title: Tissue distribution after intravenous dosing of micafungin, an antifungal drug, to rats.
abstract: 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.
authors.affiliation: Post-marketing Development Research Center, Fujisawa Pharmaceutical Co., Ltd., Osaka, Japan. toshiro_niwa@po.fujisawa.co.jp
authors.forename: Toshiro
authors.initials: T
authors.lastname: Niwa
authors.forename: Yoshiko
authors.initials: Y
authors.lastname: Yokota
authors.forename: Akira
authors.initials: A
authors.lastname: Tokunaga
authors.forename: Yasuhiro
authors.initials: Y
authors.lastname: Yamato
authors.forename: Akira
authors.initials: A
authors.lastname: Kagayama
authors.forename: Tomoichi
authors.initials: T
authors.lastname: Fujiwara
authors.forename: Junko
authors.initials: J
authors.lastname: Hatakeyama
authors.forename: Masaharu
authors.initials: M
authors.lastname: Anezaki
authors.forename: Yuko
authors.initials: Y
authors.lastname: Ohtsuka
authors.forename: Akira
authors.initials: A
authors.lastname: Takagi
mesh_terms: 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
chemical_list: D000935:Antifungal Agents; D054714:Echinocandins; D055666:Lipopeptides; D008074:Lipoproteins; D010456:Peptides, Cyclic; D000077551:Micafungin