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    • 3. 发明申请
    • METHOD AND APPARATUS FOR THE FORMATION OF PARTICLES
    • 用于形成颗粒的方法和装置
    • WO1996000610A1
    • 1996-01-11
    • PCT/GB1995001523
    • 1995-06-30
    • UNIVERSITY OF BRADFORDHANNA, MazenYORK, Peter
    • UNIVERSITY OF BRADFORD
    • B01J02/04
    • A61K9/1688B01D11/0403B01D11/0407B01D11/0411B01D11/0488B01J2/04B01J3/008B01J3/02Y02P20/544
    • The invention provides a method for forming particles of a substance, by co-introducing into a particle formation vessel, in which the temperature and pressure are controlled, of a supercritical fluid; a solution or suspension of the substance in a first vehicle; and a second vehicle which is both substantially miscible with the first vehicle and substantially soluble in the supercritical fluid, in such a way that dispersion of the solution or suspension and the second vehicle, and extraction of the vehicles, occur substantially simultaneously and substantially immediately on introduction of the fluids into the vessel, by the action of the supercritical fluid. Preferably the solution/suspension of the substance is introduced separately from the second vehicle, in such a way that contact between the solution/suspension and the second vehicle occurs either substantially simultaneously with, or immediately before, their dispersion by the supercritical fluid and extraction of the vehicles by the supercritical fluid. The method allows a high degree of control over the size, shape, crystalline form and other physico-chemical properties of the particulate product. The invention also provides apparatus for carrying out such a method, using a coaxial nozzle to introduce the fluids into the particle formation vessel, and a particulate product made using the method or the apparatus.
    • 本发明提供了通过将超临界流体共同引入其中控制温度和压力的颗粒形成容器中来形成物质颗粒的方法; 该物质在第一种载体中的溶液或悬浮液; 以及第二种载体,其基本上与第一种载体混溶并且基本上可溶于超临界流体,使得溶液或悬浮液和第二载体的分散和载体的萃取基本上同时且基本上立即出现在 通过超临界流体的作用将流体引入容器中。 优选地,物质的溶液/悬浮液与第二载体分开引入,使得溶液/悬浮液和第二载体之间的接触基本上与超临界流体分散或同时或之前由超临界流体分散出来, 车辆由超临界流体。 该方法允许高度控制颗粒产品的尺寸,形状,结晶形式和其他物理化学性质。 本发明还提供了一种使用同轴喷嘴将流体引入颗粒形成容器中的这种方法的装置,以及使用该方法或装置制成的颗粒状产品。
    • 9. 发明申请
    • SUSTAINED-RELEASE NIFEDIPINE FORMULATION
    • 持续释放NIFEDIPINE配方
    • WO1989002738A1
    • 1989-04-06
    • PCT/GB1988000779
    • 1988-09-22
    • APS RESEARCH LIMITEDBARRY, Brian, WilliamMULLEY, Bryan, ArthurYORK, Peter
    • APS RESEARCH LIMITED
    • A61K31/44
    • A61K9/5047A61K9/1652A61K9/5026A61K31/44
    • A sustained-release nifedipine (4-(2'-nitrophenyl)-2,6-dimethyl-3,5-dicarbomethoxy-1,4-dihydropyridine) formulation comprising sufficient granules to provide a predetermined dose or number of doses of nifedipine, each of said granules having a diameter of between 0.5 and 2.5 mm and comprising: (a) a core comprising 100 parts of nifedipine and from 50 to 800 parts of hydroxypropylmethyl cellulose; and (b) a coating covering substantially the whole surface of the core and comprising 100 parts of a water insoluble but water swellable acrylic polymer and from 20 to 70 parts of a water soluble hydroxylated cellulose derivative, the weight of the coating being from 2 to 25 % of the weight of the core. A method for preparing the formulation is also provided.
    • 持续释放的硝苯地平(4-(2'-硝基苯基)-2,6-二甲基-3,5-二甲氧基-1,4-二氢吡啶)制剂,其包含足够的颗粒以提供硝苯地平的预定剂量或数量的剂量 所述颗粒的直径在0.5至2.5mm之间,并且包括:(a)包含100份硝苯地平的核心和50至800份的羟丙基甲基纤维素; 和(b)基本上覆盖芯的整个表面的涂层,并且包含100份水不溶性但可水溶胀的丙烯酸类聚合物和20至70份水溶性羟基化纤维素衍生物,涂层的重量为2至 核心重量的25%。 还提供了制备该制剂的方法。