SYNTHETIC PENTASACCHARIDES HAVING SHORT HALF-LIFE AND HIGH ACTIVITY
    18.
    发明申请
    SYNTHETIC PENTASACCHARIDES HAVING SHORT HALF-LIFE AND HIGH ACTIVITY 有权
    具有短寿命和高活性的合成牙膏

    公开(公告)号:US20140315814A1

    公开(公告)日:2014-10-23

    申请号:US14126776

    申请日:2012-06-18

    IPC分类号: C07H3/06 A61K38/17 A61K31/702

    摘要: The invention concerns a pentasaccharide compound of formula (I) and the salts thereof.The invention also concerns a pharmaceutical composition comprising the synthetic pentasaccharide compound of formula (I) and its salts. The invention further concerns these compounds for use as a medicament, and in particular intended to treat blood clotting disorders, to prevent ischaemia reperfusion injury associated with solid organ transplantation, or to reduce the risk of blood clotting in an extracorporeal blood circuit during cardiac surgery, extracorporeal membrane oxygenation, or during circulatory assistance such as artificial heart.

    摘要翻译: 本发明涉及式(I)的五糖化合物及其盐。 本发明还涉及包含式(I)的合成五糖化合物及其盐的药物组合物。 本发明还涉及用作药物的这些化合物,特别是旨在治疗血液凝固病症,防止与实体器官移植相关的局部缺血再灌注损伤或降低心脏手术期间体外血液循环中血液凝固的风险, 体外膜氧合,或循环辅助如人造心脏。

    PHARMACEUTICAL ORAL DOSAGE FORM CONTAINING A SYNTHETIC OLIGOSACCHARIDE
    20.
    发明申请
    PHARMACEUTICAL ORAL DOSAGE FORM CONTAINING A SYNTHETIC OLIGOSACCHARIDE 有权
    含有合成寡糖的药物口服剂型

    公开(公告)号:US20120316132A1

    公开(公告)日:2012-12-13

    申请号:US13515965

    申请日:2010-12-17

    摘要: The present invention concerns a pharmaceutical formulation intended for oral administration containing a synthetic oligosaccharides containing one to 18 monosaccharide units and having a therapeutical activity or a pharmaceutically acceptable additions salt or solvate thereof wherein the formulation contains: a) the synthetic oligosaccharide (A) in an amount of up to 5% by weight of the total weight of the formulation, advantageously up to 1% by weight of the total weight of the formulation, b), a lipophilic phase (B) consisting of triglyceride of fatty acids in an amount of 50 to 80% by weight of the total weight of the formulation, advantageously of 50 to 70% by weight of the total weight of the formulation, c) at least one lipophilic surfactant (C) with HLB below 7 consisting of partial esters of polyol and fatty acids in an amount of 10 to 30% by weight of the total weight of the formulation, advantageously of 15 to 30% by weight of the total weight of the formulation, d) at least one hydrophilic surfactant (D) with HLB above 7 in an amount of up to 20% by weight of the total weight of the formulation, advantageously up to 15% by weight of the total weight of the formulation, e) optionally, at least one hydrophilic solvent (E) in an amount of up to 15% by weight of the total weight of the formulation, advantageously up to 10% by weight of the total weight of the formulation, (F) between 0 and 30% by weight of the total weight of the formulation of a chemical and/or physical stabilization agent (F), advantageously between 0 and 20% by weight of the total weight of the formulation, wherein when the formulation is in a form of a reverse emulsion or microemulsion and contains at least one hydrophilic solvent (E), the physical stabilization agent is present and is silicon dioxide.

    摘要翻译: 本发明涉及用于口服给药的药物制剂,其含有含有1至18个单糖单元并具有治疗活性或其药学上可接受的添加盐或溶剂合物的合成寡糖,其中所述制剂含有:a)合成寡糖(A) 最多达制剂总重量的5重量%的量,有利地高达制剂总重量的1重量%,b),由脂肪酸甘油三酯组成的亲脂相(B),其量为 50至80重量%的制剂总重量,有利地为制剂总重量的50至70重量%,c)至少一种HLB低于7的亲脂性表面活性剂(C),由多元醇的偏酯 和占制剂总重量的10至30重量%的脂肪酸​​,有利地为制剂总重量的15至30重量%,d)至少 一种HLB高于7的亲水性表面活性剂(D),其量高达制剂总重量的20重量%,有利地高达制剂总重量的15重量%,e)任选地至少一个 亲水性溶剂(E)的含量高达制剂总重量的15重量%,有利的是制剂总重量的10重量%,(F)0至30重量% 化学和/或物理稳定剂(F)的制剂的总重量,有利地为制剂总重量的0至20重量%,其中当制剂为反相乳液或微乳液的形式并且包含 至少一种亲水性溶剂(E),物理稳定剂存在并且是二氧化硅。