STABLE COMPLEX OF POORLY SOLUBLE THERAPEUTICALLY ACTIVE COMPOUND AND METHOD FOR PREPARING PHARMACEUTICAL PREPARATION

摘要

PURPOSE: A stable complex of poorly soluble compound dispersed in water-insoluble ionic polymer, which considerably increases utilization coefficient of the poorly soluble therapeutically active compound in a living body, and methods for preparing pharmaceutical preparations, are provided. CONSTITUTION: A pharmaceutical composition comprises: (i) a medicine-active stable amorphous compound; (ii) a water-insoluble complex of water-insoluble ionic polymer having molecular weight of more than about 80,000 D and glass transition temperature of more than about 50°C; and (iii) a carrier. A method for preparing pharmaceutical preparation containing the stable amorphous therapeutically active compound and the water-insoluble complex of the ionic polymer comprises steps of: (i) dissolving the therapeutically active compound and the ionic polymer in a suitable solvent; (ii) slightly precipitating complex of compound/polymer of the therapeutically active compound and the ionic polymer by contacting poorly soluble aqueous solution of the ionic polymer with the solution of step (i); and (iii) preparing a pharmaceutical preparation containing the complex of compound/polymer.