WO2011107466A3 - Melt-coated pharmaceutical forms - Google Patents

Melt-coated pharmaceutical forms Download PDF

Info

Publication number
WO2011107466A3
WO2011107466A3 PCT/EP2011/053012 EP2011053012W WO2011107466A3 WO 2011107466 A3 WO2011107466 A3 WO 2011107466A3 EP 2011053012 W EP2011053012 W EP 2011053012W WO 2011107466 A3 WO2011107466 A3 WO 2011107466A3
Authority
WO
WIPO (PCT)
Prior art keywords
melt
pharmaceutical forms
coated pharmaceutical
coatings
water
Prior art date
Application number
PCT/EP2011/053012
Other languages
German (de)
French (fr)
Other versions
WO2011107466A2 (en
Inventor
Karl Kolter
Dejan Djuric
Original Assignee
Basf Se
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 Basf Se filed Critical Basf Se
Priority to CN2011800124846A priority Critical patent/CN102781429A/en
Priority to JP2012555398A priority patent/JP2013521249A/en
Priority to EP11705898A priority patent/EP2542222A2/en
Publication of WO2011107466A2 publication Critical patent/WO2011107466A2/en
Publication of WO2011107466A3 publication Critical patent/WO2011107466A3/en

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
    • A61K9/167Agglomerates; 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
    • A61K9/1676Agglomerates; 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/216Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/4174Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/5415Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam

Abstract

The invention relates to preparations of active agents not easily soluble in water, consisting of carrier particles having active agent-containing coatings, wherein the active agents not easily soluble in water are embedded in coatings made of amphiphilic copolymers and the coatings are applied in the form of a solvent-free melt.
PCT/EP2011/053012 2010-03-05 2011-03-01 Melt-coated pharmaceutical forms WO2011107466A2 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
CN2011800124846A CN102781429A (en) 2010-03-05 2011-03-01 Melt-coated pharmaceutical forms
JP2012555398A JP2013521249A (en) 2010-03-05 2011-03-01 Pharmaceutical form coated with melt
EP11705898A EP2542222A2 (en) 2010-03-05 2011-03-01 Melt-coated pharmaceutical forms

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP10155640.5 2010-03-05
EP10155640 2010-03-05

Publications (2)

Publication Number Publication Date
WO2011107466A2 WO2011107466A2 (en) 2011-09-09
WO2011107466A3 true WO2011107466A3 (en) 2011-12-15

Family

ID=43901590

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2011/053012 WO2011107466A2 (en) 2010-03-05 2011-03-01 Melt-coated pharmaceutical forms

Country Status (4)

Country Link
EP (1) EP2542222A2 (en)
JP (1) JP2013521249A (en)
CN (1) CN102781429A (en)
WO (1) WO2011107466A2 (en)

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1103252A1 (en) * 1998-07-21 2001-05-30 Liconsa, Liberacion Controlada de Sustancias Activas, S.A. Pharmaceutical oral preparation of a compound having an antifungic activity, and preparation method
WO2006037344A1 (en) * 2004-10-01 2006-04-13 Lifecycle Pharma A/S Pharmaceutical compositions comprising fenofibrate and atorvastatin
DE102005053066A1 (en) * 2005-11-04 2007-05-10 Basf Ag Use of copolymers as solubilizers for sparingly water-soluble compounds
WO2009013202A1 (en) * 2007-07-26 2009-01-29 Basf Se Process for preparing copolymers obtained by graft polymerization in solution and based on polyethers in solid form
WO2010017918A2 (en) * 2008-08-11 2010-02-18 Ratiopharm Gmbh Amorphous ambrisentan

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0415121A (en) 2003-10-10 2006-11-28 Lifecycle Pharma As particulate material, solid dosage form, method of manufacturing it, and use of a particulate material or solid dosage form

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1103252A1 (en) * 1998-07-21 2001-05-30 Liconsa, Liberacion Controlada de Sustancias Activas, S.A. Pharmaceutical oral preparation of a compound having an antifungic activity, and preparation method
WO2006037344A1 (en) * 2004-10-01 2006-04-13 Lifecycle Pharma A/S Pharmaceutical compositions comprising fenofibrate and atorvastatin
DE102005053066A1 (en) * 2005-11-04 2007-05-10 Basf Ag Use of copolymers as solubilizers for sparingly water-soluble compounds
WO2007051743A2 (en) * 2005-11-04 2007-05-10 Basf Se Use of a copolymer in the form of a solubiliser for a poorly water-soluble compound
WO2009013202A1 (en) * 2007-07-26 2009-01-29 Basf Se Process for preparing copolymers obtained by graft polymerization in solution and based on polyethers in solid form
WO2010017918A2 (en) * 2008-08-11 2010-02-18 Ratiopharm Gmbh Amorphous ambrisentan

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
LEUNER C ET AL: "Improving drug solubility for oral delivery using solid dispersions", EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, ELSEVIER SCIENCE PUBLISHERS B.V., AMSTERDAM, NL, vol. 50, no. 1, 3 July 2000 (2000-07-03), pages 47 - 60, XP004257179, ISSN: 0939-6411, DOI: DOI:10.1016/S0939-6411(00)00076-X *

Also Published As

Publication number Publication date
WO2011107466A2 (en) 2011-09-09
CN102781429A (en) 2012-11-14
JP2013521249A (en) 2013-06-10
EP2542222A2 (en) 2013-01-09

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