PE20010911A1 - SOLID STATE FORM OF CELECOXIB THAT HAS IMPROVED BIODAVAILABILITY - Google Patents

SOLID STATE FORM OF CELECOXIB THAT HAS IMPROVED BIODAVAILABILITY

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Publication number
PE20010911A1
PE20010911A1 PE2000001299A PE0012992000A PE20010911A1 PE 20010911 A1 PE20010911 A1 PE 20010911A1 PE 2000001299 A PE2000001299 A PE 2000001299A PE 0012992000 A PE0012992000 A PE 0012992000A PE 20010911 A1 PE20010911 A1 PE 20010911A1
Authority
PE
Peru
Prior art keywords
celecoxib
amorphous
crystalization
refers
biodavailability
Prior art date
Application number
PE2000001299A
Other languages
Spanish (es)
Inventor
Michael J Hageman
Xiaorong He
Tugrul T Kararli
Kevin J Stefanski
Patricia J Miyake
Brian R Rohrs
Lesley A Mackin
Original Assignee
Pharmacia Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Pharmacia Corp filed Critical Pharmacia Corp
Publication of PE20010911A1 publication Critical patent/PE20010911A1/en

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    • 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
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    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D311/58—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4

Abstract

SE REFIERE A CELECOXIB AMORFO (4-[5-(4-METILFENIL)-3-TRIFLUOROMETIL)-1H-PIRAZOL-1-IL]BENCENOSULFONAMIDA, DE FORMULA I UTILIZANDOSE DE 10% A 100% EN PESO DE CELECOXIB; TAMBIEN SE REFIERE A UN COMPUESTO INHIBIDOR DE CRISTALIZACION DE CELECOXIB QUE CONTIENE CELECOXIB AMORFO EN INTIMA ASOCIACION PARA REDUCIR LA TRANSFORMACION DE CELECOXIB AMORFO A CRISTALINO; TAL COMO UN POLIMERO (POLIVINILPIRROLIDONA, HIDROXIPROPILMETILCELULOSA); UTILIZANDOSE DE 10% A 80% EN PESO DEL COMPUESTO. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION QUE COMPRENDE a)FUNDIR CELECOXIB, b)ENFRIAR RAPIDAMENTE CELECOXIB FUNDIDO RESULTANTE PARA FORMAR CELECOXIB EN FORMA AMORFA, c)TRITURAR CELECOXIB Y FORMAR POLVO; UN PROCESO PARA LA PREPARACION DE UN INHIBIDOR DE LA CRISTALIZACION DE CELECOXIB QUE COMPRENDE: a)DISOLVER CELECOXIB Y UNO O MAS INHIBIDORES DE CRISTALIZACION EN UN SOLVENTE (ISOPROPANOL) PARA FORMAR LA SOLUCION; b)SECAR LA SOLUCION (PULVERIZACION EN SECO) Y FORMAR UN COMPUESTO INHIBIDOR DE LA CRISTALIZACION DE CELECOXIB EN FORMA AMORFAREFERS TO AMORPHOUS CELECOXIB (4- [5- (4-METHYLPHENYL) -3-TRIFLUOROMETHYL) -1H-PIRAZOL-1-IL] BENZENOSULFONAMIDE, OF FORMULA I USING 10% TO 100% BY WEIGHT OF CELECOXIB; IT ALSO REFERS TO A CELECOXIB CRYSTALIZATION INHIBITING COMPOUND CONTAINING AMORPHOUS CELECOXIB IN INTIMATE ASSOCIATION TO REDUCE THE TRANSFORMATION OF AMORPHOUS CELECOXIB TO CRYSTALLINE; SUCH AS A POLYMER (POLYVINYLPYRROLIDONE, HYDROXYPROPYLMETHYLCELLULOSE); USING FROM 10% TO 80% BY WEIGHT OF THE COMPOUND. IT ALSO REFERS TO A PROCEDURE FOR THE PREPARATION THAT INCLUDES a) MELTING CELECOXIB, b) QUICKLY COOLING THE RESULTING MELTED CELECOXIB TO FORM CELECOXIB IN AN AMORPHOUS FORM, c) CRUSHING CELECOXIB AND FORMING POWDER; A PROCESS FOR THE PREPARATION OF A CELECOXIB CRYSTALIZATION INHIBITOR, INCLUDING: a) DISSOLVING CELECOXIB AND ONE OR MORE CRYSTALIZATION INHIBITORS IN A SOLVENT (ISOPROPANOL) TO FORM THE SOLUTION; b) DRY THE SOLUTION (DRY SPRAY) AND FORM AN INHIBITOR COMPOUND OF THE CELECOXIB CRYSTALIZATION IN AMORPHOUS FORM

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