ZA200201466B - Pharmaceutical agent comprising a benzamide derivative as active ingredient. - Google Patents
Pharmaceutical agent comprising a benzamide derivative as active ingredient. Download PDFInfo
- Publication number
- ZA200201466B ZA200201466B ZA200201466A ZA200201466A ZA200201466B ZA 200201466 B ZA200201466 B ZA 200201466B ZA 200201466 A ZA200201466 A ZA 200201466A ZA 200201466 A ZA200201466 A ZA 200201466A ZA 200201466 B ZA200201466 B ZA 200201466B
- Authority
- ZA
- South Africa
- Prior art keywords
- pharmaceutical formulation
- formulation according
- sodium
- group
- formula
- Prior art date
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- 150000003936 benzamides Chemical class 0.000 title claims description 17
- 239000004480 active ingredient Substances 0.000 title description 22
- 239000008177 pharmaceutical agent Substances 0.000 title description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims description 59
- 239000000203 mixture Substances 0.000 claims description 35
- 238000009472 formulation Methods 0.000 claims description 30
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 28
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 27
- -1 organic acid salt Chemical class 0.000 claims description 26
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical group OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 25
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims description 21
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 claims description 18
- 239000000654 additive Substances 0.000 claims description 15
- 229920002134 Carboxymethyl cellulose Polymers 0.000 claims description 14
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims description 14
- 235000010948 carboxy methyl cellulose Nutrition 0.000 claims description 14
- DDRJAANPRJIHGJ-UHFFFAOYSA-N creatinine Chemical compound CN1CC(=O)NC1=N DDRJAANPRJIHGJ-UHFFFAOYSA-N 0.000 claims description 14
- 235000019359 magnesium stearate Nutrition 0.000 claims description 14
- 238000000034 method Methods 0.000 claims description 14
- BWHMMNNQKKPAPP-UHFFFAOYSA-L potassium carbonate Chemical compound [K+].[K+].[O-]C([O-])=O BWHMMNNQKKPAPP-UHFFFAOYSA-L 0.000 claims description 14
- QGZKDVFQNNGYKY-UHFFFAOYSA-N Ammonia Chemical compound N QGZKDVFQNNGYKY-UHFFFAOYSA-N 0.000 claims description 13
- VJHCJDRQFCCTHL-UHFFFAOYSA-N acetic acid 2,3,4,5,6-pentahydroxyhexanal Chemical compound CC(O)=O.OCC(O)C(O)C(O)C(O)C=O VJHCJDRQFCCTHL-UHFFFAOYSA-N 0.000 claims description 13
- 229950008138 carmellose Drugs 0.000 claims description 13
- 150000003839 salts Chemical class 0.000 claims description 13
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 12
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims description 12
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 12
- 235000010355 mannitol Nutrition 0.000 claims description 12
- 239000002904 solvent Substances 0.000 claims description 12
- 239000000126 substance Substances 0.000 claims description 12
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims description 10
- 239000011575 calcium Substances 0.000 claims description 10
- 229910052791 calcium Inorganic materials 0.000 claims description 10
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 claims description 10
- FXHOOIRPVKKKFG-UHFFFAOYSA-N N,N-Dimethylacetamide Chemical compound CN(C)C(C)=O FXHOOIRPVKKKFG-UHFFFAOYSA-N 0.000 claims description 9
- 239000011230 binding agent Substances 0.000 claims description 9
- 239000011248 coating agent Substances 0.000 claims description 9
- 239000007884 disintegrant Substances 0.000 claims description 9
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 9
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 9
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 9
- 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 9
- 239000012669 liquid formulation Substances 0.000 claims description 9
- 239000000314 lubricant Substances 0.000 claims description 9
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 9
- 239000011736 potassium bicarbonate Substances 0.000 claims description 9
- 229910000028 potassium bicarbonate Inorganic materials 0.000 claims description 9
- 235000015497 potassium bicarbonate Nutrition 0.000 claims description 9
- TYJJADVDDVDEDZ-UHFFFAOYSA-M potassium hydrogencarbonate Chemical compound [K+].OC([O-])=O TYJJADVDDVDEDZ-UHFFFAOYSA-M 0.000 claims description 9
- 229910000029 sodium carbonate Inorganic materials 0.000 claims description 9
- 235000017550 sodium carbonate Nutrition 0.000 claims description 9
- 239000007787 solid Substances 0.000 claims description 9
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 8
- GSEJCLTVZPLZKY-UHFFFAOYSA-N Triethanolamine Chemical compound OCCN(CCO)CCO GSEJCLTVZPLZKY-UHFFFAOYSA-N 0.000 claims description 8
- SLINHMUFWFWBMU-UHFFFAOYSA-N Triisopropanolamine Chemical compound CC(O)CN(CC(C)O)CC(C)O SLINHMUFWFWBMU-UHFFFAOYSA-N 0.000 claims description 8
- ZBCBWPMODOFKDW-UHFFFAOYSA-N diethanolamine Chemical compound OCCNCCO ZBCBWPMODOFKDW-UHFFFAOYSA-N 0.000 claims description 8
- LVTYICIALWPMFW-UHFFFAOYSA-N diisopropanolamine Chemical compound CC(O)CNCC(C)O LVTYICIALWPMFW-UHFFFAOYSA-N 0.000 claims description 8
- 229940043276 diisopropanolamine Drugs 0.000 claims description 8
- 239000008187 granular material Substances 0.000 claims description 8
- 239000011734 sodium Substances 0.000 claims description 8
- 229940083542 sodium Drugs 0.000 claims description 8
- 229910052708 sodium Inorganic materials 0.000 claims description 8
- 239000000454 talc Substances 0.000 claims description 8
- 229910052623 talc Inorganic materials 0.000 claims description 8
- 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 claims description 7
- ATRRKUHOCOJYRX-UHFFFAOYSA-N Ammonium bicarbonate Chemical compound [NH4+].OC([O-])=O ATRRKUHOCOJYRX-UHFFFAOYSA-N 0.000 claims description 7
- 239000004475 Arginine Substances 0.000 claims description 7
- RVEWUBJVAHOGKA-WOYAITHZSA-N Arginine glutamate Chemical compound OC(=O)[C@@H](N)CCC(O)=O.OC(=O)[C@@H](N)CCCNC(N)=N RVEWUBJVAHOGKA-WOYAITHZSA-N 0.000 claims description 7
- 239000004471 Glycine Substances 0.000 claims description 7
- ODKSFYDXXFIFQN-BYPYZUCNSA-P L-argininium(2+) Chemical compound NC(=[NH2+])NCCC[C@H]([NH3+])C(O)=O ODKSFYDXXFIFQN-BYPYZUCNSA-P 0.000 claims description 7
- 239000004288 Sodium dehydroacetate Substances 0.000 claims description 7
- 229920002472 Starch Polymers 0.000 claims description 7
- 230000000996 additive effect Effects 0.000 claims description 7
- 239000001099 ammonium carbonate Substances 0.000 claims description 7
- 235000012501 ammonium carbonate Nutrition 0.000 claims description 7
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims description 7
- 229960003121 arginine Drugs 0.000 claims description 7
- 229960004484 carbachol Drugs 0.000 claims description 7
- AIXAANGOTKPUOY-UHFFFAOYSA-N carbachol Chemical compound [Cl-].C[N+](C)(C)CCOC(N)=O AIXAANGOTKPUOY-UHFFFAOYSA-N 0.000 claims description 7
- 229940109239 creatinine Drugs 0.000 claims description 7
- PXEDJBXQKAGXNJ-QTNFYWBSSA-L disodium L-glutamate Chemical compound [Na+].[Na+].[O-]C(=O)[C@@H](N)CCC([O-])=O PXEDJBXQKAGXNJ-QTNFYWBSSA-L 0.000 claims description 7
- BNIILDVGGAEEIG-UHFFFAOYSA-L disodium hydrogen phosphate Chemical compound [Na+].[Na+].OP([O-])([O-])=O BNIILDVGGAEEIG-UHFFFAOYSA-L 0.000 claims description 7
- 229910000397 disodium phosphate Inorganic materials 0.000 claims description 7
- 235000019800 disodium phosphate Nutrition 0.000 claims description 7
- 229960002449 glycine Drugs 0.000 claims description 7
- 235000013923 monosodium glutamate Nutrition 0.000 claims description 7
- 229910000027 potassium carbonate Inorganic materials 0.000 claims description 7
- 235000011181 potassium carbonates Nutrition 0.000 claims description 7
- 235000010413 sodium alginate Nutrition 0.000 claims description 7
- 239000000661 sodium alginate Substances 0.000 claims description 7
- 229940005550 sodium alginate Drugs 0.000 claims description 7
- 239000001509 sodium citrate Substances 0.000 claims description 7
- 235000019259 sodium dehydroacetate Nutrition 0.000 claims description 7
- 229940079839 sodium dehydroacetate Drugs 0.000 claims description 7
- 229940073490 sodium glutamate Drugs 0.000 claims description 7
- 235000011121 sodium hydroxide Nutrition 0.000 claims description 7
- 239000001488 sodium phosphate Substances 0.000 claims description 7
- DSOWAKKSGYUMTF-GZOLSCHFSA-M sodium;(1e)-1-(6-methyl-2,4-dioxopyran-3-ylidene)ethanolate Chemical compound [Na+].C\C([O-])=C1/C(=O)OC(C)=CC1=O DSOWAKKSGYUMTF-GZOLSCHFSA-M 0.000 claims description 7
- 235000019698 starch Nutrition 0.000 claims description 7
- 239000008107 starch Substances 0.000 claims description 7
- HRXKRNGNAMMEHJ-UHFFFAOYSA-K trisodium citrate Chemical compound [Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O HRXKRNGNAMMEHJ-UHFFFAOYSA-K 0.000 claims description 7
- 229940038773 trisodium citrate Drugs 0.000 claims description 7
- HZAXFHJVJLSVMW-UHFFFAOYSA-N 2-Aminoethan-1-ol Chemical compound NCCO HZAXFHJVJLSVMW-UHFFFAOYSA-N 0.000 claims description 6
- 229920000881 Modified starch Polymers 0.000 claims description 6
- UIIMBOGNXHQVGW-DEQYMQKBSA-M Sodium bicarbonate-14C Chemical compound [Na+].O[14C]([O-])=O UIIMBOGNXHQVGW-DEQYMQKBSA-M 0.000 claims description 6
- BWZOPYPOZJBVLQ-UHFFFAOYSA-K aluminium glycinate Chemical compound O[Al+]O.NCC([O-])=O BWZOPYPOZJBVLQ-UHFFFAOYSA-K 0.000 claims description 6
- 229910021529 ammonia Inorganic materials 0.000 claims description 6
- 229940015826 dihydroxyaluminum aminoacetate Drugs 0.000 claims description 6
- 238000007908 dry granulation Methods 0.000 claims description 6
- VRVKOZSIJXBAJG-TYYBGVCCSA-M monosodium fumarate Chemical compound [Na+].OC(=O)\C=C\C([O-])=O VRVKOZSIJXBAJG-TYYBGVCCSA-M 0.000 claims description 5
- 229920001223 polyethylene glycol Polymers 0.000 claims description 5
- 239000004320 sodium erythorbate Substances 0.000 claims description 5
- 235000010352 sodium erythorbate Nutrition 0.000 claims description 5
- RBWSWDPRDBEWCR-RKJRWTFHSA-N sodium;(2r)-2-[(2r)-3,4-dihydroxy-5-oxo-2h-furan-2-yl]-2-hydroxyethanolate Chemical compound [Na+].[O-]C[C@@H](O)[C@H]1OC(=O)C(O)=C1O RBWSWDPRDBEWCR-RKJRWTFHSA-N 0.000 claims description 5
- 235000019263 trisodium citrate Nutrition 0.000 claims description 5
- 239000002202 Polyethylene glycol Substances 0.000 claims description 3
- 235000015424 sodium Nutrition 0.000 claims description 2
- 229940125904 compound 1 Drugs 0.000 description 14
- 239000007857 degradation product Substances 0.000 description 11
- 238000000354 decomposition reaction Methods 0.000 description 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 8
- 239000007788 liquid Substances 0.000 description 8
- 230000000052 comparative effect Effects 0.000 description 7
- 201000010099 disease Diseases 0.000 description 7
- 239000004615 ingredient Substances 0.000 description 6
- 239000000843 powder Substances 0.000 description 6
- 235000012222 talc Nutrition 0.000 description 6
- 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 description 5
- 235000009697 arginine Nutrition 0.000 description 5
- 239000013068 control sample Substances 0.000 description 5
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- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 4
- 239000002552 dosage form Substances 0.000 description 4
- 239000008101 lactose Substances 0.000 description 4
- AICOOMRHRUFYCM-ZRRPKQBOSA-N oxazine, 1 Chemical group C([C@@H]1[C@H](C(C[C@]2(C)[C@@H]([C@H](C)N(C)C)[C@H](O)C[C@]21C)=O)CC1=CC2)C[C@H]1[C@@]1(C)[C@H]2N=C(C(C)C)OC1 AICOOMRHRUFYCM-ZRRPKQBOSA-N 0.000 description 4
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- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 description 3
- 229920002261 Corn starch Polymers 0.000 description 3
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 3
- 239000002253 acid Substances 0.000 description 3
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- 235000001465 calcium Nutrition 0.000 description 3
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- SNAAJJQQZSMGQD-UHFFFAOYSA-N aluminum magnesium Chemical compound [Mg].[Al] SNAAJJQQZSMGQD-UHFFFAOYSA-N 0.000 description 2
- 229940024606 amino acid Drugs 0.000 description 2
- 235000001014 amino acid Nutrition 0.000 description 2
- 150000001413 amino acids Chemical class 0.000 description 2
- 210000004204 blood vessel Anatomy 0.000 description 2
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- 229910052808 lithium carbonate Inorganic materials 0.000 description 2
- HQRPHMAXFVUBJX-UHFFFAOYSA-M lithium;hydrogen carbonate Chemical compound [Li+].OC([O-])=O HQRPHMAXFVUBJX-UHFFFAOYSA-M 0.000 description 2
- 150000007522 mineralic acids Chemical class 0.000 description 2
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- WJMMDJOFTZAHHS-UHFFFAOYSA-L strontium;carbonic acid;carbonate Chemical compound [Sr+2].OC([O-])=O.OC([O-])=O WJMMDJOFTZAHHS-UHFFFAOYSA-L 0.000 description 2
- 239000013589 supplement Substances 0.000 description 2
- VZOQYVHEWHJIBG-UHFFFAOYSA-N 2-(aminomethyl)benzamide Chemical compound NCC1=CC=CC=C1C(N)=O VZOQYVHEWHJIBG-UHFFFAOYSA-N 0.000 description 1
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- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
- 239000001744 Sodium fumarate Substances 0.000 description 1
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- KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 description 1
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 description 1
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- 230000010261 cell growth Effects 0.000 description 1
- 235000015165 citric acid Nutrition 0.000 description 1
- 235000005822 corn Nutrition 0.000 description 1
- 230000000850 deacetylating effect Effects 0.000 description 1
- 238000006731 degradation reaction Methods 0.000 description 1
- 235000019425 dextrin Nutrition 0.000 description 1
- 230000004069 differentiation Effects 0.000 description 1
- MSJMDZAOKORVFC-SEPHDYHBSA-L disodium fumarate Chemical compound [Na+].[Na+].[O-]C(=O)\C=C\C([O-])=O MSJMDZAOKORVFC-SEPHDYHBSA-L 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 229940026231 erythorbate Drugs 0.000 description 1
- 235000010350 erythorbic acid Nutrition 0.000 description 1
- 229940050411 fumarate Drugs 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 238000005469 granulation Methods 0.000 description 1
- 230000003179 granulation Effects 0.000 description 1
- 230000003394 haemopoietic effect Effects 0.000 description 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 description 1
- 229920003132 hydroxypropyl methylcellulose phthalate Polymers 0.000 description 1
- 229940031704 hydroxypropyl methylcellulose phthalate Drugs 0.000 description 1
- 230000001939 inductive effect Effects 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 239000004310 lactic acid Substances 0.000 description 1
- 235000014655 lactic acid Nutrition 0.000 description 1
- 229960003511 macrogol Drugs 0.000 description 1
- 239000011777 magnesium Substances 0.000 description 1
- 229910052749 magnesium Inorganic materials 0.000 description 1
- 235000001055 magnesium Nutrition 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 229940117841 methacrylic acid copolymer Drugs 0.000 description 1
- 229920003145 methacrylic acid copolymer Polymers 0.000 description 1
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 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
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 description 1
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 1
- 229940068968 polysorbate 80 Drugs 0.000 description 1
- 229920000053 polysorbate 80 Polymers 0.000 description 1
- 229920006316 polyvinylpyrrolidine Polymers 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 229940005573 sodium fumarate Drugs 0.000 description 1
- 235000019294 sodium fumarate Nutrition 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
- A61K31/4406—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 3, e.g. zimeldine
-
- 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
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
- A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Dermatology (AREA)
- Endocrinology (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Hematology (AREA)
- Heart & Thoracic Surgery (AREA)
- Emergency Medicine (AREA)
- Oncology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Transplantation (AREA)
- Cardiology (AREA)
- Communicable Diseases (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pyridine Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP22955199A JP2001064177A (ja) | 1999-08-16 | 1999-08-16 | ベンズアミド誘導体を有効成分とする製剤 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200201466B true ZA200201466B (en) | 2002-09-02 |
Family
ID=16893948
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200201466A ZA200201466B (en) | 1999-08-16 | 2002-02-21 | Pharmaceutical agent comprising a benzamide derivative as active ingredient. |
Country Status (29)
| Country | Link |
|---|---|
| EP (1) | EP1207881B1 (xx) |
| JP (2) | JP2001064177A (xx) |
| KR (1) | KR100683876B1 (xx) |
| CN (1) | CN1205931C (xx) |
| AR (1) | AR031074A1 (xx) |
| AU (1) | AU780151B2 (xx) |
| BG (1) | BG65662B1 (xx) |
| BR (1) | BR0013283A (xx) |
| CA (1) | CA2380757C (xx) |
| CY (1) | CY1116273T1 (xx) |
| CZ (1) | CZ302924B6 (xx) |
| DK (1) | DK1207881T3 (xx) |
| EE (1) | EE05331B1 (xx) |
| ES (1) | ES2536705T3 (xx) |
| HK (1) | HK1046501B (xx) |
| HR (1) | HRP20020181B1 (xx) |
| HU (1) | HU230386B1 (xx) |
| IL (1) | IL148169A0 (xx) |
| MX (1) | MXPA02001575A (xx) |
| NO (1) | NO328957B1 (xx) |
| NZ (1) | NZ517356A (xx) |
| PL (1) | PL201388B1 (xx) |
| PT (1) | PT1207881E (xx) |
| RU (1) | RU2257206C2 (xx) |
| SK (1) | SK287547B6 (xx) |
| TW (1) | TWI245630B (xx) |
| UA (1) | UA73316C2 (xx) |
| WO (1) | WO2001012193A1 (xx) |
| ZA (1) | ZA200201466B (xx) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2001081031A (ja) * | 1999-08-30 | 2001-03-27 | Schering Ag | 溶解性および経口吸収性を改善したベンズアミド誘導体含有製剤 |
| EP1319409A4 (en) * | 2000-09-22 | 2006-05-03 | Takeda Pharmaceutical | SOLID PREPARATIONS |
| AU2003220119A1 (en) | 2002-03-07 | 2003-09-22 | University Of Delaware | Methods, compositions, and kits for enhancing oligonucleotide-mediated nucleic acid sequence alteration using compositions comprising a histone deacetylase inhibitor, lambda phage beta protein, or hydroxyurea |
| GB0316206D0 (en) * | 2003-07-10 | 2003-08-13 | Glaxo Group Ltd | Pharmaceutical formulation |
| EP2135620A4 (en) | 2007-03-28 | 2010-12-29 | Santen Pharmaceutical Co Ltd | AGAINST OKULAR HYPOTONIA CONNECTED TO HISTONE DEACETYLASE INHIBITION AS AN ACTIVE SUBSTANCE |
| KR101405615B1 (ko) * | 2007-08-27 | 2014-06-12 | (주)아모레퍼시픽 | 조성물 내 ｐＨ 조절을 통해 안정화된 벤즈아미드 화합물을함유하는 피부 외용제 조성물, 및 그 벤즈아미드 화합물안정화 방법 |
| GB2462893B (en) * | 2008-08-29 | 2010-10-13 | Bayer Schering Pharma Ag | N-(2-aminophenyl)-4-[N-(pyridine-3-yl)-methoxycarbonyl-aminomethyl]-benzamide (MS-275) polymorph B |
| NZ591387A (en) * | 2008-08-29 | 2012-03-30 | Bayer Pharma AG | N-(2-aminophenyl)-4-[n-(pyridine-3-yl)-methoxycarbonyl-aminomethyl]-benzamide (ms-275) polymorph b |
| WO2014163132A1 (ja) * | 2013-04-04 | 2014-10-09 | 第一三共株式会社 | アミノカルボン酸の塩の固形組成物 |
| CN107427483B (zh) | 2015-03-19 | 2021-06-29 | 第一三共株式会社 | 含有着色剂的固体制剂 |
| EP3272345B1 (en) | 2015-03-19 | 2019-10-16 | Daiichi Sankyo Company, Limited | Solid preparation containing antioxidant agent |
| ES2943883T3 (es) | 2018-07-30 | 2023-06-16 | Daiichi Sankyo Co Ltd | Formulación de fármaco sólido que contiene estabilizador |
| CN111867559A (zh) * | 2019-01-25 | 2020-10-30 | 株式会社爱茉莉太平洋 | 含有苯甲酰胺化合物以及增溶剂的组合物 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SU706415A1 (ru) * | 1978-04-12 | 1979-12-30 | Ташкентский Государственный Университет Им.В.И.Ленина | Итаконоил анабазин в качестве дыхательного аналептика |
| CZ284687B6 (cs) * | 1986-04-30 | 1999-02-17 | Dainippon Pharmaceutical Co., Ltd. | Substituovaný benzamidový derivát, způsob jeho výroby a farmaceutický prostředek na jeho bázi |
| JP3354090B2 (ja) * | 1996-09-30 | 2002-12-09 | シエーリング アクチエンゲゼルシャフト | 分化誘導剤 |
| US6174905B1 (en) * | 1996-09-30 | 2001-01-16 | Mitsui Chemicals, Inc. | Cell differentiation inducer |
-
1999
- 1999-08-16 JP JP22955199A patent/JP2001064177A/ja active Pending
-
2000
- 2000-08-07 TW TW089115860A patent/TWI245630B/zh not_active IP Right Cessation
- 2000-08-15 AR ARP000104212A patent/AR031074A1/es active IP Right Grant
- 2000-08-16 UA UA2002032040A patent/UA73316C2/uk unknown
- 2000-08-16 RU RU2002106815/15A patent/RU2257206C2/ru active
- 2000-08-16 BR BR0013283-7A patent/BR0013283A/pt not_active Application Discontinuation
- 2000-08-16 AU AU64427/00A patent/AU780151B2/en not_active Expired
- 2000-08-16 HU HU0203226A patent/HU230386B1/hu unknown
- 2000-08-16 HK HK02107641.6A patent/HK1046501B/zh not_active IP Right Cessation
- 2000-08-16 KR KR1020027002002A patent/KR100683876B1/ko not_active Expired - Lifetime
- 2000-08-16 EP EP00951523.0A patent/EP1207881B1/en not_active Expired - Lifetime
- 2000-08-16 MX MXPA02001575A patent/MXPA02001575A/es active IP Right Grant
- 2000-08-16 EE EEP200200073A patent/EE05331B1/xx unknown
- 2000-08-16 PT PT951523T patent/PT1207881E/pt unknown
- 2000-08-16 CA CA002380757A patent/CA2380757C/en not_active Expired - Lifetime
- 2000-08-16 WO PCT/EP2000/008011 patent/WO2001012193A1/en not_active Ceased
- 2000-08-16 IL IL14816900A patent/IL148169A0/xx active IP Right Grant
- 2000-08-16 JP JP2001516539A patent/JP4854158B2/ja not_active Expired - Lifetime
- 2000-08-16 CN CNB008117187A patent/CN1205931C/zh not_active Expired - Lifetime
- 2000-08-16 SK SK209-2002A patent/SK287547B6/sk not_active IP Right Cessation
- 2000-08-16 HR HRP20020181AA patent/HRP20020181B1/hr not_active IP Right Cessation
- 2000-08-16 ES ES00951523.0T patent/ES2536705T3/es not_active Expired - Lifetime
- 2000-08-16 DK DK00951523.0T patent/DK1207881T3/da active
- 2000-08-16 PL PL353449A patent/PL201388B1/pl unknown
- 2000-08-16 NZ NZ517356A patent/NZ517356A/en not_active IP Right Cessation
- 2000-08-16 CZ CZ20020540A patent/CZ302924B6/cs not_active IP Right Cessation
-
2002
- 2002-02-15 NO NO20020774A patent/NO328957B1/no not_active IP Right Cessation
- 2002-02-21 ZA ZA200201466A patent/ZA200201466B/en unknown
- 2002-03-14 BG BG106516A patent/BG65662B1/bg unknown
-
2015
- 2015-05-13 CY CY20151100423T patent/CY1116273T1/el unknown
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