TR201918013A2 - A pellet composition comprising propiverine or a pharmaceutically acceptable salt thereof - Google Patents
A pellet composition comprising propiverine or a pharmaceutically acceptable salt thereof Download PDFInfo
- Publication number
- TR201918013A2 TR201918013A2 TR2019/18013A TR201918013A TR201918013A2 TR 201918013 A2 TR201918013 A2 TR 201918013A2 TR 2019/18013 A TR2019/18013 A TR 2019/18013A TR 201918013 A TR201918013 A TR 201918013A TR 201918013 A2 TR201918013 A2 TR 201918013A2
- Authority
- TR
- Turkey
- Prior art keywords
- pellet
- propiverine
- feature
- composition according
- pellet composition
- Prior art date
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- 239000008188 pellet Substances 0.000 title claims abstract description 74
- 239000000203 mixture Substances 0.000 title claims abstract description 71
- QPCVHQBVMYCJOM-UHFFFAOYSA-N Propiverine Chemical compound C=1C=CC=CC=1C(C=1C=CC=CC=1)(OCCC)C(=O)OC1CCN(C)CC1 QPCVHQBVMYCJOM-UHFFFAOYSA-N 0.000 title claims abstract description 51
- 229960003510 propiverine Drugs 0.000 title claims abstract description 46
- 150000003839 salts Chemical class 0.000 title claims abstract description 19
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 33
- 229960001187 propiverine hydrochloride Drugs 0.000 claims description 25
- HWMFFWCDLWDYGX-UHFFFAOYSA-N n-(4-aminophenyl)furan-2-carboxamide Chemical group C1=CC(N)=CC=C1NC(=O)C1=CC=CO1 HWMFFWCDLWDYGX-UHFFFAOYSA-N 0.000 claims description 24
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 19
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 19
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 19
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 19
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 17
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims description 16
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 16
- 239000003795 chemical substances by application Substances 0.000 claims description 14
- VVQNEPGJFQJSBK-UHFFFAOYSA-N Methyl methacrylate Chemical compound COC(=O)C(C)=C VVQNEPGJFQJSBK-UHFFFAOYSA-N 0.000 claims description 10
- DOOTYTYQINUNNV-UHFFFAOYSA-N Triethyl citrate Chemical compound CCOC(=O)CC(O)(C(=O)OCC)CC(=O)OCC DOOTYTYQINUNNV-UHFFFAOYSA-N 0.000 claims description 10
- 239000000945 filler Substances 0.000 claims description 10
- 239000001069 triethyl citrate Substances 0.000 claims description 10
- 235000013769 triethyl citrate Nutrition 0.000 claims description 10
- VMYFZRTXGLUXMZ-UHFFFAOYSA-N triethyl citrate Natural products CCOC(=O)C(O)(C(=O)OCC)C(=O)OCC VMYFZRTXGLUXMZ-UHFFFAOYSA-N 0.000 claims description 10
- 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 description 9
- 239000008101 lactose Substances 0.000 claims description 9
- 125000005395 methacrylic acid group Chemical group 0.000 claims description 9
- -1 hydroxypropyl Chemical group 0.000 claims description 7
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims description 6
- 239000011230 binding agent Substances 0.000 claims description 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 6
- 239000004014 plasticizer Substances 0.000 claims description 6
- 239000000126 substance Substances 0.000 claims description 6
- 239000000375 suspending agent Substances 0.000 claims description 6
- JIGUQPWFLRLWPJ-UHFFFAOYSA-N Ethyl acrylate Chemical compound CCOC(=O)C=C JIGUQPWFLRLWPJ-UHFFFAOYSA-N 0.000 claims description 5
- 229920002301 cellulose acetate Polymers 0.000 claims description 5
- 239000000314 lubricant Substances 0.000 claims description 5
- PNJWIWWMYCMZRO-UHFFFAOYSA-N pent‐4‐en‐2‐one Natural products CC(=O)CC=C PNJWIWWMYCMZRO-UHFFFAOYSA-N 0.000 claims description 5
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 5
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims description 4
- 239000001856 Ethyl cellulose Substances 0.000 claims description 4
- 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 4
- PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 claims description 4
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims description 4
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 claims description 4
- WNLRTRBMVRJNCN-UHFFFAOYSA-N adipic acid Chemical compound OC(=O)CCCCC(O)=O WNLRTRBMVRJNCN-UHFFFAOYSA-N 0.000 claims description 4
- 239000002270 dispersing agent Substances 0.000 claims description 4
- 235000019325 ethyl cellulose Nutrition 0.000 claims description 4
- 229920001249 ethyl cellulose Polymers 0.000 claims description 4
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims description 4
- 125000005397 methacrylic acid ester group Chemical group 0.000 claims description 4
- 239000003002 pH adjusting agent Substances 0.000 claims description 4
- 239000003961 penetration enhancing agent Substances 0.000 claims description 4
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 3
- 230000002378 acidificating effect Effects 0.000 claims description 3
- 229910000019 calcium carbonate Inorganic materials 0.000 claims description 3
- 235000010216 calcium carbonate Nutrition 0.000 claims description 3
- 235000010980 cellulose Nutrition 0.000 claims description 3
- 229920002678 cellulose Polymers 0.000 claims description 3
- 239000001913 cellulose Substances 0.000 claims description 3
- 150000002148 esters Chemical class 0.000 claims description 3
- 229920000609 methyl cellulose Polymers 0.000 claims description 3
- 235000010981 methylcellulose Nutrition 0.000 claims description 3
- 239000001923 methylcellulose Substances 0.000 claims description 3
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims description 3
- LNAZSHAWQACDHT-XIYTZBAFSA-N (2r,3r,4s,5r,6s)-4,5-dimethoxy-2-(methoxymethyl)-3-[(2s,3r,4s,5r,6r)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxy-6-[(2r,3r,4s,5r,6r)-4,5,6-trimethoxy-2-(methoxymethyl)oxan-3-yl]oxyoxane Chemical compound CO[C@@H]1[C@@H](OC)[C@H](OC)[C@@H](COC)O[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@H]2[C@@H]([C@@H](OC)[C@H](OC)O[C@@H]2COC)OC)O[C@@H]1COC LNAZSHAWQACDHT-XIYTZBAFSA-N 0.000 claims description 2
- OOSZCNKVJAVHJI-UHFFFAOYSA-N 1-[(4-fluorophenyl)methyl]piperazine Chemical compound C1=CC(F)=CC=C1CN1CCNCC1 OOSZCNKVJAVHJI-UHFFFAOYSA-N 0.000 claims description 2
- RSWGJHLUYNHPMX-UHFFFAOYSA-N Abietic-Saeure Natural products C12CCC(C(C)C)=CC2=CCC2C1(C)CCCC2(C)C(O)=O RSWGJHLUYNHPMX-UHFFFAOYSA-N 0.000 claims description 2
- 229920000623 Cellulose acetate phthalate Polymers 0.000 claims description 2
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims description 2
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 claims description 2
- KHPCPRHQVVSZAH-HUOMCSJISA-N Rosin Natural products O(C/C=C/c1ccccc1)[C@H]1[C@H](O)[C@@H](O)[C@@H](O)[C@@H](CO)O1 KHPCPRHQVVSZAH-HUOMCSJISA-N 0.000 claims description 2
- VMHLLURERBWHNL-UHFFFAOYSA-M Sodium acetate Chemical compound [Na+].CC([O-])=O VMHLLURERBWHNL-UHFFFAOYSA-M 0.000 claims description 2
- UIIMBOGNXHQVGW-DEQYMQKBSA-M Sodium bicarbonate-14C Chemical compound [Na+].O[14C]([O-])=O UIIMBOGNXHQVGW-DEQYMQKBSA-M 0.000 claims description 2
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims description 2
- 229920002494 Zein Polymers 0.000 claims description 2
- 229960000583 acetic acid Drugs 0.000 claims description 2
- 239000001361 adipic acid Substances 0.000 claims description 2
- 235000011037 adipic acid Nutrition 0.000 claims description 2
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims description 2
- 229940103272 aluminum potassium sulfate Drugs 0.000 claims description 2
- 239000002775 capsule Substances 0.000 claims description 2
- 229940081734 cellulose acetate phthalate Drugs 0.000 claims description 2
- 239000012362 glacial acetic acid Substances 0.000 claims description 2
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 2
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 2
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 2
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims description 2
- 229920000639 hydroxypropylmethylcellulose acetate succinate Polymers 0.000 claims description 2
- 239000004310 lactic acid Substances 0.000 claims description 2
- 235000014655 lactic acid Nutrition 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
- 239000011976 maleic acid Substances 0.000 claims description 2
- 229940111688 monobasic potassium phosphate Drugs 0.000 claims description 2
- 235000019796 monopotassium phosphate Nutrition 0.000 claims description 2
- 229910000403 monosodium phosphate Inorganic materials 0.000 claims description 2
- 235000019799 monosodium phosphate Nutrition 0.000 claims description 2
- 239000011664 nicotinic acid Substances 0.000 claims description 2
- 235000001968 nicotinic acid Nutrition 0.000 claims description 2
- 229960003512 nicotinic acid Drugs 0.000 claims description 2
- 235000011007 phosphoric acid Nutrition 0.000 claims description 2
- 229940074982 poly(vinylpyrrolidone-co-vinyl-acetate) Drugs 0.000 claims description 2
- 229940100467 polyvinyl acetate phthalate Drugs 0.000 claims description 2
- 229920000915 polyvinyl chloride Polymers 0.000 claims description 2
- 239000004800 polyvinyl chloride Substances 0.000 claims description 2
- GRLPQNLYRHEGIJ-UHFFFAOYSA-J potassium aluminium sulfate Chemical compound [Al+3].[K+].[O-]S([O-])(=O)=O.[O-]S([O-])(=O)=O GRLPQNLYRHEGIJ-UHFFFAOYSA-J 0.000 claims description 2
- BWHMMNNQKKPAPP-UHFFFAOYSA-L potassium carbonate Chemical compound [K+].[K+].[O-]C([O-])=O BWHMMNNQKKPAPP-UHFFFAOYSA-L 0.000 claims description 2
- GNSKLFRGEWLPPA-UHFFFAOYSA-M potassium dihydrogen phosphate Chemical compound [K+].OP(O)([O-])=O GNSKLFRGEWLPPA-UHFFFAOYSA-M 0.000 claims description 2
- OTYBMLCTZGSZBG-UHFFFAOYSA-L potassium sulfate Chemical compound [K+].[K+].[O-]S([O-])(=O)=O OTYBMLCTZGSZBG-UHFFFAOYSA-L 0.000 claims description 2
- 229910052939 potassium sulfate Inorganic materials 0.000 claims description 2
- 235000011151 potassium sulphates Nutrition 0.000 claims description 2
- 229920002379 silicone rubber Polymers 0.000 claims description 2
- 239000001632 sodium acetate Substances 0.000 claims description 2
- 235000017281 sodium acetate Nutrition 0.000 claims description 2
- 229910000029 sodium carbonate Inorganic materials 0.000 claims description 2
- 235000017550 sodium carbonate Nutrition 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
- 235000011083 sodium citrates Nutrition 0.000 claims description 2
- AJPJDKMHJJGVTQ-UHFFFAOYSA-M sodium dihydrogen phosphate Chemical compound [Na+].OP(O)([O-])=O AJPJDKMHJJGVTQ-UHFFFAOYSA-M 0.000 claims description 2
- 229940074545 sodium dihydrogen phosphate dihydrate Drugs 0.000 claims description 2
- 239000011975 tartaric acid Substances 0.000 claims description 2
- 235000002906 tartaric acid Nutrition 0.000 claims description 2
- KHPCPRHQVVSZAH-UHFFFAOYSA-N trans-cinnamyl beta-D-glucopyranoside Natural products OC1C(O)C(O)C(CO)OC1OCC=CC1=CC=CC=C1 KHPCPRHQVVSZAH-UHFFFAOYSA-N 0.000 claims description 2
- 229940001496 tribasic sodium phosphate Drugs 0.000 claims description 2
- 125000005591 trimellitate group Chemical group 0.000 claims description 2
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 claims description 2
- 239000005019 zein Substances 0.000 claims description 2
- 229940093612 zein Drugs 0.000 claims description 2
- 229920002845 Poly(methacrylic acid) Polymers 0.000 claims 1
- 238000010979 pH adjustment Methods 0.000 claims 1
- XNGIFLGASWRNHJ-UHFFFAOYSA-L phthalate(2-) Chemical compound [O-]C(=O)C1=CC=CC=C1C([O-])=O XNGIFLGASWRNHJ-UHFFFAOYSA-L 0.000 claims 1
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 22
- 235000002639 sodium chloride Nutrition 0.000 description 15
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 11
- 235000019359 magnesium stearate Nutrition 0.000 description 11
- 230000007935 neutral effect Effects 0.000 description 10
- 235000015165 citric acid Nutrition 0.000 description 9
- 229940075614 colloidal silicon dioxide Drugs 0.000 description 8
- 229920003152 Eudragit® RS polymer Polymers 0.000 description 7
- FSXVSUSRJXIJHB-UHFFFAOYSA-M ethyl prop-2-enoate;methyl 2-methylprop-2-enoate;trimethyl-[2-(2-methylprop-2-enoyloxy)ethyl]azanium;chloride Chemical compound [Cl-].CCOC(=O)C=C.COC(=O)C(C)=C.CC(=C)C(=O)OCC[N+](C)(C)C FSXVSUSRJXIJHB-UHFFFAOYSA-M 0.000 description 7
- 238000009472 formulation Methods 0.000 description 7
- 229920003151 Eudragit® RL polymer Polymers 0.000 description 6
- 206010020853 Hypertonic bladder Diseases 0.000 description 6
- 208000009722 Overactive Urinary Bladder Diseases 0.000 description 6
- 229940079593 drug Drugs 0.000 description 6
- DNKKLDKIFMDAPT-UHFFFAOYSA-N n,n-dimethylmethanamine;2-methylprop-2-enoic acid Chemical compound CN(C)C.CC(=C)C(O)=O.CC(=C)C(O)=O DNKKLDKIFMDAPT-UHFFFAOYSA-N 0.000 description 6
- 208000020629 overactive bladder Diseases 0.000 description 6
- 229920003139 Eudragit® L 100 Polymers 0.000 description 5
- 229920003134 Eudragit® polymer Polymers 0.000 description 5
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 5
- 239000002552 dosage form Substances 0.000 description 5
- 239000003814 drug Substances 0.000 description 5
- 239000008187 granular material Substances 0.000 description 5
- 239000000454 talc Substances 0.000 description 5
- 235000012222 talc Nutrition 0.000 description 5
- 229910052623 talc Inorganic materials 0.000 description 5
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- 239000013543 active substance Substances 0.000 description 4
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- 239000012729 immediate-release (IR) formulation Substances 0.000 description 4
- 230000035699 permeability Effects 0.000 description 4
- 239000008194 pharmaceutical composition Substances 0.000 description 4
- 229920002785 Croscarmellose sodium Polymers 0.000 description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 3
- 229920003141 Eudragit® S 100 Polymers 0.000 description 3
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 3
- 239000002202 Polyethylene glycol Substances 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- 229920002472 Starch Polymers 0.000 description 3
- 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 description 3
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
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- IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 description 2
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 description 2
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- NIQCNGHVCWTJSM-UHFFFAOYSA-N Dimethyl phthalate Chemical compound COC(=O)C1=CC=CC=C1C(=O)OC NIQCNGHVCWTJSM-UHFFFAOYSA-N 0.000 description 2
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- ZFOZVQLOBQUTQQ-UHFFFAOYSA-N Tributyl citrate Chemical compound CCCCOC(=O)CC(O)(C(=O)OCCCC)CC(=O)OCCCC ZFOZVQLOBQUTQQ-UHFFFAOYSA-N 0.000 description 2
- 208000000921 Urge Urinary Incontinence Diseases 0.000 description 2
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- 239000001506 calcium phosphate Substances 0.000 description 2
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- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 2
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- OSASVXMJTNOKOY-UHFFFAOYSA-N chlorobutanol Chemical compound CC(C)(O)C(Cl)(Cl)Cl OSASVXMJTNOKOY-UHFFFAOYSA-N 0.000 description 2
- 239000011248 coating agent Substances 0.000 description 2
- 229960001681 croscarmellose sodium Drugs 0.000 description 2
- DOIRQSBPFJWKBE-UHFFFAOYSA-N dibutyl phthalate Chemical compound CCCCOC(=O)C1=CC=CC=C1C(=O)OCCCC DOIRQSBPFJWKBE-UHFFFAOYSA-N 0.000 description 2
- 235000011187 glycerol Nutrition 0.000 description 2
- 235000010417 guar gum Nutrition 0.000 description 2
- 239000000665 guar gum Substances 0.000 description 2
- 229960002154 guar gum Drugs 0.000 description 2
- 239000000594 mannitol Substances 0.000 description 2
- 235000010355 mannitol Nutrition 0.000 description 2
- 239000006186 oral dosage form Substances 0.000 description 2
- 238000003825 pressing Methods 0.000 description 2
- 230000008569 process Effects 0.000 description 2
- 235000010413 sodium alginate Nutrition 0.000 description 2
- 239000000661 sodium alginate Substances 0.000 description 2
- 229940005550 sodium alginate Drugs 0.000 description 2
- 235000000346 sugar Nutrition 0.000 description 2
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- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
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- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
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Abstract
Mevcut buluş, oral uygulama için modifiye salımlı olarak formüle edilen, propiverin veya propiverinin farmasötik olarak kabul edilebilir bir tuzunu içeren bir pellet kompozisyonu ile ilgilidir.The present invention relates to a pellet composition containing propiverine or a pharmaceutically acceptable salt of propiverine, formulated as a modified release for oral administration.
Description
TARIFNAME PROPIVERIN VEYA PROPIVERININ FARMAsöTiK OLARAK KABUL EDILEBILIR BIR TUZUNU IÇEREN PELLET KOMPOZISYONU Teknik Alan Mevcut bulus, oral uygulama için modifiye salimli olarak formüle edilen, propiverin veya propiverinin farmasötik olarak kabul edilebilir bir tuzunu içeren bir pellet kompozisyonu ile Teknigin Bilinen Durumu Asiri aktif mesane (AAM) ve iliskili bir bozukluk olan sikisma tipi üriner inkontinans, depolama fonksiyonunun baska bir majör bozuklugunu temsil etmektedir. Bu iki bozukluk, yogun bir istekle (aciliyet) sik idrara çikma ihtiyaci (siklik) ve gece idrara çikma ihtiyaci (noktüri) ile karakterizedir. Stres tipi üriner inkontinansin aksine, AAM ve sikisma tipi üriner inkontinans, üretral sfinkter kontrolüyle iliskili olmamakla birlikte, mesane fonksiyonlarinda ve bu fonksiyonlarin düzenlenmesindeki bozukluklarla ilgilidir. DESCRIPTION A PHARMACEUTICALLY ACCEPTABLE PROPIVERIN OR PROPIVERIN PELLET COMPOSITION WITH SALT Technical Area The present invention is propiverine or propiverine formulated as a modified release for oral administration. with a pellet composition containing a pharmaceutically acceptable salt of propiverine. State of the Art Overactive bladder (OAB) and a related disorder, urge urinary incontinence, represents another major impairment of the storage function. These two disorders an intense desire (urgency) to urinate frequently (frequently) and the need to urinate at night It is characterized by nocturia. Unlike stress urinary incontinence, OAB and urge urinary incontinence Although incontinence is not related to urethral sphincter control, it can affect bladder functions and It is related to disorders in the regulation of these functions.
Antimuskarinik ajanlar dahil birçok ilaç sinifi, asiri aktif mesane tedavisinde ve yönetiminde kullanilmistir. Etkilerini muskarinik reseptörler üzerinde gösteren ve mesane duvari düz kaslarinin (detrusor) istemsiz kasilma siddetini baskilayan veya azaltan antimuskarinik ajanlar, AAM için ilk tercih edilen farmakoterapi olup, etkililigi sorgulanmayan tek tedavi olabilir. Propiverin hidroklorür, kapsamli olarak incelenmis bir antimuskarinik ve kalsiyum kanal blokeri ajandir. Many drug classes, including antimuscarinic agents, are used in the treatment and management of overactive bladder. used. The bladder wall is flat and shows its effects on muscarinic receptors. antimuscarinic, which suppresses or reduces the intensity of involuntary contraction of the muscles (detrusor) agents are the first-choice pharmacotherapy for OAB and the only treatment whose efficacy is not questioned. it could be. Propiverine hydrochloride is an extensively studied antimuscarinic and calcium channel blocking agent.
Propiverin, asiri aktif mesane ve üriner inkontinans tedavisinde en sik kullanilan reçeteli antimuskarinik ilaçtir. Propiverinin kimyasal adi (I-metil-4-piperidil difenilpropoksiasetat) olup, Formül l'de gösterildigi gibi bir benzilik asit türevidir. Propiverine is the most commonly used prescription drug for the treatment of overactive bladder and urinary incontinence. It is an antimuscarinic drug. The chemical name of propiverine is (I-methyl-4-piperidyl diphenylpropoxyacetate), It is a benzylic acid derivative as shown in formula I.
Propiverin, BCS (Biyofarmasötik Siniflandirma Sistemi) Sinif lll'e dahil bir ilaç olup, düsük geçirgenlige ve yüksek çözünürlüge sahiptir. Propiverine is a BCS (Biopharmaceutical Classification System) Class III drug. It has permeability and high resolution.
Mictonorm gibi hizli salimli oral dozaj formlari seklinde preparatlar olarak hidroklorür tuzu formundaki propiverin, yillardir piyasada mevcuttur. Simdiye kadar kullanilan dozajlar, örnegin günde üç kez alinan 15 mg propiverin- hidroklorür içeren Mictonorm hapinin her biri, tekrarlayan günlük pikler sergileyen nispeten oldukça fazla dalgalanan kan düzeylerine neden olur. Propiverinin antikolinerjik etkisi nedeniyle, kan düzeyindeki hizli artisla birlikte akomodasyon bozukluklari gibi tipik antikolinerjik yan etkileri de kabul edilmelidir. Dolayisiyla, bu yan etkiler 10 ile 20 mg modifiye olmayan, hizli salimli dozaj formlarinin mümkün olan birim doz miktarini kisitlamaktadir. Hydrochloride salt as preparations in the form of immediate-release oral dosage forms such as Mictonorm form of propiverine has been commercially available for years. The dosages used so far, For example, each of the Mictonorm pills containing 15 mg of propiverine-hydrochloride, taken three times a day, relatively highly fluctuating blood levels exhibiting recurrent daily peaks causes. Due to the anticholinergic effect of propiverine, with the rapid increase in blood level Typical anticholinergic side effects such as accommodation disorders should also be acknowledged. Therefore, These side effects are possible with 10 to 20 mg unmodified, immediate-release dosage forms. It limits the amount of unit dose.
Hidroklorür tuzu formundaki propiverin halihazirda çabuk salimli (IR) ve modifiye salimli (MR) olmak üzere iki farkli dozaj formu halinde Apogepha Arzneimittel GmbH tarafindan Mictonorm®f Detrunorm®l Proprinorm® ticari adlariyla pazarlanmaktadir. propiverin veya propiverinin farmasötik olarak kabul edilebilir bir tuzunu içeren oral farmasötik bir kompozisyon ortaya konmaktadir. Önceki teknikte de propiverin veya propiverinin farmasötik olarak kabul edilebilir bir tuzunu içeren oral farmasötik dozaj formlarinin ortaya kondugu birkaç patent bulunmaktadir. Propiverine in the form of its hydrochloride salt is currently available in immediate-release (IR) and modified-release (MR) by Apogepha Arzneimittel GmbH in two different dosage forms. It is marketed under the trade names Mictonorm®f Detrunorm®l Proprinorm®. oral containing propiverine or a pharmaceutically acceptable salt of propiverine A pharmaceutical composition is disclosed. In the prior art, propiverine or a pharmaceutically acceptable salt of propiverine is used. There are several patents describing oral pharmaceutical dosage forms containing
Bununla birlikte, teknikteki formülasyonlarin birçogu, ilacin üretim maliyetini artirabilecek karmasik tekniklerle formüle edilmekte olup, etkin maddenin fizikokimyasal özellikleri göz önünde bulundurulmadan olusturulmustur. However, many of the formulations in the art can increase the production cost of the drug. It is formulated with complex techniques and the physicochemical properties of the active substance are observed. created without consideration.
Bu nedenle, önceki teknikte yukarida açiklanan sorunlari ortadan kaldiran ve bunlara ek avantajlar getiren, propiverin veya propiverinin farmasötik olarak kabul edilebilir bir tuzunu içeren bir kompozisyona hala ihtiyaç bulunmaktadir. Therefore, in the prior art, which eliminates the above-described problems and in addition to these propiverine or a pharmaceutically acceptable salt of propiverine There is still a need for a composition containing
Bulusun Ayrintili Açiklamasi Mevcut bulusun esas amaci, bir pellet kompozisyonu kullanilarak yüksek stabilite saglanmis, propiverin veya propiverinin farmasötik olarak kabul edilebilir bir tuzunu içeren bir kompozisyonunun sunulmasidir. Detailed Description of the Invention The main object of the present invention is to achieve high stability using a pellet composition, containing propiverine or a pharmaceutically acceptable salt of propiverine presenting the composition.
Bulusun baska bir amaci, bu tür bir tedaviye ihtiyaci olan bir hastaya yirmi dört saatlik (24sa) bir süre boyunca sürekli ve terapötik düzeyde propiverin veya propiverinin farmasötik olarak kabul edilebilir bir tuzunu saglayabilen modifiye salimli bir dozaj formülasyonunun elde edilmesidir. Daha spesifik olarak, mevcut bulus propiverin veya propiverinin farmasötik olarak kabul edilebilir bir tuzunu içeren pellet formunda bir oral dozaj formuyla ilgili olup, etkin maddenin salimi, pH ayarlayicilarin varliginda bir salim modifiye edici ajanla kontrol edilmektedir. kari dolasiminda ilacin sabit seviyelerde kalmasini saglayan farmasötik formülasyonlar için kullanilir. Modifiye salim, etkin maddeyi, 12 ila 24 saatlik bir süre boyunca yavas yavas ve öngörülebilir sekilde serbest birakmak üzere formüle edilmistir. It is another object of the invention to provide a twenty-four hour (24h) treatment to a patient in need of such treatment. continuous and therapeutic level of propiverine or propiverine pharmaceutically over a period of time obtaining a modified-release dosage formulation that can provide an acceptable salt is to be done. More specifically, the present invention describes propiverine or propiverine as a pharmaceutical. Relating to an oral dosage form in pellet form containing an acceptable salt of the release of the substance is controlled with a release modifying agent in the presence of pH adjusters is being done. For pharmaceutical formulations that maintain constant levels of drug in the circulation used. Modified release releases the active substance slowly over a 12 to 24 hour period. It is formulated to release predictably.
Propiverinin veya propiverinin farmasötik olarak kabul edilebilir bir tuzunun fizikokimyasal özellikleri nedeniyle modifiye salimli bir formülasyon yapilmasina uygun degildir. Bunun nedeni, propiverinin veya propiverinin farmasötik olarak kabul edilebilir bir tuzunun, özellikle de propiverin hidroklorürün kullanilan eksipiyanlara ve çevresel kosullara karsi hassas olmasidir. Bu nedenle, modifiye salim için kullanilan polimerler ve adimlar mevcut bulusta önemlidir. The physicochemical properties of propiverine or a pharmaceutically acceptable salt of propiverine Due to its properties, it is not suitable for a modified release formulation. This The reason is that propiverine or a pharmaceutically acceptable salt of propiverine, especially Also, propiverine hydrochloride is sensitive to the excipients used and environmental conditions. is that. Therefore, the polymers and steps used for modified release are in the present invention. is important.
Pelletler geçimsiz etkin maddeleri iletmek üzere karistirilabilir. Pellet formülasyonlarinin tekrarlanabilirligi, tek birim dozaj formlarinin tekrarlanabilirliginden çok daha iyidir. Bunlar düsük yüzey alani-hacim oranlari itibariyla film kaplama için uygun sistemlerdir. Ayrica, pellet formülasyonlarinin avantajli özelliklerinden birisi, nem, hava ve isik gibi dis faktörlere karsi iyi direnç göstermeleridir. Pelletler ayrica mükemmel akis özelliklerine sahiptir. Bu avantajlar göz önünde bulunduruldugunda, propiverin içeren formülasyonlarda kullanim için en uygun form pellet formudur. Pellets can be mixed to deliver incompatible active substances. Pellet formulations Its repeatability is much better than that of single unit dosage forms. These They are suitable systems for film coating due to their low surface area-volume ratios. Also, pellets One of the advantageous features of the formulations is that they are good against external factors such as humidity, air and light. their resistance. The pellets also have excellent flow properties. These advantages considered, it is the most suitable for use in formulations containing propiverine. form is pellet form.
Mevcut bulusun bir uygulamasina göre, pellet kompozisyonu propiverin veya propiverinin farmasötik olarak kabul edilebilir bir tuzunu içermekte olup, pellet kompozisyonu modifiye salimli olarak formüle edilmektedir. According to one embodiment of the present invention, the pellet composition is propiverine or propiverin. contains a pharmaceutically acceptable salt of which the pellet composition is modified. It is formulated as a release.
Mevcut bulusun bir uygulamasina göre, propiverin veya propiverinin farmasötik olarak kabul edilebilir bir tuzu propiverin hidroklorürdür. According to one embodiment of the present invention, propiverine or propiverine is pharmaceutically acceptable. An acceptable salt of it is propiverine hydrochloride.
Mevcut bulusun bir uygulamasina göre, propiverin hidroklorür miktari pelletin agirliginca Mevcut bulusun bir uygulamasina göre, propiverin hidroklorür pellet disinda da bulunmaktadir. According to one embodiment of the present invention, the amount of propiverine hydrochloride is based on the weight of the pellet. According to one embodiment of the present invention, besides propiverine hydrochloride pellet, are available.
Mevcut bulusun bir uygulamasina göre, propiverin hidroklorür miktari toplam kompozisyonda Mevcut bulusun bir uygulamasina göre, pelletler ayrica en az bir salim modifiye edici ajan içermektedir. According to one embodiment of the present invention, the amount of propiverine hydrochloride is in the total composition. According to one embodiment of the present invention, the pellets also contain at least one release modifying agent. contains.
Uygun salim modifiye edici ajanlar, poli(metakrilik asit-ko-metilmetakrilat), poli(metil akrilat- ko-metil metakrilat-ko-metakrilik asit), etil selüloz, metil selüloz, hidroksipropilmetilselüIoz, selüloz asetat, selüloz asetat ftalat, selüloz asetat trimelitat, hidroksipropil metilselüloz ftalat, hidroksipropil metilselüloz asetat süksinat, poli(metakrilik asit-ko-etilakrilat), polivinilklorür, polivinil asetat ftalat, poli(viniIpirolidon-ko-vinilasetat), silikon elastomerleri, sellak, zein, rosin esterleri veya bunlarin karisimlarini içeren gruptan seçilmektedir. Suitable release modifying agents are poly(methacrylic acid-co-methylmethacrylate), poly(methyl acrylate- co-methyl methacrylate-co-methacrylic acid), ethyl cellulose, methyl cellulose, hydroxypropylmethylcellulose, cellulose acetate, cellulose acetate phthalate, cellulose acetate trimellitate, hydroxypropyl methylcellulose phthalate, hydroxypropyl methylcellulose acetate succinate, poly(methacrylic acid-co-ethylacrylate), polyvinylchloride, polyvinyl acetate phthalate, poly(vinylpyrrolidone-co-vinylacetate), silicone elastomers, sellak, zein, rosin esters or mixtures thereof.
Mevcut bulusun bir uygulamasina göre, salim modifiye edici ajanin miktari pelletin agirliginca Mevcut bulusun bir uygulamasina göre, salim modifiye edici ajanin miktari toplam Mevcut bulusun bir uygulamasina göre, salim modifiye edici ajan poli(metakrilik asit-ko- metilmetakrilat) 1:1 (Eudragit L 100) veya poli(metil akrilat-ko-metil metakrilat-ko-metakrilik asit) 7:3:1'dir (Eudragit F8 30 D) ve bunlar birlikte veya ayri ayri kullanilabilir. According to one embodiment of the present invention, the amount of release modifying agent is equal to the weight of the pellet. According to one embodiment of the present invention, the amount of release modifying agent is total. According to one embodiment of the present invention, the release modifying agent is poly(methacrylic acid-co- methylmethacrylate) 1:1 (Eudragit L 100) or poly(methyl acrylate-co-methyl methacrylate-co-methacrylic acid) 7:3:1 (Eudragit F8 30 D) and they can be used together or separately.
Eksipiyanlarin optimum miktarlari, örnegin ilgili karisimlarin kompozisyonu, mesela istenen geciktirme etkisi, spesifik bir çözünürlüge ve geçirgenlige sahip salim modifiye edici ajanin türü ve asidik maddenin etkin madde propiverine orani gibi çesitli faktörlere baglidir. Bu parametreler tamamen birbirlerinden bagimsiz olarak degiskenlik göstermekte olup, propiverinin kontrollü ve uzun süreli modifiye salimi için oldukça yüksek önem teskil etmektedir. Optimum amounts of excipients, eg the composition of the respective mixtures, eg desired The delaying effect is due to the release-modifying agent having a specific solubility and permeability. It depends on various factors, such as the type and the ratio of the acidic substance to the active substance propiverine. This parameters vary completely independently of each other, very high importance for controlled and prolonged modified release of propiverine is doing.
Mevcut bulusun bir uygulamasina göre, tercih edilen dozaj formlari, daha uygun ve uygulanmasi daha kolay oldugundan, pelletlerle doldurulmus tablet veya kapsül seklindedir. According to one embodiment of the present invention, preferred dosage forms are more convenient and It is in the form of tablets or capsules filled with pellets, as it is easier to administer.
Mevcut bulusun bir uygulamasina göre, kompozisyon tablet formundadir. Pellet bir tabletin içinde yer alir. According to one embodiment of the present invention, the composition is in tablet form. A pellet of a tablet is located in.
Mevcut bulusun bir uygulamasina göre, tablet ayrica dolgu maddeleri, pH ayarlayicilar, baglayicilar, dagiticilar, plastiklestiriciler, lubrikanlar, glidantlar, süspansiyon ajanlari, geçirgenlik arttirici ajanlar veya bunlarin karisimlarini içeren gruptan seçilen en az bir farmasötik olarak kabul edilebilir eksipiyan içermektedir. According to one embodiment of the present invention, the tablet may also contain fillers, pH adjusters, binders, dispersants, plasticizers, lubricants, glidants, suspending agents, at least one selected from the group consisting of permeation enhancing agents or mixtures thereof. Contains pharmaceutically acceptable excipient.
Uygun dolgu maddeleri, nötral mikrokristalin selüloz pelletler, laktoz, mikrokristalin selüloz, amonyum aliinat, kalsiyum karbonat, kalsiyum fosfat, kalsiyum fosfat dehidrat, kalsiyum sülfat, selüloz, selüloz asetat, sikistirilabilir seker, dekstratlar, dekstrin, dekstroz, eritritol, etilselüloz, fruktoz, izomalt, mannitol, magnezyum karbonat, magnezyum oksit, maltodekstrin, maltoz, orta zincirli trigliseritler, polidekstroz, polimetakrilatlar, sodyum aljinat, sodyum klorür, sorbitol, nisasta, sukroz, seker küreleri, sülfobütileter beta-siklodekstrin, kitre, trehaloz, polisorbat 80, ksilitol veya bunlarin karisimlarini içeren gruptan seçilmektedir. Suitable fillers are neutral microcrystalline cellulose pellets, lactose, microcrystalline cellulose, ammonium aliinate, calcium carbonate, calcium phosphate, calcium phosphate dehydrate, calcium sulfate, cellulose, cellulose acetate, compressible sugar, dextrates, dextrin, dextrose, erythritol, ethylcellulose, fructose, isomalt, mannitol, magnesium carbonate, magnesium oxide, maltodextrin, maltose, medium chain triglycerides, polydextrose, polymethacrylates, sodium alginate, sodium chloride, sorbitol, starch, sucrose, sugar spheres, sulfobutylether beta-cyclodextrin, tragacanth, trehalose, polysorbate 80, xylitol or mixtures thereof.
Mevcut bulusun bir uygulamasina göre, dolgu maddelerinin miktari pelletin agirliginca %50 Mevcut bulusun bir uygulamasina göre, dolgu maddelerinin miktari, toplam kompozisyonun arasindadir. According to one embodiment of the present invention, the amount of fillers is 50% by weight of the pellet. According to one embodiment of the present invention, the amount of fillers is equal to the total composition. are in between.
Mevcut bulusun bir uygulamasina göre, dolgu maddesi, nötral mikrokristalin selüloz pelletleri veya laktoz veya mikrokristalin selüloz veya bunlarin karisimlaridir. According to one embodiment of the present invention, the filler is neutral microcrystalline cellulose pellets. or lactose or microcrystalline cellulose or mixtures thereof.
Mevcut bulusun bir uygulamasina göre, dolgu maddelerinin propiverin hidroklorür ile etkilesime girmesini engellemek amaciyla bu maddeler mümkün oldugunca inert olmali ve sadece propiverin hidroklorür iletimini saglamak için bir tasici olarak islev görmelidir. According to one embodiment of the present invention, fillers are combined with propiverine hydrochloride. These substances should be as inert as possible to avoid interactions and only propiverine should act as a carrier to ensure hydrochloride delivery.
Dolayisiyla, nötral mikrokristalin selüloz pelletleri, örnegin propiverin hidroklorürün çözünürlügünü arttirarak, dissolüsyonu iyilestirerek ve stabiliteyi arttirarak formülasyonu desteklemektedir. Bu nedenle pelletler içerisinde dolgu maddesi olarak mikrokristalin selüloz pelletleri kullanilmaktadir. Thus, neutral microcrystalline cellulose pellets can be used, for example, of propiverine hydrochloride. formulation by increasing its solubility, improving dissolution, and increasing stability. supports. Therefore, microcrystalline cellulose is used as a filler in pellets. pellets are used.
Tercih edilen bulusa konu kompozisyonlar, 6.65'ten düsük bir pKa degerine sahip, farmasötik olarak kabul edilebilir en az bir organik veya inorganik asit içermektedir. Asidik bilesik, mevcut propiverin tuzunun türünden bagimsiz olarak tüm bagirsak kanalinda yeterli bir salim saglayacak sekilde propiverin ve asit arasinda bir quasi iyon çifti olusturarak, propiverin ve tuzlarinin pH'tan bagimsiz çözünürlügünü saglamak amaciyla kullanilir. Preferred compositions of the invention are pharmaceutical compositions having a pKa of less than 6.65. It contains at least one organic or inorganic acid that is acceptable. acidic compound, an adequate release in the entire intestinal tract, regardless of the type of propiverine salt present. by forming a quasi ion pair between propiverine and acid, providing propiverine and It is used to provide solubility of salts independent of pH.
Uygun pH ayarlayicilar, sitrik asit, alüminyum potasyum sülfat, potasyum karbonat, susuz sodyum dihidrojen fosfat, dibazik potasyum sülfat, kalsiyum karbonat, nikotinik asit, seyreltik hidroklorik asit, glasiyal asetik asit, Iaktik asit, maleik asit, monobazik potasyum fosfat, fosforik asit, adipik asit, sodyum asetat, sodyum bikarbonat, sodyum karbonat, sodyum sitrat, sodyum dihidrojen fosfat dihidrat, tartarik asit, tribazik sodyum fosfat veya bunlarin karisimlarini içeren gruptan seçilmektedir. Suitable pH adjusters, citric acid, aluminum potassium sulfate, potassium carbonate, anhydrous sodium dihydrogen phosphate, dibasic potassium sulfate, calcium carbonate, nicotinic acid, dilute hydrochloric acid, glacial acetic acid, lactic acid, maleic acid, monobasic potassium phosphate, phosphoric acid, adipic acid, sodium acetate, sodium bicarbonate, sodium carbonate, sodium citrate, sodium dihydrogen phosphate dihydrate, tartaric acid, tribasic sodium phosphate or their selected from the group containing the mixtures.
Mevcut bulusun bir uygulamasina göre, asidik maddenin (pH ayarlama ajani) propiverin veya propiverinin farmasötik olarak kabul edilebilir bir tuzuna agirlikça orani 0.1 ve 6.0, 0.5 ile 5.0, 1.0 ile 4.0 veya tercihen 1.5 ile 3.5 arasindadir. According to one embodiment of the present invention, the acidic substance (pH adjusting agent) is propiverine or 0.1 to 6.0, 0.5 to 5.0, by weight of propiverine to a pharmaceutically acceptable salt It is between 1.0 and 4.0, or preferably between 1.5 and 3.5.
Mevcut bulusun bir uygulamasina göre, pH ayarlama maddelerinin miktari pelletin agirliginca Mevcut bulusun bir uygulamasina göre, pH ayarlayicilarin miktari, toplam kompozisyonun Mevcut bulusun bir uygulamasina göre, pH ayarlayici sitrik asittir. According to one embodiment of the present invention, the amount of pH adjusting agents is equal to the weight of the pellet. According to one embodiment of the present invention, the amount of pH adjusters is equal to the total composition. According to one embodiment of the present invention, the pH adjuster is citric acid.
Uygun baglayicilar, polivinilpirolidon, sekerler, glukoz surubu, dogal zamklar, jelatin, agar, aljinatlar, kopovidon, sodyum aljinat, guar zamki, nisasta zamki, arap zamki, bentonit, asit veya bunlarin karisimlarini içeren gruptan seçilmektedir. Suitable binders, polyvinylpyrrolidone, sugars, glucose syrup, natural gums, gelatin, agar, alginates, copovidone, sodium alginate, guar gum, gum starch, gum arabic, bentonite, acid or mixtures thereof.
Mevcut bulusun bir uygulamasina göre, baglayicilarin miktari pelletin agirliginca %10 ile Mevcut bulusun bir uygulamasina göre, baglayicilarin miktari, toplam kompozisyonun Mevcut bulusun bir uygulamasina göre baglayici, polivinilpirolidondur. According to one embodiment of the present invention, the amount of binders is 10% by weight of the pellet. According to one embodiment of the present invention, the amount of binders is equal to the total composition. According to one embodiment of the present invention, the binder is polyvinylpyrrolidone.
Uygun plastiklestiriciler, polietilen glikol, trietil sitrat, triasetin, tribütil sitrat, klorobütanol, dibütil ftalat, dibütil sebasat, dimetil ftalat, gliserin, mannitol, petrolatum, Ianolin alkolleri veya bunlarin karisimlarini içeren gruptan seçilmektedir. Suitable plasticizers are polyethylene glycol, triethyl citrate, triacetin, tributyl citrate, chlorobutanol, dibutyl phthalate, dibutyl sebacate, dimethyl phthalate, glycerine, mannitol, petrolatum, Ianoline alcohols or selected from the group containing mixtures of these.
Mevcut bulusun bir uygulamasina göre, plastiklestiricilerin miktari pelletin agirliginca %005 ile %50 ve %0.5 ile %30 arasindadir. According to one embodiment of the present invention, the amount of plasticizers is 005% by weight of the pellet. between 50% and 0.5% and 30%.
Mevcut bulusun bir uygulamasina göre, plastiklestiricilerin miktari toplam kompozisyonun Mevcut bulusun bir uygulamasina göre plastiklestirici, trietil sitrattir. According to one embodiment of the present invention, the amount of plasticizers exceeds the total composition. According to one embodiment of the present invention, the plasticizer is triethyl citrate.
Uygun dagiticilar, kroskarmelloz sodyum, karboksimetil selüloz, sodyum karboksimetil selüloz, çapraz bagli sodyum karboksimetil selüloz, kalsiyum karboksimetil selüloz, sodyum karboksimetil nisasta veya bunlarin karisimlarini içeren gruptan seçilmektedir. Suitable dispersants are croscarmellose sodium, carboxymethyl cellulose, sodium carboxymethyl cellulose, cross-linked sodium carboxymethyl cellulose, calcium carboxymethyl cellulose, sodium is selected from the group consisting of carboxymethyl starch or mixtures thereof.
Mevcut bulusun bir uygulamasina göre, dagitici miktari, toplam kompozisyonun agirliginca Uygun lubrikanlar, magnezyum stearat, sodyum stearil fumarat, polietilen glikol, sodyum lauril sülfat, magnezyum laurii sülfat, fumarik asit, gliseril palmitostearat, hidrojene dogal yaglar, çinko stearat, kalsiyum stearat, silika, talk, stearik asit, polietilen glikol, parafin veya bunlarin karisimlarini içeren bir gruptan seçilmektedir. Tercihen lubrikan, magnezyum stearatti r. According to one embodiment of the present invention, the amount of dispersant is by weight of the total composition. Suitable lubricants are magnesium stearate, sodium stearyl fumarate, polyethylene glycol, sodium lauryl sulfate, magnesium laurii sulfate, fumaric acid, glyceryl palmitostearate, hydrogenated natural oils, zinc stearate, calcium stearate, silica, talc, stearic acid, polyethylene glycol, paraffin or selected from a group containing mixtures of these. Preferably lubricant, magnesium stearate r.
Mevcut bulusun bir uygulamasina göre, Iubrikanlarin miktari, toplam kompozisyonun agirliginca %005 ile %50 arasinda, %05 ile %30 arasindadir. According to one embodiment of the present invention, the amount of lubricans is equal to that of the total composition. It is between 005% and 50%, between 05% and 30% by weight.
Mevcut bulusun bir uygulamasina göre lubrikan, magnezyum stearattir. According to one embodiment of the present invention, the lubricant is magnesium stearate.
Uygun glidantlar, kolloidal silikon dioksit, suda çözünen eksipiyan, hidrofilik polimerler, silikon dioksit veya bunlarin karisimlarini içeren gruptan seçilmektedir. Suitable glidants, colloidal silicon dioxide, water-soluble excipient, hydrophilic polymers, silicone dioxide or mixtures thereof.
Mevcut bulusun bir uygulamasina göre, glidant miktari toplam kompozisyonun agirliginca Mevcut bulusun bir uygulamasina göre glidant, kolloidal silikon dioksittir. According to one embodiment of the present invention, the amount of glidant is by weight of the total composition. According to one embodiment of the present invention, the glidant is colloidal silicon dioxide.
Uygun süspansiyon maddeleri, talk, ksantan zamki, guar zamki, gliserol, polivinil alkol, polivinil pirolidon, polietilen oksit, selüloz türevleri, etilselüloz, hidroksietilselüloz, hidroksietilmetilseloz veya bunlarin karisimlarini içeren gruptan seçilmektedir. Suitable suspending agents are talc, xanthan gum, guar gum, glycerol, polyvinyl alcohol, polyvinyl pyrrolidone, polyethylene oxide, cellulose derivatives, ethylcellulose, hydroxyethylcellulose, hydroxyethylmethylcellulose or mixtures thereof.
Mevcut bulusun bir uygulamasina göre, süspansiyon maddesi talktir. According to one embodiment of the present invention, the suspending agent is talc.
Mevcut bulusun bir uygulamasina göre, süspansiyon maddesinin miktari pelletin agirliginca Mevcut bulusun bir uygulamasina göre, süspansiyon maddesinin miktari toplam kompozisyonun agirliginca %05 ile %100 ve %10 ile %80 arasindadir. According to one embodiment of the present invention, the amount of suspending agent is equal to the weight of the pellet. According to one embodiment of the present invention, the amount of suspending agent is total between 05% and 100% and between 10% and 80% by weight of the composition.
Uygun geçirgenlik arttirici ajanlar, etil akrilat, metil metakrilat ve az miktarda metakrilik asit esteri, etanol, izopropil alkol, propilen glikol veya bunlarin karisimlarini içeren gruptan seçilmektedir. Suitable permeation enhancing agents are ethyl acrylate, methyl methacrylate and a small amount of methacrylic acid. ester, ethanol, isopropyl alcohol, propylene glycol or mixtures thereof. is selected.
Propiverin, BCS (Biyofarmasötik Siniflandirma Sistemi) Sinif lll'e dahil bir ilaç olup, düsük geçirgenlige sahiptir. Dolayisiyla, geçirgenlik arttirici ajanlarin kullanilmasi önemlidir. Propiverine is a BCS (Biopharmaceutical Classification System) Class III drug. It has permeability. Therefore, it is important to use permeation increasing agents.
Mevcut bulusun bir uygulamasina göre, geçirgenlik arttirici ajanlarin miktari pelletin agirliginca %05 ile %6.0 ve %1.0 ile %4.0 arasindadir. According to one embodiment of the present invention, the amount of permeation increasing agents It is between 05% and 6.0% and between 1.0% and 4.0% by weight.
Mevcut bulusun bir uygulamasina göre, geçirgenlik arttirici ajanlarin miktari toplam kompozisyonun agirliginca %0.05 ile %4.0 ve %0.1 ile %20 arasindadir. According to one embodiment of the present invention, the amount of permeation enhancing agents is between 0.05% and 4.0% and between 0.1% and 20% by weight of the composition.
Mevcut bulusun bir uygulamasina göre, geçirgenlik arttirici ajan etil akrilat veya metil metakrilat veya az miktarda metakrilik asit esteri (Eudragit RS veya Eudragit RL) veya bunlarin karisimlaridir. According to one embodiment of the present invention, the permeability enhancing agent is ethyl acrylate or methyl methacrylate or a small amount of methacrylic acid ester (Eudragit RS or Eudragit RL), or are mixtures of these.
Bahsedilen farmasötik kompozisyon, direkt baski veya kuru granülasyon ya da yas granülasyon sonrasinda tablet seklinde basilmaktadir. Tabletler konvansiyonel olarak film kapli olabilir. Said pharmaceutical composition can be used in direct press or dry granulation or flat It is pressed in tablet form after granulation. Tablets are conventionally film may be covered.
Mevcut bulusun bir uygulamasina göre, pelletler asagidakileri içermektedir: o Propiverin hidroklorür o Nötral mikrokristalin selüloz pelleti o Sitrik asit o Polivinilpirolidon o Laktoz o Etil akrilat veya metil metakrilat veya az miktarda metakrilik asit esteri (Eudragit RS veya Eudragit RL) o Poli(metakrilik asit-ko-metilmetakrilat) . POIi(metakrilik asit-ko-metilmetakrilat) o P0li(metil akrilat-ko-metil metakrilat-ko-metakrilik asit) o Trietilsitrat o Magnezyum stearat Mevcut bulusun bir uygulamasina göre tablet, asagidakileri içermektedir: . Propiverin hidroklorür o Nötral mikrokristalin selüloz pelleti . Sitrik asit o Polivinilpirolidon o Laktoz o Etil akrilat veya metil metakrilat veya az miktarda metakrilik asit esteri (Eudragit RS veya Eudragit RL) o POIi(metakrilik asit-ko-metilmetakrilat) . POIi(metakrilik asit-ko-metilmetakrilat) . POIi(metil akrilat-ko-metil metakrilat-ko-metakrilik asit) o Trietilsitrat o Magnezyum stearat . Kolloidal silikon dioksit ÖRNEK 1: PROPIVERIN HIDROKLORÜR BARINDIRAN PELLETLER IÇEREN BIR Içerik maddeleri (%) Miktar (ala) Propiverin hidroklorür 1.0 - 30.0 Nötral mikrokristalin selüloz pelleti 0.5 - 30.0 Sitrik asit 2.0- 40.0 Polivinilpirolidon 0.5 - 15.0 Laktoz 0.01 - 20.0 Eudragit RS 0.01 - 20.0 g Eudragit RL 0.01 - 20.0 Eudragit S 100 0.01 - 20.0 Eudragit L 100 0.01 - 20.0 Eudragit F8 30 D 0.01 - 20.0 Trietilsitrat 0.01 - 20.0 Mikrokristalin selüloz Ph101 30.0 - 85.0 Polivinilpirolidon 0.5 - 30.0 Kolloidal silikon dioksit 0.01 - 20.0 Toplam 100 ÖRNEK 2: PROPIVERIN HIDROKLORÜR BARINDIRAN PELLETLER IÇEREN BIR Içerik maddeleri (%) Miktar (ala) Propiverin hidroklorür 1.0 - 15.0 Nötral mikrokristalin selüloz pelleti 1.0 - 7.0 Sitrik asit 5.0- 20.0 Polivinilpirolidon 1.0 - 7.0 Laktoz 0.5-5.0 Eudragit RS 0.01 - 10.0 g Eudragit RL 0.01-10.0 Eudragit S 100 0.01-10.0 Eudragit L 100 0.01-10.0 Eudragit F8 30 D 0.01 - 20.0 Trietilsitrat 0.01 - 10.0 Magnezyum stearat 0.001 - 5.0 Mikrokristalin selüloz Ph101 60.0 - 75.0 Polivinilpirolidon 0.5 - 20.0 Kolloidal silikon dioksit 0.01 -10.0 Magnezyum stearat 0.001 - 5.0 Toplam 100 Örnek 1 veya 2 için proses: Pellet için: a) Propiverin hidroklorür, nötral mikrokristalin selüloz pellet, sitrik asit, polivinilpirolidon, trietilsitrat, talk ve magnezyum stearat bir homojenizatöre eklenir ve karistirilir, b) Ardindan, elde edilen pelletler akiskan yatakli kurutucuya konur, Pellet elde edildikten sonraki adimlar: c) Polivinilpirolidon içeren granülasyon çözeltisi mikrokristalin selüloz Ph101 ile granül haline getirilir, d) Granüller elenir ve nem %03 altina düsene kadar kurutulur, e) Granüller tekrar elenir, f) Kolloidal silikon dioksit ve hazirlanan pelletler eklenir ve karistirilir, g) Magnezyum stearat eklenir ve karistirilir, h) Ardindan, basilarak tablet olusturulur, i) Tabletler kaplama maddeleri ile kaplanir. ÖRNEK 3: PROPIVERIN HIDROKLORÜR BARINDIRAN PELLETLER IÇEREN BIR Içerik maddeleri (%) Miktar (ala) Propiverin hidroklorür 1.0 - 30.0 Nötral mikrokristalin selüloz pelleti 0.5 - 30.0 Sitrik asit 2.0- 40.0 Polivinilpirolidon 0.5 - 15.0 Laktoz 0.01 - 20.0 Eudragit RS 0.01 - 20.0 Eudragit L 100 0.01 - 20.0 Eudragit F8 30 D 0.01 - 20.0 Trietilsitrat 0.01 - 20.0 Propiverin hidroklorür 1.0 - 15.0 Mikrokristalin selüloz Ph101 30.0 - 85.0 Polivinilpirolidon 0.5 - 30.0 Kolloidal silikon dioksit 0.01 - 20.0 Toplam 100 Örnek 3 için proses: Pellet için: Propiverin hidroklorür, nötral mikrokristalin selüloz pellet, sitrik asit, polivinilpirolidon, laktoz, Eudragit RS, Eudragit RL, Eudragit S 100, Eudragit L 100, Eudragit F8 30 D, trietilsitrat, talk ve magnezyum stearat bir homojenizatöre eklenir ve karistirilir, Ardindan, elde edilen pelletler akiskan yatakli kurutucuya konur, Pellet elde edildikten sonraki adimlar: Polivinilpirolidon içeren granülasyon çözeltisi mikrokristalin selüloz Ph101, kroskarmelloz sodyum ve propiverin hidroklorür ile granül haline getirilir, Granüller elenir ve nem %0.3 altina düsene kadar kurutulur, Granüller tekrar elenir, Kolloidal silikon dioksit ve hazirlanan pelletler eklenir ve karistirilir, Magnezyum stearat eklenir ve karistirilir, Ardindan, basilarak tablet olusturulur, Tabletler kaplama maddeleri ile kaplanir. According to one embodiment of the present invention, pellets include: o Propiverine hydrochloride o Neutral microcrystalline cellulose pellet o Citric acid o Polyvinylpyrrolidone o Lactose o Ethyl acrylate or methyl methacrylate or a small amount of methacrylic acid ester (Eudragit RS or Eudragit RL) o Poly(methacrylic acid-co-methylmethacrylate) . POIi(methacrylic acid-co-methylmethacrylate) o P0li(methyl acrylate-co-methyl methacrylate-co-methacrylic acid) o Triethylcitrate o Magnesium stearate According to one embodiment of the present invention, the tablet contains: . Propiverine hydrochloride o Neutral microcrystalline cellulose pellet . Citric acid o Polyvinylpyrrolidone o Lactose o Ethyl acrylate or methyl methacrylate or a small amount of methacrylic acid ester (Eudragit RS or Eudragit RL) o POIi(methacrylic acid-co-methylmethacrylate) . POIi(methacrylic acid-co-methylmethacrylate) . POIi(methyl acrylate-co-methyl methacrylate-co-methacrylic acid) o Triethylcitrate o Magnesium stearate . colloidal silicon dioxide EXAMPLE 1: A CONTAINING PELLETS CONTAINING PROPIVERINE HYDROCHLORIDE Ingredients (%) Quantity (ala) Propiverine hydrochloride 1.0 - 30.0 Neutral microcrystalline cellulose pellet 0.5 - 30.0 Citric acid 2.0- 40.0 Polyvinylpyrrolidone 0.5 - 15.0 Lactose 0.01 - 20.0 Eudragit RS 0.01 - 20.0 g Eudragit RL 0.01 - 20.0 Eudragit S 100 0.01 - 20.0 Eudragit L 100 0.01 - 20.0 Eudragit F8 30 D 0.01 - 20.0 Triethylcitrate 0.01 - 20.0 Microcrystalline cellulose Ph101 30.0 - 85.0 Polyvinylpyrrolidone 0.5 - 30.0 Colloidal silicon dioxide 0.01 - 20.0 Total 100 EXAMPLE 2: A CONTAINING PELLETS CONTAINING PROPIVERINE HYDROCHLORIDE Ingredients (%) Quantity (ala) Propiverine hydrochloride 1.0 - 15.0 Neutral microcrystalline cellulose pellet 1.0 - 7.0 Citric acid 5.0-20.0 Polyvinylpyrrolidone 1.0 - 7.0 Lactose 0.5-5.0 Eudragit RS 0.01 - 10.0 g Eudragit RL 0.01-10.0 Eudragit S 100 0.01-10.0 Eudragit L 100 0.01-10.0 Eudragit F8 30 D 0.01 - 20.0 Triethylcitrate 0.01 - 10.0 Magnesium stearate 0.001 - 5.0 Microcrystalline cellulose Ph101 60.0 - 75.0 Polyvinylpyrrolidone 0.5 - 20.0 Colloidal silicon dioxide 0.01 -10.0 Magnesium stearate 0.001 - 5.0 Total 100 Process for example 1 or 2: For the pellet: a) Propiverine hydrochloride, neutral microcrystalline cellulose pellet, citric acid, polyvinylpyrrolidone, triethylcitrate, talc and magnesium stearate are added to a homogenizer and mixed, b) Afterwards, the pellets obtained are placed in a fluidized bed dryer, Steps after the pellet is obtained: c) Granulation solution containing polyvinylpyrrolidone granulate with microcrystalline cellulose Ph101 is made into, d) The granules are sieved and dried until the humidity drops below 03%, e) Granules are sieved again, f) Colloidal silicon dioxide and prepared pellets are added and mixed, g) Magnesium stearate is added and mixed, h) Then, a tablet is formed by pressing, i) Tablets are coated with coating agents. EXAMPLE 3: A CONTAINING PELLETS CONTAINING PROPIVERINE HYDROCHLORIDE Ingredients (%) Amount (take) Propiverine hydrochloride 1.0 - 30.0 Neutral microcrystalline cellulose pellet 0.5 - 30.0 Citric acid 2.0- 40.0 Polyvinylpyrrolidone 0.5 - 15.0 Lactose 0.01 - 20.0 Eudragit RS 0.01 - 20.0 Eudragit L 100 0.01 - 20.0 Eudragit F8 30 D 0.01 - 20.0 Triethylcitrate 0.01 - 20.0 Propiverine hydrochloride 1.0 - 15.0 Microcrystalline cellulose Ph101 30.0 - 85.0 Polyvinylpyrrolidone 0.5 - 30.0 Colloidal silicon dioxide 0.01 - 20.0 Total 100 Process for Example 3: For the pellet: Propiverine hydrochloride, neutral microcrystalline cellulose pellet, citric acid, polyvinylpyrrolidone, lactose, Eudragit RS, Eudragit RL, Eudragit S 100, Eudragit L 100, Eudragit F8 30 D, triethylcitrate, talc and magnesium stearate are added to a homogenizer and mixed, Afterwards, the obtained pellets are placed in a fluidized bed dryer, Steps after the pellet is obtained: Granulation solution containing polyvinylpyrrolidone microcrystalline cellulose Ph101, granulated with croscarmellose sodium and propiverine hydrochloride, The granules are sieved and dried until the humidity drops below 0.3%, The granules are sieved again, Colloidal silicon dioxide and prepared pellets are added and mixed, Magnesium stearate is added and mixed, Then, the tablet is formed by pressing, Tablets are coated with coating agents.
Claims (1)
Priority Applications (8)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| TR2019/18013A TR201918013A2 (en) | 2019-11-19 | 2019-11-19 | A pellet composition comprising propiverine or a pharmaceutically acceptable salt thereof |
| TR2020/16210A TR202016210A2 (en) | 2019-11-19 | 2020-10-12 | Pharmaceutical form containing acidic substance |
| EP20889151.5A EP4061369A4 (en) | 2019-11-19 | 2020-10-27 | A pharmaceutical form comprising acidic substance |
| PCT/TR2020/050998 WO2021101481A1 (en) | 2019-11-19 | 2020-10-27 | A pellet composition comprising propiverine or a pharmaceutically acceptable salt thereof |
| PCT/TR2020/051001 WO2021101483A1 (en) | 2019-11-19 | 2020-10-27 | A pharmaceutical form comprising acidic substance |
| EP20889321.4A EP4061370A4 (en) | 2019-11-19 | 2020-10-27 | A pellet composition comprising propiverine or a pharmaceutically acceptable salt thereof |
| CA3162409A CA3162409A1 (en) | 2019-11-19 | 2020-10-27 | A pharmaceutical form comprising acidic substance |
| CA3162408A CA3162408A1 (en) | 2019-11-19 | 2020-10-27 | A pellet composition comprising propiverine or a pharmaceutically acceptable salt thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| TR2019/18013A TR201918013A2 (en) | 2019-11-19 | 2019-11-19 | A pellet composition comprising propiverine or a pharmaceutically acceptable salt thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| TR201918013A2 true TR201918013A2 (en) | 2021-06-21 |
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Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TR2019/18013A TR201918013A2 (en) | 2019-11-19 | 2019-11-19 | A pellet composition comprising propiverine or a pharmaceutically acceptable salt thereof |
| TR2020/16210A TR202016210A2 (en) | 2019-11-19 | 2020-10-12 | Pharmaceutical form containing acidic substance |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TR2020/16210A TR202016210A2 (en) | 2019-11-19 | 2020-10-12 | Pharmaceutical form containing acidic substance |
Country Status (4)
| Country | Link |
|---|---|
| EP (1) | EP4061370A4 (en) |
| CA (1) | CA3162408A1 (en) |
| TR (2) | TR201918013A2 (en) |
| WO (1) | WO2021101481A1 (en) |
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|---|---|---|---|---|
| WO2023080856A1 (en) * | 2021-11-03 | 2023-05-11 | Santa Farma Ilac Sanayii A.S. | Enteric coated pharmaceutical composition of propiverine hydrochloride |
| WO2023128906A1 (en) * | 2021-12-30 | 2023-07-06 | Santa Farma Ilac Sanayii A.S. | Release of propiverine compositions in gastric conditions |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
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| DE10149674A1 (en) * | 2001-10-09 | 2003-04-24 | Apogepha Arzneimittel Gmbh | Orally administered composition for sustained release of propiverine, useful for treatment of hypertonic bladder disorders, especially by once-daily administration |
| ITMI20061024A1 (en) * | 2006-05-25 | 2007-11-26 | Eurand Pharmaceuticals Ltd | PELLETS BASED ON LIPOIC ACID |
| TWI519322B (en) * | 2008-04-15 | 2016-02-01 | 愛戴爾製藥股份有限公司 | Compositions comprising weakly basic drugs and controlled-release dosage forms |
| CN102579404A (en) | 2012-01-17 | 2012-07-18 | 广州科的信医药技术有限公司 | Sustained-release capsule containing propiverine hydrochloride and preparation method of sustained-release capsule |
-
2019
- 2019-11-19 TR TR2019/18013A patent/TR201918013A2/en unknown
-
2020
- 2020-10-12 TR TR2020/16210A patent/TR202016210A2/en unknown
- 2020-10-27 EP EP20889321.4A patent/EP4061370A4/en active Pending
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| Publication number | Publication date |
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| WO2021101481A1 (en) | 2021-05-27 |
| EP4061370A1 (en) | 2022-09-28 |
| CA3162408A1 (en) | 2021-05-27 |
| EP4061370A4 (en) | 2023-08-02 |
| TR202016210A2 (en) | 2021-06-21 |
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