Tissue distribution and excretion of 125I-lidamycin in mice and rats.
OBJECTIVE
To investigate the tissue distribution, urinary and fecal excretions of (125)I-lidamycin ((125)I-C-1027) in mice and its biliary excretion in rats.


METHODS
The total radioactivity assay (RA method) and the radioactivity assay after precipitation with 200 mL/L trichloroacetic acid (TCA-RA method) were used to determine the tissue distribution, and the urinary and fecal excretions of (125)I-C-1027 in mice and its biliary excretion in rats.


RESULTS
Tissue concentrations reached the peak at the fifth minute after administration of (125)I-C-1027 to mice. The highest concentration was in kidney, and the lowest in brain at all test-time points. The organs of the concentrations of (125)I-C-1027 from high to low were kidney, lung, liver, stomach, spleen, uterus, ovary, intestine, muscle, heart, testis, fat, and brain in mice. The accumulative excretion amounts of 0-24 h, and 0-96 h after administration of (125)I-C-1027 were 68.36 and 71.64% in urine, and 2.60 and 3.21% in feces of mice, respectively, and the accumulative excretion amount of 0-24 h was 3.57% in bile in rats.


CONCLUSIONS
Our results reflect the characteristics of the tissue distribution, urinary and fecal excretions of (125)I-C-1027 in mice and the biliary excretion of (125)I-C-1027 and its metabolites in rats, and indicate that (125)I-C-1027 and its metabolites are mainly distributed in kidney, and excreted in urine.
Liu
You-Ping
YP
National Key Laboratory of Pharmakinetics and Pharmacodynamics, Tianjin Institute of Pharmaceutical Research, 308 An-Shan West Road, Tianjin 300193, China.
Li
Quan-Sheng
QS
Huang
Yu-Rong
YR
Liu
Chang-Xiao
CX
D000617:Aminoglycosides / Q000493:pharmacokinetics* / Q000652:urine; D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000493:pharmacokinetics* / Q000652:urine; D001646:Bile / Q000378:metabolism; D053281:Enediynes; D005243:Feces; D005260:Female; D007457:Iodine Radioisotopes; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D051381:Rats; D017208:Rats, Wistar; D014018:Tissue Distribution
D000617:Aminoglycosides; D000903:Antibiotics, Antineoplastic; D053281:Enediynes; D007457:Iodine Radioisotopes; C058024:C 1027