公开(公告)号：US08197850B2

公开(公告)日：2012-06-12

申请号：US10415850

申请日：2001-11-19

申请人： Catherine Castan ,  Remi Meyrueix ,  Gerard Soula

发明人： Catherine Castan ,  Remi Meyrueix ,  Gerard Soula

IPC分类号： A61K9/14

CPC分类号： A61K31/155 ,  A61K9/5015 ,  A61K9/5047 ,  A61K31/00

摘要： The invention concerns an oral galenic form for prolonged release of anti-hyperglycaemic (metformin) active principles. Said medicine enables to obtain an efficient therapeutic protection over 24 hours by overcoming the problems of bypass of the absorption window and the massive localised release of active principles. Therefor, said medicine comprises several thousand anti-hyperglycaemic (metformin) microcapsules each consisting of a core comprising at least an anti-hyperglycaemic agent and of a coating film applied on the core and enabling the prolonged release in vivo of the anti-hyperglycaemic agent. Said microcapsules have a grain size distribution ranging between 50 and 100 microns. The reproducibility of the transit kinetics and hence of bioavailability are very high. There results for the patient a lesser risk of hyperglycaemic or hypoglycaemic. The invention also concerns the preparation of said medicine and the use of a plurality of said microcapsules for making an anti-hyperglycaemic medicine. The invention is applicable to the treatment of type II diabetes.

摘要翻译： 本发明涉及用于延长释放抗高血糖（二甲双胍）活性成分的口服盖仑制剂。 所述药物通过克服吸收窗旁路的问题和主动原理的大量局部释放，能够在24小时内获得有效的治疗保护。 因此，所述药物包含数千种抗高血糖（二甲双胍）微胶囊，每个微胶囊由包含至少抗高血糖剂的芯和涂覆在芯上的涂膜构成，并且能够在体内延长抗高血糖剂的释放。 所述微胶囊具有在50和100微米之间的粒度分布。 运输动力学和生物利用度的重现性非常高。 结果，患者血糖过低或低血糖的风险较小。 本发明还涉及所述药物的制备以及多种所述微胶囊用于制备抗高血糖药物的用途。 本发明适用于II型糖尿病的治疗。

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：US20100310667A1

公开(公告)日：2010-12-09

申请号：US12790201

申请日：2010-05-28

申请人： Catherine Castan ,  Philippe Caisse

发明人： Catherine Castan ,  Philippe Caisse

IPC分类号： A61K9/14 ,  C08B3/06

CPC分类号： A61K9/0065 ,  A61K9/4866 ,  A61K9/5015 ,  A61K9/5026 ,  A61K9/5031 ,  A61K9/5047 ,  A61K9/5078 ,  A61K31/155 ,  A61K31/192 ,  A61K31/403

摘要： The invention relates to a pharmaceutical composition comprising a plurality of controlled-release coated microparticles each comprising a floating core, on the surface of which is deposited a layer containing at least one active principle, said layer being covered with a controlled-release coating, characterized by the fact that said floating core is composed of cellulose acetate phthalate and has an apparent density of less than or equal to 0.6 g/mL and said coated microparticles have a density of less than or equal to 0.7 g/mL.

摘要翻译： 本发明涉及一种药物组合物，其包含多个受控释放的包被的微粒，每个包含浮芯，其表面沉积包含至少一种活性成分的层，所述层被覆盖有控释膜，其特征在于 所述浮芯由醋酸邻苯二甲酸纤维素组成，表观密度小于或等于0.6g / mL，所述涂布微粒的密度小于或等于0.7g / mL。

公开(公告)号：US07709445B2

公开(公告)日：2010-05-04

申请号：US10473821

申请日：2002-03-26

申请人： Gérard Soula ,  Nathan Bryson

发明人： Gérard Soula ,  Nathan Bryson

IPC分类号： A61K38/02 ,  A61K9/10

CPC分类号： A61K9/5146 ,  A61K9/1075 ,  Y10S514/937 ,  Y10S514/941

摘要： An aqueous suspension, stable in physiological medium, of nanoparticles for delivering active principles such as insulin. The delivery particles are based on a three-block copolymer: polyethylene glycol/hydrophilic polyaminoacid/hydrophobic polyaminoacid. These three-block copolymers can be associated with an active principle without denaturing it, and perform a controlled and long-term release of the active principle in vivo, and thus provide the active principle with a very prolonged release. Also disclosed is a powder form solid from which are derived the delivery particles, the preparation of the powder-form solid, a suspension of delivery particles based on the three-block copolymer, and pharmaceutical specialties obtainable from the delivery particles filled with active principle.

摘要翻译： 在生理介质中稳定的水性悬浮液用于递送活性成分如胰岛素的纳米颗粒。 递送颗粒基于三嵌段共聚物：聚乙二醇/亲水性聚氨基酸/疏水性聚氨基酸。 这些三嵌段共聚物可以与活性成分相关联而不使其变性，并且在体内进行活性成分的受控和长期释放，从而提供非常长期释放的活性成分。 还公开了一种粉末状固体，其衍生为递送颗粒，粉末状固体的制备，基于三嵌段共聚物的递送颗粒的悬浮液，以及可从填充有活性成分的递送颗粒获得的药物特性。

公开(公告)号：US20100098656A1

公开(公告)日：2010-04-22

申请号：US11658803

申请日：2005-07-25

申请人： Olivier Breyne ,  Gauthier Pouliquen ,  You-Ping Chan

发明人： Olivier Breyne ,  Gauthier Pouliquen ,  You-Ping Chan

IPC分类号： A61K38/16 ,  C07K2/00 ,  A61K38/18 ,  A61K38/20 ,  A61K38/21

CPC分类号： C08G69/10 ,  A61K8/88 ,  A61K2800/57 ,  A61Q19/00 ,  C08G69/48

摘要： The present invention relates to novel materials based on biodegradable polyamino acids that are useful especially for the vectorization of active principle(s) (AP). The invention further relates to novel pharmaceutical, cosmetic, dietetic or phytosanitary compositions based on these polyamino acids. The object of the invention is to provide a novel polymer starting material that is capable of being used for the vectorization of AP and makes it possible on the one hand to achieve high polymer/AP ratios, and on the other hand optimally to satisfy all the specifications required in the case in point: biocompatibility, biodegradability, ability to associate easily with numerous active principles or to solubilize them, and ability to release these active principles in vivo. This object is achieved by the present invention, which relates first and foremost to linear polyamino acids comprising aspartic units or glutamic units and having hydrophobic grafts comprising hydrophobic groups containing from 8 to 30 carbon atoms, at least one of these hydrophobic grafts having at least one anionic charge and/or one or more mutually identical or different ionizable groups each capable of giving rise to at least one anionic charge. These polymers are amphiphilic and anionic and are capable of being converted easily and economically to particles for the vectorization of active principles, these particles themselves being capable of forming stable aqueous colloidal suspensions.

摘要翻译： 本发明涉及基于可生物降解的聚氨基酸的新型材料，其特别用于活性成分（AP）的向量化。 本发明还涉及基于这些聚氨基酸的新型药物，化妆品，饮食或植物检疫组合物。 本发明的目的是提供一种新的聚合物起始材料，其能够用于AP的向量化，并且一方面可以实现高聚合物/ AP比率，另一方面最佳地满足所有 在这种情况下需要的规格：生物相容性，生物降解能力，容易与许多活性成分缔合或溶解它们的能力以及在体内释放这些活性成分的能力。 该目的通过本发明来实现，本发明首先涉及包含天冬氨酸单元或谷氨酸单元并具有包含含有8至30个碳原子的疏水基团的疏水性接枝的线性聚氨基酸，这些疏水性移植物中的至少一种具有至少一个 阴离子电荷和/或一个或多个相互相同或不同的可离子化基团，每个基团能够产生至少一种阴离子电荷。 这些聚合物是两亲性和阴离子性的，并且能够容易地和经济地转化成用于活性成分载体化的颗粒，这些颗粒本身能够形成稳定的水性胶态悬浮液。

公开(公告)号：US07683024B2

公开(公告)日：2010-03-23

申请号：US10516733

申请日：2003-06-03

申请人： You-Ping Chan ,  Stéphanie Angot ,  Olivier Breyne

发明人： You-Ping Chan ,  Stéphanie Angot ,  Olivier Breyne

IPC分类号： C07K38/02

CPC分类号： A61K8/88 ,  A61K8/678 ,  A61K9/5146 ,  A61K47/34 ,  A61K2800/57 ,  A61Q19/00 ,  C08G69/10 ,  C08G69/48

摘要： The invention concerns novel biodegradable polyaminoacid materials, useful in particular for vectoring active principle(s). The invention also concerns novel pharmaceutical, cosmetic dietetic or phytosanitary compositions based on said polyaminoacids. The invention aims at providing a novel polymer raw material, capable of being used for vectoring active principles and enabling optimal fulfillment of all specified requirements: biocompatibility, biodegradability, easy and inexpensive transformation into particles vectoring active principles, the particles being themselves capable of forming colloidal suspensions, of being easily associated with numerous active principles, and of releasing said active principles in vivo. Therefor, the present invention concerns first of all amphiphilic polyaminoacids comprising aspartic acid units and/or glutamic acid units, characterized in that at least part of said units carry grafts, including at least one alpha-tocopherol motif, for example (polyglutamate or polyaspartate grafted with alpha-tocopherol of synthetic or natural origin).

摘要翻译： 本发明涉及新型可生物降解的聚氨基酸材料，特别适用于向量活性成分。 本发明还涉及基于所述聚氨基酸的新型药物，美容饮食或植物检疫组合物。 本发明旨在提供一种新颖的聚合物原料，能够用于向导活性原理，并能够最佳地实现所有特定的要求：生物相容性，生物降解性，易于和便宜地转化成粒子的载体活性成分，颗粒本身能够形成胶体 悬浮液，易于与许多活性成分相关联，并且在体内释放所述活性成分。 因此，本发明涉及包含天冬氨酸单元和/或谷氨酸单元的所有两亲性聚氨基酸的首要问题，其特征在于所述单元的至少一部分携带移植物，包括至少一种α-生育酚基序，例如（聚谷氨酸或聚天冬氨酸嫁接 合成或天然来源的α-生育酚）。

公开(公告)号：US07678882B2

公开(公告)日：2010-03-16

申请号：US11509783

申请日：2006-08-25

申请人： Stéphanie Angot ,  Olivier Breyne ,  You-Ping Chan ,  Gérard Soula

发明人： Stéphanie Angot ,  Olivier Breyne ,  You-Ping Chan ,  Gérard Soula

IPC分类号： C07K2/00

CPC分类号： A61Q19/00 ,  A61K8/88 ,  A61K47/34 ,  A61K47/645 ,  A61K47/65 ,  C08G69/10 ,  C08G69/48

摘要： The invention relates to novel materials based on biodegradable polyamino acids that are useful for vectorizing active principle(s)(AP). The aim of the invention is to supply a new polymeric raw material that is used for vectorizing AP and optimally fulfills all requirements concerning biocompatibility, biodegradability, the ability to be easily associated with numerous active principles or solubilize the active principles and to release the active principles in vivo. Such polymers can also be readily and economically transformed into particles vectorizing active principles according to the grafting rate of the hydrophobic groups, said particles being able to form stable aqueous colloidal suspensions. The aim of the invention is achieved by the inventive amphiphile polyamino acids comprising aspartic and/or glutamic units that carry grafts which encompass at least one hydrophobic unit and are linked to the aspartic and/or glutamic units via a rotula containing two amide functions, more particularly via a spacer of the lysine or ornithine type. The amide functions ensure better stability during hydrolysis than comparable products known in prior art. The invention also relates to new pharmaceutical, cosmetic, dietetic, or phytosanitary compositions based on the inventive polyamino acids.

摘要翻译： 本发明涉及可用于向量化活性成分（AP）的可生物降解的聚氨基酸的新型材料。 本发明的目的是提供一种新的聚合物原料，其用于向AP进行载体化，并且最佳地满足关于生物相容性，生物可降解性，易于与许多活性成分相关联或增溶活性成分的能力的所有要求，并释放活性成分 体内。 这样的聚合物也可以容易地和经济地转化成根据疏水基团的接枝速率向量化活性成分的颗粒，所述颗粒能够形成稳定的水性胶态悬浮液。 本发明的目的是通过包含天冬氨酸和/或谷氨酸单元的本发明的两亲性聚氨基酸实现的，所述天然氨基酸和/或谷氨酸单元携带包含至少一个疏水单元的移植物，并通过含有两个酰胺官能团的转运体与天冬氨酸和/或谷氨酸单元连接 特别是通过赖氨酸或鸟氨酸类型的间隔物。 酰胺功能确保在水解期间比现有技术中已知的可比产品更好的稳定性。 本发明还涉及基于本发明的聚氨基酸的新的药物，化妆品，饮食或植物检疫组合物。

公开(公告)号：US20100048735A1

公开(公告)日：2010-02-25

申请号：US12581644

申请日：2009-10-19

申请人： You-Ping Chan ,  Stéphanie Angot ,  Olivier Breyne

发明人： You-Ping Chan ,  Stéphanie Angot ,  Olivier Breyne

IPC分类号： A61K47/34 ,  C08G73/10 ,  A61P43/00

CPC分类号： A61K8/88 ,  A61K8/678 ,  A61K9/5146 ,  A61K47/34 ,  A61K2800/57 ,  A61Q19/00 ,  C08G69/10 ,  C08G69/48

摘要： The invention concerns novel biodegradable polyaminoacid materials, useful in particular for vectoring active principles(s). The invention also concerns novel pharmaceutical, cosmetic dietetic or phytosanitary compositions based on said polyaminoacids. The invention aims at providing a novel polymer raw material, capable of being used for vectoring active principles and enabling optimal fulfillment of all specified requirements: biocompatibility, biodegradability, easy and inexpensive transformation into particles vectoring active principles, said particles being themselves capable of forming colloidal suspensions, of being easily associated with numerous active principles, and of releasing said active principles in vivo. Therefor, the present invention concerns first of all amphiphilic polyaminoacids comprising aspartic acid units and/or glutamic acid units, characterized in that at least part of said units carry grafts, including at least one alphα-tocopherol motif, for example (polyglutamate or polyaspartate grafted with alphα-tocopherol of synthetic or natural origin).

摘要翻译： 本发明涉及新颖的可生物降解的聚氨基酸材料，特别适用于载体活​​性成分。 本发明还涉及基于所述聚氨基酸的新型药物，美容饮食或植物检疫组合物。 本发明旨在提供一种新颖的聚合物原料，其能够用于向量活性成分的原理并且能够最佳地实现所有特定的要求：生物相容性，生物降解性，容易且便宜的转化成粒子的载体活性成分，所述颗粒本身能够形成胶体 悬浮液，易于与许多活性成分相关联，并且在体内释放所述活性成分。 因此，本发明涉及包含天冬氨酸单元和/或谷氨酸单元的所有两亲性聚氨基酸的首要问题，其特征在于至少部分所述单元携带移植物，包括至少一种α-α-生育酚基序，例如（聚谷氨酸或聚天冬氨酸酯接枝 合成或天然来源的α-生育酚）。

公开(公告)号：US20100034886A1

公开(公告)日：2010-02-11

申请号：US12084368

申请日：2006-10-31

申请人： Olivier Soula ,  Rémi Soula ,  Olivier Breyne

发明人： Olivier Soula ,  Rémi Soula ,  Olivier Breyne

IPC分类号： A61K9/14 ,  C07K5/00 ,  A61K38/07 ,  A61K38/16 ,  A61P35/00

CPC分类号： C08G69/10 ,  A61K8/88 ,  A61K2800/57 ,  A61Q19/00 ,  C07K14/001

摘要： The invention relates to novel biodegradable materials based on modified polyamino acids and suitable, in particular, for vectoring active substance(s) (AS). Said invention also relates to novel pharmaceutical, cosmetic, dietary or plant protective compositions which are based on said polyamino acids.The aim of said invention is to provide a novel polymer raw material usable for vectoring the AS and capable to optimally meet all specification in this area: biocompatibility, biodegradability, ability to become easily associated with many active substances or to solubilise them and to release said active substances in vivo. The aim is attained to 30 carbon atoms.Said polyglutamates modified by histidine derivatives are soluble with pH lower than 5 and are easily and economically convertible into active substance vectorization particles which are able to form stable aqueous colloidal suspensions. On the contrary, said modified polyglutamates are insoluble in water with a physiological pH (7.4), and thereby have to be precipitated on an injection site in the case of a subcutaneous injection.

摘要翻译： 本发明涉及基于改性聚氨基酸的新型可生物降解材料，特别适用于载体活​​性物质（AS）。 所述发明还涉及基于所述聚氨基酸的新型药物，化妆品，膳食或植物保护性组合物。 本发明的目的是提供一种可用于载体AS的新型聚合物原料，能够最佳地满足该领域的所有规格：生物相容性，生物降解性，与许多活性物质容易相关的能力或溶解它们并释放所述 体内活性物质。 目标达到30个碳原子。 由组氨酸衍生物修饰的所述聚谷氨酸可溶于pH低于5，易于经济地转化成能形成稳定的水性胶体悬浮液的活性物质载体化颗粒。 相反，所述改性聚谷氨酸不溶于具有生理pH（7.4）的水中，因此在皮下注射的情况下必须在注射部位沉淀。

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。