Method of preparing soy isoflavone nanoparticles by precipitation with compressed antisolvent (PCA) using a supercritical fluid

摘要

The present invention relates to a method of preparing a solid form of soy isoflavone (e.g. genistein). In particular, the present invention relates to a method of preparing a solid form of soy isoflavone by precipitation with compressed antisolvent using a supercritical fluid to produce nano-sized particles of soy isoflavone with an improved dissolution rate and bioavailability. An oral composition or aerosolized formulation comprising the nanoparticles of the soy isoflavone prepared by the method of the present invention is also disclosed herein. The dissolution rate and bioavailability of the nanoparticles of the soy isoflavone prepared by the method of the present invention have a 2-fold increase and a 2.6-fold increase respectively as compared to those of the raw soy isoflavone.

主权项

1. A method of preparing elongated soy isoflavone nanoparticles having a length/width ratio of 8.3 to 10.8 for improving in vivo bioavailability based on precipitation with compressed antisolvent, the method comprising:
providing a supercritical fluid as the compressed antisolvent to a precipitation chamber where said precipitation of the elongated soy isoflavone nanoparticles takes place, wherein said supercritical fluid is supercritical or near supercritical CO2; dissolving raw soy isoflavone in to an organic solvent to form a solution of soy isoflavone at a concentration of 0.4 mg/mL to 4 mg/mL, wherein said organic solvent is acetone; presetting said precipitation chamber to reach conditions comprising a temperature ranging of 31° C. to 60° C., and a pressure ranging of 85 to 120 bar; introducing said solution of soy isoflavone into the precipitation chamber through a co-axial nozzle after the conditions are reached in said precipitation chamber; mixing said supercritical fluid and said solution of soy isoflavone in said precipitation chamber to precipitate said elongated soy isoflavone nanoparticles with size reduction from the dissolved raw soy isoflavone in the organic solvent under the conditions in said precipitation chamber, wherein a feed rate ratio of said supercritical fluid to said solution of soy isoflavone ranges from 30 to 90 g/mL; providing excess supercritical fluid into the precipitation chamber to remove remaining organic residue from said elongated soy isoflavone nanoparticles; and collecting said elongated soy isoflavone nanoparticles from a metal filter at the bottom of said precipitation chamber after gradual depressurization to atmospheric pressure in said precipitation chamber.