abstract |
PURPOSE: To prepare a medicinal composition, comprising primaquine (derivative) as an active ingredient in a biodegradable polymer and capable of controlling the release of the active ingredient and prolonging the duration of actions. CONSTITUTION: This fine particle comprises an active ingredient, selected from among primaquine(PQ), a derivative represented by the formula PQ-X (X is an amino acid or a peptide having 2-4 amino acids; PQ-X bond is a peptide bond between free amino groups in the PQ to carboxyl groups of X) or a conjugate of the PQ or PQ-X with a hepatotropic vector and distributed in a matrix of a polylactide polymer, preferably the -form (having 10,000-200,000, preferably 50,000-100,000 molecular weight). The weight ratio of the active ingredient/ polymer is 1-50%, preferably 15-25%. The particle size is 1-250μm, preferably 100-200μm and prescribed for a solution for parenteral injection. |