[Pharmacokinetics of paclitaxel in experimental animals. Part 1. Blood level].
The plasma disposition of paclitaxel in rabbits (7 mg/kg, 1 h i.v. inf.) was biphasic with half-lives of 0.36 and 6.36 h, and AUC was 9.46 micrograms.hr/ml. K12 value was larger than K21 and V2 was larger than V1, suggesting that paclitaxel had a favorable distribution profile in tissues. In S 180 bearing male ICR mice (30 mg/kg, i.v. bolus), the biphasic plasma disposition was also observed. The half-lives and AUC were 0.25 h, 2.23 h and 117.93 micrograms.hr/ml. Paclitaxel distributed widely in plasma rather than blood cells. The biliary level of paclitaxel in the enlarged gallbladder of ICR mice was markedly high, about 10-fold higher than the urinary level and 100-fold higher than the plasma level. The bioavailability with oral administration to ICR mice was poor. AUC(oral)/AUC(i.v.) ratio in the bile, liver, tumor and plasma was 18.91, 6.71, 0.83 and 0.45%, respectively.
Fujita
H
H
Dept. of Bacteriology, School of Dental Medicine, Tsurumi University.
Okamoto
M
M
Takao
A
A
Mase
H
H
Kojima
H
H
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D005260:Female; D007262:Infusions, Intravenous; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D017239:Paclitaxel / Q000008:administration & dosage / Q000097:blood* / Q000493:pharmacokinetics; D011817:Rabbits; D012510:Sarcoma 180 / Q000188:drug therapy / Q000378:metabolism*
D017239:Paclitaxel