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The pharmacokinetic properties and tolerability of three different strengths of prulifloxacin (CAS 123447-62-1), a new antibacterial agent prodrug of AF3013 (CAS 112984-60-8), have been investigated in a randomized, cross-over study performed in 12 Caucasian male subjects (age range 19-34 years). Prulifloxacin was administered as a single oral dose at the dosages of 300, 450 and 600 mg. Plasma concentrations of the active metabolite AF3013 were determined in blood samples collected before the administration (pre-dose) and at 15, 30, 45 min, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36 and 48 h after dosing. Urine samples were also collected. Determination in biological samples was performed using validated and specific HPLC methods. The following parameters were calculated: Cmax, tmax, AUC0-t, AUC0--infinity, t1/2, V/F, Aeut, CLren and fe. The analysis of variance performed on dose-normalized data after logarithmic transformation evidenced no statistically significant differences between the three doses concerning Cmax and AUC. Friedman's test applied to tmax and t1/2 did not show any statistically significant difference between doses. A significant linear relationship between doses and AUC0-infinity was detected (p < 0.05). Very high urinary concentrations and the relatively long terminal half-life (10-12 h) suggest that a once-daily application would show adequate clinical efficacy, especially in urinary infections. The safety profile of the three doses was very good.

The results obtained in a controlled clinical trial aimed at evaluating the efficacy and tolerability of a mucolytic treatment in laryngectomized patients are described. Domiodol (Mucolitico Maggioni, CAS 61869-07-6), an organic iodinated mucolytic agent, was given at the dosage of 60 mg t.i.d. to 20 patients in the post-operative period after laryngectomy (average 2 weeks in hospital and 4 months follow-up at home). A matched series of patients received a placebo during the hospital period and no treatment after discharge. The patients receiving the active treatment showed a statistically and clinically significant improvement of respiratory parameters (cough intensity, sputum quantity, sputum quality, expectoration difficulty). Such improvement was earlier and greater than that observed in the placebo-treated patients. It is concluded that a mucolytic treatment may be helpful in the post-operative treatment of laryngectomized patients with permanent tracheostomy.