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    • 1. 发明申请
    • METHOD FOR PRODUCING POWDERY PARTICLE-REDUCED FORMULATIONS WITH THE AID OF COMPRESSED GASES
    • 用于生产粉状颗粒减小的制剂使用压缩气体
    • WO0103671A3
    • 2001-05-10
    • PCT/EP0006709
    • 2000-07-13
    • SUEDDEUTSCHE KALKSTICKSTOFFHEIDLAS JUERGENOBER MARTINWIESMUELLER JOHANN
    • HEIDLAS JUERGENOBER MARTINWIESMUELLER JOHANN
    • A61K9/14A61K9/16B01J3/00
    • A61K9/14A61K9/1617Y10S514/959Y10S516/922Y10S516/928
    • The invention relates to the production of powdery particle-reduced formulations with the aid of compressed gases. The inventive method is characterized in that: the solid compound to be formulated, said compound consisting of a poorly soluble and mostly bioactive substance, is homogeneously comminuted together with 10-99 wt. % (with regard to the formulation) of a supporting material, which is essentially soluble in the compressed gas mixture, in an agitated autoclave provided with a mechanical comminution device in the presence of compressed gas or mixtures thereof, at method temperatures ranging from 10 to 200 DEG C, and under method pressures ranging from 5 to 500 bar, and, in a second method step; the compressed gas mixture, consisting mostly of dimethyl ether, pure propane and/or carbon dioxide, is expanded by lowering the pressure and is separated away from the homogenate that can also be provided in the form of a molten material. Finally, the powdery particle-reduced formulation is obtained from the resulting homogenate and exhibits significant improvements with regard to solubility properties and especially with regard to the biological availability of compounds which, initially, are poorly soluble or insoluble.
    • 对于具有压缩气体的辅助下粉状颗粒减小制剂的制备是要配制固体化合物,难溶的,并且通常的生物活性剂,连同10-99重量%(基于所述制剂)的载体材料的可溶于所述压缩气体混合物基本上, 在压缩气体,或它们的混合物与机械式粉碎机的搅拌高压釜中存在的情况下处理温度10至200℃,并在5和500之间的过程压力接地棒均匀,并且在第二处理阶段,压缩气体混合物,通常是二甲醚,纯丙烷和/或之间 二氧化碳,通过降低压力和匀浆其也可以作为熔体,分离放宽。 最后,从所得到的匀浆中回收,在粉粒降低制剂可以与释放性质的所指的改进,特别是重链和最初的非水溶性化合物的生物利用度来实现。