Pharmacokinetics of temafloxacin in mice, rats and hamsters

• Published in: CHEMOTHERAPY Vol. 41; no. Supplement5; pp. 128 - 139
• Main Authors: Takeda, Katsuo, Yano, Shigeru, Sakuma, Yoshimitsu, Koyama, Yaeko, Yamaguchi, Totaro
• Format: Journal Article
• Language: English; Japanese
• Published: Japanese Society of Chemotherapy 1993
• Subjects: temafloxacin
• ISSN: 0009-3165; 1884-5894
• DOI: 10.11250/chemotherapy1953.41.Supplement5_128

The pharmacokinetics of temafloxacin (TMFX) were studied and compared with those of ofloxacin (OFLX), ciprofloxacin (CPFX) and erythromycin (EM) in mice, rats and hamsters. 1. In rats orally dosed with 20 mg/kg, there were no significant differences between males and females in the plasma AUC or in urinary recoveries. 2. In rats, the plasma AUCs were linearly related to oral dose in the range of 10-100 mg/kg. 3. In rats, the oral bioavailability of TMFX was 60% from the p.o./i.v. AUC ratio and 76% from the p.o./i.v. urinary recovery ratio. 4. In mice and rats orally dosed with 20 mg/kg, the peak serum levels were in the order of OFLX, TMFX and CPFX, whereas the serum AUCs were in the order of TMFX, OFLX and CPFX. The peak lung levels were in the order of TMFX and/or OFLX and CPFX, whereas the lung AUCs were in the order of TMFX, OFLX and CPFX. 5. In hamsters orally dosed with 50 mg/kg, the peak serum levels were in the order of OFLX, TMFX, EM and CPFX and the serum AUCs were in the same order. In contrast, the peak lung levels were in the order of TMFX, OFLX, EM and CPFX, whereas the lung AUCs were in the order of TMFX, OFLX, CPFX and EM. The lung-to-serum concentration ratios of TMFX were 2-fold higher than those of OFLX. 6. In rats intravenously dosed with 10 mg/kg, the cerebrospinal fluid (CSF)-to-serum concentration ratios of TMFX were 1/2 to 1/3 of those of OFLX. 7. In rats orally dosed with 20 mg/kg, the recoveries of TMFX in urine and bile were similar to those of OFLX. 8. Binding rates to the serum proteins of mice, rats, rabbits, dogs, monkeys and humans were 29.5, 34.1, 35.8, 25.6, 29.0 and 26.6%, respectively.