The invention discloses waterless reverse micelles nanoparticles of a water-soluble
drug, and a preparation method of a suspension
aerosol thereof. The preparation method comprises the following steps: dissolving the water-soluble
drug and a freeze-
drying protectant into water as an aqueous phase; dissolving amphiphilic substances into tert-butyl
alcohol as an
oil phase, stirring uniformly in a water bath at a constant temperature, adding dropwise the
oil phase into the aqueous, getting a nano suspension with a
bilayer vesicles structure; freezing the nano suspension rapidly and solidifying, getting a freeze-
drying product; adding an organic phase into the freeze-
drying product, and getting the waterless reverse micelles nanoparticles; filling a
spray bottle with the nanoparticles and
nitrogen, sealing, pressing a propellent into the
spray bottle, and getting the suspension
aerosol. The preparation method of the invention helps to prepared the nanoparticles with a
lipid vesicle structure in uniform particle size by one step, and the
drug molecules are not easy to damage; and by taking tert-butyl
alcohol / water as a
solvent,
energy consumption in the freeze-drying process is reduced,
solvent sublimation is accelerated, and freeze-
drying time is shortened. The
nanoparticle suspension
aerosol is high in
sedimentation rate
in vitro of pulmonary delivery, and helps to improve drug absorption.