PREPARATION OF SUBMICRON SIZED PARTICLES WITH POLYMORPH CONTROL AND NEW POLYMORPH OF ITRACONAZOLE
    2.
    发明申请
    PREPARATION OF SUBMICRON SIZED PARTICLES WITH POLYMORPH CONTROL AND NEW POLYMORPH OF ITRACONAZOLE 审中-公开
    具有聚合物控制和新戊酰胺的新型聚合物的亚型尺寸颗粒的制备

    公开(公告)号:WO2004054500A3

    公开(公告)日:2004-08-26

    申请号:PCT/US0324353

    申请日:2003-08-04

    Applicant: BAXTER INT

    CPC classification number: A61K9/14 A61K9/0019 A61K9/10 A61K31/495

    Abstract: The present invention provides a method of preparing particles with polymorph and size control of a pharmaceutical compound, the method including the steps of: (1) providing pharmaceutical compound in a first phase; (2) seeding the compound; (3) causing a phase change in the pharmaceutical compound to a second phase of a desired polymorphic form; and (4) wherein the mean particle size of the particles is less than 7µm. The present invention further provides a polymorphic form of itraconazole.

    Abstract translation: 本发明提供一种制备具有药物化合物的多晶型物和粒度控制的颗粒的方法,所述方法包括以下步骤:(1)在第一相中提供药物化合物; (2)接种化合物; (3)引起药物化合物相变为所需多晶型物的第二相; 和(4)其中颗粒的平均粒度小于7μm。 本发明还提供了伊曲康唑的多晶型物。

    Method for preparing submicron particle suspensions

    公开(公告)号:NZ526608A

    公开(公告)日:2006-06-30

    申请号:NZ52660801

    申请日:2001-12-20

    Applicant: BAXTER INT

    Abstract: A method for preparing submicron sized particles of a pharmaceutically-active compound, the solubility of which is greater in a water-miscible first solvent than in a second solvent which is aqueous is disclosed, wherein the process comprises the steps of: (i) dissolving the pharmaceutically-active compound in the water-miscible first solvent to form a solution, the first solvent being selected from the group consisting of N methyl-2-pyrrolidinone, 2-pyrrolidone, dimethyl sulfoxide, dimethylacetamide, lactic acid, methanol, ethanol, isopropanol, 3-pentanol, n-propanol, glycerol, butylene glycol, ethylene glycol, polypropylene glycol, mono- and diacylated monoglycerides, dimethyl isosorbide, acetone, dimethylformamide, 1,4-dioxane, ethyl acetate, propyl acetate, polyethylene glycol, polyethylene glycol esters, polyethylene glycol sorbitans, polyethylene glycol monoalkyl ethers, polypolypropylene glycol, polypropylene alginate, polypolypropylene glycol-10 butanediol, polypolypropylene glycol-10 methyl glucose ether, polypolypropylene glycol-20 methyl glucose ether, polypolypropylene glycol-15 stearyl ether, polypolypropylene glycol dicaprylate, polypropylene glycol dicaprate, polypropylene glycol laurate; (ii) mixing the solution with the second solvent to define a pre-suspension; and (iii) adding energy to the pre-suspension to form particles having an average effective particle size of less than about 2 micron, and said adding energy step comprises homogenization, counter-current flow homogenization, microfluidization or sonication.

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