ORAL DOSAGE FORM
    3.
    发明申请
    ORAL DOSAGE FORM 审中-公开
    口服剂型

    公开(公告)号:US20100291206A1

    公开(公告)日:2010-11-18

    申请号:US12602317

    申请日:2008-06-02

    摘要: A pharmaceutical or nutraceutical tablet for oral administration comprising at least two fatty acids or derivatives thereof and cyclodextrin. Surprisingly, we have now found that fatty acids or derivatives thereof, especially fatty acid esters, preferably in the form of complexes with cyclodextrins prepared as stable solid materials, can easily be transformed into tablets with very high concentration of the fatty acid compound. The present inventors have realised that ideal dosage forms for these compounds are tablets and these are readily swallowed and are cheap to manufacture. In particular, the inventors have found that tablets containing complexes of fatty acids or derivatives thereof with cyclodextrin can be prepared by direct compression and moreover they can be prepared having a very high concentration of the desired active agent.

    摘要翻译: 一种用于口服给药的药物或营养片剂,其包含至少两种脂肪酸或其衍生物和环糊精。 令人惊奇的是,现在我们已经发现脂肪酸或其衍生物,特别是脂肪酸酯,优选与作为稳定固体物质制备的环糊精的复合物形式,可以容易地转化成具有非常高浓度脂肪酸化合物的片剂。 本发明人已经认识到,这些化合物的理想剂型为片剂,容易吞咽,制造便宜。 特别地,本发明人已经发现,含有脂肪酸或其衍生物与环糊精的复合物的片剂可以通过直接压片制备,而且它们可以制备成具有非常高浓度的所需活性剂。

    Modulators of Preripheral 5-Ht Receptors
    6.
    发明申请
    Modulators of Preripheral 5-Ht Receptors 有权
    Preripheral 5-Ht受体的调节剂

    公开(公告)号:US20070254874A1

    公开(公告)日:2007-11-01

    申请号:US10583829

    申请日:2004-12-23

    摘要: Novel modulators of 5-HT4 receptors have been developed which have a selectivity for peripheral receptors rather than those of the central nervous systems. Theses include novel derivatives of known modulators as well as entirely novel entities. Surprisingly, the derivatised compounds of the known modulators maintain a high binding affinity to 5-HT4 receptors, despite the presence of an acidic moiety at the end of an optional chain. The entirely novel entities also exhibit good binding affinity to 5-HT4 receptors. All of the compounds of the invention have a common motif which includes a basic nitrogen moiety and an acidic moiety. The compounds of the invention, due at least in part to their high ionisation potential at physiological pH, have the unique properties of selectively for peripheral 5HT4 receptors over those of the CNS, good binding affinity, and selectively of 5HT4 receptors over other serotonin receptors.

    摘要翻译: 已经开发了具有对外周受体而不是中枢神经系统的选择性的5-HT 4受体的新型调节剂。 论文包括已知调制剂的新型衍生物以及完全新颖的实体。 令人惊奇的是,尽管已知调节剂的衍生化合物在任选链的末端存在酸性部分,但仍保持与5-HT 4受体的高结合亲和力。 完全新颖的实体也表现出对5-HT4受体的良好的结合亲和力。 本发明的所有化合物都具有共同的基序,其包括碱性氮部分和酸性部分。 本发明的化合物至少部分地由于其在生理pH下的高电离电位具有对于周围5HT4受体的选择性优于CNS的那些的独特性质,良好的结合亲和力以及5HT4受体的选择性超过其他5-羟色胺受体。