PARTICULATE PHARMACEUTICAL COMPOSITION

摘要

The present invention provides a particulate pharmaceutical composition which has improved drug encapsulation stability and is suitable for a drug delivery system. The particulate pharmaceutical composition 1 contains: a plurality of block copolymer unit 2 arranged radially, each of which has a hydrophobic polymer-chain segment 2b, which is arranged radially inside, and a hydrophilic polymer-chain segment 2a, which is arranged radially outside; a drug 4, which includes a biomacromolecule; and a charged lipid 3, which has an electrical charge opposite to that of the drug 4; wherein the charged lipid 3 is being attracted to the hydrophobic polymer-chain segment 2b, and the drug 3 is positioned radially inside the hydrophobic polymer-chain segment 2b. The pharmaceutical composition 1 can effectively prevent the drug 4 from disengaging from the particle.

主权项

1. A method for producing a particulate pharmaceutical composition, comprising:
dissolving or dispersing a block copolymer unit and a charged lipid into a solvent to form a solution, the block copolymer unit having a hydrophobic polymer-chain segment derived from a polyamino acid chain and a water-soluble hydrophilic polymer-chain segment made of polyethylene glycol; adding a drug to the solution, the drug comprising a biomacromolecule selected from a protein or a nucleic acid; removing the solvent from the solution to form a solid or paste; combining the solid or paste with an aqueous solution to form a dispersion; processing the dispersion by ultrasonic radiation, high pressure emulsification, or extrusion to form a carrier composition; and freezing the carrier composition to form the particulate pharmaceutical composition.