Distribution of oral nimesulide in female genital tissues

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Abstract
Nimesulide is a non‐steroidal anti‐inflammatory agent which has proved to be effective in reducing menstrual discomfort in dysmenorrhoeaic women. To determine the concentrations of this drug in the uterus (fundus, cervix), oviduct, and ovaries and to correlate these findings with plasma concentrations, a single oral dose of 100mg nimesulide was administered 1 to 6h before surgery to 12 women undergoing hysterectomy and salpingo‐oophorectomy, mainly for fibroids. Tissue samples were taken, concentration of nimesulide measured by HPLC, and findings compared with plasma concentrations. One patient not undergoing treatment served as control. Nimesulide concentration in the tissues studied was highest 3h after administration, as expected from the drug's pharmacokinetic profile. The highest tissue/plasma ratio (0·5) was also found at that time. Average tissue concentrations at 1, 2, 3, and 6h after drug intake ranged from 0·3 to 1·8μgg−1, and plasma concentrations from 2·6 to 4·1μgml−1. Nimesulide was evenly distributed in the tissues studied.