公开(公告)号：US20050202092A1

公开(公告)日：2005-09-15

申请号：US10521617

申请日：2003-07-14

申请人： Tommy Skantze ,  Per Lindfors ,  Sara Forssen

发明人： Tommy Skantze ,  Per Lindfors ,  Sara Forssen

IPC分类号： A61K9/51 ,  A61K9/14 ,  G01N33/553

CPC分类号： A61K9/145 ,  A61K9/146 ,  A61K9/5138

摘要： A process for the preparation of a dispersion of crystalline nano-particles in an aqueous medium comprising combining (i) a first solution comprising a substantially water-insoluble substance in a water-miscible organic solvent with; (ii) an aqueous phase comprising water and optionally a stabiliser, to form a dispersion of amorphous particles; and (iii) sonicating the dispersion of amorphous particles for a sufficient period to form crystalline nano-particles of the substantially water-insoluble substance. The process provides nano-crystals with a mean hydrodynamic diameter of less than 1 micron, particularly less than 300 nm and is particularly useful for the preparation of nano-crystalline dispersions of pharmaceutical substances.

摘要翻译： 一种在水性介质中制备结晶纳米颗粒的分散体的方法，包括将（i）在水混溶性有机溶剂中含有基本上不溶于水的物质的第一溶液与 （ii）包含水和任选的稳定剂的水相以形成无定形颗粒的分散体; 和（iii）将无定形颗粒的分散体超声处理足够的时间以形成基本上不溶于水的物质的结晶纳米颗粒。 该方法提供纳米晶体，其平均流体动力学直径小于1微米，特别是小于300nm，并且特别可用于制备药物物质的纳米结晶分散体。

公开(公告)号：US20050009908A1

公开(公告)日：2005-01-13

申请号：US10486211

申请日：2002-08-01

申请人： Pia Margaretha Hedberg ,  Tommy Skantze ,  Lars Von Corswant ,  Per Lindfors ,  Anna Zackrisson ,  Ulf Olsson

发明人： Pia Margaretha Hedberg ,  Tommy Skantze ,  Lars Von Corswant ,  Per Lindfors ,  Anna Zackrisson ,  Ulf Olsson

IPC分类号： A61K9/10 ,  A61K9/51 ,  A61K47/10 ,  A61K47/14 ,  A61K47/44 ,  A61K9/14 ,  A61K31/225

CPC分类号： A61K9/5138 ,  A61K9/10 ,  A61K9/5192

摘要： A process for the preparation of a stable dispersion of solid particles, in an aqueous medium comprising combining (a) a first solution comprising a substantially water-insoluble substance, a water-miscible organic solvent and an inhibitor with (b) an aqueous phase comprising water and optionally a stabiliser, thereby precipitating solid particles comprising the inhibitor and the substantially water-insoluble substance; and optionally removing the water-miscible organic solvent; wherein the inhibitor is a non-polymeric hydrophobic organic compound as defined in the description. The process provides a dispersion of solid particles in an aqueous medium, which particles exhibit reduced or substantially no particle growth mediated by Ostwald ripening.

摘要翻译： 一种在水性介质中制备固体颗粒的稳定分散体的方法，包括将（a）包含基本上不溶于水的物质，水混溶性有机溶剂和抑制剂的第一溶液与（b）含水相组合 水和任选的稳定剂，从而沉淀包含抑制剂和基本上不溶于水的物质的固体颗粒; 并任选地除去水混溶性有机溶剂; 其中所述抑制剂是如说明书中定义的非聚合疏水性有机化合物。 该方法提供固体颗粒在水性介质中的分散体，该颗粒表现出由Ostwald熟化介导的减少或基本上没有颗粒生长。