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    • 3. 发明授权
    • Formulations and methods for lyophilization and lyophilates provided thereby
    • 从而提供冻干和冻干液的制剂和方法
    • US08858997B2
    • 2014-10-14
    • US13610335
    • 2012-09-11
    • Sven Jacobson
    • Sven Jacobson
    • A61K47/10A61K9/10A61K9/00A61K31/64A61K31/451A61K9/16A61K31/175A61K9/19
    • A61K9/1682A61K9/0019A61K9/1611A61K9/1623A61K9/19A61K31/175A61K31/451A61K31/64Y10S514/96
    • The present invention provides compositions, methods for lyophilizing compounds and making pharmaceutical compositions, and kits providing solutions and lyophilized formulations of compounds. The compositions, methods, and kits are particularly useful in pharmaceutical applications involving therapeutic agents that have low solubility at low pH and medium pH values. Certain embodiments provide methods for lyophilizing compounds in liquid solutions, which include the steps of: a) preparing aqueous solutions of a compound of interest in the absence of buffer; b) adjusting the pH to high values of pH in order to increase the solubility of the compound of interest; and c) freeze-drying the solution to provide a lyophilized solid composition. Aqueous solutions including buffer are also disclosed. Lyophilized formulations, including micronized and non-micronized powders, are provided.
    • 本发明提供组合物,冻干化合物和制备药物组合物的方法,以及提供化合物溶液和冻干制剂的试剂盒。 组合物,方法和试剂盒在涉及在低pH值和中等pH值下具有低溶解度的治疗剂的药物应用中特别有用。 某些实施方案提供了在液体溶液中冻干化合物的方法,其包括以下步骤:a)在不存在缓冲液的情况下制备目的化合物的水溶液; b)将pH调节至高的pH值,以增加目标化合物的溶解度; 和c)冷冻干燥该溶液以提供冻干固体组合物。 还公开了包括缓冲液的水溶液。 提供冻干制剂,包括微粉化和非微粉化粉末。
    • 4. 发明申请
    • Low dose no donor-containing transdermal patch
    • 低剂量无供体透皮贴剂
    • US20070202155A1
    • 2007-08-30
    • US11701964
    • 2007-02-01
    • Robert AngLudwig WeimannSven Jacobson
    • Robert AngLudwig WeimannSven Jacobson
    • A61K9/70A61K31/21
    • A61K9/7061A61K31/21A61K47/10
    • The present invention is drawn to a transdermal patch for the delivery of a nitroglycerin or other NO donor. The patch can comprise a backing layer, and a nitroglycerin-containing composition or other NO donor-containing composition which is supported at least in part by the backing layer. The transdermal patch can have a drug delivery zone defined by the area where the composition contacts an intact human skin site, and the transdermal patch can be formulated to deliver a nitric oxide donor, such as nitroglycerin, at from about 5 μg/hour to about 70 μg/hour. In one embodiment, the transdermal patch can provide a delivery rate at the drug delivery zone of from about 1 μg/cm2/day to about 600 μg/cm2/day. In another embodiment, the transdermal patch can contain from 6 wt % to 18 wt % of the nitric oxide donor, e.g., nitroglycerin. In each embodiment, the patch can contain at least 450 μg/cm2 of nitroglycerin.
    • 本发明涉及用于递送硝酸甘油或其他NO供体的透皮贴片。 贴片可以包含背衬层和含硝酸甘油的组合物或其它含NO供体的组合物,其至少部分由背衬层支撑。 透皮贴剂可以具有由组合物接触完整的人皮肤部位的区域限定的药物递送区,并且透皮贴剂可以配制成以约5mug /小时至约约5ug /小时递送一氧化氮供体,例如硝酸甘油 70杯/小时。 在一个实施方案中,透皮贴剂可以在药物递送区域提供约1mug / cm 2 /天至约600mug / cm 2 /天的输送速率 。 在另一个实施方案中,透皮贴剂可含有6重量%至18重量%的一氧化氮供体,例如硝酸甘油。 在每个实施方案中,贴片可以含有至少450杯/平方厘米的硝酸甘油。