Method of forming polypeptide particles

A - Human Necessities – 61 – K

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A61K 38/02 (2006.01) A61K 9/10 (2006.01) A61K 9/16 (2006.01) A61K 9/50 (2006.01) A61K 47/30 (2006.01) C07K 1/00 (2006.01) C07K 1/36 (2006.01)

Patent

CA 2424069

A process for producing a dispersion of polypeptide particles characterized by comprising adding a water-miscible organic solvent in which a polypeptide is insoluble to a frozen aqueous solution containing the polypeptide and a phase separation inducing agent, and then dissolving the phase separation inducing agent in the frozen matter and ice; a dispersion of polypeptide particles obtained by the above process; polypeptide particles obtained by removing the phase separation inducing agent, water and the water-miscible organic solvent from the above polypeptide particle dispersion; a process for producing microspheres characterized by comprising dissolving a biodegradable polymer in a volatile and water-immiscible organic solvent, dispersing the above- described polypeptide particles in this solution, dispersing it in an aqueous phase to give an O/W type emulsion and then distilling off the water- immiscible organic solvent; and microsphere preparations thus obtained.

L'invention concerne un procédé de production d'une dispersion de particules polypeptidiques, caractérisé en ce qu'il consiste à ajouter un solvant organique hydrosoluble dans lequel un polypeptide est insoluble, à une solution aqueuse gelée contenant le polypeptide et un agent induisant la séparation de phase, et à ensuite dissoudre l'agent induisant la séparation de phase dans l'élément gelé et de la glace. L'invention concerne également une dispersion de particules polypeptidiques obtenues à l'aide du procédé susmentionné, ainsi que des particules polypeptidiques obtenues par élimination de l'agent induisant la séparation de phase, de l'eau et du solvant organique hydrosoluble de la dispersion de particules polypeptidiques susmentionnée. L'invention concerne également un procédé de production de microsphères, caractérisé en ce qu'il consiste à dissoudre un polymère biodégradable dans un solvant organique non hydrosoluble volatil, à disperser les particules polypeptidiques décrites ci-dessus dans cette solution, à disperser cette dernière en phase aqueuse pour obtenir une émulsion de type O/W et à ensuite distiller le solvant organique non hydrosoluble. L'invention concerne également les préparations de microsphères ainsi obtenues.

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