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PE20020833A1 - CHEMOTHERAPIC COMPOSITIONS OF PACLITAXEL IN MICROEMULSION WITH GREATER ORAL BIOAVAILABILITY - Google Patents

CHEMOTHERAPIC COMPOSITIONS OF PACLITAXEL IN MICROEMULSION WITH GREATER ORAL BIOAVAILABILITY

Info

Publication number
PE20020833A1
PE20020833A1 PE2002000030A PE2002000030A PE20020833A1 PE 20020833 A1 PE20020833 A1 PE 20020833A1 PE 2002000030 A PE2002000030 A PE 2002000030A PE 2002000030 A PE2002000030 A PE 2002000030A PE 20020833 A1 PE20020833 A1 PE 20020833A1
Authority
PE
Peru
Prior art keywords
paclitaxel
composition
microemulsion
polyoxyl
diglyceride
Prior art date
Application number
PE2002000030A
Other languages
Spanish (es)
Inventor
Walter Morozowich
Ping Gao
Original Assignee
Upjohn Co
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 Upjohn Co filed Critical Upjohn Co
Publication of PE20020833A1 publication Critical patent/PE20020833A1/en

Links

Classifications

    • BPERFORMING OPERATIONS; TRANSPORTING
    • B82NANOTECHNOLOGY
    • B82YSPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
    • B82Y5/00Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/12Ketones
    • A61K31/122Ketones having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365Lactones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/4151,2-Diazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/42Oxazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4816Wall or shell material
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4858Organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4866Organic macromolecular compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nanotechnology (AREA)
  • General Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Medical Informatics (AREA)
  • Molecular Biology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Biophysics (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

SE REFIERE A UNA COMPOSICION FARMACEUTICA QUE COMPRENDE: a) PACLITAXEL; b) UN SURFACTANTE SELECCIONADO DE ACEITE DE RICINO HIDROGENADO POLIOXIL 40, ACEITE DE RICINO HIDROGENADO POLIOXIL 35, ESTERES DE ACIDOS GRASOS POLIOXIETILENADOS SEL SORBITAN, ENTRE OTROS ; c) UN SOLVENTE SELECCIONADO DE POLIETILENGLICOL, PROPILENGLICOL, ETANOL, GLICEROL, ENTRE OTROS Y d) UN POLIMERO CELULOSICO SUSTITUIDO. LA PROPORCION EN PESO DE PACLITAXEL AL SURFACTANTE OSCILA ENTRE 1:5 Y 1:10. LA COMPOSICION CONTIENE ADEMAS UN INHIBIDOR DE LA GLICOPROTEINA P COMO ALGINATO, XANTANO, VERAPAMILO, CICLOSPORINA A Y ADICIONALMENTE UN DIGLICERIDO O UNA MEZCLA DE DIGLICERIDO Y MONOGLICERIDO. LA COMPOSICION GENERA UNA MICROEMULSION SOBRESATURADA DE PACLITAXEL AL ENTRAR EN CONTACTO CON AGUA AUMENTANDO DE ESTA FORMA LA BIODISPONIBILIDAD ORAL DEL FARMACO. LA COMPOSICION ES UTIL PARA EL TRATAMIENTO DEL CANCERIT REFERS TO A PHARMACEUTICAL COMPOSITION INCLUDING: a) PACLITAXEL; b) A SURFACTANT SELECTED FROM POLYOXYL 40 HYDROGENATED RICHINO OIL, POLYOXYL 35 HYDROGENATED RICHINE OIL, SORBITAN SEL-SORBITAN POLYOXYETHYLENED FATTY ACID ESTERS, AMONG OTHERS; c) A SOLVENT SELECTED FROM POLYETHYLENE GLYCOL, PROPYLENE GLYCOL, ETHANOL, GLYCEROL, AMONG OTHERS AND d) A SUBSTITUTE CELLULOSIC POLYMER. THE RATIO BY WEIGHT OF PACLITAXEL TO THE SURFACTANT RANGES BETWEEN 1: 5 AND 1:10. THE COMPOSITION ALSO CONTAINS A GLYCOPROTEIN P INHIBITOR SUCH AS ALGINATE, XANTHANE, VERAPAMYL, CYCLOSPORIN A AND ADDITIONALLY A DIGLYCERIDE OR A MIXTURE OF DIGLYCERIDE AND MONOGLYCERIDE. THE COMPOSITION GENERATES AN OVERRESATURATED MICROEMULSION OF PACLITAXEL WHEN IT COMES IN CONTACT WITH WATER, IN THIS WAY INCREASING THE ORAL BIODAVAILABILITY OF THE DRUG. THE COMPOSITION IS USEFUL FOR THE TREATMENT OF CANCER

PE2002000030A 2001-01-18 2002-01-17 CHEMOTHERAPIC COMPOSITIONS OF PACLITAXEL IN MICROEMULSION WITH GREATER ORAL BIOAVAILABILITY PE20020833A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US26255501P 2001-01-18 2001-01-18

Publications (1)

Publication Number Publication Date
PE20020833A1 true PE20020833A1 (en) 2002-09-19

Family

ID=22998000

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2002000030A PE20020833A1 (en) 2001-01-18 2002-01-17 CHEMOTHERAPIC COMPOSITIONS OF PACLITAXEL IN MICROEMULSION WITH GREATER ORAL BIOAVAILABILITY

Country Status (9)

Country Link
EP (1) EP1365759A2 (en)
JP (1) JP2004520398A (en)
AR (1) AR032642A1 (en)
CA (1) CA2434641A1 (en)
MX (1) MXPA03006404A (en)
NZ (1) NZ539046A (en)
PE (1) PE20020833A1 (en)
WO (1) WO2002064132A2 (en)
ZA (1) ZA200305086B (en)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6750246B1 (en) 2000-02-03 2004-06-15 Bristol-Myers Squibb Company C-4 carbonate taxanes
KR100533458B1 (en) 2002-07-20 2005-12-07 대화제약 주식회사 Composition for solubilization of paclitaxel and preparation method thereof
EP1498143A1 (en) * 2003-07-18 2005-01-19 Aventis Pharma S.A. Self-emulsifying and self-microemulsifying formulations for the oral administration of taxoids
EP1498120A1 (en) * 2003-07-18 2005-01-19 Aventis Pharma S.A. Semi-solid formulations for the oral administration of taxoids
US20050123602A1 (en) * 2003-09-25 2005-06-09 Michaelis Arthur F. Rifalazil formulations
KR20080030024A (en) * 2005-06-17 2008-04-03 호스피라 오스트레일리아 피티와이 리미티드 Pharmaceutical Liquid Formulations of Docetaxel
ES2744816T3 (en) * 2006-10-27 2020-02-26 Capsugel Belgium Nv Hydroxypropyl methyl cellulose hard capsules and manufacturing process
US20090088393A1 (en) * 2007-09-28 2009-04-02 Zomanex, Llc Methods and formulations for converting intravenous and injectable drugs into oral dosage forms
KR101053780B1 (en) * 2008-02-29 2011-08-02 동아제약주식회사 Single liquid stable pharmaceutical composition containing docetaxel
RU2603833C2 (en) * 2010-11-08 2016-11-27 Кадила Фармасьютикалз Лимитед Pharmaceutical composition of taxoids
CN103110581B (en) * 2013-02-26 2015-07-22 西南大学 Taxol microemulsion drug composition and preparation method thereof
KR101542364B1 (en) * 2014-10-31 2015-08-07 대화제약 주식회사 Pharmaceutical composition for oral administration comprising taxanes
ES2895948T3 (en) 2015-07-30 2022-02-23 Dae Hwa Pharma Co Ltd Pharmaceutical composition for oral administration comprising taxane at high concentration
CN107028931A (en) * 2016-02-04 2017-08-11 上海宣泰医药科技有限公司 A kind of taxol drug composition and its pharmaceutical preparation, preparation method and purposes
EP3701943A1 (en) * 2019-02-26 2020-09-02 CAPNOMED GmbH Delayed delivery of anticancer drugs
IL316629A (en) * 2022-05-11 2024-12-01 Lilly Co Eli Glp1 pharmaceutical compositions

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6964946B1 (en) * 1995-10-26 2005-11-15 Baker Norton Pharmaceuticals, Inc. Oral pharmaceutical compositions containing taxanes and methods of treatment employing the same
EP0868422A1 (en) * 1996-09-24 1998-10-07 Marigen S.A. Ultramicroemulsion of spontaneously dispersible concentrates of esters of baccatin-iii compounds with antitumor and antiviral effect
CH688504A5 (en) * 1997-03-26 1997-10-31 Marigen Sa Spontaneously dispersible concentrate containing a taxol analogue
ATE308365T1 (en) * 1997-05-27 2005-11-15 Ivax Research Inc COMPOSITIONS FOR ORAL ADMINISTRATION OF TAXANS AND THEIR USE
AU3574097A (en) * 1997-06-20 1999-01-04 Baker Norton Pharmaceuticals, Inc. Soluble prodrugs of paclitaxel
IL131217A0 (en) * 1998-03-10 2001-01-28 Napro Biotherapeutics Inc Novel methods and compositions for delivery of taxanes
US6638522B1 (en) * 1998-12-11 2003-10-28 Pharmasolutions, Inc. Microemulsion concentrate composition of cyclosporin
ATE312601T1 (en) * 1999-05-27 2005-12-15 Acusphere Inc POROUS MEDICINAL MATRICES AND THEIR PRODUCTION PROCESS
US6136846A (en) * 1999-10-25 2000-10-24 Supergen, Inc. Formulation for paclitaxel
US6919370B2 (en) * 2000-11-28 2005-07-19 Transform Pharmaceuticals, Inc. Pharmaceutical formulations comprising paclitaxel, derivatives, and pharmaceutically acceptable salts thereof

Also Published As

Publication number Publication date
AR032642A1 (en) 2003-11-19
CA2434641A1 (en) 2002-08-22
WO2002064132A2 (en) 2002-08-22
ZA200305086B (en) 2004-06-30
NZ539046A (en) 2006-11-30
JP2004520398A (en) 2004-07-08
WO2002064132A3 (en) 2003-05-30
MXPA03006404A (en) 2004-12-02
EP1365759A2 (en) 2003-12-03

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