DIKETOPIPERAZINE MICROPARTICLES WITH PARTICULAR SPECIFIC SURFACE AREAS Russian patent published in 2014 - IPC A61K9/14 A61K9/72 A61K38/28 A61P5/00 

FIELD: medicine.

SUBSTANCE: present invention refers to fumaryldiketopiperazine (FDKP) microparticles applicable for pulmonary delivery and having a specific surface area within the range of 15 m²/g to 67 m²/g and a diameter within the range of 0.5 mcm to 10 mcm. The invention also refers to a dry powder comprising said microparticles that is also applicable for pulmonary delivery, to an inhalation system comprising a powder inhalation apparatus and the above dry powder, as well as to a method for delivering an active agent being an ingredient of the dry powder by inhalation of the above dry powder. There are also disclosed methods for forming the FDKP microparticles, first of which comprises dissolving FDKP in aqueous ammonia, adding an acidic solution to aqueous ammonia at temperature up to 12°C to 26°C and collecting a precipitate containing the FDKP microparticles after rinsing with deionised water. A second method for forming the FDKP microparticles involves supplying equal portions of 10.5 wt % of an acetic acid solution and 2.5 wt % of a FDKP solution at temperature 14-18°C through a high-shear mixer.

EFFECT: invention aims at preparing the FDKP microparticles applicable for pulmonary delivery that have the good aerodynamic performance and provide the enhanced drug absorption.

18 cl, 4 tbl, 9 dwg, 2 ex