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1. 发明授权

US07485294B2 Galenic pectinate formulation for colon-targeted delivery of antibiotic-inactivating enzymes and method of use thereof 失效
标题翻译：用于结肠靶向递送抗生素灭活酶的加仑果胶配方及其使用方法
公开(公告)号：US07485294B2
公开(公告)日：2009-02-03
申请号：US10524318
申请日：2003-08-06
申请人： Sandrine Bourgeois , Elias Fattal , Antoine Andremont , Patrick Couvreur
发明人： Sandrine Bourgeois , Elias Fattal , Antoine Andremont , Patrick Couvreur
IPC分类号： C12N9/00 , C12N9/14 , C12N9/18 , A61K38/43 , A61K38/46 , A01N63/00
CPC分类号： A61K9/5036 , A61K9/1652
摘要： Forms of colonic delivery suited to be used orally and designed for colonic delivery of active ingredients selected from the group comprising enzymes capable of inactivating macrolide antibiotics and related compounds, enzymes capable of inactivating quinolones, and β-lactamases.
摘要翻译：适于口服使用并设计用于结肠递送活性成分的结肠递送的形式，所述活性成分选自能够灭活大环内酯类抗生素和相关化合物的酶，能够灭活喹诺酮和β-内酰胺酶的酶。

2. 发明授权

US07833765B2 Galenic formulation for colon-targeted delivery of active ingredients 有权
标题翻译：用于结肠靶向递送活性成分的Galenic制剂
公开(公告)号：US07833765B2
公开(公告)日：2010-11-16
申请号：US12345647
申请日：2008-12-29
申请人： Sandrine Bourgeois , Elias Fattal , Antoine Andremont , Patrick Couvreur
发明人： Sandrine Bourgeois , Elias Fattal , Antoine Andremont , Patrick Couvreur
IPC分类号： C12N9/00 , C12N9/18 , C12N9/86 , A61K38/43 , A61K38/54 , A61K38/46 , A61K9/50
CPC分类号： A61K9/5036 , A61K9/1652
摘要： The invention concerns multiparticulate galenic formulations for oral administration and designed for colon targeted delivery of active principles selected from the group comprising enzymes capable of inactivating macrolides and the like, enzymes capable of inactivating quinolones and β-lactamases.
摘要翻译：本发明涉及用于口服给药的多颗粒盖仑制剂，并且设计用于结肠靶向递送活性成分，所述活性成分选自能够灭活大环内酯等的酶，能够灭活喹诺酮和β-内酰胺酶的酶。

3. 发明申请

US20050249716A1 Galenic formulation for colon targeted delivery of active principles 失效
标题翻译：用于结肠靶向递送活性成分的Galenic制剂
公开(公告)号：US20050249716A1
公开(公告)日：2005-11-10
申请号：US10524318
申请日：2003-08-06
申请人： Sandrine Bourgeois , Elias Fattal , Antoine Andremont , Patrick Couvreur
发明人： Sandrine Bourgeois , Elias Fattal , Antoine Andremont , Patrick Couvreur
IPC分类号： A61K9/16 , A61K9/50 , A61K38/46 , A61K9/20
CPC分类号： A61K9/5036 , A61K9/1652
摘要： Forms of colonic delivery suited to be used orally and designed for colonic delivery of active ingredients selected from the group comprising enzymes capable of inactivating macrolide antibiotics and related compounds, enzymes capable of inactivating quinolones, and β-lactamases.
摘要翻译：适于口服使用并设计用于结肠递送活性成分的结肠递送形式，所述活性成分选自能够灭活大环内酯类抗生素和相关化合物的酶，能够灭活喹诺酮和β-内酰胺酶的酶。

4. 发明申请

US20090162339A1 GALENIC FORMULATION FOR COLON-TARGETED DELIVERY OF ACTIVE INGREDIENTS 有权
标题翻译：用于定向递送活性成分的GALENIC配方
公开(公告)号：US20090162339A1
公开(公告)日：2009-06-25
申请号：US12345647
申请日：2008-12-29
申请人： Sandrine Bourgeois , Elias Fattal , Antoine Andremont , Patrick Couvreur
发明人： Sandrine Bourgeois , Elias Fattal , Antoine Andremont , Patrick Couvreur
IPC分类号： A61K38/46 , A61P1/00
CPC分类号： A61K9/5036 , A61K9/1652
摘要： The invention concerns multiparticulate galenic formulations for oral administration and designed for colon targeted delivery of active principles selected from the group comprising enzymes capable of inactivating macrolides and the like, enzymes capable of inactivating quinolones and β-lactamases.
摘要翻译：本发明涉及用于口服给药的多颗粒盖仑制剂，并且设计用于结肠靶向递送活性成分，所述活性成分选自能够灭活大环内酯类的酶，能够灭活喹诺酮和β-内酰胺酶的酶。

5. 发明申请

US20080317666A1 Colonic Delivery of Active Agents 审中-公开
标题翻译：活性剂的结肠递送
公开(公告)号：US20080317666A1
公开(公告)日：2008-12-25
申请号：US11628832
申请日：2006-02-09
申请人： Elias Fattal , Antoine Andremont , Patrick Couvreur , Sandrine Bourgeois
发明人： Elias Fattal , Antoine Andremont , Patrick Couvreur , Sandrine Bourgeois
IPC分类号： A61K9/00 , A61K49/00 , A61K51/12 , A61P1/00
CPC分类号： A61K9/1652 , A61K9/1682 , A61K31/155 , A61K38/465 , A61K38/47 , C12Y305/02006 , G01N2800/065
摘要： Drug delivery devices that are orally administered, and that release active ingredients in the colon, are disclosed. In one embodiment, the active ingredients are those that inactivate antibiotics, such as macrolides, quinolones and beta-lactam containing antibiotics. One example of a suitable active agent is an enzyme such as beta-lactamases. In another embodiment, the active agents are those that specifically treat colonic disorders, such as Chrohn's Disease, irritable bowel syndrome, ulcerative colitis, colorectal cancer or constipation. The drug delivery devices are in the form of beads of pectin, crosslinked with calcium and reticulated with polyethyleneimine. The high crosslink density of the polyethyleneimine is believed to stabilize the pectin beads for a sufficient amount of time such that a substantial amount of the active ingredients can be administered directly to the colon. Advantageously, the amount of polyethyleneimine is sufficient to allow a substantial portion of the pectin beads to pass through the gastrointestinal tract to the colon without releasing the active agent, and is also sufficient such that the pectin beads are sufficiently degraded in the colon to release an effective amount of the active agent.
摘要翻译：公开了口服给药并且释放结肠中活性成分的药物输送装置。在一个实施方案中，活性成分是使抗生素失活的成分，例如大环内酯类，喹诺酮类和含β-内酰胺类的抗生素。合适的活性剂的一个实例是酶如β-内酰胺酶。在另一个实施方案中，活性剂是特异性治疗结肠疾病如克罗恩病，肠易激综合征，溃疡性结肠炎，结肠直肠癌或便秘的那些。药物递送装置是果胶珠的形式，与钙交联并用聚乙烯亚胺网化。据信聚乙烯亚胺的高交联密度使果胶珠稳定足够的时间，使得大量的活性成分可以直接施用于结肠。有利地，聚乙烯亚胺的量足以允许大部分果胶珠通过胃肠道至结肠而不释放活性剂，并且也足够使得果胶珠在结肠中充分降解以释放有效量的活性剂。

6. 发明授权

US08388984B2 Site-specific intestinal delivery of adsorbents, alone or in combination with degrading molecules 有权
标题翻译：吸附剂的位点特异性肠递送，单独或与降解分子组合
公开(公告)号：US08388984B2
公开(公告)日：2013-03-05
申请号：US13232976
申请日：2011-09-14
申请人： Helene-Celine Huguet , Antoine Andremont , Nicolas Tsapis , Elias Fattal
发明人： Helene-Celine Huguet , Antoine Andremont , Nicolas Tsapis , Elias Fattal
IPC分类号： A61K9/00
CPC分类号： A61K9/1611 , A61K9/10 , A61K9/1641 , A61K9/1652 , A61K9/5026 , A61K33/06 , A61K33/44 , A61K45/06 , A61K47/10 , A61K2300/00
摘要： Compositions which deliver adsorbents, alone or in combination with active drug “degrading molecules,” in a site-specific manner to the intestine, and which eliminate or at least lower the concentration of residual unwanted material within the intestine, and methods of treatment using the compositions, are disclosed. The compositions are ideally designed to specifically release the adsorbents in a programmed manner at a specific site of the intestinal tract. Programmed delivery prevents adsorbents from interfering with the normal absorption process of a given molecule after oral absorption, until it reaches the lower part of the small intestine. The compositions can be used to adsorb, and therefore remove, any residual drug, metabolite thereof, or bacterial toxin after oral or parenteral administration which would otherwise cause adverse effects in the lower intestine and/or colon.
摘要翻译：将单独或与活性药物降解分子组合的吸附剂以位点特异性方式递送到肠中并且消除或至少降低肠内残留不需要的物质的浓度的组合物以及使用该组合物的治疗方法，被披露。该组合物理想地设计成以编程方式在肠道的特定部位特异性释放吸附剂。程序传递防止吸附剂在口服吸收后干扰给定分子的正常吸收过程，直到其到达小肠的下部。组合物可以用于吸收并因此去除在口服或肠胃外给药后的任何残留药物，其代谢物或细菌毒素，否则会在下肠和/或结肠中引起不良反应。

7. 发明授权

US08106000B2 Colonic delivery of adsorbents 有权
标题翻译：结肠传递吸附剂
公开(公告)号：US08106000B2
公开(公告)日：2012-01-31
申请号：US11920713
申请日：2006-05-18
申请人： Helene-Celine Huguet , Elias Fattal , Antoine Andremont , Nicolas Tsapis
发明人： Helene-Celine Huguet , Elias Fattal , Antoine Andremont , Nicolas Tsapis
IPC分类号： A01N61/00
CPC分类号： A61K9/1652 , A61K9/16 , A61K9/5036 , A61K47/36
摘要： Orally administrable, site-specific (colonic), particulate delivery systems including adsorbents are disclosed. When delivered specifically to the colon, they can remove various substances present in, or as they reach, the colon. Methods of treatment using the delivery systems, and methods of preparing the delivery systems, are also disclosed. The particulate delivery systems are based on adsorbent matrices encapsulated into and/or onto particles, which selectively deliver the adsorbents to the colon. Representative drug delivery devices include pectin beads, which can optionally be crosslinked with metal ions such as zinc and/or calcium. The delivery system protects the adsorbent and prevents its adsorbing effect in the upper gastro-intestinal (GI) tract. When the particles are made from pectin, and the beads are administered to the colon, specific pectinolytic enzymes in the colon degrade the pectin, allowing the adsorbent to be released and to be fully active. Antibiotics, toxins, and other absorbable substances present in the colon will then be inactivated by adsorption into or onto the adsorbent.
摘要翻译：可口服给药，特异性（结肠），包括吸附剂的颗粒递送系统。当特异性地输送到结肠时，它们可以去除结肠中存在的或当它们到达的各种物质。还公开了使用递送系统的治疗方法和制备递送系统的方法。颗粒递送系统基于封装在颗粒中和/或上的吸附剂基质，其选择性地将吸附剂递送到结肠。代表性的药物递送装置包括果胶珠，其可任选地与金属离子如锌和/或钙交联。递送系统保护吸附剂并防止其在上胃肠（GI）道中的吸附作用。当颗粒由果胶制成，并且将珠子施用于结肠时，结肠中的特异性果胶分解酶降解果胶，允许吸附剂被释放并且完全活性。然后，存在于结肠中的抗生素，毒素和其它可吸收物质将通过吸附到吸附剂中或其上而被灭活。

8. 发明申请

US20090324568A1 Colonic Delivery of Adsorbents 有权
标题翻译：结肠递送吸附剂
公开(公告)号：US20090324568A1
公开(公告)日：2009-12-31
申请号：US11920713
申请日：2006-05-18
申请人： Helene-Celine Huguet , Elias Fattal , Antoine Andremont , Nicolas Tsapis
发明人： Helene-Celine Huguet , Elias Fattal , Antoine Andremont , Nicolas Tsapis
IPC分类号： A61K38/43 , A61K33/44 , A61K33/00 , A61K47/36
CPC分类号： A61K9/1652 , A61K9/16 , A61K9/5036 , A61K47/36
摘要： Orally administrable, site-specific (colonic), particulate delivery systems including adsorbents are disclosed. When delivered specifically to the colon, they can remove various substances present in, or as they reach, the colon. Methods of treatment using the delivery systems, and methods of preparing the delivery systems, are also disclosed. The particulate delivery systems are based on adsorbent matrices encapsulated into and/or onto particles, which selectively deliver the adsorbents to the colon. Representative drug delivery devices include pectin beads, which can optionally be crosslinked with metal ions such as zinc and/or calcium. The delivery system protects the adsorbent and prevents its adsorbing effect in the upper gastro-intestinal (GI) tract. When the particles are made from pectin, and the beads are administered to the colon, specific pectinolytic enzymes in the colon degrade the pectin, allowing the adsorbent to be released and to be fully active. Antibiotics, toxins, and other absorbable substances present in the colon will then be inactivated by adsorption into or onto the adsorbent.
摘要翻译：可口服给药，特异性（结肠），包括吸附剂的颗粒递送系统。当特异性地输送到结肠时，它们可以去除结肠中存在的或当它们到达的各种物质。还公开了使用递送系统的治疗方法和制备递送系统的方法。颗粒递送系统基于封装在颗粒中和/或上的吸附剂基质，其选择性地将吸附剂递送到结肠。代表性的药物递送装置包括果胶珠，其可任选地与金属离子如锌和/或钙交联。递送系统保护吸附剂并防止其在上胃肠（GI）道中的吸附作用。当颗粒由果胶制成，并且将珠子施用于结肠时，结肠中的特异性果胶分解酶降解果胶，允许吸附剂被释放并且完全活性。然后，存在于结肠中的抗生素，毒素和其它可吸收物质将通过吸附到吸附剂中或其上而被灭活。

9. 发明申请

US20120107367A1 Site-Specific Intestinal Delivery of Adsorbents, Alone or in Combination with Degrading Molecules 有权
标题翻译：吸附剂，单独或与降解分子组合的位点特异性肠递送
公开(公告)号：US20120107367A1
公开(公告)日：2012-05-03
申请号：US13232976
申请日：2011-09-14
申请人： Helene-Celine Huguet , Antoine Andremont , Nicolas Tsapis , Elias Fattal
发明人： Helene-Celine Huguet , Antoine Andremont , Nicolas Tsapis , Elias Fattal
IPC分类号： A61K9/00 , A61K33/00 , A61P1/00 , A61K33/06 , A61K31/74 , A61K33/44 , A61K33/12
CPC分类号： A61K9/1611 , A61K9/10 , A61K9/1641 , A61K9/1652 , A61K9/5026 , A61K33/06 , A61K33/44 , A61K45/06 , A61K47/10 , A61K2300/00
摘要： Compositions which deliver adsorbents, alone or in combination with active drug “degrading molecules,” in a site-specific manner to the intestine, and which eliminate or at least lower the concentration of residual unwanted material within the intestine, and methods of treatment using the compositions, are disclosed. The compositions are ideally designed to specifically release the adsorbents in a programmed manner at a specific site of the intestinal tract. Programmed delivery prevents adsorbents from interfering with the normal absorption process of a given molecule after oral absorption, until it reaches the lower part of the small intestine. The compositions can be used to adsorb, and therefore remove, any residual drug, metabolite thereof, or bacterial toxin after oral or parenteral administration which would otherwise cause adverse effects in the lower intestine and/or colon.
摘要翻译：将单独或与活性药物“降解分子”组合的吸附剂的组合物以位点特异性方式递送到肠道，并且消除或至少降低肠内残留不需要的物质的浓度，以及使用组合物。该组合物理想地设计成以编程方式在肠道的特定部位特异性释放吸附剂。程序传递防止吸附剂在口服吸收后干扰给定分子的正常吸收过程，直到其到达小肠的下部。组合物可以用于吸收并因此去除在口服或肠胃外给药后的任何残留药物，其代谢物或细菌毒素，否则会在下肠和/或结肠中引起不良反应。

10. 发明授权

US08048413B2 Site-specific intestinal delivery of adsorbents, alone or in combination with degrading molecules 有权
标题翻译：吸附剂的位点特异性肠递送，单独或与降解分子组合
公开(公告)号：US08048413B2
公开(公告)日：2011-11-01
申请号：US11804259
申请日：2007-05-17
申请人： Helene Huguet , Antoine Andremont , Nicolas Tsapis , Elias Fattal
发明人： Helene Huguet , Antoine Andremont , Nicolas Tsapis , Elias Fattal
IPC分类号： A01N59/00
CPC分类号： A61K9/1611 , A61K9/10 , A61K9/1641 , A61K9/1652 , A61K9/5026 , A61K33/06 , A61K33/44 , A61K45/06 , A61K47/10 , A61K2300/00
摘要： Compositions which deliver adsorbents, alone or in combination with active drug “degrading molecules,” in a site-specific manner to the intestine, and which eliminate or at least lower the concentration of residual unwanted material within the intestine, are disclosed. Methods of treatment using the compositions are also disclosed. The material to be eliminated can include residual active antibiotics, metabolites, bacterial or other toxins, and drugs which cause side effects in the gastrointestinal tract. The adsorbents can be formulated in capsules, tablets or any acceptable pharmaceutical composition, and are ideally designed to specifically release the adsorbents in a programmed manner at a specific site of the intestinal tract. The programmed delivery prevents adsorbents from interfering with the normal absorption process of a given molecule after oral absorption, until it reaches the lower part of the small intestine. The compositions can be used to adsorb, and therefore remove, any residual drug, metabolite thereof, or bacterial toxin after oral or parenteral administration which would otherwise cause adverse effects in the lower intestine and/or colon.
摘要翻译：公开了以位点特异性方式将吸附剂单独或与活性药物“降解分子”组合的组合物，其消除或至少降低了肠内残留的不需要的物质的浓度。还公开了使用该组合物的治疗方法。要消除的物质可以包括残留的活性抗生素，代谢物，细菌或其他毒素，以及在胃肠道中引起副作用的药物。吸附剂可以配制成胶囊，片剂或任何可接受的药物组合物，并且理想地设计为以编程方式在肠道的特定部位特异性释放吸附剂。编程的递送防止吸附剂在口服吸收后干扰给定分子的正常吸收过程，直到其到达小肠的下部。组合物可以用于吸收并因此去除在口服或肠胃外给药后的任何残留药物，其代谢物或细菌毒素，否则会在下肠和/或结肠中引起不良反应。

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