Antipsychotic Injectable Depot Composition

An injectable depot composition, comprising:

• a drug, and/or a metabolite thereof and/or a prodrug thereof;
• at least one biocompatible polymer which is a copolymer comprising lactic acid and glycolic acid monomers, wherein the monomers are present at a monomer ratio of lactic to glycolic acid in the range from about 48:52 to about 77:23, and;
• at least a water-miscible solvent with a dipole moment of about 3.9-4.3 D, wherein
• the solvent and polymer form a polymer solution having a viscosity in the range of 0.5 to 7.0 Pa·s, and the solvent/drug mass ratio ranges from about 12:1 to about 4:1;
• and
• the drug/polymer mass ratio ranges from about 15% to about 40% expressed as the weight percentage of the drug with respect of the drug plus polymer.

A pharmaceutical kit suitable for preparation of an injectable composition that forms a biodegradable non-particulate solid single body implant in situ in a subject in need thereof, the kit comprising:

• a first container comprising at least one biocompatible polymer, which is a copolymer comprising lactic acid and glycolic acid monomers, wherein the monomers are present at a monomer ratio of lactic to glycolic acid in the range from about 48:52 to about 77:23;
• and
• a second container comprising a water-miscible solvent having a dipole moment of about 3.9-4.3 D in which the biocompatible polymer is soluble;
• and
• at least one drug, and/or a metabolite thereof and/or a prodrug thereof, present in the first container, second container or a third container;
• whereby mixing of the at least one drug, and/or a metabolite thereof and/or a prodrug thereof with the contents of the first container and with the contents of the second container affects formation of an injectable composition having a viscosity in the range of about 0.5 to about 7.0 Pa·s, wherein
• the solvent/drug mass ratio ranges from about 12:1 to about 4:1;
• the drug/polymer mass ratio ranges from about 15% to about 40% expressed as the weight percentage of the drug with respect of the drug plus polymer;
• and
• the composition forms a biodegradable non-particulate solid single body implant in situ in a subject in need thereof to which it is administered.

A method for preparing an injectable composition, the method comprising:

• subjecting a biodegradable poly(L-lactide-co-glycolide) polymer, having a monomer ratio of lactic acid to glycolic acid in the range of 48:52 to 77:23 and having a first molecular weight, to a sufficient amount of -radiation to degrade at least a portion of the polymer thereby reducing its molecular weight and intrinsic viscosity;
• and
• mixing the irradiated polymer with a solvent, having a dipole moment of about 3.9-4.3 D, and with at least one drug, or at least one metabolite thereof or at least one prodrug thereof, to form an injectable composition having a viscosity in the range of about 0.5 to about 7.0 Pa·s;
• wherein
• the solvent/drug mass ratio ranges from about 12:1 to about 4:1;
• the drug/polymer mass ratio ranges from about 15% to about 40% expressed as the weight percentage of the drug with respect of the drug plus polymer;
• and
• the composition forms a biodegradable non-particulate solid single body implant in situ in a subject in need thereof to which it is administered.