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WO2007106111A3 - Compositions nanoparticulaires et a liberation controlee comprenant de la nilvadipine - Google Patents

Compositions nanoparticulaires et a liberation controlee comprenant de la nilvadipine Download PDF

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Publication number
WO2007106111A3
WO2007106111A3 PCT/US2006/025803 US2006025803W WO2007106111A3 WO 2007106111 A3 WO2007106111 A3 WO 2007106111A3 US 2006025803 W US2006025803 W US 2006025803W WO 2007106111 A3 WO2007106111 A3 WO 2007106111A3
Authority
WO
WIPO (PCT)
Prior art keywords
nilvadipine
polymorph
prodrug
derivative
salt
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/US2006/025803
Other languages
English (en)
Other versions
WO2007106111A2 (fr
Inventor
John Devane
Paul Stark
Niall Fanning
Gurvinder Rekhi
Scott Jenkins
Gary Liversidge
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Perrigo Pharma International DAC
Original Assignee
Elan Pharma International Ltd
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 Elan Pharma International Ltd filed Critical Elan Pharma International Ltd
Publication of WO2007106111A2 publication Critical patent/WO2007106111A2/fr
Anticipated expiration legal-status Critical
Publication of WO2007106111A3 publication Critical patent/WO2007106111A3/fr
Ceased legal-status Critical Current

Links

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
    • A61K9/146—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 macromolecular compounds
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5084—Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs
    • 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
    • A61K9/167—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface
    • A61K9/1676—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface having a drug-free core with discrete complete coating layer containing drug
    • 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
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005—Wall or coating material
    • A61K9/5021—Organic macromolecular compounds
    • A61K9/5026—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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5073—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings
    • A61K9/5078—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings with drug-free core

Landscapes

  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention concerne une composition comprenant de la nilvadipine ou un sel, dérivé, promédicament ou polymorphe de celle-ci, utile dans le traitement et la prévention de l'hypertension ou des troubles de type cardiovasculaire. Dans une forme de réalisation, la composition comprend des particules nanoparticulaires comprenant de la nilvadipine ou un sel, dérivé, promédicament ou polymorphe de celle, ainsi qu'au moins un stabilisant de surface. Lesdites particules nanoparticulaires possèdent une granulométrie moyenne effective inférieure à environ 2000 nm. Dans une autre forme de réalisation, la composition comprend une composition à libération modifiée qui, lorsqu'elle est administrée à un patient, libère de la nilvadipine ou un sel, dérivé, promédicament ou polymorphe de celle-ci de façon bimodale, multimodale ou continue. Cette invention concerne également des formes galéniques contenant de telles compositions ainsi que des procédés de traitement et de prévention de l'hypertension ou des troubles de type cardiovasculaire.
PCT/US2006/025803 2005-07-01 2006-06-30 Compositions nanoparticulaires et a liberation controlee comprenant de la nilvadipine Ceased WO2007106111A2 (fr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US69611705P 2005-07-01 2005-07-01
US69644205P 2005-07-01 2005-07-01
US60/696,117 2005-07-01
US60/696,442 2005-07-01

Publications (2)

Publication Number Publication Date
WO2007106111A2 WO2007106111A2 (fr) 2007-09-20
WO2007106111A3 true WO2007106111A3 (fr) 2009-02-26

Family

ID=38509921

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2006/025803 Ceased WO2007106111A2 (fr) 2005-07-01 2006-06-30 Compositions nanoparticulaires et a liberation controlee comprenant de la nilvadipine

Country Status (1)

Country Link
WO (1) WO2007106111A2 (fr)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012142927A1 (fr) * 2011-04-18 2012-10-26 合肥贝霓医药科技有限公司 Procédé de purification de bloquants du canal calcique de type dihydropyridine et préparation de nanoparticules de ceux-ci
RU2666963C2 (ru) 2012-04-13 2018-09-13 Глаксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед Агрегированные частицы

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5594013A (en) * 1992-01-13 1997-01-14 Ethical Pharmaceuticals Limited Pharmaceutical compositions containing nifedipine and process for the preparation thereof
US5785994A (en) * 1990-08-31 1998-07-28 Alza Corporation Method for administering drug to gastrointestinal tract
US5811447A (en) * 1993-01-28 1998-09-22 Neorx Corporation Therapeutic inhibitor of vascular smooth muscle cells
US20040053842A1 (en) * 2002-07-02 2004-03-18 Pfizer Inc. Methods of treatment with CETP inhibitors and antihypertensive agents
US20040141922A1 (en) * 1996-10-28 2004-07-22 Nycomed Imaging As Diagnostic/therapeutic agents

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5785994A (en) * 1990-08-31 1998-07-28 Alza Corporation Method for administering drug to gastrointestinal tract
US5594013A (en) * 1992-01-13 1997-01-14 Ethical Pharmaceuticals Limited Pharmaceutical compositions containing nifedipine and process for the preparation thereof
US5811447A (en) * 1993-01-28 1998-09-22 Neorx Corporation Therapeutic inhibitor of vascular smooth muscle cells
US20040141922A1 (en) * 1996-10-28 2004-07-22 Nycomed Imaging As Diagnostic/therapeutic agents
US20040053842A1 (en) * 2002-07-02 2004-03-18 Pfizer Inc. Methods of treatment with CETP inhibitors and antihypertensive agents

Also Published As

Publication number Publication date
WO2007106111A2 (fr) 2007-09-20

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