Abstract
A newly developed fluoroquinolone antimicrobial, pazufloxacin (PZFX), was administered to patients with respiratory tract infection, and its penetration into the serum, sputum and saliva over time, and its clinical effectiveness were evaluated. PZFX was administrated orally to a total of 13 patients, 7 with chronic bronchitis, 3 with bronchiectasis, 2 with secondary infection to bronchial asthma and 1 with acute pneumonia, at a dose of 100 mg or 200mg, 3 times daily, for 7-23 days.
The penetration of PZFX into the sputum and saliva was measured in the 2 patients with bronchiectasis. A dose of 200 mg was administrated 3 times daily for 7 days, and the serum, sputum and salivary concentrations were measured on days 1, 4 and 7.
The range of peak concentrations of PZFX in the serum was 3.19, 4.84 μg/ml respectively and in the sputum was 0.98, 2.20 μg/g respectively, reflecting the clinical response well. The penetration of PZFX from serum to saliva was about 30%. Because this rate is highly correlated with the serum concentrations, its pharmacokinetics can be calculated by saliva.
The clinical efficacy of PZFX was classified good in 12 patients and fair in 1, and the efficacy rate was 92.3%. Bacteriologically, 1 strain each of Serratia marcescens, Haemophilus influenzae, Staphylococcus aureus and Streptococcus pneumoniae, a total of 4 isolates, were eradicated. No side effects or abnormal laboratory findings were observed.