公开(公告)号：EP1368007A1

公开(公告)日：2003-12-10

申请号：EP01913827.0

申请日：2001-02-27

申请人： Röhm GmbH & Co. KG

发明人： PETEREIT, Hans-Ulrich ,  MEIER, Christian ,  ROTH, Erna

IPC分类号： A61K9/28

CPC分类号： A61K9/282 ,  A61K9/2846 ,  A61K47/10 ,  A61K47/12 ,  A61K47/20 ,  A61K47/32

摘要： The invention relates to a method for the production of a coating or binding agent for oral or dermal pharmaceutical dosage forms, comprising essentially (a) a copolymer consisting of radically polymerized C1-to C4 esters of acrylic or methacrylic acids and additional (meth)acrylate monomers having functional tertiary ammonium groups, wherein the copolymer is contained in the form of a powder with an average particle size of 1-40 νm; (b) 3 to 15 percent by weight in relation to (a) of an emulsifier with an HLB value of less than 14 and (c) 5 to 50 percent by weight in relation to (a) of a C12- to C18-monocarboxylic acid or a C12- to C18-hydroxyl compound, wherein components (a), (b) and (c) are mingled or mixed adding or not water and optionally adding a pharmaceutical active ingredient and other common additives. The coating or binding agent is produced from the mixture by melting, pouring, spreading or spraying. The invention also relates to the coating or binding agent itself.

公开(公告)号：EP1587497A1

公开(公告)日：2005-10-26

申请号：EP03767591.5

申请日：2003-11-21

申请人： Röhm GmbH & Co. KG

发明人： PETEREIT, Hans-Ulrich ,  MEIER, Christian ,  GRYCZKE, Andreas

IPC分类号： A61K9/14

CPC分类号： A61J3/10 ,  A61K9/0056 ,  A61K9/146 ,  A61K9/1647 ,  A61K9/2054 ,  A61K31/192

摘要： The invention relates to a method for producing an oral form of administration which decomposes immediately and releases active ingredients in the mouth. According to said method, (a) an anionic pharmaceutical active ingredient is intensively mixed with (b) a copolymer consisting of radically polymerised C1-C4 esters of the acrylic acid or methacrylic acid and other (meth)acrylate monomers containing functional tertiary amino groups, and (c) between 5 and 50 wt. %, in relation to (b), of a C12-C22 carboxylic acid in the melted mass; the mixture is solidified and ground to form a powder containing active ingredients having an average particle size of 200 µm or less; and the powder is encapsulated in a water-soluble matrix consisting of pharmaceutically standard adjuvants, on the condition that no more than 3 wt. %, in relation to the copolymer, of emulsifiers with an HLB value of at least 14 must be contained therein. The invention also relates to the powder containing active ingredients and the uses of the same.

公开(公告)号：EP1478344A2

公开(公告)日：2004-11-24

申请号：EP03742925.5

申请日：2003-01-30

申请人： Röhm GmbH & Co. KG

发明人： PETEREIT, Hans-Ulrich ,  MEIER, Christian ,  GRYCZKE, Andreas

IPC分类号： A61K9/16

CPC分类号： A61K9/2027 ,  A61K9/1694

摘要： The invention relates to a method for producing active ingredient-containing granules or powders involving the following steps: a) melting a mixture consisting of a pharmaceutical active ingredient and of a (meth)acrylate copolymer, which is comprised of 40 to 75 wt. % of radically polymerized C1 to C4 alkyl esters of acrylic acid or of methacrylic acid and can be comprised of 25 to 60 wt. % (meth)acrylate monomers having an anionic group in the alkyl radial; b) extruding the mixture, and; c) comminuting the extrudate to form a granule or powder. The inventive method is characterized in that the active ingredient is the salt of an alkaline substance, and in that the pH value, which can be measured on the obtained powder or granule, is equal to or less than pH 7.0. The invention also relates to pharmaceutical dosage forms or precursors thereof, which can be produced using the inventive method.

公开(公告)号：EP1432409A1

公开(公告)日：2004-06-30

申请号：EP03790791.2

申请日：2003-07-08

申请人： Röhm GmbH & Co. KG

发明人： PETEREIT, Hans-Ulrich ,  MEIER, Christian ,  ROTH, Erna ,  GRYCZKE, Andreas

IPC分类号： A61K9/28 ,  A61K9/50 ,  A61K9/16

CPC分类号： A61K9/1694 ,  A61K9/1635 ,  A61K9/1682 ,  A61K9/2846 ,  A61K9/5026

摘要： The invention relates to a method for producing a granulate or powder which is suitable as a coating and binding agent for oral and dermal medicaments, cosmetic products or food supplements and substantially consists of (a) a copolymer containing radically polymerized C1 to C4 esters of acrylic acid or methacrylic acid and additional (meth)acrylate monomers that comprise functional tertiary amino groups, (b) 3 to 25 percent by weight relative to (a) of an emulsifier having an HLB value of at least 14, and (c) 5 to 50 percent by weight relative to (a) of C12 to C18 monocarboxylic acid or a C12 to C18 hydroxyl compound. Components (a), (b), and (c) are simultaneously or successively blended or mixed by optionally adding a pharmaceutical agent and/or other common loading agents, melted and mixed in a heatable mixer, whereupon the melted product is cooled and comminuted into a granulate or powder.

公开(公告)号：EP1053258B8

公开(公告)日：2008-08-27

申请号：EP99904837.4

申请日：1999-02-01

申请人： Röhm GmbH & Co. KG

发明人： MEIER, Christian ,  SÜFKE, Thomas ,  PETEREIT, Hans-Ulrich ,  RECKTENWALD, Roger ,  BOLLER, Thomas

IPC分类号： C08F2/18 ,  C08F220/56 ,  C08F220/00 ,  C08F220/32 ,  C12N11/08

CPC分类号： C07K17/08 ,  C08F2/32 ,  C12N11/08 ,  Y10S435/803 ,  Y10S435/815 ,  Y10S530/815

摘要： The invention relates to a method for producing a bead-shaped, cross-linked hydrophilic mixed polymer which actively bonds with ligands with nucleophilic groups, by inversely bead-polymerising a monomer phase. The invention also relates to polymer support materials with a high capacity for bonding with penicillin acylase and with a lower swelling number, and to their use.

公开(公告)号：EP1053258B1

公开(公告)日：2003-04-09

申请号：EP99904837.4

申请日：1999-02-01

申请人： Röhm GmbH & Co. KG

发明人： MEIER, Christian ,  SÜFKE, Thomas ,  PETEREIT, Hans-Ulrich ,  RECKTENWALD, Roger

IPC分类号： C08F2/18 ,  C08F220/56 ,  C08F220/00 ,  C08F220/32 ,  C12N11/08

CPC分类号： C07K17/08 ,  C08F2/32 ,  C12N11/08 ,  Y10S435/803 ,  Y10S435/815 ,  Y10S530/815

摘要： The invention relates to a method for producing a bead-shaped, cross-linked hydrophilic mixed polymer which actively bonds with ligands with nucleophilic groups, by inversely bead-polymerising a monomer phase. The invention also relates to polymer support materials with a high capacity for bonding with penicillin acylase and with a lower swelling number, and to their use.

公开(公告)号：EP1098935B1

公开(公告)日：2003-01-02

申请号：EP99931245.7

申请日：1999-07-02

申请人： Röhm GmbH & Co. KG

发明人： PETEREIT, Hans-Ulrich ,  MEIER, Christian ,  ROTH, Erna

IPC分类号： C08L33/08 ,  C08L33/10 ,  A61K9/28 ,  A61K47/32 ,  A61K9/70

CPC分类号： A61K9/2846 ,  Y10S524/904

摘要： The invention relates to a method for the production of a coating and excipient agent for oral or dermal dosage forms, consisting of (a) 35-98 % by weight of a copolymer consisting of radically polymerized C1-C4 esters of acrylic or methacrylic acid and additional (meth)acrylate monomers having functional tertiary ammonium groups and (b) 1-50 % by weight of a softener and 1-15 % by weight of an emulgator with an HLB value of less than 14, wherein constituents (a), (b) and (c) are mixed with or without adding water and optionally adding a pharmaceutical active substance and other conventional additives and the coating and excipient agent is produced by melting, casting, spreading or spraying. The invention is characterized in that the copolymer (a) is applied in powder form with a mean particle size of 1-40 mu m.