公开(公告)号：US08445023B2

公开(公告)日：2013-05-21

申请号：US12638739

申请日：2009-12-15

申请人： Florence Guimberteau ,  Frederic Dargelas

发明人： Florence Guimberteau ,  Frederic Dargelas

IPC分类号： A61K9/16

CPC分类号： A61K9/5021 ,  A61K9/2031 ,  A61K9/205 ,  A61K9/2054 ,  A61K9/4866 ,  A61K9/5026 ,  A61K9/5047 ,  A61K31/485 ,  A61K47/32 ,  A61K47/34 ,  A61K47/38 ,  A61K47/44

摘要： The present invention relates to solid microparticulate oral pharmaceutical forms whose composition and structure make it possible to avoid misuse of the pharmaceutical active principle (AP) they contain.The object of the present invention is to prevent solid oral drugs from being misappropriated for any use other than the therapeutic use(s) officially approved by the competent public health authorities. In other words, the object is to avoid the voluntary or involuntary misuse of solid oral drugs.The invention relates to a solid oral pharmaceutical form which is characterized in that it contains anti-misuse means, in that at least part of the AP it comprises is contained in coated microparticles for modified release of the AP, and in that the coated microparticles of AP have a coating layer (Ra) which assures the modified release of the AP and simultaneously imparts crushing resistance to the coated microparticles of AP so as to avoid misuse.

摘要翻译： 本发明涉及固体微粒口服药物形式，其组成和结构使得可以避免滥用其含有的药物活性成分（AP）。 本发明的目的是为了防止固体口服药物被用于除主管公共卫生当局正式批准的治疗用途之外的任何用途。 换句话说，目的是避免自愿或非自愿滥用固体口服药物。 本发明涉及一种固体口服药物形式，其特征在于其含有抗滥用手段，因为其包含的至少部分AP包含在用于AP的改性释放的包被微粒中，并且其中涂覆的微粒 AP具有涂层（Ra），其确保AP的改性释放并同时赋予AP的涂覆微粒耐破碎性，从而避免误用。

公开(公告)号：US08293255B2

公开(公告)日：2012-10-23

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： A61K9/10 ,  A61K9/16 ,  A61K9/00 ,  A61K47/32 ,  A61K47/00

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 solubilize 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使其溶解并释放所述 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，所述改性的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：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：US20110091537A1

公开(公告)日：2011-04-21

申请号：US12905387

申请日：2010-10-15

申请人： Catherine Castan ,  Anne-Sophie DAVIAUD-VENET

发明人： Catherine Castan ,  Anne-Sophie DAVIAUD-VENET

IPC分类号： A61K9/14 ,  A61K31/485 ,  A61K9/20 ,  A61K9/48 ,  A61K31/137

CPC分类号： A61K31/485 ,  A61K9/1676 ,  A61K9/2077 ,  A61K9/4808 ,  A61K9/5078 ,  A61K9/5084

摘要： The present invention relates to a solid oral pharmaceutical form, with modified release of at least one active ingredient, containing at least microparticles containing said active ingredient and at least one viscosifying agent in a form isolated from said microparticles of active ingredient, characterized in that said microparticles possess an average diameter ranging from 100 to 600 μm, and are formed by a core containing at least said active ingredient and coated with at least one coating layer, said core being formed by a support particle covered by a layer comprising at least said active ingredient, said coating layer being formed by a material composed of at least 25 to 70% by weight relative to the total weight of said coating, of at least one polymer A insoluble in water, 30 to 75% by weight relative to the total weight of said coating, of at least one polymer B insoluble in water below pH 5 and soluble in water above pH 7, and 0 to 25% by weight relative to the total weight of said coating, of at least one plasticizer, said polymers A and B being in a polymer(s) B/polymer(s) A weight ratio comprised between 0.25 and 4, and said coating layer representing at least 35% by weight, relative to the total weight of said microparticle.

摘要翻译： 本发明涉及固体口服药物形式，其具有至少一种活性成分的改性释放，所述至少一种活性成分至少含有含有所述活性成分的微粒和至少一种与所述活性成分微粒分离的形式的增粘剂，其特征在于所述 微粒具有100-600μm的平均直径，并且由至少含有所述活性成分的核心形成并涂覆有至少一个涂层形成，所述芯体由覆盖有至少包含所述活性成分的层的支撑颗粒形成 成分，所述涂层由相对于所述涂层的总重量至少25至70重量％的材料形成，至少一种不溶于水的聚合物A相对于总重量为30至75重量％ 的所述涂层，至少一种聚合物B不溶于低于pH 5的水中并且可溶于高于pH 7的水中，并且相对于总重量为0至25重量％ 的所述涂层中的至少一种增塑剂，所述聚合物A和B在聚合物B /聚合物A中的重量比在0.25和4之间，所述涂层相对于相对的重量比为至少35重量％ 相对于所述微粒的总重量。

公开(公告)号：US07919572B2

公开(公告)日：2011-04-05

申请号：US10558617

申请日：2004-05-28

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

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

IPC分类号： C08G69/10 ,  A01N25/00 ,  A61K47/00

CPC分类号： A61K8/88 ,  A61K47/645 ,  A61K2800/57 ,  A61Q19/00 ,  C08G69/10 ,  C08G69/48

摘要： The invention relates to novel materials based on biodegradable polyamino acids, particularly useful for the vectorisation of active principals (PA). The invention further relates to novel, pharmaceutical, cosmetic, dietary or phytosanitary compositions. The invention provides novel polymeric raw material, for use in the vectorisation of PA and with an optimal match for all the requirements of the type: biocompatibility, biodegradability, stability, ability to easily associate with numerous active principals or to solubilise the same and to liberate said active principals in vivo. Said aim is achieved with polyamino acids comprising aspartic and/or glutamate units, some of which carry at least one graft, characterised in that at least one of said grafts is bonded to an aspartic or glutamate unit by means of an amino acids spacer based on Leu, and/or Ileu, and/or Val, and/or Phe and a hydrophobic group with C6-C30 is connected by an ester bond to the spacer.

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，特别适用于活性成分（PA）的向量化。 本发明进一步涉及新的，药物，化妆品，膳食或植物检疫组合物。 本发明提供新颖的聚合物原料，用于PA的载体化和与所有类型的所有要求的最佳匹配：生物相容性，生物可降解性，稳定性，容易与许多活性成分相关联或溶解它并释放的能力 活体检者在体内表示。 所述目的通过包含天冬氨酸和/或谷氨酸单体的聚氨基酸实现，其中一些氨基酸携带至少一个接枝物，其特征在于至少一个所述移植物通过氨基酸间隔基与天冬氨酸或谷氨酸单元结合，基于 Leu和/或Ileu和/或Val，和/或Phe和具有C6-C30的疏水基团通过酯键连接到间隔物上。

公开(公告)号：US20080152675A1

公开(公告)日：2008-06-26

申请号：US12003095

申请日：2007-12-20

申请人： Gauthier POULIQUEN

发明人： Gauthier POULIQUEN

IPC分类号： A61K47/32 ,  A61K47/36 ,  A61K9/107

CPC分类号： A61K47/36 ,  A61K9/107 ,  A61K47/34

摘要： The invention relates to injectable pharmaceutical compositions for the prolonged release of at least one active principle, comprising at least one active principle in an aqueous phase of amphiphilic polymer, said aqueous phase being in the form of a dispersion in a continuous lipid phase. The composition is in the form of a water-in-oil emulsion comprising: a pharmaceutically acceptable, continuous lipid phase, an aqueous disperse phase containing at least one amphiphilic polymer and at least one active principle not covalently bonded to said amphiphilic polymer, and at least one pharmaceutically acceptable surfactant.

摘要翻译： 本发明涉及用于延长释放至少一种活性成分的可注射药物组合物，其包含至少一种活性成分在两亲性聚合物的水相中，所述水相以连续脂质相中的分散体的形式。 该组合物为油包水型乳状液，其包含药学上可接受的连续脂质相，含有至少一种两亲聚合物的水分散相和至少一种不共价键合到所述两亲性聚合物的活性成分，以及在 至少一种药学上可接受的表面

公开(公告)号：US20080026070A1

公开(公告)日：2008-01-31

申请号：US11808456

申请日：2007-06-11

申请人： Cecile Bonnet-Gonnet

发明人： Cecile Bonnet-Gonnet

IPC分类号： A61K9/14 ,  A61K31/70 ,  A61K31/715 ,  A61K38/02 ,  A61K38/21 ,  A61P3/00 ,  A61P35/00 ,  A61P25/00 ,  A61K38/27 ,  A61K38/28 ,  A61K47/30

CPC分类号： A61K9/10 ,  A61K9/1635 ,  A61K31/70 ,  A61K31/715 ,  A61K38/212 ,  A61K38/27 ,  A61K38/28 ,  A61K47/34

摘要： The present invention relates to novel pharmaceutical formulations based on aqueous colloidal suspensions for the prolonged release of one or more active principles—AP—particularly protein and peptide active principles, and to the applications, especially therapeutic applications, of these formulations. This formulation comprises an aqueous colloidal suspension of low viscosity based on micrometric particles of a water-soluble, biodegradable, amphiphilic polymer PO carrying hydrophobic groups (GH)— alpha-tocopherol—and ionizable hydrophilic groups (GI)—Glu—that are at least partially ionized, said particles being capable of associating spontaneously and non-covalently with an AP, at pH=7.0, under isotonic conditions, and having a size of between 0.5 and 100 μm. This suspension contains multivalent ions (Mg++) of opposite polarity to that of the group GI of the PO, the ratio r, defined by the formula r = n × [ IM ] [ GI ] , where n is the valency of said multivalent ions, [IM] is the molar concentration of multivalent ions, [GI] is the molar concentration of ionizable groups GI, being between 0.3 and 10.

摘要翻译： 本发明涉及基于水性胶体悬浮液的新型药物制剂，用于延长释放这些制剂的一种或多种活性成分，特别是蛋白质和肽活性成分，以及应用，特别是治疗应用。 该制剂包含基于水溶性，可生物降解的两亲性聚合物PO的微量颗粒的低粘度的水性胶体悬浮液，其携带疏水基团（GH）-α-生育酚和可离子化亲水基团（GI）-Glu-至少是至少 部分电离，所述颗粒能够在等渗条件下在pH = 7.0下自发和非共价地与AP缔合，并且具有0.5至100μm的大小。 该悬浮液含有与PO的组GI相反极性的多价离子（Mg ++），由式