In order to enhance the dissolution of Ginkgo biloba extract (GBE), a process for the micronization of GBE by supercritical antisolvent (SAS) was developed. Four factors, namely precipitation temperature, precipitation pressure, GBE solution flow rate and solution concentration were optimized in a four-level orthogonal array design. The optimum micronization conditions were determined to be as follows: a precipitation temperature of 65 C, a precipitation pressure of 30 MPa, a GBE solution flow rate of 6.0 ml/min and a GBE solution concentration of 2.5 g/L. Under these optimum conditions, micronized GBE with a mean particle size (MPS) of 81.2 nm was obtained. The morphology of the micronized GBE was observed with scanning electron microscopy and it was determined that spherical particles were obtained. In addition, terpene lactones and flavonoids in GBE were analyzed by liquid chromatography tandem mass spectrometry and high performance liquid chromatography, respectively. The results showed that the contents of terpene lactones and flavonoids in unprocessed and processed GBE were not significantly different (P<0.05). Finally, the dissolution rates of processed and unprocessed GBE were investigated and the results proved that there is a significant increase in dissolution rate for processed GBE using the SAS process compared to unprocessed GBE. (C) 2011 Elsevier B.V. All rights reserved.