Pharmacokinetics, blood partition, and tissue distribution of itraconazole.
Pharmacokinetics of itraconazole was measured after 1-min intravenous infusion at a dose of 10 mg/kg to male New Zealand white rabbits. The terminal half-life of itraconazole was 524 min. Itraconazole was eliminated slowly in rabbits with total body clearance of 3.26 ml/min/kg. Blood partition of itraconazole between plasma and blood cells of rabbit blood was measured. Itraconazole reached equilibrium rapidly between plasma and blood cells of rabbit blood. The equilibrium plasma/blood cells concentration ratios were independent of initial rabbit blood concentrations of itraconazole, 1, 5, and 10 microg/ml; the mean value was 3.25. Tissue distribution of itraconazole was also measured after 1-min intravenous administration at a dose of 10 mg/kg to rats. The tissue-to-plasma (T/P) ratios of itraconazole were greater-than-unity in all rat tissues studied at both 1 and 24 h except in fat and stomach at 1 h. This indicated that rat tissues studied had a high affinity to itraconazole.
Lee
Joo H
JH
College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, San 56-1, Shinlim-Dong, Kwanak-Gu, Seoul 151-742, South Korea.
Shin
Jee H
JH
Lee
Myung G
MG
D000818:Animals; D000935:Antifungal Agents / Q000008:administration & dosage / Q000097:blood* / Q000737:chemistry / Q000493:pharmacokinetics*; D019540:Area Under Curve; D002851:Chromatography, High Pressure Liquid; D004305:Dose-Response Relationship, Drug; D004355:Drug Stability; D006207:Half-Life; D007262:Infusions, Intravenous; D017964:Itraconazole / Q000008:administration & dosage / Q000097:blood* / Q000737:chemistry / Q000493:pharmacokinetics*; D007700:Kinetics; D008297:Male; D011817:Rabbits; D051381:Rats; D017207:Rats, Sprague-Dawley; D014018:Tissue Distribution
D000935:Antifungal Agents; D017964:Itraconazole