Preparation and use of a stable formulation of allosteric...

A - Human Necessities – 61 – K

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A61K 31/403 (2006.01) A61K 31/195 (2006.01) A61K 31/196 (2006.01) A61K 47/12 (2006.01) A61K 47/18 (2006.01) A61K 49/10 (2006.01)

Patent

CA 2481669

A pharmaceutical composition of 2-[4-[2-[(3,5-dimethylphenyl)amino]-2- oxoethyl]phenoxyl]-2-methyl-proprionic acid or its physiologically acceptable salts suitable for parenteral administration includes an aqueous formulation of 2-[4-[2-[(3,5-dimethylphenyl)amino]-2-oxoethyl]phenoxyl]-2-methyl- proprionic acid or its physiologically acceptable salt and a buffer to maintain the pH from about 6 to about 11. The composition in accordance with the invention reduces the amount of particulate matter that forms in solution after heat sterilization. The invention also includes a process for making a pharmaceutical composition of 2-[4-[2-[(3,5-dimethylphenyl)amino]-2- oxoethyl]phenoxyl]-2-methyl-proprionic acid or its physiologically acceptable salt that has a shelf life in excess of thirty days and is useful in parental administration.

La présente invention concerne une composition à base d'acide 2-[4-[2-[(3,5-diméthylphényl)amino]-2-oxoéthyl]phénoxyl]-2-méthyl-proprionique, ou de son sel physiologiquement admis, et se prêtant à l'administration parentérale. Cette composition comprend une formulation aqueuse d'acide 2-[4-[2-[(3,5-diméthylphényl)amino]-2-oxoéthyl]phénoxyl]-2-méthyl-proprionique ou de son sel physiologiquement admis et d'un tampon permettant de maintenir le pH dans une plage allant d'environ 6 à environ 11. Cette composition réduit la quantité de matière particulaire passant en solution après stérilisation par la chaleur. L'invention concerne également un procédé pour fabriquer une composition pharmaceutique d'acide 2-[4-[2-[(3,5-diméthylphényl)amino]-2-oxoéthyl]phénoxyl]-2-méthyl-proprionique, ou de son sel physiologiquement admis, dont la durée de stockage dépasse les 30 jours, et qui se prête à l'administration parentérale.

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