Tissue Distribution after Intravenous Dosing of Micafungin, an Antifungal Drug, to Rats

• Published in: Biological & Pharmaceutical Bulletin Vol. 27; no. 7; pp. 1154 - 1156
• Main Authors: Niwa, Toshiro, Yokota, Yoshiko, Tokunaga, Akira, Yamato, Yasuhiro, Kagayama, Akira, Fujiwara, Tomoichi, Hatakeyama, Junko, Anezaki, Masaharu, Ohtsuka, Yuko, Takagi, Akira
• Format: Journal Article
• Language: English
• Published: Japan The Pharmaceutical Society of Japan 01.07.2004; Pharmaceutical Society of Japan; Japan Science and Technology Agency
• Subjects: Animals; Antifungal Agents - administration & dosage; Antifungal Agents - metabolism; antifungal drug; Echinocandins; Injections, Intravenous; Lipopeptides; Lipoproteins - administration & dosage; Lipoproteins - metabolism; Male; Micafungin; Peptides, Cyclic - administration & dosage; Peptides, Cyclic - metabolism; pharmacokinetics; rat; Rats; Rats, Sprague-Dawley; tissue distribution; Tissue Distribution - drug effects; Tissue Distribution - physiology
• ISSN: 0918-6158; 1347-5215
• DOI: 10.1248/bpb.27.1154

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 AUC0—∞ 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.