MY128971A - Solid-state form of celecoxib having enhanced bioavailability - Google Patents

Solid-state form of celecoxib having enhanced bioavailability

Info

Publication number
MY128971A
MY128971A MYPI20005730A MYPI20005730A MY128971A MY 128971 A MY128971 A MY 128971A MY PI20005730 A MYPI20005730 A MY PI20005730A MY PI20005730 A MYPI20005730 A MY PI20005730A MY 128971 A MY128971 A MY 128971A
Authority
MY
Malaysia
Prior art keywords
celecoxib
amorphous
drug substance
composition
solid
Prior art date
Application number
MYPI20005730A
Inventor
Michael J Hageman
Xiaorong He
Tugrul T Kararli
Lesley A Mackin
Patricia J Miyake
Brian R Rohrs
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 MY128971A publication Critical patent/MY128971A/en

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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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    • 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

THE SELECTIVE CYCLOOXYGENASE-2 INHIBITORY DRUG CELECOXIB IS PROVIDED IN AMORPHOUS FORM. ALSO PROVIDED IS A CELECOXIB DRUG SUBSTANCE WHEREIN THE CELECOXIB IS PRESENT, IN AT LEAST A DETECTABLE AMOUNT, AS AMORPHOUS CELECOXIB. ALSO PROVIDED IS A CELECOXIB-CRYSTALLIZATION INHIBITOR COMPOSITE COMPRISING PARTICLES OF AMORPHOUS CELECOXIB OR A CELECOXIB DRUG SUBSTANCE OF THE INVENTION IN INTIMATE ASSOCIATION WITH ONE OR MORE CRYSTALLIZATION INHIBITORS, FOR EXAMPLE POLYMERS. ALSO PROVIDED IS A PHARMACEUTICAL COMPOSITION COMPRISING SUCH A CELECOXIB-CRYSTALLIZATION INHIBITOR COMPOSITE AND ONE OR MORE EXCIPIENTS. ALSO PROVIDED ARE PROCESSES FOR PREPARING AMORPHOUS CELECOXIB, A CELECOXIB DRUG SUBSTANCE OF THE INVENTION, A CELECOXIB-CRYSTALLIZATION INHIBITOR COMPOSITION OF THE INVENTION, AND A PHARMACEUTICAL COMPOSITION OF THE INVENTION. ALSO PROVIDED IS A METHOD OF TREATING A MEDICAL CONDITION OR DISORDER IN A SUBJECT WHERE TREATMENT WITH A CYCLOOXYGENASE-2 INHIBITOR IS INDICATED, COMPRISING ADMINISTERING, FOR EXAMPLE ORALLY, A COMPOSITION OF THE INVENTION IN A THERAPEUTICALLY EFFECTIVE AMOUNT.(FIG 6)
MYPI20005730A 1999-12-08 2000-12-06 Solid-state form of celecoxib having enhanced bioavailability MY128971A (en)

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Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT1303265E (en) * 2000-07-20 2007-10-09 Lauras As Use of cox-2 inhibitors as immunostimulants in the treatment of hiv or aids
DE60233874D1 (en) 2001-06-22 2009-11-12 Pfizer Prod Inc PHARMACEUTICAL COMPOSITIONS CONTAIN DISPERSIONS FROM MEDICAMENTS AND NEUTRAL POLYMERS
WO2004026235A2 (en) * 2002-09-20 2004-04-01 Transform Pharmaceuticals, Inc. Pharmaceutical compositions with improved dissolution
US7790905B2 (en) 2002-02-15 2010-09-07 Mcneil-Ppc, Inc. Pharmaceutical propylene glycol solvate compositions
US7446107B2 (en) 2002-02-15 2008-11-04 Transform Pharmaceuticals, Inc. Crystalline forms of conazoles and methods of making and using the same
US7927613B2 (en) 2002-02-15 2011-04-19 University Of South Florida Pharmaceutical co-crystal compositions
WO2004061433A1 (en) * 2002-12-30 2004-07-22 Transform Pharmaceuticals, Inc. Pharmaceutical compositions with improved dissolution
US20030224006A1 (en) 2002-03-01 2003-12-04 Zaworotko Michael J. Multiple-component solid phases containing at least one active pharmaceutical ingredient
US7078526B2 (en) 2002-05-31 2006-07-18 Transform Pharmaceuticals, Inc. CIS-itraconazole crystalline forms and related processes, pharmaceutical compositions and methods
CA2484943A1 (en) * 2002-05-13 2004-05-21 Pharmacia Corporation Stable amorphous celecoxib composite and process therefor
IL165383A0 (en) * 2002-06-21 2006-01-15 Transform Pharmaceuticals Inc Pharmaceutical compositions with improved dissolution
US8183290B2 (en) 2002-12-30 2012-05-22 Mcneil-Ppc, Inc. Pharmaceutically acceptable propylene glycol solvate of naproxen
EP1579198A1 (en) * 2002-12-30 2005-09-28 Transform Pharmaceuticals, Inc. Pharmaceutical compositions with improved dissolution
EA014443B1 (en) * 2004-06-29 2010-12-30 Никомед Данмарк Апс Pharmaceutical composition (variants) and method for manufacturing thereof
GB0423103D0 (en) * 2004-10-19 2004-11-17 Boots Healthcare Int Ltd Therapeutic agents
WO2006097459A1 (en) * 2005-03-14 2006-09-21 Nycomed Gmbh Method for preventing cardiovascular diseases
CN103462920A (en) * 2012-06-06 2013-12-25 南京亿华药业有限公司 Oral cyclo-oxygenase-2 inhibitor Celecoxib composition
CN103524416B (en) * 2013-10-29 2016-08-17 湖北华世通生物医药科技有限公司 A kind of Novel celecoxib crystal form A and preparation method thereof
CN103539739B (en) * 2013-10-30 2016-02-10 中美华世通生物医药科技（武汉）有限公司 A kind of Novel celecoxib crystal form B and preparation method thereof
CN103508958A (en) * 2013-10-30 2014-01-15 中美华世通生物医药科技（武汉）有限公司 Novel celecoxib crystal form C and preparation method thereof
KR101476096B1 (en) * 2014-03-28 2014-12-24 대원제약주식회사 Pharmaceutical composition comprising celecoxib with improved solubility

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5474995A (en) * 1993-06-24 1995-12-12 Merck Frosst Canada, Inc. Phenyl heterocycles as cox-2 inhibitors
ATE212985T1 (en) * 1993-11-30 2002-02-15 Searle & Co TRICYCLIC SUBSTITUTED PYRAZOLYL-BENZENESULFONAMIDES AND THEIR USE AS CYCLOOXYGENASE II INHIBITORS
RU2200158C2 (en) * 1995-02-13 2003-03-10 Джи.Ди.Сирл энд Ко. Substituted isoxazoles, pharmaceutical composition based on thereof and method of inflammation suppression
US5633272A (en) * 1995-02-13 1997-05-27 Talley; John J. Substituted isoxazoles for the treatment of inflammation
US5756529A (en) * 1995-09-29 1998-05-26 G.D. Searle & Co. Substituted pyrazolyl benzenesulfonamides for use in veterinary therapies
US5981576A (en) * 1995-10-13 1999-11-09 Merck Frosst Canada, Inc. (Methylsulfonyl)phenyl-2-(5H)-furanones as COX-2 inhibitors
EP0863134A1 (en) * 1997-03-07 1998-09-09 Merck Frosst Canada Inc. 2-(3,5-difluorophenyl)-3-(4-(methyl-sulfonyl)phenyl)-2-cyclopenten-1-one useful as an inhibitor of cyclooxygenase-2
WO1999055380A1 (en) * 1998-04-27 1999-11-04 Pacific Northwest Cancer Foundation Nr-CAM GENE, NUCLEIC ACIDS AND NUCLEIC ACID PRODUCTS FOR THERAPEUTIC AND DIAGNOSTIC USES FOR TUMORS

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KR20020002386A (en) 2002-01-09
CO5251445A1 (en) 2003-02-28
PE20010911A1 (en) 2001-09-10
ECSP003807A (en) 2005-07-06
BG105808A (en) 2002-09-30
HUP0200580A2 (en) 2002-11-28
ES2236011T3 (en) 2005-07-16
EA200401397A1 (en) 2005-08-25
ZA200107146B (en) 2002-08-29
AR030039A1 (en) 2003-08-13
SV2002000235A (en) 2002-06-13
YU57801A (en) 2005-07-19
CZ20012875A3 (en) 2002-02-13
KR100717570B1 (en) 2007-05-15
WO2001041536A2 (en) 2001-06-14
OA11831A (en) 2005-08-23
CN1216869C (en) 2005-08-31
PT1150959E (en) 2008-04-21
BG65239B1 (en) 2007-09-28
PT1150960E (en) 2005-06-30
MY128366A (en) 2007-01-31
AU2041201A (en) 2001-06-18
AR027897A1 (en) 2003-04-16
CN1411447A (en) 2003-04-16
ZA200107149B (en) 2003-02-28
HUP0200580A3 (en) 2002-12-28
NZ529933A (en) 2005-06-24

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