Fine particle and pharmaceutical preparation

C - Chemistry – Metallurgy – 08 – G

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Details

C08G 81/00 (2006.01) A61K 9/14 (2006.01) A61K 9/50 (2006.01) A61K 31/7105 (2006.01) A61K 31/711 (2006.01) A61K 38/00 (2006.01) A61K 47/32 (2006.01) A61K 47/34 (2006.01)

Patent

CA 2600085

A microparticle containing an amphiphilic polymer, composed of an internal nucleus consisting of a hydrophilic segment of the amphiphilic polymer and a hydrophobic outer layer consisting of a hydrophobic segment of the amphiphilic polymer, wherein a surface modifier binds to the hydrophobic outer layer. This microparticle effectively encloses a hydrophilic large-molecular-weight-having protein/peptide pharmaceutical, nucleic acid pharmaceutical, etc. in the internal nucleus consisting of a hydrophilic segment of amphiphilic polymer, thus being suitable for in vivo stabilization and absorption promotion.

La présente invention concerne une microparticule contenant un polymère amphiphile, composé d~un noyau interne comprenant un segment hydrophile du polymère amphiphile et une couche externe hydrophobe comprenant un segment hydrophobe du polymère amphiphile, dans laquelle un modificateur de surface se lie à la couche externe hydrophobe. Cette microparticule renferme de manière efficace dans son noyau interne, qui est composé d~un segment hydrophile du polymère amphiphile, une substance pharmaceutique protéique/peptidique hydrophile de haut poids moléculaire, une substance pharmaceutique à base d~acide nucléique hydrophile de haut poids moléculaire, etc. ; ladite microparticule convient donc à la stabilisation et à la stimulation d~absorption in vivo.

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