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 particulate pharmaceutical composition comprising:
a plurality of block copolymer units, each unit having a hydrophobic polymer-chain segment and a hydrophilic polymer-chain segment, the hydrophobic polymer-chain segment being a polyamino acid segment, the plurality of block copolymer units being arranged radially with the hydrophobic polymer-chain segments radially inside and the hydrophilic polymer-chain segments radially outside; a plurality of charged lipids carrying a first charge, the plurality of charged lipids being attracted to the hydrophobic polymer-chain segment; and a drug carrying a second charge opposite to the first charge and comprising a biomacromolecule selected from the group consisting of proteins and nucleic acids, wherein the particulate pharmaceutical composition is subjected to freezing, wherein the drug is positioned radially inside relative to the hydrophobic polymer-chain segments as a result of the freezing such that the drug is prevented from disengaging from the particulate pharmaceutical composition, and wherein the particulate pharmaceutical composition has an absolute zeta potential that is higher than that of a particulate pharmaceutical composition that has not been subjected to the freezing.