PE20030472A1 - SOLID FORMULATION TO USE AS A DRUG BASED ON A PIPERAZINUREA DERIVATIVE - Google Patents

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

Info

Publication number
PE20030472A1
PE20030472A1 PE2002001027A PE2002001027A PE20030472A1 PE 20030472 A1 PE20030472 A1 PE 20030472A1 PE 2002001027 A PE2002001027 A PE 2002001027A PE 2002001027 A PE2002001027 A PE 2002001027A PE 20030472 A1 PE20030472 A1 PE 20030472A1
Authority
PE
Peru
Prior art keywords
polyuble
cellulose
methyl
refers
solid formulation
Prior art date
Application number
PE2002001027A
Other languages
Spanish (es)
Inventor
Ralph Lipp
Heiko Kranz
Christoph Volkel
Herbert Wiesinger
Johannes Tack
Original Assignee
Schering 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 Schering Ag filed Critical Schering Ag
Publication of PE20030472A1 publication Critical patent/PE20030472A1/en

Links

Classifications

    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1652Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/2027Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1635Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose

Landscapes

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

Abstract

SE REFIERE A UNA FORMULACION SOLIDA QUE CONTIENE a)(2R)-1-((4-CLORO-2-(UREIDO)FENOXI)METIL)CARBONIL-2-METIL-4-(4-FLUORO-BENCIL)-PIPERAZINA (ANTAGONISTA DEL RECEPTOR CCR-1), b)MATRIZ POLIMERICA, SE SELECCIONA DE DERIVADOS DE CELULOSA, ACRILICOS, POLIMEROS VINILICOS, POLIANHIDROS, POLIESTER POLIORTOESTER, POLIURETANOS, POLICARBONATOS, ENTRE OTROS O UNA MEZCLA DE POLIVINIL-PIRROLIDONA SOLUBLE EN AGUA Y POLIVINILACETATO INSOLUBLE EN AGUA, c)ACIDO ORGANICO COMO FUMARICO, CITRICO, ASCORBICO, MALEICO, TARTARICO, SUCCINICO, GLUTARICO, SORBICO, ENTRE OTROS, d)LUBRICANTE, e)EXCIPIENTE TAL COMO LACTOSA, DIFOSFATO DE CALCIO, ALMIDON, CELULOSA CRISTALINA; CARACTERIZADA PORQUE EL 90% DEL TAMANO DE PARTICULAS DE LAS MEZCLAS EN POLVO SE UBICAN EN EL RANGO DE 0,1 A 750µm. TAMBIEN SE REFIERE A PROCEDIMIENTOS PARA LA PREPARACION. LA FORMULACION DE LA COMPOSICION AUMENTA LA SOLUBILIDAD Y LIBERACION DEL COMPUESTO INDEPENDIENTEMENTE DEL pH Y PUEDE SER UTIL PARA EL TRATAMIENTO DE ENFERMEDADES INFLAMATORIAS, ESCLEROSIS MULTIPLE, ARTRITIS REUMATOIDE, PSORIASIS, DERMATITIS ATOPICAREFERS TO A SOLID FORMULATION CONTAINING a) (2R) -1 - ((4-CHLORINE-2- (UREIDE) PHENOXY) METHYL) CARBONYL-2-METHYL-4- (4-FLUORO-BENZYL) -PIPERAZINE (ANTAGONIST OF THE RECEIVER CCR-1), b) POLYMERIC MATRIX, SELECTED FROM DERIVATIVES OF CELLULOSE, ACRYLICS, VINYL POLYMERS, POLYANHYDRES, POLYORTOESTER POLYESTER, POLYURETHANES, POLYCARBONATES, BETWEEN OTHER WATER-INSIVINY-WATER-POLYUBLE-POLYUBLE-POLYLUBLE MIXTURE , c) ORGANIC ACID SUCH AS FUMARIC, CITRIC, ASCORBIC, MALEIC, TARTARIC, SUCCINIC, GLUTARIC, SORBIC, AMONG OTHERS, d) LUBRICANT, e) EXCIPIENT SUCH AS LACTOSE, CALCIUM DIPHOSPHATE, STARCH, CELLULOSE; CHARACTERIZED BECAUSE 90% OF THE PARTICLE SIZE OF POWDER MIXTURES ARE LOCATED IN THE RANGE OF 0.1 TO 750µm. IT ALSO REFERS TO PROCEDURES FOR PREPARATION. THE FORMULATION OF THE COMPOSITION INCREASES THE SOLUBILITY AND RELEASE OF THE COMPOUND INDEPENDENTLY OF THE pH AND MAY BE USEFUL FOR THE TREATMENT OF INFLAMMATORY DISEASES, MULTIPLE SCLEROSIS, RHEUMATOID ARTHRITIS, PSORIASIS, ATOPIC DERMATITIS

PE2002001027A 2001-10-18 2002-10-17 SOLID FORMULATION TO USE AS A DRUG BASED ON A PIPERAZINUREA DERIVATIVE PE20030472A1 (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
PE20030472A1 true PE20030472A1 (en) 2003-06-16

Family

ID=7703496

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2002001027A PE20030472A1 (en) 2001-10-18 2002-10-17 SOLID FORMULATION TO USE AS A DRUG 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
DE60222667T2 (en) 2001-06-27 2008-07-17 Smithkline Beecham Corp. FLUORPYRROLIDINES AS DIPEPTIDYLPEPTIDASE 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
US20090169617A1 (en) * 2006-04-26 2009-07-02 Panagiotis Keramidas 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
ATE337307T1 (en) * 1998-02-05 2006-09-15 Pfizer Prod Inc NEW DIHYDROXYHEXANIC ACID DERIVATIVES
ATE400251T1 (en) * 1999-02-09 2008-07-15 Pfizer Prod Inc COMPOSITIONS OF BASIC DRUGS WITH IMPROVED BIOAVAILABILITY

Also Published As

Publication number Publication date
AU2002333896A2 (en) 2003-05-06
DE10152351A1 (en) 2003-05-08
IL161166A0 (en) 2004-08-31
RU2004115328A (en) 2005-06-10
UY27500A1 (en) 2003-06-30
RS32204A (en) 2006-10-27
AU2002333896B2 (en) 2007-07-26
EP1435917A1 (en) 2004-07-14
KR20040047920A (en) 2004-06-05
HRP20040435A2 (en) 2005-06-30
PL367987A1 (en) 2005-03-21
NZ532287A (en) 2007-04-27
DE10152351B4 (en) 2005-09-22
MXPA04003522A (en) 2004-07-23
ECSP045108A (en) 2004-06-28
CO5580740A2 (en) 2005-11-30
CA2463951A1 (en) 2003-05-01
JP2005506365A (en) 2005-03-03
NO20042022L (en) 2004-05-14
WO2003035037A1 (en) 2003-05-01
BR0213340A (en) 2004-10-05
ZA200403781B (en) 2004-11-29
AR037111A1 (en) 2004-10-20
RU2311172C2 (en) 2007-11-27
CN1571660A (en) 2005-01-26

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