The oral bioavailability of genistein(GE) in its benzensulfonate prodrug was studied in search for its novel prodrug.The plasmas were collected at different points of time after the intragastric or intravenous administration of genistein benzensulfonate(GBS) 40mg /kg to rats.The GBS and GE contents in plasma were determined by HPLC.The compartment model was fitted and pharma cokinetic parameters were calculated by DAS 2.1.1.The results indicated that the dynamic processes of GE were consistent with two compartment model after intragastric administration of GBS prodrug to rats.The relative oral bioavailability of GE in prodrug GBS was 198.6%.In conclusion,the above results demonstrated that the oral bioavailability of GE in prodrug had been improved remarkably.