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 DERIVATIVEInfo
- 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
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
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.
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)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ATE374181T1 (en) | 2001-06-27 | 2007-10-15 | 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 |
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)
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 |
EA003137B1 (en) * | 1998-02-05 | 2003-02-27 | Пфайзер Продактс Инк | Novel dihydroxyhexanoic acid derivatives |
EP1027885B1 (en) * | 1999-02-09 | 2008-07-09 | Pfizer Products Inc. | Basic drug compositions with enhanced bioavailability |
-
2001
- 2001-10-18 DE DE10152351A patent/DE10152351B4/en not_active Expired - Fee Related
-
2002
- 2002-10-07 WO PCT/EP2002/011229 patent/WO2003035037A1/en not_active Application Discontinuation
- 2002-10-07 RS YU32204A patent/RS32204A/en unknown
- 2002-10-07 EP EP02801884A patent/EP1435917A1/en not_active Withdrawn
- 2002-10-07 BR BR0213340-7A patent/BR0213340A/en not_active IP Right Cessation
- 2002-10-07 AU AU2002333896A patent/AU2002333896B2/en not_active Ceased
- 2002-10-07 RU RU2004115328/15A patent/RU2311172C2/en not_active IP Right Cessation
- 2002-10-07 PL PL02367987A patent/PL367987A1/en not_active Application Discontinuation
- 2002-10-07 MX MXPA04003522A patent/MXPA04003522A/en unknown
- 2002-10-07 CN CNA02820512XA patent/CN1571660A/en active Pending
- 2002-10-07 CA CA002463951A patent/CA2463951A1/en not_active Abandoned
- 2002-10-07 KR KR10-2004-7005591A patent/KR20040047920A/en not_active Application Discontinuation
- 2002-10-07 JP JP2003537604A patent/JP2005506365A/en active Pending
- 2002-10-07 IL IL16116602A patent/IL161166A0/en unknown
- 2002-10-07 NZ NZ532287A patent/NZ532287A/en unknown
- 2002-10-17 PE PE2002001027A patent/PE20030472A1/en not_active Application Discontinuation
- 2002-10-17 UY UY27500A patent/UY27500A1/en not_active Application Discontinuation
- 2002-10-18 AR ARP020103929A patent/AR037111A1/en unknown
-
2004
- 2004-05-13 CO CO04044345A patent/CO5580740A2/en not_active Application Discontinuation
- 2004-05-14 NO NO20042022A patent/NO20042022L/en not_active Application Discontinuation
- 2004-05-17 HR HR20040435A patent/HRP20040435A2/en not_active Application Discontinuation
- 2004-05-17 EC EC2004005108A patent/ECSP045108A/en unknown
- 2004-05-17 ZA ZA200403781A patent/ZA200403781B/en unknown
Also Published As
Publication number | Publication date |
---|---|
UY27500A1 (en) | 2003-06-30 |
AR037111A1 (en) | 2004-10-20 |
WO2003035037A1 (en) | 2003-05-01 |
MXPA04003522A (en) | 2004-07-23 |
DE10152351A1 (en) | 2003-05-08 |
RS32204A (en) | 2006-10-27 |
CN1571660A (en) | 2005-01-26 |
AU2002333896B2 (en) | 2007-07-26 |
EP1435917A1 (en) | 2004-07-14 |
JP2005506365A (en) | 2005-03-03 |
AU2002333896A2 (en) | 2003-05-06 |
RU2311172C2 (en) | 2007-11-27 |
RU2004115328A (en) | 2005-06-10 |
ECSP045108A (en) | 2004-06-28 |
CA2463951A1 (en) | 2003-05-01 |
NO20042022L (en) | 2004-05-14 |
PE20030472A1 (en) | 2003-06-16 |
NZ532287A (en) | 2007-04-27 |
DE10152351B4 (en) | 2005-09-22 |
HRP20040435A2 (en) | 2005-06-30 |
ZA200403781B (en) | 2004-11-29 |
IL161166A0 (en) | 2004-08-31 |
KR20040047920A (en) | 2004-06-05 |
PL367987A1 (en) | 2005-03-21 |
BR0213340A (en) | 2004-10-05 |
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Legal Events
Date | Code | Title | Description |
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FC | Application refused |