Pharmacokinetics of butoconazole nitrate suppositories in human

The aim of the study was to investigate the pharmacokinetics of butoconazole nitrate suppositories in healthy Chinese female volunteers after single and multiple-dose vaginal administration. 12 healthy Chinese female volunteers received single 0. 05 g, single 0. 1 g, multiple doses(0. 1 g per day, 3-day consecutive administration)and multiple doses(0. 1 g per day, 5-day consecutive administration)of butoconazole nitrate suppositories. For 0. 05 g and 0. 1 g single vaginal administration of butoconazole nitrate suppositories, the c_max were(0. 895 0±0. 261 0)and(1. 740±0. 511)ng/mL and the AUC_{0-96 h} were(36. 38±10. 82)and(73. 48±28. 99)ng ·h/mL, respectively. In the range of 0. 05-0. 1 g, butoconazole demonstrated linear pharmacokinetics. In the multiple-dose study at 0. 1 g dose for 3 consecutive days, the degree of fluctuation(DF)was(0. 54±0. 27), and the accumulation parameters Rc_max and R_AUC0-τ were(1. 3±0. 3)and(1. 4±0. 3), respectively. In the multiple-dose study at 0. 1 g dose for 5 consecutive days, the DF was(0. 64±0. 25), and the accumulation parameter Rc_max and R_AUC were(1. 4±0. 3))and(1. 6±0. 2), respectively. An accumulation of 60% in AUC_0-τ occurred after a multiple administration. The main pharmacokinetic parameters between 3-day consecutive administration and 5-day consecutive administration showed no significant difference.