Objective To explore the targeted distribution of flurbiprofen axetil (FA) in hysteromyoma and its influence on prostaglandin E₂ (PGE₂). Methods A total of 40 female patients undergoing myomectomy (ASAⅠ-Ⅱ) were enrolled in the present study. The patients were randomly divided into blank control group and FA groups of three different doses. The four groups were injected with normal saline, 0.5, 1, or 1.5 mg/kg of FA 15 min before the operation. Tumor tissues and normal tissues were collected by surgical operation and the sampling time was recorded. The concentration of flurbiprofen (FP), which was the active metabolite of FA, was detected in the tumor tissues and normal tissues by HPLC. The concentrations of PGE₂ were detected by ELISA in the two samples. Results FP was not detected in the tumor tissues or normal tissues of the blank group. With the increase of FA dose in the three groups, the concentration of FP had an increasing tendency in the tumor tissues, with significant differences found among the three groups (P <0.05), but not in the normal tissues (P >0.05).The concentrations of FP in the tumor tissues were significantly higher than those in the normal tissue in the three FA groups (P <0.01).With the increase of FA dose, the concentration of PGE₂ had a tendency to decrease in the tumor tissues; and there were significant differences between blank group and 1, 1.5 mg/kg FA groups (P <0.01), not between blank group and 0.5 mg/kg FA group. The concentrations of PGE₂ in the tumor tissues were significantly higher than those in the normal tissues in the four groups (P <0.01), and there were no significant differences in pairwise comparisons in the normal tissues among the four groups (P >0.05). Conclusion FA has a certain targeted distribution in hysteromyoma and can reduce the level of PGE₂.