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WO2005060361A2 - Formulations pharmaceutiques pour l'itraconazole - Google Patents

Formulations pharmaceutiques pour l'itraconazole Download PDF

Info

Publication number
WO2005060361A2
WO2005060361A2 PCT/KR2004/003422 KR2004003422W WO2005060361A2 WO 2005060361 A2 WO2005060361 A2 WO 2005060361A2 KR 2004003422 W KR2004003422 W KR 2004003422W WO 2005060361 A2 WO2005060361 A2 WO 2005060361A2
Authority
WO
WIPO (PCT)
Prior art keywords
itraconazole
pharmaceutical composition
block
polylactic acid
acid derivative
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.)
Ceased
Application number
PCT/KR2004/003422
Other languages
English (en)
Other versions
WO2005060361A3 (fr
Inventor
Hye-Jeong Yoon
Min Hyo Seo
Jeong-Kyung Kim
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.)
Samyang Corp
Original Assignee
Samyang 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 Samyang Corp filed Critical Samyang Corp
Publication of WO2005060361A2 publication Critical patent/WO2005060361A2/fr
Publication of WO2005060361A3 publication Critical patent/WO2005060361A3/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A61K9/0024—Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/1075—Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/51—Nanocapsules; Nanoparticles
    • A61K9/5107—Excipients; Inactive ingredients
    • A61K9/513—Organic macromolecular compounds; Dendrimers
    • A61K9/5146—Organic macromolecular compounds; Dendrimers obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyamines, polyanhydrides
    • A61K9/5153—Polyesters, e.g. poly(lactide-co-glycolide)

Definitions

  • water insoluble azole compounds include oxiconazole, bifonazole, isoconazole, isoconazole nitrate, terconazole, clotrimazole, econazole nitrate, ketoconazole, miconazole, miconazole nitrate, sertaconazole nitrate, itraconazole and saperconazole.
  • the molecular formula of itraconazole is C 35 H oCl 2 N 8 O 4 and its molecular weight is 705.64.
  • biodegradable or “biodegradation” is defined as the conversion of materials into less complex intermediates or end products by solubilization hydrolysis, or by the action of biologically formed entities which can be enzymes or other products of the organism.
  • biocompatible means materials or the intermediates or end products of materials formed by solubilization hydrolysis, or by the action of biologically formed entities which can be enzymes or other products of the organism and which cause no adverse effect on the body.
  • administering and similar terms mean delivering the composition to an individual being treated such that the composition is capable of being circulated systemically.
  • the present invention relates to a pharmaceutical composition
  • a pharmaceutical composition comprising 0.1-30.0 wt.% of itraconazole, 5.0-99.9 wt.% of a polylactic acid derivative having a carboxylic acid terminal group, and 0.0-94.9 wt.%) of an amphiphilic block copolymer comprised of a hydrophihc block and a hydrophobic block.
  • the pharmaceutical composition comprises 0.1- 20.0 wt.% of itraconazole, 20.0-99.9 wt.% of a polylactic acid derivative, and 0.0-79.9 wt.% of an amphiphilic block copolymer.
  • the terminal carboxyl group of the polylactic acid derivative is combined with a di- or tri-valent metal ion where 0.5-4.0 equivalents of di- or tri-valent metal ion per equivalent of carboxyl group are combined.
  • the metal ions include Ca 2+ , Mg 2+ , Ba 2+ , Mn 2+ , Ni 2+ , Cu 2+ , Zn 2+ , Cr 3+ , Fe 3+ , and Al 3+ , more preferably Ca 2+ .

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nanotechnology (AREA)
  • Dermatology (AREA)
  • Biomedical Technology (AREA)
  • Physics & Mathematics (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Optics & Photonics (AREA)
  • Neurosurgery (AREA)
  • Dispersion Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Biotechnology (AREA)
  • Medical Informatics (AREA)
  • Condensed Matter Physics & Semiconductors (AREA)
  • General Physics & Mathematics (AREA)
  • Manufacturing & Machinery (AREA)
  • General Engineering & Computer Science (AREA)

Abstract

La présente invention a trait à une composition pharmaceutique contenant en tant que principe actif, l'itraconazole. Plus particulièrement, la présente invention a trait à une composition pharmaceutique comportant de l'itraconazole, un dérivé de l'acide polylactique, et un copolymère bloc amphiphile. Le dérivé de l'acide polylactique peut être combiné avec un ion métallique au niveau du terminal d'acide carboxylique, et le copolymère bloc forme des micelles et des nanoparticules dans un milieu aqueux.
PCT/KR2004/003422 2003-12-23 2004-12-23 Formulations pharmaceutiques pour l'itraconazole Ceased WO2005060361A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR10-2003-0095349 2003-12-23
KR1020030095349A KR20050064075A (ko) 2003-12-23 2003-12-23 이트라코나졸을 유효성분으로 하는 약학적 조성물

Publications (2)

Publication Number Publication Date
WO2005060361A2 true WO2005060361A2 (fr) 2005-07-07
WO2005060361A3 WO2005060361A3 (fr) 2005-09-15

Family

ID=34709248

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2004/003422 Ceased WO2005060361A2 (fr) 2003-12-23 2004-12-23 Formulations pharmaceutiques pour l'itraconazole

Country Status (2)

Country Link
KR (2) KR20050064075A (fr)
WO (1) WO2005060361A2 (fr)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007048423A1 (fr) * 2005-10-26 2007-05-03 Stichting Dutch Polymer Institute Micelles unimoleculaires contenant des nanoparticules metalliques et leur utilisation en tant que catalyseurs pour la synthese de liaisons carbone-carbone
WO2007073112A1 (fr) * 2005-12-23 2007-06-28 Samyang Corporation Composition comportant un medicament antifongique a base d'azole et son procede de preparation
CN101444510B (zh) * 2008-12-31 2011-03-09 南京卡文迪许生物工程技术有限公司 含有伏立康唑的药物制剂及其制备方法
EP2522338A4 (fr) * 2009-12-30 2013-09-18 Samyang Biopharmaceuticals Composition de formulation pour injection de nanoparticules polymères, contenant de la rapamycine et présentant une solubilité dans l'eau améliorée, son procédé de préparation, et composition anticancéreuse pour utilisation en combinaison avec une radiothérapie
EP3127943A4 (fr) * 2014-03-31 2017-09-27 Shimadzu Corporation Procédé de production de nanoparticules

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102184768B1 (ko) * 2018-12-31 2020-11-30 중앙대학교 산학협력단 혼합 고분자 미셀 조성물 및 이의 용도
CN111888523A (zh) * 2020-09-08 2020-11-06 尹振宇 一种用于改善肌肤的聚乳酸凝胶的制备方法

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4244466C2 (de) * 1992-12-24 1995-02-23 Pharmatech Gmbh Verfahren zur Herstellung von Pseudolatices und Mikro- oder Nanopartikeln und deren Verwendung zur Herstellung von pharmazeutischen Präparaten
US6365173B1 (en) * 1999-01-14 2002-04-02 Efrat Biopolymers Ltd. Stereocomplex polymeric carriers for drug delivery
JP2002138036A (ja) * 2000-08-24 2002-05-14 Santen Pharmaceut Co Ltd 薬物放出制御システム
KR100446101B1 (ko) * 2000-12-07 2004-08-30 주식회사 삼양사 수난용성 약물의 서방성 제형 조성물
CA2463517C (fr) * 2001-10-18 2010-03-16 Samyang Corporation Derives d'acide polylactique biodegradables sensibles au ph formant des micelles polymeres et utilisations de ceux-ci pour l'administration de medicaments faiblement hydrosolubles
ATE370988T1 (de) * 2001-10-18 2007-09-15 Samyang Corp Polymermicellenzusammensetzung mit verbesserter stabilität

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007048423A1 (fr) * 2005-10-26 2007-05-03 Stichting Dutch Polymer Institute Micelles unimoleculaires contenant des nanoparticules metalliques et leur utilisation en tant que catalyseurs pour la synthese de liaisons carbone-carbone
WO2007073112A1 (fr) * 2005-12-23 2007-06-28 Samyang Corporation Composition comportant un medicament antifongique a base d'azole et son procede de preparation
CN101444510B (zh) * 2008-12-31 2011-03-09 南京卡文迪许生物工程技术有限公司 含有伏立康唑的药物制剂及其制备方法
EP2522338A4 (fr) * 2009-12-30 2013-09-18 Samyang Biopharmaceuticals Composition de formulation pour injection de nanoparticules polymères, contenant de la rapamycine et présentant une solubilité dans l'eau améliorée, son procédé de préparation, et composition anticancéreuse pour utilisation en combinaison avec une radiothérapie
US9173841B2 (en) 2009-12-30 2015-11-03 Samyang Biopharmaceuticals Corporation Polymer nanoparticle injection formulation composition containing rapamycin with improved water solubility, preparation method thereof, and anticancer composition for combined use with radiotherapy
EP3127943A4 (fr) * 2014-03-31 2017-09-27 Shimadzu Corporation Procédé de production de nanoparticules

Also Published As

Publication number Publication date
WO2005060361A3 (fr) 2005-09-15
KR100834148B1 (ko) 2008-06-02
KR20050064075A (ko) 2005-06-29
KR20060129289A (ko) 2006-12-15

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