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    • 4. 发明申请
    • QUICK RELEASE PHARMACEUTICAL COMPOSITIONS OF DRUG SUBSTANCES
    • 快速释放药物药物组合物
    • WO00015195A1
    • 2000-03-23
    • PCT/DK1999/000480
    • 1999-09-10
    • A61K9/14A61K9/16A61K9/20A61K9/28A61K9/48A61K31/542A61K33/10A61K33/12A61K45/00A61K47/02A61K47/04A61K47/26A61P1/04A61P5/46A61P25/04A61P25/24A61P29/00A61P43/00
    • A61K9/2009A61K9/1611
    • The present invention relates to an oral modified release pharmaceutical composition for the administration of a therapeutically and/or prophylactically effective amount of an active substance (a drug substance) to obtain a relatively fast or quick onset of the therapeutic and/or prophylactic effect. The drug substances contained in a modified release pharmaceutical composition according to the invention are suitably a drug substance which has a very low solubitity under acidic conditions, i.e. under conditions similar to those present in the stomach and/or drug substances which have a pKa value below about 5.5 such as in a range of from about 4 to about 5. The composition is based on a powder comprising a therapeutically and/or prophylactically active substance and has such a particle size that: when the powder is subjected to a sieve analysis, then at least about 90 % w/w of the particles passes through sieves 180 mu m and the powder is contacted with an aqueous medium to form a particulate composition, which has such a particle size that when the particulate composition is subjected to a sieve analysis, then at least about 50 % w/w of the particles passes through sieve 180 mu m. Furthermore, the composition, when tested in accordance with the dissolution method (I) defined herein employing 0.07 N hydrochloric acid as dissolution medium, releases at least about 50 % w/w of the active substance within the first 20 min of the test.
    • 本发明涉及用于给予治疗和/或预防有效量的活性物质(药物物质)以获得治疗和/或预防效果相对快速或快速发作的口服释放药物组合物。 包含在根据本发明的调释释放药物组合物中的药物物质合适地是在酸性条件下具有非常低的溶解度的药物物质,即在与pKa值低于pKa值的胃和/或药物物质中存在的条件相似的条件下 约5.5,例如在约4至约5的范围内。该组合物基于包含治疗和/或预防活性物质的粉末,并且具有如下的粒径:当粉末进行筛分分析时,则 至少约90%w / w的颗粒通过180μm的筛子,并且粉末与水性介质接触以形成颗粒组合物,其具有这样的颗粒尺寸,即当颗粒组合物进行筛分分析时, 那么颗粒的至少约50%w / w通过筛子180μm。 此外,当根据本文定义的溶解方法(I)使用0.07N盐酸作为溶解介质测试时,组合物在试验的最初20分钟内释放至少约50%w / w的活性物质。
    • 8. 发明申请
    • PHENOXYBENZAMINE TRANSDERMAL COMPOSITION
    • 苯氧苯胺复合物
    • WO2014201083A3
    • 2015-05-14
    • PCT/US2014041846
    • 2014-06-11
    • PROFESSIONAL COMPOUNDING CT S OF AMERICA
    • GLASNAPP ANDREW B
    • A61K33/12
    • A61K31/138
    • A phenoxybenzamine transdermal composition for treating neuropathic pain is disclosed. The phenoxybenzamine transdermal composition may include phenoxybenzamine in a concentration of about 5 mg/g to about 120 mg/g, with about 15 mg/g being preferred, in combination with a pharmaceutically suitable permeation enhancer that may be included in amounts of about 20% by weight to about 99.95% by weight, with about 50% by weight being preferred. Permeation enhancer composition within disclosed phenoxybenzamine transdermal composition may improve penetration of phenoxybenzamine in a patient's tissue or skin. The phenoxybenzamine transdermal composition may provide a long duration blockade of sensitized pain receptors of 24 hours or more, resulting in an effective treatment for neuropathic pain with lower concentrations of phenoxybenzamine and requiring fewer applications.
    • 公开了用于治疗神经性疼痛的苯氧基苯甲胺透皮组合物。 苯氧基苯甲胺透皮组合物可以包括浓度为约5mg / g至约120mg / g的苯氧基苯甲胺,其中优选约15mg / g,与药学上合适的渗透增强剂组合,其可以以约20% 至约99.95重量%,优选约50重量%。 所公开的苯氧基苯甲胺透皮组合物中的渗透增强剂组合物可以改善苯氧基苯甲胺在患者组织或皮肤中的渗透。 苯氧基苯甲胺透皮组合物可提供24小时或更长时间的致敏疼痛受体的长时间阻断,导致用较低浓度苯氧基苯甲胺的神经性疼痛的有效治疗,并且需要较少的应用。