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    • 7. 发明授权
    • Pharmaceutical nanosuspensions for medicament administration as systems
with increased saturation solubility and rate of solution
    • 用于药物给药的药物纳米悬浮液作为具有增加的饱和溶解度和溶液速率的系统
    • US5858410A
    • 1999-01-12
    • US836305
    • 1997-06-19
    • Rainer H. MullerRobert BeckerBernd KrussKatrin Peters
    • Rainer H. MullerRobert BeckerBernd KrussKatrin Peters
    • A61K9/107A61K9/10A61K9/14A61K9/51B01F17/56B01J13/00
    • A61K9/145A61K9/0019A61K9/10
    • Provided is a drug carrier comprising particles of at least one pure active compound which is insoluble, only sparingly soluble or moderately soluble in water, aqueous media and/or organic solvents, wherein said active ingredient is solid at room temperature and has an average diameter, determined by photon correlation spectroscopy (PCS) of 10 nm to 1,000 nm, the proportion of particles larger than 5 .mu.m in the total population being less than 0.1% (number distribution determined with a Coulter counter), and, when introduced into water, aqueous media and/or organic solvents, the active compound has an increased saturation solubility and an increased rate of dissolution compared with powders of the active compound prepared using an ultrasonic probe, a ball mill or a pearl mill, the solid particles having been comminuted, without prior conversion into a melt, by using cavitation or shearing and impact forces with introduction of a high amount of energy.
    • PCT No.PCT / EP95 / 04401 Sec。 371日期:1997年6月19日 102(e)日期1997年6月19日PCT提交1995年11月9日PCT公布。 公开号WO96 / 14830 日期1996年5月23日提供了一种药物载体,其包含至少一种纯的活性化合物的颗粒,所述纯活性化合物是不溶的,仅微溶或适度溶于水,水性介质和/或有机溶剂,其中所述活性成分在室温下为固体, 通过10nm至1000nm的光子相关光谱(PCS)确定的平均直径,总体中大于5μm的颗粒的比例小于0.1%(用库尔特计数器确定的数量分布),以及当 引入水,水性介质和/或有机溶剂中,与使用超声波探针,球磨机或珍珠磨机制备的活性化合物的粉末相比,活性化合物具有增加的饱和溶解度和增加的溶解速率,固体颗粒 通过在引入大量能量的情况下使用空化或剪切和冲击力,已经粉碎,没有预先转化成熔体。