ES2162764B1 - POLYMORPHIC FORM OF AZITHROMYCIN DIHYDRATE, AND ITS DEOBTENTION PROCEDURE. - Google Patents

POLYMORPHIC FORM OF AZITHROMYCIN DIHYDRATE, AND ITS DEOBTENTION PROCEDURE.

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Publication number
ES2162764B1
ES2162764B1 ES200001226A ES200001226A ES2162764B1 ES 2162764 B1 ES2162764 B1 ES 2162764B1 ES 200001226 A ES200001226 A ES 200001226A ES 200001226 A ES200001226 A ES 200001226A ES 2162764 B1 ES2162764 B1 ES 2162764B1
Authority
ES
Spain
Prior art keywords
polymorphic form
procedure
dihydrate
azithromycin
azithromycin dihydrate
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
ES200001226A
Other languages
Spanish (es)
Other versions
ES2162764A1 (en
Inventor
Dominguez Ramon Asensio
Rodriguez M Carmen Cruzado
Tejo Luis Angel Diaz
Ribe Rosa Nomen
Cebrian Julia Sempere
Bilbao Jose Ignacio Borrell
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Ercros Industrial SA
Original Assignee
Ercros Industrial SA
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 Ercros Industrial SA filed Critical Ercros Industrial SA
Priority to ES200001226A priority Critical patent/ES2162764B1/en
Priority to PT10256501A priority patent/PT102565A/en
Priority to AU58409/01A priority patent/AU5840901A/en
Priority to PCT/ES2001/000183 priority patent/WO2001087912A1/en
Publication of ES2162764A1 publication Critical patent/ES2162764A1/en
Application granted granted Critical
Publication of ES2162764B1 publication Critical patent/ES2162764B1/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/04—Heterocyclic radicals containing only oxygen as ring hetero atoms
    • C07H17/08—Hetero rings containing eight or more ring members, e.g. erythromycins

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)

Abstract

Forma polimórfica del dihidrato de azitromicina, y su procedimiento de obtención. La invención se refiere, a una forma polimórfica del dihidrato de azitromicina (9-desoxo-9a- aza-9a-metil-9a-homoeritromici-na A) que presenta una endoterma en calorimetría diferencial de barrido (DSC) a 139ºC, cuando se registra en crisol abierto de aluminio con una velocidad de calentamiento de 20ºC/minuto, y la presenta a 143,7 +- 0,5ºC con un calor de fusión 54,6 +- 1,6 J/g, cuando se registra en crisol capilar con una velocidad de calentamiento de 10ºC/minuto. También es objeto de la invención el procedimiento para la obtención de dicha forma polimórfica de azitromizina dihidrato. Según el mismo se trata azitromicina monihidrato higroscópica con acetona seguido de la adición de agua a 35-40ºC, posterior agitación a dicha temperatura con sembrado opcional de cristales de dicho polimorfo y ulterior adición de agua seguida de enfriamiento a 5ºC.Polymorphic form of azithromycin dihydrate, and its procedure. The invention relates to a polymorphic form of azithromycin dihydrate (9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin-A) which has an endotherm in differential scanning calorimetry (DSC) at 139 ° C, when recorded in an open aluminum crucible with a heating rate of 20 ° C / minute, and presents it at 143.7 + - 0.5 ° C with a heat of fusion 54.6 + - 1.6 J / g, when recorded in a crucible capillary with a heating rate of 10 ° C / minute. The process for obtaining said polymorphic form of azithromizine dihydrate is also an object of the invention. According to it, hygroscopic azithromycin monhydrochloride is treated with acetone followed by the addition of water at 35-40 ° C, subsequent stirring at said temperature with optional seeding of crystals of said polymorph and subsequent addition of water followed by cooling at 5 ° C.

ES200001226A 2000-05-17 2000-05-17 POLYMORPHIC FORM OF AZITHROMYCIN DIHYDRATE, AND ITS DEOBTENTION PROCEDURE. Expired - Fee Related ES2162764B1 (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
ES200001226A ES2162764B1 (en) 2000-05-17 2000-05-17 POLYMORPHIC FORM OF AZITHROMYCIN DIHYDRATE, AND ITS DEOBTENTION PROCEDURE.
PT10256501A PT102565A (en) 2000-05-17 2001-02-12 POLYMERIC FORM OF AZITHROMYCINE DIHYDRATE AND PROCESS FOR PREPARATION
AU58409/01A AU5840901A (en) 2000-05-17 2001-05-11 Polymorphic form of azithromycin dihydrate and preparation method thereof
PCT/ES2001/000183 WO2001087912A1 (en) 2000-05-17 2001-05-11 Polymorphic form of azithromycin dihydrate and preparation method thereof

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
ES200001226A ES2162764B1 (en) 2000-05-17 2000-05-17 POLYMORPHIC FORM OF AZITHROMYCIN DIHYDRATE, AND ITS DEOBTENTION PROCEDURE.

Publications (2)

Publication Number Publication Date
ES2162764A1 ES2162764A1 (en) 2002-01-01
ES2162764B1 true ES2162764B1 (en) 2003-04-01

Family

ID=8493527

Family Applications (1)

Application Number Title Priority Date Filing Date
ES200001226A Expired - Fee Related ES2162764B1 (en) 2000-05-17 2000-05-17 POLYMORPHIC FORM OF AZITHROMYCIN DIHYDRATE, AND ITS DEOBTENTION PROCEDURE.

Country Status (4)

Country Link
AU (1) AU5840901A (en)
ES (1) ES2162764B1 (en)
PT (1) PT102565A (en)
WO (1) WO2001087912A1 (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108562380A (en) * 2018-04-15 2018-09-21 重庆大学 A kind of powder exothermic mixture heating power test method

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HRP20020231A2 (en) * 2002-03-18 2003-12-31 Pliva D D ISOSTRUCTURAL PSEUDOPOLYMORPHS OF 9-DEOXO-9a-AZA-9a-METHYL-9a-HOMOERYTHROMYCIN A
US6861413B2 (en) 2001-05-22 2005-03-01 Pfizer Inc. Stable non-dihydrate azithromycin oral suspensions
JP2004530703A (en) 2001-05-22 2004-10-07 ファイザー・プロダクツ・インク Crystalline azithromycin
HRP20020614A2 (en) 2002-07-22 2004-06-30 PLIVA-ISTRAŽIVAČKI INSTITUT d.o.o. Rhombic pseudopolymorph of 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin a
US7683162B2 (en) 2004-08-30 2010-03-23 Taro Pharmaceutical Industries Limited Process of preparing a crystalline azithromycin monohydrate
US20090318375A1 (en) * 2005-06-08 2009-12-24 Hanmi Pharm Co., Ltd Crystalline Azithromycin L-Malate Monohydrate and Pharmaceutical Composition Containing Same
US8106111B2 (en) 2009-05-15 2012-01-31 Eastman Chemical Company Antimicrobial effect of cycloaliphatic diol antimicrobial agents in coating compositions

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2066324C1 (en) * 1987-07-09 1996-09-10 Пфайзер Инк. Crystalline azithromycin dehydrate, and process for preparation thereof
ES2122905B1 (en) * 1996-07-11 1999-11-16 Astur Pharma Sa SYNTHESIS OF 11,12-HYDROGENOORTOBORATE 9-DESOXO-9A-AZA-11,12-DESOXI-9A-METHYL-9A-HOMOERYTHROMYCIN A. A PROCEDURE FOR THE PREPARATION OF 9-DESOXO-9A-AZA-9A-METHYL-9A -HOMOERYTHROMYCIN TO DIHYDRATE (AZYTHROMYCIN DIHYDRATE).
PT102130A (en) * 1998-03-13 1999-09-30 Hovione Sociedade Quimica S A METHOD FOR PREPARING AZITHROMYCY DIHYDRATE
ES2177373B1 (en) * 1999-11-26 2003-11-01 Astur Pharma Sa PREPARATION OF AZITHROMYCIN IN ITS NON-CRYSTALLINE FORM
CA2396426A1 (en) * 2000-01-04 2001-07-12 Teva Pharmaceutical Industries Ltd. Preparation method of azithromycin dihydrate

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108562380A (en) * 2018-04-15 2018-09-21 重庆大学 A kind of powder exothermic mixture heating power test method

Also Published As

Publication number Publication date
ES2162764A1 (en) 2002-01-01
AU5840901A (en) 2001-11-26
WO2001087912A1 (en) 2001-11-22
PT102565A (en) 2001-11-30

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