BRPI0715423A2 - formulaÇÕes para Éteres de benzimidazolil piridila - Google Patents

Info

Publication number

BRPI0715423A2

BRPI0715423A2 BRPI0715423-2A BRPI0715423A BRPI0715423A2 BR PI0715423 A2 BRPI0715423 A2 BR PI0715423A2 BR PI0715423 A BRPI0715423 A BR PI0715423A BR PI0715423 A2 BRPI0715423 A2 BR PI0715423A2

Authority

BR

Brazil

Prior art keywords

formulation

mixture

compound

formula

acid

Prior art date

2006-07-21

Links

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• 239000000203 mixture Substances 0.000 title claims abstract description 467
• 238000009472 formulation Methods 0.000 title claims abstract description 326
• SYLABBNLHCTJEF-UHFFFAOYSA-N 2-pyridin-2-yloxy-1h-benzimidazole Chemical class N=1C2=CC=CC=C2NC=1OC1=CC=CC=N1 SYLABBNLHCTJEF-UHFFFAOYSA-N 0.000 title description 5
• 150000001875 compounds Chemical class 0.000 claims abstract description 91
• 239000002904 solvent Substances 0.000 claims abstract description 86
• 238000000034 method Methods 0.000 claims abstract description 72
• 150000003839 salts Chemical class 0.000 claims abstract description 56
• 239000007787 solid Substances 0.000 claims abstract description 42
• 239000004615 ingredient Substances 0.000 claims abstract description 31
• 239000003995 emulsifying agent Substances 0.000 claims abstract description 30
• 239000002775 capsule Substances 0.000 claims description 94
• -1 fatty acid ester Chemical class 0.000 claims description 65
• 239000000194 fatty acid Substances 0.000 claims description 55
• 235000014113 dietary fatty acids Nutrition 0.000 claims description 53
• 229930195729 fatty acid Natural products 0.000 claims description 53
• LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 50
• DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 42
• WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 29
• ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 claims description 28
• 229920001223 polyethylene glycol Polymers 0.000 claims description 28
• 229920003171 Poly (ethylene oxide) Polymers 0.000 claims description 26
• 150000004665 fatty acids Chemical group 0.000 claims description 25
• 239000002202 Polyethylene glycol Substances 0.000 claims description 22
• 229920000642 polymer Polymers 0.000 claims description 22
• 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 21
• 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 21
• PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 20
• 239000002253 acid Substances 0.000 claims description 20
• 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims description 20
• 229920000053 polysorbate 80 Polymers 0.000 claims description 20
• OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 18
• 239000012669 liquid formulation Substances 0.000 claims description 18
• 229920002675 Polyoxyl Polymers 0.000 claims description 17
• 239000003086 colorant Substances 0.000 claims description 17
• 239000007903 gelatin capsule Substances 0.000 claims description 17
• 239000008187 granular material Substances 0.000 claims description 17
• WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 claims description 16
• GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 claims description 16
• LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 claims description 16
• QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 claims description 16
• 229920000858 Cyclodextrin Polymers 0.000 claims description 16
• 239000005642 Oleic acid Substances 0.000 claims description 16
• ZQPPMHVWECSIRJ-UHFFFAOYSA-N Oleic acid Natural products CCCCCCCCC=CCCCCCCCC(O)=O ZQPPMHVWECSIRJ-UHFFFAOYSA-N 0.000 claims description 16
• QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 claims description 16
• 229960000913 crospovidone Drugs 0.000 claims description 15
• 125000003976 glyceryl group Chemical group [H]C([*])([H])C(O[H])([H])C(O[H])([H])[H] 0.000 claims description 15
• 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims description 15
• 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims description 15
• 239000000796 flavoring agent Substances 0.000 claims description 14
• 235000003599 food sweetener Nutrition 0.000 claims description 14
• 239000003765 sweetening agent Substances 0.000 claims description 14
• LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims description 13
• 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 13
• 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 13
• 239000003963 antioxidant agent Substances 0.000 claims description 12
• 235000006708 antioxidants Nutrition 0.000 claims description 12
• 150000002148 esters Chemical class 0.000 claims description 12
• 235000013355 food flavoring agent Nutrition 0.000 claims description 12
• 229940069328 povidone Drugs 0.000 claims description 12
• 235000010980 cellulose Nutrition 0.000 claims description 11
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• ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 claims description 10
• QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims description 10
• 239000003755 preservative agent Substances 0.000 claims description 10
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• 229920001213 Polysorbate 20 Polymers 0.000 claims description 9
• 230000003078 antioxidant effect Effects 0.000 claims description 9
• 235000011187 glycerol Nutrition 0.000 claims description 9
• 239000001866 hydroxypropyl methyl cellulose Substances 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
• 229940049964 oleate Drugs 0.000 claims description 9
• 235000010486 polyoxyethylene sorbitan monolaurate Nutrition 0.000 claims description 9
• 239000000256 polyoxyethylene sorbitan monolaurate Substances 0.000 claims description 9
• FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims description 8
• 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 8
• 229920002472 Starch Polymers 0.000 claims description 8
• 125000005456 glyceride group Chemical group 0.000 claims description 8
• 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 8
• 239000008108 microcrystalline cellulose Substances 0.000 claims description 8
• 229940016286 microcrystalline cellulose Drugs 0.000 claims description 8
• 235000019698 starch Nutrition 0.000 claims description 8
• 229920001214 Polysorbate 60 Polymers 0.000 claims description 7
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• 229940032147 starch Drugs 0.000 claims description 7
• 150000005691 triesters Chemical class 0.000 claims description 7
• VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 claims description 6
• FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 6
• 235000021355 Stearic acid Nutrition 0.000 claims description 6
• 229930006000 Sucrose Natural products 0.000 claims description 6
• CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims description 6
• 229940097362 cyclodextrins Drugs 0.000 claims description 6
• OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims description 6
• 239000000600 sorbitol Substances 0.000 claims description 6
• 235000010356 sorbitol Nutrition 0.000 claims description 6
• 239000008117 stearic acid Substances 0.000 claims description 6
• 239000005720 sucrose Substances 0.000 claims description 6
• 239000000454 talc Substances 0.000 claims description 6
• 229910052623 talc Inorganic materials 0.000 claims description 6
• 229940033134 talc Drugs 0.000 claims description 6
• ZORQXIQZAOLNGE-UHFFFAOYSA-N 1,1-difluorocyclohexane Chemical compound FC1(F)CCCCC1 ZORQXIQZAOLNGE-UHFFFAOYSA-N 0.000 claims description 5
• XZIIFPSPUDAGJM-UHFFFAOYSA-N 6-chloro-2-n,2-n-diethylpyrimidine-2,4-diamine Chemical compound CCN(CC)C1=NC(N)=CC(Cl)=N1 XZIIFPSPUDAGJM-UHFFFAOYSA-N 0.000 claims description 5
• 239000004354 Hydroxyethyl cellulose Substances 0.000 claims description 5
• 229920000663 Hydroxyethyl cellulose Polymers 0.000 claims description 5
• 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 5
• 229920002690 Polyoxyl 40 HydrogenatedCastorOil Polymers 0.000 claims description 5
• 229920001577 copolymer Polymers 0.000 claims description 5
• 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims description 5
• 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 5
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• 239000001863 hydroxypropyl cellulose Substances 0.000 claims description 5
• 239000000155 melt Substances 0.000 claims description 5
• 239000001683 mentha spicata herb oil Substances 0.000 claims description 5
• 150000003904 phospholipids Chemical class 0.000 claims description 5
• 229920000136 polysorbate Polymers 0.000 claims description 5
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• GVJHHUAWPYXKBD-IEOSBIPESA-N α-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 claims description 5
• OYHQOLUKZRVURQ-NTGFUMLPSA-N (9Z,12Z)-9,10,12,13-tetratritiooctadeca-9,12-dienoic acid Chemical compound C(CCCCCCC\C(=C(/C\C(=C(/CCCCC)\[3H])\[3H])\[3H])\[3H])(=O)O OYHQOLUKZRVURQ-NTGFUMLPSA-N 0.000 claims description 4
• VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims description 4
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• LVGKNOAMLMIIKO-UHFFFAOYSA-N Elaidinsaeure-aethylester Natural products CCCCCCCCC=CCCCCCCCC(=O)OCC LVGKNOAMLMIIKO-UHFFFAOYSA-N 0.000 claims description 4
• 229920000881 Modified starch Polymers 0.000 claims description 4
• SECXISVLQFMRJM-UHFFFAOYSA-N N-Methylpyrrolidone Chemical compound CN1CCCC1=O SECXISVLQFMRJM-UHFFFAOYSA-N 0.000 claims description 4
• 229920001219 Polysorbate 40 Polymers 0.000 claims description 4
• HVUMOYIDDBPOLL-XWVZOOPGSA-N Sorbitan monostearate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O HVUMOYIDDBPOLL-XWVZOOPGSA-N 0.000 claims description 4
• 239000004147 Sorbitan trioleate Substances 0.000 claims description 4
• PRXRUNOAOLTIEF-ADSICKODSA-N Sorbitan trioleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCC\C=C/CCCCCCCC)[C@H]1OC[C@H](O)[C@H]1OC(=O)CCCCCCC\C=C/CCCCCCCC PRXRUNOAOLTIEF-ADSICKODSA-N 0.000 claims description 4
• SJLAFUFWXUJDDR-KTKRTIGZSA-N [3-[3-(2,3-dihydroxypropoxy)-2-hydroxypropoxy]-2-hydroxypropyl] (z)-octadec-9-enoate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC(O)COCC(O)COCC(O)CO SJLAFUFWXUJDDR-KTKRTIGZSA-N 0.000 claims description 4
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• LVGKNOAMLMIIKO-QXMHVHEDSA-N ethyl oleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC LVGKNOAMLMIIKO-QXMHVHEDSA-N 0.000 claims description 4
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• WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 claims description 4
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• GDCRSXZBSIRSFR-UHFFFAOYSA-N ethyl prop-2-enoate;2-methylprop-2-enoic acid Chemical compound CC(=C)C(O)=O.CCOC(=O)C=C GDCRSXZBSIRSFR-UHFFFAOYSA-N 0.000 claims description 3
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• RZRNAYUHWVFMIP-UHFFFAOYSA-N monoelaidin Natural products CCCCCCCCC=CCCCCCCCC(=O)OCC(O)CO RZRNAYUHWVFMIP-UHFFFAOYSA-N 0.000 claims description 3
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• YKTSYUJCYHOUJP-UHFFFAOYSA-N [O--].[Al+3].[Al+3].[O-][Si]([O-])([O-])[O-] Chemical compound [O--].[Al+3].[Al+3].[O-][Si]([O-])([O-])[O-] YKTSYUJCYHOUJP-UHFFFAOYSA-N 0.000 claims description 2
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