公开(公告)号：US07879362B2

公开(公告)日：2011-02-01

申请号：US11723553

申请日：2007-03-21

申请人： Catherine Castan ,  Valerie Legrand ,  Rémi Meyrueix ,  Gérard Soula

发明人： Catherine Castan ,  Valerie Legrand ,  Rémi Meyrueix ,  Gérard Soula

IPC分类号： A61K9/16

CPC分类号： A61K9/5073 ,  A61K9/2081 ,  A61K9/4858 ,  A61K9/4866

摘要： The invention concerns a galenic system with prolonged/controlled release of the medicinal and/or nutritional active principle, for oral administration. The aim is to provide a system enabling to obtain with one single tolerable and acceptable dose of active principle, efficient therapeutic protection over 24 hours (increasing the bioabsorption time without affecting bioavailability). To achieve this, the invention provides a composition comprising two controlled release systems associated in series, namely: individualised coated particles (microcapsules) of active principle forming an internal phase, the coating comprising a film-forming polymer P1 (ethylcellulose), a nitrogenous polymer (polyvinylpyrrolidone), a softener (castor oil) and a lubricant (magnesium stearate), and an external phase of functional carriers: polyelectrolytic hydrophilic polymer: (alginate), neutral hydrophilic polymer (hydroxypropylmethylcellulose) and a gelling additive (calcium acetate), said composition spontaneously forming in the presence of water, a cohesive and stable composite macroscopic solid, wherein the external continuous phase is a gelled matrix including the active principle microcapsules. The invention is useful for delayed oral galenic formulation of metformin.

摘要翻译： 本发明涉及用于口服给药的药物和/或营养活性成分的延长/受控释放的盖仑系统。 目的是提供一种能够以一个单一可耐受和可接受剂量的活性成分获得的系统，24小时以上的有效治疗保护（增加生物吸收时间而不影响生物利用度）。 为了实现这一点，本发明提供了一种组合物，其包含两个串联的控制释放系统，即：形成内相的活性成分的单独的涂覆颗粒（微胶囊），该涂层包含成膜聚合物P1（乙基纤维素），含氮聚合物 （聚乙烯吡咯烷酮），软化剂（蓖麻油）和润滑剂（硬脂酸镁）和功能性载体的外相：聚电解亲水性聚合物：（藻酸盐），中性亲水性聚合物（羟丙基甲基纤维素）和胶凝添加剂（乙酸钙），所述 在水的存在下自发形成的组合物，粘性和稳定的复合宏观固体，其中外部连续相是包含活性成分微胶囊的凝胶基质。 本发明可用于二甲双胍延迟口服盖仑制剂。

公开(公告)号：US20070207214A1

公开(公告)日：2007-09-06

申请号：US11723553

申请日：2007-03-21

申请人： Catherine Castan ,  Valerie Legrand ,  Remi Meyrueix ,  Gerard Soula

发明人： Catherine Castan ,  Valerie Legrand ,  Remi Meyrueix ,  Gerard Soula

IPC分类号： A61K9/14

CPC分类号： A61K9/5073 ,  A61K9/2081 ,  A61K9/4858 ,  A61K9/4866

摘要： The invention concerns a galenic system with prolonged/controlled release of the medicinal and/or nutritional active principle, for oral administration. The aim is to provide a system enabling to obtain with one single tolerable and acceptable dose of active principle, efficient therapeutic protection over 24 hours (increasing the bioabsorption time without affecting bioavailability). To achieve this, the invention provides a composition comprising two controlled release systems associated in series, namely: individualised coated particles (microcapsules) of active principle forming an internal phase, the coating comprising a film-forming polymer P1 (ethylcellulose), a nitrogenous polymer (polyvinylpyrrolidone), a softener (castor oil) and a lubricant (magnesium stearate), and an external phase of functional carriers: polyelectrolytic hydrophilic polymer: (alginate), neutral hydrophilic polymer (hydroxypropylmethylcellulose) and a gelling additive (calcium acetate), said composition spontaneously forming in the presence of water, a cohesive and stable composite macroscopic solid, wherein the external continuous phase is a gelled matrix including the active principle microcapsules. The invention is useful for delayed oral galenic formulation of metformin.

摘要翻译： 本发明涉及用于口服给药的药物和/或营养活性成分的延长/受控释放的盖仑系统。 目的是提供一种能够以一个单一可耐受和可接受剂量的活性成分获得的系统，24小时以上的有效治疗保护（增加生物吸收时间而不影响生物利用度）。 为了实现这一目的，本发明提供了包含两个串联相关的控制释放系统的组合物，即形成内相的活性成分的单独的涂覆颗粒（微胶囊），该涂层包含成膜聚合物P 1 （乙基纤维素），含氮聚合物（聚乙烯吡咯烷酮），软化剂（蓖麻油）和润滑剂（硬脂酸镁）和功能性载体的外相：聚电解亲水性聚合物：（藻酸盐），中性亲水性聚合物（羟丙基甲基纤维素）和 凝胶添加剂（乙酸钙），所述组合物在水的存在下自发形成，粘性和稳定的复合宏观固体，其中外部连续相是包含活性成分微胶囊的凝胶基质。 本发明可用于二甲双胍延迟口服盖仑制剂。

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。

公开(公告)号：US20060228334A1

公开(公告)日：2006-10-12

申请号：US10520626

申请日：2003-07-10

申请人： Manuel Rosa-Calatrava ,  Philippe Leissner ,  Valerie Legrand

发明人： Manuel Rosa-Calatrava ,  Philippe Leissner ,  Valerie Legrand

IPC分类号： A61K48/00 ,  C12N15/861 ,  C12N7/00

CPC分类号： C12N15/86 ,  A61K38/00 ,  A61K48/00 ,  C07K14/005 ,  C12N7/00 ,  C12N2710/10322 ,  C12N2710/10343 ,  C12N2710/10345 ,  C12N2710/10362 ,  C12N2810/40

摘要： The present invention concerns a modified adenoviral fiber containing at least one mutation affecting one or more amino acid residue(s) of said adenoviral fiber interacting with at least one glycosaminoglycan and/or sialic acid-containing cellular receptor, as well as a trimer of such a modified adenoviral fiber. The present invention also relates to a DNA fragment, an expression vector encoding said modified adenoviral fiber. The present invention also concerns an adenoviral particle lacking a wild-type fiber and comprising the trimer of modified adenoviral fibers as well as a process for producing such an adenoviral particle. Theto present invention also provides a composition comprising such an adenoviral particle and the therapeutic use thereof.

摘要翻译： 本发明涉及一种修饰的腺病毒纤维，其包含影响与至少一种糖胺聚糖和/或含唾液酸的细胞受体相互作用的所述腺病毒纤维的一个或多个氨基酸残基的至少一个突变，以及这样的三聚体 改良的腺病毒纤维。 本发明还涉及DNA片段，编码所述修饰的腺病毒纤维的表达载体。 本发明还涉及缺乏野生型纤维并且包含修饰的腺病毒纤维的三聚体的腺病毒颗粒以及产生这种腺病毒颗粒的方法。 本发明还提供了包含这种腺病毒颗粒的组合物及其治疗用途。

公开(公告)号：US20060165808A1

公开(公告)日：2006-07-27

申请号：US10519641

申请日：2003-06-24

申请人： Bruno Huet De Barochez ,  Patrick Wuthrich ,  Valerie Legrand ,  Catherine Castan ,  Remi Meyrueix

发明人： Bruno Huet De Barochez ,  Patrick Wuthrich ,  Valerie Legrand ,  Catherine Castan ,  Remi Meyrueix

IPC分类号： A61K9/50 ,  A61K9/16

CPC分类号： A61K9/5015 ,  A61K9/5026 ,  A61K9/5078 ,  A61K31/405

摘要： The present invention relates to A microcapsule composition allowing the delayed and controlled release of perindopril, or of a pharmaceutically acceptable salt thereof, for administration by the oral route.

摘要翻译： 本发明涉及一种微胶囊组合物，其允许延迟和控制释放培哚普利或其药学上可接受的盐，用于通过口服途径施用。