公开(公告)号：US20070218142A1

公开(公告)日：2007-09-20

申请号：US10580035

申请日：2004-11-19

申请人： Sophie Bignon ,  Remi Meyrueix ,  Olivier Soula

发明人： Sophie Bignon ,  Remi Meyrueix ,  Olivier Soula

IPC分类号： A61K9/14

CPC分类号： A61K38/2013 ,  A61K9/0024 ,  A61K38/20 ,  A61K47/34 ,  A61K47/6921 ,  A61K47/6935

摘要： The present invention relates to novel pharmaceutical formulations based on stable, fluid aqueous colloidal suspensions for the prolonged release of an interleukin (IL) (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 interleukin(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 IL while at the same time reducing the plasma concentration peak of this IL, 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 interleukin (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.

摘要翻译： 本发明涉及基于用于延长释放白介素（IL）（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白细胞介素（和一种或多种其它可能的活性成分）的流体药物制剂，其使得在胃肠外注射后可显着地增加体内释放时间 IL，同时降低该IL的血浆浓度峰值，所述制剂还在储存时稳定，并且也是生物相容的，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白细胞介素（和一种或多种其它物质）非共价结合 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。