CO5251445A1 - CELECOXIB SOLID STATE FORM THAT HAS IMPROVED BIODISPONIBILITY - Google Patents

CELECOXIB SOLID STATE FORM THAT HAS IMPROVED BIODISPONIBILITY

Info

Publication number
CO5251445A1
CO5251445A1 CO00094077A CO00094077A CO5251445A1 CO 5251445 A1 CO5251445 A1 CO 5251445A1 CO 00094077 A CO00094077 A CO 00094077A CO 00094077 A CO00094077 A CO 00094077A CO 5251445 A1 CO5251445 A1 CO 5251445A1
Authority
CO
Colombia
Prior art keywords
celecoxib
drug substance
amorphous
solid state
state form
Prior art date
Application number
CO00094077A
Other languages
Spanish (es)
Inventor
Michael J Hageman
He Xiaorong
T Kararli Tugrul
A Mackin Lesley
Patricia J Miyake
Brian R Rohis
Kevin J Stefanski
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 CO5251445A1 publication Critical patent/CO5251445A1/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • 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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    • 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
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    • 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
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Abstract

Celecoxib amorfo. Una sustancia de droga celecoxib donde el celecoxib está presente, en por lo menos una cantidad detectable, como celecoxib amorfo. Un compuesto inhibidor de cristalización de celecoxib que comprende partículas de celecoxib amorfo o una sustancia de droga celecoxib de alguna de las Reivindicaciones 2 a 4 en intima asociación con uno o más inhibidor (es) de cristalización en una cantidad efectiva para reducir la transformación de celecoxib amorfo a celecoxib cristalino. 1Un proceso para preparar a sustancia de droga celecoxib, el proceso que comprende: (a) fundir celecoxib; (b) enfriar rápidamente el resultante celecoxib fundido para formar una sustancia de droga celecoxib donde el celecoxib está presente, en por lo menos una cantidad detectable, en forma amorfa; y opcionalmente (c) triunfar la sustancia de droga celecoxib para formar un polvo de sustancia de droga celecoxib.Amorphous Celecoxib A drug substance celecoxib where celecoxib is present, in at least a detectable amount, as amorphous celecoxib. A celecoxib crystallization inhibitor compound comprising amorphous celecoxib particles or a celecoxib drug substance of any one of Claims 2 to 4 in intimate association with one or more crystallization inhibitor (s) in an amount effective to reduce celecoxib transformation amorphous to crystalline celecoxib. 1 A process for preparing the drug substance celecoxib, the process comprising: (a) melting celecoxib; (b) rapidly cooling the resulting molten celecoxib to form a celecoxib drug substance where celecoxib is present, in at least a detectable amount, in amorphous form; and optionally (c) triumph the drug substance celecoxib to form a powder of drug substance celecoxib.

CO00094077A 1999-12-08 2000-12-11 CELECOXIB SOLID STATE FORM THAT HAS IMPROVED BIODISPONIBILITY CO5251445A1 (en)

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TWI276435B (en) 2007-03-21
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