Suspension formulations of insulinotropic peptides and uses...

A - Human Necessities – 61 – K

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A61K 9/00 (2006.01) A61K 9/70 (2006.01) A61K 38/26 (2006.01) C07K 7/06 (2006.01) C07K 14/605 (2006.01)

Patent

CA 2683610

A suspension formulation of an insulinotropic peptide (e.g., glucagon-like peptide- 1 (GLP-1) or exenatide) is described. The suspension formulation comprises (i) a non¬ aqueous, single-phase vehicle, comprising one or more polymer and one or more one solvent, wherein the vehicle exhibits viscous fluid characteristics, and (ii) a particle formulation comprising the insulinotropic peptide, wherein the peptide is dispersed in the vehicle. The particle formulation further includes a stabilizing component comprising one or more stabilizers, for example, carbohydrates, antioxidants, amino acids, and buffers. Devices for delivering the suspension formulations and methods of use are also described.

L'invention concerne une formulation en suspension d'un peptide insulinotrope (par ex., peptide 1 ressemblant au glucagon (GLP-1) ou exénatide). La formulation en suspension comprend (i) un excipient non aqueux à simple phase, comprenant un ou plusieurs polymères et un ou plusieurs solvants, ledit excipient possédant des caractéristiques fluides visqueuses, et (ii) une formulation particulaire comprenant le peptide insulinotrope, ledit peptide étant dispersé dans l'excipient. La formulation particulaire comprend en outre un composant de stabilisation comprenant un ou plusieurs stabilisateurs, par exemple, des hydrates de carbone, des antioxydants, des acides aminés et des tampons. Des appareils pour distribuer les formulations en suspension et des procédés d'utilisation sont également inclus.

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