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    • 1. 发明授权
      US08084045B2 Pharmaceutical formulations for the prolonged release of active principle(s) and their applications 有权
    • Pharmaceutical formulations for the prolonged release of active principle(s) and their applications
    • 用于延长释放活性成分及其应用的药物制剂
    • US08084045B2
    • 2011-12-27
    • US10580023
    • 2004-11-19
    • Gauthier Pouliquen , Olivier Soula , Rémi Meyrueix , Florence Nicolas
    • Gauthier Pouliquen , Olivier Soula , Rémi Meyrueix , Florence Nicolas
    • A61K9/32 , A61K9/52 , A61K9/54 , A61K9/64 , A61K38/00
    • A61K9/0024 , A61K38/2013 , A61K38/212 , A61K47/42 , A61K47/645 , A61K51/1217
    • 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.
    • 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 2. 发明申请
      US20100098656A1 Polyamino acids functionalized by hydrophobic grafts bearing an anionic charge and applications thereof, such as therapeutic applications 审中-公开
    • Polyamino acids functionalized by hydrophobic grafts bearing an anionic charge and applications thereof, such as therapeutic applications
    • 由具有阴离子电荷的疏水性接枝物官能化的聚氨基酸及其应用，例如治疗应用
    • US20100098656A1
    • 2010-04-22
    • US11658803
    • 2005-07-25
    • Olivier Breyne , Gauthier Pouliquen , You-Ping Chan
    • Olivier Breyne , Gauthier Pouliquen , You-Ping Chan
    • A61K38/16 , C07K2/00 , A61K38/18 , A61K38/20 , A61K38/21
    • C08G69/10 , A61K8/88 , A61K2800/57 , A61Q19/00 , C08G69/48
    • 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.
    • 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 3. 发明申请
      US20070269517A1 Pharmaceutical Formulations for the Prolonged Release of Interferons and Their Therapeutic Applications 审中-公开
    • Pharmaceutical Formulations for the Prolonged Release of Interferons and Their Therapeutic Applications
    • 用于延长干扰素释放及其治疗应用的药物制剂
    • US20070269517A1
    • 2007-11-22
    • US10580037
    • 2004-11-19
    • Gauthier Pouliquen , Remi Meyrueix , Olivier Soula
    • Gauthier Pouliquen , Remi Meyrueix , Olivier Soula
    • A61K9/10 , A61K38/21
    • A61K47/42 , A61K9/0024 , A61K38/21 , A61K47/645 , A61K47/665 , B82Y5/00
    • The present invention relates to novel pharmaceutical formulations based on stable, fluid aqueous colloidal suspensions for the prolonged release of an interferon (IFN) (and one or more other possible active principles), 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 interferon(s) (and one or more other possible active principles) that makes it possible, after parenteral injection, significantly to increase the in vivo release time of the interferons while at the same time reducing the plasma concentration peak of this IFN, 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 interferon (and one or more other possible active principles) and forming a gelled deposit at the injection site, this gelling being caused by a protein present in the physiological medium.
    • 本发明涉及基于用于延长释放干扰素（IFN）（和一种或多种其它可能的活性成分）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干扰素（和一种或多种其它可能的活性成分）的流体药物制剂，其使得在肠胃外注射后可以显着地增加体内释放时间 干扰素，同时降低该IFN的血浆浓度峰值，所述制剂还在储存时稳定，并且还是生物相容的，可生物降解的，无毒的和非免疫原性的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态悬浮液，所述颗粒与至少一种干扰素（和一种或多种其它 可能的活性成分），并在注射部位形成凝胶沉积物，该胶凝是由存在于生理介质中的蛋白质引起的。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 7. 发明授权
      US08206744B2 Branched polyamino acids functionalized with hydrophobic groups, and applications thereof particularly therapeutic applications 失效
    • Branched polyamino acids functionalized with hydrophobic groups, and applications thereof particularly therapeutic applications
    • 用疏水基团官能化的支链聚氨基酸，及其应用特别是治疗应用
    • US08206744B2
    • 2012-06-26
    • US11658875
    • 2005-07-19
    • Rémi Soula , Gauthier Pouliquen , You-Ping Chan
    • Rémi Soula , Gauthier Pouliquen , You-Ping Chan
    • A61K9/00 , A61K47/42 , C08G83/00
    • A61K8/88 , A61K47/34 , A61K47/645 , A61K2800/57 , A61Q19/00 , C08G69/10 , C08G69/48
    • The invention concerns novel materials based on biodegradable branched polyaminoacids particularly useful for transporting active principle(s). The invention also concerns novel pharmaceutical, cosmetic, dietetic or phytosanitary compositions based on polyaminoacids. The invention aims at providing a novel polymeric material, capable of being used for transporting active principle(s) and enabling all the required relevant specifications to be optimally satisfied: biocompatibility, biodegradability, easy ability to be combined with a large number of active principles or to solubilize same, and to release the active principles in vivo. This is achieved by the present invention which firstly concerns branched polyaminoacids comprising aspartic acid units and or glutamic acid units, and which bear hydrophobic groups including 8 to 30 carbon atoms. The branched polyaminoacids are amphiphilic and are capable of being easily and economically transformed into particles for transporting active principles, the particles being themselves capable of forming stable aqueous colloidal suspensions.
    • 本发明涉及基于可生物降解的支化聚氨基酸的新型材料，其特别适用于输送活性成分。 本发明还涉及基于聚氨基酸的新型药物，化妆品，饮食或植物检疫组合物。 本发明旨在提供一种新型的聚合物材料，其能够用于输送活性成分，并使所有所需的相关规格得到最佳的满足：生物相容性，生物降解性，易于与许多活性成分组合的能力，或 溶解相同，并在体内释放活性成分。 这通过本发明实现，其首先涉及包含天冬氨酸单元和/或谷氨酸单元并且具有包含8至30个碳原子的疏水基团的支链聚氨基酸。 支链聚氨基酸是两亲性的，并且能够容易地和经济地转化成用于输送活性成分的颗粒，颗粒本身能够形成稳定的水性胶态悬浮液。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 8. 发明申请
      US20070196497A1 Pharmaceutical formulations for the prolonged release of active principle(s) and their applications 有权
    • Pharmaceutical formulations for the prolonged release of active principle(s) and their applications
    • 用于延长释放活性成分及其应用的药物制剂
    • US20070196497A1
    • 2007-08-23
    • US10580023
    • 2004-11-19
    • Gauthier Pouliquen , Olivier Soula , Remi Meyrueix , Florence Nicolas
    • Gauthier Pouliquen , Olivier Soula , Remi Meyrueix , Florence Nicolas
    • A61K9/14
    • A61K9/0024 , A61K38/2013 , A61K38/212 , A61K47/42 , A61K47/645 , A61K51/1217
    • 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.
    • 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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