Pharmaceutical composition comprising factor viii and...

A - Human Necessities – 61 – K

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A61K 38/37 (2006.01) A61K 45/08 (2006.01) A61K 47/24 (2006.01) A61K 47/34 (2006.01) A61P 7/04 (2006.01)

Patent

CA 2329768

A pharmaceutical composition for parenteral administration comprising a therapeutically effective amount of a protein or polypeptide and substantially neutral colloidal particles. The particles comprise approximately 1-20 mole percent of an amphipathic lipid derivatized with a biocompatible hydrophilic polymer which carries substantially no net charge. The protein or polypeptide is capable of externally binding the colloidal particles, or is capable of binding polyethylene glycol, and is not encapsulated in the colloidal particles. A preferred protein is factor VIII, whose half-life is extended and which is protected from serum inhibitor antibodies by injecting it as a component of the composition.

La présente invention concerne une composition pharmaceutique pour administration parentérale comprenant une quantité thérapeutiquement efficace d'une protéine ou d'un polypeptide et des particules colloïdales sensiblement neutres. Les particules présentent une teneur molaire d'environ 1-20 % d'un lipide amphipathique obtenu par dérivatisation avec un polymère hydrophile biocompatible sensiblement exempt de charge nette. Cette protéine ou ce polypeptide, qui sont capables d'une liaison externe avec les particules colloïdales ou sont capables d'une liaison avec le polyéthylène-glycol, ne sont pas encapsulés dans les particules colloïdales. La protéine préférée est le facteur VIII dont la demi-vie est étendue et que l'on protège des anticorps à inhibiteurs sériques en l'injectant comme composant de la composition.

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