TR2021001943A2 - A film coated tablet comprising emoxypine - Google Patents
A film coated tablet comprising emoxypineInfo
- Publication number
- TR2021001943A2 TR2021001943A2 TR2021/001943A TR2021001943A TR2021001943A2 TR 2021001943 A2 TR2021001943 A2 TR 2021001943A2 TR 2021/001943 A TR2021/001943 A TR 2021/001943A TR 2021001943 A TR2021001943 A TR 2021001943A TR 2021001943 A2 TR2021001943 A2 TR 2021001943A2
- Authority
- TR
- Turkey
- Prior art keywords
- film
- coated tablet
- tablet according
- feature
- emoxipin
- Prior art date
Links
- JPGDYIGSCHWQCC-UHFFFAOYSA-N emoxypine Chemical compound CCC1=NC(C)=CC=C1O JPGDYIGSCHWQCC-UHFFFAOYSA-N 0.000 title claims abstract description 41
- 239000007941 film coated tablet Substances 0.000 title claims abstract description 28
- 150000003839 salts Chemical class 0.000 claims abstract description 24
- 238000000034 method Methods 0.000 claims abstract description 9
- 239000000546 pharmaceutical excipient Substances 0.000 claims abstract description 9
- 239000000203 mixture Substances 0.000 claims description 39
- 238000009472 formulation Methods 0.000 claims description 15
- 239000000945 filler Substances 0.000 claims description 12
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 12
- 229920000881 Modified starch Polymers 0.000 claims description 9
- 239000000314 lubricant Substances 0.000 claims description 9
- MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 claims description 8
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims description 8
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 8
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 8
- 229940045902 sodium stearyl fumarate Drugs 0.000 claims description 8
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 6
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 6
- 229920002472 Starch Polymers 0.000 claims description 6
- 239000011230 binding agent Substances 0.000 claims description 6
- -1 hydroxypropyl Chemical group 0.000 claims description 6
- 235000019359 magnesium stearate Nutrition 0.000 claims description 6
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 6
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 6
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 6
- 239000008107 starch Substances 0.000 claims description 6
- 235000019698 starch Nutrition 0.000 claims description 6
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-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
- 125000003976 glyceryl group Chemical group [H]C([*])([H])C(O[H])([H])C(O[H])([H])[H] 0.000 claims description 4
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims description 4
- 238000005550 wet granulation Methods 0.000 claims description 4
- KZUIXWYHQJZUOK-UHFFFAOYSA-N 2-ethyl-6-methylpyridin-1-ium-3-ol;chloride Chemical compound Cl.CCC1=NC(C)=CC=C1O KZUIXWYHQJZUOK-UHFFFAOYSA-N 0.000 claims description 3
- 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 3
- PMZURENOXWZQFD-UHFFFAOYSA-L Sodium Sulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=O PMZURENOXWZQFD-UHFFFAOYSA-L 0.000 claims description 3
- 229920002125 Sokalan® Polymers 0.000 claims description 3
- 235000021355 Stearic acid Nutrition 0.000 claims description 3
- YKTSYUJCYHOUJP-UHFFFAOYSA-N [O--].[Al+3].[Al+3].[O-][Si]([O-])([O-])[O-] Chemical compound [O--].[Al+3].[Al+3].[O-][Si]([O-])([O-])[O-] YKTSYUJCYHOUJP-UHFFFAOYSA-N 0.000 claims description 3
- 239000000378 calcium silicate Substances 0.000 claims description 3
- 229910052918 calcium silicate Inorganic materials 0.000 claims description 3
- 235000012241 calcium silicate Nutrition 0.000 claims description 3
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 claims description 3
- 235000013539 calcium stearate Nutrition 0.000 claims description 3
- 239000008116 calcium stearate Substances 0.000 claims description 3
- OYACROKNLOSFPA-UHFFFAOYSA-N calcium;dioxido(oxo)silane Chemical compound [Ca+2].[O-][Si]([O-])=O OYACROKNLOSFPA-UHFFFAOYSA-N 0.000 claims description 3
- 239000008121 dextrose Substances 0.000 claims description 3
- 238000007908 dry granulation Methods 0.000 claims description 3
- 229960001031 glucose Drugs 0.000 claims description 3
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims description 3
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims description 3
- 239000008117 stearic acid Substances 0.000 claims description 3
- 239000000454 talc Substances 0.000 claims description 3
- 235000012222 talc Nutrition 0.000 claims description 3
- 229910052623 talc Inorganic materials 0.000 claims description 3
- BZSXEZOLBIJVQK-UHFFFAOYSA-N 2-methylsulfonylbenzoic acid Chemical compound CS(=O)(=O)C1=CC=CC=C1C(O)=O BZSXEZOLBIJVQK-UHFFFAOYSA-N 0.000 claims description 2
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 claims description 2
- 229920000623 Cellulose acetate phthalate Polymers 0.000 claims description 2
- 229920001661 Chitosan Polymers 0.000 claims description 2
- 229920002261 Corn starch Polymers 0.000 claims description 2
- 108010010803 Gelatin Proteins 0.000 claims description 2
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 claims description 2
- 239000004354 Hydroxyethyl cellulose Substances 0.000 claims description 2
- 229920001479 Hydroxyethyl methyl cellulose Polymers 0.000 claims description 2
- OFOBLEOULBTSOW-UHFFFAOYSA-L Malonate Chemical compound [O-]C(=O)CC([O-])=O OFOBLEOULBTSOW-UHFFFAOYSA-L 0.000 claims description 2
- 229920002774 Maltodextrin Polymers 0.000 claims description 2
- 239000005913 Maltodextrin Substances 0.000 claims description 2
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims description 2
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims description 2
- 229920000148 Polycarbophil calcium Polymers 0.000 claims description 2
- 229920001100 Polydextrose Polymers 0.000 claims description 2
- 239000002202 Polyethylene glycol Substances 0.000 claims description 2
- BCKXLBQYZLBQEK-KVVVOXFISA-M Sodium oleate Chemical compound [Na+].CCCCCCCC\C=C/CCCCCCCC([O-])=O BCKXLBQYZLBQEK-KVVVOXFISA-M 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
- WNLRTRBMVRJNCN-UHFFFAOYSA-L adipate(2-) Chemical compound [O-]C(=O)CCCCC([O-])=O WNLRTRBMVRJNCN-UHFFFAOYSA-L 0.000 claims description 2
- WNROFYMDJYEPJX-UHFFFAOYSA-K aluminium hydroxide Chemical compound [OH-].[OH-].[OH-].[Al+3] WNROFYMDJYEPJX-UHFFFAOYSA-K 0.000 claims description 2
- FUFJGUQYACFECW-UHFFFAOYSA-L calcium hydrogenphosphate Chemical compound [Ca+2].OP([O-])([O-])=O FUFJGUQYACFECW-UHFFFAOYSA-L 0.000 claims description 2
- 229920003123 carboxymethyl cellulose sodium Polymers 0.000 claims description 2
- 229940063834 carboxymethylcellulose sodium Drugs 0.000 claims description 2
- 229940081734 cellulose acetate phthalate Drugs 0.000 claims description 2
- 229940082500 cetostearyl alcohol Drugs 0.000 claims description 2
- 229940045110 chitosan Drugs 0.000 claims description 2
- 229940075614 colloidal silicon dioxide Drugs 0.000 claims description 2
- 239000008120 corn starch Substances 0.000 claims description 2
- 235000019700 dicalcium phosphate Nutrition 0.000 claims description 2
- 229940095079 dicalcium phosphate anhydrous Drugs 0.000 claims description 2
- 238000010017 direct printing Methods 0.000 claims description 2
- 239000001530 fumaric acid Substances 0.000 claims description 2
- 229920000159 gelatin Polymers 0.000 claims description 2
- 239000008273 gelatin Substances 0.000 claims description 2
- 235000019322 gelatine Nutrition 0.000 claims description 2
- 235000011852 gelatine desserts Nutrition 0.000 claims description 2
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 claims description 2
- 229960001021 lactose monohydrate Drugs 0.000 claims description 2
- 239000000395 magnesium oxide Substances 0.000 claims description 2
- CPLXHLVBOLITMK-UHFFFAOYSA-N magnesium oxide Inorganic materials [Mg]=O CPLXHLVBOLITMK-UHFFFAOYSA-N 0.000 claims description 2
- 235000012245 magnesium oxide Nutrition 0.000 claims description 2
- 239000000391 magnesium silicate Substances 0.000 claims description 2
- 229910052919 magnesium silicate Inorganic materials 0.000 claims description 2
- 235000019792 magnesium silicate Nutrition 0.000 claims description 2
- AXZKOIWUVFPNLO-UHFFFAOYSA-N magnesium;oxygen(2-) Chemical compound [O-2].[Mg+2] AXZKOIWUVFPNLO-UHFFFAOYSA-N 0.000 claims description 2
- ZADYMNAVLSWLEQ-UHFFFAOYSA-N magnesium;oxygen(2-);silicon(4+) Chemical compound [O-2].[O-2].[O-2].[Mg+2].[Si+4] ZADYMNAVLSWLEQ-UHFFFAOYSA-N 0.000 claims description 2
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 claims description 2
- 229940035034 maltodextrin Drugs 0.000 claims description 2
- 229920001206 natural gum Polymers 0.000 claims description 2
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 claims description 2
- 239000008188 pellet Substances 0.000 claims description 2
- 229960000502 poloxamer Drugs 0.000 claims description 2
- 229920001983 poloxamer Polymers 0.000 claims description 2
- 229950005134 polycarbophil Drugs 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
- 229920001223 polyethylene glycol Polymers 0.000 claims description 2
- 229920000193 polymethacrylate Polymers 0.000 claims description 2
- 239000000377 silicon dioxide Substances 0.000 claims description 2
- 235000012239 silicon dioxide Nutrition 0.000 claims description 2
- 239000001632 sodium acetate Substances 0.000 claims description 2
- 235000017281 sodium acetate Nutrition 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
- 229940032147 starch Drugs 0.000 claims description 2
- OULAJFUGPPVRBK-UHFFFAOYSA-N tetratriacontyl alcohol Natural products CCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCO OULAJFUGPPVRBK-UHFFFAOYSA-N 0.000 claims description 2
- XOOUIPVCVHRTMJ-UHFFFAOYSA-L zinc stearate Chemical compound [Zn+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O XOOUIPVCVHRTMJ-UHFFFAOYSA-L 0.000 claims description 2
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims 2
- 150000004676 glycans Chemical class 0.000 claims 2
- 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 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims 1
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 claims 1
- 229930195725 Mannitol Natural products 0.000 claims 1
- 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 1
- 229930006000 Sucrose Natural products 0.000 claims 1
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 1
- SNAAJJQQZSMGQD-UHFFFAOYSA-N aluminum magnesium Chemical compound [Mg].[Al] SNAAJJQQZSMGQD-UHFFFAOYSA-N 0.000 claims 1
- 229960004977 anhydrous lactose Drugs 0.000 claims 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims 1
- 159000000007 calcium salts Chemical class 0.000 claims 1
- 229920002678 cellulose Polymers 0.000 claims 1
- 239000001913 cellulose Substances 0.000 claims 1
- 235000010980 cellulose Nutrition 0.000 claims 1
- 229940096516 dextrates Drugs 0.000 claims 1
- 239000001341 hydroxy propyl starch Substances 0.000 claims 1
- 235000013828 hydroxypropyl starch Nutrition 0.000 claims 1
- 239000000832 lactitol Substances 0.000 claims 1
- VQHSOMBJVWLPSR-JVCRWLNRSA-N lactitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@@H]1O[C@H](CO)[C@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-JVCRWLNRSA-N 0.000 claims 1
- 235000010448 lactitol Nutrition 0.000 claims 1
- 229960003451 lactitol Drugs 0.000 claims 1
- 239000008101 lactose Substances 0.000 claims 1
- 229960001375 lactose Drugs 0.000 claims 1
- 239000011777 magnesium Substances 0.000 claims 1
- 229910052749 magnesium Inorganic materials 0.000 claims 1
- 239000000594 mannitol Substances 0.000 claims 1
- 235000010355 mannitol Nutrition 0.000 claims 1
- 229960001855 mannitol Drugs 0.000 claims 1
- 229920001282 polysaccharide Polymers 0.000 claims 1
- 239000005017 polysaccharide Substances 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
- 229960002668 sodium chloride Drugs 0.000 claims 1
- 239000000600 sorbitol Substances 0.000 claims 1
- 229960002920 sorbitol Drugs 0.000 claims 1
- 239000005720 sucrose Substances 0.000 claims 1
- 229960004793 sucrose Drugs 0.000 claims 1
- 239000003826 tablet Substances 0.000 description 10
- 238000002156 mixing Methods 0.000 description 8
- 239000007888 film coating Substances 0.000 description 6
- 238000009501 film coating Methods 0.000 description 6
- 239000002904 solvent Substances 0.000 description 5
- 238000004090 dissolution Methods 0.000 description 4
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 3
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 3
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- 239000003963 antioxidant agent Substances 0.000 description 3
- 230000003078 antioxidant effect Effects 0.000 description 3
- 239000011248 coating agent Substances 0.000 description 3
- 238000000576 coating method Methods 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- 239000004615 ingredient Substances 0.000 description 3
- 239000002245 particle Substances 0.000 description 3
- 239000008194 pharmaceutical composition Substances 0.000 description 3
- 239000004484 Briquette Substances 0.000 description 2
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 2
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 2
- 230000000141 anti-hypoxic effect Effects 0.000 description 2
- 239000011247 coating layer Substances 0.000 description 2
- VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 230000001777 nootropic effect Effects 0.000 description 2
- 230000001624 sedative effect Effects 0.000 description 2
- 238000010561 standard procedure Methods 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- IKMNOGHPKNFPTK-UHFFFAOYSA-N 2-ethyl-6-methylpyridin-1-ium-3-ol;4-hydroxy-4-oxobutanoate Chemical compound OC(=O)CCC(O)=O.CCC1=NC(C)=CC=C1O IKMNOGHPKNFPTK-UHFFFAOYSA-N 0.000 description 1
- 239000005995 Aluminium silicate Substances 0.000 description 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 1
- 208000026139 Memory disease Diseases 0.000 description 1
- 102000004316 Oxidoreductases Human genes 0.000 description 1
- 108090000854 Oxidoreductases Proteins 0.000 description 1
- VMHLLURERBWHNL-UHFFFAOYSA-M Sodium acetate Chemical compound [Na+].CC([O-])=O VMHLLURERBWHNL-UHFFFAOYSA-M 0.000 description 1
- 206010041349 Somnolence Diseases 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 235000012211 aluminium silicate Nutrition 0.000 description 1
- 238000004458 analytical method Methods 0.000 description 1
- 230000003496 anti-amnesic effect Effects 0.000 description 1
- 230000001773 anti-convulsant effect Effects 0.000 description 1
- 230000002253 anti-ischaemic effect Effects 0.000 description 1
- 239000002249 anxiolytic agent Substances 0.000 description 1
- 230000000949 anxiolytic effect Effects 0.000 description 1
- 125000003118 aryl group Chemical group 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 238000007906 compression Methods 0.000 description 1
- 230000006835 compression Effects 0.000 description 1
- 239000006184 cosolvent Substances 0.000 description 1
- 230000001186 cumulative effect Effects 0.000 description 1
- 238000007907 direct compression Methods 0.000 description 1
- 238000009826 distribution Methods 0.000 description 1
- 229960003638 dopamine Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 238000001125 extrusion Methods 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 238000005469 granulation Methods 0.000 description 1
- 230000003179 granulation Effects 0.000 description 1
- 125000001072 heteroaryl group Chemical group 0.000 description 1
- 238000009474 hot melt extrusion Methods 0.000 description 1
- 239000012943 hotmelt Substances 0.000 description 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
- 238000009776 industrial production Methods 0.000 description 1
- 239000007972 injectable composition Substances 0.000 description 1
- NLYAJNPCOHFWQQ-UHFFFAOYSA-N kaolin Chemical compound O.O.O=[Al]O[Si](=O)O[Si](=O)O[Al]=O NLYAJNPCOHFWQQ-UHFFFAOYSA-N 0.000 description 1
- 238000007561 laser diffraction method Methods 0.000 description 1
- 150000002632 lipids Chemical class 0.000 description 1
- 229940037627 magnesium lauryl sulfate Drugs 0.000 description 1
- HBNDBUATLJAUQM-UHFFFAOYSA-L magnesium;dodecyl sulfate Chemical compound [Mg+2].CCCCCCCCCCCCOS([O-])(=O)=O.CCCCCCCCCCCCOS([O-])(=O)=O HBNDBUATLJAUQM-UHFFFAOYSA-L 0.000 description 1
- 238000007909 melt granulation Methods 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 235000010981 methylcellulose Nutrition 0.000 description 1
- 230000001670 myorelaxant effect Effects 0.000 description 1
- 230000002981 neuropathic effect Effects 0.000 description 1
- 230000000324 neuroprotective effect Effects 0.000 description 1
- 230000003647 oxidation Effects 0.000 description 1
- 238000007254 oxidation reaction Methods 0.000 description 1
- 230000001717 pathogenic effect Effects 0.000 description 1
- 150000002978 peroxides Chemical class 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 229920001592 potato starch Polymers 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 238000003825 pressing Methods 0.000 description 1
- 230000002633 protecting effect Effects 0.000 description 1
- 239000000932 sedative agent Substances 0.000 description 1
- 238000007873 sieving Methods 0.000 description 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 1
- 239000007909 solid dosage form Substances 0.000 description 1
- 238000000935 solvent evaporation Methods 0.000 description 1
- 238000005563 spheronization Methods 0.000 description 1
- 238000001694 spray drying Methods 0.000 description 1
- 150000003890 succinate salts Chemical class 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- 238000011287 therapeutic dose Methods 0.000 description 1
- 239000004408 titanium dioxide Substances 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Abstract
Mevcut buluş, emoksipin veya bunun farmasötik olarak kabul edilebilir bir tuzu ile en az bir farmasötik olarak kabul edilebilir yardımcı maddeyi içeren bir film kaplı tablet ile ilgilidir. Mevcut buluş ayrıca basit, hızlı, uygun maliyetli, zamandan tasarruf edilmesini sağlayan ve endüstriyel açıdan elverişli bir proses ile ilgilidir.The present invention relates to a film-coated tablet comprising emoxipine or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable excipient. The present invention also relates to a simple, fast, cost-effective, time-saving and industrially convenient process.
Description
TARFNAME EMOKSIPIN IÇEREN BIR FILM KAPLI TABLET Teknik Alan Mevcut bulus, emoksipin veya bunun farmasötik olarak kabul edilebilir bir tuzu ile en az bir farmasötik olarak kabul edilebilir yardimci maddeyi içeren bir film kapli tablet ile ilgilidir. Mevcut bulus ayrica basit, hizli, uygun maliyetli, zamandan tasarruf edilmesini saglayan ve endüstriyel açidan elverisli bir proses ile ilgilidir. Bulusun Geçmisi Emoksipin membran koruyucu, nootropik ve yatistirici etkiye sahip bir heteroaromatik antioksidandir. Aromatik etki alani organizmalardaki stres direncini arttirmayi kapsayacak kadar genistir. Uyku hali ve miyorölaksan etkiye neden olmayan anksiyolitik görevi görmekle birlikte, nootropik özellikleri patojenik faktörler altindaki yasli hastalarda ögrenme ve hafiza kusurlarini önlemeye ya da azaltmaya yardimci olmaktadir. Emoksipinin faaliyetlerinden biri antioksidan ve antihipoksik özellikler gösteren antikonvülzan etkidir. Dikkat konsantrasyonunu ve çalisma kapasitesini arttirirken alkolün toksik etkisini azaltmaktadir. Lipitlerin peroksit oksidasyonunu engellerken süper oksit oksidaz etkisini arttirmakta ve Iipid- protein oranini yükseltmektedir. Ayrica, beyinde daha yüksek bir dopamin konsantrasyonu saglamaktadir. Kimyasal adi 2-etiI-6-metil-3-hidroksipiridindir ve kimyasal yapisi da Formül l`de gösterildigi Formül I Emoksipin MEXIDOL® markasi altinda pazarlanmakta ve günde üç kere, 125 ila 250 mg'lik terapatik bir dozda oral yoldan uygulanmaktadir ve lV/lM formlarindaki 2 ila 5 ml'lik ampüllerde 50mg/ml içeren enjekte edilebilir formülasyonlara sahiptir. Emoksipin; nöroprotektif, antiamnestik, antioksidan, antihipoksik, antiiskemik faaliyet gösteren kati dozaj formlarinda kullanilabilir. WO 96/02238 A1 dokümaninda çekirdekte emoksipin süksinat ile yardimci maddeleri ve bir kaplama katmanini içeren bir nöropatik ve sedatif formülasyon açiklanmaktadir. Çekirdekteki yardimci maddeler kaolin, patates nisastasi, kalsiyum stearat, stearik asit, talk ve metil selülozu içermektedir. Kaplama katmani ise titanyum dioksit ve Serge 80'i içermektedir. EP224131O A2 numarali patent basvurusunda en az bir farmasötik olarak kabul edilebilir yardimci madde ile birlikte emoksipin veya bunun farmasötik olarak kabul edilebilir bir tuzunu ve bir salim kontrol eden polimeri içeren bir farmasötik formülasyondan söz edilmektedir. Emoksipinin dezavantaji raf ömrü süresince ürünün stabilitesinin düsük olmasidir. Bu özellikten dolayi teknigin bilinen durumuna ait farkli ilaç formlarinda emoksipinin kullanimiyla karsilasmaktayiz. Teknigin bilinen durumunda emoksipin veya bunun farmasötik olarak kabul edilebilir bir tuzunu içeren bir farmasötik formülasyona yönelik çok sayida patent basvurusu mevcuttur. Fakat etkin maddeye bagli problemleri ortadan kaldirmak için formülasyonun iyilestirilmesine halen ihtiyaç duyulmaktadir. Teknigin bilinen durumunda yüksek stabilitesi, çözünme hizi ve mükemmel farmakoteknik Özellikleri olan, emoksipin veya bunun farmasötik olarak kabul edilebilir bir tuzunun iyilestirilmis bir farmasötik bilesimine ihtiyaç vardir. Mevcut bulusta bahsedilen problemlerin üstesinden gelmek için emoksipin veya bunun farmasötik olarak kabul edilebilir bir tuzunu içeren bir film kapli tablet ortaya konulmaktadir. Ayrica söz konusu tablet basit ve uygun maliyetli bir yöntem olan standart teknikler araciligiyla gelistirilmistir. Bulusun Detayli Açiklamasi Mevcut bulusun esas amaci emoksipin veya bunun farmasötik olarak kabul edilebilir tuzunun yol açtigi sorunlari ortadan kaldirmak ve teknigin bilinen durumuna ilave avantajlar saglamaktir. Mevcut bulusun bir diger amaci; akiskanlik, sikistirilabilirlik ve içerik tekdüzeligi gibi farmakoteknik özellikleri mükemmel olan ve arzu edilen çözünme profiline ve stabiliteye sahip olan bir film kapli tablet ortaya koymaktir. Mevcut bulusun bu düzenlemesine göre emoksipin veya tuzlari ile en az bir farmasötik olarak kabul edilebilir yardimci maddeyi içeren bir film kapli tablet ortaya konulmakta olup, burada sözü edilen tablet asagidakileri içermektedir: I toplam formülasyon agirligi bakimindan %100 ila %450 oraninda emoksipin veya tuzlari, - toplam formülasyon agirligi bakimindan %20 ila %20.0 oraninda baglayicilar. Mevcut bulusun bu düzenlemesine göre, emoksipin veya tuzlarinin miktari toplam formülasyon agirligi bakimindan %20.0 ile %400 arasindadir. Teknigin bilinen durumunda emoksipinin stabilite problemlerinin oldugu bilinmektedir. Yukarida verilen oranlarda emoksipin veya tuzlarinin yani sira baglayici içeren bir film kapli tablet ortaya koyarak sasirtici bir sekilde bu problemi çözmeyi basarmis bulunmaktayiz. Uygun baglayicilar; prejelatinize nisasta, misir nisastasi, dogal sakizlar, jelatin, karbomerler, karbomerler, karboksimetilselüloz sodyum, selüloz asetat ftalat, kitozan, dekstroz, estilselüloz, gliseril behanat, hidroksietil selüloz, hidroksietilmetil selüloz, hidroksipropil selüloz, hidroksipropil nisasta, magnezyum aluminyum silikat, poloksamer, polikarbofil, polidekstroz, polietilen oksit, polimetakrilatlar, alüminyum hidroksit, setostearil alkol, polioksietilen-alkil eterler veya bunlarin karisimlarini içeren gruptan seçilmektedir. Mevcut bulusun bu düzenlemesine göre, baglayicilarin miktari toplam formülasyon agirligi bakimindan %20 ile %20.0 arasinda; en tercihen toplam formülasyon agirligi bakimindan Mevcut bulusun bu düzenlemesine göre baglayici prejelatinize nisastadir. Mevcut bulusun bu düzenlemesine göre emoksipinin farmasötik olarak kabul edilebilir tuzu; emoksipin süksinat tuzu, emoksipin maleat, emoksipin malonat, emoksipin adipat, emoksipin HCI seklindedir. Emoksipinin farmasötik olarak kabul edilebilir tuzu tercihen emoksipin süksinat tuzu veya emoksipin HCI'dür. Burada kullanildigi sekliyle 'parçacik boyutu' lazer kirinimi yöntemi (bir baska ifadeyle Malvern Mastersizer 2000 analizi) gibi konvansiyonel olarak kabul görmüs herhangi bir yöntem ile test edilen kümülatif hacim boyut dagilimi anlamina gelmektedir. d (0.9) terimi, hacimce parçaciklarin % 90'inin daha ince oldugu boyut anlamina gelmektedir. Mevcut bulusun bir düzenlemesinde, emoksipin veya tuzlarinin d (0.9) parçacik boyutu 600 um'den daha az, tercihen 500 um'den daha az, tercihen 400 um'den daha az, tercihen 300 um'den daha azdir. Mevcut bulusun bu düzenlemesine göre farmasötik olarak kabul edilebilir yardimci maddeler; dolgu maddeleri, Iubrikanlarlglidanlar veya bunlarin karisimlarini içeren gruptan seçilmektedir. Uygun dolgu maddeleri; mikrokristalin selüloz, polivinilpirolidon, Iaktoz monohidrat, susuz pellet, nisasta, maltodekstrin, dibazik kalsiyum fosfat veya bunlarin karisimlarini içeren gruptan seçilmektedir. Dogru dolgu maddesinin kullanimi sayesinde formülasyonda içerik tekdüzeligi saglanmistir. Mevcut bulusun bu düzenlemesine göre, dolgu maddelerinin miktari toplam formülasyon agirligi bakimindan %50 ile %500 arasindadir. Mevcut bulusun bu düzenlemesine göre, dolgu maddeleri miktari toplam formülasyon agirligi Mevcut bulusun bu düzenlemesine göre dolgu maddesi; mikrokristalin selüloz veya polivinilpirolidon veya bunlarin karisimidir. Tarif edilen dolgu maddesinin kullanimi, arzu edilen çözünme profilinin elde edilmesini saglamaktadir. Uygun Iubrikanlarlglidanlar; magnezyum stearat, sodyum stearil fumarat, kolloidal silikon dioksit, kalsiyum stearat, çinko stearat, talk, silikon dioksit, aluminyum silikat, kalsiyum silikat, magnezyum silikat, magnezyum oksit, nisasta, sodyum klorat, magnezyum loril sülfat, sodyum oleat, sodyum asetat, sodyum benzoat, polietien glikol, stearik asit, fumarik asit, gliseril palmito sülfat, sodyum loril sülfat veya bunlarin karisimlarini içeren gruptan seçilmektedir. Mevcut bulusun bu düzenlemesine göre, Iubrikanlarin/glidanlarin miktari toplam formülasyon agirligi bakimindan %025 ile %1.5 arasindadir. Mevcut bulusun bu düzenlemesine göre lubrikan/glidan; magnezyum stearat veya sodyum stearil fumarat veya bunlarin karisimlaridir. Tarif edilen Iubrikanin/glidanin kullanimi, arzu edilen akiskanligin elde edilmesini saglamaktadir. Mevcut bulus konusu emoksipin veya tuzlarini içeren film kapli tablet; dogrudan baski, islak veya kuru granülasyon, sicak eriyik granülasyon, sicak eriyik ekstrüzyon, akiskan yatakli granülasyon, ekstrüzyon/küre haline getirme, ön kompresyon/çift basim, püskürterek kurutma ve çözücüyle buharlastirma gibi teknigin mevcut durumunda iyi bilinen standart teknikler ya da üretim yöntemleri kullanilarak hazirlanabilir. Mevcut bulusun bu düzenlemesine göre film kapli tablet; islak veya kuru granülasyon ya da dogrudan baski yöntemiyle hazirlanmaktadir. Mevcut bulusun bu düzenlemesine göre islak granülasyonda çözücüler veya ko-çözücüler kullanilmaktadir. Uygun çözücüler veya ko-çözücüler; su, dimetil sülfoksit, diklorometan, metanol, aseton, izopropil alkol veya bunlarin karisimlarini içeren gruptan seçilmektedir. Mevcut bulus konusu film kapli tablette arzu edilen bir çözünme profili ve arzu edilen bir içerik tekdüzeligi elde edilmektedir ve kullanilan basit üretim prosesi endüstriyel üretime elverislidir. Örnek 1: Film Kapli Tablet Bilesenler Miktar (toplam bilesim agirligi bakimindan %) Prejelatinize nisasta 2.0 - 20.0 (3-15) Magnezyum stearat 0.25 - 1.5 (0.2-1.0) Film kaplama 2.0 - 8.0 (3-7) Toplam bilesim 100 Örnek 1'e ait bir proses: a) Emoksipin veya tuzlari, mikrokristalin selüloz, prejelatinize nisastanin elekten geçirilerek karistirilmasi, b) Magnezyum stearatin eklenerek karistirilmasi, o) Toplam karisimin tabletler elde edecek sekilde sikistirilmasi, d) Tabletlerin film kaplama ile kaplanmasi. Örnek 2: Film Kapli Tablet Bilesenler Miktar (toplam bilesim agirligi bakimindan %) Emoksipin veya tuzlari 10.0 - 45.0 Prejelatinize nisasta 2.0 - 20.0 Sodyum stearil fumarat 0.25 - 1.5 Film kaplama 2.0 - 8.0 Toplam bilesim 100 Örnek 2'ye ait bir proses: a) Emoksipin veya tuzlari, polivinilpirolidonun yarisi, prejelatinize nisastanin yarisinin karistirilmasi, Hazirlanan toz karisimin çözücü/ko-çözücü ile granüle edilmesi, Hazirlanan yas granüllerin kurutulmasi, Prejeletinize nisasta ve polivinilpirolidonun kalan kisimlarinin eklenerek karistirilmasi, Sodyum stearil fumaratin eklenerek karistirilmasi, f) Toplam karisimin tabletler elde edecek sekilde sikistirilmasi, g) Tabletlerin film kaplama ile kaplanmasi. Örnek 3: Film Kapli Tablet Bilesenler Miktar (toplam bilesim agirligi bakimindan %) Emoksipin veya tuzlari 10.0 - 45.0 Polivinilpirolidon 2.0 - 10.0 Mikrokristalin selüloz 5.0 - 20.0 Prejelatinize nisasta 2.0 - 20.0 Sodyum stearil fumarat 0.25 - 1.5 Film kaplama 2.0 - 5.0 Toplam bilesim 100 Örnek 3'e ait bir proses: a) Emoksipin veya tuzlari, polivinilpirolidon, mikrokristalin nisastanin karistirilmasi, b) Karisimin briket tabletler elde edecek sekilde sikistirilmasi, c) Briket tabletlerin elekten geçirilmesi, d) Sodyum stearil fumaratin eklenerek karistirilmasi, e) Toplam karisimin tabletler elde edecek sekilde sikistirilmasi, f) Tabletlerin film kaplama ile kaplanmasi. TR TR TR TR DESCRIPTION A FILM-COATED TABLET CONTAINING EMOXIPIN Technical Field The present invention relates to a film-coated tablet containing emoxipin or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable excipient. The present invention also relates to a simple, fast, cost-effective, time-saving and industrially convenient process. Background of the Invention Emoxipin is a heteroaromatic antioxidant with membrane-protecting, nootropic and sedative effects. Its aromatic effect area is wide enough to include increasing stress resistance in organisms. While it acts as an anxiolytic without causing drowsiness and myorelaxant effects, its nootropic properties help prevent or reduce learning and memory deficits in elderly patients under pathogenic factors. One of the activities of Emoxipin is the anticonvulsant effect, which exhibits antioxidant and antihypoxic properties. It reduces the toxic effects of alcohol while increasing attention concentration and work capacity. While it prevents peroxide oxidation of lipids, it increases the effect of superoxide oxidase and increases the lipid-protein ratio. It also provides a higher concentration of dopamine in the brain. Its chemical name is 2-ethyl-6-methyl-3-hydroxypyridine and its chemical structure is shown in Formula I Emoxipine is marketed under the brand name MEXIDOL® and is administered orally at a therapeutic dose of 125 to 250 mg three times a day and is administered at lV/ It has injectable formulations containing 50mg/ml in 2 to 5ml ampoules in 1M forms. Emoxipin; It can be used in solid dosage forms that have neuroprotective, antiamnestic, antioxidant, antihypoxic and antiischemic activities. Document WO 96/02238 A1 discloses a neuropathic and sedative formulation comprising emoxipine succinate at the core, excipients and a coating layer. Excipients in the core include kaolin, potato starch, calcium stearate, stearic acid, talc and methyl cellulose. The coating layer contains titanium dioxide and Serge 80. Patent application numbered EP224131O A2 discloses a pharmaceutical formulation comprising emoxipine or a pharmaceutically acceptable salt thereof and a release controlling polymer, together with at least one pharmaceutically acceptable excipient. The disadvantage of Emoxipin is the low stability of the product during its shelf life. Due to this feature, we encounter the use of emoxipin in different drug forms belonging to the state of the art. In the prior art, there are numerous patent applications for a pharmaceutical formulation containing emoxipine or a pharmaceutically acceptable salt thereof. However, there is still a need to improve the formulation to eliminate problems related to the active ingredient. There is a need in the prior art for an improved pharmaceutical composition of emoxipine or a pharmaceutically acceptable salt thereof, with high stability, dissolution rate and excellent pharmacotechnical properties. To overcome the problems mentioned in the present invention, a film-coated tablet containing emoxipine or a pharmaceutically acceptable salt thereof is provided. Moreover, the tablet in question was developed using standard techniques, which is a simple and cost-effective method. Detailed Description of the Invention The main purpose of the present invention is to eliminate the problems caused by emoxipine or its pharmaceutically acceptable salt and to provide additional advantages to the known state of the art. Another purpose of the present invention is; The aim is to produce a film-coated tablet that has excellent pharmacotechnical properties such as fluidity, compressibility and content uniformity and has the desired dissolution profile and stability. According to this embodiment of the present invention there is provided a film-coated tablet comprising emoxipin or its salts and at least one pharmaceutically acceptable excipient, wherein said tablet comprises: I 100% to 450% of emoxipin or its salts by total weight of the formulation, - binders at 20% to 20.0% by weight of the total formulation. According to this embodiment of the present invention, the amount of emoxipine or its salts is between 20.0% and 400% by weight of the total formulation. It is known that emoxipin has stability problems in the state of the art. We have surprisingly succeeded in solving this problem by introducing a film-coated tablet containing emoxipine or its salts in the proportions given above, as well as a binder. Suitable connectors; pregelatinized starch, corn starch, natural gums, gelatin, carbomers, carbomers, carboxymethylcellulose sodium, cellulose acetate phthalate, chitosan, dextrose, estylcellulose, glyceryl behanate, hydroxyethyl cellulose, hydroxyethylmethyl cellulose, hydroxypropyl cellulose, hydroxypropyl magnese, yum aluminum silicate, poloxamer, polycarbophil , polydextrose, polyethylene oxide, polymethacrylates, aluminum hydroxide, cetostearyl alcohol, polyoxyethylene-alkyl ethers, or mixtures thereof. According to this embodiment of the present invention, the amount of binders is between 20% and 20.0% by weight of the total formulation; Most preferably, in terms of total formulation weight, the binder according to this embodiment of the present invention is pregelatinized starch. According to this embodiment of the present invention, the pharmaceutically acceptable salt of emoxipin; emoxipin succinate salt, emoxipin maleate, emoxipin malonate, emoxipin adipate, emoxipin HCl. The pharmaceutically acceptable salt of emoxipin is preferably the succinate salt of emoxipin or emoxipin HCl. 'Particle size' as used herein means the cumulative volume size distribution tested by any conventionally accepted method such as the laser diffraction method (i.e. Malvern Mastersizer 2000 analysis). The term d (0.9) refers to the size at which 90% of the particles by volume are finer. In one embodiment of the present invention, the particle size d (0.9) of emoxipin or its salts is less than 600 µm, preferably less than 500 µm, preferably less than 400 µm, preferably less than 300 µm. Pharmaceutically acceptable excipients according to this embodiment of the present invention; The fillers are selected from the group consisting of lubricants, gliders, or mixtures thereof. Suitable fillers; microcrystalline cellulose, polyvinylpyrrolidone, lactose monohydrate, anhydrous pellet, starch, maltodextrin, dibasic calcium phosphate, or mixtures thereof. Content uniformity is ensured in the formulation thanks to the use of the correct filler. According to this embodiment of the present invention, the amount of fillers is between 50% and 500% by weight of the total formulation. According to this embodiment of the present invention, the amount of fillers is the total formulation weight of the filler according to this embodiment of the present invention; microcrystalline cellulose or polyvinylpyrrolidone or mixtures thereof. The use of the described filler allows the desired dissolution profile to be achieved. Suitable lubricants and glidant; magnesium stearate, sodium stearyl fumarate, colloidal silicon dioxide, calcium stearate, zinc stearate, talc, silicon dioxide, aluminum silicate, calcium silicate, magnesium silicate, magnesium oxide, starch, sodium chlorate, magnesium lauryl sulfate, sodium oleate, sodium acetate, sodium benzoate, polyethylene glycol, stearic acid, fumaric acid, glyceryl palmito sulfate, sodium lauryl sulfate, or mixtures thereof. According to this embodiment of the present invention, the amount of lubricants/glycants is between 025% and 1.5% by weight of the total formulation. According to this embodiment of the present invention, lubricant/glidant; magnesium stearate or sodium stearyl fumarate or mixtures thereof. The use of the described lubricant/glidant allows the desired fluidity to be achieved. Film-coated tablet containing emoxipine or its salts according to the present invention; Using standard techniques or production methods well known in the state of the art, such as direct compression, wet or dry granulation, hot melt granulation, hot melt extrusion, fluidized bed granulation, extrusion/spheronization, pre-compression/double pressing, spray drying and solvent evaporation. can be prepared. According to this embodiment of the present invention, the film-coated tablet; It is prepared by wet or dry granulation or direct printing method. According to this embodiment of the present invention, solvents or co-solvents are used in wet granulation. Suitable solvents or co-solvents; is selected from the group consisting of water, dimethyl sulfoxide, dichloromethane, methanol, acetone, isopropyl alcohol or mixtures thereof. A desired dissolution profile and a desired content uniformity are achieved in the film-coated tablet of the present invention, and the simple production process used is suitable for industrial production. Example 1: Film-Coated Tablet Ingredients Amount (% by weight of total composition) Pregelatinized starch 2.0 - 20.0 (3-15) Magnesium stearate 0.25 - 1.5 (0.2-1.0) Film coating 2.0 - 8.0 (3-7) Total composition 100 Example 1 A process belonging to: a) Mixing Emoxipine or its salts, microcrystalline cellulose, pregelatinized starch by sieving, b) Adding and mixing magnesium stearate, o) Compressing the total mixture to obtain tablets, d) Coating the tablets with film coating. Example 2: Film-Coated Tablet Ingredients Amount (% by weight of total composition) Emoxipine or its salts 10.0 - 45.0 Pregelatinized starch 2.0 - 20.0 Sodium stearyl fumarate 0.25 - 1.5 Film coating 2.0 - 8.0 Total composition 100 A process of Example 2: a) Mixing emoxipine or its salts, half of the polyvinylpyrrolidone, half of the pregelatinized starch, Granulating the prepared powder mixture with solvent/co-solvent, Drying the prepared wet granules, Adding the remaining parts of the starch and polyvinylpyrrolidone to the pregel and mixing, Adding sodium stearyl fumarate and mixing, f) Total tablets of the mixture are obtained g) Coating the tablets with film coating. Example 3: Film-Coated Tablet Ingredients Amount (% by weight of total composition) Emoxipine or its salts 10.0 - 45.0 Polyvinylpyrrolidone 2.0 - 10.0 Microcrystalline cellulose 5.0 - 20.0 Pregelatinized starch 2.0 - 20.0 Sodium stearyl fumarate 0.25 - 1.5 Film coating 2.0 - 5.0 Total composition 100 Samples A process of 3: a) Mixing emoxipine or its salts, polyvinylpyrrolidone, microcrystalline starch, b) Compressing the mixture to obtain briquette tablets, c) Sifting the briquette tablets, d) Mixing by adding sodium stearyl fumarate, e) Mixing the total mixture to obtain tablets. f) Coating the tablets with film coating. TR TR TR TR
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| TR2021/001943A TR2021001943A2 (en) | 2021-02-11 | 2021-02-11 | A film coated tablet comprising emoxypine |
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| TR2021/001943A TR2021001943A2 (en) | 2021-02-11 | 2021-02-11 | A film coated tablet comprising emoxypine |
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