WO2014003678A1 - Compositions pharmaceutiques comprenant de l'ambrisentan et des particules de dispersion solide contenant du tadalafil - Google Patents

Compositions pharmaceutiques comprenant de l'ambrisentan et des particules de dispersion solide contenant du tadalafil Download PDF

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Publication number
WO2014003678A1
WO2014003678A1 PCT/SE2013/050808 SE2013050808W WO2014003678A1 WO 2014003678 A1 WO2014003678 A1 WO 2014003678A1 SE 2013050808 W SE2013050808 W SE 2013050808W WO 2014003678 A1 WO2014003678 A1 WO 2014003678A1
Authority
WO
WIPO (PCT)
Prior art keywords
tadalafil
composition
ambrisentan
composition according
solid dispersion
Prior art date
Application number
PCT/SE2013/050808
Other languages
English (en)
Inventor
Gérald JESSON
Mustafa Demirbüker
Magnus Brisander
Original Assignee
Xspray Microparticles Ab
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 Xspray Microparticles Ab filed Critical Xspray Microparticles Ab
Publication of WO2014003678A1 publication Critical patent/WO2014003678A1/fr

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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
    • A61K9/14—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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • 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

Definitions

  • ambrisentan is meant the compound named (2S)-2-[(4,6- dimethylpyrimidin-2-yl)oxy]-3-methoxy- 3,3-diphenylpropanoic acid.
  • the structure of ambrisentan can be illustrated as:
  • PVP 30K refers to polyvinylpyrrolidone K-30.
  • said solid dispersion particles are prepared by a solid dispersion process using CO2 as antisolvent.
  • Such solid dispersion particles may be produced by a process utilizing CO2, for the formation of solid dispersion particles containing tadalafil, typically as described in this disclosure.
  • said dispersing component is a polymeric dispersing component.
  • compositions of the invention for use, wherein said composition is provided during food intake.
  • the compositions of the invention are formulated for oral administration, such as wherein said composition is administered with amounts of up to a maximum of 40 mg tadalafil per day and 40 mg ambrisentan per day.
  • said composition may be administered with amounts of up to a maximum of 20 mg tadalafil per day and 40 mg ambrisentan per day.
  • Example 2 Compositions with tadalafil solid dispersion particles and ambrisentan - solubility at pH 1.4.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cardiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Organic Chemistry (AREA)
  • Inorganic Chemistry (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La présente invention concerne des compositions pharmaceutiques comprenant des particules de dispersion solide contenant du tadalafil et un composant dispersant; et de l'ambrisentan, laquelle composition comprend en outre de manière facultative au moins un excipient pharmaceutiquement acceptable, tel qu'un agent de solubilisation. En outre, la présente invention concerne une méthode de traitement de troubles chez un patient nécessitant un tel traitement, qui consiste à administrer une quantité thérapeutiquement efficace de ladite composition.
PCT/SE2013/050808 2012-06-28 2013-06-27 Compositions pharmaceutiques comprenant de l'ambrisentan et des particules de dispersion solide contenant du tadalafil WO2014003678A1 (fr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201261665399P 2012-06-28 2012-06-28
SE1250730 2012-06-28
US61/665,399 2012-06-28
SE1250730-7 2012-06-28

Publications (1)

Publication Number Publication Date
WO2014003678A1 true WO2014003678A1 (fr) 2014-01-03

Family

ID=49783647

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/SE2013/050808 WO2014003678A1 (fr) 2012-06-28 2013-06-27 Compositions pharmaceutiques comprenant de l'ambrisentan et des particules de dispersion solide contenant du tadalafil

Country Status (1)

Country Link
WO (1) WO2014003678A1 (fr)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015000853A1 (fr) * 2013-07-05 2015-01-08 Synthon B.V. Composition pharmaceutique comprenant une dispersion solide de tadalafil
CN109276546A (zh) * 2018-10-07 2019-01-29 威海贯标信息科技有限公司 一种安立生坦片剂组合物
WO2020221916A3 (fr) * 2019-05-01 2020-12-03 Novochem Green Additives B.V. Composition eutectique

Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5985326A (en) * 1995-06-02 1999-11-16 Icos Corporation Method of producing a solid dispersion of a poorly water soluble drug
WO2001008688A2 (fr) * 1999-08-03 2001-02-08 Lilly Icos Llc PRODUITS DE MEDICAMENTS A BASE DE β-CARBOLINE
EP1875914A1 (fr) * 2006-07-07 2008-01-09 Teva Pharmaceutical Industries Ltd. Les compositions solides comprenant tadalafil et au moins d'un agent de support
WO2009050291A2 (fr) * 2007-10-19 2009-04-23 Abbott Gmbh & Co. Kg Produit de dispersion solide de médicaments de type n-aryle à base d'urée
US20100179159A1 (en) * 2007-06-22 2010-07-15 Ratiopharm Gmbh Method for the production of a medicament containing tadalafil
WO2011042463A2 (fr) * 2009-10-07 2011-04-14 Lek Pharmaceuticals D.D. Composition pharmaceutique comprenant un principe actif médiocrement soluble et un polymère hyper-ramifié
US20110136815A1 (en) * 2009-12-08 2011-06-09 Horst Zerbe Solid oral film dosage forms and methods for making same
US20110245253A1 (en) * 2006-12-12 2011-10-06 Gerber Michael J Method for treating a pulmonary hypertension condition
WO2012051559A2 (fr) * 2010-10-15 2012-04-19 Gilead Sciences, Inc. Compositions et méthodes de traitement de l'hypertension artérielle pulmonaire

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5985326A (en) * 1995-06-02 1999-11-16 Icos Corporation Method of producing a solid dispersion of a poorly water soluble drug
WO2001008688A2 (fr) * 1999-08-03 2001-02-08 Lilly Icos Llc PRODUITS DE MEDICAMENTS A BASE DE β-CARBOLINE
EP1875914A1 (fr) * 2006-07-07 2008-01-09 Teva Pharmaceutical Industries Ltd. Les compositions solides comprenant tadalafil et au moins d'un agent de support
US20110245253A1 (en) * 2006-12-12 2011-10-06 Gerber Michael J Method for treating a pulmonary hypertension condition
US20100179159A1 (en) * 2007-06-22 2010-07-15 Ratiopharm Gmbh Method for the production of a medicament containing tadalafil
WO2009050291A2 (fr) * 2007-10-19 2009-04-23 Abbott Gmbh & Co. Kg Produit de dispersion solide de médicaments de type n-aryle à base d'urée
WO2011042463A2 (fr) * 2009-10-07 2011-04-14 Lek Pharmaceuticals D.D. Composition pharmaceutique comprenant un principe actif médiocrement soluble et un polymère hyper-ramifié
US20110136815A1 (en) * 2009-12-08 2011-06-09 Horst Zerbe Solid oral film dosage forms and methods for making same
WO2012051559A2 (fr) * 2010-10-15 2012-04-19 Gilead Sciences, Inc. Compositions et méthodes de traitement de l'hypertension artérielle pulmonaire

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
MEHANNA, M.M. ET AL.: "In Sight into Tadalafil - Block Copolymer Binary Solid Dispersion: Mechanistic Investigation of Dissolution Enhancement", INTERNATIONAL JOURNAL OF PHARMACEUTICS., vol. 402, no. 1-2, 2010, pages 78 - 88 *
ONIKE, O. ET AL.: "Tadalafil-Soluplus Solid Dispersion using Melt Extrusion for Improved Dissolution", JOURNAL OF PHARMACY AND PHARMACOLOGY., vol. 62, no. 10, 2010, pages 1476 - 1477 *
VIKRANT, Y. ET AL.: "Physicochemical Characterization of Solid Dispersion Systems of Tadalafil with Poloxamer 407", ACTA PHARMACEUTICA, vol. 59, no. 4, 2009, pages 453 - 461 *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015000853A1 (fr) * 2013-07-05 2015-01-08 Synthon B.V. Composition pharmaceutique comprenant une dispersion solide de tadalafil
CN109276546A (zh) * 2018-10-07 2019-01-29 威海贯标信息科技有限公司 一种安立生坦片剂组合物
WO2020221916A3 (fr) * 2019-05-01 2020-12-03 Novochem Green Additives B.V. Composition eutectique

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