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1.发明授权Bioadhesive progressive hydration tablets and methods of making and using the same 有权生物粘合剂逐步水合片及其制备和使用方法公开(公告)号：US06248358B1
公开(公告)日：2001-06-19
申请号：US09379310
申请日：1999-08-23
IPC分类号： A61K920
CPC分类号： A61K31/568 , A61K9/0034 , A61K9/006 , A61K9/2018 , A61K9/2027 , A61K9/2054 , A61K9/2059
摘要： A bioadhesive tablet wherein the active ingredient may be protected from water or the surrounding environment, thereby protecting it from metabolism or from other degradation caused by moisture, enzymes, or pH effects, and making it bioavailable only at a controlled rate. The active ingredient may be protected from moisture during the manufacturing process and more importantly may be protected from moisture and the immediate septic environment until after the patient has applied the tablet, and then only at a slow and controlled rate. It is by this process of progressive hydration that the active ingredient remains protected for many hours after administration. It is also by the process of progressive hydration that controlled and sustained release is achieved because only that part of the active ingredient that is the hydrated (aqueous) fraction of the tablet is available for absorption (bioavailable).
摘要翻译： 生物粘附片剂，其中活性成分可以被保护免受水或周围环境的影响，从而保护其不受代谢或由水分，酶或pH影响引起的其它降解，并且仅以受控的速率使其生物可利用。 活性成分可以在制造过程中受到保护，并且更重要的是可以防止水分和直接的化脓性环境，直到患者施用片剂，然后仅以缓慢和受控的速率。 正是通过这种进行性水合过程，活性成分在给药后保持多个小时。 也是通过进行性水合的过程来实现控制和持续释放，因为只有作为片剂的水合（水性）级分的活性成分的那部分可用于吸收（生物可利用的）。
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公开(公告)号：US06818672B1
公开(公告)日：2004-11-16
申请号：US10089796
申请日：2002-07-24
IPC分类号： A01N3302
CPC分类号： A61K47/32 , A61K9/0034 , A61K9/2027 , A61K31/135 , A61K31/137 , Y10S514/967
摘要： The present invention concerns compositions and methods for using a &bgr;-adrenergic agonist for treating endometriosis, for treating infertility, and for improving fertility. The present invention further concerns formulating such a composition or method in such a way as to provide therapeutically sufficient levels of the &bgr;-adrenergic agonist locally while avoiding adverse systematic concentrations in the host, thereby minimizing or avoiding adverse side effects.
摘要翻译： 本发明涉及使用β-肾上腺素能激动剂治疗子宫内膜异位症，治疗不孕症和改善生育能力的组合物和方法。 本发明还涉及以这样的方式配制这样的组合物或方法，以便局部地提供治疗上足够水平的β-肾上腺素能激动剂，同时避免宿主中不利的系统浓度，从而最小化或避免不良副作用。
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公开(公告)号：US06306914B1
公开(公告)日：2001-10-23
申请号：US09170326
申请日：1998-10-13
IPC分类号： A01N2500
CPC分类号： A61K31/57 , A61K9/0034 , A61K9/7023 , A61K47/32 , Y10S514/944 , A61K31/565 , A61K2300/00
摘要： The present invention teaches that daily, cyclical vaginal delivery of progestin may be used to provide regular, predictable withdrawal bleeding during hormone replacement therapy. The present invention also teaches that constant administration of progestin in a water-insoluble, water-swellable cross-linked polycarboxylic acid polymer may be used to maintain amenorrhea. Either regimen is accompanied by a significant decrease in adverse side effects.
摘要翻译： 本发明教导，孕激素替代治疗期间可以使用孕激素的每日周期性阴道分娩来提供规则的，可预测的撤出性出血。 本发明还教导了在水不溶性的水溶胀性交联聚羧酸聚合物中不断施用孕激素以维持闭经。 两种方案都伴随着副作用的显着降低。
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公开(公告)号：US06593317B1
公开(公告)日：2003-07-15
申请号：US09833259
申请日：2000-10-17
IPC分类号： A61K3157
CPC分类号： A61K31/57 , A61K9/0034 , A61K9/7023 , A61K47/32 , Y10S514/944 , A61K31/565 , A61K2300/00
摘要： The present invention teaches that daily, cyclical vaginal delivery of progestin may be used to provide regular, predictable withdrawal bleeding during hormone replacement therapy. The present invention also teaches that constant administration of progestin in a water-insoluble, water-swellable cross-linked polycarboxylic acid polymer may be used to maintain amenorrhea. Either regimen is accompanied by a significant decrease in adverse side effects.
摘要翻译： 本发明教导，孕激素替代治疗期间可以使用孕激素的每日周期性阴道分娩来提供规则的，可预测的撤出性出血。 本发明还教导了在水不溶性的水溶胀性交联聚羧酸聚合物中不断施用孕激素以维持闭经。 两种方案都伴随着副作用的显着降低。
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公开(公告)号：US20110053845A1
公开(公告)日：2011-03-03
申请号：US12941840
申请日：2010-11-08
IPC分类号： A61K38/22 , A61K38/14 , A61K38/00 , A61K31/138 , A61P15/06 , A61P29/00 , A61P31/00 , A61P23/00
CPC分类号： A61K9/0034 , A61K9/006 , A61K31/137 , A61K47/32
摘要： The invention relates to a pharmaceutical composition for vaginal administration of a treating agent normally associated with undesired side effects at detrimental blood levels. The composition releases the treating agent at a rate to achieve local tissue concentrations without such detrimental blood levels by using a therapeutically effective amount of the treating agent and a bioadhesive, cross-linked water swellable, but water-insoluble polycarboxylic acid polymer. Using this composition and the method of treatment provides sufficient local levels of the drug to provide therapeutic efficacy, but avoids many untoward adverse events. The invention also relates to a pharmaceutical composition for use during menses that includes a treating agent and a bioadhesive, cross-linked water swellable, but water-insoluble polycarboxylic acid polymer.
摘要翻译： 本发明涉及通常与有害血液水平的不良副作用相关的治疗剂的阴道给药的药物组合物。 组合物通过使用治疗有效量的治疗剂和生物粘附性交联水可溶胀但水不溶性多元羧酸聚合物，以达到局部组织浓度而没有这种有害血液水平的速率释放治疗剂。 使用该组合物和治疗方法提供了足够的局部水平的药物以提供治疗功效，但避免了许多不良事件。 本发明还涉及在月经期间使用的药物组合物，其包括处理剂和生物粘附剂，交联的水可溶胀但是水不溶性的多元羧酸聚合物。
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公开(公告)号：US07153845B2
公开(公告)日：2006-12-26
申请号：US10421840
申请日：2003-04-24
IPC分类号： A61K31/33 , A61K31/553 , A61K31/554
CPC分类号： A61K31/568 , A61K9/0034 , A61K9/006 , A61K9/2018 , A61K9/2027 , A61K9/2054 , A61K9/2059
摘要： A bioadhesive controlled, extended release progressive hydration composition wherein the active ingredient may be protected from water or the surrounding environment, thereby protecting it from metabolism or from other degradation caused by moisture, enzymes, or pH effects, and making it bioavailable only at a controlled rate. The active ingredient may be protected from moisture during the manufacturing process, as necessary or desired, and more importantly may be protected from moisture and the immediate septic environment until well after the patient has applied the composition, and then only at a slow and controlled rate. It is by this process of progressive hydration that the active ingredient remains protected for many hours after administration. It is also by the process of progressive hydration that controlled and sustained release is achieved because only that part of the active ingredient that is the hydrated (aqueous) fraction of the composition is available for absorption (bioavailable).
摘要翻译： 生物粘附控制的延长释放的进行性水合组合物，其中活性成分可以被保护免受水或周围环境的影响，从而保护其免受代谢或由水分，酶或pH影响引起的其它降解，并使其仅在受控的 率。 活性成分可根据需要或需要在制造过程中得到保护，并且更重要的是可以保护免受潮湿和直接的败血症环境，直到患者施用组合物，然后仅以缓慢和受控的速率 。 正是通过这种进行性水合过程，活性成分在给药后保持多个小时。 还通过进行水合的过程，控制和持续释放是实现的，因为只有作为组合物的水合（水）部分的活性成分的那部分可用于吸收（生物可利用的）。
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公开(公告)号：US08765177B2
公开(公告)日：2014-07-01
申请号：US11431611
申请日：2006-05-11
CPC分类号： A61K9/006 , A61K9/0031 , A61K9/0034
摘要： A bioadhesive controlled, extended release progressive hydration composition wherein the active ingredient may be protected from water or the surrounding environment, thereby protecting it from metabolism or from other degradation caused by moisture, enzymes, or pH effects, and making it bioavailable only at a controlled rate. The active ingredient may be protected from moisture during the manufacturing process, as necessary or desired, and more importantly may be protected from moisture and the immediate septic environment until well after the patient has applied the composition, and then only at a slow and controlled rate. It is by this process of progressive hydration that the active ingredient remains protected for many hours after administration. It is also by the process of progressive hydration that controlled and sustained release is achieved because only that part of the active ingredient that is the hydrated (aqueous) fraction of the composition is available for absorption (bioavailable).
摘要翻译： 生物粘附控制的延长释放的进行性水合组合物，其中活性成分可以被保护免受水或周围环境的影响，从而保护其免受代谢或由水分，酶或pH影响引起的其它降解，并且仅在受控的 率。 活性成分可根据需要或需要在制造过程中得到保护，并且更重要的是可以保护免受潮湿和直接的败血症环境，直到患者施用组合物，然后仅以缓慢和受控的速率 。 正是通过这种进行性水合过程，活性成分在给药后保持多个小时。 还通过进行水合的过程，控制和持续释放是实现的，因为只有作为组合物的水合（水）部分的活性成分的那部分可用于吸收（生物可利用的）。
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公开(公告)号：US06126959A
公开(公告)日：2000-10-03
申请号：US145172
申请日：1998-09-01
CPC分类号： A61K31/137 , A61K47/32 , A61K9/0034 , A61K9/006
摘要： The present invention teaches a composition comprising a .beta.-adrenergic agonist in a bioadhesive carrier. Preferably, the composition comprises terbutaline in polycarbophil. The present invention additionally teaches the local administration of a .beta.-adrenergic agonist for the purpose of treating or preventing dysmenorrhea or premature labor. Using this composition and the method of treatment provides sufficient local levels of the drug to provide therapeutic efficacy, but avoids many untoward adverse events.
摘要翻译： 本发明教导了一种在生物粘附载体中包含β-肾上腺素能激动剂的组合物。 优选地，组合物在聚卡波非内含有特布他林。 本发明另外教导了β-肾上腺素能激动剂的局部施用，用于治疗或预防痛经或早产。 使用该组合物和治疗方法提供了足够的局部水平的药物以提供治疗功效，但避免了许多不良事件。
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公开(公告)号：US06699494B2
公开(公告)日：2004-03-02
申请号：US09510527
申请日：2000-02-22
IPC分类号： A61F1300
CPC分类号： A61K31/137 , A61K9/0034 , A61K9/006 , A61K47/32
摘要： The present invention teaches a composition comprising a &bgr;-adrenergic agonist in a bioadhesive carrier. Preferably, the composition comprises terbutaline in polycarbophil. The present invention additionally teaches the local administration of a &bgr;-adrenergic agonist for the purpose of treating or preventing dysmenorrhea or premature labor. Using this composition and the method of treatment provides sufficient local levels of the drug to provide therapeutic efficacy, but avoids many untoward adverse events.
摘要翻译： 本发明教导了一种在生物粘附载体中包含β-肾上腺素能激动剂的组合物。 优选地，组合物在聚卡波非内含有特布他林。 本发明另外教导了β-肾上腺素能激动剂的局部施用，用于治疗或预防痛经或早产。 使用该组合物和治疗方法提供了足够的局部水平的药物以提供治疗功效，但避免了许多不良事件。
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公开(公告)号：US06624200B2
公开(公告)日：2003-09-23
申请号：US09877218
申请日：2001-06-11
IPC分类号： A01N3302
CPC分类号： A61K9/006 , A61K9/2027 , A61K9/2054
摘要： A bioadhesive composition wherein the active ingredient may be protected from water or the surrounding environment, thereby protecting it from metabolism or from other degradation caused by moisture, enzymes, or pH effects, and making it bioavailable only at a controlled rate. The active ingredient may be protected from moisture during the manufacturing process and more importantly may be protected from moisture and the immediate septic environment until after the patient has applied the composition, and then only at a slow and controlled rate. It is by this process of progressive hydration that the active ingredient remains protected for many hours after administration. It is also by the process of progressive hydration that controlled and sustained release is achieved because only that part of the active ingredient that is the hydrated (aqueous) fraction of the composition is available for absorption (bioavailable).
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