公开(公告)号：US20120156256A1

公开(公告)日：2012-06-21

申请号：US13328696

申请日：2011-12-16

申请人： Cecile Bonnet-Gonnet ,  Rémi Meyrueix

发明人： Cecile Bonnet-Gonnet ,  Rémi Meyrueix

IPC分类号： A61K9/00 ,  B32B5/16 ,  G01N37/00 ,  B82Y5/00

CPC分类号： A61K9/5146 ,  A61K9/0019 ,  A61K9/10 ,  A61K9/5192 ,  B82Y5/00 ,  Y10T428/2982

摘要： The present invention relates to novel nanoparticles formed by at least one active ingredient and by at least two polyelectrolytes of opposite polarity, in particular characterized in that at least one of the two polyelectrolytes bears hydrophobic side groups and at least one of the two polyelectrolytes bears side groups of the polyalkylene glycol type, said nanoparticles having an average diameter ranging from 10 to 100 nm and comprising a quantity of groups of the polyalkylene glycol type such that the mass ratio wPAG of polyalkylene glycol relative to the total polymer is greater than or equal to 0.05.

摘要翻译： 本发明涉及由至少一种活性成分和至少两种相反极性的聚电解质形成的新型纳米颗粒，其特征在于两种聚电解质中的至少一种具有疏水性侧基，并且两种聚电解质中的至少一种具有侧面 聚亚烷基二醇型的基团，所述纳米颗粒的平均直径范围为10至100nm，并且包含一定量的聚亚烷基二醇型，使得聚亚烷基二醇的质量比wPAG相对于总聚合物大于或等于 0.05。

公开(公告)号：US20110129539A1

公开(公告)日：2011-06-02

申请号：US13024835

申请日：2011-02-10

申请人： Catherine Castan ,  Florence Guimberteau ,  Rémi Meyrueix

发明人： Catherine Castan ,  Florence Guimberteau ,  Rémi Meyrueix

IPC分类号： A61K9/50 ,  A61K31/43 ,  A61P31/04

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

摘要： The invention concerns liquid pharmaceutical formulations, for oral delivery, with modified release of amoxicillin and consisting of suspensions of coated particles of amoxicillin (microcapsules). The microcapsules constituting the dispersed phase of the suspension are designed, according to the invention, to enable modified release of amoxicillin, 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 amoxicillin, said liquid phase being furthermore saturated with amoxicillin.

摘要翻译： 本发明涉及用于口服递送的液体药物制剂，其具有阿莫西林的改良释放并由阿莫西林（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根据在液体悬液的保质期内保持不变的轮廓来实现阿莫西林的改进释放。 因此，本发明在于选择由至少四种组分组成的微胶囊特异性的涂料组合物，其能够在水中保存所述微胶囊，而不改变其改性释放阿莫西林的性质，所述液相还用阿莫西林进行饱和。

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).

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。

公开(公告)号：US08017156B2

公开(公告)日：2011-09-13

申请号：US11632992

申请日：2005-06-09

申请人： Alain Constancis ,  Florence Nicolas ,  Rémi Meyrueix ,  Olivier Soula

发明人： Alain Constancis ,  Florence Nicolas ,  Rémi Meyrueix ,  Olivier Soula

IPC分类号： A61K9/14 ,  A61K38/28

CPC分类号： A61K38/28 ,  A61K9/1075 ,  A61K9/5138 ,  A61K9/5146 ,  A61K9/5192 ,  Y10S977/773 ,  Y10S977/906

摘要： The invention relates to injectable long-acting insulin formulations for the treatment of types I and II diabetes in humans and animals.The essential object of the invention is to provide an injectable long-acting insulin formulation in the form of a colloidal suspension which is stable, which has a good local tolerance and toxicity compatible with the chronic treatment of diabetics, and which maintains a substantial hypoglycemic effect extending over at least 24 hours after a single administration, e.g. by the subcutaneous route.To achieve this object, the invention relates to a stable aqueous colloidal formulation of insulin-laden nanoparticles of at least one poly(Leu-block-Glu) in which the pH is between 5.8 and 7.0, the osmolarity O (in mOsmol) . . . : 270≦O≦800, and the viscosity v (in mPa·s) is low, namely v≦40. The nanoparticles of poly(Leu-block-Glu) have a mean hydrodynamic diameter Dh such that: 15≦Dh≦40.The invention relates to an antidiabetic drug based on this long-acting insulin formulation and injectable using needles of gauge 29 G, 30 G or 31 G.

摘要翻译： 本发明涉及用于治疗人和动物中I型和II型糖尿病的可注射长效胰岛素制剂。 本发明的基本目的是提供一种稳定的胶体悬浮液形式的可注射的长效胰岛素制剂，其具有与糖尿病患者的慢性治疗相适应的良好的局部耐受性和毒性，并且其保持显着的降血糖效应 在单次给药后延长至少24小时，例如 通过皮下途径。 为了实现这个目的，本发明涉及至少一种pH（在5.8至7.0之间），渗透压浓度O（以mOsmol计）的至少一种聚（Leu-block-Glu）的含胰岛素的纳米颗粒的稳定水性胶体制剂。 。 。 ：270＆nlE; O＆nlE; 800，粘度v（mPa·s）低，即v＆nlE; 40。 聚（Leu-block-Glu）的纳米颗粒具有平均流体动力学直径Dh，使得：15＆nlE; Dh＆nlE; 40。 本发明涉及一种基于该长效胰岛素制剂的抗糖尿病药物，并使用量规29 G，30 G或31 G的针头进行注射。

公开(公告)号：US20090311315A1

公开(公告)日：2009-12-17

申请号：US11884549

申请日：2006-02-21

申请人： Catherine Castan ,  Florence Guimberteau ,  Rémi Meyrueix ,  Gérard Soula

发明人： Catherine Castan ,  Florence Guimberteau ,  Rémi Meyrueix ,  Gérard Soula

IPC分类号： A61K9/52 ,  A61K9/14 ,  A61K9/22 ,  A61K31/4178 ,  A61K31/4184 ,  A61K9/26

CPC分类号： A61K9/2081 ,  A61K9/5073 ,  A61K9/5078 ,  A61K9/5084 ,  A61K31/415 ,  A61K31/417

摘要： The invention relates to oral pharmaceutical forms with modified release of ARB, and to related treatments and delivery methods.The invention concerns a form with modified release of ARB which prolongs the bioabsorption time and enables the pharmaceutical form to be administered only once daily.Therefore, the invention is an oral pharmaceutical form with modified ARB release comprising a plurality of ARB microunits (mean diameter: 50-1000 μm) leading, after being taken, to a plasma profile wherein C18 h*≦C18 h, with C18 h=plasma ARB concentration, 18 h after being taken, C18 h*=plasma ARB concentration corresponding to C18 h and obtained under the same conditions as C18 h, with a reference immediate-release oral pharmaceutical form*, containing the same dose of ARB, Cmax=maximum plasma ARB concentration after being taken, Cmax*=maximum plasma ARB concentration corresponding to Cmax and obtained under the same conditions as Cmax, with a reference immediate-release oral pharmaceutical form*, containing the same dose of ARB.

摘要翻译： 本发明涉及具有ARB修饰释放的口服药物形式，以及相关治疗和递送方法。 本发明涉及延长生物吸收时间并延长药物形式每天只能施用一次的ARB的释放形式。 因此，本发明是具有改良的ARB释放的口服药物形式，其包含多个ARB微单位（平均直径：50-1000μm），其被引导至血浆曲线，其中C18h * <= C18h，C18h =血浆ARB浓度，服用18小时后，C18h * =对应于C18h的血浆ARB浓度，并且在与C18h相同的条件下获得，含有相同剂量的ARB的参考速释口服药物形式* Cmax =服用后最大血浆ARB浓度，Cmax * =对应于Cmax的最大血浆ARB浓度，并且在与Cmax相同的条件下获得，含有相同剂量的ARB的参考即释释口服药物形式*。