公开(公告)号：US10052289B2

公开(公告)日：2018-08-21

申请号：US12641773

申请日：2009-12-18

申请人： Rémi Meyrueix ,  Rafael Jorda ,  Gauthier Pouliquen ,  You-Ping Chan ,  Olivier Breyne

发明人： Rémi Meyrueix ,  Rafael Jorda ,  Gauthier Pouliquen ,  You-Ping Chan ,  Olivier Breyne

IPC分类号： A61K9/52 ,  A61K9/14 ,  A61K9/22 ,  A61K31/337 ,  A61K31/403 ,  A61K31/366 ,  A61K31/4418 ,  A61K31/496 ,  A61K38/13 ,  A61P35/00 ,  A61P37/00 ,  A61P31/10 ,  A61P9/12 ,  A61P3/06 ,  A61K9/50 ,  A61K9/51 ,  A61K47/34

CPC分类号： A61K9/5078 ,  A61K9/5015 ,  A61K9/5026 ,  A61K9/5146 ,  A61K47/34

摘要： The present invention relates to a composition comprising at least one active ingredient with low aqueous solubility, said active ingredient being present therein in a form noncovalently associated with nanoparticles formed by at least one POM polymer of formula (I), and in which said active ingredient is present in a proportion of at least 5 μmol/g of POM.It is also directed towards the use of such nanoparticles, noncovalently associated with an active ingredient, with a view to increasing the aqueous solubilization of said active ingredient.

公开(公告)号：US20120294832A1

公开(公告)日：2012-11-22

申请号：US13472675

申请日：2012-05-16

申请人： Gauthier Pouliquen ,  You-Ping Chan ,  Rémi Meyrueix ,  David Chognot ,  Roger Kravtzoff

发明人： Gauthier Pouliquen ,  You-Ping Chan ,  Rémi Meyrueix ,  David Chognot ,  Roger Kravtzoff

IPC分类号： A61K38/21

CPC分类号： A61K38/212 ,  A61K9/0019 ,  A61K9/19 ,  A61K47/34

摘要： The present invention relates to a novel solid composition, useful for treating hepatitis, in particular hepatitis C, comprising at least one interferon alpha and at least one grafted poly(glutamic acid) having an average molar mass ranging from 26,000 to 40,000 g/mol, preferably approximately 33,000 g/mol and carrying grafts of alpha-tocopherol at an average molar grafting rate ranging from 4.5 to 5.5%, preferably approximately 5%, the interferon alpha and said grafted poly(glutamic acid) being present in a grafted poly(glutamic acid)/interferon alpha weight ratio ranging from 21 to 125.It also relates to the use of such a solid composition for the preparation of a liquid composition by the addition of an aqueous liquid.

摘要翻译： 本发明涉及一种用于治疗肝炎，特别是丙型肝炎的新型固体组合物，其包含至少一种干扰素α和至少一种平均摩尔质量范围为26,000至40,000g / mol的接枝聚（谷氨酸） 优选约33,000g / mol，并且以干扰素α和所述接枝的聚（谷氨酸）存在于接枝的聚（谷氨酸）中的平均摩尔接枝率为4.5至5.5％，优选约5％的载体接种α-生育酚 酸）/干扰素α重量比范围为21至125.还涉及使用这种固体组合物通过加入水性液体制备液体组合物。

公开(公告)号：US08084045B2

公开(公告)日：2011-12-27

申请号：US10580023

申请日：2004-11-19

申请人： Gauthier Pouliquen ,  Olivier Soula ,  Rémi Meyrueix ,  Florence Nicolas

发明人： Gauthier Pouliquen ,  Olivier Soula ,  Rémi Meyrueix ,  Florence Nicolas

IPC分类号： A61K9/32 ,  A61K9/52 ,  A61K9/54 ,  A61K9/64 ,  A61K38/00

CPC分类号： A61K9/0024 ,  A61K38/2013 ,  A61K38/212 ,  A61K47/42 ,  A61K47/645 ,  A61K51/1217

摘要： The present invention relates to novel pharmaceutical formulations based on stable, fluid aqueous colloidal suspensions for the prolonged release of active principle(s), particularly protein active principle(s), and to the applications, especially therapeutic applications, of these formulations.The object of the invention is to propose a fluid pharmaceutical formulation for the prolonged release of active principle(s) that makes it possible, after parenteral injection, to increase significantly the in vivo release time of a therapeutic protein while at the same time reducing the plasma concentration peak of the active protein, said formulation furthermore being stable on storage and also being biocompatible, biodegradable, non-toxic and non-immunogenic and having a good local tolerance.The formulation according to the invention is an aqueous colloidal suspension of low viscosity based on submicronic particles of water-soluble biodegradable polymer PO carrying hydrophobic groups (HG), said particles being non-covalently associated with at least one active principle (AP) and forming a gelled deposit at the injection site, this gelling being caused by a protein present in the physiological medium.

摘要翻译： 本发明涉及基于用于延长释放活性成分（特别是蛋白质活性成分）的稳定的流体水性胶体悬浮液以及这些制剂的应用，特别是治疗应用的新型药物制剂。 本发明的目的是提出用于延长释放活性成分的流体药物制剂，其使得在胃肠外注射后可以显着增加治疗性蛋白质的体内释放时间，同时减少 活性蛋白质的血浆浓度峰值，所述制剂还在储存时稳定，并且还具有生物相容性，可生物降解，无毒和非免疫原性并且具有良好的局部耐受性。 根据本发明的制剂是基于具有疏水基团（HG）的水溶性生物可降解聚合物PO的亚微米颗粒的低粘度水性胶体悬浮液，所述颗粒与至少一种活性成分（AP）非共价缔合并形成 在注射部位的凝胶沉积物，这种胶凝是由存在于生理介质中的蛋白质引起的。

公开(公告)号：US20100021549A1

公开(公告)日：2010-01-28

申请号：US12509109

申请日：2009-07-24

申请人： Rémi Meyrueix ,  Rafael Jorda ,  Anne-Sophie Daviaud ,  Alain Constancis

发明人： Rémi Meyrueix ,  Rafael Jorda ,  Anne-Sophie Daviaud ,  Alain Constancis

IPC分类号： A61K9/14 ,  A61K38/02 ,  A61K38/28 ,  A61K8/73 ,  A61K8/64 ,  A61K31/715 ,  A61K31/7088

CPC分类号： A61K9/5078 ,  A61K8/11 ,  A61K8/64 ,  A61K8/731 ,  A61K8/8135 ,  A61K8/8147 ,  A61K8/8152 ,  A61K38/00 ,  A61K2800/412 ,  A61Q19/00

摘要： The present invention aims to propose novel microparticle oral forms for the modified release of active ingredient(s), in particular protein or peptide in nature. It also relates to the uses, in particular therapeutic or cosmetic, of these microparticle oral forms.

摘要翻译： 本发明的目的是提出新型的微粒口服形式用于活性成分（特别是蛋白质或肽）的改性释放。 它还涉及这些微粒口服形式的用途，特别是治疗或化妆品。

公开(公告)号：US20110117205A1

公开(公告)日：2011-05-19

申请号：US13014137

申请日：2011-01-26

申请人： Catherine Castan ,  Florence Guimberteau ,  Rémi Meyrueix

发明人： Catherine Castan ,  Florence Guimberteau ,  Rémi Meyrueix

IPC分类号： A61K9/62 ,  A61K9/58 ,  A61K31/522 ,  A61K31/58 ,  A61K31/155

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 relates to liquid pharmaceutical formulations for oral administration with the modified release of active principle(s), excluding amoxicillin, said formulations consisting of suspensions of coated particles of active principles (microcapsules). According to the invention, the microcapsules constituting the disperse phase of the suspension are designed to allow the modified release of the active principle(s) according to a profile that does not change during the storage of the liquid suspension. To do this the inventors propose the selection of a specific coating composition for the microcapsules which consists of at least four components that allow these microcapsules to be stored in water without modifying their properties of modified release of the active principle, this liquid phase furthermore being saturated with active principle(s).

摘要翻译： 本发明涉及用于口服给药的液体药物制剂，其具有活性成分的释放，不包括阿莫西林，所述制剂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被设计成允许根据在液体悬浮液储存过程中不改变的分布的活性成分的改性释放。 为此，本发明人提出了选择用于微胶囊的特定涂料组合物，其由至少四种组分组成，这些组分允许这些微胶囊储存在水中而不改变其活性成分的改性释放性质，该液相还饱和 具有积极的原则。

公开(公告)号：US07910133B2

公开(公告)日：2011-03-22

申请号：US10510621

申请日：2003-04-07

申请人： Catherine Castan ,  Florence Guimberteau ,  Rémi Meyrueix

发明人： Catherine Castan ,  Florence Guimberteau ,  Rémi Meyrueix

IPC分类号： A61K9/14 ,  A61K9/16 ,  A61K9/40

CPC分类号： A61K9/5015 ,  A61K9/5026 ,  A61K9/5047 ,  A61K31/43

摘要： The invention relates to liquid pharmaceutical formulations for oral administration with the modified release of amoxicillin, said formulations consisting of suspensions of coated particles of amoxicillin (microcapsules). According to the invention, the microcapsules constituting the disperse phase of the suspension are designed to allow the modified release of the amoxicillin according to a profile that does not change during the storage of the liquid suspension. To do this the inventors propose the selection of a specific coating composition for the microcapsules which consists of at least four components that allow these microcapsules to be stored in water without modifying their properties of modified release of the amoxicillin, this liquid phase furthermore being saturated with amoxicillin.

摘要翻译： 本发明涉及用于阿莫西林的改性释放的口服给药的液体药物制剂，所述制剂由阿莫西林（微胶囊）的包衣颗粒的悬浮液组成。 根据本发明，构成悬浮液分散相的微胶囊被设计成允许根据在液体悬浮液储存过程中不变化的分布来改变阿莫西林的释放。 为了做到这一点，发明人提出了选择用于微胶囊的特定涂料组合物，其由至少四种组分组成，这些组分允许这些微胶囊储存在水中而不改变其改性释放的阿莫西林的性质，此液相还饱和 阿莫西林

公开(公告)号：US06500783B1

公开(公告)日：2002-12-31

申请号：US09451283

申请日：1999-11-30

申请人： Nathan J. Bryson ,  Olivier Soula ,  Alain J. L. Lemercier ,  Rémi Meyrueix ,  Gérard G. Soula

发明人： Nathan J. Bryson ,  Olivier Soula ,  Alain J. L. Lemercier ,  Rémi Meyrueix ,  Gérard G. Soula

IPC分类号： A01N2530

CPC分类号： A01N57/20 ,  A01N25/30 ,  A01N2300/00

摘要： A plant treatment composition for application of an anionic exogenous chemical substance such as glyphosate to foliage of a plant is provided. The composition comprises, in addition to the exogenous chemical substance, one or more amine compound(s) each having a number n of protonatable amino groups, n being at least 1, and having the formula (I) R—NR—((CH2)p—CHR4—NR)q—R  (I) wherein q is an integer of 0 to 9, each p is independently an integer of 1 to 5, each R4 group is independently hydrogen or a C1-5 alkyl group, and R groups are independently selected from hydrogen, C1-5 hydrocarbyl groups and linear or branched, saturated or unsaturated C6-22 hydrocarbyl or acyl chains that are (a) unsubstituted or substituted at one or a plurality of carbon atoms with a functional group independently selected from hydroxyl, carboxy, carbamyl, mercapto and cyano groups and (b) uninterrupted or interrupted by one or a plurality of functional linkages independently selected from ether, thioether, sulfoxide, ester, thioester and amide linkages, and terminated by an uninterrupted hydrocarbyl segment having at least 6 carbon atoms; with the proviso that one to three R groups are such C6-22 hydrocarbyl or acyl chains, of which at least one is so substituted and/or interrupted. The exogenous chemical substance and amine compound(s) of formula (I) are dissolved or dispersed in an agronomically acceptable liquid carrier, preferably water. Also provided are a liquid concentrate composition which, upon dilution with water, forms a plant treatment composition, and a process for making such a liquid concentrate composition. Plant treatment compositions of the invention are useful for eliciting a biological activity, for example herbicidal activity, in a plant.

摘要翻译： 提供了一种用于将阴离子外源化学物质如草甘膦施用于植物叶子的植物处理组合物。 该组合物除了外源化学物质外，还包含一种或多种各自具有n个可质子化氨基的胺化合物，n至少为1，并且具有式（I），其中q为整数0 至9，每个p独立地为1至5的整数，每个R 4基团独立地为氢或C 1-5烷基，R基团独立地选自氢，C 1-5烃基和直链或支链，饱和或不饱和的 （a）未被取代或在一个或多个碳原子上具有独立选自羟基，羧基，氨基甲酰基，巯基和氰基的官能团取代的酰基，和（b）不间断或被一个或多个 多个功能键，独立地选自醚，硫醚，亚砜，酯，硫酯和酰胺键，并由具有至少6个碳原子的不间断烃基链段封端; 条件是一至三个R基团是这样的C 6-22烃基或酰基链，其中至少一个如此取代和/或中断。 将式（I）的外源化学物质和胺化合物溶解或分散在农业上可接受的液体载体中，优选水。 还提供了液体浓缩组合物，其在用水稀释时形成植物处理组合物，以及制备这种液体浓缩物组合物的方法。 本发明的植物处理组合物可用于在植物中引发生物活性，如除草活性。

公开(公告)号：US08101209B2

公开(公告)日：2012-01-24

申请号：US10826690

申请日：2004-04-19

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

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

IPC分类号： A61K9/16 ,  A61K9/50

CPC分类号： A61K9/5078 ,  A61K9/5015 ,  A61K9/5026 ,  Y10S514/951 ,  Y10S514/963 ,  Y10S514/965

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 comprises 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，其活性成分体系中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“。 该系统包括微胶囊（200至600μm），其包含涂覆有包含亲水性聚合物A（Eudragit L）和疏水化合物B（植物蜡，熔点= 40）的膜（最大40重量％））的AP芯 -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：US07906145B2

公开(公告)日：2011-03-15

申请号：US10510643

申请日：2003-04-07

申请人： Catherine Castan ,  Florence Guimberteau ,  Rémi Meyrueix

发明人： Catherine Castan ,  Florence Guimberteau ,  Rémi Meyrueix

IPC分类号： A61K9/14 ,  A61K9/16 ,  A61K9/40

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 ）。

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。