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1.发明公开COPOLYMERS AS EXCIPIENTS FOR EFFECTIVE SOLUBILIZATION OF POORLY WATER-SOLUBLE SUBSTANCES FROM SOLID MIXTURES 审中-公开共聚物作为有效溶解固体混合物中水溶性差的物质的助剂
公开(公告)号：EP3265062A1
公开(公告)日：2018-01-10
申请号：EP16719554.4
申请日：2016-02-24
发明人： TALE, Swapnil , REINEKE, Theresa M. , BATES, Frank S. , TING, Jeffrey M. , WIDANAPATHIRANA, Lakmini , GUILLAUDEU, Steven J. , GUO, Li
IPC分类号： A61K9/20
CPC分类号： C08F220/56 , A61K9/1635 , A61K9/2027 , C08F220/54 , C08F226/10
摘要： The present invention relates to the use of uncrosslinked copolymers having a backbone comprising i) a plurality of thermo-responsive structural units derived from one or more than one N-alkyl or N,N-dialkyl substituted (alkyl)acrylamide monomer and ii) a plurality of hydrophilic structural units derived from one or more than one second ethylenically unsaturated monomer as excipients in solid mixtures with poorly water-soluble substances for effective solubilization of the latter in aqueous media. Solid dosage forms comprising a solid mixture of such copolymer(s) and poorly water-soluble substance(s) are also within the scope of the invention.
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公开(公告)号：EP3265062B1
公开(公告)日：2019-05-22
申请号：EP16719554.4
申请日：2016-02-24
发明人： TALE, Swapnil , REINEKE, Theresa M. , BATES, Frank S. , TING, Jeffrey M. , WIDANAPATHIRANA, Lakmini , GUILLAUDEU, Steven J. , GUO, Li
IPC分类号： A61K9/16 , C08F220/54 , C08F220/56 , C08F226/10 , C08F301/00 , C08F238/00 , C08F220/00 , C08F138/00 , C08F120/00 , C08F38/00 , C08F20/00 , A61K9/20
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公开(公告)号：EP2997046A1
公开(公告)日：2016-03-23
申请号：EP14731443.9
申请日：2014-05-07
CPC分类号： C08B13/00 , A61K9/146 , A61K31/095 , A61K31/4166 , A61K47/38
摘要： Esterified cellulose ethers comprising groups of formula —C(O)—CHR′—CHR″—COOA, wherein, R′ and R″ are hydrogen or (—S)m(—R1)n-R2, wherein R1 is a hydrocarbon group having 1 to 4 carbon atoms, R2 is an optionally substituted 5- or 6-membered cyclic group, m and n each independently are 0 or 1, and A is hydrogen or a cation, with the proviso that in each group CHR′—CHR″ one of R′ and R″ is hydrogen and the other one is (—S)m(—R1)n-R2, are useful as excipients for maintaining the concentration of poorly water-soluble drugs in aqueous liquids at supersaturation levels.
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公开(公告)号：EP2964678B1
公开(公告)日：2018-04-04
申请号：EP14713634.5
申请日：2014-02-28
发明人： BRACKHAGEN, Meinolf , GUILLAUDEU, Steven J. , GRASMAN, Nicholas S. , PETERMANN, Oliver , SCHMITT, Robert L. , SPREHE, Matthias
CPC分类号： A61K47/38 , A61K9/2866 , A61K9/4891 , C08B13/00
摘要： Esterified cellulose ethers which comprise (i) aliphatic monovalent acyl groups or (ii) groups of the formula —C(O)—R—COOA, wherein R is a divalent aliphatic or aromatic hydrocarbon group and A is hydrogen or a cation, or (iii) a combination of aliphatic monovalent acyl groups and groups of the formula —C(O)—R—COOA, which have a viscosity of up to 2.33 mPa·s, measured as a 2.0 wt % solution of the esterified cellulose ether in 0.43 wt % aqueous NaOH at 20° C., and which have a viscosity of up to 13 mPao·s, measured as a 10 wt % solution of the esterified cellulose ether in acetone at 20° C. are useful for preparing solid dispersions comprising drugs.
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5.发明公开
公开(公告)号：EP2874607A1
公开(公告)日：2015-05-27
申请号：EP13740163.4
申请日：2013-07-12
发明人： GRASMAN, Nicholas S. , GUILLAUDEU, Steven J. , HALL, Mark, J. , SHRESTHA, Uma , ROSE, Maureen L. , PORTER, William W. , SPAULDING, Wesley J. , O'DONNELL, Kevin P. , ROGERS, True L.
IPC分类号： A61K9/14 , A61K9/16 , A61K31/343 , A61K31/415 , A61K31/58
CPC分类号： A61K47/38 , A61K9/146 , A61K9/1652 , A61K9/4891 , A61K31/343 , A61K31/4166 , A61K31/58
摘要： A solid dispersion comprising at least one active ingredient in at least one hydroxyalkyl methylcellulose having a DS of from 1.0 to 2.7 and an MS of from 0.40 to 1.30, wherein DS is the degree of substitution of methoxyl groups and MS is the molar substitution of hydroxyalkoxyl groups, can be produced by extrusion or spray-drying.
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6.发明授权SOLID DISPERSION COMPRISING A HIGHLY SUBSTITUTED HYDROXYALKYL METHYLCELLULOSE 有权FESTE散剂麻醉剂HOCHSUBSTITERERTER羟丙基甲基纤维素
公开(公告)号：EP2874607B1
公开(公告)日：2017-05-31
申请号：EP13740163.4
申请日：2013-07-12
发明人： GRASMAN, Nicholas S. , GUILLAUDEU, Steven J. , HALL, Mark, J. , SHRESTHA, Uma , ROSE, Maureen L. , PORTER, William W. , SPAULDING, Wesley J. , O'DONNELL, Kevin P. , ROGERS, True L.
IPC分类号： A61K9/14 , A61K9/16 , A61K31/343 , A61K31/4166 , A61K31/58 , A61K9/48 , A61K47/38
CPC分类号： A61K47/38 , A61K9/146 , A61K9/1652 , A61K9/4891 , A61K31/343 , A61K31/4166 , A61K31/58
摘要： A solid dispersion comprising at least one active ingredient in at least one hydroxyalkyl methylcellulose having a DS of from 1.0 to 2.7 and an MS of from 0.40 to 1.30, wherein DS is the degree of substitution of methoxyl groups and MS is the molar substitution of hydroxyalkoxyl groups, can be produced by extrusion or spray-drying.
摘要翻译： 在至少一种羟烷基甲基纤维素中的至少一种羟烷基甲基纤维素中含有至少一种活性成分的固体分散体，DS为1.0至2.7，MS为0.40至1.30，其中DS为甲氧基的取代度，MS为羟基烷氧基 组，可以通过挤出或喷雾干燥来生产。
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7.发明公开
公开(公告)号：EP2964678A1
公开(公告)日：2016-01-13
申请号：EP14713634.5
申请日：2014-02-28
发明人： BRACKHAGEN, Meinolf , GUILLAUDEU, Steven J. , GRASMAN, Nicholas S. , PETERMANN, Oliver , SCHMITT, Robert L. , SPREHE, Matthias
CPC分类号： A61K47/38 , A61K9/2866 , A61K9/4891 , C08B13/00
摘要： Esterified cellulose ethers which comprise (i) aliphatic monovalent acyl groups or (ii) groups of the formula —C(O)—R—COOA, wherein R is a divalent aliphatic or aromatic hydrocarbon group and A is hydrogen or a cation, or (iii) a combination of aliphatic monovalent acyl groups and groups of the formula —C(O)—R—COOA, which have a viscosity of up to 2.33 mPa·s, measured as a 2.0 wt % solution of the esterified cellulose ether in 0.43 wt % aqueous NaOH at 20° C., and which have a viscosity of up to 13 mPao·s, measured as a 10 wt % solution of the esterified cellulose ether in acetone at 20° C. are useful for preparing solid dispersions comprising drugs.
摘要翻译： 酯化纤维素醚，其包含（i）脂族一价酰基或（ii）式-C（O）-R-COOA的基团，其中R是二价脂族或芳族烃基，A是氢或阳离子，或（ iii）脂族一价酰基和式-C（O）-R-COOA基团的组合，其粘度高达2.33mPa·s，以2.0重量％的酯化纤维素醚溶液测量为0.43 在20℃下的wt％NaOH水溶液，其粘度高达13mPao·s，以20wt％的酯化纤维素醚在丙酮中的10wt％溶液测量，可用于制备包含药物的固体分散体 。
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