The invention discloses an
asenapine slow-release
microsphere agent and a preparation method thereof. The
microsphere agent is prepared from
asenapine or salts and polyesters thereof, wherein the weight percentage of the
asenapine or salts thereof counted by asenapine is 5-50%, and the weight percentage of the polyesters is 50-95%. The preparation method comprises the following steps: (1) conducting weighing; (2) adding the
polyester material into an
organic solvent for completely dissolving the
polyester material to obtain a settled solution, then dissolving or suspending the
medicine asenapine or the salts thereof into the settled solution to be used as an
oil phase; stirring or shearing the
oil phase at high speed to form a homogeneous
oil phase; and in case of need, adding a right amount of acid for salifying the asenapine; and (3) preparing the
microsphere agent by a microdroplet generating device, or a
spray drying method, or an atomizing extraction method. The microsphere agent provided by the invention has relatively high production efficiency, the D50 particle sizes of the prepared microspheres are all below 80mu m, are controllable and are concentrated in distribution, the
drug-
loading rate is as high as 45%, and the encapsulation rate is above 85%.