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

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Classifications

    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B82—NANOTECHNOLOGY
    • B82Y—SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
    • B82Y5/00—Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
    • 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
    • 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
    • A61K31/12—Ketones
    • A61K31/122—Ketones having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic 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
    • A61K31/352—Heterocyclic 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 
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365—Lactones
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/415—1,2-Diazoles
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/42—Oxazoles
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • 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
    • A61K9/4816—Wall or shell material
    • 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
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • 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
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs 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 (17)

* 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
FR2838349B1 (en) * 2002-04-15 2004-06-25 Laurence Paris LIQUID COMPOSITIONS FOR SUSTAINED RELEASE SOFT CAPSULES AND PROCESS FOR PRODUCING THE SAME
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
CA2538078C (en) * 2003-09-25 2012-12-04 Activbiotics, Inc. Rifalazil formulations
EP2308467A3 (en) * 2005-06-17 2011-06-22 Hospira Australia Pty Ltd Liquid pharmaceutical formulations of docetaxel
KR101170283B1 (en) 2006-10-27 2012-07-31 화이자 프로덕츠 인코포레이티드 Hydroxypropyl methyl cellulose hard capsules and process of manufacture
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
AU2011327824B2 (en) * 2010-11-08 2016-06-02 Cadila Pharmaceuticals Limited 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
WO2023220109A1 (en) * 2022-05-11 2023-11-16 Eli Lilly And Company Glp1 pharmaceutical compositions

Family Cites Families (10)

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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
WO1998013359A1 (en) * 1996-09-24 1998-04-02 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
HUP0003546A3 (en) * 1997-05-27 2002-12-28 Baker Norton Pharma Compositions for administering taxanes orally to human patients
ATE219363T1 (en) * 1997-06-20 2002-07-15 Baker Norton Pharma SOLUBLE PRODRUGS OF PACLITAXEL
IL131217A0 (en) * 1998-03-10 2001-01-28 Napro Biotherapeutics Inc Novel methods and compositions for delivery of taxanes
KR100602725B1 (en) * 1998-12-11 2006-07-20 파마솔루션스, 인코포레이티드 Self-emulsifying compositions for drugs poorly soluble in water
JP4722295B2 (en) * 1999-05-27 2011-07-13 エイカスフィアー・インコーポレーテッド Porous drug matrix and method for producing the same
US6136846A (en) * 1999-10-25 2000-10-24 Supergen, Inc. Formulation for paclitaxel
WO2002043765A2 (en) * 2000-11-28 2002-06-06 Transform Pharmaceuticals, Inc. Pharmaceutical formulations comprising paclitaxel, derivatives, and pharmaceutically acceptable salts thereof

Also Published As

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

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