Abstract
A clinical study of a new oral quinolone synthetic antimicrobial drug, pazufloxacin (PZFX), was conducted in 8 patients with respiratory infectious diseases, and a basic study was performed to examine the change in its serum level in 11 patients.
1. Clinical study PZFX was administered to 8 patients with respiratory infectious diseases (5 with pneumonia, 3 with chronic respiratory tract infection) at 600 mg a day (3 divided doses) for 7-15 days, to a total dosage of 4.2-8.6g.
Clinical effects were excellent in 3, good in 4 and fair in 1. Pseudomonas aeruginosa and Serratia marcescens were isolated from 1 patient and both were eradicated. No side effects or abnormal laboratory findings were observed in the patients.
2. Pharmacokinetic study
The time-course change of PZFX (200 mg) in serum was determined in a single-dose study by HPLC in a patient of 49 years old and 10 aged patients with chronic respiratory diseases (5 with pulmonary tuberculosis, 2 with bronchial asthma, 1 each with chronic bronchitis, bronchiectasis, pulmonary emphysema and atypical mycobacteriosis), and the pharmacokinetics were studied. The average serum level after administration in a patient of 49 years old was 2.00μg/ml at 1 hour, 2.59μg/ml at 2 hours, 1.19μg/ml at 4 hours and 0.46μg/ml at 6 hours and in the 10 patients the mean average was 0.966±0.657μg/ml at 1 hour, 2.263±1.064μg/ml at 2 hours, 2.782±1.041μg/ml at 4 hours and 1.489±0.534μ/ml at 6 hours, and the peak level was observed at 3.2 hours. Cmax was 3.122±1.002μg/ml, T1/2 2.740±0.841 hr and AUC0-∞16.75±4.32μg·hr/ml. These results show that the serum concentration of PZFX exceeds MICs of many causative organisms in respiratory infections, suggesting its clinical usefulness, and were almost consistent with the data of healthy adults obtained in the phase I clinical study, excluding AUC, Tmax; i.e., of 2 patients who showed mild renal dysfunction, 1 demonstrated elevation of AUC, and the other showed prolongation of T1/2 and elevation of AUC.
