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    • 2. 发明授权
    • Pharmaceutical oral dosage form containing a synthetic oligosaccharide
    • 含有合成寡糖的药物口服剂型
    • US09259389B2
    • 2016-02-16
    • US13515965
    • 2010-12-17
    • Julien MeissonnierNathalie SicreGuillaume SabateGuy DubreucqVanessa Nancy-PorteboisMaurice Petitou
    • Julien MeissonnierNathalie SicreGuillaume SabateGuy DubreucqVanessa Nancy-PorteboisMaurice Petitou
    • A61K31/70A61K9/107A61K9/48A61K31/702
    • A61K9/107A61K9/4891A61K31/702
    • 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.
    • 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。
    • 6. 发明申请
    • PHARMACEUTICAL ORAL DOSAGE FORM CONTAINING A SYNTHETIC OLIGOSACCHARIDE
    • 含有合成寡糖的药物口服剂型
    • US20120316132A1
    • 2012-12-13
    • US13515965
    • 2010-12-17
    • Julien MeissonnierNathalie SicreGuillaume SabateGuy DubreucqVanessa Nancy-PorteboisMaurice Petitou
    • Julien MeissonnierNathalie SicreGuillaume SabateGuy DubreucqVanessa Nancy-PorteboisMaurice Petitou
    • A61K31/727A61P7/02A61P9/10A61K31/702
    • A61K9/107A61K9/4891A61K31/702
    • 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.
    • 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。