Sustained release salts of pharmaceutically active peptides...

A - Human Necessities – 61 – K

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A61K 47/48 (2006.01) A61K 9/10 (2006.01) A61K 9/14 (2006.01) A61K 9/19 (2006.01) A61K 38/09 (2006.01)

Patent

CA 2360110

A pharmaceutical composition of a pharmacologically-active polypeptide which provides sustained release of the polypeptide over an extended period of time. In one embodiment, the composition comprises a luteinizing hormone releasing hormone (LHRH) analogue and a carrier macromolecule, such as carboxymethylcellulose. The composition is manufactured by removing the counterions of the LHRH analogue and the carrier macromolecule and combining them such that a water-insoluble salt forms.

Cette invention se rapporte à des compositions pharmaceutiques à libération prolongée, comprenant un sel insoluble dans l'eau d'un peptide ionique pharmaceutiquement actif et d'un excipient à macromolécule contre-ionique. Ce peptide peut être un antagoniste de LHRH, tel que Cetrorelix, et la macromolécule peut être un polysaccharide anionique, tel que la carboxyméthylcellulose. On prépare ce sel en utilisant des échangeurs d'ions, afin de retirer séparément les contre-ions du peptide et de l'excipient macromoléculaire, en vue de former des ions de peptide/macromolécule libres. Ces ions de peptide et de macromolécule libres sont ensuite combinés pour former le sel peptide-macromolécule insoluble dans l'eau.

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