Penetration of fluconazole into female genital tissues was examined. Flucon
azole was administered orally at a dose of 150 mg to patients undergoing to
tal abdominal hysterectomy 1 to 151 h prior to surgery, During surgery, blo
od, uterus, ovary, and oviduct were sampled, Fluconazole concentrations in
each tissue Here determined by high-performance liquid chromatography. The
peak concentrations in serum reached approximately 6.1 mu g/ml 1.0 h after
a drip infusion was begun. At each time after the infusion, the concentrati
ons in portio vaginalis, cervix uteri, myometrium, endometrium, ovary, and
oviduct were higher than those in the serum: the peaks in the tissues range
d from 6.4 to 9.5 mu g/g around 1.0 h after the drip infusion was begun, Th
us, the levels of penentration of fluconazole into gynecological tissues ap
peared to be similar to or slightly above those in serum samples. Flucanazo
le can rapidly penetrate from plasma into the female genital organs, suppor
ting high efficacy of fluconazole against fungal infections in the field of
gynecology.