BRPI1010550A8 - formas de dosagem, e, processo para a produção de preparações para formas de dosagem de substâncias ativas fracamente solúveis em água - Google Patents

formas de dosagem, e, processo para a produção de preparações para formas de dosagem de substâncias ativas fracamente solúveis em água Download PDF

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Publication number
BRPI1010550A8
BRPI1010550A8 BRPI1010550A BRPI1010550A BRPI1010550A8 BR PI1010550 A8 BRPI1010550 A8 BR PI1010550A8 BR PI1010550 A BRPI1010550 A BR PI1010550A BR PI1010550 A BRPI1010550 A BR PI1010550A BR PI1010550 A8 BRPI1010550 A8 BR PI1010550A8
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BR
Brazil
Prior art keywords
dosage forms
poorly water
active substances
weight
soluble
Prior art date
Application number
BRPI1010550A
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English (en)
Inventor
Djuric Dejan
Kolter Karl
Fischer Stefan
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.)
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Publication date
Application filed by Basf Se filed Critical Basf Se
Publication of BRPI1010550A2 publication Critical patent/BRPI1010550A2/pt
Publication of BRPI1010550A8 publication Critical patent/BRPI1010550A8/pt
Publication of BRPI1010550B1 publication Critical patent/BRPI1010550B1/pt

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    • 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
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38—Cellulose; Derivatives thereof
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/216—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/4164—1,3-Diazoles
    • 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
    • A61K31/4425—Pyridinium derivatives, e.g. pralidoxime, pyridostigmine
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/451—Non condensed piperidines, e.g. piperocaine having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
    • 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
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/54—Heterocyclic 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
    • A61K31/5415—Heterocyclic 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
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K31/63—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
    • A61K31/635—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide having a heterocyclic ring, e.g. sulfadiazine
    • 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
    • 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
    • A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
    • 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
    • A61K9/2027—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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08F—MACROMOLECULAR COMPOUNDS OBTAINED BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
    • C08F283/00—Macromolecular compounds obtained by polymerising monomers on to polymers provided for in subclass C08G
    • C08F283/06—Macromolecular compounds obtained by polymerising monomers on to polymers provided for in subclass C08G on to polyethers, polyoxymethylenes or polyacetals

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Inorganic Chemistry (AREA)
  • Polymers & Plastics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Emergency Medicine (AREA)
  • Organic Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Medicinal Preparation (AREA)
  • Graft Or Block Polymers (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

formas de dosagem, e, processo para a produção de preparações para formas de dosagem de substâncias ativas fracamente solúveis em água a invenção refere-se a formas de dosagem, que contêm preparações de substâncias fracamente solúveis em água em uma matriz de polímero de copolímeros de poliéster, os referidos copolímeros de poliéter sendo obtidos através de polimerização iniciada por radical de uma mistura de 30 a 80%, em peso, de n-vinillactama, de 10 a 50%, em peso, de acetato de vinila e de 1 o a 50%, em peso de um poliéter, e pelo menos um polímero fracamente solúvel em água, a substância fracamente solúvel em água estando presente na matriz do polímero como uma substância amorfa.
BRPI1010550-6A 2009-05-13 2010-05-11 formas de dosagem, e, processo para a produção de preparações para formas de dosagem de substâncias ativas fracamente solúveis em água BRPI1010550B1 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP09160129 2009-05-13
PCT/EP2010/056447 WO2010130728A2 (de) 2009-05-13 2010-05-11 Feste pharmazeutischen zubereitungen enthaltend copolymere auf basis von polyethern in kombination mit wasserschwerlöslichen polymeren

Publications (3)

Publication Number Publication Date
BRPI1010550A2 BRPI1010550A2 (pt) 2016-03-15
BRPI1010550A8 true BRPI1010550A8 (pt) 2019-09-03
BRPI1010550B1 BRPI1010550B1 (pt) 2019-11-05

Family

ID=42262240

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI1010550-6A BRPI1010550B1 (pt) 2009-05-13 2010-05-11 formas de dosagem, e, processo para a produção de preparações para formas de dosagem de substâncias ativas fracamente solúveis em água

Country Status (6)

Country Link
US (2) US9555002B2 (pt)
EP (1) EP2429492B1 (pt)
JP (1) JP5654002B2 (pt)
CN (1) CN102458368B (pt)
BR (1) BRPI1010550B1 (pt)
WO (1) WO2010130728A2 (pt)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2429492B1 (de) 2009-05-13 2014-06-25 Basf Se Feste pharmazeutische Zubereitungen enthaltend Copolymere auf Basis von Polyethern in Kombination mit wasserschwerlöslichen Polymeren
US8951569B2 (en) 2009-09-17 2015-02-10 Basf Se Pellets coated with coatings containing active substances
US20120202894A1 (en) 2009-09-18 2012-08-09 Basf Se Rapidly Soluble Solid Pharmaceutical Preparations Containing Amphiphilic Copolymers Based On Polyethers In Combination With Hydrophilic Polymers
JP2013505211A (ja) * 2009-09-18 2013-02-14 ビーエーエスエフ ソシエタス・ヨーロピア 界面活性剤と組み合わせたポリエーテルに基づく両親媒性コポリマーを含む固体医薬製剤
US8636929B2 (en) 2010-05-21 2014-01-28 Basf Se Nanoporous foamed active compound-containing preparations based on pharmaceutically acceptable thermoplastically workable polymers
US8715729B2 (en) 2010-12-22 2014-05-06 Basf Se Rapidly disintegrating, solid coated dosage form
JP5903686B2 (ja) * 2010-12-23 2016-04-13 アッヴィ・ドイチュラント・ゲー・エム・ベー・ハー・ウント・コー・カー・ゲー 固体分散物を基にした固体徐放製剤
CA2846446A1 (en) * 2011-08-30 2013-03-07 Universiteit Gent Multi-layered release formulation
EP2572731A1 (en) * 2011-09-26 2013-03-27 Abbott GmbH & Co. KG Formulations based on solid dispersions
US20160193151A1 (en) * 2015-01-06 2016-07-07 Maria Del Pilar Noriega Escobar Dosage form incorporating an amorphous drug solid solution
GB201502073D0 (en) * 2015-02-09 2015-03-25 Cubic Pharmaceuticals Ltd And Delta Pharmaceuticals Ltd HDEG technology
CA3073195A1 (en) 2017-08-15 2019-02-21 Nephron Pharmaceuticals Corporation Aqueous nebulization composition
WO2019063478A1 (en) * 2017-09-26 2019-04-04 Capsugel Belgium Nv SUB-MICRONIC PARTICLE FORMULATIONS
CN108623744B (zh) * 2018-06-01 2020-12-15 辽宁奥克医药辅料股份有限公司 共聚物、增溶剂及制备方法
CN111840231B (zh) * 2020-06-24 2022-10-11 浙江工业大学 一种吡罗昔康纳米晶的制备方法

Family Cites Families (17)

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Publication number Priority date Publication date Assignee Title
DE19719187A1 (de) 1997-05-07 1998-11-12 Basf Ag Verwendung von Copolymerisaten des N-Vinyl-pyrrolidons in Zubereitungen wasserunlöslicher Stoffe
DE19811919A1 (de) 1998-03-18 1999-09-23 Basf Ag Verwendung von Copolymerisaten monoethylenisch ungesättigter Carbonsäuren als Solubilisatoren
DE19814739A1 (de) 1998-04-02 1999-10-07 Basf Ag Verwendung von Polyalkylenoxid-haltigen Pfropfpolymerisaten als Solubilisatoren
JP4533531B2 (ja) * 1998-04-03 2010-09-01 ビーエム リサーチ エイ／エス 制御放出組成物
DE19935063A1 (de) 1999-07-28 2001-02-01 Basf Ag Pfropfpolymerisate als Gashydratinhibitoren
CA2551254A1 (en) 2003-12-31 2005-07-21 Pfizer Products Inc. Stabilized pharmaceutical solid compositions of low-solubility drugs, poloxamers, and stabilizing polymers
DE102005026755A1 (de) * 2005-06-09 2006-12-14 Basf Ag Herstellung von festen Lösungen schwerlöslicher Wirkstoffe durch Kurzzeitüberhitzung und schnelle Trocknung
DE102005053066A1 (de) * 2005-11-04 2007-05-10 Basf Ag Verwendung von Copolymeren als Solubilisatoren für in Wasser schwerlöslichen Verbindungen
CA2597740C (en) * 2006-04-26 2012-10-16 Supernus Pharmaceuticals, Inc. Modified-release preparations containing oxcarbazepine and derivatives thereof
CA2673111A1 (en) * 2006-12-07 2008-06-19 Schering Corporation Ph sensitive matrix formulation
US20100204425A1 (en) 2007-07-26 2010-08-12 Basf Se Process for preparing copolymers obtained by graft polymerization in solution and based on polyethers in solid form
US20100280047A1 (en) 2007-12-12 2010-11-04 Basf Se Salts of active ingredients with polymeric counter-ions
US20110178183A1 (en) 2008-09-25 2011-07-21 Meyer-Boehm Kathrin Use Of Polyether-Based And Vinyl Monomer-Based Copolymers As Binders For Dosing Forms Comprising Solid Active Ingredients
WO2010040686A1 (de) 2008-10-07 2010-04-15 Basf Se Verfahren zur herstellung oraler darreichungsformen mit kontrollierter freisetzung
WO2010072573A1 (de) 2008-12-23 2010-07-01 Basf Se Verwendung von copolymeren auf basis von polyethern und vinylmonomeren als stabilisierungsmittel für emulsionen
EP2413907B1 (de) 2009-03-31 2014-10-01 Basf Se Verfahren zur herstellung von zubereitungen von in wasser schwerlöslichen substanzen
EP2429492B1 (de) 2009-05-13 2014-06-25 Basf Se Feste pharmazeutische Zubereitungen enthaltend Copolymere auf Basis von Polyethern in Kombination mit wasserschwerlöslichen Polymeren

Also Published As

Publication number Publication date
BRPI1010550A2 (pt) 2016-03-15
US20120053248A1 (en) 2012-03-01
US10328150B2 (en) 2019-06-25
EP2429492A2 (de) 2012-03-21
CN102458368A (zh) 2012-05-16
JP2012526765A (ja) 2012-11-01
EP2429492B1 (de) 2014-06-25
JP5654002B2 (ja) 2015-01-14
CN102458368B (zh) 2014-02-26
US20170072059A1 (en) 2017-03-16
US9555002B2 (en) 2017-01-31
BRPI1010550B1 (pt) 2019-11-05
WO2010130728A2 (de) 2010-11-18
WO2010130728A3 (de) 2011-04-07

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