The invention discloses a triacetylandrographolide
nanocrystal and its preparation and application. The triacetylandrographolide
nanocrystal is mainly composed of triacetylandrographolide, a stabilizer and an
excipient. The average particle size of the
drug particles in the triacetylandrographolide
nanocrystal suspension obtained by redissolving in water is less than 500 nm, and the PDI is less than 0.2. The triacetylandrographolide and the stabilizer are prepared into a nanocrystal suspension by a high-speed shear antisolvent method combined with a high-pressure homogenization method, and then the
excipient is added and spray-dried. The triacetylandrographolide nanocrystal can significantly improve
drug absorption and improve its
bioavailability. It can be further processed into
solid preparations, liquid preparations and semisolid preparations. It can be used for the treatment of
lung injury-related diseases through
oral administration,
pulmonary inhalation, injection or local administration, especially in the treatment of chronic obstructive
pulmonary disease, it can significantly improve
lung ventilation function, inhibit
pathological changes in alveoli and
airway walls, downregulate the level of
lung tissue
protease, significantly reduce the number of lung inflammatory cells and the
secretion of
inflammatory factors, and inhibit the infiltration of inflammatory cells in
lung tissue.