Transdermal therapeutic system with protection against hydrolysis
    2.
    发明授权
    Transdermal therapeutic system with protection against hydrolysis 失效
    透皮治疗系统,防止水解

    公开(公告)号:US5932239A

    公开(公告)日:1999-08-03

    申请号:US793724

    申请日:1997-06-12

    摘要: A transdermal therapeutic system (TTS) comprising an active substance which is sensitive to hydrolysis, and having a layer-like structure comprising a backing layer impermeable to moisture and active substance, a matrix comprising the active substance, and optionally a protective layer covering the matrix is characterized in that the matrix contains a water-binding component.

    摘要翻译: PCT No.PCT / EP95 / 03204 Sec。 371日期:1997年6月12日 102(e)日期1997年6月12日PCT提交1995年8月12日PCT公布。 出版物WO96 / 06600 日期1996年3月7日一种透皮治疗系统(TTS),其包含对水解敏感的活性物质,并且具有包含不透水分和活性物质的背层的层状结构,包含活性物质的基质和任选的 覆盖基质的保护层的特征在于,基质含有水结合成分。

    Formulation comprising histone deacetylase inhibitors
    3.
    发明申请
    Formulation comprising histone deacetylase inhibitors 审中-公开
    含有组蛋白脱乙酰酶抑制剂的制剂

    公开(公告)号:US20070232528A1

    公开(公告)日:2007-10-04

    申请号:US11587979

    申请日:2005-05-02

    IPC分类号: A61K38/12 A61K31/19

    摘要: The present invention relates to an orally available galenics formulation of Valproic Acid or derivatives thereof exhibiting a specific bi-phasic pharmacokinetic profile optimized for maximum inhibition of histone deacetylases in a therapeutic setting. This specific galenics formulation is designed for the treatment of malignant diseases and diseases associated with hypoacetylation of histones or in which induction of hyperacetylation has a beneficial effect, e.g., by induction of differentiation and/or apoptosis. Due to the bi-phasic release pattern the resulting pharmacokinetic profile is able to inhibit HDAC target enzymes most efficiently and to subsequently induce histone hyperacetylation in a rapid as well as a long-lasting fashion. This profile secures the efficient modulation of a desired target gene expression profile which contributes to the therapeutic benefit.

    摘要翻译: 本发明涉及一种口服可利用的丙戊酸或其衍生物的制剂,其表现出针对在治疗环境中最大程度抑制组蛋白脱乙酰酶而优化的特定双相药代动力学特征。 这种具体的加仑制剂被设计用于治疗与组蛋白的低乙酰化相关的恶性疾病和疾病,或者其中高乙酰化的诱导具有有益效果,例如通过诱导分化和/或凋亡。 由于两相释放模式,所得的药物动力学特征能够最有效地抑制HDAC靶酶,并且随后以快速和持久的方式诱导组蛋白超乙酰化。 该概况确保有助于治疗益处的期望靶基因表达谱的有效调节。