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公开(公告)号：US20190119451A1
公开(公告)日：2019-04-25
申请号：US16072673
申请日：2017-05-01
发明人： Oliver Petermann , Jin Zhao
摘要： An aqueous composition comprising a cellulose ether acetate being at least partially dissolved in an aqueous liquid is produced in a process, wherein an aqueous liquid is mixed with a cellulose ether acetate having a degree of substitution of acetyl groups, DSAc, of from 0.05 to 0.75 and the temperature of the mixture of the cellulose ether acetate and the aqueous liquid is set to less than 10 C to at least partially dissolve the cellulose ether acetate in the aqueous liquid.
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公开(公告)号：US20170173159A1
公开(公告)日：2017-06-22
申请号：US15129505
申请日：2015-03-03
发明人： Neal J. Fetner , David L. Malotky , Jin Zhao , Matthias Knarr , Michael J. Devon , Roland Adden
CPC分类号： A61K47/38 , A61J3/07 , A61K9/2866 , A61K9/4816 , C08B13/00 , C08L1/32
摘要： An aqueous composition useful for producing capsules shells comprises a) at least one dispersed esterified cellulose ether comprising (i) groups of the formula —C(O)—R—COOA or (ii) a combination of aliphatic monovalent acyl groups and 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, and b) from 0.05 to 20 percent of at least one salt of a fatty acid, based on the weight of the dispersed esterified cellulose ether, wherein the median particle size, d50, of the dispersed esterified cellulose ether particles is up to 7 micrometers, such median particle size (d50) being the size at which 50 mass percent of the particles have a smaller equivalent diameter and 50 mass percent have a larger equivalent diameter.
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公开(公告)号：US09649278B2
公开(公告)日：2017-05-16
申请号：US14350535
申请日：2012-10-09
发明人： Michael D. Read , Karen A. Coppens , Mark J. Hall , Jin Zhao
CPC分类号： A61K9/4816 , A61K9/4833 , A61K9/4883 , C08K5/0016 , C08K5/05 , C08L1/28 , C08L1/286 , C08L5/00
摘要： An injection-molded shell of a dosage form of good quality is producible by a) providing a composition comprising i) from 25 to 90 weight percent of ethylcellulose, ii) from 7.5 to 60 weight percent of a polysaccharide or polysaccharide derivative being different from ethylcellulose, and iii) from 2.5 to 50 weight percent of at least one component being different from polysaccharides and polysaccharide derivatives, based on the total weight of the composition, with the proviso that the composition comprises zero or not more than 10 weight percent of gelatin and zero or not more than 10 weight percent of a polymer comprising homo- or copolymerized acrylic acid, homo- or copolymerized methacrylic acid, a homo- or copolymerized acrylate or a homo- or copolymerized methacrylate, and b) subjecting the composition to shearing and heat to plasticize the composition and injection-molding the plasticized composition into a three-dimensional shell of a dosage form.
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公开(公告)号：US20150374823A1
公开(公告)日：2015-12-31
申请号：US14649721
申请日：2014-01-13
IPC分类号： A61K47/10 , A61K31/095 , A61K31/343 , A61K31/192 , A61K31/58
CPC分类号： A61K47/10 , A61K9/4866 , A61K31/095 , A61K31/10 , A61K31/192 , A61K31/343 , A61K31/58 , C08G65/20 , C08L71/02
摘要： The present invention relates to the use of polyalkoxylated alcohols of the formula R—O-(AO)—H, wherein R is a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, aralkyl or heterocyclic group having 7 to 25 carbon atoms, (AO) is a polyoxyalkylene moiety of the composition (BO)m(EO)n(DO)r with random or blockwise arrangement of the constituting oxyalkylene units, wherein m, n and r represent the average number of oxybutylene (BO) units, oxyethylene (EO) units and oxyalkylene units derived from at least one epoxide selected from styrene oxide and alkylene oxides having from 5 to 10 carbon atoms (DO) per molecule of the polyalkoxylated alcohol, respectively, m being a number greater than or equal to 1, n being a number greater than or equal to 1 and r being a number in the range from 0 to 50 under the proviso that (m+n+r) is less than or equal to 200 and the ratio n/(m+r) is in the range of 1 to 20, as excipients in pharmaceutical compositions. Said polyalkoxylated alcohols enable very effective solubilisation of poorly soluble active pharmaceutical ingredients in aqueous media. Solid or semi-solid pharmaceutical compositions comprising one or more such polyalkoxylated alcohol combined with at least one active pharmaceutical ingredient are further long term stable under typical storage conditions and can be readily provided in various dosage forms such as tablets and filled capsules.
摘要翻译： 本发明涉及式R-O-（AO）-H的聚烷氧基化醇的用途，其中R是具有7至25个碳原子的取代或未取代的烷基，烯基，炔基，芳基，芳烷基或杂环基，（ AO）是组成（BO）m（EO）n（DO）r的聚氧化烯部分，其具有构成的氧化烯单元的无规或阻塞排列，其中m，n和r表示氧丁烯（BO）单元的平均数，氧化乙烯 （EO）单元和衍生自至少一种选自氧化苯乙烯和每分子聚烷氧基化醇具有5至10个碳原子的氧化烯（DO）的环氧化物的氧化烯单元，m分别大于或等于1， n是大于或等于1的数，r是0至50的数，条件是（m + n + r）小于或等于200，并且比率n /（m + r） 在1至20的范围内，作为药物组合物中的赋形剂。 所述聚烷氧基化的醇使得难溶性活性药物成分在水性介质中非常有效地溶解。 包含一种或多种这样的多烷氧基化醇与至少一种活性药物成分组合的固体或半固体药物组合物在典型的储存条件下进一步长期稳定，并且可以容易地以各种剂型例如片剂和填充的胶囊提供。
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公开(公告)号：US10961355B2
公开(公告)日：2021-03-30
申请号：US16072673
申请日：2017-05-01
发明人： Oliver Petermann , Jin Zhao
摘要： An aqueous composition comprising a cellulose ether acetate being at least partially dissolved in an aqueous liquid is produced in a process, wherein an aqueous liquid is mixed with a cellulose ether acetate having a degree of substitution of acetyl groups, DSAc, of from 0.05 to 0.75 and the temperature of the mixture of the cellulose ether acetate and the aqueous liquid is set to less than 10 C to at least partially dissolve the cellulose ether acetate in the aqueous liquid.
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公开(公告)号：US20140271833A1
公开(公告)日：2014-09-18
申请号：US14350535
申请日：2012-10-09
发明人： Michael D. Read , Karen A. Coppens , Mark J. Hall , Jin Zhao
IPC分类号： A61K9/48
CPC分类号： A61K9/4816 , A61K9/4833 , A61K9/4883 , C08K5/0016 , C08K5/05 , C08L1/28 , C08L1/286 , C08L5/00
摘要： An injection-molded shell of a dosage form of good quality is producible by a) providing a composition comprising i) from 25 to 90 weight percent of ethylcellulose, ii) from 7.5 to 60 weight percent of a polysaccharide or polysaccharide derivative being different from ethylcellulose, and iii) from 2.5 to 50 weight percent of at least one component being different from polysaccharides and polysaccharide derivatives, based on the total weight of the composition, with the proviso that the composition comprises zero or not more than 10 weight percent of gelatin and zero or not more than 10 weight percent of a polymer comprising homo- or copolymerized acrylic acid, homo- or copolymerized methacrylic acid, a homo- or copolymerized acrylate or a homo- or copolymerized methacrylate, and b) subjecting the composition to shearing and heat to plasticize the composition and injection-molding the plasticized composition into a three-dimensional shell of a dosage form.
摘要翻译： 具有良好质量的剂型的注射成型的外壳可以通过以下方式生产：a）提供组合物，其包含i）25至90重量％的乙基纤维素，ii）7.5至60重量％的不同于乙基纤维素的多糖或多糖衍生物 ，和iii）基于组合物的总重量，2.5至50重量％的至少一种与多糖和多糖衍生物不同的组分，条件是组合物包含零或不大于10重量％的明胶和 0或不超过10重量％的包含均聚或共聚的丙烯酸，均聚或共聚的甲基丙烯酸，均聚或共聚的丙烯酸酯或均聚或共聚的甲基丙烯酸酯的聚合物的聚合物，和b）使组合物经受剪切和加热 塑化组合物并将增塑组合物注塑成剂型的三维壳体。
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公开(公告)号：US10450424B2
公开(公告)日：2019-10-22
申请号：US15746207
申请日：2016-07-08
发明人： Meinolf Brackhagen , Neal J. Fetner , Matthias Knarr , Jin Zhao
摘要： A process for producing an aqueous composition comprising a dispersed esterified cellulose ether comprises the steps of grinding, in the presence of an aqueous diluent an esterified cellulose ether comprising (i) groups of the formula —C(O)—R—COOA or (ii) a combination of aliphatic monovalent acyl groups and groups of the formula —C(O)—R—COOA, wherein R is a N divalent aliphatic or aromatic hydrocarbon group and A is hydrogen or a cation, blending a salt of a fatty acid with the esterified cellulose ether and choosing the amounts of aqueous diluent, esterified cellulose ether and salt of a fatty acid that the produced aqueous composition comprises at least 20 percent of the dispersed esterified cellulose ether and heating the aqueous composition to a temperature of from 37 to 80 C during or after the grinding step.
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公开(公告)号：US20180215880A1
公开(公告)日：2018-08-02
申请号：US15746207
申请日：2016-07-08
发明人： Meinolf Brackhagen , Neal J. Fetner , Matthias Knarr , Jin Zhao
IPC分类号： C08J3/07 , C09D101/32 , C08J3/12
摘要： A process for producing an aqueous composition comprising a dispersed esterified cellulose ether comprises the steps of grinding, in the presence of an aqueous diluent an esterified cellulose ether comprising (i) groups of the formula —C(O)—R—COOA or (ii) a combination of aliphatic monovalent acyl groups and groups of the formula —C(O)—R—COOA, wherein R is a N divalent aliphatic or aromatic hydrocarbon group and A is hydrogen or a cation, blending a salt of a fatty acid with the esterified cellulose ether and choosing the amounts of aqueous diluent, esterified cellulose ether and salt of a fatty acid that the produced aqueous composition comprises at least 20 percent of the dispersed esterified cellulose ether and heating the aqueous composition to a temperature of from 37 to 80 C during or after the grinding step.
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公开(公告)号：US09782356B2
公开(公告)日：2017-10-10
申请号：US15308767
申请日：2015-04-28
发明人： Jin Zhao , Roland Adden , Brian Koblinski , Robert L. Schmitt
CPC分类号： A61K9/4816 , B29C41/003 , B29C41/14 , B29C41/46 , B29K2001/12 , B29L2031/7174
摘要： A polymeric capsule shell of high quality is prepared from an aqueous composition which comprises (A) at least one esterified cellulose ether comprising aliphatic monovalent acyl groups and groups of the formula —C(O)—R—COOH, R being a divalent aliphatic or aromatic hydrocarbon group, wherein at least a part of the groups —C(O)—R—COOH are neutralized with an ammonium salt of carbonic acid, formic acid or acetic acid, and (B) from 0 to 7 weight percent of a non-polymeric plasticizer, based on the weight of the esterified cellulose ether, wherein the weight of said at least one esterified cellulose ether is at least 80 percent of the total polymer weight in the aqueous composition.
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公开(公告)号：US20170181977A1
公开(公告)日：2017-06-29
申请号：US15308792
申请日：2015-04-28
发明人： Jin Zhao , Roland Adden , Neal J. Fetner , David L. Malotky
CPC分类号： A61K9/4816 , B29C41/14
摘要： An aqueous composition comprising at least 10 weight percent of a dispersed esterified cellulose ether, based on the total weight of the aqueous composition, wherein the esterified cellulose ether comprises (i) groups of the formula —C(O)—R—COOH or (ii) a combination of aliphatic monovalent acyl groups and groups of the formula —C(O)—R—COOH, R being a divalent aliphatic or aromatic hydrocarbon group, and at least a part of the groups —C(O)—R—COOH are neutralized with an ammonium salt of carbonic acid, formic acid or acetic acid, and wherein d90 of the dispersed esterified cellulose ether particles is up to 10 micrometers, d90 being the diameter where 90 mass percent of the particles have a smaller equivalent diameter and the other 10 mass percent have a larger equivalent diameter, is useful for preparing coating dosage forms including tablets, capsules and others, or for the formation of capsules shells.
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