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    • 5. 发明申请
    • STABLE NANOSIZED AMORPHOUS DRUG
    • 稳定的纳米非晶药物
    • WO2008054508A2
    • 2008-05-08
    • PCT/US2007/009264
    • 2007-04-13
    • ALZA CORPORATIONWEI, MinXU, ShuqianLAM, Andrew, C.
    • WEI, MinXU, ShuqianLAM, Andrew, C.
    • A61K9/146A61K9/145A61K31/445
    • Disclosed is a population of nanoparticles, together with methods of making a population of nanoparticles, wherein one or more of the nanoparticles includes: an amorphous drug core having an effective diameter less than or equal to about 2.0 microns, wherein the amorphous drug core is substantially free of dopant, and wherein the amorphous drug core includes a drug with properties that satisfy the following relationships: a glass transition temperature greater than or equal to about 50 Deg. C, a glass forming ability less than or equal to about 0.85; and water solubility at 25 Deg. C less than or equal to about 1 mg/ml; and at least one stabilizer adsorbed on a surface of the amorphous drug core; and wherein the population of nanoparticles exhibits greater than about six months amorphous stability.
    • 公开了纳米颗粒群体以及制备纳米颗粒群体的方法,其中一个或多个纳米颗粒包括:具有小于或等于约2.0微米的有效直径的无定形药物核心 其中所述无定形药心基本上不含掺杂剂,并且其中所述无定形药心包括具有满足以下关系的性质的药物:玻璃化转变温度大于或等于约50℃。 C,玻璃形成能力小于或等于约0.85; 和在25℃下的水溶性。 C小于或等于约1mg / ml; 和至少一种吸附在无定形药心表面上的稳定剂; 并且其中纳米颗粒群表现出大于约六个月的非晶稳定性。