Tissue distribution after intravenous dosing of micafungin, an antifungal drug, to rats.
The tissue distribution after an intravenous dose of micafungin (1 mg/kg), a new echinocandin-like lipopeptide antifungal agent, to male rats was investigated. Micafungin in plasma disappeared biexponentially with a terminal half-life of 5.03 h. Micafungin concentrations in liver, kidney, and lung at the first sampling time (5 min) after dosing were 1.15, 1.64, and 2.58-fold higher than the plasma concentration, and the AUC(0- infinity ) were 1.61, 3.42, and 2.89-fold higher than that for plasma. The terminal half-lives for these tissues were 5.14, 4.87, and 5.31 h, respectively, which were comparable to those for plasma. These results suggest that micafungin distributes rapidly and moderately into tissues such as the liver, kidney, and lungs, and that the concentrations in tissues decreased in parallel with the unchanged drug in plasma.
Niwa
Toshiro
T
Post-marketing Development Research Center, Fujisawa Pharmaceutical Co., Ltd., Osaka, Japan. toshiro_niwa@po.fujisawa.co.jp
Yokota
Yoshiko
Y
Tokunaga
Akira
A
Yamato
Yasuhiro
Y
Kagayama
Akira
A
Fujiwara
Tomoichi
T
Hatakeyama
Junko
J
Anezaki
Masaharu
M
Ohtsuka
Yuko
Y
Takagi
Akira
A
D000818:Animals; D000935:Antifungal Agents / Q000008:administration & dosage* / Q000378:metabolism*; D054714:Echinocandins; D007275:Injections, Intravenous; D055666:Lipopeptides; D008074:Lipoproteins / Q000008:administration & dosage* / Q000378:metabolism*; D008297:Male; D000077551:Micafungin; D010456:Peptides, Cyclic / Q000008:administration & dosage* / Q000378:metabolism*; D051381:Rats; D017207:Rats, Sprague-Dawley; D014018:Tissue Distribution / Q000187:drug effects / Q000502:physiology
D000935:Antifungal Agents; D054714:Echinocandins; D055666:Lipopeptides; D008074:Lipoproteins; D010456:Peptides, Cyclic; D000077551:Micafungin