The penetration of fluconazole into female genital tissue was examined
in this study in which fluconazole was administered intravenously for
60 minutes at a dose of 200mg to patients undergoing total abdominal
hysterectomy, at 1 to 51 hours prior to surgery. During surgery, the b
lood, uterus, ovary and oviduct were sampled, and the fluconazole conc
entrations in each tissue were determined by high-performance liquid c
hromatography. The peak serum concentrations reached approximately 6.1
mg/L 1 hour after beginning the drip infusion. At each time after the
infusion, the concentrations in the portio vaginalis, cervix uteri, m
yometrium, endometrium, ovary and oviduct were higher than those in th
e serum: the peak concentrations in tissue ranged from 6.4 to 9.5 mu g
/g about 1 hour after beginning the drip infusion. Thus, the penetrati
on of fluconazole into gynaecological tissue appeared to be similar to
or slightly higher than those in serum samples. Fluconazole can rapid
ly penetrate from plasma into the female genital organs, supporting th
e high efficacy of fluconazole against gynaecological fungal infection
s.