Formulation strategies in stabilizing peptides in organic...

A - Human Necessities – 61 – K

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A61K 38/16 (2006.01) A61K 38/00 (2006.01) A61K 38/22 (2006.01) A61K 38/24 (2006.01) A61K 47/02 (2006.01) A61K 47/20 (2006.01) C07K 1/00 (2006.01) C07K 14/575 (2006.01) A61K 9/19 (2006.01) A61K 47/10 (2006.01) A61K 47/12 (2006.01) A61K 47/14 (2006.01) A61K 47/18 (2006.01) A61K 47/22 (2006.01)

Patent

CA 2472956

The invention relates to stabilized formulations of therapeutically active peptides, particularly PACAP 66. Formulations of the invention include a peptide containing at least one histidine residue, a transition metal salt and an organic solvent. The above formulations may contain peptides that have at least one asparagine residue and are acidified and dried (such as spray-dried or freeze-dried) before formulation preparation. Other formulations of the invention relate to stabilized formulations of PACAP 66 or peptides containing an asparagine residue, which are acidified and dried (such as spray-dried or freeze-dried) with or without a transition metal salt.

La présente invention a trait à des formulations stabilisées de peptides thérapeutiquement actifs, notamment le polypeptide d'activation de l'adénylcyclase pituitaire (PACAP 66). Les formulations de l'invention comprennent un peptide contenant au moins un résidu d'histidine, un sel de métal de transition et un solvant organique. Lesdites formulations peuvent contenir des peptides comportant au moins un résidu d'asparagine et sont acidifiés et séchés (par atomisation ou lyophilisation) avant la préparation de la formulation. D'autres formulations de l'invention concernent les formulations stabilisées de PACAP 66 ou de peptides contenant un résidu d'asparagine, qui sont acidifiés et séchés (par atomisation ou lyophilisation) avec ou sans un sel de métal de transition.

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