[Penetration into bone and joint tissues of rabbits and in vitro antibacterial activity of tosufloxacin].
The penetration of tosufloxacin (TFLX) into the bone and joint tissues of rabbits and its in vitro antibacterial activity were compared with those of lomefloxacin (LFLX) which is a efficacious drug for orthopedic infections. Serum levels of TFLX at 1, 2, 4 and 6 hours after oral administration (100 mg/kg) were 0.41, 0.65, 0.62 and 0.42 micrograms/ml, respectively. Except in synovial fluid and femur, TFLX concentrations in bone and joint tissues were higher than those in serum (0.69 approximately 1.92 micrograms/g in bone marrow of sternum, 0.55 approximately 1.53 micrograms/g in bone marrow of femur). TFLX concentrations in synovial fluid at 4 and 6 hours after the administration were equal to those in serum, which were lower than those of LFLX, but the ratio of tissue level/serum level of TFLX was similar to that of LFLX. TFLX was 8- to 64-fold more active than LFLX against Staphylococcus aureus (including methicillin-resistant S. aureus), Streptococcus pyogenes, Haemophilus influenzae, which are major pathogens of purulent osteomyelitis and arthritis. TFLX inhibited the growth of these bacteria at less than 0.39 micrograms/ml. These results indicate that TFLX is a useful drug for orthopedic infection.
Research Laboratory, Toyama Chemical Co., Ltd.
Y
Y
Yamashiro
M
M
Nunome
M
M
Takahata
T
T
Yasuda
D000284:Administration, Oral; D000818:Animals; D000890:Anti-Infective Agents / Q000493:pharmacokinetics / Q000494:pharmacology*; D001842:Bone and Bones / Q000187:drug effects* / Q000378:metabolism; D024841:Fluoroquinolones; D006193:Haemophilus influenzae / Q000187:drug effects*; D007596:Joints / Q000187:drug effects* / Q000378:metabolism; D008297:Male; D008826:Microbial Sensitivity Tests; D009287:Naphthyridines / Q000493:pharmacokinetics / Q000494:pharmacology*; D015363:Quinolones / Q000493:pharmacokinetics / Q000494:pharmacology; D011817:Rabbits; D013211:Staphylococcus aureus / Q000187:drug effects*; D013297:Streptococcus pyogenes / Q000187:drug effects*
D000890:Anti-Infective Agents; D024841:Fluoroquinolones; D009287:Naphthyridines; D015363:Quinolones; C055185:tosufloxacin; C053091:lomefloxacin