OBJECTIVE To study the pharmacokinetic parameters of genistein in female and male rats. METHODS Genistein was orally administered to rats. The genistein and glucuronidated genistein in plasma and in different tissues were detected by a high performance liquid chromatography assay. RESULTS The concentration of genistein in ovaries or uterus was significantly higher than that in testis, and there was no remarkable gender-based differences in the genistein concentration in other tissues. AUCs were 1.120 mg·h·L~(-1) in female and 0.592 mg·h·L~(-1) in male, and ρ_(max) S were 0.167 mg·L~(-1) in female and 0.106 mg·L~(-1) in male. The t_(1/2) were 5.767 h in female and 4.486 h in male. The concentration of glucuronidated genistein in female rats is much higher than that in male rats. CONCLUSION The distribution of genistein in the sexual organ of female and male rats is significantly different. Compared with male rats, the absorption and glucuronidation of genistein are much more in female rats, and this resultes in the half-life prolongation of genistein.