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    • 4. 发明申请
    • METHOD FOR PRODUCING POWDERY PARTICLE-REDUCED FORMULATIONS WITH THE AID OF COMPRESSED GASES
    • 利用压缩气体帮助生产粉状颗粒减少制剂的方法
    • WO01003671A2
    • 2001-01-18
    • PCT/EP2000/006709
    • 2000-07-13
    • 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 二氧化碳通过减压放松并从匀浆中分离出来,也可以以熔体形式存在。 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。
    • 7. 发明申请
    • PROCESS FOR FORMING A DISPERSION OF POLYTETRAFLUOROETHYLENE
    • 形成聚四氟乙烯分散体的方法
    • WO99010416A1
    • 1999-03-04
    • PCT/US1998/017129
    • 1998-08-19
    • C08J3/12C08F2/16C08F8/00C08J3/09C08J3/16C08J3/28C10M147/02C10M177/00C08J3/11
    • C08J3/09C08J2327/18C10M147/02C10M177/00C10M2211/06C10M2213/02C10M2213/062Y10S516/922
    • A process for forming a dispersion of dry polytetrafluoroethylene particles in an organic carrier fluid comprising the steps of: a) surface functionalizing the polytetrafluoroethylene particles having an average primary particle size of less than 1 micron with electron beam or gamma irradiation of at least 4 Mrad in the presence of atmospheric oxygen and water or selecting polytetrafluoroethylene particles having an average primary particle size of less than 1 micron that have been subjected to electron beam or gamma irradiation of at least 4 Mrad in the presence of atmospheric oxygen and water to functionalize the particle surface; b) mixing the irradiated particles with the liquid and at least one dispersant in an amount sufficient to stabilize the dispersion to form a mixture; c) passing the mixture, at least once, through a plurality of nozzles within a liquid-jet interaction chamber at a pressure of at least 1000 psi to deagglomerate the polytetrafluoroethylene particles.
    • 一种在有机载体流体中形成干燥的聚四氟乙烯颗粒的分散体的方法,包括以下步骤:a)使用至少4Mrad的电子束或γ照射使平均初级粒径小于1微米的聚四氟乙烯颗粒表面官能化 存在大气中的氧和水,或选择平均初级粒径小于1微米的聚四氟乙烯颗粒,其在大气氧和水的存在下进行至少4Mrad的电子束或γ照射以使颗粒表面官能化 ; b)将辐射的颗粒与液体和至少一种分散剂混合,其量足以使分散体稳定以形成混合物; c)使混合物至少一次通过喷液相互作用室内的多个喷嘴在至少1000psi的压力下使聚四氟乙烯颗粒解聚。