WO2011088806A3 - A method of industrial production of an amorphous form of atorvastatin with a high specific surface area and its use in a dosage form - Google Patents

A method of industrial production of an amorphous form of atorvastatin with a high specific surface area and its use in a dosage form Download PDF

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Publication number
WO2011088806A3
WO2011088806A3 PCT/CZ2011/000003 CZ2011000003W WO2011088806A3 WO 2011088806 A3 WO2011088806 A3 WO 2011088806A3 CZ 2011000003 W CZ2011000003 W CZ 2011000003W WO 2011088806 A3 WO2011088806 A3 WO 2011088806A3
Authority
WO
WIPO (PCT)
Prior art keywords
atorvastatin
surface area
specific surface
high specific
industrial production
Prior art date
Application number
PCT/CZ2011/000003
Other languages
French (fr)
Other versions
WO2011088806A2 (en
Inventor
Jan Stach
Martin Holan
Jaroslav Havlicek
Stanislav Simek
Jan Linek
Hana Brusova
Stanislav Radl
Michaela Dubovska
Alena Prokopova
Jaroslav Riha
Pavel Sebek
Original Assignee
Zentiva, K.S.
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 Zentiva, K.S. filed Critical Zentiva, K.S.
Priority to EP11707780A priority Critical patent/EP2526089A2/en
Publication of WO2011088806A2 publication Critical patent/WO2011088806A2/en
Publication of WO2011088806A3 publication Critical patent/WO2011088806A3/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics

Abstract

The invention deals with an amorphous form of the hemicalcium salt of (3R,5R) 7-[3-phenyl- 4-phenylcarbamoyl-2-(4-fluorophenyl)-5-isopropylpyrrol-1-y1]-3,5-dihydroxyheptanoic acid (atorvastatin of formula I) with a high specific surface area, based on controlled precipitation, and its use in a medical dosage form. (I)
PCT/CZ2011/000003 2010-01-19 2011-01-12 A method of industrial production of an amorphous form of atorvastatin with a high specific surface area and its use in a dosage form WO2011088806A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EP11707780A EP2526089A2 (en) 2010-01-19 2011-01-12 A method of industrial production of an amorphous form of atorvastatin with a high specific surface area and its use in a dosage form

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CZ20100039A CZ201039A3 (en) 2010-01-19 2010-01-19 Method of industrial production of amorphous form of (3R,5R) 7-[3-phenyl-4-phenylcarbamoyl-2-(4-fluorophenyl)-5-isopropylpyrrol-1-yl]-3,5-dihydroxyheptanoic acid hemicalcium salt (atorvastatin) with low specific surface and use thereof in medicamento
CZPV2010-39 2010-01-19

Publications (2)

Publication Number Publication Date
WO2011088806A2 WO2011088806A2 (en) 2011-07-28
WO2011088806A3 true WO2011088806A3 (en) 2011-09-22

Family

ID=43902821

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CZ2011/000003 WO2011088806A2 (en) 2010-01-19 2011-01-12 A method of industrial production of an amorphous form of atorvastatin with a high specific surface area and its use in a dosage form

Country Status (3)

Country Link
EP (1) EP2526089A2 (en)
CZ (1) CZ201039A3 (en)
WO (1) WO2011088806A2 (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG11201505680RA (en) 2013-02-21 2015-09-29 Pfizer Solid forms of a selective cdk4/6 inhibitor

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CZ2003987A3 (en) * 2003-04-08 2004-11-10 Zentiva A. S. Process for preparing amorphous form of hemi calcium salt of (3R,5R) 7-[3-phenyl-4-phenylcarbamoyl-2-(4-fluorophenyl)-5-isopropylpyrrol-1-yl]-3,5-dihydroxyheptanoic acid (atorvastatin) suitable for industrial production and apparatus for making the same
US20090124817A1 (en) * 2007-11-09 2009-05-14 The Industry & Academic Cooperation In Chungnam National University Process for Preparing Amorphous Atorvastatin Calcium Nanoparticles

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4681893A (en) 1986-05-30 1987-07-21 Warner-Lambert Company Trans-6-[2-(3- or 4-carboxamido-substituted pyrrol-1-yl)alkyl]-4-hydroxypyran-2-one inhibitors of cholesterol synthesis
FI94339C (en) 1989-07-21 1995-08-25 Warner Lambert Co Process for the preparation of pharmaceutically acceptable [R- (R *, R *)] - 2- (4-fluorophenyl) -, - dihydroxy-5- (1-methylethyl) -3-phenyl-4 - [(phenylamino) carbonyl] -1H- for the preparation of pyrrole-1-heptanoic acid and its pharmaceutically acceptable salts
HRP960312B1 (en) 1995-07-17 2001-10-31 Warner Lambert Co NOVEL PROCESS FOR THE PRODUCTION OF AMORPHOUS /R-(R*, R*)/-2-(4-FLUOROPHENYL)-"beta", "delta"-DIHYDROXY-5-PHENYL-4-/(PHENYLAMINO)CARBONYL/-1H-PYRROLE -1-HEPTANOIC ACID CALCIUM SALT (2 : 1)
JP3296564B2 (en) 1995-07-17 2002-07-02 ワーナー−ランバート・コンパニー Crystalline [R- (R ▲ *, R ▲ *)]-2- (4-fluorophenyl) -β, δ-dihydroxy-5- (1-methylethyl) -3-phenyl-4 -[(Phenylamino) carbonyl] -1H-pyrrole-1-heptanoic acid hemicalcium salt (atorvastatin)
HRP960313B1 (en) 1995-07-17 2002-08-31 Warner Lambert Co Form iii crystalline (r- (r*, r*)-2- (4-fluorophenyl) -beta-delta-hydroxy-5-(1-methylethyl) -3-phenyl-4- ((phenylamino) carbonyl -1h-pyrrole-1-heptanoic acid calcium salt (2:1)
IN191236B (en) 1999-05-25 2003-10-11 Ranbaxy Lab Ltd
HU226640B1 (en) 1999-10-18 2009-05-28 Egis Gyogyszergyar Nyilvanosan Process for producing amorphous atorvastatin calcium salt
WO2001036384A1 (en) 1999-11-17 2001-05-25 Teva Pharmaceutical Industries Ltd. Polymorphic form of atorvastatin calcium
SI20425A (en) 1999-12-10 2001-06-30 LEK tovarna farmacevtskih in kemi�nih izdelkov d.d. Preparation of amorphous atorvastatin
WO2002008368A1 (en) 2000-07-21 2002-01-31 Cargill, Incorporated Method for removing contaminants from vegetable oil and lecithin
JP2002038174A (en) 2000-07-24 2002-02-06 Nippon Mitsubishi Oil Corp Refrigerating machine oil composition
WO2002057228A1 (en) 2001-01-17 2002-07-25 Biocon India Limited Atorvastatin calcium
EP1423364B1 (en) 2001-06-29 2015-11-04 Warner-Lambert Company LLC Crystalline forms of [r-(r*,r*)]-2-(4-fluorophenyl)-beta, delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-phenylamino)carbonyl]-1h-pyrrole-1-heptanoic acid calcium salt (2:1) (atorvastatin)
EP1572638A4 (en) 2001-08-31 2010-05-05 Morepen Lab Ltd An improved process for the preparation of amorphous atorvastatin calcium salt (2:1)
CZ296967B6 (en) 2002-02-01 2006-08-16 Zentiva, A.S. Process for preparing amorphous form of hemicalcium salt of (3R,5R)7-[3-phenyl-phenylcarbamoyl-2-(4-fluorophenyl)-5-isopropylpyrrol-l-yl]-3,5-dihydroxyheptanoic acid (atorvastatin)

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CZ2003987A3 (en) * 2003-04-08 2004-11-10 Zentiva A. S. Process for preparing amorphous form of hemi calcium salt of (3R,5R) 7-[3-phenyl-4-phenylcarbamoyl-2-(4-fluorophenyl)-5-isopropylpyrrol-1-yl]-3,5-dihydroxyheptanoic acid (atorvastatin) suitable for industrial production and apparatus for making the same
US20090124817A1 (en) * 2007-11-09 2009-05-14 The Industry & Academic Cooperation In Chungnam National University Process for Preparing Amorphous Atorvastatin Calcium Nanoparticles

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
"FDA Approval package for Lipitor", 7 April 2000 (2000-04-07), XP002635528, Retrieved from the Internet <URL:www.fda.org> *
"Ph. Eur. 4", 2004, COUNCIL OF EUROPE EQDM, XP002635527 *
"Ph. Eur. 7.1 monograph on Atorvastatin", 2010, COUNCIL OF EUROPE EQDM, XP002636005 *
ARUNKUMAR N ET AL: "Preparation and solid state characterization of atorvastatin nanosuspensions for enhanced solubility and dissolution", INTERNATIONAL JOURNAL OF PHARMTECH RESEARCH, SHPINX KNOWLEDGE HOUSE, IN, vol. 1, no. 4, 1 October 2009 (2009-10-01), pages 1725 - 1730, XP008136161, ISSN: 0974-4304, Retrieved from the Internet <URL:http://sphinxsai.com/PTVOL4/index_pharm_1_vol4.htm> *
KIM M S ET AL: "Preparation, characterization and in vivo evaluation of amorphous atorvastatin calcium nanoparticles using supercritical antisolvent (SAS) process", EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, ELSEVIER SCIENCE PUBLISHERS B.V., AMSTERDAM, NL, vol. 69, no. 2, 1 June 2008 (2008-06-01), pages 454 - 465, XP022664260, ISSN: 0939-6411, [retrieved on 20080118], DOI: DOI:10.1016/J.EJPB.2008.01.007 *
ZHANG H X ET AL: "Micronization of atorvastatin calcium by antisolvent precipitation process", INTERNATIONAL JOURNAL OF PHARMACEUTICS, ELSEVIER BV, NL, vol. 374, no. 1-2, 5 June 2009 (2009-06-05), pages 106 - 113, XP026109001, ISSN: 0378-5173, [retrieved on 20090304], DOI: DOI:10.1016/J.IJPHARM.2009.02.015 *

Also Published As

Publication number Publication date
CZ201039A3 (en) 2011-07-27
WO2011088806A2 (en) 2011-07-28
EP2526089A2 (en) 2012-11-28

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