AR065301A1 - Formulaciones farmaceuticas solidas de una dispersion homogenea de principios activos cuya solubilidad es dependiente del ph - Google Patents
Formulaciones farmaceuticas solidas de una dispersion homogenea de principios activos cuya solubilidad es dependiente del phInfo
- Publication number
- AR065301A1 AR065301A1 ARP080100585A ARP080100585A AR065301A1 AR 065301 A1 AR065301 A1 AR 065301A1 AR P080100585 A ARP080100585 A AR P080100585A AR P080100585 A ARP080100585 A AR P080100585A AR 065301 A1 AR065301 A1 AR 065301A1
- Authority
- AR
- Argentina
- Prior art keywords
- solid
- pharmaceutical
- pharmaceutical formulations
- acceptable
- solid pharmaceutical
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 7
- 239000007787 solid Substances 0.000 title abstract 7
- 230000001419 dependent effect Effects 0.000 title abstract 2
- 239000006185 dispersion Substances 0.000 title 1
- 238000000034 method Methods 0.000 abstract 4
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 abstract 3
- 150000003839 salts Chemical class 0.000 abstract 3
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 2
- 201000011510 cancer Diseases 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 238000009472 formulation Methods 0.000 abstract 2
- 239000007970 homogeneous dispersion Substances 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 230000002062 proliferating effect Effects 0.000 abstract 2
- 239000007909 solid dosage form Substances 0.000 abstract 2
- YCOYDOIWSSHVCK-UHFFFAOYSA-N vatalanib Chemical compound C1=CC(Cl)=CC=C1NC(C1=CC=CC=C11)=NN=C1CC1=CC=NC=C1 YCOYDOIWSSHVCK-UHFFFAOYSA-N 0.000 abstract 2
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical group OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 abstract 1
- 229930195725 Mannitol Natural products 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 239000012736 aqueous medium Substances 0.000 abstract 1
- XSCHRSMBECNVNS-UHFFFAOYSA-N benzopyrazine Natural products N1=CC=NC2=CC=CC=C21 XSCHRSMBECNVNS-UHFFFAOYSA-N 0.000 abstract 1
- 150000001720 carbohydrates Chemical class 0.000 abstract 1
- 150000001735 carboxylic acids Chemical class 0.000 abstract 1
- 230000001427 coherent effect Effects 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 239000012738 dissolution medium Substances 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 239000001530 fumaric acid Substances 0.000 abstract 1
- 235000010355 mannitol Nutrition 0.000 abstract 1
- 239000000594 mannitol Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- -1 or a hydrate thereof Chemical compound 0.000 abstract 1
- LFSXCDWNBUNEEM-UHFFFAOYSA-N phthalazine Chemical compound C1=NN=CC2=CC=CC=C21 LFSXCDWNBUNEEM-UHFFFAOYSA-N 0.000 abstract 1
- 238000003756 stirring Methods 0.000 abstract 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 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
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/145—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with 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
- A61K9/20—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
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
Formulaciones farmacéuticas solidas de una dispersion homogénea de al menos un principio activo cuya solubilidad es dependiente del pH, por ejemplo, 1-[4-cloroanilino]-4-[4-piridilmetil]ftalazina, o una sal de ésta aceptable para uso farmacéutico; formas de dosificacion solidas que comprenden dichas formulaciones farmacéuticas solidas; métodos para preparar dichas formulaciones farmacéuticas solidas y dichas formas de dosificacion solidas; usos de dichas formulaciones farmacéuticas solidas, solas o en combinacion con uno o más compuestos con actividad farmacéutica, especialmente para la fabricacion de un medicamento para el tratamiento de una enfermedad proliferativa, tal como el cáncer; y un método para el tratamiento de una enfermedad proliferativa, tal como el cáncer. Reivindicacion 1: Una formulacion farmacéutica solida caracterizada porque es una dispersion homogénea de: a) una sal aceptable para uso farmacéutico de 1-[4-cloroanilino]-4-[4- piridilmetil]ftalazina; y b) un ácido carboxílico aceptable para uso farmacéutico que tiene un valor de pKa igual o menor que 3,2, como una fase coherente; donde al menos 70% de dicha 1-[4-cloroanilino]-4-[4-piri-dimetil]ftalazina, o la sal de ésta aceptable para uso farmacéutico, se libera de dicha formulacion farmacéutica solida en 30 minutos, lo que se determina con el método de paletas o el método de paletas rotativas USP XXVI, usando un medio acuoso no amortiguado con un pH de 6,8 a 37°C como medio de disolucion, y una velocidad de agitacion de 100 rpm. Reivindicacion 9: La formulacion de acuerdo con la reivindicacion 7 u 8, caracterizada porque dicho ácido es ácido cítrico, o un hidrato de éste, o ácido fumárico, o un hidrato de éste. Reivindicacion 13: La formulacion de acuerdo con la reivindicacion 12, caracterizada porque dicho vehículo que contiene un sacárido es manitol.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP07090018A EP1958615A1 (en) | 2007-02-13 | 2007-02-13 | Solid pharmaceutical formulations of a homogeneous dispersion of active principles having pH-dependent solubility |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR065301A1 true AR065301A1 (es) | 2009-05-27 |
Family
ID=37964604
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP080100585A AR065301A1 (es) | 2007-02-13 | 2008-02-12 | Formulaciones farmaceuticas solidas de una dispersion homogenea de principios activos cuya solubilidad es dependiente del ph |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US20080194570A1 (es) |
| EP (2) | EP1958615A1 (es) |
| JP (1) | JP2010518133A (es) |
| AR (1) | AR065301A1 (es) |
| CA (1) | CA2676684A1 (es) |
| TW (1) | TW200845992A (es) |
| WO (1) | WO2008098760A2 (es) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RS55157B2 (sr) * | 2008-10-07 | 2023-10-31 | Kudos Pharm Ltd | Farmaceutska formulacija 514 |
| CA3050696A1 (en) * | 2017-01-20 | 2018-07-26 | Constellation Pharmaceuticals, Inc. | Solid dispersions of (r)-n-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1h-indole-3-carboxamide |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2470599A1 (fr) * | 1979-12-07 | 1981-06-12 | Panoz Donald | Perfectionnements apportes aux procedes de preparation de formes galeniques a action retard et a liberation programmee et formes galeniques de medicaments ainsi obtenus |
| US20040127470A1 (en) * | 1998-12-23 | 2004-07-01 | Pharmacia Corporation | Methods and compositions for the prevention or treatment of neoplasia comprising a Cox-2 inhibitor in combination with an epidermal growth factor receptor antagonist |
| EP1722762A2 (en) * | 2004-03-02 | 2006-11-22 | Massachusetts Institute of Technology | Nanocell drug delivery system |
| US20060275365A1 (en) * | 2005-06-07 | 2006-12-07 | Thomas Backensfeld | Immediate-release and high-drug-load pharmaceutical formulations of micronised (4-chlorophenyl) [4-(4-pyridylmethyl)phthalazin-1-yl] and salts thereof |
| EP1731154A1 (en) * | 2005-06-07 | 2006-12-13 | Schering Aktiengesellschaft | Immediate-release and high-drug-load pharmaceutical formulations of micronised (4-chlorophenyl)|4-(4-pyridylmethyl)pht halazin-1-yl| and salts thereof |
-
2007
- 2007-02-13 EP EP07090018A patent/EP1958615A1/en not_active Withdrawn
-
2008
- 2008-02-09 JP JP2009549374A patent/JP2010518133A/ja active Pending
- 2008-02-09 EP EP08715762A patent/EP2111221A2/en not_active Withdrawn
- 2008-02-09 CA CA002676684A patent/CA2676684A1/en not_active Abandoned
- 2008-02-09 WO PCT/EP2008/001122 patent/WO2008098760A2/en not_active Ceased
- 2008-02-12 TW TW097104862A patent/TW200845992A/zh unknown
- 2008-02-12 AR ARP080100585A patent/AR065301A1/es unknown
- 2008-02-12 US US12/029,746 patent/US20080194570A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| WO2008098760A2 (en) | 2008-08-21 |
| EP1958615A1 (en) | 2008-08-20 |
| EP2111221A2 (en) | 2009-10-28 |
| WO2008098760A3 (en) | 2009-07-30 |
| US20080194570A1 (en) | 2008-08-14 |
| TW200845992A (en) | 2008-12-01 |
| CA2676684A1 (en) | 2008-08-21 |
| JP2010518133A (ja) | 2010-05-27 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |