Solid dispersion containing sialic acid derivative

C - Chemistry – Metallurgy – 07 – J

Patent

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C07J 17/00 (2006.01) A61K 31/70 (2006.01) C07J 41/00 (2006.01)

Patent

CA 2328085

The invention provides a medicament comprising a sialic acid derivative represented by the following formula and have superior solubility and absorbability. A solid dispersion comprising a water-soluble macromolecule such as hydroxypropylmethylcellulose and a sialic acid derivative dispersed in the water-soluble macromolecule and represented by the following formula (I): (see figure I) [R1 represents a steroid compound residue R2 represents hydrogen atom or a C1- C4 alkyl group, R3 represents a C1-C15 alkyl group etc.; X represents an oxygen atom or a sulfur atom], e.g., 3.alpha.-[N-(5-acetamido-3,5-dideoxy-2-O-methyl-.alpha.-D- glycero-D- galacto-2-noneuropyranosonyl)amino]cholestane.

L'invention concerne un médicament renfermant un dérivé d'acide sialique, représenté par la formule (I) ci-après, et présentant une excellente stabilité et une excellente absorbabilité. Ce médicament est une dispersion solide comprenant un polymère soluble dans l'eau, tel que l'hydroxypropylméthylcellulose, dans lequel est dispersé un dérivé d'acide sialique représenté par la formule (I), (où R<1> représente un reste d'un composé stéroïde; R<2> représente hydrogène ou C1-4alkyle; R<3> représente C1-15 alkyle, etc.; et X représente oxygène ou soufre), par exemple, 3 alpha -[N-(5-acétamido-3,5-didéoxy-2-O-méthyl- alpha -D-glycéro-D-galacto-2-nonulopyranosonyl)amino]cholestane.

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