Patent ID: 7906479
Filing Date: 2011-03-15
Classification: A61K,A61P

Abstract:
1. A composition, comprising: a slightly soluble salt or complex of a basic peptide and an aliphatic or aromatic organic carboxylic acid; a solvent or a solvent mixture; and at least one of a pharmaceutical excipient, carrier or bulking agent; wherein the basic peptide is cetrorelix, the aliphatic or aromatic organic carboxylic acid is selected from the group consisting of embonic acid, citric acid, palmitic acid, salicylic acid, tannic acid, stearic acid, benzoic acid and cinnamic acid, the composition is a sterile homogeneous suspension of the slightly soluble salt or complex, which can be administered parenterally, the at least one of a pharmaceutical excipient, carrier or bulking agent is at least one selected from the group consisting of mannitol, sorbitol, xylitol, trehalose, glucose, soluble starch, sucrose and saccharose, and the composition is obtained by a process, comprising: under aseptic conditions, i) mixing a sterile solution comprising at least one of a salt or a complex of a basic peptide and of an aliphatic or aromatic organic carboxylic acid and/or salts thereof in a solvent or solvent mixture, optionally with the addition of solubility-increasing and/or agglomeration-suppressing additives, or ii) combining and mixing a sterile solution of a salt or complex of at least one basic peptide in a solvent or solvent mixture and a sterile solution of an aliphatic or aromatic organic carboxylic acid and/or salts thereof in a solvent or solvent mixture, optionally with the addition of solubility-increasing and/or agglomeration-suppressing additives, b) generating, by mixing and addition of a diluent or diluent mixture in one or more steps, a suspension of a slightly soluble basic peptide complex of the basic peptide with the carboxylic acid, which complex precipitates at the latest after addition of the diluent or diluent mixture, c) depleting, while mixing in a continuous or stepwise separation process, the solvent or solvent mixture, free non-peptide ions, excess carboxylic acid and optionally added solubility-increasing and/or agglomeration-suppressing additives in the resulting suspension, with the liquid content of the suspension being reduced to an extent enabling lyophilization of the suspension of the slightly soluble basic peptide complex and optionally further diluent or diluent mixture being added in one or more steps, and d) adding to the slightly soluble basic peptide complex, while mixing the sterile suspension during c) and/or thereafter, the at least one pharmaceutical excipient, carrier or bulking agent.