ABSTRACT
OBJECTIVE: To determine the concentrationsof antofloxacin hydrochloride in the lung tissuesafter single dose preoperative oral administration of 400 mg in patientsreceiving pulmonry lobectomy for, preliminary evaluation of the rationality of this regimen to prevent infection. METHODS: Forty-eight patients with no clinical evidence of preoperative infection undergoing pulmonary lobectomy were selected and randomized into four treatment groups. 400 mg antofloxacin hydrochloride was administered orally at 4, 8, 12, and 24 h before the removal of the bronchi. Blood samples and lung tissues were collected after operation. The antofloxacin hydrochloride in blood serum and lung tissues was determined by high performance liquid chromatogram. RESULTS: The average concentrations of antofloxacin hydrochloride in serum andlung tissuesin the four groupswere (3.281±0.817)μg·mL-1 and (5.992±3.228)μg·g-1, (3.192±0.953)μg·mL-1 and (5.885 ±2.952)μg·g-1, (1.712 ±0.576) μg·mL-1 and (3.419±1.107)μg·g-1, and (0.431±0.095)μg·mL-1 and (1.258±0.306) μg·g-1, respectively. CONCLUSION: The clearance time of oral antofloxacin hydrochloride in lung tissue was longer than that in serum. Single dose administration of oral antofloxacin hydrochloride 400mg within 12 h before operation can achieve effective bactericidal levels in serum and lung tissues, which could be a method to prevent infection for pulmonary lobectomy.
ABSTRACT
Objective To evaluate the clinical efficacy and safety of antofloxacin hydrochloride tablet for the treatment of acute bacterial infections. Methods A multi-center randomized control, double blind and double dummy clinical trial was conducted; levofloxacin tablet was chosed as controlled drug. The duration of treatment was 7-14 days in both groups. Results A total of 719 patients were enrolled in the study, in which 359 patients treated with antofloxacin and 360 patients treated with levofloxacin were included. Three hundred and thirty and 337 patients completed the study and met with all the criteria for perprotocol analysis, respectively. By the end of chemotherapy, the cured rates in per protocol set (PPS)population were 79.7% and 77.4%, the effective rates were 95.2% and 96. 7%, and the bacterial clearance were 96. 7% and 97. 5% for the treating and control group, respectively. The clinical and bacterial efficacy of antofloxacin and levofloxacin was comparable by the analysis of infectious sites. Three hundred and fifty-seven and 356 patients in antofloxacin and levofloxacin groups were evaluated the safety.The drug adverse events occurred both in 10. 1%, and drug adverse reactions accurred in 7. 8% and 7.9%patients in the two groups. The most common drug adverse reactions were mild gastroenteric symptoms. No QTc prologation was detected in all the patients. One patient in each group had mild blood glucose increase at the end of therapy, but the glucose returned to normal level without any intervention. No statistic significant difference between the two groups in clinical efficacy and safety was detected (P＞0.05).Conclusions Antofloxacin hydrochloride tablet was effective and safe for the treatment of acute bacterial infections.