AR080934A1 - Procedimiento de preparacion de composiciones farmaceuticas destinadas a la administracion por via oral que comprenden uno o varios principios activos y las composiciones que las comprenden - Google Patents

Procedimiento de preparacion de composiciones farmaceuticas destinadas a la administracion por via oral que comprenden uno o varios principios activos y las composiciones que las comprenden

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Publication number
AR080934A1
AR080934A1 ARP110101364A ARP110101364A AR080934A1 AR 080934 A1 AR080934 A1 AR 080934A1 AR P110101364 A ARP110101364 A AR P110101364A AR P110101364 A ARP110101364 A AR P110101364A AR 080934 A1 AR080934 A1 AR 080934A1
Authority
AR
Argentina
Prior art keywords
weight
composition
coated granule
binder
relation
Prior art date
Application number
ARP110101364A
Other languages
English (en)
Inventor
Axelle Lesot
Damia Leydet
Aranaud Moussel
Original Assignee
Sanofi Aventis
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42797556&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR080934(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Sanofi Aventis filed Critical Sanofi Aventis
Publication of AR080934A1 publication Critical patent/AR080934A1/es

Links

Classifications

    • 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
    • A61K9/1682Processes
    • 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
    • A61JCONTAINERS SPECIALLY ADAPTED FOR MEDICAL OR PHARMACEUTICAL PURPOSES; DEVICES OR METHODS SPECIALLY ADAPTED FOR BRINGING PHARMACEUTICAL PRODUCTS INTO PARTICULAR PHYSICAL OR ADMINISTERING FORMS; DEVICES FOR ADMINISTERING FOOD OR MEDICINES ORALLY; BABY COMFORTERS; DEVICES FOR RECEIVING SPITTLE
    • A61J3/00Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms
    • A61J3/005Coating of tablets or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0087Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • 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
    • 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
    • A61K9/167Agglomerates; 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
    • 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
    • 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
    • A61K9/2072Pills, 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
    • A61K9/2077Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
    • A61K9/2081Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets with microcapsules or coated microparticles according to A61K9/50
    • 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
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • 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
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2893Tablet coating processes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules 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
    • A61K9/5005Wall or coating material
    • A61K9/5015Organic compounds, e.g. fats, sugars
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules 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
    • A61K9/5089Processes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • A61K9/14Particulate 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
    • A61K9/1641Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers

Landscapes

  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pulmonology (AREA)
  • Physiology (AREA)
  • Zoology (AREA)
  • Nutrition Science (AREA)
  • Immunology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Otolaryngology (AREA)
  • Dermatology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Compositions Of Macromolecular Compounds (AREA)
  • Paints Or Removers (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)

Abstract

Procedimiento de recubrimiento en caliente denominado ½ Hot melt coating de principios activos farmacéuticos caracterizados por propiedades organolépticos o fisicoquímicas que son deseables enmascarar. Principios activos medicamentosos con propiedades organolépticas o fisicoquímicas enmascaradas así obtenidas y a las composiciones que los comprenden. Reivindicacion 1: Procedimiento de preparacion de una composicion de principio activo medicamentoso que comprende (a) un centro granulado constituido por granos de principio activo aglomerados en presencia de aglomerante y (b) una capa de recubrimiento de dicho centro granulado constituida por matriz grasa, composicion en la que: ò el principio activo representa como mínimo 10%, de preferencia 20% o incluso 30% en peso con relacion al peso de la composicion del gránulo recubierto; el principio activo representa como máximo 48%, de preferencia como máximo 40%, de preferencia el principio activo representa de 20% a menos de 40% con relacion al peso de la composicion del gránulo recubierto, más preferentemente el principio activo representa de 30% a 40% con relacion al peso de la composicion del gránulo recubierto; ò la matriz grasa representa más de 50% y hasta 85% en peso de la composicion del gránulo recubierto de preferencia de 51% a 65%, la matriz grasa que comprende opcionalmente un adyuvante, de preferencia se elige entre los agentes hidrofilos, los agentes tensioactivos o sus mezclas, y representando estos ultimos menos de 10%, de preferencia de 1 a 3% en peso con relacion al peso de la composicion del gránulo recubierto; ò el aglomerante, de preferencia un agente hidrofilo elegido entre les polímeros hidrofilos o los agentes termofusibles, representa de 0,2 a 18% en peso con relacion al peso de la composicion del gránulo recubierto, de preferencia el aglomerante representa menos de 18% en peso para un agente termofusible o incluso de preferencia el aglomerante representa menos de 10% en peso para un polímero hidrofilo; ò el diluyente, si es necesario, como agente de carga representa un contenido de 0 a 39% con relacion al peso de la composicion del gránulo recubierto; ò el lubricante, si es necesario, como agente de flujo representa un contenido de 0 a 1,8% con relacion al peso de la composicion del gránulo recubierto; el procedimiento comprende las etapas de: E1) preparacion del centro granulado por pulverizacion de una disolucion acuosa que comprende el aglomerante o por pulverizacion del aglomerante en fusion sobre el principio activo solo o mezclado con un diluyente y/o un lubricante; E2) recubrimiento por pulverizacion sobre los gránulos de dicha matriz grasa previamente fundida en un fusor a una temperatura de alrededor de 10 a 20°C superior a su punto de fusion; E3) enfriamiento de la composicion obtenida. Reivindicacion 16: Procedimiento segun una de las reivindicaciones 1 a 15 en el que el principio activo se elige entre el grupo constituido por antibioticos tales como cefalosporinas y macrolidos, ventajosamente se elige entre: pristinamicina, cefpodoxima, roxitromicina, espiramicina, rovamicina, levofloxacina o el grupo constituido por corticoides tales como prednisolona, metilprednisolona, o también el grupo constituido por AINS tales como ácido tiaprofénico, cetoprofeno, lisinato de cetoprofeno, ibuprofeno, o el grupo constituido por analgésicos como paracetamol, o también el grupo constituido por zopiclona, riluzol, zolpidem, clobazam, tiocolchicosico, hidrocloruro o base de drotaverina, hidrocloruro de amodiaquina, diltiazem, levocetirizina, mizolastina, dronedarona, celivarona, dramamina, ramiprilo, irbesartan, clopidogrel, leflunomida, nicorandil, acetil salicilato de lisina, ramiprilo, citrato de magnesio, levotiroxina, valproato de sodio, rifampicina, artesunato y omeprazol.
ARP110101364A 2010-04-21 2011-04-20 Procedimiento de preparacion de composiciones farmaceuticas destinadas a la administracion por via oral que comprenden uno o varios principios activos y las composiciones que las comprenden AR080934A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
FR1053034A FR2959130A1 (fr) 2010-04-21 2010-04-21 Procede de preparation de compositions pharmaceutiques destinees a l'administration par voie orale comprenant un ou plusieurs principes actifs et les compositions les comprenant.

Publications (1)

Publication Number Publication Date
AR080934A1 true AR080934A1 (es) 2012-05-16

Family

ID=42797556

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP110101364A AR080934A1 (es) 2010-04-21 2011-04-20 Procedimiento de preparacion de composiciones farmaceuticas destinadas a la administracion por via oral que comprenden uno o varios principios activos y las composiciones que las comprenden
ARP110101365A AR081539A1 (es) 2010-04-21 2011-04-20 Composicion a base de fexofenadina y procedimiento de preparacion, sobre o comprimido, uso de la composicion

Family Applications After (1)

Application Number Title Priority Date Filing Date
ARP110101365A AR081539A1 (es) 2010-04-21 2011-04-20 Composicion a base de fexofenadina y procedimiento de preparacion, sobre o comprimido, uso de la composicion

Country Status (22)

Country Link
US (2) US20130251794A1 (es)
EP (2) EP2560612B1 (es)
JP (2) JP2013525341A (es)
KR (2) KR20130094716A (es)
CN (2) CN102946857A (es)
AR (2) AR080934A1 (es)
AU (2) AU2011262319A1 (es)
BR (2) BR112012026596A2 (es)
CA (2) CA2796816A1 (es)
CL (2) CL2012002898A1 (es)
CO (2) CO6620042A2 (es)
EA (2) EA201291088A1 (es)
ES (2) ES2525163T3 (es)
FR (1) FR2959130A1 (es)
IL (2) IL222578A0 (es)
MA (2) MA34226B1 (es)
MX (1) MX2012012275A (es)
PL (2) PL2560613T3 (es)
SG (3) SG184951A1 (es)
TW (2) TWI478713B (es)
UY (2) UY33350A (es)
WO (2) WO2011151733A2 (es)

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EP2560613B1 (en) 2014-10-15
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EP2560612B1 (en) 2014-09-03
MA34226B1 (fr) 2013-05-02
CN103002874A (zh) 2013-03-27
PL2560613T3 (pl) 2015-03-31
EA201291088A1 (ru) 2013-03-29
IL222576A0 (en) 2012-12-31
EA201291089A1 (ru) 2013-05-30
CL2012002898A1 (es) 2013-03-01
US20130251794A1 (en) 2013-09-26
TW201204415A (en) 2012-02-01
MA34227B1 (fr) 2013-05-02
KR20130080428A (ko) 2013-07-12
KR20130094716A (ko) 2013-08-26
TW201206434A (en) 2012-02-16
TWI478713B (zh) 2015-04-01
WO2011151733A3 (en) 2012-01-26
WO2011132167A1 (en) 2011-10-27
CO6620042A2 (es) 2013-02-15
IL222578A0 (en) 2012-12-31
ES2527390T3 (es) 2015-01-23
JP2013525341A (ja) 2013-06-20
SG184951A1 (en) 2012-11-29
PL2560612T3 (pl) 2015-03-31
CA2796816A1 (en) 2011-12-08
MX2012012275A (es) 2012-11-16
AR081539A1 (es) 2012-10-03
EP2560613A2 (en) 2013-02-27
AU2011262319A1 (en) 2012-11-08
BR112012026938A2 (pt) 2017-10-03
AU2011244020A1 (en) 2012-11-08
EP2560612A1 (en) 2013-02-27
CO6620043A2 (es) 2013-02-15
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WO2011151733A2 (en) 2011-12-08
FR2959130A1 (fr) 2011-10-28
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BR112012026596A2 (pt) 2016-07-12
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