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1. 发明授权

US10052289B2 Composition comprising an active agent with low aqueous solubility 有权
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.

2. 发明申请

US20110117205A1 ORAL PHARMACEUTICAL FORMULATION IN THE FORM OF AQUEOUS SUSPENSION FOR MODIFIED RELEASE OF ACTIVE PRINCIPLE(S) 有权
标题翻译：用于改性活性原料释放的水性悬浮剂形式的口服药物制剂（S）
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。

3. 发明申请

US20120294832A1 COMPOSITION COMPRISING INTERFERON ALPHA 审中-公开
标题翻译：包含干扰素的组合物
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。

4. 发明授权

US08101209B2 Microparticulate oral galenical form for the delayed and controlled release of pharmaceutical active principles 有权
标题翻译：用于延迟和控制释放药物活性成分的微孔口服盖仑形式
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。

5. 发明授权

US07906145B2 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：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）。

6. 发明授权

US07879362B2 Oral pharmaceutical compositions with controlled release and prolonged absorption 有权
标题翻译：具有控制释放和延长吸收的口服药物组合物
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。

7. 发明申请

US20100178337A1 Composition comprising an active agent with low aqueous solubility 审中-公开
标题翻译：组合物，其含有低溶解度的活性剂
公开(公告)号：US20100178337A1
公开(公告)日：2010-07-15
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
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.
摘要翻译：本发明涉及包含至少一种具有低溶解度的活性成分的组合物，所述活性成分以与式（I）的至少一种POM聚合物形成的纳米颗粒非共价结合的形式存在，其中所述活性成分以至少5μmol/ g的POM的比例存在。还涉及使用与活性成分非共价结合的这种纳米颗粒，以增加所述活性成分的水溶性。

8. 发明申请

US20100068291A1 Oral Medicament Based on a Proton Pump Inhibitor 审中-公开
标题翻译：基于质子泵抑制剂的口服药物
公开(公告)号：US20100068291A1
公开(公告)日：2010-03-18
申请号：US11920278
申请日：2006-05-15
申请人： Philippe CAISSE , Catherine CASTAN , Rémi MEYRUEIX , Gérard SOULA
发明人： Philippe CAISSE , Catherine CASTAN , Rémi MEYRUEIX , Gérard SOULA
IPC分类号： A61K9/50 , A61K31/4439 , A61K31/426 , A61K31/4164 , A61K31/341 , A61K47/02 , A61K47/06
CPC分类号： A61K9/5047 , A61K9/5015 , A61K9/5026 , A61K31/00 , A61K31/4184 , A61K31/4439
摘要： The invention relates to oral medicaments having a modified release of proton pump inhibitors (PPI's) that are, in particular, useful in preventing and treating gastrointestinal disorders. The aim of the invention is to provide a novel oral medicament based on PPI's ideally having all or some of the following characteristics: a) quickly providing relief to the patient by increasing the gastric pH after oral administration of the medicament; b) accelerating the recovery of patients while maintaining this increase in the gastric pH for as long as possible after oral administration of the medicament and, in particular, during the night; c) improving the observance of the treatment and the comfort of the patient by taking the medicament once daily. To this end, the microcapsules of the invention, preferably non-enteric, are constituted of PPI microparticles coated with ethyl cellulose, an ammonio methacrylate copolymer (Eudragit® RL 100), polyvinylpyrrolidone, castor oil and polyoxyethylenated hydrogenated castor oil (40). This medicament is designed so that after its ingestion for a once daily administration, it makes it possible to maintain, from the first day of treatment onward, an average gastric pH, between 0 and 24 h, of greater than or equal to the average gastric pH between 0 and 24 h obtained by an enteric oral medicament having a reference* immediate release, administered under the same conditions. The invention also relates to these microcapsules per se.
摘要翻译：本发明涉及具有特别可用于预防和治疗胃肠道疾病的质子泵抑制剂（PPI's）的改良释放的口服药物。本发明的目的是提供一种基于PPI的新型口服药物，其理想地具有以下所有或一些特征：a）通过在口服给药药物后增加胃pH，快速地向患者提供缓解; b）加速患者的恢复，同时在药物口服给药后，尽可能长时间地保持胃pH的增加，特别是在夜间; c）通过每天服用一次药物来改善患者的治疗和舒适度。为此，本发明的微胶囊优选为非肠溶性，由涂覆有乙基纤维素的PPI微粒，氨基甲基丙烯酸共聚物（RL100），聚乙烯吡咯烷酮，蓖麻油和聚氧乙烯化氢化蓖麻油（40）构成。这种药物被设计成使其在摄入一次每日给药后，可以从治疗的第一天开始维持0至24小时之间的平均胃pH大于或等于胃平均值通过具有参考*立即释放的肠溶口服药物在相同条件下给药获得的0至24小时的pH。本发明还涉及这些微胶囊本身。

9. 发明授权

US10004693B2 Oral pharmaceutical formulation in the form of aqueous suspension for modified release of active principle(s) 有权
公开(公告)号：US10004693B2
公开(公告)日：2018-06-26
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： A61K9/50 , A61K31/522 , A61K9/10 , A61K9/00 , A61K31/585 , A61K31/155 , A61K31/192 , A61K31/43
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).

10. 发明授权

US08652523B2 Oral pharmaceutical formulation in the form of a plurality of microcapsules for prolonged release of active principle(s) with slow solubility 有权
标题翻译：多种微胶囊形式的口服药物制剂，用于延长释放缓慢溶解度的活性成分
公开(公告)号：US08652523B2
公开(公告)日：2014-02-18
申请号：US10522252
申请日：2003-07-28
申请人： Florence Guimberteau , Catherine Castan , Rémi Meyrueix
发明人： Florence Guimberteau , Catherine Castan , Rémi Meyrueix
IPC分类号： A61K9/14 , A61K9/16
CPC分类号： A61K9/5047 , A61K9/5015 , A61K9/5026 , A61K9/5078
摘要： The invention concerns microcapsules with prolonged release of active principles with low solubility, consisting of a core containing the active principle and coated with a polymer layer which controls the release of the active principle. The aim is that said oral microcapsules containing hardly soluble active principles, should have a coating film of sufficient thickness to ensure controlled permeability and should be adapted to industrial reproduction. This is achieved by the inventive microcapsules of mean diameter less than 1000 microns, and whereof 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 microcapsules are characterized in that their coating films represents at least 3% p/p of dry matter, relative to their total weight and their core contains a hardly soluble active principle and a solubilizing agent (polyoxyethylene hydrogenated castor oil) which provides the core wherein it is contained with properties such that the behavior of the exposed core (non-coated) in a given dissolving test (TD), is as follows: release of 80% of active principle in less than two hours. The invention also concerns the use of such microcapsules in galenic formulation.
摘要翻译：本发明涉及具有低溶解度的活性成分的延长释放的微胶囊，其由含有活性成分的核心组成并涂覆有控制活性成分释放的聚合物层。目的是所述含有难溶性活性成分的口服微胶囊应具有足够厚度的涂膜以确保受控的渗透性，并且应适于工业繁殖。这通过本发明的平均直径小于1000微米的微胶囊实现，并且其中的涂膜含有不溶于胃肠道液体的成膜聚合物（P1），水溶性聚合物（P2），增塑剂（PL），和任选的润滑表面活性剂（TA）。所述微胶囊的特征在于，它们的涂膜相对于它们的总重量表示至少3％的干物质的p / p，并且它们的芯含有难溶的活性成分和提供核的增溶剂（聚氧乙烯氢化蓖麻油），其中含有这样的性质，使得在给定的溶解试验（TD）中暴露的芯（未涂覆）的行为如下：在少于两小时内释放80％的活性成分。本发明还涉及这种微胶囊在盖仑制剂中的用途。

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