[Distribution of hydroxycamptothecin after aerosol inhalation in rabbits].
OBJECTIVE
To investigate the tissue distribution and pharmacokinetics of hydroxycamptothecin (HCPT) after aerosol inhalation in rabbits.


METHODS
RP-HPLC was used to determine the concentration of HCPT in different tissues and plasma of rabbits. The tissue distribution of HCPT after aerosol inhalation or iv administration was compared. The plasma concentrations at different time after aerosol inhalation were compared with iv injection.


RESULTS
The HCPT concentrations in lung after aerosol inhalation at 0.5, 1 and 2 h were 13.52, 27.81 and 20.82 times higher than that of iv administration group, respectively. At the same time, concentrations in other tissues were decreased obviously. The absolute bioavailability of HCPT after aerosol inhalation was 7.38%.


CONCLUSIONS
After aerosol inhalation, HCPT is retained mostly in lung. So this administration route can raise the therapeutic index and reduce adverse effects.
Chen
Jun
J
Department of Clinical Pharmacy, the Affiliated Drum Tower Hospital of Medical School, Nanjing University, Nanjing 210008, China.
Fang
Yun
Y
Zhang
Hai-xia
HX
Huang
Li-li
LL
Qian
Xiao-ping
XP
Liu
Bao-rui
BR
D000280:Administration, Inhalation; D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D001682:Biological Availability; D002166:Camptothecin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000097:blood / Q000493:pharmacokinetics*; D005260:Female; D007275:Injections, Intravenous; D008168:Lung / Q000378:metabolism; D008297:Male; D011817:Rabbits; D014018:Tissue Distribution
D000972:Antineoplastic Agents, Phytogenic; C028098:10-hydroxycamptothecin; D002166:Camptothecin