BR112012014926A2 - composição compreendendo uma forma vítrea não cristalina e amorfa de azitromicina - Google Patents

composição compreendendo uma forma vítrea não cristalina e amorfa de azitromicina

Info

Publication number
BR112012014926A2
BR112012014926A2 BR112012014926A BR112012014926A BR112012014926A2 BR 112012014926 A2 BR112012014926 A2 BR 112012014926A2 BR 112012014926 A BR112012014926 A BR 112012014926A BR 112012014926 A BR112012014926 A BR 112012014926A BR 112012014926 A2 BR112012014926 A2 BR 112012014926A2
Authority
BR
Brazil
Prior art keywords
azithromycin
crystalline
composition
amorphous
methyl
Prior art date
Application number
BR112012014926A
Other languages
English (en)
Inventor
Marique Aucamp
Roelf Willem Odendaal
Wilna Liebenberg
Original Assignee
Univ Northwest
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 Univ Northwest filed Critical Univ Northwest
Publication of BR112012014926A2 publication Critical patent/BR112012014926A2/pt

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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00—Processes for the preparation of sugar derivatives

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Immunology (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Cosmetics (AREA)
  • Saccharide Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

composição compreendendo uma forma vítrea não cristalina e amorfa de azitromicina. a presente invenção refere-se a ima forma vítrea não cristalina e amorfa (2r,3s,4r,5r,8r,10r,11r,12s,13s,14r) -2-etil-3,4, 10-triidroxi-3,5,6,8,10,12,14- heptametil-15-oxo- 11- {[3,4,6- trideoxi-3 -(dimetilamino) -<225>- d-xilo- hexopiranosil]oxi}- 1- oxa- 6- azaciclopentadec- 13-il 2,6-dideoxi-3-c-metil-3-o-metil-a-l-ribo- hexopiranosídeo ou azitromicina tendo um padrão infravermelho apresentado picos relativamente amplos característicos em aproximadamente 3500 e 1727 cm^ -1^ e picos característicos em aproximadamente 2970 e 2938 cm^ -1^. a invenção adicionalmente se refere a um método de preparação consistindo em aumentar a solubilidade da azitromicina incluindo as etapas de selecionar azitromicina anídrica, mono-hidratada ou di-hidratada; elevar a temperatura da azitromicina até acima do ponto de fusão da mesma; e reduzir a temperatura da fusão suficientemente para possibilitar que endureça em uma forma vítrea não cristalina e amorfa (forma-ii) de azitromicina tendo solubilidade relativamente aumentada sem diminuir a estabilidade estrutural da mesma.
BR112012014926A 2009-12-18 2010-12-15 composição compreendendo uma forma vítrea não cristalina e amorfa de azitromicina BR112012014926A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
ZA200909098 2009-12-18
PCT/IB2010/055842 WO2011073927A1 (en) 2009-12-18 2010-12-15 Composition comprising an amorphous non- crystalline glass form of azithromycin

Publications (1)

Publication Number Publication Date
BR112012014926A2 true BR112012014926A2 (pt) 2015-09-15

Family

ID=43709135

Family Applications (2)

Application Number Title Priority Date Filing Date
BR112012014941A BR112012014941A2 (pt) 2009-12-18 2010-12-15 composição compreendendo uam forma vítrea não cristalina e amorfa de roxitromicina
BR112012014926A BR112012014926A2 (pt) 2009-12-18 2010-12-15 composição compreendendo uma forma vítrea não cristalina e amorfa de azitromicina

Family Applications Before (1)

Application Number Title Priority Date Filing Date
BR112012014941A BR112012014941A2 (pt) 2009-12-18 2010-12-15 composição compreendendo uam forma vítrea não cristalina e amorfa de roxitromicina

Country Status (12)

Country Link
US (2) US8901089B2 (pt)
EP (2) EP2513130B1 (pt)
JP (1) JP2013514346A (pt)
KR (1) KR20120107989A (pt)
CN (2) CN102712670A (pt)
AP (1) AP2012006312A0 (pt)
AU (2) AU2010331866A1 (pt)
BR (2) BR112012014941A2 (pt)
CA (2) CA2784494C (pt)
RU (1) RU2012130435A (pt)
WO (2) WO2011073927A1 (pt)
ZA (2) ZA201204409B (pt)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102286045B (zh) * 2011-09-07 2013-08-07 山东罗欣药业股份有限公司 罗红霉素一水合物结晶、其制备方法及含该结晶和盐酸氨溴索组合的组合物干混悬剂
WO2013088274A1 (en) 2011-12-14 2013-06-20 Wockhardt Limited Anhydrous amorphous azithromycin composition free of azithromycin dihydrate
CN106589022B (zh) * 2016-11-16 2019-06-18 山东裕欣药业有限公司 一种罗红霉素化合物及其制备方法、药物组合物

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE201026T1 (de) * 1996-08-07 2001-05-15 Russinsky Ltd Verfahren zur herstellung von salzen von erythromicyn, roxithromicyn, clarythromicyn und azithromycin
CA2245398C (en) 1998-08-21 2002-01-29 Apotex Inc. Azithromycin monohydrate isopropanol clathrate and methods for the manufacture thereof
WO2000023081A1 (en) * 1998-10-20 2000-04-27 Lauteral Limited Derivatives of erythromycin, clarithromycin, roxithromycin or azithromycin with antibiotic and mucolytic activity
ES2177373B1 (es) * 1999-11-26 2003-11-01 Astur Pharma Sa Preparacion de azitromicina en su forma no cristalina
EP1671979B1 (en) * 2001-05-22 2008-08-13 Pfizer Products Inc. New Cristal Form of 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
JP2009501206A (ja) * 2005-07-14 2009-01-15 ファイザー・プロダクツ・インク 非晶質アジスロマイシン粒子の生成方法

Also Published As

Publication number Publication date
US20130045936A1 (en) 2013-02-21
BR112012014941A2 (pt) 2015-09-15
EP2513130A1 (en) 2012-10-24
AU2010331867A1 (en) 2012-07-12
AU2010331866A1 (en) 2012-07-12
RU2012130435A (ru) 2014-01-27
CN102822187A (zh) 2012-12-12
EP2513130B1 (en) 2016-05-25
ZA201204409B (en) 2013-02-27
WO2011073927A1 (en) 2011-06-23
US20130059805A1 (en) 2013-03-07
ZA201204411B (en) 2013-02-27
EP2513129A1 (en) 2012-10-24
JP2013514346A (ja) 2013-04-25
CA2784494C (en) 2019-03-12
US8901089B2 (en) 2014-12-02
KR20120107989A (ko) 2012-10-04
CA2784494A1 (en) 2011-06-23
CN102712670A (zh) 2012-10-03
WO2011073926A1 (en) 2011-06-23
AP2012006312A0 (en) 2012-06-30
CN102822187B (zh) 2015-05-20
CA2784497A1 (en) 2011-06-23

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Legal Events

Date Code Title Description
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE AS 4A E 5A ANUIDADES.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: EM VIRTUDE DO ARQUIVAMENTO PUBLICADO NA RPI 2343 DE 01-12-2015 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDO O ARQUIVAMENTO DO PEDIDO DE PATENTE, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013.