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    • 32. 发明申请
    • 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 PouliquenOlivier SoulaRemi MeyrueixFlorence Nicolas
    • Gauthier PouliquenOlivier SoulaRemi MeyrueixFlorence Nicolas
    • A61K9/14
    • A61K9/0024A61K38/2013A61K38/212A61K47/42A61K47/645A61K51/1217
    • 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。
    • 33. 发明申请
    • Microcapsules with modified release of active principles with low solubility for oral delivery
    • 具有改进释放活性成分的微胶囊,具有低溶解性用于口服递送
    • US20060275376A1
    • 2006-12-07
    • US10522234
    • 2003-07-28
    • Florence GuimberteauCatherine CastanRemi MeyrueixGerard Soula
    • Florence GuimberteauCatherine CastanRemi MeyrueixGerard Soula
    • A61K9/50A61K9/16
    • A61K9/5015A61K9/5026A61K9/5047
    • The invention concerns microcapsules for reliably modified release and adapted to industrial reproduction of an active principle hardly water-soluble, other than anti-hyperglycemia agents Each of said microcapsules comprises a core of hardly soluble active principle and a coating film applied on the core. Their mean diameter is less than 1000 microns. 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 coating film represents at least 4% p/p of dry mraner of their total weight. and its components P1, P2. PL satisfy the following characteristics: dry weight mass fraction of PI relative to the total coating weight ranging between 40 and 90%; dry matter weight fraction of PL/P1+P2 ranging between 15 and 60%: dry matter weight fraction of PL/P1+P2 ranging between 1 and 30%. The invention also concerns the uses of said microcapsules in galenic formulation.
    • 本发明涉及用于可靠调节释放的微胶囊,并且适用于除抗高血糖剂以外的几乎不溶于水的活性成分的工业复制。所述微胶囊中的每一种都包含难溶的活性成分的核心和涂覆在芯上的涂膜。 它们的平均直径小于1000微米。 涂膜含有不溶于胃肠道液的成膜聚合物(P1),水溶性聚合物(P2),增塑剂(PL)和任选的润滑表面活性剂(TA)。 所述涂膜占其总重量的至少4%p / p干燥颗粒。 及其部件P1,P2。 PL满足以下特征:相对于总涂层重量的40重量%至90重量%的PI的干重质量分数; PL / P1 + P2的干物质重量分数在15和60%之间:PL / P1 + P2的干物质重量分数范围在1%和30%之间。 本发明还涉及所述微胶囊在盖仑制剂中的用途。