Solid ionic complex of LHRH analogue containing 5-20 amino acids with a weight ratio of carrier:analogue 0.5:1 to 0.1:1 suitable for administration with in a syringe

摘要

Sustained delivery formulations comprising a water-insoluble complex of a peptide and a carrier macromolecule are described. The formulations allow for loading of high concentrations of peptide in a small volume and for delivery of a pharmaceutically active peptide for prolonged periods, e.g., one month, after administration of the complex. The complexes can be milled or crushed to a fine powder. In powdered form, the complexes form stable aqueous suspensions and dispersions, suitable for injection. In a preferred embodiment, the peptide of the complex is an LHRH analogue, preferably an LHRH antagonist, and the carrier macromolecule is an anionic polymer, preferably carboxymethylcellulose. Methods of making the complexes, and methods of using LHRH-analogue-containing complexes to treat conditions treatable with an LHRH analogue, are also described.