CO5580740A2 - SOLID FORMULATION TO USE AS A MEDICATION BASED ON A PIPERAZINUREA DERIVATIVE - Google Patents

SOLID FORMULATION TO USE AS A MEDICATION BASED ON A PIPERAZINUREA DERIVATIVE

Info

Publication number
CO5580740A2
CO5580740A2 CO04044345A CO04044345A CO5580740A2 CO 5580740 A2 CO5580740 A2 CO 5580740A2 CO 04044345 A CO04044345 A CO 04044345A CO 04044345 A CO04044345 A CO 04044345A CO 5580740 A2 CO5580740 A2 CO 5580740A2
Authority
CO
Colombia
Prior art keywords
acid
solid formulation
glyceryl
stearate
polymer matrix
Prior art date
Application number
CO04044345A
Other languages
Spanish (es)
Inventor
Heiko Kranz
Christoph Volkel
Ralph Lipp
Johannes Tack
Herbert Wiesinger
Original Assignee
Bayer Schering Pharma Ag
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 Bayer Schering Pharma Ag filed Critical Bayer Schering Pharma Ag
Publication of CO5580740A2 publication Critical patent/CO5580740A2/en

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
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1635—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Pulmonology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

1.- Formulación sólida para utilizar como medicamento que contiene (2R)-1-((4-cloro-2-(ureido)fenoxi)metil) carbonil -2-metil-4-(4-fluoro-bencil)-piperazina o una de sus sales caracterizada porque contiene adicionalmente una matriz polimérica, un ácido orgánico, un lubricante y uno o varios excipientes y porque el 90% de los tamaños de partículas de las mezclas en polvo se ubican en el rango de 0,1 a 750 µm.2.- Formulación sólida para utilizar como medicamento de acuerdo a la reivindicación 1, en la que la matriz polimérica se seleccionó del grupo compuesto por derivados de celulosa, derivados acrílicos, polímeros vinílicos, polianhídridos, poliéster poliortoéster, poliuretanos, policarbonatos, polifosfacenos, poliacetales, polisacáridos, éster de azúcar, dietilenglicol-monoetiléter, dietilenglicol-monopalmito-estearato, etilenglicol-monopalmitoestearato, behenatos de glicerilo y dibehenatos de glicerilo, diestearatos de glicerilo y palmitoestearatos de glicerilo, monooleato de glicerilo 40, monoestearato de glicerilo 40-55, laurato de macrogolglicerilo, estearato de macrogolglicerilo, monopalmito-estearato de propilenglicol, quitosán, galactomanano, pectina, goma laca y alginatos.3.- Formulación sólida para utilizar como medicamento de acuerdo a la reivindicación 1 ó 2, en la que la matriz polimérica está compuesta por una mezcla de polivinilpirrolidona soluble en agua y polivinilacetato insoluble en agua.4.- Formulación sólida para utilizar como medicamento de acuerdo a una de las reivindicaciones 1-3, en la que la matriz polimérica presenta la siguiente composición: 80% de acetato de polivinilo, 19% polivinilpirrolidona, 0,8% de laurilsulfato sódico y 0,2% de dióxido de silicio.5.- Formulación sólida para utilizar como medicamento de acuerdo a una de las reivindicaciones 1-4, en la que se seleccionó el ácido orgánico del grupo compuesto por ácido fumárico, ácido cítrico, citrato trisódico, hidrocitrato sódico, ácido ascórbico, ácido maleico, anhídrido maleico, ácido tartárico, ácido adípico, hidrofosfato sódico, ácido succínico, ácido glutárico, anhídrido glutárico, sorbato de potasio y ácido sórbico.1.- Solid formulation for use as a medicine containing (2R) -1 - ((4-chloro-2- (ureido) phenoxy) methyl) carbonyl -2-methyl-4- (4-fluoro-benzyl) -piperazine or one of its salts characterized in that it additionally contains a polymer matrix, an organic acid, a lubricant and one or several excipients and because 90% of the particle sizes of the powder mixtures are in the range of 0.1 to 750 µm .2.- Solid formulation for use as a medicament according to claim 1, wherein the polymer matrix was selected from the group consisting of cellulose derivatives, acrylic derivatives, vinyl polymers, polyanhydrides, polyester polyether ester, polyurethanes, polycarbonates, polyphosphazenes, polyacetals, polysaccharides, sugar ester, diethylene glycol monoethyl ether, diethylene glycol monopalmite stearate, ethylene glycol monopalmito stearate, glyceryl behenates and glyceryl dibehenates, glyceryl distearates and glyceryl palmostearates , glyceryl monooleate 40, glyceryl monostearate 40-55, macrogolglyceryl laurate, macrogolglyceryl stearate, propylene glycol monopalmite-stearate, chitosan, galactomannan, pectin, shellac and alginates. 3.- Solid formulation to be used as medicine according to claim 1 or 2, wherein the polymer matrix is composed of a mixture of water soluble polyvinylpyrrolidone and water insoluble polyvinyl acetate. 4. Solid formulation for use as a medicament according to one of claims 1-3, in the The polymer matrix has the following composition: 80% polyvinyl acetate, 19% polyvinyl pyrrolidone, 0.8% sodium lauryl sulfate and 0.2% silicon dioxide. 5.- Solid formulation to be used as a medicine according to a of claims 1-4, wherein the organic acid was selected from the group consisting of fumaric acid, citric acid, trisodium citrate, sodium hydrocytrate, acid ascorbic, maleic acid, maleic anhydride, tartaric acid, adipic acid, sodium hydrophosphate, succinic acid, glutaric acid, glutaric anhydride, potassium sorbate and sorbic acid.

CO04044345A 2001-10-18 2004-05-13 SOLID FORMULATION TO USE AS A MEDICATION BASED ON A PIPERAZINUREA DERIVATIVE CO5580740A2 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE10152351A DE10152351B4 (en) 2001-10-18 2001-10-18 Solid drug formulation for a piperazine urea derivative

Publications (1)

Publication Number Publication Date
CO5580740A2 true CO5580740A2 (en) 2005-11-30

Family

ID=7703496

Family Applications (1)

Application Number Title Priority Date Filing Date
CO04044345A CO5580740A2 (en) 2001-10-18 2004-05-13 SOLID FORMULATION TO USE AS A MEDICATION BASED ON A PIPERAZINUREA DERIVATIVE

Country Status (23)

Country Link
EP (1) EP1435917A1 (en)
JP (1) JP2005506365A (en)
KR (1) KR20040047920A (en)
CN (1) CN1571660A (en)
AR (1) AR037111A1 (en)
AU (1) AU2002333896B2 (en)
BR (1) BR0213340A (en)
CA (1) CA2463951A1 (en)
CO (1) CO5580740A2 (en)
DE (1) DE10152351B4 (en)
EC (1) ECSP045108A (en)
HR (1) HRP20040435A2 (en)
IL (1) IL161166A0 (en)
MX (1) MXPA04003522A (en)
NO (1) NO20042022L (en)
NZ (1) NZ532287A (en)
PE (1) PE20030472A1 (en)
PL (1) PL367987A1 (en)
RS (1) RS32204A (en)
RU (1) RU2311172C2 (en)
UY (1) UY27500A1 (en)
WO (1) WO2003035037A1 (en)
ZA (1) ZA200403781B (en)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1723196A (en) 2001-06-27 2006-01-18 史密丝克莱恩比彻姆公司 Fluoropyrrolidines as dipeptidyl peptidase inhibitors
EP1749519A1 (en) * 2005-08-05 2007-02-07 Schering Aktiengesellschaft Dosage form with pH-independent sustained release for active substances with pH-dependent solubility
NZ703464A (en) * 2006-04-26 2016-05-27 Alphapharm Pty Ltd Controlled release formulations comprising uncoated discrete unit(s) and an extended release matrix
DE102008047910A1 (en) 2008-09-19 2010-03-25 Molkerei Meggle Wasserburg Gmbh & Co. Kg Tabletting excipient based on lactose and cellulose
KR101654582B1 (en) 2016-05-12 2016-09-06 그린로드(주) Conical Shaped Buoyant Polymer Filter and Apparatus for Manufacturing the same and Method for Manufacturing the same and Water Treatment Filter including the same
RU2729223C1 (en) * 2020-05-13 2020-08-05 Мераб Георгиевич Чикобава Dosage form for amplification of nucleic acids

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6207665B1 (en) * 1997-06-12 2001-03-27 Schering Aktiengesellschaft Piperazine derivatives and their use as anti-inflammatory agents
SK11262000A3 (en) * 1998-02-05 2001-01-18 Pfizer Products Inc. Novel dihydroxyhexanoic acid derivatives and pharmaceutical compositon containing the same
EP1027885B1 (en) * 1999-02-09 2008-07-09 Pfizer Products Inc. Basic drug compositions with enhanced bioavailability

Also Published As

Publication number Publication date
RS32204A (en) 2006-10-27
AR037111A1 (en) 2004-10-20
PL367987A1 (en) 2005-03-21
RU2311172C2 (en) 2007-11-27
AU2002333896A2 (en) 2003-05-06
EP1435917A1 (en) 2004-07-14
MXPA04003522A (en) 2004-07-23
HRP20040435A2 (en) 2005-06-30
BR0213340A (en) 2004-10-05
DE10152351B4 (en) 2005-09-22
CA2463951A1 (en) 2003-05-01
NZ532287A (en) 2007-04-27
DE10152351A1 (en) 2003-05-08
KR20040047920A (en) 2004-06-05
AU2002333896B2 (en) 2007-07-26
ECSP045108A (en) 2004-06-28
UY27500A1 (en) 2003-06-30
JP2005506365A (en) 2005-03-03
WO2003035037A1 (en) 2003-05-01
RU2004115328A (en) 2005-06-10
ZA200403781B (en) 2004-11-29
IL161166A0 (en) 2004-08-31
CN1571660A (en) 2005-01-26
NO20042022L (en) 2004-05-14
PE20030472A1 (en) 2003-06-16

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