Penetration of Oral Fluconazole into Gynecological Tissues

Penetration of fluconazole into female genital tissues was examined. Fluconazole was administered orally at a dose of 150 mg to patients undergoing total abdominal hysterectomy 1 to 151 h prior to surgery. During surgery, blood, uterus, ovary, and oviduct were sampled. Fluconazole concentrations in each tissue were determined by high-performance liquid chromatography. The peak concentrations in serum reached approximately 6.1 μg/ml 1.0 h after a drip infusion was begun. At each time after the infusion, the concentrations in portio vaginalis, cervix uteri, myometrium, endometrium, ovary, and oviduct were higher than those in the serum: the peaks in the tissues ranged from 6.4 to 9.5 μg/g around 1.0 h after the drip infusion was begun. Thus, the levels of penentration of fluconazole into gynecological tissues appeared to be similar to or slightly above those in serum samples. Fluconazole can rapidly penetrate from plasma into the female genital organs, supporting high efficacy of fluconazole against fungal infections in the field of gynecology.

本研究考察了氟康唑（fluconazole）在女性生殖组织中的渗透特性。对接受全腹子宫切除术的患者，于术前1至151小时口服给予150 mg氟康唑。手术过程中采集血液、子宫、卵巢及输卵管样本。采用高效液相色谱法（high-performance liquid chromatography）测定各组织中的氟康唑浓度。滴注开始后1.0小时，血清中的峰浓度约达6.1 μg/ml。滴注后的各时间点，子宫颈阴道部、子宫颈、子宫肌层、子宫内膜、卵巢及输卵管中的药物浓度均高于血清浓度；各组织的峰浓度范围为6.4至9.5 μg/g，出现在滴注开始后约1.0小时。由此可见，氟康唑在妇科组织中的渗透水平与血清样本中的浓度相近或略高。氟康唑可快速从血浆渗透进入女性生殖器官，为其在妇科领域对抗真菌感染的高效性提供了实验支撑。