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1.发明授权公开(公告)号：US06955821B2
公开(公告)日：2005-10-18
申请号：US10121706
申请日：2002-04-15
IPC分类号： A61K9/20 , A61K9/22 , A61K9/24 , A61K9/50 , A61K9/52 , A61K9/58 , A61K31/09 , A61K31/137 , A61K31/485 , A61K31/495 , A61K47/04 , A61K47/08 , A61K47/12 , A61K47/18 , A61K47/20 , A61K47/26 , A61K47/30 , A61K47/32 , A61K47/34 , A61K47/36 , A61K47/38 , A61K47/44 , A61P11/10 , A61K9/26 , A61K9/48
CPC分类号： A61K9/5084 , A61K9/2027 , A61K9/2054 , A61K9/209 , A61K31/09 , A61K31/137 , A61K31/485 , A61K31/495 , A61K2300/00
摘要： The invention relates to a novel pharmaceutical sustained release formulation of guaifenesin and at least one additional drug ingredient. The formulation may comprise a hydrophilic polymer, preferably a hydroxypropyl methylcellulose, and a water-insoluble polymer, preferably an acrylic resin, in a ratio range of about one-to-one (1:1) to about nine-to-one (9:1), more preferably a range of about three-to-two (3:2) to about six-to-one (6:1), and most preferably in a range of about two-to-one (2:1) to about four-to-one (4:1) by weight. This formulation capable of providing therapeutically effective bioavailability of guaifenesin for at least twelve hours after dosing in a human subject. The invention also relates to a modified release product which has two portions: a first portion having an immediate release formulation of guaifenesin and a second portion having a sustained release formulation of guaifenesin, wherein one or both portions has at least one additional drug ingredient. The modified release product has a maximum guaifenesin serum concentration equivalent to that of an immediate release guaifenesin tablet, and is capable of providing therapeutically effective bioavailability of guaifenesin for at least twelve hours after dosing in a human subject.
摘要翻译： 本发明涉及愈创甘油醚和至少一种另外的药物成分的新型药物缓释制剂。 制剂可包含亲水性聚合物，优选羟丙基甲基纤维素和水不溶性聚合物，优选丙烯酸树脂，其比例范围为约一对一（1：1）至约九对一（9 ：1），更优选约三至二（3:2）至约六对一（6:1）的范围，最优选在约二至一（2:1）的范围内 ）至约四对一（4:1）重量比。 该制剂能够在给予人受试者后至少十二个小时提供愈创甘油的治疗有效的生物利用度。 本发明还涉及一种具有两部分的改性释放产物：第一部分具有愈创甘油醚的立即释放制剂，第二部分具有愈创甘油醚的缓释制剂，其中一个或两个部分具有至少一种另外的药物成分。 改性释放产物具有与立即释放愈创甘油醚片剂相当的最大愈创甘油醚血清浓度，并且能够在给予人受试者后至少十二个小时提供愈创甘油醚治疗有效的生物利用度。
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公开(公告)号：US08012504B2
公开(公告)日：2011-09-06
申请号：US10413530
申请日：2003-04-15
IPC分类号： A61K9/22
CPC分类号： A61K9/2027 , A61K9/2054 , A61K9/209 , A61K9/5084 , A61K31/09 , A61K31/137 , A61K31/485 , A61K31/495 , A61K2300/00
摘要： The invention relates to a novel pharmaceutical modified release formulation of guaifenesin and dextromethorphan. The formulation may comprise a hydrophilic polymer, preferably a hydroxypropyl methylcellulose, and a water-insoluble polymer, preferably an acrylic resin, in a ratio range of about one-to-one (1:1) to about nine-to-one (9:1), more preferably a range of about three-to-two (3:2) to about six-to-one (6:1), and most preferably in a range of about two-to-one (2:1) to about four-to-one (4:1) by weight. This formulation capable of providing therapeutically effective bioavailability of guaifenesin for at least twelve hours after dosing in a human subject. The invention also relates to a modified release product which has two portions: a first portion having an immediate release formulation of guaifenesin and a second portion having a sustained release formulation of guaifenesin, wherein one or both portions further comprises dextromethorphan. The modified release product has a maximum guaifenesin serum concentration equivalent to that of an immediate release guaifenesin tablet, and is capable of providing therapeutically effective bioavailability of guaifenesin for at least twelve hours after dosing in a human subject.
摘要翻译： 本发明涉及愈创甘油醚和右美沙芬的新型药物改良释放制剂。 制剂可包含亲水性聚合物，优选羟丙基甲基纤维素和水不溶性聚合物，优选丙烯酸树脂，其比例范围为约一对一（1：1）至约九对一（9 ：1），更优选约三至二（3:2）至约六对一（6:1）的范围，最优选在约二至一（2:1）的范围内 ）至约四对一（4:1）重量比。 该制剂能够在给予人受试者后至少十二个小时提供愈创甘油的治疗有效的生物利用度。 本发明还涉及一种具有两部分的改性释放产物：第一部分具有愈创甘油醚的立即释放制剂，第二部分具有愈创甘油醚的持续释放制剂，其中一个或两个部分还包含右美沙芬。 改性释放产物具有与立即释放愈创甘油醚片剂相当的最大愈创甘油醚血清浓度，并且能够在给予人受试者后至少十二个小时提供愈创甘油的治疗有效的生物利用度。
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3.发明授权公开(公告)号：US07985421B2
公开(公告)日：2011-07-26
申请号：US11158012
申请日：2005-06-22
IPC分类号： A61K9/22
CPC分类号： A61K9/5084 , A61K9/2027 , A61K9/2054 , A61K9/209 , A61K31/09 , A61K31/137 , A61K31/485 , A61K31/495 , A61K2300/00
摘要： The invention relates to a novel pharmaceutical sustained release formulation of guaifenesin and at least one additional drug ingredient. The formulation may comprise a hydrophilic polymer, preferably a hydroxypropyl methylcellulose, and a water-insoluble polymer, preferably an acrylic resin, in a ratio range of about one-to-one (1:1) to about nine-to-one (9:1), more preferably a range of about three-to-two (3:2) to about six-to-one (6:1), and most preferably in a range of about two-to-one (2:1) to about four-to-one (4:1) by weight. This formulation capable of providing therapeutically effective bioavailability of guaifenesin for at least twelve hours after dosing in a human subject. The invention also relates to a modified release product which has two portions: a first portion having an immediate release formulation of guaifenesin and a second portion having a sustained release formulation of guaifenesin, wherein one or both portions has at least one additional drug ingredient. The modified release product has a maximum guaifenesin serum concentration equivalent to that of an immediate release guaifenesin tablet, and is capable of providing therapeutically effective bioavailability of guaifenesin for at least twelve hours after dosing in a human subject.
摘要翻译： 本发明涉及愈创甘油醚和至少一种另外的药物成分的新型药物缓释制剂。 制剂可包含亲水性聚合物，优选羟丙基甲基纤维素和水不溶性聚合物，优选丙烯酸树脂，其比例范围为约一对一（1：1）至约九对一（9 ：1），更优选约三至二（3:2）至约六对一（6:1）的范围，最优选在约二至一（2:1）的范围内 ）至约四对一（4:1）重量比。 该制剂能够在给予人受试者后至少十二个小时提供愈创甘油的治疗有效的生物利用度。 本发明还涉及一种具有两部分的改性释放产物：第一部分具有愈创甘油醚的立即释放制剂，第二部分具有愈创甘油醚的缓释制剂，其中一个或两个部分具有至少一种另外的药物成分。 改性释放产物具有与立即释放愈创甘油醚片剂相当的最大愈创甘油醚血清浓度，并且能够在给予人受试者后至少十二个小时提供愈创甘油的治疗有效的生物利用度。
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公开(公告)号：US07985420B2
公开(公告)日：2011-07-26
申请号：US10406574
申请日：2003-04-04
IPC分类号： A61K9/22
CPC分类号： A61K9/2027 , A61K9/2054 , A61K9/209 , A61K9/5084 , A61K31/09 , A61K31/137 , A61K31/485 , A61K31/495 , A61K2300/00
摘要： The invention relates to a novel pharmaceutical sustained release formulation of guaifenesin and pseudoephedrine. The formulation may comprise a hydrophilic polymer, preferably a hydroxypropyl methylcellulose, and a water-insoluble polymer, preferably an acrylic resin, in a ratio range of about one-to-one (1:1) to about nine-to-one (9:1), more preferably a range of about three-to-two (3:2) to about six-to-one (6:1), and most preferably in a range of about two-to-one (2:1) to about four-to-one (4:1) by weight. This formulation capable of providing therapeutically effective bioavailability of guaifenesin for at least twelve hours after dosing in a human subject. The invention also relates to a modified release product which has two portions: a first portion having an immediate release formulation of guaifenesin and a second portion having a sustained release formulation of guaifenesin, wherein one or both portions further comprises pseudoephedrine. The modified release product has a maximum guaifenesin serum concentration equivalent to that of an immediate release guaifenesin tablet, and is capable of providing therapeutically effective bioavailability of guaifenesin for at least twelve hours after dosing in a human subject.
摘要翻译： 本发明涉及愈创甘油醚和伪麻黄碱的新型药物缓释制剂。 制剂可包含亲水性聚合物，优选羟丙基甲基纤维素和水不溶性聚合物，优选丙烯酸树脂，其比例范围为约一对一（1：1）至约九对一（9 ：1），更优选约三至二（3:2）至约六对一（6:1）的范围，最优选在约二至一（2:1）的范围内 ）至约四对一（4:1）重量比。 该制剂能够在给予人受试者后至少十二个小时提供愈创甘油的治疗有效的生物利用度。 本发明还涉及一种具有两部分的改性释放产物：第一部分具有愈创甘油醚的立即释放制剂，第二部分具有愈创甘油醚的缓释制剂，其中一个或两个部分还包含伪麻黄碱。 改性释放产物具有与立即释放愈创甘油醚片剂相当的最大愈创甘油醚血清浓度，并且能够在给予人受试者后至少十二个小时提供愈创甘油的治疗有效的生物利用度。
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公开(公告)号：US20110052689A1
公开(公告)日：2011-03-03
申请号：US12940781
申请日：2010-11-05
CPC分类号： A61K9/2086 , A61K9/2027 , A61K9/2054 , A61K9/209 , A61K9/5084 , A61K31/09 , A61K31/137 , A61K31/485 , A61K31/495 , A61K2300/00
摘要： The invention relates to a novel pharmaceutical sustained release formulation of guaifenesin. The formulation may comprise a hydrophilic polymer, preferably a hydroxypropyl methylcellulose, and a water-insoluble polymer, preferably an acrylic resin, in a ratio range of about one-to-one (1: 1) to about nine-to-one (9: 1), more preferably a range of about three-to-two (3:2) to about six-to-one (6: 1), and most preferably in a range of about two-to-one (2: 1) to about four-to-one (4: 1) by weight. This formulation capable of providing therapeutically effective bioavailability of guaifenesin for at least twelve hours after dosing in a human subject. The invention also relates to a modified release product which has two portions: a first portion having an immediate release formulation of guaifenesin and a second portion having a sustained release formulation of guaifenesin. The modified release product has a maximum guaifenesin serum concentration equivalent to that of an immediate release guaifenesin tablet, and is capable of providing therapeutically effective bioavailability of guaifenesin for at least twelve hours after dosing in a human subject.
摘要翻译： 本发明涉及愈创甘油醚的新型药物缓释制剂。 制剂可包含亲水性聚合物，优选羟丙基甲基纤维素和水不溶性聚合物，优选丙烯酸树脂，其比例范围为约一对一（1：1）至约九对一（9 ：1），更优选约三至二（3:2）至约六对一（6:1）的范围，最优选在约二至一（2:1）的范围内 ）至约四对一（4:1）重量比。 该制剂能够在给予人受试者后至少十二个小时提供愈创甘油的治疗有效的生物利用度。 本发明还涉及一种具有两部分的改良释放产物：第一部分具有愈创甘油醚的立即释放制剂，第二部分具有愈创甘油醚的缓释制剂。 改性释放产物具有与立即释放愈创甘油醚片剂相当的最大愈创甘油醚血清浓度，并且能够在给予人受试者后至少十二个小时提供愈创甘油的治疗有效的生物利用度。
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公开(公告)号：US06372252B1
公开(公告)日：2002-04-16
申请号：US09559542
申请日：2000-04-28
IPC分类号： A61K920
CPC分类号： A61K9/5084 , A61K9/2027 , A61K9/2054 , A61K9/209 , A61K31/09 , A61K31/137 , A61K31/485 , A61K31/495 , A61K2300/00
摘要： The invention relates to a novel pharmaceutical sustained release formulation of guaifenesin. The formulation may comprise a hydrophilic polymer, preferably a hydroxypropyl methylcellulose, and a water-insoluble polymer, preferably an acrylic resin, in a ratio range of about one-to-one (1:1) to about six-to-one (6:1), more preferably a range of about three-to-two (3:2) to about four-to-one (4:1), and most preferably about two-to-one (2:1), by weight. This formulation capable of providing therapeutically effective bioavailability of guaifenesin for at least twelve hours after dosing in a human subject. The invention also relates to a modified release guaifenesin tablet which has two portion: the first portion comprises an immediate release formulation of guaifenesin and the second portion comprises a sustained release formulation of guaifenesin as described above. This two portion, or bi-layer, tablet has a maximum serum concentration equivalent to that of an immediate release guaifenesin tablet, and is capable of providing therapeutically effective bioavailability of guaifenesin for at least twelve hours after dosing in a human subject.
摘要翻译： 本发明涉及愈创甘油醚的新型药物缓释制剂。 制剂可以包含亲水性聚合物，优选羟丙基甲基纤维素和水不溶性聚合物，优选丙烯酸树脂，其比例范围为约一对一（1：1）至约六比一（6 ：1），更优选约三至二（3:2）至约四对一（4:1），最优选约二比一（2:1）的范围 。 该制剂能够在给予人受试者后至少十二个小时提供愈创甘油的治疗有效的生物利用度。 本发明还涉及一种具有两部分的改性释放愈创甘油醚片剂：第一部分包含愈创甘油醚的立即释放制剂，第二部分包含如上所述的愈创甘油醚缓释制剂。 这两部分或双层片剂具有与立即释放愈创甘油醚片剂相当的最大血清浓度，并且能够在给予人受试者后至少十二个小时提供愈创甘油醚治疗有效的生物利用度。
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公开(公告)号：US07838032B2
公开(公告)日：2010-11-23
申请号：US10406557
申请日：2003-04-04
IPC分类号： A61K9/22
CPC分类号： A61K9/2086 , A61K9/2027 , A61K9/2054 , A61K9/209 , A61K9/5084 , A61K31/09 , A61K31/137 , A61K31/485 , A61K31/495 , A61K2300/00
摘要： The invention relates to a novel pharmaceutical sustained release formulation of guaifenesin. The formulation may comprise a hydrophilic polymer, preferably a hydroxypropyl methylcellulose, and a water-insoluble polymer, preferably an acrylic resin, in a ratio range of about one-to-one (1:1) to about nine-to-one (9:1), more preferably a range of about three-to-two (3:2) to about six-to-one (6:1), and most preferably in a range of about two-to-one (2:1) to about four-to-one (4:1) by weight. This formulation capable of providing therapeutically effective bioavailability of guaifenesin for at least twelve hours after dosing in a human subject. The invention also relates to a modified release product which has two portions: a first portion having an immediate release formulation of guaifenesin and a second portion having a sustained release formulation of guaifenesin. The modified release product has a maximum guaifenesin serum concentration equivalent to that of an immediate release guaifenesin tablet, and is capable of providing therapeutically effective bioavailability of guaifenesin for at least twelve hours after dosing in a human subject.
摘要翻译： 本发明涉及愈创甘油醚的新型药物缓释制剂。 制剂可包含亲水性聚合物，优选羟丙基甲基纤维素和水不溶性聚合物，优选丙烯酸树脂，其比例范围为约一对一（1：1）至约九对一（9 ：1），更优选约三至二（3:2）至约六对一（6:1）的范围，最优选在约二至一（2:1）的范围内 ）至约四对一（4:1）重量比。 该制剂能够在给予人受试者后至少十二个小时提供愈创甘油的治疗有效的生物利用度。 本发明还涉及一种具有两部分的改良释放产物：第一部分具有愈创甘油醚的立即释放制剂，第二部分具有愈创甘油醚的缓释制剂。 改性释放产物具有与立即释放愈创甘油醚片剂相当的最大愈创甘油醚血清浓度，并且能够在给予人受试者后至少十二个小时提供愈创甘油的治疗有效的生物利用度。
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公开(公告)号：US08802152B2
公开(公告)日：2014-08-12
申请号：US13371080
申请日：2012-02-10
IPC分类号： C07F7/02 , A61K33/24 , A61K9/20 , A61K9/48 , B01J19/18 , B01J39/14 , B01J39/02 , C01B39/00 , B01J19/00 , A61K9/14 , A61K45/06 , A61K33/00
CPC分类号： A61K33/24 , A61K9/14 , A61K9/143 , A61K33/00 , A61K45/06 , B01J19/0013 , B01J19/006 , B01J19/0066 , B01J19/18 , B01J39/02 , B01J39/14 , B01J2219/00063 , B01J2219/00094 , B01J2219/00768 , C01B33/20 , C01B39/00 , C01B39/02 , C01B39/46 , C01P2002/72 , C01P2002/82 , C01P2004/52 , C01P2004/61 , C07F7/025 , Y10T428/2982 , A61K2300/00
摘要： The present invention relates to novel microporous zirconium silicate compositions that are formulated to remove toxins, e.g. potassium ions, from the gastrointestinal tract at an elevated rate without causing undesirable side effects. The preferred formulations are designed avoid increase in pH of urine in patients and/or avoid potential entry of particles into the bloodstream of the patient. Also disclosed is a method for preparing high purity crystals of UZSi-9 exhibiting an enhanced level of potassium exchange capacity. These compositions are particularly useful in the therapeutic treatment of hyperkalemia.
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公开(公告)号：US20120213847A1
公开(公告)日：2012-08-23
申请号：US13371080
申请日：2012-02-10
CPC分类号： A61K33/24 , A61K9/14 , A61K9/143 , A61K33/00 , A61K45/06 , B01J19/0013 , B01J19/006 , B01J19/0066 , B01J19/18 , B01J39/02 , B01J39/14 , B01J2219/00063 , B01J2219/00094 , B01J2219/00768 , C01B33/20 , C01B39/00 , C01B39/02 , C01B39/46 , C01P2002/72 , C01P2002/82 , C01P2004/52 , C01P2004/61 , C07F7/025 , Y10T428/2982 , A61K2300/00
摘要： The present invention relates to novel microporous zirconium silicate compositions that are formulated to remove toxins, e.g. potassium ions, from the gastrointestinal tract at an elevated rate without causing undesirable side effects. The preferred formulations are designed avoid increase in pH of urine in patients and/or avoid potential entry of particles into the bloodstream of the patient. Also disclosed is a method for preparing high purity crystals of UZSi-9 exhibiting an enhanced level of potassium exchange capacity. These compositions are particularly useful in the therapeutic treatment of hyperkalemia.
摘要翻译： 本发明涉及配制成去除毒素的新型微孔硅酸锆组合物，例如， 钾离子，来自胃肠道以升高的速率，而不引起不期望的副作用。 设计优选的制剂避免了患者尿液pH值的增加和/或避免颗粒潜在地进入患者的血液中。 还公开了一种制备显示增强的钾交换容量水平的UZSi-9的高纯度晶体的方法。 这些组合物特别可用于治疗高钾血症。
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