Pharmaceutical oral dosage form containing a synthetic oligosaccharide

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.

主权项

1. A pharmaceutical formulation intended for oral administration containing a synthetic oligosaccharides containing 3 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, b) a lipophilic phase (B) consisting of triglyceride of fatty acids in an amount of 58 to 64% 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, 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, e) optionally, at least one hydrophilic solvent (E) in an amount of up to 15% 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),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.