.000 claims description 2
- 150000001735 carboxylic acids Chemical class 0.000 claims description 2
- 235000010418 carrageenan Nutrition 0.000 claims description 2
- 239000000679 carrageenan Substances 0.000 claims description 2
- 229920001525 carrageenan Polymers 0.000 claims description 2
- 229940113118 carrageenan Drugs 0.000 claims description 2
- 229960001927 cetylpyridinium chloride Drugs 0.000 claims description 2
- 229960004926 chlorobutanol Drugs 0.000 claims description 2
- 229940075614 colloidal silicon dioxide Drugs 0.000 claims description 2
- BEFDCLMNVWHSGT-UHFFFAOYSA-N ethenylcyclopentane Chemical compound C=CC1CCCC1 BEFDCLMNVWHSGT-UHFFFAOYSA-N 0.000 claims description 2
- 235000019325 ethyl cellulose Nutrition 0.000 claims description 2
- 229920001249 ethyl cellulose Polymers 0.000 claims description 2
- 239000008273 gelatin Substances 0.000 claims description 2
- 229920000159 gelatin Polymers 0.000 claims description 2
- 235000019322 gelatine Nutrition 0.000 claims description 2
- 235000011852 gelatine desserts Nutrition 0.000 claims description 2
- 239000008103 glucose Substances 0.000 claims description 2
- 235000001727 glucose Nutrition 0.000 claims description 2
- 229940075507 glyceryl monostearate Drugs 0.000 claims description 2
- 239000000665 guar gum Substances 0.000 claims description 2
- 235000010417 guar gum Nutrition 0.000 claims description 2
- 229960002154 guar gum Drugs 0.000 claims description 2
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 claims description 2
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 claims description 2
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 2
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims description 2
- 235000010445 lecithin Nutrition 0.000 claims description 2
- 239000000787 lecithin Substances 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
- 229960002900 methylcellulose Drugs 0.000 claims description 2
- 239000001788 mono and diglycerides of fatty acids Substances 0.000 claims description 2
- 229960000649 oxyphenbutazone Drugs 0.000 claims description 2
- 229940067107 phenylethyl alcohol Drugs 0.000 claims description 2
- 239000002504 physiological saline solution Substances 0.000 claims description 2
- 229960002702 piroxicam Drugs 0.000 claims description 2
- QYSPLQLAKJAUJT-UHFFFAOYSA-N piroxicam Chemical compound OC=1C2=CC=CC=C2S(=O)(=O)N(C)C=1C(=O)NC1=CC=CC=N1 QYSPLQLAKJAUJT-UHFFFAOYSA-N 0.000 claims description 2
- 239000001259 polydextrose Substances 0.000 claims description 2
- 235000013856 polydextrose Nutrition 0.000 claims description 2
- 229940035035 polydextrose Drugs 0.000 claims description 2
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims description 2
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 claims description 2
- 229920002451 polyvinyl alcohol Polymers 0.000 claims description 2
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims description 2
- 239000004323 potassium nitrate Substances 0.000 claims description 2
- 235000010333 potassium nitrate Nutrition 0.000 claims description 2
- 229940069328 povidone Drugs 0.000 claims description 2
- 229960003101 pranoprofen Drugs 0.000 claims description 2
- 238000002360 preparation method Methods 0.000 claims description 2
- 125000001453 quaternary ammonium group Chemical group 0.000 claims description 2
- 229960004889 salicylic acid Drugs 0.000 claims description 2
- 239000011734 sodium Substances 0.000 claims description 2
- 229910052708 sodium Inorganic materials 0.000 claims description 2
- WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 claims description 2
- 239000004299 sodium benzoate Substances 0.000 claims description 2
- 235000010234 sodium benzoate Nutrition 0.000 claims description 2
- 229910000029 sodium carbonate Inorganic materials 0.000 claims description 2
- 229940046303 sodium cetostearyl sulfate Drugs 0.000 claims description 2
- 239000001509 sodium citrate Substances 0.000 claims description 2
- 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 2
- 239000004290 sodium methyl p-hydroxybenzoate Substances 0.000 claims description 2
- 235000010268 sodium methyl p-hydroxybenzoate Nutrition 0.000 claims description 2
- 239000004404 sodium propyl p-hydroxybenzoate Substances 0.000 claims description 2
- 235000010230 sodium propyl p-hydroxybenzoate Nutrition 0.000 claims description 2
- GEHJYWRUCIMESM-UHFFFAOYSA-L sodium sulfite Chemical compound [Na+].[Na+].[O-]S([O-])=O GEHJYWRUCIMESM-UHFFFAOYSA-L 0.000 claims description 2
- PESXGULMKCKJCC-UHFFFAOYSA-M sodium;4-methoxycarbonylphenolate Chemical compound [Na+].COC(=O)C1=CC=C([O-])C=C1 PESXGULMKCKJCC-UHFFFAOYSA-M 0.000 claims description 2
- IXMINYBUNCWGER-UHFFFAOYSA-M sodium;4-propoxycarbonylphenolate Chemical compound [Na+].CCCOC(=O)C1=CC=C([O-])C=C1 IXMINYBUNCWGER-UHFFFAOYSA-M 0.000 claims description 2
- CLBALUNQCMWJSU-UHFFFAOYSA-L sodium;hexadecyl sulfate;octadecyl sulfate Chemical compound [Na+].CCCCCCCCCCCCCCCCOS([O-])(=O)=O.CCCCCCCCCCCCCCCCCCOS([O-])(=O)=O CLBALUNQCMWJSU-UHFFFAOYSA-L 0.000 claims description 2
- UPUIQOIQVMNQAP-UHFFFAOYSA-M sodium;tetradecyl sulfate Chemical compound [Na+].CCCCCCCCCCCCCCOS([O-])(=O)=O UPUIQOIQVMNQAP-UHFFFAOYSA-M 0.000 claims description 2
- 239000004334 sorbic acid Substances 0.000 claims description 2
- 235000010199 sorbic acid Nutrition 0.000 claims description 2
- 229940075582 sorbic acid Drugs 0.000 claims description 2
- 229960002920 sorbitol Drugs 0.000 claims description 2
- 239000005720 sucrose Substances 0.000 claims description 2
- 229960004793 sucrose Drugs 0.000 claims description 2
- 239000008215 water for injection Substances 0.000 claims description 2
- 229920001285 xanthan gum Polymers 0.000 claims description 2
- XOOUIPVCVHRTMJ-UHFFFAOYSA-L zinc stearate Chemical class [Zn+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O XOOUIPVCVHRTMJ-UHFFFAOYSA-L 0.000 claims description 2
- UHVMMEOXYDMDKI-JKYCWFKZSA-L zinc;1-(5-cyanopyridin-2-yl)-3-[(1s,2s)-2-(6-fluoro-2-hydroxy-3-propanoylphenyl)cyclopropyl]urea;diacetate Chemical compound [Zn+2].CC([O-])=O.CC([O-])=O.CCC(=O)C1=CC=C(F)C([C@H]2[C@H](C2)NC(=O)NC=2N=CC(=CC=2)C#N)=C1O UHVMMEOXYDMDKI-JKYCWFKZSA-L 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 6
- QBYMCVQZZZQPHE-UHFFFAOYSA-N 2-[2-[bis(carboxymethyl)amino]ethyl-(carboxymethyl)amino]acetic acid;calcium Chemical compound [Ca].OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O QBYMCVQZZZQPHE-UHFFFAOYSA-N 0.000 claims 1
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical class C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 1
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims 1
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- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 description 1
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- 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
- NFCRBQADEGXVDL-UHFFFAOYSA-M cetylpyridinium chloride monohydrate Chemical compound O.[Cl-].CCCCCCCCCCCCCCCC[N+]1=CC=CC=C1 NFCRBQADEGXVDL-UHFFFAOYSA-M 0.000 description 1
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Landscapes
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Mevcut buluş, oküler ağrı, katarakt cerrahisi ile ilişkili postoperatif ağrı ve inflamasyonun profilaktik ve/veya semptomatik ve/veya terapötik tedavisinde; diyabetik hastalarda katarakt cerrahisi ile ilişkili postoperatif maküler ödem riskinin azaltılmasında kullanılmak üzere steroid yapılı olmayan antiinflamatuvar (NSAID) özellikteki uygun etken maddeyi ve/veya farmasötik olarak kabul edilebilir türevlerini içeren farmasötik bileşim/ler ile ilgilidir.The present invention relates to prophylactic and / or symptomatic and / or therapeutic treatment of ocular pain, postoperative pain and inflammation associated with cataract surgery; The present invention relates to pharmaceutical composition (s) containing suitable non-steroidal anti-inflammatory (NSAID) active agent and / or pharmaceutically acceptable derivatives thereof for use in reducing the risk of postoperative macular edema associated with cataract surgery in diabetic patients.
Description
TARIFNAME OFTALMIK FARMASÖTIK BILESIMLER BULUSUN ILGILI OLDUGU ALAN Mevcut bulus, oküler agri, katarakt cerrahisi ile iliskili postoperatif agri ve inflamasyonun profilaktik ve/veya semptoinatik ve/veya terapötik tedavisinde; diyabetik hastalarda katarakt cerrahisi ile iliskili postoperatif maküler ödem riskinin azaltilmasinda kullanilmak üzere steroid yapili olmayan antiinflamatuvar (NSAID) özellikteki uygun etken maddeyi ve/veya farmasötik olarak kabul edilebilir türevlerini içeren farmasötik bilesim/ler ile Mevcut bulus; steroid yapili olmayan antiintlamatuvar (NSAID) özellikteki etken maddenin Nepafenak, 2-(2-Amino-3-benzoilfenil) asetamit (Formül 1) ve/veya farmasötik olarak kabul edilebilir türevleri oldugu ve uygun farmasötik formlarda etken madde olarak kullanildigi farmasötik bilesimler ile ilgilidir. DESCRIPTION OPHTHALMIC PHARMACEUTICAL COMPOSITIONS FIELD OF THE INVENTION The present invention is related to ocular pain, postoperative pain and inflammation associated with cataract surgery. prophylactic and/or symptomatic and/or therapeutic treatment; in diabetic patients To be used to reduce the risk of postoperative macular edema associated with cataract surgery Appropriate active substance with non-steroidal anti-inflammatory (NSAID) properties, such as and/or pharmaceutical composition(s) containing pharmaceutically acceptable derivatives The present invention; non-steroidal anti-inflammatory (NSAID) agent Nepafenac, 2-(2-Amino-3-benzoylphenyl) acetamide (Formula 1) and/or pharmaceutical as an active ingredient in suitable pharmaceutical forms. relates to the pharmaceutical compositions in which it is used.
Formül 1: Ayrica bulus, Nepafenak ve/veya farmasötik olarak kabul edilebilir türevlerini içeren farmasötik bilesimlerin oftalmik uygulama için uygun olan formülasyonlarmi ve profilaktik, semptomatik veya terapötik kullaniinlarini da kapsamaktadir. ÖNCEKI TEKNIK (TEKNIGIN BILINEN DURUMU) NSAID'ler, oküler yanginin kontrol altina alinmasinda siklikla kullanilmaktadir. Bu ajanlarin, alerjik konjunktivitis semptomlarinin hafifletilmesi, intra-operatif miyozisiii önlenmesi, pre ve post-operatif Oküler yangi ve katarakt cerrahisi ile iliskili cystoid macular ödemin tedavisi ve refraktif cerrahi sonrasinda sekillenebilecek agrinin azaltilmasi gibi birçok kullanim alani vardir. Formula 1: In addition, the invention includes Nepafenac and/or its pharmaceutically acceptable derivatives. formulations of pharmaceutical compositions suitable for ophthalmic administration, and includes prophylactic, symptomatic or therapeutic uses. PRIOR ART (KNOWN STATE OF THE ART) NSAIDs are frequently used to control ocular inflammation. This agents, alleviation of symptoms of allergic conjunctivitis, intra-operative miosisiii Cystoid associated with prevention, pre- and post-operative ocular inflammation and cataract surgery Treatment of macular edema and reduction of pain that may occur after refractive surgery It has many uses such as
NSAlD'lerin steroid tedavisinden kaynaklanan potansiyel komplikasyonlardan sakinmak için özellikle kuru göz sendromu (KGS) gibi kronik yangisal göz hastaliklarinin tedavisinde kortikosteroidlere alternatif olarak kullanilmasi önerilmektedir (Lekhanont K, Park CY, Smith JA, et al. Effects of T0pical Anti-inflainniatory Agents in a Botulinuni Toxin B-Induced bromfeiiak, diklofenak, flurbiprofen, indometazin, ketorolak, nepafenak ve suprofen gibi ajanlar Slkllkla kullanilmaktadir (Schalnus R. Topical Nonsteroidal Aiiti-Inflammatory Therapy in Nepafenak oküler agri, katarakt cerrahisi ile iliskili postoperatif agri ve intlamasyonun önlenmesi ve tedavi edilmesi. diyabetik hastalarda katarakt cerrahisi ile iliskili postoperatif maküler ödem riskinin azaltilmasinda kullanilan steroid yapili olmayan antiinflamatuvar (NSAID) topikal bir ön ilaçtir. Ön ilaç özelligine sahip ilk oftalmik NSAID4tir. Avoid potential complications from steroid therapy of NSAlDs especially for chronic inflammatory eye diseases such as dry eye syndrome (KGS) It is recommended to be used as an alternative to corticosteroids in the treatment of Park CY, Smith JA, et al. Effects of T0pical Anti-inflainniatory Agents in a Botulinuni Toxin B-Induced such as brompheiac, diclofenac, flurbiprofen, indomethacin, ketorolac, nepafenac, and suprofen agents are used frequently (Schalnus R. Topical Nonsteroidal Drug-Inflammatory Therapy in Nepafenac ocular pain, postoperative pain and inflammation associated with cataract surgery prevention and treatment. Postoperative associated with cataract surgery in diabetic patients Non-steroidal anti-inflammatory drug used to reduce the risk of macular edema (NSAID) is a topical prodrug. It is the first ophthalmic NSAID4 with prodrug properties.
Nepafenakin ön ilaç seklindeki yapisi, bir yandan korneaya hizli penetrasyonuna ve hedef bölgelere dagilima olanak tanirken, diger yandan yüzeyde akümülasyonu ve oküler yüzey komplikasyonlarini azaltir. içeren oftalmik bilesimlerden bahsedilmektedir. Nepafenacine's prodrug form allows, on the one hand, its rapid penetration into the cornea and targeted while allowing distribution to regions, on the other hand, surface accumulation and ocular surface reduces complications. ophthalmic compositions containing
BULUSUN AÇIKLAMASI Mevcut bulus, oküler agri, katarakt cerrahisi ile iliskili postoperatif agri ve inflamasyonun profilaktik ve/veya semptomatik ve/veya terapötik tedavisinde; diyabetik hastalarda katarakt cerrahisi ile iliskili postoperatif maküler ödem riskinin azaltilmasinda kullanilmak üzere steroid yapili olmayan antiintlamatuvar (NSAID) özellikteki uygun etken maddeyi ve/veya farmasötik olarak kabul edilebilir türevlerini içeren farmasötik bilesim/ler ile Mevcut bulusun bir diger yönü; oftalrnik kullanilmak üzere steroid yapili olmayan antiinflamatuvar (NSAID) özellikteki uygun etken maddeyi ve/veya farmasötik olarak kabul edilebilir türevlerini ve farmasötik olarak kabul edilebilir yardimci maddeleri içeren farmasötik bilesimler ile ilgilidir. DESCRIPTION OF THE INVENTION The present invention is related to ocular pain, postoperative pain and inflammation associated with cataract surgery. prophylactic and/or symptomatic and/or therapeutic treatment; in diabetic patients To be used to reduce the risk of postoperative macular edema associated with cataract surgery Appropriate active substance with non-steroidal anti-inflammatory (NSAID) properties, such as and/or pharmaceutical composition(s) containing pharmaceutically acceptable derivatives Another aspect of the present invention is; non-steroidal for ophthalmological use Appropriate anti-inflammatory (NSAID) active substance and/or pharmaceutical containing acceptable derivatives and pharmaceutically acceptable excipients. relates to pharmaceutical compositions.
Bulusta steroid yapili olmayan antiintlamatuvar (NSAID) özellikteki uygun etken madde bunlarla sinirli olmamakla birlikte, bromfenak, nepafenak, pranoprofen, salisilik asit, bendazak, piroksikam, ketorolak, flurbiprofen, diklofenak, oksifenbütazon, indometasin ve/veya farmasötik olarak kabul edilebilir türevlerinin arasindan tercihen Nepafenak olarak seçilir. In the invention, suitable active substance with non-steroidal anti-inflammatory (NSAID) properties including but not limited to bromfenac, nepafenac, pranoprofen, salicylic acid, bendazac, piroxicam, ketorolac, flurbiprofen, diclofenac, oxyphenbutazone, indomethacin and/or pharmaceutically acceptable derivatives, preferably Nepafenac. is selected.
Bulusta “farmasötik olarak kabul edilebilir türevleri” terimi ile farmasötik olarak kabul edilebilir uygun tuzlar, esterler, solvatlar, hidratlar, kompleksler, polimorflar, enantiyomerler, önilaçlar, asit adisyon tuzlari, analoglar, izomerler, rasematlar, amidler, enantiyomer tuzlari, bazik tuzlar, konjugeler, tautoinerler, anhidratlar, anhidritler, bazlar, asitler, eterler, kristal ve amorf formlar veya serbest formlarindan bir veya daha fazlasi ifade edilmektedir. In the invention, the term "pharmaceutically acceptable derivatives" is defined as pharmaceutically acceptable. Suitable salts, esters, solvates, hydrates, complexes, polymorphs, enantiomers, prodrugs, acid addition salts, analogs, isomers, racemates, amides, enantiomer salts, basic salts, conjugates, tautoiners, anhydrates, anhydrides, bases, one or more of acids, ethers, crystalline and amorphous forms or free forms is expressed.
Oftalmik uygulama için hazirlanan farmasötik bilesim/ler damla (solüsyon, süspansiyon), krein, jel, merhem, losyon, liniment (sivi merhem), solüsyon, süspansiyon, emülsiyon (su/yag, yag/su) ve sivi Çözelti gibi dozaj formlarinda olabilir. Pharmaceutical composition(s) prepared for ophthalmic administration, drops (solution, suspension), Crein, gel, ointment, lotion, liniment (liquid ointment), solution, suspension, emulsion It can be in dosage forms such as (water/oil, oil/water) and liquid solution.
Bulusta kullanilan oftalmik uygulamaya yönelik farmasötik göz damlasi formülasyonu; uygun etken madde/ler yaninda en az bir viskozite ajani, en az bir tonisite ajani, en az bir yüzey aktif madde, en az bir selat yapici ajan, en az bir koruyucu madde, en az bir pH ayarlayici ajan ve çözücünün de dahil oldugu gruptan seçilen bir veya daha fazla yardimci madde içerebilen bir bilesimi tanimlar. Pharmaceutical eye drop formulation for ophthalmic administration used in the invention; In addition to the appropriate active ingredient/s, at least one viscosity agent, at least one tonicity agent, at least one surfactant, at least one chelating agent, at least one preservative, at least one pH one or more auxiliary agents selected from the group that includes the setting agent and solvent defines a composition that can contain a substance.
Bulusta “viskozite ajani” terimi, sivinin kalinligini arttirarak yavas akmasini saglayan bir ajan veya ajan karisimini belirtmektedir. Viskozite ajani olarak karbomer, ksantam gami, guar gam, acacia, povidon, aljinik asit, etilselüloz, jelatin, hidroksietil selüloz, hidroksipropil selüloz, poliVinil pirolidon, hidroksi propil metil selüloz (HPMC), polidekstroz, karragenan, metil selüloz, sukroz, sorbitol, ksilitol, hidroksipropil metilselüloz, polivinil alkol, ketearil alkol, kolloidal silikon dioksit ve bunlarin karisimlari kullanilabilir. Bulusta tercihen hidroksi propil metil selüloz (HPMC) kullanilmaktadir. In the invention, the term “viscosity agent” is a liquid that increases the thickness of the liquid and makes it flow slowly. denotes an agent or a mixture of agents. Carbomer, xantham gum as viscosity agent, guar gum, acacia, povidone, alginic acid, ethylcellulose, gelatin, hydroxyethyl cellulose, hydroxypropyl cellulose, polyVinyl pyrrolidone, hydroxy propyl methyl cellulose (HPMC), polydextrose, carrageenan, methyl cellulose, sucrose, sorbitol, xylitol, hydroxypropyl methylcellulose, polyvinyl alcohol, ketaryl alcohol, colloidal silicon dioxide and mixtures thereof can be used. Hydroxypropyl methyl cellulose (HPMC) is preferably used in the invention.
Bulusta kullanilan viskozite ajani miktari %0.01-5 agirlik/hacim oranindadir. The amount of viscosity agent used in the invention is 0.01-5% weight/volume.
Bulusta “tonisite ajani” terimi, standart referans madde ile ayni osmotik basinca sahip maddeleri ifade etmektedir. Tonisite ajani olarak; sodyum klorür, mannitol, sorbitol, gliserin, borik asit, potasyum nitrat, glukoz veya bunlarin karisimlari kullanilabilir. Bulusta belirtilen göz damlasinin izotonik olmasi tercih edilir, izotonik sivilar gözyasi ile ayni ozmotik basinca sahip oldugundan gözde yanma batma gibi yan etkilere ve lakrimal drenaja neden olmaz. Bulusta tercihen sodyum klorür ve mannitol kullanilmaktadir. In the invention, the term "tonicity agent" means having the same osmotic pressure as the standard reference substance. means items. As a tonicity agent; sodium chloride, mannitol, sorbitol, glycerin, boric acid, potassium nitrate, glucose or their mixtures can be used. in the find it is preferred that the specified eye drops be isotonic, isotonic liquids the same as tears Since it has osmotic pressure, it has side effects such as burning and stinging in the eye and lacrimal does not cause drainage. Sodium chloride and mannitol are preferably used in the invention.
Bulusta kullanilan tonisite ajani miktari %0.05-10 agirlik/hacim oranindadir. The amount of tonicity agent used in the invention is 0.05-10% w/v.
Bulusta “yüzey aktif madde” terimi suda veya sulu bir çözeltide çözündügünde yüzey gerilimini etkileyen kimyasal bilesigi ifade etmektedir. Yüzey aktif madde olarak sodyum lauril sülfat, sodyum setostearil sülfat ve sodyum tetradesil sülfat gibi uzun zincirli alkil sülfonat esterlerinin tuzlari, stearatlar gibi uzun zincirli karboksilik asitlerinin tuzlari, benzalkonyum klorür, tetradesiltrimetil amonyum bromür ve setilpiridinyum klorür gibi piridinyum bilesikleri ya da kuaterner amonyum, soya lesitin gibi lesitinleri ve lauril-l- karboksiglisin, polisorbat, gliseril monostearat gibi gliserol esterleri ve glikol, sorbitan tristearat gibi sorbitan ve mannitan esterleri (polioksietilen sorbitan mono-oleat), sorbitan esterlerinin polioksietilen türevleri veya bunlarin karisimlari kullanilabilir. Bulusta tercihen polisorbat kullanilmaktadir. Bulusta kullanilan yüzey aktif madde miktari %0.001-5 agirlik/hacim oranindadir. In the invention, the term "surfactant" is applied when dissolved in water or an aqueous solution. It refers to the chemical compound that affects the voltage. Sodium as surfactant long-chain alkyl sulfate, such as lauryl sulfate, sodium cetostearyl sulfate, and sodium tetradecyl sulfate salts of sulfonate esters, salts of long chain carboxylic acids such as stearates, such as benzalkonium chloride, tetradecyltrimethyl ammonium bromide, and cetylpyridinium chloride pyridinium compounds or lecithins such as quaternary ammonium, soy lecithin, and lauryl-l- esters of glycerol such as carboxyglycine, polysorbate, glyceryl monostearate, and glycol, sorbitan esters of sorbitan and mannitan such as tristearate (polyoxyethylene sorbitan mono-oleate), sorbitan Polyoxyethylene derivatives of esters or mixtures thereof can be used. preferably in the invention polysorbate is used. The amount of surfactant used in the invention is 0.001-5% weight/volume ratio.
Bulusta selat yapici ajan olarak EDTA (etilen diamin tetraasetik asit), disodyuin EDTA (disodyum etilen diamin tetraasetik asit) veya kalsiyum EDTA (kalsiyum etilen diamin tetraasetik asit) veya bunlarin karisimlari kullanilabilir. Bulusta tercihen disodyum EDTA kullanilmaktadir. Bulusta kullanilan selat yapici ajan miktari %0.001-5 agirlik/hacim oranindadir. EDTA (ethylene diamine tetraacetic acid), disodium EDTA as chelating agent in the invention (disodium ethylene diamine tetraacetic acid) or calcium EDTA (calcium ethylene diamine) tetraacetic acid) or mixtures thereof can be used. In the invention, preferably disodium EDTA is used. The amount of chelating agent used in the invention is 0.001-5% w/v is in the ratio.
Bulusta “koruyucu madde” terimi mikrobiyal aktiviteye karsi koruyan maddeleri ifade etmektedir. Koruyucu madde olarak; p- hidroksibenzoik asit ester, sodyuin benzoat, sodyum metil para hidroksibenzoat, sodyum propil para hidroksibenzoat, benzoik asit, borik asit, etilendiamintetraasetik asit, sorbik asit, klorobütanol, benzetonyum klorür, benzododesinyum bromür, feniletil alkol, benzalkonyum klorür, parabenler, sodyum propionat, propilen glikol, sorbatlar, polikuaterniyum veya bunlarin karisimlari kullanilabilir. Bulusta tercihen benzalkonyum klorür kullanilmaktadir. Bulusta kullanilan koruyucu madde miktari %0.000`l-l agirlik/hacim oranindadir. In the invention, the term "preservative" refers to substances that protect against microbial activity. is doing. As a preservative; p-hydroxybenzoic acid ester, sodium benzoate, sodium methyl para hydroxybenzoate, sodium propyl para hydroxybenzoate, benzoic acid, boric acid, ethylenediaminetetraacetic acid, sorbic acid, chlorobutanol, benzetonium chloride, benzododecinium bromide, phenylethyl alcohol, benzalkonium chloride, parabens, sodium propionate, propylene glycol, sorbates, polyquaternium or mixtures thereof can be used. Benzalkonium chloride is preferably used in the invention. used in the invention the amount of preservative is 0.000`l-l% weight/volume.
Bulusta pH ayarlayici ajan olarak; sülfürik asit, sodyum hidroksit, hidroklorik asit, sodyum klorit, asetik asit, borik asit, anhidröz sodyum sülfit, sodyum sitrat, sodyum karbonat veya bunlarin karisimlari kullanilabilir. Bulusta tercihen sodyum hidroksit kullanilmaktadir. As a pH adjusting agent in the invention; sulfuric acid, sodium hydroxide, hydrochloric acid, sodium chloride, acetic acid, boric acid, anhydrous sodium sulfite, sodium citrate, sodium carbonate or mixtures of these can be used. Sodium hydroxide is preferably used in the invention.
Bulusta çözücü olarak; saf su, enjeksiyonluk su, fizyolojik serum, sterilize damitilmis su gibi uygun sulu çözeltiler kullanilabilir. Bulusta tercihen saf su kullanilmaktadir. As a solvent in the invention; pure water, water for injection, physiological saline, sterilized distilled water Suitable aqueous solutions such as Pure water is preferably used in the invention.
Bulusta, Nepafenak ve/veya farmasötik olarak kabul edilebilir türevlerinin kullanildigi farmasötik bilesimlerin oftalmik uygulamasina yönelik göz damlasi formülasyonu asagidakileri içermektedir; - yaklasik %0.01-3 agirlik/hacim oraninda Nepafenak - yaklasik %001-5 agirlik/hacim oraninda bir veya daha fazla Viskozite ajani - yaklasik %005-10 agirlik/hacim oraninda bir veya daha fazla tonisite ajani - yaklasik %0.001-5 agirlik/hacim oraninda bir veya daha fazla yüzey aktif madde - yaklasik %0001-5 agirlik/hacim oraninda bir veya daha fazla selat yapici ajan - yaklasik %00001-1 agirlik/hacim oraninda bir veya daha fazla koruyucu madde - kafi miktar pH ayarlayici ajan ve çözücü. Nepafenac and/or pharmaceutically acceptable derivatives are used in the invention. eye drop formulation for ophthalmic administration of pharmaceutical compositions It includes the following; - ca. 0.01-3% w/v Nepafenac - one or more Viscosity agents at a weight/volume ratio of approximately 001-5% - one or more tonicity agents at a weight/volume ratio of approximately 005-10% - one or more surfactants in an approximate 0.001-5% weight/volume ratio - one or more chelating agents at a weight/volume ratio of approximately 0001-5% - one or more preservatives at a weight/volume ratio of approximately 00001-1% - sufficient amount of pH adjusting agent and solvent.
Bulus esas olarak oftalmik kullanilmak üzere steroid yapili olmayan antiinflamatuvar (NSAID) özellikteki uygun etken maddeyi ve/Veya farmasötik olarak kabul edilebilir türevlerini ve farmasötik olarak kabul edilebilir uygun yardimci maddeleri içeren farmasötik bilesim/lerin hazirlanmasi ile ilgilidir. Bulusun farmasötik bilesimlerinin oftalmik göz damlasi formunda olmasi temeldir. Böylece Nepafenak ve/Veya farmasötik olarak kabul edilebilir türevlerini ve farmasötik olarak kabul edilebilir uygun yardimci maddeleri içeren farmasötik dozaj form/lari tahris edici özelliklerinin düsük olmasi, çabuk etki etmesi: gözde kuruluk yapmamasi, kullanimlarinin daha kolay olmasi gibi üstünlüklere sahiptir ve bu farmasötik bilesimler fiziksel ve kimyasal kararlilik açisindan oldukça stabil bir davranis sergilemistir. The invention is primarily a non-steroidal anti-inflammatory drug for ophthalmic use. (NSAID) and/or pharmaceutically acceptable derivatives and suitable pharmaceutically acceptable excipients. relates to the preparation of pharmaceutical composition(s). Pharmaceutical compositions of the invention It is essential that it be in the form of ophthalmic eye drops. Thus, Nepafenac and/or pharmaceutical acceptable derivatives and suitable pharmaceutically acceptable excipients. Pharmaceutical dosage form/s containing substances have low irritant properties, effect: it does not dry the eyes, it has advantages such as being easier to use. and these pharmaceutical compositions are quite stable in terms of physical and chemical stability. exhibited a behavior.
Asagidaki örnekler bulusu açiklamaktadir, fakat hiçbir suretle kisitlamamaktadirlar. The following examples illustrate the invention, but in no way limit it.
Nepafenak ve/Veya farmasötik olarak kabul edilebilir türevlerinin kullanildigi farmasötik bilesimlerin oftalmik uygulamasina yönelik göz damlasi formülasyonu asagidakileri içermektedir; - yaklasik %001-3 agirlik/hacim oraninda Nepafenak - yaklasik %0.01-5 agirlik/hacim oraninda hidroksi propil metil selüloz - yaklasik %005-10 agirlik/hacim oraninda sodyum klorür ve mannitol - yaklasik %0001-5 agirlik/hacim oraninda polisorbat - yaklasik %0.001-5 agirlik/hacim oraninda disodyuni EDTA - yaklasik %00001-1 agirlik/hacim oraninda benzalkonyum klorür - kafi miktar sodyum hidroksit ve saf su. Pharmaceutical use of Nepafenac and/or its pharmaceutically acceptable derivatives eye drop formulation for ophthalmic administration of the compounds includes; - approximately 001-3% w/v Nepafenac - approx. 0.01-5% w/v hydroxy propyl methyl cellulose - approximately 005-10% w/v sodium chloride and mannitol - polysorbate ca. 0001-5% w/v - approximately 0.001-5% w/v disodium EDTA - benzalkonium chloride approx. 00001-1% by weight/volume - enough sodium hydroxide and purified water.
Nepafenak ve/Veya farmasötik olarak kabul edilebilir türevlerinin kullanildigi farmasötik bilesimlerin oftalmik uygulamasina yönelik göz damlasi formülasyonu asagidakileri içermektedir; - yaklasik 0.1-10mg Nepafenak - yaklasik 0.5-15mg hidroksi propil metil selüloz - yaklasik 0.1-75mg sodyum klorür ve mannitol - yaklasik 0.01-5mg disodyum EDTA - yaklasik 0.001-1mg benzalkonyum klorür - kafi miktar sodyum hidroksit ve saf su. Üretim prosesi: Saf suya yavas yavas HPMC eklenerek belirli bir hiz altinda karistirma ile belirli bir süre karistirilir. Benzalkonyum klorür eklenerek belirli bir süre karistirilir. Mannitol eklenerek belirli bir süre karistirilir. Sodyum klorür eklenerek belirli bir süre karistirilir. Disodyuni EDTA eklenerek belirli bir süre karistirilir (Çözelti I). Pharmaceutical use of Nepafenac and/or its pharmaceutically acceptable derivatives eye drop formulation for ophthalmic administration of the compounds includes; - about 0.1-10mg of Nepafenac - about 0.5-15mg hydroxypropyl methyl cellulose - about 0.1-75mg of sodium chloride and mannitol - about 0.01-5mg of disodium EDTA - about 0.001-1mg of benzalkonium chloride - enough sodium hydroxide and purified water. Production process: By slowly adding HPMC to pure water, mixing under a certain speed for a certain time. is mixed. Benzalkonium chloride is added and mixed for a certain time. By adding mannitol is mixed for a certain period of time. Sodium chloride is added and mixed for a certain time. dysodynia EDTA is added and mixed for a certain time (Solution I).
Polisorbat saf suyun bir kisminda çözündürülür. Uygun filtreden geçirilir (Çözelti II). Çözelti II” ye Nepafenak eklenerek belirli bir süre hoinojenize edilir. Elde edilen çözelti çözelti Ve eklenir. Belirli bir süre homojenize edilir. Uygun pH ayarlayiei ajan/lar ile pH ayarlanir. Geri kalan saf su ile hacmine tamamlanir. The polysorbate is dissolved in some of the purified water. It is passed through the appropriate filter (Solution II). Nepafenac is added to Solution II and homogenized for a certain time. The resulting solution solution and is added. It is homogenized for a certain time. pH with appropriate pH adjusting agent/s is set. The remainder is made up to volume with pure water.
Claims (4)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| TR2014/02298A TR201402298A2 (en) | 2014-02-26 | 2014-02-26 | Ophthalmic pharmaceutical compositions. |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| TR2014/02298A TR201402298A2 (en) | 2014-02-26 | 2014-02-26 | Ophthalmic pharmaceutical compositions. |
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| Publication Number | Publication Date |
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| TR201402298A2 true TR201402298A2 (en) | 2015-09-21 |
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| TR2014/02298A TR201402298A2 (en) | 2014-02-26 | 2014-02-26 | Ophthalmic pharmaceutical compositions. |
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| TR (1) | TR201402298A2 (en) |
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2014
- 2014-02-26 TR TR2014/02298A patent/TR201402298A2/en unknown
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