HIGHLY POROUS POLY(LACTIC-CO-GLYCOLIC) ACID MICROPARTICLES FOR SUSTAINED TIOTROPIUM RELEASE AND PREPARING METHOD THEREOF

摘要

The present invention relates to porous PLGA micro-particles used for the sustained tiotropium release for treatment of chronic obstructive pulmonary diseases and a preparation method thereof. According to the present invention, the PLGA micro-particle preparation method includes the steps of: a) dissolving the tiotropium, ammonium bicarbonate (AB), and the biodegradable polysaccharide in water to prepare am internal aqueous phase; b) applying a biodegradable polymer in an organic solvent to prepare an organic phase; c) emulsifying the internal aqueous phase obtained in the step a) and the organic phase obtained in the step b) to prepare the water in oil emulsion (W/O); and d) injecting the W/O obtained in the step c) in an external aqueous phase including an aqueous coating material to obtain the water in oil in water (W/O/W) through multi-emulsion. The porous PLGA micro-particles used for the sustained tiotropium release have low density and large particle size mot to be removed by macrophages and remain in the lungs for an extended period of time.