发明名称 NANOPARTICULATE AND MACROPARTICULATE FORMULATIONS
摘要 The present invention is directed to particles prepared via the polymerization of at least one surfactant and an isocyanate-containing compound. Pharmaceutical compositions prepared using these particles are also described.
申请公布号 US2016002173(A1) 申请公布日期 2016.01.07
申请号 US201414772540 申请日期 2014.03.12
申请人 CEPHALON, INC. 发明人 BROWN Peter D.;DRAGER Anthony S.
分类号 C07D235/16;A61K9/50;A61K31/4184 主分类号 C07D235/16
代理机构 代理人
主权项 1. A method of preparing bendamustine free base-containing particles comprising: forming an emulsion by mixing a continuous phase comprising an organic solvent, a dispersed phase comprising an aqueous solution of a pharmaceutically acceptable salt of bendamustine, and at least one polyhydric alcohol surfactant; treating the emulsion with an amount of base sufficient to convert the pharmaceutically acceptable salt of bendamustine to bendamustine free base; treating the emulsion with a compound comprising at least two isocyanate moieties; allowing sufficient time for the isocyanate-containing compound to polymerize with the at least one polyhydric alcohol surfactant at the water-polyhydric alcohol interface to form the bendamustine-containing particles; and optionally isolating the particles.
地址 Frazer PA US