Pharmacokinetics of C-1027 in mice as determined by TCA-RA method.
OBJECTIVE
To validate a radioactivity assay, the TCA-RA method, for the measurement of C-1027 in serum and to evaluate its application in determination of pharmacokinetics of C-1027 in mice.


METHODS
(125)I-C-1027 was prepared by the Iodogen method and separated by HPLC. The radioactivity assay was established and used to determine (125)I-C-1027 in mice at doses of 10, 50 and 100 microg/kg after precipitation with 20% trichloroacetic acid (TCA-RA method). Several pharmacokinetic parameters were determined after intravenous injection of (125)I-C-1027 to mice.


RESULTS
After intravenous injection of (125)I-C-1027 to mice, at doses of 10, 50 and 100 microg/kg; the apparent distribution volumes (V(d)) were 0.26, 0.31 and 0.33 L/kg; the biological half-lives (T(1/2)) were 3.10, 3.40 and 3.90 h; the areas under curve (AUC) were 18.41, 103.69 and 202.74 ng/h/mL; the elimination rate constants (K) were 1.04, 1.26 and 0.58/h; and the total body clearance (Cl) were 0.54, 0.48 and 0.49 L/kg/h, respectively.


CONCLUSIONS
TCA-RA is a sensitive, reliable and suitable method for the determination of (125)I-C-1027 in mouse serum.
Liu
You-Ping
YP
Tianjin Institute of Pharmaceutical Research, 308 An-Shan West Road, Tianjin 300193, China.
Li
Quan-Sheng
QS
Huang
Yu-Rong
YR
Zhou
Mao-Jin
MJ
Liu
Chang-Xiao
CX
D000617:Aminoglycosides / Q000493:pharmacokinetics*; D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000493:pharmacokinetics*; D011232:Chemical Precipitation; D053281:Enediynes; D005260:Female; D007275:Injections, Intravenous; D007457:Iodine Radioisotopes / Q000493:pharmacokinetics; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D011863:Radioimmunoassay / Q000379:methods* / Q000592:standards; D015203:Reproducibility of Results; D014238:Trichloroacetic Acid
D000617:Aminoglycosides; D000903:Antibiotics, Antineoplastic; D053281:Enediynes; D007457:Iodine Radioisotopes; C058024:C 1027; D014238:Trichloroacetic Acid