ES2525648T3 - Formulaciones galénicas que comprenden Aliskiren - Google Patents

Formulaciones galénicas que comprenden Aliskiren Download PDF

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Publication number
ES2525648T3
ES2525648T3 ES10702092.7T ES10702092T ES2525648T3 ES 2525648 T3 ES2525648 T3 ES 2525648T3 ES 10702092 T ES10702092 T ES 10702092T ES 2525648 T3 ES2525648 T3 ES 2525648T3
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Spain
Prior art keywords
aliskiren
minitableta
coating
core
galenic formulations
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ES10702092.7T
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English (en)
Inventor
Sabine DESSET-BRÈTHES
Stefan Hirsch
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Novartis AG
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Novartis AG
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Application filed by Novartis AG filed Critical Novartis AG
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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
    • A61K9/20—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
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • 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
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
    • A61K9/2846—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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
    • A61K9/2866—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
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • A61P9/12—Antihypertensives

Landscapes

  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Una forma de dosificación unitaria sólida para administración oral en Ia forma de una minitableta que tiene un núcleo y un recubrimiento externo, en donde: - el núcleo comprende una cantidad terapéuticamente efectiva de Aliskiren, o una sal farmacéuticamente aceptable del mismo, y - el recubrimiento exterior es en forma de una película de revestimiento que comprende un material de enmascaramiento del sabor seleccionado de entre poliacrilatos, y/o un componente de recubrimiento de liberación modificada seleccionado a partir de derivados de celulosa, copolímeros acrílicos, y mezclas de los mismos, en donde dicha minitableta tiene un tamaño de entre 1 mm y 4 mm, y en donde dicha minitableta contiene entre aproximadamente 2 mg y aproximadamente 4 mg de Aliskiren.

Description

imagen1
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imagen18
E10702092
28-11-2014
Tabla 3 Relación de la media geométrica y 90% de CI de SSP de la Variante A
Variante A / Referencia
Pt estimada
90% de CI
Cmáx (ng/mL)
1,499 1,181 -1,901
AUC0-t (ng.h/mL)
1,164 1,004 -1,350
AUC0-inf (ng.h/mL)
1,168 1,010 -1,350
Tabla 4 Valores de la media geométrica de Cmax y AUC de SSP de la solución de SPP100 de 75 mg
Dos cápsulas de SPP de 37,5 mg (referencia)
Solución de SPP de 75 mg
Media geométrica
Media geométrica
Cmax (ng/mL)
28 15
AUC0-inf (ng.h/mL)
225 158
La biodisponibilidad de la formulación de acuerdo con la presente invención tenía una biodisponibilidad comparable a la tableta de Aliskiren comercializada (referencia), así como la formulación de cápsula, y una biodisponibilidad mucho mejor comparada con la formulación líquida.
Tabla 5 Farmacocinéticas en pacientes pediátricos
Grupo de edad (años)
Dosis Día Cmáx (ng/mL) Tmáx* (h) AUCtau (ng.h/mL) AI T1/2 (h)
12 -17
Media 136 1,0 391 - --
DE
1 133 0,5, 3,0 264 - -
% de CV
97 68 - -
2 mg/kg
Media
279 1,0 846 2,1 40
DE
8 358 0,5, 3,0 804 1,3 5,0
% de CV
128 95 62 13
Media
424 1,8 1801 - --
DE
1 189 0,5, 4,0 811 - -
% de CV
44 45 - -
20
E10702092
28-11-2014
(continuación)
Grupo de edad (años)
Dosis Día Cmáx (ng/mL) Tmáx* (h) AUCtau (ng.h/mL) AI T1/2 (h)
12-17
6 mg/kg
Media
486 2,0 2089 1,3 42
DE
8 301 0,5, 3,0 1003 0,6 6,5
% de CV
62 48 50 16
Media
39 0,5 149 - --
DE
1 21 0,5, 3,0 74 - -
% de CV
53 49 - -
2 mg/kg
6 -11
Media 48 0,5 240 1,5 40
DE
8 39 0,5, 1,0 183 0,5 6,6
% de CV
81 76 31 16
Media
323 1,3 1841 - --
DE
1 55 1,0, 1,5 1168 - -
% de CV
17 63 - -
6 mg/kg
Media
259 0,8 956 0,5 36
DE
8 274 0,5, 1,0 568 0,0 0,7
% de CV
106 59 0 2
* Mediana (min, máx.)
21

Claims (1)

  1. imagen1
    imagen2
ES10702092.7T 2009-01-28 2010-01-27 Formulaciones galénicas que comprenden Aliskiren Active ES2525648T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09151496 2009-01-28
EP09151496 2009-01-28
PCT/EP2010/050886 WO2010086312A1 (en) 2009-01-28 2010-01-27 Galenic formulations of organic compounds

Publications (1)

Publication Number Publication Date
ES2525648T3 true ES2525648T3 (es) 2014-12-26

Family

ID=40770648

Family Applications (1)

Application Number Title Priority Date Filing Date
ES10702092.7T Active ES2525648T3 (es) 2009-01-28 2010-01-27 Formulaciones galénicas que comprenden Aliskiren

Country Status (28)

Country Link
US (1) US20110287100A1 (es)
EP (1) EP2391345B1 (es)
JP (1) JP2012516299A (es)
KR (1) KR20110117199A (es)
CN (1) CN102300558A (es)
AR (1) AR075179A1 (es)
AU (1) AU2010209787B2 (es)
BR (1) BRPI1007452A2 (es)
CA (1) CA2749531A1 (es)
CL (1) CL2011001817A1 (es)
CO (1) CO6400184A2 (es)
EC (1) ECSP11011289A (es)
ES (1) ES2525648T3 (es)
HK (1) HK1161125A1 (es)
IL (1) IL213918A0 (es)
MA (1) MA33060B1 (es)
MX (1) MX2011007779A (es)
MY (1) MY153852A (es)
NZ (1) NZ593622A (es)
PE (1) PE20110943A1 (es)
PL (1) PL2391345T3 (es)
PT (1) PT2391345E (es)
RU (1) RU2535090C2 (es)
SG (1) SG172226A1 (es)
TN (1) TN2011000307A1 (es)
TW (1) TWI468191B (es)
WO (1) WO2010086312A1 (es)
ZA (1) ZA201104489B (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5822758B2 (ja) * 2011-03-02 2015-11-24 第一三共ヘルスケア株式会社 速溶性防湿フィルムコーティング製剤及びその製造方法
EP2596802A1 (en) * 2011-11-23 2013-05-29 PLS-Design GmbH Pharmaceutical composition for treatment of allergic reactions
CN108601741B (zh) * 2016-02-03 2022-05-24 诺华股份有限公司 有机化合物的盖伦制剂
US20210308054A1 (en) * 2018-08-10 2021-10-07 Kissei Pharmaceutical Co., Ltd. Sucroferric oxyhydroxide-containing granules and pharmaceutical composition
TW202045140A (zh) * 2019-02-22 2020-12-16 英商康泰倫特英國斯文敦載迪斯有限公司 保存水性懸浮液中以無溶劑混合方法製備的功能性塗覆之活性醫藥成份微粒
MX2021009679A (es) 2019-02-22 2021-09-10 Catalent Uk Swindon Zydis Ltd Minimizacion de aglomeracion, aireacion y conservacion del revestimiento de composiciones farmaceuticas que comprenden ibuprofeno.
WO2021011538A1 (en) * 2019-07-15 2021-01-21 R.P. Scherer Technologies, Llc Capsule dosage forms, methods of preparation and methods of use thereof

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MY119161A (en) 1994-04-18 2005-04-30 Novartis Ag Delta-amino-gamma-hydroxy-omega-aryl-alkanoic acid amides with enzyme especially renin inhibiting activities
DE19842753A1 (de) * 1998-09-18 2000-03-23 Bayer Ag Agitationsunabhängige pharmazeutische Retardzubereitungen und Verfahren zu ihrer Herstellung
US6248363B1 (en) * 1999-11-23 2001-06-19 Lipocine, Inc. Solid carriers for improved delivery of active ingredients in pharmaceutical compositions
AR034813A1 (es) * 2001-07-20 2004-03-17 Novartis Ag Composiciones farmaceuticas y uso de las mismas
WO2004100871A2 (en) * 2003-05-09 2004-11-25 Pharmacia Corporation Combination of an aldosterone receptor antagonist and a renin inhibitor
PE20110121A1 (es) * 2004-03-17 2011-02-28 Novartis Ag Composiciones farmaceuticas de aliskiren
BRPI0509971A (pt) * 2004-04-15 2007-10-02 Reddys Lab Inc Dr uma forma de dosagem farmacêutica, comprimido e método de preparação
KR20070101843A (ko) * 2004-10-08 2007-10-17 노파르티스 아게 확장기 기능장애 또는 확장기 심부전의 예방 또는 치료를위한 레닌 억제제의 용도
RU2010116526A (ru) * 2007-09-28 2011-11-10 Новартис АГ (CH) Фармацевтическая комбинация алискирена и валсартана

Also Published As

Publication number Publication date
AU2010209787A1 (en) 2011-07-14
TN2011000307A1 (en) 2012-12-17
AU2010209787B2 (en) 2013-06-06
AR075179A1 (es) 2011-03-16
MA33060B1 (fr) 2012-02-01
RU2535090C2 (ru) 2014-12-10
JP2012516299A (ja) 2012-07-19
TW201038300A (en) 2010-11-01
CL2011001817A1 (es) 2012-01-13
HK1161125A1 (en) 2012-08-24
PE20110943A1 (es) 2012-01-22
RU2011135417A (ru) 2013-03-10
US20110287100A1 (en) 2011-11-24
BRPI1007452A2 (pt) 2016-02-16
KR20110117199A (ko) 2011-10-26
SG172226A1 (en) 2011-07-28
EP2391345B1 (en) 2014-09-03
CA2749531A1 (en) 2010-08-05
EP2391345A1 (en) 2011-12-07
ZA201104489B (en) 2012-02-29
NZ593622A (en) 2013-12-20
PL2391345T3 (pl) 2015-03-31
MY153852A (en) 2015-03-31
MX2011007779A (es) 2011-08-12
CN102300558A (zh) 2011-12-28
IL213918A0 (en) 2011-07-31
ECSP11011289A (es) 2011-09-30
CO6400184A2 (es) 2012-03-15
TWI468191B (zh) 2015-01-11
WO2010086312A1 (en) 2010-08-05
PT2391345E (pt) 2014-12-03

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