AR059739A1 - Formulaciones y procesos para tabletas - Google Patents
Formulaciones y procesos para tabletasInfo
- Publication number
- AR059739A1 AR059739A1 ARP070100900A ARP070100900A AR059739A1 AR 059739 A1 AR059739 A1 AR 059739A1 AR P070100900 A ARP070100900 A AR P070100900A AR P070100900 A ARP070100900 A AR P070100900A AR 059739 A1 AR059739 A1 AR 059739A1
- Authority
- AR
- Argentina
- Prior art keywords
- pharmaceutical formulation
- alkyl
- component
- weight
- trifluoralkoxy
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title abstract 5
- 239000008194 pharmaceutical composition Substances 0.000 abstract 10
- 229910052736 halogen Inorganic materials 0.000 abstract 6
- 150000002367 halogens Chemical group 0.000 abstract 6
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 5
- -1 C1-6 trifluoralkyl Chemical group 0.000 abstract 5
- 125000003342 alkenyl group Chemical group 0.000 abstract 5
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 5
- 101100134925 Gallus gallus COR6 gene Proteins 0.000 abstract 4
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 4
- 239000003085 diluting agent Substances 0.000 abstract 4
- 239000000945 filler Substances 0.000 abstract 4
- 125000000041 C6-C10 aryl group Chemical group 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000000304 alkynyl group Chemical group 0.000 abstract 3
- 239000002831 pharmacologic agent Substances 0.000 abstract 3
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 2
- 235000014113 dietary fatty acids Nutrition 0.000 abstract 2
- 229930195729 fatty acid Natural products 0.000 abstract 2
- 239000000194 fatty acid Substances 0.000 abstract 2
- 239000004615 ingredient Substances 0.000 abstract 2
- 229910052751 metal Inorganic materials 0.000 abstract 2
- 239000002184 metal Substances 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 239000000080 wetting agent Substances 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 1
- MQIMZDXIAHJKQP-UHFFFAOYSA-N 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol Chemical group N=1C2=CC(O)=CC(C=C)=C2OC=1C1=CC=C(O)C(F)=C1 MQIMZDXIAHJKQP-UHFFFAOYSA-N 0.000 abstract 1
- 125000002373 5 membered heterocyclic group Chemical group 0.000 abstract 1
- 125000004070 6 membered heterocyclic group Chemical group 0.000 abstract 1
- CTKXFMQHOOWWEB-UHFFFAOYSA-N Ethylene oxide/propylene oxide copolymer Chemical compound CCCOC(C)COCCO CTKXFMQHOOWWEB-UHFFFAOYSA-N 0.000 abstract 1
- 229920003171 Poly (ethylene oxide) Chemical class 0.000 abstract 1
- 239000002202 Polyethylene glycol Substances 0.000 abstract 1
- 229920001214 Polysorbate 60 Polymers 0.000 abstract 1
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 abstract 1
- 150000008051 alkyl sulfates Chemical class 0.000 abstract 1
- 239000007864 aqueous solution Substances 0.000 abstract 1
- 239000011230 binding agent Substances 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 239000004359 castor oil Substances 0.000 abstract 1
- 235000019438 castor oil Nutrition 0.000 abstract 1
- 239000007884 disintegrant Substances 0.000 abstract 1
- MOTZDAYCYVMXPC-UHFFFAOYSA-N dodecyl hydrogen sulfate Chemical compound CCCCCCCCCCCCOS(O)(=O)=O MOTZDAYCYVMXPC-UHFFFAOYSA-N 0.000 abstract 1
- 229940043264 dodecyl sulfate Drugs 0.000 abstract 1
- 238000009472 formulation Methods 0.000 abstract 1
- 125000005456 glyceride group Chemical group 0.000 abstract 1
- 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 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 239000000314 lubricant Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 1
- 229920001993 poloxamer 188 Polymers 0.000 abstract 1
- 229940044519 poloxamer 188 Drugs 0.000 abstract 1
- 229920001223 polyethylene glycol Polymers 0.000 abstract 1
- APSBXTVYXVQYAB-UHFFFAOYSA-M sodium docusate Chemical compound [Na+].CCCCC(CC)COC(=O)CC(S([O-])(=O)=O)C(=O)OCC(CC)CCCC APSBXTVYXVQYAB-UHFFFAOYSA-M 0.000 abstract 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 abstract 1
- 125000004001 thioalkyl group Chemical group 0.000 abstract 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/426—1,3-Thiazoles
-
- 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
- A61K9/2009—Inorganic compounds
-
- 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
- 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
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Inorganic Chemistry (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Reivindicacion 1: Una formulacion farmacéutica que comprende: (a) una cantidad farmacéuticamente efectiva de un agente farmacologico activo que tiene la formula (1): en donde: R1 es hidrogeno, hidroxilo, halogeno, alquilo C1-6, trifluoralquilo C1-6, cicloalquilo C3-8, alcoxi C1-6, trifluoralcoxi C1-6, tioalquilo C1-6, sulfoxoalquilo C1-6, sulfonoalquilo C1-6, arilo C6-10, -NO2, -NR5R6, -N(R5)COR6, -CN, -CHFCN, -CF2CN, alquinilo C2-7, alquenilo C2-7, o un anillo heterocíclico de 5 o 6 miembros que tiene 1 a 4 heteroátomos seleccionados de O, N y S; en donde dichos restos alquilo o alquenilo están opcionalmente sustituidos con hidroxilo, -CN, halogeno, trifluoralquilo, trifluoralcoxi, -COR5, -CO2R5, -NO2, CONR5R6, NR5R6 o N(R5)COR6; R2 y R2a son cada uno, independientemente, hidrogeno, hidroxilo, halogeno, alquilo C1-6, alcoxi C1-4, alquenilo C2-7, alquinilo C2-7, trifluoralquilo C1-6, o trifluoralcoxi C1-6, en donde dichos restos alquilo o alquenilo están opcionalmente sustituidos con hidroxilo, -CN, halogeno, trifluoralquilo, trifluoralcoxi, -COR5, - CO2R5, -NO2, CONR5R6, NR5R6 o N(R5)COR6; R3, R3a, y R4 son cada uno, independientemente, hidrogeno, alquilo C1-6, alquenilo de 2-7 átomos de carbono, alquinilo C2-7, halogeno, alcoxi C1-4, trifluoralquilo C1-6, o trifluoralcoxi C1-6 en donde dichos restos alquilo o alquenilo están opcionalmente sustituidos con hidroxilo, -CN, halogeno, trifluoralquilo, trifluoralcoxi, -COR5, -CO2R5, -NO2, CONR5R6, NR5R6 o N(R5)COR6; R5, R6 son cada uno, independientemente hidrogeno, alquilo C1-6, o arilo C6-10; X es O, S, o NR7 y R7 es hidrogeno, alquilo C1-6, o arilo C6-10, -COR5, -CO2R5 o -SO2R5 o una sal farmacéuticamente aceptable del mismo; y (b) un sistema excipiente o portador que comprende: (i) un primer componente diluyente/rellenador que comprende desde aproximadamente 30% hasta aproximadamente 95% en peso de dicha formulacion; (ii) un segundo componente diluyente/rellenador opcional que comprende, cuando se encuentra presente, hasta aproximadamente 40% en peso de dicha formulacion farmacéutica; (iii) un componente desintegrante que comprende desde aproximadamente 0,5% hasta aproximadamente 20% en peso de dicha formulacion farmacéutica; (iv) un componente aglutinante que comprende desde aproximadamente 0,5% hasta aproximadamente 10% en peso de dicha formulacion farmacéutica; (v) un componente de agente humectante que comprende desde aproximadamente 0,5% hasta aproximadamente 8% en peso de dicha formulacion farmacéutica; y (vi) un componente lubricante opcional que comprende, cuando se encuentra presente, desde aproximadamente 0,01% hasta aproximadamente 5% en peso de dicha formulacion farmacéutica; con la condicion de que cuando dicha formulacion farmacéutica comprende uno o más ingredientes seleccionados de lauril sulfato metálico, lauril sulfato de sodio, alquil sulfato metálico, polietilenglicol, glicérido de éster graso, Poloxámero 188, éster de ácido graso de polioxietilen sorbitan, derivado de polioxietilen aceite de ricino, éster de ácido graso de azucar, glicérido poliglicolizado, compuesto de amina de amonio cuaternario, y docusato sodico, entonces la suma de las cantidades de dichos ingrediente no excede aproximadamente 8% en peso de dicha formulacion farmacéutica. Reivindicacion 21: La formulacion farmacéutica de cualquiera de las reivindicaciones 1 a 20 en donde dicho agente farmacologico activo es 2-(3-fluor-4-hidroxifenil)-7-vinil-1,3- benzoxazol-5-ol, o una sal farmacéuticamente aceptable del mismo. Reivindicacion 23: Un proceso para preparar la formulacion farmacéutica de cualquiera de las reivindicaciones 1 a 21 que comprende: (a) mezclar el agente farmacologico activo con el primer componente diluyente/rellenador, el componente desintegrante, y el segundo componente diluyente/rellenador opcional, si se encuentra presente, para formar una mezcla inicial; y (b) granular dicha mezcla inicial con una solucion acuosa que comprende el componente de agente humectante para formar una mezcla granulada.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US78004506P | 2006-03-06 | 2006-03-06 | |
| US79750306P | 2006-05-04 | 2006-05-04 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR059739A1 true AR059739A1 (es) | 2008-04-23 |
Family
ID=38475764
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP070100900A AR059739A1 (es) | 2006-03-06 | 2007-03-05 | Formulaciones y procesos para tabletas |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20070208067A1 (es) |
| EP (1) | EP1993516A2 (es) |
| JP (1) | JP2009529061A (es) |
| AR (1) | AR059739A1 (es) |
| AU (1) | AU2007223278A1 (es) |
| BR (1) | BRPI0708592A2 (es) |
| CA (1) | CA2643015A1 (es) |
| MX (1) | MX2008011459A (es) |
| PE (1) | PE20071315A1 (es) |
| TW (1) | TW200803850A (es) |
| WO (1) | WO2007103867A2 (es) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20080175900A1 (en) * | 2006-11-21 | 2008-07-24 | Wyeth | Pharmaceutical formulations of an anhydrate crystal form of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol |
| US20090239920A1 (en) * | 2006-11-21 | 2009-09-24 | Wyeth | Pharmaceutical formulations of an anhydrate crystal form of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol |
| US20080175901A1 (en) * | 2006-11-21 | 2008-07-24 | Wyeth | Pharmaceutical formulations of a crystal form of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol |
| US20080241234A1 (en) * | 2006-11-21 | 2008-10-02 | Wyeth | Pharmaceutical formulations of an anhydrate crystal form of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol |
| AR083417A1 (es) | 2010-10-14 | 2013-02-21 | Novartis Ag | Composiciones farmaceuticas que contienen un dgat1 inhibidor |
| US20120107393A1 (en) * | 2010-10-29 | 2012-05-03 | University Of Tennessee Research Foundation | Pellets for Delivery of Biologically Active Substances |
| US20160213030A1 (en) | 2013-08-28 | 2016-07-28 | Sensient Colors Llc | Edible coating compositions, edible coatings, and methods for making and using the same |
| HUE048950T2 (hu) * | 2014-05-29 | 2020-09-28 | Novartis Ag | Ceritinib formuláció |
| GB202006760D0 (en) * | 2020-05-07 | 2020-06-24 | Univ Helsinki | Bioinformatics |
| WO2021253380A1 (en) * | 2020-06-19 | 2021-12-23 | InventisBio Co., Ltd. | Oral formulations and uses thereof |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3437599C2 (de) * | 1984-10-13 | 1987-04-16 | Dolorgiet GmbH & Co KG, 5205 St Augustin | Ibuprofen enthaltende Weichgelatinekapseln |
| US5468502A (en) * | 1994-12-20 | 1995-11-21 | American Home Products Corporation | Ibuprofen enhancing solvent system |
| UA83620C2 (ru) * | 2001-12-05 | 2008-08-11 | Уайт | Замещенные бензоксазолы и их аналоги как эстрогенные агенты |
| EP1819322A2 (en) * | 2004-12-02 | 2007-08-22 | Wyeth a Corporation of the State of Delaware | Formulations of substituted benzoxazoles |
| KR20070089921A (ko) * | 2004-12-02 | 2007-09-04 | 와이어쓰 | 치환된 벤족사졸의 제형 |
| BRPI0518789A2 (pt) * | 2004-12-02 | 2008-12-09 | Wyeth Corp | formulaÇço farmacÊutica, processo para preparar uma formulaÇço farmacÊutica, produto, e, cÁpsula ou tablete |
| CN101137626A (zh) * | 2005-03-08 | 2008-03-05 | 惠氏公司 | 2－(3－氟－4－羟基苯基)－7－乙烯基－1,3－苯并唑－5－醇的晶形及其作为雌激素受体调节剂的用途 |
-
2007
- 2007-03-05 TW TW096107503A patent/TW200803850A/zh unknown
- 2007-03-05 US US11/682,127 patent/US20070208067A1/en not_active Abandoned
- 2007-03-05 BR BRPI0708592-3A patent/BRPI0708592A2/pt not_active Application Discontinuation
- 2007-03-05 WO PCT/US2007/063304 patent/WO2007103867A2/en not_active Ceased
- 2007-03-05 PE PE2007000232A patent/PE20071315A1/es not_active Application Discontinuation
- 2007-03-05 EP EP07757910A patent/EP1993516A2/en not_active Withdrawn
- 2007-03-05 CA CA002643015A patent/CA2643015A1/en not_active Abandoned
- 2007-03-05 JP JP2008558488A patent/JP2009529061A/ja active Pending
- 2007-03-05 AU AU2007223278A patent/AU2007223278A1/en not_active Abandoned
- 2007-03-05 AR ARP070100900A patent/AR059739A1/es not_active Application Discontinuation
- 2007-03-05 MX MX2008011459A patent/MX2008011459A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US20070208067A1 (en) | 2007-09-06 |
| CA2643015A1 (en) | 2007-09-13 |
| EP1993516A2 (en) | 2008-11-26 |
| PE20071315A1 (es) | 2008-02-14 |
| BRPI0708592A2 (pt) | 2011-06-07 |
| WO2007103867A2 (en) | 2007-09-13 |
| MX2008011459A (es) | 2008-09-24 |
| AU2007223278A1 (en) | 2007-09-13 |
| TW200803850A (en) | 2008-01-16 |
| JP2009529061A (ja) | 2009-08-13 |
| WO2007103867A3 (en) | 2008-07-10 |
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