Distribution, excretion and pharmacokinetic research of dual target ligand-based lidamycin in rats / 中国药理学与毒理学杂志

ABSTRACT

OBJECTIVE: To study the distribution, excretion and other pharmacokinetic characteristics of dual target ligand-based lidamycin (DTLL) in rats. METHODS: [125l] radioactivity isotope tracing method was used to determine the pharmacokinetic parameters of DTLL which was injected intravenously via the tail vein of healthy Wistar rats at a single dose of [125l] DTLL 2625 kBq · 0.05 mg-1· kg-1. The samples from rat plasma, tissue, feces, urine and bile were obtained to analyze the distributions of DTLL in rats after administration and to calculate the cumulative excretion scores by using a liquid scintillation counting analyzer with the WinNolin program. RESULTS: The area under the concentration-time curve (AUC0-∞) of DTLL was (184±33) h·μg·L-1, with half time (t1/2) and cleanrance (Cl) at (3.98±0.75) h and (278±41) mL·h-1· kg-1, respectively. DTLL was mainly distributed in whole body tissues without any accumulation observed. The excretion rate of DTLL was (82.5±2.6)% for urine, compared with (10.4±6.6)% in feces and (92.9±7.4)% in total. CONCLUSION: DTLL is distributed rapidly in the whole body without obvious accumulation. Most of the DTLL administered is excreted through feces and urine.