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21. 发明申请

US20080305160A1 Oral Medicament For The Modified Release Of At Least One Active Principle, In Multimicrocapsule Form 审中-公开
标题翻译：口服药物的修饰释放至少一个主动原则，在多微囊形式
公开(公告)号：US20080305160A1
公开(公告)日：2008-12-11
申请号：US11791466
申请日：2005-11-02
申请人： Florence Guimberteau , Catherine Castan , Remi Meyrueix , Gerard Soula
发明人： Florence Guimberteau , Catherine Castan , Remi Meyrueix , Gerard Soula
IPC分类号： A61K9/52 , A61K9/26 , A61K31/585 , A61K31/4166 , A61K31/435 , A61K31/43 , A61K31/522
CPC分类号： A61K9/5031
摘要： The field of the invention is that of oral medicaments or pharmaceutical compositions, in particular of the type including one or more active principles. The aim of the invention is to provide an improved oral medicament to be administered in one or several daily doses and enabling the modified release of active principles (in particular of one active principle), whereby the prophylactic and therapeutic effectiveness of said medicament is improved. This aim is achieved by the oral multimicrocapsule galenic form according to the invention, in which the active principle release is controlled by a dual release trigger mechanism: “time-dependent trigger” and “pH-dependent trigger”. Said medicament includes microcapsules providing the modified release of the active principle, each comprising a core containing
摘要翻译：本发明的领域是口服药物或药物组合物，特别是包括一种或多种活性成分的类型。本发明的目的是提供一种或多种日剂量施用的改进的口服药物，并且能够改变释放活性成分（特别是一种活性成分），从而提高所述药物的预防和治疗效果。该目的通过根据本发明的口服多微囊盖仑型形式实现，其中主动释放由双重释放触发机制控制：“时间依赖性触发”和“依赖于pH的触发”。所述药物包括提供活性成分的改性释放的微胶囊，每个包含含有的核心

22. 发明申请

US20060275376A1 Microcapsules with modified release of active principles with low solubility for oral delivery 审中-公开
标题翻译：具有改进释放活性成分的微胶囊，具有低溶解性用于口服递送
公开(公告)号：US20060275376A1
公开(公告)日：2006-12-07
申请号：US10522234
申请日：2003-07-28
申请人： Florence Guimberteau , Catherine Castan , Remi Meyrueix , Gerard Soula
发明人： Florence Guimberteau , Catherine Castan , Remi Meyrueix , Gerard Soula
IPC分类号： A61K9/50 , A61K9/16
CPC分类号： A61K9/5015 , A61K9/5026 , A61K9/5047
摘要： The invention concerns microcapsules for reliably modified release and adapted to industrial reproduction of an active principle hardly water-soluble, other than anti-hyperglycemia agents Each of said microcapsules comprises a core of hardly soluble active principle and a coating film applied on the core. Their mean diameter is less than 1000 microns. The coating film contains a film-forming polymer (P1) insoluble in gastrointestinal tract fluids, a water-soluble polymer (P2), a plasticizer (PL), and optionally a lubricating surfactant (TA). Said coating film represents at least 4% p/p of dry mraner of their total weight. and its components P1, P2. PL satisfy the following characteristics: dry weight mass fraction of PI relative to the total coating weight ranging between 40 and 90%; dry matter weight fraction of PL/P1+P2 ranging between 15 and 60%: dry matter weight fraction of PL/P1+P2 ranging between 1 and 30%. The invention also concerns the uses of said microcapsules in galenic formulation.
摘要翻译：本发明涉及用于可靠调节释放的微胶囊，并且适用于除抗高血糖剂以外的几乎不溶于水的活性成分的工业复制。所述微胶囊中的每一种都包含难溶的活性成分的核心和涂覆在芯上的涂膜。它们的平均直径小于1000微米。涂膜含有不溶于胃肠道液的成膜聚合物（P1），水溶性聚合物（P2），增塑剂（PL）和任选的润滑表面活性剂（TA）。所述涂膜占其总重量的至少4％p / p干燥颗粒。及其部件P1，P2。 PL满足以下特征：相对于总涂层重量的40重量％至90重量％的PI的干重质量分数; PL / P1 + P2的干物质重量分数在15和60％之间：PL / P1 + P2的干物质重量分数范围在1％和30％之间。本发明还涉及所述微胶囊在盖仑制剂中的用途。

23. 发明申请

US20060165807A1 Oral pharmaceutical formulation in the form of aqueous suspension for modified release of active principle(s) 有权
标题翻译：用于修饰释放活性成分的水性悬浮液形式的口服药物制剂
公开(公告)号：US20060165807A1
公开(公告)日：2006-07-27
申请号：US10510643
申请日：2003-04-07
申请人： Catherine Castan , Florence Guimberteau , Remi Meyrueix
发明人： Catherine Castan , Florence Guimberteau , Remi Meyrueix
IPC分类号： A61K9/50 , A61K9/16
CPC分类号： A61K9/5047 , A61K9/0053 , A61K9/0095 , A61K9/10 , A61K9/5015 , A61K9/5026 , A61K9/5042 , A61K31/155 , A61K31/192 , A61K31/43 , A61K31/522 , A61K31/585
摘要： The invention concerns liquid pharmaceutical formulations, for oral delivery, with modified release of active principle(s) excluding amoxicillin and consisting of suspensions of coated particles of active principles (microcapsules). The microcapsules constituting the dispersed phase of the suspension are designed, according to the invention, to enable modified release of the active principle(s), in accordance with a profile which remains unaltered during the shelf life of the liquid suspension. Therefor, the invention consists in selecting a coating composition specific to the microcapsules consisting of at least four components enabling preservation of said microcapsules in water without altering their properties of modified release of the active principle, said liquid phase being furthermore saturated with active principle(s).
摘要翻译：本发明涉及用于口服递送的液体药物制剂，其具有除阿莫西林以外的活性成分的改进释放，并且由活性成分的包被颗粒（微胶囊）的悬浮液组成。根据本发明，构成悬浮液分散相的微胶囊根据在液体悬浮体的保质期内保持不变的轮廓来实现活性成分的改性释放。因此，本发明在于选择由至少四种组分组成的微胶囊特性的涂料组合物，所述组合物能够在水中保存所述微胶囊，而不改变其活性成分的改性释放性质，所述液相还用活性成分）。

24. 发明申请

US20050196459A1 Carvedilol salts, anhydrates and/or solvate thereof, corresponding pharmaceutical compositions, controlled release formulations, and treatment or delivery methods 有权
标题翻译：卡维地洛盐，其水合物和/或溶剂合物，相应的药物组合物，控制释放制剂和治疗或递送方法
公开(公告)号：US20050196459A1
公开(公告)日：2005-09-08
申请号：US10996780
申请日：2004-11-24
申请人： Catherine Castan , Florence Guimberteau , Remi Meyrueix , Gerard Soula
发明人： Catherine Castan , Florence Guimberteau , Remi Meyrueix , Gerard Soula
IPC分类号： A61K20060101 , A61K9/16 , A61K9/22 , A61K9/50 , A61K31/403
CPC分类号： A61K9/1635 , A61K9/1641 , A61K9/1658 , A61K9/2077 , A61K31/403
摘要： The field of the invention is that of oral pharmaceutical medicinal products or compositions, more particularly of the type of those comprising one or more active principles. The aim of the invention is to provide an improved oral medicinal product that can be administered in one or more daily doses, with modified release of active principle (in particular an active principle), for improving the prophylactic and therapeutic efficacy of such a medicinal product. This aim is achieved by means of the multimicrocapsular oral pharmaceutical form according to the invention in which the release of the AP is controlled by means of a double mechanism of triggering the release: “time triggering” and “pH triggering”. This medicinal product comprises microcapsules with modified release of active principle, each containing a core comprising the active principle and one or more swelling agents, and at least one coating making possible the modified release of the active principle.
摘要翻译：本发明的领域是口服药物药物产品或组合物的领域，更特别是包含一种或多种活性成分的那些类型。本发明的目的是提供一种改进的口服药物产品，其可以以一种或多种日剂量施用，具有改进的活性成分释放（特别是活性成分），用于改善这种药物的预防和治疗功效。该目的通过根据本发明的多微囊口服药物形式实现，其中AP的释放通过触发释放的双重机制来控制：“时间触发”和“pH触发”。这种药用产品包括具有活性成分释放的微胶囊，每个微胶囊含有包含活性成分的核心和一种或多种溶胀剂，以及至少一种使活性成分的修饰释放成为可能的涂层。

25. 发明授权

US08197850B2 Medicine based on anti-hyperglycaemic microcapsules with prolonged release and method for preparing same 失效
标题翻译：基于抗高血糖微胶囊延长释药的药物及其制备方法
公开(公告)号：US08197850B2
公开(公告)日：2012-06-12
申请号：US10415850
申请日：2001-11-19
申请人： Catherine Castan , Remi Meyrueix , Gerard Soula
发明人： Catherine Castan , Remi Meyrueix , Gerard Soula
IPC分类号： A61K9/14
CPC分类号： A61K31/155 , A61K9/5015 , A61K9/5047 , A61K31/00
摘要： The invention concerns an oral galenic form for prolonged release of anti-hyperglycaemic (metformin) active principles. Said medicine enables to obtain an efficient therapeutic protection over 24 hours by overcoming the problems of bypass of the absorption window and the massive localised release of active principles. Therefor, said medicine comprises several thousand anti-hyperglycaemic (metformin) microcapsules each consisting of a core comprising at least an anti-hyperglycaemic agent and of a coating film applied on the core and enabling the prolonged release in vivo of the anti-hyperglycaemic agent. Said microcapsules have a grain size distribution ranging between 50 and 100 microns. The reproducibility of the transit kinetics and hence of bioavailability are very high. There results for the patient a lesser risk of hyperglycaemic or hypoglycaemic. The invention also concerns the preparation of said medicine and the use of a plurality of said microcapsules for making an anti-hyperglycaemic medicine. The invention is applicable to the treatment of type II diabetes.
摘要翻译：本发明涉及用于延长释放抗高血糖（二甲双胍）活性成分的口服盖仑制剂。所述药物通过克服吸收窗旁路的问题和主动原理的大量局部释放，能够在24小时内获得有效的治疗保护。因此，所述药物包含数千种抗高血糖（二甲双胍）微胶囊，每个微胶囊由包含至少抗高血糖剂的芯和涂覆在芯上的涂膜构成，并且能够在体内延长抗高血糖剂的释放。所述微胶囊具有在50和100微米之间的粒度分布。运输动力学和生物利用度的重现性非常高。结果，患者血糖过低或低血糖的风险较小。本发明还涉及所述药物的制备以及多种所述微胶囊用于制备抗高血糖药物的用途。本发明适用于II型糖尿病的治疗。

26. 发明申请

US20100310667A1 CONTROLLED-RELEASE FLOATING PHARMACEUTICAL COMPOSITIONS 有权
标题翻译：控制释放浮选药物组合物
公开(公告)号：US20100310667A1
公开(公告)日：2010-12-09
申请号：US12790201
申请日：2010-05-28
申请人： Catherine Castan , Philippe Caisse
发明人： Catherine Castan , Philippe Caisse
IPC分类号： A61K9/14 , C08B3/06
CPC分类号： A61K9/0065 , A61K9/4866 , A61K9/5015 , A61K9/5026 , A61K9/5031 , A61K9/5047 , A61K9/5078 , A61K31/155 , A61K31/192 , A61K31/403
摘要： The invention relates to a pharmaceutical composition comprising a plurality of controlled-release coated microparticles each comprising a floating core, on the surface of which is deposited a layer containing at least one active principle, said layer being covered with a controlled-release coating, characterized by the fact that said floating core is composed of cellulose acetate phthalate and has an apparent density of less than or equal to 0.6 g/mL and said coated microparticles have a density of less than or equal to 0.7 g/mL.
摘要翻译：本发明涉及一种药物组合物，其包含多个受控释放的包被的微粒，每个包含浮芯，其表面沉积包含至少一种活性成分的层，所述层被覆盖有控释膜，其特征在于所述浮芯由醋酸邻苯二甲酸纤维素组成，表观密度小于或等于0.6g / mL，所述涂布微粒的密度小于或等于0.7g / mL。

27. 发明申请

US20100015220A1 NIACIN AND NSAID COMBINATION THERAPY 审中-公开
标题翻译： NIACIN和NSAID组合治疗
公开(公告)号：US20100015220A1
公开(公告)日：2010-01-21
申请号：US12469653
申请日：2009-05-20
申请人： John R. WETTERAU , Lingyu Zhu , Robert A. Scott , Constance H. Keyserling , Jean-Louis H. Dasseux , Daniela Carmen Oniciu , Pierre Autant , Roger Kravtzoff , Catherine Castan , Hervé Guillard
发明人： John R. WETTERAU , Lingyu Zhu , Robert A. Scott , Constance H. Keyserling , Jean-Louis H. Dasseux , Daniela Carmen Oniciu , Pierre Autant , Roger Kravtzoff , Catherine Castan , Hervé Guillard
IPC分类号： A61K9/48 , A61K9/20 , A61K31/455 , A61K9/50 , A61K31/60 , A61P25/34
CPC分类号： A61K31/455 , A61K31/616 , A61K2300/00
摘要： Provided are pharmaceutical compositions and methods for preventing or reducing niacin-induced flushing comprising an aspirin component and a niacin component having different release profiles. Also provided are methods and compositions for preventing or reducing niacin-induced flushing comprising niacin, aspirin and a lipid-lowering drug other than niacin.
摘要翻译：提供了用于预防或减少烟酸诱发的潮红的药物组合物和方法，其包含具有不同释放特征的阿司匹林组分和烟酸组分。还提供了用于预防或减少烟酸诱发的潮红的方法和组合物，其包含烟酸，阿司匹林和除了烟酸以外的降脂药物。

28. 发明授权

US09561179B2 Controlled-release floating pharmaceutical compositions 有权
标题翻译：控制释放的浮动药物组合物
公开(公告)号：US09561179B2
公开(公告)日：2017-02-07
申请号：US12790201
申请日：2010-05-28
申请人： Catherine Castan , Philippe Caisse
发明人： Catherine Castan , Philippe Caisse
IPC分类号： A61K9/14 , C08B3/06 , A61K9/00 , A61K9/50
CPC分类号： A61K9/0065 , A61K9/4866 , A61K9/5015 , A61K9/5026 , A61K9/5031 , A61K9/5047 , A61K9/5078 , A61K31/155 , A61K31/192 , A61K31/403
摘要： The invention relates to a pharmaceutical composition comprising a plurality of controlled-release coated microparticles each comprising a floating core, on the surface of which is deposited a layer containing at least one active principle, said layer being covered with a controlled-release coating, characterized by the fact that said floating core is composed of cellulose acetate phthalate and has an apparent density of less than or equal to 0.6 g/mL and said coated microparticles have a density of less than or equal to 0.7 g/mL.
摘要翻译：本发明涉及一种药物组合物，其包含多个受控释放的包被的微粒，每个包含浮芯，其表面沉积包含至少一种活性成分的层，所述层被覆盖有控释膜，其特征在于所述浮芯由醋酸邻苯二甲酸纤维素组成，表观密度小于或等于0.6g / mL，所述涂布微粒的密度小于或等于0.7g / mL。

29. 发明申请

US20050037077A1 Galenic microparticulate oral formulation for delayed and controlled release of pharmaceutical active principles 审中-公开
标题翻译：用于延迟和控制释放药物活性成分的Galenic微粒口服制剂
公开(公告)号：US20050037077A1
公开(公告)日：2005-02-17
申请号：US10492129
申请日：2002-10-09
申请人： Valerie Legrand , Catherine Castan , Remi Meyrueix , Gerard Soula
发明人： Valerie Legrand , Catherine Castan , Remi Meyrueix , Gerard Soula
IPC分类号： A61K9/14 , A61K9/22 , A61K9/26 , A61K9/48 , A61K9/50 , A61K9/52 , A61K31/155 , A61K31/522 , A61K47/14 , A61K47/26 , A61K47/32 , A61K47/36 , A61K47/38 , A61P3/10 , A61P7/02 , A61P15/18 , A61P25/00 , A61P29/00 , A61P31/04 , A61P31/10 , A61P31/12
CPC分类号： A61K9/5078
摘要： The invention relates to a microparticulate system for the delayed and controlled release of active principles (AP) whose absorption window in vivo is essentially limited to the upper parts of the gastrointestinal tract, this system being intended for oral administration. The object of the invention is to provide a system ensuring that the AP is released with certainty by means of a dual mechanism of “time-dependent” and “pH-dependent” release. To achieve this object, the invention proposes a multimicrocapsular oral galenical form which is designed so as to guarantee therapeutic efficacy, and in which the release of the AP is governed by a dual release triggering mechanism that is “time-triggering” and “pH-triggering”. This system consists of microcapsules (200 to 600 μm) comprising a core of AP coated with a film (maximum 40% by weight) comprising a hydrophilic polymer A (Eudragit® L) and a hydrophobic compound B (vegetable wax, melting point=40-90° C.), B/A being between 0.2 and 1.5. These microcapsules have a dissolution behavior in vitro such that, at a constant pH of 1.4, a latency phase of between 1 and 5 hours is observed, followed by a release of the AP, and such that the change from pH 1.4 to pH 6.8 results in a release of the AP without a latency period in vitro.
摘要翻译：本发明涉及一种用于延迟和控制释放活性成分（AP）的微粒体系，其活性成分在体内的吸收窗口基本上限于胃肠道的上部，该系统用于口服给药。本发明的目的是提供一种确保通过“时间依赖”和“依赖于pH”释放的双重机制确定地释放AP的系统。为了实现该目的，本发明提出了一种多微囊口服盖仑型，其设计以保证治疗功效，并且其中AP的释放由双时间触发机制（“触发时间”和“pH- 触发“。该系统由包含涂覆有包含亲水性聚合物A（EudragitL）和疏水性化合物B（植物蜡，熔点）的膜（最大40重量％））的AP芯组成的微胶囊（200至600μm） = 40-90℃），B / A在0.2和1.5之间。这些微胶囊在体外具有溶解行为，使得在1.4的恒定pH下，观察到1至5小时的潜伏期，随后释放AP，并且使得从pH1.4变为pH6.8的结果在AP的释放中没有潜伏期在体外。

30. 发明申请

US20160310420A1 CONTROLLED-RELEASE FLOATING PHARMACEUTICAL COMPOSITIONS 审中-公开
标题翻译：控制释放浮选药物组合物
公开(公告)号：US20160310420A1
公开(公告)日：2016-10-27
申请号：US15201000
申请日：2016-07-01
申请人： Catherine Castan , Philippe Caisse
发明人： Catherine Castan , Philippe Caisse
IPC分类号： A61K9/00 , A61K31/155 , A61K31/403 , A61K31/192 , A61K9/50 , A61K9/48
CPC分类号： A61K9/0065 , A61K9/4866 , A61K9/5015 , A61K9/5026 , A61K9/5031 , A61K9/5047 , A61K9/5078 , A61K31/155 , A61K31/192 , A61K31/403
摘要： The invention relates to a pharmaceutical composition comprising a plurality of controlled-release coated microparticles each comprising a floating core, on the surface of which is deposited a layer containing at least one active principle, said layer being covered with a controlled-release coating, characterized by the fact that said floating core is composed of cellulose acetate phthalate and has an apparent density of less than or equal to 0.6 g/mL and said coated microparticles have a density of less than or equal to 0.7 g/mL.
摘要翻译：本发明涉及一种药物组合物，其包含多个受控释放的包被的微粒，每个包含浮芯，其表面沉积包含至少一种活性成分的层，所述层被覆盖有控释膜，其特征在于所述浮芯由醋酸邻苯二甲酸纤维素组成，表观密度小于或等于0.6g / mL，所述涂布微粒的密度小于或等于0.7g / mL。

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