http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-059739-A1
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_24e76490bed88751680a5fef9bc73892 |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K9-2027 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K9-2009 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K9-2018 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4164 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-421 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4184 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K9-2054 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-426 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 |
filingDate | 2007-03-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationDate | 2008-04-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | AR-059739-A1 |
titleOfInvention | FORMULATIONS AND PROCESSES FOR TABLETS |
abstract | Claim 1: A pharmaceutical formulation comprising: (a) a pharmaceutically effective amount of an active pharmacological agent having the formula (1): wherein: R1 is hydrogen, hydroxyl, halogen, C1-6 alkyl, C1-6 trifluoralkyl, C3-8 cycloalkyl, C1-6 alkoxy, C1-6 trifluoralkoxy, C1-6 thioalkyl, C1-6 sulfoxoalkyl, C1-6 sulfonoalkyl, C6-10 aryl, -NO2, -NR5R6, -N (R5) COR6, -CN , -CHFCN, -CF2CN, C2-7 alkynyl, C2-7 alkenyl, or a 5- or 6-membered heterocyclic ring having 1 to 4 heteroatoms selected from O, N and S; wherein said alkyl or alkenyl moieties are optionally substituted with hydroxyl, -CN, halogen, trifluoralkyl, trifluoralkoxy, -COR5, -CO2R5, -NO2, CONR5R6, NR5R6 or N (R5) COR6; R2 and R2a are each independently hydrogen, hydroxy, halogen, C1-6 alkyl, C1-4 alkoxy, C2-7 alkenyl, C2-7 alkynyl, C1-6 trifluoralkyl, or C1-6 trifluoralkoxy, wherein said moieties alkyl or alkenyl are optionally substituted with hydroxyl, -CN, halogen, trifluoralkyl, trifluoralkoxy, -COR5, - CO2R5, -NO2, CONR5R6, NR5R6 or N (R5) COR6; R3, R3a, and R4 are each independently hydrogen, C1-6 alkyl, 2-7 carbon alkenyl, C2-7 alkynyl, halogen, C1-4 alkoxy, C1-6 trifluoralkyl, or C1-6 trifluoralkoxy wherein said alkyl or alkenyl moieties are optionally substituted with hydroxyl, -CN, halogen, trifluoralkyl, trifluoralkoxy, -COR5, -CO2R5, -NO2, CONR5R6, NR5R6 or N (R5) COR6; R5, R6 are each independently hydrogen, C1-6 alkyl, or C6-10 aryl; X is O, S, or NR7 and R7 is hydrogen, C1-6 alkyl, or C6-10 aryl, -COR5, -CO2R5 or -SO2R5 or a pharmaceutically acceptable salt thereof; and (b) an excipient or carrier system comprising: (i) a first diluent / filler component comprising from about 30% to about 95% by weight of said formulation; (ii) a second optional diluent / filler component comprising, when present, up to about 40% by weight of said pharmaceutical formulation; (iii) a disintegrating component comprising from about 0.5% to about 20% by weight of said pharmaceutical formulation; (iv) a binder component comprising from about 0.5% to about 10% by weight of said pharmaceutical formulation; (v) a wetting agent component comprising from about 0.5% to about 8% by weight of said pharmaceutical formulation; and (vi) an optional lubricant component comprising, when present, from about 0.01% to about 5% by weight of said pharmaceutical formulation; with the proviso that when said pharmaceutical formulation comprises one or more ingredients selected from metal lauryl sulfate, sodium lauryl sulfate, metal alkyl sulfate, polyethylene glycol, fatty ester glyceride, Poloxamer 188, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene derivative castor oil, sugar fatty acid ester, polyglycolized glyceride, quaternary ammonium amine compound, and sodium docusate, then the sum of the amounts of said ingredient does not exceed approximately 8% by weight of said pharmaceutical formulation. Claim 21: The pharmaceutical formulation of any one of claims 1 to 20 wherein said active pharmacological agent is 2- (3-fluor-4-hydroxyphenyl) -7-vinyl-1,3-benzoxazol-5-ol, or a salt pharmaceutically acceptable thereof. Claim 23: A process for preparing the pharmaceutical formulation of any one of claims 1 to 21 comprising: (a) mixing the active pharmacological agent with the first diluent / filler component, the disintegrant component, and the second optional diluent / filler component, if present, to form an initial mixture; and (b) granulating said initial mixture with an aqueous solution comprising the wetting agent component to form a granulated mixture. |
priorityDate | 2006-03-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 29.