Penetration of ravuconazole, a new triazole antifungal, into rat tissues.
Ravuconazole (BMS 207147, ER-30346) is a long-lasting triazole antifungal agent active against a broad spectrum of fungal pathogens including non-albicans Candida, Aspergillus, Cryptococcus and key dermatophytic fungi. The penetration of ravuconazole into rat tissues was examined. Fifty-five 7-week-old specific pathogen free female rats were used in this study. Plasma, lung and uterus tissue of rats were taken at 1, 2, 4, 8, 12, 16, 24, 32, 48, 60, and 72 h (n = 5) after oral administration of 10 mg/kg of ravuconazole. The quantitative assays of ravuconazole by HPLC after the extraction with diethylether were conducted for each tissue sample homogenate. tmax, t1/2, and Cmax of ravuconazole is 8 h, 16.9 h and 1.68 microg/ml, respectively. The concentrations of ravuconazole in rat uterus and lung tissues were 2-to 6 times higher than the corresponding blood concentrations. The ratio of plasma to lung levels of ravuconazole was superior to the published data of other azoles. Considering its antifungal spectrum, ravuconazole would thus be a good candidate for treatment of deep-seated fungal infections caused by Candida, Aspergillus and Cryptococcus.
Mikamo
Hiroshiege
H
Department of Obstetrics and Gynecology, School of Medicine, Gifu University, Japan. mikamo@cc.gifu-u.ac.jp
Yin
Xiang Hua
XH
Hayasaki
Yoh
Y
Shimamura
Yoshiko
Y
Uesugi
Keizo
K
Fukayama
Nobuyuki
N
Satoh
Masaru
M
Tamaya
Teruhiko
T
D000284:Administration, Oral; D000818:Animals; D000935:Antifungal Agents / Q000493:pharmacokinetics*; D001682:Biological Availability; D005260:Female; D006207:Half-Life; D008168:Lung / Q000378:metabolism*; D051381:Rats; D013047:Specific Pathogen-Free Organisms; D013844:Thiazoles / Q000493:pharmacokinetics*; D014230:Triazoles / Q000493:pharmacokinetics*; D014599:Uterus / Q000378:metabolism*
D000935:Antifungal Agents; D013844:Thiazoles; D014230:Triazoles; C104066:ER 30346