AR038369A1 - Metodo para preparar dispersiones solidas amorfas de farmacos secadas por pulverizacion utilizando inyectores a presion y producto - Google Patents
Metodo para preparar dispersiones solidas amorfas de farmacos secadas por pulverizacion utilizando inyectores a presion y productoInfo
- Publication number
- AR038369A1 AR038369A1 ARP030100268A ARP030100268A AR038369A1 AR 038369 A1 AR038369 A1 AR 038369A1 AR P030100268 A ARP030100268 A AR P030100268A AR P030100268 A ARP030100268 A AR P030100268A AR 038369 A1 AR038369 A1 AR 038369A1
- Authority
- AR
- Argentina
- Prior art keywords
- trifluoromethyl
- drug
- microns
- benzyl
- drops
- Prior art date
Links
- 239000003814 drug Substances 0.000 title abstract 7
- 229940079593 drug Drugs 0.000 title abstract 7
- 238000000034 method Methods 0.000 title abstract 4
- 239000007962 solid dispersion Substances 0.000 title abstract 3
- 238000005507 spraying Methods 0.000 title 1
- 238000001035 drying Methods 0.000 abstract 5
- 229920000642 polymer Polymers 0.000 abstract 4
- -1 3,5-bis-trifluoromethyl-benzyl Chemical group 0.000 abstract 3
- 230000002708 enhancing effect Effects 0.000 abstract 3
- 239000012527 feed solution Substances 0.000 abstract 3
- 239000011236 particulate material Substances 0.000 abstract 2
- 239000000243 solution Substances 0.000 abstract 2
- JRBOFAXVGHMLMM-APWZRJJASA-N (2r,4s)-4-[[3,5-bis(trifluoromethyl)phenyl]methyl-methoxycarbonylamino]-2-ethyl-6-(trifluoromethyl)-3,4-dihydro-2h-quinoline-1-carboxylic acid Chemical compound COC(=O)N([C@H]1C[C@H](N(C2=CC=C(C=C21)C(F)(F)F)C(O)=O)CC)CC1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1 JRBOFAXVGHMLMM-APWZRJJASA-N 0.000 abstract 1
- GZILZCCGDNKAAV-UHFFFAOYSA-N 5-chloro-1h-indole-2-carboxamide Chemical compound ClC1=CC=C2NC(C(=O)N)=CC2=C1 GZILZCCGDNKAAV-UHFFFAOYSA-N 0.000 abstract 1
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 238000000889 atomisation Methods 0.000 abstract 1
- 239000006185 dispersion Substances 0.000 abstract 1
- 238000010438 heat treatment Methods 0.000 abstract 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 239000002245 particle Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000007787 solid Substances 0.000 abstract 1
- 239000002904 solvent Substances 0.000 abstract 1
- 238000001694 spray drying Methods 0.000 abstract 1
Classifications
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
-
- 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
- A61K9/1682—Processes
- A61K9/1694—Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- 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)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Manufacturing Of Micro-Capsules (AREA)
- Vaporization, Distillation, Condensation, Sublimation, And Cold Traps (AREA)
- Glanulating (AREA)
- Medical Preparation Storing Or Oral Administration Devices (AREA)
- Disintegrating Or Milling (AREA)
Abstract
Dispersiones sólidas amorfas homogéneas de fármacos en polímeros mejoradores de la concentración se preparan en tamanos de partícula más grandes adecuados con mínimo contenido de fines, utilizando un atomizador y condiciones de procedimiento capaces de producir gotas que tienen un diámetro medio de al menos 50 micrones y un D10 de al menos 10 micrones. Reivindicación 1: Un procedimiento para producir una composición farmacéutica, caracterizado porque comprende las etapas de: (a) formar una disolución de alimentación que comprende un fármaco, un polímero mejorador de la concentración y un disolvente; (b) dirigir dicha disolución de alimentación hacia un aparato de secado por pulverización que comprende una cámara de secado, medios de atomización para atomizar en gotas dicha disolución de alimentación en dicha cámara de secado, una fuente de gas de secado calentando para secar dichas gotas y medios de recogida del producto secado; (c) atomizar en gotas dicha disolución de alimentación en dicha cámara de secado mediante dichos medios de atomización, teniendo dichas gotas un diámetro medio de al menos 50 micrones y un D10 de al menos 10 micrones; (d) poner en contacto dichas gotas con dicho gas de secado calentado para preparar materiales en partículas de una dispersión sólida amorfa de dicho fármaco y dicho polímero mejorador de la concentración; y (e) recoger dichos materiales en partículas: en el que dicho polímero mejorador de la concentración está presente en dicha disolución en una cantidad suficiente, de manera que dicha dispersión sólida amorfa proporciona una mejora de la concentración de dicho fármaco en un medio de utilización con respecto a una composición testigo que consiste esencialmente en una cantidad equivalente de dicho fármaco solo. Reivindicación 9: El procedimiento según la reivindicación 1, caracterizado porque dicho fármaco se elige del grupo que consta [R-(R*S*)]-5-cloro-N-2-hidroxi-3-{metoximetilamino}-3-oxo-1-(fenilmetil)propil-1H-indol-2-carboxamida, [(1S)-bencil-(2R)-hidroxi-3-((3R,4S)-dihidroxi-pirrolidin-1-il)-3-oxipropil]amida del ácido 5-cloro-1H-indol-2-carboxílico, éster isopropílico del ácido [2R,4S]-4-[acetil(3,5-bis-trifluorometil-bencil)-amino]-2-etil-6-trifluorometil-3,4-dihidro-2H-quinolin-1-carboxílico, éster etílico del ácido [2R,4S]-4-(3,5-bis-trifluorometil-bencil)-metoxicarbonil-amino]-2-etil-6-trifluorometil-3,4-dihidro-2H-quinolin-1-carboxílico y éster isopropílico del ácido [2R,4S]-4-[(3,5-bis-trifluorometil-bencil)-metoxicarbonil-amino]-2-etil-6-trifluorometil-3,4-dihidro-2H-quinolin-1-carboxílico.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US35398602P | 2002-02-01 | 2002-02-01 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR038369A1 true AR038369A1 (es) | 2005-01-12 |
Family
ID=27663274
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP030100268A AR038369A1 (es) | 2002-02-01 | 2003-01-30 | Metodo para preparar dispersiones solidas amorfas de farmacos secadas por pulverizacion utilizando inyectores a presion y producto |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US7780988B2 (es) |
| EP (1) | EP1469830A2 (es) |
| JP (1) | JP2005523260A (es) |
| KR (1) | KR100758045B1 (es) |
| CN (1) | CN1787808A (es) |
| AR (1) | AR038369A1 (es) |
| AU (1) | AU2003239463B2 (es) |
| BR (1) | BR0307515A (es) |
| CA (1) | CA2474958A1 (es) |
| GT (1) | GT200300024A (es) |
| MX (1) | MXPA04007435A (es) |
| PA (1) | PA8565401A1 (es) |
| PE (1) | PE20030804A1 (es) |
| PL (1) | PL371593A1 (es) |
| RS (1) | RS67304A (es) |
| RU (1) | RU2288703C2 (es) |
| TW (1) | TW200404576A (es) |
| UY (1) | UY27645A1 (es) |
| WO (1) | WO2003063821A2 (es) |
| ZA (1) | ZA200405971B (es) |
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| DE10026698A1 (de) | 2000-05-30 | 2001-12-06 | Basf Ag | Selbstemulgierende Wirkstoffformulierung und Verwendung dieser Formulierung |
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| DE602005019509D1 (de) | 2004-06-01 | 2010-04-08 | Teva Gyogyszergyar Zartkoeruen | Verfahren für die zubereitung der amorphen form eines medikamentes |
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| AR027656A1 (es) | 2000-03-16 | 2003-04-09 | Pfizer Prod Inc | Composiciones farmaceuticas de inhibidores de la glucogeno-fosforilasa |
| UY26615A1 (es) * | 2000-03-16 | 2001-10-25 | Pfizer Prod Inc | Inhibidor de la glucogeno fosforilasa. |
| US7115279B2 (en) * | 2000-08-03 | 2006-10-03 | Curatolo William J | Pharmaceutical compositions of cholesteryl ester transfer protein inhibitors |
| CA2474958A1 (en) | 2002-02-01 | 2003-08-07 | Pfizer Products Inc. | Method for making homogeneous spray-dried solid amorphous drug dispersions using pressure nozzles |
| WO2003063822A2 (en) * | 2002-02-01 | 2003-08-07 | Pfizer Products Inc. | Method for making homogeneous spray-dried solid amorphous drug dispersions utilizing modified spray-drying apparatus |
-
2003
- 2003-01-20 CA CA002474958A patent/CA2474958A1/en not_active Abandoned
- 2003-01-20 BR BR0307515-0A patent/BR0307515A/pt not_active IP Right Cessation
- 2003-01-20 WO PCT/IB2003/000120 patent/WO2003063821A2/en not_active Ceased
- 2003-01-20 PL PL03371593A patent/PL371593A1/xx not_active Application Discontinuation
- 2003-01-20 RU RU2004123639/04A patent/RU2288703C2/ru not_active IP Right Cessation
- 2003-01-20 EP EP20030700071 patent/EP1469830A2/en not_active Withdrawn
- 2003-01-20 JP JP2003563515A patent/JP2005523260A/ja active Pending
- 2003-01-20 MX MXPA04007435A patent/MXPA04007435A/es active IP Right Grant
- 2003-01-20 RS YU67304A patent/RS67304A/sr unknown
- 2003-01-20 CN CNA038047640A patent/CN1787808A/zh active Pending
- 2003-01-20 AU AU2003239463A patent/AU2003239463B2/en not_active Ceased
- 2003-01-20 KR KR1020047011807A patent/KR100758045B1/ko not_active Expired - Fee Related
- 2003-01-24 US US10/351,568 patent/US7780988B2/en active Active
- 2003-01-28 TW TW092101817A patent/TW200404576A/zh unknown
- 2003-01-29 PE PE2003000096A patent/PE20030804A1/es not_active Application Discontinuation
- 2003-01-30 GT GT200300024A patent/GT200300024A/es unknown
- 2003-01-30 AR ARP030100268A patent/AR038369A1/es unknown
- 2003-01-31 UY UY27645A patent/UY27645A1/es not_active Application Discontinuation
- 2003-02-03 PA PA20038565401A patent/PA8565401A1/es unknown
-
2004
- 2004-07-27 ZA ZA200405971A patent/ZA200405971B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2003063821A3 (en) | 2003-11-13 |
| AU2003239463B2 (en) | 2007-10-18 |
| GT200300024A (es) | 2003-09-22 |
| PA8565401A1 (es) | 2003-12-10 |
| WO2003063821A2 (en) | 2003-08-07 |
| RU2004123639A (ru) | 2005-04-20 |
| PL371593A1 (en) | 2005-06-27 |
| RS67304A (sr) | 2006-10-27 |
| CN1787808A (zh) | 2006-06-14 |
| RU2288703C2 (ru) | 2006-12-10 |
| PE20030804A1 (es) | 2003-09-19 |
| US7780988B2 (en) | 2010-08-24 |
| JP2005523260A (ja) | 2005-08-04 |
| CA2474958A1 (en) | 2003-08-07 |
| KR20040083491A (ko) | 2004-10-02 |
| EP1469830A2 (en) | 2004-10-27 |
| KR100758045B1 (ko) | 2007-09-11 |
| TW200404576A (en) | 2004-04-01 |
| UY27645A1 (es) | 2003-09-30 |
| BR0307515A (pt) | 2004-12-07 |
| ZA200405971B (en) | 2006-05-31 |
| MXPA04007435A (es) | 2004-10-11 |
| US20030185893A1 (en) | 2003-10-02 |
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